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    5-lipoxygenase inhibitors
    1.
    发明授权
    5-lipoxygenase inhibitors 失效
    5-脂氧合酶抑制剂

    公开(公告)号：US5883106A

    公开(公告)日：1999-03-16

    申请号：US020014

    申请日：1998-02-06

    申请人： Rodney W. Stevens ,  Takashi Mano ,  Kazunari Nakao ,  Yoshiyuki Okumura

    发明人： Rodney W. Stevens ,  Takashi Mano ,  Kazunari Nakao ,  Yoshiyuki Okumura

    IPC分类号： C07D231/12 ,  C07D309/08 ,  C07D521/00 ,  A61K31/085 ,  A61K31/11 ,  A61K31/15 ,  A61K31/19 ,  A61K31/34 ,  A61K31/40 ,  A61K31/44 ,  C07C69/76 ,  C07C233/28 ,  C07C233/64 ,  C07C235/40 ,  C07C323/23 ,  C07D207/30 ,  C07D249/04 ,  C07D309/32

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D309/08

    摘要： Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, and C.sub.1-4 alkyl; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, and amino X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino and C.sub.1-4 alkyl; R.sup.1 and R.sup.2 are each C.sub.1-4 alkyl, or together they form a group of formula --D.sup.1 --Z--D.sup.2 -- which together with the carbon atom to which it is attached defines a ring having 3 to 8 atoms, wherein D.sup.1 and D.sup.2 are C.sub.1-4 alkylene and Z is a direct bond or oxy, thio, sulfinyl, sulfonyl, or vinylene, and D.sup.1 and D.sup.2 may be substituted by C.sub.1-3 alkyl; and Y is CONR.sup.3 R.sup.4, CN, C(R.sup.3).dbd.N--OR.sup.4, COOR.sup.3, COR.sup.3 or CSNR.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are each H or C.sub.1-4 alkyl. These compounds are useful in the treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.

    摘要翻译： 具有抑制5-脂肪氧合酶并具有下式I的能力的新型化合物：其中Ar1是选自咪唑基，吡咯基，吡唑基，1,2,3或3位的杂环部分 三唑基，1,2,4-三唑基，吲哚基，吲唑基和苯并咪唑基，其通过环氮原子与X1键合，并且其可任选被一个或两个选自卤素，羟基，氰基，氨基和 C 1-4烷基; X1是直接键或C1-4亚烷基; Ar 2是任选被卤素，羟基，氰基取代的亚苯基，氨基X2是-A-X-或-X-A-，其中A是直接键或C 1-4亚烷基，X是氧基，硫代，亚磺酰基或磺酰基; Ar 3是任选被一个或两个选自卤素，羟基，氰基，氨基和C 1-4烷基的取代基取代的亚苯基，亚吡啶基，亚噻吩基，呋喃基，恶唑基或噻唑基; R1和R2各自为C1-4烷基，或者它们一起形成式-D1-Z-D2-的基团，与其所连接的碳原子一起形成具有3至8个原子的环，其中D1和D2是 C 1-4亚烷基，Z是直接键或氧基，硫基，亚磺酰基，磺酰基或亚乙烯基，D1和D2可以被C 1-3烷基取代; 并且Y是CONR 3 R 4，CN，C（R 3）= N-OR 4，COOR 3，COR 3或CSNR 3 R 4，其中R 3和R 4各自为H或C 1-4烷基。 这些化合物可用于治疗或缓解哺乳动物的炎性疾病，变态反应和心血管疾病，并用作治疗这些病症的药物组合物中的活性成分。

    5-lipoxygenase inhibitors
    2.
    发明授权
    5-lipoxygenase inhibitors 失效
    5-脂氧合酶抑制剂

    公开(公告)号：US6063928A

    公开(公告)日：2000-05-16

    申请号：US207342

    申请日：1998-12-08

    申请人： Rodney W. Stevens ,  Takashi Mano ,  Kazunari Nakao ,  Yoshiyuki Okumura

    发明人： Rodney W. Stevens ,  Takashi Mano ,  Kazunari Nakao ,  Yoshiyuki Okumura

    IPC分类号： C07D233/60 ,  C07D233/61 ,  C07D309/08 ,  C07D521/00 ,  C07D207/323 ,  C07D207/36 ,  C07D235/10 ,  C07D235/14 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D309/08

    摘要： Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, amino and the like; X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; R.sup.1 and R.sup.2 are each C.sub.1-4 alkyl, or together they form a group of formula --D.sup.1 --Z--D.sup.2 -- which together with the carbon atom to which it is attached defines a ring having 3 to 8 atoms, wherein D.sup.1 and D.sup.2 are C.sub.1-4 alkylene and Z is a direct bond or oxy, thio, sulfinyl, sulfonyl, or vinylene, and D.sup.1 and D.sup.2 may be substituted by C.sub.1-3 alkyl; and Y is CONR.sup.3 R.sup.4, CN, C(R.sup.3).dbd.N--OR.sup.4, COOR.sup.3, COR.sup.3 or CSNR.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are each H or C.sub.1-4 alkyl. These compounds are useful in the treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.

    摘要翻译： 具有抑制5-脂肪氧合酶并具有下式I的能力的新型化合物及其药学上可接受的盐，其中Ar1是选自咪唑基，吡咯基，吡唑基，1,2,3-三唑基， ，2,4-三唑基，吲哚基，吲唑基和苯并咪唑基，其通过环氮原子与X1连接，并且其可任选被一个或两个选自卤素，羟基，氰基，氨基，C 1-4烷基的取代基取代， 类似; X1是直接键或C1-4亚烷基; Ar 2是任选被卤素，羟基，氰基，氨基等取代的亚苯基; X2是-A-X或-X-A-，其中A是直接键或C 1-4亚烷基，X是氧基，硫代，亚磺酰基或磺酰基; Ar 3是任选被一个或两个选自卤素，羟基，氰基，氨基，C 1-4烷基等的取代基取代的亚苯基，亚吡啶基，亚噻吩基，呋喃基，恶唑基或噻唑基; R1和R2各自为C1-4烷基，或者它们一起形成式-D1-Z-D2-的基团，与其所连接的碳原子一起形成具有3至8个原子的环，其中D1和D2是 C 1-4亚烷基，Z是直接键或氧基，硫基，亚磺酰基，磺酰基或亚乙烯基，D1和D2可以被C 1-3烷基取代; 并且Y是CONR 3 R 4，CN，C（R 3）= N-OR 4，COOR 3，COR 3或CSNR 3 R 4，其中R 3和R 4各自为H或C 1-4烷基。 这些化合物可用于治疗或缓解哺乳动物的炎性疾病，变态反应和心血管疾病，并用作治疗这些病症的药物组合物中的活性成分。