Ring Chalcogen In The Bicyclo Ring System Patents (Class 514/260.1)
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Publication number: 20110082136Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: ApplicationFiled: June 8, 2009Publication date: April 7, 2011Inventors: Michelle Machacek, Gabriela de Almeida, Jonathan B. Grimm, Rachel N. MacCoss, Eric Romeo, Tony Siu, Catherine White, Kevin Wilson
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Publication number: 20110082157Abstract: The invention relates to 5-HT receptor antagonists. Novel piperidinylamino-thieno [2,3-d] pyrimidine compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as pulmonary arterial hypertension, migraine, hypertension, disorders of the gastrointestinal tract, restenosis, asthma, obstructive airway disease, prostatic hyperplasia and priapism, anxiety, depression, schizophrenia, neural injury and stroke. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also provided.Type: ApplicationFiled: June 8, 2010Publication date: April 7, 2011Inventors: Dale S. Dhanoa, Oren Becker, Silvia Noiman, Sekar A. Reddy, Srinivasa Rao Cheruku, Rosa E. Mele'ndez, Anurag Sharadendu, Dongli Chen, Yael Marantz, Sharon Shacham, Alexander Heifetz, Boaz Inbal, Venkitasamy Kesavan, Shay Bar-Haim
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Publication number: 20110082158Abstract: Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed having the general Formula II: These compounds are useful in methods for treating cancer, selectively targeting cancerous cells via the proton coupled folate transporter, folate receptor alpha, and/or folate receptor beta pathways, inhibiting GARFTase and/or other folate metabolizing enzymes in cancerous cells, and selectively targeting activated macrophages in a patient having an autoimmune disease, such as rheumatoid arthritis.Type: ApplicationFiled: October 12, 2010Publication date: April 7, 2011Inventors: Aleem Gangjee, Larry H. Matherly
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Patent number: 7915267Abstract: The present invention provides a novel amide compound represented by the following formula, which has a matrix metalloproteinase inhibitory activity and is useful as a pharmaceutical agent. wherein each symbol is as defined in the specification.Type: GrantFiled: October 27, 2006Date of Patent: March 29, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Hiroshi Nara, Akira Kaieda, Kenjiro Sato, Jun Terauchi
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Publication number: 20110065715Abstract: The present invention provides a method for identifying compounds which modulate the interaction of Nogo and Nogo receptor (NgR). The present invention also provides compounds that modulate the interaction of Nogo and Nogo receptor (NgR), the use of such compounds and compositions in the treatment or amelioration of conditions diseases or disorders, such as spinal cord injury, traumatic brain injury, stroke, multiple sclerosis, ALS, Huntington's disease, Alzheimer's disease, Parkinson's disease, epilepsy, Schizophrenia or schizoaffective disorders.Type: ApplicationFiled: November 26, 2008Publication date: March 17, 2011Applicant: Yale UniversityInventors: Stephen M. Strittmatter, Erik Gunther
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Publication number: 20110065676Abstract: The present invention is directed to a pharmaceutical composition comprising an effective amount of at least one PAR1 antagonist, at least one NAR agonist, optionally, an effective amount of at least one cardiovascular agent, and, optionally, a pharmaceutically acceptable carrier. The present invention also provides for the use of theses pharmaceutical compositions to treat various diseases associated with thrombosis.Type: ApplicationFiled: June 22, 2010Publication date: March 17, 2011Applicant: Schering CorporationInventors: Michael Sidney Perelman, Madhu Chintala
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Publication number: 20110065714Abstract: This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: March 17, 2011Applicant: Shire LLCInventors: Bernard Golding, Peter Cicala, Richard Franklin, Kim Hirst
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Publication number: 20110065703Abstract: The present invention includes a group of chemical compounds useful as modulators of calcium ion (Ca2+) channels, especially for T-type, N-Type and L-type channels. The present invention also includes pharmaceutical compositions comprising these calcium ion channel modulating agents and methods of using these calcium ion channel modulating agents for the treatment diseases and conditions associated with the calcium ion channels.Type: ApplicationFiled: March 12, 2008Publication date: March 17, 2011Inventor: Jay Jie-Qiang Wu
