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    • 1. 发明授权
      US5026729A Lipoxygenase inhibiting compounds 失效
    • Lipoxygenase inhibiting compounds
    • 脂氧合酶抑制化合物
    • US5026729A
    • 1991-06-25
    • US430841
    • 1989-11-02
    • Dee W. Brooks , James B. Summers , James H. Holms
    • Dee W. Brooks , James B. Summers , James H. Holms
    • C07C275/64
    • C07C275/64
    • Compounds having 5- and 12-lipoxygenase inhibitory activity have the structure ##STR1## where A is straight or branched divalent alkylene of from one to four carbon atoms, R.sub.1 is methyl, amino, or alkylamino of from one to six carbon atoms and the substituent group R.sub.2 is C.sub.1 -C.sub.2 alkyl.The group R.sub.3 is one or more substituents selected from hydrogen, alkyl of from one to six carbon atoms, alkoxy of from one to six carbon atoms, thioalkoxy of from one to six carbon atoms, halogen, cyano, and trihalomethyl, and R.sub.4 is one or more substituents selected from hydrogen, alkyl of from one to six carbon atoms, alkoxy of from one to six carbon atoms, thioalkoxy of from one to six carbon atoms, hydroxy, halogen, cyano, and trihalomethyl, with the proviso that when R.sub.1 is amino and A is >CHCH.sub.3, R.sub.3 and R.sub.4 may not both be hydrogen.The group designated M is hydrogen, a pharmaceutically acceptable cation, or a metabolically cleavable group. Pharmaceutical compositions and a method of inhibiting 5- and 12-lipoxygenase activity are also disclosed.
    • 具有5-和12-脂氧合酶抑制活性的化合物具有结构，其中A是1-4个碳原子的直链或支链二价亚烷基，R1是甲基，氨基或1-6个碳原子的烷基氨基， 基团R2是C1-C2烷基。 基团R3是一个或多个选自氢，一至六个碳原子的烷基，一个至六个碳原子的烷氧基，一个至六个碳原子的硫代烷氧基，卤素，氰基和三卤甲基的取代基，R4是一个 或更多取代基选自氢，一至六个碳原子的烷基，一至六个碳原子的烷氧基，一至六个碳原子的硫代烷氧基，羟基，卤素，氰基和三卤代甲基，条件是当R1为 氨基和A是> CHCH 3，R 3和R 4可以不都是氢。 指定为M的基团是氢，可药用阳离子或代谢可裂解基团。 还公开了药物组合物和抑制5-和12-脂肪氧合酶活性的方法。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 3. 发明授权
      US4992464A Heteroaryl N-hydroxy amides and ureas with polar substituents as 5-lipoxygenase inhibitors 失效
    • Heteroaryl N-hydroxy amides and ureas with polar substituents as 5-lipoxygenase inhibitors
    • US4992464A
    • 1991-02-12
    • US430710
    • 1989-11-01
    • Dee W. Brooks , James B. Summers , Karen E. Rodriques , Robert G. Maki , Joseph F. Dellaria , James H. Holms , Jimmie L. Moore
    • Dee W. Brooks , James B. Summers , Karen E. Rodriques , Robert G. Maki , Joseph F. Dellaria , James H. Holms , Jimmie L. Moore
    • C07D209/14 , C07D307/81 , C07D333/58 , A61K31/38 , C07D333/56
    • C07D333/58 , C07D209/14 , C07D307/81
    • Compounds, compositions a method of inhibiting lipoxygenase and treating related disorders are disclosed. The compounds are of the formula:Ar-A(R.sub.2).sub.n -N(OM)-CZ-R.sub.1whereinAr is ##STR1## where X is O, S, SO.sub.2 or NR.sub.3 ;R.sub.3 is hydrogen, alkyl, alkylaryl, alkoyl, alkylakoyl, aroyl or alkylaroyl;Y is hydrogen, halogen, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, arylalkenyl, --OR, --SR, --COOR, --COR, --CON(R).sub.2, --OCOR, --N(R).sub.2, --O(CH).sub.2, --SO.sub.2 R, --SO.sub.2 N(R).sub.2, --O(CH.sub.2).sub.p OR, --CN, --NO.sub.2, --O(CH).sub.p O(CH.sub.2).sub.p OR or --CF.sub.3 ;R is hydrogen, hydroxyl, alkyl, alkylaryl or aryl;m is 0 to 5;p is 1 to 4;A is C.sub.1 -C.sub.12 alkylene or C.sub.2 -C.sub.14 alkenylene;R.sub.2 is --OR, --SR, --COOR, --COR, --CON(R).sub.2, --OCOR, --N(R).sub.2, --O(CH.sub.2).sub.y CON(R).sub.2, --O(CH.sub.2).sup.y OR, --CN, --NO.sub.2, 1-tetrazolo, C.sub.4 -C.sub.8 cyclic amido, imidazolo, --O(CH.sub.2).sub.y O(CH.sub.2).sub.y OR, --CF.sub.3, --N(R) COCHR--NH(R), CONHCH(R)CO.sub.2 R, --OCOCHR-NH(R), --CR(NHR)CONR, --CR(NHR)COR, morpholino, --NH(CH.sub.2).sub.y OH, --N[(CH.sub.2).sub.y OH].sub.2, --N.sub.3, --SO.sub.2 N(R).sub.2, --N(R)COR, --N(R)COOR, --N(R)CON(R).sub.2, --C(.dbd.NOH)NHOH or --C(.dbd.NOH)NH.sub.2 where R is as defined