摘要:
2-Substituted-1-naphthols are 5-lipoxygenase inhibitors which make them useful in the treatment of inflammation, obstructive lung diseases 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 of 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).
摘要:
Disclosed are compounds of the formula ##STR1## wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, 2-imidazolyl or 4,5-dihydro-2-imidazolyl or any said grouping substituted by lower alkyl; R and R.sub.0 independently represent hydrogen, lower alkyl, (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, or aryl-lower alkyl in which aryl represents phenyl, pyridyl, thienyl, furyl, biphenyl or naphthyl, each unsubstituted or mono- or di-substituted by halogen, lower alkyl, hydroxy, acyloxy, lower alkoxy, trifluoromethyl or cyano; A represents straight chain (C.sub.2 -C.sub.5)-alkylene; or A represents straight chain (C.sub.2 -C.sub.5)-alkylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by amino or acyl-amino, by amino-lower alkyl, by acylamino-lower alkyl, by (C.sub.3 -C.sub.7)-cycloalkyl, by (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, by aryl or aryl-lower alkyl in which aryl represents phenyl or phenyl mono- or disubstituted by halogen, lower alkyl, lower alkoxy, hydroxy, acyloxy, trifluoromethyl or cyano; or A represents phenylene or cyclohexylene; pharmaceutically acceptable prodrug derivatives of any said compounds having a free carboxy group; pharmaceutically acceptable salts of any said compounds with a salt-forming group; methods for synthesis; pharmaceutical compositions thereof; and use thereof as enkephalinase inhibitors.
摘要:
Compounds of the formula ##STR1## wherein A is ##STR2## B is ##STR3## R.sup.1 is hydrogen; halogen, cyano or optionally substituted C.sub.1-4 alkyl; andQ is NR.sup.8 R.sup.9 or ##STR4## where R.sup.2 to R.sup.11 are substituents of various types. The compounds are useful as fungicides.
摘要:
The described novel pyridine derivatives are those of the general formula I ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl, phenyl, benzyl, phenyl substituted by C.sub.1 -C.sub.4 -alkyl, halogen, C.sub.1 -C.sub.4 -alkoxy, NO.sub.2 and/or CF.sub.3, or benzyl substituted by C.sub.1 -C.sub.4 -alkyl, halogen, C.sub.1 -C.sub.4 -alkoxy, NO.sub.2 and/or CF.sub.3,R.sub.1 and R.sub.2 independently of one another are each hydrogen, C.sub.1 -C.sub.4 -alkyl, halogen or C.sub.1 -C.sub.4 -alkoxy,R.sub.3, R.sub.4 and R.sub.5 independently of one another are each hydrogen, halogen, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, phenyl, or phenyl substituted by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, halogen, NO.sub.2 and/or CF.sub.3,U and V independently of one another are each C.sub.1 -C.sub.6 -alkyl, or alkyl substituted by halogen or C.sub.1 -C.sub.4 -alkoxy, or together form one of the following alkylene bridges: ##STR2## R.sub.a is hydrogen, C.sub.1 -C.sub.12 -alkyl, C.sub.1 -C.sub.12 -alkyl which is mono- or polysubstituted by halogen, or is phenyl, phenyl which is mono- or polysubstituted by halogen and/or C.sub.1 -C.sub.4 -alkyl, or is the group --CH.sub.2 --Z--R.sub.h,R.sub.b is C.sub.1 -C.sub.12 -alkyl, C.sub.1 -C.sub.12 -alkyl which is mono- or polysubstituted by halogen, or is phenyl, phenyl which is mono- or polysubstituted by halogen and/or C.sub.1 -C.sub.4 -alkyl, or is the group --CH.sub.2 --Z--R.sub.h, whereinZ is oxygen or sulfur, andR.sub.h is hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkyl which is substituted by C.sub.1 -C.sub.4 -alkoxy, or is C.sub.3 -C.sub.4 -alkenyl, 2-propynyl, 3-halo-2-propynyl, phenyl, phenyl which is substituted by halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, NO.sub.2 and/or CF.sub.3, or is benzyl, or benzyl substituted by halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, NO.sub.2 and/or CF.sub.3,R.sub.c, R.sub.d and R.sub.f independently of one another are each hydrogen or C.sub.1 -C.sub.4 -alkyl, andR.sub.g is hydrogen or C.sub.1 -C.sub.4 -alkyl; including the acid addition salts thereof.There is also described the production of these substances, as well as agrochemical compositions containing these substances as active ingredients for controlling phytopathogenic microorganisms.
摘要:
The present invention provides novel nitromethylene derivatives of the formula (I) ##STR1## wherein R represents a hydrogen atom or an alkyl group, X represents a haloalkyl, haloalkoxy, haloalkylthio, haloalkylsulfinyl, haloalkylsulfonyl, nitro, cyano, thiocyanato, haloalkenyl, haloalkynyl, hydroxyl, alkoxycarbonyl, amino, acyl, dialkylamino, acylamino or alkoxy group, l represents 1, 2 or 3 provided that when l is 1, X does not represent an alkoxy group and when l is 2 or 3, not all substituents X represent an alkoxy group, m represents 2, 3 or 4, and n represents 0 or 1,and the use of the new compounds as insecticides.
摘要:
The invention relates to a process for the preparation of monocarbonyl or biscarbonyl compounds by reacting organic carbon compounds having one or more olefinic or aromatic double bonds in the molecule with the equivalent amount of ozone and by subsequently catalytically hydrogenating the ozonization products, wherein the peroxide-containing ozonization solution is fed continuously into a suspension of the hydrogenation catalyst in a lower aliphatic alcohol, while a peroxide content of not more than 0.1 mole/l is maintained, and the ozonization products are continuously cleaved reductively to give the corresponding carbonyl compounds.
摘要:
The present invention relates to new pyridines substituted in the 3-position, of the formula ##STR1## and to a process for their preparation. The compounds bring about specific inhibition of thromboxane synthetase and can thus be used as medicaments.
摘要:
TCNQ complexes with organic pyridinium ions, which may be kept in a molten condition for a relatively long time without the electrical conductivity thereof being substantially reduced after cooling.
摘要:
2-Benzyl-4-(4-pyridyl)thiazoles and derivatives thereof have been made from converting a benzyl cyanide to the corresponding thioamide followed by condensation with a 4-bromoacetylpyridine. The thiazole derivatives are found to be effective immunoregulants.
摘要:
New compositions of matter are disclosed which are the products resulting from reacting an alkyl substituted aromatic heterocyclic nitrogen-containing compound such as 2,4,6-trimethylpyridine or 2,3,5,6-tetramethylpyrazine with a dicarboxylic acid monoanhydride such as 2-dodecen-1-yl succinic anhydride. These compositions are useful in preventing corrosion of metallic articles in corrosive environments. They are particularly useful in down hole oil and gas well applications.