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1. 发明申请

WO1994004555A1 ANTI-ANDROGENE STEROIDS WITH AN ANNULATED FIVE-MEMBERED RING 审中-公开
标题翻译：抗雄激素类固醇融合五环
公开(公告)号：WO1994004555A1
公开(公告)日：1994-03-03
申请号：PCT/EP1993002194
申请日：1993-08-17
申请人： SCHERING AKTIENGESELLSCHAFT , SAUER, Gerhard , SCHRÖTER, Bernd , HOFMEISTER, Helmut , BRUMBY, Thomas , FRITZEMEIER, Karl-Heinrich , MICHNA, Horst
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J71/00
CPC分类号： C07J1/0037 , C07J53/002 , C07J71/0005 , C07J71/0047 , C07J71/0078
摘要： New steroids with an annulated five-membered ring have general formula (I), in which Y stands for an oxygene or sulphur atom or for a sulfonyl group or for the groups (a) or (b), in which X stands for a hydrogen atom, a saturated, straight or branched chain or cyclic hydrocarbon residue substituted if required by a cyano group of by a fluorine, chlorine or bromine atom, having 1 to 8 carbon atoms in the case of the branched chain or 3 to 8 carbon atomes in the cyclic case, or an alkanoyl group with 1 to 5 carbon atoms, or a benzoyl residue or a methylsulfonyl group, or X stands for a group Z-NH or Z-O, in which Z stands for the above-mentioned substituents represented by X; R17 stands for a hydrogene atom or a straight or branched chain, saturated or unsaturated hydrocarbon residue with up to 6 carbon atoms substituted if required by a hydroxy group; R17' stands for a hydrogen atom or an alkanoyl group with 1 to 4 carbon atoms, and (c) stands for a C-C simple (5(alpha)-H) or C-C double bond and the dotted circle stands for two double bonds in the annulated five-membered ring. These new compounds have strong anti-androgene activity and are suitable for preparing medicaments.

2. 发明申请

WO1993013122A1 3-METHYLSULPHONYLHYDRAZONO AND 3-OXYIMINO STEROIDS, A METHOD OF PREPARING THEM, PHARMACEUTICAL PREPARATIONS CONTAINING THEM AND THEIR USE IN THE PREPARATION OF DRUGS 审中-公开
标题翻译： 3-甲基磺酰脲和3-氧亚氨基甾体，其制备方法，包含它们的药物制剂及其在制备药物中的用途
公开(公告)号：WO1993013122A1
公开(公告)日：1993-07-08
申请号：PCT/EP1992002983
申请日：1992-12-22
申请人： SCHERING AKTIENGESELLSCHAFT , BITTLER, Dieter , HOFMEISTER, Helmut , BRUMBY, Thomas , KROLL, Jörg , KÜNZER, Hermann , SAUER, Gerhard , FRITZEMEIER, Karl-Heinrich , MICHNA, Horst
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J41/00
CPC分类号： C07J41/0016 , C07J41/0005
摘要： Described are 3-methylsulphonylhydrazono and 3-oxyimino steroids of the general formula (I), in which X is an oxygen atom or an NH group; the C4-C5 bond is a single or double C-C bond and the C15-C16 bond is a single or double C-C bond, and R', which depends on the nature of X, and the other substituents are as defined in the description. The new compounds are anti-androgens with peripheral selectivity and with an activity comparable to that of cyproterone acetate, and are suitable for use in the preparation of drugs.
摘要翻译：描述了通式（I）的3-甲基磺酰肼基和3-氧亚氨基类固醇，其中X是氧原子或NH基团; C4-C5键是单或双C-C键，C15-C16键是单或双C-C键，R'取决于X的性质，其他取代基如说明书中所定义。新化合物是具有周围选择性的抗雄激素，具有与醋酸环丙孕酮相当的活性，并且适用于制备药物。

