Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Hetero Ring Patents (Class 549/425)
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Patent number: 10464934Abstract: Compounds are provided that are modulators of the CCR2 receptor. The compounds have the general formula (I): and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of CCR2 receptors.Type: GrantFiled: August 31, 2017Date of Patent: November 5, 2019Assignee: ChemoCentryx, Inc.Inventors: Junfa Fan, Jaroslaw Kalisiak, Rebecca M. Lui, Venkat Reddy Mali, Jeffrey P. McMahon, Jay P. Powers, Hiroko Tanaka, Yibin Zeng, Penglie Zhang
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Patent number: 9890103Abstract: A method of extracting (meth)acrylic acid from an aqueous reaction medium into an organic phase in contact therewith is described. The aqueous reaction medium is formed from at least one base catalyst and at least one dicarboxylic acid selected from maleic, fumaric, malic, itaconic, citraconic, mesaconic, and citramalic acid or mixtures thereof in aqueous solution and contains the base catalyzed decarboxylation products of the base catalyzed reaction. The method includes either the addition of at least one of the said dicarboxylic acids and/or a pre-cursor thereof to the aqueous reaction medium to enhance the solvent extraction of the (meth)acrylic acid into the organic solvent or maintaining the level of base catalyst to dicarboxylic acid and/or pre-cursor at a sub-stoichiometric level during the extraction process. The method extends to a process of producing (meth)acrylic acid, its esters and polymers and copolymers thereof.Type: GrantFiled: April 30, 2015Date of Patent: February 13, 2018Assignee: LUCITE INTERNATIONAL UK LIMITEDInventors: David William Johnson, Graham Ronald Eastham, Martyn Poliakoff, Thomas Andrew Huddle
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Patent number: 8981129Abstract: The compounds are intermediates in the preparation of therapeutic agents useful in the treatment of viral infections, particularly HIV infection. The compounds are 2-(2-hydroxy-2-phenylethyl)-3-[(phenylmethyl)oxy]-4H-pyran-4-one of the formula P-3 and/or 2-[(E)-2-phenylethenyl]-3-[(phenylmethyl)oxy]-4H-pyran-4-one of the formula P-4.Type: GrantFiled: May 20, 2014Date of Patent: March 17, 2015Assignees: Shionogi & Co., Ltd., ViiV Healthcare CompanyInventors: Brian Alvin Johns, Jason Gordon Weatherhead, Toshikazu Hakogi, Yasunori Aoyama
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Patent number: 8940912Abstract: The present invention features a process for the preparation of 4-oxo-3-[(phenylmethyl)oxy]-4-H-pyran-2-carboxylic acid, an intermediate useful in the synthesis of HIV integrase inhibitors. The process involves (a) treating a compound of formula P-2 with lithium bis(trimethylsilyl)amide and benzaldehyde to form a compound of formula P-3, (b) treating the compound of formula P-3 with triethylamine and methanesulfonyl chloride followed by N-methyl-2-pyrrolidone and 1,8-diazabicyclo[5.4.0]undec-7-ene to form a compound of formula P-4, and (c) treating the compound of formula P-4 with RuCl3 and NaIO4 to form the compound of formula P-5.Type: GrantFiled: October 2, 2013Date of Patent: January 27, 2015Assignees: ViiV Healthcare Company, Shionogi & Co., Ltd.Inventors: Brian Alvin Johns, Jason Gordon Weatherhead, Toshikazu Hakogi, Yasunori Aoyama
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Publication number: 20140275008Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventors: Qing Xu, Zhe Li
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Publication number: 20130338116Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.Type: ApplicationFiled: August 16, 2013Publication date: December 19, 2013Inventor: Irving Sucholeiki
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Publication number: 20130296414Abstract: Metabolites of [2-(3-methoxyphenyl)-cyclohexylmethyl]dimethylamine as free bases and/or in the form of physiologically acceptable salts, corresponding medicaments, the use of [2-(3-methoxyphenyl)-cyclohexylmethyl]-dimethylamine and the metabolites thereof for producing a medicament used for treating depression, and related methods of treating depression, pain and urinary incontinence.Type: ApplicationFiled: July 3, 2013Publication date: November 7, 2013Inventors: Elmar FRIDERICHS, Wolfgang STRASSBURGER, Ulrich JAHNEL, Helmut BUSCHMANN, Joerg HOLENZ, Oswald ZIMMER, Derek SAUNDERS, Werner ENGLBERGER, Hagen-Heinrich HENNIES
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Publication number: 20130165486Abstract: Tetrasubstituted benzenes that act as modulators of gamma secretase and their use in the treatment of one or more symptoms of treating neurodegenerative disorders, e.g., Alzheimer's disease, are described.Type: ApplicationFiled: February 1, 2013Publication date: June 27, 2013Applicant: ENVIVO PHARMACEUTICALS, INC.Inventor: ENVIVO PHARMACEUTICALS, INC.
