Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Bicyclo Ring System Patents (Class 546/120)
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Publication number: 20110034468Abstract: Disclosed are triazolopyridine compounds of Formula (I), including pharmaceutically acceptable salts thereof. Also, disclosed are methods of using the compound in the treatment of obesity, dyslipidemia, diabetes and atherosclerosis, and to pharmaceutical compositions comprising at least one compound of Formula (I) or a stereoisomer or pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 7, 2009Publication date: February 10, 2011Inventors: Yanting Huang, Chongqing Sun, R. Michael Lawrence, William R. Ewing, Huji Turdi
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Publication number: 20110028447Abstract: This invention relates to compounds, pharmaceutical compositions and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective amount of the compound of formula (I) wherein R1, R2 and R3 are as defined in this specification.Type: ApplicationFiled: February 26, 2009Publication date: February 3, 2011Inventors: Ingrid Price Buchler, Michael Joseph Hayes, Shridhar Gajanan Hegde, Susan Landis Hockerman, Darin Eugene Jones, Steven Wade Kortum, Joseph Gerace Rico, Ruth Elizabeth TenBrink, Kun Ken Wu
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Patent number: 7879873Abstract: Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.Type: GrantFiled: September 22, 2009Date of Patent: February 1, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Brian Nicholas Cook, Darren DiSalvo, Daniel Robert Fandrick, Christian Harcken, Daniel Kuzmich, Thomas Wai-Ho Lee, Pingrong Liu, John Lord, Can Mao, Jochen Neu, Brian Christopher Raudenbush, Hossein Razavi, Jonathan Timothy Reeves, Jinhua J. Song, Alan David Swinamer, Zhulin Tan
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Publication number: 20110021557Abstract: The present invention relates to deuterium-enriched pyridinone carboxamides and their derivatives of the formula I, and pharmaceutically acceptable salts thereof, are partial or full agonists of serotonin (5-Hydroxytryptamine or 5-HT4) receptor subtype 4, and are useful compounds for the prevention and treatment of Alzheimer's disease, cognitive and memory dysfunction, mild cognition impairment, memory decline, cognitive impairment associated with schizophrenia, cognitive impairment associated with age-related dementia or Alzheimer's disease, cognitive impairment associated with post-coronary bypass surgery, attention deficit hyperactivity disorder, speech improvement in autistic children, sleep apnea in Alzheimer's patients, irritable bowel syndrome, gastroesophageal reflux disease, Crobn's disease, emesis, nausea, vomiting, prokinesia, non-ulcer dyspepcia, anxiety, depression, pain, migraine, urinary incontinence, arterial fibrillation, arrhythmia, ischemic stroke, gastric emptying disorders, gastritis,Type: ApplicationFiled: July 26, 2010Publication date: January 27, 2011Inventor: Daljit Singh Dhanoa
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Publication number: 20100273776Abstract: Compounds and compositions are provided for treatment or amelioration of one or more symptoms of ?-synuclein toxicity, ?-synuclein mediated diseases or diseases in which ?-synuclein fibrils are a symptom or cause of the disease.Type: ApplicationFiled: March 29, 2007Publication date: October 28, 2010Applicants: FOLDRx PHARMACEUTICALS, INC, WHITEHEAD INSTITUTE FOR BIOMEDICAL RESEARCHInventors: Susan L. Lindquist, Tiago Outeiro, Richard Labaudinière, James Fleming, Christine Ellen Bulawa, Charlotte Weigel, Feng Liang, Sandeep Gupta, Amy Ripka
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Publication number: 20100267747Abstract: The invention provides N-cyclic sulfonamido compounds of Formula I wherein A, B, R1, R1a, R2, R2a, R3 and R3a are as described in the specification. Compounds of Formula I are useful in treating or preventing cognitive disorders, such as Alzheimer's disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I, methods of preparing compounds of formula I, and methods of treating cognitive disorders, such as Alzheimer's disease.Type: ApplicationFiled: June 8, 2010Publication date: October 21, 2010Applicant: Elan Pharmaceuticals, Inc.Inventors: Xiaocong Michael Ye, Albert W. Garofalo, Jacek J. Jagodzinski, Andrei W. Konradi, Christopher M. Semko, Jenifer L. Smith, Ying-zi Xu
