Diazine Ring Patents (Class 544/114)
  • Publication number: 20100261697
    Abstract: Compounds of the formula (I) in which R1, R2, R3, R4 and R5 have the meanings indicated in claim 1 are inhibitors of tyrosine kinases, in particular of met kinase and can be employed inter alia for the treatment of tumours.
    Type: Application
    Filed: July 12, 2007
    Publication date: October 14, 2010
    Inventors: Dieter Dorsch, Oliver Schadt, Andree Blaukat, Frank Stieber
  • Publication number: 20100256149
    Abstract: The invention provides novel arylamino N-heteroaryl MEK inhibitors of Formula (I): Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: June 14, 2010
    Publication date: October 7, 2010
    Applicant: MERCK SERONO S.A.
    Inventors: Andreas Goutopoulos, Benny C. Askew, JR., Nhut Kiet Diep, Srinivasa Karra, Matthias Schwarz, Henry Yu
  • Publication number: 20100234354
    Abstract: Compounds of the formula (I), in which R1, R2, R, R4, R4? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: April 29, 2008
    Publication date: September 16, 2010
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Dieter Dorsch, Frank Stieber, Oliver Schadt, Andree Blaukat
  • Publication number: 20100216793
    Abstract: The present invention is concerned with novel pyridazinone derivatives of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.
    Type: Application
    Filed: February 16, 2010
    Publication date: August 26, 2010
    Inventors: Daniela Alberati, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rose Maria Rodriguez Sarmiento, Mark Rogers-Evans, Markus Rudolph
  • Publication number: 20100210594
    Abstract: The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
    Type: Application
    Filed: July 25, 2008
    Publication date: August 19, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
  • Publication number: 20100210649
    Abstract: The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries.
    Type: Application
    Filed: December 21, 2007
    Publication date: August 19, 2010
    Applicant: Sloan-Kettering Institute for Cancer Research
    Inventors: Hakim Djaballah, Harold E. Varmus, David Shum, Romel Somwar, Alexander Chucholowski, Mohan Santhanam Thiruvazhi
  • Patent number: 7772233
    Abstract: The invention provides novel arylamino N-heteroaryl MEK inhibitors of Formula (I): Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: August 10, 2010
    Assignee: Merck Serono, S.A.
    Inventors: Andreas Goutopoulos, Benny C. Askew, Jr., Nhut Kiet Diep, Srinivasa Karra, Matthias Schwarz, Henry Yu
  • Publication number: 20100197908
    Abstract: The present invention relates to compounds of general formula I wherein the groups and radicals B, W, X, Y, Z, R1, R2, have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
    Type: Application
    Filed: December 10, 2007
    Publication date: August 5, 2010
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Thorsten Lehmann-Lintz, Dirk Stenkamp, Gerald Juergen Roth, Stephan Georg Mueller, Joerg Kley, Armin Heckel, Klaus Rudolf, Marcus Schindler, Ralf Lotz, Patrick Tielmann
  • Publication number: 20100197651
    Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0): wherein R1 represents a substituent, R2 represents a hydrogen atom, or a substituent, R3 represents a hydrogen atom, or a substituent, Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.
    Type: Application
    Filed: February 4, 2010
    Publication date: August 5, 2010
    Inventors: Takahiko Taniguchi, Akira Kawada, Mitsuyo Kondo, John F. Quinn, Jun Kunitomo, Masato Yoshikawa, Makoto Fushimi
  • Patent number: 7767669
    Abstract: Compounds having formula I are provided where the variables have the values described herein. Pharmaceutical formulations include the compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and combinations with other agents. A method of treating a patient comprises administering a pharmaceutical formulation according to the invention to a patient in need thereof.
