Tricyclo Ring System Having 1,3-diazine As One Of The Cyclos Patents (Class 514/267)
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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: 20110064671Abstract: The present invention relates to a method of increasing blood brain barrier permeability in a subject. This method involves selecting a subject who would benefit from increased blood brain barrier permeability and subjecting the selected subject to a treatment. That treatment increases adenosine level and/or bioavailability, modulates adenosine receptors, and/or increases CD73 level and/or activity under conditions effective to increase blood brain barrier permeability in the subject. Methods of decreasing blood brain barrier permeability in a subject, treatment of a subject for a disorder or condition of the central nervous system, and screening compounds effective in increasing blood brain barrier permeability, as well as pharmaceutical agents are also disclosed.Type: ApplicationFiled: March 10, 2009Publication date: March 17, 2011Applicant: CORNELL UNIVERSITYInventor: Margaret S. Bynoe
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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: 20110059997Abstract: The invention relates to substituted 2-alkylsulfanyl-3-(arylsulfonyl)-cycloalkyl[e and d]pyrazolo[1,5-a]pyrimidines, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions, comprising the said conpounds as active ingredients, to novel medicaments and methods for treatment and prophylaxis of CNS diseases of humans and warm blooded animals pathogenesis of which is associated with 5-HT6 receptors. In general formulas 1 and 2 R1 represents hydrogen or C1-C3 alkyl; R2 represents C1-C3 alkyl; R3 represents hydrogen, one or more optionally identical halogens, C1-C3 alkyl or hydroxyl optionally substituted with C1-C3 alkyl; n represents the whole numbers 1, 2 or 3.Type: ApplicationFiled: January 23, 2009Publication date: March 10, 2011Inventors: Andrey Alexandrovich Ivashchenko, Alexander Vasilievich Ivashchenko, Nikolay Filippovich Savchuk
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Patent number: 7902203Abstract: The present invention provides an HCV polymerase inhibiting compound having the formula (I) and a composition comprising a therapeutically effective amount of said compound. The present invention also provides a method for inhibiting hepatitis C virus (HCV) polymerase, a method for inhibiting HCV viral replication, and a method for treating or preventing HCV infection. Processes for making said compounds, and synthetic intermediates employed in said processes, are also provided.Type: GrantFiled: October 31, 2003Date of Patent: March 8, 2011Assignee: Abbott Laboratories, Inc.Inventors: John K. Pratt, David A. Betebenner, Pamela L. Donner, Brian E. Green, Dale J. Kempf, Keith F. McDaniel, Clarence J. Maring, Vincent S. Stoll, Rong Zhang, Hui-Ju Chen, William J. Flosi, Larry L. Klein, Allan C. Krueger, Dachun Liu, Darold L. Madigan, Laura M. Maymon, Todd W. Rockway, Kent D. Stewart, Ming C. Yeung, Qinghua Xie
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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: 20110046126Abstract: Novel methods and compositions for the prevention and treatment of all forms of atherosclerosis with 2,4-pyrimidinediamine compounds are described. Also disclosed is the coating of prosthetic devices, such as stents, with the compounds of the invention for the prevention and/or treatment of restenosis.Type: ApplicationFiled: February 20, 2009Publication date: February 24, 2011Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Esteban Masuda, Jochen Schmitz
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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: 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: 20110021493Abstract: This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly cancer.Type: ApplicationFiled: September 2, 2008Publication date: January 27, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Hartmut Schirok, Ying Li-Sommer, Michael Brands, Mario Lobell, Adrian Tersteegen, Herbert Himmel, Karl-Heinz Schlemmer, Dieter Lang, Kirsten Petersen, Matthias Renz, Dominik Mumberg, Jens Hoffman, Gerhard Siemeister, Ulf Bömer
