Additional Hetero Ring, Attached Directly Or Indirectly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 548/465)
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Publication number: 20110034461Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R9, Ar, Q1, Q2 and Q3 are each as defined below. The compounds of the formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of the formula I and to the use thereof as a medicament.Type: ApplicationFiled: August 5, 2010Publication date: February 10, 2011Applicant: sanofi-aventisInventors: Uwe HEINELT, Volkmar WEHNER, Matthias HERRMANN, Karl SCHOENAFINGER, Henning STEINHAGEN
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Patent number: 7884125Abstract: The present invention relates to a group of substituted-7-azabicyclo-[2.2.1]heptyl derivatives with biological activity. The present invention also relates to synthetic methods for producing said substituted-7-azabicyclo-[2.2.1]heptyl derivatives. The present invention also relates to certain intermediates for producing such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as a synthetic method for producing such intermediates. The present invention also relates to pharmaceutical compositions comprising such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as their use as medicaments for the treatment of diseases mediated by a Nicotinic Acetylcholine Receptor or a receptor being a member of the Neurotransmitter-gated Ion Channel Superfamily, such as pain, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy and nicotine addiction.Type: GrantFiled: August 8, 2008Date of Patent: February 8, 2011Assignee: Universiteit GentInventors: Christian Stevens, Thomas Heugebaert
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Publication number: 20110028463Abstract: [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.Type: ApplicationFiled: July 2, 2008Publication date: February 3, 2011Applicant: Astellas Pharma Inc.Inventors: Eisuke Nozawa, Ryotaro Ibuka, Kazuhiro Ikegai, Keisuke Matsuura, Tatsuya Zenkoh, Ryushi Seo
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Publication number: 20110015180Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the variants R, R9, Z, X, Q and Y are defined in the specification.Type: ApplicationFiled: September 20, 2010Publication date: January 20, 2011Inventors: René Hersperger, Philipp Janser, Emil Pfenninger, Hans Juerg Wuethrich, Wolfgang Miltz
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Publication number: 20110009379Abstract: [Problems] A compound, which is useful as an active ingredient for a pharmaceutical composition, for example a pharmaceutical composition for treating constipation-type irritable bowel syndrome, atonic constipation and/or functional gastrointestinal disorder, is provided. [Means for Solution] The present inventors have extensively studied compounds having TRPA1 channel activation activity, and confirmed that an indolinone compound has a TRPA1 channel activation activity, and thus completed the present invention. The indolinone compound of the present invention has a TRPA1 channel activation activity and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating constipation-type irritable bowel syndrome, atonic constipation and/or functional gastrointestinal disorder or the like.Type: ApplicationFiled: March 30, 2009Publication date: January 13, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Hidetaka Kaku, Tomofumi Takuwa, Michihito Kageyama, Katsura Nozawa, Hitoshi Doihara
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Publication number: 20100311715Abstract: This invention provides alpha-carboline compounds of formula I: wherein R1, R2, R3, R4, R5, and x are as described in the specification. The compounds are useful for treating inflammatory diseases and cancer.Type: ApplicationFiled: August 19, 2010Publication date: December 9, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Michael E. Hepperle, Julie Fields Liu, R. Scott Rowland, Dilrukshi Vitharana
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Patent number: 7847106Abstract: The present invention relates to a new process for the preparation of tripeptides of formula I wherein R1 is an amino protecting group and X is a halogen atom and wherein the tipeptide contains two olefinic moieties suitably disposed to undergo an intramolecular olefin metathesis reaction and produce macrocyclic tripeptides useful for the manufacture of macrocyclic HCV protease inhibitors.Type: GrantFiled: April 24, 2008Date of Patent: December 7, 2010Assignee: Roche Palo Alto LLCInventors: Francois Gantz, Helmut Stahr
