Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 546/18)
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Patent number: 8084609Abstract: The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. The compounds of present invention are described with formula (I) wherein R1 to R5, R5?, R7 to R9, R7?, R8?, X and Y are as defined in the specification.Type: GrantFiled: December 13, 2007Date of Patent: December 27, 2011Assignee: Hoffman-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20110306765Abstract: The present invention relates to a method comprising reducing a ketone of formula I: with an enantioselective hydrogenating agent to form substantially enantiomerically pure alcohol of formula II: where R—R4 and m are as defined herein. The method of the present invention is useful for making CCR2 modulators as wells as precursors CCR2 modulators.Type: ApplicationFiled: February 23, 2010Publication date: December 15, 2011Inventors: Pamela A. Haile, Clark A. Sehon, Huan Wang
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Publication number: 20110306595Abstract: The present invention is directed to spiropyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: February 20, 2010Publication date: December 15, 2011Inventors: Kun Liu, Shawn J. Stachel, Craig A. Coburn, Thomas G. Steele, Richard Soll, Hao Wu, Xuanjin Peng, Yaxian Cai, Xiaoxiang Du, Jian Li
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Patent number: 8076482Abstract: There are provided compounds of the formula or a pharmaceutically acceptable salt or ester thereof wherein X, Y, W, W?, V, V?, V?, R1, R2 and R3 are as herein described. The compounds have utility as antiproliferative agents, especially, as anticancer agents.Type: GrantFiled: March 29, 2010Date of Patent: December 13, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Li Chen, Xingchun Han, Song Yang, Zhuming Zhang
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Patent number: 8076349Abstract: Compounds according to formula (I): wherein A, R1 and R2 are as defined herein, and the pharmaceutically acceptable salts, hydrates and solvates thereof are useful for the modulation of CCR5 chemokine receptor activity.Type: GrantFiled: December 9, 2005Date of Patent: December 13, 2011Assignee: Virochem Pharma Inc.Inventors: Laval Chan Chun Kong, Christophe Moinet, Marc Courchesne, Louis Vaillancourt, Monica Bubenik
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Patent number: 8076350Abstract: The invention relates to compounds that are spirocyclic azaadamantane derivatives derivatives, particularly spirocyclic azaadamantanyl ether or amine derivatives, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.Type: GrantFiled: November 20, 2007Date of Patent: December 13, 2011Assignee: Abbott LaboratoriesInventors: Jianguo Ji, Michael R. Schrimpf, Kevin B. Sippy, Tao Li, Chih-Hung Lee
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Publication number: 20110301352Abstract: Methods are provided for making pharmaceutical-grade cis-2-methylspiro(1,3-oxathiolane-5,3?)quinuclidine and pharmaceutically acceptable salts thereof by isomerizing racemic 2-methylspiro(1,3-oxathiolane-5,3?)quinuclidine to cis-2-methylspiro(1,3-oxathiolane-5,3?)quinuclidine and subsequent purification of the C-MSOQ by salt formation with inexpensive and commercially available material such as sulfuric acid. Purification methods are disclosed which employ an organic solvent/water system and recrystallization with an organic solvent such as acetone.Type: ApplicationFiled: June 8, 2010Publication date: December 8, 2011Applicant: APICORE, LLCInventors: Ravishanker Kovi, Jayaraman Kannapan, Talluri Buhshaiah Chowdari, Chirag Vasantlal Shah
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Patent number: 8071771Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B, E1, E2, E3, E4, E5, G1, G2 and R6 are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.Type: GrantFiled: November 14, 2006Date of Patent: December 6, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Harold G. Selnick, Craig A. Stump, Cory R. Theberge, C. Blair Zartman
