Benzoxazine oxazolidinone compounds, preparation methods and uses thereof
AssigneesShanghai Institute of Materia Medica, Chinese Academy of Sciences, Nanjing Changao Pharmaceutical Science & Technology Co., Limited
InventorsYushe Yang, Qisheng Xin, Houxing Fan, Bin Guo, Xin Liu, Huili He, Wei Li, Zhan Li
Life of this patent
Estimating the term…
Abstract
Novel benzoxazine oxazolidinone compounds, preparation methods and uses thereof are disclosed, which belong to the field of pharmacy. More specifically, novel benzoxazine oxazolidinone compounds represented by the following general formula (I), preparation methods and uses thereof in preparing medicament for treating infectious diseases, especially infectious diseases caused by multi-drug resistant bacteria, are disclosed.
Claims16
Benzoxazine oxazolidinone compounds represented by the formula (I), optical isomers or pharmaceutically acceptable salts thereof,
- Wherein:
- U is H or F;
- R1 is
- R2 is a phenyl group, or a five membered or six membered aromatic or non-aromatic heterocyclic group;
- said phenyl group is optionally substituted by F, —CN, —NH2, or C1-C3 alkylcarbonyl group;
- said five membered or six membered aromatic or non-aromatic heterocyclic group comprises at least one heteroatom selected from N, O or S;
- Said five membered or six membered aromatic or non-aromatic heterocyclic group may optionally be substituted by the following functional groups:
- F, Cl, Br, —OH, —NO2, —CHO, —CN, —NH2, —CF3, —C≡CH, —C≡CCH2OH, —COOH, —OR3, —NHCOR3, —COR3;
- —CONR3R4, and —COOR3, wherein each of R3 and R4 can independently be a C1-C3 alkyl;
- or said five membered or six membered aromatic or non-aromatic heterocyclic group may optionally be substituted by C1-C6 straight chain or branched chain alkyl group, or C3-C6 cycloalkyl group, and said C1-C6 straight chain or branched chain alkyl group or C3-C6 cycloalkyl group may optionally be substituted by —OH, —CN, or —NH2;
- or said five membered or six membered aromatic or non-aromatic heterocyclic group may optionally be substituted by five membered or six membered aromatic or non-aromatic heterocyclic group, which comprises at least one heteroatom selected from N and O and is either unsubstituted or substituted by C1-C3 alkyl or oxygen.
A method for treating an infectious disease caused by multi-drug resistant bacteria selected from the group consisting of Enterococcus, Staphylococcus aureus, Staphylococcus epidermidis, and pneumococcus, which comprises administering a therapeutically effective benzoxazine oxazolidinone compound represented by the formula (I), or an optical isomers or pharmaceutically acceptable salt thereof
- wherein:
- U is H or F;
- R1 is
- R2 is a phenyl group, or a five membered or six membered aromatic or non-aromatic heterocyclic group;
- said phenyl group is optionally substituted by F, —CN, —NH2 or C1-C3 alkylcarbonyl group;
- said five membered or six membered aromatic or non-aromatic heterocyclic group comprises at least one heteroatom selected from N, O or S;
- Said five membered or six membered aromatic or non-aromatic heterocyclic group may optionally be substituted by the following functional groups:
- F, Cl, Br, —OH, —NO2, —CHO, —CN, —NH2, —CF3, —C≡CH, —C≡CCH2OH, —COOH, —OR3, —NHCOR3, —COR3, —CONR3R4, and —COOR3, wherein each of R3 and R4 can independently be a C1-C3 alkyl;
- or said five membered or six membered aromatic or non-aromatic heterocyclic group may optionally be substituted by C1-C6 straight chain or branched chain alkyl group, or C3-C6 cycloalkyl group, and said C1-C6 straight chain or branched chain alkyl group or C3-C6 cycloalkyl group may optionally be substituted by —OH, —CN, or —NH2;
- or said five membered or six membered aromatic or non-aromatic heterocyclic group may optionally be substituted by five membered or six membered aromatic or non-aromatic heterocyclic group, which comprises at least one heteroatom selected from N and O and is either unsubstituted or substituted by C1-C3 alkyl or oxygen, to a living organism in need of said treatment.
Dependencies are inferred from the claim text.