Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/141)
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Patent number: 7615565Abstract: VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridinamides, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis, as well as intermediate products for the production of the compounds are described. The compounds according to the invention can be used as or in the case of tumor or metastasis growth, psoriasis, Kaposi's sarcoma, restenosis, such as, e.g.Type: GrantFiled: September 22, 2006Date of Patent: November 10, 2009Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Andreas Huth, Ludwig Zorn, Martin Kruger, Stuat Ince, Karl-Heinz Thierauch, Andreas Menrad, Martin Haberey, Holger Hess-Stumpp
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Publication number: 20090274656Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: ApplicationFiled: September 2, 2008Publication date: November 5, 2009Inventors: Alan Xiangdong Wang, Li-Qiang Sun, Sing-Yuen Sit, Ny Sin, Paul Michael Scola, Yan Chen
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Publication number: 20090274652Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: ApplicationFiled: April 6, 2009Publication date: November 5, 2009Inventors: Ny Sin, Brian Lee Venables, Paul Michael Scola, Alan Xiangdong Wang
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Patent number: 7612091Abstract: The present invention provides a compound of formula I: wherein: X is —OR1 or —N(R5)2, Y is halo, trifluorophenoxy, or tetrafluorophenoxy; R1 is: C1-6 straight chained or branched alkyl, alkenyl, or alkynyl, wherein the alkyl, alkenyl, or alkynyl is optionally substituted with optionally substituted aryl, CF3, Cl, F, OMe, OEt, OCF3, CN, or NMe2; C1-6 cycloalkyl, wherein 1-2 carbon atoms in the cycloalkyl is optionally replaced with —O— or —NR5—; R2 is C1-6 straight chained or branched alkyl; R3 is hydrogen, halo, OCF3, CN, or CF3; R4 is hydrogen, halo, OCF3, CN, or CF3; and each R5 is independently H, C1-6 straight chained or branched alkyl, aryl, —O—C1-6 straight chained or branched alkyl, or —O-aryl. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated disease, particularly in the central nervous system.Type: GrantFiled: December 22, 2003Date of Patent: November 3, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Michael Mortimore, John R. Studley
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Publication number: 20090270362Abstract: In one aspect, the invention relates to bicyclic MGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: October 31, 2008Publication date: October 29, 2009Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
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Publication number: 20090264403Abstract: The invention relates to azacyclyl-substituted aryldihydroisoquinolinones and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one azacyclyl-substituted aryldihydroisoquinolinone of the invention or its derivative, and the use of the azacyclyl-substituted aryidihydroisoquinolinones of the invention and their derivatives as MCH antagonists.Type: ApplicationFiled: August 14, 2008Publication date: October 22, 2009Applicant: SANOFI-AVENTISInventors: Lothar SCHWINK, Siegfried STENGELIN, Matthias GOSSEL, Gerhard HESSLER, Torsten HAACK, Petra LENNIG
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Patent number: 7605265Abstract: Novel heterodimers of tetrahydroacridines and tetrahydroquinolinones are disclosed. The heterodimers are capable of acting as both acetylcholinesterase inhibitors and N-methyl-D-aspartate (NMDA) receptor antagonists. The heterodimers may be used to improve cognitive defects via treatment or prevention in both humans and non-humans.Type: GrantFiled: January 22, 2007Date of Patent: October 20, 2009Assignee: Biotechnology Research Corporation Ltd.Inventors: Nancy Y Ip, Fanny Chui Fun Ip, Yueqing Hu, Yifan Han, Sookja Kim Chung
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Publication number: 20090221575Abstract: The present invention is related to sulfonamide derivatives of Formula (Ia) where the groups are as defined in the description, and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: ApplicationFiled: October 24, 2006Publication date: September 3, 2009Applicant: Laboratoires Serono SAInventors: Patrick Gerber, Dominique Swinnen, Agnes Bombrun
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Patent number: 7582638Abstract: The present invention provides kinase inhibitors of Formula (I) wherein R1, R2, and X are as described herein, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 23, 2006Date of Patent: September 1, 2009Assignee: Eli Lilly and CompanyInventors: Alfonso De Dios, Cristina Garcia-Paredes, Beatriz López de Uralde Garmendia, Mary Margaret Mader, Mark Andrew Pobanz, Chuan Shih, Boyu Zhong