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Patent number: 8071770Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B, E1, E2, E3, E4, E5, G1, G2 and R6 are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.Type: GrantFiled: November 14, 2006Date of Patent: December 6, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Craig A. Stump, Cory R. Theberge, Michael R. Wood, C. Blair Zartman
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Patent number: 8071773Abstract: The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R1, R2, W, X, Y, Z and n have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.Type: GrantFiled: May 30, 2006Date of Patent: December 6, 2011Assignee: NovartisAGInventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Aleksandar Stojanovic, Christiane Marti, Nathalie Jotterand, Christoph Schumacher, Michael Quirmbach
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Publication number: 20110278549Abstract: The present invention relates to a new fused cyclic compound, and an organic electronic device using the same. Since the compound according to an exemplary embodiment of the present invention may be used as a material of an organic material layer of the organic electronic device and in particular may effectively inject, transport or extract a hole, it is possible to provide an organic electronic device having excellent efficiency and performance.Type: ApplicationFiled: November 12, 2010Publication date: November 17, 2011Applicant: LG CHEM, LTD.Inventors: Kong-Kyeom Kim, Jae-Chol Lee, Ji-Eun Kim, Hyun Nam, Jun-Gi Jang, Byung-Sun Jeon
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Publication number: 20110275613Abstract: The invention relates to organic compounds which have interesting pharmaceutical properties. In particular, the compounds are useful in the treatment and/or prevention of infections such as those caused by Plasmodium falciparum, Plasmodium vivax, Plasmodium malariae, Plasmodium ovale, Trypanosoma cruzi and parasites of the Leishmania genus such as, for example. Leishmania donovani. The invention also relates to pharmaceutical compositions containing the compounds, as well as processes for their preparation.Type: ApplicationFiled: July 19, 2011Publication date: November 10, 2011Applicant: NOVARTIS AGInventors: Shi Hua ANG, Philipp KRASTEL, Seh Yong LEONG, Liying Jocelyn TAN, Wei Lin Josephine WONG, Bryan K.S. YEUNG, Bin ZOU
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Patent number: 8053442Abstract: The invention relates to organic compounds which have interesting pharmaceutical properties. In particular, the compounds are useful in the treatment and/or prevention of infections such as those caused by Plasmodium falciparum, Plasmodium vivax, Plasmodium malariae, Plasmodium ovale, Trypanosoma cruzi and parasites of the Leishmania genus such as, for example, Leishmania donovani. The invention also relates to pharmaceutical compositions containing the compounds, as well as processes for their preparation.Type: GrantFiled: April 27, 2009Date of Patent: November 8, 2011Assignee: Novartis AGInventors: Shi Hua Ang, Philipp Krastel, Seh Yong Leong, Liying Jocelyn Tan, Wei Lin Josephine Wong, Bryan KS Yeung, Bin Zou
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Patent number: 8053576Abstract: Spirocyclic cyclohexane compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them.Type: GrantFiled: February 17, 2009Date of Patent: November 8, 2011Assignee: Gruenenthal GmbHInventors: Claudia Hinze, Otto Aulenbacher, Bernd Sundermann, Stefan Oberboersch, Elmar Friderichs, Werner Englberger, Babette-Yvonne Koegel, Klaus Linz, Hans Schick, Helmut Sonnenschein, Birgitta Henkel, Valerie Sarah Rose, Michael Jonathan Lipkin
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Publication number: 20110263605Abstract: The disclosure provides compounds of formula I, including Ia, Ib, Ic, or Id, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic ?7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.Type: ApplicationFiled: October 19, 2010Publication date: October 27, 2011Inventors: Ivar M. McDonald, Robert A. Mate, James H. Cook, II, Dalton King, Richard E. Olson, Nenghui Wang, Christiana I. Iwuagwu, F. Christopher Zusi, Matthew D. Hill, Haiquan Fang, John E. Macor
