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11. 发明授权

US4797411A Cycloalkyl-substituted 4-pyridyl derivatives and use as aromatase inhibitors 失效
标题翻译：环烷基取代的4-吡啶基衍生物并用作芳香酶抑制剂
公开(公告)号：US4797411A
公开(公告)日：1989-01-10
申请号：US72678
申请日：1987-07-13
申请人： Angelo Crugnola , Enrico di Salle , Paolo Lombardi
发明人： Angelo Crugnola , Enrico di Salle , Paolo Lombardi
IPC分类号： C07D213/24 , C07D213/16 , C07D213/18 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/50 , C07D213/55 , C07D213/56 , A61K31/44 , C07D213/26 , C07D213/28
CPC分类号： C07D213/16 , C07D213/18 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/50 , C07D213/55 , C07D213/56
摘要： The invention relates to cycloalkyl-substituted 4-pyridyl derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.4 alkyl;each of R.sub.1 and R.sub.2 is, independently, hydrogen or C.sub.1 -C.sub.4 alkyl;n is an integer of 1 to 5; and either(a) A is >C.dbd.O and B is --O--, --NH-- or --CH.sub.2 --; or(b) A is --CH.sub.2 --and B is --O--, --NH--, --CH.sub.2 -- or >C.dbd.O; or(c) A is --O-- and B is >C.dbd.O or --CH.sub.2 --; or(d) A is --NH-- and B is >C.dbd.O or --CH.sub.2 --,and their pharmaceutically acceptable salts.The compounds of the invention show aromatase inhibiting activity and can be useful, e.g., in treating hormone-dependent tumors and prostatic hyperplasia.
摘要翻译：本发明涉及式（I）的环烷基取代的4-吡啶基衍生物，其中R是C 1 -C 4烷基; R 1和R 2各自独立地为氢或C 1 -C 4烷基; n为1〜5的整数，和（a）A是> C = O，B是-O - ， - NH-或-CH 2 - ; 或（b）A是-CH 2 - ，B是-O - ， - NH - ， - CH 2 - 或> C = O; 或（c）A为-O-，B为> C = O或-CH 2 - ; 或（d）A是-NH-，B是> C = O或-CH 2 - ，及其药学上可接受的盐。本发明的化合物显示芳香酶抑制活性，并且可用于例如治疗激素依赖性肿瘤和前列腺增生。

12. 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。

13. 发明授权

US4769483A Cycloalkyl-substituted 4-aminophenyl derivatives and process for their preparation 失效
标题翻译：环烷基取代的4-氨基苯基衍生物及其制备方法
公开(公告)号：US4769483A
公开(公告)日：1988-09-06
申请号：US902873
申请日：1986-09-02
申请人： Paolo Lombardi , Angelo Crugnola , Enrico di Salle
发明人： Paolo Lombardi , Angelo Crugnola , Enrico di Salle
IPC分类号： C12N9/99 , A61K31/135 , A61K31/165 , A61K31/215 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07C67/00 , C07C201/00 , C07C205/06 , C07C205/42 , C07C205/56 , C07C205/57 , C07C209/00 , C07C209/36 , C07C209/50 , C07C211/45 , C07C213/00 , C07C217/76 , C07C227/00 , C07C227/04 , C07C227/18 , C07C229/42 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/12 , C07C233/62 , C07C237/20 , C07C101/00
CPC分类号： C07C205/56 , C07C205/42 , C07C205/45
摘要： The invention relates to cycloalkyl substituted 4-aminophenyl derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.4 alkyl:n is an integer of 1 to 5; and either(a) A is ##STR2## and B is --O--, --NH-- or --CH.sub.2 --; or (b) A is --CH.sub.2 -- and B is --O--, --NH--, --CH.sub.2 -- or ##STR3## or (c) A is --O-- and B is ##STR4## or --CH.sub.2 --; or (d) A is --NH-- and B is ##STR5## or --CH.sub.2 -- and their pharmaceutically acceptable salts.The scope of the invention includes also a process for preparing the said compounds of formula (I) and pharmaceutical compositions containing same.The compounds of the invention show aromatase inhibiting activity and can be useful, e.g., in treating hormone-dependent tumors and prostatic hypertrophy or hyperplasia.
摘要翻译：本发明涉及式（I）的环烷基取代的4-氨基苯基衍生物其中R是C 1 -C 4烷基：n是1至5的整数; 和（a）A是＆lt; IMAGE＆gt;而B是-O - ， - NH-或-CH 2 - ; 或（b）A是-CH 2 - ，B是-O - ， - NH - ， - CH 2 - 或者（c）A是-O-并且B是<或> 或（d）A是-NH-，B是或者-CH 2 - 及其药学上可接受的盐。本发明的范围还包括制备所述式（I）化合物和含有其的药物组合物的方法。本发明的化合物显示芳香酶抑制活性，并且可用于例如治疗激素依赖性肿瘤和前列腺肥大或增生。

