Chalcogen Attached Indirectly To The 1,3-diazole Ring By Acyclic Nonionic Bonding Patents (Class 546/275.1)
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Publication number: 20100190788Abstract: The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula (I) or (II) or a stereoisomer, tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, wherein Ar1, Ar2, R1, R3, p and n have the meaning defined in the claims. In particular, the present invention relates to more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.Type: ApplicationFiled: July 11, 2006Publication date: July 29, 2010Inventors: Olivier Defert, Philippe Van Rompaey, Petra Blom, Dirk Leysen, Gert De Wilde, Thomas Brown
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Patent number: 7750026Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.Type: GrantFiled: January 27, 2005Date of Patent: July 6, 2010Assignee: GlaxoSmithKline LLCInventors: Vipulkumar Kantibhai Patel, Stephen Swanson
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Publication number: 20100022598Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.Type: ApplicationFiled: October 16, 2007Publication date: January 28, 2010Inventors: David Chen, Christopher L. Franklin, Peter R. Guzzo, Linus S. Lin, Michael M.C. Lo, Ravi P. Nargund, Iyassu K. Sebhat
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Publication number: 20100004280Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.Type: ApplicationFiled: October 16, 2007Publication date: January 7, 2010Inventors: David Chen, Christopher L. Franklin, Peter R. Guzzo, Linus S. Lin, Jian Liu, Michael M.-C. Lo, Ravi P. Nargund, Iyassu K. Sebhat
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Patent number: 7626040Abstract: The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses of the compounds.Type: GrantFiled: August 9, 2006Date of Patent: December 1, 2009Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: Paul A. Barsanti, Yi Xia, Weibo Wang, Kris G. Mendenhall, Liana M. Lagniton, Savithri Ramurthy, Megan C. Phillips, Sharadha Subramanian, Rustum Boyce, Nathan M. Brammeier, Ryan Constantine, David Duhl, Annette O. Walter, Tinya J. Abrams, Paul A. Renhowe
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Publication number: 20090209597Abstract: This invention relates to novel imidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.Type: ApplicationFiled: October 12, 2006Publication date: August 20, 2009Applicant: NeuroSearch A/SInventors: William Dalby Brown, Janus S. Larsen, Lene Teuber, David Tristram Brown, Philip K. Ahring, Naheed Mirza, Elsebet Ostergaard Nielsen
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Patent number: 7572921Abstract: The invention comprises a class of derivatives of substituted benzylimidazoles of the formula (I) and methods for making the same. These compounds are useful for the treatment of inflammatory conditions.Type: GrantFiled: April 4, 2006Date of Patent: August 11, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Jin Mi Kim, Rene' Marc Lemieux, Bryan McKibben, Matt Aaron Tschantz, Hui Yu
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Publication number: 20090181949Abstract: The present invention relates to a group of novel 1H-imidazole derivatives, to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component. These 1H-imidazole derivatives are potent cannabinoid-CB1 receptor agonists, partial agonists or antagonists, useful for the treatment of psychiatric and neurological disorders, as well as and other diseases involving cannabinoid neurotransmission. The compounds have the general formula (I) wherein R and R1-R4 have the meanings given in the specification.Type: ApplicationFiled: September 2, 2008Publication date: July 16, 2009Inventors: Cornelis G. KRUSE, Josephus H.M. LANGE, Arnoldus H.J. HERREMANS, Herman H. VAN STUIVENBERG
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Publication number: 20090156619Abstract: The present invention related to compounds of formula (I): or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof. Compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. Compounds of the present invention are useful for treating or preventing neurodegenerative diseases, schizophrenia and stroke among other diseases.Type: ApplicationFiled: October 26, 2006Publication date: June 18, 2009Inventors: Philip Jones, Jesus Maria Ontoria Ontoria
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Publication number: 20090093462Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds (I) pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: October 19, 2005Publication date: April 9, 2009Inventors: Ulricn Abel, Holger Deppe, Achim Feurer, Ulrich Gradler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
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Publication number: 20090030045Abstract: The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: ApplicationFiled: July 2, 2008Publication date: January 29, 2009Inventors: Yonghong Song, Zhaozhong J. Jia, Robert M. Scarborough, Anjali Pandey, Carroll Scarborough