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Patent number: 8044202Abstract: The present invention is concerned with novel indol-3-yl-carbonyl-azaspiropiperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein R1 to R6, U, V, W, X, Y and Z are as defined in the specification.Type: GrantFiled: December 20, 2007Date of Patent: October 25, 2011Assignee: Hoffmann-la Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20110251224Abstract: This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.Type: ApplicationFiled: April 1, 2011Publication date: October 13, 2011Inventors: Mikhail Chafeev, Nagasree Chakka, Sultan Chowdhury, Robert Fraser, Jianmin Fu, Duanjie Hou, Tom Hsieh, Rajender Kamboj, Shifeng Liu, Vandna Ralna, Mehran Seid Bagherzadeh, Jianyu Sun, Shaoyi Sun, Serguei Sviridov
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Publication number: 20110251190Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and other related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, R2, R7, X and Y of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: March 14, 2011Publication date: October 13, 2011Applicant: Amgen Inc.Inventors: Yuan CHENG, Ryan White, Albert Amegadzie, James Brown, Alan C. Cheng, Erin F. Dimauro, Thomas Dineen, Oleg Epstein, Vijay Keshav Gore, Jason Brooks Human, Ted Judd, Charles Kreiman, Qingyian Liu, Patricia Lopez, Vu Van Ma, Isaac Marx, Ana Minatti, Hanh Nho Nguyen, Nick A. Paras, Vinod F. Patel, Wenyuan Qian, Matthew Weiss, Qiufen Xue, Xiao Mei Zheng, Wenge Zhong
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Patent number: 8034936Abstract: Spirocyclic cyclohexane compounds useful in pharmaceutical compositions for use in the treatment of substance dependency.Type: GrantFiled: November 4, 2010Date of Patent: October 11, 2011Assignee: Gruenenthal GmbHInventors: Elmar Friderichs, Babette-Yvonne Koegel, Klaus Linz
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Patent number: 8022213Abstract: Present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them. The active compounds of the present invention are useful in the treatment of anxiety and depressive disorders and other diseases. The compounds of present invention have the general formula (I) wherein R1 to R11 and X are as defined in the description.Type: GrantFiled: November 30, 2007Date of Patent: September 20, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Patent number: 8017775Abstract: An object of the present invention is to study synthesis of a novel 1,2-dihydroquinoline derivative and to find a pharmacological action of the derivative. A compound represented by the general formula (1) or a salt thereof is effective in the treatment of a glucocorticoid receptor-related disease. In the formula, the ring X represents a benzene ring or a pyridine ring; R1 represents a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, an amino group or the like; p represents an integer of 0 to 5; R2 represents a halogen atom, an alkyl group, a hydroxy group or the like; q represents an integer of 0 to 2; R3 represents a hydrogen atom, an alkyl group, an alkenyl group or the like; R4 and R5 represent a hydrogen atom or the like; R6 represents a hydrogen atom or the like; A represents an alkylene group or the like; and R7 represents OR8, NR8R9, SR8, S(O)R8 or S(O)2R8, wherein R8 represents an aryl group, a heterocyclic group or the like and R9 represents a hydrogen atom or the like.Type: GrantFiled: September 14, 2006Date of Patent: September 13, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Mamoru Matsuda, Toshiyuki Mori, Kenji Kawashima, Masato Nagatsuka, Sachiko Kobayashi, Minoru Yamamoto, Masatomo Kato, Miwa Takai, Tomoko Oda
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Patent number: 8008496Abstract: The compounds represented in general formula (1) and a salt thereof are useful for glucocorticoid receptor modulator. The R1 represents a hydrogen atom or a lower alkyl group; R2 represents a hydrogen atom or a lower alkyl group; R3 and R4 may be the same or different and represent a hydrogen atom or a lower alkyl group; R5 represents a hydrogen atom or a lower alkyl group; R6 represents a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group or a nitro group; X represents —C(O)—, —C(O)NR8—, —S(O)2— and the like; R7 and/or R8 may be the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, a heterocyclic group which may have a substituent, a lower alkoxy group which may have a substituent and the like; Y represents a lower alkylene group; Z represents a chalcogen atom; and P represents 0, 1, 2 or 3.Type: GrantFiled: November 14, 2007Date of Patent: August 30, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Mamoru Matsuda, Masato Nagatsuka, Toshiyuki Mori, Sachiko Kobayashi, Masatomo Kato, Miwa Takai
