发明名称 1,2,4-thiazoloidin-3-one derivatives and their use in the treatment of cancer
摘要 According to the invention there is provided a compound of formula (I) wherein: A represents C(═N—W-D) or S; B represents S or C(—NH—W-D); when: A represents C(═N—W-D) and B represents S then the bond between B and the NH atom is a single bond; or A represents S and B represents C(—NH—W-D) then the bond between B and the NH atom is a double bond; X represents -Q-[CRxRy]n—; W represents —[CRxRy]m— or —C(O)—[CRxRy]p—; Q represents a bond, —N(Ra)—, —S—, or —O—; A1 to A5 respectively represent C(R1), C(R2), C(R3), C(R4) and C(R5), or, alternatively, up to two of A1 to A5 may independently represent N; D represents phenyl, pyridyl or pyrimidinyl optionally substituted by one or more R6 groups, which compounds are useful in the treatment of cancer.
申请公布号 US9162994(B2) 申请公布日期 2015.10.20
申请号 US201013381426 申请日期 2010.07.08
申请人 BETAGENON AB 发明人 Westman Jacob;Hallett Allan;Vågberg Jan
分类号 C07D285/08;C07D417/10;C07D417/12;A61K31/433;A61K31/4439;A61P35/00 主分类号 C07D285/08
代理机构 McCarter & English, LLP 代理人 McCarter & English, LLP ;Davis Steven G.;Bai Mei
主权项 1. A compound of formula I, wherein: A represents S; B represents C(—NH—W-D); the bond between B and the NH group is a double bond; X represents —Q-[CRxRy]n—; W represents —[CRxRy]m— or —C(O)—[CRxRy]p—; Q represents a bond, —N(Ra)—, —S—, or —O—; A1 to A5 respectively represent C(R1), C(R2), C(R3), C(R4) and C(R5), or, alternatively, up to two of A1 to A5 may independently represent N; D represents phenyl, pyridyl or pyrimidinyl optionally substituted by one or more R6 groups; Rx and Ry, on each occasion when used herein, are independently selected from H, halo, C1-6 alkyl (optionally substituted by one or more halo atoms), aryl (optionally substituted by one or more halo atoms) or Rx and Ry are linked to form, along with the carbon atom to which they are attached, a non-aromatic 3- to 8-membered ring, optionally containing 1 to 3 heteroatoms selected from O, S and N, which ring is itself optionally substituted by one or more substituents selected from halo or C1-6 alkyl (optionally substituted by one or more halo atoms); R1 to R5 independently represent H, halo, —R7, —CF3, —CN, —NO2, —C(O)R7, —C(O)OR7, —C(O)—N(R7a)R7b, —N(R7a)R7b, —N(R7)3+, —SR7, —OR7, —NH(O)R7, —SO3R7, aryl or heteroaryl (which aryl and heteroaryl groups are themselves optionally and independently substituted by one or more groups selected from halo and R16), or any two of R1 to R5 which are adjacent to each other are optionally linked to form, along with two atoms of the essential benzene ring in the compound of formula I, an aromatic or non-aromatic 3- to 8-membered ring, optionally containing 1 to 3 heteroatoms selected from O, S and N, which ring is itself optionally substituted by one or more substituents selected from halo, —R7, —OR7 and ═O; R6 independently represents, on each occasion when used herein, cyano, —NO2, halo, C1-6 alkyl (which alkyl group is substituted by one or more halo atoms), —OR8, —N(R8)C(O)R8, —NR9R10, —SR11, —Si(R12)3, —OC(O)R13, —C(O)OR13, —C(O)R14, —C(O)NR15aR15b, —S(O)2NR15cR15d, aryl or heteroaryl (which aryl and heteroaryl groups are themselves optionally and independently substituted by one or more groups selected from halo and R16), or any two R6 groups which are adjacent to each other are optionally linked to form, along with two atoms of the essential benzene ring in the compound of formula I, an aromatic or non-aromatic 3- to 8-membered ring, optionally containing 1 to 3 heteroatoms selected from O, S and N, which ring is itself optionally substituted by one or more substituents selected from halo, —R7, —OR7 and ═O; R7, on each occasion when used herein, is selected from H or C1-C6 alkyl, C1-C6 cycloalkyl, aryl and heteroaryl (wherein the latter four groups are optionally substituted by one or more halo atoms); R7a and R7b are independently selected from H, or C1-C6 alkyl, C1-C6 cycloalkyl, aryl and heteroaryl, or R7a and R7b are optionally linked to form, along with the nitrogen atom to which they are attached, an aromatic or non-aromatic 3- to 8-membered ring, optionally containing 1 to 3 heteroatoms selected from O, S and N, which ring is itself optionally substituted by one or more substituents selected from halo, —R7, —OR7 and ═O; Ra, R8, R9, R10, R11, R12, R13, R14, R15a, R15b, R15c and R15d, on each occasion where used herein, independently represent H or R16; R16 represents, on each occasion when used herein, C1-6 alkyl optionally substituted by one or more halo atoms; n represents 1 or 2; m represents 0, 1 or 2; and p represents 0, 1 or 2; or a pharmaceutically acceptable salt or solvate, or a pharmaceutically functional derivative thereof.
地址 Umea SE