公开(公告)号：EP1467967B1

公开(公告)日：2011-04-27

申请号：EP03700255.7

申请日：2003-01-17

申请人： THE HOSPITAL FOR SICK CHILDREN

发明人： ROIFMAN, Chaim, M. ,  DEMIN, Peter ,  GRUNBERGER, Thomas ,  ROUNOVA, Olga ,  CIMPEAN, Octavian Laurand

IPC分类号： C07C255/41 ,  A61K31/165

CPC分类号： C07C255/41 ,  C07C317/46 ,  C07D213/71

摘要： The following compounds of formulae (I) and (III) which may be useful in treating a variety of cell proliferative disorders are disclosed: Fomula (I), (II), wherein R1, R2 and R3 are each independently selected from H, OH, C1-6 alkyl, C1-6 alkoxy, NH2, NH-C1-6alkyl, N(C1-6 alkyl)(C1-6 alkyl), SH, S-C1-6 alkyl, NO2, CF3, OCF3 and halo; R4 is unsubstituted Ar, or Ar substituted with 1-4 substituents, independently selected from C1-6 alkyl, C1-6 alkoxy and halo; X is selected from (CH2CH2O)n and (CH2)n, and n=1-4.

公开(公告)号：EP1654220A1

公开(公告)日：2006-05-10

申请号：EP04738022.5

申请日：2004-07-30

申请人： THE HOSPITAL FOR SICK CHILDREN

发明人： ROIFMAN, Chaim, M. ,  DEMIN, Peter ,  ROUNOVA, Olga ,  GRUNBERGER, Thomas ,  CIMPEAN, Octavian, Laurand

IPC分类号： C07C255/41 ,  C07C255/38 ,  C07C255/32 ,  C07D213/71 ,  A61P35/00

CPC分类号： A61K31/4402 ,  C07C255/41 ,  C07C323/46 ,  C07D213/71

摘要： Compounds having the Formula (I) or (III) wherein R1, R2 and R3 are each independently selected from H, OH, C1-6alkyl, C1-6alkoxy, NH2, NH-(Cl-6a1kyl), N(C1-6a1kyl)(C1-6alkyl), SH, S-C1-6alkyl, NO2, CF3, OCF3, and halo; R4 is unsubstituted Ar or Ar substituted with 1-4 substituents independently selected from C1-6alkyl, C1-6alkoxy and halo; X is selected from (CH2CH2O)n and (CH)n, and n = 1-4, salts, solvates and hydrates thereof, useful for modulating or inhibiting cell proliferation, are described.

摘要翻译： 其中R 1，R 2和R 3各自独立地选自H，OH，C 1-6烷基，C 1-6烷氧基，NH 2，NH-（C 1-6烷基），N（C 1-6烷基） （C 1-6烷基），SH，S-C 1-6烷基，NO 2，CF 3，OCF 3和卤素; R4是未取代的Ar或被1-4个独立选自C1-6烷基，C1-6烷氧基和卤素的取代基取代的Ar; 描述了用于调节或抑制细胞增殖的X选自（CH 2 CH 2 O）n和（CH）n，并且n = 1-4，其盐，溶剂化物和水合物。

公开(公告)号：EP1467967A1

公开(公告)日：2004-10-20

申请号：EP03700255.7

申请日：2003-01-17

申请人： The Hospital for Sick Children

发明人： ROIFMAN, Chaim, M. ,  DEMIN, Peter ,  GRUNBERGER, Thomas ,  ROUNOVA, Olga ,  CIMPEAN, Octavian Laurand

IPC分类号： C07C255/41 ,  C07C309/73 ,  A61K31/165

CPC分类号： C07C255/41 ,  C07C317/46 ,  C07D213/71

摘要： The following compounds of formulae (I) and (III) which may be useful in treating a variety of cell proliferative disorders are disclosed: Fomula (I), (II), wherein R1, R2 and R3 are each independently selected from H, OH, C1-6 alkyl, C1-6 alkoxy, NH2, NH-C1-6alkyl, N(C1-6 alkyl)(C1-6 alkyl), SH, S-C1-6 alkyl, NO2, CF3, OCF3 and halo; R4 is unsubstituted Ar, or Ar substituted with 1-4 substituents, independently selected from C1-6 alkyl, C1-6 alkoxy and halo; X is selected from (CH2CH2O)n and (CH2)n, and n=1-4.

