Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/141)
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Publication number: 20130005965Abstract: The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3-a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optType: ApplicationFiled: July 2, 2012Publication date: January 3, 2013Applicants: BRISTOL-MYERS SQUIBB COMPANY, ALBANY MOLECULAR RESEARCH, INC.Inventors: Bruce F. MOLINO, Shuang LIU, Peter R. GUZZO, James P. BECK
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Publication number: 20130005709Abstract: The present invention relates to novel sulfone compounds as 5-HT6 receptor ligands of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. These compounds are useful in the treatment/prevention of various disorders that are related to 5-HT6 receptor functions.Type: ApplicationFiled: March 24, 2010Publication date: January 3, 2013Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Rama Sastri Kambhampati, Rajesh Kumar Badange, Veena Reballi, Anil Kashinath Chindhe, Rambabu Namala, Mohamad Sadik Abdulhamid Mulla, Ishtiyaque Ahmad, Renny Abraham, Venkateswarlu Jasti
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Publication number: 20120330019Abstract: 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: August 29, 2012Publication date: December 27, 2012Inventors: Xiangdong Alan Wang, Li-Qiang Sun, Sing-Yuen Sit, Ny Sin, Paul Michael Scola, Piyasena Hewawasam, Andrew Charles Good, Yan Chen, Jeffrey Allen Campbell
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Patent number: 8338449Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: April 2, 2010Date of Patent: December 25, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: B. Wesley Trotter, Christopher Claiborne, Gerald S. Ponticello, Charles J. McIntyre, Nigel Liverton, David A. Claremon
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Publication number: 20120309786Abstract: Compounds represented by the general formula (I): pharmaceutically acceptable salts or solvates thereof, a process for their manufacture; pharmaceutical compositions containing them; and use of the compounds in the treatment of metabolic disorders related to insulin resistance or hyperglycemia are described.Type: ApplicationFiled: August 13, 2012Publication date: December 6, 2012Inventors: Nabajyoti DEKA, Kamlesh Jyotindra Padiya, Swapnil Ramesh Bajare, Rhushikesh Arun Kulkarni, Taj Usman Khan, Sivaramakrishnan Hariharan, Rosalind Adaikalasamy Marita
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Patent number: 8318941Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure formula (I) enantiomers, diastereomers, solvates, salts, tautomers or prodrugs thereof wherein, A, W, X, Y and R1 are defined herein.Type: GrantFiled: July 2, 2007Date of Patent: November 27, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Jeffrey A. Robl, Shung C. Wu, David S. Yoon
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Publication number: 20120295885Abstract: This application discloses compounds according to generic Formula I: wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.Type: ApplicationFiled: May 16, 2012Publication date: November 22, 2012Inventors: Roland Joseph Billedeau, Rama K. Kondru, Francisco Javier Lopez-Tapia, Yan Lou, Timothy D. Owens, Yimin Qian, Sung-Sau So, Kshitij C. Thakkar, Jutta Wanner
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Patent number: 8314120Abstract: The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved.Type: GrantFiled: March 28, 2011Date of Patent: November 20, 2012Assignee: Abbott GmbH & Co. KGInventors: Wilfried Braje, Katja Jantos, Hervé Geneste, Mario Mezler, Margaretha Henrica Maria Bakker
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Patent number: 8309573Abstract: The invention provides a salt of (R)-3-[2-(2-hydroxymethylpyrrolidin-1-yl)ethyl]-5-methyl-2H-isoquinolin-1-one and a crystal thereof. (R)-3-[2-(2-Hydroxymethylpyrrolidin-1-ypethyl]-5-methyl-2H-1-isoquinolin-1-one monophosphate is a compound which is chemically stable, has high solubility, and shows less weight change due to humidity as compared to a free form and monohydrochloride dihydrate, and is superior as a bulk drug for pharmaceutical products.Type: GrantFiled: August 8, 2008Date of Patent: November 13, 2012Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Masakazu Fujio, Toshihiko Tanaka, Hisao Takayanagi, Hiroyuki Satoh, Takanori Ito
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Publication number: 20120283216Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Q is O or S; Z1 and Z2 are each independently CR9 or N; and R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: December 22, 2010Publication date: November 8, 2012Inventors: Alvin Donald Crews, JR., Amy X. Ding, Chi-Ping Tseng
