Oxadiazole Ring Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/269.4)
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Publication number: 20100247514Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: May 5, 2008Publication date: September 30, 2010Inventors: Zhaoning Zhu, William J. Greenlee, Zhong-Yue Sun, Gioconda Gallo, Theodros Asberom, Xianhai Huang, Xiaohong Zhu, Mark D. McBriar, Dmitri A. Pissarnitski, Zhiqiang Zhao, Ruo Xu, Hongmei Li, Anandan Palani, Johannes H. Voigt, Robert D. Mazzola, JR., John Clader, Hubert Josien, Jun Qin
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Publication number: 20100234404Abstract: Compounds and compositions for modulating the activity of p38 kinases are provided, including p38?, and p38? kinase. Methods for treating, preventing or ameliorating one or more symptoms of a p38 kinase mediated disease or disorder are also provided.Type: ApplicationFiled: May 28, 2010Publication date: September 16, 2010Inventors: Hengyuan Lang, Jiong Lan, Yungeng Fang
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Publication number: 20100227845Abstract: The present invention relates to compounds represented by Formula (I), Formula (II) and Formula (III) and pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical compositions comprising the instant compounds. This invention further provides methods to treat and prevent pain, respiratory and non-respiratory diseases.Type: ApplicationFiled: October 14, 2008Publication date: September 9, 2010Inventors: Zhicai Wu, John C. Hartnett
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Patent number: 7781460Abstract: The present invention relates to isoxazoline derivatives of structure Ia, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. Compounds disclosed herein can be useful in the treatment of CNS disorders, AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases especially in humans. Processes for the preparation of disclosed compounds are provided, as well as pharmaceutical compositions containing the disclosed compounds, and their use as phosphodiesterase (PDE) type IV inhibitors.Type: GrantFiled: August 30, 2006Date of Patent: August 24, 2010Assignee: Ranbaxy Laboratories LimitedInventors: Venkata Palle, Sarala Balachandran, Lalit Kumar Baregama, Saswati Chakladar, Sarika Ramnani, Nagarajan Muthukamal, Abhijit Ray, Sunanda G. Dastidar
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Publication number: 20100204278Abstract: The present invention encompasses compounds of Formula (I) as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: October 16, 2007Publication date: August 12, 2010Inventors: Richard T. Beresis, Steven L. Colletti
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Publication number: 20100168113Abstract: This invention relates to novel substituted nitrocatechol derivatives, their use in the treatment of some central and peripheral nervous system disorders and pharmaceutical compositions containing them.Type: ApplicationFiled: April 10, 2007Publication date: July 1, 2010Inventors: David Alexander Learmonth, Laszlo Erno Kiss, Pedro Nuno Leal Palma, Humberto Dos Santos Ferreira, Patricio Manuel Vieira Soares da Silva
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Publication number: 20100168159Abstract: [Problems] To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.Type: ApplicationFiled: January 29, 2010Publication date: July 1, 2010Applicant: ASTELLAS PHARMA INC.Inventors: Hironori Harada, Kazuyuki Hattori, Kazuya Fujita, Masataka Morita, Sunao Imada, Yoshito Abe, Hiromichi Itani, Tatsuaki Morokata, Hideo Tsutsumi
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Publication number: 20100168005Abstract: The invention relates to pyridin-3-yl derivatives of Formula (I) wherein R1, R2, R3, R4, R5; R6 and A are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.Type: ApplicationFiled: September 6, 2007Publication date: July 1, 2010Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner
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Publication number: 20100144778Abstract: The present invention encompasses compounds of Formula (I): as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: June 26, 2006Publication date: June 10, 2010Inventors: Subharekha Raghavan, Steven L. Colletti, Fa-Xiang Ding, Hong Shen, James R. Tata, Ashley Rouse Lins, Abigail Lee Smenton, Weichun Chen, Darby Rye Schmidt, George Scott Tria
