Lg Life Sciences, Limited

Jong-Ryoo Choi

Chung-Mi Kim

Tae-Saeng Choi

Yong-Zu Kim

Hyun-Sook Jang

Seung-Joo Cho

Woo-Young Cho

Tae-Kyun Kim

Jae-Hong Lim

Chang-Ho Lee

Gyoung-Won Kim

Jeong-Min Kim

Dong-Gyu Cho

Jae-Taeg Hwang

Kee-Yoon Roh

The present invention relates to an acyclic nucleoside phosphonate derivative which is useful as an antiviral agent (particularly, against hepatitis B virus), pharmaceutically acceptable salts, stereoisomers, and a process for the preparation thereof.

Acyclic nucleoside phosphonate derivatives, salts thereof and process for the preparation of the same

The present invention relates to an acyclic nucleoside phosphonate derivative represented by the following formula (1): in whichrepresents single bond or double bond, R, R, R, Rand Rare defined herein, Y represents &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;CH(Z)-, &#x2550;C(Z)-, &#x2014;N(Z)-, &#x2550;N&#x2014;, or &#x2014;SiH(Z)-, wherein Z represents hydrogen, hydroxy or halogen, or represents C-C-alkyl, C-C-alkoxy, allyl, hydroxy-C-C-alkyl, C-C-aminoalkyl or phenyl, Q represents a group having the following formula: wherein X, and Xindependently of one another represent hydrogen, amino, hydroxy or halogen, or represent C-C-alkyl, C-C-alkoxy, allyl, hydroxy-C-C-alkyl, phenyl or phenoxy each of which is optionally substituted by nitro or C-C-alkoxy, or represent C-C-arylthio which is optionally substituted by nitro, amino, C-C-alkyl or C-C-alkoxy, or represent C-C-arylamino, C-C-alkylamino, di(C-C-alkyl)amino, C-C-cycloalkylamino or a structure of wherein n denotes an integer of 1 or 2 and Yrepresents O, CHor N&#x2014;R (R represents C-C-alkyl or C-C-aryl), which is useful as an antiviral agent (particularly, against hepatitis B virus), pharmaceutically acceptable salts, stereoisomers, and a process for the preparation thereof.

The present invention relates to a nucleoside phosphonate derivative represented by formula (1): pharmaceutically acceptable salts, and stereoisomers. This nucleoside phosphonate derivative is useful as an antiviral agent, particularly, against hepatitis B virus. Also disclosed are processes for the preparation of the nucleoside phosphonate derivative. Also disclosed are methods treating hepatitis B by administering a nucleoside phosphonate derivative of formula (1).

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Taejeon, South Korea

Jong-Ryoo Choi