At 4- Or 6-position Patents (Class 544/326)
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Publication number: 20090082567Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: August 27, 2008Publication date: March 26, 2009Inventors: Rajinder Singh, Ankush Argade, Donald Yayan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
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Publication number: 20090076047Abstract: 2-Substituted pyrimidines of the formula I, where the indices and substituents are as defined in the description.Type: ApplicationFiled: September 21, 2006Publication date: March 19, 2009Inventors: Joachim Rheinheimer, Thomas Grote, Bernd Muller, Jan Klaas Lohmann, Wassilios Grammenos, Udo Hunger, Frank Schieweck, Sarah Ulmschneider, Jochen Dietz, Jens Renner, John-Bryan Speakman, Maria Scherer, Siegfried Strathmann, Reinhard Stierl
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Publication number: 20090054647Abstract: Disclosed a method for preparing a compound of Formula 1, wherein R1 is cyclopropyl, 4-chlorophenyl or 4-bromophenyl; and R2 is C1-C14 alkyl; comprising contacting a compound of Formula 2 with a persulfate oxidant in the presence of a strong sulfur- or phosphorus-containing mineral acid and an oxidation resistant solvent. Also disclosed are methods for preparing the compound of Formula 2 from a compound of Formula 5 as well as compounds of Formula 6 and salts thereof, wherein R is NH2, Cl or OH; X is H or Cl; R1 is cyclopropyl, 4-chlorophenyl or 4-bromophenyl; and R2 is C1-C14 alkyl; provided that when R is NH2 or Cl, then X is Cl; which are useful a process intermediates.Type: ApplicationFiled: May 12, 2006Publication date: February 26, 2009Inventor: Gary David Annis
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Publication number: 20090036420Abstract: The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.Type: ApplicationFiled: July 28, 2008Publication date: February 5, 2009Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20090036448Abstract: The present invention encompasses novel substituted pyrimidine compounds of Formula (I): which act as MCH receptor antagonists. These compounds are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction.Type: ApplicationFiled: March 29, 2005Publication date: February 5, 2009Applicants: TAISHO PHARMECUTICAL CO., LTD., ARENA PHARMACEUTICALS, INC.Inventors: Yoshinori Sekiguchi, Kosuke Kanuma, Katsunori Omodera, Thuy-Anh Tran, Graeme Semple, Bryan A. Kramer
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Patent number: 7485641Abstract: The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, n and R2 are as described herein; compositions thereof; and uses thereof.Type: GrantFiled: June 18, 2007Date of Patent: February 3, 2009Assignee: Pfizer, Inc.Inventors: David W. Piotrowski, Yu Hui, John W. Benbow
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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: 7482351Abstract: The present disclosure provides 4-pyrimidineamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferative diseases such as tumorigenic cancers.Type: GrantFiled: June 29, 2005Date of Patent: January 27, 2009Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, David Carroll, Tarikere Gururaja, Taisei Kinoshita
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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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Publication number: 20090005560Abstract: The present invention relates to a novel production method of a diaminopyrimidine compound useful as an intermediate for various compounds having a pharmacological activity, a novel intermediate useful for producing said compound, and a production method of the intermediate. The present invention provides a novel 5-aminopyrimidine compound represented by the following formula (2) and a novel 4,5-diaminopyrimidine compound represented by the formula (3), as well as production methods of the compounds of the following formulas (2) to (6). wherein each symbol is as defined in the specification.Type: ApplicationFiled: June 27, 2008Publication date: January 1, 2009Applicant: AJINOMOTO CO. INCInventors: Sachiko OKA, Daisuke TAKAHASHI, Kunisuke IZAWA
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Publication number: 20080312237Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: July 18, 2008Publication date: December 18, 2008Inventors: Michael G. Kelly, Satyanarayana Janagani, Ravindra B. Upasani
