Plural Ring Nitrogens In The Additional Hetero Ring (e.g., Imidazole, Pyrazine, Etc.) Patents (Class 514/235.8)
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Publication number: 20110301109Abstract: The present invention relates to a class of phenylpyrimidone compounds, the pharmaceutical composition, the preparation method and the use thereof. More specifically, the present invention relates to a type of phenylpyrimidone compounds of the following formula I, the pharmaceutically acceptable salts or solvates thereof and to the pharmaceutical composition as well as the preparation method of the compounds. The compounds of formula I according to the present invention can effectively inhibit type V phosphodiesterase (PDE5), and thus can be used for the treatment of various vascular disorders, such as male erectile dysfunction, pulmonary hypertension and the like.Type: ApplicationFiled: December 10, 2009Publication date: December 8, 2011Applicants: TOPHARMAN SHANGHAI CO., LTD.Inventors: Zheng Liu, Jianfeng Li, Xiaojun Yang, Zhen Wang, Jinfeng Zhang, Yi Zhu, Guanghui Tian, Qing Jin, Jingkang Shen, Weiliang Zhu, Hualiang Jiang, Jingshan Shen
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Publication number: 20110294798Abstract: The invention relates to cyclic hydrazone compounds, compositions including the cyclic hydrazone compounds and methods of using and methods of making thereof. The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-12.Type: ApplicationFiled: December 23, 2010Publication date: December 1, 2011Applicant: Synta Pharmaceuticals Corp.Inventors: Zachary Demko, Lijun Sun, Howard P. Ng
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Publication number: 20110294810Abstract: The present invention relates (pyridyl)-azinylamino derivatives of formula (I) wherein Q1 and p, Ra to Rc, X, Y, Z, L2 and Q2 represent various substituents, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: November 13, 2009Publication date: December 1, 2011Inventors: Christian Beier, Jurgen Benting, Pierre-Yves Coqueron, Ralf Dunkel, Jorg Greul, Marie-Claire Grosjean-Cournoyer, Hiroyuki Hadano, Philippe Rinolfi, Jean-Pierre Vors
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Publication number: 20110294749Abstract: A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.Type: ApplicationFiled: June 28, 2011Publication date: December 1, 2011Applicant: Astellas Pharma Inc.Inventors: Shinya Nagashima, Hiroshi Nagata, Masahiro Iwata, Masaki Yokota, Hiroyuki Moritomo, Eiichi Nakai, Sadao Kuromitsu, Keiko Ohga, Makoto Takeuchi
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Publication number: 20110294811Abstract: ABT-263 free base and crystalline forms thereof are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.Type: ApplicationFiled: July 28, 2011Publication date: December 1, 2011Applicant: ABBOTT LABORATORIESInventors: Geoff G. Z. Zhang, Paul J. Brackemeyer, Nathaniel D. Catron, Thomas B. Borchardt
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Publication number: 20110293628Abstract: This application describes methods and compositions for reducing, inhibiting and/or treating pain that involve use of ERK2 inhibitors.Type: ApplicationFiled: June 12, 2009Publication date: December 1, 2011Applicant: Cornell UniversityInventors: Charles E. Inturrisi, Qinghao Xu, Sandra M. Garraway
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Patent number: 8067409Abstract: Compounds that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.Type: GrantFiled: November 20, 2008Date of Patent: November 29, 2011Assignee: Abbott LaboratoriesInventors: Nwe Y. Ba-Maung, Randy L. Bell, Richard F. Clark, Scott A. Erickson, Steve D. Fidanze, Robert D. Hubbard, Robert A. Mantei, George S. Sheppard, Bryan K. Sorensen, Gary T. Wang, Jieyi Wang
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Publication number: 20110288071Abstract: The present invention encompasses compounds of general formula (1) wherein A, B, X, R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: November 24, 2009Publication date: November 24, 2011Applicant: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Ioannis Sapountzis
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Publication number: 20110288081Abstract: This invention features pyrimidine compounds of formula (I): Rt is aryl, or heteroaryl; each of R2 and R4, independently, is halogen, nitro, cyano, isothionitro, SRc, or ORc; or R2 and R4, taken together, is carbonyl; R3 is Rc, alkenyl, alkynyl, ORc, OC(O)Rc, SO2Rc, S(O)Rc, S(O2)NRcRd, NRcRd, NRcCORd, NRcC(O)ORd, NRcC(O)NRcRd, NRcSO2Rd, CORc, C(O)ORc, or C(O)NRcRd; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is O, S, S(O), S(O2), or NRc; Y is a covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and each of Rc and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.Type: ApplicationFiled: December 9, 2010Publication date: November 24, 2011Applicant: Synta Pharmaceuticals CorporationInventors: Yumiko Wada, Rongzhen Lu, Albert Y. Hsia
