📜(1S)-2-氯-1-(3-氯苯基)乙醇置于盐酸,氨体系中,用 1,4-二氧六环,甲醇,水 作为反应溶剂,化学反应 120.0H,反应生成 胰岛素样生长因子-1 受体拮抗剂 参考文献:Discovery Of A 1H-Benzoimidazol-2-yl)-1H-Pyridin-2-One (Bms-536924) Inhibitor Of Insulin-Like Growth Factor I Receptor Kinase With In Vivo Antitumor Activity 标题:Discovery Of A 1H-Benzoimidazol-2-yl)-1H-Pyridin-2-One (Bms-536924) Inhibitor Of Insulin-Like Growth Factor I Receptor Kinase With In Vivo Antitumor Activity 摘要:Compound 3 (Bms-536924),A Novel Small-Molecule Inhibitor Of The Insulin-Like Growth Factor Receptor Kinase With Equal Potency Against The Insulin Receptor Is Described. The In Vitro And In Vivo Biological Activity Of This Interesting Compound Is Also Reported. DOI:10.1021/jm050392Q
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 from†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 to†that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonal†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 (“SAGEs†). 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-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.
专利号:US-2008281105-A1 优先权日:2005-01-18 标题:Novel Quinolinium Salts and Derivatives 发明人:MACDONALD JAMES E; HYSELL MICHELLE K; YU DEHUA; LI HENRY; WONG-STAAL FLOSSIE 权利人:IMMUSOL INC 摘要:The present invention relates generally to the synthesis of novel quinolinium salts and derivative compounds. Such salts and compounds are useful for inhibiting the growth of cancer cells.
专利号:CA-2555219-A1 优先权日:2004-02-03 标 题 :Synthesis of cyanoimino-benzoimidazoles
1: Velaparthi U, Saulnier MG, Wittman MD, Liu P, Frennesson DB, Zimmermann K, Carboni JM, Gottardis M, Li A, Greer A, Clarke W, Yang Z, Menard K, Lee FY, Trainor G, Vyas D. Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2- one. Bioorg Med Chem Lett. 2010 May 15;20(10):3182-5. Epub 2010 Mar 27. Epub 2010 Jan 12. Epub 2009 Sep 29. 4: Beauchamp MC, Knafo A, Yasmeen A, Carboni JM, Gottardis MM, Pollak MN, Gotlieb WH. BMS-536924 sensitizes human epithelial ovarian cancer cells to the PARP inhibitor, 3-aminobenzamide. Gynecol Oncol. 2009 Nov;115(2):193-8. Epub 2009 Aug 21. Epub 2009 Mar 3. Review. Chinese. 8: Huang F, Greer A, Hurlburt W, Han X, Hafezi R, Wittenberg GM, Reeves K, Chen J, Robinson D, Li A, Lee FY, Gottardis MM, Clark E, Helman L, Attar RM, Dongre A, Carboni JM. The mechanisms of differential sensitivity to an insulin-like growth factor-1 receptor inhibitor (BMS-536924) and rationale for combining with EGFR/HER2 inhibitors. Cancer Res. 2009 Jan 1;69(1):161-70. Epub 2008 Sep 2.
合成参考文献
参考文献:10.1016/j.bmcl.2010.01.087 摘要:Zimmermann K, Wittman MD, Saulnier MG, Velaparthi U, Sang X, Frennesson DB, Struzynski C, Seitz SP, He L, Carboni JM, Li A, Greer AF, Gottardis M, Attar RM, Yang Z, Balimane P, Discenza LN, Lee FY, Sinz M, Kim S, Vyas D. SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors. Bioorganic & Medicinal Chemistry Letters. 2010 Mar;20(5):1744–8. doi: 10.1016/j.bmcl.2010.01.087.