Additional Nitrogen Other Than Cyano Patents (Class 514/523)
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Patent number: 5489605Abstract: Cyanooxime ethers of the formula IR.sup.1 R.sup.2 CH--ON.dbd.C(CN)--R.sup.3 IwhereR.sup.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl;R.sup.2 is an unsubstituted or substituted mononuclear to trinuclear aliphatic or aromatic ring system which, in addition to carbon atoms, may contain from one to four nitrogen atoms or from one to three hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen andR.sup.3 is unsubstituted or substituted alkyl or an unsubstituted or substituted aliphatic ring system which, in addition to carbon atoms, may contain one or two hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen,processes for their preparation, agents containing them and their use.Type: GrantFiled: August 24, 1994Date of Patent: February 6, 1996Assignee: BASF AktiengesellschaftInventors: Klaus Oberdorf, Uwe Kardorff, Hans Theobald, Albrecht Harreus, Hartmann Koenig, Volker Harries
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Patent number: 5476875Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Type: GrantFiled: October 21, 1994Date of Patent: December 19, 1995Assignee: Hoffman-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
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Patent number: 5457132Abstract: A kit containing benzeneacetonitrile and calcium or dihydropyridine and calcium hypertensive mammals may be treated to lower mean blood pressure by administering a calcium channel blocking agent together with one or both of a calcium supplement and Vitamin D. The hypotensive effect of this combination is synergistic and the dose response is more predictable than the administration of any of these agents singly.Type: GrantFiled: June 22, 1994Date of Patent: October 10, 1995Assignee: Peter K. T. PangInventors: Peter K. T. Pang, Richard Z. Lewanczuk, Christine G. Benishin
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Patent number: 5457131Abstract: The present invention relates to cyclopentane heptanoic or cyclopentane heptenoic acid, 2-hydrocarbyl sulfonamidomethyl, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.Type: GrantFiled: August 18, 1994Date of Patent: October 10, 1995Assignee: Allergan, Inc.Inventor: Steven W. Andrews
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Patent number: 5455273Abstract: The invention relates to N,N-disubstituted arylcycloalkylamines of general formula ##STR1## wherein n, m, A, X and R.sup.1 to R.sup.7 are defined as in claim 1, the isomers, isomer mixtures and salts thereof, which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis.Type: GrantFiled: November 19, 1993Date of Patent: October 3, 1995Assignee: Karl Thomae GmbHInventors: Roland Maier, Peter Muller, Eberhard Woitun, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
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Patent number: 5451607Abstract: There are disclosed hydrazone derivatives of the general formula [I]: ##STR1## wherein R.sup.1 is halogen, etc.; R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl, etc.; R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, etc.; R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl, etc.; R.sup.5 is C.sub.1 -C.sub.6 alkyl, etc.; R.sup.6 is hydrogen or C.sub.1 -C.sub.6 alkyl, etc.; A is (CH.sub.2).sub.t, O, S(O).sub.n, etc.; a is an integer of 1 to 4; n is an integer of 0 to 2; and t is an integer of 1 to 3; as well as production processes therefor, insecticides and/or acaricides containing the same as an active ingredient and intermediate compounds thereof.Type: GrantFiled: April 19, 1993Date of Patent: September 19, 1995Assignee: Sumitomo Chemical Co., Ltd.Inventors: Toshiaki Taki, Hirosi Kisida, Shigeru Saito, Shinji Isayama
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Patent number: 5449686Abstract: Novel cyclohexanes of Formulas (I) and (II) ##STR1## are described herein. They inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production; these compounds are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase V.Type: GrantFiled: September 29, 1994Date of Patent: September 12, 1995Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Paul E. Bender, Cornelia J. Forster
