Plural Ring Nitrogens In The Polycyclo Ring System Patents (Class 514/322)
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Patent number: 8293738Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A1, A2, A3 and L are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora and KDR.Type: GrantFiled: May 12, 2011Date of Patent: October 23, 2012Assignee: Abbott LaboratoriesInventors: Michael R. Michaelides, James H. Holms, Douglas H. Steinman
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Publication number: 20120264737Abstract: Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.Type: ApplicationFiled: March 8, 2012Publication date: October 18, 2012Applicant: 3-V BIOSCIENCES, INC.Inventors: Johan D. Oslob, Robert S. McDowell, Russell Johnson, Hanbiao Yang, Marc Evanchik, Cristiana A. Zaharia, Haiying Cai, Lily W. Hu
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Publication number: 20120264733Abstract: Compounds represented by the formulas wherein each symbol is as defined in the specification, and a prodrug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.Type: ApplicationFiled: April 13, 2012Publication date: October 18, 2012Inventors: Takanobu KUROITA, Yasuhiro Imaeda, Kouichi Iwanaga, Naohiro Taya, Hidekazu Tokuhara, Yoshiyuki Fukase
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Patent number: 8288412Abstract: Compounds of formula (I) and salts are provided: wherein R5 is selected from halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano; R6 is selected from halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano; and Q is hydrogen or C1-6alkyl. The compounds are M1 agonists and are useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.Type: GrantFiled: September 27, 2006Date of Patent: October 16, 2012Assignee: Glaxo Group LimitedInventors: Brian Budzik, David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Jian Jin, Dongchuan Shi, Paul William Smith, Graham Walker
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Patent number: 8288413Abstract: Compounds of formula (I) and salts are provided: wherein R6 is selected from hydrogen, halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano, and Q is hydrogen or C1-6alkyl. The compounds are M1 agonists and are useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.Type: GrantFiled: September 27, 2006Date of Patent: October 16, 2012Assignee: Glaxo Group LimitedInventors: Brian Budzik, David Gwyn Cooper, Ian Thomson Forbes, Jian Jin, Dongchuan Shi, Paul William Smith, Graham Walker
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Publication number: 20120258181Abstract: The present invention relates to combinations between artemisinin-based potent anti-malarial agents, selected from the group consisting of ART, DHA and ARM, and a further chemotherapeutic drug selected from the group consisting of a camptothecin derivative, or a PARP-1 inhibitor, or an intercalating DNA agent, or an alkylating agent. Such combinations, showed medium to strong synergism in various models of cancer, in particular in NSCL.Type: ApplicationFiled: December 6, 2010Publication date: October 11, 2012Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.Inventors: Claudio Pisano, Loredana Vesci
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Patent number: 8283364Abstract: Compounds of formula (I) and salts are provided: wherein R4 is fluoro, R5 is selected from hydrogen, halogen, cyano, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C1-6alkoxy, and C1-6alkoxy substituted with one or more fluorine atoms; and R6 is selected from halogen, cyano, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6alkoxy and C1-6alkoxy substituted with one or more fluorine atoms, and Q is hydrogen or C1-6alkyl. The compounds are expected to be useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.Type: GrantFiled: September 27, 2006Date of Patent: October 9, 2012Assignee: Glaxo Group LimitedInventors: Brian Budzik, David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Jian Jin, Dongchuan Shi, Paul William Smith, Graham Walker
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Publication number: 20120252843Abstract: Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases.Type: ApplicationFiled: June 11, 2012Publication date: October 4, 2012Inventors: George W. Muller, Alexander L. Ruchelman
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Patent number: 8278341Abstract: Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2?-diindolylmethane, 2?,3-diindolylmethane, and 3,3?-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.Type: GrantFiled: September 17, 2009Date of Patent: October 2, 2012Assignee: SRI InternationalInventors: Ling Jong, Faming Jiang, Gaoquan Li, Kristien Mortelmans
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Patent number: 8273740Abstract: The invention relates to 2-sulfanyl-benzoimidazol-1-yl-acetic acid derivatives and their use as potent “chemoattractant receptor-homologous molecule expressed on Th2 cells” antagonists in the treatment of prostaglandin mediated diseases, to pharmaceutical compositions containing these derivatives and to processes for their preparation.Type: GrantFiled: August 23, 2005Date of Patent: September 25, 2012Assignee: Actelion Pharmaceuticals, Ltd.Inventors: Heinz Fretz, Markus Gude, Kurt Hilpert, Julien Pothier, Markus Riederer, Matthias Steger
