Patents by Inventor Reinhard Sarges
Reinhard Sarges 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: 5998463Abstract: This invention relates to certain 5-acyl-2-oxo-indole-3-carboxamides useful as inhibitors of glycogen phosphorylase, methods of treating glycogen phosphorylase dependent diseases or conditions with such compounds and pharmaceutical compositions comprising such compounds. This invention also relates to pharmaceutical compositions comprising those 5-acyl-2-oxo-indole-3-carboxamides in combination with antidiabetes agents and methods of treating glycogen phosphorylase dependent diseases or conditions with such compositions.Type: GrantFiled: February 16, 1999Date of Patent: December 7, 1999Assignee: Pfizer IncInventors: Bernard Hulin, Reinhard Sarges
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Patent number: 5362743Abstract: Certain novel 3-acyl-4-amino-8-alkoxyquinoline compounds have been prepared, including their pharmaceutically-acceptable salts. These compounds are useful for inhibiting gastric acid secretion in mammals and therefore, are of value in therapy as anti-ulcer agents. They are also useful for treating osteoporosis in a mammalian subject afflicted with said condition. Methods for preparing these compounds from known starting materials are provided.Type: GrantFiled: March 9, 1993Date of Patent: November 8, 1994Assignee: Pfizer Inc.Inventors: Reinhard Sarges, Li-An Yeh
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Patent number: 5064852Abstract: A series of novel 3-mono(substituted methyl)- and 3,3-di(substituted methyl)-2-oxo-indoline-1-alkanoic acid compounds have been prepared, including their lower alkyl esters and unsubstituted amide derivatives, as well as the base salts of said acids with pharmacologically acceptable cations. These compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. Typical members include those compounds derived from 2-oxo-indoline-1-acetic acid wherein a 3,4-dichlorobenzyl or 3,4-dichloro-.alpha.-methylbenzyl moiety is substituted at 3-position of the molecule. Preferred member compounds include 3-(3,4-dichlorobenzyl)-2-oxo-indoline-1-acetic acid, 5-chloro-3-(3,4-dichlorobenzyl)-2-oxo-indoline-1-acetic acid, 3-(3,4-dichlorobenzyl)-6-methoxy-2-oxo-indoline-1-acetic acid, 3-(3,4-dichlorobenzyl)-6-hydroxy-2-oxo-indoline-1-acetic acid and 3-(3,4-dichloro-.alpha.-methylbenzyl)-2-oxo-indoline-1-acetic acid.Type: GrantFiled: August 1, 1990Date of Patent: November 12, 1991Assignee: Pfizer Inc.Inventors: Harry R. Howard, Jr., Reinhard Sarges
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Patent number: 5011840Abstract: A series of novel 5-substituted imidazolidinedione derivatives and their base salts with pharmacologically acceptable cations are disclosed. These particular compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. 5-Naphthalimido-imidazolidine-2,4-dione and 5-[3-(4'-bromo-2'-fluorobenzyl)-3,4-dihydro-4-oxophthalazin-1-yl]-imidazol idine-2,4-dione represent typical and preferred member compounds. Methods for preparing all these compounds from known starting materials are provided.Type: GrantFiled: May 5, 1989Date of Patent: April 30, 1991Assignee: Pfizer Inc.Inventor: Reinhard Sarges
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Patent number: 4980357Abstract: A series of novel spiro-deteroazolones derived from a 2,3-dihydropryrano[2,3-b]pyridine ring system have been prepared, including their pharmaceutically acceptable salts. These compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. Typical member compounds include spiro-imides, spiro-oxazolidinediones, spiro-thiazolidinediones and spiro-imidazolidinediones derived from the aforesaid ring system. (4'S) (2'R)-6'-Chloro-2',3'-dihydro-2'-methyl-spiro-[imidazolidine-4,4'-4'H-pyra no[2,3-b]pyridine]-2,5-dione represents a typical and preferred member compound. Methods for preparing all these compounds from known starting materials are provided.Type: GrantFiled: March 1, 1990Date of Patent: December 25, 1990Assignee: Pfizer Inc.Inventors: Steven W. Goldstein, Reinhard Sarges
