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
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:
March 19, 1992
Date of Patent:
March 23, 1993
Assignee:
Pfizer Inc.
Inventors:
Nicholas A. Saccomano, Fredric J. Vinick
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: A process and intermediates for the manufacture of S-3-methylheptanoic acid from S-citronellol; a novel crystallline form of immunoregulatory N-(S-3-methylheptanoyl)-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: A process for preparing 3,4,6-trifluorophthalonitrile from 3,4,5,6-tetrachlorophthalonitrile comprising the sequential steps of reductively dechlorinating the tetrachlorophthalonitrile, in the presence of a metal in an aqueous acidic medium, to produce 3,4,6-trichlorophthalonitrile and then subjecting the trichlorophthalonitrile to a chlorine-fluorine exchange by reaction with a fluoride source in a polar aprotic solvent.
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: Hypoglycemic thiazolidine-2,4-dione derivatives ##STR1## wherein the dotted line represents a bond or no bond;V is --CH.dbd.CH--, --N.dbd.CH--, --CH.dbd.N-- or S;W is CH.sub.2, CHOH, CO, C.dbd.NOR or --CH.dbd.CH--;X is S, O, NR.sup.1, --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, naphthyl, 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 is hydrogen or methyl; andn is 1, 2 or 3;a pharmaceutically acceptble cationic salt thereof; or a pharmaceutically acceptable acid addition salt thereof when the compound contains a basic nitrogen.
Type:
Grant
Filed:
March 26, 1991
Date of Patent:
July 14, 1992
Assignee:
Pfizer Inc.
Inventors:
David A. Clark, Steven W. Goldstein, Bernard Hulin
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; and Y comprises a 5-membered heterocyclic ring having one or two nitrogens.
Type:
Grant
Filed:
May 30, 1991
Date of Patent:
July 7, 1992
Assignee:
Pfizer Inc.
Inventors:
Nicholas A. Saccomano, Fredric J. Vinick
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
Abstract: A new acidic polycyclic ether antibiotic UK-58,852 has the formula: ##STR1## wherein R and R.sup.1 are both hydrogen, and can be prepared by the submerged aerobic propagation in aqueous nutrient media of Actinomadura sp. ATCC 39697. The antibiotic and its cationic salts are active against a variety of microorganisms and are effective in controlling coccidiosis, enteritis, swine dysentery and theileriosis as well as being effective in promotion of growth and/or improving efficiency of feed utilization in swine and ruminants. Two minor components, wherein R is H and R.sup.1 is CH.sub.3 and wherein R and R.sup.1 are both CH.sub.3, have also been isolated from the fermentation.
Type:
Grant
Filed:
December 17, 1990
Date of Patent:
March 31, 1992
Assignee:
Pfizer Inc.
Inventors:
Walter P. Cullen, Hiroshi Maeda, John C. Ruddock, Junsuke Tone
Abstract: A new acidic polycyclic antibiotic UK-61,689 has the formula: ##STR1## or a pharmaceutically acceptable cationic salt thereof. The antibiotic and its cationic salts are active against a variety of microorganisms and are effective in controlling coccidiosis, enteritis and swine dysentery as well as being effective in promotion of growth and/or improving efficiency of feed utilization in swine and ruminants.
Type:
Grant
Filed:
December 17, 1990
Date of Patent:
March 10, 1992
Assignee:
Pfizer Inc.
Inventors:
Alexander C. Goudie, Nigel D. A. Walshe
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: Certain 7-beta-[2-(2-amino-4-thiazolyl)-(Z)-2-(chloromethylene acetamido]-3-[(substituted)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: Improved processes for preparation of racemic, cis- and optically active (3S,4R)-3[1(R)-t-butyl-dimethylsilyloxy)-ethyl]-4-[1-oxo-3-thiolanylthio(t hiocarbonyl)thio]azetidin-2-ones, process improvements for certain intermediates therefor and a novel intermediate for said racemic, cis- and trans-compounds, which compounds are useful as intermediates for antibacterial 5R,6S-6-[1(R)-hydroxyethyl]-2-(1-oxo-3-thiolanylthio)-2-penem-3-carboxylic acids and the pharmaceutically-acceptable salts and the pivaloyloxymethyl esters thereof.
Type:
Grant
Filed:
January 18, 1991
Date of Patent:
December 24, 1991
Assignee:
Pfizer Inc.
Inventors:
Frank R. Busch, Robert W. Dugger, George J. Quallich
Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Streptomyces sp. ATCC 53862. This novel antibiotic is useful as an anticoccidial in chickens, in the prevention or treatment of swine dysentery, and as a growth promotant in cattle and swine.
Type:
Grant
Filed:
January 28, 1991
Date of Patent:
November 12, 1991
Assignee:
Pfizer Inc.
Inventors:
Walter P. Cullen, James R. Hauske, Gloria J. Kostek, Hiroshi Maeda, Junsuke Tone
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
Abstract: An improved method of operating a membrane separation system is provided, which comprises applying a reduced pressure to one side of the or each membrane to thereby cause fluid to be drawn through the or each membrane from the other side thereof.As the method does not utilize fluid under pressure, which has typically been required in prior art procedures, the risk of damage to the membranes is eliminated, or at least minimized.
Abstract: An improved separation system and its method of operation for the separation of solutes, colloidal particles, or suspended matter from solutions of suspensions containing the same is disclosed. In a preferred embodiment, this invention relates to a simple and economic membrane filtration system that can be operated in many of the modes of operation of a membrane filtration system, especially suction backwashing, without mixing the filtrate with the feed stream.