    Type: Grant
    Filed: August 8, 2008
    Date of Patent: August 3, 2010
    Assignee: Novartis AG
    Inventors: John M. Nuss, Sabina Pecchi, Paul A. Renhowe
  • Publication number: 20100179149
    Abstract: Compounds of the formula I, in which R1, R2, R3, R4, R5 and X have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: May 2, 2008
    Publication date: July 15, 2010
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNG
    Inventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
  • Publication number: 20100179148
    Abstract: Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: May 2, 2008
    Publication date: July 15, 2010
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
  • Patent number: 7750001
    Abstract: A novel method for immunosuppressive in a mammal suffering from an immune disease, including administering to the mammal a therapeutically effective amount of a heterocyclic compound represented by the general formula (I) (wherein X or other variables are as defined in the specification) or a pharmaceutically acceptable salt thereof is disclosed. A novel heterocyclic compound represented by the general formula (II) (wherein X or other variables are as defined in the specification) or a pharmaceutically acceptable salt thereof is also disclosed.
    Type: Grant
    Filed: August 30, 2007
    Date of Patent: July 6, 2010
    Assignee: Zenyaku Kogyo Kabushikikaisha
    Inventors: Kazuhiko Haruta, Shinichi Yaguchi, Toshiyuki Matsuno, Yoshio Tsuchida, Tetsuo Watanabe, Kimitomo Yoshioka, Ryogo Yui
  • Publication number: 20100168076
    Abstract: The instant invention provides compounds of Formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
    Type: Application
    Filed: August 29, 2007
    Publication date: July 1, 2010
    Inventors: Anthony Ogawa, Feroze Ujjainwalla, Ellenk Vande Bunte, Lin Chu, Debra Ondeyka, Ihor Kopka, Bing Li, Hyun Ok, Minal J. Patel, Jinyou Xu, Rosemary Sisco
  • Patent number: 7723330
    Abstract: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Grant
    Filed: March 6, 2007
    Date of Patent: May 25, 2010
    Assignees: Array BioPharma Inc., Genentech, Inc.
    Inventors: James F. Blake, Steven Armen Boyd, Jason De Meese, Kin Chiu Fong, John J. Gaudino, Tomas Kaplan, Allison L. Marlow, Jeongbeob Seo, Allen A. Thomas, Hongqi Tian, Frederick Cohen, Wendy B. Young
  • Patent number: 7709466
    Abstract: The present invention relates to pyridazinone compounds and their derivatives according to the general formula (I), with the substituents X, R1 and R2 defined herein, as well as their physiologically acceptable salts, methods for producing these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase GSK-3? (glycogen synthase kinase-3?) which are useful in the treatment of neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, strokes, cranial and spinal traumas and peripheral neuropathies, obesity, metabolic diseases, type II diabetes, essential hypertension, atherosclerotic cardiovascular diseases, polycystic ovary syndrome and syndrome X or immunodeficiency.
    Type: Grant
    Filed: October 24, 2006
    Date of Patent: May 4, 2010
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Swen Hoelder, Karl Schoenafinger, David William Will, Hans Matter, Guenter Mueller, Martin Bossart
  • Patent number: 7696202
    Abstract: The invention relates to heterocyclic compounds, compositions including the compounds and methods of using and methods of making thereof. The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-12.
    Type: Grant
    Filed: November 10, 2005
    Date of Patent: April 13, 2010
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Elena Kostik, Teresa Przewloka, Howard P. Ng, Dinesh Chimmanamada, Zachary Demko
  • Publication number: 20100075970
    Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
    Type: Application
    Filed: November 18, 2009
    Publication date: March 25, 2010
    Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D.P. Cosford, Jacob M. Hoffman, Johnny Yasou Nagasawa
  • Patent number: 7678802
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: March 3, 2004
    Date of Patent: March 16, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jesus E. Gonzalez, III, Dean Mitchell Wilson, Andreas Peter Termin, Peter Diederik Jan Grootenhuis, Yulian Zhang, Benjamin John Petzoldt, Lev Tyler Dewey Fanning, Timothy Donald Neubert, Roger Tung, Esther Martinborough, Nicole Zimmerman
  • Publication number: 20100063031
    Abstract: Pyridine and pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.
