Nitrogen Attached Directly At 2-position By Nonionic Bonding Patents (Class 544/320)
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Patent number: 8476434Abstract: The present invention relates to chemical compounds having a general formula I wherein A, B, D, E, G, H1-5 and R1-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of these kinases. For example, the compounds are capable of modulating kinase enzymes thereby influencing the process of angiogenesis and treating angiogenesis-related diseases and other proliferative disorders, including cancer and inflammation. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of protein kinases.Type: GrantFiled: November 22, 2010Date of Patent: July 2, 2013Assignee: Amgen Inc.Inventors: Stephanie D. Geuns-Meyer, Brian L. Hodous, Stuart C. Chaffee, Paul Tempest, Ning Xi, Phillip R. Olivieri, Joseph L. Kim, Steven Bellon, Xiaotian Zhu, Yuan Cheng, Brian K. Albrecht, Vinod F. Patel, Victor J. Cee, Karina Romero, Hanh Nho Nguyen, Holly L. Deak, Rebecca E. Johnson
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Publication number: 20130158021Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.Type: ApplicationFiled: October 26, 2012Publication date: June 20, 2013Applicant: Massachusetts Institute of TechnologyInventor: Massachusetts Institute of Technology
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Patent number: 8466155Abstract: 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: GrantFiled: September 29, 2010Date of Patent: June 18, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Ioannis Sapountzis
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Publication number: 20130150391Abstract: The present invention relates to compounds of Formula (I) as described herein or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof and methods of treating, or manufacture of a medicament to treat, a disease, disorder, or condition of the central nervous system, including bipolar disorder, depressive disorders, anxiety disorders, cognitive disorders, pain disorders, urogentital disorder, and epilepsy, among the other diseases, disorders or conditions discussed herein as mono-therapy or in combination with another active pharmaceutical ingredient.Type: ApplicationFiled: June 20, 2011Publication date: June 13, 2013Applicant: PFIZER INC.Inventors: Michelle Marie Claffey, Jennifer Elizabeth Davoren, John Adams Lowe, III, Robert Joseph Mather
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Publication number: 20130090326Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.Type: ApplicationFiled: October 15, 2010Publication date: April 11, 2013Applicant: Rib-X Pharmaceuticals, Inc.Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Hardwin O'Dowd, Marco DeVivo, Yanming Du, Sandra Sinishtaj, Yuanqing Tang, Brian T. Wimberly
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Publication number: 20130079518Abstract: 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: November 16, 2012Publication date: March 28, 2013Inventors: Guenter LINZ, Gerd KRAEMER, Adil DURAN
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Patent number: 8399381Abstract: The present invention provides a compound represented by the formula: wherein Q represents a fused heterocyclic group, X and Y are the same or different and each represent an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group, etc., or a salt thereof, as well as a herbicide comprising the compound or a salt thereof, which exhibits a significant effect for control of sulfonylurea herbicide-resistant weeds in paddy fields and can reduce the number of active ingredients in a combined preparation and a method of controlling sulfonylurea herbicide-resistant weeds which comprises using the same.Type: GrantFiled: February 26, 2010Date of Patent: March 19, 2013Assignee: Sumitomo Chemical Company, LimitedInventors: Yasushi Tanaka, Yukari Kajiwara, Makoto Noguchi, Takeshi Kajiwara, Takanori Tabuchi
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Patent number: 8362005Abstract: Compounds of formula (I): wherein variables B, m, n, J, R4, Ea, Eb, Ec, Re, Rf, RPG and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: August 31, 2009Date of Patent: January 29, 2013Assignee: Merk. Sharp & Dohme Corp.Inventors: Ian M. Bell, Howard G. Selnick
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Publication number: 20130018053Abstract: The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: ApplicationFiled: April 18, 2011Publication date: January 17, 2013Inventors: Changyou Zhou, Wuxin Zou, Yuxia Hua, Qun Dang
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Patent number: 8334381Abstract: 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: GrantFiled: May 20, 2010Date of Patent: December 18, 2012Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Alessandro Falchi, Ennio Grendele, Riccardo Motterle, Mariano Stivanello
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Publication number: 20120316188Abstract: The present invention relates to novel compounds of Formula (I), wherein M, P, X, A and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: January 14, 2011Publication date: December 13, 2012Inventor: Christelle Boléa