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Publication number: 20120238567Abstract: The present invention relates to compounds having pharmacological activity towards the sigma (?) receptor, and more particularly to some 4, 5, 6, 7 tetrahydrobenzo[b]thiophene derivatives, wherein n is selected from 0, 1, 2, 3 or 4; m is selected from 0, 1 or 2; the dotted line represents either a single or a double bond; to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis.Type: ApplicationFiled: May 30, 2012Publication date: September 20, 2012Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Jordi CORBERA-ARJONA, Daniel MARTINEZ-OLMO, David VANO-DOMENECH
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Publication number: 20120237475Abstract: Novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein Ra, n, R1 and R2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).Type: ApplicationFiled: March 16, 2012Publication date: September 20, 2012Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Daniel Ramsbeck
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Publication number: 20120238574Abstract: The present invention relates to (1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl derivatives having the general formula (I) to pharmaceutical compositions comprising the same and to the use of these (1,1,1,3,3,3-hexafluoro-2-hydroxy-propan-2-yl)phenyl derivatives in the treatment of atherosclerosis.Type: ApplicationFiled: October 26, 2010Publication date: September 20, 2012Applicant: N.V. ORGANONInventors: Andrew John Cooke, Emma Louise Carswell, David Jonathan Bennett
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Patent number: 8269019Abstract: Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: GrantFiled: March 10, 2011Date of Patent: September 18, 2012Assignee: Probiodrug AGInventors: Ulrich Heiser, Ulf-Torsten Gaertner, Hans-Ulrich Demuth
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Publication number: 20120232052Abstract: The present invention relates to aryl carboxamide derivatives of formula (I), wherein Ar1 is phenyl; Ar2 is aryl; n is 1-4; X is —O—, —S—, —SO— or —SO2—, a prodrug thereof or a pharmaceutically acceptable salt thereof, which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of such disorders and diseases as pain in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases as pain in which voltage gated sodium channels are involved.Type: ApplicationFiled: November 16, 2010Publication date: September 13, 2012Inventors: Tatsuya Yamagishi, Yoshimasa Arano, Mikio Morita, Tadashi Inoue
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Publication number: 20120232112Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, G, R10, R11, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: January 24, 2012Publication date: September 13, 2012Applicant: SANOFIInventors: Sven RUF, Thorsten SADOWSKI, Georg HORSTICK, Herman SCHREUDER, Christian BUNING, Thomas OLPP, Klaus WIRTH
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Patent number: 8263597Abstract: Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: July 18, 2011Date of Patent: September 11, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Daniel Kuzmich, Can Mao, Alan David Swinamer, David Smith Thomson
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Publication number: 20120220562Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: February 24, 2012Publication date: August 30, 2012Applicant: ABBOTT LABAORATORIESInventors: David A DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Yi Gao, Dachun Liu, John K. Pratt, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, David A. Betebenner, Kathy Sarris, Kevin R. Woller, William A. Carroll
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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: 20120214766Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor.Type: ApplicationFiled: August 27, 2010Publication date: August 23, 2012Inventors: Robert M. Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
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Publication number: 20120208811Abstract: A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like <R1 and R2 together form a (substituted) 3- to 10-membered heterocyclyl group or a (substituted) 5- to 10-membered heteroaryl group>; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.Type: ApplicationFiled: August 5, 2010Publication date: August 16, 2012Applicants: F. HOFFMANN-LA ROCHE AG, CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Naoki Taka, Masayuki Ohmori, Kyoko Takami, Masayuki Matsushita, Tadakatsu Hayase, Ikumi Hyodo, Masami Kochi, Hiroki Nishii, Hirosato Ebiike, Yoshito Nakanishi, Toshiyuki Mio, Lisha Wang, Weili Zhao
