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    Heteroaryl N-hydroxy amides and ureas with polar substituents as 5-lipoxygenase inhibitors
    1.
    发明授权
    Heteroaryl N-hydroxy amides and ureas with polar substituents as 5-lipoxygenase inhibitors 失效

    公开(公告)号：US4992464A

    公开(公告)日：1991-02-12

    申请号：US430710

    申请日：1989-11-01

    申请人： Dee W. Brooks ,  James B. Summers ,  Karen E. Rodriques ,  Robert G. Maki ,  Joseph F. Dellaria ,  James H. Holms ,  Jimmie L. Moore

    发明人： Dee W. Brooks ,  James B. Summers ,  Karen E. Rodriques ,  Robert G. Maki ,  Joseph F. Dellaria ,  James H. Holms ,  Jimmie L. Moore

    IPC分类号： C07D209/14 ,  C07D307/81 ,  C07D333/58 ,  A61K31/38 ,  C07D333/56

    CPC分类号： C07D333/58 ,  C07D209/14 ,  C07D307/81

    摘要： 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.

    Lipoxygenase inhibiting compounds
    3.
    发明授权
    Lipoxygenase inhibiting compounds 失效
    脂氧合酶抑制化合物

    公开(公告)号：US5026729A

    公开(公告)日：1991-06-25

    申请号：US430841

    申请日：1989-11-02

    申请人： Dee W. Brooks ,  James B. Summers ,  James H. Holms

    发明人： Dee W. Brooks ,  James B. Summers ,  James H. Holms

    IPC分类号： C07C275/64

    CPC分类号： C07C275/64

    摘要： 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.

    摘要翻译： 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。

    Indole-,benzofuran-,and benzothiophene-containing lipoxygenase-inhibiting compounds
    6.
    发明授权
    Indole-,benzofuran-,and benzothiophene-containing lipoxygenase-inhibiting compounds 失效
    含吲哚，苯并呋喃和苯并噻吩的脂氧合酶抑制化合物

    公开(公告)号：US5250565A

    公开(公告)日：1993-10-05

    申请号：US823411

    申请日：1992-01-21

    申请人： Dee W. Brooks ,  James B. Summers

    发明人： Dee W. Brooks ,  James B. Summers

    IPC分类号： C07D209/14 ,  C07D307/81 ,  C07D333/58 ,  A61K31/38 ,  A61K31/34 ,  C07D209/04 ,  C07D333/52

    CPC分类号： C07D209/14 ,  C07D307/81 ,  C07D333/58

    摘要： Pro-drugs of potent 5-lipoxygenase inhibiting compounds comprise compounds of the formula ##STR1## in which A is an alkylene or alkenylene group, X is oxygen, sulfur, sulfoxyl, or substituted nitrogen, and Y is a group which includes substituted or unsubstituted carbocyclic or substituted or unsubstituted heterocyclic aryl. R.sup.1 is an alkyl, alkenyl, amino, alkylamino, dialkylamino, or hydroxyamino group or an amine group bearing a metabolically cleavable leaving group. M is hydrogen, a pharmaceutically acceptable cation or a metabolically cleavable leaving group, with the proviso that either M or R.sup.1 must bear a metabolically cleavable leaving group.

    摘要翻译： 有效的5-脂氧合酶抑制化合物的前药包括其中A为亚烷基或亚烯基的式（IMAGE）化合物，X为氧，硫，亚砜基或取代的氮，Y为包括取代或未取代的基团 碳环或取代或未取代的杂环芳基。 R 1是烷基，烯基，氨基，烷基氨基，二烷基氨基或羟基氨基或具有代谢可切割离去基团的胺基。 M是氢，药学上可接受的阳离子或代谢可切割的离去基团，条件是M或R 1必须承载代谢可切割的离去基团。

    Dibenzofuran lipoxygenase inhibiting compounds, compositions and use
    9.
    发明授权
    Dibenzofuran lipoxygenase inhibiting compounds, compositions and use 失效
    二苯并呋喃脂氧合酶抑制化合物，组合物和用途

