Carbocyclic Ring Containing Patents (Class 544/321)
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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: 20100121060Abstract: HIV replication inhibitors of formula pharmaceutically acceptable addition salts; or stereochemically isomeric forms thereof, wherein R1 is halo; R2 and R3 each independently are C1-6alkyl; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.Type: ApplicationFiled: January 20, 2010Publication date: May 13, 2010Inventors: Herman Augustinus De Kock, Piet Tom Bert Paul Wigerinck
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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: 7700603Abstract: 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: June 9, 2005Date of Patent: April 20, 2010Assignee: Schering CorporationInventors: Zhaoning Zhu, Brian A 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, Michelle L. Morris, Gang Qian, Dawit Tadesse
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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: 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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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: 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: 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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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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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: 20090186373Abstract: The invention relates to pyrimidines suitable as substrates for O6-alkylguanine-DNA alkyltransferases (AGT) of formula (I) wherein R1 is hydrogen, lower alkyl, halogen, cyano, trifluoromethyl or azido; R2 is a linker; and L is a label or a plurality of same or different labels. The invention further relates to methods of transferring a label from pyrimidines of formula (I) to O6-alkylguanine-DNA alkyltransferases (AGT) and AGT fusion proteins.Type: ApplicationFiled: April 25, 2006Publication date: July 23, 2009Inventors: Maik Kindermann, Markus Schwab
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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: 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: 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: 20090118505Abstract: Intermediates and synthetic processes for the preparation of substituted phenylalanine-based compounds (e.g.Type: ApplicationFiled: October 24, 2008Publication date: May 7, 2009
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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: 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: 7504410Abstract: This invention relates to pyrimidine derivatives of general formula (I) as inhibitors of kinases, their production as well as their use as medications for treating various diseases.Type: GrantFiled: November 28, 2003Date of Patent: March 17, 2009Assignee: Schering AktiengesellschaftInventors: Judi Bryant, Monica J. Kochanny, Shendong Yuan, Seock-Kyu Khim, Brad O. Buckman, Damian O. Arnaiz, Ulf Bomer, Hans Briem, Peter Esperling, Christoph Huwe, Joachim Kuhnke, Martina Schafer, Lars Wortmann, Dirk Kosemund, Emil Eckle, Richard I. Feldman, Gary B. Phillips
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Patent number: 7504396Abstract: The present invention relates to pyrimidine or pyridine carboxamides or pharmaceutically-acceptable salts thereof.Type: GrantFiled: June 23, 2004Date of Patent: March 17, 2009Assignee: Amgen Inc.Inventors: Joseph J. Nunes, Xiaotian Zhu, Patricia Amouzegh, Chiara Ghiron, David N. Johnson, Eoin Christopher Power
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Publication number: 20090062282Abstract: This invention relates to novel compounds having the structural formula Ia or formula Ib below: (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: March 5, 2009Applicant: AstraZeneca ABInventors: 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: 20090062540Abstract: Methods useful for preparing compounds of formula I: and salts thereof are disclosed. Also disclosed are intermediates useful in the preparation of such compounds.Type: ApplicationFiled: August 22, 2008Publication date: March 5, 2009Inventors: Mark S. Bednarz, Hugh Alfred Burgoon, JR., Shinya Iimura, Ramanaiah C. Kanamarlapudi, Qiuling Song, Wenxue Wu, Jie Yan, Haiming Zhang
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Publication number: 20090054436Abstract: The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.Type: ApplicationFiled: October 17, 2008Publication date: February 26, 2009Inventors: Robert M. Borzilleri, Lyndon A.M. Cornelius, Robert J. Schmidt, Gretchen M. Schroeder, Kyoung S. Kim
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Publication number: 20090048280Abstract: Intermediates and synthetic processes for the preparation of substituted phenylalanine-based compounds (e.g.Type: ApplicationFiled: December 28, 2006Publication date: February 19, 2009
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Publication number: 20090047252Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: June 26, 2008Publication date: February 19, 2009Applicant: Gilead Sciences, Inc.Inventors: Zhenhong R. Cai, Aesop Cho, Choung U. Kim, Jie Xu
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Publication number: 20090029994Abstract: The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted phenyl group, and the like; R1 is an optionally substituted alkyl group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.Type: ApplicationFiled: July 28, 2008Publication date: January 29, 2009Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Yoshinori Nakamura, Norimitsu Hayashi, Takanori Higashijima, Hitoshi Kubota, Kozo Oka
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Patent number: 7479495Abstract: N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I: Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-? expression utilizing compounds of the present invention are also disclosed.Type: GrantFiled: June 2, 2005Date of Patent: January 20, 2009Assignees: Pharmacopeia, Inc., Bristol-Myers Squibb CompanyInventors: Kevin Joseph Moriarty, Yvonne Shimshock, Gulzar Ahmed, Junjun Wu, James Wen, Wei Li, Shawn David Erickson, Jeffrey John Letourneau, Edward McDonald, Katerina Leftheris, Stephen T. Wrobleski, Zahid Hussain, Ian Henderson, Axel Metzger, John J. Baldwin, Alaric J. Dyckman
