专利号:WO-2022192582-A1 优先权日:2021-03-10 标 题 :Methods of synthesizing halogenated cannabinoids and derivatives of cannabinoids 发明人:DAVIS ROBERT; BLACK JACOB; SMELTZER THOMAS; COLVIN SEAN 权利人:TREEHOUSE BIOSCIENCES INC 摘要:The technology described herein provides for the synthesis of various cannabinoids, cannabinoid derivatives, and intermediate molecules useful in the synthesis of cannabinoids. For example, the technology described herein provides methods for synthesis of cannabinoids halogenated at the 4-position.
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-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:US-8207337-B2 优先权日:2007-01-29 标 题:Reagent for organic synthesis reaction containing organic triol borate salt 发明人:MIYAURA NORIO; YAMAMOTO YASUNORI 权利人:MIYAURA NORIO; YAMAMOTO YASUNORI; WAKO PURE CHEM IND LTD 摘要:[Problem] n To provide an organoboron compound-containing reagent for organic synthesis reactions which undergoes no trimerization with dehydration, does not necessitate activation with a base, and is stable and highly active. n [Means for Solving Problems] n The reagent for organic synthesis reactions contains an organic triol borate salt represented by any of the general formulae (I) to (III) and general formula (XVI): (wherein R 1 represents alkyl, alkenyl, etc.; R 2 represents optionally substituted alkyl, alkenyl, alkynyl, etc. or represents hydrogen; m + represents an alkaline metal ion, phosphonium ion, or given ammonium ion; M 2+ represents an alkaline earth metal; X represents halogen or alkoxide; Y represents an alkali metal ion, etc.; A represents optionally substituted methylene; and n represents an integer).
专利号:US-9920056-B2 优先权日:2015-06-16 标题:2-oxo-1,3,8-triazaspiro[4.5]decan-3-yl] carboxylic acid derivatives 发明人:BEAUCHAMP THOMAS JAMES; COATES DAVID ANDREW; MARTINEZ-GRAU MARIA ANGELES; TOLEDO MIGUEL ANGEL 权利人:LILLY CO ELI 摘要:The present invention provides compounds of Formula 1, n nwhere A is selected fromn n nand R1, R2 and R3 are defined in the specification, or a pharmaceutically acceptable salt thereof, methods of using the compounds to treat diabetes, and processes for the synthesis of the compounds.
专利号:US-2007232631-A1 优先权日:2005-04-18 标 题 :Design and synthesis of novel tubulin polymerization inhibitors: benzoylphenylurea (bpu) sulfur analogs
[参考文献]: Kenneth D Clevenger, Et Al. N-Alkylboronic Acid Inhibitors Reveal Determinants Of Ligand Specificity In The Quorum-Quenching And Siderophore Biosynthetic Enzyme Pvdq. Biochemistry. 2014 Oct 28;53(42):6679-86.
合成参考文献
摘要:Weibel, J.-M.; Blanc, A.; Pale, P., Science of Synthesis Knowledge Updates, (2018) 1, 84. 摘要:Liang, Y.; Wen, Z.; Cabrera, M.; Howlader, A. H.; Wnuk, S. F., Science of Synthesis Knowledge Updates, (2020) 1, 216.