Four Or More Ring Nitrogens In The Tricyclo Ring System Patents (Class 544/251)
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Publication number: 20120004203Abstract: The present invention relates to novel heterocyclically fused diaryldihydropyrimidine derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: ApplicationFiled: December 29, 2009Publication date: January 5, 2012Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig
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Publication number: 20110312940Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4, A, X, m and k 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: October 15, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Lars Van Der Veen, Darryl McConnell, Tobias Wunberg
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Patent number: 8080658Abstract: A material for organic electroluminescence devices for use as a host material in combination with at least one phosphorescent metal complex contains a compound represented by formula 1: wherein R1 to R10 are each independently hydrogen atom, halogen atom, alkyl group having 1 to 40 carbon atoms, cycloalkyl group having 3 to 15 carbon atoms, heterocyclic group having 3 to 20 carbon atoms which is optionally substituted, alkoxy group having 1 to 40 carbon atoms, non-condensed aryl group having 6 to 40 carbon atoms, condensed aryl group having 10 to 18 carbon atoms, aryloxy group having 6 to 20 carbon atoms, aralkyl group having 7 to 20 carbon atoms, arylamino group having 6 to 40 carbon atoms, alkylamino group having 1 to 40 carbon atoms, aralkylamino group having 7 to 60 carbon atoms, arylcarbonyl group having 7 to 40 carbon atoms, alkyl halide group having 1 to 40 carbon atoms, or cyano group, R8 and R9 being optionally bonded to each other to form a ring structure and each of R1 to R10 being optionallyType: GrantFiled: July 10, 2007Date of Patent: December 20, 2011Assignee: Idemitsu Kosan Co., Ltd.Inventors: Toshihiro Iwakuma, Jun Endo, Masaki Numata, Kenichi Fukuoka
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Publication number: 20110294662Abstract: The present invention relates to the use of new and known dithiine derivatives for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to new dithiine derivatives, to processes for preparing them, to their use, and to crop protection compositions comprising these new dithiine derivatives.Type: ApplicationFiled: April 14, 2011Publication date: December 1, 2011Applicant: Bayer CropScience AGInventors: Thomas SEITZ, Jürgen Benting, Ulrike Wachendorff-Neumann
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Patent number: 8058270Abstract: Disclosed is the use of a compound of general Formula (1), optionally in form of its tautomers, racemates, enantiomers, diastereomers and the mixtures thereof and optionally in form of the pharmacologically acceptable acid addition salts, solvates, hydrates, polymorphs, physiologically functional derivatives or prodrugs thereof, for the preparation of a pharmaceutical composition for the treatment of diseases characterized by abnormal cell proliferation in a human or non-human mammalian body by inhibition of polo like kinases as mitotic regulators.Type: GrantFiled: May 15, 2008Date of Patent: November 15, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Gerd Munzert, Martin Steegmaier
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Publication number: 20110274679Abstract: Compositions and methods of SIRT activation are presented in which one or more vitamin compounds, and especially vitamin B compounds are used to significantly increase SIRT activity in vitro and in vivo. In especially preferred compositions, vitamin B6, vitamin B12, and vitamin B2 are present in synergistic quantities.Type: ApplicationFiled: November 5, 2009Publication date: November 10, 2011Applicant: VDF FutureCeuticals, Inc.Inventor: Zbigniew Pietrzkowski
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Publication number: 20110262970Abstract: A method for producing a fermentation product from a lignocellulose-containing material comprises pre-treating the lignocellulose-containing material; introducing a cationic polysaccharide to the pre-treated lignocellulose-containing material; exposing the pre-treated lignocellulose-containing material to an effective amount of a first hydrolyzing enzyme; and fermenting with a fermenting organism to produce a fermentation product. The cationic polysaccharide may be a cationic starch.Type: ApplicationFiled: September 30, 2009Publication date: October 27, 2011Applicant: Novozymes North America, Inc.Inventors: Xin Li, Ye Chen, Jing Luo, Lindsay Jones
