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1. 发明授权

US4771043A Steroidic aromatase inhibitors 失效
标题翻译：类固醇芳香酶抑制剂
公开(公告)号：US4771043A
公开(公告)日：1988-09-13
申请号：US887438
申请日：1986-07-21
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 , A61P5/00 , A61P13/02 , A61P15/00 , A61P35/00 , A61P35/02 , C07J1/00 , C07J41/00 , C12N9/99 , A61K31/56
CPC分类号： C07J41/0005 , C07J1/0011 , C07J41/0027
摘要： The invention relates to 6-substituted androsta-1,4-diene-3,17-dione derivatives wherein the 6 substituent is an azido, amino or substituted amino group.The invention provides also a process for preparing the said 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.
摘要翻译：本发明涉及6-取代的雄甾-1,4-二烯-3,17-二酮衍生物，其中6个取代基是叠氮基，氨基或取代的氨基。本发明还提供了制备所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族酶抑制剂，可用于例如激素依赖性肿瘤的治疗。

2. 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。

3. 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。

4. 发明授权

US4543353A Ester and amide derivatives of 13,14-didehydro prostaglandins 失效
标题翻译： 13,14-二脱氢前列腺素的酯和酰胺衍生物
公开(公告)号：US4543353A
公开(公告)日：1985-09-24
申请号：US436419
申请日：1982-10-25
申请人： Franco Faustini , Vittoria Villa , Carmelo Gandolfi , Enrico Di Salle
发明人： Franco Faustini , Vittoria Villa , Carmelo Gandolfi , Enrico Di Salle
IPC分类号： A61K31/557 , A61K31/5575 , A61P13/02 , A61P15/00 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D231/12 , C07D233/02 , C07D295/18 , C07C177/00
CPC分类号： C07C405/0041 , C07C405/00
摘要： Esters of 13,14-didehydro prostaglandins have been prepared.
摘要翻译：已经制备了13,14-didehydro前列腺素的酯。

5. 发明授权

US4626597A 16-fluoro-16,17-didehydro prostanoids and process for their preparation 失效
标题翻译： 16-氟-16,17-二氢前列腺素类及其制备方法
公开(公告)号：US4626597A
公开(公告)日：1986-12-02
申请号：US643014
申请日：1984-08-22
申请人： Franco Faustini , Roberto d'Alessio , Achille Panzeri , Enrico di Salle
发明人： Franco Faustini , Roberto d'Alessio , Achille Panzeri , Enrico di Salle
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D207/32 , C07D207/333 , C07D207/337 , C07D213/30 , C07D213/55 , C07D241/12 , C07D261/08 , C07D307/42 , C07D307/54 , C07D309/12 , C07D333/24 , C07C177/00
CPC分类号： C07D207/337 , C07C405/00 , C07C405/0033 , C07C405/0041 , C07D213/55 , C07D241/12 , C07D261/08 , C07D307/54 , C07D333/24
摘要： 16-Fluoro-16,17-didehydro prostanoids, processes for their preparation, compositions containing them and methods of using them are disclosed. The compounds and compositions have pharmaceutical utility including, for example, luteolytic activity.
摘要翻译：公开了16-氟-16,17-二氢前列腺素类，其制备方法，含有它们的组合物及其使用方法。化合物和组合物具有药物效用，包括例如溶血活性。

