1,3-thiazines Patents (Class 514/226.8)
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Patent number: 11014896Abstract: Provided are methods of treating and/or preventing dermatological disorders. Provided are methods of reducing skin inflammation, reducing pain, and/or reducing itch in a subject in need thereof. The methods may include administering to the subject an effective amount of a TRPA1 and/or TRPV4 inhibitor. Further provided are compositions including a TRPA1 and/or TRPV4 inhibitor compound in combination with a carrier, vehicle, or diluent that is suitable for topical application.Type: GrantFiled: April 22, 2019Date of Patent: May 25, 2021Assignee: Duke UniversityInventors: Wolfgang Liedtke, Farshid Guilak
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Patent number: 10793557Abstract: Compounds of general formula (I), of general formula (II), of general formula (III), of general formula (IV), of general formula (V), of general formula (VI), and their pharmaceutically acceptable salts, wherein all variables are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer.Type: GrantFiled: April 1, 2019Date of Patent: October 6, 2020Assignee: Merck Sharp & Dohme Corp.Inventors: Michael D. Altman, Brandon D. Cash, Matthew Lloyd Childers, Jared N. Cumming, Duane E. DeMong, Andrew Marc Haidle, Timothy J. Henderson, James P. Jewell, Matthew A. Larsen, Jongwon Lim, Min Lu, Ryan D. Otte, Benjamin Wesley Trotter
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Patent number: 10278955Abstract: One embodiment is a method of treating cancer. The method includes administering a therapeutically effective amount of a compound to a patient.Type: GrantFiled: December 13, 2017Date of Patent: May 7, 2019Assignee: Macau University of Science and TechnologyInventors: Xiao Jun Yao, Lai Han Elaine Leung, Liang Liu, Qian Qian Wang, Jia Hui Xu, Ying Li
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Patent number: 9925191Abstract: Fumarate compounds, pharmaceutical compositions comprising the fumarate compounds, and methods of using fumarate compounds and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed.Type: GrantFiled: June 19, 2016Date of Patent: March 27, 2018Inventor: Mark Quang Nguyen
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Publication number: 20150031687Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4 and A are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: September 10, 2013Publication date: January 29, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Lei Guo, Taishan Hu, Yimin Hu, Buelent Kocer, Xianfeng Lin, Haixia Liu, Alexander V Mayweg, Zongxing Qiu, Hong Shen, Guozhi Tang, Lisha Wang, Guolong Wu, Shixiang Yan, Weixing Zhang, Mingwei Zhou, Wei Zhu
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Publication number: 20150018346Abstract: The present invention relates to methods of inhibiting one or more signs of aging and/or degenerative disorder in a subject in need of such treatment, which comprise administering, to the subject, an effective amount of one or more of the compounds as set forth herein. “Inhibiting a sign of aging or degenerative disorder” means reducing the risk of occurrence, delaying the onset, slowing the progression, and/or reducing the severity and/or manifestation, of a sign of aging or degenerative disorder, and includes, but is not limited to, preventing the occurrence, development or progression of a sign of aging or degenerative disorder.Type: ApplicationFiled: March 18, 2014Publication date: January 15, 2015Applicant: University of Pittsburgh - Of the Commonwealth System of Higher EducationInventors: Laura J. Niedernhofer, Paul D. Robbins, Peter Wipf
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Patent number: 8563779Abstract: A description is given of (4-trifluoromethyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.Type: GrantFiled: July 19, 2011Date of Patent: October 22, 2013Assignee: Bayer CropScience AGInventors: Hartmut Ahrens, Andreas Van Almsick, Elmar Gatzweiler, Dieter Feucht, Isolde Haeuser-Hahn, Stefan Lehr, Christopher Hugh Rosinger
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Publication number: 20130267415Abstract: The present invention relates to pesticidal mixtures comprising a component A and a component B, wherein component A is a compound of formula I wherein one of Y1 and Y2 is S, SO or SO2 and the other is CH2; L is a direct bond or methylene; A1 and A2 are C—H, or one of A1 and A2 is C—H and the other is N; R1 is hydrogen or methyl; R2 is chlorodifluoromethyl or trifluoromethyl; R3 is 3,5-dibromo-phenyl, 3,5-dichloro-phenyl, 3,4-dichloro-phenyl, or 3,4,5-trichloro-phenyl, 3,5-dichloro-4-fluoro-phenyl, or 3,5-bis-trifluoromethylphenyl; R4 is methyl or chlorine; R5 is hydrogen; or R4 and R5 together form a bridging 1,3-butadiene group; and wherein component B is an insecticide. The invention also relates to methods of controlling insects, acarines, nematodes or molluscs which comprises applying to a pest, to a locus of a pest, or to a plant susceptible to attack by a pest a combination of components A and B.Type: ApplicationFiled: December 15, 2011Publication date: October 10, 2013Applicant: SYNGENTA PARTICIPATIONS AGInventors: Peter Renold, Jerome Yves Cassayre, Myriem El Qacemi, Jagadish Pabba, Thomas Pitterna