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Publication number: 20100120794Abstract: The invention relates to compounds of formula I and to pharmaceutically acceptable salts, prodrugs, solvates or hydrates thereof; wherein B, D, E, R1, R2, R3, R4, R5, R8, m, n, p, q, r, s, t and u are as defined herein. This invention also relates to a method of using such compounds in the treatment of hyperproliferative diseases and autoimmune diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: January 4, 2010Publication date: May 13, 2010Inventors: Samit Kumar Bhattacharya, Matthew Frank Brown, Peter Hans Dorff, Susan LaGreca
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Publication number: 20100113796Abstract: The invention relates to compounds of formula (I) wherein one of R5 and R6 is hydrogen or R2 and the other is (a) pharmaceutical compositions containing them and their use in the treatment of conditions or disorders which are mediated via the S1P1 receptor.Type: ApplicationFiled: December 19, 2007Publication date: May 6, 2010Inventor: Mahmood AHMED
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Publication number: 20100113529Abstract: The invention relates to the use of an oxodiazolyl compound (I) for the preparation of a medicament for the prevention or treatment of central and peripheral nervous system associated disorders, wherein said medicament is administered according to a dosing regimen having a dosing periodicity ranging from about twice a day to about once every other day.Type: ApplicationFiled: October 10, 2007Publication date: May 6, 2010Inventors: David Alexander Learmonth, Laszlo Erno Kiss, Pedro Nuno Leal Palma, Humberto dos Santos Ferreira, Patricio Manuel Vieira Araujo Soares da Silva
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Publication number: 20100113528Abstract: The present invention provides compounds of formula (I) or salts thereof: having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders mediated by S1P1 receptors.Type: ApplicationFiled: April 17, 2008Publication date: May 6, 2010Inventors: Mahmood Ahmed, Gerard Martin Paul Giblin, James Myatt, David Norton, Dean Andrew Rivers
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Publication number: 20100099718Abstract: The present invention provides an antifungal agent that has excellent antifungal action, and is also excellent in terms of its properties, safety, and metabolic stability.Type: ApplicationFiled: September 20, 2007Publication date: April 22, 2010Inventors: Masayuki Matsukura, Satoshi Inoue, Keigo Tanaka, Norio Murai, Shuji Shirotori
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Publication number: 20100087491Abstract: The invention relates to novel diaryl oxadiazole compounds of Formula I: in which all the variables are as defined in the specification; to their preparation and to their use in the treatment of disorder or disease mediated by lymphocytes.Type: ApplicationFiled: September 27, 2007Publication date: April 8, 2010Inventors: Rainer Albert, Nigel Graham Cooke, Ian Lewis, Sven Weiler, Frederic Zecri
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Publication number: 20100087417Abstract: The invention relates to novel amino-pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.Type: ApplicationFiled: February 29, 2008Publication date: April 8, 2010Inventors: Martin Bolli, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jorg Velker
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Patent number: 7687491Abstract: A compound having immunosuppressive activity with low toxicity or a pharmacological salt thereof.Type: GrantFiled: October 19, 2007Date of Patent: March 30, 2010Assignee: Daiichi Sankyo Company, LimitedInventors: Takahide Nishi, Tsuyoshi Nakamura, Yukiko Sekiguchi, Yumiko Mizuno, Takaichi Shimozato, Futoshi Nara
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Publication number: 20100048639Abstract: The present invention relates to novel oxadiazole compounds of formula (I) having pharmacological activity, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: ApplicationFiled: December 19, 2007Publication date: February 25, 2010Applicant: GLAXO GROUP LIMITEDInventors: Mahmood Ahmed, James Myatt, David Norton, Dean Andrew Rivers
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Patent number: 7659294Abstract: The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.Type: GrantFiled: October 18, 2005Date of Patent: February 9, 2010Assignee: Merck & Co., Inc.Inventors: Jeffrey John Hale, Lin Yan
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Publication number: 20100029685Abstract: This invention relates to oxadiazolyl and thiadiazolyl derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: October 24, 2007Publication date: February 4, 2010Applicant: NeuroSearch A/SInventors: Bjarne H. Dahl, Dan Peters, Gunnar M. Olsen, Daniel B. Timmermann, Susanne Jorgensen
