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    • 125. 发明授权
    • Alpha-methylene-6-styryl-acrylic acid derivatives
    • α-亚甲基-6-苯乙烯基 - 丙烯酸衍生物
    • US5310746A
    • 1994-05-10
    • US981071
    • 1992-11-24
    • Jean-Louis BrayerJean-Pierre DemouteYannick Le StancNicole Reinier
    • Jean-Louis BrayerJean-Pierre DemouteYannick Le StancNicole Reinier
    • C07B61/00A01N37/36A01N43/78A01N43/82A01N43/836C07C67/343C07C69/734C07C69/738C07C317/44C07C323/56C07D271/06C07D277/22C07D277/30C07D417/04C07F9/40C07F9/653C07F9/6539C07F9/6558C07C69/618A01N37/10
    • C07D271/06A01N37/36A01N43/78A01N43/82C07C69/734C07C69/738C07D277/30C07D417/04C07F9/4056C07F9/65318C07F9/6539C07F9/65583
    • All possible stereoisomer forms and mixtures of a compound of the formula ##STR1## wherein X is a halogen, R.sub.2 and R.sub.3 are individually selected from the group consisting of alkyl and cycloalkyl of up to 8 carbon atoms optionally substituted with at least one halogen, R.sub.1 is selected from the group consisting of alkyl, alkenyl, alkynyl and cycloalkyl of up to 12 carbon atoms optionally substituted with at least one halogen, aryl and heteroaryl of 5 to 6 ring members optionally substituted with at least one member of the group consisting of halogen, alkyl, alkenyl, alkynyl and cycloalkyl of up to 8 carbon atoms optionally substituted with at least one member of the group consisting of --NO.sub.2, --NH.sub.2, --CN, --OR', --SR", --SOR", --SO.sub.2 R", --NR"'.sub.2, --Ar, OAr.sub.1 and SAr.sub.2, R', R" and R"' are individually selected from the group consisting of alkyl, alkenyl, alkynyl and cycloalkyl of up to 12 carbon atoms optionally substituted by at least one halogen, Ar, Ar.sub.1 and Ar.sub.2 are aryl or heteroaryl of up to 14 carbon atoms optionally substituted with at least one member of the group consisting of halogen and alkyl, alkenyl, alkynyl and cycloalkyl of up to 8 carbon atoms optionally substituted by at least one member of the group consisting of halogen, --NO.sub.2, --NH.sub.2, --CN, --OR', --SR", --SOR", --SO.sub.2 R" and --NR"'.sub.2 and R', R" and R"' have the above definitions and their preparations and novel intermediates useful as pesticides.
    • 所有可能的立体异构体形式和式I化合物的混合物,其中X是卤素,R 2和R 3分别选自任选被至少一个卤素取代的至多8个碳原子的烷基和环烷基, R 1选自由至多12个碳原子的烷基,烯基,炔基和环烷基组成的组,其任选被至少一个5至6个环成员的卤素,芳基和杂芳基取代,任选被至少一个成员 卤素,烷基,烯基,炔基和至多8个碳原子的环烷基,任选被至少一个由-NO 2,-NH 2,-CN,-OR',-SR“,-SOR”, -SO 2 R“,-NR”'2,-Ar,OAr 1和SAr 2,R',R“和R”'分别选自至多12个碳的烷基,烯基,炔基和环烷基 任选被至少一个卤素取代的原子,Ar,Ar 1和Ar 2是至多1个的芳基或杂芳基 4个碳原子,任选被至少一个由卤素和至多8个碳原子的烷基,烯基,炔基和环烷基组成的组取代,任选被至少一个卤素,-NO 2,-NH 2, -CN,-OR',-SR“,-SOR”,-SO 2 R“和-NR”'2和R',R“和R”'具有上述定义及其制备和新型中间体 作为农药有用
    • 127. 发明授权
    • Mercapto-acylamino acids
    • 巯基 - 酰氨基酸
    • US5219886A
    • 1993-06-15
    • US768647
    • 1991-10-01
    • Elizabeth M. SmithPhilip M. DeCapiteBernard R. Neustadt
    • Elizabeth M. SmithPhilip M. DeCapiteBernard R. Neustadt
    • A61K38/22A61K31/16A61K31/195A61K31/215A61K31/265A61K31/38A61K31/40A61K31/47A61K31/55A61K31/675A61K38/55A61K45/06A61P3/00A61P9/00A61P9/12A61P13/02A61P15/00A61P43/00C07C319/12C07C323/00C07C323/56C07C323/60C07C327/06C07C327/32
    • C07C327/32A61K38/2242A61K38/556C07C323/60
    • Novel mercapto-acylamino acids of the formula ##STR1## wherein Q is hydrogen or R.sup.7 CO--;R.sup.1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl;R.sup.2 is hydrogen; lower alkyl; cyclolower alkyl; lower alkyl substituted with hydroxy, lower alkoxy, mercapto, lower alkylthio, aryl or heteroaryl; aryl; or heteroaryl;R.sup.3 is --OR.sup.5 or --NR.sup.5 R.sup.6 ;R.sup.4 and R.sup.9 are independently --(CH.sub.2).sub.q R.sup.8, provided that when R.sup.4 and R.sup.9 are both hydrogen, R.sup.2 is biphenylyl, phenoxyphenyl, phenylthiophenyl, naphthyl, heteroaryl, or lower alkyl substituted with hydroxy, lower alkoxy, mercapto or lower alkylthio;R.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl and aryl lower alkyl, or R.sup.5 and R.sup.6 together with the nitrogen to which they are attached form a 5-7 membered ring;R.sup.7 is hydrogen, lower alkyl or aryl;R.sup.8 is hydrogen, hydroxy, lower alkoxy, mercapto, lower alkylthio, aryl or heteroaryl;n is 1 or 2;p is 0 or 1;q is 0, 1 or 2; andt is 0 or 1; and the pharmaceutically acceptable salts thereof useful in the treatment of cardiovascular disorders and pain conditions and combinations of mercapto-acrylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating cardiovascular disorders are disclosed.
    • PCT No.PCT / US90 / 01787 Sec。 371日期1991年10月1日 102(e)1991年10月1日授权PCT 1990年4月6日提交。式IMA的新型巯基酰基氨基酸其中Q为氢或R7CO-; R 1是低级烷基,环己烷基,芳基或杂芳基; R2是氢; 低级烷基 环状烷基; 被羟基,低级烷氧基,巯基,低级烷硫基,芳基或杂芳基取代的低级烷基; 芳基; 或杂芳基; R3为-OR5或-NR5R6; R 4和R 9独立地为 - (CH 2)q R 8,条件是当R 4和R 9均为氢时,R 2为联苯基,苯氧基苯基,苯硫基苯基,萘基,杂芳基或被羟基,低级烷氧基,巯基或低级烷硫基取代的低级烷基; R 5和R 6独立地选自氢,低级烷基,羟基低级烷基,低级烷氧基低级烷基和芳基低级烷基,或者R 5和R 6与它们所连接的氮一起形成5-7元环; R7是氢,低级烷基或芳基; R8是氢,羟基,低级烷氧基,巯基,低级烷硫基,芳基或杂芳基; n为1或2; p为0或1; q是0,1或2; t为0或1; 和其可用于治疗心血管疾病和疼痛病症的药学上可接受的盐,以及用于治疗心血管疾病的巯基丙烯酰胺酸和心房利钠因子或血管紧张素转换酶抑制剂的组合。