    Type: Application
    Filed: January 18, 2008
    Publication date: March 11, 2010
    Applicant: XCOVERY, INC.
    Inventor: Congxin Liang
  • Publication number: 20100063027
    Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted lower alkyl, Y is —S(O)n— wherein n is 1 or 2, or —CO—, R2 is hydrogen or lower alkyl, R7 is hydrogen or lower alkyl, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, and Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like.
    Type: Application
    Filed: April 25, 2007
    Publication date: March 11, 2010
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Takayuki Okuno, Naoki Kouyama, Masahiro Sakagami
  • Patent number: 7655649
    Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
    Type: Grant
    Filed: April 5, 2005
    Date of Patent: February 2, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
  • Patent number: 7652051
    Abstract: 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: Grant
    Filed: August 24, 2005
    Date of Patent: January 26, 2010
    Assignee: TargeGen, Inc.
    Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
  • Publication number: 20090312327
    Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, Ar and n are as defined herein and pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers or tautomeric forms thereof. The compounds can be used for the treatment of depression, anxiety or schizophrenia.
    Type: Application
    Filed: June 11, 2009
    Publication date: December 17, 2009
    Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Andreas Koblet, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer
  • Patent number: 7608563
    Abstract: A compound represented by the formula: [wherein R1 represents a hydrogen atom, a halogen, atom, alkyl group, etc., R2 represents a hydrogen atom, a halogen atom, alkyl group, etc., R3, R4, R5, R6 and R7 each independently represent a hydrogen atom, a halogen atom, a substitutable alkyl group, a substitutable alkenyl group, alkynyl group, a substituteable cycloalkyl group, etc., or R3, R4, R5, R6 and R7 may form a ring which may be substituted, which is formed by the adjacent two of them with carbon atoms to which the respective substituents are bonded, m and n each independently represent 0 or 1.] a salt thereof, an ester derivative thereof and an agricultural chemical containing the same as an effective ingredient, and a herbicidal composition containing the compound and a second herbicidally active compound as effective ingredients.
    Type: Grant
    Filed: August 14, 2002
    Date of Patent: October 27, 2009
    Assignee: Mitsui Agro Chemicals, Inc.
    Inventors: Yoshihisa Tsukamoto, Hiroyuki Komai, Junji Kadotani, Kiyoshi Koi, Shigeru Mio, Hideo Takeshiba
  • Publication number: 20090258851
    Abstract: The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula II are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
    Type: Application
    Filed: April 6, 2007
    Publication date: October 15, 2009
    Inventors: LIN Chu, Bing Li, Anthony K. Ogawa, Hyun O. Ok, Debra L Ondeyka, Minal Patel, Rosemary Sisco, Feroze Ujjainwalla, Jinyou Xu
  • Publication number: 20090253906
    Abstract: The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3 -a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle opt
    Type: Application
    Filed: April 2, 2009
    Publication date: October 8, 2009
    Applicant: AMR TECHNOLOGY, INC.
    Inventors: Bruce F. MOLINO, Shuang LIU, Peter R. GUZZO, James P. BECK
  • Patent number: 7598244
    Abstract: Novel [1,2,4]triazolo[1,5-a]pyrimidine derivative of the general formula (1): (1) its prodrug or a pharmaceutically acceptable salt thereof, which exhibits an antigen presentation inhibiting activity and is useful as a preventive and/or therapeutic agent for immunological rejection and/or graft versus host reaction in organ/bone marrow transplant, autoimmune disease, allergic disease and/or inflammatory disease and also useful as an anticancer drug or as an immunological tolerance inducer for transplanted organ/transplanted bone marrow.
