CAS: 125317-39-7; Methyl (3Ar,3A1R,4R,5S,5Ar,10Br)-4-Acetoxy-3A-Ethyl-9-((8R)-4-Ethyl-8-(Methoxycarbonyl)-1,3,6,7,8,9-Hexahydro-2,6-Methanoazecino[4,3-B]Indol-8-yl)-5-Hydroxy-8-Methoxy-6-Methyl-3A,3A1,4,5,5A,6,11,12-Octahydro-1H-Indolizino[8,1-Cd]Carbazole-5-Carboxylate Bi

专利信息

专利号:US-5220016-A
优先权日:1991-07-29
标 题:Synthesis of navelbine analogs
发明人：MAGNUS PHILIP D; THURSTON LEE S
权利人:UNIV TEXAS
摘要:The invention is a de novo synthesis of the norcatharanthine moiety of navelbine. The synthesis includes condensing a Grignard reagent prepared from an amine-protected R(+)-piperidinyl methanol with an N-protected 2-methoxyoxalyl indole. The indole N-protecting group is removed to provide a 2-methoxyindole hydroxy ester which is coupled to vindoline. After removal of the amineprotecting group from the piperidinyl group, ring closure to the indole moiety provides dihydrodesethyl navelbine. Other derivatives and analogs of navelbine with potential clinical applications in cancer chemotherapy may be readily synthesized. The synthesis opens a route to a wide variety of navelbine modifications, including modifications at or near the tryptamine bridge.

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-2017283878-A1
优先权日:2015-12-11
标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
权利人:ACADEMIA SINICA
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

专利号:US-2024173256-A1
优先权日:2022-11-29
标 题:Hdl mimicking targeted drug delivery system for the treatment of solid tumors
发明人：SABNIS NIRUPAMA; LACKO ANDRAS; FUDALA RAFAL
权利人:UNIV OF NORTH TEXAS HEALTH SCIENCE CENTER
摘要:The present disclosure is directed to an SR-B1-targeting nanomicelle and compositions, methods of synthesis and methods of use thereof. The nanomicelle may be an HDL-mimetic drug delivery system and may be cross-linked with DSS. The composition may contain a therapeutic agent with the ability to treat cancers, especially sarcomas.

专利号:US-2016318862-A1
优先权日:2013-09-25
标 题:Synthesis of delta 12-pgj3 and related compounds
发明人：NICOLAOU KYRIACOS C; HERETSCH PHILIPP; HALE CHRISTOPHER R H; EL GHZAOUI ABDELLATIF EL MARROUNI; PULUKURI KIRAN KUMAR; YU RUOCHENG; GROVE CHARLES
权利人:UNIV RICE WILLIAM M
摘要:In one aspect, the present invention provides novel derivatives of Δ 12 -PGJ 3 and modular synthetic pathways to obtaining Δ 12 -PGJ 3 and derivatives thereof. In some aspects, the present derivatives of Δ 12 -PGJ 3 are useful as chemotherapeutic agents. The present disclosure also describes compositions of these derivatives as well as methods of use of the derivatives thereof.

专利号:US-8147805-B2
优先权日:2005-01-05
标题:Conjugates for dual imaging and radiochemotherapy: composition, manufacturing, and applications
发明人：YANG DAVID; YU DONGFANG; CHANDA MITHU; AZHDARINIA ALI; OH CHANGSOK; KIM E EDMUND
权利人:YANG DAVID; YU DONGFANG; CHANDA MITHU; AZHDARINIA ALI; OH CHANGSOK; KIM E EDMUND; UNIV T EXAS SYSTEM BOARD OF REGENTS
摘要:Compositions and methods for dual imaging and for dual chemotherapy and radiotherapy are disclosed. More particularly, the invention concerns compounds comprising the structure X 1 —Y—X 2 , wherein Y comprises two or more carbohydrate residues covalently attached to one another, X 1 and X 2 are diagnostic or therapeutic moieties covalently attached to Y, provided that when Y does not comprise a glucosamine residue, X 1 and X 2 are diagnostic moieties. The present invention also concerns methods of synthesis of these compounds, application of such compounds for dual imaging and treatment of hyperproliferative disease, and kits for preparing a radiolabeled therapeutic or diagnostic compound.