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11. 发明申请

WO2008040441A2 RADIOFLUORINATION 审中-公开
标题翻译：放射性氟化
公开(公告)号：WO2008040441A2
公开(公告)日：2008-04-10
申请号：PCT/EP2007008044
申请日：2007-09-07
申请人： BAYER SCHERING PHARMA AG , SRINIVASAN ANANTH , LEHMANN LUTZ , VOIGTMANN ULRIKE , STELLFELD TIMO , AMETAMEY SIMON , KLAR ULRICH , HOEHNE AILEEN , MU LINJING
发明人： SRINIVASAN ANANTH , LEHMANN LUTZ , VOIGTMANN ULRIKE , STELLFELD TIMO , AMETAMEY SIMON , KLAR ULRICH , HOEHNE AILEEN , MU LINJING
IPC分类号： A61K31/695 , A61K51/04 , A61K51/08 , C07F7/02 , C07K1/13
CPC分类号： C07K1/13 , A61K49/085 , A61K49/10 , A61K49/14 , A61K51/0491 , C07B59/004 , C07B59/008 , C07F7/0834 , C07F7/0896 , C07F7/12 , C07K7/02 , C07K7/086
摘要： The present invention relates to novel compounds suitable for or already radiolabeled with 18 F, methods of making such compounds and use of such compounds for diagnostic imaging. Such labeled vompounds are characerized by Formula II, wherein the moieties F, R 1 , R 2 , B 1,2, Y 1.2 ,, Z 1.2
摘要翻译：本发明涉及适用于或已经用<！ - SIPO - >已经放射性标记的新化合物，制备这些化合物的方法和用于诊断成像的这些化合物的用途。这种标记的化合物通过式II化合，其中部分F，R 1，R 2，B，1,2， 1.2，Z <1.2>

12. 发明申请

WO2009083268A3 17-(1'-PROPENYL)-17-3'-OXIDOESTRA-4-EN-3-ONE DERIVATIVE, USE THEREOF, AND MEDICAMENT CONTAINING SAID DERIVATIVE 审中-公开
标题翻译： 17-（1'-丙烯基）-17-3'-OXIDOESTRA -4-烯-3-酮衍生物，它们的用途及药物衍生物含
公开(公告)号：WO2009083268A3
公开(公告)日：2009-09-24
申请号：PCT/EP2008011161
申请日：2008-12-23
申请人： BAYER SCHERING PHARMA AG , KLAR ULRICH , KUHNKE JOACHIM , BOHLMANN ROLF , HUEBNER JAN , RING SVEN , FRENZEL THOMAS , MENGES FREDERIK , BORDEN STEFFEN , MUHN HANS PETER , PRELLE KATJA
发明人： KLAR ULRICH , KUHNKE JOACHIM , BOHLMANN ROLF , HUEBNER JAN , RING SVEN , FRENZEL THOMAS , MENGES FREDERIK , BORDEN STEFFEN , MUHN HANS PETER , PRELLE KATJA
IPC分类号： C07J21/00 , A61K31/58 , A61P5/26 , A61P5/34 , A61P5/42 , C07J41/00 , C07J53/00
CPC分类号： C07J21/00 , C07J41/0016 , C07J53/001 , C07J53/007
摘要： The invention relates to 17-(1'-propenyl)-17-3'-oxidoestra-4-en-3-one derivatives with general chemical formula (1) wherein the radicals Z, R4, R6a, R6b, R7, R15, R16a, R16b and R18 have the designations given in claim 1, and to the solvates, hydrates and salts thereof, including all stereoisomers of said compounds. The invention also relates to the use of said derivatives for producing a medicament for oral contraception and for the treatment of premenopausal, perimenopausal and postmenopausal complaints, and medicaments containing said derivatives, especially the application thereof in the cited cases. The derivatives according to the invention have a gestagenic effect, and in preferred cases, also an anti-mineral corticoidal and neutral to lightly androgenous effect.
摘要翻译：本发明涉及17-（1'-丙烯基）-17-3'-oxidoestra -4-烯-3-酮具有化学式（I）其中基团Z，R 4中，R 6a，经R 6b，R 7的衍生物， R15，R16A，R18和R 16b具有权利要求1中给出的含义，以及它们的溶剂化物，水合物和它们的盐，包括这些化合物的所有立体异构体。本发明还涉及使用这些衍生物用于制备药物的口服避孕和用于治疗前，绝经期和绝经后病症，以及含有这些衍生物中，在指示的前述情况下特定的应用的药物组合物。本发明的衍生物显示出促孕和在优选的情况下，也是一个抗盐和中性至微雄激素作用。