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Publication number: 20100256356Abstract: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: January 26, 2010Publication date: October 7, 2010Applicants: Array BioPharma Inc., Genentech, Inc.Inventors: James F. Blake, Steven Armen Boyd, Jason De Meese, Kin Chiu Fong, John J. Gaudino, Tomas Kaplan, Allison L. Marlow, Jeongbeob Seo, Allen A. Thomas, Hongqi Tian, Frederick Cohen, Wendy B. Young
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Patent number: 7790726Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: August 14, 2006Date of Patent: September 7, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
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Patent number: 7772248Abstract: The present disclosure is directed to modulators of GABAA receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the medical use of such compounds for the treatment and/or management of sleep disorders and/or for providing a patient in need with a hypnotic, anxiolytic or anti-convulsive effect are described.Type: GrantFiled: May 30, 2007Date of Patent: August 10, 2010Assignee: Auspex Pharmaceuticals, Inc.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100197684Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: February 9, 2010Publication date: August 5, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki
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Publication number: 20100137288Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the ?7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: ApplicationFiled: February 5, 2010Publication date: June 3, 2010Inventors: Richard Schumacher, Mihaela Diana Danca, Jianguo Ma, Brian Herbert, True Minh Nguyen, Wenge Xie, Ashok Tehim
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Publication number: 20100130543Abstract: The present invention relates to new pyrazole carboxamide inhibitors of factor Xa, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: September 14, 2009Publication date: May 27, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Manoucherhr M. Shahbaz
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Patent number: 7723330Abstract: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: March 6, 2007Date of Patent: May 25, 2010Assignees: Array BioPharma Inc., Genentech, Inc.Inventors: James F. Blake, Steven Armen Boyd, Jason De Meese, Kin Chiu Fong, John J. Gaudino, Tomas Kaplan, Allison L. Marlow, Jeongbeob Seo, Allen A. Thomas, Hongqi Tian, Frederick Cohen, Wendy B. Young
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Patent number: 7709497Abstract: The invention provides 4-{[1-(aminocarbonyl)-4-piperidinyl]amino}-N-[(3,4-dimethylphenyl)methyl]-1-ethyl-1H-pyrazolo[3,4-b]pyridine-5-carboxamide, which is the compound of formula (I): or a salt thereof.Type: GrantFiled: March 15, 2005Date of Patent: May 4, 2010Assignee: Glaxo Group LimitedInventors: Siegfried Benjamin Christensen, IV, Caroline Mary Cook, Christopher David Edlin, Martin Redpath Johnson, Paul Spencer Jones, Mika Kristian Lindvall, Amyn Pyarali Sayani, Naimisha Trivedi, Lionel Trottet
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Publication number: 20100093724Abstract: Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.Type: ApplicationFiled: September 22, 2009Publication date: April 15, 2010Applicant: Boehringer Ingelheim International GmbHInventors: Brian Nicholas COOK, Darren DiSALVO, Daniel Robert FANDRICK, Christian HARCKEN, Daniel KUZMICH, Thomas Wai-Ho LEE, Pingrong LIU, John LORD, Can MAO, Jochen NEU, Brian Christopher RAUDENBUSH, Hossein RAZAVI, Jonathan Timothy REEVES, Jinhua J. SONG, Alan David SWINAMER, Zhulin TAN
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Publication number: 20100048611Abstract: The invention relates to novel tetrahydropyrrolopyridine, tetrahydropyrazolopyridine, tetrahydroimidazopyridine and tetrahydrotriazolopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disordersType: ApplicationFiled: May 26, 2007Publication date: February 25, 2010Applicant: Bayer Healthcare AGInventors: Susanne Röhrig, Mario Jeske, Elisabeth Perzborn
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Publication number: 20100035756Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: July 10, 2007Publication date: February 11, 2010Applicants: SYNGENTA LIMITED, SYNGENTA CROP PROTECTION, INC.Inventors: Christoph Luthy, Roger Graham Hall, Andrew Edmunds, Suzanna Riley, Martin Diggelmann
