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1. 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。

2. 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.

3. 发明申请

WO1993025569A1 OESTRADIOL PRODRUGS 审中-公开
标题翻译：雌二醇前体药物
公开(公告)号：WO1993025569A1
公开(公告)日：1993-12-23
申请号：PCT/EP1993001543
申请日：1993-06-15
申请人： SCHERING AKTIENGESELLSCHAFT , MUHN-SEIPOLDY, Hans-Peter , CLEVE, Arwed , PETZOLDT, Karl , NEEF, Günter , KRATTENMACHER, Rolf , STÖCKEMANN, Klaus , GOTTWALD, Matthias
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J41/00
CPC分类号： C07J41/0016 , C07J1/007 , C07J1/0074 , C07J11/00 , C07J21/006
摘要： The invention concerns compounds of general formula (I), in which either X is a hydroxyimino group (= N SIMILAR OH), a hydroxy group and a hydrogen atom, a C1-C20 alkanoyloxy group and a hydrogen atom or two hydrogens atoms and A----B is a C-C double bond and B----C is a C-C single bond or X is a keto group protected in the form of a cyclic ketal and A----B is a C-C single bond and B----C is a C-C double bond and in both cases Z is an oxygen atom or an OR group and a hydrogen atom, and R and R , independently of each other, are each a hydrogen atom or a C1-C20 alkanoyl group. The compounds of formula (I) have oestrogenic properties.

4. 发明申请

WO1997028826A2 CONTRACEPTIVE RELEASE SYSTEMS WITH ANTIBACTERIAL AND/OR ANTIVIRAL EFFECT 审中-公开
标题翻译：具有抗菌和/或抗病毒效果避孕释放系统
公开(公告)号：WO1997028826A2
公开(公告)日：1997-08-14
申请号：PCT/DE1997000321
申请日：1997-02-11
申请人： SCHERING AKTIENGESELLSCHAFT , STÖCKEMANN, Klaus , CLEVE, Arwed , HOFFMANN, Karin , KOCH, Ulrich
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： A61K45/06
CPC分类号： A61K45/06 , A61F6/08 , A61F6/14 , A61K9/0036 , A61K9/0039 , A61K31/57 , A61K31/575 , A61K31/565 , A61K31/415 , A61K2300/00
摘要： The invention relates to the combination of at least one compound with contraceptive effect and/or one compound with antibacterial and/or antiviral effect for incorporation/application to an intravaginal, intrauterine or intracervical release system. The invention also relates to the use of said release system.
摘要翻译：本发明涉及至少一种化合物与避孕效果和/或具有用于结合/应用到阴道内，子宫内或intracervicales递送系统抗菌和/或抗病毒效果和使用这样的释放系统的化合物的组合。

5. 发明申请

WO1996032376A1 NOVEL BORNEOL ESTERS, PROCESS FOR THEIR PREPARATION AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译：新BORNEO LESTER，PROCESS FOR THEIR和制药用
公开(公告)号：WO1996032376A1
公开(公告)日：1996-10-17
申请号：PCT/EP1996001404
申请日：1996-03-29
申请人： SCHERING AKTIENGESELLSCHAFT , KLAR, Ulrich , GRAF, Hermann , NEEF, Günter , BLECHERT, Siegfried
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C271/22
CPC分类号： C07D303/16
摘要： The invention concernes borneol esters of general formula (I), in which R means T-C(O)-CH(OR )-CH(NR R )-R , C(O)-CH(OR )-CH[NR (C(O)-CH(OR )-CH(NR R )-R )]-R ; R R are identical or different and means R ; R means hydrogen, A, -C(O)R , -C(O)OR , -C(O)SR , -C(O)NHR , -C(O)NR R , -SO2R , C1-C10 alkyl; R , R are identical or different and mean R ; R means (i), heteroaryl substituted by X , C7-C16 aralkyl, alkyl; A is B-[O-(CH2)t-C(O)]0 or 1-, farnesyl-P(O)(OR )-O-(CH2)t-C(O)-; B means protein kinase-inhibitors or farnesyl protein transferase-inhibitors such as for example farnesyl (ii); and T is a bond, Z or a group (iii). The borneol esters can influence tubulin polymerisation and tubulin depolymerisation.
摘要翻译：通式婆罗洲莱斯特（I）其中，R <1>（O）-CH（OR <6>）TC - CH（NR <7A> - [R <7B>） - R的<8>，C（O）-CH（或<6>） - CH [NR <7>（C（O）-CH（OR <6B>） - CH（NR <7A> - [R <7B>） - R的<8A>）] - R的<8B> [R <7A>，R <7B>是相同的或不同的并且R <7>，R <7>是氢，A，-C（O）R <12>，-C（O）OR <12>，-C （O）SR <12>，-C（O）NHR <9D>，-C（O）NR <9D> - [R <9E>，-SO 2 R <12>，C1-C10烷基，R <8A>，R <8B>是相同的或不同的并且R <8>，R <8>（ⅰ）<3>取代的杂芳基，C7-C16芳烷基，烷基，A B- [O-（CH 2）TC（通过×○ ）] 0或1，法尼基 - P（O）（OR <9D>） - O-（CH 2）TC（O） - ，蛋白激酶B抑制剂或法尼基蛋白转移酶的抑制剂，例如表示法呢，（ii）中，T是一个键，Z的或基团（III），能够将影响微管蛋白聚合的微管蛋白或具有解聚。

