Abstract: Tricyclic oxindole carboxamides, prepared by (a) reaction of an isocyanate with the basic ring system or (b) ammonolysis of a corresponding alkyl ester, are non-steroidal antiinflammatory agents useful in the treatment of rheumatoid arthritis.
Abstract: Hypoglycemic 5-furyl and 5-thienyl derivatives of oxazolidine-2,4-dione and the pharmaceutically-acceptable salts thereof; certain 3-acylated derivatives thereof; and intermediates useful in the preparation of said compounds.
Abstract: Hypoglycemic 5-chromanyl, 2,3-dihydro-5-benzo[b]-furanyl, 5-pyridyl, 5-quinolyl, 5-pyrrolyl, 5-indolyl, 5-thiazolyl, 5-oxazolyl, 5-isothiazolyl and 5-isoxazolyl oxazolidine-2,4-diones and the pharmaceutically-acceptable salts thereof; certain 3-acylated derivatives thereof; a method of treating hyperglycemic animals therewith; and intermediates useful in the preparation of said compounds.
Abstract: Ketone containing 1-substituted oxindole-3-carboxamides as antiinflammatory agents prepared by reaction of the 1-substituted oxindole with an isocyanate or by aminolysis of the corresponding alkyl oxindole-3-carboxylate.
Abstract: 7.alpha.-Hydroxyamino-7.beta.-[2-substituted-2-(acylamino)acetamido]cephalo sporin antibiotics, pharmaceutically-acceptable salts and in vivo hydrolyzable esters thereof, a method of treating susceptible infections therewith, and intermediates therefor.
Type:
Grant
Filed:
March 5, 1986
Date of Patent:
August 4, 1987
Assignee:
Pfizer Inc.
Inventors:
Colin W. Greengrass, David W. T. Hoople, Thomas T. Howarth
Abstract: 7.alpha.-Hydroxyamino-7.beta.-[2-substituted-2-(acylamino)acetamido]-cephal osporin antibiotics, pharmaceutically-acceptable salts and in vivo hydrolyzable esters thereof, a method of treating susceptible infections therewith, and intermediates therefor.
Type:
Grant
Filed:
June 27, 1985
Date of Patent:
August 4, 1987
Assignee:
Pfizer Inc.
Inventors:
Colin W. Greengrass, David W. T. Hoople, Thomas T. Howarth
Abstract: Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 and Q.sub.
Type:
Grant
Filed:
August 9, 1984
Date of Patent:
July 14, 1987
Assignee:
Pfizer Inc.
Inventors:
James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
Abstract: Compounds of the general formula: ##STR1## wherein Ar is naphthyl, biphenylyl, phenyl or substituted phenyl; n is 0, 1 or 2; and Het is a heterocyclic group which may optionally be substituted or fused to a phenyl, substituted phenyl or further heterocyclic ring; and their pharmaceutically acceptable salts are antifungal agents useful in combatting fungal infections in animals, including humans.
Abstract: 4-(S)-8-(.omega.-carboxy-1-oxoalkylamino) derivatives of sorbinil useful as ligands for affinity chromatographic purification of aldose reductase; methods for their preparation and use for the above-mentioned purpose.
Abstract: An improved antiinflammatory composition and method of treating inflammation which employs a combination of antiinflammatory piroxicam, or a pharmaceutically acceptable salt thereof, with analgesis acetaminophen, antidepressant doxepin, bronchodilator pirbuterol, minor tranquilizer diazepam, or antihypertensive trimazosin.
Type:
Grant
Filed:
January 21, 1986
Date of Patent:
June 9, 1987
Assignee:
Pfizer Inc.
Inventors:
Thomas C. Crawford, Stanley L. Keely, David L. Larson, Joseph G. Lombardino, James J. Maciejko
Abstract: Dihydropyridine anti-ischaemic agents of the formula: ##STR1## and their salts where R is aryl or heteroaryl, R.sup.1 and R.sup.2 are each C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl, Y is --(CH.sub.2).sub.n -- where n is 2, 3, or 4 and is optionally substituted by 1 or 2 CH.sub.3 groups, and R.sup.3 is an optionally substituted 5- or 6-membered heterocyclic group attached to the adjacent N atom by a C atom, said group R.sup.3 being optionally fused to a further heterocyclic group or to a benzene ring.
