-
1.
公开(公告)号:US20210276957A1
公开(公告)日:2021-09-09
申请号:US17254565
申请日:2019-06-20
发明人: Syaulan S. YANG , Kuang Yuan LEE , Meng Hsien LIU , Yan-Feng JIANG , Yu-Shiou FAN , Chiung Wen WANG , Mei-Chi HSU
IPC分类号: C07D223/16 , C07D215/26 , C07D401/10 , C07D409/04 , C07D491/056 , C07D495/04
摘要: 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.
-
公开(公告)号:US20210130316A1
公开(公告)日:2021-05-06
申请号:US16473745
申请日:2017-12-19
发明人: Syaulan S. YANG , Kuang-Yuan LEE , Edwin SC WU , Ming-Yu HSIAO , Hsiao-Chun WANG , Meng-Hsien LIU , Peter JS CHIU
IPC分类号: C07D401/04 , C07D221/28
摘要: Novel antagonists of toll-like receptor 4 (TLR-4) are provided. More specifically, the novel antagonists of TLR-4 are derived from morphinan. Further, use of said morphinan derivatives in the treatment of diseases and/or disorders mediated by TLR-4, such as autoimmune diseases, inflammation disease and infectious diseases, is provided. Pharmaceutical compositions including said morphinan derivatives are also provided.
-
公开(公告)号:US20210261579A1
公开(公告)日:2021-08-26
申请号:US17253939
申请日:2019-06-20
发明人: Syaulan S. YANG , Kuang Yuan LEE , Yan-Feng JIANG
IPC分类号: C07F9/24
摘要: A novel structure of an opioid antagonist is provided. One of the exemplary compounds of the present disclosure has the structure of Formula (II). The present disclosure overcomes the discomfort of conventional opioid antagonist due to rapid absorption and improves the patient compliance thereof.
-
公开(公告)号:US20200157088A1
公开(公告)日:2020-05-21
申请号:US16620702
申请日:2018-11-30
发明人: Syaulan S. YANG , Kuang Yuan LEE , Yan-Feng JIANG , Yu-Shiou FAN , Meng Hsien LIU , Sheng Hung LIU , Jhih-Liang HUANG
IPC分类号: C07D417/06 , C07D401/06 , C07D413/06 , C07D211/70 , C07D403/06 , C07D417/14 , C07D405/14 , C07D405/10
摘要: The present disclosure provides a benzene fused heterocyclic compound of Formula (I): wherein (A) is a single or double bond; n is 0 or 1; X is —CH2—, O, NR1, or S; A is —C(Ra1)(Ra2)(Ra3) or —N(Ra1)(Ra2), wherein Ra1, Ra2 and Ra3 are independently selected from a group consisting of: H, alkyl, cycloalkyl, heterocyclic alkyl, aryl, heteroaryl, C1-C3 hydrocarbon, —RaaORbb, —C(O)ORaaRbb, —C(O)RaaRbb, —C(O)NRaaRbb, —SO2 RaaRbb and —SO2 NRaaRbb which are optionally substituted by at least one substituent independently selected from a group consisting of: alkyl, cycloalkyl, heterocyclic alkyl, aryl, —Ybb, —ArbbYbb, —ORcc, and —OArbbYbb, wherein Raa, Rbb and Rcc independently are nil, H, halogen, alkyl, or aryl, Ybb is CN or halogen, and Araa and Arbb independently are aryl or heteroaryl; R1 is H or alkyl; R2 is alkyl, cycloalkyl, heterocylic alkyl, aryl, heteroaryl, C1-C6 hydrocarbon optionally substituted by at least one substituent independently selected from a group consisting of: —R2aOR2b, —R2aC(O)OR2bR2c, —R2aC(O)R2bR2c, —R2aC(O)NR2bR2c, —R2aNR2bC(O)NR2cR2d, —R2aNR2bC(O)R2cR2d, —R2aNR2bC(O)OR2cR2d, —R2aSO2R2bR2c, —R2aNR2bSO2NR2cR2d and —R2aSO2NR2bR2c, optionally substituted by at least one substituent independently selected from a group consisting of alkyl, cycloalkyl, heterocyclic alkyl, heteroaryl, and aryl, wherein R2a, R2b, R2c and R2d are independently selected from nil, H, halogen, alkyl, cycloalkyl, heterocyclic alkyl, heteroaryl, aryl or C1-C6 hydrocarbons, optionally substituted by at least one substituent independently selected from a group consisting of —OR2e, ═O, ═S, —SO2R2e, —SO2NR2eR2f, —NR2gSO2NR2eR2f, —NR2gC(O)NR2eR2f, —C(O)NHR2e, —NHC(O)R2e, —NHC(O)OR2e, —NO2, —CO2R2e and —C(O)R2e, wherein R2e, R2f, and R2g independently are H or alkyl.
-
公开(公告)号:US20220153687A1
公开(公告)日:2022-05-19
申请号:US17442296
申请日:2020-03-27
发明人: Syaulan S. YANG , Yan-feng JIANG , Meng-hsien LIU , Chia-hao CHANG , Hao Shiuan LIU , Ying-chu SHIH , Sheng Hung LIU , Chiung Wen WANG , Ting-ni HUANG
IPC分类号: C07C233/42 , C07C235/38 , C07C259/06 , C07C311/20 , C07D233/74 , C07D209/14
摘要: 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.
-
公开(公告)号:US20200247761A1
公开(公告)日:2020-08-06
申请号:US16488517
申请日:2018-01-25
发明人: Syaulan S. YANG , Kuang-Yuan LEE , Meng-Hsien LIU , Ming-Yu HSIAO , Huang-Kai PENG , Chiung-Wen WANG , Edwin SC WU , Peter JS CHIU
IPC分类号: C07D241/04 , C07D211/78 , C07D215/36 , C07C311/21 , C07D231/18 , C07D233/38 , C07D207/48 , C07D211/60 , A61P29/00
摘要: The present invention related to novel sulfonamides or amides as TLR-4 antagonists, and pharmaceutical formulations containing the same and the methods of use thereof. Uses of the present novel sulfonamides or amides include, but are not limited to, the prophylaxis and/or treatment of autoimmune, inflammation, or infection related disorders.
-
-
-
-
-