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Publication number: 20080312287Abstract: Formula (I): Where R1 is an optionally substituted C3-C12 hydrocarbyl group (preferably a cyclic alkyl group), an optionally substituted heterocyclic group, an optionally substituted aromatic group or an optionally substituted heteroaromatic group; R is a C(O)yR? group (preferably forming an optionally substituted C2-C5 acyl group), or a S(O)xR? group, where y is 0 or 1 and x is 0, 1 or 2 and R? is H or an optionally substituted C1-C12 alkyl group, or R? is an optionally substituted C5-C12 cycloalkyl group, an optionally substituted heterocyclic group, an optionally substituted aromatic group or an optionally substituted heteroaromatic group; R5, R6, R7, R8, R9 and R10 are each independently selected from H, an optionally substituted C1-C12 hydrocarbyl group, including a C5-C12 cycloalkyl group, an optionally substituted heterocyclic group, an optionally substituted aromatic group or an optionally substituted heteroaromatic group, or R5 and R6, R7 and R8 or R9 and R10 together form a keto (C?O) group; RN is HType: ApplicationFiled: March 17, 2006Publication date: December 18, 2008Applicant: University of WashingtonInventors: Andrew Hamilton, Frederick Buckner, Matthew Glenn, Wesley Van Voorhis, Said Sebti
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Patent number: 7452909Abstract: The present invention relates to imidazole derivatives of formula I wherein R1, R2, R3, R4, X, Y and R are described hereinabove, or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition comprising the imidazole derivatives of formula I, a process for preparing a compound of formula I, and a method of treating or preventing acute and/or chronic neurological disorder comprising administering to a patient in need of such treatment and/or prevention a therapeutically effective amount of said pharmaceutical composition. These disorders include Alzheimer's disease. These disorders also include mild cognitive impairment.Type: GrantFiled: August 26, 2004Date of Patent: November 18, 2008Assignee: Hoffman-La Roche Inc.Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
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Publication number: 20080280769Abstract: A fragment-based strategy, involving “multicomponent reaction chemistry” (MCR), can identify novel chemotypes that disrupt the p53/MDM2 or p53/MDM4 complex employs. This approach uses high resolution structural information to delineate the region of a first protein or a ligand that is nestled within the binding pocket of a second target protein. The identified region is imported into a database containing MCR scaffolds to generate a virtual library of compounds, which subsequently are docked into the binding pocket of the target protein. Results from docking then are used to select compounds for synthesis and screening. A complementary, NMR-based methodology allows for screening the ability of compounds, selected using MCR, to disrupt the p53/MDM2 or p53/MDM4 complex.Type: ApplicationFiled: April 19, 2008Publication date: November 13, 2008Inventor: Alexander Doemling
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Patent number: 7442702Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: September 25, 2002Date of Patent: October 28, 2008Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Bruce A. Lefker, Robert L. Rosati
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Patent number: 7432287Abstract: Compounds represented by formula (I): as well as their pharmaceutically acceptable salts are disclosed. The compounds are useful as glucokinase activating agents for the treatment of diabetes and related conditions. Compositions and methods of treatment are also included.Type: GrantFiled: February 26, 2004Date of Patent: October 7, 2008Assignee: Banyu Pharmeceutical Co., Ltd.Inventors: Tomoharu Iino, Noriaki Hashimoto, Hiroshi Nakashima, Keiji Takahashi, Teruyuki Nishimura, Jun-ichi Eiki
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Patent number: 7425639Abstract: An improved process for preparing arylethanoldiamines is described. Compounds of this type are known to be useful as agonists at a typical beta-adrenoceptors (also known as beta-3-adrenoceptors).Type: GrantFiled: December 17, 2001Date of Patent: September 16, 2008Assignee: SmithKline Beecham CorporationInventors: Jason William Beames Cooke, Bobby Neal Glover, Ronnie Maxwell Lawrence, Matthew Jude Sharp, Maria Fumiko Tymoschenko
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Publication number: 20080177077Abstract: This invention is directed generally to processes for the preparation of compounds of Formula I: wherein R2, R3, R4, R5, X1, X2, X3, X4, X5, X6 are as defined in the specification.Type: ApplicationFiled: December 12, 2007Publication date: July 24, 2008Inventors: Daniel Dukesherer, Michael Mao, Richard Vonder Embse, Gopi Yalamanchili, Rajappa Vaidyanathan, Brian Chekal, George Klemm, Ronald VanderRoset, Randy Geurink
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Patent number: 7390907Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: September 30, 2004Date of Patent: June 24, 2008Assignee: Amgen Inc.Inventors: Ning Chen, Thomas Nixey, Mark H. Norman
