The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 546/237)
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Patent number: 5434171Abstract: This invention relates to a process for preparing certain 3,4,4-trisubstituted-piperidinyl-N-alkylcarboxylates, intermediates, and congeners. Finally, the invention provides new 3,4,4-trisubstituted-piperidinyl-N-alkylcarboxylates with formulations and methods for using the compounds.Type: GrantFiled: December 8, 1993Date of Patent: July 18, 1995Assignee: Eli Lilly and CompanyInventors: Scott A. Frank, Douglas E. Prather, Jeffrey A. Ward, John A. Werner
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Patent number: 5422356Abstract: This invention provides trans-3,4 1-substituted-3-substituted-4-methyl-4-(3-substituted phenyl)piperidines as opioid antagonists capable of blocking the mu or kappa receptors in the brain.Type: GrantFiled: June 1, 1994Date of Patent: June 6, 1995Assignee: Eli Lilly and CompanyInventors: Dennis M. Zimmerman, Charles H. Mitch
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Patent number: 5395841Abstract: 4-Benzylpiperidine derivatives of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein X is hydrogen or fluorine and R is hydrogen, or a group selected from p-fluorobenzoyl, .alpha.-hydroxy-p-fluorobenzyl, p-fluorophenoxy, bis(p-fluorophenyl)methyl and 8-azaspiro[4,5]decane-7,9-dione-8-yl-methyl, with the proviso that X and R may not be simultaneously hydrogen and p-fluorobenzoyl respectively.Such compounds are useful as sigma-receptor ligands.Type: GrantFiled: June 4, 1993Date of Patent: March 7, 1995Assignee: Ferrer Internacional, S.A.Inventors: Rafael Foguet, Jordi Bolos, Aurelio Sacristan, Jose A. Ortiz
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Patent number: 5387593Abstract: Novel piperazinyl- and piperidinyl-cyclohexanols of the following formula are useful as anxiolytic agents and have other psychotropic properties ##STR1##Type: GrantFiled: February 17, 1994Date of Patent: February 7, 1995Assignee: Briston-Myers SquibbInventors: Ronald J. Mattson, John D. Catt
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Patent number: 5319087Abstract: This invention provides trans-3,4 1-substituted-3-substituted-4-methyl-4-(3-substituted phenyl)piperidines as opioid antagonists capable of blocking the mu or kappa receptors in the brain.Type: GrantFiled: September 3, 1992Date of Patent: June 7, 1994Assignee: Eli Lilly and CompanyInventors: Dennis M. Zimmerman, Charles H. Mitch
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Patent number: 5317024Abstract: Novel unsaturated ether derivatives of alkyl piperidine and pyrrolidine compounds, pharmaceutical compositions containing them, methods of preparation and methods of using these compounds as antipsychotic agents are disclosed.Type: GrantFiled: August 3, 1993Date of Patent: May 31, 1994Assignee: DuPont Merck Pharmaceutical Co.Inventors: Gary A. Cain, Thomas E. Christos, Sang W. Tam
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Patent number: 5296485Abstract: Substituted N-phenylpiperidines I ##STR1## (R.sup.1 =H, NO.sub.2, CN, halogen, C.sub.1 -C.sub.4 -alkyl, CF.sub.3, OCF.sub.3, OH, CH.sub.2 OH, COOH, CHO, NH--CHO, NH.sub.2, CO--NH.sub.2, 5-tetrazinyl, R.sup.4 --O--, R.sup.4 --O--CH.sub.2 --, R.sup.4 O--CO--, R.sup.4 --CO--, R.sup.4 --NH--CO, R.sup.4 --CO--NH--, R.sup.4 --SO.sub.2 --NH--;R.sup.2 =H, NO.sub.2, halogen, C.sub.1 -C.sub.4 -alkyl or R.sup.4 --O--; ##STR2## R.sup.4 =C.sub.1 -C.sub.4 -alkyl or phenyl which can carry one of the R.sup.2 radicals;R.sup.5, R.sup.6 =H or one of the R.sup.4 radicals; R.sup.7 =one of the R.sup.1 radicals;n=0 or 1; m=1 or 2; with the proviso that R.sup.3 is ##STR3## only when n is 1, and the optical isomers in the case of optical isomerism, and the physiologically tolerated acid addition salts, are suitable as drugs.Type: GrantFiled: March 11, 1992Date of Patent: March 22, 1994Assignee: BASF AktiengesellschaftInventors: Wilfried Lubisch, Sabine Schult, Berthold Behl, Michael Kirchengast
