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19 条记录 (耗时 0.034 秒)

    Benzimidazole cyclooxygenase-2 inhibitors
    13.
    发明授权
    Benzimidazole cyclooxygenase-2 inhibitors 失效
    苯并咪唑环加氧酶-2抑制剂

    公开(公告)号：US06713482B2

    公开(公告)日：2004-03-30

    申请号：US09924351

    申请日：2001-08-08

    申请人： Yoshiyuki Okumura ,  Yoshinori Murata ,  Takashi Mano

    发明人： Yoshiyuki Okumura ,  Yoshinori Murata ,  Takashi Mano

    IPC分类号： A61K3506

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14

    摘要： This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof, wherein Ar is heteroaryl; X1 and X2 are independently selected from halo, C1-C4 alkyl, hydroxy, C1-C4 alkoxy, amino, C1-C4 alkanoyl, carboxy, carbamoyl, cyano, nitro, mercapto, (C1-C4 alkyl)thio, (C1-C4 alkyl)sulfinyl, (C1-C4 alkyl)sulfonyl, aminosulfonyl, or the like; R1 is selected from hydrogen, straight or branched C1-C4 alkyl, C3-C8 cycloalkyl, C4-C8 cycloalkenyl, phenyl, heteroaryl and the like; R2 and R3 are independently selected from hydrogen, halo, C1-C4 alkyl, phenyl and the like; or R1 and R2 can form, together with the carbon atom to which they are attached, a C5-C7 cycloalkyl ring; and m and n are independently 0, 1, 2 or 3. These compounds and pharmaceutical compositions containing such compounds are useful as analgesics and anti-inflammatory agents.

    摘要翻译： 本发明提供下式的化合物或其药学上可接受的盐，其中Ar是杂芳基; X 1和X 2独立地选自卤素，C 1 -C 4烷基，羟基，C 1 -C 4烷氧基，氨基，C 1 -C 4烷酰基，羧基，氨基甲酰基，氰基，硝基，巯基，（C 1 -C 4烷基） 硫代，（C 1 -C 4烷基）亚磺酰基，（C 1 -C 4烷基）磺酰基，氨基磺酰基等; R 1选自氢，直链或支链C 1 -C 4烷基，C 3 -C 8环烷基，C 4 -C 8环烯基，苯基，杂芳基等; R 2和R 3独立地选自氢，卤素，C 1 -C 4烷基，苯基等; 或R 1和R 2可以与它们所连接的碳原子一起形成C5-C7环烷基环; 并且m和n独立地为0,1,2或3.这些化合物和含有这些化合物的药物组合物可用作止痛剂和抗炎剂。

    5-membered heteroaryl substituted 1,4-dihydropyridine compounds as bradykinin antagonists
    14.
    发明授权
    5-membered heteroaryl substituted 1,4-dihydropyridine compounds as bradykinin antagonists 失效
    5元杂芳基取代的1,4-二氢吡啶化合物作为缓激肽拮抗剂

    公开(公告)号：US06444677B2

    公开(公告)日：2002-09-03

    申请号：US09731995

    申请日：2000-12-07

    申请人： Takafumi Ikeda ,  Mitsuhiro Kawamura ,  Noriaki Murase ,  Seiji Nukui ,  Yuji Shishido ,  Makato Kawai ,  Yoshiyuki Okumura

    发明人： Takafumi Ikeda ,  Mitsuhiro Kawamura ,  Noriaki Murase ,  Seiji Nukui ,  Yuji Shishido ,  Makato Kawai ,  Yoshiyuki Okumura

    IPC分类号： C07D40100

    CPC分类号： C07D417/06 ,  C07D417/12 ,  C07D417/14

    摘要： This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein A is independently halo; Y1 is —(CH2)m—, C(O) or S(O); Y2 is N or CH; R1 and R2 are independently C1-4 alkyl; R3 is selected from the following: (a) optionally substituted —(CH2)p—C3-7 cycloalkyl; (b) optionally substituted —C5-7 alkyl; and (c) substituted —C1-4 alkyl; and (d) optionally substituted C7-9 bicycloalkyl; R4 is optionally substituted thiazolyl, imidazolyl or oxazolyl; X is S, —NH, —N—C1-4 alkyl or O; R5 is hydrogen or C1-4 alkyl; R6 is C1-4 alkyl or halo; m is 0, 1 or 2; n is 0, 1, 2, 3, 4 or S; and p is 0, 1, 2, 3, 4, 5 or 6. These compounds are useful for the treatment of medical conditions caused by bradykinin such as inflammation, cardiovascular disease, pain, etc. This invention also provides a pharmaceutical composition comprising the above compound.

