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    • 1. 发明授权
      US4873259A Indole, benzofuran, benzothiophene containing lipoxygenase inhibiting compounds 失效
    • Indole, benzofuran, benzothiophene containing lipoxygenase inhibiting compounds
    • 吲哚，苯并呋喃，苯并噻吩含脂氧合酶抑制化合物
    • US4873259A
    • 1989-10-10
    • US138073
    • 1988-01-11
    • James B. Summers, Jr. , Bruce P. Gunn , Dee W. Brooks
    • James B. Summers, Jr. , Bruce P. Gunn , Dee W. Brooks
    • C07D209/14 , C07D307/81 , C07D333/58
    • C07D333/58 , C07D209/14 , C07D307/81
    • 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 (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl and (3) hydroxyl, but R.sub.2 and R.sub.3 are not simultaneously hydroxyl;wherein X is oxygen, sulfur, SO.sub.2, or 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, (4) aroyl, or (5) alkylsulfonyl;A is selected from C.sub.1 to C.sub.6 alkylene and C.sub.2 to C.sub.6 alkenylene;n is 1-5;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) C.sub.1 -C.sub.8 thioalkyl, (11) aryl, (12) aryloxy, (13) aroyl, (14) C.sub.1 to C.sub.12 arylalkyl, (15) C.sub.2 to C.sub.12 arylalkenyl, (16) C.sub.1 to C.sub.12 arylalkoxy, (17) C.sub.1 to C.sub.12 arylthioalkoxy, and substituted derivatives of (18) aryl, (19) aryloxy, (20) aroyl, (21) C.sub.1 to C.sub.12 arylalkyl, (22) C.sub.2 to C.sub.12 arylalkenyl, (23) C.sub.1 to C.sub.12 arylalkoxy, or (24) 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;Z is oxygen or sulfur;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 for inhibiting lipoxygenase activity.
    • 其中R 1是（1）氢，（2）C 1至C 4烷基，（3）C 2至C 4链烯基或（4）NR 2 R 3，其中R 2和R 3独立地选自（1）氢 ，（2）C1至C4烷基和（3）羟基，但R2和R3不同时为羟基; 其中X是氧，硫，SO 2或NR 4，其中R 4是（1）氢，（2）C 1至C 6烷基，（3）C 1至C 6烷酰基，（4）芳酰基或（5）烷基磺酰基; A选自C1至C6亚烷基和C2至C6亚烯基; n为1-5; 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）C1-C8硫代烷基，（11）芳基，（12）芳氧基，（13）芳酰基，（14）C1至C12芳烷基，（15） （18）芳基，（19）芳氧基，（20）芳酰基，（21）C1〜C12芳基烷基，（22）C1〜C12芳基烷氧基，（17）C1〜C12芳基烷氧基，（17） ）C 2至C 12芳基烯基，（23）C 1至C 12芳基烷氧基或（24）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; Z是氧或硫; 和M是氢，可药用阳离子，芳酰基或C 1至C 12烷酰基，是5-和/或12-脂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
    • 6. 发明授权
      US5183818A Arylalkylether and arylalkylthioether inhibitors of lipoxygenase enzyme activity 失效
    • Arylalkylether and arylalkylthioether inhibitors of lipoxygenase enzyme activity
    • 芳基烷基醚和芳烷基硫醚抑制剂的脂氧合酶活性
    • US5183818A
    • 1993-02-02
    • US750362
    • 1991-08-27
    • Dee W. Brooks , Andrew O. Stewart , Jonathan G. Martin
    • Dee W. Brooks , Andrew O. Stewart , Jonathan G. Martin
    • C07D307/38 , C07D307/42 , C07D333/16 , C07D333/34 , C07D333/56 , C07D495/04
    • C07D307/42 , C07D307/38 , C07D333/16 , C07D333/34 , C07D333/56 , C07D495/04
    • The present invention provides compounds having the structureY-Het-[Q.sub.1 ]-X-[Q.sub.2 ]-Zwhich inhibit the catalytic action of lipoxygenase enzymes, particularly 5-lipoxygenase, and thereby reduce the biosynthesis of leukotrienes B.sub.4, C.sub.4, D.sub.4, and E.sub.4.In the generic formula given above, X is oxygen or sulfur and Het is a heteroaryl group selected from the group consisting of furyl, thienyl, 2-, 3-, and 4-pyridyl, 2- and 3-benzo[b]furyl, 2- and 3-benzo[b]thienyl and thienothienyl.Y is one or two substituents independently selected from hydrogen, hydroxy, halogen, cyano, alkyl, haloalkyl, alkoxy, alkylthio, alkoxyaryl), alkylthioaryl, arylalkoxy, arylalkylthio, aryloxy, arylthio, alkylamido, cycloalkyl, alkanoyl, alkoxycarbonyl, amino, alkylamino, dialkylamino, and the following groups wherein R, at each occurrence, is independently selected from hydrogen and alkyl of from one to six carbon atoms: --CRROR, --NRC(O)R, --NRC(O)OR, and --C(O)NRR.The group Q.sub.1 is absent or is divalent alkylene of from one to six carbon atoms, and Q.sub.2 is divalent alkylene from from two to ten carbon atoms.The group Z is N(OR.sub.1)COR.sub.2 where R.sub.1 is selected from hydrogen or a pharmaceutically suitable salt. R.sub.2 is selected from hydrogen; alkyl; cycloalkyl; amino; alkylamino, optionally substituted by hydroxyl, halogen, alkoxy or carboxyl; dialkylamino in which the alkyl groups are independently are optionally substituted by hydroxyl, halogen, alkoxy or carboxyl; cycloalkylamino; 2-hydroxyethylamino; N-morpholino; N-thiomorpholino; N-piperazine; N'-alkyl-N-piperazine and cyclopropylmethylamino.
