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11. 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。

12. 发明授权

US4560506A Mercaptocycloalkylcarbonyl and mercaptoarylcarbonyl dipeptides 失效
标题翻译：巯基环烷基羰基和巯基芳基羰基二肽
公开(公告)号：US4560506A
公开(公告)日：1985-12-24
申请号：US614090
申请日：1984-05-25
申请人： Harold N. Weller, III , Eric M. Gordon , Norma G. Delaney
发明人： Harold N. Weller, III , Eric M. Gordon , Norma G. Delaney
IPC分类号： C07D207/16 , A61K31/40 , A61K38/00 , A61K38/55 , A61P9/12 , A61P25/04 , A61P43/00 , C07K5/06 , C07K5/062 , C07K5/065 , C07K14/81 , C07D , C07D207/00 , C07D209/02 , C07D209/44 , C07D211/06 , C07D213/22 , C07D231/06 , C07D241/36 , C07D277/04 , C07D277/60 , C07D499/00
CPC分类号： C07K5/06078
摘要： Compounds of the formula ##STR1## wherein A is a cycloalkyl ring, a substituted cycloalkyl ring, a phenyl ring, or a substituted phenyl ring and ##STR2## are various dipeptide groups are disclosed. The compounds possess angiotensin converting enzyme inhibition activity and depending upon the terminal amino acid may also possess enkephalinase inhibition activity.
摘要翻译：其中A是环烷基环，取代的环烷基环，苯基环或取代的苯环，并且“IMAGE”的化合物是各种二肽基团。该化合物具有血管紧张素转换酶抑制活性，并且取决于末端氨基酸也可以具有脑啡肽酶抑制活性。

13. 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。

14. 发明授权

US4337197A O-sulfated .beta.-lactam hydroxamic acids and intermediates 失效
标题翻译： O-硫酸化β-内酰胺异羟肟酸和中间体
公开(公告)号：US4337197A
公开(公告)日：1982-06-29
申请号：US202830
申请日：1980-10-31
申请人： Eric M. Gordon , Miguel A. Ondetti
发明人： Eric M. Gordon , Miguel A. Ondetti
IPC分类号： C07D205/08 , A61K31/395 , A61K31/397 , A61K31/435 , A61K31/505 , A61P31/04 , C07D205/085 , C07D403/12 , C07D409/12 , C07D417/12 , C07D471/04
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。

15. 发明授权

US5166364A Mevinic acid derivatives useful as antihypercholesterolemic agents and method for preparing same 失效
标题翻译：可用作抗高胆固醇血症药的米维酸衍生物及其制备方法
公开(公告)号：US5166364A
公开(公告)日：1992-11-24
申请号：US765806
申请日：1991-09-26
申请人： Jeffrey O. Saunders , Eric M. Gordon
发明人： Jeffrey O. Saunders , Eric M. Gordon
IPC分类号： C07C59/11 , C07D309/30 , C07F7/18
CPC分类号： C07F7/1856 , C07C59/11 , C07D309/30
摘要： Mevinic acid derivatives are provided which are 6-hydroxy-8-(2,2-dimethyl-1-oxybutoxy- 2-methyl)-substituted-decahydronaphthalene esters and have the structure ##STR1## wherein Z is ##STR2## wherein R is alkali metal such as Na, or H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis, and also as antifungal agents.In addition, a method for preparing the above-mevinic acid derivatives is also provided.
摘要翻译：提供了6-羟基-8-（2,2-二甲基-1-氧丁氧基-2-甲基） - 取代十氢萘酯的维甲酸衍生物，其结构为：其中R为碱金属如Na或H或低级烷基，并且是HMG CoA还原酶抑制剂，因此可用作抗高胆固醇血症药物和治疗动脉粥样硬化，并且还可用作抗真菌剂。此外，还提供了制备上述维甲酸衍生物的方法。

