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公开(公告)号：US4602022A
公开(公告)日：1986-07-22
申请号：US673722
申请日：1984-11-21
IPC分类号： A61K31/415 , A61K31/4164 , A61K31/4178 , A61K31/44 , A61K31/443 , A61P1/04 , A61P3/00 , A61P3/06 , A61P7/02 , A61P9/00 , A61P9/10 , A61P9/12 , A61P25/04 , A61P25/06 , A61P29/00 , C07D233/54 , C07D233/56 , C07D233/58 , C07D233/60 , C07D405/04 , C07D405/14 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , Y10S514/822 , Y10S514/825 , Y10S514/866 , Y10S514/927 , Y10S514/929
摘要： Compounds of the formula (I) ##STR1## wherein the symbol represents a single or a double bond;each of R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different is(a) hydrogen; hydroxy; halogen; cyano; C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 alkoxy; a C.sub.2 -C.sub.4 acyl or C.sub.2 -C.sub.4 acylamino group; --SR', --N(R') (R"), --CH.sub.2 OR', --COR or --CH.sub.2 COR, wherein R is OR' or --N(R') (R") and each of R' and R", being the same or different, is hydrogen or C.sub.1 -C.sub.6 alkyl; or(b) one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is 5-tetrazolyl or a group selected from --COCH.sub.2 OR', --CH.dbd.C(R')--COR and --X--C(R')(R")--COR, wherein R, R' and R" are as defined above, and X is --O--, --S--, or --NH--, and the others are as defined above under (a);R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, or a phenyl or 3-pyridyl ring, wherein the phenyl or pyridyl ring is unsubstituted or substituted by one to three substituents chosen from hydroxy and C.sub.1 -C.sub.4 alkoxy; or pharmaceutically acceptable salt thereof exhibit pharmaceutical activity as vasodilators or blood platelet aggregation inhibitors. Additionally, these compounds and their pharmaceutically acceptable salts are useful in the treatment of migraine, diabetic microangiopathy, rheumatoid arthritis, hypertension, peptic ulcers, osteoporosis, angina pectoris, atherosclerosis and dislipidaemies.
摘要翻译： 式（I）的化合物其中符号表示单键或双键; R 1，R 2，R 3和R 4各自可以相同或不同，是（a）氢; 羟基; 卤素; 氰基; C1-C6烷基; C1-C6烷氧基; C 2 -C 4酰基或C 2 -C 4酰氨基; -SR'，-N（R'）（R“），-CH 2 OR'，-COR或-CH 2 COR，其中R是OR'或-N（R'）（R”），R'和R “相同或不同”是氢或C 1 -C 6烷基; 或（b）R 1，R 2，R 3和R 4中的一个是5-四唑基或选自-COCH 2 OR'，-CH = C（R'） - COR和-XC（R'）（R“'） 其中R，R'和R“如上所定义，X是-O - ， - S - 或-NH-，其它如上文（a）中所定义。 R 5是氢，C 1 -C 6烷基，C 3 -C 6环烷基或苯基或3-吡啶基环，其中苯基或吡啶基环是未取代的或被1至3个选自羟基和C 1 -C 4烷氧基的取代基取代; 或其药学上可接受的盐显示作为血管扩张剂或血小板聚集抑制剂的药物活性。 此外，这些化合物及其药学上可接受的盐可用于治疗偏头痛，糖尿病性微血管病变，类风湿性关节炎，高血压，消化性溃疡，骨质疏松症，心绞痛，动脉粥样硬化和血脂紊乱。
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公开(公告)号：US4510149A
公开(公告)日：1985-04-09
申请号：US510358
申请日：1983-07-01
IPC分类号： A61K31/415 , A61K31/4164 , A61K31/4178 , A61K31/44 , A61K31/443 , A61P1/04 , A61P3/00 , A61P3/06 , A61P7/02 , A61P9/00 , A61P9/10 , A61P9/12 , A61P25/04 , A61P25/06 , A61P29/00 , C07D233/54 , C07D233/56 , C07D233/58 , C07D233/60 , C07D405/04 , C07D405/14 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , Y10S514/822 , Y10S514/825 , Y10S514/866 , Y10S514/927 , Y10S514/929
摘要： Compounds of the formula (I) ##STR1## wherein the symbol represents a single or a double bond; Z completes a single bond or is a --CH.sub.2 -- group; each of R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different is(a) hydrogen; hydroxy; halogen; cyano; C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 alkoxy; a C.sub.2 -C.sub.4 acyl or C.sub.2 -C.sub.4 acylamino group; --SR', --N(R') (R"), --CH.sub.2 OR', --COR or --CH.sub.2 COR, wherein R is OR' or --N(R') (R") and each of R' and R", being the same or different, is hydrogen or C.sub.1 -C.sub.6 alkyl; or(b) one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is 5- tetrazolyl or a group selected from --COCH.sub.2 OR', --CH.dbd.C(R')-COR and --X-C(R') (R")-COR, wherein R, R' and R" are as defined above, and X is --O--, --S--, or --NH--, and the others are as defined above under (a);one of R.sub.5 and R.sub.6 is hydrogen and the other is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, or a phenyl or pyridyl ring, wherein the phenyl or pyridyl ring is unsubstituted or substituted by one to three substituents chosen from hydroxy and C.sub.1 -C.sub.4 alkoxy; or pharmaceutically acceptable salts thereof exhibit pharmaceutical activity as vasodilators or blood platelet aggregation inhibitors. Additionally, these compounds and their pharmaceutically acceptable salts are useful in the treatment of migraine, diabetic microangeopathy, rheumatoid arthritis, hypertension, peptic ulcers, osteoporosis, angina pectoris, atherosclerosis and dislipidaemies.
摘要翻译： 式（I）的化合物其中符号表示单键或双键; Z完成单键或是-CH 2 - 基团; R 1，R 2，R 3和R 4各自可以相同或不同，是（a）氢; 羟基; 卤素; 氰基; C1-C6烷基; C1-C6烷氧基; C 2 -C 4酰基或C 2 -C 4酰氨基; -SR'，-N（R'）（R“），-CH 2 OR'，-COR或-CH 2 COR，其中R是OR'或-N（R'）（R”），R'和R “相同或不同”是氢或C 1 -C 6烷基; 或（b）R 1，R 2，R 3和R 4中的一个是5-四唑基或选自-COCH 2 OR'，-CH = C（R'） - COR和-XC（R'）（R“） - COR 其中R，R'和R“如上所定义，X是-O - ， - S - 或-NH-，其它如上文（a）中所定义。 R 5和R 6之一是氢，另一个是氢，C 1 -C 6烷基，C 3 -C 6环烷基或苯基或吡啶基，其中苯基或吡啶基环是未取代的或被1至3个选自羟基和C 1 -C4烷氧基 或其药学上可接受的盐显示作为血管扩张剂或血小板聚集抑制剂的药物活性。 此外，这些化合物及其药学上可接受的盐可用于治疗偏头痛，糖尿病性微病变，类风湿性关节炎，高血压，消化性溃疡，骨质疏松症，心绞痛，动脉粥样硬化和血脂紊乱。
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