摘要:
A compound of the formula: ##STR1## wherein Ar is a phenyl group substituted with halogen, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 alkylthio, C.sub.1 -C.sub.8 alkylsulfonyl, nitro, trihalomethyl, cyano, C.sub.1 -C.sub.8 alkylamino, di(C.sub.1 -C.sub.8)-alkylamino, amino, hydroxyl, phenyl and/or phenoxy, a naphthyl group or a thienyl group optionally substituted with halogen, which is useful as an antifungal agent.
摘要:
An N-substituted imidazole compound of the formula: ##STR1## wherein R and R' are independently a phenyl group optionally substituted with one or more halogen, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 alkylthio, phenyl, phenoxy, phenylthio, hydroxyl, trifluoromethyl, amino, carbamoyl, di(C.sub.1 -C.sub.8) alkylamino, C.sub.1 -C.sub.8 alkanoylamino, nitro, cyano, carboxy, C.sub.1 -C.sub.8 alkoxycarbonyl, C.sub.1 -C.sub.8 alkylsulfonyloxy or C.sub.1 -C.sub.8 alkanoylpiperazino groups; a C.sub.1 -C.sub.15 alkyl group or a phenyl (C.sub.1 -C.sub.2) alkyl group optionally bearing halogen on the benzene ring, and its acid-addition salts, which is useful as an antifungal agent.
摘要:
An imidazolylcarboxylic acid compound of the formula: ##STR1## wherein Ph is a phenyl group or a phenyl group substituted with one or two halogen atoms, R is a hydrogen atom or a C.sub.1 -C.sub.8 alkyl group and n is an integer of 1 to 8, which is useful as an antifungal agent.
摘要:
Novel phenylserine derivatives of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions, and a process for preparing the compounds are disclosed. The phenylserine derivatives and pharmaceutically acceptable acid addition salts are capable of inhibiting the biosynthesis of leucotrienes and/or antagonistic activity against SRS-A and hence are useful for prophylaxis and treatment of various allergic diseases (e.g. bronchial asthma, allergic nasitis, urticaria), ischemic heart diseases, ischemic encephalopathy, inflammation, or the like.
摘要:
Novel anti-atheroscelersosis agents having the formula, ##SPC1##Wherein typical examples of R.sup.1 and R.sup.2 are hydrogen, C.sub.1 -C.sub.8 alkyl, phenyl, benzyl and phenethyl, or R.sup.1 and R.sup.2 may form cycloalkylidene together with a carbon atom bonded therewith; R.sup.3 and R.sup.4 each is hydrogen or C.sub.1 -C.sub.4 alkyl; Y is hydroxyl, C.sub.1 -C.sub.4 alkoxy, phenoxy or an amine residue; A is hydrogen or a group of the formula, ##EQU1## wherein R.sup.3, R.sup.4 and Y have the same meanings as defined above; and D and E each is hydrogen or halogen.These compounds are produced, for example, by reacting a bisphenolic compound of the formula, ##SPC2## with chloroform and a ketone compound of the formula,R.sup.3 --CO--R.sup.4in the presence of an alkali. Alternatively, they are produced by reacting the bisphenolic compound with .alpha.-halogeno- or .alpha.-hydroxycarboxylic acid derivative of the formula, ##EQU2## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, d, e and T have the same meanings as definend above; and X is halogen or hydroxyl.
摘要:
Bisphenoxy carboxylic acid derivatives useful as an antiarteriosclerosis agent with good absorbability and low toxicity, which are novel compounds represented by the general formula, ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen atoms or lower alkyl groups and A preresents ##STR2## (wherein in case R.sub.3 is a hydrogen atom, R.sub.4 represents an amino-lower-alkyl group, an N-lower-alkylaminoalkyl group, a heterocyclic group, or a heterocyclic group-substituted alkyl group; or R.sub.3 and R.sub.4 may join through an intermediary hetero atom to form a heterocyclic group and if said hetero atom is a nitrogen atom, this nitrogen atom can bear a lower alkyl group as a substituent) or ##STR3## (wherein R.sub.5 represents a hydrogen atom, a hydroxyalkyl group or a derivative thereof, and R.sub.6 represents a hydroxyalkyl group or a heterocyclic group; or R.sub.5 and R.sub.6 may join to form a cyclic group, or may join through another intermediary hetero atom to form a heterocyclic group and if said hetero atom is a nitrogen atom, this nitrogen atom can bear a lower alkyl group as a substituent).
摘要:
Novel compounds having the formula, ##SPC1##Wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen or a C.sub.1 -C.sub.4 alkyl; n is an integer of 4-6; and Y is hydrogen or a group of the formula ##EQU1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above. These compounds are produced, for example, by reacting a bisphenolic compound of the formula, ##SPC2##With chloroform and a ketone compound of the formula,R.sub.1 -- CO -- R.sub.2in the presence of an alkali. Alternatively, they are produced by reacting the bisphenolic compound with .alpha.-halogeno- or .alpha.-hydroxycarboxylic acid derivative of the formula, ##EQU2## wherein R.sub.1, R.sub.2, and R.sub.3 are as defined above, and X is a halogen or hydroxyl. The novel compounds are anti-atherosclerosis agents useful for lowering elevated levels of cholesterol or lipids.
