Chalcogen Bonded Directly To Ring Carbon Of The Diazole Ring Patents (Class 548/361.5)
  • Patent number: 11168065
    Abstract: The invention relates to the compounds of formula I, formula II, formula III, formula IV, formula V, formula VI, formula VII and formula VIII, or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV, formula V, formula VI, formula VII and formula VIII, and methods for the treatment of mucositis may be formulated for oral, mouth wash, buccal, rectal, topical, transdermal, transmucosal, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of oral and gastrointestinal mucositis, mucosal inflammatory and oral infectious diseases.
    Type: Grant
    Filed: January 19, 2016
    Date of Patent: November 9, 2021
    Assignee: Cellix Bio Private Limited
    Inventor: Mahesh Kandula
  • Publication number: 20150141455
    Abstract: The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: June 27, 2013
    Publication date: May 21, 2015
    Applicant: NOVARTIS AG
    Inventors: Eva Altmann, Ulrich Hommel, Edwige Liliane Jeanne Lorthiois, Jeurgen Klaus Maibaum, Nils Ostermann, Jean Quancard, Stefan Andreas Randl, Olivier Rogel, Anna Vulpetti
  • Patent number: 8940730
    Abstract: Briefly described, embodiments of this disclosure include compounds, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, methods of treating liver fibrosis in a host, and the like.
    Type: Grant
    Filed: March 16, 2010
    Date of Patent: January 27, 2015
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Jeffrey S. Glenn, Wenjin Yang, Ingrid C. Choong
  • Publication number: 20140336170
    Abstract: The present invention is directed to substituted indazole compounds, pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated metabolic disorders and/or diseases such as obesity, Type II diabetes mellitus and Metabolic Syndrome X.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Xuqing Zhang, Marta C. Abad, Alan C. Gibbs, Gee-Hong Kuo, Fengbin Song, Zhihua Sui
  • Patent number: 8822447
    Abstract: The present invention is directed to substituted indazole compounds of formula (I) pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated metabolic disorders and/or diseases such as obesity, Type II diabetes mellitus and Metabolic Syndrome X.
    Type: Grant
    Filed: April 21, 2011
    Date of Patent: September 2, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Xuqing Zhang, Marta C. Abad, Alan C. Gibbs, Gee-Hong Kuo, Lawrence C. Kuo, Fengbin Song, Zhihua Sui
  • Patent number: 8809427
    Abstract: Provided is a phthalocyanine compound which is halogen-free and which has a green hue, excellent resistance to organic solvents and acids, and high chroma. Also provided are a metal-free phthalocyanine compound or a metal phthalocyanine compound represented by specified general formula (1-1) or (1-2) and having a N,N?-disubstituted imidazolone structure or piperazinedione structure introduced therein, and a coloring composition including the compound and a synthetic resin. The phthalocyanine compound of the present invention exhibits a clear green color and is halogen-free, and is thus useful as a clear green pigment for coloring materials such as a coating material, plastic, a printing ink, rubber, leather, textile printing, a color filter, a jet ink, a heat transfer ink, etc.
    Type: Grant
    Filed: August 6, 2010
    Date of Patent: August 19, 2014
    Assignee: DIC Corporation
    Inventors: Hitoshi Kondou, Yoshiyuki Sano, Yutaka Tachikawa
  • Patent number: 8637677
    Abstract: Organic dicarboxylic acid compounds, salts and preparation methods thereof are described. The compounds have activity of resisting oxidation damage to crystalline lens of eyes. The structures of the above organic dicarboxylic acid compounds are shown as wherein R is a hydrogen atom, a C1-3 alkyl group, a C1-3 alkoxyl group, or a halogen atom.
    Type: Grant
    Filed: November 12, 2010
    Date of Patent: January 28, 2014
    Assignees: Southeast University, Nanjing Medical University, Zhejiang Shapuaisi Pharmacy Ltd.