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Publication number: 20110015214Abstract: The invention relates to novel tricyclic benzo[4,5]thieno-[2,3-d]pyrimidine-4-yl-amin derivatives, as well as their pharmaceutically acceptable salts. The subject of the invention too the process for producing the compounds and their use as a pharmaceutically active agent and as pharmaceutical compositions for prophylaxis and/or treatment of proliferative diseases such as cancer.Type: ApplicationFiled: February 19, 2008Publication date: January 20, 2011Inventors: Pèter Bánhegyi, Kéri György, Lászlõ Örfi, Zsolt Szekélyhidi, Frigyes Wáczek
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Publication number: 20110014204Abstract: The present invention relates to targets of loss of imprinting (LOI) affected IGF2 gene products in pre-malignant tissues, where methods of inhibiting those targets, including IGFR1, are disclosed to prevent tumor development in subjects at risk for developing colorectal cancer (CRC). The present invention also relates to methods of identifying increased risk in developing CRC in a subject, including methods of assessing the efficacy of a chemotherapeutic regimen. Further, the present invention relates to methods for identifying anti-neoplastic agents.Type: ApplicationFiled: December 7, 2007Publication date: January 20, 2011Inventors: Andrew P. Feinberg, Andre Levchenko, Dan L. Longo, Minoru S.H. Ko
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Publication number: 20110015201Abstract: The present disclosure provides for compounds, pharmaceutical preparations, kits and methods for the inhibition of the Hh pathway and the alleviation of cancer and developmental disorders associated with the Hh pathway.Type: ApplicationFiled: February 12, 2009Publication date: January 20, 2011Inventors: James K. Chen, Joel M. Hyman, Cory A. Ocasio
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Publication number: 20110009394Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials.Type: ApplicationFiled: January 7, 2009Publication date: January 13, 2011Applicant: Glaxo Group LimitedInventors: Pamela Brown, Steven Dabbs, Alan Joseph Hennessy
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Publication number: 20110003786Abstract: The present invention relates to compounds of formula I and salts thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.Type: ApplicationFiled: July 2, 2010Publication date: January 6, 2011Inventors: Robin Alec FAIRHURST, Marc GERSPACHER, Robert MAH
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Publication number: 20110003824Abstract: This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2-X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N?C, C(R3)?C, C(?O)—N, or C(?O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ?O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.Type: ApplicationFiled: September 16, 2010Publication date: January 6, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORDTEDInventors: Jean-Damien Charrier, Guy Brenchley
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Patent number: 7863285Abstract: 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: January 4, 2011Assignee: Incyte CorporationInventors: Chu-Biao Xue, Brian Metcalf, Anlai Wang, Changsheng Zheng, Ganfeng Cao, Ke Zhang
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Patent number: 7863284Abstract: Cyclopenta[g]quinazolines of the formula (I): —wherein: A is a group OR or NR0R1 wherein R0 and R1 are each independently hydrogen C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanalkyl, or R0 and R1 together with the intermediate N form a five- or six-membered heterocyclic ring; p is an integer in the range 1 to 4; R2 is hydrogen, C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl; Ar1 is phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, C1-4 alkyl and C1-4 alkoxy; and R3 is a group of one of the following formulae: -A1-Ar2-A2-Y1-A5-CON(R)CH(Y4)Y5-A8-X—Ar4 and pharmaceutically acceptable salts or esters thereof are of therapeutic value particularly in the treatment of cancer.Type: GrantFiled: February 27, 2007Date of Patent: January 4, 2011Assignee: BTG International LimitedInventors: Vassilios Bavetsias, Ann Lesley Jackman