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Patent number: 7906513Abstract: The present invention relates to novel hydrazide-containing compounds of Formula I or Formula II, including pharmaceutically acceptable salts, esters, or prodrugs thereof which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: April 26, 2007Date of Patent: March 15, 2011Assignee: Enanta Pharmaceuticals, Inc.Inventors: Joel D. Moore, Eric L. Elliott, Yat Sun Or, Zhe Wang
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Patent number: 7902203Abstract: The present invention provides an HCV polymerase inhibiting compound having the formula (I) and a composition comprising a therapeutically effective amount of said compound. The present invention also provides a method for inhibiting hepatitis C virus (HCV) polymerase, a method for inhibiting HCV viral replication, and a method for treating or preventing HCV infection. Processes for making said compounds, and synthetic intermediates employed in said processes, are also provided.Type: GrantFiled: October 31, 2003Date of Patent: March 8, 2011Assignee: Abbott Laboratories, Inc.Inventors: John K. Pratt, David A. Betebenner, Pamela L. Donner, Brian E. Green, Dale J. Kempf, Keith F. McDaniel, Clarence J. Maring, Vincent S. Stoll, Rong Zhang, Hui-Ju Chen, William J. Flosi, Larry L. Klein, Allan C. Krueger, Dachun Liu, Darold L. Madigan, Laura M. Maymon, Todd W. Rockway, Kent D. Stewart, Ming C. Yeung, Qinghua Xie
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Publication number: 20110052536Abstract: Briefly described, embodiments of this disclosure include compositions, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of treating HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, methods of treating liver fibrosis in a host, and the like.Type: ApplicationFiled: September 18, 2008Publication date: March 3, 2011Inventors: Shirit Einav, Jeffrey S. Glenn, Robert McDowell, Wenjin Yang, Hadas Dvory-Sobol
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Publication number: 20110046165Abstract: Chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with P13 kinase activity are described herein.Type: ApplicationFiled: January 5, 2009Publication date: February 24, 2011Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Katrina Chan, Christian Rommel, Liansheng Li
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Publication number: 20110046096Abstract: The invention relates to the novel dihydrothienopyrimidine sulfoxides of formula (I) and to the pharmacologically acceptable salts thereof, wherein X represents SO or SO2, preferably however SO, and wherein R3, R4, R4?, R5, R6 and R7 are defined as in claim 1. The invention also relates to pharmaceutical compositions containing said compounds. The novel dihydrothienopyrimidine sulfoxides are suitable for use in the treatment of respiratory or gastrointestinal disorders or diseases, inflammatory diseases of the joints, the skin or the eyes, diseases of the peripheral or central nervous system or cancers.Type: ApplicationFiled: October 16, 2008Publication date: February 24, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pascale Pouzet, Christoph Hoenke, Peter Nickolaus, Rolf Goeggel, Thomas Fox, Dennis Fiegen, Klaus Klinder
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Publication number: 20110046163Abstract: Furanopyrimidine cannabinoid analog compounds of the formula I are disclosed. The compounds are useful to modify the activity of CB1 and CB2 receptors and treat conditions mediated by these receptors.Type: ApplicationFiled: August 20, 2010Publication date: February 24, 2011Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
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Patent number: 7893085Abstract: The invention relates to azabenzothiophenyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azabenzothiophenyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: GrantFiled: August 20, 2007Date of Patent: February 22, 2011Assignee: Genentech, IncInventors: Pascal Pierre Savy, Stephen Price, Hazel Joan Dyke, John Gary Montana, Karen Williams, Mark S. Stanley, Liang Bao
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Publication number: 20110028420Abstract: A method is disclosed for treating and inducing the regression of established atherosclerotic plaques. A method is disclosed for treating asthma, including treatment of an ongoing asthma attack. In both cases, treatment with PARP inhibitors, such as the PARP inhibitor TIQ-A (Thieno[2,3-c]isoquinolin-5-one), can lead to regression of existing disease and symptoms.Type: ApplicationFiled: April 7, 2009Publication date: February 3, 2011Inventors: Hamid A. Boulares, Chetan P. Hans, Amarjit S. Naura
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Publication number: 20110028472Abstract: Novel thienopyrimidines of the formula (I), in which R1, R2 and X have the meanings indicated in Claim 1, are inhibitors of TGF-beta receptor kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: March 23, 2009Publication date: February 3, 2011Applicant: MERCK PATENT CESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Guenter Hoelzemann, Hartmut Greiner, Christiane Amendt, Frank Zenke
