Chalcogen Bonded Directly To Ring Carbon Of The Additional Six-membered Nitrogen Containing Hetero Ring Patents (Class 514/253.12)
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Publication number: 20140142083Abstract: The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: ApplicationFiled: April 13, 2012Publication date: May 22, 2014Applicant: EPIZYME, INC.Inventors: Kevin Wayne Kuntz, Richard Chesworth, Kenneth William Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah K. Knutson, Timothy James Nelson Wigle, Masashi Seki
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Publication number: 20140142084Abstract: Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer. As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.Type: ApplicationFiled: February 26, 2013Publication date: May 22, 2014Applicants: KOTOBUKI PHARMACEUTICAL CO., LTD., Astellas Pharma Inc.Inventors: Minoru Kameda, Ikumi Kuriwaki, Kazuhiko Iikubo, Hiroyuki Hisamichi, Yuichiro Kawamoto, Hiroyuki Moritomo, Tomoyuki Suzuki, Takashi Futami, Atsushi Suzuki, Kazuhisa Tsunoyama, Makoto Asaumi, Hiroshi Tomiyama, Atsushi Noda, Yoshinori Iwai, Kazuo Tokuzaki, Haruki Okada, Kozo Miyasaka
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Publication number: 20140135304Abstract: The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to Histamine H3 receptors.Type: ApplicationFiled: June 7, 2011Publication date: May 15, 2014Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Ramasastri Kambhampati, Amol Dinakar Deshpande, Adi Reddy Dwarampudi, Narasimhareddy Gangadasari, Sangram Keshari Saraf, Vishwottam Nagaraj Kandikere, Pradeep Jayarajan, Ishtiyaque Ahmad, Mohmadsadik Abdulhamid Mulla, Venkateswarlu Jasti
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Patent number: 8722663Abstract: The present invention provides a novel compound having an excellent antitumor effect. The compound of the present invention is represented by the following general formula (1) wherein R1 and R2 are aryl or the like; A is lower alkylene; Ring X is optionally substituted arylene; E is bond or lower alkenylene; Ring Y is optionally substituted heterocycloalkylene containing one or more nitrogen atoms, one of which is attached to the adjacent carbonyl group; G is —NH-G2-, —N(lower alkyl)-G2-, —NH—CH2-G2-, —N(lower alkyl)-CH2-G2- or —CH2-G2-, [wherein G2 binds to R2, G2-R2 is bond-R2, phenylene-G3-R2, phenylene-G4-O—R2, phenylene-G5-NH—R2, phenylene-G6-N(lower alkyl)-R2 or quinolinediyl-O—R2, the phenylene of said phenylene-containing groups being optionally substituted with one or more substituents; G3-R2 is —O-lower alkylene-R2 or the like; G4-O— is lower alkylene-O— or the like; G5 is lower alkylene; G6 is lower alkylene].Type: GrantFiled: January 28, 2011Date of Patent: May 13, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hideki Takasu, Shigekazu Fujita, Shinya Ohtsuka, Toshiyuki Hirose, Yosuke Sato, Satoshi Yamada, Keisuke Miyajima, Koji Sakai, Yutaka Kojima, Kazuo Sekiguchi, Yasuo Yanagihara, Takashi Suzuki, Hideo Tanaka, Kazuhisa Sugiyama, Mitsuhiro Okuno, Takumi Sumida
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Patent number: 8716283Abstract: The invention, in some aspects, relates to compounds and compositions useful for inhibiting Type III secretion systems in pathogenic bacteria, such as Yersinia Pestis. In some aspects, the invention relates to methods for discovering inhibitors of the Type III secretion system and uses of such inhibitors in the treatment and prevention of disease.Type: GrantFiled: April 1, 2009Date of Patent: May 6, 2014Assignees: University of Massachusetts, President and Fellows of Harvard CollegeInventors: Jon Goguen, Ning Pan, Kyungae Lee
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Publication number: 20140121213Abstract: In general, the present invention relates to uses of voltage-gated sodium channel blocker compounds, which include corresponding precursors, intermediates, monomers and dimers, corresponding pharmaceutical compositions, compound preparation and treatment methods for respiratory and respiratory tract diseases. In particular, the present invention also relates to methods and uses for treatment of respiratory or respiratory tract diseases, which comprises administering to a subject in need thereof an effective amount of a compound of the present invention.Type: ApplicationFiled: July 3, 2012Publication date: May 1, 2014Inventors: Jeffrey Charles Boehm, Roderick S. Davis, Jeffrey Kerns, Guoliang Lin, Robert D. Murdoch, Hong NIE
