Ring Chalcogen In The Bicyclo Ring System Patents (Class 514/260.1)
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Publication number: 20110275645Abstract: The invention provides compounds that inhibit protein kinases, prodrugs of the compounds, intermediates and methods of synthesizing the compounds and/or prodrugs, pharmaceutical compositions including the compounds and/or prodrugs and methods of using the compounds and/or prodrugs in a variety of contexts, including, for example, in the treatment and/or prevention of various diseases that are responsive to protein kinase inhibition and/or that are mediated, at least in part, by inappropriate kinase activity.Type: ApplicationFiled: May 5, 2010Publication date: November 10, 2011Inventors: Renee Desai, Ketan Desai
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Publication number: 20110269772Abstract: Axl kinase inhibitory compounds are disclosed, as well as compositions and methods of using the same in the treatment of cancer and other conditions mediated by and/or associated with Axl kinase.Type: ApplicationFiled: July 14, 2011Publication date: November 3, 2011Applicant: SUPERGEN, INC.Inventors: David J. BEARSS, Hariprasad VANKAYALAPATI, Yong XU
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Publication number: 20110263532Abstract: The present invention provides novel analogs and derivatives of halofuginone. The invention also provides pharmaceutical and cosmetic compositions thereof and methods for using halofuginone analogs in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, ischemic damage, transplant and implant rejection, neurodegenerative diseases, and cosmetic applications.Type: ApplicationFiled: August 11, 2009Publication date: October 27, 2011Applicant: President and Fellows of Harvard CollegeInventors: Tracy Keller, Ralph Mazitschek, Malcolm Whitman, Jinbo Lee
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Publication number: 20110263605Abstract: The disclosure provides compounds of formula I, including Ia, Ib, Ic, or Id, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic ?7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.Type: ApplicationFiled: October 19, 2010Publication date: October 27, 2011Inventors: Ivar M. McDonald, Robert A. Mate, James H. Cook, II, Dalton King, Richard E. Olson, Nenghui Wang, Christiana I. Iwuagwu, F. Christopher Zusi, Matthew D. Hill, Haiquan Fang, John E. Macor
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Publication number: 20110257201Abstract: An agent comprising, as an active ingredient, a xanthine oxidase inhibitor such as 2-[3-cyano-4-(4-fluorophenoxy)phenyl]-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-[3-cyano-4-(4-fluorophenoxy)phenyl]thiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-(3-cyano-4-phenoxyphenyl)thiazolo[5,4-d]pyrimidine, TMX-67, and FYX-051, which can be used as an agent for overcoming anti-cancer agent resistance.Type: ApplicationFiled: June 27, 2011Publication date: October 20, 2011Applicant: NIPPON CHEMIPHAR CO., LTD.Inventors: Masuharu HIRANO, Tomio YAMAKAWA, Toshihisa ISHIKAWA, Hikaru SAITO
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Publication number: 20110251216Abstract: The present invention relates to therapeutic targets for cancer. In particular, the present invention relates to small molecules and nucleic acids that target EZH2 expression in cancer (e.g., prostate cancer, breast cancer, other solid tumors, multiple myeloma).Type: ApplicationFiled: February 10, 2011Publication date: October 13, 2011Applicant: The Regents of The University of MichiganInventors: Arul M. Chinnaiyan, Sooryanaryana Lnu, Qi Cao
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Patent number: 8030307Abstract: The present invention relates to compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising a compound of the present invention.Type: GrantFiled: November 26, 2008Date of Patent: October 4, 2011Assignee: Enanta Pharmaceuticals, Inc.Inventors: Joel D. Moore, Yat Sun Or, Zhe Wang
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Publication number: 20110230502Abstract: The present invention provides screening methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors as well as modifiers capable of modulating chemosensory receptors and their ligands.Type: ApplicationFiled: March 18, 2011Publication date: September 22, 2011Applicant: SENOMYX, INC.Inventors: Catherine TACHDJIAN, Xiao-Qing Tang, Sara Werner, Marketa Rinnova, Qing Chen, Guy Servant, Xiaodong Li, Feng Zhang, Haitian Liu, Albert Zlotnik, Mark Zoller, Boris Klebansky, Richard Fine, Xinshan Kang