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Publication number: 20100305100Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.Type: ApplicationFiled: July 1, 2010Publication date: December 2, 2010Applicant: PTC THERAPEUTICS, INC.Inventors: Gary Mitchell Karp, Peter Seongwoo Hwang, James J. Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey Allen Campbell, Chunshi Li, Steven Paget, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
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Patent number: 7842819Abstract: Sulfonamide derivatives act as ion channel antagonists. The compositions are useful for treating or relieving pain-related conditions.Type: GrantFiled: October 23, 2006Date of Patent: November 30, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Esther Martinborough, Andreas P. Termin, Timothy D. Neubert, Nicole Zimmermann, Corey Don Gutierrez
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Patent number: 7834004Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: GrantFiled: September 4, 2008Date of Patent: November 16, 2010Assignee: Kalypsys, IncInventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D Bayne, Mehmet Kahraman, Boliang Lou, Steven P. Govek
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Patent number: 7834048Abstract: The present invention relates to a compound of the formula (I) wherein R1 is H, C1-C6-alkyl which may be substituted by C3-C6-cycloalkyl, fluorinated C1-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6-alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one or more substituents selected from halogen, methyl, methoxy and CF3; E is NR5 or CH2, wherein R5 is H or C1-C3-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, O and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR8, where R8 is H, C1-C4-alkType: GrantFiled: October 14, 2005Date of Patent: November 16, 2010Assignee: Abbott GmbH & Co. KGInventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel
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Publication number: 20100261721Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors.Type: ApplicationFiled: June 24, 2010Publication date: October 14, 2010Inventors: Thomas MAIER, Thomas Beckers, Thomas Baer, Petra Gimmnich, Frank Dullweber, Matthias Vennemann
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Publication number: 20100240642Abstract: The present invention relates to certain indole derivatives that are modulators of PPAR?, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine.Type: ApplicationFiled: August 31, 2007Publication date: September 23, 2010Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Jeffrey Alan Oplinger, Paul Kenneth Spearing, Millard Hurst Lambert, John A. Ray, Christopher P. Laudeman, Jerzy R. Szewczyk, Pierette Banker
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Publication number: 20100234350Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 14, 2009Publication date: September 16, 2010Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-McGuire, Hans-Michael Jantzen, David M. Sedlock
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Publication number: 20100234431Abstract: A compound of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, X, Y, and Z are as defined herein. Also disclosed is a method for inhibiting actively of fibroblast activation protein or for treating cancer or inflammation conditions with such a compound.Type: ApplicationFiled: February 19, 2010Publication date: September 16, 2010Applicant: National Health Research InstitutesInventors: Weir-Tong Jiaang, Xin Chen
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Publication number: 20100222381Abstract: Compounds represented by Formula (I): are useful in treating diseases, such as cancer, that are mediated and/or associated (at least in part) with DNMT3b activity. The compounds can be formulated as pharmaceutically acceptable compositions for administration to a subject in need thereof.Type: ApplicationFiled: February 26, 2010Publication date: September 2, 2010Inventors: Hariprasad Vankayalapati, Krzysztof Swierczek, Scott Albert Pearce
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Patent number: 7776910Abstract: Compounds of the formula I: wherein m, n, Ar, R1 and R2 are as defined herein. Methods of making the compounds and using the compounds are disclosed.Type: GrantFiled: November 8, 2007Date of Patent: August 17, 2010Assignee: Roche Palo Alto LLCInventors: Francisco Javier Lopez-Tapia, Lee Edwin Lowrie, Jr., Dov Nitzan
