1,1-dimethylethyl 7-(methyloxy)-1,2,4,5-tetrahydro-3H-3-benzazepine-3-carboxylate | 583025-99-4

• 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: 1,1-dimethylethyl 7-(methyloxy)-1,2,4,5-tetrahydro-3H-3-benzazepine-3-carboxylate
• 英文别名: 7-methoxy-1,2, 4, 5-tetrahydro-benzo[d]azepine-3-carboxylic acid tert-butyl ester；7-Methoxy-1,2,4,5-tetrahydro-3-benzazepine-3-carboxylic acid tert-butyl ester；tert-butyl 7-methoxy-1,2,4,5-tetrahydro-3-benzazepine-3-carboxylate
• CAS: 583025-99-4
• 化学式: C₁₆H₂₃NO₃
• 分子量: 277.364
• InChiKey: VVHJRAQXANZXBL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  38.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1,1-dimethylethyl 7-(methyloxy)-1,2,4,5-tetrahydro-3H-3-benzazepine-3-carboxylate 在 硝酸 、 乙酸酐 作用下， 生成 tert-butyl 7-methoxy-8-nitro-1,2,4,5-tetrahydro-3H-benzo[d]azepine-3-carboxylate
  参考文献：
  名称：

  [EN] DOPAMINE RECEPTOR MODULATORS AS ANTIPSYCHOTIC AGENTS
  [FR] MODULATEURS DES RECEPTEURS DE DOPAMINE UTILISES COMME AGENTS ANTIPSYCHOTIQUES

  摘要：

  该发明提供了以下化合物的结构（I）： 其中A和B分别代表基团-(CH2)m-和-(CH2)n-；R1代表氢或C1-6烷基；R2代表氢、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、-(CH2)pC3-6环烷基、-(CH2)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、-(CH2)pNR7R8、-(CH2)pNR7COR8、可选择地取代的芳基、可选择地取代的杂芳基或可选择地取代的杂环烷基；R3代表氢或C1-6烷基；R4代表可选择地取代的芳基或可选择地取代的杂芳基；R5和R6分别独立地代表氢、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、-(CH2)pC3-6环烷基、-(CH2)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、-(CH2)pNR7R8、-(CH2)pNR7COR8、可选择地取代的芳基、可选择地取代的杂芳基或可选择地取代的杂环烷基；R7和R8分别独立地代表氢、C1-6烷基或与它们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；m和n分别独立地代表1和2中选择的整数；p独立地代表0、1、2和3中选择的整数；并且：Z代表-CR9R10X-或-XCR9R10-，X代表氧、硫、-SO-或-SO2，或Z代表-CONR11-或-NR9CO-，X代表-CH2-、氧、硫、-SO-或-SO2；R9和R10分别独立地代表氢、C1-6烷基或氟代基；R11代表氢或C1-6烷基；或其药学上可接受的盐或溶剂。该发明的化合物在治疗中特别作为抗精神病药物具有用途。

  公开号：

  WO2003095428A1
• 作为产物：
  描述：

  7-羟基-4,5-二氢-1H-苯并[d]氮杂卓-3(2H)-羧酸叔丁酯 在 K₂CO₃ 、 碘甲烷 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 1,1-dimethylethyl 7-(methyloxy)-1,2,4,5-tetrahydro-3H-3-benzazepine-3-carboxylate
  参考文献：
  名称：

  [EN] SULFONAMIDE DERIVATIVES AS ANTIPSYCHOTIC AGENTS
  [FR] DERIVES DE SULFONAMIDE UTILISES COMME AGENTS ANTIPSYCHOTIQUES

  摘要：

  该发明提供了以下结构的化合物（I），其中A和B分别代表基团-(CH2)m-和-(CH2)n-；R1代表C1-6烷基；R2代表氢、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、-(CH2)pC3-6环烷基、-(CH2)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、-CO2NR4R5、-SO2NR4R5、-(CH2)pNR4R5、-(CH2)pNR4COR5、一个可选择取代的芳基、一个可选择取代的杂芳基或一个可选择取代的杂环烷基；R3代表氢或C1-6烷基；Ar1代表一个可选择取代的杂芳基；Ar2代表一个可选择取代的苯基或一个可选择取代的杂芳基；Y代表一个键、-O-、-C1-6烷基-、-CR6R7X-、-XCR6R7-、-NR8CO-或-CONR8-；X代表氧、硫、-SO-或-SO2-；R4和R5分别独立地代表氢或C1-6烷基，或者与它们连接的氮或其他原子一起形成一个氮杂环烷基环或一个氧代取代的氮杂环烷基环；R6和R7分别独立地代表氢、C1-6烷基或氟；R8代表氢或C1-6烷基；m和n独立地代表从1和2中选择的整数；p独立地代表从0、1、2和3中选择的整数；或其药学上可接受的盐、溶剂或药学上可接受的衍生物。这些化合物在治疗中很有用，特别是作为抗精神病药物。

