1,2-diazole (including Hydrogenated) Patents (Class 546/211)
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Publication number: 20080139620Abstract: The invention provides a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein: R1 is 2,6-dichlorophenyl; R2a and R2 are both hydrogen; and R3 is a group: where R4 is C1-4 alkyl. The compounds have activity as inhibitors of CDK kinases and inhibit the proliferation of cancer cells.Type: ApplicationFiled: January 20, 2006Publication date: June 12, 2008Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Paul Graham Wyatt, Valerio Berdini, Adrian Liam Gill, Gary Trewartha, Andrew James Woodhead
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Patent number: 7381721Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.Type: GrantFiled: March 17, 2003Date of Patent: June 3, 2008Assignee: Adolor CorporationInventors: Roland Ellwood Dolle, Bertrand Le Bourdonnec
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Publication number: 20080125416Abstract: The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.Type: ApplicationFiled: August 29, 2005Publication date: May 29, 2008Inventors: Christian Laggner, Maria Rosa Cuberes-Altisent, Joerg Holenz, Juana Maria Berrocal-Romero, Maria Montserrat Contijoch-Llobet
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Publication number: 20080119653Abstract: A process for the preparation of for the preparation of N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazole-3-carboxamide and of its salts, wherein 1,5-dibromopentane is reacted with a compound of formula (IIIa) in the presence of Na2CO3 in acetonitrile heated at reflux.Type: ApplicationFiled: November 14, 2006Publication date: May 22, 2008Applicant: SANOFI-AVENTISInventors: Philippe VAYRON, Marc DAUMAS, Raphael SOLE, Alain DLUBALA
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Publication number: 20080085904Abstract: Novel 1,5 diphenylpyrazole derivatives of the formula (I), in which R1-R6 have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: July 14, 2005Publication date: April 10, 2008Inventors: Hans-Michael Eggenweiler, Michael Wolf
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Publication number: 20080070949Abstract: Crystalline form C of rimonabant and amorphous rimonabant, processes for their preparation and pharmaceutical compositions thereof.Type: ApplicationFiled: April 17, 2007Publication date: March 20, 2008Applicant: Cipla LimitedInventors: Manjinder Singh, Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan
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Publication number: 20080064698Abstract: The invention relates to 1-(2,4,6-trisubstituted-phenyl)-5-amino-4-substituted-pyrazole derivatives of formula (I) or salts thereof wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests (including arthropods and helminths).Type: ApplicationFiled: February 25, 2005Publication date: March 13, 2008Applicant: Bayer CropScience S.A.Inventors: Stefan Schnatterer, David Teh-Wei Chou, Werner Knauf, Daniela Jans, Karl Seeger
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Patent number: 7332508Abstract: A novel class of substituted homopiperidine, piperidine and pyrrolidine derivatives, methods for their preparation, pharmaceutical compositions comprising them and use thereof in the treatment of disorders related to the histamine H3 receptor. More particularly, the compounds possess histamine H3 receptor antagonistic activity and are thus useful in the treatment of disorders in which a histamine H3 receptor blockade is beneficial.Type: GrantFiled: December 15, 2003Date of Patent: February 19, 2008Assignee: Novo Nordisk A/SInventors: Jan Lindy Sorensen, Knud Erik Andersen, Ingrid Pettersson
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Publication number: 20080033013Abstract: Two chemical genera of pyrazolylphenyl and pyrrolylphenyl derivatives are disclosed. They have the general formula: In these compounds ring (a) is a pyrazole or pyrrole; Q is selected from the group consisting of a direct bond, O, S, SO, SO2, NR1, CH2, CF2, and C(O); HET is a 4-7-membered saturated nitrogenous heterocycle; and taken together ZW is H or Z is (CH2)1-10 in which one or two (CH2) may optionally be replaced by —O—, —NR1—, —SO—, —S(O)2—, —C(?O)— or —C?O(NH)—; and W is hydrogen, acyl, hydroxyl, carboxyl, amino, carboxamido, aminoacyl, —COOalkyl, —CHO, heterocyclyl, substituted aryl or substituted heterocyclyl. The compounds are inhibitors of LTA4H (leukotriene A4 hydrolase). They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.Type: ApplicationFiled: August 3, 2007Publication date: February 7, 2008Applicant: deCODE genetics ehf.Inventors: Vincent Sandanayaka, Jasbir Singh, Lei Zhao, Peng Yu, Mark E. Gurney
