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    Hexahydro-trans- and tetrahydropyridoindole neuroleptic agents
    11.
    发明授权
    Hexahydro-trans- and tetrahydropyridoindole neuroleptic agents 失效
    六氢反式和四氢吡啶吲哚精神抑制剂

    公开(公告)号：US4427679A

    公开(公告)日：1984-01-24

    申请号：US379826

    申请日：1982-05-20

    申请人： Willard M. Welch ,  Charles A. Harbert

    发明人： Willard M. Welch ,  Charles A. Harbert

    IPC分类号： C07D471/04 ,  C07D487/04 ,  A61K31/495

    CPC分类号： C07D471/04

    摘要： Derivatives of 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole and of (+)enantiomeric, mixtures of (+) and (-)enantiomeric or (.+-.)racemic 2,3,4,4a,5,9b-hexahydro-4a,9b-trans-1H-pyrido[4,3-b]indole, substituted at the 5-position with an aryl group and at the 2-position with a carbonylaminoalkyl group or an aminoalkyl group, are neuroleptic agents useful in the treatment of certain psychoses and neuroses.

    摘要翻译： （+）对映异构体的（+）和（ - ）对映异构体或（+/-）外消旋2,3的（+）和（+）对映异构体的混合物的衍生物（2,3,4,5-四氢-1H-吡啶并[4,3-b] ，4,4a，5,9b-六氢-4a，9b-反式-1H-吡啶并[4,3-b]吲哚，其在5-位被芳基取代，在2-位被羰基氨基烷基取代，或 氨基烷基是用于治疗某些精神病和神经元的神经安定药。

    Intermediates to 1,9-dihydroxyoctahydrophenanthrenes
    14.
    发明授权
    Intermediates to 1,9-dihydroxyoctahydrophenanthrenes 失效
    中间体至1,9-二羟基焦合氢离子

    公开(公告)号：US4310669A

    公开(公告)日：1982-01-12

    申请号：US219319

    申请日：1980-12-22

    申请人： Thomas H. Althuis ,  Charles A. Harbert ,  Michael R. Johnson ,  Lawrence S. Melvin, Jr.

    发明人： Thomas H. Althuis ,  Charles A. Harbert ,  Michael R. Johnson ,  Lawrence S. Melvin, Jr.

    IPC分类号： C07C41/22 ,  C07C41/26 ,  C07C43/225 ,  C07C43/23 ,  C07C45/45 ,  C07C45/54 ,  C07C45/61 ,  C07C45/67 ,  C07C45/68 ,  C07C45/71 ,  C07C45/73 ,  C07C49/747 ,  C07C49/755 ,  C07D211/32 ,  C07D213/30 ,  C07D213/50 ,  C07D317/22 ,  C07D317/72 ,  C07D213/55 ,  C07D211/34

    CPC分类号： C07D213/30 ,  C07C41/01 ,  C07C41/22 ,  C07C41/26 ,  C07C45/45 ,  C07C45/54 ,  C07C45/61 ,  C07C45/67 ,  C07C45/68 ,  C07C45/71 ,  C07C45/73 ,  C07C49/747 ,  C07C49/755 ,  C07D211/32 ,  C07D213/50 ,  C07D317/22 ,  C07D317/72 ,  C07C2101/14

    摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrrolo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) -(alk.sub.1).sub.m -X-(alk.sub.2).sub.n - wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;m and n are each 0 or 1;X is selected from O, S, SO and SO.sub.2 ; andW is selected from hydrogen, methyl, pyridyl, piperidyl, phenyl, monochlorophenyl, monofluorophenyl and ##STR2## from hydrogen, phenyl, monochlorophenyl and monofluorophenyl; a is an integer from 1 to 5 and b is 0 or an integer from 1 to 4, with the proviso that the sum of a and b is not greater than 5.Compounds I and II are useful as analgesics. Compound III is useful as an intermediate for the preparation of Compounds I and II. Intermediates for the preparation of I, II and III are disclosed. A process for the use of Compounds I and II to produce analgesia is also described.