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Patent number: 8299055Abstract: The present invention relates to a compound represented by the following formula (1): wherein D1, A1, D2, R1, D3, and R2 each have the same meaning as defined in the present specification or a salt thereof. The compound represented by the formula (1) or a salt thereof has an IKK? inhibiting activity and the like and is useful for the prevention and/or treatment of IKK?-associated diseases or symptoms and the like.Type: GrantFiled: October 1, 2009Date of Patent: October 30, 2012Assignee: Asahi Kasei Pharma CorporationInventors: Shunsuke Kaneko, Kenichiro Sato, Daisuke Shikanai, Rintaro Yamada, Katsuhiko Sakurada
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Patent number: 8293911Abstract: This invention provides a compound of formula IA where X?O or S; Y is O or S; q=1 or 0; and other substituents are defined herein. Such compounds can affect the opening of, or otherwise modulate, voltage-gated potassium channels. They are potentially useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.Type: GrantFiled: August 22, 2007Date of Patent: October 23, 2012Assignee: Valeant Pharmaceuticals InternationalInventors: Jean-Michel Vernier, Martha Alicia De La Rosa, Huanming Chen, Jim Zhen Wu, Gary Lee Larson, Ian Wayne Cheney
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Publication number: 20120258513Abstract: Compounds and related methods for selective inhibition of neuronal nitric oxide synthase over inducible and endothelial isoforms, such compounds as can provide reduced cationic character and enhanced bioavailability.Type: ApplicationFiled: April 6, 2012Publication date: October 11, 2012Inventors: Richard B. Silverman, Haitao Ji, He Huang
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Publication number: 20120259094Abstract: The present invention relates generally to affinity ligands and chemical affinity ligand-matrix conjugates for use as chromatographic adsorbents and methods which utilise the adsorbents in the purification of proteins by affinity chromatography. The affinity ligand-matrix conjugates of the present invention comprise ligands of general formula (I): wherein m represents an integer from 0-2, n represents an integer from 0-6, p represents an integer from 0-4, R1 represents H or C1-3 alkyl, R2 is an optional substituent, and X is the position at which the ligand is immobilized, optionally via a linker.Type: ApplicationFiled: October 15, 2010Publication date: October 11, 2012Inventors: Milton TW Hearn, Anjali Makarand Bhagwat, William Roy Jackson, Simon John Mountford
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Publication number: 20120252814Abstract: Compounds of the following formula are provided for use with glucokinase: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: March 21, 2012Publication date: October 4, 2012Applicant: TAKEDA CALIFORNIA, INC.Inventors: Zacharia Cheruvallath, Jun Feng, Prasuna Guntupalli, Stephen L. Gwaltney, Joanne Miura, Mark Sabat, Mingnam Tang, Haxia Wang
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Patent number: 8278442Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are opioid receptor modulators, e.g. mu-opioid receptor antagonists, neutral antagonists or inverse agonists, and are useful for the treatment of metabolic disorders including obesity.Type: GrantFiled: May 22, 2008Date of Patent: October 2, 2012Assignee: Prosidion LimitedInventors: Jason Bloxham, Stuart Edward Bradley, Tom Banksia Dupree, Peter Timothy Fry, Patrick Eric Hanrahan, Thomas Martin Krulle, Martin James Procter, Colin Peter Sambrook-Smith, Karen Lesley Schofield, Donald Smyth, Alan John Stewart
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Patent number: 8278325Abstract: The present invention relates to compounds suitable for use in mediating hypoxia inducible factor and for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo.Type: GrantFiled: July 19, 2011Date of Patent: October 2, 2012Assignee: FibroGen, Inc.Inventors: Michael P. Arend, Lee A. Flippin, Volkmar Guenzler-Pukall, Wen-Bin Ho, Eric Turtle, Xiaohui Du
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Patent number: 8273767Abstract: Compounds of formula (I) 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: August 3, 2010Date of Patent: September 25, 2012Assignee: Abbott LaboratoriesInventors: Robert J. Altenbach, Lawrence A. Black, Sou-Jen Chang, Marlon D. Cowart, Ramin Faghih, Gregory A. Gfesser, Yi-Yin Ku, Huaqing Liu, Kirill A. Lukin, Diana L. Nersesian, Yu-ming Pu, Padam N. Sharma, Youssef L. Bennani, Michael P. Curtis
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Publication number: 20120237874Abstract: According to one embodiment, an actinic-ray- or radiation-sensitive resin composition includes any of the compounds (A) of general formula (I) below that when exposed to actinic rays or radiation, generates an acid and a resin (B) whose rate of dissolution into an alkali developer is increased by the action of an acid. (The characters used in general formula (I) have the meanings mentioned in the description.Type: ApplicationFiled: May 31, 2012Publication date: September 20, 2012Applicant: FUJIFILM CORPORATIONInventors: Shuhei Yamaguchi, Akinori Shibuya
