Polycyclo Ring System Having The 1,2-diazole Ring As One Of The Cyclos Patents (Class 546/275.7)
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Patent number: 7081468Abstract: Ortho-substituted anthranilic acid amides and use thereof as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are described.Type: GrantFiled: May 8, 2001Date of Patent: July 25, 2006Assignee: Schering AGInventors: Martin Krueger, Andreas Huth, Orlin Petrov, Dieter Seidelmann, Karl-Heinz Thierauch, Martin Haberey, Andreas Menrad, Alexander Ernst
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Patent number: 7071182Abstract: 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 reproduction and sexual behavior, thyroid hormone secretion, diuresis and water/electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.Type: GrantFiled: December 22, 2004Date of Patent: July 4, 2006Assignee: Abbott LaboratoriesInventors: Andrew J. Souers, Christine A. Collins, Ju Gao, Andrew S. Judd, Philip R. Kym, Mathew M. Mulhern, Hing L. Sham, Dariusz Wodka
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Patent number: 7056932Abstract: The invention is concerned with novel heterocyclyl substituted 1-alkoxy acetic acid derivatives of formula (I) wherein R1 to R6 and A are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments.Type: GrantFiled: December 10, 2004Date of Patent: June 6, 2006Assignee: Hoffman-La Roche Inc.Inventors: Luca Claudio Gobbi, Katrin Groebke Zbinden, Peter Mohr, Ulrike Obst
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Patent number: 7053107Abstract: Indazole compounds that modulate and/or inhibit the ophthalmic diseases and the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating ophthalmic diseases and cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: GrantFiled: December 15, 2003Date of Patent: May 30, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Allen J. Borchardt, Robert Steven Kania, Cynthia L. Palmer
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Patent number: 7019011Abstract: The present invention relates to novel derivatives of general formula (I) in which R3 is a (1–6C)alkyl, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, aryl or heteroaryl fused to a (1–10C) cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(?NH)R1 or C(?NH)NR1 radical; R5, R6 and R7 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, OR8, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1–6C)alkyl, (1–6C)alkoxy, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl.Type: GrantFiled: September 4, 2003Date of Patent: March 28, 2006Assignee: Aventis Pharma S.A.Inventors: Dominique Lesuisse, Gilles Dutruc-Rosset, Franck Halley, Didier Babin, Thomas Rooney, Gilles Tiraboschi
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Patent number: 6992092Abstract: The present invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs; wherein R1, R2, Ra, Rb, X, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof.Type: GrantFiled: April 15, 2004Date of Patent: January 31, 2006Assignee: Pfizer Inc.Inventors: Donald L. Bussolotti, Ronald B. Gammill
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Patent number: 6974813Abstract: NHE-1 inhibitors, methods of using such NHE-1 inhibitors and pharmaceutical compositions containing such NHE-1 inhibitors. The NHE-1 inhibitors are useful for the reduction of tissue damage resulting from tissue ischemia.Type: GrantFiled: December 9, 2002Date of Patent: December 13, 2005Assignee: Warner-Lambert CompanyInventors: Ernest S. Hamanaka, Angel Guzman-Perez, Christian J. Mularski, Roger B. Ruggeri, Ronald T. Wester
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Patent number: 6956052Abstract: The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.Type: GrantFiled: September 19, 2002Date of Patent: October 18, 2005Assignee: Pharmacia CorporationInventors: Arija A. Bergmanis, Michael Clare, Joyce Z. Crich, Lifeng Geng, Timothy J. Hagen, Gunnar J. Hanson, Stephen C. Houdek, He Huang, Donna M. Iula, Francis J. Koszyk, Shuyuan Liao, Scott B. Mohler, Maria Nguyen, Richard A. Partis, Michael A. Stealey, Michael B. Tollefson, Richard M. Weier, Xiangdong Xu, Dominique Bonafoux, Theresa R. Fletcher, Bruce C. Hamper, Patrick J. Lennon, Subo Liao, Suzanne Metz, David S. Oburn, Thomas J. Owen, Angela M. Scates, Michael L. Vazquez, Serge G. Wolfson
