Abstract: An improved condensation process for preparing N-[4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenylidene]methanamine from 4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenone and methylamine is disclosed. The process involves the use of a hydratable molecular sieve having a pore size that is at least about three Angstrom units in diameter as the dehydrating agent (catalyst) in a reaction-inert aprotic organic solvent. The ketimine final product so produced is known to be useful as an intermediate leading to cis-(1S)(4S)-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthal enamine (sertraline), which is an anti-depressant agent.
Abstract: Racemic and chiral (2R,4R)-4-c-hydroxy-2-4-(substituted)chroman(and thiochroman)-4-acetic acids and their pharmaceutically acceptable salts, their use in the treatment of diabetic complications and intermediates therefor.
Abstract: Compounds of the formula ##STR1## where R.sup.1 is lower alkyl, R.sup.2 is chlorophenyl, Y is alkylene, X is heterocyclic and Z is a fused ring are useful as antiinflammatory and antiallergy agents.
Type:
Grant
Filed:
July 11, 1988
Date of Patent:
August 1, 1989
Assignee:
Pfizer Inc.
Inventors:
Kelvin Cooper, Peter E. Cross, Michael J. Fray, Kenneth Richardson
Abstract: This invention relates to the use of certain 3-substituted-2-oxindole-1-carboxamides of the formula ##STR1## and the pharmaceutically-acceptable base salts thereof wherein X is H, Cl or F; Y is H or Cl; and R is benzyl or thienyl to suppress T-cell function in a mammal. This invention also relates to the use of such compounds for treating T-cell mediated autoimmune disorders of the systemic or organ specific type. The methods of this invention comprise administering a T-cell function suppressing amount of the compounds and salts of this invention to such a mammal.
Abstract: Compounds of the formula: ##STR1## where R is substituted phenyl, R.sup.1 is alkyl or pyridyl, R.sup.2 is hydrogen, R.sup.3 is alkoxy, alkylamino, hydroxy or benzyloxy, Y is alkylene and X is heterocyclic as antiallergic and antiinflammatory agents.
Type:
Grant
Filed:
May 24, 1988
Date of Patent:
July 25, 1989
Assignee:
Pfizer Inc.
Inventors:
Kelvin Cooper, Michael J. Fray, Kenneth Richardson
Abstract: When an aqueous system containing dissolved oxygen and erythorbate or ascorbate is passed through an activated carbon bed, the oxygen is removed at ambient temperatures. This method of oxygen removal finds practical application in the removal of oxygen from boiler condensate, low temperature boiler feedwater and oil well injection water or brine.
Abstract: A sensor for determining the partial pressure of carbon dioxide in a liquid, which comprises a carbon dioxide - permeable, liquid and ion-impermeable membrane enveloping an aqueous medium containing an absorber, a fluorescer and a source of bicarbonate ions, which medium exhibits variations in pH as a function of the partial pressure of dissolved carbon dioxide, the ratio of absorber to fluorescer and the characteristics of the absorption spectrum of the absorber and the excitation and emission spectra of the fluorescer being such that the partial pressure of carbon dioxide in the liquid may be determined from the pH of the aqueous medium as measured by the intensity of the fluorescent emission of the fluorescer.
Type:
Grant
Filed:
August 17, 1987
Date of Patent:
July 25, 1989
Assignee:
Pfizer Hospital Products Group, Inc.
Inventors:
Richard S. Matthews, Frederick E. Witherell, Jr.
Abstract: Peptides useful as antiinfective agents, immunomodulators for stimulation of host defenses in patients with an increased risk of bacterial infections, intermediates and process therefor.
Abstract: Boric acid or aluminum salts, especially aluminum chloride, aluminum sulfate and aluminum nitrate and hydrates of said salts, are superior catalysts for preparation of 3-amino-2,2,4,4-tetramethylthietane via the Leuckart reaction.
Abstract: Variously substituted trans-3-[3-(3-hydroxypiperid-2-yl)-2-oxopropyl]quinazoline-4(3H)-ones, a method of controlling or preventing coccidiosis in poultry therewith, intermediates therefor, and a process for the preparation of certain intermediates thereof.
Abstract: N-Demethylefrotomycin, a valuable new antibiotic substance, is produced by the microbial conversion of mocimycin using a novel, efrotomycin-producing, microbial species ATCC 53758.
Type:
Grant
Filed:
April 18, 1988
Date of Patent:
July 11, 1989
Assignee:
Pfizer Inc.
Inventors:
Martin R. Jefson, Jeiji Kaneda, Satoshi Nishiyama, Junsukse Tone
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 where Q.sub.
Type:
Grant
Filed:
August 9, 1984
Date of Patent:
June 20, 1989
Assignee:
Pfizer Inc.
Inventors:
James F. Eggler, Michael R. Johnson, Lawrence Sherman
Abstract: An improved process for preparing (4S)-6-fluorospiro-[chroman-4,4'-imidazolidine]-2',5'-dione (sorbinil) or its (2R)-methyl derivative (2-methylsorbinil) is disclosed herein, starting from p-fluorophenol in each instance. The final products obtained have known pharmaceutical value as agents for the control of certain chronic diabetic complications. Key steps concerned with the process involve converting p-fluorophenol into the appropriate .beta.-(4-fluorophenoxy)alkane halide, followed by amidoalkylation with N-benzoyl or N-(lower alkanoyl)-.alpha.-hydroxyglycine to form an intermediate 2-amidoalkylated derivative thereof, and then dehydration and spiroalkylation of said intermediate by treatment with a dehydrating agent and a base to yield a spiroalkylated azlactone compound.
