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    1,9-Dihydroxyoctahydrophenanthrenes
    3.
    发明授权
    1,9-Dihydroxyoctahydrophenanthrenes 失效
    1,9-二羟基焦氢氯苯

    公开(公告)号：US4237133A

    公开(公告)日：1980-12-02

    申请号：US78473

    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 ,  C07C45/72 ,  C07C45/73 ,  C07C49/747 ,  C07C49/755 ,  C07C49/757 ,  C07C49/83 ,  C07D211/32 ,  C07D213/30 ,  C07D213/50 ,  C07D317/22 ,  C07D317/72 ,  C07D295/14 ,  A61K31/22 ,  A61K31/535 ,  C07C101/19

    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 ,  C07C45/72 ,  C07C45/73 ,  C07C49/747 ,  C07C49/755 ,  C07C49/757 ,  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## 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R1是氢，苄基，苯甲酰基，1至5个碳原子的烷酰基或-CO-（CH2）p-NR'R“，其中p是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。

    Method of regulating the immune response with pyridine derivatives
    4.
    发明授权
    Method of regulating the immune response with pyridine derivatives 失效
    用吡啶衍生物调节免疫应答的方法

    公开(公告)号：US4500535A

    公开(公告)日：1985-02-19

    申请号：US470813

    申请日：1983-03-07

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

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

    IPC分类号： C07D213/26 ,  C07D213/30 ,  C07D213/32 ,  C07D213/55 ,  C07D213/65 ,  C07D239/26 ,  A61K31/44 ,  C07D213/48 ,  C07D213/51

    CPC分类号： C07D213/30 ,  C07D213/26 ,  C07D213/32 ,  C07D213/55 ,  C07D213/65 ,  C07D239/26

    摘要： A series of 4-(2-carboxymethylthiomethyl)pyridines and related compounds, and their pharmaceutically acceptable salts, are disclosed as having immunoregulatory activity. Preferred compounds include 4-(2-carboxymethylthiomethyl)pyridine [alternatively named 2-(4-picolylthio)acetic acid] and (C.sub.1 -C.sub.4)alkyl esters thereof, and 4-(1-formylmethylthiomethyl)-pyridine [alternatively named 2-(4-picolylthio)acetaldehyde] and bis(C.sub.1 -C.sub.4)alkyl or cyclic acetals thereof. These acids, esters, aldehydes and acetals also have utility as intermediates in the synthesis of the corresponding 4-(2-hydroxyethylthiomethyl)pyridines.

    摘要翻译： 公开了一系列4-（2-羧甲硫基甲基）吡啶及其相关化合物及其药学上可接受的盐，具有免疫调节活性。 优选的化合物包括4-（2-羧甲硫基甲基）吡啶[或称为2-（4-吡啶甲硫基）乙酸]及其（C 1 -C 4）烷基酯和4-（1-甲酰基甲硫基甲基） - 吡啶[ 4-吡啶甲硫基）乙醛]和双（C1-C4）烷基或环状缩醛。 这些酸，酯，醛和缩醛在合成相应的4-（2-羟基乙硫基甲基）吡啶时也可用作中间体。

    Hexahydro-trans-pyridoindole
    5.
    发明授权
    Hexahydro-trans-pyridoindole 失效
    六氢 - 反 - 吡啶并吲哚

    公开(公告)号：US4432978A

    公开(公告)日：1984-02-21

    申请号：US380182

    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 ,  A61K31/44 ,  A61K31/50 ,  A61K31/505

    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，（+）和（ - ）对映异构体或（+/-）外消旋2的混合物的衍生物2,3,4,5-四氢-1H-吡啶并[4,3-b] 3,4,4a，5,9b-六氢-4a，9b-反-1H-吡啶并[4,3-b]吲哚，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。

    Certain 4-(2-hydroxyethylthiomethyl)pyridines and derivatives thereof having immunoregulatory activity
    10.
    发明授权
    Certain 4-(2-hydroxyethylthiomethyl)pyridines and derivatives thereof having immunoregulatory activity 失效
    某些具有免疫调节活性的4-（2-羟基乙硫基甲基）吡啶及其衍生物

    公开(公告)号：US4535084A

    公开(公告)日：1985-08-13

    申请号：US474571

    申请日：1983-03-18

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

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

    IPC分类号： C07D213/32 ,  C07D213/55 ,  C07D213/65 ,  C07D239/26 ,  A61K31/44

    CPC分类号： C07D239/26 ,  C07D213/32 ,  C07D213/55 ,  C07D213/65

    摘要： A series of 4-(2-hydroxyethylthiomethyl)pyridines and related compounds, and their pharmaceutically acceptable acid addition salts, having immunoregulatory activity are disclosed. Preferred compounds include 4-(2-hydroxyethylthiomethyl)pyridine itself, as well as 4-(2-hydroxy-1-propylthiomethyl)pyridine, 4-(3-hydroxy-2-butylthiomethyl)pyridine, the acetate esters corresponding to the above compounds, and 4-(2,3-dihydroxy-1-propylthiomethyl)pyridine.

    摘要翻译： 公开了一系列具有免疫调节活性的4-（2-羟基乙硫基甲基）吡啶及其相关化合物及其药学上可接受的酸加成盐。 优选的化合物包括4-（2-羟基乙硫基甲基）吡啶本身以及4-（2-羟基-1-丙硫基甲基）吡啶，4-（3-羟基-2-丁硫基甲基）吡啶，对应于上述化合物的乙酸酯 和4-（2,3-二羟基-1-丙硫基甲基）吡啶。