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标题翻译： 4-氨基噻唑衍生物，它们的制备及其作为依赖于细胞周期蛋白依赖性激酶的抑制剂的用途

公开(公告)号：WO9921845A2

公开(公告)日：1999-05-06

申请号：PCT/US9822809

申请日：1998-10-27

申请人： AGOURON PHARMA , CHONG WESLEY K M , CHU SHAO SONG , DUVADIE ROHIT R , LI LIN , XIAO WEI , YANG YI

发明人： CHONG WESLEY K M , CHU SHAO SONG , DUVADIE ROHIT R , LI LIN , XIAO WEI , YANG YI

IPC分类号： C07D277/20 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/551 , A61P35/00 , A61P43/00 , C07D213/00 , C07D235/00 , C07D277/42 , C07D277/56 , C07D333/00 , C07D417/06 , C07D417/12 , C07D417/14 , C07D521/00 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/50

CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/42 , C07D417/06 , C07D417/12 , C07D417/14

摘要： This invention is directed to aminothiazole compounds of formula (I) wherein R is a substituted or unsubstituted group selected from: C1-6-alkyl; C1-6-alkenyl; C1-6-alkynyl; C1-6-alkoxyl; C1-6-alcohol; carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, cycloalkyl; carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, aryl; carbonyl; ether; (C1-6-alkyl)-carbonyl; (C1-6-alkyl)-aryl; (C1-6-alkyl)-cycloalkyl; (C1-6-alkyl)-(C1-6-alkoxyl); aryl-(C1-6-alkoxyl); thioether; thiol; and sulfonyl; wherein when R is substituted, each substituent independently is a halogen; haloalkyl; C1-6-alkyl; C1-6-alkenyl; C1-6-alkynyl; hydroxyl; C1-6-alkoxyl; amino; nitro; thiol; thioether; imine; cyano; amido; phosphonato; phosphine; carboxyl; thiocarbonyl; sulfonyl; sulfonamide; ketone; aldehyde; ester; oxygen; carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, cycloalkyl; or carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, aryl; and R is a carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, ring structure having a substituent at the position adjacent to the point of attachment, which ring structure is optionally further substituted, where each substituent of R independently is a halogen; haloalkyl; C1-6-alkyl; C1-6-alkenyl; C1-6-alkynyl; hydroxyl; C1-6-alkoxyl; amino; nitro; thiol; thioether; imine; cyano; amido; phosphonato; phosphine; carboxyl; thiocarbonyl; sulfonyl; sulfonamide; ketone; aldehyde; ester; oxygen; carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, cycloalkyl; or carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, aryl; or a pharmaceutically acceptable salt of a compound of formula (I), or a prodrug or pharmaceutically active metabolite of a compound of formula (I) or pharmaceutically acceptable salt thereof, for inhibiting cyclin-dependent kinases (CDKs), such as CDK1, CDK2, CDK4, and CDK6. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds and to methods of treating malignancies and other disorders by administering effective amounts of such compounds.

摘要翻译：本发明涉及式（I）的氨基噻唑化合物，其中R 1是取代或未取代的选自以下的基团：C 1-6 - 烷基; C 1-6 - 链烯基; C 1-6 - 炔基; C 1-6 - 烷氧基取代; C 1-6 - 醇; 碳环或杂环，单环或稠合或非稠合多环，环烷基; 碳环或杂环，单环或稠合或非稠合多环，芳基; 羰; 醚; （C 1-6 - 烷基）羰基; （C 1-6 - 烷基） - 芳基; （C 1-6 - 烷基） - 环烷基; （C 1-6 - 烷基） - （C 1-6 - 烷氧基）; 芳基 - （C 1-6 - 烷氧基）; 硫醚; 巯基; 和磺酰基; 其中当R 1被取代时，每个取代基独立地为卤素; 卤代; C 1-6 - 烷基; C 1-6 - 链烯基; C 1-6 - 炔基; 羟; C 1-6 - 烷氧基取代; 氨基; 硝基; 巯基; 硫醚; 亚胺; 氰基; 酰胺基; 膦酸; 膦; 羧基; 硫代羰基; 磺酰基; 磺胺; 酮; 醛; 酯; 氧; 碳环或杂环，单环或稠合或非稠合多环，环烷基; 或碳环或杂环，单环或稠合或非稠合的多环芳基; 并且R 2是碳环或杂环的单环或稠合或非稠合的多环环结构，其在与连接点相邻的位置上具有取代基，该环结构任选进一步被取代，其中R 2的每个取代基 >独立地为卤素; 卤代; C 1-6 - 烷基; C 1-6 - 链烯基; C 1-6 - 炔基; 羟; C 1-6 - 烷氧基取代; 氨基; 硝基; 巯基; 硫醚; 亚胺; 氰基; 酰胺基; 膦酸; 膦; 羧基; 硫代羰基; 磺酰基; 磺胺; 酮; 醛; 酯; 氧; 碳环或杂环，单环或稠合或非稠合多环，环烷基; 或碳环或杂环，单环或稠合或非稠合的多环芳基; 或式（I）化合物的药学上可接受的盐，或式（I）化合物或其药学上可接受的盐的前药或药学活性代谢物用于抑制细胞周期蛋白依赖性激酶（CDK）如CDK1，CDK2 ，CDK4和CDK6。本发明还涉及含有这些化合物的药物组合物的治疗或预防用途以及通过施用有效量的这些化合物治疗恶性肿瘤和其他病症的方法。

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