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Publication number: 20130012701Abstract: A compound useful as a building block for the manufacture of various compounds is represented by Formula A or D. In Formula A and D, z is 0 or 1; Q is a heteroatom; R1 through R11 and Ra through Rf are each independently hydrogen, a substituted or unsubstituted hydrocarbyl group, a substituted or unsubstituted heteroatom containing hydrocarbyl group, or a functional group; d, e and f are each independently 0 or greater; each of A, B and D is independently a carbon atom or a heteroatom; and two or more of R1 though R11, Ra through Rf and Y optionally combine to form a ring. In some embodiments, R8 and R9 combine to form a carbonyl group. In some embodiments, R2 and Y combine to form a ring with the Q atom. In some embodiments, the ring includes at least one double bond.Type: ApplicationFiled: June 22, 2012Publication date: January 10, 2013Applicant: California Institute of TechnologyInventors: Brian M. Stoltz, Scott C. Virgil, David E. White, Taiga Yurino, Yiyang Liu, Douglas C. Behenna, Douglas Duquette, Christian Eidamshaus
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Patent number: 8283383Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 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: GrantFiled: June 22, 2010Date of Patent: October 9, 2012Assignee: Roche Palo Alto LLCInventors: Chris Allen Broka, Ronald Charles Hawley
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Patent number: 8242289Abstract: The present invention relates to alkyl-substituted tetrahydropyrans, mixtures containing these alkyl-substituted tetrahydropyrans, their respective use and corresponding flavored products.Type: GrantFiled: January 29, 2010Date of Patent: August 14, 2012Assignee: SYMRISE AGInventors: Heiko Oertling, Constanze Brocke, Hubert Loges, Arnold Machinek
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Publication number: 20120190865Abstract: The present invention relates to a novel process for the preparation of 1-H-pyrrolidine-2,4-dione derivatives and to novel intermediates and to a process for their preparation.Type: ApplicationFiled: January 25, 2012Publication date: July 26, 2012Applicant: Bayer CropScience AGInventors: Reiner FISCHER, Thomas HIMMLER
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Patent number: 8193239Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: May 6, 2010Date of Patent: June 5, 2012Assignee: AstraZeneca ABInventors: Rhonan Ford, Andrew Mather, Antonio Mete, Ian Millichip
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Publication number: 20120101039Abstract: A compound of general formula I their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, methods of treating diseases with said compounds, and the use of said compounds in the manufacture of medicaments.Type: ApplicationFiled: May 26, 2010Publication date: April 26, 2012Applicant: LEO PHARMA A/SInventors: Jef Fenscholdt, Thomas Høyer, Xifu Liang, Sophie Elisabeth Havez
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Publication number: 20120053208Abstract: Curcumin analogues and methods of making and using the same are disclosed.Type: ApplicationFiled: April 15, 2010Publication date: March 1, 2012Applicant: THE OHIO STATE UNIVERSITY RESEARCH FOUNDATIONInventors: Pui-Kai Li, Chenglong Li, Jiayuh Lin, James R. Fuchs
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Patent number: 8115019Abstract: Disclosed are cis-2,6-disubstituted tetrahydropyran derivatives represented by Chemical Formula 1 and a preparation method thereof. The tetrahydropyran derivatives can be prepared by Prins-reacting tetrahydropyran derivatives with homopargylicalcohol derivatives in the presence of trimethylsilyltriflate. The tetrahydropyran derivatives with cis-substituents at both C2 and C6 positions of the tetrahydropyran ring are useful as intermediates for use in the synthesis and development of therapeutically effective, naturally occurring compounds. (wherein, R1, R2 and R3 are as defined in the specification.).Type: GrantFiled: October 1, 2008Date of Patent: February 14, 2012Assignee: Korea Institute of Science and TechnologyInventors: Yong Seo Cho, You Seung Kim, Jae Kyun Lee, Hyunah Choo, Ae Nim Pae
