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71. 发明授权

US5369123A Nitrogen-substituted mevinic acid derivatives useful as HMG-CoA reductase inhibitors 失效
标题翻译：可用作HMG-CoA还原酶抑制剂的氮取代的维甲酸衍生物
公开(公告)号：US5369123A
公开(公告)日：1994-11-29
申请号：US958849
申请日：1992-10-09
申请人： Dinos P. Santafianos , Kathleen M. Poss , Eric M. Gordon , Peggy J. McCann
发明人： Dinos P. Santafianos , Kathleen M. Poss , Eric M. Gordon , Peggy J. McCann
IPC分类号： C07C229/46 , C07C233/81 , C07C235/14 , C07C237/12 , C07C237/38 , C07C271/24 , C07C275/26 , C07C307/08 , C07D295/155 , C07D309/30 , A61K31/40 , A61K31/365 , C07C69/74
CPC分类号： C07D295/155 , C07C229/46 , C07C233/81 , C07C235/14 , C07C237/12 , C07C237/38 , C07C271/24 , C07C275/26 , C07C307/08 , C07D309/30 , C07C2102/28
摘要： Novel nitrogen-substituted mevinic acid derivatives which inhibit the activity of HMG-CoA reductase. Pharmaceutical compositions, and methods of use for the treatment or prevention of hypercholesterolemia, atherosclerosis, hyperlipoproteinaemia and hyperlipidemia are provided, as are novel methods for preparation and intermediate compounds.
摘要翻译：抑制HMG-CoA还原酶活性的新型含氮取代的维甲酸衍生物。还提供了用于治疗或预防高胆固醇血症，动脉粥样硬化，高脂蛋白血症和高脂血症的药物组合物和方法，以及新制备方法和中间体化合物。

72. 发明授权

US5256692A Sulfur-containing HMG-COA reductase inhibitors 失效
标题翻译：含硫HMG-COA还原酶抑制剂
公开(公告)号：US5256692A
公开(公告)日：1993-10-26
申请号：US817875
申请日：1992-01-07
申请人： Eric M. Gordon , Jelka Pluscec
发明人： Eric M. Gordon , Jelka Pluscec
IPC分类号： C07C317/46 , C07C323/52 , A01N37/10 , C07C317/00
CPC分类号： C07C323/52 , C07C317/46
摘要： Novel sulfur-containing compounds which inhibit the activity of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, having a sulfur-containing side-chain bonded to a hydrophobic anchor group through an acetylenic or ethylenic linkage. Pharmaceutical compositions, and methods of use for the treatment or prevention of hypercholesterolemia, atheroschlerosis, hyperlipoproteinaemia and hyperlipidemia are provided, as are novel methods for preparation and intermediate compounds.
摘要翻译：抑制3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶活性的新型含硫化合物，其具有通过炔属或烯键与疏水性锚定基键合的含硫侧链。还提供了用于治疗或预防高胆固醇血症，动脉粥样硬化，高脂蛋白血症和高脂血症的药物组合物和方法，以及制备新颖的方法和中间体化合物。

73. 发明授权

US5049577A 2-pyrrolidone substituted dihydroxy alkanoic, alkenoic and alkynoic acids, compositions and HMG-CoA reductase inhibition therewith 失效
标题翻译： 2-吡咯烷酮取代的二羟基链烷酸，链烯酸和炔酸，组合物和HMG-CoA还原酶抑制
公开(公告)号：US5049577A
公开(公告)日：1991-09-17
申请号：US471461
申请日：1990-01-29
申请人： Ravi K. Varma , Eric M. Gordon , Sam T. Chao
发明人： Ravi K. Varma , Eric M. Gordon , Sam T. Chao
IPC分类号： C07D207/26 , C07D209/96
CPC分类号： C07D207/26 , C07D209/96
摘要： Antihypercholesterolemic activity has been discovered in compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein: Z is ##STR2## X is lower alkyl, lower alkenyl, or lower alkenyl; R.sup.1 is hydrogen, alkyl, alkenyl, aryl, alkylaryl, or substituted aryl having one or more substituents; andone of R.sup.2 and R.sup.3 is hydrogen and the other is hydrogen, alkyl, alkenyl, aryl, alkylaryl or alkenyl aryl; or R.sup.2 and R.sup.3 are both lower alkyl; or R.sup.2 and R.sup.3 together complete a substituted or unsubstituted hydrocarbon ring that is cycloalkyl or cycloalkenyl with substituents as defined in the specification.
摘要翻译：抗高血胆固醇活性已经在下式化合物及其药学上可接受的盐中发现，其中：Z是低级烷基，低级链烯基或低级链烯基; R1是氢，烷基，烯基，芳基，烷基芳基或具有一个或多个取代基的取代的芳基; R2和R3中的一个是氢，另一个是氢，烷基，烯基，芳基，烷基芳基或烯基芳基; 或R 2和R 3均为低级烷基; 或者R 2和R 3一起完成取代或未取代的烃环，其是具有如说明书中定义的取代基的环烷基或环烯基。

