Carbocyclic Ring Containing Patents (Class 546/194)
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Publication number: 20130303509Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.Type: ApplicationFiled: May 10, 2013Publication date: November 14, 2013Applicant: ABBVIE INC.Inventors: Todd M. Hansen, Kenton Longenecker, Howard R. Heyman, Michael L. Curtin, Richard F. Clark, Bryan Sorensen, Zhiqin Ji, Kevin Woller, George Doherty, Robin Frey
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Patent number: 8580965Abstract: Substituted sulfonamide compounds with bradykinin receptor (B1R) modulating activity; processes for the preparation thereof, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or inhibit pain and/or other disorders and/or disease states.Type: GrantFiled: October 16, 2007Date of Patent: November 12, 2013Assignee: Gruenenthal GmbHInventors: Stefan Oberboersch, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
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Patent number: 8569340Abstract: Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, E, T, n and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: GrantFiled: January 11, 2012Date of Patent: October 29, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Hong, Xiang Xu, Jiaxin Yu, Rajinder Singh, Ihab S. Darwish, Sambaiah Thota
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Patent number: 8569311Abstract: The present invention is directed to pyridyl piperidine compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.Type: GrantFiled: August 7, 2012Date of Patent: October 29, 2013Assignee: Merch Sharp & Dohme Corp.Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, John D. Schreier
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Publication number: 20130281690Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.Type: ApplicationFiled: June 12, 2013Publication date: October 24, 2013Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
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Publication number: 20130281428Abstract: Novel compounds or salts thereof, or crystals thereof, which inhibit Axl and are useful for treating diseases caused by Axl hyperfunction, diseases associated with Axl hyperfunction and/or diseases accompanied by Axl hyperfunction are provided. Pyridone derivatives represented by the formula (1) having various substituents or salts thereof, or crystals thereof (where R1, R2, R3, R5, R6, A, W, X and n in the formula (1) are as defined in the specification, respectively) are provided.Type: ApplicationFiled: January 30, 2013Publication date: October 24, 2013Inventors: Hitoshi Ohki, Masahiro Ota, Kosuke Takeuchi, Hideaki Watanabe, Akitake Yamaguchi, Yoshihiro Shibata, Yuichi Tominaga, Takeshi Jimbo, Keijiro Kobayashi, Katsuhiro Kobayashi, Daisuke Fukatsu
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Publication number: 20130281387Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.Type: ApplicationFiled: October 18, 2011Publication date: October 24, 2013Applicant: ELCELYX THERAPEUTICS, INC.Inventors: Alain D. Baron, Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley
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Publication number: 20130273034Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.Type: ApplicationFiled: September 2, 2011Publication date: October 17, 2013Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng, Po-Wai Yuen
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Publication number: 20130274288Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: June 11, 2013Publication date: October 17, 2013Applicant: THERAVANCE, INC.Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
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Publication number: 20130274468Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.Type: ApplicationFiled: June 12, 2013Publication date: October 17, 2013Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
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Publication number: 20130274469Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.Type: ApplicationFiled: June 12, 2013Publication date: October 17, 2013Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
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Publication number: 20130267700Abstract: The present application relates to novel 6-alkylamino-substituted dicyanopyridines, to their amino acid ester prodrugs, 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.Type: ApplicationFiled: March 13, 2013Publication date: October 10, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Alexandros VAKALOPOULOS, Daniel MEIBOM, Barbara ALBRECHT-KÜPPER, Katja ZIMMERMANN, Jörg KELDENICH, Hans-Georg LERCHEN, Peter NELL, Frank SÜßMEIER, Ursula KRENZ
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Publication number: 20130267702Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: March 13, 2013Publication date: October 10, 2013Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
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Publication number: 20130267701Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: March 13, 2013Publication date: October 10, 2013Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
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Publication number: 20130267492Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: March 28, 2013Publication date: October 10, 2013Applicant: ChemoCentryx, Inc.Inventors: Solomon Ungashe, John J. Wright, Andrew Pennell, Zheng Wei
