At 2-position And At 4- Or 6-position Patents (Class 544/323)
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Publication number: 20100261722Abstract: HIV replication inhibitors of formula R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2, R3, R7 and R8 are hydrogen; hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(?O)R10; C1-6alkyl optionally substituted with halo, cyano or —C(?O)R10; optionally substituted C1-6alkyl, C2-6alkenyl, or C2-6alkynyl; R4 and R9 are hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; formyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(?O)R10; cyano; —S(?O)rR10; —NH—S(?O)2R10; —NHC(?O)H; —C(?O)NHNH2; —NHC(?O)R10; Het; —Y-Het; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R5 is C2-6alkenyl or C2-6alkynyl both substituted with cyano, aminocarbonyl, mono- and di(C1-6alkyl)aminocarbonyl, aryl, pyridyl, thienyl, furanyl, or with one or two C1-6alkyloxy groups; Het; —C(?O)NR5aR5b; —CType: ApplicationFiled: December 28, 2007Publication date: October 14, 2010Inventors: Jerôme Emile Georges Guillemont, Céline Isabelle Mordant, Benoit Antoine Schmitt
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Publication number: 20100249092Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: December 29, 2009Publication date: September 30, 2010Applicant: Avila Therapeutics, Inc.Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
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Patent number: 7803939Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: GrantFiled: November 10, 2008Date of Patent: September 28, 2010Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Jeffrey Clough, Holger Keim, Someasekhar Bhamidipati, Catherine Sylvain, Hui Li
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Patent number: 7790736Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV inhibitors comprising Formula I: wherein the substituents are as described herein.Type: GrantFiled: August 12, 2004Date of Patent: September 7, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Jun Feng, Stephen L. Gwaltney, II, Stephen W. Kaldor, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
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Publication number: 20100221259Abstract: The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.Type: ApplicationFiled: May 10, 2010Publication date: September 2, 2010Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Masaya KOKUBO, Shiro SHIBAYAMA, Hideaki TADA, Tatsuya TANIHIRO
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Patent number: 7776869Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A1, A2, A3, A4, R1 and R2 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.Type: GrantFiled: October 14, 2005Date of Patent: August 17, 2010Assignee: Amgen Inc.Inventors: Stuart C. Chaffee, Brian K. Albrecht, Brian L. Hodous, Matthew W. Martin, David C. McGowan, Erin F. DiMauro, Gade Reddy, Victor J. Cee, Philip R. Olivieri, Anthony Reed, Karina Romero
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Publication number: 20100197918Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: April 16, 2010Publication date: August 5, 2010Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
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Publication number: 20100189796Abstract: This invention concerns polymorph I of TMC278, its use and preparation. It further concerns pharmaceutical formulations comprising this polymorph.Type: ApplicationFiled: July 11, 2008Publication date: July 29, 2010Inventor: Sigrid Carl Maria Stokbroekx
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Patent number: 7763632Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: January 12, 2009Date of Patent: July 27, 2010Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Christopher Michael Semko, Ying-zi Xu, Frank Stappenbeck, Jenifer Lea Smith, Kassandra Inez Rossiter, Juri Y. Fukuda, Andrei W. Konradi
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Publication number: 20100179164Abstract: 2,4-Pyrimidinediamine compounds represented by formula (I), methods for preparing the same and methods for treating an inflammatory disorder and for inhibiting the production of IL-23 and/or stimulating the production of IL-10 using the same:Type: ApplicationFiled: January 13, 2010Publication date: July 15, 2010Inventors: Hui Li, Esteban Masuda, Stephanie Yung, Taisei Kinoshita, Rongxian Ding, Rajinder Singh, Tarikere Gururaja, Donald G. Payan, Kin Tso
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Patent number: 7754714Abstract: The present disclosure provides 2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers.Type: GrantFiled: May 18, 2005Date of Patent: July 13, 2010Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Ankush Argade, Rajinder Singh, Sambaiah Thota, David Carroll, Kin Tso, Vanessa Taylor, John McLaughlin, Vadim M. V. Markovtsov
