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| Number | Title | Issue Date |
| 8067601 | 1-[2-(4-benzyl-4-hydroxy-piperidin-1 -yl )-ethyl]-3-(2-methyl-quinolin- 4-yl)- urea as crystalline sulfate salt The invention relates to 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea as a crystalline, stoichiometrically defined and non-hygroscopic sulfate salt and a process for its preparation. Further, the present invention relates to the us... | 11/29/2011 |
| 7964731 | Isotopically marked quinoline derivatives as adenosin A3 receptor ligands The invention relates to adenozin A3 receptor ligands labeled with iodine isotops of mass number 125, within those favorably to antagonists and their isomers, to the experimental materials containing them, to a process for the preparation of the compounds... | 06/21/2011 |
| 7868174 | Form of a benzenesulfonamide derivative The present disclosure relates to an improved process for the preparation of enantiomerically enriched alcohols of Formula (I), from the corresponding ketone of Formula (II), | 01/11/2011 |
| 7368573 | Triamide-substituted heterobicyclic compounds This invention relates to MTP/Apo-B secretion inhibitors of Formula (I) wherein R1-R7, X1, m and n are as defined in the specification, as well as pharmaceutical compositions comprising the ... | 05/06/2008 |
| 7365081 | Indole derivatives and their use as medicaments The invention relates to novel indole derivatives of the general formula 1, to their preparation and to their use as medicaments, in particular for treating tumors ... | 04/29/2008 |
| RE40278 | Heterocyclic amines having central nervous system activity Tricyclic nitrogen containing compounds, having anxiolytic and anti-depressant activity and central nervous system activity of the following structural formula: and pharmaceutically acceptable salts thereof wherein R1 ... | 04/29/2008 |
| 7332504 | Heterocyclic substituted aminoazacycles useful as central nervous system agents Heterocyclic substituted aminoazacyclic compounds of formula I Z-R3I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions ... | 02/19/2008 |
| 7314939 | Compositions and methods for inhibiting TGF-β The present invention provides compounds of the formula: and pharmaceutically acceptable isomers, salts, hydrates, solvates, and prodrug derivatives thereof, wherein R1, R6, R7, R... | 01/01/2008 |
| 7312230 | Carboxylic acid derivatives as IP antagonists This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein: R1, R2, and R3 ... | 12/25/2007 |
| 7309715 | Compound A compound having Formula I wherein one of R1 and R2 is a group of the formula wherein R4 is selected from H and hydrocarbyl... | 12/18/2007 |
| 7304083 | 2-iminoimidazole derivatives (2) A 2-iminoimidazole derivative represented by the formula: {wherein R1, R2 and R3 represent hydrogen, optionally substituted C1-6 alkyl, etc.; R6 represents h... | 12/04/2007 |
| 7183414 | Processes for the preparation of benzoimidazole derivatives The present invention relates to a process for preparing a compound of the formula I or a pharmaceutically acceptable salt, prodrug, hydrate or solvate thereof, wherein R1, R2, R3 | 02/27/2007 |
| 7183413 | Aminoquinoline compounds This invention relates to treating inflammatory and immune diseases with certain aminoquinoline compounds that bind to CXCR3 receptors. The aminoquinoline compounds are covered by the formula (I) shown below. Each variable is defined in the specification. | 02/27/2007 |
| 7151110 | Pyrazole compounds as transforming growth factor (TGF) inhibitors Novel pyrazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming gro... | 12/19/2006 |
| 7148227 | Fungicidal triazolopyrimidines, methods for producing the same, use thereof for combating harmful fungi and agents containing said substances The invention relates to triazolopyrimidines of formula (I), in which the substituents are defined as follows: L1 represents cyano, S(═O)nA1 or C(═O)A2, wherein A1 stands for hydrogen, hydroxy, alkyl, alkyla... | 12/12/2006 |
| 7084156 | 2-Aminoquinoline compounds The present invention is concerned with compounds of the general Formula I: and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-... | 08/01/2006 |
| 7060834 | N-type calcium channel antagonists for the treatment of pain Compounds useful for the treatment of pain in accord with the following structural diagram, wherein A, R1, b, R4, R5, R6, R7 and R8 are any of a n... | 06/13/2006 |
| 6995175 | Chemical derivatives and their application as antitelomerase agent The present invention relates to cancer therapy and to novel anticancer agents having a mechanism of action which is quite specific. It also relates to novel chemical compounds as well as their therapeutic application in humans. ... | 02/07/2006 |
| 6989392 | 2-Aminoquinolines as melanin concentrating hormone receptor antagonists The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, which antagonize the effects of melanin-concentrating hormone (MCH) through the melanin concentrating ... | 01/24/2006 |
