Ring Nitrogen Is Shared By The Cyclos Of The Bicyclo Ring System (e.g., Tetramisole, Etc.) Patents (Class 514/368)
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Publication number: 20120108576Abstract: The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1, R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections.Type: ApplicationFiled: November 30, 2011Publication date: May 3, 2012Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Suoming Zhang, Avinash Phadke, Cuixian Liu, Xiangzhu Wang, Jesse Quinn, Dawei Chen, Venkat Gadhachanda, Shouming Li, Milind Deshpande
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Publication number: 20120088771Abstract: This invention relates generally to the field of mineralization, and specifically to the role of TNAP in regulating the levels of extracellular inorganic pyrophosphate. The invention provides methods for modulating the activity of TNAP activity; methods for screening for modulators of TNAP activity; modulators of TNAP activity; and methods for treating pathologic conditions known of suspected to be affected by modulation of TNAP activity.Type: ApplicationFiled: October 11, 2011Publication date: April 12, 2012Inventor: Jose Luis Millan
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Patent number: 8138210Abstract: The present invention refers to new indanyl sulphonamide compounds with general formula (I), as well as to their preparation procedure, their application as medicine and the pharmaceuticals composition which they are made up of. The new compounds of formula I show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.Type: GrantFiled: August 18, 2006Date of Patent: March 20, 2012Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Maria De Las Ermitas Alcalde-Pais, Maria De Les Neus Mesquida-Estevez, Sara Lopez-Perez, Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal
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Patent number: 8138182Abstract: The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).Type: GrantFiled: September 24, 2009Date of Patent: March 20, 2012Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Akira Hatayama, Hiroshi Tsuruta, Yasuo Ochi, Haruo Imawaka, Kazuyuki Ohmoto
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Patent number: 8106215Abstract: The invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as orexin receptor antagonists.Type: GrantFiled: July 2, 2008Date of Patent: January 31, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
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Publication number: 20120015926Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: ApplicationFiled: November 9, 2009Publication date: January 19, 2012Inventors: Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Joseph A. Kozlowski, Michael K.C. Wong, Lei Chen, Guowei Zhou, Razia K. Rizvi, Robert Feltz, Aneta Maria Kosinski, De-Yi Yang, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristen E. Rosner, M. Arshad Siddiqui, Liping Yang
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Publication number: 20120003335Abstract: The invention provides a method of controlling obesity or type two diabetes in a human. In accordance with the inventive method, the constitutive androstane receptor (CAR) is agonized within the human, which effectively controls obesity or type two diabetes.Type: ApplicationFiled: November 18, 2009Publication date: January 5, 2012Applicant: UNIVERSITY OF PITTSBURGH-OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATIONInventors: Wen Xie, Jie Gao
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Patent number: 8080569Abstract: The present invention relates to derivatives of imidazo[2,1-b]thiazoles of formula I, in which R, R1 to R3 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.Type: GrantFiled: May 15, 2009Date of Patent: December 20, 2011Assignee: Sanofi-AventisInventors: Gerhard Zoller, Hartmut Strobel, David William Will, Paulus Wohlfart
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Publication number: 20110288153Abstract: In certain embodiments this invention pertains to the discovery that inhibition of the expression and/or activity of eukaryotic initiation factor 4A (eIF4A) inhibits the aging process. Accordingly, in certain embodiments, methods are provided for inhibiting/slowing aging. The methods typically involve administering to a mammal an agent that inhibits the expression and/or activity of eukaryotic initiation factor 4A (eIF4A) in an amount sufficient to inhibit expression or activity of EIF4A, where the agent is not resveratrol.Type: ApplicationFiled: November 18, 2009Publication date: November 24, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Jing Huang, Rui Hao, Brett Eugene Lomenick, Nao Jonai, Simon Diep