    Inventors: Shaohua Gou, Hong Shen, Yindi Zhang, Jianping Shen, Yanqin Zhu, Luzhong Feng, Jianwei Wu, Dekang Chen
  • Patent number: 8598078
    Abstract: Compounds of Formula I wherein the substituents are as defined in Claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Grant
    Filed: August 21, 2008
    Date of Patent: December 3, 2013
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Olivier Loiseleur, Roger Graham Hall, André Denis Stoller, Gerald Wayne Craig, André Jeanguenat, Andrew Edmunds
  • Publication number: 20130012708
    Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 10, 2013
    Applicant: Nissan Chemical Industries Limited
    Inventors: Shingo Owada, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
  • Patent number: 8304443
    Abstract: Compounds represented by the Formula (A-1) and the Formula (1) or salt thereof are provided. The compounds represented by the Formula (A-1) and the Formula (1) or salt thereof have a ?3 adrenergic receptor agonist activity, and therefore are useful as an agent for the prevention and treatment of diabetes, obesity, hyperlipidemia, depression, biliary stone, a disorder derived from hyperactivity of biliary tract, a disorder derived from hyperactivity of digestive tract, interstitial cystitis, overactive bladder, urinary incontinence or a disorder derived from decreased tear secretion, etc.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: November 6, 2012
    Assignee: Asahi Kasei Pharma Corporation
    Inventors: Seiji Nakano, Akifumi Morimoto, Yasuhiro Wada
  • Publication number: 20120226051
    Abstract: Organic dicarboxylic acid compounds, salts and preparation methods thereof. The said compounds have activity of resisting oxidation damage to crystalline lens of eyes. The structures of the above organic dicarboxylic acid compounds are shown as formula (1).
    Type: Application
    Filed: November 12, 2010
    Publication date: September 6, 2012
    Inventors: Shaohua Gou, Hong Shen, Yindi Zhang, Jianping Shen, Yanqin Zhu, Luzhong Feng, Jianwei Wu, Dekang Chen
  • Publication number: 20120225909
    Abstract: [Objective] To provide a drug that selectively stimulates the ?3-adrenergic receptors, particularly a drug capable of preferentially stimulating the ?3-adrenergic receptors over the ?1-adrenergic receptors. This drug can be used in the treatment and prevention of diabetes, obesity, hyperlipidemia, depression, cholelithiasis, diseases caused by biliary hyperkinesia, diseases caused by hyperfunction of the gastrointestinal tract, interstitial cystitis, overactive bladder or urinary incontinence, diseases associated with decreased lacrimation, and the like. [Solution] Indazole analogs represented by the general formula (I) or a salt thereof. Drugs that contains these indazole analogs or a salt thereof as the active ingredient.
    Type: Application
    Filed: September 30, 2010
    Publication date: September 6, 2012
    Applicant: ASAHI KASEI PHARMA CORPORATION
    Inventors: Yasuhiro Wada, Akifumi Morimoto
  • Publication number: 20120148534
    Abstract: Briefly described, embodiments of this disclosure include compounds, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, methods of treating liver fibrosis in a host, and the like.
    Type: Application
    Filed: March 16, 2010
    Publication date: June 14, 2012
    Inventors: Jeffrey S. Glenn, Wenjin Yang, Ingrid C. Choong
  • Publication number: 20120071503
    Abstract: The disclosure provides compounds and compositions, and methods of using these compounds and compositions, as positive allosteric modulators of the metabotropic glutamate subtype 2 (mGlu2) receptor, and for treating CNS disorders associated with the mGlu2 receptor including schizophrenia, anxiety, addiction, e.g. cocaine addiction, nicotine addiction, and the like.
    Type: Application
    Filed: March 18, 2011
    Publication date: March 22, 2012
    Applicant: Sanford-Burnham Medical Research Institute
    Inventors: Nicholas D. P. Cosford, Dhanya Raveendra Panickar, Shyama Sidique
  • Patent number: 8114865
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer formula (I).
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: February 14, 2012
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Tiziano Bandiera, Andrea Lombardi Borgia, Marcella Nesi, Ettore Perrone, Roberto Bossi, Paolo Polucci
  • Publication number: 20110263559
    Abstract: The present invention is directed to substituted indazole compounds, pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated metabolic disorders and/or diseases such as obesity, Type II diabetes mellitus and Metabolic Syndrome X.
