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    • 1. 发明申请
    • COMPOUND
    • 复合
    • WO2007003934A2
    • 2007-01-11
    • PCT/GB2006002465
    • 2006-07-03
    • STERIX LTDVICKER NIGELDAY JOANNA MARYBAILEY HELEN VICTORIAHEATON WESLEYGONZALEZ ANA MARIA RAMOSSHARLAND CHRISTOPHER MARKREED MICHAEL JOHNPUROHIT ATULPOTTER BARRY VICTOR LLOYD
    • VICKER NIGELDAY JOANNA MARYBAILEY HELEN VICTORIAHEATON WESLEYGONZALEZ ANA MARIA RAMOSSHARLAND CHRISTOPHER MARKREED MICHAEL JOHNPUROHIT ATULPOTTER BARRY VICTOR LLOYD
    • C07C211/00C07C211/58C07C233/36C07C237/22C07D209/20C07D211/56C07D211/58C07D211/62C07D211/96C07D215/38C07D215/44C07D223/12C07D223/16C07D239/42C07D401/12C07D401/14C07D405/06C07D409/06C07D409/12C07D451/04
    • C07C237/22C07C233/36C07D209/20C07D211/56C07D211/58C07D211/62C07D211/96C07D215/38C07D215/44C07D223/12C07D223/16C07D239/42C07D401/12C07D401/14C07D405/06C07D409/06C07D409/12C07D451/04
    • There is provided a compound having Formula (I) wherein each of R 1 , R 2 , R 4 , R 5 , R 6 and R 7 are independently selected from (a) H, (b) R 17 , -OC(R 17 ) 3 , -OCH(R 17 ) 2 , -(OCH 2 R) 17 , -C(R 17 ) 3 , -CH(R 17 ) 2 , or -CH 2 R 17 wherein R 17 is a halogen; (c) -CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (l) aryloxy; (m) -SO 2 -alkyl; and (n) -N(R 11 )C(O)R 13 ; wherein the optional substituents of (d) (e) (f) (h) and (i) are selected from the group consisting of: C 1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl ; each of rings A and B are selected from five or six membered carbon rings optionally containing one or more hetero atoms selected from N, S, and O and optionally having fused thereto a further ring; X is an optional group selected from O, S, S=O, S(=O)2, C=O, S(=O) 2 NR 8 , C=ONR 9 , NR 10 , wherein R 8 , R 9 and R 10 are independently selected from H and hydrocarbyl, wherein n and p are independently selected from O and 1 ; Y is (R 11 ) 1-3 wherein each R 11 is independently selected from NR 12 , CR 13 R 14 , S(=O) 2 and C=O, wherein R 12 , R 13 and R 14 are independently selected from H and hydrocarbyl; Z is selected from (i) six or seven membered ring containing carbon and at least one nitrogen, which may be optionally substituted wherein the substituents may together form further ring fused thereto; and (ii) a -R 15 -NR 16 - group wherein R 15 is an optionally substituted C 1-6 alkyl chain and R 16 is selected from H and hydrocarbyl; and R 3 is selected from Formula (A).
    • 提供了具有式(I)的化合物,其中R 1,R 2,R 4,R 5, R a,R 6和R 7独立地选自(a)H,(b)R 17,-OC(R a 3, - OCH(R 17)2 - , - (OCH 2 R 2) ) - (R 17)3 - , - (R 17)2 - , - (R 17) 或者其中R 17是卤素;或者其中R 17是卤素; (c)-CN; (d)任选取代的烷基,(e)任选取代的杂烷基; (f)任选取代的芳基; (g)任选取代的杂芳基; (h)任选取代的芳基烷基; (i)任选取代的杂芳基烷基; (j)羟基; (k)烷氧基; (I)芳氧基; (m)-SO 2 - 烷基; 和(n)-N(R 11)C(O)R 13; 其中(d)(e)(f)(h)和(i)的任选取代基选自:C 1-6烷基,卤素,氰基,硝基,卤代烷基, 羟基,烷氧基,羧基,羧基烷基,羧酰胺,巯基,氨基,烷基氨基,二烷基氨基,磺酰基,亚磺酰氨基,芳基和杂芳基; 环A和B各自选自5或6元碳环,任选地含有一个或多个选自N,S和O的杂原子,并且任选地与另外的环稠合; X是选自O,S,S = O,S(= O)2,C = O,S(= O)2 NR 8,C 其中R 8,R 9和R 10各自独立地为氢, 独立地选自H和烃基,其中n和p独立地选自O和1; Y是(R 11-11)1-3,其中每个R 11独立地选自NR 12,CR 11, S(= O)2和C = O,其中R 12,R 12, 13和R 14独立地选自H和烃基; Z选自(i)含有六元或七元环的碳和至少一个氮,其可以是任选取代的,其中取代基可以一起形成稠合的另外的环; 其中R 15是任选取代的C 1-6烷基,和(ⅱ)R 15是-NR 16 - 烷基链和R 16选自H和烃基; 和R 3选自式(A)。
    • 2. 发明申请
    • INHIBITORS OF 17BETA-HYDROXYSTEROID DEHYDROGENASE
    • 17BA-羟基脱氢酶抑制剂的抑制剂
    • WO2009066072A3
    • 2009-10-15
    • PCT/GB2008003889
    • 2008-11-19