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Publication number: 20100022597Abstract: The present invention relates to 2-adamantyl-butyramide derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.Type: ApplicationFiled: November 22, 2007Publication date: January 28, 2010Inventors: Didier Roche, Denis Carniato, Liliane Doare, Christine Charon, Caroline Leriche
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Publication number: 20090312347Abstract: This invention relates to novel oxadiazole derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: April 24, 2006Publication date: December 17, 2009Inventors: Bjarne H. Dahl, Dan Peters, Gunnar M. Olsen, Daniel B. Timmermann, Susanne Jørgensen
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Patent number: 7629337Abstract: Heterocyclic compounds that bind chemokine receptors and inhibit the binding of their natural ligands are disclosed. The invention compounds are protective against infection by HIV and exert effects characteristic of antagonists to the CXCR4 receptor.Type: GrantFiled: July 27, 2006Date of Patent: December 8, 2009Assignee: Genzyme CorporationInventors: Gary J. Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols
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Publication number: 20090281060Abstract: Compounds of Formula (I), R1-A-V—B—R2; or pharmaceutically acceptable salts thereof, are agonists of GPR116 and are useful as regulators of satiety, e.g. for the treatment of obesity, and for the treatment of diabetes.Type: ApplicationFiled: December 23, 2004Publication date: November 12, 2009Applicant: PROSIDION LIMITEDInventors: Matthew Fyfe, John King-Underwood, Lisa Sarah Bertram (Gardner), Gerard Hugh Thomas, Martin Procter, Chrystelle Rasamison, Karen Schofield
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Publication number: 20090264653Abstract: Indoles that have activity as inhibitors of FAAH are described as are indoles and indole derivatives that have activity as inhibitors of DAO.Type: ApplicationFiled: December 18, 2006Publication date: October 22, 2009Inventors: Wilmin Bartolini, Brian M Cali, Barbara Chen, Yueh-Tyng Chien, Mark G. Currie, G. Todd Milne, James Philip Pearson, John Jeffrey Talley, Jane Yang, Craig Zimmerman, Charles Kim, Kevin Sprott, Timothy Barden, Regina Lundigran, Ara Mermerian
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Patent number: 7605171Abstract: The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.Type: GrantFiled: December 13, 2004Date of Patent: October 20, 2009Assignee: Merck & Co., Inc.Inventors: Vincent J. Colandrea, George A. Doherty, Jeffrey J. Hale, Pei Huo, Irene E. Legiec, Leslie Toth, Petr Vachal, Lin Yan
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Publication number: 20090239798Abstract: The present application relates to novel compounds, methods and formulations useful for the oral delivery of a glucagon like peptide-1 compound or a melanocortin 4 receptor agonist peptide.Type: ApplicationFiled: November 3, 2008Publication date: September 24, 2009Applicant: Emisphere Technologies, Inc.Inventors: Louis Nickolaus Jungheim, John McNeill McGill, III, Kenneth Jeff Thrasher, Robert Jason Herr, Muralikrishna Valluri
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Publication number: 20090197897Abstract: The present invention relates to new compounds which are Oxadiazole derivatives of formula (I) wherein B, P, Q, W, R1 and R2 are defined in the description. Invention compounds are useful in the prevention or treatment of central or peripheral nervous system disorders as well as other disorders modulated by mGluR5 receptors.Type: ApplicationFiled: May 17, 2006Publication date: August 6, 2009Applicant: Addex Pharma SAInventors: Piergiuliano Bugada, Stefania Gagliardi, Emmanuel Le Poul, Vincent Mutel, Giovanni Palombi, Jean-Philippe Rocher
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Publication number: 20090186891Abstract: The present invention provides compounds of the following structure; A-Q-B—C-D that are useful for treating conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: ApplicationFiled: September 26, 2008Publication date: July 23, 2009Inventors: Young-Shin Kwak, Gary Mark Coppola
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Publication number: 20090176842Abstract: The invention relates to substituted arylsulfonamides of formula (I) and methods for their preparation as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, particularly against cytomegaloviruses.Type: ApplicationFiled: September 3, 2008Publication date: July 9, 2009Inventors: Niels Svenstrup, Holger Zimmermann, Dagmar Karthaus, Andreas Goeller, Dirk Heimbach, Kerstin Henninger, Dieter Lang, Daniela Paulsen, Bernd Riedl, Rudolf Schohe-Loop, Joachim Schuhmacher, Tobias Wunberg
