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1. 发明授权

US5041567A Antibacterial monic acid derivatives 失效
标题翻译：抗菌单酸衍生物
公开(公告)号：US5041567A
公开(公告)日：1991-08-20
申请号：US276910
申请日：1988-11-28
申请人： Norman H. Rogers , Peter J. O'Hanlon , Graham Walker , Michael J. Crimmin
发明人： Norman H. Rogers , Peter J. O'Hanlon , Graham Walker , Michael J. Crimmin
IPC分类号： A01N43/16 , A61K8/49 , A61K31/41 , A61K31/42 , A61K31/425 , A61P31/00 , A61P31/04 , A61P33/02 , C07C205/45 , C07D261/00 , C07D261/08 , C07D261/18 , C07D263/00 , C07D263/32 , C07D275/00 , C07D277/00 , C07D277/22 , C07D303/00 , C07D309/00 , C07D333/00 , C07D333/22 , C07D333/28 , C07D407/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/14 , C07F9/653
CPC分类号： C07D277/22 , C07C205/45 , C07C255/00 , C07C309/00 , C07C323/00 , C07D261/08 , C07D261/18 , C07D263/32 , C07D333/22 , C07D333/28 , C07D407/06 , C07D409/14 , C07D413/14 , C07D417/14 , C07F9/653
摘要： ##STR1## wherein R
1 is unsubstituted or substituted phenyl, have been prepared which have antibacterial and/or antimycoplasmal activity.

2. 发明授权

US4861788A Antibacterial 1-normon-2-yl-heterocyclic compounds 失效
标题翻译：抗菌1-正二-2-基 - 杂环化合物
公开(公告)号：US4861788A
公开(公告)日：1989-08-29
申请号：US8893
申请日：1987-01-30
申请人： Norman H. Rogers , Graham Walker , Michael J. Crimmin , Peter J. O'Hanlon
发明人： Norman H. Rogers , Graham Walker , Michael J. Crimmin , Peter J. O'Hanlon
IPC分类号： A61K31/41 , A61K31/44 , A61K31/443 , A61K31/4433 , A61P15/14 , A61P31/00 , A61P31/04 , C07D405/06 , C07D405/14 , C07D407/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07F7/18
CPC分类号： C07D405/14 , C07D407/06 , C07D413/14
摘要： Compounds of formula (I): ##STR1## wherein ##STR2## is a 5-membered heterocyclic group having a 6-.pi.electron system, the five ring atoms being either(a) one carbon atom and four atoms selected from carbon and nitrogen,(b) two carbon atoms, two nitrogen atoms and one atom selected from oxygen and sulphur, or(c) four carbon atoms and one atom selected from oxygen and sulphurand R.sup.1 is a substituent on a carbon or nitrogen of ##STR3## selected from C.sub.1-20 alkyl, C.sub.2-8 alkenyl aryl, aralkyl and heterocyclyl, each of which may optionally be substituted; hydrogen and C.sub.3-7 cycloalkyl,and, where appropriate, R.sup.2 is a substituent on a carbon or nitrogen of ##STR4## and when present is the same or different to R.sup.1 and is selected from C.sub.1-20 alkyl, C.sub.2-8 alkenyl, aryl, aralkyl and heterocyclyl each of which may optionally be substituted; hydrogen and C.sub.3-7 cycloalkyl, have antibacterial and antimycoplasmal activity.
摘要翻译：式（I）的化合物：其中是具有6-pi电子系统的5元杂环基，5个环原子是（a）一个碳原子和选自碳的四个原子和氮，（b）两个碳原子，两个氮原子和一个选自氧和硫的原子，或（c）四个碳原子和一个选自氧和硫的原子，并且R1是

