The present invention relates to certain 3-substituted 1 H-pyrrolo[2,3-b]pyridine compounds of the formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful in the treatment or prevention of a disease or medical condition mediated through GRK5 selected from heart disease, inflammatory and immunological disease, metabolic disease and cancer.

Background of the invention

G protein-coupled receptor kinases (GRKs) constitute a family of seven mammalian serine/threonine protein kinases that based on sequence homology can be divided into the three subfamilies “GRK1“ (composed of GRK1 and GRK7), “GRK2“ (composed of GRK2 and GRK3) and “GRK4“ (composed of GRK4, GRK5, and GRK6). Whereas GRK1 , GRK4, and GRK7 are expressed in limited tissues such as retina (GRK1 and GRK7) and testis (GRK4), GRK2, GRK3, GRK5, and GRK6 are expressed ubiquitously throughout the body.

GRKs were originally identified by their ability to phosphorylate and desensitize agonist- bound G protein-coupled receptors (GPCRs). GPCRs represent the largest superfamily of transmembrane receptor proteins and facilitate cell sensitivity to a diverse array of external stimuli. As a consequence, GPCR dysregulation is a critical contributor to many diseases such as neurodegeneration, cancer and autoimmune diseases (Hauser et al. , Nat Rev Drug Discov. 2017 Dec;16(12):829-842). Upon ligand binding, GPCRs become activated resulting in downstream intracellular signaling via heterotrimeric G proteins. The phosphorylation of agonist-bound GPCR by GRKs leads to the translocation and binding of b-arrestins to the receptors, inhibiting further G protein activation by blocking receptor-G protein coupling and promoting the internalization of agonist-bound GPCR. Thus, GRK-catalyzed phosphorylation and binding of b-arrestin to the receptors are believed to be the common mechanism to turn off activated GPCRs as an important mechanism for maintaining homeostasis (Wang et al. , Trends Pharmacol Sci. 2018 Apr; 39(4): 367-386).

In addition to their canonical role in GPCR desensitization, recent studies have demonstrated a much broader, non-canonical function for this kinase family including phosphorylation of cytosolic substrates involved in cell signaling pathways stimulated by both GPCRs and non-GPCRs. Moreover, GRKs modulate signaling via phosphorylation- independent functions (Lieu and Koch, Expert Opin Ther Targets. 2019 Mar;23(3):201- 214.). Since GRKs possess multiple biologic functions and have been shown to affect critical physiological and pathophysiological processes, they are considered as drug targets in diseases such as as cardiac hypertrophy and heart failure, obesity and diabetes, atherosclerosis, inflammation and fibrosis, neurodegeneration, opioid tolerance and addiction, and cancer (Hullmann et al., Pharmacol Res. 2016 Aug; 110:52- 64; Gold et al., Circ Res. 2012 Sep 28; 111 (8): 1048-53; Li et al., Diabetes. 2013 Jan;62(1 ):291-8.; Lutz et al., Sci Rep. 2018 May 17;8(1):7745.; Xia et al., PLoS One. 2014 Mar 3;9(3):e90597; Packiriswamy and Parameswaran, Genes Immun. 2015 Sep;16(6):367-77; Murga et al., Front Pharmacol. 2019 Feb 19; 10: 112; Pham et al., Oncotarget. 2020 Apr 21 ;11(16): 1448-1461 ; Jiang et al, Cell Death Dis. 2018 Feb 20;9(3):295; Sommer et al., Sci Rep. 2019 Oct 29;9(1):15548; Hendrickx et al., Front Pharmacol. 2018 Dec 17;9:1484; Marzano et al., Int J Mol Sci. 2021 Feb 15;22(4):1920; Patial et al., J Cell Physiol. 2011 May;226(5): 1323-33; De Lucia et al., Cardiovasc Res. 2021 Feb 9:cvab044; Eguchi et al., Proc Natl Acad Sci U S A. 2021 Feb 2;118(5):e2012854118, Kliewer et al., Nat Commun. 2019 Jan 21 ;10(1):367).

Among the cardiovascular diseases that involve the heart is a pathologic condition termed concentric ventricular hypertrophy (VH). VH can affect both the right ventricular (RVH) as well as the left ventricular (LVH) with the latter being the more common form. In contrast to eccentric VH which is regarded as a physiologic, adaptive process resulting from intense aerobic exercise training or in pregnancy in response to increased blood volume, concentric VH is considered as a maladaptive cardiac remodeling of the heart that is commonly observed in conditions of increased hemodynamic or metabolic stress from various stressors including hypertension, congenital heart defects, valvular defects (aortic coarction or stenosis) and primary defects of the myocardium which directly cause VH (hypertrophic cardiomyopathy). The underlying commonality in these disease states is an increase in pressures that the ventricles try to compensate by undergoing thickening. VH as a result of increased ventricular pressure or volume load is problematic and actually poses a serious health risk which can even lead to heart failure (Nakamura and Sadoshima, Nat Rev Cardiol. 2018 Jul;15(7):387-407; Shimizu and Minamino, J Mol Cell Cardiol. 2016 Aug;97:245-62). In the treatment of LVH, sarcolemmal receptors of the renin-angiotensin-aldosterone (RAAS) system remain the most important targets for the therapeutic treatment of cardiac hypertrophy. However, several trials have shown that a combination of RAAS inhibitors, despite synergistic, may increase the risk of unwanted side effects in some patients (Weir et al., Eur J Heart Fail. 2008 Feb; 10(2): 157-63). A variety of intracellular targets have been identified in maladaptive signaling cascades, but the lack of target- and organ-specific small molecules delays clinical translation (Bisping et al., J Cardiovasc Pharmacol. 2014 Oct;64(4):293-305).

GRK2 and GRK5 are the predominant GRKs in the heart and have been intensively studied for their potential role in cardiac hypertrophy (Gold et al., Circ Res. 2012 Sep 28; 111 (8): 1048-53). It has been observed that GRK5 expression is increased after cardiac injury resulting in worsen disease prognosis and mortality which is clinically associated with maladaptive cardiac remodelling (Dzimiri et al., Eur J Pharmacol. 2004 Apr 12;489(3): 167-77). In contrast, depletion GRK5 in knock-out (KO) mice delays maladaptive cardiac hypertrophy after ventricular pressure-overload (TAC) surgery (Traynham et al., Circ Res. 2015 Dec 4;117(12):1001-12). The development of TAC- induced hypertrophy seems to be dependent on the presence of GRK5 in the nucleus as deletion of its nuclear location sequence (NLS) significantly ameliorates maladaptive cardiac remodeling after TAC (Johnson et al., Mol Cell Biol. 2004 Dec;24(23): 10169-79). This points to a non-canonical function of GRK5 in cardiac hypertrophy which is believed to be triggered by the nuclear translocation of GRK5 upon hypertrophic stress. Subsequent phosphorylation of HDAC5 by GRK5 in the nucleus leads to derepression of MEF2 resulting in activation of MEF2-dependent hypertrophic genes. In addition, nuclear GRK5 interacts and enhances the activity of pro-hypertrophic transcription factors NFkB and NFAT in a kinase-independent manner.

Little has been reported regarding GRK5 inhibitors in clinical development. The anti inflammatory, antiallergic immunomodulator Amlexanox is the only marketed drug that is known to moderately inhibit GRK5 (with an IC50 value of ca. 10 mM) which could contribute to its mechanism of action which, on the other hand, is not well-determined (Homan et al., Molecules. 2014 Oct 22; 19(10): 16937-49, Lee et al., Biomol Ther (Seoul). 2020 Sep 1 ;28(5):482-489).

Compared to GRK5, the role of GRK2 in cardiac hypertrophy is less clear. Although in vitro overexpression of GRK2 is enough to elict hypertrophic response via NFkB and NFAT activation, cardiac-specific transgenic GRK2 mice stressed with TAC undergo maladaptive hypertrophy not significantly different from non-transgenic controls but have increased mortality and decreased cardiac function. Thus, as GRK2 obviously has a role in other maladaptive pathways, dual inhibition of GRK2 and GRK5 could be a therapeutic strategy for pathological hypertrophy and overall cardiovascular health (Huang et al., Antioxid Redox Signal. 2014 Nov 10;21(14):2032-43; Pfleger et al. , Nat Rev Cardiol. 2019 Oct; 16(10):612-622).

It is object to the present invention to provide novel compounds as mono-specific GRK5 or dual-specific GRK2/5 inhibitors and/or pharmaceutically acceptable salts thereof, which can be used as pharmaceutically active agents, and use thereof especially for prophylaxis and/or treatment of selected from heart disease, inflammatory and immunological disease, metabolic disease and cancer as well as compositions comprising at least one of those compounds and/or pharmaceutically acceptable salts thereof as pharmaceutically active ingredients. The objective of the present invention is solved by the teaching of the independent claims. Further advantageous features, aspects and details of the invention are evident from the dependent claims, the description, and the examples of the present application.

The following two compounds are known as such from Chemical Abstracts without the disclosure of the chemical synthesis or any use of such compounds are both compounds are excluded from the scope of the present application:

Chemical Abstracts, May 5. 2004, “(E)-N- benzyl-2-cyano-3-(1 H-pyrrolo[2,3-b]pyridin- 3-yl)acrylamide “

Chemical Abstracts, April 28. 2004, “(E)-N- (1 ,3-benzodioxol-5-yl-methyl)-2-cyano-3- (1 H-pyrrolo[2,3-b]pyridin-3-yl)acrylamide “

Description of the invention

The present invention relates to a compound of the general formula (I) wherein X represents ^H or –CN, Y represents CH or N, R1 – R2 represent independently of each other ^H, ^Ph, ^CH ₃ , ^CF ₃ , ^C ₂ H ₅ , ^C ₃ H ₇ , ^CH(CH ₃ ) ₂ , ^C ₄ H ₉ , ^CH ₂ ^CH(CH ₃ ) ₂ , ^CH(CH ₃ ) ^C ₂ H _5, ^C(CH ₃ ) ₃ , ^C ₅ H ₁₁ , cyclo-C ₃ H ₅ , cyclo-C ₄ H ₇ , cyclo-C ₅ H ₉ , cyclo-C ₆ H ₁₁ , –F, –Cl, –Br, –CN, N N ^OH, ^NH ^Ph, ^R9, ^O ^R10, ^, N N N N N N , , Z4 , R3 represents ^H, ^F, ^Cl, or ^Br; R4 represents ^H, ^CH ₃ , ^CF ₃ , ^C ₂ H ₅ , ^C ₃ H ₇ , ^CH(CH ₃ ) ₂ , ^C ₄ H ₉ , ^CH ₂ ^CH(CH ₃ ) ₂ , ^CH(CH ₃ ) ^C ₂ H _5, ^C(CH ₃ ) ₃ , ^C ₅ H ₁₁ , ^CH ₂ –OH, ^C ₂ H ₄ –OH, ^C ₃ H ₆ –OH, –CN, ^CH ₂ –NH ₂ , ^CH ₂ –NHCH ₃ , ^CH ₂ –NHC ₂ H ₅ , ^CH ₂ –NHC ₃ H ₇ , ^CH ₂ –N(CH ₃ ) ₂ , ^CH ₂ –N(C ₂ H ₅ ) ₂ , ^CH ₂ –N(C ₃ H ₇ ) ₂ , ^C ₂ H ₄ –NH ₂ , ^C ₂ H ₄ –NHCH ₃ ,