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Publication number: 20120015807Abstract: The present invention relates to novel trifluoromethoxyphenyl-substituted tetramic acid derivatives of the formula (I), in which J, X, Y, A, B, D and G have the meanings given above, to a number of processes for their preparation, and to their use as pesticides and/or herbicides. The invention further provides selective herbicidal compositions which comprise, firstly, trifluoromethoxyphenyl-substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetrants.Type: ApplicationFiled: October 13, 2007Publication date: January 19, 2012Applicant: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Christian Arnold, Thomas Auler, Jan Dittgen, Dieter Feucht, Eva-Maria Franken, Waltraud Hempel, Martin Jeffrey Hills, Heinz Kehne, Peter Losel, Olga Malsam, Christopher Hugh Rosinger, Erich Sanwald, Ulrich Gorgens, Stefan Antons, Wolfgang Ebenbeck, Axel Pleschke, Marielouise Schneider, Ralf Wischnat
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Publication number: 20110306542Abstract: Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.Type: ApplicationFiled: June 9, 2011Publication date: December 15, 2011Applicant: Receptos, Inc.Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Liming Huang, Junko Tamiya, Mark T. Griffith, Thomas Fowler, Andrew Novak, Michael Knaggs, Premji Meghani
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Patent number: 8076494Abstract: Disclosed is a process for the manufacture of a compound of formula (I) wherein Hal represents fluoro or chloro, and R1 and R2 represent, independently from one another, hydrogen or Hal; in which process a compound of formula (II) is converted to a corresponding alkyl, fluoroalkyl or aryl sulfonic acid ester, which is then reacted with an alkali metal nitrite in the presence of a suitable crown ether in a polar non-nucleophilic solvent at a temperature of ?10 to 50° C. to give the compound of formula (I).Type: GrantFiled: August 31, 2010Date of Patent: December 13, 2011Assignee: Basilea Pharmaceutica AGInventors: Marc Muller, Lin Xu
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Patent number: 8071625Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: GrantFiled: August 1, 2007Date of Patent: December 6, 2011Assignee: Cytokinetics, Inc.Inventors: Xiangping Qian, Pu-Ping Lu, Chihyuan (Grace) Chuang, Bradley P. Morgan, David J. Morgans, Jr.
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Patent number: 8067638Abstract: The present invention is to provide a compound represented by the general formula (1) exhibiting a high insecticidal effect and an insecticide comprising the compound as an active ingredient. The compound represented by the general formula (1) and an insecticide comprising the compound as an active ingredient, wherein, in the formula, A1, A2, A3 and A4 each represent a carbon atom or the like; R1 and R2 each represent a hydrogen atom or the like; G1 and G2 represent an oxygen atom or the like; Xs each represent a hydrogen atom, a halogen atom or the like; n represents an integer of 0 to 4; Q1 represents a substituted phenyl group, a substituted heterocyclic group or the like; Q2 represents a substituted phenyl group, a substituted heterocyclic group or the like.Type: GrantFiled: June 20, 2006Date of Patent: November 29, 2011Assignee: Mitsui Chemicals, Inc.Inventors: Akiyoshi Kai, Takeo Wakita, Hiroyuki Katsuta, Kei Yoshida, Hidetaka Tsukada, Yusuke Takahashi, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido
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Publication number: 20110263428Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: July 1, 2009Publication date: October 27, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Stephane Andre Marie Jeanmart, Russell Colin Viner, John Benjamin Taylor, William Guy Whittingham, Jeffrey Steven Wailes, Sarah Margaret Targett, Christopher John Mathews, Mangala Govenkar, Matthew Robert Cordingley, Claire Janet Russell, Melloney Tyte
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Publication number: 20110237592Abstract: The present invention relates to substituted amido phenoxybenzamide compounds of general formula (I): in which A, R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the claims, to pharmaceutical compositions and combinations containing said compounds, to methods of preparing said compounds, and to the use of said compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: October 29, 2009Publication date: September 29, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Ingo Hartung, Marion Hitchcock, Knut Eis, Florian Puhler
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Publication number: 20110230452Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.Type: ApplicationFiled: September 23, 2010Publication date: September 22, 2011Inventor: Irving Sucholeiki