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Publication number: 20110028496Abstract: The present invention is concerned with deuterium-enriched pyrimidine compounds of formula I, their derivatives and pharmaceutically acceptable salts and methods of use thereof for the treatment of pulmonary arterial hypertension, pulmonary hypertension associated with chronic obstructive pulmonary disease (COPD), asthma, cystic fibrosis, hypertension, ischemic stroke, angina pectoris, congestive heart failure, arrhythmia, arterial fibrillation, Alzheimer's disease, cognition impairment, memory decline, and schizophrenia, and depression.Type: ApplicationFiled: August 3, 2010Publication date: February 3, 2011Inventor: Daljit Singh Dhanoa
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Publication number: 20110021541Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed.Type: ApplicationFiled: November 12, 2008Publication date: January 27, 2011Inventors: Stephen L. White, Fuqiang Ruan, Edward A. Kesicki, Eugene Thorsett, Francine Farouz
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Publication number: 20110021501Abstract: The invention relates to new piperidino-dihydrothienopyrimidines of formula 1, as well as pharmacologically acceptable salts thereof, wherein X is SO or SO2, but preferably SO, and wherein R1, R2, R3 and R4 may have the meanings given in claim 1, as well as pharmaceutical compositions which contain these compounds. These new piperidino-dihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers.Type: ApplicationFiled: October 16, 2008Publication date: January 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pascale Pouzet, Ralf Anderskewitz, Horst Dollinger, Dennis Fiegen, Thomas Fox, Rolf Goeggel, Christoph Hoenke, Domnic Martyres, Peter Nickolaus, Klaus Klinder
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Publication number: 20110002886Abstract: The invention provides compounds of formula (I), as described herein, or pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of formula (I) are useful as anti-viral agents and/or as anti-cancer agents.Type: ApplicationFiled: May 8, 2008Publication date: January 6, 2011Applicant: BIOCRYST PHARMACEUTICALS, INC.Inventors: Yarlagadda S. Babu, Pooran Chand
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Publication number: 20110003806Abstract: This invention provides compounds of formula IA or IB: wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: January 28, 2010Publication date: January 6, 2011Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company LimitedInventors: Masaaki Hirose, Steven P. Langston, Hirotake Mizutani, Stepan Vyskocil
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Publication number: 20100331329Abstract: The invention concerns a compound of the formula (I) wherein Ring A is heterocyclyl; m is 0-4 and each R1 is a group such as hydroxy, halo, trifluoromethyl and cyano; R2 is halo and n is 0-2; and each R4 is a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and R3 is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical condions mediated by histone deacetylase.Type: ApplicationFiled: September 10, 2010Publication date: December 30, 2010Applicant: ASTRAZENECA ABInventors: Elaine Sophie Elizabeth Stokes, Craig Anthony Roberts, Michael James Waring
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Publication number: 20100331348Abstract: Compounds of formula (I) wherein the substituents have the meanings assigned to them in claim 1, are useful as pesticides.Type: ApplicationFiled: July 10, 2008Publication date: December 30, 2010Applicants: SYNGENTA CROP PROTECTION, INC., SYNGENTA LIMITEDInventors: Patrice Selles, Eric Daniel Clarke, Alison Clare Elliot, Delphine Fawke, Ottmar Franz Hueter, Urs Mueller, Peter Renold, Sarah Targett, William Guy Whittingham
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Publication number: 20100331283Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: June 23, 2010Publication date: December 30, 2010Applicant: Array BioPharma Inc.Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Shelley Allen, Ellen Laird, Joseph P. Lyssikatos, John E. Robisnson, Christopher P. Corrette, Robert Kirk DeLisle, Walter C. Voegtti
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Publication number: 20100331305Abstract: Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).Type: ApplicationFiled: June 23, 2010Publication date: December 30, 2010Applicant: Genentech, Inc.Inventors: Philippe Bergeron, Frederick Cohen, Anthony Estrada, Michael F.T. Koehler, Cuong Ly, Joseph P. Lyssikatos, Zhonghua Pei, Wendy Lee, Xianrui Zhao
