Carbocyclic Ring Containing Patents (Class 544/321)
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Publication number: 20110294838Abstract: The invention relates to sulfoximine-substituted anilino-pyrimidine derivatives of formula (I). methods of production thereof, and use thereof as medication for the treatment of various diseases.Type: ApplicationFiled: October 9, 2009Publication date: December 1, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Ulrich Lücking, Rolf Jautelat, Gerhard Siemeister, Julia Schulze, Philip Lienau
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Publication number: 20110288054Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: ApplicationFiled: September 22, 2009Publication date: November 24, 2011Applicant: Schering CorporationInventors: Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K.C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
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Publication number: 20110288071Abstract: The present invention encompasses compounds of general formula (1) wherein A, B, X, R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: November 24, 2009Publication date: November 24, 2011Applicant: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Ioannis Sapountzis
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Publication number: 20110288109Abstract: The present invention includes compounds of general Formula (1), wherein A, X, R1 and R2 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: November 24, 2009Publication date: November 24, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Heinz Stadtmueller, Bodo Betzemeier, Ioannis Sapountzis
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Patent number: 8063057Abstract: Compounds of formulae I and II are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and manage serotonin-mediated diseases and disorders:Type: GrantFiled: March 30, 2010Date of Patent: November 22, 2011Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Arokiasamy Devasagayaraj, Haihong Jin, Brett Marinelli, Lakshama Samala, Zhi Cai Shi, Ashok Tunoori, Ying Wang, Chengmin Zhang
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Publication number: 20110281899Abstract: The present invention provides methods and therapeutic agents for lowering or increasing serum serotonin levels in a patient in order to increase or decrease bone mass, respectively. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis and the agents are TPH1 inhibitors or serotonin receptor antagonists.Type: ApplicationFiled: November 13, 2009Publication date: November 17, 2011Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Gerard Karsenty, Patricia F. Ducy, Vijay Kumar Yadav, Donald Landry, Shi-Xian Deng
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Publication number: 20110281873Abstract: Disclosed herein are pyrimidinyl compounds that are contemplated to be modulators of cystic fibrosis transmembrane regulators (CFTR), and methods of making and using same. Also provided are pharmaceutical compositions and methods of treating disorders associated with cystic fibrosis transmembrane regulators, such as airway inflammation, cystic fibrosis, and the like.Type: ApplicationFiled: December 11, 2009Publication date: November 17, 2011Inventors: Phoebe Chiang, Shomir Ghosh
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Publication number: 20110275611Abstract: The invention is directed to 6-(4-pyrimidinyl)-1H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R1-R4 are defined herein. The compounds of the invention axe inhibitors of PDK1 and can be useful in the treatment of immune and metabolic diseases and disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention.Type: ApplicationFiled: November 18, 2009Publication date: November 10, 2011Inventors: Jeffrey Michael Axten, Charles William Blackledge, JR., Gerald Patrick Brady, JR., Yanhong Feng, Seth W. Grant, Jesus Raul Medina, William H. Miller, Stuart P. Romeril
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Publication number: 20110275812Abstract: In one embodiment the present invention encompasses 4-(2,6-dichloropyrimidin-4-yloxy)-3,5-dimethylbenzonitrile (“ETHER”), 4-(4,6-dichloropyrimidin-2-yloxy)-3,5-dimethyl-benzonitrile (“ETHER C-2 isomer”), mixtures and salts thereof of. The present invention encompasses the use of ETHER and salts thereof to prepare Etravirine and Etravirine intermediates, and salts thereof. In another embodiment the present invention encompasses the use of ETHER and salts thereof to prepare debrometravirine (“DEBETV”) and salts thereof. In yet another embodiment the present invention encompasses the use of ETHER and salts thereof to prepare 4-(6-chloro-2-(4-cyanophenylamino)pyrimidin-4-yloxy)-3,5-dimethyl-benzonitrile (“ARCPBN”) and salts thereof. The compound, 4-(2,6-dichloropyrimidin-4-yloxy)-3,5-dimethylbenzonitrile “ETHER” of formula (A) wherein n is either 0 or 1 and HA is an acid.Type: ApplicationFiled: July 27, 2010Publication date: November 10, 2011Inventors: Irena Krizmanic, Jasna Dogan, Marina Marinkovic, Maja Sepelj
