Ring Oxygen In The Bicyclo Ring System Patents (Class 546/115)
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Patent number: 7323494Abstract: Disclosed is a compound of having the formula: pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein. The compounds, salts and solvates of this invention are useful as LXR agonists.Type: GrantFiled: March 26, 2003Date of Patent: January 29, 2008Assignee: SmithKline Beecham CorporationInventors: Scott K. Thompson, James S. Frazee, Lara S. Kallander, Chun Ma, Joseph Marino, Michael J. Neeb, Ajita Bhat
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Patent number: 7265115Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.Type: GrantFiled: April 11, 2003Date of Patent: September 4, 2007Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Daniela Barlocco Cristina, Jerome F. Daanen, Michael J. Dart, Michael D. Meyer, Keith B. Ryther, Michael R. Schrimpf, Kevin B. Sippy, Richard B. Toupence
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Patent number: 7265128Abstract: The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: January 13, 2004Date of Patent: September 4, 2007Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Charles G. Caldwell, Robert J. Mathvink, Hyun O. Ok, Leah Bitalac Reigle, Ann E. Weber
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Patent number: 7262300Abstract: Two new crystalline monhydrates and two new crystalline anhydrates of gaboxadol are disclosed together with methods for preparing them.Type: GrantFiled: January 28, 2005Date of Patent: August 28, 2007Assignee: Merck Sharp & Dohme Ltd.Inventor: Vincent Brett Cooper
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Patent number: 7253154Abstract: The invention relates to compounds of the following formula (I) or their salts: in which R1 represents OR4 or others, in which R4 is an alkyl group having 1-8 carbon atoms which may have a substituent or the like; R2 is halogen, nitro, cyano, carboxyl, or the like; R3 is hydrogen, halogen, hydroxyl, amino, carboxyl, or the like; X is NR11, oxygen, or sulfur, in which R11 is hydrogen, or an alkyl group having 1-8 carbon atom which may have a substituent; and each of Y and Z is CR12 or nitrogen, in which R12 has the same meaning as R3 above, and a xanthine oxidase inhibitor containing the compound as an active ingredient.Type: GrantFiled: November 14, 2002Date of Patent: August 7, 2007Assignee: Nippon Chemiphar Co., Ltd.Inventors: Shinichi Yoshida, Atsushi Tendo, Kunio Kobayashi, Nobutaka Mochiduki, Tomio Yamakawa, Yoriko Shinohara
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Patent number: 7253165Abstract: The compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.Type: GrantFiled: May 12, 2004Date of Patent: August 7, 2007Assignee: Aventis Pharmaceuticals Inc.Inventors: Gregory M. Shutske, James A. Hendrix, John G. Jurcak, Brian S. Freed, Nicholas J. Hrib, John D. Tomer, IV, Reda G. Hanna
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Patent number: 7220860Abstract: A compound has the formula in racemic form, enantiomerically enriched form or enantiomerically pure form. R6 is preferably —Si(R8R9R10) or —(R7)Si(R8R9R10), wherein R7 is an alkylene group, an alkenylene group, or an alkynylene group; and R8, R9 and R10 are independently a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group, an aryl group or a —(CH2)NR11 group, wherein N is an integer within the range of 1 through 10 and R11 is a hydroxy group, alkoxy group, an amino group, an alkylamino group, a dialkylamino group, a halogen atom, a cyano group, —SRc or a nitro group. R1–R4 can be broadly substituted. R5 is preferably a C1-10 alkyl group, an alkenyl group, an alkynyl group, or a benzyl group. R13 is preferably H, F or —CH3. R16 is R16 is —C(O)Rf or H. The E-ring (the lactone ring) may be opened. A method of synthesis of compound (1) and intermediates in the synthesis thereof are provided.Type: GrantFiled: August 16, 2004Date of Patent: May 22, 2007Assignee: University of PittsburghInventors: Dennis P. Curran, Bom David, Thomas G. Burke