    Type: Application
    Filed: April 21, 2011
    Publication date: October 27, 2011
    Inventors: Xuqing ZHANG, Marta G. ABAD, Alan C. GIBBS, Gee-Hong KUO, Lawrence C. KUO, Fengbin SONG, Zhihua SUI
  • Patent number: 8030340
    Abstract: Compounds of formula (I): or a pharmaceutically acceptable salt thereof, compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).
    Type: Grant
    Filed: November 21, 2007
    Date of Patent: October 4, 2011
    Assignees: AstraZeneca AB, Bayer Schering Pharma Aktiengesellschaft
    Inventors: Markus Berger, Lena Bergstrom, Jan Dahmen, Anders Eriksson, Balint Gabos, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepisto, Stinabritt Nilsson, Camilla Taflin, Hartmut Rehwinkel, Darren McKerrecher
  • Publication number: 20110212078
    Abstract: This invention relates to compounds of the following Formula (I); or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.
    Type: Application
    Filed: June 24, 2009
    Publication date: September 1, 2011
    Inventors: Panduranga Adulla P. Reddy, Umar Faruk Mansoor, M. Arshad Siddiqui
  • Patent number: 8008506
    Abstract: Provided are compounds represented by the following formula (A-1) and formula (1), or salts thereof. The compounds of formula (A-1) and formula (1) or salts thereof have ?3 adrenergic receptor agonist activity, and thus are useful as therapeutic and prophylactic agent for diabetes mellitus, obesity, hyperlipidemia, depression, diseases caused by gallstones or hypermotility of the biliary tract, diseases caused by hyperactivity of the digestive tract, interstitial cystitis, overactive bladder or urinary incontinence, or as therapeutic and prophylactic agents for diseases concomitant with decreased tears.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: August 30, 2011
    Assignee: Asahi Kasei Pharma Corporation
    Inventors: Seiji Nakano, Taisuke Iwanami, Kei Yamanishi, Yasuhiro Wada, Akifumi Morimoto
  • Patent number: 7960563
    Abstract: The present invention relates to novel indazole derivatives having pharmacological activity, processes for their preparation, compositions containing them and uses of these compounds in the treatment of estrogen receptor beta mediated diseases.
    Type: Grant
    Filed: March 5, 2008
    Date of Patent: June 14, 2011
    Assignee: Glaxo Group Limited
    Inventors: Christopher Norbert Johnson, David G Jones, Xi Liang, David Timothy MacPherson, Aaron B Miller, Antoinette Naylor, Steven James Stanway, Andrew Kenneth Takle, Giancarlo Trani
  • Publication number: 20110118303
    Abstract: The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity. In a first embodiment, the present invention relates to compounds derived from taurine, in which taurine is bound directly by means of an amide bond or through an spacing group, to a compound selected from the group of non-steroidal anti inflammatory compounds, cited as derived from taurine presenting the Formula (I): in which R means the component with non-steroidal anti inflammatory activity. In a second embodiment, the invention provides a process for obtaining the compounds of Formula (I) by reaction of taurine with a compound belonging to the group of non-steroidal anti inflammatory (NSAIs), in order to obtain a compound derived from taurine by direct bond or through a spacing group of the taurine to the NSAI. The invention also relates to the pharmaceutical compositions comprising at least one compound derived from taurine presenting non-steroidal anti inflammatory activity.
    Type: Application
    Filed: April 9, 2009
    Publication date: May 19, 2011
    Applicants: EMS S.A., Universidade Estadual Paulista Julio De Mesquita Filho - UNESP
    Inventors: Ednir de Oliveira Vizioli, Chung Man Chin, Renato Farina Menegon, Lorena Blau, Jean Leandro Dos Santos, Maria do Carmo Longo
  • Publication number: 20110112147
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
    Type: Application
    Filed: October 5, 2010
    Publication date: May 12, 2011
    Inventors: David Robert Bolin, Stuart Hayden, Yimin Qian
  • Patent number: 7939520
    Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.