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Publication number: 20130267516Abstract: Compounds of general formula I, (formula [I)], their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.Type: ApplicationFiled: November 21, 2011Publication date: October 10, 2013Applicant: LEO PHARMA A/SInventors: Kristoffer Månsson, Lars Kristian Albert Blæhr
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Patent number: 8552031Abstract: A compound represented by the formula (1): wherein A, B, R1, L1, R2, L2, L3, Y, L4, R3 and X are the same as defined in the description, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: GrantFiled: December 7, 2005Date of Patent: October 8, 2013Assignee: Nissan Chemical Industries, Ltd.Inventors: Katsuaki Miyaji, Yukihiro Shigeta, Satoshi Nakano, Shunuske Iwamoto, Yutaka Hirokawa, Hirofumi Ota, Kazufumi Yanagihara, Shingo Owada, Norihisa Ishiwata
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Patent number: 8551989Abstract: This invention relates to novel 4-(indazolyl)-1,4-dihydropyridine of the following formula (I) derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.Type: GrantFiled: May 29, 2009Date of Patent: October 8, 2013Assignee: Bayer Intellectual Property GmbHInventors: Martin Michels, Markus Follmann, Alexandros Vakalopoulos, Katja Zimmermann, Nicole Teusch, Karen Engel
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Patent number: 8551999Abstract: The present invention provides a heterocyclic compound represented by General Formula (1): wherein R1 is a group R5—Z1—, etc., Z1 is a lower alkylene group, etc., and R5 is a group represented by General Formula; wherein R13 is a hydrogen atom, etc., m is an integer from 1 to 5; R2 is a hydrogen atom: Y is CH or N: A1 is a heterocyclic ring selected from the group consisting of indolediyl groups, wherein the heterocyclic ring may have at least one substituent: T is a group —CO—, etc.: R3 is a hydrogen atom, etc.: R4 is a lower alkyl group optionally substituted by one or more hydroxy groups, etc.: R3 and R4, together with the nitrogen atom to which they bind, may bind to each other and form a 5- to 10-membered saturated heterocyclic ring, wherein the heterocyclic ring may have at least one substituent. The heterocyclic compound of the present invention has excellent effects of suppressing the production of collagen and/or treating tumors.Type: GrantFiled: October 29, 2008Date of Patent: October 8, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Takumi Sumida, Fujio Tabusa, Kazuo Sekiguchi, Takeshi Kodama, Koichi Yasumura, Yutaka Kojima, Masaaki Motoyama, Keisuke Miyajima, Kenji Yoshida, Keizo Kan, Makoto Sakamoto, Hideki Takasu, Takashi Nakagawa, Naoto Ohi, Yasuo Harada, Norikazu Hashimoto, Hironori Matsuyama, Masatoshi Iida, Shigekazu Fujita, Tae Fukushima
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Patent number: 8552205Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: November 20, 2008Date of Patent: October 8, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Antonio Jose del Moral Barbosa, Jr., Joerg Martin Bentzien, Steven Richard Brunette, Zhidong Chen, Derek Cogan, Donghong A. Gao, Alexander Heim-Riether, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Rene Marc Lemieux, Weimin Liu, Bryan McKibben, Craig Andrew Miller, Neil Moss, Matt Aaron Tschantz, Zhaoming Xiong, Hui Yu, Yang Yu
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Publication number: 20130261129Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.Type: ApplicationFiled: March 29, 2013Publication date: October 3, 2013Applicant: AbbVie Inc.Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Wei, Lijuan Jane Wang
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Publication number: 20130261100Abstract: The invention relates pyridine amide derivative of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently hydrogen, linear o branched (C1-C3)alkyl or joined together they form a cyclopropyl ring; R is independently selected from the group consisting of halogens and trifluoromethyl and p is 1, 2 or 3; A is C or N; E is a group of formula (B) or (C), wherein B is C(O)OH, C(O)O(C1-C3)alkyl, and C is selected from the group consisting of formula (I) m is 1,2 or 3, n is 0 or 1, W is —O—, —O(C1-C3 alkyl)-; —(C1-C3 alkyl)O—; —C(O)—; —C(?N—O(C1-C3 alkyl))-; —NH— or —NH(C1-C3alkyl)-; Ar is phenyl, optionally substituted with one or more substituents selected from the group consisting of halogen, trifluoromethyl, trifluoromethoxy, methyl, —NH(C1-C3alkyl)-; —N(C1-C3alkyl)(C1-C3alkyl)-, a from 5 to 7 membered heterocyclic ring containing one nitrogen atom which is covalently bonded to Ar and optionally containing one or two heteroatoms selected from N, O and S; and a 5- or 6-memberType: ApplicationFiled: December 10, 2010Publication date: October 3, 2013Inventors: Manuela Borriello, Lucio Rovati, Luigi Piero Stasi, Benedetta Buzzi, Fabrizio Colace
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Publication number: 20130261153Abstract: The present invention relates to CCR3 inhibitors of formula 1, wherein R1 is H, C1-6-alkyl, C0-4-alkyl-C3-6-cycloalkyl, C1-6-haloalkyl; R2 is H, C1-6-alkyl; X is an anion selected from the group consisting of chloride or ½ dibenzoyltartrate j is 1 or 2. for use as a medicament for the treatment of diseases selected from dry age-related macular degeneration (dAMD), wet age-related macular degeneration (wAMD), retinopathy of prematurity (ROP), central retinal vein occlusion (CRVO), nasal polyposis, eosinophilic esophagitis, eosinophillic gastroenteritis (e.g. eosinophilic gastritis and eosinophilic ententeritis), hypereosinophilic syndrome and Churg Strauss syndrome.Type: ApplicationFiled: March 27, 2013Publication date: October 3, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Michael Chadham NIVENS, Thierry BOUYSSOU, Peter SEITHER, Rolf GOEGGEL
