CAS: 132036-88-5; (1-Methylindol-3-yl)-[(5R)-4,5,6,7-Tetrahydro-3H-Benzimidazol-5-Yl]Methanone

上下游产品

5-[(1-甲基吲哚-3-基)羰基]-4,5,6,7-四氢苯并咪唑 Ramosetron 132036-39-6

📜5-[(1-甲基吲哚-3-基)羰基]-4,5,6,7-四氢苯并咪唑置于(+)-2,3-Dibenzoyl-D-Tartaric Acid体系中,用 甲醇 用作溶剂,以62.71%的收率获得拉莫司琼
参考文献:一种雷莫司琼的合成方法
标题:一种雷莫司琼的合成方法
摘要:本发明公开了一种雷莫司琼的合成方法,以3,4-二氨基苯甲酸为起始原料,经过合成苯并咪唑-5-羧酸,苯并咪唑-5-羧酸甲酯硫酸盐,4,5,6,7-四氢苯并咪唑-5-羧酸甲酯硫酸盐,4,5,6,7-四氢苯并咪唑-5-羧酸硫酸盐,N-[(4,5,6,7-四氢苯并咪唑-5-基)]吡咯盐酸盐,5-[(1-甲基吲哚-3-基)羰基]-4,5,6,7-四氢苯并咪唑最终制成雷莫司琼.本发明的发明方法与现有技术相比优化了反应条件,优化后反应确实可行,提高4,5,6,7-四氢苯并咪唑-5-羧酸硫酸盐,N-[(4,5,6,7-四氢苯并咪唑-5-基)]吡咯盐酸盐等的收率,反应总收率达到30%以上,具有较高的经济效益.

专利信息

专利号:US-8734846-B2
优先权日:2008-06-16
标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
发明人：ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
权利人:BIND BIOSCIENCES INC
摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

专利号:US-2013035307-A1
优先权日:2010-01-26
标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
发明人：PRESTWICH GLENN D; KENNEDY THOMAS P
权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

专利号:US-2008214827-A1
优先权日:2004-02-03
标 题:Synthesis of Cyanoimino-Benzoimidazoles
发明人：GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
权利人:EURO CELTIQUE SA
摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

专利号:US-9220714-B2
优先权日:2006-03-16
标 题 :Nitrofuran compounds for the treatment of cancer and angiogenesis
发明人：SAULNIER SHOLLER GISELLE L; SWAMY NARASIMHA; KALKUNTE STAYAN; SINGH RAKESH K; BRARD LAURENT; KIM KYU KWANG
权利人:WOMEN AND INFANTS HOSPITAL OF RHODE ISLAND; UNIV BROWN; WOMEN AND INFANTS HOSPITAL RHODE ISLAND
摘要:The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.

专利号:US-2022118123-A1
优先权日:2019-02-22
标 题 :Combination of ar antagonists and targeted thorium conjugates
发明人：HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY
权利人:BAYER AG; BAYER AS
摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.

专利号:US-2024382626-A1
优先权日:2023-05-16
标题 :Irradiation amenable liposomal dye aggregates and methods of synthesis and use thereof
发明人：PORTER TYRONE; STERN NOAH; TUNNELL JAMES; SHRESTHA BINITA
权利人:UNIV TEXAS
摘要:The present invention provides lipid nanoparticles that are amenable to an irradiation at a wavelength at or above 850 nm, have an absorption peak from about 850 to 1100 nm wavelength, and comprise a high transition temperature lipid and a dye (e.g., a J-aggregate of a dye). In some embodiments, the dye (e.g., J-aggregate of the dye) is encapsulated in the lipid nanoparticle. In various embodiments, the present invention also relates to compositions comprising said lipid nanoparticles and methods of generating said lipid nanoparticles and compositions thereof. The present invention further relates to methods relating to the said lipid nanoparticles for imaging, detection, and treatment of diseases or disorders (e.g., phototherapy) in a subject.