    Type: Grant
    Filed: May 13, 2008
    Date of Patent: May 10, 2011
    Assignee: Wyeth LLC
    Inventors: Simon Nicolas Haydar, Patrick Andrae
  • Publication number: 20110082143
    Abstract: Bicyclic heteroaryl compounds of formula (I) shown below are disclosed. Each variable in formula (I) is defined in the specification. Also disclosed is treatment of cancer with these compounds.
    Type: Application
    Filed: October 1, 2010
    Publication date: April 7, 2011
    Applicant: National Taiwan University
    Inventors: Chung-Ming Sun, Min-Liang Kuo
  • Patent number: 7868184
    Abstract: There is provided a method to convert O-functionalized indazolinone-derivatives to the corresponding N2-functionalized indazolinone derivatives, by use of microwave energy or a transition metal catalyst. A preferred catalyst is palladium tetrakis. The method described allows the creation of a library of chemical compounds which can be screened for biological activity.
    Type: Grant
    Filed: June 8, 2005
    Date of Patent: January 11, 2011
    Assignee: The University of the University of St. Andrews
    Inventors: Nicholas James Westwood, Nicolas Stanislas Jean Isambert
  • Patent number: 7842712
    Abstract: The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK2, CDK2, MK2, SRC, SYK, and Aurora-2. Accordingly, compounds and compositions of the invention are useful for treating or lessening the severity of a variety of disorders, including, but not limited to, heart disease, diabetes, Alzheimer's disease, immunodeficiency disorders, inflammatory diseases, allergic diseases, autoimmune diseases, destructive bone disorders such as osteoporosis, proliferative disorders, infectious diseases and viral diseases.
    Type: Grant
    Filed: August 20, 2007
    Date of Patent: November 30, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Alex Aronov, David J. Lauffer, Huan Qiu Li, Ronald Charles Tomlinson, Pan Li
  • Publication number: 20100286133
    Abstract: The invention relates to diacyl indazole derivatives of general formulae (I) or (II) and to the pharmaceutically acceptable salts thereof: Wherein X, R1 and R2 are as defined herein. The invention also relates to the use of these compounds as pharmaceutical products.
    Type: Application
    Filed: July 20, 2010
    Publication date: November 11, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Gerhard ZOLLER, Stefan PETRY, Gunter MĂœLLER, Hubert HEUER, Norbert TENNAGELS
  • Patent number: 7803830
    Abstract: The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Grant
    Filed: October 8, 2008
    Date of Patent: September 28, 2010
    Assignee: Roche Palo Alto LLC
    Inventors: Pravin Iyer, Matthew C. Lucas, Ryan Craig Schoenfeld, Marzia Villa, Robert James Weikert
  • Publication number: 20100222275
    Abstract: Provided are a pharmaceutical product capable of treating vitiligo by thickening the epidermis at a vitiligo-affected site, which has been thinned, to thereby accelerate pigmentation, and a method of accelerating pigmentation by thickening the epidermis. Vitiligo can be treated by using a compound having an epidermis thickening action, for example, a therapeutic agent for a skin ulcer which is used in the treatment of burn ulcer, crural ulcer, diabetic ulcer or post-operative ulcer, or a therapeutic agent for bedsore.
    Type: Application
    Filed: October 17, 2008
    Publication date: September 2, 2010
    Inventors: Kunihiko Tamaki, Kanako Kikuchi, Mayumi Komine, Seiki Fujimoto
  • Patent number: 7776910
    Abstract: Compounds of the formula I: wherein m, n, Ar, R1 and R2 are as defined herein. Methods of making the compounds and using the compounds are disclosed.
    Type: Grant
    Filed: November 8, 2007
    Date of Patent: August 17, 2010
    Assignee: Roche Palo Alto LLC
    Inventors: Francisco Javier Lopez-Tapia, Lee Edwin Lowrie, Jr., Dov Nitzan
  • Patent number: 7772268
    Abstract: The invention relates to diacyl indazole derivatives of general formulae (I) or (II) and to the pharmaceutically acceptable salts thereof: Wherein X, R1 and R2 are as defined herein. The invention also relates to the use of these compounds to treat diabetes mellitus, dyslipidemia and atherosclerotic disorders.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: August 10, 2010
    Assignee: Sanofi-Aventis
    Inventors: Gerhard Zoller, Stefan Petry, Gunter MĂ¼ller, Hubert Heuer, Norbert Tennagels
  • Publication number: 20100137291
    Abstract: The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.