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Patent number: 7205314Abstract: The present invention relates to new compounds of formula (I) wherein Y, P, R1, R2, R3, n, m are defined as in claim 1, a process for their preparation and new intermediates used therein, pharmaceutical composition containing said therapeutically active compounds and to the use of said active compounds in therapy, especially in the prevention and/or treatment of dementia related disease, Alzheimer's Disease and conditions associated with glycogen synthase kinase-3Type: GrantFiled: December 18, 2002Date of Patent: April 17, 2007Assignee: AstraZeneca ABInventors: Stefan Berg, Ratan Bhat, James Empfield, Sven Hellberg, Michael Klimas, James Woods
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Patent number: 7205316Abstract: Compounds of formula (I) wherein R1 or R2 is a tricyclic or bicyclic ring, each of which contains at least two heteroatoms, and R1, R2, R3, R3a, R3b, R4, R5, L, X, X?, Y, Y?, Z, and Z? are as defined herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: GrantFiled: May 6, 2005Date of Patent: April 17, 2007Assignee: Abbott LaboratoriesInventors: Robert J. Altenbach, Lawrence A. Black, Marlon D. Cowart, Huaqing Liu
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Patent number: 7199128Abstract: The invention provides compounds and salts of Formula I and Formula II: which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A1, A8, R2, R3, R5, R6, R7, and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of compounds of Formula I and/or Formula II and one or more other active agents. The invention also provides methods for treating microbial and protozoal infections in animals.Type: GrantFiled: February 1, 2006Date of Patent: April 3, 2007Assignee: Achillion Pharmaceuticals, Inc.Inventors: Barton J. Bradbury, Jason Allan Wiles, Milind Deshpande, Qiuping Wang, Akihiro Hashimoto, Edlaine Lucien
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Patent number: 7173022Abstract: The invention encompasses a series cyclic bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS.Type: GrantFiled: May 26, 2005Date of Patent: February 6, 2007Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Jacques Banville, John D. Matiskella, Serge Plamondon, Yasutsugu Ueda
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Patent number: 7173134Abstract: The present invention includes novel retinoid compounds that have selectivity as RXR agonists on one or more isoforms of RXR, currently, RXR?, RXR?, or RXR?. The present compounds, and pharmaceutical compositions incorporating these compounds, therefore, are effective in treating conditions mediated by RXRs. Among other physiological responses, the compounds of the present invention reduce blood glucose and maintain body weight, and, thus, are useful for the treatment of diabetes (NIDDIM) and obesity.Type: GrantFiled: September 16, 2002Date of Patent: February 6, 2007Assignee: SmithKline Beecham CorporationInventors: Curt Dale Haffner, Istvan Kaldor, Darryl Lynn McDougald, Aaron Bayne Miller
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Patent number: 7141564Abstract: Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.Type: GrantFiled: May 24, 2002Date of Patent: November 28, 2006Assignee: SmithKline Beecham p.l.c.Inventors: Gerald Brooks, David Thomas Davies, Graham Elgin Jones, Roger Edward Markwell, Neil David Pearson
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Patent number: 7115654Abstract: The invention provides compounds of Formula I and derivatives thereof, pharmaceutical compositions comprising a compound of Formula I, and methods of treatment utilizing such compounds and compositions: wherein: R1 is chosen from optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, and optionally substituted heteroaralkyl; L is a linker; R2 is chosen from optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, and optionally substituted heteroaralkyl; and or single stereoisomers, mixtures of stereoisomers, or the pharmaceutically acceptable salts, amides, or esters thereof.Type: GrantFiled: June 5, 2003Date of Patent: October 3, 2006Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Darin Allen, Bruce Fahr, Johan Oslob, Brian C. Raimundo, Michael J. Romanowski