3. 发明申请

WO1998023634A1 CYCLOALKYL STEROIDS, METHOD FOR THE PRODUCTION THEREOF, PHARMACEUTICAL PREPARATIONS CONTAINING SAME CYCLOALKYL STEROIDS AND THE USE THEREOF AS MEDICAMENTS 审中-公开
标题翻译： CYCLOALKYLSTEROIDE，加工生产这些CYCLOALKYLSTEROIDE药物制剂和它们在药品生产
公开(公告)号：WO1998023634A1
公开(公告)日：1998-06-04
申请号：PCT/EP1997006542
申请日：1997-11-24
申请人： SCHERING AKTIENGESELLSCHAFT , KASCH, Helmut , SCHÖLLKOPF, Klaus , FRITZEMEIER, Karl-Heinrich , KRATTENMACHER, Rolf , MUHN, Hans-Peter
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J53/00
CPC分类号： C07J53/002
摘要： Novel 16 alpha , 17 alpha carbocylic steroids of general formula (I), wherein R =C2-C5 alcanoyl, but not acetyl, when R and R both mean a hydrogen atom, C2-C5-(1-hydroxy)-alkyl, C2-C5 -(1-aroyloxy)-alkyl, C2-C5-(1-C1-C5-alkanoyloxy)-alkyl, C2-C5-1(aroyloxy)-alkyl, C2-C5-(1-aroyloxy)-alkyl, C2-C5-(2-hydroxy)-alcanoyl, cyano, (hydroxyamino)-carbonyl, (C1-C5-alcoxyamino)-carbonyl, C1-C5-(1 hydroxyimino)-alkyl, C1-C5-(1-C1-C5-alcoxyimino)-alkyl, C1-C5-(1-C1-C5- alkylimino)-alkyl, C1-C5-(1-C1-C5-alkanoyloximino)-alkyl, C1-C5-(1-alkylaminocarbonyloxy)-alkyl, C2-C5-(1-arylaminocarbonyloxy)-alkyl, R =methyl or ethyl, R , R , R mean individually a hydrogen atom or a methyl group, C -C mean a C-C- single or double bond, X means 2 hydrogen atoms, a hydrogen atom and a hydroxy group, a radical of formula -S-(CH2)n-S- with n=2,3,4 or 5, an oxygen atom, a hydroxyimino-, C1-C6-alcoxy-, C1-C6-alcanoyl, C1-C6 alcoxycarbonylimino, C1-C6-alcoxyimimino, C1-C6-alcoxycarbonyloximino- or a C1-C6 alkanoyloximino group. The invention also describes a method for the production thereof. The compounds of formula (I) exhibit high progestogenic efficiency, and are suitable for the production of medicaments.
摘要翻译：有通式I，其中R，如果R <2 '>和R <3'>是<17> = C2-C5烷酰基，但不乙酰基，各自代表氢原子的新的16α，17的α-碳环甾族化合物， C2〜C5的（1-羟基）烷基，C2〜C5的（1-C1-C5烷氧基）烷基，C2〜C5的（1-C 1 -C 5烷酰氧基）烷基，C2〜C5的（1 芳酰氧基）烷基，C2〜C5的（2-羟基）烷酰基，氰基，（羟氨基）羰基，（C1-C5烷氧基）羰基，C1-C5（1-羟基亚氨基）烷基，C 1 -C C5（1-C 1 -C 5烷氧基亚氨基）烷基，C1-C5（1-C 1 -C 5烷基亚氨基）烷基，C1-C5（1-C1-C5-Alkanoyloximino）烷基，C1-C5 （1-烷基氨基羰）烷基，C1-C5（1- arylaminocarbonyloxy）烷基，R <13> =甲基或乙基，R <2 '>，R <3'>，R <4“>独立地为氢原子，意味着或甲基，C <2“> - Visual C <3”>是CC单键或双键，X代表两个氢原子，一个氢原子和一个羟基基团，一个基团的式-S-（CH 2）n的S-，其中n = 2 ，3，4或5，氧原子，羟基亚，C1-C6烷氧基，C1-C6烷酰基，C1-C6-Alkoxyca rbonylimino-，C1-C6烷氧基亚，C1-C6-Alkoxycarbonyloximino-或C1-C6-Alkanoyloximinogruppe装置描述以及它们的制备方法。式I的化合物具有很强的促孕活性和适用于药物的制备。

4. 发明申请

WO1994006819A1 GESTAGEN-EFFECTIVE 4,5;11,12-ESTRADIENES, PROCESS FOR THEIR PRODUCTION, MEDICAMENTS CONTAINING THESE ESTRADIENES AND THEIR USE IN PRODUCING MEDICAMENTS 审中-公开
标题翻译：孕激素EFFECTIVE 4,5; 11,12- ESTRADIENE，产生的方法，ESTRADIENE DRUGS容纳和它们在药物的生产
公开(公告)号：WO1994006819A1
公开(公告)日：1994-03-31
申请号：PCT/EP1993002573
申请日：1993-09-22
申请人： SCHERING AKTIENGESELLSCHAFT , SCHWEDE, Wolfgang , HALFBRODT, Wolfgang , NEEF, Günter , OTTOW, Eckhard , SCHÖLLKOPF, Klaus , KRATTENMACHER, Rolf , FRITZEMEIER, Karl-Heinrich
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J01/00
CPC分类号： C07J21/003 , C07J1/0096 , C07J7/0045 , C07J21/00
摘要： The proposal is for the novel 4,5;11,12-estradienes of general formula (I) in which the substituents W, R11, R14, R15, R16, R17(alpha), R17(beta), R18 have the meanings given in the description, and a process for their production. The novel compounds have a strong gestagen activity and are suitable for use in medicaments, e.g. as gestagen components in preparations for hormonal contraception.

