2,2-dimethyl-N-[[4-pyridin-3-yl-2-[3-(trifluoromethyl)anilino]-1,3-thiazol-5-yl]methyl]propanamide | 929561-99-9

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 2,2-dimethyl-N-[[4-pyridin-3-yl-2-[3-(trifluoromethyl)anilino]-1,3-thiazol-5-yl]methyl]propanamide
• CAS: 929561-99-9
• 化学式: C₂₁H₂₁F₃N₄OS
• 分子量: 434.485
• InChiKey: GVPMGAGCHOGONR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  30
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  95.2
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• 2-ANILINE-4-ARYL SUBSTITUTED THIAZOLE DERIVATIVES
  申请人：Thuring Johannes Wilhelmus John F.

  公开号：US20110269748A1

  公开（公告）日：2011-11-03

  This invention concerns the use of a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is hydrogen, halo, C 1-6 alkyl, Het 1 , HO—C 1-6 alkyl-, cyano-C 1-6 alkyl-, amino-C(═O)—C 1-6 alkyl-, formylamino-C 1-6 alkyl-, C 1-6 alkyl-C(═O)—NH—C 1-6 alkyl-, mono- or di(C 1-6 alkyl)amino-C(═O)—C 1-6 alkyl-, phenyl-C 1-6 alkyl-, or Het 4 -C 1-6 alkyl-; Q is phenyl, pyridyl, benzofuranyl, 2,3-dihydro-benzofuranyl, pyrazolyl, isoxazolyl or indazolyl wherein each of said ring systems is optionally being substituted with up to three substituents each independently selected from halo, cyano, C 1-6 alkyl, C 1-6 alkyl-O—, C 1-6 alkylthio, Ar or polyhaloC 1-6 alkyl; L is phenyl, pyridyl, pyrimidazolyl, 8-Azapyrimidazolyl, pyridazinyl, imidazothiazolyl or furanyl wherein each of said ring systems may optionally be substituted with one or two or more substituents, each substituent independently being selected from halo, hydroxy, amino, cyano, C 1-6 alkyl or C 1-6 alkyl-O—; Het 1 represents morpholinyl; pyrazolyl or imidazolyl; Het 4 represents morpholinyl, pyrazolyl or imidazolyl; Ar represents phenyl optionally substituted with halo, C 1-6 alkyl, C 1-6 alkyl-O— or polyhaloC 1-6 alkyl; for the manufacture of a medicament for the prevention or the treatment or prophylaxis of psychotic disorders, intellectual impairment disorders or diseases or conditions in which modulation of the α7 nicotinic receptor is beneficial.

  这项发明涉及使用式(I)中的化合物，其中N-氧化物是药用可接受的加合盐，季铵基和其立体化异构形式，其中Z为氢、卤素、C1-6烷基、Het1、HO—C1-6烷基、氰基-C1-6烷基、氨基-C(═O)—C1-6烷基、甲酰氨基-C1-6烷基、C1-6烷基-C(═O)—NH—C1-6烷基、单烷基或二烷基胺基-C(═O)—C1-6烷基、苯基-C1-6烷基或Het4-C1-6烷基；Q为苯基、吡啶基、苯并呋喃基、2,3-二氢苯并呋喃基、吡唑基、异噁唑基或吲唑基，其中每个环系统可选地被取代，每个取代基可独立地选择自卤素、氰基、C1-6烷基、C1-6烷基-O—、C1-6烷基硫醚、Ar或多卤代C1-6烷基；L为苯基、吡啶基、嘧啶嗪基、8-吡啉嗪基、吡啶嗪基、咪唑噻唑基或呋喃基，其中每个环系统可选地被取代，每个取代基可独立地选择自卤素、羟基、氨基、氰基、C1-6烷基或C1-6烷基-O—；Het1代表吗啉基；吡唑基或咪唑基；Het4代表吗啉基、吡唑基或咪唑基；Ar代表苯基，可选地被卤素、C1-6烷基、C1-6烷基-O—或多卤代C1-6烷基取代；用于制备一种用于预防或治疗或预防精神障碍、智力障碍或调节α7尼古丁受体有益的疾病或情况的药物。
• US9388175B2
  申请人：——

  公开号：US9388175B2

  公开（公告）日：2016-07-12