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Publication number: 20120315230Abstract: The invention relates to a cosmetic composition comprising, in a cosmetically acceptable medium, a compound that can be obtained by reaction between an OH-functionalized or COOH-functionalized wax and a junction group capable of establishing hydrogen bonds with one or more partner junction groups, said junction group comprising at least one unit of formula (I) or (II): The invention also relates to a cosmetic treatment process using said compounds.Type: ApplicationFiled: December 13, 2010Publication date: December 13, 2012Applicant: L'OREALInventors: Sandrine Chodorowski-Kimmes, Nathalie Jager Lezer
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Patent number: 8324230Abstract: Crystalline forms of the p38 kinase inhibitor 3-[5-chloro-4-[(2,4-difluorobenzyl)oxy]-6-oxopyrimidin-1(6H)-yl]-N-(2-hydroxyethyl)-4-methylbenzamide is provided. Also provided are combinations and pharmaceutical compositions comprising the crystalline forms, and methods for the prophylaxis and/or treatment of a p38 kinase-mediated condition comprising administering to a subject a therapeutically effective amount of the crystalline forms.Type: GrantFiled: October 3, 2005Date of Patent: December 4, 2012Assignee: Pfizer Inc.Inventor: Jon G. Selbo
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Patent number: 8293729Abstract: 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 R1, R2, R3, n, p, q, and Ar are as defined herein, including stereoisomers, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.Type: GrantFiled: June 23, 2010Date of Patent: October 23, 2012Assignees: Boehringer Ingelheim International GmbH, Neurocrine Biosciences Inc.Inventors: Brian Dyck, Joe A. Tran, Junko Tamiya, Florence Jovic, Troy Vickers, Chen Chen, Nicole Harriott, Timothy Coon, Neil J. Ashweek
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Publication number: 20120253039Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lupus erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: ApplicationFiled: April 9, 2012Publication date: October 4, 2012Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
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Patent number: 8268849Abstract: Compositions comprising multifunctional agents and methods of use thereof are provided. Particularly, a series of analogs of 1-N, N?-dimethylsulfamoyl-4-(2-pyrimidyl)piperazine are provided which are useful for treating and/or preventing cataract, macular degeneration, neurodegenerative disorders, and/or injury or symptoms associated with radiation exposure.Type: GrantFiled: September 25, 2008Date of Patent: September 18, 2012Assignee: Board of Regents of the University of NebraskaInventors: Peter F. Kador, Hongxia Jin
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Publication number: 20120232064Abstract: Disclosed are compounds of formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R1, R2, R6, R7, R30 and R31 are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: ApplicationFiled: March 15, 2012Publication date: September 13, 2012Applicant: SCHERING CORPORATIONInventors: Yusheng Wu, Ulrich Iserloh, Jared N. Cumming, Xiaoxiang Liu, Robert D. Mazzola, Zhong-Yue Sun, Ying Huang, Andrew Stamford, Brian McKittrick, Zhaoning Zhu
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Publication number: 20120122819Abstract: The present invention includes novel compounds and pharmaceutically acceptable formulations of said compounds which exhibit antibiotic activity against microorganisms bearing a guanine riboswitch that controls the expression of the guaA gene, including organisms which are resistant to certain antibiotic families, and which are useful as antibacterial agents for treatment or prophylaxis of bacterial infections in animals or in humans, in particular but not limited to infections of the mammary gland, or their use as antiseptics, agents for sterilization or disinfection.Type: ApplicationFiled: June 14, 2010Publication date: May 17, 2012Applicant: SOCPRA - SCIENCES ET GENIE S.E.C.Inventors: Jérôme Mulhbacher, Daniel Lafontaine, François Malouin, Marianne Allard, Eric Marsault
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Patent number: 8178671Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: GrantFiled: July 30, 2004Date of Patent: May 15, 2012Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
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Patent number: 8158642Abstract: 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: October 15, 2009Date of Patent: April 17, 2012Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Christopher Michael Semko, Ying-zi Xu, Frank Stappenbeck, Jenifer Lea Smith, Kassandra Inez Rossiter, Juri Y. Fukuda, Andrei W. Konradi
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Patent number: 8133886Abstract: The invention relates to novel 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 tumor diseases.Type: GrantFiled: March 13, 2007Date of Patent: March 13, 2012Assignee: Novartis AGInventors: Guido Bold, Andrea Vaupel, Carole Pissot Soldermann, Paul W Manley
