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    Symmetrical bis-heteroaryl-methoxy-phenylalkyl carboxylates as inhibitors of leukotriene biosynthesis
    2.
    发明授权
    Symmetrical bis-heteroaryl-methoxy-phenylalkyl carboxylates as inhibitors of leukotriene biosynthesis 失效
    对称双杂芳基 - 甲氧基 - 苯基烷基羧酸盐作为白三烯生物合成的抑制剂

    公开(公告)号：US5795900A

    公开(公告)日：1998-08-18

    申请号：US703441

    申请日：1996-09-17

    申请人： Clint D. Brooks ,  Pramila Bhatia ,  Teodozyj Kolasa ,  Andrew O. Stewart ,  David E. Gunn ,  Richard A. Craig

    发明人： Clint D. Brooks ,  Pramila Bhatia ,  Teodozyj Kolasa ,  Andrew O. Stewart ,  David E. Gunn ,  Richard A. Craig

    IPC分类号： C07D239/26 ,  A61K31/4184 ,  A61K31/421 ,  A61K31/4402 ,  A61K31/454 ,  A61K31/47 ,  A61K31/498 ,  A61K31/506 ,  A61P37/08 ,  A61P43/00 ,  C07D213/30 ,  C07D215/14 ,  C07D215/18 ,  C07D235/12 ,  C07D241/42 ,  C07D263/56 ,  C07D277/24 ,  C07D277/64 ,  C07D417/14 ,  C07D401/10

    CPC分类号： C07D213/30 ,  C07D215/14 ,  C07D215/18 ,  C07D235/12 ,  C07D241/42 ,  C07D277/64

    摘要： Compounds having the formula: ##STR1## wherein W is the same at each occurrence and is selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl, halolalkyl, alkoxy, halogen; R.sup.3 is a valence bond or is selected from hydrogen and alkyl; X is a valence bond or is selected from alkylene, alkenylen, and alkynylene; and Z is selected from (a) COM, (b) CH.dbd.N--O--A--COM, (c) CH.sub.2 --O--N.dbd.A--COM wherein A is selected from alkylene and cycloalkylene, and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) --OR.sup.6, (c) --NR.sup.7 R.sup.8, (d)--NR.sup.6 SO.sub.2 R.sup.9, (e)-NH-Tetrazolyl, and (f) glycinyl inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states. Also disclosed are leukotriene biosynthesis inhibiting compositions and a method of inhibiting leukotriene biosynthesis.

    摘要翻译： 具有下式的化合物：其中W在每次出现时相同，并且选自任选取代的喹啉基，任选取代的苯并噻唑基，任选取代的苯并恶唑基，任选取代的苯并咪唑基，任选取代的喹喔啉基，任选取代的吡啶基，任选取代的嘧啶基， 取代的噻唑基; R 1和R 2独立地选自氢，烷基，卤代烷基，烷氧基，卤素; R3是价键或选自氢和烷基; X是价键或选自亚烷基，烯基和亚炔基; 并且Z选自（a）COM，（b）CH = NOA-COM，（c）CH2-ON = A-COM其中A选自亚烷基和亚环烷基，M选自（a）药学上可接受的代谢 可裂解基团，（b）-OR6，（c）-NR7R8，（d）-NR6SO2R9，（e）-NH-四唑基，（f）甘氨酰抑制白三烯生物合成，可用于治疗过敏性和炎性疾病状态。 还公开了白三烯生物合成抑制组合物和抑制白三烯生物合成的方法。

    Iminoxyderivatives of fenamates as inhibitors of prostaglandin biosynthesis
    3.
    发明授权
    Iminoxyderivatives of fenamates as inhibitors of prostaglandin biosynthesis 失效
    作为前列腺素生物合成抑制剂的灭火剂的亚硝基衍生物

    公开(公告)号：US5863946A

    公开(公告)日：1999-01-26

    申请号：US660046

    申请日：1996-06-06

    申请人： Clint D. W. Brooks ,  Richard A. Craig ,  Teodozyj Kolasa ,  Andrew O. Stewart

