CAS: 1438-30-8; Netropsin

专利信息

专利号:US-6683189-B1
优先权日:1996-02-26
标 题 :Method for the synthesis of pyrrole and imidazole carboxamides on a solid support
发明人：DERVAN PETER B; BAIRD ELDON
权利人:CALIFORNIA INST OF TECHN
摘要:The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.

专利号:EP-3378556-A1
优先权日:2017-03-20
标题 :Method for the preparation of a low unspecific binding-support for affinity chromatography and/or on-line synthesis of oligonucleotides
发明人：PLATELLA CHIARA; MUSUMECI DOMENICA; AMATO JUSSARA; RANDAZZO ANTONIO; PAGANO BRUNO; MONTESARCHIO DANIELA
权利人:PLATELLA CHIARA; MUSUMECI DOMENICA; AMATO JUSSARA; RANDAZZO ANTONIO; PAGANO BRUNO; MONTESARCHIO DANIELA
摘要:A method for preparing functionalized solid supports to be used in the on-line synthesis of support-bound, fully deprotected secondary structure-forming oligonucleotides and/or for low unspecific binding affinity chromatography is disclosed.

专利号:US-7157477-B2
优先权日:2000-10-25
标题 :Aliphatic amino-substituted demethoxylated hypocrellins and their synthesis
发明人：ZHANG MANHUA; XU SHANGJIE; WU TAO; CHEN SHEN; SHEN TAO
权利人:INST OF PHOTOGRAPHIC CHEMISTRY
摘要:The invention involves a methods and compositions for use in photodynamic therapy. Novel perylenequinone derivatives, conjugates comprising perylenequinone derivatives and a binding agent, and methods of treatment using these compositions are disclosed. The present invention relates to the field of photosensitizers possessing photodynamic activities. They possess high photodynamic activities and low dark toxicities, which makes them as more potent photodynamic agents than HPD against cancer and AIDS virus.

专利号:WO-9741109-A1
优先权日:1996-04-26
标 题 :Synthesis of (±) - calicheamicinone, precursors, intermediates and derivatives
发明人：CLIVE DERRICK L J; DAIGNEAULT SYLVAIN; BO YUNXIN; TAO YONG
权利人:UNIV ALBERTA; CLIVE DERRICK L J; DAIGNEAULT SYLVAIN; BO YUNXIN; TAO YONG
摘要:This invention relates to calicheamicinone and related compounds, and processes for the preparation of these compounds and derivatives or analogs thereof. Many of the products that can be synthesized using these compounds have antibiotic activity including, but not limited to, anticancer, antifungal or antimicrobial activity.

专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人：MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

专利号:US-7579167-B2
优先权日:2002-10-08
标题:Polypeptides involved in the biosynthesis of spiramycins, nucleotide sequences encoding these polypeptides and applications thereof
发明人：BLONDELET-ROUAULT MARIE-HELENE; DOMINGUEZ HELENE; DARBON-RONGERE EMMANUELLE; GERBAUD CLAUDE; GONDRAN ANNE; KARRAY FATMA; LACROIX PATRICIA; OESTREICHER-MERMET-BOUVIER NATHALIE; JEAN-LUC PERNODET; TUPHILE KARINE
权利人:AVENTIS PHARMA S; CENTRE NAT RECH SCIENT
摘要:The present invention relates to the isolation and identification of novel genes of the biosynthetic pathway for spiramycins and to novel polypeptides involved in this biosynthesis. The invention also relates to a method for producing these polypeptides. It also relates to the use of these genes for the purpose of increasing the levels of production and the purity of the spiramycin produced. The invention relates in particular to a microorganism which produces spiramycin I but which does not produce spiramycin II and III, and to the use of such a microorganism. The invention also relates to the use of the genes of the biosynthetic pathway for spiramycins for constructing mutants which can lead to the synthesis of novel antibiotics or to derived forms of spiramycins. The invention also relates to the molecules produced through the expression of these genes and to pharmacologically active compositions of a molecule produced through the expression of such genes.