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Publication number: 20120196896Abstract: One aspect of the invention relates to compounds, compositions and methods for treating oxidative stress and/or hypertension. In certain embodiments, the invention relates to a mixture of tempol and an angiotensin receptor blocker (ARB) and the use of said mixture to treat oxidative stress and/or hypertension. In certain embodiments, the invention relates to a tempol/ARB adduct and the use of said adduct to treat oxidative stress and/or hypertension.Type: ApplicationFiled: September 17, 2010Publication date: August 2, 2012Applicant: Georgetown UniversityInventors: Milton L. Brown, Yali Kong, Christopher Stuart Wilcox
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Publication number: 20120196897Abstract: The present invention relates to compounds of general formula I in which A, L, M, Q2, Q3, Q4, R1, R5, Ra, Rb, Rc, W, X, Y, Z1, Z2, Z3 are defined in the description, the salts thereof, particularly the physiologically acceptable salts thereof. The compounds are of potential utility in the treatment and/or prevention of inflammatory diseases and associated conditions, in particular, in the treatment and/or prevention of pain. The invention also relates to the use of such compounds as medicaments, to pharmaceutical compositions containing them, and to their preparation.Type: ApplicationFiled: April 6, 2012Publication date: August 2, 2012Applicant: Boehringer Ingelheim International GmbHInventors: Roland PFAU, Kirsten ARNDT, Henri DOODS, Klaus KLINDER, Raimund KUELZER, Dimitrijs LUBRIKS, Juergen MACK, Benjamin PELCMAN, Henning PRIEPKE, Robert ROENN, Dirk STENKAMP, Edgars SUNA
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Patent number: 8227472Abstract: Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.Type: GrantFiled: October 9, 2007Date of Patent: July 24, 2012Assignee: Nerviano Medical Sciences S.R.L.Inventors: Michele Caruso, Italo Beria, Maria Gabriella Brasca, Ron Ferguson, Helena Posteri
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Patent number: 8227485Abstract: The invention relates to novel benzimidazole and imidazopyridine derivatives having general formula (I), which have a good affinity with certain sub-types of melanocortin receptors, particularly MC4 receptors. Said derivatives are particularly suitable for the treatment of pathological states and diseases involving one or more melanocortin receptors. The invention also relates to pharmaceutical compositions containing said products.Type: GrantFiled: May 26, 2006Date of Patent: July 24, 2012Assignee: Ipsen Pharma S.A.S.Inventors: Lydie Poitout, Valerie Brault, Carole Sackur, Pierre Roubert, Pascale Plas
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Publication number: 20120184556Abstract: Disclosed are substituted benzoimidazolesulfonamides and substituted indolesulfonamides as mGluR4 potentiators.Type: ApplicationFiled: July 23, 2010Publication date: July 19, 2012Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Yiu-Yin Cheung
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Publication number: 20120178719Abstract: The present invention relates to methods of treating neurodegenerative diseases comprising administering, to a subject in need of such treatment, one or more agent that inhibits or reduces the action, including the catalytic activity, of an enzyme of the phospholipase D family, such as phospholipase D1 and/or phospholipase D2. The present invention also relates to cell-based assays which may be used to identify agents that inhibit or reduce the activity of enzymes of the phospholipase D family and that may be used in the treatment of neurodegenerative diseases.Type: ApplicationFiled: November 28, 2011Publication date: July 12, 2012Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Gilbert DiPaolo, Tae-Wan Kim, Tiago Gil Oliveira
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Publication number: 20120171129Abstract: Disclosure is provided for benzimidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.Type: ApplicationFiled: June 10, 2010Publication date: July 5, 2012Inventors: Christian Melander, Steven A. Rogers, Robert W. Huigens, III
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Publication number: 20120165311Abstract: Thieno[2,3-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: February 24, 2012Publication date: June 28, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Daniele Fancelli, Paola Vianello, Mario Varasi, Simona Bindi, Sergio Vioglio, Dania Tesei
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Publication number: 20120165305Abstract: The present invention relates to substituted imidazopyridazines and substituted benzimidazoles, as well as pharmaceutical compositions comprising the same, which are FGFR3 inhibitors useful in the treatment of cancer and other diseases.Type: ApplicationFiled: December 21, 2011Publication date: June 28, 2012Inventors: Wenqing YAO, Colin ZHANG, Meizhong XU, Jincong ZHUO, Chunhong HE
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Patent number: 8207201Abstract: The present invention provides an agent for the prophylaxis or treatment of substance abuse and dependence, which contains a compound of the formula (I) represented by (R)-2-{3-[1-(acenaphthen-1-yl)piperidin-4-yl]-2,3-dihydro-2-oxo-benzimidazol-1-yl}-N-methylacetamide, or a pharmaceutically acceptable salt thereof as an active ingredient.Type: GrantFiled: October 16, 2007Date of Patent: June 26, 2012Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Koji Teshima, Roberto Ciccocioppo, Maurizio Massi