    Type: Grant
    Filed: June 2, 2004
    Date of Patent: October 6, 2009
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Akira Masuda, Yoshitaka Satoh, Yuji Akiyama, Kan Saiga, Eriko Toyoda
  • Patent number: 7598242
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-? or combinations thereof.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: October 6, 2009
    Assignee: Schering Corporation
    Inventors: Zhaoning Zhu, Robert Mazzola, Zhuyan Guo, Brian J. Lavey, Lisa Sinning, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih
  • Patent number: 7560458
    Abstract: This invention concerns compounds of formula N-oxides, pharmaceutically acceptable addition salts, quaternary amines and stereochemically isomeric forms thereof, their use, pharmaceutical compositions comprising them, and processes for their preparation.
    Type: Grant
    Filed: July 12, 2004
    Date of Patent: July 14, 2009
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Eddy Jean Edgard Freyne, Christopher John Love, Ludwig Paul Cooymans, Nele Vandermaesen, Peter Jacobus Johannes Antonius Buijnsters, Marc Willems, Werner Constant Johan Embrechts
  • Publication number: 20090143385
    Abstract: The invention relates to isoxazolo-pyridazine compounds, in particular those of formula I as described above and to a pharmaceutically acceptable salts thereof, having affinity and selectivity for the GABA A ?5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the treatment of cognitive disorders like Alzheimer's disease.
    Type: Application
    Filed: November 25, 2008
    Publication date: June 4, 2009
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Andrew Thomas
  • Publication number: 20090088431
    Abstract: Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; lipid disorders; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; fatty liver disease and cancer.
    Type: Application
    Filed: December 18, 2006
    Publication date: April 2, 2009
    Inventors: Denis Deschenes, Rejean Fortin, Chun Sing Li, Renata M. Oballa, Yeeman K. Ramtohul
  • Patent number: 7507734
    Abstract: Disclosed are compounds according to the general formula (I), where the definitions of the substituents X, R1 and R2 are detailed in the description, as well as their physiologically acceptable salts and solvate, methods for producing these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).
    Type: Grant
    Filed: November 16, 2006
    Date of Patent: March 24, 2009
    Assignee: Aventis Pharma S.A.
    Inventors: Swen Hoelder, Gunter Muller, Karl Schoenafinger, David William Will, Hans Matter, Martin Bossart, Cecile Combeau, Christine Delaisi, Ingrid Sassoon, Anke Steinmetz, Didier Benard
  • Patent number: 7507834
    Abstract: The present invention relates to anilinopyrazole derivatives, methods for the preparation of such anilinopyrazoles, and use of such anilinopyrazoles in the treatment of certain diseases or conditions. In particular, the present invention relates to a nilinopyrazole derivatives useful as CDK2 inhibitors and use of the anilinopyrazoles in the treatment of disorders mediated by inappropriate CDK2 activity.
    Type: Grant
    Filed: February 25, 2004
    Date of Patent: March 24, 2009
    Assignee: SmithKline Beechan Corporation
    Inventor: Jun Tang
  • Publication number: 20090075968
    Abstract: The present invention relates to a compound of formula or a pharmaceutically acceptable salt thereof, wherein the variables are as defined.
    Type: Application
    Filed: December 27, 2006
    Publication date: March 19, 2009
    Inventors: Junichi Sakaki, Masashi Kishida, Naoko Matsuura, Ichiro Umemura, Eiji Kawahara, Ken Yamada, Kazuhide Konishi, Yuki Iwaki, Hidetomo Imase, Takahiro Miyake
  • Patent number: 7494990
    Abstract: The compounds of a certain formula (1), in which R1, R2, R3 and R9 have the meanings as given in the description, are novel effective PDE4 inhibitors.
