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, antipyretic 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: Vicinal steroidal epoxides are prepared by reacting the corresponding vicinal steroidal bromohydrin with a heterocyclic base such as 1,5-diazabicyclo[4.3.0]non-5-ene or 1,5-diazabicyclo[5.4.0]-undec-5-ene.
Abstract: A dental handpiece is disclosed having at least two connectable portions and having a substantially rigid connection between the two connectable portions, there being resilient means forming a portion of the substantially rigid connection. The resilient means inhibits transfer of vibration from one of the connectable portions which contains a gas-driven motor to the other connectable portion which provides a hand-grippable surface.
Type:
Grant
Filed:
September 29, 1978
Date of Patent:
May 20, 1980
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Arthur A. Knopp, John E. Nash, Richard P. Lewis
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, chloro or bromo 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,-17 alpha-positions with isopropylidenedioxy; and substituted at 16 alpha (or 16 beta) with methyl or hydrogen when there is a 17 alpha-hydroxy (or an ester).
Abstract: Certain 3-ketoandrost-4-ene and 3-ketoandrosta-1,4-diene 17 beta-carboxylic acids and esters substituted at the 6 alpha and 6 beta positions with fluorine substituents 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 when there is a 17 alpha-hydroxy (or an ester).
Abstract: This invention is a process for preparing 3-keto-androst-4-ene 17.alpha.-carboxylic acids, androsta-1,4-diene 17.alpha.-carboxylic acids and their 17.alpha.-esters by reacting a corresponding 21-hydroxypregn-4-ene-3,20-dione, 21-hydroxypregna-1,4-diene-3, 20-dione, or their 21-esters with an alkali metal carbonate base in a lower alkanol in the presence of oxygen. The 17.alpha.-esters are formed by reacting the 17.alpha.-carboxylic acid with a suitable alkylating agent.
Abstract: A breath-actuated inhalation device for dispensing a powdered medicament from a powdered medicament-holding capsule, comprising an elongate housing having a passageway for the movement of air therethrough, one end of the housing being an output end adapted for insertion into a user's mouth or nasal passage, the passageway having an inlet end terminating in an emptying chamber at the output end of said housing, the cross-sectional area of the passageway being less than the cross-sectional area of the emptying chamber, and means associated with said housing for receiving a powdered medicament-holding capsule. A collar surrounds at least a portion of the periphery of the housing adjacent the emptying chamber and has at least one substantially flat surface with a notch therein, which allows a first, smaller part of a two-part capsule to fit therein but which is too small to allow the second, larger part of the capsule to fit therein.
Abstract: Benzene ring substituted benzimidazole-2-carbamate derivatives represented by the formula: ##STR1## where R is a lower alkyl group having 1 to 4 carbon atoms; ##STR2## is a 5, 6, 7 or 8 membered heterocyclic ring containing 1 or 2 hetero atoms; the ##STR3## substitution being at the 5(6)-position; and the pharmaceutically acceptable salts thereof. The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.
Abstract: Certain 3-oxoandrost-4-ene and 3-oxoandrosta-1,4-diene 17 beta-thiocarboxylic acid esters are useful as antiinflammatory 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 on a beta-chloro (the latter only when there is a 9 alpha-chloro); substituted at 16 alpha, 17 alpha-positions with isopropylidenedioxy; and substituted at 16 alpha (or 16 beta) with methyl or hydrogen when there is a 17 alpha-hydroxy (or an ester).
Abstract: Certain 3-oxoandrost-4-ene and 3-oxoandrosta-1,4-diene 17 beta-thiocarboxylic acid esters substituted at the 6 alpha, 6 beta-positions with fluorine substituents 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, 17 alpha-positions with isopropylidenedioxy; and substituted at 16 alpha (or 16 beta) with methyl or hydrogen when there is a 17 alpha-hydroxy (or an ester).
Abstract: 22-Optionally substituted steroids of the corticoid series are prepared from the corresponding 21-methylene steroids through the 20,21-dione steroid intermediates. These compounds have utility as anti-inflammatory agents.
Abstract: This invention concerns a minus prescription hydrogel contact lens that permits oxygen diffusion to the cornea in sufficient quantity to avoid the effects of oxygen deprivation; avoids the physiological complications arising from damage to the bulbar conjunctivia due to compression of the limbal capillaries; and avoids corneal scleral or wetting deficiencies. These advantages are accomplished through a combination of lens design and hydrogel properties.
Type:
Grant
Filed:
October 28, 1976
Date of Patent:
December 25, 1979
Assignee:
Syntex (USA) Inc.
