Patents by Inventor Jean-Pierre Kaplan
Jean-Pierre Kaplan 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: 4588748Abstract: Benzylidene derivatives of the formula: ##STR1## wherein n is 3, R represents an amino or hydroxy radical, or a group --OM in which M is an alkali metal, X.sub.1 and X.sub.2 are both Cl, and X.sub.3 is hydrogen are new compounds possessing useful pharmacological properties; they are, more particularly, useful in the treatment of various diseases of the central nervous system.Type: GrantFiled: September 25, 1984Date of Patent: May 13, 1986Assignee: SynthelaboInventor: Jean-Pierre Kaplan
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Patent number: 4558062Abstract: Diphenylazomethines of the formula ##STR1## in which X.sub.1, X.sub.2, X.sub.3 and X.sub.4, which may be the same or different, each represent a hydrogen or halogen atom or a nitro, cyano, hydroxy, methoxy, C.sub.1 -C.sub.3 -alkyl, allyl or phenyl group, and either R represents a 2-(1H-imidazolyl) radical and n is 1 or R represents a 4- (1H-imidazolyl) radical and n is 1 or 2 have antidepressant, analgesic and antiulcerative properties.Type: GrantFiled: June 29, 1984Date of Patent: December 10, 1985Assignee: SynthelaboInventor: Jean-Pierre Kaplan
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Patent number: 4521619Abstract: Benzylidene derivatives of the formula: ##STR1## wherein n represents an integer from 1 through 4, R represents an amino radical, a monoalkylamino group containing 1 through 4 carbon atoms in the alkyl radical, a dialkylamino group containing 1 through 4 carbon atoms in each alkyl radical, or when n represents 2, 3 or 4 a group ##STR2## in which m represents 4 or 5, or a group --OM in which M represents an alkali metal or alkaline earth metal, and X.sub.1 X.sub.2, X.sub.3 and X.sub.4 each represent a hydrogen atom, a halogen atom, or an alkyl radical containing 1 through 6 carbon atoms, are new therapeutically useful compounds. They possess antidepressant, anticonvulsant, anxiolytic, analgesic, anti-inflammatory, ulcer-inhibiting, gastric antisecretory and antihypertensive properties.Type: GrantFiled: November 17, 1983Date of Patent: June 4, 1985Assignee: SynthelaboInventor: Jean-Pierre Kaplan
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Patent number: 4501745Abstract: Imidazo[1,2-a]pyridine derivatives of the general formula: ##STR1## wherein n represents 2, 3 or 4, Y represents a hydrogen or halogen atom or a C.sub.1-4 alkyl radical, Z represents a naphthyl radical; a phenyl radical ##STR2## in which X.sub.1 and X.sub.2 independently of one another each represent a hydrogen or halogen atom, a C.sub.1-4 alkoxy radical, a C.sub.1-6 alkyl radical or the group --CF.sub.3, CH.sub.3 S--, CH.sub.3 SO.sub.2 -- or --NO.sub.2 ; or a thien-2-yl, furan-2-yl or pyridine-2-yl radical optionally carrying a halogen atom or the methyl or ethyl radical in the 5-position, and R represents the hydroxy radical, or a group --NR.sub.1 R.sub.2 in which R.sub.1 and R.sub.2 independently of one another each represent a hydrogen atom; a straight- or branched-chain C.sub.1-5 alkyl radical optionally carrying one or more halogen atoms, a hydroxy radical, a group --N(C.sub.1-4 alkyl).sub.2, a carbamoyl radical or a C.sub.1-4 alkoxy radical; the allyl radical; the propargyl radical; a C.sub.Type: GrantFiled: April 13, 1983Date of Patent: February 26, 1985Assignee: SynthelaboInventors: Jean-Pierre Kaplan, Pascal George
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Patent number: 4492695Abstract: An imidazo[1,2-a]pyridine derivative of the formula: ##STR1## wherein Y represents a hydrogen or halogen atom or a C.sub.1-4 alkyl radical, Z represents a furan-2-yl, thien-2-yl or pyridin-2-yl radical optionally carrying a halogen atom or a methyl or ethyl radical in the 5-position, and R represents the hydroxy radical, a C.sub.1-4 alkoxy radical or a group --NR.sub.1 R.sub.2 in which R.sub.1 and R.sub.2 independently of one another each represent a hydrogen atom; a straight- or branched-chain C.sub.1-5 alkyl radical optionally carrying one or more halogen atoms or a hydroxy radical, a group --N(C.sub.1-4 alkyl).sub.2, a carbamoyl radical or a C.sub.1-4 alkoxy radical; the allyl radical; the propargyl radical; a C.sub.3-6 cycloalkyl radical; the benzyl radical; or the phenyl radical, or alternatively --NR.sub.1 R.sub.Type: GrantFiled: April 13, 1983Date of Patent: January 8, 1985Assignee: SynthelaboInventors: Jean-Pierre Kaplan, Pascal George, Jean-Michel Bernardon
