Additional Nitrogen Containing Hetero Ring (e.g., Thiazetidine, Etc.) Patents (Class 544/111)
  • Patent number: 7666863
    Abstract: The present invention relates to benzofuran derivatives and analogs, as well as compositions containing the same and to the use thereof for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the hepatitis C virus.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: February 23, 2010
    Assignees: ViroPharma Incorporated, WYETH
    Inventors: Ashis K. Saha, Christopher J Burns, Alfred M. Del Vecchio, Thomas R. Bailey, Jason A. Reinhardt, Bheemashankar A. Kulkarni, Thomas H. Faitg, Hao Feng, Susan R. Rippin, Charles W. Blackledge, David J. Rys, Thomas A. Lessen, John Swestock, Yijun Deng, Theodore J. Nitz
  • Patent number: 7652051
    Abstract: 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: Grant
    Filed: August 24, 2005
    Date of Patent: January 26, 2010
    Assignee: TargeGen, Inc.
    Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
  • Patent number: 7652020
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-? or combinations thereof.
    Type: Grant
    Filed: June 1, 2005
    Date of Patent: January 26, 2010
    Assignee: Schering Corporation
    Inventors: Zhuyan Guo, Peter Orth, Zhaoning Zhu, Robert D. Mazzola, Tin-Yau Chan, Henry A. Vaccaro, Brian McKittrick, Joseph A. Kozlowski, Brian J. Lavey, Guowei Zhou, Sunil Paliwal, Shing-Chun Wong, Neng-Yang Shih, Pauline C. Ting, Kristin E. Rosner, Gerald W. Shipps, Jr., M. Arshad Siddiqui, David B. Belanger, Chaoyang Dai, Dansu Li, Vinay M. Girijavallabhan, Janeta Popovici-Muller, Wensheng Yu, Lianyun Zhao
  • Patent number: 7649004
    Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.
    Type: Grant
    Filed: July 12, 2005
    Date of Patent: January 19, 2010
    Assignee: Pfizer, Inc.
    Inventors: Charlotte Alice Louise Lane, Graham Nigel Maw, David James Rawson, Lisa Rosemary Thompson
  • Patent number: 7645752
    Abstract: The present invention is directed to compounds of Formula I: which are modulators of the 5-hydroxtryptamine-6 and 5-hydroxytryptamine-2A receptors and which are inhibitors of norepinephrine reuptake. The compounds of the invention, and pharmaceutical composition thereof, are useful in the treatment of disorders related to or associated with the 5-hydroxytryptamine-6 and 5-hydroxtryptamine-2A receptors or with norepinephrine reuptake inhibition.
    Type: Grant
    Filed: January 12, 2007
    Date of Patent: January 12, 2010
    Assignee: Wyeth LLC
    Inventors: Robert E. McDevitt, Yanfang Li, Albert J. Robichaud, Gavin D. Heffernan, Richard D. Coghlan, Ronald C. Bernotas
  • Patent number: 7642276
    Abstract: Compounds of formula (I): wherein A is a 5-membered heteroaryl ring are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38, such as rheumatoid arthritis.
    Type: Grant
    Filed: July 30, 2003
    Date of Patent: January 5, 2010
    Assignee: SmithKline Beecham Corporation
    Inventors: Richard Martyn Angell, Ian Robert Baldwin, Paul Bamborough, Nigel Marc Deboeck, Timothy Longstaff, Stephen Swanson
  • Patent number: 7638118
    Abstract: The present invention relates to aminoalkyl substituted fumarates and there use as malodor neutralizers.
    Type: Grant
    Filed: August 20, 2004
    Date of Patent: December 29, 2009
    Assignee: Givaudan SA
    Inventors: Felix Flachsmann, Markus Gautschi
  • Patent number: 7638513
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, aggrecanase, ADMP, LpxC, ADAMs, TACE, TNF-? or combinations thereof.
