Abstract: A visual inspection system for inspecting pharmaceutical tablets. The system comprises a photoelectric detection means for detecting the light intensity within an inspection area on a tablet and for generating a detection signal which varies with that light intensity. The system also comprises a signal processing means for comparing the detection signal to a predetermined standard in order to generate a selection signal and a transducer means which is responsive to the selection signal. A separation means separates the tablets into at least two groups in accordance with the selection signal. Yet another aspect of this invention is a method for inspecting the surface of pharmaceutical tablets using the above-described vision inspection system.
Abstract: Preparation of 2-oxindole-1-carboxamides by reaction of 2-oxindoles with trichloracetyl isocyanate to produce novel N-trichloroacetyl-2-oxindole-1-carboxamides which are then hydrolyzed to 2-oxindole-1-carboxamides useful as analgesic and antiinflammatory agents and/or intermediates for such agents.
Abstract: This invention relates to certain benzoxazolinones which inhibit lipoxygenase and/or cyclooxygenase enzymes. Such compounds are useful in inhibiting such enzymes, per se, and are useful in treating allergic and inflammatory conditions in a mammal. This invention also relates to methods of inhibiting lipoxygenase and/or cyclooxygenase in a mammal with such benzoxazolinones; methods of treating an allergic condition in a mammal with such compounds; methods of treating an inflammatory condition in a mammal with such compounds; and pharmaceutical compositions comprising the benzoxazolinones hereof.
Abstract: There is disclosed a low calorie fat substitute comprising a non-flowable aqueous phase and an oil phase, with the interaction between said aqueous and oil phases resulting in a pourable emulsion. Also disclosed are food compositions containing pourable and nonpourable emulsions.
Abstract: A process for the preparation of high purity calcium titanate hydrates, particularly various forms of kassite, is disclosed. Calcium carbonate and titanium tetraisopropoxide are used as starting materials. The process utilizes a hydrothermal reaction step. Hydrates having both hexagonal plate form, wherein the particles have a hexagonally shaped flat plate-like morphology, and lath form, wherein the particles have a rod-like morphology are produceable according to the process. Particle morphology is determined by the choice of process parameters, especially the rate of heating during the hydrothermal reaction step. Kassite particles of the hexagonal plate form, which are useful as a high opacity paper coating pigment, are produced when the rate of heating is less than or equal to 1.5.degree. C./min. Faster rates of heating result in kassite particles of a lath form. These particles are useful as a reinforcing material in polymers and ceramics.
Abstract: A novel process for converting trans-isomeric N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine to cis-isomeric N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine is disclosed. The process involves contacting trans-isomeric N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine, or a mixture of same with up to about an equal part by weight of the corresponding cis-isomer, with a basic equilibration agent like potassium tert.-butoxide in a reaction-inert polar organic solvent to ultimately afford a cis/trans-mixture wherein the amount of cis-amine present in said mixture achieves a constant value of about 2:1 on a weight-by-weight basis. The aforesaid resultant mixture is useful as an intermediate product that ultimately leads to pure cis-(1S) (4S)-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine (sertraline), which is a known antidepressant agent.
Abstract: A series of novel oxyethyl derivatives of certain selected enolic oxicam compounds are disclosed, including certain novel oxyethyl derivatives of 4-hydroxy-2-methyl-N-(2-pyridinyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide (piroxicam). These particular compounds are useful in therapy as prodrug forms of the known anti-inflammatory and analgesic oxicams. Said oxyethyl derivatives of enoic oxicam compounds like piroxicam are of the formulae: ##STR1## wherein R.sub.1 is hydrogen, methyl, fluorine or chlorine, and R.sub.2 is hydrogen or --COOR.sub.3 wherein R.sub.3 is alkyl having from one to eight carbon atoms.
Abstract: There is disclosed a low calorie fat substitute comprising a continuous aqueous phase containing carbohydrate and protein and a dispersed phase containing protein and fat.
Abstract: Certain 7-beta-[2-(2-amino-4-thiazolyl)-(Z)-2-(chloromethylene acetamido]-3-[(substituted)methyl]-ceph-3-em-4-carboxylic acids, pharmaceutically-acceptable salts thereof and conventional in vivo hydrolyzable esters thereof are valuable as broad spectrum antibacterial agents, particularly useful for the treatment of bacterial infections in man and other mammals.
Abstract: A series of [N-alkyl-N-(nitro-, alkylsulphonamido, or amino-phenalkyl) amino]-alkyl, alkoxy or alkylthio phenyl derivatives having utility as anti-arrhythmic agents.
Type:
Grant
Filed:
June 20, 1990
Date of Patent:
January 7, 1992
Assignee:
Pfizer Inc.
Inventors:
Peter E. Cross, Geoffrey N. Thomas, John E. Arrowsmith
Abstract: A series of bridged bicyclic imides having a 4-[4-(3-benzisothiazolyl)-1-piperazinyl]butyl group attached to the imide nitrogen are useful antipsychotic agents.
Abstract: A method is disclosed for the containment and controlled release of and the substantial reduction of the leaching from the site of application of agricultural chemicals. In the disclosed method, the agricultural chemicals are applied to the soil dispersed in an aqueous gel-forming composition. Novel compositions of the agricultural chemicals dispersed in aqueous gel-forming compositions are also disclosed.