Type:
Grant
Filed:
February 14, 1986
Date of Patent:
June 2, 1987
Assignee:
Pfizer Inc.
Inventors:
Simon F. Campbell, Peter E. Cross, John K. Stubbs, John E. Arrowsmith
Abstract: Racemic endo- and exo-1-methoxybicyclo[2.2.2]oct-5-ene-2-carboxylic acids are starting materials for a novel and efficient synthesis of chiral 3R-[2-hydroxy-4-(1,1-dimethylheptyl)phenyl]-4R-(3-hydroxypropyl)-1R-cycloh exanol, a compound having valuable central nervous system (CNS) activity, particularly as an analgesic and as an antiemetic.
Abstract: Compounds of the general formula: ##STR1## wherein R is naphthyl, biphenylyl, phenyl or substituted phenyl; n is 0, 1 or 2; and R.sup.1 is H, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-4 alkanoyl, or C.sub.1-2 alkyl substituted by C.sub.2-4 alkenyl with the provisos that when R.sup.1 is H or C.sub.2-4 alkanoyl, n is 0; and when n is 2, R.sup.1 is C.sub.1-3 alkyl; and their pharmaceutically acceptable salts are antifungal agents useful in combatting fungal infections in animals, including humans.
Abstract: Topical vaginal forms of tioconazole and related antimicrobic compounds, especially miconazole, econazole, clotrimazole, butaconazole and ketoconazole, are useful for the control (chemotherapeutic and chemoprophylactic) of Herpes virus infections.
Abstract: Dihydropyridine Anti-ischaemic agents of the formula ##STR1## and their salts where R is aryl, R.sup.1 and R.sup.2 are each C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl, Y is --(CH.sub.2).sub.n -- where n is 2, 3 or 4 and is optionally substituted by 1 or 2 methyl groups and R.sup.3 is pyrimidyl or di- or tetrahydropyrimidyl.
Type:
Grant
Filed:
February 14, 1986
Date of Patent:
April 28, 1987
Assignee:
Pfizer Inc.
Inventors:
Simon F. Campbell, Peter E. Cross, John K. Stubbs, John E. Arrowsmith
Abstract: Compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof wherein R is 2-pyridyl, 6-chloro-2-pyridyl, 6-methyl-2-pyridyl or 5-methylisoxazol-3-yl; useful as prodrug forms of the corresponding known oxicam antiinflammatory and analgesic agents, piroxicam, the corresponding 6-chloro-2-pyridyl and 6-methyl-2-pyridylcarboxamides, isoxicam and tenoxicam; methods for their use, pharmaceutical compositions containing them and a process for their preparation.
Abstract: Compounds of the formula: ##STR1## where R is an optionally substituted aryl or heteroaryl group;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl; and Y is --(CH.sub.2).sub.n -- where n is 2, 3 or 4, --CH.sub.2 CH(CH.sub.3)-- or --Ch.sub.2 C(CH.sub.3).sub.2 --; and their pharmaceutically acceptable salts.The compounds have utility as anti-ischaemic and antihypertensive agents and as synthetic intermediates to other dihydropyridine calcium antagonists.
Type:
Grant
Filed:
April 26, 1985
Date of Patent:
March 31, 1987
Assignee:
Pfizer Inc.
Inventors:
David Alker, Simon F. Campbell, Peter E. Cross
Abstract: Dihydropyridines of the formulae ##STR1## wherein R is chlorothienyl or mono- or disubstituted phenyl where said substituent is fluoro, chloro, bromo or trifluoromethyl; R.sup.1 and R.sup.2 are each alykl; R.sup.3 and R.sup.4 when taken separately are each hydrogen or alkyl; R.sup.3 and R.sup.4 when taken together with the nitrogen to which they are attached are piperidine or pyrrolidine; R.sup.5 is alkyl or 2-hydroxyethyl; R.sup.6 is hydrogen or methoxy; X and Z are each hydrogen or methoxy; Y is alkylene; R.sup.7 is chlorophenyl or trifluoromethyl-chlorophenyl; p is 0 or 1; and Q is CH or N are useful in the treatment of hypertension, heart failure and angina.
Type:
Grant
Filed:
June 5, 1985
Date of Patent:
March 3, 1987
Assignee:
Pfizer Inc.
Inventors:
John E. Arrowsmith, Simon F. Campbell, Peter E. Cross, Roger P. Dickinson