LDC-P04312WO10 Application (final).docx ^C ₂ H ₄ –NHC ₂ H ₅ , ^C ₂ H ₄ –NHC ₃ H ₇ , ^C ₂ H ₄ –N(CH ₃ ) ₂ , ^C ₂ H ₄ –N(C ₂ H ₅ ) ₂ , ^C ₂ H ₄ –N(C ₃ H ₇ ) ₂ , ^C ₃ H ₆ –NH ₂ , ^C ₃ H ₆ –NHCH ₃ , ^C ₃ H ₆ –NHC ₂ H ₅ , ^C ₃ H ₆ –NHC ₃ H ₇ , ^C ₃ H ₆ –N(CH ₃ ) ₂ , ^C ₃ H ₆ –N(C ₂ H ₅ ) ₂ , ^C ₃ H ₆ –N(C ₃ H ₇ ) ₂ ; R5 – R7 represent independently of each other –R8, ^CH 8 8 2–R , ^SO ₂ –R , CH ₃ cyclo-C ₃ H ₅ , cyclo-C ₄ H ₇ , cyclo-C ₅ H ₉ , cyclo-C ₆ H ₁₁ , cyclo-C ₇ H ₁₃ , –H, –OH, –OCH ₃ , –OC ₂ H ₅ , –OC ₃ H ₇ , –O–cyclo-C ₃ H ₅ , –OCH(CH ₃ ) ₂ , –OC(CH ₃ ) ₃ , –OC ₄ H ₉ , ^OPh, ^OCH ₂ ^Ph, ^OCPh ₃ , ^CH ₂ –OCH ₃ , ^C ₂ H ₄ –OCH ₃ , ^C ₃ H ₆ –OCH ₃ , ^CH ₂ –OC ₂ H ₅ , ^C ₂ H ₄ –OC ₂ H ₅ , ^C ₃ H ₆ –OC ₂ H ₅ , ^CH ₂ –OC ₃ H ₇ , ^C ₂ H ₄ –OC ₃ H ₇ , ^C ₃ H ₆ –OC ₃ H ₇ , ^CH ₂ –O–cyclo-C ₃ H ₅ , ^C ₂ H ₄ –O–cyclo-C ₃ H ₅ , ^C ₃ H ₆ –O–cyclo-C ₃ H ₅ , ^CH ₂ –OCH(CH ₃ ) ₂ , ^C ₂ H ₄ –OCH(CH ₃ ) ₂ , ^C ₃ H ₆ –OCH(CH ₃ ) ₂ , ^CH ₂ –OC(CH ₃ ) ₃ , ^C ₂ H ₄ –OC(CH ₃ ) ₃ , ^C ₃ H ₆ –OC(CH ₃ ) ₃ , ^CH ₂ –OC ₄ H ₉ , ^C ₂ H ₄ –OC ₄ H ₉ , ^C ₃ H ₆ –OC ₄ H ₉ , ^CH ₂ –OPh, ^C ₂ H ₄ –OPh, ^C ₃ H ₆ –OPh, ^CH ₂ –OCH ₂ ^Ph, ^C ₂ H ₄ –OCH ₂ ^Ph, ^C ₃ H ₆ –OCH ₂ ^Ph, –SH, –SCH ₃ , –SC ₂ H ₅ , –SC ₃ H ₇ , –S–cyclo-C ₃ H ₅ , –SCH(CH ₃ ) ₂ , –SC(CH ₃ ) ₃ , –F, –Cl, –Br, –I, –CN, –COCH ₃ , –COC ₂ H ₅ , –COC ₃ H ₇ , –CO–cyclo-C ₃ H ₅ , –COCH(CH ₃ ) ₂ , –COC(CH ₃ ) ₃ , –COOH, –COOCH ₃ , –COOC ₂ H ₅ , –COOC ₃ H ₇ , –COO–cyclo-C ₃ H ₅ , –COOCH(CH ₃ ) ₂ , –COOC(CH ₃ ) ₃ , –OOC–CH ₃ , –OOC–C ₂ H ₅ , –OOC–C ₃ H ₇ , –OOC–cyclo-C ₃ H ₅ , –OOC–CH(CH ₃ ) ₂ , –OOC–C(CH ₃ ) ₃ , –CONH ₂ , –CONHCH ₃ , –CONHC ₂ H ₅ , –CONHC ₃ H ₇ , –CONH–cyclo-C ₃ H ₅ , –CONH[CH(CH ₃ ) ₂ ], –CONH[C(CH ₃ ) ₃ ], –CON(CH ₃ ) ₂ , –CON(C ₂ H ₅ ) ₂ , –CON(C ₃ H ₇ ) ₂ , –CON(cyclo-C ₃ H ₅ ) ₂ , –CON[CH(CH ₃ ) ₂ ] ₂ , –CON[C(CH ₃ ) ₃ ] ₂ , –NHCOCH ₃ , –NHCOC ₂ H ₅ , –NHCOC ₃ H ₇ , –NHCO–cyclo-C ₃ H ₅ , –NHCO–CH(CH ₃ ) ₂ , –NHCO–C(CH ₃ ) ₃ , –NHCO–OCH ₃ , –NHCO–OC ₂ H ₅ , –NHCO–OC ₃ H ₇ , –NHCO–O–cyclo-C ₃ H ₅ , –NHCO–OCH(CH ₃ ) ₂ , –NHCO–OC(CH ₃ ) ₃ , –NH ₂ , –NHCH ₃ , –NHC ₂ H ₅ , –NHC ₃ H ₇ , –NH–cyclo-C ₃ H ₅ , –NHCH(CH ₃ ) ₂ , –NHC(CH ₃ ) ₃ , –N(CH ₃ ) ₂ , –N(C ₂ H ₅ ) ₂ , –N(C ₃ H ₇ ) ₂ , –N(cyclo-C ₃ H ₅ ) ₂ , –N[CH(CH ₃ ) ₂ ] ₂ , –N[C(CH ₃ ) ₃ ] ₂ , –SOCH ₃ , –SOC ₂ H ₅ , –SOC ₃ H ₇ , –SO–cyclo-C ₃ H ₅ , –SOCH(CH ₃ ) ₂ , –SOC(CH ₃ ) ₃ , –SO ₂ CH ₃ , –SO ₂ C ₂ H ₅ , –SO ₂ C ₃ H ₇ , –SO ₂ –cyclo-C ₃ H ₅ , –SO ₂ CH(CH ₃ ) ₂ , –SO ₂ C(CH ₃ ) ₃ , –SO ₃ H, –SO ₃ CH ₃ , –SO ₃ C ₂ H ₅ , –SO ₃ C ₃ H ₇ , –SO ₃ –cyclo-C ₃ H ₅ , –SO ₃ CH(CH ₃ ) ₂ , –SO ₃ C(CH ₃ ) ₃ , –SO ₂ NH ₂ , –SO ₂ NHCH ₃ , –SO ₂ NHC ₂ H ₅ , –SO ₂ NHC ₃ H ₇ , –SO ₂ NH–cyclo-C ₃ H ₅ , –SO ₂ NHCH(CH ₃ ) ₂ , –SO ₂ NHC(CH ₃ ) ₃ , –SO ₂ N(CH ₃ ) ₂ , –SO ₂ N(C ₂ H ₅ ) ₂ , –SO ₂ N(C ₃ H ₇ ) ₂ , –SO ₂ N(cyclo-C ₃ H ₅ ) ₂ , –SO ₂ N[CH(CH ₃ ) ₂ ] ₂ , –SO ₂ N[C(CH ₃ ) ₃ ] ₂ , ^CH ₂ –SO ₂ NH ₂ , ^CH ₂ –SO ₂ NHCH ₃ , ^CH ₂ –SO ₂ NHC ₂ H ₅ , ^CH ₂ –SO ₂ NHC ₃ H ₇ , ^CH ₂ –SO ₂ NH–cyclo-C ₃ H ₅ , ^CH ₂ –SO ₂ NHCH(CH ₃ ) ₂ , ^CH ₂ –SO ₂ NHC(CH ₃ ) ₃ , ^CH ₂ –SO ₂ N(CH ₃ ) ₂ , ^CH ₂ –SO ₂ N(C ₂ H ₅ ) ₂ , ^CH ₂ –SO ₂ N(C ₃ H ₇ ) ₂ , ^CH ₂ –SO ₂ N(cyclo-C ₃ H ₅ ) ₂ , ^CH ₂ –SO ₂ N[CH(CH ₃ ) ₂ ] ₂ , ^CH ₂ –SO ₂ N[C(CH ₃ ) ₃ ] ₂ , ^O–S(=O)CH ₃ , ^O–S(=O)C ₂ H ₅ , ^O–S(=O)C ₃ H ₇ , ^O–S(=O)–cyclo-C ₃ H ₅ , ^O–S(=O)CH(CH ₃ ) ₂ , ^O–S(=O)C(CH ₃ ) ₃ , –S(=O)(=NH)CH ₃ , –S(=O)(=NH)C ₂ H ₅ , –S(=O)(=NH)C ₃ H ₇ , –S(=O)(=NH)–cyclo-C ₃ H ₅ , –S(=O)(=NH)CH(CH ₃ ) ₂ , –S(=O)(=NH)C(CH ₃ ) ₃ , ^NH–SO ₂ –CH ₃ , ^NH–SO ₂ –C ₂ H ₅ , ^NH–SO ₂ –C ₃ H ₇ , ^NH–SO ₂ –cyclo-C ₃ H ₅ , ^NH–SO ₂ –CH(CH ₃ ) ₂ , ^NH–SO ₂ –C(CH ₃ ) ₃ , ^O–SO ₂ –CH ₃ , ^O–SO ₂ –C ₂ H ₅ , ^O–SO ₂ –C ₃ H ₇ , ^O–SO ₂ –cyclo-C ₃ H ₅ , ^O–SO ₂ –CH(CH ₃ ) ₂ , ^O–SO ₂ –C(CH ₃ ) ₃ , –OCH ₂ F, –OCHF ₂ –OCF ₃ , ^CH ₂ –OCF ₃ , ^C ₂ H ₄ –OCF ₃ , ^C ₃ H ₆ –OCF ₃ , –OC ₂ F ₅ , ^CH ₂ –OC ₂ F ₅ , ^C ₂ H ₄ –OC ₂ F ₅ , ^C ₃ H ₆ –OC ₂ F ₅ , –O–COOCH ₃ , –O–COOC ₂ H ₅ , –O–COOC ₃ H ₇ , –O–COO–cyclo-C ₃ H ₅ , –O–COOCH(CH ₃ ) ₂ , –O–COOC(CH ₃ ) ₃ , –NH–CO–NH ₂ , –NH–CO–NHCH ₃ , –NH–CO–NHC ₂ H ₅ , –NH–CO–NHC ₃ H ₇ , –NH–C(=NH)–NH ₂ , –NH–CO–N(C ₃ H ₇ ) ₂ , –NH–CO–NH[CH(CH ₃ ) ₂ ], –NH–CO–NH[C(CH ₃ ) ₃ ], –NH–CO–N(CH ₃ ) ₂ , –NH–CO–N(C ₂ H ₅ ) ₂ , –NH–CO–NH–cyclo-C ₃ H ₅ , –NH–CO–N(cyclo-C ₃ H ₅ ) ₂ , –NH–CO–N[CH(CH ₃ ) ₂ ] ₂ , –NH–C(=NH)–NHCH ₃ , –NH–C(=NH)–NHC ₂ H ₅ , –NH–C(=NH)–NHC ₃ H ₇ , –O–CO–NH–cyclo-C ₃ H ₅ , –NH–C(=NH)–NH–cyclo-C ₃ H ₅ , –NH–C(=NH)–NH[CH(CH ₃ ) ₂ ], –O–CO–NH[CH(CH ₃ ) ₂ ], –NH–C(=NH)–NH[C(CH ₃ ) ₃ ], –NH–C(=NH)–N(CH ₃ ) ₂ , –NH–C(=NH)–N(C ₂ H ₅ ) ₂ , –NH–C(=NH)–N(C ₃ H ₇ ) ₂ , –NH–C(=NH)–N(cyclo-C ₃ H ₅ ) ₂ , –O–CO–NHC ₃ H ₇ , –NH–C(=NH)–N[CH(CH ₃ ) ₂ ] ₂ , –NH–C(=NH)–N[C(CH ₃ ) ₃ ] ₂ , –O–CO–NH ₂ , –O–CO–NHCH ₃ , –O–CO–NHC ₂ H ₅ , –O–CO–NH[C(CH ₃ ) ₃ ], –O–CO–N(CH ₃ ) ₂ , –O–CO–N(C ₂ H ₅ ) ₂ , –O–CO–N(C ₃ H ₇ ) ₂ , –O–CO–N(cyclo-C ₃ H ₅ ) ₂ , –O–CO–N[CH(CH ₃ ) ₂ ] ₂ , –O–CO–N[C(CH ₃ ) ₃ ] ₂ , –O–CO–OCH ₃ , –O–CO–OC ₂ H ₅ , –O–CO–OC ₃ H ₇ , –O–CO–O–cyclo-C ₃ H ₅ , –O–CO–OCH(CH ₃ ) ₂ , –O–CO–OC(CH ₃ ) ₃ , ^CH ₂ F, ^CHF ₂ , ^CF ₃ , ^CH ₂ ^CH ₂ F, ^CH ₂ ^CHF ₂ , ^CH ₂ ^CF ₃ , cyclo-C ₈ H ₁₅ , ^Ph, ^CH ₂ ^Ph, ^CH ₂ ^CH ₂ ^Ph, ^CH=CH ^Ph, ^CPh ₃ , ^CH ₃ , ^C ₂ H ₅ , ^C ₃ H ₇ , ^CH(CH ₃ ) ₂ , ^C ₄ H ₉ , ^CH ₂ ^CH(CH ₃ ) ₂ , ^CH(CH ₃ ) ^C ₂ H _5, ^C(CH ₃ ) ₃ , ^C ₅ H ₁₁ , ^CH(CH ₃ )–C ₃ H ₇ , –CH ₂ –CH(CH ₃ )–C ₂ H ₅ , –CH(CH ₃ )–CH(CH ₃ ) ₂ , –C(CH ₃ ) ₂ –C ₂ H ₅ , –CH ₂ –C(CH ₃ ) ₃ , –CH(C ₂ H ₅ ) ₂ , –C ₂ H ₄ –CH(CH ₃ ) ₂ , ^C ₆ H ₁₃ , ^C ₇ H ₁₅ , ^C ₈ H ₁₇ , –C ₃ H ₆ –CH(CH ₃ ) ₂ , –C ₂ H ₄ –CH(CH ₃ )–C ₂ H ₅ , –CH(CH ₃ )–C ₄ H ₉ , –CH ₂ –CH(CH ₃ )–C ₃ H ₇ , –CH(CH ₃ )–CH ₂ –CH(CH ₃ ) ₂ , –CH(CH ₃ )–CH(CH ₃ )–C ₂ H ₅ , –CH ₂ –CH(CH ₃ )–CH(CH ₃ ) ₂ , –CH ₂ –C(CH ₃ ) ₂ –C ₂ H ₅ , –C(CH ₃ ) ₂ –C ₃ H ₇ , –C(CH ₃ ) ₂ –CH(CH ₃ ) ₂ , –C ₂ H ₄ –C(CH ₃ ) ₃ , –CH(CH ₃ )–C(CH ₃ ) ₃ , ^CH=CH ₂ , ^CH ₂ ^CH=CH ₂ , ^C(CH ₃ )=CH ₂ , ^CH=CH ^CH ₃ , –C ₂ H ₄ –CH=CH ₂ , –CH ₂ –CH=CH–CH ₃ , –CH=CH–C ₂ H ₅ , –CH ₂ –C(CH ₃ )=CH ₂ , –CH(CH ₃ )–CH=CH, –CH=C(CH ₃ ) ₂ , –C(CH ₃ )=CH–CH ₃ , –CH=CH–CH=CH ₂ , ^C ₃ H ₆ –CH=CH ₂ , –C ₂ H ₄ –CH=CH–CH ₃ , –CH ₂ –CH=CH–C ₂ H ₅ , –CH=CH–C ₃ H ₇ , –CH=CH–CH=CH–CH ₃ , –C ₂ H ₄ –C(CH ₃ )=CH ₂ , –CH ₂ –CH(CH ₃ )–CH=CH ₂ , –CH(CH ₃ )–CH ₂ –CH=CH ₂ , –CH ₂ –CH=C(CH ₃ ) ₂ , –CH ₂ –C(CH ₃ )=CH–CH ₃ , –CH(CH ₃ )–CH=CH–CH ₃ , –CH=CH–CH(CH ₃ ) ₂ , –CH=C(CH ₃ )–C ₂ H ₅ , R ⁵ and R ⁶ , or R ⁶ and R ⁷ form together

R ⁹ represents -H, R ¹⁰ represents -CH _3I -CF _3I C ₂ H _5I -C ₃ H _7I CH(CH ₃ ) _2I -C ₄ H ₉ , -CH ₂ -CH(CH ₃ )2, -CH(CH ₃ )-C ₂ H _5, -C(CH ₃ ) _3I C ₅ H ₁₁ -(CH ₂ )n-NH ₂ , -(CH ₂ ) _n -NHCH ₃ , -(CH ₂ ) _n -NHC ₂ H ₅ , (CH ₂ )n-NHC ₃ H ₇ , (CH ₂ )n-N(CH ₃ ) ₂ , -(CH ₂ )n-N(C ₂ H ₅ ) ₂ , (CH ₂ )n-N(C ₃ H ₇ ) ₂ ,

R ¹¹ and R ¹² represent independently of each other -H, -CH ₃ , -C ₂ H ₅ , -C ₃ H ₇ ,

-CH(CH ₃ ) ₂ , -CF _3I -(CH ₂ ) _m- NH ₂ , -(CH ₂ ) _m- NHCH ₃ , -(CH ₂ ) _m- NHC ₂ H ₅ , -(CH ₂ ) _m- NHC ₃ H ₇ , -(CH ₂ ) _m- N(CH ₃ ) ₂ , -(CH ₂ ) _m- N(C ₂ H ₅ ) ₂ , -(CH ₂ ) _m- N(C ₃ H ₇ ) ₂ , -OCH ₃ , -OC ₂ H _S , -OC ₃ H ₇ , -O-cyclo-CsHs, -OCH(CH ₃ ) ₂ , -F, -Cl, -Br,

-CN, -(CH ₂ ) _m -S0 ₂ CH ₃ , -(CH ₂ ) _m -S0 ₂ C ₂ H ₅ , -(CH ₂ ) _m -S0 ₂ C ₃ H ₇ ,

-(CH ₂ ) _m -SO^cyclo-C ₃ H ₅ , -(CH ₂ ) _m -S0 ₂ CH(CH ₃ ) ₂ , -(CH ₂ ) _m -S0 ₂ C(CH ₃ ) ₃ ,

-0-(CH ₂ ) _m- NH ₂ , -0-(CH ₂ ) _m- NHCH ₃ , -0-(CH ₂ ) _m- NHC ₂ H ₅ , -0-(CH ₂ ) _m- NHC ₃ H ₇ ,

-0-(CH ₂ ) _m- N(CH ₃ ) ₂ , -0-(CH ₂ ) _m- N(C ₂ H ₅ ) ₂ , -0-(CH ₂ ) _m- N(C ₃ H ₇ ) ₂ , -NHCOCH ₃ , (CH ₂ ) _m NHCOCHs, (CH ₂ ) _m -NHCOC ₂ H ₅ , (CH ₂ ) _m NHCO-cyclo-C ₃ H ₅ ,

-(CH ₂ ) _m- NHCOC ₃ H ₇ , -(CH ₂ ) _m- NHCO-CH(CH ₃ ) ₂ , -(CH ₂ ) _m- NHCO-CH=CH ₂ , -S0 ₂ NH _2I -S0 ₂ NHCH _3I -S0 ₂ NHC ₂ H _5I -S0 ₂ NHC ₃ H _7I -S0 ₂ NH-cyclo-C ₃ H _5l -S0 ₂ NHCH(CH ₃ ) _2I -S0 ₂ N(CH ₃ ) _2I -S0 ₂ N(C ₂ H ₅ ) _2I -S0 ₂ N(C ₃ H ₇ ) _2I

-S0 ₂ N(cyclo-C ₃ H ₅ ) ₂ , -S0 ₂ N[CH(CH ₃ ) ₂ ] ₂ , -NH-SO^CH ₃ , -NH-S0 ₂ -C ₂ H ₅ , -NH-S0 ₂ -C ₃ H _7I -NH-S0 ₂ -cyclo-C ₃ H ₅ , -NH-S0 ₂ -CH(CH ₃ ) ₂ , -CONH ₂ ,

-SOCHs, -SOC ₂ H _5I -SOC ₃ H _7I -SO-cyclo-C ₃ H ₅ , -SOCH(CH ₃ ) ₂ , -SCH ₃ , -SOCF _3I -S0 ₂ CF _3I or -SO(NH)CH ₃ ;

R ^N1 and R ^N2 represent independently of each other -H, -CH ₃ , -C ₂ H ₅ , -C ₃ H ₇ , -CH(CH ₃ ) ₂ , cyclo-C ₃ H ₅ , cyclo-C ₄ H ₇ , cyclo-CsHg, cyclo-CeHn, -C ₄ H ₉ ,

-C(CH ₃ ) _3I -CH ₂ -CH(CH ₃ ) ₂ , -CH(CH ₃ )-C ₂ H _5, -C ₅ H- _1-1 , -Ph, -CH _2- Ph,

-CH=CH ₂ , -CH ₂ -CH=CH ₂ , -CH=CH-CH ₃ , -CºCH, -CH ₂ -CºCH, -CºC-CH ₃ , -COCHs, -COC ₂ H _5I -COC ₃ H _7I -CO-cyclo-C ₃ H ₅ , -COCH(CH ₃ ) ₂ , -COOCH ₃ , -COOC ₂ H _5I -COOC ₃ H _7I -COO-cyclo-CsHs, -COOCH(CH ₃ ) ₂ , -COOC(CH ₃ ) ₃ , Z ¹ - Z ⁴ represent independently of each other -H, -CH ₃ , -C ₂ H ₅ , -C ₃ H ₇ ,

-CH(CH ₃ ) ₂ , -Ph, -COCH ₃ , -COC ₂ H ₅ , -COOH, -COOCH ₃ , -COOC ₂ H _5I -NH ₂ , -NHCHS, -NHC ₂ H _5I -N(CH ₃ ) _2I -N(C ₂ H ₅ )2, -CH ₂ -NH ₂ , -SO ₃ H,

-F, -Cl, -Br, -I, -CN, -CF ₃ , -OCF ₃ , -OH, -OCH ₃ , or -OC ₂ H ₅ ; m is an integer selected from 0, 1 , 2, 3, or 4; n is an integer selected from 1 , 2, 3, or 4; p is an integer selected from 0, 1 , 2, 3, or 4; q is an integer selected from 1 , 2, 3, or 4; with the proviso that when X is -H at least one of R ¹ - R ³ is not -H; and when R ⁴ is

-H, at least one of R ¹ - R ³ and R ⁵ - R ⁷ is not -H; and the following two compounds are excluded from the scope of the present application:

(E)-N-benzyl-2-cyano-3-(1 H-pyrrolo[2,3-b]pyridin-3-yl)acrylamide

(E)-N-(1 ,3-benzodioxol-5-yl-methyl)-2-cyano-3-(1 H-pyrrolo[2,3-b]pyridin-3-yl)acrylamide, or an enantiomer, a stereoisomeric form, a mixture of enantiomers, a diastereomer, a mixture of diastereomers, a hydrate, a solvate, an acid salt form, a tautomer, or a racemate of the above mentioned compound, or a pharmaceutically acceptable salt thereof .

Preferred are compounds wherein R ⁴ is different from hydrogen (-H). In case R ⁴ is hydrogen one or at least one of the substituents R ¹ - R ³ and R ⁵ - R ⁷ is not hydrogen and preferably two or three or more than three substituents R ¹ - R ³ and R ⁵ - R ⁷ are not hydrogen. Even more preferred are the compounds wherein one or at least one of the substituents R ⁴ - R ⁷ is not hydrogen. Still more preferred are the compounds wherein one or at least one of the substituents R ¹ - R ⁴ is not hydrogen. Most preferred are the compounds wherein one or at least one of the substituents R ¹ - R ³ is not hydrogen and wherein one or at least one of the substituents R ⁵ - R ⁷ is not hydrogen. Preferably, the compounds of general formula (I) as defined herein are under the proviso that when X is -H at least one of R ¹ - R ³ is not -H and under the second proviso that R ⁵ , R ⁶ and R ⁷ are not -H at the same time or preferably under the further proviso that at least one of R ¹ - R ³ is not -H, when R ^s and R ⁶ or R ⁶ and R ⁷ form together ~~0 ; more preferably under the further proviso that when X is -CN or when R ⁴ is -H or -C ₂ H ₅ or -CH ₂ OH or -C ₂ H ₄ OH, at least one of R ⁵ , R ⁶ and R ⁷ is different from -H or still more preferably under the second proviso that in case X is -CN and R ⁴ is -FI or -C ₂ Fl5 or -CFI ₂ OFI or — C ₂ H ₄ OH, at least one of R ⁵ , R ⁶ and R ⁷ is different from -H.

