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.
Claims13
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 or 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 includes 1-3 heteroatoms selected from N, O or S, preferably R1 is a short-chain hydrocarbon group or hydrogen;
- R2 is selected from the group consisting of H, short-chain hydrocarbon group, C3-10 cycloalkyl or 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 includes 1-3 heteroatoms selected from N, O or S, preferably R2 is H or a short-chain hydrocarbon group;
- or R1 and R2 may be mutually joined 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 or alkoxy, and said heterocycle includes 1-3 heteroatoms selected from N, O or S;
- M is absent or selected from the group consisting of O, S, NH or C1-5 alkylene, wherein said alkylene is substituted with 0-4 substituents selected from the group consisting of halogen, trifluoromethyl and C1-6 alkoxy, and preferably M is O;
- R3 is selected from the group consisting of H, short-chain hydrocarbon group and —(CH2)a—(O)b—R5, wherein R5 can be C3-10 cycloalkyl and 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, or —NHC1-4 alkyl, and said heterocyclic ring includes 1-3 heteroatoms selected from N, O, or S. Preferably, R3 is a short-chain hydrocarbon group;
- a is selected from 0, 1 and 2;
- b is 0 or 1;
- R4 represents a pyridine ring with nitrogen at position 2, 3 or 4, and preferably R4 is a pyridine ring with nitrogen at position 2;
- each of X is independently selected from the group consisting of halogen, substituted or unsubstituted C1-8 alkyl, substituted or unsubstituted C1-8 alkoxy;
- the substituent of said alkyl or alkoxy is halogen;
- n is selected from 1, 2, 3 and 4;
- HA is various pharmaceutically acceptable inorganic and organic acids.
Dependencies are inferred from the claim text.