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Publication number: 20100173910Abstract: The present invention relates to triaminopyrimidine derivatives of formula (I) where Y, R3, W, R4a, R5a, R4b, R5b, n and m are variable. These compounds have CDC25 phosphatase-inhibiting activity and can therefore be used as drugs in diseases in which CDC25 phosphatases are involved. The invention also relates to pharmaceutical compositions containing said products and methods of using the drug.Type: ApplicationFiled: July 10, 2008Publication date: July 8, 2010Applicant: IPDRN PHSTMS D.S.S.Inventors: Anne-Marie Liberatore, Dominique Pons, Dennis Bigg, Grégorie Prevost, Marie-Christine Brezak Pannetier
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Publication number: 20100167934Abstract: Compounds of the formula (I) and their agrochemically compatible salts and their use in the field of crop protection are described.Type: ApplicationFiled: December 23, 2009Publication date: July 1, 2010Applicant: BAYER CROPSCIENCE AGInventors: Klemens MINN, Hansjöerg Dietrich, Jan Dittgen, Dieter Feucht, Isolde Häeuser-Hahn, Christopher Hugh Rosinger
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Publication number: 20100158921Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.Type: ApplicationFiled: December 22, 2009Publication date: June 24, 2010Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Somasekhar Bhamidipati, Hui Li, Rajinder Singh, Vanessa Taylor, Jeffrey Clough, Darren McMurtrie
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Patent number: 7741336Abstract: The present invention relates to a compound of the formula 1 wherein R1-R4 are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: July 29, 2008Date of Patent: June 22, 2010Assignee: Pfizer Inc.Inventors: John Charles Kath, Michael Joseph Luzzio
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Publication number: 20100152218Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.Type: ApplicationFiled: February 24, 2010Publication date: June 17, 2010Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Ankush Argade, Arvinder Sran, David Carroll, Jeffrey Clough, Kin Tso, Somasekhar Bhamidipati, Sambaiah Thota, Rajinder Singh, Vanessa Taylor, Hui Li, Esteban Masuda
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Publication number: 20100152182Abstract: Disclosed are pyrimidine derivatives of formula wherein R0, R1, R3 to R9, and Z have a signification as indicated in claim 1, which have interesting pharmaceutical properties.Type: ApplicationFiled: January 13, 2010Publication date: June 17, 2010Inventors: Rolf Baenteli, Marie Claude Bernhard, Peter Buehlmayer, Nigel Graham Cooke, Rudolf Duthaler, Klaus Hinterding, Gebhard Thoma, Maurice Van Eis, Anette Von Matt, Louis Walliser, Gerhard Zenke
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Publication number: 20100144722Abstract: Novel heterocyclic compounds, sstereoisomers thereof and/or pharmaceutically acceptable salts of formula (I) and its stereoisomers are provided. Additionally, methods of forming novel heterocyclic compounds, stereoisomers thereof and/or pharmaceutically acceptable salts of formula (I) and its stereoisomers are provided.Type: ApplicationFiled: September 3, 2009Publication date: June 10, 2010Applicant: Dr. Reddy's Laboratories Ltd.Inventors: Christopher W. Alexander, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti
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Publication number: 20100144706Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4, X and n are defined as in claim 1, which are suitable for the treatment of ailments characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: December 20, 2007Publication date: June 10, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan Karl Zahn, Guido Boehmelt, Ulrich Guertler, Andreas Mantoulidis, Andreas Schoop, Flavio Solca, Ulrike Tontsch-Grunt, Matthias Treu
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Publication number: 20100137275Abstract: The present invention relates to the novel triaminopyrimidine derivatives of formula (I) in which R1, R2, W, R3, R4, and R5 are variable groups. These products have a Cdc25-phosphatase-inhibiting activity. The invention also relates to a process for synthesizing these compounds and also to therapeutic compositions containing these products and to the use thereof as medicaments.Type: ApplicationFiled: April 30, 2008Publication date: June 3, 2010Applicant: IPSEN PHARMA S.A.S.Inventors: Grégorie Prevost, Anne-Marie Liberatore, Dennis Bigg, Dominique Pons
