Polycyclo Heterocyclic Ring System Containing Ring Nitrogen Patents (Class 548/181)
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Publication number: 20120010187Abstract: The invention provides FIG. 1 novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.Type: ApplicationFiled: March 16, 2010Publication date: January 12, 2012Applicant: University of Virginia Patent FoundationInventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. Macdonald, Thomas Eric Ballard, JR.
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Patent number: 8088770Abstract: The present application provides for a compound of Formula IV: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.Type: GrantFiled: July 3, 2008Date of Patent: January 3, 2012Assignee: Gilead Sciences, Inc.Inventors: Manoj C. Desai, Hon C. Hui, Hongtao Liu, Jianyu Sun, Lianhong Xu
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Publication number: 20110312935Abstract: There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A 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 a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.Type: ApplicationFiled: September 25, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Roland Pfau, Kirsten Arndt, Henri Doods, Norbert Hauel, Klaus Klinder, Raimund Kuelzer, Juergen Mack, Henning Priepke, Dirk Stenkamp
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Publication number: 20110312976Abstract: The present invention relates to a compound represented by formula (I): (wherein R, R2, R3 and R4 each independently represent a hydrogen or halogen atom; R5 and R6 each independently represent a hydrogen atom or lower alkyl or together represent oxo; X represents C(O) or the like; Y represents an oxygen atom or the like; Z represents a hydrogen atom or the like; R represents 5- or 6-membered heteroaryl having 1-3 hetero atoms selected from the group consisting of nitrogen, sulfur and oxygen atoms, contained within a ring, or the like) or to a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 9, 2010Publication date: December 22, 2011Applicant: MSD K.K.Inventors: Keisuke Arakawa, Teruyuki Nishimura, Yuichi Sugimoto, Hiroyuki Takahashi, Tadashi Shimamura
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Publication number: 20110312989Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: ApplicationFiled: June 17, 2011Publication date: December 22, 2011Inventors: Wenge Xie, Brian Herbert, Jianguo Ma, Truc Minh Nguyen, Richard Schumacher, Carla Maria Gauss, Ashok Tehim
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Publication number: 20110306592Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, X, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: ApplicationFiled: June 9, 2011Publication date: December 15, 2011Inventors: Xuqing Zhang, Zhihua Sui, James C. Lanter
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Publication number: 20110301155Abstract: The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like.Type: ApplicationFiled: June 18, 2008Publication date: December 8, 2011Inventors: Tsuneo Yasuma, Shigekazu Sasaki, Osamu Ujikawa, Yasufumi Miyamoto, Stephen L. Gwaltney, Sheldon Cao, Andy Jennings
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Patent number: 8071628Abstract: The invention is concerned with novel indazole derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used in the prevention or treatment of diseases which are modulated by L-CPT1 inhibitors.Type: GrantFiled: September 8, 2010Date of Patent: December 6, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
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Publication number: 20110294780Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: May 24, 2011Publication date: December 1, 2011Inventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
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Publication number: 20110275665Abstract: Compounds are provided for use with hexokinases that comprise: 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: July 18, 2011Publication date: November 10, 2011Applicant: TAKEDA SAN DIEGO, INC.Inventors: Sheldon X. Cao, Jun Feng, Stephen L. Gwaltney, David J. Hosfield, Robert J. Skene, Jeffrey A. Stafford, Mingnam Tang
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Publication number: 20110275630Abstract: Compounds having the formula: are useful for inhibiting protein kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: November 3, 2010Publication date: November 10, 2011Applicant: ABBOTT LABORATORIESInventors: Mark Matulenko, Tammie Jinkerson, Brian S. Brown, Wilfried Braje, Michael Curtin, Howard Robin Heyman, Victoria Scott, Karen Kage, Steven Cassar, Anil Vasudevan
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Patent number: 8044213Abstract: The invention is directed to compounds of formula (1) and pharmaceutically acceptable salts thereof, methods for the preparation thereof, and methods of use thereof.Type: GrantFiled: December 10, 2009Date of Patent: October 25, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Jianping Cai, Shaoqing Chen, Yi Chen, Xin-Jie Chu, Robert Alan Goodnow, Jr., Kang Le, Kin-Chun Luk, Steven Gregory Mischke, Peter Michael Wovkulich