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Patent number: 6949579Abstract: The present invention relates to the novel indazole derivatives of general formula (I): in which: R is either O, S or NH; R3 is an alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, aryl, heterocycle, cycloalkyl, alkenyl, etc. radical; these radicals being optionally substituted with one or more substituents; R4, R5, R6 and R7 are chosen, independently of each other, from the following radicals: hydrogen, halogen, CN, NO2, NH2, OH, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycle, cycloalkyl, alkenyl, etc.; these radicals being optionally substituted with one or more substituents.Type: GrantFiled: March 11, 2003Date of Patent: September 27, 2005Assignee: Aventis Pharma S.A.Inventors: Gilles Dutruc-Rosset, Dominique Lesuisse, Thomas Rooney, Franck Halley
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Patent number: 6943186Abstract: The present invention features a method for treating sepsis. The method includes administrating to a subject in need thereof an effective amount of a fused pyrazolyl compound of formula (I): A is H, C1˜C6 alkyl, or in which n is 0, 1, 2, or 3; each of Ar1, Ar2, and Ar3, independently, is phenyl, pyridinyl, thienyl, furyl, or pyrrolyl; and each of R1, R2, R3, R4, R5, and R6, independently, is XYZ; or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)1-6O; in which X is a bond or C1˜C6 alkylene, Y is a bond, O, S, OC(O), OC(O)(CH2)1-6C(O)O, C(O)O, C(O)S, C(O)NH, C(O)NC1˜C6 alkyl, NH, or NC1˜C6 alkyl, and Z is H, halogen, CN, NO2, or C1˜C6 alkyl; and provided that one of R3 and R4 is not H.Type: GrantFiled: January 24, 2003Date of Patent: September 13, 2005Assignee: Yung Shin Pharmaceutical Ind. Co., Ltd.Inventors: Che-Ming Teng, Shiow-Lin Pan, Jih-Hwa Guh, Sheng-Chu Kuo, Fang-Yu Lee
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Patent number: 6890925Abstract: Disclosed are methods of using soluble epoxide hydrolase (sEH) inhibitors of the formulas I and Ia for diseases related to cardiovascular disease.Type: GrantFiled: September 25, 2003Date of Patent: May 10, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Richard H. Ingraham, John R. Proudfoot
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Patent number: 6891044Abstract: Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: GrantFiled: February 15, 2003Date of Patent: May 10, 2005Assignee: Agouron Pharmaceuticals, Inc.Inventors: Robert Steven Kania, Steven Lee Bender, Allen J. Borchardt, Stephan James Cripps, Ye Hua, Michael David Johnson, Theodore Otto Johnson, Jr., Hiep The Luu, Cynthia Louise Palmer, Siegfried Heinz Reich, Anna Maria Tempczyk-Russell, Min Teng, Christine Thomas, Michael David Varney, Michael Brennan Wallace, Michael Raymond Collins
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Patent number: 6884890Abstract: Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: GrantFiled: February 13, 2003Date of Patent: April 26, 2005Assignee: Agouron Pharmaceuticals, Inc.Inventors: Robert Steven Kania, Steven Lee Bender, Allen J. Borchardt, Stephan James Cripps, Ye Hua, Michael David Johnson, Theodore Otto Johnson, Jr., Hiep The Luu, Cynthia Louise Palmer, Siegfried Heinz Reich, Anna Marie Tempczyk-Russell, Min Teng, Christine Thomas, Michael David Varney, Michael Brennan Wallace, Michael Raymond Collins
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Patent number: 6849643Abstract: The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.Type: GrantFiled: December 6, 2001Date of Patent: February 1, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Han-Cheng Zhang, Bruce Maryanoff, Bruce Conway, Kimberly White, Hong Ye, Leonard Robert Hecker, David F. McComsey
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Patent number: 6846819Abstract: Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.Type: GrantFiled: October 6, 2000Date of Patent: January 25, 2005Assignee: Affinium Pharmaceuticals, Inc.Inventors: William H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas, Walter E. DeWolf, Jr., Dalia R. Jakas