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Patent number: 7572913Abstract: Substituted piperidine compounds represented by the structure I are provided, wherein each of R1a, R1b, R1c, R1d, R1e, R1f, R1g, R1h, R2, R2A, R3, R4, A, X, a, x and n is as defined in the specification. Substituted piperidine compounds of structure I may permeate or penetrate across a nerve cell membrane into the interior of a nerve cell, may inhibit intracellular Rho kinase enzyme found in nerve cells in mammals, and may find utility in repair of damaged nerves in the central and peripheral nervous system of such mammals. These compounds may induce the regeneration or growth of neurites in mammalian nerve cells and may thereby induce regeneration of damaged or diseased nerve tissue. These compounds also find additional utility as antagonists of the enzyme Rho kinase in treatment of disease states in which Rho kinase is implicated.Type: GrantFiled: February 24, 2005Date of Patent: August 11, 2009Assignee: Bioaxone Therapeutique Inc.Inventors: Lisa McKerracher, Eryk Thouin, William Lubell, Robert Snow, Karine Gingras
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Patent number: 7572809Abstract: The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of such compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: December 12, 2006Date of Patent: August 11, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Li Chen, Guy Georges, Alfred Mertens, Xihan Wu
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Publication number: 20090182007Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of aldosterone synthase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, renal failure, in particular, chronic renal failure, restenosis, atherosderosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, increased formation of collagen, cardiac fibrosis and remodeling following hypertension and endothelial dysfunction. Finally, the present invention also provides a pharmaceutical composition.Type: ApplicationFiled: March 27, 2007Publication date: July 16, 2009Inventors: Christopher Adams, Julien Papillon, Gary Michael Ksander
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Publication number: 20090170838Abstract: Bicycloheteroaryl compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: July 16, 2008Publication date: July 2, 2009Inventors: Michael G. Kelly, John Kincaid
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Publication number: 20090171090Abstract: It is an object of the present invention to provide 2-iminocarboxylic acid derivatives, and a practically suitable industrial method for producing benzazepinones in a short process under mild conditions. The present invention provides a method for producing a benzazepinone or a salt thereof, which comprises opening a ring of an isoquinoline derivative and subsequently converting the thus generated amine into a benzazepinone through lactamization reaction.Type: ApplicationFiled: January 31, 2007Publication date: July 2, 2009Applicant: API CORPORATIONInventor: Hisatoshi Uehara
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Patent number: 7553852Abstract: The present invention relates to compounds of formula I: useful as inhibitors of caspases. The present invention also provides pharmaceutically acceptable compositions comprising said compounds, processes for preparing the compounds, and methods of using the compounds and compositions in the treatment of various diseases, conditions, or disorders.Type: GrantFiled: June 27, 2003Date of Patent: June 30, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Ronald Knegtel, Michael Mortimore, John Studley, David Millan
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Publication number: 20090163497Abstract: The present invention provides compounds of general formula (I) or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.Type: ApplicationFiled: October 26, 2006Publication date: June 25, 2009Inventors: Amy M. Elder, Shomir Ghosh, Sian Griffiths, Prakash Raman, Francois Soucy, Kevin Sprott, Qing Ye
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Publication number: 20090156823Abstract: (S)-1-(4-Chloro-5-isoquinolinesulfonyl)-3-(methylamino)pyrrolidine monohydrochloride and a crystal thereof, and a crystal of the aforementioned monohydrochloride having a major peak or peaks at one or more positions selected from the group consisting of positions where 2?s are about 13.9°, 21.5°, 21.7°, 22.4°, 22.8°, 24.5° and 35.0° in a powder X-ray diffraction spectrum, which have excellent properties as active ingredient of a medicament for prophylactic and/or therapeutic treatment of glaucoma and the like.Type: ApplicationFiled: July 1, 2008Publication date: June 18, 2009Applicant: Asahi Kasei Pharma CorporationInventors: Hitoshi Kida, Koki Matsubara, Shunsuke Kaneko, Yoshihito Kanzawa
