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    Process
    86.
    发明授权
    Process 失效
    处理

    公开(公告)号：US4565876A

    公开(公告)日：1986-01-21

    申请号：US612606

    申请日：1984-05-21

    Applicant: Alain Jouquey ,  Peter F. Hunt

    Inventor： Alain Jouquey ,  Peter F. Hunt

    IPC: C07J1/00 ,  C07C67/00 ,  C07C239/00 ,  C07C253/00 ,  C07C255/31 ,  C07C255/47 ,  C07C271/00 ,  C07J41/00 ,  C07J73/00 ,  C07J75/00 ,  C07D209/56

    CPC classification number: C07J41/0016 ,  C07J73/005 ,  C07C2103/26

    Abstract: A novel process for the preparation of a 16-imino-17-aza-steroid of the formula ##STR1## wherein A is selected from the group consisting of hydrogen and tritium comprising reacting a compound of the formula ##STR2## wherein A has the above definition and R is an acyl of an organic carboxylic acid of 1 to 8 carbon atoms with an oximation agent to obtain a compound of the formula ##STR3## reacting the latter with an agent to form an acid chloride to obtain a compound of the formula ##STR4## reacting the latter with ammonia to obtain a compound of the formula ##STR5## reacting the latter with an alkali metal hypohalite in the presence of a base to obtain a compound of the formula ##STR6## wherein X is a halogen and reacting the latter with a base to obtain the desired compound and the novel compound of formula I wherein A is tritium and the novel intermediates of formulae III, IV, V and VI.

    Abstract translation: 一种用于制备式I的16亚氨基-17-氮杂类固醇的新方法，其中A选自氢和氚，包括使下式化合物II与式 上述定义，R为具有1至8个碳原子的有机羧酸的酰基与肟化剂反应，得到下式化合物，其中后者与试剂反应形成酰氯，得到化合物 IV使后者与氨反应，得到下式的化合物，其中R 1在碱的存在下与碱金属次卤酸盐反应，得到式VI的化合物，其中X为 卤素并使其与碱反应以获得所需化合物和式I的新型化合物，其中A是氚，以及式III，IV，V和VI的新型中间体。

    Fluoranthene derivatives
    87.
    发明授权
    Fluoranthene derivatives 失效
    荧蒽衍生物

    公开(公告)号：US4532344A

    公开(公告)日：1985-07-30

    申请号：US496853

    申请日：1983-05-23

    Applicant: Kenneth W. Bair

    Inventor： Kenneth W. Bair

    CPC classification number: C07C2103/24 ,  C07C2103/26 ,  C07C2103/48 ,  C07C2103/50 ,  Y10S514/908

    Abstract: The present invention relates to compounds of formula (I) ##STR1## wherein Ar is a fluoranthene or substituted fluoranthene ring system; R.sup.1 is a C.sub.1-3 alkylene moiety; R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; R.sup.3 is a hydroxy C.sub.1-6 alkyl group; R.sup.4 and R.sup.5 are the same or different and are hydrogen, C.sub.1-6 alkyl or hydroxy C.sub.1-6 alkyl, esters thereof derived from condensation of carboxylic acids and hydroxyl groups of R.sup.3, R.sup.4, and R.sup.5 ;Acid addition salts thereof, which have been found useful for the treatment of tumors in mammals.

    Abstract translation: 本发明涉及式（I）的化合物：其中Ar是荧蒽或取代的荧蒽环体系; R1是C1-3亚烷基部分; R2是氢或C1-6烷基; R3是羟基C1-6烷基; R 4和R 5相同或不同，为氢，C 1-6烷基或羟基C 1-6烷基，其衍生自羧酸和R3，R4和R5的羟基的缩合的酯; 已经发现其酸加成盐可用于治疗哺乳动物的肿瘤。

    .beta.-Glycerophosphate salts of antimalarial phenanthrenemethanol compounds
    89.
    发明授权
    .beta.-Glycerophosphate salts of antimalarial phenanthrenemethanol compounds 失效
    抗疟药菲酚甲醇化合物的β-甘油磷酸盐

    公开(公告)号：US4507288A

    公开(公告)日：1985-03-26

    申请号：US533019

    申请日：1983-09-16

    Applicant: Jean F. Rossignol

    Inventor： Jean F. Rossignol

    IPC: C07D453/04 ,  C07F9/09 ,  A61K31/685

    CPC classification number: C07D453/04 ,  C07F9/091 ,  C07C2103/26

    Abstract: The compounds of formula (I) ##STR1## wherein R.sub.1 is hydrogen or an alkyl radical containing one to six carbon atoms and R.sub.2 is an alkyl radical containing one to six carbon atoms possess markedly increased activity against malaria-causing parasites. Pharmaceutical compositions and method of treatment of subjects with malaria are also disclosed.

    Abstract translation: 式（I）化合物其中R 1是氢或含有1至6个碳原子的烷基，R 2是含有1至6个碳原子的烷基，具有显着增加的抗疟原虫寄生虫的活性。 还公开了治疗疟疾受试者的药物组合物和方法。

    1,9-Dihydroxyoctahydrophenanthrenes
    90.
    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

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

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

    IPC: 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 classification number: 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

    Abstract: 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.

    Abstract translation: 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。

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