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Patent number: 7105535Abstract: Compounds which are oxazolyl-pyrazole derivatives, as defined in the specification, and pharmaceutically acceptable salts thereof; are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, viral infections, autoimmune diseases and neurodegenerative disorders.Type: GrantFiled: January 28, 2002Date of Patent: September 12, 2006Assignee: Pfizer Italia S.R.L.Inventors: Daniela Berta, Eduard Felder, Anna Vulpetti, Marzia Villa
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Patent number: 7102008Abstract: The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein the variables A, R1, R2, R3, R4, Z, U, X, Y, Za, and n are defined are as defined herein, which are useful as inhibitors of matrix metalloproteinases (MMP) and/or TNF-? converting enzyme (TACE), or a combination thereof.Type: GrantFiled: July 31, 2003Date of Patent: September 5, 2006Assignee: Bristol-Myers Squibb CompanyInventor: Thomas P. Maduskuie
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Patent number: 7091216Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.Type: GrantFiled: August 1, 2003Date of Patent: August 15, 2006Assignee: Merck & Co., Inc.Inventors: Richard B. Toupence, John S. Debenham, Mark T. Goulet, Christina B. Madsen-Duggan, Thomas F. Walsh, Shrenik K. Shah
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Patent number: 7087601Abstract: Phenyl compounds substituted at the 1-position with a fused bicyclo moeity formed from a five-membered heterocycle fused to a six-membered carbocycle, to a six-membered aryl, or to a six-membered hetaryl, and further optionally substituted at the 3,4 positions, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.Type: GrantFiled: November 26, 2002Date of Patent: August 8, 2006Assignee: Merck & Co., Inc.Inventors: Jeannie Arruda, Celine Bonnefous, Brian T. Campbell, Rowena V. Cube, Benito Munoz, Brian Stearns, Jean-Michel Vernier, Bowei Wang, Xiumin Zhao
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Patent number: 7087756Abstract: The invention provides compounds of formula I, wherein X, Y, R1, R2, and R3 are as defined in the description, and the preparation thereof. The compounds of formula I are useful as pharmaceuticals.Type: GrantFiled: August 14, 2002Date of Patent: August 8, 2006Assignee: Novartis AGInventors: Samuel Hintermann, Bastian Hengerer, Ulrike Von Krosigk
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Patent number: 7071192Abstract: The present invention concerns compounds of formula (I), prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof wherein -a1=a2-a3=a4-represents a radical of formula —CH?CH—CH?CH—; —N—CH—CH?CH—; —CH?N—CH?CH—; —CH?CH—N?CH—; —CH?CH—CH?N—; wherein each hydrogen atom may optionally be substituted; Q is a radical of formulae (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), wherein Alk is C1-6alkanediyl; Y1 is a bivalent radical of formula —NR2— or —CH(NR2R4)—; X1 is NR4, S, S(?O), S(?O)2, O, CH2, C(?O), CH(?CH2), CH(OH), CH(CH3), CH(OCH3), CH(SCH3), CH(NR5aR5b), CH2—NR4 or NR4—CH2; X2 is a direct bond, CH2, C(?O), NR4, C1-4alkyl-NR4, NR4—C1-4alkyl, t is 2 to 5; u is 1 to 5; v is 2 or 3; and whereby each hydrogen in Alk and in (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), may optionally be replaced by R3: provided that when R3 is hydroxy or C1-6alkyloxy, then R3 cannot replace a hydrogen atom in the a position relative to a nitrogen atom; G is a diType: GrantFiled: June 20, 2000Date of Patent: July 4, 2006Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Jean Fernand Armand Lacrampe, Jérôme Emile Georges Guillemont, Marc Gaston Venet, Koenraad Jozef Lodewijk Marcel Andries
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Patent number: 7067515Abstract: The invention provides compounds of Formula I: where in W is These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful to treat diseases or conditions in which ?7 is known to be involved.Type: GrantFiled: June 6, 2002Date of Patent: June 27, 2006Assignee: Pfizer Inc.Inventors: Donn G. Wishka, Steven Charles Reitz, David W. Piotrowski, Vincent E. Groppi, Jr.
