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1. 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。

2. 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。

3. 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。

4. 发明申请

WO1997035839A1 NOVEL BORNEOLS, PROCESSES FOR PRODUCING THEM AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：新冰片，PROCESS FOR THEIR和制药用
公开(公告)号：WO1997035839A1
公开(公告)日：1997-10-02
申请号：PCT/EP1996001324
申请日：1996-03-27
申请人： SCHERING AKTIENGESELLSCHAFT , KLAR, Ulrich , GRAF, Hermann , BLECHERT, Siegfried , SACHSE, Anke
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C271/02
CPC分类号： C07D303/16 , C07C233/83 , C07C271/22 , C07C2602/42 , C07F7/1804
摘要： The disclosure relates to borneol derivatives of general formula (I) wherein: R represents a phenyl residue optionally substituted by halogen atoms, C1-C4 alkyl groups, C1-C4 alkoxy groups, C1-C6 alkoxycarbonyl groups or C1-C8 acyloxy groups; R stands for a hydrogen atom, a C1-C4 alkyl group, substituted aryl, a C1-C6 alkoxycarbonyl group or a C1-C8 acyl group; R stands for a hydrogen atom, a C1-C4 alkyl group, a C1-C4 acyl group or a tri-C1-C4 alkylsilyl group; R and R represent a hydrogen atom, a C1-C4 alkyl residue or a phenyl residue optionally substituted by halogen atoms, C1-C4 alkyl group, C1-C9 alkoxy groups, C1-C4 alkoxycarbonyl groups or C1-C8 acyloxy groups; R and R stand for a hydrogen atom, hydroxy group or a C1-C8 acyloxy group, or together represent a carbon-carbon bond or oxygen atom; or R and R and/or R and R respectively stand together for a carbonyl group, a C1-C4 alkylidene group or if required an oxirane group substituted by a C1-C3 alkyl group. Also disclosed are the salts of these derivatives with physiologically tolerable acids, their alpha -, beta - or gamma -cyclodextrin clathrates and compounds of general formula (I) encapsulated in liposomes.
摘要翻译： Borneolderivate通式（I）中有所描述，其中R <1>表示任选被卤原子，C1-C4烷基，C1-C4烷氧基，C1-C6烷氧羰基或C 1 -C 8 - 酰氧基苯基取代; [R <2>表示一个氢原子，一个C1-C4烷基，取代的芳基，一个C1-C6烷氧基羰基或C1-C8酰基基团; [R <3>代表氢原子，C1-C4烷基，C1-C4酰基或三C1-C4烷基甲硅烷基，并且其中; [R <4>和R <7>代表氢原子，C1-C4烷基或任选地被卤素原子，C1-C4烷基，C1-C9烷氧基，C1-C4烷氧羰基或C 1 -C 8 - 酰氧基苯基取代的且R <5>和R <6>代表氢原子，羟基或C1-C8-酰氧基或一起代表碳 - 碳键或氧原子，或R <4>和R <5>和/或R <6> 且R <7>的每个一起表示羰基，C1-C4亚烷基，或者，如果需要的话，由一个C1-C3烷基取代的环氧乙烷基团，和任选地它们的盐与生理上可接受的酸，以及它们的α - ，β - 或伽马-Cyclodextrinclathrate和通式（I）的脂质体包裹的化合物的意思。

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

WO1996000207A1 CYCLOHEXANONE DERIVATIVES, METHOD OF PREPARING THEM AND INTERMEDIATES USED IN THE METHOD 审中-公开
标题翻译：环己酮衍生物，工艺为自己的产品和对过程的
公开(公告)号：WO1996000207A1
公开(公告)日：1996-01-04
申请号：PCT/EP1995002274
申请日：1995-06-13
申请人： SCHERING AKTIENGESELLSCHAFT , STEINMEYER, Andreas , NEEF, Günter , MÜLLER, Gunnar , KNÖLKER, Hans-Joachim
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C69/013
CPC分类号： C07C49/647 , C07C43/188 , C07C43/196 , C07C45/29 , C07C45/40 , C07C45/69 , C07C49/497 , C07C49/517 , C07C49/577 , C07C69/013 , C07C251/44 , C07F7/1804
摘要： Described are cyclohexanone derivatives of general formula (I), a method of preparing them and intermediates used in the method.
摘要翻译：有通式（I）环己酮衍生物描述它们的制备方法和该方法的中间产物。

7. 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.

