TS-1120(TS-1120) - 药物靶点：Aurora A_在研适应症：心血管疾病_专利_临床

概要

基本信息

药物类型

生物药

别名

yingwenbie-1121

靶点

Aurora A

作用方式

抑制剂

作用机制

Aurora A抑制剂(丝氨酸/苏氨酸蛋白激酶Aurora-A抑制剂)

治疗领域

心血管疾病

在研适应症

心血管疾病

非在研适应症-

原研机构

Pfizer Inc.

在研机构

Pfizer Japan, Inc.

非在研机构-

最高研发阶段批准上市

首次获批日期-

最高研发阶段(中国)-

特殊审评特殊审批 (中国)

登录后查看时间轴

关联

100 项与 TS-1120 相关的临床结果

登录后查看更多信息

100 项与 TS-1120 相关的转化医学

登录后查看更多信息

100 项与 TS-1120 相关的专利（医药）

登录后查看更多信息

1

项与 TS-1120 相关的文献（医药）

Nippon Kagaku Kaishi

Rotational isomerism in fluorene derivatives. 5. Restricted rotation around the C(11)-aryl single bond in 11-arylbenzo[a]fluorenes

作者: Kajigaeshi, Shoji ; Fujimoto, Minoru ; Fujisaki, Shizuo ; Fujii, Noriki ; Umeno, Masayuki

11-Arylbenzo[a]fluoren-11-ols I (R = 2-MeC₆H₄, 3-MeC₆H₄, 4-MeC₆H₄, 2-methyl-1-naphthyl, R¹ = OH) were prepared by treating benzo[a]fluorenone with arylmagnesium bromides or aryllithiums.Reduction of I (R¹ = OH) with HI-HOAc gave I (R¹ = H).Both rotational isomers, ap-form of I (R = 2-methyl-1-naphthyl, R¹ = OH, II) and 11R-, -sc (or 11S, + sc)-form of I (R = 2-methyl-1-naphthyl, R¹ = H) were stable crystals at room temperatureThe rotational barriers (ΔG^# = ∼19 kcal/mol) around the C_sp³-C_sp² single bond in I (R = 2-MeC₆H₄, R¹ = OH, III) were determined by NMR.Furthermore, the rates of isomerization for II ap → sp and III 11R, -sc (or 11S, +sc) → 11R, + ac (or 11S, -ac) were measured at various temperaturesThe free energies of activation for each process were ΔG^#_50s = 24.6 kcal/mol and ΔG^#_170° = 32.8 kcal/mol, resp.

100 项与 TS-1120 相关的药物交易

登录后查看更多信息