发明申请
WO2013176698A1 CARBOLINE AND CARBAZOLE BASED IMAGING AGENTS FOR DETECTING NEUROLOGICAL DYSFUNCTION
审中-公开
基本信息:
- 专利标题： CARBOLINE AND CARBAZOLE BASED IMAGING AGENTS FOR DETECTING NEUROLOGICAL DYSFUNCTION
- 专利标题（中）：基于CARBOLINE和CARBAZOLE的成像剂用于检测神经性功能障碍
- 申请号：PCT/US2012/061912 申请日：2012-10-25
- 公开(公告)号：WO2013176698A1 公开(公告)日：2013-11-28
- 发明人： SZARDENINGS, Anna Katrin , KOLB, Hartmuth C. , WALSH, Joseph C. , CHEN, Gang , GANGADHARMATH, Umesh B. , KASI, Dhanalakshmi , LIU, Changhui , SINHA, Anjana , WANG, Eric , YU, Chul , ZHANG, Wei , CHEN, Kai , MOCHARLA, Vani P. , SCOTT, Peter J.H.
- 申请人： ELI LILLY AND COMPANY , SZARDENINGS, Anna Katrin , KOLB, Hartmuth C. , WALSH, Joseph C. , CHEN, Gang , GANGADHARMATH, Umesh B. , KASI, Dhanalakshmi , LIU, Changhui , SINHA, Anjana , WANG, Eric , YU, Chul , ZHANG, Wei , CHEN, Kai , MOCHARLA, Vani P. , SCOTT, Peter J.H.
- 申请人地址： Lilly Corporate Center Indianapolis, Indiana 46285 US
- 专利权人： ELI LILLY AND COMPANY,SZARDENINGS, Anna Katrin,KOLB, Hartmuth C.,WALSH, Joseph C.,CHEN, Gang,GANGADHARMATH, Umesh B.,KASI, Dhanalakshmi,LIU, Changhui,SINHA, Anjana,WANG, Eric,YU, Chul,ZHANG, Wei,CHEN, Kai,MOCHARLA, Vani P.,SCOTT, Peter J.H.
- 当前专利权人： ELI LILLY AND COMPANY,SZARDENINGS, Anna Katrin,KOLB, Hartmuth C.,WALSH, Joseph C.,CHEN, Gang,GANGADHARMATH, Umesh B.,KASI, Dhanalakshmi,LIU, Changhui,SINHA, Anjana,WANG, Eric,YU, Chul,ZHANG, Wei,CHEN, Kai,MOCHARLA, Vani P.,SCOTT, Peter J.H.
- 当前专利权人地址： Lilly Corporate Center Indianapolis, Indiana 46285 US
- 代理机构： DESAI, Manisha, A. et al.
- 优先权： US13/477,095 20120522
- 主分类号： C07D209/88
- IPC分类号： C07D209/88 ; C07D403/12 ; C07D471/04 ; C07D471/14 ; A61K51/04 ; A61K49/10 ; C07B59/00
摘要：
Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, allowing the com¬ pound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal mal is suffering from or is at risk of developing Alzheimer's Disease. The claimed compounds have the structure of formula (I) wherein: L is N or CR5, M is N or CR6; P is N or CR7; and Q is N or CR8; X is a bond or is Cl-14alkyl, wherein at least one carbon is optionally replaced by C(O), 0, S, S02, or NH, NH-Cl-8alkyl, and wherein at least one H of Cl-8alkyl is optionally replaced by halo, OH, Cl-6alkyl; wherein at least one halo is optionally replaced with a radionuclide or a fluorescent tag. The other variables are as defined in the claims.
摘要（中）：
本文公开了在哺乳动物中诊断阿尔茨海默氏病或其倾向的化合物和方法，所述方法包括向哺乳动物施用诊断有效量的放射性标记化合物，允许该组分分布于脑组织中，并使脑成像 组织，其中与正常对照水平的结合相比，化合物与脑组织的结合增加表明哺乳动物的马曾患有或有发展为阿尔茨海默病的风险。 所要求保护的化合物具有式（I）的结构，其中：L是N或CR 5，M是N或CR 6; P为N或CR7; Q为N或CR8; X是一个键或是C 1-4烷基，其中至少一个碳任选地被C（O），O，S，SO 2或NH，NH-C 1-8烷基取代，并且其中至少一个C 1-8烷基的H 任选被卤素，OH，C 1-6烷基取代; 其中至少一个卤素任选被放射性核素或荧光标记替代。 其他变量如权利要求中所定义。
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07D | 杂环化合物 |
| ------C07D209/00 | 杂环化合物，含五元环、与其他环稠合、带1个氮原子作为惟一的杂环原子 |
| --------C07D209/02 | .与一个碳环稠合 |
| ----------C07D209/58 | ..［b］-或［c］-稠合 |
| ------------C07D209/82 | ...咔唑；氢化咔唑 |
| --------------C07D209/88 | ....有杂原子或有以3个键连杂原子、其中最多以1个键连卤素的碳原子，例如，酯基或腈基，直接连在环系的碳原子上 |