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    • 6. 发明授权
    • Process for the preparation of polypeptide 1
    • 多肽1的制备方法
    • US07049399B2
    • 2006-05-23
    • US10326994
    • 2002-12-24
    • Elena BejanGamini WeeratungaStephen E. Horne
    • Elena BejanGamini WeeratungaStephen E. Horne
    • C07K1/00C07K2/00
    • C07K14/001A61K38/00C07K14/195
    • A process for the preparation of a polypeptide designated in the present invention as 1, composed of the following amino acid units in the structure, namely: L-alanine, L-glutamic acid, L-lysine and L-tyrosine randomly arranged in the polypeptide 1, or pharmaceutically acceptable salts thereof, comprising the steps of: (a) polymerization of a mixture of the N-carboxyanhydrides of L-alanine, L-tyrosine, a protected L-glutamate and a protected L-lysine to obtain protected copolymer 6 or salt thereof; (b) deprotection of the protected copolymer 6 (or salt thereof) to produce polypeptide 1 or a pharmaceutically acceptable salt thereof in one single step; (c) separation and purification of the polypeptide 1 (or a pharmaceutically acceptable salt) to obtain a purified polypeptide 1
    • 制备本发明中指定的多肽的方法为1,由以下结构中的氨基酸单元组成,即随机排列在多肽中的L-丙氨酸,L-谷氨酸,L-赖氨酸和L-酪氨酸 1或其药学上可接受的盐,包括以下步骤:(a)将L-丙氨酸,L-酪氨酸,受保护的L-谷氨酸和受保护的L-赖氨酸的N-羧酸酐的混合物聚合,得到被保护的共聚物6 或其盐; (b)在一个单一步骤中保护的共聚物6(或其盐)去保护以产生多肽1或其药学上可接受的盐; (c)分离和纯化多肽1(或其药学上可接受的盐)以获得纯化的多肽1
    • 10. 发明授权
    • Process for the preparation of tetrahydrothieno[3,2-c] pyridine derivatives
    • 四氢噻吩并[3,2-c]吡啶衍生物的制备方法
    • US07060831B2
    • 2006-06-13
    • US10774506
    • 2004-02-10
    • Robert P. SmyjGamini Weeratunga
    • Robert P. SmyjGamini Weeratunga
    • C07D471/02C07F7/04C07F7/08
    • C07D495/04
    • A process for the preparation of tetrahydrothieno[3,2-c]pyridine compound of formula 6: or their pharmaceutically acceptable salts, wherein the meaning of X is carboxyl, alkoxycarbonyl, aryloxycarbonyl, or carbamoyl of formula wherein R1 and R2 can be individually or simultaneously hydrogen, alkyl or part of a heterocyclic structure; Z can be hydrogen, halogen, alkyl, aryl, aryloxy or alkoxy group, the process comprising conducting a dehydroxylation reaction on the compound of formula 5 in order to obtain a compound of formula 6, wherein said dehydroxylation reaction is effected by iodosilane represented by the formula Si(R3)3I, wherein R3 selected from an alkyl, alkenyl, alkynyl, aromatic group, or combinations of thereof
    • 制备式6的四氢噻吩并[3,2-c]吡啶化合物或其药学上可接受的盐的方法,其中X的含义是羧基,烷氧基羰基,芳氧基羰基或下式的氨基甲酰基,其中R 1, SUB和R 2可以单独或同时地氢,烷基或部分杂环结构; Z可以是氢,卤素,烷基,芳基,芳氧基或烷氧基,该方法包括对式5化合物进行脱羟基化反应,以获得式6化合物,其中所述脱羟基化反应是由 其中R 3选自烷基,烯基,炔基,芳族基团或其组合的式(Ⅺ)3Ⅺ