Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/443)
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Publication number: 20090258906Abstract: The invention relates to compounds of the formula I in which R1, R2, A, B, X and Y have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.Type: ApplicationFiled: December 18, 2008Publication date: October 15, 2009Applicant: SANOFI-AVENTISInventors: Stephanie HACHTEL, Juergen DEDIO, Josef PERNERSTORFER, Stephen SHIMSHOCK, Carolina LANTER, Raymond KOSLEY
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Publication number: 20090258936Abstract: The invention relates to compounds of the formula I in which R1, R2, A, B, X and Y have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.Type: ApplicationFiled: December 18, 2008Publication date: October 15, 2009Applicant: SANOFI-AVENTISInventors: Stephanie HACHTEL, Juergen DEDIO, Josef PERNERSTORFER, Stephen SHIMSHOCK, Carolina LANTER
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Publication number: 20090253656Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.Type: ApplicationFiled: March 29, 2006Publication date: October 8, 2009Applicant: Kabushiki Kaisha Yakult HonshaInventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
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Patent number: 7598417Abstract: The present patent application is directed to novel fluoroethyl urea compounds and compositions and their therapeutic use in the treatment of pain and other conditions.Type: GrantFiled: March 28, 2008Date of Patent: October 6, 2009Assignee: Allergan, Inc.Inventors: Ken Chow, Wenkui K. Fang, Evelyn G. Corpuz, Daniel W. Gil, Michael E. Garst
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Publication number: 20090247567Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: March 30, 2009Publication date: October 1, 2009Applicant: Genentech, Inc.Inventors: Steven Do, Richard Goldsmith, Tim Heffron, Aleksandr Kolesnikov, Steven Staben, Alan G. Olivero, Michael Siu, Daniel P. Sutherlin, Bing-Yan Zhu, Paul Goldsmith, Tracy Bayliss, Adrian Folkes, Neil Pegg
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Publication number: 20090247536Abstract: Embodiments of the present invention provide bissulfonamide compounds that are agonists of GalR1. The present invention further provides compositions comprising bissulfonamide compounds that are agonists of GalR1, and methods of use of such compounds and compositions.Type: ApplicationFiled: June 12, 2009Publication date: October 1, 2009Inventors: Adnan M.M. Mjalli, Bapu Gaddam, Mohan Rao, Muralidhar Bondlela, Ramesh Gopalaswamy, Robert C. Andrews, Stephen Davis, Suvi Simila, Tan Ren
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Patent number: 7595343Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: September 12, 2002Date of Patent: September 29, 2009Assignee: MethylGene, Inc.Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain
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Publication number: 20090233963Abstract: The present invention provides a method of determining the susceptibility of a subject to treatment with a leukotriene modifier by determining the subject's cysteinyl leukotriene (CysLT) level and the subject's level of eosinophilic airway inflammation and identifying a subject with a high ratio of CysLT levels to eosinophilic airway inflammation as susceptible to treatment with the leukotriene modifier. Also discussed is a method of treatment of subjects who are susceptible to treatment that includes administering a leukotriene modifier to such a subject.Type: ApplicationFiled: March 16, 2009Publication date: September 17, 2009Inventors: Nathan Rabinovitch, Erwin Gelfand
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Patent number: 7589089Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, R4, and X are as defined herein or to pharmaceutically acceptable acid addition salts thereof, with the exception of 4-methoxy-N-[2-oxo-2-(phenylamino)ethyl]-N-phenyl-benzamide, 4-chloro-N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-chloro-N-[2-[5-chloro-2-methoxyphenyl)amino]-2-oxoethyl]-N-benzamide, 4-methyl-N-(2-oxo-2-[(2,4,6-trichlorophenyl)amino]ethyl]-N-benzamide, N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-methyl-N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-chloro-N-(2-oxo-2-[(2,4,6-trichlorophenyl)amino]ethyl]-N-benzamide and N-[2-[(2,4-dimethoxyphenyl)amino]-2-oxoethyl]-N-[(2-fluorophenyl)methyl]-benzeneacetamide. The compounds are useful in the treatment of neurological and neuropsychiatric disorders.Type: GrantFiled: August 23, 2007Date of Patent: September 15, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Emmanuel Pinard
