The 1,3-diazole Ring Is Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/274.1)
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Patent number: 7750032Abstract: The invention provides trisubstituted pyrazoles and imidazoles of Formula I: wherein L2, q, R13, R14, R15, R16, Z1 and Z2 are as described in the Summary of the Invention; and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the peroxisome proliferator-activated receptor (PPAR) families, particularly the activity of PPAR?.Type: GrantFiled: February 3, 2006Date of Patent: July 6, 2010Assignee: IRM LLCInventors: Christopher Cow, Robert Epple, Xing Wang, Yongping Xie, Hans Martin Seidel
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Publication number: 20100152248Abstract: The invention relates to the use of at least on inhibitor selected from the group consisting of raf-, protein kinase C(PKC)-, MEK1/2-, or ERK1/2-inhibitors, for the manufacturing of a medicament to be administrated from 1 up to 12 hours after initiation of an ischemic disease.Type: ApplicationFiled: March 25, 2008Publication date: June 17, 2010Applicant: Pronas Pharma ABInventors: Lars Edvinsson, Saema Ansar
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Publication number: 20100152178Abstract: A CB2 receptor modulator comprising an imidazole derivative represented by the general formula (I): [wherein, R1 represents optionally substituted lower alkyl or the like; R2 represents optionally substituted cycloalkyl or the like; R3 represents optionally substituted aryl or the like; and n represents an integer of 0 to 3] or a pharmaceutically acceptable salt thereof as an active ingredient, and the like are provided.Type: ApplicationFiled: September 5, 2007Publication date: June 17, 2010Applicant: Kyowa Hakko Kirin Co., Ltd.Inventors: Naoto Osakada, Mariko Osakada, Takashi Sawada, Satoshi Kaneko, Atsuko Mizutani, Noriaki Uesaka, Yoshisuke Nakasato, Keishi Katayama, Masamori Sugawara, Yushi Kitamura
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Publication number: 20100105726Abstract: The present invention relates to a pharmaceutical composition comprising compound for induction of apoptosis, a method for inducing cancer cell apoptosis, a method to suppress lymphocyte activation, a method to improve intracellular trafficking of misfolded mutants and a screening method to identify additional compounds useful for inducing apoptosis, and more specifically, it relates to pharmaceutical compositions comprising imidazole derivatives as active gradients for induction of apoptosis to treat various diseases including cancers and immune-related diseases, the method of inducing apoptosis by treating cancer cells with the said pharmaceutical composition, the method of inactivating human lymphocytes by treating lymphocytes with the said pharmaceutical composition, the method of improving intracellular trafficking of misfolded mutants by treating cells containing the mutants with the said pharmaceutical composition, and the screening method for identifying additional compound useful for inducing apoptosType: ApplicationFiled: February 26, 2007Publication date: April 29, 2010Applicant: Industry-Academic Cooperation Foundation, Yonsei UniversityInventors: In-Jae Shin, Myung-ryul Lee, Darren Williams
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Publication number: 20100093808Abstract: The invention is concerned with (2S)-1-{[1,1-Dimethyl-3-(4-pyridin-3-yl-imidazol-1-yl)-propylamino]-acetyl}-pyrrolidine-2-carbonitrile fumarate and crystalline polymorphs of this compound. This compound and its polymorphic forms exhibits superior properties compared to the previously known compounds and can be used as medicament for the treatment of disorders which are associated with DPP-IV.Type: ApplicationFiled: December 14, 2009Publication date: April 15, 2010Inventors: André Bubendorf, Olaf Grassmann, Daniel Hunziker, Holger Kuehne, Regina Moog, Urs Schwitter
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Publication number: 20100087486Abstract: A pharmaceutical composition useful in the prevention of subconjunctival scarring that may occur after glaucoma filtration surgery comprising an effective amount of an activin receptor-like kinase 5 inhibitor. Also disclosed is a method of treating corneal haze and subconjunctival scarring that may develop after ocular surgery comprising applying an amount of a pharmaceutical composition including an activin receptor-like kinase 5 inhibitor.Type: ApplicationFiled: May 29, 2009Publication date: April 8, 2010Inventors: Hiroshi Nakamura, Beatrice Y.J.T. Yue
