Patents by Inventor Henri Demarne
Henri Demarne 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: 4946868Abstract: The invention concerns compositions with antimicrobial activity.These compositions contain a benzoic acid derivative with the formula: ##STR1## in which: A represents a straight or branched alkyl chain with 3 to 4 carbon atoms,X represents the oxygen atom or a direct bond,R represents hydrogen or an alkyl group with 2 to 6 carbon atoms, possibly substituted by an alcohol function and a salt of such a derivative.Applications: drugs, disinfectants and preservative agents.Type: GrantFiled: August 13, 1984Date of Patent: August 7, 1990Assignee: SanofiInventors: Henri Demarne, Robert Filhol, Madeleine Mosse
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Patent number: 4820717Abstract: The present invention relates to new aromatic derivatives of formula: ##STR1## wherein: Alk is an alkylene group with 1 to 10 carbon atoms,R.sub.1 is hydrogen or an alkyl with 1 to 6 carbon atoms,R.sub.2 and R.sub.3 are similar or different and represent a cycloalkyl with 3 to 6 carbon atoms or a striaght or branched alkyl with 1 to 6 carbon atoms, either substituted or non-substituted by a phenyl or methyl phenyl group, or R.sub.2 and R.sub.3 form, together with the atom of nitrogen to which they are bonded, a mono-nitrogenous heterocycle containing no other heteroatom, such as pyrrolidino, piperidino, azepino, hexamethylene-imino, 4-methyl-piperidino, 4-phenyl-piperidino, 1,2,3,4-tetrahydro-2-isoquinolyl, 4-benzyl-piperidino;R.sub.4 is hydrogen, halogen, methyl or phenyl,R.sub.5 is hydrogen, halogen or methyl,or R.sub.4 and R.sub.5 together with the benzene ring to which they are bonded, constitute a 1-naphthyl or 2-naphthyl group,and the pharmaceutically acceptable salts with mineral or organic acids.Type: GrantFiled: September 30, 1986Date of Patent: April 11, 1989Assignee: SanofiInventors: Madeleine Mosse, Henri Demarne, Vincenzo Proietto
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Patent number: 4797469Abstract: A process for the synthesis, in liquid phase and by fragments, of hGRF 1-44 and hGRF 1-40. This process consists in coupling, one after the other and in the order of the sequence of the GRF,(1) on the one hand, the following fragments:__________________________________________________________________________ H--Ala--Arg--Ala--Arg--Leu--NH.sub.2 called Fragment A hGRF (40-44) or alaninamide (40) H--Gln--Glu--Arg--Gly--OH called Fragment B'.sub.1 hGRF (36-39) H--Glu--Ser--Asn--OH called Fragment B'.sub.2 hGRF (33-35) H--Ser--Arg--Gln--Gln--Gly--OH called Fragment C hGRF (28-32) H--Leu--Gln--Asp--Ile--Met--OH called Fragment D' hGRF (23-27) H--Arg--Lys--Leu--OH called Fragment E'.sub.1 hGRF (20-22) __________________________________________________________________________to obtain the peptide K.sub.Type: GrantFiled: August 21, 1987Date of Patent: January 10, 1989Assignee: SanofiInventors: Joseph Diaz, Henri Demarne, Romeo Roncucci, Paul-Henry Schmelck
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Patent number: 4720581Abstract: The present invention relates to benzamidine derivatives corresponding to the general formula ##STR1## in which: A represents a linear or branched alkyl chain containing from 3 to 9 carbon atoms; andX represents the oxygen atom or a direct bond, with the restriction that if X represents a direct bond, the benzamidine and the alkanol group are located in the para position, and also the pharmaceutically acceptable salts of the products of the formula (I);it also relates to a process for the preparation of the products of the formula (I) and the drugs for external use which contain a product of the formula (I).Type: GrantFiled: July 17, 1984Date of Patent: January 19, 1988Assignee: SanofiInventors: Madeleine Mosse, Henri Demarne, Robert Filhoi
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Patent number: 4707541Abstract: A process for the synthesis, in liquid phase and by fragments, of hGRF 1-44 and hGRF 1-40. This process consists in coupling, one after the other and in the order of the sequence of the GRF,(1) on the one hand, the following fragments:______________________________________ H--Ala--Arg--Ala--Arg--Leu--NH.sub.2 called hGRF Frag- (40-44) or ment A alaninamide (40) H--Gln--Glu--Arg--Gly--OH called hGRF Frag- (36-39) ment B'.sub.1 H--Glu--Ser--Asn--OH called hGRF Frag- (33-35) ment B'.sub.2 H--Ser--Arg--Gln--Gln--Gly--OH called hGRF Frag- (28-32) ment C H--Leu--Gln--Asp--Ile--Met--OH called hGRF Frag- (23-27) ment D' H--Arg--Lys--Leu--OH called hGRF Frag- (20-22) ment E'.sub.1 ______________________________________to obtain the peptide K.sub.1 [(hGRF (20-44)] on the corresponding peptide having the sequence (20-40) and(2) on the other hand, the following fragments: ______________________________________ H--Gln--Leu--Ser--Ala called hGRF Frag- (16-19) ment F.sub.Type: GrantFiled: July 8, 1985Date of Patent: November 17, 1987Assignee: SanofiInventors: Joseph Diaz, Henri Demarne, Romeo Roncucci, Paul-Henry Schmelck
