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21. 发明授权

US5536833A Process for the preparation of intermediates useful in the preparation of pyranyl cyanoguanidine derivatives 失效
公开(公告)号：US5536833A
公开(公告)日：1996-07-16
申请号：US452238
申请日：1995-05-26
申请人： Jollie D. Godfrey, Jr. , Richard H. Mueller , Thomas C. Sedergran , Nachimuthu Soundararajan
发明人： Jollie D. Godfrey, Jr. , Richard H. Mueller , Thomas C. Sedergran , Nachimuthu Soundararajan
IPC分类号： C07C41/16 , C07C43/20 , C07C43/235 , C07C49/84 , C07C69/92 , C07C205/37 , C07C235/44 , C07C237/30 , C07C253/30 , C07C255/49 , C07C255/54 , C07C315/04 , C07C317/22 , C07C317/36 , C07C319/20 , C07C323/20 , C07C323/37 , C07D311/20 , C07D311/68 , C07D491/052 , C07F9/40 , C07F9/58 , C07F9/655 , C07F9/6561 , C07F9/6574 , C07D279/18 , C07D311/74
CPC分类号： C07C255/54 , C07C253/30 , C07D311/68
摘要： A process for preparing compounds of the formula ##STR1## where a, b, c, R.sub.1, R.sub.2, and R.sub.3 are as defined herein including the step of alkylating a phenol of formula ##STR2## with an acetylene of formula ##STR3## where X is chlorine; bromine; --OC(O)--R.sub.5, where R.sub.5 is alkyl, aryl or substituted aryl; or --OCO.sub.2 R.sub.6, where R.sub.6 is alkyl or ##STR4## in the presence of a catalytic amount of a cuprous or cupric salt. The compounds of formula I are intermediates useful in the preparation of pyranyl cyanoguanidine derivatives.

22. 发明授权

US5218142A Process for the preparation of an antiviral agent 失效
标题翻译：制备抗病毒剂的方法
公开(公告)号：US5218142A
公开(公告)日：1993-06-08
申请号：US962517
申请日：1992-10-16
申请人： Jollie D. Godfrey, Jr. , Richard H. Mueller , Thomas P. Kissick , Janak Singh
发明人： Jollie D. Godfrey, Jr. , Richard H. Mueller , Thomas P. Kissick , Janak Singh
IPC分类号： C07B57/00 , C07C45/58 , C07C49/753 , C07C51/487 , C07C61/35 , C07C69/68 , C07C69/743 , C07C309/73 , C07D473/00
CPC分类号： C07D473/00 , C07B57/00 , C07C309/73 , C07C45/58 , C07C49/753 , C07C51/487 , C07C61/35 , C07C69/68 , C07C69/743 , C07C2101/04
摘要： Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylenecyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl ester which is an intermediate in the preparation of the antiviral agent [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobutyl]-1,9-dihydro-6H-purin-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.
摘要翻译：外消旋Feist酸用（R） - （+） - α-甲基苄胺处理，得到（1R-反式）-3-亚甲基环丙烷-1,2-二羧酸，（R）-α-甲基苄胺（1:1）盐。然后将该盐转化为（1R-反式）-3-亚甲基-1,2-环丙烷二羧酸二甲酯，其是制备抗病毒剂[1R-（1α，2β，3α） ] -2-氨基-9- [2,3-双（羟甲基）环丁基] -1,9-二氢-6H-嘌呤-6-酮。改进的方法还可以从分辨率中回收外消旋的Feist酸。

23. 发明授权

US5185463A Process for the preparation of an antiviral agent 失效
标题翻译：制备抗病毒剂的方法
公开(公告)号：US5185463A
公开(公告)日：1993-02-09
申请号：US770191
申请日：1991-10-02
申请人： Jollie D. Godfrey, Jr. , Richard H. Mueller , Thomas P. Kissick , Janak Singh
发明人： Jollie D. Godfrey, Jr. , Richard H. Mueller , Thomas P. Kissick , Janak Singh
IPC分类号： C07C67/08 , C07B57/00 , C07C45/58 , C07C49/753 , C07C51/487 , C07C61/35 , C07C69/743 , C07C211/27 , C07C309/73 , C07D473/00 , C07D473/18
CPC分类号： C07D473/00 , C07B57/00 , C07C309/73 , C07C45/58 , C07C49/753 , C07C51/487 , C07C61/35 , C07C69/743 , C07C2101/04
摘要： Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylenecyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl ester which is an intermediate in the preparation of the antiviral agent [1R-(1.alpha.,2.beta., 3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobutyl]-1,9-dihydro-6H-purin-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.

24. 发明授权

US5106977A Intermediates for a process for making 2-oxo-1-[[(substituted sulfonyl)-amino]carbonyl]azetidines 失效
标题翻译： 2-氧代-1 - [[（取代的磺酰基） - 氨基]羰基]氮杂环丁烷的制备方法的中间体
公开(公告)号：US5106977A
公开(公告)日：1992-04-21
申请号：US589289
申请日：1990-09-27
申请人： Jollie D. Godfrey, Jr. , Richard H. Mueller
发明人： Jollie D. Godfrey, Jr. , Richard H. Mueller
IPC分类号： C07D213/79 , C07D417/12 , C07D417/14
CPC分类号： C07D213/79 , C07D417/12 , C07D417/14
摘要： Novel intermediates for preparing 2-oxo-1-[[(substituted sulfonyl)-amino]carbonyl]azetidines are disclosed. These intermediates have the formula ##STR1## wherein Prot is as defined herein.
摘要翻译：公开了用于制备2-氧代-1 - [[（取代的磺酰基） - 氨基]羰基]氮杂环丁烷的新型中间体。这些中间体具有其中Prot如本文所定义的式“IMAGE”XX。

25. 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。

26. 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。

27. 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。

28. 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。

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