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Patent number: 8080659Abstract: The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine CXCR4 receptor for the treatment of proliferative conditions mediated by CXCR4 receptors or for the treatment of viral infections. The compounds provided interfere with the binding of SDF1 to the receptor. These compounds are particularly useful for treating or reducing the severity of hyperproliferative diseases by inhibiting metastasis, or for reducing entry of HIV in to a cell while not reducing the capacity of the stem cells to proliferate. The compounds may be useful for long term treatment regimes.Type: GrantFiled: July 11, 2007Date of Patent: December 20, 2011Assignee: Emory UniversityInventors: Dennis C. Liotta, James P. Snyder, Weiqiang Zhan
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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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Patent number: 8030487Abstract: Compounds having the general structure (A) are provided. The compounds of the invention are capable of inhibiting kinases, such as members of the Src kinase family, Vegfr and various other specific receptor and non-receptor kinases.Type: GrantFiled: July 2, 2007Date of Patent: October 4, 2011Assignee: TargeGen, Inc.Inventors: Glenn Noronha, Jianguo Cao, Colleen Gritzen, Chi Ching Mak, Andrew McPherson, Ved P. Pathak, Joel Renick, Richard M. Soll, Binqi Zeng, Elena Dneprovskaia
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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: 8022221Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.Type: GrantFiled: February 12, 2009Date of Patent: September 20, 2011Assignee: Amgen Inc.Inventors: Victor J. Cee, Holly L. Deak, Bingfan Du, Stephanie D. Geuns-Meyer, Brian L. Hodous, Hanh Nho Nguyen, Philip R. Olivieri, Vinod F. Patel, Karina Romero, Laurie Schenkel
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Patent number: 8022205Abstract: A drug is provided that is useful as a preventive or therapeutic for cancer as a result of having superior PI3K inhibitory effects as well as superior stability in the body and water-solubility. A compound, or pharmaceutically acceptable salt thereof, represented by formula (I): [wherein, X represents a single bond, etc.; Y represents a single bond, etc. (provided that X and Y are not simultaneously single bonds); Z represents a hydrogen atom, etc.; m represents an integer of 1 or 2; and R1 represents a cyclic substituent].Type: GrantFiled: August 7, 2007Date of Patent: September 20, 2011Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Nobuo Shimma, Hirosato Ebiike, Jun Ohwada, Hatsuo Kawada, Kenji Morikami, Mitsuaki Nakamura, Miyuki Yoshida, Nobuya Ishii, Masami Hasegawa, Shun Yamamoto, Kohei Koyama
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Patent number: 8013154Abstract: N-Azinyl-N?-aryl ureas and thioureas derivatives are effective at controlling insects.Type: GrantFiled: September 26, 2008Date of Patent: September 6, 2011Inventors: Noormohamed M. Niyaz, Ricky Hunter, Timothy C. Johnson, Tony K. Trullinger, Annette V. Brown, Kristy Bryan
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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: 7968559Abstract: 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: GrantFiled: April 5, 2010Date of Patent: June 28, 2011Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Arokiasamy Devasagayaraj, Haihong Jin, Zhi-Cai Shi, Ashok Tunoori, Ying Wang, Chengmin Zhang
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Patent number: 7935710Abstract: The present invention concerns the microbicidal activity of certain pyrimidine or triazine containing non-nucleoside reverse transcriptase inhibitors. The compounds of the present invention inhibit the systemic infection of a human being with HIV, in particular, the present compounds prevent sexual HIV transmission in humans.Type: GrantFiled: May 13, 2003Date of Patent: May 3, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Jens Marcel Van Roey, Marie-Pierre T.M. M. G. De Bethune, Paul Stoffels
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Patent number: 7923556Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, and solvates thereof, are useful as kinase inhibitors, wherein: two of X1, X2, and X3 are N, and the remaining one of X1, X2, and X3 is —CR1; R1 is hydrogen or —CN; and N, G, Z, R2, R3, R4, R5, and R6 are described in the specification. Also disclosed are pharmaceutical compositions containing compounds of formula (I), and methods of treating conditions associated with the activity of p38 kinase and/or conditions associated with the activity of LIM kinase.Type: GrantFiled: September 30, 2009Date of Patent: April 12, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Stephen T. Wrobleski, Shuqun Lin, Katerina Leftheris, Liqi He, Steven P. Seitz, Tai-An Lin, Wayne Vaccaro
