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WO/2010/014586 |
The invention provides two process for synthesizing substituted aminothiazolone compounds as inhibitors of 11-β-hydroxy steroid dehydrogenase type 1. The processes allow the stereoselective synthesis of the desired compounds without the...
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WO/2010/010435 |
The present invention provides fused oxazole and thiazole derivatives as TRPM8 (Transient Receptor Potential subfamily M, member 8) modulators. In particular, compounds described herein are useful for treating diseases, disorders, condit...
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WO/2010/011926 |
The invention relates to a novel betaine cocrystal of 5-[(lZ,2E)-2-methyl-3- phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel betaine cocrystal according to various embodime...
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WO/2010/011922 |
The invention relates to novel crystalline salts of 5-[(1Z,2E)-2-methyl-3- phenyIpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the crystalline salts according to various embodiments of t...
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WO/2010/011922 |
The invention relates to novel crystalline salts of 5-[(lZ,2E)-2-methyl-3- phenyIpropenylidene]-4-oxo-2-thioxo-3-thiazolidineaeetic acid. The preparation and characterization of the crystalline salts according to various embodiments of t...
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WO/2010/010435 |
The present invention provides fused oxazole and thiazole derivatives as TRPM8 (Transient Receptor Potential subfamily M, member 8) modulators. In particular, compounds described herein are useful for treating diseases, disorders, condit...
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WO/2010/010288 |
Compound corresponding to general formula (I): in which R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or NR8R9 group; n is an integer equal to 1, 2 or 3 and m is an integer equal to 1 or...
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WO/2010/010797 |
Disclosed is a pharmaceutical composition for treating or preventing a disease accompanied by the increase in an activity of at least one member selected from DYRK1A, DYRK1B and DYRK2. Specifically disclosed is a pharmaceutical composit...
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WO/2010/011926 |
The invention relates to a novel betaine cocrystal of 5-[(lZ,2E)-2-methyl-3- phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel betaine cocrystal according to various embodime...
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WO/2010/010288 |
Compound of general formula (I), in which R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or NR8R9 group, n is an integer equal to 1, 2 or 3, and m is an integer equal to 1 or 2, A is a co...
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WO/2010/007316 |
The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, -COORc-CO-Rc or -CO-NRcRd; where Rc represents alkyl, cycloalkyl, heter...
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WO/2010/009120 |
Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. M...
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WO/2010/009120 |
Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. M...
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WO/2010/007389 |
The present invention pertains to certain thiazole carboxylic acid amide compounds which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function and/or Checkpoint Kinase 2 (CHK2) kinase function, to pharmaceutical compositions co...
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WO/2010/008522 |
Iodylbenzene derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are used as precursors in aromatic nucleophilic substitution reactions. The iodyl group (IO2) is regiospecifically su...
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WO/2010/007482 |
The present invention provides thiazole derivatives as Stearoyl CoA Desaturase (SCD) inhibitors. In particular, the compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by Stear...
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WO/2010/007482 |
The present invention provides thiazole derivatives as Stearoyl CoA Desaturase (SCD) inhibitors. In particular, the compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by Stear...
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WO/2010/008729 |
The present invention relates to methods of making compounds that inhibit 11-β-hydroxysteroid dehydrogenase type 1 enzyme (11-β HSD1). One method comprises (a) contacting a compound of formula (II) with a chiral base, deprotonating age...
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WO/2010/008729 |
The present invention relates to methods of making compounds that inhibit 11-β-hydroxysteroid dehydrogenase type 1 enzyme (11-β HSD1). One method comprises (a) contacting a compound of formula (II) with a chiral base, deprotonating age...
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WO/2010/007046 |
The invention relates to compounds of formula (I): where A is an optionally substituted heteroaryl, useful for treating disorders mediated by acyl coA- diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention al...
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WO/2010/007317 |
The invention relates to the novel products of formula (I): in which: Ra is H, Hal, aryl or heteroaryl, which are optionally substituted; Rb is H, Rc, -COORc-CO-Rc or -CO-NRcRd; where Rc is alkyl, cycloalkyl, heterocycloalkyl, aryl and h...
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WO/2010/007046 |
The invention relates to compounds of formula (I): where A is an optionally substituted heteroaryl, useful for treating disorders mediated by acyl coA- diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention al...
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WO/2010/007027 |
The present invention provides a compound of formula (I) said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP- 13....
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WO/2010/009120 |
Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. M...
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WO/2010/007318 |
The invention relates to the novel products of formula (I): in which: n = 0,1 or 2; X is H, Hal or alk; R is H, NH2, NHalk or N(alk)2; Ra is H, Hal, -O-cycloalkyl, -O-alkyl, -O-aryl, -O-heteroaryl, ‑NRd(cycloalkyl), ‑NRd(alkyl), -NRd...
