公开(公告)号：US20090087376A1

公开(公告)日：2009-04-02

申请号：US11632328

申请日：2005-07-15

申请人： Brian Bacskai ,  Bradley T. Hyman ,  William E. Klunk ,  Chester A. Mathis ,  Timothy Swager ,  Evgueni Nesterov ,  Ivory Hills

发明人： Brian Bacskai ,  Bradley T. Hyman ,  William E. Klunk ,  Chester A. Mathis ,  Timothy Swager ,  Evgueni Nesterov ,  Ivory Hills

IPC分类号： A61K51/04 ,  C07D249/04 ,  C07D403/02 ,  C07D277/62 ,  C07D263/54 ,  C07D209/04 ,  A61P25/00 ,  C07D409/02 ,  C07D333/50 ,  A61K49/00 ,  A61K49/06

CPC分类号： C07D333/54 ,  C07D333/18 ,  C07D409/04 ,  C07D409/14 ,  C07D417/14

摘要： The present invention relates to the identification of compounds that are suitable for imaging amyloid deposits in living patients. The invention relates, in part, to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease. The present invention also relates to therapeutic uses for such compounds, as exemplified by compounds of the formula (1) in which Y is independently S, O, or N and m is 1, 2, or 3.

摘要翻译： 本发明涉及适合于在活体患者中淀粉样沉积成像的化合物的鉴定。 本发明部分地涉及在体内成像淀粉样蛋白沉积物的方法，以允许阿尔茨海默氏病的止血诊断。 本发明还涉及这样的化合物的治疗用途，例如式（1）化合物，其中Y独立地为S，O或N，m为1,2或3。

公开(公告)号：US20130053572A1

公开(公告)日：2013-02-28

申请号：US13574315

申请日：2011-01-19

申请人： Steven L. Colletti ,  Zhengwu James Deng ,  Matthew G. Stanton ,  Weimin Wang ,  Ivory Hills

发明人： Steven L. Colletti ,  Zhengwu James Deng ,  Matthew G. Stanton ,  Weimin Wang ,  Ivory Hills

IPC分类号： C07C217/40 ,  C07D211/44 ,  C07D211/32 ,  C07C217/52 ,  C07D211/46 ,  C07D207/08 ,  C07D207/12

CPC分类号： C12N15/113 ,  C07C217/40 ,  C07C217/52 ,  C07C2601/02 ,  C07D207/08 ,  C07D207/12 ,  C07D209/48 ,  C07D211/22 ,  C07D211/44 ,  C07D211/46 ,  C07D295/088 ,  C07H21/02 ,  C12N15/1137 ,  C12N2310/14 ,  C12N2310/141 ,  C12N2310/321 ,  C12N2330/30

摘要： The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that is susceptible to hydrolytic instability that may translate into reduced liver residence times and reduced hepatocellular toxicity. The present invention employs acetals and ketals to provide a low pH sensitive chemical handle for degradation.

摘要翻译： 本发明提供了可以与其它脂质组分如胆固醇和PEG-脂质组合使用以与寡核苷酸形成脂质纳米颗粒的新型阳离子脂质。 本发明的目的是提供一种易于水解不稳定性的阳离子脂质支架，其可能转化为减少的肝停留时间和降低的肝细胞毒性。 本发明使用缩醛和缩酮来提供用于降解的低pH敏感化学手柄。

公开(公告)号：US09670487B2

公开(公告)日：2017-06-06

申请号：US13574315

申请日：2011-01-19

申请人： Steven L. Colletti ,  Zhengwu James Deng ,  Matthew G. Stanton ,  Weimin Wang ,  Ivory Hills

发明人： Steven L. Colletti ,  Zhengwu James Deng ,  Matthew G. Stanton ,  Weimin Wang ,  Ivory Hills

IPC分类号： C07C217/40 ,  C12N15/113 ,  C07C217/52 ,  C07D207/08 ,  C07D207/12 ,  C07D209/48 ,  C07D211/22 ,  C07D211/44 ,  C07D211/46 ,  C07D295/088 ,  C07H21/02

CPC分类号： C12N15/113 ,  C07C217/40 ,  C07C217/52 ,  C07C2601/02 ,  C07D207/08 ,  C07D207/12 ,  C07D209/48 ,  C07D211/22 ,  C07D211/44 ,  C07D211/46 ,  C07D295/088 ,  C07H21/02 ,  C12N15/1137 ,  C12N2310/14 ,  C12N2310/141 ,  C12N2310/321 ,  C12N2330/30

摘要： The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that is susceptible to hydrolytic instability that may translate into reduced liver residence times and reduced hepatocellular toxicity. The present invention employs acetals and ketals to provide a low pH sensitive chemical handle for degradation.