Patents Examined by Richard S. Myers, Jr.
-
Patent number: 5889022Abstract: Novel indole, indoline and quinoline derivatives of formula (I) processes for their preparation, pharmaceutical compositions containing them, and their use in medicine is disclosed. A structurally distinct class of compounds have now been discovered and have been found to exhibit 5HT.sub.1-D antagonist activity. In a first aspect, the present invention therefore provides a compound of formula (I) or a salt thereof, in which P is a 5-7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur, A, B, m, R.sup.1 -R.sup.8 are defined in the application.Type: GrantFiled: June 20, 1996Date of Patent: March 30, 1999Assignee: SmithKline Beecham, p.l.c.Inventors: Laramie Mary Gaster, Paul Adrian Wyman
-
Patent number: 5703106Abstract: The present invention provides novel compounds having pharmacological properties represented by the general formula I ##STR1## processes for the manufacture, pharmaceutical compositions and the use of the compounds of formula I and salts thereof.Type: GrantFiled: September 25, 1996Date of Patent: December 30, 1997Assignee: Japat Ltd.Inventors: Thomas Fruh, Thomas Pitterna, Toshiki Murata, Lene D. Svensson, Yoko Yuumoto, Junichi Sakaki
-
Patent number: 5703112Abstract: The present invention provides methods of preventing emesis and treating sexual dysfunction in mammals utilizing certain tetrahydrobenz?cd!indoles. The invention further provides pharmaceutical formulations suitable for use in such methods.Type: GrantFiled: November 17, 1995Date of Patent: December 30, 1997Assignee: Eli Lilly and CompanyInventors: Mark M. Foreman, J. David Leander
-
Patent number: 5703082Abstract: Levorotatory and dextrorotatory enantiomers of 1-?(4-chlorophenyl)phenylmethyl!-4-?(4-methylphenyl)sulfonyl!piperazine of the formula ##STR1## their preparation and use for the preparation of substantially optically pure enantiomers of 1-?(4-chlorophenyl)phenylmethyl!piperazine, which are themselves valuable intermediate products for the preparation of optically active therapeutic compounds having a very high degree of optical purity.Type: GrantFiled: June 5, 1995Date of Patent: December 30, 1997Assignee: U C B S.A.Inventors: Eric Cossement, Guy Bodson, Jean Gobert
-
Patent number: 5698708Abstract: Processes for preparing substituted 3-aryl-5-haloalkyl-pyrazoles and, specifically, for preparing C.sub.1-5 alkyl esters of 5-?1-(C.sub.1-5 alkyl)-4-halo-5-(C.sub.1-3 haloalkyl)-1H-pyrazole-3-yl!-2,4-dihalo-benzoic acids such as isopropyl 5-?4-bromo-1-methyl-5-(trifluoromethyl)-1H-pyrazole-3-yl!-2-chloro-4-fluor obenzoate, are presented. The described processes include novel approaches for forming phenyldiketones, forming and alkylating pyrazoles, brominating heterocyclic compounds, oxidizing alkyl-substituted benzene compounds, and esterifying carboxylic acids. These processes may be combined to prepare 3-aryl-5-haloalkyl pyrazoles, or alternatively, used in subcombinations or individually to prepare intermediates or other useful compounds.Type: GrantFiled: June 20, 1996Date of Patent: December 16, 1997Assignee: Monsanto CompanyInventors: Bruce C. Hamper, Michael K. Mao, Wendell Gary Phillips
-
Patent number: 5693633Abstract: This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.Type: GrantFiled: May 30, 1995Date of Patent: December 2, 1997Assignee: Eli Lilly and CompanyInventors: Donald B. Boyd, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, K. Jeff Thrasher, Venkatraghavan Vasudevan, Celia A. Whitesitt
-
Patent number: 5691376Abstract: A compound of the following structure: ##STR1## wherein R.sub.8 =H: R.sub.1 =alkyl, cycloalkyl, arylalkyl, aryl;R.sub.2 =cycloalkyl, aryl, C.sub.3 -C.sub.10 alkyl;X,Y=O, S(O).sub.n, NH;Z=CO.sub.2 R.sub.3, C(O)CO.sub.2 R.sub.3, CH(OH)CO.sub.2 R.sub.3, CHFCO.sub.2 R.sub.3, CF.sub.2 CO.sub.2 R.sub.3, CONR.sub.3 R.sub.4, CONR.sub.3 OR.sub.4, CONR.sub.3 NR.sub.4 R.sub.5, 1-tetrazole, C(O)CONR.sub.3 R.sub.4, CH(OH)CONR.sub.3 R.sub.4, CF.sub.2 CONR.sub.3 R.sub.4R.sub.3, R.sub.4, R.sub.5 =hydrogen, alkyl, aryl, aryalkyl, cycloalkyl, or fluoroalkyl;halo=Cl, Br, or I;fluoroalkyl=CF.sub.3, CHF.sub.2, CH.sub.2 F, CH.sub.2 CF.sub.3, C.sub.2 F.sub.5 ;cycloalkyl=C.sub.3 -C.sub.6 cycloalkyl;arylalkyl=C.sub.1 -C.sub.4 alkyl aryl;aryl=phenyl, furanyl, thienyl, or pyridyl; andn=0-2;or pharmaceutically acceptable salts thereof, useful in the treatment of asthma, and allergic and inflammatory diseases, as well as methods of treatment and pharmaceutical compositions utilizing the same.Type: GrantFiled: October 17, 1996Date of Patent: November 25, 1997Assignee: American Home Products CorporationInventors: Thomas J. Caggiano, Joseph Prol, Jr.
