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: The present invention relates to certain antibiotic compounds, designated N787-182 compounds herein and derivatives thereof, which are antiparasitic agents, active against insect pests, acari, free-living nematodes and endo- and ectoparasites. This invention also relates to pharmaceutical and other compositions containing such compounds, methods of using such compounds, the microorganism Streptomyces hygroscopicus ATCC 53718 and mutants or genetically transformed or recombinant form thereof, and processes for producing such compounds.
Type:
Grant
Filed:
November 7, 1995
Date of Patent:
November 12, 1996
Assignee:
Pfizer Inc.
Inventors:
Mark A. Haxell, David A. Perry, Hiroshi Maeda, Junsuke Tone
Abstract: Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of formula (I) and the pharmaceutically-acceptable salts thereof, wherein X.sup.1 is alkoxy or halosubstituted alkoxy; X.sup.2 is hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, halosubstitued alkyl, halosubstituted alkoxy, alkylamino, dialkylamino, alkylsulfonylamino (which may be substituted), N-alkyl-N-alkylsulfonylamino (which may be substituted), alkanoylamino (which may be substituted) or N-alkyl-N-alkanoylamino (which may be substituted); Ar.sup.1 and Ar.sup.2 are each, independently, thienyl, phenyl, fluorophenyl, chlorophenyl or bromophenyl; A is Y--(CH.sub.2).sub.m --CH(R.sup.2)--(CH.sub.2).sub.n --NR.sup.1 --; R.sup.1 is hydrogen, alkyl, benzyl or --(CH.sub.2).sub.p --Y; R.sup.2 is hydrogen, alkyl (which may be substituted), benzyl, 4-hydroxybenzyl, 3-indolylmethyl or --(CH.sub.2).sub.p --Y; Y is --CN, --CH.sub.
Abstract: The invention provides antifungal compounds of the formula: ##STR1## and pharmaceutical salts thereof, whereinR is phenyl substituted by 1 to 3 substituents each independently selected from halo, --CF.sub.3 and --OCF.sub.3 ;R.sup.1 is C.sub.1 -C.sub.4 alkyl;R.sup.2 is H or C.sub.1 -C.sub.4 alkyl;X is CH or N; andY is F or Cl.
Abstract: Streptomyces avermitilis lacking branched-chain 2-oxo acid dehydrogenase activity and avermectin B O-methyltransferase activity, method for preparation thereof, and use thereof to produce natural and non-natural B avermectins useful as parasiticides.
Type:
Grant
Filed:
May 23, 1995
Date of Patent:
October 15, 1996
Assignee:
Pfizer Inc.
Inventors:
Edmund W. Hafner, Kelvin S. Holdom, S. Edward Lee
Abstract: Compounds of the formula ##STR1## the pharmaceutically acceptable salts thereof wherein R.sup.2, R.sup.3, R.sup.4, m, X and Q are as defined below, and novel intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.
Abstract: Antipsychotic compounds having the formula ##STR1## wherein R is hydrogen, acyl or substituted acyl; and a pharmaceutically acceptable acid addition salt thereof.
Type:
Grant
Filed:
March 24, 1994
Date of Patent:
October 15, 1996
Assignee:
Pfizer Inc.
Inventors:
Gene M. Bright, Kishor A. Desai, Thomas F. Seeger, Teresa A. Smolarek
Abstract: Macrolides of formula (I) and methods of treatment of resistance to transplantation, fungal infections and auto-immune diseases such as rheumatoid arthritis and psoriasis using said macrolides of formula (I), ##STR1## wherein n is 1 or 2; A and B are taken together and form .dbd.O or A and B are taken separately and are each H or A is OH and B is H; R.sup.1 is a desosamino group; R.sup.2 is OH or a desosaminyloxy group; and R.sup.3 is an alkyl or allyl group.
Abstract: This invention relates to catechol diether compounds which are inhibitors of tumor necrosis factor (TNF). The catechol diether compounds are useful as inhibitors of TNF per se and in the treatment or alleviation of inflammatory conditions or disease, including but not limited to rheumatoid arthritis, osteoarthritis, asthma, bronchitis, chronic obstructive airways disease, psoriasis, allergic rhinitis, dermatitis and inflammatory bowel disease, sepsis, septic shock, tuberculosis, graft versus host disease and cachexia associated with AIDS or cancer. This invention also relates to pharmaceutical compositions useful therefor.