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Publication number: 20090143402Abstract: Isoquinolone derivatives of the general formula are provided. The compounds are NK3 antagonists and useful for the treatment of e.g. psychosis and schizophrenia.Type: ApplicationFiled: April 11, 2008Publication date: June 4, 2009Applicant: H. LUNDBECK A/SInventors: Klaus Baek Simonsen, Jan Kehler, Karsten Juhl, Nikolay Khanzhin, Soren Moller Nielsen
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Publication number: 20090131456Abstract: This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors. These compounds have the general formula I: where R1, R2, and R3 are as described herein, Ring A contains zero to two double bonds, each X is independently selected from nitrogen or carbon, at least one X in Ring A is a nitrogen, Ring A is optionally substituted as described, and may be fused to a saturated or unsaturated five to seven membered ring containing zero to three heteroatoms, and provided that when X3 is a carbon, a substituent on X3 is attached by an atom other than nitrogen.Type: ApplicationFiled: January 26, 2009Publication date: May 21, 2009Inventors: Julian M.C. Golec, Paul S. Charifson, Jean-Damien Charrier, Hayley Binch
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Publication number: 20090131473Abstract: The present invention relates generally to novel 2-(aryloxy)acetamides of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables W, Y, Z, R7, R8, and R9 are as defined herein. These compounds are selective inhibitors of the serine protease coagulation factor VIIa which can be used as medicaments.Type: ApplicationFiled: March 8, 2007Publication date: May 21, 2009Inventors: Alexandra A. Nirschl, Xiaojun Zhang
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Publication number: 20090093518Abstract: The invention relates to 6-piperidinyl-substituted isoquinolone derivatives of the formula (I) or isoquinoline derivatives of the formula (I?) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.Type: ApplicationFiled: January 25, 2008Publication date: April 9, 2009Applicant: SANOFI-AVENTISInventors: Oliver Plettenburg, Armin Hofmeister, Dieter Kadereit, Joachim Brendel, Matthias Loehn
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Publication number: 20090076276Abstract: The present invention relates to an isoquinoline compound represented by the following formula (I), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease caused by hyperreactivity of poly(ADP-ribose)polymerase, containing the compound, and a poly(ADP-ribose)polymerase inhibitor containing the compound. In addition, this compound is useful as an agent for the prophylaxis and/or treatment of cerebral infarction, particularly as an agent for the prophylaxis and/or treatment of acute cerebral infarction. Furthermore, this compound is useful as a prophylactic and/or therapeutic agent that improves neurological symptoms associated with cerebral infarction, particularly acute cerebral infarction. wherein the symbols are the same as defined in the description.Type: ApplicationFiled: November 3, 2008Publication date: March 19, 2009Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Masakazu FUJIO, Hiroyuki SATOH, Shinya INOUE, Toshifumi MATSUMOTO, Yasuhiro EGI
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Publication number: 20090075975Abstract: Arylsulfonamide compounds of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:Type: ApplicationFiled: November 24, 2008Publication date: March 19, 2009Inventors: Michael R. DeGraffenreid, JAY P. POWERS, Daqing Sun, Xuelei Yan
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Publication number: 20090069300Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.Type: ApplicationFiled: September 11, 2008Publication date: March 12, 2009Applicant: WyethInventors: Dahui Zhou, Jonathan Laird Gross, Albert Jean Robichaud
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Publication number: 20090069370Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.Type: ApplicationFiled: September 11, 2008Publication date: March 12, 2009Applicant: WyethInventors: Dahui Zhou, Jonathan Laird Gross, Albert Jean Robichaud
