Patents by Inventor Gerald F. Holland
Gerald F. Holland 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: 5223522Abstract: Hypoglycemic thiazolidine-2,4-dione derivatives of the formula ##STR1## wherein the dotted line represents a bond or no bond;A and B are each independently CH;X is S, SO, SO.sub.2, CH.sub.2, CHOH or CO;n is 0 or 1;Y is CHR.sup.1 or NR.sup.2, with the proviso that when n is 1 and Y is NR.sup.2, X is SO.sub.2 or CO;Z is CHR.sup.3, CH.sub.2 CH.sub.2, CH.dbd.CH, ##STR2## OCH.sub.2, SCH.sub.2, SOCH.sub.2 or SO.sub.2 CH.sub.2 ; R, R.sup.1, R.sup.2 and R.sup.3 are each independently hydrogen or methyl; andX.sup.1 and X.sup.2 are each independently hydrogen, methyl, trifluoromethyl, phenyl, benzyl, hydroxy, methoxy, phenoxy, benzyloxy, bromo, chloro or fluoro;a pharmaceutically-acceptable cationic salt thereof; ora pharmaceutically-acceptable acid addition salt thereof.Type: GrantFiled: March 24, 1992Date of Patent: June 29, 1993Assignee: Pfizer Inc.Inventors: David A. Clark, Steven W. Goldstein, Gerald F. Holland, Bernard Hulin, James P. Rizzi
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Patent number: 5120754Abstract: Hypoglycemic thiazolidine-2,4-dione derivatives of the formula ##STR1## wherein the dotted line represents a bond or no bond; A and dB are each independently CH or N, with the proviso that when A or B is N, the other is CH;X is S, SO, SO.sub.2, CH.sub.2, CHOH or CO;n is 0 or 1;Y is CHR.sup.1 or NR.sup.2, with the proviso that when n is 1 and Y is NR.sup.2, X is SO.sub.2 or CO;Z is CHR.sup.3, CH.sub.2 CH.sub.2, CH.dbd.CH, ##STR2## OCH.sub.2, SCH.sub.2, SOCH.sub.2 or SO.sub.2 CH.sub.2 ; R, R.sup.1, R.sup.2 and R.sup.3 are each independently hydrogen or methyl; andX.sup.1 and X.sup.2 are each independently hydrogen, methyl, trifluoromethyl, phenyl, benzyl, hydroxy, methoxy, phenoxy, benzyloxy, bromo, chloro or fluoro; a pharmaceutically-acceptable cationic salt thereof; or a pharmaceutically-acceptable acid addition salt thereof when A or B is N.Type: GrantFiled: April 3, 1991Date of Patent: June 9, 1992Assignee: Pfizer Inc.Inventors: David A. Clark, Steven W. Goldstein, Gerald F. Holland, Bernard Hulin, James P. Rizzi
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Patent number: 5061717Abstract: Hypoglycemic thiazolidine-2,4-dione derivatives of the formula ##STR1## wherein the dotted line represents a bond or no bond; A and B are each independently CH or N, with the proviso that when A or B is N, the other is CH;X is S, SO, SO.sub.2, CH.sub.2, CHOH or CO;n is 0 or 1;Y is CHR.sup.1 or NR.sup.2, with the proviso that when n is 1 and Y is NR.sup.2, X is SO.sub.2 or CO;Z is CHR.sup.3, CH.sub.2 CH.sub.2, CH.dbd.CH, ##STR2## OCH.sub.2, SCH.sub.2, SOCH.sub.2 or SO.sub.2 CH.sub.2 ; R, R.sup.1, R.sup.2 and R.sup.3 are each independently hydrogen or methyl; andX.sup.1 and X.sup.2 are each independently hydrogen, methyl, trifluoromethyl, phenyl, benzyl, hydroxy, methoxy, phenoxy, benzyloxy, bromo, chloro or fluoro; a pharmaceutically-acceptable cationic salt thereof; or a pharmaceutically-acceptable acid addition salt thereof when A or B is N.Type: GrantFiled: August 14, 1990Date of Patent: October 29, 1991Assignee: Pfizer Inc.Inventors: David A. Clark, Steven W. Goldstein, Gerald F. Holland, Bernard Hulin, James P. Rizzi
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Patent number: 4738972Abstract: Hypoglycemic 5-[1-(5,6,7,8-tetrahydro-2-napthyl-; 1,2,3,4-tetrahydro-6-quinolyl-; 2-indanyl-; and 2-indolyl)alkyl]thiazolidine-2,4-dione derivatives, pharmaceutically acceptable salts thereof, and a method for their use in the treatment of hyperglycemic mammals.Type: GrantFiled: June 26, 1987Date of Patent: April 19, 1988Assignee: Pfizer Inc.Inventors: James F. Eggler, Gerald F. Holland, Michael R. Johnson, Robert A. Volkmann
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Patent number: 4703052Abstract: Hypoglycemic 2,3-dihydro-5-benzo[b]furanyl-2,3-dihydro-5-benzo[b]thienyl-, 3,4-dihydro(2H)-6-benzopyranyl- and 6-thiochromanyl-thiazolidine-2,4-diones and pharmaceutically acceptable salts thereof, method for their use in treatment of hyperglycemic animals and pharmaceutical compositions containing them.Type: GrantFiled: December 29, 1986Date of Patent: October 27, 1987Assignee: Pfizer Inc.Inventors: James F. Eggler, Gerald F. Holland, Mickael R. Johnson, Robert A. Volkmann
