发明名称 HEPATITIS B ANTIVIRAL AGENTS
摘要 The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:;X-A1-Y-A2-Z-L-R  (I);which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
申请公布号 US2017022150(A1) 申请公布日期 2017.01.26
申请号 US201615216124 申请日期 2016.07.21
申请人 Enanta Pharmaceuticals, Inc. 发明人 Qiu Yao-Ling;Li Wei;Cao Hui;Jin Meizhong;Kass Jorden;Gao Xuri;Peng Xiaowen;Or Yat Sun
分类号 C07C235/56;A61K45/06;A61K31/265;C07C233/66;A61K31/4164;A61K31/277;C07C271/12;A61K31/27;C07D233/64;A61K31/167;C07C255/60 主分类号 C07C235/56
代理机构 代理人
主权项 1. A compound represented by Formula (I): X-A1-Y-A2-Z-L-R  (I),or a pharmaceutically acceptable salt thereof, wherein: X is an optionally substituted aryl or optionally substituted heteroaryl; A1 is absent, or selected from the group consisting of —NH—, —NHC(O)—, —NHC(O)N(R3)—, and optionally substituted azolyl; Y is an optionally substituted aryl or optionally substituted heteroaryl; A2 is absent or —N(R4)—; Z is —CRaRb—; wherein Ra and Rb are each independently selected from the group consisting of hydrogen, OH, OMe, halogen, and methyl optionally substituted with 1 to 3 substituents selected from the group consisting of fluoro, chloro, OH, and OMe; wherein at least one of Ra and Rb is not hydrogen; alternatively, Ra, Rb, and the carbon atom to which they are attached form an oxetanyl, 5- to 6-membered cyclic ketal, or —C(═CF2)—; L is —NR1—, O or —CR1R2—; and R, R1, R2, R3 and R4 at each occurrence are independently selected from the group consisting of hydrogen, optionally substituted —C1-C8 alkyl, optionally substituted —C2-C8 alkenyl, optionally substituted —C2-C8 alkynyl, optionally substituted —C3-C8 cycloalkyl, optionally substituted 3- to 8-membered heterocyclic, optionally substituted aryl and optionally substituted heteroaryl; alternatively, R1 and R2 or R1 and R are taken together with the atom to which they are attached to form an optionally substituted C3-C8 cycloalkyl or an optionally substituted 3- to 8-membered heterocyclic.
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