Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 540/490)
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Patent number: 11117905Abstract: The present invention relates to bisaryl heterocycle compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 activators.Type: GrantFiled: December 11, 2017Date of Patent: September 14, 2021Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITEDInventors: James Francis Callahan, Roderick S. Davis, Nicole Cathleen Goodwin, Jeffrey K. Kerns
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Patent number: 10421747Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: GrantFiled: December 28, 2017Date of Patent: September 24, 2019Assignee: ASTEX THERAPEUTICS LTDInventors: Wim Vermeulen, Steven Anna Hostyn, Filip Albert Celine Cuyckens, Russell Mark Jones, Diego Fernando Domenico Broggini
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Patent number: 9902714Abstract: The invention relates to new quinoxaline derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: GrantFiled: March 26, 2015Date of Patent: February 27, 2018Assignee: ASTEX THERAPEUTICS LTDInventors: Wim Vermeulen, Steven Anna Hostyn, Filip Albert Celine Cuyckens, Russell Mark Jones, Diego Fernando Domenico Broggini
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Patent number: 9125916Abstract: The present disclosure relates to a compound of formula (I) or formula (II) or a pharmaceutically acceptable salt thereof, for use in the treatment of hypertrophic cardiomyopathy.Type: GrantFiled: July 28, 2014Date of Patent: September 8, 2015Assignee: Gilead Sciences, Inc.Inventors: Luiz Belardinelli, Ramin Farzaneh-Far
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Patent number: 9040517Abstract: This invention relates to novel compounds which are inhibitors of acyl coenzymeA: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, hypertriglyceridemia, hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, hepatitis C virus infection and acne or other skin disorders.Type: GrantFiled: September 5, 2014Date of Patent: May 26, 2015Assignee: GlaxoSmithKline Intellectual Property (No. 2) LimitedInventors: Mui Cheung, Raghuram Tangirala
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Publication number: 20150126490Abstract: The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.Type: ApplicationFiled: October 29, 2014Publication date: May 7, 2015Applicant: Novartis AGInventors: Jeffrey T. BAGDANOFF, Yu DING, Wooseok HAN, Zilin HUANG, Qun JIANG, Jeff Xianming JIN, Xiang KOU, Patrick LEE, Mika LINDVALL, Zhongcheng MIN, Yue PAN, Sabina PECCHI, Keith Bruce PFISTER, Daniel POON, Vivek RAUNIYAR, Xiaojing Michael WANG, Qiong ZHANG, Jianguang ZHOU, Shejin ZHU
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Publication number: 20150105548Abstract: The present invention relates to anti-HCV compounds, compositions comprising the same and methods of using the same to treat HCV infection.Type: ApplicationFiled: May 25, 2012Publication date: April 16, 2015Inventors: Allan Krueger, Warren M. Kati, Clarence J. Maring, Rolf Wagner, Charles W. Hutchins
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Patent number: 8987250Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: GrantFiled: April 19, 2013Date of Patent: March 24, 2015Assignee: Gilead Sciences, Inc.Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Publication number: 20150064196Abstract: The present disclosure provides hetero-bicyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by Bruton's tyrosine kinase (Btk) activity, The disclosure also relates to the process of preparation of compounds of Formula (I). These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of Bruton's tyrosine kinase (Btk), such as inflammatory and/or autoimmune disorder, cell proliferation, rheumatoid arthritis, psoriasis, psoriatic arthritis, transplant rejection, graft-versus-host disease, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, B-cell malignancies, systemic lupus, erythematosus or other disorders.Type: ApplicationFiled: October 8, 2014Publication date: March 5, 2015Inventors: Mahesh Thakkar, Summon Koul, Debnath Bhuniya, Kasim Mookhtiar, Santosh Kurhade, Yogesh Munot, Tanaji Mengawade, Bheemashankar A. Kulkarni
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Patent number: 8962610Abstract: The present disclosure relates to compounds that are sodium channel inhibitors 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 Y, Z, n, R1 and R3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: GrantFiled: June 29, 2012Date of Patent: February 24, 2015Assignee: Gilead Sciences, Inc.Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
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Publication number: 20150038487Abstract: The present disclosure relates to a compound of formula (I) or formula (II) or a pharmaceutically acceptable salt thereof, for use in the treatment of hypertrophic cardiomyopathy.Type: ApplicationFiled: July 28, 2014Publication date: February 5, 2015Inventors: Luiz Belardinelli, Ramin Farzaneh-Far
