专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2008117061A3 TETRAHYDROISOQUINOLINES AS TUMOUR GROWTH INHIBITORS 审中-公开
标题翻译：四氢叶酸作为肿瘤生长抑制剂
公开(公告)号：WO2008117061A3
公开(公告)日：2009-05-14
申请号：PCT/GB2008001072
申请日：2008-03-27
申请人： STERIX LTD , JOURDAN FABRICE , KIMBERLEY MERIEL , LEESE MATTHEW , POTTER BARRY VICTOR LLOYD , PUROHIT ATUL , REED MICHAEL JOHN
发明人： JOURDAN FABRICE , KIMBERLEY MERIEL , LEESE MATTHEW , POTTER BARRY VICTOR LLOYD , PUROHIT ATUL , REED MICHAEL JOHN
IPC分类号： A61K31/40 , A61K31/403 , A61K31/435 , A61K31/47 , A61K31/55 , A61P35/00
CPC分类号： A61K31/40 , A61K31/403 , A61K31/435 , A61K31/47 , A61K31/55
摘要： The present invention provides a compound of Formula (I) or Formula (Il) wherein A is selected from CR10R11, -S(=O)2-, -NR12-,and C=O, wherein R10 and R11 independently selected from H, -OH, hydrocarbyl, -CN, -NO2, and halogens, R12 is selected from H and hydrocarbyl; B is selected from (CR13R14)1-3, C=O, CR15R16C=O, -S(=O)2-, -NR17- and -NR18-C(=O)-, wherein each of R13, R14, R15 and R16 is independently selected from H, -OH, hydrocarbyl, -CN, -NO2, and halogens, R17 and R18 are independently selected from H and hydrocarbyl; R1 is selected from OH, O-hydrocarbyl, O-heterohydrocarbyl, -SO2-hydrocarbyl, -CH=CH2, halogen, -OSO2NR19R20, -C(=O)-NR21R22, -NR23-C(=O)H and -NR35R36; wherein each of R19, R20, R21, R22, R23, R35 and R36 is independently is selected from H and hydrocarbyl; R2 is selected from H, -O-hydrocarbyl, -S-hydrocarbyl, hydrocarbyl, -CN, -NO2, and halogens, R3 is selected from Formula (A), Formula (B), Formula (C), Formula (D) wherein each of R4, R5, R6, R7 and R8 is independently selected from H, -OH, hydrocarbyl, -O-hydrocarbyl, -COOH or an ester thereof, halocarbyl, -O-halocarbyl, acyl, -O-acyl, -NR29-acyl, -O-SO2NR19R20, -NR30R31, -NR32SO2R33, -CN, -NO2, and halogens, R9 is selected from H and hydrocarbyl, and each R29 to R33 is independently selected from H and hydrocarbyl; and wherein two or more of R4, R5, R6, R7, R8 and R9 may together form a ring; wherein when R1 is OH and R3 is of Formula (D), (i) at least one of R4, R5, R6, R7 and R8 is independently selected from halocarbyl, -O-halocarbyl, -O-acyl, -NR29-acyl, -O- SO2NR19R20, -NR30R31, -NR32SO2R33, -CN, and halogens, or (ii) two or more of R4, R5, R6, R7 and R8 together form a ring, or (iii) at least three of R4, R5, R6, R7 and R8 are independently selected from -OH, hydrocarbyl, -O-hydrocarbyl, halocarbyl, -O-halocarbyl, -O-acyl, -NR29-acyl, -O-SO2NR19R20, -NR30R31, -NR32SO2R33, -CN, -NO2, and halogens; wherein h is an optional bond, wherein G is CR24R25, wherein R24 and R25 independently selected from H, -OH, hydrocarbyl, -CN, -NO2, and halogens, or wherein when h is present G is CR24, wherein R24 is selected from H, -OH, hydrocarbyl, -CN, -NO2, and halogens; n is 0, 1 or 2, each D is independently selected from O, NR26 and CR27R28, wherein each R26 is independently selected from H and hydrocarbyl; and each R27 and R28 is independently selected from H, -OH, hydrocarbyl, -CN, -NO2, and halogens.