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Patent number: 5286733Abstract: The invention is related to compounds, being useful in treating psychosis, of the formula: ##STR1## wherein: R.sup.1 is hydrogen, lower-alkyl, phenyl-lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl-lower-alkyl, or hydroxy-C.sub.3 -C.sub.7 -monocycliccycloalkyl-lower-alkyl;R.sup.2 is lower-alkyl;R.sup.3 is hydrogen or lower-alkyl;R.sup.4 is lower-alkyl;n is an integer from zero to three; andR.sup.5 is hydroxy, lower-alkoxy, lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl, phenyl, or a 5-membered heterocycle selected from furanyl, thienyl and isoxazolyl;with the proviso that when n is zero, R.sup.5 is other than hydroxy or a pharmaceutically acceptable acid-addition salt thereof.Type: GrantFiled: November 20, 1992Date of Patent: February 15, 1994Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, John P. Mallamo, William F. Michne, Martha R. Heimann
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Patent number: 5252586Abstract: Novel unsaturated ether derivatives of alkyl piperidine and pyrrolidine compounds, pharmaceutical compositions containing them, methods of preparation and methods of using these compounds as antipsychotic agents are disclosed.Type: GrantFiled: September 28, 1990Date of Patent: October 12, 1993Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Gary A. Cain, Thomas E. Christos, Sang W. Tam
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Patent number: 5250735Abstract: Novel 2-(N-substituted-aminoalkyl)-5-(E)-alkylidene cyclopentanones, 2-(N-substituted-aminoalkyl)-5-(E)-arylalkylidene cyclopentanones, and derivatives thereof having the formula ##STR1## wherein x is methylene or ethylene; R.sub.1 is dimethylamino, diethylamino, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, anilino or substituted anilino; R.sub.2 is hydrogen, straight or branched alkyl of 1 to 9 carbon atoms, aryl or arylalkyl; R.sub.3 is hydrogen, straight or branched alkyl of 1 to 9 carbon atoms, aryl or arylalkyl; and R.sub.4 is hydrogen, methyl, ethyl, allyl, benzyl, substituted benzyl, cyclopentyl, substituted cyclopentyl, cyclopenten-1-yl, or substituted cyclopenten-1-yl; and wherein aryl is phenyl or phenyl substituted with one or more methoxyl, hydroxyl, methylenedioxy, chloro, bromo, fluoro, ethoxycarbonylmethoxy, benzoxy, alkyl group, or their combination, possess anti-inflammatory, analgesic and anticancer properties.Type: GrantFiled: April 3, 1992Date of Patent: October 5, 1993Assignee: University of PittsburghInventors: Lan K. Wong, Hai-Tao Chen, Zhi-Zhong Ji
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Patent number: 5231105Abstract: An ethylamine derivative of formula (I): ##STR1## wherein A represents a carbon atom or a nitrogen atom;B represents a substituted or unsubstituted aralkyl or aryl group;C represents hydrogen, alkyl, aralkyl, or aryl, each of which may optionally be substituted orC may optionally be bonded to A to form an alkylene bridge which is optionally substituted,Q represents a substituted or unsubstituted aryl group, said group optionally being substituted by hetero atom(s) or substituent(s) optionally containing hetero atom(s); andX represents an alkylene bridge having from 2 to 20 carbon atoms and is optionally substituted with groups which include hetero atoms with the non-hetero atom substituents optionally containing hetero atoms.Type: GrantFiled: May 22, 1989Date of Patent: July 27, 1993Assignee: Ajinomoto Co., Inc.Inventors: Masataka Shoji, Kozo Toyota, Chikahiko Eguchi, Ryota Yoshimoto, Yosikatsu Koyama, Hideki Domoto, Akira Kamimura
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Patent number: 5227490Abstract: Novel fibrinogen receptor antagonists of the formula ##STR1## are provided in which the claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating thrombus formation.Type: GrantFiled: February 21, 1992Date of Patent: July 13, 1993Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Wasyl Halczenko
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Patent number: 5192799Abstract: Amine represented by the following formula (1), or their acid addition salts or their quaternary ammonium salts. ##STR1## The amines of formula (1) or their pharmaceutically acceptable acid addition salts or quaternary ammonium salts are useful for the treatment and prevention of heart diseases of animals, particularly arrhythima, myocardial infarction, angina pectoris and heart failure and psychoneurological diseases.Type: GrantFiled: June 5, 1992Date of Patent: March 9, 1993Assignee: Mitsui Petrochemical Industries, Ltd.Inventors: Ikuo Tomino, Masaharu Ishiguro, Takumi Kitahara, Keiichi Yokoyama, Noriaki Kihara, Joji Kamiya, Kanji Yoshihara, Masaaki Ishii, Akira Mizuchi, Kazutoshi Horikomi, Akira Awaya, Takuo Nakano