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Publication number: 20110281920Abstract: The present invention provides levamisole/macrocyclic lactone-containing injectable formulations that are effective against animal pests, including endoparasites. The formulations may be used for combating parasites in or on birds and mammals. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation of birds and mammals.Type: ApplicationFiled: May 12, 2011Publication date: November 17, 2011Inventors: Robert Holmes, Majid Razzak, Alan Johnson, Jitendra Goswami, Atul Awasthi
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Publication number: 20110275663Abstract: The present invention relates to the use of acylthiourea or acylurea derivatives for the treatment of pathologies involving a tissue dysfunction associated with a deregulation of the Hedgehog protein signalling pathway, and also to novel acylthiourea or acylurea derivatives as such, to their use as a medicinal product, and to pharmaceutical compositions containing them.Type: ApplicationFiled: April 16, 2009Publication date: November 10, 2011Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Angèle Schoenfelder, André Mann, Maurizio Taddei, Antonio Solinas, Fabrizio Manetti
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Publication number: 20110269748Abstract: This invention concerns the use of a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is hydrogen, halo, C1-6alkyl, Het1, HO—C1-6alkyl-, cyano-C1-6alkyl-, amino-C(?O)—C1-6alkyl-, formylamino-C1-6alkyl-, C1-6alkyl-C(?O)—NH—C1-6alkyl-, mono- or di(C1-6alkyl)amino-C(?O)—C1-6alkyl-, phenyl-C1-6alkyl-, or Het4-C1-6alkyl-; Q is phenyl, pyridyl, benzofuranyl, 2,3-dihydro-benzofuranyl, pyrazolyl, isoxazolyl or indazolyl wherein each of said ring systems is optionally being substituted with up to three substituents each independently selected from halo, cyano, C1-6alkyl, C1-6alkyl-O—, C1-6alkylthio, Ar or polyhaloC1-6alkyl; L is phenyl, pyridyl, pyrimidazolyl, 8-Azapyrimidazolyl, pyridazinyl, imidazothiazolyl or furanyl wherein each of said ring systems may optionally be substituted with one or two or more substituents, each substituent independently being selected from halo, hydroxy, amino, cyano, C1-6alkylType: ApplicationFiled: February 13, 2008Publication date: November 3, 2011Inventors: Johannes Wilhelmus John F. Thuring, Gregor James MacDonald, Christopher James Grantham, Theodorus Dinklo, Anne Simone Josephine Lesage
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Publication number: 20110269817Abstract: The invention relates to modulation of circadian rhythm and underlying biological processes.Type: ApplicationFiled: July 24, 2009Publication date: November 3, 2011Applicant: The Regents of the University of CaliforniaInventors: Paolo Sassone-Corsi, Yasukazu Nakahata
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Publication number: 20110263662Abstract: The invention relates to 1,2-diamido-ethylene derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: August 14, 2008Publication date: October 27, 2011Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
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Publication number: 20110218232Abstract: The invention relates to inhibitors of Multi drug Resistant Protein 4 (MRP4) for the treatment and/or the prevention of cardiac disorders, such as acute or chronic heart failure and cardiogenic shock. The invention also relates to agents stimulating MRP4 activity for the treatment and/or the prevention of cardiac hypertrophy.Type: ApplicationFiled: July 17, 2009Publication date: September 8, 2011Applicant: INSERM (Institut National de la Sante et de la Recherche Medicale)Inventors: Jean-Sebastien Hulot, Anne-Marie Lompre, Yassine Sassi
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Publication number: 20110207751Abstract: Novel compounds having a fused bicyclic heteroaromatic ring system substituted with a thiazole ring are disclosed. The compounds inhibit growth of a variety of types of cancer cells, and are thus useful for treating cancer. Efficacy of these compounds is demonstrated with a system for monitoring cell growth/migration, which shows they are potent inhibitors of growth and/or migration of cancer cells. In addition, compounds of the invention were shown to stop growth of tumors in vivo, and to reduce the size of tumors in vivo. Compositions comprising these compounds, and methods to use these compounds and compositions for treatment of cancers, are disclosed.Type: ApplicationFiled: February 18, 2011Publication date: August 25, 2011Inventors: Long Mao, Xiaobo Wang, Xiao Xu, Li Zhao, Jia Liu