3. 发明授权

US4812470A Antibacterial monic acid derivatives 失效
标题翻译：抗菌单酸衍生物
公开(公告)号：US4812470A
公开(公告)日：1989-03-14
申请号：US469819
申请日：1983-02-25
申请人： Norman H. Rogers , Peter J. O'Hanlon , Graham Walker , Michael J. Crimmin
发明人： Norman H. Rogers , Peter J. O'Hanlon , Graham Walker , Michael J. Crimmin
IPC分类号： A01N43/16 , A61K8/49 , A61K31/41 , A61K31/42 , A61K31/425 , A61P31/00 , A61P31/04 , A61P33/02 , C07C205/45 , C07D261/00 , C07D261/08 , C07D261/18 , C07D263/00 , C07D263/32 , C07D275/00 , C07D277/00 , C07D277/22 , C07D303/00 , C07D309/00 , C07D333/00 , C07D333/22 , C07D333/28 , C07D407/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/14 , C07F9/653 , A01N43/78
CPC分类号： C07D277/22 , C07C205/45 , C07C255/00 , C07C309/00 , C07C323/00 , C07D261/08 , C07D261/18 , C07D263/32 , C07D333/22 , C07D333/28 , C07D407/06 , C07D409/14 , C07D413/14 , C07D417/14 , C07F9/653
摘要： A compound of the formula (I) ##STR1## wherein R is a group ##STR2## R.sup.1 is hydrogen, phenyl, C.sub.1-20 alkyl, C.sub.2-8 alkenyl or C.sub.2-8 alkynyl each of which may optionally be substituted; or C.sub.3-7 cycloalkyl,X is a divalent group --Y--C.dbd.C--, andY is oxygen or sulphur,have antibacterial and/or antimycoplasmal activity.
摘要翻译：式（I）化合物其中R是一个基团R 1是氢，苯基，C 1-20烷基，C 2-8链烯基或C 2-8炔基，各自可任选地被取代; 或C 3-7环烷基，X是二价基团-Y-C = C-，Y是氧或硫，具有抗细菌和/或抗支原体活性。

4. 发明授权

US4435583A 2-Halo-substituted monic acid A useful as antibacterial compounds 失效
标题翻译： 2-卤代取代的单酸A可用作抗菌化合物
公开(公告)号：US4435583A
公开(公告)日：1984-03-06
申请号：US447516
申请日：1982-12-07
申请人： Norman H. Rogers , Michael J. Crimmin
发明人： Norman H. Rogers , Michael J. Crimmin
IPC分类号： A61K31/35 , A61P31/04 , C07D407/06 , C07D309/06
CPC分类号： C07D407/06
摘要： Compounds of formula (I): ##STR1## wherein Y is halogen,R.sup.1 is hydrogen, a salt forming radical, alkyl or aralkyl,have antibacterial and/or antimycoplasmal activity.
摘要翻译：式（I）的化合物：其中Y是卤素，R 1是氢，成盐基，烷基或芳烷基，具有抗菌和/或抗支原体活性。

5. 发明授权

US5453438A Hydroxamic acid based collagenase inhibitors 失效
标题翻译：基于羟肟酸的胶原酶抑制剂
公开(公告)号：US5453438A
公开(公告)日：1995-09-26
申请号：US820664
申请日：1992-01-16
申请人： Colin Campion , Alan H. Davidson , Jonathan P. Dickens , Michael J. Crimmin
发明人： Colin Campion , Alan H. Davidson , Jonathan P. Dickens , Michael J. Crimmin
IPC分类号： A61K31/16 , A61K31/165 , A61K31/22 , A61K31/40 , A61K31/4015 , A61P17/00 , A61P43/00 , C07C20060101 , C07C237/22 , C07C259/06 , C07C317/44 , C07C323/51 , C07C327/38 , C07D207/00 , C07D207/26 , C07D207/38 , C07K5/06 , C07D207/27 , A61K31/505 , C07D401/12 , C07D405/12 , C07D409/12
CPC分类号： C07C259/06 , C07D207/38
摘要： Compounds of general formula I: ##STR1## are presented that have collagenase inhibition activity and are useful in the management of disease involving the tissue degradation and the promotion of would healing. Diseases involving tissue degradation include arthropathy (particularly rheumatoid arthritis), inflammation, dermatological diseases, bone resorption diseases and tumor invasion.
摘要翻译： PCT No.PCT / GB90 / 01117 Sec。 371日期：1992年1月16日 102（e）日期1992年1月16日PCT提交1990年7月20日PCT公布。出版物WO91 / 02716 PCT 日期为1991年3月7日。具有通式I：化合物（I）的化合物具有胶原酶抑制活性，可用于治疗涉及组织降解和促进愈合的疾病。涉及组织降解的疾病包括关节病（特别是类风湿性关节炎），炎症，皮肤病，骨吸收疾病和肿瘤侵袭。