    摘要翻译： 本发明提供式（I）的化合物或其药学上可接受的盐，其中A独立地为卤素; Y1是 - （CH2）m-，C（O）或S（O）; Y2是N或CH; R1和R2独立地是C1-4烷基; R3选自如下：（a）任选取代的 - （CH 2）p -C 3-7环烷基;（b）任选取代的-C 5-7烷基; 和（c）取代的C 1-4烷基; 和（d）任选取代的C 7-9双环烷基; R 4是任选取代的噻唑基，咪唑基或恶唑基; X是S，-NH，-N-C 1-4烷基或O; R 5是氢或C 1-4烷基; R6是C1-4烷基或卤素; m是0,1或2; n为0，1，2，3，4或S; 并且p为0,1,2,3,4,5或6.这些化合物可用于治疗由缓激肽引起的疾病如炎症，心血管疾病，疼痛等。本发明还提供一种药物组合物，其包含 以上化合物。

    Benzimidazole cyclooxygenase-2 inhibitors
    15.
    发明授权
    Benzimidazole cyclooxygenase-2 inhibitors 失效
    苯并咪唑环加氧酶-2抑制剂

    公开(公告)号：US06310079B1

    公开(公告)日：2001-10-30

    申请号：US09244875

    申请日：1999-02-05

    申请人： Yoshiyuki Okumura ,  Yoshinori Murata ,  Takashi Mano

    发明人： Yoshiyuki Okumura ,  Yoshinori Murata ,  Takashi Mano

    IPC分类号： A61K31443

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14

    摘要： This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof, wherein Ar is heteroaryl; X1 and X2 are independently selected from halo, C1-C4 alkyl, hydroxy, C1-C4 alkoxy, amino, C1-C4 alkanoyl, carboxy, carbamoyl, cyano, nitro, mercapto, (C1-C4 alkyl)thio, (C1-C4 alkyl)sulfinyl, (C1-C4 alkyl)sulfonyl, aminosulfonyl, or the like; R1 is selected from hydrogen, straight or branched C1-C4 alkyl, C3-C8 cycloalkyl, C4-C8 cycloalkenyl, phenyl , heteroaryl and the like; R2 and R3 are independently selected from hydrogen, halo, C1-C4 alkyl, phenyl and the like; or R1 and R2 can form, together with the carbon atom to which they are attached, a C5-C7 cycloalkyl ring; and m and n are independently 0, 1, 2 or 3. These compounds and pharmaceutical compositions containing such compounds are useful as analgesics and anti-inflammatory agents.

    摘要翻译： 本发明提供下式的化合物或其药学上可接受的盐，其中Ar是杂芳基; X1和X2独立地选自卤素，C1-C4烷基，羟基，C1-C4烷氧基，氨基，C1-C4烷酰基，羧基，氨基甲酰基，氰基，硝基，巯基，（C1-C4烷基）硫基，（C1-C4 烷基）亚磺酰基，（C 1 -C 4烷基）磺酰基，氨基磺酰基等; R 1选自氢，直链或支链C 1 -C 4烷基，C 3 -C 8环烷基，C 4 -C 8环烯基，苯基，杂芳基等; R2和R3独立地选自氢，卤素，C1-C4烷基，苯基等; 或者R 1和R 2可以与它们所连接的碳原子一起形成C 5 -C 7环烷基环; 并且m和n独立地为0,1,2或3.这些化合物和含有这些化合物的药物组合物可用作止痛剂和抗炎剂。

    5-lipoxygenase inhibitors
    16.
    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。