Abstract: The invention provides a process for preparing a compound of the formula: ##STR1## or a base salt thereof, wherein R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl optionally substituted by up to 3 substituents each independently selected from the group consisting of C.sub.1 -C.sub.6 alkoxy and C.sub.1 -C.sub.6 alkoxy(C.sub.1 -C.sub.6 alkoxy)-; and R.sup.3 is C.sub.1 -C.sub.6 alkyl or benzyl, said benzyl group being optionally ring-substituted by up to 2 nitro or C.sub.1 -C.sub.4 alkoxy substituents comprising reacting a compound of the formula: ##STR2## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl, phenyl or benzyl or C.sub.1 -C.sub.4 alkoxy; and R.sup.2 and R.sup.3 are as previously defined for a compound of the formula (I), with hydrogen peroxide or a source of peroxide ions: said process being optionally followed by conversion of the compound of the formula (I) to a base salt thereof. The present invention also relates to novel compounds of the formula (II).
Abstract: Process for the production of 5-fluoro-6-chlorooxindole, (III), which is useful in the synthesis of certain analgesic and antiinflammatory agents, via two different synthetic pathways.Compounds of formula (I) and (II) shown below ##STR1## which are intermediates in the process of this invention.
Abstract: A series of cis-3-[(cyclic)methylamino]-2-[(.alpha.-substituted)arylmethyl]quinuclidin es, 3-[(cyclic)methylimino]-2-[(.alpha.-substituted)-arylmethyl]quinuclidines and cis-3-[(cyclic)-methyleneamino]-2-[(.alpha.-substituted)arylmethyl]-quinuc lidines, including their pharmaceutically acceptable salts, are disclosed. These particular compounds are found to be useful as substance P antagonists and therefore, are of value in treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases and pain or migraine. Preferred member compounds include cis-3-[(2-chlorophenyl)methylamino]-2-benzhydryl-quinuclidine, cis-3-[(2-trifluorophenyl)methylamino]2-benzhydrylquinuclidine and cis-[(2-methoxyphenyl)methylamino]-2-benzhydrylquinuclidine. Methods for preparing these compounds from known starting materials are provided.
Abstract: There is disclosed a low calorie fat substitute comprising an emulsion containing a non-flowable aqueous phase, an oil phase and a fat extender. Also disclosed are low calorie fat substitutes wherein the fat or oil is replaced by a fat mimetic.
Type:
Grant
Filed:
January 11, 1991
Date of Patent:
October 27, 1992
Assignee:
Pfizer Inc.
Inventors:
Fu-Ning Fung, James W. Miller, Michael T. Wuesthoff
Abstract: A series of novel N-alkyl N-(alkanesulphonamidoheterocyclicmethyl)-4-alkanesulphonamidophenethylamin es have been prepared, including their pharmaceutically acceptable salts and various key novel intermediates therefor. The heterocyclic moiety present in these compounds is a benzo-fused heterocyclic group derived from either benzofuran, benzothiophene, benzoxazole or quinoline, and it is attached to the adjacent methyl group of the molecule by means of the available ring carbon atom which is situated alpha to the hetero atom. These particular compounds are useful in therapy as highly effective anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrhythmias. Preferred member compounds include N-methyl-N-(5 methanesulphonamidobenzofur-2-ylmethyl)-4-methanesulphonamidophenethylamin e and N-methyl-N-(6 methanesulphonamidoquinol-2-ylmethyl)-4-methanesulphonamidophenethylamine. Methods for preparing all these compounds from known starting materials are provided.
Type:
Grant
Filed:
July 8, 1991
Date of Patent:
October 27, 1992
Assignee:
Pfizer Inc.
Inventors:
John E. Arrowsmith, Peter E. Cross, Geoffrey N. Thomas
Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Actinomadura sp. ATCC 53708. This novel antibiiotic is useful as an anticoccidial in chickens, in the prevention or treatment of swine dysentery, and as a growth promotant in cattle and swine.
Type:
Grant
Filed:
June 15, 1990
Date of Patent:
October 27, 1992
Assignee:
Pfizer Inc.
Inventors:
John P. Dirlam, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone
Abstract: 1S, 4S and 1R,4R-2-Alkyl-2,5-diazabicyclo[2.2.1]-heptanes useful as intermediates in the synthesis of certain antibacterial quinolones, are prepared respectively, from trans-4-hydroxy-L-proline and trans-4-hydroxy-D-proline via multistep procedures.
Abstract: The invention provides the substantially optically pure 2(S)-steroisomeric form of compounds of the formulae: ##STR1## and the salts thereof, together with processes for their preparation. The compounds are intermediates for the preparation of antihypertensive agents.
Abstract: A form of calcium carbonate, acid-stabilized by the addition to finely divided calcium carbonate of one of a calcium- chelating agent and a conjugate base, such as sodium hexametaphosphate, followed by the addition of a weak acid, such as phosphoric acid, is disclosed. A process for producing this material, and a method for its use in the making of neutral to acidic paper in order to improve the optical properties of the paper are also disclosed.
