Nitrogen Bonded Directly To The 1,3-diazine At 2-position Patents (Class 514/272)
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Publication number: 20100183606Abstract: The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.Type: ApplicationFiled: March 19, 2010Publication date: July 22, 2010Inventors: ROBERT M BORZILLERI, Lyndon A.M. Cornelius, Robert J. Schmidt, Gretchen M. Schroeder, Kyoung S. Kim
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Publication number: 20100184717Abstract: The invention relates generally to treatment of muscle pain and/or fatigue and to methods of treatment of side effects of statin therapy which involve the administration of uridine, biological precursors or derivatives or uridine or salts, esters, tautomers or analogues thereof, which are collectively referred to as uridine related compounds. The invention is also directed to compositions, uses and combination packs or kits related to the treatment method.Type: ApplicationFiled: January 22, 2010Publication date: July 22, 2010Applicant: MAGRAL PTY LTD.Inventor: Anthony William Linnane
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Publication number: 20100184787Abstract: The invention relates to the hetaryl-substituted guanidine compounds of general formula (I), enantiomeres, diastereomeres and/or tautomeres thereof, in addition to the pharmaceutically acceptable salts thereof and the prodrugs of the known compounds. The invention also relates to the use of said hetaryl-substituted guanidine compounds as binding partners for 5-HT5-receptors for treating and/or for the prophylaxis of illnesses which are modulated by a 5-HT5-receptor activity, in particular, for treating and/or for the prophylaxis of neurodegenerative and neuropsychiatric disorders, and signs, symptoms and dysfunctions associated with said disorders.Type: ApplicationFiled: August 23, 2006Publication date: July 22, 2010Inventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Charles W. Hutchins, Francisco Javier Garcia-Ladona, Wolfgang Wernet
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Publication number: 20100172970Abstract: The present invention is concerned with pharmaceutical compositions of antiviral compounds which can be administered to a mammal, in particular a human, suffering from a viral infection. These compositions comprise particles obtainable by melt-extruding a mixture comprising one or more antiviral compounds and one or more appropriate water-soluble polymers and subsequently milling said melt-extruded mixture.Type: ApplicationFiled: March 16, 2010Publication date: July 8, 2010Inventors: Geert VERRECK, Lieven Baert
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Patent number: 7745454Abstract: Disclosed are certain alpha amino acid 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 mammalian patient, e.g., human, 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: September 7, 2004Date of Patent: June 29, 2010Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Farouz, Christopher M. Semko, Ying-Zi Xu
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Publication number: 20100152214Abstract: This disclosure relates to novel HIV integrase inhibitors their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating HIV infections.Type: ApplicationFiled: February 25, 2010Publication date: June 17, 2010Applicant: Concert Pharmaceuticals Inc.Inventor: Scott L. Harbeson
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Publication number: 20100144732Abstract: The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein Q, X, Y, Z, R1, R2, R4, m and n are as defined herein.Type: ApplicationFiled: December 13, 2007Publication date: June 10, 2010Inventors: Elaine B. Krueger, Thomas E. Rawson, Daniel J. Burdick, Jun Liang, Bing-Yan Zhu
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Publication number: 20100144718Abstract: The invention provides a method for the treatment of H4R modulated diseases and/or conditions comprising administering to the subject an effective amount of a H4R agonist. The invention also provides a method for treating COPD comprising administering to the subject an effective amount of a H4R agonist, a H1R antagonist and an anticholinergic drug. Further, the invention provides a pharmaceutical formulation comprising a H4R agonist, a second active agent and a pharmaceutically acceptable carrier.Type: ApplicationFiled: June 17, 2009Publication date: June 10, 2010Inventors: Michalis Nicolaou, Emile Loria, Gaetan Terrasse, Yves Trehin
