Abstract: Compounds represented by the formula ##STR1## wherein R is hydrogen or alkyl of 1-4 carbons, R.sup.1 is alkyl of 1-6 carbons and the naphthyl group is attached to the imidazole ring at the 1 or 2 positions of the naphthyl ring and the pharmaceutically acceptable salts thereof are useful as centrally acting skeletal muscle relaxants.
Type:
Grant
Filed:
June 3, 1977
Date of Patent:
August 29, 1978
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Colin C. Beard, Marshall B. Wallach, Klaus Weinhardt
Abstract: Apparatus for subcutaneously implanting drug-containing pellets in animals. The apparatus comprises a handle; attached to the handle, a track along which a carriage moves; a carriage which moves along the track, the carriage having (i) a front part adapted to receive and retain a detachable needle having a passageway extending the length of the needle and (ii) a passageway extending the length of the carriage and corresponding to the needle passageway when retained in the carriage; a means to propel the carriage from the front to the rear of the track; means at the front and rear of the track to stop the carriage; a straight, retractable rod detachably attached to the rear stopping means so that the rod extends straight through the carriage passageway; a finger actuatable trigger attached to the handle to actuate the retraction of the carriage.
Abstract: A novel spherical implant pellet containing estradiol, estradiol benzoate, or mixtures thereof as the sole active ingredients which exhibits a substantially constant drug release rate over a timer period and substantially abrupt termination of drug release at the end of the time period is prepared which has an inert spherical core of a diameter of about 2-10 mm and a uniform coating of about 0.05-1 mm completely covering the core, the coating comprising about 5-99% suitable carrier and 1-95% drug. A drug may be administered at a constant rate over a chosen period by implanting the novel pellet and the release is substantially abruptly terminated at the end of said period without removing the pellet.
Abstract: A position sensitive detector including a curved detector housing having a hollow detector chamber therein, the housing having an elongate opening in the curved side wall thereof and an x-ray transmissive material adjacent thereto to render the detector chamber air-tight, a back cathode plane comprising a plurality of spaced cathode conductors on an insulator support and at least one curved anode wire, extending at least substantially transverse to the back cathode plane, disposed within the detector chamber in the path of x-rays entering through the elongate opening. Each anode wire, which is mechanically supported only at the ends thereof, is caused, during operation of the detector, to be supported in planar arcuate form solely by electrostatic forces. During operation of the detector, the chamber is filled with an ionizable gas and voltage is applied to the curved anode wire(s), thereby enabling detection of ionizing events occuring within the detector chamber.
Type:
Grant
Filed:
July 29, 1976
Date of Patent:
February 28, 1978
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Robert A. Sparks, George B. Rothbart, Roger N. Samdahl
Abstract: The novel compounds 6,11-dihydrodibenzo[b.e.]-thiepin-11-one-3-acetaldehyde and (dl) 2(6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-yl)propionaldehyde, certain dialkyl- and cyclic acetals thereof, and processes and novel intermediates for making same.
Abstract: 21-Cyclic acetals of steroids of the corticoid series are prepared from the corresponding 21-hydroxy steroids. The products have utility as anti-inflammatory agents.
Abstract: Esters of 6,11-dihydrodibenzo-[b.e.]-thiepin-11-ones of the formula: ##STR1## wherein R is hydrogen or methyl and R.sup.1 is --CH.sub.2 --CH(OH)--CH.sub.2 OH, ##STR2## where Y is either O or S, or ##STR3## where R.sup.2 and R.sup.3 are independently hydrogen, alkyl having 1 to 6 carbon atoms, phenyl or benzyl or together R.sup.2 and R.sup.3 form an alkylene bridge having 4, 5 or 6 carbon atoms, and processes for the production thereof.
Abstract: This application describes a dental burr including a cutting surface having one or more grooves therein, each of the grooves being defined by a plane which encircles the cutting surface at a skewed angle with respect to the axis of rotation of the burr. Such groove(s) provide an oscillatory chip clearing action as the burr rotates to give edge cutting and fast chip clearance. The cutting surface has abrasive particles coated thereon.
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: 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: 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 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: 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: 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: (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: 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