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Patent number: 8008497Abstract: The compounds represented in general formula (1) and a salt thereof are useful for glucocorticoid receptor modulator. The R1 represents a hydrogen atom or a lower alkyl group; R2 represents a hydrogen atom or a lower alkyl group; R3 and R4 may be the same or different and represent a hydrogen atom or a lower alkyl group; R5 represents a hydrogen atom or a lower alkyl group; R6 represents a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, a nitro group or a cyano group; X represents —C(O)—, —C(O)NR8—, —S(O)2— and the like; R7 and/or R8 may be the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, a heterocyclic group which may have a substituent, a lower alkoxy group which may have a substituent and the like; Y represents a lower alkylene group; Z represents a benzene ring or a heterocyclic ring; and P represents 0, 1, 2 or 3.Type: GrantFiled: November 14, 2007Date of Patent: August 30, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Mamoru Matsuda, Masato Nagatsuka, Toshiyuki Mori, Sachiko Kobayashi, Masatomo Kato, Miwa Takai
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Patent number: 8008498Abstract: The compounds represented in general formula (1) and a salt thereof are useful for glucocorticoid receptor modulator. The R1 represents a hydrogen atom or a lower alkyl group; R2 represents a hydrogen atom or a lower alkyl group; R3 and R4 may be the same or different and represents a hydrogen atom or a lower alkyl group; R5 represents a hydrogen atom or a lower alkyl group; R6 represents a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, a nitro group or a cyano group; X represents —C(O)—, —C(O)NR8—, —S(O)2— and the like; R7 and/or R8 may be the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, a heterocyclic group which may have a substituent, a lower alkoxy group which may have a substituent and the like; Y represents a lower alkylene group; and P represents 0, 1, 2 or 3.Type: GrantFiled: November 14, 2007Date of Patent: August 30, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Mamoru Matsuda, Masato Nagatsuka, Toshiyuki Mori, Sachiko Kobayashi, Masatomo Kato, Miwa Takai
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Patent number: 8008279Abstract: The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases, including cathepsins B, K, C, F, H, L, O, S, W and X. Of particular interest are diseases associated with Cathepsin K.Type: GrantFiled: June 25, 2008Date of Patent: August 30, 2011Assignee: AstraZeneca ABInventors: Alexander Graham Dossetter, Nicola Murdoch Heron
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Publication number: 20110207700Abstract: The present invention relates to the compound represented by formula (I): (wherein, all the symbols have the same meaning as that of the specification), a salt thereof, a solvate thereof or a prodrug thereof. Since the compound of the present invention has an anti stress action, it is useful for preventive and/or therapeutic agent for a disease caused by stress, especially a digestive system disease caused by stress and is superior to oral absorption.Type: ApplicationFiled: April 29, 2011Publication date: August 25, 2011Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Kazuyuki OHMOTO, Masashi KATO, Yoshifumi KAGAMIISHI, Junichiro MANAKO
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Patent number: 8003792Abstract: The present invention is directed to compounds of Formula I: (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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 CGRP is involved.Type: GrantFiled: September 9, 2005Date of Patent: August 23, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Cory R. Theberge, Craig A. Stump, Xufang Zhang, Steven N. Gallicchio, C. Blair Zartman