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Publication number: 20100324029Abstract: The invention encompasses 2-[4-(imidazolyl)-phenyl]vinyl-heterocycle derivatives which selectively attenuate production of Abeta(1-42) and are useful in the treatment of Alzheimer's disease. Pharmaceutical compositions and methods of use are also encompassed.Type: ApplicationFiled: February 5, 2008Publication date: December 23, 2010Inventors: Christian Fischer, Benito Munoz, Alexey A. Rivkin
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Patent number: 7855194Abstract: This invention is concerned with compounds of the formula wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: GrantFiled: March 15, 2007Date of Patent: December 21, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Alfred Binggeli, Andreas Christ, Hans-Peter Maerki, Rainer Eugen Martin
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Publication number: 20100298349Abstract: Compounds of formula (I) are A2B wherein R1 and R2 are independently selected from hydrogen, or optionally substituted CrC6 alkyl, C1-C6alkoxy-(C1-C6)-alkyl, C3-C8 cycloalkyl, aryl, heteroaryl, aryl-(C1-C6)-alkyl, or heteroaryl-(C1-C6) -alkyl; or R?1 and R2 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R3 and R4 are independently selected from hydrogen, or optionally substituted C1-C6 alkyl, C1-C6 alkoxy-(C1-C6)-alkyl, C3-C8 cycloalkyl, aryl, heteroaryl, aryl-(C1-C6)-alkyl, or heteroaryl-C1-C6)-alkyl; or R3 and R4 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R5 and R6 are independently selected from hydrogen, C1-C6 alkyl, aryl, aryl-(C1-C6)-alkyl, —NHR7—N(—R8)—R9, —NH—(C?O)—R10, —(C?O)—NH—R11, —(C?O)—O—R12, or halo; and R7, R8, R9, R10, R?11, and R12 are independently selected from C1-C6 alkyl, aryl, aryl-(C1-C6)-alkyl and heteroaryl.Type: ApplicationFiled: September 19, 2008Publication date: November 25, 2010Inventors: Allan Jordan, Simon Bedford, Klenke Burkhard, Ian Yule, Karinne Poullennec
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Publication number: 20100297097Abstract: The present invention relates to substituted triazole compounds of the formula (I): and salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for inhibiting SCD activity, such as diseases related to elevated lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome, skin disorders such as acne, diseases or conditions related to cancer and the treatment of symptoms linked to the production of the amyloid plaque-forming A?42 peptide such as Alzheimer's disease and the like.Type: ApplicationFiled: November 7, 2008Publication date: November 25, 2010Inventors: Anne Marie Jeanne Bouillot, Alain Laroze
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Publication number: 20100298331Abstract: The present invention relates to compounds according to formulae (IA) to (ID) and compositions that inhibit the activity of Hsp90. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: March 24, 2008Publication date: November 25, 2010Inventors: Chi-Wan Lee, Teresa Przewloka, Weiwen Ying, Minghu Song, Zhenjian Du, Kevin Foley, Dan Zhou, Shuzhen Qin
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Publication number: 20100298334Abstract: The present invention relates to N-(hetero)aryl-pyrrolidine derivatives of Formula I: which are JAK inhibitors, such as selective JAK1 inhibitors, useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.Type: ApplicationFiled: May 21, 2010Publication date: November 25, 2010Inventors: James D. Rodgers, Stacey Shepard, Argyrios G. Arvanitis, Haisheng Wang, Louis Storace, Beverly Folmer, Lixin Shao, Wenyu Zhu, Joseph Glenn
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Publication number: 20100292241Abstract: The present invention is directed to 3,5-disubstituted-1,3-oxazolidin-2-one derivatives which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neuro-ological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: January 14, 2009Publication date: November 18, 2010Applicant: Merck Sharp & Dohme Corp.Inventors: Edward Brnardic, Mark Fraley, Mark Layton, Robert Garbaccio
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Publication number: 20100286166Abstract: The present invention relates to the use of specific types of compounds acting as pharmacological chaperones having a stabilizing activity on the phenylalanine hydroxylase (PAH) enzyme for the prophylaxis and/or treatment of hyperphenylalaninemia (HPA) and phenylketonuria PKU) and diseases, disorders and conditions related thereto. Further, the present invention relates to pharmaceutical compositions containing the compounds according to the present invention as well as to methods of treatment of HPA, in particular, PKU and diseases, disorders and conditions related thereto.Type: ApplicationFiled: June 27, 2008Publication date: November 11, 2010Applicant: UNIVERSIDAD DE ZARAGOZAInventors: Ángel Pey Rodríguez, Aurora Martínez Ruiz, Javier Sancho Sanz, Nunilo Cremades Casasín, Adrián Velázquez Campoy, Ming Ying