13. 发明申请

WO2009083267A2 STEROID-17,17-LACTOL DERIVATIVE, USE THEREOF, AND MEDICAMENT CONTAINING SAID DERIVATIVE 审中-公开
标题翻译：甾体-17,17-乳酸衍生物，它们的用途和衍生物药物
公开(公告)号：WO2009083267A2
公开(公告)日：2009-07-09
申请号：PCT/EP2008011160
申请日：2008-12-23
申请人： BAYER SCHERING PHARMA AG , FRENZEL THOMAS , KLAR ULRICH , KUHNKE JOACHIM , BOHLMANN ROLF , HUEBNER JAN , RING SVEN , MENGES FREDERIK , BORDEN STEFFEN , MUHN HANS PETER , PRELLE KATJA
发明人： FRENZEL THOMAS , KLAR ULRICH , KUHNKE JOACHIM , BOHLMANN ROLF , HUEBNER JAN , RING SVEN , MENGES FREDERIK , BORDEN STEFFEN , MUHN HANS PETER , PRELLE KATJA
IPC分类号： C07J53/00 , A61K31/58 , A61P5/34 , A61P5/42
CPC分类号： C07J53/001 , C07J53/007
摘要： The invention relates to steroid-17, 17-lactol-derivatives with the chemical formula (I) and the tautomer forms thereof with general chemical formula (Ia) wherein R4, R6a, R6b, R7, R15, R16a, R16b, R18, R22and Z have the designations given in claim 1, and to the solvates, hydrates, stereoisomers and salts thereof. The invention also relates to the use of said derivatives for producing a medicament for oral contraception and for the treatment of premenopausal, perimenopausal and postmenopausal troubles, and medicaments containing said derivatives. The derivatives according to the invention have a gestagen effect, and in preferred cases, also an anti-mineral corticoid and neutral to lightly androgenous effect.
摘要翻译：本发明涉及类固醇-17，具有化学式（I）以及具有化学式（Ia）及其互变异构形式17-乳醇衍生物，其中R 4中，R 6a，经R 6b，R 7，R 15，R16A，R 16B，R 18， R22和Z具有权利要求1中给出的含义，以及它们的溶剂合物，水合物，立体异构体和盐。本发明进一步涉及这些衍生物在制造用于口服避孕药物和治疗绝经前后，绝经期和绝经后疾病的药物以及含有这些衍生物的药物中的用途。根据本发明的衍生物具有孕激素作用，并且在优选的情况下还具有抗矿物质类固醇和中性到轻度雄激素作用。

