1,3-thiazines Patents (Class 514/226.8)
  • Patent number: 11014896
    Abstract: 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: Grant
    Filed: April 22, 2019
    Date of Patent: May 25, 2021
    Assignee: Duke University
    Inventors: Wolfgang Liedtke, Farshid Guilak
  • Patent number: 10793557
    Abstract: 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: Grant
    Filed: April 1, 2019
    Date of Patent: October 6, 2020
    Assignee: 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
  • Patent number: 10278955
    Abstract: One embodiment is a method of treating cancer. The method includes administering a therapeutically effective amount of a compound to a patient.
    Type: Grant
    Filed: December 13, 2017
    Date of Patent: May 7, 2019
    Assignee: Macau University of Science and Technology
    Inventors: Xiao Jun Yao, Lai Han Elaine Leung, Liang Liu, Qian Qian Wang, Jia Hui Xu, Ying Li
  • Patent number: 9925191
    Abstract: 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: Grant
    Filed: June 19, 2016
    Date of Patent: March 27, 2018
    Inventor: Mark Quang Nguyen
  • Publication number: 20150031687
    Abstract: 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: Application
    Filed: September 10, 2013
    Publication date: January 29, 2015
    Applicant: 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
  • Publication number: 20150018346
    Abstract: 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: Application
    Filed: March 18, 2014
    Publication date: January 15, 2015
    Applicant: University of Pittsburgh - Of the Commonwealth System of Higher Education
    Inventors: Laura J. Niedernhofer, Paul D. Robbins, Peter Wipf
  • Patent number: 8563779
    Abstract: 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: Grant
    Filed: July 19, 2011
    Date of Patent: October 22, 2013
    Assignee: Bayer CropScience AG
    Inventors: Hartmut Ahrens, Andreas Van Almsick, Elmar Gatzweiler, Dieter Feucht, Isolde Haeuser-Hahn, Stefan Lehr, Christopher Hugh Rosinger
  • Publication number: 20130267415
    Abstract: 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: Application
    Filed: December 15, 2011
    Publication date: October 10, 2013
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Peter Renold, Jerome Yves Cassayre, Myriem El Qacemi, Jagadish Pabba, Thomas Pitterna
  • Patent number: 8507472
    Abstract: 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: Grant
    Filed: April 5, 2011
    Date of Patent: August 13, 2013
    Assignee: Bayer CropScience AG
    Inventors: 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
  • Patent number: 8450308
    Abstract: 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: Grant
    Filed: August 14, 2009
    Date of Patent: May 28, 2013
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
  • Patent number: 8334316
    Abstract: 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: Grant
    Filed: February 9, 2009
    Date of Patent: December 18, 2012
    Assignee: ACEA Biosciences, Inc.
    Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
  • Publication number: 20120277222
    Abstract: 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: Application
    Filed: May 24, 2012
    Publication date: November 1, 2012
    Applicant: EMORY UNIVERSITY
    Inventor: Keqiang Ye
  • Patent number: 8263527
    Abstract: 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: Grant
    Filed: September 9, 2011
    Date of Patent: September 11, 2012
    Assignee: FMC Corporation
    Inventor: Timothy Martin
  • Publication number: 20120122856
    Abstract: 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: Application
    Filed: January 19, 2012
    Publication date: May 17, 2012
    Applicant: FMC CORPORATION
    Inventors: James B. Ballard, Cristi L. Palmer, Kim Watson
  • Publication number: 20120115722
    Abstract: 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: Application
    Filed: August 3, 2010
    Publication date: May 10, 2012
    Applicant: E. I. DU PONT DE NEMOURS AND COMPANY
    Inventors: Caleb William Holyoke, JR., Wenming Zhang, My-Hanh Thi Tong
  • Publication number: 20120053051
    Abstract: 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: Application
    Filed: February 28, 2011
    Publication date: March 1, 2012
    Applicant: E.I. DU PONT DE NEMOURS AND COMPANY
    Inventors: George Philip Lahm, Kanu Maganbhai Patel, Thomas Francis Pahutski, JR., Benjamin Kenneth Smith
  • Publication number: 20120004103
    Abstract: 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: Application
    Filed: September 9, 2011
    Publication date: January 5, 2012
    Applicant: FMC CORPORATION
    Inventor: Timothy Martin
  • Publication number: 20110251178
    Abstract: 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: Application
    Filed: April 5, 2011
    Publication date: October 13, 2011
    Applicant: Bayer CropScience AG
    Inventors: 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
  • Publication number: 20110218192
    Abstract: 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: Application
    Filed: August 14, 2009
    Publication date: September 8, 2011
    Applicant: VITAE PHARMACEUTICALS, INC.
