摘要:
[1,1-dithien-(3)-yl-1-hydroxy-(3)-propyl]-[1-phenyl-1-hydroxy-(2)-propyl]-amine is prepared by condensing thien-(3)-yl lithium with a .beta.-halogen propionic acid alkyl ester of the formula ##STR1## where R is a lower alkyl group and Hal is chlorine, bromine or iodine, in an inert medium at a temperature below -50.degree. C. to form a compound of the formula ##STR2## which is then reacted with 2-amino-1-hydroxy-1-phenylpropane in an inert medium in the presence of a basic compound. The product cn be converted to [1,1-dithien-(3)-yl-(1)-propen-(3)-yl]-[1-phenyl-(2)-propyl]-amine by dehydration.
摘要:
Biodegradable insecticides having the formula: ##STR1## where X, Y and R are different, and X and Y are selected from the group consisting of hydrogen, halo, lower alkyl and lower alkoxy, and R is selected from the group consisting of nitrogen, oxygen, sulfur and sulfone.
摘要:
The present invention provides a method of preparing thieno[3,2-c]pyridine derivatives of formula I: ##STR1## wherein R.sub.1 is selected from the group consisting of lower alkyl; lower alkylene phenyl; substituted lower alkylene phenyl wherein the phenyl is substituted from 1 to 3 times with lower alkyl, lower alkoxy, lower acyloxy, hydroxy, nitro and halo; lower alkylene naphthyl, lower alkylene thienyl; lower alkylene diphenyl; lower alkylene-hydroxy-phenyl; substituted lower alkylene-hydroxy-phenyl wherein the phenyl is substituted from 1 to 3 times with lower alkyl, lower alkoxy, lower acyloxy, hydroxy, nitro, and halo; lower alkylene-hydroxy-naphthyl; lower alkylene-hydroxy-thienyl; lower alkylene-hydroxy-diphenyl, and R.sub.2 is H or lower alkylene. The method comprises reacting a compound of a formula II: ##STR2## with a cyclic dioxy or cyclic dithio in the presence of catalyst.
摘要:
The invention relates to new compounds corresponding to formula I: ##STR1## in which: W represents C=O, CH.sub.2 or CHOH,Z represents ##STR2## R.sub.1 and R.sub.2 represent especially Cl or F, R, R' and R" represent especially H,X represents especially CH.sub.2,Y represents especially COOH,u and v are two integers ranging from 0 to 10,p and q take the value 0 or 1,n and m are two integers ranging 0 to 10 andt is 0 or 1the total number of carbon atoms in the chain ##STR3## ranging from 2 to 20, and to their physiologically acceptable salts obtained with organic or inorganic acids.These compounds are useful for preparing medicinal products which have, especially, anti-inflammatory properties.
摘要:
Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein V is an oxygen or a sulphur atom; X and Y, which may be the same or different, are hydrogen or halogen atoms, or optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkynyl, haloalkyl, alkoxy, haloalkoxy, optionally substituted aryloxy, optionally substituted arylalkoxy, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, nitrile, --CO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, or --COR.sup.6 groups; or the groups X and Y, when they are in adjacent positions on the phenyl ring, may join to form a fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; and Z is optionally substituted methylene, optionally substituted amino, oxygen or sulphur and when Z is a substituted methylene group, the substituent may join the 2-position of the phenyl ring to form a non-aromatic fused ring; R.sup.1 and R.sup.2 are alkyl groups containing from one to four carbon atoms, optionally substituted with one or more halogen atoms; and R.sup.3, R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are hydrogen atoms or optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, optionally substituted aryl, optionally substituted aralkyl, or cycloalkylalkyl groups; and metal complexes thereof.
