Having Chalcogen Or Nitrogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/362.5)
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Patent number: 7820683Abstract: A quinazoline derivative of the Formula I: wherein the substituents are as defined in the text for use in the production of an anti-proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm-blooded animal such as man.Type: GrantFiled: September 14, 2006Date of Patent: October 26, 2010Assignee: AstraZeneca ABInventors: Robert Hugh Bradbury, Bernard Christophe Barlaam, Richard Ducray
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Publication number: 20100267671Abstract: The present invention includes and relates generally to compounds which modulate apoptosis in cells. The present invention also provides pharmaceutical compositions containing these compounds, methods of making these compounds, and methods of using these compounds and pharmaceutical compositions for treatment of diseases associated with irregular apoptosis in cells.Type: ApplicationFiled: February 9, 2010Publication date: October 21, 2010Inventors: Jay Jie-Qiang Wu, Ling Wang
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Publication number: 20100256137Abstract: Novel indazole derivatives of the formula (I), in which R1-R3 have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: May 23, 2008Publication date: October 7, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Hans Peter Buchstaller, Hans Michael Eggenweiler, Christian Sirrenberg
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Publication number: 20100256108Abstract: A compound of the formula: wherein ring X is benzene or pyridine; R1 is substituted alkyl; R2 is optionally substituted aryl or optionally substituted heterocyclic group; R3 is hydrogen or alkyl; R4 is hydrogen, halogen or alkyl; R5 is hydrogen or alkyl; R6 and R7 are the same or different and each hydrogen or halogen, or a pharmaceutically acceptable salt thereof, which is useful as IKur blocker effective for preventing or treating cardiac arrhythmia such as atrial fibrillation.Type: ApplicationFiled: September 26, 2008Publication date: October 7, 2010Inventors: Tetsuo Yamaguchi, Hiroyuki Kawanishi, Hideki Ushirogochi, Tatsuyuki Takahashi, Tohru Takebe
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Publication number: 20100247534Abstract: A compound of formula I wherein m, n, A, B, D, E, G, H, Y, R1, R2, R3, R4, R5, and R8, are described herein.Type: ApplicationFiled: June 10, 2010Publication date: September 30, 2010Inventors: James A. Johnson, John Lloyd, Alexander Kover
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Patent number: 7803825Abstract: The present invention provides a compound of formula Ia: and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.Type: GrantFiled: July 15, 2008Date of Patent: September 28, 2010Assignee: Wyeth LLCInventors: Jonathan Laird Gross, Albert Jean Robichaud, Marla Jean Williams, Alessandro Mazzacani
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Patent number: 7803830Abstract: The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: GrantFiled: October 8, 2008Date of Patent: September 28, 2010Assignee: Roche Palo Alto LLCInventors: Pravin Iyer, Matthew C. Lucas, Ryan Craig Schoenfeld, Marzia Villa, Robert James Weikert
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Publication number: 20100240650Abstract: The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.Type: ApplicationFiled: May 25, 2010Publication date: September 23, 2010Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, David F. McComsey, Kimberly White, Hong Ye, Leonard R. Hecker, Bruce Conway, Keith Demarest
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Publication number: 20100234348Abstract: The present invention provides compounds that potentiate the activity of antibiotic agents, particularly quinolones such as norflaxin. The invention further provides compositions, e.g., pharmaceutical compositions, comprising the inventive compounds. The invention also provides compositions comprising an antibiotic (e.g., a quinolone) and a compound that potentiates activity of the antibiotic. The invention further provides methods of treating a subject comprising administering any of the inventive compounds or compositions to the subject. The invention also provides screening methods to identify compounds that potentiate the activity of an antibiotic, e.g., a quinolone.Type: ApplicationFiled: August 2, 2007Publication date: September 16, 2010Applicant: TRUSTEES OF BOSTON UNIVERSITYInventors: Guillaume Cottarel, Timothy S. Gardner, Xiaoguang Lei, John Porco, Scott E. Schaus, Jamey Wierzbowski, Kollol Pal