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Patent number: 7589232Abstract: The present invention is related to alkynyl aryl carboxamides of Formula (I?) and use thereof for the treatment and/or prevention of an inflammatory disorder, obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia-hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkynyl aryl carboxamides of Formula (I?) to modulate, notably to inhibit the activity of PTPs. (I?) A is a C2-C15 alkynyl, C2-C6-alkynyl aryl, C2-C6-alkynyl heteroaryl. Cy is an aryl, heteroaryl, cycloalkyl or heterocycle group; n is either 0 or 1. Cy? is an aryl, which may optionally be fused by a 3-8 membered cycloalkyl. R1 and R2 are independently from each other is selected from the group consisting of hydrogen or (C1-C6)alkyl. R4 and R5 are each independently from each other selected from the group consisting of H, hydroxy.Type: GrantFiled: July 20, 2004Date of Patent: September 15, 2009Assignee: Laboratories Serono S.A.Inventors: Dominique Swinnen, Patrick Gerber, Jerome Gonzalez, Agnes Bombrun, Catherine Jorand-Lebrun
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Publication number: 20090227667Abstract: Compounds of Formula (I), are provided where T is CHO, COR8, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y=C, or substituted diene fused to Y when Y=C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.Type: ApplicationFiled: May 5, 2009Publication date: September 10, 2009Applicant: WyethInventors: Anthony Frank Kreft, Lynn Resnick, Scott Christian Mayer, George Diamantidis, Derek Cecil Cole, Boyd Lynn Harrison, Minsheng Zhang, Molly Hoke, Tingzhong Wang, Rocco John Galante
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Publication number: 20090226422Abstract: The present invention provides identification of inhibitors of inhibitors of differentiation (Id) for use in the treatment and prevention of diseases in mammals. The inhibitors of Id are effective alone in the treatment of a variety of cellular proliferative disorders including, but not limited to, diseases such as cancer, arthritis, age-related macular degeneration, psoriasis, neoplasms, angiomas, endometriosis, obesity, age-related macular degeneration, retinopathies, restenosis, scaring, fibrogenesis, fibrosis, cardiac remodeling, pulmonary fibrosis, scleroderma, failure associated with myocardial infarction, keloids, fibroid tumors and stenting.Type: ApplicationFiled: October 16, 2008Publication date: September 10, 2009Inventors: Jaideep CHAUDHARY, William A. Garland
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Publication number: 20090227625Abstract: The invention relates to compounds of the formula I in which R1, R2, X, A, B, Z and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.Type: ApplicationFiled: December 17, 2008Publication date: September 10, 2009Applicant: sanofi-aventisInventors: Stephanie HACHTEL, Juergen DEDIO, Elisabeth DeFOSSA, Sven GRUENEBERG, Holger HEITSCH, William BOCK, Charlie CHEN, Raymond KOSLEY, Chung-Yi KUNG, Marcel PATEK, Rosy SHER, Stephen SHIMSHOCK, Aleksandra WEICHSEL
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Patent number: 7585888Abstract: This invention relates to novel benzofuran and benzothiophene derivatives of the general formula and their use for the treatment of hyper-proliferative disorders.Type: GrantFiled: March 31, 2008Date of Patent: September 8, 2009Assignee: Bayer Pharmaceuticals CorporationInventors: Chengzhi Zhang, Michael J. Burke, Zhi Chen, Jacques P. Dumas, Dongping Fan, Jianmei Fan, Holia Hatoum-Mokdad, Benjamin D. Jones, Gaetan Ladouceur, Wendy Lee, Barton Phillips
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Publication number: 20090221654Abstract: A prostaglandin analog with selectivity to EP receptors and demonstrating EP agonist activity that may be used to expand hematopoietic stem cell populations or to treat or prevent influenza, bone fracture, bone disease, glaucoma, ocular hypertension, dysmenorrhoea, pre-term labor, immune disorders, osteoporosis, asthma, allergy, male sexual dysfunction, female sexual dysfunction, periodontal disease, gastric ulcer, renal disease, or other EP receptor-mediated conditions.Type: ApplicationFiled: November 14, 2008Publication date: September 3, 2009Applicant: CAYMAN CHEMICAL COMPANYInventors: Nancy S. Barta, Stephen D. Barrett, Gregory W. Endres, Andrei M. Kornilov, Kirk M. Maxey, Adam Uzieblo