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Publication number: 20110288065Abstract: The present invention relates to a compound represented by general formula [1] satisfying the following (I) or (II), or a pharmaceutical acceptable salt of the compound. (I) X is CH or N; R1 is a halogen atom,; and R2 is H, a halogen atom, CN, [2], [3], [8], [9], an —O-alkyl, an —O-(saturated ring), etc. [2]: —C(RC)(RD)(RE) (RC to RE each are H, an alkyl, etc.) [3]: —N(RF)(RG) (RF and RG each are H, OH, amino, a (hetero)aryl, etc.) [8]: —C(?O)RL (RL is an alkyl, OH, an alkoxy, amino, etc.) [9]: a (substituted)phenyl; (II) X is >C—C(—O)R3 (R3 is a (substituted)amino, an alkoxy, OH, etc.); R1 is a halogen atom; R2 is H; R3 is H or OH; and R3 and R4 each are H or an alkyl.Type: ApplicationFiled: February 5, 2010Publication date: November 24, 2011Applicant: NIPPON SHINYAKU CO., LTD.Inventors: Hidetaka Fujihara, Tetsuo Asaki, Katsutoshi Hori, Haruna Naito
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Publication number: 20110281851Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 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: July 29, 2011Publication date: November 17, 2011Applicant: THERAVANCE, INC.Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
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Publication number: 20110281872Abstract: The invention relates to compositions and methods for the treatment and prevention of cancer and other cell proliferative disorders.Type: ApplicationFiled: March 11, 2011Publication date: November 17, 2011Applicant: Kinex Pharmaceuticals, LLCInventors: David G. Hangauer, JR., Michael J. Ciesielski, Robert A. Fenstermaker
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Publication number: 20110281867Abstract: Compositions and methods are provided for using tyrosine kinase inhibitors to treat pathogenic infection. In particular, methods for using Abl-family tyrosine kinase inhibitors to treat pathogenic infection are provided. Infections to be treated according to the present invention include, particularly, those caused by microbial pathogens such as bacteria and viruses.Type: ApplicationFiled: December 16, 2010Publication date: November 17, 2011Inventors: Daniel KALMAN, William Gerard Bornmann, Patrick Michael Reeves, Alyson Irene Swimm
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Publication number: 20110281838Abstract: The present invention encompasses compounds of general Formula (1) wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: July 28, 2009Publication date: November 17, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Tobias Wunberg, Ralph Brueckner, Dirk Kessler, Oliver Kraemer, Darryl McConnell, Siegfried Schneider, Lars van der Veen
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Publication number: 20110281873Abstract: Disclosed herein are pyrimidinyl compounds that are contemplated to be modulators of cystic fibrosis transmembrane regulators (CFTR), and methods of making and using same. Also provided are pharmaceutical compositions and methods of treating disorders associated with cystic fibrosis transmembrane regulators, such as airway inflammation, cystic fibrosis, and the like.Type: ApplicationFiled: December 11, 2009Publication date: November 17, 2011Inventors: Phoebe Chiang, Shomir Ghosh
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Publication number: 20110281841Abstract: The present invention provides a new group of protein kinase inhibitors, pyrropyrimidine and pyrazolopyrimidine derivatives, and pharmaceutically acceptable salts and prodrugs thereof that are useful for treating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrropyrimidine and pyrazolopyrimidine derivatives.Type: ApplicationFiled: November 12, 2010Publication date: November 17, 2011Applicants: Oscotec, Inc., GenoscoInventors: Jaekyoo Lee, Ho-Juhn Song, Jong Sung Kon, Hee Kyu Lee, Yougsam Kim, Hong Woo Kim, Sunhwa Chang, Sun-Hee Lim, Jang-Sik Choi, Jung-Ho Kim, Se-Won Kim
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Patent number: 8058045Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin-2-yl-pyridin-2-yl-amine and pyrazine-2-yl-pyrimidin-4-yl-amine compounds of formula (I), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. 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 CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc.Type: GrantFiled: October 6, 2008Date of Patent: November 15, 2011Assignee: Cancer Research Technology LimitedInventors: Ian Collins, John Charles Reader, Thomas Peter Matthews, Kwai Ming Cheung, Nicolas Proisy, David Hugh Williams, Sukhbinder Singh Klair, Jane Elizabeth Scanlon, Nelly Piton, Glynn Jonathan Addison, Michael Cherry
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Publication number: 20110275633Abstract: The present invention encompasses compounds of general formula (1) wherein R1-R3 and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: November 13, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ioannis Sapountzis, Bodo Betzemeier, Heinz Stadtmueller
