Abstract: Compounds of the formula ##STR1## wherein Z is C.sub.1 and C.sub.4 alkoxymethylene, hydroxymethylene, esterified hydroxymethylene, carbonyl, or ketal-protected carbonyl, and the pharmaceutically acceptable acid addition salts thereof, are useful as anticonvulsant and anti-secretory agents.
Abstract: A powered dental scaler is disclosed of a type which drives a vibrating scaling tip in a circular or ellipsoidal pattern of motion. A scaling tip having working surfaces provided by the edges of an elongated, curved element which has a cross-sectional configuration in the shape of a multi-sided figure, e.g., a triangle or a diamond, is particularly useful with a scaler having this type of vibrational pattern. Each of the longitudinal edges has a radius of curvature in the range of about 0.001 inch to about 0.005 inch. The free end of the scaler work tool preferably terminates in rounded or ball-shaped configurations, and the working surfaces can be joined along inactive edges by a convex surface to provide "safe" surfaces. The absence of sharp edges or points on the scaler tool work surfaces substantially reduces the likelihood of damage to tooth dentin, cementum or gums.
Abstract: Certain 3-oxoandrost-4-ene and 3-oxoandrosta-1,4-diene 17.beta.-carboxylic acids (and esters thereof) substituted at the 4-position with a fluoro or chloro, optionally substituted at the 6- position with fluoro or chloro and at 16.beta. with methyl are useful as anti-inflammatory steroids. These compounds are optionally substituted at the 9.alpha. position with fluoro, chloro or bromo; substituted at the 11 with a keto, a beta-hydroxy or a beta-chloro (the latter only when there is a 9.alpha.-chloro); when there is a 17.alpha.-hydroxy (or an ester).
Abstract: Compounds of the formula ##STR1## wherein m is the integer 1, 2 or 3; R is independently selected from the group C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy, halo, trifluoromethyl and hydroxy when m is the integer 1, 2 or 3 and methylenedioxy when m is the integer 2; Z is hydroxymethylene, esterified hydroxymethylene, alkoxymethylene, alkylthiomethylene, carbonyl, or ketal-, thioketal- or hemithioketal- protected carbonyl, and the pharmaceutically acceptable acid addition salts thereof, are useful as anticonvulsants, anti-secretory agents and spermatocides.
Abstract: 1-Substituted imidazole derivatives exhibit spermatostatic and spermatocidal activity and are useful for contraceptive purposes both in male and female mammals.
Abstract: Certain pregn-4-ene-3,20-diones or pregn-1,4-diene-3,20-diones 4-substituted with a fluoro or chloro are useful as topical anti-inflammatory steroids. These compounds are substituted at 9.alpha. with hydrogen, fluoro, chloro or bromo; at 6.alpha. with hydrogen, fluoro or chloro; at the 11 position with a keto, a .beta.-hydroxy or a .beta.-chloro (the latter only when there is a 9.alpha.-chloro); at 16.alpha., 17.alpha.-positions with isopropylidenedioxy or at 16.alpha.- (or 16.beta.) with methyl when 17.alpha. is hydroxy (or an ester); and at the 21-position with mono-fluoro, chloro, bromo, hydroxy or alkanoyloxy of 2-6 carbons or difluoro, dichloro, dihydroxy or dimethoxy.
Abstract: A unique crystalline form of flunisolide is prepared by crystallizing flunisolide from a solution of an alkanol of three or four carbon atoms, e.g. n-butanol, containing 0.2 to 5%, preferably 1.0 to 4.0% by volume water.
Type:
Grant
Filed:
May 16, 1980
Date of Patent:
June 16, 1981
Assignee:
Syntex Corporation
Inventors:
Richard E. Jones, Jacquelyn A. Smithers
Abstract: The compounds of the present invention are represented by the formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are optionally substituted furyl or thienyl the substituents independently selected from the group halo, C.sub.1 to C.sub.6 alkyl and C.sub.1 to C.sub.6 alkoxy or optionally substituted phenyl the substituents independently selected from the group halo, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy and trifluoromethyl; X is oxygen or sulfur; m is the integer 0; and n is the integer 2 or 3; and the antimicrobial acid addition salts thereof, with the proviso that when either R.sup.1 or R.sup.2 is said optionally substituted phenyl the other R.sup.1 or R.sup.2 is said optionally substituted furyl or thienyl.The compounds are useful for combatting fungi, bacteria and protozoa. They also have spermatocidal and spermatostatic activity.