8. 发明申请

WO1994000429A1 22-ENE-25-OXA DERIVATIVES OF THE VITAMIN D SERIES, METHOD OF PREPARING SUCH DERIVATIVES, PHARMACEUTICAL PREPARATIONS CONTAINING THEM AND THUS USE OF SUCH PREPARATIONS AS DRUGS 审中-公开
标题翻译：中的维生素D系列22-EN-25-OXA衍生物，制备这些衍生物的方法所含药物制剂和它们作为药物
公开(公告)号：WO1994000429A1
公开(公告)日：1994-01-06
申请号：PCT/EP1993001735
申请日：1993-06-30
申请人： SCHERING AKTIENGESELLSCHAFT , STEINMEYER, Andreas , KIRSCH, Gerald , NEEF, Günter , SCHWARZ, Katica , THIEROFF-EKERDT, Ruth , WIESINGER, Herbert , HABEREY, Martin
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C401/00
CPC分类号： C07C401/00 , C07F7/1804
摘要： The invention concerns 22-ene-25-oxa derivatives of the vitamin D series of general formula (I), in which R1, R2 and R4, independently of each other, may each be a hydrogen atom, an alkanoyl group with 1 to 9 carbon atoms or an aroyl group; each R3 may be a hydrogen atom, a straight-chain or branched-chain alkyl group with 1 to 4 carbon atoms or a trifluoromethyl group, or the two R3 groups, together with the tertiary carbon atom to which they are attached, may form a saturated or unsaturated 3-, 4-, 5- or 6-membered carboxyclic or heterocyclic ring; and X is an alkylene group of the formula -(CH2)n- in which n = 1, 2 or 3. The invention also concerns a method of preparing such derivatives and their pharmaceutical use in the treatment of hyperproliferative diseases.

9. 发明申请

WO1997000242A1 NOVEL VITAMIN D DERIVATIVES WITH C-25 SUBSTITUENTS, PROCESS FOR THEIR PREPARATION, INTERMEDIATE PRODUCTS AND THEIR USE IN PREPARING MEDICAMENTS 审中-公开
标题翻译：在C-25，生产，中间体用于制造药物的方法和使用带有取代基NEW维生素D衍生物
公开(公告)号：WO1997000242A1
公开(公告)日：1997-01-03
申请号：PCT/EP1996001788
申请日：1996-04-30
申请人： SCHERING AKTIENGESELLSCHAFT , KIRSCH, Gerald , STEINMEYER, Andreas , NEEF, Günter , SCHWARZ, Katica , THIEROFF-EKERDT, Ruth , WIESINGER, Herbert , MENRAD, Andreas , HABEREY, Martin
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C401/00
CPC分类号： C07C401/00
摘要： The invention concerns novel vitamin D derivatives with C-25 substituents of general formula (I). The invention also concerns a process for their preparation and their use in preparing medicaments.
摘要翻译：本发明涉及具有取代基的新型维生素D衍生物在C-25的通式（I）的，用于制备和使用用于制造药物的方法。

10. 发明申请

WO1997041096A1 NEW VITAMIN D DERIVATIVES WITH CARBO- OR HETEROCYCLIC SUBSTITUENTS AT C-25, A PROCESS FOR THEIR PRODUCTION, INTERMEDIATE PRODUCTS AND THEIR USE FOR PRODUCING MEDICAMENTS 审中-公开
标题翻译：在C-25，生产，中间体用于制造药物的方法和使用具有碳环或杂环取代基NEW维生素D衍生物
公开(公告)号：WO1997041096A1
公开(公告)日：1997-11-06
申请号：PCT/EP1997002013
申请日：1997-04-21
申请人： SCHERING AKTIENGESELLSCHAFT , STEINMEYER, Andreas , KIRSCH, Gerald , NEEF, Günter , SCHWARZ, Katica , THIEROFF-EKERDT, Ruth , WIESINGER, Herbert , HABEREY, Martin , FÄHNRICH, Marianne
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C401/00
CPC分类号： C07D207/333 , C07C35/32 , C07C401/00 , C07D233/64 , C07D263/32 , C07D271/06 , C07D271/10 , C07D277/24 , C07D307/42 , C07D333/16
摘要： The invention concerns new vitamin D derivatives of general formula (I) a process for their production, their use for production of medicaments, and intermediate products used in the process.
摘要翻译：本发明涉及通式（I）的新的维生素D衍生物，其制备方法，使用用于该方法的药物和中间体的制造。

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