Abstract: R.sup.1 is hydrogen, halogen or C.sub.1 to C.sub.4 alkyl;R.sup.2 is hydrogen or C.sub.1 to C.sub.4 alkyl; and Ar is phenyl or phenyl substituted with one or more substituents selected from C.sub.1 to C.sub.4 alkyl, halo, trifluoromethyl, nitro, hydroxyl, halophenyl, or C.sub.1 to C.sub.4 alkoxy.The compounds are useful in treating inflammation or other prostaglandin or leukotriene mediated diseases.
Abstract: A new acidic polycyclic antibiotic UK-61,689 has the formula: ##STR1## or a pharmaceutically acceptable cationic salt thereof. The antiobiotic and its cationic salts are active against a variety of microorganisms and are effective in controlling coccidiosis, enteritis and swine dysentery as well as being effective in promotion of growth and/or improving efficiency of feed utilization in swine and ruminants.
Type:
Grant
Filed:
December 6, 1988
Date of Patent:
March 27, 1990
Assignee:
Pfizer Inc.
Inventors:
Alexander C. Goudie, Nigel D. A. Walshe
Abstract: A compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is hydrogen; R.sup.2 is (C.sub.1 -C.sub.15) alkyl, (C.sub.3 -C.sub.15)alkenyl, phenyl, substituted phenyl, (C.sub.7 -C.sub.20)-phenylalkyl, or substituted (C.sub.7 -C.sub.20)phenylalkyl wherein the substituents on the substituted phenyl and substituted phenylalkyl are independently one or two of fluoro, chloro, (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3 alkoxy, and trifluoromethyl; or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a pyrrolodinyl, substituted pyrrolidinyl, piperidyl or substituted piperidyl group, wherein the substituents on said substituted pyrrolidinyl and piperidyl groups are independently one of (C.sub.1 -C.sub.6)alkyl, phenyl, and (C.sub.7 -C.sub.9)phenylalkyl; and R.sup.3 is hydrogen, (C.sub.1 -C.sub.6)alkyl, phenyl, substituted phenyl, (C.sub.7 -C.sub.9)phenylalkyl, or substituted (C.sub.7 -C.sub.
Type:
Grant
Filed:
June 28, 1988
Date of Patent:
March 20, 1990
Assignee:
Pfizer Inc.
Inventors:
Frederick J. Walker, John L. LaMattina, Brian T. O'Neill
Abstract: An antibiotic has been isolated from fermentation of a new Streptomyces culture. The new ionophore is active as an antibacterial and anticoccidial agent.
Type:
Grant
Filed:
February 29, 1988
Date of Patent:
March 13, 1990
Assignee:
Pfizer Inc.
Inventors:
Walter P. Cullen, John R. Oscarson, Junsuke Tone, Hiroshi Maeda
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:
February 27, 1989
Date of Patent:
February 27, 1990
Assignee:
Pfizer Inc.
Inventors:
Yoshihiko Kitaura, Fumitaka Ito, Rodney W. Stevens, Nobuko Asai
Abstract: This invention relates to a process for the production of phthalazineacetic acid ester derivatives of the formula ##STR1## wherein R is (C.sub.1 -C.sub.4) alkyl which comprises reacting (Z)-3-oxo-1(3H)-isobenzofuranylideneacetic acid with hydrazine in the presence of a solvent; reacting the resulting mixture of the novel compound 1-hydrazino-1,2,3,4-tetrahydro-4-oxo-phthalazineacetic acid and 3,4-dihydro-4-oxo-phthalazineacetic acid with acid in the presence of a solvent; and reacting the resulting 3,4-dihydro-4-oxo-phthalazineacetic acid with acid in the presence of an alcohol.This invention also relates to the novel compound 1-hydrazino-1,2,3,4-tetrahydro-4-oxo-phthalazineacetic acid of the formula ##STR2## which is an intermediate formed in the process of this invention and which is useful for the production of phthalazineacetic acid ester derivatives of formula IV. The compounds of formula IV are useful for the preparation of certain heterocyclic oxophthalazinyl acetic acids and esters thereof.