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Publication number: 20100069436Abstract: The invention relates to imidazole derivatives of the Formula (I) in which the radicals R1, R2, R3, R4 and R5 have the meanings indicated in the description. The compounds of the invention have an immunomodulating and/or cytokine release-inhibiting effect and are therefore suitable for the treatment of disorders associated with an impairment of the immune system.Type: ApplicationFiled: August 24, 2007Publication date: March 18, 2010Applicant: MerckleInventors: Wolfgang Albrecht, Dominik Hauser, Stefan Laufer, Hans-Gunter Striegel, Karola Tollmann
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Publication number: 20100063105Abstract: Disclosed are nicotinanilide-N-oxide compounds, methods for their production, pharmaceutical compositions which include these compounds, and methods for their use in various therapies.Type: ApplicationFiled: October 18, 2006Publication date: March 11, 2010Applicant: UCB SAInventors: Neil S. Cutshall, Kraig M. Yager
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Patent number: 7674901Abstract: An improved process for the preparation of imatinib base and its pharmaceutically acceptable acid addition salts by (a) reacting 2-methyl-5-nitroaniline with cyanamide in the presence of hydrochloric acid to obtain 1-(2-methyl-5-nitrophenyl)guanidine hydrochloride; (b) converting 1-(2-methyl-5-nitrophenyl)guanidine hydrochloride to 1-(2-methyl-5-nitrophenyl)guanidine nitrate; (c) condensing 3-acetylpyridine with N,N-dimethylformamide dimethyl acetal to obtain 3-(dimethylamino)-1-(3-pyridinyl)-prop-2-en-1-one; (d) reacting 3-(dimethylamino)-1-(3-pyridinyl)-prop-2-en-1-one with 1-(2-methyl-5-nitrophenyl)guanidine nitrate to obtain N-(5-nitro-2-methylphenyl)-4-(3-pyridinyl)-2-pyrimidineamine; (e) reducing N-(5-nitro-2-methylphenyl)-4-(3-pyridinyl)-2-pyrimidineamine using hydrazine in the presence of Raney nickel to obtain N-(5-amino-2-methylphenyl)-4-(3-pyridinyl)-2-pyrimidine-amine; (f) condensing N-(5-amino-2-methylphenyl)-4-(3-pyridinyl)-2-pyrimidine-amine with 4-chloromethylbenzoyl chloride in the presence oType: GrantFiled: December 30, 2005Date of Patent: March 9, 2010Assignee: Instytut FarmaceutycznyInventors: Wojciech Szczepek, Wojciech Luniewski, Lukasz Kaczmarek, Bogdan Zagrodzki, Dorota Samson-Lazinska, Wieslaw Szelejewski, Maciej Skarzynski
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Publication number: 20100056569Abstract: The invention relates a kind of antiviral agents, more concretely, relates to a kind of heterocyclic non-nucleoside compounds with the following structures, their preparation and pharmaceutical compositions including the compounds. The said compounds can be used as antiviral agents and as medicaments for treating diseases such as hepatitis B, influenza, herpes, HIV and so on.Type: ApplicationFiled: June 13, 2007Publication date: March 4, 2010Applicant: Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Fajun Nan, Jianping Zuo, Haijun Chen, Guifeng Wang, Min Gu, Fenghua Zhu, Wei Tang
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Patent number: 7659270Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: August 8, 2007Date of Patent: February 9, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
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Patent number: 7635702Abstract: Novel imidazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)- signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.Type: GrantFiled: November 10, 2006Date of Patent: December 22, 2009Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Michael J. Munchhof, Laura C. Blumberg
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Patent number: 7625931Abstract: Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma.Type: GrantFiled: January 13, 2006Date of Patent: December 1, 2009Assignee: CGI Pharmaceuticals, Inc.Inventors: Scott A. Mitchell, Mihaela Diana Danca, Peter A. Blomgren, Robert W. DeSimone, Douglas A. I. Pippin
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Publication number: 20090286827Abstract: The present invention relates to novel bi-aryl amines of formula (I) and to pharmaceutically acceptable prodrugs, salts, solvates, hydrates, and N-oxides thereof and to pharmaceutical compositions comprising them, methods of their use, and methods of their preparation.Type: ApplicationFiled: April 2, 2007Publication date: November 19, 2009Inventors: Ralf Glatthar, David Carcache, Carsten Spanka, Ivan-toma Vranesic, Thomas J. Troxler
