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-2025172829-A1 优先权日:2025-02-11 标 题:Synthesis of chimeric peptosomes hybridized with rod-shaped gold nanoparticles and aptamer-targeted for breast cancer therapy and imaging 发明人:SABOURY SICHANI BITA 权利人:SABOURY SICHANI BITA 摘要:The invention focuses on creating chimeric peptosomes combined with gold nanoparticles and fitted with aptamers for targeted therapy and imaging of breast cancer. It aims to solve the problem of effectively targeting breast cancer cells without harming healthy cells. The method uses a special polypeptide made of polyethylene glycol (PEG) and poly(γ-benzyl L-glutamate) (PGBLG) to form a peptosome with a strong core for containing the chemotherapy drug doxorubicin. The peptosome is designed for controlled release of the drug and also allows for the inclusion of gold nanoparticles. The EpCAM aptamer is used to target cancer cells more precisely, improving therapy effectiveness and imaging through the unique properties of gold nanoparticles. This new platform enhances treatment success while minimizing side effects, representing a major advance in targeted cancer therapy.
专利号:US-6703213-B2 优先权日:1998-02-02 标 题:Substrate analogs for MurG, methods of making same and assays using same 发明人:KAHNE SUZANNE WALKER; MEN HONGBIN; PARK PETER; GE MIN 权利人:UNIV PRINCETON 摘要:General methods for monitoring the activity of MurG, a GlcNAc transferase involved in bacterial cell wall biosynthesis, is disclosed. More particularly, the synthesis of simplified substrate analogs of Lipid I (the natural substrate for MurG), which function as acceptors for UDP-GlcNAc in an enzymatic reaction catalyzed by MurG, is described. Assays using the substrate analogs of the invention are further disclosed, which are useful for identifying a variety of other substrates, including inhibitors of MurG activity, for facilitating mechanistic and/or structural studies of the enzyme and for other uses. High throughput assays are also described.
专利号:US-10927147-B2 优先权日:2015-12-10 标 题:Muramyl peptide derivative compound, synthesis and uses thereof 发明人:ELLA KRISHNA MURTHY; BRUNDA GANNERU; KUMAR HALMATHUR MAHABALARAO SAMPATH; SREEKANTH MIRYALA 权利人:BHARAT BIOTECH INT LTD; COUNCIL SCIENT IND RES 摘要:The invention relates to novel Muramyl Dipeptide (MDP) derivative compound of structural Formula-VIII, a process for synthesis, intermediates used in the synthesis and use thereof. n n n n n n n n n n Wherein, R can be both linear and branched alkyl, aryl, substituted aryl and alkoxy alkyl. These compounds possess excellent pharmacological properties, in particular immunomodulating properties for use as adjuvant in vaccine formulations. These compounds are, particularly useful as adjuvants in vaccines.
专利号:US-10576147-B2 优先权日:2015-12-15 标题:Muramyl peptide derivative compound, synthesis and uses thereof 发明人:ELLA KRISHNA MURTHY; BRUNDA GANNERU; KUMAR HALMATHUR MAHABALARAO SAMPATH; SREEKANTH MIRYALA 权利人:BHARAT BIOTECH INT LTD; COUNCIL SCIENT IND RES 摘要:The invention relates to novel Muramyl Dipeptide (MDP) derivative compound of structural Formula-VIII, a process for synthesis, intermediates used in the synthesis and use thereof; n nwherein R 1 and R 2 both are hydrogen; or R 1 is hydrogen and R 2 is alkyl or aryl; or R 1 is alkyl or aryl and R 2 is hydrogen; or R 1 and R 2 both are alkyl or aryl (same or different groups); wherein alkyl group constitute C1-C6 alkyl or higher (both linear and branched) with or without heteroatoms; and aryl group constitute phenyl, substituted phenyl, heteraryl, arylalkyl and polynuclear aromatics. These compounds possess excellent pharmacological properties, in particular immunomodulating properties for use as adjuvant in vaccine formulations. These compounds are, particularly useful as adjuvants in vaccines.
专利号:EP-2772497-B1 优先权日:2011-10-24 标 题 :Controlled synthesis of polyglutamates with low polydispersity and versatile architectures
参考标题:Synthèse D'Analogues Structuraux De L'élédoïsine. 1RePartie: Préparation Des Produits Intermédiaires 作者:Ed. Sandrin,R. A. Boissonnas 摘要:The Preparation Of New Dipeptides And Tripeptides, Which Are Useful Intermediates In The Synthesis Of Eledoisin Analogues, Is Described.
合成参考文献
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