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Patent number: 7326705Abstract: Heterocyclic are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 1 to 5; X is N or C—R5 wherein R5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; Z is a heteroaryl group, R1, R2, R3 and R4 are as defined herein, and where X is N, R1 is preferably aryl or heteroaryl, and are useful as antianginal and cardioprotective agents. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, and arrhythmia employing the above heterocyclic derivatives.Type: GrantFiled: January 31, 2005Date of Patent: February 5, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Saleem Ahmad, Shung C. Wu, Steven V. O'Neil, Khehyong Ngu, Karnail S. Atwal, David S. Weinstein
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Publication number: 20080004313Abstract: This invention relates to three novel solvate forms of crystalline rimonabant hydrochloride (Form A, B, and C) and two novel crystalline polymorphic forms of rimonabant hydrochloride anhydrous (Form D and E), to processes for preparing such polymorphic forms or solvate forms, to pharmaceutical compositions containing them and to the use of them in medicine.Type: ApplicationFiled: June 18, 2007Publication date: January 3, 2008Inventors: Hui Min He Huang, Cai Gu Huang
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Patent number: 7312218Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: December 15, 2006Date of Patent: December 25, 2007Assignee: Bristol Myers Squibb Co.Inventors: Wei Han, Zilun Hu, Timur Gungor
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Publication number: 20070281973Abstract: The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of these pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.Type: ApplicationFiled: May 29, 2007Publication date: December 6, 2007Inventors: Josephus H.M. Lange, Cornelis G. Kruse, Bernard J. Van Vliet
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Patent number: 7291632Abstract: The present invention relates to compounds of formula I: (I) or a pharmaceutically acceptable acid addition salt thereof, where; X is C(R3c? or N?; R1 is C2–C6 alkyl, substituted C2–C6 alkyl, C3–C7 cycloalkyl, substituted C3–C7 cycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1–C3 n-alkyl, C3–C6 cycloalkyl-C1–C3 alkyl, or a group of formula II (II) provided that when R1 is C2–C6 alkyl or substituted C2–C6 alkyl, R2 is hydrogen or methyl; R3a, R3b, and, when X is C(R3c)?, R3c, are each independently hydrogen, fluoro, or methyl, provided that no more than one of R3a, R3b, and R3c may be other than hydrogen; R4 is hydrogen or C1–C3 alkyl; R5 is hydrogen, C1–C3 alkyl, or C3–C6 cycloalkylcarbonyl, provided that when R3a is other than hydrogen, R5 is hydrogen; R6 is hydrogen or C1–C6 alkyl; and n is an integer from 1 to 6 inclusively.Type: GrantFiled: September 3, 2004Date of Patent: November 6, 2007Assignee: Eli Lilly and CompanyInventors: Maria-Jesus Blanco-Pillado, Michael Philip Cohen, Sandra Ann Filla, Kevin John Hudziak, Daniel Timothy Kohlman, Dana Rae Benesh, Frantz Victor, Yao-Chang Xu, Bai-Ping Ying, DeAnna Piatt Zacherl, Deyi Zhang, Brian Michael Mathes
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Patent number: 7285554Abstract: Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: D: pyrazolyl which may have 1 to 3 substituents selected from the group consisting of -Alk, -lower alkenyl, -lower alkynyl, -halogeno-lower alkyl, -Alk-cycloalkyl, -Alk-O-Alk, -cycloalkyl, —O-Alk, —COOH, —COO-Alk and -Hal, n: 0 or 1, B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4?CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substiType: GrantFiled: April 7, 2006Date of Patent: October 23, 2007Assignee: Astellas Pharma Inc.Inventors: Hirokazu Kubota, Yasuhiro Yonetoku, Keizo Sugasawa, Masashi Funatsu, Souichirou Kawazoe, Akira Toyoshima, Yoshinori Okamoto, Jun Ishikawa, Makoto Takeuchi
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Publication number: 20070225280Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.Type: ApplicationFiled: March 14, 2007Publication date: September 27, 2007Inventors: Kevin William Anderson, Nader Fotouhi, Paul Gillespie, Robert Alan Goodnow, Kevin Richard Guertin, Nancy-Ellen Haynes, Michael Paul Myers, Sherrie Lynn Pietranico-Cole, Lida Qi, Pamela Loreen Rossman, Nathan Robert Scott, Kshitij Chhabilbhai Thakkar, Jefferson Wright Tilley, Qiang Zhang