Preferably, a compound of the general formula (la) wherein

X represents -H or -CN,

R ¹ - R ² represent independently of each other -H, -Ph, -CH ₃ , -CF ₃ , -C2H5,

C ₃ H _7I CH(CH ₃ ) _2I C ₄ H _9I CH ₂ CH(CH ₃ ) _2I CH(CH ₃ ) C ₂ H _5, C(CH ₃ ) _3I -C5H11, cyclo-C ₃ H ₅ , cyclo-C4H ₇ , cyclo-C ₅ H ₉ , cyclo-C ₆ Hn, -F, -Cl, -Br, -CN,

OH, NH Ph, R ⁹ O R ¹⁰ ,

R ³ represents -H, -F, -Cl, or -Br;

R ⁴ represents -H, -CH ₃ , -CF ₃ , -C ₂ H ₅ , -C ₃ H ₇ , -CH(CH ₃ ) ₂ , -C ₄ H ₉ ,

-CH ₂ -CH(CH ₃ ) _2I -CH(CH ₃ )-C ₂ H _5, -C(CH ₃ ) _3I -C ₅ H ₁₁ , -CH^OH, -C ₂ H ₄ -OH,

-C ₃ H _S -OH, -CN, -CH^NH _2I -CH^NHCH _S , -CH^NHC ₂ H _5I -CH^NHC ₃ H _7I -CH^N(CH ₃ ) _2I -CH^N(C ₂ H ₅ ) ₂ , -CH^N(C ₃ H ₇ ) _2I -C ₂ H ₄ -NH ₂ , -C ₂ H ₄ -NHCH ₃ ,

-C ₂ H ₄ -NHC ₂ H ₅ , -C ₂ H ₄ -NHC ₃ H ₇ , -C ₂ H ₄ -N(CH ₃ ) ₂ , -C ₂ H ₄ -N(C ₂ H ₅ ) ₂ ,

-C ₂ H ₄ -N(C ₃ H ₇ ) ₂ , -C ₃ H ₆ -NH ₂ , -C ₃ H ₆ -NHCH ₃ , -C ₃ H ₆ -NHC ₂ H ₅ ,

-C ₃ H _S -NHC ₃ H ₇ , -C ₃ H ₆ -N(CH ₃ ) _2I -C ₃ H ₆ -N(C ₂ H ₅ ) _{2I -} C ₃ H ₆ -N(C ₃ H ₇ ) ₂ ; R ⁵ - R ⁷ represent independently of each other -R ⁸ , cyclo-C ₃ H ₅ , cyclo-C ₄ H ₇ , cyclo-C ₅ H ₉ , cyclo-C ₆ Hn, cyclo-C ₇ Hi ₃ ,

-H, -OH, -OCH ₃ , -0C ₂ H ₅ , -OC ₃ H ₇ , -0-cyclo-C ₃ H ₅ , -OCH(CH ₃ ) ₂ ,

-OC(CH ₃ ) ₃ , -OC ₄ H _9I -OPh, -OCH _2- Ph, -OCPh ₃ , -CHHCCH ₃ , -C ₂ H ₄ -OCH ₃ , -C ₃ H ₆ -OCH ₃ , -CH^OC ₂ H ₅ , -C ₂ H ₄ -OC ₂ H _5I -C ₃ H ₆ -OC ₂ H ₅ , -CH^OC ₃ H ₇ ,

— C ₂ H ₄ — OC ₃ H ₇ , — C ₃ H ₆ — OC ₃ H _{7I —} CH ₂ — 0— cyclo-C ₃ H5, — C ₂ H ₄ — O— cyclo-C ₃ H5, -C ₃ H _s -0-cyclo-C ₃ H ₅ , -CH^OCH(CH ₃ ) ₂ , -C ₂ H ₄ -OCH(CH ₃ ) ₂ , -C ₃ H ₆ -OCH(CH ₃ ) ₂ ,

-CH^OC(CH ₃ ) ₃ , -C ₂ H ₄ -OC(CH ₃ ) ₃ , -C ₃ H ₆ -OC(CH ₃ ) ₃ , -CH^OC ₄ H ₉ ,

-C ₂ H ₄ -OC ₄ H ₉ , -C ₃ H ₆ -OC ₄ H _9I -CH ₂ -OPh, -C ₂ H ₄ -OPh, -C ₃ H ₆ -OPh, -CHHCCH _2- Ph, -C ₂ H ₄ -OCH _2- Ph, -C ₃ H ₆ -OCH _2- Ph, -SH, -SCH ₃ , -SC ₂ H ₅ , -SC ₃ H ₇ , -S-cyclo-C ₃ H ₅ , -SCH(CH ₃ ) ₂ , -SC(CH ₃ ) ₃ , -F, -Cl, -Br, -I, -CN, -COCHs, -COC ₂ H ₅ , -COC ₃ H _7I -CO-cyclo-CsHs, -COCH(CH ₃ ) ₂ , -COC(CH ₃ ) ₃ , -COOH, -COOCH _S , -COOC ₂ H ₅ , -COOC ₃ H _7I -COO-cyclo-CsHs, -COOCH(CH ₃ ) _2I -COOC(CH ₃ ) _3I -OOC-CH ₃ , -OOC-C2H5, -OOC-C ₃ H ₇ ,

-OOC-cyclo-C ₃ H ₅ , -OOC-CH(CH ₃ ) ₂ , -OOC-C(CH ₃ ) ₃ , -CONH ₂ ,

-CONHCHs, -CONHC ₂ H ₅ , -CONHC ₃ H ₇ , -CONH-cyclo-C ₃ H ₅ ,

-CONH[CH(CH ₃ ) ₂ ], -CONH[C(CH ₃ ) ₃ ], -CON(CH ₃ ) _2I -CON(C ₂ H ₅ )2,

-CON(C ₃ H ₇ ) _2I -CON(cyclo-C ₃ H ₅ ) ₂ , -CON[CH(CH ₃ ) ₂ ] ₂ , -CON[C(CH ₃ ) ₃ ] ₂ ,

-NHCOCHa, -NHCOC ₂ H ₅ , -NHCOC ₃ H ₇ , -NHCO-cyclo-C ₃ H ₅ ,

-NHCO-CH(CH ₃ ) _2I -NHCO-C(CH ₃ ) _3I -NHCO-OCH ₃ , -NHCO-OC ₂ H ₅ ,

-NHCO-OC ₃ H _7I -NHCO-O-cyclo-CsHs, -NHCO-OCH(CH ₃ ) ₂ , -NHCO-OC(CH ₃ ) ₃ , -NH _2I -NHCH _S , -NHC ₂ H ₅ , -NHC ₃ H _7I -NH-cyclo-CsHs, -NHCH(CH ₃ ) ₂ ,

-NHC(CH ₃ ) ₃ , -N(CH ₃ ) ₂ , -N(C ₂ H ₅ ) ₂ , -N(C ₃ H ₇ ) ₂ , -N(cyclo-C ₃ H ₅ )2,

-N[CH(CH ₃ ) ₂ ] ₂ , -N[C(CH ₃ ) ₃ ] ₂ , -SOCH _S , -SOC ₂ H ₅ , -SOC ₃ H _7I -SO-cyclo-C ₃ H ₅ ,

-SOCH(CH ₃ ) _2I -SOC(CH ₃ ) _3I -S0 ₂ CH _3I -SO ₂ C ₂ H ₅ , -SO ₂ C ₃ H ₇ ,

-S0 ₂ -cyclo-C ₃ H ₅ , -S0 ₂ CH(CH ₃ ) ₂ , -S0 ₂ C(CH ₃ ) ₃ , -S0 ₃ H, -S0 ₃ CH ₃ ,

-S0 ₃ C ₂ H _5I -S0 ₃ C ₃ H _7I -S0 ₃ -cyclo-C ₃ H ₅ , -S0 ₃ CH(CH ₃ ) ₂ , -S0 ₃ C(CH ₃ ) ₃ ,

-SO ₂ NH ₂ , -S0 ₂ NHCH ₃ , -SO ₂ NHC ₂ H ₅ , -S0 ₂ NHC ₃ H _7I -S0 ₂ NH-cyclo-C ₃ H ₅ , -S0 ₂ NHCH(CH ₃ ) _2I -S0 ₂ NHC(CH ₃ ) ₃ , -S0 ₂ N(CH ₃ ) _2I -S0 ₂ N(C ₂ H ₅ )2,

-S0 ₂ N(C ₃ H ₇ ) ₂ , -S0 ₂ N(cyclo-C ₃ H ₅ )2, -S0 ₂ N[CH(CH ₃ ) ₂ ] ₂ , -S0 ₂ N[C(CH ₃ ) ₃ ] ₂ ,

-CH^SO ₂ NH ₂ , -CH^SO ₂ NHCH ₃ , -CH^SO ₂ NHC ₂ H ₅ , -CH^SO ₂ NHC ₃ H ₇ ,

CH2-S0 ₂ NH-cyclo-C ₃ H ₅ , CH^S0 ₂ NHCH(CH ₃ ) ₂ , CH^S0 ₂ NHC(CH ₃ ) _3I

-CH^S0 ₂ N(CH ₃ ) _2I -CH^S0 ₂ N(C ₂ H ₅ )2, -CH^S0 ₂ N(C ₃ H ₇ ) _2I

-CH^S0 ₂ N(cyclo-C ₃ H ₅ )2, -CH^S0 ₂ N[CH(CH ₃ ) ₂ ] ₂ , -CH^S0 ₂ N[C(CH ₃ ) ₃ ] ₂ ,

-0-S(=0)CH _3I -0-S(=0)C ₂ H _5I -0-S(=0)C ₃ H _7I -0-S(=0)-cyclo-C ₃ H ₅ ,

-0-S(=0)CH(CH ₃ ) _2I -0-S(=0)C(CH ₃ ) _3I -S(=0)(=NH)CH _3I -S(=0)(=NH)C ₂ H _5I

-S(=0)(=NH)C ₃ H _7I -S(=0)(=NH)-cyclo-C ₃ H ₅ , -S(=0)(=NH)CH(CH ₃ ) ₂ ,

-S(=0)(=NH)C(CH ₃ ) _3I -NH-S0 ₂ -CH _3I -NH-SO2-C2H5, -NH-SO ₂ -C ₃ H ₇ ,

-NH-S0 ₂ -cyclo-C ₃ H ₅ , -NH-S0 ₂ -CH(CH ₃ ) ₂ , -NH-S0 ₂ -C(CH ₃ ) ₃ , -0-S0 ₂ -CH ₃ ,

-O-SO2-C2H5, -0-S0 ₂ -C ₃ H ₇ , -0-S0 ₂ -cyclo-C ₃ H ₅ , -0-S0 ₂ -CH(CH ₃ ) ₂ ,

_0-S0 ₂ -C(CH ₃ ) ₃ , -OCH2F, -OCHF2 -OCF _3I -CH^OCF _S ,

-C ₂ H ₄ -OCF ₃ , -C ₃ H ₆ -OCF _3I -OC2F5, -CH^OC ₂ F ₅ , -C2H4-OC2F5, -C ₃ H ₆ -OC ₂ F ₅ , -0-C00CH ₃ , -O-COOC2H5, -0-C00C ₃ H ₇ , -O-COO-cyclo-CsHs,

-0-C00CH(CH ₃ ) _2I -0-C00C(CH ₃ ) _3I -NH-CO-NH2, -NH-CO-NHCH ₃ ,

-NH-CO-NHC2H5, -NH-CO-NHC ₃ H _7I -NH-C(=NH)-NH _2I -NH-C0-N(C ₃ H ₇ ) ₂ ,

-NH-CO-NH[CH(CH ₃ ) ₂ ], -NH-CO-NH[C(CH ₃ ) ₃ ], -NH-CO-N(CH ₃ ) _2I

-NH-CO-N(C ₂ H ₅ )2, -NH-CO-NH-cyclo-CsHs, -NH-CO-N(cyclo-C ₃ H ₅ ) ₂ ,

-NH-C0-N[CH(CH ₃ ) ₂ ] ₂ , -NH-C(=NH)-NHCH _3I -NH-C(=NH)-NHC ₂ H _5I

-NH-C(=NH)-NHC ₃ H _7I -0-CO-NH-cyclo-C ₃ H ₅ , -NH-C(=NH)-NH-cyclo-C ₃ H ₅ , -NH-C(=NH)-NH[CH(CH ₃ ) ₂ ], -0-C0-NH[CH(CH ₃ ) ₂ ], -NH-C(=NH)-NH[C(CH ₃ ) ₃ ],

-NH-C(=NH)-N(CH ₃ ) ₂ , -NH-C(=NH)-N(C ₂ H ₅ ) ₂ , -NH-C(=NH)-N(C ₃ H ₇ ) _2I -NH-C(=NH)-N(cyclo-C ₃ H ₅ ) ₂ , -O-CO-NHC3H7, -NH-C(=NH)-N[CH(CH ₃ ) ₂ ] ₂ , -NH-C(=NH)-N[C(CH ₃ ) ₃ ] _2I -O-CO-NH ₂ , -O-CO-NHCH ₃ , -0-C0-NHC ₂ H _5I

-0-CO-NH[C(CH ₃ ) ₃ ], -0-C0-N(CH ₃ ) _2I -0-C0-N(C ₂ H ₅ ) _2I -0-C0-N(C ₃ H ₇ ) _2I

-0-CO-N(cyclo-C ₃ H ₅ ) ₂ , -0-C0-N[CH(CH ₃ ) ₂ ] ₂ , -0-C0-N[C(CH ₃ ) ₃ ] ₂ , -0-C0-0CH ₃ , -0-C0-0C ₂ H _5I -0-C0-0C ₃ H _7I -O-CO-O-cyclo-CsHs, -0-C0-0CH(CH ₃ ) ₂ ,

-0-C0-0C(CH ₃ ) _3I -CH ₂ F, -CHF ₂ , -CF ₃ , -CH ₂ -CH ₂ F, -CH ₂ -CHF ₂ ,

-CH _2- CF ₃ , cyclo-C ₈ Hi ₅ , -Ph, -CH _2- Ph, -CH _2- CH _2- Ph, -CH=CH-Ph, -CPh ₃ , -CH ₃ , -C ₂ H _5I -C ₃ H _7I -CH(CH ₃ ) _2I -C ₄ H _9I -CH ₂ -CH(CH ₃ ) _2I

-CH(CH ₃ )-C ₂ H _5, -C(CH ₃ ) _3I -C ₅ HH, -CH(CH ₃ )-C ₃ H _7I -CH ₂ -CH(CH ₃ )-C ₂ H ₅ ,

-CH(CH ₃ )-CH(CH ₃ ) _2I -C(CH ₃ ) ₂ -C ₂ H _5I -CH ₂ -C(CH ₃ ) _3I -CH(C ₂ H ₅ ) _2I

-C ₂ H ₄ -CH(CH ₃ ) ₂ , -C ₆ H ₁₃ , -C ₇ H ₁₅ , -C ₈ H _17I -C ₃ H ₆ -CH(CH ₃ ) ₂ , -C ₂ H ₄ -CH(CH ₃ )-C ₂ H ₅ , -CH(CH ₃ )-C ₄ H _9I -CH ₂ -CH(CH ₃ )-C ₃ H _7I -CH(CH ₃ )-CH ₂ -CH(CH ₃ ) _2I

-CH(CH ₃ )-CH(CH ₃ )-C ₂ H _5I -CH ₂ -CH(CH ₃ )-CH(CH ₃ ) _2I -CH ₂ -C(CH ₃ ) ₂ -C ₂ H _5I -C(CH ₃ ) ₂ -C ₃ H _7I -C(CH ₃ ) ₂ -CH(CH ₃ ) _2I -C ₂ H ₄ -C(CH ₃ ) _3I -CH(CH ₃ )-C(CH ₃ ) _3I -CH=CH ₂ , -CH ₂ -CH=CH _2I -C(CH ₃ )=CH _2I -CH=CH-CH ₃ , -C ₂ H ₄ -CH=CH ₂ , -CH ₂ -CH=CH-CH _3I -CH=CH-C ₂ H _5I -CH ₂ -C(CH ₃ )=CH _2I -CH(CH ₃ )-CH=CH,

-CH=C(CH ₃ ) _2I -C(CH ₃ )=CH-CH _3I -CH=CH-CH=CH ₂ , -C ₃ H ₆ -CH=CH ₂ ,

-C ₂ H ₄ -CH=CH-CH ₃ , -CH ₂ -CH=CH-C ₂ H ₅ , -CH=CH-C ₃ H ₇ ,

-CH=CH-CH=CH-CH ₃ , -C ₂ H ₄ -C(CH ₃ )=CH ₂ , -CH ₂ -CH(CH ₃ )-CH=CH _2I

-CH(CH ₃ )-CH ₂ -CH=CH _2I -CH ₂ -CH=C(CH ₃ ) _2I -CH ₂ -C(CH ₃ )=CH-CH _3I

-CH(CH ₃ )-CH=CH-CH _3I -CH=CH-CH(CH ₃ ) ₂ , -CH=C(CH ₃ )-C ₂ H _5I

-C(CH ₃ )=CH-C ₂ H _5I -C(CH ₃ )=C(CH ₃ ) _2I -C(CH ₃ ) ₂ -CH=CH _2I

-CH(CH ₃ )-C(CH ₃ )=CH _2I -C ₄ H ₈ -CH=CH ₂ , -C ₃ H ₆ -CH=CH-CH ₃ ,

-C ₂ H ₄ -CH=CH-C ₂ H ₅ , -CH ₂ -CH=CH-C ₃ H _7I -CH=CH-C ₄ H _9I -C ₃ H ₆ -C(CH ₃ )=CH _2I -C ₂ H ₄ -CH(CH ₃ )-CH=CH _2I -CH ₂ -CH(CH ₃ )-CH ₂ -CH=CH _2I -C ₂ H ₄ -CH=C(CH ₃ ) _2I -CH(CH ₃ )-C ₂ H ₄ -CH=CH _2I -C ₂ H ₄ -C(CH ₃ )=CH-CH ₃ , -CH ₂ -CH(CH ₃ )-CH=CH-CH _3I -CH(CH ₃ )-CH ₂ -CH=CH-CH _3I -CH ₂ -CH=CH-CH(CH ₃ ) _2I

-CH ₂ -CH=C(CH ₃ )-C ₂ H ₅ , -CH ₂ -C(CH ₃ )=CH-C ₂ H ₅ , -CH(CH ₃ )-CH=CH-C ₂ H ₅ ,

-CH=CH-CH ₂ -CH(CH ₃ ) _2I -CH=CH-CH(CH ₃ )-C ₂ H _5I -CH=C(CH ₃ )-C ₃ H _7I

-C(CH ₃ )=CH-C ₃ H _7I -CH ₂ -CH(CH ₃ )-C(CH ₃ )=CH _2I -C[C(CH ₃ ) ₃ ]=CH _2I

-CH(CH ₃ )-CH ₂ -C(CH ₃ )=CH _2I -CH(CH ₃ )-CH(CH ₃ )-CH=CH _2I

-CH=CH-C ₂ H ₄ -CH=CH _2I -C(CH ₃ ) ₂ -CH ₂ -CH=CH _2I -CH ₂ -C(CH ₃ )=C(CH ₃ ) _2I

-CH(CH ₃ )-CH=C(CH ₃ ) _2I -C(CH ₃ ) ₂ -CH=CH-CH _3I -CH=CH-CH ₂ -CH=CH-CH ₃ , -CH(CH ₃ )-C(CH ₃ )=CH-CH _3I -CH=C(CH ₃ )-CH(CH ₃ ) _2I -C(CH ₃ )=CH-CH(CH ₃ ) _2I -C(CH ₃ )=C(CH ₃ )-C ₂ H _5I -CH=CH-C(CH ₃ ) _3I -C(CH ₃ ) ₂ -C(CH ₃ )=CH _2I