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Patent number: 7994336Abstract: The invention relates to novel azetidine compounds of formula (I), wherein R1, R2, and X are as described in the description and their use as orexin receptor antagonists.Type: GrantFiled: August 15, 2007Date of Patent: August 9, 2011Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
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Publication number: 20110150827Abstract: Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: ApplicationFiled: December 17, 2010Publication date: June 23, 2011Applicant: Idenix Pharmaceuticals, Inc.Inventors: Cyril B. Dousson, David Dukhan, Christophe Claude Parsy, Claire Pierra, Francois-Rene Alexandre, Guillaume Brandt, Daniel Da Costa, Houcine Rahali, Jean-Laurent Paparin, Michel Derock, Thierry Convard, Dominique Surleraux
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Patent number: 7960568Abstract: The present invention relates to heterocyclyl-substituted sulfonamides with 5-HT6 receptor affinity, and compositions thereof, and the use of said compounds for the treatment or prophylaxis of various disorders.Type: GrantFiled: January 30, 2008Date of Patent: June 14, 2011Assignee: Laboratorios Del Dr. Esteve, S.A.Inventor: José-Luis Diaz-Fernández
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Publication number: 20110130387Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. 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 related 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: November 29, 2010Publication date: June 2, 2011Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Joseph J. Nunes, Jill Milne, Jean Bemis, Roger Xie, Chi B. Vu, Pui Yee Ng, Jeremy S. Disch, Thomas Salzmann, David Armistead
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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: 20110105555Abstract: The invention relates to compounds having pharmacological activity towards the 5-HT6 receptor, and more particularly to some N-imidazo[2,1-b]thiazole-5-sulfonamide derivatives, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT6 is involved.Type: ApplicationFiled: May 8, 2009Publication date: May 5, 2011Inventors: Josep Mas Prio, Antoni Torrens Jover
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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: 20110092540Abstract: The invention relates to compounds having pharmacological activity towards the 5-HT6; receptor, and more particularly to some N-phenyl-2,3-dihydroimidazol[2,1-b]thiazole-5-sulfonamide derivatives, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT6 is involved.Type: ApplicationFiled: May 8, 2009Publication date: April 21, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Josep Mas Prio, Antoni Torrens Jover
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Publication number: 20110086882Abstract: A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism wherein X is a nitrogen atom or CH; R1 is -A11-A12; A11 is a single bond or a C1-6 alkylene group; A12 is a hydrogen atom, a C1-6 alkyl group or a C3-6 cycloalkyl group, etc.; R2 is -A21-A22; A21 is a single bond or a C1-6 alkylene group; A22 is a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a non-aromatic heterocyclic group, or a heteroaryl group, etc.; R3 is a C1-6 alkyl group, a C3-6 cycloalkyl group, a C1-6 alkoxy group, a C3-6 cycloalkoxy C1-6 alkyl group, di-C1-6 alkyl amino group, a halogen atom, a cyano group, a formyl group, or a carboxyl group, etc; R4 is a hydrogen atom or a C1-6 alkoxy group; R5 is a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group; R6 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkylthio group, or a C1-6 alkyl sulfinyl group etc.Type: ApplicationFiled: October 7, 2010Publication date: April 14, 2011Applicant: Eisai R&D Management Co., Ltd.Inventors: Kogyoku SHIN, Taro TERAUCHI, Yoshinori TAKAHASHI, Minako HASHIZUME, Kunitoshi TAKEDA, Kodo SHIKATA, Akira INOMATA
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Publication number: 20110086800Abstract: A method to aid in identifying a familial or sporadic pattern of risk in at least one individual for developing cancer of a mucosal epithelial tissue, the method comprising screening said at least one individual for heterozygosity or homozygosity for a mutation in a gene coding for a Poly-Ig (Fc) receptor or a Poly-Ig-like (Fc) receptor capable of mediating inhibition of cancer cell growth by an immunoglobulin inhibitor. A method of treating an individual so identified includes enhancing the amount of immunoglobulin inhibitor contacting a mucosal epithelial tissue of said individual, and, especially in individuals homozygous for the defective receptor, may also include prophylactic surgery. Other methods include implementation of a risk reduction or prevention program in individuals identified as being at risk.Type: ApplicationFiled: November 30, 2010Publication date: April 14, 2011Inventor: David A. Sirbasku