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Publication number: 20100331351Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections.Type: ApplicationFiled: January 21, 2010Publication date: December 30, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: David Ginsburg, Hongmin Sun, Scott Larsen, Bryan Yestrepsky
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Publication number: 20100324029Abstract: The invention encompasses 2-[4-(imidazolyl)-phenyl]vinyl-heterocycle derivatives which selectively attenuate production of Abeta(1-42) and are useful in the treatment of Alzheimer's disease. Pharmaceutical compositions and methods of use are also encompassed.Type: ApplicationFiled: February 5, 2008Publication date: December 23, 2010Inventors: Christian Fischer, Benito Munoz, Alexey A. Rivkin
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Publication number: 20100323997Abstract: The present invention relates to a new use for compounds that inhibit phosphodiesterase 1 (PDE1), e.g., that inhibit PDE1-mediated suppression of the dopamine D1 receptor and/or progesterone signaling pathways, including, e.g., methods of treatment or prophylaxis for conditions which may be ameliorated by enhancing the progesterone signaling response, particularly female sexual dysfunction.Type: ApplicationFiled: December 5, 2007Publication date: December 23, 2010Applicant: INTRACELLULAR THERAPIES, INC.Inventors: Allen A. Fienberg, Sharon Mates, Lawrence P. Wennogle
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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: 7855214Abstract: The present invention relates to compounds useful as inhibitors of Tec family protein kinases. These compounds have the general formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, G, Cy1, and X are as defined 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.Type: GrantFiled: January 26, 2005Date of Patent: December 21, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Sanjay Patel, David Kay, Ronald Knegtel, Oliver Philps
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Publication number: 20100317677Abstract: The invention relates to methods and compositions for treating a microbial infection. In the present invention, RNase-L activity has been shown to play an integral role in innate immunity and for defense against invading microbes. The present invention is drawn to exploiting the role of RNase-L in innate immunity for methods of treating a microbial infection. The present invention is also drawn to exploiting the role of RNase-L in innate immunity for methods of treating an immune related disease or disorder.Type: ApplicationFiled: September 10, 2008Publication date: December 16, 2010Inventors: Bret A. Hassel, Alan S. Cross, Xiao-Ling Li, Tae Jin Kang
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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: 20100311683Abstract: The present invention provides methods of treating a patient having a higher risk myelodysplastic syndrome, which comprises administering to a patient having a higher risk myelodysplastic syndrome a therapeutically effective amount of a cytidine analog.Type: ApplicationFiled: November 3, 2008Publication date: December 9, 2010Inventors: C. L. Beach, Jay Thomas Backstrom
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Publication number: 20100311770Abstract: The present invention provides in vitro assays, e.g., FtsZ GTPase assays, and/or in vivo assays and methods of use thereof to identify particular compounds and combinations of compounds that affect microbial cell division. The invention further provides such compounds and compound combinations, including combinations that result in inhibition of cell survival or growth when present together at concentrations below their individual MICs. Certain of the compound combinations display synergism. Certain of the combinations include a compound that inhibits FtsZ GTPase activity and a compound that inhibits cell growth by a mechanism other than inhibition of FtsZ GTPase activity. The present invention further provides pharmaceutical compositions that have anti-microbial activity and methods of treating microbial infections.Type: ApplicationFiled: June 14, 2006Publication date: December 9, 2010Applicants: President and Fellows of Harvard College, Trustees of Tufts CollegeInventors: Marc Kirschner, Debrabata RayChaudhuri
