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1. 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。

2. 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。

3. 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。

4. 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。

5. 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。

6. 发明授权

US5304604A Hydroxamic acid collagenase inhibotors 失效
标题翻译：羟肟酸胶原酶抑制剂
公开(公告)号：US5304604A
公开(公告)日：1994-04-19
申请号：US674363
申请日：1991-04-15
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 , A61K31/395
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: R.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl, phenyl, phenyl(C.sub.1 -C.sub.6)alkyl, C.sub.1 -C.sub.6 alkylthiomethyl, phenylthiomethyl, substituted phenylthiomethyl, phenyl(C.sub.1 -C.sub.6)alkylthiomethyl or heterocyclylthiomethyl group; or 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;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)alkoxybenzyl or benzyloxy(C.sub.1 -C.sub.6)alkyl group;R.sup.4 represents a hydrogen atom or a methyl group;n is an integer from 1 to 6; andA represents the group --NH.sub.2, a substituted acyclic amine or a heterocyclic base;or a salt and/or N-oxide and/or (where the compound is a thio-compound) a sulphoxide or sulphone thereof 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： PCT No.PCT / GB89 / 01398 Sec。 371日期：1991年4月15日 102（e）日期1991年4月15日PCT提交1989年11月23日PCT公布。出版物WO90 / 05716 通式I的化合物：（*化学结构*）（I）其中：R1表示氢原子或C1-C6烷基，C1-C6烯基，苯基，苯基（C1-C6）烷基， C 1 -C 6烷基硫甲基，苯硫基甲基，取代的苯硫基甲基，苯基（C 1 -C 6）烷硫基甲基或杂环硫基甲基; 或R1表示-SRx，其中Rx表示基团（*化学结构*）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; R4代表氢原子或甲基; n是1至6的整数; 并且A表示基团-NH 2，取代的无环胺或杂环碱基; 或盐和/或N-氧化物和/或（其中化合物是硫代化合物），其亚砜或其砜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。

7. 发明授权

US5308864A 6-(hydronaphtyl-1-ethyl)-4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-ones and the corresponding hydroxy acids 失效
标题翻译： 6-（氢化萘基-1-乙基）-4-羟基-3,4,5,6-四氢-2H-吡喃-2-酮和相应的羟基酸
公开(公告)号：US5308864A
公开(公告)日：1994-05-03
申请号：US773657
申请日：1991-10-15
申请人： Christopher N. Lewis , Alan H. Davidson , Christopher D. Floyd , Jonathan P. Dickens
发明人： Christopher N. Lewis , Alan H. Davidson , Christopher D. Floyd , Jonathan P. Dickens
IPC分类号： A61K31/215 , A61K31/23 , A61K31/365 , A61K47/48 , A61P3/06 , A61P9/10 , C07C69/28 , C07C69/732 , C07C69/738 , C07D309/00 , C07D309/30 , A61K31/35 , A61K31/225
CPC分类号： C07C69/732 , C07C69/738 , C07D309/30
摘要： Compounds of either of general formulae (I) and (II), wherein: R.sup.1 represents a C.sub.1-8 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl(C.sub.1-8)alkyl, C.sub.2-8 alkenyl, or C.sub.1-6 alkyl substituted phenyl group; R.sup.2 represents a C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl group or a C.sub.1-5 alkyl, C.sub.2-5 alkenyl or C.sub.2-5 alkynyl group substituted with a substituted phenyl group; R.sup.3 represents a hydrogen atom or a substituent R.sup.4 or M; R.sup.4 represents a C.sub.1-5 alkyl group, or C.sub.1-5 alkyl group substituted with a group chosen from substituted phenyl, dimethylamino and acetylamino; R.sup.5 represents a hydrogen atom or a methyl or ethyl group except that when R.sup.2 is methyl then R.sup.5 is not methyl; M represents a cation capable of forming a pharmaceutically acceptable salt; Q represents C.dbd.O or CHOH; and each of a, b, c, and d, is independently a single or double bond except that when a and c are double bonds then b is a single bond; are inhibitors of the enzyme 24 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase), the rate limiting enzyme in the biosynthesis of cholesterol in mammals including man, and as such are useful in the treatment of hypercholesterolemia in general and arteriosclerosis, familiar hypercholesterolemia or hyperlipidemia in particular.
摘要翻译： PCT No.PCT / GB90 / 01030 Sec。 371日期1991年10月15日 102（e）1991年10月15日PCT PCT 1990年7月4日PCT公布。公开号WO91 / 00280 1991年1月10日。通式（I）和（II）的化合物，其中：R1表示C1-8烷基，C3-8环烷基，C3-8环烷基（C1-8）烷基，C2-8 烯基或C 1-6烷基取代的苯基; R2表示被取代的苯基取代的C1-8烷基，C2-8烯基，C2-8炔基或C1-5烷基，C2-5烯基或C2-5炔基; R3表示氢原子或取代基R4或M; R4表示C1-5烷基或被选自取代的苯基，二甲基氨基和乙酰氨基的基团取代的C1-5烷基; R5表示氢原子或甲基或乙基，不同之处在于当R 2为甲基时，R 5不是甲基; M表示能够形成药学上可接受的盐的阳离子; Q表示C = O或CHOH; a，b，c和d各自独立地为单键或双键，不同之处在于当a和c为双键时，b为单键; 是酶24-羟基-3-甲基戊二酰辅酶A还原酶（HMG-CoA还原酶）的抑制剂，包括人在内的哺乳动物的胆固醇生物合成中的限速酶，因此可用于一般治疗高胆固醇血症，动脉硬化，熟悉的高胆固醇血症或高脂血症。

