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    • 6. 发明授权
    • 3-[4-(1-substituted-4-piperazinyl)butyl]-4-thiazolidinone and related
compounds
    • 3- [4-(1-取代-4-哌嗪基)丁基] -4-噻唑烷酮及相关化合物
    • US5229388A
    • 1993-07-20
    • US795608
    • 1991-11-21
    • Nicholas J. HribJohn G. Jurcak
    • Nicholas J. HribJohn G. Jurcak
    • A61K31/425A61K31/44A61K31/47A61K31/495A61K31/505A61P25/04A61P25/08A61P25/18A61P25/20A61P25/24A61P25/26C07D277/14C07D277/60C07D277/82C07D417/12C07D417/14C07D513/10
    • C07D277/60C07D277/14C07D277/82C07D417/12C07D417/14
    • There are disclosed compounds of the formula, ##STR1## where n is 0, 1 or 2; A is ##STR2## where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; Y in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; m is 1 or 2; k is 1 or 2; R.sub.1 and R.sub.2 are independently hydrogen, loweralkyl, ##STR3## or aryl except that when R.sub.1 is ##STR4## or aryl, R.sub.2 is hydrogen, or alternatively R.sub.1 +R.sub.2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, indan or piperidine ring; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl, or alternatively R.sub.3 +R.sub.4 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, pyrrolidine or piperidine ring, the term aryl signifying an unsubstituted phenyl group or a phenyl group substituted with 1, 2 or 3 substituents each of which being independently loweralkyl, loweralkoxy, hydroxy, halogen, loweralkylthio, cyano, amino or trifluoromethyl, which are useful as antipsychotic, analgesic, anticonvulsant and anxiolytic agents.
    • 公开了下式的化合物,其中n为0,1或2; A是每一次出现的X独立地是氢,卤素,低级烷基,羟基,硝基,低级烷氧基,氨基,氰基,三氟甲基或甲硫基; Y在每次出现时独立地是氢,卤素,低级烷基,羟基,硝基,低级烷氧基,氨基,氰基,三氟甲基或甲硫基; m为1或2; k为1或2; R1和R2独立地是氢,低级烷基,低级或芳基,除了当R 1是芳基或芳基时,R 2是氢,或者R 1 + R 2与它们所连接的碳原子一起形成环戊烷,环己烷 ,环庚烷,吡喃,噻喃,茚满或哌啶环; R3和R4独立地是氢或低级烷基,或者R3 + R4与它们所连接的碳原子一起形成环戊烷,环己烷,环庚烷,吡喃,噻喃,吡咯烷或哌啶环,术语表示未取代的苯基的芳基 或被1,2或3个取代基取代的苯基,各自独立地为低级烷基,低级烷氧基,羟基,卤素,低级烷硫基,氰基,氨基或三氟甲基,其可用作抗精神病药,镇痛药,抗惊厥药和抗焦虑剂。
    • 10. 发明授权
    • 3-(4-substituted-4-piperazinyl)butyl-4-thiazolidinone and related
compounds
    • 3-(4-取代-4-哌嗪基)丁基-4-噻唑烷酮和相关化合物
    • US5136037A
    • 1992-08-04
    • US713247
    • 1991-06-07
    • Nicholas J. HribJohn G. Jurcak
    • Nicholas J. HribJohn G. Jurcak
    • A61K31/425A61K31/44A61K31/47A61K31/495A61K31/505A61P25/04A61P25/08A61P25/18A61P25/20A61P25/24A61P25/26C07D277/14C07D277/60C07D277/82C07D417/12C07D417/14C07D513/10
    • C07D277/60C07D277/14C07D277/82C07D417/12C07D417/14
    • There are disclosed compounds of the formula, ##STR1## where n is 0 or 1; A is ##STR2## where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; Y in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; m is 1 or 2; k is 1 or 2; R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, ##STR3## or alternatively R.sub.1 +R.sub.2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, indan or piperidine ring; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl, or alternatively R.sub.3 +R.sub.4 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, pyrrolidine or piperidine ring, the term aryl signifying an unsubstituted phenyl group or a phenyl group substituted with 1, 2 or 3 substituents each of which being independently loweralkyl, loweralkoxy, hydroxy, halogen, loweralkylthio, cyano, amino or trifluoromethyl, which are useful as antipsychotic, analgesic, anticonvulsant and anxiolytic agents.
    • 公开了下式的化合物,其中n为0或1; 其中每次出现的X独立地是氢,卤素,低级烷基,羟基,硝基,低级烷氧基,氨基,低级烷氧基,低级烷氧基, 氰基,三氟甲基或甲硫基; Y在每次出现时独立地是氢,卤素,低级烷基,羟基,硝基,低级烷氧基,氨基,氰基,三氟甲基或甲硫基; m为1或2; k为1或2; R1和R2独立地是氢,低级烷基,或者R1 + R2与它们所连接的碳原子一起形成环戊烷,环己烷,环庚烷,吡喃,噻喃,茚满或哌啶 环; R3和R4独立地是氢或低级烷基,或者R3 + R4与它们所连接的碳原子一起形成环戊烷,环己烷,环庚烷,吡喃,噻喃,吡咯烷或哌啶环,术语表示未取代的苯基的芳基 或被1,2或3个取代基取代的苯基,各自独立地为低级烷基,低级烷氧基,羟基,卤素,低级烷硫基,氰基,氨基或三氟甲基,其可用作抗精神病药,镇痛药,抗惊厥药和抗焦虑剂。