    摘要翻译： 其中R 1为氢，苄基，苯甲酰基，1至5个碳原子的烷酰基或-CO-（CH 2）p -NR'R“，其中p为0或1至 4; 当单独使用时，R'和R“各自为氢或1至4个碳原子的烷基; 当与它们所连接的氮一起取代时，R'和R“与烷基中具有1至4个碳原子的5-或6-元杂环选自哌啶子基，吡咯烷基，吡咯烷子基，吗啉代和N-烷基哌嗪基 组; R 2选自氢，1至6个碳原子的烷酰基和苯甲酰基; R3选自氢，甲基和乙基; R4选自氢，1至6个碳原子的烷基和苄基; Z选自：（a）具有1至9个碳原子的亚烷基; （b） - （alk1）mX-（alk2）n-其中（alk1）和（alk2）各自为具有1至9个碳原子的亚烷基，条件是（alk1）加（alk2） ）不大于9; m和n分别为0或1; X选自O，S，SO和SO2; W选自氢，甲基，吡啶基，哌啶基，苯基，一氯苯基，一氟苯基和氢，苯基，一氯苯基和单氟苯基; a为1至5的整数，b为0或1至4的整数，条件是a和b之和不大于5.化合物I和II可用作止痛剂。 化合物III可用作制备化合物I和II的中间体。 公开了制备I，II和III的中间体。 还描述了使用化合物I和II产生镇痛的方法。

    1,9-Dihydroxyoctahydrophenanthrenes and intermediates therefor
    15.
    发明授权
    1,9-Dihydroxyoctahydrophenanthrenes and intermediates therefor 失效
    1,9-二羟基八氢菲和其中间体

    公开(公告)号：US4268692A

    公开(公告)日：1981-05-19

    申请号：US78475

    申请日：1979-09-24

    申请人： Thomas H. Althuis ,  Charles A. Harbert ,  Michael R. Johnson ,  Lawrence S. Melvin, Jr.

    发明人： Thomas H. Althuis ,  Charles A. Harbert ,  Michael R. Johnson ,  Lawrence S. Melvin, Jr.

    IPC分类号： C07C41/22 ,  C07C41/26 ,  C07C43/225 ,  C07C43/23 ,  C07C45/45 ,  C07C45/46 ,  C07C45/54 ,  C07C45/61 ,  C07C45/67 ,  C07C45/68 ,  C07C45/71 ,  C07C45/73 ,  C07C49/747 ,  C07C49/755 ,  C07C49/83 ,  C07D211/32 ,  C07D213/30 ,  C07D213/50 ,  C07D317/22 ,  C07D317/72 ,  C07C49/733 ,  C07C69/78

    CPC分类号： C07D213/30 ,  C07C41/01 ,  C07C41/22 ,  C07C41/26 ,  C07C45/45 ,  C07C45/46 ,  C07C45/54 ,  C07C45/61 ,  C07C45/67 ,  C07C45/68 ,  C07C45/71 ,  C07C45/73 ,  C07C49/747 ,  C07C49/755 ,  C07C49/83 ,  C07D211/32 ,  C07D213/50 ,  C07D317/22 ,  C07D317/72 ,  C07C2101/14 ,  C07C2103/26

    摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrollo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) -(alk.sub.1).sub.m -X-(alk.sub.2).sub.n -wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;m and n are each 0 or 1;X is selected from O, S, SO and SO.sub.2 ; andW is selected from hydrogen, methyl, pyridyl, piperidyl, phenyl, monochlorophenyl, monofluorophenyl and ##STR2## from hydrogen, phenyl, monochlorophenyl and monofluorophenyl; a is an integer from 1 to 5 and b is 0 or an integer from 1 to 4, with the proviso that the sum of a and b is not greater than 5.Compounds I and II are useful as analgesics. Compound III is useful as an intermediate for the preparation of Compounds I and II. Intermediates for the preparation of I, II and III are disclosed. A process for the use of compounds I and II to produce analgesia is also described.