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Patent number: 5432196Abstract: A process for preparing an aqueous active substance solution which can be sterilized by filtration entails mixing anipamil hydrochloride with a phospholipid in the ratio of from 1:2 to 2:1 by weight, converting the resulting mixture into a gel by adding water at elevated temperature, and subsequently adding water to the gel at elevated temperature until the active substance is present in the required concentration.Type: GrantFiled: January 13, 1994Date of Patent: July 11, 1995Assignee: Knoll AGInventors: Joerg Rosenberg, Rolf Neidhardt, Guenter Blaich
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Patent number: 5420165Abstract: There are provided substituted acid amide, arylhydrazone compounds (amidrazones) of formula I ##STR1## the use thereof for the control of insect and acarid pests and methods and compositions for the protection of crops from the damage and loss caused by said pests.Type: GrantFiled: December 29, 1992Date of Patent: May 30, 1995Assignee: American Cyanamid CompanyInventors: Joseph A. Furch, David G. Kuhn, David A. Hunt
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Patent number: 5395853Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, orPh(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, orR.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, orR.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; ##STR2## Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.Type: GrantFiled: November 24, 1993Date of Patent: March 7, 1995Assignee: Burroughs Wellcome Co.Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
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Patent number: 5389619Abstract: Compounds of the formula I ##STR1## where n, W, X, Y, Z, R.sup.1, R.sup.2, and R.sup.3 are as defined herein exhibit fungicidal, insecticidal, and acaracidal activity.Type: GrantFiled: March 29, 1993Date of Patent: February 14, 1995Assignee: BASF AktiengesellschaftInventors: Reinhard Doetzer, Hubert Sauter, Horst Wingert, Reinhard Kirstgen, Albrecht Harreus, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5387608Abstract: The present invention relates to cyclopentane heptanoic or cyclopentane heptenoic acid, 2-hydrocarbyl sulfonamidomethyl, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.Type: GrantFiled: August 17, 1993Date of Patent: February 7, 1995Assignee: Allergan, Inc.Inventor: Steven W. Andrews
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Patent number: 5380755Abstract: The present invention provides alkyl and alkylbenzyl ethers of substituted hydroquinones and pharmaceutical compositions containing them. The present invention further provides methods of using these compounds and compositions to inhibit monoamine oxidase, particularly monoamine oxidase B. The present invention further provides methods for the treatment of diseases involving monoamine oxidase.Type: GrantFiled: July 24, 1992Date of Patent: January 10, 1995Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Argyrios G. Arvanitis, Everett L. Scholfield
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Patent number: 5366994Abstract: A combination of angiotensin-converting enzyme inhibitors and calcium antagonists for the treatment of proteinuria is disclosed. The invention relates to the prevention and therapy of proteinuria by administration of a combination of ACE inhibitor and calcium antagonist.Type: GrantFiled: May 6, 1993Date of Patent: November 22, 1994Assignee: Hoechst AktiengesellschaftInventors: Reinhard Becker, Rainer Henning, Volker Teetz, Hansjorg Urbach
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Patent number: 5356931Abstract: Alpha-Arylacrylic acid derivatives of the general formula I ##STR1## where X is ethylene or ethenylene; n is 0 or 1;m is 0, 1, 2, 3 or 4;R.sup.1 is cyano, cyanato, thiocyanato, nitro, hydroxyl, carboxyl, haloalkyl, haloalkoxy, unsubstituted or substituted cycloalkyl, cycloalkenyl, cycloalkadienyl, alkenyl, alkynyl or amino, alkylcarbonyl, alkoxycarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, unsubstituted or substituted benzyloxycarbonyl, benzoyl, phenylalkyl, phenylalkoxy or phenoxyalkyl,or R.sup.1 together with one of the radicals R.sup.2 forms an unsubstituted or substituted 1,3-butadiene-1,4-diyl group or an unsubstituted or substituted chain consisting of carbon members and an oxygen member, andR.sup.2 is halogen, unsubstituted or substituted alkyl, alkoxy, alkenyloxy, alkynyloxy, alkadienyloxy, benzyloxy or benzylthio, are used for controlling pests.Type: GrantFiled: January 4, 1993Date of Patent: October 18, 1994Assignee: BASF AktiengesellschaftInventors: Reinhard Kirstgen, Rainer Otter, Christoph Kuenast, Uwe Kardorff, Wolfgang Steglich, Gunda Bertram
