Abstract: 2-(2'-Naphthyl) acetaldehyde derivatives optionally substituted at the 2 position and/or positions C-1',4',5',7' or 8'; and/or position C-6' or positions C-5' and 7' exhibit anti-inflammatory, analgesic, antipyretic and anti-pruritic activity.
Abstract: Compounds of the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is phenyl, phenyl straight chain lower alkyl or phenyl straight chain lower alkenyl or one of the above substituted in the phenyl ring with one or more substituents independently selected from the group consisting of lower alkyl of from one to four carbon atoms, halo and trifluoromethyl; the other of R.sup.1 and R.sup.2 is alkyl, cyclohexyl, cyclohexyl lower alkyl or cyclohexyl substituted with from 1 to 3 lower alkyl groups; X is oxygen or sulfur; n is an integer of from 1 to 8 with the proviso that n is not 1 when R.sup.1 is phenyl or substituted phenyl; and the antimicrobial acid addition salts thereof are useful as antifungal, antibacterial and antiprotozoal agents.
Abstract: Biotin is prepared by (a) ozonizing methylcyclohexene; (b) reacting nitromethane with the methyl-6-oxohexanoate from a to form 7-nitro-6 hydroxyheptanoic acid methyl ester; (c) acylating to form the corresponding 6 acyloxy compound; (d) forming a double bond at the 6 position; (e) reacting the product of d with nitroethanethiol to form dl-7-thia-6-nitromethyl-9-nitro-nonanoic acid methyl ester; (f) forming a furoxan by cyclization; (g) reducing the furoxan and acylating to form dl-2(4-carbomethoxybutyl)-3,4-bis(acylamido)-2,5-dihydro thiophene; (h) selectively hydrogenating to form the 3,4-cis-bis(acylamido)-2,5-dihydro thiophene; and (i) hydrolyzing and cyclizing to form dl-biotin. The products formed at steps (e)-(h) are novel, as are the individual steps (e), (f), (g), and (h).
Abstract: Novel 1-phenethylimidazoles substituted at the position .beta. to the imidazole ring by an optionally substituted hydrocarbyl carbonate or a mono-, di-, or trithiocarbonate are useful as antimicrobial agents and as intermediates in the preparation of novel 1-phenethylimidazoles substituted at the position .beta. to the imidazole with a mercapto. Both the former and latter compounds are useful as intermediates in the preparation of certain 1-[.beta.-(R-thio)phenethyl]imidazoles.
Abstract: Novel 1-phenethylimidazoles substituted at the position .beta. to the imidazole ring by an optionally substituted hydrocarbyl ester, thioester, or dithioester are useful as antimicrobial agents and as intermediates in the preparation of novel 1-phenethylimidazoles substituted at the position .beta. to the imidazole with a mercapto. Both the former and latter compounds are useful as intermediates in the preparation of certain 1-[.beta.-(R-thio)phenethyl] imidazoles.
Abstract: 2-Substituted-5-oxo-5H-dibenzo [a,d] cycloheptenes represented by the following formula: ##STR1## where one of R.sup.2 and R.sup.3 is hydrogen, and the other is hydrogen, methyl, or ethyl, or together R.sup.2 and R.sup.3 are methylene; the dotted line represents an optional, additional bond between the carbon atoms at the 10- and 11-positions; and the pharmaceutically acceptable esters and ethers thereof. The compounds have anti-inflammatory, analgesic, and antipyretic activities and, accordingly, are useful in the treatment of inflammation, pain and pyrexia.
Abstract: Compounds of the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is alkyl or the group ##STR2## IN WHICH N IS 0 TO 3 AND THE OTHER OF R.sup.1 and R.sup.2 is benzyl, substituted benzyl, phenyl or substituted phenyl, said substituted benzyl and substituted phenyl substituted on the phenyl ring with one or more substituents independently selected from the group consisting of halo, lower alkyl and trifluoromethyl; X and Y are independently oxygen or sulfur with the proviso that Y is not oxygen when R.sup.2 is phenyl or substituted phenyl; and the antimicrobial acid addition salts thereof are useful as antifungal, antibacterial and antiprotozoal agents.
