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    Psychotropic polycyclic imides
    1.
    发明公开
    Psychotropic polycyclic imides 失效
    精神分析多环氰化物。

    公开(公告)号：EP0286263A1

    公开(公告)日：1988-10-12

    申请号：EP88302499.4

    申请日：1988-03-22

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： Stack, Gary Paul ,  Golobish, Thomas David ,  Abou-Gharbia, Magid Abdel-Megid

    IPC分类号： C07D401/12 ,  C07D221/24 ,  C07D313/06 ,  C07C61/125 ,  A61K31/45

    CPC分类号： C07C61/125 ,  C07D221/24 ,  C07D313/06 ,  C07D401/12

    摘要： Substituted imides of the following formula are antipsychotic, anxiolytic agents with very little extrapyramidal side effects:
    in which X is -O-, -S-, -SO-, -SO₂-, -CR₃R₄- where R₃ and R₄, independently, are hydrogen, alkyl of 1 to 4 carbon atoms or, taken together with the carbon atom to which they are attached, R₃ and R₄ form a cycloalkyl group of 3 to 5 carbon atoms; n is one of the integers 2, 3, 4 or 5; R is phenyl, alkylphenyl in which the alkyl group contains 1 to 4 carbon atoms, halophenyl, trifluoromethylphenyl, alkoxyphenyl, in which the alkoxy substituent contains 1 to 3 carbon atoms, 2-pyrimidinyl, halopyrimidin-2-yl, 2-pyrazinyl, halopyrazin-2-yl, 2-pyridinyl, cyanopyridin-2-yl, halopyridin-2-yl, quinolyl, or haloquinolyl; R₁ and R₂, taken together, are alkylene of 3 to 5 carbon atoms or alkenylene of 3 to 5 carbon atoms, or taken with the carbon atoms to which they are attached, R₁ and R₂ complete a benzene ring, or a group of the formula:
    where Y is -CH₂, -CH₂-CH₂-, -O- or -S- and the dotted line represents optional unsaturation; or a pharmaceutically acceptable salt thereof. In addition, the intermediate b3-dicarboxylic and the corresponding anhydrides - 2,3,3a,4,5,6,6a,7,7a-decahydro-­4,6,7-metheno-1 H -cyclopena[a]pentalene-1,3-dicarboxyli­c acid and octahydro-1, 5-methano-6,8,9-metheno-­pentaleno[1,2,-d]oxepin-2,4(1 H , 5 H )-dione represent especially significant aspects of the invention.

    摘要翻译： 下式的取代酰亚胺是具有极少锥体束外副作用的抗精神病药，抗焦虑剂：其中X是-O - ， - S-，-SO-，-SO 2 - ， - CR 3 R 4的，其中R3和R4独立地 是氢，1至4个碳原子的烷基，或与它们所连接的碳原子一起，R3和R4形成3至5个碳原子的环烷基; n是整数2,3,4或5之一; R为苯基，烷基含有1至4个碳原子的烷基苯基，卤代苯基，三氟甲基苯基，烷氧基苯基，其中烷氧基取代基含有1至3个碳原子，2-嘧啶基，卤代嘧啶-2-基，2-吡嗪基，卤代吡嗪 2-吡啶基，2-吡啶基，氰基吡啶-2-基，卤代吡啶-2-基，喹啉基或卤代喹啉基; R 1和R 2一起是3至5个碳原子的亚烷基或3至5个碳原子的亚烯基，或与它们所连接的碳原子一起取代，R 1和R 2完全是苯环，或者式 ：其中Y是-CH 2，-CH 2 -CH 2 - ， - O-或-S-，虚线表示任选的不饱和键; 或其药学上可接受的盐。 此外，中间体b3-二羧酸和相应的酸酐-2,3,3a，4,5,6,6a，7,7a-十氢-4,6,7-元 - 1H-环戊烯并[a] ，3-二羧酸和八氢-1,5-甲基-6,8,9-亚氨基 - 异戊烯[1,2， - ]氧杂七环-2,4（1H，5H） - 二酮代表本发明的特别重要的方面 。

    Chromane derivatives
    3.
    发明公开
    Chromane derivatives 失效
    Chromanderivate

    公开(公告)号：EP0771801A1

    公开(公告)日：1997-05-07

    申请号：EP96307772.2

    申请日：1996-10-28

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： Stack, Gary Paul ,  Mewshaw, Richard Eric