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Patent number: 8710060Abstract: To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; R1 represents a hydrogen atom or a C1-C3 alkyl group; R2 represents a hydrogen atom or a C1-C3 alkyl group; R3 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C3 alkoxy C1-C3 alkyl group, or a C1-C3 hydroxyalkyl group; R4 represents a hydrogen atom, a C1-C6 alkyl group, or a halogen atom; n represents an integer of 1 to 4; and X represents methylene, —O—, —NH—, —N(C1-C3 alkyl)-, —C(?O)—, —S—, —S(O)—, —S(O2)—, or a single bond.Type: GrantFiled: March 26, 2013Date of Patent: April 29, 2014Assignee: Daiichi Sankyo Company, LimitedInventors: Narihiro Toda, Rieko Takano, Takeshi Shida, Takahiro Katagiri, Mitsuhiro Iwamoto, Shinji Ashida, Mami Yamazaki
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Publication number: 20140107105Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.Type: ApplicationFiled: December 18, 2013Publication date: April 17, 2014Applicant: Janssen Pharmaceutica NVInventors: John M. Keith, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, John E. Mills, Chennagiri R. Pandit, Frank J. Villani, Hua Zhong
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Publication number: 20140073634Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.Type: ApplicationFiled: August 23, 2013Publication date: March 13, 2014Applicant: Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer CenterInventors: Philip Jones, Maria Emilia DiFrancesco, Alessia Petrocchi, Joe Marszalek, Gang Liu, Zhijun Kang, Chris Carroll, Timothy McAfoos, Barbara Czako
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Publication number: 20140038979Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: October 14, 2013Publication date: February 6, 2014Applicant: Janssen Pharmaceutica NVInventors: Kristof VAN EMELEN, Janine Arts, Leo-Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noelle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviene Van Heusden
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Publication number: 20140038963Abstract: The present disclosure provides methods for identifying therapeutic agents that are multifunctional radical quenchers. It also provides compounds of formula (I), (II), or (II-A): and pharmaceutically acceptable salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.Type: ApplicationFiled: April 4, 2012Publication date: February 6, 2014Inventors: Sidney Hecht, Omar Khdour, Sandipan Roy Chowdhury, Poulami Talukder
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Publication number: 20140011810Abstract: Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.Type: ApplicationFiled: September 11, 2013Publication date: January 9, 2014Applicant: Gatekeeper Pharmaceuticals, Inc.Inventors: Nathanael S. Gray, Wenjun Zhou
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Publication number: 20140011796Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.Type: ApplicationFiled: September 12, 2013Publication date: January 9, 2014Applicant: AMGEN INC.Inventors: Michael David BARTBERGER, Ana Gonzalez Buenrostro, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason Duquette, John Eksterwicz, Benjamin Fisher, Brian Matthew Fox, Jiasheng Fu, Zice Fu, Felix Gonzalez Lopez De Turiso, Michael William Gribble, Dann James Gustin, Julie Anne Heath, Xin Huang, Xianyun Jiao, Michael Johnson, Frank Kayser, David John Kopecky, Sujen Lai, Yihong Li, Zhihong Li, Jiwen Liu, Jonathan Dante Low, Brian Stuart Lucas, Zhihua Ma, Lawrence R. McGee, Joel McIntosh, Dustin McMinn, Julio Cesar Medina, Jeffrey Thomas Mihalic, Steven Howard Olson, Yosup Rew, Philip Marley Roveto, Daqing Sun, Xiaodong Wang, Yingcai Wang, Xuelei Yan, Ming Yu, Jiang Zhu