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Publication number: 20100234601Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional 2H-indazoles or 2H-azaindazoles of the formula (I) from 2-halo-phenylacetylenes or (2-sulfonato)phenylacetylenes and monosubstituted hydrazines.Type: ApplicationFiled: December 22, 2009Publication date: September 16, 2010Applicant: SANOFI-AVENTISInventors: Nis HALLAND, Marc NAZARE, Andreas LINDENSCHMIDT, Jorge ALONSO, Omar RKYEK, Matthias URMANN
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Patent number: 7781454Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein V, W, X, Y, Z, R1, R2, R4, R5, R6, ring A, ring B, j and k are defined herein. The compounds of Formula I, and the pharmaceutically acceptable salts and prodrugs thereof, are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. 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: December 6, 2007Date of Patent: August 24, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Neville J. Anthony, Robert Gomez
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Publication number: 20100210036Abstract: Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile.Type: ApplicationFiled: April 28, 2010Publication date: August 19, 2010Inventors: James Arnold, Dean R. Artis, Clarence H. Hurt, Prabha N. Ibrahim, Heike Krupka, Jack Lin, Michael V. Milburn, Weiru Wang, Chao Zhang
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Publication number: 20100204284Abstract: Hetero-substituted acetanilide derivatives are disclosed as analgesic agents. The compounds of the invention are useful in methods for treating a disease or condition in a mammal characterized by pain and/or fever.Type: ApplicationFiled: March 31, 2010Publication date: August 12, 2010Inventors: John R. Carson, James J. McNally
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Patent number: 7772232Abstract: A compound of formula I wherein m, n, A, B, D, E, G, H, Y, R1, R2, R3, R4, R5, and R8, are described herein. Said compounds being useful as inhibitors of potassium channel function and in the treatment of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.Type: GrantFiled: April 13, 2005Date of Patent: August 10, 2010Assignee: Bristol-Myers Squibb CompanyInventors: James A. Johnson, John Lloyd
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Patent number: 7759380Abstract: The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.Type: GrantFiled: May 8, 2007Date of Patent: July 20, 2010Assignee: Janssen Pharmaceutica, NVInventors: Han-Cheng Zhang, Bruce E. Maryanoff, David F. McComsey, Kimberly White, Hong Ye, Leonard R. Hecker
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Publication number: 20100173897Abstract: The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor.Type: ApplicationFiled: March 15, 2010Publication date: July 8, 2010Applicant: SANOFI-AVENTISInventors: Werngard CZECHTIZKY, Zhongli GAO, William J. HURST, Lothar SCHWINK, Siegfried STENGELIN
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Publication number: 20100173946Abstract: Compounds useful as GnRH receptor antagonists are provided. The present inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound which has benzene or thiophene ring substituted with a group derived from 1-hydroxymethyl, shows excellent availability, in addition to its excellent GnRH receptor antagonism, thereby accomplishing the invention. Since the compound of the invention shows excellent availability, in addition to its strong GnRH receptor antagonism, it can be expected that it exerts superior drug effect in the living body, and it is useful for the treatment of sex hormone dependent diseases such as prostate cancer, breast cancer, endometriosis, uterine leiomyoma, benign prostatic hypertrophy and the like.Type: ApplicationFiled: March 18, 2010Publication date: July 8, 2010Applicant: ASTELLAS PHARMA INCInventors: Masaaki Hirano, Eiji Kawaminami, Isao Kinoyama, Shunichiro Matsumoto, Kei Ohnuki, Kazuyoshi Obitsu, Toshiyuki Kusayama
