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    5-lipoxygenase inhibitors
    3.
    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。

    Imidazole lipoxygenase inhibitors
    6.
    发明授权
    Imidazole lipoxygenase inhibitors 失效
    咪唑脂氧合酶抑制剂

    公开(公告)号：US5753682A

    公开(公告)日：1998-05-19

    申请号：US553546

    申请日：1996-05-06

    申请人： Rodney W. Stevens ,  Takashi Mano ,  Kazuo Ando

    发明人： Rodney W. Stevens ,  Takashi Mano ,  Kazuo Ando

    IPC分类号： A61K31/415 ,  A61K31/4178 ,  A61P9/00 ,  A61P11/00 ,  A61P17/00 ,  A61P19/02 ,  A61P25/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D233/54 ,  C07D233/60 ,  C07D305/04 ,  C07D309/02 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D521/00

    CPC分类号： C07D233/64 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D405/12 ,  C07D405/14

    摘要： Certain novel imidazole derivatives having the ability to inhibit the lipoxygenase enzyme and having formula (I), wherein Y is hydrogen, C.sub.1 -C.sub.8 alkyl, halosubstituted C.sub.1 -C.sub.4 alkyl, phenyl, substituted phenyl, C.sub.7 -C.sub.14 phenylalkyl, C.sub.7 -C.sub.14 (substituted phenyl)alkyl, pyridyl, substituted pyridyl, C.sub.6 -C.sub.13 pyridylalkyl or C.sub.6 -C.sub.13 (substituted pyridyl)alkyl, wherein each substituent is independently halo, nitro, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halosubstituted C.sub.1 -C.sub.4 alkyl, halosubstituted C.sub.1 -C.sub.4 alkoxy, NR.sup.4 R.sup.5, CO.sub.2 R.sup.4 or CONR.sup.4 R.sup.5, wherein R.sup.4 and R.sup.5 are each, independently, hydrogen or C.sub.1 -C.sub.6 alkyl; Ar.sup.1 and Ar.sup.2 are each, independently, phenylene, mono-substituted phenylene or di-substituted phenylene, wherein the substituents are, independently, halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo-substituted C.sub.1 -C.sub.4 alkyl or halo-substituted C.sub.1 -C.sub.4 alkoxy; X and X.sup.1 are each, independently, O, S, SO or SO.sub.2 ; R' is hydrogen or C.sub.1 -C.sub.4 alkyl; and R.sup.2 and R.sup.3 are each, independently, methylene, ethylene or propylene. These compounds are useful for the treatment of disease states such as bronchial asthma, skin disorders and arthritis in mammals, and as the active ingredient in pharmaceutical compositions for treating such conditions.

    摘要翻译： PCT No.PCT / JP94 / 00836 Sec。 371日期：1996年5月6日 102（e）日期1996年5月6日PCT 1994年5月25日PCT公布。 第WO94 / 29299号公报 日期：1994年12月22日具有抑制脂氧合酶和具有式（I）的能力的新型咪唑衍生物，其中Y为氢，C1-C8烷基，卤代C1-C4烷基，苯基，取代苯基，C7-C14苯基烷基， C7-C14（取代苯基）烷基，吡啶基，取代的吡啶基，C6-C13吡啶基烷基或C6-C13（取代的吡啶基）烷基，其中各取代基独立地为卤素，硝基，氰基，C 1 -C 4烷基，C 1 -C 4烷氧基， C 1 -C 4烷基，卤代C 1 -C 4烷氧基，NR 4 R 5，CO 2 R 4或CONR 4 R 5，其中R 4和R 5各自独立地为氢或C 1 -C 6烷基; Ar 1和Ar 2各自独立地为亚苯基，单取代亚苯基或二取代亚苯基，其中取代基独立地为卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，卤素取代的C 1 -C 4烷基或卤素取代的 C1-C4烷氧基; X和X1各自独立地为O，S，SO或SO 2; R'是氢或C 1 -C 4烷基; 并且R 2和R 3各自独立地为亚甲基，亚乙基或亚丙基。 这些化合物可用于治疗疾病状态，例如哺乳动物中的支气管哮喘，皮肤病和关节炎，以及用作治疗这些病症的药物组合物中的活性成分。

    Imidazole lipoxygenase inhibitors
    7.
    发明授权
    Imidazole lipoxygenase inhibitors 失效
    咪唑脂氧合酶抑制剂

    公开(公告)号：US6037355A

    公开(公告)日：2000-03-14

    申请号：US43256

    申请日：1998-06-29

    申请人： Takashi Mano ,  Rodney W. Stevens

    发明人： Takashi Mano ,  Rodney W. Stevens

    IPC分类号： C07D493/08 ,  A61K31/35 ,  A61K31/415 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D521/00 ,  A01N43/40 ,  A01N43/50 ,  C07D233/02 ,  C07D401/04

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

    摘要： The present invention provides a compound of formula (I): ##STR1## and a pharmaceutically acceptable salt thereof, wherein Ar is phenylene optionally substituted with halo, hydroxy, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 halo-substituted alkyl or C.sub.1 -C.sub.4 halo-substituted alkoxy, X is --A--X.sup.1 -- or --X.sup.2 --A--, where A is a direct bond or C.sub.1 -C.sub.4 alkylene, and X.sup.1 is oxy, thio, sulfinyl or sulfonyl; Ar is phenylene, pyridylene or thienylene optionally substituted with halo, hydroxy, cyano, nitro, amino, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 halo-substituted alkyl, C.sub.1 -C.sub.4 halo-substituted alkoxy, C.sub.1 -C.sub.4 alkylamino or di(C.sub.1 -C.sub.4)alkylamino; Y is CN or CONR.sup.1 R.sup.2 wherein R.sup.1 and R.sup.2 are independently hydrogen or C.sub.1 -C.sub.4 alkyl; and R is hydrogen or C.sub.1 -C.sub.6 alkyl; W is C.sub.2 -C.sub.3 alkylene, one carbon atom of which may be replaced by an oxygen atom. Further the invention provides a pharmaceutical composition for treating an inflammatory disease, allergy or cardiovascular diseases or the like in a mammalian subject which comprises a compound of formula (I) and a pharmaceutically acceptable carrier.

    摘要翻译： PCT No.PCT / IB96 / 00744 Sec。 371日期1998年6月29日第 102（e）1998年6月29日PCT PCT 1996年7月24日PCT公布。 出版物WO97 / 11079 日期：1997年3月27日本发明提供式（I）化合物及其药学上可接受的盐，其中Ar为任选被卤素，羟基，氰基，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4 烷硫基，C 1 -C 4卤素取代的烷基或C 1 -C 4卤素取代的烷氧基，X是-A-X 1或-X 2 -A-，其中A是直接键或C 1 -C 4亚烷基，X 1是氧基，硫代 ，亚磺酰基或磺酰基; Ar是任选被卤素，羟基，氰基，硝基，氨基，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4烷硫基，C 1 -C 4卤素取代的烷基，C 1 -C 4卤素取代的烷氧基取代的亚苯基，亚吡啶基或噻吩基 ，C 1 -C 4烷基氨基或二（C 1 -C 4）烷基氨基; Y是CN或CONR1R2，其中R1和R2独立地是氢或C1-C4烷基; 和R是氢或C 1 -C 6烷基; W是C 2 -C 3亚烷基，其一个碳原子可被氧原子代替。 此外，本发明提供了用于治疗哺乳动物受试者中的炎性疾病，过敏或心血管疾病等的药物组合物，其包含式（I）化合物和药学上可接受的载体。

    5-lipoxygenase inhibitors
    8.
    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。