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Patent number: 8269010Abstract: The present invention provides novel compounds represented by the general formula (I): their pharmaceutically acceptable salts and their pharmaceutically acceptable solvates thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia. The invention also relates to a process for the manufacture of compounds of formula (I) and pharmaceutical compositions containing them.Type: GrantFiled: September 20, 2007Date of Patent: September 18, 2012Assignee: Piramal Healthcare LimitedInventors: Nabajyoti Deka, Kamlesh Jyotindra Padiya, Swapnil Ramesh Bajare, Rhushikesh Arun Kulkarni, Taj Usman Khan, Sivaramakrishnan Hariharan, Rosalind Adaikalasamy Marita
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Publication number: 20120225857Abstract: Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.Type: ApplicationFiled: March 2, 2012Publication date: September 6, 2012Inventors: David John Augeri, Jeffrey Thomas Bagdanoff, Simon David Peter Baugh, Marianne Carlsen, Kenneth Gordon Carson, John Anthony Gilleran, Wei He, Tamas Oravecz, Konstantin Salojin, Leonard Sung
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Publication number: 20120225847Abstract: The present application discloses novel squaric acid derivatives of the formula A: from —C(?O)—, —S(?O)2—, —C(?S)— and —P(?O)(R5)—; B: -, —O—, —NR6— and —C(?O)—NR6—; D: -, —O—, —CR7R8— and —NR9; m=0-12; n=0-12; m+n=1-20; p=0-2; R1: heteroaryl, aryl; R2: H, C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; R3: C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; or R2 and R3: N-containing heterocyclic/heteroaromatic ring; R4 and R4*: H, C1-12-alkyl, C1-12-alkenyl; and pharmaceutically acceptable salts and prodrugs thereof, and their use in the treatment of diseases/conditions caused by an elevated level of NAMPRT (inflammatory and tissue repair disorders, particularly rheumatoid arthritis, inflammatory bowel disease, asthma and CPOD, osteoarthritis, osteoporosis and fibrotic diseases; dermatosis; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankylType: ApplicationFiled: June 24, 2009Publication date: September 6, 2012Inventors: Mette Knak Christensen, Fredrik Bjorkling
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Patent number: 8258302Abstract: 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: GrantFiled: January 31, 2007Date of Patent: September 4, 2012Assignee: API CorporationInventor: Hisatoshi Uehara
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Publication number: 20120220622Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.Type: ApplicationFiled: November 2, 2010Publication date: August 30, 2012Inventors: Julia Adam, Jonathan Gillespie, Steven Laats, John Kinnaird Ferguson MacLean, Duncan Robert McArthur
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Publication number: 20120220774Abstract: The present disclosure generally relates to a process for synthesizing optionally substituted 1-chloro-4-methoxyisoquinolines. The present disclosure also relates to intermediates useful in this process.Type: ApplicationFiled: May 10, 2012Publication date: August 30, 2012Inventors: Shawn A. Springfield, Wendel W. Doubleday, Frederic Buono, Michel A. Couturier, Yvonne Lear, Denis Favreau, Kathia Levesque, Percy Sarwood Manchand, Markus Frieser, Anthony J. Cocuzza
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Publication number: 20120214807Abstract: 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, 2011Publication date: August 23, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Shomir Ghosh, Prakash Raman, Kevin Sprott, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
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Publication number: 20120214837Abstract: The invention relates to compounds of the formula wherein R?, R1, through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicants: ExonHit Therapeutics SA, ALLERGAN, INC.Inventors: Bertrand Leblond, Cédric Chauvignac, Thierry Taverne, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Désiré, Matthew P. Pando, John E. Donello, Rong Yang
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Publication number: 20120208827Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of benzimidazoles in the treatment of cancer.Type: ApplicationFiled: October 27, 2010Publication date: August 16, 2012Inventors: Steven Dock, Jason Hallman, Christopher Laudeman, Ronggang Liu, Aaron Miller, Michael Lee Moore, David Musso, Cynthia Parrish
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Publication number: 20120208818Abstract: 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 10, 2011Publication date: August 16, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Amy M. Elder, Shomir Ghosh, Sian Griffiths, Prakash Raman, Francois Soucy, Kevin Sprott, Qing Ye
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Publication number: 20120208842Abstract: The present invention relates to novel 1-(1-Oxo-1,2,3,4-tetrahydroisoquinolin-7-yl)urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: ApplicationFiled: February 10, 2012Publication date: August 16, 2012Applicant: ALLERGAN, INCInventors: Richard L. Beard, John E. Donello, Tien T. Duong, Michael E. Garst, Veena Viswanath