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Publication number: 20100204285Abstract: The invention relates to novel trans-3-aza-bicyclo[3.1.0]hexane derivatives of formula (I), wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: July 25, 2008Publication date: August 12, 2010Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, David Lehman, Thierry Sifferlen, Daniel Trachsel
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Publication number: 20100204200Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula 1: wherein Q is an optionally substituted azetidinyl, pyrrolidinyl, piperidyl, and indolinyl; or Q is NR25R26; and A, R5, R6, R7, R8, R9, R25, R26 and Ar are substituents.Type: ApplicationFiled: April 21, 2010Publication date: August 12, 2010Applicant: IRM LLCInventors: Hong Liu, Arnab Chatterjee, David C. Tully, Phillip Alper, Badry Bursulaya, Jianhua Guo, David H. Woodmansee, Daniel Mutnick, Donald S. Karanewsky, Yun He
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Patent number: 7772270Abstract: The invention relates to a bicycloazaheterocyclyl carboxylic acid sulfonamide derivative of formula I herein, pharmaceutical preparation comprising it, process for preparing it and method for its pharmaceutical use.Type: GrantFiled: April 18, 2006Date of Patent: August 10, 2010Assignee: sanofi-aventis Deutschland GmbHInventors: Manfred Schudok, Sven Ruf, Hans Matter, Volkmar Wehner, Reinhard Kirsch, Petra Lennig
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Patent number: 7758861Abstract: The present invention discloses dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions. The compounds of the present invention may contain either a mixture of Type 1 and Type 2 agents or a single entity that integrates both units in the same molecules. The compounds are designed to produce both Type 1 and Type 2 phototherapeutic effect at once using dual wavelength light source that will produce singlet oxygen and free radicals at the lesion of interest.Type: GrantFiled: March 21, 2006Date of Patent: July 20, 2010Assignee: Mallinckrodt Inc.Inventors: Raghavan Rajagopalan, Samuel I. Achilefu, Joseph E. Bugaj, Richard D. Dorshow
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Publication number: 20100179176Abstract: The present invention relates to a V3 antagonist for use in the treatment of chronic pain, in particular neuropathic pain.Type: ApplicationFiled: December 13, 2007Publication date: July 15, 2010Inventor: Inga Neumann
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Publication number: 20100172623Abstract: A compound containing a crosslinkable moiety, a curable prepolymer, a blend, and a polymer sheet obtained therefrom, and an optical waveguide for optical interconnection. The compound is represented by the formula below: Ar—H wherein Ar includes a crosslinkable moiety at one end, a moiety selected from the group consisting of —O—, —S—, —COO—, —CO—, —COS—, —SO2—, and —NH—, and one or two repeating units selected from the group consisting of the following repeating units: wherein A in the repeating unit is carbon or nitrogen, and X is hydrogen or halogen. At least one of the core and the cladding in the optical waveguide includes the polymer sheet.Type: ApplicationFiled: December 9, 2009Publication date: July 8, 2010Applicant: ELECTRONICS AND TELECOMMUNICATIONS RESEARCH INSTITUTEInventors: Seung Koo PARK, Jung Jin Ju, Suntak Park, Jong-Moo Lee, Min-Su Kim, Jin Tae Kim, Joong-Seon Choe
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Publication number: 20100173908Abstract: The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine ureas of formula (I). Wherein R, R1, R2, R3, R4 and R5 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 ureas 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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PRO-DRUGS OF NSAIAS WITH VERY HIGH SKIN AND MEMBRANES PENETRATION RATES AND THEIR NEW MEDICINAL USES