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Publication number: 20110198571Abstract: Organic compounds and organic electroluminescence devices employing the same are provided. The organic compound has a chemical structure represented as follows: wherein: R1, R2, R3, R4, R5, R6, and R7 are each independently an H, C1-8 alkyl group, C1-8 alkoxy group, C1-8 halo-alkyl group, aryl group, heteroaryl group, cycloalkyl group, hetero-cycloalkyl group, or cycloaliphatic group; Z is independently and R8 and R9 are each independent an aryl group, heteroaryl group, cycloalkyl group, hetero-cycloalkyl, or cycloaliphatic group.Type: ApplicationFiled: August 20, 2010Publication date: August 18, 2011Applicant: INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTEInventors: Heh-Lung Huang, Chi-Jen Lin, Teng-Chih Chao, Hao-Chun Lee, Chien-Hong Cheng
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Publication number: 20110195929Abstract: Described are various compounds and methods for the treatment of flaviviral infections. In particular, alkaloids and imino sugars in arabinose and/or lyxose stereochemical configuration with antiflaviviral activity are described.Type: ApplicationFiled: August 4, 2009Publication date: August 11, 2011Applicant: SUMMIT CORPORATION PLCInventors: Olivier De Moor, Graeme Horne, Penny Jane Middleton, Frank Schroer, Stephen Paul Wren, Maria Ines Passos Eleuterio, Renate Van Well, Colin Richard Dorgan, Francis Xavier Wilson, Robert Nash, Richard Storer, Graham Michael Wynne, Alan Geoffrey Roach, Akane Kawamura, Jonathon Mark Tinsley
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Publication number: 20110195933Abstract: The invention encompasses pyrazolo[1,5-a]pyridine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: July 27, 2009Publication date: August 11, 2011Inventors: Jason D. Katz, Sandra L. Knowles, James P. Jewell, David L. Sloman, Matthew G. Stanton, Njamkou Noucti
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Publication number: 20110190330Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula IA, IB, I?A or I?B: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.Type: ApplicationFiled: October 13, 2009Publication date: August 4, 2011Applicant: AMGEN INC.Inventors: Sean P. Brown, Paul Dransfield, Xiaohui Du, Zice Fu, Jonathan Houze, XianYun Jiao, Sujen Lai, An-Rong Li, Jiwen Liu, Zhihua Ma, Julio C. Medina, Vatee Pattaropong, Wang Shen, Marc Vimolratana, Yingcai Wang, Zhongyu Wang, Ming Yu, Liusheng Zhu
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Patent number: 7989624Abstract: The present invention is directed to compounds of Formula (I): where variables A1, A2, B, J, K, m, n, R4, R5a, R5b, R5c and X are as defined herein useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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 CGRP is involved.Type: GrantFiled: September 6, 2005Date of Patent: August 2, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Craig A. Stump, Cory R. Theberge
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Patent number: 7982038Abstract: A radioactive compound having the formula: and pharmaceutically-acceptable salts thereof, wherein R1 and Ar are as defined in the specification, enantiomers, in vivo-hydrolysable precursors, pharmaceutical compositions and formulations containing them, methods of using them to treat diseases and conditions either alone or in combination with other therapeutically-active compounds or substances, processes and intermediates used to prepare them and uses of them for diagnostic and analytic purposes.Type: GrantFiled: September 24, 2004Date of Patent: July 19, 2011Assignee: AstraZeneca ABInventors: Peter Dorff, John Gordon, John Richard Heys, Richard A Keith, Dennis J McCarthy, Mark A Smith, Eifion Phillips
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Publication number: 20110171172Abstract: The present invention relates to compounds of Formula (I), below, (wherein R1, R2, R3, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity.Type: ApplicationFiled: October 16, 2008Publication date: July 14, 2011Inventors: M. Arshad Siddiqui, Chaoyang Dai, Umar Faruk Mansoor, Liping Yang, Lalalnthi Dilrukshi Vitharana