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Publication number: 20120208796Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by nicotinic acetylcholine receptors, such as schizophrenia and Alzheimer's disease.Type: ApplicationFiled: October 11, 2010Publication date: August 16, 2012Inventors: Paul David Ratcliffe, Thomas Russell Clarkson, Fiona Jeremiah, John Kinnard Ferguson MacLean
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Patent number: 8242134Abstract: The invention relates to compounds useful in therapy, in particular in the treatment of psychosis, to compositions comprising said compounds, and to methods of treating diseases comprising the administration of said compounds.Type: GrantFiled: September 11, 2009Date of Patent: August 14, 2012Assignee: H. Lundbeck A/SInventors: Nikolay Khanzhin, Karsten Juhl, Soren Moller Nielsen, Klaus Baek Simonsen
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Publication number: 20120202795Abstract: The present invention relates to a series of 2,3,5-substituted pyridone derivatives of formula I: wherein R, R1, R2, R3 and R4 are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5?-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.Type: ApplicationFiled: April 18, 2012Publication date: August 9, 2012Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: Philip M. WEINTRAUB, Paul R. EASTWOOD, Shujaath MEHDI, David W. STEFANY, Kwon Yon MUSICK, Neil MOORCROFT, Sungtaek LIM, John Z. JIANG, Hartmut RUTTEN, Stefan PEUKERT, Uwe SCHWAHN
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Publication number: 20120172392Abstract: Compositions and methods are disclosed for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1). The compounds disclosed are amine-containing and amide-containing compounds. The compounds and compositions are useful for treatment of diseases, including inflammation, inflammatory diseases and autoimmune disorders.Type: ApplicationFiled: March 7, 2012Publication date: July 5, 2012Inventors: LUISA M. SALTER-CID, ERIC Y. WANG, MARY T. MACDONALD, JINGJING ZHAO
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Patent number: 8211897Abstract: The present invention is directed to a method of using compounds of Formula (I) to inhibit Cathepsin B. Specifically the compounds of the present invention are useful as therapeutic agents for the treatment of tumor invasion, metastasis, Alzheimer's Disease, arthritis, inflammatory diseases such as chronic and acute pancreatitis, inflammatory airway disease, and bone and joint disorders, including osteoporosis, osteoarthritis, rheumatoid arthritis, psoriasis, and other autoimmune disorders, liver fibrosis, including liver fibrosis associated with HCV, all types of steatosis (including non-alcoholic steatohepatitis) and alcohol-associated steatohepatitis, non-alcoholic fatty liver disease, forms of pulmonary fibrosis including idiopathic pulmonary fibrosis, pathological diagnosis of interstitial pneumonia following lung biopsy, renal fibrosis, cardiac fibrosis, retinal angiogenesis and fibrosis/gliosis in the eye, schleroderma, and systemic sclerosis.Type: GrantFiled: February 5, 2009Date of Patent: July 3, 2012Assignee: ViroBay, Inc.Inventor: Leslie Holsinger
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Patent number: 8207341Abstract: The present disclosure generally relates to a process for synthesizing optionally substituted 1-chloro-4-methoxyisoquinolines. The present disclosure also relates to intermediates useful in this process.Type: GrantFiled: August 25, 2009Date of Patent: June 26, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Shawn A. Springfield, Wendel W. Doubleday, Percy Sarwood Manchand, Hyungcheol Kim, Sangsoo Lee, Chunyoung Kim, Soonha Yang, Eunhee Choi
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Publication number: 20120157403Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: ApplicationFiled: February 24, 2012Publication date: June 21, 2012Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
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Publication number: 20120149688Abstract: Novel compounds of formulae (I) and (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 10, 2011Publication date: June 14, 2012Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles K. Marlowe, Kim A. Kane-Maguire
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Publication number: 20120135984Abstract: Provided are compounds, compositions, and methods for treating diseases and conditions wherein an inhibitor of a kinase, such as rho kinase (ROCK), and an inhibitor of one or more of the monoamine transporters, such as NET or SERT, act in concert to improve the condition.Type: ApplicationFiled: May 1, 2010Publication date: May 31, 2012Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty, Geoffrey Richard Heintzelman, Jeffrey D. Yingling, Casey Kopczynski