  公开号：

  WO2004031181A1

文献信息

• [EN] DOPAMINE RECEPTOR MODULATORS AS ANTIPSYCHOTIC AGENTS<br/>[FR] MODULATEURS DES RECEPTEURS DE DOPAMINE UTILISES COMME AGENTS ANTIPSYCHOTIQUES
  申请人：GLAXO GROUP LTD

  公开号：WO2003095428A1

  公开（公告）日：2003-11-20

  The invention provides compounds of formula (I):wherein A and B represent the groups -(CH2)m- and -(CH2)n-respectively; R1 represents hydrogen or C1-6alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, -(CH2)pC3-6cycloalkyl, -(CH2)pOC3-6cycloalkyl, -COC1-6alkyl, -SO2C1-6alkyl, -SOC1-6alkyl, -S-C1-6alkyl, -CO2C1-6alkyl, -CO2NR7R8, -SO2NR7R8, -(CH2)pNR7R8, -(CH2)pNR7COR8, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocyclyl; R3 represents hydrogen or C1-6alkyl; R4 represents optionally substituted aryl or optionally substituted heteroaryl; R5 and R6 each independently represent hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, -(CH2)pC3-6cycloalkyl, -(CH2)pOC3-6cycloalkyl, -COC1-6alkyl, -SO2C1-6alkyl, -SOC1-6alkyl, -S-C1-6alkyl, -CO2C1-6alkyl, -CO2NR7R8, -SO2NR7R8, -(CH2)pNR7R8, -(CH2)pNR7COR8, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocyclyl; R7 and R8 each independently represent hydrogen, C1-6alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalkyl ring or an oxo-substituted azacycloalkyl ring; m and n independently represent an integer selected from 1 and 2; p independently represents an integer selected from 0, 1, 2 and 3; and either: Z represents -CR9R10X- or -XCR9R10- and X represents oxygen, sulfur, -SO- or -SO2, or Z represents -CONR11- or -NR9CO- and X represents -CH2-, oxygen, sulfur, -SO- or -SO2; R9 and R10 each independently represent hydrogen, C1-6alkyl or fluoro; R11 represents hydrogen or C1-6alkyl;or a pharmaceutically acceptable salt or solvate thereof.The compounds of the invention are useful in therapy, in particular as antipsychotic agents.

  该发明提供了以下化合物的结构（I）： 其中A和B分别代表基团-(CH2)m-和-(CH2)n-；R1代表氢或C1-6烷基；R2代表氢、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、-(CH2)pC3-6环烷基、-(CH2)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、-(CH2)pNR7R8、-(CH2)pNR7COR8、可选择地取代的芳基、可选择地取代的杂芳基或可选择地取代的杂环烷基；R3代表氢或C1-6烷基；R4代表可选择地取代的芳基或可选择地取代的杂芳基；R5和R6分别独立地代表氢、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、-(CH2)pC3-6环烷基、-(CH2)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、-(CH2)pNR7R8、-(CH2)pNR7COR8、可选择地取代的芳基、可选择地取代的杂芳基或可选择地取代的杂环烷基；R7和R8分别独立地代表氢、C1-6烷基或与它们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；m和n分别独立地代表1和2中选择的整数；p独立地代表0、1、2和3中选择的整数；并且：Z代表-CR9R10X-或-XCR9R10-，X代表氧、硫、-SO-或-SO2，或Z代表-CONR11-或-NR9CO-，X代表-CH2-、氧、硫、-SO-或-SO2；R9和R10分别独立地代表氢、C1-6烷基或氟代基；R11代表氢或C1-6烷基；或其药学上可接受的盐或溶剂。该发明的化合物在治疗中特别作为抗精神病药物具有用途。
• Benzenesulfonamide derivatives as antipsychotic agents
  申请人：Bromidge Mark Steven