6. 发明授权

US4585791A Furyl derivatives of 16-substituted prostaglandins 失效
标题翻译： 16取代前列腺素的呋喃衍生物
公开(公告)号：US4585791A
公开(公告)日：1986-04-29
申请号：US667367
申请日：1984-11-01
申请人： Franco Faustini , Achille Panzeri , Fabrizio Orzi , Enrico di Salle , Roberto Ceserani
发明人： Franco Faustini , Achille Panzeri , Fabrizio Orzi , Enrico di Salle , Roberto Ceserani
IPC分类号： C07D307/38 , A61K31/557 , A61P43/00 , C07C67/00 , C07C401/00 , C07D307/54 , C07D307/935 , A61K31/34
CPC分类号： C07D307/935 , C07D307/54
摘要： The present invention relates to new furyl derivatives of 16-substituted prostaglandins, to a process for their preparation and to pharmaceutical and veterinary compositions containing them.The new compounds of the invention are optically active or racemic prostaglandins of the following formula (I) ##STR1## wherein R is(1) --OH or --OR' wherein R' is C.sub.1 -C.sub.6 alkyl optionally substituted by phenyl or by a monocycloalkyl group or by a pentatomic or hexatomic heteromonocyclic ring containing at least one heteroatom chosen from O, S and N;(2) ##STR2## wherein each of R" and R"', is independently, hydrogen; C.sub.1 -C.sub.6 alkyl; phenyl; or a pentatomic or hexatomic heteromonocyclic ring containing at least one heteroatom chosen from O, S and N; or R" and R"', together with the nitrogen atom to which they are linked, form a pentatomic or hexatomic heteromonocyclic ring optionally containing a further heteroatom chosen from O, S and N;(3) --W--(CH.sub.2).sub.n --X wherein W is --O-- or --NH--, n is an integer of 1 to 4 and X represents a group --OR' or a group ##STR3## wherein R', R" and R"' are as defined above;one of R.sub.1 and R.sub.2 is hydrogen and the other is hydroxy orR.sub.1 and R.sub.2, taken together, form an oxo group;one of R.sub.3 and R.sub.4 is hydrogen and the other is hydroxy;one of R.sub.5 and R.sub.6 is hydroxy and the other is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, or phenyl;one of R.sub.7 and R.sub.8 is hydrogen and the other is a C.sub.1 -C.sub.4 alkyl or tri-halo-C.sub.1 -C.sub.4 alkyl group;m is an integer of 1 to 3;R.sub.9 is a 2-furyl or 3-furyl group, optionally substituted by one or more substituents chosen from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, tri-halo-C.sub.1 -C.sub.4 alkyl and halogen; and the symbol represents a single bond or a cis double bond.
摘要翻译：本发明涉及16-取代的前列腺素的新呋喃衍生物，其制备方法和含有它们的药物和兽药组合物。本发明的新化合物是下式（I）的光学活性或外消旋前列腺素其中R是（1）-OH或-OR'，其中R'是任选被苯基取代的C 1 -C 6烷基或通过单环烷基或含有至少一个选自O，S和N的杂原子的五原子或六原子杂单环; （2）其中R“和R”'各自独立地为氢; C1-C6烷基; 苯基; 或含有至少一个选自O，S和N的杂原子的五原子或六原子杂单环; 或R“和R”'与它们所连接的氮原子一起形成任选地含有选自O，S和N的另外的杂原子的五原子或六原子异单环; （3）-W-（CH2）nX其中W是-O-或-NH-，n是1至4的整数，X表示基团-OR'或基团，其中R'，R“ 和R“'如上所定义; R 1和R 2之一是氢，另一个是羟基或R 1和R 2一起形成氧代基; R3和R4之一是氢，另一个是羟基; R 5和R 6之一是羟基，另一个是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或苯基; R 7和R 8中的一个是氢，另一个是C 1 -C 4烷基或三卤代-C 1 -C 4烷基; m为1〜3的整数。 R9是2-呋喃基或3-呋喃基，任选被一个或多个选自C 1 -C 4烷基，C 1 -C 4烷氧基，三卤代-C 1 -C 4烷基和卤素的取代基取代; 符号表示单键或顺式双键。

7. 发明授权

US4293705A 13,14-Dehydro-11-deoxy-prostaglandins and process for their preparation 失效
标题翻译： 13,14-脱氢-11-脱氧前列腺素及其制备方法
公开(公告)号：US4293705A
公开(公告)日：1981-10-06
申请号：US122276
申请日：1980-02-19
申请人： Carmelo Gandolfi , Renato Pellegata , Franco Faustini , Angelo Fumagalli
发明人： Carmelo Gandolfi , Renato Pellegata , Franco Faustini , Angelo Fumagalli
IPC分类号： C07C405/00 , C07D307/935 , C07D309/12 , C07D319/12 , C07F9/54 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07D309/12 , C07D319/12 , C07F9/5407
摘要： Novel optically active 13,14-dehydro-11-deoxy-prostaglandins having a phenyl or substituted-phenyl group on the lower side chain are disclosed.
摘要翻译：公开了在下侧链上具有苯基或取代苯基的新型光学活性13,14-脱氢-11-脱氧前列腺素。