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Publication number: 20110065728Abstract: The present invention provides pharmaceutical compositions containing benzene compound(s) represented by General Formula (1) below and, particularly, LPL-activating compositions for use in hyperlipidemia therapeutic and preventive agents, anti-obesity agents, and the like: wherein R1, R2, R3 and R4 are as defined in the specification.Type: ApplicationFiled: May 14, 2008Publication date: March 17, 2011Applicant: OTSUKA PHARMACEUTICAL FACTORY, INC.Inventors: Irina Neagu, Michael Ohlmeyer, Vidyadhar M. Paradkar, Kurt W. Saionz, Koushi Iwata, Takashi Okamura, Tadao Shibutani
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Publication number: 20110065704Abstract: The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.Type: ApplicationFiled: June 25, 2010Publication date: March 17, 2011Inventor: Sean RYDER
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Publication number: 20110053994Abstract: Provided herein include compositions, all related stereoisomers as well as pharmaceutically acceptable salts provided as simplified analogs of pateamine A, in which the analogs generally are devoid of the C3-amino and C5-methyl groups, also referred to as desmethyl, desamino-pateamine A. Suitable analogs provide anticancer and antiproliferative effects in vivo and in vitro by a novel drugs mechanism of action described herein for pateamine A, including inhibition of eIF4A-dependent translation initiation. As with pateamine A, as described herein, suitable analogs cause cell cycle arrest or induce apoptosis in transformed cells. However, toxicity of such compounds to slow growing normal cells is low. In addition, such analogs, like pateamine A, target translation initiation factors and are useful as anticancer and antiproliferative agents in subjects in need thereof.Type: ApplicationFiled: June 11, 2010Publication date: March 3, 2011Applicants: THE TEXAS A & M UNIVERSITY SYSTEM, JOHNS HOPKINS UNIVERSITY, THEInventors: Daniel Romo, Jun Liu, Nam Song Choi, Zonggao Shi, Woon-Kai Low, Yongjun Dang, Tilman Schneider-Poetsch
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Patent number: 7893069Abstract: Substituted imidazo[2,1-b]thiazole compounds corresponding to formula I, a method for producing them, pharmaceutical compositions containing them, and the use thereof for regularing mGluR5 receptors, or for treating or inhibiting disorders or disease states at least partially mediated by mGluR5 receptor such as pain, anxiety attacks, drug or alcohol dependency, and others.Type: GrantFiled: September 9, 2008Date of Patent: February 22, 2011Assignee: Gruenenthal GmbHInventors: Sven Kuehnert, Saskia Zemolka, Michael Haurand, Klaus Schiene
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Publication number: 20110028423Abstract: The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect choline acetyltransferase; a method for assaying pesticidal activity of a test substance, which comprises measuring the activity of a choline acetyltransferase in a reaction system in which the choline acetyltransferase contacts with a test substance, and the like.Type: ApplicationFiled: November 21, 2008Publication date: February 3, 2011Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Junko Otsuki, Marc Van De Craen, Annelies Roobrouck, Guy Nys, Bert Demey
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Publication number: 20110009385Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: R3 is selected from cyclopentyl and cyclohexyl; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high dual efficacies for human cathepsin S and K and are useful for the treatment of rheumatoid arthritis, osteoarthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, cardiovascular diseases which exhibit significant damage and remodeling of extracellular matrix (ECM) and chronic pain.Type: ApplicationFiled: August 9, 2010Publication date: January 13, 2011Applicant: Amura Therapeutics LimitedInventors: MARTIN QUIBELL, John P. Watts, Nicholas S. Flinn
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Publication number: 20110009461Abstract: The invention relates to 2-aza-bicyclo[3.3.0]octane derivatives of Formula (I) wherein A, B, 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: January 13, 2011Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen, Daniel Trachsel