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Patent number: 6841563Abstract: Disclosed is a compound represented by structural formula (I): R1 is a substituted or unsubstituted aryl group. R2 and R3 are independently —H, a C1-C4 straight chained or branched alkyl group. R4 and R5 are independently —H, a C1-C4 straight chained or branched alkyl group or, taken together with the nitrogen atom to which each is bonded, a non-aromatic heterocyclic ring. Ring A and Ring B are independently further substituted with zero, one or two substituents. Physiologically acceptable salts of structural formula shown above are also included. Also disclosed is a method promoting growth, efficiency of feed utilization and/or production of lean body mass in a livestock animal. The method comprises administering to the animal an effective amount of one or more compounds represented by the structural formula as shown or a physiologically acceptable salt thereof.Type: GrantFiled: November 13, 2000Date of Patent: January 11, 2005Assignee: Eli Lilly and CompanyInventors: Randall Bruce Hopkins, Deana Lori Hancock, Michael Eugene Quimby
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Patent number: 6831175Abstract: Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.Type: GrantFiled: December 12, 2002Date of Patent: December 14, 2004Assignee: Abbott LaboratoriesInventors: Qun Li, Keith W. Woods, Gui-Dong Zhu, John P. Fischer, Jianchun Gong, Tongmei Li, Virajkumar Gandhi, Sheela A. Thomas, Garrick K. Packard, Xiaohong Song, Jason N. Abrams, Robert B. Diebold, Jürgen Dinges, Charles W. Hutchins, Vincent S. Stoll, Saul H. Rosenberg, Vincent L. Giranda
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Publication number: 20040224988Abstract: The invention provides dosage forms of a compound of formula 1: 1Type: ApplicationFiled: April 1, 2004Publication date: November 11, 2004Applicant: Agouron Pharmaceuticals, Inc.Inventors: James Freddo, Dana Hu-Lowe, Yazdi Kersi Pithavala, Heidi Steinfeldt
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Patent number: 6800641Abstract: Compounds of the formula: useful for treatment of disorders of the dopaminergic system, such as schizophrenia, schizoaffective disorder, bipolar disorder, Parkinson's disease, L-DOPA induced pychoses and dyskinesias, Tourette's syndrome and hyperprolactinemia and in the treatment of drug addiction such as the addiction to ethanol, nicotine or cocaine and related illnesses.Type: GrantFiled: April 23, 2002Date of Patent: October 5, 2004Assignee: WyethInventors: Megan Tran, Gary P. Stack
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Publication number: 20040192735Abstract: Indazole compounds that modulate and/or inhibit the ophthalmic diseases and the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating ophthalmic diseases and cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: ApplicationFiled: December 15, 2003Publication date: September 30, 2004Applicant: Agouron Pharmaceuticals, Inc.Inventors: Allen J. Borchardt, Robert Steven Kania, Cynthia L. Palmer
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Publication number: 20040158067Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: 1Type: ApplicationFiled: November 7, 2003Publication date: August 12, 2004Applicant: Neurogen CorporationInventors: Alan J. Hutchison, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zihong Guo, Peter Hrnciar
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Publication number: 20040152902Abstract: PDE4 inhibition is achieved by novel nitroxide compounds, e.g., N-substituted aniline and diphenylamine analogs.Type: ApplicationFiled: November 19, 2003Publication date: August 5, 2004Inventors: Richard A. Schumacher, Elizabeth Doorly Graham, Allen T. Hopper, Ashok Tehim
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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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Publication number: 20040110956Abstract: The present invention relates to novel derivatives of general formula (I) 1Type: ApplicationFiled: September 4, 2003Publication date: June 10, 2004Inventors: Dominique Lesuisse, Gilles Dutruc-Rosset, Franck Halley, Didier Babin, Thomas Rooney
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Patent number: 6747046Abstract: Substituted N-(1,4,5,6-tetrahydro-cyclopentapyrazol-3-yl) derivatives, their production, as well as intermediate products for their production, and the use as pharmaceutical agents for treating various diseases are described.Type: GrantFiled: September 25, 2002Date of Patent: June 8, 2004Assignee: Schering AktiengesellschaftInventors: Martin Krüger, Olaf Prien, Andreas Steinmeyer, Jörg Kroll, Alexander Ernst, Gerhard Siemeister, Martin Haberey, Jens Hoffmann