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Patent number: 5350771Abstract: Hypertensive mammals may be treated to lower mean blood pressure by administering a calcium channel blocking agent together with one or both of a calcium supplement and Vitamin D. The hypotensive effect of this combination is synergistic and the dose response is more predictable than the administration of any of these agents singly.Type: GrantFiled: December 28, 1992Date of Patent: September 27, 1994Assignee: Peter K. T. PangInventors: Peter K. T. Pang, Richard Z. Lewanczuk, Christine G. Benishin
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Patent number: 5342853Abstract: The use of nor-verapamil and nor-gallopamil and the salts thereof with physiologically tolerated acids is disclosed for the preparation of drugs with antiarteriosclerotic properties.Type: GrantFiled: November 12, 1991Date of Patent: August 30, 1994Assignee: Knoll AGInventors: Claus D. Mueller, Liliane Unger
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Patent number: 5294613Abstract: This invention provides benzene derivatives, pharmaceutical formulations of those derivatives, and a method of using the derivatives for the treatment of inflammation in mammals.Type: GrantFiled: February 7, 1992Date of Patent: March 15, 1994Assignee: Eli Lilly and CompanyInventors: Nancy G. Bollinger, Theodore Goodson, Jr., David K. Herron
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Patent number: 5290814Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, or Ph(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, or R.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, or R.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; X is ##STR2## where A is halogen; Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.Type: GrantFiled: November 5, 1992Date of Patent: March 1, 1994Assignee: Burroughs Wellcome Co.Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
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Patent number: 5288742Abstract: The invention concerns .alpha.,.alpha.-dialkylbenzyl derivatives of the formula I ##STR1## wherein Ar.sup.1 is phenyl or naphthyl, or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;A.sup.1 is a direct link to X.sup.1 or is (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;the phenylene group may optionally bear one or two substituents R.sup.3 ;each of R.sup.1 and R.sup.2, which may be the same or different, is (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, fluoro-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl, provided that both of R.sup.1 and R.sup.2 are not methyl or fluoromethyl; andQ is cyano, amino, nitro, formyl, (1-4C)alkoxy, thiazolyl or (2-4C)alkanoyl;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.Type: GrantFiled: March 18, 1992Date of Patent: February 22, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Philip N. Edwards, David Waterson
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Patent number: 5268385Abstract: This invention provides a method for treating the symptoms of schizophrenia by interacting selectively with presynaptic dopaminergic D.sub.2 receptors without appreciably activating postsynaptic dopamine receptors which comprises administering to a schizophrenic an effective amount of a compound selected from the group consisting essentially of the stereoisomers of mixtures thereof of compounds represented by the general formula: ##STR1## wherein R.sub.1 is selected from the group consisting of pyridyl and ##STR2## X is oxygen or sulfur, Y, if present, is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms, and a is an integer between zero and 3, R.sub.2 is H, R.sub.Type: GrantFiled: November 18, 1991Date of Patent: December 7, 1993Assignee: Whitby Research, Inc.Inventor: Alan S. Horn