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Patent number: 7612100Abstract: To provide a novel anthranilamide compound or its salt which is useful as a pesticide; a process for its production; and a pesticide containing such a compound as an active ingredient. An anthranilamide compound represented by the formula (I) or its salt. In the formula, R1 is halogen, alkyl, haloalkyl, etc.; each of R2 and R3 which are independent of each other, is halogen, alkyl, haloalkyl, etc.; A is alkyl substituted by Y; Y is C3-4 cycloalkyl which may be substituted by at least one substituent selected from the group consisting of halogen, alkyl and haloalkyl; m is from 0 to 4; n is 0 or 1; and q is from 0 to 4.Type: GrantFiled: February 16, 2005Date of Patent: November 3, 2009Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Toru Koyanagi, Masayuki Morita, Akihiro Hisamatsu
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Publication number: 20090258910Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, PDGF-R, lck, SAPK2?, p38, TGF?, KDR, c-Kit, b-RAF, c-RAF, FLT1 and FLT4 kinases.Type: ApplicationFiled: June 25, 2009Publication date: October 15, 2009Applicant: IRM LLCInventors: Nathanael S. Gray, Jiqing Jiang, Yi Liu, Ruo Steensma
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Publication number: 20090247587Abstract: The object is to provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. The solving means is a 1,3-dihydroisobenzofuran derivative represented by the following general formula (1) or salt thereof, or their solvate.Type: ApplicationFiled: March 30, 2009Publication date: October 1, 2009Applicant: KOWA COMPANY, LTD.Inventors: Ayumu OKUDA, Takayuki MATSUDA, Toru MIURA, Koichi YAMAZAKI, Yuki YAMAGUCHI, Minoru KOURA, Sayaka KUROBUCHI, Yuuichiro WATANABE, Kimiyuki SHIBUYA
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Publication number: 20090227602Abstract: The present invention provides compositions of matter, kits and methods for their use in the treatment of MAP kinase-related conditions and/or HMG-CoA reductase-related conditions. In particular, the invention provides compositions for treating inflammatory and/or cardiovascular conditions in an animal subject by inhibiting p38?MAP kinase and/or HMG-CoA reductase, as well as providing formulations and modes of administering such compositions. The invention further provides methods for the rational design of inhibitors of MAP kinase, HMG-CoA reductase, or both for use in the practice of the present invention.Type: ApplicationFiled: October 30, 2006Publication date: September 10, 2009Inventors: John Griffin, Guido Lanza, Jessen Yu
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Patent number: 7582660Abstract: The invention relates to 2-thio-substituted imidazole derivatives of the formula I in which the radicals R1, R2, R3 and m are as defined in the description. The compounds according to the invention have immunomodulating and/or cytokine-release-inhibiting action and are therefore suitable for treating disorders associated with a disturbed immune system.Type: GrantFiled: August 20, 2003Date of Patent: September 1, 2009Assignee: c-a-i-r biosciences GmbHInventors: Stefan Laufer, Hans-Günter Striegel, Karola Tollmann, Wolfgang Albrecht
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Publication number: 20090209759Abstract: The present invention relates to methods and systems for de novo iterative synthesis, an automated iterative drug discovery method and system providing for rapid identification and synthesis of novel compounds.Type: ApplicationFiled: June 18, 2007Publication date: August 20, 2009Applicant: Cresset Biomolecular Discovery, Ltd.Inventors: Brian Warrington, Jeremy Vinter, Mark Mackey
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Patent number: 7569593Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, PDGF-R, lck, SAPK2?, p38, TGF?, KDR, c-Kit, b-RAF, c-RAF, FLT1 and FLT4 kinases.Type: GrantFiled: October 1, 2004Date of Patent: August 4, 2009Assignee: IRM LLCInventors: Nathanael Schiander Gray, Jiqing Jiang, Yi Liu, Ruo Steensma
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Publication number: 20090176766Abstract: Imidazolidinone and imidazolinethione compounds of formula (I): wherein R1, R2, R3, A1, A2, X, Y, Z, m, n, p, x, and y are defined herein. Also disclosed is a method of treating hepatitis C virus infection with these compounds.Type: ApplicationFiled: January 5, 2009Publication date: July 9, 2009Applicant: National Health Research InstitutesInventors: Jyh-Haur Chern, Tsu-An Hsu, Iou-Jiun Kang, Li-Wen Wang, Chung-Chi Lee, Yen-Chun Lee, Yen-Shian Wu, Sheng-Ju Hsu, Yueh Andrew Yueh, Yu-Sheng Chao