    发明人： Clint D. W. Brooks ,  Richard A. Craig ,  Teodozyj Kolasa ,  Andrew O. Stewart

    IPC分类号： C07C251/58 ,  C07D257/04 ,  A61K31/195

    CPC分类号： C07D257/04 ,  C07C251/58

    摘要： Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein Y is selected from halogen, alkyl, and haloalkyl; n is 0, 1, 2, or 3; X is absent or is alkylene; A is absent or is selected from optionally substituted alkylene, optionally substituted cycloalkylene, optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, optionally substituted alkenylene, and ##STR2## or R.sup.2 and A together define a saturated 5- to 8-membered optionally substituted carbocyclic or heterocyclic ring to which the group Z is attached; Z is selected from (a) hydrogen, (b) COM wherein M is selected from the group consisting of --OR.sup.5, a pharmaceutically acceptable cation, --NR.sup.7 R.sup.8, and a pharmaceutically acceptable, metabolically cleavable group, (c) --OR.sup.3, (d) tetrazolyl, (e) --CH(OR.sup.3)--CH.sub.2 OR.sup.9, (f) --CH(OR.sup.3)--CH.sub.2 --CH.sub.2 OR.sup.9, (g) --CH(OR.sup.3)--CH(OR.sup.9)--CH.sub.2 OR.sup.10, and (h) .dbd.N--OR.sup.3 ; and R.sup.1, R.sup.2, R.sup.3, R.sup.9, and R.sup.10 are independently selected from (a) hydrogen, (b) alkyl, and (c) optionally substituted phenyl, are prostaglandin biosynthesis inhibitors and are useful in the treatment of inflammatory disease states. Also disclosed are prostaglandin inhibiting compositions, a method of inhibiting prostaglandin biosynthesis in a mammal.

    摘要翻译： 具有式“IMAGE”的化合物或其药学上可接受的盐，其中Y选自卤素，烷基和卤代烷基; n为0,1,2或3; X不存在或是亚烷基; A不存在或选自任选取代的亚烷基，任选取代的亚环烷基，任选取代的亚环烷基，其中一个或两个碳原子被一个或两个独立地选自O，S和N的杂原子，任选取代的亚烯基取代，以及

    Oxime derivatives of indole and indene compounds as inhibitors of prostaglandin biosynthesis
    6.
    发明授权
    Oxime derivatives of indole and indene compounds as inhibitors of prostaglandin biosynthesis 失效
    吲哚和茚化合物的肟衍生物作为前列腺素生物合成的抑制剂

    公开(公告)号：US5750558A

    公开(公告)日：1998-05-12

    申请号：US660048

    申请日：1996-06-06

    申请人： Clint D. W. Brooks ,  Teodozyj Kolasa ,  Wendy Lee ,  Andrew O. Stewart

    发明人： Clint D. W. Brooks ,  Teodozyj Kolasa ,  Wendy Lee ,  Andrew O. Stewart

    IPC分类号： C07C317/32 ,  C07D209/14 ,  C07D257/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  C07D417/14 ,  A61K31/40

    CPC分类号： C07D257/04 ,  C07C317/32 ,  C07D209/14 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  C07D417/14 ,  C07C2102/08