74. 发明授权

US4904646A Phosphorus-containing HMG-COA reductase inhibitors 失效
标题翻译：含磷的HMG-COA还原酶抑制剂
公开(公告)号：US4904646A
公开(公告)日：1990-02-27
申请号：US182696
申请日：1988-04-18
申请人： Donald S. Karanewsky , Scott A. Biller , Eric M. Gordon
发明人： Donald S. Karanewsky , Scott A. Biller , Eric M. Gordon
IPC分类号： C07F9/30 , C07F9/32 , C07F9/36 , C07F9/38 , C07F9/40 , C07F9/44
CPC分类号： C07F9/4006 , C07F9/301 , C07F9/3211 , C07F9/36 , C07F9/3808 , C07F9/4407
摘要： Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesterolemic agents are provided which have the structure ##STR1## including salts thereof, wherein R is OH, lower alkoxy or lower alkyl; R.sup.x is H or alkyl;X is --O-- or --NH--;n is 1 or 2Z is a hydrophobic anchor, such as ##STR2## wherein the dotted lines represent optional double bonds. New intermediates used in preparing the above compounds, pharmaceutical compositions containing such compounds and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.
摘要翻译：提供了可用作胆固醇生物合成抑制剂并因此作为低胆固醇血症药物的化合物，其具有包括其盐的结构，其中R是OH，低级烷氧基或低级烷基; Rx是H或烷基; X是-O-或-NH-; n为1或2，Z为疏水锚，例如“IMAGE”或“IMAGE”，其中虚线表示任选的双键。还提供了用于制备上述化合物的新中间体，含有这些化合物的药物组合物和使用这些化合物抑制胆固醇生物合成的方法。

75. 依法登记的发明

USH725H Ureido amino and imino acids, compositions and methods for use 失效
标题翻译：脲基氨基和亚氨基酸，组合物和使用方法
公开(公告)号：USH725H
公开(公告)日：1990-01-02
申请号：US19469
申请日：1987-02-26
申请人： Eric M. Gordon
发明人： Eric M. Gordon
IPC分类号： C07C323/60 , C07D207/16 , C07D209/18 , C07D209/42 , C07D209/44 , C07D233/54 , C07D401/12 , C07D409/12 , C07D495/10
CPC分类号： C07D233/64 , C07C323/60 , C07D207/16 , C07D209/18 , C07D209/42 , C07D209/44 , C07D401/12 , C07D409/12 , C07D495/10
摘要： Compounds of the formula ##STR1## wherein X is various amino or imino acids and esters are disclosed. These compounds are useful 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.

76. 发明授权

US4849525A Phosphinylcycloalkylcarbonyl and phosphinylcycloalkenylcarbonyl dipeptides 失效
标题翻译：氧膦基环烷基羰基和氧膦基环烯基羰基二肽
公开(公告)号：US4849525A
公开(公告)日：1989-07-18
申请号：US98651
申请日：1987-09-21
申请人： Harold N. Weller, III , Eric M. Gordon
发明人： Harold N. Weller, III , Eric M. Gordon
IPC分类号： A61K38/55 , A61K31/675 , A61K38/00 , A61P9/12 , A61P43/00 , C07K5/06 , C07K5/08 , C07K14/81 , C12N9/99
CPC分类号： C07K5/06191 , C07K5/0827 , A61K38/00
摘要： Compounds of the formula ##STR1## and their pharmaceutically acceptable salts wherein Z completes a cycloalkyl ring, a substituted cycloalkyl ring, a cycloalkenyl ring, a substituted cycloalkenyl ring or a saturated heteroalkyl ring; R.sub.2 is lower alkyl, aralkyl or aminoalkyl and X is an amino or imino acid. The compounds possess angiotensin converting enzyme inhibition activity.
摘要翻译：其中Z完成环烷基环，取代的环烷基环，环烯基环，取代的环烯基环或饱和杂烷基环的式IMA化合物及其药学上可接受的盐; R2是低级烷基，芳烷基或氨基烷基，X是氨基或亚氨基酸。该化合物具有血管紧张素转换酶抑制活性。

