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    Use of diamino ketones as analgesic agents
    4.
    发明授权
    Use of diamino ketones as analgesic agents 失效
    使用二氨基酮作为止痛剂

    公开(公告)号：US4594188A

    公开(公告)日：1986-06-10

    申请号：US735924

    申请日：1985-05-20

    Applicant: Norma G. Delaney ,  Eric M. Gordon

    Inventor： Norma G. Delaney ,  Eric M. Gordon

    IPC: A61K38/00 ,  C07K5/065 ,  C07K7/02 ,  C07K5/06 ,  C07C61/08 ,  C07C69/74 ,  C07C101/00 ,  C07C101/02 ,  C07C101/24 ,  C07C101/26 ,  C07C101/42 ,  C07C109/10 ,  C07C147/02 ,  C07C149/20 ,  C07C149/243 ,  C07C149/40 ,  C07C149/43

    CPC classification number: C07K7/02 ,  C07K5/06078 ,  A61K38/00

    Abstract: An enkephalin-degrading aminopentidase enzyme is inhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl, carboxyalkyl, halo substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl, or heteroaryl;R.sub.3 is hydroxy, alkoxy, (substituted alkyl)oxy, arylalkoxy, (heteroaryl)alkoxy or --NY.sub.1 Y.sub.2, wherein Y.sub.1 and Y.sub.2 are each independently hydrogen, alkyl, aryl, or arylalkyl or Y.sub.1 is hydrogen and Y.sub.2 is substituted alkyl or (heteroaryl)alkyl;A.sub.1 is glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, prolyl, norleucyl, norvalyl, or ##STR2## wherein n.sub.6 is an integer of 2 to 15; A.sub.2, A.sub.3, A.sub.4 and A.sub.5 each is independently glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, or prolyl, norleucyl, or norvalyl; andn.sub.1, n.sub.2, n.sub.3, n.sub.4 and n.sub.5 each is independently 0 or 1.

    Abstract translation: 脑啡肽降解氨基肽酶被具有式（IMAGE）+ TR（A2）n2（A3）n3（A4）n4（A5）n5R3的化合物及其药学上可接受的盐抑制，其中R 1和R 2各自独立地为氢， 烷基，羧基烷基，卤素取代的烷基，羟基烷基，氨基烷基，巯基烷基，烷硫基烷基，（环烷基）烷基，（杂芳基）烷基，芳基烷基，氨基甲酰基烷基，胍基烷基或杂芳基; R3是羟基，烷氧基，（取代的烷基）氧基，芳基烷氧基，（杂芳基）烷氧基或-NY1Y2，其中Y1和Y2各自独立地是氢，烷基，芳基或芳烷基或Y1是氢，Y2是取代的烷基或（杂芳基） 烷基; A1是甘氨酰基，丙氨酰基，亮氨酰基，苯丙氨酰，精氨酰，肌氨酰，丝氨酰，天冬酰胺基，赖氨酰，谷氨酰，组氨酸，色氨酸，半胱氨酰，甲硫氨酰，苏氨酰，酪氨酰，亮氨酰，缬氨酰，天冬氨酰，脯氨酰， 其中n6为2至15的整数; A2，A3，A4和A5各自独立地是甘氨酰，丙氨酰，亮氨酰，苯丙氨酰，精氨酰，肌氨酰，丝氨酰，天冬酰胺酰基，赖氨酰，谷氨酰，组氨酸，色氨酰，半胱氨酰，甲硫氨酰，苏氨酰，酪氨酰，亮氨酰，缬氨酰，天冬氨酰或脯氨酰 ，正亮酰基或诺瓦尔基; n1，n2，n3，n4和n5各自独立地为0或1。

    Ampholyte and its use in separation processes
    7.
    发明授权
    Ampholyte and its use in separation processes 失效
    两性电解质及其在分离过程中的应用

    公开(公告)号：US4334972A

    公开(公告)日：1982-06-15

    申请号：US199232

    申请日：1980-10-21

    Applicant: John L. Soderberg

    Inventor： John L. Soderberg

    IPC: C09K3/00 ,  C07C67/00 ,  C07C213/00 ,  C07C215/06 ,  C07C227/00 ,  C07C227/08 ,  C07C227/18 ,  C07C229/02 ,  C07D233/54 ,  C07D233/64 ,  C07K5/04 ,  G01N27/26 ,  G01N27/447 ,  B01D57/02 ,  C07C101/00

    CPC classification number: C07D233/64 ,  G01N27/44747 ,  G01N27/44795

    Abstract: A water-soluble ampholyte which comprises the reaction product between(a) one or more compounds selected from the group comprising certain amino-acids, hydroxylamine, an amine of the formula ##STR1## wherein R.sub.1 is hydrogen, the group H.sub.2 N--(CH.sub.2).sub.n --, wherein n is an integer 2-6, or the group H.sub.2 N--(CH.sub.2).sub.3 --NH--(CH.sub.2).sub.3 --, R.sub.2 and R.sub.3 are the same or different and each representing hydrogen, methyl, ethyl or hydroxyethyl or together with the intermediate nitrogen atom form certain heterocyclic groups, and certain di- and tripeptides, at least one of these compounds being one which contains at least one carboxyl group, or salts of the aforementioned compounds, and(b) at least one bifunctional alkylating agent containing a straight or branched alkylene chain having 2-10 carbon atoms and which chain may be substituted with certain substituents and/or be broken by 1-3 oxygen atoms with certain conditions, in a molar relationship between (b) and (a) of 1:2-9:10.

    Abstract translation: 一种水溶性两性电解质，其包含（a）一种或多种选自包含某些氨基酸，羟胺，式IMA的胺，其中R 1是氢，H 2 N - （CH 2） n-，其中n是整数2-6，或基团H 2 N-（CH 2）3 -NH-（CH 2）3 - ，R 2和R 3相同或不同，各自表示氢，甲基，乙基或羟乙基或一起 中间氮原子形成某些杂环基，某些二肽和三肽，这些化合物中的至少一种是含有至少一个羧基的化合物，或上述化合物的盐，和（b）至少一种双官能烷基化剂 含有2-10个碳原子的直链或支链亚烷基链，并且该链可被一些取代基取代和/或在某些条件下被1-3个氧原子破坏，以（b）和（a）之间的摩尔关系 1：2-9：10。

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