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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: 8022076Abstract: This invention relates to novel compound of formula (I) or pharmaceutically acceptable salts thereof. The invention is also directed to the uses of compounds having formula (I) in the treatment or prevention of diseases or disorders which requires potassium channel inhibition to an animal, mammal or human in need thereof. The invention is also directed to the use of compounds having formula (I) in the treatment or prevention of arrhythmia to an animal, mammal or human in need thereof.Type: GrantFiled: June 10, 2004Date of Patent: September 20, 2011Assignee: Xention LimitedInventors: John Ford, Nicholas John Palmer, John Frederick Atherall, David John Madge, Brad Sherborne, Mark Bushfield, Edward Benedict Stevens
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Publication number: 20110217311Abstract: The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.Type: ApplicationFiled: February 25, 2011Publication date: September 8, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thorsten LEHMANN-LINTZ, Armin HECKEL, Joerg KLEY, Elke LANGKOPF, Nobert REDEMANN, Achim SAUER, Leo THOMAS, Dieter WIEDENMAYER, Matthias AUSTEN, John DANILEWICZ, Martin SCHNEIDER, Kay SCHREITER, Phillip BLACK, Wesley BLACKABY, Ian LINNEY
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Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
Patent number: 8012965Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: December 28, 2007Date of Patent: September 6, 2011Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak -
Patent number: 8012973Abstract: Adenosine A2A receptor antagonists are useful for the preparation of medicaments against atrial fibrillation in mammals, including humans. It has been found that the adenosine A2A receptor is present in human atrial cardiomyocytes and participates in the pathological mechanisms underlying atrial fibrillation. An advantage of using A2A antagonists over other agents known in the art is that the A2A antagonists specifically target patients with atrial fibrillation.Type: GrantFiled: October 10, 2006Date of Patent: September 6, 2011Assignee: Proyecto de Biomedicina Cima S.L.Inventors: Rafael Franco Fernández, Franciso Ciruela Alférez, Carmen Lluís Biset, Christa Müller, Joan Cinca Cuscullola, Leif Hove-Madsen
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Publication number: 20110212974Abstract: The present invention concerns a method for identifying a compound which inhibits the activation of RAC GTPase by DOCK5 protein comprising the steps of (i) coexpressing the DOCK5 and the RAC proteins in a cell, wherein said DOCK5 protein induces the conversion of inactive RAC, which inactive RAC is bound to GDP, to active RAC, which active RAC is bound to GTP, (ii) contacting or not said cell with said compound, (iii) determining the conversion of inactive RAC to active RAC in the presence or absence of said compound, and (iv) selecting the compound inhibiting the conversion of inactive RAC to active RAC. Said compound is useful for treating disease-associated bone loss.Type: ApplicationFiled: August 18, 2009Publication date: September 1, 2011Inventor: Anne Blangy
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Publication number: 20110212102Abstract: The present invention relates to novel pharmaceutical compositions comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.Type: ApplicationFiled: February 25, 2011Publication date: September 1, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thorsten LEHMANN-LINTZ, Joerg KLEY, Norbert REDEMANN, Achim SAUER, Leo THOMAS, Dieter WIEDENMAYER, Matthias AUSTEN, John DANILEWICZ, Martin SCHNEIDER, Kay SCHREITER, Phillip BLACK, Wesley BLACKABY, Ian LINNEY
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Publication number: 20110212103Abstract: The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.Type: ApplicationFiled: February 25, 2011Publication date: September 1, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Armin HECKEL, Frank HIMMELSBACH, Joerg KLEY, Thorsten LEHMANN-LINTZ, Norbert REDEMANN, Achim SAUER, Leo THOMAS, Dieter WIEDENMAYER, Phillip BLACK, Wesley BLACKABY, Ian LINNEY, Matthias AUSTEN, John DANILEWICZ, Martin SCHNEIDER, Kay SCHREITER
