Oxadiazole Ring Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/269.4)
  • Publication number: 20100247514
    Abstract: 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: Application
    Filed: May 5, 2008
    Publication date: September 30, 2010
    Inventors: 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
  • Publication number: 20100234404
    Abstract: 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: Application
    Filed: May 28, 2010
    Publication date: September 16, 2010
    Inventors: Hengyuan Lang, Jiong Lan, Yungeng Fang
  • Publication number: 20100227845
    Abstract: 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: Application
    Filed: October 14, 2008
    Publication date: September 9, 2010
    Inventors: Zhicai Wu, John C. Hartnett
  • Patent number: 7781460
    Abstract: 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: Grant
    Filed: August 30, 2006
    Date of Patent: August 24, 2010
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Venkata Palle, Sarala Balachandran, Lalit Kumar Baregama, Saswati Chakladar, Sarika Ramnani, Nagarajan Muthukamal, Abhijit Ray, Sunanda G. Dastidar
  • Publication number: 20100204278
    Abstract: 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: Application
    Filed: October 16, 2007
    Publication date: August 12, 2010
    Inventors: Richard T. Beresis, Steven L. Colletti
  • Publication number: 20100168113
    Abstract: 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: Application
    Filed: April 10, 2007
    Publication date: July 1, 2010
    Inventors: David Alexander Learmonth, Laszlo Erno Kiss, Pedro Nuno Leal Palma, Humberto Dos Santos Ferreira, Patricio Manuel Vieira Soares da Silva
  • Publication number: 20100168159
    Abstract: [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: Application
    Filed: January 29, 2010
    Publication date: July 1, 2010
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Hironori Harada, Kazuyuki Hattori, Kazuya Fujita, Masataka Morita, Sunao Imada, Yoshito Abe, Hiromichi Itani, Tatsuaki Morokata, Hideo Tsutsumi
  • Publication number: 20100168005
    Abstract: 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: Application
    Filed: September 6, 2007
    Publication date: July 1, 2010
    Applicant: ACTELION PHARMACEUTICALS LTD.
    Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner
  • Publication number: 20100144778
    Abstract: 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: Application
    Filed: June 26, 2006
    Publication date: June 10, 2010
    Inventors: 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
  • Publication number: 20100120794
    Abstract: 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: Application
    Filed: January 4, 2010
    Publication date: May 13, 2010
    Inventors: Samit Kumar Bhattacharya, Matthew Frank Brown, Peter Hans Dorff, Susan LaGreca
  • Publication number: 20100113796
    Abstract: 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: Application
    Filed: December 19, 2007
    Publication date: May 6, 2010
    Inventor: Mahmood AHMED
  • Publication number: 20100113529
    Abstract: 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: Application
    Filed: October 10, 2007
    Publication date: May 6, 2010
    Inventors: David Alexander Learmonth, Laszlo Erno Kiss, Pedro Nuno Leal Palma, Humberto dos Santos Ferreira, Patricio Manuel Vieira Araujo Soares da Silva
  • Publication number: 20100113528
    Abstract: 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: Application
    Filed: April 17, 2008
    Publication date: May 6, 2010
    Inventors: Mahmood Ahmed, Gerard Martin Paul Giblin, James Myatt, David Norton, Dean Andrew Rivers
  • Publication number: 20100099718
    Abstract: 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: Application
    Filed: September 20, 2007
    Publication date: April 22, 2010
    Inventors: Masayuki Matsukura, Satoshi Inoue, Keigo Tanaka, Norio Murai, Shuji Shirotori
  • Publication number: 20100087491
    Abstract: 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: Application
    Filed: September 27, 2007
    Publication date: April 8, 2010
    Inventors: Rainer Albert, Nigel Graham Cooke, Ian Lewis, Sven Weiler, Frederic Zecri
  • Publication number: 20100087417
    Abstract: 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: Application
    Filed: February 29, 2008
    Publication date: April 8, 2010
    Inventors: Martin Bolli, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jorg Velker
  • Patent number: 7687491
    Abstract: A compound having immunosuppressive activity with low toxicity or a pharmacological salt thereof.
    Type: Grant
    Filed: October 19, 2007
    Date of Patent: March 30, 2010
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Takahide Nishi, Tsuyoshi Nakamura, Yukiko Sekiguchi, Yumiko Mizuno, Takaichi Shimozato, Futoshi Nara
  • Publication number: 20100048639
    Abstract: 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: Application
    Filed: December 19, 2007
    Publication date: February 25, 2010
    Applicant: GLAXO GROUP LIMITED
    Inventors: Mahmood Ahmed, James Myatt, David Norton, Dean Andrew Rivers
  • Patent number: 7659294
    Abstract: 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: Grant
    Filed: October 18, 2005
    Date of Patent: February 9, 2010
    Assignee: Merck & Co., Inc.