  公开号：US20050222124A1

  公开（公告）日：2005-10-06

  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 alkoxyC 1-6 alkyl, C 3-7 cycloalkylC 1-6 alkoxy, —(CH 2 ) p C 3-6 cycloalkyl, —(CH 2 ) p C 3-6 cycloalkyloxy, —COC 1-6 alkyl, —SO 2 C 1-6 alkyl, —SOC 1-6 alkyl, —S—C 1-6 alkyl, C 1-6 alkylsulfonyloxy, C 1-6 alkylsulfonylC 1-6 alkyl, —CO 2 C 1-6 alkyl, —CO 2 NR 7 R 8 , —SO 2 NR 7 R 8 , C 1-6 alkylsulfonamido, C 1-6 alkylsulfonamidoC 1-6 alkyl, —(CH 2 ) p NR 7 R 8 , C 1-6 alkylamidoC 1-6 alkyl, —(CH 2 ) p NR 7 COR 8 , arylsulfonyl, arylsulfonyloxy, arylsulfonylC 1-6 alkyl, arylsulfonamido, arylcarboxamido, arylsulfonamidoC 1-6 alkyl, arylcarboxamidoC 1-6 alkyl, aroyl, aroylC 1-6 alkyl, arylC 1-6 alkanoyl, —SO 2 NR 7 R 8 , optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocyclyl, or a group CONR 7 R 8 or SO 2 NR 7 R 8 wherein R 7 and R 8 together may be fused to form a 5- 7-membered aromatic or non-aromatic heterocyclic ring optionally interrupted by an O or S atom; R 3 represents hydrogen or C 1-6 alkyl; Ar represents optionally substituted phenyl or optionally substituted monocyclic heteroaryl group; R 4 represents optionally substituted aryl or optionally substituted heteroaryl; R 7 and R 8 each independently represent hydrogen, C 1-6 alkyl or together form a 5- to 7-membered heterocyclic ring; Z represents a bond, an oxygen atom or C 1-6 alkyl; Y represents 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 represents an integer from 1 to 3; r represents an integer from 1 to 4; or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful in therapy, in particular as antipsychotic agents.

  本发明提供了化合物的公式（I），其中A和B分别表示基团—（CH2）m-和—（CH2）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烷氧基C1-6烷基、C3-7环烷基C1-6烷氧基、—（CH2）pC3-6环烷基、—（CH2）pC3-6环烷氧基、—COC1-6烷基、—SO2C1-6烷基、—SOC1-6烷基、—S—C1-6烷基、C1-6烷基磺酰氧基、C1-6烷基磺酰C1-6烷基、—CO2C1-6烷基、—CO2NR7R8、—SO2NR7R8、C1-6烷基磺酰胺基、C1-6烷基磺酰胺基C1-6烷基、—（CH2）pNR7R8、C1-6烷基酰胺基C1-6烷基、—（CH2）pNR7COR8、芳基磺酰基、芳基磺酰氧基、芳基磺酰C1-6烷基、芳基磺酰胺基、芳基羧酰胺基、芳基磺酰胺基C1-6烷基、芳基羧酰胺基C1-6烷基、芳基、芳基C1-6酰基、—SO2NR7R8、可选择取代的芳基、可选择取代的杂芳基或可选择取代的杂环基，或者是一个CONR7R8或SO2NR7R8基团，其中R7和R8可以共轭形成一个5-7成员的芳香族或非芳香族杂环，该杂环可以被O或S原子打断；R3表示氢或C1-6烷基；Ar表示可选择取代的苯基或可选择取代的单环杂芳基；R4表示可选择取代的芳基或可选择取代的杂芳基；R7和R8各自独立地表示氢、C1-6烷基或共同形成一个5-7成员的杂环；Z表示键，氧原子或C1-6烷基；Y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表示1至3的整数；r表示1至4的整数；或其药学上可接受的盐或溶剂。这些化合物在治疗中有用，特别是作为抗精神病药物。
• Benzenesulfonamide derivatives
  申请人：Cooper G David