Abstract: A dental tool for generating a relatively smooth surface on tooth enamel comprises an elongated shank with an operative end and an end adapted to engage a chuck of a dental handpiece. Any cross-section of the operative end perpendicular to the shank's longitudinal axis is circular with a diameter of less than 0.140 inch. Adjacent, continuous annular grooves extend around the operative end, each groove being defined by a pair of inwardly sloping side surfaces intersecting with each other at least about 0.010 inch from the shank's longitudinal axis and forming an included angle of 60.degree. to 150.degree. between the side surfaces. An abrasive material, such as diamond grit, having a particle size of less than 0.006 inch covers at least a portion of each surface.
Abstract: The invention provides new hydrogel forming materials comprising synthetic, hydrophilic, aqueous-insoluble polymer networks formed by copolymerization of a hydrophilic dihydroxyalkyl acrylate or methacrylate, a substantially water insoluble alkyl acrylate or methacrylate, one or more additional hydrophilic comonomers selected from the group of vinylic monomers, acrylates, and methacrylates, and a cross-linking agent. The hydrogels are preferably used for the formation of contact lenses, but may also be used for drug and pesticides delivery devices; dialysis, ultrafiltration and reverse osmosis membranes; implants in surgery and dentistry; and the like.
Abstract: Certain 16.beta.-methyl-3-oxoandrost-4-ene and 16.beta.-methyl-3-oxoandrosta-1,4-diene 17.beta.-thiocarboxylic acid esters are useful as anti-inflammatory steroids. These compounds are optionally substituted at the 6.alpha.-position with fluoro or chloro; optionally substituted at the 9.alpha. position with fluoro, chloro or bromo; substituted at the 11 position with a keto, a .beta.-hydroxy or a .beta.-chloro (the latter only when there is a 9.alpha.-chloro); and substituted with 17.alpha.-hydroxy (or an ester thereof).
Abstract: Certain 1,4,5,6-tetrahydropyrimidine compounds which are substituted with an amino, amido or carbamate at the 2-position, with an optionally substituted phenyl at the 5-position or at the 4-position when there is no alkyl at the 1-position and optionally a lower alkyl at the 1-position when the phenyl is at the 5-position are useful as CNS agents and as antihypertensives.
Abstract: Certain 3-oxoandrost-4-ene and 3-oxoandrosta-1,4-diene 17.beta.-thiocarboxylic acid esters substituted at the 4-position with a fluoro or chloro, optionally substituted at the 6- position with fluoro or chloro and at 16.beta. with methyl are useful as anti-inflammatory steroids. These compounds are optionally substituted at the 9.alpha. position with fluoro, chloro or bromo; substituted at the 11 with a keto, a beta-hydroxy or a beta-chloro (the latter only when there is a 9.alpha.-chloro); when there is a 17.alpha.-hydroxy (or an ester).
Abstract: Certain 3-oxoandrost-4-ene and 3-oxoandrosta-1,4-diene 17.beta.-carboxylic acids and esters substituted at the 4-position with a fluoro or chloro and optionally substituted at the six position with fluoro or chloro are useful as anti-inflammatory steroids. These compounds are optionally substituted at the 9.alpha.-position with fluoro, chloro or bromo; substituted at the 11 with a keto, a .beta.-hydroxy or a .beta.-chloro (the latter only when there is a 9.alpha.-chloro); substituted at 16.alpha. (or 16.beta.) with methyl or hydrogen, and at 17.alpha. with hydroxy or an ester.
Abstract: An air-driven dental scaler is disclosed having water transport means for delivering water to a scaling type work tool. The water transport means comprises a tube coaxially disposed within a vibratable hollow shaft. The water tube is supported at one end within a resilient support assembly which provides a water seal between the coaxially disposed vibratable shaft and water transport tube. The water seal assembly is positioned forwardly of a vibrational node characteristic of a standing wave created during operation of the dental scaler. An axial force exerted on the water seal assembly during vibration of the vibratable shaft improves the efficacy of the water seal between the shaft and the water transport tube. The single, resilient support for the water transport tube provides for quick replacement of the water tube in the event of clogging of the tube by mineral deposits or sediment.
Abstract: The biological activity of super agonist analogues of LH-RH is extended for long periods of time by incorporation of such analogues in a vehicle comprising an oil of vegetable origin and a gelling agent, preferably an aluminum mono-fatty acid ester. Pharmaceutical compositions thus formed are suitable for depot injection.