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Patent number: 7741494Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with HDAC that comprise a compound selected from the group consisting of: wherein the substituents are as defined herein.Type: GrantFiled: October 31, 2007Date of Patent: June 22, 2010Assignee: Takeda San Diego, Inc.Inventors: Jerome C. Bressi, Anthony R. Gangloff, Lily Kwok
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Patent number: 7732475Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with HDAC that comprise a compound selected from the group consisting of: wherein the substituents are as defined herein.Type: GrantFiled: July 13, 2006Date of Patent: June 8, 2010Assignee: Takeda San Diego, Inc.Inventors: Jerome C. Bressi, Anthony R. Gangloff, Lily Kwok
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Patent number: 7713974Abstract: The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A1, A2, A3 or A4 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.Type: GrantFiled: August 15, 2007Date of Patent: May 11, 2010Assignee: Roche Palo Alto LLCInventors: Joshua Kennedy-Smith, Wylie Solang Palmer, Zachary Kevin Sweeney
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Patent number: 7700607Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: GrantFiled: July 18, 2007Date of Patent: April 20, 2010Inventors: Essa Hu, Jason Brooks Human, Roxanne Kunz, Andrew Tasker, Ryan White
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Publication number: 20100094011Abstract: The present invention provides novel methods for preparing 5-(trifluoromethoxy)-1H-3-indazolecarboxylic acid (3), which is a useful precursor for the preparation of bicyclic-5-trifluoromethoxy-1H-indazole-3-carboxylic acid amides of Formula (1). Compounds of Formula (1) are active as agonists and partial agonists of the nicotinic ?-7 receptor and are being studied for their use in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. The present methods are useful for preparing compound (3) on scale up levels.Type: ApplicationFiled: October 9, 2009Publication date: April 15, 2010Inventors: Thomas Cleary, Yaohui Ji, Thimma Rawalpally
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Publication number: 20100087489Abstract: A compound of formula Ia: The present invention relates to novel indazolyl derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicamentsType: ApplicationFiled: May 19, 2009Publication date: April 8, 2010Inventors: Markus Berger, Hartmut Rehwinkel, Jan Dahmén, Anders Eriksson, Thomas Hansson, Nafizal Hossain, Per Tomas Klingstedt, Matti Lepistö, Stinabritt Nilsson, Martin Hemmerling, Karl Edman
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Patent number: 7687532Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.Type: GrantFiled: January 27, 2005Date of Patent: March 30, 2010Assignee: GlaxoSmithkline LLCInventors: Sebastien Andre Campos, Stephen Swanson, Ann Louise Walker
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Publication number: 20100076027Abstract: This invention relates to novel indazole or 4,5,6,7-tetrahydro-indazole derivatives of formula I wherein R1 to R8 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are FXR modulators and can be used as medicaments.Type: ApplicationFiled: September 21, 2009Publication date: March 25, 2010Inventors: Gregory Martin Benson, Konrad Bleicher, Uwe Grether, Bernd Kuhn, Hans Richter, Sven Taylor
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Patent number: 7678803Abstract: The current invention is directed toward compounds and pharmaceutically acceptable salts of Formula I wherein Q1 is CR1, Q2 is N, Q4 and Q5 are each CR1, Q3 is CR2, X1 is N or CRc, Y is CRc, X2 and X3 are each C(R5)(R6), R7 is O. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer The current invention is also directed toward pharmaceutical compositions comprising compounds of the invention.Type: GrantFiled: August 24, 2007Date of Patent: March 16, 2010Assignee: Serenex, Inc.Inventors: Kenneth He Huang, James Veal, Thomas Barta, Emilie D. Smith, Wei Ma, Andy Ommen
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Patent number: 7674802Abstract: The present invention relates to a chemical genus of biaryl nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula: They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.Type: GrantFiled: August 3, 2006Date of Patent: March 9, 2010Assignee: deCODE genetics, ehfInventors: Vincent Sandanayaka, Jasbir Singh, Lei Zhao, Mark E. Gurney
