Patents Examined by Cecilia Jaisle
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Patent number: 7361759Abstract: To provide a method for producing L-biopterin on a large industrial scale by using a reagent which is inexpensive and easy to handle, without requiring a use of any particular equipment or plants. A method for porducing a biopterin derivative represented by the formula (6): wherein R1 and R2, which are the same or different from each other, each represents a hydrogen atom, an alkyl group, or an aryl group, comprising: reacting a compound belonging to triacetoxy-5-deoxy-L-arabinose phenylhydrazones represented by the formula (4): wherein R1 and R2 are the same as defined above, with 6-hydroxy-2,4,5-triaminopyrimidine (5) under catalytic influence of a Lewis acid in an aqueous solvent.Type: GrantFiled: February 28, 2005Date of Patent: April 22, 2008Assignees: Shiratori Pharmaceutical Co., Ltd, Asubio Pharma Co., Ltd.Inventor: Shinnosuke Tazawa
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Patent number: 7338954Abstract: A method is provided for treating disorders of gastrointestinal motility which include the steps of administering to a patient in need of treatment of a compound having the structure or a pharmaceutically acceptable salt thereof, a prodrug ester thereof, and all stereoisomers thereof, wherein R1 is selected from alkyl, aryl, cycloalkyl, alkenyl, alkynyl, arylalkyl, heteroaryl, heteroarylalkyl or heterocycloalkyl; Z is selected from —CON(R4)R4a, —SO2N(R4)R4a, —CN, and R4 and R4a are the same or different and are independently selected from hydrogen, alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl or R4 and R4a can be joined together to form a heterocycle; R4b is selected from hydrogen, halogen, hydroxyl, CN, OCF3, CF3, CONH2, SONH2, SO2CH3, NHCOCH3 or NHCO2CH3; and Q is a substituted bicyclic heterocycle. New compounds for use in treating disorders of gastrointestinal motility are also provided.Type: GrantFiled: September 14, 2004Date of Patent: March 4, 2008Assignee: Bristol-Myers Squibb CompanyInventors: James J. Li, Hannguang J. Chao, Joseph A. Tino, William R. Ewing
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Patent number: 7288542Abstract: The present invention relates to a compounds according to formula I, methods for treating diseases mediated by human immunodeficieny virus by administration of a compound according to formula I and pharmaceutical compositions for treating diseases mediated by human immunodeficieny virus containing a compound according to formula I where R1, R2, R3, R4, R5, R6, R7 and R8 are as defined hereinType: GrantFiled: March 22, 2005Date of Patent: October 30, 2007Assignee: Roche Palo Alto LLCInventors: James Patrick Dunn, Todd Richard Elworthy, Joan Heather Hogg, Dimitrios Stefanidis
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Patent number: 7241889Abstract: Disclosed are 6-formyl-tetrahydropteridines of the formula (I) wherein the groups R1 to R6 have the meanings given in the claims and specification, the isomers thereof, methods of preparing these 6-formyl-tetrahydropteridines and their use as medicaments.Type: GrantFiled: July 12, 2005Date of Patent: July 10, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Hoffmann, Matthias Grauert, Martin Steegmaier, Flavio Solca
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Patent number: 7238808Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, M, L, E, G, and J are as defined in the description and claims. The invention also relates to a process for the manufacture of such compounds, pharmaceutical compositions containing them, and methods for treating CNS disorders.Type: GrantFiled: March 15, 2006Date of Patent: July 3, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Silvia Gatti McArthur, Erwin Goetschi, Wylie Solang Palmer, Juergen Wichmann, Thomas Johannes Woltering
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Patent number: 7235660Abstract: A process for the preparation of aminopterin with a purity greater than 90%, which comprises reacting folic acid, with a silazane in an organic solvent at a temperature from 60 to 180° C., the said solvent being a tertiary amine organic solvent, or, if a catalyst which is acid in nature is present, a basic organic solvent or acetonitrile, and further adding water such that there is about 2.8 to 7.0 mole water for each mole of folic acid.Type: GrantFiled: January 2, 2007Date of Patent: June 26, 2007Inventor: John A. Zebala