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Publication number: 20090317842Abstract: The present invention concerns compositions and methods for the treatment of neurodegenerative diseases in which the cognitive functions are altered, such as observed in Alzheimer's disease. More particularly, the invention presents a strategy for human clinical monitoring of the activity and/or effectiveness of neuroprotective treatments, based on biochemical assay of certain platelet parameters, and thus can be done by blood sampling. The invention also concerns methods, tools, constructions and compositions suitable for implementing these strategies.Type: ApplicationFiled: July 20, 2007Publication date: December 24, 2009Applicant: EXONHIT THERAPEUTICS SAInventors: Fabien Schweighoffer, Laurent Desire, Jérôme Bourdin
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Publication number: 20090306129Abstract: The present invention relates to phosphodiesterase (PDE) type IV selective inhibitors. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type IV selective inhibitors are provided. Prepared compounds correspond to structure XIV Formula (XIV).Type: ApplicationFiled: September 11, 2006Publication date: December 10, 2009Inventors: Venkata P. Palle, Sarala Balachandran, Nidhi Gupta, Vinayak Vasantrao Khairnar, Mandadapu Raghuramaiah, Abhijit Ray, Sunanda Ghose Dastidar
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Patent number: 7579472Abstract: A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds can be useful as factor Xa inhibitors.Type: GrantFiled: August 15, 2007Date of Patent: August 25, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Boguslaw M. Mudryk, Nicolas Cuniere, Dau-Ming Hsieh, Lucius Rossano, Jing Liang, Bang-Chi Chen, Huiping Zhang, Rulin Zhao, Bei Wang, Adrian David
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Publication number: 20090176825Abstract: The invention described herein relates to certain bicyclic heteroaromatic N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.Type: ApplicationFiled: May 8, 2007Publication date: July 9, 2009Inventors: Duke M. Fitch, Deping Chai
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Patent number: 7511058Abstract: Disclosed are compounds of the Formula III and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9 R10, and W are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: GrantFiled: April 24, 2006Date of Patent: March 31, 2009Assignee: Array BioPharma Inc.Inventors: T. Brian Hurley, Eli M. Wallace, Joseph P. Lyssikatos, James Blake
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Publication number: 20090076069Abstract: The present application describes deuterium-enriched apixaban, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 8, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090048226Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1? converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-? inducing factor-(IGIF), or interferon-?-(“IFN-?”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-? production and methods for treating interleukin-1, apoptosis-, and interferon-?-mediated diseases using the compounds and compositions of this invention.Type: ApplicationFiled: January 22, 2008Publication date: February 19, 2009Inventors: Marion W. Wannamaker, Guy W. Bemis, Paul S. Charifson, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, Keith P. Wilson, James W. Janetka, Robert J. Davies, Anne-Laure Grillot, Zhan Shi, Cornelia J. Forster
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Publication number: 20090012103Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: July 3, 2008Publication date: January 8, 2009Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki
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Patent number: 7465743Abstract: The invention relates to a compound of formula (I) or a salt thereof: wherein: R1 is Et, n-Pr, i-Pr, C2fluoroalkyl, or —CH2CH2OH; R2 is H, Me, Et, n-Pr, i-Pr, C1-2fluoroalkyl, cyclopropyl or (cyclopropyl)methyl-; and NHR3 has the sub-formula (nhr3): wherein R3a is methyl or ethyl; R3b is H, methyl or ethyl; R3c is H, methyl or ethyl, R3d is H, methyl or ethyl, and R3e is H or methyl, provided that: (a) R3b is methyl or ethyl; and/or (b) R3c and R3d are independently methyl or ethyl; and provided that: (c) when R3c is ethyl and/or when R3d is ethyl and/or when R3e is methyl, then: R3a is methyl and/or R3b is hydrogen or methyl. These compounds are PDE4 inhibitors.Type: GrantFiled: March 15, 2005Date of Patent: December 16, 2008Assignee: Glaxo Group LimitedInventors: Diane Mary Coe, Caroline Mary Cook, Anthony William James Cooper, Christopher David Edlin, Julie Nicole Hamblin, Martin Redpath Johnson, Paul Spencer Jones, Mika Kristian Lindvall, Charlotte Jane Mitchell, Alison Judith Redgrave, John Edward Robinson
