专利号:US-9573873-B2 优先权日:2014-06-03 标题:Catalytic method for dibenzocycloheptane synthesis and allocolchicinoid synthesis 发明人:GREEN JAMES; MEHDI MARIAM; DJURDJEVIC SINISA 权利人:UNIV OF WINDSOR 摘要:In a non-limiting embodiment, there is provided a compound of formula (I), which may permit for a method or use in treating or preventing a cancer, such as pancreatic cancer or leukemia. In one embodiment, there is also provide a method of preparing a compound of formula (Ia), the method including conducting a cyclization reaction of a compound of formula (III) to obtain a compound of formula (IV), wherein conducting the cyclization reaction comprises conducting a Michael reaction in the presence of a Lewis acid.
专利号:WO-2004087679-A1 优先权日:2003-04-01 标 题 :2, 4, 6-trisubstituted pyrimidine derivatives useful for the treatment of neoplastic and autoimmune diseases 发明人:OBRECHT DANIEL; ERMERT PHILIPP; LUTHER ANATOL; EBERLE MARTIN; BACHMANN FELIX 权利人:APONETICS AG; OBRECHT DANIEL; ERMERT PHILIPP; LUTHER ANATOL; EBERLE MARTIN; BACHMANN FELIX 摘要:The invention relates to substituted pyrimidines of formula (I) wherein V represents a bond or CR6R7, W represents a bond, NR8 or oxygen, X represents sulfur, or nitrogen substituted by hydrogen or R5, Y represents -CH2-, -CH2CH2-, -CO- or -CS-, R1 represents unsubstituted or substituted aryl or heteroaryl, and the substituents R2, R3, R4, R5, R6, R7 and R8 have the meanings given in the specification. These compounds are selectively inducing apoptosis in cancer cells and can be used for the treatment of neoplastic and autoimmune diseases. The invention relates also to methods of synthesis of such compounds, to their use as medicaments, to pharmaceutical compositions containing same, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same.
专利号:US-9611281-B2 优先权日:2013-12-05 标题:BODIPY derivatives and methods of synthesis and use thereof 发明人:YOU YOUNGJAE; AWUAH SAMUEL; WATLEY RYAN 权利人:UNIV OKLAHOMA 摘要:Derivatives of BODIPY (boron dipyrromethene difluoride) and their synthesis and use are disclosed.
专利号:US-7572778-B2 优先权日:2003-07-18 标题 :Fluorocombretastatin and derivatives thereof 发明人:GIANNINI GIUSEPPE; ALLOATTI DOMENICO; MARCELLINI MARCELLA; MARZI MAURO; RICCIONI TERESA; TINTI MARIA ORNELLA 权利人:SIGMA TAU IND FARMACEUTI 摘要:The present invention is related to new derivatives of Combretastatin, of Formula n nobtained by total synthesis. The strategy developed for each of the compounds is to i) replace a halogen (i.e. fluorine atom) to hydrogen on olefinic bound; ii) replace an aromatic ring in a natural product with an amino-aromatic ring. Said compounds recognize and bind the tubulin site: are useful for treating pathological states which arise from or are exacerbated by cell proliferation—as anticancer and/or antiangiogenic activity, in a mammal—to pharmaceutical compositions comprising these compounds.
专利号:US-11306103-B2 优先权日:2017-11-30 标题:Thieno[3,2-b]pyridine-5(4H)-one derivative compound, preparation method thereof and use thereof 发明人:LEE JONG SEOK; SUNG DAN BI; MUN BO HYUN; LEE HYI SEUNG; LEE YEON JU; LEE JI HOON; SHIN HEE JAE; PARK SOL 权利人:KOREA INST OCEAN SCI & TECH 摘要:The present invention relates to a novel thieno[3,2-b]pyridine-5(4H)-one derivative compound, a preparation method thereof, and a use thereof. The novel thieno[3,2-b]pyridine-5(4H)-one derivative compound according to the present invention is synthesized via an aza-[3+3] cyclization addition reaction using BOP, wherein the compound is obtained by synthesizing a 4-arylthiophen-3-amine in which aryl groups such as 4-piperidyl-C6H4, 4-pyrrolidyl-C6H4, 4-MeOC6H4, 3,4,5-(MeO)3C6H4, C6H5, 4-C6H5C6H4, and 4-F3COC6H4 are introduced via a synthesis process by a bromination reaction, a hydrolysis reaction, a decarboxylation reaction, and a Suzuki coupling reaction of methyl 3-aminothiophene carboxylate, and by synthesizing 4-arylthiophen-3-amine and mono-methyl fumarate via a formal aza-[3+3] cyclization addition reaction using BOP and conjugation. Accordingly, novel thieno[3,2-b]pyridine-5(4H)-one derivative compounds according to the present invention have fluorescence properties with a wide range of emission wavelengths and thus may be utilized in various industrial fields such as physics, chemistry, and biomedical research.
专利号:US-2015158888-A1 优先权日:2013-12-05 标题:BODIPY Derivatives and Methods of Synthesis and Use Thereof
摘要:Tomé, A. C., Science of Synthesis Knowledge Updates, (2015) 2, 89. 摘要:Guram, A. S.; Milne, J. E.; Tedrow, J. S.; Walker, S. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 22. 摘要:Guram, A. S.; Milne, J. E.; Tedrow, J. S.; Walker, S. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 102. 摘要:Le Bras, J.; Muzart, J., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 187. 摘要:Cormier, M.; Goddard, J.-P., Science of Synthesis, (2020) , 171.