摘要:
The present invention is directed to (S)-(−)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride dihydrate, to a method producing the dihydrate, and to a drug composition containing the dihydrate. The compound of the present invention has less hygroscopicity as compared with (S)-(−)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride anhydrous crystals and thus, exhibits excellent chemical stability.
摘要:
The present invention is directed to (S)-(−)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride dihydrate, to a method producing the dihydrate, and to a drug composition containing the dihydrate. The compound of the present invention has less hygroscopicity as compared with (S)-(−)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride anhydrous crystals and thus, exhibits excellent chemical stability.
摘要:
The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: ##STR1## [wherein R.sup.1 represents a lower alkyl group; each of R.sup.2 and R.sup.3 represents H, alkyl, or alkoxy; each of R.sup.4 and R.sup.5 represents H or alkyl; R.sup.6 represents alkyl, --OR.sup.7, or --NR.sup.8 R.sup.9 ; and n is a number between 0 and 3 inclusive (wherein each of R.sup.7, R.sup.8, and R.sup.9 represents H, alkyl, aryl, aralkyl, amino, a heterocyclic ring, etc.)], as well as to a medicine containing the derivative or salt as the active ingredient. The present compounds exhibit strong binding inhibitory activity against endothelin having potent vasoconstrictive effect and cell proliferation effect. Therefore, the compounds are effective as remedies for various diseases including circulatory diseases.
摘要翻译:PCT No.PCT / JP95 / 02605 Sec。 371日期:1997年6月27日 102(e)日期1997年6月27日PCT 1995年12月19日PCT公布。 公开号WO96 / 20177 PCT 日期:1996年7月4日本发明涉及下述式(1)所示的嘧啶衍生物或其衍生物的盐:其中R1表示低级烷基; R 2和R 3各自表示H,烷基或烷氧基; R 4和R 5各自表示H或烷基; R 6表示烷基,-OR 7或-NR 8 R 9; 并且n是0和3之间的数字(其中R7,R8和R9各自表示H,烷基,芳基,芳烷基,氨基,杂环等)],以及含有该衍生物或 盐作为活性成分。 本发明化合物对内皮素具有强烈的结合抑制活性,具有强烈的血管收缩作用和细胞增殖作用。 因此,该化合物作为包括循环系统疾病在内的各种疾病的治疗方法是有效的。
摘要:
The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: ##STR1## �wherein R.sup.1 represents a hydroxyl group, a lower alkoxy group, a phenyloxy group which may have a substituent, an aralkyloxy group which may have a substituent, or --NR.sup.2 R.sup.3 ; X represents an oxygen atom or N--R.sup.4 ; m is 2 or 3; and n is 1 or 2 (wherein each of R.sup.2 and R.sup.3, which are identical to or different from each other, represents a hydrogen atom, a hydroxyl group, a lower alkyl group which may have a substituent, a phenyl group which may have a substituent, an aralkyl group which may have a substituent, or a heterocyclic group which may have a substituent; R.sup.4 represents a lower alkyl group, a phenyl group, a formyl group, or a lower alkoxycarbonyl group)!, as well as to a medicine containing the derivative or salt as the active ingredient. The compounds exhibit strong binding inhibitory activity against endothelin having potent vasoconstrictive effect. Therefore, the compounds are effective as remedies for various diseases including circulatory diseases.
摘要:
The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: [wherein R1 represents a lower alkyl group; each of R2 and R3 represents H, alkyl, or alkoxy; each of R4 and R5 represents H or alkyl; R6 represents alkyl, —OR7, or —NR8R9; and n is a number between 0 and 3 inclusive (wherein each of R7, R8, and R9 represents H, alkyl, aryl, aralkyl, amino, a heterocyclic ring, etc.)], as well as to a medicine containing the derivative or salt as the active ingredient. The present compounds exhibit strong binding inhibitory activity against endothelin having potent vasoconstrictive effect and cell proliferation effect. Therefore, the compounds are effective as remedies for various diseases including circulatory diseases.