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Patent number: 4704450Abstract: The invention relates to synthesis of hpGRF (Somatocrinin) in liquid phase and to intermediate peptides, comprising: coupling, one after the other and in the order of the sequence of the GRF, the fragments in which: (a) the side acid functions of the aspartic and glutamic acids and the side amine function of the lysine are protected by protector groups stable in the conditions of deprotection of the group Boc, (b) the guanidine function of the arginine is protected by protonation, and (c) the N-terminal amino acid is protected on the amine by the Boc group; selectively eliminating the group Boc from the N-terminal amine of the peptide in phase of elongation by hydrolysis with trifluoroacetic acid, said coupling being effected in an aprotic polar solvent and eliminating, at the end of sequence, all the protector groups by hydrolysis with the aid of a 0.1 to 1M solution of methanesulfonic or trifluoromethanesulfonic acid in trifluoroacetic acid.Type: GrantFiled: December 11, 1985Date of Patent: November 3, 1987Assignee: SanofiInventors: Joseph Diaz, Henri Demarne, Romeo Roncucci, Paul-Henry Schmelck
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Patent number: 4696937Abstract: The invention relates to novel thiosulfonate derivatives of general formu a:R--S--SO.sub.2 --R.sub.1in which R represents a 1H-imidazol-2-yl, quinolin-2-yl, 5-amino-1,3,4-thiadizol-2-yl or 4,5-dihydro-thiazol-2-yl radical and R.sub.1 represents a lower alkyl, (hydroxy)lower alkyl, phenyl, (lower alkyl) phenyl, (hydroxy lower alkyl) phenyl, (lower alkanoyl) phenyl or quinolin-8-yl radical.The thiosulfonate derivatives in question exert an inhibitory action with respect to the malformation or destruction of red blood corpuscules due to a genetic modification of haemoglobin or to parasites and can, therefore, be used in the treatment of drepanocytosis, malaria and babebiosis.Type: GrantFiled: November 13, 1985Date of Patent: September 29, 1987Assignees: Sanofi, Institut National de la Sante et de la Recherche Medicale (Inserm)Inventors: Bernard Sebille, Yves Beuzard, Henri Demarne
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Patent number: 4694015Abstract: The invention relates to pharmaceutical or veterinary compositions for initing the malformation or destruction of red blood corpuscules due to a genetic modification of haemoglobin or to parasites, compositions comprising, as active ingredient, at least one thiosulfonate derivative of general formula:R--S--SO.sub.2 --R.sub.1in which R represents a 1-methyl-imidazol-2-yl, 1H-benzimidazol-2-yl or benzoxazol-2-yl radical and R.sub.1 represents a lower alkyl, (hydroxy) lower alkyl, lower alkanoyl, phenyl, (lower alkyl) phenyl, (hydroxy lower alkyl) phenyl, (lower alkanoyl) phenyl or quinolin-8-yl radical.The compositions in question can be used in the treatment of drepanocytosis, malaria and babebiosis.Type: GrantFiled: November 13, 1985Date of Patent: September 15, 1987Assignees: Sanofi, Institut National de la Sante et de la Recherche Medicale (Inserm)Inventors: Bernard Sebille, Yves Beuzard, Henri Demarne
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Patent number: 4691043Abstract: Benzoic acid derivatives with the general formula: ##STR1## in which: A represents a straight or branched alkyl chain with 5 to 10 carbon atoms,X represents the oxygen atom or a direct bond,R represents hydrogen or an alkyl group with 2 to 6 carbon atoms, possibly substituted by an alcohol function,and the salts of the said derivatives.These derivatives display antimicrobial activity and are suitable as antiseptics, disinfectants and preservatives, particularly in the fields of pharmaceuticals, cosmetology and agri-foodstuffs.Type: GrantFiled: January 7, 1986Date of Patent: September 1, 1987Assignee: SanofiInventors: Henri Demarne, Robert Filhol, Madeleine Mosse