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Patent number: 7666867Abstract: One aspect of the invention is concerned with cannabimimetic heteroindane analogs having affinities and/or selectivities for a cannabinoid receptor. A further aspect of the invention is concerned with pharmaceutical preparations employing the inventive analogs and methods of administering therapeutically effective amounts of the inventive analogs to provide a physiological effect.Type: GrantFiled: October 28, 2002Date of Patent: February 23, 2010Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Qian Liu, Alexander M Zvonok
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Patent number: 7655802Abstract: PDE4 inhibition is achieved by novel compounds, e.g., aminoindazole and aminobenzofuran analogs. The compounds of the present invention are of Formulas I and II: wherein R1, R2, R3, R4, R7 and R8 are as defined herein.Type: GrantFiled: December 21, 2006Date of Patent: February 2, 2010Assignee: Memory Pharmaceuticals CorporationInventors: Richard A. Schumacher, Allen T. Hopper, Ashok Tehim
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Publication number: 20100016368Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Q, R1-R3 and n are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.Type: ApplicationFiled: July 6, 2009Publication date: January 21, 2010Inventors: Li Chen, Fariborz Firooznia, Paul Gillespie, Yun He, Tai-An Lin, Sung-Sau So, HongYing Yun
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Publication number: 20090312366Abstract: The present application is directed to novel P2X7R antagonists that are indol-3-carboxamide or azaindole-3-carboxamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity.Type: ApplicationFiled: March 25, 2009Publication date: December 17, 2009Applicant: AFFECTIS PHARMACEUTICALS AGInventor: Michael Bös
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Publication number: 20090312386Abstract: [Object] In the case of using 3-[3-amino-4-(indan-2-yloxy)-5-(1-methyl-1H-indazol-5-yl)phenyl]propionic acid, methyl 3-[4-(indan-2-yloxy)-3-(1-methyl-1H-indazol-5-yl)-5-nitrophenyl]propionate, or methyl 3-[3-amino-4-(indan-2-yloxy)-5-(1-methyl-1H-indazol-5-yl)phenyl]propionate as a medicine, more preferable aspects or improved methods are provided. [Means] Crystals of any compound among 3-[3-amino-4-(indan-2-yloxy)-5-(1-methyl-1H-indazol-5-yl)phenyl]propionic acid, methyl 3-[4-(indan-2-yloxy)-3-(1-methyl-1H-indazol-5-yl)-5-nitrophenyl]propionate, and methyl 3-[3-amino-4-(indan-2-yloxy)-5-(1-methyl-1H-indazol-5-yl)phenyl]propionate, and methods of producing the same are provided.Type: ApplicationFiled: June 12, 2009Publication date: December 17, 2009Inventors: Yuichi ARIMOTO, Naoyuki ISHII, Motoshi SHODA
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Patent number: 7622594Abstract: Compounds of Formula (IA) and (IB) wherein R1, R2, R3, A, B, C, D, and E are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: GrantFiled: June 8, 2006Date of Patent: November 24, 2009Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Ingo Andreas Mugge, David S. Thomson, Abdelhakim Hammach, Michael Jason Burke, Mark Stephen Ralph, Jennifer A. Kowalski, Joerg Martin Bentzien
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Patent number: 7622493Abstract: The present invention is directed to compounds of formula (I) wherein variables X1, X2, Y, R1a, R1b, R2a, R2b, A1, A2, A3, and A4 are as defined in the description, and methods of use to treat pain, neuropathic pain, allodynia, pain associated with inflammation or an inflammatory disease, inflammatory hyperalgesia, bladder overactivity, and urinary incontinence.Type: GrantFiled: April 13, 2007Date of Patent: November 24, 2009Assignee: Abbott LaboratoriesInventors: Brian S. Brown, John R. Koenig, Arthur R. Gomtsyan, Chih-Hung Lee
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Publication number: 20090286800Abstract: Compounds are provided for use with glucokinase that comprise the formula: 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: May 15, 2009Publication date: November 19, 2009Applicant: TAKEDA SAN DIEGO, INC.Inventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Jeffrey A. Stafford, Mingnam Tang, Haxia Wang