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Publication number: 20110243850Abstract: Provided is a novel probe for a biological specimen for labelling by itself and clearly visualizing one of a specific cell and a specific cell organ in a living body, the probe having excellent spectral characteristics and exhibiting excellent storage stability. The probe for a biological specimen contains, as an active agent, at least one kind of compound represented by a general formula (I).Type: ApplicationFiled: December 24, 2009Publication date: October 6, 2011Applicant: CANON KABUSHIKI KAISHAInventors: Taichi Shintou, Takeshi Miyazaki, Masashi Hirose, Taketoshi Okubo, Kohei Watanabe, Tsuyoshi Nomoto, Toshio Tanaka, Yuhei Nishimura, Yasuhito Shimada, Norihiro Nishimura
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Publication number: 20110245263Abstract: The invention relates to heterocyclic derivatives of formula I wherein R, R1, A, B, D, M, L and n are as defined herein, or their physiologically compatible salts, their pharmaceutical compositions and their uses as SCD1 inhibitors.Type: ApplicationFiled: June 15, 2011Publication date: October 6, 2011Applicant: SANOFI-AVENTISInventors: Gerhard Zoller, Marc Dietrich Voss, Stefanie Keil, Andreas Herling, Hans Matter
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Patent number: 8030322Abstract: The present invention relates to compounds of formula (I) or salts thereof wherein A, X, R2, R4 and n are defined herein, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g., to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or to enhance cognition.Type: GrantFiled: April 24, 2007Date of Patent: October 4, 2011Assignee: Glaxo Group LimitedInventors: Barbara Bertani, Romano Di Fabio, Fabrizio Micheli, Alessandra Pasquarello, Luca Tarsi, Silvia Terreni
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Publication number: 20110237517Abstract: The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.Type: ApplicationFiled: September 16, 2009Publication date: September 29, 2011Inventors: Stephen M. Condon, Matthew G. Laporte
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Publication number: 20110224188Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: ApplicationFiled: November 20, 2008Publication date: September 15, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Antonio Jose del Moral Barbosa, Joerg Martin Benzien, Steven Richard Brunette, Zhidong Chen, Derek Cogan, Donghong A. Gao, Alexander Heim-Riether, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Rene Marc Lemieux, Weimin Liu, Bryan Mckibben, Craig Andrew Miller, Neil Moss, Matt Aaron Tschantz, Zhaoming Xiong, Hui Yu, Yang Yu
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Publication number: 20110224207Abstract: Methods of treating, preventing, and/or ameliorating a Flavivirus infection in a subject are disclosed. The methods comprise administering to the subject a therapeutically effective amount of a Flavivirus inhibitor, e.g., a Flavivirus serine protease inhibitor. These methods are useful in treating, preventing, and/or ameliorating Flavivurs infections such as, for example, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus.Type: ApplicationFiled: September 23, 2009Publication date: September 15, 2011Applicant: GEORGETOWN UNIVERSITYInventors: Radhakrishnan Padmanabhan, Nagarajan Pattabiraman, Niklaus Mueller, Kuppuswamy Nagarajan
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Publication number: 20110213158Abstract: It is an object of the present invention to provide the crystalline form of a thiazolidinedione compound, which is effective as a pharmaceutical ingredient for manufacturing a peroxisome proliferator-activated receptor (PPAR) activator and an anticancer pharmaceutical composition. The present invention relates to a crystalline form of a hydrate of 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H benzimidazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione dihydrochloride represented by the following formula (I).Type: ApplicationFiled: February 8, 2008Publication date: September 1, 2011Inventors: Hisaki Kajino, Yutaka Ikeuchi, Hiroshi Miyamoto, Eiji Numagami, Satoru Nihei
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N-(2-THIAZOLYL)-AMIDE DERIVATIVES FOR THE TREATMENT OF OBESITY, DIABETES AND CARDIOVASCULAR DISEASES
Publication number: 20110213000Abstract: The invention relates to the use of a compound of formula (I): its pharmaceutically acceptable salts, prodrugs and/or solvates, in the preparation of a medicinal product for the treatment of a disease presenting altered adiponectin levels or in which it is necessary to alter the adiponectin protein levels.Type: ApplicationFiled: August 1, 2008Publication date: September 1, 2011Applicant: ZELTIA, S.A.Inventors: Ana Martínez Gil, Mercedes Alonso Cascón, Gema Santamaría Núñez, Marta Martínez Díez, Javier López Ogalla -
Patent number: 8008332Abstract: Compounds are provided for use with hexokinases that comprise: 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: GrantFiled: May 25, 2007Date of Patent: August 30, 2011Assignee: Takeda San Diego, Inc.Inventors: Sheldon X. Cao, Jun Feng, Stephen L. Gwaltney, David J. Hosfield, Robert J. Skene, Jeffrey A. Stafford, Mingnam Tang