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Publication number: 20070213302Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.Type: ApplicationFiled: March 9, 2007Publication date: September 13, 2007Applicant: JENRIN DISCOVERYInventors: John Francis McElroy, Robert J. Chorvat
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Patent number: 7259157Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.Type: GrantFiled: April 2, 2002Date of Patent: August 21, 2007Assignee: Merck & Co., Inc.Inventors: Nigel J. Liverton, John W. Butcher, Charles McIntyre, Christopher F. Claiborne, David A. Claremon, John A. McCauley, Joseph J. Romano, Wayne Thompson, Peter M. Munson
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Patent number: 7253170Abstract: The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.Type: GrantFiled: June 28, 2006Date of Patent: August 7, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Alaric J. Dyckman, Jagabandhu Das, Katerina Leftheris, Chunjian Liu, Robert V. Moquin, Stephen T. Wrobleski
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Patent number: 7253186Abstract: Disclosed herein are compounds of Formula I, or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof. Also disclosed are methods of inhibiting an activity of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Disclosed are also methods of inhibiting an activation of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Furthermore, methods of treating psychotic disease using a compound of Formula I are disclosed.Type: GrantFiled: June 20, 2003Date of Patent: August 7, 2007Inventors: Carl-Magnus Andersson, Nathalie Schlienger, Alma Fejzic, Eva Louise Hansen, Jan Pawlas
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Patent number: 7247635Abstract: Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4?CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more sType: GrantFiled: June 17, 2005Date of Patent: July 24, 2007Assignee: Astellas Pharma Inc.Inventors: Hirokazu Kubota, Yasuhiro Yonetoku, Keizo Sugasawa, Masashi Funatsu, Souichirou Kawazoe, Akira Toyoshima, Yoshinori Okamoto, Jun Ishikawa, Makoto Takeuchi
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Patent number: 7217714Abstract: Compounds of Formula 1 [Region ?]?[Region ?]?[Region ?]?[Region ?] ??(I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.Type: GrantFiled: November 30, 1999Date of Patent: May 15, 2007Assignee: Agouron Pharmaceuticals, Inc.Inventors: Duncan Robert Armour, David Anthony Price, Blanda Luzia Christa Stammen, Anthony Wood, Manoussos Perros, Martin Paul Edwards
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Patent number: 7189679Abstract: 3-Amino-2-thiomethylbenzoylpyrazoles of the formula (I) and their use as herbicides are described. In this formula (I) R1 to R9 are various radicals.Type: GrantFiled: April 1, 2005Date of Patent: March 13, 2007Assignee: Bayer CropScience GmbHInventors: Monika Schmitt, Andreas van Almsick, Lothar Willms, Thomas Auler, Heinz Kehne, Martin Hills, Dieter Feucht
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Patent number: 7157472Abstract: The present invention discloses compounds which, are receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: June 30, 2003Date of Patent: January 2, 2007Assignee: Schering CorporationInventors: Andrew W. Stamford, Yusheng Wu
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Patent number: 7153868Abstract: The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: wherein, generally, Q is R1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 16, 2003Date of Patent: December 26, 2006Assignee: Merck Sharp & Dohme Ltd.Inventors: Mark Stuart Chambers, Philip Jones, Helen Jane Szekeres
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Patent number: 7141585Abstract: This invention relates to the use of pyrazole derivatives of the formula and pharmaceutically acceptable salts and solvates thereof, in the manufacture of a reverse transcriptase inhibitor or modulator, to certain novel such pyrazole derivatives and to processes for the preparation of and compositions containing such novel derivatives.Type: GrantFiled: April 26, 2004Date of Patent: November 28, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Romuald Gaston Corbau, Charles Eric Mowbray, Manoussos Perros, Paul Anthony Stupple, Anthony Wood