    IPC分类号： C07D491/06 ,  A61K31/40

    CPC分类号： C07D491/04

    摘要： Compounds of Formula I are selective autoreceptor agonists useful in treating disease states involving hyperactivity of dopamine systems:
    in which X is -(CH 2 ) n -; n is 1-3; R 1 is hydrogen, alkyl, hydroxyalkyl, cycloalkyl-methyl, bicyclo-alkylmethyl or -(CH 2 ) m YAr; where m is 04, Y is -CH 2 -, and Ar is phenyl, halophenyl, alkylphenyl, dialkylphenyl or alkoxyphenyl; R 2 is hydrogen or alkyl; R 3 is hydrogen, halogen, alkyl, alkoxy or hydroxy; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 式I化合物是可用于治疗涉及多巴胺系统多动症的疾病状态的选择性自体受体激动剂：其中X是 - （CH 2）n - 的CHEM> n为1-3; R1是氢，烷基，羟基烷基，环烷基 - 甲基，双环烷基甲基或 - （CH2）mYAr; 其中m为04，Y为-CH 2 - ，Ar为苯基，卤代苯基，烷基苯基，二烷基苯基或烷氧基苯基; R2是氢或烷基; R3是氢，卤素，烷基，烷氧基或羟基; 或其药学上可接受的盐。

    Substituted cycloalkanols
    7.
    发明公开
    Substituted cycloalkanols 失效
    取代基环烷醇

    公开(公告)号：EP0310268A2

    公开(公告)日：1989-04-05

    申请号：EP88308565.6

    申请日：1988-09-16

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： Husbands, George Edward Morris ,  Stack, Gary Paul

    IPC分类号： C07D295/08 ,  C07D239/42 ,  C07D241/20 ,  A61K31/495 ,  A61K31/505

    CPC分类号： C07D239/42 ,  C07D241/20 ,  C07D295/084

    摘要： Compounds of the formula:
    in which m is one of the integers 1,2 or 3; n is one of the integers 0,1 or 2; o is one of the integers 0,1 or 2; R₁ and R₂ are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, trifluoromethyl, halo, or, when taken together, 3,4-methylenedioxy; R₃ is alkyl,
    where R₄ and R₅ are, independently, hydrogen, hydroxy;l, alkyl, alkoxy, alkanoyloxy, halo or trifluoromethyl; and R₆ is hydrogen or halo; or a pharmaceutically acceptable salt thereof, are useful in treatment of psychiatric disorders.

    摘要翻译： 式中的化合物：其中m为整数1,2或3之一; n是整数0,1或2之一; o是整数0,1或2之一; R 1和R 2分别独立地为氢，羟基，烷基，烷氧基，烷酰氧基，三氟甲基，卤素，或当一起为3,4-亚甲二氧基时; R3是烷基，CHEM，其中R4和R5独立地是氢，羟基;烷基，烷氧基，烷酰氧基，卤素或三氟甲基; 和R6是氢或卤素; 或其药学上可接受的盐可用于治疗精神疾病。

    Dioxino derivatives and their use as dopamine agonists
    8.
    发明公开
    Dioxino derivatives and their use as dopamine agonists 失效
    Dioxinoderivate及其作为多巴胺受体激动剂使用

    公开(公告)号：EP0771800A3

    公开(公告)日：1998-01-28

    申请号：EP96307616.1

    申请日：1996-10-22

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： Stack, Gary Paul ,  Mewshaw, Richard Eric ,  Bravo, Byron Abel ,  Kang, Young Hee