8. 发明授权

US5314880A Benzimidazole derivatives 失效
标题翻译：苯并咪唑衍生物
公开(公告)号：US5314880A
公开(公告)日：1994-05-24
申请号：US752443
申请日：1991-09-30
申请人： Mark Whittaker , Christopher D. Floyd , Jonathan P. Dickens , Alan H. Davidson
发明人： Mark Whittaker , Christopher D. Floyd , Jonathan P. Dickens , Alan H. Davidson
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/44 , A61K31/445 , A61K31/454 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5355 , A61K31/675 , A61P7/02 , A61P9/00 , A61P11/00 , A61P13/02 , A61P15/00 , A61P17/00 , A61P27/02 , A61P29/00 , A61P37/00 , C07C211/52 , C07C309/65 , C07C309/66 , C07C309/72 , C07D235/02 , C07D235/06 , C07D235/08 , C07D235/10 , C07D235/18 , C07D235/26 , C07D235/28 , C07D401/04 , C07D401/12 , C07D403/04 , C07D417/04 , C07F9/6506 , C07D235/04 , C07D417/12
CPC分类号： C07D235/02 , C07C211/52 , C07C309/65 , C07C309/66 , C07C309/72 , C07D235/06 , C07D235/08 , C07D235/10 , C07D235/18 , C07D235/28 , C07D401/04 , C07D401/12 , C07D417/04
摘要： Compounds of general formula I: ##STR1## wherein: each of R.sup.1 -R.sup.8, k, and V represent disclosed functional groups that have been chosen such that all disclosed variations of compound I and their pharmaceutically and veterinarily acceptable acid addition salts and hydrates are antagonists of platelet activating factor (PAF) and as such are useful in the treatment or amelioration of various diseases or disorders mediated by PAF.
摘要翻译：通式I的化合物：其中：R1-R8，k和V各自表示所公开的官能团，其被选择为使得化合物I及其药学上和兽医学上可接受的酸加成盐和水合物的所有公开变体是血小板活化因子（PAF）的拮抗剂，因此可用于治疗或改善由PAF介导的各种疾病或病症。

9. 发明授权

US4743587A 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：US4743587A
公开(公告)日：1988-05-10
申请号：US880130
申请日：1986-07-07
申请人： Jonathan P. Dickens , David K. Donald , Geoffrey Kneen , William R. McKay
发明人： Jonathan P. Dickens , David K. Donald , Geoffrey Kneen , William R. McKay
IPC分类号： C12N9/99 , A61K31/16 , A61K31/165 , A61K38/43 , A61P29/00 , A61P43/00 , C07C233/02 , C07C237/00 , C07C237/06 , C07C237/20 , C07C237/22 , C07C259/06 , C07C83/10 , A61K31/085 , A61K31/185
CPC分类号： C07C233/02 , C07C237/00
摘要： Thid disclosure relates to a novel class of hydroxamic acid based collagenase inhibitor derivatives. The disclosure further relates to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions in the treatment of collagenase induced diseases.
摘要翻译：公开涉及一类新型异羟肟酸胶原酶抑制剂衍生物。本公开还涉及含有这些化合物的药物组合物以及这些化合物和组合物在治疗胶原酶诱导的疾病中的用途。

10. 发明授权

US4628104A Imidazole ketone derivatives 失效
标题翻译：咪唑酮衍生物
公开(公告)号：US4628104A
公开(公告)日：1986-12-09
申请号：US720917
申请日：1985-04-08
申请人： Jonathan P. Dickens , William R. McKay
发明人： Jonathan P. Dickens , William R. McKay
IPC分类号： C07D233/54 , C07D249/08 , C07D521/00 , C07D233/66 , C07D401/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： This disclosure relates to a class of novel compounds of the formula: ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl, phenyl or C.sub.1 -C.sub.4 alkylphenyl;R.sup.2 is C.sub.1 -C.sub.7 alkyl, benzyl, pyridyl, phenyl, halophenyl or dihalophenyl; andA is imidazol-1-yl, 1,2,4-triazol-1-yl or substituted imidazol-1-yl wherein the substituent is one or more groups selected from class consisting of C.sub.1 -C.sub.4 alkylthio and carboxy(C.sub.2 -C.sub.4 alkenyl);and pharmaceutically acceptable acid addition salts thereof. This invention further relates to pharmaceutical compositions containing the compounds and to the use of such compounds and compositions as anti-anaerobic agents.
摘要翻译：本公开涉及一类新的下式化合物：其中R 1是C 1 -C 4烷基，苯基或C 1 -C 4烷基苯基; R2是C1-C7烷基，苄基，吡啶基，苯基，卤代苯基或二卤代苯基; 和A是咪唑-1-基，1,2,4-三唑-1-基或取代的咪唑-1-基，其中取代基是一个或多个选自C 1 -C 4烷硫基和羧基（C 2 -C 4）烯基）; 及其药学上可接受的酸加成盐。本发明还涉及含有这些化合物的药物组合物以及这种化合物和组合物作为抗厌氧剂的用途。

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