1,2,3-thiadiazoles (including Hydrogenated) Patents (Class 548/127)
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Patent number: 7872146Abstract: Process for the preparation of a carboxamide derivative of formula (I) or a salt thereof Intermediates for preparing this compound are also provided.Type: GrantFiled: May 6, 2006Date of Patent: January 18, 2011Assignee: Bayer CropScience AGInventors: Thierry Eynard, Cécile Franc
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Publication number: 20110009418Abstract: The present invention discloses compounds of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Phenylene Compound”); compositions comprising an effective amount of a Phenylene Compound; and methods for treating or preventing pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Phenylene Compound.Type: ApplicationFiled: July 29, 2010Publication date: January 13, 2011Applicant: Purdue Pharma L.P.Inventor: Qun Sun
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Publication number: 20110009457Abstract: The invention relates to a composition comprising at least one aminobenzamide compound or a salt thereof for controlling animal parasites, veterinary pharmaceutical compositions comprising at least one aminobenzamide of formula (I) for preventing infection with diseases transmitted through parasites, its use for the preparation of a veterinary pharmaceutical for controlling animal parasites, and a method for preventing infection with diseases transmitted through parasites.Type: ApplicationFiled: December 9, 2008Publication date: January 13, 2011Applicant: BAYER CROPSCIENCE AGInventors: Ulrich Görgens, Katsuaki Wada, Yukiyoshi Watanabe, Jun Mihara, Koichi Araki
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Patent number: 7855292Abstract: Certain sulfonamide compounds are dual CCK1/CCK2 inhibitors useful in the treatment of CCK1/CCK2 mediated diseases.Type: GrantFiled: November 20, 2007Date of Patent: December 21, 2010Assignee: Janssen Pharmaceutica NVInventors: Brett Allison, Victor K. Phuong, Marna C. W. Pippel, Michael H. Rabinowitz, Hariharan Venkatesan
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Publication number: 20100317854Abstract: The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.Type: ApplicationFiled: August 23, 2010Publication date: December 16, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Cristina Alonso-Alija, Markus Heil, Dietmar Flubacher, Paul Naab, Josef Pernerstorfer, Johannes-Peter Stasch, Frank Wunder, Klaus Dembowsky, Elizabeth Perzborn, Elke Stahl
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Publication number: 20100317701Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: ApplicationFiled: August 20, 2010Publication date: December 16, 2010Inventors: Gregory D. Cuny, Xin Teng, Junying Yuan, Alexei Degterev, John A. Porco, JR.
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Publication number: 20100298340Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: April 12, 2007Publication date: November 25, 2010Applicants: AstraZeneca AB, Astex Therapeutics Ltd.Inventors: Stefan Berg, Karin Kolmodin
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Publication number: 20100292472Abstract: The present invention can provide a novel medicament that is safe, cheap and effective for prophylaxis or therapy of apicomplexan infections, such as malaria and toxoplasmosis by applying a plant growth regulator selected from the group consisting of gibberellin inhibitors, cytokinins and ethylene inhibitors to the prophylactic or therapeutic treatment of such apicomplexan infections.Type: ApplicationFiled: January 22, 2009Publication date: November 18, 2010Inventors: Tomoko Toyama, Kisaburo Nagamune, Toshihiro Horii, Kazuyuki Tanabe
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Publication number: 20100273832Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of Formula (I), to insecticidal, acaricidal, molluscicidal or nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc or nematode pests.Type: ApplicationFiled: December 18, 2008Publication date: October 28, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Pierre Joseph Marcel Jung, Peter Renold
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Publication number: 20100261675Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.Type: ApplicationFiled: June 24, 2010Publication date: October 14, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
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Publication number: 20100256115Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.Type: ApplicationFiled: March 18, 2010Publication date: October 7, 2010Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
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Publication number: 20100247534Abstract: A compound of formula I wherein m, n, A, B, D, E, G, H, Y, R1, R2, R3, R4, R5, and R8, are described herein.Type: ApplicationFiled: June 10, 2010Publication date: September 30, 2010Inventors: James A. Johnson, John Lloyd, Alexander Kover