Abstract: Antipsychotic compounds having the formula ##STR1## wherein Z is H or Cl; Y is O or S; n is 1-4; separately, X is H or (C.sub.1 -C.sub.2)alkyl and L is R(CH.sub.2).sub.m CO, m is 0 or 1-3, R is (C.sub.1 -C.sub.6)alkyl, (C.sub.3 -C.sub.7)cycloalkyl, phenyl, naphthyl, furyl, benzofuranyl, thienyl, benzothienyl, pyrrolyl, indolyl, isoindolyl or one of said groups substituted on aromatic or heteroaromatic ring with fluoro, chloro, (C.sub.1 -C.sub.2)alkyl or (C.sub.1 -C.sub.2)alkoxy; or together L and X, in combination with the nitrogen to which they are attached, form certain cyclic imides, 4-substituted piperidines or a cyclic sulfonamide.
Type:
Grant
Filed:
February 27, 1991
Date of Patent:
October 20, 1992
Assignee:
Pfizer Inc.
Inventors:
Gene M. Bright, Kishor A. Desai, Thomas F. Seeger
Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Streptomyces sp. ATCC 55028. This novel antibiotic is useful as an anticoccidial in chickens, in the prevention or treatment of swine dysentery, as a growth promotant in cattle and swine, and as an anthelmintic in mammals, particularly in dogs, cats, sheep, cattle and swine.
Type:
Grant
Filed:
May 23, 1990
Date of Patent:
October 13, 1992
Assignee:
Pfizer Inc
Inventors:
Walter P. Cullen, John P. Dirlam, Hiroshi Maeda, Junsuke Tone
Abstract: Heteropolysaccharide 105-4, prepared by fermentation of a new unnamed Pseudomonas species ATCC 53923 is useful as an industrial thickening, suspending or stabilizing agent.
Abstract: A series of novel N-alkyl or oxyalkyl arylpiperidine derivatives have been prepared, including their pharmaceutically acceptable acid addition salts, wherein the N-alkyl or oxyalkyl side chain is further substituted by certain aryl or heterocyclic ring groups. These particular compounds are useful in therapy as neuroleptic agents for the control of various psychotic disorders. Typical and preferred member compounds include 4-{{4-{2-[4-(2-methoxyphenyl)-1-piperidinyl]ethyl}phenyl}}thiazole-2-amine , 4-{{4-{4-[4-(2-methoxyphenyl)-1-piperidinyl]-n-butyl}phenyl}}thiazole-2-a mine, 3-{4-[4-(2-methoxyphenyl)-1-piperidinyl]-n-butyl}-1,8,8-trimethyl-3-azabic yclo[3.2.1]octane-2,4-dione, 5-{2-[4-(2-methoxyphenyl)-1-piperidinyl]ethyl}oxindole and 3-{2-[4-(1-naphthyl)-1-piperidinyl]ethyl}-2-methyl-4H-pyrido[1,2-a]pyrimid ine-4-one, respectively. Methods for preparing all these compounds from known starting materials are provided.
Abstract: Variously substituted 3,5-dihydroxy-6,8-nonadienoic acids and esters, are blood cholesterol lowering agents and so are useful in the prevention and treatment of cardiovascular diseases such as atherosclerosis.
Abstract: A device suitable for use in a wide variety of types of joints of the body of a human or other mammal is provided. The device is especially useful for implantation into the human femur so as to repair an anterior cruciate ligament. The device is self-locking and can be used to connect two parts of a joint together by means of an artificial ligament (if desired) or by means of a biological graft (either allegraft or autogenous, including bone with a natural tendon attached thereto). The device permits the surgeon very simply to do a revision from such a mechanical ligament to a biological graft or vice-versa, as desired; that is, the device of the invention is fully revisable. A method of connecting two parts of a joint is also given.
Abstract: Intermediates useful in the synthesis of dihydropyridine platelet activating factor antagonists of the formula ##STR1## where R is phenyl or substituted phenyl; R.sup.3 is lower alkyl; Y is 1,4-phenylene and X is 2-alkylimidazopyridyl.
Type:
Grant
Filed:
September 11, 1991
Date of Patent:
September 22, 1992
Assignee:
Pfizer Inc
Inventors:
Kelvin Cooper, Michael J. Fray, Kenneth Richardson, John Steele
Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, or a pharmaceutically acceptable cation;Y is cyclopropyl, ethyl or p-fluorophenyl, and X is hydrogen or fluoro, or X and Y taken together form a group ##STR2## wherein R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl; or a pharmaceutically acceptable salt thereof. Also disclosed are antibacterial pharmaceutical compositions comprising the foregoing compounds, methods of using the compounds in treating bacterial infections, and intermediates for the preparation of the compounds.