Type:
Grant
Filed:
May 25, 1990
Date of Patent:
December 31, 1991
Assignee:
Pfizer Inc.
Inventors:
Judson C. Philips, Hazen L. Hoyt, IV, Christopher A. Macri, Wesley L. Miller, John J. O'Neill
Abstract: Oxophthalazinyl acetic acids having benzothiazole side chains are prepared by reacting an oxophthalazinyl thioacetamide acetate with hydrogen sulfide and a nitrophenyl compound having a reactive group such that the benzothiazole side chain may be formed by ring closure involving the thiocaetamide group. The oxophthalazinyl thioacetamide may be prepared by reacting the corresponding cyanomethyloxophthalazinyl acetate with hydrogen sulfide in the presence of tertiary amines. Analogous indazole and oxopyridopyridazinone acetic acids may be prepared similarly, as well as oxophthalazinyl, indazole and oxopyridopyridazinone acetic acids having thiazolopyridinyl side chains.
Type:
Grant
Filed:
June 15, 1990
Date of Patent:
December 24, 1991
Assignee:
Pfizer Inc.
Inventors:
Banavara L. Mylari, William J. Zembrowski
Abstract: Improved processes for preparation of racemic, cis- and optically active (3S,4R)-3[1(R)-t-butyl-dimethylsilyloxy)-ethyl]-4-[1-oxo-3-thiolanylthio(t hiocarbonyl)thio]azetidin-2-ones, process improvements for certain intermediates therefor and a novel intermediate for said racemic, cis- and trans-compounds, which compounds are useful as intermediates for antibacterial 5R,6S-6-[1(R)-hydroxyethyl]-2-(1-oxo-3-thiolanylthio)-2-penem-3-carboxylic acids and the pharmaceutically-acceptable salts and the pivaloyloxymethyl esters thereof.
Type:
Grant
Filed:
January 18, 1991
Date of Patent:
December 24, 1991
Assignee:
Pfizer Inc.
Inventors:
Frank R. Busch, Robert W. Dugger, George J. Quallich
Abstract: An antibiotic compound of the formula: ##STR1## is an antiparasitic agent active against insect pests, acari, free living nematodes and endo- and ectoparasites. It is prepared by fermentation using the microorganism Streptomyces griseochromogenes ATCC 53928.
Type:
Grant
Filed:
July 25, 1990
Date of Patent:
December 17, 1991
Assignee:
Pfizer Inc.
Inventors:
Yasuhiro Kojima, Hiroshi Maeda, Satoshi Nishiyama, David A. Perry
Abstract: This invention relates to the use of certain derivatives of 5-hydroxy and 5-methoxy 2-aminopyrimidines of the formula ##STR1## and the pharmaceutically-acceptable salts thereof, wherein R.sup.1 is H or CH.sub.3 ; R.sup.2 is (C.sub.3 -C.sub.15) straight chain alkyl or (C.sub.7 -C.sub.20)phenylalkyl which may be substituted in the phenyl by one or two fluoro or chloro substituents; and R.sup.3 is H or CH.sub.3 to inhibit interleukin-1 production in a mammal. This invention also relates to the use of such compounds for treating interleukin-1 mediated disorders and dysfunctions such as bone and connective tissue metabolism disorders and immune dysfunction in a mammal. The methods of this invention comprise administering an interleukin-1 production inhibiting amount of the compounds and salts of this invention to such a mammal.
Abstract: Certain 6-aryl- or 6-heteroaryl- alkylaminobenzoxazolones, and their pharmaceutically-acceptable salts, are dual inhibitors of lipoxygenase and cyclooxygenase enzymes, and so are useful as antiallergy and antiinflammatory agents.
Type:
Grant
Filed:
July 18, 1990
Date of Patent:
December 10, 1991
Assignee:
Pfizer Inc.
Inventors:
Fumitaka Ito, Takashi Mano, Masami Nakane
Abstract: The invention provides compounds of the formula: ##STR1## wherein k is 1, 2 or 3;m is 1, 2 or 3;n is 1, 2 or 3;p is 0, 1 or 2;X is O, S or a direct link, with the proviso that when X is O or S, n is 2 or 3;R.sup.1 is H or C.sub.1-C.sub.4 alkyl; andR.sup.2 is an optionally substituted phenyl or heteroaryl group; andpharmaceutically acceptable salts thereof.These compounds are useful for the treatment of motility disorders, particularly those of the gut such as irritable bowel syndrome.
Type:
Grant
Filed:
May 23, 1990
Date of Patent:
December 10, 1991
Assignee:
Pfizer Inc.
Inventors:
David Alker, Robert J. Bass, Peter E. Cross
Abstract: Process for transformation of Yarrowia lipolytica, vectors useful therefor comprising DNA of a microbial vector and chromosomal DNA of Y. lipolytica and transformants comprising said vectors in E. coli and Y. lipolytica, and integrative shuttle vectors for Escherichia-Yarrowia transgeneric cloning. Said vectors or subclones thereof enable creation of Y. lipolytica cloning vectors into which specific or random segments of DNA can be inserted and the resulting vectors used to transform a suitable host microbe, especialy Y. lipolytica, to improve the fermentation characteristics thereof and hence their industrial utilization.The methodology described permits the cloning of genes from a gene library of Y. lipolytica by complementation with an integrating vector.