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Patent number: 7119108Abstract: Novel cannabimimetic pyrazole derivatives are presented which have preferentially high affinities for both of the cannabinoid CB1 or CB2 receptor sites. The improved receptor affinity makes these analogs useful as experimental tools for cannabinoid receptor studies as well as clinically useful agents in individuals and animals for treatment of memory deficits associated with aging or neurological diseases, as anti-obesity agents, as medications for schizophrenia and treatment of septic shock syndrome.Type: GrantFiled: October 18, 2000Date of Patent: October 10, 2006Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Qian Liu
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Patent number: 7115635Abstract: The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration. The present inventors have found that the following benzylpiperidine derivative (the formula (1)) has a chemokine inhibitory activity. Further intensive studies have resulted in successful enhancement of the chemokine inhibitory activity and stability in blood of the present compound, as well as the completion of the present invention. wherein each symbol is as defined in the specification.Type: GrantFiled: April 26, 2002Date of Patent: October 3, 2006Assignee: Mitsubishi Pharma CorporationInventors: Masatoshi Kiuchi, Takanobu Kuroita, Hideo Tomozane, Shuuzou Takeda, Yoshihito Tanaka, Hidemitsu Higashi, Shigeki Kuwahara
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Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Patent number: 7091350Abstract: The invention relates to diaminopyrazole derivatives having the following structure (I), wherein R1 represents an alkyl or alkenyl radical bearing at least one substituent selected from among OR, NRR?, SR, SOR, SO2R, COOR, CONRR?, PO(OH)2, SO3X, NHCONRR, a non-cationic heterocycle, an aryl, a halogen. R2 and R3 are different from H and represent, independently of each other, an alkyl or alkenyl group; R2 and R3, together with the nitrogen atom to which they are attached, can form a heterocycle possibly comprising at least one other heteroatom selected from among N, O and S; R2 and R3 or the heterocycle that they form with the nitrogen to which they are attached can be substituted by at least one substituent defined above.Type: GrantFiled: February 14, 2002Date of Patent: August 15, 2006Assignee: L'OrealInventors: Thilo Fessmann, Eric Terranova
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Patent number: 7067656Abstract: A sulfamoyl compound of the general formulae (1): wherein R1 and R2 are each independently C1-4 alkyl, or R1 and R2 together are C4-6 alkylene or C4-6 alkyleneoxy, Y is H, halogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylthio, C1-8 haloalkyl, C1-8 haloalkoxy or C1-8 haloalkylthio, A is a predetermined heterocyclic group, B is a predetermined heterocyclic group which is identical with or different from A, W is a chemical bond or O, V is O or S, D, E, F and G are each independently N, CR7, CR8, CR9 or CR10, and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are each independently predetermined group such as H, or an unsubstituted or substituted aliphatic, aromatic or heterocyclic group. The sulfamoyl compound is useful as an agricultural and horticultural fungicide.Type: GrantFiled: July 9, 2003Date of Patent: June 27, 2006Assignee: Nissan Chemical Industries, Ltd.Inventors: Toshiaki Takeyama, Toshimasa Hamada, Hiroaki Takahashi, Junichi Watanabe, Kazuhiro Yamagishi, Masanori Nishioka, Hiroyuki Suzuki
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Patent number: 7034049Abstract: Compounds which are 3-amino-pyrazole derivatives represented by formula (I) wherein R is C3–C6 cycloalkyl group optionally substituted by a straight or branched C1–C6 alkyl or arylalkyl group; R1 is a straight or branched C1–C6 alkyl, C2–C4 alkenyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, arylalkyl, arylcarbonyl, aryloxyalkyl or arylalkenyl group, each of which may be optionally further substituted as indicated in the description; or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.Type: GrantFiled: May 5, 2000Date of Patent: April 25, 2006Assignees: Pharmacia Italia S.p.A., Pharmacia & Upjohn Company LLCInventors: Paolo Pevarello, Paolo Orsini, Gabriella Traquandi, Mario Varasi, Edward L. Fritzen, Martha A. Warpehoski, Betsy S. Pierce, Maria Grabriella Brasca
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Patent number: 7009056Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof, are capable of blockading voltage-dependent sodium channels and are useful in particular, in treating glaucoma and multiple sclerosis.Type: GrantFiled: February 5, 2001Date of Patent: March 7, 2006Assignee: University College LondonInventors: Giti Garthwaite, David Selwood, Marcel Kling, Grant Wishart