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Publication number: 20120157495Abstract: The present invention relates to a compound of the Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3A, R3B, R4, R5, X, m, and n are as defined herein. Such novel benzamidazole derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: February 24, 2012Publication date: June 21, 2012Inventors: Michael J. MUNCHHOF, Lawrence A. Reiter, Susan D. La Greca, Christopher S. Jones, Qifang Li
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Publication number: 20120149683Abstract: The present invention is directed to novel substituted aminopiperidines of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-ÏV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: September 15, 2010Publication date: June 14, 2012Inventors: Jason M. Cox, Tesfaye Biftu, Hong Dong Chu, Danqing Feng, Ann E. Weber
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Publication number: 20120148534Abstract: Briefly described, embodiments of this disclosure include compounds, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, methods of treating liver fibrosis in a host, and the like.Type: ApplicationFiled: March 16, 2010Publication date: June 14, 2012Inventors: Jeffrey S. Glenn, Wenjin Yang, Ingrid C. Choong
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Publication number: 20120149676Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.Type: ApplicationFiled: December 8, 2011Publication date: June 14, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Alexander HEIM-RIETHER, Raimund KUELZER, Roland PFAU, Klaus RUDOLF, Dirk STENKAMP
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Patent number: 8198307Abstract: The present invention is directed to a novel imidazole derivative having an aryl piperidine substituent of formula (I) and a method for preparation thereof, and a pharmaceutical composition containing said imidazole derivative as an active ingredient for preventing or treating a MCH (melanine-concentrating hormone)-related disease.Type: GrantFiled: May 13, 2008Date of Patent: June 12, 2012Assignee: Korea Research Institute of Chemical TechnologyInventors: Jee Hee Suh, Kyu Yang Yi, Nack Jeong Kim, Sung Eun Yoo, Kwang-Seok Oh, Hyae Gyeong Cheon, Mija Ahn, Byung Ho Lee, Won Hoon Jung, Sang Dal Rhee
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Publication number: 20120142686Abstract: The present invention relates to viral polymerase inhibitors of formula (I), salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections:Type: ApplicationFiled: October 20, 2011Publication date: June 7, 2012Inventors: Rosliana Halim, Michael Harding, Richard Hufton, Craig James Morton, Saba Jahangiri, Brett Raymond Pool, Tyrone Pieter Jeynes, Alistair George Draffan, Barbara Frey, Michael John Lilly
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Patent number: 8193229Abstract: Disclosed are methods of treating a hyperproliferative disorder or a disease related to vasculogenesis or angiogenesis in a mammal, comprising administering to said mammal an effective amount of a compound of the formula or a pharmaceutically accepted salt thereof, wherein A, R1, R2, R7, R8, and R9 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals.Type: GrantFiled: June 28, 2010Date of Patent: June 5, 2012Assignee: Array Biopharma Inc.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
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Patent number: 8193369Abstract: The present invention is related to novel benzimidazole compounds of Formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.Type: GrantFiled: March 25, 2008Date of Patent: June 5, 2012Assignee: Janssen Pharmaceutica NVInventors: Henricus Jacobus Maria Gijsen, Michel Anna Jozef De Cleyn, Michel Surkyn
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Publication number: 20120135953Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.Type: ApplicationFiled: August 6, 2010Publication date: May 31, 2012Applicant: Tibotec PharmaceuticalsInventors: David Mc Gowan, Samuel Dominique Demin, Stefaan Julien Last, Koen Vandyck, Pierre Jean-Marie Bernard Raboisson
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Publication number: 20120135990Abstract: The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.Type: ApplicationFiled: May 27, 2010Publication date: May 31, 2012Applicant: TETRALOGIC PHARMACEUTICALS CORP.Inventors: Stephen M. Condon, Yijun Deng, Matthew D. Alexander, Matthew G. Laporte
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Publication number: 20120129850Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.Type: ApplicationFiled: January 24, 2012Publication date: May 24, 2012Inventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