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Patent number: 7375232Abstract: Compounds of Formula I, their N-oxides and salts are disclosed wherein A is O or S; G is a 5- or 6-membered heteroaromatic ring or a 5- or 6-membered nonaromatic heterocyclic ring optionally including one or two ring members selected from C(?O), SO or S(O)2, each ring optionally substituted with one to four R2; each J is independently a phenyl ring, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused carbobicyclic or heterobicyclic ring system, wherein each ring or ring system is optionally substituted with one to four R3; and R1, R2, R3, R4 and n are as defined in the disclosure. A composition comprising a compound of Formula I, and a method for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula I are also disclosed.Type: GrantFiled: August 12, 2002Date of Patent: May 20, 2008Assignee: E.I. du Pont de Nemours and CompanyInventors: David Alan Clark, Bruce Lawrence Finkelstein, George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
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Patent number: 7375122Abstract: Compounds useful to control pests are provided.Type: GrantFiled: December 19, 2003Date of Patent: May 20, 2008Assignee: Dow AgroSciences LLCInventors: Jack Geno Samaritoni, David Anthony Demeter, Zoltan Laszlo Benko, James Michael Gifford, Paul Allen Neese, Leonard Paul Dintenfass, Carrie Lynn Rau Schmidt
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Patent number: 7332510Abstract: The present invention relates to imidazole derivatives of formula I wherein R1, R2, R3 and R4 are described hereinbelow. These compounds can be used in the treatment or prevention of mGluR5 receptor mediated disorders. These compounds are useful, inter alia, in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer' disease, cognitive disorders and memory deficits, as well as chronic and acute pain.Type: GrantFiled: June 2, 2004Date of Patent: February 19, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
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Patent number: 7291642Abstract: The present invention provides bradykinin-B1 antagonists of the formula in which A, Ar, G, Q, R1 and R4 are as defined in claim 1, their enantiomers, their diastereomers, their mixtures and their salts, in particular their physiologically acceptable salts with organic or inorganic acids or bases having useful properties, their preparation, medicaments comprising the pharmacologically effective compounds, their preparation and their use.Type: GrantFiled: October 21, 2005Date of Patent: November 6, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Iris Kauffmann-Hefner, Norbert Hauel, Henri Doods, Angelo Ceci, Stefan Peters
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Patent number: 7288541Abstract: The present invention includes ketone derivatives (I) and (II), which are useful as cathepsin K inhibitors.Type: GrantFiled: October 2, 2002Date of Patent: October 30, 2007Assignee: SmithKline Beecham CorporationInventors: David Norman Deaton, John George Catalano
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Publication number: 20070185058Abstract: Compounds of formula I wherein R1, R2, R4, R5, A, B, D and n are as defined, and pharmaceutically acceptable salts thereof, processes for their preparation, their use as pharmaceuticals and pharmaceutical compositions comprising them.Type: ApplicationFiled: January 25, 2007Publication date: August 9, 2007Inventors: Aurelia Conte, Holger Kuehne, Thomas Luebbers, Patrizio Mattei, Cyrille Maugeais, Werner Mueller, Philippe Pflieger
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Patent number: 7153874Abstract: The present invention provides 4-[1-Aryl-imidazol-4-ylethynyl]-2-alkyl-pyridine and 1-heteroaryl-imidazol-4-ylethynyl]-2-alkyl-pyridine derivatives and pharmaceutically acceptable salts thereof for the treatment or prevention of disorders mediated in full or in part by metabotropic glutamate receptor 5. These disorders include, e.g. acute, traumatic and chronic degenerative processes of the nervous system, such as Alzheimer's disease, senile dementia, Parkinson's disease, Huntington's chorea, amyotrophic lateral sclerosis and multiple sclerosis, psychiatric diseases, such as schizophrenia and anxiety, depression, pain and drug dependency.Type: GrantFiled: March 8, 2004Date of Patent: December 26, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
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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: 7091222Abstract: The present invention relates to imidazole derivatives of the general formula wherein R1, R2, R3 and R4 are as defined hereinabove. This invention also relates to the compound's pharmaceutically acceptable salt and processes for the preparation thereof. These compounds can be used for the manufacture of pharmaceutical compositions for the treatment and prevention of mGluR5 receptor mediated disorders. These compounds are useful, inter alia, in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer's disease, cognitive disorders and memory deficit disorders, as well as chronic and acute pain.Type: GrantFiled: June 23, 2004Date of Patent: August 15, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