    Type: Grant
    Filed: February 1, 2005
    Date of Patent: February 24, 2009
    Assignee: NYCOMED GmbH
    Inventors: Wiro M. P. B. Menge, Geert Jan Sterk
  • Publication number: 20090042856
    Abstract: A pyridazinone derivative compound shown by the following formula (I): wherein R1 is selected from hydrogen, etc.; R2 is selected from substituted or unsubstituted aryl, etc.; R3 is hydrogen, etc.; p is 0, 1 or 2; R4 and R5, are each hydrogen, etc.; R6 and R7, are taken together to form a group of the formula: wherein R8 is hydrogen; X is selected from oxygen, etc; R10 is selected from hydrogen, etc.; R11 is selected from hydrogen, etc.; R12 is selected from hydrogen, etc.; R13 is selected from hydrogen, etc.; R14 is selected from hydrogen, etc.; m and n are each 0, 1, or 2, or a pharmaceutically acceptable salt thereof, which is useful as a medicament.
    Type: Application
    Filed: August 31, 2006
    Publication date: February 12, 2009
    Applicants: Astellas Pharma Inc, Wakunaga Pharmaceutical Co., Ltd.
    Inventors: Hitoshi Yamazaki, Chiyoshi Kasahara, Hirokazu Kubota, Toru Kontani, Toru Asano, Hidekazu Mizuhara, Masaharu Yokomoto, Keiji Misumi, Tomohiko Kinoshita
  • Publication number: 20090029996
    Abstract: The invention relates to new therapeutically useful pyridazin-3(2H)-one derivatives, to processes for their preparation and to pharmaceutical compositions containing them. These compounds are potent and selective inhibitors of phosphodiesterase 4 (PDE4) and are thus useful in the treatment, prevention and suppression of related pathological conditions, diseases and disorders, in particular asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, topic dermatitis, psoriasis or irritable bowel disease.
    Type: Application
    Filed: June 21, 2005
    Publication date: January 29, 2009
    Inventors: Nuria Aguilar Izquierdo, Marta Carrascal Riera, Vittorio Dal Piaz, Jordi Gracia Ferrer, Wenceslao Lumeras Amador, Maria Del Carmen Masdeu Margalef, Graham Warrellow
  • Patent number: 7462613
    Abstract: The present invention relates to novel pyridazinone derivatives of the general formula (I) wherein A is A1 or A2; R is unsubstituted or at least monosubstituted C1-C10-alkyl, aryl, aryl-(C1-C10-alkyl)-, heteroaryl, heteroaryl-(C1-C10-alkyl)-, heterocyclyl, heterocyclyl-(C1-C10-alkyl)-, C3-C10-cycloalkyl, polycycloalkyl, C2-C10-alkenyl or C2-C10-alkinyl and Ar is unsubstituted or at least monosubstituted aryl or heteroaryl.
    Type: Grant
    Filed: November 19, 2003
    Date of Patent: December 9, 2008
    Assignee: SANOFI-AVENTIS Deutschland GmbH
    Inventors: Swen Hölder, Thorsten Naumann, Karl Schönafinger, David William Will, Hans Matter, Günther Müller, Dominique Le Suisse, Bernard Baudoin, Thomas Rooney, Franck Halley, Gilles Tiraboschi, Cécile Combeau, Ingrid Sassoon, Anke Steinmetz
  • Publication number: 20080293719
    Abstract: Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours
    Type: Application
    Filed: November 7, 2006
    Publication date: November 27, 2008
    Inventors: Dieter Dorsch, Oliver Schadt, Andree Blaukat
  • Publication number: 20080293705
    Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.
    Type: Application
    Filed: August 6, 2008
    Publication date: November 27, 2008
    Applicant: Endacea, Inc.
    Inventors: Constance Neely Wilson, John J. Partridge
  • Publication number: 20080280889
    Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration (if the compounds of the invention.
    Type: Application
    Filed: April 5, 2005
    Publication date: November 13, 2008
    Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D.P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
  • Patent number: 7429660
    Abstract: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and RN1 is selected from hydrogen, an optionally substituted C1-7 alkyl group, an optionally substituted C3-20 heterocyclyl group, an optionally substituted C5-20 aryl group, an acyl group, an ester group and an amido group, and its use as a pharmaceutical.
