Substituted pyrazole compound, preparation method therefor, pharmaceutical composition and medical use thereof
AssigneeJiangsu Vanguard Pharmaceutical Co., Ltd.
InventorsQingzhi Gao, Junhua Yao
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Abstract
The invention discloses a substituted pyrazole compound of formula (I), preparation method therefor, a pharmaceutical composition and a medical use thereof. The said compound features excellent stability, solubility, and low cytotoxicity, which is significantly beneficial for neurological protection, effectively preventing and treating nerve cell injuries. It is an ideal pharmaceutical compound for preventing or treating stroke, cerebral embolism, stroke sequelae, stroke-related motor dysfunction, mitochondrial encephalomyopathy, and amyotrophic lateral sclerosis.
Claims9
A substituted pyrazole compound of formula (I), or a pharmaceutically acceptable salt thereof, or a solvate thereof,
- wherein:
- R1 is H or methyl;
- X is —O— or —NH—;
- is a double bond and A is O;
- R2 is C1-C17 branched or linear alkyl, C3-6 cycloalkyl, phenyl-C1-C6 alkyl, pyridyl, phenyl optionally substituted by one or more than one group selected from hydroxyl, C1-6 alkanoyloxy, C1-6 alkoxy acyloxy or —NR′R″, wherein R′ and R″ are each independently C1-C6 linear or branched alkyl;
- or, is a single bond, the following formula (i) in formula (I)
- forms the group of the formula (ii)
- wherein n is 1 or 2, and m is 1, 2, 3 or 4;
- R3 is independently hydroxy, hydroxymethyl, or unsubstituted or mono-substituted amino with C1-6 alkanoyl;
- wherein the alkyl moiety of the “branched or linear alkyl”, “alkoxy”, “arylalkoxy”, and “alkanoyloxy” is each independently a C1-20 linear or branched alkyl;
- a C1-17 linear or branched alkyl;
- a C1-8 linear or branched alkyl;
- a C1-6 linear or branched alkyl;
- a C1-4 linear or branched alkyl;
- methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, tert-butyl, sec-butyl, n-pentyl, isopentyl, neopentyl, tert-pentyl, n-hexyl, isohexyl, heptyl, n-octyl, n-nonyl, n-decyl, dodecyl, pentadecyl or hexadecyl;
- wherein the “cycloalkyl” is a C3-8 cycloalkyl, a cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl.
A substituted pyrazole compound of formula (I), or a pharmaceutically acceptable salt thereof, or a solvate thereof,
- wherein
- the following formula (i) in formula (I)
- forms the group of the following formula (iii) or (iv),
- wherein, R′1 is hydrogen, hydroxymethyl or C1-4 here;
- R′2 is hydroxy or C1-4 alkanoyloxy;
- R′3 is hydrogen, hydroxy, C1-4 alkanoyloxy, amino, or C1-4 alkanoylamino.
Dependencies are inferred from the claim text.