首页> 外国专利> CRYSTALLINE FORM OF (R)-4-(5-(CYCLOPROPYLETHYNYL)ISOXAZOL-3-YL)-N-HYDROXY-2-METHYL-2-(METHYLSULFONYL)BUTANAMIDE AS AN ANTIBACTERIAL AGENT

CRYSTALLINE FORM OF (R)-4-(5-(CYCLOPROPYLETHYNYL)ISOXAZOL-3-YL)-N-HYDROXY-2-METHYL-2-(METHYLSULFONYL)BUTANAMIDE AS AN ANTIBACTERIAL AGENT

机译:作为抗菌剂的(R)-4-(5-(环丙基乙炔基)异恶唑-3-基)-N-羟基-2-甲基-2-(甲基磺酰基)丁二酸的结晶形式

摘要

The invention relates to a crystalline form of the (R)-4-(5- (cyclopropylethynyl)isoxazol-3-yl)-N-hydroxy-2-methyl-2- (methylsulfonyl)butanamide (i.e. the compound of formula (A)) with low hydroscopicity. The compound and compositions thereof are useful to treat bacterial infections and in particular Gram negative bacterial infections, including mult-drug resistant strains. The crystalline form is prepared by dissolving an amorphous form of the compound in a halogenated organic solvent (e.g. dichloromethane) and precipitating the crystalline form with a hydrocarbon solvent (e.g. heptane).(A)
机译:本发明涉及(R)-4-(5-(环丙基乙炔基)异恶唑-3-基)-N-羟基-2-甲基-2-(甲基磺酰基)丁酰胺的结晶形式(即式(A)化合物))低吸湿性。该化合物及其组合物可用于治疗细菌感染,尤其是革兰氏阴性细菌感染,包括多重耐药菌株。通过将化合物的无定形形式溶解在卤化有机溶剂(例如二氯甲烷)中,然后用烃类溶剂(例如庚烷)沉淀该晶体形式来制备晶体形式。

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