公开(公告)号：EP1807386A1

公开(公告)日：2007-07-18

申请号：EP05784997.8

申请日：2005-09-14

申请人： THE HOSPITAL FOR SICK CHILDREN

发明人： ROIFMAN, Chaim ,  DEMIN, Peter ,  ROUNOVA, Olga ,  GRUNBERGER, Tom

IPC分类号： C07C235/34 ,  A61K31/165 ,  A61P35/00

CPC分类号： C07C235/34

摘要： There is described compounds of Formula (I), and salts, solvates and hydrates thereof wherein Formula (I): R1, R2 and R3 are each independently selected from OH, C1- 6alkyl, OC1- 6alkyl, OC(O)C1_6alkyl, C(O)OC1_6alkyl, NH2, NH-C1-6alkyl, N(C1-6alkyl)(C1-6alkyl), C(O)NHC1-6alkyl, C(O)N(C1-6alkyl)(C1-6alkyl), SH, SC1-6alkyl, NO2, CF3, OCF3 and halogen; and Ar is an aromatic or heteroaromatic group chosen from benzene, naphthalene, quinoline, isoquinoline, indole, pyridine, pyrasine, pyrimidine, imidazole, furan and thiophene, unsubstituted or substituted with 1-4 substituents independently selected from OH, C1-6alkyl, C1-6alkoxy, C1-3alkylenedioxy, NH2, NH­C1-6alkyl, N(C1-6alkyl)(C1-6alkyl), SH, S-C1-6alkyl, NO2, CF3, OCF3 and halogen. The compounds of Formula (I) are useful: in therapeutic methods and compositions for modulating cell proliferation, in diagnostic assays and as research tools.

公开(公告)号：EP1797064A1

公开(公告)日：2007-06-20

申请号：EP05786685.7

申请日：2005-09-14

申请人： THE HOSPITAL FOR SICK CHILDREN

发明人： ROIFMAN, Chaim ,  DEMIN, Peter ,  ROUNOVA, Olga ,  GRUNBERGER, Tom

IPC分类号： C07D333/24 ,  C07C255/29 ,  C07D307/16 ,  C07D211/60 ,  A61P35/00 ,  A61K31/38 ,  A61K31/34 ,  A61K31/44 ,  A61K31/275

CPC分类号： C07C255/41 ,  C07D213/40 ,  C07D213/57 ,  C07D307/54 ,  C07D333/24

摘要： There is described compounds of Formula (I), (II), (III), (IV) and (V), the salts, solvates, and hydrates thereof and pharmaceutical compositions comprising these compounds. In Formula (II), A is a ring chosen from pyridine, pyrazine, pyrimidine, imidazole, furan and thiophene. In Formula (IV), A is a ring chosen from benzene, pyridine, pyrazine, pyrimidine, imidazole, furan and thiophene (either substituted or unsubstituted) and B is a ring chosen from benzene and pyridine. The compounds of Formula (I), (II), (III), (IV) and (V) are useful in therapeutic methods and compositions for modulating and inhibiting cell proliferation, such as cancer cell proliferation, in diagnostic assays and as research tools.

摘要翻译： 描述了式（I），（II），（III），（IV）和（V）的化合物，其盐，溶剂合物和水合物以及包含这些化合物的药物组合物。 在式（II）中，A是选自吡啶，吡嗪，嘧啶，咪唑，呋喃和噻吩的环。 在式（IV）中，A是选自苯，吡啶，吡嗪，嘧啶，咪唑，呋喃和噻吩（取代或未取代的）的环，并且B是选自苯和吡啶的环。 式（I），（II），（III），（IV）和（V）的化合物可用于治疗方法和用于调节和抑制细胞增殖的组合物，例如癌症细胞增殖，诊断测定和研究工具 。