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Patent number: 7544807Abstract: Low melting ionic compounds of the general formula (cation) (R?SO4) in which R? is a branched or linear, saturated or unsaturated, aliphatic or alicyclic functionalized or non-functionalized hydrocarbon chain with 3-36 carbon atoms are provided. These compounds can serve as ionic liquids, e.g. as solvents or solvent additives in chemical reactions, as extraction agents or as heat carriers. The compounds comprise a cation and anionic sulfate ester.Type: GrantFiled: August 3, 2007Date of Patent: June 9, 2009Assignee: Merck Patent GmbHInventors: Peter Wasserscheid, Andreas Bösmann, Roy Van Hal
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Publication number: 20090118506Abstract: The present invention discloses compounds of formula I, II or, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.Type: ApplicationFiled: September 17, 2008Publication date: May 7, 2009Inventors: IN JONG KIM, Tongzhu Liu, Yao-Ling Qiu, Guoqiang Wang, Jiang Long, Heejin Kim, Yanchun Wang, Ly Tam Phan, Yat Sun Or
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Publication number: 20090111789Abstract: There are provided compounds of the formula or the pharmaceutically acceptable salts thereof, wherein X, Y, Z, V1, V2, R1, R2, R3, R4 and R5 are herein described. These compounds are useful as anticancer agents.Type: ApplicationFiled: October 9, 2008Publication date: April 30, 2009Inventors: David Joseph Bartkovitz, Jianping Cai, Xin-Jie Chu, Hongju Li, Allen John Lovey, Binh Thanh Vu, Chunlin Zhao
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Patent number: 7517894Abstract: VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridinamides, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis, as well as intermediate products for the production of the compounds are described. The compounds according to the invention can be used as or in the case of tumor or metastasis growth, psoriasis, Kaposi's sarcoma, restenosis, such as, e.g.Type: GrantFiled: June 18, 2004Date of Patent: April 14, 2009Assignee: Bayer Schering Pharma AGInventors: Andreas Huth, Ludwig Zorn, Martin Krueger, Stuart Ince, Karl Heinz Thierauch, Andreas Menrad, Martin Haberey, Holger Hess-Stumpp
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Patent number: 7517994Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y 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: GrantFiled: May 18, 2005Date of Patent: April 14, 2009Assignee: Array Biopharma Inc.Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
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Publication number: 20090088422Abstract: The present invention relates to a compound of the formula [I]: wherein G1 is an alkyl which is substituted by a halogen atom or an alkoxy, or a group of the formula: wherein ring B is benzene ring which may be substituted, etc., Q1 and Q2 may be the same or different, and each is hydrogen atom, a halogen atom or an alkyl, n is 0, 1, 2, 3 or 4, R1 is hydrogen atom, an alkyl which may be substituted, a cycloalkyl which may be substituted, a phenyl which may be substituted, etc., Z1, Z2, Z3 and Z4 may be the same or different, and each is CH or N, provided that 3 or more of Z1, Z2, Z3 and Z4 should not be N at the same time, G2 is hydrogen atom, —NR3R4, —OR5, etc., where R3 to R8 each is independently hydrogen atom, an alkyl which may be substituted, an alkenyl, an alkynyl, etc., or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: November 13, 2008Publication date: April 2, 2009Inventors: Akira Kubo, Ritsuo Imashiro, Hiroaki Sakurai, Hidetaka Miyoshi, Akihito Ogasawara, Hajime Hiramatsu, Tatsuo Nakajima, Tetsu Nakane
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Patent number: 7501445Abstract: This invention relates to compounds of the following formula: in which R1, R2, A1, A2, X, Y, m, n, p, x and y are as defined herein, pharmaceutical compositions comprising the compounds and use of the compounds in treating enterovirus infection.Type: GrantFiled: October 30, 2006Date of Patent: March 10, 2009Assignee: National Health Research InstitutesInventors: Jyh-Haur Chern, Shin-Ru Shih, Chiung-Tong Chen, Chih-Shiang Chang, Chung-Chi Lee, Yen-Chun Lee, Chia-Liang Tai
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Patent number: 7491826Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: July 14, 2004Date of Patent: February 17, 2009Assignee: Cytokinetics, Inc.Inventors: Bradley Paul Morgan, Kathleen A. Elias, Erica Anne Kraynack, Pu-Ping Lu, Fady Malik, Alex Muci, Xiangping Qian, Whitney Walter Smith, Todd Tochimoto, Adam Lewis Tomasi, David J. Morgans, Jr.