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Patent number: 7799933Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R1, R2, R3, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: GrantFiled: December 6, 2007Date of Patent: September 21, 2010Assignee: Hoffman-La Roche Inc.Inventors: Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander
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Publication number: 20100227900Abstract: The present invention relates to the use of compounds according to formula (I) for controlling bacterial harmful organisms in useful plants. Moreover, the present invention relates to a method for controlling bacterial harmful organisms in useful plants by treating them with compounds according to formula (I).Type: ApplicationFiled: February 3, 2010Publication date: September 9, 2010Applicant: Bayer CropScience AGInventors: Lutz Aßmann, Karl-Wilhelm Münks, Peter Howard Davies, Rolf Christian Becker, Ingo Wetcholowsky
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Patent number: 7786040Abstract: The present invention relates to 1,2,3 -thiadiazole compounds represented by formula (I): wherein R1, R2, R3, R4 and R5 each represents H, halogen, CN, alkyl, alkoxyalkyl, aryl, arylalkyl, alkylcarbonyl or the like; R6 represents —C?(W1)YR7 in which R7 represents H, alkyl, alkenyl, phenylcarbonyl, heterocyclic ring-carbonyl, arylsulfonyl or the like; Y represents O, S, —N(R11), —N(R11)O— in which R11 represents H, alkyl, cycloalkyl, substituted phenyl, or the like; W1 represents O or S; and symbols in the formula are defined in detail in the specification or salts thereof, and to a plant disease control agent for agricultural and horticultural use which contains the compound as an active ingredient.Type: GrantFiled: February 23, 2006Date of Patent: August 31, 2010Assignee: Nihon Nohyaku Co., Ltd.Inventors: Kunihisa Umetani, Takashi Shimaoka, Minoru Yamaguchi, Masatsugu Oda, Nobuo Kyomura, Tsuyoshi Takemoto, Kazuhiko Kikutake
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Patent number: 7786149Abstract: Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.Type: GrantFiled: September 26, 2007Date of Patent: August 31, 2010Assignees: Schering Corp., Pharmacopeia Drug Discovery, Inc.Inventors: Purakkattle J. Biju, Arthur G. Taveras, J. Robert Merritt, John J. Baldwin, Younong Yu, Junying Zheng, Jianhua Chao, Cynthia J. Aki
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Publication number: 20100216827Abstract: Aryl GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.Type: ApplicationFiled: October 20, 2009Publication date: August 26, 2010Inventors: Jingyuan Ma, Aaron Novack, Imad Nashashibi, Phuongly Pham, Christopher J. Rabbat, Jiangao Song, Dong Fang Shi, Zuchun Zhao, Yun-Jung Choi, Xin Chen
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Publication number: 20100216850Abstract: A compound of formula (I) wherein A1, A2, A3, A4, G1, G2, R1, R2, R3, R4, Q1, Y1, Y2, Y3 and Y4 are as defined in claim 1; or a salt or TV-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests.Type: ApplicationFiled: October 13, 2008Publication date: August 26, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Pierre Joseph Marcel Jung, Peter Renold, Christopher Richard Ayles Godfrey, William Lutz, Peter Maienfisch, Werner Zambach
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Patent number: 7772285Abstract: A benzophenone derivative represented by the following formula: wherein R1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl; R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.Type: GrantFiled: November 13, 2002Date of Patent: August 10, 2010Assignee: Toyama Chemical Co., Ltd.Inventors: Hisaaki Chaki, Hironori Kotsubo, Tadashi Tanaka, Yukihiko Aikawa, Shuichi Hirono, Shunichi Shiozawa
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Publication number: 20100152203Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted thiadiazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: ApplicationFiled: December 12, 2009Publication date: June 17, 2010Inventors: Li Chen, Lichun Feng, Minmin Yang, Michael Patrick Dillon, Yingjie Lai
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Publication number: 20100143499Abstract: Compounds, compositions, and methods of using such compounds to modulate apoptosis including IAP antagonists are provided herein. Compositions including mimetics of the invention and, optionally, secondary agents, may be used to treat proliferative disorders such as, cancer and autoimmune diseases.Type: ApplicationFiled: July 24, 2007Publication date: June 10, 2010Applicant: TETRALOGIC PHARMACEUTICALS CORPORATIONInventor: Stephen M. Condon