5. 发明申请

WO1995031471A1 19,11'beta' BRIDGED 18-NOR STEROIDS, PROCESS FOR PRODUCING THEM, MEDICAMENTS CONTAINING SAID STEROIDS AND THEIR USE IN THE PRODUCTION OF MEDICAMENTS 审中-公开
标题翻译： 19.11的β-ÜBERBRÜCKTE18-NOR-类固醇，PROCESS FOR PRODUCING这些药物含类固醇和它们在药物的生产
公开(公告)号：WO1995031471A1
公开(公告)日：1995-11-23
申请号：PCT/EP1995001905
申请日：1995-05-18
申请人： SCHERING AKTIENGESELLSCHAFT , KLAR, Ulrich , CLEVE, Arwed , NEEF, Günter , OTTOW, Eckhard , STÖCKEMANN, Klaus , FRITZEMEIER, Karl-Heinrich
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J53/00
CPC分类号： C07J53/002
摘要： The present invention describes the novel 19,11 beta bridged 18-nor steroids of general formula (I) in which the symbols A, V and Z and the substituents R , B and G have the meanings given in the description. The novel compounds are distinguished from prior art steroids by the dealkylated position 13. They exhibit partially better binding to steroid receptors than comparable 13-alkyl steroids and are suitable for the production of medicaments.
摘要翻译：本发明描述了新的β-19,11-überbrückte通式（I）的18-去甲甾类，其中符号A，V和Z，以及取代基R <1>，B和G具有说明书中所示的含义，的新化合物通过从脱烷基化位置13是从已知的类固醇可分辨。部分，它们具有到类固醇受体比同类13 Alkylsteroide更好的结合，并适用于生产药物。

6. 发明申请

WO1995027726A1 10,11-C3-BRIDGED STEROIDS 审中-公开
标题翻译： 10,11-桥C3类固醇
公开(公告)号：WO1995027726A1
公开(公告)日：1995-10-19
申请号：PCT/EP1995001340
申请日：1995-04-12
申请人： SCHERING AKTIENGESELLSCHAFT , SCHWEDE, Wolfgang , HALFBRODT, Wolfgang , KUHNKE, Joachim , KRATTENMACHER, Rolf , MUHN, Hans-Peter , FRITZEMEIER, Karl-Heinrich
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J53/00
CPC分类号： C07J53/002
摘要： The invention discloses new 10,11-C3-bridged steroids of the general formula I, in which W, R , R , R , R , R , R as well as R , R , R and R are as defined in the description. Disclosed also is a method for preparing them. The new compounds have strong progestational activity and may be used in the manufacture of drugs.
摘要翻译：在本发明中，新颖的10,11- C3-桥接通式（I）的类固醇被描述，其中W，R <6A>，R <6B>，R <7>，R <15>，R <16> ，R <17的α>和R <17的β>，R <18>，R <11>和R <11“>是如在说明书中所定义，以及它们的制备方法。新的化合物具有强的促孕活性和适用于生产药物。

7. 发明申请

WO1995027725A1 11'beta',19-BRIDGED 13'alpha'-ALKYL STEROIDS 审中-公开
标题翻译： 11的β，19的α-桥13 -ALKYLSTEROIDE
公开(公告)号：WO1995027725A1
公开(公告)日：1995-10-19
申请号：PCT/EP1995001339
申请日：1995-04-12
申请人： SCHERING AKTIENGESELLSCHAFT , SCHWEDE, Wolfgang , HALFBRODT, Wolfgang , KUHNKE, Joachim , KRATTENMACHER, Rolf , MUHN, Hans-Peter , FRITZEMEIER, Karl-Heinrich
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J53/00
CPC分类号： C07J53/002
摘要： The invention discloses new 11 beta ,19-bridged 13 alpha -alkyl steroids of general formula (I), in which W, R , R , R , R , R , R as well as R , R , R and R are as defined in the description. Disclosed also is a method for preparing them. The new compounds have strong progestational activity and may be used in the manufacture of drugs.
摘要翻译：在本发明中，该新颖的β11 19 - 桥连的α通式-Alkylsteroide 13（I），其中W，R <6A>，R <6B>，R <7>，R <15>，R < 16>，R <17A>和R <17B>，R <18>，R <11 '>和R <19'>具有说明书中所示的含义，并且它们的制备方法。新的化合物具有强的促孕活性和适用于生产药品到的。

