HETEROARYLMETHOXYPHENYLTHIOALKYL CARBOXYLATES AS INHIBITORS OF LEUKOTRIENE BIOSYNTHESIS
    22.
    发明申请
    HETEROARYLMETHOXYPHENYLTHIOALKYL CARBOXYLATES AS INHIBITORS OF LEUKOTRIENE BIOSYNTHESIS 审中-公开
    作为紫杉醇生物合成酶的抑制剂的二异丙氧基甲基邻氨基甲酸酯

    公开(公告)号:WO1998014429A1

    公开(公告)日:1998-04-09

    申请号:PCT/US1997017265

    申请日:1997-09-26

    Abstract: Compounds having formula (I), wherein W and W are independently selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted naphthyl; R anb R are independently selected from hydrogen, alkyl, halolalkyl, alkoxy, halogen; R 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 , (c) -NR R , (d) -NR SO2R (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.

    Abstract translation: 具有式(I)的化合物,其中W 1和W 2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)-OR 4,(c)-NR 5 R 6,(d)-NR 4 SO 2 R 7 e)-NH-四唑基,和(f)甘氨酰; 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-(HETEROARYLMETHOXYPHENYL)CYCLOALKYL DERIVATIVES, THEIR PREPARATION AND THEIR USE AS INHIBITORS OF LEUKOTRIENE BIOSYTHESIS
    23.
    发明申请
    BIS-(HETEROARYLMETHOXYPHENYL)CYCLOALKYL DERIVATIVES, THEIR PREPARATION AND THEIR USE AS INHIBITORS OF LEUKOTRIENE BIOSYTHESIS 审中-公开
    BIS-(异邻甲氧基苯基)环烷基衍生物,其制备及其作为紫杉醇生物合成抑制剂的用途

    公开(公告)号:WO1997029090A1

    公开(公告)日:1997-08-14

    申请号:PCT/US1997001953

    申请日:1997-02-06

    CPC classification number: C07D215/18 C07D215/14 C07D241/42 C07D277/64

    Abstract: Compounds having structure (I), where m is an integer of from one to nine; n is an integer of from one to four; W is selected from unsubstituted quinolyl, benzothiazolyl, or quinoxalyl, or quinolyl, benzothiazolyl, or quinoxalyl substituted with one, two or three substituents selected from the group consisting of halogen, C1-6 alkyl, and C1-6 alkoxy; X is absent or is selected from the group consisting of (a) C1-6 alkylene; (b) C1-6 alkenylene; and (c) C1-6 alkynylene; Y is one to four substituents independently selected from halogen, C1-6 alkyl, and C1-6 alkoxy; Z is selected from the group consisting of (a) COB; (b) C(R )2-O-N=A-COB; and (c) C(R )=N-O-A-COB where A is C1-6 alkylene, and B is selected from the group consisting of (a) -OH; (b) -O M where M is a pharmaceutically acceptable cation; (c) -OR where R is hydrogen or alkyl of one to six carbon atoms; (d) -NR R where R is as previously defined and R is selected from the group consisting of hydrogen, alkyl of one to six carbon atoms, hydroxy, and alkoxy of from one to six carbon atoms, or R and R , together with the atom to which they are attached, form a ring of five to eight members containing one optional heteratom selected from N, O and S; and (e) -O-D where D is a metabolically cleavable group, are inhibitors of leukotriene biosynthesis.

    Abstract translation: 具有结构(I)的化合物,其中m是1至9的整数; n是1到4的整数; W选自未取代的喹啉基,苯并噻唑基或喹喔啉基,或喹啉基,苯并噻唑基或喹喔啉基,其被一个,两个或三个选自卤素,C 1-6烷基和C 1-6烷氧基的取代基取代; X不存在或选自(a)C 1-6亚烷基; (b)C 1-6亚烯基; 和(c)C1-6亚炔基; Y是一至四个独立地选自卤素,C 1-6烷基和C 1-6烷氧基的取代基; Z选自(a)COB; (b)C(R 2)2 -O-N = A-COB; 和(c)C(R 2)= N-O-A-COB,其中A是C 1-6亚烷基,B选自(a)-OH; (b)-O - M +,其中M是药学上可接受的阳离子; (c)-OR 6其中R 6为氢或1至6个碳原子的烷基; (d)-NR 6 R 7,其中R 6如前所定义,R 7选自氢,1至6个碳原子的烷基,羟基和1位的烷氧基 至6个碳原子,或R 6和R 7与它们所连接的原子一起形成含有一个任选的选自N,O和S的杂原子的五至八个成员的环; 和(e)-O-D,其中D是代谢可裂解基团,是白三烯生物合成的抑制剂。

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