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51. 发明授权

US5776933A Method of inhibiting protease 失效
标题翻译：抑制蛋白酶的方法
公开(公告)号：US5776933A
公开(公告)日：1998-07-07
申请号：US456125
申请日：1995-05-31
申请人： Eric M. Gordon , Joel C. Barrish , Gregory S. Bisacchi , Chong-Qing Sun , Joseph A. Tino , Gregory D. Vite , Robert Zahler
发明人： Eric M. Gordon , Joel C. Barrish , Gregory S. Bisacchi , Chong-Qing Sun , Joseph A. Tino , Gregory D. Vite , Robert Zahler
IPC分类号： A61K31/13 , A61K31/16 , A61K31/18 , A61K31/265 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4166 , A61K31/4184 , A61K31/496 , A61K31/505 , A61P31/12 , A61P31/18 , A61P37/00 , C07C215/28 , C07C233/40 , C07C233/78 , C07C235/40 , C07C237/10 , C07C271/10 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/05 , C07C313/06 , C07C333/04 , C07C333/12 , C07D207/09 , C07D207/16 , C07D207/26 , C07D207/267 , C07D209/12 , C07D209/14 , C07D209/18 , C07D209/44 , C07D209/46 , C07D213/30 , C07D213/36 , C07D213/40 , C07D213/55 , C07D213/56 , C07D213/65 , C07D215/14 , C07D215/48 , C07D217/16 , C07D231/56 , C07D233/30 , C07D233/32 , C07D233/54 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/24 , C07D239/34 , C07D239/91 , C07D241/42 , C07D243/04 , C07D263/22 , C07D263/24 , C07D263/26 , C07D263/32 , C07D263/56 , C07D265/32 , C07D277/64 , C07D295/092 , C07D295/185 , C07D303/36 , C07D305/08 , C07D307/20 , C07D307/24 , C07D309/10 , C07D333/64 , C07D413/14 , C07D491/04 , C07D521/00 , C07F7/08 , C07F7/18 , A61K31/445 , A61K31/535
CPC分类号： C07D207/267 , C07C215/28 , C07C233/40 , C07C233/78 , C07C235/40 , C07C237/10 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C333/04 , C07C333/12 , C07D207/09 , C07D207/16 , C07D209/12 , C07D209/14 , C07D209/18 , C07D209/44 , C07D209/46 , C07D213/30 , C07D213/40 , C07D213/56 , C07D213/65 , C07D215/14 , C07D215/48 , C07D217/16 , C07D231/12 , C07D231/56 , C07D233/32 , C07D233/56 , C07D233/64 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/24 , C07D239/91 , C07D241/42 , C07D249/08 , C07D263/22 , C07D263/24 , C07D263/26 , C07D263/32 , C07D263/56 , C07D265/32 , C07D277/64 , C07D295/088 , C07D295/185 , C07D305/08 , C07D307/20 , C07D307/24 , C07D309/10 , C07D333/64 , C07D413/14 , C07D491/04 , C07F7/0812 , C07F7/0818 , C07F7/1852 , C07F7/1856 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2103/18
摘要： Novel aminediol compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds in inhibiting retroviral protease, particularly useful in the treatment and/or prevention of HIV infection (AIDS).
摘要翻译：新型二胺化合物，含有这些化合物的药物组合物，以及使用这些化合物抑制逆转录病毒蛋白酶的方法，特别可用于治疗和/或预防HIV感染（AIDS）。

53. 发明授权

US5264455A Sulfur-substituted mevinic acid derivatives 失效
标题翻译：硫取代的维甲酸衍生物
公开(公告)号：US5264455A
公开(公告)日：1993-11-23
申请号：US724272
申请日：1991-07-01
申请人： Ravi K. Varma , Jeffrey O. Saunders , Sam T. Chao , Eric M. Gordon , Dinos P. Santafianos
发明人： Ravi K. Varma , Jeffrey O. Saunders , Sam T. Chao , Eric M. Gordon , Dinos P. Santafianos
IPC分类号： C07C317/46 , C07C323/61 , C07C323/65 , A61K31/35 , A61K31/215 , C07D339/00
CPC分类号： C07C317/46 , C07C323/61 , C07C323/65 , C07C2101/08 , C07C2101/14 , C07C2102/10
摘要： X is hydrogen or --S(O).sub.m --R.sup.1 and Y is hydrogen or S(O).sub.n --R.sup.2, except that X and Y are not both hydrogen, or one of X and Y is --S--alkyl--SH and the other is hydrogen; ##STR2## and the remaining symbols are as defined in the specification.
摘要翻译：其作为细胞选择性HMG-CoA还原酶抑制剂具有活性，因此可用作抗高胆固醇血症药。在上式中，X是氢或-S（O）m -R 1，Y是氢或S（O）n -R 2，不同之处在于X和Y不同时为氢，X和Y之一为-S- 烷基-SH，另一个是氢; ＆lt; IMAGE＆gt;其余符号如说明书中所定义。

54. 发明授权

US5177104A 6-.alpha.-hydroxy derivatives of mevinic acids 失效
标题翻译： 6-（ALPHA） - 甲氧基衍生物
公开(公告)号：US5177104A
公开(公告)日：1993-01-05
申请号：US503576
申请日：1990-04-03
申请人： Ravi K. Varma , Sam T. Chao , Eric M. Gordon
发明人： Ravi K. Varma , Sam T. Chao , Eric M. Gordon
IPC分类号： A61K31/22 , A61K31/365 , A61P3/06 , A61P9/10 , A61P43/00 , C07C69/013 , C07C69/03 , C07C69/675 , C07C69/732 , C07D309/30
CPC分类号： C07D309/30 , C07C69/732 , Y10S514/824
摘要： Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof have been found to possess activity as cell-selective HMG-CoA reductase inhibitors, thus making them useful as antihypercholesterolemic agents. In the above formula, ##STR2## R.sup.1 is hydrogen, alkyl, cycloalkyl, aryl or arylalkyl; and R.sup.2 is hydrogen, alkyl, ammonium, or alkali metal.