    Type: Application
    Filed: December 11, 2009
    Publication date: June 3, 2010
    Inventors: Richard A. EARL, Maiko EZAWA, Xinqin FANG, David S. GARVEY, Ricky D. GASTON, Subhash P. KHANAPURE, L. Gordon LETTS, Chia-En LIN, Ramani R. RANATUNGA, Stewart K. RICHARDSON, Joseph D. SCHROEDER, Cheri A. STEVENSON, Shiow-Jyi WEY
  • Patent number: 7723329
    Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
    Type: Grant
    Filed: August 14, 2006
    Date of Patent: May 25, 2010
    Assignee: Wyeth LLC
    Inventors: Hassan Mahmoud Elokdah, Alexander Alexei Greenfield, Kevin Liu, Robert Emmett McDevitt, Geraldine Ruth McFarlane, Cristina Grosanu, Jennifer Rebecca Lo, Yanfang Li, Albert Jean Robichaud, Ronald Charles Bernotas
  • Publication number: 20100094011
    Abstract: The present invention provides novel methods for preparing 5-(trifluoromethoxy)-1H-3-indazolecarboxylic acid (3), which is a useful precursor for the preparation of bicyclic-5-trifluoromethoxy-1H-indazole-3-carboxylic acid amides of Formula (1). Compounds of Formula (1) are active as agonists and partial agonists of the nicotinic ?-7 receptor and are being studied for their use in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. The present methods are useful for preparing compound (3) on scale up levels.
    Type: Application
    Filed: October 9, 2009
    Publication date: April 15, 2010
    Inventors: Thomas Cleary, Yaohui Ji, Thimma Rawalpally
  • Patent number: 7576087
    Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
    Type: Grant
    Filed: June 19, 2007
    Date of Patent: August 18, 2009
    Assignee: Wyeth
    Inventors: Ronald Charles Bernotas, Yinfa Yan
  • Publication number: 20090163546
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
    Type: Application
    Filed: December 1, 2008
    Publication date: June 25, 2009
    Inventors: David Robert Bolin, Jianping Cai, Robert Alan Goodnow, JR.
  • Publication number: 20090149459
    Abstract: This invention relates to inhibitors of p38 and methods of utilizing the inhibitors and pharmaceutical compositions thereof in the treatment and prevention of various disorders mediated by p38.
    Type: Application
    Filed: February 2, 2009
    Publication date: June 11, 2009
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Mark Munson, David A. Mareska, Youngboo Kim, Robert D. Groneberg, James Rizzi, Martha Rodriguez, Ganghyeok Kim, Guy Vigers, Chang Rao, Devan Balachari, Darren Harvey
  • Patent number: 7528158
    Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R7 have the significances given in the description and claims can be used in the form of pharmaceutical compositions.
    Type: Grant
    Filed: September 26, 2005
    Date of Patent: May 5, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kurt Amrein, Jianping Cai, Robert Alan Goodnow, Jr., Daniel Hunziker, Bernd Kuhn, Alexander Mayweg, Werner Neidhart
  • Patent number: 7524842
    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, aggrecanase, TNF-? or combinations thereof.
    Type: Grant
    Filed: January 16, 2007
    Date of Patent: April 28, 2009
    Assignee: Schering Corporation
    Inventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Bandarpalle B. Shankar, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Razia Rizvi, Lei Chen, De-Yi Yang, Robert Feltz, Seong Heon Kim
  • Publication number: 20090099236
    Abstract: The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Application
    Filed: October 8, 2008
    Publication date: April 16, 2009
    Inventors: Pravin Iyer, Matthew C. Lucas, Ryan Craig Schoenfeld, Marzia Villa, Robert James Weikert
  • Patent number: 7514457
    Abstract: Compounds of the general formula (I): pharmaceutical compositions comprising a compound of general formula (I); and methods of treating disease conditions caused by overactivation of the VR1 receptor by administering a compound of general formula (I) to a subject.