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Patent number: 8003806Abstract: The invention relates to compounds of the Formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X2, X4, X5 and X1 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of Formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of Formula 1.Type: GrantFiled: November 9, 2005Date of Patent: August 23, 2011Assignee: OSI Pharmaceuticals, LLCInventors: Jason Bloxham, Gary V. Borzillo, Eric William Collington, Shazia Sadiq, Colin Peter Sambrook Smith, Chris L. Waller, Graham M. Wynne
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Publication number: 20110200586Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: February 16, 2011Publication date: August 18, 2011Inventors: Gilles BIGNAN, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Publication number: 20110200587Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: February 16, 2011Publication date: August 18, 2011Inventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Publication number: 20110195986Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R4, R5, R3, R3a, W, D, R2a, R2b and R2c are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression, anxiety or intestinal inflammation, by administration of a therapeutically effective dose of a compound according to Formula I.Type: ApplicationFiled: October 8, 2009Publication date: August 11, 2011Inventors: Guohua Zhao, William N. Washburn, James J. Mignone
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Publication number: 20110189096Abstract: To provide a central nervous system tissue-labeling composition labeling the central nervous tissue system. Also, another object of the present invention is to provide a method for non-invasively labeling the central nervous tissue system. Further, another object of the present invention is to provide a screening method using the above central nervous system tissue-labeling composition. A central nervous system tissue-labeling composition containing, as an active ingredient, at least one of compounds represented by the general formula (1) or (7).Type: ApplicationFiled: April 12, 2011Publication date: August 4, 2011Applicant: CANON KABUSHIKI KAISHAInventors: Kohei Watanabe, Taichi Shintou, Tsuyoshi Nomoto, Takeshi Miyazaki, Mie Okano, Toshio Tanaka, Yuhei Nishimura, Yasuhito Shimada
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Publication number: 20110178075Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the ?7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: ApplicationFiled: March 7, 2011Publication date: July 21, 2011Inventors: Wenge XIE, Brian Herbert, Jianguo Ma, Truc Minh Nguyen, Richard Schumacher, Carla Maria Gauss, Ashok Tehim
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Publication number: 20110155241Abstract: The dye for a dye-sensitized solar cell, which dye is a compound classified into melocyanine dyes and has a structure in which an electron donor unit and an electron acceptor unit are connected with conjugated double bonds, provided by this invention, has excellent photoelectric conversion efficiency and excellent durability, and according to this invention, there can be provided a semiconductor electrode sensitized by the dye and a dye-sensitized solar cell using the semiconductor electrode.Type: ApplicationFiled: August 5, 2009Publication date: June 30, 2011Inventors: Masakazu Takata, Koichi Sumioka, Takaaki Kozai
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Publication number: 20110155249Abstract: A photoelectric conversion device capable of improving conversion efficiency is provided. The photoelectric conversion device includes a work electrode, an opposed electrode, and an electrolyte-containing layer. In the work electrode, a metal oxide semiconductor layer supporting a dye is provided. The dye contains a cyanine compound that has a methine chain, an indolenine skeleton bonded with both ends of the methine chain, and anchor groups introduced to a nitrogen atom included in the indolenine skeleton. Electron injection efficiency to the metal oxide semiconductor layer is improved, and the dye is hardly exfoliated from the metal oxide semiconductor layer.Type: ApplicationFiled: September 9, 2009Publication date: June 30, 2011Applicants: TDK CORPORATION, ADEKA CORPORATIONInventors: Junji Tanabe, Atsushi Monden, Masahiro Shinkai, Mitsuhiro Okada, Toru Yano, Yohei Aoyama, Yusuke Kubota
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Publication number: 20110150864Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: December 16, 2010Publication date: June 23, 2011Inventors: Gilles BIGNAN, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Publication number: 20110144153Abstract: [Problems] A compound, which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy, is provided. [Solving Means] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic activity, and confirmed that the amide compound of the present invention has an EP4 receptor antagonistic activity, thereby completing the present invention. The amide compound of the present invention has an EP4 receptor antagonistic activity, and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating various EP4-related diseases, for example, chronic renal failure and/or diabetic nephropathy, and the like.Type: ApplicationFiled: May 12, 2009Publication date: June 16, 2011Applicant: Astellas Pharma Inc.Inventors: Eisuke Nozawa, Ryotaro Ibuka, Kazuhiro Ikegai, Keisuke Matsuura, Tatsuya Zenkoh, Ryushi Seo, Susumu Watanuki, Michihito Kageyama