above, y is 1 to 4 and --N(R).sub.2 can form a heterocyclic ring of 5-8 atoms;M is hydrogen, a pharmaceutically acceptable cation or a metabolically cleavable group;Z is oxygen or sulfur; andR.sub.1 us hydrogen, alkyl, alkenyl, --NR.sub.4 R.sub.5, --NCOR.sub.6 or --Q--(R.sub.2).sub.2 where R.sub.4 and R.sub.5 independently selected from the group consisting of hydrogen, hydroxyl, alkyl, substituted alkyl with 1-3 substituents selected from the group consisting of R.sub.2 as defined above, acyl, aryl and CON(R).sub.2 is as defined above, R.sub.6 is hydrogen alkyl, alkylaryl, aryl or NR.sub.4 R.sub.5 where R.sub.4 and R.sub.5 are as defined above and where NR.sub.4 R.sub.5 can form a heterocyclic ring of a 5-8 atoms, Q is alkyl, alkenyl or aryl and z is 0 to 3; provided when n is O, R.sub.1 is not hydrogen, alkyl, alkenyl, or NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are as defined above; and the pharmaceutically acceptable salts thereof.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 4. 发明授权
      US5124342A 4-hydroxythiazoles as 5-lipoxygenase inhibitors 失效
    • 4-hydroxythiazoles as 5-lipoxygenase inhibitors
    • US5124342A
    • 1992-06-23
    • US553836
    • 1990-07-18
    • Francis A. J. Kerdesky , James H. Holms , Dee W. Brooks
    • Francis A. J. Kerdesky , James H. Holms , Dee W. Brooks
    • C07D277/20 , A61K31/425 , A61K31/426 , A61K31/44 , A61P1/00 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D277/34 , C07D277/54 , C07D277/64 , C07D417/04
    • C07D417/04 , C07D277/34 , C07D277/54 , C07D277/64
    • A composition for the inhibition of lipoxygenase enzymes comprising a pharmaceutically acceptable carrier and a compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, arylalkenyl, reduced heteroaryl, and reduced heteroarylalkyl and substituted derivatives thereof having one or more substituents independently selected from the group consisting of halogen, alkyl, halosubstituted alkyl, aryl, arylalkyl, reduced heteroaryl, arylalkoxy, cyano, nitro, COR.sub.4, SO.sub.2 R.sub.4, NR.sub.5 R.sub.6, OR.sub.6, COCX.sub.1 X.sub.2 NR.sub.6 R.sub.7, CON(OH)R.sub.6, NR.sub.6 COR.sub.4, CR.sub.5 (NH.sub.2)CO.sub.2 R.sub.5, NHCX.sub.1 X.sub.2 CO.sub.2 R.sub.5, N(OH)CONR.sub.5 R.sub.6, N(OH)COR.sub.4, NHCONR.sub.5 R.sub.6, C(NOH)NHOH and CONHNR.sub.5 R.sub.6 ;R.sub.3 is selected from the group consisting of hydrogen, a pharmaceutically acceptable salt, COR.sub.4, COCX.sub.1 X.sub.2 NR.sub.6 R.sub.7, CR.sub.8 R.sub.9 OR.sub.10, CH.sub.2 CR.sub.8 (OR.sub.10)CH.sub.2 OR.sub.11 and SiR.sub.12 R.sub.13 R.sub.14 ;R.sub.4 is selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced heteroaryl, reduced heteroarylalkyl, OR.sub.5, NHCX.sub.1 X.sub.2 CO.sub.2 R.sub.5 and NR.sub.6 R.sub.7 ;R.sub.5 is selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, reduced heteroaryl, and reduced heteroarylalkyl;R.sub.6 and R.sub.7 are independently selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, reduced heteroaryl, reduced heteroarylalkyl and (CH.sub.2).sub.n OR.sub.5 where n is 2-4 and R.sub.5 is as defined above;R.sub.8, R.sub.9, R.sub.10 and R.sub.11 are independently selected from the group consisting of hydrogen, alkyl, aryl, arylalkyl and (CH.sub.2).sub.n OR.sub.5 or at least two of R.sub.8, R.sub.9, R.sub.10 and R.sub.11 together form a ring system containing 5-10 atoms wherein said ring system is carbocyclic, heterocyclic or reduced heterocyclic and R.sub.5 and n are as defined above;R.sub.12, R.sub.13 and R.sub.14 are independently selected from the group consisting of alkyl and aryl; andX.sub.1 and X.sub.2 are independently selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, aryl, and arylalkyl; and the acid addition salts thereof.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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