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Patent number: 4687760Abstract: The invention relates to the peptides of the formula: ##STR1## in which: R.sub.1 represents hydrogen or a protecting group for the amine group, such as t-butoxycarbonyl, benzyloxycarbonyl or lower alkanoyl groups;X represents beta-alanine glycine or a direct bond between R.sub.1 and the amine group; andR.sub.2 represents a group chosen from: ##STR2## corresponding to the side chains of the natural amino acid leucine, methionine and norleucine.These peptides inhibit gastric secretion.Type: GrantFiled: December 16, 1985Date of Patent: August 18, 1987Assignees: Sanofi, Centre National de la Recherche Scientifque (CNRS)Inventors: Jean Martinez, Jean-Pierre Bali, Richard Magous, Bertrand Castro, Henri Demarne
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Patent number: 4687759Abstract: The invention relates to the peptides of the formula: ##STR1## in which: R represents hydrogen or a protecting group for the terminal amine group, such as t-butoxycarbonyl (Boc), benzyloxycarbonyl (Z) or lower alkanoyl;X.sub.1 represents either beta-Ala or a direct bond between R and the terminal amine group of the amino acid TRP;TRP denotes either the L isomer or the D isomer of tryptophan;X.sub.2 represents L-leucine, L-methionine or L-norleucine; andY denotes hydrogen, a halogen atom (preferably fluorine or chlorine), a trifluoromethyl group, a cyano group or a nitro group.These peptides inhibit gastric secretion.Type: GrantFiled: December 16, 1985Date of Patent: August 18, 1987Assignees: Sanofi, Centre National de la Recherche Scientifique (CNRS)Inventors: Jean Martinez, Jean-Pierre Bali, Richard Magous, Bertrand Castro, Henri Demarne
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Patent number: 4642306Abstract: The present invention relates to cyclic dithiodiacetamides with action inhibiting the malformation or the destruction of the red blood corpuscles due to a genetic modification of the haemoglobin or to parasites, of formula: ##STR1## in which X is a direct bond, an atom of oxygen or of sulfur, a methylene group, an ethylene group or an N--R group, where R is an atom of hydrogen or a lower alkyl group, lower (hydroxy)alkyl group, lower alkanoyl group or a phenyl group; to their possible pharmaceutically acceptable salts; to a process for preparing them from a dithiodiacetate or a mercaptoacetate of lower alkyl by transamination and possible oxidation; and to pharmaceutical compositions containing them as active ingredients, useful for the treatment for example of drepanocytosis, or sickle cell anaemia, of malaria and of babebiosis.Type: GrantFiled: May 17, 1984Date of Patent: February 10, 1987Assignees: Sanofi, Institut National de la Sante et de la Recherche MedicaleInventors: Jean Rosa, Jean-Paul Castaigne, Henri Demarne, Pierre Tozzolino
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Patent number: 4636490Abstract: The invention relates to peptides of general formula:R--A--Gly--Trp--B--Asp--NH.sub.2 (I)in which:Asp NH.sub.2 represents the amide in .alpha. position of the aspartic acid of formula: ##STR1## R represents hydrogen, a protector group of the terminal amine function such as t.butyloxy carbonyl (BOC), benzyloxy carbonyl (Z), lower alkanoyl,A designates:either tyrosine, tyrosine-O-sulfate, threonine or methionine;or a dipeptide selected from: --Ala--TYR--, --TYR--Thr--, --TYR Met--, TYR designating either of the 2 amino-acids tyrosine or tyrosine-O-sulfate;or a tripeptide selected from: --Glu--Ala--TYR--, Asp--TYR--Thr--, --Asp--TYR--MET--;or a tetrapeptide selected from: --Glu--Glu--Ala--TYR--, --Gln Asp--TYR--Thr--, --Arg--ASP--TYR--Met--;or a pentapeptide selected from: --Glu--Glu--Glu--Ala--TYR--, --Pyr--Gln--Asp--TYR--Thr--, --Asp--Arg--Asp--TYR--Met;B designates methionine, leucine or norleucine.Type: GrantFiled: April 6, 1984Date of Patent: January 13, 1987Assignees: Sanofi, Centre National de la Recherche ScientifiqueInventors: Jean Martinez, Jean-Pierre Bali, Bertrand Castro, Dino Nisato, Henri Demarne
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Patent number: 4587245Abstract: Benzodiazepines of formula ##STR1## wherein R3 is methyl or ethyl and R4 is chlorine or fluorine are useful therapeutic agents for the treatment of neuropsychic disturbances.Type: GrantFiled: January 28, 1985Date of Patent: May 6, 1986Assignee: SanofiInventors: Henri Demarne, Andre Hallot
