Abstract: Mono- or poly-unsaturated fatty acid hydrazides, e.g. cis,-9-octadecenoic acid, 2-(o-methylphenyl)-hydrazide are useful as pharmaceutical agents and are obtainable by reacting a derivative, e.g. mixed anhydride, of a long chain unsaturated carboxylic acid with an appropriate hydrazine compound.
Abstract: A process for the production of compounds of formula I, ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms,R.sub.2 is hydrogen, fluorine, chlorine or bromine, andR.sub.3 is bromine, iodine, isobutyl, tert. butyl, cyclohexyl, cyclohexenyl; or phenyl, optionally substituted by fluorine, chlorine, bromine or alkoxy of 1 to 4 carbon atoms; or a radical of formula II, ##STR2## in which either R.sub.4 and R.sub.5 are the same or different and each signifies alkyl of 1 to 3 carbon atoms,orR.sub.4 and R.sub.5 together signify the radical --(CH.sub.2).sub.n --, in which n is 4 or 5, the radical --CH.sub.2 --CH.sub.2 --0--CH.sub.2 --CH.sub.2 --, the radical --CH.sub.2 --CH.dbd.CH--CH.sub.2 --, or the radical --CH.sub.2 --CH.sub.2 --N(R.sub.6)--CH.sub.2 --CH.sub.2 --, in which R.sub.6 is hydrogen or alkyl of 1 to 3 carbon atoms. Hydroxyketone and hydroxy imine intermediates are also disclosed.The compounds of formula I are known to exhibit anti-inflammatory activity.
Abstract: The compounds are amino- or cyano-bearing dihydroquinolines, which have either of the combinations of (a) 2-amino, 3-carboxylic and 4-oxo functions, or (b) 2-oxo, 3-cyano and 4-hydroxy functions, and may be optionally substituted at 1 or 2 of the 5, 6, 7 or 8 positions, eg 1-allyl-2-amino-1,4-dihydro-6,7-dimethoxy-4-oxo-quinoline-3-carboxylic acid ethyl ester, and 1-allyl 3-cyano-1,2-dihydro-4-hydroxy-6,7-dimethoxy-2-oxo-quinoline. The compounds are useful as pharmaceuticals.
Abstract: 2-amino-4H-3,1 benzoxazines, eg 6-chloro 2-dimethylamino-4H, 3,1-benzoxazine, are useful as herbicides. The compounds may be prepared by reacting an amine with a 2-halomethylphenyl isocyanate.
Abstract: Cyclopropanyl-group-bearing-hydrazides, e.g. cis-2-octyl-cyclopropanoctanoic acid, 2-(o-methylphenyl)-hydrazide, are useful as pharmaceutical agents and are obtainable by reacting a derivative, e.g. mixed anhydride, of a cyclopropanyl-group bearing-long chain carboxylic acid with an appropriate hydrazine.
Abstract: Long chain fatty acid amides of styryl hexahydroindolinols in which the amido portions have ethyleneically unsaturated positions or cyclopropanyl rings, eg 1-(1-oxo-9-cis-octadecenyl)-(3aRS, 4RS, 7aRS)-4-(Z)-(3,4-dimethoxy)-styryl-hexahydro-4-indolinol, are useful as cholesterol ester-reducing agents and are obtainable by reacting corresponding long chain carboxylic acids (or derivatives thereof) with appropriate 4-styryl-4-hexahydroindolinols.
Abstract: Unsaturated fatty acid amides of benzocycloalkylamines, eg. N-(1-indanyl)-cis,cis-9,12-octadecadienylamide, are useful as pharmaceutical agents and are obtainable by reacting a mixed anhydride of a long chain unsaturated carboxylic acid with an appropriate benzocycloalkylamine.
Abstract: 2-amino-4H-3,1 benzoxazines, e.g. 6-chloro 2-dimethylamino-4H, 3,1-benzoxazine, are useful as herbicides. The compounds may be prepared by reacting an amine with a 2-halomethylphenyl isocyanate.