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Patent number: 7459451Abstract: The invention relates to compound of the formula (I) or its salt, in which R1, R2, R3 and R4 are as defined in the description, their use of as medicament, the process for their preparation and use for the treatment of PDE-IV or TNF-? mediated diseases.Type: GrantFiled: July 1, 2005Date of Patent: December 2, 2008Assignee: Astellas Pharma Inc.Inventors: Yoshito Abe, Kazuhiko Ohne, Kentaro Sato, Makoto Inoue, Mitsuaki Okumura
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Publication number: 20080287434Abstract: The invention relates to a compound of the general formula (I), as defined herein which is useful for the treatment of a pathology in a patient wherein a CCR3 receptor plays a role in the development of the pathology, and pharmaceutical preparations containing such compound. The invention is also directed to a process for preparing the compound of the general formula (I), and intermediate useful in the preparation.Type: ApplicationFiled: March 19, 2008Publication date: November 20, 2008Applicant: SANOFI-AVENTISInventors: Agnes PAPPNE BEHR, Zoltan KAPUI, Peter ARANYI, Sandor BATORI, Veronika BARTANE BODOR, Lajos T. NAGY, Mihalyne T. Santa, Marton VARGA, Gyorgy FERENCZY, Endre MIKUS, Katalin URBAN-SZABO, Judit VARGANE SZEREDI, Erzsebet WALCZ, Edit SUSAN
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Publication number: 20080287448Abstract: The invention relates to diacyl indazole derivatives of general formulae (I) or (II) and to the pharmaceutically acceptable salts thereof: Wherein X, R1 and R2 are as defined herein. The invention also relates to the use of these compounds as pharmaceutical products.Type: ApplicationFiled: April 8, 2008Publication date: November 20, 2008Applicant: SANOFI-AVENTISInventors: Gerhard Zoller, Stefan Petry, Gunter Muller, Hubert Heuer, Norbert Tennagels
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Patent number: 7449585Abstract: Compounds of formula (I), which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).Type: GrantFiled: November 12, 2004Date of Patent: November 11, 2008Assignee: Merck Sharp & Dohme Ltd.Inventors: Frank Burkamp, Stephen Robert Fletcher
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Publication number: 20080275052Abstract: A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.Type: ApplicationFiled: November 15, 2007Publication date: November 6, 2008Inventors: T.G. Murali Dhar, Stephen T. Wrobleski
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Publication number: 20080275078Abstract: The invention provides a compound of formula (I) or a salt thereof: wherein: R1 is C1-3alkyl, C1-3fluoroalkyl, or —CH2CH2OH; R2 is hydrogen, methyl or C1fluoroalkyl; R3 is of sub-formula (aa) or (bb): wherein Y is NCONH2 and n1 is 0 or 1; R4 is H; and R5 is a group of the sub-formula (x), (y), (y1) or (z): These compounds are PDE4 inhibitors.Type: ApplicationFiled: March 15, 2005Publication date: November 6, 2008Applicant: Glaxo Group LimitedInventors: Caroline Mary Cook, Michael Dennis Dowle, Christopher David Edlin, Martin Redpath Johnson, Paul Spencer Jones, Mika Kristian Lindvall, Naimisha Trivedi, Alison Judith Redgrave
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Patent number: 7435820Abstract: Substituted tetrahydro-1H-pyrazolo[3,4-c]pyridines, compositions comprising them and use. The present invention relates in particular to novel substituted tetrahydro-1H-pyrazolo[3,4-c]pyridines having therapeutic activity, which can be used in particular in oncology.Type: GrantFiled: May 23, 2006Date of Patent: October 14, 2008Assignee: Aventis Pharma S.A.Inventors: Fabienne Thompson, Catherine Souaille, Fabrice Viviani, Michel Tabart, Patrick Mailliet, Teresa Damiano, Marie-Pierre Cherrier, Francois Clerc, Frank Halley, Herve Bouchard, Laurence Gauzy-Lazo, Bernard Baudoin
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Patent number: 7435821Abstract: A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds can be useful as factor Xa inhibitors.Type: GrantFiled: August 15, 2007Date of Patent: October 14, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Boguslaw M. Mudryk, Nicolas Cuniere, Dau-Ming Hsieh, Lucius Rossano, Jing Liang, Bang-Chi Chen, Huiping Zhang, Rulin Zhao, Bei Wang, Adrian David
