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1.发明授权1-methyl-15.alpha.-(1-oxyalkyl)androsta-1,4-diene-3,17-diones, processes for their production, and pharmaceutical preparations containing them 失效1-甲基-15α-（1-氧烷基）雄甾-1,4-二烯-3,17-二酮，其生产方法和含有它们的药物制剂
公开(公告)号：US4871725A
公开(公告)日：1989-10-03
申请号：US157568
申请日：1988-02-19
申请人： Ulrich Kerb , Yukishige Nishino , David Henderson
发明人： Ulrich Kerb , Yukishige Nishino , David Henderson
IPC分类号： A61K31/565 , C07J1/00 , C07J17/00 , C07J31/00 , C07J41/00
CPC分类号： C07J1/0011 , C07J1/0022 , C07J17/00 , C07J31/006 , C07J41/0038
摘要： 1-Methyl-15.alpha.-(1-oxyalkyl)androsta-1,4-diene-3,17-diones of general Formula I ##STR1## wherein R.sup.1 is a hydrogen atom or an acyl group of 1-10 carbon atoms,R.sup.2 is an OR.sup.4, NHR.sup.5 or an S(O).sub.n R.sup.6 group, R.sup.4 being straight- or branched-chain alkyl group of 1-10 carbon atoms, R.sup.5 being an acyl group of 1-10 carbon atoms, R.sup.6 being a straight- or branched-chain alkyl group of 1-10 carbon atoms or an aryl group of 6-10 carbon atoms,R.sup.3 is a hydrogen atom or a straight- or branched-chain alkyl group of 1-8 carbon atoms, and n is 0, 1 or 2,are suitable as inhibitors of estrogen biosynthesis for fertility control and for the treatment of diseases that are evoked by estrogens.
摘要翻译： 通式Ⅰ的1-甲基-15α-（1-氧烷基）雄甾-1,4-二烯-3,17-二酮其中R1是氢原子或1-10碳的酰基 原子，R2是OR4，NHR5或S（O）nR6基团，R4是1-10个碳原子的直链或支链烷基，R5是1-10个碳原子的酰基，R6是直链 - 或支链的1-10个碳原子的烷基或6-10个碳原子的芳基，R3是氢原子或1-8个碳原子的直链或支链烷基，并且n是0 ，1或2，适合作为雌激素生物合成的抑制剂，用于生育控制和治疗由雌激素诱发的疾病。
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2.发明授权1-alkyl-androsta-1,4-diene-3,17-diones their production and pharmaceutical preparations containing same 失效1-烷基 - 雄甾-1,4-二烯-3,17-将其制备和含有它们的药物制剂分离
公开(公告)号：US4591585A
公开(公告)日：1986-05-27
申请号：US621769
申请日：1984-06-18
申请人： Ulrich Kerb , Gerhard Sauer , Rudolf Wiechert , David Henderson , Yukishige Nishino , Sybille Beier
发明人： Ulrich Kerb , Gerhard Sauer , Rudolf Wiechert , David Henderson , Yukishige Nishino , Sybille Beier
CPC分类号： C07J1/0011
摘要： 1-Alkyl androsta-1,4-diene-3,17-diones of the formula ##STR1## wherein R.sub.1 is a methyl, ethyl, hydroxymethyl, C.sub.1 -C.sub.3 -alkoxymethyl, or C.sub.1 -C.sub.4 -alkanoyloxymethyl group, R.sub.6 is a hydrogen atom or a methyl group, and R.sub.7 is a hydrogen atom or a methyl group in the 7.alpha.- or 7.beta.-position, are useful for fertility control and for the treatment of estrogen-triggered diseases.
