Heterocyclic Compounds

Matches 851 - 900 out of 3,661	< 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 >

Document	Document Title
WO/2001/046135A1	SYNTHESIS OF CHIRAL 2-AZETIDINEMETHANOL COMPOUNDS A process for preparing chiral isomers of N-protected 2-azetidinemethanol compounds of formula (5), particularly N-(phenylmethyl)-2-azetidinemethanol and N-BOC-2-azetidinemethanol, and especially the (R)-isomers thereof, as well as O-sub...
WO/2001/041724A2	COMPOSITIONS FOR DYEING KERATINIC FIBRES, CONTAINING PARAPHENYLENEDIAMINE DERIVATIVES WITH AN AZETIDINYL GROUP The invention relates to novel compositions for oxidation dyeing keratinic fibres, containing at least one paraphenylenediamine derivative with an azetidinyl group of formulae (I) and (II) as the oxidation base; to the dyeing method and ...
WO/2001/042249A1	OLEFIN POLYMERIZATION COCATALYSTS DERIVED FROM GROUP-15 COMPOUNDS AND PROCESSES USING THEM Fluorinated amine compounds, R'¿i?ArF-ER¿2?, where ArF is a fluoroaryl substituent, E is nitrogen or phosphorous, each R is independently a C¿1?-C¿20? hydrocarbyl substituent, or the two R's may be connected to form an unsubstituted ...
WO/2001/029245A2	ENZYMATIC PROCESS FOR THE RESOLUTION OF ENANTIOMERIC MIXTURES OF $g(b)-LACTAMS A process for the resolution of an enantiomeric mixture of $g(b)-lactams containing an ester, the process comprising selectively hydrolyzing the ester of one of the enantiomers by combining the mixture with homogenized liver.
WO/2001/019816A1	NOVEL SPIROHETEROCYCLIC COMPOUNDS USEFUL AS REVERSIBLE INHIBITORS OF CYSTEINE PROTEASES Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for makin...
WO/2001/017956A1	SUBSTITUTED N-PHENYL 2-HYDROXY-2-METHYL-3,3,3-TRIFLUOROPROPANAMIDE DERIVATIVES WHICH ELEVATE PYRUVATE DEHYDROGENASE ACTIVITY A compound of formula (I) wherein: n is 1 or 2; R?1¿ is chloro, fluoro, bromo, methyl or methoxy; R?2¿ is as defined within; R?3¿ is as defined within; and R?4¿ is hydrogen or fluoro; or a pharmaceutically acceptable salt or an in vi...
WO/2001/012186A1	CELL ADHESION INHIBITORS A cell adhesion inhibitor of the general formula: R?3¿-L-L'-R?1¿ is disclosed. An inhibitor of the present invention interacts with VLA-4 molecules and inhibits VLA-4 dependent cell adhesion. Also disclosed are methods for preparing an...
WO/2001/010842A2	MELANOCORTIN-4 RECEPTOR BINDING COMPOUNDS AND METHODS OF USE THEREOF MC4-R binding compounds of the formula (I): B-Z-E wherein B is an anchor moiety, Z is a central moiety, and E is an MC4-R interacting moiety are discussed. Methods of using the compounds to treat MC4-R associated disorders, such as disor...
WO/2001/007043A1	AZETIDINE CARBOXAMIDE DERIVATIVES FOR THE TREATMENT OF CNS DISORDERS Use of a compound of formula (I) wherein R?1¿ is aryl; and R?2¿, R?3¿, R?4¿, R?5¿ and R?6¿ which may be the same or different are selected from H, alkyl and aryl, or a pharmaceutically acceptable salt or prodrug thereof, in the man...
WO/2001/007438A1	ENANTIOSELECTIVE ACYLATION OF CIS RACEMIC AZETIDINONES Cis- beta -lactam compounds having structure (II) are described herein which are prepared by enantioselective acylation of the free amine in the presence of Penicillin G Amidase.
WO/2001/007023A2	AZETIDINE COMPOUNDS IN CNS AND EYE DISEASES Use of a compound of formula (I) wherein: R?1¿ is aryl; R?2¿ is H, alkyl or aryl; and R?3¿ is hydrogen or alkyl; or a pharmaceutically acceptable salt or prodrug thereof, in the manufacture of a medicament for neuroprotection in a sub...
