Patents Examined by Jane T. Fan
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Patent number: 5389649Abstract: Oxathiane derivatives of formula ##STR1## in which R represents alkyl and A represents optionally substituted phenyl or a heteroaromatic group containing 1 or 2 nitrogen atoms optionally substituted by alkyl, alkoxy or halogen, and salts thereof possess pharmacological activity and are also useful in inhibiting head hair loss.Type: GrantFiled: July 20, 1992Date of Patent: February 14, 1995Assignee: Rhone-Poulenc Rorer LimitedInventors: Iain M. McLay, Roger J. A. Walsh
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Patent number: 5382593Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and X are as defined in the description, its Z and E isomers, its optical isomers, in pure form or in the form of a mixture, and its addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful in treating a disorder resulting from or associated with peroxidation phenomena, disturbances in eicosanoid synthesis, or with platelet aggregation disorders.Type: GrantFiled: July 20, 1993Date of Patent: January 17, 1995Assignee: Adir et CompagnieInventors: Guillaume Le Baut, Marie-Renee Nourrisson, Jean-Francois Renaud de la Faverie, Jean-Guy Bizot Espiard, Daniel-Henri Caignard, Pierre Renard, Gerard Adam
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Patent number: 5380853Abstract: The compounds of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl, alkoxy or phenylalkyloxy; R.sub.1 is thienyl, imidazolyl, thiazolyl, pyridinyl, quinolinyl, pyrimidinyl, pyrazinyl, benzamidazolyl, phenylalkylpiperidinyl or morpholino or athaae analogous hetercyclic groups with from one to tahree substituents selected from halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino of 1 to 6 carbon atoms, dialkylamino in which each alkyl group has 1 to 6 carbon atoms, alkyl of 1 to 6 carbon atoms, or alkoxy of 1 to 6 carbon atoms; R.sub.2 is hydrogen, alkyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl in which said substituent is alkyl, alkoxy, halogen, cyano, trifluoromethyl amino, nitro, alkylamino or dialkylamino; and a pharmaceutically acceptable salt thereof; are ACAT inhibitors, some of which possess antioxidant properties.Type: GrantFiled: November 15, 1993Date of Patent: January 10, 1995Assignee: American Home Products CorporationInventors: William F. Fobare, Donald P. Strike
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Patent number: 5380857Abstract: A process for the production of 7-acylindoles of the general formula: ##STR1## starting from indoline of the formula: ##STR2## Indoline is cyanized in a first stage to 7-cyanoindoline of the formula: ##STR3## The latter is catalytically dehydrogenated in a second stage to 7-cyanindole of the formula: ##STR4## The latter is then acylated in a third stage with an organometallic compound of the formula:R--Q Vinto the end product according to formula I.Type: GrantFiled: June 30, 1993Date of Patent: January 10, 1995Assignee: Lonza Ltd.Inventors: Jean-Paul Roduit, Alain Wellig
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Patent number: 5378718Abstract: Compounds a formula (I) ##STR1## wherein the substituents and symbols have the meanings given in the specification, are new compounds with marked cardiovascular activity.Type: GrantFiled: January 22, 1993Date of Patent: January 3, 1995Assignee: Cedona Pharmaceuticals B.V.Inventors: Jan Bron, Geert J. Sterk, Hendrik Timmerman, Jan F. Van Der Werf
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Patent number: 5376668Abstract: The present invention relates to therapeutically active azacyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease, severe painful conditions and glaucoma.Type: GrantFiled: March 5, 1993Date of Patent: December 27, 1994Assignee: Novo Nordisk A/SInventors: Per Sauerberg, Preben H. Olesen, Charles H. Mitch
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Patent number: 5376677Abstract: The invention relates to novel compounds of the formula ##STR1## in which R is as defined in the description, to their preparation, to fungicidal compositions which contain such compounds as active substances, and to the use of the active substances or compositions for controlling fungi in agriculture and horticulture.Type: GrantFiled: March 22, 1993Date of Patent: December 27, 1994Assignee: Ciba-Geigy CorporationInventor: Stephan Trah