-CH(C ₂ H ₅ )-C(CH ₃ )=CH _2I -C(CH ₃ )(C ₂ H ₅ )-CH=CH _2I -CH(CH ₃ )-C(C ₂ H ₅ )=CH _2I

-CH ₂ -C(C ₃ H ₇ )=CH _2I -CH^C(C ₂ H ₅ )=CH-CH _3I -CH(C ₂ H ₅ )-CH=CH-CH _3I

-C(C ₄ H ₉ )=CH _2I -C(C ₃ H ₇ )=CH-CH _3I -C(C ₂ H ₅ )=CH-C ₂ H ₅ , -C(C ₂ H ₅ )=C(CH ₃ ) _2I

-C[CH(CH ₃ )(C ₂ H ₅ )]=CH ₂ , -C[CH ₂ -CH(CH ₃ ) ₂ ]=CH _2I -C ₂ H ₄ -CH=CH-CH=CH ₂ ,

R ¹¹ and R ¹² represent independently of each other -H, -CH ₃ , -C ₂ H5, -C ₃ H ₇ ,

-CH(CH ₃ ) _2I -CF _3I -(CH ₂ ) _m- NH ₂ , -(CH ₂ ) _m- NHCH ₃ , -(CH ₂ ) _m- NHC ₂ H ₅ ,

Z ¹ - Z ⁴ represent independently of each other -H, -CH ₃ , -C ₂ H ₅ , -C ₃ H ₇ ,

-CH(CH ₃ ) ₂ , -Ph, -COCH ₃ , -COC ₂ H ₅ , -COOH, -COOCH ₃ , -COOC ₂ H _5I -NH ₂ , -NHCH _S , -NHC ₂ H _5I -N(CH ₃ ) _2I -N(C ₂ H ₅ ) _2I -CH ₂ -NH ₂ , -SO ₃ H,

-F, -Cl, -Br, -I, -CN, -CF ₃ , -OCF ₃ , -OH, -OCH ₃ , or -OC ₂ H ₅ ; m is an integer selected from 0, 1 , 2, 3, or 4; n is an integer selected from 1 , 2, 3, or 4; p is an integer selected from 0, 1 , 2, 3, or 4; q is an integer selected from 1, 2, 3, or 4; with the proviso that when X is -H at least one of R ¹ - R ³ is not -H; and when R ⁴ is -H, at least one of R ¹ - R ³ and R ⁵ - R ⁷ is not -H; and the following two compounds are excluded from the scope of the present application: or an enantiomer, a stereoisomeric form, a mixture of enantiomers, a diastereomer, a mixture of diastereomers, a hydrate, a solvate, an acid salt form, a tautomer, or a racemate of the above mentioned compound, or a pharmaceutically acceptable salt thereof .

Preferred are compounds wherein R ⁴ is different from hydrogen (-H). In case R ⁴ is hydrogen one or at least one of the substituents R ¹ - R ³ and R ⁵ - R ⁷ is not hydrogen and preferably two or three or more than three substituents R ¹ - R ³ and R ⁵ - R ⁷ are not hydrogen. Even more preferred are the compounds wherein one or at least one of the substituents R ⁴ - R ⁷ is not hydrogen. Still more preferred are the compounds wherein one or at least one of the substituents R ¹ - R ⁴ is not hydrogen. Most preferred are the compounds wherein one or at least one of the substituents R ¹ - R ³ is not hydrogen and wherein one or at least one of the substituents R ⁵ - R ⁷ is not hydrogen.

Preferably, the present invention relates to a compound of the general formula (la) wherein

X represents -H or -CN,

R ¹ - R ² represent independently of each other -H, -Ph, -CH ₃ , -CF ₃ , -C ₂ H ₅ ,

-C3H7, -CH(CH ₃ ) ₂ , -C ₄ H _9I -CH _2- CH(CH ₃ ) ₂ , -CH(CH ₃ )-C ₂ H _5, -C(CH ₃ ) ₃ , C ₅ H ₁₁ , cyclo-C ₃ H ₅ , cyclo-C ₄ H ₇ , cyclo-C ₅ H ₉ , cyclo-C ₆ Hn, -F, -Cl, -Br, -CN,

R ³ represents -H, -F, -Cl, or -Br;

R ⁴ represents -H, -CH ₃ , -CF ₃ , -C ₂ H ₅ , -C ₃ H ₇ , -CH(CH ₃ ) ₂ , -C ₄ H ₉ ,

-CH ₂ -CH(CH ₃ ) _2I -CH(CH ₃ )-C ₂ H _5, -C(CH ₃ ) _3I -C ₅ H ₁₁ , -CH^OH, -C ₂ H ₄ -OH,

-C ₃ H ₆ -OH, -CN, -CH^NH _2I -CH^NHCH _S , -CH^NHC ₂ H ₅ , -CH^NHC ₃ H _7I -CH^N(CH ₃ ) _2I -CH^N(C ₂ H ₅ ) ₂ , -CH^N(C ₃ H ₇ ) ₂ , -C ₂ H ₄ -NH ₂ , -C ₂ H ₄ -NHCH ₃ ,

-C ₂ H ₄ -NHC ₂ H _5I -C ₂ H ₄ -NHC ₃ H ₇ , -C ₂ H ₄ -N(CH ₃ ) _2I -C ₂ H ₄ -N(C ₂ H ₅ ) _2I

C ₂ H ₄ -N(C ₃ H ₇ ) _2I C ₃ H ₆ -NH ₂ , C ₃ H ₆ -NHCH ₃ , C ₃ H ₆ -NHC ₂ H ₅ ,

-C ₃ H ₆ -NHC ₃ H _7I -C ₃ H ₆ -N(CH ₃ ) _2I -C ₃ H ₆ -N(C ₂ H ₅ ) _{2I -} C ₃ H ₆ -N(C ₃ H ₇ ) ₂ ; R ⁵ - R ⁷ represent independently of each other -R ⁸ , -CH^R ⁸ -SO^R ⁸ , cyclo-C ₃ Fl5, cyclo-C ₄ FI ₇ , cyclo-C ₅ H ₉ , cyclo-CeH-n, cyclo-C ₇ hli ₃ ,

-H, -OH, -OCH3, -OC ₂ H ₅ , -OC ₃ H _7I -0-cyclo-C ₃ H ₅ , -OCH(CH ₃ ) ₂ ,

-OC(CH ₃ ) ₃ , -OC ₄ H _9I -OPh, -OCH _2- Ph, -OCPh ₃ , -CH^OCH ₃ , -C ₂ H ₄ -OCH ₃ , -C ₃ H ₆ -OCH ₃ , -CH^OC ₂ H ₅ , -C ₂ H ₄ -OC ₂ H _5I -C ₃ H ₆ -OC ₂ H ₅ , -CH^OC ₃ H ₇ ,

— C ₂ H ₄ — OC ₃ H ₇ , — C ₃ H ₆ — OC ₃ H _{7I —} CH ₂ — 0— cyclo-C ₃ H5, — C ₂ H ₄ — O— cyclo-C ₃ H5, C ₃ H _s -0-cyclo-C ₃ H ₅ , CH^OCH(CH ₃ ) _2I -C ₂ H ₄ -OCH(CH ₃ ) _2I - C ₃ H ₆ -0CH(CH ₃ ) ₂ ,

CHH3C(CH ₃ ) ₃ , C ₂ H ₄ -OC(CH ₃ ) ₃ , -C ₃ H _S -OC(CH ₃ ) ₃ , -CHH3C ₄ H ₉ ,

C ₂ H ₄ -OC ₄ H _9I C ₃ H ₆ -0C ₄ H ₉ , -CH ₂ -OPh, -C ₂ H ₄ -OPh, -C ₃ H ₆ -OPh, CH ₂ -OCH _2- Ph, C ₂ H ₄ -OCH _2- Ph, -C ₃ H ₆ -OCH _2- Ph, -SH, -SCH ₃ , -SC ₂ H _5I

^■ SC ₃ H _7I -S-cyclo-C ₃ H ₅ , -SCH(CH ₃ ) ₂ , -SC(CH ₃ ) _3I -F, -Cl, -Br, -I, -CN, ■COCHs — COC ₂ H5, — COC ₃ H _7I — CO— cyclo-C ₃ H5, -COCH(CH ₃ ) _2I ■COC(CH ₃ ) _3I -COOH, -COOCHs, -COOC ₂ H _5I -COOC ₃ H _7I -COO-cyclo-C ₃ H ₅ , ■COOCH(CH ₃ ) ₂ , -COOC(CH ₃ ) _3I -OOC-CH ₃ , -OOC-C ₂ H ₅ , -OOC-C ₃ H _7I

^■ OOC-cyclo-C ₃ H ₅ , -OOC-CH(CH ₃ ) ₂ , -OOC-C(CH ₃ ) _3I -CONH _2I

^■ CONHCHs, -CONHC ₂ H ₅ , -CONHC ₃ H ₇ , -CONH-cyclo-C ₃ H ₅ ,

^■ CONH[CH(CH ₃ ) ₂ ], -CONH[C(CH ₃ ) ₃ ], -CON(CH ₃ ) ₂ , -CON(C ₂ H ₅ ) ₂ ,

^■ C0N(C ₃ H ₇ ) ₂ , -CON(cyclo-C ₃ H ₅ ) ₂ , -CON[CH(CH ₃ ) ₂ ] ₂ , -CON[C(CH ₃ ) ₃ ] _2I

^■ NHCOCHs, -NHCOC ₂ H ₅ , -NHCOC ₃ H ₇ , -NHCO-cyclo-CsHs,

NHCO-CH(CH ₃ ) _2I -NHCO-C(CH ₃ ) _3I -NHCO-OCH ₃ , -NHCO-OC ₂ H _5I NHC0-0C ₃ H ₇ , -NHCO-0-cyclo-C ₃ H ₅ , -NHCO-OCH(CH ₃ ) ₂ , -NHCO-OC(CH ₃ ) _3I

-NH ₂ , -NHCH ₃ , -NHC ₂ H ₅ , -NHC ₃ H _7I -NH-cyclo-CsHs, -NHCH(CH ₃ ) _2I

^■ NHC(CH ₃ ) _3I -N(CH ₃ ) _2I -N(C ₂ H ₅ ) _2I -N(C ₃ H ₇ ) _2I -N(cyclo-C ₃ H ₅ ) ₂ , ■N[CH(CH ₃ ) ₂ ] _2I -N[C(CH ₃ ) ₃ ] ₂ , -SOCH ₃ , -SOC ₂ H ₅ , -SOC ₃ H ₇ , -SO-cyclo-C ₃ H ₅ , ■SOCH(CH ₃ ) _2I -SOC(CH ₃ ) _3I -SO ₂ CH ₃ , -SO ₂ C ₂ H ₅ , -S0 ₂ C ₃ H ₇ , -SO^cyclo-CsHs, -S0 ₂ CH(CH ₃ ) _2I -S0 ₂ C(CH ₃ ) _3I -SO ₃ H -SO ₃ CH ₃ ,

^■ S0 ₃ C ₂ H _5I -S0 ₃ C ₃ H ₇ , -S0 ₃ -cyclo-C ₃ H ₅ , -S0 ₃ CH(CH ₃ ) ₂ , -S0 ₃ C(CH ₃ ) _3I ■S0 ₂ NH _2I -SO ₂ NHCH ₃ , -SO ₂ NHC ₂ H ₅ , -SO ₂ NHC ₃ H ₇ , -S0 ₂ NH-cyclo-C ₃ H ₅ , ■S0 ₂ NHCH(CH ₃ ) _2I -S0 ₂ NHC(CH ₃ ) ₃ , -S0 ₂ N(CH ₃ ) _2I -S0 ₂ N(C ₂ H ₅ ) ₂ , ■S0 ₂ N(C ₃ H ₇ ) ₂ , -S0 ₂ N(cyclo-C ₃ H ₅ ) ₂ , -S0 ₂ N[CH(CH ₃ ) ₂ ] ₂ , -S0 ₂ N[C(CH ₃ ) ₃ ] _2I

CH^SO ₂ NH ₂ , -CH^SO ₂ NHCH ₃ , -CH^SO ₂ NHC ₂ H ₅ , -CH^S0 ₂ NHC ₃ H ₇ ,

CH ₂ -S0 ₂ NH-cyclo-C ₃ H _5l -CH^S0 ₂ NHCH(CH ₃ ) _2I -CH^S0 ₂ NHC(CH ₃ ) _3I CH^S0 ₂ N(CH ₃ ) _2I -CH^S0 ₂ N(C ₂ H ₅ ) ₂ , -CH^S0 ₂ N(C ₃ H ₇ ) _2I CH ₂ -S0 ₂ N(cyclo-C ₃ H ₅ ) ₂ , CH^S0 ₂ N[CH(CH ₃ ) ₂ ] ₂ , -CH^S0 ₂ N[C(CH ₃ ) ₃ ] ₂ ,

0-S(=0)CH _3I 0-S(=0)C ₂ H ₅ , -0-S(=0)C ₃ H ₇ , 0-S(=0)-cyclo-C ₃ H ₅ , -NH-CO-NH[CH(CH ₃ ) ₂ ], -NH-CO-NH[C(CH ₃ ) ₃ ], -NH-CO-N(CH ₃ ) _2I

-NH-CO-N(C ₂ H ₅ )2, -NH-CO-NH-cyclo-CsHs, -NH-CO-N(cyclo-C ₃ H ₅ ) ₂ ,

-NH-CO-N[CH(CH ₃ ) ₂ ] ₂ , -NH-C(=NH)-NHCH _3I -NH-C(=NH)-NHC ₂ H _5I

-NH-C(=NH)-NHC ₃ H _7I -O-CO-NH-cyclo-CsHs, -NH-C(=NH)-NH-cyclo-C ₃ H ₅ ,

-NH-C(=NH)-NH[CH(CH ₃ ) ₂ ], -0-C0-NH[CH(CH ₃ ) ₂ ], -NH-C(=NH)-NH[C(CH ₃ ) ₃ ],

-NH-C(=NH)-N(CH ₃ ) _2I -NH-C(=NH)-N(C ₂ H ₅ ) _2I -NH-C(=NH)-N(C ₃ H ₇ ) _2I

-NH-C(=NH)-N(cyclo-C ₃ H ₅ ) ₂ , -0-C0-NHC ₃ H ₇ , -NH-C(=NH)-N[CH(CH ₃ ) ₂ ] ₂ ,

-NH-C(=NH)-N[C(CH ₃ ) ₃ ] _2I -O-CO-NH ₂ , -O-CO-NHCH ₃ , -O-CO-NHC ₂ H ₅ ,

-0-C0-NH[C(CH ₃ ) ₃ ], -0-C0-N(CH ₃ ) _2I -0-C0-N(C ₂ H ₅ ) _2I -0-C0-N(C ₃ H ₇ ) _2I

-0-CO-N(cyclo-C ₃ H ₅ ) ₂ , -0-C0-N[CH(CH ₃ ) ₂ ] ₂ , -0-C0-N[C(CH ₃ ) ₃ ] ₂ , -0-C0-0CH ₃ , -0-C0-0C ₂ H ₅ , -0-C0-0C ₃ H ₇ , -O-CO-O-cyclo-CsHs, -0-C0-0CH(CH ₃ ) ₂ ,

-0-C0-0C(CH ₃ ) _3I -CH ₂ F, -CHF ₂ , -CF ₃ , -CH ₂ -CH ₂ F, -CH ₂ -CHF _2I

-CH ₂ -CF _3I cyclo-C ₈ H ₁₅ , -Ph, -CH _2- Ph, -CH _2- CH _2- Ph, -CH=CH-Ph, -CPh ₃ , -CH ₃ , -C ₂ H _5I -C ₃ H _7I -CH(CH ₃ ) _2I -C ₄ H _9I -CH ₂ -CH(CH ₃ ) _2I

-CH(CH ₃ )-C ₂ H _5, -C(CH ₃ ) _3I -C5H11, -CH(CH ₃ )-C ₃ H _7I -CH ₂ -CH(CH ₃ )-C ₂ H _5I

-CH(CH ₃ )-CH(CH ₃ ) _2I -C(CH ₃ ) ₂ -C ₂ H ₅ , -CH ₂ -C(CH ₃ ) _3I -CH(C ₂ H ₅ ) _2I

-C ₂ H ₄ -CH(CH ₃ ) _2I -C ₆ H ₁₃ , -C ₇ H _15I -C ₈ H ₁₇ , -C ₃ H ₆ -CH(CH ₃ ) _2I -C ₂ H ₄ -CH(CH ₃ )-C ₂ H _5I -CH(CH ₃ )-C ₄ H _9I -CH ₂ -CH(CH ₃ )-C ₃ H _7I -CH(CH ₃ )-CH ₂ -CH(CH ₃ ) _2I

-CH(CH ₃ )-CH(CH ₃ )-C ₂ H _5I -CH ₂ -CH(CH ₃ )-CH(CH ₃ ) _2I -CH ₂ -C(CH ₃ ) ₂ -C ₂ H _5I -C(CH ₃ ) ₂ -C ₃ H _7I -C(CH ₃ ) ₂ -CH(CH ₃ ) _2I -C ₂ H ₄ -C(CH ₃ ) _3I -CH(CH ₃ )-C(CH ₃ ) _3I

-CH=CH ₂ , -CH ₂ -CH=CH _2I -C(CH ₃ )=CH _2I -CH=CH-CH ₃ , -C ₂ H ₄ -CH=CH ₂ , -CH ₂ -CH=CH-CH _3I -CH=CH-C ₂ H _5I -CH ₂ -C(CH ₃ )=CH _2I -CH(CH ₃ )-CH=CH,