6. 发明申请

WO1996025392A1 NOVEL BORNEOL DERIVATIVES, METHODS OF MANUFACTURING THEM, AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译：新BORNEOLDERIVATE，PROCESS FOR THEIR和制药用
公开(公告)号：WO1996025392A1
公开(公告)日：1996-08-22
申请号：PCT/DE1996000297
申请日：1996-02-19
申请人： SCHERING AKTIENGESELLSCHAFT , KLAR, Ulrich , GRAF, Hermann , NEEF, Günter , BLECHERT, Siegfried
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C271/22
CPC分类号： C07D303/16 , C07C271/22 , C07C2603/86
摘要： The invention concerns borneol derivatives of general formula (I), wherein: R represents C(O)-CH(OR )-CH(NR R )-R , C(O)-CH(OR )-CH[NH(C(O)-CH(OR )-CH(NR R )-R )] -R ; R and R are identical or different and the same as R ; R and R are identical or different and the same as R ; R is -C(O)R , -SO2R , -C(O)OR , -C(O)SR , -C(O)NHR , -C(O)NR R , (a), alkyl; R is phenyl; R and R are identical or different and stand for alkyl, cycloalkyl, aryl or aralkyl; R are identical or different and stand for hydrogen, alkyl, aryl, acyl, aralkyl, -SO2R , -P(O) (OH)2; R stands for hydrogen, alkyl, aryl, aralkyl. The invention also concerns salts of the said compounds with physiologically tolerable bases, alpha -, beta - or gamma -cyclodextrine clathrates of the said compounds and compounds of formula (I) encapsulated with liposomes. The compounds are active as tubulin polymerisation antagonists.
摘要翻译：本发明betrfifft Borneolderivate通式（I）其中R <1>（O）-CH（OR <6>）C - CH（NR <7A> - [R <7B>） - R的<8>，C（O） -CH（OR <6>） - CH [NH（（O）-CH（OR <6B>）C - CH（NR <7A> - [R <7B>） - R的<8>）] - R的<8>， [R <6A>，R <6B>是相同的或不同的并且R <6>，R <7A>，R <7B>是相同的或不同的并且R <7>，R <7> -C（O）R <12>，-SO 2 R <12>，-C（O）OR <12>，-C（O）SR <12>，-C（O）NHR <9D>，-C（O）NR <9D>ř <9A>中，（a）烷基，R <8>是苯基，R ，R <12>是相同的或不同的并且是烷基，环烷基，芳基，芳烷基，R <6>是相同的或不同的，是氢烷基，芳基，酰基，芳烷基，-SO 2 R <9C>，-P（O）（OH）指2，R <13>为氢，烷基，芳基，芳烷基，以及与生理上可耐受的碱，以及它们的α它们的盐 - ，β - 或伽马-Cyclodextrinclathrate和平均封装有通式（I）的脂质体的化合物。该化合物作为活性聚合的微管蛋白拮抗剂。