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Patent number: 6974810Abstract: The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (Ia) or (Ib) wherein the symbols have the meanings given in the specification.Type: GrantFiled: September 17, 2002Date of Patent: December 13, 2005Assignee: Solvay Pharmaceuticals B.V.Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Jacobus Tipker, Herman H. van Stuivenberg, Arnoldus H. J. Herremans
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Patent number: 6958339Abstract: The present invention is directed to drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, wherein each substituent is defined in the specification. The present invention also relates to a pharmaceutical composition containing an effective amount of the compound of formula (I) and a pharmaceutically effective carrier. The present invention further relates to methods of treatment of diseases associated with calcium release-activated calcium channels, diseases associated with IL-2 production, and methods of treatment of allergic, inflammatory or auto-immune diseases.Type: GrantFiled: February 2, 2001Date of Patent: October 25, 2005Assignee: Astellas Pharma Inc.Inventors: Hirokazu Kubota, Yasuhiro Yonetoku, Keizo Sugasawa, Masashi Funatsu, Souichirou Kawazoe, Akira Toyoshima, Jun Ishikawa, Makoto Takeuchi
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Patent number: 6958350Abstract: The invention provides a compound of formula (I): wherein R1, R2, R3, R4, R5, N, X and Y are as defined in the specification, processes, for their preparation, pharmaceutical compositions containing them, and their use in therapy, especially for the treatment of chemokine receptor related diseases and conditions.Type: GrantFiled: February 18, 2002Date of Patent: October 25, 2005Assignee: AstraZeneca ABInventors: Stephen Brough, Thomas McInally, Matthew Perry, Brian Springthorpe
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Patent number: 6953793Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.Type: GrantFiled: August 10, 2001Date of Patent: October 11, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Christopher R. Butler, Hui Cai, James P. Edwards, Cheryl A. Grice, Darin J. Gustin, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Clark A. Sehon, Kevin L. Tays, Jianmei Wei
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Patent number: 6894173Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.Type: GrantFiled: February 10, 2003Date of Patent: May 17, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Lin-Hua Zhang, Lei Zhu
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Patent number: 6890928Abstract: This invention is directed to aromatic sulfone hydroxamic acids (including hydroxamates) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.Type: GrantFiled: September 5, 2003Date of Patent: May 10, 2005Assignee: Pharmacia CorporationInventors: John N. Freskos, Yvette M. Fobian, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffrey N. Carroll, Gary A. DeCrescenzo, Susan L. Hockerman, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Monica B. Norton, Joseph G. Rico, John J. Talley, Clara I. Villamil, Lijuan Jane Wang
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Patent number: 6864249Abstract: The present invention relates to a compound having formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I and pharmaceutical compositions containing them are of the class of thrombin inhibitors which are useful as anticoagulants.Type: GrantFiled: November 1, 2002Date of Patent: March 8, 2005Assignee: LG Life Sciences, Ltd.Inventors: Koo Lee, Won Hyuk Jung, Cheol Won Park, Sang Koo Lee, Sun Hwa Lee, Hee Dong Park
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Patent number: 6861530Abstract: This invention relates to substituted piperidine derivatives having at least one six-membered ring substituent. The piperidine derivatives exhibit antitumor activity and are useful as pharmaceuticals such as an antitumor agent.Type: GrantFiled: July 6, 2001Date of Patent: March 1, 2005Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Shinji Nara, Rieko Nakatsu, Yutaka Kanda, Shiro Akinaga, Mitsunobu Hara, Jun Eishima, Timothy A. Grese, Douglas L. Gernert
