Patents Examined by Dale A. Bjorkman
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Patent number: 4794187Abstract: A radioactively labelled dihydropyridine compound of the formula ##STR1## in which R.sup.1 represents a phenyl radical which is optionally substituted once or twice, identically or differently, by halogen, nitro, trifluoromethyl or difluoromethoxy, or R.sup.1 represents benzoxadiazolyl,R.sup.2 represents a straight-chain or branched alkyl which has up to 8 carbon atoms and which is optionally substituted by cyano, phenyl, halogen, N-benzyl-N-methylamino, N-phenylpiperazino or by alkoxy having up to 4 carbon atoms, andR.sup.3 and R.sup.4 are identical or different and each represents a cyano or represents a straight-chain or branched alkyl which has up to 6 carbon atoms, is optionally interrupted in the chain by one oxygen atom and is optionally substituted by hydroxyl or amino. The compounds are useful in investigating the pharmacokinetics and pharmacodynamics of dihydropyridines, especially for determining metabolism, modes of elimination and organ-specific action.Type: GrantFiled: January 5, 1987Date of Patent: December 27, 1988Assignee: Bayer AktiengesellschaftInventor: Hartmut Glossmann
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Patent number: 4785111Abstract: This invention provides novel N-cyclohexyl-polycarboxamide compounds having inclusion power for a variety of compounds, the N-cyclohexyl-polycarboxamide compound being of the general formula ##STR1## where R is a benzene ring, an ethylidene group, a benzylidene group, a 1,2-cyclohexylene group, a 1,2-cyclohexenylene-4 group, or a 2,3-, 2,5- or 2,6-pyridinediyl group, and n is equal to 2, 3 or 4 when R is a benzene ring, and equal to 2 when R is one of the aforesaid groups excluding a benzene ring. These compounds exhibit the host function of taking up a variety of compounds as guest compounds to form inclusion complexes, and can be utilized for the separation and purification thereof.Type: GrantFiled: March 10, 1986Date of Patent: November 15, 1988Assignee: Mitsubishi CorporationInventor: Fumio Toda
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Patent number: 4780538Abstract: A process for the preparation of 1,4-dihydropyridine compounds, especially N-substituted 1,4-dihydropyridine compounds, is disclosed. The compounds are useful as cardiovascular agents and also as starting materials for the preparation of certain cyclized compounds which have properties as calcium entry blockers.Type: GrantFiled: February 12, 1986Date of Patent: October 25, 1988Assignee: Merck & Co., Inc.Inventors: Steven M. Pitzenberger, Barry M. Trost
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Patent number: 4777256Abstract: Novel 5-halopyridine-3-carboxamide compounds having the general formula (I) ##STR1## or salts thereof wherein R is hydrogen atom or a group of --(CH.sub.2).sub.n --R.sub.1 wherein n is an integer from 1 to 4 and R.sub.1 is hydrogen atom, hydroxy group, lower alkoxy group, mercapto group, lower alkylthio group, amino group, di-lower alkylamino group, C.sub.1-11 alkyl group, lower alkenyl group, lower alkynyl group, cycloalkyl group, 5- or 6-membered heterocyclic group or aryl group which may be substituted by one or two substituents of halogen, lower alkyl or lower alkoxy;R.sub.2 and R.sub.3 are, the same of different, hydrogen atom, halogen atom, cyano group, nitro group, amino group, lower akyl group, halogenated lower alkyl group, hydroxy group, lower alkoxy group, aryloxy group, carboxy group or lower alkoxycarbonyl group;X is halogen atom; which compounds possess growth inhibitory activities and also anti-inflammatory activity.Type: GrantFiled: January 6, 1986Date of Patent: October 11, 1988Assignee: Daicel Chemical Industries Ltd.Inventors: Yoichiro Ueda, Kazuhisa Masamoto, Yukihisa Goto, Yoshiyuki Hirako, Hiroshi Yagihara, Yasuo Morishima, Hirokazu Osabe
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Patent number: 4775763Abstract: Metal values are extracted from aqueous solutions of metal salts containing halide or pseudo halide ions by pyridine derivatives containing the substituent --(COX).sub.A where X is the group --OR.sub.1 or --NR.sub.2 R.sub.3 and n is 1, 2 or 3. R.sub.1 is a hydrocarbyl group containing from 5 to 36 carbon atoms and R.sub.2 and R.sub.3 are hydrogen or a hydrocarbyl group wherein R.sub.2 and R.sub.3 together contain from 5 to 36 carbon atoms. The process is especially useful for the recovery of metals from leach solutions derived from sulphur-containing ores such as chalcopyrite.Type: GrantFiled: March 27, 1985Date of Patent: October 4, 1988Assignee: Imperial Chemical IndustriesInventors: Raymond F. Dalton, Raymond Price, Peter M. Quan, David Stewart