WO/2001/007022A2	AZETIDINE COMPOUNDS IN CNS AND EYE DISEASES Use of a compound of formula (I) wherein R?1¿ is aryl; and R?2¿ is hydrogen or alkyl; or a pharmaceutically acceptable salt or prodrug thereof in the manufacture of a medicament for neuroprotection in a subject or for the treatment of ...
WO/2001/004091A1	NEUROTROPHIC 2-AZETIDINECARBOXYLIC ACID DERIVATIVES, AND RELATED COMPOSITIONS AND METHODS Compounds having general structure (a) wherein R?1¿ is selected from the group consisting of COCOR?2¿, CONHR?3¿, SO¿2?R?4¿ and (b). X and Y are (i) C=O and (ii) O or NR?5¿, Z is (C¿1?-C¿5?)-straight or branched alkyl or alkenyl s...
WO/2001/002426A1	A SUBSTANTIALLY CRYSTALLINE FORM OF MELAGATRAN There is provided melagatran in a form which is substantially crystalline. It has been found that crystalline forms of melagatran have a high chemical and solid state stability when compared to amorphous forms of the compound.
WO/2000/076964A1	PROCESS FOR REDUCTION OF (2R)-4-OXOAZETIDINONE-2-CARBOXYLIC ACID The present invention relates to a process for the reduction of an azetidinone-carboxylic acid to an azetidine-alcohol.
WO/2000/071511A2	INHIBITORS OF FACTOR Xa Compounds of the formula A - Y - D - E - G - J - Z - L in which D is a direct link, a substituted or unsubstituted phenyl or naphtyl group or a heterocyclic ring system; Z is a substituted or unsubstituted phenyl or naphthyl group or a h...
WO/2000/071508A2	INHIBITORS OF FACTOR Xa Compounds of the formula A - Y - D - E - G - J - Z - L in which D is a direct link, a substituted or unsubstituted phenyl or naphthyl group or a heterocyclic ring system and the other variables are as defined in the claims, their salts a...
WO/2000/071510A2	INHIBITORS OF FACTOR Xa Compounds of formula A - Y - D - E - G - J - Z - L in which D is direct link, a substutited or unsubstituted phenyl or napththyl group or a heterocyclic ring system; and the other variables are as defined in the claims, their salts and c...
WO/2000/071518A2	HETEROCYCLIC ANALGESIC COMPOUNDS AND THEIR USE One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate rece...
WO/2000/071572A1	SUBSTITUTED BETA-ALANINE DERIVATIVES AS CELL ADHESION INHIBITORS $g(b)-Alanine derivatives of Formula (I) are antagonists of VLA-4 and/or $g(a)4$g(b)7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into...
WO/2000/069816A1	METABOTROPIC GLUTAMATE RECEPTOR ANTAGONISTS This invention relates to a novel series of compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of stimulation of the human Group I metabotropic glutamate receptors, especially ...
WO/2000/069817A1	PROCESS FOR PRODUCING OPTICALLY ACTIVE AZETIDINE-2-CARBOXYLIC ACIDS A compound (5) can be produced by preparing a compound (3) by subjecting compound (1) to halogenation with inversion to obtain a compound (2) and hydrolyzing the compound (2), by subjecting a compound (6) to halogenation with inversion t...
WO/2000/068193A1	NEW PROCESS There is provided a process for the production of a N-Benzyl azetidine-2-carboxylic acid alkylphenyl, or alkyl, ester which process comprises the reaction of an optionally substituted alkylphenyl, or an optionally substituted alkyl, 2-br...
WO/2000/066557A1	NEW COMPOUNDS The present invention relates to compounds of Formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatm...
WO/2000/063168A1	SYNTHESIS OF AZETIDINE DERIVATIVES The present invention provides compound having formula (I), useful as building blocks for combinatorial libraries and methods of making such compounds. Also provided is a novel process for synthesizing such compounds. In addition, the pr...
WO/2000/059881A1	SUBSTITUTED AZETIDIN-2-ONES AS CYSTEINE PROTEASE INHIBITORS This invention relates to substituted azetidin-2-ones and to pharmaceutical compositions containing such compounds. Their use in medicine as inhibitors of cysteine proteases, particularly the cathepsins is also described. The invention i...
