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1. 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。

2. 发明授权

US4636560A Amino thiol peptides 失效
标题翻译：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。

3. 发明授权

US4558150A Intermediates for preparing amino thiol dipeptides 失效
标题翻译：制备氨基硫醇二肽的中间体
公开(公告)号：US4558150A
公开(公告)日：1985-12-10
申请号：US680119
申请日：1984-12-10
申请人： Eric M. Gordon , Jollie D. Godfrey, Jr.
发明人： Eric M. Gordon , Jollie D. Godfrey, Jr.
IPC分类号： A61K38/00 , C07D233/64 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07D239/02 , C07C103/22 , C07D209/02 , C07D209/04 , C07D209/10 , C07D209/44 , C07D211/70 , C07D211/72 , C07D211/78 , C07D213/04 , C07D213/40 , C07D213/44 , C07D233/54 , C07D307/02 , C07D333/22 , C07D401/00 , C07D403/00 , C07D409/00
CPC分类号： C07K5/06026 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06095 , C07K5/06104 , A61K38/00
摘要： Intermediates of the formula ##STR1## are disclosed. These compounds are useful in the preparation of amino thiol dipeptides possessing angiotensin converting enzyme inhibition activity and enkephalinase inhibition activity.
摘要翻译：公开了“IMAGE”公式的中间体。这些化合物可用于制备具有血管紧张素转换酶抑制活性和脑啡肽酶抑制活性的氨基硫醇二肽。

4. 发明授权

US4604402A Hydroxy substituted ureido amino and imino acids 失效
标题翻译：羟基取代的脲基氨基和亚氨基酸
公开(公告)号：US4604402A
公开(公告)日：1986-08-05
申请号：US595218
申请日：1984-03-30
申请人： Jollie D. Godfrey, Jr. , Eric M. Gordon , Sesha I. Natarajan
发明人： Jollie D. Godfrey, Jr. , Eric M. Gordon , Sesha I. Natarajan
IPC分类号： C07D333/22 , A61K31/397 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/4427 , A61P9/12 , A61P43/00 , C07C67/00 , C07C239/00 , C07C275/00 , C07C279/04 , C07C313/00 , C07C323/44 , C07D205/04 , C07D207/16 , C07D209/44 , C07D213/55 , C07D231/06 , C07D263/42 , C07D277/06 , C07D307/52 , C07D401/12 , C07D403/12 , C07D413/04 , C07D495/10 , C07K1/113 , C07K5/06 , C07K14/81 , C12N9/99 , C07D207/04 , C07D207/20
CPC分类号： C07D401/12 , C07D207/16 , C07D403/12
摘要： Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
摘要翻译：公开了式“IMAGE”的化合物。这些化合物由于其血管紧张素转换酶抑制活性而可用作降压剂，并且取决于X的定义，由于其脑啡肽酶抑制活性也可用作镇痛药。

5. 发明授权

US4524212A Acyloxyketone substituted imino and amino acids 失效
标题翻译：芳氧基酮取代亚氨基和氨基酸
公开(公告)号：US4524212A
公开(公告)日：1985-06-18
申请号：US423875
申请日：1982-09-27
申请人： Eric M. Gordon , Jollie D. Godfrey, Jr.
发明人： Eric M. Gordon , Jollie D. Godfrey, Jr.
IPC分类号： C07C69/003 , A61K31/215 , A61K31/425 , A61K31/426 , A61P9/12 , A61P25/04 , C07C59/48 , C07C67/00 , C07C231/00 , C07C235/12 , C07C235/26 , C07C235/34 , C07C235/74 , C07C237/12 , C07C239/00 , C07C271/10 , C07C279/14 , C07C313/00 , C07C323/58 , C07D207/16 , C07D207/22 , C07D217/26 , C07D233/64 , C07D277/06 , C07D307/54 , C07D319/06 , C07D333/38 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D491/113 , C07D495/10 , C07D207/20 , C07D207/09
CPC分类号： C07D319/06 , C07C59/48 , C07D207/16
摘要： Acyloxyketone substituted imino and amino acids of the formula ##STR1## are disclosed. These compounds are useful hypotensive agents due to their angiotensin converting enzyme inhibition activity.
摘要翻译：公开了芳基氧基酮取代的亚氨基和式“IMAGE”的氨基酸。由于它们的血管紧张素转换酶抑制活性，这些化合物是有用的降血糖药。