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Patent number: 8507472Abstract: Bicyclic pyridinylpyrazoles of the formula (I) in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling unwanted microorganisms in crop protection and the protection of materials and for reducing mycotoxins in plants and plant parts, and also processes for preparing compounds of the formula (I).Type: GrantFiled: April 5, 2011Date of Patent: August 13, 2013Assignee: Bayer CropScience AGInventors: Amos Mattes, Hendrik Helmke, Stefan Hillebrand, Gorka Peris, Alexander Sudau, Lars Rodefeld, Stefan Gauger, Jürgen Benting, Peter Dahmen, Ruth Meissner, Ulrike Wachendorff-Neumann, Hiroyuki Hadano
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Patent number: 8450308Abstract: The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.Type: GrantFiled: August 14, 2009Date of Patent: May 28, 2013Assignee: Vitae Pharmaceuticals, Inc.Inventors: Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
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Patent number: 8334316Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.Type: GrantFiled: February 9, 2009Date of Patent: December 18, 2012Assignee: ACEA Biosciences, Inc.Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
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Publication number: 20120277222Abstract: Novel compounds and methods for activating the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing four six-membered rings and a substituted or unsubstituted C5 or C6 heteroaryl or heterocycloalkyl ring and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods and compounds for the treatment of disorders including neurologic, neuropsychiatric, and metabolic disorders are provided. For example, a method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes selecting a subject with or at risk of developing depression, anxiety, or obesity, and administering to the subject a therapeutically effective amount of the described compounds.Type: ApplicationFiled: May 24, 2012Publication date: November 1, 2012Applicant: EMORY UNIVERSITYInventor: Keqiang Ye
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Patent number: 8263527Abstract: Insecticidal compositions suitable for use in preparation of insecticidal liquid fertilizers comprising a pyrethroid, a hydrated aluminum-magnesium silicate, and at least one dispersant selected from the group consisting of a sucrose ester, a lignosulfonate, an alkylpolyglycoside, a naphthalenesulfonic acid formaldehyde condensate and a phosphate ester are disclosed.Type: GrantFiled: September 9, 2011Date of Patent: September 11, 2012Assignee: FMC CorporationInventor: Timothy Martin
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Publication number: 20120122856Abstract: The present invention relates to liquid termiticide compositions comprising a pyrethroid and a neonicotinoid selected from the group consisting of imidacloprid, nithiazine, thiamethoxam, dinotefuran, nitenpyram, thiacloprid and clothianadin, these compositions result in an increase in termite mortality at low application rates and a continuous chemical bather of a termiticide in soil surrounding and beneath a structure in a locus where termites are suspected or known to exist.Type: ApplicationFiled: January 19, 2012Publication date: May 17, 2012Applicant: FMC CORPORATIONInventors: James B. Ballard, Cristi L. Palmer, Kim Watson
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Publication number: 20120115722Abstract: Disclosed are compositions comprising (a) at least one compound selected from compounds of Formula 1, N-oxides, and salt thereof, wherein R1 is phenyl optionally substituted with up to 5 substituents independently selected from R3, or pyridinyl optionally substituted with up to 4 substituents independently selected from R3; R2 is C1-C4 haloalkyl; or thiazolyl, pyridinyl or pyrimidinyl, each optionally substituted with up to 2 substituents independently selected from the group consisting of halogen and C1-C4 alkyl; each R3 is independently halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C(R4)?NOR4 or Q; each R4 is independently C1-C4 alkyl; Z is CH?CH or S; and each Q is independently phenyl or pyridinyl, each optionally substituted with up to 3 substituents independently selected from the group consisting of halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy and C1-C4 haloalkoxy; and (b) at least one invertebrate pest control agent.Type: ApplicationFiled: August 3, 2010Publication date: May 10, 2012Applicant: E. I. DU PONT DE NEMOURS AND COMPANYInventors: Caleb William Holyoke, JR., Wenming Zhang, My-Hanh Thi Tong
