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    • 1. 发明授权
    • Tocolytic oxytocin receptor antagonists
    • 溶血性催产素受体拮抗剂
    • US5756504A
    • 1998-05-26
    • US718415
    • 1996-09-23
    • Mark G. BockBen E. EvansJ. Christopher CulbersonKevin F. GilbertKenneth E. RittlePeter D. Williams
    • Mark G. BockBen E. EvansJ. Christopher CulbersonKevin F. GilbertKenneth E. RittlePeter D. Williams
    • A61K31/435A61K31/4427A61K31/445A61K31/451A61K31/495A61P7/02A61P7/10A61P9/08A61P9/12A61P43/00C07D211/46C07D221/20C07D235/06C07D241/04C07D241/08C07D295/096C07D401/12C07D401/14C07D403/12
    • C07D221/20C07D235/06C07D241/04C07D241/08C07D295/096C07D401/12C07D401/14C07D403/12
    • Compounds of the formula X--Y--R, or the pharmaceutically acceptable salts and esters thereof, wherein X is ##STR1## Y is --SO.sub.2 --, --(CH.sub.2).sub.p -- or --CO--(CH.sub.2).sub.p --; R is unsubstituted or substituted phenyl where said substitutents are one or more of R.sup.5, R.sup.6 or R.sup.7 ; R.sup.1 is hydrogen, cyano, phenyl, --CONHR.sup.2, --CONR.sup.2 R.sup.2, --(CH.sub.2).sub.m --OR.sup.2, --(CH.sub.2).sub.p --S(O).sub.r --R.sup.2, --(CH.sub.2).sub.m --CO.sub.2 R.sup.2, --(CH.sub.2).sub.m --N.sub.3, --(CH.sub.2).sub.m --NH.sub.2 or --(CH.sub.2).sub.m --NR.sup.2 R.sup.2 ; R.sup.2 is hydrogen, C.sub.3-8 cycloalkyl or C.sub.1-5 alkyl; R.sup.5 and R.sup.6 are each independently selected from hydrogen, C.sub.1-5 alkoxy, halogen or --(CH.sub.2).sub.n --N(R.sup.2)--C(O)--R.sup.18 ; R.sup.7 is hydrogen or ##STR2## R.sup.11 is selected from hydrogen, C.sub.1-5 alkyl-carbonyl, --Z--R.sup.13, ##STR3## or substituted C.sub.1-5 alkyl wherein said alkyl substituent is unsubstituted, mono-, di- or tri-substituted pyridyl wherein said substitutents on said pyridyl are independently selected from halogen, C.sub.1-5 alkyl or C.sub.1-5 alkoxyl; R.sup.13 is unsubstituted or substituted C.sub.1-10 alkyl wherein the substituent is selected from --N(R.sup.2).sub.2, --NHR.sup.2 or imidazolyl; R.sup.14 and R.sup.15 are each independently selected from C.sub.1-5 alkyl, C.sub.1-5 alkoxy or halogen; R.sup.16 is hydrogen or oxo; R.sup.18 is C.sub.1-5 alkoxyl, unsubstituted or substituted C.sub.1-5 alkyl where said substituent is Het, unsubstituted or substituted C.sub.2-5 alkenyl where said subsituent is Het or Het; Het is benzimidazolyl, carboxymethyl-substituted benzimidazolyl or indolyl; m is an integer of from 1 to 5; p is an integer of from 1 to 3; and r is an integer of from 0 to 2. Such compounds as useful as oxytocin and vasopressin receptor antagonists.
    • PCT No.PCT / US95 / 03738 Sec。 371日期1996年9月23日 102(e)1996年9月23日PCT 1995年3月23日PCT公布。 WO95 / 25443 PCT出版物 日期为1995年9月28日,式X-Y-R或其药学上可接受的盐和酯的化合物,其中X为Y 2 - , - (CH 2)p - 或-CO-(CH 2)p - ; R是未取代或取代的苯基,其中所述取代基是R5,R6或R7中的一个或多个; R 1是氢,氰基,苯基,-CONHR 2,-CONR 2 R 2, - (CH 2)m OR 2, - (CH 2)pS(O)r -R 2, - (CH 2)m -CO 2 R 2, - (CH 2)m -N 3, - (CH 2)m -NH 2或 - (CH 2)m -NR 2 R 2; R2是氢,C3-8环烷基或C1-5烷基; R 5和R 6各自独立地选自氢,C 1-5烷氧基,卤素或 - (CH 2)n -N(R 2)-C(O)-R 18; R 7是氢或R 11选自氢,C 1-5烷基 - 羰基,-Z-R 13,取代基是未取代的,一取代,二取代或三取代的吡啶基,其中所述吡啶基上的所述取代基独立地 选自卤素,C 1-5烷基或C 1-5烷氧基; R 13是未取代的或取代的C 1-10烷基,其中取代基选自-N(R 2)2,-NHR 2或咪唑基; R 14和R 15各自独立地选自C 1-5烷基,C 1-5烷氧基或卤素; R 16是氢或氧代; R 18是C 1-5烷氧基,未取代或取代的C 1-5烷基,其中所述取代基是Het,未取代或取代的C2-5烯基,其中所述取代基是Het或Het; Het是苯并咪唑基,羧甲基取代的苯并咪唑基或吲哚基; m为1〜5的整数, p为1〜3的整数, 并且r是0至2的整数。用作催产素和加压素受体拮抗剂的这类化合物。