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Patent number: 4511575Abstract: Certain pyrrolecarboxylic and pyrroleacetic acid derivatives substituted on the pyrrole ring with thioether groups, acyl groups, phenyl, substituted phenyl, phenoxy, substituted phenoxy, benzyl or halo and optionally substituted on the pyrrole nitrogen with alkyl, and the pharmaceutically acceptable salts thereof, are useful in lowering the blood glucose levels of hyperglycemic animals.Type: GrantFiled: August 9, 1982Date of Patent: April 16, 1985Assignee: Pfizer Inc.Inventor: Gerald F. Holland
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Patent number: 4511576Abstract: Certain pyrrolecarboxylic and pyrroleacetic acid derivatives substituted on the pyrrole ring with thioether groups, acyl groups, phenyl, substituted phenyl, phenoxy, substituted phenoxy, benzyl or halo and optionally substituted on the pyrrole nitrogen with alkyl, and the pharmaceutically acceptable salts thereof, are useful in lowering the blood glucose levels of hyperglycemic animals.Type: GrantFiled: August 10, 1982Date of Patent: April 16, 1985Assignee: Pfizer Inc.Inventor: Gerald F. Holland
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Patent number: 4454320Abstract: A process for the preparation of certain 5-substituted dialuric acids, compounds having utility as intermediates for the synthesis of certan hypoglycemic 5-substituted oxazolidine-2,4-diones.Type: GrantFiled: July 28, 1980Date of Patent: June 12, 1984Assignee: Pfizer Inc.Inventors: Faustas J. Rajeckas, Gerald F. Holland
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Patent number: 4430337Abstract: Hypoglycemic oxazolidine-2,4-diones, substituted at the 5-position with a (C.sub.5 -C.sub.9) unsaturated monocyclic, saturated bicyclic or unsaturated bicyclic hydrocarbon radical; methods for their preparation; and method for their use in the treatment of hyperglycemic mammals.Type: GrantFiled: June 23, 1982Date of Patent: February 7, 1984Assignee: Pfizer Inc.Inventor: Gerald F. Holland
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Patent number: 4377521Abstract: Certain mono- and disubstituted-5-sulfamylbenzoic acids, many of which are novel, and their use in lowering blood lipid levels in mammals.Type: GrantFiled: January 4, 1980Date of Patent: March 22, 1983Assignee: Pfizer Inc.Inventor: Gerald F. Holland
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Patent number: 4351843Abstract: Certain pyrrolecarboxylic and pyrroleacetic acid derivatives substituted on the pyrrole ring with thioether groups, acyl groups, phenyl, substituted phenyl, phenoxy, substituted phenoxy, benzyl or halo and optionally substituted on the pyrrole nitrogen with alkyl, and the pharmaceutically acceptable salts thereof, are useful in lowering the blood glucose levels of hyperglycemic animals.Type: GrantFiled: April 23, 1981Date of Patent: September 28, 1982Assignee: Pfizer Inc.Inventor: Gerald F. Holland
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Patent number: 4282246Abstract: Compounds of the structure ##STR1## wherein Z is oxygen or sulfur;R is (C.sub.1 -C.sub.2)alkoxy;phenoxy;benzyl;phenylthiomethyl;phenylthio;phenylthio monosubstituted in the 2-, 3- or4-position with (C.sub.1 -C.sub.3)alkyl, phenyl, methoxy, chloro, fluoro or trifluoromethyl;phenylthio disubstituted in the 2,5- or 3,5- positions with methyl, methoxy, chloro, or fluoro;2,3,5,6-tetrafluorophenylthio;1- or 2-naphthylthio;(C.sub.2 -C.sub.6)alkylthio; orhalo (bromo or chloro); andthe pharmaceutically-acceptable salts thereof are useful in lowering the blood glucose levels of hyperglycemic mammals.Type: GrantFiled: March 7, 1980Date of Patent: August 4, 1981Assignee: Pfizer Inc.Inventor: Gerald F. Holland