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Publication number: 20130261307Abstract: The present invention relates to a process for preparing CCR3 inhibitors of formula 1, wherein R1 is H, C1-6-alkyl, C0-4-alkyl-C3-6-cycloalkyl, C1-6-haloalkyl; R2 is H, C1-6-alkyl; X is an anion selected from the group consisting of chloride or ½ dibenzoyltartrate j is 1 or 2.Type: ApplicationFiled: March 27, 2013Publication date: October 3, 2013Applicant: Boehringer Ingelehim International GmbHInventors: Adil DURAN, Rolf SCHMID
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Patent number: 8546429Abstract: The present invention relates to certain trisubstituted aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.Type: GrantFiled: October 13, 2010Date of Patent: October 1, 2013Assignee: Arena Pharmaceuticals, Inc.Inventors: Robert M. Jones, Graeme Semple, Yifeng Xiong, Young-Jun Shin, Albert S. Ren, Imelda Calderon, Beatriz Fioravanti, Jin Sun Karoline Choi, Juerg Lehmann, Marc Bruce
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Publication number: 20130252957Abstract: The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p, R1, R2, R3, R4, R5 and R6 are defined in the specification. The invention further provides pharmaceutical compositions including the compounds of the invention as well as methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various conditions and disorders, such as Crohn's disease and ulcerative colitis.Type: ApplicationFiled: December 28, 2012Publication date: September 26, 2013Applicant: ELAN PHARMACEUTICALS, INC.Inventors: Ying-Zi Xu, Shendong Yuan, David Wone, Andrei Konradi
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Patent number: 8541402Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: GrantFiled: May 3, 2012Date of Patent: September 24, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Joly, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
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Publication number: 20130245016Abstract: Herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: ApplicationFiled: November 30, 2011Publication date: September 19, 2013Inventors: Steven David Knight, William Henry Miller, Kenneth Allen Newlander, Sharad Kumar Verma
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Publication number: 20130245010Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTC”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: April 26, 2013Publication date: September 19, 2013Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
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Publication number: 20130245011Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTC”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: May 6, 2013Publication date: September 19, 2013Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
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Publication number: 20130245000Abstract: The present invention relates to compounds of Formula (I) that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of GPR119 receptor activity. The invention also relates to the process for preparation of the compounds, pharmaceutical compositions thereof. The invention further relates to methods of treating, preventing and/or managing diseases, disorders syndromes or conditions associated with the modulation of GPR119 receptor by using either alone or in combinations of Formula (I).Type: ApplicationFiled: November 24, 2011Publication date: September 19, 2013Applicant: LUPIN LIMITEDInventors: Rajesh Thotapally, Onkar Gangaram Kachi, Atish Harishchandra Rodge, Ashok Bhau Pathak, Bhavana Shrirang Kardile, Milind Dattatraya Sindkhedkar, Venkata P. Palle, Rajender Kumar Kamboj
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Patent number: 8536092Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.Type: GrantFiled: December 14, 2011Date of Patent: September 17, 2013Assignee: Bayer Cropscience AGInventors: Bernd Alig, Rüdiger Fischer, Christian Funke, Rudolf F. Ernst Gesing, Achim Hense, Olga Malsam, Mark Wilhelm Drewes, Ulrich Görgens, Tetsuya Murata, Katsuaki Wada, Christian Arnold, Erich Sanwald
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Patent number: 8536198Abstract: The present application describes modulators of MIP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed.Type: GrantFiled: July 23, 2008Date of Patent: September 17, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Joseph B. Santella, John Hynes, Daniel S. Gardner
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Publication number: 20130237515Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, L1, L2, U and B are as defined in the application, which have valuable pharmacological properties, and in particular modulate the activity of the MCH receptor.Type: ApplicationFiled: February 28, 2013Publication date: September 12, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Thorsten OOST, Ralf LOTZ, Dirk STENKAMP
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Publication number: 20130237518Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).Type: ApplicationFiled: October 24, 2011Publication date: September 12, 2013Inventors: Sobhana Babu Boga, Joseph M. Kelly, Hugh Y. Zhu, Abdul-Basit Alhassan, Xin Yao, Xiaolei Gao, James J-S Wang, Jagdish A. Desai, Subrahmanyam Gudipati, Sie-Mun Lo, Liang Zhu, Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, JR.