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Patent number: 4772596Abstract: 2-(Amino or methyl)-6-(methyl or amino)-4-(substituted phenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid esters have a specific class of heterocyclic groups as thealcohol moiety. These compounds have a variety of valuable activities, including antihypertensive and Ca.sup.++ -blocking activities, leading to their use for the treatment of circulatory and coronary disorders. They may be prepared by condensation of appropriate substituted benzylideneacetoacetic acid esters with appropriate amidinoacetic acid esters.Type: GrantFiled: October 5, 1987Date of Patent: September 20, 1988Assignees: Sankyo Company Limited, Ube Industries LimitedInventors: Hiroyuki Koike, Hiroshi Nishino, Masafumi Yoshimoto
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Patent number: 4772611Abstract: Novel cardioactive compounds of the formula ##STR1## in which R.sup.1 is alkyl, aryl or heterocyclic, preferably substituted phenyl,R.sup.2 is alkyl, preferably methyl,R.sup.3 is hydrogen, halogen, acyloxy or alkyl, preferably hydrogen, andR.sup.4 is phenyl, carbalkoxy or together with R.sup.3 forms a ring, preferably carbalkoxy,are produced by reducing the corresponding nitro compounds.Type: GrantFiled: April 28, 1987Date of Patent: September 20, 1988Assignee: Bayer AktiengesellschaftInventors: Jurgen Stoltefuss, Fred R. Heiker, Martin Bechem, Rainer Gross, Michael Kayser, Matthias Schramm, Gunter Thomas
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Patent number: 4772713Abstract: Disclosed are compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 independently are H or C.sub.1-8 -alkyl or together are C.sub.2-7 -alkylene forming a ring with the connecting N-atom; X is CN, halo, C.sub.6-10 -arylsulfonyl, C.sub.6-10 -arylsulfinyloxy, C.sub.6-10 -aryloxy, C.sub.6-10 -arylthio or C.sub.1-8 -alkylsulfonyloxy or nitro, and Y is the anion of an acid having a pK.sub.a of about 3 or less.These compounds are intermediates in the preparation of 4-substituted pyridines.Type: GrantFiled: May 21, 1987Date of Patent: September 20, 1988Assignee: Nepera, Inc.Inventor: Laurence J. Nummy
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Patent number: 4772621Abstract: Novel antihypertensive and coronary dilating asymmetric diesters of 1,4-dihydro-2,6-dimethylpyridine-3,5-dicarboxylic acid (or the stereoisomers or pharmaceutically acceptable acid addition salts thereof) have the general formula (I): ##STR1## wherein Ph is phenyl, Ar is 2-nitrophenyl, 3-nitrophenyl, 2,3-dichlorophenyl or benzofurazan-4-yl, A is a straight or branched chain alkylene radical having from 2 to 6 carbon atoms, R is a straight or branched chain alkyl radical having from 1 to 6 carbon atoms, optionally mono-substituted by an alkoxy substituent having from 1 to 6 carbon atoms, R.sub.1 is hydrogen, hydroxy or an alkyl radical having from 1 to 4 carbon atoms, and R.sub.2 is hydrogen or methyl. The subject diesters are facilely prepared from the aldehydes ArCHO and esters of acetoacetic and 3-aminocrotonic acids.Type: GrantFiled: August 19, 1987Date of Patent: September 20, 1988Assignee: Recordati S.A., Chemical and Pharmaceutical CompanyInventors: Dante Nardi, Amedeo Leonardi, Gabriele Graziani, Giorgio Bianchi
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Patent number: 4772612Abstract: Novel circulation active dihydropyridines of the formula ##STR1## in which X is CO, SO.sub.2 or CONH,R.sup.4 is H, OH, alkyl, halogen, acyloxy, alkoxyalkoxy, aralkyloxy, or together with R.sup.5 forms a heterocyclic ring, andthe other radicals are conventional in the dihydropyridine art,and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 3, 1986Date of Patent: September 20, 1988Assignee: Bayer AktiengesellschaftInventors: Siegfried Goldmann, Jurgen Stoltefuss, Gerhard Franckowiak, Rainer Gross, Matthias Schramm, Gunter Thomas
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Patent number: 4772615Abstract: Analogs of nipecotic acid are the novel compounds of the present invention. The analogs are GABA uptake inhibitors for use to treat epilepsy and, thus, the invention is also pharmaceutical compositions and methods of use therefor.Type: GrantFiled: October 14, 1987Date of Patent: September 20, 1988Assignee: Warner-Lambert CompanyInventor: Michael R. Pavia
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Patent number: 4771059Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are compounds of the formula ##STR1## and the non-toxic pharmaceutically acceptable salts thereof, wherein D is the residue of a centrally acting primary, secondary or tertiary amine and ##STR2## is an unsubstituted or substituted dihydropyridyl, dihydroquinolyl or dihydroisoquinolyl radical. The corresponding ionic pyridinium, quinolinium and isoquinolinium salts ##STR3## X.sup.-, wherein X.sup.- is the anion of a non-toxic pharmaceutically acceptable acid, are also disclosed.Type: GrantFiled: August 29, 1985Date of Patent: September 13, 1988Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 4769465Abstract: A new, technologically easily feasible process for the preparation of 2-(N-benzyl-N-methylamino)ethyl methyl 2,6-dimethyl-4(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, comprising a partrial hydrolysis of dimethyl 2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate in an inert organic solvent at a temperature between room temperature and the reflux temperature of the reaction mixture with an aqueous solution of alkali hydroxide and the reaction of the obtained 3-methoxycarbonyl-2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-5-car boxylic acid either with N-(2-hydroxyethyl)-N-benzyl-methylamine in the presence or absence of an organic solvent in the presence of N,N'-dicyclohexylcarbodiimide at a temperature of between 25.degree. and 120.degree. C. or with N-(2-haloethyl)-N-benzyl-methylamine in the presence of an inert organic solvent and of a proton acceptor at a temperature of between 25.degree. and 140.degree. C.Type: GrantFiled: May 14, 1986Date of Patent: September 6, 1988Assignee: LEK, tovarna farmacevtskih in kemicnih izdelkov, n.sol.o.Inventors: Ljubo Antoncic, Iztok Jazbec, Darko Kocjan, Ivana Krivec
