Quinazoline derivatives substituted by aniline, preparation method and use thereof
AssigneeXuanzhu Pharma Co., Ltd.
InventorsYanyan DONG, Shih CHENGKON
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Abstract
The invention relates to quinazoline derivatives substituted by aniline which are represented by the below formula (I), pharmaceutical acceptable salts and stereoisomer thereof, wherein these groups of R1, R2, R3, R4, R5, R6, L and n have the meanings given in the specification. The invention also relates to preparation methods, pharmaceutical compositions, pharmaceutical preparation and the use for preparation of medicine of treating excessive hyperplasia and chronic obstructive pulmonary disease and uses for treating excessive hyperplasia and chronic obstructive pulmonary disease thereof.
Claims14
A compound represented by a general formula (I), a pharmaceutically acceptable salt thereof or a stereoisomer thereof:
- wherein
- R1 is selected from the group consisting of the following groups that are unsubstituted or substituted by 1-2 Q1 substituents:
- a 6-10-membered fused ring-C0-6alkyl group, a 7-10-membered spiro ring-C0-6alkyl group or a 7-10-membered bridged ring-C0-6alkyl group, wherein 1-3 carbon atoms of said fused ring, spiro ring or bridged ring can be replaced with 1-3 hetero atoms and/or groups that can be identical or different and are selected from the group consisting of O, S(O)m, N(H)m, NCH3 and C(O), provided that after the replacement, O and C(O) in the ring are not adjacent to each other,
- Q1 is selected from the group consisting of halogen, hydroxyl, amino, carboxyl, cyano, a C1-16alkyl group, a C1-6alkoxyl group, a C1-6alkylamino group, a di(C1-6alkyl)amino group, a C1-6alkylcarbonyloxy group, a C1-6alkylacylamino group, a C1-6alkylsulfonyl group, a C1-6alkylsulfinyl group, a C1-6alkylsulfonylamino group and a C3-8cycloalkyl group;
- R2 is selected from the group consisting of hydrogen, a C1-6alkyl group or a C1-6alkoxyl group that is unsubstituted or substituted by 1-2 Q2 substituents, a formyl group that is substituted by a Q2 substituent or N(H)m,
- Q2 is selected from the group consisting of halogen, hydroxyl, amino, carboxyl, cyano, a C1-16alkyl group, a C1-6alkoxyl group, a C1-6alkylamino group, a di(C1-6alkyl)amino group, a C1-6alkylcarbonyloxy group, a C1-6alkylacylamino group, a C1-6alkylsulfonyl group, a C1-6alkylsulfinyl group, a C1-6alkylsulfonylamino group, a C3-8cycloalkyl group, an unsaturated C5-7 cyclic hydrocarbyl and a saturated or unsaturated 3-8-membered heterocyclyl, wherein the C3-8cycloalkyl, the unsaturated C5-7 cyclic hydrocarbyl and the saturated or unsaturated 3-8-membered heterocyclyl can further substituted by 1-2 Q3 substituents,
- Q3 is selected from the group consisting of halogen, hydroxyl, amino, carboxyl, cyano, a C1-16alkyl group, a C1-6alkoxyl group, a C1-6alkylamino group, a di(C1-6alkyl)amino group, a C1-6alkylcarbonyloxy group, a C1-6alkylacylamino group, a C1-6alkylsulfonyl group, a C1-6alkylsulfinyl group, a C1-6alkylsulfonylamino group and a halogen-substituted C1-6alkoxy group;
- R3 is selected from the group consisting of hydrogen, halogen, hydroxyl, cyano, nitro, a C1-6alkyl group, a C1-6alkoxyl group, a C1-6alkyl group or a C1-6alkoxyl group that is substituted by halogen, a C1-6alkylcarbonyloxy group, a C1-6alkylacylamino group, a C1-6alkylsulfonyl group, a C1-6alkylsulfinyl group or a C1-6alkylsulfonylamino group;
- R4, R5 and R6 are each independently selected from the group consisting of hydrogen, halogen, a C1-6alkyl group, a C1-6alkoxyl group, a C1-6alkyl group or a C1-6alkoxyl group that is substituted by halogen, a C1-6alkylamino group or a di(C1-6alkyl)amino group;
- L is selected from the group consisting of a covalent bond, O, S(O)m, N(H)m, NCH3 or C(O);
- n is 1, 2 or 3;
- and
- m is 0, 1 or 2.
Dependencies are inferred from the claim text.