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Patent number: 8530663Abstract: The invention relates to compounds of formula I: where X, HAr, a, and R1 through R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: March 21, 2011Date of Patent: September 10, 2013Assignee: Theravance, Inc.Inventors: Eric L. Stangeland, Lori Jean Patterson, Sheila Zipfel
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Publication number: 20130231369Abstract: Provided are N-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives represented by formula I, stereoisomers, pharmaceutically acceptable salts or solvates thereof. The above compounds have the dual activities of 5-hydroxytryptamine 1A receptor ligand and selective serotonin reuptake inhibitor. The preparation methods of the above compounds, the uses of these compounds for the prevention or treatment of nervous system diseases related to 5-hydroxytryptamine system dysfunction and the pharmaceutical compositions containing these compounds are also provided.Type: ApplicationFiled: April 8, 2011Publication date: September 5, 2013Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. ChinaInventors: Yunfeng Li, Rifang Yang, Youzhi Zhang, Yongzhen Li, Zengliang Jin, Peng Li, Li Yuan, Liuhong Yun, Nan Zhao, Cheng Zhang, Xiaodan Xu, Rusheng Zhao, Hongxia Chen, Rui Xue, Juanjuan Qin, Zhenzhen Wang, Jiazhi Yao
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Publication number: 20130231339Abstract: The present invention relates to novel benzofuran-2-sulfonamide pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: March 1, 2013Publication date: September 5, 2013Applicant: ALLERGAN, INC.Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
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Publication number: 20130231329Abstract: The present patent application concerns new ligands of the H4-receptor of formula (I), their process of preparation and their therapeutic use.Type: ApplicationFiled: September 27, 2011Publication date: September 5, 2013Applicant: BIOPROJETInventors: Isabelle Berrebi-Bertrand, Xavier Billot, Thierry Calmels, Marc Capet, Denis Danvy, Stéphane Krief, Olivier Labeeuw, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Philippe Robert, Jean-Charles Schwartz
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Patent number: 8524709Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.Type: GrantFiled: January 12, 2012Date of Patent: September 3, 2013Assignee: Tyrogenex, Inc.Inventors: Congxin Liang, Ming Qi, Shu Gao, Zhigang Li
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Publication number: 20130224195Abstract: New substituted benzazole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: April 3, 2013Publication date: August 29, 2013Inventors: Abran Costales, Teresa Hansen, Barry H. Levine, Christopher McBride, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Cynthia M. Shafer, Sharadha Subramanian, Joelle Verhagen
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Publication number: 20130225548Abstract: A main object of the present invention is to provide a novel pyridine derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof. In formula [1], R represents an aryl group or a heteroaryl group, which may be substituted by an optionally substituted alkyl group, a hydroxy group, a halogen atom or a group represented by general formula [2]. In formula [2], -L1-L2-L3-RA ??[2] L1 and L3 independently represent a single bond, an alkylene group or a cycloalkylene group; L2 represents a single bond, O, or NRB; RB represents H or an optionally substituted alkyl group; and RA represents B, an amino group, a cyano group, a hydroxy group, an alkoxy group, an aryl group, a monoalkylamino group, a dialkylamino group, a carbamoyl group, an alkyloxycarbonyl group, a monoalkylaminocarbonyl group, a dialkylaminocarbonyl group, an alkylcarbonylamino group, and a saturated heterocyclic group, among other groups.Type: ApplicationFiled: October 27, 2011Publication date: August 29, 2013Applicant: NIPPON SHINYAKU CO., LTD.Inventors: Hidetaka Fujihara, Hiroyuki Sugiyama, Takashi Tsuji, Takara Ino, Yoshinari Haruta
