Abstract: Novel thioesters of 6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-acetic acid, (dl) 2-(6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-yl)propionic acid and the individual (d) isomers of the latter, and processes for making the same.
Abstract: Novel prostaglandin intermediates and process for the production thereof. Compounds, and process for the production thereof, useful in the production of (dl)-[1.alpha.-hydroxy-3.beta.-(3S-tetrahydropyranyloxy-trans-1-octenyl)-4 .alpha.-tetrahydropyranyloxy-cyclopent-1.alpha.-yl] acetaldehyde hemiacetal and [1.alpha.-hydroxy-3.beta.-(3S-tetrahydropyranyloxy-trans-1-octenyl)-4.alph a.-tetrahydropyranyloxycyclopent-1.alpha.-yl] acetaldehyde hemiacetal.
Type:
Grant
Filed:
August 23, 1976
Date of Patent:
October 25, 1977
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Francisco S. Alvarez, Albert R. Van Horn
Abstract: 2-(5H-dibenzo[a,d]cyclohepten-5-on-2-yl)acetic, propionic and butyric acids, and esters and salts thereof, are prepared by solvolysis of nitrile or amide intermediates, or of ketal-protected nitrile, amide, acid, ester or salt intermediates.
Type:
Grant
Filed:
June 21, 1976
Date of Patent:
October 18, 1977
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Peter H. Nelson, Karl G. Untch, James P. Dunn
Abstract: The method of calibrating an axial tomographic scanner including frame means having an opening therein in which an object to be examined is to be placed, source and detector means mounted on the frame means for directing one or more beams of penetrating radiation through the object from the source to the detector means, and means to rotate the scanner including the source and detector means about the object whereby a plurality of sets of data corresponding to the transmission or absorption by the object of a plurality of beams of penetrating radiation are collected; the calibration method comprising mounting calibration means supporting an adjustable centering member onto the frame means, positioning the adjustable centering member at approximately the center of rotation of the scanner, placing position-sensitive indicator means adjacent the approximately centered member, rotating the scanner and the calibration means mounted thereon at least one time and, if necessary, adjusting the positioning of the center
Abstract: This invention relates to a novel method for the preparation of 6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-acetic acid and the novel intermediate 6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-carboxaldehyde used in the preparation thereof.
Type:
Grant
Filed:
June 18, 1976
Date of Patent:
September 27, 1977
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Anthony Prince, Otto Halpern, Jack Ackrell
Abstract: This invention relates to a method of treating allergic, dermatologic and rheumatic diseases in mammals which comprises daily orally administering to said mammal in a single dose an effective amount of 6-chloro-11.beta.,17.alpha.,21-trihydroxypregna-1,4,6-triene-3,20-dione.
Abstract: 2-Substituted-5-oxo-5H-dibenzo[a,d]cycloheptenes represented by the following formula: ##STR1## where one of R.sup.2 and R.sup.3 is hydrogen, and the other is hydrogen, methyl, or ethyl, or together R.sup.2 and R.sup.3 are methylene; and R' and R.sup.4 are alkoxy, or together R' and R.sup.4 are .dbd.O, .dbd.NOH, .dbd.NNHCONH.sub.2, or alkylenedioxy of the formula --O--CH.sub.2 --(CR.sup.5.sub.2).sub.n --CH.sub.2 --O-- where n.sub.5 is O-2, R.sup.5 is hydrogen or methyl when n is 1, and R.sup.5 is hydrogen when n is 2, or one of R' and R.sup.4 is --OH and the other is (SO.sub.3 Y) where Y is sodium or potassium. The compounds have anti-inflammatory, analgesic and anti-pyretic activities and, accordingly, are useful in the treatment of inflammation, pain and pyrexia.
Abstract: This invention relates to a novel method for the preparation of 6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-acetic acid and the novel intermediates 3-(2-dialkylamino-2-dialkylphosphonylvinyl)-6,11-dihydrodibenzo-[b.e.]-thi epin-11-one in the preparation thereof.
Abstract: 6,11-Dihydrodibenzo-[b.e.]-thiepin-11-one-3-acetic acid is prepared from 6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-acetonitrile, a novel intermediate, by strong acid or base hydrolysis.
Abstract: 2-Naphthyl acetic acid derivatives and the corresponding amides, esters, hydroxamic acids and addition salts thereof, optionally substituted at the .alpha.-position on the acetic acid moiety and/or at position 6 and/or at positions 1, 4, 7 or 8 on the naphthyl ring and optionally saturated at positions 3 and 4, are anti-inflammatory, analgesic, anti-pyretic and anti-pruritic agents. A pharmaceutical method of effecting treatment of inflammation, pain, pyrexia and pruritus by the administration of naphthyl acetic acid derivatives. A pharmaceutical composition for use in the treatment of the above maladies comprising a naphthyl acetic acid derivative.