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Patent number: 5240922Abstract: The present invention relates to a method of enhancing implantation of an embryo within the uterus of a female mammal. The method comprises administering an amount of a PAF antagonist, effective to enhance implantation, to the mammal. The invention also relates to a method of increasing the level of PAF around an embryo in the uterus of a female mammal by administering an amount of a PAF antagonist sufficient to inhibit PAF catabolism. Desirably the PAF antagonist is administered together with PAF or a homologue or analogue thereof. The invention also provides compositions comprising a PAF antagonist together with PAF or a homologue or analogue thereof, and a process for preparing the same.Type: GrantFiled: December 27, 1991Date of Patent: August 31, 1993Assignee: Northern Sydney Area Health ServiceInventor: Christopher O'Neill
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Patent number: 5236952Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adensoylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuornal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.Type: GrantFiled: April 16, 1991Date of Patent: August 17, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose DaPrada, Gerhard Zurcher
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Patent number: 5223536Abstract: The 1,4-diaryl-1-cyclopropyl-4-substituted butane pesticides of the following formula are effective as insecticides and acaricides: ##STR1## in which X and Y are independently hydrogen, halogen, alkyl, alkoxy, cycloalkylalkoxy, alkylcarbonyl, alkoxycarbonyl, haloalkyl, haloalkoxy, alkylthio, haloalkylthio, alkylsulfinyl, alkylsulfonyl, trialkylamino, nitro, or cyano; or X and Y together are --OCH.sub.2 O-- or --OCF.sub.2 O-- bridging the 2-3 or 3-4 positions of the phenyl ring; Ar is 3-phenoxyphenyl, 4-fluoro-3-phenoxyphenyl, 6-phenoxypyridin-2-yl, or 2-methyl(1,1'-biphenyl)-3-yl;R is cyano, methyl, trifluoromethyl, alkenyl, alkynyl, or halogen.Type: GrantFiled: July 23, 1991Date of Patent: June 29, 1993Assignee: FMC CorporationInventors: Thomas G. Cullen, Scott McN. Sieburth, Gary A. Meier, John F. Engel
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Patent number: 5214041Abstract: A hair revitalizing tonic composition comprising (i) an amine oxide and (ii) a compound having a calmodulin inhibitory activity and/or a compound having an activity as a calcium antagonist.Type: GrantFiled: April 8, 1991Date of Patent: May 25, 1993Assignee: Shiseido Company Ltd.Inventors: Akihiro Ishino, Kiyoshi Miyazawa, Seishiro Fujii
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Patent number: 5202130Abstract: Treatment of an animal with calcium flux inhibitors results in a decrease in the number of epidermal Langerhans cells and a simultaneous decrease in the ability to respond to contact sensitizing agents. Also, topical application of calcium flux inhibitors will reduce inflammation in patients experiencing delayed-type hypersensitivity reaction or atopic eczema. Thus, calcium flux inhibitors represent a new class of therapeutic agents in the treatment of contact dermatitis and eczema.Type: GrantFiled: August 31, 1989Date of Patent: April 13, 1993Assignee: The Johns Hopkins UniversityInventors: Anhalt Grant, Diezel Wolfgang
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Patent number: 5180737Abstract: Compound of the formula (I):Q.sup.1 Q(CR.sup.2 .dbd.CR.sup.3).sub.a (CR.sup.4 .dbd.CF)(CR.sup.5 .dbd.CR.sup.6).sub.b C(.dbd.O)NHR.sup.1 (1)or a salt thereof, wherein Q.sup.1 is a phenyl ring or a fused bicyclic ring system containing 9 or 10 ring carbon atoms at least one ring being aromatic, or Q.sup.1 is a dihalovinyl group; Q is an alkyl chain containing 1 to 12 carbon atoms and optionally containing one or two oxygen atoms and/or an unsaturated group --CR.sup.7 .dbd.CR.sup.8 --, or --C.dbd.C--, wherein R.sup.7 and R.sup.8 are selected from hydrogen or halo; a is 0 or 1; b is 0 or 1; the sum of a and b is 0 or 1; R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different, and are independently selected from hydrogen, halo and C.sub.1-4 alkyl; R.sup.1 is selected from hydrogen and C.sub.1-6 hydrocarbyl optionally substituted by dioxalanyl, halo, cyano, trifluoromethyl, trifluoromethylthio or C.sub.1-6 alkoxy are disclosed which have pesticidal activity.Type: GrantFiled: June 8, 1989Date of Patent: January 19, 1993Assignee: Roussel UclafInventor: Robert J. Blade
