Substituted derivatives of 20,21-dinoreburnamenine, their use as
medicaments and the pharmaceutical compositions containing them
    3.
    发明授权
    Substituted derivatives of 20,21-dinoreburnamenine, their use as medicaments and the pharmaceutical compositions containing them 失效
    其作为药物和含有它们的药物组合物的二十二碳三烯酸的取代衍生物

    公开(公告)号:US5093337A

    公开(公告)日:1992-03-03

    申请号:US391511

    申请日:1989-07-18

    CPC classification number: C07D461/00

    Abstract: The invention concerns compounds of formula (I); ##STR1## in which R.sub.1, R.sub.2 and R.sub.3, identical or different, stand for hydrogen, halogen, alkyl or alkoxy (C.sub.1-5), hydroxy, trifluoromethyl, nitro, amino, alkylamino, dialkylamino, acylamino, R.sub.1, R.sub.2 and R.sub.3 being unable to stand for hydrogen simultaneously and in which (a) stands for (b), (c), or (d), all possible isomeric forms of said products of formula (I) being racemic or optically active, as well as their additional salts with acids, their preparation and the new intermediate products obtained, their application as drugs in particular nootropes, antidepressants, neuronal protectors, anti-anoxics, anti-ischemics, and the compositions containing them.

    Abstract translation: PCT No.PCT / FR88 / 00562 Sec。 371日期:1989年7月18日 102(e)日期1989年7月18日PCT提交1988年11月16日PCT公布。 出版物WO89 / 04830 日期:1989年6月1日。本发明涉及式(I)化合物。 其中R1,R2和R3相同或不同,代表氢,卤素,烷基或烷氧基(C1-5),羟基,三氟甲基,硝基,氨基,烷基氨基,二烷基氨基,酰基氨基, R1,R2和R3不能同时代表氢,其中(a)代表(b),(c)或(d),所有式(I)产物的所有可能的异构形式是外消旋或光学活性的 以及它们与酸的附加盐,它们的制备和获得的新的中间产物,它们作为药物特别是助推剂,抗抑郁药,神经元保护剂,抗缺氧剂,抗缺血剂以及含有它们的组合物的应用。

    Novel apovincaminic acid derivatives
    4.
    发明授权
    Novel apovincaminic acid derivatives 失效
    新型氨基丁酸衍生物

    公开(公告)号:US4614824A

    公开(公告)日:1986-09-30

    申请号:US754671

    申请日:1985-07-11

    CPC classification number: C07D461/00

    Abstract: The invention relates to new racemic and optically active apovincaminic acid derivatives of the general formula (I) ##STR1## wherein A is hydroxyl, halogen or a group --O--(CH.sub.2).sub.n --OR.sup.1 or --OMe, in whichR.sup.1 is alkyl having from one to 6 carbon atoms,n is an integer between 2 and 6,Me is an alkali metal,R.sup.2 stands for an alkyl group having from one to 6 carbon atoms, which may be identical with or different from R.sup.1,and the hydrogen in the 3-position and the R.sup.2 group have an .alpha.,.alpha.- and/or .beta.,.beta.- or .alpha.,.beta.- and/or .beta.,.alpha.-configuration, and pharmaceutically acceptable acid addition salts thereof, which are pharmaceutically active, e.g. show antihypoxial activity or are potent peripheral vasodilators. Their preparation and pharmaceutical composition containing them are also within the scope of the invention.

