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    Leukotriene A4 hydrolase inhibitors
    1.
    发明授权
    Leukotriene A4 hydrolase inhibitors 失效
    白三烯A4水解酶抑制剂

    公开(公告)号：US06242476B1

    公开(公告)日：2001-06-05

    申请号：US09381256

    申请日：1999-09-17

    申请人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Ken-ichi Fujimura ,  Hiroshi Suhara

    发明人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Ken-ichi Fujimura ,  Hiroshi Suhara

    IPC分类号： A61K31401

    CPC分类号： C07D207/16

    摘要： The present invention relates to leukotriene A4 hydrolase inhibitors containing compounds represented by the formula [I] or salts thereof as active ingredients, wherein R1 represents hydrogen, alkyl, phenylalkyl, alkanoyl or benzoyl; R2 and R3 each represent hydrogen or alkyl; R4 represents hydroxyl, alkoxy, phenylalkoxy, amino, alkylamino or phenylalkylamino; R5 represents phenylalkyl or naphthylalkyl; “Z” represents sulfur or oxygen; “A” represents alkylene; and “n” represents 0, 1 or 2; providing that the phenyl ring in R1 can be substituted by alkyl, alkoxy or halogen, and that the phenyl ring or the naphthyl ring in R5 can be substituted by alkyl, cycloalkyl, alkoxy, alkylthio or halogen.

    摘要翻译： 本发明涉及含有由式[I]表示的化合物或其盐作为活性成分的白三烯A4水解酶抑制剂，其中R1代表氢，烷基，苯基烷基，烷酰基或苯甲酰基; R2和R3各自表示氢或烷基; R4表示羟基，烷氧基，苯基烷氧基，氨基，烷基氨基或苯基烷基氨基; R5代表苯基烷基或萘基烷基; “Z”表示硫或氧; “A”表示亚烷基; “n”表示0,1或2; 条件是R1中的苯环可以被烷基，烷氧基或卤素取代，R5中的苯环或萘环可以被烷基，环烷基，烷氧基，烷硫基或卤素取代。

    Urea derivatives useful as synthetic intermediates
    2.
    发明授权
    Urea derivatives useful as synthetic intermediates 失效
    尿素衍生物可用作合成中间体

    公开(公告)号：US06730784B2

    公开(公告)日：2004-05-04

    申请号：US10147131

    申请日：2002-05-15

    申请人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Hiroshi Suhara

    发明人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Hiroshi Suhara

    IPC分类号： C07D26530

    CPC分类号： C07D295/185 ,  C07C317/50 ,  C07C323/44 ,  C07C323/59 ,  C07C323/60 ,  C07C327/30 ,  C07C329/06 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2603/74 ,  C07D333/32

    摘要： Objects of the present invention are to create compounds having urea structure as basic structure and having a sulfur atom and an amide bond in side chains and to find pharmacological effects thereof, particularly TNF-&agr; production inhibitory effects. The present invention provides compounds represented by the following formula [I] wherein R1 is H, alkyl, aromatic, RA—CO—, RC—S— or the formula [II]; R2, R3 and R4 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or aromatic; R5 and R6 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or aromatic; R5 and R6 can together form a nonaromatic heterocyclic ring; R7 is H, alkyl, cycloalkyl, hydroxy, mercapto, phenyl, RB—O—, RC—S—, RD—COS—, RE—OCO—, RF—N(RG)— or —CONHOH; and A1 and A2 are alkylene.

    摘要翻译： 本发明的目的是产生具有尿素结构作为碱性结构并在侧链中具有硫原子和酰胺键的化合物，并找到其药理作用，特别是TNF-α产生抑制作用。本发明提供了由 下式[I]其中R 1是H，烷基，芳基，R A -CO-，R c -S-或式[II]; R 2，R 3和R 4是H，烷基，烯基，环烷基，环烯基或芳族; R 5和R 6是H，烷基，烯基，环烷基，环烯基或芳族; R 5和R 6可以一起形成非芳族杂环; R 7是H，烷基，环烷基，羟基，巯基，苯基，R -O-，R C，-S-，R 6 -COS-，R e -OCO-，R F -N（R G） - 或-CONHOH; A 1和A 2是亚烷基。

    Urea derivatives having nitrogen aromatic heterocycle
    4.
    发明授权
    Urea derivatives having nitrogen aromatic heterocycle 失效
    具有氮芳香杂环的脲衍生物

    公开(公告)号：US06420398B2

    公开(公告)日：2002-07-16

    申请号：US09775420

    申请日：2001-02-01

    申请人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Hiroshi Suhara

    发明人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Hiroshi Suhara

    IPC分类号： C07D21302

    CPC分类号： C07D213/40

    摘要： An object of the present invention is to provide novel urea derivatives which have TNF-&agr; production inhibitory effects and are useful as therapeutic agents for various diseases, particularly as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. The urea derivatives according to the present invention are compounds represented by the formula [I] and salts thereof. In the formula, R1 is H, alkyl, phenyl or a group of the formula [`I]; R2 is H, alkyl, carboxyl or ester thereof or the like; R3 and R4 are each H, alkyl, cycloalkyl or the like; R5 is H, alkyl, hydroxy or the like; R6 is a nitrogen aromatic heterocycle; and A1 and A2 are alkylene.

