3,7-dimethyl-6-[2-(1,3,4,5-tetrahydro-8-hydroxy-2H-pyrido[4,3-b]indol-2-yl)ethyl ]-5H-thiazolo[3,2-a]pyrimidin-5-one | 221228-96-2

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 3,7-dimethyl-6-[2-(1,3,4,5-tetrahydro-8-hydroxy-2H-pyrido[4,3-b]indol-2-yl)ethyl ]-5H-thiazolo[3,2-a]pyrimidin-5-one
• 英文别名: 6-[2-(8-Hydroxy-1,3,4,5-tetrahydropyrido[4,3-b]indol-2-yl)ethyl]-3,7-dimethyl-[1,3]thiazolo[3,2-a]pyrimidin-5-one
• CAS: 221228-96-2
• 化学式: C₂₁H₂₂N₄O₂S
• 分子量: 394.497
• InChiKey: PBUGMXBGRQXEBI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  28
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  97.2
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• Tetrahydro gamma-carbolines
  申请人：——

  公开号：US20020103209A1

  公开（公告）日：2002-08-01

  The present invention concerns the compounds of formula 1 the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R 1 is hydrogen, optionally substituted C 1-6 alkyl, aryl; R 2 is each independently a halogen, hydroxy, C 1-6 alkyl, C 1-6 alkyloxy or nitro; n is 0, 1, 2 or 3; Alk is C 1-6 alkanediyl; D is an optionally substituted saturated or unsaturated nitrogen containing heterocycle; and aryl is optionally substituted phenyl; having a great therapeutic breadth. It further relates to their use as a medicine, their preparation as well as compositions containing them.

  本发明涉及公式1的化合物，其N-氧化物形式，药学上可接受的加盐形式和立体化学异构体形式，其中R1是氢，可选取代的C1-6烷基，芳基；R2各自独立地是卤素，羟基，C1-6烷基，C1-6烷氧基或硝基；n为0、1、2或3；Alk为C1-6烷基二亚基；D是可选的取代饱和或不饱和含氮杂环；芳基是可选的取代苯基；具有广泛的治疗范围。还涉及它们作为药物的用途，它们的制备以及含有它们的组合物。
• TETRAHYDRO GAMMA-CARBOLINES
  申请人：JANSSEN PHARMACEUTICA N.V.

  公开号：EP1015451A1

  公开（公告）日：2000-07-05
• US6303614B1
  申请人：——

  公开号：US6303614B1

  公开（公告）日：2001-10-16
• US6506768B2
  申请人：——

  公开号：US6506768B2

  公开（公告）日：2003-01-14
• [EN] TETRAHYDRO GAMMA-CARBOLINES<br/>[FR] TETRAHYDRO GAMMA-CARBOLINES
  申请人：JANSSEN PHARMACEUTICA N.V.

  公开号：WO1999012926A1

  公开（公告）日：1999-03-18

  (EN) The present invention concerns the compounds of formula (I), the $i(N)-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, optionally substituted C1-6alkyl, aryl; R2 is each independently a halogen, hydroxy, C1-6alkyl, C1-6alkyloxy or nitro; n is 0, 1, 2 ou 3; Alk is C1-6alkanediyl; D is optionally substituted saturated or unsaturated nitrogen containing heterocycle; and aryl is optionally substituted phenyl; having a great therapeutic breadth. It further relates to their use as a medecine, their preparation as well as compositions containing them.(FR) La présente invention concerne les composés de la formule (I), ainsi que leurs formes $i(N)-oxyde, leurs sels d'addition acceptables du point de vue pharmaceutique et leurs formes stéréoisomères; R1 représente un hydrogène, un alkyle en C1-6 éventuellement substitué, un aryle; R2 représente chacun indépendamment un halogène, un hydroxy, un alkyle en C1-6, un alkyloxy en C1-6 ou un nitro; n désigne 0, 1, 2 ou 3; Alk représente un alcanediyl en C1-6; D représente un azote éventuellement saturé ou non saturé contenant un hétérocycle; et aryle représente un phényle éventuellement substitué; les composés de la présente invention possèdent un large spectre thérapeutique. La présente invention concerne également l'utilisation de ces composés comme médicaments, leur préparation ainsi que les compositions les contenant.