    Abstract translation: 本发明涉及通式(I)的新的外消旋和光学活性氨基丁酸衍生物,其中A是羟基,卤素或-O-(CH2)n-OR1或-OMe基团,其中R1 是具有1至6个碳原子的烷基,n是2和6之间的整数,Me是碱金属,R 2表示具有1至6个碳原子的烷基,其可以与R 1相同或不同, 3-位和R2基团中的氢具有药学活性的α,α - 和/或β,β-或α,β-和/或β,α-构型及其药学上可接受的酸加成盐 ,例如 显示抗低氧活性或是有效的外周血管扩张剂。 它们的制备和含有它们的药物组合物也在本发明的范围内。

    Process for the preparation of apovincaminic acid ester derivatives
    6.
    发明授权
    Process for the preparation of apovincaminic acid ester derivatives 失效
    氨基丁酸酯衍生物的制备方法

    公开(公告)号:US4400514A

    公开(公告)日:1983-08-23

    申请号:US209265

    申请日:1980-11-21

    CPC classification number: C07D461/00

    Abstract: The invention concerns a new process for the preparation of apovincaminic acid ester derivatives of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 independently represent an alkyl group having 1 to 6 carbon atoms,and pharmaceutically acceptable salts thereof.According to the invention the apovincaminic acid ester derivatives of the general formula (I) are prepared by reacting the corresponding 9- and/or 10- and/or 11-halo-14-oxo-15-hydroxyimino-E-homo-eburnane derivatives with an alkanol of the general formula R.sup.1 --OH, wherein R.sup.1 is as defined above, and with a dehydrating concentrated acid, and subsequently reducing the 9- and/or 10- and/or 11-halo-apovincaminic acid esters obtained, selectively on the aromatic ring. Alternatively, the 9- and/or 10- and/or 11-halo-apovincaminic acid esters can also be used as starting materials. The invention includes the preparation of racemic and optically active apovincaminic acid ester derivatives and of their pharmaceutically acceptable salts, as well.

    Abstract translation: 本发明涉及一种制备通式(I)的氨基苯甲酸酯衍生物的新方法,其中R1和R2独立地表示具有1至6个碳原子的烷基,及其药学上可接受的盐。 根据本发明,通式(I)的氨基亚氨酸酯衍生物通过相应的9-和/或10-和/或11-卤代-14-氧代-15-羟基亚氨基-E-高 - 伊本恩衍生物 与通式R 1 -OH的烷醇,其中R 1如上定义,并与脱水浓酸反应,然后选择性地将所得的9-和/或10-和/或10-卤代 - 氨基丁酸酯还原 芳香环。 或者,9-和/或10-和/或11-卤代 - 氨基丁酸酯也可以用作原料。 本发明还包括外消旋和光学活性氨肽酸酯衍生物及其药学上可接受的盐的制备。

    Process for the manufacture of prolonged action vincamine preparations,
the vincamine preparations so obtained, and medicaments containing them
    7.
    发明授权
    Process for the manufacture of prolonged action vincamine preparations, the vincamine preparations so obtained, and medicaments containing them 失效
    用于制备延长活性长春胺制剂,如此获得的长春胺制剂和含有它们的药物的方法

    公开(公告)号:US4369175A

    公开(公告)日:1983-01-18

    申请号:US288236

    申请日:1981-07-27

    Inventor: Satish C. Khanna

    CPC classification number: C07D461/00 A61K47/48184

    Abstract: The invention relates to a process for the manufacture of prolonged action and stable vincamine preparations, which process comprises reacting an acid addition salt of vincamine with an alkali metal salt or alkaline earth metal salt of a sulfonic acid cation exchange resin, in particular an alkali metal salt of a sulfonated copolymer of styrene with a small amount of divinyl benzene, in a polar reaction medium such as water. The invention further relates to the vincamine preparations so obtained, to the use thereof for the manufacture of ready-for-use medicaments for oral administration and to these medicaments themselves.

