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1. 发明授权

US5965609A Borneol esters, process for their production, and their pharmaceutical use 失效
标题翻译：苯甲酸酯，其制备方法及其药物用途
公开(公告)号：US5965609A
公开(公告)日：1999-10-12
申请号：US930009
申请日：1998-03-13
申请人： Ulrich Klar , Hermann Graf , Gunter Neef , Siegfried Blechert
发明人： Ulrich Klar , Hermann Graf , Gunter Neef , Siegfried Blechert
IPC分类号： A61K31/335 , A61K31/336 , A61P25/00 , A61P31/04 , A61P33/02 , A61P35/00 , A61P35/02 , C07D303/16 , C07D405/12 , C07D407/12 , C07D409/12 , C07D303/10
CPC分类号： C07D303/16
摘要： The invention concernes borneol esters of general formula (I), in which R.sup.1 means T--C(O)--CH(OR.sup.6)--(NR.sup.7a R.sup.7b)--R.sup.8, C(O)--CH(OR.sup.6a)--CH[NR.sup.7 (C(O)--CH(OR.sup.6b)--CH (NR.sup.7a R.sup.7b)--R.sup.8a)]--R.sup.8b ; R.sup.7a R.sup.7b are identical or different and means R.sup.7 ; R.sup.7 means hydrogen, A, --C(O)R.sup.12, --C(O)OR.sup.12, --C(O)SR.sup.12, --C(O)NHR.sup.9d, --C(O)NR.sup.9d R.sup.9e, --SO.sub.2 R.sup.12, C.sub.1 -C.sub.10 alkyl; R.sup.8a, R.sup.8b are identical or different and mean R.sup.8 ; R.sup.8 means (i), heteroaryl substituted by X.sup.3, C.sub.7 -C.sub.16 aralkyl, alkyl; A is B--[O--(CH.sub.2).sub.t --C(O)].sub.0 or 1-, farnesyl--P(O)(OR.sup.9d)--O--(CH.sub.2).sub.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.sup.i or a group (iii). The borneol esters can influence tubulin polymerisation and tubulin depolymerisation.
摘要翻译： PCT No.PCT / EP96 / 01404 Sec。 371日期1998年3月13日 102（e）1998年3月13日PCT 1996年3月29日PCT公布。第WO96 / 32376号公报日期：1996年10月17日本发明涉及通式（I）的冰片酯，其中R1表示TC（O）-CH（OR6） - （NR7aR7b）-R8，C（O）-CH（OR6a）-CH [NR7 （C（O）-CH（OR6b）-CH（NR7aR7b）-R8a）] -R8b; R7a R7b相同或不同，表示R7; R7表示氢，A，-C（O）R12，-C（O）OR12，-C（O）SR12，-C（O）NHR9d，-C（O）NR9dR9e，-SO2R12，C1-C10烷基; R8a，R8b相同或不同，表示R8; R8表示（i），被X3，C7-C16芳烷基，烷基取代的杂芳基; A是B- [O-（CH 2）t -C（O）] 0或1-，法呢基-P（O）（OR 9d）-O-（CH 2）t -C（O） - ; B表示蛋白激酶抑制剂或法呢基蛋白转移酶抑制剂，例如法呢基（ii）; 和T是一个键，Zi或一个组（iii）。冰片酯可影响微管蛋白聚合和微管蛋白解聚。