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Publication number: 20100130538Abstract: The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or a heterocyclic group optionally having substituent(s); R2 is a hydrogen atom or a hydrocarbon group optionally having substituent(s); Xa and Xb are each C, N, O or S; Xc and Xd are each C or N; m is 0-2; n is 1-3; ring A is a 5-membered ring optionally having substituent(s); ring B is a 6-membered ring optionally having substituent(s); and ring C is a 3- to 5-membered ring optionally having substituent(s), provided that when Xa, Xc and Xd are each C, then Xb is N or S, or a salt thereof, which is useful as an agent for the prophylaxis or treatment of a disease relating to an action of melatonin, and the like.Type: ApplicationFiled: April 25, 2008Publication date: May 27, 2010Inventors: Tatsuki Koike, Takafumi Takai, Yasutaka Hoashi
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Patent number: 7718678Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof. X is N or N+O?, and Y is N or N+O?, provided that at least X or Y is N. The compounds are useful for the treatment of chemokine-mediated diseases such as COPD.Type: GrantFiled: June 27, 2006Date of Patent: May 18, 2010Assignee: Schering CorporationInventor: Purakkattle J. Biju
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Publication number: 20100022772Abstract: The present invention relates to processes for the preparation of biaryl oxazolidinones. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.Type: ApplicationFiled: July 28, 2004Publication date: January 28, 2010Applicant: RIB-X PHARMACEUTICALS, INC.Inventors: Yusheng Wu, Chen Shili, Yi Chen, Roger Hanselmann, Rongliang Lou, Jiacheng Zhou
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Publication number: 20090326016Abstract: The present invention relates to N-cycloalkyl-thiocarboxamide or N-cycloalkyl-N-substituted carboximidamide derivatives of formula (I) wherein A and B represent a 5-membered heterocyclyl groups, T represents an oxygen, sulphur or amino derivatives, Z1 represents a cycloalkyl group and Z2 and Z3 represent various substituents, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 30, 2007Publication date: December 31, 2009Inventors: Ralf Dunkel, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Philippe Rinolfi, Arounarith Tuch
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Publication number: 20090286835Abstract: The present invention provides compounds of formula (I) wherein n, p, R1, R2, X1, X2, X3, X4, X5, R3a, R3b, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: October 3, 2008Publication date: November 19, 2009Applicant: AstraZeneca ABInventors: Hakan BLADH, Frank Burkamp, Balint Gabos, Peter Hansen, Svetlana Ivanova, Karolina Lawitz
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Patent number: 7601744Abstract: The present invention is directed to benzothiadiazolylphenylalkylamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: GrantFiled: September 27, 2006Date of Patent: October 13, 2009Assignee: WyethInventors: Casey Cameron McComas, Puwen Zhang, Eugene John Trybulski, An Thien Vu, Eugene Anthony Terefenko
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Publication number: 20090221564Abstract: Heterocyclic compounds of the formula (I) are provided: wherein ring A, ring B, R1, R2, R3, R4, Y, m, n and q are as identified herein. R1 is in particular amidino. The invention further provides particular benzothiophene compounds. Compounds of the invention may be useful as inhibitors of Factor IXa and in the therapy of cardiovascular conditions and diseases, e.g. thrombosis.Type: ApplicationFiled: February 20, 2007Publication date: September 3, 2009Applicant: TRIGEN LIMITEDInventors: Shouming Wang, Toby Jonathan Blench, Frederic Marlin, Richard Beck, Roger Peter Dickinson
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Publication number: 20090215623Abstract: Novel 3-acylaminobenzanilides of the formula (I) wherein R1 represents phenyl which may be substituted or a 5-member or 6-member heterocyclic ring group, which may be substituted, containing at least one hetero-atom selected from the group consisting of N, O, and S; R2 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; R3 represents C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl, or C1-6 haloalkylsulfonyl; R4 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; X represents halogen, C1-6 alkyl, or C1-6 haloalkyl; and n represents 0 or 1 and the compounds are used as insecticides, and a use of the new compounds as insecticides.Type: ApplicationFiled: July 21, 2006Publication date: August 27, 2009Applicant: BAYER CROPSCIENCE AGInventors: Akihiko Yanagi, Yukiyoshi Watanabe, Katsuaki Wada, Tetsuya Murata, Jun Mihara, Katsuhiko Shibuya, Eiichi Shimojo, Akira Emoto
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Patent number: 7566716Abstract: Compounds of Formula I are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formula I, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: May 18, 2006Date of Patent: July 28, 2009Assignee: Array Biopharma Inc.Inventors: Ellen Laird, George Topalov, Joseph P. Lyssikatos, Mike Welch, Jonas Grina, Josh Hansen, Brad Newhouse
