Patents Examined by Richard S. Myers, Jr.
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Patent number: 5672790Abstract: The invention relates to the gas-phase hydrogenolysis of chlorofluorocarbons or of chlorofluorohydrocarbons in the presence of a palladium-based catalyst deposited on a support in which sulfur is incorporated into the catalyst in order to stabilize the catalytic activity.Type: GrantFiled: March 15, 1996Date of Patent: September 30, 1997Assignee: Elf Atochem S.A.Inventors: Dominique Guillet, Serge Hub
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Patent number: 5670509Abstract: Compounds of the formula X-Y-Z-R.sup.1 wherein:X is ##STR1## Y is --CO-- or --SO.sub.2 --; Z is an optional substituent selected from --NH--, --O--, --CHR--, --CH.dbd.CH--, --CH.dbd., --(CH.sub.2).sub.m -- or--CHCHOH--; andR.sup.1 is --CH.sub.3 --, --CH(CH.sub.3).sub.2, or substituted phenyl are tocolytic oxytocin antagonists useful in the treatment of pre-term labor, stripping labor preparatory to Caesarean delivery and dysmenorrhea.Type: GrantFiled: April 5, 1995Date of Patent: September 23, 1997Assignee: Merck & Co., Inc.Inventors: Ben E. Evans, Douglas W. Hobbs, Joseph M. Pawluczyk, Douglas J. Pettibone, Kenneth E. Rittle, Peter D. Williams
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Patent number: 5670655Abstract: The invention relates to a method for analyzing degenerates of enalapril maleate and enalaprilat, potent angiotensin converting enzyme inhibitors.Type: GrantFiled: September 10, 1996Date of Patent: September 23, 1997Assignee: Merck & Co. Inc.Inventors: Xue-Zhi Qin, Giuseppina Visentini, Qingxi Wang
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Patent number: 5665887Abstract: A novel methine compound is disclosed, which contains a rhodanine ring substituted with a linear or branched alkyl, alkenyl, or alkynyl group containing at least one carboxyl group and at least one ester bond, amide bond, or ether bond. The methine compound has excellent stability and dyeing power.Type: GrantFiled: August 9, 1996Date of Patent: September 9, 1997Assignee: Fuji Photo Film Co., Ltd.Inventor: Toyohisa Oya
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Patent number: 5665721Abstract: The present invention provides new heterocyclic substituted cyclopentane compounds that are useful in inhibiting adenosine kinase. The present invention also provides pharmaceutical compositions containing such compounds and methods of using such compounds for inhibiting adenosine kinase.Type: GrantFiled: June 7, 1995Date of Patent: September 9, 1997Assignee: Abbott LaboratoriesInventors: Shripad S. Bhagwat, Marlon Daniel Cowart
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Patent number: 5665717Abstract: Carbacephalosporin compounds of formula (I), ##STR1## salts thereof, processes for their synthesis and uses thereof, wherein: R.sup.1 is hydrogen, methoxy or formamido; R.sup.2 is an acyl group; CO.sub.2 R.sup.3 is a carboxy group or a carboxylate anion, or R.sup.3 is a carboxy protecting group or a pharmaceutically acceptable salt-forming group or in vivo hydrolysable ester group; R.sup.4, R.sup.5, R.sup.6 and R.sup.7 represent hydrogen or a substituent; R.sup.4 and R.sup.7 may be replaced by a chemical bond between the two carbon atoms shown; R.sup.5 and R.sup.6 may be linked together into a cyclic system. The compounds (I) have antibacterial properties.Type: GrantFiled: January 18, 1996Date of Patent: September 9, 1997Assignee: Pfizer Inc.Inventors: Richard Leonard Elliott, Neville Hubert Nicholson, Andrew Kenneth Takle
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Patent number: 5663190Abstract: There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperldinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl,with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.Type: GrantFiled: October 16, 1992Date of Patent: September 2, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Richard L. Hamer, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang
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Patent number: 5658910Abstract: Novel compounds of the formula: ##STR1## wherein R is selected from saturated or unsaturated alkyls, saturated or unsaturated cycloalkyls, heterocyclic compounds, or from (a) or (b) wherein G is carbon wherein G is carbon or nitrogen; m is 0-10, wherein R.sub.1, R.sub.2, and R.sub.3 are the same or different and selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbons or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl and the pharmacologically acceptable salts thereof; being useful for treating disorder in the central nervous system.Type: GrantFiled: May 3, 1995Date of Patent: August 19, 1997Assignee: Pharmacia ABInventors: Anders Bjork, Gunnar Andersson, Catarina Ludwig, Elisabeth Seifert, Arne Nilsson, Torbjorn Lundstedt, Lisbeth Abramo, Goran Pettersson, Curt Nordvi, Jin Chang Wu
