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

    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。

    Symmetrical bis-heteroarylmethoxyphenyliminoxyalkyl carboxylates as
inhibitors of leukotriene biosynthesis
    4.
    发明授权
    Symmetrical bis-heteroarylmethoxyphenyliminoxyalkyl carboxylates as inhibitors of leukotriene biosynthesis 失效
    对称双杂芳基甲氧基苯基亚氨基烷基羧酸盐作为白三烯生物合成的抑制剂

    公开(公告)号:US5668146A

    公开(公告)日:1997-09-16

    申请号:US703442

    申请日:1996-09-17

    摘要: Compounds having the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein W and Y at each occurrence are the same and W is selected from the group consisting of 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; Y is selected from optionally substituted phenylene and optionally substituted ##STR2## wherein the alkylene portion is of one to six carbon atoms; A is selected from alkylene, alkenylene, cycloalkylene, and optionally substituted ##STR3## wherein the alkylene portion is of one to six carbon atoms; and M is selected from hydrogen, a pharmaceutically acceptable cation, a pharmaceutically acceptable, metabolically cleavable group, --OR.sup.3, and --NR.sup.4 R.sup.5, 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 in a mammal.

    摘要翻译: 具有下式的化合物或其药学上可接受的盐,其中W和Y在每次出现时相同,W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,任选地 取代的喹喔啉基,任选取代的吡啶基,任选取代的嘧啶基和任选取代的噻唑基; Y选自任选取代的亚苯基和任选取代的,其中亚烷基部分具有1至6个碳原子; A选自亚烷基,亚烯基,亚环烷基和任选取代的,其中亚烷基部分为1至6个碳原子; 并且M选自氢,药学上可接受的阳离子,药学上可接受的,代谢可切割的基团-OR3和-NR4R5,抑制白三烯生物合成,并且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哺乳动物中白细胞三烯生物合成的方法。

    Bis-heteroarylylmethoxyphenyl ketone derivatives as inhibitors of
leukotriene biosynthesis
    5.
    发明授权
    Bis-heteroarylylmethoxyphenyl ketone derivatives as inhibitors of leukotriene biosynthesis 失效
    双杂芳基甲氧基苯基酮衍生物作为白三烯生物合成的抑制剂

    公开(公告)号:US5714488A

    公开(公告)日:1998-02-03

    申请号:US703440

    申请日:1996-09-17

    摘要: Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein W is selected from the group consisting of 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 one or more groups independently selected from hydrogen, alkyl, halolalkyl, alkoxy, and halogen; Z is selected from the group consisting of N--OH, N--O--A--COM, CH--COM, and CH--CH.dbd.N--0--A--COM wherein A is selected from the group consisting of alkylene, alkenylene, cycloalkylene, and optionally substituted alkylphenyl wherein the alkyl portion is of one to six carbon atoms, and M is selected from the group consisting of a pharmaceutically acceptable, metabolically clearable group, --OR.sup.3, and --NR.sup.4 R.sup.5, 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: 具有式“IMAGE”的化合物或其药学上可接受的盐,其中W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, 和任选取代的噻唑基; R1和R2是独立地选自氢,烷基,卤代烷基,烷氧基和卤素的一个或多个基团; Z选自N-OH,NOA-COM,CH-COM和CH-CH = N-O-A-COM,其中A选自亚烷基,亚烯基,亚环烷基和任选取代的 烷基苯基,其中烷基部分为1至6个碳原子,M选自药学上可接受的,可代谢的基团-OR3和-NR4R5,抑制白三烯生物合成,并且可用于治疗过敏和炎症 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。

    N-substituted-furylalkenyl hydroxamic acid and N-hydroxyurea compounds
having lipoxygenase inhibitory activity
    6.
    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

    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。