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Patent number: 4977178Abstract: Certain substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones are highly potent gabaergic agents, valuable in the treatment of individuals suffering from schizophrenia or reversing the side effects of a previously or concurrently administered neuroleptic agent; or in the treatment of epilepsy. A wider class of substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones, together with 1-phenyl-3-(2-pyrrolidinylidene)-2(1H,3H)-indolones, and homologs thereof, are valuable in the treatment of anxiety.Type: GrantFiled: July 19, 1989Date of Patent: December 11, 1990Assignee: Pfizer Inc.Inventors: Harry R. Howard, Jr., Reinhard Sarges
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Patent number: 4960785Abstract: A series of novel 3-mono(substituted methyl)- and 3,3-di(substituted methyl)-2-oxo-indoline-1-alkanoic acid compounds have been prepared, including their lower alkyl esters and unsubstituted amide derivatives, as well as the base salts of said acids with pharmacologically acceptable cations. These compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. Said oxindole-1-alkanoic acid compounds are of the formulae: ##STR1## wherein X is hydrogen and X.sup.1 is hydrogen, hydroxy, fluorine, chlorine, bromine, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy; or X and X.sup.1, when taken separately, are each chlorine, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, and when taken together are --OCH.sub.2 (CH.sub.2).sub.n O-- at the 4,5-, 5,6- or 6,7-positions of the molecule wherein n is zero or one; R.sub.1 is hydrogen or methyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.Type: GrantFiled: December 16, 1988Date of Patent: October 2, 1990Assignee: Pfizer Inc.Inventors: Harry R. Howard, Jr., Reinhard Sarges
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Patent number: 4940708Abstract: A series of novel 4-arylsulfonyl-3,4-dihydro-2(1H)-quinoxalinone-1-alkanoic acid compounds have been prepared, including their lower alkyl ester derivatives, as well as the base salts of said acids with pharmacologically acceptable cations. These particular compounds are useful in therapy as agents for the control of certain chronic diabetic complications. Typical members include those compounds derived from 3,4-di-hydro-2-(1H)-quinoxalinone-1-acetic acid wherein an unsubstituted or substituted phenylsulfonyl moiety is located at the 4-position of the molecule. Ethyl 4-benzenesulfonyl-3,4-dihydro-2(1H)-quinoxalinone-1-acetate and 4-benzenesulfonyl-3,4-dihydro-2(1H)-quinoxalinone-1-acetic acid represent typical and preferred member compounds. Methods for preparing all these compounds from known starting materials are provided.Type: GrantFiled: June 30, 1988Date of Patent: July 10, 1990Assignee: Pfizer Inc.Inventor: Reinhard Sarges
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Patent number: 4879391Abstract: Certain substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones are highly potent gabaergic agents, valuable in the treatment of individuals suffering from schizophrenia or reversing the side effects of a previously or concurrently administered neuroleptic agent; or in the treatment of epilepsy. A wider class of substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones, together with 1-phenyl-3-(2-pyrrolidinylidiene-2(1H,3H)-indolones, and homologs thereof, are valuable in the treatment of anxiety.Type: GrantFiled: August 3, 1987Date of Patent: November 7, 1989Assignee: Pfizer Inc.Inventors: Harry R. Howard, Jr., Reinhard Sarges
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Patent number: 4861880Abstract: Certain substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones are highly potent gabaergic agents, valuable in the treatment of individuals suffering from schizophrenia or reversing the side effects of a previously or concurrently administered neuroleptic agent; or in the treatment of epilepsy. A wider class of substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones, together with 1-phenyl-3-(2-pyrrolidinylidene)-2(1H,3H)-indolones, and homologs thereof, are valuable in the treatment of anxiety.Type: GrantFiled: August 15, 1984Date of Patent: August 29, 1989Assignee: Pfizer Inc.Inventors: Harry R. Howard, Jr., Reinhard Sarges