-CH=C(CH ₃ ) _2I -C(CH ₃ )=CH-CH _3I -CH=CH-CH=CH ₂ , -C ₃ H ₆ -CH=CH ₂ ,

C ₂ H ₄ -CH=CH-CH ₃ , -CH ₂ -CH=CH-C ₂ H ₅ , -CH=CH-C ₃ H ₇ ,

CH=CH-CH=CH-CH ₃ , -C ₂ H ₄ -C(CH ₃ )=CH ₂ , -CH ₂ -CH(CH ₃ )-CH=CH _2I

CH(CH ₃ )-CH ₂ -CH=CH _2I -CH ₂ -CH=C(CH ₃ ) _2I -CH ₂ -C(CH ₃ )=CH-CH _3I

CH(CH ₃ )-CH=CH-CH _3I -CH=CH-CH(CH ₃ ) ₂ , -CH=C(CH ₃ )-C ₂ H _5I

C(CH ₃ )=CH-C ₂ H ₅ , -C(CH ₃ )=C(CH ₃ ) ₂ , -C(CH ₃ ) ₂ -CH=CH ₂ ,

CH(CH ₃ )-C(CH ₃ )=CH _2I -C ₄ H ₈ -CH=CH ₂ , -C ₃ H ₆ -CH=CH-CH ₃ ,

-C ₂ H ₄ -CH=CH-C ₂ H ₅ , -CH ₂ -CH=CH-C ₃ H _7I -CH=CH-C ₄ H _9I -C ₃ H ₆ -C(CH ₃ )=CH _2I -C ₂ H ₄ -CH(CH ₃ )-CH=CH _2I -CH ₂ -CH(CH ₃ )-CH ₂ -CH=CH _2I -C ₂ H ₄ -CH=C(CH ₃ ) _2I -CH(CH ₃ )-C ₂ H ₄ -CH=CH _2I -C ₂ H ₄ -C(CH ₃ )=CH-CH _3I -CH ₂ -CH(CH ₃ )-CH=CH-CH _3I -CH(CH ₃ )-CH ₂ -CH=CH-CH _3I -CH ₂ -CH=CH-CH(CH ₃ ) _2I

-CH ₂ -CH=C(CH ₃ )-C ₂ H _5I -CH ₂ -C(CH ₃ )=CH-C ₂ H _5I -CH(CH ₃ )-CH=CH-C ₂ H _5I

-CH=CH-CH ₂ -CH(CH ₃ ) _2I -CH=CH-CH(CH ₃ )-C ₂ H _5I -CH=C(CH ₃ )-C ₃ H _7I

-C(CH ₃ )=CH-C ₃ H _7I -CH ₂ -CH(CH ₃ )-C(CH ₃ )=CH _2I -C[C(CH ₃ ) ₃ ]=CH _2I

-CH(CH ₃ )-CH ₂ -C(CH ₃ )=CH _2I -CH(CH ₃ )-CH(CH ₃ )-CH=CH _2I

-CH=CH-C ₂ H ₄ -CH=CH _2I -C(CH ₃ ) ₂ -CH ₂ -CH=CH _2I -CH ₂ -C(CH ₃ )=C(CH ₃ ) _2I

-CH(CH ₃ )-CH=C(CH ₃ ) _2I -C(CH ₃ ) ₂ -CH=CH-CH _3I -CH=CH-CH ₂ -CH=CH-CH ₃ , -CH(CH ₃ )-C(CH ₃ )=CH-CH _3I -CH=C(CH ₃ )-CH(CH ₃ ) _2I -C(CH ₃ )=CH-CH(CH ₃ ) ₂ ,

-C(CH ₃ )=C(CH ₃ )-C ₂ H _5I -CH=CH-C(CH ₃ ) _3I -C(CH ₃ ) ₂ -C(CH ₃ )=CH ₂ ,

-CH(C ₂ H ₅ )-C(CH ₃ )=CH _2I -C(CH ₃ )(C ₂ H ₅ )-CH=CH _2I -CH(CH ₃ )-C(C ₂ H ₅ )=CH _2I

-CH ₂ -C(C ₃ H ₇ )=CH _2I -CH^C(C ₂ H ₅ )=CH-CH ₃ , -CH(C ₂ H ₅ )-CH=CH-CH _3I

-C(C ₄ H ₉ )=CH _2I -C(C ₃ H ₇ )=CH-CH _3I -C(C ₂ H ₅ )=CH-C ₂ H ₅ , -C(C ₂ H ₅ )=C(CH ₃ ) ₂ ,

-C[CH(CH ₃ )(C ₂ H ₅ )]=CH _2I -C[CH ₂ -CH(CH ₃ ) ₂ ]=CH _2I -C ₂ H ₄ -CH=CH-CH=CH ₂ ,

-CH ₂ -CH=CH-CH ₂ -CH=CH ₂ , -C ₃ H ₆ -CºC-CH ₃ , -CH ₂ -CH=CH-CH=CH-CH ₃ ,

-CH=CH-CH=CH-C ₂ H _5I -CH(CH ₃ )-CH ₂ -CºCH, -CH(CH ₃ )-CºC-CH _3I

-C ₂ H ₄ -CH(CH ₃ )-CºCH, -CH=CH-CH=C(CH ₃ ) _2I -CH ₂ -CH(CH ₃ )-CH ₂ -CºCH, -CH=CH-C(CH ₃ )=CH-CH _3I -CH=C(CH ₃ )-CH=CH-CH _3I -CH ₂ -CH(CH ₃ )-CºCH, -C(CH ₃ )=CH-CH=CH-CH ₃ , -CºCH, -CºC-CH ₃ , -CH ₂ -CºCH,

-C ₂ H ₄ -CºCH, -CH ₂ -CºC-CH ₃ , -CºC-C ₂ H ₅ , -C ₃ H ₆ -CºCH, -C ₂ H ₄ -CºC-CH ₃ , -CH ₂ -CºC-C ₂ H ₅ , -CºC-C ₃ H _7I -CH(CH ₃ )-CºCH, -C ₄ H ₈ -CºCH,

-C ₂ H ₄ -CºC-C ₂ H ₅ , -CH ₂ -CºC-C ₃ H ₇ , -CºC-C ₄ H ₉ , -CºC-CH ₂ -CH(CH ₃ ) _2I

-CH(CH ₃ )-C ₂ H ₄ -CºCH, -CH ₂ -CH(CH ₃ )-CºC-CH _3I -C(CH ₃ )(C ₂ H ₅ )-CºCH,

-CH(CH ₃ )-CH ₂ -CºC-CH ₃ , -CH(CH ₃ )-CºC-C ₂ H _5I -CH ₂ -CºC-CH(CH ₃ ) _2I -CºC-CH(CH ₃ )-C ₂ H ₅ , -CH ₂ -CºC-CºC-CH ₃ , -CH(C ₂ H ₅ )-CºC-CH ₃ ,

-C(CH ₃ ) ₂ -CºC-CH _3I -CH(C ₂ H ₅ )-CH ₂ -CºCH, -CH^CH(C ₂ H ₅ )-CºCH,

-C(CH ₃ ) ₂ -CH ₂ -CºCH, -CH ₂ -C(CH ₃ ) ₂ -CºCH, -CH(CH ₃ )-CH(CH ₃ )-CºCH,

-CH(C ₃ H ₇ )-CºCH, -CH ₂ -CH(CºCH) _2I -CºC-CºCH, -CH ₂ -CºC-CºCH, -CºC-CºC-CH _3I -CH(CºCH) _2I -C ₂ H ₄ -CºC-CºCH, -CH ₂ -CºC-CH ₂ -CºCH,

-CºC-C ₂ H ₄ -CºCH, -CºC-C(CH ₃ ) _3I -CºC-CH ₂ -CºC-CH ₃ , or

^— C=C— C=C— C ₂ H _5, or R ⁵ and R ⁶ , or R ⁶ and R ⁷ form together

R 9 represents H,

R 10 represents -CH ₃ , -CF 3, -C ₂ H _5I -C ₃ H _7I -CH(CH ₃ ) ₂ , -C4H9, -CH _2- CH(CH ₃ )2, -CH(CH ₃ )-C ₂ H _5, -C(CH ₃ ) ₃ , -C5H11, -(CH ₂ ) _n- NH ₂ ,

-(CH ₂ ) _n- NHCH ₃ , -(CH ₂ ) _n -NHC ₂ H ₅ , -(CH ₂ ) _n- NHC ₃ H ₇ , -(CH ₂ ) _n- N(CH ₃ ) ₂ ,

-(CH ₂ ) _n- N(C ₂ H ₅ ) ₂ , -(CH ₂ ) _n- N(C ₃ H ₇ ) ₂ ,

R ¹¹ and R ¹² represent independently of each other -H, -CH ₃ , -C2H5, -C3H7,

-CH(CH ₃ ) ₂ , -CF _3I -(CH ₂ ) _m- NH ₂ , -(CH ₂ ) _m- NHCH ₃ , -(CH ₂ ) _m- NHC ₂ H ₅ , -(CH ₂ ) _m- NHC ₃ H ₇ , -(CH ₂ ) _m- N(CH ₃ ) ₂ , -(CH ₂ ) _m- N(C ₂ H ₅ ) ₂ , -(CH ₂ ) _m- N(C ₃ H ₇ ) ₂ ,

-OCH ₃ , -OC2H5, -OC ₃ H _7I -0-cyclo-C ₃ H ₅ , -OCH(CH ₃ ) ₂ , -F, -Cl, -Br,

-CN, -(CH ₂ ) _m -S0 ₂ CH ₃ , -(CH ₂ ) _m -S0 ₂ C ₂ H ₅ , -(CH ₂ ) _m -S0 ₂ C ₃ H ₇ ,

-(CH ₂ ) _m -SO^cyclo-C ₃ H ₅ , -(CH ₂ ) _m -S0 ₂ CH(CH ₃ ) ₂ , -(CH ₂ ) _m -S0 ₂ C(CH ₃ ) ₃ ,

-0-(CH ₂ ) _m- NH ₂ , -0-(CH ₂ ) _m- NHCH ₃ , -0-(CH ₂ ) _m- NHC ₂ H ₅ , -0-(CH ₂ ) _m- NHC ₃ H ₇ ,

-0-(CH ₂ ) _m- N(CH ₃ ) ₂ , -0-(CH ₂ ) _m- N(C ₂ H ₅ ) ₂ , -0-(CH ₂ ) _m- N(C ₃ H ₇ ) ₂ , -NHCOCH ₃ ,

-(CH ₂ ) _m- NHCOCH ₃ , -(CH ₂ ) _m -NHCOC ₂ H ₅ , -(CH ₂ ) _m- NHCO-cyclo-C ₃ H ₅ ,

-(CH ₂ ) _m- NHCOC ₃ H ₇ , -(CH ₂ ) _m- NHCO-CH(CH ₃ ) ₂ , -(CH ₂ ) _m- NHCO-CH=CH ₂ , -S0 ₂ NH _2I -S0 ₂ NHCH _3I -S0 ₂ NHC ₂ H _5I -S0 ₂ NHC ₃ H _7I -S0 ₂ NH-cyclo-C ₃ H ₅ , -S0 ₂ NHCH(CH ₃ ) ₂ , -S0 ₂ N(CH ₃ ) _2I -S0 ₂ N(C ₂ H ₅ ) ₂ , -S0 ₂ N(C ₃ H ₇ ) _2I

-S0 ₂ N(cyclo-C ₃ H ₅ ) ₂ , -S0 ₂ N[CH(CH ₃ ) ₂ ] ₂ , -NH-SO^CH ₃ , -NH-S0 ₂ -C ₂ H ₅ ,

-NH-S0 ₂ -C ₃ H _7I -NH-S0 ₂ -cyclo-C ₃ H ₅ , -NH-S0 ₂ -CH(CH ₃ ) ₂ , -CONH ₂ , -SOCHs, -SOC ₂ H _5I -SOC ₃ H _7I -SO-cyclo-C ₃ H ₅ , -SOCH(CH ₃ ) ₂ , -SCH ₃ , -SOCF ₃ , -S0 ₂ CF _3I or -SO(NH)CH ₃ ;

R ^N1 and R ^N2 represent independently of each other -H, -CH ₃ , -C ₂ H ₅ , -C ₃ H ₇ ,

-CH(CH ₃ ) _2I cyclo-C ₃ H ₅ , cyclo-C ₄ H ₇ , cyclo-C ₅ H ₉ , cyclo-C ₆ Hii, -C ₄ H ₉ , -C(CH ₃ ) ₃ , -CH _2- CH(CH ₃ ) ₂ , -CH(CH ₃ )-C ₂ H _5, -C ₅ H ₁₁ , -Ph, -CH _2- Ph,

-CH=CH ₂ , -CH ₂ -CH=CH ₂ , -CH=CH-CH ₃ , -CºCH, -CH ₂ -CºCH, -CºC-CH ₃ ,

-COCHs, -COC ₂ H _5I -COC ₃ H _7I -CO-cyclo-C ₃ H ₅ , -COCH(CH ₃ ) ₂ , -COOCH ₃ , -COOC ₂ H _5I -COOC ₃ H _7I -COO-cyclo-C ₃ H ₅ , -COOCH(CH ₃ ) ₂ , -COOC(CH ₃ ) ₃ , -CH _2- CH(0H)-CH ₃ , -(CH ₂ ) _q- NH ₂ , -(CH ₂ ) _q- NHCH ₃ , -(CH ₂ ) _q- NHC ₂ H ₅ ,

-(CH ₂ ) _q- NHC ₃ H ₇ , -(CH ₂ ) _q- N(CH ₃ ) ₂ , -(CH ₂ ) _q- N(C ₂ H ₅ ) ₂ , -(CH ₂ ) _q- N(C ₃ H ₇ ) ₂ ,

Z ¹ - Z ⁴ represent independently of each other -H, -CH ₃ , -C ₂ H ₅ , -C ₃ H ₇ ,

-CH(CH ₃ ) ₂ , -Ph, -COCH ₃ , -COC ₂ H ₅ , -COOH, -COOCH ₃ , -COOC ₂ H _5I -NH ₂ , -NHCH _S , -NHC ₂ H _5I -N(CH ₃ ) _2I -N(C ₂ H ₅ ) ₂ , -CH ₂ -NH ₂ , -SO ₃ H,

-F, -Cl, -Br, -I, -CN, -CF ₃ , -OCF ₃ , -OH, -OCH ₃ , or -OC ₂ H ₅ ; m is an integer selected from 0, 1 , 2, 3, or 4; n is an integer selected from 1 , 2, 3, or 4; p is an integer selected from 0, 1 , 2, 3, or 4; q is an integer selected from 1 , 2, 3, or 4; with the proviso that when X is -H at least one of R ¹ - R ³ is not -H; and when R ⁴ is

-H, at least one of R ¹ - R ³ and R ⁵ - R ⁷ is not -H; and the following two compounds are excluded from the scope of the present application: or an enantiomer, a stereoisomeric form, a mixture of enantiomers, a diastereomer, a mixture of diastereomers, a hydrate, a solvate, an acid salt form, a tautomer, or a racemate of the above mentioned compound, or a pharmaceutically acceptable salt thereof .

Preferred are compounds wherein R ⁴ is different from hydrogen (-H). In case R ⁴ is hydrogen one or at least one of the substituents R ¹ - R ³ and R ⁵ - R ⁷ is not hydrogen and preferably two or three or more than three substituents R ¹ - R ³ and R ⁵ - R ⁷ are not hydrogen. Even more preferred are the compounds wherein one or at least one of the substituents R ⁴ - R ⁷ is not hydrogen. Still more preferred are the compounds wherein one or at least one of the substituents R ¹ - R ⁴ is not hydrogen. Most preferred are the compounds wherein one or at least one of the substituents R ¹ - R ³ is not hydrogen and wherein one or at least one of the substituents R ⁵ - R ⁷ is not hydrogen.

Preferably, the compounds of general formula (la) as defined herein are under the proviso that when X is -H at least one of R ¹ - R ³ is not -H and under the second proviso that R ⁵ , R ⁶ and R ⁷ are not -H at the same time or preferably under the further proviso that at least one of R ¹ - R ³ is not -H, when R ^s and R ⁶ or R ⁶ and R ⁷ form together ~ ^' 0 ; more preferably under the further proviso that when X is -CN or when R ⁴ is -H or -C ₂ H ₅ or - CH ₂ OH or -C ₂ H ₄ OH, at least one of R ⁵ , R ⁶ and R ⁷ is different from -H or still more preferably under the second proviso that in case X is -CN and R ⁴ is -H or -C ₂ H ₅ or - CH ₂ OH or -C ₂ H ₄ OH, at least one of R ⁵ , R ⁶ and R ⁷ is different from -H.

Also preferred are the following general formulae (la-1), (la-2), (la-3), and (la-4)

wherein the substituents R ¹ - R ⁷ and X have the meanings or the preferred meanings as disclosed herein, but the substituents R ¹ and R ² are different from hydrogen (-H).

In general formula (I) and all other general formulae disclosed herein, the substituents R ⁵ and R ⁶ or R ⁶ and R ⁷ form together preferably one of the following five-membered ring systems systems

In some embodiments, the present invention refers to the compound of the formula (I), or (la), wherein wherein R ⁹ , R ¹⁰ , R ¹¹ , R ¹² , R ^N2 Z ³ , Z ⁴ have the meanings as defined in the formula (I).

In some embodiments, the present invention refers to the compound of the formula (I), wherein

wherein n, p, R ¹¹ , R ¹² , R ^N2 , Z ³ , Z ⁴ have the meanings as defined in the formula (I).