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Publication number: 20110212937Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.Type: ApplicationFiled: July 28, 2010Publication date: September 1, 2011Inventors: Kenneth M. Boy, Jason M. Guernon, John E. Macor, Richard E. Olson, Jianliang Shi, Lorin A. Thompson, III, Yong-Jin Wu, Li Xu, Yunhui Zhang, Dmitry S. Zuev
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Patent number: 8003656Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: GrantFiled: August 22, 2007Date of Patent: August 23, 2011Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
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Publication number: 20110201628Abstract: The present invention relates to compounds of Formula (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer.Type: ApplicationFiled: September 29, 2009Publication date: August 18, 2011Inventors: Claudio Edmundo Chuaqui, Shan Huang, Stephanos Ioannidis, Jie Shi, Mei Su, Qibin Su
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Publication number: 20110190241Abstract: Drug candidates for inhibition of HIV-I replication can target Src family kinases (SFK), such as Hck, that interact with Nef protein of the virus. Compounds characterized by such inhibitory activity were identified via an assay for kinase activity of an SFK in a Nef:SFK complex. Illustrative of inhibitors identified using the kinase assay are various 2,3-diaminoquinaxolines and furo[2,3-d]pyrimidines. The inventive inhibitors were found to arrest HIV-I viral replication in vitro.Type: ApplicationFiled: May 14, 2009Publication date: August 4, 2011Inventors: Lori Emert-Sedlak, Toshiaki Kodama, Billy W. Day, Weixiang Dai, Ronald P. Trible, Thomas E. Smithgall
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Patent number: 7989433Abstract: The present invention provides compounds having the following Formula IA and IB, which are useful as MCHR1 antagonists, and includes prodrugs and pharmaceutically acceptable salts thereof:Type: GrantFiled: May 28, 2009Date of Patent: August 2, 2011Assignee: Bristol-Myers Squibb CompanyInventors: William N. Washburn, Pratik Devasthale, Jeffrey A. Robl
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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: 20110178070Abstract: The invention relates to PI3K/mTOR inhibiting compounds consisting of the formula: wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: June 23, 2009Publication date: July 21, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Xianchang Gong, Bohan Jin, Massaki Hirose, Feng Zhou, Qing Dong
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Patent number: 7977342Abstract: The present invention relates to the use of bi-cyclic pyrimidines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to processes for preparation of such pharmaceutical compositions. The present invention also concerns combinations of the present bi-cyclic pyrimidines with other anti-HCV agents.Type: GrantFiled: March 9, 2007Date of Patent: July 12, 2011Assignee: Tibotec-Virco Virology BVBAInventors: Kenneth Alan Simmen, Tse-I Lin, Oliver Lenz, Dominique Louis Nestor Ghislain Surleraux, Pierre Jean-Marie Bernard Raboisson
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Publication number: 20110166163Abstract: The present application relates to novel substituted furopyrimidine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular diseases.Type: ApplicationFiled: June 3, 2008Publication date: July 7, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Thomas Lampe, Raimund Kast, Mario Jeske, Friederike Stoll, Joachim Schuhmacher, Eva-Maria Becker, Hartmut Beck
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Publication number: 20110166121Abstract: The present invention relates to a fused heterocyclic compound having the Formula 1, which is useful as a platelet aggregation inhibitor, a method for preparing the same, and a pharmaceutical composition for inhibiting platelet aggregation comprising the same.Type: ApplicationFiled: September 8, 2009Publication date: July 7, 2011Applicant: LG LIFE SCIENCES LTD.Inventors: Chang Seok Lee, Tae Hee Lee, Sook Kyung Yoon, Jeung Soon Choi, Yong Jin Jang, Sung Wook Kim, Hye Kyung Chang, Mi Jeong Park, Tae Hun Kim, Young Ha Ahn, Hee Dong Park, Hyun Jung Park, Dong Chul Lim, Joo Youn Lee, Sung Hack Lee, Wan Su Park, Yeong Soo Oh
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Publication number: 20110165118Abstract: The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: November 13, 2008Publication date: July 7, 2011Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