    • 2. 发明授权
    • Tocolytic oxytocin receptor antagonists
    • 溶血性催产素受体拮抗剂
    • US5464788A
    • 1995-11-07
    • US217270
    • 1994-03-24
    • Mark G. BockBen E. EvansJ. Christopher CulbersonKevin F. GilbertKenneth E. RittlePeter D. Williams
    • Mark G. BockBen E. EvansJ. Christopher CulbersonKevin F. GilbertKenneth E. RittlePeter D. Williams
    • A61K31/435A61K31/4427A61K31/445A61K31/451A61K31/495A61P7/02A61P7/10A61P9/08A61P9/12A61P43/00C07D211/46C07D221/20C07D235/06C07D241/04C07D241/08C07D295/096C07D401/12C07D401/14C07D403/12C07D273/00C07D413/00C07D451/00
    • C07D221/20C07D235/06C07D241/04C07D241/08C07D295/096C07D401/12C07D401/14C07D403/12
    • Compounds of the formula X--Y--R, or the pharmaceutically acceptable salts and esters thereof, wherein X is ##STR1## Y is --SO.sub.2 --, --(CH.sub.2).sub.p -- or --CO--(CH.sub.2).sub.p --; R is unsubstituted or substituted phenyl where said substitutents are one or more of R.sup.5, R.sup.6 or R.sup.7 ; R.sup.1 is hydrogen, cyano, phenyl,--CONHR.sup.2, --CONR.sup.2 R.sup.2, --(CH.sub.2).sub.m --OR.sup.2, --(CH.sub.2).sub.p --S(O).sub.r --R.sup.2, --(CH.sub.2).sub.m --CO.sub.2 R.sup.2, --(CH.sub.2).sub.m --N.sub.3, --(CH.sub.2).sub.m --NH.sub.2 or --(CH.sub.2).sub.m --NR.sup.2 R.sup.2 ; R.sup.2 is hydrogen, C.sub.3-8 cycloalkyl or C.sub.1-5 alkyl; R.sup.5 and R.sup.6 are each independently selected from hydrogen, C.sub.1-5 alkoxy, halogen or --(CH.sub.2).sub.n --N(R.sup.2)--C(O)--R.sup.18 ; R.sup.7 is hydrogen or ##STR2## R.sup.11 is selected from hydrogen, C.sub.1-5 alkylcarbonyl, ##STR3## or substituted C.sub.1-5 alkyl wherein said alkyl substituent is unsubstituted, mono-, di- or tri-substituted pyridyl wherein said substitutents on said pyridyl are independently selected from halogen, C.sub.1-5 alkyl or C.sub.1-5 alkoxyl; R.sup.13 is unsubstituted or substituted C.sub.1-10 alkyl wherein the substituent is selected from --N(R.sup.2).sub.2, --NHR.sup.2 or imidazolyl; R.sup.14 and R.sup.15 are each independently selected from C.sub.1-5 alkyl, C.sub.1-5 alkoxy or halogen; R.sup.16 is hydrogen or oxo; R.sup.18 is C.sub.1-5 alkoxyl, unsubstituted or substituted C.sub.1-5 alkyl where said substituent is Het, unsubstituted or substituted C.sub.2-5 alkenyl where said subsituent is Het or Het; Het is benzimidazolyl, carboxymethyl-substituted benzimidazolyl or indolyl; m is an integer of from 1 to 5; p is an integer of from 1 to 3; and r is an integer of from 0 to 2. Such compounds as useful as oxytocin and vasopressin receptor antagonists.
    • 式X-Y-R化合物或其药学上可接受的盐和酯,其中X为Y是-SO 2 - , - (CH 2)p - 或-CO-(CH 2)p - ; R是未取代或取代的苯基,其中所述取代基是R5,R6或R7中的一个或多个; R 1是氢,氰基,苯基,-CONHR 2,-CONR 2 R 2, - (CH 2)m OR 2, - (CH 2)pS(O)r -R 2, - (CH 2)m -CO 2 R 2, - (CH 2)m -N 3, - (CH 2)m -NH 2或 - (CH 2)m -NR 2 R 2; R2是氢,C3-8环烷基或C1-5烷基; R 5和R 6各自独立地选自氢,C 1-5烷氧基,卤素或 - (CH 2)n -N(R 2)-C(O)-R 18; R 7是氢或者R 11选自氢,C 1-5烷基羰基,或者被取代的C 1-5烷基,其中所述烷基取代基是未被取代的,一取代,二取代或三取代的吡啶基,其中所述吡啶基 独立地选自卤素,C 1-5烷基或C 1-5烷氧基; R 13是未取代的或取代的C 1-10烷基,其中取代基选自-N(R 2)2,-NHR 2或咪唑基; R 14和R 15各自独立地选自C 1-5烷基,C 1-5烷氧基或卤素; R 16是氢或氧代; R 18为C 1-5烷氧基,未取代或取代的C 1-5烷基,其中所述取代基为Het,未取代或取代的C2-5烯基,其中所述取代基为Het或Het; Het是苯并咪唑基,羧甲基取代的苯并咪唑基或吲哚基; m为1〜5的整数, p为1〜3的整数, 并且r是0至2的整数。用作催产素和加压素受体拮抗剂的这类化合物。