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Patent number: 5132295Abstract: An alginate-based depot drug form for which the rate of release of the active substance in vitro can be adjusted very precisely is described.Type: GrantFiled: January 24, 1991Date of Patent: July 21, 1992Assignee: Knoll AGInventors: Evamarie Balz, Heinz Einig, Peter Dresen
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Patent number: 5132119Abstract: This invention pertains to a method for controlling hypertrophic wound healing disorders by administering calcium channel blockers to the wound site. Calcium channel blockers are found to regulate fibroblast biosynthesis and can therefore be used to therapeutically control diseases characterized by excessive fibroblast biosynthesis.Type: GrantFiled: December 17, 1990Date of Patent: July 21, 1992Assignee: Massachusetts Institute of TechnologyInventor: Raphael C. Lee
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Patent number: 5124354Abstract: A composition suitable for topical application to mammalian skin or hair for inducing, maintaining or increasing hair growth comprises:(i) a special protein tyrosine kinase inhibitor; and(ii) a cosmetically acceptable vehicle for the inhibitor.Type: GrantFiled: June 11, 1990Date of Patent: June 23, 1992Assignee: Chesebrough Pond's USA Co., Division of Conopco, Inc.Inventor: Martin R. Green
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Patent number: 5120721Abstract: An acaricidal composition comprising as active ingredients(A) either .alpha.-cyano-3-phenoxybenzyl 2,2,3,3-tetramethylcyclopropanecarboxylate or .alpha.-cyano-3-phenoxybenzyl N-(2-chloro-.alpha.,.alpha.,.alpha.-trifluor o-p-tolyl)-valinate, and(B) O,O,O',O'-tetraethyl S,S'-methylene bis(phosphorodithioate), is very effectively applicable as a composition for controlling acarine pests such as two-spotted spider mite (Tetranychus urticae Koch), carmine spider mite (Tetranychus cinnabarinus Boisduval), Kanazawa spider mite (Tetranychus Kansawai Kishida), citrus red mite (Panonychus citri McGregor), European red mite (Panonychus ulmi Koch), broad mite (Polyphagotarsonemus latus Banks), etc. in areas cultivated with fruit trees, tea-plant, vegetables, flowering plants, etc.Type: GrantFiled: September 28, 1990Date of Patent: June 9, 1992Assignee: Sumitomo Chemical Company, LimitedInventors: Teruichi Morimoto, Haruo Sasayama, Kiyoshi Kasamatsu
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Patent number: 5112382Abstract: Compounds of the formula ##STR1## wherein A is selected from the group consisting of (1) phenyl, (2) naphthyl, (3) phenyl substituted with one or more halo, cyano, (C.sub.1 -C.sub.4) alkyl, nitro, (C.sub.1 -C.sub.4)haloalkyl, and (C.sub.1 -C.sub.4)thioalkyl, (4) naphthyl substituted with one or more halo, cyano, (C.sub.1 -C.sub.4)alkyl,nitro,(C.sub.1 -C.sub.4), and (C.sub.1 -C.sub.4) thioalkyl, (5) thiophene, (6) furan, (7) thiophene substituted with one or more substituents selected from halo and nitro, and (8) furan substituted with one or more substituents selected from halo and nitro;R disclose as microbicidally and fungicidally active.Type: GrantFiled: May 24, 1990Date of Patent: May 12, 1992Assignee: Rohm and Haas CompanyInventor: Adam C. Hsu
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Patent number: 5089502Abstract: A method is provided for inhibiting onset of or treating anxiety by administering a calcium channel blocker such as diltiazem or nifedipine, over a prolonged period of treatment.Type: GrantFiled: August 9, 1990Date of Patent: February 18, 1992Assignee: E. R. Squibb & Sons, Inc.Inventors: Abraham Sudilovsky, Zola P. Horovitz
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Patent number: 5077294Abstract: Products contain verapamil or gallopamil and prazosin, in each case in depot form, as a combination preparation for simultaneous use in the therapy of high blood pressure.Type: GrantFiled: April 13, 1990Date of Patent: December 31, 1991Assignee: BASF AktiengesellschaftInventor: Christine Tetzner
