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).

  • Patent number: 5223522
    Abstract: 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: Grant
    Filed: March 24, 1992
    Date of Patent: June 29, 1993
    Assignee: Pfizer Inc.
    Inventors: David A. Clark, Steven W. Goldstein, Gerald F. Holland, Bernard Hulin, James P. Rizzi
  • Patent number: 5120754
    Abstract: 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: Grant
    Filed: April 3, 1991
    Date of Patent: June 9, 1992
    Assignee: Pfizer Inc.
    Inventors: David A. Clark, Steven W. Goldstein, Gerald F. Holland, Bernard Hulin, James P. Rizzi
  • Patent number: 5061717
    Abstract: 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: Grant
    Filed: August 14, 1990
    Date of Patent: October 29, 1991
    Assignee: Pfizer Inc.
    Inventors: David A. Clark, Steven W. Goldstein, Gerald F. Holland, Bernard Hulin, James P. Rizzi
  • Patent number: 4738972
    Abstract: 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: Grant
    Filed: June 26, 1987
    Date of Patent: April 19, 1988
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Gerald F. Holland, Michael R. Johnson, Robert A. Volkmann
  • Patent number: 4703052
    Abstract: 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: Grant
    Filed: December 29, 1986
    Date of Patent: October 27, 1987
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Gerald F. Holland, Mickael R. Johnson, Robert A. Volkmann
  • Patent number: 4511575
    Abstract: 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: Grant
    Filed: August 9, 1982
    Date of Patent: April 16, 1985
    Assignee: Pfizer Inc.
    Inventor: Gerald F. Holland
  • Patent number: 4511576
    Abstract: 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: Grant
    Filed: August 10, 1982
    Date of Patent: April 16, 1985
    Assignee: Pfizer Inc.
    Inventor: Gerald F. Holland
  • Patent number: 4454320
    Abstract: 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: Grant
    Filed: July 28, 1980
    Date of Patent: June 12, 1984
    Assignee: Pfizer Inc.
    Inventors: Faustas J. Rajeckas, Gerald F. Holland
  • Patent number: 4430337
    Abstract: 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: Grant
    Filed: June 23, 1982
    Date of Patent: February 7, 1984
    Assignee: Pfizer Inc.
    Inventor: Gerald F. Holland
  • Patent number: 4377521
    Abstract: Certain mono- and disubstituted-5-sulfamylbenzoic acids, many of which are novel, and their use in lowering blood lipid levels in mammals.
    Type: Grant
    Filed: January 4, 1980
    Date of Patent: March 22, 1983
    Assignee: Pfizer Inc.
    Inventor: Gerald F. Holland
  • Patent number: 4351843
    Abstract: 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: Grant
    Filed: April 23, 1981
    Date of Patent: September 28, 1982
    Assignee: Pfizer Inc.
    Inventor: Gerald F. Holland
  • Patent number: 4282246
    Abstract: 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: Grant
    Filed: March 7, 1980
    Date of Patent: August 4, 1981
    Assignee: Pfizer Inc.
    Inventor: Gerald F. Holland
  • Patent number: 4282242
    Abstract: 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: Grant
    Filed: March 7, 1980
    Date of Patent: August 4, 1981
    Assignee: Pfizer Inc.
    Inventor: Gerald F. Holland
  • Patent number: 4252957
    Abstract: 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: Grant
    Filed: September 14, 1979
    Date of Patent: February 24, 1981
    Assignee: Pfizer Inc.
    Inventor: Gerald F. Holland
  • Patent number: 4163784
    Abstract: 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: Grant
    Filed: March 9, 1978
    Date of Patent: August 7, 1979
    Assignee: Pfizer Inc.
    Inventor: Gerald F. Holland
  • Patent number: 4138399
    Abstract: Certain mono- and disubstituted-5-sulfamylbenzoic acids, many of which are novel, and their use in lowering blood lipid levels in mammals.
    Type: Grant
    Filed: June 1, 1977
    Date of Patent: February 6, 1979
    Assignee: Pfizer Inc.
    Inventor: Gerald F. Holland
  • Patent number: 4136180
    Abstract: Method for lowering blood lipid levels in mammals, using certain derivatives of N-carbamoyl-2-phenylethenesulfonamide, many of which are novel.
    Type: Grant
    Filed: September 12, 1977
    Date of Patent: January 23, 1979
    Assignee: Pfizer Inc.
    Inventor: Gerald F. Holland
  • Patent number: 4124590
    Abstract: Certain mono- and disubstituted-S-sulfamylbenzoic acids, many of which are novel, and their use in lowering blood lipid levels in mammals.
    Type: Grant
    Filed: August 11, 1976
    Date of Patent: November 7, 1978
    Assignee: Pfizer Inc.
    Inventor: Gerald F. Holland
  • Patent number: 4062960
    Abstract: Method for lowering blood lipid levels in mammals, using certain derivatives of N-carbamoyl-2-phenylethenesulfonamide, many of which are novel.
    Type: Grant
    Filed: May 24, 1976
    Date of Patent: December 13, 1977
    Assignee: Pfizer Inc.
    Inventor: Gerald F. Holland
  • Patent number: 3984409
    Abstract: 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: Grant
    Filed: October 4, 1974
    Date of Patent: October 5, 1976
    Assignee: Pfizer Inc.
    Inventor: Gerald F. Holland