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Publication number: 20110275628Abstract: Disclosed is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, which is useful as a selective antagonist of a 5-HT2B receptor. The compound and salt are useful for treatment or prevention of various diseases and conditions associated with a 5-HT2B receptor.Type: ApplicationFiled: November 24, 2009Publication date: November 10, 2011Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Tadashi Inoue, Yuji Shishido, Hiroaki Ito
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Publication number: 20110275615Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH?CH—, —C?C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by a maximum of two R8 radicals, where R8 is hydrogen, C1-C4-alkyl, branched or unType: ApplicationFiled: October 29, 2010Publication date: November 10, 2011Inventors: Hans-Jörg Treiber, Monika Knopp, Wilfried Lubisch, Achim Moeller
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Patent number: 8053457Abstract: The invention relates to 3-heterocyclyl indolyl compounds of formula I capable of inhibiting the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively: wherein R1, R2, R3, R4, RA, Y and Y are as defined in the specification. Due to their activity, the compounds are useful in the treatment of various disorders and diseases mediated by the activity of MDM2 and/or MDM4, or variants thereof, such as inflammatory or proliferative diseases or in the protection of cells.Type: GrantFiled: March 27, 2008Date of Patent: November 8, 2011Assignee: Novartis AGInventors: Andreas Boettcher, Nicole Buschmann, Pascal Furet, Jean-Marc Groell, Jorg Kallen, Joanna Hergovich Lisztwan, Keiichi Masuya, Lorenz Mayr, Andrea Vaupel
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Publication number: 20110269759Abstract: 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 R1, R2, R3, Ra, and Y are defined herein.Type: ApplicationFiled: October 28, 2010Publication date: November 3, 2011Inventors: Steven J. COATS, Haiyan BIAN, Chaozhong CAI, Bart L. DECORTE, Li LIU, Mark J. MACIELAG, Scott L. DAX, Philip M. PITIS, Peter J. CONNOLLY, Wei HE
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Publication number: 20110269760Abstract: Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerisation and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).Type: ApplicationFiled: July 14, 2011Publication date: November 3, 2011Applicant: Cytopia Research Pty LtdInventors: Christopher John Burns, Andrew Frederick Wilks, Michael Francis Harte, Harrison Sikanyika, Emmanuelle Fantino
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Publication number: 20110269721Abstract: Provided herein are method of treating, ameliorating, or delaying at least one symptom of a genetic blood disorder, e.g. sickle cell disorder or thalassemia, in a patient in need thereof, comprising administering a therapeutically effective amount of a Jak2 inhibitor. Also provided in part is a method of reducing an enlarged spleen in a patient suffering from thalassemia, comprising administering a therapeutically effective amount of a Jak2 inhibitor.Type: ApplicationFiled: August 3, 2009Publication date: November 3, 2011Applicant: TargeGen, Inc.Inventor: John D. Hood
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Publication number: 20110269761Abstract: The invention relates to substituted aryl-sulphonylglycine derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as in the specification and claims, which are suitable for preparing a pharmaceutical composition for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.Type: ApplicationFiled: April 17, 2009Publication date: November 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Elke Langkopf, Frank Himmelsbach, Juergen Mack, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
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Patent number: 8048881Abstract: The invention relates to 4-aminocarbonyl-pyrimidine derivatives and their use as P2Y12 receptor antagonists in the treatment and/or prevention and/or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.Type: GrantFiled: April 27, 2006Date of Patent: November 1, 2011Assignee: Actelion Pharmaceuticals Ltd.Inventors: Eva Caroff, Heinz Fretz, Kurt Hilpert, Olivier Houille, Francis Hubler, Emmanuel Meyer
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Publication number: 20110263601Abstract: Methods are disclosed for treating ulcerative colitis and related diseases and disorders, which comprise inhibiting tryptophan hydroxylase (TPH) in patients in need thereof.Type: ApplicationFiled: October 25, 2010Publication date: October 27, 2011Inventors: Philip Manton Brown, Qingyun Liu, Brian Zambrowicz
