NOVEL 4-METHYL-DIHYDROPYRIMIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION,申请号US201514839376-传众专利搜索

NOVEL 4-METHYL-DIHYDROPYRIMIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION

申请公布号：US2016052921(A1)

申请号：US201514839376

申请日期：2015.08.28

申请公布日期：2016.02.25

申请人：

HOFFMANN-LA ROCHE INC.

发明人：Guo Lei;Lin Xianfeng;Liu Haixia;Qiu Zongxing;Sheng Hong;Tang Guozhi;Wu Guolong;Zhang Weixing;Zhu Wei

分类号：C07D417/14;C07D413/14;C07D401/14;C07D417/04

主分类号：C07D417/14

地址：Little Falls NJ US

摘要：The invention provides novel compounds having the general formula:;;wherein R1, R2, R3, R4, R5, M and X are as described herein, compositions including the compounds and methods of using the compounds.

主权项：1. A compound of formula (I)wherein: R1 is C1-2 alkoxycarbonyl or cyano; R2 is phenyl, which is substituted by halogen; R3 is thiazolyl, thienyl, imidazolyl, isoxazolyl or pyridinyl; which is unsubstituted or substituted by halogen or C1-6alkyl; X is oxygen or —NR7; R4 and R5 are independently selected from hydrogen, C1-6alkyl and trifluoroC1-6alkyl; or R4 and R5, together with the carbon atom to which they are attached, form a 3 to 7 membered cycloalkyl; or when X is —NR7, one of R4 and R5 is hydrogen or C1-6alkyl, and the other of R4 and R5 along with R7 and the atoms to which R4 or R5 and R7 are attached form a pyrrolidinyl, morpholinyl or piperidinyl ring, which pyrrolidinyl, morpholinyl or piperidinyl ring is unsubstituted or substituted by fluoro; M is C1-6alkoxycarbonyl, carboxy, di-C1-6alkylaminoC2-6alkoxycarbonyl, aminocarbonyl, C1-6alkylaminocarbonyl, di-C1-6alkylaminocarbonyl, C1-6alkylsulfonylaminocarbonyl, 2-thiazolylaminocarbonyl, hydroxy-CyH2y—, R7 is C1-6alkyl or trifluoroC1-6alkyl; y is 1-6;or pharmaceutically acceptable salts, or tautomerism isomers thereof.