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Patent number: 5158961Abstract: Novel piperidine compounds having the formula ##STR1## wherein the symbols have the same meaning as set forth in the specification, and salts thereof with a pharmaceutically acceptable acid, are disclosed.The novel compound are useful in the treatment of anoxia, migraine, ischemia and epilepsy.Type: GrantFiled: March 22, 1991Date of Patent: October 27, 1992Assignee: Novo Nordisk A/SInventors: Palle Jakobsen, Jorgen Drejer
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Patent number: 5144029Abstract: The present invention relates to compounds of formula: ##STR1## in which: R.sub.3 is hydrogen, 2-tetrahydropyranyl or benzyl;R.sub.1 and R.sub.2 are such that:either R.sub.1 represents a methoxy group in which case R.sub.2 is a group chosen from the following: hydroxyl; C.sub.1 -C.sub.4 alkyl; C.sub.2 -C.sub.8 alkyloxy; C.sub.5 -C.sub.7 cycloalkloxy; benzyloxy;or R.sub.2 represents a methoxy group in which case R.sub.1 is a group chosen from the following: hydroxyl; C.sub.2 -C.sub.8 alkyloxy; C.sub.2 -C.sub.8 alkyloxy substituted by a methoxy group; C.sub.1 -C.sub.4 trifluoroalkyloxy; C.sub.3 -C.sub.4 alkenyloxy; C.sub.5 -C.sub.7 cycloalkyloxy; benzyloxy; C.sub.1 -C.sub.4 alkylthio;n=2 or 3; andp=4, 5 or 6,as well as their addition salts with mineral or organic acids, said compounds and salts being useful as drugs.Type: GrantFiled: January 3, 1991Date of Patent: September 1, 1992Assignee: Delalande S.A.Inventors: Mona Ward, Pierre-Andre Ph. Settembre, Alain Renaud, Michel Langlois
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Patent number: 5118682Abstract: p-Hydroxy phenone derivatives of the general formula I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are identical or different and are methyl, chlorine, bromine and hydrogen, but R.sup.1, R.sup.2 and R.sup.3 are not all H,R.sup.4 and R.sup.5 are identical or different and are H, C.sub.1 -C.sub.4 -alkyl, or OR.sup.6, but R.sup.4 and R.sup.5 are not both H,X is a --CH.dbd.CH--, --CH.sub.2 CH.sub.2 or --CH.sub.2 -- bridge,Y is a straight-chain or branched, saturated or unsaturated C.sub.1 -C.sub.4 bridge, andZ is NR.sup.6 R.sup.7, where R.sup.6 and R.sup.7 are, independently of one another, hydrogen or C.sub.1-4 -alkyl, or Z is a 5- or 6-membered ring with a nitrogen atom in the 1 position and, where appropriate, additionally a second N atom or an O or S atom, the second N atom being substituted by R.sup.7, as well as the physiologically tolerated salts thereof,are used to prepare drugs antiarrhythmic of Vaughan-Williams class III.Type: GrantFiled: July 12, 1989Date of Patent: June 2, 1992Assignee: BASF AktiengesellschaftInventors: Wilfried Lubisch, Manfred Raschack, Gerda von Philipsborn
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Patent number: 5100902Abstract: Compounds of formula I ##STR1## in which m represents an integer from 0 to 5, n represents an integer from 1 to 2, p is equal to 0, 1 or 2,X, Y and Z, which may be identical or different, each represent a hydrogen atom, a halogen atom, a linear or branched alkyl radical, a trifluoromethyl radical, an alkoxy radical, an alkylthio radical or a hydroxyl radical, andR represents a 2-benzofuranyl or 2,3-dihydro-2-benzofuranyl radical (it being possible for each to be substituted on the benzene ring), a 2,3,6,7-tetrahydrobenzo[1,2-b:4,5-b']difuran-2-yl radical, a 4-oxo-4H-chromen-2-yl radical (optionally substituted on the benzene ring), a benzocyclobutenyl radical of formula A or an indanyl radical of formula B: ##STR2## (in which: R.sub.1 and R.sub.Type: GrantFiled: October 26, 1990Date of Patent: March 31, 1992Assignee: Adir et CompagnieInventors: Jean L. Peglion, Francis Colpaert
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Patent number: 5098915Abstract: Substituted N-benzylpiperidine amides, which have activity as Class III antiarrhythmic agents, acting by prolonging cardiac action potential repolarization. The invention further provides for compositions incorporating the compunds and methods of their use, as well as providing for pharmaceutically acceptable salts of the compounds.Type: GrantFiled: September 5, 1989Date of Patent: March 24, 1992Assignee: G. D. Searle & Co.Inventors: Bipinchandra N. Desai, Kerry W. Fowler, Alan E. Moormann