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Publication number: 20130289048Abstract: To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; R1 represents a hydrogen atom or a C1-C3 alkyl group; R2 represents a hydrogen atom or a C1-C3 alkyl group; R3 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C3 alkoxy C1-C3 alkyl group, or a C1-C3 hydroxyalkyl group; R4 represents a hydrogen atom, a C1-C6 alkyl group, or a halogen atom; n represents an integer of 1 to 4; and X represents methylene, —O—, —NH—, —N(C1-C3 alkyl)-, —C(?O)—, —S—, —S(O)—, —S(O2)—, or a single bond.Type: ApplicationFiled: March 26, 2013Publication date: October 31, 2013Inventors: Narihiro Toda, Rieko Takano, Takeshi Shida, Takahiro Katagiri, Mitsuhiro Iwamoto, Shinji Ashida, Mami Yamazaki
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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: 8536181Abstract: Disclosed herein are prolyl hydroxylase inhibitors that can stabilize hypoxia inducible factor-1 alpha (HIF-1?), as well as hypoxia inducible factor-2 (HIF-2). Also disclosed herein are pharmaceutical compositions comprising one or more of the disclosed compounds. Yet further disclosed are methods for stimulating the cellular immune response in a mammal such as increasing phagocytosis, for example, prolonging the life of phagocytes, inter alia, kerotyiocytes, neutrophils. As such the disclosed compounds provide methods for treating diseases that relate to the body's immune response.Type: GrantFiled: November 5, 2010Date of Patent: September 17, 2013Assignee: Aerpio Therapeutics Inc.Inventors: Joseph H. Gardner, Robert Shalwitz
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Patent number: 8507474Abstract: This invention is directed to compounds of the formula (I) and salts therefore that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds of this invention, pharmaceutical compositions and kits comprising the compounds of this invention, uses of the compounds of this invention to make medicaments, and treatments comprising the administration of the compounds of this invention to animals in need of the treatments.Type: GrantFiled: June 16, 2010Date of Patent: August 13, 2013Assignee: Intervet International B.V.Inventors: Christophe Pierre Alain Chassaing, Thorsten Meyer
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Publication number: 20130203768Abstract: This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of the N-heteroaryl compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.Type: ApplicationFiled: September 28, 2011Publication date: August 8, 2013Inventors: Michael Berger, Christopher Kern, Marko Eck, Jörg Schröder
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Publication number: 20130190325Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or solvate or physiologically hydrolysable, solubilising or immobilisable derivative thereof; wherein: any one or two of X.Type: ApplicationFiled: June 21, 2011Publication date: July 25, 2013Applicant: ITEK VENTURES PTY LTDInventors: Shudong Wang, Osama Chahrour, Tiangong Lu, Anran Hu
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Publication number: 20130184259Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention and intermediate compounds useful in these processes.Type: ApplicationFiled: November 16, 2012Publication date: July 18, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: VERTEX PHARMACEUTICALS INCORPORATED
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Publication number: 20130158045Abstract: Disclosed herein are prolyl hydroxylase inhibitors that can stabilize hypoxia inducible factor-1 alpha (HIF-1?), as well as hypoxia inducible factor-2 (HIF-2). Also disclosed herein are pharmaceutical compositions comprising one or more of the disclosed compounds. Yet further disclosed are methods for stimulating the cellular immune response in a mammal such as increasing phagocytosis, for example, prolonging the life of phagocytes, inter alia, kerotyiocytes, neutrophils. As such the disclosed compounds provide methods for treating diseases that relate to the body's immune response.Type: ApplicationFiled: February 15, 2013Publication date: June 20, 2013Applicant: Aerpio Therapeutics Inc.Inventor: Aerpio Therapeutics Inc.