8. 发明申请

WO1994027610A1 AGENTS CONTAINING A COMPOUND WITH AN ANTI-ANDROGEN EFFECT AND A COMPOUND WITH A COMPETITIVE, PROGESTERONE-ANTAGONISTIC EFFECT 审中-公开
标题翻译： MEDIUM含有抗雄激素和相关的竞争，孕激素拮抗作用的连接
公开(公告)号：WO1994027610A1
公开(公告)日：1994-12-08
申请号：PCT/EP1994001756
申请日：1994-05-30
申请人： SCHERING AKTIENGESELLSCHAFT , MICHNA, Horst , SCHNEIDER, Martin
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： A61K31/575
CPC分类号： A61K31/575 , A61K31/57 , A61K2300/00
摘要： Agents contain at least one compound with an anti-androgen effect (AA) as well as at least one compound with a competitive, progesterone-antagonistic effect (PA). These agents are suitable for preparing medicaments for the prophylaxis and therapy of prostate carcinome and benign prostate hyperplasia (BPH). Also disclosed is the use of at least one compound with a PA effect to prepare medicaments for the prophylaxis and therapy of BPH.
摘要翻译：本发明涉及包含具有至少一种化合物的抗雄激素（AA）和有竞争力的，黄体酮拮抗（PA）作用的至少一种化合物的组合物。这些试剂适合于生产药物用于预防和前列腺癌和良性前列腺增生（BPH）的治疗。本发明还涉及使用至少一种化合物与PA活性药物用于预防和治疗BPH的制造。

9. 发明申请

WO1989012064A1 1'beta',15'alpha'-DIHYDROXY-1'alpha'-METHYL-5'alpha'-ANDROSTAN-3,17-DIONE, ITS PREPARATION AND USE 审中-公开
标题翻译： 1β，15α-DIHYDROXY-1α-甲基-5α-萘啶-3,17-二酮，其制备和使用
公开(公告)号：WO1989012064A1
公开(公告)日：1989-12-14
申请号：PCT/DE1989000362
申请日：1989-05-30
申请人： SCHERING AKTIENGESELLSCHAFT , PETZOLDT, Karl , HOFMEISTER, Helmut
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J01/00
CPC分类号： C07J41/0094 , C07J1/0011 , C07J21/008 , C12P33/00
摘要： 1beta,15alpha-Dihydroxy-1alpha-methyl-5alpha-androstan-3,17-dione of formula (I) and its subsequent processing to pharmacologically active steroids.

10. 发明申请

WO1990011290A1 METHOD FOR THE PREPARATION OF 3-DESOXY-4-ENE STEROIDS 审中-公开
标题翻译：制备3-脱氧-4-烯酮甾体的方法
公开(公告)号：WO1990011290A1
公开(公告)日：1990-10-04
申请号：PCT/DE1990000183
申请日：1990-03-08
申请人： SCHERING AKTIENGESELLSCHAFT , WINTERFELDT, Ekkehard , TILSTAMM, Ulf , HOFMEISTER, Helmut , LAURENT, Henry
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J11/00
CPC分类号： C07J11/00
摘要： The invention concerns a method for the preparation of 3-desoxy-4-ene steroids of the general formula I in which R1, R2 and R3 are a hydrogen atom or a methyl group, R4 is a lower alkyl group, a phenyl group or a free, esterified or etherified hydroxyl group, R5 is a hydrogen atom, a vinyl group or the -C=CR6 grouping, R6 being a hydrogen atom, an alkyl group with at the most 4 carbon atoms or a halogen atom, X is a methylene group, a fluoromethylene group, an ethylidene group or a vinylidene group, Y and U are a methylene group or an ethylidene group, and Z is a methylene group, an ethylidene group, a vinylidene group, a chloromethylene group or a hydroxymethylene group, and in which the bonds are three single bonds, or a double bond and two single bonds, or a conjugated double bond. The 3-oxo-4-ene steroid is reduced using a reaction mixture comprising trifluoroacetic or trichloroacetic acid, optionally additional carboxylic acid, and sodium borohydride.
摘要翻译：本发明涉及制备通式Ⅰ的3-脱氧-4-烯类固醇的方法，其中R1，R2和R3为氢原子或甲基，R4为低级烷基，苯基或游离的，酯化的或醚化的羟基，R5是氢原子，乙烯基或-C = CR6基，R6是氢原子，具有最多4个碳原子的烷基或卤素原子，X是亚甲基亚乙基，亚乙烯基，Y和U是亚甲基或亚乙基，Z是亚甲基，亚乙基，亚乙烯基，氯亚甲基或羟基亚甲基，和其中键是三个单键，或双键和两个单键，或共轭双键。使用包含三氟乙酸或三氯乙酸，任选的另外的羧酸和硼氢化钠的反应混合物还原3-氧代-4-烯类固醇。

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