14. 发明申请

WO2008151746A3 17ß-CYANO-19-NOR-ANDROST-4-ENE DERIVATIVE, USE THEREOF AND MEDICAMENTS CONTAINING SAID DERIVATIVE 审中-公开
标题翻译： 17-氰基-19-去甲雄甾-4-烯衍生物，其用途及药物含有该衍生物的
公开(公告)号：WO2008151746A3
公开(公告)日：2009-03-12
申请号：PCT/EP2008004429
申请日：2008-06-04
申请人： BAYER SCHERING PHARMA AG , KUHNKE JOACHIM , HUEBNER JAN , BOHLMANN ROLF , FRENZEL THOMAS , KLAR ULRICH , MENGES FREDERIK , RING SVEN , BORDEN STEFFEN , MUHN HANS-PETER , PRELLE KATJA
发明人： KUHNKE JOACHIM , HUEBNER JAN , BOHLMANN ROLF , FRENZEL THOMAS , KLAR ULRICH , MENGES FREDERIK , RING SVEN , BORDEN STEFFEN , MUHN HANS-PETER , PRELLE KATJA
IPC分类号： C07J53/00 , A61K31/56 , A61P5/34 , C07J41/00
CPC分类号： C07J53/008 , C07J41/0094 , C07J53/007
摘要： The 17ß-cyano-19-nor-androst-4-ene derivatives of the present invention have gestagenic activity. They have the general chemical formula (1), in which Z is selected from the group comprising O, two hydrogen atoms, NOR and NNHSO2R, wherein R is hydrogen or C1-C4 alkyl, R4 is hydrogen or halogen and in addition either: R6a, R6b together form methylene or 1,2 ethanediyl or R6a is hydrogen and R6b is selected from the group comprising hydrogen, methyl and hydroxymethylene, and R7 is selected from the group comprising hydrogen, C1-C4 alkyl, C2-C3 alkenyl and cyclopropyl, or: R6a is hydrogen and R6b and R7 together form methylene, or are omitted, whereby a double bond is formed between C6 and C7, R9 and R10 are hydrogen, or are omitted, whereby a double bond is formed between C9 and C10, R15 and R16 are hydrogen or together form methylene, R17 is selected from the group comprising hydrogen, C1-C4 alkyl and aIIyI, at least one of the substituents R4, R6a, R6b, R7, R15, R16 and R17 not being hydrogen, or R6b and R7 being omitted, whereby a double bond is formed between C6 and C7. The derivatives also comprise the solvates, hydrates, stereoisomers, diastereomers, enantiomers and salts of the aforementioned substances.
摘要翻译：本发明的17-氰基-19-去甲雄甾-4-烯衍生物具有促孕活性。它们具有一般化学式（1）所示，在Z选自选自包含O，两个氢原子的组中选出，NOR和NNHSO2R，其中R是氢或C1-C4烷基，R 4是氢或卤素，其还可以：R6A ，R 6b中一起形成亚甲基或1,2-乙二基或R 6a是氢和R 6b是选自包含氢，亚甲基和羟基亚甲基，且R 7选自包含氢，C1-C4烷基，C2-C3 烯基和环丙基，或，R 6a是氢，且R 6b和R 7一起形成亚甲基或消除以形成C6和C7，R9之间的双键，R 10是氢或消除以形成C9和C10，R15之间的双键，是R16是氢或共同形成亚甲基，R17选自包含氢，C 1 -C 4烷基和烯丙基，其中取代基R4中，R 6a，经R 6b，R 7，R 15，R16和R17中的至少一个不是氢或R 6b和R R7 unte选择 R型C6和C7之间entfllen双键，并且还包括它们的溶剂合物，水合物; 立体异构体，非对映体，对映体和盐。