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Publication number: 20130158010Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.Type: ApplicationFiled: February 19, 2013Publication date: June 20, 2013Applicant: Aerpio Therapeutics Inc.Inventors: Robert Shalwitz, Joseph H. Gardner
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Publication number: 20130137661Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.Type: ApplicationFiled: November 19, 2010Publication date: May 30, 2013Applicant: SK CHEMICALS CO. LTD.Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
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Publication number: 20130131052Abstract: Ophthalmically acceptable compositions used in arresting the development of cataracts or macular degeneration comprising a pharmaceutically acceptable carrier or diluent and a compound having the formula: where R1 and R2 are, independently, H or C1 to C3 alkyl; R3 and R4 are, independently C1 to C3 alkyl; and where R1 and R2, taken together, or R3 and R4, taken together, or both may be cycloalkyl; R5 is H, OH, or C1 to C6 alkyl; R6 is or C1 to C6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl; R7 is C1 to C6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl or where R6 and R7, or R5, R6 and R7, taken together, form a carbocycle or heterocycle having from 3 to 7 atoms in the ring.Type: ApplicationFiled: December 21, 2012Publication date: May 23, 2013Inventors: William L. Matier, Ghanshyam Patil
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Patent number: 8445495Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: June 11, 2009Date of Patent: May 21, 2013Assignee: Cytokinetics, Inc.Inventors: Bradley P. Morgan, David J. Morgans, Jr., Alex Muci, Pu-Ping Lu, Erica A. Kraynack, Todd Tochimoto
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Publication number: 20130123274Abstract: An antitumor agent for combined use of a compound or pharmaceutically acceptable salt thereof represented by Formula (I) and a compound or pharmaceutically acceptable salt thereof represented by Formula (II) exhibits an excellent antitumor effect compared to cases where these are individually used, and exhibits antitumor effects against various cancer types: wherein R1 is azetidinyl and the like, R2 to R5 is a hydrogen atom or a halogen atom, R6 is C3-8 cycloalkyl and the like, R7 is a hydrogen atom and the like, and R8 is a halogen atom and the like.Type: ApplicationFiled: June 23, 2011Publication date: May 16, 2013Applicant: Eisai R&D Management Co., Ltd.Inventors: Takayuki Nakagawa, Tomohiro Matsushima, Yasuhiro Funahashi
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Patent number: 8431563Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.Type: GrantFiled: August 23, 2011Date of Patent: April 30, 2013Assignee: Amgen Inc.Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, Jr., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
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Patent number: 8426407Abstract: A 1-(substituted aryl)-5-trifluoromethyl-2-(1H)pyridone compounds and pharmaceutical acceptable salts, preparation methods and uses for preparing the drugs for treating fibrosis thereof.Type: GrantFiled: May 24, 2010Date of Patent: April 23, 2013Assignee: Central South UniversityInventors: Gaoyun Hu, Lijian Tao, Jun Chen
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Patent number: 8415354Abstract: The present invention relates to inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.Type: GrantFiled: February 20, 2009Date of Patent: April 9, 2013Assignee: Abbott LaboratoriesInventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Steven Fung, Peer B. Jacobson, Lynne E. Rueter, Marina I. Strakhova, Jiahong Wang, James T. Link, Yixian Chen, Hwan-soo Jae, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Qi Shuai, Bryan K. Sorensen, Martin Winn, Dariusz Wodka, Hong Yong
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Patent number: 8410088Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: GrantFiled: April 13, 2012Date of Patent: April 2, 2013Assignees: Epizyme, Inc., Eisai R&D Management Co., Ltd.Inventors: Kevin W. Kuntz, Richard Chesworth, Kenneth W. Duncan, Masashi Seki, Syuji Shirotori
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Publication number: 20130072468Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.Type: ApplicationFiled: September 14, 2012Publication date: March 21, 2013Inventors: Eric J. Gilbert, William J. Greenlee, Michael W. Miller, Jack D. Scott, Andrew W. Stamford
