Abstract: Selective muscarinic receptor antagonists of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are both optionally substituted phenyl, the broken line is an optional bond, X is >COH--, >SiOH-- or CH-- when the double bond is absent or is >C.dbd. when the double bond is present, X being attached to a carbon atom of A, A is selected from certain piperidine and pyrrolidine groups, n is 1 to 3 and R.sup.3 is optionally substituted phenyl or thienyl, pyridyl or pyrazinyl.
Abstract: The compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein X, m, n, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined herein are useful in the treatment of shock and other TNF.alpha.-related disorders.
Abstract: Benzimidazole anthelmintic agents of the formula (I) and their non-toxic salts, wherein R.sup.1, which is in the 5(6)-position, is either H or certain stated substituents, "alk" is a methylene or ethylene group; R.sup.2 is cyano, C.sub.1 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, C.sub.2 -C.sub.4 alkanoyl, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkenoxy, aryl, heteroaryl, aryl-(C.sub.1 -C.sub.4 alkoxy) or heteroaryl-(C.sub.1 -C.sub.4 alkoxy), in which "aryl" means phenyl optionally substituted by 1 to 3 substituents each independently selected from halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulphinyl, and C.sub.1 C.sub.4 alkylsulphonyl in which "heteroaryl" means thienyl, furyl or pyridininyl all optionally substituted by 1 to 3 substituents each independently selected from halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulphinyl and C.sub.1 -C.sub.4 alkylsulphonyl; and R.sub.3 is a C.
Type:
Grant
Filed:
May 9, 1994
Date of Patent:
December 12, 1995
Assignee:
Pfizer Inc.
Inventors:
Bernard J. Banks, Christopher J. Dutton, Alexander C. Goudie
Abstract: Racemic or optically active compound of the formula ##STR1## wherein X, Y, R.sup.1 and R.sup.2 are as defined above useful in the treatment of asthma or inflammatory airway or skin diseases.
Abstract: The present invention relates to bicyclic carbamate compounds and, specifically, to compounds of the formula ##STR1## wherein X, Y, R.sup.1 and R.sup.2 are as defined in the specification. The compounds of this invention are useful in the treatment of asthma, rheumatoid arthritis, osteoarthritis, bronchitis, chronic obstructive airways disease, psoriasis, allergic rhinitis, atopic dermatitis, shock, other inflammatory diseases, and other conditions where the treatment is effected or facilitated by blocking the leukotriene D4 receptor.
Abstract: The culture ATCC 74256 and its mutants are capable of producing zaragozic acid A and other squalene synthase inhibitors.The compound of formula I herein may be prepared from culture ATCC 74256 and is useful in the treatment of fungal infections, and inhibition of squalene synthase, and protein farnesyltransferase.
Type:
Grant
Filed:
April 8, 1994
Date of Patent:
July 4, 1995
Assignee:
Pfizer Inc.
Inventors:
Thomas T. Dabrah, H. James Harwood, Jr., Liang H. Huang, Takushi Kaneko
Abstract: Compounds of the formula ##STR1## wherein ring A, ring B, ring D, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6,R.sup.11, R.sup.12, R.sup.13, E, G, X and P are as defined below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.
Abstract: An assay tray assembly and an assay tray primarily for chromatographic analysis has a plastics moulded test tray 1 mounted on a plastics moulded collection tray 72, The test tray has a spaced array of chambers 3 disposed as per a microtiter plate, Each chamber has a bottom outlet port 5 formed by a flange 8 which retains within the chamber a chromatographic medium to which test liquid deposited in the chamber is to be subjected for the percolate or eluate liquid to emerge from the respective outlet ports, The collection tray 72 has a spaced array of wells 16 disposed as per a microtiter plate to correspond with the chambers 3 and the tray 14 is mounted on the tray 72 for each chamber to communicate with a corresponding well 16. Each chamber 3 has a tubular spigot part 12 which extends into the respective well 16 to alleviate cross contamination of the liquid derived from the outlet ports 5.