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Patent number: 5374730Abstract: Omeprazole and lansoprazole, which are chemically pyridine-benzimidazole sulfinyl compounds, are produced from the corresponding acetamide-sulfide compounds by a process of oxidation to form the amide sulfinyl compound, followed by alkaline hydrolysis to the sulfinyl carboxylate or salt, and decarboxylation.Type: GrantFiled: November 4, 1993Date of Patent: December 20, 1994Assignee: Torcan Chemical Ltd.Inventors: Clarke Slemon, Bob Macel
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Patent number: 5374640Abstract: The present invention relates to pyridyl-1,2,5-oxadiazolcarboxamide-2-oxides of the general formula I ##STR1## in which one of the radicals R.sup.1 and R.sup.2 represents pyridyl and the other represents ##STR2## and R.sup.3 and R.sup.4 are defined as indicated in claim 1, processes for their preparation and their use.Type: GrantFiled: May 25, 1993Date of Patent: December 20, 1994Assignee: Cassella AktiengesellschaftInventors: Karl Schonafinger, Helmut Bohn
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Patent number: 5371096Abstract: Disclosed are compounds of formula ##STR1## wherein R is OR' and R' is aryl-lower alkyl, biaryl-lower alkyl, lower alkyl or cycloalkyl-lower alkyl; or R is arylsulfonylamido;n is 1, 2 or 3;m is 1, 2 or 3;Y is vinylene, ethylene or methyleneoxy; a stereoisomer or optical isomer thereof; and their pharmaceutically acceptable esters or salts; which are useful as thromboxane synthetase inhibitors and thromboxane receptor antagonists.Type: GrantFiled: August 27, 1993Date of Patent: December 6, 1994Assignee: Ciba-Geigy CorporationInventor: Isodoros Vlattas
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Patent number: 5369086Abstract: Substituted N-benzotriazoles of the general formula ##STR1## exhibit herbicidal activity. Herbicidal compositions and related methods of using the substituted N-benzotriazoles are also disclosed.Type: GrantFiled: April 28, 1993Date of Patent: November 29, 1994Assignee: Zeneca LimitedInventors: Donald R. James, Raymond A. Felix
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Patent number: 5364872Abstract: The diastereoisomer A of a dihydropyridine-3,5-dicarboxylic acid ester derivative is provided as well as its pharmaceutically acceptable acid addition salts. The invention further discloses a process for producing the compounds and their use as medicaments in imparting vasodilating activity.Type: GrantFiled: January 23, 1992Date of Patent: November 15, 1994Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kazuharu Tamazawa, Tadao Kojima, Hideki Arima, Yukiyasu Murakami, Yasuo Isomura, Minoru Okada, Toichi Takenaka, Kiyoshi Takanobu
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Patent number: 5362729Abstract: Compounds which are useful in anti-tumors therapy having the formula (I) ##STR1## wherein Het imidazole, A represents a direct linkage at the phenyl 4-position: R is hydrogen; one of R.sub.3 and R.sub.4 is C.sub.1 -C.sub.3 alkyl unsubstituted or omega substituted by C.sub.1 -C.sub.3 alkoxy, and the other, independently, is:a) C.sub.1 -C.sub.3 alkyl unsubstituted or omega substituted by C.sub.1 -C.sub.3 alkoxy; orb) --(CH.sub.2).sub.m --O--(CH.sub.2).sub.n --NR.sub.a R.sub.b wherein each of m and n, which may be the same or different is an integer of 1 to 3, each of R.sub.a and R.sub.b, which may be the same or different, is hydrogen or C.sub.1 -C.sub.3 alkyl; R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by a morpholino;each of R.sub.1 and R.sub.2 is independently a group --OR' wherein R' is C.sub.1 -C.sub.6 alkyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 1, 1992Date of Patent: November 8, 1994Assignee: Farmitalia Carlo ERBA S.r.l.Inventors: Paolo Cozzi, Maria Menichincheri, Laura Capolongo, Nicola Mongelli
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Patent number: 5362873Abstract: A compound of the formula: ##STR1## wherein n is an integer of from 2 to 6; and p and q each is an integer of 0 or 1, excluding the case where p is 0 when q is 1; or a pharmaceutically acceptable acid addition salt thereof. This compound has a high affinity and specificity to .sigma. receptors, and is thought to be effective for treatment of some psychoses.Type: GrantFiled: June 14, 1993Date of Patent: November 8, 1994Assignee: Shionogi & Co., Ltd.Inventors: Hiromu Matsumura, Toshisada Yano, Hiroshi Hashizume, Akira Matsushita, Masami Eigyo