Abstract: A novel three-step process for preparing 4-(3,4-dichlorophenyl)-4-phenylbutanoic acid is disclosed, which involves (1) reducing 4-(3,4-dichlorophenyl)-4-ketobutanoic acid to 4-(3,4-dichlorophenyl)-4-hydroxybutanoic acid; (2) then converting the intermediate hydroxy acid formed in the first step to 5-(3,4-dichlorophenyl)-dihydro-2(3H)-furanone, and (3) thereafter reacting the resulting gamma-butyrolactone compound with benzene in a Friedel-Crafts type reaction to form the desired final product. The latter compound is known to be useful as an intermediate leading to 4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenone and ultimately, to cis-(1S)(4S)-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthal ene amine (sertraline), which is known to be a preferred anti-depressant agent in the field of medicinal chemistry. The aforementioned 5-(3,4-dichlorophenyl)-dihydro-2(3H)-furanone and 4-(3,4-dichlorophenyl)-4-hydroxybutanoic acid are both novel compounds.
Type:
Grant
Filed:
June 16, 1988
Date of Patent:
June 13, 1989
Assignee:
Pfizer, Inc.
Inventors:
George J. Quallich, Michael T. Williams
Abstract: There is disclosed a bone cement composition comprising (a) a liquid component comprising a monomer of an acrylic ester and (b) a powdered component comprising, based on the weight of the powdered component,(i) from 0 to about 20 percent of a methyl methacrylate homopolymer,(ii) from about 30 to about 60 percent of a methyl methacrylate-styrene copolymer, and(iii) from about 30 to about 60 percent of a methyl methacrylate-butyl methacrylate copolymer.
Abstract: A series of novel heterocyclic-substituted 2-(1H)-quinolone compounds have been prepared, including the 3,4-dihydro derivatives thereof, wherein the heterocyclic ring moiety is a pyrrolyl, imidazolyl, pyrazolyl, triazolyl or tetrazolyl group attached by a nitrogen atom of said group to the 5-, 6-, 7- or 8-positions of the quinolone ring. These particular compounds are useful in therapy as highly potent inotropic agents and therefore, are of value in the treatment of various cardiac conditions. Preferred member compounds include 6-(2,4-dimethylimidazol-1-yl)-8-methyl-2-(1H)-quinolone, 6-(2,4-dimethyl-5-nitroimidazol-1-yl)-8-methyl-2-(1H)-quinolone, 8-methyl-6-(tetrazol-1-yl)-2-(1H)-quinolone, 8-methyl-6-(1,2,4-triazol-4-yl)-2-(1H)-quinolone, and 6-(4-cyano-2-methylimidazol-1-yl)-8-methyl-2-(1H)-quinolone, respectively. Methods for preparing these compounds from known starting material are provided.
Abstract: An improved metallic bone prosthesis having a porous coating for bone ingrowth or interlocking with bone cement is disclosed. The porous coating comprises two layers of generally ball-shaped metallic particles bonded together at their points of contact, e.g. by sintering, and defining between them a plurality of connected interstitial pores having an average pore size of from about 350 microns to about 500 microns. A high resistance to failure at the coating-substrate and bone-coating (or cement-coating) interfaces is achieved with the use of the improved prosthesis. Also disclosed are a novel method for affixing the porous coating to a metal substrate, and a knee joint prosthesis having bearing portions designed so that the function of said prosthesis closely approximates that of the natural knee.
Abstract: Compounds of the formula ##STR1## where Y is alkyl, aryl or heterocyclic, n is 1-7, R is hydrogen, alkyl, aralkyl or carboxymethyl, R.sub.1 is acetoxy, thiophenoxy, hydrogen, halo, alkyl, alkoxy or trifluoromethyl, R.sub.2 is hydrogen, alkyl or alkanoyl and X is C.dbd.O, CH.sub.2, NH, O or S as antiallergy and antiinflammatory agents.
Type:
Grant
Filed:
December 7, 1987
Date of Patent:
May 30, 1989
Assignee:
Pfizer Inc.
Inventors:
Yoshihiko Kitaura, Fumitaka Ito, Rodney W. Stevens, Nobuko Asai
Abstract: A cardiac antiarrhythmic agent of the formula: ##STR1## or a pharmaceutically acceptable salt thereof; wherein R is R.sup.3 SO.sub.2 NH--, R.sup.3 CONH-- or R.sup.1 R.sup.2 NSO.sub.2 --;R.sup.1 and R.sup.2 are each independently H or C.sub.1 -C.sub.4 alkyl;R.sup.3 is C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl or --NR.sup.1 R.sup.2 where R.sup.1 andR.sup.2 are as defined above; andHet is either (a) a 2-, 3- or 4-pyridyl group optionally substituted by a C.sub.1 -C.sub.4 alkyl or an amino group, or (b) a 2-imidazolyl group optionally substituted by one or two C.sub.1 -C.sub.4 alkyl groups.
Abstract: An antibiotic complex, containing three major components, has been isolated from fermentations of a new strain of the microorganism Streptomyces hirsutus. The major components are new, neutral, macrolide antibiotic compounds, which are useful as antibacterial agents against certain gram-positive bacteria.
Type:
Grant
Filed:
December 5, 1986
Date of Patent:
May 30, 1989
Assignee:
Pfizer Inc.
Inventors:
Walter P. Cullen, James R. Hauske, Hiroshi Maeda, Junsuke Tone