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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: 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: 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: 7439358Abstract: The present invention relates to a specific salt of a dihydropteridione derivative, namely the trihydrochloride salt of the compound N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide, to its crystallisation in the form of an hydrate with water, to a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.Type: GrantFiled: January 30, 2007Date of Patent: October 21, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Guenter Linz, Peter Sieger, Matthias Grauert, Rolf Schmid
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Publication number: 20080249304Abstract: The present invention is directed to a process for chemoselective substitution on a halopyrimidine carboxaldehyde having multiple reactive sites and subsequent stereoselective oxime formation.Type: ApplicationFiled: June 21, 2007Publication date: October 9, 2008Inventors: Hongfeng Chen, Peter J. Connolly, Kirk L. Sorgi, Anusuya Choudhury, Christopher N. Nilsen
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Publication number: 20080242861Abstract: This invention relates to methods of preparing the compounds of formula (V): Each variable in this formula is defined in the specification.Type: ApplicationFiled: April 2, 2007Publication date: October 2, 2008Inventors: Chi-Feng Yen, Chang-Pin Huang, Cheng-Kung Hu, Ming-Chen Chou, Chi-Hsin Richard King
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Publication number: 20080242863Abstract: The present invention relates to a novel process for the manufacture of Grewe-diamine comprising the following step: hydrolyzing a compound of formula (II), wherein R is hydrogen or straight- or branched chain C1-4 alkyl, with an aqueous alkali or alkaline-earth metal hydroxide solution, characterized in that the hydrolysis is carried out in the presence of an organic solvent.Type: ApplicationFiled: January 24, 2006Publication date: October 2, 2008Inventors: Werner Bonrath, Jocelyn Fischesser, Lisa Giraudi, Reinhard Karge
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Patent number: 7419984Abstract: The invention relates to pyrimidines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase ? (LPAAT-?) activity and/or proliferation of cells such as tumor-cells.Type: GrantFiled: September 24, 2003Date of Patent: September 2, 2008Assignee: Cell Therapeutics, Inc.Inventors: Rama Bhatt, Baoqing Gong, Feng Hong, Scott A Jenkins, J Peter Klein, Cory T Kohm, John Tulinsky
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Publication number: 20080176744Abstract: The invention relates to the use of 4-aminopyrimidines of formula (I), in which R1?H, halogen, cyano, alkyl, alkylhalide, alkenyl, alkinyl, cycloalkyl, alkoxy, alkoxyalkyl, benzyloxyalkyl, alkoxyalkenyl or alkoxyalkinyl, R2?H, halogen, cyano, alkyl, alkylhalide, alkenyl, alkinyl, cycloalkyl, alkoxy, alkoxyalkyl and alkylthioalkyl, whereby the hydrocarbon chain in R1 and/or R2 can be substituted as given in the description, R1 and R2 can form, together with the carbon atom to which they are bonded, a 5-7-membered ring which can contain one to three same or different heteroatoms selected from the group O, N or S, R3?H, halogen, cyano, hydroxy, mercapto, azido, alkyl, alkenyl, alkinyl, alkylhalide, —O-D, —S(O)m-D, ON?CRaRb, CRc?NORa, NRcN?CRaRb, NRaRb, NRcNRaRb, NORa, NRcC(?NRc)NRaRb, NRcC(?O)NRaRb, NRaCN, —NRaC(?O)Rc, NRaC(?NORc)Rc?, OC(?O)Ra, C(?NORc)NRaRb, CRc(?NNRaRb), C(?O)NRaRb, C(?O)Ra, CO2Ra, C(?O)NRzRb, C(?O)—N—ORb, C(?S)—NRzRb, C(?O)NRa—NRzRb, C(?N—NRzRc)NRaRb, C(?NORb)Ra, C(?N—NRzRb)Ra, CRaRb—ORz, CRaType: ApplicationFiled: March 8, 2006Publication date: July 24, 2008Applicant: BASF AktiengesellschaftInventors: Anja Schwogler, Joachim Rheinheimer, Wassilios Grammenos, Thomas Grote, Udo Hunger, Bernd Muller, Peter Schafer, Frank Schieweck
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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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Publication number: 20080125417Abstract: 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 Formula 1, 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: ApplicationFiled: September 11, 2007Publication date: May 29, 2008Inventors: Kevin S. Currie, Tony Lee, James W. Darrow, Peter A. Blomgren
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Patent number: 7335654Abstract: PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.Type: GrantFiled: August 8, 2003Date of Patent: February 26, 2008Assignee: Memory Pharmaceuticals CorporationInventors: Allen T. Hopper, Ruiping Liu