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Publication number: 20110257137Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.Type: ApplicationFiled: March 10, 2011Publication date: October 20, 2011Applicant: KALYPSYS, INC.Inventors: Allen Borchardt, Robert Davis, Clay Beauregard, Daniel Becker, Daniel Gamache, Stewart A. Noble, Mark Hellberg, Peter Klimko, Zhihai Qiu, Joseph Payne, John Yanni
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Patent number: 8039478Abstract: The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease.Type: GrantFiled: November 3, 2008Date of Patent: October 18, 2011Assignee: Incyte CorporationInventors: Changsheng Zheng, Chu-Biao Xue, Ganfeng Cao, Michael Xia, Anlai Wang, Hai Fen Ye, Brian Metcalf
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Publication number: 20110237561Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-imidazo[1,2-a]pyrrolo[3,4-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-pyrimido[1,2-a]pyrrolo[3,4-e]pyrimidine compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising the same.Type: ApplicationFiled: December 7, 2009Publication date: September 29, 2011Inventors: Peng Li, Jun Zhao, Hailin Zeng, Lawrence Wennogle
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Publication number: 20110224195Abstract: The present invention is directed to substituted six-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as obesity and diabetes, 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: ApplicationFiled: August 18, 2008Publication date: September 15, 2011Inventors: Tesfaye Biftu, Danqing Feng, Ann E. Weber, Jason M. Cox, Xiaoxia Qian, Jinyou Xu
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Publication number: 20110224222Abstract: The invention provides a low molecular weight ATP-competitive CDK inhibitor for use in the treatment of mesothelioma. The compound can be administered together with one or more cytotoxic or cytostatic agents.Type: ApplicationFiled: November 23, 2009Publication date: September 15, 2011Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Marina Ciomei, Angela Scaburri
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Publication number: 20110212942Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: December 21, 2010Publication date: September 1, 2011Inventors: Robert A. Galemmo, Dean R. Artis, Xiaocong Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Publication number: 20110207740Abstract: Disclosed are useful pharmaceutical compositions.Type: ApplicationFiled: April 4, 2011Publication date: August 25, 2011Inventors: Susan K. Heimbecher, Jim H. Kou, Irina Kazakevich
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Publication number: 20110207716Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, E1, E2, R1, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: December 21, 2010Publication date: August 25, 2011Inventors: Robert A. Galemmo, Dean R. Artis, Xiaocong Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Publication number: 20110190311Abstract: The invention provides a low molecular weight ATP-competitive CDK inhibitor able to cross the blood brain barrier for use in the treatment of malignant glioma and, in particular, of glioblastoma. The compound can be administered together with one or more agents selected from the group consisting of cytotoxic or cytostatic agents and ionizing radiation.Type: ApplicationFiled: July 28, 2009Publication date: August 4, 2011Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Marina Ciomei, Francesco Fiorentini, Enrico Pesenti
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Publication number: 20110183992Abstract: Provided are therapeutic and/or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof; therapeutic and/or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A2A receptor antagonistic activity, which has an affinity for the adenosine A2A receptor 10 times or higher than that for the adenosine A1 receptor, or a pharmaceutically acceptable salt thereof; and the like.Type: ApplicationFiled: July 23, 2009Publication date: July 28, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Junichi Ikeda, Shunji Ichikawa, Masako Kurokawa, Tomoyuki Kanda
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Publication number: 20110160233Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.Type: ApplicationFiled: December 19, 2007Publication date: June 30, 2011Applicant: ABBOTT LABORATORIESInventors: David A. Betebenner, Clarence J. Maring, Todd W. Rockway, Curt S. Cooper, David D. Anderson, Rolf Wagner, Rong Zhang, Akhteruzzaman Molla, Hongmei Mo, Tami J. Pilot-Matias, Sherie VL. Masse, Robert J. Carrick, Wenping He, Liangjun Lu
