Taiwanj Pharmaceuticals Co., Ltd.

Sheng Hung Liu

Yan-Feng Jiang

Syaulan S Yang

Chia-Hao Chang

Kuang Yuan Lee

Ting-ni Huang

Chiung Wen Wang

Meng Hsien Liu

Yu-Shiou Fan

Hao Shiuan Liu

Meng-hsien Liu

Ying-chu Shih

Chi-Han Chen

The compounds represented by Formula (I), which are peripheral alkyl and alkenyl chains extended benzene derivatives, are useful as dual autotaxin (ATX)/histone deacetylase (HD AC) inhibitors. These compounds may be included in a pharmaceutical composition along with a pharmaceutically acceptable carrier, and be used in a therapeutically effective amount for prophylaxis or treatment of various diseases and disorders.

Peripheral alkyl and alkenyl chains extended benzene derivatives and pharmaceutical composition including the same

The present disclosure provides a benzene fused heterocyclic derivative of Formula (I):is a single or double bond; n is an integer of 0 or 1; A is &#x2014;CH&#x2014;, &#x2014;CH(OH)&#x2014;, or &#x2014;C(O)&#x2014;; G is C or N; X is &#x2014;CH&#x2014;, O, or &#x2014;C(O)&#x2014;; Y is alkyl, aryl, or heterocyclic alkyl optionally substituted with at least one substituent independently selected from a group consisting of: H, halogen, alkyl, alkyl substituted with at least one halogen, aryl, aryl substituted with at least one halogen, &#x2014;NRR, &#x2014;OR, &#x2014;RC(O)R, &#x2014;C(O)R, &#x2014;C(O)OR, &#x2014;C(O)ORRy3, &#x2014;NRC(O)R, &#x2014;NRC(O)NRR, &#x2014;NRC(O)ORR, &#x2014;NRC(O)ROR, C(O)NR(RR), &#x2014;C(O)NR(ROR), &#x2014;ORR, and &#x2014;OROR, wherein each of Rand Ris independently selected from a group consisting of H, oxygen, alkyl, and aryl, and Ris aryl optionally substituted with at least one halogen; Z is &#x2014;NRR, &#x2014;NRR, &#x2014;OR, &#x2014;ORR, &#x2014;C(O)RR, &#x2014;C(O)ORR, &#x2014;NRC(O)RR, &#x2014;NRC(O)ORR, &#x2014;C(O)NRR, or OROR, wherein each of Rand Ris independently selected from a group consisting of H, oxygen, alkyl and aryl, and Ris aryl optionally substituted with at least one substituent independently selected from a group consisting of halogen, OH, &#x2014;RCOOR, &#x2014;ORCOOR, &#x2014;RSOR, &#x2014;RSONRRR, &#x2014;RC(O)RR, &#x2014;RC(O)NRRR, &#x2014;RZC(O)NRSOR, wherein Rza is nil or alkyl, Ris H or alkyl, each of Rand Ris independently selected from a group consisting of H, OH, alkyl, aryl, alkoxyl, or NRRis a nitrogen-containing heterocyclic alkyl ring, Ris nil or a sulfonyl alkyl group. 

Benzene fused heterocyclic derivative and pharmaceutical composition comprising the same

Growing community of inventors

Zhubei, Taiwan

Sheng Hung Liu