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Patent number: 5091393Abstract: The invention relates to a group of tertiary 2,5-dialkyl-3-phenylpiperidine derivatives, having opiate-antagonistic activity represented by general formula 4, ##STR1## wherein A.sub.1 is hydrogen, an optionally esterified hydroxyl group or mercapto group, a group NHA.sub.8 or --CONHA.sub.8, wherein A.sub.8 is hydrogen, alkyl having 1-6 C-atoms or alkylcarbonyl having 2-7 C-atoms;A.sub.2 is hydrogen or, when A.sub.1 is hydrogen, one of the other meanings of A.sub.1, orA.sub.1 and A.sub.2 together with the 2 carbon atoms of the benzene ring,constitute a heterocyclic group which consists of five or six ring atoms and which comprises a group --NH-- and optionally as a second hetero atom may comprise an oxygen atom, sulphur atom or nitrogen atom;A.sub.3 and A.sub.4 independently of each other are straight or branched alkyl or alkenyl having 1-6 C-atoms;A.sub.Type: GrantFiled: May 29, 1990Date of Patent: February 25, 1992Assignee: Duphar International Research B.V.Inventors: Jacobus A. Den Hartog, Ineke Van Wijngaarden, Martinus T. Tulp
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Patent number: 5053504Abstract: A process is disclosed for providing benzazepine intermediates of the formulae ##STR1## wherein R.sub.3, R.sub.4 and Y are as defined herein, which intermediates are useful in a process for the preparation of pharmaceutically useful benzazepine derivatives.Type: GrantFiled: November 29, 1989Date of Patent: October 1, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Wen-Sen Li, John K. Thottathil, Michael Murphy
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Patent number: 4971979Abstract: Substituted alkadienes of formula: ##STR1## in which R.sub.1 is hydroxy or acetoxy, R.sub.2 is hydrogen, carboxy, alkoxycarbonyl, phenyl or benzoyl, andR.sub.3 is alkylthio or alkoxy and R.sub.4 is naphthoyl or optionally substituted benzoyl,or R.sub.3 is alkoxycarbonyl, cycloalkyloxycarbonyl or cyano and R.sub.4 is alkyl, naphthyl, optionally substituted phenyl, alkylthio, naphthylmethanethio, optionally substituted benzylthio, optionally substituted phenylthio, naphthylthio, phenethylthio or allylthio,or R.sub.3 and R.sub.4 form, with the carbon atom to which they are attached, a ring-system of formula: ##STR2## in which R.sub.5 is hydrogen or alkoxy and X is methylene or S inhibit 5-lipoxygenase and are useful, for example, as anti-inflammatories.Type: GrantFiled: July 19, 1989Date of Patent: November 20, 1990Assignee: Rhone-Poulenc SanteInventors: Jean-Luc Malleron, Gerard Ponsinet, Gerard Roussel
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Patent number: 4966914Abstract: In accordance with the present invention, disclosed herein are compounds of the formula ##STR1## wherein R is hydrogen, straight or branched loweralkyl, cycloalkyl, amino, loweralkoxy or acylamino, and R.sub.1 is straight or branched loweralkyl, amino, cyclohexyl phenyl or phenyl substituted with loweralkyl, loweralkoxy or halo, benzyl, morpholino, piperidino, tetrahydrofuranyl, dihydrofuranyl, furanyl, tetrahydropyranyl, dioxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolidinyl, tetrahydrooxazolyl, and dihydrooxazolyl, R.sub.2 is hydrogen or --COR.sub.3 wherein R.sub.3 is straight or branched loweralkyl, provided, however, when R.sub.1 is loweralkyl or cyclohexyl, R.sub.2 is not hydrogen, and pharmaceutically acceptable salts thereof. The compounds are useful in the treatment of glaucoma.Type: GrantFiled: December 15, 1988Date of Patent: October 30, 1990Assignee: E. I. Du Pont de Nemours and CompanyInventors: Ghanshyam Patil, William L. Matier, Khuong H. X. Mai
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Patent number: 4950602Abstract: The present invention relates to inhibitors of lactate dehydrogenase that can cross the blood brain barrier and there is described herein the preparation of several analogues of nicotinamide-adenine-dinucleotide (NAD.sup.+) pyruvate adduct, of which 3(-4-(reduced 3-pyridine aldehyde-adenine dinucleotide))-pyruvate (RAP) and similar compounds appear to have a very high affinity for lactate dehydrogenase; one of which (RAP) was shown to strongly inhibit lactate production in rat brain extracts.Type: GrantFiled: February 20, 1987Date of Patent: August 21, 1990Assignee: Cornell Research Foundation, Inc.Inventor: Arthur J. L. Cooper