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Patent number: 7053219Abstract: The invention relates to isoxazolopyridone derivatives of a formula (I-a): wherein R1a represents an optionally-substituted heteroaryl or phenyl group, R2a represents an optionally-substituted phenyl or heteroaryl group, and R3a represents a methyl group, provided that, (1) when R1a is an unsubstituted phenyl group, then R2a must not be a para-substituted phenyl group of which the substituent is any of a methoxy group, a chloro group, a methyl group, a trifluoromethyl group, a fluoro group, a bromomethyl group or a dimethylaminomethyl group, and R2a must not be an unsubstituted heteroaryl group, and (2) when R1a is a 4-tolyl group or a 4-fluorophenyl group, then R2a must not be an unsubstituted phenyl group, a 4-methoxyphenyl group or a 4-fluorophenyl group, or their pharmaceutically-acceptable salts.Type: GrantFiled: December 10, 2003Date of Patent: May 30, 2006Assignee: Banyu Pharmaceutical Co. Ltd.Inventors: Masayuki Nakamura, Hideki Kurihara, Mitsuru Ohkubo, Naohiro Tsukamoto
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Patent number: 6998407Abstract: Chemical compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function, pharmaceutical compositions comprising these compounds, methods of treatment employing these compounds and compositions, and processes for preparing these compounds. The compounds are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection.Type: GrantFiled: November 18, 2003Date of Patent: February 14, 2006Assignees: Telik, Inc., Sanwa Kagaku Kenkyusho Co. Ltd.Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
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Patent number: 6992188Abstract: Corticotropin-releasing factor (CRF) antagonists having the formula wherein the dashed lines, A, B, D E, F, Z, G, R3, and R5 having the definitions set forth in the specification pharmaceutical compositions containing them.Type: GrantFiled: December 6, 1996Date of Patent: January 31, 2006Assignee: Pfizer, Inc.Inventor: Yuhpyng L. Chen
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Patent number: 6992086Abstract: The present invention relates to chemical compounds, pharmaceutical compositions comprising said compounds, uses of said compounds and compositions, methods of treatment employing said compounds and compositions, and processes for preparing said compounds. Specifically, this invention relates to novel compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection. More specifically, the invention is related to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases.Type: GrantFiled: November 17, 2003Date of Patent: January 31, 2006Assignee: Telik, Inc.Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
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Patent number: 6987117Abstract: Compounds of the formula useful for the treatment of depression, obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety disorder, sexual dysfunction, eating disorders, obesity, addictive disorders caused by ethanol or cocaine abuse, and dysthymia.Type: GrantFiled: September 12, 2003Date of Patent: January 17, 2006Assignee: WyethInventors: Megan Tran, Gary P. Stack
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Patent number: 6982264Abstract: The invention relates to substituted alcohol compounds of the formula (I): wherein X, R1, R2, R3, RN, R20 and RC are defined herein. The compounds are useful in the treatment or prevention of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers.Type: GrantFiled: June 27, 2002Date of Patent: January 3, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Varghese John, Roy Hom, John Tucker
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Patent number: 6962942Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.Type: GrantFiled: September 16, 2002Date of Patent: November 8, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Scott C. Miller, Juan José Marugán Sánchez, Kristin D. Haslow, Jonathan Hall
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Patent number: 6951863Abstract: Pyridoarylphenyl oxazolidinone compounds of the formula: in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.Type: GrantFiled: February 6, 2002Date of Patent: October 4, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Steven D. Paget, Michele A. Weidner-Wells, Harvey M. Werblood
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Patent number: 6951868Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is any of: These compounds may be in the form of pharmaceutical salts or compositions, and racemic mixtures or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which ?7 is known to be involved.Type: GrantFiled: November 1, 2002Date of Patent: October 4, 2005Assignee: Pfizer Inc.Inventors: Daniel Patrick Walker, David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Vincent E. Groppi, Jr.