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Publication number: 20110152256Abstract: Compounds of the Formula I wherein R1 and R2 together with the carbon atoms to which they are bonded optionally form a further heteroaromatic ring of the formula (II) as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.Type: ApplicationFiled: March 3, 2009Publication date: June 23, 2011Inventors: Joel M. Harris, Bernard R. Neustadt, Hong Liu, Jinsong Hao, Andrew W. Stamford
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Publication number: 20110142796Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.Type: ApplicationFiled: December 18, 2008Publication date: June 16, 2011Applicant: Amgen IncInventors: Richard V. Connors, Kang Dai, John Eksterowicz, Pingchen Fan, Benjamin Fisher, Jiasheng Fu, Kexue Li, Zhihong Li, Lawrence R. Mcgee, Rajiv Sharma, Xiaodong Wang, Dustin L. Mcminn, Jeffrey T. Mihalic, Jeffrey Deignan
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Publication number: 20110130405Abstract: This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula (I) shown below wherein the meanings of the substituents are defined in claim 1 and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: June 2, 2011Applicant: Shire LLCInventors: Bernard Golding, Richard Franklin, Kim Hirst
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Publication number: 20110124654Abstract: The invention relates to 1,5-diazacarbazole compounds of Formula (I), (I-a), (I-b), (I-c), (I-d), (I-e), (I-f), (I-g) and (I-h) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: June 10, 2009Publication date: May 26, 2011Inventors: Huifen Chen, Hazel Joan Dyke, Emanuela Gancia, Lewis J. Gazzard, Simon Goodacre, Joseph Lyssikatos, Calum Macleod, Karen Williams
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Publication number: 20110110914Abstract: Methods and formulations for treating oncological disorders in humans using epimetabolic shifters, multidimensional intracellular molecules or environmental influencers are described.Type: ApplicationFiled: May 11, 2010Publication date: May 12, 2011Inventors: Niven Rajin Narain, John Patrick McCook, Rangaprasad Sarangarajan
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Publication number: 20110105542Abstract: The present invention relates to pyrazolo-quinazolines, characterized by an ortho-substituted-arylamino, heterocyclylamino- or C3-C7 cycloalkylamino residue at 8 position and an aryl, heterocyclyl or C3-C7 cycloalkyl as substituent of a carboxamide at 3 position of the molecula framework. The compounds of this invention modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular MPS1/TTK. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: June 17, 2009Publication date: May 5, 2011Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Marina Caldareli, Mauro Angiolini, Riccardo Colombo, Teresa Disingrini, Stefano Nuvoloni, Helena Posteri, Matteo Salsa, Marco Silvagni
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Publication number: 20110105477Abstract: The present invention relates to HIV protease, and methods for inhibiting the function of HIV protease. In particular, present invention provides compounds that inhibit or block the biological activity of HIVp, thereby causing the replication of the HIV virus to be inhibited or to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS. The compounds and formulations also find use in diagnostic and research settings.Type: ApplicationFiled: September 12, 2008Publication date: May 5, 2011Applicant: The Regents of the University of MichiganInventors: Heather A. Carlson, Kelly L. Damm, Kristen L. Meagher
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Patent number: 7932257Abstract: The present invention provides compounds having the formula: wherein A-B together represent one of the following structures: wherein one of is a double bond, as valency permits; and R2, R4, X1A, X2A, X1B, X2B, L1, L2, Y and Z are as defined in classes and subclasses herein, and pharmaceutical compositions thereof, as described generally and in subclasses herein, which compounds are useful as inhibitors of protein kinase (e.g., Aurora), and thus are useful, for example, for the treatment of Aurora mediated diseases.Type: GrantFiled: July 21, 2006Date of Patent: April 26, 2011Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Johan D. Oslob, Chul Hyun Yu
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Publication number: 20110092525Abstract: The resent invention relates to novel compounds of the general formula (I) having anxiolytic, anticonvulsant, sedative-hypnotic and myorelaxant conditions as well as anxiogenic, somnolytic and convulsant conditions in mammals, including humans, as GABAA receptor modulator.Type: ApplicationFiled: April 2, 2009Publication date: April 21, 2011Inventors: Mogens Nielsen, Tommy Liljefors, Jakob Nilsson, Olov Sterner