    Type: Grant
    Filed: December 1, 2005
    Date of Patent: December 29, 2009
    Assignee: Schering Corporation
    Inventors: M. Arshad Siddiqui, Umar Faruk Mansoor, Panduranga A. Reddy, Vincent S. Madison
  • Patent number: 7601751
    Abstract: There is provided a series of substituted acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, and R8 as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    Type: Grant
    Filed: August 23, 2006
    Date of Patent: October 13, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lorin A. Thompson, III, Jianliang Shi, F. Christopher Zusi, Michael F. Dee, John E. Macor
  • Patent number: 7592337
    Abstract: Tetrazole compounds substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal, obesity and other diseases.
    Type: Grant
    Filed: March 7, 2003
    Date of Patent: September 22, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Chixu Chen, Nicholas D. P. Cosford, Brian W. Eastman, Dehua Huang, Steve F. Poon, Thomas S. Reger, Jeffrey R. Roppe, Nicholas D. Smith
  • Patent number: 7589197
    Abstract: This invention relates to a method for treating inflammatory diseases or immune diseases, developmental or degenerative diseases, or tissue injuries. The method includes administering to a subject in need thereof an effective amount of one or more compounds of formula (I). Each variable in this formula is defined in the specification.
    Type: Grant
    Filed: June 13, 2006
    Date of Patent: September 15, 2009
    Assignee: Taigen Biotechnology
    Inventors: Chi-Feng Yen, Cheng-Kung Hu, Ming-Chen Chou, Chen-Tso Tseng, Chien-Huang Wu, Ying-Huey Huang, Shu-Jen Chen, Chi-Hsin Richard King
  • Patent number: 7582657
    Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritis, vitiligo, general gastrointestinal disorders, gastric ulceration, d
    Type: Grant
    Filed: December 10, 2002
    Date of Patent: September 1, 2009
    Assignee: Amgen Inc.
    Inventors: Ning Chen, Elizabeth M. Doherty, Michael G. Kelly
  • Patent number: 7576110
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Grant
    Filed: September 8, 2006
    Date of Patent: August 18, 2009
    Assignee: Abbott Laboratories
    Inventors: Marlon D. Cowart, Minghua Sun, Chen Zhao, Guo Zhu Zheng
  • Patent number: 7576083
    Abstract: The present invention is directed to morpholinyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
    Type: Grant
    Filed: April 29, 2005
    Date of Patent: August 18, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Craig W. Lindsley, Scott E. Wolkenberg, Zhijian Zhao
  • Patent number: 7572792
    Abstract: The present invention is directed to azetidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
    Type: Grant
    Filed: April 25, 2005
    Date of Patent: August 11, 2009
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Limited
    Inventors: Craig W Lindsley, David Hallett, Scott E. Wolkenberg
  • Patent number: 7572793
    Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1: wherein R1 represents a C1-C12 alkyl group which may be substituted; R represents, for example, a group represented by the following formula (II): wherein R2 and R3 independently represent a hydrogen atom or a C1-C8 alkyl group; R4 represents 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: Grant
    Filed: September 20, 2002
    Date of Patent: August 11, 2009
    Assignees: Mitsubishi Tanabe Pharma Corporation, Sanofi-Aventis
    Inventors: Fumiaki Uehara, Keiichi Aritomo, Aya Shoda, Shinsuke Hiki, Masahiro Okuyama, Yoshihiro Usui, Mitsuru Ooizumi, Kazutoshi Watanabe
  • Patent number: 7563791
    Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis.
    Type: Grant
    Filed: June 3, 2005
    Date of Patent: July 21, 2009
    Assignee: Bayer Pharmaceuticals Corporation
    Inventors: Julie A. Dixon, Catherine Brennan, Karl Miranda, Brent Chandler, Barton Phillips, Jianmei Fan, Michael Brands, Andrea McClure, Benjamin Jones, Wenlang Fu, Donald Bierer, Steven Magnuson, Harold C. E. Kluender
  • Patent number: 7563787
    Abstract: Disclosed are protein kinase inhibitors, compositions comprising such inhibitors, and methods of use thereof. More particularly, disclosed are inhibitors of Aurora A (Aurora-2) protein kinase. Also disclosed are methods of treating diseases associated with protein kinases, especially diseases associated with Aurora-2, such as cancer.