    摘要： Described herein are compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein L is selected from the group consisting of ##STR2## R.sup.2 is selected from (a) ##STR3## R.sup.3 is selected from optionally substituted phenyl, and optionally substituted pyridyl; Y is selected from halogen, alkyl, haloalkyl, alkoxy, pyridylmethoxy, thiazolylmethoxy, benzothiazolylmethoxy, quinolylmethoxy, and optionally substituted quinolylmethoxy; W is selected from hydrogen, alkyl, hydroxyalkyl, and hydroxy; A is absent or is selected from optionally substituted alkylene optionally substituted cycloalkylene, optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, and ##STR4## and X is absent or is alkylene; Z is selected from (a) hydrogen, (b) COM wherein M is selected from (b-1) a pharmaceutically acceptable metabolically cleavable group, (b-2)--OR.sup.10,(b-3)--O(CH.sub.2).sub.w --CH(OR.sup.12)--CH.sub.2 OR.sup.13, and (b-4)--NR.sup.15 R.sup.16 (c)--OR.sup.17, (d) tetrazolyl, (e)--CH(OR.sup.17)--CH.sub.2 OR.sup.18,(f)--CH(OR.sup.17)--CH.sub.2 --CH.sub.2 OR.sup.18, (g)--CH(OR.sup.17)--CH(OR.sup.18)--CH.sub.2 OR.sup.19, and (h).dbd.N--OR.sup.17 ; and R.sup.1 and R.sup.4 selected from (a) hydrogen, (b) alkyl, and (c) optionally substituted phenyl, are prostaglandin biosynthesis inhibitors and are useful in the treatment of inflammatory disease states. Also disclosed are prostaglandin inhibiting compositions, and a method of inhibiting prostaglandin biosynthesis in a mammal.

    摘要翻译： 本文描述的是具有式“IMAGE”的化合物或其药学上可接受的盐，其中L选自由下列组成的组：R 2选自（a）图像（b）图像（c） （d）R 3选自任选取代的苯基和任选取代的吡啶基; Y选自卤素，烷基，卤代烷基，烷氧基，吡啶基甲氧基，噻唑基甲氧基，苯并噻唑基甲氧基，喹啉基甲氧基和任选取代的喹啉基甲氧基; W选自氢，烷基，羟基烷基和羟基; A不存在或选自任选取代的亚烷基任选取代的亚环烷基，任选取代的亚环烷基，其中一个或两个碳原子被一个或两个独立地选自O，S和N的杂原子替代，并且X不存在 或者是亚烷基; Z选自（a）氢，（b）COM，其中M选自（b-1）可药用代谢裂解基团，（b-2）-OR10，（b-3）-O（CH2）w- CH（OR 12）-CH 2 OR 13和（b-4）-NR 15 R 16（c）-OR 17，（d）四唑基，（e）-CH（OR 17）-CH 2 OR 18，（f）-CH（OR 17） （g）-CH（OR 17）-CH（OR 18）-CH 2 OR 19，和（h）= N-OR 17; 并且选自（a）氢，（b）烷基和（c）任选取代的苯基的R 1和R 4是前列腺素生物合成抑制剂，并且可用于治疗炎性疾病状态。 还公开了前列腺素抑制组合物和抑制哺乳动物中前列腺素生物合成的方法。

    Oxime derivatives of fenamates as inhibitors of prostaglandin biosynthesis
    7.
    发明授权
    Oxime derivatives of fenamates as inhibitors of prostaglandin biosynthesis 失效
    芥酸肟衍生物作为前列腺素生物合成的抑制剂

    公开(公告)号：US5840758A

    公开(公告)日：1998-11-24

    申请号：US659474

    申请日：1996-06-06

    申请人： Clint D. W. Brooks ,  Teodozyj Kolasa ,  Wendy Lee ,  Andrew O. Stewart

    发明人： Clint D. W. Brooks ,  Teodozyj Kolasa ,  Wendy Lee ,  Andrew O. Stewart

    IPC分类号： C07C251/16 ,  C07C251/60 ,  C07C259/06 ,  C07D257/04 ,  A61K31/41 ,  A61K31/165 ,  A61K31/19 ,  A61K31/275

    CPC分类号： C07D257/04 ,  C07C251/16 ,  C07C251/60 ,  C07C259/06 ,  Y10S514/824 ,  Y10S514/825 ,  Y10S514/863 ,  Y10S514/886 ,  Y10S514/887 ,  Y10S514/916