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Patent number: 4921863Abstract: Cyclic amine derivatives of the formula: ##STR1## or the pharmacologically acceptable salts thereof, wherein the symbols are as defined in the specification, as effective in relieving, curing or preventing mental symptoms due to cerebral vascular disorders.Type: GrantFiled: February 17, 1988Date of Patent: May 1, 1990Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Norio Karibe, Isao Saito, Kunizou Higurashi, Masahiro Yonaga, Takeru Kaneko, Takahiro Nakazawa, Masataka Ueno, Kiyomi Yamatsu
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Patent number: 4897417Abstract: In accordance with the present invention, disclosed herein are compounds of the formula ##STR1## wherein R is straight or branched loweralkyl, R.sub.1 is hydrogen, straight or branched loweralkyl, lowercycloalkyl, amino, loweralkoxy or acylamino, and R.sub.2 is straight or branched loweralkyl, amino, cyclohexyl, morpholino, piperidino, tetrahydrofuranyl, dihydrofuranyl, tetrahydropyranyl, dioxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolidinyl, tetrahydrooxazolyl, and dihydrooxazolyl, and pharmaceutically acceptable salts thereof. The compounds are useful in the treatment of glaucoma.Type: GrantFiled: December 15, 1988Date of Patent: January 30, 1990Assignee: E. I. Du Pont de Nemours & Co.Inventors: Ghanshyam Patil, William L. Matier, Khuong H. X. Mai
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Patent number: 4889953Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.Type: GrantFiled: July 22, 1987Date of Patent: December 26, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
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Patent number: 4879300Abstract: A compound, or a solvate or salt thereof, of formula I: ##STR1## in which: R.CO-- is an acyl group containing a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic group;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkenyl, C.sub.1-6 cycloalkyl or C.sub.1-12 cycloalkylalkyl or together form a C.sub.2-6 polymethylene or C.sub.2-6 alkenylene group, optionally substituted with a hetero-atom, provided that R.sub.1 and R.sub.2 are not simultaneously hydrogen;Rx is C.sub.1-6 alkyl or phenyl, or Rx together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group, is useful for the treatment of pain.Type: GrantFiled: December 21, 1987Date of Patent: November 7, 1989Assignee: Dr. Lo. Zambeletti S.p.A.Inventors: Antonio Giordani, Vittorio Vecchietti
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Patent number: 4871748Abstract: Compounds of the formula: ##STR1## wherein R represents hydroxymethyl, alkoxymethyl of 2 to 6 carbon atoms, optionally substituted phenoxymethyl, alkanoyloxymethyl of 3 to 10 carbon atoms, optionally substituted benzoyloxymethyl, alkylsulphonyloxymethyl of 2 to 9 carbon atoms, optionally substituted phenylsulphonyloxymethyl, formyl, aminomethyl optionally substituted by 1 or 2 alkyl groups of 1 to 4 carbon atoms, or hydroxyiminomethyl, and acid addition salts thereof, are useful as rodenticides.Type: GrantFiled: January 23, 1985Date of Patent: October 3, 1989Assignee: May & Baker LimitedInventor: Leslie R. Hatton
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Patent number: 4870083Abstract: The present invention relates to 1,4-disubstituted-piperidinyl compounds and their use as analgesic agents and as muscle relaxants.Type: GrantFiled: October 11, 1988Date of Patent: September 26, 1989Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Albert A. Carr, Thaddeus R. Nieduzak, Francis P. Miller, Stephen M. Sorensen
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Patent number: 4833244Abstract: Novel ethanobenzazepines, processes for the preparation thereof, and a method of alleviating pain utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: October 1, 1987Date of Patent: May 23, 1989Assignee: Hoechst-Rouseel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Bernhard Seuring
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Patent number: 4803268Abstract: The present invention relates to a novel, optimized process for the preparation of cyclohexanedionecarboxylic acid derivatives of formula I which can be carried out in a single vessel affording a very good yield, which process comprises heating a reactive carboxylic acid derivative of formula III ##STR1## wherein X is a halide, an alkylsulfonic or arylsulfonic acid radical or the molecular radical ##STR2## which is necessary to form an anhydride and R.sub.1 is alkyl or cycloalkyl, with an alkali metal cyanide or copper cyanide, in an inert organic solvent, to give a mixture, then adding in succession to said mixture, at a temperature in the range from 0.degree. C.Type: GrantFiled: January 29, 1987Date of Patent: February 7, 1989Assignee: Ciba-Geigy CorporationInventors: Hans-Georg Brunner, Urs Muller