-
Patent number: 5691339Abstract: A circulatory disorder improving agent comprising, as an active ingredient, a dihydropyridine derivative of the formula (I) ##STR1## or an acid addition salt thereof. Said circulatory disorder improving agent is particularly useful as an organ circulation disorder improving agent or peripheral circulation improving agent.Type: GrantFiled: April 21, 1995Date of Patent: November 25, 1997Assignee: The Green Cross CorporationInventors: Hiroshi Shinyama, Toru Kawamura, Minori Okita, Takeshi Uchida, Masahiro Watanabe
-
Patent number: 5691337Abstract: Oxy-phenyl-(phenyl)glycinolamides with heterocyclic substituents are prepared by reaction of the corresponding oxyphenylcarboxylic acids with heterocyclic substituents with phenylglycinol. The new substances are suitable as active compounds in medicaments, in particular in agents having an antiatherosclerotic action.Type: GrantFiled: January 13, 1997Date of Patent: November 25, 1997Assignee: Bayer AktiengesellschaftInventors: Ulrich Muller, Richard Connell, Siegfried Goldmann, Klaus-Helmut Mohrs, Siegfried Raddatz, Michael Matzke, Rudi Grutzmann, Martin Beuck, Stefan Wohlfeil, Hilmar Bischoff, Dirk Denzer
-
Patent number: 5688826Abstract: Compounds for formula I ##STR1## in which X represents O, NR.sup.a, S, SO or SO.sub.2 and R is as defined in the specification; and non-toxic metabolically labile esters or amides thereof; and pharmaceutically acceptable salts thereof are useful as modulators of metabotropic glutamate receptor function.Type: GrantFiled: November 14, 1996Date of Patent: November 18, 1997Assignee: Eli Lilly and CompanyInventors: Steven Marc Massey, James Allen Monn, Matthew John Valli
-
Patent number: 5686461Abstract: The invention relates to compounds of formula (I). ##STR1## or a salt, or metabolically labile ester thereof wherein R.sub.1 represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SO.sub.2 R.sub.3 or COR.sub.3 wherein R.sub.3 represents hydroxy, methoxy, or amino; m is zero or an integer 1 or 2;A represents an ethynyl group or an optionally substituted ethenyl group;X represents a bond or a C.sub.1-4 alkylene chain;R.sub.2 represents a bridged cycloalkyl or bridged heterocyclic group; which are antagonists of excitatory amino acids, to processes for their preparation and to their use in medicine.Type: GrantFiled: September 18, 1995Date of Patent: November 11, 1997Assignee: Glaxo Wellcome S.p.A.Inventors: Alfredo Cugola, Giovanni Gaviraghi, Fabrizio Micheli
-
Patent number: 5686392Abstract: The herbicidally active substituted N-carbamoyl-tetrazolinones of the formula (I) ##STR1## in which R.sup.1 represents, inter alia, an (optionally substituted) phenyl radical,R.sup.2 represents, inter alia, an alkyl radical, andR.sup.3 represents, inter alia, a cycloalkyl radical,are obtained in very good yields and at high purity--i.e. free from the isomeric O-carbamoyloxytetrazoles (Ia)--by reacting tetrazolinones of the formula (II) with carbamoyl halides of the formula (III) (X=halogen) ##STR2## in the presence of an acid acceptor and in the presence of a diluent, at temperatures of between 0.degree. C. and 200.degree. C., and either isomerizing the O-carbamoylation product of the formula (Ia), which is formed under these circumstances as a byproduct, into the desired product of the formula (I) by heating, or else converting it by hydrolysis or alcoholysis into water-soluble, and thus readily separable, components (variable (a)).Type: GrantFiled: February 1, 1996Date of Patent: November 11, 1997Assignee: Bayer AktiengesellschaftInventors: Uwe Stelzer, Wolfgang Gau, Karl-Julius Reubke
-
Patent number: 5683965Abstract: The aryl-keto-enolic heterocycles according to the invention have the formula (I), in which Het stands for a heterocyclic group from the series (a), (b) or (c), and X, Y, Z, n, A, B, E, L and M have the meanings given in the description. The compounds having the formula (I) are pesticides, in particular acaricides, insecticides, fungicides and herbicides. Also disclosed is their preparation.Type: GrantFiled: May 13, 1996Date of Patent: November 4, 1997Assignee: Bayer AktiengesellschaftInventors: Jurgen Bachmann, Thomas Bretschneider, Reiner Fischer, Bernd-Wieland Kruger, Hans-Joachim Santel, Markus Dollinger, Christoph Erdelen, Ulrike Wachendorff-Neumann
-