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Patent number: 4581168Abstract: The invention relates to synthesis of hpGRF (Somatocrinin) in liquid phase and to intermediate peptides, comprising:--coupling, one after the other and in the order of the sequence of the GRF, the fragments in which: (a) the side acid functions of the aspartic and glutamic acids and the side amine function of the lysine are protected by protector groups stable in the conditions of deprotection of the group Boc, (b) the guanidine function of the arginine is protected by protonation, and (c) the N-terminal amino acid is protected on the amine by the Boc group;--selectively eliminating the group Boc from the N-terminal amine of the peptide in phase of elongation by hydrolysis with trifluoroacetic acid, said coupling being effected in an aprotic polar solvent and--eliminating, at the end of sequence, all the protector groups by hydrolysis with the aid of a 0.1 to 1M solution of methanesulfonic or trifluoromethanesulfonic acid in trifluoroacetic acid.Type: GrantFiled: February 17, 1984Date of Patent: April 8, 1986Assignee: SanofiInventors: Joseph Diaz, Henri Demarne, Romeo Roncucci, Paul-Henry Schmelck
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Patent number: 4510315Abstract: The present invention discloses a 4-[3-(1,1-dimethyl-2-3(3-indolyl)ethylamino)-2-hydroxypropoxy]indole of formula ##STR1## and pharmaceutically acceptable acid salts thereof, which are particularly active on the cardiovascular system.Type: GrantFiled: September 9, 1983Date of Patent: April 9, 1985Assignee: Sanofi, S.A.Inventors: Henri Demarne, Jean Wagnon
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Patent number: 4435426Abstract: The present invention relates to novel products, responding to general formula: ##STR1## in which R.sub.1 and R.sub.2 taken together represent an atom of oxygen .dbd.O or R.sub.1 represents hydrogen and R.sub.2 represents an OH radical, R.sub.3 designates an atom of hydrogen or a straight or branched alkyl radical, or an alkynyl group having from 1 to 6 atoms of carbon, R.sub.4 represents a straight or branched alkyl radical having from 1 to 6 atoms of carbon, R.sub.5 designates an atom of hydrogen, an alkyl group having from 1 to 4 atoms of carbon or an acylamine group and n=3 or 4; as well as to the acid addition salts of said products, to a process for preparing said products and to drugs, particularly active on the cardiovascular system, containing at least one of said products.Type: GrantFiled: May 25, 1982Date of Patent: March 6, 1984Assignee: Societe Anonyme dite: SanofiInventors: Henri Demarne, Jean Wagnon
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Patent number: 4404217Abstract: The present invention relates to the chemical products of general formula: ##STR1## in which R.sub.1 and R.sub.2 designate hydrogen; halogen, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 designate hydrogen, alkyl, alkoxy, halogen, nitro, acyl, alkylthio, alkylsulfinyl, alkylsulfonyl, a (CH.sub.2).sub.n COOR, (CH.sub.2).sub.2 CONHR, (CH.sub.2).sub.n NHCOOR or (CH.sub.2).sub.n NHCOR group; or R.sub.3 and R.sub.4 together form a heterocycle bonded to the benzene cycle; X.sub.1 is hydrogen, alkyl, hydroxymethyl or COOR and X.sub.2 is hydrogen or methyl; and to the pharmaceutically acceptable salts of said products. It also relates to a process for preparing said products and to the drugs active in particular on the cardiovascular system, containing at least one of said products.Type: GrantFiled: August 15, 1980Date of Patent: September 13, 1983Assignee: C. M. IndustriesInventors: Henri Demarne, Jean Wagnon
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Patent number: 4356177Abstract: The present invention relates to new pyridine derivatives of formula: ##STR1## wherein R.sub.1 is an alkyl or an alicyclic group, R.sub.2 and R.sub.3 are alkyls or alicyclic groups or form an heterocycle with the atom of nitrogen to which they are bonded; the invention also relates to a process for the preparation of said derivatives and the medicines containing at least one of the said derivatives.Type: GrantFiled: October 7, 1980Date of Patent: October 26, 1982Assignee: C.M. IndustriesInventors: Henri Demarne, Claude Bernhart, Jacqueline Lansen
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Patent number: 4302601Abstract: The present invention relates to phenoxypropane having the formula ##STR1## in which R.sup.1 and R.sup.2 are like or unlike and each is an alkyl group having 1-4 carbon atoms, R.sup.3 is hydrogen or an alkyl group having 1-4 carbon atoms, R.sup.4 is a halogen atom, preferably fluorine, chlorine or bromine, including their optical isomers and also their addition salts with acids.These compounds are of therapeutic value in the treatment of cardiovascular conditions.The invention also relates to methods of synthesis of these products including a synthesis which involves the production, as a intermediate of an 8-aza-4,9-dioxa-2,3-benzo-bicyclo-[4,2,1]-octane having the formula ##STR2## in which R.sup.1 and R.sup.4 are as above defined.Type: GrantFiled: March 12, 1980Date of Patent: November 24, 1981Assignee: C M IndustriesInventor: Henri Demarne