Abstract: 4-Aryl-2,6-disubstituted-3,5-dicarbamyl-1,4-dihydropyridines and 4-Aryl-2,6-disubstituted-3-alkoxycarbonyl-5-carbamyl-1,4-dihydropyridines as antiallergy and antiinflammatory agents.
Abstract: A pressure regulator including high and low pressure chambers separated by a divider having an opening, a closing member biassed to a closing position for closing the opening with a biassing force according to a desired pressure differential between the chambers, and a damping device for damping the resulting force on the closing member. There is also disclosed a fluid drainage system having a suction chamber with a suction regulator, and various arrangements of diaphragms for measuring pressure differentials. An anti-spill device for the draining system is disclosed as well.
Type:
Grant
Filed:
December 27, 1988
Date of Patent:
February 20, 1990
Assignee:
Pfizer Inc.
Inventors:
Nicholas F. D'Antonio, Nicholas J. D'Antonio
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 materials are provided.
Abstract: A process for the preparation of oxophthalazinyl acetic acids having benzothiazole or other heterocyclic side chains comprising reacting an oxophthalizinyl acetic acid ester with an aniline derivative is disclosed. Also disclosed are processes for the preparation of such oxopthalizinyl esters.
Type:
Grant
Filed:
May 19, 1989
Date of Patent:
February 13, 1990
Assignee:
Pfizer Inc.
Inventors:
Banavara L. Mylari, William J. Zembrowski
Abstract: A series of novel heterobicyclic substituted 2-(1H)-quinolone compounds have been prepared, including the 3,4-dihydro derivatives thereof, wherein the heterobicyclic ring moiety is an optionally-substituted indolyl, phthalizinyl, benzimidazolyl, imidazopyridinyl, quinolinyl or isoquinolinyl group attached by an nitrogen or carbon atom of said group to the 6-position of the quinolone ring. The optional substituent is a C.sub.1 -C.sub.14 alkyl group located on either of the two heterobicyclic rings and/or an oxo group situated on the heterocyclic portion of said heterobicyclic ring system. These particular compounds are useful in therapy as cardiac stimulants and therefore, are of value in the treatment of various cardiac conditions. 6-{1(H)-Imidazo[4,5-b]pyridin-6-yl}-8-methyl-2-(1H)-quinolone represents a typical and preferred member compound. Methods for preparing these compounds from known starting materials are provided.
Type:
Grant
Filed:
April 21, 1988
Date of Patent:
February 6, 1990
Assignee:
Pfizer Inc.
Inventors:
Simon F. Campbell, David S. Morris, David A. Roberts
Abstract: A forceps for use in orthopedic surgical procedures having readily interchangeable tip elements and a reversible ratchet mechanism, for controlling the tip elements. A variety of tips for compression and distraction are provided. The ratchet mechanism permits controlled increments of force to be applied to the tips.
Type:
Grant
Filed:
February 5, 1988
Date of Patent:
January 30, 1990
Assignee:
Pfizer, Inc.
Inventors:
Roy Bogert, Michael W. Chapman, Charles C. Edwards, Dana C. Mears
Abstract: Compositions for the controlled and prolonged release of macromolecular compounds comprise a porous matrix of chitosan having dispersed therein the macromolecular compound. Examples of macromolecules used in the composition are pharmacologically active ones such as peptide hormones, e.g. growth hormone.
Type:
Grant
Filed:
June 7, 1985
Date of Patent:
January 23, 1990
Assignee:
Pfizer Inc.
Inventors:
John R. Cardinal, William J. Curatolo, Charles D. Ebert
Abstract: An efficient, multistep process for the synthesis of 6-(1-hydroxyethyl) 2-thio-substituted penem antibiotics from 2-[4R-(triphenylmethy lthio)-3S-(1S-(dimethyl-t-butylsilyloxy)ethyl)-2-azetidon-1-yl]acetic acid esters.
