专利号:US-9745303-B2 优先权日:2012-10-12 标题:Synthesis and intermediates of pyrrolobenzodiazepine derivatives for conjugation 发明人:HOWARD PHILIP WILSON 权利人:SPIROGEN SÀRL; MEDIMMUNE LTD 摘要:A method of synthesing a compound of formula (I) from a compound of formula (III).
专利号:US-9707301-B2 优先权日:2011-10-14 标题 :Pyrrolobenzodiazepines and targeted conjugates 发明人:JEFFREY SCOTT; BURKE PATRICK; HOWARD PHILIP WILSON 权利人:SEATTLE GENETICS INC; MEDIMMUNE LTD 摘要:This invention relates to pyrrolobenzodiazepines (PBDs), in particular pyrrolobenzodiazepine dimers having a C2-C3 double bond and an aryl group at the C2 position in each monomer unit, and their inclusion in targeted conjugates. The differing substituent groups may offer advantages in the preparation and use of the compounds, particularly in their biological properties and the synthesis of conjugates, and the biological properties of these conjugates.
专利号:US-7122694-B2 优先权日:1998-11-06 标 题 :Hydroboronation process 发明人:MARCUCCIO SEBASTIAN MARIO; RODOPOULOS MARY; WEIGOLD HELMUT 权利人:BORON MOLECULAR PTY LTD 摘要:The invention relates to processes for the synthesis of aryl or alkene borates which comprises reacting: (i) an olefinic compound having a halogen or halogen-like substituent in a vinylic substitution position, or (ii) an aromatic ring having a halogen or halogen-like substituent in a ring substitution position, with a disubstituted monohydroborane in the presence of a Group 8-11 metal catalyst. The invention also relates to the use of these borates in coupling reactions. The invention further relates to certain disubstituted monohydroboranes and aryl or alkene borates.
专利号:US-2025026766-A1 优先权日:2022-01-12 标题 :Thiazolopyridyl Amide Derivatives as DNA Polymerase Theta Inhibitors 发明人:LI JING; XU WENQING; WANG ZHIWEI 权利人:BEIGENE LTD 摘要:The present invention relates to compounds containing thiazolopyridyl amide structure, the process for their synthesis, as well as the use of such compounds for inhibiting DNA Polymerase Theta (Pol Theta), and in the treatment of various diseases including cancers.
专利号:US-8785632-B2 优先权日:2004-08-26 标 题:Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors 发明人:CUI JINGRONG JEAN; FUNK LEE ANDREW; JIA LEI; KUNG PEI-PEI; MENG JERRY JIALUN; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; SHEN HONG; TRAN-DUBE MICHELLE 权利人:CUI JINGRONG JEAN; FUNK LEE ANDREW; JIA LEI; KUNG PEI-PEI; MENG JERRY JIALUN; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; SHEN HONG; TRAN-DUBE MICHELLE; AGOURON PHARMA; PFIZER 摘要:Enantiomerically pure compound of formula 1 n nare provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.
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.
[参考文献]: Dai, Y., Hartandi, K., Ji, Z., Et Al Al. Discovery Of N-(4-(3-Amino-1H-Indazol-4-Yl)Phenyl)-N'-(2-Fluoro-5-Methylphenyl)Urea (Abt-869), A 3-Aminoindazole-Based Orally Active Multitarged Receptor Tyrosine Kinase Inchibitorj. Chem.50 (7) 1584-1597 (2007). [参考文献]: Paraiso, Kht, Haarberg, He, Wood, E., Et Al.The Hsp9 0 Inhibitor Xl888 Overcomes Braf Inchibitor Resistance Mediated Through Diverse Mechanisms Clin. Cancer Res. 18(9) 2502-2514(2012).
合成参考文献
摘要:Kitanosono, T.; Kobayashi, S., Science of Synthesis: Advances in Organoboron Chemistry towards Organic Synthesis, (2019) 1, 303. 摘要:Jiang, R.; Yang, P.; You, S.-L., Science of Synthesis: Knowledge Updates, (2023) 1, 162.