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Patent number: 4778804Abstract: New nitro aliphatic compounds and their pharmaceutically acceptable salts are disclosed.Type: GrantFiled: October 11, 1985Date of Patent: October 18, 1988Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masanori Okamoto, Morita Iwami, Shigehiro Takase, Itsuo Uchida, Kazuyoshi Umehara, Masanobu Kohsaka, Hiroshi Imanaka
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Patent number: 4767768Abstract: New Nitro aliphatic compounds and their pharmaceutically acceptable salts are disclosed.Type: GrantFiled: December 8, 1983Date of Patent: August 30, 1988Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masanori Okamoto, Morita Iwami, Shigehiro Takase, Itsuo Uchida, Kazuyoshi Umehara, Masanobu Kohsaka, Hiroshi Imanaka
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Patent number: 4764533Abstract: Erythro-1,2,3-triphenyl-1-pentanones of Formula 1 ##STR1## wherein R.sup.1 may be a dimethylamino, diethylamino, piperidin-1-yl- or pyrrolidin-1-yl group and R.sup.2 represents a hydrogen atom, a methoxy or hydroxy group, and their pharmacologically acceptable salts, have a pronounced antiestrogenic effect and are suitable for the treatment of hormone-dependent tumors.They may be prepared by reacting 1,2-diphenyl-ethanone of Formula 2 ##STR2## wherein R.sup.1 is as set forth in Formula 1 and R.sup.2 represents a hydrogen atom or a methoxy group, with sodium hydride in anhydrous dimethyl-formamide, isolating after conversion with 1-chloro-1-phenylpropane, the erythro form from the reaction product and possibly releasing the hydroxy group from the methoxy group by selective cleavage with hydrobromic acid.Type: GrantFiled: July 2, 1984Date of Patent: August 16, 1988Assignee: Klinge Pharma GmbHInventors: Helmut Schickaneder, Roland Loser
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Patent number: 4755522Abstract: This invention is drawn to compounds of the formula: ##STR1## in which R is --CH.sub.2 OH, --COOH and --COOR.sub.1, R.sub.1 being a C.sub.1 to C.sub.4 alkyl group, and their pharmaceutically acceptable salts. The compounds of the invention are useful as anti-depressants and as anti-arrhythmics.Type: GrantFiled: April 24, 1987Date of Patent: July 5, 1988Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4743595Abstract: A process for efficiently preparing 2-amino-5-nitrophenol derivatives in which benzoxazole derivatives are subjected to nucleophilic substitution reaction at the 5 position thereof to obtain corresponding benzoxazole derivatives, and the oxazole ring of the benzoxazole derivatives is then subjected to ring-opening to obtain 2-amino-5-nitrophenol derivatives. The 2-amino-5-nitrophenol derivatives are useful as industrial starting materials, reducing agents or antioxidants and intermediates for cyan-image-forming couplers.Type: GrantFiled: June 12, 1985Date of Patent: May 10, 1988Assignee: Fuji Photo Film Co., Ltd.Inventors: Isamu Itoh, Mitsunori Ono, Hidetoshi Kobayashi, Kazuyoshi Yamakawa
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Patent number: 4739052Abstract: Compounds of the formula I, II or III ##STR1## in which Ar and Ar' are an oxygen-containing aromatic radical, R.sup.1 and R.sup.2 are a monovalent hydrocarbon radical which is substituted or unsubstituted, or R.sup.1 and R.sup.2 together form alkylene, oxaalkylene or azaalkylene, R.sup.3 is a direct bond or a divalent hydrocarbon radical, X and X' are a monovalent amino group and Y is a divalent amino or diamino group, are excellent photoinitiators for the photocuring of colored, especially pigmented, compositions containing an olefinically unsaturated, photopolymerizable binder.Type: GrantFiled: October 2, 1985Date of Patent: April 19, 1988Assignee: Ciba-Geigy CorporationInventors: Rinaldo Husler, Rudolf Kirchmayr, Werner Rutsch
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Patent number: 4723009Abstract: Novel ethanobenzazepines, processes for the preparation thereof, and a method of alleviating pain utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: October 14, 1986Date of Patent: February 2, 1988Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Raymond W. Kosley, Jr., Bernhard Seuring