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Publication number: 20090221572Abstract: The present invention relates to compounds having pharmacological activity towards the sigma (?) receptor, and more particularly to some 4, 5, 6, 7 tetrahydrobenzo[b]thiophene derivatives, wherein n is selected from 0, 1, 2, 3 or 4; m is selected from 0, 1 or 2; the dotted line represents either a single or a double bond; to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis.Type: ApplicationFiled: March 2, 2007Publication date: September 3, 2009Applicant: Laboratorios Del Dr. Esteve, S.A.Inventors: Jordi Corbera-Arjona, Daniel Martinez-Olmo, David Vano-Domenech
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Publication number: 20090221564Abstract: Heterocyclic compounds of the formula (I) are provided: wherein ring A, ring B, R1, R2, R3, R4, Y, m, n and q are as identified herein. R1 is in particular amidino. The invention further provides particular benzothiophene compounds. Compounds of the invention may be useful as inhibitors of Factor IXa and in the therapy of cardiovascular conditions and diseases, e.g. thrombosis.Type: ApplicationFiled: February 20, 2007Publication date: September 3, 2009Applicant: TRIGEN LIMITEDInventors: Shouming Wang, Toby Jonathan Blench, Frederic Marlin, Richard Beck, Roger Peter Dickinson
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Publication number: 20090221687Abstract: Novel tetracyclic dibenzo(e,h)azulene compounds of formula I; their pharmacologically acceptable derivatives; process and intermediates for their preparation; pharmaceutical compositions containing them and their activity and use in the treatment of central nervous system (CNS) diseases and conditions in humans and animals.Type: ApplicationFiled: February 1, 2006Publication date: September 3, 2009Inventors: Milan Mesic, Mladen Mercep, Dijana Pesic, Renata Rupcic, Barbara Stanic
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Publication number: 20090220583Abstract: There is provided homogeneous pharmaceutical compositions for the treatment of inflammatory disorders comprising an antiinflammatory and/or antihistaminic active ingredient, a polar lipid liposome and a pharmaceutically-acceptable aqueous carrier.Type: ApplicationFiled: June 8, 2006Publication date: September 3, 2009Inventors: Lena Pereswetoff-Morath, Anders Carlsson
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Patent number: 7582673Abstract: Embodiments of the present invention provide bissulfonamide compounds that are agonists of GalR1. The present invention further provides compositions comprising bissulfonamide compounds that are agonists of GalR1, and methods of use of such compounds and compositions.Type: GrantFiled: October 20, 2005Date of Patent: September 1, 2009Assignee: High Point Pharmaceuticals, LLCInventors: Adnan M. M. Mjalli, Bapu Gaddam, Mohan Rao, Muralidhar Bondlela, Ramesh Gopalaswamy, Robert C. Andrews, Stephen Davis, Suvi Simila, Tan Ren
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Publication number: 20090209532Abstract: Compounds of formula (I) exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.Type: ApplicationFiled: July 17, 2006Publication date: August 20, 2009Inventors: Marko Ahlmark, Reijo Backstrom, Anne Luiro, Jarmo Pystynen, Eija Tiainen
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Patent number: 7576122Abstract: This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.Type: GrantFiled: August 27, 2004Date of Patent: August 18, 2009Assignee: Merck & Co. Inc.Inventors: Dong-Ming Shen, James B. Doherty
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Publication number: 20090191283Abstract: The formulation provides a method of treating headaches, neck, joint and inflammatory-type pain in a mammalian subject by administering to the subject a therapeutically effective amount of a nitrate-containing compound and a therapeutically effective amount of a selenium-containing compound. The formulation also provides kits and systems for practicing the subject methods.Type: ApplicationFiled: January 24, 2008Publication date: July 30, 2009Inventors: Bryan Todd Oronsky, Neil Charles Oronsky
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Publication number: 20090192213Abstract: The present invention relates to benzo[b]furane and benzo[b]thiophene derivatives of the general formula IV as the free base or salts thereof and their use.Type: ApplicationFiled: February 20, 2009Publication date: July 30, 2009Applicant: H. Lundbeck A/SInventors: Jan Kehler, Karsten Juhl, Morten Bang Norgaard