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Patent number: 4623725Abstract: A series of novel [1,2,4]triazolo[4,3-a]quinoxaline-4-amine derivatives wherein the amine group is optionally substituted with lower alkyl, phenylalkyl having up to three carbon atoms in the alkyl moiety or alkanoyl having from two to five carbon atoms, or the amine group alternatively completes a piperazino ring, the quinoxaline ring is optionally substituted with fluorine, chlorine, bromine or methoxy, and the triazolo ring is optionally substituted with lower alkyl, lower perfluoroalkyl or phenyl are disclosed. These novel compounds are useful for treatment of symptoms associated with depression. Also disclosed are pharmaceutical compositions containing the novel compounds of this invention.Type: GrantFiled: November 8, 1985Date of Patent: November 18, 1986Assignee: Pfizer Inc.Inventors: Saul B. Kadin, Reinhard Sarges
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Patent number: 4623728Abstract: Certain novel 1-(substituted-alkyl)-3-(3-hydroxyphenyl)piperidine compounds, and the pharmeceutically-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 aggression, 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: February 14, 1986Date of Patent: November 18, 1986Assignee: Pfizer Inc.Inventor: Reinhard Sarges
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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: 4547501Abstract: A series of novel [1,2,4]triazolo[4,3-a]quinoxaline-4-amine derivatives wherein the amine group is optionally substituted with lower alkyl, phenylalkyl having up to three carbon atoms in the alkyl moiety or alkanoyl having from two to five carbon atoms, or the amine group alternatively completes a piperazino ring, the quinoxaline ring is optionally substituted with fluorine, chlorine, bromine or methoxy, and the triazolo ring is optionally substituted with lower alkyl, lower perfluoroalkyl or phenyl are disclosed. These novel compounds are useful for treatment of symptoms associated with depression. Also disclosed are pharmaceutical compositions containing the novel compounds of this invention and a method of using the compounds in the treatment of depression and fatigue.Type: GrantFiled: October 10, 1984Date of Patent: October 15, 1985Assignee: Pfizer Inc.Inventor: Reinhard Sarges
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Patent number: 4495187Abstract: A series of novel [1,2,4]triazolo[4,3-a]quinoxaline-4-amine derivatives wherein the amine group is optionally substituted with lower alkyl, phenylalkyl having up to three carbon atoms in the alkyl moiety or alkanoyl having from two to five carbon atoms, or the amine group alternatively completes a piperazino ring, the quinoxaline ring is optionally substituted with fluorine, chlorine, bromine or methoxy, and the triazolo ring is optionally substituted with lower alkyl, lower perfluoroalkyl or phenyl are disclosed. These novel compounds are useful for treatment of symptoms associated with depression. Also disclosed are pharmaceutical compositions containing the novel compounds of this invention and a method of using the compounds in the treatment of depression and fatigue.Type: GrantFiled: September 2, 1983Date of Patent: January 22, 1985Assignee: Pfizer Inc.Inventor: Reinhard Sarges
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Patent number: 4476307Abstract: Certain substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones are highly potent gabaergic agents, valuable in the treatment of individuals suffering from schizophrenia or reversing the side effects of a previously or concurrently administered neuroleptic agent; or in the treatment of epilepsy. A wider class of substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones, together with 1-phenyl-3-(2-pyrrolidinylidene)-2(1H,3H)-indolones, and homologs thereof, are valuable in the treatment of anxiety.Type: GrantFiled: September 20, 1982Date of Patent: October 9, 1984Assignee: Pfizer Inc.Inventors: Harry R. Howard, Jr., Reinhard Sarges
