Benzodiazepine compound, preparation method therefor, and use thereof in medicine
AssigneeWest China Hospital, Sichuan University
InventorsBowen Ke, Jin Liu, Jun Yang
Life of this patent
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Abstract
A benzodiazepine compound represented by formula I, or a salt thereof has an intravenous sedative anesthesia effect. The recovery quality of the compound is significantly improved compared with remimazolam in rat and mouse caudal venous anesthesia models. During anesthetization, the compound has a rapid onset, a short duration, a quick recovery and a good tolerance, can be used for anesthesia induction, anesthesia maintenance and day surgery anesthesia.
Claims23
A compound of formula I, or a salt thereof, or a stereoisomer thereof, or a solvate thereof, or a cocrystallization thereof, or a composition thereof:
- wherein,
- R1 is selected from the group consisting of H, short-chain hydrocarbon group, C3-10 cycloalkyl, and 3-10 membered heterocyclic group, wherein said short-chain hydrocarbon group, cycloalkyl or heterocyclic group is substituted with 0-4 substituents selected from the group consisting of halogen, trifluoromethyl, cyano, nitro, short-chain alkyl or alkoxy, and said heterocycle comprises 1-3 heteroatoms selected from N, O, and S;
- R2 is selected from the group consisting of H, short-chain hydrocarbon group, C3-10 cycloalkyl and 3-10 membered heterocyclic group, wherein said short-chain hydrocarbon group, cycloalkyl or heterocyclic group is substituted with 0-4 substituents selected from the group consisting of halogen, trifluoromethyl, cyano, nitro, short-chain alkyl, and alkoxy, and said heterocycle comprises 1-3 heteroatoms selected from N, O, and S;
- or R1 and R2 are connected to form C3-10 cycloalkyl or 3-10 membered heterocyclic group, wherein said cycloalkyl or heterocyclic group is substituted with 0-4 substituents selected from the group consisting of halogen, trifluoromethyl, cyano, nitro, short-chain alkyl, and alkoxy, and said heterocycle comprises 1-3 heteroatoms selected from N, O, and S;
- M is absent or selected from the group consisting of O, S, NH, and C1-5 alkylene, wherein said alkylene is substituted with 0-4 substituents selected from the group consisting of halogen, trifluoromethyl, and C1-6 alkoxy;
- R3 is selected from the group consisting of H, short-chain hydrocarbon group, and —(CH2)a—(O)b—R5, wherein R5 is C3-10 cycloalkyl or 3-10 membered heterocyclic group, said hydrocarbon group, cycloalkyl or heterocyclic group is substituted with 0-4 substituents selected from the group consisting of halogen, trifluoromethyl, amino, C1-4 alkyl, C1-4 alkoxy, C2-6 alkenyl, C2-6 alkynyl, and —NHC1-4 alkyl, and said heterocyclic ring comprises 1-3 heteroatoms selected from N, O, and S;
- a is selected from 0, 1 and 2;
- b is 0 or 1;
- R4 is a pyridine ring with nitrogen at position 2, 3 or 4;
- each of X is independently selected from the group consisting of halogen, substituted or unsubstituted C1-8 alkyl, and substituted or unsubstituted C1-8 alkoxy;
- the substituent of said alkyl or alkoxy is halogen;
- n is selected from 1, 2, 3 and 4;
- and
- HA is a pharmaceutically acceptable organic acid or inorganic acid.
A compound, or a salt thereof, or a stereoisomer thereof, or a solvate thereof, or a cocrystallization thereof, or a composition thereof, wherein said compound is selected from the following compounds:
Dependencies are inferred from the claim text.