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Patent number: 6716837Abstract: Described herein are compounds useful in the treatment of migraine, which have the general formula: wherein: W is a CH group or a N atom; Z is N or C—R4; B and D are selected independently from CH and N, with the proviso that at least one of B and D is CH and with the further proviso that one of B and D can represent N only when W and Z are both other than N; A is a group of Formula II, III or IV, such that group A contains at least 1 N atom; NR7 is either —NH— or —N═; is a single or double bond; X is a N atom, a CH group or a C(OH) group when is a single bond; or, when is a double bond, a C atom; Y is an NH, N-alkyl, N-benzyl or CH2 group; U and V each represent a N atom or a CH group, with the proviso that both cannot be N; a and b are, independently, 0 or 1; c is an integer from 0 to 3; d is an integer from 1 to 3; e is an integer from 1 to 2; f is an integer from 0 to 3; g is an integer from 3 to 6 and h is an integer from 2 to 3; such that the sum of c aType: GrantFiled: November 13, 2000Date of Patent: April 6, 2004Assignee: NPS Allelix Biopharmaceuticals, Inc.Inventors: Louise Edwards, Methvin Isaac, Shawn Maddaford, Abdelmalik Slassi, Tao Xin
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Patent number: 6677452Abstract: The present invention relates to novel pyridine carboxamide or sulfonamide derivative compounds of the following formula: wherein R1 to R6 have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing pyridine carboxamide or sulfonamide derivative compounds.Type: GrantFiled: September 30, 1999Date of Patent: January 13, 2004Assignee: Lion Bioscience AGInventors: Yuewu Chen, Hengyuan Lang, Yazhong Pei
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Patent number: 6656941Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables R1, R2, R3, n, and Ar are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: September 6, 2001Date of Patent: December 2, 2003Assignee: Neurogen CorporationInventors: George Maynard, Pamela Albaugh, Stanislaw Rachwal, Linda Gustavson
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Publication number: 20030203922Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: July 17, 2002Publication date: October 30, 2003Applicant: Amgen Inc.Inventors: Vinod F. Patel, Benny Askew, Shon Booker, Guoqing Chen, Lucian V. DiPietro, Julie Germain, Gregory J. Habgood, Qi Huang, Tae-Seong Kim, Aiwen Li, Nobuko Nishimura, Rana Nomak, Babak Riahi, Chester Chenguang Yuan, Daniel Elbaum
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Publication number: 20030199455Abstract: The invention is directed to novel indazole peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted indazole peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.Type: ApplicationFiled: March 31, 2003Publication date: October 23, 2003Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, Anjali Pandey, Robert M. Scarborough
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Patent number: 6635639Abstract: Described are compounds having formula I or II: wherein: X is N, and Ak represents a C1-3 alkylene chain; and a salt, solvate or prodrug thereof.Type: GrantFiled: February 13, 2002Date of Patent: October 21, 2003Assignee: NPS Allelix Corp.Inventors: Jalaj Arora, Louise Edwards, Methvin Issac, Anne O'Brien, Abdelmalik Slassi, Ashok Tehim, Tao Xin
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Publication number: 20030186966Abstract: This invention concerns amide derivatives of Formula (I) wherein X is CH or N; Y is CH or N; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-3; R2 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and (1-6C)alkoxycarbonyl; R3 is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; q is 0-4; and Q is a group such as aryl, aryloxy, aryl-(1-6C)alkoxy, arylamino, N-(1-6C)alkyl-arylamino and aryl-(1-6C)alkylamino; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: ApplicationFiled: January 29, 2003Publication date: October 2, 2003Applicant: ASTRAZENECA ABInventor: Dearg S. Brown
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Patent number: 6610692Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is NY or O; c is CY2 or N; d is CY3 or N; e is CY4 or N; f is CY5 or N; g is CY6 or N; Y4, Y5, and Y6 are independently hydrogen, C1-4 alkyl, or halogen; Y1 and Y2 are independently hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, NH2, OH or C1-4 alkoxy, and Y3 is hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, —CN, NH2, OH or C1-4 alkoxy; A is and W, W1, R1, R3, R4, R5, X and Z are defined in the specification.Type: GrantFiled: October 28, 1999Date of Patent: August 26, 2003Assignee: Merck & Co., Inc.Inventors: Philip E. Sanderson, Bruce D. Dorsey, Terry A. Lyle, Matthew G. Stanton, Donnette Staas, Adel M. Naylor-Olsen, Craig Coburn, Matthew M. Morrissette