摘要翻译： 其中R 1是甲基，乙基，羟甲基，C 1 -C 3 - 烷氧基甲基或C 1 -C 4 - 烷酰氧基甲基，R 6是氢原子的1-烷基雄甾-1,4-二烯-3,17-二酮 原子或甲基，R7是7α-或7β-位中的氢原子或甲基，可用于生育调控和用于治疗雌激素引发的疾病。
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公开(公告)号：US5280035A
公开(公告)日：1994-01-18
申请号：US889331
申请日：1992-05-28
IPC分类号： A61K31/415 , A61K31/41 , A61K31/4174 , A61K31/4178 , A61K31/4192 , A61K31/4196 , A61P5/32 , A61P13/00 , A61P13/02 , A61P15/00 , A61P35/00 , C07D233/56 , C07D233/58 , C07D233/64 , C07D249/04 , C07D249/08 , C07D401/08 , C07D405/08 , C07D409/06 , C07D409/08 , C07D521/00 , C07D407/06
CPC分类号： C07D231/12 , C07D233/56 , C07D249/04 , C07D249/08
摘要： The disclosure relates to cycloalkylene azoles of general Formula I ##STR1## wherein ##STR2## is a carbocyclic or carbopolycyclic group optionally carrying at least one alkyl substituent,is the grouping ##STR3## an oxygen or sulfur atom, and Y and Z, independently of each other, are ##STR4## or a nitrogen atom, as well as their pharmaceutically compatible addition salts with acids as well as processes for production thereof. The compounds possess strongly aromatase-inhibiting activity and are suitable for the preparation of medicinal agents.Methods for treating estrogen induced or stimulated tumors, male infertility, and impending cardiac infarction with these compounds are also provided as well as methods for inhbiiting female fertility.
摘要翻译： 本公开涉及通式I的环亚烷基唑类（I）其中，IMAGE是任选携带至少一个烷基取代基的碳环或多碳环，是氧或硫原子，Y和Z 彼此独立地是氮或氮原子，以及它们与酸的药学上相容的加成盐以及其制备方法。 该化合物具有强烈的芳香酶抑制活性，适用于制备药剂。 还提供了用于治疗雌激素诱导或刺激的肿瘤，男性不育症和即将发生的这些化合物的心肌梗死的方法以及用于吸收女性生殖力的方法。
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公开(公告)号：US5411982A
公开(公告)日：1995-05-02
申请号：US153326
申请日：1993-11-16
IPC分类号： A61K31/415 , A61K31/41 , A61K31/4174 , A61K31/4178 , A61K31/4192 , A61K31/4196 , A61P5/32 , A61P13/00 , A61P13/02 , A61P15/00 , A61P35/00 , C07D233/56 , C07D233/58 , C07D233/64 , C07D249/04 , C07D249/08 , C07D401/08 , C07D405/08 , C07D409/06 , C07D409/08 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/04 , C07D249/08
摘要： The disclosure relates to cycloalkylene azoles of general Formula I ##STR1## wherein ##STR2## is a carbocyclic or carbopolycyclic group optionally carrying at least on a alkyl substituent,X is a grouping ##STR3## an oxygen or sulfur atom, and Y and Z, independently of each other, are ##STR4## or a nitrogen atom, as well as their pharmaceutically compatible addition salts with acids as well as processes for production thereof. The compounds possess strongly aromatase-inhibiting activity and are suitable for the preparation of medicinal agents.Methods for treating estrogen induced or stimulated tumors, male infertility, and impending cardiac infarction with these compounds are also provided as well as methods for inhibiting female fertility.
摘要翻译： 本公开涉及通式I的环亚烷基唑（I），其中，IMAGE是任选地至少带有烷基取代基的碳环或多碳环，X是氧或硫原子，Y 和Z彼此独立地是氮或氮原子，以及它们与酸的药学上相容的加成盐以及其制备方法。 该化合物具有强烈的芳香酶抑制活性，适用于药剂的制备。 还提供了用于治疗雌激素诱导或刺激的肿瘤，男性不育症和即将发生的这些化合物的心肌梗塞的方法以及抑制女性生育能力的方法。
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5.发明授权3-methylene-4-androsten-17-ones, process for their production and pharmaceutical preparations containing them 失效3-亚甲基-4-雄酮-17-酮，其制备方法和含有它们的药物制剂
公开(公告)号：US4925834A
公开(公告)日：1990-05-15
申请号：US188569
申请日：1988-04-29
CPC分类号： C07J71/001 , C07J1/0011 , C07J1/0022 , C07J17/00 , C07J31/006 , C07J41/0094
摘要： A 3-methylene-4-androsten-17-one of formula I ##STR1## wherein R.sub.a represents a hydrogen atom or a saturated or unsaturated straight-chain or branched-chain, optionally substituted alkyl radical with 1-6 carbon atoms, in which R.sub.a is in the alpha- or beta-position, andR.sub.b represents a hydrogen atom, a hydroxyl or an --S(O).sub.n R.sub.c group, in which R.sub.c is a hydrogen atom or an alkyl or acyl group with 1-4 carbon atoms, n=0, 1 or 2, andX represents CH.sub.2, CHF, CHCl or CHBr, in which if R.sub.a is hydrogen and R.sub.b is hydroxyl or R.sub.a and R.sub.b each are hydrogen, X is not CH.sub.2.The new compounds of formula I are suitable for fertility control and for treatment of diseases which are promoted by estrogens.