Preferred, is the compound of the formula (I): wherein

X represents -H or -CN,

Y represents CH or N, R ¹ represents -H, -CH ₃ , -Cl, -Ph,

R ² represents -H, -CH ₃ , -Ph, -Cl, -Br, -CF ₃ , -CN, -OH, -NH-Ph, -0-CH ₂ CH _2- N(CH ₃ ) ₂ , -R ⁹ , -O-R ¹⁰

R ³ represents -H, -CH ₃ , or -Br;

R ⁴ represents -H, -CH ₃ , -CF ₃ , -CN, -CH ₂ OH, -CH ₂ CH ₂ OH, -CH ₂ N(CH ₃ ) ₂ ,

-CH ₂ CH ₂ N(CH ₃ ) ₂ , or -CH ₂ CH ₂ N(CH ₂ CH ₃ ) ₂ ;

R ⁵ , R ⁶ and R ⁷ represents independently of each other -R ⁸ , -CH^R ⁸ , -SO^R ⁸ ,

-H, -F, -Cl, -Br, -CN, -CH ₃ , -CF ₃ , -OCH _{3 ,} -COCH ₃ , -CONH ₂ , -NHCOCH ₃ , ,

-N(CH ₃ ) ₂ , -S0 ₂ CH ₃ , -S0 ₂ NH ₂ , -S0 ₂ NHCH ₃ , -CH^S0 ₂ NH ₂ , , -NH-S0 ₂ -CH ₃ , or R ⁵ and R ⁶ , or R ⁶ and R ⁷ form R ⁸ represents Nr or z

R ¹¹ and R ¹² represent independently of each other -H, -CH ₃ , -C2H5, -C ₃ H ₇ ,

-CH(CH ₃ ) _2I -CF _3I -(CH ₂ ) _m -NH ₂ , -(CH ₂ ) _m -NHCH ₃ , -(CH ₂ ) _m -NHC ₂ H ₅ , -(CH ₂ ) _m -NHC ₃ H ₇ , -(CH ₂ ) _m -N(CH ₃ ) ₂ , -(CH ₂ ) _m -N(C ₂ H ₅ ) ₂ , -(CH ₂ ) _m -N(C ₃ H ₇ ) ₂ , -OCH _3I -OC ₂ H _5I -OC ₃ H _7I -O-cyclo-CsHs, -OCH(CH ₃ ) ₂ , -F, -Cl, -Br,

-CN, -(CH ₂ ) _m -S0 ₂ CH ₃ , -(CH ₂ ) _m -S0 ₂ C ₂ H ₅ , -(CH ₂ ) _m -S0 ₂ C ₃ H ₇ ,

-(CH ₂ ) _m -SO^cyclo-C ₃ H ₅ , -(CH ₂ ) _m -S0 ₂ CH(CH ₃ ) ₂ , -(CH ₂ ) _m -S0 ₂ C(CH ₃ ) ₃ ,

-0-(CH ₂ ) _m -NH ₂ , -0-(CH ₂ ) _m -NHCH ₃ , -0-(CH ₂ ) _m -NHC ₂ H ₅ , -0-(CH ₂ ) _m -NHC ₃ H ₇ , -0-(CH ₂ ) _m- N(CH ₃ ) ₂ , -0-(CH ₂ ) _m- N(C ₂ H ₅ ) ₂ , -0-(CH ₂ ) _m- N(C ₃ H ₇ ) ₂ , -NHCOCH ₃ ,

-(CH ₂ ) _m- NHCOCH ₃ , -(CH ₂ ) _m -NHCOC ₂ H5, -(CH ₂ ) _m- NHCO-cyclo-C ₃ H ₅ ,

-(CH ₂ )m-NHCOC ₃ H ₇ , -(CH ₂ ) _m- NHCO-CH(CH ₃ ) ₂ , -(CH ₂ )m-NHCO-CH=CH ₂ , -SO2NH2, -S0 ₂ NHCH _3I -SO2NHC2H5, -S0 ₂ NHC ₃ H _7I -S0 ₂ NH-cyclo-C ₃ H ₅ ,

-S0 ₂ NHCH(CH ₃ ) _2I -S0 ₂ N(CH ₃ ) _2I -S0 ₂ N(C ₂ H ₅ ) ₂ , -S0 ₂ N(C ₃ H ₇ ) _2I

-S0 ₂ N(cyclo-C ₃ H ₅ )2, -S0 ₂ N[CH(CH ₃ ) ₂ ]2, -NH-SC>2-CH _3I -NH-SO2-C2H5,

-NH-S0 ₂ -C ₃ H _7I -NH-S0 ₂ -cyclo-C ₃ H ₅ , -NH-S0 ₂ -CH(CH ₃ ) ₂ , -CONH ₂ , -SOCHs, -SOC2H5, -SOC ₃ H _7I -SO-cyclo-C ₃ H ₅ , -SOCH(CH ₃ ) ₂ , -SCH ₃ , -SOCF _3I -S0 ₂ CF _3I or -SO(NH)CH ₃ ;

Preferably, R ¹¹ and R ¹² represent independently of each other -H, -CH ₃ , -C ₂ H ₅ ,

-C ₃ H _7I -CH(CH ₃ ) _2I -CF _3I -(CH ₂ ) _m- N(CH ₃ ) ₂ , -(CH ₂ ) _m- N(C ₂ H ₅ ) ₂ , -OCH ₃ , -OC ₂ H ₅ ,

-OC ₃ H ₇ , -0-cyclo-C ₃ H ₅ , -OCH(CH ₃ ) ₂ , -F, -Cl, -Br,

-CN, -(CH ₂ ) _m -S0 ₂ CH ₃ , -(CH ₂ ) _m -SO^cyclo-C ₃ H ₅ , -0-(CH ₂ ) _m- N(CH ₃ ) ₂ ,

-0-(CH ₂ ) _m- N(C ₂ H ₅ ) ₂ , -NHCOCHs, -(CH ₂ ) _m- NHCOCH ₃ , -(CH ₂ ) _m -NHCOC ₂ H ₅ ,

-(CH ₂ ) _m- NHCO-cyclo-C ₃ H ₅ , -(CH ₂ ) _m- NHCO-CH(CH ₃ ) ₂ , -(CH ₂ )m-NHCO-CH=CH ₂ , -SO ₂ NH ₂ , -S0 ₂ NHCH ₃ , -SO ₂ NHC ₂ H ₅ , -SO ₂ NHC ₃ H ₇ ,

-S0 ₂ N H-cyclo-C ₃ H ₅ , -S0 ₂ NHCH(CH ₃ ) _2l -S0 ₂ N(CH ₃ ) ₂ , -S0 ₂ N(C ₂ H ₅ ) ₂ ,

-S0 ₂ N(C ₃ H ₇ ) _2I -S0 ₂ N(cyclo-C ₃ H ₅ )2, -S0 ₂ N[CH(CH ₃ ) ₂ ]2, -NH-S0 ₂ -CH ₃ ,

NH-SO ₂ -C ₂ H ₅ , NH-S0 ₂ -C ₃ H _7I NH-S0 ₂ -cyclo-C ₃ H ₅ , NH-S0 ₂ -CH(CH ₃ ) ₂ , -CONH ₂ , -SOCHs, -SOC ₂ H ₅ , -SOC ₃ H _7I -SO-cyclo-CsHs, -SOCH(CH ₃ ) ₂ , -SCH ₃ , -SOCF _3I -S0 ₂ CF _3I or -SO(NH)CH ₃ ;

More preferably, R ¹¹ and R ¹² represent independently of each other -H, CH ₃ , -C2H5, -CF ₃ , -(CH ₂ ) _m- N(CH ₃ ) ₂ , -OCH ₃ , -OC2H5, -F, -Cl, -Br,

-CN, -(CH ₂ ) _m -S0 ₂ CH ₃ , -(CH ₂ ) _m -S02-cyclo-C ₃ H ₅ , -0-(CH ₂ ) _m- N(CH ₃ ) ₂ ,

-NHCOCHs, -(CH ₂ ) _m- NHCOCH ₃ , -(CH ₂ ) _m- NHCO-CH=CH ₂ , -S0 ₂ NH ₂ , -S0 ₂ NHCH ₃ , -S0 ₂ N(CH ₃ ) ₂ , -S0 ₂ N(C ₂ H ₅ ) ₂ , -S0 ₂ N(C ₃ H ₇ ) ₂ , -NH-SO ₂ -CH ₃ ,

-NH-SO2-C2H5, -NH-S0 ₂ -C ₃ H ₇ , -NH-S0 ₂ -cyclo-C ₃ H ₅ , -NH-S0 ₂ -CH(CH ₃ ) ₂ ,

-CONH2, -SOCHs, -SOC2H5, -S0C ₃ H ₇ , -SO-cyclo-CsHs, -SOCH(CH ₃ ) ₂ , -SCH ₃ , -SOCF ₃ , -S0 ₂ CF _3I or -SO(NH)CH ₃ ;

R ^N1 and R ^N2 represents independently of each other -H, -CH ₃ , -C ₂ H ₅ , -C ₃ H ₇ ,

-CH(CH ₃ ) ₂ , cyclo-C ₃ H ₅ , cyclo-C ₄ H ₇ , -CH _2- CH(CH ₃ ) ₂ , -Ph, -CH _2- Ph, -COCHs, -COC ₂ H ₅ , -COC ₃ H ₇ , -CO-cyclo-CsHs, -COCH(CH ₃ ) ₂ , -COOCH ₃ , -COOC ₂ H ₅ , -COOC ₃ H ₇ , -COO-cyclo-CsHs, -COOCH(CH ₃ ) ₂ , -COOC(CH ₃ ) ₃ , CH ₂ CH(OH) CH ₃ , (CH ₂ )q NH _2I (CH ₂ ) _q NHCH _3I (CH ₂ ) _q NHC ₂ H ₅ ,

-(CH ₂ ) _q- NHC ₃ H ₇ , -(CH ₂ ) _q- N(CH ₃ ) ₂ , -(CH ₂ ) _q- N(C ₂ H ₅ ) ₂ , -(CH ₂ ) _q- N(C ₃ H ₇ ) ₂ ,

Z ¹ , Z ² , Z ³ and Z ⁴ represent independently of each other -H, -CH3, -C2H5, -C3H7,

-CH(CH ₃ ) ₂ , -F, -Cl, -Br, -I, -CN, -CF ₃ ; m is an integer selected from 0, 1 , 2, or 3; n is an integer selected from 1 , or 2; p is an integer selected from 0, or 1 ; q is an integer selected from 1 , or 2; with the proviso that when X is -FI at least one of R ¹ - R ³ is not -FI; when R ⁴ is -H, at least one of R ¹ - R ³ and R ⁵ - R ⁷ is not -FI; and (E)-N-benzyl-2-cyano-3-(1 Fl- pyrrolo[2,3-b]pyridin-3-yl)acrylamide and (E)-N-(1 ,3-benzodioxol-5-yl-methyl)-2-cyano-3- (1 FI-pyrrolo[2,3-b]pyridin-3-yl)acrylamide are excluded; or an enantiomer, a stereoisomeric form, a mixture of enantiomers, a diastereomer, a mixture of diastereomers, a hydrate, a solvate, an acid salt form, a tautomer, or a racemate of the above mentioned compound, or a pharmaceutically acceptable salt thereof.

Also preferred, is the compound of the formula (la): wherein

X represents -H or -CN,

R ¹ is -H, -CH ₃ , -Cl, -Ph, R ² represents -H, -CH3, -Ph, -Cl, -Br, CF ₃ , -CN, -OH, -NH-Ph -0-CH ₂ CH2-N(CH ₃ )2, -R ⁹ -O-R ¹⁰

R ³ represents -H, -CH ₃ , or -Br;

R ⁴ represents -H, -CH ₃ , -CF ₃ , -CN, -CH ₂ OH, -CH ₂ CH ₂ OH, -CH ₂ N(CH ₃ ) ₂ ,

-CH ₂ CH ₂ N(CH ₃ ) ₂ , or -CH ₂ CH ₂ N(CH ₂ CH ₃ ) ₂ ;

R ⁵ , R ⁶ and R ⁷ represents independently of each other -R ⁸ , -CH2-R ⁸ , -SO2-R ⁸ , -H, -F, -Cl, -Br, -CN, -CH ₃ , -CF ₃ , -OCH _{3 ,} -COCH ₃ , -CONH ₂ , -NHCOCH ₃ , ,

-N(CH ₃ ) ₂ , -SO ₂ CH ₃ , -S0 ₂ NH _2I -S0 ₂ NHCH _3I -CH^S0 ₂ NH _2I , -NH-S0 ₂ -CH ₃ ,

I or R ⁵ and R ⁶ , or R ⁶ and R ⁷ form more preferred, R ⁵ and R ⁶ , or R ⁶ and R ⁷ form R ⁸ represents

-S0 ₂ N(cyclo-C ₃ H ₅ ) _2l -S0 ₂ N[CH(CH ₃ ) ₂ ] ₂ , -NH-S(VCH ₃ , -NH-S0 ₂ -C ₂ H ₅ , -NH-SO2-C3H7, -NH-S0 ₂ -cyclo-C ₃ H ₅ , -NH-S0 ₂ -CH(CH ₃ )2, -CONH ₂ , -SOCHs, -SOC ₂ H _5I -SOC ₃ H _7I -SO-cyclo-C ₃ H ₅ , -SOCH(CH ₃ ) ₂ , -SCH ₃ , -SOCF _3I -S0 ₂ CF _3I or -SO(NH)CH ₃ ;

Preferably, R ¹¹ and R ¹² represent independently of each other -H, — CH ₃ , — C ₂ H5,

-C ₃ H _7I -CH(CH ₃ ) _2I -CF _3I — (CH ₂ ) _m— N(CH ₃ ) ₂ , -(CH ₂ ) _m- N(C ₂ H ₅ ) ₂ , -OCH ₃ , -OC ₂ H ₅ , -OC ₃ H ₇ , -O-cyclo-CsHs, -OCH(CH ₃ ) ₂ , -F, -Cl, -Br,

-CN, -(CH ₂ ) _m -S0 ₂ CH ₃ , -(CH ₂ ) _m -SO^cyclo-C ₃ H ₅ , -0-(CH ₂ ) _m- N(CH ₃ ) ₂ , -0-(CH ₂ ) _m- N(C ₂ H ₅ ) ₂ , -NHCOCHs, -(CH ₂ ) _m- NHCOCH ₃ , -(CH ₂ ) _m -NHCOC ₂ H ₅ ,

-(CH ₂ ) _m- NHCO-cyclo-C ₃ H ₅ , -(CH ₂ ) _m- NHCO-CH(CH ₃ ) ₂ , -(CH ₂ ) _m- NHCO-CH=CH ₂ , -S0 ₂ NH ₂ , -S0 ₂ NHCH ₃ , -S0 ₂ NHC ₂ H ₅ , -S0 ₂ NHC ₃ H ₇ ,

-S0 ₂ NH-cyclo-C ₃ H ₅ , -S0 ₂ NHCH(CH ₃ ) ₂ , -S0 ₂ N(CH ₃ ) ₂ , -S0 ₂ N(C ₂ H ₅ ) ₂ ,

-S0 ₂ N(C ₃ H ₇ ) _2I -S0 ₂ N(cyclo-C ₃ H ₅ ) ₂ , -S0 ₂ N[CH(CH ₃ ) ₂ ] ₂ , -NH-S0 ₂ -CH ₃ ,

-NH-S0 ₂ -C ₂ H _5I -NH-S0 ₂ -C ₃ H _7I -NH-S0 ₂ -cyclo-C ₃ H ₅ , -NH-S0 ₂ -CH(CH ₃ ) ₂ ,

-CONH ₂ , -SOCH _S , -SOC ₂ H _5I -SOC ₃ H _7I -SO-cyclo-CsHs, -SOCH(CH ₃ ) ₂ , -SCH ₃ , -SOCFs, -S0 ₂ CF ₃ , or -SO(NH)CH ₃ ;

More preferably, R ¹¹ and R ¹² represent independently of each other -H, — CH ₃ ,

-C ₂ H ₅ , -CF _3I — (CH ₂ ) _m— N(CH ₃ ) _2I -OCH _3I -OC ₂ H _5I -F, -Cl, -Br,

-CN, (CH ₂ ) _m -S0 ₂ CH ₃ , (CH ₂ ) _m -SO^cyclo-C ₃ H ₅ , 0 (CH ₂ ) _m N(CH ₃ ) ₂ , -NHCOCHs, -(CH ₂ ) _m- NHCOCH ₃ , -(CH ₂ ) _m- NHCO-CH=CH ₂ , -S0 ₂ NH ₂ , -S0 ₂ NHCH ₃ , -S0 ₂ N(CH ₃ ) _2I -S0 ₂ N(C ₂ H ₅ ) ₂ , -S0 ₂ N(C ₃ H ₇ ) _2I -NH-SO ₂ -CH ₃ ,

-NH-S0 ₂ -C ₂ H _5I -NH-S0 ₂ -C ₃ H _7I -NH-S0 ₂ -cyclo-C ₃ H ₅ , -NH-S0 ₂ -CH(CH ₃ ) ₂ ,

-CONH ₂ , -SOCH _S , -SOC ₂ H _5I -SOC ₃ H _7I -SO-cyclo-C ₃ H ₅ , -SOCH(CH ₃ ) ₂ , -SCH ₃ , -SOCF ₃ , -S0 ₂ CF _3I or -SO(NH)CH ₃ ;

R ^N1 and R ^N2 represents independently of each other -H, — CH ₃ , — C ₂ Hs, — C ₃ H ₇ ,

-CH(CH ₃ ) ₂ , cyclo-C ₃ H ₅ , cyclo-C ₄ H ₇ , -CH _2- CH(CH ₃ ) ₂ , -Ph, -CH _2- Ph, -COCHs, -COC ₂ H ₅ , -COC ₃ H _7I -CO-cyclo-C ₃ H ₅ , -COCH(CH ₃ ) ₂ , -COOCH ₃ , -COOC ₂ H ₅ , -COOC ₃ H _7I -COO-cyclo-C ₃ H ₅ , -COOCH(CH ₃ ) ₂ , -COOC(CH ₃ ) ₃ , -CH _2- CH(OH)-CH ₃ , -(CH ₂ ) _q- NH ₂ , -(CH ₂ ) _q- NHCH ₃ , -(CH ₂ ) _q- NHC ₂ H ₅ ,

-(CH ₂ ) _q- NHC ₃ H ₇ , — (CH ₂ ) _q— N(CH ₃ ) ₂ , -(CH ₂ ) _q- N(C ₂ H ₅ ) ₂ , -(CH ₂ ) _q- N(C ₃ H ₇ ) ₂ ,

Z ¹ , Z ² , Z ³ and Z ⁴ represent independently of each other -H, — CH ₃ , — C ₂ H ₅ , — C ₃ H ₇ ,

-CH(CH ₃ ) ₂ , -F, -Cl, -Br, -I, -CN, -CF ₃ ; m is an integer selected from 0, 1 , 2, or 3; n is an integer selected from 1 , or 2; p is an integer selected from 0, or 1 ; q is an integer selected from 1 , or 2; with the proviso that when X is -H, at least one of R ¹ - R ³ is not -H, when R ⁴ is -H, at least one of R ¹ - R ³ and R ⁵ - R ⁷ is not -H; and (E)-N-benzyl-2-cyano-3-(1 H- pyrrolo[2,3-b]pyridin-3-yl)acrylamide and (E)-N-(1 ,3-benzodioxol-5-yl-methyl)-2-cyano-3- (1 H-pyrrolo[2,3-b]pyridin-3-yl)acrylamide are excluded; or an enantiomer, a stereoisomeric form, a mixture of enantiomers, a diastereomer, a mixture of diastereomers, a hydrate, a solvate, an acid salt form, a tautomer, or a racemate of the above mentioned compound, or a pharmaceutically acceptable salt thereof . More preferred, is the compound of the formula (I) wherein

X represents -H or -CN,

Y represents CH or N,

R ³ represents -H, -CH ₃ , or -Br;

R ⁴ represents -H, -CH ₃ , -CF ₃ , -CN, -CH ₂ OH, -CH ₂ CH ₂ OH, -CH ₂ N(CH ₃ ) ₂ ,

-CH ₂ CH ₂ N(CH ₃ ) _2I or -CH ₂ CH ₂ N(CH ₂ CH ₃ ) ₂ ;

R ⁵ , R ⁶ and R ⁷ represents independently of each other -H, -F, -Cl, -Br,

-CN, , -CH ₃ , -CF _3I -OCH _{3 ,} -COCH3, -CONH ₂ , -NHCOCH ₃ , ,

-N(CH ₃ ) ₂ , -SO ₂ CH ₃ , -SO ₂ NH ₂ , -SO ₂ NHCH ₃ , -CH^SO ₂ NH ₂ , , -NH-SO ₂ -CH ₃ , with the proviso that when X is -H at least one of R ¹ - R ³ is not -H; when R ⁴ is -H, at least one of R ¹ - R ³ and R ⁵ - R ⁷ is not -H; and (E)-N-benzyl-2-cyano-3-(1 H- pyrrolo[2,3-b]pyridin-3-yl)acrylamide and (E)-N-(1 ,3-benzodioxol-5-yl-methyl)-2-cyano-3- (1 H-pyrrolo[2,3-b]pyridin-3-yl)acrylamide are excluded; or an enantiomer, a stereoisomeric form, a mixture of enantiomers, a diastereomer, a mixture of diastereomers, a hydrate, a solvate, an acid salt form, a tautomer, or a racemate of the above mentioned compound, or a pharmaceutically acceptable salt thereof.