2. 发明授权

US5792792A Borenol derivatives, process for their production and their pharmaceutical use 失效
标题翻译： Borenol衍生物，其生产过程及其药物用途
公开(公告)号：US5792792A
公开(公告)日：1998-08-11
申请号：US732449
申请日：1997-01-03
申请人： Ulrich Klar , Hermann Graf , Gunter Neef , Siegfried Blechert
发明人： Ulrich Klar , Hermann Graf , Gunter Neef , Siegfried Blechert
IPC分类号： C07D303/31 , C07C271/22 , C07C309/63 , C07D303/14 , C07D303/16 , C07F9/38 , A61K31/335 , C07D303/10
CPC分类号： C07C271/22 , C07D303/14 , C07D303/16 , C07C2103/86
摘要： The invention relates to borneol derivatives of general formula I ##STR1## in which R.sup.1 means C(O)--CH(OR.sup.6)--CH(NHR.sup.7)--R.sup.8, R.sup.2 means hydrogen, --OH, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, --OC(O)R.sup.9a, --OSO.sub.2 R.sup.9a, --OP(O)(OH).sub.2, NHR.sup.9a, NR.sup.9a R.sup.9b, R.sup.3 means hydrogen, --OH, C.sub.1 -C.sub.10 alkoxy, --OC(O)R.sup.9b, --OSO.sub.2 R.sup.9b, --OP(O)(OH).sub.2, or R.sup.2, R.sup.3 together mean an oxygen atom, R.sup.4 means hydrogen, C.sub.1 -C.sub.10 alkyl, --(CH.sub.2).sub.n --OR.sup.11a, R.sup.5 means hydrogen, C.sub.1 -C.sub.10 alkyl, --(CH.sub.2).sub.p --OR.sup.11b, or R.sup.4, R.sup.5 together mean an oxygen atom, a=CHR.sup.10 group, n means 0 to 8, p means 1 to 8, R.sup.7 means --C(O)R.sup.12, --SO.sub.2 R.sup.12, --C(O)OR.sup.12, --C(O)NHR.sup.9d, --C(O)NR.sup.9d R.sup.9e, ##STR2## R.sup.8 means aryl, R.sup.9a-e, R.sup.12 are the same or different and mean C.sub.1 -C.sub.10 alkyl, C.sub.4 -C.sub.8 cycloalkyl, aryl, C.sub.7 -C.sub.16 aralkyl, R.sup.10 means hydrogen, C.sub.1 -C.sub.10 alkyl, --(CH.sub.2).sub.s --OR.sup.14, s means 1 to 8, R.sup.6, R.sup.11a,b, R.sup.14 are the same or different and mean hydrogen, C.sub.1 -C.sub.10 alkyl, aryl, C.sub.7 -C.sub.16 aralkyl, --SO.sub.2 R.sup.9c, --P(O)(OH).sub.2, R.sup.13, R.sup.15a,b are the same or different and mean hydrogen, C.sub.1 -C.sub.10 alkyl, aryl, C.sub.7 -C.sub.16 aralkyl, X.sup.1, X.sup.2 are the same or different and mean X, X can be hydrogen, halogen, --OH, --NO.sub.2, --N.sub.3, --CN, --NR.sup.15a R.sup.15b, --NHSO.sub.2 R.sup.15a, --CO.sub.2 R.sup.15, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, C.sub.1 -C.sub.10 acyloxy, C.sub.1 -C.sub.10 acyl, and, if R.sup.15 means hydrogen, their salts with physiologically compatible bases, as well as the .alpha.-, .beta.-or .gamma.-cyclodextrin clathrates, as well as the compounds of formula I that are encapsulated with liposomes.
摘要翻译： PCT No.PCT / EP95 / 01341 Sec。 371日期1997年1月3日 102（e）日期1997年1月3日PCT提交1995年4月13日PCT公布。 WO95 / 30650 PCT出版物日本公开号为1995年11月16日本发明涉及通式I的冰片衍生物，其中R1表示C（O）-CH（OR6）-CH（NHR7）-R8，R2表示氢，-OH，C1-C10 烷基，C1-C10烷氧基，-OC（O）R9a，-OSO2R9a，-OP（O）（OH）2，NHR9a，NR9aR9b，R3表示氢，-OH，C1-C10烷氧基，-OC（O）R9b， -OSO2R9b，-OP（O）（OH）2或R2，R3一起表示氧原子，R4表示氢，C1-C10烷基， - （CH2）n-OR11a，R5表示氢，C1-C10烷基，（CH2）p-OR11b或R4，R5一起表示氧原子，a = CHR10基，n表示0至8，p表示1至8，R7表示-C（O）R12，-SO2R12，-C（O ）OR 12，-C（O）NHR 9 d，-C（O）NR 9 d R 9e，R 8表示芳基，R 9a-基，R12相同或不同，表示C1-C10烷基，C4-C8环烷基，芳基，C7- C16芳烷基，R10表示氢，C1-C10烷基， - （CH2）s-OR14，s表示1至8，R6，R11a，b，R14相同或不同，表示氢，C1-C10烷基，芳基，C7 -C 16芳烷基，-SO 2 R 9c，-P（O）（OH）2，R 13，R 15a，b相同或不同，表示氢，C 1 -C 10烷基，芳基，C 7 -C 16芳烷基， X1，X2相同或不同，表示X，X可以是氢，卤素，-OH，-NO 2，-N3，-CN，-NR15aR15b，-NHSO2R15a，-CO2R15，C1-C10烷基，C1-C10烷氧基， C1-C10酰氧基，C1-C10酰基，如果R15表示氢，则它们与生理上相容的碱的盐以及α，β或γ-环糊精包合物以及被包封的式I化合物与脂质体。