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Patent number: 8399454Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: GrantFiled: April 22, 2010Date of Patent: March 19, 2013Assignee: Janssen Pharmaceutica, NVInventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Publication number: 20130065876Abstract: The present invention relates to compounds of formula I, wherein R1 to R5 are defined in the description and claims, and to pharmaceutically acceptable salts thereof. The present invention relates also to the manufacture of said compounds, pharmaceutical compositions containing them and methods for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: September 11, 2012Publication date: March 14, 2013Inventors: Uwe Grether, Paul Hebeisen, Peter Mohr, Fabienne Ricklin, Stephan Roever
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Patent number: 8377932Abstract: 1-(substituted benzyl)-5-trifluoromethyl-2(1H)pyridone compounds and their pharmaceutical acceptable salts are disclosed. The preparation methods of the compounds and their salts and the use of the same for preparing the medicaments for treating fibrosis are also disclosed. New pyridine compounds and their salts are obtained from trifluoromethyl pyridone as starting material.Type: GrantFiled: May 24, 2010Date of Patent: February 19, 2013Assignee: Central South UniversityInventors: Gaoyun Hu, Lijian Tao, Jun Chen
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Publication number: 20130040949Abstract: The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.Type: ApplicationFiled: December 29, 2010Publication date: February 14, 2013Applicant: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael S. Gray, Hwan G. Choi, Xianming Deng, Jianming Zhang
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Publication number: 20130030006Abstract: [Problem] Provided is an agent for preventing or treating diseases accompanied by urinary pain. [Means for Solution] A pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound or a salt thereof was confirmed to have not only an action of increasing effective bladder capacity but also an analgesic action against bladder pain and testis pain, based on FAAH inhibitory action. Accordingly, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound or a salt thereof can be used for preventing or treating interstitial cystitis/bladder pain syndrome and/or chronic nonbacterial prostatitis/chronic pelvic pain syndrome.Type: ApplicationFiled: April 27, 2011Publication date: January 31, 2013Inventors: Akiyoshi Someya, Hiroko Hayashida, Mai Koda, Masayuki Tanahashi, Katsuro Yoshioka
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Publication number: 20130012444Abstract: The present invention relates to crystalline solvates of 6-(Piperidin-4-yloxy)-2H-isoquinolin-1-one hydrochloride, processes for their preparation and the use thereof.Type: ApplicationFiled: June 27, 2012Publication date: January 10, 2013Applicant: SANOFIInventors: Norbert NAGEL, Bruno BAUMGARTNER, Harald BERCHTOLD, Oliver PLETTENBURG, Dieter KADEREIT, Mandy MOHNICKE, Simon GESSLER, Joachim TILLNER
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Publication number: 20130005710Abstract: The present invention provides a novel aminopyridine derivative that is excellent in pharmaceutical effects such as a neuroprotective effect, a neurogenesis or nerve regeneration promoting effect, and a cognitive function improving effect and, preferably, is low toxic and delivered at a high rate to the central nervous system.Type: ApplicationFiled: November 17, 2010Publication date: January 3, 2013Inventors: Tetsuya Tsukamoto, Takeshi Wakabayashi, Norihito Tokunaga, Yuhei Miyanohana
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Publication number: 20120302539Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.Type: ApplicationFiled: May 7, 2012Publication date: November 29, 2012Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas Macdonald, John Wityak
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Patent number: 8318769Abstract: Substituted sulfonamide compounds corresponding to formula I: processes for the preparation thereof, pharmaceutical compositions containing these compounds, and the use of such substituted sulfonamide compounds in pharmaceutical compositions for the treatment and/or inhibition of pain and other conditions at least partly mediated by the bradykinin 1 receptor.Type: GrantFiled: April 8, 2009Date of Patent: November 27, 2012Assignee: Gruenethal GmbHInventors: Stefan Oberboersch, Melanie Reich, Stefan Schunk, Michael Franz-Martin Engels, Ruth Jostock, Tieno Germann, Jean De Vry, Klaus Schiene, Sabine Hees
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Patent number: 8309537Abstract: Disclosed herein are compositions and methods for treating colitis and other inflammatory bowel diseases, inter alia, indeterminate colitis, Crohn's disease, irritable bowel syndrome and ischemic colitis.Type: GrantFiled: November 5, 2010Date of Patent: November 13, 2012Assignee: Aerpio Therapeutics Inc.Inventors: Joseph H. Gardner, Robert Shalwitz
