| 发明名称 |
Substituted phthalazines for inducing insulin secretion and protecting beta-cells |
| 摘要 |
Phthalazine analogs of a Lisofylline (LSF) and synthetic methods for preparation of such analogs are provided. Compounds of the invention have structural formula III:;
wherein 1) R3a is hydrogen and R3b is selected from C5-22alkyl, C2-22alkenyl, or C2-22alkynyl; or a pharmaceutically acceptable salt thereof; or 2) R3b is hydrogen and R3a is selected from C9alkyl, C15-22alkyl, C9-22alkenyl, or C2-22alkynyl; or a pharmaceutically acceptable salt thereof; or 3) R3a and R3b are the same or different and are selected from C9alkyl, C15-22alkyl, C4-22alkenyl, or C2-22alkynyl; or a pharmaceutically acceptable salt thereof. The analogs of LSF provided have the ability to protect cell viability, particularly the ability to protect pancreatic β-cells, to induce insulin secretion. |
| 申请公布号 |
US9278098(B2) |
申请公布日期 |
2016.03.08 |
| 申请号 |
US201414524724 |
申请日期 |
2014.10.27 |
| 申请人 |
UNIVERSITY OF VIRGINIA PATENT FOUNDATION |
发明人 |
MacDonald Timothy L.;Nadler Jerry L.;Cui Peng |
| 分类号 |
C07D237/32;A61K31/502 |
主分类号 |
C07D237/32 |
| 代理机构 |
|
代理人 |
Sparks Rodney L. |
| 主权项 |
1. A method for protecting β-cells in a mammal against apoptosis comprising administering to said mammal an effective amount of a compound having formula III: wherein: (i) R3a is hydrogen and R3b is selected from C5-22alkyl, C2-22alkenyl, or C2-22alkynyl; or (ii) R3b is hydrogen and R3a is selected from C9alkyl, C15-22alkyl, C9-22alkenyl, or C2-22alkynyl; or (iii) R3a and R3b are the same or different and are selected from C9alkyl, C15-22alkyl, C4-22alkenyl, or C2-22alkynyl; or a pharmaceutically acceptable salt thereof. |
| 地址 |
Charlottesville VA US |