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Publication number: 20080039447Abstract: This invention relates to pyrimidine derivatives of general formula I in which R1, R2, X, A and B have the meanings that are contained in the description, as inhibitors of the cyclin-dependent kinases, their production as well as their use as medications for treating various diseases.Type: ApplicationFiled: June 26, 2007Publication date: February 14, 2008Inventors: Thomas Brumby, Rolf Jautelat, Olaf Prien, Martina Schafer, Gerhard Siemeister, Ulrich Lucking, Christoph Huwe
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Patent number: 7326715Abstract: Disclosed herein are 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives having Formula I, wherein each of the substituents is given the definition as set forth in the specification and claims; or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions comprising these 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives and use of these 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives for the treatment of cathepsin K and cathepsin S related disorders, e.g. osteoporosis, atherosclerosis, inflammation and immune disorders such as rheumatoid arthritis and chronic pain.Type: GrantFiled: September 21, 2006Date of Patent: February 5, 2008Assignee: N.V. OrganonInventors: Zoran Rankovic, Jiaqiang Cai
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Publication number: 20080027076Abstract: The invention relates to a compound of the Formula (I); or salt thereof, wherein R1, R2, R3, R4, R5, R6, A, B, L, n and m are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm blooded animal. The invention also relates to processes for the preparation of said compounds.Type: ApplicationFiled: December 20, 2004Publication date: January 31, 2008Applicant: ASTRAZENECA ABInventors: Clifford David Jones, Richard William Arthur Luke, William McCoull
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Publication number: 20080015185Abstract: 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: ApplicationFiled: July 16, 2007Publication date: January 17, 2008Inventors: Gulzar Ahmed, Axel Metzger, Ian Henderson, David J. Diller, Jun Wen, Stephen T. Wrobleski, Katerina Leftheris, Chunjian Liu
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Patent number: 7319100Abstract: Compounds provided herein are novel substituted pyrazinones, pyridines and pyrimidines of Formula (I) and (II): Such compounds are particularly useful as CRF receptor ligands, and hence, in the treatment of various neurologically-related disorders such as affective disorder, anxiety and depression.Type: GrantFiled: February 14, 2007Date of Patent: January 15, 2008Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Argyrios G. Arvanitis, Paul J. Gilligan, Richard A. Hartz
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Patent number: 7309704Abstract: The present invention relates to compounds represented by the structural Formula I: or a pharmaceutically acceptable salt thereof, which are useful for the treatment of metabolic and eating disorders such as obesity and hyperphagia, and for the treatment of diabetes and associated disorders.Type: GrantFiled: August 24, 2005Date of Patent: December 18, 2007Assignee: Schering CorporationInventors: Andrew Stamford, Youhao Dong, Stuart W. McCombie, Yusheng Wu
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Patent number: 7300907Abstract: 6-Amino-5-halo-4-pyrimidinecarboxylic acids having poly-substituted aryl substituents in the 2-position, and their amine and acid derivatives, are potent herbicides demonstrating a broad spectrum of weed control.Type: GrantFiled: January 12, 2007Date of Patent: November 27, 2007Assignee: Dow Agrosciences LLCInventors: Jeffrey B. Epp, James M. Ruiz, Paul R. Schmitzer, Terry W. Balko, Thomas L. Siddall, Carla N. Yerkes
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Patent number: 7291730Abstract: Pyrimidine compounds of formula (1): wherein R1 is C3-C7 alkynyl optionally substituted with halogen; R2 and R3 are independently hydrogen or the like; and R4 is C3-C7 alkynyloxy optionally substituted with halogen, optionally substituted phenyl, or the like have an excellent pesticidal effect.Type: GrantFiled: October 15, 2004Date of Patent: November 6, 2007Assignee: Sumitomo Chemical Company, LimitedInventors: Hajime Mizuno, Noriyasu Sakamoto, Yoshiharu Kinoshita
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Patent number: 7253174Abstract: 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: July 12, 2006Date of Patent: August 7, 2007Assignees: Bristol-Myers Squibb Company, Pharmacopeia, Inc.Inventors: Gulzar Ahmed, Axel Metzger, Ian Henderson, David J. Diller, Jun Wen, Stephen T. Wrobleski, Katerina Leftheris, Chunjian Liu
