Patents by Inventor Henry Najer
Henry Najer has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 4663340Abstract: The present invention relates to imidazolines of general formula (I) ##STR1## and the addition salts formed therefrom with the pharmaceutically acceptable mineral or organic acids, possibly having their own specific pharmacological properties.The invention further relates to the preparation of these products, to their use as new medicines and to the medicinal compositions containing them.Type: GrantFiled: July 3, 1985Date of Patent: May 5, 1987Inventors: Henry Najer, Jean-Francois Giudicelli, Jean-Claude Dufour
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Patent number: 4358451Abstract: Pyrimido- and imidazo-pyridoindole derivatives, in the form of racemates or optically active isomers, of formula: ##STR1## in which n=0 or 1, R.sub.1 =H, Hal, alkyl or alkoxy or CF.sub.3, R.sub.2 =H, alkyl, cycloalkyl-alkyl, cycloalkyl, N,N-dialkylaminoalkyl or phenyl, R.sub.3 =H or alkyl and R.sub.4 =H, alkyl or benzyl are useful as anti-anoxia or psychotropic agents in therapy. They are prepared by cyclizing a compound of formula: ##STR2## wherein R.sub.5 is alkyl, by heating it in an acidic medium, such as ethanolic hydrogen chloride.Type: GrantFiled: January 15, 1980Date of Patent: November 9, 1982Assignee: SynthelaboInventors: Gabor I. Koletar, Jonathan R. Frost, Regis DuPont, Patrick Lardenois, Claude Morel, Henry Najer
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Patent number: 4336256Abstract: Pyridoindole derivatives of formula ##STR1## n=0 or 1; R.sub.1 =H, Hal, alk, alk--O--, CF.sub.3 ; R.sub.2 =--COOalk; --CONHR.sub.5 (R.sub.5 =H or various substituents); R.sub.3 =H, alk, --COOalk; R.sub.4 =H, Ac, alk, --CONHR.sub.6 (R.sub.6 =H or various substituents), and acid addition salts, except certain known compounds, are useful in treating anoxia and depression and in psychotropic therapy. They are prepared from tryptamine or a derivative thereof by reaction thereof with a pyruvic ester or 3-ethoxycarbonyl-1,2-dioxo-1-ethoxypropane to form compounds in which R.sub.4 is H and R.sub.2 is --COOalk. These compounds are reacted with amines, isocyanates or usual N-acylating or N-alkylating reagents to prepare the other compounds.Type: GrantFiled: September 4, 1980Date of Patent: June 22, 1982Assignee: SynthelaboInventors: Gabor I. Koletar, Jonathan B. Frost, Regis DuPont, Patrick Lardenois, Claude Morel, Henry Najer
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Patent number: 4311708Abstract: The invention provides phenol ethers of the formula: ##STR1## whereinR is branched C.sub.3-4 alkyl, C.sub.3-4 cycloalkyl, branched cyano(C.sub.3-4 alkyl), phenyl(C.sub.2-3 alkyl), halophenyl(C.sub.2-3 alkyl), (C.sub.1-4 alkoxy)phenyl(C.sub.2-4 alkyl), or (C.sub.1-4 acyl)amino(C.sub.1-4 alkyl),alk is C.sub.1-4 alkyl substituted by a 3 to 6 membered cycloalkyl group,X is --O--, --S-- or --SO.sub.2 --; andR.sub.1 is --C.sub.1-4 alkyl- or --C.sub.1-4 alkoxy-,in their racemic and optically active forms, and their addition salts with pharmaceutically acceptable acids. These compounds are useful in therapy as .beta.-adrenergic blocking agents. Intermediates are also provided.Type: GrantFiled: March 14, 1979Date of Patent: January 19, 1982Assignee: SynthelaboInventors: Philippe M. J. Manoury, Icilio A. G. Cavero, Henry Najer, Don P. R. L. Giudicelli
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Patent number: 4272539Abstract: Pyridoindole derivatives of formula ##STR1## n=0 or 1; R.sub.1 =H, Hal, alk, alk-O-, CF.sub.3 ; R.sub.2 =--COOalk; --CONHR.sub.5 (R.sub.5 =H or various substituents); R.sub.3 =H, alk, --COOalk; R.sub.4 =H, Ac, alk, --CONHR.sub.6 (R.sub.6 =H or various substituents), and acid addition salts, except certain known compounds, are useful in treating anoxia and depression and in psychotropic therapy. They are prepared from tryptamine or a derivative thereof by reaction thereof with a pyruvic ester or 3-ethoxycarbonyl-1,2-dioxo-1-ethoxypropane to form compounds in which R.sub.4 is H and R.sub.2 is --COOalk. These compounds are reacted with amines, isocyanates or usual N-acylating or N-alkylating reagents to prepare the other compounds.Type: GrantFiled: January 15, 1980Date of Patent: June 9, 1981Assignee: SynthelaboInventors: Gabor I. Koletar, Jonathan R. Frost, Regis Dupont, Patrick Lardenois, Claude Morel, Henry Najer