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Patent number: 7470713Abstract: The present invention provides compounds having formula I and their use for the treatment of cancer.Type: GrantFiled: February 18, 2005Date of Patent: December 30, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Anne Marinier, Stephan Roy, Alain Martel
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Publication number: 20080319022Abstract: 2-pyridyl-substituted imidazoles and their use in inhibiting ALK 5 and/or ALK 4 receptors is disclosed.Type: ApplicationFiled: June 12, 2008Publication date: December 25, 2008Applicants: IN2GEN CO., LTD., SK CHEMICALS CO., LTD., EWHA UNIVERSITY INDUSTRYInventors: Dae-Kee Kim, Yung-Jue Bang, Hun-Taek Kim, Il-Sang Cho, Myoung-Soon Park, Young Jae An, Joon Hun Choi
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Publication number: 20080312288Abstract: The present invention relates to the mono-sulfate salt, crystalline forms A and B of the mono-sulfate salt, an amorphous form of the mono-sulfate salt, hemi-sulfate salts, and a crystalline form A of the hemi-sulfate salt of the compound 2-chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine.Type: ApplicationFiled: December 17, 2007Publication date: December 18, 2008Inventors: Thomas Cleary, Alexander Glomme, Olaf Grassmann, Shan-Ming Kuang, Roland Meier, Doreen Miller, Regina Moog, Franziska E. Rohrer, Jason Yang
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Patent number: 7449484Abstract: The present invention is directed to novel compounds of Formula (I) for use in the treatment of diseases in a mammal, in which inappropriate, excessive or undesirable angiogenesis has occurred and/or where excessive Tie2 receptor activity has occurred.Type: GrantFiled: March 23, 2006Date of Patent: November 11, 2008Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Deborah L. Bryan
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Patent number: 7442713Abstract: The invention relates to 2-thio-substituted imidazole derivatives of the formula I in which the radicals R1, R2, R3, R4 and p are as defined in the description. The compounds according to the invention have immunomodulating and/or cytokine-release-inhibiting action and are therefore suitable for treating disorders associated with a disturbed immune system.Type: GrantFiled: May 16, 2003Date of Patent: October 28, 2008Assignee: Merckle GmbHInventors: Stefan Laufer, Hans-Guenter Striegel, Wolfgang Albrecht, Karola Tollmann
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Patent number: 7425570Abstract: The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions containing a therapeutically effective amount of at least one of these analogues. In accordance with the present invention, the pyridoxal and pyridoxine analogues can be used in the treatment or prevention of of heparin induced thrombocytopenia (HIT), stroke, and ischemia, and in the treatment of symptoms thereof. The the pyridoxal and pyridoxine analogues can be used in neuroprotection.Type: GrantFiled: December 21, 2004Date of Patent: September 16, 2008Assignee: Medicure International Inc.Inventor: Wasimul Haque
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Publication number: 20080188527Abstract: Disclosed are nicotine-related compounds that selectively inhibit cytochrome P-450 2A6 (CYP2A6), selectively inhibit cytochrome P-450 2A13 (CYP2A13), and/or selectively modulate a nicotinic acetylcholine receptor (nAChR). Also disclosed are pharmaceutical compositions comprising a compound of the invention, as well as methods of using the pharmaceutical compositions for treating or preventing a disease or disorder associated with nicotine-ingestion, or a disease or disorder amenable to treatment by selective modulation of nAChRs.Type: ApplicationFiled: December 10, 2004Publication date: August 7, 2008Inventor: John R. Cashman
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Patent number: 7399866Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: January 14, 2004Date of Patent: July 15, 2008Assignee: Cytokinetics, Inc.Inventors: Bradley Paul Morgan, Kathleen A. Elias, Erica Anne Kraynack, Pu-Ping Lu, Fady Malik, Alex Muci, Xiangping Qian, Whitney Walter Smith, Todd Tochimoto, Adam Lewis Tomasi, David J. Morgans, Jr.