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Publication number: 20110263557Abstract: 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; such as, but not limited to, diabetes, obesity and associated metabolic disorders. Formula (I) is a compound, in which A can have up to 2 ring —CH2- group substituted with —C(O)— and can be partially unsaturated with up to 2 double bonds; Wi and W2 are independently selected from CR10 and N; wherein R10 is selected from hydrogen and C1_6alkyl; Yi is selected from NRn, O and S; wherein Rn is selected from hydrogen and C1_6alkyl; Y2 and Y3 are independently selected from CH and N; Y4 is selected from CH2, OCH2 and NR15; wherein R15 is selected from hydrogen and C1_6alkyl; or the pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 3, 2009Publication date: October 27, 2011Applicant: IRM LLCInventors: Christopher Cow, Robert Epple
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Publication number: 20110263565Abstract: The present invention encompasses compounds of general formula (1), wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: July 28, 2009Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Treu, Thomas Karner, Ulrich Reiser
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Publication number: 20110257155Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.Type: ApplicationFiled: June 29, 2011Publication date: October 20, 2011Applicant: IRM LLCInventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, Bei Chen, Tetsuo Uno
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Publication number: 20110257154Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.Type: ApplicationFiled: June 29, 2011Publication date: October 20, 2011Applicant: IRM LLCInventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
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Publication number: 20110251174Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: June 14, 2011Publication date: October 13, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan Karl ZAHN, Guido BOEHMELT, Andreas MANTOULIDIS, Ulrich REISER, Matthias TREU, Ulrich GUERTLER, Andreas SCHOOP, Flavio SOLCA, Ulrike TONTSCH-GRUNT, Ralph BRUECKNER, Charlotte REITHER, Lars HERFURTH, Oliver KRAEMER, Heinz STADTMUELLER, Harald ENGELHARDT
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Publication number: 20110245249Abstract: Heterocyclically substituted anilinopyrimidines of the formula (I) in which R1 to R12 and E1, E2, E3, L1, Y, Z and L2 have the meanings given in the description, and agrochemically active salts thereof, their use and also methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants, processes for preparing such compositions and treated seed and also their use for controlling phytopathogenic harmful fungi in agriculture, horticulture and forestry, in the protection of materials and in the domestic and hygiene field. The present invention furthermore relates to a process for preparing heterocyclically substituted anilinopyrimidinenes of the formula (I).Type: ApplicationFiled: August 22, 2009Publication date: October 6, 2011Applicant: Bayer CropScience AGInventors: Pierre Wasnaire, Jorg Nico Greul, Oliver Gaertzen, Hendrik Helmke, Stefan Hillebrand, Amos Mattes, Carl Friedrich Nising, Ulrike Wachendorff-Neumann, Peter Dahmen, Arnd Voerste, Ruth Meissner, Christoph Andreas Braun, Martin Kaussmann, Hiroyuki Hadano
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Publication number: 20110245205Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.Type: ApplicationFiled: December 15, 2010Publication date: October 6, 2011Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Sathesh Bhat, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Jean-Francois Fournier, Jacques Yves Gauthier, Jonathan Grimm, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Matthew L. Maddess, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Alessia Petrocchi, Michael H. Reutershan, Joel S. Robichaud, Eric Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hyun Chong Woo, Hua Zhou
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Publication number: 20110245156Abstract: Compounds are disclosed. Compositions that include the compounds are disclosed. Methods of making and using the compounds are also disclosed.Type: ApplicationFiled: December 9, 2009Publication date: October 6, 2011Applicant: CYTOKINE PHARMASCIENCES, INC.Inventor: Thais M. Sielecki-Dzurdz
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Publication number: 20110237586Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade. The invention relates to compounds of the formula I: or a pharmaceutically acceptable salt thereof The compounds of the invention are useful for methods of protecting against or treating hearing loss, osteoporosis, cell proliferative disorders, obesity, diabetes, eye disease, stroke, atherosclerosis, neuropathic pain or hepatitis B.Type: ApplicationFiled: June 3, 2011Publication date: September 29, 2011Applicant: Kinex Pharmaceuticals, LLCInventor: David G. Hangauer, JR.
