Abstract: A series of novel 2-substituted 4-amino-6,7-dimethoxyquinoline derivatives have been prepared, including their pharmaceutically acceptable acid addition salts. These particular compounds are useful in therapy as highly potent antihypertensive agents. Preferred member compounds include 4-amino-2-[4-(2-furoyl)piperazin-1-yl]-6,7-dimethoxyquinoline, 4-amino-2-[4-(1,4-benzodioxan-2-carbonyl)piperazin-1-yl]-6,7-dimethoxyquin oline and 4-amino-6,7-dimethoxy-2-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinol-2-yl)qu inoline, respectively. Methods for preparing these compounds from known starting materials are provided.
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]-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: 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: Discrete copper-nickel-tin spinodal alloy articles, such as bearings, containing from about 5 to about 35 wt. % nickel, from about 4 to about 13 wt. % tin and the balance copper are produced by processing a prealloyed alloy powder to form a green body having substantially the desired shape of, and proportionally sized to, the final article and sintering the green body in a reducing atmosphere or a vacuum at a temperature of at least 1650.degree. F. for sufficient time to achieve at least 90% of the theoretical density. The green body may be formed by either compaction or injection molding of the prealloyed powder. The resulting sintered article may be age hardened to effect a spinodal decomposition of the copper-nickel-tin alloy. The age hardened articles exhibit excellent strength properties and homogeneity while retaining significant ductility.
Abstract: Spiro-imidazolones are disclosed which are useful as aldose reductase inhibitors and as therapeutic agents for the treatment of complications arising from diabetes. Pharmaceutical compositions containing the spiro compounds and a method of treating diabetic complications are also disclosed.
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: 1-Acylcarbamoyloxindole-3-carboxamides as antiinflammatory agents prepared by reaction of the 1-acylcarbamoyloxindole with an isocyanate in the presence of a basic reagent.
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: A novel formulation of piroxicam for dermatological administration is disclosed. Pharmaceutical compositions containing piroxicam, lower alkanols, water, carboxyvinyl polymer, polyhydric alcohols, alkanolamines and optionally film-forming agents are prepared, said compositions having a pH of from about 6.5 to about 9.0. The novel formulation is characterized by excellent applicability on the skin, skin-permeability and good stability. The novel formulation, which is in gel ointment form, is as effective as orally administered peroxicam and is well suited for topical administration through skin for the treatment of various types of inflammatory conditions.
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: Novel protogynous Zea mays plants are disclosed, including a novel protogynous inbred line, LALGI. Also disclosed are a process to produce such Zea mays plants and hybrids resulting from crossing such plants with other inbred lines such as Iowa Stiff Stalk Synthetic Lines.
Abstract: A method for the treatment of gastrointestinal disorders in a patient which comprises administering to the patient a gastric anti-secretory effective amount of a 2-amino-5-hydroxy-4-methylpyrimidine or a substituted amino derivative thereof, optionally in admixture with an additional gastric anti-secretory agent.
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: A process for the preparation of a thieno-imidazole derivative, particularly descarboxybiotin, a useful intermediate for the preparation of d-biotin, which comprises reacting a thio-substituted intermediate, for example descarboxythiobiotin, with an epoxy compound in an alkanol solvent; and a process for the preparation of said intermediate by reacting a substituted imidazothiazole alcohol with anhydrous hydrogen fluoride.
Type:
Grant
Filed:
March 14, 1985
Date of Patent:
June 2, 1987
Assignee:
Pfizer Inc.
Inventors:
Gordon D. Gruetzmacher, Robert A. Volkmann
Abstract: A dispersion strengthened cobalt-chromium-molybdenum alloy produced by gas atomization containing a fine oxide dispersion, and characterized, after fabrication by gas atomization, thermomechanical processing and further high temperature exposure, by excellent corrosion resistance, high fatigue strength, high ductility and high temperature stability; a process for producing said alloy and prostheses formed from said alloy.
Type:
Grant
Filed:
August 13, 1985
Date of Patent:
May 26, 1987
Assignee:
Pfizer Hospital Products Group Inc.
Inventors:
Kathy K. Wang, Larry J. Gustavson, John H. Dumbleton
Abstract: A steerable catheter having a Doppler crystal at the tip to measure the velocity of blood in vivo--and inferentially the blood flow. The catheter includes two passageways, one passageway being exposed to the blood stream with the other passageway containing the electrical leads to the Doppler crystal. The one passageway is dimensioned for receiving a wire guide for accurately manipulating the catheter. Preferably, the catheter incorporates an inflatable angio-balloon operable to distend the blood vessel in the region of a stenosis. Thus, blood flow can be determined in the region of the stenosis before and/or after the vessel is distended. The passageways are preferably defined by a pair of generally concentric tubes with the Doppler crystal doughnut-shaped and sealingly disposed at the tip of the catheter.
Abstract: An acetabular cup assembly prosthesis comprises the combination of a support shell for introduction into an acetabulum and a socket insert in nesting engagement within the shell. The shell has a generally hemispherical outer surface and a downwardly extending concavity surrounded by a peripheral rim, At least one anchoring post secures the shell to the acetabulum, and a central opening in the bottom of the concavity serves as a connection location for the socket insert. The insert has a hemispherical concavity that articulates with the rounded head of a femoral prosthesis, while the outer surface of the insert nests within the concavity of the support shell. A central fastening tab extends from the insert into locking engagement with the opening in the support shell, and structure is provided to prevent relative rotation of the shell and insert.