    公开(公告)号：US4769387A

    公开(公告)日：1988-09-06

    申请号：US120301

    申请日：1987-11-13

    申请人： James B. Summers ,  Jimmie L. Moore

    发明人： James B. Summers ,  Jimmie L. Moore

    IPC分类号： C07D209/86 ,  C07D307/91 ,  C07D333/76 ,  A61K31/34

    CPC分类号： C07D307/91 ,  C07D209/86 ,  C07D333/76

    摘要： Compounds of the formula: ##STR1## wherein R.sub.1 is (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl, (3) C.sub.2 to C.sub.4 alkenyl, or (4) NR.sub.2 R.sub.3, wherein R.sub.2 and R.sub.3 are independently selected from hydrogen, C.sub.1 to C.sub.4 alkyl and hydroxyl, but R.sub.2 and R.sub.3 are not simultaneously hydroxyl;X is (1) oxygen, (2) sulfur, (3) SO.sub.2, or (4) NR.sub.4, wherein R.sub.4 is (1) hydrogen, (2) C.sub.1 to C.sub.6 alkyl, (3) C.sub.1 to C.sub.6 alkoyl or (4) aroyl;A is selected from C.sub.1 to C.sub.6 alkylene and C.sub.2 to C.sub.6 alkenylene;n is 0-4;Y is selected independently at each occurrence from (1) hydrogen, (2) halogen, (3) hydroxy, (4) cyano, (5) halosubstituted alkyl, (6) C.sub.1 to C.sub.12 alkyl, (7) C.sub.2 to C.sub.12 alkenyl, (8) C.sub.1 to C.sub.12 alkoxy, (9) C.sub.3 to C.sub.8 cycloalkyl, (10) aryl, (11) aryloxy, (12) aroyl, (13) C.sub.1 to C.sub.12 arylalkyl, (14) C.sub.2 to C.sub.12 arylalkenyl, (15) C.sub.1 to C.sub.12 arylalkoxy, (16) C.sub.1 to C.sub.12 arylthioalkoxy, and substituted derivatives fo (17) aryl, (18) aryloxy, (19) aroyl, (20) C.sub.1 to C.sub.12 arylalkyl, (21) C.sub.2 to C.sub.12 arylalkenyl, (22) C.sub.1 to C.sub.12 arylalkoxy, or (23) C.sub.1 to C.sub.12 arylthioalkoxy, wherein substituents are selected from halo, nitro, cyano, C.sub.1 to C.sub.12 alkyl, alkoxy, and halosubstituted alkyl;and M is hydrogen, a pharmaceutically acceptable cation, aroyl, or C.sub.1 to C.sub.12, alkoyl are potent inhibitors of 5- and/or 12-lipoxygenase enzymes. Also disclosed are lipoxygenase inhibiting compositions and a method of inhibiting lipoxygenase.

    摘要翻译： 其中R 1为（1）氢，（2）C 1至C 4烷基，（3）C 2至C 4烯基或（4）NR 2 R 3的化合物，其中R 2和R 3独立地选自氢，C 1至 C4烷基和羟基，但R2和R3不同时为羟基; X为（1）氧，（2）硫，（3）SO2或（4）NR4，其中R4为（1）氢，（2）C1至C6烷基，（3）C1至C6烷酰基或（4） 芳酰基 A选自C1至C6亚烷基和C2至C6亚烯基; n为0-4; 在（1）氢，（2）卤素，（3）羟基，（4）氰基，（5）卤代烷基，（6）C1至C12烷基，（7）C2至C12烯基， （8）C1至C12烷氧基，（9）C3至C8环烷基，（10）芳基，（11）芳氧基，（12）芳酰基，（13）C1至C12芳烷基，（14）C2至C12芳基烯基，（15） （17）芳基，（18）芳氧基，（19）芳酰基，（20）C1〜C12芳基烷基，（21）C2〜C12芳基烯基，（22）C1〜C12芳基烷氧基，（16）C1〜C12芳基硫代烷氧基， ）C 1 -C 12芳基烷氧基或（23）C 1至C 12芳硫基烷氧基，其中取代基选自卤素，硝基，氰基，C 1至C 12烷基，烷氧基和卤代烷基; 和M是氢，药学上可接受的阳离子，芳酰基或C1至C12烷酰基是5-和/或12-脂肪氧合酶的有效抑制剂。 还公开了脂氧合酶抑制组合物和抑制脂氧合酶的方法。