  公开号：US20050085461A1

  公开（公告）日：2005-04-21

  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 1-4 alkyl; R 2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC 1-6 alkyl, trifluoromethyl, trifluoromethoxy, C 1-6 alkyl, C 1-6 alkoxy, —(CH 2 ) p C 3-6 cycloalkyl, —(CH 2 ) p C 3-6 cycloalkyloxy, —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 , —(CH 2 ) p NR 7 COR 8 , optionally substituted aryl, optionally substituted heteroaryl or a fused bicyclic heterocyclic ring system; R 3 represents hydrogen or C 1-6 alkyl; R 4 represents halogen, trifluoromethyl, trifluoromethoxy, C 1-6 alkyl, C 1-6 alkoxy, —(CH 2 ) p C 3-6 cycloalkyl or —(CH 2 ) p C 3-6 cycloalkyloxy; R 5 and R 6 each independently represent hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC 1-6 alkyl, trifluoromethyl, trifluoromethoxy, C 1-6 alkyl, C 1-6 alkoxy, —(CH 2 ) p C 3-6 cycloalkyl, —(CH 2 ) p C 3-6 cycloalkyloxy, —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 , —(CH 2 ) p NR 7 COR 8 , optionally substituted aryl, optionally substituted heteroaryl or a fused bicyclic heterocyclic ring system; 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; or a pharmaceutically acceptable salt or solvate thereof, with the proviso that the compounds 4-methyl-N-(1,2,3,4-tetrahydroisoquinolin-6-yl)-benzenesulfonamide, 7-(4-chlorophenyl)sulfonamido-1,2,3,4-tetrahydroisoquinoline hydrochloride and N-(2-ethyl-5-isoindolinyl)-p-toluenesulfonamide 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分别代表基团CH2）m-和CH2）n-; R1代表氢或C1-4烷基; R2代表氢，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， -（CH2）pC3-6环烷基， -（CH2）pC3-6环烷氧基， -COC1-6烷基， -SO2C1-6烷基， -SOC1-6烷基， -S-C1-6烷基， -CO2C1-6烷基， -CO2NR7R8， -SO2NR7R8， -（CH2）pNR7R8， -（CH2）pNR7COR8，可选地取代的芳基，可选地取代的杂环芳基或融合的双环杂环环系; R3代表氢或C1-6烷基; R4代表卤素，三氟甲基，三氟甲氧基，C1-6烷基，C1-6烷氧基， -（CH2）pC3-6环烷基或 -（CH2）pC3-6环烷氧基; R5和R6各自独立地代表氢，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， -（CH2）pC3-6环烷基， -（CH2）pC3-6环烷氧基， -COC1-6烷基， -SO2C1-6烷基， -SOC1-6烷基， -S-C1-6烷基， -CO2C1-6烷基， -CO2NR7R8， -SO2NR7R8， -（CH2）pNR7R8， -（CH2）pNR7COR8，可选地取代的芳基，可选地取代的杂环芳基或融合的双环杂环环系; R7和R8各自独立地代表氢或C1-6烷基; m和n各自独立地代表选自1和2的整数; p独立地代表选自0、1、2和3的整数; 或其药学上可接受的盐或溶剂，但不包括4-甲基-N-（1,2,3,4-四氢异喹啉-6-基）-苯磺酰胺，7-（4-氯苯基）磺酰胺-1,2,3,4-四氢异喹啉盐酸盐和N-（2-乙基-5-异吲哚基）-对甲苯磺酰胺。该化合物在治疗中有用，特别是作为抗精神病药物。
• 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—（CH2）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、—（CH2）pC3-6环烷基、—（CH2）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、—（CH2）NR5R6、—（CH2）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、—（CH2）pC3-6环烷基、—（CH2）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、—（CH2）pNR7R8或—（CH2）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、—（CH2）pC3-6环烷基、—（CH2）qOC1-6烷基或—（CH2）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。
• COMPOUNDS HAVING AFFINITY FOR DOPAMINE D3 RECEPTOR AND USES THEREOF"
  申请人：Bonanomi Giorgio

  公开号：US20100016287A1

  公开（公告）日：2010-01-21

  Compounds of formula (I) wherein A is a 5 or 6 membered heteroaromatic ring or a 5 or 6 membered heterocyclic ring, and which are useful for treating mental disorders such as schizophrenia are set out herein.

  本文介绍了式子（I）中A为5或6成员杂芳环或5或6成员杂环的化合物，可用于治疗精神障碍，如精神分裂症。