Six-membered ring benzo derivatives as DPP-4 inhibitor and use thereof
AssigneesEast China University of Science and Technology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
InventorsHonglin Li, Hualiang Jiang, Yufang Xu, Jia Li, Zhenjiang Zhao, Jingya Li, Hongling Xu, Shiliang Li
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Abstract
The present invention relates to six-membered ring benzo derivatives as a DPP-4 inhibitor and a use thereof. In particular, the present invention relates to a compound as shown in formula I, a pharmaceutical composition containing the compound as shown in formula I and a use of the compound in the preparation of drugs for treating DPP-4 related diseases or inhibiting DPP-4.
Claims17
A compound having formula I, or a pharmaceutically acceptable salt or prodrug thereof, or an optically active isomer or solvate thereof:
- wherein:
- X is O
- A is a benzene ring with 1 to 5 substituents, wherein each substituent is independently a halogen, a cyano, a hydroxy, a C1-6 alkyl, a C1-6 alkyl substituted by halogen, a C1-6 alkoxy, or a C1-6 alkoxy substituted by halogen;
- A is a nitrogen-containing, or sulfur-containing five-membered or six-membered saturated or unsaturated heterocycle with 1 to 4 substituents, wherein each substituent is independently a halogen, a cyano, or a boronic acid group;
- or
- A is a heterocycle selected from the following structures:
- R is H, a halogen, a cyano, a hydroxy, a C1-6 alkyl, C1-6 alkyl with 1 to 5 F atoms, C1-6 alkoxy, or C1-6 alkoxy with 1 to 5 F atoms;
- n is an integer of 1-2;
- Ring B is an aromatic benzene ring, an aromatic heterocycle, a saturated or unsaturated 5-membered or 6-membered ring, a nitrogen-, oxygen-, or sulfur-containing five- or six-membered saturated or unsaturated heterocycle;
- R1 is independently selected from the group consisting of a halogen, a cyano, a hydroxy, a C1-6 alkyl, a C1-6 alkyl group containing 1 to 5 F atoms, a C1-6 alkoxy, a C1-10 alkylcarbonyloxy, a C1-3 alkoxymethoxy, a disubstituted OCH2CH2O and OCH2O, COOH, a C1-6 alkoxycarbonyl, a carbamoyl, a methylcarbamido, a cyanomethylcarbonyl, an acetamidomethylcarbonyl, a 2-pyrrocarbonyl, a methoxycarbonylmethyl, a 4-pyranylcarbonyl, a 4-morpholinecarbonyl, a 1-piperazinecarbonyl, an amino, a NR2R3, a C1-5alkylcarboxamido, a C3-5 alkyllactam group, a C1-6 alkylsulfonamido, a C3-5 alkylsultam group, a mercapto, a C1-6 alkylthio, a C1-6 alkylthio containing 1 to 5 F atoms, a C1-6 alkylsulfinyl, a C1-6 alkylsulfonyl, a C3-5 cycloalkylsulfonyl, and a C1-5alkylsulfinyl, a N-propanesulfonyllactam group, a N-butanesulfonyllactam group, and a 3-pyrazolylamino;
- m is an integer of 1 to 4;
- and
- R2, R3 are independently selected from a C1-6 alkyl, or R2 and R3 together form a substituted or unsubstituted 5- or 6-membered heterocycloalkyl, or a substituted or unsubstituted 5-or 6-membered heterocycle group additionally containing N or O.
A compound selected from the following group, or a pharmaceutically acceptable salt or prodrug thereof:
A compound selected from the following group, or a pharmaceutically acceptable salt or prodrug thereof:
Dependencies are inferred from the claim text.