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Patent number: 7728131Abstract: The present invention is directed to an amide derivative having excellent BCR-ABL tyrosine kinase inhibitory activity, or a salt thereof. The present invention provides an amide derivative represented by the following general formula (1): [Chemical 23] (wherein R1 represents —CH2—R11, etc.; R2 represents alkyl, halogen, haloalkyl, etc.; R3 represents hydrogen, etc.; Het1 represents a group of the formula [6] as above, etc.; and Het2 represents pyrimidinyl, etc.), or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention is useful as a BCR-ABL tyrosine kinase inhibitor.Type: GrantFiled: December 27, 2004Date of Patent: June 1, 2010Assignee: Nippon Shinyaku Co., Ltd.Inventors: Tetsuo Asaki, Yukiteru Sugiyama, Jun Segawa
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Patent number: 7727986Abstract: The present invention relates to 2,5-disubstituted-4-pyrimidinyl-substituted-phenyl-amidine derivatives of formula (I) in which the substituents are as in the description, notably to 2,5-dialkyl-4-pyrimidinyl-substituted-phenyl-amidine derivatives, their process of preparation, their use as fungicide or insecticide active agents, particularly in the form of fungicide or insecticide compositions, and methods for the control of phytopathogenic fungi or damaging insects, notably of plants, using these compounds or compositions.Type: GrantFiled: September 12, 2006Date of Patent: June 1, 2010Assignee: Bayer CropScience AGInventors: Klaus Kunz, Jörg Greul, Oliver Guth, Benoît Hartmann, Kerstin Ilg, Wahed Ahmed Moradi, Thomas Seitz, Jean-Pierre Vors, Peter Dahmen, Arnd Voerste, Ulrike Wachendorff-Neumann, Mark Drewes, Ralf Dunkel, Ronald Ebbert, Herbert Gayer, Peter Lösel, Eva-Maria Franken, Olga Malsam
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Publication number: 20100129321Abstract: The present invention relates to pharmaceutical compositions for treating virus infections and/or diseases caused thereby comprising 4{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide optionally combined with at least one additional therapeutic agent.Type: ApplicationFiled: December 6, 2006Publication date: May 27, 2010Applicant: BAYER HEALTHCARE LLCInventors: Olaf Weber, Bernd Riedl
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Publication number: 20100113490Abstract: The invention relates to substituted pyrimidine ether compounds having general formula I: The groups are as defined as specification. The compounds of formula I show high insecticidal activities for imagoes, larvae and nits of harmful acari and insects in the agricultural, civil and zoic fields, especially show excellent insecticidal activities for harmful acari such as Tetranychus cinnabarinus. Good effects can be obtained at very low dose. The compounds also exhibit preferably fungicidal activity. Wherefore, the invention also comprises the uses of compounds of formula I as insecticides, acaricides and/or fungicides in agricultural and other fields.Type: ApplicationFiled: May 22, 2008Publication date: May 6, 2010Inventors: Changling Liu, Baoshan Chai, Hong Zhang, Huichao Li, Junfeng Wang, Yongwu Peng, Jichun Yang, Guangxin Liu, Zhinian Li
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Patent number: 7696211Abstract: Methods and compositions for treating and preventing sepsis are provided. The methods of the invention comprise administering to a subject a therapeutically effective amount of an A1 adenosine receptor antagonist in combination with an antibiotic agent. The invention further encompasses pharmaceutical compositions comprising a combination of an A1 adenosine receptor antagonist and an antibiotic agent in a pharmaceutically acceptable carrier. The pharmaceutical compositions of the invention find use in methods for treating and preventing sepsis.Type: GrantFiled: April 27, 2006Date of Patent: April 13, 2010Inventor: Constance N. Wilson
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Patent number: 7696217Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient.Type: GrantFiled: June 25, 2004Date of Patent: April 13, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: William P. Dankulich, Mildred L. Kaufman, Robert S. Meissner, Helen J. Mitchell