16. 发明授权

US4906667A Phenyl hydroxamic acids including a hetero-containing substituent 失效
标题翻译：苯基异羟肟酸，包括含杂原子的取代基
公开(公告)号：US4906667A
公开(公告)日：1990-03-06
申请号：US203527
申请日：1988-05-23
申请人： Ravi K. Varma , Eric M. Gordon , Martin F. Haslanger
发明人： Ravi K. Varma , Eric M. Gordon , Martin F. Haslanger
IPC分类号： C07C259/10
CPC分类号： C07C259/10 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： Phenyl hydroxamic acids are disclosed having the general formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein X is NR, oxygen, sulfur, ##STR2## or a single bond, and Y is NR, oxygen, sulfur, ##STR3## or a single bond, where R can be hydrogen or lower alkyl, g can be 1 or 2, and with the proviso that at least one of X and Y is other than a single bond; Z is aryl, aralkyl or cycloalkyl; R.sub.1 is hydrogen, substituted or unsubstituted lower alkyl, cycloalkyl, lower alkenyl or aryl; R.sub.2 is hydrogen, lower alkyl, aroyl or acyl; m is 0 to 4 carbon atoms; and, n is 0 to 4 carbon atoms further providing that if one of X or Y is oxygen, the other of X or Y must be oxygen and further that when X and Y are oxygen Z cannot be aralalkyl.These new compounds have been found to be inhibitors or arachidonic acid 5-lipoxygenase and are therefore useful as antiallergy agents and antipsoriatics.
摘要翻译：公开了具有通式为“IMAGE”或其药学上可接受的盐的苯基异羟肟酸，其中X是NR，氧，硫，或单键，Y是NR，氧，硫，单键，其中R可以是氢或低级烷基，g可以是1或2，条件是X和Y中的至少一个不是单键; Z是芳基，芳烷基或环烷基; R 1是氢，取代或未取代的低级烷基，环烷基，低级烯基或芳基; R2是氢，低级烷基，芳酰基或酰基; m为0〜4个碳原子; 并且n为0至4个碳原子，条件是如果X或Y中的一个为氧，X或Y中的另一个必须为氧，此外，当X和Y为氧时，Z不能为芳烷基。已经发现这些新化合物是抑制剂或花生四烯酸5-脂氧合酶，因此可用作抗过敏剂和抗牛皮癣剂。

17. 发明授权

US4818757A Ureidoalkanoylaminocarbonyl amino and imino acids and esters 失效
标题翻译：脲基链烷酰氨基羰基氨基和亚氨基酸和酯
公开(公告)号：US4818757A
公开(公告)日：1989-04-04
申请号：US140448
申请日：1987-12-28
申请人： Harold N. Weller, III , Eric M. Gordon
发明人： Harold N. Weller, III , Eric M. Gordon
IPC分类号： C07C275/24 , C07D205/04 , C07D207/10 , C07D207/16 , C07D207/22 , C07D209/42 , C07D209/52 , C07D211/42 , C07D211/60 , C07D217/26 , C07D231/06 , C07D233/38 , C07D233/54 , C07D277/06 , C07D295/215 , C07D401/12 , C07D403/12 , C07D409/12 , C07D487/04 , C07D495/10 , A61K31/535
CPC分类号： C07D231/06 , C07C275/24 , C07D205/04 , C07D207/10 , C07D207/16 , C07D207/22 , C07D209/42 , C07D209/52 , C07D211/42 , C07D211/60 , C07D217/26 , C07D233/38 , C07D233/64 , C07D277/06 , C07D295/215 , C07D401/12 , C07D403/12 , C07D409/12 , C07D487/04 , C07D495/10
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。

18. 发明授权

US4742067A Acylalkylaminocarbonyl substituted amino and imino acid compounds 失效
标题翻译：酰基烷基氨基羰基取代的氨基和亚氨基酸化合物
公开(公告)号：US4742067A
公开(公告)日：1988-05-03
申请号：US890681
申请日：1986-07-30
申请人： Sesha I. Natarajan , Eric M. Gordon
发明人： Sesha I. Natarajan , Eric M. Gordon
IPC分类号： C07D205/04 , C07D207/16 , C07D207/48 , C07D209/20 , C07D211/60 , C07D217/26 , C07D231/06 , C07D277/06 , C07D401/12 , C07D405/12 , C07D409/12 , A61K31/44
CPC分类号： C07D231/06 , C07D205/04 , C07D207/16 , C07D207/48 , C07D209/20 , C07D211/60 , C07D217/26 , C07D277/06 , C07D401/12 , C07D405/12 , C07D409/12
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。