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Publication number: 20110263625Abstract: This invention concerns the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently is hydroxy, halo, optionally substituted C3-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkylamino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substitutType: ApplicationFiled: July 6, 2011Publication date: October 27, 2011Inventors: Bart De Corte, Marc René de Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken, Koenraad Jozef Lodewijk Marcel Andries, Frank Xavier Jozef Herwig Arts
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Publication number: 20110257152Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.Type: ApplicationFiled: April 14, 2011Publication date: October 20, 2011Applicant: ABBOTT LABORATORIESInventors: Thomas D. Penning, Keith W. Woods, Chunqiu Lai, Yunsong Tong, Alan S. Florjancic
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Publication number: 20110245205Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.Type: ApplicationFiled: December 15, 2010Publication date: October 6, 2011Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Sathesh Bhat, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Jean-Francois Fournier, Jacques Yves Gauthier, Jonathan Grimm, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Matthew L. Maddess, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Alessia Petrocchi, Michael H. Reutershan, Joel S. Robichaud, Eric Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hyun Chong Woo, Hua Zhou
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Publication number: 20110237598Abstract: The present invention encompasses compounds of general formulae (1a) and (1b) wherein the groups R1 to R5, A, Q, m, n, p and q are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use as medicaments.Type: ApplicationFiled: September 29, 2010Publication date: September 29, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Heinz Stadtmueller, Ioannis Sapountzis
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Publication number: 20110237576Abstract: The present invention provides a compound which has an effect of inhibiting amyloid-? production and is useful as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-? proteins. The present invention relates to a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein A is optionally substituted carbocyclic diyl or optionally substituted heterocyclic diyl; B is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is a group such as optionally substituted lower alkyl; R2 is a group such as hydrogen; and R3a and R3b are each independently a group such as hydrogen, provided that the following compound is excluded.Type: ApplicationFiled: October 22, 2009Publication date: September 29, 2011Applicant: SHIONOGI & CO., LTD.Inventors: Shuji Yonezawa, Yuusuke Tamura, Yuuji Kooriyama, Gaku Sakaguchi
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Patent number: 8026247Abstract: The invention relates to compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising 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: GrantFiled: September 14, 2005Date of Patent: September 27, 2011Assignee: Novartis AGInventors: Guido Bold, Hans-Georg Capraro, Giorgio Caravatti, Andreas Floersheimer, Pascal Furet, Paul W. Manley, Andrea Vaupel
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Publication number: 20110229724Abstract: The present invention relates to a supramolecular compound comprising a low molecular weight, apolar compound, said low molecular weight, apolar compound having a melting point of below 45° C., a molecular weight of about 80 to about 1500 amu and a HLB-value of lower than 8, said low molecular weight, apolar compound bearing a single 4H-unit per molecule. The supramolecular compound according to the present invention may be used in coating, ink, toner, resin, lacquer, adhesive or glue compositions.Type: ApplicationFiled: July 6, 2009Publication date: September 22, 2011Inventors: Gaby Maria Leonarda Hoorne- Van Gemert, Chodorowski-Kimmès Sandrine, Janssen Henricus Marie, Meijer Egbert Willem, Bosman Anton Willem
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Patent number: 8013153Abstract: The present invention is directed to substituted pyrimidine compounds of formula (I): and forms thereof, their synthesis and use for treating a chronic or acute protein kinase mediated disease, disorder or condition.Type: GrantFiled: March 23, 2007Date of Patent: September 6, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: Jeannene Butler, Peter J. Connolly, Angel R. Fuentes-Pesquera, Lee M. Greenberger, Shenlin Huang, Kenneth R. LaMontagne, Jr., Ronghua Li, Guozhang Xu