Abstract: Processes and intermediates for preparing 1,4-diazabicyclo[3.2.2.]nonane including a process for the preparation of a compound of the formula ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkyl substituted with 1 to 6 halo groups; and R.sup.2 is hydrogen, naphthoyl, substituted naphthoyl, benzyl, substituted benzyl, benzoyl or substituted benzoyl, wherein each of said substituted naphthoyl, substituted benzyl, and substituted benzoyl is substituted with one to three substituents selected from the group consisting of halo, C.sub.1 -C.sub.4 alkoxy and C.sub.1 -C.sub.4 alkyl, comprising reacting a compound of the formula ##STR2## wherein R.sup.1 and R.sup.3 are independently selected from C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkyl substituted with 1 to 6 halo groups with an alkyl stannane or a trialkyl aluminum and, if desired, reacting the resulting compound of the formula III wherein R.sup.
Type:
Grant
Filed:
October 25, 1988
Date of Patent:
January 23, 1990
Assignee:
Pfizer Inc.
Inventors:
Robert C. Friedmann, John W. Lackey, Brian T. O'Neill
Abstract: Amides of L-aspartyl-D-amino acid dipeptides of the formula ##STR1## and physiologically acceptable cationic and acid addition salts thereof wherein R.sup.a is methyl, ethyl, n-propyl or isopropyl; R is a branched member selected from the group consisting of fenchyl, diisopropylcarbinyl, d-methyl-t-butylcarbinyl, d-ethyl-t-butylcarbinyl, di-t-butylcarbinyl, 2-methylthio-2,4-dimethylpentan-3-yl, ##STR2## where at least one of R.sup.3, R.sup.4, R.sup.5, R.sup.6 is alkyl having from one to four carbon atoms and the remainder are hydrogen or alkyl having from one to four carbon atoms, X is O, S, SO, SO.sub.2 C.dbd.O or CHOH; m is zero or 1-4, n and p are each zero, 1, 2 or 3 where the sum of n+p is not greater than 3 and the sum of the carbon atoms in R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is not greater than six, and when both of R.sup.3 and R.sup.4 or R.sup.5 and R.sup.6 are alkyl they are methyl or ethyl, ##STR3## where one of R.sup.7, R.sup.8, R.sup.
Abstract: A two component binder system comprising a highly dispersible, high specific surface area precipitated calcium carbonate (colloidal PCC) and a cationic starch, especially a cationic potato starch, for improving filler retention, opacity and strength during papermaking.
Abstract: 1,4-Dihydropyridine anti-ischaemic and antihypertensive agent of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is 2-chlorophenyl, 2,3-dichlorophenyl or 2-chloro-3-trifluoromethylphenyl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl;X is O or S;R.sup.3 is H or C.sub.1 -C.sub.4 alkyl; andR.sup.4 is 1,2,4-triazol-1-ylmethyl, imidazol-1-ylmethyl, azidomethyl, 2,4,5-trimethylimidazol-1-ylmethyl, 3,4-dihydro-4-oxopyrimidin-2-ylthiomethyl, pyrimidin-2-ylthiomethyl; pyrimidin-2-ylaminomethyl, 3,4-dihydro-4-oxopyrimidin-2-ylaminomethyl, 2-aminopyrimidin-4-yloxymethyl, methoxymethyl, 2-furyl, 2-pyridylmethyl, imidazol-2-yl, hydroxymethyl, aminomethyl, 1,2,4-triazol-4-ylmethyl or 2-hydroxyethyl, and intermediates leading thereto.
Type:
Grant
Filed:
November 2, 1987
Date of Patent:
January 9, 1990
Assignee:
Pfizer Inc.
Inventors:
David Alker, Simon F. Campbell, Peter E. Cross
Abstract: An antiarrhythmic agent of the formula ##STR1## or a pharmaceutically acceptable salt thereof; wherein R.sup.1 is H, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy;X is O, ##STR2## or a direct link; and R.sup.2 and R.sup.3, which are the same or different, are each C.sub.1 -C.sub.4 alkyl, with the proviso that when X is ##STR3## R.sup.2 and R.sup.3 are the same.