    摘要： Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein Y is selected from halogen, alkyl, and haloalkyl; n is 0, 1, 2, or 3; A is selected from (a) optionally substituted alkylene, (b) optionally substituted cycloalkylene, (c) optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, (d) optionally substituted alkenylene and (e) ##STR2## X is absent or is alkylene; Z is selected from (a) hydrogen, (b) COM wherein M is selected from --OR.sup.4, --NR.sup.6 R.sup.7, and a pharmaceutically acceptable metabolically cleavable group, (c) --OR.sup.2, (d) tetrazolyl, (e) --CH(OR.sup.2)--CH.sub.2 OR.sup.8, (f) --CH(OR.sup.2)--CH.sub.2 --CH.sub.2 OR.sup.8, (g) --CH(OR.sup.2)--CH(OR.sup.8)--CH.sub.2 OR.sup.9, and (h).dbd.N--OR.sup.2 ; and R.sup.1 is selected from hydrogen, alkyl, and optionally substituted phenyl, are prostaglandin biosynthesis inhibitors and are useful in the treatment of inflammatory disease states. Also disclosed are prostaglandin inhibiting compositions, a method of inhibiting prostaglandin biosynthesis in a mammal.

    摘要翻译： 具有式“IMAGE”的化合物或其药学上可接受的盐，其中Y选自卤素，烷基和卤代烷基; n为0,1,2或3; A选自（a）任选取代的亚烷基，（b）任选取代的亚环烷基，（c）任选取代的亚环烷基，其中一个或两个碳原子被一个或两个独立地选自O，S和N的杂原子置换，（ d）任选取代的亚烯基和（e）X不存在或是亚烷基; Z选自（a）氢，（b）COM，其中M选自-OR4，-NR6R7和药学上可接受的代谢可裂解基团，（c）-OR2，（d）四唑基，（e）-CH（OR2） ）-CH 2 OR 8，（f）-CH（OR 2）-CH 2 -CH 2 OR 8，（g）-CH（OR 2）-CH（OR 8）-CH 2 OR 9和（h）= N-OR 2; 并且R 1选自氢，烷基和任选取代的苯基，是前列腺素生物合成抑制剂，并且可用于治疗炎性疾病状态。 还公开了前列腺素抑制组合物，在哺乳动物中抑制前列腺素生物合成的方法。

    N-substituted-furylalkenyl hydroxamic acid and N-hydroxyurea compounds having lipoxygenase inhibitory activity
    8.
    发明授权
    N-substituted-furylalkenyl hydroxamic acid and N-hydroxyurea compounds having lipoxygenase inhibitory activity 失效
    N-取代呋喃基异羟肟酸和具有脂氧合酶抑制活性的N-羟基脲化合物

    公开(公告)号：US5169854A

    公开(公告)日：1992-12-08

    申请号：US841968

    申请日：1992-02-26

    申请人： Dee W. Brooks ,  Andrew O. Stewart ,  Pramila Bhatia ,  Richard A. Craig

    发明人： Dee W. Brooks ,  Andrew O. Stewart ,  Pramila Bhatia ,  Richard A. Craig

    IPC分类号： A61K31/34 ,  A61K31/341 ,  A61P43/00 ,  C07D307/58 ,  C07D307/64 ,  C07D405/12

    CPC分类号： C07D405/12 ,  C07D307/58 ,  C07D307/64

    摘要： Compounds useful in inhibiting the biosynthesis of leukotrienes have the structure ##STR1## where M is hydrogen, a pharmaceutically acceptable cation, or a metabolically cleavable group, R.sup.4 is alkyl, cycloalkyl or --NR.sup.5 R.sup.6, where R.sup.5 and R.sup.6 are hydrogen, alkyl, cycloalkyl or alkanoyl, where A is a valence bond or is a straight or branched divalent alkylene group of from one to twelve carbon atoms, R.sup.2 and R.sup.3 are independently selected from hydrogen, straight or branched alkyl of from one to twelve carbon atoms, halogen, or trifluoroalkyl, and R.sup.1 is selected from phenoxy, phenylthio, 2-, 3-, or 4-pyridyloxy, 1 or 2-naphthyloxy, or 2,4,5, or 8-quinolyloxy, all optionally substituted with alkyl, haloalkyl, alkoxy, hydroxy or halogen.

