Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and are hydrogen, C.sub.1 to C.sub.6 alkyl, C.sub.6 to C.sub.12 carbocyclic aryl or aralkyl of 1 to 6 carbon atoms in the alkyl moiety and 6 to 12 carbon atoms in the carbocyclic aryl moiety;R.sup.4 and R.sup.5 are the same or different and are hydrogen or C.sub.1 to C.sub.6 alkyl; andR.sup.6 and R.sup.7 are the same or different and are hydrogen, C.sub.1 to C.sub.6 alkyl or C.sub.1 to C.sub.6 alkoxy. Methods for preparing these compounds are also disclosed. The compounds are useful as antihypertensives and as diuretics. They also function as antihistamines and as bronchodilating agents and are therefore effective in inhibiting the effects of allergic reactions. They are also of use in the treatment of migraine and in the treatment of vasospastic disorders.
Type:
Grant
Filed:
September 6, 1979
Date of Patent:
March 10, 1981
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Arthur F. Kluge, Arthur M. Strosberg, Stefan H. Unger
Abstract: Compositions containing and methods of employing as the essential ingredients substituted xanthone carboxylic acid compounds which are useful in the prevention of complications of diabetes. Methods for preparing these compounds and the compositions and intermediates therein are also disclosed.
Abstract: A single-unit turbine cartridge assembly for a gas-driven dental handpiece includes a pair of bearing assemblies mounted on a turbine rotor shaft and a ring of resilient material around each bearing assembly. The resilient ring provides radial support for the turbine cartridge assembly within the housing of the handpiece and substantially dampens the transfer of vibration from the cartridge assembly to the handpiece during use of the handpiece. The turbine cartridge assembly may optionally include bearing axial pre-load means in association with one or more of the bearing assemblies. The turbine cartridge assembly also includes means for retaining the resilient radial support means and the bearing axial preload means, when used, in association with the bearing assemblies, so as to permit removal, and reinstallation, of the cartridge assembly as an entire unit from, and to, the housing in the dental handpiece.
Abstract: 1-Substituted imidazole derivatives exhibit spermatostatic and spermatocidal activity and are useful for contraceptive purposes both in male and female mammals.
Type:
Grant
Filed:
January 11, 1979
Date of Patent:
January 27, 1981
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Duane W. Hallesy, Richard E. Jones, Brian H. Vickery, Keith A. M. Walker
Abstract: Mixtures of d 2-(6-methoxy-2-naphthyl)propionic acid and 1 2-(6-methoxy-2-naphthyl)propionic acid or soluble salts thereof are resolved with N-R-D-glucamine or salts thereof, where R is alkyl having 2 to 36 carbon atoms or cycloalkyl having 3 to 8 carbon atoms, to yield a product substantially enriched in d 2-(6-methoxy-2-naphthyl)-propionic acid.
Abstract: The subject of the invention is a process for resolving mixtures of (+)- and (-)-6-methoxy-.alpha.-methyl-2-naphthaleneacetic acid into the enantiomers thereof, characterized in that N-methyl-D-glucamine [=1-deoxy-1-(methylamino)-D-glucitol] is used as the resolving agent, so that the 6-methoxy-.alpha.-methyl-2-naphthaleneacetic acid is converted into the corresponding diastereoisomeric N-methyl-D-glucamine salt pair which, because of very different solubilities, can be separated easily and completely with high yield.
Type:
Grant
Filed:
July 6, 1979
Date of Patent:
January 20, 1981
Assignee:
Syntex Corporation
Inventors:
Ernst Felder, Davide Pitre, Hans Zutter
Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and are hydrogen, C.sub.1 to C.sub.6 alkyl, C.sub.6 to C.sub.14 carbocyclic aryl or aralkyl of 1 to 6 carbon atoms in the alkyl moiety and 6 to 12 carbon atoms in the carbocyclic aryl moiety and R.sup.4 is selected from the group having the formula ##STR2## where R is C.sub.1 to C.sub.8 alkyl, C.sub.1 to C.sub.8 alkoxy, halo, cyano, AlkNHC(O)-- or AlkC(O)NH-- and R' is Alk NHC(O) or Alk C(O)NH where Alk is C.sub.1 to C.sub.6 alkyl or the group 2-(endobicyclo[3.1.0]hexyl)ethyl. Methods for preparing the compounds are disclosed. The compounds are useful for the treatment of hypertension and cardiac disorders.
