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31. 发明授权

US06451823B1 Use of substituted N-phenoxy-N-phenyl aminoalcohol compounds for inhibiting cholesteryl ester transfer protein activity 失效
标题翻译：使用取代的N-苯氧基-N-苯基氨基醇化合物抑制胆固醇酯转移蛋白活性
公开(公告)号：US06451823B1
公开(公告)日：2002-09-17
申请号：US09990645
申请日：2001-11-14
申请人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
发明人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
IPC分类号： C07C23300
CPC分类号： C07C323/25 , B01D2201/345 , C07B2200/07 , C07C215/08 , C07C215/16 , C07C217/58 , C07C217/84 , C07C217/88 , C07C217/90 , C07C217/92 , C07C219/06 , C07C219/28 , C07C219/34 , C07C225/22 , C07C229/38 , C07C229/52 , C07C229/60 , C07C233/25 , C07C233/43 , C07C233/69 , C07C233/80 , C07C235/20 , C07C235/24 , C07C235/56 , C07C237/30 , C07C237/38 , C07C255/13 , C07C255/21 , C07C255/24 , C07C255/54 , C07C255/58 , C07C271/28 , C07C275/34 , C07C275/40 , C07C311/21 , C07C311/58 , C07C317/32 , C07C317/36 , C07C323/19 , C07C323/20 , C07C323/31 , C07C323/32 , C07C323/37 , C07C323/44 , C07C323/65 , C07C327/30 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/18 , C07D207/335 , C07D209/82 , C07D213/38 , C07D213/62 , C07D225/08 , C07D239/26 , C07D239/34 , C07D251/46 , C07D257/04 , C07D263/04 , C07D265/14 , C07D295/088 , C07D295/108 , C07D295/135 , C07D295/192 , C07D307/04 , C07D307/38 , C07D333/20 , C07D333/28 , C07D491/10
摘要： The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenoxy-N-phenyl aminoalcohols. A preferred specific N-phenoxy-N-phenyl aminoalcohol is the compound:
摘要翻译：本发明涉及可用作胆固醇酯转移蛋白（CETP;血浆脂质转移蛋白-1）的抑制剂的取代多环芳基和杂芳基叔杂烷基胺化合物的用途以及用于治疗动脉粥样硬化和其它冠状动脉疾病的化合物，组合物和方法。优选的叔杂烷基胺化合物是取代的N-苯氧基-N-苯基氨基醇。优选的特定N-苯氧基-N-苯基氨基醇是化合物：

32. 发明申请

US20020103256A1 Pesticidal and parasiticidal use of 1-aryl-1-(substituted thio, sulfinyl and sulfonyl)-2-nitroethane compounds 失效
公开(公告)号：US20020103256A1
公开(公告)日：2002-08-01
申请号：US09920264
申请日：2001-08-01
申请人： American Cyanamid Company
发明人： William Wakefield Wood , Annmarie Enos
IPC分类号： A01N043/42 , A01N037/34 , A01N037/12
CPC分类号： C07D307/38 , A01N33/20 , A01N37/36 , A01N37/38 , A01N37/44 , A01N37/48 , A01N39/00 , A01N41/10 , A01N43/08 , A01N43/10 , A01N43/30 , A01N43/40 , C07D213/32 , C07D317/56 , C07D333/18 , C07D405/12
摘要： The present invention relates to the pesticidal use of 1-aryl-1-(substituted thio, sulfinyl and sulfonyl)-2-nitroethane compounds having the structural formula I 1