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Publication number: 20110077401Abstract: The invention relates to compounds of formula 1, tautomers and salts thereof, wherein R1, R2, R3, R4, and R5 have the meanings indicated in the specification. These compounds are receptor tyrosine kinase EphB4 inhibitors useful for the treatment of angiogenesis dependent cancers and intraocular neovascular syndromes. The invention further relates to a method termed ALTA (anchor-based library tailoring) of selecting compounds from a large compound library for screening as EphB4 inhibitors by computational procedures.Type: ApplicationFiled: January 23, 2009Publication date: March 31, 2011Applicant: UNIVERSITAET ZUERICHInventors: Danzhi Huang, Peter Kolb, Karine Lafleur, Cristina Nevado, Amedeo Caflisch
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Publication number: 20110065738Abstract: The present invention relates to Polycyclic Guanine Derivatives, compositions comprising the Polycyclic Guanine Derivatives and methods of using the Polycyclic Guanine Derivatives to treat pain or an inflammatory disease.Type: ApplicationFiled: June 18, 2008Publication date: March 17, 2011Inventors: Deen Tulshian, William B. Geiss, Gregory S. Martin, Van-Duc Le, James C. Haber, JR., Julius J. Matasi, Michael F. Czarniecki, Stephanie Nicole Cooke
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Publication number: 20110065712Abstract: The invention provides compounds that inhibit CK2 and/or Pim kinases and compositions containing such compounds. These tricyclic compounds and compositions containing them are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, pathogenic infections, and certain immunological disorders.Type: ApplicationFiled: September 16, 2010Publication date: March 17, 2011Applicant: CYLENE PHARMACEUTICALS , INC.Inventors: Mustapha HADDACH, Fabrice Pierre
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Publication number: 20110065703Abstract: The present invention includes a group of chemical compounds useful as modulators of calcium ion (Ca2+) channels, especially for T-type, N-Type and L-type channels. The present invention also includes pharmaceutical compositions comprising these calcium ion channel modulating agents and methods of using these calcium ion channel modulating agents for the treatment diseases and conditions associated with the calcium ion channels.Type: ApplicationFiled: March 12, 2008Publication date: March 17, 2011Inventor: Jay Jie-Qiang Wu
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Patent number: 7902205Abstract: The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease.Type: GrantFiled: September 25, 2008Date of Patent: March 8, 2011Assignee: Incyte CorporationInventors: Chu-Biao Xue, Brian Metcalf, Anlai Wang, Changsheng Zheng, Ganfeng Cao, Ke Zhang
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Publication number: 20110046149Abstract: The invention relates to serotonin 5-HT6 receptor antagonists—novel 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines, drug substances and pharmaceutical compositions comprising the said drug substances as the said compounds, and also to method of prophylaxis and treatment of various diseases of central nervious system in humans and animals pathogenesis of which is associated with serotonin 5-HT6 receptors including cognitive and neurodegenerative diseases. Substituted 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines of the general formula 1 and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines of the general formula 2 and pharmaceutically acceptable salts and/or hydrates thereof.Type: ApplicationFiled: April 30, 2009Publication date: February 24, 2011Inventors: Andrey Alexandrovich Ivashchenko, Volodymyr Mikhailovich Kysil, Nikolay Filippovich Savchuk, Alexander Vasilievich Ivashchenko
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Publication number: 20110039870Abstract: The present invention relates to serotonin 5-HT6 receptor antagonists-novel substituted 3-sulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 3-sulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines, drug substances and pharmaceutical compositions comprising drug substances as the mentioned above compounds and to the method of prophylaxis and treatment of various conditions and diseases of central nervous system in humans and warm-blooded animals pathogenesis of which is associated with serotonin 5-HT6 receptors. In formulas 1 and 2 Ar is optionally substituted aryl or optionally substituted heterocyclyl; R1 is hydrogen, optionally substituted lower C1-C3 alkyl, substituted hydroxyl group, substituted sulfanyl group; R2 is hydrogen or optionally substituted C1-C3 alkyl; R3 is hydrogen, optionally substituted C1-C3 alkyl or tert.-butyloxycarbonyl.Type: ApplicationFiled: April 30, 2009Publication date: February 17, 2011Inventors: Andrey Alexandrovich Ivashchenko, Volodymyr Mikhailovich Kysil, Nikolay Filippovich Savchuk, Alexander Vasilievich Evashchenko
