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1. 发明授权

US5418238A 17.beta.-substituted 4-aza-5.alpha.-androstan-3-one derivatives 失效
标题翻译： 17β-取代的4-氮杂-5α-雄甾烷-3-酮衍生物
公开(公告)号：US5418238A
公开(公告)日：1995-05-23
申请号：US98935
申请日：1993-07-29
申请人： Achille Panzeri , Marcella Nesi , Enrico di Salle
发明人： Achille Panzeri , Marcella Nesi , Enrico di Salle
IPC分类号： A61K31/58 , C07J73/00 , C12N9/99
CPC分类号： C07J73/005
摘要： A compound of formula (I): ##STR1## wherein R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group;A is a single bond or a straight or branched C.sub.1 -C.sub.6 alkylene chain;R.sub.1 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group;R.sub.2 is a C.sub.1 -C.sub.6 alkyl group, a C.sub.5 -C.sub.7 cycloalkyl or a C.sub.6 -C.sub.10 cycloalkylalkyl group, aryl or a C.sub.7 -C.sub.10 arylalkyl group, or a C.sub.6 -C.sub.10 heterocyclylalkyl group;R.sub.3 is hydrogen, a C.sub.1 -C.sub.4 alkyl group or an aryl or a C.sub.7 -C.sub.10 arylalkyl group;Z is a C.sub.1 -C.sub.6 alkyl group, an --OR.sub.5 group wherein R.sub.5 is a C.sub.1 -C.sub.6 alkyl group, ##STR2## group wherein each of R.sub.6 and R.sub.7 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl or R.sub.6 and R.sub.7 taken together with the nitrogen to which they are linked form a pentatomic or hexatomic saturated heteromonocyclic ring; and the symbol represents a single or a double bond, is a testosterone 68 5.alpha.-reductase inhibitor and is therapeutically useful in benign prostatic hyperplasia, prostatic and breast cancers, seborrhoea, female hirsutism and male pattern baldness.
摘要翻译：式（I）的化合物：其中R是氢原子或C 1 -C 4烷基; A是单键或直链或支链C1-C6亚烷基链; R1是氢原子或C1-C6烷基; R2是C1-C6烷基，C5-C7环烷基或C6-C10环烷基烷基，芳基或C7-C10芳基烷基或C6-C10杂环基烷基; R3是氢，C1-C4烷基或芳基或C7-C10芳烷基; Z是C1-C6烷基，其中R5是C1-C6烷基的-OR5基团，其中R6和R7各自是氢，C1-C6烷基，C5-C7环烷基，苯基或R6和 R7与它们所连接的氮一起形成五原子或六原子饱和杂单环; 符号表示单键或双键，是睾酮685α-还原酶抑制剂，可用于良性前列腺增生，前列腺和乳腺癌，皮脂溢，女性多毛症和男性型秃发。

2. 发明授权

US4840943A Androst-4-ene-3,17-diones and process for their preparation 失效
标题翻译：雄甾-4-烯-3,17-二酮及其制备方法
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.

3. 发明授权

US4810423A 1,2-beta-methylene-4-substituted androstene-3,17-dione derivatives and process for their preparation 失效
标题翻译： 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.

4. 发明授权

US4757061A 4-amino androstendione derivatives and process for their preparation 失效
标题翻译： 4-氨基雄甾烯二酮衍生物及其制备方法
公开(公告)号：US4757061A
公开(公告)日：1988-07-12
申请号：US828637
申请日：1986-02-10
申请人： Franco Faustini , Roberto D'Alessio , Vittoria Villa , Enrico di Salle , Paolo Lombardi
发明人： Franco Faustini , Roberto D'Alessio , Vittoria Villa , Enrico di Salle , Paolo Lombardi
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。