33. 发明授权

US06288086B1 N-hydroxy-2-(alkyl, aryl, or heteroaryl, sulfanyl, sulfinyl or sulfonyl)-3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors 失效
标题翻译： N-羟基-2-（烷基，芳基或杂芳基，硫烷基，亚磺酰基或磺酰基）-3-取代的烷基，芳基或杂芳基酰胺作为基质金属蛋白酶抑制剂
公开(公告)号：US06288086B1
公开(公告)日：2001-09-11
申请号：US09593918
申请日：2000-06-14
申请人： Aranapakam Mudumbai Venkatesan
发明人： Aranapakam Mudumbai Venkatesan
IPC分类号： A61K31445
CPC分类号： C07D209/48 , A61K31/165 , A61K31/192 , A61K31/341 , A61K31/351 , A61K31/381 , A61K31/40 , A61K31/4418 , A61K31/445 , A61K31/451 , A61K31/495 , A61K31/5375 , C07C317/44 , C07C317/46 , C07C323/60 , C07C2601/08 , C07C2601/18 , C07D207/12 , C07D211/20 , C07D211/54 , C07D211/62 , C07D211/66 , C07D213/32 , C07D213/56 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/89 , C07D215/14 , C07D215/36 , C07D231/18 , C07D233/64 , C07D233/78 , C07D233/84 , C07D235/28 , C07D239/26 , C07D257/04 , C07D263/58 , C07D277/36 , C07D277/74 , C07D285/14 , C07D295/088 , C07D307/10 , C07D307/38 , C07D307/64 , C07D309/12 , C07D333/18 , C07D333/28 , C07D333/34 , C07D409/04
摘要： Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection having the formula wherein R2 and R3 form a heterocyclic ring and A is S, S(O), or S(O)2, and R1 and R4 are defined herein.
摘要翻译：基质金属蛋白酶（MMPs）是一组涉及结缔组织和基底膜的病理破坏的酶。这些含锌的内肽酶由几种酶组成，包括胶原酶，基质溶胶蛋白和明胶酶。 TNF-α转化酶（TACE）是促炎细胞因子，从膜结合的TNF-α前体蛋白催化TNF-α的形成。预期MMP和TACE的小分子抑制剂具有治疗各种疾病状态的潜力。本发明提供用于治疗关节炎，肿瘤转移，组织溃疡，异常伤口愈合，牙周病，骨病，糖尿病的基质金属蛋白酶（MMP）和TNF-α转换酶（TACE）的低分子量非肽抑制剂（胰岛素抵抗）和具有式R 2和R 3的HIV感染形成杂环，A是S，S（O）或S（O）2，并且R 1和R 4在本文中定义。

34. 发明授权

US06274590B1 Method of treating skin related conditions 失效
标题翻译：治疗皮肤相关病症的方法
公开(公告)号：US06274590B1
公开(公告)日：2001-08-14
申请号：US09661719
申请日：2000-09-14
申请人： John J. Talley , Stephen R Bertenshaw , Paul W Collins , Thomas D. Penning , David B. Reitz , Roland S Rogers
发明人： John J. Talley , Stephen R Bertenshaw , Paul W Collins , Thomas D. Penning , David B. Reitz , Roland S Rogers
IPC分类号： A61K31381
CPC分类号： C07D307/38 , A61K31/341 , A61K31/365 , C07D307/58 , C07D333/16 , C07D333/18 , C07D333/28 , C07D333/38 , C07D409/04
摘要： A class of 3,4-diaryl substituted thiophene, derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: wherein Y is S; wherein X is one or two substituents selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R2 and R3 are independently aryl or heteroaryl; and wherein R2 and R3 are optionally substituted with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：一类3,4-二芳基取代的噻吩，其衍生物和类似物，含有它们的药物组合物和使用它们治疗炎症和炎症相关疾病的方法。特别感兴趣的化合物由式I定义：其中Y是S; 其中X是一个或两个选自氢，卤素，低级烷氧基羰基和羧基的取代基; 其中R2和R3独立地是芳基或杂芳基; 并且其中R2和R3任选地被一个或多个选自亚磺酰基，烷基磺酰基，卤素，低级烷氧基和低级烷基的基团取代; 或其药学上可接受的盐。