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Patent number: 6949651Abstract: The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula wherein A, B, X, Y, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating arthritis, inflammation, cancer and other disorders.Type: GrantFiled: August 5, 2003Date of Patent: September 27, 2005Assignee: Warner-Lambert CompanyInventor: Michael William Wilson
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Patent number: 6946473Abstract: Compounds of the formula which are useful in disease conditions mediated by TNF-?, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.Type: GrantFiled: March 17, 2003Date of Patent: September 20, 2005Assignee: Wyeth Holdings CorporationInventors: Jeremy I. Levin, James M. Chen, Xue-Mei Du, Jay D. Albright, Arie Zask
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Patent number: 6933306Abstract: Pharmacologically active compounds are provided as well as pharmaceutical compositions and methods for treating cancer; inflammation; an autoimmune, infectious or ocular disease; or age-related macular degeneration in a mammal.Type: GrantFiled: October 25, 2002Date of Patent: August 23, 2005Assignee: Darwin Discovery Ltd.Inventors: Duncan Robert Hannah, Hazel Joan Dyke, Robert John Watson, John Fraser Keily, Andrew Douglas Baxter
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Patent number: 6924280Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.Type: GrantFiled: February 21, 2003Date of Patent: August 2, 2005Assignee: Pfizer Inc.Inventors: Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
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Patent number: 6916810Abstract: The present invention relates to cyclic urea derivatives, their synthesis, and their use as ?v integrinreceptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors ?v?3 and/or ?v?5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, tumor growth and metastasis.Type: GrantFiled: September 7, 2001Date of Patent: July 12, 2005Assignee: Merck & Co., Inc.Inventors: John H. Hutchinson, Aiwen Li
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Patent number: 6911543Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which ?7 is known to be involved.Type: GrantFiled: October 1, 2002Date of Patent: June 28, 2005Assignee: Pfizer Inc.Inventors: Daniel Patrick Walker, David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Donn G. Wishka, Steven Charles Reitz
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Patent number: 6897223Abstract: The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula wherein A, B, X, Y, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating arthritis, inflammation, cancer and other disorders.Type: GrantFiled: August 5, 2003Date of Patent: May 24, 2005Assignee: Warner-Lambert CompanyInventor: Michael William Wilson
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Patent number: 6891043Abstract: Potent inhibitors of fatty acid amide hydrolase (FAAH) are constructed having K1's below 200 pM and activities 102-103 times more potent than the corresponding trifluoromethyl ketones. The potent inhibitors combine several features, viz.: 1.) an ?-keto heterocylic head group; 2.) a hydrocarbon linkage unit employing an optimal C12-C8 chain length; and 3.) a phenyl or other ?-unsaturation corresponding to the arachidonyl ?8,9/?11,12 and/or oleyl ?9,10 positions. A preferred ?-keto heterocylic head group is ?-keto N4 oxazolopyridine, with incorporation of a second weakly basic nitrogen. Fatty acid amide hydrolase is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors).Type: GrantFiled: October 8, 2002Date of Patent: May 10, 2005Assignee: The Scripps Research InstituteInventor: Dale L. Boger
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Patent number: 6867217Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: GrantFiled: May 18, 2000Date of Patent: March 15, 2005Assignee: Pharmacia CorporationInventors: Michael S. South, Qingping Zeng, Ashton T. Hamme, II, Melvin L. Rueppel
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Patent number: 6852739Abstract: The present invention describes novel nitrosated and/or nitrosylated proton pump inhibitor compounds, and novel compositions comprising at least one proton pump inhibitor compound that is optionally substituted with at least one NO and/or N02 group, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one nonsteroidal antiinflammatory drug, selective COX-2 inhibitor, antacid, bismuth-containing reagent, acid-degradable antibacterial compound, and mixtures thereof.Type: GrantFiled: February 25, 2000Date of Patent: February 8, 2005Assignee: Nitromed Inc.Inventors: David S. Garvey, L. Gordon Letts, Sang William Tam
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Patent number: 6849620Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is W0 is a bicyclic moiety and is These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals in which ?7 is known to be involved.Type: GrantFiled: October 17, 2002Date of Patent: February 1, 2005Assignee: Pfizer IncInventors: Daniel Patrick Walker, Eric Jon Jacobsen, David W. Piotrowski, Brad A. Acker, Donn G. Wishka, Jeffrey W. Corbett, Mark R. Rauckhorst, Vincent E. Groppi, Jr.