6. 发明授权

US5525629A Inhibition of cytokine production 失效
标题翻译：抑制细胞因子产生
公开(公告)号：US5525629A
公开(公告)日：1996-06-11
申请号：US146083
申请日：1993-11-04
申请人： Michael J. Crimmin , William A. Galloway , Andrew J. Gearing
发明人： Michael J. Crimmin , William A. Galloway , Andrew J. Gearing
IPC分类号： A61K31/16 , A61K31/165 , A61K31/215 , A61K31/38 , A61K31/381 , A61P1/02 , A61P7/00 , A61P9/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/00 , A61P43/00 , C07C315/04 , C07C317/44 , C07C317/46 , C07C319/20 , C07C323/52 , C07C323/60 , C07C323/62 , C07C323/63 , C07C327/32 , C07D333/34 , A61K31/265
CPC分类号： C07C323/60 , C07C317/44 , C07C327/32 , C07D333/34
摘要： Hydroxamic acid derivatives of formula (I): ##STR1## wherein R.sup.1 represents hydrogen or an (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxycarbonyl(C.sub.1 -C.sub.6)alkyl, phenyl, substituted phenyl, phenyl(C.sub.1 -C.sub.6)alkyl, heterocyclyl, (C.sub.1 -C.sub.6)alkylcarbonyl, phenacyl or substituted phenacyl group;R.sup.2 represents hydrogen or a (C.sub.1 -C.sub.6)alkyl, (C.sub.2 -C.sub.6)alkenyl, phenyl(C.sub.1 -C.sub.6)alkyl, cycloalkyl(C.sub.1 -C.sub.6)alkyl or cycloalkenyl(C.sub.1 -C.sub.6)alkyl group,R.sup.3 represents a group --CH.sub.2 CO.sub.2 (C.sub.1 -C.sub.4)alkyl or --CH.sub.2 CH.sub.2 CO.sub.2 (C.sub.1 -C.sub.4)alkyl;R.sup.4 represents hydrogen or a (C.sub.1 -C.sub.6)alkyl or phenyl(C.sub.1 -C.sub.6)alkyl group;R.sup.5 represents hydrogen or a methyl group;n is 0, 1 or 2;and A represents a (C.sub.1 -C.sub.6)hydrocarbon chain optionally substituted with one or more (C.sub.1 -C.sub.6)alkyl, phenyl, or substituted phenyl groups;or a salts, solvates or hydrates thereof, are inhibitors of tumour necrosis factor production and of matrix metalloproteinases.
摘要翻译： PCT No.PCT / GB93 / 00706 Sec。 371日期：1993年11月4日 102（e）日期1993年11月4日PCT 1993年4月5日PCT PCT。第WO93 / 20047号公报式（I）的羟氨基酸衍生物：（C1-C6）烷基，（C1-C6）烷氧基羰基（C1-C6）烷基，苯基，取代苯基，苯基（C1-C6）烷基，杂环基，（C1-C6）烷基羰基，苯甲酰甲基或取代的苯甲酰甲基; R2表示氢或（C1-C6）烷基，（C2-C6）烯基，苯基（C1-C6）烷基，环烷基（C1-C6）烷基或环烯基（C1-C6）烷基，R3表示基团-CH2CO2 （C 1 -C 4）烷基或-CH 2 CH 2 CO 2（C 1 -C 4）烷基; R4表示氢或（C1-C6）烷基或苯基（C1-C6）烷基; R5代表氢或甲基; n为0,1或2; 并且A表示任选被一个或多个（C 1 -C 6）烷基，苯基或取代的苯基取代的（C 1 -C 6）烃链; 或其盐，溶剂化物或水合物，是肿瘤坏死因子产生抑制剂和基质金属蛋白酶的抑制剂。