摘要翻译：本发明提供式（I）或式（II）的化合物，其中A选自CR 10 R 11，-S（= O）2 - ， - NR 12 - 和C = O，其中R 10和R 11独立地选自H， -OH，烃基，-CN，-NO 2和卤素，R 12选自H和烃基; B选自（CR13R14）1-3，C = O，CR15R16C = O，-S（= O）2-，-NR17-和-NR18-C（= O） - ，其中R13，R14，R15 并且R 16独立地选自H，-OH，烃基，-CN，-NO 2和卤素，R 17和R 18独立地选自H和烃基; R 1选自OH，O-烃基，O-杂烃基，-SO 2 - 烃基，-CH = CH 2，卤素，-OSO 2 NR 19 R 20，-C（= O）-NR 21 R 22，-NR 23 -C（= O）H和-NR 35 R 36 ; 其中R19，R20，R21，R22，R23，R35和R36各自独立地选自H和烃基; R2选自H，-O-烃基，-S-烃基，烃基，-CN，-NO 2和卤素，R 3选自式（A），式（B），式（C），式（D）其中R4，R5，R6，R7和R8各自独立地选自H，-OH，烃基，-O-烃基，-COOH或其酯，卤代羰基，-O-卤代羰基，酰基，-O-酰基， NR29-酰基，-O-SO2NR19R20，-NR30R31，-NR32SO2R33，-CN，-NO2和卤素，R9选自H和烃基，每个R29至R33独立地选自H和烃基; 并且其中R4，R5，R6，R7，R8和R9中的两个或更多个可以一起形成环; 其中当R 1是OH且R 3具有式（D）时，（i）R 4，R 5，R 6，R 7和R 8中的至少一个独立地选自卤代烃基，-O-卤代羰基，-O-酰基，-NR 29 - ，-O-SO 2 NR 19 R 20，-NR 30 R 31，-NR 32 SO 2 R 33，-CN和卤素，或（ii）R4，R5，R6，R7和R8中的两个或更多个一起形成环，或（iii） R5，R6，R7和R8独立地选自-OH，烃基，-O-烃基，卤代烃基，-O-卤代烃基，-O-酰基，-NR29-酰基，-O-SO2NR19R20，-NR30R31，-NR32SO2R33， CN，-NO 2和卤素; 其中h是任选的键，其中G是CR 24 R 25，其中R 24和R 25独立地选自H，-OH，烃基，-CN，-NO 2和卤素，或其中当存在h时，G是CR 24，其中R 24选自 H，-OH，烃基，-CN，-NO 2和卤素; n是0,1或2，每个D独立地选自O，NR 26和CR 27 R 28，其中每个R 26独立地选自H和烃基; 并且每个R 27和R 28独立地选自H，-OH，烃基，-CN，-NO 2和卤素。

2. 发明申请

WO2008117061A2 COMPOUND 审中-公开
标题翻译：复合
公开(公告)号：WO2008117061A2
公开(公告)日：2008-10-02
申请号：PCT/GB2008/001072
申请日：2008-03-27
申请人： STERIX LIMITED , JOURDAN, Fabrice , KIMBERLEY, Meriel , LEESE, Matthew , POTTER, Barry, Victor, Lloyd , PUROHIT, Atul , REED, Michael, John
发明人： JOURDAN, Fabrice , KIMBERLEY, Meriel , LEESE, Matthew , POTTER, Barry, Victor, Lloyd , PUROHIT, Atul , REED, Michael, John
IPC分类号： A61K31/40 , A61K31/403 , A61K31/435 , A61K31/47 , A61K31/55 , A61P35/00
CPC分类号： A61K31/40 , A61K31/403 , A61K31/435 , A61K31/47 , A61K31/55
摘要： The present invention provides a compound of Formula (I) or Formula (Il) wherein A is selected from CR 10 R 11 , -S(=O) 2 -, -NR 12 -,and C=O, wherein R 10 and R 11 independently selected from H, -OH, hydrocarbyl, -CN, -NO 2 , and halogens, R 12 is selected from H and hydrocarbyl; B is selected from (CR 13 R 14 ) 1-3 , C=O, CR 15 R 16 C=O, -S(=O) 2 -, -NR 17 - and -NR 18 -C(=O)-, wherein each of R 13 , R 14 , R 15 and R 16 is independently selected from H, -OH, hydrocarbyl, -CN, -NO 2 , and halogens, R 17 and R 18 are independently selected from H and hydrocarbyl; R 1 is selected from OH, O-hydrocarbyl, O-heterohydrocarbyl, -SO 2 -hydrocarbyl, -CH=CH 2 , halogen, -OSO 2 NR 19 R 20 , -C(=O)-NR 21 R 22 , -NR 23 -C(=O)H and -NR 35 R 36 ; wherein each of R 19 , R 20 , R 21 , R 22 , R 23 , R 35 and R 36 is independently is selected from H and hydrocarbyl; R 2 is selected from H, -O-hydrocarbyl, -S-hydrocarbyl, hydrocarbyl, -CN, -NO 2 , and halogens, R 3 is selected from Formula (A), Formula (B), Formula (C), Formula (D) wherein each of R 4 , R 5 , R 6 , R 7 and R 8 is independently selected from H, -OH, hydrocarbyl, -O-hydrocarbyl, -COOH