Abstract: The present invention provides compounds of formula I, ##STR1## wherein R.sub.1 and R.sub.2 are, independently, hydrogen, fluorine, chlorine, trifuoromethyl, alkyl of 1 to 4 carbon atoms, or alkoxy of 1 to 4 carbon atoms, andR.sub.3 is hydrogen, or alkoxy of 1 to 4 carbon atoms, with the proviso that when R.sub.3 is alkoxy then at least one of R.sub.1 and R.sub.2 is alkoxy, orR.sub.1 and R.sub.2 are bound to adjacent ring carbon atoms and are together --(CH.sub.2).sub.m --, wherein m is 3 or 4, --CH.dbd.CH--CH.dbd.CH--, or --O--CH.sub.2 --X--, wherein X is --O-- or --CH.sub.2 --, andR.sub.3 is hydrogen, fluorine, chlorine, trifluoromethyl, alkyl of 1 to 4 carbon atoms, or alkoxy of 1 to 4 carbon atoms,Useful as hypolipidemic agents and anti-arrhythmics.
Abstract: Disclosed are compounds of the class 1-phenyl-2,3-butadien-1-ol e.g. 2-(p-biphenylyl)-3,4-pentadien-2-ol, which are useful by reason of their pharmacological activity in animals, e.g., as anti-inflammatory agents and tranquilizers. Said compounds can be prepared, e.g., by reduction of a corresponding 4-substituted-1-phenyl-2-butyne-1-ol with a complex hydride such as lithium aluminum hydride.
Abstract: 2-Amino-3-pyridyl (or phenyl) nitromethylketones are prepared eg by reacting a 3,4-dihydro-1,3-dioxo-1H-pyrido [2,3-d][1,3]oxazine (a 3-azaisatoic anhydride) with the carbanion resulting from the reaction of nitromethane with a porton abstracting agent. The compounds are useful as anti-allergic agents.
Abstract: Alpha-cyano-o-anisidino derivatives, e.g., alpha-cyano-o-acetanisidide, are useful as hypolipidemic agents. The compounds are obtainable by reacting an appropriate 2-amidophenol with a haloalkylnitrile.
Abstract: Disclosed are compounds of the class 1-phenyl-2,3-butadien-1-ol e.g. 2-(p-biphenyl)-3,4-pentadien-2-ol, which are useful by reason of their pharmacological activity in animals, e.g., as anti-inflammatory agents and tranquilizers. Said compounds can be prepared, e.g., by reduction of a corresponding 4-substituted-1-phenyl-2-butyne-1-ol with a complex hydride such as lithium aluminum hydride.
Abstract: Phenoxyphenyl pyridyl carbinols and ketones, e.g., p-phenoxyphenyl-nicotinyl ketone, are useful as pharmaceutical agents. The ketones are obtainable by oxidation of corresponding phenoxyphenyl pyridyl carbinols.
Abstract: The compounds are 1-aryl-1-alknyl-1-(t-butyl)-substituted methanols, e.g. 3-(2'-naphthyl)-4,4-dimethyl-pent-1-yn-3-ol, are useful as hypolipidemic agents, and are prepared by reacting a 4-aryl-pivalophenone with a metallo-alkynyl reagent under Grignard reaction conditions.
Abstract: The compounds are 1-aryl-1-lower alkyl-substituted-1-buten-3-ols, butan-3-ols, and acylation products thereof, e.g., (p-biphenylyl)-2-penten-4-ol and are useful as pharmaceuticals.
Abstract: The compounds are 4-aryl substituted buta-2,3-dienoic acids and esters thereof which may also be lower alkyl-substituted at any of the 2- and 4- positions, e.g., 4-(p-methoxyphenyl)-2-methyl-buta-2,3-dienoic acid. The compounds are useful as pharmaceuticals, e.g., as antiinflammatory agents and hypolipidemic agents.
Type:
Grant
Filed:
November 17, 1976
Date of Patent:
February 14, 1978
Assignee:
Sandoz, Inc.
Inventors:
Eugene E. Galantay, Faizulla G. Kathawala
Abstract: Hydroxymethyl-substituted-2(1H)-quinazolinones, e.g., 7-hydroxymethyl-1-isopropyl-4-phenyl-2(1H)-quinazolinone, are useful as anti-inflammatory agents.