3. 发明授权

US6025507A Borneol derivatives, methods of manufacturing them, and their pharmaceutical use 失效
标题翻译：苯并呋喃衍生物，制造方法及其药物用途
公开(公告)号：US6025507A
公开(公告)日：2000-02-15
申请号：US894180
申请日：1998-08-28
申请人： Ulrich Klar , Hernamm Graf , Gunter Neef , Siegfried Blechert
发明人： Ulrich Klar , Hernamm Graf , Gunter Neef , Siegfried Blechert
IPC分类号： A61K9/127 , A61K31/16 , A61K31/215 , A61P35/00 , A61P43/00 , C07C271/22 , C07D303/16 , C07D303/17 , A61K31/325 , A61K31/335
CPC分类号： C07D303/16 , C07C271/22 , C07C2103/86
摘要： Borneol derivatives of formula I ##STR1## in which R.sup.1 to R.sup.5 and X.sup.1 to X.sup.2 are defined in the specification, and the method of making the same.
摘要翻译： PCT No.PCT / DE96 / 00297 Sec。 371日期1998年8月28日 102（e）1998年8月28日PCT PCT 1996年2月19日PCT公布。公开号WO96 / 25392 日期：1996年8月22日在说明书中定义R1至R5和X1至X2的式I的波烯醇衍生物及其制备方法。

4. 发明授权

US6162920A Taxane derivatives having a pyridyl substituted C13 side chain, their preparation and their use as anti-tumor agents 失效
公开(公告)号：US6162920A
公开(公告)日：2000-12-19
申请号：US117506
申请日：1998-07-30
申请人： Ulrich Klar , Gunter Neef , Hermann Graf
发明人： Ulrich Klar , Gunter Neef , Hermann Graf
IPC分类号： C07D305/14 , A61K31/337 , A61K31/4427 , A61K31/445 , A61P35/00 , C07D405/12 , A61K31/44 , C07D405/04
CPC分类号： C07D405/12
摘要： The invention relates to pharmacologically active compounds that have the ability to influence the polymerisation and depolymerisation of tubulin.A range of natural mitosis toxins are used as anti-tumor agents or are in the process of being clinically tested. There are various classes of such mitosis toxins that either demonstrate their cytotoxic action by inhibiting the polymerisation of microtubules in the spindle system (for example, Vinca alkaloids, colchicine) or achieve their cytotoxic action by a GTP-independent increase in the polymerisation of the tubulin and by preventing the depolymerisation of microtubules (for example, taxol, taxoters).Owing to their physico-chemical properties, hitherto not understood, and as a result of the characteristics of neoplastic cells, mitosis toxins have a certain selectivity for tumor cells, but there still remains a not inconsiderable cytotoxicity towards non-transformed cells. The search for more selective compounds that are easier to manufacture and--like the taxane class of substances--are able to inhibit the depolymerisation of microtubules, had, surprisingly, led to the discovery of borneol esters, as described in P 4416374.6 and 19513040.5. Structural modifications in that class of compounds have revealed a considerable potential for optimisation in respect of the action on microtubules. Outstanding results have been obtained, inter alia, by formal esterification of those broneols with an acid of the Sk-H type. By synthesising the taxol derivatives described herein, in which the isoserine chain of the taxol has been replaced by Sk, the intention was to study whether it is also possible in that class of substances to achieve an improved stabilisation of microtubules, compared with taxol.