    • 本发明提供具有抑制脂氧合酶，特别是5-脂氧合酶的催化作用的结构为Y-Het- [Q1] -X- [Q2] -Z的化合物，从而减少白三烯B4，C4，D4的生物合成， 和E4。 在上述通式中，X是氧或硫，Het是选自呋喃基，噻吩基，2-，3-和4-吡啶基，2-和3-苯并[b]呋喃基的杂芳基， 2-和3-苯并[b]噻吩基和噻吩并噻吩基。 Y是一个或两个独立地选自氢，羟基，卤素，氰基，烷基，卤代烷基，烷氧基，烷硫基，烷氧基芳基），烷基硫代芳基，芳基烷氧基，芳基烷硫基，芳氧基，芳硫基，烷基酰氨基，环烷基，烷酰基，烷氧基羰基，氨基，烷基氨基， 二烷基氨基和下列基团，其中R 1在每次出现时独立地选自氢和1至6个碳原子的烷基：-CRROR，-NRC（O）R，-NRC（O）OR和-C（O ）NRR。 基团Q1不存在或为1至6个碳原子的二价亚烷基，Q 2为2至10个碳原子的二价亚烷基。 基团Z是N（OR 1）COR 2，其中R 1选自氢或药学上合适的盐。 R2选自氢; 烷基; 环烷基 氨基; 任选被羟基，卤素，烷氧基或羧基取代的烷基氨基; 其中烷基独立的二烷基氨基任选被羟基，卤素，烷氧基或羧基取代; 环烷基氨基; 2-羟基乙基氨基; N-吗啉代; N-硫代吗啉代 N-哌嗪; N'-烷基-N-哌嗪和环丙基甲基氨基。
    • 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
    • 9. 发明授权
      US5354865A Phenylmethyl derivatives having lipoxygenase inhibitory activity 失效
    • Phenylmethyl derivatives having lipoxygenase inhibitory activity
    • 具有脂氧合酶抑制活性的苯甲基衍生物
    • US5354865A
    • 1994-10-11
    • US942870
    • 1992-09-10
    • Joseph F. Dellaria , Linda J. Dorn , Dee W. Brooks
    • Joseph F. Dellaria , Linda J. Dorn , Dee W. Brooks
    • C07D305/06 , C07D309/04 , C07D309/06 , C07D309/10 , C07D405/12 , C07D235/26 , C07D215/227 , C07D265/36
    • C07D405/12 , C07D305/06 , C07D309/04 , C07D309/06 , C07D309/10
    • Compounds of the structure ##STR1## where Ar is optionally substituted carbocyclic aryl, 5- or 6-membered heterocyclic aryl, 10-membered bicyclic heterocyclic aryl containing one or two nitrogen atoms, 9- or 10-membered heterocyclic containing one or two nitrogen atoms and optionally containing a further nitrogen or oxygen atom and one oxo or thioxo substituent, benzo[b]furyl, benzo[b]thienyl, A.sub.1 is propynylene, methylene, or a valence bond, X is O, S, SO.sub.2, or NR.sub.2, Y is selected from alkyl, haloalkyl, alkoxy, halogen, and hydrogen, A.sub.2 is selected from ##STR2## and methylene where Z is OR.sub.5 or NHR.sub.5 where R.sub.5 is hydrogen or alkyl, R.sub.1 is hydrogen, alkyl, or OR.sub.5, and m and n are integers having a value of 1 or 2 are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
    • 其中Ar是任选取代的碳环芳基，5-或6-元杂环芳基，含有一个或两个氮原子的10元双环杂环芳基，含有一个或两个氮原子的9元或10元杂环的结构化合物 并且任选地含有另外的氮或氧原子和一个氧代或硫代取代基，苯并[b]呋喃基，苯并[b]噻吩基，A 1是亚丙炔基，亚甲基或价键，X是O，S，SO 2或NR 2， Y选自烷基，卤代烷基，烷氧基，卤素和氢，A2选自：其中Z是OR 5或亚甲基，其中R 5是氢或烷基，R 1是氢，烷基或OR 5，和m和n 是具有1或2值的整数是脂氧合酶的有效抑制剂，因此抑制白细胞三烯的生物合成。 这些化合物可用于治疗或改善过敏性和炎性疾病状态。
    • 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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