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Patent number: 4705795Abstract: The present invention relates to new derivatives of (2,4,6-trimethoxyphenyl)-(3-piperidinopropyl)-ketone which are selected from the group consisting of:(i) (2,4,6-trimethoxyphenyl)-[3-(alkylpiperidino)-propyl)]-ketones of general formula: ##STR1## wherein R.sub.1 is CH.sub.3 or C.sub.2 H.sub.5 in 2- or 3-position of the piperidine ring, andR.sub.2 is H, CH.sub.3 or C.sub.2 H.sub.5 ; and(ii) their addition salts. These new derivatives are useful in therapeutics.Type: GrantFiled: February 14, 1986Date of Patent: November 10, 1987Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4695652Abstract: .beta.-Aminoethyl ketones are obtained in a low-polluting manner by Mannich condensation of an aryl ketone having an acidic H with an aldehyde and ammonia or an amine by carrying out the reaction in organic nitriles in the presence of a sulphonic acid or in gycol either in the presence of a sulphonic acid or sulphuric acid.Type: GrantFiled: October 2, 1985Date of Patent: September 22, 1987Assignee: Bayer AktiengesellschaftInventors: Florin Seng, Josef Bremen
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Patent number: 4680296Abstract: Piperidine derivatives which are compounds of formula (I) ##STR1## wherein Ar.sub.1 and Ar.sub.2 independently represent a phenyl group optionally substituted by a halogen atom, a thienyl group or a pyridinyl group, A represents an alkylene group of 2 to 6 carbon atoms, X represents a CO group or a bond, R.sub.1 represents a hydrogen atom or an alkyl group of 1 to 4 carbon atoms, either R.sub.2 represents a hydrogen atom and R.sub.3 represents a hydrogen atom or a hydroxy group, or R.sub.2 and R.sub.3 together represent a bond, and R.sub.4 represents a hydrogen or halogen atom, or pharmaceutically acceptable acid addition salts thereof are useful as antiallergics and antipruritics.Type: GrantFiled: October 15, 1985Date of Patent: July 14, 1987Assignee: SynthelaboInventors: Philippe Manoury, Jean Binet, Elisabeth Dewitte
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Patent number: 4650874Abstract: The invention relates to compounds of the formula: ##STR1## which are useful cardiovascular agents.Type: GrantFiled: November 26, 1984Date of Patent: March 17, 1987Assignee: G. D. Searle & Co.Inventors: Kurt J. Rorig, Chi-Dean Liang, Robert W. Hamilton
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Patent number: 4613597Abstract: Compounds are described of the formulae (1a) and 1b) ##STR1## in which: R.sup.1 is -H, C.sub.1-6 alkyl or C.sub.7-10 aralkyl,W is C.sub.1-7 alkyleneX is cis or trans --CH.dbd.CH--,Y is a saturated heterocyclic amino group having 5-8 ring members,R.sup.2 is (i) substituted or unsubstituted phenylalkyl, thienylalkyl or naphthylalkyl or (ii) cinnamyl, and Z is --CH.sub.2 OH, --CHO or --CONHR.sup.4 where R.sup.4 is --H or methyl,and their salts and solvates.These compounds inhibit blood platelet aggregation, bronchoconstriction and vasoconstriction, and may be formulated for use as antithrombotic and antiasthmatic agents.Type: GrantFiled: September 5, 1984Date of Patent: September 23, 1986Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes
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Patent number: 4593037Abstract: Certain novel 1-(substituted-alkyl)-3-(3-hydroxyphenyl)piperidine compounds, and the pharmaceutically-acceptable acid-addition salts thereof, possess pharmaceutical activity as neuroleptic agents, and they are useful for treating psychotic disorders, e.g. schizophrenia, in human subjects. In particular, they are useful for alleviating such symptoms as anxiety, agitation, excessive agression, tension and social or emotional withdrawal in psychotic patients.Certain 3-(3-methoxyphenyl)piperidine compounds are useful as chemical intermediates to the aforementioned neuroleptic agents.Type: GrantFiled: July 26, 1984Date of Patent: June 3, 1986Assignee: Pfizer Inc.Inventor: Reinhard Sarges