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Patent number: 4267328Abstract: Phenylpiperazine derivatives having the general formula (I) ##STR1## in which R.sub.1 represents a radical S(O).sub.m R.sub.3, S(O).sub.n CF.sub.3 or ##STR2## in which radicals m is 0, 1 or 2, n is 1 or 2, R.sub.3 is an alkyl radical having 1 to 10 carbon atoms and R.sub.4 and R.sub.5 independently represent a hydrogen atom or an alkyl radical having 1 to 4 carbon atoms, or the N atom, R.sub.4 and R.sub.5 together form a heterocyclic ring, which can contain another hetero-atom, and R.sub.2 represents a hydrogen atom, the radical CH.sub.2 --CH.sub.2 --OH or a radical of formula CH.sub.2 --CH.sub.2 --O--COR.sub.6, CH.sub.2 --CH.sub.2 --O--CONHR.sub.6 or CH.sub.2 --CH.sub.2 --O--R.sub.6 in which radicals R.sub.6 being an alkyl radical having 1 to 6 carbon atoms and their pharmaceutically acceptable acid addition salts are useful psychotropic agents and analgesics. Compounds in which R.sub.1 is --SCH.sub.3 and simultaneously R.sub.2 is H are not part of the invention.Type: GrantFiled: July 27, 1979Date of Patent: May 12, 1981Assignee: SynthelaboInventors: Henry Najer, Philippe Manoury
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Patent number: 4265911Abstract: Propionamidoxime derivatives which are compounds of formula (I) ##STR1## in which A is a tetrahydronaphthyl or dihydronaphthyl radical and their pharmaceutically acceptable salts are valuable for treatment of the central nervous system and depression.The above compounds are prepared by reacting the nitrile (II) ##STR2## with hydroxylamine hydrochloride.Type: GrantFiled: October 9, 1979Date of Patent: May 5, 1981Assignee: SynthelaboInventors: Henry Najer, Daniel Obitz
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Patent number: 4261998Abstract: 2-(2-Chlorobenzyl)-1,2,3,4-tetrahydroisoquinoline of the formula ##STR1## and its pharmaceutically acceptable addition salts, are useful for the treatment of arterial or venous thrombosis. They can be prepared by reducing the amide 2-(2-chlorobenzoyl)-1,2,3,4-tetrahydroisoquinoline, for example with boron hydride in an inert organic solvent, and optionally converting a free amine thereby produced into a salt.Type: GrantFiled: November 13, 1979Date of Patent: April 14, 1981Assignee: SynthelaboInventor: Henry Najer
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Patent number: 4252984Abstract: The invention provides phenol ethers of the formula: ##STR1## wherein R is branched C.sub.3-4 alkyl, C.sub.3-4 cycloalkyl, branched cyano(C.sub.3-4 alkyl), phenyl(C.sub.2-3 alkyl), halophenyl(C.sub.2-3 alkyl), (C.sub.1-4 alkoxy)phenyl(C.sub.2-4 alkyl), or (C.sub.1-4 acyl)amino(C.sub.1-4 alkyl),alk is C.sub.1-4 alkyl substituted by a 3 to 6 membered cycloalkyl group,X is --O--, --S-- or --SO.sub.2 --; andR.sub.1 is --C.sub.1-4 alkyl- or --C.sub.1-4 alkoxy-,in their racemic and optically active forms, and their addition salts with pharmaceutically acceptable acids. These compounds are useful in therapy as .beta.-adrenergic blocking agents. Intermediates are also provided.Type: GrantFiled: October 20, 1976Date of Patent: February 24, 1981Assignee: SynthelaboInventors: Philippe M. J. Manoury, Icilio A. G. Cavero, Henry Najer, Don Pierre R. L. Giudicelli
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Patent number: 4242343Abstract: Phenylpiperazine derivatives corresponding to the formula (I) ##STR1## in which n is 1, 2 or 3 and R represents the tetrahydrofuryl-2 radical, or the radical CH.sub.2 -SH, or a radical CH.sub.2 -S-alkyl, or a radical CH.sub.2 -O-alkyl or a radical CH.sub.2 -S-CO-alkyl, the alkyls having from 1 to 8 carbon atoms,and also their addition salts with pharmaceutically acceptable acids.These compounds are tranquilizers with psychotropic properties which permit their use in anxiety and depression.Type: GrantFiled: June 15, 1979Date of Patent: December 30, 1980Assignee: SynthelaboInventors: Henry Najer, Philippe Manoury