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Publication number: 20100310477Abstract: A pharmaceutical composition comprising an anticholinergic and at least one additional active ingredient selected from among corticosteroids, dopamine agonistes, PDE-IV inhibitors, NK1-antagonists, endothelin antagonists, antihistamines, and EGFR-kinase inhibitors, processes for preparing them and their use in the treatment of respiratory diseases.Type: ApplicationFiled: August 13, 2010Publication date: December 9, 2010Applicant: Boehringer Ingelheim Pharma GmbH & Co. Kg.Inventors: Michel Pairet, Michael P. Pieper, Christopher John Montague Meade, Richard Reichl, Christel Schmelzer, Birgit Jung
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Publication number: 20100298287Abstract: There is provided a compound of the formula (I?): wherein X is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to -8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or ‘a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.Type: ApplicationFiled: January 21, 2009Publication date: November 25, 2010Inventors: Kazuyoshi Aso, Katsumi Kobayashi, Takafumi Takai, Takuto Kojima, Kazuyuki Tokumaru, Michiyo Mochizuki, Yasutaka Hoashi
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Publication number: 20100298297Abstract: This invention relates to compounds of Formula (I), wherein the variables are as disclosed in the specification, to pharmaceutical compositions containing them, to methods of making the compounds and pharmaceutical compositions, and to methods of using the compounds and pharmaceutical compositions for treating or preventing disorders, in particular cancer.Type: ApplicationFiled: March 20, 2007Publication date: November 25, 2010Applicant: BAYER HEALTHCARE AGInventors: Chengzhi Zhang, Kanwar Sidhu, Mario Lobell, Gaeten Ladouceur, Qian Zhao, Zheng Liu, Kristen Allegue, Chetan Darne, Jason Newcom
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Publication number: 20100298360Abstract: The present invention relates to compositions for use in the modulation of PDZ domain interactions with cognate ligands. Methods of assessing and characterizing PDZ domain interactions from various polypeptides also are provided.Type: ApplicationFiled: April 30, 2010Publication date: November 25, 2010Inventors: MICHAEL P. BELMARES, Peter S. Lu, Kenneth A. Mendoza
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Publication number: 20100292256Abstract: The invention relates to substituted 2-alkylamino-3-(arylsulfonyl)cycloalkyl[e or d]pyrazolo[1,5-a]pyrimidines, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions comprising the said compounds as active ingredients, and to novel medicaments and method for treatment and prophylaxis of various CNS diseases. 2-Alkylamino-3-arylsulfonylcycloalkyl[e]pyrazolo[1,5-a]pyrimidines of general formula 1 and 2-alkylamino-3-arylsulfonylcycloalkyl[d]pyrazolo[1,5-a]pyrimidines of general formula 2, wherein: R1 is hydrogen or C1-C3 alkyl; R2 is C1-C3 alkyl; R3 is hydrogen, one or more optionally identical halogen atoms, C1-C3 alkyl or hydroxyl group optionally substituted with C1-C3 alkyl; n is the whole numbers 1, 2 or 3.Type: ApplicationFiled: January 23, 2009Publication date: November 18, 2010Inventor: Andrey Alexandrovich IVASHCHENKO
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Publication number: 20100292257Abstract: The present invention discloses new uses of 2-[piperidinyl]methyl-2,3-dihydroimidazo[1,2-c]quinazolin-5(6H)-one in providing an analgesic effect in a patient, treating passive cutaneous anaphylaxis in a patient, and in eliciting a histamine H1 receptor antagonism effect in a patient to treat a disease or disorder, such as allergy.Type: ApplicationFiled: July 26, 2010Publication date: November 18, 2010Applicant: Medical and Pharmaceutical Industry Technology and Development CenterInventors: Feng-Nien KO, Yuan-Ling Ku
