摘要:
Benzofuro[3,2-c]quinoline compounds of the general formula: ##STR1## wherein (1) each of R.sup.1 and R.sup.2 is the same, and represent a group of the formula of --OR.sup.3 in which R.sup.3 represents a carbamoyl group, an N-mono-alkylcarbamoyl group, an N,N-dialkylcarbamoyl group, an alkylsulfonyl group, a formyl group or an aliphatic acyl group which may have an alkoxycarbonyl group as a substituent; m represents zero, 1 or 2; n represents zero or 1; with the proviso that n is not zero when m is zero,(2) each of R.sup.1 and R.sup.2 is different, and represent a hydroxy group or an N,N-di-alkylcarbamoyloxy group; m represents 1 or 2; n represents 1, possess a strong inhibitory action on bone resorption and a stimulatory effect on ossification. Some benzofuro[3,2-c]quinoline compounds of the above general formula also possess a stimulatory effect on longitudinal bone growth, and thus are useful for the prevention or treatment of osteoporosis.
摘要:
The present invention provides an improved method for producing a nuclear substituted cinnamoylanthranilic acid compound.Illustrative of the process is the reaction of 3-hydroxy-4-methoxybenzaldehyde with 2-carboxymalonanilic acid in an inert solvent medium in the presence of a molar excess of piperidine to provide a high purity intermediate salt precipitate, and the salt is treated with an acidic reagent to yeild N-(3-hydroxy-4-methoxycinnamoyl)anthranilic acid product.
摘要:
The imidazole derivatives of the general formula: ##STR1## wherein A and B may be the same or different, and each is a straight- or branched-chain alkylene or alkenylene group having 1 to 8 carbon atoms, D is an acyl group having 2 to 10 carbon atoms, an alkoxycarbonyl group having 2 to 7 carbon atoms or a dialkoxymethyl group having 3 to 13 carbon atoms, Q is a cyano group or an alkoxycarbonyl group having 2 to 7 carbon atoms, X is a halogen atom, Z is ##STR2## (wherein E is a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms or an alkoxy group having 1 to 6 carbon atoms, Y is an oxygen atom or a sulfur atom and may be connected with either A or B), n is zero or 1, with the proviso that n is 1 when Y connects with B.These compounds are novel compounds and are useful as intermediates in producing 1-substituted imidazole derivatives which possess strong and specific inhibitory effects on thromboxane synthetase and thus are useful as therapeutically active agents for treatment of diseases caused by thromboxane A.sub.2.
摘要:
The present invention provides an improved method for producing a nuclear substituted cinnamoylanthranilic acid compound.Illustrative of the process is the reaction of 3,4-dimethoxybenzaldehyde with 2-carboxymalonanilic acid in an inert solvent medium in the presence of piperidine to provide an intermediate salt precipitate, and the salt is treated with an acidic reagent to yield N-(3,4-dimethoxycinnamoyl)anthranilic acid product.
摘要:
Piperidino-3,4-dihydrocarbostyril compounds represented by the formula: ##STR1## wherein R.sup.1 represents a hydroxy group or an acyloxy group having 2 to 11 carbon atoms; one of R.sup.2 and R.sup.3 represents a nitro group, a cyano group, an alkoxycarbonyl group having 2 to 7 carbon atoms, an alkyl group having 1 to 4 carbon atoms, a haloalkyl group having 1 to 3 carbons atoms, or a halogen atom, and the other represents a hydrogen atom; and pharmaceutically acceptable salts thereof, exhibit platelet aggregation inhibiting activity and thus being useful as therapeutic agents for the prevention or treatment of cerebral ischemic disorders and arterial ischemic disorders.
摘要翻译:由下式表示的哌啶子基-3,4-二氢喹诺酮化合物:其中R 1表示羟基或具有2至11个碳原子的酰氧基; R 2和R 3中的一个表示硝基,氰基,具有2至7个碳原子的烷氧基羰基,具有1至4个碳原子的烷基,具有1至3个碳原子的卤代烷基或卤素原子,以及 另一个表示氢原子; 其药学上可接受的盐具有血小板聚集抑制活性,因此可用作预防或治疗脑缺血障碍和动脉缺血障碍的治疗剂。
摘要:
1,3-Disubstituted imidazoles of the general formula (I): ##STR1## wherein A and B may be the same or different, and each is a straight- or branched-chain alkylene or alkenylene group having 1 to 8 carbon atoms, Y is an acyl group having 2 to 10 carbon atoms, an alkoxycarbonyl group having 2 to 7 carbon atoms or an dialkoxymethyl group having 3 to 13 carbon atoms, Z is a cyano group or an alkoxycarbonyl group having 2 to 7 carbon atoms, X is a halogen atom, n is zero or 1. The said compounds are intermediates for producing the imidazole derivatives of the general formula (V) above which possess strong and specific inhibitory effects on thromboxane synthetase and thus are useful as therapeutical agents for treatment of diseases caused by thromboxane A.sub.2.
摘要:
The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has β3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus. The present invention also provides a process for preparing said intermediates and a method of using said intermediates.
摘要:
The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has β3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus. The present invention also provides a process for preparing said intermediates and a method of using said intermediates.
摘要:
The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has β3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus. The present invention also provides a process for preparing said intermediates and a method of using said intermediates.
摘要:
A poly(phenylene ether) resin composed of structural units represented by the general formula: ##STR1## (wherein R.sup.1, R.sup.2 and R.sup.3 represent each alkyl, cycloalkyl, etc. or H (provided that two or more of R.sup.1, R.sup.2 and R.sup.3 do not represent H at the same time), or one of R.sup.1, R.sup.2 and R.sup.3 represents alkyl or H while the others together form a saturated ring, or R.sup.1, R.sup.2 and R.sup.3 together form an aromatic ring; A represents alkyl; p is an integer of from 3 to 5; and Y.sup.- represents a pharmaceutically acceptable acid residue) and/or structural units represented by the general formula: ##STR2## (wherein R.sup.4, R.sup.5 and R.sup.6 represents each alkyl, cycloalkyl, etc. or H (provided that two or more of R.sup.4, R.sup.5 and R.sup.6 do not represent H at the same time), or one of R.sup.4, R.sup.5 and R.sup.6 represents alkyl or H while the others together form a saturated ring, or R.sup.4, R.sup.5 and R.sup.6 together form an aromatic ring; and A, p and Y.sup.- have same meanings as defined above) and structural units represented by the general formula: ##STR3## (wherein R.sup.7 and R.sup.8 represents each alkyl, cycloalkyl, etc. or together form a saturated ring; q is an integer of from 3 to 20; and A, p, and Y.sup.- have same meanings as defined above) wherein the sum of the contents of the structural units represented by the general formula (I) and the structural units represented by the general formula (II) amounts to 40 to 96% by mole and the content of the structural units represented by the general formula (III) amounts to 4 to 60% by mole based upon the content of phenylene ether component and a process for producing the same. The poly(phenylene ether) resins have the effect of adsorbing bile acids and are useful as a cholesterol reducing agent.