    Type: Grant
    Filed: September 29, 2006
    Date of Patent: July 21, 2009
    Assignee: Miikana Therapeutics, Inc.
    Inventors: Xiao-Yi Xiao, Dinish V. Patel, John S. Ward, Mark R. Bray, Gregory E. Agoston, Anthony M. Treston
  • Patent number: 7560546
    Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
    Type: Grant
    Filed: August 5, 2003
    Date of Patent: July 14, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, Douglas C. Beshore, Jeffrey M. Bergman, Craig W. Lindsley
  • Patent number: 7560548
    Abstract: There are provided according to the invention, novel compounds of formula (I) wherein R1, R2, R3, R4, R5, X, a, b and Z are as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.
    Type: Grant
    Filed: November 22, 2005
    Date of Patent: July 14, 2009
    Assignee: Glaxo Group Limited
    Inventors: Rachael Anne Ancliff, Simon Teanby Hodgson, Xiao Qing Lewell, Graeme Michael Robertson
  • Publication number: 20090156576
    Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
    Type: Application
    Filed: October 5, 2006
    Publication date: June 18, 2009
    Applicant: EXELIXIS INC.
    Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
  • Patent number: 7544690
    Abstract: The present invention relates to novel compounds of the formula (I) which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of obesity, obesity related disorders, anxiety, or depression.
    Type: Grant
    Filed: September 30, 2002
    Date of Patent: June 9, 2009
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Yoshinori Sekiguchi, Kosuke Kanuma, Katsunori Omodera, Thuy-Anh Tran, Bryan Aubrey Kramer, Nigel Robert Arnold Beeley
  • Patent number: 7544315
    Abstract: Photochromic h-annellated benzo[f]chromene compounds, especially photochromic compounds derived from benzo[f]chromenes, which compounds have particular long wavelength absorption maxima in their closed form and exhibit good performance in the open, colored form, so that good compatibility is achieved with indenonaphthopyrans which are diffused in phototropic glasses used in phototropic glass applications, and the use of such photochromic h-annellated benzo[f]chromene compounds in photochromic synthetic resin articles, particularly ophthalmic lenses.
    Type: Grant
    Filed: April 20, 2007
    Date of Patent: June 9, 2009
    Assignee: Rodenstock GmbH
    Inventors: Manfred Melzig, Yven Rohlfing, Udo Weigand
  • Patent number: 7538138
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salts or prodrug thereof which are useful for the modulation of the histamine-3 receptors in mammals and which are useful for the treatment of disorders ameliorated by histamine-3 receptor ligands.
    Type: Grant
    Filed: April 8, 2005
    Date of Patent: May 26, 2009
    Assignee: Abbott Laboratories
    Inventors: Marlon D. Cowart, Youssef L. Bennani, Ramin Faghih, Gregory A. Gfesser, Lawrence A. Black
  • Patent number: 7521449
    Abstract: The invention relates to compounds corresponding to formula (I): in which: Ar represents a mono- or disubstituted phenyl; R1 represents an unsubstituted or substituted phenyl; R2 represents: a pyridyl; an unsubstituted or substituted phenyl; a benzyl that is unsubstituted or substituted on the phenyl; R2 may moreover represent: a heterocyclic radical; R3 represents various values. The invention also comprises methods for the compounds preparation, formulations comprising them and therapeutic applications thereof.