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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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Publication number: 20100279971Abstract: This invention relates to compounds of the formula X) or XI) (X) (XI) wherein: each —R1, —R2 and —R3 is independently -Q1, —OH or —H, where at least one of —R1, —R2 and —R3 is not —H or —OH; each —R4 and —R5 is independently -Q2 or —H; each -Q1 is independently selected from: —F, —Cl, —RA, —ORA, —SH, —SRA, where each —RA is independently selected from methyl and ethyl, which may substituted by one or more fluoro or chloro groups; and each -Q2 is selected from: —F, —Cl, —RB, —ORB, —SH, —SRB, where each —RB is independently selected from methyl and ethyl, which may substituted by one or more fluoro or chloro groups; which are useful in the treatment of melanoma.Type: ApplicationFiled: December 18, 2008Publication date: November 4, 2010Inventors: Jose Neptuno Rodriguez-Lopez, Luis Sanchez Del Campo Ferrer, Juan Cabezas-Herrera, Alberto Tarraga Tomas, Magali Maria Saez Ayala
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Publication number: 20100280026Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: February 26, 2010Publication date: November 4, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Juan-Miguel Jimenez, Jeremy Green, Huai Gao, Young-Choon Moon, Guy Brenchley, Ronald Knegtel, Francoise Pierard
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Publication number: 20100273817Abstract: Cyclopenta[g]quinazolines of the formula (I):—wherein: A is a group OR or NR0R1 wherein R0 and R1 are each independently hydrogen C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl, or R0 and R1 together with the intermediate N form a five- or six-membered heterocyclic ring; p is an integer in the range 1 to 4; R2 is hydrogen, C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl; Ar1 is phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, C1-4 alkyl and C1-4 alkoxy; and R3 is a group of one of the following formulae: -A1-Ar2-A2-Y1-A5-CON(R)CH(Y4) Y5-A8-X—Ar4 and pharmaceutically acceptable salts or esters thereof are of therapeutic value particularly in the treatment of cancer.Type: ApplicationFiled: June 29, 2010Publication date: October 28, 2010Applicant: BGT International LimitedInventors: Vassilios Bavetsias, Ann Lesley Jackman
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Pharmaceutical formulations comprising salts of a protein kinase inhibitor and methods of using same
Patent number: 7820684Abstract: The present invention relates to pharmaceutical formulations comprising the protein kinase inhibitor, MP470, and methods of using same in treating conditions involving undesirable cell proliferation, such as cancer.Type: GrantFiled: March 3, 2008Date of Patent: October 26, 2010Assignee: SuperGen, Inc.Inventors: David J. Bearss, Rajashree Joshi-Hangal, Xiao-Hui Liu, Pasit Phiasivongsa, Sanjeev G. Redkar, Hariprasad Vankayalapati -
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: 20100261714Abstract: Compounds of formula (I): wherein R1, R2, A1, A2, A3, A4, X and Y are as defined herein, are useful as inhibitors of HIV replication.Type: ApplicationFiled: April 8, 2010Publication date: October 14, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Claudio STURINO, Patrick DEROY, Martin DUPLESSIS, Paul J. EDWARDS, Anne-Marie FAUCHER, Teddy HALMOS, Clint JAMES, Jean-Eric LACOSTE, Eric MALENFANT, Joannie MINVILLE, Louis MORENCY, Sebastien MORIN, Martin TREMBLAY, Christiane YOAKIM
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Patent number: 7807687Abstract: The present invention relates to pyrido[3,2-h]quinazolines and/or 5,6-dihydro derivatives thereof, methods for their production and doped organic semiconductor material which use such quinazolines.Type: GrantFiled: March 12, 2008Date of Patent: October 5, 2010Assignee: Novaled AGInventors: Josef Salbeck, Manfred Kussler, Andrea Lux
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Patent number: 7807688Abstract: Tri-heterocyclic compound of formula (I) wherein each of W, X and Y is carbon or nitrogen; each of U and Z is CR2, NR13, nitrogen, oxygen, sulfur etc.; A ring is carbocyclic ring, heterocyclic ring; R1 is alkyl, alkenyl, alkynyl, NR4R5, OR6 etc.; R3 is carbocyclic ring, heterocyclic ring; and a pharmaceutically acceptable salt thereof, a process for the preparation thereof, a pharmaceutical comprising them as an active ingredient. A compound of formula (I) is useful, in order to possess corticotropin releasing factor receptor antagonistic activity, for the prevention and/or treatment of depression, anxiety, eating disorder, posttraumatic stress disorder, peptic ulcer, irritable bowl syndrome, Alzheimer's disease, drug addiction or alcohol dependence syndrome etc.Type: GrantFiled: September 2, 2008Date of Patent: October 5, 2010Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Nakai, Yoshifumi Kagamiishi
