摘要:
The present invention relates to an amino acid derivative having an angiotensin I-converting enzyme inhibition activity, a vasopressin antagonism and an atrial natriuretic peptide hydrolase inhibition activity. This amino acid derivative is represented by the following general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or an acyl group; R.sup.2 represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, an ary group which may have a substituent, a heteroaryl group which may have a substituent, an arylalkyl group which may have a substituent or a heteroarylalkyl group which may have a substituent; m and n represent each independently an integer of 0, 1 or 2 and J represents a cyclic group having an angiotensin I-converting enzyme inhibition activity.
摘要翻译:本发明涉及具有血管紧张素I-转化酶抑制活性,加压素拮抗作用和心房利尿钠肽水解酶抑制活性的氨基酸衍生物。 该氨基酸衍生物由以下通式(I)表示:其中R 1表示氢原子或酰基; R 2表示氢原子,低级烷基,环烷基,可以具有取代基的芳基,可以具有取代基的杂芳基,可以具有取代基的芳烷基或可以具有取代基的杂芳基烷基 ; m和n各自独立地表示0,1或2的整数,J表示具有血管紧张素I-转化酶抑制活性的环状基团。
摘要:
A pyrrolidine compound having the following formula and a pharmacologically acceptable salt thereof is disclosed. It is useful in the pharmaceutical field. ##STR1## in which X is hydrogen, a halogen, or a lower alkyl, Y is --(CH2)n--, n being zero, 1 or 2, --S(O)p--, p being zero, 1 or 2, --O--, or --NH-- and R is phenyl, a substituent-having phenyl, naphtyl, a substituent-having naphthyl, a heteroaryl or a substituent-having heteroaryl.
摘要:
The biphenylmethane derivative having the formula (I) is useful to prevent and treat hypertension and cardiac failure. ##STR1## in which R1 is hydrogen, an alkyl, a cycloalkyl, a halogenated alkyl, --S--R7, --SO2--R7, --C.tbd.C--R7 or --(CH2)--OR7, R7 being hydrogen, an alkyl, a cycloalkyl or a halogenated alkyl, p being zero or 1, --A1.dbd.A2--A3.dbd.A4-- is CH.dbd.CH--CH.dbd.CH--, --N.dbd.CH--CH.dbd.CH--, --CH.dbd.N--CH.dbd.CH--, --CH.dbd.CH--N.dbd.CH--, --CH.dbd.CH--CH.dbd.N-- or --CH.dbd.N--CH.dbd.N--, R2 and R3 are each hydrogen, a halogen, a lower alkyl, a lower alkoxy, a carbamoyl or cyano, R4 is hydrogen or a lower alkyl, R5 is 1H-tetrazol-5-yl, carboxyl (--COOH) or a carboxylic ester and R6 is hydrogen, a halogen, hydroxyl or a lower alkoxy, or a pharmacologically acceptable salt thereof.
摘要:
The biphenylmethane derivative having the formula (I) is useful to prevent and treat hypertension and cardiac failure. ##STR1## in which R1 is hydrogen, an alkyl, a cycloalkyl, a halogenated alkyl, --S--R7, --SO2--R7, --C.tbd.C--R7 or --(CH2)p--OR7, R7 being hydrogen, an alkyl, a cycloalkyl or a halogenated alkyl, p being zero or 1, --A1=A2--A3=A4-- is --CH=CH--CH=CH--, --N=CH--CH=CH--, --CH=N--CH=CH--, --CH=CH--N=CH--, --CH=CH--CH=N-- or --CH=N--CH=N--, R2 and R3 are each hydrogen, a halogen, a lower alkyl, a lower alkoxy, a carbamoyl or cyano, R4 is hydrogen or a lower alkyl, R5 is 1H-tetrazol-5-yl, carboxyl (--COOH) or a carboxylic ester and R6 is hydrogen, a halogen, hydroxyl or a lower alkoxy, or a pharmacologically acceptable salt thereof.
摘要:
The biphenylmethane derivative having the formula (I) is useful to prevent and treat hypertension and cardiac failure. ##STR1## in which R1 is hydrogen, an alkyl, a cycloalkyl, a halogenated alkyl, --S--R7, --SO2--R7, --C.tbd.C--R7 or --(CH2)p--OR7, R7 being hydrogen, an alkyl, a cycloalkyl or a halogenated alkyl, p being zero or 1, --A1.dbd.A2--A3.dbd.A4-- is --CH.dbd.CH--CH.dbd.CH--, --N.dbd.CH--CH.dbd.CH--, --CH.dbd.N--CH.dbd.CH--, --CH.dbd.CH--N.dbd.CH--, --CH.dbd.CH--CH.dbd.N-- or --CH.dbd.N--CH.dbd.N--, R2 and R3 are each hydrogen, a halogen, a lower alkyl, a lower alkoxy, a carbamoyl or cyano, R4 is hydrogen or a lower alkyl, R5 is 1H-tetrazol-5-yl, carboxyl (--COOH) or a carboxylic ester and R6 is hydrogen, a halogen, hydroxyl or a lower alkoxy, or a pharmacologically acceptable salt thereof.
摘要:
The present invention provides a thioformamide derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is highly safe, easy to use, and useful as an excellent hypotensive or heart disease remedy: ##STR1## wherein Y represents ##STR2## or the like [wherein R.sup.7 represents benzyloxy or the like; R.sup.11 and R.sup.12 each represent hydrogen, hydroxyl, benzoyloxy, benzyloxy, ##STR3## (wherein R.sup.14 and R.sup.15 each represent hydrogen, benzyl or the like) or the like];Z represents --CH.sub.2 -- or the like; A represents imidazolyl or imidazopyridyl which may have one or two substituents, or the like; R.sup.1 and R.sup.2 each represent hydrogen, lower alkyl or the like; and R.sup.3 and R.sup.4 each represent hydrogen, lower alkyl or the like.
