Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 546/118)
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Publication number: 20110086817Abstract: Embodiments herein provide compounds and methods of making and using such compounds for prevention and treatment of multidrug resistant bacteria. In particular, embodiments are directed to anti-bacterial agents from benzo[d]heterocyclic scaffolds for prevention and treatment of multidrug resistant bacteria.Type: ApplicationFiled: May 29, 2009Publication date: April 14, 2011Applicant: University of Notre Dame du LacInventors: Marvin J. Miller, Garrett C. Moraski
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Patent number: 7923560Abstract: The present invention provides immune response modifiers (IRMs) associated with (typically, attached to, and preferably, covalently attached to) macromolecular support materials. The IRM compounds in such IRM-support complexes retain biological activity. Such attachment of an IRM to a macromolecular support material provides for the localized biological activity of the IRM.Type: GrantFiled: April 9, 2004Date of Patent: April 12, 2011Assignee: 3M Innovative Properties CompanyInventors: Paul D. Wightman, Isidro Angelo E. Zarraga, Naiyong Jing, Jie J. Liu
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Publication number: 20110082138Abstract: A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: November 24, 2010Publication date: April 7, 2011Applicant: Daiichi Sankyo Company, LimitedInventors: Masami Ohtsuka, Noriyasu Haginoya, Masanori Ichikawa, Hironori Matsunaga, Hironao Saito, Yoshihiro Shibata, Tomoyuki Tsunemi
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Publication number: 20110077154Abstract: The present invention relates to pyridin-4-ylmethyl sulfonamides of formula I wherein Het, Ra, Rc, Rf, m, n, p, R, A and Y are as defined in the claims, to the N-oxides, and salts thereof and their use for combating harmful fungi, and also to compositions and seed comprising at least one such compound. The invention also relates to a process and intermediates for preparing these compounds.Type: ApplicationFiled: May 20, 2009Publication date: March 31, 2011Applicant: BASF SEInventors: Alice Glaettli, Wassilios Grammenos, Bernd Mueller, Jan Klaas Lohmann, Marianna Vrettou
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Patent number: 7915281Abstract: Imidazo ring compounds, (e.g. imidazo[4,5-c]pyridine, imidazo[4,5-c]quinoline, 6,7,8,9-tetrahydro imidazo[4,5-c]quinoline, and imidazo[4,5-c]naphthyridine compounds) having an isoxazole, dihydroisoxazole, or oxadiazole substituent at the 1-position, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: GrantFiled: June 17, 2005Date of Patent: March 29, 2011Assignee: 3M Innovative Properties CompanyInventors: William H. Moser, Joan T. Moseman, Tushar A. Kshirsagar, Philip D. Heppner
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Publication number: 20110070595Abstract: The present invention relates to immobilization compounds and methods useful for the identification of PARP interacting compounds or for the purification or identification of PARP proteins.Type: ApplicationFiled: May 14, 2009Publication date: March 24, 2011Inventors: Gerard Drewes, Valerie Reader
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Publication number: 20110070297Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: ApplicationFiled: December 1, 2010Publication date: March 24, 2011Applicants: Takeda San Diego, Inc., Takeda Pharmaceutical Company LimitedInventors: Sheldon X. Cao, Jun Feng, Yasuhiro Imaeda, Stephen L. Gwaltney, David J. Hosfield, Nobuyuki Takakura, Mingnam Tang
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Publication number: 20110064693Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.Type: ApplicationFiled: August 26, 2008Publication date: March 17, 2011Inventors: Dongcheng Dai, Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Ryan A. Larson
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Patent number: 7906553Abstract: Described herein are compounds of Formula (I) having the structure: where A, J, R1, R4, Z and X are described herein; and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: GrantFiled: August 26, 2009Date of Patent: March 15, 2011Assignee: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20110059954Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2 and R3 are defined as stated hereinafter, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, their use and processes for preparing them.Type: ApplicationFiled: October 16, 2008Publication date: March 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Schaenzle, Dirk Stenkamp