Publication number: 20100172960Abstract: The novel positively charged pro-drugs of NSAIAs in the general formulas (1, 2a, 2b, 2c, or 2d) “Structure 1, 2a, 2b, 2c, or 2d” were designed and synthesized. The compounds of the general formulas (1, 2a, 2b, 2c, or 2d) “Structure 1, 2a, 2b, 2c, or 2d” indicated above can be prepared from metal salts, organic base salts, or immobilized base salts of NSAIAs with suitable halide compounds. The positively charged amino groups in the pro-drugs in this invention largely increase the solubility of the drugs in water and will bond to the negative charge on the phosphate head group of membrane. Thus, the local concentration of the outside of the membrane or skin will be very high and will facilitate the passage of these pro-drugs from a region of high concentration to a region of low concentration. This bonding will disturb the membrane a little bit and may make some room for the lipophilic portion of the pro-drug.Type: ApplicationFiled: June 4, 2007Publication date: July 8, 2010Inventors: Chongxi Yu, Lina Xu -
Patent number: 7745473Abstract: There is provided a novel pyrrole-imidazole polyamide compound for alkylating the specific base sequence of DNA, the polyamide compound being capable of being synthesized through fewer reaction steps than known hybrid molecules and having a combination of a high reactivity in DNA alkylation and the ability to recognize a sequence. Furthermore, there is provided an alkylating agent and a molecule serving as a drug, the alkylating agent and the molecule containing the polyamide compound.Type: GrantFiled: March 10, 2005Date of Patent: June 29, 2010Assignee: Kyoto UniversityInventors: Hiroshi Sugiyama, Toshikazu Bando
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Patent number: 7737293Abstract: An amide is formed by reacting an ?-ketoacid or salt thereof in a decarboxylative condensation reaction with an amine or salt thereof comprising a nitrogen covalently bound to an atom selected from oxygen, nitrogen, and sulfur. The amide bond is formed between the ?-carbon of the ketoacid and the nitrogen of the amine. The ?-ketoacid can be formed using a novel sulfur reagent.Type: GrantFiled: November 10, 2008Date of Patent: June 15, 2010Assignee: Regents of the University of CaliforniaInventors: Jeffrey W. Bode, Ryan M. Fox
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Patent number: 7718691Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: October 3, 2006Date of Patent: May 18, 2010Assignee: Schering CorporationInventors: Srikanth Venkatraman, F. George Njoroge, Melissa L. Blackman, Wanil Wu, Latha G. Nair, Ashok Arasappan, Stephane L. Bogen, Kevin X. Chen, Mousumi Sannigrahi, Frank Bennett, Viyyor M. Girijavallabhan
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Publication number: 20100120749Abstract: The present invention is related to tetrahydroindole derivatives of Formula (I), pharmaceutical composition thereof, methods of preparation thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: ApplicationFiled: March 28, 2008Publication date: May 13, 2010Applicant: GENKYO TEX SAInventors: Patrick Page, Mike Orchard, Laeticia Fioraso-Cartier, Bianca Mottironi
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Publication number: 20100113777Abstract: A compound, or its salt, or a solvate thereof having a cPLA2 inhibiting activity having the formula (I): or a pharmaceutical composition, cPLA2 inhibitor and inhibitors of various lipid mediator production containing the same as active ingredients.Type: ApplicationFiled: March 28, 2008Publication date: May 6, 2010Applicant: Asubio Pharma Co., Ltd.Inventors: Toshiyuki Tomoo, Takashi Nakatsuka, Yasuhiro Hayashi, Toyoko Katayama
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Patent number: 7705023Abstract: There is provided a compound of formula: (I), wherein X, R1, R2, R3, R4, R5 and R6 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of microsomal prostaglandin E synthase-1 is desired and/or required, and particularly in the treatment of inflammation.Type: GrantFiled: June 17, 2005Date of Patent: April 27, 2010Assignee: Biolipox ABInventors: Kristofer Olofsson, Benjamin Pelcman, Ivars Kalvins, Edgars Suna, Vita Ozola, Martins Katkevics
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Patent number: 7691894Abstract: The present invention provides a VLA-4 inhibitor having high water-solubility and excellent long-term stability; i.e., sodium trans-4-[1-[2,5-dichloro-4-[(1-methyl-1H-3-indolylcarbonyl)amino]phenylacetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylate pentahydrate.Type: GrantFiled: July 23, 2004Date of Patent: April 6, 2010Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Makoto Ono, Shigeru Noguchi