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Publication number: 20110165183Abstract: The invention provides a compound of formula (I): wherein W is a bicyclic heteroaromatic group; or a salt thereof. The compounds and salts thereof have beneficial therapeutic properties (e.g. immunosuppressant properties).Type: ApplicationFiled: July 31, 2009Publication date: July 7, 2011Applicant: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, Pravin L. Kotian, V. Satish Kumar
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Publication number: 20110166164Abstract: The present disclosure relates to thiazolo[5,4-d]pyrimidines and their use as agrochemicals and animal health products.Type: ApplicationFiled: January 6, 2011Publication date: July 7, 2011Inventors: William K. Brewster, Carla J. R. Klittich, Brent J. Rieder, Thomas L. Siddall, Chenglin Yao
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Publication number: 20110166116Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R1, R2, R3, n, p, q, and Ar are as defined herein, including stereoisomers, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.Type: ApplicationFiled: June 23, 2010Publication date: July 7, 2011Applicants: BOEHRINGER INGELHEIM INTERNATIONAL GMBH, NEUROCRINE BIOSCIENCES, INC.Inventors: Brian DYCK, Joe A. TRAN, Junko TAMIYA, Florence JOVIC, Troy VICKERS, Chen CHEN, Nicole HARRIOTT, Timothy COON, Neil J. ASHWEEK
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Publication number: 20110160207Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.Type: ApplicationFiled: March 2, 2011Publication date: June 30, 2011Inventors: Stephen T. Wrobleski, Jagabandhu Das, T.G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
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Patent number: 7968536Abstract: The present invention provides compounds useful as inhibitors of protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: GrantFiled: June 30, 2008Date of Patent: June 28, 2011Assignees: Millennium Pharmaceuticals, Inc., Sunesis Pharmaceuticals, Inc.Inventors: Jennifer Cossrow, Bing Guan, Alexey Ishchenko, John Howard Jones, Gnanasambandam Kumaravel, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin
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Publication number: 20110152242Abstract: A compound of formula (I), wherein W is formula (1); A is a benzene ring, a fÊve-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S atom is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; n is zero, one, two or three; when n is zero or one, V is CH2; when n is two or three, V is CH2, O or NR5; when V is CH2, the bond formed by V and an adjacent carbon ring atom is optionally fused to a phenyl ring, a five-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; the ring being optionally substituted by one or more R1 groups; and R7 and R8 are independently hydrogen, hydroxy, halogen or C1-4alkyl; Z is a phenyl ring, a five-membered heteroaromatic ring containing one, two, three or four heteroatoms independently chosen from O, N or S, atType: ApplicationFiled: March 21, 2006Publication date: June 23, 2011Inventors: Tracy Bayliss, Rebecca Elizabeth Brown, Gregory John Hollingworth, Brian A. Jones, Christopher Richard Moyes, Lauren Rogers
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Publication number: 20110152259Abstract: The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, esters, and tautomers thereof, wherein: Q is selected from the group consisting of: and L is selected from the group consisting of: pharmaceutically compositions comprising one or more compounds of formula (I), and methods of using the compounds of formula (I).Type: ApplicationFiled: February 24, 2011Publication date: June 23, 2011Inventors: Anandan Palani, Jing Su, Dong Xiao, Xianhai Huang, Ashwin U. Rao, Xiao Chen, Haiqun Tang, Jun Qin, Ying R. Huang, Robert G. Aslanian, Brain A. McKittrick, Syliva J. Degrado
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Patent number: 7960395Abstract: There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) wherein R1, R2, R3, R4 and n are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.Type: GrantFiled: September 27, 2007Date of Patent: June 14, 2011Assignee: AstraZeneca ABInventors: Rolf Johansson, Sofia Karlström, Annika Kers, Gunnar Nordvall, Tobias Rein, Can Slivo