35. 发明授权

US5591869A Process for the preparation of methylene compounds and the novel compound 2-(2,4-Dichloro-5-fluorobenzyl)thiophene 失效
标题翻译：制备亚甲基化合物和新化合物2-（2,4-二氯-5-氟苄基）噻吩的方法
公开(公告)号：US5591869A
公开(公告)日：1997-01-07
申请号：US568050
申请日：1995-12-06
申请人： Helmut Fiege , Ferdinand Hagedorn
发明人： Helmut Fiege , Ferdinand Hagedorn
IPC分类号： C07B31/00 , C07C1/32 , C07C17/35 , C07D307/38 , C07D333/08 , C07D333/12
CPC分类号： C07D307/38 , C07B31/00 , C07D333/08 , C07D333/12
摘要： Methylene compounds are preferably prepared by reducing an aluminum halide complex of the formula ##STR1## in which R.sup.1 represents a C.sub.6 -C.sub.10 -aryl radical which is optionally substituted by 1 to 4 C.sub.1 -C.sub.4 -alkyl radicals, 1 to 4 fluorine, chlorine and/or bromine atoms, one C.sub.1 -C.sub.8 -alkoxy group and/or one acetoxy group, or represents a heteroaryl radical which is optionally substituted by one C.sub.1 -C.sub.4 -alkyl radical and/or one fluorine, chlorine or bromine atom and contains 5 to 10 C atoms and one O or S atom andR.sup.2 represents a C.sub.1 -C.sub.12 -alkyl radical which is optionally substituted by 1 to 5 fluorine, chlorine and/or bromine atoms, independently of R.sup.1 represents a radical as defined for R.sup.1 and, in the case where R.sup.1 =a C.sub.6 -C.sub.10 -aryl radical which is substituted by 1 to 4 fluorine, chlorine and/or bromine atoms, also represents a furyl or thienyl radical,Y represents fluorine, chlorine or bromine,with an amineborane of the formula ##STR2## in which R.sup.3 represents C.sub.1 -C.sub.4 -alkyl andR.sup.4 represents hydrogen or C.sub.1 -C.sub.4 -alkyl and/orwith sodium borohydride and/or with potassium borohydride.2-(2,4-Dichloro-5-fluorobenzyl)thiophene is obtainable in this way for the first time.
摘要翻译：亚甲基化合物优选通过还原任选被1至4个C 1 -C 4烷基，1至4个氟，氯和/或溴原子，一个C 1 -C 8 - 烷氧基取代的式偕基的卤化铝配合物和/或一个乙酰氧基，或表示任选被一个C 1 -C 4 - 烷基和/或一个氟，氯或溴原子取代且含有5至10个C原子和一个O或S原子且R 2表示任选被1至5个氟，氯和/或溴原子取代的C1-C12-烷基，独立于R1表示对R1定义的基团，并且在R1 = C6-C10芳基的情况下，其中被1至4个氟，氯和/或溴原子取代，也代表呋喃基或噻吩基，Y代表氟，氯或溴，与式（III）的胺硼烷反应，其中R 3表示C 1 -C 4 - 烷基和R 4表示氢或C 1 -C 4烷基和/或与硼氢化钠 ydride和/或用硼氢化钾。 2-（2,4-二氯-5-氟苄基）噻吩可以首次以这种方式获得。