7. 发明授权

US5514677A Hydroxamic acid based collagenase inhibitors 失效
标题翻译：基于羟肟酸的胶原酶抑制剂
公开(公告)号：US5514677A
公开(公告)日：1996-05-07
申请号：US229154
申请日：1994-04-18
申请人： Alan H. Davidson , Jonathan P. Dickens , Michael J. Crimmin
发明人： Alan H. Davidson , Jonathan P. Dickens , Michael J. Crimmin
IPC分类号： C07D295/12 , A61K31/16 , A61K31/165 , A61K31/40 , A61K31/415 , A61K31/4184 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/454 , A61P17/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07C237/22 , C07C259/06 , C07C317/44 , C07C323/60 , C07D207/09 , C07D207/32 , C07D207/335 , C07D211/14 , C07D213/40 , C07D233/60 , C07D233/61 , C07D235/14 , C07D295/13 , C07D521/00 , A61K31/13
CPC分类号： C07D207/335 , C07C237/22 , C07C259/06 , C07D207/09 , C07D213/40 , C07D231/12 , C07D233/56 , C07D235/14 , C07D249/08 , C07D295/13
摘要： Compounds of general formula I: ##STR1## wherein: A represents the group --NH.sub.2, a substituted acyclic amine or a heterocyclic base;have collagenase inhibition activity and are useful in the management of disease involving tissue degradation and/or the promotion of wound healing. Diseases involving tissue degradation include arthropathy (particularly rheumatoid arthritis), inflammation, dermatological diseases, bone resorption diseases and tumour invasion.
摘要翻译：通式I的化合物：其中：A表示基团-NH 2，取代的无环胺或杂环碱基; 具有胶原酶抑制活性，并且可用于治疗涉及组织降解和/或促进伤口愈合的疾病。涉及组织降解的疾病包括关节病（特别是类风湿性关节炎），炎症，皮肤病，骨吸收疾病和肿瘤侵袭。

8. 发明授权

US5530161A Hydroxamic acid based collagenase inhibitors 失效
标题翻译：基于羟肟酸的胶原酶抑制剂
公开(公告)号：US5530161A
公开(公告)日：1996-06-25
申请号：US195818
申请日：1994-02-14
申请人： Colin Campion , Alan H. Davidson , Jonathan P. Dickens , Michael J. Crimmin
发明人： Colin Campion , Alan H. Davidson , Jonathan P. Dickens , Michael J. Crimmin
IPC分类号： C07C317/44 , C07C323/60 , C07C327/32 , C07D333/34 , C07C259/04 , A61K31/19
CPC分类号： C07D333/34 , C07C317/44 , C07C323/60 , C07C327/32
摘要： Compounds of general formula I: ##STR1## wherein: R.sup.1 represents a C.sub.1 -C.sub.6 alkyl, phenyl, thiophenyl, substituted phenyl, phenyl(C.sub.1 -C.sub.6)alkyl, heterocyclyl, (C.sub.1 -C.sub.6)alkylcarbonyl phenacyl or substituted phenacyl group; or, when n=O, R.sup.1 represents SR.sup.x, wherein R.sup.x represents a group: ##STR2## R.sup.2 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl, phenyl(C.sub.1 -C.sub.6)alkyl, cycloalkyl(C.sub.1 -C.sub.6)alkyl or cycloalkenyl(C.sub.1 -C.sub.6)alkyl group;R.sup.3 represents an amino acid residue with R or S stereochemistry or a C.sub.1 -C.sub.6 alkyl, benzyl, (C.sub.1 -C.sub.6 alkoxy)benzyl or benzyloxy(C.sub.1 -C.sub.6 alkyl) group;R.sup.4 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group;R.sup.5 represents a hydrogen atom or a methyl group;n is an integer having the value 0, 1 or 2; andA represents a C.sub.1 -C.sub.6 hydrocarbon chain, optionaly substituted with one or more C.sub.1 -C.sub.6 alkyl, phenyl or substituted phenyl groups;and their salts and N-oxides are collagenase inhibitors are and useful in the management of disease involving tissue degradation and/or the promotion of wound healing. Diseases involving tissue degradation include arthropathy (particularly rheumatoid arthritis), inflammation, dermatological diseases, bone resorption diseases and tumor invasion.
摘要翻译：通式I的化合物：其中：R1表示C1-C6烷基，苯基，噻吩基，取代的苯基，苯基（C1-C6）烷基，杂环基，（C1-C6）烷基羰基苯甲酰甲基或取代的苯甲酰甲基 ; 或者当n = O时，R1表示SRx，其中Rx表示一个基团：R 2表示氢原子或C 1 -C 6烷基，C 1 -C 6烯基，苯基（C 1 -C 6）烷基，环烷基（C 1 -C 6 ）烷基或环烯基（C 1 -C 6）烷基; R3表示具有R或S立体化学的氨基酸残基或C1-C6烷基，苄基，（C1-C6烷氧基）苄基或苄氧基（C1-C6烷基）基团; R4表示氢原子或C1-C6烷基; R5表示氢原子或甲基; n是0或1或2的整数; 且A代表C1-C6烃链，任选被一个或多个C 1 -C 6烷基，苯基或取代的苯基取代; 其盐和N-氧化物是胶原酶抑制剂，并且可用于治疗涉及组织降解和/或促进伤口愈合的疾病。涉及组织降解的疾病包括关节病（特别是类风湿性关节炎），炎症，皮肤病，骨吸收疾病和肿瘤侵袭。