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Patent number: 4478851Abstract: Benzylidene derivatives of the formula: ##STR1## in which each of X.sub.1, X.sub.2, X.sub.3 and X.sub.4 independently of one another represents hydrogen, halogen, a linear or branched alkyl radical of 1 to 4 carbon atoms, CF.sub.3, NO.sub.2, phenyl, methoxy, or amino, at least two of the substituents X.sub.1, X.sub.2, X.sub.3 and X.sub.4 being different from hydrogen, and R represents a linear or branched alkyl radical of 1 to 16 carbon atoms or an alkenyl radical of 2 to 8 carbon atoms, which may be produced by reaction of the corresponding ketones with an amine, are active on the central nervous system, especially as anti-convulsants.Type: GrantFiled: May 2, 1983Date of Patent: October 23, 1984Assignee: SynthelaboInventors: Jean-Pierre Kaplan, Bernard Raizon
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Patent number: 4460592Abstract: 6-Methyl-2-(4-methylthiophenyl)-imidazo[1,2-a]-pyridine-3-N,N-dimethylaceta mide is provided, preferably in the form of a pharmaceutically acceptable salt, for example, 6-methyl-2-(4-methylthiophenyl)-imidazo[1,2-a]-pyridine-3-N,N-dimethylacet amide methylsulfate. Also provided is a method of providing a patient with a hypnotic effect which comprises administering to said patient a hynotically effective amount of the compound 6-methyl-2-(4-methylthiophenyl)-imidazo[1,2-a]-pyridine-3-N,N-dimethylacet amide or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 10, 1983Date of Patent: July 17, 1984Assignee: SynthelaboInventors: Jean-Pierre Kaplan, Pascal George
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Patent number: 4400536Abstract: Benzylidene derivatives of the formula: ##STR1## in which each of X.sub.1, X.sub.2, X.sub.3 and X.sub.4 independently of one another represents hydrogen, halogen, a linear or branched alkyl radical of 1 to 4 carbon atoms, CF.sub.3, NO.sub.2, phenyl, methoxy, or amino, at least two of the substituents X.sub.1, X.sub.2, X.sub.3 and X.sub.4 being different from hydrogen, and R represents a linear or branched alkyl radical of 1 to 16 carbon atoms or an alkenyl radical of 2 to 8 carbon atoms, which may be produced by reaction of the corresponding ketones with an amine, are active on the central nervous system, especially as anti-convulsants.Type: GrantFiled: February 11, 1981Date of Patent: August 23, 1983Assignee: SynthelaboInventors: Jean-Pierre Kaplan, Bernard Raizon
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Patent number: 4400394Abstract: Compounds of the formula: ##STR1## in which X.sub.1, X.sub.2 and X.sub.3, which are identical or different, each represent hydrogen, halogen, methyl, or methoxy, n represents an integer from 1 to 10, and R represents hydroxyl, OM, NH.sub.2, NH(CH.sub.2).sub.3 --COOH, --NH(CH.sub.2).sub.3 --COOM, (where M represents an alkali metal atom), NH(CH.sub.2).sub.3 --COOC.sub.2 H.sub.5, NH-cycloalkyl, NH-phenyl, NH-benzyl (where the benzyl radical is unsubstituted or substituted by halogen or trifluoromethyl), NH-alkyl, N(alkyl).sub.2 and N-(alkyl)-(benzyl), the aforesaid alkyls being straight or branched and having from 1 to 4 carbon atoms and the aforesaid cycloalkyls having from 3 to 6 carbon atoms, except that when X.sub.1 and X.sub.3 are both hydrogen, n is 1 and R is OH, X.sub.2 is not chlorine in the 5-position are useful in the treatment of epilepsy by oral or parenteral administration.Type: GrantFiled: August 3, 1981Date of Patent: August 23, 1983Assignee: SynthelaboInventors: Jean-Pierre Kaplan, Naurice Jalfre, Don P. Giudicelli
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Patent number: 4382938Abstract: Imidazo[1,2-a] pyridines of the formula: ##STR1## and their acid addition salts in which Y represents a hydrogen or halogen atom or a C.sub.1-4 alkyl radical, Z represents a naphthyl radical or a radical ##STR2## in which each of X.sub.1 and X.sub.2 independently of one another is a hydrogen or halogen atom, a C.sub.1-4 alkoxy radical, a C.sub.1-6 alkyl radical or CF.sub.3, CH.sub.3 S--, CH.sub.3 SO.sub.2 --, --NO.sub.2, --NH.sub.2 or --NHCOCH.sub.3, and each of R.sub.1 and R.sub.2 independently of one another represents a hydrogen atom, a straight or branched C.sub.1-5 alkyl radical which is unsubstituted or substituted by one or more halogen atoms or hydroxyl, --N(C.sub.1-4 alkyl).sub.2, carbamoyl or C.sub.1-4 alkoxy radicals, allyl, propargyl, a C.sub.3-6 cycloalkyl radical, benzyl, or phenyl, not both R.sub.1 and R.sub.2 being hydrogen, or --NR.sub.1 R.sub.Type: GrantFiled: October 21, 1981Date of Patent: May 10, 1983Assignee: SynthelaboInventors: Jean-Pierre Kaplan, Pascal George