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Patent number: 8188117Abstract: 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: GrantFiled: January 25, 2008Date of Patent: May 29, 2012Assignee: Sanofi-AventisInventors: Oliver Plettenburg, Armin Hofmeister, Dieter Kadereit, Joachim Brendel, Matthias Loehn
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Patent number: 8173639Abstract: 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: GrantFiled: April 11, 2008Date of Patent: May 8, 2012Assignee: H. Lundbeck A/SInventors: Klaus Baek Simonsen, Jan Kehler, Karsten Juhl, Nikolay Khanzhin, Soren Moller Nielsen
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Patent number: 8173674Abstract: The invention relates to sulfonyl-phenyl-oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma agonist activity. What are described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: GrantFiled: June 9, 2009Date of Patent: May 8, 2012Assignee: Sanofi-AventisInventors: Stefanie Keil, Matthias Urmann, Karl Schoenafinger, Wolfgang Wendler, Maike Glien, Hans-Ludwig Schaefer, Eugen Falk
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Publication number: 20120108605Abstract: The present invention provides inhibitors of O-GIcNAc transferase. Typically, the inhibitors are quinolinone-6-sulfonamides. The invention also provides pharmaceutical compositions thereof and methods for using the same in diabetes and complications thereof, neurodegenerative diseases, cancers, autoimmune diseases, and inflammatory diseases.Type: ApplicationFiled: June 1, 2010Publication date: May 3, 2012Applicant: President and Fellows of Harvard CollegeInventors: Suzanne Walker Kahne, Michael Block Lazarus, Benjamin J. Gross
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Patent number: 8168798Abstract: This invention relates to prodrugs of caspase inhibitors comprising of a furo[3,2-d]oxazolin-5-one moiety which, under specific conditions, can convert into biologically active compounds, particularly caspase inhibitors. This invention also relates to the processes for preparing these prodrugs of caspase inhibitors. This invention further relates to pharmaceutical compositions comprising said prodrugs and to the use thereof for the treatment of diseases related to inflammatory or degenerative conditions.Type: GrantFiled: December 17, 2010Date of Patent: May 1, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Steven Durrant, Jean-Damien Charrier, John Studley
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Patent number: 8163756Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions, hyperproliferative diseases, cancer, and diseases characterized by hyper-vascularization are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein, abl kinase protein, ber-abl kinase protein, braf kinase protein, VEGFR kinase protein, or PDGFR kinase protein comprises the step of contacting said kinase protein with the novel compounds.Type: GrantFiled: December 21, 2007Date of Patent: April 24, 2012Assignee: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo
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Patent number: 8163744Abstract: 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: GrantFiled: March 17, 2006Date of Patent: April 24, 2012Assignee: NexusPharma, Inc.Inventors: Lutz Weber, Vladimir Khazak, Günther F Ross, Cotïc Kalinski, Christoph Burdack
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Patent number: 8163921Abstract: 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: GrantFiled: April 6, 2009Date of Patent: April 24, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Ny Sin, Brian Lee Venables, Paul Michael Scola, Alan Xiangdong Wang
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Publication number: 20120094997Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, Ra, R2a, R2b, R1, and X have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: October 14, 2011Publication date: April 19, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Dylan B. England, Kenneth M. Gigstad, Alexandra E. Gould, Liting Ma, He Xu
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Publication number: 20120094971Abstract: This invention relates to compounds of Formula (I) wherein Cy1, L1, Y, R1, L2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions.Type: ApplicationFiled: September 3, 2009Publication date: April 19, 2012Applicant: REPLIGEN CORPORATIONInventors: James R. Rusche, Norton P. Peet, Allen T. Hopper
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Publication number: 20120094958Abstract: The invention relates to a compound of formula (I) wherein the substituents are as described in the specification, which are useful as farnesyl pyrophosphate synthase modulators, e.g. in the treatment of proliferative diseases, to methods of manufacturing such compounds and to intermediates thereof.Type: ApplicationFiled: February 26, 2009Publication date: April 19, 2012Applicant: NOVARTIS AGInventors: Rene Amstutz, Guido Bold, Simona Cotesta, Wolfgang Jahnke, Andreas Marzinzik, Juliane Constanze Desiree Hartwieg, Silvio Ofner, Frédérik Stauffer, Johann Zimmermann