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Publication number: 20040224945Abstract: The present invention relates to novel substituted pyrazole derivatives of the general formula (I) 1Type: ApplicationFiled: May 28, 2004Publication date: November 11, 2004Applicant: Bayer HealthCare AGInventors: Alexander Straub, Achim Feurer, Cristina Alonso-Alija, Johannes-Peter Stasch, Elisabeth Perzborn, Joachim Hutter, Klaus Dembowsky, Elke Stahl
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Publication number: 20040220170Abstract: Compounds of the present invention modulate PN3 in mammals and are useful in treating pain in mammals.Type: ApplicationFiled: May 1, 2003Publication date: November 4, 2004Inventors: Robert N. Atkinson, Irene Drizin, Robert J. Gregg, Michael F. Gross, Michael E. Kort, Lei Shi
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Patent number: 6806279Abstract: Compounds of formulae I and I′, methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are antagonists of IL-2/IL-2R binding; and are useful for the treatment of interleukin-2 mediated diseases, such as autoimmune diseases (such as rheumatoid arthritis, multiple sclerosis, uveitis, and psoriasis), allograft rejection, and graft-versus-host disease.Type: GrantFiled: December 17, 2001Date of Patent: October 19, 2004Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Michelle R. Arkin, Robert S. McDowell, Johan D. Oslob, Brian C. Raimundo, Nathan D. Waal, Chul Hyun Yu
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Publication number: 20040204406Abstract: The present invention is directed to a compound of formula I, 1Type: ApplicationFiled: December 23, 2003Publication date: October 14, 2004Applicant: AVENTIS PHARMA DEUTSCHLAND GMBHInventors: Marc Nazare, Volkmar Wehner, David W. Will, Hans Matter
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Publication number: 20040192667Abstract: One aspect of the invention is concerned with cannabimimetic pyrazole analogs. Another aspect of the invention is concerned with new and improved pyrazole analogs having high affinities and/or selectivities for the CB1 cannabinoid receptor. A further aspect of the invention is concerned with pharmaceutical preparations employing the inventive analogs and methods of administering therapeutically effective amounts of the inventive analogs to provide a physiological effect.Type: ApplicationFiled: March 1, 2004Publication date: September 30, 2004Applicant: University of ConnecticutInventors: Alexandros Makriyannis, Qian Liu, Rajesh Thotapally
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Publication number: 20040180882Abstract: The present invention provides compounds having formula (I): 1Type: ApplicationFiled: December 18, 2003Publication date: September 16, 2004Inventors: David E. Zembower, David A. Eiznhamer
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Patent number: 6770659Abstract: Provided herein are racemic or enantiomerically enriched benzoyl piperidine compounds and pharmaceutically useful salts thereof, pharmaceutical compositions comprising an effective amount of racemic or enantiomerically enriched benzoyl piperidine compounds to treat central nervous system diseases and methods of treating central nervous system diseases in a mammal, in particular psychoses and cognition disorders.Type: GrantFiled: August 26, 2002Date of Patent: August 3, 2004Assignee: SK CorporationInventors: Yong-Moon Choi, Yong-Kil Kim, Jin-Uk Yoo, Eun-Ah Paek, Chun-Eung Park, Sung-Yong Seo, Coo-Min Chung, Joon Heo
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Patent number: 6750230Abstract: This invention relates to the use of pyrazole derivatives of the formula and pharmaceutically acceptable salts and solvates thereof, in the manufacture of a reverse transcriptase inhibitor or modulator, to certain novel such pyrazole derivatives and to processes for the preparation of and compositions containing such novel derivatives.Type: GrantFiled: July 5, 2001Date of Patent: June 15, 2004Assignee: Pfizer, Inc.Inventors: Romuald Gaston Corbau, Charles Eric Mowbray, Manoussos Perros, Paul Anthony Stupple, Anthony Wood
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Patent number: 6750231Abstract: There is provided a compound of formula I, wherein Het1, R1, R2, R3, X and n have meanings given in the description, which are useful in the prophylaxis and in the treatment of diseases mediated by opiate receptors, such as pruritus.Type: GrantFiled: March 19, 2002Date of Patent: June 15, 2004Assignee: Pfizer IncInventors: Stephen Paul Gibson, Ivan Tommasini, Kimberley Verrier, Christopher James Dutton, David Morris Gethin, Douglas James Critcher, Richard Edward Armer