Patents by Inventor Fritz Gerhart
Fritz Gerhart 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: 4914240Abstract: Gem-dihalo-1,8-diamino-4-aza-octane derivatives useful as antiproliferative or antitumor agents.Type: GrantFiled: March 30, 1989Date of Patent: April 3, 1990Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Fritz Gerhart, Pierre Mamont
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Patent number: 4851448Abstract: Gem-dihalo-1,8-diamino-4-aza-octane derivatives useful as antiproliferative or antitumor agents.Type: GrantFiled: June 15, 1987Date of Patent: July 25, 1989Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Fritz Gerhart, Pierre Mamont
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Patent number: 4847401Abstract: The large scale preparation of ethyl 2,2-difluoro-4- pentenoate and 2-fluorinated methyl aminoacetonitriles by reaction of 2-H-perfluoroethyl allyl ether and n-butyl lithium and fluoromethylacetonitrile and a Grignard reagent, respectively, is largly unsuccessful because of side reactions which convert intermediate products and reactants to undesired products. Applicants have overcome these problems by performing the reactions with cooling in a continuous manner in a flow reactor with short residence time.Type: GrantFiled: January 15, 1988Date of Patent: July 11, 1989Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Fritz Gerhart, Michael Kolb
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Patent number: 4778926Abstract: Gem-dihalo and gem-tetrahalo-1,12-diamino-4,9-diazadodecane derivatives useful as antiproliferative or antitumor agents.Type: GrantFiled: June 15, 1987Date of Patent: October 18, 1988Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Fritz Gerhart, Pierre Mamont
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Patent number: 4730006Abstract: This invention relates to amino acid, dipeptide and tripeptide derivatives of 2,6-diamino-3-haloheptanedioic acids, processes for preparing the same, and their use as antibacterial agents.Type: GrantFiled: January 27, 1986Date of Patent: March 8, 1988Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Ekkehard H. Bohme, Fritz Gerhart, William Higgins
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Patent number: 4719313Abstract: Gem-dihalo and gem-tetrahalo-1,12-diamino-4,9-diaza-dodecane derivatives useful as antiproliferative or antitumor agents.Type: GrantFiled: February 12, 1986Date of Patent: January 12, 1988Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Fritz Gerhart, Pierre Mamont
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Patent number: 4695654Abstract: Gem-dihalo-1,8-diamino-4-aza-octane derivatives useful as antiproliferative or antitumor agents.Type: GrantFiled: August 21, 1985Date of Patent: September 22, 1987Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Fritz Gerhart, Pierre Mamont
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Patent number: 4621145Abstract: 4-Amino-5-hexenoic acid is prepared by:(a) reacting 5-oxo-2-pyrrolidine-acetonitrile with hydrogen and dimethylamine in the presence of a palladium catalyst to form N,N-dimethyl-2-[5'-oxo-2'-pyrrolidine]ethylamine;(b) oxidizing N,N-dimethyl-2-[5'-oxo-2'-pyrrolidine]-ethylamine to produce the corresponding N-oxide derivative;(c) pyrolysis of the N-oxide derivative to form 5-vinyl-2-pyrrolidinone;(d) optionally, separating N,N-dimethyl-2-[5'-oxo-2'-pyrrolidine]ethylamine by-product from the 5-vinyl-2-pyrrolidinone product; and(e) hydrolyzing 5-vinyl-2-pyrrolidinone to form 4-amino-5-hexenoic acid.Type: GrantFiled: November 29, 1983Date of Patent: November 4, 1986Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Wolfgang Frieben, Fritz Gerhart
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Patent number: 4446151Abstract: Novel fluorinated diamine derivatives are inhibitors of ornithine decarboxylase enzyme and have the following general Formula I: ##STR1## wherein: R.sub.c represents hydrogen or carboxy;R.sub.1 represents hydrogen or C.sub.1 -C.sub.6 alkyl;Z represents methylene or oxygen;m and n each represent 0 or 1 but m+n=1; andp represents 1 or 2.Type: GrantFiled: August 11, 1982Date of Patent: May 1, 1984Assignee: Merrell Toraude et CompagnieInventors: Fritz Gerhart, Viviane Van Dorsselaer
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Patent number: 4439619Abstract: Fluorinated alkenylene diamine compounds are inhibitors of ornithine decarboxylase enzyme in vivo and have the following formula: ##STR1## wherein: R.sub.a represents hydrogen or R.sub.2, where R.sub.2 is as defined below;R.sub.b represents hydrogen or, when R.sub.a is hydrogen, R.sub.2, where R.sub.2 is as defined below;R.sub.c represents hydrogen or --COR.sub.3, where R.sub.3 is as defined below;R.sub.1 represents hydrogen or C.sub.1 --C.sub.6 alkyl;each R.sub.2, independently, represents C.sub.2 -C.sub.5 alkylcarbonyl, phenylcarbonyl, phenyl-(C.sub.1 -C.sub.4 alkyl) carbonyl, or an aminocarboxylic acid residue derived by removal of an hydroxy group from a carboxy moiety of an L-aminocarboxylic acid;R.sub.3 represents hydroxy, or, when R.sub.a and R.sub.b are both hydrogen, C.sub.1 -C.sub.8 alkoxy, --NR.sub.4 R.sub.5, where R.sub.4 and R.sub.5 are as defined below, or an aminocarboxylic acid residue derived by removal of an hydrogen atom from the amino moiety of an L-aminocarboxylic acid;R.sub.4 and R.sub.Type: GrantFiled: August 21, 1981Date of Patent: March 27, 1984Assignee: Merrell Toraude et CompagnieInventors: Philippe Bey, Fritz Gerhart, Michel Jung