Abstract: Quinolone carboxylic acids of the formula ##STR1## wherein R.sup.1, R.sup.2, A and Y are as defined herein, and R.sup.3 is ##STR2## have antibacterial properties.
Abstract: Racemic or optically active compound of the formula ##STR1## wherein X is O or NH, R.sup.1 is a (C.sub.7 -C.sub.11)polycycloalkyl group, R.sup.2 is methyl or ethyl, Y is ##STR2## R.sup.3 is hydrogen, (C.sub.1 -C.sub.3)alkyl, (C.sub.2 -C.sub.3)alkenyl, benzyl or phenethyl, and R.sup.4 is hydrogen, (C.sub.1 -C.sub.3)alkyl or (C.sub.2 -C.sub.3)alkanoyl, are useful in the treatment of asthma or inflammatory airway or skin diseases.
Abstract: A stable liquid oral prebrushing composition for loosening and removing plaque present on dental surfaces has a pH of about 7.2 to about 7.9 and comprises dialkali metal pyrophosphate salts, tetraalkali metal pyrophosphate salts or mixtures thereof, together with sodium lauryl sulfate in amounts effective for removal of plaque when the composition is applied to dental surfaces.
Type:
Grant
Filed:
June 18, 1993
Date of Patent:
August 16, 1994
Assignee:
Pfizer Inc
Inventors:
Robert E. Tricca, William T. Doran, Catherine L. Gray
Abstract: The monohydrate of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydr o-2H-indole-2-one hydrochloride has advantageous stability for formulation as a neuroleptic agent.
Type:
Grant
Filed:
September 1, 1992
Date of Patent:
May 17, 1994
Assignee:
Pfizer Inc.
Inventors:
Douglas J. M. Allen, Frank R. Busch, Sabeto A. DiRoma, Dennis M. Godek
Abstract: The following 3-carboxaldehyde quinolines and naphthyridines have antibacterial activity ##STR1## wherein A, Y, R, and R.sub.2 are as defined herein. These compounds are particularly suitable for administration by injection. A specific example of such compound is 1-cyclopropyl-6-fluoro-7-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-y l]-4-oxo-1,4-dihydroquinoline-3-carboxaldehyde.
Abstract: Azabicyclo[2.2.2]octan-3-imines of the general formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined herein are prepared by reacting a compound of the formula ##STR2## ps with a compound of the formula wherein A is MgCl, MgBr or Li.
Abstract: Oxophthalazinyl acetic acids having benzothiazole side chains are prepared by reacting an oxophthalazinyl thioacetamide acetate with hydrogen sulfide and a nitrophenyl compound having a reactive group such that the benzothiazole side chain may be formed by ring closure involving the thioacetamide group. The oxophthalazinyl thioacetamide may be prepared by reacting the corresponding cyanomethyloxophthalazinyl acetate with hydrogen sulfide in the presence of tertiary amines. Analogous indazole and oxopyridopyridazinone acetic acids may be prepared similarly, as well as oxophthalazinyl, indazole and oxopyridopyridazinone acetic acids having thiazoloyridinyl side chains.
Type:
Grant
Filed:
June 30, 1992
Date of Patent:
January 26, 1993
Assignee:
Pfizer Inc.
Inventors:
Banavara L. Mylari, William J. Zembrowski
Abstract: Oxophthalazinyl acetic acids having benzothiazole side chains are prepared by reacting an oxophthalazinyl thioacetamide acetate with hydrogen sulfide and a nitrophenyl compound having a reactive group such that the benzothiazole side chain may be formed by ring closure involving the thioacetamide group. The oxophthalazinyl thioacetamide may be prepared by reacting the corresponding cyanomethyloxophthalazinyl acetate with hydrogen sulfide in the presence of tertiary amines. Analogous indazole and oxopyridopyridazinone acetic acids may be prepared similarly, as well as oxophthalazinyl, indazole and oxopyridopyridazinone acetic acids having thiazolopyridinyl side chains.
Type:
Grant
Filed:
September 30, 1991
Date of Patent:
December 15, 1992
Assignee:
Pfizer Inc.
Inventors:
Banavara L. Mylari, William J. Zembrowski