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Publication number: 20080227777Abstract: The invention relates to 6-amido substituted pyrazolopyridine derivatives of the formula (I) useful as inhibitors of beta-adrenergic receptor kinase 1 (?ARK-1), compositions containing such compounds and their use for the treatment and prevention of chronic heart failure, hypertension, myocardial ischemia and hepatitis C virus (HCV) infections, and for the prevention of opiate addiction.Type: ApplicationFiled: December 20, 2007Publication date: September 18, 2008Applicant: SANOFI-AVENTISInventors: Henning STEINHAGEN, Jochen HUBER, Kurt RITTER, Bernard PIRARD, Kirsten BJERGARDE, Marcel PATEK, Martin SMRCINA, Linli WEI
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Patent number: 7417041Abstract: Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-? signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.Type: GrantFiled: February 20, 2004Date of Patent: August 26, 2008Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Laura C. Blumberg, Michael J. Munchhof, Andrei Shavnya
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Publication number: 20080194588Abstract: The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2;Type: ApplicationFiled: December 28, 2007Publication date: August 14, 2008Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20080188491Abstract: The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2.Type: ApplicationFiled: December 28, 2007Publication date: August 7, 2008Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20080175914Abstract: The invention relates to a compound of formula (I) or a salt thereof: wherein: R1 is C1-4alkyl, C1-3fluoroalkyl, —CH2CH2OH or —CH2CH2CO2C1-2alkyl; R2 is a hydrogen atom (H), methyl or C1fluoroalkyl; R3 is optionally substituted C3-8cycloalkyl or optionally substituted mono-unsaturated-C5-7cycloalkenyl or an optionally substituted heterocyclic group of sub-formula (aa), (bb) or (cc); in which n1 and n2 independently are 1 or 2; and in which Y is O, S, SO2, or NR10; or R3 is a bicyclic group (dd) or (ee): and wherein X is NR4R5 or OR5a. The compounds are phosphodiesterase (PDE) inhibitors, in particular PDE4 inhibitors. Also provided is the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment and/or prophylaxis of an inflammatory and/or allergic disease in a mammal such as a human, for example chronic obstructive pulmonary disease (COPD), asthma, or allergic rhinitis.Type: ApplicationFiled: January 14, 2008Publication date: July 24, 2008Inventors: David George ALLEN, Diane Mary Coe, Caroline Mary Cook, Michael Dennis Dowle, Christopher David Edlin, Julie Nicole Hamblin, Martin Redpath Johnson, Paul Spencer Jones, Richard Graham Knowles, Mika Kristian Lindvall, Charlotte Jane Mitchell, Alison Judith Redgrave, Peter Ward
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Publication number: 20080167306Abstract: A compound of the following formula (1), or its prodrug or pharmaceutically acceptable salt thereof, being useful as a diabetic medicine or preventive, or blood sugar regulator, or therapeutic agent for hyperlipemia, etc. wherein the ring Z is an optionally substituted heteroaryl, W4 is a single bond, lower alkylene, etc., Ar2 is an optionally substituted aryl, etc., W3 is a single bond, lower alkylene, etc., Ar1 is an optionally substituted arylene, etc., each of W1 and W2 is an optionally substituted lower alkylene, etc., and R1 is carboxyl, an alkoxycarbonyl.Type: ApplicationFiled: January 12, 2006Publication date: July 10, 2008Inventors: Yoko Takahashi, Ryu Nagata, Kantaro Ushiroda
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Patent number: 7396932Abstract: A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds can be useful as factor Xa inhibitors.Type: GrantFiled: September 26, 2005Date of Patent: July 8, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Rafael Shapiro, Lucius T Rossano, Boguslaw M Mudryk, Nicolas Cuniere, Matthew Oberholzer, Huiping Zhang, Bang-Chi Chen
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Patent number: 7388096Abstract: The instant invention provides crystalline forms of 1-(3-chlorophenyl)-7-oxo-6-[4-(2-oxo-1 (2H)pyridinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide and its solvates thereof; processes for the production of such crystalline forms; pharmaceutical compositions comprising such crystalline forms; and methods of treating thromboembolic disorders with such crystalline forms or such pharmaceutical compositions.Type: GrantFiled: September 26, 2005Date of Patent: June 17, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Margaret M. Gleeson, Gary McGeorge, Bang-Chi Chen, Huiping Zhang, Mary F. Malley, John D. DiMarco, Denette K. Murphy, Xiaotian Yin, Steven R. Fabian, Jasmine M. Gupta