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Publication number: 20090068144Abstract: The present invention provides a compound selected from compounds of formula I as ligand binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy. Compounds of formula (I) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events, heart valvular degenerative disease Moreover, compounds of formula (I) can be used to decrease the side effects from cytotoxic cancer agents and to treat viral infections.Type: ApplicationFiled: March 17, 2006Publication date: March 12, 2009Inventors: Lutz Weber, Vladimir Khazak, Gunther Ross, Cotic Kalinski, Chritoph Burdack
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Patent number: 7501412Abstract: The present invention relates to an isoquinoline compound represented by the following formula (I) or (II), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease caused by hyperreactivity of poly(ADP-ribose)polymerase, containing the compound, and a poly(ADP-ribose)polymerase inhibitor containing the compound. In addition, this compound is useful as an agent for the prophylaxis and/or treatment of cerebral infarction, particularly as an agent for the prophylaxis and/or treatment of acute cerebral infarction.Type: GrantFiled: November 21, 2003Date of Patent: March 10, 2009Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Masakazu Fujio, Hiroyuki Satoh, Shinya Inoue, Toshifumi Matsumoto, Yasuhiro Egi, Taichi Takahashi
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Publication number: 20090054434Abstract: The present invention is directed to certain isoquinolin-1(2H)-one compounds, useful as PDE10 inhibitors, having the formula: where R1, R2, R3, R4 and R5 are as defined herein, pharmaceutical compositions containing such compounds and processes for preparing such compounds. The invention is also directed to methods of treating diseases mediated by PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: August 22, 2008Publication date: February 26, 2009Applicants: Amgen Inc., Memory Pharmaceuticals Corp.Inventors: Essa Hu, Roxanne Kunz, Ning Chen, Ruiping Liu
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Publication number: 20090030195Abstract: The present invention provides a compound having high antitumor activity, which is useful for therapeutic and preventive agents effective for proliferative diseases such as cancer; a production method thereof; an intermediate compound useful for such production; and a pharmaceutical composition comprising such a compound. The present invention provides a compound represented by the formula (1): wherein X represents an aryl group or heteroaryl group which may be substituted, Cy represents a 4- to 7-membered monocyclic heterocyclic ring or a 8- to 10-membered condensed heterocyclic ring which may be substituted, and Z represents O, S, or NRa; or a prodrug thereof; or a pharmaceutically acceptable salt thereof; and a pharmaceutical and a pharmaceutical composition which comprise the compound.Type: ApplicationFiled: February 22, 2006Publication date: January 29, 2009Applicant: Chugai Seiyaku Kabushiki KaishaInventors: Kazuo Hattori, Satoshi Niizuma, Miyako Masubuchi, Kohei Koyama, Osamu Kondoh, Toshiyuki Tsukaguchi, Takehiro Okada
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Publication number: 20090023746Abstract: The present invention relates to isoquinolinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: April 4, 2008Publication date: January 22, 2009Applicant: AstraZeneca ABInventors: Matthew Hallam, Barrie Martin, Piotr Raubo, Bryan Roberts, Stephen St-Gallay, Paul Willis
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Publication number: 20090017112Abstract: Provided are compounds useful for treating diseases associated with a cerebral accumulation of Alzheimer's amyloid, such as Alzheimer's disease. Also provided are methods of treating or reducing the risk of developing ?-amyloid production, ?-amyloid deposition, ?-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) and microgliosis associated with cerebral accumulation of Alzheimer's amyloid by administering therapeutically effective amounts of the compounds. Further provided are methods for diagnosing diseases associated with cerebral accumulation of Alzheimer's amyloid in animals or humans by administering diagnostically effective amounts of the compounds.Type: ApplicationFiled: February 28, 2007Publication date: January 15, 2009Applicant: ROSKAMP RESEARCH LLCInventors: Michael J. Mullan, Daniel Paris, Pancham Bakshi
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Publication number: 20090012097Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families.Type: ApplicationFiled: January 25, 2007Publication date: January 8, 2009Applicant: IRM LLCInventors: Robert Epple, Christopher Cow