5. 发明授权

US6096732A Steroid esters, process for their production and their pharmaceutical use 失效
标题翻译：类固醇酯，其生产过程及其药物用途
公开(公告)号：US6096732A
公开(公告)日：2000-08-01
申请号：US986592
申请日：1997-12-08
申请人： Ulrich Klar , Arwed Cleve , Wolfgang Schwede , Gunter Neef , Eckhard Ottow , Kristof Chwalisz , Martin Schneider
发明人： Ulrich Klar , Arwed Cleve , Wolfgang Schwede , Gunter Neef , Eckhard Ottow , Kristof Chwalisz , Martin Schneider
IPC分类号： A61K31/565 , A61P35/00 , C07J53/00 , A61K31/56
CPC分类号： C07J53/002 , Y10S514/843
摘要： Steroid esters of formula I ##STR1## are described, wherein m, n and x are as defined by the specification. The compounds are distinguished from the basic hydroxy compounds by considerably improved solubility as well by increased biological activity and selectivity.The compounds are suitable for the production of pharmaceutical agents.
摘要翻译：描述式I的类固醇酯，其中m，n和x如本说明书所定义。通过显着改善溶解度以及增加的生物活性和选择性，化合物与碱性羟基化合物的区别。该化合物适用于生产药剂。

6. 发明授权

US06806263B2 Antigestagenically active steroids with a fluorinated 17-alpha-alkyl chain 失效
标题翻译：具有氟化17-α-烷基链的抗发生活性类固醇
公开(公告)号：US06806263B2
公开(公告)日：2004-10-19
申请号：US10304742
申请日：2002-11-27
申请人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
发明人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
IPC分类号： A61K3156
CPC分类号： C07J1/0033 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J53/002
摘要： 17&agr;-fluoroalkyl steroids of formula I as well as their physiologically compatible salts with acids and for —CO2R9 radicals with R9 meaning hydrogen, as well their physiologically compatible salts with bases, have an extraordinarily strong antigestagenic action and are suitable for the production of pharmaceutical preparations.
摘要翻译：具有式I的17α-氟烷基类固醇以及其与酸的生理上相容的盐以及具有R 9意义氢的-CO 2 R 9基团以及它们与碱的生理上相容的盐具有非常强的抗前体作用，并且适用于生产药物制剂。

7. 发明授权

US06503895B2 Antigestagenically active steroids with a fluorinated 17&agr;-alkyl chain 失效
标题翻译：具有氟化17α-烷基链的抗发生活性类固醇
公开(公告)号：US06503895B2
公开(公告)日：2003-01-07
申请号：US09978689
申请日：2001-10-18
申请人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
发明人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
IPC分类号： A61K3156
CPC分类号： C07J1/0033 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J53/002
摘要： This invention describes the new 17&agr;fluoroalkyl steroids of general formula I as well as their physiologically compatible salts with bases. The new compounds have an extraordinary strong antigestagenic action and are suitable for the production of pharmaceutical preparations.
摘要翻译：本发明描述了通式Ⅰ的新型17-氟烷基类固醇，以及它们与碱的生理上相容的盐。新化合物具有特别强的抗前列腺素作用，适用于制备药物制剂。

