Heteroarylmethoxyphenylthioalkyl carboxylates as inhibitors of
leukotriene biosynthesis
    53.
    发明授权
    Heteroarylmethoxyphenylthioalkyl carboxylates as inhibitors of leukotriene biosynthesis 失效
    作为白三烯生物合成抑制剂的杂芳基甲氧基苯硫基烷基羧酸盐

    公开(公告)号:US5783586A

    公开(公告)日:1998-07-21

    申请号:US724200

    申请日:1996-10-01

    摘要: Compounds having the formula: ##STR1## wherein W.sup.1 and W.sup.2 are independently selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted naphthyl; R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl, halolalkyl, alkoxy, halogen; R.sup.3 is selected from thienyl, furyl, phenyl, naphthyl, benzo�b!thienyl, alkyl, hydroxyl, and hydrogen; Y an alkylene of one to six carbon atoms; and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) --OR.sup.4, (c) --NR.sup.5 R.sup.6, (d)--NR.sup.4 SO.sub.2 R.sup.7 (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W1和W2独立地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,任选取代的萘基; R 1和R 2独立地选自氢,烷基,卤代烷基,烷氧基,卤素; R 3选自噻吩基,呋喃基,苯基,萘基,苯并[b]噻吩基,烷基,羟基和氢; Y为1至6个碳原子的亚烷基; 并且M选自(a)药学上可接受的代谢可裂解基团,(b)-OR4,(c)-NR5R6,(d)-NR4SO2R7(e)-NH-四唑基和(f)甘氨酰基; 抑制白细胞三烯生物合成,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。

    Bis-heteroarylylmethoxyphenyl ketone derivatives as inhibitors of
leukotriene biosynthesis
    54.
    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。

    Non-symmetrical bis-heteroarylmethoxyphenylalkyl carboxylates as
inhibitors of leukotriene biosynthesis
    55.
    发明授权
    Non-symmetrical bis-heteroarylmethoxyphenylalkyl carboxylates as inhibitors of leukotriene biosynthesis 失效
    非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:US5668150A

    公开(公告)日:1997-09-16

    申请号:US686841

    申请日:1996-07-26

    摘要: Compounds having the formula ##STR1## wherein W and Y are independently selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, and optionally substituted naphthyl with the proviso that W and Y are not simultaneously the same substituent; R.sup.1 and R.sup.2 are independently hydrogen, alkyl, haloalkyl, alkoxy, or halogen; R.sup.3 is hydrogen or alkyl; X is absent or is alkylene, alkenylene, or alkynylene; and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) --OR.sup.4 wherein R.sup.4 is hydrogen or alkyl; and (c) --NR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are independently selected from hydrogen, alkyl, hydroxy and alkoxy are disclosed. These compounds inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states.

    摘要翻译: 具有式的化合物,其中W和Y独立地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和任选取代的萘基,条件是W和Y不同时为 相同的取代基; R1和R2独立地是氢,烷基,卤代烷基,烷氧基或卤素; R3是氢或烷基; X不存在或是亚烷基,亚烯基或亚炔基; 并且M选自(a)药学上可接受的代谢可切割基团,(b)-OR 4,其中R 4是氢或烷基; 和(c)-NR 5 R 6,其中R 5和R 6独立地选自氢,烷基,羟基和烷氧基。 这些化合物抑制白细胞三烯生物合成,并且可用于治疗过敏性和炎性疾病状态。

    Compounds as cannabinoid receptor ligands
    57.
    发明授权
    Compounds as cannabinoid receptor ligands 有权
    化合物作为大麻素受体配体

    公开(公告)号:US08586596B2

    公开(公告)日:2013-11-19

    申请号:US13160952

    申请日:2011-06-15

    摘要: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein A1 and Rx are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.

    摘要翻译: 本文公开了式(I)的大麻素受体配体,其中A1和Rx如说明书中所定义。 还提出了包含这些化合物的组合物和使用这些化合物和组合物治疗病症和障碍的方法。