    摘要翻译： 其中R 1为氢，苄基，苯甲酰基，1至5个碳原子的烷酰基或-CO-（CH 2）p -NR'R“，其中p为0或从 1至4; 当单独使用时，R'和R“各自为氢或1至4个碳原子的烷基; 当与它们所连接的氮一起取代时，R'和R“与烷基中具有1至4个碳原子的5-或6-元杂环选自哌啶子基，吡咯烷基，吡咯烷子基，吗啉代和N-烷基哌嗪基 组; R 2选自氢，1至6个碳原子的烷酰基和苯甲酰基; R3选自氢，甲基和乙基; R4选自氢，1至6个碳原子的烷基和苄基; Z选自：（a）具有1至9个碳原子的亚烷基; （b） - （alk1）mX-（alk2）n - 其中（alk1）和（alk2）各自为具有1至9个碳原子的亚烷基，条件是（alk1）加（alk2） ）不大于9; m和n分别为0或1; X选自O，S，SO和SO2; W选自氢，甲基，吡啶基，哌啶基，苯基，一氯苯基，一氟苯基和氢，苯基，一氯苯基和单氟苯基; a为1至5的整数，b为0或1至4的整数，条件是a和b之和不大于5.化合物I和II可用作止痛剂。 化合物III可用作制备化合物I和II的中间体。 公开了制备I，II和III的中间体。 还描述了使用化合物I和II产生止痛的方法。

    Amide therapeutic agents
    17.
    发明授权
    Amide therapeutic agents 失效
    酰胺治疗剂

    公开(公告)号：US4217355A

    公开(公告)日：1980-08-12

    申请号：US899065

    申请日：1978-04-24

    申请人： Charles A. Harbert ,  Joseph G. Lombardino

    发明人： Charles A. Harbert ,  Joseph G. Lombardino

    IPC分类号： C07D277/20 ,  A61K31/425 ,  A61K31/426 ,  A61K31/445 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55 ,  A61P29/00 ,  A61P37/00 ,  C07D207/16 ,  C07D211/60 ,  C07D223/06 ,  C07D265/30 ,  C07D277/46 ,  C07D279/12 ,  C07D307/14 ,  C07D307/52 ,  C07D317/00 ,  C07D333/00 ,  C07D333/36 ,  C07D417/12 ,  C07D277/38

    CPC分类号： C07D265/30 ,  C07D207/16 ,  C07D211/60 ,  C07D223/06 ,  C07D277/46 ,  C07D279/12 ,  C07D307/14 ,  C07D307/52 ,  C07D333/36

    摘要： A series of N-(2-thiazolyl)amides has been prepared, including their pharmaceutically acceptable acid addition salts as well as pharmaceutical compositions containing same. These compounds are useful in therapy as anti-inflammatory agents in addition to being useful as immunoregulatory agents for modulating various body immune responses. Preferred member compounds include N-(2-thiazolyl)-.alpha.-methylaminoacetamide, N-(2-thiazolyl)-.alpha.-benzylaminoacetamide, N-(2-thiazolyl)-.alpha.-(p-fluorobenzylamino)acetamide, N-(2-thiazolyl)-.alpha.-(2-thenylamino)acetamide and N-(4-methyl-2-thiazolyl)-.alpha.-amino-.beta.-phenylpropionamide, and their hydrohalide acid addition salts. Three different methods of preparation are provided and these are all described in some detail, including the various synthetic routes leading to the required novel intermediates and/or starting materials.

    摘要翻译： 已经制备了一系列N-（2-噻唑基）酰胺，包括其药学上可接受的酸加成盐以及含有它们的药物组合物。 除了作为用于调节各种身体免疫应答的免疫调节剂之外，这些化合物可用作治疗作为抗炎剂。 优选的成员化合物包括N-（2-噻唑基）-α-甲基氨基乙酰胺，N-（2-噻唑基）-α-苄基氨基乙酰胺，N-（2-噻唑基）-α-（对氟苄基氨基）乙酰胺，N-（2- 噻唑基）-α-（2-叔丁基氨基）乙酰胺和N-（4-甲基-2-噻唑基）-α-氨基-β-苯基丙酰胺及其氢卤酸加成盐。 提供了三种不同的制备方法，这些都被详细描述，包括导致所需新型中间体和/或起始材料的各种合成途径。

