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1.发明授权6- or 7-methylenandrosta-1,4-diene-3,17-dione derivatives and process for their preparation 失效6-或7-亚甲基雄甾-1,4-二烯-3,17-二酮衍生物及其制备方法
公开(公告)号：US4824830A
公开(公告)日：1989-04-25
申请号：US070685
申请日：1987-07-07
CPC分类号： C07J21/008 , C07J1/0011 , C07J71/001
摘要： The invention relates to new 6- or 7-methylenandrosta-1,4-diene-3,17-diones of the following formula ##STR1## wherein R is hydrogen or fluorine; R.sub.1 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.2 is hydrogen or halogen; one of R.sub.3 and R.sub.4 is .dbd.CH.sub.2 and the other is hydrogen or C.sub.1 -C.sub.4 alkyl, and when R.sub.3 is .dbd.CH.sub.2, at least one of R and R.sub.4 is other than hydrogen; and the symbol ##STR2## represents a double bond and the symbol ##STR3## represents a single bond when R.sub.3 is .dbd.CH.sub.2 or the symbol ##STR4## represents a single bond and the symbol ##STR5## represents a double bond when R.sub.4 is .dbd.CH.sub.2, which are useful in therapy, in particular as anti-cancer agents.
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公开(公告)号：US4904650A
公开(公告)日：1990-02-27
申请号：US225674
申请日：1988-07-26
IPC分类号： A61K31/565 , A61P13/02 , A61P15/00 , A61P35/00 , C07J1/00
CPC分类号： C07J1/0011
摘要： The invention relates to 6-alkylidenadrosta-1,4-diene-3,17-dione derivatives, having the following general formula ##STR1## wherein each of R and R.sub.2, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sub.1 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl, which are useful in therapy, in particular in the treatment of hormone-dependent cancers.
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3.发明授权4-substituted 6-alkylidenandrosteine-3,17-dione derivatives and process for their preparation 失效4-取代的6-亚烷基亚磺酰-3,17-二酮衍生物及其制备方法
公开(公告)号：US4822528A
公开(公告)日：1989-04-18
申请号：US86608
申请日：1987-08-18
IPC分类号： A61K31/565 , A61P35/00 , C07J1/00 , C07J31/00 , C07J41/00 , C07J71/00 , C07C117/00
CPC分类号： C07J41/0005 , C07J1/0011 , C07J31/003 , C07J71/001
摘要： The invention relates to 4-substituted 6-alkylidenandrostene-3,17-dione derivatives of the following formula ##STR1## wherein each of R.sub.1, R.sub.2 and R.sub.3 is, independently, hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.4 is hydrogen of fluorine; (x) represents a single or double bond; and R is, especially, a hydroxy or mercapto or amino group or a functional derivative thereof. The compounds of the invention show aromatase inhibitory activity and may be useful, for instance, in the treatment of hormone-dependent tumors and of prostatic hyperplasia.
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公开(公告)号：US4808616A
公开(公告)日：1989-02-28
申请号：US882364
申请日：1986-07-07
CPC分类号： C07J1/0011
摘要： The invention relates to 6-alkylidenandrosta-1,4-diene-3,17-dione derivatives, having the following general formula ##STR1## wherein each of R and R.sub.2, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sub.1 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl, which are useful in therapy, in particular in the treatment of hormone-dependent cancers.
摘要翻译： 本发明涉及6-亚烷基雄甾-1,4-二烯-3,17-二酮衍生物，具有以下通式：其中R和R 2各自独立地是氢或C 1 -C 6烷基，R 1是氢， 卤素或C 1 -C 6烷基，其可用于治疗，特别是用于激素依赖性癌症的治疗。
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公开(公告)号：US4840943A
公开(公告)日：1989-06-20
申请号：US061663
申请日：1987-06-15
申请人： Franco Buzzetti , Enrico di Salle , Paolo Lombardi
发明人： Franco Buzzetti , Enrico di Salle , Paolo Lombardi
IPC分类号： A61K31/565 , A61P35/00 , C07J1/00 , C07J53/00
CPC分类号： C07J53/005
摘要： The present invention relates to new 6-substituted 1.2.beta.methylenandrost-4-ene-3,17-diones of the following general formula: ##STR1## wherein one of R.sub.1 and R.sub.2 is hydrogen and the other is halogen, amino or azido, or R.sub.1 and R.sub.2, taken together, form a .dbd.CH.sub.2 or .dbd.O group, and, when one of R.sub.1 and R.sub.2 is amino, the pharmaceutically acceptable salts thereof.The compounds of the invention are useful in therapy, in particular as anti-cancer agents.
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6.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.
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7.发明授权6-Alkylidene 10 .beta.-alkynylestrene derivatives and pharmaceutical methods for their use 失效6-亚烷基10β-炔雌醇衍生物及其使用的药物方法
公开(公告)号：US4808578A
公开(公告)日：1989-02-28
申请号：US941348
申请日：1986-12-15
IPC分类号： A61K31/565 , A61P35/00 , C07J1/00 , C07J21/00 , C07J41/00 , C07J71/00 , C10L1/32 , A61K31/56
CPC分类号： C07J1/0011 , C07J1/0022 , C07J21/006 , C07J41/0011 , C07J41/0027 , C07J71/001
摘要： The invention relates to 6-substituted 10.beta.-alkynylestrene derivatives wherein the 6 substituent is amino, azido, halogen or an alkylidene group and to corresponding 6,7-dihalo analogs.The invention provides also a process for the preparation of the above compounds and pharmaceutical compositions containing same.The compounds of the invention are useful aromatase inhibitors and can be used, e.g., in the treatment of hormone-dependent tumors and prostatic hyperplasia.