WO/2000/060107A1	STEREOSELECTIVE MICROBIAL REDUCTION FOR THE PREPARATION OF 1 - (4-FLUOROPHENYL) - 3(R)-[3(S) - HYDROXY-3 - (4-FLUOROPHENYL) PROPYL)]-4(S) - (4-HYDROXYPHENYL)-2-AZETIDINONE A process for the stereoselective microbial reduction of compound of formula (II) to compound of formula (I) comprising adding compound of formula (II) to a medium, medium and buffer, medium and solvent, or medium and a mixture of buffer...
WO/2000/059880A1	CELL ADHESION-INHIBITING ANTIINFLAMMATORY AND IMMUNE-SUPPRESSIVE COMPOUNDS The present invention relates to cinnamide compounds of formula (I), in which at least one of R¿1? to R¿5? is a '$i(cis)-cinnamide' (a) or a '$i(trans)-cinnamide' (b) and the other variables are as defined in the claims, that are usefu...
WO/2000/058283A1	BIOCATALYST AND ITS USE IN ENZYMATIC RESOLUTION OF RACEMIC BETA-LACTAMS A process for the preparation of an enantiomerically enriched $g(b)-lactam, comprises enantioselective hydrolysis of the corresponding racemic $g(b)-lactam in the presence of a lactamase enzyme capable of enantioselective hydrolysis of 3...
WO/2000/042059A1	NEW AMIDINOBENZYLAMINE DERIVATIVES AND THEIR USE AS THROMBIN INHIBITORS There is provided compounds of formula (I) wherein R?1¿, R?2¿ Y, R?3¿ and R?4¿ have meanings given in the description which are useful as, or as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and in ...
WO/2000/039073A1	STEREOSPECIFIC RING OPENING OF CHIRAL AZETIDINIUM SALTS The invention is directed to a process for stereoselective chemical synthesis which comprises reacting a nucleophilic agent and a chiral quaternary azetidinum salt (QAS) substrate of formula (I), to produce a compound of formula (II).
WO/2000/039124A1	THROMBIN INHIBITORS The present invention relates to thrombin inhibitors of formula (I), wherein A, B, C, D, E, F and n have the meaning given in the description, that are useful as anticoagulants. In particular, this invention relates to peptide derivative...
WO/2000/035869A1	NEW AMIDINO DERIVATIVES AND THEIR USE AS THROMBIN INHIBITORS There is provided compounds of formula (I), wherein R?1¿, R¿x?, Y, R?y¿, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the t...
WO/2000/035442A1	HYDROXY DIPHENYL UREA SULFONAMIDES AS IL-8 RECEPTOR ANTAGONISTS The invention relates to novel hydroxy diphenylurea sulfonamides, compositions and intermediates thereof. The hydroxy diphenylurea sulfonamides are useful in the treatment of disease states mediated by the chemokine, Interleukin-8.
WO/2000/035859A1	SUBSTITUTED ARYL AND HETEROARYL DERIVATIVES, THEIR PRODUCTION AND THEIR USE AS MEDICINES The invention relates to new substituted aryl and heteroaryl derivatives of the general formula (I) Ar - A - HCR¿1? - X - Y, in which A, Ar, X, Y and R¿1? have the meanings given in claim 1, and to their tautomers, stereoisomers, mixtu...
WO/2000/034240A1	PROCESS FOR THE SYNTHESIS OF AZETIDINONES This invention provides a process for preparing the hypocholesterolemic compound (I) comprising: (a) reacting p-fluorobenzoylbutyric acid with pivaloyl chloride and acylating the product with a chiral auxiliary to obtain a ketone of form...
WO/2000/020623A1	RESOLUTION OF TRANS-2 -(ALKOXYCARBONYLETHYL) -LACTAMS USEFUL IN THE SYNTHESIS OF 1- (4-FLUOROPHENYL) -3(R) -[3(S) -HYDROXY-3 -(4-FLUOROPHENYL) -PROPYL)] -4(S) -(4-HYDROXYPHENYL) -2-AZETIDINONE A process for the microbiological or enzymatic hydrolytic resolution of racemic $i(trans)-2-(alkoxycarbonylethyl)-lactams of formula (I) wherein R is C¿1?-C¿7? alkyl, 2,2,2-trifluoroethyl or methoxyethoxyethyl and RL is hydrogen or a p...