77. 发明授权

US4782085A Arylhydroxamates and use thereof in treating allergies 失效
标题翻译：芳基羟基化合物及其在治疗过敏中的用途
公开(公告)号：US4782085A
公开(公告)日：1988-11-01
申请号：US78437
申请日：1987-07-27
申请人： Ravi K. Varma , Eric M. Gordon
发明人： Ravi K. Varma , Eric M. Gordon
IPC分类号： C07C69/76 , C07D213/56 , C07C81/00 , C07C83/10
CPC分类号： C07C69/76 , C07D213/56
摘要： Arylhydroxamates are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, aryl, lower alkenyl, cycloalkyl, or aralkyl;R.sup.2 is hydrogen, lower alkyl, aryl, cycloalkyl, alkanoyl or aroyl;m is 2 to 8; andZ is ##STR2## wherein R.sup.3 is OH, COOH ##STR3## These compounds are useful as inhibitors of .DELTA..sup.5 -lipoxygenase and as such are useful as antiallergy agents.
摘要翻译：提供了具有结构的芳基羟基化合物，其中R 1是氢，低级烷基，芳基，低级烯基，环烷基或芳烷基; R2是氢，低级烷基，芳基，环烷基，烷酰基或芳酰基; m为2〜8; Z是其中R 3是OH，COOH，这些化合物可用作DELTA5-脂肪氧合酶的抑制剂，因此可用作抗过敏剂。

78. 发明授权

US4707494A 7-oxabicyclo(2.2.1)heptane compounds useful in the treatment of inflammation 失效
标题翻译：可用于治疗炎症的7-氧杂二环（2.2.1）庚烷化合物
公开(公告)号：US4707494A
公开(公告)日：1987-11-17
申请号：US900564
申请日：1986-08-26
申请人： Ravi K. Varma , Carl P. Ciosek , Eric M. Gordon
发明人： Ravi K. Varma , Carl P. Ciosek , Eric M. Gordon
IPC分类号： A61K31/34 , A61P25/04 , A61P29/00 , C07D493/08 , A61K31/557 , C07D307/00
CPC分类号： C07D493/08
摘要： 7-Oxabicyclo(2.2.1)heptane analogs are disclosed having the general formula ##STR1## wherein R.sub.1 is lower alkyl, alkenyl, substituted alkenyl or alkynyl; R.sub.2 is lower alkyl, alkenyl or alkynyl; A is --CH.sub.2 --CH.dbd.CH-- or a single bond; X is --CH.sub.2, --CH(CH.sub.3) or --C(CH.sub.3).sub.2 ; 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.These new compounds have been found to be inhibitors of arachidonic acid cyclooxygenase and are therefore useful as antiinflammatory antipyretic and analgesic agents.
摘要翻译：公开了具有通式为“IMAGE”的7-氧杂双环（2.2.1）庚烷类似物，其中R 1是低级烷基，烯基，取代的链烯基或炔基; R2是低级烷基，烯基或炔基; A是-CH 2 -CH = CH-或单键; X是-CH 2，-CH（CH 3）或-C（CH 3）2; n为0〜9的整数，条件是当A为单键时，n为1〜9的整数，包括所有立体异构体。已经发现这些新化合物是花生四烯酸环氧合酶的抑制剂，因此可用作抗炎解热和止痛剂。

79. 发明授权

US4670541A 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：US4670541A
公开(公告)日：1987-06-02
申请号：US732331
申请日：1985-05-10
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 , C07K7/06 , C07K5/08
CPC分类号： C07K7/06 , C07K5/06026 , C07K5/06043 , C07K5/06078 , C07K5/0808 , 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（IMAGE）+ TR（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; 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。

80. 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。

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