15. 发明申请

WO2008152112A2 17ß-CYANO-19-ANDROST-4-ENE DERIVATIVE, USE THEREOF AND MEDICAMENTS CONTAINING SAID DERIVATIVE 审中-公开
标题翻译： 17-氰基-19-雄甾-4-烯衍生物，其用途及药物含有该衍生物的
公开(公告)号：WO2008152112A2
公开(公告)日：2008-12-18
申请号：PCT/EP2008057427
申请日：2008-06-12
申请人： BAYER SCHERING PHARMA AG , KUHNKE JOACHIM , HUEBNER JAN , BOHLMANN ROLF , FRENZEL THOMAS , KLAR ULRICH , MENGES FREDERIK , RING SVEN , BORDEN STEFFEN , MUHN HANS-PETER , PRELLE KATJA
发明人： KUHNKE JOACHIM , HUEBNER JAN , BOHLMANN ROLF , FRENZEL THOMAS , KLAR ULRICH , MENGES FREDERIK , RING SVEN , BORDEN STEFFEN , MUHN HANS-PETER , PRELLE KATJA
IPC分类号： C07J41/00 , C07J53/00
CPC分类号： C07J41/0094 , C07J53/007 , C07J53/008
摘要： The 17ß-cyano-19-androst-4-ene derivatives of the present invention have gestagenic activity. They have the general chemical formula (1), in which Z is selected from the group comprising O, two hydrogen atoms, NOR and NNHSO2R, wherein R is hydrogen or C1-C4 alkyl, R1 and R2 independently of one another are hydrogen or methyl, or R1 and R2 together form methylene, or are omitted, whereby a double bond is formed between C1 and C2, R4 is hydrogen or halogen and in addition either: R6a, R6b together form methylene or 1,2 ethanediyl or R6a is hydrogen and R6b is selected from the group comprising hydrogen, methyl and hydroxymethylene, and R7 is selected from the group comprising hydrogen, C1-C4 alkyl, C2-C3 alkenyl and cyclopropyl, or: R6a is hydrogen and R6b and R7 together form methylene, or are omitted, whereby a double bond is formed between C6 and C7, or: R6a is methyl and R6b and R7 are omitted, whereby a double bond is formed between C6 and C7, R15 and R16 are hydrogen, or together form methylene and R17 is selected from the group comprising hydrogen, C1-C4- alkyl and aIIyI. The derivatives also comprise the solvates, hydrates, stereoisomers, diastereomers, enantiomers and salts of the aforementioned substances, with the proviso that certain compounds are excluded.
摘要翻译：本发明的17-氰基-19-雄甾-4-烯衍生物具有促孕活性。它们具有一般化学式（1）所示，在Z选自选自包含O，两个氢原子的组中选出，NOR和NNHSO2R，其中R是氢或C1-C4烷基，R1，R2彼此独立地是氢或甲基或 R1和R2一起形成亚甲基或消除，以形成C1和C2之间的双键，是进一步任一R 4为氢或卤素：R6A，经R 6b一起形成亚甲基或1,2-乙二基或R 6a和R 6b为选自氢被选择时，包括氢，甲基和羟基亚甲基，且R 7选自包括氢，C1-C4烷基，C2-C3链烯基和环丙基，或，R 6a是氢，且R 6b和R 7一起形成亚甲基或形成C 6和C之间的双键 C7省略或R6a和R6b和R 7是甲基消除以形成C6和C7，R15，R16之间的双键被氢，或者一起形成亚甲基，R17选自ù选择 mfassend氢，C1-C4烷基和烯丙基，并且还包括它们的溶剂合物，水合物，立体异构体，非对映体，对映体和盐，与被排除某些化合物为条件。

16. 发明申请

WO0181342A2 NOVEL EPOTHILONE DERIVATIVES, METHOD FOR THE PREPARATION THEREOF AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译：新的埃博霉素衍生物，PROCESS FOR THEIR和制药用
公开(公告)号：WO0181342A2
公开(公告)日：2001-11-01
申请号：PCT/EP0104552
申请日：2001-04-19
申请人： SCHERING AG , BUCHMANN BERND , KLAR ULRICH , SKUBALLA WERNER , SCHWEDE WOLFGANG , LICHTNER ROSEMARIE , HOFFMANN JENS
发明人： BUCHMANN BERND , KLAR ULRICH , SKUBALLA WERNER , SCHWEDE WOLFGANG , LICHTNER ROSEMARIE , HOFFMANN JENS
IPC分类号： A61K31/427 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D401/06 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D491/04 , C07D493/04 , C07D493/10 , C07D498/04 , C07D419/06 , A61K31/42 , A61K31/425 , A61K31/44
CPC分类号： C07D401/06 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D491/04 , C07D493/04 , C07D493/10 , Y02P20/55
摘要： The invention relates to novel epothilone derivatives of general formula (I), wherein R represents a halogen atom or a cyano group and the other substituents have the meanings as cited in the description. The novel compounds interact with tubulin by stabilizing formed microtubules. They are capable of influencing the cell division in a phase-specific manner and are well-suited for the treatment of malignant tumors, for example, ovarian, stomach, colon, adeno, breast, lung, head and neck carcinomas, malignant melanoma, acute lymphocytic and myelocytic leukemia. In addition, they are well-suited for anti-angiogenesis therapy and for the treatment of chronic inflammable medical disorders (psoriasis, arthritis). In order to prevent uncontrolled cell growths as well as to improve the compatibility of medical implants, the inventive epothilone derivatives can be applied to or introduced into polymeric materials. The inventive compounds can be used alone or in order to obtain additive or synergistic effects, in conjunction with additional principles and substance classes that can be used in tumor therapy.
摘要翻译：本发明描述了通式I的埃坡霉素的新衍生物，其中R <5>表示卤原子或氰基，而另一取代基具有本说明书中给出的含义。所述新的化合物通过稳定微管形成与微管蛋白相互作用。它们能够影响细胞分裂期特异性和适用于治疗恶性肿瘤，如卵巢癌，胃癌，结肠癌，腺，乳腺，肺，头和颈癌，恶性黑色素瘤，急性淋巴细胞和myelocytäre白血病。它们也适用于抗血管生成治疗和用于慢性炎症性疾病（银屑病关节炎）的治疗。为了避免上不受控制的细胞生长和医疗植入物的更好的相容性，它们可以向上移动到聚合物材料或贡献。新化合物可单独使用或以达到添加剂或与其它肿瘤治疗适用的原则和物质类组合的协同效应。

17. 发明申请

WO9907692A2 NEW EPOTHILONE DERIVATIVES, METHOD FOR PRODUCING SAME AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译：新的爱泼罗宁衍生物，其制备方法和它们的药物使用
公开(公告)号：WO9907692A2
公开(公告)日：1999-02-18
申请号：PCT/EP9805064
申请日：1998-08-10
申请人： SCHERING AG , KLAR ULRICH , SCHWEDE WOLFGANG , SKUBALLA WERNER , BUCHMANN BERND , SCHIRNER MICHAEL
发明人： KLAR ULRICH , SCHWEDE WOLFGANG , SKUBALLA WERNER , BUCHMANN BERND , SCHIRNER MICHAEL
IPC分类号： C07D313/00 , A61K31/335 , A61K31/427 , A61K31/4427 , A61K31/443 , A61P35/00 , A61P43/00 , C07C45/29 , C07C45/56 , C07C45/67 , C07C49/185 , C07C49/337 , C07C49/355 , C07C51/31 , C07C59/185 , C07D213/50 , C07D213/55 , C07D263/22 , C07D277/22 , C07D277/24 , C07D307/33 , C07D309/12 , C07D319/06 , C07D319/08 , C07D319/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/04 , C07D407/12 , C07D417/06 , C07D417/12 , C07D417/14 , C07D493/04 , C07F7/18
CPC分类号： C07D307/33 , C07C45/29 , C07C45/56 , C07C45/673 , C07C49/185 , C07C49/337 , C07C49/355 , C07C59/185 , C07D213/50 , C07D213/55 , C07D263/22 , C07D277/24 , C07D309/12 , C07D319/06 , C07D319/08 , C07D319/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/04 , C07D407/12 , C07D417/06 , C07D417/12 , C07D417/14 , C07D493/04 , C07F7/1852 , C07F7/1856 , Y02P20/55
摘要： The invention relates to new epothilone derivatives of the general formula (I), in which the substituents Y, Z, R , R , R , R , D-E, R , R , R , R and X have the meanings assigned to them in the description. The new compounds interact with tubulin by stabilizing formed microtubuli. They are capable of influencing cell division in a phase-specific manner and are suitable for the treatment of malignant tumours, such as ovarian, gastric, colon, breast, lung, head and neck carcinoma, adenocarcinoma, malignant melanoma, and acute lymphocytic and myelocytic leukaemia. They are also suited for anti-angiogenesis therapy and for the treatment of chronic inflammatory diseases (psoriasis, arthritis). To prevent uncontrolled cell growth on, and for better tolerability of, medical implants, the derivatives can be introduced into or applied to polymeric materials. The compounds provided for in the invention can be used alone or, to achieve additive or synergistic effects, in combination with other principles and substance categories used in tumour therapy.
摘要翻译：本发明涉及通式（I）的新的埃坡霉素衍生物，其中取代基Y，Z，R <2A>，R <2B>，R <3>，R <4A> - [R <4B>，DE，R R 5，R 6，R 7，R 8和X具有说明书中指定的含义。新化合物通过稳定形成的微管与微管蛋白相互作用。它们能够影响细胞分裂期特异性和适用于治疗恶性肿瘤，如卵巢癌，胃癌，结肠癌，腺，乳腺，肺，头和颈癌，恶性黑色素瘤，急性淋巴细胞和髓细胞性白血病。此外，它们适用于抗血管生成疗法和治疗慢性炎症性疾病（牛皮癣，关节炎）。为了避免不受控制的细胞增殖以及医疗植入物的更好的相容性，可以将它们掺入或掺入聚合物材料中。根据本发明的化合物可以单独使用或与可用于肿瘤治疗的其他原理和物质类别组合使用实现叠加或协同效应。

18. 发明申请

WO0049020A3 NOVEL EPOTHILON DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND THEIR PHARMACEUTICAL APPLICATION 审中-公开
标题翻译：新的埃博霉素衍生物，PROCESS FOR THEIR和制药用
公开(公告)号：WO0049020A3
公开(公告)日：2000-12-28
申请号：PCT/EP0001332
申请日：2000-02-18
申请人： SCHERING AG , KLAR ULRICH , SCHWEDE WOLFGANG , BUCHMANN BERND , SKUBALLA WERNER , SCHIRNER MICHAEL , GRIMM MICHAEL
发明人： KLAR ULRICH , SCHWEDE WOLFGANG , BUCHMANN BERND , SKUBALLA WERNER , SCHIRNER MICHAEL , GRIMM MICHAEL
IPC分类号： C07D417/06 , A61K31/427 , A61K31/4427 , A61P35/00 , C07D405/06 , C07D493/08
CPC分类号： C07D417/06 , Y02P20/55
摘要： The invention relates to novel epothilon derivatives of general formula (I), wherein the substituents Y, Z, R , R , R , R , R , R , E, R , R , R , R , R and X have the meanings cited more specifically in the description. The novel compounds interact with tubulin by stabilizing the formed microtubuli. The compounds are able to influence the cell division in a phase-specific manner and are suited for treating malignant tumors, for example, ovarian cancer, gastric carcinoma, colon cancer, breast cancer, lung cancer, head and neck cancer, malignant melanoma, and acute lymphocytic and myelocytic leukemia. The inventive compounds are suited for use in anti-angiogenic therapy as well as for treating chronic inflammatory diseases (psoriasis, arthritis). In order to prevent uncontrolled cell proliferations and to improve the compatibility of medical implants, the inventive compounds can be applied or incorporated in polymeric materials. The inventive compounds can be used alone or, in order to achieve additive or synergistic effects, in conjunction with additional constituents and substance classes which can be use in tumor therapy.
摘要翻译：本发明涉及通式（I）的新的埃坡霉素衍生物，其中取代基Y，Z，R <1A>，R <1B>，R <2A>，R <2B>，R <3A>，R < 图3b>，E，R <5> - [R <6> - [R <7> - [R <8>，R <14>和X具有说明书中更详细地给出的含义。所述新的化合物通过稳定微管形成与微管蛋白相互作用。它们能够影响细胞分裂期特异性和适用于治疗恶性肿瘤，如卵巢癌，胃癌，结肠癌，腺，乳腺，肺，头和颈癌，恶性黑色素瘤，急性淋巴细胞和myelocytäre白血病。它们也适用于抗血管生成治疗和用于慢性炎症性疾病（银屑病关节炎）的治疗。为了避免上不受控制的细胞生长和医疗植入物的更好的相容性，它们可以向上移动到聚合物材料或贡献。新化合物可单独使用或以达到添加剂或与其它肿瘤治疗适用的原则和物质类组合的协同效应。

19. 发明申请

WO0181341A3 9-oxa-epothilon derivatives, method for the production and use thereof in pharmaceutical preparations 审中-公开
标题翻译： -9-氧杂埃坡霉素衍生物及其制备方法和它们在药物制剂使用
公开(公告)号：WO0181341A3
公开(公告)日：2002-04-25
申请号：PCT/EP0104551
申请日：2001-04-19
申请人： SCHWEDE WOLFGANG , KLAR ULRICH , HOFFMANN JENS , SCHERING AG
发明人： SCHWEDE WOLFGANG , BUCHMANN BERND , LICHTNER ROSEMARY , KLAR ULRICH , HOFFMANN JENS
IPC分类号： A61K31/427 , A61P35/00 , C07D405/04 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/06 , C07D493/04 , C07D493/10 , C07D498/04 , C07D498/10 , A61K31/425 , C07D417/04 , C07D471/06
CPC分类号： C07D405/04 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/06 , C07D493/04 , C07D493/10 , Y02P20/55
摘要： The invention relates to novel epothilon derivatives which are characterized by an oxygen atom in position 9 of the epothilon skeleton. The novel compounds interact with tubulin, stabilizing formed microtubuli. They can influence cell division in a phase-specific manner and are suitable for use in the treatment of malignant tumors such as ovarian, stomach, colon, adeno, breast, lungs, head and neck carcinoma, malignant melanoma, acute lymphocytic and myelocytic leukaemia. They are also suitable for anti-angiogenesis thereapy and for use in the treatment of chronic inflamatory diseases (psoriasis, arthritis). In order to avoid uncontrolled proliferation of cells on and to improve the compatibility of medical implants, they can be placed on or in polymer materials. The inventive compounds can be used on their own or to obtain additive or synergistic effects in combination with other classes of substances and principles which can be used in tumoral therapy.

20. 发明申请

WO0049019A3 NOVEL EPOTHILONE DERIVATIVES, METHOD FOR PRODUCING THEM AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译：新的埃博霉素衍生物，PROCESS FOR THEIR和制药用
公开(公告)号：WO0049019A3
公开(公告)日：2001-03-01
申请号：PCT/EP0001331
申请日：2000-02-18
申请人： SCHERING AG , KLAR ULRICH , SCHWEDE WOLFGANG , SKUBALLA WERNER , BUCHMANN BERND , SCHIRNER MICHAEL , MENRAD ANDREAS
发明人： KLAR ULRICH , SCHWEDE WOLFGANG , SKUBALLA WERNER , BUCHMANN BERND , SCHIRNER MICHAEL , MENRAD ANDREAS
IPC分类号： C07D405/06 , C07D417/06 , C07D493/04 , C07D493/08 , C07D493/10 , C07D493/14 , C07D493/20 , C07F7/18 , A61K31/427 , A61P35/00
CPC分类号： C07D405/06 , C07D417/06 , C07D493/04 , C07D493/08 , C07D493/10 , C07D493/14 , C07F7/1856 , Y02P20/55
摘要： The invention relates to novel epothilone derivatives of general formula (I), wherein the substituents Y, Z, R , R , R , R , G'-G-E-E', R , R , R , R , R and X have the meanings specified in the description. The novel compounds interact with tubulin by stabilising the microtubuli which are formed. They are able to influence the cell division phase-specifically and are suitable for treating malignant tumours such as cancers of the ovaries, stomach, colon, glands, breasts, lungs and head and neck, malignant melanoma and acute lymphocytic and myelocytic leukaemia. The compounds are also suitable for anti-angiogenesis therapy and for treating chronic inflammatory diseases (psoriasis, arthritis) and can be deposited on or in polymer materials in order to prevent uncontrolled cell proliferations on medical implants and to improve the compatibility thereof. The inventive compounds can be used alone or in combination with other principles and classes of substances that can be used in the therapy of tumours in order to achieve additive or synergistic effects.
摘要翻译：本发明涉及通式（I），其中取代基Y，Z，R <1A>，R <1B>，R <2A>，R <2B>，G 'GE-E' 的新的埃坡霉素衍生物，R <5> - [R <6> - [R <7> - [R <8>，R <14>和X具有说明书中更详细地给出的含义。所述新的化合物通过稳定微管形成与微管蛋白相互作用。它们能够影响细胞分裂期特异性和适用于治疗恶性肿瘤，如卵巢癌，胃癌，结肠癌，腺，乳腺，肺，头和颈癌，恶性黑色素瘤，急性淋巴细胞和myelocytäre白血病。它们也适用于抗血管生成治疗和用于慢性炎症性疾病（银屑病关节炎）的治疗。为了避免上不受控制的细胞生长和医疗植入物的更好的相容性，它们可以向上移动到聚合物材料或贡献。新化合物可单独使用或以达到添加剂或与其它肿瘤治疗适用的原则和物质类组合的协同效应。

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