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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: 7683069Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof useful as a tau protein kinase 1 inhibitor: wherein X represents CH or nitrogen atom; R1 represents a C?1#191-C?12#191 alkyl group which may be substituted; R2 represents a C?1#191-C?8#191 alkyl group which may be substituted, a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom, and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.Type: GrantFiled: December 12, 2003Date of Patent: March 23, 2010Assignees: Mitsubishi Tanabe Pharma Corporation, Sanofi-AventisInventors: Yoshihiro Usui, Masahiro Okuyama, Tokushi Hanano
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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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Publication number: 20100056512Abstract: Pyrimidine compounds of the following formula: wherein R1, R2, R3, R4, R5, X, Q1, Q2, and Q3 are defined herein. Also disclosed is a method of treating cancer with one of these compounds.Type: ApplicationFiled: August 29, 2008Publication date: March 4, 2010Applicant: Hutchison MediPharma Enterprises LimitedInventors: Wei-Guo Su, Hong Jia, Rick B. Ye, Yang Sai
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Publication number: 20100048567Abstract: The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk 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 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 kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: ApplicationFiled: April 16, 2009Publication date: February 25, 2010Applicant: Portola Pharmaceuticals Inc.Inventors: Zhaozhong Jia, Chandrasekar Venkataramani, Wolin Huang, Mukund Mehrota, Yonghong Song, Qing Xu, Shawn M. Bauer, Jack W. Rose, Brian Kane, Anjali Pandey
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Publication number: 20100041684Abstract: Objects of the present invention are the compounds of formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.Type: ApplicationFiled: December 19, 2007Publication date: February 18, 2010Inventors: Guy Georges, Matthias Koerner, Irene Kolm, Ulrike Reiff, Wolfgang Schaefer, Edgar Voss, Stefan Weigand
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Publication number: 20100028277Abstract: Composition containing, in a cosmetically or dermatologically acceptable medium, a compound that may be obtained by reaction between: an oil bearing at least one nucleophilic and/or electrophilic reactive function, and a junction group capable of establishing hydrogen bonds with one or more partner junction groups, the junction group bearing at least one reactive function capable of reacting with the reactive function borne by the oil, and also comprising at least one unit of formula (I) or (II):Type: ApplicationFiled: July 1, 2009Publication date: February 4, 2010Applicant: L'OREALInventors: Sandrine CHODOROWSKI-KIMMES, Ivan Rodriguez
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Patent number: 7652021Abstract: The present invention relates to the novel compounds of the general formula (I) possessing dipeptidyl peptidase IV enzyme inhibitory activity, pharmaceutical compositions thereof, methods of using said compounds, processes for their preparation and intermediates of the general formulae (II), (IV), (V), (VII), (VIII) and (IX).Type: GrantFiled: February 28, 2006Date of Patent: January 26, 2010Assignee: Sanofi-AventisInventors: Peter Aranyi, Imre Bata, Sandor Batori, Eva Boronkay, Philippe Bovy, Zoltan Kapui, Edit Susan, Tibor Szabo, Katalin Urban-Szabo, Marton Varga
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Publication number: 20100016319Abstract: This invention relates to a pharmaceutical comprising as an effective ingredient an arylmethylene urea exemplified by the following formula: or a pharmaceutically acceptable salt thereof. The arylmethylene urea and the pharmaceutically acceptable salts thereof are useful for therapy or prophylaxis of inflammatory bowel disease and overactive bladder.Type: ApplicationFiled: November 29, 2006Publication date: January 21, 2010Applicant: TORAY INDUSTRIES, INC. a corporation of JapanInventors: Michihiro Ohno, Hideki Inoue, Shinnosuke Hayashi, Mie Kaino, Sunao Hara, Satoru Yoshikawa
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Publication number: 20090318481Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.Type: ApplicationFiled: August 28, 2009Publication date: December 24, 2009Inventors: Thomas Daniel AICHER, Guillermo S. CORTEZ, Todd Michael GROENDYKE, Albert KHILEVICH, James Allen KNOBELSDORF, Fredrik Pehr MARMSATER, Jeffrey Michael SCHKERYANTZ, Tony Pisal TANG
