Patents Examined by Venkataraman Balasubram
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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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Patent number: 7563922Abstract: 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: April 23, 2007Date of Patent: July 21, 2009Assignee: 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: 7544690Abstract: The present invention relates to novel compounds of the formula (I) which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of obesity, obesity related disorders, anxiety, or depression.Type: GrantFiled: September 30, 2002Date of Patent: June 9, 2009Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Yoshinori Sekiguchi, Kosuke Kanuma, Katsunori Omodera, Thuy-Anh Tran, Bryan Aubrey Kramer, Nigel Robert Arnold Beeley
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Patent number: 7511140Abstract: An improved process for manufacture of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl)(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid calcium salt, which is useful for the production of a pharmaceutical useful in the treatment of, inter alia, hypercholesterolemia, hyperlipoproteinemia and atherosclerosis, is described.Type: GrantFiled: August 7, 2003Date of Patent: March 31, 2009Assignee: AstraZeneca ABInventors: John Horbury, Nigel Philip Taylor
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Patent number: 7491730Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable derivative thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK3 mammalian protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.Type: GrantFiled: August 1, 2003Date of Patent: February 17, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Cornelia J. Forster, Larry C. Park, Marion W. Wannamaker, Yung-Mae M. Yao
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Patent number: 7470700Abstract: 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: December 30, 2008Assignee: 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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Patent number: 7470681Abstract: This invention features pyrimidine compounds of formula (I): R1 is each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.Type: GrantFiled: July 29, 2005Date of Patent: December 30, 2008Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Mitsunori Ono, Teresa Przewloka, Elena Kostik, Yumiko Wada
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Patent number: 7465725Abstract: This invention features pyrimidine compounds of formula (I): R1 is aryl, or heteroaryl; each of R2 and R4, independently, is Rc, halogen, nitro, cyano, isothionitro, SRc, or ORc; or R2 and R4, taken together, is carbonyl; R3 is Rc, alkenyl, alkynyl, ORc, OC(O)Rc, SO2Rc, S(O)Rc, S(O2)NRcRd, SRc, NRcRd, NRcCORd, NRcC(O)ORd, NRcC(O)NRcRd, NRcSO2Rd, CORc, C(O)ORc, or C(O)NRcRd; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is O, S, S(O), S(O2), or NRc; Y is a covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and each of Rc and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.Type: GrantFiled: July 29, 2005Date of Patent: December 16, 2008Assignee: Synta Pharmaceuticals Corp.Inventors: Mitsunori Ono, Lijun Sun, Teresa Przewloka, Shijie Zhang, Elena Kostik, Weiwen Ying, Yumiko Wada, Keizo Koya
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Patent number: 7465735Abstract: 5-Phenylpyrimidines, their preparation, compositions comprising them and their use 5-Phenylpyrimidines of the formula I in which the substituents and the index are as defined below: R1,R2 are hydrogen, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl, and R1 and R2 together with the nitrogen atom to which they are attached may also form a saturated or unsaturated ring which may be interrupted by an ether, thio, sulfoxyl or sulfonyl group and may be substituted by one to four groups Ra and/or Rb; R3 is hydrogen, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy or alkenyloxy; R4 is hydrogen, halogen, cyano, hydroxyl, mercapto, azido, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, alkenyloxy, alkynyloxy, haloalkoxy, alkylthio, alkenylthio, alkynylthio, haloalkylthio, —ON?CRaRb, —CRc?NORa, —NRcN?CRaRb, —NRaRb, —NRcNRaRb, —NORa, —NRcC(?NRc?)NRaRb, —NRcC(?O)NRaRb, —NRaC(?O)Rc, —NRaC(?NORc)Rc?, —OC(?O)Rc, —C(?NORc)NRaRb, —CRc(?NNRaRb), —C(?O)NRaRb or —C(?O)Rc; in whicType: GrantFiled: November 15, 2002Date of Patent: December 16, 2008Assignee: BASF AktiengesellschaftInventors: Andreas Gypser, Thomas Grote, Anja Schwögler, Joachim Rheinheimer, Frank Schieweck, Jordi Tormo i Blasco, Ingo Rose, Peter Schäfer, Markus Gewehr, Wassilios Grammenos, Bernd Müller, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Patent number: 7465736Abstract: An azole derivative of formula (I) a medicament that contains the azole derivative of formula (I), a method of treating a disease with the azole derivative of formula (I), and a method of preparing the azole derivative of formula (I).Type: GrantFiled: June 13, 2003Date of Patent: December 16, 2008Assignee: Laboratoires Serono S.A.Inventors: Pascale Gaillard, Jean-Pierre Gotteland, Isabelle Jeanclaude-Etter, Matthias Schwarz, Russel J. Thomas
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Patent number: 7462625Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: September 11, 2006Date of Patent: December 9, 2008Assignee: Neurocrine Biosciences, Inc.Inventors: Yun-Fei Zhu, Chen Chen, Fabio C. Tucci, Zhiqiang Guo, Timothy D. Gross, Martin Rowbottom, R. Scott Struthers