摘要翻译： 其中R a表示氢原子或具有1-6个碳原子的饱和或不饱和的直链或支链的任选取代的烷基的式I的3-亚甲基-4-雄酮-17-酮 ，其中Ra为α或β位，Rb表示氢原子，羟基或-S（O）nRc基团，其中Rc为氢原子或具有1-4个碳原子的烷基或酰基基团 碳原子，n = 0,1或2，X表示CH 2，CHF，CHCl或CHBr，其中如果Ra是氢，Rb是羟基或R a和R b各自是氢，X不是CH 2。 新的式I化合物适用于生育控制和治疗由雌激素促进的疾病。
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公开(公告)号：US4916144A
公开(公告)日：1990-04-10
申请号：US331283
申请日：1989-03-31
IPC分类号： C07D401/06 , A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/495 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07D233/56 , C07D233/58 , C07D233/60 , C07D233/61 , C07D401/12 , C07D409/00 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： The invention relates to N-substituted imidazoles of the formula, ##STR1## processes for their production as well as their use in pharmaceutical agents. The compounds according to the invention have aromatase-inhibiting properties and are suitable for therapy of estrogen-caused diseases.
摘要翻译： 本发明涉及下式的N-取代咪唑，其生产方法及其在药剂中的应用。 根据本发明的化合物具有芳香酶抑制性质并且适用于治疗雌激素引起的疾病。
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公开(公告)号：US5045558A
公开(公告)日：1991-09-03
申请号：US331399
申请日：1989-03-31
IPC分类号： C07D401/06 , A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/495 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07D233/56 , C07D233/58 , C07D233/60 , C07D233/61 , C07D401/12 , C07D409/00 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： The invention relates to N-substituted imidazoles, processes for their production as well as their use in pharmaceutical agents. The compounds according to the invention have aromatase-inhibiting properties.
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8.发明授权14,17.alpha.-etheno- and -ethanoestratrienes, processes for the preparation of these compounds, as well as their use for the production of medicinal agents 失效14,17（ALPHA） - 乙酸和乙二胺，其制备这些化合物的方法，以及其用于生产药物的用途
公开(公告)号：US5145847A
公开(公告)日：1992-09-08
申请号：US558340
申请日：1990-07-27
申请人： Rolf Bohlmann , Hermann Kunzer , Rudolf Wiechert , David Henderson , Martin Schneider , Yukishige Nishino
发明人： Rolf Bohlmann , Hermann Kunzer , Rudolf Wiechert , David Henderson , Martin Schneider , Yukishige Nishino
IPC分类号： A61K31/565 , A61P35/00 , C07J1/00 , C07J53/00
CPC分类号： C07J53/002
摘要： Disclosed are novel 14,17.alpha.-etheno- and -ethanoestratrienes according to general Formula I ##STR1## wherein X is a --CH.sub.2 --CH.sub.2 or ##STR2## R.sup.1 is a hydrogen atom, a C.sub.1 - to C.sub.15 -acyl, benzoyl, C.sub.1 - to C.sub.15 -alkyl, C.sub.3 - to C.sub.9 -cycloalkyl or alkylcycloalkyl group, andR.sup.2 is the grouping ##STR3## wherein R.sup.3 and R.sup.4 independently of each other mean a hydrogen atom or a straight-chain or branched, optionally partially or completely fluorinated C.sub.1 -C.sub.8 -alkyl group,a process for their preparation, pharmaceutical preparations containing these compounds, as well as their use for the production of medicinal agents.The novel compounds exhibit strong antiestrogenic efficacy.