    摘要翻译： 可用于抑制白细胞三烯生物合成的化合物具有其中M是氢，药学上可接受的阳离子或代谢可裂解基团的结构，R 4是烷基，环烷基或-NR 5 R 6，其中R 5和R 6是氢，烷基，环烷基或 烷酰基，其中A是价键或是具有1至12个碳原子的直链或支链二价亚烷基，R 2和R 3独立地选自氢，具有1至12个碳原子的直链或支链烷基，卤素或三氟烷基 ，R1选自苯氧基，苯硫基，2-，3-或4-吡啶氧基，1或2-萘氧基或2,4,5或8-喹啉氧基，全部任选被烷基，卤代烷基，烷氧基，羟基 或卤素。

    Lipoxygenase and cyclooxygenase inhibiting compounds
    9.
    发明授权
    Lipoxygenase and cyclooxygenase inhibiting compounds 失效
    脂氧合酶和环加氧酶抑制化合物

    公开(公告)号：US5516789A

    公开(公告)日：1996-05-14

    申请号：US421125

    申请日：1995-04-12

    申请人： Clint D. W. Brooks ,  Andrew O. Stewart ,  Anwer Basha ,  Randy L. Bell

    发明人： Clint D. W. Brooks ,  Andrew O. Stewart ,  Anwer Basha ,  Randy L. Bell

    IPC分类号： C07C275/64 ,  C07D307/52 ,  C07D333/20 ,  C07D333/58 ,  C07D409/12 ,  A61K31/405 ,  C07D209/14

    CPC分类号： C07D409/12 ,  C07C275/64 ,  C07D307/52 ,  C07D333/20 ,  C07D333/58

    摘要： Compounds having the structure ##STR1## or a pharmaceutically acceptable salt thereof have activity as inhibitors of cylooxygenase and 5-lipoxygenase, reduce the biosynthesis of leukotrienes B.sub.4, C.sub.4, D.sub.4, and E.sub.4 and cylooxygenase products such as prostaglandins and thromboxane and are useful in the treatment of inflammatory and allergic disease states. The compounds have the structure indicated above wherein A is selected from (a) optinally substituted carbocyclic aryl, (b) optinally substituted furyl, (c) optinally substituted benzo[b]furyl, (d) optinally substituted thienyl, (e) optinally substituted pyridyloxy, (f) optinally substituted pyridylalkyl, (g) optinally substituted benzo[b]thienyl, (h) optinally substituted pyridyl, (i) optinally substituted quinolyl, and (j) optinally substituted indolyl; X is selected from (a) optionally substituted alkyl, (b) optinally substituted alkenyl, and (c) optinally substituted alkynyl; R.sup.1 and R.sup.2 are independently selected from hydrogen, hydroxy, and alkyl; and Z is a residue of a non-steroidal anti-inflammatory drug of the general formula Z--COOH.

    摘要翻译： 具有结构或其药学上可接受的盐的化合物具有作为环氧合酶和5-脂氧合酶抑制剂的活性，降低白细胞三烯B4，C4，D4和E4以及环加氧酶产物如前列腺素和血栓烷的生物合成，并且可用于 治疗炎症和过敏性疾病状态。 化合物具有上述结构，其中A选自（a）光学取代的碳环芳基，（b）光取代的呋喃基，（c）光取代的苯并[b]呋喃基，（d）最佳取代的噻吩基，（e） 吡啶基氧基，（f）选择性取代的吡啶基烷基，（g）最佳取代的苯并[b]噻吩基，（h）最佳取代的吡啶基，（i）最佳取代的喹啉基和（j） X选自（a）任选取代的烷基，（b）光学取代的烯基和（c）最佳取代的炔基; R 1和R 2独立地选自氢，羟基和烷基; Z为通式Z-COOH的非甾体抗炎药物的残基。