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Publication number: 20090170911Abstract: Azole compounds represented by formula I: wherein ring A is isoxazole and the like, R1 is a substituted or unsubstituted aryl group and the like, R2 is a hydrogen atom and the like, and R3 is a substituted or unsubstituted alkyl group and the like, and pharmaceutically acceptable salts thereof inhibit the physiological activity of lysophosphatidic acid (LPA), and are useful as for the prophylaxis or treatment of diseases in which inhibition of the physiological activity of LPA is useful for the prophylaxis or treatment thereof, such as diseases involving the LPA receptor.Type: ApplicationFiled: February 20, 2009Publication date: July 2, 2009Applicant: AJINOMOTO CO. INCInventors: Takashi YAMAMOTO, Akira Chiba, Koichi Fujita, Yuka Kataba, Koji Ohsumi, Sayaka Asari, Naoyuki Fukuchi, Misato Noguchi, Itsuya Tanabe, Chiori Ijichi, Naoko Oomuta, Yuko Iida, Satoshi Iwayama
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Publication number: 20090137573Abstract: 1,3-disubstituted 4-methyl-1H-pyrrole-2-carboxamides corresponding to formula I methods for their production, pharmaceutical compositions containing them, and the use thereof for noradrenalin receptor regulation, particularly for inhibiting noradrenalin reuptake, and/or for 5-HT receptor regulation, particularly for inhibiting 5-hydroxy tryptophan reuptake, and/or for opioid receptor regulation and/or for batrachotoxin (BTX) receptor regulation and/or for treating or inhibiting pain and other conditions.Type: ApplicationFiled: December 9, 2008Publication date: May 28, 2009Applicant: Gruenenthal GmbHInventors: Stefan Oberboersch, Bernd Sundermann, Corinna Sundermann, Edward Bijsterveld, Hagen-Heinrich Hennies
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Publication number: 20090099242Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: ApplicationFiled: August 15, 2008Publication date: April 16, 2009Inventors: Gregory D. Cuny, Xin Teng, Junying Yuan, Alexei Degterev, John A. Porco, JR.
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Patent number: 7514459Abstract: Compounds of formula I: are potent inhibitors of gamma-secretase and hence find use in treatment or prevention of diseases associated with deposition of ?-amyloid.Type: GrantFiled: September 16, 2004Date of Patent: April 7, 2009Assignee: Merck Sharp & Dohme Ltd.Inventors: Ian James Collins, Joanne Clare Hannam, Andrew Madin, Mark Peter Ridgill
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Publication number: 20090048225Abstract: The present invention provides a novel compound of Formula (I) or a pharmaceutically acceptable salt thereof, having histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another, embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.Type: ApplicationFiled: August 15, 2005Publication date: February 19, 2009Inventors: Don Richard Finley, Terry Patrick Finn, Philip Arthur Hipskind, William Joseph Hornback, Cynthia Darshini Jesudason, Takako Takakuwa
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Publication number: 20090042866Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.Type: ApplicationFiled: November 23, 2005Publication date: February 12, 2009Inventors: William Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
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Publication number: 20090042918Abstract: Compounds of formula (I), useful for inhibiting PIM-I and/or PIM-3: and pharmaceutically acceptable salts thereof, wherein Y, Z, R1, R3, Q, X and R4 are as defined above. Pharmaceutical compositions and methods of treating diseases and conditions, such as cancer, are also disclosed.Type: ApplicationFiled: October 5, 2006Publication date: February 12, 2009Applicant: EXELIXIS, INC.Inventors: Patrick Kearney, S. David Brown, Elena S. Koltun
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Publication number: 20090032106Abstract: There is provided novel n-type conjugated compounds based on 2-vinyl-4,5-dicyanoimidazole moieties conjugated via the vinyl group to an aromatic moiety. Also provided are thin films and photovoltaics comprising the novel compounds, as well as methods of synthesizing the compounds.Type: ApplicationFiled: July 31, 2007Publication date: February 5, 2009Inventors: Alan Sellinger, Richard Yee Cheong Shin, Thomas Kietzke, Zhikuan Chen, Sundarraj Sudhakar
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Publication number: 20090029995Abstract: This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R1, Q, S, T, U, V, and R2 are as defined in the specification. The invention also provides pharmaceutical compositions and methods of treating diseases.Type: ApplicationFiled: November 29, 2006Publication date: January 29, 2009Applicants: WARNER-LAMBERT COMPANY, WARNER-LAMBERT COMPANY LLCInventors: Amy Mae Bunker, Mark Anthony Morris, Patrick Michael O'Brien, Michael William Wilson