摘要翻译： 公开了根据通式I（I）的新型14,17α-乙烯 - 和 - 乙二醇三亚甲基，其中X是-CH 2 -CH 2或者R 1是氢原子，C 1至C 15酰基， 苯甲酰基，C 1至C 15 - 烷基，C 3至C 9 - 环烷基或烷基环烷基，并且R 2为分组，其中R 3和R 4彼此独立地表示氢原子或直链或支链，任选地部分或部分 完全氟化的C 1 -C 8烷基，其制备方法，含有这些化合物的药物制剂，以及它们用于制备药剂的用途。 新化合物表现出强的抗雌激素疗效。
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9.发明授权Cycloalkylene azoles and pharmaceutical preparations obtained therefrom 失效CYCLOALKYLENE AZOLES和药物制剂
公开(公告)号：US5135937A
公开(公告)日：1992-08-04
申请号：US563114
申请日：1990-08-03
IPC分类号： A61K31/415 , A61K31/41 , A61K31/4174 , A61K31/4178 , A61K31/4192 , A61K31/4196 , A61P5/32 , A61P13/00 , A61P13/02 , A61P15/00 , A61P35/00 , C07D233/56 , C07D233/58 , C07D233/64 , C07D249/04 , C07D249/08 , C07D401/08 , C07D405/08 , C07D409/06 , C07D409/08 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/04 , C07D249/08
摘要： The disclosure relates to cycloalkylene azoles of general Formula I ##STR1## wherein ##STR2## is a carbocyclic or carbopolycyclic group optionally carrying at least one alkyl substituent,X is the grouping ##STR3## an oxygen or sulfur atom, and Y and Z, independently of each other, are ##STR4## or a nitrogen atom, as well as their pharmaceutically compatible addition salts with acids as well as processes for production thereof. The compounds possess strongly aromatase-inhibiting activity and are suitable for the preparation of medicinal agents.Methods for treating estrogen induced or stimulated tumors, male infertility, and impending cardiac infarction with these compounds are also provided as well as methods for inhibiting female fertility.
摘要翻译： 本公开涉及通式I的环亚烷基唑类（I），其中，IMAGE是任选携带至少一个烷基取代基的碳环或多碳环基，X是氧或硫原子的基团，Y和 Z，彼此独立地是氮原子，以及它们与酸的药学上相容的加成盐以及其制备方法。 该化合物具有强烈的芳香酶抑制活性，适用于制备药剂。 还提供了用于治疗雌激素诱导或刺激的肿瘤，男性不育症和即将发生的这些化合物的心肌梗塞的方法以及抑制女性生育能力的方法。
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10.发明授权7 &agr;-(5-methylaminopentyl)-estratrienes, process for their production, pharmaceutical preparations that contain these 7 &agr;(5-methylaminopentyl)-estratrienes as well as their use for the production of pharmaceutical agents 失效7α-（5-甲基氨基戊基） - 雌三烯，其制备方法，含有这些7α（5-甲基氨基戊基） - 雌三醇的药物制剂及其制备药剂的用途公开(公告)号：US06288051B1
公开(公告)日：2001-09-11
申请号：US09417765
申请日：1999-10-14
申请人： Dieter Bittler , Rolf Bohlmann , Nikolaus Heinrich , Jorg Kroll , Gerhard Sauer , Yukishige Nishino , Karsten Parczyk , Martin Schneider , Christa Hegelehartung , Rosemarie Lichtner
发明人： Dieter Bittler , Rolf Bohlmann , Nikolaus Heinrich , Jorg Kroll , Gerhard Sauer , Yukishige Nishino , Karsten Parczyk , Martin Schneider , Christa Hegelehartung , Rosemarie Lichtner
IPC分类号： A61K3156
CPC分类号： C07J1/0059 , C07J1/007 , C07J1/0074 , C07J17/00 , C07J31/006 , C07J41/0072 , C07J51/00
摘要： This invention describes the new 7&agr;-(5-methylaminopentyl)-estratrienes of general formula I in which R2 stands for a hydrogen or fluorine atom, R17 stands for a hydrogen atom, a methyl or ethinyl group, n stands for 2, 3 or 4, and x stands for 0, 1 or 2. The new compounds are strong, pure antiestrogens and can be used for the production of pharmaceutical agents for treatment of estrogen-dependent diseases, for example, breast cancer, endometrial carcinoma, prostatic hyperplasia, anovulatory infertility and melanoma.
摘要翻译： 本发明描述了通式Iin的新的7α-（5-甲基氨基戊基） - 三亚甲基，其中R 2表示氢或氟原子，R 17表示氢原子，甲基或乙炔基，n表示2,3或4，x表示 代表0，1或2.新化合物是强的纯粹的抗雌激素，可用于生产用于治疗雌激素依赖性疾病的药剂，例如乳腺癌，子宫内膜癌，前列腺增生，排卵不育和黑素瘤 。
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