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Publication number: 20110060002Abstract: The invention relates to conglomerates of tenatoprazole potassium salts of the following general formula (I), that consist of an equimolar mixture of enantiomers having R and S configurations and capable of crystallisation in the form of a conglomerate, wherein said salts are selected from tenatoprazole dehydrated potassium salt, tenatoprazole potassium dimethanolate, tenatoprazole potassium diethanolate and tenatoprazole potassium ethylene-glycolate. The invention also relates to a pharmaceutical composition containing such salt, and to the use of said salt.Type: ApplicationFiled: December 3, 2007Publication date: March 10, 2011Applicant: SIDEM PHARAMA SAInventors: Avraham Cohen, Francois Schutze, Suzy Charbit, Stéphane Bernad, Cuillaume Tauvel, Marie-Noëlle Petit, Gérard Coquerel
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Publication number: 20110060004Abstract: Compounds of formula (I): in free or salt or solvate form, where X, R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: April 27, 2009Publication date: March 10, 2011Applicant: NOVARTIS AGInventors: Catherine Leblanc, Ritchie Cathy, Duncan Shaw, Nikolaus Johannes Stiefl
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Publication number: 20110059941Abstract: Compounds of Formula (I), wherein R1-R10, A and X1 to X3 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: ApplicationFiled: May 19, 2006Publication date: March 10, 2011Inventors: Peter William Rodney Caulkett, Darren McKerrecher, Nicholas John Newcombe, Kurt Gordon Pike, Michael James Waring
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Publication number: 20110053946Abstract: The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain aryl-quinolyl compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.Type: ApplicationFiled: April 27, 2009Publication date: March 3, 2011Applicants: CANCER RESEARCH TECHNOLOGY LIMITED, INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)Inventors: Ion Niculescu-Duvaz, Alfonso Zambon, Dan Niculescu-Duvaz, Steven Whittaker, Richard Marais, Caroline Joy Springer
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Patent number: 7897616Abstract: The present invention relates to imidazopyridin-2-one derivatives of the formula I with the definitions specified in the description, to their pharmaceutically usable salts and to their use as medicaments.Type: GrantFiled: September 22, 2008Date of Patent: March 1, 2011Assignee: Sanofi-AventisInventors: Gerhard Zoller, Stefan Petry, Markus Follmann, Gunter Muller, Norbert Tennagels
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Publication number: 20110039884Abstract: The invention relates to imidazopyridinones, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. By activating TLRs, it should be possible to induce or stimulate immune cells to mount an immune response. In particular, the TLR7 has been implicated in viral infections (such as HCV or HBV), cancers and tumours, and T2 Helper cell (TH2) mediated diseases, and hence TLR7 agonists are potentially useful in the treatment of such diseases. We have now found a series of imidazopyridinones which are agonists of TLR7. According, there is provided a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is 3- to 8-membered saturated heterocyclic group wherein one ring member is —O—; and R2 is phenyl or pyridinyl, each optionally substituted by C1-C6alkyl.Type: ApplicationFiled: October 28, 2010Publication date: February 17, 2011Applicant: Pfizer LimitedInventors: Peter H. Jones, David Cameron Pryde, Thien Duc Tran
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Publication number: 20110039822Abstract: The present invention provides a compound having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases, inflammatory diseases, and allergic diseases. As a result of studies on a novel condensed heterocyclic derivative, the inventors have found that a compound having a cross-linked structure has an excellent JAK3 inhibition activity, and have completed the present invention. In other words, it is verified that the compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g.Type: ApplicationFiled: October 28, 2010Publication date: February 17, 2011Applicant: Astellas Pharma Inc.Inventors: Takayuki INOUE, Akira Tanaka, Kazuo Nakai, Hiroshi Sasaki, Fumie Takahashi, Shohei Shirakami, Keiko Hatanaka, Yutaka Nakajima, Koichiro Mukoyoshi, Hisao Hamaguchi, Shigeki Kunikawa, Yasuyuki Higashi