Abstract: A mechanism for moving an X-ray source around the patient's head so that the image of an object, having shape of the dental arch, can be obtained on the film, the mechanism including a stationary frame, a rotatably movable support arm with an X-ray source and a film holder attached to its opposite ends on different sides of the object to be radiographed, and means for moving the center of rotation of the support arm rectilinearly during the radiographing, throughout the procedure in the same direction, perpendicular to the axis of symmetry of the dental arch, in such a manner that the position of the center of rotation in its rectilinear movement is dependent on the angular position of the support arm at any given moment, with the purpose of directing the X-ray beam from the X-ray source so that at any given moment it is substantially perpendicular to that part of the object which has the shape of the dental arch.
Abstract: Nonapeptide and decapeptide analogs of LH-RH of the formula(pyro)Glu-His-V-Ser-W-X-Y-Arg-Pro-Z (I)and the pharmaceutically acceptable salts thereof wherein:V is tryptophyl, phenylalanyl or 3-(1-naphthyl)-L-alanyl;W is tyrosyl, phenylalanyl or 3-(1-pentafluorophenyl)-L-alanyl;X is a D-amino acid residue ##STR1## wherein R is (a) a carbocyclic aryl-containing radical selected from the group consisting of naphthyl, anthryl, fluorenyl, phenanthryl, biphenylyl, benzhydryl and phenyl substituted with three or more straight chain lower alkyl groups; or(b) a saturated carbocyclic radical selected from the group consisting of cyclohexyl substituted with three or more straight chain lower alkyl groups, perhydronaphthyl, perhydrobiphenylyl, perhydro-2,2-diphenylmethyl and adamantyl;Y is leucyl, isoleucyl, nor-leucyl or N-methyl-leucyl;Z is glycinamide or --NH--R.sup.1, whereinR.sup.1 is lower alkyl, cycloalkyl, fluoro lower alkyl or ##STR2## wherein R.sup.2 is hydrogen or lower alkyl,are disclosed.
Type:
Grant
Filed:
June 11, 1979
Date of Patent:
November 18, 1980
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
John J. Nestor, Gordon H. Jones, Brian H. Vickery
Abstract: The tricyclic intermediate ##STR1## is prepared in a three step sequence from the bicyclic intermediate ##STR2## The key step of this process involves the addition of a Grignard reagent to a mixed anhydride. Tricyclic compound of formula (I) may be readily converted by known methods to valuable steroids.
Abstract: Novel 5-alkylsulfinylbenzoyl- and 5-alkylsulfonylbenzoyl,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid compounds represented by the formula ##STR1## and the pharmaceutically acceptable, non-toxic esters and salts thereof, wherein n is 1 or 2, R is hydrogen or a lower alkyl group containing from 1-4 carbon atoms and R.sup.1 is a lower alkyl group having from 1-4 carbon atoms at the ortho, meta or para postions of the benzoyl group and process for the production of such compounds. These compounds are useful as anti-inflammatory, analgesic and antipyretic agents and as smooth muscle relaxants.
Abstract: Compositions containing and methods of employing as the essential ingredients substituted xanthone carboxylic acid compounds which are useful in the prevention of complications of diabetes. Methods for preparing these compounds and the compositions and intermediates therein are also disclosed.
Abstract: Psoriasis in mammals is relieved by topically administering substituted naphthaquinones of the formula: ##STR1## where R.sup.1 and R.sup.2 are the same or different and are hydrogen, hydroxy, alkoxy or acylamino and R.sup.3 is hydrogen, halo, cyano or alkoxy with the proviso that R.sup.1 and R.sup.2 are not both hydrogen.
Abstract: Compounds of the formula ##STR1## where R.sup.1 and R.sup.2 are the same or different and are phenyl optionally substituted with a substituent selected from the group C.sub.1 and C.sub.6 alkyl, C.sub.1 and C.sub.6 alkoxy and halo; or C.sub.4 or C.sub.5 heterocyclic aryl, the heteroatom selected from the group oxygen, nitrogen and sulfur; R.sup.3 and R.sup.4 are the same or different and are C.sub.1 to C.sub.6 alkyl; m is the integer 2 through 5; and X is selected from the group methanesulfonate, benzenesulfonate, p-toluene-sulfonate, nitrate, chloride, bromide and iodide. Methods for preparing these compounds are also disclosed. The compounds of the present invention are useful as anticholinergic agents.