More preferred, is the compound of the formula (la) wherein

X represents -H or -CN,

R ³ represents -H, -CH ₃ , or -Br; R ⁴ represents -H, -CH ₃ , -CF ₃ , -CN, -CH ₂ OH, -CH ₂ CH ₂ OH, -CH ₂ N(CH ₃ ) ₂ ,

-CH ₂ CH ₂ N(CH ₃ )2, or -CH ₂ CH ₂ N(CH ₂ CH ₃ )2;

R ⁵ , R ⁶ and R ⁷ represents independently of each other -H, -F, -Cl, -Br, -CN, , -CHs, -CF ₃ , -OCH _{3 ,} -COCH ₃ , -CONN _S , -NHCOCH ₃ , ,

-N(CH ₃ ) , -SO2CH3, -SO2NH2, -SO2NHCH3, -CH^SO ₂ NH ₂ , -NH-S0 ₂ -CH _3I with the proviso that when X is -H, at least one of R ¹ - R ³ is not -H, when R ⁴ is -H, at least one of R ¹ - R ³ and R ⁵ - R ⁷ is not -H; and (E)-N-benzyl-2-cyano-3-(1 H- pyrrolo[2,3-b]pyridin-3-yl)acrylamide and (E)-N-(1 ,3-benzodioxol-5-yl-methyl)-2-cyano-3- (1 H-pyrrolo[2,3-b]pyridin-3-yl)acrylamide are excluded; or an enantiomer, a stereoisomeric form, a mixture of enantiomers, a diastereomer, a mixture of diastereomers, a hydrate, a solvate, an acid salt form, a tautomer, or a racemate of the above mentioned compound, or a pharmaceutically acceptable salt thereof . Still more preferred, is the compound of the formula (la) wherein X represents H or -CN, R ¹ represents -H, -CHs, -Cl, -Ph,

R ³ represents -H, -CH ₃ , or -Br;

R ⁴ represents -H, -CH ₃ , -CF ₃ , -CN, -CH ₂ OH, -CH ₂ CH ₂ OH, -CH ₂ N(CH ₃ ) ₂ ,

-CH ₂ CH ₂ N(CH ₃ ) _2I or -CH ₂ CH ₂ N(CH ₂ CH ₃ ) ₂ ;

R ⁵ , R ⁶ and R ⁷ represents independently of each other -FI, -F, -Cl, -Br, -CN, , -CH ₃ , -CF _3I -OCH _{3 ,} -COCHs, -CONH ₂ , -NHCOCHs, ,

-N(CH ₃ ) _2I -S0 ₂ CH ₃ , -S0 ₂ NH _2I -S0 ₂ NHCH _3I -CH^SO ₂ NH ₂ , -NH-S0 ₂ -CH ₃ , or R ⁵ and R ⁶ , or R ⁶ and R ⁷ form preferably, R ⁵ and R ⁶ , or R ⁶ and R ⁷ form with the proviso that when X is -H, at least one of R ¹ - R ³ is not -FI, when R ⁴ is -FI, at least one of R ¹ - R ³ and R ⁵ - R ⁷ is not -FI; and (E)-N-benzyl-2-cyano-3-(1 Fl- pyrrolo[2,3-b]pyridin-3-yl)acrylamide and (E)-N-(1 ,3-benzodioxol-5-yl-methyl)-2-cyano-3- (1 FI-pyrrolo[2,3-b]pyridin-3-yl)acrylamide are excluded; or an enantiomer, a stereoisomeric form, a mixture of enantiomers, a diastereomer, a mixture of diastereomers, a hydrate, a solvate, an acid salt form, a tautomer, or a racemate of the above mentioned compound, or a pharmaceutically acceptable salt thereof .

In some embodiments, the present invention relates to the compound having any one of the formulae (la), (lb), (11-1) - (II-5):

wherein R ¹ , R ² , R ³ , R ⁴ , R ⁵ , R ⁶ , R ⁷ and X have the meanings as defined in the formula (I). In formulae (11-1 ) and (II-5) R ¹ is preferably not -H.

In formulae (II-2) and (II-6) R ² is preferably not -H.

In formulae (II-3) and (II-4) when X is -H at least one of R ¹ - R ³ is not -H and preferably at least one of R ⁵ , R ⁶ and R ⁷ is not -H; or more preferably in case X is -CN at least one of R ⁵ R ⁶ and R ⁷ is not -H.

Preferably, is the compound of any one of the formulae (11-1) to (II-6), wherein X represents -H or -CN,

R ¹ represents -H, -CH3, -Cl, -Ph,

R ² represents -H, -CH ₃ , -Ph, -Cl, -Br, CF ₃ , -CN, -OH, -NH-Ph, -0-CH ₂ CH _2- N(CH ₃ )2, -R ⁹ , -O-R ¹⁰ R ³ represents -H, -CH ₃ , or -Br;

R ⁴ represents -H, -CH ₃ , -CF ₃ , -CN, -CH ₂ OH, -CH ₂ CH ₂ OH, -CH ₂ N(CH ₃ ) ₂ ,

-CH ₂ CH ₂ N(CH ₃ ) ₂ , or -CH ₂ CH ₂ N(CH ₂ CH ₃ ) ₂ ; R ⁵ , R ⁶ and R ⁷ represents independently of each other -R ⁸ , -CH^R ⁸ , -SO^R ⁸ ,

-H, -F, -Cl, -Br, -CN, -CH ₃ , -CF ₃ , -OCH _{3 ,} -COCH ₃ , -CONH ₂ , -NHCOCH ₃ , ,

-N(CH ₃ ) _2I -SO ₂ CH ₃ , -SO ₂ NH ₂ , -SO ₂ NHCH ₃ , -CH^SO ₂ NH ₂ , , -NH-S0 ₂ -CH ₃ , or R ⁵ and R ⁶ , or R ⁶ and R ⁷ form

R ⁹ represents -H, R ¹¹ and R ¹² represent independently of each other -H, -CH ₃ , -C2H5, -C3H7,

-CH(CH ₃ ) ₂ , -CF _3I -(CH ₂ ) _m- NH ₂ , -(CH ₂ ) _m- NHCH ₃ , -(CH ₂ ) _m- NHC ₂ H ₅ , -(CH ₂ ) _m- NHC ₃ H ₇ , -(CH ₂ ) _m- N(CH ₃ ) ₂ , -(CH ₂ ) _m- N(C ₂ H ₅ ) ₂ , -(CH ₂ ) _m- N(C ₃ H ₇ ) ₂ ,

-OCH _3I -OC ₂ H _5I -OC ₃ H _7I -0-cyclo-C ₃ H ₅ , -OCH(CH ₃ ) ₂ , -F, -Cl, -Br,

-CN, -(CH ₂ ) _m -S0 ₂ CH ₃ , -(CH ₂ ) _m -S0 ₂ C ₂ H ₅ , -(CH ₂ ) _m -S0 ₂ C ₃ H ₇ ,

-(CH ₂ ) _m -SO^cyclo-C ₃ H ₅ , -(CH ₂ ) _m -S0 ₂ CH(CH ₃ ) ₂ , -(CH ₂ ) _m -S0 ₂ C(CH ₃ ) ₃ ,

-0-(CH ₂ ) _m- NH ₂ , -0-(CH ₂ ) _m- NHCH ₃ , -0-(CH ₂ ) _m- NHC ₂ H ₅ , -0-(CH ₂ ) _m- NHC ₃ H ₇ ,

-0-(CH ₂ ) _m- N(CH ₃ ) ₂ , -0-(CH ₂ ) _m- N(C ₂ H ₅ ) ₂ , -0-(CH ₂ ) _m- N(C ₃ H ₇ ) ₂ , -NHCOCH ₃ ,

-(CH ₂ ) _m- NHCOCH ₃ , -(CH ₂ ) _m -NHCOC ₂ H ₅ , -(CH ₂ ) _m- NHCO-cyclo-C ₃ H ₅ ,

-(CH ₂ ) _m- NHCOC ₃ H ₇ , -(CH ₂ ) _m- NHCO-CH(CH ₃ ) ₂ , -(CH ₂ ) _m- NHCO-CH=CH ₂ , -S0 ₂ NH _2I -S0 ₂ NHCH _3I -S0 ₂ NHC ₂ H _5I -S0 ₂ NHC ₃ H _7I -S0 ₂ NH-cyclo-C ₃ H ₅ , -S0 ₂ NHCH(CH ₃ ) _2I -S0 ₂ N(CH ₃ ) _2I -S0 ₂ N(C ₂ H ₅ ) _2I -S0 ₂ N(C ₃ H ₇ ) _2I

-S0 ₂ N(cyclo-C ₃ H ₅ ) ₂ , -S0 ₂ N[CH(CH ₃ ) ₂ ] ₂ , -NH-SO^CH ₃ , -NH-S0 ₂ -C ₂ H ₅ ,

-NH-S0 ₂ -C ₃ H ₇ , -NH-S0 ₂ -cyclo-C ₃ H ₅ , -NH-S0 ₂ -CH(CH ₃ ) ₂ , -CONH ₂ , -SOCHs, -SOC ₂ H _5I -SOC ₃ H _7I -SO-cyclo-C ₃ H ₅ , -SOCH(CH ₃ ) ₂ , -SCH ₃ , -SOCF ₃ , -S0 ₂ CF _3I or -SO(NH)CH ₃ ;

Preferably, R ¹¹ and R ¹² represent independently of each other -FI, — CH ₃ , — C ₂ H ₅ , C ₃ H ₇ , CH(CH ₃ ) _2I CF _3I (CH ₂ ) _m N(CH ₃ ) ₂ , (CH ₂ ) _m N(C ₂ H ₅ ) _2I -OCH ₃ , -OC ₂ H _5I -OC ₃ H ₇ , -O-cyclo-CsHs, -OCH(CH ₃ ) ₂ , -F, -Cl, -Br,

-CN, -(CH ₂ ) _m -S0 ₂ CH ₃ , -(CH ₂ ) _m -SO^cyclo-C ₃ H ₅ , -0-(CH ₂ ) _m- N(CH ₃ ) ₂ ,

— 0— (CH ₂ ) _m— N(C ₂ H ₅ ) ₂ , -NHCOCH _S , -(CH ₂ ) _m- NHCOCH ₃ , -(CH ₂ ) _m -NHCOC ₂ H ₅ ,

-(CH ₂ ) _m- NHCO-cyclo-C ₃ H ₅ , -(CH ₂ ) _m- NHCO-CH(CH ₃ ) ₂ , -(CH ₂ ) _m- NHCO-CH=CH ₂ ,

-S0 ₂ NH ₂ , -SO ₂ NHCH ₃ , -SO ₂ NHC ₂ H ₅ , -SO ₂ NHC ₃ H ₇ ,

-S0 ₂ NH-cyclo-C ₃ H ₅ , -S0 ₂ NHCH(CH ₃ ) ₂ , -S0 ₂ N(CH ₃ ) ₂ , -S0 ₂ N(C ₂ H ₅ ) ₂ ,

-S0 ₂ N(C ₃ H ₇ ) _2I -S0 ₂ N(cyclo-C ₃ H ₅ ) ₂ , -S0 ₂ N[CH(CH ₃ ) ₂ ] ₂ , -NH-S0 ₂ -CH ₃ ,

-NH-S0 ₂ -C ₂ H ₅ , -NH-S0 ₂ -C ₃ H ₇ , -NH-S0 ₂ -cyclo-C ₃ H ₅ , -NH-S0 ₂ -CH(CH ₃ ) ₂ ,

-CONH ₂ , -SOCH _S , -SOC ₂ H _5I -SOC ₃ H _7I -SO-cyclo-C ₃ H ₅ , -SOCH(CH ₃ ) ₂ , -SCH ₃ , -SOCF ₃ , -S0 ₂ CF _3I or -SO(NH)CH ₃ ;

More preferably, R ¹¹ and R ¹² represent independently of each other -H, -CH ₃ ,

-C ₂ H ₅ , -CF _3I -(CH ₂ ) _m- N(CH ₃ ) ₂ , -OCH ₃ , -OC ₂ H _5I -F, -Cl, -Br, -CN, -(CH ₂ ) _m -S0 ₂ CH ₃ , -(CH ₂ ) _m -SO^cyclo-C ₃ H ₅ , -0-(CH ₂ ) _m- N(CH ₃ ) ₂ ,

-NHCOCHs, -(CH ₂ ) _m- NHCOCH ₃ , -(CH ₂ ) _m- NHCO-CH=CH ₂ , -S0 ₂ NH ₂ ,

-S0 ₂ NHCH ₃ , -S0 ₂ N(CH ₃ ) ₂ , -S0 ₂ N(C ₂ H ₅ ) ₂ , -S0 ₂ N(C ₃ H ₇ ) _2I -NH-SO ₂ -CH ₃ ,

NH-S0 ₂ -C ₂ H _5I NH-S0 ₂ -C ₃ H _7I NH-S0 ₂ -cyclo-C ₃ H ₅ , NH-S0 ₂ -CH(CH ₃ ) ₂ ,

-CONH ₂ , -SOCH _S , -SOC ₂ H _5I -SOC ₃ H _7I -SO-cyclo-C ₃ H ₅ , -SOCH(CH ₃ ) ₂ , -SCH ₃ , -SOCF ₃ , -S0 ₂ CF _3I or -SO(NH)CH ₃ ; R ^N1 and R ^N2 represents independently of each other -H, -CH ₃ , -C2H5, -C3H7,

-CH(CH ₃ ) ₂ , cyclo-C ₃ H ₅ , cyclo-C ₄ H ₇ , -CH _2- CH(CH ₃ ) ₂ , -Ph, -CH _2- Ph, -COCHs, -COC ₂ H ₅ , -COC ₃ H _7I -CO-cyclo-C ₃ H ₅ , -COCH(CH ₃ ) ₂ , -COOCH ₃ , -COOC ₂ H ₅ , -COOC ₃ H _7I -COO-cyclo-C ₃ H ₅ , -COOCH(CH ₃ ) ₂ , -COOC(CH ₃ ) ₃ , -CH _2- CH(OH)-CH ₃ , -(CH ₂ ) _q- NH ₂ , -(CH ₂ ) _q- NHCH ₃ , -(CH ₂ ) _q- NHC ₂ H ₅ ,

-(CH ₂ ) _q- NHC ₃ H ₇ , -(CH ₂ ) _q- N(CH ₃ ) ₂ , -(CH ₂ ) _q- N(C ₂ H ₅ ) ₂ , -(CH ₂ ) _q- N(C ₃ H ₇ ) ₂ ,

Z ¹ , Z ² , Z ³ and Z ⁴ represent independently of each other -H, -CH ₃ , -C ₂ H5, -C ₃ H ₇ ,

-CH(CH ₃ ) _2I -F, -Cl, -Br, -I, -CN, -CF ₃ ; m is an integer selected from 0, 1, 2, or 3; n is an integer selected from 1 , or 2; p is an integer selected from 0, or 1 ; q is an integer selected from 1 , or 2; with the proviso that when X is -H, at least one of R ¹ - R ³ is not -H; when R ⁴ is -H, at least one of R ¹ - R ³ and R ⁵ - R ⁷ is not -H; and (E)-N-benzyl-2-cyano-3-(1 H- pyrrolo[2,3-b]pyridin-3-yl)acrylamide and (E)-N-(1 ,3-benzodioxol-5-yl-methyl)-2-cyano-3- (1 H-pyrrolo[2,3-b]pyridin-3-yl)acrylamide are excluded;

More preferably, is the compound of any one of the formulae (11-1) to (II-6), wherein X represents -H or -CN;

R ¹ and R ² represents independently of each other -H, -CH ₃ , -Ph, -Cl, -Br,

-CF ₃ , -CN, -OH, -NH-Ph, -0-CH(CH ₃ ) ₂ ,

-0-CH ₂ CH(CH ₃ ) ₂ , -0-CH(CH ₃ )(CH ₂ CH ₃ ), -0-CH ₂ CH _2- N(CH ₃ ) ₂ ,

, -H, at least one of R ¹ - R ³ and R ⁵ - R ⁷ is not -H; and (E)-N-benzyl-2-cyano-3-(1 H- pyrrolo[2,3-b]pyridin-3-yl)acrylamide and (E)-N-(1 ,3-benzodioxol-5-yl-methyl)-2-cyano-3- (1 H-pyrrolo[2,3-b]pyridin-3-yl)acrylamide are excluded;

Still more preferably, is the compound of any one of the formulae (11-1) to (II-6), wherein X represents -H or -CN,

R ¹ represents -H, -CH ₃ , -Cl, -Ph,

R ³ represents -H, -CH3, or -Br;

R ⁴ represents -H, -CH ₃ , -CF ₃ , -CN, -CH ₂ OH, -CH ₂ CH ₂ OH, -CH ₂ N(CH ₃ ) ₂ ,

-CH ₂ CH ₂ N(CH ₃ ) _2I or -CH ₂ CH ₂ N(CH ₂ CH ₃ ) ₂ ;

R ⁵ , R ⁶ and R ⁷ represents independently of each other -H, -F, -Cl, -Br, -CN, , -CH ₃ , -CF _3I -OCH _{3 ,} -COCHs, -CONH ₂ , -NHCOCHs, ,

-N(CH ₃ ) _2I -SO ₂ CH ₃ , -SO ₂ NH ₂ , -SO ₂ NHCH ₃ , -CH^SO ₂ NH ₂ , -NH-S0 ₂ -CH ₃ , with the proviso that when X is -H, at least one of R ¹ - R ³ is not -H; when R ⁴ is -H, at least one of R ¹ - R ³ and R ⁵ - R ⁷ is not -H; and (E)-N-benzyl-2-cyano-3-(1 H- pyrrolo[2,3-b]pyridin-3-yl)acrylamide and (E)-N-(1 ,3-benzodioxol-5-yl-methyl)-2-cyano-3- (1 FI-pyrrolo[2,3-b]pyridin-3-yl)acrylamide are excluded;

In some embodiments, the present invention relates to the compound having any one of the formulae (MI-1) - (MI-6):

wherein R ¹ , R ² , R ³ , R ⁴ , R ⁶ , R ⁷ and X have the meanings as defined in the formula (I).