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Patent number: 8003789Abstract: This invention concerns the use of compounds of formula the N-oxides, pharmaceutically acceptable addition salts, quaternary amines, stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl with the attached vinyl group; n is 0 to 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6, 5-membered heterocyclic ring; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or —X—R3; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl, optionally substituted amino group; Y represents hydroxy, halType: GrantFiled: October 31, 2007Date of Patent: August 23, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: Bart De Corte, Marc René de Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken, Koenraad Jozef Lodewijk Marcel Andries
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Patent number: 7998969Abstract: The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, R5a, R5b, R6a, R6b and X are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.Type: GrantFiled: December 13, 2007Date of Patent: August 16, 2011Assignee: Roche Palo Alto LLCInventors: Denis John Kestesz, Christine E. Brotherton-Pleiss, Minmin Yang
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Publication number: 20110196156Abstract: A method for synthesis of diarylpyrimidine non-nucleoside reverse transcriptase inhibitor such as etravirine is provided Typically, etravirine is synthesized by the steps of a Condensing 2,4,6-trichlorpyrimidine with 3,5-dimethyl-4-hydroxybenzonitrile to obtain compound (V), b Condensing compound (V) with 4-aminobenzonitrile to obtain compound (VI), c Ammonolysis of compound (VI) to get compound (IV), d Halogenation of compound (IV) to get etravirine.Type: ApplicationFiled: June 18, 2010Publication date: August 11, 2011Inventors: Mukund Keshav Gurjar, Golakchandra Sudarshan Maikap, Shashikant Gangaram Joshi, Devising Rameshing Pardeshi, Mangesh Gorakhanath Kamble, Samit Satish Mehta
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Publication number: 20110195979Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 and Ar are as defined in description and in claims, can be used as a medicament.Type: ApplicationFiled: February 7, 2011Publication date: August 11, 2011Inventors: Li Chen, Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Lisha Wang, Jim Zhen Wu, Wengang Yang
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Publication number: 20110130564Abstract: Intermediates and synthetic processes for the preparation of substituted phenylalanine-based compounds (e.g.Type: ApplicationFiled: February 10, 2011Publication date: June 2, 2011
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Publication number: 20110124865Abstract: Intermediates and synthetic processes for the preparation of substituted phenylalanine-based compounds are disclosed.Type: ApplicationFiled: November 18, 2010Publication date: May 26, 2011Inventors: Shinya IIMURA, Wenxue WU, Matthew Mangzhu ZHAO
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Publication number: 20110105455Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, Y, R2, R3, and Ra are defined herein.Type: ApplicationFiled: October 28, 2010Publication date: May 5, 2011Inventors: STEVEN J. COATS, Yue-Mei Zhang, Shu-Chen Lin, Li Liu, Tamara A. Miskowski, Scott L. Dax, Henry Breslin, Bart L. De Corte, Wei He
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Patent number: 7935711Abstract: HIV replication inhibitors of formula (I) a pharmaceutically acceptable addition salt; or a stereochemically isomeric form 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: GrantFiled: February 20, 2006Date of Patent: May 3, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Herman Augustinus De Kock, Piet Tom Bert Paul Wigerinck
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Patent number: 7919490Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: October 4, 2007Date of Patent: April 5, 2011Assignee: Wyeth LLCInventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
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Patent number: 7915268Abstract: The present invention provides novel purines useful for the prevention and treatment of autoimmune diseases, inflammatory diseases, mast cell mediated disease and transplant rejection.Type: GrantFiled: October 4, 2007Date of Patent: March 29, 2011Assignee: Wyeth LLCInventors: Yingchun Lu, Celia Kingsbury, Adolph Bohnstedt, Michael Ohlmeyer, Vidyadhar Paradkar
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Publication number: 20110060141Abstract: The present invention relates to a method of making pyrimidines of formula (III), wherein X1, X2, R1 and R2 have the meanings as defined herein.Type: ApplicationFiled: March 19, 2009Publication date: March 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Guenter Linz, Adil Duran, Gerd Kraemer
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Patent number: 7902187Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: August 22, 2008Date of Patent: March 8, 2011Assignee: Wyeth LLCInventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