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Publication number: 20090275619Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly (ADP-ribose) polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes, neurodegenerative diseases, retroviral infection, retinal damage or skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment.Type: ApplicationFiled: April 2, 2007Publication date: November 5, 2009Inventors: Julia Boueres, Danila Branca, Federica Ferrigno, Philip Jones, Ester Muraglia, Jesus Maria Ontoria Ontoria, Federica Orvieto, Rita Scarpelli, Carsten Schultz-Fademrecht
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Patent number: 7608633Abstract: The invention relates to novel heteroaryl substituted acetone derivatives which inhibit the enzyme phospholipase A2, pharmaceutical preparations containing these compounds and a method of producing these compounds.Type: GrantFiled: February 6, 2004Date of Patent: October 27, 2009Assignee: Merckle GmbHInventors: Matthias Lehr, Joachim Ludwig
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Patent number: 7605272Abstract: The present invention provides a type I insulin-like growth factor receptor (IGF-1R) inhibitor comprising, as an active ingredient, an indazole derivative represented by Formula (I): {wherein R1 represents —NR4R5 [wherein R4 represents a hydrogen atom or the like, R5 represents substituted or unsubstituted lower alkyl, —C(?O)R6 (wherein R6 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like), or the like], or the like, and R2 and R3 may be the same or different and each represents a hydrogen atom, hydroxy, substituted or unsubstituted lower alkoxy, or the like} or a pharmaceutically acceptable salt thereof, and the like.Type: GrantFiled: January 27, 2006Date of Patent: October 20, 2009Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Yutaka Kanda, Hiromi Ando, Keiko Kawashima, Takamasa Sugita, Masayo Suzuki, Hisashi Tagaya, Tomoyuki Nakazato, Yoshinori Yamashita, Takeshi Takahashi, Shinji Nara, Hiroaki Nakamura
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Publication number: 20090247504Abstract: Compounds of formula (IA) and (IB) are inhibitors of MARK, and hence are suitable for treatment of Alzheimer's disease.Type: ApplicationFiled: February 2, 2007Publication date: October 1, 2009Inventors: Ian Churcher, Hedaythul Choudhury, Neil Wilkie, Peter Hunt, Richard Jelley, Alan Nadin, Carmel Nanthakumar, Peter Simpson
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Patent number: 7592338Abstract: The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.Type: GrantFiled: August 2, 2007Date of Patent: September 22, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Alaric J. Dyckman, Jagabandhu Das, Katerina Leftheris, Chunjian Liu, Robert V. Moquin, Stephen T. Wrobleski
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Publication number: 20090233901Abstract: There is provided a VLA-4 inhibitory drug having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally.Type: ApplicationFiled: December 13, 2006Publication date: September 17, 2009Applicant: Daiichi Sankyo Company, LimitedInventors: Nobuo Machinaga, Shin Iimura, Yoshiyuki Yoneda, Jun Chiba, Fumihito Muro, Hideko Hoh, Atsushi Nakayama
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Publication number: 20090203691Abstract: The present invention provides a novel 1H-indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein R1 is a C6-C14 aromatic cyclic hydrocarbon group etc.; R2, R4 and R5 each independently represent a hydrogen atom, a halogen atom, a cyano group etc.; L is a single bond, or a C1-C6 alkylene group etc.; X is a single bond, or a group represented by —CO—NH— or —NH—CO—, etc.; and Y is a C3-C8 cycloalkyl group, a C6-C14 aromatic cyclic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group etc.Type: ApplicationFiled: April 20, 2009Publication date: August 13, 2009Inventors: Hitoshi Oinuma, Norihito Ohi, Nobuaki Sato, Motohiro Soejima, Hidenori Seshimo, Taro Terauchi, Takashi Doko, Naohiro Kohmura
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Patent number: 7563816Abstract: This invention relates to potent potassium channel blocker compounds of Formula (I) or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.Type: GrantFiled: July 15, 2005Date of Patent: July 21, 2009Assignee: Merck & Co. Inc.Inventors: James B. Doherty, Dong-Ming Shen