5. 发明授权

US6114345A Phenylsubstituted 4-azasteroid fluoroderivatives 失效
标题翻译：苯基取代的4-azasteroid氟代衍生物
公开(公告)号：US6114345A
公开(公告)日：2000-09-05
申请号：US300454
申请日：1999-04-28
申请人： Achille Panzeri , Marcella Nesi , Enrico Di Salle
发明人： Achille Panzeri , Marcella Nesi , Enrico Di Salle
IPC分类号： A61K31/58 , A61P43/00 , C07J73/00
CPC分类号： C07J73/005
摘要： Compounds of formula (I), wherein: the symbol ---- represents a single or a double bond; R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; R.sub.f and R'.sub.f, each independently, are C.sub.1 -C.sub.4 alkyl groups substituted by one or more fluorine atoms; and R.sub.1 and R.sub.2, each independently, are selected from: a hydrogen atom; a phenyl group; a C.sub.1 -C.sub.4 alkyl group unsubstituted or substituted by one or more fluorine atoms; a halogen atom; a cyano (CN) group; a group OR.sub.4, wherein R.sub.4 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; a group SR.sub.5, wherein R.sub.5 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; and a group COR.sub.6, wherein R.sub.6 is a group OR.sub.4 in which R.sub.4 is as defined above or a C.sub.1 -C.sub.4 alkyl group unsubstituted or substituted by one or more fluorine atoms. They are useful as testosterone 5a-reductase inhibitors.
摘要翻译：式（I）的化合物，其中：符号+ E，uns ---- + EE表示单键或双键; R是氢原子或C 1 -C 4烷基; Rf和R'f各自独立地是被一个或多个氟原子取代的C 1 -C 4烷基; 并且R 1和R 2各自独立地选自：氢原子; 苯基; 未被取代或被一个或多个氟原子取代的C 1 -C 4烷基; 卤素原子; 氰基（CN）基团; OR 4，其中R 4是氢原子或C 1 -C 4烷基; 基团SR5，其中R5是氢原子或C1-C4烷基; 和基团COR6，其中R6是其中R4如上定义的基团OR4或未被取代或被一个或多个氟原子取代的C 1 -C 4烷基。它们可用作睾酮5a还原酶抑制剂。

6. 发明授权

US5407939A Fluorinated 17 .beta.-substituted 4-aza-5 .alpha.-androstan-3-one derivatives 失效
标题翻译：氟化17β-取代的4-氮杂-5α-雄甾烷-3-酮衍生物
公开(公告)号：US5407939A
公开(公告)日：1995-04-18
申请号：US98729
申请日：1993-07-29
申请人： Achille Panzeri , Marcella Nesi , Enrico Di Salle
发明人： Achille Panzeri , Marcella Nesi , Enrico Di Salle
IPC分类号： A61K31/58 , A61P5/28 , A61P17/00 , A61P17/08 , A61P17/14 , A61P35/00 , C07J73/00 , C12N9/99 , A61K31/47
CPC分类号： C07J73/005
摘要： Compounds of formula (I) ##STR1## wherein: the symbol represents a single or a double bond;B is a bond or a straight or branched C.sub.1 -C.sub.6 alkylene chain;R is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or benzyl;R.sub.2 isa) hydrogen, fluorine, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl or C.sub.6 -C.sub.9 cycloalkylalkyl; orb) aryl or C.sub.7 -C.sub.10 arylalkyl;R.sub.3 isa) hydrogen, fluorine or C.sub.1 -C.sub.4 alkyl; orb) aryl or C.sub.7 -C.sub.10 arylalkyl;R.sub.4 is hydrogen, fluorine, or is absent when Y is a double bond;R.sub.5 is hydrogen, fluorine or C.sub.1 -C.sub.6 alkyl; and when Y is a single bond, A is hydrogen, fluorine or ##STR2## wherein each of R.sub.6, R.sub.7 and R.sub.8 independently is hydrogen, fluorine or C.sub.1 -C.sub.6 alkyl; and when Y is a double bond, A is a ##STR3## wherein each of R.sub.6 and R.sub.7 is independently hydrogen, fluorine or C.sub.1 -C.sub.6 alkyl; with the proviso that at least one of the groups R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 or A contains at least one fluorine atom.
摘要翻译：式（I）化合物其中：符号表示单键或双键; B是键或直链或支链C1-C6亚烷基链; R是氢或C 1 -C 4烷基; R1是氢，C1-C6烷基或苄基; R2是a）氢，氟，C1-C6烷基，C5-C7环烷基或C6-C9环烷基烷基; 或b）芳基或C7-C10芳基烷基; R3是a）氢，氟或C1-C4烷基; 或b）芳基或C7-C10芳基烷基; R4是氢，氟，或当Y是双键时不存在; R5是氢，氟或C1-C6烷基; 当Y是单键时，A是氢，氟或者其中R6，R7和R8各自独立地是氢，氟或C1-C6烷基; 当Y是双键时，A是一个，其中R6和R7各自独立地是氢，氟或C1-C6烷基; 条件是基团R，R 1，R 2，R 3，R 4，R 5或A中的至少一个含有至少一个氟原子。

