专利号:WO-2017080770-A1 优先权日:2015-11-10 标题 :Synthesis of (z)-endoxifen hydrochloride 发明人:HEINKELE GEORG; MUERDTER THOMAS; SCHWAB MATTHIAS 权利人:ROBERT BOSCH GES FÜR MEDIZINISCHE FORSCHUNG MBH 摘要:The invention relates to the synthesis of tamoxifen, endoxifen and derivatives thereof. Starting from a substituted benzoic acid derivative and 2-phenoxyethyl halide, the intermediate product of general formula (I) is obtained. The compound of general formula (VI) or a salt thereof is obtained from the compound of general formula (I), via isomer purification of the compound of general formula (I) by obtaining the (Z)-isomers and reacting the (Z)-isomers with an amine of formula HNR 6 R 7 . Alternatively, the compound of general formula (I) is reacted with a compound of formula HNR 6 R 7 , and the amine thus obtained is then subjected to isomer purification, wherein the compound of general formula (VI) or a salt thereof is obtained.
专利号:US-5446203-A 优先权日:1992-08-25 标题:Synthesis of haloenones and aryl or alkyl substituted enones or alkenes 发明人:MCNELIS EDWARD 权利人:UNIV NEW YORK 摘要:Alternative methods for synthesizing haloenones and haloakenes and their use as starting materials for synthesis of substituted or unsubstituted alkyl and aryl substituted enones and alkenes, including tamoxifen and tamoxifen analogs, using such haloenones and haloalkenes.
专利号:US-10975069-B2 优先权日:2014-04-01 标 题 :Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof 发明人:HAWKINS WILLIAM; MACH ROBERT; SPITZER DIRK; VANGVERAVONG SUWANNA; VAN TINE BRIAN 权利人:UNIV WASHINGTON 摘要:Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described, such as the methanesulfonate salt of a compound of structural Formula IV, n n, wherein n is an integer chosen from 1, 2, 3, 4, and 5, and R 2 is H or methyl. At least one described molecular species exhibits an IC 50 value below 5 μM against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo. It led to a 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.
专利号:US-2006177929-A1 优先权日:2003-03-24 标题 :Regulation of self-renewal in stem cells 发明人:KLUG CHRISTOPHER A 权利人:KLUG CHRISTOPHER A 摘要:Disclosed are methods for regulating the self-renewal capacity of stem cells such as, but not limited to, primitive hematopoietic stem cells (HSCs) (both mouse and human) by modulating the function and/or activity of target factors that are controlled or altered in their regulation by AML1-ETO expression in stem cells such as HSC. Target factors include, but are not limited to, AML1, C/EBP alpha, and/or PU.1 either individually, or in combinations, Altering the function and/or activity of such target factors in HSC leads to inhibition of HSC differentiation and stimulation of HSC self-renewal capacity. Modulation of target factor activity may be achieved at the level of synthesis of these target factors, interaction with cellular factors required for basal activity or enhanced activity, such as cofactors, interactions with their DNA binding motifs, or by targeted degradation or inhibition of their mRNAs.
专利号:US-2006078560-A1 优先权日:2003-06-23 标 题 :Method of inducing apoptosis and inhibiting cardiolipin synthesis 发明人:JAMIL HARIS; AHMAD MOGHIS U; AHMAD IMRAN 权利人:NEOPHARM INC 摘要:The present invention provides a method for inducing apoptosis within a cell by exposing the cell to an inhibitor of cardiolipin synthesis under conditions sufficient to induce apoptosis within the cell. The method can be used to investigate or treat disorders such as cancer, obesity, and cardiovascular disorders. The invention also provides a pharmaceutical composition including an inhibitor of cardiolipin synthesis and a liposomal carrier.
专利号:US-11999693-B2 优先权日:2015-09-24 标 题:Synthetic sphingolipid-like molecules, drugs, methods of their synthesis and methods of treatment 发明人:EDINGER AIMEE L; HANESSIAN STEPHEN 权利人:UNIV CALIFORNIA; THE UNIV DE MONTREAL 摘要:Small molecules comprised of azacyclic constrained sphingolipid-like compounds and methods of their synthesis are provided. Formulations and medicaments are also provided that are directed to the treatment of disease, such as, for example, neoplasms, cancers, and other diseases. Therapeutics are also provided containing a therapeutically effective dose of one or more small molecule compounds, present either as pharmaceutically effective salt or in pure form, including, but not limited to, formulations for oral, intravenous, or intramuscular administration.
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合成参考文献
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