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Publication number: 20110034497Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: ApplicationFiled: August 9, 2010Publication date: February 10, 2011Applicant: EPITHERIX, LLCInventors: John Hood, David Mark Wallace, Sunil Kumar KC
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Publication number: 20110034458Abstract: The present invention is related to pyridine methylene azolidinone derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: ApplicationFiled: October 18, 2010Publication date: February 10, 2011Applicant: APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.Inventors: Thomas RUECKLE, Anna Quattropani, Vincent Pomel, Jerome Dorbais, David Covini, Alexander Bischoff
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Patent number: 7884104Abstract: The present invention is directed to novel substituted aminopiperidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: September 27, 2005Date of Patent: February 8, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Jason M. Cox, Scott D. Edmondson, Bart Harper, Ann E. Weber
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Patent number: 7884109Abstract: The present invention provides novel purine and imidazopyridine derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: October 11, 2007Date of Patent: February 8, 2011Assignee: Wyeth LLCInventors: Michael J. Ohlmeyer, Adolph C. Bohnstedt, Celia Kingsbury, Koc-Kan Ho, Jorge Gabriel Quintero, Ming You, Haengsoon Park, Yingchun Lu
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Publication number: 20110027227Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family is disclosed.Type: ApplicationFiled: January 14, 2009Publication date: February 3, 2011Inventors: Dongcheng Dai, Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Travis K. Warren
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Patent number: 7879844Abstract: The present invention provides a compound of formula (I) having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases inflammatory diseases, and allergic diseases. The compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g., rejection during organ/tissue transplantation, autoimmune diseases, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, Alzheimer's disease, and atherosclerotic disease), or diseases caused by abnormal cytokine signal transmission (e.g., cancer and leukemia).Type: GrantFiled: December 25, 2006Date of Patent: February 1, 2011Assignee: Astellas Pharma Inc.Inventors: Takayuki Inoue, Akira Tanaka, Kazuo Nakai, Hiroshi Sasaki, Fumie Takahashi, Shohei Shirakami, Keiko Hatanaka, Yutaka Nakajima, Koichiro Mukoyoshi, Hisao Hamaguchi, Shigeki Kunikawa, Yasuyuki Higashi
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Patent number: 7879880Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt thereof, wherein M1 is M2 is N; X is a bond, optionally substituted alkylene, alkenylene, —O—, —CH2N(R12)—, —N(R12)CH2—, —N(R12)—, —NHC(O)—, —OCH2—, —CH2O—, or —S(O)0-2—; and Y is —(CH2)1-2—, —C(?O)—, —C(?NOR13)— or —SO0-2—; or M1 is N; M2 is N or CH; X is a bond, alkylene, alkenylene, —C(O)—, —NHC(O)—, —OC(O)— or —S(O)1-2—; Y is —(CH2)1-2—, —C(?O)— or —SO0-2—; and when M2 is CH, Y is also Y is —O— or —C(?NOR13)—; Z is a bond or optionally substituted alkylene or alkenylene; U and W are CH, or one is CH and one is N; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; and compositions and methods of treating obesity, metabolic syndrome and a cognition deficit disorder, alone or in combinatType: GrantFiled: December 19, 2006Date of Patent: February 1, 2011Assignee: Schering CorporationInventors: Daniel M. Solomon, Robert G. Aslanian, Michael Y. Berlin, Manuel de Lera Ruiz, Kevin D. McCormick, Mwangi W. Mutahi, Wing C. Tom
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Publication number: 20110020388Abstract: This invention relates to compositions, and related methods, of synthetic nanocarriers that target sites of action in cells, such as antigen presenting cells (APCs), and comprise immunomodulatory agents that dissociate from the synthetic nanocarriers in a pH sensitive manner. Also disclosed are compositions and methods relating to synthetic nanocarriers that encapsulate labile immunomodulatory agents that dissociate from the synthetic nanocarriers in a pH sensitive manner.Type: ApplicationFiled: May 26, 2010Publication date: January 27, 2011Applicant: Selecta Biosciences, Inc.Inventors: CHARLES ZEPP, Yun Gao, Mark J. Keegan, Sam Baldwin, Fen-ni Fu, Lloyd Johnston, Grayson B. Lipford
