3-HYDROXY-4-OXO-1,2,3-TRIAZINES AND DERIVATIVES THEREOF FOR AMIDE AND ESTER BOND FORMATION
    1.
    发明申请
    3-HYDROXY-4-OXO-1,2,3-TRIAZINES AND DERIVATIVES THEREOF FOR AMIDE AND ESTER BOND FORMATION 审中-公开
    3-羟基-4-氧代-1,2,3-三唑及其衍生物,用于酰胺和酯键形成

    公开(公告)号:WO2005007634A1

    公开(公告)日:2005-01-27

    申请号:PCT/IL2004/000652

    申请日:2004-07-18

    IPC分类号: C07D253/04

    摘要: The present invention relates to the use of a compound of formula I as a coupling reagent in forming amide or ester bonds from a reaction between a carboxylic acid and an amine or an alcohol, respectively. The compounds of formula I are especially useful as coupling reagents in the preparation of peptide bonds during peptide synthesis. In particular, the compounds of formula I are useful in promoting the formation of reactive reaction intermediates, inhibiting side reactions and in suppression of racemization. In addition, the present invention provides novel compounds of Formula I, and salts of N-oxides thereof.

    摘要翻译: 本发明涉及分别由羧酸和胺或醇之间的反应形成酰胺或酯键的式I化合物作为偶联剂的用途。 在肽合成期间,式I化合物特别可用作偶联试剂在制备肽键中。 特别地,式I化合物可用于促进反应中间体的形成,抑制副反应和抑制外消旋化。 此外,本发明提供新的式I化合物及其N-氧化物的盐。

    METHODS FOR THE REDUCTION OF DISULFIDE BONDS
    4.
    发明申请
    METHODS FOR THE REDUCTION OF DISULFIDE BONDS 审中-公开
    减少破坏债券的方法

    公开(公告)号:WO2004101597A3

    公开(公告)日:2005-09-09

    申请号:PCT/IL2004000392

    申请日:2004-05-10

    CPC分类号: C07K1/1133

    摘要: This invention provides a method for reducing disulfide bonds in a chemical agent, the method may include, inter alia, the step of contacting the chemical agent with 1,4-dimercapto-2,3-dihydroxybutane, wherein the 1,4-dimercapto-2,3­dihydroxybutane is prepared by a non-stereoselective reaction. This invention further provides a method for protecting a protein against oxidation, the method may include, inter alia, the step of contacting the protein with 1,4-dimercapto-2,3­dihydroxybutane, wherein the 1,4-dimercapto-2,3-dihydroxybutane is prepared by a non-stereoselective reaction. This invention further provides a method for reducing a disulfide bond in a. chemical agent, the method may include, inter alia, the step of contacting the chemical agent with a compound represented by the structure of formula (I) wherein R1, R2 and R3 are the same or different, independently of each other represent H, an unsubstituted or substituted linear, branched or cyclic hydroxyalkyl, an unsubstituted or substituted linear, branched or cyclic hydroxyalkenyl or an unsubstituted or substituted hydroxyaryl, an unsubstituted or substituted linear, branched or cyclic alkoxyalkyl ether, an unsubstituted or substituted linear, branched or cyclic alkoxy alkoxyalkyl ether, an unsubstituted or substituted linear, branched or cyclic alkylthioalkyl ether. This invention further provides a method for protecting a protein against oxidation, the method may include, inter alia, the step of contacting the protein with a compound represented by the structure of formula (I) wherein R1, R2 and R3 are the same or different, independently of each other represent H, an unsubstituted or substituted linear, branched or cyclic hydroxyalkenyl, an unsubstituted or substituted linear, branched or cyclic hydroxyalkenyl or an unsubstituted hydroxyaryl, an unsubstituted or subsituted linear, branched or cyclic alkoxyalkyl ether, an unsubstituted or substituted linear, branched or cyclic alkoxy alkoxyalkyl ether, an unsubstituted or substituted linear, branched or cyclic alkylthioalkyl ether.

    摘要翻译: 本发明提供了用于还原化学试剂中的二硫键的方法,该方法尤其可以包括使化学试剂与1,4-二巯基-2,3-二羟基丁烷接触的步骤,其中1,4-二巯基 - 2,3-二羟基丁烷是通过非立体选择性反应制备的。 本发明还提供了一种保护蛋白质免受氧化的方法,该方法尤其可包括使蛋白质与1,4-二巯基-2,3-二羟基丁烷接触的步骤,其中1,4-二巯基-2,3 - 二羟基丁烷通过非立体选择性反应制备。 本发明还提供了一种用于还原二硫键的方法。 化学试剂,该方法尤其可以包括使化学试剂与由式(I)结构表示的化合物接触的步骤,其中R 1,R 2和R 3相同或不同,彼此独立地表示H, 未取代或取代的直链,支链或环状羟基烷基,未取代或取代的直链,支链或环状羟基烯基或未取代或取代的羟基芳基,未取代或取代的直链,支链或环状烷氧基烷基醚,未取代或取代的直链,支链或环状烷氧基烷氧基烷基 醚,未取代或取代的直链,支链或环状烷硫基烷基醚。 本发明还提供了一种保护蛋白质免受氧化的方法,该方法尤其可包括使蛋白质与由式(I)结构表示的化合物接触的步骤,其中R 1,R 2和R 3相同或不同 未取代或取代的直链,支链或环状羟基烯基,未取代或取代的直链,支链或环状羟基烯基或未取代的羟基芳基,未取代或取代的直链,支链或环状烷氧基烷基醚,未取代或取代的 直链,支链或环状烷氧基烷基醚,未取代或取代的直链,支链或环状烷硫基烷基醚。