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Publication number: 20110237585Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: March 15, 2011Publication date: September 29, 2011Applicant: JANSSEN PHARMACEUTICA N.V.Inventors: Sven Franciscus Anna Van Brandt, Kristof Van Emelen, Patrick René Angibaud, Laurence Françoise Bernadette Marconnet-Decrane, Janine Arts
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Publication number: 20110230485Abstract: This invention relates to novel 6-phenyl-phymidin-4-yl-(phenylannine or phenoxy) derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: October 9, 2009Publication date: September 22, 2011Applicant: NEUROSEARCH A/SInventors: Antonio Nardi, Jeppe Kejser Christensen, Dan Peters
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Publication number: 20110230483Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: March 14, 2011Publication date: September 22, 2011Inventors: Urs BAETTIG, Kamlesh Jagdis BALA, Emma BUDD, Lee EDWARDS, Catherine Howsham, Glyn HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
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Publication number: 20110230479Abstract: The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.Type: ApplicationFiled: October 22, 2010Publication date: September 22, 2011Inventors: Frank M. Longo, Stephen M. Massa
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Publication number: 20110230484Abstract: This invention relates to novel pyrazolyl-pyrimidine derivatives and their use as potassium channel modulating agents. In another aspect the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.Type: ApplicationFiled: August 26, 2009Publication date: September 22, 2011Applicant: NEUROSEARCH A/SInventors: Birgitte L. Eriksen, Charlotte Hougaard, Dan Peters, Palle Christophersen
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Publication number: 20110230476Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: September 9, 2010Publication date: September 22, 2011Applicant: AVILA THERAPEUTICS, INC.Inventors: DEQIANG NIU, RUSSELL C. PETTER, JUSWINDER SINGH, ARTHUR F. KLUGE, HORMOZ MAZDIYASNI, ZHENDONG ZHU, LIXIN QIAO, KEVIN KUNTZ
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Patent number: 8022061Abstract: Compounds having formula I: where A1, A2, L, V, W, R1, R2, R3, R4 and R5 are as described herein, compositions thereof, and their use for the treatment or prevention of type 2 diabetes and type 2 diabetes-related conditions are provided herein.Type: GrantFiled: October 9, 2007Date of Patent: September 20, 2011Assignee: Amgen Inc.Inventors: Yasuyuki Ogawa, Ryo Okuyama, Satoshi Shibuya, Narihiro Toda, Zhaodan Cao, Zice Fu, Xiaolin Hao, Yong-Jae Kim, Leping Li, Sarah E. Lively, Mike Lizarzaburu, Hui Tian, Ming Yu
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Publication number: 20110224211Abstract: Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.Type: ApplicationFiled: November 19, 2009Publication date: September 15, 2011Inventors: Frank Ulrich Schmitz, Roopa Rai, Christopher Ron Roberts, Wieslaw Kazmierski, Richard Grimes
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Publication number: 20110224185Abstract: 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: May 23, 2011Publication date: September 15, 2011Inventors: 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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Patent number: 8017608Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: March 5, 2004Date of Patent: September 13, 2011Assignee: Novartis AGInventors: Graham Charles Bloomfield, Ian Bruce, Catherine Leblanc, Mrinalini Sachin Oza, Lewis Whithead, Bernard Cuenoud, Thomas Hugo Keller, Louise Kirman, Clive McCarthy, Gaynor Elizabeth Woodward
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Publication number: 20110218175Abstract: The present invention relates to antiviral compounds of formula (I), compositions containing these compounds, processes for their preparation, intermediates in their synthesis, and their use as therapeutics for prevention of organ transplantation rejection, the treatment of immune disorders and inflammation, and treatment of viral (particularly hepatitis C viral) infection.Type: ApplicationFiled: February 23, 2011Publication date: September 8, 2011Inventors: Yat Sun Or, Guoqiang Wang, Xuri Gao
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Publication number: 20110218200Abstract: The present invention is directed to compounds that inhibit amyloid aggregation and methods of treatment there-with.Type: ApplicationFiled: August 28, 2009Publication date: September 8, 2011Inventors: Christopher J. Barden, Michael D. Carter, Mark A. Reed, Donald F. Weaver, Arun Yadav, Shengguo Sun
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Publication number: 20110218188Abstract: The present invention relates to phenyl-pyrimidinyl-amino derivatives of formula (I) wherein Q1 and p, Ra to Rc, L1, Y, L2 and Q2 represent various substituents, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: November 12, 2009Publication date: September 8, 2011Inventors: Christian Beier, Jurgen Benting, Isabelle Christian, Pierre-Yves Coqueron, Peter Dahmen, Ralf Dunkel, Jorg Greul, Marie-Claire Grosjean-Cournoyer, Hiroyuki Hadano, Philippe Rinolfi, Arnd Voerste, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
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Publication number: 20110218182Abstract: The invention relates to chemical compounds of formula (I), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of PIM kinase related conditions and diseases, preferably cancer.Type: ApplicationFiled: July 2, 2009Publication date: September 8, 2011Applicant: ASTRAZENECA ABInventors: Leslie Dakin, James Edward Dowling, Michelle Lamb, Jon Read, Qibin Su, Xiaolan Zheng