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Patent number: 4190657Abstract: The present invention relates to new indolo [3,2,1-de]-[1,5]naphthyridine derivatives and their addition salts with pharmaceutically acceptable acids, the preparation of such derivatives and salts and medicaments in which they are present as active principle.Type: GrantFiled: April 11, 1977Date of Patent: February 26, 1980Assignee: SynthelaboInventors: Gabor I. Koletar, Henry Najer, Jean P. G. LeFevre, Regis Dupont, Don Pierre R. L. Giudicelli, Claude C. H. Morel
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Patent number: 4189495Abstract: The invention provides novel 2-methoxy-benzamide derivatives of the formula: ##STR1## in which n is 1 or 2; R.sub.1 represents a cycloalkyl-alkyl radical of formula: ##STR2## a phenylalkyl radical of formula ##STR3## (in which m is an integer from 2 to 5, A is a linear or branched alkylene chain of 1 to 4 carbon atoms, and R.sub.4 is hydrogen, halogen, especially fluorine or chlorine, trifluoromethyl, or alkyl or alkoxy of 1 to 3 carbon atoms), CNCH.sub.2 --CH.sub.2 --, CH.tbd.C--CH.sub.2 --, ##STR4## R.sub.2 is either chlorine, SO.sub.2 R.sub.5 (in which R.sub.5 is alkyl of 1 to 4 carbon atoms), or SO.sub.2 NR.sub.6 R.sub.7 (in which, R.sub.6 and R.sub.7, which are identical or different, represent, independently of one another, hydrogen or alkyl of 1 to 4 carbon atoms); and R.sub.3 is hydrogen or alkyl of 1 to 4 carbon atoms; in the form of racemates or optical isomers, and their pharmaceutically acceptable acid addition salts, which are useful in the treatment of psychosomatic and pyschotic disturbances.Type: GrantFiled: October 4, 1978Date of Patent: February 19, 1980Assignee: SynthelaboInventors: Jean-Pierre Kaplan, Bernard M. Raizon, Daniel C. L. Obitz, Philippe M. J. Manoury, Henry Najer, Maurice Jalfre, Don P. R. L. Giudicelli
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Patent number: 4172143Abstract: The invention provides novel 2-methoxy-benzamide derivatives of the formula: ##STR1## WHEREIN,M IS AN INTEGER FROM 2 TO 5;A is a linear or branched alkylene chain of 1 to 4 carbon atoms;R.sub.2 is chlorine, SO.sub.2 R.sub.5 or SO.sub.2 NR.sub.6 R.sub.7 ;R.sub.3 is hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.5 is alkyl of 1 to 4 carbon atoms;EACH OF R.sub.6 and R.sub.7 is independently hydrogen or alkyl of 1 to 4 carbon atoms in the form of racemates or optical isomers and their pharmaceutically acceptable acid addition salts which are useful in the treatment of psychosomatic and psychotic disturbances.Type: GrantFiled: June 16, 1977Date of Patent: October 23, 1979Assignee: SynthelaboInventors: Jean-Pierre Kaplan, Bernard M. Raizon, Daniel C. L. Obitz, Philippe M. J. Manoury, Henry Najer, Maurice Jalfre, Don P. R. L. Giudicelli
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Patent number: 4158060Abstract: The invention provides novel 2-methoxy-benzamide derivatives of the formula: ##STR1## in which n is 1 or 2; R.sub.1 represents a cycloalkyl-alkyl radical of formula: ##STR2## a phenylalkyl radical of formula ##STR3## (in which m is an integer from 2 to 5, A is a linear or branched alkylene chain of 1 to 4 carbon atoms, and R.sub.4 is hydrogen, halogen, especially fluorine or chlorine, trifluoromethyl, or alkyl or alkoxy of 1 to 3 carbon atoms), CNCH.sub.2 --CH.sub.2 --, CH.tbd.C--CH.sub.2 --, ##STR4## R.sub.2 is either chlorine, SO.sub.2 R.sub.5 (in which R.sub.5 is alkyl of 1 to 4 carbon atoms), or SO.sub.2 NR.sub.6 R.sub.7 (in which, R.sub.6 and R.sub.7, which are identical or different, represent, independently of one another, hydrogen or alkyl of 1 to 4 carbon atoms); and R.sub.3 is hydrogen or alkyl of 1 to 4 carbon atoms; in the form of racemates or optical isomers, and their pharmaceutically acceptable acid addition salts, which are useful in the treatment of psychosomatic and psychotic disturbances.Type: GrantFiled: December 10, 1976Date of Patent: June 12, 1979Assignee: SynthelaboInventors: Jean-Pierre Kaplan, Bernard M. Raizon, Daniel C. L. Obitz, Philippe M. J. Manoury, Henry Najer, Maurice Jalfre, Don P. R. L. Giudicelli