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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: 4118572Abstract: Dibenz[b,f]oxepins of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as hereinafter described, are described. The foregoing compounds exhibit strong central depressant and neuroleptic properties, and are useful, for example, in the treatment of acute or chronic schizophrenia and also as tranquilizers.Type: GrantFiled: March 18, 1977Date of Patent: October 3, 1978Assignee: Hoffmann-La Roche Inc.Inventors: Max Gerecke, Emilio Kyburz, Jean-Pierre Kaplan
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Patent number: 4105664Abstract: Dibenz[b,f]oxepins of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as hereinafter described. The foregoing compounds exhibit strong central depressant and neuroleptic properties, and are useful, for example, in the treatment of acute or chronic schizophrenia and also as tranquilizers.Type: GrantFiled: March 18, 1977Date of Patent: August 8, 1978Assignee: Hoffmann-La Roche Inc.Inventors: Max Gerecke, Emilio Kyburz, Jean-Pierre Kaplan
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Patent number: 4100173Abstract: Dibenz[b,f]oxepins of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as hereinafter described,Are described. The foregoing compounds exhibit strong central depressant and neuroleptic properties, and are useful, for example, in the treatment of acute or chronic schizophrenia and also as tranquilizers.Type: GrantFiled: March 18, 1977Date of Patent: July 11, 1978Assignee: Hoffmann-La Roche Inc.Inventors: Max Gerecke, Emilio Kyburz, Jean-Pierre Kaplan
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Patent number: 4094992Abstract: Compounds of the formula: ##STR1## in which X.sub.1, X.sub.2 and X.sub.3, which are identical or different each represent hydrogen, halogen, methyl, or methoxy, n represents an integer from 1 to 10, and R represents hydroxyl, OM, NH.sub.2, NH(CH.sub.2).sub.3 --COH, --NH(CH.sub.2).sub.3 --COOM, (where M represents an alkali metal atom), NH(CH.sub.2).sub.3 --COOC.sub.2 H.sub.5, NH-cycloalkyl, NH-phenyl, NH-benzyl (where the benzyl radical is unsubstituted or substituted by halogen or trifluoromethyl), NH-alkyl, N(alkyl).sub.2 and N-(alkyl)-(benzyl), the aforesaid alkyls being straight or branched and having from 1 to 4 carbon atoms and the aforesaid cycloalkyls having from 3 to 6 carbon atoms, except that when X.sub.1 and X.sub.3 are both hydrogen, n is 1 and R is OH, X.sub.2 is not chlorine in the 5-position are useful in the treatment of epilepsy by oral or parenteral administration.Type: GrantFiled: July 16, 1976Date of Patent: June 13, 1978Assignee: SynthelaboInventors: Jean-Pierre Kaplan, Maurice Jalfre, Don Pierre Rene Lucien Giudicelli
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Patent number: 4091023Abstract: Dibenz[b,f]oxepins of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as hereinafter described, are described. The foregoing compounds exhibit strong central depressant and neuroleptic properties, and are useful, for example, in the treatment of acute or chronic schizophrenia and also as tranquilizers.Type: GrantFiled: March 18, 1977Date of Patent: May 23, 1978Assignee: Hoffmann-La Roche Inc.Inventors: Max Gerecke, Emilio Kyburz, Jean-Pierre Kaplan
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Patent number: 4044010Abstract: Compounds of the formfulas ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, m and n and X are as hereinafter set forth,Are described. The compounds of formulas I and Ia are useful as neuroleptic agents.Type: GrantFiled: February 4, 1976Date of Patent: August 23, 1977Assignee: Hoffmann-La Roche Inc.Inventors: Max Gerecke, Jean-Pierre Kaplan, Emilio Kyburz
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Patent number: 4035385Abstract: Compounds of the formulas ##STR1## WHEREIN R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and X are as hereinafter set forth, are described. The compounds of formulas I and Ia are useful as neuroleptic agents.Type: GrantFiled: August 13, 1976Date of Patent: July 12, 1977Assignee: Hoffmann-La Roche Inc.Inventors: Jean-Pierre Kaplan, Emilio Kyburz