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Publication number: 20110135691Abstract: The present invention is directed to immune adjuvants containing IAP inhibitors, including Smac mimetics. The invention further provides pharmaceutical compositions and vaccines containing an IAP inhibitor and an antigen. Methods of enhancing an immune response by administration of an IAP inhibitor, methods of treating or preventing cancer, methods of treating or preventing infections, methods of treating autoimmune disorders, and methods of potentiating cytokine or antibody production are also provided.Type: ApplicationFiled: May 14, 2009Publication date: June 9, 2011Inventors: Leigh Zawel, Christopher S. Straub, Brant G. Firestone, Glenn Dranoff, Michael Dougan
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Publication number: 20110135594Abstract: A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: ApplicationFiled: July 14, 2009Publication date: June 9, 2011Inventors: Michael Graupe, Chandrasekar Venkataramani
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Publication number: 20110124636Abstract: The invention relates to novel 2-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: December 28, 2007Publication date: May 26, 2011Applicant: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen, Daniel Trachsel
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Publication number: 20110124637Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: July 2, 2009Publication date: May 26, 2011Inventors: Chi B Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
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Publication number: 20110124692Abstract: Thiazolidinedione compound crystalline forms useful as a bulk material for the manufacture of a peroxisome proliferator-activated receptor (PPAR) ? activator or an anticancer pharmaceutical composition are provided, which are hydrate crystalline forms of 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H-benzimi dazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione represented by Formula (I) below and of its dihydrochloride.Type: ApplicationFiled: July 30, 2009Publication date: May 26, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Hisaki Kajino, Yutaka Ikeuchi, Eiji Numagami, Satoru Nihei
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Patent number: 7947683Abstract: The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or cognition impairment.Type: GrantFiled: April 12, 2006Date of Patent: May 24, 2011Assignee: Glaxo Group LimtedInventors: Giorgio Bonanomi, Anna Checchia, Elettra Fazzolari, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Silvia Terreni
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Patent number: 7947713Abstract: The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.Type: GrantFiled: October 30, 2007Date of Patent: May 24, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Henry Joseph Breslin, Hans Louis Jos De Winter, Michael Joseph Kukla
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Publication number: 20110112299Abstract: Provided are a tetracyclic compound represented by the formula (I): [in the formula (I), the formula (A) represents a benzene ring or the like, X represents CH or a nitrogen atom, Q represents —O— or the like, R1, R2, and R3 may be the same or different and each represent a hydrogen atom or the like, l, m, and n each represent an integer from one to the maximum substitutable number of substituents, and R4 and R5 may be the same or different and each represent a hydrogen atom or the like], or a pharmaceutically acceptable salt thereof, and the like.Type: ApplicationFiled: July 3, 2009Publication date: May 12, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Junichiro Yamamoto, Kiyotoshi Mori, Tomohiro Era, Yoshisuke Nakasato, Kenji Uchida
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Publication number: 20110105491Abstract: The invention relates to thiazolidine derivatives of the formula (I) wherein A, B, and R1 are as described in the description, to salts, especially pharmaceutically acceptable salts, of such compounds and to their use as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: July 7, 2009Publication date: May 5, 2011Inventors: Hamed Aissaoui, Christoph Boss, Julien Hazemann, Ralf Koberstein, Romain Siegrist, Thierry Sifferlen
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Publication number: 20110105573Abstract: The invention relates to benzimidazole acetic acid compounds which function as antagonists of the Chemoattractant Receptor-homologous molecule expressed on T-Helper type 2 cells (CRTH2) receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.Type: ApplicationFiled: June 8, 2010Publication date: May 5, 2011Inventors: Youssef L. Bennani, Lawrence Nathan Tumey, Elizabeth Ann Gleason, Michael Joseph Robarge