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Publication number: 20120129811Abstract: This invention relates to tricycle I and its therapeutic and prophylactic uses, wherein the variables C1, C2, Z1, Z2, Q, J, R1, and R3 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.Type: ApplicationFiled: November 16, 2011Publication date: May 24, 2012Inventors: Aihua WANG, Yan Zhang, Kristi Anne Leonard, Michael Hawkins, Brett Andrew Tounge, Umar S.M. Maharoof, Joseph Kent Barbay
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Publication number: 20120122773Abstract: The present invention provides a compound of formula (I): wherein R1a is optionally substituted C1-6 alkyl, etc.; R1m is hydrogen atom, etc.; G1, G2, G3 and G4 are (i), etc. ((i) G1 is —N(R1b)—, G2 is —CO—, G3 is —C(R1c)(R1d)—, and G4 is oxygen, etc.); R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are each independently optionally substituted C1-6 alkyl, etc.; R2 is optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are each independently a group: -A-B (A is a single bond, etc., B is hydrogen atom, etc.), etc.; n is 1, etc.; R5 is C1-4 alkoxycarbonyl, etc., or a pharmaceutically acceptable salt thereof, which is useful as a renin inhibitor.Type: ApplicationFiled: June 24, 2010Publication date: May 17, 2012Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Satoshi Suetsugu, Nobuhisa Fukuda, Yoshio Nakai, Takashi Takada, Yohei Ikuma, Hiroyuki Nakahira
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Publication number: 20120115856Abstract: A compound depicted by the formula below, or a pharmaceutically acceptable salt or solvate thereof. wherein, R1 represents (1) a C3-6 alkyl group, (2) a C1-6 alkyl group substituted with one or more substituent group(s) selected from those consisting a halogen atom, etc., (3) a C3-10 non-aromatic cyclic hydrocarbon group or a 5- to 6-membered non-aromatic heterocyclic group which respectively is optionally substituted with one or more substituent group(s) selected from those consisting an oxo group, etc., (4) an aromatic cyclic hydrocarbon group substituted with one or more substituent selected from the group consisting halogen atom and C1-4 alkoxy group; X represents NH, O, or S; Y represents CH or N; Z represents N or a C—R2; R2 represents (1) hydrogen atom, (2) a C1-6 alkyl group, a C2-6 alkenyl group or a C2-6 alkynyl group that respectively is optionally substituted with one or more substituent group(s) selected from among those consisting (a) a halogen atom, etc.Type: ApplicationFiled: May 28, 2010Publication date: May 10, 2012Inventors: Junichi Ishikawa, Koichi Saito, Norihisa Ohe, Kentaro Kobayashi
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Patent number: 8173679Abstract: The present invention relates to compounds of formula (I): in which R1, R2, R3, X, Y and A are as defined in the specification. The compounds are modulators of the estrogen receptors.Type: GrantFiled: June 3, 2011Date of Patent: May 8, 2012Assignee: Laboratoire ThermamexInventors: Benoit Rondot, Jean Lafay, Paule Bonnet, Thierry Clerc, Igor Duc, Eric Duranti, Francois Puccio, Jacqueline Shields, Christian Blot, Philippe Maillos
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Publication number: 20120108584Abstract: Compounds corresponding to the formula (I) as defined in the disclosure, as well as methods for making such compounds, intermediates employed in such methods, pharmaceutical compositions containing the compounds of the invention, and methods of treatment using them.Type: ApplicationFiled: January 11, 2012Publication date: May 3, 2012Applicant: SANOFI-AVENTISInventors: Laurent DUBOIS, Yannick Evanno, Christian Maloizel, Mireille Sevrin
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Publication number: 20120108575Abstract: The invention relates to Heterocyclic-Substituted Piperidine Compounds, compositions comprising an effective amount of a Heterocyclic-Substituted Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Heterocyclic-Substituted Piperidine Compound.Type: ApplicationFiled: January 12, 2012Publication date: May 3, 2012Applicants: Shionogi & Co., Ltd., Purdue Pharma L.P.Inventors: Kevin C. Brown, R, Richard Goehring, Yoshiyasu BABA, Naoki Tsuno
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Patent number: 8163774Abstract: The present invention comprises the use of amino-substituted 8-N-benzimidazoles compounds of formula I wherein R3, R4-R5, R11 and R20-R21 are hereinafter defined which display a therapeutically utilizable blood sugar-lowering action. These compounds are intended to be particularly suitable in the treatment of diabetes.Type: GrantFiled: September 13, 2007Date of Patent: April 24, 2012Assignee: Sanofi-AventisInventors: Elisabeth DeFossa, Karl Schoenafinger, Gerhard Jaehne, Christian Buning, Georg Tschank, Ulrich Werner
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Publication number: 20120088752Abstract: Heterocyclic compounds that modulate the hedgehog signaling pathway, pharmaceutical composition thereof and their therapeutic applications.Type: ApplicationFiled: June 9, 2010Publication date: April 12, 2012Applicant: SIENA BIOTECH S.p.A.Inventors: J. Russell Thomas, Gal.la Pericot Mohr, Chiara Caramelli, Giacomo Minetto, Marta Bellini