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专利信息

专利号:US-9623125-B2
优先权日:2011-10-24
标 题:Controlled synthesis of polyglutamates with low polydispersity and versatile architectures
发明人：VICENT DOCON MARIA JESUS; BARZ MATTHIAS; CANAL FABIANA; CONEJOS SANCHEZ INMACULADA; DURO CASTANO AROA; ENGLAND RICHARD MARK
权利人:FUND DE LA COMUNIDAD VALENCIANA “CENTRO DE INVESTIG PRINCIPE FELIPEâ€?
摘要:Polyglutamates are well known to be highly biocompatible, biodegradable and multifunctional polymers, which have been already used as building blocks in polymer drug conjugates and polymeric micelles. Those systems have been applied to various medical applications ranging from therapy to molecular imaging. Furthermore a polyglutamic acid (PGA) paclitaxel conjugate has already entered clinical studies (Opaxioâ„¢ PGA-PTX conjugate currently in phase III of Clinical trials). n In this context, a synthetic pathway to a plethora functional polyglutamates (homopolymers, block-co-polymers, tribocks) with well-defined structure, adjustable molecular weight (Mw) and low dispersity (D=Mw/Mn<1.2) applying the ring opening polymerization (ROP) of N-carboxyanhydrides (NCA) has been developed. Additionally, the acid moieties of the polyglutamates can be activated with 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium (DMTMM) and various functionalities can be easily introduced by “post-polymerization modificationâ€? yielding a set orthogonal reactive attachment sides. The reactive moieties, such as azides, maleimides, thiols, akynes (linear or cyclic) offer the opportunity of specific conjugation of the drugs, targeting moieties or markers. Besides introducing reactive groups the functionalization strategy was also used for PEGylation of PGA reducing charge induced interactions and therefore pharmacological properties, such as blood circulation time may be adjusted. n In summary, a tool kit of various polyglutamates has been developed enabling the synthesis of a variety of polymer drug conjugates or polymer based imaging agents. The functional polymeric precursors developed will allow us to functionalize and therefore adjust the polymer properties to a desired aplication.

专利号:WO-2023169082-A1
优先权日:2022-10-24
标 题:Synthesis method and application of benzothiadiazole-1-ketone compound and derivative thereof
发明人：YI WEI; ZHOU ZHI; WU LIEXIN
权利人:UNIV GUANGZHOU MEDICAL
摘要:Disclosed in the present invention are a synthesis method and application of a benzoselenazole-1-ketone compound and a derivative thereof. Sulfoximine and the element selenium are used as raw materials, and by means of a rhodium catalysis direct C-H functionalization reaction, synthesis of a series of benzoselenazole-1-ketone compounds is achieved. The solution has the advantages of strong functional group compatibility, wide substrate universality, mild conditions, simple operations, and high efficiency and universality. Meanwhile, sulfoximine and the element selenium are used as initial raw materials, a direct C-H functionalization reaction is carried out, and by means of chiral phosphoric acid, synthesis of the chiral benzoselenazole-1-ketone compound is achieved. The application prospect is good, and a sulfydryl structure in biomacromolecules such as polypeptides, saccharides, drug molecules and proteins can be specifically marked. Good anti-SARS-CoV-2 virus activity is exhibited, a trastuzumab biological conjugate can effectively image HER 2 receptors on the cell surface, displays strong fluorescence, and can be applied to the preparation of an imaging reagent for the HER 2 receptor on the cell surface.

专利号:US-2015087788-A1
优先权日:2011-10-24
标题 :Controlled Synthesis of Polyglutamates with Low Polydispersity and Versatile Architectures

专利号:US-2009286938-A1
优先权日:2008-04-30
标题 :Synthesis of hybrid block copolymers from difluoroacetate ammonium salts
发明人：SILL KEVIN N; CARDOEN GREGOIRE; BREITENKAMP KURT
权利人:INTEZYNE TECHNOLOGIES INC
摘要:The present invention provides polymerization initiators and uses thereof.