Abstract:
The invention relates to the pyrrolyl-substituted hydroxamic acid derivatives of the formula ##STR1## wherein R represents aryl, aryl-lower alkyl, cycloalkyl, bicycloalkyl or adamantyl; R.sub.1 and R.sub.2 represent hydrogen or lower alkyl; Y represents a direct bond, lower alkylene, lower alkenylene or lower alkadienylene; Z represents ##STR2## wherein R.sub.3 represents hydrogen or acyl; R.sub.4 represents lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, aryl or aryl-lower alkyl; or Z represents ##STR3## wherein R.sub.3 represents hydrogen or acyl; R.sub.5 represents lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, aryl, aryl-lower alkyl, amino or N-(mono- or di-lower alkyl)-amino; R.sub.6 and R.sub.7 represent hydrogen or lower alkyl; and pharmaceutically acceptable salts thereof provided that R.sub.3 represents hydrogen; which are useful as lipoxygenase inhibitors.
Abstract:
For inhibiting 3-hydroxy-3-methylglutaryl coenzyme A and cholesterol biosynthesis, the novel disubstituted pyrroles of the formula ##STR1## in which R.sup.1 is aryl or heteroaryl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen or cycloalkyl, or optionally substituted alkyl, aryl or heteroaryl,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.6 is hydrogen or alkyl, and R.sup.7 is hydrogen, a cation or alkyl, aryl or aralkyl.
Abstract:
Compounds are disclosed, including 2-diethylamino-3-isobutoxy-N-phenyl-N-2-furanyl-methyl-propylamine and compounds of the formula: ##STR1## wherein R.sub.1 is an iso-C.sub.4 -C.sub.6 -alkyl radical; A is a valency bond or a straight-chained or branched alkyl radical containing up to 6 carbon atoms; R.sub.4 is a phenyl radical which is unsubstituted or substituted one or more times by C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.1 -C.sub.3 -alkoxy, C.sub.2 -C.sub.6 -alkenyloxy, hydroxy-C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkylenedioxy, hydroxy-C.sub.1 -C.sub.3 -alkoxy, C.sub.1 -C.sub.3 -alkoxy-C.sub.1 -C.sub.3 -alkoxy, C.sub.1 -C.sub.6 -alkylamino, di(C.sub.1 -C.sub.6 -alkyl)amino, C.sub.1 -C.sub.3 -alkoxycarbonyl-C.sub.1 -C.sub.3 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulphinyl, C.sub.1 -C.sub.6 -alkylsulphonyl, C.sub.1 -C.sub.6 -alkylsulphonyloxy, carboxyl, C.sub.1 -C.sub.3 -alkoxycarbonyl, aminocarbonyl, mono- or di(C.sub.1 -C.sub.6 -alkyl)aminocarbonyl, halo-C.sub.1 -C.sub.6 -alkyl, cyano, or halogen; and R.sub.5 is a benzyl radical substituted at least once by C.sub.1 -C.sub.3 -alkoxy. The compounds are useful for the treatment of heart circulatory diseases.
Abstract:
2-Substituted-1-naphthols are 5-lipoxygenase inhibitors which make them useful in the treatment of inflammation, obstructive lung disease and/or psoriasis. Useful 2-substituent groups are alkyls, alkenyls, alkynyls, cycloalkyls, cycloalkenyls, the groups CH.sub.2 --C.tbd.C--(CH.sub.2).sub.m R.sup.5 and CH.dbd.CH--(CH.sub.2).sub.n R.sup.5 (where m is 1-4, n is 0-3 and R.sup.5 includes phenyl, COOR.sup.9, where R.sup.9 is H or alkyl or 1-4 carbons, AR.sup.6 (where A is a methylene chain and R.sup.6 is a variety of groups including Cl, Br, I, CHO, CN, COOR.sup.9, NH.sub.2, SC(NH)NH.sub.2, phenyl, P(O)(OR.sup.9).sub.2, etc.), and CHR.sup.7 R.sup.21 (where R.sup.7 is a variety of aromatic and heterocyclic groups and R.sup.21 is H, optionally substituted phenyl and a variety of heterocyclic groups).