Patent number: 5684006Abstract: A class of substituted isoxazole and pyrazole derivatives of formula (I), or a salt thereof of or a prodrug thereof, wherein the broken circle represents two non-adjacent double bonds whereby the five-membered ring containing X and Y is aromatic; one of X and Y represents nitrogen, and the other of X and Y represents oxygen or N--R.sup.5 ; R.sup.1 represents hydrogen, C.sub.1-6 alkyl or trifluoromethyl; R.sup.2 and R.sup.3 independently represent hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro, --OR.sup.a, --SR.sup.a, --SOR.sup.a, --SO.sub.2 R.sup.a, --SO.sub.2 NR.sup.a R.sup.b, --NR.sup.a R.sup.a, --NR.sup.a CO.sub.2 R.sup.b, --COR.sup.a, --CO.sub.2 R.sup.a or --CONR.sup.a R.sup.b, R.sup.4 represents hydrocarbon or a heterocyclic group; R.sup.5 represents hydrogen or C.sub.1-6 alkyl; and R.sup.a and R.sup.Type: GrantFiled: May 14, 1996Date of Patent: November 4, 1997Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Sylvie Bourrain, Joseph George Neduvelil, Paul David Leeson, Graham Andrew Showell
-
Patent number: 5681954Abstract: A compound represented by formula (I): ##STR1## wherein Q represents an aryl group, a heterocyclic group, a diarylmethyl group, an aralkyl group composed of an aryl group and an alkylene group, an alkyl group or a cycloalkyl group, in which the aryl group, heterocyclic group, and the aryl moiety of the diarylmethyl group and aralkyl group may be substituted with one or more substituents; R represents a bicyclic, substituted, nitrogen-containing heterocyclic group or a substituted phenyl group, in which the nitrogen-containing heterocyclic group is composed of a 5-membered, substituted, aromatic or saturated ring containing one or two nitrogen atoms and a 6-membered ring; and Z represents an alkylene group, an alkenylene group, an alkylene group, a carbonyl group, an alkylene group containing a carbonyl group or an oxalyl group, or a salt thereof.Type: GrantFiled: April 4, 1995Date of Patent: October 28, 1997Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Kenjiro Yamamoto, Atsushi Hasegawa, Hideki Kubota, Masahiro Ando, deceased, Hitoshi Yamaguchi
-
Patent number: 5679700Abstract: Novel phosphinic acid-containing peptidyl compounds of formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, and coronary thrombosis associated with atherosclerotic plaque rupture. These inhibitors may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation.Type: GrantFiled: November 9, 1995Date of Patent: October 21, 1997Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Philippe L. Durette, Joung L. Goulet, William K. Hagmann, Soumya P. Sahoo
-
Patent number: 5679677Abstract: The invention relates to heterocyclic carbamates of the formula (I) ##STR1## processes for their preparation and medicaments containing them.Type: GrantFiled: June 5, 1995Date of Patent: October 21, 1997Assignee: Luitpold Pharma GmbHInventors: Thomas Pill, Peter Zeiller, Wolfram Raake, Rainer Klauser
-
Patent number: 5677457Abstract: The present invention relates to a novel process for the preparation of physostigmine carbamate derivatives and to pharmaceutically acceptable salts thereof. The present invention further relates to a novel process for the preparation of eseroline derivatives and to pharmaceutically acceptable salts thereof.Type: GrantFiled: December 19, 1996Date of Patent: October 14, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Thomas B. K. Lee, Zhongli Gao, Barbara S. Rauckman
-
Patent number: 5672611Abstract: Novel compounds of Formula ##STR1## are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the Formula 1.0 to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.Type: GrantFiled: May 22, 1995Date of Patent: September 30, 1997Assignee: Schering CorporationInventors: Ronald J. Doll, Alan K. Mallams, Adriano Afonso, Dinanath F. Rane, Randall R. Rossman, F. George Njoroge
-
Patent number: 5672714Abstract: There is disclosed a method of manufacturing a 3-substituted-3-oxo-2-halopropionic acid amide compound, comprising halogenating a 3-substituted-3-oxopropionic acid amide compound with a 1,3-dihalo-5,5-dimethylhydantoin. There is also disclosed a method of manufacturing a 3-substituted-3-oxo-2-(5,5-dimethylhydantoin-3-yl)propionic acid amide compound, comprising steps of halogenating a 3-substituted-3-oxopropionic acid amide compound with a 1,3-dihalo-5,5-dimethylhydantoin, to obtain a corresponding 3-substituted-3-oxo-2-halopropionic acid amid compound, and reacting the resultant amide compound with 5,5-dimethylhydantoin in the presence of a base. This 3-substituted-3-oxo-2-hydantoinylpropionic acid amide compound is useful as a photographic yellow coupler for a color-photographic light-sensitive material.Type: GrantFiled: November 8, 1995Date of Patent: September 30, 1997Assignee: Fuji Photo Film Co., Ltd.Inventors: Katsuyoshi Yamakawa, Tadahisa Sato