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Patent number: 7459465Abstract: The present invention relates to an isoquinoline compound represented by the following formula (I), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease caused by hyperreactivity of poly(ADP-ribose)polymerase, containing the compound, and a poly(ADP-ribose)polymerase inhibitor containing the compound. In addition, this compound is useful as an agent for the prophylaxis and/or treatment of cerebral infarction, particularly as an agent for the prophylaxis and/or treatment of acute cerebral infarction. Furthermore, this compound is useful as a prophylactic and/or therapeutic agent that improves neurological symptoms associated with cerebral infarction, particularly acute cerebral infarction. wherein the symbols are the same as defined in the description.Type: GrantFiled: March 19, 2007Date of Patent: December 2, 2008Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Masakazu Fujio, Hiroyuki Satoh, Shinya Inoue, Toshifumi Matsumoto, Yasuhiro Egi
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Publication number: 20080293709Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: November 13, 2006Publication date: November 27, 2008Applicant: AstraZeneca ABInventors: Jeffrey Albert, Gianni Chessari, Miles Stuart Congreve, Phil Edwards, Christopher Murray, Sahil Patel, Mark Sylvester
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Patent number: 7456183Abstract: Compounds having the general structure I are provided. X and Y are independently selected from the group consisting of CH2, N, NR9, C?O, C?S, S?O, SO2, S, O, (CR6R7)n, C(?O)—(CR6R7)n, and C(?S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of (formula I) and L is selected from the group consisting of N, O, S?O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r2) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.Type: GrantFiled: April 8, 2002Date of Patent: November 25, 2008Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: Daniel Chu, Rustum Boyce, David Duhl, Bryan Chang
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Publication number: 20080287415Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: March 7, 2008Publication date: November 20, 2008Inventors: Michael G. Kelly, John Kincaid, Yunfeng Fang, Yeyu Cao, Carl Kaub, Sumithra Gowlugari, Zhan Wang
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Publication number: 20080275056Abstract: The present invention provides kinase inhibitors of Formula (I) wherein R1, R2, and X are as described herein, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 23, 2006Publication date: November 6, 2008Inventors: Alfonso De Dios, Cristina Garcia-Paredes, Beatriz Lopez Uralde Garmendia, Mary Margaret Mader, Mark Andrew Pobanz, Chuan Shih, Boyu Zhong
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Patent number: 7442710Abstract: The present invention relates to compounds of general formula IA or IB wherein X1 and X2 are each independently N or C—R? and R1, R2,R3, R4, R5, and R6 are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds can be used for the treatment of diseases related to the glycine transporter inhibitor, such as schizophrenia and Alzheimer's disease.Type: GrantFiled: January 24, 2006Date of Patent: October 28, 2008Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
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Patent number: 7439242Abstract: Modulators of PPAR? activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.Type: GrantFiled: April 15, 2002Date of Patent: October 21, 2008Assignee: Amgen Inc.Inventors: Jonathan B. Houze, Lawrence R. McGee, Steven Marc Rubenstein
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Publication number: 20080242699Abstract: The invention relates to 6-cyclohexylamine-substituted isoquinolone derivatives of the formula (I) or isoquinoline derivatives of the formula (I?) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.Type: ApplicationFiled: January 25, 2008Publication date: October 2, 2008Applicant: SANOFI-AVENTISInventors: Oliver PLETTENBURG, Armin HOFMEISTER, Dieter KADEREIT, Joachim BRENDEL, Matthias LOEHN
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Publication number: 20080227778Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: ApplicationFiled: September 17, 2004Publication date: September 18, 2008Inventors: Christopher J. Dinsmore, Jeffrey M. Bergman, Charles J. McIntyre, David A. Claremon
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Patent number: 7425563Abstract: The invention provides 4-substituted aryl-5-hydroxyisoquinolinone derivatives and their pharmacologically acceptable addition salts with excellent inhibitory effect on poly (ADP-ribose) synthetase. 4-Substituted aryl-5-hydroxyisoquinolinone derivatives, represented by a general formula (1) and their pharmacologically acceptable addition salts.Type: GrantFiled: July 23, 2003Date of Patent: September 16, 2008Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Futoshi Shiga, Takahiro Kanda, Tetsuya Kimura, Yasuo Takano, Jyunichi Ishiyama, Tomoyuki Kawai, Tsuyoshi Anraku, Kumi Ishikawa
