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    • 41. 发明授权
    • Enkaphalin derivatives
    • 恩考芬素衍生物
    • US4341698A
    • 1982-07-27
    • US130431
    • 1980-03-14
    • Albert A. CarrRobert A. FarrJohn M. Kane
    • Albert A. CarrRobert A. FarrJohn M. Kane
    • A61K38/00C07D241/08C07K5/078C07K5/117C07C103/52
    • C07K5/06139C07D241/08C07K5/1024A61K38/00
    • Novel analgesic and antipsychotic agents having the formula ##STR1## wherein Q is ##STR2## in which R.sub.1 is hydrogen, hydroxy or halogen and R.sub.4 is hydrogen or, R.sub.1 and R.sub.4 are both hydroxy; Z is hydrogen or straight chain lower alkyl having from 1 to 4 carbon atoms and X is methylene, carbonyl, hydroxymethylene, thio, sulfinyl or sulfonyl, or Z and X, taken together, are methylidenyl, with the proviso that when X is sulfonyl or sulfinyl, Z is other than hydrogen; R.sub.5 is hydrogen or halogen, and R.sub.2 is H, a straight or branched lower alkyl group having from 1 to 4 carbon atoms, the group ##STR3## or the group ##STR4## wherein R.sub.3 is hydroxy, amino, alkylamino or dialkylamino wherein the alkyl moiety is straight or branched and has from 1 to 4 carbon atoms, diastereomers, enantiomers and pharmaceutically acceptable salts thereof.
    • 其中Q为 的新型止痛剂和抗精神病药,其中R1为氢,羟基或卤素,R4为氢或R1和R4均为羟基; Z是氢或具有1至4个碳原子的直链低级烷基,X是亚甲基,羰基,羟基亚甲基,硫代,亚磺酰基或磺酰基,或Z和X一起是亚甲基,条件是当X是磺酰基或 亚磺酰基,Z不是氢; R 5是氢或卤素,R 2是H,具有1至4个碳原子的直链或支链低级烷基,基团“IMAGE”或基团“IMAGE”,其中R 3是羟基,氨基,烷基氨基或二烷基氨基,其中烷基 部分是直链或支链的并且具有1至4个碳原子,非对映异构体,对映异构体和药学上可接受的盐。
    • 49. 发明授权
    • Calcium antagonists
    • 钙拮抗剂
    • US5106845A
    • 1992-04-21
    • US457997
    • 1990-01-10
    • Albert A. CarrHsien C. ChengJohn M. Kane
    • Albert A. CarrHsien C. ChengJohn M. Kane
    • C07D233/48C07D235/30C07D239/14C07D243/04C07D245/02C07D401/04
    • C07D401/04C07D233/48C07D235/30C07D239/14C07D243/04C07D245/02
    • The present invention is directed to a new class of cyclic guanidines of the formula: ##STR1## in which Q is represented by a substituent selected from the group consisting of (CH.sub.2).sub.n in which n is an integer from 2-10, ##STR2## A is a substituent selected from the group consisting of --NH--(CH.sub.2).sub.m in which m is an integer from 0-5, a piperidino substituent, or a piperazino substituent; both Ar and Ar.sub.1 are each independently represented by a phenyl ring, each of which may be optionally substituted with up to 3 substituents, each selected from the group consisting of halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, and trifluoromethyl; and R is represented by either hydrogen or a C.sub.1-4 alkyl; R.sub.1 is represented by hydrogen or a C.sub.1-4 alkyl; the optional isomers and tautomers thereof; and the pharmaceutically acceptable acid addition salts thereof, and their use as calcium antagonists.
    • 本发明涉及一类新的具有下式的环状胍,其中Q由选自(CH 2)n的取代基表示,其中n是2-10的整数,IMA图 > A是选自-NH-(CH 2)m的取代基,其中m是0-5的整数,哌啶子基取代基或哌嗪基取代基; Ar和Ar 1各自独立地表示为苯环,每个苯基环可任选被至多3个选自卤素,C 1-4烷基,C 1-4烷氧基和三氟甲基的取代基取代; 并且R由氢或C 1-4烷基表示; R1由氢或C1-4烷基表示; 其可选的异构体和互变异构体; 及其药学上可接受的酸加成盐及其作为钙拮抗剂的用途。