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Patent number: 4148923Abstract: Trifluoromethylthiophenylethylamine derivatives, made from the corresponding acid chlorides by successive reduction, condensation with nitroethane, reduction, and condensation with an amine, possess anorexigenic properties, unaccompanied by central stimulant activity or cardiovascular effects.Type: GrantFiled: January 16, 1978Date of Patent: April 10, 1979Assignee: SynthelaboInventors: Don P. R. L. Giudicelli, Henry Najer
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Patent number: 4129598Abstract: Trifluoromethylthiophenylethylamine derivatives, made from the corresponding acid chlorides by successive reduction, condensation with nitroethane, reduction, and condensation with an amine, possess anorexigenic properties, unaccompanied by central stimulant activity or cardiovascular effects.Type: GrantFiled: May 24, 1974Date of Patent: December 12, 1978Assignee: SynthelaboInventors: Don P. R. L. Giudicelli, Henry Najer
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Patent number: 4067996Abstract: The invention provides novel phenylacetic acid derivatives of the formula: ##STR1## in which X and Y are the same or different and each represents halogen and R represents hydroxyl, alkoxy of 1 to 4 carbon atoms, a radical of formula R.sub.1 --NH--C.sub.n H.sub.2n --O--, in which n is an integer from 1 to 4 and R.sub.1 is hydrogen or an alkanoyl radical R.sub.2 CO--, in which R.sub.2 is alkyl of 1 to 4 carbon atoms, a radical of formula R.sub.4 NH--, in which R.sub.4 is hydrogen or --C.sub.m H.sub.2m OH, where m is an integer from 1 to 3, or a radical of formula: ##STR2## --OC.sub.m H.sub.2m --COOR.sub.2 or --O(CH.sub.2).sub.p --Z radical, where n, m and R.sub.2 have the meanings given above, p is 0 or 1, and Z is a saturated or unsaturated ring with 6 ring atoms, one of which can be nitrogen, and which can carry from 1 to 3 methyl radicals, and the addition salts which such a derivative which contains a salifiable basic group forms with pharmaceutically acceptable acids and a process for their preparation.Type: GrantFiled: December 30, 1975Date of Patent: January 10, 1978Assignee: SynthelaboInventors: Henry Najer, Don Pierre Rene Lucien Giudicelli, Philippe Michel Jacques Manoury, Jean-Marie Louis Eugene Roger
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Patent number: 4044132Abstract: The invention provides a new piperazine derivative, 1-(4-fluoro-3-trifluoromethylthio-phenyl)-piperazine of the formula ##STR1## and its pharmaceutically acceptable acid addition salts, which is useful as a medicament in human and veterinary therapy because of its anorexia-inducing effect.Type: GrantFiled: March 11, 1976Date of Patent: August 23, 1977Assignee: SynthelaboInventors: Henry Najer, Regis Dupont, Don Pierre Rene Lucien Giudicelli
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Patent number: 4031094Abstract: Compounds particularly useful in view of their anorexigenic and anxiolytic properties are provided which are the N'-alcoxycarbonylalkyl, N'-cyanoalkyl and N'-carboxyalkyl derivatives of N-meta-trifluoromethylphenylpiperazine.Type: GrantFiled: January 22, 1976Date of Patent: June 21, 1977Assignee: SynthelaboInventors: Don Pierre Rene Lucien Giudicelli, Henry Najer
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Patent number: 4021567Abstract: The invention provides novel 2-methoxy-benzamide derivatives of the formula: ##STR1## in which n is 1 or 2; R.sub.1 represents a cycloalkyl-alkyl radical of formula:(CH.sub.2).sub.m -CH-A- ,a phenylalkyl radical of formula ##STR2## (in which m is an integer from 2 to 5, A is a linear or branched alkylene chain of 1 to 4 carbon atoms, and R.sub.4 is hydrogen, halogen, especially fluorine or chlorine, trifluoromethyl, or alkyl or alkoxy of 1 to 3 carbon atoms), CNCH.sub.2 -CH.sub.2 -, CH.tbd.C-CH.sub.2 -, ##STR3## R.sub.2 is either chlorine, SO.sub.2 R.sub.5 (in which R.sub.5 is alkyl of 1 to 4 carbon atoms), or SO.sub.2 NR.sub.6 R.sub.7 (in which, R.sub.6 and R.sub.7, which are identical or different, represent, independently of one another, hydrogen or alkyl of 1 to 4 carbon atoms); and R.sub.Type: GrantFiled: December 16, 1975Date of Patent: May 3, 1977Assignee: SynthelaboInventors: Jean-Pierre Kaplan, Bernard Michel Raizon, Daniel Charles Leon Obitz, Philippe Michel Jacques Manoury, Henry Najer, Maurice Jalfre, Don Pierre Rene Lucien Giudicelli