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Publication number: 20120053051Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2 and A3 are independently selected from the group consisting of CR3 and N; B1 B2 and B3 are independently selected from the group consisting of CR2 and N; Q is a phenyl ring or a 5- or 6-membered saturated or unsaturated heterocyclic ring, each ring optionally substituted with one or more substituents independently selected from halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, —CN, —NO2, —N(R4)R5, —C(W)N(R4)R5, —C(O)OR5 and R8; or —S(O)2N(R21)R22, —S(O)pR25 or —S(O)(?NR28)R29; and R1, R2, R3, R4, R5, R8, R21, R22, R25, R28, R29; p and n are as defined in the disclosure.Type: ApplicationFiled: February 28, 2011Publication date: March 1, 2012Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: George Philip Lahm, Kanu Maganbhai Patel, Thomas Francis Pahutski, JR., Benjamin Kenneth Smith
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Publication number: 20120004103Abstract: Insecticidal compositions suitable for use in preparation of insecticidal liquid fertilizers comprising a pyrethroid, a hydrated aluminum-magnesium silicate, and at least one dispersant selected from the group consisting of a sucrose ester, a lignosulfonate, an alkylpolyglycoside, a naphthalenesulfonic acid formaldehyde condensate and a phosphate ester are disclosed.Type: ApplicationFiled: September 9, 2011Publication date: January 5, 2012Applicant: FMC CORPORATIONInventor: Timothy Martin
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Publication number: 20110251178Abstract: Bicyclic pyridinylpyrazoles of the formula (I) in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling unwanted microorganisms in crop protection and the protection of materials and for reducing mycotoxins in plants and plant parts, and also processes for preparing compounds of the formula (I).Type: ApplicationFiled: April 5, 2011Publication date: October 13, 2011Applicant: Bayer CropScience AGInventors: Amos MATTES, Hendrik HELMKE, Stefan HILLEBRAND, Gorka PERIS, Alexander SUDAU, Lars RODEFELD, Stefan GAUGER, Jürgen BENTING, Peter DAHMEN, Ruth MEISSNER, Ulrike WACHENDORFF-NEUMANN, Hiroyuki HADANO
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Publication number: 20110218192Abstract: The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.Type: ApplicationFiled: August 14, 2009Publication date: September 8, 2011Applicant: VITAE PHARMACEUTICALS, INC.Inventors: Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
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Publication number: 20110150957Abstract: The present invention relates to an insecticidal granular composition, comprising (a) at least one insecticide, selected from the group consisting of an enaminocarbonyl compound, a neonicotinoid, a tetronic acid derivative or a tetramic acid derivative compound, a carbamate compound, an organophosphate compound, a diamide compound, a pyrethroid compound and flonicamid; (b) optionally at least one moisture-retaining agent; and (c) vegetable meal.Type: ApplicationFiled: August 26, 2009Publication date: June 23, 2011Applicant: Bayer CropScience AGInventors: Wolfgang Wirth, Wolfgang Thielert, Heike Hungenberg, Jean-Pierre Trijau
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Publication number: 20110152081Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2 and A3 are independently selected from the group consisting of CR3 and N; B1 B2 and B3 are independently selected from the group consisting of CR2 and N; Q is a phenyl ring or a 5- or 6-membered saturated or unsaturated heterocyclic ring, each ring optionally substituted with one or more substituents independently selected from halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, —CN, —NO2, —N(R4)R5, —C(W)N(R4)R5, —C(O)OR5 and R8; or —S(O)2N(R21)R22, —S(O)pR25 or —S(O)(?NR28)R29; and R1, R2, R3, R4, R5, R8, R21, R22, R25, R28, R29; p and n are as defined in the disclosure.Type: ApplicationFiled: February 28, 2011Publication date: June 23, 2011Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: George Philip Lahm, Kanu Maganbhai Patel, Thomas Francis Pahutski, JR., Benjamin Kenneth Smith