    Abstract translation: 本发明涉及一种制备延长作用和稳定的长春胺制剂的方法,该方法包括使长春胺的酸加成盐与磺酸阳离子交换树脂的碱金属盐或碱土金属盐,特别是碱金属 苯乙烯与少量二乙烯基苯的磺化共聚物的盐,在极性反应介质如水中。 本发明还涉及如此获得的长春胺制剂及其用于制备用于口服给药的即用型药物及其用途。

    Vincamine saccharinate and a pharmaceutical composition containing it
dissolved therein
    8.
    发明授权
    Vincamine saccharinate and a pharmaceutical composition containing it dissolved therein 失效
    甘氨酸长春胺和其中溶解有其的药物组合物

    公开(公告)号:US4362730A

    公开(公告)日:1982-12-07

    申请号:US283706

    申请日:1981-07-16

    CPC classification number: C07D275/06 C07D461/00

    Abstract: Vincamine saccharinate, a novel derivative of vincamine, and pharmaceutical compositions containing vincamine saccharinate are disclosed. The solubility of vincamine saccharinate in glycerol-ethanol mixtures and the superior taste characteristics of vincamine saccharinate allow the preparation of preferred pharmaceutical compositions in solution form which are suitable for oral administration, especially in the form of drops.

    Abstract translation: 公开了长春胺的新型衍生物,并且含有长春胺糖精酸盐的药物组合物。 长春胺糖精在甘油 - 乙醇混合物中的溶解度以及长春胺长春胺的优越味道特性允许制备适合于口服给药,特别是滴剂形式的溶液形式的优选药物组合物。

    Synthesis of vincaminic acid derivatives
    9.
    发明授权
    Synthesis of vincaminic acid derivatives 失效
    长春胺酸衍生物的合成

    公开(公告)号:US4316029A

    公开(公告)日:1982-02-16

    申请号:US161359

    申请日:1980-06-20

    Applicant: Guy Rossey

    Inventor: Guy Rossey

    CPC classification number: C07D471/14 C07D461/00 Y02P20/55

    Abstract: Vincaminic acid derivatives of formula (A) ##STR1## useful in treating cerebral insufficiency, are prepared by reacting 1-ethyl-2,3,4,6,7,12-hexahydroindolo[2,3-a]quinolizine with the 2,4-DNP hydrazone of ethyl or methyl bromopyruvate followed by (i) reduction of the C.dbd.N bond and (ii) simultaneous cyclization with removal of the ketone-protecting group in either order.

    Abstract translation: 通过使1-乙基-2,3,4,6,7,12-六氢吲哚并[2,3-a]喹嗪与...的制备,可用于治疗脑功能不全的式(A)< IMAGE>(A) 乙基或甲基溴丙酮酸盐的2,4-DNP腙,然后(i)还原C = N键,和(ii)以任何顺序除去酮保护基团同时环化。

    Process for producing eburnane derivatives
    10.
    发明授权
    Process for producing eburnane derivatives 失效
    生产伊本恩衍生物的方法

    公开(公告)号:US4316028A

    公开(公告)日:1982-02-16

    申请号:US93606

    申请日:1979-11-13

    CPC classification number: C07D471/14 C07D461/00

    Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is a C.sub.1 -C.sub.6 alkyl group and R is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, and their salts, which are useful as cerebral vasodilator; and a compound of the formula: ##STR2## wherein R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, R.sup.3 is a hydrogen atom or the formula: --CO.sub.2 R.sup.1 (R.sup.1 is a C.sub.1 -C.sub.6 alkyl group) and W is an oxygen atom, an imino group or ##STR3## but not an imino group in case that R.sup.3 is a hydrogen atom, which are intermediates of the compound (I), useful per se as cerebral vasodilator and/or antihypertensive agents.

    Abstract translation: 下式的化合物:其中R1是C1-C6烷基,R是氢原子或C1-C6烷基,它们的盐可用作脑血管扩张剂; 和下式的化合物:其中R 2是氢原子或C 1 -C 6烷基,R 3是氢原子或式-CO 2 R 1(R 1是C 1 -C 6烷基)和W 在R3是氢原子的情况下是氧原子,亚氨基或亚氨基,而不是亚氨基,它是作为脑血管扩张剂和/或抗高血压药物的化合物(I)的中间体。

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