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Patent number: 7547720Abstract: This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.Type: GrantFiled: December 19, 2006Date of Patent: June 16, 2009Assignee: Merck & Co. Inc.Inventors: James B. Doherty, Meng-Hsin Chen, Luping Liu, Swaminathan R. Natarajan, Robert M. Tynebor
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Patent number: 7541376Abstract: The present invention provides a novel 1H-indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein R1 is a C6-C14 aromatic cyclic hydrocarbon group etc.; R2, R4 and R5 each independently represent a hydrogen atom, a halogen atom, a cyano group etc.; L is a single bond, or a C1-C6 alkylene group etc.; X is a single bond, or a group represented by —CO—NH— or —NH—CO—, etc.; and Y is a C3-C8 cycloalkyl group, a C6-C14 aromatic cyclic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group etc.Type: GrantFiled: August 12, 2005Date of Patent: June 2, 2009Assignee: Eisai R&D Management Co., Ltd.Inventors: Hitoshi Oinuma, Norihito Ohi, Nobuaki Sato, Motohiro Soejima, Hidenori Seshimo, Taro Terauchi, Takashi Doko, Naohiro Kohmura
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Patent number: 7541358Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: GrantFiled: August 14, 2007Date of Patent: June 2, 2009Assignee: WyethInventors: Ping Zhou, Michael Gerard Kelly
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Publication number: 20090131681Abstract: A fused pyrazolyl compound having an anti-tumor potency of the following formula is synthesized: wherein A is in which n is 0, 1, 2, or 3; Ar1 is benzene, thiophene or furan; Ar2 is furyl; and Ar3 is phenyl; R1 and R2 independently are hydrogen, halogen or —(CH2)mORe; R3 is hydrogen or alkyl; R4 is —(CH2)r-A1, wherein r is an integer of 1-5, and A1 has a formula of —O—C(O)—(CRcH)q—NRc?Rd?; R5 and R6 independently are hydrogen, halogen, or alkyl, or R5 and R6 together are —O(CH2)mO—; Rc is H, halogen, nitro, cyano, alkyl, or aryl; Re is H, alkyl, or aryl; Rc? and Rd? independently are H, alkyl, or aryl; m is 0, 1, 2, 3, 4, 5, or 6; and q is 1, 2, 3, 4, 5, or 6; or a salt thereof.Type: ApplicationFiled: November 13, 2008Publication date: May 21, 2009Applicant: YUNG SHIN PHARM. IND. CO., LTD.Inventors: Sheng-Chu Kuo, Che-Ming Teng, Fang-Yu Lee
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Patent number: 7528163Abstract: This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.Type: GrantFiled: November 4, 2003Date of Patent: May 5, 2009Assignee: Merck & Co. Inc.Inventors: James B. Doherty, Meng-Hsin Chen, Luping Liu, Swaminathan R. Natarajan, Dong-Ming Shen, Robert M. Tynebor
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Publication number: 20090099178Abstract: This invention is directed to Indazole Compounds or pharmaceutically acceptable salts, solvates and hydrates thereof. The Indazole Compounds have utility in the treatment or prevention of a wide range of diseases and disorders that are responsive to the inhibition, modulation or regulation of kinases, such as inflammatory diseases, abnormal angiogenesis and diseases related thereto, cancer, atherosclerosis, a cardiovascular disease, a renal disease, an autoimmune condition, macular degeneration, disease-related wasting, an asbestos-related condition, pulmonary hypertension, diabetes, obesity, pain and others. Thus, methods of treating or preventing such diseases and disorders are also disclosed, as are pharmaceutical compositions comprising one or more of the Indazole Compounds. This invention is based, in part, upon the discovery of a novel class of 5-triazolyl substituted indazole molecules that have potent activity with respect to the modulation of protein kinases.Type: ApplicationFiled: December 19, 2008Publication date: April 16, 2009Inventors: Shripad S. Bhagwat, Yoshitaka Satoh, Steven T. Sakata, Chris A. Buhr, Ronald Albers, John Sapienza, Veronique Plantevin, Qi Chao, Kiran Sahasrabudhe, Rachel Stengone, Rama K. Narla
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Patent number: 7514463Abstract: Novel compounds useful for inhibiting spermatogenesis and cancer treatment, and in particular as inhibitors of heat shock proteins and/or elongation factor 1 alpha.Type: GrantFiled: August 20, 2004Date of Patent: April 7, 2009Assignees: University of Kansas, University of Kansas Medical CenterInventors: Gunda I. Georg, Joseph S. Tash, Ramappa Chakrasali, Sudhakar Rao Jakkaraj