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Patent number: 6608058Abstract: The present invention relates to novel 6-methylnicotinamide derivatives and their pharmaceutically acceptable salts, the process for preparing them, and the pharmaceutical compositions containing said compounds as active ingredients. The 6-methylnicotinamide derivatives of the present invention exhibit their inhibitory activity against the proliferation of human immunodeficiency virus (HIV) as well as hepatitis B virus (HBV) and hepatitis C virus (HCV), such that they can be used for hepatitis B, hepatitis C and acquired immune deficiency syndrome (AIDS).Type: GrantFiled: October 10, 2002Date of Patent: August 19, 2003Assignee: Dong Wha Pharm. Ind. Co., Ltd.Inventors: Sung-June Yoon, Sang-Wook Lee, Jin-Soo Lee, Nam-Doo Kim, Geun-Hyung Lee, Hak-Dong Lee, Jong-Woo Kim, Sang-Jin Park, Hee-Jeong Park
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Publication number: 20030153576Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I):Type: ApplicationFiled: December 19, 2001Publication date: August 14, 2003Inventors: Albert J. Robichaud, Ian S. Mitchell
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Publication number: 20030139463Abstract: Indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating, e.g., kinases-dependent diseases to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: ApplicationFiled: November 8, 2002Publication date: July 24, 2003Inventors: Siegfried Heinz Reich, Ted Michael Bleckman, Susan Elizabeth Kephart, William Henry Romines, Michael B. Wallace
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Patent number: 6593349Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides bisarylamines, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases) and as neuroprotective agents (e.g., to prevent stroke and the like) by opening potassium channels associated with the onset or recurrence of the indicated conditions.Type: GrantFiled: March 11, 2002Date of Patent: July 15, 2003Assignee: ICAgen, Inc.Inventors: Grant Andrew McNaughton-Smith, George Salvatore Amato
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Publication number: 20030109709Abstract: Provided are processes and chemical intermediates useful for preparing a compound of the formula I 1Type: ApplicationFiled: September 18, 2002Publication date: June 12, 2003Inventors: M.V. Ramana Reddy, Stanley C. Bell
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Publication number: 20030100554Abstract: This invention relates to pyrazole derivatives of formula (I) 1Type: ApplicationFiled: April 5, 2002Publication date: May 29, 2003Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
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Publication number: 20030092709Abstract: The present invention relates to novel 6-methylnicotinamide derivatives and their pharmaceutically acceptable salts, the process for preparing them, and the pharmaceutical compositions containing said compounds as active ingredients. The 6-methylnicotinamide derivatives of the present invention exhibit their inhibitory activity against the proliferation of human immunodeficiency virus (HIV) as well as hepatitis B virus (HBV) and Hepatitis C virus (HCV), such that they can be used for hepatitis B, hepatitis C and acquired immune deficiency syndrome (AIDS).Type: ApplicationFiled: October 10, 2002Publication date: May 15, 2003Inventors: Sung-June Yoon, Sang-Wook Lee, Jin-Soo Lee, Nam-Doo Kim, Geun-Hyung Lee, Hak-Dong Lee, Jong-Woo Kim, Sang-Jin Park, Hee-Jeong Park
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Patent number: 6559174Abstract: Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.Type: GrantFiled: March 13, 2002Date of Patent: May 6, 2003Assignee: Merck & Co., Inc.Inventors: Linus S. Lin, Shrenik K. Shah, Linda L. Chang, William K. Hagmann, Richard A. Mumford
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Patent number: 6545033Abstract: The present invention is directed to novel pyrazole derivatives and their use as pesticidal agents.Type: GrantFiled: October 6, 2000Date of Patent: April 8, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Daljit S. Dhanoa, Sanath Meegalla, Richard M. Soll, Dario Doller, Deyou Sha, Ruiping Liu, Gary Silver, Yu-Kai Lee