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Publication number: 20140378434Abstract: This invention relates to novel compounds which are inhibitors of acyl coenzymeA: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, hypertriglyceridemia, hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, hepatitis C virus infection and acne or other skin disorders.Type: ApplicationFiled: September 5, 2014Publication date: December 25, 2014Inventors: Mui CHEUNG, Raghuram TANGIRALA
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Publication number: 20140378433Abstract: The invention relates to bicydic heterocyclic derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.Type: ApplicationFiled: January 25, 2013Publication date: December 25, 2014Applicant: SANOFIInventors: Alain Braun, Olivier Crespin, Yann Foricher, Gilbert Marciniak, Nicolas Muzet, Eric Nicolai, Cecile Pascal, Bertrand Vivet, Fabrice Viviani
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Patent number: 8859536Abstract: This invention relates to novel compounds which are inhibitors of acyl coenzymeA: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, hypertriglyceridemia, hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, hepatitis C virus infection and acne or other skin disorders.Type: GrantFiled: May 18, 2012Date of Patent: October 14, 2014Assignee: GlaxoSmithKline Intellectual Property (No.2) LimitedInventors: Donghui Qin, Mui Cheung, Hemant Joshi, Raghuram Tangirala, Sridhar Reddy Bethi
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Publication number: 20140179676Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: December 20, 2013Publication date: June 26, 2014Applicant: ABBVIE INC.Inventors: Kevin P. Cusack, Thomas D. Gordon, Michael Z. Hoemann, David C. Ihle, Bin Li, Gloria Y. Lo Schiavo, Gagandeep K. Somal, Michael Friedman, Martin E. Hayes, Wouter Iwema Bakker
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Publication number: 20140148437Abstract: This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia-related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, exceType: ApplicationFiled: November 22, 2013Publication date: May 29, 2014Applicant: GlaxoSmithKline LLCInventors: Mui CHEUNG, Raghuram S. TANGIRALA
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Patent number: 8710045Abstract: The present invention provides compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells.Type: GrantFiled: November 2, 2010Date of Patent: April 29, 2014Assignee: The Trustees of Columbia University in the City of New YorkInventors: Andrew Robert Marks, Donald W. Landry, Shixian Deng
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Patent number: 8697863Abstract: The present disclosure relates to compounds that are sodium channel inhibitors 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 Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: GrantFiled: March 7, 2013Date of Patent: April 15, 2014Assignee: Gilead Sciences, Inc.Inventors: Elfatih Elzein, Dmitry Koltun, Xiaofen Li, Jeff Zablocki, Chandrasekar Venkataramani
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Publication number: 20140100216Abstract: The invention relates to the area of medicinal chemistry, pharmacology and medicine and includes description of pharmaceutical compositions and combined medicaments on the base of secretion stimulators and protectors of incretin hormones for treatment of metabolic diseases (among them, diabetes, obesity, metabolic syndrome and the like). The invention consists in that that pharmaceutical composition or combined medicament comprises a derivative of tetrahydrobenzo[f][1,4]oxazepine—either nonsteroidal agonist of bile aids receptor TGR5, or one of endogenous bile acids which stimulate incretin hormones secretion, and also one of the known inhibitors of DPP-IV proteinase. In this case administration of TGR5 agonists is carried out peroral, and administration of endogenous bile acids is exercised rectal in the form of suppository or gel. As proteinase DPP-IV inhibitors could be used Vildagliptin, Saxagliptin, Sitagliptin, Teneligliptin, Linagliptin, Dutogliptin, Alogliptin, Gemigliptin, Carmegliptin and the like.Type: ApplicationFiled: May 12, 2012Publication date: April 10, 2014Inventors: Nikolay Filippovich Savchuk, Sergey Yevgenievich Tkachenko, Denis Yevgenievich Nazarenkov
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Publication number: 20140080809Abstract: This invention relates to novel compounds which are inhibitors of acyl coenzymeA: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, hypertriglyceridemia, hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, hepatitis C virus infection and acne or other skin disorders.Type: ApplicationFiled: May 18, 2012Publication date: March 20, 2014Applicant: GlaxoSmithKline Intellectual Property (No.2) LimitedInventors: Donghui Qin, Mui Cheung, Hemant Joshi, Raghuram Tangirala, Sridhar Reddy Bethi
