4-氰基苯硼酸置于氢气体系中,用 甲醇 作为反应溶剂,20.0 °C,344.75 Kpa 条件下,反应 4.0H,以38.9%的收率获得产物4-氨甲基苯硼酸 参考文献: Bromodomain Ligands Capable Of Dimerizing In An Aqueous Solution[fr] Ligands De Bromodomaine Pouvant Se Dimériser Dans Une Solution Aqueuse 标题: Bromodomain Ligands Capable Of Dimerizing In An Aqueous Solution[fr] Ligands De Bromodomaine Pouvant Se Dimériser Dans Une Solution Aqueuse 摘要:本文描述的是一种单体,当与水性介质中的一个,两个,三个或更多其他单体接触时,能够形成具有生物学用途的多聚体.在一个方面,这些单体可能能够在水性介质中(例如体内)与另一个单体结合,形成一个多聚体(例如二聚体).考虑到的单体可能包括一个配体基团,一个连接元素和连接配体基团与连接元素的连接元素.在水性介质中,这些考虑到的单体可以通过每个连接元素相互结合,因此可以同时调节一个或多个生物分子,例如,调节蛋白质上的两个或更多结合结构域或不同蛋白质上的结合结构域.
专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-9839642-B2 优先权日:2014-05-09 标 题:Beta-tetrazolyl-propionic acids as metallo-beta-lactamase inhibitors 发明人:TANG HAIFENG; YANG SHU-WEI; MANDAL MIHIR; SU JING; LI GUOQING; PAN WEIDONG; TANG HAIQUN; DEJESUS REYNALDA; PAN JIANPING; HAGMANN WILLIAM; DING FA-XIANG; XIAO LI; PASTERNAK ALEXANDER; HUANG YUHUA; DONG SHUZHI; YANG DEXI 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
专利号:US-2007275968-A1 优先权日:2004-09-07 标 题 :Substituted Biphenyl Derivative 发明人:KURATA HITOSHI; NISHIMATA TOYOKI; WATANABE YUKIKO; EBISAWA MASAYUKI; FUJIMOTO TEPPEI; KOBAYASHI HIDEKI 权利人:KURATA HITOSHI; NISHIMATA TOYOKI; WATANABE YUKIKO; EBISAWA MASAYUKI; FUJIMOTO TEPPEI; KOBAYASHI HIDEKI 摘要:The present invention relates to a biaryl derivative or a pharmacologically acceptable salt thereof having an excellent collagen-synthesis inhibition activity. A biaryl derivative having a structure represented by the following General Formula (I) or a pharmacologically acceptable salt thereof: n nwherein n R 1 represents a C 6 -C 10 aryl group which is substituted with one to three group(s) each independently selected from the group consisting of a group defined by formula R-L-, a di-(C 1 -C 6 alkyl)amino group, a di-(C 1 -C 6 alkyl)aminosulfonyl group, a hydroxyaminocarbonyl group, and a halogen atom, and so on; R represents a C 1 -C 6 alkyl group, and so on; L represents a sulfonyl group, an aminosulfonyl group, or a sulfonylamino group, and so on; R 2 represents a hydrogen atom, and so on; A represents a group defined by formula (II), (III), or (IV); R 3 represents a C 1 -C 6 alkyl group, and so on; and R 4 represents a C 1 -C 6 alkyl group, and so on.
专利号:US-7659399-B2 优先权日:2005-01-05 标 题 :1-thia-2,4a-diaza-cyclopenta[b]napththalene-3,4-diones and related compounds as anti-infective agents 发明人:BRADBURY BARTON JAMES; WILES JASON ALLAN 权利人:ACHILLION PHARMACEUTICALS INC 摘要:The invention provides compounds and salts of Formula I and Formula II: n nwhich possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A 1 , A 8 , R 2 , R 3 , R 5 , R 6 , R 7 , and R 9 are defined herein.n n Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.
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