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Patent number: 5360812Abstract: The present invention relates to fused 1,2,5-oxadiazole-2-oxides of the general formula I ##STR1## in which A denotes ##STR2## and X, Y, Z as well as R.sup.1, R.sup.2, R.sup.3 and n are defined as indicated in Claim 1, to processes for their preparation and to their use for the control and prevention of disorders of the cardiovascular system, in particular for the control and prevention of angina pectoris, and for the treatment of erectile dysfunctions.Type: GrantFiled: May 25, 1993Date of Patent: November 1, 1994Assignee: Cassella AktiengesellschaftInventors: Joachim Brendel, Karl Schonafinger, Helmut Bohn
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Patent number: 5358964Abstract: The manufacture and use of compounds of the formula ##STR1## wherein Y is O or S, R.sub.1 is hydrogen or alkyl, and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are hydrogen or various substituent groups, and pharmaceutically acceptable acid addition salts thereof. The compounds have activity as inhibitors of the IL-I or other agonist-induced proteoglycan degradation in bovine nasal cartilage and pharmaceutical compositions containing such compounds are described to treat conditions advantageously affected by such inhibition including arthritis.Type: GrantFiled: July 26, 1993Date of Patent: October 25, 1994Assignee: Warner-Lambert CompanyInventors: Vijaykumar Baragi, Diane H. Boschelli, David T. Connor, Richard R. Renkiewicz
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Patent number: 5356911Abstract: Substituted biphenylpyridones can be prepared by alkylating pyridones on the nitrogen. The substituted biphenylpyridones are suitable as active substances in medicaments, in particular in hypotensive and anti-atherosclerotic medicaments.Type: GrantFiled: November 2, 1992Date of Patent: October 18, 1994Assignee: Bayer AktiengesellschaftInventors: Matthias Muller-Gliemann, Martin Beuck, Stanislav Kazda, Johannes-Peter Stasch, Andreas Knorr, Stefan Wohlfeil, Walter Hubsch, Jurgen Dressel, Peter Fey, Rudolf Hanko, Thomas Kramer, Ulrich Muller, Siegfried Zaiss
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Patent number: 5356915Abstract: The present invention relates to new tetralones having formula I: ##STR1## wherein R.sup.1 to R.sup.7 are as defined in claim 1. The invention also relates to processes for their preparation, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments. These compounds are antihypertensive and bronchodilator agents.Type: GrantFiled: April 20, 1993Date of Patent: October 18, 1994Assignee: J. Uriach & Cia. S.A.Inventors: Carmen Almansa, Concepcion Gonzalez, Ma. Carmen Torres, Elena Carceller, Javier Bartroli
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Patent number: 5354866Abstract: A retroviral protease inhibiting compound of the formula A--X--B is disclosed. Also disclosed are a composition and method for inhibiting a retroviral protease and for treating an HIV infection. Also disclosed are processes and intermediates useful for the preparation of the retroviral protease inhibitors.Type: GrantFiled: September 14, 1993Date of Patent: October 11, 1994Assignee: Abbott LaboratoriesInventors: Dale J. Kempf, Daniel W. Norbeck, Lynn M. Codacovi, Jacob J. Plattner, Hing L. Sham, Chen Zhao
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Patent number: 5352795Abstract: The invention is concerned with aromatase inhibiting compounds of formula I ##STR1## wherein R and Ro represent hydrogen or lower alkyl; or R and Ro located on adjacent carbon atoms and together when combined with the benzene ring to which they are attached form a naphthalene or tetrahydronaphthalene ring; R.sub.1 and R.sub.2 independently represent hydrogen, lower alkyl, (lower alkyl, aryl or aryl-lower alkyl)-thio, lower alkenyl, aryl, aryl-lower alkyl, C.sub.3 -C.sub.6 -cycloalkyl, or C.sub.3 -C.sub.6 -cycloalkyl-lower alkyl; or R.sub.1 and R.sub.2 combined represent lower alkylidene, mono-or di-aryl-lower alkylidene; R.sub.1 and R.sub.2 combined also represent C.sub.4 -C.sub.6 -straight chain alkylene, lower alkyl-substituted straight chain alkylene or ortho-phenylene bridged-C.sub.2 -C.sub.Type: GrantFiled: May 11, 1992Date of Patent: October 4, 1994Assignee: Ciba-Geigy CorporationInventors: Robert M. Bowman, Leslie J. Browne