发明申请
WO2009095872A3 LABELLED ANALOGUES OF HALOBENZAMIDES AS MULTIMODAL RADIOPHARMACEUTICALS AND THEIR PRECURSORS
审中-公开
基本信息:
- 专利标题： LABELLED ANALOGUES OF HALOBENZAMIDES AS MULTIMODAL RADIOPHARMACEUTICALS AND THEIR PRECURSORS
- 专利标题（中）：作为多模式放射治疗剂及其前体的哈芬碱的标记类似物
- 申请号：PCT/IB2009050355 申请日：2009-01-28
- 公开(公告)号：WO2009095872A3 公开(公告)日：2009-12-03
- 发明人： CHEZAL JEAN-MICHEL , DOLLE FREDERIC , MADELMONT JEAN-CLAUDE , MAISONIAL AURELIE , MIOT-NOIRAULT ELISABETH , MOINS NICOLE , PAPON JANINE , KUHNAST BERTAND , TAVITIAN BERTRAND , BOISGARD RAPHAEL
- 申请人： INST NAT SANTE RECH MED , COMMISSARIAT ENERGIE ATOMIQUE , UNIV D AUVERGNE CLERMONT 1 , CYCLOPHARMA LAB , CHEZAL JEAN-MICHEL , DOLLE FREDERIC , MADELMONT JEAN-CLAUDE , MAISONIAL AURELIE , MIOT-NOIRAULT ELISABETH , MOINS NICOLE , PAPON JANINE , KUHNAST BERTAND , TAVITIAN BERTRAND , BOISGARD RAPHAEL
- 专利权人： INST NAT SANTE RECH MED,COMMISSARIAT ENERGIE ATOMIQUE,UNIV D AUVERGNE CLERMONT 1,CYCLOPHARMA LAB,CHEZAL JEAN-MICHEL,DOLLE FREDERIC,MADELMONT JEAN-CLAUDE,MAISONIAL AURELIE,MIOT-NOIRAULT ELISABETH,MOINS NICOLE,PAPON JANINE,KUHNAST BERTAND,TAVITIAN BERTRAND,BOISGARD RAPHAEL
- 当前专利权人： INST NAT SANTE RECH MED,COMMISSARIAT ENERGIE ATOMIQUE,UNIV D AUVERGNE CLERMONT 1,CYCLOPHARMA LAB,CHEZAL JEAN-MICHEL,DOLLE FREDERIC,MADELMONT JEAN-CLAUDE,MAISONIAL AURELIE,MIOT-NOIRAULT ELISABETH,MOINS NICOLE,PAPON JANINE,KUHNAST BERTAND,TAVITIAN BERTRAND,BOISGARD RAPHAEL
- 优先权： EP08101187 2008-01-31
- 主分类号： C07D401/12
- IPC分类号： C07D401/12 ; A61K31/47 ; A61K31/498 ; A61P35/00 ; C07D215/48 ; C07D215/50 ; C07D215/54 ; C07D241/44
摘要：
The present invention relates to the compound of formula (I): in which R1 represents a hydrogen atom, an optionally labelled halogen, a radionuclide or a Sn[(C1 -C4 )alkyl]3 group, Ar represents an aryl group or a heteroaryl group, R9 represents a hydrogen atom, a (C1 -C4 )alkyl group or forms together with the group R1 -Ar a ring fused with the Ar group, A represents a group of formula (ß) or (d): R3 and R4 independently represent a hydrogen atom, a (C1 -C6 )alkyl group, a (C1 -C6 )alkenyl group or a group of formula (y): wherein R11 represents an optionally labelled halogen, a radionuclide, an aryl or heteroaryl group optionally substituted by an optionally labelled halogen, a radionuclide, a -NO2 group, a -NR5 R6 group, a N+R5R6R7X- group, or a -OSO2R12 group, and their addition salts with pharmaceutically acceptable acids. The present invention also relates to pharmaceutical compositions comprising themand to their use in diagnosis, in particular with SPECTor PET imaging and in therapyofmelanoma, viatargeted radionuclide therapy.
摘要（中）：
本发明涉及式（I）化合物：其中R 1表示氢原子，任选标记的卤素，放射性核素或Sn [（C 1 -C 4）烷基] 3基团，Ar表示芳基或杂芳基 基团，R 9表示氢原子，（C 1 -C 4）烷基或与Ar基团稠合的基团R 1 -Ar a，A表示式（ß）或（d）的基团：R 3和R 4 独立地表示氢原子，（C1-C6）烷基，（C1-C6）烯基或式（y）的基团：其中R11表示任选标记的卤素，放射性核素，芳基或杂芳基任选取代 通过任选标记的卤素，放射性核素，-NO 2基团，-NR 5 R 6基团，N + R 5 R 6 R 7 X基或-OSO 2 R 12基团，以及它们与药学上可接受的酸的加成盐。 本发明还涉及包含它们的药物组合物，并且用于诊断，特别是用于SPECTOR PET成像和黑素瘤治疗靶向放射性核素治疗。
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07D | 杂环化合物 |
| ------C07D401/00 | 杂环化合物，含有两个或更多个杂环，以氮原子作为仅有的杂环原子，至少有1个环是仅含有1个氮原子的六元环 |
| --------C07D401/02 | .含有两个杂环 |
| ----------C07D401/12 | ..被含有杂原子的链作为键链连接的 |