09-04-2015 дата публикации
Номер: US20150099800A1
Принадлежит:
The invention provides for novel lipase inhibitors, and compositions and devices comprising the same. The invention further provides for methods for treatment of disorders comprising administration of novel diacylglycerol lipase inhibitors, and compositions and devices comprising said inhibitors. In some embodiments, the disorders are pancreatitis, obesity, shock or pancreatic necrosis. The invention further provides for novel ether lipid reporter compounds and methods of assaying enzymatic activity comprising contacting a compound with a novel ether lipid reporter compound. 2. The compound of claim 1 , wherein at least one of B or X is a solid support.3. The compound of claim 1 , wherein{'sub': 1', '6', '6', '12, 'R is (C-C)-alkyl or (C-C)-aryl;'}{'sub': 1', '3, 'A is a linking group comprising —V—, —V—O—, —V—S—, —V—N(H)—, or —V—N((C-C)-alkyl)-;'}{'sub': 1', '12', '2', '2', 'n', '1', '12', '2', '2', 'n, 'V is (C-C)-alkyl or —(OCHCH)—, wherein any carbon atom in said (C-C)-alkyl or —(OCHCH)— is optionally replaced with one or more heteroatom, cycloalkyl group, heterocycle, aryl or heteroaryl group;'}B is a solid support or H;X is a solid support or H, wherein at least one of B or X is a solid support;{'sub': 1', '3, 'Y is a linking group comprising -J-, —O-J-, —S-J-, —N(H)-J-, or —N((C-C)-alkyl)-J-;'}{'sub': 1', '12', '2', '2', 'n', '1', '12', '2', '2', 'n, 'J is (C-C)-alkyl or —(OCHCH)—, wherein any carbon atom in said (C-C)-alkyl or —(OCHCH)— is optionally replaced with one or more heteroatom, cycloalkyl group, heterocycle, aryl or heteroaryl group; and'}each n is independently 0-100.4. The compound of claim 1 , wherein{'sub': 1', '6', '6', '12, 'R is (C-C)-alkyl or (C-C)-aryl;'}{'sub': 1', '3, 'A is a linking group comprising —V—, —V—O—, —V—S—, —V—N(H)—, or —V—N((C-C)-alkyl)-;'}{'sub': 1', '12', '2', '2', 'n', '1', '12', '2', '2', 'n, 'V is (C-C)-alkyl or —(OCHCH)—, wherein any carbon atom in said (C-C)-alkyl or —(OCHCH)— is optionally replaced with one or more ...
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