CAS: 2001-94-7; Potassium 2,2'-((2-(Bis(Carboxymethyl)Amino)Ethyl)Azanediyl)Diacetate

相似化合物

25102-12-9 65501-24-8 139-33-3

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-12221452-B2
优先权日:2017-10-04
标题:Synthesis of cantharidin
发明人：DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R
权利人:VERRICA PHARMACEUTICALS INC
摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).

专利号:US-6962780-B2
优先权日:2000-06-12
标 题 :Method for synthesis of nucleic acids
发明人：NAKAYAMA TOMOKO; NISHIMURA NAOYUKI
权利人:SHIMADZU CORP
摘要:The present invention is a method for synthesis of nucleic acids to amplify an intended nucleic acid in a region in which a GC content is rich, wherein a polyhydric alcohol and/or ammonium sulfate is present in an amplification reaction solution. According to the present invention, it is possible to amplify nucleic acids in a GC rich region efficiently and directly from a sample such as blood containing lots of PCR inhibitory substances without undergoing a process of isolating and purifying the nucleic acid, even though conducting PCR in the GC rich region tends to be difficult using conventional processes even if purified DNA is used.

专利号:US-11155562-B2
优先权日:2014-06-30
标 题 :Synthesis of halichondrin analogs and uses thereof
发明人：KISHI YOSHITO; UEDA ATSUSHI; YAMAMOTO AKIHIKO; KATO DAISUKE
权利人:HARVARD COLLEGE
摘要:The present invention provides halichondrin analogs, such as compounds of Formula (I). The compounds may bind to microtubule sites, thereby inhibiting microtubule dynamics. Also provided are methods of synthesis, pharmaceutical compositions, kits, methods of treatment, and uses that involve the compounds for treatment of a proliferative disease (e.g., cancer). Compounds of the present invention are particularly useful for the treatment of metastatic breast cancer, non-small cell lung cancer, prostate cancer, and sarcoma. The included methods of synthesis are useful for the preparation of compounds of Formula (I)-(III) along with naturally occurring halicondrins (e.g., halichondrin B & C, norhalichondrin A, B, & C, and homohalichondrin A, B, & C). Also included are methods for interconverting between the halichondrins, norhalichondrins, and homohalichondrins and their unnatural epimers at the C38 ketal stereocenter through the use of an acid-mediated equilibration.

专利号:US-9982005-B2
优先权日:2013-04-04
标 题 :Macrolides and methods of their preparation and use
发明人：MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG
权利人:HARVARD COLLEGE
摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.

专利号:WO-2022260545-A1
优先权日:2021-06-11
标题:Synthesis of a novel glucose-conjugated methotrexate and its application for the treatment and prevention of neoplasms
发明人：AGRAWAL SIDDARTH; WOŹNIAK MARTA; MAKUCH SEBASTIAN; Szeja WiesÅ‚aw; PASTUCH-GAWOÅ?EK GABRIELA; KRAWCZYK MONIKA; WiÅ›niewski Jerzy; GAMIAN ANDRZEJ; ZIÓÅ?KOWSKI PIOTR
权利人:UNIV MEDYCZNY IM PIASTOW SLASKICH WE WROCLAWIU
摘要:The subject of the invention is a new methotrexate-glucose conjugate derivative, its synthesis, and its use in the treatment and prevention of neoplasms, preferably in the treatment and prevention of neoplasms selected from: skin cancer, colorectal cancer, breast cancer, gastric cancer, sarcoma and lung cancer.