8. 发明申请

US20050080060A1 Antigestagenically active steroids with a fluorinated 17alpha-alkyl chain 失效
标题翻译：具有氟化17α-烷基链的抗发生活性类固醇
公开(公告)号：US20050080060A1
公开(公告)日：2005-04-14
申请号：US10948652
申请日：2004-09-24
申请人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
发明人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
IPC分类号： A61K31/56 , A61P5/36 , C07J1/00 , C07J41/00 , C07J43/00 , C07J53/00
CPC分类号： C07J1/0033 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J53/002
摘要： This invention describes the new 17α-fluoroalkyl steroids of general formula I in which R1 stands for a methyl or ethyl group, R2 stands for a radical of formula CnFmHo, whereby n is 2, 3, 4, 5 or 6, m>1 and m+o=2n+1, R3 stands for a free, etherified or esterified hydroxy group, R4 and R5 each stand for a hydrogen atom, or together for an additional bond or a methylene group, St stands for a steroidal ABC-ring system of partial formula A, B or C in which R6 means a hydrogen atom, a straight-chain C1-C4 alkyl group or branched C3-C4 alkyl group or a halogen atom, R7 means a hydrogen atom, a straight-chain C1-C4 alkyl group or a branched C3-C4 alkyl group, or if St stands for a steroidal ABC-ring system A or B, in addition R6 and R7 together can mean an additional bond, X means an oxygen atom, a hydroxyimino grouping ═N—OH or two hydrogen atoms, R8 means a radical Y or an aryl radical that is optionally substituted in several places with a group Y, whereby Y is a hydrogen atom, a halogen atom, an —OH, —NO2, —N3, —CN, —NR9aR9b, —NHSO2R9, —CO2R9, C1-C10 alkoxy, C1-C10 alkanoyloxy, benzoyloxy, C1-C10 alkanoyl, C1-C10 hydroxyalkyl or benzoyl group, and R9a and R9b are the same or different and in the same way as R9 represent a hydrogen atom or a C1-C10 alkyl group, and for —NR9aR9b radicals, as well as their physiologically compatible salts with acids and for —CO2R9 radicals with R9 meaning hydrogen, as well as their physiologically compatible salts with bases. The new compounds have an extraordinarily strong antigestagenic action and are suitable for the production of pharmaceutical preparations.
摘要翻译：本发明描述了通式I的新型17α-氟烷基类固醇，其中R 1代表甲基或乙基，R 2代表式C n F m H o基团，其中n为2,3,4,5或 6，m> 1和m + o = 2n + 1，R 3表示游离的醚化或酯化的羟基，R 4和R 5各自代表氢原子，或一起代表另外的键或亚甲基，St代表部分式A，B或C的甾族ABC-环体系，其中R 6表示氢原子，直链C 1 -C 4烷基或支链C 3 -C 4烷基或卤素原子，R 7表示氢原子，直链C 1 -C 4烷基或支链C 3 -C 4烷基，或者如果St代表甾族ABC环系统A或B，另外R R 6和R 7一起可以表示另外的键，X表示氧原子，羟基亚氨基= N-OH或两个氢原子，R 8表示任意取代的基团Y或芳基几个地方有一个Y组，Y是一个氢原子，卤素原子，-OH，-NO 2，-N 3，-CN，-NR 9a R 9b，-NHSO 2 R 9，-CO 2 R 9，C 1 -C 10烷氧基，C 1 -C 10 烷酰氧基，苯甲酰氧基，C 1 -C 10烷酰基，C 1 -C 10羟烷基或苯甲酰基，R 9a和R 9b相同或不同，并且R 9表示氢原子或C1- C10烷基，对于-NR 9a R 9b基团，以及它们与酸的生理上相容的盐以及具有R 9表示氢的-CO 2 R 9基团，以及它们与基地新化合物具有非常强的抗前体作用，适用于制备药物制剂。

9. 发明授权

US07148213B2 Antigestagenically active steroids with a fluorinated 17α-alkyl chain 失效
标题翻译：具有氟化17α-烷基链的抗发生活性类固醇
公开(公告)号：US07148213B2
公开(公告)日：2006-12-12
申请号：US10948652
申请日：2004-09-24
申请人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
发明人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
IPC分类号： A61K31/56
CPC分类号： C07J1/0033 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J53/002
摘要： This invention describes the new 17α-fluoroalkyl steroids of general formula I as well as their physiologically compatible salts with bases. The new compounds have an extraordinary strong antigestagenic action and are suitable for the production of pharmaceutical preparations.
摘要翻译：本发明描述了通式I的新的17α-氟烷基类固醇以及它们与碱的生理上相容的盐。新化合物具有非常强的抗前体作用，适用于制备药物制剂。

10. 发明授权

US06316432B1 Antigestagenically active steroids with a flourinated 17 &agr;-alkyl chain 失效
标题翻译：具有氟化17α-烷基链的抗发生活性类固醇
公开(公告)号：US06316432B1
公开(公告)日：2001-11-13
申请号：US09516359
申请日：2000-03-01
申请人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
发明人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
IPC分类号： A61K3156
CPC分类号： C07J1/0033 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J53/002
摘要： This invention describes the new 17&agr;-fluoroalkyl steroids of general formula I as well as their physiologically compatible salts with acids, and for —CO2R9 radicals with R9 meaning hydrogen as well as their physiologically compatible salts with bases. The new compounds have an extraordinarily strong antigestagenic action and are suitable for the production of pharmaceutical preparations.
摘要翻译：本发明描述了具有通式Ⅰ的新的17α-氟烷基类固醇以及它们与酸的生理上相容的盐，对于含有R9的-CO 2 R 9基团以及它们与碱的生理上相容的盐。新化合物具有非常强的抗前体作用适用于药物制剂的生产。

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