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Publication number: 20100081610Abstract: The present invention relates to ?-hydroxy and amino substituted carboxylic acids, which act as matrix metalloprotease inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for the synthesis of and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase using the compounds.Type: ApplicationFiled: August 21, 2007Publication date: April 1, 2010Inventors: Viswajanani J. Sattigeri, Venkata P. Palle, Manoj Kumar Khera, Ranaheer Reddy, Manoj Kumar Tiwari, Ajay Soni, Abdul Rehman Abdul Rauf, Sony Joseph, Arpita Musib, Sunanda G. Dastidar, Punit Kumar Srivastava
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Patent number: 7687504Abstract: A compound of the following formula: wherein R1 R2, R3, R4, R5, R6, W, X, Y, Z, m, n, and p are as defined herein. This invention also covers methods for inhibiting dipeptidyl peptidase IV or VIII, or treating Type II diabetes with such a compound.Type: GrantFiled: March 9, 2005Date of Patent: March 30, 2010Assignee: National Health Research InstitutesInventors: Weir-Torn Jiaang, Xin Chen, Su-Ying Wu, Yu-Sheng Chao, Hsing-Pang Hsieh
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Patent number: 7683057Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.Type: GrantFiled: December 28, 2007Date of Patent: March 23, 2010Assignee: Tyrogenex, Inc.Inventors: Congxin Liang, Ming Qi, Shu Gao, Zhigang Li
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Patent number: 7683068Abstract: The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: GrantFiled: June 23, 2006Date of Patent: March 23, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Jinlong Jiang, Robert J. DeVita, Sanjeev Kumar, Sander G. Mills, Richard A. Tschirret-Guth
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Patent number: 7678790Abstract: Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 23, 2005Date of Patent: March 16, 2010Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles Marlowe
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Publication number: 20100063088Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: ApplicationFiled: November 17, 2009Publication date: March 11, 2010Inventors: Jill E. WOOD, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
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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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Publication number: 20100056521Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.Type: ApplicationFiled: April 10, 2008Publication date: March 4, 2010Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
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Patent number: 7671141Abstract: Disclosed herein are second order nonlinear optic polyimide polymers comprising repeating units represented by the formula: wherein each of the substituents is given the definition as set forth in the Specification and Claims. Also disclosed are the preparation processes of these polymers, chromophore-forming compounds for synthesis of these polymers, and the intermediate polymers thereof. The second order nonlinear optic polyimide polymers of formula (I) may be used in the manufacture of electro-optic (EO) devices, such as electro-optic waveguide devices.Type: GrantFiled: June 28, 2006Date of Patent: March 2, 2010Assignee: National Sun Yat-Sen UniversityInventors: Tzu-Chien Hsu, Chien-Fan Chen, Shou-Shiun Wu
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Patent number: 7670512Abstract: Disclosed herein are second order nonlinear optic polyimide polymers comprising repeating units represented by the formula: wherein each of the substituents is given the definition as set forth in the Specification and Claims. Also disclosed are the preparation processes of these polymers, chromophore-forming compounds for synthesis of these polymers, and the intermediate polymers thereof. The second order nonlinear optic polyimide polymers of formula (I) may be used in the manufacture of electro-optic (EO) devices, such as electro-optic waveguide devices.Type: GrantFiled: June 28, 2006Date of Patent: March 2, 2010Assignee: National Sun Yat-Sen UniversityInventors: Tzu-Chien Hsu, Chien-Fan Chen, Shou-Shiun Wu
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Patent number: 7662995Abstract: 1-Phenylalkanecarboxylic acid derivatives, the processes for the preparation thereof and the use thereof in the treatment and/or prevention of neurodegenerative diseases such as Alzheimer's disease.Type: GrantFiled: February 19, 2004Date of Patent: February 16, 2010Assignee: Chiesi Farmaceutici S.p.A.Inventors: Luca Raveglia, Ilaria Peretto, Stefano Radaelli, Bruno Pietro Imbimbo, Andrea Rizzi, Gino Villetti
