CAS: 6151-30-0; Quinacrine 2Hcl 2H2O

专利信息

专利号:WO-2017082924-A1
优先权日:2015-11-13
标题 :Peptide and peptide mimetic binding antagonists of polo-like kinase 1 polo box domain and methods of use
发明人：BURKE TERRENCE R JR; HYMEL DAVID
权利人:THE US SECRETARY DEPT OF HEALTH & HUMAN SERVICES
摘要:The description provides novel compounds that may serve as anticancer therapeutics. The compounds of the description bind to polo-like kinases through the polo-box domain. The peptide derivatives of the description have achieved improved efficacy in biochemical assays against Plk1. The description also provides methods of use, methods of preparation, compositions, and kits thereof. Further, the description provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.

专利号:US-10905769-B2
优先权日:2015-11-13
标 题:Peptide and peptide mimetic binding antagonists of polo-like kinase 1 polo box domain and methods of use
发明人：BURKE JR TERRENCE R; HYMEL DAVID T; TSUJI KOHEI
权利人:THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES
摘要:The description provides novel compounds that may serve as anticancer therapeutics. The compounds of the description bind to polo-like kinases through the polo-box domain. The peptide derivatives of the description have achieved improved efficacy in biochemical assays against Plk1. Exemplary compounds of the description include macrocyclic peptidomimetics with high affinity and selectivity for polo-like kinases, which may provide the basis for a new genre of anticancer therapeutics. Other exemplary compounds of the description include bi-valent compounds with that bind to polo-like kinases through both kinase domain and polo-box domain simultaneously by incorporating additional moieties that target Plk1 kinase domain, which significantly enhances affinitity relative and may provide the basis for a new genre of anticancer therapeutics. The description also provides methods of use, methods of preparation, compositions, and kits thereof. Further, the description provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.

专利号:US-7393954-B2
优先权日:2002-12-12
标题:Process for the production of pentostatin aglycone and pentostatin
发明人：NADJI SOURENA; SMOOT JAMES; SAMPATH UMASHANKER
权利人:RELIABLE BIOPHARMACEUTICAL COR
摘要:A novel, scaleable and improved process for preparing pentostatin and its analogs is disclosed. The method comprises the diastereospecific synthesis of the nucleobase from commercially available L-Dialkyl tartarates.

专利号:US-7582748-B2
优先权日:2003-03-20
标题:Methods of manufacture of 2′-deoxy-β-L-nucleosides
发明人：RABI JAIME A
权利人:MICROBIOL QUIMICA FARMACEUTICA
摘要:The present invention relates to the synthesis of 2′-deoxy-β-L-thymidine, 2′-deoxy-β-L-uridine and 2′-deoxy-β-L-cytidine, and their derivatives, such as the 3′-O-acyl or 3′,5′-O-diacyl prodrugs, including the 3′-O-L-aminoacyl and 3′,5′-O-L-diaminoacyl prodrugs, and particularly the 3′-O-L-valinyl and 3′,5′-O-L-divalinyl prodrugs.

专利号:US-2014243404-A1
优先权日:2010-09-14
标题 :Unique halogen-induced cyclizations, reagents therefor, and compounds produced thereby
发明人：SNYDER SCOTT ALAN; TREITLER DANIEL S; BRUCKS ALEXANDRIA P; GOLLNER ANDREAS; CHIRIAC MARIA I; WRIGHT NATHAN E; PFLUEGER JASON J; BREAZZANO STEVEN P
权利人:SNYDER SCOTT ALAN; TREITLER DANIEL S; BRUCKS ALEXANDRIA P; GOLLNER ANDREAS; CHIRIAC MARIA I; WRIGHT NATHAN E; PFLUEGER JASON J; BREAZZANO STEVEN P; UNIV COLUMBIA
摘要:This disclosure is related to halonium compounds useful for cyclization of polyenes, alkenoic acids, and alkenyl alkyl ethers, and halogenation of aromatic compounds. The synthesis of such halonium compounds, compounds made using such halonium compounds, and synthesis of natural compounds, including decalins, using the halonium compounds is also disclosed. A representative halonium compound of the disclosure is:

专利号:US-5688992-A
优先权日:1995-03-31
标题 :O-malonyltryrosyl compounds, O-malonyltryrosyl compound-containing peptides, and use thereof
发明人：BURKE JR TERRENCE R; YE BIN; AKAMATSU MIKI; KOLE HEMANTA K; YAN XINJIAN; ROLLER PETER R
权利人:US HEALTH
摘要:The present invention relates to non-phosphorus containing O-malonyltryrosyl compounds, derivatives thereof, uses of the O-malonyltryrosyl compounds in the synthesis of peptides, and O-malonyltryrosyl compound-containing peptides. The O-malonyltyrosyl malonyltyrosyl compounds and O-malonyltryrosyl compound-containing peptides of the present invention are uniquely stable to phosphotases, capable of crossing cell membranes, suitable for application to peptide synthesis of O-malonyltryrosyl compound-containing peptides, and amenable to prodrag defivatization for delivery into cells. The present invention also provides for O-malonyltryrosyl compound-containing peptides which exhibit inhibitory potency against binding interactions of receptor domains with phosphotyrosyl-containing peptide ligands.