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Publication number: 20090286817Abstract: Compounds of formula I are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and/or manage diseases and disorders:Type: ApplicationFiled: May 20, 2009Publication date: November 19, 2009Inventors: Arokiasamy Devasagayaraj, Haihong Jin, Zhi-Cai Shi, Ashok Tunoori, Ying Wang, Chengmin Zhang
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Publication number: 20090275599Abstract: A therapeutic or prophylactic agent for multiple sclerosis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for multiple sclerosis according to the present invention shows the excellent absorbability and in vivo stability when orally administered, and exhibits high therapeutic or prophylactic effects.Type: ApplicationFiled: June 18, 2007Publication date: November 5, 2009Applicant: TORAY INDUSTRIES, INC.Inventors: Kenichi Hayashi, Mie Kaino, Hiroyuki Meguro
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Patent number: 7592348Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: GrantFiled: December 13, 2004Date of Patent: September 22, 2009Assignee: Schering CorporationInventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X. H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
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Publication number: 20090232828Abstract: The invention provides methods of treating cancer with a compound which inhibits kinases, more specifically IGF1R and Abl, in combination with treatments(s) selected from surgery, radiation, monoclonal antibody, bone marrow or peripheral blood stem cell transplantation, and one or more chemotherapeutic agent(s).Type: ApplicationFiled: July 3, 2007Publication date: September 17, 2009Applicant: EXELIXIS, INC.Inventor: Wentao Zhang
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Patent number: 7585870Abstract: This invention concerns HIV replication inhibitors of formula (I), the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.Type: GrantFiled: February 20, 2004Date of Patent: September 8, 2009Assignee: Tibotec BVBAInventors: Jerôme Emile Georges Guillemont, Elisabeth Thérese Jeanne Pasquier, Jan Heeres, Kurt Hertogs, Eva Bettens, Paulus Joannes Lewi, Marc René De Jonge, Lucien Maria Henricus Koymans, Frederik Frans Desiré Daeyaert, Hendrik Maarten Vinkers, Frank Xavier Jozef Herwig Arts
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Publication number: 20090221579Abstract: This invention relates to novel compounds having the structural formula Ia or formula Ib: Ia Ib and their pharmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of A? related pathologies such as cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: October 14, 2005Publication date: September 3, 2009Inventors: Jeffrey Scott Albert, Don Andisik, James Arnold, Dean Brown, Owen Callaghan, James Campbell, Robin Arthur Ellis Carr, Gianni Chessari, Miles Stuart Congreve, Phil Edwards, James R. Empfield, Martyn Frederickson, Gerard M. Koether, Jennifer Krumrine, Russ Mauger, Christopher William Murray, Sahil Patel, Mark Sylvester, Scott Throner
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Publication number: 20090215801Abstract: This invention relates to novel compounds having the structural formula I below: (I) and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: November 13, 2006Publication date: August 27, 2009Applicant: ASTRAZENECA AB, SODERTAIJE, SWEDENASTEX THEREAPEUTICS LTDInventors: Jeffrey Albert, Donald Andisik, Phil Edwards, Mark Sylvester
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Publication number: 20090197903Abstract: This invention relates to a process for producing a spray-dried powder comprising microcrystalline cellulose in a solid dispersion of the anti-HIV compound etravirine (TMC125) in a water-soluble polymer.Type: ApplicationFiled: June 6, 2007Publication date: August 6, 2009Applicant: TIBOTEC PHARMACEUTICALS LTD.Inventors: Filip Rene Irene Kiekens, Jody Firmin Marceline Voorspoels, Lieven Elvire Colette Baert