Abstract: A process for the synthesis of peracyl-1-O-steroidal-.beta.-cellobiosides that provides excellent .beta.-anomeric selectivity without the use of a metal salt promoter. The process comprises reacting heptaacyl-.beta.-D-cellobiosyl-1-fluoride and a trisubstituted silyl-3-O-steroid, wherein the steroid is tigogenin, hecogenin, 11-ketotigogenin or diosgenin in the absence of a metal salt under suitable conditions.
Type:
Grant
Filed:
December 20, 1994
Date of Patent:
October 8, 1996
Assignee:
Pfizer Inc.
Inventors:
Kathleen D. Goggin, John F. Lambert, Stanley W. Walinsky
Abstract: A post-foaming gel shaving composition is disclosed which contains from about 40 to about 90 percent by weight water; from about 4 to about 25 percent by weight water-soluble soap; from about 0.5 to about 12 percent by weight aliphatic liquid post-foaming agent selected from the group consisting of saturated aliphatic hydrocarbons; from about 0.01 to about 5 percent by weight of at least one water-soluble gelling agent forming in said composition a gel having a yield value sufficiently high to restrain said composition from foaming for at least about 60 seconds; and from about 0.1 to about 2 percent by weight of a poly(ethylene oxide) having an average molecular weight of at least 2.times.10.sup.5.
Type:
Grant
Filed:
June 1, 1995
Date of Patent:
October 1, 1996
Assignee:
Pfizer Inc.
Inventors:
Barbara A. Hartmann, Athanasios S. Ladas, Dino G. Muccia
Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, X and n are as defined in the claims and the pharmaceutically acceptable salts thereof are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting hypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of dihalogenated intermediate is also disclosed.
Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, X and n are as defined in the claims and the pharmaceutically acceptable salts thereof are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting hypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of dihalogenated intermediate is also disclosed.
Abstract: Avermectin and milbemycin derivatives of formula (I) ##STR1## having a double bond at the 3-4 position and a cyano substituent at the 3-position have outstanding anthelmintic properties. They may be prepared by allowing an avermectin or milbemycin derivative having a leaving group at the 5-position, or having double bonds at the 2-3 and 4-5 positions and no substituent at the 5-position, to react with an ionic cyanide.
Abstract: A device for the non-invasive measurement of the concentration of a specific analyte, particularly glucose, in arterial blood flowing in a patient's body part, which device comprises a solid first portion having a surface profile adapted to be held against the selected body part, a source of near infrared radiation mounted in a second portion associated with said first portion such that near infrared radiation is transmitted through or reflected from said body part, a third portion containing a detector and filters to receive radiation transmitted through or reflected from said body part, to select signals generated by the pulsatile component of the absorption spectrum and to provide a ratio representative of the desired concentration. A method for the determination of glucose concentration in arterial blood is also disclosed.
Abstract: Benzopyran and other benzo-fused leukotriene B.sub.4 antagonists have the formula ##STR1## wherein R.sup.1 is a phenyl or substituted phenyl group, and A, n, R.sup.2 and R.sup.3 are as defined herein.
Abstract: Certain novel isoxazoline compounds having the ability to inhibit the 5-lipoxygenase enzyme and having formula (I), ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.4 alkyl or --NR.sub.3 R.sub.4 ; R.sub.3 and R.sub.4 are each independently H or C.sub.1 -C.sub.4 alkyl; M is H or a pharmaceutically acceptable cation; A is C.sub.1 -C.sub.6 alkylene, C.sub.2 -C.sub.6 alkenylene or C.sub.2 -C.sub.6 alkynylene; Ar is phenylene or mono-, di- or tri-substituted phenylene wherein the substituents are each independently selected from halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy; n is an integer of 0 or 1; Y is H or C.sub.1 -C.sub.4 alkyl; R.sub.2 is C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.4 arylalkyl or C.sub.2 -C.sub.4 arylalkenyl; and said aryl and each aryl moiety in said arylalkyl and arylalkenyl may be substituted by from one to three substituents independently selected from halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halosubstituted C.sub.1 -C.sub.4 alkyl, halosubstituted C.sub.1 -C.sub.
Abstract: The borane reduction of prochiral ketones to optically pure alcohols is effectively achieved by the utilization of catalytic amounts of the new and valuable oxazaborolidine catalysts of formula (I).
Abstract: Compounds of this formula ##STR1## are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.
Type:
Grant
Filed:
January 9, 1995
Date of Patent:
September 3, 1996
Assignee:
Pfizer Inc
Inventors:
Kimberly O. Cameron, Paul A. Dasilva Jardine, Robert L. Rosati