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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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Publication number: 20080318985Abstract: This invention relates to novel compounds having the structural formula Ia or Ib below: (Ia); (Ib) 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: December 25, 2008Applicants: AstraZeneca AB, Astex Therapeutics LimitedInventors: Jeffrey Albert, Phil Edwards, James Empfield
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Patent number: 7468243Abstract: Nucleic acid labeling compounds are disclosed having the formula: These compounds are useful for attaching a detectable label to a nucleic acid.Type: GrantFiled: March 12, 2002Date of Patent: December 23, 2008Assignee: Affymetrix, Inc.Inventors: Glenn McGall, Anthony D. Barone
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Publication number: 20080287427Abstract: The invention relates to compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising en a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.Type: ApplicationFiled: September 14, 2005Publication date: November 20, 2008Inventors: Guido Bold, Hans-Georg Capraro, Giorgio Caravatti, Andreas Floersheimer, Pascal Furet, Paul W. Manley, Andreas Vaupel, Carole Pissot Soldermann, Francois Gessier, Christian Schnell, Amanda Jane Littlewood-Evans, Prasad Koteswara Kapa, Joginder S. Bajwa, Xinglong Jiang
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Patent number: 7442705Abstract: 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: October 28, 2008Assignee: Tibotec Pharmaceuticals LtdInventors: 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, legal representative, Paul Adriaan Jan Janssen
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Publication number: 20080255164Abstract: 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: October 16, 2008Applicant: ASTRAZENECA ABInventors: Jeffrey Albert, Donald Andisik, Phil Edwards, Mark Sylvester
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Publication number: 20080255167Abstract: This invention relates to novel compounds having the structural formula I below 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: October 16, 2008Inventors: Jeffrey Albert, Gianni Chessari, Phil Edwards
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Patent number: 7429594Abstract: The present invention relates to compounds having the general formula or a pharmaceutically acceptable salt thereof, wherein R1 is a saturated or unsaturated 5-, 6- or 7-membered, ring containing 0, 1, 2 or 3 atoms selected from N, O and S, wherein the ring may be fused with a benzo group, and is substituted by 0, 1 or 2 oxo groups, and wherein R1 is additionally substituted; and R2 is a substituted C1-6alkyl. Also included is a method of prophylaxis or treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ? cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs.Type: GrantFiled: August 20, 2004Date of Patent: September 30, 2008Assignee: Amgen Inc.Inventors: Longbin Liu, Patricia Lopez, Manoj Bajpai, Aaron C. Siegmund
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Patent number: 7427681Abstract: This invention describes novel pyrazole compounds of formula II: wherein Z1 is nitrogen or CR8; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and Ry, R2, and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: February 10, 2004Date of Patent: September 23, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Françoise Pierard
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Patent number: 7423148Abstract: 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: GrantFiled: November 21, 2003Date of Patent: September 9, 2008Assignee: Chiron CorporationInventors: John N. Nuss, Sabina Pecchi, Paul A. Renhowe
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Publication number: 20080214544Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as c-met mediated diseases and/or HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: December 19, 2007Publication date: September 4, 2008Applicant: Amgen Inc.Inventors: Steven Bellon, Shon Booker, Noel D'Angelo, Ingrid M. Fellows, Jean-Christophe Harmange, Tae-Seong Kim, Matthew Lee, Longbin Liu, Mark H. Norman
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Patent number: 7414011Abstract: Disclosed are compounds of the formula (I) or salts thereof in which R1, R2, R3, R4, I, R5, Q, R4, W, X, Y, V and Z, are as defined in the specification, which are suitable for use as herbicides or plant growth regulators. Also disclosed are processes for preparing the compounds of formula (I) or salts thereof.Type: GrantFiled: September 12, 2005Date of Patent: August 19, 2008Assignee: Hoechst Schering Agrevo GmbHInventors: Hansjörg Dietrich, Christian Waldraff, Lothar Willms, Hermann Bieringer, Christopher Rosinger, Felix Thürwächter, Thomas Auler
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Publication number: 20080194545Abstract: The present invention is directed to compounds of formula I, pharmaceutical compositions comprising the compounds, and methods for making and using the inventive compounds.Type: ApplicationFiled: February 7, 2008Publication date: August 14, 2008Applicant: TRIUS THERAPEUTICSInventors: Xiaoming Li, John M. Finn, Mark T. Hilgers
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Publication number: 20080171878Abstract: This invention relates to a process for preparing 4-[(1,6-dihydro-6-oxo-2-pyrimidinyl)-amino]benzonitrile (I) starting from a 4-oxo-1,6-dihydro-pyrimidinylcarboxylic acid ester (II) or starting from a guanidine derivative which is reacted with an alkoxy-methylene malonic acid ester to an ester (II) which is converted to (I), which reaction sequence may be a one-pot procedure.Type: ApplicationFiled: May 24, 2006Publication date: July 17, 2008Inventors: Didier Philippe Robert Schils, Alfred Elisabeth Stappers
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Publication number: 20080167330Abstract: The invention relates to carbamoylsulphoximides as protein kinase inhibitors of the general formula 1.Type: ApplicationFiled: August 28, 2007Publication date: July 10, 2008Inventors: Ulrich Luecking, Gerhard Siemeister, Rolf Jautelat
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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