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Publication number: 20100249102Abstract: The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.Type: ApplicationFiled: April 6, 2010Publication date: September 30, 2010Applicant: ALANTOS PHARMACEUTICALS HOLDINGS, INC.Inventors: Christian Gege, Carine Chevrier, Matthias Schneider, Harald Bluhm, Matthias Hochgürtel, Hongbo Deng, Brian M. Gallagher, JR., Irving Sucholeiki, Arthur Taveras
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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: 20100239526Abstract: The present invention relates to substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: December 30, 2009Publication date: September 23, 2010Applicant: ArQule, Inc.Inventors: Syed M. Ali, Mark Ashwell, Chris Brassard, Audra Dalton, Anton Filikov, Jason Hill, Nivedita Namdev, Rocio Palma, Manish Tandon, David Vensel, Jianqiang Wang, Neil Westlund
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Publication number: 20100239525Abstract: The present invention relates to substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: December 30, 2009Publication date: September 23, 2010Applicant: ArQule, Inc.Inventors: Syed M. Ali, Mark A. Ashwell, Sudharshan Eathiraj, Eugene Kelleher, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Rocio Palma, Manish Tandon, David Vensel, Neil Westlund, Hui Wu, Rui-Yang Yang
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Patent number: 7799775Abstract: This invention provides pyrimidine derivatives represented by a formula, in the formula, ring A stands for carbocyclic group or heterocyclic group, X1 stands for hydrogen, lower alkyl, amino, etc., X2 stands for hydrogen or lower alkyl, Y stands for a direct bond or sulfur or nitrogen, n stands for an integer of 0-4, and Ar stands for a group of the following formula, or a salt thereof, which concurrently exhibit 5-HT1A agonistic activity and 5-HT3 antagonistic activity and are useful for therapy and treatments of diseases such as IBS. The invention furthermore provides a therapeutic method of IBS, characterized by having 5-HT1A agonistic activity and 5-HT3 antagonistic activity work simultaneously and cooperatively in vivo, which comprises either administering 5-HT3 antagonistic agent which concurrently exhibits 5-HT1A agonistic activity, or administering 5-HT1A agonistic agent and 5-HT3 antagonistic agent simultaneously, in sequence or at an interval.Type: GrantFiled: February 25, 2005Date of Patent: September 21, 2010Assignee: ASKA Pharmaceutical Co., Ltd.Inventors: Michitaka Sato, Teruaki Matsui, Akira Asagarasu, Hiroyuki Hayashi, Sei-ichi Araki, Satoru Tamaoki, Nobuyuki Takahashi, Yukinao Yamauchi, Yoshiko Yamamoto, Norio Yamamoto, Chisato Ogawa
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Publication number: 20100227853Abstract: Recombinant fission yeast cells and methods of using them are described, which provide for identification of chemical and biological inhibitors or activators of a target exogenous phosphodiesterase (PDE). The invention provides, in some aspects, compounds that inhibit cAMP PDE activity and compositions that include such compounds. The invention, in part, also includes methods of using cAMP PDE-inhibiting compounds in the treatment of cAMP PDE-associated diseases and/or disorders.Type: ApplicationFiled: April 17, 2009Publication date: September 9, 2010Applicant: Trustees of Boston CollegeInventors: Charles S. Hoffman, Frank Douglas Ivey, Arlene Wyman Petri
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Publication number: 20100215771Abstract: The present invention refers to the use of sodium channel blockers such as tetrodotoxin or saxitoxin, its analogues/derivatives as well as their acceptable salts, for the production of a medicament for the treatment of neuropathic pain resulting from chemotherapy.Type: ApplicationFiled: March 26, 2007Publication date: August 26, 2010Applicant: WEX PHARMACEUTICALS INC.Inventors: Helmut Heinrich Buschmann, Jose Miguel Vela Hernandez, Jose Manuel Baeyens