Abstract: This invention is an apparatus and process for culturing aquatic animals. The apparatus comprises a container suitable for retaining water; a plurality of platforms vertically spaced from each other located in said container, the platforms being substantially parallel to each other and being designed to allow water to circulate therethrough while at the same time allowing solid food particles when dropped into the platform area to pass therethrough; and a feeding station placed on each of the platforms in a manner so that each feeding station is vertically and horizontally spaced from each adjacent station, has a structure such that the solid food particles are retained on the feeding station, and is substantially the same area as the adjacent feeding station.
Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently benzyl substituted benzyl, phenyl or substituted phenyl, said substituted benzyl and substituted phenyl substituted on the phenyl ring with one or more substituents independently selected from the group consisting of halo, lower alkyl and trifluoromethyl; X and Y are independently oxygen or sulfur with the proviso that Y is not oxygen when R.sup.2 is phenyl or substituted phenyl; and the antimicrobial acid addition salts thereof are useful as antifungal, antibacterial and antiprotozoal agents.
Abstract: Compounds of the formula ##STR1## wherein R is alkyl, cycloalkyl, cycloalkyl lower alkyl, phenyl or phenyl lower alkyl, said phenyl and phenyl lower alkyl optionally substituted on the phenyl ring with one or more substituents independently selected from the group consisting of halo, lower alkyl and trifluoromethyl; and X is oxygen or sulfur with the proviso that X is not oxygen when R is phenyl or substituted phenyl; and the antimicrobial acid addition salts thereof are useful as antifungal, antibacterial and antiprotozoal agents.
Type:
Grant
Filed:
March 8, 1976
Date of Patent:
July 19, 1977
Assignee:
Xyntex (U.S.A) Inc.
Inventors:
Keith A. M. Walker, Stefan Howard Unger
Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently alkyl or the group ##STR2## IN WHICH N IS 0 TO 3; X and Y are independently oxygen or sulfur; and the antimicrobial acid addition salts thereof are useful as antifungal, antibacterial and antiprotozoal agents.
Abstract: 2-Substituted-5-oxo-5H-dibenzo[a,d]cycloheptenes represented by the following formula: ##STR1## where R' is hydrogen, alkyl having 1 to 12 carbon atoms, or ##STR2## where n is an integer from 2 to 4, inclusive, and R.sup.4 and R.sup.5 are independently lower alkyl having 1 to 6 carbon atoms or together R.sup.4 and R.sup.5 and the nitrogen atom to which they are attached form a heterocyclic ring having 5 or 6 total ring atoms; and the pharmaceutically acceptable salts thereof. The compounds are useful in the treatment of auto-immune diseases and allergic reactions.
Abstract: 3-Carboxy-5-substituted-thiacycl[2.2.2]azines of the formula: ##STR1## wherein R is phenyl or phenyl monosubstituted in the meta or para position with fluoro, chloro, lower alkyl of from 1 to 4 carbon atoms or lower alkoxy of from 1 to 4 carbon atoms, and the pharmaceutically acceptable salts thereof.These compounds are useful as anticomplimentary agents, specifically for the treatment of inflammatory conditions, auto-immune diseases, allergic reactions and vascular diseases.
Abstract: An axial tomographic system having scanner means normally in an "off" condition where all power sources associated therewith are electrically isolated from the units driven thereby, means for activating the scanner means to establish an "on" condition, control means including means to measure one or more system parameters when the scanner means is in an "on" condition and to determine if the measured parameters are within predetermined limits therefor, and means for maintaining the "on" condition only if the control means is properly operational and all measured system parameters are within the predetermined limits therefor.