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Publication number: 20110098297Abstract: The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like. The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is defined in the specification, or a salt thereof or a prodrug thereof.Type: ApplicationFiled: April 9, 2009Publication date: April 28, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Tsuneo Yasuma, Nobuyuki Takakura
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Publication number: 20110092555Abstract: A compound which is 5-{4-[(6-methoxy-1-methyl-1H-benzimidazol-2-yl)methoxy]benzyl}thiazolidine-2,4-dione hydrochloride, in crystal form wherein a powder x-ray diffraction pattern obtained by irradiation with a Cu K? line shows main peaks at interplanar spacings d=14.29, 7.12, 5.34, 4.97, 4.74, 3.95, 3.85, 3.75, 3.55, 3.51, 3.15, 2.84, 2.76, 2.52 and 2.37.Type: ApplicationFiled: December 14, 2010Publication date: April 21, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Yoshitaka Nakamura, Chiharu Satoh, Hiroshi Miyamoto, Hisaki Kajino
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Publication number: 20110086834Abstract: Selected compounds are effective for prophylaxis and treatment of inflammation and inflammatory disorders, such as NIK-mediated disorders. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, inflammation and the like.Type: ApplicationFiled: June 26, 2009Publication date: April 14, 2011Applicant: AMGEN INC.Inventors: Guoqing Chen, Timothy D. Cushing, Paul Faulder, Benjamin Fisher, Xiao He, Kexue Li, Zhihong Li, Wen Liu, Lawrence R. Mcgee, Vatee Pattaropong, Jennifer L. Seganish, Youngshook Shin, Zhulun Wang
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Publication number: 20110071141Abstract: Condensed-ring aryl compounds of formula (I) and use of the same as a agrochemical for controlling noxious organisms wherein (X)mQ, A, R1, (Y)n and the grouping —W1—W2—W3—W4— are as defined herein.Type: ApplicationFiled: March 13, 2009Publication date: March 24, 2011Inventors: Tetsuya Murata, Yasushi Yoneta, Jun Mihara, Kei Domon, Mamoru Hatazawa, Koichi Araki, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara, Ulrich Görgens, Arnd Voerste, Angela Becker, Eva-Maria Franken, Klaus-Helmut Müller
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Publication number: 20110071195Abstract: The present invention provides compounds of formula (I), as well as pharmaceutical acceptable salt thereof, wherein R1 to R7 have the significance given herein. The compounds are useful in the treatment of prophylaxis of diseases that are related to AMPK regulation.Type: ApplicationFiled: September 14, 2010Publication date: March 24, 2011Inventors: Li Chen, Lichun Feng, Mengwei Huang, Jia Li, Fajung Nan, Tao Pang, Lifang Yu, Mei Zhang
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Publication number: 20110065685Abstract: The present invention provides novel compounds of Formula (I) which are CB2 selective ligands useful for the treatment of pain.Type: ApplicationFiled: June 14, 2010Publication date: March 17, 2011Applicant: Abbott LaboratoriesInventors: Jennifer M. Frost, Karin Tietje, Michael J. Dart, Michael D. Meyer
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Patent number: 7902369Abstract: The present invention provides the compounds represented by formula (I): (I) or pharmaceutical salts thereof, wherein: X1 represents oxygen atoms and the like, X2 represents nitrogen atoms and the like, X3 represents nitrogen atoms and the like, X4 represents nitrogen atoms and the like, R1 represents formula (II-1): wherein X5 represents sulfur atoms and the like, A1 represents carbon atoms and the like, A2 represents nitrogen atoms and the like and A ring represents phenyl group and the like, having mGluR1 inhibiting effect, and being usefull for preventing or treating convulsion, acute pain, inflammatory pain, chronic pain, brain disorder such as cerebral infarction or transient ischemick attack, psychotic disorder such as schizophrenia, anxiety, drug dependence, Parkinson's disease, or gastrointestinal disorder.Type: GrantFiled: March 7, 2005Date of Patent: March 8, 2011Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yukari Hirata, Satoru Ito, Hiroshi Kawamoto, Toshifumi Kimura, Yasushi Nagatomi, Hisashi Ohta, Akio Sato, Atsushi Satoh, Gentaroh Suzuki
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Publication number: 20110046388Abstract: It is an object of the present invention to provide the crystalline form of a thiazolidinedione compound, which is effective as a pharmaceutical ingredient for manufacturing a peroxisome proliferator-activated receptor (PPAR) activator and an anticancer pharmaceutical composition. The present invention relates to a crystalline form of a hydrate of 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H benzimidazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione dihydrochloride represented by the following formula (I).Type: ApplicationFiled: February 8, 2008Publication date: February 24, 2011Inventors: Hisaki Kajino, Yutaka Ikeuchi, Hiroshi Miyamoto, Eiji Numagami, Satoru Nihei
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Publication number: 20110046367Abstract: Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.Type: ApplicationFiled: November 1, 2010Publication date: February 24, 2011Applicant: President and Fellows of Harvard CollegeInventors: José A. Halperin, Amarnath Natarajan, Huseyin Aktas, Yun-Hua Fan, Han Chen