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Publication number: 20110038876Abstract: Disclosed are the ERK inhibitors of formula 1.0: [Formula (1.0)] and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.Type: ApplicationFiled: June 17, 2008Publication date: February 17, 2011Inventors: Robert Sun, Alan B. Cooper, Yongqi Deng, Tong Wang, Yang Nan, Hugh Y. Zhu, Sobhana Babu Boga, Xiaolei Gao, Joseph M. Kelly, Sunil Paliwal, Hon-Chung Tsui, Ronald J. Doll, Neng-Yang Shih
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Publication number: 20110021519Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. 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 compounds of the inventions.Type: ApplicationFiled: June 8, 2010Publication date: January 27, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jean-Damien Charrier, David Kay, Ronald Knegtel
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Publication number: 20110002855Abstract: Piperazinyl oxoalkyl tetrahydro-beta-carbolines and related analogues of the formula (I): are provided, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).Type: ApplicationFiled: June 25, 2008Publication date: January 6, 2011Applicant: NEUROGEN CORPORATIONInventors: Timothy M. Caldwell, Yang Gao, Linghong Xie, Yuelian Xu
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Patent number: 7855206Abstract: The present invention is directed to novel substituted tricyclic heteroaromatic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme 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: November 9, 2007Date of Patent: December 21, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Jason M. Cox, Hong Dong
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Patent number: 7851478Abstract: For example, an agent for preventing and/or treating movement disorder comprising, as an active ingredient, a triazolopyrimidine derivative having an adenosine A2A receptor antagonistic action, which is represented by the following formula (I): (wherein R1 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, R2 represents a hydrogen atom, or the like, R3 represents —WR4, or the like, and Q1 represents a hydrogen atom or 3,4-dimethoxybenzyl), or a pharmaceutically acceptable salt thereof, and the like are provided.Type: GrantFiled: June 7, 2006Date of Patent: December 14, 2010Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Takako Kadowaki, Minoru Kobayashi, Shizuo Shiozaki, Naoki Seno
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Publication number: 20100311762Abstract: The use of tetrahydrofolate, methylene-tetrahydrofolate and/or methyl-tetrahydrofolate, and at least one multi-targeting antifolate, for the manufacture of a pharmaceutical composition for the treatment of cancer is disclosed. By combining the multi-targeting antifolate with tetrahydrofolate, methylene-tetrahydrofolate and/or methyl-tetrahydrofolate, it is possible to remarkably reduce toxic side-effects without diminishing the anti-tumour action of the drugs. A pharmaceutical composition, a kit comprising the pharmaceutical composition as well as a method for the treatment of cancer are also disclosed.Type: ApplicationFiled: July 22, 2010Publication date: December 9, 2010Inventors: Bengt Gustavsson, Göran Carlsson
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Publication number: 20100284913Abstract: Saxitoxin analogue compounds, compositions, pharmaceutical compositions, methods of synthesis of saxitoxin analogues, methods of imaging, methods of treatment, including methods of treating pain, are provided. Saxitoxin (STX), gonyautoxin (GTX), and zetekitoxin, and variant STX compounds bind to sodium channels and are effective to reduce or block flow of sodium ions through such channels. Such channel block affects nerve and muscle action, and may be effective to reduce or block pain sensations, relax muscles, reduce muscle spasm, and reduce wrinkles. STX analogue binding to sodium channels may also be useful to locate, image, or mark sodium channels, and so be useful in studying sodium channels and sodium channel disorders, and in the diagnosis and treatment of patients suffering from sodium channel disorders. In embodiments, the variant STX compounds include conjugates having increased serum half-life as compared to STX when administered to a subject.Type: ApplicationFiled: May 7, 2010Publication date: November 11, 2010Applicant: The Board of Trustees of the Leland Stanford JunioInventors: Justin Du Bois, John Mulcahy, Brian Andresen, David C. Yeomans, Sandip Biswal