    IPC分类号： C07D491/056 ,  A61K31/40 ,  A61K31/435

    CPC分类号： C07D491/04

    摘要： The compounds of formula I:
    wherein R 1 and R 2 are, independently, hydrogen, alkyl, phenyl or benzyl; or R 1 and R 2, taken together, are benzylidene optionally substituted with R 3 as defined below or alkylidene, or R 1 and R 2 , taken together with the carbon to which they are attached, form a carbonyl moiety or a cycloalkyl group; R 3 is hydrogen, hydroxy, halo, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, aralkoxy, alkanoyloxy, amino, mono- or di-alkylamino, alkanamido or alkanesulfonamido; R 4 is hydrogen or alkyl; m is an integer 0, 1 or 2; n is an integer from 0 to 6, inclusive; Z is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, polycyclo-alkyl, phenyl optionally substituted with R 3 as defined above, phenoxy optionally substituted with R 3 as defined above, naphthyl optionally substituted with R 3 as defined above or naphthyloxy optionally substituted with R 3 as defined above, heteroaryl or heteroaryloxy, in which the heterocyclic ring of the heteroaryl or heteroaryloxy group is selected from thiophene, furan, pyridine, pyrazine, pyrimidine, indole, indazole, imidazole, chroman, coumarin, carbostyril, quinoline, benzisoxazole, benzoxazole, pyrazole, pyrrole, thiazole, oxazole, or isoxazole and the heterocyclic ring is optionally substituted by R 3 as defined above; or a pharmaceutically acceptable salt thereof, are useful in treating disorders of the dopaminergic system.

    Dioxino derivatives and their use as dopamine agonists
    9.
    发明公开
    Dioxino derivatives and their use as dopamine agonists 失效
    Dioxinoderivate und ihre Verwendung als Dopamine Agonisten

    公开(公告)号：EP0771800A2

    公开(公告)日：1997-05-07

    申请号：EP96307616.1

    申请日：1996-10-22

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： Stack, Gary Paul ,  Mewshaw, Richard Eric ,  Bravo, Byron Abel ,  Kang, Young Hee

    IPC分类号： C07D491/056 ,  A61K31/40 ,  A61K31/435

    CPC分类号： C07D491/04

    摘要： The compounds of formula I:
    wherein R 1 and R 2 are, independently, hydrogen, alkyl, phenyl or benzyl; or R 1 and R 2, taken together, are benzylidene optionally substituted with R 3 as defined below or alkylidene, or R 1 and R 2 , taken together with the carbon to which they are attached, form a carbonyl moiety or a cycloalkyl group; R 3 is hydrogen, hydroxy, halo, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, aralkoxy, alkanoyloxy, amino, mono- or di-alkylamino, alkanamido or alkanesulfonamido; R 4 is hydrogen or alkyl; m is an integer 0, 1 or 2; n is an integer from 0 to 6, inclusive; Z is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, polycyclo-alkyl, phenyl optionally substituted with R 3 as defined above, phenoxy optionally substituted with R 3 as defined above, naphthyl optionally substituted with R 3 as defined above or naphthyloxy optionally substituted with R 3 as defined above, heteroaryl or heteroaryloxy, in which the heterocyclic ring of the heteroaryl or heteroaryloxy group is selected from thiophene, furan, pyridine, pyrazine, pyrimidine, indole, indazole, imidazole, chroman, coumarin, carbostyril, quinoline, benzisoxazole, benzoxazole, pyrazole, pyrrole, thiazole, oxazole, or isoxazole and the heterocyclic ring is optionally substituted by R 3 as defined above; or a pharmaceutically acceptable salt thereof, are useful in treating disorders of the dopaminergic system.

    摘要翻译： 式I化合物：其中R 1和R 2独立地是氢，烷基，苯基或苄基; 或R 1和R 2彼此一起是任选被如下定义的R 3取代的亚苄基或亚烷基或R 1和R 2与它们所连接的碳一起连接 ，形成羰基部分或环烷基; R 3是氢，羟基，卤素，三氟甲基，三氟甲氧基，烷基，烷氧基，芳烷氧基，烷酰氧基，氨基，单 - 或二 - 烷基氨基，烷酰氨基或烷烃磺酰氨基; R 4是氢或烷基; m是整数0,1或2; n是0至6的整数，包括0和6; Z是氢，羟基，烷基，烯基，炔基，烷氧基，环烷基，多环烷基，任选被如上所定义的R 3取代的苯基，任选被如上定义的R 3取代的苯氧基， 3或如上定义的R 3所取代的萘氧基，杂芳基或杂芳氧基，其中杂芳基或杂芳氧基的杂环选自噻吩，呋喃，吡啶，吡嗪，嘧啶，吲哚，吲唑， 咪唑，苯并二氢吡喃酮，香豆素，喹诺酮，喹啉，苯并异恶唑，苯并恶唑，吡唑，吡咯，噻唑，恶唑或异恶唑，杂环任选被上述定义的R 3取代; 或其药学上可接受的盐可用于治疗多巴胺能系统的病症。