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Publication number: 20140031338Abstract: The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.Type: ApplicationFiled: April 13, 2012Publication date: January 30, 2014Applicant: LABORATOIRE BIODIMInventors: Sophie Chasset, Francis Chevreuil, Benoit Ledoussal, Frédéric Le Strat, Richard Benarous
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Publication number: 20130345123Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein A is a five to eight membered monocyclic or a nine to twelve membered bicyclic heterocyclic ring, as further defined herein; Y is S, CH2, or CH; Z is CH or N; R7 and R9 are hydrogen or (C1-C6)alkyl; R2 is (C1-C6)alkoxy, OH, CN, (C1-C6)alkyl, halogen, or CF3; r and s are 0, 1, or 2; and R1 and R3 are as further defined herein. These compounds are agonists, partial agonists and/or modulators of the NPY4 receptor and may be used for the treatment and prophylaxis of obesity, food intake, and other diseases and conditions modulated by the NPY4 receptor.Type: ApplicationFiled: March 13, 2012Publication date: December 26, 2013Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Chongqing Sun, William R. Ewing, Scott A. Bolton, Zhengxiang Gu, Yanting Huang, Natesan Murugesan, Yeheng Zhu
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Publication number: 20130338142Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of an imidazopyrazine compound effective to reduce signs or symptoms of the disease or disorder are provided.Type: ApplicationFiled: June 14, 2013Publication date: December 19, 2013Inventors: Peter A. BLOMGREN, Kevin S. CURRIE, Randall HALCOMB, Jeffrey E. KROPF, Seung H. LEE, Jiayao LI, Jennifer R. LO, Scott A. MITCHELL, Aaron SCHMITT, Qiaoyin WU, Jin-Min XIONG, Jianjun XU, Zhongdong ZHAO, Jayaraman CHANDRASEKHAR, Eric LANSDON
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Patent number: 8609648Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: June 15, 2010Date of Patent: December 17, 2013Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Lu Ying, Xiaowen Peng, Datong Tang, Ce Wang, Yao-Ling Qiu
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Patent number: 8586732Abstract: The present disclosure relates to compounds that are sodium channel inhibitors 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 Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: GrantFiled: June 29, 2012Date of Patent: November 19, 2013Assignee: Gilead Sciences, Inc.Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
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Publication number: 20130281433Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: ApplicationFiled: April 19, 2013Publication date: October 24, 2013Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Publication number: 20130184255Abstract: The present disclosure relates to compounds that are sodium channel inhibitors 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 Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: March 7, 2013Publication date: July 18, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
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Publication number: 20130158006Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.Type: ApplicationFiled: November 28, 2012Publication date: June 20, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Patent number: 8440652Abstract: 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: GrantFiled: March 2, 2012Date of Patent: May 14, 2013Assignee: Lexicon Pharmaceuticals, Inc.Inventors: 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: 20130012492Abstract: The present disclosure relates to compounds that are sodium channel inhibitors 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 Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: June 29, 2012Publication date: January 10, 2013Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
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Publication number: 20120328599Abstract: The present invention provides moieties that bind to the asymmetric contact interface of a receptor tyrosine kinase (RTK), wherein the moieties inhibit ligand induced trans autophosphorylation of the RTK. The present invention also provides methods of treating or preventing an RTK-associated disease and methods for identifying moieties that bind to an asymmetric contact interface of an RTK.Type: ApplicationFiled: January 13, 2011Publication date: December 27, 2012Applicant: YALE UNIVERSITYInventors: Jae Hyun Bae, Irit Lax, Joseph Schlessinger