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Patent number: 7566710Abstract: The invention relates to dual molecules formed from coupling products complying with the formula wherein A represents a residue of molecule with anti-malarial activity, Y1 and Y2, represent a linear or branched alkylene chain at C1 to C5, or either Y1 or Y2 is absent, U is an amine, amide, sulphonamide, carboxyl, ether or thioether function, said function linking Y1 and Y2, Z1 and Z2, represent a linear arylene or alkylene, or either Z1 or Z2 is absent, or Z1+Z2 together represent a cyclic or polycyclic structure including the junction carbons Ci and Cj, R1 and R2, represent a hydrogen atom or a functional group capable of increasing the hydrosolubility of the dual molecule, Rx and Ry form a cyclic peroxide with 4 to 8 chain links, Cj being one of the peaks of said cyclic peroxide, or -Rx or Ry is a cyclic peroxide with 4 to 8 chain links, which may comprise 1 or 2 additional oxygen atoms in the cyclic structure, and one or more substituents R3, identical or different, at least one R3 representing a halType: GrantFiled: August 4, 2005Date of Patent: July 28, 2009Assignee: Centre National de la Racherche Scientifique (C.N.R.S.)Inventors: Bernard Meunier, Anne Robert, Odile Dechy-Cabaret, Francoise Benoit-Vical
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Patent number: 7563788Abstract: Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I as disclosed herein can be used in a variety of applications including use as antibacterial agents.Type: GrantFiled: March 7, 2005Date of Patent: July 21, 2009Assignee: Pfizer Inc.Inventors: Richard John Sciotti, Jeremy Tyson Starr, Christopher Richardson, Gordon William Rewcastle, Huifen Chen, Brian Desmond Palmer, Hamish Scott Sutherland, Julie Ann Spicer
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Patent number: 7560464Abstract: The present invention provides a genus of polycyclic pyrimidines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods.Type: GrantFiled: April 13, 2005Date of Patent: July 14, 2009Assignee: Icagen, Inc.Inventors: Xiaodong Wang, Kerry Leigh Spear, Alan Bradley Fulp, Darrick Seconi, Takeshi Suzuki, Takahiro Ishii, Ayako Moritomo
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Patent number: 7560466Abstract: 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: GrantFiled: October 6, 2006Date of Patent: July 14, 2009Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
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Patent number: 7557210Abstract: 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: January 31, 2003Date of Patent: July 7, 2009Assignee: 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: 20090149467Abstract: The present invention relates to pyridinyloxy- and pyrimidinyloxyindole derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: September 11, 2006Publication date: June 11, 2009Applicant: MERCK & CO., INC.Inventors: Christopher J. Dinsmore, David J. Guerin, Barbara Hanney, Yuntae Kim, Keith L. Spencer, Maricel Torrent
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Publication number: 20090124645Abstract: This invention relates to novel pyrimidine-2,4-diamine derivatives useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: October 13, 2006Publication date: May 14, 2009Applicant: NeuroSearch A/SInventors: Ulrik Svane Sorensen, Birgitte L. Eriksen, Lene Teuber, Dan Peters, Dorte Strobaek, Tina Holm Johansen, Palle Christophersen
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Publication number: 20090124644Abstract: HIV replication inhibitors of formula pharmaceutically acceptable addition salts or stereochemically isomeric forms thereof, wherein X is NR4, S, SO or SO2; the preparation of these compounds as well as pharmaceutical compositions comprising these compounds; the use of these compounds for the prevention or the treatment of HIV infection.Type: ApplicationFiled: January 27, 2006Publication date: May 14, 2009Applicant: JANSSEN PHARMACEUTICA N.V.Inventors: Jan Heeres, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, Rudolf Leemans, Luc Jozef Raphael Moens
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Patent number: 7531547Abstract: Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): wherein D, X, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.Type: GrantFiled: August 25, 2006Date of Patent: May 12, 2009Assignee: Roche Palo Alto LLCInventors: Michael Patrick Dillon, Alam Jahangir, Amy Geraldine Moore, Paul J. Wagner
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Patent number: 7531548Abstract: HIV replication inhibitors of formula (I) N-oxides, a pharmaceutically acceptable addition salts, a quaternary amines or a stereoisomeric forms thereof, wherein -a1=a2-a3=a4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; -b1=b2-b3=b4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; —S(?O)rR6; C(?NH)R6; R2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C2-6alkyloxy; substituted carbonyl; —CH?N—NH—C(?O)—R16; optionally substituted C1-6alkyloxy C1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7 or —X3—R7; X1 is —NR1—, —O—, —C(?O)—, CH2, —CHOH—, —S—, —S(?O)r—; R3 is CN; amino; C1-6alkyl; halo; optionally subsType: GrantFiled: September 29, 2005Date of Patent: May 12, 2009Assignee: Tibotec Pharmaceuticals LtdInventors: Jerôme Emile Georges Guillemont, Jan Heeres, Paulus Joannes Lewi
