Steroids with pregnane skeleton, pharmaceutical compositions containing
them
    33.
    发明授权
    Steroids with pregnane skeleton, pharmaceutical compositions containing them 失效
    具有孕烷骨架的类固醇,含有它们的药物组合物

    公开(公告)号:US5547949A

    公开(公告)日:1996-08-20

    申请号:US351448

    申请日:1994-12-08

    摘要: Novel, therapeutically active 21-aminosteroids of formula (I) ##STR1## with pregnane skeleton, are disclosed wherein two of X, Y and Z are a nitrogen atom each and the third one is a methine group; R.sup.1 and R.sup.2 are independently from each other, a primary amino group bearing as substituent a branched-chain C.sub.4-8 alkyl -alkenyl or -alkynyl group, or a C.sub.4-10 cycloalkyl group comprising 1 to 3 ring(s) and being optionally substituted by at least one C.sub.1-3 alkyl group; or R.sup.1 and R.sup.2 are each a spiro-heterocyclic secondary amino group containing at most 10 carbon atoms and optionally at least one oxygen atom as additional heteroatom; or one of R.sup.1 and R.sup.2 is an unsubstituted heterocyclic secondary amino group containing 4 to 7 carbon atoms and the other one is an above-identified primary amino group, an above-identified spiro-heterocyclic secondary amino group, or a heterocyclic secondary amino group containing 4 to 7 carbon atoms and substituted by at least one C.sub.1-4 alkyl group; and n is 1 or 2, as well as their acid addition salts and pharmaceutical compositions containing these compounds.

    摘要翻译: PCT No.PCT / HU93 / 00035 Sec。 371日期1994年12月8日第 102(e)日期1994年12月8日PCT提交1993年6月8日PCT公布。 公开号WO93 / 25570 日期:1993年12月23日公开了具有孕烷骨架的式(I)< IMAGE>(I)< IMAGE>中的新型治疗活性的21-氨基甾体,其中X,Y和Z中的两个各自为氮原子, 次甲基; R1和R2彼此独立地是带有支链C4-8烷基 - 烯基或 - 炔基的取代基的伯氨基或包含1〜3个环的C4-10环烷基,并且任选地被 至少一个C 1-3烷基; 或R 1和R 2各自为含有至多10个碳原子的螺杂环仲氨基和任选的至少一个氧原子作为其它杂原子; R 1和R 2中的一个是含有4至7个碳原子的未取代的杂环仲氨基,另一个是上述的伯氨基,上述的螺杂环仲氨基或含有 4至7个碳原子并被至少一个C 1-4烷基取代; 和n为1或2,以及它们的酸加成盐和含有这些化合物的药物组合物。

    Biologically active eburnamenine derivatives, pharmaceutical
compositions containing them and process for preparing same
    35.
    发明授权
    Biologically active eburnamenine derivatives, pharmaceutical compositions containing them and process for preparing same 失效
    生物活性白蛋白衍生物,含有它们的药物组合物及其制备方法

    公开(公告)号:US5510345A

    公开(公告)日:1996-04-23

    申请号:US351447

    申请日:1994-12-08

    CPC分类号: C07D461/00

    摘要: The invention relates to novel eburnamenine derivatives of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 as well as R.sup.3 and R.sup.4, independently from each other, stand for hydrogen, C.sub.2-6 alkyl group, C.sub.2-6 alkenyl group; or a C.sub.3-10 alicyclic group involving 1 to 3 rings, and this latter group may be substituted by a C.sub.1-6 alkyl or C.sub.2-6 alkenyl group; or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4, together with the adjacent nitrogen atom and optionally with an additional oxygen or nitrogen atom, form a 4- to 6-membered, saturated or unsaturated cyclic group which may be substituted by a C.sub.1-6 alkyl or C.sub.2-6 alkenyl group; two of X, Y and Z are nitrogen whereas the third of them means a methine group; n is 1 or 2; W means oxygen or two hydrogen atoms; and the wavy line means .alpha.-/.alpha.-, .alpha.-/.beta.- or .beta.-/.alpha.- steric position, as well as their acid addition salts and solvates. The invention further relates to pharmaceutical compositions containing the above compounds as well as a process for preparing the compounds of formula (I). The compounds of formula (I) possess antioxidant effect and therefore, they are useful for inhibiting the peroxidation of lipids occurring in mammals (including human).