36. 发明授权

US5550142A Phenyl heterocycles as cox-2 inhibitors 失效
标题翻译：苯基杂环作为cox-2抑制剂
公开(公告)号：US5550142A
公开(公告)日：1996-08-27
申请号：US438130
申请日：1995-05-08
申请人： Yves Ducharme , Jacques Y. Gauthier , Petpiboon Prasit , Yves Leblanc , Zhaoyin Wang , Serge Leger , Michel Therien
发明人： Yves Ducharme , Jacques Y. Gauthier , Petpiboon Prasit , Yves Leblanc , Zhaoyin Wang , Serge Leger , Michel Therien
IPC分类号： C07D333/06 , A61K31/00 , A61K31/10 , A61K31/12 , A61K31/122 , A61K31/18 , A61K31/19 , A61K31/255 , A61K31/34 , A61K31/341 , A61K31/35 , A61K31/351 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/4015 , A61K31/425 , A61K31/426 , A61K31/66 , A61P1/00 , A61P1/02 , A61P1/04 , A61P7/04 , A61P11/06 , A61P15/00 , A61P17/02 , A61P19/00 , A61P19/02 , A61P21/00 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/16 , A61P35/00 , A61P43/00 , C07C20060101 , C07C13/08 , C07C13/10 , C07C305/18 , C07C307/02 , C07C311/15 , C07C311/16 , C07C311/29 , C07C311/37 , C07C311/46 , C07C311/49 , C07C311/51 , C07C317/10 , C07C317/24 , C07C323/29 , C07D207/26 , C07D207/333 , C07D207/38 , C07D207/444 , C07D207/448 , C07D275/02 , C07D277/02 , C07D277/22 , C07D277/24 , C07D277/26 , C07D307/33 , C07D307/38 , C07D307/58 , C07D309/32 , C07D333/04 , C07D333/12 , C07D333/16 , C07D333/18 , C07D333/24 , C07D333/38 , C07D333/40 , C07D405/04 , C07D407/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D503/04 , C07F9/40 , C07F9/547 , C07F9/572 , C07F9/6506 , C07F9/653 , C07F9/6539 , C07F9/655
CPC分类号： C07D275/02 , C07C311/29 , C07C311/46 , C07C311/49 , C07C317/24 , C07D277/26 , C07D307/38 , C07D307/58 , C07D333/18 , C07D333/38 , C07D405/04 , C07C2101/08
摘要： The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
摘要翻译：本发明包括可用于治疗环氧合酶-2介导的疾病的新颖的式I化合物。本发明还包括用于治疗环氧合酶-2介导的疾病的某些药物组合物，其包含式I化合物。