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Patent number: 7482465Abstract: The invention relates to indol derivatives of Formula (I) in which R1, R2, R3, X, A, n, m and p have the meanings indicated above.Type: GrantFiled: November 17, 2003Date of Patent: January 27, 2009Assignee: Merck Patent GmbHInventors: Günter Hölzemann, Helene Crassier, Henning Böttcher, Timo Heinrich, Kai Schiemann, Joachim Leibrock, Chrisoph Van Amsterdam, Gerd Bartoszyk, Christoph Seyfried
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Publication number: 20090023730Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.Type: ApplicationFiled: February 25, 2008Publication date: January 22, 2009Applicant: ACHILLION PHARMACEUTICALSInventors: Avinash Phadke, Dawei Chen, Milind Deshpande, Andrew Thurkauf, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
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Patent number: 7439242Abstract: Modulators of PPAR? activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.Type: GrantFiled: April 15, 2002Date of Patent: October 21, 2008Assignee: Amgen Inc.Inventors: Jonathan B. Houze, Lawrence R. McGee, Steven Marc Rubenstein
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Publication number: 20080249095Abstract: Compounds of the formula (I), in which R1, R2, R3a, R3b, R3c and R3d have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: July 18, 2006Publication date: October 9, 2008Inventors: Dieter Dorsch, Oliver Schadt, Andree Blaukat
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Publication number: 20080200457Abstract: The present invention relates to 1,2,3 -thiadiazole compounds represented by formula (I): wherein R1, R2, R3, R4 and R5 each represents H, halogen, CN, alkyl, alkoxyalkyl, aryl, arylalkyl, alkylcarbonyl or the like; R6 represents —C?(W1)YR7 in which R7 reresents H, alkyl, alkenyl, phenylcarbonyl, heterocyclic ring-carbonyl, arylsulfonyl or the like; Y represents O, S, —N(R11), —N(R11)O— in which R11 represents H, alkyl, cycloalkyl, substituted phenyl, or the like; W1 represents O or S; and symbols in the formula are defined in detail in the specification or salts thereof, and to a plant disease control agent for agricultural and horticultural use which contains the compound as an active ingredient.Type: ApplicationFiled: February 23, 2006Publication date: August 21, 2008Applicant: NIHON NOHYAKU CO., LTD.Inventors: Kunihisa Umetani, Takashi Shimaoka, Minoru Yamaguchi, Masatsugu Oda, Nobuo Kyomura, Tsuyoshi Takemoto, Kazuhiko Kikutake
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Patent number: 7414142Abstract: Compounds of formula I, wherein R1-R9 and n are defined herein, and pharmaceutical compositions and kits containing these compounds are provided. Also provided are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I or formula II, wherein R3-R5, R10, and R11 are defined herein.Type: GrantFiled: September 18, 2006Date of Patent: August 19, 2008Assignee: WyethInventors: Puwen Zhang, Jeffrey Curtis Kern, Eugene Anthony Terefenko, Eugene John Trybulski
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Patent number: 7407976Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: November 15, 2004Date of Patent: August 5, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark T. Miller, Sarah S. Hadida Ruah, Peter D. J. Grootenhuis, Matthew Hamilton
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Patent number: 7402606Abstract: Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle substituted ketoamide derivatives as well as method of using the same in the manufacture of medicaments for the treatment of disorders, including osteoporosis, associated with an imbalance between bone resorption and formation which can ultimately lead to fracture.Type: GrantFiled: April 1, 2003Date of Patent: July 22, 2008Assignee: SmithKline Beecham CorporationInventors: David Gene Barrett, John G. Catalano, David Norman Deaton, Aaron Bayne Miller, John A. Ray, Vicente Samano
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Publication number: 20080132506Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.Type: ApplicationFiled: June 9, 2006Publication date: June 5, 2008Inventors: Daniel L. Flynn, Peter A. Petillo
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Publication number: 20080132511Abstract: Certain sulfonamide compounds are dual CCK1/CCK2 inhibitors useful in the treatment of CCK1/CCK2 mediated diseases.Type: ApplicationFiled: November 20, 2007Publication date: June 5, 2008Inventors: Brett ALLISON, Victor K. Phuong, Marna C.W. Pippel, Michael H. Rabinowitz, Hariharan Venkatesan
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Patent number: 7378448Abstract: A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3?, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosedType: GrantFiled: March 2, 2005Date of Patent: May 27, 2008Assignee: Eli Lilly and CompanyInventors: Charles Howard Mitch, Steven James Quimby, Miles Goodman Siegel