Abstract: This invention relates to compounds of the formula ##STR1## wherein Q, Z, D, E, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined as below, and the pharmaceutically acceptable salts thereof are disclosed. The compounds are useful as antihypertensive agents.
Type:
Grant
Filed:
March 8, 1993
Date of Patent:
August 15, 1995
Assignee:
Pfizer Inc.
Inventors:
Dennis J. Hoover, Bruce A. Lefker, Robert L. Rosati
Abstract: The invention provides the substantially geometrically and optically pure trans-stereoisomeric form of a compound of formula (I): ##STR1## wherein R.sup.1 is H or C.sub.1 -C.sub.4 alkyl, together with processes for its preparation. The compounds are intermediates for the preparation of the antidepressant agent known as sertraline.
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: Certain 3-(phenyl, chroman-2-yl, benzofuran-5-yl or benzoxazol-5-yl)-2-(hydroxy or mercapto)propionic acid derivatives and analogs are useful as hypoglycemic and hypocholesterolemic agents.
Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, fluoro, chloro, bromo, nitro, trifluoromethyl, C.sub.1 to C.sub.4 alkoxy, C.sub.1 to C.sub.4 alkylthio or C.sub.1 to C.sub.6 alkyl and R.sup.2 is a group of the formula ##STR2## wherein R.sup.3 is hydrogen or C.sub.1 to C.sub.6 alkyl, R.sup.4 is --CH.dbd.C.sub.2, --CH.sub.2 --YR.sup.5, or --COR.sup.6, R.sup.5 is hydrogen or an acid labile alcohol protecting group, Y is oxygen or sulfur, and R.sup.6 is --NR.sup.7 R.sup.8 or --OR.sup.9 wherein R.sup.7, R.sup.8 and R.sup.9 are independently selected from hydrogen or C.sub.1 to C.sub.6 alkyl, or an alkaline or alkaline earth metal salt thereof, which are intermediates in the preparation of hydantoin aldose reductase inhibitors and methods of preparing these intermediates.
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 are disclosed.
Abstract: Compounds of the formula ##STR1## which are intermediates in the preparation of 4,5-difluoroanthranilic acid, an intermediate itself in the synthesis of quinolone antibacterials, and methods of preparing these intermediates.
Abstract: The use of rapamycin prodrugs of formula I as immunosuppressant agents, intermediates formed in the preparation of its prodrugs as well as the prodrugs themselves.
Abstract: A device for the controlled delivery of an insoluble or partially aqueous insoluble beneficial agent to an aqueous containing environment. The device comprises a shaped wall that surrounds and defines an internal reservoir. The wall is formed at least in part of a sintered polymer microporous membrane permeable to a beneficial agent-containing hydrophobic medium when the wall is present in the aqueous containing environment. The reservoir contains a mixture of a hydrophilic swellable composition and a beneficial agent-containing hydrophobic medium.
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: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof are selective cGMP PDE inhibitors which are useful in the treatment of such diseases and adverse conditions as angina, hypertension, congestive heart failure, reduced blood vessel patency, peripheral vascular disease, stroke, bronchitis, chronic asthma, allergic asthma, allergic rhinitis, glaucoma, and diseases characterized by disorders of gut motility.
Abstract: Quinuclidine derivatives of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein m, P, Z, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined below. The compounds are substance P antagonists and, therefore, are useful in treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases, pain and migraine.
Abstract: Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein: Y is a direct link, --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.sub.2 O-- or --CH.sub.2 S--; R is --CN or --CONH.sub.2 ; and R.sup.1 is ##STR2## where X and X.sup.1 are each independently O or CH.sub.2 ; and m is 1, 2 or 3, are muscarinic receptor antagonists useful in the treatment of diseases and conditions associated with the altered motility and/or tone of smooth muscle, such as irritable bowel syndrome.
Abstract: This invention relates to with a novel synthesis of (R)-2-benzylsuccinic acid 4-[4-(N-t-butoxycarbonyl-methylamino)-piperidine]amide from racemic intermediates. The racemic (R)-2-benzylsuccinic acid 4-[4-(N-t-butoxycarbonyl-methylamino)piperidine]amine is resolved through the formation of diasteromic salts with (S)-cyclohexylethylamine or (R)-cyclohexylethylamine. The pure diasteromic salt can be subsequently hydrolyzed with dilute acid to yield the pure enantiomer of (R)-2-benzylsuccinic acid 4-[4-(N-t-butoxycarbonyl-methylamino) piperidine]amide.
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: This invention relates to novel pyrimido-benzothiazine derivative compounds. ##STR1## The compounds of the present invention inhibit the action of the lipoxygenase enzyme and are useful in the treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals. This invention also relates to pharmaceutical compositions comprising such compounds.
Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Actinomadura sp. ATCC 55080. This novel antibiotic is useful as an anticoccidial in poultry, in the prevention and treatment of swine dysentery and as a growth promotant in cattle and swine.
Type:
Grant
Filed:
March 12, 1993
Date of Patent:
May 23, 1995
Assignee:
Pfizer Inc
Inventors:
Walter P. Cullen, John P. Dirlam, Hiroshi Maeda, Junsuke Tone
Abstract: A method and apparatus for preparing a planar surface on the distal femur prior to implantation of a femoral knee prosthesis has a femoral plate with an opening therein for exposing both condyles of the femur. A guide with a central aperture is used to align the femoral plate on the distal femur. The guide is releasably secured to the femoral plate and an intramedullary guide rod is placed through the aperture therein and into the intramedullary canal of the femur. After alignment with the intramedullary canal, the femoral plate is pinned to the femur and the rod and guide are removed. A milling guide having two bores, one adjacent each condyle, is then placed on the femoral plate and an end mill is used to mill a planar surface on at least one of the condyles.