Patents Examined by Dale A. Bjorkman
  • Patent number: 4794187
    Abstract: 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: Grant
    Filed: January 5, 1987
    Date of Patent: December 27, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventor: Hartmut Glossmann
  • Patent number: 4785111
    Abstract: 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: Grant
    Filed: March 10, 1986
    Date of Patent: November 15, 1988
    Assignee: Mitsubishi Corporation
    Inventor: Fumio Toda
  • Patent number: 4780538
    Abstract: 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: Grant
    Filed: February 12, 1986
    Date of Patent: October 25, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Steven M. Pitzenberger, Barry M. Trost
  • Patent number: 4777256
    Abstract: 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: Grant
    Filed: January 6, 1986
    Date of Patent: October 11, 1988
    Assignee: Daicel Chemical Industries Ltd.
    Inventors: Yoichiro Ueda, Kazuhisa Masamoto, Yukihisa Goto, Yoshiyuki Hirako, Hiroshi Yagihara, Yasuo Morishima, Hirokazu Osabe
  • Patent number: 4775763
    Abstract: 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: Grant
    Filed: March 27, 1985
    Date of Patent: October 4, 1988
    Assignee: Imperial Chemical Industries
    Inventors: Raymond F. Dalton, Raymond Price, Peter M. Quan, David Stewart
  • Patent number: 4772596
    Abstract: 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: Grant
    Filed: October 5, 1987
    Date of Patent: September 20, 1988
    Assignees: Sankyo Company Limited, Ube Industries Limited
    Inventors: Hiroyuki Koike, Hiroshi Nishino, Masafumi Yoshimoto
  • Patent number: 4772611
    Abstract: 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: Grant
    Filed: April 28, 1987
    Date of Patent: September 20, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Jurgen Stoltefuss, Fred R. Heiker, Martin Bechem, Rainer Gross, Michael Kayser, Matthias Schramm, Gunter Thomas
  • Patent number: 4772713
    Abstract: 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: Grant
    Filed: May 21, 1987
    Date of Patent: September 20, 1988
    Assignee: Nepera, Inc.
    Inventor: Laurence J. Nummy
  • Patent number: 4772621
    Abstract: 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: Grant
    Filed: August 19, 1987
    Date of Patent: September 20, 1988
    Assignee: Recordati S.A., Chemical and Pharmaceutical Company
    Inventors: Dante Nardi, Amedeo Leonardi, Gabriele Graziani, Giorgio Bianchi
  • Patent number: 4772612
    Abstract: 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: Grant
    Filed: June 3, 1986
    Date of Patent: September 20, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Siegfried Goldmann, Jurgen Stoltefuss, Gerhard Franckowiak, Rainer Gross, Matthias Schramm, Gunter Thomas
  • Patent number: 4772615
    Abstract: 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: Grant
    Filed: October 14, 1987
    Date of Patent: September 20, 1988
    Assignee: Warner-Lambert Company
    Inventor: Michael R. Pavia
  • Patent number: 4771059
    Abstract: 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: Grant
    Filed: August 29, 1985
    Date of Patent: September 13, 1988
    Assignee: University of Florida
    Inventor: Nicholas S. Bodor
  • Patent number: 4769465
    Abstract: 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 and 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 and C.
    Type: Grant
    Filed: May 14, 1986
    Date of Patent: September 6, 1988
    Assignee: LEK, tovarna farmacevtskih in kemicnih izdelkov, n.sol.o.
    Inventors: Ljubo Antoncic, Iztok Jazbec, Darko Kocjan, Ivana Krivec
  • Patent number: 4769374
    Abstract: 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: Grant
    Filed: September 23, 1985
    Date of Patent: September 6, 1988
    Assignee: Poli Industria Chimica S.p.A.
    Inventor: Giangiacomo Massaroli
  • Patent number: 4769464
    Abstract: 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: Grant
    Filed: December 17, 1984
    Date of Patent: September 6, 1988
    Assignee: Chemie Linz Gesellschaft m.b.H.
    Inventor: Alexander Sajtos
  • Patent number: 4766213
    Abstract: 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: Grant
    Filed: January 16, 1987
    Date of Patent: August 23, 1988
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Horst Juraszyk, Rolf Gericke, Inge Lues, Rolf Bergmann, Claus J. Schmitges
  • Patent number: 4766136
    Abstract: 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: Grant
    Filed: March 3, 1987
    Date of Patent: August 23, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Christa Fest, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
  • Patent number: 4764522
    Abstract: 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: Grant
    Filed: August 16, 1985
    Date of Patent: August 16, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rene Imhof, Emilio Kyburz
  • Patent number: 4764516
    Abstract: 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: Grant
    Filed: December 6, 1985
    Date of Patent: August 16, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gerhard Franckowiak, Rolf Grosser, Gunter Thomas, Matthias Schramm, Rainer Gross
  • Patent number: 4762928
    Abstract: 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 to 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: Grant
    Filed: December 18, 1986
    Date of Patent: August 9, 1988
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Yasuhiro Tsujii, Tatsuo Isogai, Takao Awazu, Hisayoshi Jyonishi, Tokiya Kimura