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Patent number: 7232827Abstract: The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: (I) X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an ethynylene group or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring optionally substituted; R2 represents a heterocyclic bicyclic rings, having 1–4 heteroatoms selected from an oxygen atom, a sulfur atom and a nitrogen atom and having 5–9 carbon atoms, of formula (II) R3 represents a hydrogen atom, a C1-6 alkyl group, a hydroxy group, a C1-4 alkoxy group or a halogen atom; R4 represents a hydrogen atom, a C1-6 alkyl group, a C1-4 alkoxy group or a halogen atom.Type: GrantFiled: February 26, 2003Date of Patent: June 19, 2007Assignees: Sanofi-Aventis, Mitsubishi Pharma CorporationInventors: Alistair Lochead, Alain Nedelec, Mourad Saady, Philippe Yaiche
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Patent number: 7230101Abstract: The present invention relates to novel compositions of methotrexate-containing heterodimeric probe molecules, also known as chemical inducers of dimerization (CID), useful in three-hybrid assays. The invention further relates to synthesis of said compositions and their intermediates. Another aspect of the invention is a method for using the heterodimeric probe molecules described herein in drug screens to identify potential protein targets to a given ligand, optimize protein-ligand interactions, or identify potential ligands for a given protein target.Type: GrantFiled: August 28, 2003Date of Patent: June 12, 2007Assignee: GPC Biotech, Inc.Inventors: Krishna K. Murthi, Chase C. Smith
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Patent number: 7214682Abstract: The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an ethynylene group an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group, a carbonyl group, a hydroxyiminomethylene group, a dioxolan group, a nitrogen atom being optionally substituted; or a methylene group optionally substituted; or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring optionally substituted; R2 may represent a C1-6 alkyl group optionally; a C3-6 cycloalkyl group, a C1-4 alkythio group, a C1-4 alkoxy group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a phenylthio group, a benzyl group, a benzene ring, an indan ring, a 5,6,7,8-tetrahydronaphthalene ring, a naphthalene ring, a pyridine ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring; R3 and R4 represent, eacType: GrantFiled: September 19, 2002Date of Patent: May 8, 2007Assignees: Sanofi-aventis, Mitsubishi Pharma CorporationInventors: Thierry Gallet, Patrick Lardenois, Alistair Lochead, Séverine Marguerie, Alain Nedelec, Mourad Saady, Franck Slowinski, Philippe Yaiche
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Patent number: 7205405Abstract: The process consists in condensing (2-methyl-6,7,8,9-tetrahydro-4 H-pyrido-[1,2-a]pyrimidin-3-yl)-acetaldehyd with 6-fluoro-3-piperidinyl)-1,2-benzisoxazole to yield the intermediate enamine, 3-{2-[4-(6-fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]vinyl}-2-methyl-6,7,8,9-tetrahydro-pyrido[1,2,-a]pyrimidin-4 -one followed by reduction of such an enamine.Type: GrantFiled: March 3, 2003Date of Patent: April 17, 2007Assignee: Ferrer Internacional, S.A.Inventors: Rafael Foguet, Jorge Ramentol, Diego Fernandez-Cano, Miguel P. Armengol, Francesc X. Camps, Juan Sallares, Inés Petschen, Mireia Pasto, Esther Gordo
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Patent number: 7202360Abstract: Risperidone is prepared in a high yield by reacting 2,4-difluorophenyl(4-piperidinyl)methanone oxime hydrochloride and 3-(2-chloroethyl)-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one in an aqueous alkali hydroxide solution having an alkali hydroxide concentration in the range of 20 to 40%.Type: GrantFiled: October 17, 2003Date of Patent: April 10, 2007Assignee: Hanmi Pharm Co., Ltd.Inventors: Nam-Du Kim, Jae-Heon Lee, Moon-Sub Lee, Young-Kil Chang, Gwan-Sun Lee
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Patent number: 7193082Abstract: New process for the production of (6S)-5,6,7,8-tetrahydrofolic acid or derivatives thereof starting from the corresponding (6S, 6R) racemic mixture. The procedure comprises in the steps of adding an organic acid to a non-alkaline suspension of (6S,6R)-5,6,7,8-tetraydrofolic acid, up to a pH value in the range of 1 to 3; heating the suspension from 30° to 80° C.; cooling the suspension from 20° to 60° C., with selective crystallization of the (6S)-isomer. The procedure gives the (6S)-isomer in high yields and with a high degree of stereoselectivity. It follows that the synthetic access to a large number of pharmacologically active stereoisomers of folic acid is simpler and more-effective.Type: GrantFiled: January 21, 2003Date of Patent: March 20, 2007Assignee: GMT Fine Chemicals SAInventor: Pascal Jequier