    METHODS FOR THE REDUCTION OF DISULFIDE BONDS
    7.
    发明申请
    METHODS FOR THE REDUCTION OF DISULFIDE BONDS 审中-公开
    减少破坏债券的方法

    公开(公告)号:WO2004101597A2

    公开(公告)日:2004-11-25

    申请号:PCT/IL2004/000392

    申请日:2004-05-10

    IPC分类号: C07K

    CPC分类号: C07K1/1133

    摘要: This invention provides a method for reducing disulfide bonds in a chemical agent, the method may include, inter alia, the step of contacting the chemical agent with 1,4-dimercapto-2,3-dihydroxybutane, wherein the 1,4-dimercapto-2,3­dihydroxybutane is prepared by a non-stereoselective reaction. This invention further provides a method for protecting a protein against oxidation, the method may include, inter alia, the step of contacting the protein with 1,4-dimercapto-2,3­dihydroxybutane, wherein the 1,4-dimercapto-2,3-dihydroxybutane is prepared by a non-stereoselective reaction. This invention further provides a method for reducing a disulfide bond in a. chemical agent, the method may include, inter alia, the step of contacting the chemical agent with a compound represented by the structure of formula (I) wherein R 1 , R 2 and R 3 are the same or different, independently of each other represent H, an unsubstituted or substituted linear, branched or cyclic hydroxyalkyl, an unsubstituted or substituted linear, branched or cyclic hydroxyalkenyl or an unsubstituted or substituted hydroxyaryl, an unsubstituted or substituted linear, branched or cyclic alkoxyalkyl ether, an unsubstituted or substituted linear, branched or cyclic alkoxy alkoxyalkyl ether, an unsubstituted or substituted linear, branched or cyclic alkylthioalkyl ether. This invention further provides a method for protecting a protein against oxidation, the method may include, inter alia, the step of contacting the protein with a compound represented by the structure of formula (I) wherein R 1 , R 2 and R 3 are the same or different, independently of each other represent H, an unsubstituted or substituted linear, branched or cyclic hydroxyalkenyl, an unsubstituted or substituted linear, branched or cyclic hydroxyalkenyl or an unsubstituted hydroxyaryl, an unsubstituted or subsituted linear, branched or cyclic alkoxyalkyl ether, an unsubstituted or substituted linear, branched or cyclic alkoxy alkoxyalkyl ether, an unsubstituted or substituted linear, branched or cyclic alkylthioalkyl ether.

    摘要翻译: 本发明提供了用于还原化学试剂中的二硫键的方法,该方法尤其可以包括使化学试剂与1,4-二巯基-2,3-二羟基丁烷接触的步骤,其中1,4-二巯基 - 2,3-二羟基丁烷是通过非立体选择性反应制备的。 本发明还提供了一种保护蛋白质免受氧化的方法,该方法尤其可包括使蛋白质与1,4-二巯基-2,3-二羟基丁烷接触的步骤,其中1,4-二巯基-2,3 - 二羟基丁烷通过非立体选择性反应制备。 本发明还提供了一种用于还原二硫键的方法。 化学试剂,该方法尤其可以包括使化学试剂与由式(I)结构表示的化合物接触的步骤,其中R 1,R 2和R 3相同或不同,彼此独立地表示H, 未取代或取代的直链,支链或环状羟基烷基,未取代或取代的直链,支链或环状羟基烯基或未取代或取代的羟基芳基,未取代或取代的直链,支链或环状烷氧基烷基醚,未取代或取代的直链,支链或环状烷氧基烷氧基烷基 醚,未取代或取代的直链,支链或环状烷硫基烷基醚。 本发明还提供了一种保护蛋白质免受氧化的方法,该方法尤其可包括使蛋白质与由式(I)结构表示的化合物接触的步骤,其中R 1,R 2和R 3相同或不同 未取代或取代的直链,支链或环状羟基烯基,未取代或取代的直链,支链或环状羟基烯基或未取代的羟基芳基,未取代或取代的直链,支链或环状烷氧基烷基醚,未取代或取代的 直链,支链或环状烷氧基烷基醚,未取代或取代的直链,支链或环状烷硫基烷基醚。