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Publication number: 20080207685Abstract: The present invention is directed to a compound of formula (I), or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomer thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.Type: ApplicationFiled: November 16, 2004Publication date: August 28, 2008Applicant: Eli Lilly And CompanyInventors: James Robert Henry, Yihong Li, Jeffrey Michael Scheryantz, Alan M. Warshawsky
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Publication number: 20080207596Abstract: The invention concerns a compound of formula (I) or pharmaceutically-acceptable salts thereof wherein R1, R2, R3, R4, R5 and m are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: ApplicationFiled: June 19, 2007Publication date: August 28, 2008Inventors: Barrie Martin, Paul Willis
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Publication number: 20080188467Abstract: The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.Type: ApplicationFiled: February 1, 2007Publication date: August 7, 2008Inventors: Norman C.W. Wong, Joseph E.L. Tucker, Henrik C. Hansen, Fabrizio S. Chiacchia, David McCaffrey
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Patent number: 7405227Abstract: Methods of treating ovarian cancer, endometrium cancer, cervical cancer, pancreatic cancer, bladder cancer, eve cancer, central nervous system cancer, thyroid cancer and lung cancer are disclosed. Specifically disclosed are methods of treating ovarian adenocarcinoma that has migrated into the abdominal cavity, a transitional cell carcinoma of the bladder, an epithelioid carcinoma in a pancreatic duct, an adenocarcinoma in a pancreatic duct, an adenocarcinoma in the cervical epithelium. The methods comprise administering to a patient a therapeutically effective amount of a compound of formula (Ia) wherein R1, R2, R3, R4, and R5 are described herein, wherein at least two of the five R1, R2, R3, R4, and R5 substituents are always hydrogen, at least one of the five substituents is always nitro, and at least one substituent positioned adjacent to a nitro is always iodo, and pharmaceutically acceptable salts thereof.Type: GrantFiled: July 18, 2006Date of Patent: July 29, 2008Assignee: BiPAr Sciences, Inc.Inventors: Ernest Kun, Jerome Mendeleyev, Carol Basbaurn, Hassan Lemjabbar-Alaoui, Valeria Ossovskaya
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Patent number: 7402595Abstract: A JNK inhibitor containing a compound having an isoquinolinone skeleton or a salt thereof, such as a compound represented by the formula wherein ring A and ring B are each an optionally substituted benzene ring, X is —O—, —N?, —NR3— or —CHR3—, R2 is an acyl group, an optionally esterified or thioesterified carboxyl group, an optionally substituted carbamoyl group or an optionally substituted amino group and the like, a broken line shows a single bond or a double bond, and R1 is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group and the like, and the like.Type: GrantFiled: February 12, 2003Date of Patent: July 22, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Fumio Itoh, Hiroyuki Kimura, Hideki Igata, Tomohiro Kawamoto, Mitsuru Sasaki, Shuji Kitamura
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Patent number: 7402673Abstract: The invention provides novel ?2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with ?2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: June 2, 2005Date of Patent: July 22, 2008Assignee: Theravance, Inc.Inventor: Martin S. Linsell
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Patent number: 7402596Abstract: Bicycloheteroaryl compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: GrantFiled: March 17, 2006Date of Patent: July 22, 2008Assignee: Renovis, Inc.Inventors: Michael G. Kelly, John Kincaid
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Publication number: 20080161297Abstract: Disclosed are novel substituted 2H-isoquinolin-1-one and 3H-quinazolin-4-one derivatives useful as inhibitors of Rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of Rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds.Type: ApplicationFiled: September 18, 2007Publication date: July 3, 2008Inventors: Todd Bosanac, John David Ginn, Eugene Richard Hickey, Thomas Martin Kirrane, Weimin Liu, Anthony S. Prokopowicz, Sabine K. Schlyer, Cheng-Kon Shih, Roger John Snow, Michael Robert Turner, Frank Wu, Erick Richard Young