CAS: 653-03-2; 1-[10-[3-(4-Methylpiperazin-1-yl)Propyl]Phenothiazin-2-Yl]Butan-1-One

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CAS号1063-55-4 bis[1-[3-[2-(1-...

📜N-甲基哌嗪,在 Sodium Hydride体系中,用 二甲基亚砜 作为反应溶剂,化学反应 13.0H,反应生成 布他哌嗪
参考文献:作为 Mdr 逆转剂的新型吩噻嗪和相关药物的合成和生化表征
标题:作为 Mdr 逆转剂的新型吩噻嗪和相关药物的合成和生化表征
摘要:化疗是治疗癌症最重要的方法之一.然而,化疗期间耐药性的发展是癌症患者治疗失败和生存率下降的主要原因.多药耐药 (Mdr) 是 30 多年来广泛研究的耐药形式之一.atp 结合盒蛋白家族的成员负责以 P-糖蛋白作为最具代表性的转运蛋白的多药耐药性.为了克服多药耐药性,外排泵抑制剂对转运蛋白的药理学调节似乎是首选,但临床前研究并未导致临床应用.因此,对药效基团结构进行系统研究是提高那些仍影响多药耐药性的药物疗效的有前途的策略.在这项研究中,一系列吩噻嗪衍生物合成了三个分子结构域的系统变异.多药耐药逆转活性的生化测定是通过对 Llc-Pk1/mdr1 细胞的结晶紫测定实现的.将考虑文献中关于新的结构-活性关系以克服未来耐药性的假设来讨论结果.
DOI:10.1002/ardp.200800115

专利信息

专利号:US-9617230-B2
优先权日:2014-12-22
标题:Creatine prodrugs, compositions and methods of use thereof
发明人：BRUBAKER WILLIAM F
权利人:FARMINGTON PHARMA DEV
摘要:The invention describes membrane permeable creatine prodrugs, pharmaceutical compositions comprising membrane permeable creatine prodrugs, and methods of treating diseases such as ischemia, heart failure, neurodegenerative disorders and genetic disorders affecting the creatine kinase system comprising administering creatine prodrugs or pharmaceutical compositions thereof. The invention also describes treating a genetic disease affecting the creatine kinase system, such as, for example, a creatine transporter disorder or a creatine synthesis disorder comprising administering creatine prodrugs or pharmaceutical compositions thereof.

专利号:US-11021501-B2
优先权日:2015-03-30
标题:Creatine phosphate analog prodrugs, compositions and methods of use thereof
发明人：BRUBAKER WILLIAM F
权利人:FARMINGTON PHARMA DEV
摘要:The invention describes membrane permeable creatine phosphate analog prodrugs, pharmaceutical compositions comprising membrane permeable creatine phosphate analog prodrugs, and methods of treating diseases such as ischemia, heart failure, neurodegenerative disorders and genetic disorders affecting the creatine kinase system comprising administering creatine phosphate analog prodrugs or pharmaceutical compositions thereof. The invention also describes treating a genetic disease affecting the creatine kinase system, such as, for example, a creatine transporter disorder or a creatine synthesis disorder comprising administering creatine phosphate analog prodrugs or pharmaceutical compositions thereof.

专利号:US-2005053642-A1
优先权日:2000-08-23
标题:Biocompatible materials
发明人：ULBRICHT MATHIAS; THOM VOLKMAR; JANKOVA KATJA; ALTANKOV GEORGE; JONSSON GUNNAR
摘要:The present invention teaches a novel approach of creating biocmpatible surfaces, said surfaces being capable of functionally interact with biological material. SAid biocompatible surfaces comrise at least two comonents, such as a hydrophobic substratum and a macromolecule of hydrophilic nature, which, in a cooperativity, form together the novel biocoompatible surfaces. The novel approach is ased on contacting said hydrophobic substratum with a laterally patterned monomolecular layer of said hydrophilic and flexible macromolecules, exhibiting a pronounced excluded volume. The htus formed two component surface is, in respect to polarity and morphology, a molecularly heterogeneous surface. Structural features of said macromolecular monolayer (as e.g. the layer thickness or its lateral density) are determined by: i) the structural features of the layer forming macromolecules (as e.g. their MW or their molecular architecture) and ii) the method of creating said monomolecular layer (as e.g. by physi- or chemisorbing, or by chemically binding said macromolecules). The structural features of the layer forming macromolecules(s) is in turn determined by synthesis. AMount and conformation and thus also biological activity of biological material (as e.g. polypeptides) which contact the novel biocompatible surface, is determined and maintained by the cooperative action of the underlying hydrophobic substratum and the macromolecular layer. In this way it becomes possible to maintain and control biological interactions between said contacted polypeptides and other biological compounds as e.g. cells, antibodies and the like. Consequently, the present invention aims to reduce and/or eliminate the deactivation and/or denaturation associated with the contacting of polypeptides and/or other biological material to a hydrophobic substratum surface.

专利号:WO-2025118034-A1
优先权日:2023-12-06
标题 :Compounds active at the serotonergic 5-ht2a receptor
发明人：JORGENSON WILLIAM; TAN JINLONG; WHISH LACHLAN; BANISTER SAMUEL
权利人:Psylo Pty Ltd
摘要:The present disclosure relates to compounds of formula (I), their methods of synthesis, and their use in the treatment of mental illness or central nervous system disorders.

专利号:WO-2023230649-A1
优先权日:2022-05-30
标题:Compounds
发明人：BANISTER SAMUEL; JORGENSEN WILLIAM; TAN JINLONG; WHISH LACHLAN
权利人:Psylo Pty Ltd
摘要:The present disclosure relates to compounds of formula (I), their methods of synthesis, and their use in the treatment of mental illness or central nervous system disorders.

专利号:US-2014315720-A1
优先权日:2012-10-24
标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
发明人：FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
权利人:CELANESE ACETATE LLC
摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.