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Patent number: 6835731Abstract: Tertiary amines containing a multiplicity of heteroaromatic substituents are useful as chemokine receptor modulators.Type: GrantFiled: September 17, 2001Date of Patent: December 28, 2004Assignee: AnorMED, Inc.Inventors: Gary Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis, Rosaria Maria Di Fluri
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Publication number: 20040259908Abstract: The present invention relates to a 2-phenyl-3-heteroarylpropionic acid derivative or a salt thereof, and also relates to a pharmaceutical agent and a VLA-4 and/or LPAM-1 antagonist each of which contains the same as an active ingredient.Type: ApplicationFiled: July 27, 2004Publication date: December 23, 2004Inventors: Satoru Ikegami, Yoichiro Hoshina
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Patent number: 6833370Abstract: Heterocyclic substituted aminoazacyclic compounds of formula I Z—R3 I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: April 26, 2000Date of Patent: December 21, 2004Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Kevin B. Sippy, Jerome F. Daanen, Keith Brian Ryther, Jianguo Ji
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Publication number: 20040254199Abstract: Di- and trifluorosubstituted alkene compounds of formula I 1Type: ApplicationFiled: March 9, 2004Publication date: December 16, 2004Inventors: William Wakefield Wood, David Kuhn, Yulin Hu, Berhane Tecle
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Publication number: 20040254200Abstract: Compounds of formulae (1a) and (1b) are described: in which the dashed line represents an optional bond; A is a —N=atom or a —N(Rb)—, —C(Rb)═ or —C(Rb)(RC)— group; Ra, Rb and Rc is each independently a hydrogen atom or an optionally substituted C1-6alkyl group; X is an —O— or —S— atom or —NH— group or substituted N atom; each Y is independently a N atom or CH group or substituted C atom; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain L1 is a covalent bond or a linker atom or group; Cy1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Ar is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof; The compounds are potent inhibitors of p38 kinase and are use in the prophylaxis or treatment of p38 kinase medType: ApplicationFiled: July 20, 2004Publication date: December 16, 2004Inventors: Jeremy Martin Davis, Daniel Christopher Brookings, Barry John Langham
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Patent number: 6828330Abstract: The invention provides compounds of Formula I: wherein W0 is a bicyclic moiety and is These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful to treat diseases or conditions in which &agr;7 is known to be involved.Type: GrantFiled: June 6, 2002Date of Patent: December 7, 2004Assignee: Pharmacia & Upjohn CompanyInventors: Daniel Patrick Walker, Donn G. Wishka, David W. Piotrowski, Vincent E. Groppi, Jr.
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Publication number: 20040242884Abstract: The invention provides a compound of formula I: 1Type: ApplicationFiled: January 14, 2003Publication date: December 2, 2004Inventors: Scott D. Larsen, Paul May, Karen Romines, Mark E. Schnute, Steven P. Tanis, James A. Nieman, David John Anderson, Euibong J. Kim, Steven R. Turner
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Publication number: 20040242885Abstract: A process for the manufacture of a=:1-1,3-dihydrofuro[3,4-c]pyridine (I) 1 which is 4,7-disubstituted with a readily cleavable group (R) involves reacting a bis(3-R-substituted 2-propynyl) ether of the formula (R—C≡C—CH2)2O (II) with acetonitrile in the presence of a cobalt(I) complex catalyst of the formula XCo(I)Lig1/2 (III), wherein X signifies cyclopentadienyl, acetylcyclopentadienyl, indenyl or phenylborinato and Lig1/2 signifies the cyclooctadiene or norbornadiene ligand (Lig1) or two carbonyl or ethene ligands (Lig2), in an aliphatic, alicyclic or aromatic hydrocarbon solvent, or in excess acetonitrile as the reagent and simultaneously the solvent, or in water alone or in admixture with an ethereal co-solvent, or in a mixture of two or more of the aforementioned types of solvents, at a temperature in the range from about 0° C. to about 80° C.Type: ApplicationFiled: March 19, 2004Publication date: December 2, 2004Inventors: Werner Bonrath, Barbara Heller
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Publication number: 20040235867Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.Type: ApplicationFiled: January 23, 2004Publication date: November 25, 2004Inventors: Mark T. Bilodeau, Peter J. Manley, George D. Hartman