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Publication number: 20100286174Abstract: Treatment of myocardial infarction to reduce infarct size and organogenesis is provided by administration of agents selected from the group consisting ofType: ApplicationFiled: May 18, 2010Publication date: November 11, 2010Applicant: Duke UniversityInventors: Jonathan S. Stamler, Howard A. Rockman
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Patent number: 7829570Abstract: The present application is directed to compounds of the formula (I) wherein the substituents are as defined herein, which are useful as kinase inhibitors.Type: GrantFiled: December 3, 2008Date of Patent: November 9, 2010Assignee: Abbott LaboratoriesInventors: Gavin C. Hirst, Andrew Burchat, Neil Wishart, David J. Calderwood, Michael R. Michaelides, Zhiqin Ji
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Publication number: 20100280050Abstract: The invention provides a method of treating or preventing fibrosis in a subject by administering a 5-HT modulator, e.g., a 5-HT2B modulator. In particular embodiments, the 5-HT modulator is a piperidinylamino-thieno[2,3-d]pyrimidine compound.Type: ApplicationFiled: September 4, 2008Publication date: November 4, 2010Inventors: Kimberley Gannon, Ohilip B. Graham
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Publication number: 20100273815Abstract: The present invention discloses novel compounds of the Formula (1), containing thieno-[2,3-d]pyrimidin-4(3H)-one moieties and pharmaceutically acceptable salts thereof, methods for preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds.Type: ApplicationFiled: September 5, 2008Publication date: October 28, 2010Inventors: Hanumant Bapurao Borate, Suleman Riyajsaheb Maujan, Sangmesher Prabhakar Sawargave, Sheerang Vidhyadhar Joshi, Sharangi Vaiude, Mohan Anand Chandavarkar
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Publication number: 20100273784Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides quinazolinone, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.Type: ApplicationFiled: April 9, 2010Publication date: October 28, 2010Applicant: Icagen, Inc.Inventors: Grant Andrew McNaughton-Smith, George Salvatore Amato, James Barnwell Thomas, JR.
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Patent number: 7820658Abstract: Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, Cancer: wherein R2 is a group of formula —(Ar1)m-(Alk1)P-(Z)r-(Alk 2)S-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk? and Alk 2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C?O)—, —(C?S)—, —SO2—, —C(?O)O—, —C(?O)NRA—, —C(?S)NRA—, —SO2NRA—, —NRAC(?O)_, —NRASO2- or —NRA—wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group.Type: GrantFiled: August 26, 2004Date of Patent: October 26, 2010Assignees: Vernalis (Cambridge) Limited, Cancer Research Technology Ltd., Institute Of Cancer ResearchInventors: Brian William Dymock, Martin James Drysdale, Christofe Fromont, Allan Jordan, Xavier Barril-Alonso
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Patent number: 7820631Abstract: A nucleoside analogue compound is provided which has a six-membered aromatic ring system, the aromatic ring system being substituted in the para position with an unbranched unsubstituted alkyl or alkoxy moiety, wherein the alkyl or alkoxy moiety, in total, has from 3 to 8 carbon atoms. This compound shows anti-vira1 activity, for example with respect to varicella zoster virus and can thus be used in therapeutic methods for the prophylaxis and treatment of viral infections such as varicella zoster virus.Type: GrantFiled: April 12, 2001Date of Patent: October 26, 2010Assignees: Rega Foundation, University College Cardiff Consultants LimitedInventors: Christopher McGuigan, Jan Balzarini
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Publication number: 20100267749Abstract: The invention relates to the novel 4,5,6-trisubstituted furo[2,3-d]pyrimidine derivatives of formula (I), to methods for their production, their use in the treatment and/or prophylaxis of diseases and their use in the production of drugs for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular diseases.Type: ApplicationFiled: November 3, 2008Publication date: October 21, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Thomas Lampe, Raimund Kast, Friederike Stoll, Joachim Schuhmacher
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Publication number: 20100261736Abstract: The present application relates to novel substituted bicyclic heteroaryl compounds, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.Type: ApplicationFiled: June 3, 2008Publication date: October 14, 2010Inventors: Thomas Lampe, Raimund Kast, Hartmut Beck, Friederike Stoll, Eva-Maria Becker, Mario Jeske, Joachim Schuhmacher