    Intermediates to 1,9-dihydroxyoctahydrophenanthrenes
    20.
    发明授权
    Intermediates to 1,9-dihydroxyoctahydrophenanthrenes 失效
    中间体至1,9-二羟基焦合氢离子

    公开(公告)号：US4310529A

    公开(公告)日：1982-01-12

    申请号：US218712

    申请日：1980-12-22

    申请人： Thomas H. Althuis ,  Charles A. Harbert ,  Michael R. Johnson ,  Lawrence S. Melvin, Jr.

    发明人： Thomas H. Althuis ,  Charles A. Harbert ,  Michael R. Johnson ,  Lawrence S. Melvin, Jr.

    IPC分类号： C07C41/22 ,  C07C41/26 ,  C07C43/225 ,  C07C43/23 ,  C07C45/45 ,  C07C45/54 ,  C07C45/61 ,  C07C45/67 ,  C07C45/68 ,  C07C45/71 ,  C07C45/73 ,  C07C49/747 ,  C07C49/755 ,  C07D211/32 ,  C07D213/30 ,  C07D213/50 ,  C07D317/22 ,  C07D317/72 ,  A61K31/44 ,  A61K31/445 ,  C07D213/55

    CPC分类号： C07D213/30 ,  C07C41/01 ,  C07C41/22 ,  C07C41/26 ,  C07C45/45 ,  C07C45/54 ,  C07C45/61 ,  C07C45/67 ,  C07C45/68 ,  C07C45/71 ,  C07C45/73 ,  C07C49/747 ,  C07C49/755 ,  C07D211/32 ,  C07D213/50 ,  C07D317/22 ,  C07D317/72 ,  C07C2101/14

    摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrrolo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) --(alk.sub.1).sub.m --X--(alk.sub.2).sub.n --wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;m and n are each 0 or 1;X is selected from O, S, SO and SO.sub.2 ; andW is selected from hydrogen, methyl, pyridyl, piperidyl, phenyl, monochlorophenyl, monofluorophenyl and ##STR2## wherein W.sub.1 is selected from hydrogen, phenyl, monochlorophenyl and monofluorophenyl; a is an integer from 1 to 5 and b is 0 or an integer from 1 to 4, with the proviso that the sum of a and b is not greater than 5.Compounds I and II are useful as analgesics. Compound III is useful as an intermediate for the preparation of Compounds I and II. Intermediates for the preparation of I, II and III are disclosed. A process for the use of compounds I and II to produce analgesia is also described.

    摘要翻译： 其中R 1为氢，苄基，苯甲酰基，1至5个碳原子的烷酰基或-CO-（CH 2）p -NR'R“，其中p为0 或1到4的整数; 当单独使用时，R'和R“各自为氢或1至4个碳原子的烷基; 当与它们所连接的氮一起取代时，R'和R“与烷基中具有1至4个碳原子的5-或6-元杂环选自哌啶子基，吡咯烷基，吡咯烷子基，吗啉代和N-烷基哌嗪基 组; R 2选自氢，1至6个碳原子的烷酰基和苯甲酰基; R3选自氢，甲基和乙基; R4选自氢，1至6个碳原子的烷基和苄基; Z选自：（a）具有1至9个碳原子的亚烷基; （b） - （alk1）mX-（alk2）n - 其中（alk1）和（alk2）各自为具有1至9个碳原子的亚烷基，条件是（alk1）加（alk2） ）不大于9; m和n分别为0或1; X选自O，S，SO和SO2; W选自氢，甲基，吡啶基，哌啶基，苯基，一氯苯基，一氟苯基和其中W1选自氢，苯基，一氯苯基和单氟苯基; a为1至5的整数，b为0或1至4的整数，条件是a和b之和不大于5.化合物I和II可用作止痛剂。 化合物III可用作制备化合物I和II的中间体。 公开了制备I，II和III的中间体。 还描述了使用化合物I和II产生止痛的方法。