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Patent number: 5057304Abstract: Antitumor compositions and methods in which a cancerostatic agent and an effective amount of (+)-verapamil, (+)-gallopamil, (+)-devapamil and/or (+)-emopamil which reinforce the antitumor action of the cancerostatic agent are administered to a patient either together or in sequence.Type: GrantFiled: January 3, 1989Date of Patent: October 15, 1991Assignee: BASF AktiengesellschaftInventors: Rolf Kretzschmar, Erich Schlick, Michel Eichelbaum
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Patent number: 5049583Abstract: Noremopamil and its preparation are described. The substance is suitable for the treatment of disorders.Type: GrantFiled: February 17, 1989Date of Patent: September 17, 1991Assignee: BASF AktiengesellschaftInventors: Hans P. Hofmann, Werner Seitz, Hans-Joerg Treiber
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Patent number: 5047410Abstract: New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## , wherein the substituents are defined hereinbelow, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.Type: GrantFiled: July 12, 1989Date of Patent: September 10, 1991Assignee: Istituto de Angeli S.p.A.Inventors: Arturo Donetti, Marco Turconi, Massimo Nicola, Rosamaria Micheletti
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Patent number: 5047426Abstract: The invention provides fungicidal compositions which comprise a carrier and, as active ingredient, a compound of the general formula ##STR1##Type: GrantFiled: August 23, 1989Date of Patent: September 10, 1991Assignee: Shell Internationale Research Maatschappij B.V.Inventor: Paul H. Briner
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Patent number: 5030656Abstract: A method of treating injuries in a patient associated with spinal cord trauma is disclosed. The method comprises administering to the patient a therapeutically effective amount of (S)-emopamil or a physiologically acceptable salt thereof.Type: GrantFiled: March 30, 1990Date of Patent: July 9, 1991Assignee: BASF K&F CorporationInventors: Robert A. O'Brien, Steven K. Salzman
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Patent number: 5001154Abstract: This invention provides a fervescence composition containing 15-keto-PHEs separated from any substantial activity such as decrease of blood pressure.Type: GrantFiled: November 22, 1989Date of Patent: March 19, 1991Assignee: K.K. Ueno Seiyaku Oyo KenkyujoInventors: Ryuzo Ueno, Ryuji Ueno, Tomio Oda
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Patent number: 4981871Abstract: Elevated intraocular pressure in a mammalian eye is lowered by administering to the eye an amount of a Class I calcium channel blocking agent effective to lower the elevated intraocular pressure. A preferred calcium channel blocking agent is verapamil and the preferred mode of administration is topical directly to the eye, e.g., with drops.Type: GrantFiled: May 15, 1987Date of Patent: January 1, 1991Inventor: Mark B. Abelson
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Patent number: 4968717Abstract: Compounds of the formula ##STR1## where R.sup.1 to R.sup.7, m, n and p have the meanings stated in the description, and certain derivatives which are p-substituted in the left-hand phenyl ring, are useful for the treatment of disorders.Type: GrantFiled: May 12, 1989Date of Patent: November 6, 1990Assignee: BASF AktiengesellschaftInventors: Liliane Unger, Manfred Raschack, Verena Baldinger, Ferdinand Dengel, Oskar Ehrmann, Hans J. Treiber, Werner Seitz
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Patent number: 4954523Abstract: A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower aralalkyl, --CH2--NHSO3--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.Type: GrantFiled: June 9, 1989Date of Patent: September 4, 1990Assignee: Eisai Co., Ltd.Inventors: Youji Yamagishi, Kozo Akasaka, Takeshi Suzuki, Mitsuaki Miyamoto, Kouji Nakamoto, Kazuo Okano, Shinya Abe, Hironori Ikuta, Kenji Hayashi, Hiroyuki Yoshimura, Tohru Fujimori, Koukichi Harada, Isao Yamatsu
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Patent number: 4935445Abstract: Improvement in method for treating tumors sensitive to treatment with anti-tumor agents employing Norverapamil.Type: GrantFiled: March 28, 1988Date of Patent: June 19, 1990Inventor: Stephen Merry