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Patent number: 4769374Abstract: 1,4-Dihydropiridine derivatives having the formula ##STR1## wherein R is methyl, ethyl or isopropyl, are endowed with a hypotensive, vasodilator and Ca.sup.++ -antagonistic activity.Type: GrantFiled: September 23, 1985Date of Patent: September 6, 1988Assignee: Poli Industria Chimica S.p.A.Inventor: Giangiacomo Massaroli
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Patent number: 4769464Abstract: The invention relates to a process for the preparation of monocarbonyl or biscarbonyl compounds by reacting organic carbon compounds having one or more olefinic or aromatic double bonds in the molecule with the equivalent amount of ozone and by subsequently catalytically hydrogenating the ozonization products, wherein the peroxide-containing ozonization solution is fed continuously into a suspension of the hydrogenation catalyst in a lower aliphatic alcohol, while a peroxide content of not more than 0.1 mole/l is maintained, and the ozonization products are continuously cleaved reductively to give the corresponding carbonyl compounds.Type: GrantFiled: December 17, 1984Date of Patent: September 6, 1988Assignee: Chemie Linz Gesellschaft m.b.H.Inventor: Alexander Sajtos
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Patent number: 4766213Abstract: Compounds of the formula ##STR1## are disclosed wherein the variables are herein described. These compounds are intermediates to compounds which influence the influx of calcium into the cell.Type: GrantFiled: January 16, 1987Date of Patent: August 23, 1988Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Horst Juraszyk, Rolf Gericke, Inge Lues, Rolf Bergmann, Claus J. Schmitges
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Patent number: 4766136Abstract: Novel fungicidally active phenylsulphonyl-pyridine aldoximes of the formula ##STR1## in which R.sup.1 represents halogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, nitro, alkoxycarbonyl or alkylcarbonylamino,R.sup.2 represents halogen or alkyl,n represents an integer 0, 1, 2, 3, 4 or 5, andm represents an integer 0, 1, 2, 3 or 4.Type: GrantFiled: March 3, 1987Date of Patent: August 23, 1988Assignee: Bayer AktiengesellschaftInventors: Christa Fest, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
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Patent number: 4764522Abstract: Compounds of the formula ##STR1## wherein R is an aromatic, 5- or 6-membered heterocyclic residue, as described herein, and their pharmaceutically usable acid addition salts are described. These compounds have interesting monoamine oxidase inhibiting properties with low toxicity and can accordingly be used for the treatment of depressive states and parkinsonism.Type: GrantFiled: August 16, 1985Date of Patent: August 16, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Rene Imhof, Emilio Kyburz
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Patent number: 4764516Abstract: Pure enantiomers of 5-nitrodihydropyridine of the formula ##STR1## are mixed, wherein one of the enantiomers has a high vasodilative action and a low negative inotropic activity on heart muscle, the other enantiomer has a low vasoconstrictive action and a high positive inotropic activity on heart muscle, the mixture being high in vasodilative activity and in positive inotropic activity on heart muscle.Type: GrantFiled: December 6, 1985Date of Patent: August 16, 1988Assignee: Bayer AktiengesellschaftInventors: Gerhard Franckowiak, Rolf Grosser, Gunter Thomas, Matthias Schramm, Rainer Gross
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Patent number: 4762928Abstract: A novel amino-trifluoromethylpyridine compound selected from the group consisting of 3-amino-5-trifluoromethylpyridine, 2-amino-4-trifluoromethylpyridine, and 2-amino-4,6-bis(trifluoromethyl)pyridine, and, a process for preparing the same by reacting a halogeno-trifluoromethylpyridine compound with ammonia at a temperature of 50.degree. to 200.degree. C. The compound is useful as an intermediate from which a compound effective in controlling various harmful organisms or an effective component compound of medicines can be easily derived.Type: GrantFiled: December 18, 1986Date of Patent: August 9, 1988Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Yasuhiro Tsujii, Tatsuo Isogai, Takao Awazu, Hisayoshi Jyonishi, Tokiya Kimura