    Type: Grant
    Filed: January 9, 2007
    Date of Patent: April 21, 2009
    Assignee: Sanofi-Aventis
    Inventors: Xavier Emonds-Alt, Vincenzo Proietto
  • Publication number: 20090093452
    Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein RQ, R7, n, Q2, Q3, Y, and X1-X3 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
    Type: Application
    Filed: August 24, 2007
    Publication date: April 9, 2009
    Inventors: Kenneth He Huang, Steven E. Hall, James Veal
  • Patent number: 7498329
    Abstract: This invention relates to a novel salt form of dopamine agonist 5-[(2R,5S)-5-methyl-4-propylmorpholin-2-yl]pyridin-2-amine (I): More particularly, this invention relates to 5-[(2R,5S)-5-methyl-4-propylmorpholin-2-yl]pyridin-2-amine di-(1S)-camphorsulfonate (di-S-camsylate) and to processes for the preparation of, intermediates used in the preparation of, compositions containing, and the uses of this salt.
    Type: Grant
    Filed: February 6, 2006
    Date of Patent: March 3, 2009
    Assignee: Pfizer Inc.
    Inventors: Stuart Peter Green, Olivier Alain Lazzari, Duncan Charles Miller, Fabrice Henri Salingue
  • Patent number: 7498354
    Abstract: or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of tumors and cancers.
    Type: Grant
    Filed: March 30, 2006
    Date of Patent: March 3, 2009
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Andrew Philip Crew, Bijoy Panicker, Han-Qing Dong
  • Patent number: 7498328
    Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them.
    Type: Grant
    Filed: July 17, 2006
    Date of Patent: March 3, 2009
    Assignee: Laboratorias Del Dr. Esteve, S.A.
    Inventors: Ramón Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
  • Patent number: 7488728
    Abstract: The invention relates to compounds of formula (I): wherein R, R1, R2 and X are defined herein, their preparation, and their use as pharmaceuticals.
    Type: Grant
    Filed: August 9, 2004
    Date of Patent: February 10, 2009
    Assignee: Eli Lilly and Company
    Inventors: Barry Peter Clark, Peter Thaddeus Gallagher
  • Publication number: 20090012075
    Abstract: The present invention relates to a novel class of fluorinated arylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: January 8, 2007
    Publication date: January 8, 2009
    Inventors: Thomas A. Miller, David L. Sloman, Matthew G. Stanton, Kevin J. Wilson, David J. Witter
  • Patent number: 7470685
    Abstract: This invention features pyrimidine compounds of formula (I): R1 is in which one of Ra and Rb is H or alkyl, and the other is aryl or heteroaryl optionally substituted with Rd and Rem; each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; Rd is halogen, CN, alkyl, alkyloxy, alkylcarbonyl, alkyloxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, hydroxyalkyl, alkylamino, or alkylaminocarbonyl; Re is halogen, CN, hydroxyl, alkyl, aryl, heteroaryl, alkoxyl, aryloxyl, or heteroaryloxyl; and m is 0, 1, 2, 3, or 4. The pyrimidine compounds can be used to treat an IL-12 overproduction-related disorder (e.g.
    Type: Grant
    Filed: January 21, 2005
    Date of Patent: December 30, 2008
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Mitsunori Ono, Elena Kostik, Yumiko Wada
  • Patent number: 7470681
    Abstract: This invention features pyrimidine compounds of formula (I): R1 is each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.
    Type: Grant
    Filed: July 29, 2005
    Date of Patent: December 30, 2008
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Mitsunori Ono, Teresa Przewloka, Elena Kostik, Yumiko Wada
  • Patent number: 7470795
    Abstract: Disclosed is a multi-step process for preparing a compound of Formula I: wherein R1 to R3 are as defined herein. The compounds of formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a result, these compounds are useful in the treatment of inflammatory and immune cell-mediated diseases.