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WO/2010/007060 |
The present invention relates to azolin-2-ylamino compounds of formula (I), wherein A is a radical of the formulae (A.1) or (A.2), wherein * denotes the binding site and wherein the indices and variables are as defined in the description...
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WO/2010/008522 |
Iodylbenzene derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are used as precursors in aromatic nucleophilic substitution reactions. The iodyl group (IO2) is regiospecifically su...
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WO/2010/007318 |
The invention relates to the novel products of formula (I): in which: n = 0,1 or 2; X is H, Hal or alk; R is H, NH2, NHalk or N(alk)2; Ra is H, Hal, -O-cycloalkyl, -O-alkyl, -O-aryl, -O-heteroaryl, ‑NRd(cycloalkyl), ‑NRd(alkyl), -NRd...
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WO/2010/001922 |
Disclosed is a novel imino derivative which can be used as a pesticidal compound having excellent properties including long-acting efficacy and a broad spectrum. Specifically disclosed is an imino derivative represented by chemical formu...
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WO/2010/002209 |
This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The...
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WO/2010/001169 |
The invention relates to chemical compounds of formula (I), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In stil...
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WO/2010/001821 |
Disclosed are a compound represented by general formula (I) (wherein R1 and R2 each represents a hydrogen, a lower acyl, a lower alkoxycarbonyl or the like; R3 represents a lower alkyl, a halogenated lower alkyl, a cycloalkyl, a heterocy...
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WO/2010/002209 |
This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The...
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WO/2009/157528 |
An amide compound of the formula (I): (wherein, R1 represents a hydrogen atom or fluorine atom and R2 represents a C3 to C8 linear alkenyl group or C3 to C8 linear alkynyl group.) has an excellent controlling effect on a plant disease.
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WO/2009/157196 |
Disclosed is a compound having GPR52 agonist activity and serving as an agent for preventing or treating schizophrenia or the like. Specifically disclosed is a compound represented by formula (I) or a salt thereof. In the formula, A repr...
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WO/2009/156336 |
The invention relates to sulfoximinamid compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the sulfoximinamid compounds, o...
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WO/2009/157418 |
Disclosed is a highly safe agent for treating and/or preventing diabetes or the like, which has excellent activity. Specifically disclosed is a compound represented by general formula (I) or a pharmacologically acceptable salt thereof. (...
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WO/2009/158374 |
Invented are novel hetero-pyrrole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
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WO/2009/157527 |
An amide compound of the formula (I): (wherein, R1 represents a hydrogen atom or fluorine atom and R2 represents a C1 to C6 linear alkyl group or linear (C1-C2 alkoxy)C2-C5 alkyl group.) has an excellent controlling effect on a plant dis...
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WO/2009/157399 |
Disclosed is a compound useful as an EP1 receptor antagonist. Studies are made on EP1 receptor antagonists, and it is confirmed that a compound having a sulfonamide structure in which a nitrogen atom in the sulfonamide structure is subst...
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WO/2009/155001 |
The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases...
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WO/2009/154014 |
Disclosed is an external composition usable as an external skin preparation or a cosmetic which has an excellent effect of removing active oxygen, a tyrosinase inhibitory effect and a reducing effect and exerts an antiaging function base...
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WO/2009/155001 |
The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases...
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WO/2009/152735 |
Histone deacetylase inhibitors and uses thereof. The histone deacetylase inhibitors are useful in the treatment of malignant tumor and the diseases associated with differentiation and proliferation. The histone deacetylase inhibitors are...
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WO/2009/153238 |
The present invention relates to aminothiazoline compounds of the general formula (I): wherein A is a radical of the formulae A1 or A2: wherein * denotes the binding site and wherein the indices and variables are as defined in the descri...
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WO/2009/153180 |
The present invention is concerned with novel sulfonamides of formula I wherein R1, R2, R3, R4, R5, Ar, Ar1, Ar2, n, o and p are as described in the description and claims. The compounds are orexin receptor antagonists may be useful in t...
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WO/2009/153226 |
The invention relates to the use of a compound of formula (I) or a pharmaceutically acceptable salt, prodrug and/or solvate thereof, in the preparation of a medicament for the treatment of an acute or chronic inflammatory disease, by inh...
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WO/2009/152082 |
The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, c...
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WO/2009/146539 |
Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing 4-(aminome...
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WO/2009/148269 |
The present invention relates to a benzofluoranthene derivative and to an organic electroluminescent element employing the same. More specifically, the present invention relates to a benzofluoranthene derivative comprising one or more su...
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