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Patent number: 7189731Abstract: Compounds having the formula (I) or (II), are useful as p38 kinase inhibitors, wherein R is an optionally substituted alkyl, cycloalkyl, or aryl; R6 is hydrogen or lower alkyl; R7 is hydrogen or a non-interfering substituent, and Q is a non-aromatic moiety as defined in the specification.Type: GrantFiled: April 15, 2004Date of Patent: March 13, 2007Assignee: Roche Palo Alto LLCInventors: Nolan James Dewdney, David Michael Goldstein
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Patent number: 7189732Abstract: The invention describes compounds of the general formula I a process for their manufacture, compositions containing them and their manufacture as well as the use of these compounds as pharmaceutically active agents. These compounds show activity as protein kinase inhibitors, in particular src family tyrosine kinase inhibitors, and may therefore be useful for the treatment of diseases mediated by said tyrosine kinases.Type: GrantFiled: March 14, 2005Date of Patent: March 13, 2007Assignee: Hoffman-La Roche Inc.Inventors: Konrad Honold, Wolfgang Schaefer, Stefan Scheiblich
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Patent number: 7169778Abstract: Disclosed are compounds of Formulae (Ia), (Ib), (Ic), (Id) wherein: W is NH, S, SO, or SO2; R2 is (un)substituted aryl, (un)substituted heteroaryl, or (un)substituted carbocycle or heterocycle; Q is hydrogen or lower alkyl; R4 and R6 are the same or different and represent hydrogen, halogen, lower alkyl, lower alkoxy, (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl; and R8 is hydrogen, lower alkyl or an (un)substituted carbocyclic group containing from 3–7 members, up to two of which members are optionally hetero atoms selected from oxygen and nitrogen; or R8 is (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl. These compounds are useful for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases.Type: GrantFiled: June 21, 2000Date of Patent: January 30, 2007Assignee: Warner-Lambert CompanyInventors: William Alexander Denny, Gordon William Rewcastle, Ellen Dobrusin, James Bernard Kramer, Dennis Joseph McNamara, Howard Daniel Hollis Showalter, Peter Laurence Toogood
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Patent number: 4021560Abstract: 2-[(Dimethylamino)(3-pyridyl)methyl]-cyclohexanol and related compounds, methods for their preparation and use are disclosed. The final products have analgesic activity.Type: GrantFiled: August 11, 1975Date of Patent: May 3, 1977Assignee: American Home Products CorporationInventor: John P. Yardley
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Patent number: 4013771Abstract: This invention relates to substituted 2-aminothiochromones of the general structure I: ##STR1## wherein R.sub.1 and R.sub.2 may be hydrogen; lower alkyl or lower alkoxy of 1 to 6 carbon atoms; or halogen such as chloro or bromo; and X may be cyano or carboxamido. The compounds are prepared using a thiosalicylic acid or a substituted thiosalicylic acid as starting material.The compounds of this invention are active in the prevention of allergic and asthmatic reactions in mammals.Type: GrantFiled: December 15, 1975Date of Patent: March 22, 1977Assignee: Warner-Lambert CompanyInventors: Richard E. Brown, David M. Lustgarten
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Patent number: 4011177Abstract: Compounds having the formula ##STR1## wherein R is an alkyl group having from 1 to 4 carbon atoms are produced by the condensation of the appropriate alkoxylated epoxide with diethyl malonate. The unsaturated compound is formed by the dealkoxylation of an alkoxylated compound. These compounds have attractive fruity-floral type odors and are useful as ingredients of compounded perfumery compositions. The invention also includes perfumery compositions containing at least one of said compounds.Type: GrantFiled: June 5, 1975Date of Patent: March 8, 1977Assignee: Bush Boake Allen LimitedInventors: Hifzur Rahman Ansari, Paul Edgar Fido, Horst Richard Wagner
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Patent number: 4007208Abstract: Ester and amide derivatives of threo-hydroxycitric acid .gamma.-lactone inhibit fatty acid synthesis in biological systems and are useful in the treatment of obesity and in correcting conditions of lipid abnormalities.Type: GrantFiled: August 1, 1975Date of Patent: February 8, 1977Assignee: Hoffmann-La Roche Inc.Inventors: Robert William Guthrie, Richard Wightman Kierstead
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Patent number: 4006166Abstract: Ester and amide derivatives of threo-hydroxycitric acid .gamma.-lactone inhibit fatty acid synthesis in biological systems and are useful in the treatment of obesity and in correcting conditions of lipid abnormalities.Type: GrantFiled: August 1, 1975Date of Patent: February 1, 1977Assignee: Hoffmann-La Roche Inc.Inventors: Robert William Guthrie, Richard Wightman Kierstead