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    • 15. 发明申请
    • Processes for Preparing a Polypeptide
    • 制备多肽的方法
    • US20100234566A1
    • 2010-09-16
    • US12727653
    • 2010-03-19
    • Anup Kumar RayHiren Kumar V. PatelJohannes LudescherMariappan AnbazhaganMahendra R. PatelIngolf Macher
    • Anup Kumar RayHiren Kumar V. PatelJohannes LudescherMariappan AnbazhaganMahendra R. PatelIngolf Macher
    • C07K1/08
    • C08G69/10A61K38/00C07K14/001
    • The present invention relates to an improved process for preparing a polypeptide or pharmaceutically acceptable salt thereof comprising L-tyrosine, L-alanine, L-glutamate, and L-lysine. The polypeptide or pharmaceutically acceptable salt thereof is preferably glatiramer acetate. The process comprises: (a) polymerizing a mixture of N-carboxyanhydride of L-tyrosine, N-carboxyanhydride of L-alanine, N-carboxyanhydride of a protected L-glutamate and N-carboxyanhydride of a protected L-lysine, in a polar aprotic solvent in the presence of an initiator, to form a protected polypeptide; (b) admixing an acid with the protected polypeptide formed in Step (a) and a solvent, to form a product; and (c) admixing a substance selected from the group consisting of an alkali or alkaline earth metal hydroxide, a carbonate, a hydrogencarbonate, and mixtures thereof, with the product formed in Step (b), and a solvent or a mixture of a solvent and water, to form a deprotected polypeptide or a pharmaceuticaly acceptable salt thereof.
    • 本发明涉及制备包含L-酪氨酸,L-丙氨酸,L-谷氨酸和L-赖氨酸的多肽或其药学上可接受的盐的改进方法。 多肽或其药学上可接受的盐优选为醋酸格拉司他。 该方法包括:(a)将L-酪氨酸的N-羧酸酐,L-丙氨酸的N-羧酸酐,受保护的L-谷氨酸的N-羧酸酐和受保护的L-赖氨酸的N-羧酸酐的极性 在引发剂存在下的非质子溶剂,以形成受保护的多肽; (b)将酸与步骤(a)中形成的被保护的多肽和溶剂混合以形成产物; 和(c)将选自碱金属或碱土金属氢氧化物,碳酸盐,碳酸氢盐及其混合物的物质与步骤(b)中形成的产物和溶剂或溶剂的混合物 和水,以形成去保护的多肽或其药学上可接受的盐。
    • 17. 发明授权
    • Novel bendroflumethiazide formulations and method
    • 新型弯甲氟噻嗪配方及方法
    • US4304773A
    • 1981-12-08
    • US163128
    • 1980-06-26
    • Thomas M. WongMahendra R. Patel
    • Thomas M. WongMahendra R. Patel
    • A61K9/20A61K31/54A61K47/00
    • A61K31/54A61K9/2004
    • New bendroflumethiazide formulations in solid form are provided which are characterized by excellent disintegration and dissolution capabilities even after long periods of storage. The new bendroflumethiazide formulations, for example, in the form of tablets, contain in addition to bendroflumethiazide, a combination of microcrystalline cellulose which serves as a diluent and aids in disintegration of the tablets, lactose which serves as a diluent, optionally starch (in the gelatinized form) which serves as a disintegrant, and one or more auxilliary disintegrants, such as sodium carboxymethyl starch, a tablet lubricant, such as magnesium stearate, and a colorant, if desired.A method for preparing the above formulations is also provided.
    • 提供固体形式的新的四氟嘧啶配方,其特征在于即使在长时间储存​​后也具有优异的崩解和溶解能力。 新的四氟嘧磺隆配方,例如以片剂的形式,除了含有四氟嘧啶以外,还含有作为稀释剂的微晶纤维素的组合,有助于片剂的崩解,用作稀释剂的乳糖,任选的淀粉(在 用作崩解剂的一种或多种辅助崩解剂,如羧甲基淀粉钠,片剂润滑剂如硬脂酸镁和着色剂。 还提供了制备上述配方的方法。