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Publication number: 20070167413Abstract: The present invention relates to novel heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof. The present invention more particularly provides novel hetereocycles of the general formula (I).Type: ApplicationFiled: December 4, 2006Publication date: July 19, 2007Applicant: ORCHID RESEARCH LABORATORIES LIMITED.Inventors: Akella Satya Surya Visweswara Srinivas, Ravikumar Tadiparthi, Ganapavarapu Veera Raghava Sharma, Sappanimuthu Thirunavukkarasu, Durairaj Peter Bhakiaraj, Virendra Kachhadia, Kilambi Narsimhan, Sathya Narayana Thara, Sriram Rajagopal, Gaddam Om Reddy, Sukunath Narayanan, Venkatesan Parameswaran, Venkatesan Janarthanam
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Patent number: 7226927Abstract: The present invention is directed to substituted 2-aryl-4-arylaminopyrimidine and analogs thereof, represented by the general Formula I: wherein A, Ar1, Ar2, R1 and R3 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. The compounds of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: November 10, 2003Date of Patent: June 5, 2007Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, John A Drewe, P. Sanjeeva Reddy, Bao Nguyen, Azra Pervin
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Patent number: 7208499Abstract: The present invention relates to a compound of the formula 1 wherein A and Ar are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: May 6, 2005Date of Patent: April 24, 2007Assignee: Pfizer Inc.Inventors: John Charles Kath, Michael Joseph Luzzio
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Patent number: 7205306Abstract: Compounds provided herein are novel substituted pyrazinones, pyridines and pyrimidines of Formula (I) and (II): Such compounds are particularly useful as CRF receptor ligands, and hence, in the treatment of various neurologically-related disorders such as affective disorder, anxiety and depression.Type: GrantFiled: May 14, 2002Date of Patent: April 17, 2007Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Argyrios G Arvanitis, Paul J Gilligan, Richard A Hartz
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Patent number: 7205297Abstract: The present invention relates to a series of novel substituted 5-alkynyl pyrimidines, pharmaceutical compositions which contain them, methods for their preparation, and their use in therapy, particularly in the treatment of neurodegenerative or other neurological disorders of the central and peripheral nervous systems, including age related cognitive disorders such as senility and Alzheimer's disease, nerve injuries, peripheral neuropathies, and seizure disorders such as epilepsy.Type: GrantFiled: July 20, 2001Date of Patent: April 17, 2007Assignee: Krenitsky Pharmaceuticals, Inc.Inventors: Lilia M. Beauchamp, Thomas A. Krenitsky, James L. Kelley
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Patent number: 7189729Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, EGF-R, c-erbB2 kinase (HER-2), CHK2, FGFR3, p70S6K, PKC, PDGF-R, p38, TGF?, KDR, c-Kit, b-RAF, c-RAF, FLT1 and/or FLT4 kinases.Type: GrantFiled: September 30, 2004Date of Patent: March 13, 2007Assignee: IRM LLCInventors: Greg Chopiuk, Pascal Furet, Nathanael Schiander Gray, Patricia Imbach, Yi Liu, Joseph Schoepfer, Ruo Steensma
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Patent number: 7176312Abstract: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.Type: GrantFiled: October 12, 2002Date of Patent: February 13, 2007Assignees: The Scripps Research Institute, IRM LLCInventors: Sheng Ding, Qiang Ding, Nathanael S. Gray
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Patent number: 7157462Abstract: A compound of formula: wherein Ar, Ar1, Ar2, R3–R6, R13, m, and t are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Hydroxyiminopiperazine Compound”); compositions comprising an effective amount of a Hydroxyiminopiperazine Compound; and methods for treating or preventing pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Hydroxyiminopiperazine Compound are disclosed.Type: GrantFiled: September 23, 2003Date of Patent: January 2, 2007Assignee: Euro-Celtique S.A.Inventors: Qun Sun, Xiaoming Zhou
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Patent number: 7125881Abstract: The present invention therefore provides use of a compound of formula (I) and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases associated with Cathepsin S.Type: GrantFiled: June 23, 2003Date of Patent: October 24, 2006Assignee: AstraZeneca ABInventors: Andrew Bailey, Garry Pairaudeau, Anil Patel, Stephen Thom