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Publication number: 20110136834Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.Type: ApplicationFiled: February 11, 2011Publication date: June 9, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Stephen Critchley, Thomas G. Gant, Steven P. Langston, Edward J. Olhava, Stephane Peluso
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Publication number: 20110136813Abstract: The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.Type: ApplicationFiled: May 27, 2009Publication date: June 9, 2011Inventors: Lawrence Lum, Michael G. Roth, Baozhi Chen, Chuo Chen, Michael E. Dodge, Wei Tang
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Publication number: 20110124665Abstract: The present application relates to novel, cyclically substituted furopyrimidine derivatives, methods for their production, their use for the treatment and/or prophylaxis of diseases and their use for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.Type: ApplicationFiled: December 8, 2006Publication date: May 26, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Thomas Lampe, Eva-Maria Becker, Raimund Kast, Hartmut Beck, Mario Jeske, Joachim Schuhmacher, Friederike Stoll, Martina Klein, Metin Akbaba, Andreas Knorr, Johannes-Peter Stasch, Lars Bärfacker, Alexander Hillisch, Gunter Karig, Mark Meininghaus, Karl-Heinz Schlemmer, Rudolf Schohe-Loop
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Patent number: 7947690Abstract: The present invention provides a condensed pyrimidine compound represented by formula (I) or pharmaceutically acceptable salt thereof: where A represents a ring where at least one carbon atom within said ring is optionally substituted with one or more groups selected from the group consisting of lower alkyl, —O-(lower alkyl), halogen atom, carboxyl, —CO2-(lower alkyl), and carbamoyl, R1 represents: (1) phenyl substituted with at least three halogen atoms, which may have at least one additional substituent, or (2) cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl, each of which is optionally substituted; and R2 represents a group represented by formula (II) or an optionally substituted cyclic amino: wherein R21 and R22 may be identical or different and each represents —H, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, phenyl, heteroaryl, non-aromatic heterocyclyl, or —O-(lower alkyl), each of which is optionally substituted.Type: GrantFiled: October 17, 2005Date of Patent: May 24, 2011Assignee: Astellas Pharma Inc.Inventors: Yasuhiro Yonetoku, Kenji Negoro, Kenichi Onda, Masahiko Hayakawa, Daisuke Sasuga, Takahiro Nigawara, Kazuhiko Iikubo, Hiroyuki Moritomo, Shigeru Yoshida, Takahide Ohishi
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Patent number: 7947692Abstract: There are presented compounds of the formula or a pharmaceutically acceptable salt thereof, which are active adenosine A2B receptor antagonists and useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea.Type: GrantFiled: May 11, 2007Date of Patent: May 24, 2011Assignee: Hoffmann-La Roche Inc.Inventors: John A. Brinkman, Adrian Wai-Hing Cheung, Fariborz Firooznia, Kevin Richard Guertin, Nicholas Marcopulos, Lida Qi, Jagdish Kumar Racha, Ramakanth Sarabu, Jenny Tan, Jefferson Wright Tilley
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Patent number: 7947691Abstract: Acrylic n-hydroxy imides and their use in pharmaceutical compositions and in the inhibition of flap endonuclease are disclosed.Type: GrantFiled: July 20, 2005Date of Patent: May 24, 2011Assignee: Athersys, Inc.Inventors: Lawrence N. Tumey, Youssef Bennani, Bayard Huck, David C. Bom
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Patent number: 7947693Abstract: There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.Type: GrantFiled: April 3, 2006Date of Patent: May 24, 2011Assignee: AstraZeneca ABInventors: Gunnar Nordvall, Colin Ray, Tobias Rein, Daniel Sohn
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Publication number: 20110118284Abstract: Compounds of formula (I) are A2B receptor antagonists, wherein R1 is optionally substituted aryl or an optionally substituted 5- or 6-membered heteroaryl ring; R2 and R3 are independently selected from hydrogen, C1-C6 alkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl-(C1-C6)-alkyl, aryl-(C1-C6)-alkyl optionally substituted in the ring part thereof, a 5- or 6-membered monocyclic heterocyclic group optionally linked via a C1-C6 alkylene chain and optionally substituted in the ring part thereof, benzimidazol-2-yl-methyl, pyrid-3-yl-carbonyl, or (1-methyl-piperidin-4-yl)-carbonyl-methyl; or R2 and R3 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R4 is C1-C3 alkyl, C2-C3 alkenyl, —N(—R5)—R6, or optionally substituted heteroarylmethylamino; and R5 and R6 are independently selected from hydrogen or C1-C3 alkyl; or R5 and R6 taken together with the nitrogen atom to which they are attached form an optionally substituted 4- to 6-membered saturated ring.Type: ApplicationFiled: September 19, 2008Publication date: May 19, 2011Applicant: VERNALIS (R&D) LTD.Inventors: Allan Jordan, Simon Bedford, Klenke Burkhard, Ian Yule, Karine Poullennec