    Inventors: Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
  • Publication number: 20110152081
    Abstract: 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: Application
    Filed: February 28, 2011
    Publication date: June 23, 2011
    Applicant: E.I. DU PONT DE NEMOURS AND COMPANY
    Inventors: George Philip Lahm, Kanu Maganbhai Patel, Thomas Francis Pahutski, JR., Benjamin Kenneth Smith
  • Publication number: 20110150957
    Abstract: 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: Application
    Filed: August 26, 2009
    Publication date: June 23, 2011
    Applicant: Bayer CropScience AG
    Inventors: Wolfgang Wirth, Wolfgang Thielert, Heike Hungenberg, Jean-Pierre Trijau
  • Publication number: 20110144096
    Abstract: 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: Application
    Filed: July 28, 2009
    Publication date: June 16, 2011
    Applicant: EMORY UNIVERSITY
    Inventor: Keqiang Ye
  • Patent number: 7947675
    Abstract: 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: Grant
    Filed: February 16, 2006
    Date of Patent: May 24, 2011
    Assignee: Merck Patent GmbH
    Inventors: Bruno Roux, Isabelle Berard
  • Patent number: 7939537
    Abstract: 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: Grant
    Filed: September 26, 2006
    Date of Patent: May 10, 2011
    Assignee: Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.p.A.
    Inventors: Vincenzo Summa, Olaf Kinzel, Monica Donghi
  • Publication number: 20110105481
    Abstract: 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: Application
    Filed: March 8, 2010
    Publication date: May 5, 2011
    Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
  • Patent number: 7879886
    Abstract: 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: Grant
    Filed: October 17, 2006
    Date of Patent: February 1, 2011
    Assignee: University of Florida Research Foundation, Inc.
    Inventor: Raymond J. Bergeron, Jr.
  • Patent number: 7776867
    Abstract: 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: Grant
    Filed: June 29, 2005
    Date of Patent: August 17, 2010
    Assignee: 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
  • Publication number: 20100183629
    Abstract: 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: Application
    Filed: March 29, 2010
    Publication date: July 22, 2010
    Applicant: ALCON RESEARCH, LTD.
    Inventors: Debra L. Fleenor, Allan R. Shepard, Iok-Hou Pang
  • Patent number: 7687067
    Abstract: 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: Grant
    Filed: April 25, 2005
    Date of Patent: March 30, 2010
    Assignee: Bayer Cropscience S.A.
    Inventors: Pierre-Yves Coqueron, Darren James Mansfield, Philippe Desbordes, Heiko Rieck, Marie-Claire Grosjean-Cournoyer, Pierre Genix, Alain Villier
  • Publication number: 20100056504
    Abstract: 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: Application
    Filed: November 14, 2007
    Publication date: March 4, 2010
    Inventors: Mamoru Matsuda, Masato Nagatsuka, Toshiyuki Mori, Sachiko Kobayashi, Masatomo Kato, Miwa Takai
  • Publication number: 20090048256
    Abstract: 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: Application
    Filed: October 20, 2006
    Publication date: February 19, 2009
    Inventors: Yasunori Moritani, Ritsuo Imashiro, Atsushi Sato
  • Patent number: 7482337
    Abstract: 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: Grant
    Filed: October 28, 2003
    Date of Patent: January 27, 2009
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Michael Mark, Mohammad Tadayyon, Ralf R. H. Lotz
  • Patent number: 7482339
    Abstract: 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: Grant
    Filed: August 24, 2004
    Date of Patent: January 27, 2009
    Assignee: Shionogi and Co., Ltd.