or an ester thereof, halocarbyl, -O-halocarbyl, acyl, -O-acyl, -NR 29 -acyl, -O-SO 2 NR 19 R 20 , -NR 30 R 31 , -NR 32 SO 2 R 33 , -CN, -NO 2 , and halogens, R 9 is selected from H and hydrocarbyl, and each R 29 to R 33 is independently selected from H and hydrocarbyl; and wherein two or more of R 4 , R 5 , R 6 , R 7 , R 8 and R 9 may together form a ring; wherein when R 1 is OH and R 3 is of Formula (D), (i) at least one of R 4 , R 5 , R 6 , R 7 and R 8 is independently selected from halocarbyl, -O-halocarbyl, -O-acyl, -NR 29 -acyl, -O- SO 2 NR 19 R 20 , -NR 30 R 31 , -NR 32 SO 2 R 33 , -CN, and halogens, or (ii) two or more of R 4 , R 5 , R 6 , R 7 and R 8 together form a ring, or (iii) at least three of R 4 , R 5 , R 6 , R 7 and R 8 are independently selected from -OH, hydrocarbyl, -O-hydrocarbyl, halocarbyl, -O-halocarbyl, -O-acyl, -NR 29 -acyl, -O-SO 2 NR 19 R 20 , -NR 30 R 31 , -NR 32 SO 2 R 33 , -CN, -NO 2 , and halogens; wherein h is an optional bond, wherein G is CR 24 R 25 , wherein R 24 and R 25 independently selected from H, -OH, hydrocarbyl, -CN, -NO 2 , and halogens, or wherein when h is present G is CR 24 , wherein R 24 is selected from H, -OH, hydrocarbyl, -CN, -NO 2 , and halogens; n is 0, 1 or 2, each D is independently selected from O, NR 26 and CR 27 R 28 , wherein each R 26 is independently selected from H and hydrocarbyl; and each R 27 and R 28 is independently selected from H, -OH, hydrocarbyl, -CN, -NO 2 , and halogens.
摘要翻译：本发明提供式（I）或式（II）的化合物，其中A选自CR 10 R 11，-S（= O）2 -NR 12 - 和C = O，其中R 10和R 11独立地选自H，-OH ，烃基，-CN，-NO 2 N 2和卤素，R 12选自H和烃基; B选自（CR 13，R 14）1-3，C = O，CR 15 R， C 16 -C 16 O，-S（= O）2 - ， - NR 17 - 和-NR 18 - C（= O） - ，其中R 13，R 14，R 15和R 16中的每一个为独立地选自H，-OH，烃基，-CN，-NO 2 2和卤素，R 17和R 18独立地选自 H和烃基; R 1选自OH，O-烃基，O-杂烃基，-SO 2 - 烃基，-CH = CH 2，卤素， -OSO 2 NR 20 R 20，-C（= O）-NR 21 R 22 R 23，-C（= O）H和-NR 35 R 36; 其中R 19，R 20，R 21，R 22，R 23， R 35和R 36独立地选自H和烃基; R 2选自H，-O-烃基，-S-烃基，烃基，-CN，-NO 2 2和卤素，R 3， SUB>选自式（A），式（B），式（C），式（D），其中R 4，R 5，R 5， R 6，R 7和R 8独立地选自H，-OH，烃基，-O-烃基，-COOH或其酯，卤代烃基，-O-卤代烃基，酰基，-O-酰基，-NR 29 - 酰基，-O-SO 2 NR 19 R > 20 ，-NR 30 30，-NR 32，SO 2， 33，-CN，-NO 2，和卤素，R 9选自H和烃基，每个R 29是氢， R 33独立地选自H和烃基; 并且其中R 4，R 5，R 6，R 7，R 7， 8和R 9可以一起形成环; 其中当R 1是OH且R 3具有式（D）时，（i）R 4，R 1，R 2中的至少一个 R 5，R 7，R 8和R 8独立地选自卤代烃基，-O-卤代烃基，-O- 酰基，-NR 29 - 酰基，-O- SO 2 NR 19 R 20，-NR N > 30 32，-NR 32 SO 2 R 33，-CN和卤素，或（ii）R 4，R 5，R 6，R 7和R 2中的两个或更多个一起形成环，或（iii）R 4，R 5，R 6和R 5中的至少三个， R 7和R 8独立地选自-OH，烃基，-O-烃基，卤代烃基，-O-卤代烃基，-O-酰基，-NR _{29-酰基，-O-SO 2 NR 20 R 20，-NR 30， R 31，-NR 32，SO 2，R 33，-CN，-NO 2， SUB>和卤素; 其中h是任选的键，其中G是CR 24 R 25，其中R 24和R 25独立地是选自H，-OH，烃基，-CN，-NO 2 N 2和卤素，或其中当存在h时，G是CR 24，其中R 24 H，-OH，烃基，-CN，-NO 2，和卤素; n是0,1或2，每个D独立地选自O，NR 26和CR 27 R 28，其中每个R _{26 独立地选自H和烃基; 并且每个R 27和R 28独立地选自H，-OH，烃基，-CN，-NO 2 N 2和卤素。}}

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式