    Type: Grant
    Filed: August 13, 2004
    Date of Patent: September 30, 2008
    Assignee: Kudos Pharmaceuticals Limited
    Inventors: Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Laurent Jean Martin Rigoreau, Marc Geoffrey Hummersone, Roger John Griffin
  • Patent number: 7423148
    Abstract: Compounds having formula I are provided where the variables have the values described herein. Pharmaceutical formulations include the compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and combinations with other agents. A method of treating a patient comprises administering a pharmaceutical formulation according to the invention to a patient in need thereof.
    Type: Grant
    Filed: November 21, 2003
    Date of Patent: September 9, 2008
    Assignee: Chiron Corporation
    Inventors: John N. Nuss, Sabina Pecchi, Paul A. Renhowe
  • Publication number: 20080153834
    Abstract: At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical compositions comprising at least one chemical entity of the invention, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
    Type: Application
    Filed: September 11, 2007
    Publication date: June 26, 2008
    Inventors: Peter A. Blomgren, Seung H. Lee, Scott A. Mitchell, Jianjun Xu, Aaron C. Schmitt, Jeffrey E. Kropf, Kevin S. Currie
  • Patent number: 7371753
    Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups R1 to R5, Ra to Rc, W, Q1 and Q2 have the meanings given in the claims and specification, the isomers thereof and the use thereof for preparing a pharmaceutical composition for the treatment of diseases characterised by excessive or abnormal cell proliferation.
    Type: Grant
    Filed: August 25, 2005
    Date of Patent: May 13, 2008
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heinz Stadtmueller, Harald Engelhardt, Andreas Schoop, Martin Steegmaier, Matthias Hoffmann, Matthias Grauert
  • Patent number: 7365067
    Abstract: The present invention provides a compound having the following general formula (I) which is useful as a neurokinin receptor antagonist: (wherein, R1, R2: optionally substituted (hetero)aryl, R3: —CO—R4, —CO—O—R4, etc., R4: alkyl, cycloalkyl, etc., A: CH2, CO, SO2, B: a single bond, etc., D: oxygen, CH2, E: alkylene, alkenylene, n: 1 to 3).
    Type: Grant
    Filed: February 24, 2005
    Date of Patent: April 29, 2008
    Assignee: Sankyo Company, Limited
    Inventors: Takahide Nishi, Toshiyasu Takemoto, Takuya Ikeda, Kiyoshi Morimoto
  • Patent number: 7332483
    Abstract: The invention concerns amide derivatives of Formula (Ia) wherein X is —NHCO— or —CONH—; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-2; R2 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino and carboxy; R3 is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; q is 0-4; and Q is a group such as aryl, aryloxy, aryl-(1-6C)alkoxy, arylamino and N-(1-6C)alkyl-arylamino; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines
    Type: Grant
    Filed: August 18, 2006
    Date of Patent: February 19, 2008
    Assignee: AstraZeneca AB
    Inventor: Dearg S Brown
  • Patent number: 7320977
    Abstract: The invention relates to substituted 2-Phenyl-3(2H)-Pyridazinones, to a method for the production thereof, and to their use as medicaments for the prophylaxis and/or treatment of diseases in humans and/or animals.
    Type: Grant
    Filed: April 8, 2003
    Date of Patent: January 22, 2008
    Assignee: Bayer Healthcare AG
    Inventors: Rudolf Schohe-Loop, Elmar Burchardt, Christiane Faeste, Claudia Hirth-Dietrich, Jörg Keldenich, Andreas Knorr, Thomas Lampe, Paul Naab, Delf Schmidt, Gunter Schmidt
  • Patent number: 7312215
    Abstract: Benzimidazole derivatives having the general formula I are provided. These compounds are useful as tyrosine kinase inhibitors, especially for the treatment of cancer.
    Type: Grant
    Filed: July 20, 2004
    Date of Patent: December 25, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Francis Beaulieu, Anne Marinier, Carl Ouellet, Stephan Roy, Mark D. Wittman