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Publication number: 20100035862Abstract: The invention relates to aza-cyclic-indole-2-carboxamide derivatives, compositions comprising such compounds, and methods of preventing or treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: June 24, 2009Publication date: February 11, 2010Applicant: ABBOTT LABORATORIESInventors: Murali Gopalakrishnan, Jianguo Ji, Chih-Hung Lee, Tao Li, Kevin B. Sippy
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Publication number: 20100016400Abstract: The present invention generally relates to muscarinic receptor antagonists, which are useful for treating various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to processes for preparing compounds described herein, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors.Type: ApplicationFiled: November 18, 2005Publication date: January 21, 2010Inventors: Naresh Kumar, Mohammad Salman, Kirandeep Kaur, Anita Mehta, Sudershan K. Arora, Anita Chugh
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Patent number: 7635694Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: February 24, 2005Date of Patent: December 22, 2009Assignee: Schering CorporationInventors: Stephane L. Bogen, Weidong Pan, Sumie Ruan, F. George Njoroge
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Publication number: 20090306124Abstract: The present invention relates to a compound of formula (I) wherein R1 is H, C1-C6-alkyl, phenyl-C1-C4-alkyl or phenyl, R2 is a phenyl group which is substituted with 2 or 3 C1-C6-alkoxy groups and R3 is indolyl or azaindolyl which may carry one or two substituents independently selected from C1-C6-alkyl, C1-C6-alkoxy, phenyl, OH, halogen, NH2, C1-C6-alkylamino, di-C1-C6-alkylamino, heteroaryl with 5 or 6 ring atoms containing 1 or 2 heteroatoms which are independently selected from O, N, and S and heterocyclyl with 5 or 6 ring atoms containing 1 or 2 heteroatoms which are independently selected from O, N, and S and the physiologically acceptable salts thereof as well as the physiologically acceptable solvates of the compounds of formula 1 and of the salts thereof. The compounds of formula (I) are suitable for controlling angiogenesis.Type: ApplicationFiled: December 7, 2005Publication date: December 10, 2009Applicant: Johannes Gutenberg-Universitat MainzInventors: Gerd Dannhardt, Christian Peifer, Stanislav Plutizki, Jan-Peter Kramb
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Publication number: 20090304631Abstract: The invention provides compounds that inhibit a viral protease enzyme of the hepatitis C virus (HCV). The compounds are adapted for treatment of a HCV infection in a patient with the disease. The compounds include analogs of tripeptides and tetrapeptides that resemble the viral protease substrate. The invention also provides pharmaceutical compositions and combinations, methods of preparation of the compounds, and methods of treatment of patients afflicted with HCV using the compounds.Type: ApplicationFiled: January 25, 2007Publication date: December 10, 2009Inventors: David Alan Campbell, Michael E. Hepperle, Juan Manuel Betancort, David T. Winn
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Publication number: 20090297473Abstract: Compounds of a certain formula 1, in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, as well as salts thereof are novel effective HDAC inhibitors.Type: ApplicationFiled: September 8, 2006Publication date: December 3, 2009Applicant: Nycomed GmbHInventors: Thomas Maier, Thomas Beckers, Rolf-Peter Hummel, Martin Feth, Matthias Müller, Thomas Bär
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Publication number: 20090291998Abstract: The present invention provides compounds having formula (1): wherein R1-R6, A, J, D, A, G, Q, w, x, y, and z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of cancer and/or inflammatory disorders, and more generally as proteasome inhibitors.Type: ApplicationFiled: March 3, 2009Publication date: November 26, 2009Inventors: Sergei Agoulnik, Kozo Akasaka, Francis Fang, Jean-Christophe Harmange, Lynn Hawkins, Yimin Jiang, Charles Johannes, Xiang-Yi Li, Pamela McGuinness, Erin A. Murphy, Shawn Schiller, Mary Vermeulen, Jiayi Wu