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Patent number: 7973047Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.Type: GrantFiled: May 13, 2010Date of Patent: July 5, 2011Assignee: Amgen Inc.Inventors: Wenge Zhong, Stephen Hitchcock, Brian K. Albrecht, Michael D. Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Dean Hickman, Daniel Horne, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig E. Masse, Thomas Nixey, Vinod F. Patel, Lewis Pennington, Matthew Weiss, Qiufen Xue, Bryant Yang, Holger Monenschein, Thomas Nguyen
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Publication number: 20110160238Abstract: This invention relates to octahydroquinolizines for pharmaceutical use with the following formula: (I), X=H, F; R=Methyl, Ethyl, nPropyl, nButyl.Type: ApplicationFiled: June 29, 2009Publication date: June 30, 2011Applicant: 55PHARMA DRUG DISCOVERY & DEVELOPMENT AGInventors: Immanuel Adorjan, Leonhardt Bauer, Klaus Frobel, Clemens Fuernsinn
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Publication number: 20110152304Abstract: The present invention relates to spiroazaindole compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: ApplicationFiled: April 28, 2009Publication date: June 23, 2011Applicant: MERCK SHARP & DOHME CORP.Inventors: Joan M. Pierce (nee Fletcher), Jeffrey J. Hale, Shouwu Miao, Petr Vachal
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Publication number: 20110145970Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.Type: ApplicationFiled: August 26, 2009Publication date: June 23, 2011Applicant: BASF SEInventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
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Publication number: 20110150757Abstract: The present invention relates to compounds of Formula (I), below, (wherein R1, R2, R3, R27, R28, R29, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity.Type: ApplicationFiled: October 16, 2008Publication date: June 23, 2011Inventors: M. Arshad Siddiqui, Chaoyang Dai, Umar Faruk Mansoor, Liping Yang, Lalalnthi Dilrukshi Vitharana, Angie R. Angeles
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Patent number: 7964726Abstract: The present invention relates to the compound represented by formula (I): (wherein, all the symbols has the same meanings as that of the specification), a salt thereof, a solvate thereof or a prodrug thereof. Since the compound of the present invention has an anti stress action, it is useful for preventive and/or therapeutic agent for a disease caused by stress, especially a digestive system disease caused by stress and is superior to oral absorption.Type: GrantFiled: December 21, 2005Date of Patent: June 21, 2011Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kazuyuki Ohmoto, Masashi Kato, Yoshifumi Kagamiishi, Junichiro Manako
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Patent number: 7960403Abstract: Compounds according to formula (I): wherein A, R1, R2 and R3 are defined as defined herein, and the pharmaceutically acceptable salts, hydrates and solvates thereof, are useful for the modulation of CCR5 chemokine receptor activity.Type: GrantFiled: December 9, 2005Date of Patent: June 14, 2011Assignee: Virochem Pharma Inc.Inventors: Laval Chan Chun Kong, Christophe Moinet, Marc Courchesne, Louis Vaillancourt, Charles Blais, Monica Bubenik
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Patent number: 7960401Abstract: The use of a compound of formula I Y is a single bond, C?O, C?S or S(O)m m where m is 0, 1 or 2; the ring represented by T is a 5 or 6 membered heteroaromatic and R1, R2, R3, R8 and Ra are specified organic groups and p is 0, 1, 2, 3, 4, 5 or 6; q is 0, 1, 2, 3, 4, 5 or 6; p+q is 1, 2, 3, 4, 5 or 6; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs; novel compounds are also provided.Type: GrantFiled: December 9, 2004Date of Patent: June 14, 2011Assignee: Syngenta Crop Protection, Inc.Inventors: Jérôme Cassayre, Louis-Pierre Molleyres, Peter Maienfisch, Fredrik Cederbaum
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Patent number: 7960404Abstract: Spirocyclic cyclohexane compounds corresponding to formula I in which R1 and R2 form a pyrrolidine ring or an azetidine ring and which exhibit increased metabolic stability, a process for producing such spirocyclic cyclohexane compounds, pharmaceutical compositions containing such spirocyclic cyclohexane compounds, and the use of such spirocyclic cyclohexane compounds to treat or inhibit pain and/or other disorders.Type: GrantFiled: August 21, 2009Date of Patent: June 14, 2011Assignee: Gruenenthal GmbHInventors: Stefan Schunk, Derek Saunders, Stephanie Harlfinger, Sonja Steufmehl
