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81. 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。

82. 发明授权

US4533660A Antibacterial O-sulfated .beta.-lactam hydroxamic acids 失效
标题翻译：抗菌O-硫酸化β-内酰胺异羟肟酸
公开(公告)号：US4533660A
公开(公告)日：1985-08-06
申请号：US320407
申请日：1981-11-12
申请人： Eric M. Gordon , Miguel A. Ondetti
发明人： Eric M. Gordon , Miguel A. Ondetti
IPC分类号： C07D205/085 , C07D205/08 , A61K31/395
CPC分类号： C07D205/085
摘要： Antibacterial activity is exhibited by .beta.-lactams having a sulfate substituent in the 1-position and an acylamino substituent in the 3-position.
摘要翻译：在1-位具有硫酸酯取代基和3-位酰基氨基取代基的β-内酰胺显示出抗菌活性。

83. 发明授权

US4470973A Substituted peptide compounds 失效
标题翻译：取代的肽化合物
公开(公告)号：US4470973A
公开(公告)日：1984-09-11
申请号：US500581
申请日：1983-06-02
申请人： Sesha I. Natarajan , Eric M. Gordon
发明人： Sesha I. Natarajan , Eric M. Gordon
IPC分类号： A61K38/00 , C07D233/64 , C07K5/06 , C07K5/062 , A61K37/00 , A01N43/36 , A01N43/50 , C07D211/60 , C07D217/00 , C07D231/00
CPC分类号： C07K5/06078 , C07K5/06026 , C07K5/06034 , C07K5/06095 , C07K5/06139 , C07K5/06191 , A61K38/00 , Y10S530/80
摘要： 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：公开了取代的式“IMAGE”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。

84. 发明授权

US4456595A Carboxy and substituted carboxy aroly peptides 失效
标题翻译：羧基和取代的羧基芳香肽
公开(公告)号：US4456595A
公开(公告)日：1984-06-26
申请号：US446923
申请日：1982-12-06
申请人： Harold N. Weller, III , Eric M. Gordon
发明人： Harold N. Weller, III , Eric M. Gordon
IPC分类号： C07K5/06 , C07K5/062 , C07K5/072 , C07K5/078 , A61K37/00 , C07C103/52
CPC分类号： C07K5/06034 , C07K5/06026 , C07K5/06078 , C07K5/06095 , C07K5/06147 , C07K5/06156 , Y10S530/80
摘要： Peptides of the formula ##STR1## wherein X is various amino or imino acids or esters are useful as hypotensive agents.
摘要翻译：其中X是各种氨基或亚氨基酸或酯的式“IMAGE”的肽可用作降压剂。

85. 发明授权

US4169946A Reactions of thiooxime cephalosporin and penicillin derivatives 失效
标题翻译：硫氧嘧啶和哌啶醇衍生物的反应
公开(公告)号：US4169946A
公开(公告)日：1979-10-02
申请号：US917000
申请日：1978-06-19
申请人： Eric M. Gordon
发明人： Eric M. Gordon
IPC分类号： C07D499/00 , C07D501/57 , C07D501/18 , C07D499/42
CPC分类号： C07D499/00
摘要： Compounds of the formula ##STR1## wherein A is ##STR2## R is hydrogen, lower alkyl, benzyl, p-methoxybenzyl, p-nitrobenzyl, diphenylmethyl, tri(lower alkyl)silyl, lower alkoxymethyl, 2,2,2-trichloroethyl, ##STR3## Y is halogen or lower alkoxy; R.sub.1 is lower alkyl, phenyl, or substituted phenyl; and X is hydrogen, lower alkanoyloxy, ##STR4## or certain heterothio groups; R.sub.4 is hydrogen or lower alkyl; R.sub.5 is lower alkyl; are disclosed. These compounds, particularly the free acids, possess the useful pharmacological property of inhibiting .beta.-lactamase enzymes as well as being useful as intermediates, particularly where R is a readily cleavable ester, in the preparation of antibacterially active 6.alpha.-methoxy penicillins and 7.alpha.-methoxy cephalosporins.

86. 发明授权

US4129731A Process for converting 3-methylene cephalosporins to 3-heterothiomethyl cephalosporins 失效
标题翻译：将3-亚甲基头孢菌素转化为3-异硫代甲基头孢菌素的方法
公开(公告)号：US4129731A
公开(公告)日：1978-12-12
申请号：US748426
申请日：1976-12-08
申请人： William A. Slusarchyk , Eric M. Gordon , William H. Koster
发明人： William A. Slusarchyk , Eric M. Gordon , William H. Koster
IPC分类号： C07D20060101 , C07D501/02 , C07D501/04 , C07D501/36 , C07D501/57 , C07D501/60
CPC分类号： C07D501/36 , Y02P20/55
摘要： This invention relates to the preparation of 3-heterothiomethyl cephalosporanic acid esters of the formula ##STR1## by treating a 3-methylene cephalosporin of the formula ##STR2## with a compound of the formulaHETERO-S-S-hetero or X-S-heteroin the presence of a base wherein R is a readily removable ester group, R.sub.1 is in the .alpha.-configuration and is hydrogen or methoxy, and X is a leaving group. The resulting 3-heterothio cephalosporin esters are treated according to known methods to remove the ester protecting group and yield the corresponding free acids which have antibacterial activity.
摘要翻译：本发明涉及通过用式HETERO-SS-异或XS-杂的化合物处理式（IMAGE）的3-亚甲基头孢菌素来制备式“IMAGE”的3-异硫代甲基头孢菌酸酯。其中R是容易除去的酯基，R 1是α构型并且是氢或甲氧基，X是离去基团。根据已知方法对所得的3-异头孢菌素酯进行处理以除去酯保护基团并产生具有抗菌活性的相应游离酸。

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