| 摘要 |
<P>PROBLEM TO BE SOLVED: To provide small molecule, nonpeptide caspase inhibitors that are potent and stable, and penetrate membranes to provide effective inhibition of apoptosis in vivo. <P>SOLUTION: The present invention provides a compound of formula I (wherein R<SP POS="POST">1</SP>is R<SP POS="POST">6</SP>C(O)-, HC(O)-, R<SP POS="POST">6</SP>SO<SB POS="POST">2</SB>-, R<SP POS="POST">6</SP>OC(O)-, (R<SP POS="POST">6</SP>)<SB POS="POST">2</SB>NC(O)-, (R<SP POS="POST">6</SP>)(H)NC(O)-, R<SP POS="POST">6</SP>C(O)C(O)-, R<SP POS="POST">6</SP>-, (R<SP POS="POST">6</SP>)<SB POS="POST">2</SB>NC(O)C(O)-, R<SP POS="POST">6</SP>(H)NC(O)C(O)- or R<SP POS="POST">6</SP>C(O)C(O)-; R<SP POS="POST">2</SP>is hydrogen, -CF<SB POS="POST">3</SB>, halo, -OR<SP POS="POST">7</SP>, -NO<SB POS="POST">2</SB>, -OCF<SB POS="POST">3</SB>, -CN, or R<SP POS="POST">8</SP>; R<SP POS="POST">3</SP>is hydrogen or (C1-C4)-aliphatic-; R<SP POS="POST">4</SP>is -COOH or -COOR<SP POS="POST">8</SP>; and R<SP POS="POST">5</SP>is -CH<SB POS="POST">2</SB>F or -CH<SB POS="POST">2</SB>O-2,3,5,6-tetrafluorophenyl). <P>COPYRIGHT: (C)2012,JPO&INPIT |