摘要翻译:PCT No.PCT / JP92 / 01297 Sec。 371日期1994年04月26日 102(e)日期1994年4月26日PCT提交1992年10月6日PCT公布。 出版物WO93 / 08168 日本1994年4月29日。本发明提供由以下通式(I)表示的硫代甲酰胺衍生物或其药理学上可接受的盐,其是高度安全,易于使用的,并且可用作优异的降压药或心脏病药物: (I)其中Y表示酰氧基等; R 11和R 12各自表示氢,羟基,苯甲酰氧基,苄氧基,苯甲酰基等)等。 Z表示-CH 2 - 等; A表示可具有一个或两个取代基的咪唑基或咪唑并吡啶等; R 1和R 2各自表示氢,低级烷基等; R 3和R 4各自表示氢,低级烷基等。
摘要:
The present invention provides a thioformamide derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is highly safe, easy to use, and useful as an excellent hypotensive or heart disease remedy: ##STR1## wherein Y represents ##STR2## or the like [wherein R.sup.7 represents benzyloxy or the like; R.sup.11 and R.sup.12 each represent hydrogen, hydroxyl, benzoyloxy, benzyloxy, ##STR3## (wherein R.sup.14 and R.sup.15 each represent hydrogen, benzyl or the like) or the like];Z represents --CH.sub.2 -- or the like; A represents imidazolyl or imidazopyridyl which may have one or two substituents, or the like; R.sup.1 and R.sup.2 each represent hydrogen, lower alkyl or the like; and R.sup.3 and R.sup.4 each represent hydrogen, lower alkyl or the like.
摘要翻译:本发明提供由下列通式(I)表示的硫代甲酰胺衍生物或其药学上可接受的盐,其安全性高,易于使用,可用作优异的降血压或心脏病治疗药物:其中 Y表示等[其中R7表示苄氧基等; R 11和R 12各自表示氢,羟基,苯甲酰氧基,苄氧基,(其中R 14和R 15各自表示氢,苄基等)等。 Z表示-CH 2 - 等; A表示可具有一个或两个取代基的咪唑基或咪唑并吡啶等; R 1和R 2各自表示氢,低级烷基等; R 3和R 4各自表示氢,低级烷基等。
摘要:
The present invention provides a thioformamide derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is highly safe, easy to use, and useful as an excellent hypotensive or heart disease remedy: ##STR1## wherein Y represents ##STR2## or the like [wherein R.sup.7 represents benzyloxy or the like; R.sup.11 and R.sup.12 each represent hydrogen, hydroxyl, benzoyloxy, benzyloxy, ##STR3## (wherein R.sup.14 and R.sup.15 each represent hydrogen, benzyl or the like) or the like];Z represents --CH.sub.2 -- or the like; A represents imidazolyl or imidazopyridyl which may have one or two substituents, or the like; R.sup.1 and R.sup.2 each represent hydrogen, lower alkyl or the like; and R.sup.3 and R.sup.4 each represent hydrogen, lower alkyl or the like.
摘要翻译:本发明提供由下列通式(I)表示的硫代甲酰胺衍生物或其药理学上可接受的盐,其是高度安全,易于使用的,并且可用作优异的降血压或心脏病治疗药物:其中 Y表示等[其中R7表示苄氧基等; R 11和R 12各自表示氢,羟基,苯甲酰氧基,苄氧基,(其中R 14和R 15各自表示氢,苄基等)等。 Z表示-CH 2 - 等; A表示可具有一个或两个取代基的咪唑基或咪唑并吡啶等; R 1和R 2各自表示氢,低级烷基等; R 3和R 4各自表示氢,低级烷基等。
摘要:
There are provided a method for producing a magnesium alloy sheet having good press formability and a magnesium alloy coil stock obtained by coiling the magnesium alloy sheet. After a raw material sheet 1 composed of a magnesium alloy is preheated to 280° C. or less, the heated raw material sheet 1 is rolled with a reduction roll 3 and the obtained long rolled sheet is coiled. The surface temperature of the reduction roll 3 is set to be 230° C. or more and 290° C. or less. The preheating, rolling, and coiling are repeatedly performed in a continuous manner. By setting both the temperatures of the raw material sheet 1 and reduction roll 3 to be certain temperatures, the rolling property of the raw material sheet can be improved and the raw material sheet can be properly rolled in a continuous manner. In addition, a variation in temperature in the width direction of the reduction roll can be suppressed and uniform rolling can be performed, resulting in the production of a long magnesium alloy sheet. In this magnesium alloy sheet, working strain is sufficiently introduced by rolling and an increase in the size of crystal grains is suppressed. Thus, the magnesium alloy sheet has good press formability. Furthermore, a coil stock in which telescoping is not easily caused and that has good appearance is obtained.
摘要:
Provided are a rolled Mg alloy material which has a wide width and whose mechanical properties are uniform in a width direction, a Mg alloy structural member produced by plastically working the rolled Mg alloy material, and a method for producing the rolled Mg alloy material. The method for producing a rolled Mg alloy material includes rolling a Mg alloy material with a reduction roll. The Mg alloy material has a width of 1,000 mm or more, and the reduction roll has three or more regions in the width direction. The temperature is controlled in each of the regions so that a difference between a maximum temperature and a minimum temperature is 10° C. or less in the width direction of a surface of the reduction roll. The variation in the rolled state in the width direction can be reduced by reducing a difference in temperature over the width direction of the reduction roll. As a result, it is possible to produce a rolled Mg alloy material whose mechanical properties are substantially uniform in the width direction.