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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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Publication number: 20110028318Abstract: There are described compounds of the formula (I) in which the respective substituents have the meanings given in the description. The compounds of the formula (I) can be used as herbicides and plant growth regulators.Type: ApplicationFiled: December 4, 2008Publication date: February 3, 2011Applicant: Bayer CropScience AGInventors: Klaus-Helmut Mueller, Ernst Rudolf Gesing, Christian Waldraff, Heînz Kehne, Dieter Feucht, Jeffrey Martin Hills, Christopher Hugh Rosinger, Jan Dittgen
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Patent number: 7880000Abstract: The present invention relates to chemical compounds having a general formula I wherein A, B, D, E, G, H1-5 and R1-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of these kinases. For example, the compounds are capable of modulating kinase enzymes thereby influencing the process of angiogenesis and treating angiogenesis-related diseases and other poliferative disorders, including cancer and inflammation. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of protein kinases.Type: GrantFiled: May 9, 2005Date of Patent: February 1, 2011Assignee: Amgen Inc.Inventors: Stephanie D. Geuns-Meyer, Brian L. Hodous, Stuart C. Chaffee, Paul A. Tempest, Philip R. Olivieri, Rebecca E. Johnson, Brian K. Albrecht, Vinod F. Patel, Victor J. Cee, Joseph L. Kim, Steven Bellon, Xiaotian Zhu, Yuan Cheng, Ning Xi, Karina Romero, Hanh Nho Nguyen, Holly L. Deak
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Patent number: 7855291Abstract: Intermediates and synthetic processes for the preparation of substituted phenylalanine-based compounds (e.g.Type: GrantFiled: December 28, 2006Date of Patent: December 21, 2010
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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: 20100292260Abstract: The invention relates to 6-vinyl pyrimidine pyrimidinone derivatives and the use thereof as medicaments in particular for the treatment of HTV infections, the use thereof for preparing pharmaceutical compositions and methods for the preparation thereof.Type: ApplicationFiled: October 13, 2006Publication date: November 18, 2010Applicant: UNIVERSITA DEGLI STUDI DE SIENAInventors: Maurizio Botta, Federico Corelli, Elena Petricci, Marco Radi, Giovanni Maga, Jose A. Este, Antonello Mai
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Patent number: 7820818Abstract: The invention provides compounds of formula I or a pharmaceutically acceptable salt or ester thereof 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. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors.Type: GrantFiled: March 6, 2009Date of Patent: October 26, 2010Assignee: Novartis AGInventors: Eva Altmann, Claudia Betschart, Kenji Hayakawa, Osamu Irie, Junichi Sakaki, Genji Iwasaki, Rene Lattmann, Martin Missbach, Naoki Teno
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Patent number: 7816526Abstract: The present invention provides a compound represented by the formula: wherein Q represents a fused heterocyclic group, X and Y are the same or different and each represent an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group, etc., or a salt thereof, as well as a herbicide comprising the compound or a salt thereof, which exhibits a significant effect for control of sulfonylurea herbicide-resistant weeds in paddy fields and can reduce the number of active ingredients in a combined preparation and a method of controlling sulfonylurea herbicide-resistant weeds which comprises using the same.Type: GrantFiled: January 15, 2003Date of Patent: October 19, 2010Assignee: Sumitomo Chemical Company, LimitedInventors: Yasushi Tanaka, Yukari Kajiwara, Makoto Noguchi, Takeshi Kajiwara, Takanori Tabuchi
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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: 7790736Abstract: 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: September 7, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Jun Feng, Stephen L. Gwaltney, II, Stephen W. Kaldor, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
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Patent number: 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: 7727996Abstract: 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: September 28, 2006Date of Patent: June 1, 2010Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Christopher Michael Semko, Ying-zi Xu, Frank Stappenbeck, Jenifer Lea Smith, Kassandra Inez Rossiter, Juri Y. Fukuda, Andrei W. Konradi
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Patent number: 7709493Abstract: 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: GrantFiled: May 20, 2009Date of Patent: May 4, 2010Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Arokiasamy Devasagayaraj, Haihong Jin, Zhi-Cai Shi, Ashok Tunoori, Ying Wang, Chengmin Zhang
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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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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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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
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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