9. 发明授权

US5240958A Hydroxamic acid based collagenase inhibitors 失效
标题翻译：基于羟基酸的胶原蛋白抑制剂
公开(公告)号：US5240958A
公开(公告)日：1993-08-31
申请号：US689848
申请日：1991-07-08
申请人： Colin Campion , Alan H. Davidson , Jonathan P. Dickens , Michael J. Crimmin
发明人： Colin Campion , Alan H. Davidson , Jonathan P. Dickens , Michael J. Crimmin
IPC分类号： A61K31/16 , A61K31/13 , A61K31/165 , A61K31/21 , A61K31/215 , A61K31/38 , A61K31/381 , A61P3/00 , A61P17/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07C317/44 , C07C317/48 , C07C317/50 , C07C323/52 , C07C323/60 , C07C323/62 , C07C327/32 , C07D333/34
CPC分类号： C07C323/52 , C07C317/44 , C07C327/32 , C07D333/34
摘要： Compounds of general formula I: ##STR1## wherein: R.sup.1 represents a C.sub.1 -C.sub.6 alkyl, phenyl, thiophenyl, substituted phenyl, phenyl(C.sub.1 -C.sub.6)alkyl, heterocyclyl, (C.sub.1 -C.sub.6)alkylcarbonyl phenacyl or substituted phenacyl group; or, when n=O, R.sup.1 represents SR.sup.x, wherein R.sup.x represents a group: ##STR2## R.sup.2 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl, phenyl (C.sub.1 -C.sub.6) alkyl, cycloalkyl(C.sub.1 -C.sub.6)alkyl or cycloalkenyl(C.sub.1 -C.sub.6)alkyl group;R.sup.3 represents an amino acid residue with R or S stereochemistry or a C.sub.1 -C.sub.6 alkyl, benzyl, (C.sub.1 -C.sub.6 alkoxy)benzyl or benzyloxy(C.sub.1 -C.sub.6 alkyl) group;R.sup.4 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group;R.sup.5 represents a hydrogen atom or a methyl group;n is an integer having the value 0, 1 or 2; andA represents a C.sub.1 -C.sub.6 hydrocarbon chain, optionaly substituted with one or more C.sub.1 -C.sub.6 alkyl, phenyl or substituted phenyl groups;and their salts and N-oxides are collagenase inhibitors are and useful in the management of disease involving tissue degradation and/or the promotion of wound healing. Diseases involving tissue degradation include arthropathy (particularly rheumatoid arthritis), inflammation, dermatological diseases, bone resorption diseases and tumour invasion.
摘要翻译： PCT No.PCT / GB89 / 01399 Sec。 371日期：1991年7月8日 102（e）日期1991年7月8日PCT提交1989年11月23日PCT公布。公开号WO90 / 05719 通式I的化合物：其中：R1表示C1-C6烷基，苯基，噻吩基，取代的苯基，苯基（C1-C6）烷基，杂环基，（C1-C6）烷基，烷基羰基苯甲酰甲基或取代苯甲酰甲基; 或者当n = O时，R1表示SRx，其中Rx表示一个基团：R 2表示氢原子或C 1 -C 6烷基，C 1 -C 6烯基，苯基（C 1 -C 6）烷基，环烷基（C 1 -C 6 ）烷基或环烯基（C 1 -C 6）烷基; R 3表示具有R或S立体化学的氨基酸残基或C1-C6烷基，苄基，（C1-C6烷氧基）苄基或苄氧基（C1-C6烷基）基团; R4表示氢原子或C1-C6烷基; R5表示氢原子或甲基; n是0或1或2的整数; 且A代表C1-C6烃链，任选被一个或多个C 1 -C 6烷基，苯基或取代的苯基取代; 其盐和N-氧化物是胶原酶抑制剂，并且可用于治疗涉及组织降解和/或促进伤口愈合的疾病。涉及组织降解的疾病包括关节病（特别是类风湿性关节炎），炎症，皮肤病，骨吸收疾病和肿瘤侵袭。

