Taiwanj Pharmaceuticals Co., Ltd.

Yu-Shiou Fan

Syaulan S Yang

Kuang Yuan Lee

Yan-Feng Jiang

Meng Hsien Liu

Meng-Hsien Liu

Sheng Hung Liu

Mei-chi Hsu

Chiung Wen Wang

Chi-Han Chen

Yan-feng Jiang

The present disclosure relates to a compound of Formula I, or a geometric isomer, enantiomer, diastereomer, racemate, atropisomer, pharmaceutically acceptable salt, prodrug or solvate thereof. The present disclosure further relates to a composition comprising the compound of Formula (I). The compound and the composition described herein can be used to inhibit NADPH oxidase activity. 

NADPH oxidase inhibitors, pharmaceutical composition comprising the same, and application thereof

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

Taipei, Taiwan

Yu-Shiou Fan