In formulae (III-4), (III-5) and (III-6) R ² is preferably not -H.

In formulae (III-2) and (MI-3) when X is -H at least one of R ¹ - R ³ is not -H and preferably at least one of R ⁶ and R ⁷ is not -H; or more preferably in case X is -CN at least one of R ⁶ and R ⁷ is not -H.

In formula (MI-1) when X is -H at least one of R ¹ - R ³ is not -H and preferably at least one of R ⁶ and R ⁷ is not -H; or more preferably in case X is -CN or R ⁴ is -H or -C ₂ H ₅ or -CH ₂ OH or -C ₂ H ₄ OH, at least one of R ⁶ and R ⁷ is not -H; or still more preferably in case X is -CN and R ⁴ is -H or -C ₂ H ₅ or -CH ₂ OH or -C ₂ H ₄ OH, at least one of R ⁶ and R ⁷ is not -H.

Preferably, is the compound of any one of the formulae (MI-1 ) to (MI-6), wherein X represents -H or -CN, R

R ² represents -H, -CH ₃ , -Ph, -Cl, -Br, CF ₃ , -CN, -OH, -NH-Ph, -0-CH ₂ CH2-N(CH ₃ )2, -R ⁹ , -O-R ¹⁰

R ³ represents -H, -CH ₃ , or -Br;

R ⁴ represents -H, -CH ₃ , -CF ₃ , -CN, -CH ₂ OH, -CH ₂ CH ₂ OH, -CH ₂ N(CH ₃ ) ₂ , -CH ₂ CH ₂ N(CH ₃ ) ₂ , or -CH ₂ CH ₂ N(CH ₂ CH ₃ ) ₂ ;

R ⁶ and R ⁷ represents independently of each other -R ⁸ , -CH2-R ⁸ , -S0 ₂ -R ⁸ , - H, preferably, R ⁶ and R ⁷ form

R ⁸ represents

R ¹¹ and R ¹² represent independently of each other -H, -CH ₃ , -C ₂ H , -C ₃ H , -CH(CH ₃ ) ₂ , -CF _3I -(CH ₂ ) _m- NH ₂ , -(CH ₂ ) _m- NHCH ₃ , -(CH ₂ ) _m- NHC ₂ H ₅ ,

-(CH ₂ ) _m- NHC ₃ H ₇ , -(CH ₂ ) _m- N(CH ₃ ) ₂ , -(CH ₂ ) _m- N(C ₂ H ₅ ) ₂ , -(CH ₂ ) _m- N(C ₃ H ₇ ) ₂ , -OCH3, -OC2H5, -OC3H7, -O-cyclo-CsHs, -OCH(CH ₃ ) ₂ , -F, -Cl, -Br,

-CN, -(CH ₂ )m-S0 ₂ CH3, -(CH ₂ ) _m -S0 ₂ C ₂ H ₅ , -(CH ₂ ) _m -S0 ₂ C ₃ H ₇ ,

-(CH ₂ ) _m -SO^cyclo-C ₃ H ₅ , -(CH ₂ ) _m -S0 ₂ CH(CH ₃ ) ₂ , -(CH ₂ ) _m -S0 ₂ C(CH ₃ ) ₃ ,

-0-(CH ₂ ) _m- NH ₂ , -0-(CH ₂ ) _m- NHCH ₃ , -0-(CH ₂ ) _m- NHC ₂ H ₅ , -0-(CH ₂ ) _m- NHC ₃ H ₇ ,

-0-(CH ₂ ) _m- N(CH ₃ ) ₂ , -0-(CH ₂ ) _m- N(C ₂ H ₅ ) ₂ , -0-(CH ₂ ) _m- N(C ₃ H ₇ ) ₂ , -NHCOCH3,

-(CH ₂ ) _m- NHCOCH ₃ , -(CH ₂ ) _m -NHCOC ₂ H ₅ , -(CH ₂ ) _m- NHCO-cyclo-C ₃ H ₅ ,

-(CH ₂ ) _m- NHCOC ₃ H ₇ , -(CH ₂ ) _m- NHCO-CH(CH ₃ ) ₂ , -(CH ₂ ) _m- NHCO-CH=CH ₂ , -S0 ₂ NH _2I -S0 ₂ NHCH _3I -S0 ₂ NHC ₂ H _5I -S0 ₂ NHC ₃ H _7I -S0 ₂ NH-cyclo-C ₃ H ₅ , -S0 ₂ NHCH(CH ₃ ) _2I -S0 ₂ N(CH ₃ ) _2I -S0 ₂ N(C ₂ H ₅ ) _2I -S0 ₂ N(C ₃ H ₇ ) _2I

-S0 ₂ N(cyclo-C ₃ H ₅ ) _2l -S0 ₂ N[CH(CH ₃ ) ₂ ] ₂ , -NH-SO2-CH3, -NH-S0 ₂ -C ₂ H ₅ , -NH-S0 ₂ -C ₃ H ₇ , -NH-S0 ₂ -cyclo-C ₃ H ₅ , -NH-S0 ₂ -CH(CH ₃ ) ₂ , -CONH ₂ , -SOCH3, -SOC ₂ H _5I -SOC ₃ H _7I -SO-cyclo-C ₃ H ₅ , -SOCH(CH ₃ ) ₂ , -SCH ₃ , -SOCF3, -S0 ₂ CF _3I or -SO(NH)CH ₃ ;

Preferably, R ¹¹ and R ¹² represent independently of each other -H, -CH ₃ , -C ₂ H ₅ ,

-C ₃ H _7I -CH(CH ₃ ) ₂ , -CF _3I -(CH ₂ ) _m- N(CH ₃ ) ₂ , -(CH ₂ ) _m- N(C ₂ H ₅ ) ₂ , -OCH3, -OC ₂ H ₅ , -OC ₃ H ₇ , -0-cyclo-C ₃ H ₅ , -OCH(CH ₃ ) ₂ , -F, -Cl, -Br,

-CN, -(CH ₂ ) _m -S0 ₂ CH ₃ , -(CH ₂ ) _m -SO^cyclo-C ₃ H ₅ , -0-(CH ₂ ) _m- N(CH ₃ ) ₂ ,

-0-(CH ₂ ) _m- N(C ₂ H ₅ ) ₂ , -NHCOCH3, -(CH ₂ ) _m- NHCOCH ₃ , -(CH ₂ ) _m -NHCOC ₂ H ₅ ,

(CH ₂ ) _m NHCO-cyclo-C ₃ H ₅ , (CH ₂ ) _m NHCO-CH(CH ₃ ) ₂ , (CH ₂ ) _m NHCO-CH=CH ₂ ,

-S0 ₂ NH ₂ , -SO ₂ NHCH ₃ , -SO ₂ NHC ₂ H ₅ , -SO ₂ NHC ₃ H ₇ ,

-S0 ₂ N H-cyclo-C ₃ H ₅ , -S0 ₂ NHCH(CH ₃ ) ₂ , -S0 ₂ N(CH ₃ ) ₂ , -S0 ₂ N(C ₂ H ₅ ) ₂ ,

-S0 ₂ N(C ₃ H ₇ ) _2I -S0 ₂ N(cyclo-C ₃ H ₅ ) ₂ , -S0 ₂ N[CH(CH ₃ ) ₂ ]2, -NH-SO2-CH3,

-NH-SO ₂ -C ₂ H ₅ , -NH-S0 ₂ -C ₃ H ₇ , -NH-S0 ₂ -cyclo-C ₃ H ₅ , -NH-S0 ₂ -CH(CH ₃ ) ₂ ,

-CONH ₂ , -SOCH ₃ , -SOC ₂ H ₅ , -SOC ₃ H ₇ , -SO-cyclo-C ₃ H ₅ , -SOCH(CH ₃ ) ₂ , -SCH ₃ , -SOCF ₃ , -SO ₂ CF ₃ , or -SO(NH)CH ₃ ;

More preferably, R ¹¹ and R ¹² represent independently of each other -H, -CH ₃ ,

-C ₂ H ₅ , -CF ₃ , -(CH ₂ ) _m- N(CH ₃ ) ₂ , -OCH ₃ , -OC ₂ H ₅ , -F, -Cl, -Br,

-CN, -(CH ₂ ) _m -S0 ₂ CH ₃ , -(CH ₂ ) _m -S0 ₂ -cyclo-C ₃ H ₅ , -0-(CH ₂ ) _m- N(CH ₃ ) ₂ ,

-NHCOCH ₃ , -(CH ₂ ) _m- NHCOCH ₃ , -(CH ₂ ) _m- NHCO-CH=CH ₂ , -S0 ₂ NH ₂ , -SO2NHCH3, -S0 ₂ N(CH ₃ ) ₂ , -S0 ₂ N(C ₂ H5)2, -S0 ₂ N(C ₃ H ₇ ) ₂ , -NH-SO2-CH3,

-NH-S0 ₂ -C ₂ H ₅ , -NH-S0 ₂ -C ₃ H ₇ , -NH-S0 ₂ -cyclo-C ₃ H ₅ , -NH-S0 ₂ -CH(CH ₃ ) ₂ ,

-CONH ₂ , -SOCH ₃ , -SOC ₂ H ₅ , -SOC ₃ H ₇ , -SO-cyclo-C ₃ H ₅ , -SOCH(CH ₃ ) ₂ , -SCH ₃ , -SOCF ₃ , -S0 ₂ CF ₃ , or -SO(NH)CH ₃ ;

R ⁿ¹ and R ^N2 represents independently of each other -H, -CH ₃ , -C ₂ H ₅ , -C ₃ H ₇ ·,

-CH(CH ₃ ) ₂ , cyclo-C ₃ H ₅ , cyclo-C ₄ H ₇ , -CH _2- CH(CH ₃ ) ₂ , -Ph, -CH _2- Ph, -COCH ₃ , -COC ₂ H ₅ , -COC ₃ H ₇ , -CO-cyclo-C ₃ H ₅ , -COCH(CH ₃ ) ₂ , -COOCH ₃ , -COOC2H5, -COOC3H7, -COO-cyclo-CsHs, -COOCH(CH ₃ ) ₂ , -COOC(CH ₃ ) ₃ , -CH _2- CH(OH)-CH ₃ , -(CH ₂ ) _q- NH ₂ , -(CH ₂ ) _q- NHCH ₃ , -(CH ₂ ) _q- NHC ₂ H ₅ ,

-(CH ₂ ) _q- NHC ₃ H ₇ , -(CH ₂ ) _q- N(CH ₃ ) ₂ , -(CH ₂ ) _q- N(C ₂ H ₅ ) ₂ , -(CH ₂ ) _q- N(C ₃ H ₇ ) ₂ ,

Z ¹ , Z ² , Z ³ and Z ⁴ represent independently of each other -H, -CH ₃ , -C ₂ H5, -C ₃ H ₇ ,

-CH(CH ₃ ) _2I -F, -Cl, -Br, -I, -CN, -CF ₃ ; m is an integer selected from 0, 1 , 2, or 3; n is an integer selected from 1 , or 2; p is an integer selected from 0, or 1 ; q is an integer selected from 1 , or 2; with the proviso that when X is -H, at least one of R ¹ - R ³ is not -H; when R ⁴ is -H, at least one of R ¹ - R ³ and R ⁵ - R ⁷ is not -H; and (E)-N-benzyl-2-cyano-3-(1 H- pyrrolo[2,3-b]pyridin-3-yl)acrylamide and (E)-N-(1 ,3-benzodioxol-5-yl-methyl)-2-cyano-3- (1 FI-pyrrolo[2,3-b]pyridin-3-yl)acrylamide are excluded.

More preferably, is the compound of any one of the formulae (III-1) to (III-6), wherein X represents -FI or -CN;

R ¹ and R ² represents independently of each other H, CFH ₃ , Ph, -Cl, -Br, -CF ₃ , -CN, -OH, -NH-Ph, -0-CH(CH ₃ ) ₂ ,

-0-CH ₂ CH(CH ₃ ) ₂ , -0-CH(CH ₃ )(CH ₂ CH ₃ ), -0-CH ₂ CH _2- N(CH ₃ ) ₂ ,

with the proviso that when X is -H, at least one of R ¹ - R ³ is not -H; when R ⁴ is -H, at least one of R ¹ - R ³ and R ⁵ - R ⁷ is not -H; and (E)-N-benzyl-2-cyano-3-(1 H- pyrrolo[2,3-b]pyridin-3-yl)acrylamide and (E)-N-(1 ,3-benzodioxol-5-yl-methyl)-2-cyano-3- (1 H-pyrrolo[2,3-b]pyridin-3-yl)acrylamide are excluded.

Still more preferably, is the compound of any one of the formulae (111-1 ) to (MI-6), wherein X represents -H or -CN,

R ¹ represents -H, -CH ₃ , -Cl, -Ph,

R ³ represents -H, -CH ₃ , or -Br; R ⁴ represents -H, -CH ₃ , -CF ₃ , -CN, -CH ₂ OH, -CH ₂ CH ₂ OH, -CH ₂ N(CH ₃ ) _2I

-CH ₂ CH ₂ N(CH ₃ )2, or -CH ₂ CH ₂ N(CH ₂ CH ₃ )2;

R ⁶ and R ⁷ represents independently of each other -H, -F, -Cl, -Br, -CN, , -CHs, -CF _3I -OCH3 _, -COCH3, -CONN _S , -NHCOCH3, ,

-N(CH _3)2, -SO2CH3, -SO2NH2, -SO2NHCH3, -CH^SO ₂ NH _2, -NH-SO ₂ -CH _3, with the proviso that when X is -H, at least one of R ¹ - R ³ is not -H; when R ⁴ is -H, at least one of R ¹ - R ³ and R ⁵ - R ⁷ is not -H; and (E)-N-benzyl-2-cyano-3-(1 H- pyrrolo[2,3-b]pyridin-3-yl)acrylamide and (E)-N-(1 ,3-benzodioxol-5-yl-methyl)-2-cyano-3- (1 H-pyrrolo[2,3-b]pyridin-3-yl)acrylamide are excluded.

In some embodiments, the present invention relates to the compound having any one of the formulae (IV-1) - (IV-6) and (V-1) - (V-6):

wherein R ¹ , R ² , R ³ , R ⁴ R ⁶ , R ⁷ , R ⁹ , R ¹¹ , R ¹² , R ^N2 , X, Z ³ , and Z ⁴ have the meanings as defined in the formula (I). In formulae (IV-4), (IV-5) and (IV-6) R ² is preferably not -H.

In formula (V-1 ) one of R ⁶ and R ⁷ is preferably not -H.

Preferably, is the compound of any one of the formulae (IV-1) to (IV-6),

wherein

X represents -H or -CN,

R ¹ represents -H, -CH ₃ , -Cl, -Ph,

R ² represents -H, -CH ₃ , -Ph, -Cl, -Br, -CF ₃ , -CN, -OH, -NH-Ph, -0-CH ₂ CH _2- N(CH ₃ ) ₂ , -R ⁹ -O-R ¹⁰ ,

R ³ represents -H, -CH ₃ , or -Br;

R ⁴ represents -H, -CH ₃ , -CF ₃ , -CN, -CH ₂ OH, -CH ₂ CH ₂ OH, -CH ₂ N(CH ₃ ) ₂ , -CH ₂ CH ₂ N(CH ₃ ) ₂ , or -CH ₂ CH ₂ N(CH ₂ CH ₃ ) ₂ ;

R ⁹ represents -H, R ¹¹ and R ¹² represent independently of each other -H, -CH ₃ , -C2H5, -C3H7,

-CH(CH ₃ ) ₂ , -CF _3I -(CH ₂ ) _m- NH ₂ , -(CH ₂ ) _m- NHCH ₃ , -(CH ₂ ) _m- NHC ₂ H ₅ , -(CH ₂ ) _m- NHC ₃ H ₇ , -(CH ₂ ) _m- N(CH ₃ ) ₂ , -(CH ₂ ) _m- N(C ₂ H ₅ ) ₂ , -(CH ₂ ) _m- N(C ₃ H ₇ ) ₂ ,

-OCH _3I -OC ₂ H _5I -OC ₃ H _7I -0-cyclo-C ₃ H ₅ , -OCH(CH ₃ ) ₂ , -F, -Cl, -Br,

-CN, -(CH ₂ ) _m -S0 ₂ CH ₃ , -(CH ₂ ) _m -S0 ₂ C ₂ H ₅ , -(CH ₂ ) _m -S0 ₂ C ₃ H ₇ ,

-(CH ₂ ) _m -SO^cyclo-C ₃ H ₅ , -(CH ₂ ) _m -S0 ₂ CH(CH ₃ ) ₂ , -(CH ₂ ) _m -S0 ₂ C(CH ₃ ) ₃ ,

-0-(CH ₂ ) _m- NH ₂ , -0-(CH ₂ ) _m- NHCH ₃ , -0-(CH ₂ ) _m- NHC ₂ H ₅ , -0-(CH ₂ ) _m- NHC ₃ H ₇ ,

-0-(CH ₂ ) _m- N(CH ₃ ) ₂ , -0-(CH ₂ ) _m- N(C ₂ H ₅ ) ₂ , -0-(CH ₂ ) _m- N(C ₃ H ₇ ) ₂ , -NHCOCH ₃ ,