    Type: Grant
    Filed: July 25, 2005
    Date of Patent: December 30, 2008
    Assignees: Boehringer Ingelheim Pharmaceuticals, Inc., Boehringer Ingelheim International GmbH
    Inventors: Xiao-jun Wang, Thomas Wirth, Thomas Nicola, Li Zhang, Rogelio Perez Frutos, Yibo Xu, Dhileepkumar Krishnamurthy, Laurence John Nummy, Richard J. Varsolona, Chris Hugh Senanayake, Jutta Kroeber, Diana Reeves
  • Patent number: 7465725
    Abstract: This invention features pyrimidine compounds of formula (I): R1 is aryl, or heteroaryl; each of R2 and R4, independently, is Rc, halogen, nitro, cyano, isothionitro, SRc, or ORc; or R2 and R4, taken together, is carbonyl; R3 is Rc, alkenyl, alkynyl, ORc, OC(O)Rc, SO2Rc, S(O)Rc, S(O2)NRcRd, SRc, NRcRd, NRcCORd, NRcC(O)ORd, NRcC(O)NRcRd, NRcSO2Rd, CORc, C(O)ORc, or C(O)NRcRd; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is O, S, S(O), S(O2), or NRc; Y is a covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and each of Rc and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.
    Type: Grant
    Filed: July 29, 2005
    Date of Patent: December 16, 2008
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Mitsunori Ono, Lijun Sun, Teresa Przewloka, Shijie Zhang, Elena Kostik, Weiwen Ying, Yumiko Wada, Keizo Koya
  • Patent number: 7465811
    Abstract: Sulfonylindoline compounds of formula I, wherein R1 through R4, Y and Z have defined meanings, a process for preparation of such compounds, and the use as pharmaceutically active substances, particularly for the treatment or inhibition of neurodegeneration, cardiovascular disease, inflammatory disease, hypercholesterolemia, dyslipidemia, obesity or diabetes.
    Type: Grant
    Filed: November 30, 2007
    Date of Patent: December 16, 2008
    Assignee: Laboratoires Fournier S.A.
    Inventors: Luc Lebreton, Christine Dumas, Christine Massardier, Michel Bondoux
  • Publication number: 20080306065
    Abstract: Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.
    Type: Application
    Filed: May 6, 2008
    Publication date: December 11, 2008
    Inventors: Anders Eriksson, Matti Lepisto, Michael Lundkvist, Magnus Munck Af Rosenschold, Pavol Zlatoidsky
  • Patent number: 7456173
    Abstract: The invention is directed to racemic and stereomerically pure compounds of Formula 3: and to pharmaceutical compositions comprising them, methods of their use, and methods of their preparation.
    Type: Grant
    Filed: October 26, 2006
    Date of Patent: November 25, 2008
    Assignee: Sepracor Inc.
    Inventors: Thomas P. Jerussi, Qun K. Fang
  • Patent number: 7452881
    Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them.
    Type: Grant
    Filed: February 16, 2007
    Date of Patent: November 18, 2008
    Assignee: Laboratories Del Dr. Esteve, S.A.
    Inventors: Ramón Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
  • Patent number: 7452879
    Abstract: 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: Grant
    Filed: October 5, 2006
    Date of Patent: November 18, 2008
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
  • Patent number: 7449457
    Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: November 11, 2008
    Assignee: Eli Lilly and Company
    Inventors: David Kent Herron, Sajan Joseph, Angela Lynn Marquart, John Joseph Masters, David Mendel, Gerald Floyd Smith, Anne Louise Tebbe, Philip Parker Waid, Michael Robert Wiley, Ying Kwong Yee
  • Patent number: 7442716
    Abstract: The invention encompasses novel compounds of Formula I or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed.
    Type: Grant
    Filed: November 23, 2005
    Date of Patent: October 28, 2008
    Assignee: Merck Frosst Canada Ltd.
    Inventors: Anh Chau, Bernard Cote, Yves Ducharme, Richard Frenette, Richard Friesen, Marc Gagnon, Andre Giroux, Evelyn Martins, Hongping Yu, Tom Wu
  • Patent number: 7425572
    Abstract: Novel dioxinoindazole compounds and dioxoloindazole compounds are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions of one or more of the compounds of the present invention.