10. 发明授权

US5310763A Hydroxamino acid based collagenase inhibitors 失效
标题翻译：羟基氨基酸胶原酶抑制剂
公开(公告)号：US5310763A
公开(公告)日：1994-05-10
申请号：US048413
申请日：1993-04-14
申请人： Colin Campion , Alan H. Davidson , Jonathan P. Dickens , Michael J. Crimmin
发明人： Colin Campion , Alan H. Davidson , Jonathan P. Dickens , Michael J. Crimmin
IPC分类号： A61K31/16 , A61K31/13 , A61K31/165 , A61K31/21 , A61K31/215 , A61K31/38 , A61K31/381 , A61P3/00 , A61P17/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07C317/44 , C07C317/48 , C07C317/50 , C07C323/52 , C07C323/60 , C07C323/62 , C07C327/32 , C07D333/34 , A61K31/19 , C07C327/04
CPC分类号： C07C323/52 , C07C317/44 , C07C327/32 , C07D333/34
摘要： Compounds of general formula I: ##STR1## wherein: R.sup.1 represents a C.sub.1 -C.sub.6 alkyl, phenyl, thiophenyl, substituted phenyl, phenyl(C.sub.1 -C.sub.6)alkyl, heterocyclyl, (C.sub.1 -C.sub.6)alkylcarbonyl phenacyl or substituted phenacyl group; or, when n=O, R.sup.1 represents SR.sup.x, wherein R.sup.x represents a group: ##STR2## R.sup.2 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl, phenyl(C.sub.1 -C.sub.6)alkyl, cycloalkyl(C.sub.1 -C.sub.6)alkyl or cycloalkenyl(C.sub.1 -C.sub.6)alkyl group;R.sup.3 represents an amino acid residue with R or S stereochemistry or a C.sub.1 -C.sub.6 alkyl, benzyl, (C.sub.1 -C.sub.6 alkoxy)benzyl or benzyloxy(C.sub.1 -C.sub.6 alkyl) group;R.sup.4 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group;R.sup.5 represents a hydrogen atom or a methyl group;n is an integer having the value 0, 1 or 2; andA represents a C.sub.1 -C.sub.6 hydrocarbon chain, optionaly substituted with one or more C.sub.1 -C.sub.6 alkyl, phenyl or substituted phenyl groups;and their salts and N-oxides are collagenase inhibitors are and useful in the management of disease involving tissue degradation and/or the promotion of wound healing. Diseases involving tissue degradation include arthropathy (particularly rheumatoid arthritis), inflammation, dermatological diseases, bone resorption diseases and tumor invasion.
摘要翻译：通式I的化合物：其中：R1表示C1-C6烷基，苯基，噻吩基，取代的苯基，苯基（C1-C6）烷基，杂环基，（C1-C6）烷基羰基苯甲酰甲基或取代的苯甲酰甲基 ; 或者当n = O时，R1表示SRx，其中Rx表示一个基团：R 2表示氢原子或C 1 -C 6烷基，C 1 -C 6烯基，苯基（C 1 -C 6）烷基，环烷基（C 1 -C 6 ）烷基或环烯基（C 1 -C 6）烷基; R 3表示具有R或S立体化学的氨基酸残基或C1-C6烷基，苄基，（C1-C6烷氧基）苄基或苄氧基（C1-C6烷基）基团; R4表示氢原子或C1-C6烷基; R5表示氢原子或甲基; n是0或1或2的整数; 且A代表C1-C6烃链，任选被一个或多个C 1 -C 6烷基，苯基或取代的苯基取代; 其盐和N-氧化物是胶原酶抑制剂，并且可用于治疗涉及组织降解和/或促进伤口愈合的疾病。涉及组织降解的疾病包括关节病（特别是类风湿性关节炎），炎症，皮肤病，骨吸收疾病和肿瘤侵袭。

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