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Publication number: 20110144096Abstract: Novel compounds and methods for activating the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing four six-membered rings and a substituted or unsubstituted C5 or C6 heteroaryl or hetero-cycloalkyl ring and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods and compounds for the treatment of disorders including neurologic, neuropsychiatric, and metabolic disorders are provided. For example, a method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes selecting a subject with or at risk of developing depression, anxiety, or obesity, and administering to the subject a therapeutically effective amount of the described compounds.Type: ApplicationFiled: July 28, 2009Publication date: June 16, 2011Applicant: EMORY UNIVERSITYInventor: Keqiang Ye
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Patent number: 7947675Abstract: Compounds of the formula (I), in which the radicals R1 to R3 and AR are as defined in the description, processes for the preparation thereof, the use thereof in the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.Type: GrantFiled: February 16, 2006Date of Patent: May 24, 2011Assignee: Merck Patent GmbHInventors: Bruno Roux, Isabelle Berard
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Patent number: 7939537Abstract: Pyridopyrimidine carboxamide compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein R1, R2, R3, R4, R5 and R6 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: September 26, 2006Date of Patent: May 10, 2011Assignee: Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.p.A.Inventors: Vincenzo Summa, Olaf Kinzel, Monica Donghi
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Publication number: 20110105481Abstract: A compound or its pharmaceutically acceptable salt, optionally including both individual enantiomeric forms, a racemate, diastereomers and mixtures thereof, composition and method are disclosed that can provide analgesia and reduce inflammation. A contemplated compound has a structure that corresponds to Formula A, wherein the R group substituents, d, e, f, k, n, m, D, E, F, K, G, P, Q, W, and Z are defined within.Type: ApplicationFiled: March 8, 2010Publication date: May 5, 2011Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
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Patent number: 7879886Abstract: Composition, article of manufacture for and method of treating malaria in a human having an infestation of Plasmodium protozoans are described. The method comprises administering a therapeutically-effective amount of a compound of formula (I) or (IV), i.e. sufficient quantity to reduce the population of Plasmodium. The composition of the invention is a compound of formula (I) or (IV) with a pharmaceutical excipient. The article of manufacture is the composition in combination with labeling for treating malaria. The substituents are detailed in the specification.Type: GrantFiled: October 17, 2006Date of Patent: February 1, 2011Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 7776867Abstract: The present invention relates to furanopyrimidine compounds having the general Formula I: and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula I, methods of treating various diseases and conditions in a mammal, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma and thymoma, comprising administering to the mammal a therapeutically effective amount of a compound of Formula I.Type: GrantFiled: June 29, 2005Date of Patent: August 17, 2010Assignee: Amgen Inc.Inventors: John Laird Buchanan, William H. Buckner, Simon A. Burkitt, Erin F. DiMauro, Christopher N. Farthing, Alexander D. Frenkel, Martin J. Harrison, Frank Kayser, Jinqian Liu, Sarah E. Lively, Teresa L. Marshall, David C. McGowan, Rajiv Sharma, Stephen J. Shuttleworth, Xiaotian Zhu
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Publication number: 20100183629Abstract: Antagonists of S1P3 (Edg-3) receptors are provided for attenuation of Smad signaling in a method of down-regulation of receptor signaling and downstream decreased production of connective tissue growth factor in ocular disorders involving CTGF accumulation. Ocular disorders involving inappropriate CTGF accumulation include ocular hypertension, glaucoma, glaucomatous retinopathy, optic neuropathy, macular degeneration, diabetic retinopathy, choroidal neovascularization, proliferative vitreoretinopathy and ocular wound healing, for example. Such disorders are treated by administering antagonists of the present invention.Type: ApplicationFiled: March 29, 2010Publication date: July 22, 2010Applicant: ALCON RESEARCH, LTD.Inventors: Debra L. Fleenor, Allan R. Shepard, Iok-Hou Pang