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Publication number: 20090186916Abstract: Provided is a compound that is an NMDA receptor antagonist having a broader safety margin, and is useful as an agent for treating or preventing Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, or pain. A novel compound or a salt thereof, which is characterized in that it has an amino group and R1 (lower alkyl, cycloalkyl, -lower alkylene-aryl, aryl which may be substituted, and the like) on carbon atoms of indane, cyclopenta[b]thiophene, cyclopenta[b]furan, cyclopenta[b]pyridine, or cyclopenta[c]pyridine ring, or 2,3-dihydrdo-1-benzofuran, 2,3-dihydrdo-1-benzothiophene, indoline ring, or the like, and has R2 and R3 (the same or different, each lower alkyl or aryl) on carbon atoms beside them, and an NMDA receptor antagonist comprising the same as an active component.Type: ApplicationFiled: July 17, 2007Publication date: July 23, 2009Applicant: ASTELLAS PHARMA INC.Inventors: Satoshi Hayashibe, Shingo Yamasaki, Kazushi Watanabe, Nobuyuki Shiraishi, Daisuke Suzuki, Hiroaki Hoshii, Junya Ohmori, Takatoshi Kanayama
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Publication number: 20090176865Abstract: The present invention is directed to novel sulfamide derivatives, pharmaceutical compositions comprising said compounds and methods for the treatment of epilepsy and related disorders comprising administering to a subject in need thereof, said compounds, either alone or as co-therapy with one or more anticonvulsant and/or anti-epileptic agents.Type: ApplicationFiled: August 7, 2008Publication date: July 9, 2009Inventors: Michael Breslav, Brian Klein, John A. Moyer, Frank J. Villani
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Publication number: 20090163547Abstract: The present invention makes reference to new indene derivatives with general formula (I), as well as to their preparation procedures, their application as medicament and the pharmaceutical compositions containing them. The new compounds of formula (I) show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.Type: ApplicationFiled: November 7, 2006Publication date: June 25, 2009Inventors: Maria De Las Ermitas Alcalde-Pais, Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal, Maria De Les Neus Mesquida-Estevez, Sara Lopez-Perez
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Patent number: 7550461Abstract: Disclosed are amide compounds of formula (I): wherein Ar1, Q, Y and R3-R6 of formula (I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: April 10, 2003Date of Patent: June 23, 2009Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Donghong Amy Gao, Daniel R. Goldberg, Abdelhakim Hammach, Ming-Hong Hao, Victor Marc Kamhi, Neil Moss, Kevin Chungeng Qian, Gregory Paul Roth, Christopher Ronald Sarko, Alan David Swinamer, Zhaoming Xiong
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Patent number: 7547722Abstract: The invention relates to a group of novel thieno-pyrrole compounds of Formula (I): wherein: R1, R2, R3, R4 and R5 are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.Type: GrantFiled: May 22, 2007Date of Patent: June 16, 2009Assignee: AstraZeneca ABInventors: Kevin Michael Foote, Zbigniew Stanley Matusiak, Alexander Graham Dossetter, Jean Claude Arnould, Maryannick Andree Lamorlette, Benedicte Delouvrie, Annie Hamon
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Publication number: 20090143411Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.Type: ApplicationFiled: October 18, 2005Publication date: June 4, 2009Applicant: COMPASS PHARMACEUTICALS LLCInventors: John Ward, Rama Jain, Donald R. James, Herman J. Verheij, Jan C.C. Schultz
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Publication number: 20090137659Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: August 15, 2008Publication date: May 28, 2009Applicant: CALCIMEDICA, INC.Inventors: Gonul VELICELEBI, Kenneth A. STAUDERMAN, David P.M. PLEYNET, Song CHENG, Jeffrey P. WHITTEN
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Publication number: 20090131510Abstract: Disclosed herein are compounds of Formula I as disclosed herein, methods of modulating the activity of an estrogen receptor and methods of treating a disorder associated with estrogen receptors.Type: ApplicationFiled: October 24, 2008Publication date: May 21, 2009Inventors: Roger Olsson, Lene Hyldtoft, Magnus Gustafsson, Birgitte Wintherlund
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Publication number: 20090131400Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.Type: ApplicationFiled: July 25, 2008Publication date: May 21, 2009Applicant: IRM LLCInventors: Yuan Mi, Shifeng Pan, Nathanael Schiander Gray, Wenqi Gao, Yi Fan, Tao Jiang
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Publication number: 20090131468Abstract: The invention provides compounds of formula wherein R1, R2, R3, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.Type: ApplicationFiled: November 14, 2008Publication date: May 21, 2009Applicant: AstraZeneca ABInventors: Johan Bylund, Marie E. Ek, Annika Kers, Gunnar Nordvall, Liselotte Ohberg, Jenny Viklund, Stefan Von Berg, Jorg Holenz, Katja Narhi, Daniel Sohn, Martin H. Johansson