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Patent number: 4548951Abstract: Compounds of the formula ##STR1## and the pharmaceutically acceptable, nontoxic, acid addition salts thereof, whereinR.sub.1 and R.sub.2 are each independently --H, lower alkyl, or cycloalkyl, with the proviso that R.sub.1 and R.sub.2 cannot both be --H or cycloalkyl at the same time;R.sub.1 and R.sub.2 taken together are cycloalkyl of 4-7 carbons;n is 0 or 1;X is (CH.sub.2).sub.2, CH.dbd.CH, or C.tbd.C;Y is independently selected from the group of --H, --Fl, --Br, --Cl, lower alkyl, and --OR.sub.3 ; wherein R.sub.3 is --H or lower alkyl; anda is 1 or 2, ortwo Y's taken together are --OCH.sub.2 O--;are useful as regulators of the cardiovascular system, particularly as hypotensive agents.Type: GrantFiled: April 21, 1983Date of Patent: October 22, 1985Assignee: Syntex (U.S.A.) Inc.Inventors: Joseph M. Muchowski, Jack Ackrell
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Patent number: 4529732Abstract: 2-[2-Hydroxy-4-(substituted)phenyl]piperidines and derivatives thereof of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sub.1 is H, benzyl or certain acyl groups, R.sub.2 is H, certain alkyl, alkenyl, alkynyl, hydroxyalkyl, acyl or alkylsulfonyl groups; R.sub.3 is H.sub.2, O, ##STR2## and Z is (C.sub.1 -C.sub.13)alkylene or -(alk.sub.1).sub.m -O-(alk.sub.2).sub.n - where each of (alk.sub.1) and (alk.sub.2) is (C.sub.1 -C.sub.13)alkylene, provided that the number of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 13; each of m and n is 0 or 1; and W is H, pyridyl or optionally substituted phenyl; their use as analgesic agents, intermediates therefor and processes for their preparation.Type: GrantFiled: March 14, 1983Date of Patent: July 16, 1985Assignee: Pfizer Inc.Inventors: Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4528294Abstract: The present invention relates to new benzoyl-phenyl-piperidine derivatives selected from the group consisting of:(i) 2-piperidinobenzophenones of the general formula: ##STR1## in which: R.sub.1, R.sub.2 and R.sub.3, which are identical or different, each represent an atom of hydrogen, a hydroxy group, CF.sub.3, a halogen, a lower alkyl group or a lower alkoxy group;R.sub.4 represents an atom of hydrogen, a halogen, an NO.sub.2 group, an NR'R" group [where R' and R", which are identical or different, represent an atom of hydrogen, a lower alkyl group or a CO.sub.2 R group (where R represents a lower alkyl group or a benzyl group)];R.sub.5 and R.sub.6, which are identical or different, each represent an atom of hydrogen, a C.sub.1 -C.sub.4 -alkyl group, an OH group, a phenyl group or a benzyl group; and(ii) acid addition salts thereof.The invention also relates to the method for preparing these new derivatives and to their use in therapeutics, particularly as immunostimulant and immunoadjuvant agents.Type: GrantFiled: June 24, 1982Date of Patent: July 9, 1985Assignee: Societe de Recherches Industrielle S.O.R.I.Inventors: Bernard Majoie, Francois Bellamy, Pierre Dodey, Jacques Robin
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Patent number: 4481315Abstract: Compounds which contain, in their molecule, at least one 2-(2'-hydroxyphenyl)-benztriazole group or one 2-hydroxybenzophenone group and at least one polyalkylpiperidine group are effective light stabilizers for organic materials, in particular for polymers. The use of the compounds as light stabilizers for lacquers is of particular importance.Type: GrantFiled: February 28, 1983Date of Patent: November 6, 1984Assignee: Ciba-Geigy CorporationInventors: Jean Rody, Mario Slongo
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Patent number: 4463177Abstract: m-Hydroxyphenyl substituted compounds of formula ##STR1## where R is an organic radical and R.sup.1 is hydroen or an organic radical are prepared by dehydrohalogenating a compound of formula ##STR2## (where X is chlorine or bromine, and R and R.sup.1 have the above meanings). Preferred novel starting materials of formula (II) are of the formula ##STR3## (where R.sup.1 and X are as above, n is 2,3 or 4, R.sup.2 is hydrogen or lower alkyl and R.sup.3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl(lower)alkyl or aryl(lower)alkyl).Type: GrantFiled: November 26, 1982Date of Patent: July 31, 1984Assignee: John Wyeth & Brother LimitedInventor: Robin G. Shepherd
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Patent number: 4430334Abstract: Phenethanolamine derivatives in the (+)-erythro form of the formula: ##STR1## wherein X represents a halogen atom, are new compounds useful in therapy.Type: GrantFiled: April 13, 1982Date of Patent: February 7, 1984Assignee: SynthelaboInventors: Alexander E. Wick, Jonathan R. Frost