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Patent number: 8008514Abstract: Process for preparing 2-methoxycarbonylmethyl-6,6-dimethyl-2-tetrahydropyran carboxylic acid (I) comprising: a) Reaction of 5-bromo-2-methyl-2-pentene (III) with magnesium and then diethyloxalate to obtain ethyl-2-oxo-6-methyl-5-heptenoate (IV); b) Reaction of ethyl-2-oxo-6-methyl-5-heptenoate (IV) with an alkali amide and methyl acetate to obtain ethyl-2-methoxycarbonylmethyl-2-hydroxy-6-methyl-5-heptenoate (V); c) Reaction of ethyl-2-methoxycarbonylmethyl-2-hydroxy-6-methyl-5-heptenoate (V) with an alkali metal hydroxide to obtain the corresponding 2-carboxymethyl-2-hydroxy-6-methyl-5-heptenoic acid (VI); d) Cyclisation of 2-carboxymethyl-2-hydroxy-6-methyl-5-heptenoic acid (VI) with formic acid to give 2-carboxymethyl-6,6-dimethyl-2-tetrahydropyrancarboxylic acid (VII); e) Monoesterification of 2-carboxymethyl-6,6-dimethyl-2-tetrahydropyrancarboxylic acid (VII) to 2-methoxycarbonylmethyl-6,6-dimethyl-2-tetrahydropyran carboxylic acid (I), characterised in that in stage (e) the 2-methoxycarbonylmethyl-6,6Type: GrantFiled: July 14, 2006Date of Patent: August 30, 2011Assignees: Erregierre S.p.A., Stragen Pharma SAInventors: Massimo Ferrari, Paolo Belotti
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Patent number: 7994093Abstract: The invention relates to a fungicidally active compound of formula (I): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, provided that the ring is not 1,2,3-triazole, the ring being substituted by groups R8, R9 and R10; X is a single or double bond; Y is O, S, N(R11) or (CR12R13)(CR14R15)m(CR16R17)n; m is 0 or 1; n is 0 or 1; and R1 to R17 each, independently, have a range of values; to the preparation of these compounds, to novel intermediates used in the preparation of these compounds, to agrochemical compositions which comprise at least one of the novel compounds as active ingredient, to the preparation of the compositions mentioned and to the use of the active ingredients or compositions in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.Type: GrantFiled: August 28, 2009Date of Patent: August 9, 2011Assignee: Syngenta Crop Protection, Inc.Inventors: Josef Ehrenfreund, Hans Tobler, Harald Walter
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Patent number: 7977344Abstract: The present invention includes novel compounds useful in the treatment of various disorders in particular infectious diseases, cancer, and allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, and as vaccine adjuvants.Type: GrantFiled: February 15, 2008Date of Patent: July 12, 2011Assignee: GlaxoSmithKline LLCInventors: Linos Lazarides, Stephen Allan Smith, Richard Stocker, Colin Jack Theobald
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Publication number: 20110046212Abstract: This invention relates to the use of oleuropein, specifically oleuropein in non-glycated form, and its derivatives in the treatment of type 2 diabetes mellitus. Furthermore, this invention relates to the use of oleuropein, specifically oleuropein in non-glycated form, and its derivatives both from synthesis and from degradation, in the treatment of pathologies associated with protein aggregation phenomena. Specifically, this invention relates to the use of oleuropein to prepare a pharmaceutical formula for the prophylactic and therapeutic treatment of pathologies connected to or deriving from amyloid deposit.Type: ApplicationFiled: March 26, 2009Publication date: February 24, 2011Inventors: Andrea Berti, Massimo Stefani, Stefania Rigacci
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Patent number: 7772269Abstract: The invention relates to the compounds of formula (I): or a pharmaceutically acceptable salt and solvate thereof, wherein R1 is F or H and to processes for the preparation of, intermediates used in the preparation of, compositions containing the uses of, such compounds. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: November 26, 2007Date of Patent: August 10, 2010Assignee: Pfizer Inc.Inventors: Mathew J. Graneto, Todd M. Maddux, Jaime L. Masferrer