    Type: Grant
    Filed: May 31, 2006
    Date of Patent: April 7, 2009
    Assignee: Pfizer Inc.
    Inventors: Tadashi Inoue, Satoshi Nagayama, Yuji Shishido
  • Patent number: 7504424
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
    Type: Grant
    Filed: January 17, 2006
    Date of Patent: March 17, 2009
    Assignee: Schering Corporation
    Inventors: Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K. C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankar, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Umar Faruk Mansoor, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li
  • Patent number: 7495015
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein m, k, B, R1, R2 and R3 are those defined herein, and compositions comprising the same. Also provided are methods for preparing compounds of formula I and using the same in treating p38 mediated disorders in a patient.
    Type: Grant
    Filed: February 25, 2005
    Date of Patent: February 24, 2009
    Assignee: Roche Palo Alto LLC
    Inventors: Nidhi Arora, Tobias Gabriel, David Michael Goldstein, Teresa Alejandra Trejo-Martin
  • Patent number: 7488745
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
    Type: Grant
    Filed: January 16, 2007
    Date of Patent: February 10, 2009
    Assignee: Schering Corporation
    Inventors: Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K. C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankar, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Razia Rizvi, Aneta M. Micula, Robert Feltz
  • Patent number: 7485643
    Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, R10, R20, R21, and R22 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: November 18, 2004
    Date of Patent: February 3, 2009
    Assignee: Array BioPharma Inc.
    Inventors: Eli Wallace, Joseph P. Lyssikatos, Hong Woon Yang
  • Patent number: 7482370
    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: July 13, 2005
    Date of Patent: January 27, 2009
    Assignee: Schering Corporation
    Inventors: Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K. C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankar
  • Publication number: 20090012308
    Abstract: The present invention provides a process for the manufacture of an arylmethyl-sulfonylarene, R1CH2SO2R2, wherein R1 and R2 are each independently an optionally substituted phenyl or naphthyl group which process comprises reacting an arylmethylhalide, R1CH2-Hal wherein R1 is as defined hereinabove and Hal is Cl, Br or I with a sodium arylsulfinate R2SO2Na wherein R2 is as defined hereinabove in the presence of a base optionally in the presence of a solvent. Also provided is the use of the inventive process in the manufacture of a 3-arylsulfonylindazole 5-HT6 ligand.
    Type: Application
    Filed: June 9, 2008
    Publication date: January 8, 2009
    Applicant: Wyeth
    Inventors: Mahmut Levent, Panolil Raveendranath, Sanjay Raveendranath, Vijay Raveendranath, Girija Raveendranath
  • Publication number: 20080293688
    Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.
    Type: Application
    Filed: May 13, 2008
    Publication date: November 27, 2008
    Applicant: Wyeth
    Inventors: Simon Nicolas Haydar, Patrick Andrae
  • Publication number: 20080293715
    Abstract: The present invention provides for compounds of Formula I: wherein R2, R3, R4, R5, R6, R7, X, and L have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of central nervous disorders and conditions including attention deficit hyperactivity disorder, neuropathic pain, urinary incontinence, anxiety, depression, and schizophrenia and fibromyalgia. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
    Type: Application
    Filed: August 4, 2008
    Publication date: November 27, 2008
    Applicant: WARNER LAMBERT COMPANY LLC
    Inventors: Robert M. Schelkun, Po-Wai Yuen
  • Publication number: 20080287516
    Abstract: The present invention relates to phenyl-substituted pyrrolidones and compounds related to phenyl-substituted pyrrolidones. One use of these compounds is for the inhibition of viruses, e.g., HIV. The invention further relates to methods of malting these compounds, methods of identifying the efficacy of these compounds, and methods of using these compounds to inhibit or prevent HIV infection and related disease states such as AIDS.
    Type: Application
    Filed: January 30, 2006
    Publication date: November 20, 2008
    Applicant: IRM LLC
    Inventors: Baogen Wu, Truc Ngoc Nguyen, David Archer Ellis, Xiaohui He, Beth Marie Anaclerio, Kunyong Yang, Ha-soon Choi, Zhicheng Wang, Thomas H. Marsilje, Yun He