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Publication number: 20110009400Abstract: The disclosure relates to compounds of formula (I): wherein X1, X2, X3, X4, Y, n, A, and W are as defined in the disclosure, or a salt thereof, or a hydrate or solvate thereof, and to processes for the preparation of these compounds and the therapeutic use thereof.Type: ApplicationFiled: July 21, 2010Publication date: January 13, 2011Applicant: SANOFI-AVENTISInventors: Laurent Dubois, Yannick Evanno, Catherine Gille, André Malanda
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Publication number: 20110009444Abstract: This disclosure relates to compounds of formula (I): wherein X1, X2, X3, X4, n, Y, W, and A are as defined in the disclosure, or a salt thereof, or a hydrate or solvate thereof, and to processes for the preparation of these compounds and the therapeutic use thereof.Type: ApplicationFiled: July 21, 2010Publication date: January 13, 2011Applicant: SANOFI-AVENTISInventors: Laurent DUBOIS, Yannick EVANNO, André MALANDA, Odile LECLERC
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Patent number: 7868002Abstract: As discussed above, there remains a need for the development of novel therapeutic agents useful for treating inflammatory or autoimmune and proliferative diseases. The present invention provides novel compounds of general formula (I), and pharmaceutical compositions thereof, as described generally and in classes and subclasses herein, as well as methods of making and using such compounds.Type: GrantFiled: September 28, 2007Date of Patent: January 11, 2011Assignee: Eisai R&D Management Co., Ltd.Inventors: Jane Daun, Heather A. Davis, Bruce DeCosta, Fabian Gusovsky, Ieharu Hishinuma, Yimin Jiang, Toshihiko Kaneko, Kouichi Kikuchi, Seiichi Kobayashi, André Lescarbeau, Xiang-Yi Li, Kenzo Muramoto, Norihito Ohi, Marc Pesant, Boris M. Seletsky, Motohiro Soejima, Mark Spyvee, Lynda Tremblay, Ye Yao, Hiromitsu Yokohama, Yan (Janet) Zhao, Wanjun Zheng
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Publication number: 20110003809Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: February 27, 2009Publication date: January 6, 2011Inventor: Kateri A. Ahrendt
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Publication number: 20110003827Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: ApplicationFiled: December 10, 2004Publication date: January 6, 2011Inventors: Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
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Publication number: 20110003798Abstract: The invention provides a novel class of 2,7-naphthyridin derivatives; pharmaceutical compositions comprising such compounds and methods of using such compounds to treat o prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT*, c-Kit, RET, TrkA, TrkB, TrkC-GR-1R, Alk, c-FMS or combinations thereof.Type: ApplicationFiled: January 27, 2009Publication date: January 6, 2011Applicant: IRM LLCInventors: Barun Okram, Tetsuo Uno, Qiang Ding, Yahua Liu, Yunho Jin, Qihui Jin, Xu Wu, Jianwei Che, S. Frank Yan, Xueshi Hao
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Publication number: 20100331323Abstract: The present invention provides active compounds for modulating nicotinic acetylcholine receptors and methods of making the same. The methods of preparing the active compounds utilize different intermediate compounds.Type: ApplicationFiled: September 10, 2010Publication date: December 30, 2010Inventors: Daniel L. Comins, Florence F. Wagner, Pauline Ondachi
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Publication number: 20100331302Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease 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: July 8, 2010Publication date: December 30, 2010Applicant: Chemocentryx, Inc.Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
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Publication number: 20100324028Abstract: The present invention relates to new CGRP-antagonists of general formulae Ia and Ib wherein R1, R2, R3, R4 and R5 are defined as mentioned below, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.Type: ApplicationFiled: November 21, 2008Publication date: December 23, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Georg Schaenzle, Dirk Stenkamp