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Patent number: 7960402Abstract: A compound represented by, e.g. the formula (I): [wherein X, Y, Z, and W each independently represent optionally substituted methine; A, B, and D each independently represent —C(O)—, etc.; Q represents a methine or a nitrogen; and R represents the formula (II-1), optionally substituted with lower alkyl, etc.; (wherein R6 represents a lower alkyl, etc; and R7 and R8 each independently represents a lower alkyl, etc.)] or a pharmaceutically acceptable salt of the compound. The compounds and salt have antagonistic activity against a histamine H3 receptor or inverse agonistic activity against a histamine H3 receptor. They are useful in the prevention or treatment of metabolic diseases, circulatory diseases, or neurotic diseases.Type: GrantFiled: September 6, 2005Date of Patent: June 14, 2011Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Makoto Jitsuoka, Norikazu Ohtake, Nagaaki Sato, Shigeru Tokita, Daisuke Tsukahara
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Publication number: 20110136821Abstract: This invention relates to novel compounds of the Formulae I or II and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ?-HSD 1 in mammals. Formula (I).Type: ApplicationFiled: February 26, 2009Publication date: June 9, 2011Inventors: David A. Claremon, Colin M. Tice, Yuanjie Ye, Suresh B. Singh, Wei He, Wei Zhao, Robert D. Simpson
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Publication number: 20110136804Abstract: Nicotinic acetylcholine receptor ligands of Formula I wherein X, n, R1 and R2 are as described in the specification, diastereoisomers, enantiomers, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing, and methods for using the same.Type: ApplicationFiled: November 5, 2010Publication date: June 9, 2011Applicant: AstraZeneca ABInventors: Hui-Fang Chang, Christopher Holmquist, Eifion Phillips, Timothy Piser, Thomas Simpson, Rebecca Urbanek, James Woods, Hui Xiong
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Patent number: 7951948Abstract: Spirocyclic cyclohexane compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them.Type: GrantFiled: April 19, 2010Date of Patent: May 31, 2011Assignee: Gruenenthal GmbHInventors: Claudia Hinze, Otto Aulenbacher, Bernd Sundermann, Stefan Oberboersch, Elmar Friderichs, Werner Englberger, Babette-Yvonne Koegel, Klaus Linz, Hans Schick, Helmut Sonnenschein, Birgitta Henkel, Valerie Sarah Rose, Michael Jonathan Lipkin
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Publication number: 20110123435Abstract: The present invention relates to compounds of Formula (I), below, (wherein X, R1, R2, R3, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity.Type: ApplicationFiled: October 16, 2008Publication date: May 26, 2011Inventors: M. Arshad Siddiqui, Chaoyang Dai, Umar Faruk Mansoor, Liping Yang, Lalalnthi Dilrukshi Vitharana, Angie R. Angeles
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Patent number: 7947692Abstract: There are presented compounds of the formula or a pharmaceutically acceptable salt thereof, which are active adenosine A2B receptor antagonists and useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea.Type: GrantFiled: May 11, 2007Date of Patent: May 24, 2011Assignee: Hoffmann-La Roche Inc.Inventors: John A. Brinkman, Adrian Wai-Hing Cheung, Fariborz Firooznia, Kevin Richard Guertin, Nicholas Marcopulos, Lida Qi, Jagdish Kumar Racha, Ramakanth Sarabu, Jenny Tan, Jefferson Wright Tilley
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Publication number: 20110118250Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.Type: ApplicationFiled: October 21, 2010Publication date: May 19, 2011Applicant: Amgen Inc.Inventors: Brian K. Albrecht, Denise Lyn Andersen, Michael Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Stephen Hitchcock, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig Masse, Holger Monenschein, Thomas Nguyen, Thomas Nixey, Vinod F. Patel, Lewis Pennington, Matthew Weiss, Qiufen Xue, Bryant Yang, Wenge Zhong