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Publication number: 20100184999Abstract: Methods of performing cycloadditions are described that include (a) combining a first reactant and a second reactant in a hydrogen bonding solvent to form a reaction mixture; and (b) reacting the first reactant and the second reactant to form a cycloadduct. Methods of performing asymmetric catalytic reactions are also described that include (a) combining a first reactant, a second reactant, and a catalytic amount of a chiral hydrogen-bond donor in a solvent to form a reaction mixture; and (b) reacting the first reactant and the second reactant to form an enantiomeric excess of a reaction product. Reaction mixtures corresponding to these methods are also described.Type: ApplicationFiled: June 11, 2007Publication date: July 22, 2010Inventors: Viresh H. Rawal, Yong Huang, Aditya K. Unni, Avinash N. Thadani
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Patent number: 7741497Abstract: The present invention is to provide a process for preparing an alkyl 3-(4-tetrahydropyranyl)-3-oxopropanoate compound represented by the formula (1): wherein R1 and R2 may be the same or different from each other, and represent a group which does not participate in the reaction, and R1 and R2 may be bonded to form a ring, and the ring may contain a hetero atom(s), and R3 represents a hydrocarbon group, which comprises reacting 4-acyltetrahydropyran represented by the formula (2): wherein R1 and R2 have the same meanings as defined above, and a carbonic acid diester represented by the formula (3): wherein R3 has the same meanings as defined above, and two R3s may be bonded to each other to form a ring, in the presence of a base, and a process for preparing 4-acyltetrahydropyran.Type: GrantFiled: December 17, 2004Date of Patent: June 22, 2010Assignee: Ube Industries, Ltd.Inventors: Shigeyoshi Nishino, Kenji Hirotsu, Hidetaka Shima, Keiji Iwamoto, Takashi Harada
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Publication number: 20100076068Abstract: A compound of formula (1) Including pharmaceutically acceptable salts thereof, wherein: R1 is aryl or heteroaryl optionally substituted with R8; R2 is H or alkyl or CH2 (when forming part of a ring with R3, R4 or R5); R3 is H, alkyl, CH2OH or CH2OR6 and can be part of a ring with R2; R4 is H, alkyl, CH2OH or CH2OR6 and can be part of a ring with R2; R5 is H, alkyl, CH2OH or CH2OR6 and can be part of a ring with R2; R6 is H, alkyl, COH, COOR9, CON(R9)2, COR9, COR10, COR11, P(O)nR9, P(O)nR10S(O)nR10 or S(O)nR9 and can be part of a ring with R2, R3, R4 or R5; R7 is H, alkyl, COOR9, COOR11, COR9 or CON(R9)2, and can be part of a ring with R2, R3, R4, R5 or R6; R8 is alkyl, CF3, OR9, OCOR9, CONH2, CN, F, Cl, Br, I, N(R9)2, NO2, NHCHO, NHCONH2, NHSO2R9, CON(R9)2, S(O)nR9, CH2OH Or OCON(R9)2; R9 is H, alkyl or cycloalkyl; R10 is aryl or heteroaryl (optionally substituted with R8) or a four to seven membered ring (which is optionally substituted with R8 and can contain one or more additional heteroatoms selected fromType: ApplicationFiled: December 12, 2007Publication date: March 25, 2010Inventors: Andrea Walmsley, Elena Lasterra
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Patent number: 7638641Abstract: The invention relates to tetrahydropyran derivatives of the general formula I and to processes for the preparation thereof.Type: GrantFiled: November 17, 2003Date of Patent: December 29, 2009Assignee: Merck Patent GmbHInventors: Peer Kirsch, Alexander Hahn, Eike Poetsch, Werner Binder, Volker Meyer
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Publication number: 20090043093Abstract: Process for preparing 2-methoxycarbonylmethyl-6,6-dimethyl-2-tetrahydropyran carboxylic acid (I) comprising: a) Reaction of 5-bromo-2-methyl-2-pentene (III) with magnesium and then diethyloxalate to obtain ethyl-2-oxo-6-methyl-5-heptenoate (IV); b) Reaction of ethyl-2-oxo-6-methyl-5-heptenoate (IV) with an alkali amide and methyl acetate to obtain ethyl-2-methoxycarbonylmethyl-2-hydroxy-6-methyl-5-heptenoate (V); c) Reaction of ethyl-2-methoxycarbonylmethyl-2-hydroxy-6-methyl-5-heptenoate (V) with an alkali metal hydroxide to obtain the corresponding 2-carboxymethyl-2-hydroxy-6-methyl-5-heptenoic acid (VI); d) Cyclisation of 2-carboxymethyl-2-hydroxy-6-methyl-5-heptenoic acid (VI) with formic acid to give 2-carboxymethyl-6,6-dimethyl-2-tetrahydropyrancarboxylic acid (VII); e) Monoesterification of 2-carboxymethyl-6,6-dimethyl-2-tetrahydropyrancarboxylic acid (VII) to 2-methoxycarbonylmethyl-6,6-dimethyl-2-tetrahydropyran carboxylic acid (I), characterised in that in stage (e) the 2-methoxycarbonylmethyl-6,6Type: ApplicationFiled: July 14, 2006Publication date: February 12, 2009Inventors: Massimo Ferrari, Paolo Belotti
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Patent number: 7485752Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: May 5, 2006Date of Patent: February 3, 2009Assignee: Hoffman-La Roche Inc.Inventor: Christophe Michoud