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Publication number: 20100324040Abstract: The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.Type: ApplicationFiled: May 2, 2008Publication date: December 23, 2010Applicant: ASTRAZENECA ABInventors: Audrey Davies, Stephanos Ioannidis, Michelle Lamb, Mei Su, Tao Wang, Hai-Jun Zhang
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Publication number: 20100317689Abstract: The compounds of formulas (I), (II), (III) and (IV), where the symbols are as defined in the specification are prodrugs of proton pump inhibitors. The R4 group includes at least one acidic group or its pharmaceutically acceptable salt, and the compound having the R4 group have improved aqueous solubility, stability in plasma and improved bioavailability.Type: ApplicationFiled: September 15, 2007Publication date: December 16, 2010Inventors: Michael E. Garst, George Sachs, Jai Moo Shin
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Publication number: 20100317660Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist of formula (I) in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.Type: ApplicationFiled: August 2, 2010Publication date: December 16, 2010Inventors: Oivin M. Guicherit, Edward Andrew Boyd, Judith Boyd, Shirley Ann Brunton, Stephen Price, John Harry Alexander Stibbard, Colin H. Mackinnon
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Patent number: 7851484Abstract: Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of muscle weakness and/or cachexia, as part of a rehabilitation or conditioning exercise regimen, or in the treatment of fraility, post-polio syndrome, obesity, sarcopenia, wasting syndrome, muscle spasm, and other indications.Type: GrantFiled: March 28, 2008Date of Patent: December 14, 2010Assignee: Cytokinetics, Inc.Inventors: Bradley P. Morgan, David J. Morgans, Jr., Gustave Bergnes, Alex Muci, Scott Collibee, Pu-Ping Lu, Luke W. Ashcraft, William F. Browne, IV, Marc Andrew Garard
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Patent number: 7846928Abstract: The invention relates to substituted pyrazolopyridines according to the general formula (I): in which A, B, D, E, Ra, R1, R2, R3, R4, R5 and q are as defined in the claims, and salts thereof, to pharmaceutical compositions comprising said substituted pyrazolopyridine compounds, to methods of preparing said substituted pyrazolopyridines, as well as to uses thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.Type: GrantFiled: June 12, 2007Date of Patent: December 7, 2010Assignee: Bayer Schering Pharma AGInventors: Ingo Hartung, Stuart Ince, Georg Kettschau, Karl-Heinz Thierauch, Hans Briem, Ulf Boemer
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Publication number: 20100305324Abstract: A phamaceutical composition comprising a phenyltetrazole derivative of formula (I) or a pharmaceutical acceptable salt thereof is effective in preventing or treating osteoporosis, obesity, diabetes, or hyperlipidemia, by regulating protein TAZ. wherein, A is ethyl or n-butyl; R1 is methyl, —CH2OH, —CO2CH3, —CH2F, —CH(OCH3)2, —CH2OC(?O)CH3, styryl or —CH2OCH2SCH3; R2 is H, Br, —CO2CH3, phenyl, pyridin-2-yl, pyridin-3-yl, ?or styryl; R3 is H or methyl; X is CH or N; and P is H or —CH(CH3)OCH2CH3.Type: ApplicationFiled: April 22, 2010Publication date: December 2, 2010Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Nak Jeong KIM, Myung-Ae Bae, Sung-Eun Yoo, Namsook Kang, Jung Nyoung Heo, Kyu Yang Yi, Jee Hee Suh, Sung Youn Chang, Eun Sook Hwang, Jeong-Ho Hong
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Patent number: 7842698Abstract: The present invention relates to pyridine methylene azolidinone compounds of Formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, allergy, asthma, pancreatitis, multi-organ failure, kidney diseases, platelet aggregation, cancer, sperm motility, graft rejection or lung injuries. Specifically, the present invention is related to pyridine methylene azolidinone derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide-3-kinases, PI3Ks.Type: GrantFiled: September 2, 2005Date of Patent: November 30, 2010Assignee: Merck Serono S.A.Inventors: Thomas Rueckle, Anna Quattropani, Vincent Pomel, Jerome Dorbais, David Covini, Alexander Bischoff
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Publication number: 20100297128Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula [Chemical formula should be inserted here as it appears on abstract in electronic form.] Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).Type: ApplicationFiled: December 9, 2008Publication date: November 25, 2010Inventors: Xianhai Huang, Anandan Palani, Robert G. Aslanian