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Patent number: 4474967Abstract: The 8-deutero, and 8-tritio-substituted derivatives of D-4S-6-fluoro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione (sorbinil) have been prepared. These compounds all have the 4S-configuration and are of value in the field of medicinal chemistry as aldose reductase inhibitors for the control of chronic diabetic complications. The labeled 8-deutero and 8-tritio derivatives are useful in metabolism pharmacokinetic studies and in binding studies with the drug in animals and man. The 8-halo derivatives are useful as intermediates for the labeled forms of the drug, in addition to being potent aldose reductase inhibitors per se. Methods for the preparation of these compounds are provided in some detail.Type: GrantFiled: April 27, 1983Date of Patent: October 2, 1984Assignee: Pfizer Inc.Inventor: Reinhard Sarges
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Patent number: 4471124Abstract: A series of spiro-imide compounds and their base salts with pharmacologically acceptable cations are disclosed. These particular compounds are useful in therapy as agents for the control of certain chronic diabetic complications. Preferred member compounds include 2,3-dihydro-spiro-[1H-indene-1,3'-pyrrolidone]-2', 5'-dione, 2,3-dihydro-spiro-[1H-indene-2,3'-pyrrolidine]-2',5'-dione, 3,4-dihydro-spiro-[2H-naphthalene-1,3'-pyrrolidine]-2',5'-dione, 3,4-dihydro-spiro-[2H-naphthalene-1,3'-piperidine]-2', 6'-dione, 6-chloro-2,3-dihydro-spiro-[4H-1-benzopyran-4,3'-pyrrolidine]-2',5'-dione and 6,7-dihydro-spiro-[5H-benzo(b)thiophene-4,3'-pyrrolidine]-2',5'-dione. Methods for preparing these compounds from known starting materials are provided.Type: GrantFiled: December 22, 1983Date of Patent: September 11, 1984Assignee: Pfizer Inc.Inventors: John L. Belletire, Reinhard Sarges
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Patent number: 4442114Abstract: A series of spiro-imide compounds and their base salts with pharmacologically acceptable cations are disclosed. These particular compounds are useful in therapy as agents for the control of certain chronic diabetic complications. Preferred member compounds include 2,3-dihydro-spiro-[1H-indene-1,3'-pyrrolidone]-2',5'-dione, 2,3-dihydro-spiro-[1H-indene-2,3'-pyrrolidine]-2',5'-dione, 3,4-dihydro-spiro-[2H-naphthalene-1,3'-pyrrolidine]-2',5'-dione, 3,4-dihydro-spiro-[2H-naphthalene-1,3'-piperidine]-2',6'-dione, 6-chloro-2,3-dihydro-spiro-[4H-1-benzopyran-4,3'-pyrrolidine]-2',5'-dione and 6,7-dihydro-spiro-[5H-benzo(b)thiophene-4,3'-pyrrolidine]-2',5'-dione. Methods for preparing these compounds from known starting materials are provided.Type: GrantFiled: January 17, 1983Date of Patent: April 10, 1984Assignee: Pfizer Inc.Inventors: John L. Belletire, Reinhard Sarges
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Patent number: 4419521Abstract: A novel process for the synthesis of chiral hydantoins of the structure ##STR1## wherein X is fluoro or chloro, from the corresponding 6-halo-4-chromanone of the structure ##STR2## is described. The compounds I are valuable in the treatment of certain chronic complications arising from diabetes mellitus. In addition the compound of the formula I wherein X is chloro possesses complementary hypoglycemic activity.The process comprises the sequence of dehydrative coupling of the halochromanone (II) with S-(-)-alpha-methylbenzylamine to form the imine of structure ##STR3## addition of hydrogen cyanide to form the nitrile of structure ##STR4## condensation with chlorosulfonylisocyanate (or its equivalent) to form the alpha-methylbenzylhydantoin of structure ##STR5## and finally solvolysis of the latter to the chiral hydantoin of structure I.Type: GrantFiled: June 17, 1982Date of Patent: December 6, 1983Assignee: Pfizer Inc.Inventor: Reinhard Sarges