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Patent number: 7476686Abstract: 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: GrantFiled: December 17, 2004Date of Patent: January 13, 2009Assignee: Achillion Pharmaceuticals, Inc.Inventors: Dawei Chen, Milind Deshpande, Andrew Thurkauf, Avinash Phadke, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
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Publication number: 20080306287Abstract: The present invention is to provide a process for preparing tetrahydropyran-4-carboxylic acid represented by the formula (1): which comprises hydrolyzing a 4-cyanotetrahydropyran-4-carboxylic acid compound represented by the formula (2): wherein R represents a hydrogen atom or a hydrocarbon group, in the presence of an acid; a process for preparing a tetrahydropyran-4-carboxylic acid ester which comprises reacting the tetrahydropyran-4-carboxylic acid represented by the above-mentioned formula (1) with an alcohol in the presence of an acid; and a process for preparing tetrahydropyran-4-carboxylic acid amide which comprises reacting the tetrahydropyran-4-carboxylic acid represented by the above-mentioned formula (1) with a halogenating agent to prepare tetrahydropyran-4-carboxylic acid halide, and then, reacting an amine compound to the resulting compound.Type: ApplicationFiled: November 18, 2005Publication date: December 11, 2008Applicant: UBE INDUSTRIES, LTD.Inventors: Shigeyoshi Nishino, Kenji Hirotsu, Hidetaka Shima, Takashi Harada, Taku Nakamura, Keiji Iwamoto
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Patent number: 7442793Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: December 11, 2003Date of Patent: October 28, 2008Assignee: SmithKline Beecham CorporationInventors: Jinhwa Lee, Siegfried B. Christensen, IV
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Publication number: 20080226716Abstract: Compounds that provide for sustained systemic concentrations of GABA analogs following oral administration to animals are disclosed. Pharmaceutical compositions including, and methods using, such compounds are also disclosed.Type: ApplicationFiled: May 28, 2008Publication date: September 18, 2008Applicant: XenoPortInventors: Mark Gallop, Kenneth C. Cundy, Randall A. Scheuerman, Ronald W. Barrett, Noa Zerangue
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Patent number: 7402687Abstract: Compounds of formula I are described herein which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. or pharmaceutically acceptable salts thereof, wherein each of R1, R2, R3, R4, Rx, Ry, and n are as defined herein. Such compounds, and compositions thereof, are useful for treating a variety of central nervous system disorders such as schizophrenia.Type: GrantFiled: April 21, 2006Date of Patent: July 22, 2008Assignee: WyethInventors: Gary Paul Stack, Jianyao Wang, William Demaio, Ronald Jordan, John Chuck Lem Erve, Rasmy Elsayed Talaat, Matthew John Hoffmann
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Patent number: 7390803Abstract: The present invention is directed to compounds of the formula (I) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R27, R28, R29, R30, R31, X, m, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity.Type: GrantFiled: October 24, 2003Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Gabor Butora, Sander G. Mills, Alexander Pasternak, Kothandaraman Shankaran, Lihu Yang, Changyou Zhou, Stephen D. Goble
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Publication number: 20080125474Abstract: The invention relates to the compounds of formula (I): or a pharmaceutically acceptable salt and solvate thereof, wherein R1 is F or H and to processes for the preparation of, intermediates used in the preparation of, compositions containing the uses of, such compounds.Type: ApplicationFiled: November 26, 2007Publication date: May 29, 2008Inventors: Mathew J. Graneto, Todd M. Maddux, Jaime L. Masferrer
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Patent number: 7317125Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: January 31, 2006Date of Patent: January 8, 2008Assignee: Hoffman-La Roche Inc.Inventors: David Robert Bolin, Christophe Michoud