7. 发明授权

US5155107A 17.beta.-substituted-4-aza-5.alpha.-androstan-3-one derivatives and process for their preparation 失效
标题翻译： 17（BETA）-SUBSTITUTED-4-AZA-5（ALPHA）-ANDROSTAN-3-ONE衍生物及其制备方法
公开(公告)号：US5155107A
公开(公告)日：1992-10-13
申请号：US650970
申请日：1991-02-05
申请人： Achille Panzeri , Enrico Di Salle , Marcella Nesi
发明人： Achille Panzeri , Enrico Di Salle , Marcella Nesi
IPC分类号： A61K31/56 , A61K31/58 , A61P35/00 , C07J20060101 , C07J73/00
CPC分类号： C07J73/005
摘要： The present invention concerns steroidic 5.alpha.-reductase inhibitors having the formula: ##STR1## As a result of their 5.alpha.-reductase inhibiting activity, these compounds are useful in the treatment of androgen dependent conditions and diseases.
摘要翻译：本发明涉及具有下式的类固醇5α-还原酶抑制剂：作为其5α-还原酶抑制活性的结果，这些化合物可用于治疗雄激素依赖性病症和疾病。

8. 发明授权

US4824830A 6- or 7-methylenandrosta-1,4-diene-3,17-dione derivatives and process for their preparation 失效
标题翻译： 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
申请人： Franco Buzzetti , Natale Barbugian , Paolo Lombardi , Enrico di Salle
发明人： Franco Buzzetti , Natale Barbugian , Paolo Lombardi , Enrico di Salle
IPC分类号： A61K31/565 , A61P35/00 , C07J1/00 , C07J21/00 , C07J71/00 , A61K31/56
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.

9. 发明授权

US4808578A 6-Alkylidene 10 .beta.-alkynylestrene derivatives and pharmaceutical methods for their use 失效
标题翻译： 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
申请人： Franco Faustini , Enrico di Salle , Vittoria Villa , Paolo Lombardi
发明人： Franco Faustini , Enrico di Salle , Vittoria Villa , Paolo Lombardi
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。

10. 发明授权

US4151283A 6-Methyl-and 1,6-dimethyl-8.beta.-carbobenzyloxy-aminomethyl-10.alpha.-ergoline as inhibitors of prolactin secretion 失效
标题翻译： 6-甲基 - 和1,6-二甲基-8（62-羰基苄氧基 - 氨基甲基-10（60-麦角灵）作为催乳素分泌的抑制剂
公开(公告)号：US4151283A
公开(公告)日：1979-04-24
申请号：US810872
申请日：1977-06-28
申请人： Enrico DI Salle , Claudio Praga , Erminia Castegnaro
发明人： Enrico DI Salle , Claudio Praga , Erminia Castegnaro
IPC分类号： C07D457/02
CPC分类号： C07D457/02
摘要： A method is disclosed for inhibiting prolactin secretion in a female mammal which comprises administering to the mammal an effective dose of 6-methyl-8.beta.-carbobenzyloxy-aminomethyl-10.alpha.-ergoline, or 1,6-dimethyl-8.beta.-carbobenzyloxy-aminomethyl-10.alpha.-ergoline, or a pharmaceutically acceptable acid addition salt thereof.
摘要翻译：公开了一种用于抑制雌性哺乳动物中的催乳素分泌的方法，其包括向哺乳动物施用有效剂量的6-甲基-8β-羰基苄氧基 - 氨基甲基-10α-麦角蛋白或1,6-二甲基-8β-苄氧羰基 - 氨基甲基-10α-麦角林，或其药学上可接受的酸加成盐。

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