Abstract: Certain 1-substituted 4-(1,2-benzisoxazolyl)-piperidine compounds exhibit neuroleptic activity and are useful in the treatment of psychosis and anxiety.
Abstract: Compounds of the formula ##STR1## wherein X is --CH.sub.2 --, --O-- or --S--, m is 1 to 3, n is 1 or 2 and R.sub.1 is hydrogen, C.sub.1 to C.sub.4 alkyl, aryl or aryl substituted with one or more substituents selected independently from the group consisting of halogen, nitro, cyano, C.sub.1 to C.sub.10 alkyl, C.sub.1 to C.sub.10 halosubstituted alkyl, C.sub.1 to C.sub.6 alkoxy, alkoxycarbonyl having from one to ten carbon atoms in the alkoxy moiety, aminocarbonyl, alkylaminocarbonyl having from one to ten carbon atoms in the alkyl moiety and dialkylaminocarbonyl having from one to ten carbon atoms in each of the alkyl moieties, and the pharmaceutically acceptable salts thereof, inhibit the enzyme lipoxygenase and are useful in treating allergy and inflammatory and cardiovascular conditions for which the action of lipoxygenase has been implicated. These compounds form the active ingredient in pharmaceutical compositions for treating such conditions.
Abstract: A process and intermediates for the manufacture of S-3-methylheptanoic acid from S-citronellol; a novel crystalline form of immunoregulatory N-(S-3-methlylheptanoyl)-D-gamma-glutamyl-glycyl-D-alanine, an immunoregulatory agent; and an improved process and intermediates therefor.
Abstract: 1S,4S and 1R,4R-2-Alkyl-2,5-diazabicyclo[2.2.1]heptanes useful as intermediates in the synthesis of certain antibacterial quinolones, are prepared respectively, from trans-4-hydroxy-L-proline and trans-4-hydroxy-D-proline via multistep procedures.
Abstract: 3-Piperidino-1-chromanol derivatives and analogs having the formula ##STR1## wherein A and B are taken together and are --CH.sub.2 CH.sub.2 -- or A and B are taken separately and are each H;X is CH.sub.2 or O;X.sup.1 is H or OH;Z is H, F, Cl, Br or OH;Z.sup.1 is H, F, Cl, Br or (C.sub.1 -C.sub.3)alkyl;n is 0 or 1; andm is 0 or an integer from 1 to 6;pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.
Abstract: Hypoglycemic thiazolidine-2,4-dione derivatives of the formula ##STR1## wherein the dotted line represents a bond or no bond;V is --CH.dbd.CH--, --N.dbd.CH--, --CH.dbd.N--, S, O or NR;W is S, SO, SO.sub.2, SO.sub.2 NR.sup.1, NR.sup.1 SO.sub.2, CONR.sup.1 or NR.sup.1 CO;X is S, O, NR.sup.2, --CH.dbd.N-- or --N.dbd.CH;Y is CH or N;Z is hydrogen, (C.sub.1 -C.sub.7)alkyl, (C.sub.3 -C.sub.7)cycloalkyl, phenyl, pyridyl, furyl, thienyl or phenyl mono- or disubstituted with the same or different groups which are (C.sub.1 -C.sub.3)alkyl, trifluoromethyl, (C.sub.1 -C.sub.3)alkoxy, fluoro, chloro or bromo;Z.sup.1 is hydrogen or (C.sub.1 -C.sub.3)alkyl;R, R.sup.1 and R.sup.2 are each independently hydrogen or (C.sub.1 -C.sub.4); andn is 1, 2 or 3;a pharmaceutically acceptable cationic salt thereof; or a pharmaceutically acceptable acid addition salt thereof when the compound contains a basic nitrogen.
Type:
Grant
Filed:
August 14, 1990
Date of Patent:
July 19, 1994
Assignee:
Pfizer Inc.
Inventors:
David A. Clark, Steven W. Goldstein, Bernard Hulin
Abstract: Certain 1H-indazole-3-acetic acid derivatives, and their pharmaceutically-acceptable esters and salts, are inhibitors of the aldose reductase enzyme, and so are useful in the treatment of diabetic complications.
Type:
Grant
Filed:
February 24, 1993
Date of Patent:
July 19, 1994
Assignee:
Pfizer Inc.
Inventors:
Banavara L. Mylari, William J. Zembrowski
Abstract: Intermediates and a stepwise process for the conversion of D-methionine or certain of its derivatives to optically active compounds of the formula ##STR1## wherein R is (C.sub.1 -C.sub.3)alkyl, phenyl or tolyl. The latter compounds are in turn useful as an intermediate in the preparation of penem antibiotic 5R,6S-6-(1R-hydroxyethyl)-2-(1R-oxo-3S-thiolanylthio)-2-penem-3-carboxylic acid and corresponding pharmaceutically acceptable salts and esters.