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Publication number: 20100137592Abstract: A process for the preparation of famciclovir a compound of Formula (I) and its intermediates.Type: ApplicationFiled: June 2, 2008Publication date: June 3, 2010Inventors: Asif Parvez Sayyed, Murali Krishna Ankaraju, Ravinder Reddy Vennapureddy, Shankar Rama, Ramesh Dandala, Sivakumaran Meenakshisunderam
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Publication number: 20100137311Abstract: The present invention relates to pyrimidine derivatives of the general formula I or salts thereof and their use.Type: ApplicationFiled: January 30, 2010Publication date: June 3, 2010Applicant: H. LUNDBECK A/SInventors: Nikolay Khanzhin, Daniel Rodriguez Greve, Mario Rottländer
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Patent number: 7723340Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.Type: GrantFiled: January 12, 2006Date of Patent: May 25, 2010Assignees: Signal Pharmaceuticals, LLC, Pharmacopeia Drug Discovery, Inc.Inventors: Ronald J. Albers, Leticia Ayala, Steven S. Clareen, Maria Mercedes Delgado Mederos, Robert Hilgraf, Sayee G. Hegde, Kevin Hughes, Adam Kois, Veronique Plantevin-Krenitsky, Meg McCarrick, Lisa Nadolny, Moorthy S. S. Palanki, Kiran Sahasrabudhe, John Sapienza, Yoshitaka Satoh, Marianne K. Sloss, Elise Sudbeck, Jonathan Wright, Ian Henderson, Andrew G. Cole
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Publication number: 20100113445Abstract: The present invention relates to dianilinopyrimidine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such dianilinopyrimidine derivatives are useful in the treatment of diseases associated with inappropriate Wee1 kinase activity.Type: ApplicationFiled: March 12, 2008Publication date: May 6, 2010Inventors: Felix Deanda, JR., David Harold Drewry, Paul Reid
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Patent number: 7709480Abstract: The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterized by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.Type: GrantFiled: December 21, 2005Date of Patent: May 4, 2010Assignees: Boehringer Ingelheim Pharma GmbH & Co. KG, Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Georg Dahmann, Frank Himmelsbach, Bernd Krist, Martin Lenter, Alexander Pautsch, Gisela Schapp, Martin Steegmaier, Helmut Wittneben, Anthony S. Prokopowicz, Walter Spevak, Andreas Schoop, Steffen Steurer
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Publication number: 20100105674Abstract: The present invention relates to dianilinopyrimidine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such dianilinopyrimidine derivatives are useful in the treatment of diseases associated with inappropriate Wee1 kinase activity.Type: ApplicationFiled: March 12, 2008Publication date: April 29, 2010Inventors: Felix Deanda Jr., David Harold Drewry, James Andrew Linn, Paul Reid
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Patent number: 7705148Abstract: Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).Type: GrantFiled: February 14, 2008Date of Patent: April 27, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Didier Philippe Robert Schils, Joannes Josephus Maria Willems, Bart Petrus Anna Maria Jozef Medaer, Elisabeth Therese Jeanne Pasquier, Paul Adriaan Jan Janssen, Jan Heeres, Ruben Gerardus George Leenders, Jérôme Emile Georges Guillemont
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Patent number: 7705009Abstract: Novel 4-aminopyrimidine-5-thione derivatives are disclosed. These compounds inhibit cyclin-dependent kinases, in particular Cdk1, Cdk2 and Cdk4. These compounds and their pharmaceutically acceptable salts have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. This invention is also directed to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors.Type: GrantFiled: October 16, 2006Date of Patent: April 27, 2010Assignee: Hoffman-La Roche Inc.Inventors: Qingjie Ding, Nan Jiang, Allen John Lovey
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Publication number: 20100081679Abstract: Use of diaminopyrimidines of the formula (I) in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and X1, X2 and A have the meanings given in the description, and also agrochemically active salts thereof as fungicides. Diaminopyrimidines of the formulae (Ia), (Ib), (Ic), (Id), (Ie), (If) in which R8a, R8b, R8c, R8d, R8e, R8f, R3b, R3c, R3e, X1b, X1c, X1e and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and X1, X2 and A have the meanings given in the description, and also agrochemically active salts thereof and their use for controlling unwanted microorganisms.Type: ApplicationFiled: February 26, 2008Publication date: April 1, 2010Applicant: Bayer CropScience AGInventors: Joerg Nico Greul, Oliver Gaertzen, Ralf Dunkel, Amos Mattes, Stefen Hillebrand, Ulrike Wachendorff-Neumann, Peter Dahmen, Arnd Voerste, Peter Schreier, Pierre-Yves Coqueron