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Publication number: 20110105537Abstract: There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) wherein R1, R2, R3, R4 and n are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.Type: ApplicationFiled: January 19, 2011Publication date: May 5, 2011Applicant: AstraZeneca ABInventors: Rolf Johansson, Sofia Karlström, Annika Kers, Gunnar Nordvall, Tobias Rein, Can Slivo
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Publication number: 20110104109Abstract: The present invention relates to Tetracyclic Indole Derivatives, compositions comprising at least one Tetracyclic Indole Derivative, and methods of using the Tetracyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: May 5, 2011Inventors: Frank Bennett, Qingbei Zeng, Srikanth Venkatraman, Mousumi Sannigrahi, Kevin X. Chen, Gopinadhan N. Anilkumar, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
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Publication number: 20110105465Abstract: Provided are: an agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), which comprises a compound having adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof as an active ingredient; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance or constipation; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance; and the like.Type: ApplicationFiled: May 29, 2009Publication date: May 5, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Jun Ouchi, Shunji Kunori, Yozo Kojima, Katsumi Shinoda, Katsutoshi Sasaki, Shiro Shirakura
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Publication number: 20110092519Abstract: There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.Type: ApplicationFiled: December 28, 2010Publication date: April 21, 2011Applicant: AstraZeneca ABInventors: Gunnar Nordvall, Colin Ray, Tobias Rein, Daniel Sohn
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Publication number: 20110092499Abstract: The present invention relates to N-containing heterocyclic compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2, JAK3 or TYK2 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.Type: ApplicationFiled: November 14, 2008Publication date: April 21, 2011Applicant: YM BIOSCIENCES AUSTRALIA PTY LTDInventors: David Gerard Bourke, Christopher John Burns, Antony Nicholas Cuzzupe, John Thomas Feutrill, Marcel Robert Kling, Tracy Leah Nero
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Patent number: 7928111Abstract: The present invention provides compounds including substituted thienopyrimidinone derivatives of Formula (IIc) as ligands for modulating chemosensory receptors: These compounds are useful as sweet taste enhancers in comestible or medicinal compositions. The present invention also provides screening methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors as well as modifiers capable of modulating chemosensory receptors and their ligands.Type: GrantFiled: August 8, 2007Date of Patent: April 19, 2011Assignee: Senomyx, Inc.Inventors: Catherine Tachdjian, Xiao-Qing Tang, Sara Werner, Marketa Rinnova, Qing Chen, Guy Servant, Xiaodong Li, Feng Zhang, Haitian Liu, Albert Zlotnik, Mark Zoller, Boris Klebansky, Richard Fine, Xinshan Kang
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Publication number: 20110086865Abstract: The invention relates to molecules ANT-ligands having a substituted nitrogeneous heterocycle A wherein —A is a substituted pyrazinone of formula I wherein R1 is —(CH2)n —CO—OH; —(CH2)n —CO—OR; —(CH2)n —CO—NHR; —(CH2)n —CO—N(R, R?); —(CH2)n —OH; —(CH2)n —OR; —(CH2)n —OAr; —(CH2)n —C(R,R?) —(CH2)n —OH, R and R?, in the above radicals, being identical or different and representing H or a C1-C12 alkyl or cycloalkyl radical; and Ar is a phenyl or Het., Het.Type: ApplicationFiled: May 29, 2009Publication date: April 14, 2011Applicant: MITOLOGICSInventors: Annie Borgne-Sanchez, Etienne Jacotot, Catherine Brenner