6. 发明授权

US4500518A Amino thiol dipeptides 失效
标题翻译：氨基硫醇二肽
公开(公告)号：US4500518A
公开(公告)日：1985-02-19
申请号：US602030
申请日：1984-04-19
申请人： Eric M. Gordon , Jollie D. Godfrey, Jr.
发明人： Eric M. Gordon , Jollie D. Godfrey, Jr.
IPC分类号： C07D207/16 , A61K38/00 , A61K38/55 , A61P9/12 , A61P25/04 , A61P43/00 , C07K1/113 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07K14/81 , A01N43/36 , A01N43/50 , C07C103/52 , C07D211/60 , C07D217/00 , C07D231/00
CPC分类号： C07K5/06026 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06104 , C07K5/06139 , A61K38/00
摘要： Amino thiol substituted dipeptides of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
摘要翻译：披露式“IMAGE”的氨基硫醇取代的二肽。这些化合物由于其血管紧张素转换酶抑制活性而可用作降压剂，并且取决于X的定义，由于其脑啡肽酶抑制活性也可用作镇痛药。

7. 发明授权

US4720585A Aminopeptidase inhibitors 失效
标题翻译：氨肽酶抑制剂
公开(公告)号：US4720585A
公开(公告)日：1988-01-19
申请号：US777122
申请日：1985-09-18
申请人： Jollie D. Godfrey Jr. , Eric M. Gordon
发明人： Jollie D. Godfrey Jr. , Eric M. Gordon
IPC分类号： C07C149/24 , C07C149/14
CPC分类号： C07C323/25 , C07C323/29 , C07D209/14 , C07D233/64
摘要： Aminopeptidase inhibitory activity is exhibited by compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl, carboxyalkyl, halo-substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl or heteroaryl; andR.sub.2 and R.sub.3 are each independently hydrogen, alkyl, cycloalkyl, hydroxyalkyl, aminoalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl.
摘要翻译：氨基肽酶抑制活性由具有下式的化合物表现：其中R1是氢，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; 并且R 2和R 3各自独立地为氢，烷基，环烷基，羟基烷基，氨基烷基，芳基，芳基烷基，杂芳基或杂芳基烷基。

8. 发明授权

US4514391A Hydroxy substituted peptide compounds 失效
标题翻译：羟基取代的肽化合物
公开(公告)号：US4514391A
公开(公告)日：1985-04-30
申请号：US515729
申请日：1983-07-21
申请人： Eric M. Gordon , Jollie D. Godfrey, Jr. , Sesha I. Natarajan
发明人： Eric M. Gordon , Jollie D. Godfrey, Jr. , Sesha I. Natarajan
IPC分类号： C07D209/30 , A61K31/397 , A61K31/40 , A61K31/403 , A61K31/404 , A61K38/00 , A61K38/55 , A61P9/12 , A61P25/04 , A61P43/00 , C07D205/04 , C07D207/16 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/078 , C07K14/81 , A61K37/00 , C07C103/52
CPC分类号： C07K5/06026 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06095 , C07K5/06139 , C07K5/06191 , A61K38/00 , Y10S530/80
摘要： Hydroxy substituted peptide compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
摘要翻译：公开了式“IMAGE”的羟基取代的肽化合物。这些化合物由于其血管紧张素转换酶抑制活性而可用作降压剂，并且取决于X的定义，由于其脑啡肽酶抑制活性也可用作镇痛药。

9. 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。

10. 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。

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