摘要翻译:式(I)化合物:其中V是氧或硫原子; X和Y可以相同或不同,是氢或卤素原子,或任选取代的烷基,任选取代的烯基,任选取代的芳基,任选取代的杂芳基,任选取代的炔基,卤代烷基,烷氧基,卤代烷氧基,任选取代的芳氧基, 取代的芳基烷氧基,任选取代的酰氧基,任选取代的氨基,酰氨基,硝基,腈,-CO 2 R 3,-CONR 4 R 5或-COR 6基团; 或基团X和Y当它们在苯环上的相邻位置时,可以连接形成任选含有一个或多个杂原子的芳族或脂族稠合的稠环; Z是任选取代的亚甲基,任选取代的氨基,氧或硫,当Z是取代的亚甲基时,取代基可以连接苯环的2-位,形成非芳香稠环; R1和R2是含有1-4个碳原子的烷基,任选地被一个或多个卤素原子取代; 可以相同或不同的R 3,R 4,R 5和R 6是氢原子或任选取代的烷基,环烷基,烯基,炔基,任选取代的芳基,任选取代的芳烷基或环烷基烷基; 及其金属络合物。
摘要:
The invention provides compounds of general formula ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichY and Z, which may be the same or different, each represent oxygen, sulphur, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 is hydrogen, nitro, cyano, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl;p has a value from 2 to 12;R.sub.1 represents ##STR2## in which R.sub.4 and R.sub.5 which may be the same or different, each represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group >N-R.sub.6 in which R.sub.6 represents hydrogen or lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a 5 to 7-membered saturated heterocyclic ring which may contain an additional oxygen atom or the group >NR.sub.6 ;Q represents a furan or thiophen ring in which incorporation into the rest of the molecule is through bonds at the 2 and 5 positions, or a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1 and 3 or 1 and 4 positions;X represents --CH.sub.2 --, --O-- or --S--;n represents zero or 1;m represents 2, 3 or 4 and Alk represents a straight chain alkylene group of 1 to 3 carbon atoms,andR.sub.2 represents lower alkyl or the group--(CH.sub.2).sub.y E(CH.sub.2).sub.x Gin whichy represents 2, 3 or 4 or can additionally represent zero or 1 when E is a --CH.sub.2 -- group, x represents zero, 1 or 2;E represents --CH.sub.2 --, --O-- or --S--; andG represents a monocyclic 5 or 6 membered carbocyclic or heterocyclic aromatic ring, or G represents the group ##STR3## where Q' represents any of the rings defined for Q; Alk' represents any of the groups defined for Alk; and R.sub.4 ' and R.sub.5 ' which may be the same or different represent any of the groups defined for R.sub.4 or R.sub.5.The compounds of formula (I) have pharmacological activity as selective histamine H.sub.2 -antagonists.
摘要:
The invention provides compounds of general formula ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichY and Z, which may be the same or different, each represent oxygen, sulphur, =CHNO.sub.2 or =NR.sub.3 where R.sub.3 is hydrogen, nitro, cyano, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl;p has a value from 2 to 12;R.sub.1 represents ##STR2## in which R.sub.4 and R.sub.5 which may be the same or different, each represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group >N-R.sub.6 in which R.sub.6 represents hydrogen or lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a 5 to 7-membered saturated heterocyclic ring which may contain an additional oxygen atom or the group >NR.sub.6 ;Q represents a furan or thiophen ring in which incorporation into the rest of the molecule is through bonds at the 2 and 5 positions, or a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1 and 3 or 1 and 4 positions;X represents --CH.sub.2 --, --O-- or --S--;n represents zero or 1;m represents 2, 3 or 4 andAlk represents a straight chain alkylenegroup of 1 to 3 carbon atoms;and R.sub.2 represents lower alkyl or the group--(CH.sub.2).sub.y E(CH.sub.2).sub.x Gin whichY represents 2, 3 or 4 or can additionallyrepresent zero or 1 when E is a --CH.sub.2 -- group;x represents zero, 1 or 2;E represents --CH.sub.2 --, --0-- or --S--; andG represents a monocyclic 5 or 6 membered carbocyclic or heterocyclic aromatic ring, or G represents the group ##STR3## where Q' represents any of the rings defined for Q;Alk' represents any of the groups defined for Alk;and R.sub.4 ' and R.sub.5 ' which may be the same or different represent any of the groups defined for R.sub.4 or R.sub.5.The compounds of formula (I) have pharmacological activity as selective histamine H.sub.2 -antagonists.
摘要:
A sulfoalkylthiophene compound of the following formula [1] and a hydroxyalkylthiophene compound of the following formula [2], from which a useful π-conjugated conductive polymer monomer capable of oxidation polymerization can be provided: (wherein R is a hydrogen atom, an alkali metal atom or an alkaline earth metal atom, and n is an integer of 1 to 3) (wherein n is as defined above).
摘要:
Retinoid-like activity is exhibited by compounds of the formula ##STR1## where R is hydrogen or lower alkyl; A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-5; and B is H, --COOH or an ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative thereof, or --CHO or an acetal derivative thereof, or --COR.sub.1 or a ketal derivative thereof where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4; or a pharmaceutically acceptable salt thereof.
摘要:
A compound of the general formula (I): ##STR1## or a pharmaceutically acceptable ester thereof; or a pharmaceutically acceptable salt thereof, wherein,R.sup.o represents a substituted or unsubstituted aryl group or a substituted or unsubstituted benzofuranyl group,X represents a bond or --O--CH.sub.2 --,R.sup.1 represents a hydrogen atom or a moiety ##STR2## wherein R.sup.o and X are as defined above; R.sup.2 and R.sup.3 independently represent a hydrogen atom or an alkyl group,n represents an integer 1 or 2,Y represents a bond or a moiety --CH.sub.2 --O--, moiety A represents an aryl group,R.sup.4 represents a linking group, andR.sup.5 represents a substituted or unsubstituted, monocyclic or fused ring heterocyclic group, having up to four heteroatoms in each ring selected from, oxygen, nitrogen and sulphur; provided that R.sup.5 is not N-piperazinyl, N-piperadinyl, N-homopiperadinyl, N-pyrrolidinyl or N-morpholinyl; pharmaceutical compositions containing such compounds and their use in medicine and agriculture.