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Patent number: 7687067Abstract: A compound of general formula (I): A process for preparing this compound. An intermediate of general formula (II) for the preparation of a compound of general formula (I). A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: GrantFiled: April 25, 2005Date of Patent: March 30, 2010Assignee: Bayer Cropscience S.A.Inventors: Pierre-Yves Coqueron, Darren James Mansfield, Philippe Desbordes, Heiko Rieck, Marie-Claire Grosjean-Cournoyer, Pierre Genix, Alain Villier
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Publication number: 20100056504Abstract: The compounds represented in general formula (1) and a salt thereof are useful for glucocorticoid receptor modulator. The R1 represents a hydrogen atom or a lower alkyl group; R2 represents a hydrogen atom or a lower alkyl group; R3 and R4 may be the same or different and represent a hydrogen atom or a lower alkyl group; R5 represents a hydrogen atom or a lower alkyl group; R6 represents a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group or a nitro group; X represents —C(O)—, —C(O)NR8—, —S(O)2— and the like; R7 and/or R8 may be the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, a heterocyclic group which may have a substituent, a lower alkoxy group which may have a substituent and the like; Y represents a lower alkylene group; Z represents a chalcogen atom; and P represents 0, 1, 2 or 3.Type: ApplicationFiled: November 14, 2007Publication date: March 4, 2010Inventors: Mamoru Matsuda, Masato Nagatsuka, Toshiyuki Mori, Sachiko Kobayashi, Masatomo Kato, Miwa Takai
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Publication number: 20090048256Abstract: The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc., R3 is an alkyl group etc., E is one of the following groups of the formula (i) to (iv): Q1 is a single bond, an alkylene group or a group of the formula: —N(R7)—, R7 is a hydrogen atom or an alkyl group, Q2 is a single bond, an oxygen atom or an alkylene group, R4 is a cycloalkyl group, a group of the formula: —N(R5)(R6) etc., one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: —N(R8)(R9) etc., D is an oxygen atom etc., RA1 is an amino group etc., RA2 is an optionally substituted aliphatic heterocyclic group, R is an alkyl group optionally substituted by one to three halogen atom(s) etc., one of R8 and R9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc.Type: ApplicationFiled: October 20, 2006Publication date: February 19, 2009Inventors: Yasunori Moritani, Ritsuo Imashiro, Atsushi Sato
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Patent number: 7482337Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: October 28, 2003Date of Patent: January 27, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Michael Mark, Mohammad Tadayyon, Ralf R. H. Lotz
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Patent number: 7482339Abstract: The formula (I): wherein each of R2 and R3 is, same or different, C2-C4 alkyl or the like; or R2 and R3 are taken together with the adjacent carbon atom to form a 5 to 8 membered non-aromatic carbocyclic ring; R4 is C1-C6 alkyl or the like; X is an oxygen atom or a sulfur atom; A is the group of the formula: wherein R1 is, same or different, alkyl or the like; W is C2-C6 alkylene which may contain an optionally substituted heteroatom(s) or the like; n is an integer of 0 to 7, a pharmaceutically acceptable salt, or a solvate thereof.Type: GrantFiled: August 24, 2004Date of Patent: January 27, 2009Assignee: Shionogi and Co., Ltd.Inventors: Hiroyuki Kai, Yasuhide Morioka, Katsumi Koike
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Patent number: 7459450Abstract: The present invention discloses compounds, which are novel receptor antagonists for NPY Y1 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y1 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: April 28, 2005Date of Patent: December 2, 2008Assignee: Schering CorporationInventors: Zhaoning Zhu, Zhong-Yue Sun, Yuanzan C. Ye, Deborra E. Mullins, Brian McKittrick, Andrew Stamford, William J. Greenlee