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Patent number: 5658899Abstract: The invention provides a series of crystalline salts of (S)-8-chloro-5-(5-bromo-2,3-dihydrobenzofuran-7-yl)-3-methyl-2,3,4,5-tetra hydro-1H-3-benzazepine-7-ol, their preparation and use as therapeutic agents.Type: GrantFiled: March 14, 1995Date of Patent: August 19, 1997Assignee: Novo Nordisk A/SInventors: Louis Brammer Hansen, Rolf Emil Amsler, Scott Eugene McGraw
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Patent number: 5654296Abstract: The compound ##STR1## wherein ring A represents a benzene ring;Ar represents an aromatic group;R.sup.1 and R.sup.2 independently represent hydrogen, acyl or hydrocarbon group or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom represent a nitrogen-containing heterocyclic group;m represents an integer of 1 to 6;n represents an integer of 2 to 3;- - - - - represents a single bond or a double bond;X stands for --O-- or --NR.sup.3 -- in which R.sup.3 represents hydrogen, acyl or hydrocarbon group where - - - - - is a single bond or .dbd.N-- where - - - - - is a double bond has excellent GnRH receptor antagonizing activity, calcium antagonizing and monoamine-uptake inhibiting activities and and value as a prophylactic/therapeutic drug for sex hormone-dependent diseases and for central nervous system diseases.Type: GrantFiled: December 6, 1996Date of Patent: August 5, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato, Yasuo Nagai
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Patent number: 5654305Abstract: The present invention provides compounds of formula ##STR1## wherein Y is >C.dbd.O or >S(O).sub.t wherein t is 1 or 2 and the pharmaceutically acceptable salts thereof which are potent antagonists of PAF and are useful in the treatment of PAF-related disorders including asthma, rhinitis, shock, respiratory distress syndrome, acute inflammation, transplanted organ rejection, gastrointestinal ulceration, allergic skin diseases, delayed cellular immunity, parturition, fetal lung maturation, and cellular differentiation.Type: GrantFiled: July 2, 1996Date of Patent: August 5, 1997Assignee: Abbott LaboratoriesInventors: George S. Sheppard, Steven K. Davidsen, James B. Summers, George M. Carrera, Jr.
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Patent number: 5652242Abstract: Compounds of formula I ##STR1## and metabolically labile esters and amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.13, M.sup.2, X.sup.1, Z.sup.1, Z.sup.1a, X.sup.2 and A.sup.1 have the meanings given in the specification. The compounds are useful as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa. Novel intermediates are also disclosed.Type: GrantFiled: June 1, 1995Date of Patent: July 29, 1997Assignee: Zeneca LimitedInventors: Michael Garth Wayne, Michael James Smithers, John Wall Rayner, Alan Wellington Faull, Robert James Pearce, Andrew George Brewster, Richard Eden Shute, Stuart Dennett Mills, Peter William Rodney Caulkett
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Patent number: 5650411Abstract: The use for the manufacture of a medicament for treating Helicobacter-related diseases of a compound of formula ##STR1## a pharmaceutically acceptable acid addition salt or a stereochemically isomeric form thereof, whereinX and Y each independently are CH or N;R.sup.1, R.sup.2 and R.sup.3 each independently are hydrogen or C.sub.1-4 alkyl;R.sup.4 and R.sup.5 each independently are hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy;Z is C.dbd.O or CHOH; andAr is phenyl optionally substituted with up to three substituents selected from hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, halo, trifluoromethyl, triC.sub.1-4 alkylsilyloxy, nitro, amino and cyano or pyridinyl substituted with hydroxy or C.sub.Type: GrantFiled: July 18, 1995Date of Patent: July 22, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Jan Heeres, Joseph Hector Mostmans, Luc Alfons Leo Van Der Eycken, Frank Christopher Odds, Raymond Antoine Stokbroekx, Marcel Jozef Maria Van der Aa
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Patent number: 5646158Abstract: This invention relates to certain 1,3,3-(trisubstituted)cyclohex-1-ene monomers and related compounds which are useful in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).Type: GrantFiled: February 27, 1996Date of Patent: July 8, 1997Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, M. Dominic Ryan, Paul E. Bender