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Patent number: 7897763Abstract: Intermediates and synthetic processes for the preparation of substituted phenylalanine-based compounds (e.g.Type: GrantFiled: October 24, 2008Date of Patent: March 1, 2011
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Publication number: 20110021491Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein X1, X2, X3, X4, Y1, Y2, A, R1, R2, R3, R4, m, n, p, and q are as defined herein, including stereoisomers, esters, 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 in a patient in need thereof.Type: ApplicationFiled: June 23, 2010Publication date: January 27, 2011Applicants: BOEHRINGER INGELHEIM INTERNATIONAL GMBH, NEUROCRINE BIOSCIENCES, INC.Inventors: Joe A. TRAN, Chen CHEN
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Publication number: 20110009369Abstract: The present invention provides pyrimidinyl compounds of formula (I) and pharmaceutically acceptable salts thereof. These compounds may be used for the inhibition of influenza. In particular, the compounds of the invention may be used for the treatment or prophylaxis of influenza A, most particularly H1N1 or H5N1 influenza. The compounds of the invention can also be used for the treatment or prophylaxis of a disease caused by Vibrio cholerae, Clostridium perfringens, Streptococcus pneumoniae, Arthrobacter sialophilus, an orthomyxovirus, a paramyxovirus, a parainfluenza virus, mumps virus, Newcastle disease virus, fowl plague virus or Sendai virus.Type: ApplicationFiled: February 4, 2009Publication date: January 13, 2011Applicant: BRITISH COLUMBIA CANCER AGENCY BRANCHInventors: Steven J. Jones, Allan Sik-Yin Lau, Jianghong An, Hing Yee Law, Chun Wai Davy Lee, Lit Man Poon
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Publication number: 20100330069Abstract: 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: ApplicationFiled: January 8, 2010Publication date: December 30, 2010Applicant: TargeGen, Inc.Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
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Publication number: 20100317524Abstract: The present invention relates to a compound of the formula (I) and/or salts thereof The compound is suitable in the field of crop protection.Type: ApplicationFiled: June 17, 2010Publication date: December 16, 2010Applicant: Bayer CropScience AGInventors: Christian Waldraff, Hansjörg Dietrich, Oswald Ort, Heinz Kehne, Martin Hills, Thomas Auler, Klaus-Helmut Müller, Dieter Feucht
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Publication number: 20100311754Abstract: Naphthalene-based compounds having linked heterocyclic and aromatic rings capable of inhibiting P38, methods for inhibiting P38 in vivo or in vitro, diagnostics for determining activity in the treatment of P38 and/or cytokine-associated conditions and methods for treating conditions associated with P38 activity or cytokine activity; more particularly naphthalene-based compounds of Formula (I) having a morpholine heterocyclic ring, and methods of use thereof.Type: ApplicationFiled: August 11, 2010Publication date: December 9, 2010Applicant: ARQULE, INC.Inventors: Mark A. Ashwell, Yanbin Liu, Syed Ali, Jason Hill, Woj Wrona
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Publication number: 20100292205Abstract: The invention pertains to pyrimidone compounds that serve as effective GSK-3 inhibitors. The invention further relates to pharmaceutical compositions and methods comprising such pyrimidone compounds; and the use of such compounds for treating certain disorders.Type: ApplicationFiled: August 13, 2007Publication date: November 18, 2010Applicant: PFIZER INC.Inventors: Bruce A. Lefker, Michael A. Brodney, Subas M. Sakya, Bruce A. Hay, Matthew D. Wessel, Edward L. Conn
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Publication number: 20100292203Abstract: 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: ApplicationFiled: January 26, 2010Publication date: November 18, 2010Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey O. Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert D. Mazzola, John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoxiang Liu, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan
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Publication number: 20100285963Abstract: The invention relates to substituted fluoroalkoxyphenylsulfonylureas of the general formula (I) in which n, A, R1, R2, R3 and R4 are as defined in the description, to their use as plant treatment agents, in particular as herbicides and fungicides, and to a process and intermediates for their preparation.Type: ApplicationFiled: July 16, 2010Publication date: November 11, 2010Inventors: Klaus-Helmut Muller, Ernst-Rudolf Gesing, Joachim Kluth, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen, Ulrike Wachendorff-Neumann
