Salt containing piperazine polycyclic derivative, crystal form thereof, preparation method therefor, and use thereof
AssigneesShanghai Hansoh Biomedical Co., Ltd., Jiangsu Hansoh Pharmaceutical Group Co., Ltd.
InventorsJinyao Chen, Yuanyuan Li
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Abstract
Provided are a salt containing a piperazine polycyclic derivative, a crystal form thereof, a preparation method therefor, and the use thereof. In particular, the present invention relates to a salt containing a compound of general formula (I) and a stereoisomer thereof, a crystal form of the salt, a preparation method, a pharmaceutical composition containing a therapeutically effective amount of the crystal form, and the use as a G protein-coupled receptor regulator in treatment or prevention of central nervous system diseases and/or mental diseases.
Claims20
An acid salt of a compound of formula (III) or a stereoisomer thereof,
- wherein:
- R5 is selected from the group consisting of hydrogen, amino, C1-3 alkyl, C1-3 alkoxy, C1-3 hydroxyalkyl, C3-8 cycloalkyl, phenyl, oxiranyl, thiiranyl, aziridinyl, oxetanyl, azetidinyl, thietanyl, tetrahydrofuryl, tetrahydrothienyl, furyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, 1,3,5-triazinyl, benzofuryl, benzothienyl, indolyl, benzimidazolyl, indazolyl, benzoxazolyl, benzotriazolyl, quinolinyl and isoquinolyl, the amino, C1-3 alkyl, C1-3 alkoxy, C1-3 hydroxyalkyl, C3-8 cycloalkyl, phenyl, oxiranyl, thiiranyl, aziridinyl, oxetanyl, azetidinyl, thietanyl, tetrahydrofuryl, tetrahydrothienyl, furyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, 1,3,5-triazinyl, benzofuryl, benzothienyl, indolyl, benzimidazolyl, indazolyl, benzoxazolyl, benzotriazolyl, quinolinyl and isoquinolyl are each optionally further substituted by one or more substituents selected from the group consisting of deuterium, halogen, hydroxy, cyano, oxo, C1-3 alkyl, C1-3 alkoxy and C1-3 hydroxyalkyl;
- the acid in the acid salt is an inorganic acid or an organic acid;
- wherein, the inorganic acid is selected from the group consisting of hydrochloric acid, sulfuric acid, nitric acid, hydrobromic acid, hydrofluoric acid, hydroiodic acid and phosphoric acid;
- the organic acid is selected from the group consisting of 2,5-dihydroxybenzoic acid, 1-hydroxy-2-naphthoic acid, acetic acid, dichloroacetic acid, trichloroacetic acid, acetohydroxamic acid, adipic acid, benzenesulfonic acid, 4-chlorobenzenesulfonic acid, benzoic acid, 4-acetamidobenzoic acid, 4-aminobenzoic acid, decanoic acid, caproic acid, caprylic acid, cinnamic acid, citric acid, cyclamic acid, camphorsulfonic acid, aspartic acid, camphoric acid, gluconic acid, glucuronic acid, glutamic acid, isoascorbic acid, lactic acid, malic acid, mandelic acid, pyroglutamic acid, tartaric acid, dodecyl sulfuric acid, dibenzoyl tartaric acid, ethane-1,2-disulfonic acid, ethanesulfonic acid, formic acid, fumaric acid, galactonic acid, gentisic acid, glutaric acid, 2-ketoglutaric acid, glycolic acid, hippuric acid, isethionic acid, lactobionic acid, ascorbic acid, aspartic acid, lauric acid, camphoric acid, maleic acid, malonic acid, methanesulfonic acid, 1,5-naphthalenedisulfonic acid, naphthalene-2-sulfonic acid, nicotinic acid, oleic acid, orotic acid, oxalic acid, palmitic acid, embonic acid, propionic acid, salicylic acid, 4-aminosalicylic acid, decanedioic acid, stearic acid, succinic acid, thiocyanic acid, pamoic acid, methanoic acid, undecylenic acid, trifluoroacetic acid, benzenesulfonic acid, p-toluenesulfonic acid and L-malic acid;
- and
- V is 0 or 1.
Dependencies are inferred from the claim text.