8-methoxy-3-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-amine | 919099-10-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 英文名称: 8-methoxy-3-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-amine
• 英文别名: 8-methoxy-3-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-ylamine；7-Methoxy-3-methyl-1,2,4,5-tetrahydro-3-benzazepin-8-amine
• CAS: 919099-10-8
• 化学式: C₁₂H₁₈N₂O
• 分子量: 206.288
• InChiKey: VXAMFYMGRJDMFU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  38.5
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• [EN] ANILINOPYRIMIDINES AS HAEMATOPOIETIC PROGENITOR KINASE 1 (HPK1) INHIBITORS<br/>[FR] ANILINOPYRIMIDINES EN TANT QU'INHIBITEURS DE KINASE 1 PROGÉNITRICES HÉMATOPOÏÉTIQUES (HPK1)
  申请人：ARIAD PHARMA INC

  公开号：WO2018102366A1

  公开（公告）日：2018-06-07

  The invention relates to HPK1 inhibitors useful in the treatment of cancers, and other serine-threonine kinase mediated diseases, having the Formula: where A, R1, R2, R3, R4, R5, R6, R16, R17, X1, X2, X3, X4, m, and n are described herein.

  这项发明涉及用于治疗癌症和其他丝氨酸-苏氨酸激酶介导的疾病的HPK1抑制剂，其化学式为：其中A、R1、R2、R3、R4、R5、R6、R16、R17、X1、X2、X3、X4、m和n如本文所述。
• SUBSTITUTED GLYCINAMIDES, PROCESS FOR THEIR MANUFACTURE AND USE THEREOF AS MEDICAMENTS
  申请人：Priepke Henning

  公开号：US20100216769A1

  公开（公告）日：2010-08-26

  The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R 3 , R 4 and R 5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.

  本发明涉及一般式(I)的新取代甘氨酰胺，其中D、M、R3、R4和R5如规范中定义，其互变异构体、对映异构体、非对映异构体、混合物以及其盐，特别是其与无机或有机酸或碱形成的生理上可接受的盐，具有有价值的特性。
• Sulfonamide derivatives as antipsychotic agents
  申请人：Forbes Thomson Ian

  公开号：US20060063757A1

  公开（公告）日：2006-03-23

  The invention provides compounds of formula (I): wherein A and B represent the groups —(CH 2 ) m — and —(CH 2 ) n — respectively; R 1 represents hydrogen or C 1-6 alkyl; R 2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC 1-6 alkyl, trifluoromethyl, trifluoromethoxy, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 fluoroalkoxy, —(CH 2 ) p C 3-6 cycloalkyl, —(CH 2 ) p OC 3-6 cycloalkyl, —COC -6 alkyl, —SO 2 C 1-6 alkyl, —SOC 1-6 alkyl, —S—C 1-6 alkyl, —CO 2 C 1-6 alkyl, —CO 2 NR 5 R 6 , —SO 2 NR 5 R 6 , —(CH 2 )NR 5 R 6 , —(CH 2 ) p NR 5 COR 6 , optionally substituted aryl ring, optionally substituted heteroaryl ring or optionally substituted heterocyclyl ring; R 3 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC 1-6 alkyl, trifluoromethyl, trifluoromethoxy, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 fluoroalkoxy, —(CH 2 ) p C 3-6 cycloalkyl, —(CH 2 ) p OC 3-6 cycloalkyl, —COC 1-6 alkyl, —SO 2 C 1-6 alkyl, —SOC 1-6 alkyl, —S—C 1-6 alkyl, —CO 2 C 1-6 alkyl, —CO 2 NR 7 R 8 , —SO 2 NR 7 R 8 , —(CH 2 ) p NR 7 R 8 or —(CH 2 ) p NR 7 COR 8 ; R 4 represents hydrogen, hydroxy, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 fluoroalkoxy, trifluoromethyl, trifluoromethoxy, halogen, —OSO 2 CF 3 , —(CH 2 ) p C 3-6 cycloalkyl, —(CH 2 ) q OC 1-6 alkyl or —(CH 2 ) p OC 3-6 cycloalkyl; R 5 and R 6 each independently represent hydrogen, C 1-6 alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalkyl ring or an oxo-substituted azacycloalkyl ring; R 7 and R 8 each independently represent hydrogen or C 1-6 alkyl; m and n independently represent an integer selected from 1 and 2; p independently represents an integer selected from 0, 1, 2 and 3; q independently represents an integer selected from 1, 2 and 3; or a pharmaceutically acceptable salt or solvate thereof, with the proviso that the compounds 8-hydroxy-3-methyl-7-phenylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine, 8-hydroxy-7-4-(hydroxyphenyl)sulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine, 7-phenylsulfonyl- 1,2,3,4-tetrahydroisoquinoline and 7-phenylsulfonyl-1,2,3,4-tetrahydroisoquinoline hydrochloride are excluded. The compounds are useful in therapy, in particular as antipsychotic agents

