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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：US4539312A

    公开(公告)日：1985-09-03

    申请号：US629934

    申请日：1984-07-11

    申请人： Norma G. Delaney ,  Eric M. Gordon

    发明人： Norma G. Delaney ,  Eric M. Gordon

    IPC分类号： A61K38/00 ,  C07K5/065 ,  C07K7/02 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K7/02 ,  C07K5/06078 ,  A61K38/00

    摘要： An enkephalin-degrading aminopeptidase 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 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.

    摘要翻译： 脑啡肽降解氨基肽酶被具有下式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， 烷基硫代烷基，（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独立地是氢，烷基，芳基或芳基烷基或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。

    Use of diamino alcohols as analgesic agents
    6.
    发明授权
    Use of diamino alcohols as analgesic agents 失效
    二氨基醇用作止痛剂

    公开(公告)号：US4670541A

    公开(公告)日：1987-06-02

    申请号：US732331

    申请日：1985-05-10

    申请人： Norma G. Delaney ,  Eric M. Gordon

    发明人： Norma G. Delaney ,  Eric M. Gordon

    IPC分类号： A61K38/00 ,  C07K5/06 ,  C07K5/062 ,  C07K5/065 ,  C07K5/083 ,  C07K7/06 ,  C07K5/08

    CPC分类号： C07K7/06 ,  C07K5/06026 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/0808 ,  A61K38/00

    摘要： An enkephalin-degrading aminopeptidase 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.

    摘要翻译： 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。

    Use of diamino ketones as analgesic agents
    7.
    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

    申请人： Norma G. Delaney ,  Eric M. Gordon

    发明人： Norma G. Delaney ,  Eric M. Gordon

    IPC分类号： 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分类号： C07K7/02 ,  C07K5/06078 ,  A61K38/00

    摘要： 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.

    摘要翻译： 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。

    Use of diamino alcohols as analgesic agents
    8.
    发明授权
    Use of diamino alcohols as analgesic agents 失效
    二氨基醇用作止痛剂

    公开(公告)号：US4552866A

    公开(公告)日：1985-11-12

    申请号：US628004

    申请日：1984-07-05

    申请人： Norma G. Delaney ,  Eric M. Gordon

    发明人： Norma G. Delaney ,  Eric M. Gordon

    IPC分类号： A61K38/00 ,  C07K5/06 ,  C07K5/062 ,  C07K5/065 ,  C07K5/083 ,  A61K37/00

    CPC分类号： C07K5/0808 ,  C07K5/06026 ,  C07K5/06043 ,  C07K5/06078 ,  A61K38/00

    摘要： An enkephalin-degrading aminopeptidase 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.

    摘要翻译： 脑啡肽降解氨基肽酶被具有式（IMA）> TR（A1）n1（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R1和R2是 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。

    Aminopeptidase inhibitors
    9.
    发明授权
    Aminopeptidase inhibitors 失效
    氨肽酶抑制剂

    公开(公告)号：US4714757A

    公开(公告)日：1987-12-22

    申请号：US777121

    申请日：1985-09-18

    申请人： Eric M. Gordon ,  Jollie D. Godfrey, Jr. ,  Norma G. Delaney

    发明人： Eric M. Gordon ,  Jollie D. Godfrey, Jr. ,  Norma G. Delaney

    IPC分类号： C07K5/02

    CPC分类号： C07K5/02

    摘要： Aminopeptidase inhibitory activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts 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 hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl, (heteroaryl)alkyl, ##STR2## R.sub.4 and R.sub.5 are each independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl, or (heteroaryl)alkyl;A is glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, valyl, aspartyl, prolyl, norleucyl, or norvalyl; andn is an integer of 1 to 6.

    摘要翻译： 氨基肽酶抑制活性由具有下式的化合物及其药学上可接受的盐显示，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; R 3是氢，烷基，环烷基，芳基，杂芳基，芳基烷基，（杂芳基）烷基，+ R CH 2 NR 4 R 5; R 4和R 5各自独立地为氢，烷基，环烷基，芳基，杂芳基，芳烷基或（杂芳基）烷基; A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，赖氨酰，谷氨酰，组氨酰，色氨酰，半胱氨酰，甲硫氨酰，苏氨酰，酪氨酰，缬氨酰，天冬氨酰，脯氨酰， n为1〜6的整数。

    Amino thiol peptides
    10.
    发明授权
    Amino thiol peptides 失效
    氨基硫醇肽

    公开(公告)号：US4636560A

    公开(公告)日：1987-01-13

    申请号：US672044

    申请日：1984-11-16

    申请人： Jollie D. Godfrey, Jr. ,  Eric M. Gordon ,  Norma G. Delaney

    发明人： Jollie D. Godfrey, Jr. ,  Eric M. Gordon ,  Norma G. Delaney

    IPC分类号： C07D521/00 ,  A61K31/16 ,  A61K31/165 ,  A61K31/195 ,  A61K31/215 ,  A61K31/22 ,  A61K38/00 ,  A61K38/55 ,  A61P25/04 ,  A61P43/00 ,  C07C67/00 ,  C07C313/00 ,  C07C323/25 ,  C07C323/26 ,  C07C323/29 ,  C07C323/44 ,  C07C323/58 ,  C07C323/60 ,  C07K5/04 ,  C07K5/06 ,  C07K5/065 ,  C07K5/072 ,  C07K5/083 ,  C07K5/09 ,  C07K5/103 ,  C07K7/06 ,  C07K14/81 ,  C07C149/273

    CPC分类号： C07K5/1008 ,  C07C323/44 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/06095 ,  C07K5/0804 ,  C07K5/0815 ,  A61K38/00 ,  Y10S530/80

    摘要： Analgesic and hypotensive activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts 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, 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.

    摘要翻译： 具有式（IMA）> TR（A1）n1（A2）n2（A3）n3（A4）n4（A5）n5R3的化合物及其药学上可接受的盐，其中R1和R2各自独立地表现出止痛和降血压活性 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各自独立地为甘氨酰，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，组氨酰，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， 正亮片或正戊基; n1，n2，n3，n4和n5各自独立地为0或1。