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Patent number: 7390907Abstract: 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, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: September 30, 2004Date of Patent: June 24, 2008Assignee: Amgen Inc.Inventors: Ning Chen, Thomas Nixey, Mark H. Norman
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Publication number: 20080132550Abstract: The present invention relates to a novel series of 4,5-diphenyl-2-amino-4,5-dihydro-imidazole derivatives of the formula II: wherein R, R1, R2, R3, R4, R5, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are P2X7 ion channel blockers and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases having an inflammatory component, including inflammatory bowel disease, rheumatoid arthritis and disease conditions associated with the central nervous system, such as stroke, Alzheimer's disease, etc.Type: ApplicationFiled: November 29, 2007Publication date: June 5, 2008Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: Patrick SHUM, Alexandre GROSS, Liang MA, Daniel G. MCGARRY, Gregory H. MERRIMAN, David RAMPE, Garth RINGHEIM, Jeffrey Stephen SABOL, Francis A. VOLZ
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Publication number: 20080119476Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.Type: ApplicationFiled: July 1, 2005Publication date: May 22, 2008Inventors: Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
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Publication number: 20080114015Abstract: A diastereomers of imidazolines as 4-position acids are described. The imidazoline diastereomers potentiate the activity of antitumor drugs and are potent inhibitors of the transcription factor NF-?B.Type: ApplicationFiled: May 16, 2006Publication date: May 15, 2008Applicant: Board of Trustees of MICHIGAN STATE UNIVERSITYInventor: Jetze J. Tepe
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Publication number: 20080044379Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: August 8, 2007Publication date: February 21, 2008Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
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Publication number: 20080044380Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: August 8, 2007Publication date: February 21, 2008Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
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Patent number: 7332487Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein symbols in the formula have the following meanings; A: —CH2— or —S—, B: CH or N, R1: H, a lower alkyl group, etc., X: a single bonding arm, —CO—, —Alk—CO—, —COCH2—, —Alk—O—, —O—CH2—, —SO2—, —S—, —COO—, —CON(R3)—, —Alk—CON(R3)—, —CON(R3)CH2—, —NHCH2—, etc., R3: hydrogen atom or a lower alkyl group, Alk: a lower alkylene group, and R2: (1) a cyclic group which may be substituted, (2) a substituted amino group, etc., provided that when X is —CO—, then B is N, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 15, 2006Date of Patent: February 19, 2008Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
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Patent number: 7253191Abstract: The invention relates to 2-thio-substituted imidazole derivatives of the formula I in which the radicals R1, R2, R3 and R4 are as defined in the description. The compounds according to the invention have immunomodulating and/or cytokine-release-inhibiting action and are therefore suitable for treating disorders associated with a disturbed immune system.Type: GrantFiled: February 19, 2002Date of Patent: August 7, 2007Assignee: Merckle GmbHInventors: Stefan Laufer, Dunja Kotschenreuther, Philipp Merckle, Karola Tollmann, Hans-Guenter Striegel
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Patent number: 7253187Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein Z1 and Z2 are each independently nitrogen or CH and Ring A, TmR1, QR2, UnR3, and Sp are as described in the specification. The compounds are especially useful as inhibitors of ERK2 and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.Type: GrantFiled: February 3, 2004Date of Patent: August 7, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jingrong Cao, Jeremy Green, Michael Hale, Francois Maltais, Judy Straub, Qing Tang, Alex Aronov
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Patent number: 7247647Abstract: This invention provides compounds of Formula 1, N-oxides and suitable salts thereof wherein R1 is Me, Cl, Br or F; R2 is F, Cl, Br, C1-C4 haloalkyl or C1-C4 haloalkoxy; R3 is F, Cl or Br; R4 is H; C1-C4 alkyl, C3-C4 alkenyl, C3-C4 alkynyl, C3-C5 cycloalkyl, or C4-C6 cycloalkylalkyl, each optionally substituted with one substituent selected from the group consisting of halogen, CN, SMe S(O)Me, S(O)2Me, and OMe; R5 is H or Me; R6 is H, F or Cl; and R7 is H, F or Cl. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula 1, an N-oxide thereof or a suitable salt of the compound (e.g., as a composition described herein).Type: GrantFiled: January 21, 2004Date of Patent: July 24, 2007Assignee: E. I. du Pont de Nemours and CompanyInventors: Kenneth Andrew Hughes, George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
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Patent number: 7241787Abstract: The invention relates to substituted N-cyclohexylheterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to processes for their preparation and to their use as medicaments. Compounds of the formula I, in which the radicals have the stated meanings, and the physiologically tolerated salts thereof, and process for their preparation are described. The compounds bring about for example a weight reduction in mammals and are suitable for example for the prevention and treatment of obesity and diabetes.Type: GrantFiled: January 25, 2005Date of Patent: July 10, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Lothar Schwink, Thomas Boehme, Matthias Gossel, Siegfried Stengelin
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Patent number: 7199137Abstract: Novel compounds (I) and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy wherein Ar is a group of formula a) or b).Type: GrantFiled: September 19, 2001Date of Patent: April 3, 2007Assignee: SmithKline Beecham plcInventors: David Kenneth Dean, Andrew Kenneth Takle, David Matthew Wilson