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Patent number: 7807684Abstract: Compounds having the structure: are HIV reverse transcriptase inhibitors, wherein A, X, Y, Z, R1 and R2 are defined herein. The compounds and their pharmaceutically acceptable salts 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, 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: July 17, 2006Date of Patent: October 5, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Sandeep A. Saggar, John T. Sisko, Thomas J. Tucker, Robert M. Tynebor, Dai-Shi Su, Neville J. Anthony
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Publication number: 20100249114Abstract: The present invention relates to the CGRP antagonists of general formula wherein A, X, D, E, G, M, Q and R1 to R3 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.Type: ApplicationFiled: February 25, 2010Publication date: September 30, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan Georg MUELLER, Klaus RUDOLF, Philipp LUSTENBERGER, Dirk STENKAMP, Alexander DREYER, Kirsten ARNDT, Henri DOODS, Gerhard SCHAENZLE, Marco SANTAGOSTINO, Fabio PALEARI
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Publication number: 20100249119Abstract: The present invention provides a heterocyclic compound having a strong Raf inhibitory activity, which is represented by the following formula wherein each substituent is as defined in the present specification, or a salt thereof.Type: ApplicationFiled: August 28, 2008Publication date: September 30, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masaaki Hirose, Masanori Okaniwa, Yoko Hayashi, Terufumi Takagi
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Patent number: 7799775Abstract: This invention provides pyrimidine derivatives represented by a formula, in the formula, ring A stands for carbocyclic group or heterocyclic group, X1 stands for hydrogen, lower alkyl, amino, etc., X2 stands for hydrogen or lower alkyl, Y stands for a direct bond or sulfur or nitrogen, n stands for an integer of 0-4, and Ar stands for a group of the following formula, or a salt thereof, which concurrently exhibit 5-HT1A agonistic activity and 5-HT3 antagonistic activity and are useful for therapy and treatments of diseases such as IBS. The invention furthermore provides a therapeutic method of IBS, characterized by having 5-HT1A agonistic activity and 5-HT3 antagonistic activity work simultaneously and cooperatively in vivo, which comprises either administering 5-HT3 antagonistic agent which concurrently exhibits 5-HT1A agonistic activity, or administering 5-HT1A agonistic agent and 5-HT3 antagonistic agent simultaneously, in sequence or at an interval.Type: GrantFiled: February 25, 2005Date of Patent: September 21, 2010Assignee: ASKA Pharmaceutical Co., Ltd.Inventors: Michitaka Sato, Teruaki Matsui, Akira Asagarasu, Hiroyuki Hayashi, Sei-ichi Araki, Satoru Tamaoki, Nobuyuki Takahashi, Yukinao Yamauchi, Yoshiko Yamamoto, Norio Yamamoto, Chisato Ogawa
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Publication number: 20100234399Abstract: An agent comprising, as an active ingredient, a xanthine oxidase inhibitor such as 2-[3-cyano-4-(4-fluorophenoxy)phenyl]-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-[3-cyano-4-(4-fluorophenoxy)phenyl]thiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-(3-cyano-4-phenoxyphenyl)thiazolo[5,4-d]pyrimidine, TMX-67, and FYX-051, which can be used as an agent for overcoming anti-cancer agent resistance.Type: ApplicationFiled: June 22, 2007Publication date: September 16, 2010Applicant: NIPPON CHEMIPHAR CO., LTD.Inventors: Masuharu Hirano, Tomio Yamakawa, Toshihisa Ishikawa, Hikaru Saito
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Publication number: 20100227853Abstract: Recombinant fission yeast cells and methods of using them are described, which provide for identification of chemical and biological inhibitors or activators of a target exogenous phosphodiesterase (PDE). The invention provides, in some aspects, compounds that inhibit cAMP PDE activity and compositions that include such compounds. The invention, in part, also includes methods of using cAMP PDE-inhibiting compounds in the treatment of cAMP PDE-associated diseases and/or disorders.Type: ApplicationFiled: April 17, 2009Publication date: September 9, 2010Applicant: Trustees of Boston CollegeInventors: Charles S. Hoffman, Frank Douglas Ivey, Arlene Wyman Petri
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Publication number: 20100227873Abstract: The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, esters, and tautomers thereof, wherein: Q is selected from the group consisting of: and L is selected from the group consisting of: pharmaceutically compositions comprising one or more compounds of formula (I), and methods of using the compounds of formula (I).Type: ApplicationFiled: April 30, 2010Publication date: September 9, 2010Inventors: Anandan Palani, Jing Su, Dong Xiao, Xianhai Huang, Ashwin U. Rao, Xiao Chen, Haiqun Tang, Jun Qin, Ying R. Huang, Robert G. Aslanian, Brian A. McKittrick, Syliva J. Degrado