摘要翻译： 本发明涉及6-取代的10β-炔雌醇衍生物，其中6个取代基是氨基，叠氮基，卤素或亚烷基，以及相应的6,7-二卤代类似物。 本发明还提供了制备上述化合物的方法和含有它们的药物组合物。 本发明的化合物是有用的芳香酶抑制剂，可用于例如激素依赖性肿瘤和前列腺增生的治疗。
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8.发明授权Cycloalkyl-substituted 4-aminophenyl halo derivatives and process for their preparation 失效环烷基取代的4-氨基苯基卤衍生物及其制备方法
公开(公告)号：US4847295A
公开(公告)日：1989-07-11
申请号：US142207
申请日：1988-01-11
申请人： Angelo Crugnola , Enrico di Salle , Paolo Lombardi
发明人： Angelo Crugnola , Enrico di Salle , Paolo Lombardi
IPC分类号： C12N9/99 , A61K20060101 , A61K31/13 , A61K31/135 , A61K31/16 , A61K31/165 , A61K31/195 , A61K31/205 , A61K31/215 , A61K31/24 , A61P35/00 , A61P43/00 , C07C20060101 , C07C67/00 , C07C209/00 , C07C209/36 , C07C209/50 , C07C209/68 , C07C211/44 , C07C211/45 , C07C211/53 , C07C213/00 , C07C217/76 , C07C221/00 , C07C225/22 , C07C227/00 , C07C227/04 , C07C227/18 , C07C229/10 , C07C229/42 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/00 , C07C233/08 , C07C233/12 , C07C237/20 , C07C237/38 , C07F13/00
CPC分类号： C07C205/45 , C07C211/52 , C07C217/76 , C07C225/22 , C07C229/42 , C07C237/20 , C07C2101/08 , C07C2101/14
摘要： The invention relates to cycloalkyl substituted 4-aminophenyl halo derivatives of formula (I) ##STR1## wherein n is an integer of 1 to 5;A is >C.dbd.O or --CH.sub.2 -- and B is, independently, --O--, --NH-- or --CH.sub.2 --; andeither R is halogen and R.sub.1 is unsubstituted C.sub.1 -C.sub.4 alkyl; or R is hydrogen and R.sub.1 is C.sub.1 -C.sub.4 alkyl substituted by 1 to 4 halogen atoms,including the pharmaceutically acceptable salts thereof. The compounds of the invention show aromatase inhibiting activity and can find use, for example, in the treatment of estrogen-dependent tumors and of prostatic hyperplasia.
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公开(公告)号：US4757061A
公开(公告)日：1988-07-12
申请号：US828637
申请日：1986-02-10
IPC分类号： A61K31/565 , A61K31/58 , A61P3/00 , A61P35/00 , C07J1/00 , C07J17/00 , C07J31/00 , C07J33/00 , C07J41/00 , C07J43/00 , A61K31/56
CPC分类号： C07J41/0005 , C07J41/0027
摘要： The invention discloses 4-substituted androstendione derivatives of the following formula (I) ##STR1## wherein R is amino or substituted amino or azido,one of R.sub.1 and R.sub.2 is hydrogen and the other is hydrogen, alkyl, alkenyl or alkynyl, and(x) and (y) are each, independently, a single bond or a double bond.The compounds of formula (I) are useful aromatase inhibitors.
摘要翻译： 本发明公开了下式（I）的4-取代的雄烯二酮衍生物：其中R是氨基或取代的氨基或叠氮基，R1和R2之一是氢，另一个是氢，烷基，烯基或炔基， 和（x）和（y）各自独立地为单键或双键。 式（I）化合物是有用的芳香酶抑制剂。
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公开(公告)号：US4873233A
公开(公告)日：1989-10-10
申请号：US242855
申请日：1988-09-12
申请人： Vittoria Villa , Enrico di Salle , Paolo Lombardi
发明人： Vittoria Villa , Enrico di Salle , Paolo Lombardi
CPC分类号： C07J31/006 , C07J1/0022 , C07J17/00 , C07J71/001 , Y02P20/55
摘要： The invention relates to new 17-hydroxy androsta-1,4-diene-3-one derivatives of the following formula ##STR1## wherein each of R and R.sub.3, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.1 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.4 is hydrogen or fluorine;R.sub.5 is (a) hydrogen or C.sub.1 -C.sub.6 alkyl; (b) phenyl unsubstituted or substituted by one or two substituents independently chosen from C.sub.1 -C.sub.6 alkyl, halogen and amino; (c) an acyl group; or (d) a hydroxy protecting group; and the pharmaceutically acceptable salts thereof,which are useful in therapy, in particular as anti-cancer agents.
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