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Patent number: 8518971Abstract: A compound of formula (I): wherein A, p, R1, R3, R4, R5, R6, m, R7, n and R8 are as defined in claim 1. Furthermore, the present invention relates to intermediates used to prepare compounds of formula (I), to methods of using them to combat and control insect, acarine, nematode and mollusc pests and to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them.Type: GrantFiled: July 6, 2009Date of Patent: August 27, 2013Assignee: Syngenta Crop Protection, Inc.Inventors: Thomas Pitterna, Jerome Yves Cassayer, Camilla Corsi, Peter Maienfisch
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Patent number: 8518972Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: GrantFiled: February 10, 2011Date of Patent: August 27, 2013Assignee: Celgene CorporationInventors: Hon-Wah Man, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Roger Shen-Chu Chen, Weihong Zhang
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Patent number: 8519136Abstract: The present invention relates to a compound of formula I: wherein: R1 is a hydrogen atom, F, CN, etc.; R2 is CO, SO2, etc.; R3 is a phenyl which may be substituted; X1, X2, and X3 each independently CH, N, etc. provided, however, that among X1, X2 and X3, the number of nitrogen is 0 or 1; W is the following residue: wherein: W1, W2, and W3 each independently CH, N, etc., or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: February 18, 2009Date of Patent: August 27, 2013Assignee: MSD K.K.Inventors: Tetsuya Kato, Nobuhiko Kawanishi, Takashi Mita, Katsumasa Nonoshita, Mitsuru Ohkubo
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Patent number: 8518916Abstract: This invention relates to novel heterocyclic compounds having selective affinity for the mGlu5 subtype of metabotropic receptors, pharmaceutical compositions thereof and uses for such compounds and compositions in the treatment of lower urinary tract disorders, such as neuromuscular dysfunction of the lower urinary tract, and in the treatment of migraine and gastroesophagael reflux disease (GERD).Type: GrantFiled: August 4, 2008Date of Patent: August 27, 2013Assignee: Recordati Ireland LimitedInventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Elena Poggesi, Davide Graziani, Matteo Longhi
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Patent number: 8518948Abstract: Compounds of general Formula (I): wherein R1, R2, R3, Ra, A, B and x are as defined herein are inhibitors of protein kinases in particular members of the cyclin-dependent kinase family and/or the glycogen synthase kinase 3 family and are useful in preventing and/or treating any type of pain, inflammatory disorders, cancer, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases, metabolic disorders, renal diseases, neurologic and neuropsychiatric diseases and neurodegenerative diseases.Type: GrantFiled: March 10, 2011Date of Patent: August 27, 2013Assignee: Ingenium Pharmaceuticals GmbHInventors: Lutz Zeitlmann, Andre Niestroj, Ulrich Heiser
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Patent number: 8518938Abstract: The present invention relates to compounds of formula I useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative disorders.Type: GrantFiled: April 20, 2011Date of Patent: August 27, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: David J. Lauffer, Pan Li, Kira McGinty, Steven M. Ronkin, Qing Tang, Anne-Laure Grillot, Nathan D. Waal
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Publication number: 20130217686Abstract: A novel methylcyclohexane derivative, and a pharmaceutical composition including the same that is effective for the prevention or treatment of pain.Type: ApplicationFiled: September 28, 2011Publication date: August 22, 2013Applicant: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Sung Jin Bae, Han Ju Yi, Sun Gwan Hwang, Mo Ses Jeong, Yeo Jin Yoon, Sang Mi Chae, Joo Young Park, Eun Ju Ryu
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Publication number: 20130217715Abstract: Substituted pyrazolophenyl-benzenesulfonamide compounds of formula (I) are described, wherein m, R1, R2, R3, and R4 are defined in the description, which modulate the activity of protein kinases, These compounds find utility in treating diseases caused by deregulated protein kinase activity, such as cancer and cell proliferative disorders.Type: ApplicationFiled: August 2, 2011Publication date: August 22, 2013Inventors: Maurizio Pulici, Chiara Marchionni, Gabriella Traquandi, Alessandra Scolaro, Daniele Donati