| 6962930 | Compounds, compositions and method suitable for amelioration of withdrawal syndromes and withdrawal-induced brain damage Compounds, composition and method for ameliorating alcohol or drug dependency withdrawal syndromes and withdrawal-induced brain damage are disclosed. In particular, a series of N-substituted-4-uredo-5,7-dihalo-2-carboxy quinoline compounds are disclosed having combi... | 11/08/2005 |
| 6946473 | Preparation and use of acetylenic ortho-sulfonamido and phosphinic acid amido bicyclic heteroaryl hydroxamic acids as TACE inhibitors Compounds of the formula which are useful in disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative c... | 09/20/2005 |
| 6930185 | Melanin-concentrating hormone antagonist A melanin-concentrating hormone antagonist comprising a compound of the formula (I): wherein Ar1 is a cyclic group which may be substituted; X and Y are the same or different and are a spacer having a main c... | 08/16/2005 |
| 6903104 | Indol-3-YL-2-oxoacetamide compounds and methods of use thereof The invention is based on the discovery that certain 3-oxoacetamideindolyl compounds have potent anticancer and anti-angiogenic activity. The 3-oxoacetamideindolyl compounds are of the following formula. In this formul... | 06/07/2005 |
| 6903094 | Amide derivatives and nociceptin antagonists The present invention relates to a compound of the formula [1′] wherein R2 is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the lik... | 06/07/2005 |
| 6894167 | Method of preparation of (s)-n-tert-butyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide A new method is described here for the synthesis of (S)-N-tert-butyl-1,2,3,4-tetrahydroiso-quinoline-3-carboxamide comprising the following steps: a) (3S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid is reacted with formic acid... | 05/17/2005 |
| 6881753 | Potassium channel inhibitors and method Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure: where A, B, D, Q, X1, R, R1, X2 and R2 are as defined... | 04/19/2005 |
| 6875769 | Substituted6,6-hetero-bicyclicderivatives This invention relates to compounds of the formula wherein A, B, D, E, K, G, R3 and R5 are defined as in the specification, and to the pharmaceutically acceptable salts of such compounds. ... | 04/05/2005 |
| 6875768 | Phthalamide derivatives, intermediates in the production thereof, and agricultural/horticultural insecticides and method for using the same Heterocyclic amine derivatives represented by general formula (I): wherein R1, R2 and R3 represent each H, optionally halogenated C3-6 cycloalkyl, etc.; Q represents an optio... | 04/05/2005 |
| 6861436 | 1-glyoxylamide indolizines for treating cancer Disclosed is a compound represented by Structural Formula (I): Ring A is substituted or unsubstituted and optionally fused to an aryl group. Z1 and Z2 are... | 03/01/2005 |
| 6841673 | N-heterocyclic derivatives as nos inhibitors N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using the... | 01/11/2005 |
| 6833370 | Heterocycle substituted aminoazacycles useful as central nervous system agents Heterocyclic substituted aminoazacyclic compounds of formula I Z—R3 I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said comp... | 12/21/2004 |
| 6825352 | Preparation and use of ortho-sulfonamido arylhydroxamic acids as matrix metalloproteinase inhibitors Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs. ... | 11/30/2004 |
| 6818772 | Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in repro... | 11/16/2004 |
| 6800650 | Pyridine and quinoline derivatives The present invention provides compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compou... | 10/05/2004 |
| 6784189 | Potassium channel inhibitors and method Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure where A, B, D, Q, X1, R, R1, X2 and R2 are as defined he... | 08/31/2004 |
| 6720427 | Thiazole derivatives The invention provides compounds of formula 1 wherein R1, R3, and R4 are as defined, and their pharmaceutically acceptable salts. Compounds of formula 1 are indicated to have activity inh... | 04/13/2004 |
| 6706699 | Quinolines and uses thereof This invention relates to compounds of the general formula: in which RA, RB, RC and RD are as defined herein, and to their preparation and use. ... | 03/16/2004 |
| 6699879 | Phenyl urea and phenyl thiourea derivatives as orexin receptor antagonists The present invention provides phenyl urea and phenyl thiourea derivatives which are non-peptide antagonists of human orexin receptors, in particular orexin-1 receptors, of formula (I) ##STR1## in which: Z represents oxygen or sulfur; and R1 | 03/02/2004 |
| 6696467 | Quinoline derivatives Compounds of general formula I ##STR1## as well as pharmaceutically acceptable salts and esters thereof, are potent inhibitors of neuropeptide Y and can be used in the form of pharmaceutical preparations for the treatment or prevention of various disease ... | 02/24/2004 |
| 6653321 | Naphthylsulfonic acids and related compounds as glucose uptake agonists Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptabl... | 11/25/2003 |