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 radical 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: This invention is a composition useful for dyeing keratinous fiber red without using o-, m- or p-phenylenediamine, 2,4-diaminoanisole or nitro compounds. The composition consists essentially of .alpha.-hydroxynaphthalene, p-aminophenol, a suitable modifier, a suitable coupler and a suitable base. This composition is combined with an oxidizing agent before contacting the hair to dye hair red.
Abstract: This invention is a composition useful for dyeing keratinous fiber blond without using o-, m- or p-phenylenediamine, 2,4-diaminoanisole or nitro compounds. The composition consists essentially of m-aminophenol, p-aminophenol, p-methylaminophenol or a suitable acid addition salt thereof, a suitable modifier, a suitable coupler and a suitable base. This composition is combined with an oxidizing agent before contacting the hair to dye hair blond.
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: 1-Alkylamino-3-(3- or 4-[2-(endobicyclo[3.1.0]-hex-6-yl)ethylaminocarbonyl]-1-phenoxy)-2-propano l and substituted derivatives thereof and methods for preparing such compounds are disclosed. 5-(3- Or 4-[2-(endobicyclo[3.1.0]hex-6-yl)ethylaminocarbonyl]-phenoxy)methyl 3-alkyl-2-optionally substituted oxazolidine and derivatives thereof, and methods for preparing such compounds are also disclosed. These compounds exhibit cardiovascular acitivity and are useful in the treatment of abnormal heart condition as well as hypertension in mammals. The former compounds are prepared by treatment of the corresponding 1,2-epoxy-3-(3- or 4-[2-(endobicyclo[3.1.0]hex-6-yl)-ethylaminocarbonyl]phenoxy)propane with the desired alkylamine or by base or acid hydrolysis of the corresponding 5-(3- or 4-[2-(endobicyclo[3.1.0]hex-6-yl)-ethylaminocarbonyl)-3-alkyl oxazolidine. The latter compounds are prepared from the corresponding 1-alkylamino-3-(3- or 4-[2-(endobicyclo[3.1.
Type:
Grant
Filed:
October 31, 1977
Date of Patent:
April 24, 1979
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Karl G. Untch, Stefan H. Unger, Brian Lewis
Abstract: Compounds of the formula ##STR1## wherein Z is hydroxymethylene, esterified hydroxymethylene, carbonyl, or ketal-, thioketal- or hemithioketal- protected carbonyl, and the pharmaceutically acceptable acid addition salts thereof, are useful as anticonvulsant and anti-secretory agents.
Abstract: This invention is a filtration and aeration apparatus which comprises (a) an elongated tubular member which is closed at its lower end, open at the opposite end, and provided at its lower portion with a plurality of passages which extend through the longitudinal wall of the tubular member and (b) an air delivery means for supplying air to the interior of said tubular member at a point at or slightly below the lowermost level of said passages so that the air is discharged parallel to the length of said tubular member in the interior of said tubular member. Another aspect of this invention is a unique air delivery means which comprises an air tube connected to and extending into a chamber designed to allow air to escape from said chamber through passages in the chamber walls so that the air is discharged through said chamber wall passages in a direction opposite from the direction said air is delivered to said chamber through said air tube.
Type:
Grant
Filed:
December 22, 1976
Date of Patent:
March 20, 1979
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
George D. Bliss, Joseph E. Kercso, Richard J. McGuire
Abstract: 1-Alkylamino-3-(?2-(endobicyclo?3.1.0!-hex-6-yl)ethylaminocarbonyl!naphthyl oxy)-2-propanols and methods for preparing these compounds are disclosed. The compounds are useful in the treatment of hypertension and abnormal heart conditions in mammals. These compounds are prepared by the treatment of the corresponding 1,2-epoxy-3-?2-(endobicyclo?3.1.0!hex-6-yl)ethylaminocarbonyl!naphthyloxy) -propane with an alkylamine having the desired alkyl substituent or by base or acid hydrolysis of the corresponding 2-optionally substituted -3-alkyl-5-(?2-(endobicyclo?3.1.0!hex-6-yl)ethylaminocarbonyl!naphthyloxym ethyl)oxazolidine. These latter compounds can be prepared by condensing a hydroxy-substituted naphthalene with a 3-alkyl-5-tosyloxymethyloxazolidine such substituted or unsubstituted at the 2-position or alternatively, by treating the former aminopropanol compounds of the present invention with an aldehyde having the desired substituent.
Abstract: Valuable 2-aryl-propionic acids are prepared by the direct coupling of aryl magnesium bromides with a mixed magnesium halide complex of alpha-bromopropionic acid.
Abstract: 5-Substituted-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids of the formula ##STR1## wherein Y is a moiety selected from the group consisting of ##STR2## in which R is hydrogen, methyl, chloro or bromo, the R substitution being at the 3, 4 or 5 positions of the thiophene ring,R.sup.1 is hydrogen, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having from 1 to 4 carbon atoms, chloro, fluoro or bromo, the R.sup.1 substitution being at the ortho, meta or para positions of the aroyl group, andR.sup.2 is hydrogen or a lower alkyl group having from 1 to 4 carbon atoms, are prepared, by hydrolysis, from their corresponding nitriles.
Type:
Grant
Filed:
May 30, 1978
Date of Patent:
February 20, 1979
Assignee:
Syntex (USA) Inc.
