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1. 发明授权

US4798904A Certain [(lower alkanoyl-thio)methyl-1-oxo-3-phenyl propyl amino]benzene lower alkanoic acid or ester derivatives which inhibit enkephalinase 失效
标题翻译：某些[（低级链烷酰硫基）甲基-1-氧代-3-苯基丙基氨基]苯低级链烷酸或酯衍生物，其抑制脑啡肽酶
公开(公告)号：US4798904A
公开(公告)日：1989-01-17
申请号：US119930
申请日：1987-11-13
申请人： Norma G. Delaney , Eric M. Gordon , Miguel A. Ondetti
发明人： Norma G. Delaney , Eric M. Gordon , Miguel A. Ondetti
IPC分类号： A61K31/16 , C07C153/11
CPC分类号： A61K31/16
摘要： Acylmercaptoalkanoyl compounds of the formula ##STR1## wherein n is an integer from one to fifteen possess enkephalinase inhibition activity and are useful as analgesic agents.
摘要翻译：其中n是1至15的整数，具有脑啡肽酶抑制活性，并且可用作镇痛剂，式αIMAGE的酰基巯基烷酰基化合物。

2. 发明授权

US4722810A Enkephalinase inhibitors 失效
标题翻译：脑啡肽酶抑制剂
公开(公告)号：US4722810A
公开(公告)日：1988-02-02
申请号：US896318
申请日：1986-08-13
申请人： Norma G. Delaney , Eric M. Gordon , Miguel A. Ondetti
发明人： Norma G. Delaney , Eric M. Gordon , Miguel A. Ondetti
IPC分类号： A61K31/16 , C08H3/00 , C07C149/273
CPC分类号： A61K31/16
摘要： Mercaptoalkanoyl and acylmercaptoalkanoyl compounds of the formula ##STR1## wherein n is an integer from one to fifteen possess enkephalinase inhibition activity and are useful as analgesic agents.
摘要翻译：式为“IMAGE”的巯基烷酰基和酰基巯基烷酰基化合物，其中n为1至15的整数，具有脑啡肽酶抑制活性，可用作止痛剂。

3. 发明授权

US4774256A Use of enkephalinase inhibitors as analgesic agents 失效
标题翻译：使用脑啡肽酶抑制剂作为止痛剂
公开(公告)号：US4774256A
公开(公告)日：1988-09-27
申请号：US120453
申请日：1987-11-13
申请人： Norma G. Delaney , Eric M. Gordon , Miguel A. Ondetti
发明人： Norma G. Delaney , Eric M. Gordon , Miguel A. Ondetti
IPC分类号： A61K31/16 , A61K31/20 , A61K31/195 , A61K31/21
CPC分类号： A61K31/16
摘要： Mercaptoalkanoyl and acylmercaptoalkanoyl compounds of the formula ##STR1## wherein n is an integer from one to fifteen possess enkephalinase inhibition activity and are useful as analgesic agents.
摘要翻译：式为“IMAGE”的巯基烷酰基和酰基巯基烷酰基化合物，其中n为1至15的整数，具有脑啡肽酶抑制活性，可用作止痛剂。

4. 发明授权

US4539312A Use of diamino ketones as analgesic agents 失效
标题翻译：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。

5. 发明授权

US5496805A Inhibitors of neutral endopeptidase 失效
标题翻译：中性内肽酶抑制剂
公开(公告)号：US5496805A
公开(公告)日：1996-03-05
申请号：US554976
申请日：1990-07-12
申请人： Norma G. Delaney , Eric M. Gordon , Jack M. DeForrest , David W. Cushman
发明人： Norma G. Delaney , Eric M. Gordon , Jack M. DeForrest , David W. Cushman
IPC分类号： A61K38/00 , A61K38/05
CPC分类号： A61K38/005
摘要： Diuresis, natriuresis, and the lowering of blood pressure are produced in a host by administering one or more neutral endopeptidase inhibitors. An additional blood pressure lowering agent such as an angiotensin converting enzyme inhibitor can be administered along with the neutral endopeptidase inhibitor.
摘要翻译：通过施用一种或多种中性内肽酶抑制剂，在宿主中产生利尿，利尿和降低血压。可以与中性内肽酶抑制剂一起施用另外的降血压药如血管紧张素转化酶抑制剂。

6. 发明授权

US4670541A Use of diamino alcohols as analgesic agents 失效
标题翻译：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。

7. 发明授权

US4594188A Use of diamino ketones as analgesic agents 失效
标题翻译：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。

8. 发明授权

US4552866A Use of diamino alcohols as analgesic agents 失效
标题翻译：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。

9. 发明授权

US4234489A Pyroglutamic acid derivatives and analogs 失效
标题翻译：焦谷氨酸衍生物和类似物
公开(公告)号：US4234489A
公开(公告)日：1980-11-18
申请号：US51772
申请日：1979-06-25
申请人： Miguel A. Ondetti , Eric M. Gordon , Denis E. Ryono
发明人： Miguel A. Ondetti , Eric M. Gordon , Denis E. Ryono
IPC分类号： A61K31/40 , A61K31/401 , A61K31/4015 , A61P9/12 , C07D207/24 , C07D207/28 , C07D207/36
CPC分类号： C07D207/24 , C07D207/28
摘要： Pyroglutamic acid derivatives and analogs having the formula ##STR1## and salts thereof, wherein R is hydrogen, alkyl or diphenylmethyl;R.sub.1 is hydrogen, alkyl or trifluoromethyl;R.sub.2 is hydrogen, ##STR2## or ##STR3## R.sub.3 is hydrogen, alkyl, phenyl, or phenylalkyl; X is oxygen or sulfur; andn is 0 or 1;have useful hypotensive activity.
摘要翻译：具有式“IMAGE”的焦谷氨酸衍生物和类似物及其盐，其中R是氢，烷基或二苯基甲基; R1是氢，烷基或三氟甲基; R 2是氢，R 3是氢，烷基，苯基或苯基烷基; X是氧或硫; 并且n为0或1; 有用的降血压活动。

10. 发明授权

US4714757A Aminopeptidase inhibitors 失效
标题翻译：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。

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