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Patent number: 7834000Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.Type: GrantFiled: June 13, 2007Date of Patent: November 16, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Corey Gutierrez, Andreas Termin, Sara Hadida-Ruah, Pramod Joshi, Daniele Bergeron, Sanghee Yoo, Hayley Binch, Jon Come, Jingrong Cao, Suganthi Nanthakumar
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Publication number: 20100286191Abstract: The invention encompasses compounds of Formula I or pharmaceutically acceptable salts thereof, which are modulators of the CXCR3 chemokine receptor function useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed.Type: ApplicationFiled: December 8, 2006Publication date: November 11, 2010Inventors: Rachel G. Samuel, Conrad Santini
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Publication number: 20100280012Abstract: An azaazulene compound is provided. The azaazulene compound has formula (I) shown below. Each variable in formula (I) is defined in the specification. The compound can be used to treat cancer. The invention also provides a method for treating cancer. The method includes administering to a subject in need thereof an effective amount of one or more azaazulene compounds of formula (I).Type: ApplicationFiled: April 28, 2010Publication date: November 4, 2010Applicant: INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTEInventor: On LEE
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Publication number: 20100278833Abstract: The invention relates to thiophene-imidazopyridine compounds according to formula (I), wherein the substituents and symbols are as defined in the description. The compounds are inhibitors of PIk1.Type: ApplicationFiled: June 26, 2008Publication date: November 4, 2010Inventors: Thomas Stengel, Mathias Schmidt, Steffen Weinbrenner, Alexander Weber, Petra Gimmnich, Volker Gekeler, Thomas Beckers, Astrid Zimmermann, Thomas Maier, Beata Schmidt, Florian Dehmel
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Publication number: 20100280065Abstract: The invention relates to trisubstituted or tetrasubstituted imidazo[4,5b]pyridines, to their uses as well as to a process for manufacturing them. The compounds of the invention are imidazo[4,5b]pyridines. The first general synthesis of 3,5,7 imidazo[4,5b]pyridines is disclosed in the description. The invention founds application, in particular, in the pharmaceutical field.Type: ApplicationFiled: February 19, 2010Publication date: November 4, 2010Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE RENNES 1, UNIVERSITE PARIS DESCARTESInventors: Laurent MEIJER, Karima BETTAYEB, Herve GALONS, Luc DEMANGE, Nassima OUMATA
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Patent number: 7820664Abstract: This invention concerns to N-(2-aylamino)aryl sulfonamides, which are inhibitors of MEK, methods of using such compounds in the treatment of hyperproliferative diseases, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: January 18, 2008Date of Patent: October 26, 2010Assignee: Bayer Schering Pharma AGInventors: Jean-Michel Vernier, Andreas Maderna, Yung-hyo Koh, Zhi Hong
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Publication number: 20100267698Abstract: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.Type: ApplicationFiled: January 5, 2010Publication date: October 21, 2010Inventors: Guiying Li, Pamela Albaugh, Kevin S. Currie, Guolin Cai, Linda M. Gustavson, Kyungae Lee, Alan Hutchison, George D. Maynard, Jun Yuan, Ling Hong Xie, Manuka Ghosh, Nian Liu, George P. Luke, Scott Mitchell, Martin Patrick Allen, Spiros Liras
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Publication number: 20100267952Abstract: The invention provides a reagent for detecting amyloid in a biological tissue which can be detect amyloid in vitro and in vivo with high sensitivity using a compound which has affinity with amyloid and is suppressed in toxicity such as mutagenicity. The reagent for detecting amyloid deposited in a biological tissue comprises a compound represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represents a carbon or nitrogen; R1 is a halogen substituent; R2 is a halogen substituent; and m is an integer of 0 to 2, provided that at least one of R1 and R2 is a radioactive halogen substituent, at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 and A4.Type: ApplicationFiled: October 28, 2008Publication date: October 21, 2010Applicant: NIHON MEDI-PHYSICS CO., LTD.Inventors: Shigeyuki Tanifuji, Daisaku Nakamura, Shinya Takasaki