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1. 发明授权

US08829003B2 Compounds for treating proliferative disorders 有权
公开(公告)号：US08829003B2
公开(公告)日：2014-09-09
申请号：US13806602
申请日：2011-06-21
申请人： Shudong Wang , Osama Chahrour , Tiangong Lu , Anran Hu
发明人： Shudong Wang , Osama Chahrour , Tiangong Lu , Anran Hu
IPC分类号： A61K31/497 , C07D213/62
CPC分类号： C07D213/74 , C07D213/73 , C07D213/75 , C07D213/76 , C07D239/47 , C07D401/04
摘要： A compound of formula (I) or a pharmaceutically acceptable salt or solvate or physiologically hydrolysable, solubilizing or immobilizable derivative thereof; wherein: any one or two of X., X2 and X3 is a N atom and the remaining two or one of X1, X2 and X3 are independently CR13; Y is selected from SO2 and SO; R1, R2, R3, and R7 and the one or two R13 groups are each independently selected from H and R10, R10 is selected from R8, alkyl, aryl, heteroaryl and combinations of two or more thereof and combinations with one or more R9, or R10 is one or more moieties R11 Sinking one or more alkyl, alkoxy, aryl, heteroaryl or R8 or R9 groups or combinations thereof, directly or via a moiety selected from alkylene, arylene, heteroarylene or combinations thereof, wherein alkyl, aryl, heteroaryl groups or moieties thereof may be substituted with one or more groups R12, or R10 is selected from a group R12; R11 is selected from 0-, N—, NH—, N═C, CO—, C00-, CON—, CONH—, S02-, S02N—, S02NH—; R12 is selected from halogen, NH2, N02, CN, OH, COOH, CONH2, C(═NH)NH2, S03H, S02NH2, S02CH3, OCH3, OCH2CH3, CF3; R8 and R9 comprise one or more solubilizing moieties independently chosen from i) neutral hydrophilic groups, ii) ionisable organic acids, iii) ionisable organic bases, iv} chemical functions or moieties providing covalent or non-covalent attachment or binding to a solid phase or an immobile receptor and combinations thereof; R4, R5 and R6 are each independently selected from H and R10, or two of R4 to R6 are linked to form a cyclic ether or amine containing one or more additional oxygen or nitrogen atoms. The compound may be used for treating a condition mediated by one or more enzymes selected from AKT, Aurora kinase, BCR-ABL, CDK, FLT, GSK3, IKK, JAK, MAPK, PDGF, PI3K, PKA, PKB, PKC, PLK, Src and VEGF family enzymes, or for treating cancer or other proliferative disorder, or for inhibiting growth of cancer cells, or for inducing apoptosis of cancer cells, in a human or animal subject.

2. 发明申请

US20130190325A1 COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS 有权
公开(公告)号：US20130190325A1
公开(公告)日：2013-07-25
申请号：US13806602
申请日：2011-06-21
申请人： Shudong Wang , Osama Chahrour , Tiangong Lu , Anran Hu
发明人： Shudong Wang , Osama Chahrour , Tiangong Lu , Anran Hu
IPC分类号： C07D213/74 , C07D239/47 , C07D213/75 , C07D213/76 , C07D401/04
CPC分类号： C07D213/74 , C07D213/73 , C07D213/75 , C07D213/76 , C07D239/47 , C07D401/04
摘要： A compound of formula (I) or a pharmaceutically acceptable salt or solvate or physiologically hydrolysable, solubilising or immobilisable derivative thereof; wherein: any one or two of X., X2 and X3 is a N atom and the remaining two or one of X1, X2 and X3 are independently CR13; Y is selected from SO2 and SO; R1, R2, R3, and R7 and the one or two R13 groups are each independently selected from H and R10, R10 is selected from R8, alkyl, aryl, heteroaryl and combinations of two or more thereof and combinations with one or more R9, or R10 is one or more moieties R11 Sinking one or more alkyl, alkoxy, aryl, heteroaryl or R8 or R9 groups or combinations thereof, directly or via a moiety selected from alkylene, arylene, heteroarylene or combinations thereof, wherein alkyl, aryl, heteroaryl groups or moieties thereof may be substituted with one or more groups R12, or R10 is selected from a group R12; R11 is selected from 0-, N—, NH—, N═C, CO—, C00-, CON—, CONH—, S02-, S02N—, S02NH—; R12 is selected from halogen, NH2, N02, CN, OH, COOH, CONH2, C(═NH)NH2, S03H, S02NH2, S02CH3, OCH3, OCH2CH3, CF3; R8 and R9 comprise one or more solubilising moieties independently chosen from i) neutral hydrophilic groups, ii) ionisable organic acids, iii) ionisable organic bases, iv} chemical functions or moieties providing covalent or non-covalent attachment or binding to a solid phase or an immobile receptor and combinations thereof; R4, R5 and R6 are each independently selected from H and R10, or two of R4 to R6 are linked to form a cyclic ether or amine containing one or more additional oxygen or nitrogen atoms. The compound may be used for treating a condition mediated by one or more enzymes selected from AKT, Aurora kinase, BCR-ABL, CDK, FLT, GSK3, IKK, JAK, MAPK, PDGF, PI3K, PKA, PKB, PKC, PLK, Src and VEGF family enzymes, or for treating cancer or other proliferative disorder, or for inhibiting growth of cancer cells, or for inducing apoptosis of cancer cells, in a human or animal subject.

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