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Patent number: 7060721Abstract: Imidazole compounds represented by general formula (I): wherein each symbol is as defined in the specification, and salts thereof, and a pharmaceutical composition containing same are provided. These compounds are useful in treating the diseases curable based on a hypoglycemic action, and the diseases curable based on a cGMP-PDE inhibitory action, a smooth muscle relaxing action, a bronchodilating action, a vasodilating action, a smooth muscle cell inhibitory action and an allergy inhibitory action.Type: GrantFiled: December 20, 1999Date of Patent: June 13, 2006Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Noriko Oku, legal representative, Chikako Oku, legal representative, Tomohito Oku, legal representative, Hiroshi Kayakiri, Yoshito Abe, Hitoshi Hamashima, Hitoshi Sawada, Naoki Ishibashi, Hiroyuki Setoi, Noritsugu Yamasaki, Takafumi Imoto, Takahiro Hiramura, Teruo Oku, deceased
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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: 6956050Abstract: This invention provides a compound of the formula (I): wherein: R1 represents a hydrogen atom, an alkyl group, etc.; R2 represents a hydrogen atom, a halogen atom, etc.; R3 represents a hydrogen atom, an alkyl group, etc.; R4 represents an aryl group, etc.; A represents an aryl1, etc; B represents an alkylene etc.; X represents NH, etc.; or a pharmaceutically acceptable ester of such compound, and pharmaceutically acceptable salts thereof. These compounds are useful for the treatment of medical conditions mediated by prostaglamndin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.Type: GrantFiled: April 9, 2003Date of Patent: October 18, 2005Assignee: Pfizer, Inc.Inventors: Misato Hirano, Satoru Iguchi, Kazunari Nakao, Tatsuya Yamagishi
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Patent number: 6943183Abstract: The present invention provides novel 5-substituted tetralones of Formulas I, II, III, and IV and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, which are useful for treating and preventing uncontrolled or abnormal proliferation of tissues, such as cancer, atherosclerosis, restenosis, and psoriasis.Type: GrantFiled: April 16, 2001Date of Patent: September 13, 2005Assignee: Pfizer IncInventors: William Alexander Denny, Richard H. Hutchings, Douglas S. Johnson, James Stanley Kaltenbronn, Ho Huat Lee, Daniele Marie Leonard, Jared Bruce John Milbank, Joseph Thomas Repine, Gordon William Rewcastle, Andrew David White
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Patent number: 6916813Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts thereof, are useful for modulating mitochondrial F1F0 ATPase activity and treating ischemic conditions including myocardial infarction, congestive heart failure, and cardiac arrhythmias.Type: GrantFiled: December 10, 2002Date of Patent: July 12, 2005Assignee: Bristol-Myers Squibb Co.Inventors: Karnail S. Atwal, Gary J. Grover, Charles Z. Ding, Philip D. Stein, John Lloyd, Saleem Ahmad, Lawrnce G. Hamann, David Green, Francis N. Ferrara
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Patent number: 6750338Abstract: This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors.Type: GrantFiled: October 10, 2002Date of Patent: June 15, 2004Assignee: Pharmacia CorporationInventors: Matthew J. Graneto, Michael L. Vazquez, Susan J. Hartmann, Suzanne Metz, John J. Talley, David L. Brown, Richard M. Weier, Michael A. Stealey, Xiangdong Xu
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Patent number: 6706743Abstract: The instant invention provides &bgr;3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, wherein Ar, R, R1, R2, R3, R4, R5, R6, R7, R8, X, and Y, are as defined herein.Type: GrantFiled: March 5, 2003Date of Patent: March 16, 2004Assignee: Pfizer IncInventors: Robert F. Day, Jennifer A. Lafontaine
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Patent number: 6677341Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6649638Abstract: The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylation in an organism using the same.Type: GrantFiled: January 3, 2003Date of Patent: November 18, 2003Assignee: PPD Discovery, Inc.Inventors: Bradley B. Brown, Kenneth S. Rehder
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Publication number: 20030187053Abstract: The invention relates to triamide MTP/ApoB inhibitors of the formula 1 1Type: ApplicationFiled: June 20, 2002Publication date: October 2, 2003Applicant: Pfizer Inc.Inventors: Peter Bertinato, Alan E. Blize, Brian S. Bronk, Hengmiao Cheng, Jin Li, Hiep Huatan, Clive Mason
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Patent number: 6620826Abstract: Novel N-phenyl imidazole derivatives, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.Type: GrantFiled: January 29, 2003Date of Patent: September 16, 2003Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, Joseph Weinstock, Jia-Ning Xiang
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Patent number: 6610687Abstract: The invention relates to benzofuranylsulfonates of the general formula (I), their preparation and their use for the treatment of inflammation.Type: GrantFiled: February 25, 2002Date of Patent: August 26, 2003Assignee: Bayer AktiengesellschaftInventors: Gabriele Bräunlich, Mazen Es-Sayed, Rüdiger Fischer, Burkhard Fugmann, Rolf Henning, Stephan Schneider, Michael Sperzel, Karl-Heinz Schlemmer, Graham Sturton, Mary F. Fitzgerald, Barbara Briggs, Arnel Concepcion, William Bullock