19. 发明授权

US4740508A Ureidoalkanoylaminocarbonyl amino and imino acids and esters 失效
标题翻译：脲基链烷酰氨基羰基氨基和亚氨基酸和酯
公开(公告)号：US4740508A
公开(公告)日：1988-04-26
申请号：US726264
申请日：1985-04-22
申请人： Harold N. Weller, III , Eric M. Gordon
发明人： Harold N. Weller, III , Eric M. Gordon
IPC分类号： A61K31/195 , A61K31/215 , A61K31/22 , A61K31/397 , A61K31/40 , A61K31/4025 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4166 , A61K31/425 , A61K31/426 , A61K31/47 , A61K31/472 , A61K31/535 , A61P9/12 , A61P25/04 , A61P43/00 , C07C67/00 , C07C239/00 , C07C275/24 , C07C275/50 , C07D205/04 , C07D207/10 , C07D207/16 , C07D207/22 , C07D209/42 , C07D209/52 , C07D211/42 , C07D211/60 , C07D217/26 , C07D231/06 , C07D233/34 , C07D233/38 , C07D233/54 , C07D277/06 , C07D295/215 , C07D333/00 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D487/04 , C07D495/10 , C12N9/99 , C07D401/00 , A61K31/44 , C07D211/06
CPC分类号： C07D231/06 , C07C275/24 , C07D205/04 , C07D207/10 , C07D207/16 , C07D207/22 , C07D209/42 , C07D209/52 , C07D211/42 , C07D211/60 , C07D217/26 , C07D233/38 , C07D233/64 , C07D277/06 , C07D295/215 , C07D401/12 , C07D403/12 , C07D409/12 , C07D487/04 , C07D495/10
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。

20. 发明授权

US4692455A Certain acyclic, alicyclic, aromatic or heterocyclic derivatives of 3-benzoylamino-2-oxo- butyl-amino-carbonyl-oxy-3-propanoic acids, esters thereof, pharmaceutical compositions containing same and their enkephalinase inhibiting properties 失效
标题翻译：某些3-苯甲酰基氨基-2-氧代丁基 - 氨基 - 羰基 - 氧基-3-丙酸的无环，脂环，芳族或杂环衍生物，其酯，含有它们的药物组合物及其脑啡肽酶抑制性质
公开(公告)号：US4692455A
公开(公告)日：1987-09-08
申请号：US694871
申请日：1985-01-25
申请人： Eric M. Gordon
发明人： Eric M. Gordon
IPC分类号： A61K31/27 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61P9/12 , A61P25/04 , A61P43/00 , C07C67/00 , C07C239/00 , C07C271/20 , C07C279/04 , C07C313/00 , C07C323/44 , C07C323/52 , C07C323/62 , C07C325/00 , C07C333/04 , C07D209/22 , C07D213/55 , C07D213/81 , C07D233/54 , C07D307/52 , C07D333/22 , C07D333/24 , C07C125/04 , A61K31/44 , C07C149/437
CPC分类号： C07D213/81 , C07D209/22 , C07D213/55 , C07D233/64 , C07D307/52 , C07D333/22 , C07D333/24
摘要： Compounds of the formula ##STR1## wherein Y is oxygen or sulfur are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of R.sub.1 may also be useful as analgesics due to their enkepahlinase inhibition activity.
摘要翻译：公开了其中Y是氧或硫的式“IMAGE”的化合物。由于它们的血管紧张素转换酶抑制活性，这些化合物可用作降压剂，并且取决于R1的定义也可以由于其脑啡肽激酶抑制活性而用作镇痛药。

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