FIELD: medicine.
SUBSTANCE: invention relates to a compound having the formula (I), having properties of an inhibitor of β-lactamase, or its pharmaceutically acceptable salt, a pharmaceutical composition based on it, as well as a pharmaceutical composition containing a compound of the formula (I) and ceftazidime. In the general formula (I), R1 is 5-element heterocycle optionally substituted with one or two substitutes T1, where heterocycle is selected among
; R2 is -SO3H or -CF2COOH; T1, the same or different, are independently a fluorine atom; =O; C(O)Q1; -(CH2)m-S(O)2-NQ1Q2; -(CH2)m-C(=NOQ1)Q3; -(CH2)mOQ1; -(CH2)m-CN; -(CH2)m-C(O)OQ1; -(CH2)m-C(O)NQ1Q2; -(CH2)m-C(O)NQ1OQ2; -(CH2)m-NQ1C(O)Q2; -(CH2)m-NQ1C(O)NQ1Q2; -(CH2)m-NQ1Q2; -(CH2)m-NH-C(NHQ3)=NQ4; -(CH2)m-C(NHQ3)=NQ4; or T1, the same or different, are independently T2 unsubstituted or substituted with one or more substitutes, -(CH2)m-(5- or 6-element saturated, partially unsaturated, or aromatic heterocycle containing 2 heteroatoms selected from N, O, or S); (C1-C3)-alkyl; (C1-C3)-fluoroalkyl; T2, the same or different, are independently -OH; -NH2; Q1 and Q2, the same or different, are independently a hydrogen atom; -(CH2)r-NHQ3; -(CH2)r-NH-C(NHQ3)=NQ4; -(CH2)r-OQ3; -(CH2)n-CONHQ3; or T2 unsubstituted or substituted with one or more substitutes, (C1-C3)-alkyl; (C1-C3)-fluoroalkyl; saturated, partially unsaturated, or aromatic -(CH2)m-(4-, 5-, or 6-element heterocycle containing 1-3 heteroatoms selected from N, O, or S, where at least one heteroatom is a nitrogen atom); or Q1, Q2, and a nitrogen atom, to which they are attached, together form unsubstituted, saturated 5- or 6-element heterocycle containing 1 or 2 heteroatoms selected from N or O; Q3 and Q4, the same or different, are independently a hydrogen atom or (C1-C3)-alkyl; m, the same or different, are independently equal to 0,1,2; n, the same or different, are independently equal to 1 or 2; r is equal to 1, 2, or 3, when (CH2)r is directly bound to a carbon atom, or 2 in other cases.
EFFECT: provision of a compound of the formula (I), having properties of an inhibitor of β-lactamase.
(I)
18 cl, 6 tbl, 86 ex
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Authors
Dates
2022-11-09—Published
2017-09-29—Filed