    • STERIX LTDVICKER NIGELBAILEY HELEN VICTORIAHEATON WESLEYDAY JOANNA MARYPUROHIT ATULPOTTER BARRY VICTOR LLOYD
    • VICKER NIGELBAILEY HELEN VICTORIAHEATON WESLEYDAY JOANNA MARYPUROHIT ATULPOTTER BARRY VICTOR LLOYD
    • C07C209/14A61K31/167A61K31/36A61K31/4409A61P5/24A61P35/00C07C211/50C07C233/43C07C237/42C07D207/26C07D211/58C07D211/62C07D317/66
    • C07D207/26C07C217/90C07C233/43C07C237/42C07D211/58C07D211/62C07D317/66
    • There is provided a compound having Formula (I), wherein each of R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently selected from (a) H, (b) R13, -OC(R13)3, -OCH(R13)2, -OCH2R13, -C(R13)3, -CH(R13)2, or -CH2R13 wherein R13 is a halogen; (c) -CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (I) aryloxy; (m) -SO2-alkyl; and (n) -N(R14)C(O)R15, wherein R14 and R15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (T) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=O, S(=O)2, C=O, S(=O)2NR16, C=ONR17, NR18, in which R16, R17, and R18 are independently selected from H and hydrocarbyl, R10 is selected from H and hydrocarbyl, R11 is selected from CR19R20 and C=O, in which R19 and R20 are independently selected from H and hydrocarbyl, R12 is selected from a substituted five or six membered carbon rings optionally containing one or more hetero atoms selected from N, S, and O and optionally having fused thereto a further ring, and wherein the one or more substituents are selected from hydrocarbyl groups.
    • 提供具有式(I)的化合物,其中R1,R2,R3,R4,R5,R6,R7,R8和R9各自独立地选自(a)H,(b)R13,-OC(R13) 3,-OCH(R 13)2,-OCH 2 R 13,-C(R 13)3,-CH(R 13)2或-CH 2 R 13,其中R 13是卤素; (c)-CN; (d)任选取代的烷基,(e)任选取代的杂烷基; (f)任选取代的芳基; (g)任选取代的杂芳基; (h)任选取代的芳基烷基; (i)任选取代的杂芳基烷基; (j)羟基; (k)烷氧基; (I)芳氧基; (m)-SO 2 - 烷基; 和(n)-N(R 14)C(O)R 15,其中R 14和R 15独立地选自H和烃基,其中选择(d)(e)(T)(h)和(i) 羟基,C 1-6烷氧基,羧基,羧基烷基,羧酰胺,巯基,氨基,烷基氨基,二烷基氨基,磺酰基,亚磺酰氨基,芳基和杂芳基; 其中n和p独立地选自0和1; X是选自O,S,S = O,S(= O)2,C = O,S(= O)2NR16,C = ONR17,NR18的任选基团,其中R 16,R 17和R 18独立地选自 R 10选自H和烃基,R 11选自CR 19 R 20和C = O,其中R 19和R 20独立地选自H和烃基,R 12选自取代的五或六元碳环,任选含有 一个或多个选自N,S和O的杂原子,并且任选地与另一个环稠合,并且其中一个或多个取代基选自烃基。
    • 6. 发明专利
    • COMPOUND
    • CA2703893A1
    • 2009-05-28
    • CA2703893
    • 2008-11-19
    • STERIX LTD
    • VICKER NIGELBAILEY HELEN VICTORIAHEATON WESLEYDAY JOANNA MARYPUROHIT ATULPOTTER BARRY VICTOR LLOYD
    • C07C209/14A61K31/167A61K31/36A61K31/4409A61P5/24A61P35/00C07C211/50C07C233/43C07C237/42C07D207/26C07D211/58C07D211/62C07D317/66
    • There is provided a compound having Formula (I), wherein each of R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently selected from (a) H, (b) R13, -OC(R13)3, -OCH(R13)2, -OCH2R13, -C(R13)3, -CH(R13)2, or -CH2R13 wherein R13 is a halogen; (c) -CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (I) aryloxy; (m) -SO2-alkyl; and (n) -N(R14)C(O)R15, wherein R14 and R15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (T) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=O, S(=O)2, C=O, S(=O)2NR16, C=ONR17, NR18, in which R16, R17, and R18 are independently selected from H and hydrocarbyl, R10 is selected from H and hydrocarbyl, R11 is selected from CR19R20 and C=O, in which R19 and R20 are independently selected from H and hydrocarbyl, R12 is selected from a substituted five or six membered carbon rings optionally containing one or more hetero atoms selected from N, S, and O and optionally having fused thereto a further ring, and wherein the one or more substituents are selected from hydrocarbyl groups.