公开(公告)号：US6130239A

公开(公告)日：2000-10-10

申请号：US464502

申请日：1999-12-15

申请人： Yi Chen ,  Wendy Lea Corbett ,  Apostolos Dermatakis ,  Jin-Jun Liu ,  Kin-Chun Luk ,  Paige E. Mahaney ,  Steven Gregory Mischke

发明人： Yi Chen ,  Wendy Lea Corbett ,  Apostolos Dermatakis ,  Jin-Jun Liu ,  Kin-Chun Luk ,  Paige E. Mahaney ,  Steven Gregory Mischke

IPC分类号： A61K31/404 ,  A61K31/4178 ,  A61K31/4409 ,  A61K31/454 ,  A61K31/5377 ,  A61P35/00 ,  A61P43/00 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D209/34

CPC分类号： C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14

摘要： Disclosed are novel 4-alkenyl- and 4-alkynyl oxindoles having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, a, b, and X are as defined herein. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer, more particularly, the treatment or control of breast and colon tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I and II as well as intermediates useful in the preparation of the compounds of formula I and II.

摘要翻译： 公开了具有下式的新的4-烯基 - 和4-炔基羟基吲哚及其药学上可接受的盐，其中R1，R2，R3，a，b和X如本文所定义。 这些化合物抑制细胞周期蛋白依赖性激酶（CDK），特别是CDK2。 这些化合物及其药学上可接受的盐和所述化合物的前药是可用于治疗或控制细胞增殖性疾病，特别是癌症的抗增殖剂，更特别是乳腺癌和结肠肿瘤的治疗或控制。 还公开了含有式I和II化合物的药物组合物以及可用于制备式I和II化合物的中间体。

公开(公告)号：US06307056B1

公开(公告)日：2001-10-23

申请号：US09464466

申请日：1999-12-15

申请人： Wendy Lea Corbett ,  Kin-Chun Luk ,  Paige E. Mahaney

发明人： Wendy Lea Corbett ,  Kin-Chun Luk ,  Paige E. Mahaney

IPC分类号： C07D40302

CPC分类号： C07D409/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14

摘要： Disclosed are 4-aryloxindoles that inhibit or modulate protein kinases, in particular JNK protein kinases. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are useful as anti-inflammatory agents, particularly useful in the treatment of rheumatoid arthritis. Also disclosed are pharmaceutical compositions containing the foregoing compounds, as well as methods for the treatment and/or control of inflammation, particularly in the treatment or control of rheumatoid arthritis, using said compounds.

摘要翻译： 公开了抑制或调节蛋白激酶，特别是JNK蛋白激酶的4-芳氧基吲哚。 这些化合物及其药学上可接受的盐和所述化合物的前药可用作抗炎剂，特别可用于治疗类风湿性关节炎。 还公开了含有前述化合物的药物组合物，以及使用所述化合物治疗和/或控制炎症，特别是治疗或控制类风湿性关节炎的方法。

公开(公告)号：US06313310B1

公开(公告)日：2001-11-06

申请号：US09464238

申请日：1999-12-15

申请人： Kin-Chun Luk ,  Paige E. Mahaney ,  Steven Gregory Mischke

发明人： Kin-Chun Luk ,  Paige E. Mahaney ,  Steven Gregory Mischke

IPC分类号： C07D40302

CPC分类号： C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14

摘要： Disclosed are 4- and 5-alkynyloxindoles as well as 4- and 5-alkenyloxindoles that inhibit or modulate protein kinases, in particular JNK protein kinases. The compounds of the invention and their pharmaceutically acceptable salts, and prodrugs of said compounds, are useful as anti-inflammatory agents, particularly useful in the treatment of rheumatoid arthritis. Also disclosed are pharmaceutical compositions containing the foregoing compounds, methods for the treatment and/or control of inflammation, particularly in the treatment or control of rheumatoid arthritis using these compounds, as well as intermediates useful in the preparation of compounds of the invention.

摘要翻译： 公开了抑制或调节蛋白激酶，特别是JNK蛋白激酶的4-和5-炔氧基吲哚以及4-和5-链烯氧基吲哚。 本发明的化合物及其药学上可接受的盐和所述化合物的前药可用作抗炎剂，特别可用于治疗类风湿性关节炎。 还公开了含有前述化合物的药物组合物，用于治疗和/或控制炎症的方法，特别是在使用这些化合物治疗或控制类风湿性关节炎的药物组合物中，以及可用于制备本发明化合物的中间体。