55. 发明授权

US5173487A Mevinic acid derivatives 失效
标题翻译：油酸衍生物
公开(公告)号：US5173487A
公开(公告)日：1992-12-22
申请号：US435843
申请日：1989-11-13
申请人： Jeffrey O. Saunders , Eric M. Gordon
发明人： Jeffrey O. Saunders , Eric M. Gordon
IPC分类号： A61K31/21 , A01N37/02 , A01N43/16 , A61K31/215 , A61K31/27 , A61K31/365 , A61K31/435 , A61K31/505 , A61P3/06 , A61P9/10 , A61P43/00 , C07C69/013 , C07C69/675 , C07C69/732 , C07C317/44 , C07C323/52 , C07C323/61 , C07D211/62 , C07D213/79 , C07D233/36 , C07D295/20 , C07D309/30 , C07D405/12 , C07D471/04 , C07F7/18
CPC分类号： C07D309/30 , C07C69/732
摘要： Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, is exhibited by a compound of the formula ##STR1## m is 0 to 3; R is selected from:(1) alkyl;(2) substituted alkyl;(3) alkoxy;(4) alkenyl;(5) cycloalkyl;(6) phenyl; and(7) substituted aryl; andR.sup.1 and R.sup.2 are as defined in the specification.

56. 发明授权

US4810791A 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：US4810791A
公开(公告)日：1989-03-07
申请号：US138477
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： 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 , C07D251/18 , C07D409/00
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 definintion of X may also be useful as analgesics due to their enkephalinase inhibition activity.

57. 发明授权

US4749781A Aminocarbonyl renin inhibitors 失效
标题翻译：氨基羰基肾素抑制剂
公开(公告)号：US4749781A
公开(公告)日：1988-06-07
申请号：US909434
申请日：1986-09-19
申请人： Eric M. Gordon
发明人： Eric M. Gordon
IPC分类号： A61K38/00 , C07D233/54 , C07K5/02 , C07K5/065 , A61K37/02
CPC分类号： C07D233/64 , C07K5/0227 , C07K5/06078 , A61K38/00 , Y10S530/86
摘要： Compounds of the formula ##STR1## are disclosed. These compounds intervene in the conversion of angiotensinogen to angiotensin II by inhibiting renin and thus are useful as antihypertensive agents.
摘要翻译：公开了式“IMAGE”的化合物。这些化合物通过抑制肾素来介入血管紧张素原转化成血管紧张素II，因此可用作抗高血压药。

58. 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。

59. 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。

60. 发明授权

US4695585A 7-oxabicyclo(2.2.1)heptane analogs useful as inhibitors of 5-lipoxygenase and cyclooxygenase 失效
标题翻译：可用作5-脂氧合酶和环氧合酶抑制剂的7-氧杂二环（2.2.1）庚烷类似物
公开(公告)号：US4695585A
公开(公告)日：1987-09-22
申请号：US910583
申请日：1986-09-23
申请人： Ravi K. Varma , Eric M. Gordon
发明人： Ravi K. Varma , Eric M. Gordon
IPC分类号： A61K31/34 , A61P11/08 , A61P29/00 , A61P37/08 , C07D493/08 , C07D307/00
CPC分类号： C07D493/08 , Y10S514/826 , Y10S514/863
摘要： A compound of the formula ##STR1## wherein R.sub.1 is hydrogen, hydroxy, alkoxy or aryloxy; R.sub.2 is hydrogen, hydroxy, alkoxy or aryloxy; or wherein R.sub.1 and R.sub.2 taken together is an aromatic ring; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is lower alkyl, substituted alkyl, alkenyl or alkynyl; X is amino, alkylamino, alkanoylamino, oxygen or a single bond; A is CH.sub.2 --CH.dbd.CH or a single bond; and n is an integer from 0 to 9, with the proviso that when A is a single bond, n is an integer from 1 to 9 including all stereoisomers thereof.These new compounds have been found to simultaneously inhibit the arachidonic acid enzymes 5-lipoxygenase and cyclooxygenase and as such are useful, for example, as antiinflammatory agents.
摘要翻译：式IMA的化合物，其中R 1是氢，羟基，烷氧基或芳氧基; R2是氢，羟基，烷氧基或芳氧基; 或其中R 1和R 2一起为芳环; R3是氢或低级烷基; R4是低级烷基，取代的烷基，烯基或炔基; X是氨基，烷基氨基，烷酰基氨基，氧或单键; A是CH 2 -CH = CH或单键; 且n为0至9的整数，条件是当A为单键时，n为1至9的整数，包括其所有立体异构体。已经发现这些新化合物同时抑制花生四烯酸5-脂氧合酶和环氧合酶，因此可用作例如抗炎剂。

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