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Publication number: 20090170907Abstract: This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.Type: ApplicationFiled: June 6, 2006Publication date: July 2, 2009Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Philip Stewart Turnbull, Rodolfo Cadilla, Andrew Lamont Larkin, Eugene Lee Stewart, Katherine Stetson
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Publication number: 20090170891Abstract: The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: April 6, 2007Publication date: July 2, 2009Inventors: Steven L. Colletti, James R. Tata, Weichun Chen, Richard T. Beresis, Fa-Xiang Ding, Darby Rye Schmidt, Hong Shen, Subharekha Raghavan
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Publication number: 20090137636Abstract: The present invention relates to polycyclic compounds, processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: ApplicationFiled: January 25, 2007Publication date: May 28, 2009Inventors: Rainer Albert, Frederic Zecri
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Publication number: 20090118506Abstract: The present invention discloses compounds of formula I, II or, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.Type: ApplicationFiled: September 17, 2008Publication date: May 7, 2009Inventors: IN JONG KIM, Tongzhu Liu, Yao-Ling Qiu, Guoqiang Wang, Jiang Long, Heejin Kim, Yanchun Wang, Ly Tam Phan, Yat Sun Or
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Patent number: 7517994Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: GrantFiled: May 18, 2005Date of Patent: April 14, 2009Assignee: Array Biopharma Inc.Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
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Publication number: 20090093462Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds (I) pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: October 19, 2005Publication date: April 9, 2009Inventors: Ulricn Abel, Holger Deppe, Achim Feurer, Ulrich Gradler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
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Publication number: 20090066245Abstract: The present invention is a light-emitting device material characterized by containing a pyrene compound represented by the following general formula (1): wherein R1 to R10 are specific functional groups, provided that at least one of the R1 to R10 is a substituent represented by the following general formula (2): wherein R11 to R14 are specific functional groups, provided that any one of the R11 to R14 is used for a single bond with a pyrene skeleton; X1 is a group represented by the following general formula (3): wherein R15 is a specific functional group; and Y1 to Y4 is selected from among a nitrogen atom and a carbon atom, provided that at least one of the Y1 to Y4 is a nitrogen atom and at least one thereof is a carbon atom, and no substituents exist on the nitrogen atom in the case of the nitrogen atom. This material provides a light-emitting device having high luminous efficiency and excellent durability.Type: ApplicationFiled: February 23, 2006Publication date: March 12, 2009Applicant: TORAY INDUSTRIES, INC.Inventors: Kazunori Sugimoto, Seiichiro Murase, Daisuke Kitazawa, Kazumasa Nagao, Takafumi Ogawa, Tsuyoshi Tominaga
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Publication number: 20090062269Abstract: The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: February 2, 2007Publication date: March 5, 2009Inventors: Subharekha Raghavan, Darby Rye Schmidt, Steven L. Colletti, Abigail Lee Smenton
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Publication number: 20090042926Abstract: The present invention encompasses compounds of Formula (I): as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: December 20, 2006Publication date: February 12, 2009Inventors: Jason Imbriglio, Steven L. Colletti, James R. Tata, Richard T. Beresis, Daria Marley, Subharekha Raghavan, Darby Rye Schmidt, Ashley Rouse Lins, Abigail L. Smenton, Weichun Chen, Hong Shen, Fa-Xiang Ding, Rena Bodner
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Publication number: 20080317676Abstract: This invention relates to new fluorescent chemical entities that are designed to attach to biocompatible molecules to form in vivo optical imaging agents.Type: ApplicationFiled: September 1, 2006Publication date: December 25, 2008Inventors: Milind Rajopadhye, Kevin Groves