  该发明提供了式（I）的化合物：其中A和B分别表示基团—（CH2）m—和—（ ）n—；R1表示氢或C1-6烷基；R2表示氢、卤素、羟基、氰基、硝基、羟基C1-6烷基、三氟甲基、三氟甲氧基、C1-6烷基、C1-6烷氧基、C1-6氟烷氧基、—（ ）pC3-6环烷基、—（ ）pOC3-6环烷基、—COC-6烷基、—SO2C1-6烷基、—SOC1-6烷基、—S—C1-6烷基、—CO2C1-6烷基、—CO2NR5R6、—SO2NR5R6、—（ ）NR5R6、—（ ）pNR5COR6、可选取代的芳香环、可选取代的杂芳环或可选取代的杂环基；R3表示氢、卤素、羟基、氰基、硝基、羟基C1-6烷基、三氟甲基、三氟甲氧基、C1-6烷基、C1-6烷氧基、C1-6氟烷氧基、—（ ）pC3-6环烷基、—（ ）pOC3-6环烷基、—COC1-6烷基、—SO2C1-6烷基、—SOC1-6烷基、—S—C1-6烷基、—CO2C1-6烷基、—CO2NR7R8、—SO2NR7R8、—（ ）pNR7R8或—（ ）pNR7COR8；R4表示氢、羟基、C1-6烷基、C1-6烷氧基、C1-6氟烷氧基、三氟甲基、三氟甲氧基、卤素、—OSO2CF3、—（ ）pC3-6环烷基、—（ ）qOC1-6烷基或—（ ）pOC3-6环烷基；R5和R6分别独立地表示氢、C1-6烷基或与它们所连接的氮或其他原子一起形成氮杂环烷基环或氧代取代的氮杂环烷基环；R7和R8分别独立地表示氢或C1-6烷基；m和n独立地表示选自1和2的整数；p独立地表示选自0、1、2和3的整数；q独立地表示选自1、2和3的整数；或其药学上可接受的盐或溶剂，但排除8-羟基-3-甲基-7-苯基磺酰基-2,3,4,5-四氢-1H-3-苯并噁唑、8-羟基-7-4-（羟基苯基）磺酰基-2,3,4,5-四氢-1H-3-苯并噁唑、7-苯基磺酰基-1,2,3,4-四氢异喹啉和7-苯基磺酰基-1,2,3,4-四氢异喹啉盐酸盐。这些化合物在治疗中有用，特别是作为抗精神病药物。
• FUSED BICYCLIC DERIVATIVES OF 2,4-DIAMINOPYRIMIDINE AS ALK AND c-MET INHIBITORS
  申请人：Ahmed Gulzar

  公开号：US20090221555A1

  公开（公告）日：2009-09-03

  The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , A 1 , A 2 , A 3 , A 4 , and A 5 , are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.

  本发明提供公式I或II化合物或其药学上可接受的盐形式，其中R1、R2、R3、R4、R5、A1、A2、A3、A4和A5如本文所定义。公式I或II化合物具有ALK和/或c-Met抑制活性，可用于治疗增殖性疾病。
• NEW SUBSTITUTED GLYCINAMIDES, PROCESS FOR THEIR MANUFACTURE AND USE THEREOF AS MEDICAMENTS
  申请人：PRIEPKE Henning

  公开号：US20130184256A1

  公开（公告）日：2013-07-18

  The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R 3 , R 4 and R 5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.

  本发明涉及一种新的取代的甘氨酰胺，其一般式为（I），其中D、M、R3、R4和R5如规范中所定义，其互变异构体、对映异构体、顺反异构体、混合物和盐，特别是与无机或有机酸或碱的生理上可接受的盐，具有有价值的性质。