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51. 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 By synthesising the taxol derivatives described herein, in which the isoserine chain of the taxol has been replaced by Sk, the intention was to study whether it is also possible in that class of substances to achieve an improved stabilisation of microtubules, compared with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.

52. 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。

53. 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。

54. 发明授权

US5663157A 22-en-25-oxa derivatives in the vitamin D series, process for their production, pharmaceutical preparations containing these derivatives as well as their use as pharmaceutical agents 失效
标题翻译：维生素D系列中的22-en-25-氧杂衍生物，其制备方法，含有这些衍生物的药物制剂及其作为药剂的用途
公开(公告)号：US5663157A
公开(公告)日：1997-09-02
申请号：US362438
申请日：1995-03-16
申请人： Andreas Steinmeyer , Gerald Kirsch , Gunter Neef , Katica Schwarz , Ruth Thieroff-Ekerdt , Herbert Wiesinger , Martin Haberey
发明人： Andreas Steinmeyer , Gerald Kirsch , Gunter Neef , Katica Schwarz , Ruth Thieroff-Ekerdt , Herbert Wiesinger , Martin Haberey
IPC分类号： A61K31/59 , A61P3/02 , A61P17/00 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/06 , C07C401/00 , C07F7/18
CPC分类号： C07F7/1852 , C07C401/00
摘要： 22-En-24-a-oxa derivatives in the vitamin D series of general formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.4, independently of one another, each mean a hydrogen atom, an alkanoyl group with 1 to 9 carbon atoms or an aroyl group,R.sup.3 mean a hydrogen atom each or a linear or branched alkyl group each with 1 to 4 carbon atoms, a trifluoromethyl group each or a saturated or unsaturated carbocyclic or heterocyclic 3-, 4-, 5- or 6-membered ring formed together with the tertiary carbon atom, andX means an alkylene radical --(CH.sub.2).sub.n --with n=1, 2 or 3, process for their production and their pharmaceutical use for treating hyperproliferative diseases are disclosed.
摘要翻译： PCT No.PCT / EP93 / 01735 Sec。 371日期1995年3月16日 102（e）日期1995年3月16日PCT Filed 1993年6月30日PCT公布。第WO94 / 00429号公报日期1994年1月6日22-通式I（I）的维生素D系列中的En-24-α-氧杂衍生物，其中R 1，R 2和R 4彼此独立地各自表示氢原子，具有1至9个碳原子的烷酰基或芳酰基，R 3表示氢原子或各自具有1至4个碳原子的直链或支链烷基，三氟甲基或饱和或不饱和的碳环或杂环3-，4 - ，与叔碳原子一起形成的5-或6-元环，X表示具有n = 1,2或3的亚烷基 - （CH 2）n - ，其制备方法及其用于治疗过度增殖性疾病的药物用途被披露。

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