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Patent number: 7829560Abstract: 1,4 disubstituted napthylenes, of formula (I), are disclosed. These compounds may be useful in treating cell-proliferative diseases.Type: GrantFiled: July 8, 2005Date of Patent: November 9, 2010Assignee: Arqule, Inc.Inventors: Mark A. Ashwell, Yanbin Liu, Syed Ali, Jason Hill, Woj Wrona
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Publication number: 20100280054Abstract: Compounds of formulae I and II are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and manage serotonin-mediated diseases and disorders:Type: ApplicationFiled: March 30, 2010Publication date: November 4, 2010Inventors: Arokiasamy Devasagayaraj, Haihong Jin, Qingyun Liu, Brett Marinelli, Lakshama Samala, Zhi-Cai Shi, Ashok Tunoori, Ying Wang, Wenxue Wu, Chengmin Zhang, Haiming Zhang
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Patent number: 7816353Abstract: Compounds of formula III: wherein R5a, R3, X, Y, Q, R1a and R1b are as defined in the specification, pharmaceutically acceptable salts thereof, and methods of use thereof.Type: GrantFiled: October 22, 2004Date of Patent: October 19, 2010Assignee: Exelixis, Inc.Inventors: Wei Cheng, Erick Wang Co, Moon Hwan Kim, Rhett Ronald Klein, Donna T. Le, Amy Lew Tsuhako, John M. Nuss, Wei Xu
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Publication number: 20100256356Abstract: 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: ApplicationFiled: January 26, 2010Publication date: October 7, 2010Applicants: 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
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Publication number: 20100249092Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: December 29, 2009Publication date: September 30, 2010Applicant: Avila Therapeutics, Inc.Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
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Publication number: 20100234598Abstract: It is the object of the present invention a process for the preparation of 4-methyl-N3-[4-(3-pyridinyl)-2-pyrimidinyl]-1,3-benzenediamine and analogues thereof, intermediates useful for the synthesis of Imatinib, or 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide.Type: ApplicationFiled: May 20, 2010Publication date: September 16, 2010Inventors: Alessandro Falchi, Ennio Grendele, Riccardo Motterle, Mariano Stivanello
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Patent number: 7795271Abstract: Disclosed are compounds Formula I and pharmaceutically acceptable salts thereof, wherein R1, R2, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.Type: GrantFiled: May 4, 2009Date of Patent: September 14, 2010Assignee: Pharmacia CorporationInventor: Richard C. Durley
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Patent number: 7776869Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A1, A2, A3, A4, R1 and R2 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.Type: GrantFiled: October 14, 2005Date of Patent: August 17, 2010Assignee: Amgen Inc.Inventors: Stuart C. Chaffee, Brian K. Albrecht, Brian L. Hodous, Matthew W. Martin, David C. McGowan, Erin F. DiMauro, Gade Reddy, Victor J. Cee, Philip R. Olivieri, Anthony Reed, Karina Romero
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Patent number: 7767669Abstract: 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: August 8, 2008Date of Patent: August 3, 2010Assignee: Novartis AGInventors: John M. Nuss, Sabina Pecchi, Paul A. Renhowe
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Patent number: 7767670Abstract: The invention provides methods and compositions for treating conditions mediated by various kinases wherein substituted 3-carboxamido isoxazoles compounds are employed. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.Type: GrantFiled: November 15, 2004Date of Patent: August 3, 2010Assignee: Ambit Biosciences CorporationInventors: Shamal A. Mehta, Robert M. Grotzfeld, Zdravko V. Milanov, Andiliy G. Lai, Hitesh K. Patel, David J. Lockhart
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Patent number: 7737157Abstract: 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: GrantFiled: August 29, 2008Date of Patent: June 15, 2010Assignee: Hutchison MediPharma Enterprises LimitedInventors: Wei-Guo Su, Hong Jia, Rick B. Ye, Yang Sai
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Patent number: RE42015Abstract: The present invention is directed to a compound, method and composition of treating or preventing viral infections, in particular, human immunodeficiency virus (HIV) and hepatitis B virus (HBV) infections, in human patients or other animal hosts, comprising the administration of N4-acylcytosine-1,3-dioxolane and pharmaceutically acceptable salts, prodrugs, and other derivatives thereof.Type: GrantFiled: June 21, 2007Date of Patent: December 28, 2010Assignee: Pharmasset, Inc.Inventors: Kyoichi A. Watanabe, Junxing Shi, Michael J. Otto