摘要翻译:本发明涉及下式(1)的嘧啶衍生物或其衍生物的盐:其中R 1表示低级烷基; R 2和R 3各自表示H,烷基或烷氧基; R 4和R 5各自表示H或烷基; R 6表示烷基,-OR 7或-NR 8 R 9; 并且n是0和3之间的数字(其中R7,R8和R9各自表示H,烷基,芳基,芳烷基,氨基,杂环等)],以及含有该衍生物或 盐作为活性成分。 本发明化合物对内皮素具有强烈的结合抑制活性,具有强烈的血管收缩作用和细胞增殖作用。 因此,该化合物作为包括循环系统疾病在内的各种疾病的治疗方法是有效的。
摘要:
Because fluazinam is excellent as an active ingredient of pesticides and highly useful, it is desired to produce it efficiently in a proper form with simple operations at low cost in an environmentally friendly manner. The desired product is obtained in good yields with simple operations by using industrially advantageous reaction systems by a process comprising (1) a step of reacting ACTF and DCDNBTF in the presence of an alkali component, a solvent selected from the group consisting of ketones, nitriles, ethers and esters and a sufficient amount of water to substantially dissolve the alkali component, (2) a step of neutralizing or acidifying the reaction mixture with an acid and (3) a step of removing the solvent by distillation from the mixture containing fluazinam as the reaction product and the reaction solvent to precipitate crystals the product.
摘要:
Because fluazinam is excellent as an active ingredient of pesticides and highly useful, it is desired to produce it efficiently in a proper form with simple operations at low cost in an environmentally friendly manner. The desired product is obtained in good yields with simple operations by using industrially advantageous reaction systems by a process comprising (1) a step of reacting ACTF and DCDNBTF in the presence of an alkali component, a solvent selected from the group consisting of ketones, nitriles, ethers and esters and a sufficient amount of water to substantially dissolve the alkali component, (2) a step of neutralizing or acidifying the reaction mixture with an acid and (3) a step of removing the solvent by distillation from the mixture containing fluazinam as the reaction product and the reaction solvent to precipitate crystals the product.
摘要:
A process for producing 2-phenylacetophenone derivatives represented by the formula (I): (wherein X is an alkyl group or a haloalkyl group, and Y is a hydrogen atom, a halogen atom or an alkyl group which may be substituted), which comprises reacting a compound represented by the formula (II): (wherein X and Y are as defined above, and R is a hydrogen atom or an alkyl group) with an acid.
摘要:
There is provided a surface treating agent for ligneous floorings that makes the surface of a treated floor resistant to slipping and thus is capable of preventing tumbling. The surface treating agent for ligneous floorings contains a drying oil, Japan wax, candelilla wax, and powdery carnauba wax.
摘要:
An imidazole compound is disclosed, which is represented by formula (I): ##STR1## wherein: X represents a --COOT group, in which T represents a hydrogen atom, an alkyl group, a benzyl group, or a phenyl group; or a --CONH.sub.2 group,Y represents a hydrogen atom, a chlorine atom, or a bromine atom,Z represents an alkyl group containing from 2 to 6 carbon atoms, which may be substituted with one or more halogen atoms; or a phenyl group which may be substituted with one or more halogen atoms or alkyl groups, andQ represents a hydrogen atom; an --SO.sub.2 R.sup.1 group, in which R.sup.1 represents an alkyl group, a dialkylamino group, or a phenyl group which may be substituted with one or more alkyl groups; or a --CH(R.sup.2)(R.sup.3) group, in which R.sup.2 represents a hydrogen atom, a methyl group, or an alkoxy group, and R.sup.3 represents an alkoxy group, an --OCH.sub.2 CH.sub.2 Si (CH.sub.3) group, or a phenyl group which may be substituted with one or more alkyl groups or alkoxy groups,provided that when Y and Q each represents a hydrogen atom and Z represents a phenyl group, X represents a group other than a --COOH-phenyl group, and a --CONH.sub.2 group; and that when Y and Q each represents a hydrogen atom and Z represents an n--C.sub.5 H.sub.11 group, X represents a group other than a --COOH group and a --COOC.sub.2 H.sub.5 group.Processes for preparing imidazole compounds are also disclosed.The imidazole compounds are useful as an intermediate for production of biocides for controlling harmful organisms in the agricultural and horticultural areas, or medical and pharmaceutical fungicides.