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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: 20110003807Abstract: The present invention relates to a compound represented by the formula (I) or (I?): wherein each symbol is as defined in the specification, or a salt thereof, and a PI3K and(or) mTOR inhibitor containing the compound or a prodrug thereof.Type: ApplicationFiled: January 28, 2010Publication date: January 6, 2011Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company LimitedInventors: Hiroshi Banno, Masaaki Hirose, Osamu Kurasawa
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Publication number: 20100330114Abstract: The present disclosure provides a method of increasing an immune response in an individual, the method involving administering to an individual in need thereof an inhibitor of SIRT1. The present disclosure provides a method of reducing an immune response, e.g., to treat chronic immune hyperactivity, the method generally involving administering to an individual in need thereof an activator of SIRT1. The present disclosure provides a method of modulating activation and differentiation of CD4+T cells.Type: ApplicationFiled: July 16, 2010Publication date: December 30, 2010Inventors: ERIC M. VERDIN, MELANIE OTT, HYE-SOOK KWON, HYUNGWOOK LIM
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Publication number: 20100298348Abstract: The present invention provides a method of decreasing the level of ubiquitylated protein in a subject, the method comprising administering a heterocyclic compound disclosed herein or a pharmaceutically acceptable salt, hydrate or prodrug thereof to a subject in need thereof.Type: ApplicationFiled: May 11, 2010Publication date: November 25, 2010Inventors: Kim Nicholas Green, Eckard Weber, Tilman Oltersdorf, Sharon Rogers, Frank LaFerla
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Patent number: 7838513Abstract: The present invention relates to the treatment of a mammal with a pharmaceutical composition comprising an H2-blocker, at least one anti-inflammatory agent, a cytotoxic agent and, optionally, levamisole, a retinoid, an NFkB inhibitor, a redox quinone, an agent that enhances the intracellular accumulation of NADH+H+, a poly-alcohol, an inhibitor of pro-angiogenic growth factor(s) and an MMP inhibitor, such pharmaceutical composition allowing for the enhanced therapy and/or prevention of neoplastic diseases and disorders.Type: GrantFiled: July 4, 2007Date of Patent: November 23, 2010Assignee: Tiltan Pharma Ltd.Inventor: Shmuel A. Ben-Sasson
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Publication number: 20100292232Abstract: Disclosed herein are antiviral agents, in particular non-nucleoside reverse transcriptase inhibitors (NNRTIs) of the formula Also disclosed are methods of making the NNRTIs, as well as compositions that include such NNRTIs and methods of their use for treating viral infections, in particular retroviral infections, such as HIV infection.Type: ApplicationFiled: November 5, 2008Publication date: November 18, 2010Inventors: Daniel Elleder, John A.T. Young, Thomas J. Baiga, Joseph P. Noel
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Publication number: 20100261710Abstract: The present invention provides hydroxamic acid compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the hydroxamic acid compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of the present invention.Type: ApplicationFiled: August 21, 2008Publication date: October 14, 2010Applicant: ARQULE, INC.Inventors: Mark A. Ashwell, Manish Tandon, Nivedita D. Namdev, Jean-Marc Lapierre, Yanbin Liu, Hui Wu
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Publication number: 20100261758Abstract: Compounds of Formula (I) wherein R1 is aryl, cyclohexyl or heterocyclyl, or (C1-4)alkyl substituted by aryl, cyclohexyl or heterocyclyl, R2 is defined heterocyclyl, R3 is alkyl, aryl, cyclohexyl or heterocyclyl, or (C1-4)alkyl substituted by aryl, cyclohexyl or heterocyclyl, R4 is H or alkyl, or R3 and R4 together with the carbon atom to which they are attached are cycloalkyl fused with aryl, and their use as pharmaceuticals.Type: ApplicationFiled: March 28, 2007Publication date: October 14, 2010Applicant: NOVARTIS AGInventors: Luca Arista, Klemens Hogenauer, Niko Schmiedeberg, Gudrun Werner, Herbert Jaksche
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Publication number: 20100226913Abstract: This invention provides a compositions for transport of a therapeutic agent. The compositions contain a therapeutic agent and a monoterpene or an analog thereof. In one aspect, the monoterpene is perillyl alcohol (POH) or an analog thereof. In one aspect, the therapeutic agent is provided in an amount effective to treat the disease or subject of choice.Type: ApplicationFiled: February 4, 2010Publication date: September 9, 2010Inventors: Thomas C. Chen, Clovis O. da Fonseca, Thereza Quirico dos Santos, Gilberto Schwartsmann