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Patent number: 7384938Abstract: The present invention relates to water-containing formulations for the dermal control of parasitic insects on animals, having the following composition a) agonists or antagonists of the nicotinic acetylcholine receptors of insects in a concentration of from 1 to 20% by weight based on the overall weight of the formulation; b) water in a concentration of from 2.5 to 15% by weight; c) solvents from the group alcohols such as benzyl alcohol, tetrahydrofuryl alcohol or optionally substituted pyrrolidones in a concentration of at least 20% by weight based on the overall weight of the formulation; d) solvents from the group of the cyclic carbonates or lactones in a concentration of from 5 to up to 50% by weight based on the overall weight of the formulation; e) if desired, further auxiliaries from the group thickeners, spreading agents, colorants, antioxidants, propellants, preservatives, adhesives, emulsifiers, in a concentration of from 0.025 up to 10% by weight based on the overall weight of the formulation.Type: GrantFiled: January 17, 2003Date of Patent: June 10, 2008Assignee: Bayer AktiengesellschaftInventors: Kirkor Sirinyan, Hubert Dorn, Ulrich Heukamp
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Patent number: 7375102Abstract: Compounds are provided having the formula: wherein variables A1, A2, A3, A4, R1, R2, R3, R4, Q and L are as described herein. The subject compounds are useful for treatment of inflammatory and immune conditions and diseases. Compositions and methods of treatment using the subject compounds are also provided. For example, the subject methods are useful for treatment of inflammatory and immune disorders and disease such as multiple sclerosis, rheumatoid arthritis, psoriasis, and inflammatory bowel disease.Type: GrantFiled: June 27, 2005Date of Patent: May 20, 2008Assignee: AMGEN SF, LLCInventors: Zice Fu, Michael G. Johnson, An-Rong Li, Andrew P. Marcus, Julio C. Medina, Philippe Bergeron, Xiaoqi Chen, Xiaohui Du, Jeffrey Deignan, Jason A. Duquette, Darin Gustin, Jeffrey T. Mihalic, Jiwen Liu
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Patent number: 7223754Abstract: The invention relates to methods of using Cav2.2 subunit calcium channel modulators, particularly thiazolidinone, oxazolidinone, and imidazolone derivatives, to treat lower urinary tract and related disorders.Type: GrantFiled: November 17, 2004Date of Patent: May 29, 2007Assignee: Dynogen Pharmaceuticals, Inc.Inventors: Matthew Oliver Fraser, Karl Bruce Thor, Edward C. Burgard
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Patent number: 7205309Abstract: Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3 and A have the significance given in the specification are provided. The compounds can be used for the treatment or prevention of obesity.Type: GrantFiled: July 3, 2003Date of Patent: April 17, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Patrizio Mattei, Werner Mueller, Werner Neidhart, Matthias Heinrich Nettekoven, Philippe Pflieger
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Patent number: 7166590Abstract: A compound of the formula (I): [wherein R1 is (substituted) alkyl, alkoxy, phenyl, hetero ring etc.; A is bond, CO, SO2; R2 is H, (substituted) alkyl etc.; D is alkylene etc.; E is COO, OCO, O, S, SO, SO2 etc.; R3 is (substituted) alkyl, carbocyclic ring, hetero ring; J is O, NR16 (R16 is H, substituted alkyl); R4 is (substituted) alkyl, carbocyclic ring, hetero ring.] or non-toxic salt thereof, and an N-type calcium channel blocker comprising it as an active ingredient. The compounds of the formula (I) possess an inhibitory action on N-type calcium channel, so they are useful as agent for the prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis or epilepsy etc. or agent for the treatment of pain.Type: GrantFiled: May 28, 2002Date of Patent: January 23, 2007Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Takuya Seko, Masashi Kato
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Patent number: 7166609Abstract: Pyrimidine-4,6-dicarboxylic acid diamides of the formula I are suitable for selectively inhibiting collagenase (MMP 13). The pyrimidine-4,6-dicarboxylic acid diamides can therefore be used for treating degenerative joint diseases.Type: GrantFiled: November 3, 2003Date of Patent: January 23, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Otmar Klingler, Reinhard Kirsch, Joerg Habermann, Klaus-Ulrich Weithmann, Christian Engel, Bernard Pirard
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Patent number: 7148221Abstract: 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: August 1, 2005Date of Patent: December 12, 2006Assignee: Amgen Inc.Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Hui-Ling Wang, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Celia Dominguez, James Richard Falsey, Christopher Hulme, Jodie Katon, Thomas Nixey, Vassil I. Ognyanov, Liping H. Pettus, Robert Michael Rzasa
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Patent number: 7087626Abstract: Novel pyrrazole derivative compounds and their use as pharmaceutical agents, in particular their use as TGF-beta signal transduction inhibitors.Type: GrantFiled: May 13, 2002Date of Patent: August 8, 2006Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Todd Vincent DeCollo, Alexander Glenn Godfrey, Theodore Goodson, Jr., Hong-Yu Li, William Thomas McMillen, Shawn Christopher Miller, Jason Scott Sawyer, Edward C. R. Smith, Jonathan Michael Yingling