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Patent number: 7230028Abstract: The invention relates to compounds of general formula (I); in which R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; and n is an integer from 10 to 18 or a pharmaceutically acceptable derivative thereof, methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infectionType: GrantFiled: November 8, 2002Date of Patent: June 12, 2007Assignee: Biota Scientific Management Pty Ltd.Inventors: Derek A. Demaine, Graham G. A. Inglis, Simon J. F. MacDonald, Stephen E. Shanahan, Simon P. Tucker, Keith G. Watson, Wen-Yang Wu
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Patent number: 7223790Abstract: The invention relates to compounds of general formula (I); in which R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; X is CONH, NHCO or O; n is an integer from 2 to 6; and Y is C2–C8 alkyl C3-8 cycloalkyl, C1–C4 alkoxyalkyl, an amino acid or dipeptide, or a pharmaceutically acceptable derivative thereof, methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infectionType: GrantFiled: November 8, 2002Date of Patent: May 29, 2007Assignee: Biota Scientific Management Pty Ltd.Inventors: Betty Jin, Simon J. F. MacDonald, Darryl McConnell, Van T. T. Nguyen, Stephen E. Shanahan, Wen-Yang Wu
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Patent number: 7214707Abstract: The invention relates to compounds of general formula (I), in which: R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; n and q are either the same or different and selected from 0, 1 or 2; and X is an optionally substituted phenyl, optionally substituted naphthyl or optionally substituted phenyl-Y-optionally substituted phenyl in which Y is selected from a covalent bond, CH2, CH2CH2, O or SO2, or a pharmaceutically acceptable derivative thereof, with the proviso that when X is phenyl or naphthyl, n and q are both 2 and when X is phenyl-Y-phenyl in which Y is a covalent bond, then n and q are not both 0, methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infectionType: GrantFiled: November 8, 2002Date of Patent: May 8, 2007Assignee: Biota Scientific Management Pty Ltd.Inventors: Derek A. Demaine, Haydn T. Jones, Simon J. F. MacDonald, Andrew McM Mason, Stephen E. Shanahan
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Patent number: 7157494Abstract: The invention relates to compounds of general formula (I); in which R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; X is CONH, SO2NH, NHCO or NHCONH; m is either 0 or 1; n is an integer from 2 to 6; q is an integer from 0 to 3; and Y is hydrogen or an aromatic substituent, or a pharmaceutically acceptable derivative thereof; methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infectionType: GrantFiled: November 8, 2002Date of Patent: January 2, 2007Assignee: Biota Scientific Management Pty. Ltd.Inventors: Michael D. Dowle, Betty Jin, Simon J. F. Macdonald, Andrew McM Mason, Darryl McConnell, Van T. T. Nguyen, Stephen E. Shanahan, Wen-Yang Wu
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Patent number: 7053109Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: GrantFiled: July 10, 2002Date of Patent: May 30, 2006Assignee: Pharmacia & Upjohn CompanyInventors: Heinrich Josef Schostarez, Robert Alan Chrusciel
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Patent number: 6884897Abstract: A process is provided for preparing 3,6-dihydro-2H-pyran-2-carboxylic esters via a thermal hetero Diels-Alder reaction of 1,3-dienes with glyoxylic esters without the use of catalysts and stabilizers using a special metering technique.Type: GrantFiled: February 19, 2003Date of Patent: April 26, 2005Assignee: Bayer AktiengesellschaftInventor: Michael Lögers
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Patent number: 6849660Abstract: Provided are antibacterial compounds having Formula I: In such compositions, X is O or S; Y is CH2; n is 0 or 1. One of R1 and R1? is —C(O)NR5R5?, —C(O)—Q—NR5R5?, —CH2NR5R5? or —S(O)2NR5R5? and the other is H or R3. One of R2 and R2? is —NHC(O)R6 or —NHS(O)2R6 and the other is H or R4. Q is an amino acid or peptide. R3 is H, halogen, —NR5R5? or —NHC(O)R6; and R4 is selected from the group consisting of H, halogen, hydroxyl, amino, carboxyl, alkyl, alkenyl and alkynyl. R5 is selected from the group consisting of H, alkyl, alkenyl or alkynyl optionally substituted with halogen, OH, amino, amidinyl, guanidinyl, urea, alkyl, carboxyl, oxo, carboxamide; R5? is H or R5 and R5? together form a 5-16 member heterocycle optionally substituted with halogen, OH, amino, alkyl, carboxyl, carbonyl or carboxamide.Type: GrantFiled: August 1, 2000Date of Patent: February 1, 2005Assignee: ISIS Pharmaceuticals, Inc.Inventors: Elizabeth Jefferson, Eric Swayze