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Patent number: 6566377Abstract: The instant invention provides &bgr;3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, wherein Ar, R, R1, R2, R3, R4, R5, R6, R7, R8, X, and Y, are as defined herein.Type: GrantFiled: October 17, 2001Date of Patent: May 20, 2003Assignee: Pfizer Inc.Inventors: Robert F. Day, Jennifer A. Lafontaine
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Patent number: 6562846Abstract: The present invention relates to bisarylimidazolyl derivatives and pharmaceutical compositions comprising said compounds inhibiting fatty acid amide hydrolase and useful for the treatment of pain, particularly neuropathic pain, psychomotor disorder, hypertension, cardiovascular disease, eating disorder, nausea, AIDS-related complex, glaucoma, inflammation, psoriasis or multiple sclerosis, and other conditions the treatment of which can be effected by inhibiting fatty acid amide hydrolase.Type: GrantFiled: April 23, 2002Date of Patent: May 13, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Sing-Yuen Sit, Kai Xie
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Patent number: 6528650Abstract: The invention relates to novel 4-hydroxyindole derivatives comprising at least one cationic group Z, Z being selected from quaternized aliphatic chains, aliphatic chains containing at least one quaternized saturated ring, and aliphatic chains containing at least one quaternized unsaturated ring, to their use as a coupler for the oxidation dyeing of keratinous fibers, to the dyeing compositions comprising them, and to the methods of oxidation dyeing which employ them.Type: GrantFiled: August 9, 2001Date of Patent: March 4, 2003Assignee: L'Oreal S.A.Inventors: Eric Terranova, Aziz Fadli, Alain LaGrange
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Patent number: 6525076Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: February 8, 2000Date of Patent: February 25, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Robert M. Scarborough
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Patent number: 6518257Abstract: To provide a composition having a steroid C17,20-lyase inhibitory activity and useful as an agent for the prophylaxis or treatment of prostatism and tumors such as breast cancer. A compound represented by the formula: wherein R is a hydrogen atom or a protecting group, R1 is a lower alkyl group or a cyclic hydrocarbon group, R2 is an aromatic hydrocarbon group optionally having substituents or an aromatic heterocyclic group optionally having substituents, R3 is a hydrocarbon group optionally having substituents, a hydroxyl group optionally having substituents, a thiol group optionally having substituents, an amino group optionally having substituents, an acyl group or a halogen atom, and n is an integer of 0 to 4, and a salt thereof have a steroid C17,20-lyase inhibitory activity, and are useful as an agent for the pophylaxis or treatment of prostatism and tumors such as beast cancer and the like.Type: GrantFiled: April 18, 2002Date of Patent: February 11, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Akihiro Tasaka, Tomohiro Kaku, Masami Kusaka
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Patent number: 6518287Abstract: The present invention discloses novel substituted imidazole compounds which have either or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, inflammatory and CNS-related diseases and others.Type: GrantFiled: September 18, 2001Date of Patent: February 11, 2003Assignee: Schering CorporationInventors: Robert G. Aslanian, Stuart Rosenblum, Mwangi Wa Mutahi, Neng-Yang Shih, John J. Piwinski
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Patent number: 6498172Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: August 20, 1999Date of Patent: December 24, 2002Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Bruce A. Lefker, Robert L. Rosati
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Antipsychotic aminomethyl derivatives of 7,8-dihydro-3H-6,9-dioxa-2,3-diaza-cyclopenta[a]naphthalene
Publication number: 20020183331Abstract: Compounds of the formula: 1Type: ApplicationFiled: April 23, 2002Publication date: December 5, 2002Applicant: WyethInventors: Megan Tran, Gary P. Stack -
Patent number: 6482955Abstract: This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors.Type: GrantFiled: August 6, 2001Date of Patent: November 19, 2002Assignee: Pharmacia CorporationInventors: Matthew J. Graneto, Susan J. Hartmann, Suzanne Metz, John J. Talley, Michael L. Vazquez, David Brown, Richard M. Weier, Michael A. Stealey, Xiangdong Xu
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Patent number: RE39634Abstract: The present invention relates to bisarylimidazolyl derivatives and pharmaceutical compositions comprising said compounds inhibiting fatty acid amide hydrolase and useful for the treatment of pain, particularly neuropathic pain, psychomotor disorder, hypertension, cardiovascular disease, eating disorder, nausea, AIDS-related complex, glaucoma, inflammation, psoriasis or multiple sclerosis, and other conditions the treatment of which can be effected by inhibiting fatty acid amide hydrolase.Type: GrantFiled: July 1, 2004Date of Patent: May 15, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Sing-Yuen Sit, Kai Xie