37. 发明授权

US5481036A N-acylamino acid derivatives and their use 失效
标题翻译： N-酰基氨基酸衍生物及其用途
公开(公告)号：US5481036A
公开(公告)日：1996-01-02
申请号：US179195
申请日：1994-01-10
申请人： Hajime Morishima , Yutaka Koike , Masato Nakano , Shugo Atsuumi , Seiichi Tanaka , Kenji Matsuyama
发明人： Hajime Morishima , Yutaka Koike , Masato Nakano , Shugo Atsuumi , Seiichi Tanaka , Kenji Matsuyama
IPC分类号： A61K31/195 , A61K31/535 , C07C59/66 , C07C317/00 , C07C317/44 , C07C323/43 , C07D207/08 , C07D211/14 , C07D215/12 , C07D233/54 , C07D239/38 , C07D257/04 , C07D265/30 , C07D285/12 , C07D285/125 , C07D295/084 , C07D295/12 , C07D295/125 , C07D295/13 , C07D295/24 , C07D307/38 , C07D319/18 , C07D401/12 , C07F7/18 , C07C321/00
CPC分类号： C07D207/08 , C07C323/00 , C07C323/43 , C07C59/66 , C07D211/14 , C07D215/12 , C07D233/64 , C07D239/38 , C07D257/04 , C07D285/125 , C07D295/084 , C07D295/125 , C07D295/13 , C07D295/24 , C07D307/38 , C07D319/18 , C07D401/12 , C07F7/1856
摘要： An N-acylamino acid derivative of the formula: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.4 and R.sup.6 is hydrogen lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from to 4 hetero atoms; each of R.sup.3 and R.sup.5 is hydrogen or lower alkyl; A is --CH(OH)--(CH.sub.2).sub.q R.sup.7 wherein R.sup.7 is hydrogen, lower alkyl, cycloalkyl, cyloalkylalkyl, aryl, aralkyl, a monocyclic or bicyclic heterocyclic group containing from to 4 hereto atoms or --E--R.sup.10 wherein E is --S(O).sub.i -- wherein i is 0, 1 or 2, oxygen, --NR.sup.11 -- wherein R.sup.11 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, or ##STR2## wherein each of R.sup.12 and R.sup.13 is hydrogen, lower alkyl cycloalkyl, cycloalkylalkyl, aryl or aralkyl, and R.sup.10 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms provided that when R.sup.10 is hydrogen, i is 0, and a is an integer of from 0 to 5; or --CH.sub.2 --CHR.sup.8 --CO--R.sup.9 wherein R.sup.8 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms, and R.sup.9 is hydroxyl, --OX wherein X is alkyl, aryl, lower alkoxycarbonyloxyalkyl or 1-phthalidyl, or --N(Y.sup.1) (Y.sup.2) wherein each of Y.sup.1 and Y.sup.2 is hydrogen, lower alkyl, aryl, aralkyl or cycloalkyl, or Y and.sup.1 and Y.sup.2 form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may contain a further hereto atom; m is 0, 1 or 2; and n is an integer of from 1 to 5, provided that when R.sup.1 is hydrogen, m is 0; or a salt thereof, which is useful as hypotensive drugs.
摘要翻译：下式的N-酰基氨基酸衍生物：其中R 1，R 2，R 4和R 6各自为氢低级烷基，环烷基，环烷基烷基，芳基，芳烷基或含有4个杂原子的单环或双环杂环基原子 R 3和R 5各自为氢或低级烷基; A是-CH（OH） - （CH 2）q R 7，其中R 7是氢，低级烷基，环烷基，环烷基烷基，芳基，芳烷基，含有至4原子的单环或双环杂环基或-E-R 10，其中E是-S （O）i-其中i是0,1或2，氧，-NR 11 - ，其中R 11是氢，低级烷基，环烷基，环烷基烷基，芳基或芳烷基，或者其中R 12和R 13各自是氢，环烷基，环烷基烷基，芳基或芳烷基，R 10为含有1至4个杂原子的氢，低级烷基，环烷基，环烷基烷基，芳基，芳烷基或单环或双环杂环基，条件是当R 10为氢时，i为0，是从0到5的整数; 或-CH 2 -CHR 8 -CO-R 9，其中R 8是氢，低级烷基，环烷基，环烷基烷基，芳基，芳烷基或含有1至4个杂原子的单环或双环杂环基，并且R 9是羟基，，芳基，低级烷氧基羰氧基烷基或1-苯酞基，或-N（Y1）（Y2），其中Y1和Y2各自为氢，低级烷基，芳基，芳烷基或环烷基，或Y和1和Y2与相邻的氮原子一起形成可含有其它原子的5-或6-元杂环基; m为0,1或2; 且n为1至5的整数，条件是当R 1为氢时，m为0; 或其盐，其可用作降压药物。

38. 发明授权

US5466827A Use of thioalkanediones as aroma substances 失效
标题翻译：使用硫代烷二酮作为芳香物质
公开(公告)号：US5466827A
公开(公告)日：1995-11-14
申请号：US128440
申请日：1993-09-28
申请人： Heinz-Jurgen Bertram , Roland Emberger , Matthias Guntert , Peter Werkhoff
发明人： Heinz-Jurgen Bertram , Roland Emberger , Matthias Guntert , Peter Werkhoff
IPC分类号： A61K8/35 , A23L27/20 , A61Q13/00 , C07C323/22 , C07D213/70 , C07D307/38 , C07D307/64 , C07D333/18 , C07D333/34 , C11B9/00 , C07D333/32 , C07C49/105 , C07C319/00 , C07D307/02
CPC分类号： C07D213/70 , A23L27/20 , A23L27/204 , A23L27/2052 , A23L27/2054 , C07C323/22 , C07D307/38 , C07D307/64 , C07D333/18 , C07D333/34
摘要： Thioalkane .alpha.,.beta.-diketones have interesting organoleptic properties and are therefore suitable as aroma substances.
摘要翻译：硫代烷烃α，β-二酮具有有趣的感官特性，因此适合作为芳香物质。