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Patent number: 4282242Abstract: Certain pyrrolecarboxylic and pyrroleacetic acid derivatives substituted on the pyrrole ring with thioether groups, acyl groups, phenyl, substituted phenyl, phenoxy, substituted phenoxy, benzyl or halo and optionally substituted on the pyrrole nitrogen with alkyl, and the pharmaceutically acceptable salts thereof, are useful in lowering the blood glucose levels of hyperglycemic animals.Type: GrantFiled: March 7, 1980Date of Patent: August 4, 1981Assignee: Pfizer Inc.Inventor: Gerald F. Holland
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Patent number: 4252957Abstract: Heterocyclylcarbonyl derivatives of urea having the formula ##STR1## wherein R is a heterocyclyl group; and R.sub.1 and R.sub.2 when taken together with the nitrogen to which they are attached are morpholino, thiomorpholino or a 6-8 membered nitrogen containing heterocyclic ring; methods for their preparation and use as agents for dissolving gallstones.Type: GrantFiled: September 14, 1979Date of Patent: February 24, 1981Assignee: Pfizer Inc.Inventor: Gerald F. Holland
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Patent number: 4163784Abstract: Heterocyclylcarbonyl derivatives of urea having the formula ##STR1## wherein R is a heterocyclyl group; R.sub.1 is hydrogen, alkyl having up to ten carbon atoms or phenyl; R.sub.2 is R.sub.1, 1-naphthyl and phenylalkyl having 1 to 4 carbon atoms in the alkyl group; and R.sub.1 and R.sub.2 when taken together with the nitrogen to which they are attached are morpholino, thiomorpholino or a 6-8 membered nitrogen containing heterocyclic ring; methods for their preparation and use as agents for dissolving gallstones.Type: GrantFiled: March 9, 1978Date of Patent: August 7, 1979Assignee: Pfizer Inc.Inventor: Gerald F. Holland
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Patent number: 4138399Abstract: Certain mono- and disubstituted-5-sulfamylbenzoic acids, many of which are novel, and their use in lowering blood lipid levels in mammals.Type: GrantFiled: June 1, 1977Date of Patent: February 6, 1979Assignee: Pfizer Inc.Inventor: Gerald F. Holland
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Patent number: 4136180Abstract: Method for lowering blood lipid levels in mammals, using certain derivatives of N-carbamoyl-2-phenylethenesulfonamide, many of which are novel.Type: GrantFiled: September 12, 1977Date of Patent: January 23, 1979Assignee: Pfizer Inc.Inventor: Gerald F. Holland
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Patent number: 4124590Abstract: Certain mono- and disubstituted-S-sulfamylbenzoic acids, many of which are novel, and their use in lowering blood lipid levels in mammals.Type: GrantFiled: August 11, 1976Date of Patent: November 7, 1978Assignee: Pfizer Inc.Inventor: Gerald F. Holland
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Patent number: 4062960Abstract: Method for lowering blood lipid levels in mammals, using certain derivatives of N-carbamoyl-2-phenylethenesulfonamide, many of which are novel.Type: GrantFiled: May 24, 1976Date of Patent: December 13, 1977Assignee: Pfizer Inc.Inventor: Gerald F. Holland
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Patent number: 3984409Abstract: Compounds of the formulae: ##SPC1##And ##SPC2##And the salts thereof with pharmaceutically acceptable cations wherein n and m are each two or three; X is oxygen or sulphur; R.sup.2 and R.sup.3, when taken separately, are each hydrogen or alkyl having 1 to 4 carbon atoms; R.sup.2 and R.sup.3, when taken together, are alkylene having 2 to 4 carbon atoms; Y is methylene or a single bond; R.sup.4 and R.sup.5, when taken separately, are each hydrogen, hydroxy or alkoxy having 1 to 5 carbon atoms, and R.sup.4 and R.sup.5, when taken together, are oxo or alkylene dioxy having 2 to 4 carbon atoms, each oxygen atom in R.sup.4 and R.sup.5, when taken separately, and in R.sup.4 and R.sup.5, when taken together, being separated from the nitrogen atom of the heterocyclic ring by two or more carbon atoms, said compounds being cerebral vasodilators.Type: GrantFiled: October 4, 1974Date of Patent: October 5, 1976Assignee: Pfizer Inc.Inventor: Gerald F. Holland