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Publication number: 20080132536Abstract: The invention provides a compound of formula (I) or a salt thereof: wherein Ar has the sub-formula (x) or (z): and wherein R3 is optionally substituted C3-8cycloalkyl, optionally substituted C5-7cycloalkenyl, an optionally substituted heterocyclic group (aa), (bb) or (cc), or a bicyclic group (ee); and wherein R4 is H, C1-3alkyl, C1-2fluoroalkyl, cyclopropyl, —CH2OR4a, —CH(Me)OR4a, or —CH2CH2OR4a; and R5 is inter alia H, C1-8alkyl, C1-3fluoroalkyl, C3-8cycloalkyl, certain substituted alkyl groups, —(CH2)n13-Het, or optionally substituted phenyl or —CH2-Ph; or R4 and R5 taken together are —(CH2)p1— or —(CH2)p3—X5—(CH2)p4—; provided that at least one of R4 and R5 is not a hydrogen atom (H). The invention also provides the use of the compounds as inhibitors of phosphodiesterase type IV (PDE4) and/or for the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, allergic rhinitis or atopic dermatitis.Type: ApplicationFiled: January 30, 2008Publication date: June 5, 2008Inventors: David George Allen, Diane Mary Coe, Caroline Mary Cook, Michael Dennis Dowle, Christopher David Edlin, Julie Nicole Hamblin, Martin Redpath Johnson, Paul Spencer Jones, Mika Kristian Lindvall, Charlotte Jane Mitchell, Alison Judith Redgrave, John Edward Robinson, Naimisha Trivedi
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Patent number: 7371761Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4-P-M-M4I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: January 16, 2007Date of Patent: May 13, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Donald J. P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y. S. Lam, Stephanie L Koch
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Patent number: 7371864Abstract: The instant invention provides crystalline forms of 3-(1-hydroxy-1-methyl-ethyl)-1-(4-methoxy-phenyl)-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one and its solvates thereof; processes for the production of such crystalline forms; pharmaceutical compositions comprising such crystalline forms; and methods of treating thromboembolic disorders with such crystalline forms or such pharmaceutical compositions.Type: GrantFiled: December 14, 2005Date of Patent: May 13, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Michael J. Orwat, Mary F. Malley, Roxana Schlam, Steven R. Fabian, Bing-Shiou Yang, Victor W. Rosso
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Patent number: 7354929Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described hereinType: GrantFiled: October 4, 2006Date of Patent: April 8, 2008Assignee: Pfizer Inc.Inventors: Philip A. Carpino, David A. Griffith
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Patent number: 7348324Abstract: A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1 and R2 may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.Type: GrantFiled: October 18, 2002Date of Patent: March 25, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Shinichi Imamura, Shohei Hashiguchi, Taeko Hattori, Osamu Nishimura, Naoyuki Kanzaki, Masanori Baba, Yoshihiro Sugihara
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Patent number: 7332506Abstract: A compound represented by the formula I: wherein A represents the following heterocycles: and R1-9 are as defined herein, a composition containing this compound and methods for treating disorders of the serotonin-affected neurological systems utilizing such a compound or composition.Type: GrantFiled: August 28, 2006Date of Patent: February 19, 2008Assignee: WyethInventors: Aranapakam M. Venkatesan, Jamie M. Davis, Yansong Gu
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Publication number: 20070281965Abstract: The present disclosure is directed to modulators of GABAA receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the medical use of such compounds for the treatment and/or management of sleep disorders and/or for providing a patient in need with a hypnotic, anxiolytic or anti-convulsive effect are described.Type: ApplicationFiled: May 30, 2007Publication date: December 6, 2007Applicant: Auspex Pharmaceuticals, Inc.Inventors: Thomas G. GANT, Sepehr SARSHAR
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Patent number: 7304157Abstract: A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds can be useful as factor Xa inhibitors.Type: GrantFiled: September 26, 2005Date of Patent: December 4, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Boguslaw M. Mudryk, Nicolas Cuniere, Dau-Ming Hsieh, Lucius Rossano, Jing Liang, Bang-Chi Chen, Huiping Zhang, Rulin Zhao, Bei Wang, Adrian David