专利号:US-2009099218-A1 优先权日:2007-09-17 标题 :Synthesis of novel tubulin polymerization inhibitors: benzoylphenylurea (bpu) sulfur analogs 发明人:KHAN SAEED R; HALLUR GURULINGAPPA; HIDALGO MANUEL; JIMENO ANTONIO 权利人:KHAN SAEED R; HALLUR GURULINGAPPA; HIDALGO MANUEL; JIMENO ANTONIO 摘要:This invention provides a series of BPU analogues; their synthesis and evaluated biological activity. BPU sulfur analogues were found to possess up to 20 fold increased potency, when compared to compound 1, in various cancerous cell lines.
专利号:US-12275733-B2 优先权日:2016-11-07 标 题:Substituted pyrido[3,4-b]indoles for the treatment of cartilage disorders 发明人:GRETZKE DIRK; RITZELER OLAF; HEINELT UWE; WEHNER VOLKMAR; SCHMIDT FRIEDEMANN 权利人:SANOFI SA 摘要:The present invention relates to 8-aryl-substituted and 8-heteroaryl-substituted 9H-pyrido[3,4-b]indoles of the formula (I), in which A, E, G, R1 to R6 and R10 are as defined in the claims, which stimulate chondrogenesis and cartilage matrix synthesis and can be used in the treatment of cartilage disorders and conditions in which a regeneration of damaged cartilage is desired, for example joint diseases such as osteoarthritis. The invention furthermore relates to processes for the synthesis of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
专利号:US-7595326-B2 优先权日:2005-04-18 标题 :Synthesis of novel tubulin polymerization inhibitors: benzoylphenylurea (BPU) sulfur analogs 发明人:KHAN SAEED R; HALLUR GURULINSAPPA; HIDALGO MANUEL; JIMENO ANTONIO 权利人:CHAMPIONS BIOTECHNOLOGY INC 摘要:A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6 n and 7 d were shown to possess up to 10-fold increased potency, when compared to compound 1, against cancer cell lines. 6 n was more effective than compound 1 in causing apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6 n retained significant ability to inhibit tubulin assembly, with an IC 50 of 2.1 μM.
专利号:WO-2024064745-A1 优先权日:2022-09-21 标 题:Synthesis of reldesemtiv 发明人:PETERSON MATTHEW W; LU QING; MORGAN BRADLEY P; ASHCRAFT LUKE W; ANDERSEN DENISE 权利人:CYTOKINETICS INC 摘要:Provided herein is a process for the preparation of reldesemtiv and salts thereof. Also provided herein are intermediates used in this process and their preparation.
专利号:WO-2025102245-A1 优先权日:2023-11-14 标题:Synthesis method for dual endothelin receptor antagonist aprocitentan 发明人:XU XIANGUANG; WANG ZHEN; ZHU GUORONG; TU YONGJUN 权利人:ZHEJIANG TIANYU PHARMACEUTICAL CO LTD 摘要:Provided in the present invention is a synthesis method for aprocitentan, comprising the following steps: 1) a compound of formula X and a sulfonylation reagent compound of formula XI undergoing a sulfonylation reaction to prepare a compound of formula XII; and 2) removing an R protective group on the pyrimidine sulfonamide compound of formula XII obtained in the previous step, so as to obtain aprocitentan. The synthesis method of the present invention overcomes the problem in the prior art that preparing macitentan by means of condensation of chloropyrimidine and sulfonamide needs to use an excessive amount of a strong base and involves a relatively low conversion efficiency, relatively many side products and other defects. The synthesis method does not need using a fluorine reagent for fluorination, involves economical steps, is environmentally-friendly, and has a relatively low comprehensive production cost. Compared with existing methods for preparing aprocitentan, the method of the present invention has characteristics of easily available raw materials, being environmentally-friendly and economical, and the like, thereby facilitating the industrial production of aprocitentan.
专利号:US-6121448-A 优先权日:1995-03-28 标题 :Pyrimidine compounds 发明人:LEWIS ROBERT ANDREWS; GOODBY JOHN WILLIAM; TOYNE KENNETH JOHNSON; HIRD MICHAEL 权利人:SECR DEFENCE BRIT 摘要:The synthesis of novel compound (I) is described: 5-bromo-2-iodopyrimidine may be used for the synthesis of a range of chemical compounds both known and novel. The synthesis of a number of novel liquid crystalline compounds is described.
[参考文献]: Angeles Mosquera, Et Al. Cross-Coupling Reactions Of Indium Organometallics With 2,5-Dihalopyrimidines: Synthesis Of Hyrtinadine A. Org Lett. 2008 Sep 4;10(17):3745-8.