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US 2026/0265270 A1Published application
Epoxy compound and use thereof
AssigneeShanghai Huilun Pharmaceutical Co., Ltd.
InventorsShuangqi Tang, Xinfeng Wang, Shengcai Huang, Qibin Huang, Guoqi Huang, Shuqi Du, Yeying Chen, Lei Chen, Jihong Qin
Life of this patent
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Abstract
An epoxy compound and a use thereof. Specifically disclosed are an epoxy compound as shown in formula I, a pharmaceutically acceptable salt or stereoisomer and use thereof. The compound has high inhibitory activity on β5i and β1i, but has a low inhibition level on β5c and β1c. The compound has relatively high selectivity and can be used for treating autoimmune diseases.
Claims16
An epoxy compound of Formula I, or a pharmaceutically acceptable salt or a stereoisomer thereof,
- wherein in Formula I,
- RA is C1-6 alkyl, cyclopentenyl, cyclohexenyl, cyclohexyl, cyclopentyl, or C6-14 aryl, in which the cyclopentenyl, cyclohexenyl, cyclohexyl, cyclopentyl and C6-14 aryl are optionally substituted with one or more RA1;
- RA1 is independently C1-6 alkyl, C1-6 alkoxy, halogen, hydroxyl, or C1-6 haloalkyl;
- RB is C1-6 alkyl or C1-6 haloalkyl;
- Rc is
- C1-6 alkyl, or C1-6 alkyl substituted with one or more Rc3;
- ring A is phenyl, 4- to 7-membered heterocycloalkyl, 8- to 10-membered heterocycloalkyl, 5- to 8-membered heteroaryl, C4-7 cycloalkyl, pyridinonyl or C4-7 cycloalkenyl;
- Rc1 is C1-6 alkylene optionally substituted with one or more RC1-1;
- RC1-1 is hydroxyl, C1-6 alkoxy, or halogen;
- Rc2 is C1-6 alkyl, C1-6 alkoxy, halogen, hydroxyl, C3-6 cycloalkoxy, NH(C1-6 alkyl), or N(C1-6 alkyl)2;
- or two adjacent Rc2 form, together with the atoms to which they are attached, a 4- to 6-membered ring;
- Rc3 is independently hydroxyl, halogen, C1-6 alkoxy, or C1-6 alkoxy substituted with one or more Rc3-1;
- Rc3-1 is independently C1-6 haloalkyl or C3-8cycloalkyl;
- RD is
- L4a is a bond, C1-6 alkylene, C2-6 alkenylene, C3-8 cycloalkylene, or 3- to 8-membered heterocycloalkylene, in which the C1-6 alkylene, C2-6 alkenylene, C3-8 cycloalkylene, and 3- to 8-membered heterocycloalkylene are optionally substituted with one or more L4a-1;
- L4a-1 is hydroxyl, halogen, oxo (═O), C1-6 alkylsulfonamido, or C1-6 alkoxy;
- L3a, L2a, and L1a are each independently a bond, —O—, —NH—, —N(C1-6 alkyl)-, carbonyl (—C═O—), C1-6 alkylene, sulfonyl (—SO2—), —C(═O) NH—, —NHC(═O)—, or —NHC(═O) NH—;
- Rd1 is C6-14 aryl, C1-6 alkyl, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C3-6 cycloalkyloxy, 3- to 8-membered heterocycloalkyloxy, 5- to 8-membered heteroaryl, or C1-6 alkylsulfonyl, in which the C6-14 aryl, C1-6 alkyl, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C3-6cycloalkyloxy, 3- to 8-membered heterocycloalkyloxy, 5- to 8-membered heteroaryl, and C1-6 alkylsulfonyl are optionally substituted with one or more Rd1-1;
- Rd1-1 is hydroxyl, halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, oxo (═O), C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylsulfonyl, C3-6cycloalkylsulfonyl, 3- to 6-membered heterocycloalkyl, 3- to 6-membered heterocycloalkylmethylene, C3-6cycloalkyl, or C6-14 aryl-C1-6 alkylene-;
- n is 0, 1, 2 or 3;
- and
- in the 3- to 8-membered heterocycloalkylene, 3- to 10-membered heterocycloalkyl, 3- to 8-membered heterocycloalkyloxy, 4- to 7-membered heterocycloalkyl, 8- to 10-membered heterocycloalkyl, 3- to 6-membered heterocycloalkyl, 3- to 6-membered heterocycloalkylmethylene, and 5- to 8-membered heteroaryl, the number of the heteroatom or heteroatom group is independently 1, 2, 3, or 4, and the heteroatom or heteroatom group is independently one or more of N, O, S, and —SO2—.
19 more elements
Dependencies are inferred from the claim text.