WO/2000/015609A1	AZETIDINE DERIVATIVES, PREPARATION AND MEDICINES CONTAINING THEM The invention concerns compounds of formula (1) wherein: R represents an chain (A) or (B); R¿1? is methyl or ethyl; R¿2? is either an optionally substituted aromatic or an optionally substituted heteroaromatic; R¿3? and R¿4?, identic...
WO/2000/014063A1	THERAPEUTIC COMPOUNDS AND METHODS The invention provides agents and compounds (see (I) and (II)) for use in the treatment or prophylaxis of disease conditions caused or exacerbated by mammalian papillomaviruses, such as human papillomaviruses, as well as methods for the ...
WO/2000/012474A1	AN EFFICIENT PROCESS FOR THE PREPARATION OF A HUMAN LEUKOCYTE ELASTASE INHIBITOR Processes for the preparation of [S- (R,S)]-N- [(1,3- benzodioxol- 5-yl)butyl]- 3,3- diethyl- 2[4- [(4- methyl-1- piperazinyl)carbonyl]phenoxy] -4-oxo- 1-azetidine carboxamide, a useful inhibitor of human leukocyte elastase (HLE), are de...
WO/2000/012473A1	PROCESS FOR THE PRODUCTION OF N-PROTECTED AZETIDINE-2-CARBOXYLIC ACIDS (AzeOHs) There is provided a process for the production of a N-protected azetidine-2-carboxylic acid, which process comprises the steps of: (a) addition of base to an aqueous solvent comprising an organic acid addition salt of an azetidine-2-carb...
WO/2000/009463A1	STEREOSELECTIVE RING OPENING REACTIONS The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile, selected from the group consisting of water, alcohols, carboxylic acids, and thiols, an...
WO/2000/005204A1	MONOCYCLIC $g(b)-LACTAM COMPOUNDS AND CHYMASE INHIBITORS CONTAINING THE SAME Chymase inhibitors and cytokine production inhibitors containing compounds represented by general formula (I), prodrugs of the same, pharmaceutically acceptable salts thereof or hydrates of them, wherein A is -CO-, -CONH- or the like; R?...
WO/2000/004892A2	COADMINISTRATION OF ACAT AND MMP INHIBITORS FOR THE TREATMENT OF ATHEROSCLEROTIC LESIONS This invention is the coadministration of ACAT and MMP inhibitors for the reduction of both the macrophage and smooth muscle cell component of atherosclerotic lesions, thus impairing the expansion of existing lesions and the development ...
WO/2000/003982A1	CYCLISATION PROCESS There is provided a process for the cyclisation of 4-amino-2-halobutyric acid to azetidine-2-carboxylic acid wherein more than 20 g of 4 amino-2-halobutyric acid is cyclised per litre of reaction mixture.
WO/2000/000465A1	HYDRAZINE DERIVATIVES The invention provides hydrazine derivatives of formula (I) wherein R?1¿ is lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R?2¿ is an acyl group derived from an $g(a)-, $g(b)-, $g(...
WO/1999/067230A1	INHIBITORS OF $g(a)¿4?$g(b)¿1? MEDIATED CELL ADHESION The present invention relates to compound of formula (I), that are potent inhibitors of $g(a)¿4?$g(b)¿1? mediated adhesion to either VCAM or CS-1 and which could be useful for the treatment of inflammatory diseases. Specifically, the m...
WO/1999/067215A1	AMIDINO AND GUANIDINO AZETIDINONE TRYPTASE INHIBITORS Compounds of formulae (I), (II), (III).
WO/1999/064395A1	HETEROCYCLIC AMIDE COMPOUNDS AS CELL ADHESION INHIBITORS Compounds of Formula (I) are antagonists of VLA-4 and/or $g(a)¿4?$g(b)¿7?, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceu...
WO/1999/061020A1	BENZIMIDAZOLE ANALOGS AS DOWN-REGULATORS OF IgE This invention relates to a family of diacyl benzimidazole analogs, which are inhibitors of the IgE response to allergens. These compounds are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic.

Matches 851 - 900 out of 3,661	< 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 >