Abstract: Antibacterial compounds of the formula ##STR1## wherein n is 0 or 1, R is hydrogen or a radical forming an ester hydrolyzable under physiological conditions, and R.sup.1 is hydrogen or methyl; the pharmaceuticallyacceptable cationic salts thereof when R is hydrogen; pharmaceutical compositions thereof; a method of treating bacterial infections therewith; and intermediates useful in the synthesis of said compounds.
Abstract: A method of producing analgesia and treating antiinflammatory disease in a human subject while avoiding proteinuria by administering 6-chloro-5-fluoro-3-(2-thenoyl)-2-oxindole-1-carboxamide or a pharmaceutically-acceptable base salt thereof.
Type:
Grant
Filed:
January 22, 1993
Date of Patent:
March 29, 1994
Assignee:
Pfizer Inc.
Inventors:
Kelvin Cooper, Bruce H. Littman, Christopher J. Pazoles, Keith D. Wilner
Abstract: Antidepressant agents having the formula ##STR1## wherein R.sup.1 is a polycycloalkyl group; R.sup.2 is methyl or ethyl, X is O or NH; and Y comprises a 5- or 6-membered heterocyclic ring having one or two nitrogens; or fused bicyclic heterocyclic rings having a total of three nitrogen atoms, one in each ring and one angular nitrogen.
Type:
Grant
Filed:
November 20, 1992
Date of Patent:
March 15, 1994
Assignee:
Pfizer Inc.
Inventors:
Nicholas A. Saccomano, Fredric J. Vinick
Abstract: Immunoregulatory N-(S-3-alkyl-4-heptenoyl)- and N-(S-3-alkylheptanoyl)-D-gamma-glutamyl-glycyl-D-alanine and esters thereof are synthesized via R-trans-2-hexen-4-ols, R-3-alkyl-4-heptanoic acid and S-3-alkylheptanoic acid.
Abstract: An efficient, multistep process for the synthesis of certain 6-(1-hydroxyethyl) 2-substituted penem antibiotics from 2-[4R-(triphenylmethylthio)-3S-(1R-(dimethyl-t-butylsilyloxy)ethyl)-2-azet idon-1-yl]acetic acid esters.
Abstract: Antiinflammatory and analgesic oxindole prodrugs of the formula ##STR1## wherein R.sup.10, R.sup.11, R.sup.12 and R.sup.13 are hydrogen, alkyl or halogen and R is methyleneoxyalkanoyl, methyleneoxyalkenoyl or alkenoyl.
Type:
Grant
Filed:
January 26, 1993
Date of Patent:
December 14, 1993
Assignee:
Pfizer, Inc.
Inventors:
Wayne E. Barth, Kelvin Cooper, Edward F. Kleinman, Lawrence A. Reiter, Ralph P. Robinson
Abstract: A process and intermediates for the manufacture of S-3-methylheptanoic acid from S-citronellol; a novel crystalline form of immunoregulatory N-(S-3-methylheptanoyl)-D-gamma-glutamyl-glycyl-D-alanine, an immunoregulatory agent; and an improved process and intermediates therefor.
Abstract: Immunoregulatory N-(S-3-alkyl-4-heptenoyl)- and N-(S-3-alkylheptanoyl)-D-gamma-glutamyl-glycyl-D-alanine and esters thereof are synthesized via R-trans-2-hexen-4-ols, R-3-alkyl-4-heptenoic acid and S-3-alkylheptanoic acid.
Abstract: Certain 7-beta-[2-(2-amino-4-thiazolyl)-(Z)-2-(chloromethylene)acetamido]-3-[(subs tituted)methyl]-ceph-3-em-4-carboxylic acids, pharmaceutically-acceptable salts thereof and conventional in vivo hydrolyzable esters thereof are valuable as broad spectrum antibacterial agents, particularly useful for the treatment of bacterial infections in man and other mammals.
Abstract: Abstract Certain 1H-indazole-3-acetic acid derivatives, and their pharmaceutically-acceptable esters and salts, are inhibitors of the aldose reductase enzyme, and so are useful in the treatment of diabetic complications.
Type:
Grant
Filed:
October 11, 1991
Date of Patent:
August 17, 1993
Assignee:
Pfizer Inc.
Inventors:
Banavara L. Mylari, William J. Zembrowski