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Publication number: 20100076000Abstract: This invention relates to pyrimidine derivatives of general formula I in which Q, R1, R2, R3, R4, R5, X, and m have the meanings that are contained in the description, as inhibitors of cyclin-dependent kinases and VEGF-receptor tyrosine kinases, their production as well as their use as medications for treatment of various diseases.Type: ApplicationFiled: October 12, 2004Publication date: March 25, 2010Inventors: Ulrich Lücking, Martin Krüger, Rolf Jautelat, Gerhard Siemeister
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Patent number: 7678804Abstract: Pyrimidine derivatives of formula (I) in which J and Y represent aromatic or heteroaromatic rings; R2, G, G?, and G? represent substituent groups and R2a represents H or halogen; L represents a linking group; and M represents CH or N. Pharmaceutical compositions containing these compounds, and methods of using these compounds in treatment of hyperproliferative diseases such as cancer are also disclosed and claimed.Type: GrantFiled: March 10, 2005Date of Patent: March 16, 2010Assignee: Bayer Healthcare LLCInventors: Julie A. Dixon, Dhanapalan Nagarathnam, Lei Zhang, Chunguang Wang, Lin Yi, Yuanwei Chen, Jianqing Chen, Brian R. Bear, Michael Brands, Alexander Hillisch, Donald Bierer, Ming Wang, Wenlang Fu, Martin F. Hentemann, Ann-Marie Bullion, Manoj Patel
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Publication number: 20100063077Abstract: The present invention provides (I) These compounds are useful in prevention and treatment of neurodegenerative disorders, such as Alzheimer's, Parkinson's and Huntington's as well as type II diabetes.Type: ApplicationFiled: April 27, 2007Publication date: March 11, 2010Applicant: SENEXIS LIMITEDInventors: David Christopher Horwell, David Ian Carter Scopes
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Patent number: 7674796Abstract: The present invention relates to a compound of the formula 1 wherein R1-R4 are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: March 31, 2008Date of Patent: March 9, 2010Assignee: Pfizer Inc.Inventors: John Charles Kath, Michael Joseph Luzzio
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Patent number: 7671063Abstract: Disclosed are pyrimidine derivatives of formula wherein R0, R1, R3 to R9, and Z have a signification as indicated in claim 1, which have interesting pharmaceutical properties.Type: GrantFiled: March 16, 2006Date of Patent: March 2, 2010Assignee: Novartis AGInventors: Rolf Baenteli, Marie Claude Bernhard, Peter Buehlmayer, Nigel Graham Cooke, Rudolf Duthaler, Klaus Hinterding, Gebhard Thoma, Maurice Van Eis, Anette Von Matt, Louis Walliser, Gerhard Zenke
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Publication number: 20100048891Abstract: Thiazolidinones of general formula (I) production thereof and use as inhibitors of polo like kinase (PLK) for the treatment of various diseases.Type: ApplicationFiled: April 29, 2009Publication date: February 25, 2010Inventors: Klause SCHULZE, Knut Eis, Lars Wortmann, Dirk Kosemund, Olaf Prien, Gerhard Siemeister, Holger Hess-Stumpp, Uwe Eberspaecher, Dominic E.A. Brittain, Imadul Islam
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Publication number: 20100041680Abstract: Compounds of formula I: I selectively inhibit production of Ab(1-42) and hence find use in treatment of Alzheimer's disease and other conditions associated with deposition of A(b) in the brain.Type: ApplicationFiled: February 8, 2008Publication date: February 18, 2010Inventor: Alexey A. Rivkin
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Patent number: 7662819Abstract: The present invention discloses pteridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like.Type: GrantFiled: October 5, 2007Date of Patent: February 16, 2010Assignee: Gilead Palo Alto, Inc.Inventors: Jeffrey Chisholm, Dmitry Koltun, Jeff Zablocki, Eric Parkhill, Andrey Glushkov, Natalya Vasilevich, Timur Zilbershtein, Andrew Cole, Tsung Lin, Ian Henderson
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Publication number: 20100035907Abstract: The disclosure relates to a compound of formula (I): wherein R1, R2, R3, R4, R5, A and Y are as defined in the specification, to compositions containing them, to processes for preparing them, and to their use in the treatment or prevention of conditions capable of being modulated by the inhibition of the activity of protein kinases.Type: ApplicationFiled: July 1, 2009Publication date: February 11, 2010Applicant: Sanofi-aventisInventors: Monsif BOUABOULA, Michael BOSCH, Pierre CASELLAS, Jean-Flaubert Nguefack, Bernard Tonnerre, Jean Wagnon