7. 发明申请

WO1995030650A1 BORNEOL DERIVATIVES AFFECTING TUBULIN POLYMERIZATION AND DEPOLYMERIZATION 审中-公开
标题翻译：微管蛋白聚合或 -DEPOLYMERISATION - 影响BORNEOLDERIVATE
公开(公告)号：WO1995030650A1
公开(公告)日：1995-11-16
申请号：PCT/EP1995001341
申请日：1995-04-13
申请人： SCHERING AKTIENGESELLSCHAFT , KLAR, Ulrich , GRAF, Hermann , NEEF, Günter , BLECHERT, Siegfried
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C271/22
CPC分类号： C07C271/22 , C07C2603/86 , C07D303/14 , C07D303/16
摘要： The invention relates to borneol derivatives of the general formula (I) in which R is C(O)-CH(OR )-CH(NHR )-R , R is hydrogen, -OH, C1-C10-Alkyl, C1-C10-alkoxy, -OC(O)R , -OP(O)(OH)2 or R and R are together an oxygen atom, R is hydrogen, C1-C10-alkyl, -(CH2)n-OR , R is hydrogen, C1-C10-alkyl, -(CH2)p-OR , or R and R together are an oxygen atom, a =CHR group, n is 0 to 8, p is 1 to 8, R is -C(O)R , -SO2R , -C(O)NHR , -C(O)NR R , (formula), R is aryl, R and R are the same or different and represent C1-C10-akyl, C4-C8-cycloalkyl, aryl, C7-C16-aralkyl, R is hydrogen, C1-C10-alkyl, -(CH2)s-OR , s is 1 to 8, R , R and R are the same or different and represent hydrogen, C1-C10-alkyl, aryl, C7-C16 aralkyl, SO2R , -P(O)(OH)2, R and R are the same or different and represent hydrogen, C1-C10-alkyl, aryl, C7-C16-aralkyl, X and X are the same or different and mean X, X may be hydrogen, halogen, -OH, -NO2, -N3, -CN, -NR R , -NHSO2R , -CO2R , C1-C10-alkyl, C1-C10-alkoxy, C1-C10-acyloxy, C1-C10-acyl and, if R is hydrogen, their salts with physiologically tolerable bases, and alpha -, beta - or gamma -cyclodextrin clathrates, and the compounds of the general formula (I) encapsulated with liposomes.
摘要翻译：本发明涉及Borneolderivate通式（I）其中R <1> C（O）-CH（OR <6>） - CH（NHR <7>） - R的<8>，R <2>是氢，-OH ，C1-C10烷基，C1-C10烷氧基，-OC（O）R <9A>，-OSO 2 R <9A>，-OP（O）（OH）2，NHR <9>，NR <9> - [R < 图9b>，R <3>是氢，-OH，C1-C10烷氧基，-OC（O）R <9B>，-OSO 2 R <9B>，-OP（O）（OH）2，或R <2>， [R <3>一起为氧原子，R <4>为氢，C1-C10烷基， - （CH 2）N-OR <11A>，R <5>是氢，C1-C10烷基， - （CH 2）p OR <11B>或R <4>，R <5>在一起的氧原子，= CHR <10>基团，n是0至8，p为1至8，R <7> -C（O）R <12？，-SO> 2 ，-C（O）OR <12>，-C（O）NHR <9D>，-C（O）NR <9D> - [R <9E>中，（a）中，R <8>芳基，R <9A-E>，R <12>是相同的或不同的并且是C 1 -C 10烷基，C 4 -C 8 - 环烷基，芳基，C7-C16芳烷基，R <10>为氢，C 1 -C C10烷基， - （CH 2）S-或<14>，S为1〜8，R <6>，R <11A，b>，R <14>是相同的或不同的，是氢，C1-C10烷基，芳基，C7-C16芳烷基，-SO 2 R <9C>平均-P（O）（OH）2，R <13>，R <15A，b>是相同的或不同的并且是氢，C1-C10-A lkyl，芳基，C7-C16芳烷基，X <1>中，X <2>是相同的或不同的，X，X是氢，卤素，-OH，-NO 2，-N 3，-CN，-NR <15A> [R <15B>，-NHSO 2 <15>，-CO 2 R <15>，C1-C10烷基，C1-C10烷氧基，C1-C10酰氧基，可以是C1-C10酰基，和，如果R <15>为氢基，它们与生理上可耐受的碱的盐，以及它们的α - ，β - 或伽马-Cyclodextrinclathrate，并用通式（I）的脂质体包封的化合物的意思。

8. 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。

9. 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。

10. 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。

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