    Type: Grant
    Filed: December 2, 2005
    Date of Patent: September 16, 2008
    Assignee: Alcon, Inc.
    Inventors: Hwang-Hsing Chen, Jesse A. May
  • Patent number: 7425555
    Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.
    Type: Grant
    Filed: April 29, 2003
    Date of Patent: September 16, 2008
    Assignee: SmithKline Beecham Corporation
    Inventors: Richard Martyn Angell, Paul Bamborough, Ian Robert Baldwin, Anne-Marie Li-Kwai-Cheung, Timothy Longstaff, Suzanne Joy Merrick, Kathryn Jane Smith, Stephen Swanson, Ann Louise Walker
  • Patent number: 7414054
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: November 15, 2005
    Date of Patent: August 19, 2008
    Assignee: Allergan, Inc.
    Inventors: Steven W. Andrews, Julie A. Wurster, Edward H. Wang, Thomas Malone
  • Patent number: 7405210
    Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants.
    Type: Grant
    Filed: May 20, 2004
    Date of Patent: July 29, 2008
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Stuart Edward Bradley, Thomas Martin Krulle, Peter John Murray, Martin James Procter, Robert John Rowley, Colin Peter Sambrook Smith, Gerard Hugh Thomas
  • Patent number: 7402579
    Abstract: The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, W, X, Z, B, L, R1, R3, R4 and R5 are substituents. The present invention also relates to methods for using such compounds.
    Type: Grant
    Filed: April 14, 2006
    Date of Patent: July 22, 2008
    Assignee: Cylene Pharmaceuticals, Inc.
    Inventors: Jeffrey P. Whitten, Fabrice Pierre, Michael Schwaebe
  • Patent number: 7402581
    Abstract: The present invention relates to a compound of the general formula (I) wherein Het is an optionally substituted 4-, 5-, 6- or 7-membered heterocyclic ring having at least one nitrogen atom; R1 is hydrogen, hydroxy, C1-C4 alkyl, C3-C4 cycloalkyl, C2-C4 alkenyl or C2-C4 alkynyl; R2 and R3 is each and independently selected from hydrogen, C1-C4 alkyl, C3-C4 cycloalkyl, C2-C4 alkenyl, C2-C4 alkynyl, C1-C4 alkoxy, halogen and cyano, provided that R2 and R3 may not both be hydrogen; R4 is C1-C4 alkyl, C3-C4 cycloalkyl, C2-C4 alkenyl or C2-C4 alkynyl; Ar is an optionally substituted aromatic ring system selected from pyridinyl; 1-naphthyl; 5,6,7,8-tetrahydro-1-naphthyl; quinolinyl; 2,3-dihydro-1,4-benzodioxinyl; 1,3-benzodioxolyl; 5,6,7,8-tetrahydroquinolinyl; 5,6,7,8-tetrahydroisoquinolinyl; 5,6,7,8-tetrahydroquinazolin-4-yl; 1-benzo[b]thiophen-7-yl; 1-benzo[b]thiophen-4-yl; 1-benzo[b]thiophen-3-yl; isoquinolinyl; quinazolinyl; and indan-4-yl; or Ar is substituted phenyl; or an enantiomer thereof or any salt thereo
    Type: Grant
    Filed: June 9, 2004
    Date of Patent: July 22, 2008
    Assignee: Albireo AB
    Inventors: Anders Johansson, Joachim Persson
  • Patent number: 7388007
    Abstract: There is provided a series of novel substituted gamma-lactams of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R4, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    Type: Grant
    Filed: August 18, 2005
    Date of Patent: June 17, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lorin A. Thompson, III, Kenneth M. Boy, Jianliang Shi, John E. Macor
  • Patent number: 7388095
    Abstract: The present invention relates to compounds of formula I wherein R1 to R4 and G are as defined in the description and claims and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
    Type: Grant
    Filed: November 27, 2006
    Date of Patent: June 17, 2008
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor