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1. 发明申请

WO2011157443A1 (11B,17A)-11-(4-(2-11C-ACETYL)PHENYL)-17,23-EPOXY-19,24-DINORCHOLA-4,9,20-TRIEN-3-ONE 审中-公开
标题翻译：（11B，17A）-11-（4-（2-11C - 乙酰基）苯基）-17,23-EPOXY-19,24-DINORCHOLA-4,9,20三烯-3-酮
公开(公告)号：WO2011157443A1
公开(公告)日：2011-12-22
申请号：PCT/EP2011/003012
申请日：2011-06-17
申请人： N.V. ORGANON , BRANDS, Franciscus Theodorus Leonardus , HAMERSMA, Johannes, Antonius, Maria , WIEGERINCK, Peter, Hermanus, Gerardus
发明人： BRANDS, Franciscus Theodorus Leonardus , HAMERSMA, Johannes, Antonius, Maria , WIEGERINCK, Peter, Hermanus, Gerardus
IPC分类号： C07J21/00 , A61K31/58 , G01N33/74 , A61P5/36
CPC分类号： C07J53/001 , A61K51/0493 , C07J21/00
摘要： The present invention relates to (11β,17α)-11-(4-(2- 11 C-acetyl)phenyl)-17,23- epoxy-19,24-dinorchola-4,9,20-trien-3-one, an 11 C-labelled ORG 33628; a process for the preparation thereof, intermediates used in this process and the use of this compound as a PET tracer for the detection of breast cancer.
摘要翻译：本发明涉及（11β，17a）-11-（4-（2-11C-乙酰基）苯基）-17,23-环氧-19,24-二肉豆蔻-4,9,20-三烯-3-酮， 11C标记的ORG 33628; 其制备方法，该方法中使用的中间体以及该化合物作为PET示踪剂用于检测乳腺癌的用途。

2. 发明申请

WO2011157443A8 (11ß,17a)-11-(4-(2-11C-ACETYL)PHENYL)-17,23-EPOXY- 19,24-DINORCHOLA-4,9,20-TRIEN-3-ONE 审中-公开
标题翻译：（11β，17α）-11-（4-（2-11C-乙酰基）苯基）-17,23-环氧-29,24-十八醇-4,9,20-三烯-3-酮
公开(公告)号：WO2011157443A8
公开(公告)日：2012-08-02
申请号：PCT/EP2011003012
申请日：2011-06-17
申请人： MSD OSS BV , BRANDS FRANCISCUS THEODORUS LEONARDUS , HAMERSMA JOHANNES ANTONIUS MARIA , WIEGERINCK PETER HERMANUS GERARDUS
发明人： BRANDS FRANCISCUS THEODORUS LEONARDUS , HAMERSMA JOHANNES ANTONIUS MARIA , WIEGERINCK PETER HERMANUS GERARDUS
IPC分类号： C07J21/00 , A61K31/58 , A61P5/36 , G01N33/74
CPC分类号： C07J53/001 , A61K51/0493 , C07J21/00
摘要： The present invention relates to (11ß,17a)-11-(4-(2-11C-acetyl)phenyl)-17,23- epoxy-19,24-dinorchola-4,9,20-trien-3-one, an 11C-labelled ORG 33628; a process for the preparation thereof, intermediates used in this process and the use of this compound as a PET tracer for the detection of breast cancer.
摘要翻译：本发明涉及（11β，17a）-11-（4-（2-11C-乙酰基）苯基）-17,23-环氧-19,24-二肉豆蔻-4,9,20-三烯-3-酮， 11C标记的ORG 33628; 其制备方法，该方法中使用的中间体以及该化合物作为PET示踪剂用于检测乳腺癌的用途。

3. 发明申请

WO2005092912A1 PROGESTERONE RECEPTOR MODULATORS 审中-公开
标题翻译：孕激素受体调节剂
公开(公告)号：WO2005092912A1
公开(公告)日：2005-10-06
申请号：PCT/EP2005/051265
申请日：2005-03-18
申请人： AKZO NOBEL N.V. , HAMERSMA, Johannes, Antonius, Maria , REWINKEL, Johannes, Bernardus, Maria
发明人： HAMERSMA, Johannes, Antonius, Maria , REWINKEL, Johannes, Bernardus, Maria
IPC分类号： C07J43/00
CPC分类号： C07J43/003 , C07J5/00 , C07J43/00 , C07J53/001
摘要： The subject invention provides a compound according to Formula I, wherein Formula (1) is O, NOH, NO(1-4C)alkyl, NO(1-4C)acyl; Al-A5 are C, substituted with RI, or N, provided that at least one and not more than three of Al-A5 are N; or one or two of Al, A2 and A5 are N, and the others are C, substituted with Rl, and A3 and A4 together represent a fused benzo ring or a fused five- or six-membered nitrogen-containing aromatic ring, both optionally substituted with one or more halogen and/or (1-4C)alkyl; RI is H, halogen, (1 -4C)alkyl, (1 -4C)alkoxy; R2 is H, (1-4C)alkyl or (1-6C)alkenyl, both optionally substituted with an (6-10)aryl group, which is optionally substituted with one or more halogen and/or (1-4C)alkyl; and R3 is H or (1-4C)alkyl, optionally substituted with one or more halogen atoms; and R4 is cyclopropyl or cyclopropenyl, both optionally substituted with one or more halogen and/or (1-4C)alkyl; or R2 together with R3 forms a 3-, 4-, 5- or 6-membered carbocyclic ring; and R4 is cyclopropyl or cyclopropenyl, both optionally substituted with one or more halogen and/or (1-4C)alkyl); or R2 is H or (1-4C)alkyl; and R3 together with R4 forms a 5-, 6- or 7-membered saturated or unsaturated carbocyclic ring; R5 is H or (1-4C)alkyl; or a pharmaceutically acceptable salt and/or hydrate form and/or prodrug thereof.
摘要翻译：本发明提供式I化合物，其中式（1）为O，NOH，NO（1-4C）烷基，NO（1-4C）酰基; Al-A5是C，被RI或N取代，条件是Al-A5中至少一个不超过三个是N; 或者A1，A2和A5中的一个或两个为N，其余为C，被R1取代，A3和A4一起代表稠合的苯并环或稠合的五元或六元含氮芳香环，被一个或多个卤素和/或（1-4C）烷基取代; R 1是H，卤素，（1-4C）烷基，（1-4C）烷氧基; R 2是H，（1-4C）烷基或（1-6C）烯基，两者任选地被（6-10）芳基取代，其任选被一个或多个卤素和/或（1-4C）烷基取代; 并且R 3是H或（1-4C）烷基，任选地被一个或多个卤素原子取代; 并且R 4是环丙基或环丙烯基，其任选被一个或多个卤素和/或（1-4C）烷基取代; 或R 2与R 3一起形成3-，4-，5-或6-元碳环; 并且R 4是环丙基或环丙烯基，两者均任选被一个或多个卤素和/或（1-4C）烷基取代）; 或R 2为H或（1-4C）烷基; 并且R 3与R 4一起形成5-，6-或7-元饱和或不饱和碳环; R5是H或（1-4C）烷基; 或其药学上可接受的盐和/或水合物形式和/或前药。

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