Inventors:
Albert R. Van Horn, Pasquale G. Gallegra
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 to 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: 3-[3-(methyl-1,3,4-thiadiazol-5-ylthio)-prop-1-(t)-enyl]-7.beta.-(.alpha.-s ubstituted acetamido)-ceph-3-em-4-carboxylic acids; 3-[3-(3-methyl-1,2,4-thiadiazol-5-ylthio)-prop-1-(t)-enyl]-7.beta.-(.alpha .-substituted acetamido)-ceph-3-em-4-carboxylic acids; and 3-[3-(2-methyl-1,3,4-oxadiazol-5-ylthio)-prop-1-(t)-enyl]-7.beta.-(.alpha. -substituted acetamido)-ceph-3-em-4-carboxylic acids and derivatives and salts thereof 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: (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: This invention relates to novel 4-(8X-6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-yl)-4-oxobutyric acids and their derivatives, wherein X is hydrogen, methoxy or chloro, methods of preparation, compositions and uses thereof.
Abstract: 4,5-Dihydro-2-lower alkoxycarbonylamino-4-phenylimidazole, and substituted phenyl derivatives thereof, and pharmaceutically acceptable salts thereof, and methods of preparing such compounds. In one method, the compounds can be prepared by treating the corresponding .beta.-amino-.beta.-(phenyl or substituted phenyl)-ethylamine with the desired 1,3-bis(alkoxycarbonyl)-S-methylisothiourea or 1-alkoxycarbonyl-S-methylisothiourea. The compounds can also be prepared by treating the corresponding 2-amino-4,5-dihydro-4-(phenyl or substituted phenyl)-imidazole with the desired dialkylcarbonate. The subject compounds are useful as psychotherapeutic agents for treating, preventing or palliating abnormal conditions, in mammals, which are related to the central nervous system.
Type:
Grant
Filed:
October 17, 1977
Date of Patent:
December 12, 1978
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Adolph P. Roszkowski, Colin C. Beard, Charles Dvorak, Klaus Weinhardt
Abstract: The present invention relates to novel assay reagents, their composition, methods of preparation, and use in the detection and measurement of various biological systems and/or components, e.g. enzymes, antibodies, antigens, and periodate concentration. This invention in its basic form utilizes a class of compounds having, inter alia., a backbone chain, an indicator group, and vicinal oxidizable groups.
Abstract: Compounds of the formula ##STR1## wherein R is lower alkyl; R.sup.1 is substituted or unsubstituted phenyl or phenyl straight chain lower alkyl; R.sup.2 is substituted or unsubstituted phenyl, phenyl straight chain lower alkyl or phenyl straight chain lower alkenyl; and wherein said substitution, solely in the phenyl ring of the aforesaid groups, comprises one or more substituents independently selected from the group consisting of lower alkyl, lower alkoxy, halo and trifluoromethyl; X is oxygen or sulfur; n is an integer of from 1 to 4 with the proviso that n cannot be 1 when X is oxygen and R.sup.1 is phenyl or substituted phenyl; and the antimicrobial acid addition salts thereof are useful as antifungal antibacterial and antiprotozoal agents.
Abstract: 1-Alkylamino-3-([2-(endobicyclo[3.1.0]hex-6-yl)ethylaminocarbonyl]thienylox y)-2-propanols and methods for preparing these compounds are disclosed. The compounds are useful in the treatment of hypertension and abnormal heart conditions in mammals. These compounds are prepared by the treatment of the corresponding 1,2-epoxy-3-[2-(endobicyclo[3.1.0]hex-6-yl)ethylaminocarbonyl]heterocyclic aryloxy)propane with an alkylamine having the desired alkyl substituent or by base or acid hydrolysis of the corresponding 2-optionally substituted-3-alkyl-5-([2-(endobicyclo[3.1.0]hex-6-yl)ethylaminocarbonyl]h eterocyclic aryloxymethyl)oxazolidine. These latter compounds can be prepared by condensing a halo-substituted thiophene with a 3-alkyl-5-hydroxymethyloxazolidine such substituted or unsubstituted at the 2-position or alternatively, by treating the former aminopropanol compounds of the present invention with an aldehyde having the desired substituent.
Type:
Grant
Filed:
October 31, 1977
Date of Patent:
October 31, 1978
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Karl G. Untch, Stefan H. Unger, Brian Lewis
Abstract: Visual defects of the human eye in the form of refractive errors such as myopia, hyperiopia, astigmatism, athakis and keratoconus are corrected by a therapeutic method which includes the step of fitting to the patient's eye a corrective contact lens fabricated from a copolymer of a polysiloxanylalkyl acrylic ester and an alkyl acrylic ester. These visual corrections are made in accordance with this method with concommitent reduction in corneal edema since lenses so used have improved oxygen permeability. According to the preferred practice of this method, the lenses utilized have improved wettability which increases wearing confort and reduces interference with corneal metabolism, thereby extending the time period during which the corrective effect of the method is achieved. The corrective effect of this method is also enhanced by the capability of the lenses utilized therein to be precisely machined and polished.
Abstract: Compounds of the formula ##STR1## wherein R is alkyl having 1 to 4 carbon atoms, .beta.-haloethyl, allyl, propargyl, cyclopentyl or benzyl; R.sup.1 is hydrogen or an .alpha.-substituted acetamido group; R.sup.2 is hydrogen or a protecting group; and the pharmaceutically acceptable salts thereof. The 7.beta.-amino compounds are useful as intermediates for the 7.beta.-(.alpha.-substituted acetamido) compounds which are useful as antibacterials against a wide variety of gram positive and gram negative bacteria.