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Publication number: 20120283242Abstract: The present invention provides a novel compound having an excellent antitumor effect. The compound of the present invention is represented by the following general formula (1) wherein R1 and R2 are aryl or the like; A is lower alkylene; Ring X is optionally substituted arylene; E is bond or lower alkenylene; Ring Y is optionally substituted heterocycloalkylene containing one or more nitrogen atoms, one of which is attached to the adjacent carbonyl group; G is —NH-G2-, —N(lower alkyl)-G2-, —NH—CH2-G2-, —N(lower alkyl)-CH2-G2- or —CH2-G2-, [wherein G2 binds to R2, G2-R2 is bond-R2, phenylene-G3-R2, phenylene-G4-O—R2, phenylene-G5-NH—R2, phenylene-G6-N(lower alkyl)-R2 or quinolinediyl-O—R2, the phenylene of said phenylene-containing groups being optionally substituted with one or more substituents; G3-R2 is —O-lower alkylene-R2 or the like; G4-O— is lower alkylene-O— or the like; G5 is lower alkylene; G6 is lower alkylene].Type: ApplicationFiled: January 28, 2011Publication date: November 8, 2012Inventors: Hideki Takasu, Shigekazu Fujita, Shinya Ohtsuka, Toshiyuki Hirose, Yosuke Sato, Satoshi Yamada, Keisuke Miyajima, Koji Sakai, Yutaka Kojima, Kazuo Sekiguchi, Yasuo Yanagihara, Takashi Suzuki, Hideo Tanaka, Kazuhisa Sugiyama, Mitsuhiro Okuno, Takumi Sumida
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Publication number: 20120263706Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.Type: ApplicationFiled: June 29, 2012Publication date: October 18, 2012Inventors: Jingrong Jean Cui, Lee Andrew Funk, Lei Jia, Pei-Pei Kung, Jerry Jialun Meng, Mitchell David Nambu, Mason Alan Pairish, Hong Shen, Michelle Tran-Dube
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Publication number: 20120258947Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: April 18, 2012Publication date: October 11, 2012Applicant: Grunenthal GmbHInventors: Sven KÜHNERT, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
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Publication number: 20120232088Abstract: This invention relates to piperazinedione compounds shown in the specification. These compounds are tyrosine kinase inhibitors and can be used to treat cancer.Type: ApplicationFiled: February 24, 2012Publication date: September 13, 2012Applicants: National Taiwan University, Taipei Medical UniversityInventors: Hui-Po Wang, Che-Ming Teng, Chun-Li Wang, Jih-hwa Guh, Shiow-Lin Pan, Yuan-Yi Wang, Jang-Feng Lian
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Publication number: 20120232049Abstract: A pyridine or pyrimidine derivative represented by the formula (I) has an excellent HGFR inhibitory activity and exhibits strong cell proliferation inhibitory effect and anti-tumor effect against cancer cell lines with amplified HGFR gene. wherein R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH?, nitrogen.Type: ApplicationFiled: February 22, 2008Publication date: September 13, 2012Applicant: Eisai R&D Management Co., Ltd.Inventors: Hiroshi Obaishi, Takayuki Nakagawa, Tomohiro Matsushima, Setsuo Funasaka, Shuji Shirotori, Keiko Takahashi
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Publication number: 20120225854Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: August 23, 2011Publication date: September 6, 2012Applicant: AMGEN INC.Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, JR., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
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Publication number: 20120196844Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.Type: ApplicationFiled: March 16, 2012Publication date: August 2, 2012Applicant: IRM LLCInventors: Phillip B. Alper, Mihai Azimioara, Christopher Cow, Robert Epple, Songchun Jiang, Gerald lelais, Pierre-Yves Michellys, Daniel Mutnick, Victor Nikulin, Lucas Westcott-Baker
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Publication number: 20120165324Abstract: Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.Type: ApplicationFiled: December 29, 2011Publication date: June 28, 2012Inventors: Francesco G. Salituro, Jeffrey Saunders
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Patent number: 8207171Abstract: Cosmetic compositions comprising 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging.Type: GrantFiled: June 21, 2011Date of Patent: June 26, 2012Assignee: Avon Products, Inc.Inventors: Dmitri S. Ptchelintsev, Hong Hu, Gopinathan K. Menon, Kristine Schmalenberg, John W. Lyga