8. 发明授权

US4303670A Bicyclic prostaglandins and process for their preparation 失效
标题翻译：双环前列腺素及其制备方法
公开(公告)号：US4303670A
公开(公告)日：1981-12-01
申请号：US29925
申请日：1979-04-13
申请人： Carmelo Gandolfi , Carlo Passarotti , Alessandro Andreoni , Angelo Fumagalli , Franco Faustini , Roberto Ceserani , Maria M. Usardi
发明人： Carmelo Gandolfi , Carlo Passarotti , Alessandro Andreoni , Angelo Fumagalli , Franco Faustini , Roberto Ceserani , Maria M. Usardi
IPC分类号： A61K31/31 , A61K31/41 , A61P43/00 , C07C405/00 , C07D307/935 , C07D307/937 , C07D407/12 , A61K31/557 , A61K31/34
CPC分类号： C07D307/937 , C07C405/00 , Y10S514/822 , Y10S514/826 , Y10S514/926 , Y10S514/927 , Y10S514/929
摘要： Bicyclic prostaglandins and pharmaceutical and veterinary compositions containing them having numerous pharmaceutical or veterinary utilities, including, for example, hypotensive, vasodilatory, anti-aggregating, luteolytic, and cytoprotective activities. Processes for preparing the compounds and compositions are also disclosed.
摘要翻译：双环前列腺素和含有它们的药物和兽药组合物具有许多药物或兽医用途，包括例如降血压，血管扩张，抗聚集，溶血性和细胞保护活性。还公开了制备化合物和组合物的方法。

9. 发明授权

US4271184A Bicyclic prostaglandins 失效
标题翻译：双环前列腺素
公开(公告)号：US4271184A
公开(公告)日：1981-06-02
申请号：US98963
申请日：1979-11-30
申请人： Carmelo Gandolfi , Carlo Passarotti , Alessandro Andreoni , Angelo Fumagalli , Franco Faustini , Roberto Ceserani , Maria M. Usardi
发明人： Carmelo Gandolfi , Carlo Passarotti , Alessandro Andreoni , Angelo Fumagalli , Franco Faustini , Roberto Ceserani , Maria M. Usardi
IPC分类号： A61K31/31 , A61K31/41 , A61P43/00 , C07C405/00 , C07D307/935 , C07D307/937 , C07D407/12 , A61K31/557
CPC分类号： C07D307/937 , C07C405/00 , Y10S514/822 , Y10S514/826 , Y10S514/926 , Y10S514/927 , Y10S514/929
摘要： Bicyclic prostaglandins and pharmaceutical and veterinary compositions containing them having numerous pharmaceutical or veterinary utilities including, for example, hypotensive, vasodilatory, antiaggregating, luteolytic, and cytoprotective activities. Processes for preparing the compounds and compositions are also disclosed.
摘要翻译：双环前列腺素和含有它们的药物和兽药组合物具有许多药物或兽医用途，包括例如降血压，血管扩张，抗聚集，溶血性和细胞保护活性。还公开了制备化合物和组合物的方法。

10. 发明授权

US4262016A Bicyclic prostaglandins and process for their preparation 失效
标题翻译：双环前列腺素及其制备方法
公开(公告)号：US4262016A
公开(公告)日：1981-04-14
申请号：US49326
申请日：1979-06-18
申请人： Carmelo Gandolfi , Carlo Passarotti , Alessandro Andreoni , Angelo Fumagalli , Franco Faustini , Roberto Ceserani , Maria M. Usardi
发明人： Carmelo Gandolfi , Carlo Passarotti , Alessandro Andreoni , Angelo Fumagalli , Franco Faustini , Roberto Ceserani , Maria M. Usardi
IPC分类号： A61K31/31 , A61K31/41 , A61P43/00 , C07C405/00 , C07D307/935 , C07D307/937 , C07D407/12 , A61K31/35 , C07D311/02
CPC分类号： C07D307/937 , C07C405/00 , Y10S514/822 , Y10S514/826 , Y10S514/926 , Y10S514/927 , Y10S514/929
摘要： Bicyclic Prostaglandins and pharmaceutical and veterinary compositions containing them, having numerous pharmaceutical and veterinary utilities, including for example hypotensive, vasodilatory, anti-aggregating, and anti-thrombotic activities. Methods for preparing the compounds and compositions are also disclosed.
摘要翻译：双环前列腺素和含有它们的药物和兽药组合物，具有许多药物和兽医用途，包括例如降血压，血管扩张，抗凝集和抗血栓形成活性。还公开了制备化合物和组合物的方法。

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