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Patent number: 7534791Abstract: The present invention relates to benzo[b]furane and benzo[b]thiophene derivatives of the general formula IV as the free base or salts thereof and their use.Type: GrantFiled: June 14, 2006Date of Patent: May 19, 2009Assignee: H. Lundbeck A/SInventors: Jan Kehler, Karsten Juhl, Morten Bang Norgaard
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Publication number: 20090118323Abstract: The present invention provides antitumor compounds of the formula (I); and antitumor methods.Type: ApplicationFiled: September 11, 2007Publication date: May 7, 2009Inventors: Mary Margaret Mader, Luisa Maria Martin-Cabrejas, Michael Enrico Richett
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Patent number: 7524866Abstract: This invention provides: 1) a method of treating androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of Bone Mineral Density (BMD) in a male subject suffering from prostate cancer; 2) a method of preventing androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of Bone Mineral Density (BMD) in a male subject suffering from prostate cancer; 3) a method of suppressing or inhibiting androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of BMD in a male subject suffering from prostate cancer; and 4) a method of reducing the risk of developing androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of BMD in a male subject suffering from prostate cancer, by administering to the subject a pharmaceutical composition comprising an anti-estrogen agent and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof.Type: GrantFiled: February 17, 2004Date of Patent: April 28, 2009Assignee: GTx, Inc.Inventors: Mitchell S. Steiner, Sharan Raghow, Karen A. Veverka
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Publication number: 20090105241Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, Y, R1 and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.Type: ApplicationFiled: December 12, 2008Publication date: April 23, 2009Applicant: Cephalon FranceInventors: Brigitte Lesur, Christophe Yue, Sophie Chasset, Olivier Renault
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Publication number: 20090105308Abstract: The present invention relates to novel benzoheterocyclylethylcarboxamide derivatives of formula (I) in which the substituents are in the description, their process of preparation, their use as fungicides, particularly in the form of fungicidal compositions, methods for the control of phytopathogenic fungi of plants using these compounds or their compositions:Type: ApplicationFiled: July 6, 2006Publication date: April 23, 2009Inventors: Darren Mansfield, Pierre-Yves Coqueron, Heiko Rieck, Philippe Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
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Publication number: 20090105259Abstract: This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain acyclic diamines, which are agonists of TRPV4 channel receptors.Type: ApplicationFiled: September 8, 2006Publication date: April 23, 2009Inventors: Jae U. Jeong, Robert W. Marquis
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Publication number: 20090099147Abstract: The present invention relates to non-steroidal progesterone receptor modulators of the general formula I the use of the progesterone receptor modulators for producing medicaments, and pharmaceutical compositions which comprise these compounds. The compounds according to the invention are suitable for the therapy and prophylaxis of gynaecological disorders such as endometriosis, leiomyomas of the uterus, dysfunctional bleeding and dysmenorrhoea, and for the therapy and prophylaxis of hormone-dependent tumours and for use for female fertility control and for hormone replacement therapy.Type: ApplicationFiled: July 9, 2008Publication date: April 16, 2009Inventors: Wolfgnag SCHWEDE, Carsten Moeller, Anja Schmidt, Ulrike Fuhrmann, Andrea Rotgeri, Thomas Kirkland
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Publication number: 20090087409Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; represents either a single or a double bond; R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4; M is N or CR7, wherein R7 has the same definition as R4; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; and R6 is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het; or R6 is wherein R7 and R8 and Q are as defined herein; Y2 is O or S; R9 is H, (C1-6 alkyl), (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl, aryl, Het, (C1-6)alkyl-aryl or (C1-6)alkyl-Het, alType: ApplicationFiled: November 26, 2008Publication date: April 2, 2009Applicant: Boehringer Ingelheim (Canada) Ltd.Inventors: Pierre Louis Beaulieu, Gulrez Fazal, Sylvie Goulet, George Kukolj, Martin Poirier, Youla S. Tsantrizos, Eric Jolicoeur, James Gillard, Marc-Andre Poupart, Jean Rancourt