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Patent number: 6545157Abstract: A dye-forming method comprising: reacting a dye-forming coupler and a color developing agent precursor represented by the following general formula (I): wherein A3 represents a group other than a hydrogen atom which leaves, accompanied by the bonding electron pair with the nitrogen atom in general formula (I), to thereby form a color developing agent; A2 represents a group which leaves in association with a dye-formation; and A1 represents a group which forms a dye together with the nitrogen atom and the coupler.Type: GrantFiled: November 14, 2001Date of Patent: April 8, 2003Assignee: Fuji Photo Film Co., Ltd.Inventors: Kensuke Morita, Shun-ichi Ishikawa, Hideaki Naruse, Koki Nakamura, Toshio Kawagishi, Tadashi Ohmatsu, Kozo Aoki
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Patent number: 6538009Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, n, p, W, X, Y and Z are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats, horses and livestock.Type: GrantFiled: April 2, 2001Date of Patent: March 25, 2003Assignee: Pfizer, Inc.Inventor: Subas Man Sakya
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Patent number: 6534504Abstract: Disclosed is compound represented by Structural Formula (I), wherein Ring A, Ring B and Ring C are independently substituted or unsubstituted. R1 and R2 are independently a C1-C4 straight chained or branched alkyl group. Also disclosed is a method of increasing the quantity and improving quality of meat obtained from a livestock animal. The method comprises administering to the animal an effective amount of one or more compounds represented by Structural Formula (I).Type: GrantFiled: April 16, 2002Date of Patent: March 18, 2003Assignee: Eli Lilly and CompanyInventors: Deana Lori Hancock, Randall Bruce Hopkins, Michael Eugene Quimby, Andrew Jason Wuethrich
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Patent number: 6534655Abstract: Chemical compounds that are derivatives of indeno[1,2-c]pyrazole are inhibitors of tyrosine kinase activity. Several of the tyrosine kinases, whose activity is inhibited by these chemical compounds, are involved in angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell proliferation is a factor. Compounds of this invention also inhibit the induction of vascular hyperpermeability and the associated formation of edema, ascites, and exudates.Type: GrantFiled: April 3, 2000Date of Patent: March 18, 2003Assignee: BASF AktiengesellschaftInventors: Lee D. Arnold, Yajun Xu, Teresa Barlozzari, Paul Rafferty, Michael Hockley, Allyson Turner
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Patent number: 6534524Abstract: Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: GrantFiled: October 25, 2001Date of Patent: March 18, 2003Assignee: Agouron Pharmaceuticals, Inc.Inventors: Robert Steven Kania, Steven Lee Bender, Allen J. Borchardt, Stephan James Cripps, Ye Hua, Michael David Johnson, Theodore Otto Johnson, Jr., Hiep The Luu, Cynthia Louise Palmer, Siegfried Heinz Reich, Anna Marie Tempczyk-Russell, Min Teng, Christine Thomas, Michael David Varney, Michael Brennan Wallace, Michael Raymond Collins
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Patent number: 6531491Abstract: Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: GrantFiled: October 25, 2001Date of Patent: March 11, 2003Assignee: Agouron Pharamaceuticals, Inc.Inventors: Robert Steven Kania, Steven Lee Bender, Allen J. Borchardt, Stephan James Cripps, Cynthia Louise Palmer, Anna Maria Tempczyk-Russell, Michael David Varney, Michael Raymond Collins
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Publication number: 20020193597Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides bisarylamines, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases) and as neuroprotective agents (e.g., to prevent stroke and the like) by opening potassium channels associated with the onset or recurrence of the indicated conditions.Type: ApplicationFiled: March 11, 2002Publication date: December 19, 2002Applicant: ICAgen, Inc.Inventors: Grant Andrew McNaughton-Smith, George Salvatore Amato
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Publication number: 20020169322Abstract: Described are compounds having formula I or II: 1Type: ApplicationFiled: February 13, 2002Publication date: November 14, 2002Applicant: NPS Allexlix Corp.Inventors: Jalaj Arora, Louise Edwards, Methvin Isaac, Anne O'Brien, Abdelmalik Slassi, Ashok Tehim, Tao Xin