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Patent number: 7115599Abstract: This invention relates to compounds of the formula in which R1, R2, and R3 are as defined in the claims, to a process for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods of using such compounds for treatment of hypertension and sexual dysfunction.Type: GrantFiled: November 12, 2001Date of Patent: October 3, 2006Assignee: Bayer AktiengesellschaftInventors: Johannes-Peter Stasch, Achim Feurer, Stefan Weigand, Elke Stahl, Dietmar Flubacher, Cristina Alonso-Alija, Frank Wunder, Dieter Lang, Klaus Dembowsky, Alexander Straub, Elisabeth Perzborn
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Patent number: 7112589Abstract: The invention provides compounds of formula I or a pharmaceutically acceptable salt or ester thereof (I), wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g.Type: GrantFiled: August 29, 2002Date of Patent: September 26, 2006Assignee: Novartis AGInventors: Eva Altmann, Kenji Hayakawa, Genji Iwasaki
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Patent number: 7112676Abstract: Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and FGFR kinases and are selective against LCK. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.Type: GrantFiled: October 20, 2003Date of Patent: September 26, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Apostolos Dermatakis, Marek Michal Kabat, Kin-Chun Luk, Pamela Loreen Rossman, Sung-Sau So
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Patent number: 7067522Abstract: Pyrimidine derivatives of formula (I) wherein Q1, Q2, G and R1 are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) and focal adhesion kinase (FAK) inhibitors are also described.Type: GrantFiled: November 24, 2004Date of Patent: June 27, 2006Assignee: AstraZeneca ABInventors: Elizabeth Janet Pease, Emma Jane Williams, Robert Hugh Bradbury, Stuart Eric Pearson
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Patent number: 7034019Abstract: The present invention concerns compounds of formula (A1)(A2)N—R1 (I),the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 is substituted C1-6alkyl; —S(?O)—R8; —S(?O)2—R8; C7-12alkylcarbonyl; optionally substituted C1-6alkyloxycarbonylC1-6alkylcarbonyl; with R8 being C1-6alkyl, aryl1 or Het1; (A1)(A2)N— is the covalently bonded form of the corresponding intermediate of formula (A1)(A2)N—H, which is a HIV replication inhibiting pyrimidine of formulaType: GrantFiled: May 3, 2001Date of Patent: April 25, 2006Assignee: Janssen Pharmaceutica N.V.Inventors: Michael Joseph Kukla, Donald William Ludovici, Robert William Kavash, Bart Lieven Daniel De Corte, Jan Heeres, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Marc René de Jonge, Koen Jeanne Alfons Van Aken, Alain Krief
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Patent number: 6958340Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.Type: GrantFiled: July 26, 2002Date of Patent: October 25, 2005Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, Peter J. Manley, Adrienne Balitza, George D. Hartman, Leonard Rodman
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Patent number: 6953802Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a 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: July 20, 2001Date of Patent: October 11, 2005Assignees: 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. Grant, Christopher Semko, Ying-Zi Xu
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Patent number: 6949551Abstract: Dihalopropene compounds, process for their preparation, compositions comprising them and their use as pesticides What is described are dihalopropene compounds of the formula (I) in which R1 and R2 are halogen, Y is —O—, —S— or —NH—, X is —O—, —S(O)r— or —NR5— (where r=0, 1, 2 and R5 is hydrogen or C1-C8-alkyl), X? is a direct C—C bond, —O—, —S(O)r— or —NR5— (where R5 is as defined above), R3 is hydrogen, halogen, nitro, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy, C1-C8-haloalkoxy, C3-C10-cycloalkyl or has one of the meanings defined for A, A has the meaning given in the description (inter alia aryl, heterocyclyl), B is a divalent bridge having the meanings given in the description (inter alia alkylene) and R4 is a monovalent C6-C14-aryl radical or nitrogen-containing heteroaryl radical having at least one ring heteroatom which has the meanings given in the description. These compounds can be used for preparing pesticides.Type: GrantFiled: November 7, 2002Date of Patent: September 27, 2005Assignee: Bayer Cropscience S.A.Inventors: Jörg Tiebes, Ralf Braun, Joachim Dickhaut, Harald Jakobi, Stephen Lindell, Vincent L. Salgado, Eva Wojtech, Daniela Jans, Jutta Maria Waibel, Waltraud Hempel, Ronald Wilhelm