CAS: 897016-82-9; N-Benzyl-2-(5-(4-(2-Morpholinoethoxy)Phenyl)Pyridin-2-yl)Acetamide

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CAS号1038395-64-0 methyl 2-[5-[4-... | CAS号100-46-9 苄胺

📜4-(2-吗啉乙氧基)苯基硼酸频哪醇酯置于四(三苯基膦)钯,硫酸,Sodium Hexamethyldisilazane体系中,化学反应生成 Kx 01; 5-[4-[2-(4-吗啉基)乙氧基]苯基]-N-(苯基甲基)-2-吡啶乙酰胺
参考文献:发现新的双重作用机制 Src 信号和微管蛋白聚合抑制剂(kx2-391 和 Kx2-361)
标题:发现新的双重作用机制 Src 信号和微管蛋白聚合抑制剂(kx2-391 和 Kx2-361)
摘要:发现有效的肽定点酪氨酸激酶抑制剂仍然是一个难以实现的目标.在本文中,我们描述了两种抑制酪氨酸激酶 Src 的临床候选药物的发现.化合物1是 3 期临床试验候选药物,与现有标准疗法相比,它可能为光化性角化病 (Ak) 提供一流的局部治疗,具有非常好的疗效和显着更低的毒性.化合物2是一项 1 期临床试验候选药物,可能为恶性胶质母细胞瘤提供一流的治疗,并在动物模型中诱导 30% 的长期肿瘤完全缓解.这些化合物的发现策略反复利用分子建模,以及越来越详细的概念化合物证明的合成和测试,直到得出最终的临床候选药物.随后进行的作用机制 (Moa) 研究表明,微管蛋白聚合抑制是第二个 Moa.
DOI:10.1021/acs.Jmedchem.8B00164

专利信息

专利号:EP-4186890-A1
优先权日:2021-11-29
标题 :Preparation of n-benzyl-2-(5-bromo-pyridin-2-yl)-acetamide for the synthesis of tirbanibulin
发明人：ARE CELESTE; BALLETTE ROBERTO; DOBARRO RODRÃ?GUEZ ALICIA
权利人:MOEHS IBERICA SL
摘要:The present invention relates to a process for the preparation of N-benzyl-2-(5-bromo-pyridin-2-yl)-acetamide, which is a suitable intermediate for the synthesis of tirbanibulin or a pharmaceutically acceptable salt thereof, as well as to a process for the preparation of tirbanibulin or a pharmaceutically acceptable salt thereof using said N-benzyl-2-(5-bromo-pyridin-2-yl)-acetamide intermediate.

专利号:US-2024343691-A1
优先权日:2006-12-28
标题:Compositions for modulating a kinase cascade and methods of use thereof
发明人：HANGAUER JR DAVID G; PATRA DEBASIS; CODY JEREMY A; PALMER GRANT J; ISBESTER PAUL K; SALSBURY JONATHON
权利人:ATNX SPV LLC
摘要:The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl) pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.

专利号:US-8293739-B2
优先权日:2006-12-28
标题:Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof
发明人：HANGAUER JR DAVID G; COUGHLIN DANIEL; GALE JONATHAN; CODY JEREMY A; PATRA DEBASIS; PALMER GRANT J; ISBESTER PAUL K; SALSBURY JONATHON
权利人:HANGAUER JR DAVID G; COUGHLIN DANIEL; GALE JONATHAN; CODY JEREMY A; PATRA DEBASIS; PALMER GRANT J; ISBESTER PAUL K; SALSBURY JONATHON; KINEX PHARMACEUTICALS LLC
摘要:The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. More specifically, the invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy) phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention.

专利号:US-9556120-B2
优先权日:2006-12-28
标题:Compositions for modulating a kinase cascade and methods of use thereof
发明人：HANGAUER JR DAVID G; PATRA DEBASIS; CODY JEREMY A; PALMER GRANT J; ISBESTER PAUL K; SALSBURY JONATHON
权利人:ATHENEX INC
摘要:The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxyl)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxyl)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxyl)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.

专利号:US-12390420-B1
优先权日:2024-10-22
标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof
发明人：EGUCHI MASAKATSU
权利人:BRYET US INC
摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.

专利号:WO-2024008625-A1
优先权日:2022-07-04
标 题:Procedure for the synthesis of tirbanibulin