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Patent number: 7511046Abstract: The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.Type: GrantFiled: July 21, 2006Date of Patent: March 31, 2009Assignee: Aventis Hoklings Inc.Inventors: David M Fink, Brian S Freed, Nicholas J Hrib, Raymond W Kosley, George E Lee, Gregory H Merriman, Barbara S Rauckman
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Publication number: 20090082308Abstract: The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: April 14, 2006Publication date: March 26, 2009Inventors: Jed Lee Hubbs, Dawn M. Mampreian, Joey L. Methot, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, David L. Sloman, Matthew G. Stanton, Kevin J. Wilson, David J. Witter
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Publication number: 20090069408Abstract: This invention is directed to, for example, compounds of formula (I): wherein n, m, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment of iron disorders. This invention is also directed to pharmaceutical compositions comprising the compounds and methods of using the compounds to treat iron disorders.Type: ApplicationFiled: March 7, 2008Publication date: March 12, 2009Applicant: XENON PHARMACEUTICALS INC.Inventors: Mikhail Chafeev, Nagasree Chakka, Jean-Jacques Cadieux, Jianmin Fu, Rajender Kamboj, Vishnumurthy Kodumuru, Jonathan Langille, Shifeng Liu, Jianyu Sun, Serguei Sviridov, Zaihui Zhang
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Publication number: 20090069391Abstract: The present invention relates to a novel class of hydroxamic acid derivatives. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: April 14, 2006Publication date: March 12, 2009Inventors: Jed Lee Hubbs, Sam Kattar, Joey Methot, Thomas Miller, Phieng Siliphaivanh, Matthew Stanton, Kevin Wilson, David J. Witter
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Publication number: 20090062297Abstract: The present invention relates to a novel class of hydroxyalkylarylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: January 8, 2007Publication date: March 5, 2009Inventors: Richard W. Heidebrecht, Thomas A. Miller, Kevin J. Wilson, David J. Witter, Jonathan Grimm
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Publication number: 20090062284Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted biaryl-methanesulfinyl acetamides of Formula (I): wherein Ar, Y, R1, R2, R4, R5, q and x are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness associated with narcolepsy, obstructive sleep apnea, or shift work disorder; Parkinson's disease; Alzheimer's disease; attention deficit disorder; attention deficit hyperactivity disorder; depression; or fatigue associated with a neurological disease; as well as the promotion of wakefulness.Type: ApplicationFiled: August 27, 2008Publication date: March 5, 2009Applicant: Cephalon, Inc.Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, Marie-Edith Gourdel, Greg A. Hostetler, Mohamed Iqbal, Brigitte Lesur, Philippe Louvet, Eric Riguet, Dominique Schweizer, Christophe Yue
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Publication number: 20090054235Abstract: The present invention relates to novel benzoheterocyclylethylbenzamide derivatives of formula (I) in which the substituents are in the description, their process of preparation, their use as fungicides, particularly in the form of fungicidal compositions, and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.Type: ApplicationFiled: July 6, 2006Publication date: February 26, 2009Inventors: Darren Mansfield, Pierre-Yves Coqueron, Heiko Rieck, Philippe Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
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Publication number: 20090048286Abstract: Protein tyrosine phosphatases (PTPases) such as PTP1B can play a role in regulating a wide variety of cellular responses such as insulin signaling. Substituted bicyclic fused-thiophene compounds can inhibit PTP1B and thereby induce greater insulin sensitivity. Accordingly, PTP1B inhibition can provide an alternate treatment for PTPase-mediated disorders such as diabetes.Type: ApplicationFiled: September 23, 2008Publication date: February 19, 2009Applicant: WyethInventors: Jinbo Lee, Steven J. Kirincich, Michael J. Smith, Douglas P. Wilson, Bruce C. Follows, Zhao-Kui Wan, Diane M. Joseph-McCarthy, David V. Erbe, Yan-Ling Zhang, Weixin Xu, Steve Y. Tam