14. 发明授权

US4526892A Dimethylaminoalkyl-3-(ergoline-8'.beta.carbonyl)-ureas 失效
标题翻译：二甲氨基烷基-3-（麦角灵-8'β羰基） - 脲
公开(公告)号：US4526892A
公开(公告)日：1985-07-02
申请号：US448364
申请日：1982-12-09
申请人： Patricia Salvati , Anna M. Caravaggi , Aldemio Temperilli , Germano Bosisio , Osvaldo Sapini , Enrico di Salle
发明人： Patricia Salvati , Anna M. Caravaggi , Aldemio Temperilli , Germano Bosisio , Osvaldo Sapini , Enrico di Salle
IPC分类号： C07D457/06 , A61K31/48
CPC分类号： C07D457/06
摘要： Novel ergoline derivatives formed by reaction of an 8-carboxy ergoline with a carbodiimide and having hypotensive and antiprolatinic activity.
摘要翻译：通过8-羧基麦角灵与碳二亚胺的反应形成的具有降血压和抗抑素活性的新型麦角灵衍生物。

15. 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。

16. 发明授权

US4732897A Steroidic 5.alpha.-reductase inhibitors 失效
标题翻译：类固醇5α-还原酶抑制剂
公开(公告)号：US4732897A
公开(公告)日：1988-03-22
申请号：US825348
申请日：1986-02-03
申请人： Gianfranco Cainelli , Giorgio Martelli , Mauro Panunzio , Giuseppe Spunta , Giuliano Nannini , Enrico di Salle
发明人： Gianfranco Cainelli , Giorgio Martelli , Mauro Panunzio , Giuseppe Spunta , Giuliano Nannini , Enrico di Salle
IPC分类号： C07C231/00 , A61K31/47 , A61K31/48 , C07C67/00 , C07C69/716 , C07C235/72 , C07C235/74 , C07C235/82 , C07J41/00 , C07J73/00 , A61K31/58
CPC分类号： C07J41/0061 , C07J73/005 , C07C2103/16
摘要： The present invention relates to new 4-aza-17.beta.-substituted 5.alpha.-androstan-3-ones, to a process for their preparation, to pharmacological compostions containing them, and to the use of said compounds as inhibitors of androgen action by means of testosterone 5-reductase inhibition.
摘要翻译：本发明涉及新的4-氮杂-17β-取代的5α-雄甾烷-3-酮，其制备方法，含有它们的药物组合物，以及所述化合物作为雄激素作用的抑制剂的用途的睾酮5-还原酶抑制。

17. 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。

18. 发明授权

US4632990A Ergoline carboxamides 失效
标题翻译：二氢吡啶甲酰胺
公开(公告)号：US4632990A
公开(公告)日：1986-12-30
申请号：US484477
申请日：1983-04-13
申请人： Luigi Bernardi , Enzo Brambilla , Laura Chiodini , Enrico di Salle , Daniela Ruggieri , Osvaldo Sapini , Aldemio Temperilli
发明人： Luigi Bernardi , Enzo Brambilla , Laura Chiodini , Enrico di Salle , Daniela Ruggieri , Osvaldo Sapini , Aldemio Temperilli
IPC分类号： A61K31/435 , A61P13/02 , A61P15/00 , A61P25/00 , A61P43/00 , C07D457/02 , C07D457/06 , A61K31/48 , C07D239/42
CPC分类号： C07D457/06 , C07D457/02
摘要： There are provided ergoline derivatives of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group, R.sub.2 represents a hydrogen or halogen atom or a methyl group, R.sub.3 represents a hydrogen atom or a methoxy group, R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms; each of X and W independently represents a hydrogen atom, a methyl group, a chlorine atom or a methoxy group, and n is 0, 1 or 2. A method for their preparation is also provided. The compounds have strong antiprolactin activity.
摘要翻译：提供下式的麦角灵衍生物：其中R 1表示氢原子或甲基，R 2表示氢或卤原子或甲基，R 3表示氢原子或甲氧基，R 4表示烃具有1至4个碳原子的基团; X和W各自独立地表示氢原子，甲基，氯原子或甲氧基，n为0,1或2.也可以提供其制备方法。该化合物具有较强的抗孕激素活性。

19. 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。

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