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Publication number: 20090105147Abstract: This disclosure relates to novel di-aryl-pyrimidine (DAPY) compounds and pharmaceutically acceptable salts thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a non-nucleoside reverse transcriptase inhibitor (NNRTI).Type: ApplicationFiled: October 17, 2008Publication date: April 23, 2009Applicant: Concert Pharmaceuticals Inc.Inventor: Craig E. Masse
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Publication number: 20090099217Abstract: This invention relates to novel compounds having the structural formula (I) below: [Chemical formula should be inserted here. Please see paper copy] and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: April 4, 2007Publication date: April 16, 2009Applicants: ASTEX THERAPEUTICS LTD., ASTRAECA ABInventors: Stefan Berg, Johan Hedstrom, Sven Hellberg, Johan Malmberg
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Publication number: 20090093486Abstract: N-Azinyl-N?-aryl ureas and thioureas derivatives are effective at controlling insects.Type: ApplicationFiled: September 26, 2008Publication date: April 9, 2009Applicant: Dow AgroSciences LLCInventors: Noormahamed M. Niyaz, Ricky Hunter, Timothy C. Johnson, Tony K. Trullinger, Annette V. Brown, Kristy Bryan
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Publication number: 20090093485Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).Type: ApplicationFiled: October 26, 2005Publication date: April 9, 2009Applicant: ASTRAZENECA ABInventors: Hakan Bladh, Krister Henriksson, Vijaykumar Hulikal, Matti Lepisto
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Patent number: 7514445Abstract: This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A is a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is a direct bond or a linker atom or group; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C2-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21—C1-6alkyl; R21—O—; R21—S—; R21—C(?O)—; R21—S(?O)p—; R7—S(?O)p—; R7—S(?O)p—NH—; R21—S(?O)p—NH—; R7—C(?O)—; —NHC(?O)H; —CType: GrantFiled: October 29, 2002Date of Patent: April 7, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy Jean Edgard Freyne, Peter Jacobus Johannes Antonius Buijnsters, Marc Willems, Werner Constant Johan Embrechts, Christopher John Love, Paul Adriaan Jan Janssen, Paulus Joannes Lewi, Jan Heeres, Marc René de Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Koen Jeanne Alfons Van Aken, Gaston Stanislas Marcella Diels
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Publication number: 20090088447Abstract: Solid forms of (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate and salts thereof are disclosed.Type: ApplicationFiled: September 25, 2008Publication date: April 2, 2009Inventors: Mark S. Bednarz, Susan De Paul, Ramanaiah C. Kanamarlapudi, Anett Perlberg, Haiming Zhang
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Patent number: 7507738Abstract: The present invention provides a production method of 5-aminopyrimidine compound represented by the formula (5) by reacting a glycine compound represented by the formula (1) with t-butoxybisdimethylaminomethane, dimethylformamidedimethylacetal or dimethylformamidediethylacetal to produce a dialkylaminomethylene compound represented by the formula (2), reacting the compound of formula (2) in the presence of an acid to produce a hydroxymethylene compound represented by the formula (3), and reacting the compound of formula (3) with an amidine compound represented by the formula (4) or a salt thereof.Type: GrantFiled: March 17, 2005Date of Patent: March 24, 2009Assignee: Ajinomoto Co., Inc.Inventors: Daisuke Takahashi, Kunisuke Izawa
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Patent number: RE41289Abstract: The subject invention concerns novel compounds that are useful as ultrashort acting hypnotic barbiturates. Specifically exemplified are derivatives of barbituric and thiobarbituric acids. They are rapidly metabolized by blood and tissue enzymes to form polar metabolites with no hypnotic activity and which are rapidly eliminated.Type: GrantFiled: December 20, 2007Date of Patent: April 27, 2010Assignee: ARYx Therapeutics, Inc.Inventors: Pascal Druzgala, Peter G. Milner