摘要:
Thiazolidin-4-one derivative represented by the following general formula (I) and acid addition salts thereof ##STR1## wherein; R.sup.1 and R.sup.2 are the same or different and denote each(i) a residue represented by the general formula--A--R.sup.4 wherein, A denotes a single bond, C.sub.1 -C.sub.8 alkylene, C.sub.2 -C.sub.8 alkenylene, or C.sub.2 -C.sub.8 alkynylene and R.sup.4 denotes hydrogen, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, or C.sub.1 -C.sub.6 haloalkyl,or(ii) a residue represented by the general formula ##STR2## wherein, B denotes a single bond or C.sub.1 -C.sub.6 alkylene, R.sup.5 denotes hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, substituted silyl, or substituted or unsubstituted aryl, n and n' denote each an integer of 2 to 4, m denotes an integer of 1 to 3, and m' denotes an integer of 0 to 2;R.sup.3 denotes hydrogen, C.sub.1 -C.sub.2 alkyl, allyl, 2-propynyl,or(c) the general formula--F--R.sup.9 wherein, F denotes C.sub.2 -C.sub.6 alkylene and R.sup.9 denotes a nitrogen-containing heterocyclic aromatic residue or an amino group represented by the general formula ##STR3## (R.sup.10 denotes hydrogen, C.sub.2 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkanoyl and R.sup.11 denotes hydrogen or C.sub.1 -C.sub.4 alkyl or R.sup.10 in combination with R.sup.11 denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms.Having selective PAF-antagonistic activities, these compounds are very useful as preventive and curative agents for PAF-induced diseases, for example, various kinds of inflammation, allergic diseases, circulatory diseases, and gastro-intestinal diseases.
摘要:
Thiazolidin-4-one derivative represented by the folowing general formula (I) and acid addition salts thereof ##STR1## wherein; R.sup.1 and R.sup.2 are the same or different and denote each(i) a residue represented by the general formula--A--R.sup.4 wherein, A denotes a single bond, C.sub.1 -C.sub.8 alkylene, C.sub.2 -C.sub.8 alkenylene, or C.sub.2 -C.sub.8 alkynylene and R.sup.4 denotes hydrogen, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, or C.sub.1 -C.sub.6 haloalkyl, or(ii) a residue represented by the general formula{(CH.sub.2).sub.n O}.sub.m {(CH.sub.2).sub.n' O}B--R.sup.5 wherein, B denotes a single bond or C.sub.1 -C.sub.6 alkylene, R.sup.5 denotes hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, substituted silyl, or substituted or unsubstituted aryl, n and n' denote each an integer of 2 to 4, m denotes an integer of 1 to 3, and m' denotes an integer of 0 to 2; andR.sup.3 denotes hydrogen, C.sub.1 -C.sub.2 alkyl, allyl, 2-propynyl, or a residue represented by(a) the general formula--CH.sub.2).sub.l R.sup.6 wherein, R.sup.6 denotes halogen, an aryl group substituted or unsubstituted by one or more hydroxy or C.sub.1 -C.sub.4 alkoxy groups, or a residue represented by the general formula --D--R.sup.7 (D denotes oxygen or sulfur and R.sup.7 denotes hydrogen, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 alkanol) and l denotes an integer of 2 to 4,(b) the general formula--CH.sub.2).sub.k CO--E--R.sup.8 wherein, E denotes oxygen, sulfur, imino, or C.sub.1 -C.sub.4 alkylimino, R.sup.8 denotes hydrogen or C.sub.1 -C.sub.4 alkyl, or --(E--R.sup.8) denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms, and k denotes an integer of 1 to 3, or(c) the general formula--F--R.sup.9 wherein, F denotes C.sub.2 -C.sub.6 alkylene and R.sup.9 denotes a nitrogen-containing heterocyclic aromatic residue or an amino group represented by the general formula ##STR2## (R.sup.10 denotes hydrogen, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 alkyl or R.sup.10 in combination with R.sup.11 denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms), with the proviso that, when R.sup.1 is hydrogen and R.sup.2 is methyl, R.sup.3 denotes hydrogen, C.sub.1 -C.sub.2 alkyl, 2-propynyl, or a residue represented by(a) the general formula--CH.sub.2).sub.l R.sup.6 wherein, R.sup.6 denotes halogen, an aryl group substituted or unsubstituted by one or more hydroxy or C.sub.1 -C.sub.4 alkoxy groups, or a residue represented by the general formula --D--R.sup.7 (D denotes oxygen or sulfur and R.sup.7 denotes hydrogen, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 alkanoyl) and l denotes an integer of 2 to 4,(b) the general formula--CH.sub.2).sub.k CO--E--R.sup.8 wherein, E denotes oxygen, sulfur, imino, or C.sub.1 -C.sub.4 alkylimino, R.sup.8 denotes hydrogen or C.sub.1 -C.sub.4 alkyl, or --(E--R.sup.8) denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms, and k denotes an integer of 1 to 3, or(c) the general formula--F--R.sup.9 wherein, F denotes C.sub.2 -C.sub.6 alkylene and R.sup.9 denotes a nitrogen-containing heterocyclic aromatic residue or an amino group represented by the general formula ##STR3## (R.sup.10 denotes hydrogen, C.sub.2 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkanoyl and R.sup.11 denotes hydrogen or C.sub.1 -C.sub.4 alkyl or R.sup.10 in combination with R.sup.11 denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms.Having selective PAF-antagonistic activities, these compounds are very useful as preventive and curative agents for PAF-induced diseases, for example, various kinds of inflammation, allergic diseases, circulatory diseases, and gastro-intestinal diseases.
摘要:
Novel imidazo[2,1-b]quinazolines and pyrimido-[2,1-b]quinozolines represented by the formula, ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and A are as defined in the specification were prepared. They have prominent pharmacological properties such as diuretic and vasodilating activity.