Abstract translation:2-取代的1-萘酚是5-脂氧合酶抑制剂,其可用于治疗炎症,阻塞性肺病和/或牛皮癣。 有用的2-取代基是烷基,烯基,炔基,环烷基,环烯基,基团CH 2 -C 3 CF(CH 2)m R 5和CH = CH-(CH 2)n R 5(其中m是1-4,n是0-3 并且R 5包括苯基,COOR 9,其中R 9是H或烷基或1-4个碳,AR 6(其中A是亚甲基链,R 6是各种基团,包括Cl,Br,I,CHO,CN,COOR9,NH2,SC (NH)NH 2,苯基,P(O)(OR 9)2等)和CHR 7 R 21(其中R 7是多种芳族和杂环基团,R 21是H,任选取代的苯基和各种杂环基团)。
Abstract:
A polyimide composition consisting essentially of recurring units having the following structural formula: ##STR1## is produced by the copolymerization of a bismaleimide and bis[4-(3,4-dimethylenepyrrolidyl)phenyl] methane.
Abstract:
N-monosubstituted and N,N-disubstituted amides of the 1-methyl-5-p-toluoylpyrrole-2-acetic acid, which are active as antiinflammatory, analgesic, antipyretic, antisecretive and antitussive agents, are disclosed.These amides are prepared by reacting an amine with an activated derivative of the 1-methyl-5-p-toluoylpyrrole-2-acetic-acid of formula ##STR1## where X is an activating group suitable for promoting the formation of an amide bond.
Abstract:
2,3-Dihydro-1H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid compounds of the formula, ##STR1## in which Y is OH;O.sup.- M.sup.+, wherein M is an alkali metal; orNRR', wherein R is lower alkyl and R' is lower alkyl or aryl, or NRR' is the residue of a saturated cyclic amine,are prepared from pyrrole.
Abstract:
Certain N-acetonyl-substituted-amides of the formula: ##STR1## wherein A is a heterocycle, a phenylalkyl, a phenylalkoxy, naphthyl, cycloalkyl, alkoxyalkyl, alkyl, haloalkyl or alkenyl group; X, Y and Z are selected from the group consisting of hydrogen, halo, cyano, thiocyano, isothiocyano, methylsulfonyloxy, thio(C.sub.1 -C.sub.2) alkyl, (C.sub.1 -C.sub.2)alkoxy, carbamoyloxy, thiocarbamoylthio, hydroxy, azide, trifluoromethylcarboxy, (C.sub.1 -C.sub.4)alkylcarbonyloxy, phenylcarbonyloxy, phenoxy, thiophenyl, imidazolyl or triazolyl group as described herein; R.sup.1 and R.sup.2 are each independently a hydrogen atom or a (C.sub.1 -C.sub.6)alkyl group; and compositions containing these amides are fungicidally active, particularly against phytopathogenic fungi.
Abstract translation:某些具有下式的N-丙酰基取代的酰胺:其中A是杂环,苯基烷基,苯基烷氧基,萘基,环烷基,烷氧基烷基,烷基,卤代烷基或烯基; X,Y和Z选自氢,卤素,氰基,硫氰基,异硫氰基,甲基磺酰氧基,硫代(C1-C2)烷基,(C1-C2)烷氧基,氨基甲酰氧基,硫代氨基甲酰硫基,羟基,叠氮化物,三氟甲基羧基,( C 1 -C 4)烷基羰基氧基,苯基羰基氧基,苯氧基,噻吩基,咪唑基或三唑基; R1和R2各自独立地为氢原子或(C1-C6)烷基; 并且含有这些酰胺的组合物是杀真菌活性的,特别是针对植物病原真菌。
Abstract:
A polyimide composition consisting essentially of recurring units having the following structural formula: ##STR1## is produced by the copolymerization of a bismaleimide and bis[4-(3,4-dimethylenepyrrolidyl)phenyl]methane.
Abstract:
This invention relates to new lipoxygenase inhibitors possessing anti-inflammatory and anti-allergic properties. The present new compounds are of the formula: ##STR1## and salts thereof; wherein, R is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aralkyl, phenyl, naphthyl, or a nitrogen oxygen or sulfur heterocyclic; andY.sub.1 and Y are independently hydrogen, lower alkyl, hydroxy, lower alkoxy, aryloxy, lower aralkoxy, aryl, lower aralkyl, carboxy, lower carbalkoxy, lower carbaralkoxy, carbaryloxy, formyl, or alkyl, alkenyl or alkynyl containing up to 6 carbon atoms in the principal chain and up to a total of 10 carbon atoms;provided that when Y and Y.sub.1 are both hydrogen or when Y.sub.1 is hydrogen and Y is CHO, the R is other than hydrogen, unsubstituted phenyl, or lower alkyl.