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Patent number: 7084151Abstract: The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by Progesterone Receptor. Also provided are methods of making such compounds and pharmaceutical compositions.Type: GrantFiled: October 10, 2003Date of Patent: August 1, 2006Assignee: Ligand Pharmaceuticals IncorporatedInventors: Lin Zhi, Cornelis Arjan Van Oeveren
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Patent number: 7022705Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein, for example, HET is an N-linked 5-membered, fully or partially unsaturated heterocyclic ring, or HET is an N-linked 6-membered di-hydro-heteroaryl ring; Q is, for example, Q1 or Q2: wherein R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example a group of the formula (TC7) wherein Rc is, for example, hydrogen, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1–10C)alkyl or R14C(O)O(1–6C)alkyl wherein R14 is optionally substituted (1–10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.Type: GrantFiled: October 23, 2002Date of Patent: April 4, 2006Assignee: AstraZeneca ABInventor: Michael John Betts
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Patent number: 6936606Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful for treating autoimmune and other diseases.Type: GrantFiled: September 27, 2002Date of Patent: August 30, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R. R. Young, Eugene R. Hickey, Weimin Liu, Usha R. Patel
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Patent number: 6916806Abstract: A compound of the formula (I) having a binding activity to the cannabinoid type 2 receptor: wherein R1 is optionally substituted heterocyclic group or the like; R2 and R2 each is independently hydrogen or the like; m is an integer of 0 to 2; A is optionally substituted aromatic carbocyclic group or the like.Type: GrantFiled: February 14, 2002Date of Patent: July 12, 2005Assignee: Shionogi & Co., Ltd.Inventors: Hiroyuki Kai, Takami Murashi, Minoru Tomida
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Patent number: 6903119Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-type calcium channel, so they are useful as drug for prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis, epilepsy, asthma and pollakiuria etc. or agent for the treatment of pain.Type: GrantFiled: July 13, 1999Date of Patent: June 7, 2005Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Takuya Seko, Masashi Kato
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Publication number: 20040235751Abstract: The present invention provides methods of inhibiting release of zinc from neurons and of preventing zinc-mediated brain injury. Also provided are methods of improving cerebral blood flow while preventing zinc-mediated brain injury. Inhibitors of or activators of nitric oxide synthases modulate nitric oxide synthesis to reduce nitric oxide-induced release of neurotoxic amounts of zinc, thereby reducing zinc-mediated neuronal injury after brain trauma.Type: ApplicationFiled: March 22, 2004Publication date: November 25, 2004Inventor: Christopher J. Frederickson
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Patent number: 6767907Abstract: 4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH2 and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9 is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10 and R11 are hydrogen, alkyl or aryl, or R10 and R11 are linked to form a ring; R2 is hydrogen, alkyl, cykcloalkyl or cycloalkylalkyl; or R1 and R2 are linked to form a ring; R3-R5 are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6 and R7 are hydrogen or alkyl or they are linked to constitute 3-7 membered ring; R8 is hydrogen or alkyl; have effects at cType: GrantFiled: April 14, 2000Date of Patent: July 27, 2004Assignee: H. Lundbeck A/SInventors: Jens Kristian Perregaard, John Willie Stenberg, Bitten Hansen
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Patent number: RE39130Abstract: Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group in which R2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R3 represents a hydrogen atom or an alkyl group, and Z represents an optionally substituted 5- or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group. The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.Type: GrantFiled: June 6, 1994Date of Patent: June 13, 2006Assignee: Bayer Cropscience K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hatori