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Patent number: 4933367Abstract: This invention relates to carboxylic acid derivatives and their use thereof. The compounds are useful in treatment of various diseases such as diabetes, prediabetic conditions, adipositas ailments or atherosclerosis.Type: GrantFiled: March 12, 1987Date of Patent: June 12, 1990Assignee: Boehringer Mannheim GmbHInventors: Hans P. Wolff, Ernst-Christian Witte, Hans-Frieder Kuhnle
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Patent number: 4925837Abstract: Pharmaceutical compositions containing, by way of active substance, a combination of an alpha-blocker and a calcium antagonist. The composition is useful in treating cardiovascular disorders, especially hypertension.Type: GrantFiled: October 13, 1987Date of Patent: May 15, 1990Assignee: SynthelaboInventors: Icilio Cavero, Jean-Louis Cazor, Peter Hicks, Salomon Langer
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Patent number: 4925672Abstract: Combinations of calcium antagonists and lipid-lowering agents are suitable for controlling diseases.Type: GrantFiled: March 6, 1989Date of Patent: May 15, 1990Assignee: Knoll AGInventors: Dorothee Gremm, Ingetraud Perstel
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Patent number: 4921872Abstract: A method of combating acarids which comprises applying to such acarids or to an acarid habitat an acaricidally effective amount of an azomethine of 2,3-diaminomaleic acid nitrile of the formula ##STR1## in which X represents halogen, halogenoalkyl or CN and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 can be identical or different and represent hydrogen, optionally substituted alkyl, optionally substituted alkoxy, halogen, CN, NO.sub.2, optionally substituted dialkylamino, alkoxycarbonyl, optionally substituted alkylthio, optionally substituted alkylthionyl, optionally substituted alkylsulphonyl, OH, SH or NH.sub.2. The compounds other than the 2-chloro-and 2,6-dichloro-toluylideneamino-compounds are new.Type: GrantFiled: January 27, 1988Date of Patent: May 1, 1990Assignee: Bayer AktiengesellschaftInventors: Holger Heidenreich, Benedikt Becker
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Patent number: 4908386Abstract: The present invention provides compounds of general formula (I) ##STR1## wherein Ar represents an unsubstituted or substituted phenyl gorup;R.sup.1 and R.sup.2 each represents a hydrogen atom or a C.sub.1-3 alkyl group;X represents a bond or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene chain;Y represents a bond or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain;Q represents a substituted phenyl or pyridyl ring;and physiologically acceptable salts and solvates thereof useful as stimulants of .sub.2 -adrenoreceptors and particularly in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.Type: GrantFiled: December 20, 1988Date of Patent: March 13, 1990Assignee: Glaxo Group LimitedInventors: Harry Finch, Lawrence H. C. Lunts, Alan Naylor, Ian F. Skidmore, Ian B. Campbell, David Middlemiss, Charles Willbe
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Patent number: 4897419Abstract: A method for combating arachnida which comprises applying to arachnida and/or to a habitat thereof an effective pest combating amount of at least one derivative of a 2,3-diaminomaleonitrile of the formula ##STR1## in which X represents hydrogen, halogen, halogenoalkyl or CN, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined or different and represent hydrogen, alkyl, alkoxy, halogen, CN, NO.sub.2, dialkylamino, alkoxycarbonyl, alkylthio, alkylthionyl, alkylsulphonyl, OH, SH or NH.sub.2, wherein R.sub.1 and R.sub.b together represent the radical (II) ##STR2## in which Y represents hydrogen, halogen, halogenoalkyl or CN, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are identical or different and represent hydrogen, alkyl, alkoxy, halogen, CN, NO.sub.2, dialkylamino, alkoxycarbonyl, alkylthio, alkylthionyl, alkylsulphonyl, OH, SH or NH.sub.2, and in which R.sub.c and R.sub.d together represent a chemical bond,or R.sub.a and R.sub.b together represent the radical (II), in which Y, R.sup.5, R.sup.6, R.sup.7 and R.sup.Type: GrantFiled: June 27, 1988Date of Patent: January 30, 1990Assignee: Bayer AktiengesellschaftInventors: Holger Heidenreich, Benedikt Becker