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Patent number: 7825242Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound of the formula: wherein R2 is amino (C1-6)alkyl, hetero(C3-12)cycloakyl, hetero(C4-12)bicycloaryl, heteroaryl, or cyano; and W, X, Y, Z, R1, R5 and R7 are as defined herein.Type: GrantFiled: July 15, 2005Date of Patent: November 2, 2010Assignee: Takeda Pharmaceutical Company LimtedInventors: Jun Feng, Stephen L. Gwaltney, Betty Lam, Zhiyuan Zhang
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Publication number: 20100267728Abstract: This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors.Type: ApplicationFiled: September 19, 2008Publication date: October 21, 2010Applicant: CORTEX PHARMACEUTICALS, INC.Inventors: Rudolf Mueller, Leslie J. Street, Stanislaw Rachwal, Kashinatham Alisala
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Publication number: 20100267671Abstract: The present invention includes and relates generally to compounds which modulate apoptosis in cells. The present invention also provides pharmaceutical compositions containing these compounds, methods of making these compounds, and methods of using these compounds and pharmaceutical compositions for treatment of diseases associated with irregular apoptosis in cells.Type: ApplicationFiled: February 9, 2010Publication date: October 21, 2010Inventors: Jay Jie-Qiang Wu, Ling Wang
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Publication number: 20100249110Abstract: The present invention relates to substituted pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: March 31, 2010Publication date: September 30, 2010Applicant: ArQule, Inc.Inventors: Manish Tandon, Jianqiang Wang, Nivedita Namdev
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Publication number: 20100216808Abstract: Pyrazolo-quinazoline derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: December 17, 2007Publication date: August 26, 2010Applicant: Nerviano Medical Sciences S.r.lInventors: Michele Caruso, Italo Beria, Maria Gabriella Brasca, Ronald Ferguson, Helena Posteri, Barbara Valsasina
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Publication number: 20100210639Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain tricyclic compounds (referred to herein as TC compounds), and especially certain 9H-pyrimido[4,5-b]indole, 9H-pyrido[4?,3?:4,5]pyrrolo[2,3-d]pyridine, and 9H-1,3,6,9-tetraaza-fluorene compounds, 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., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.Type: ApplicationFiled: July 1, 2008Publication date: August 19, 2010Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Ian Collins, John Charles Reader, Suki Klair, Jane Scanlon, Glynn Addison, Michael Cherry
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Patent number: 7763629Abstract: The present invention relates to compounds useful as inhibitors of protein kinase, represented by Structural Formula (I): wherein the variables in Structural Formula (I) are as described herein. 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 compounds of the inventions.Type: GrantFiled: April 12, 2007Date of Patent: July 27, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, David Kay, Ronald Knegtel
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Publication number: 20100163813Abstract: The instant invention relates to novel benzotriazole UV-absorbers having a long wavelength shifted absorption spectrum with significant absorbance up to 410-420 nm. Further aspects of the invention are a process for their preparation, a UV stabilized composition containing the new UV-absorbers and the use of the new compounds as UV-light stabilizers for organic materials.Type: ApplicationFiled: June 18, 2007Publication date: July 1, 2010Inventors: Katharina Fritzsche, Markus Grob, Adalbert Braig, Iloan Marion Kienzle, Gérard Daniel Georges Vilain
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Publication number: 20100144744Abstract: Novel compounds are provided which are 1 1-beta-hydroxysteroid dehydrogenase type I inhibitors. 1 1-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 1 1-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: W-L-Z or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, L are defined herein and Z is selected from the following bicyclic heteroaryl groups: (a), (b), (c), (d).Type: ApplicationFiled: April 16, 2008Publication date: June 10, 2010Inventors: Jun Li, James J. Li, Stephen P. O'Connor, Haixia Wang, Lawrence J. Kennedy, Jeffrey A. Robl, Lawrence G. Hamann