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Patent number: 7462614Abstract: The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.Type: GrantFiled: March 29, 2004Date of Patent: December 9, 2008Assignee: Smithkline Beecham CorporationInventors: Mui Cheung, Nigel Paul King, Kevin Wayne Kuntz, Robert Anthony Mook, Jr., Mark Andrew Pobanz, James Michael Salovich, Brian John Wilson
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Patent number: 7462616Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.Type: GrantFiled: October 24, 2006Date of Patent: December 9, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Alaric J. Dyckman, John T. Hynes, Katerina Leftheris, Chunjian Liu, Stephen T. Wrobleski
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Patent number: 7456176Abstract: The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases.Type: GrantFiled: April 7, 2005Date of Patent: November 25, 2008Assignee: TargeGen, Inc.Inventors: Glenn Noronha, Kathy Barrett, Jianguo Cao, Colleen Gritzen, Xianchang Gong, John D. Hood, Chi Ching Mak, Andrew McPherson, Ved Prakash Pathak, Joel Renick, Richard M. Soll, Ute Splittgerber, Wolfgang Wrasidlo, Binqi Zeng, Ningning Zhao, Elena Dneprovskaia
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Patent number: 7452897Abstract: The invention relates to therapeutic uses of a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I): Wherein R1, R2, R3, R4 and n are as defined herein. Specifically, the compounds of formula (I) are used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer's disease. The invention relates also to intermediates for the preparation of compound of formula (I).Type: GrantFiled: March 29, 2007Date of Patent: November 18, 2008Assignees: Sanofi-Aventis, Mitsubishi Pharma CorporationInventors: Alistair Lochead, Mourad Saady, Franck Slowinski, Philippe Yaiche
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Patent number: 7452879Abstract: 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 5, 2006Date of Patent: November 18, 2008Assignee: 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: 7449470Abstract: The invention provides a compound of formula (I) wherein R and R? are selected from hydrogen, alkyl, alkenyl, alkynyl, or aryl; R? and R?? are selected from hydrogen, acyl, thio-acyl, seleno-acyl, alkyl, alkenyl, alkynyl, or aryl; or a pharmaceutically acceptable salt thereof, to interact with the adenosine receptors in the beneficial treatment and/or prevention of a (dis)order arising from the said receptors. The invention further provides pharmaceutical compositions comprising said compounds. The invention also relates to the use of said compositions for treating an/or preventing a variety of diseases.Type: GrantFiled: October 1, 2004Date of Patent: November 11, 2008Assignee: Universiteit LeidenInventors: Lisa Chung Wai Chang, Adriaan P. Ijzerman, Johannes Brussee
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Patent number: 7449574Abstract: The present invention relates to a triazine based photoactive compound containing an oxime ester group. The compound according to the present invention is a photoactive compound containing both an oxime ester group and a triazine group in one molecule, has excellent radical-generating efficiency due to effective absorption of UV radiation, particularly i-line (365 nm) radiation and can function as an effective initiator for photopolymerization of various compounds containing unsaturated groups, particularly an acryl compound.Type: GrantFiled: November 6, 2006Date of Patent: November 11, 2008Assignee: LG Chem, Ltd.Inventors: Sung Hyun Kim, Jeong Ae Yoon, Raisa Kharbash, Han Soo Kim, Xiang Li Li, Min Young Lim, Chang Ho Cho
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Patent number: 7449471Abstract: 5-Phenylpyrimidines of the formula I in which the substituents and the index are as defined below: R1,R2 are hydrogen, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl, and R1 and R2 together with the nitrogen atom to which they are attached may also form a saturated or unsaturated ring which may be interrupted by an ether, thio, sulfoxyl or sulfonyl group and may be substituted by one to four groups Ra and/or Rb; R3 is hydrogen, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy or alkenyloxy; R4 is hydrogen, halogen, cyano, hydroxyl, mercapto, azido, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, alkenyloxy, alkynyloxy, haloalkoxy, alkylthio, alkenylthio, alkynylthio, haloalkylthio, —ON?CRaRb, —CRc?NORa, —NRcN?CRaRb, —NRaRb, —NRcNRaRb, —NORa, —NRcC(?NRc?)NRaRb, —NRcC(?O)NRaRb, —NRaC(?O)Rc, —NRaC(?NORc)Rc?, —OC(?O)Rc, —C(?NORc)NRaRb, —CRc(?NNRaRb), —C (?O)NRaRb or —C(?O)Rc; in which Ra, Rb and Rc are as defined in the description; X is halogen, alkyl, alkoxy oType: GrantFiled: February 22, 2007Date of Patent: November 11, 2008Assignee: BASF AktiengesellschaftInventors: Andreas Gypser, Thomas Grote, Anja Schwögler, Joachim Rheinheimer, Frank Schieweck, Jordi Tormo i Blasco, Ingo Rose, Peter Schäfer, Markus Gewehr, Wassilios Grammenos, Bernd Müller, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Patent number: 7446209Abstract: This invention relates to a novel process for the synthesis of Temozolomide, an antitumor compound, and analogs, and to intermediates useful in this novel process.Type: GrantFiled: June 14, 2006Date of Patent: November 4, 2008Assignee: Schering CorporationInventors: Shen-Chun Kuo, Janet L. Mas, Donald Hou