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Patent number: 7790741Abstract: The present invention is directed to novel compounds of formula (I) wherein the variables are as defined herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.Type: GrantFiled: October 5, 2007Date of Patent: September 7, 2010Assignee: Abbott LaboratoriesInventors: David J. Calderwood, Kristine E. Frank, David W. Borhani, Heather M. Davis, Nathan S. Josephsohn, Barbara S. Skinner
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Publication number: 20100203110Abstract: The present invention relates to methods of treating a cancerous tumor in a subject comprising administering to the subject an effective amount of 3-bromopyruvate. The 3-bromopyruvate may be administered intraarterially directly to a tumor as a continuous intraarterial infusion. The present invention also relates to methods for identifying agents that inhibit type II hexokinase activity.Type: ApplicationFiled: December 17, 2007Publication date: August 12, 2010Applicant: The Johns Hopkins UniversityInventors: Jean-Francois Geschwind, Mustafa Vali
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Patent number: 7767824Abstract: Heterocyclic compound represented by the formula I wherein represents or the like; R1 represents hydrogen atom, C1-C6 alkyl or benzyloxy; R2 represents methyl or nil; R3 represents hydrogen atom, C1-C6 alkyl, C2-C6 alkenyl, C3-C8 cycloalkyl or —CH2R5 [wherein R5 represents phenyl (which may be substituted with C1-C6 alkyl, halogen atom or cyano)] or thienyl; R4 represents C1-C6 alkyl, C2-C6 alkenyl, C3-C8 cycloalkyl or —CH2R6 [wherein R6 represents phenyl (which may be substituted with C1-C6alkyl, halogen atom or cyano), naphtyl or thienyl]; or R3 is coupled with R4.Type: GrantFiled: May 15, 2006Date of Patent: August 3, 2010Assignee: Zenyaku Kogyo Kabushiki KaishaInventors: Seiichiro Kawashima, Toshiyuki Matsuno, Naoki Fukuda, Kenichi Saitoh, Yoshimasa Yamaguchi, Masaya Higashi
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Publication number: 20100184808Abstract: The invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as orexin receptor antagonists.Type: ApplicationFiled: July 2, 2008Publication date: July 22, 2010Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
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Publication number: 20100184772Abstract: The present invention relates to substituted pyrazoline compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: ApplicationFiled: October 10, 2007Publication date: July 22, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Helmut H. Buschmann, Antonio Torrens-Jover, Josef Mas-Prio, Susana Yenes-Minguez
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Publication number: 20100168135Abstract: The present invention provides a method of inducing cleavage of amyloid precursor protein to produce an approximately 17 kilodalton carboxy-terminal fragment of amyloid precursor protein in a subject, the method comprising administering a heterocyclic compound or a pharmaceutically acceptable salt, hydrate or prodrug thereof to a subject in need thereof, wherein the approximately 17 kilodalton fragment includes the carboxyterminal amino acid sequence of amyloid precursor protein and amyloid-beta amino acid sequence. Also provided is a screening method for identifying compounds induce cleavage of amyloid precursor protein to produce the approximately 17 kilodalton carboxy-terminal fragment of amyloid precursor protein.Type: ApplicationFiled: December 15, 2009Publication date: July 1, 2010Inventors: Kim Nicholas Green, Tilman Oltersdorf, Eckard Weber
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Publication number: 20100152192Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.Type: ApplicationFiled: December 11, 2009Publication date: June 17, 2010Applicant: Glenmark Pharmaceuticals S.AInventors: Sachin Sundarlal Chaudhari, Abraham Thomas, Ashok Bhausaheb Kadam, Sachin Vasantrao Dhone, Suresh Mahdadev Kadam, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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Publication number: 20100137384Abstract: The invention relates to a novel formulation having the advantage of including triclabendazole in solution. In addition a further anthelmintic may be included. The formulation is made by mixing the abamectin and benzyl alcohol and mixing this with triclabendazole and butyl dioxitol. The mix is then heated to dissolve the active, and allowed to cool at which stage the solution is diluted to volume with PEG 4000. The present invention overcomes the solubility difficulties of triclabendazole and presents the triclabendazole in a solution.Type: ApplicationFiled: December 7, 2009Publication date: June 3, 2010Inventor: Colin Mason Harvey