Abstract: (dl)-13-Substituted sulfinyl-prostaglandin-like [(dl)-2.alpha.-substituted-3.beta.-(1.alpha.-substituted sulfinyl-trans-2-alkenyl)-1-oxygenated cyclopentane and (dl)-2.alpha.-substituted-3.beta.-(1.alpha.-substituted sulfinyl-trans-2-alkenyl)-4-oxygenated-1-oxygenated cyclopentane] compounds exhibit prostaglandin-like biological properties and are also useful intermediates in the preparation of known prostaglandins.
Abstract: 3-[3-(1-Methyltetrazol-5-ylthio)-prop-1-(t)-enyl]-7.beta.-(.alpha.-phenylac etamido)-ceph-3-em-4-carboxylic acid; 7.beta.-(.alpha.-phenylacetamido)-3-[3-(1,2,4-triazol-5-ylthio)-prop-1-(t) -enyl]-ceph-3-em-4-carboxylic acid derivatives and salts thereof; and intermediates and processes for preparing such compounds. The compounds are useful as antibacterials and are active against a wide variety of gram positive and gram negative bacteria.
Abstract: The use of dicyclopentadienyl iron, or derivatives thereof, in physical mixture with polyvinyl chloride plastics to produce polyvinyl chloride plastic having reduced smoke generating properties.
Abstract: Compositions containing 2-(6'-substituted-2'-naphthyl)acetic acid derivatives substituted at the 2-position of the acetic acid moiety with methyl, ethyl, difluoromethyl, or methylene, and the salts and esters thereof, having anti-inflammatory, analgesic and anti-pyretic activities, and methods for the use thereof in the treatment of inflammation, pain and pyrexia.
Abstract: Human serum prealbumin is shown to possess thymus hormone-like properties of increasing immunologic competence. Pharmaceutical compositions containing this material, useful for increasing immunologic competence, are described.
Abstract: 13-Cis prostaglandin derivatives; cis-octenol ether copper.sup.(I) lithium reagents and methods of making such reagents and using the reagents to prepare the 13-cis prostaglandin derivatives. The 13-cis prostaglandin derivatives exhibit prostaglandin-like pharmacological properties and are further useful as intermediates for the corresponding prostaglandin isomers having the normal 13-trans configuration.
Type:
Grant
Filed:
December 9, 1974
Date of Patent:
September 6, 1977
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Arthur F. Kluge, Karl G. Untch, John H. Fried
Abstract: 2-(2'-Naphthyl) acetaldehyde derivatives optionally substituted at the 2 position and/or positions C-1',4',5',7' or 8'; and/or position C-6' or positions C-5' and 7' exhibit anti-inflammatory, analgesic, antipyretic and anti-pruritic activity.
Abstract: Compounds of the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is phenyl, phenyl straight chain lower alkyl or phenyl straight chain lower alkenyl or one of the above substituted in the phenyl ring with one or more substituents independently selected from the group consisting of lower alkyl of from one to four carbon atoms, halo and trifluoromethyl; the other of R.sup.1 and R.sup.2 is alkyl, cyclohexyl, cyclohexyl lower alkyl or cyclohexyl substituted with from 1 to 3 lower alkyl groups; X is oxygen or sulfur; n is an integer of from 1 to 8 with the proviso that n is not 1 when R.sup.1 is phenyl or substituted phenyl; and the antimicrobial acid addition salts thereof are useful as antifungal, antibacterial and antiprotozoal agents.
Abstract: Biotin is prepared by (a) ozonizing methylcyclohexene; (b) reacting nitromethane with the methyl-6-oxohexanoate from a to form 7-nitro-6 hydroxyheptanoic acid methyl ester; (c) acylating to form the corresponding 6 acyloxy compound; (d) forming a double bond at the 6 position; (e) reacting the product of d with nitroethanethiol to form dl-7-thia-6-nitromethyl-9-nitro-nonanoic acid methyl ester; (f) forming a furoxan by cyclization; (g) reducing the furoxan and acylating to form dl-2(4-carbomethoxybutyl)-3,4-bis(acylamido)-2,5-dihydro thiophene; (h) selectively hydrogenating to form the 3,4-cis-bis(acylamido)-2,5-dihydro thiophene; and (i) hydrolyzing and cyclizing to form dl-biotin. The products formed at steps (e)-(h) are novel, as are the individual steps (e), (f), (g), and (h).