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Publication number: 20080269236Abstract: The invention relates to 1,2,4 oxadiazole compounds and analogs thereof, represented by formula (II), and compositions and methods of use thereof.Type: ApplicationFiled: June 6, 2008Publication date: October 30, 2008Applicant: ABBOTT LABORATORIESInventors: Jianguo Ji, Chih-Lung Lee, Kevin B. Sippy, Tao Li, Murali Gopalakrishnan
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Publication number: 20080255202Abstract: The present application relates to novel phenylthioacetic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders, in particular dyslipidaemias and arteriosclerosis.Type: ApplicationFiled: March 26, 2005Publication date: October 16, 2008Applicant: Bayer HealthCare AGInventors: Hilmar Bischoff, Elke Dittrich-Wengenroth, Nils Griebenow, Axel Kretschmer, Joachim Kruger, Elisabeth Woltering, Lars Barfacker, Claudia Hirth-Dietrich, Peter Ellinghaus, Martin Raabe, Stephen Bartel, Christian Pilger, Ulrich Rosentreter, Klemens Lustig, Armin Kern, Dieter Lang
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Publication number: 20080249093Abstract: The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.Type: ApplicationFiled: December 13, 2004Publication date: October 9, 2008Applicant: MERCK & CO., INC.Inventors: Vincent J. Colandrea, George A. Doherty, Jeffrey J. Hale, Pei Huo, Irene E. Legiec, Leslie Toth, Petr Vachal, Lin Yan
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Publication number: 20080234273Abstract: Compounds of formula (I) wherein R1, R2, R3, and HET-1 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: ApplicationFiled: June 3, 2006Publication date: September 25, 2008Inventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Publication number: 20080214620Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, wherein R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl; carbocyclyl which may optionally be substituted by alkyl; alkenyl; alkynyl, provided a triple bond is not adjacent to X; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl in which heterocyclyl may optionally be substituted by alkyl; -alkyl-carbocyclyl in which carbocyclyl may optionally be substituted by alkyl; aryl; heteroaryl; or H; X represents S or NR3; R3 represents H or C1-4 alkyl.Type: ApplicationFiled: November 28, 2007Publication date: September 4, 2008Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Daniel Ramsbeck, Mirko Buchholz, Andre J. Niestroj
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Publication number: 20080167286Abstract: The invention relates to a composition comprising a neuronal nicotinic receptor ligand and an ?4?2 positive allosteric modulator, a method of using the same, and a related article of manufacture.Type: ApplicationFiled: December 10, 2007Publication date: July 10, 2008Applicant: Abbott LaboratoriesInventors: Murali Gopalakrishnan, Marie P. Honore, Chih-Hung Lee, John Malysz, Jianguo Ji, Tao Li, Michael R. Schrimpf, Kevin B. Sippy, David J. Anderson
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Patent number: 7390804Abstract: An N-containing five-membered ring compound of formula (I) wherein all symbols are the same as described in the specification, and a non-toxic salt thereof. The compound of formula (I) has an inhibitory activity against cysteine protease and therefore it is useful as an agent for the prophylaxis and/or treatment of inflammatory diseases, diseases induced by apoptosis, diseases induced by disorders of immune responses, autoimmune diseases, diseases induced by decomposition of proteins which compose organism, shock, circulatory system disorders, blood coagulation systems disorders, malignant tumors, acquired immune deficiency syndrome (AIDS) and AIDS-related complex (ARC), parasitic diseases, nerve degeneration diseases, pulmonary disorders, bone resorption diseases, endocrinesthenia, etc.Type: GrantFiled: December 22, 2004Date of Patent: June 24, 2008Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kazuyuki Ohmoto, Iori Itagaki
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Patent number: 7390907Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: September 30, 2004Date of Patent: June 24, 2008Assignee: Amgen Inc.Inventors: Ning Chen, Thomas Nixey, Mark H. Norman
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Patent number: 7365196Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.Type: GrantFiled: March 15, 2001Date of Patent: April 29, 2008Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
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Patent number: 7351724Abstract: Certain oxadiazole ketone compounds are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as MS).Type: GrantFiled: October 14, 2005Date of Patent: April 1, 2008Assignee: The Scripps Research InstituteInventor: Dale L. Boger