Inventors:
William L. Mancini, Donald R. Korb, Miguel F. Refojo
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: Novel 16-phenoxy and 16-(o, m or p)-substituted phenoxy derivatives of (dl)-9-keto-11.alpha.,15.alpha.-dihydroxy-17,18,19,20-tetranorprosta-4,5,1 3-trans-trienoic acid, the pharmaceutically acceptable, non-toxic lower alkyl esters and salts thereof and processes for the production of such compounds. These compounds possess prostaglandin-like activities and thus are useful in the treatment of mammals where prostaglandins are indicated. They are particularly useful as inhibitors of gastric acid secretion; and as agents for the control of asthmatic attack, because of their bronchodilating activity.
Type:
Grant
Filed:
July 10, 1978
Date of Patent:
December 11, 1979
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Albert R. Van Horn, Gabriel Garay, John A. Edwards
Abstract: 1-Alkylamino-3-(4-[(endobicyclo[3.1.0]hex-6-yl)alkylure ido]-1-phenoxy)-2-propanol and substituted derivatives thereof; 1-alkylamino-3-(4-[(endobicyclo[3.1.0]hex-6-yl)-alkylcarbonylamino]-1-phen oxy)-2-propanol and substituted derivatives thereof; and 1-alkylamino-3-(4-[(endobicyclo-[3.1.0]hex-6-yl)alkoxycarbonylamino]-1-phe noxy)-2-propanol and substituted derivatives thereof as well as methods for preparing such compounds are disclosed. 5-(4-[(Endobicyclo[3.1.0]hex-6-yl)alkylureido]-1-phenoxy) methyl-3-alkyl-2-optionally substituted oxazolidine and derivatives thereof; 5-(4-[(endobicyclo[3.1.0]hex-6-yl alkylcarbonylamino]-1-phenoxy)methyl-3-alkyl-2-optionally substituted oxazolidine and derivatives thereof; and 5-(4-[(endobicyclo[3.1.0]hex-6-yl)alkoxycarbonylamino]-1-phenoxy)methyl-3- alkyl-2-optionally substituted oxazolidine and derivatives thereof and methods for preparing these compounds are also disclosed.
Type:
Grant
Filed:
July 3, 1978
Date of Patent:
December 4, 1979
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Karl G. Untch, Belig Berkoz, Stefan H. Unger
Abstract: 6-(N-vinylureido)penicillanic acids and salts thereof; and processes for preparing such compounds are disclosed. The compounds are useful as inhibitors of lactic acidosis in ruminants.
Abstract: Compounds of the formula ##STR1## wherein R is hydrogen or methyl; R.sup.1 is hydrogen, C.sub.1 to C.sub.8 linear or branched alkyl or C.sub.1 to C.sub.8 linear or branched alkanoyl; X is oxygen or sulfur; R.sup.2 is selected from the group hydrogen, C.sub.1 to C.sub.18 linear or branched alkyl and the radicals --(CH.sub.2).sub.n --NR.sup.3 R.sup.4, --CH.sub.2 --CH(OH)--CH.sub.2 --OH or a ketal thereof formed from the aldehyde or ketone R.sup.5 R.sup.6 CO, wherein R.sup.3 and R.sup.4 are each independently C.sub.1 to C.sub.6 linear or branched alkyl or R.sup.3 and R.sup.4 taken together with the nitrogen atom of the first radical are attached to form a 5- or 6-membered heterocyclic ring, R.sup.5 and R.sup.6 are each independently hydrogen, C.sub.1 to C.sub.6 linear or branched alkyl, phenyl or benzyl or R.sup.5 and R.sup.
Type:
Grant
Filed:
June 28, 1978
Date of Patent:
October 30, 1979
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
James P. Dunn, Peter H. Nelson, Karl G. Untch
Abstract: This invention is a composition useful for dyeing keratinous fiber brown without using o-, m- or p-phenylenediamine, 2,4-diaminoanisol or nitro compounds. The composition consists essentially of 1,5-dihydroxynaphthalene, m-aminophenol, p-aminodiphenylamine or a suitable acid addition salt thereof, a suitable modifier, a suitable coupler and a suitable base. This composition in combination with an oxidizing agent dyes hair brown.
Abstract: Compounds of the formula ##STR1## wherein R is alkyl, benzyl, substituted benzyl, phenyl or substituted phenyl, said substituted benzyl and substituted phenyl substituted on the phenyl ring with from one to three substituents independently selected from the group consisting of halo, lower alkyl and trifluoromethyl; X is oxygen or sulfur; and the pharmaceutically acceptable acid addition salts thereof are CNS-active agents, inhibitors of gastric secretion and antifungal, antibacterial and antiprotozoal agents.
Abstract: This invention is a composition useful for dyeing keratinous fibers black without using o-, m- or p-phenylenediamine, 2,4-diaminoanisole or nitro compounds. The composition consists essentially of 1,5-dihydroxynaphthalene, 4,4'-diaminodiphenylamine or a suitable acid addition salt thereof, p-aminodiphenylamine or a suitable acid addition salt thereof, a suitable modifier, a suitable coupler and a suitable base. This composition in combination with an oxidizing agent dyes hair black.