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US 8,044,080 B2Granted
Isoxazoline derivative and novel process for its preparation
AssigneeLG Life Sciences Ltd.
InventorsHyun Ik Shin, Hyeong Wook Choi, Tae Ho Heo, Kyu Woong Lee, Jae Hoon Lee, Ki Sook Park
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Abstract
The present invention relates to an isoxazoline derivative having the cyclic carboxylic acid hemiketal moiety of formula (1) for use as caspase inhibitor, a process for preparing it, and a pharmaceutical composition comprising it.
Claims19
A compound of formula (1):
- wherein
- R1 is alkyl or aryl, selected from isoquinolinyl, quinolinyl or naphthyl and
- R2 is alkyl.
A process for preparing a compound of formula (1), comprising:
- (a) activating a compound of formula (2), then reacting it with a compound of formula (4) to produce a compound of formula (13);
- (b) hydrolyzing the compound of formula (13) to produce a compound of formula (14);
- (c) deprotecting the compound of formula (14);
- and
- (d) carrying out crystallization-induced dynamic transformation;
- wherein,
- R1 is alkyl or aryl,
- R2 is alkyl,
- R3 and R′3 are each alkyl, or
- R3 and R′3 together with oxygen atom to which they are attached form heterocycle, and
- R4 is alkyl.
8 more elements
A compound of the following structure:
Dependencies are inferred from the claim text.