    摘要翻译: PCT No.PCT / Hu93 / 00036 Sec。 371日期1994年12月8日第 102(e)日期1994年12月8日PCT提交1993年6月8日PCT公布。 出版物WO93 / 25550 本发明涉及式(I)的新颖白蛋白衍生物:其中R 1和R 2以及R 3和R 4彼此独立地代表氢,C 2-6烷基 ,C 2-6烯基; 或含有1〜3个环的C 3〜10环亚烷基,后者可以被C 1-6烷基或C 2-6烯基取代; 或R 1和R 2和/或R 3和R 4与相邻的氮原子以及任选的另外的氧或氮原子一起形成可被C 1-6烷基取代的4-至6-元饱和或不饱和的环状基团 或C 2-6烯基; X,Y和Z中的两个是氮,而第三个是次甲基; n为1或2; W表示氧或两个氢原子; 波浪线表示α - /α - ,α - /β - 或β - / - - - 立体位置,以及它们的酸加成盐和溶剂合物。 本发明还涉及含有上述化合物的药物组合物以及制备式(I)化合物的方法。 式(I)化合物具有抗氧化作用,因此它们可用于抑制哺乳动物(包括人)中发生的脂质的过氧化反应。

    N-substituted isoquinoline derivatives and pharmaceutical compositions
containing them
    37.
    发明授权
    N-substituted isoquinoline derivatives and pharmaceutical compositions containing them 失效
    N-取代的异喹啉衍生物和含有它们的药物组合物

    公开(公告)号:US4668688A

    公开(公告)日:1987-05-26

    申请号:US664770

    申请日:1984-10-25

    CPC分类号: C07D217/16

    摘要: The invention relates to new N-substituted bis(hydroxymethyl)-methyl-isoquinoline derivatives of the formula (I), ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,the dotted line is an optional double bond in the 1,2-position,R.sup.3 is alkyl having from 1 to 6 carbon atoms or aralkyl containing from 1 to 4 carbon atoms in the alkyl moiety, or--if there is a single bond in the 1,2-position--represents a group of the formula ##STR2## in which X is oxygen ifR.sup.4 is alkyl having from 1 to 5 carbon atoms, alkoxy having from 1 to 4 carbon atoms, hydroxyl, phenyl or substituted phenyl; orX is oxygen or sulfur ifR.sup.4 is an --NH.sub.2, --NH--C.sub.1-4 -alkyl, --NH--C.sub.3-6 -cycloalkyl, --NH-phenyl or --NH--C.sub.1-4 -alkyl-phenyl group; andR.sup.5 and R.sup.6 independently stand for hydrogen, alkyl having from 1 to 4 carbon atoms or phenyl, with the proviso that at least one of them is other than phenyl,and salts thereof. Processes for the preparation of these compounds and pharmaceutical compositions are also within the scope of the invention.

    摘要翻译: 本发明涉及式(I)的新的N-取代双(羟甲基) - 甲基 - 异喹啉衍生物,其中R1和R2代表羟基或具有1-6个碳原子的烷氧基,虚线是 在1,2-位上的任选的双键,R3是具有1至6个碳原子的烷基或在烷基部分含有1至4个碳原子的芳烷基,或 - 如果1,2-二烷基中存在单键, 位置 - 表示如果R 4是具有1至5个碳原子的烷基,具有1至4个碳原子的烷氧基,羟基,苯基或取代的苯基,其中X是氧的式“IMAGE”的基团; 如果R 4是-NH 2,-NH-C 1-4 - 烷基,-NH-C 3-6 - 环烷基,-NH-苯基或-NH-C 1-4 - 烷基 - 苯基,则X是氧或硫; 并且R 5和R 6独立地代表氢,具有1至4个碳原子的烷基或苯基,条件是它们中的至少一个不是苯基,及其盐。 用于制备这些化合物和药物组合物的方法也在本发明的范围内。

    E-Homo-eburnane derivatives, process for their preparation, and
pharmaceutical compositions containing these compounds
    40.
    发明授权
    E-Homo-eburnane derivatives, process for their preparation, and pharmaceutical compositions containing these compounds 失效
    E-Homo-eburnane衍生物,其制备方法和含有这些化合物的药物组合物

    公开(公告)号:US4481204A

    公开(公告)日:1984-11-06

    申请号:US509150

    申请日:1983-06-29

    CPC分类号: C07D471/22

    摘要: The invention relates to racemic or optically active E-homo-eburnane derivatives of the formula /I/, ##STR1## wherein R.sup.1 and R.sup.2 independently represent an alkyl group having 1 to 6 carbon atoms,and acid addition salts thereof.The new compounds are pharmaceutically active, for example their certain representatives, in particular from the cis-series, show antidepressive activity, while others, especially the compounds of the trans-series, are potent anthypoxial agents. The compounds of the formula /I/ and pharmaceutically acceptable acid addition salts thereof can therefore be employed as active ingredients of pharmaceutical compositions.

    摘要翻译: 本发明涉及式/ I /,其中R 1和R 2独立地表示具有1至6个碳原子的烷基的式/ I /,/ IMAGE / I / C的外消旋或光学活性的E-均 - burn烷衍生物及其酸加成盐。 新化合物是药学上活性的,例如它们的特定代表,特别是顺式的化合物显示出抗抑郁活性,而其它代表,特别是反式系列的化合物是有效的抗氧化剂。 因此,式/ I /的化合物及其药学上可接受的酸加成盐可用作药物组合物的活性成分。