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Patent number: 5643922Abstract: The present invention provides compounds of formula ##STR1## and the pharmaceutically acceptable salts thereof which are potent antagonists of PAF and are useful in the treatment of PAF-related disorders including asthma, rhinitis, shock, respiratory distress syndrome, acute inflammation, transplanted organ rejection, gastrointestinal ulceration, allergic skin diseases, delayed cellular immunity, parturition, fetal lung maturation, and cellular differentiation.Type: GrantFiled: July 2, 1996Date of Patent: July 1, 1997Assignee: Abbott LaboratoriesInventors: George S. Sheppard, Steven K. Davidsen, James B. Summers
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Patent number: 5644057Abstract: Disclosed are compounds of the formula ##STR1## wherein Ar represents an aryl or heteroaryl group; andR.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 represent organic or inorganic substituents,which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and, thus, are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as well as depression, headache and anxiety.Type: GrantFiled: May 12, 1995Date of Patent: July 1, 1997Assignee: Neurogen CorporationInventors: Jun Yuan, Alan Hutchison
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Patent number: 5641779Abstract: The present invention relates to compounds having the formula: ##STR1## wherein R.sub.1 is a hydrogen atom, a linear or branched alkyl radical or a phenyl, benzyl, cycloalkyl, polycycloalkyl, dibenzocycloalkyl, dibenzooxepine, dibenzoazepine, dibenzothiepine, benzopyrrolocycloalkyl, benzothienocycloalkyl or naphthyl radical, optionally substituted by one or a number of substituents chosen from halogen atoms and alkyl, aryl acyl, alkoxy and alkyl thio radicals.Z is C.dbd.O, SO.sub.2 or (CH.sub.2).sub.n in which n is between 1 and 5.R.sub.2 is a hydrogen atom, a linear or branched alkyl radical or a phenyl, benzyl, cycloalkyl, pyrrole, furan, pyridinyl or thiophenyl radical, optionally substituted by one or a number of substituents chosen from halogen atoms and alkyl, aryl, acyl, alkoxy and alkylthio radicals.R'.sub.2 is a hydrogen atom, a linear or branched alkyl radical or a phenyl radical.R.sub.3 is a hydrogen atom, a linear or branched alkyl radical or a benzyl or phenethyl radical.R.sub.Type: GrantFiled: June 29, 1995Date of Patent: June 24, 1997Assignee: Pierre Fabre MedicamentInventors: Serge Halazy, Michel Perez, Michael Briley
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Patent number: 5639877Abstract: Novel amidine salts of 7-Amino-3-hydroxymethyl-3-cephem-4-carboxylic acid (=HACA), particular guanidine and diaza-bicyclo-alkylene salts, are useful as intermediates in the synthesis of cephalosporins.Type: GrantFiled: July 28, 1994Date of Patent: June 17, 1997Assignee: Biochemie Gesellschaft m.b.H.Inventors: Johannes Ludescher, Ingolf Macher
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Patent number: 5637584Abstract: The invention provides a methylene chloride solvate of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine. The invention provides a method for using such solvate.Type: GrantFiled: March 24, 1995Date of Patent: June 10, 1997Assignees: Eli Lilly and Company, Lilly Industries LimitedInventor: Samuel D. Larsen
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Patent number: 5637586Abstract: A benzimidazolesulfonamide derivative of the formula (I): ##STR1## wherein R.sup.1 is an alkyl group of 1 to 6 carbon atoms or a haloalkyl group of 1 to 6 carbon atoms; R.sup.2 is a hydrogen atom, an alkyl group of 1 to 6 carbon atoms, a haloalkyl group of 1 to 6 carbon atoms, --OR.sup.4, --O(CH.sub.2).sub.m C.sub.6 H.sub.5, --(CH.sub.2).sub.n C.sub.6 H.sub.5, --NH.sub.2, --NHR.sup.5, --NHC (.dbd.O)R.sup.6, --N(R.sup.7).sub.2, --NHC(.dbd.O) (CH.sub.2).sub.p C.sub.6 H.sub.5, or --NHC(.dbd.O)CH(C.sub.6 H.sub.5).sub.2 ; R.sup.3 is an azole group, --COOH, --COOR.sup.8, or --SO.sub.3 H; A is --O--, --NH--, or --S(O).sub.q --; R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are independently an alkyl group of to 6 carbon atoms; m, n, and p are independently 0 or an integer of 1 to 6; and q is 0, 1, or 2, or a salt thereof; and a pharmaceutical composition comprising the above compound are disclosed. The compound exhibits a stable and strong antagonism to angiotensin II.Type: GrantFiled: August 4, 1995Date of Patent: June 10, 1997Assignee: Kureha Chemical Industry Co., Ltd.Inventors: Mikiro Yanaka, Hiroyuki Enari, Toshikazu Dewa, Toru Yamazaki