    Inventors: Hiroyuki Kai, Yasuhide Morioka, Katsumi Koike
  • Patent number: 7459450
    Abstract: 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: Grant
    Filed: April 28, 2005
    Date of Patent: December 2, 2008
    Assignee: Schering Corporation
    Inventors: Zhaoning Zhu, Zhong-Yue Sun, Yuanzan C. Ye, Deborra E. Mullins, Brian McKittrick, Andrew Stamford, William J. Greenlee
  • Patent number: 7384938
    Abstract: 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: Grant
    Filed: January 17, 2003
    Date of Patent: June 10, 2008
    Assignee: Bayer Aktiengesellschaft
    Inventors: Kirkor Sirinyan, Hubert Dorn, Ulrich Heukamp
  • Patent number: 7375102
    Abstract: 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: Grant
    Filed: June 27, 2005
    Date of Patent: May 20, 2008
    Assignee: AMGEN SF, LLC
    Inventors: 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
  • Patent number: 7223754
    Abstract: 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: Grant
    Filed: November 17, 2004
    Date of Patent: May 29, 2007
    Assignee: Dynogen Pharmaceuticals, Inc.
    Inventors: Matthew Oliver Fraser, Karl Bruce Thor, Edward C. Burgard
  • Patent number: 7205309
    Abstract: 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: Grant
    Filed: July 3, 2003
    Date of Patent: April 17, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Patrizio Mattei, Werner Mueller, Werner Neidhart, Matthias Heinrich Nettekoven, Philippe Pflieger
  • Patent number: 7166609
    Abstract: 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: Grant
    Filed: November 3, 2003
    Date of Patent: January 23, 2007
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Otmar Klingler, Reinhard Kirsch, Joerg Habermann, Klaus-Ulrich Weithmann, Christian Engel, Bernard Pirard
  • Patent number: 7166590
    Abstract: 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: Grant
    Filed: May 28, 2002
    Date of Patent: January 23, 2007
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Takuya Seko, Masashi Kato
  • Patent number: 7148221
    Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, d
    Type: Grant
    Filed: August 1, 2005
    Date of Patent: December 12, 2006
    Assignee: 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
  • Patent number: 7087626
    Abstract: Novel pyrrazole derivative compounds and their use as pharmaceutical agents, in particular their use as TGF-beta signal transduction inhibitors.
    Type: Grant
    Filed: May 13, 2002
    Date of Patent: August 8, 2006
    Assignee: Eli Lilly and Company
    Inventors: 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
  • Patent number: 7084151
    Abstract: 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: Grant
    Filed: October 10, 2003
    Date of Patent: August 1, 2006
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Lin Zhi, Cornelis Arjan Van Oeveren
  • Patent number: 7022705
    Abstract: 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: Grant
    Filed: October 23, 2002
    Date of Patent: April 4, 2006
    Assignee: AstraZeneca AB
    Inventor: Michael John Betts
  • Patent number: 6936606
    Abstract: 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: Grant
    Filed: September 27, 2002
    Date of Patent: August 30, 2005
    Assignee: 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
  • Patent number: 6916806
    Abstract: 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: Grant
    Filed: February 14, 2002
    Date of Patent: July 12, 2005
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hiroyuki Kai, Takami Murashi, Minoru Tomida
  • Patent number: 6903119
    Abstract: 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: Grant
    Filed: July 13, 1999
    Date of Patent: June 7, 2005
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Takuya Seko, Masashi Kato
  • Publication number: 20040235751
    Abstract: 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: Application
    Filed: March 22, 2004
    Publication date: November 25, 2004
    Inventor: Christopher J. Frederickson
  • Patent number: 6767907
    Abstract: 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 c
    Type: Grant
    Filed: April 14, 2000
    Date of Patent: July 27, 2004
    Assignee: H. Lundbeck A/S
    Inventors: Jens Kristian Perregaard, John Willie Stenberg, Bitten Hansen
  • Patent number: RE39130
    Abstract: 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: Grant
    Filed: June 6, 1994
    Date of Patent: June 13, 2006
    Assignee: Bayer Cropscience K.K.
    Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hatori