39. 发明授权

US5424325A Aminoketone derivatives 失效
标题翻译：氨基酮衍生物
公开(公告)号：US5424325A
公开(公告)日：1995-06-13
申请号：US171695
申请日：1993-12-22
申请人： Ryoichi Ando , Naoko Ando , Hirokazu Masuda , Toshiro Sasaki , Yasuhiro Morinaka , Chizuko Takahashi , Yoshikuni Tamao , Akihiro Tobe
发明人： Ryoichi Ando , Naoko Ando , Hirokazu Masuda , Toshiro Sasaki , Yasuhiro Morinaka , Chizuko Takahashi , Yoshikuni Tamao , Akihiro Tobe
IPC分类号： C07D213/32 , C07D213/38 , C07D263/20 , C07D277/26 , C07D307/38 , C07D307/42 , C07D307/46 , C07D307/85 , C07D333/16 , C07D333/18 , C07D333/22 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12 , A61K31/34 , A61K31/425 , C07D213/30
CPC分类号： C07D263/20 , C07D213/32 , C07D213/38 , C07D277/26 , C07D307/38 , C07D307/42 , C07D307/46 , C07D307/85 , C07D333/16 , C07D333/18 , C07D333/22 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12
摘要： Aminoketone derivatives according to the present invention strongly inhibit thiol protease such as calpain, papain, cathepsin B, cathepsin H, cathepsin L or the like and have excellent properties concerning absorbance on oral administration, tissue distribution and cell membrane permeability. The aminoketone derivatives cart thus be used as therapeutic agents for treating muscular dystrophy, cataract, cardiac infarction, stroke, Alzheimer's disease, amyotrophy, osteoporosis and hypercalcemia and so on. It may also be used as therapeutic agents for preventing metastasis of cancer. In addition, the present derivatives are also applicable as intermediates for the preparation of ketone derivatives, which have inhibitory activity against thiol protease.
摘要翻译：根据本发明的氨基酮衍生物强烈地抑制硫蛋白酶如钙蛋白酶，木瓜蛋白酶，组织蛋白酶B，组织蛋白酶H，组织蛋白酶L等，并且对于口服给药，组织分布和细胞膜通透性的吸光度具有优异的性质。因此，氨基酮衍生物载体可用作治疗肌营养不良症，白内障，心肌梗塞，中风，阿尔茨海默病，肌萎缩，骨质疏松症和高钙血症等的治疗剂。它也可以用作预防癌转移的治疗剂。此外，本发明的衍生物也可用作制备对硫醇蛋白酶具有抑制活性的酮衍生物的中间体。

40. 发明授权

US5122523A N-acylamino acid derivatives and their pharmaceutical compositions 失效
标题翻译： N-亚氨基酸衍生物及其药物组合物
公开(公告)号：US5122523A
公开(公告)日：1992-06-16
申请号：US240725
申请日：1988-09-06
申请人： Hajime Morishima , Yutaka Koike , Masato Nakano , Shugo Atsuumi , Seiichi Tanaka , Kenji Matsuyama
发明人： Hajime Morishima , Yutaka Koike , Masato Nakano , Shugo Atsuumi , Seiichi Tanaka , Kenji Matsuyama
IPC分类号： A61K31/195 , A61K31/535 , C07C59/66 , C07C317/00 , C07C317/44 , C07C323/43 , C07D207/08 , C07D211/14 , C07D215/12 , C07D233/54 , C07D239/38 , C07D257/04 , C07D265/30 , C07D285/12 , C07D285/125 , C07D295/084 , C07D295/12 , C07D295/125 , C07D295/13 , C07D295/24 , C07D307/38 , C07D319/18 , C07D401/12 , C07F7/18
CPC分类号： C07D207/08 , C07C323/00 , C07C323/43 , C07C59/66 , C07D211/14 , C07D215/12 , C07D233/64 , C07D239/38 , C07D257/04 , C07D285/125 , C07D295/084 , C07D295/125 , C07D295/13 , C07D295/24 , C07D307/38 , C07D319/18 , C07D401/12 , C07F7/1856
摘要： An N-acylamino acid derivative of the formula: ##STR1## wherein the substituents are herein defined or a salt thereof, which is useful as hypotensive drugs.

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