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Patent number: 4435425Abstract: Fluorinated diaminobutane compounds in vivo are inhibitors of gamma-aminobutyric acid transaminase and have the following formula: ##STR1## wherein: R.sub.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl, or phenyl-(C.sub.1 -C.sub.4 alkyl);R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl-(C.sub.1 -C.sub.4 alkyl), or R.sub.4, where R.sub.4 is as defined below;R.sub.3 represents hydrogen, or, except when R.sub.2 represents R.sub.4, R.sub.4, where R.sub.4 is as defined below;each R.sub.4, independently, represents C.sub.2 -C.sub.5 alkylcarbonyl, phenylcarbonyl, phenyl-(C.sub.1 -C.sub.4 alkyl) carbonyl, or an aminocarboxylic acid residue derived by removal of an hydroxy group from the carboxy moiety of an L-aminocarboxylic acid; andp represents 1 or 2,and pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: April 9, 1982Date of Patent: March 6, 1984Assignee: Merrell Toraude et CompagnieInventors: Albert Sjoerdsma, Philippe Bey, Michel Jung, Fritz Gerhart, Daniel Schirlin
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Patent number: 4423073Abstract: Novel fluorinated alkenylene diamine derivatives are inhibitors of ornithine decarboxylase enzyme and have the following general Formula I: ##STR1## wherein: R.sub.c represents hydrogen or --COR.sub.5, where R.sub.5 is as defined below;R.sub.1 represents hydrogen or C.sub.1 -C.sub.6 alkyl;one of R.sub.2 and R.sub.3 represents hydrogen and the other represents C.sub.1 -C.sub.6 alkyl.R.sub.5 represents hydroxy or C.sub.1 -C.sub.8 alkoxy; andp represents 1 or 2.Type: GrantFiled: August 11, 1982Date of Patent: December 27, 1983Assignee: Merrell Toraude et CompagnieInventors: Fritz Gerhart, Viviane Van Dorsselaer
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Patent number: 4418077Abstract: Fluorinated aminobutyric acid and diaminobutane compounds in vivo are inhibitors of gamma-aminobutyric acid transaminase and have the following formula: ##STR1## wherein: Y represents hydrogen or fluorine;Z represents --CH.sub.2 NR.sub.1 R.sub.2, where R.sub.1 and R.sub.2 are as defined below, or --COR.sub.3 where R.sub.3 is as defined below;R.sub.a represents hydrogen or R.sub.4, where R.sub.4 is as defined below;R.sub.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl-(C.sub.1 -C.sub.4 alkyl);R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl-(C.sub.1 -C.sub.4 alkyl) or, when R.sub.a is hydrogen, R.sub.4, where R.sub.4 is as defined below;R.sub.3 represents hydroxy, or when R.sub.a is hydrogen, C.sub.1 -C.sub.8 alkoxy, --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are as defined below, or an aminocarboxylic acid residue derived by removal of an hydrogen atom from the amino moiety of an L-aminocarboxylic acid;each R.sub.4, independently, represents C.sub.2 -C.sub.Type: GrantFiled: August 21, 1981Date of Patent: November 29, 1983Assignee: Merrell Toraude et CompagnieInventors: Philippe Bey, Fritz Gerhart, Michel Jung, Daniel Schirlin
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Patent number: 4375477Abstract: Beta-monofluoromethyl beta-alanine, beta-difluoromethyl beta-alanine and pharmaceutically acceptable esters and amides derived from the acid group, amides derived from the amine group, and salts thereof are novel compounds which inhibit .gamma.-aminobutyric acid transaminase (GABA-T).Type: GrantFiled: July 21, 1980Date of Patent: March 1, 1983Assignee: Merrell Toraude et CompagnieInventors: Philippe Bey, Michael Jung, Fritz Gerhart
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Patent number: 4353828Abstract: Fluorinated alkenylamines of the Formula V ##STR1## wherein n represents 0, 1, 2 or 3; R.sub.1 represents hydrogen or C.sub.1 -C.sub.10 alkyl and Y represents (a), when n represents O, CH.sub.2 F, (b), when n represents 1, CH.sub.2 F or CHF.sub.2, or (c) when n represents 2 or 3, CH.sub.2 F, CHF.sub.2 or CF.sub.3 are novel process intermediates. They are obtained by hydrolysis and subsequent reduction of the corresponding alkenyl fluorinated methyl ketimine magnesium halides, which are novel compounds resulting from reaction of the corresponding alkenyl magnesium halides with the corresponding fluorinated acetonitriles. The fluorinated alkenylamines of Formula V are oxidized while the amino group is protected to provide, after removal of the amine protecting group, the corresponding fluorinated methyl aminoalkanoic acids which are useful pharmacological or anti-bacterial agents.Type: GrantFiled: July 21, 1980Date of Patent: October 12, 1982Assignee: Merrell Toraude et CompagnieInventors: Philippe Bey, Fritz Gerhart, Viviane Van Dorsselaer