阅读说明：本技术 化合物a与化合物b联合在制备治疗痛风或高尿酸血症的药物中的用途 (Application of combination of compound A and compound B in preparation of medicine for treating gout or hyperuricemia ) 是由 陈建文 沈扬 宁睿 于 2019-11-01 设计创作，主要内容包括：本公开涉及化合物A与化合物B联合在制备治疗痛风或高尿酸血症的药物中的用途。具体而言,化合物A选自式(I)化合物、或其可药用盐、或其酯,化合物B选自别嘌呤醇、非布司他。尤其是式(I-1)化合物联合非布司他治疗痛风或高尿酸血症的方法,显示了良好的治疗效果。(The disclosure relates to the use of compound a in combination with compound B in the preparation of a medicament for the treatment of gout or hyperuricemia. Specifically, the compound A is selected from a compound shown in a formula (I), or a pharmaceutically acceptable salt or an ester thereof, and the compound B is selected from allopurinol and febuxostat. In particular, the compound shown in the formula (I-1) and the febuxostat show good treatment effect.)

Use of compound A selected from compounds of formula (I), or pharmaceutically acceptable salts, or esters thereof, preferably of formula (I-1), in combination with compound B selected from allopurinol, febuxostat,

the use according to claim 1, wherein compound a and compound B have a synergistic uric acid lowering effect.

Use according to claim 1, wherein the weight ratio of compound a to non-bustazide is selected from 0.01-100:1, preferably from 1:20, 1:19, 1:18, 1:17, 1:16, 1:15, 1:14, 1:13, 1:12, 1:11, 1:10, 1:9, 1:8, 2:15, 1:7, 1:6, 1:5, 5:24, 2:9, 1:4, 4:15, 5:18, 2:7, 3:10, 5:16, 1:3, 5:14, 3:8, 2:5, 5:12, 3:7, 4:9, 1:2, more preferably from 1:16, 1:8, 1:4, 1: 2.

Use according to claim 1, wherein the weight ratio of compound a to allopurinol is selected from 0.01 to 100:2, preferably from 0.01 to 1:2, more preferably from 1:180, 1:170, 1:160, 1:150, 1:140, 1:130, 1:120, 1:110, 1:100, 1:90, 1:80, 1:70, 1:60, 1:50, 1:40, 1:30, 1:20, 1:10, 1: 5.

The use according to claim 1, wherein the amount of compound a is selected from 1-100mg, preferably 1-50mg, more preferably 1-20mg, most preferably about 5mg, about 6mg, about 7mg, about 8mg, about 9mg, about 10mg, about 11mg, about 12mg, about 13mg, about 14mg, about 15mg, about 16mg, about 17mg, about 18mg, about 19mg or about 20 mg.

The use according to claim 1, wherein the febuxostat is used in an amount selected from the group consisting of 1-200mg, preferably 10-120mg, more preferably about 10mg, about 20mg, about 30mg, about 40mg, about 50mg, about 60mg, about 70mg, about 80mg, about 90mg, about 100mg, about 110mg, about 120 mg.

The use according to claim 1, wherein the amount of allopurinol is selected from the group consisting of 50-900mg, preferably 100-600mg, more preferably 100mg, 150mg, 200mg, 250mg, 300mg, 350mg, 400mg, 450mg, 500mg, 550mg, 600 mg.

Use according to claim 1, wherein both compound a and compound B are administered orally, preferably both compound a and compound B are administered in the form of tablets.

Use of a compound of formula (I-1) in combination with febuxostat for the preparation of a medicament for the treatment of hyperuricemia or gout.

The use according to claim 9, wherein the amount of the compound of formula (I-1) is selected from 5mg/qd, 10mg/qd and the amount of febuxostat is selected from 20mg/qd, 40mg/qd, 80 mg/qd.

The use according to claim 9, wherein the amount of the compound of formula (I-1) is selected from 5mg/qd, 10mg/qd, the amount of febuxostat is selected from 20mg/qd, 40mg/qd, 80mg/qd, and both the compound of formula (I-1) and febuxostat are administered once daily, in the form of a tablet.

A pharmaceutical composition comprising

Compound a selected from a compound of formula (I), or a pharmaceutically acceptable salt, or ester thereof;

a compound B selected from febuxostat and allopurinol;

at least one pharmaceutically acceptable carrier;

wherein the compound A is preferably a compound of formula (I-1), and the compound B is preferably febuxostat.

The pharmaceutical composition of claim 12, wherein the compound of formula (I-1) is contained in an amount of 5mg or 10mg, the febuxostat is contained in an amount selected from the group consisting of 20mg, 40mg and 80mg, and the allopurinol is contained in an amount selected from the group consisting of 100mg and 600 mg.