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Publication number: 20100029610Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: June 26, 2009Publication date: February 4, 2010Applicant: Avila Therapeutics, Inc.Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
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Patent number: 7655797Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: GrantFiled: August 27, 2008Date of Patent: February 2, 2010Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B Rossi
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Patent number: 7652051Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.Type: GrantFiled: August 24, 2005Date of Patent: January 26, 2010Assignee: TargeGen, Inc.Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
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Publication number: 20100016318Abstract: The present invention relates to a compound represented by the following formula: or a pharmaceutically acceptable salt thereof; wherein R1, R1? R2, R3, R4, R5, r and s are as defined herein. Compounds of the present invention are useful in the treatment of diseases associated with Aurora kinase activity such as cancer.Type: ApplicationFiled: January 25, 2008Publication date: January 21, 2010Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Jeffrey Michael Axten, Deborah L. Bryan, David Harold Drewry, Thomas H. Faitg, Timothy Francis Gallagher, Neil W. Johnson, Jiri Kasparec, Jeffrey M. Ralph, Domingos J. Silva
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Patent number: 7642351Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: GrantFiled: October 5, 2006Date of Patent: January 5, 2010Assignee: Rogel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
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Patent number: 7638522Abstract: The present invention relates to a pharmaceutical composition comprising as active ingredient the hydrochloric acid salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethyl-phenyl]amino]-2-pyrimidinyl]amino]benzonitrile and to processes for their preparation.Type: GrantFiled: September 2, 2005Date of Patent: December 29, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Jérôme Emile Georges Guillemont, Paul Theodoor Agnes Stevens, Alex Herman Copmans, Jozef Peeters, Alfred Elisabeth Stappers, Roger Petrus Gerebern Vandecruys, Paul Stoffels
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Publication number: 20090318407Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: ApplicationFiled: April 16, 2009Publication date: December 24, 2009Applicant: Portola Pharmaceuticals, Inc.Inventors: Shawn M. Bauer, Zhaozhong J. Jia, Yonghong Song, Qing Xu, Mukund Mehrota, Jack W. Rose, Wolin Huang, Chandrasekar Venkataramani, Anjali Pandey
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Publication number: 20090318687Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: ApplicationFiled: June 18, 2009Publication date: December 24, 2009Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
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Publication number: 20090286794Abstract: The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).Type: ApplicationFiled: July 27, 2009Publication date: November 19, 2009Applicant: BTG International Ltd.Inventors: Masaki Meguro, Tomiichiro Oda, Yasuhiro Nakagami, Shinji Marumoto, Kazuo Koyama, Isao Kaneko
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Patent number: 7615553Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: March 11, 2003Date of Patent: November 10, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Kristof Van Emelen, Marc Gustaaf Celine Verdonck, Sven Franciscus Anna Van Brandt, Patrick René Angibaud, Lieven Meerpoel, Alexey Borisovich Dyatkin
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Patent number: 7601714Abstract: Disclosed are novel compounds of formula (I): wherein X, Y, R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: July 6, 2005Date of Patent: October 13, 2009Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Antonio J. M. Barbosa, Jr., Steven Richard Brunette, Eugene Richard Hickey, Jin Mi Kim, Michael David Lawlor, René Marc Lemieux, Bryan McKibben, Matt Aaron Tschantz, Hui Yu
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Patent number: 7598260Abstract: This invention relates to pyrimidine derivatives of general formula I in which R1, R2, X, A and B have the meanings that are contained in the description, as inhibitors of the cyclin-dependent kinases, their production as well as their use as medications for treating various diseases.Type: GrantFiled: June 26, 2007Date of Patent: October 6, 2009Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Thomas Brumby, Rolf Jautelat, Olaf Prien, Martina Schäfer, Gerhard Siemeister, Ulrich Lücking, Christoph Huwe