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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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Patent number: 8247403Abstract: Compounds represented by the general formula (I): wherein each symbol is as defined in the description [with the proviso that 9-chloro-7-(1,1-dimethylethyl)-2,3,4,5-tetrahydro-1,4-benz-oxazepine and N-[[(5S)-2-oxo-3-(2,3,4,5-tetrahydro-1,4-benz-oxazepin-7-yl)-5-oxazolidinyl]methyl]acetamide are excluded], salts of the same, and prodrugs thereof have selective activation effect on serotonin 5-HT2C receptor and are useful as preventive and therapeutic agents for lower urinary tract diseases, obesity, and/or pelvic organ prolapse.Type: GrantFiled: March 6, 2008Date of Patent: August 21, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Junya Shirai, Takahiro Matsumoto, Izumi Kamo
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Publication number: 20120184732Abstract: The present invention provides a nitrogen-containing heterocyclic compound represented by formula (I) and salt thereof, which is useful as an active ingredient of a fungicide for agricultural and horticultural use, having an assured effect and being safely usable.Type: ApplicationFiled: September 22, 2010Publication date: July 19, 2012Inventors: Akira Mitani, Jun Inagaki, Raito Kuwahara, Motoaki Sato
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Patent number: 8158617Abstract: The present invention relates to a serotonin 5-HT2C receptor activator containing a compound represented by the formula wherein ring A is a 5- or 6-membered aromatic heterocycle optionally having substituent(s), and ring B is a 7- to 9-membered ring optionally having substituent(s) other than an oxo group wherein the combination of m and n (m,n) is (1,2), (2,1), (2,2), (3,1), (3,2) or (4,1), or a salt thereof or a prodrug thereof, and a fused heterocyclic compound having a serotonin 5-HT2C receptor activating action and the like.Type: GrantFiled: May 15, 2007Date of Patent: April 17, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Junya Shirai, Tomokazu Kusumoto, Hiroyuki Nagamiya
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Publication number: 20120065189Abstract: The present invention provides a novel heterocyclic compound. A heterocyclic compound represented by general formula (1) wherein, R1 and R2, each independently represent hydrogen; a phenyl lower alkyl group that may have a substituent(s) selected from the group consisting of a lower alkyl group and the like on a benzene ring and/or a lower alkyl group; or a cyclo C3-C8 alkyl lower alkyl group; or the like; R3 represents a lower alkynyl group or the like; R4 represents a phenyl group that may have a substituent(s) selected from the group consisting of a 1,3,4-oxadiazolyl group that may have e.g., halogen or a heterocyclic group selected from pyridyl group and the like; the heterocyclic group may have at least one substituent(s) selected from a lower alkoxy group and the like or a salt thereof.Type: ApplicationFiled: May 27, 2010Publication date: March 15, 2012Inventors: Akira Takahashi, Masaki Suzuki, Yuichi Nakamura, Yohji Sakurai
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Publication number: 20110288071Abstract: The present invention encompasses compounds of general formula (1) wherein A, B, X, R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: November 24, 2009Publication date: November 24, 2011Applicant: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Ioannis Sapountzis
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Publication number: 20110251173Abstract: DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, diabetes and obesity wherein, R1, R2, R3, R4, X2, q, Y1, Y2, n, Q and Z are as defined in the description.Type: ApplicationFiled: March 31, 2011Publication date: October 13, 2011Applicant: AstraZeneca ABInventors: Alan Martin BIRCH, Frederick Woolf GOLDBERG, Andrew LEACH
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Patent number: 8022058Abstract: The present invention provides novel compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells. Such disorders and diseases include, by way of example only, cardiac disorders and diseases, skeletal muscular disorders and diseases, cognitive disorders and diseases, malignant hyperthermia, diabetes, and sudden infant death syndrome.Type: GrantFiled: August 25, 2005Date of Patent: September 20, 2011Assignee: The Trustees of Columbia University in the City of New YorkInventors: Andrew Robert Marks, Donald W. Landry, Shixian Deng
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Patent number: 8012960Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: June 7, 2010Date of Patent: September 6, 2011Assignee: Schering CorporationInventors: Zhaoning Zhu, Andrew W. Stamford, Brian McKittrick
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Patent number: 7994160Abstract: Disclosed are pyridazine compounds of the formula I which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds: In formula I indicates a single bond or a double bond; X is O, S or N—R5; R1, R2 are independently selected from the group consisting of H, NH2, NH—C1-C6-alkyl, OH, ?O, (i.e.Type: GrantFiled: July 12, 2006Date of Patent: August 9, 2011Assignee: Abbott GmbH & Co. KGInventors: Sean C. Turner, Margaretha Bakker, Roland Grandel, Michael Vierling