Abstract: Flame retardant latex bases having an excellent balance of properties are prepared most efficiently and economically by blending together two separately polymerized latexes of different types, the polymeric content of one of said latexes being formed predominantly from a monomer mixture consisting of from about 70 to about 92% by weight vinylidene chloride and 8 to 30% by weight of certain polar comonomers principally of the lower alkyl acrylate class while the polymeric content of the second latex is formed from a monomer mixture consisting predominantly of styrene and butadiene. This technique of producing the desired flame retardant latex bases by combining two separately prepared but simpler component latexes not only maximizes quality control and manufacturing flexibility but also permits the simultaneous realization of higher conversions and reduced polymerization cycles or residence times so that productivity is also maximized.
Type:
Grant
Filed:
July 3, 1978
Date of Patent:
October 14, 1980
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Ramchandra K. Hulyalkar, Rodrigue V. Lauzon
Abstract: An inhalation device for dispensing a powdered medicament from a medicament-holding container having a first part which is 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 the mouth or nasal passage of the user thereof, the passageway terminating in an emptying chamber at the output end of the housing, the cross-sectional area of the passageway being less than the cross-sectional area of the emptying chamber, and means for receiving the second part of the device which is a carriage moveably connected to the first part and having means to receive a medicament-holding container so that when an open end of the medicament-holding container is placed adjcent the inner end of the emptying chamber during inhalation the medicament is dispensed from the container.
Abstract: A method for preparing 4,5-dihydro-2-alkoxycarbonylamino-5-carbocyclic aryl imidazoles and substituted aryl derivatives thereof is disclosed. The compounds are prepared by treating a 1-(carbocyclic aryl)-2-(2',3'-bis-carboalkoxyguanidino) ethane of the formula ##STR1## where R is C.sub.1 to C.sub.6 linear or branched alkyl, R' is phenyl optionally substituted with the radial methylenedioxy or at least one hydroxy, halo, trifluoromethyl, C.sub.1 to C.sub.6 linear or branched alkoxy, or 1-naphthyl or 2-naphthyl and X is halo, mesyloxy or tosyloxy with a protic solvent solution or dispersion of an alkali metal or alkaline earth metal hydroxide, carbonate or alkoxide. 1-(Optionally substituted carbocyclic aryl)-2-(carboalkoxyguanidino) ethanes are also disclosed herein, such prepared by treating the above bis-carboalkoxyguanadino ethane with an aprotic solvent solution or dispersion of an alkali metal or alkaline earth metal hydroxide, carbonate or alkoxide.
Abstract: Compositions containing and methods employing, as the essential ingredient, novel substituted xanthone-2-carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions and intermediates therein are also disclosed.
Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is phenethyl and R.sup.2 is phenyl, each of said phenethyl or phenyl independently being unsubstituted or substituted in the phenyl ring by from 1 to 3 substituents selected from the group consisting of halo, lower alkyl and lower alkoxy with the proviso that at least one of R.sup.1 and R.sup.2 be substituted by lower alkoxy; X is oxygen or sulfur; and the antimicrobial acid addition salts thereof are useful as antifungal, antibacterial and antiprotozoal agents.
Abstract: Compounds of the formula ##STR1## where R.sup.1 and R.sup.2 are the same or different and are C.sub.1 to C.sub.6 alkyl; C.sub.5 or C.sub.6 cycloalkyl; C.sub.5 or C.sub.6 cycloalkenyl; phenyl optionally substituted with a substitutent selected from the group C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy and halo; or C.sub.4 or C.sub.5 heterocyclic aryl, the heteroatom selected from the group oxygen, nitrogen and sulfur; Y is the radical selected from (CH.sub.2).sub.n, (C.sub.4 H.sub.8 S), (C.sub.4 H.sub.8 O) and ##STR2## where R is hydrogen or C.sub.1 to C.sub.6 alkyl and n is the integer 4 or 5; and X is selected from the group methanesulfonate, benzenesulfonate, p-toluenesulfonate, nitrate, chloride, bromide and iodide. Methods for preparing these compounds are also disclosed. The compounds of the present invention are useful as anticholinergic agents.