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33 条记录 (耗时 0.019 秒)

    1,2-beta-methylene-4-substituted androstene-3,17-dione derivatives and process for their preparation
    5.
    发明授权
    1,2-beta-methylene-4-substituted androstene-3,17-dione derivatives and process for their preparation 失效
    1,2-β-亚甲基-4-取代雄甾烯-3,17-二酮衍生物及其制备方法

    公开(公告)号：US4810423A

    公开(公告)日：1989-03-07

    申请号：US86607

    申请日：1987-08-18

    申请人： Franco Buzzetti ,  Enrico di Salle ,  Paolo Lombardi

    发明人： Franco Buzzetti ,  Enrico di Salle ,  Paolo Lombardi

    IPC分类号： C07J53/00 ,  C07J71/00 ,  A61K31/56 ,  C07C117/00

    CPC分类号： C07J53/005 ,  C07J71/001 ,  Y02P20/55

    摘要： The invention relates to new aromatase inhibitor agents having the general formula (I) ##STR1## wherein R.sub.1 is hydrogen or a group=CHR.sub.3 wherein R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl; the symbol indicates the presence of a single or double bond in such a way that, when R.sub.1 is hydrogen, (a) is single bond and (b) is either single or double bond, while, when R.sub.1 is a group.dbd.CHR.sub.3 as defined above, (a) is double bond and (b) is single bond; R.sub.2 is hydrogen or fluorine; and R is(1) a group --OR.sub.4 wherein R.sub.4 is(a) hydrogen;(b) C.sub.1 -C.sub.6 alkyl;(c) a phenyl or benzyl group, each unsubstituted or ring-substituted by one or more substituents chosen from C.sub.1 -C.sub.4 alkyl, halogen, trifluoromethyl, nitro, amino, hydroxy and C.sub.1 -C.sub.4 alkoxy;(d) a group--COR.sub.5 wherein R.sub.5 is(i) a C.sub.1 -C.sub.22 saturated or C.sub.2 -C.sub.22 unsaturated aliphatic hydrocarbon radical;(ii) a C.sub.4 -C.sub.7 monocycloalkyl group; or(iii) a phenyl or benzyl group, each unsubstituted or ring substituted as reported above; or(e) a hydroxy protecting group;(2) a group--SR.sub.6 wherein R.sub.6 either has one of the meanings (a) to (d) indicated above for R.sub.4 or is a group --SR.sub.7 wherein R.sub.7 is(iv) C.sub.1 -C.sub.6 alkyl;(v) a phenyl or benzyl group, each unsubstituted or ring-substituted as reported above; or(vi) a steroidic residue of formula ##STR2## wherein R.sub.1, R.sub.2, (a), (b) and the symbol are as defined above; (3) the group --N.sub.3 ; or(4) a group ##STR3## wherein each of R.sub.8 and R.sub.9, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof, which are useful in therapy, in particular, as anti-cancer agents.

    Fluorinated 4-aminoandrostadienone derivatives and process for their preparation
    7.
    发明授权
    Fluorinated 4-aminoandrostadienone derivatives and process for their preparation 失效
    氟化4-氨基雄二烯酮衍生物及其制备方法

    公开(公告)号：US5502044A

    公开(公告)日：1996-03-26

    申请号：US195205

    申请日：1994-02-14

    申请人： Franco Buzzetti ,  Antonio Longo ,  Enrico Di Salle

    发明人： Franco Buzzetti ,  Antonio Longo ,  Enrico Di Salle

    IPC分类号： A61K31/565 ,  C07J1/00 ,  C07J41/00 ,  C07J71/00 ,  A61K31/56

    CPC分类号： C07J41/0005 ,  C07J1/0011 ,  C07J41/0011 ,  C07J41/0027 ,  C07J71/001

    摘要： The present invention relates to a compound of formula (I) ##STR1## wherein (x) and (y) are single or double bonds; A is a ##STR2## R and R.sup.3 are hydrogen or acyl; R.sup.1 is hydrogen or fluorine;and wherein:when (y) is a single bond, R.sup.2 is hydrogen, fluorine methyl, trifluoromethyl;when (y) is a double bond, R.sup.2 is methylene provided that when one of (x) or (y) is a double bond the other is a single bond and at least one of R.sub.1 and R.sub.2 is fluorine or trifluoromethyl or a pharmaceutically acceptable salt thereof. The compounds of formula (I) are useful as aromatase inhibitors.

    摘要翻译： 本发明涉及式（I）化合物，其中（x）和（y）是单键或双键; A是R 1和R 3是氢或酰基; R1是氢或氟; 并且其中：当（y）为单键时，R 2为氢，氟甲基，三氟甲基; 当（y）是双键时，R2是亚甲基，条件是当（x）或（y）中的一个是双键时，另一个是单键，并且R 1和R 2中的至少一个是氟或三氟甲基或药学上可接受的 的盐。 式（I）化合物可用作芳香酶抑制剂。

    Androst-4-eno[4,5-b]pyrrole derivatives
    8.
    发明授权
    Androst-4-eno[4,5-b]pyrrole derivatives 失效
    雄甾-4-烯[4,5-b]吡咯衍生物

    公开(公告)号：US5457097A

    公开(公告)日：1995-10-10

    申请号：US92789

    申请日：1993-07-19

    申请人： Franco Buzzetti ,  Antonio Longo ,  Enrico Di Salle

    发明人： Franco Buzzetti ,  Antonio Longo ,  Enrico Di Salle

    IPC分类号： C12N9/99 ,  A61K31/58 ,  A61P43/00 ,  C07J7/00 ,  C07J51/00 ,  C07J71/00 ,  C07J1/00 ,  A61K31/56

    CPC分类号： C07J71/0042 ,  C07J7/0085

    摘要： This invention refers to compounds of formula (I) ##STR1## wherein x, y, z represent single or double bonds;R is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.1 is hydrogen or an acyl group;R.sub.2 is hydrogen; C.sub.1 -C.sub.4 alkyl unsubstituted or substituted by phenyl; phenyl unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy; andA is a >C.dbd.O, >CH OH or >CH OR.sub.3 group, in which R.sub.3 is an acyl group provided that one of z and y is a double bond and the other is a single bond.The compounds are useful as aromatase inhibitors.

    摘要翻译： 本发明涉及式（I）的化合物：其中x，y，z表示单键或双键; R是氢或C 1 -C 4烷基; R1是氢或酰基; R2是氢; 未被取代或被苯基取代的C 1 -C 4烷基; 未被取代或被C 1 -C 4烷基或C 1 -C 4烷氧基取代的苯基; 并且A是> C = O，> CH OH或> CH OR 3基团，其中R 3是酰基，条件是z和y之一是双键，而另一个是单键。 该化合物可用作芳香酶抑制剂。