Abstract: This application relates to 1,5(6)-disubstituted benzimidazole-2-carbamate derivatives represented by the following formula: ##STR1## where R is lower alkyl having 1 to 4 carbon atoms; R.sup.1 is --SOR.sup.2, --SR.sup.5, --OR.sup.5 or M'(CH.sub.2).sub.n MR.sup.7 ; R.sup.2 is lower alkyl having from 1 to 6 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, lower alkenyl or lower alkynyl having 3 to 6 carbon atoms, or aralkyl or aryl; R.sup.5 is lower alkenyl, lower alkynyl or aralkyl; R.sup.7 is lower alkyl having 1 to 4 carbon atom, or aryl; M and M' are independently O, S, ##STR2## n is 1-4; and R.sup.8 is lower alkyl having 1 to 12 carbon atoms optionally substituted with a --COOR group where R is lower alkyl having 1 to 4 carbon atoms, aryl or aralkyl. The R.sup.1 substitution is at the 5(6)-position.The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.
Type:
Grant
Filed:
June 18, 1976
Date of Patent:
June 21, 1977
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Colin C. Beard, John A. Edwards, John H. Fried
Abstract: Compositions and method for treating, or reducing the occurrence, of stomach and duodenum ulcers. The compositions and methods are characterized by the administration of a composition containing (dry weight basis) 10 to 40% sucrose; 10 to 40% glucose; 12 to 20% amino acids and 7.5 to 12% lipids. The composition is typically administered orally as an aqueous liquid emulsion.
Abstract: 2-Substituted-5-oxo-5H-dibenzo[a,d]cycloheptenes represented by the following formula: ##STR1## where R' is hydrogen, alkyl having 1 to 12 carbon atoms, or ##STR2## where n is an integer from 2 to 4, inclusive, and R.sup.4 and R.sup.5 are independently lower alkyl having 1 to 6 carbon atoms or together R.sup.4 and R.sup.5 and the nitrogen atom to which they are attached form a heterocyclic ring having 5 or 6 total ring atoms; one of R.sup.2 and R.sup.3 is hydrogen and the other is hydrogen, methyl, or ethyl, or together R.sup.2 and R.sup.3 are methylene; and the pharmaceutically acceptable salts thereof. The compounds have anti-inflammatory, analgesic, and antipyretic activities and, accordingly, are useful in the treatment of inflammation, pain and/or pyrexia.
Abstract: An inhalation device having an elongate housing having one or more passageways for the passage of air therethrough. Each passageway, of relatively small diameter, opens into an emptying chamber, of relatively greater diameter, adjacent that end of the housing which is adapted for insertion into the mouth or nose of a user. Adjacent that end of the emptying chamber closest to the passageway(s), the housing has means for receiving or presenting a unit dose of powdered medicament for administration. Means are provided to open the medicament holder as it is being inserted into, or after it has been inserted into, the means for receiving or presenting a unit dose of powdered medicament for administration. During inhalation, the air stream passing over and directed into the powdered medicament holder entrains the powdered medicament which is then carried into the nose, throat or lungs of the user where beneficial or therapeutic action of the medicament occurs.
Abstract: 7(8)-substituted triazinobenzimidazoles represented by the formula: ##STR1## where R is a lower alkyl group having 1 to 4 carbon atoms; R' is diloweralkylaminoalkyl (C.sub.2-6) or alkyl having 1 to 18 carbon atoms; R.sup.2 is phenylsulfinyl, phenoxyethoxy, benzyloxyethoxy, methoxyethylsulfinyl, or 3-chloroprop-1-ylsulfinyl; the R.sup.2 -substitution being at the 7(8)-position; or a pharmaceutically acceptable salt thereof.The compounds are useful as pesticides, particularly as antifungal and anthelmintic agents.
Type:
Grant
Filed:
March 8, 1976
Date of Patent:
March 8, 1977
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Colin C. Beard, John A. Edwards, John H. Fried