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Patent number: 7981879Abstract: Compounds of Formula I are inhibitors of FHV integrase and inhibitors of FHV replication (I), wherein m, n, X, R1, R2, R3, R4, R5, R6, R7; R8, R9 and R10 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HTV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HTV infection and ADDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: March 22, 2006Date of Patent: July 19, 2011Assignee: Instituto di Ricerchi di Biologia Molecolare P. Angeletti S.p.A.Inventors: Vincenzo Summa, Paola Pace
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Publication number: 20110172190Abstract: The present invention provides compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells.Type: ApplicationFiled: November 2, 2010Publication date: July 14, 2011Inventors: Andrew Robert Marks, Donald W. Landry, Shixian Deng
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Publication number: 20110150864Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: December 16, 2010Publication date: June 23, 2011Inventors: Gilles BIGNAN, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Patent number: 7943607Abstract: Compounds of formula (I), wherein R1, R4, HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: GrantFiled: May 23, 2006Date of Patent: May 17, 2011Assignee: AstraZeneca ABInventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Patent number: 7879840Abstract: The present invention provides compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells.Type: GrantFiled: August 17, 2006Date of Patent: February 1, 2011Assignee: The Trustees of Columbia University in the City of New YorkInventors: Andrew Robert Marks, Donald W. Landry, Shixian Deng
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Publication number: 20100273768Abstract: This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-II: wherein, variables Q1, Q2, R, X, Y1, Y2, Y2?, Y3, Y4, Y5, m, and p 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 Formulae I-II and at least one carrier, diluent or excipient.Type: ApplicationFiled: April 23, 2010Publication date: October 28, 2010Inventors: Nolan James Dewdney, Ronald Charles Hawley, Rama Kondru, Yingjie Lai, Yan Lou
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Publication number: 20100267945Abstract: A compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, where R1 is optionally substituted lower alkyl, Y is —S(O)2—, R2 is hydrogen or optionally substituted lower alkyl, R7 is hydrogen or optionally substituted lower alkyl, X is a group of the formula: where R5 and R6 are each independently hydrogen, a group of the formula: is optionally substituted cycloalkylene, p is 0, and q is 1 or 2, Z is optionally substituted carbocyclyl or optionally substituted heterocyclyl, and provided that a compound wherein Z is fused heterocyclyl consisting of three rings or optionally substituted pyrimidinyl is excluded.Type: ApplicationFiled: June 25, 2010Publication date: October 21, 2010Applicant: Shionogi & Co., Ltd.Inventors: Takayuki Okuno, Naoki Kouyama, Masahiro Sakagami
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Publication number: 20100261641Abstract: The present invention relates to a spiro-piperidine compound represented by formula (I): wherein R1 represents hydrogen, an aliphatic hydrocarbon group which may have a substituent(s) or a cyclic group which may have a substituent(s); and ring A represents a 5- to 8-membered cyclic group which may have a substituent(s), a salt thereof, an N-oxide thereof, a quaternary ammonium salt thereof or a solvate thereof, or a prodrug thereof. The compounds represented by formula (I) have chemokine antagonistic action, so that they are useful for prevention and/or treatment of various inflammatory diseases, immune diseases such as autoimmune diseases or allergic diseases, or HIV infection.Type: ApplicationFiled: December 11, 2008Publication date: October 14, 2010Applicant: Ono Pharmaceutical Co., Ltd.Inventors: Rena Nishizawa, Yoshikazu Takaoka, Hiromu Habashita, Shiro Shibayama, Masaya Kokubo
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Publication number: 20100204119Abstract: The invention provides compounds of Formula (I), wherein R1, R2a, R2b, R3, m and A are as defined herein, as well as compositions thereof and methods for treating a disease, condition or disorder that is modulated by the inhibition of the diacylglycerol O-acyltransferase 1 (DGAT-1) enzyme by administering the compounds of the present invention and/or compositions thereof.Type: ApplicationFiled: February 1, 2010Publication date: August 12, 2010Inventors: Gary E. Aspnes, Robert L. Dow, Michael J. Munchhof