    Inventors: Jeffrey John Hale, Lin Yan
  • Publication number: 20100029685
    Abstract: 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: Application
    Filed: October 24, 2007
    Publication date: February 4, 2010
    Applicant: NeuroSearch A/S
    Inventors: Bjarne H. Dahl, Dan Peters, Gunnar M. Olsen, Daniel B. Timmermann, Susanne Jorgensen
  • Publication number: 20100022597
    Abstract: 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: Application
    Filed: November 22, 2007
    Publication date: January 28, 2010
    Inventors: Didier Roche, Denis Carniato, Liliane Doare, Christine Charon, Caroline Leriche
  • Publication number: 20090312347
    Abstract: 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: Application
    Filed: April 24, 2006
    Publication date: December 17, 2009
    Inventors: Bjarne H. Dahl, Dan Peters, Gunnar M. Olsen, Daniel B. Timmermann, Susanne Jørgensen
  • Patent number: 7629337
    Abstract: 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: Grant
    Filed: July 27, 2006
    Date of Patent: December 8, 2009
    Assignee: Genzyme Corporation
    Inventors: 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
  • Publication number: 20090281060
    Abstract: 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: Application
    Filed: December 23, 2004
    Publication date: November 12, 2009
    Applicant: PROSIDION LIMITED
    Inventors: Matthew Fyfe, John King-Underwood, Lisa Sarah Bertram (Gardner), Gerard Hugh Thomas, Martin Procter, Chrystelle Rasamison, Karen Schofield
  • Publication number: 20090264653
    Abstract: Indoles that have activity as inhibitors of FAAH are described as are indoles and indole derivatives that have activity as inhibitors of DAO.
    Type: Application
    Filed: December 18, 2006
    Publication date: October 22, 2009
    Inventors: 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
  • Patent number: 7605171
    Abstract: 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: Grant
    Filed: December 13, 2004
    Date of Patent: October 20, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Vincent J. Colandrea, George A. Doherty, Jeffrey J. Hale, Pei Huo, Irene E. Legiec, Leslie Toth, Petr Vachal, Lin Yan
  • Publication number: 20090239798
    Abstract: 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: Application
    Filed: November 3, 2008
    Publication date: September 24, 2009
    Applicant: Emisphere Technologies, Inc.
    Inventors: Louis Nickolaus Jungheim, John McNeill McGill, III, Kenneth Jeff Thrasher, Robert Jason Herr, Muralikrishna Valluri
  • Publication number: 20090197897
    Abstract: 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: Application
    Filed: May 17, 2006
    Publication date: August 6, 2009
    Applicant: Addex Pharma SA
    Inventors: Piergiuliano Bugada, Stefania Gagliardi, Emmanuel Le Poul, Vincent Mutel, Giovanni Palombi, Jean-Philippe Rocher
  • Publication number: 20090186891
    Abstract: 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: Application
    Filed: September 26, 2008
    Publication date: July 23, 2009
    Inventors: Young-Shin Kwak, Gary Mark Coppola
  • Publication number: 20090176842
    Abstract: 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: Application
    Filed: September 3, 2008
    Publication date: July 9, 2009
    Inventors: 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
  • Publication number: 20090170907
    Abstract: 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: Application
    Filed: June 6, 2006
    Publication date: July 2, 2009
    Applicant: SMITHKLINE BEECHAM CORPORATION
    Inventors: Philip Stewart Turnbull, Rodolfo Cadilla, Andrew Lamont Larkin, Eugene Lee Stewart, Katherine Stetson
  • Publication number: 20090170891
    Abstract: 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: Application
    Filed: April 6, 2007
    Publication date: July 2, 2009
    Inventors: Steven L. Colletti, James R. Tata, Weichun Chen, Richard T. Beresis, Fa-Xiang Ding, Darby Rye Schmidt, Hong Shen, Subharekha Raghavan
  • Publication number: 20090137636
    Abstract: The present invention relates to polycyclic compounds, processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Application
    Filed: January 25, 2007
    Publication date: May 28, 2009
    Inventors: Rainer Albert, Frederic Zecri
  • Publication number: 20090118506
    Abstract: 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: Application
    Filed: September 17, 2008
    Publication date: May 7, 2009
    Inventors: IN JONG KIM, Tongzhu Liu, Yao-Ling Qiu, Guoqiang Wang, Jiang Long, Heejin Kim, Yanchun Wang, Ly Tam Phan, Yat Sun Or
  • Patent number: 7517994
    Abstract: 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: Grant
    Filed: May 18, 2005
    Date of Patent: April 14, 2009
    Assignee: Array Biopharma Inc.
    Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
  • Publication number: 20090093462
    Abstract: 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: Application
    Filed: October 19, 2005
    Publication date: April 9, 2009
    Inventors: Ulricn Abel, Holger Deppe, Achim Feurer, Ulrich Gradler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
  • Publication number: 20090066245
    Abstract: 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: Application
    Filed: February 23, 2006
    Publication date: March 12, 2009
    Applicant: TORAY INDUSTRIES, INC.
    Inventors: Kazunori Sugimoto, Seiichiro Murase, Daisuke Kitazawa, Kazumasa Nagao, Takafumi Ogawa, Tsuyoshi Tominaga
  • Publication number: 20090062269
    Abstract: 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: Application
    Filed: February 2, 2007
    Publication date: March 5, 2009
    Inventors: Subharekha Raghavan, Darby Rye Schmidt, Steven L. Colletti, Abigail Lee Smenton
  • Publication number: 20090042926
    Abstract: 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: Application
    Filed: December 20, 2006
    Publication date: February 12, 2009
    Inventors: 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
  • Publication number: 20080317676
    Abstract: This invention relates to new fluorescent chemical entities that are designed to attach to biocompatible molecules to form in vivo optical imaging agents.
    Type: Application
    Filed: September 1, 2006
    Publication date: December 25, 2008
    Inventors: Milind Rajopadhye, Kevin Groves
  • Publication number: 20080269236
    Abstract: The invention relates to 1,2,4 oxadiazole compounds and analogs thereof, represented by formula (II), and compositions and methods of use thereof.
    Type: Application
    Filed: June 6, 2008
    Publication date: October 30, 2008
    Applicant: ABBOTT LABORATORIES
    Inventors: Jianguo Ji, Chih-Lung Lee, Kevin B. Sippy, Tao Li, Murali Gopalakrishnan
  • Publication number: 20080255202
    Abstract: 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: Application
    Filed: March 26, 2005
    Publication date: October 16, 2008
    Applicant: Bayer HealthCare AG
    Inventors: 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
  • Publication number: 20080249093
    Abstract: 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: Application
    Filed: December 13, 2004
    Publication date: October 9, 2008
    Applicant: MERCK & CO., INC.
    Inventors: Vincent J. Colandrea, George A. Doherty, Jeffrey J. Hale, Pei Huo, Irene E. Legiec, Leslie Toth, Petr Vachal, Lin Yan
  • Publication number: 20080234273
    Abstract: 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: Application
    Filed: June 3, 2006
    Publication date: September 25, 2008
    Inventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
  • Publication number: 20080214620
    Abstract: 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: Application
    Filed: November 28, 2007
    Publication date: September 4, 2008
    Applicant: PROBIODRUG AG
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Mirko Buchholz, Andre J. Niestroj
  • Publication number: 20080167286
    Abstract: 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: Application
    Filed: December 10, 2007
    Publication date: July 10, 2008
    Applicant: Abbott Laboratories
    Inventors: Murali Gopalakrishnan, Marie P. Honore, Chih-Hung Lee, John Malysz, Jianguo Ji, Tao Li, Michael R. Schrimpf, Kevin B. Sippy, David J. Anderson
  • Patent number: 7390804
    Abstract: 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: Grant
    Filed: December 22, 2004
    Date of Patent: June 24, 2008
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Kazuyuki Ohmoto, Iori Itagaki
  • Patent number: 7390907
    Abstract: 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, d
    Type: Grant
    Filed: September 30, 2004
    Date of Patent: June 24, 2008
    Assignee: Amgen Inc.
    Inventors: Ning Chen, Thomas Nixey, Mark H. Norman
  • Patent number: 7365196
    Abstract: 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: Grant
    Filed: March 15, 2001
    Date of Patent: April 29, 2008
    Assignees: 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
  • Patent number: 7351724
    Abstract: 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: Grant
    Filed: October 14, 2005
    Date of Patent: April 1, 2008
    Assignee: The Scripps Research Institute
    Inventor: Dale L. Boger