    摘要翻译： 本发明的目的是提供具有TNF-α产生抑制作用的新型尿素衍生物，可用作各种疾病的治疗剂，特别是作为自身免疫疾病如类风湿性关节炎的治疗剂。 根据本发明的脲衍生物是由式[I]表示的化合物及其盐。 在该式中，R 1是H，烷基，苯基或式[Ⅷ]的基团。 R2是H，烷基，羧基或其酯等; R3和R4各自为H，烷基，环烷基等; R5是H，烷基，羟基等; R6是氮芳香杂环; 并且A1和A2是亚烷基。

    Urea derivatives and pharmaceutical compositions thereof
    5.
    发明授权
    Urea derivatives and pharmaceutical compositions thereof 失效
    尿素衍生物及其药物组合物

    公开(公告)号：US06492370B1

    公开(公告)日：2002-12-10

    申请号：US09623779

    申请日：2000-09-08

    申请人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Hiroshi Suhara

    发明人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Hiroshi Suhara

    IPC分类号： C07C32344

    CPC分类号： C07D295/185 ,  C07C317/50 ,  C07C323/44 ,  C07C323/59 ,  C07C323/60 ,  C07C327/30 ,  C07C329/06 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2603/74 ,  C07D333/32

    摘要： Objects of the present invention are to create compounds having urea structure as basic structure and having a sulfur atom and an amide bond in side chains and to find pharmacological effects thereof, particularly TNF-&agr; production inhibitory effects. The present invention provides compounds represented by the following formula [I] wherein R1 is H, alkyl, aromatic, RA—CO—, RC—S—or the formula [II]; R2, R3 and R4 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or aromatic; R5 and R6 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or aromatic; R5 and R6 can together form a nonaromatic heterocyclic ring; R7 is H, alkyl, cycloalkyl, hydroxy, mercapto, phenyl, RB—O—, RC—S—, RD—COS—, RE—OCO—, RF—N(RG)— or —CONHOH; and A1 and A2 are alkylene.

    摘要翻译： 本发明的目的是产生具有尿素结构作为碱性结构并在侧链中具有硫原子和酰胺键的化合物，并找到其药理作用，特别是TNF-α产生抑制作用。本发明提供了由 下式[I]其中R 1是H，烷基，芳族，RA-CO-，RC-S-或式[II]; R2，R3和R4是H，烷基，烯基，环烷基，环烯基或芳族; R5和R6是H，烷基，烯基，环烷基，环烯基或芳族; R5和R6可以一起形成非芳族杂环; R 7是H，烷基，环烷基，羟基，巯基，苯基，RB-O-，RC-S-，RD-COS-，RE-OCO-，RF-N（RG） - 或-CONHOH; 并且A1和A2是亚烷基。

    TNF-α production inhibitors
    10.
    发明授权
    TNF-α production inhibitors 失效
    TNF-α产生抑制剂

    公开(公告)号：US07923461B2

    公开(公告)日：2011-04-12

    申请号：US12586515

    申请日：2009-09-23

    申请人： Masakazu Ban ,  Hiroshi Suhara ,  Masato Horiuchi ,  Noriyoshi Yamamoto ,  Hiroshi Enomoto ,  Hiroyuki Inoue

    发明人： Masakazu Ban ,  Hiroshi Suhara ,  Masato Horiuchi ,  Noriyoshi Yamamoto ,  Hiroshi Enomoto ,  Hiroyuki Inoue

    IPC分类号： C07D213/46 ,  A61K31/4409

    CPC分类号： C07D213/56 ,  C07D213/30 ,  C07D213/32 ,  C07D213/38 ,  C07D213/40 ,  C07D213/68 ,  C07D213/75 ,  C07D401/06

    摘要： A compound having the following formula wherein A is —O—; B is alkylene or alkenylene optionally containing —O—, —S—, —(NR7)—, —CO— or —N═; R1 and R2 are alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, wherein the alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl is unsubstituted or substituted by halogen, cycloalkyl, aryl, adamantyl or amino; R3 is a substituted or unsubstituted pyridine ring; R5 and R6 are hydrogen or alkyl; R7 is hydrogen or alkyl; X is O or S; and each hydrogen of the said amino is unsubstituted or substituted by alkyl, alkoxycarbonyl, cycloalkyloxycarbonyl, arylalkoxycarbonyl or halogenoalkyloxycarbonyl. The compound is a TNF-α production inhibitor that is useful for treating autoimmune diseases such as rheumatoid arthritis.

    摘要翻译： 具有下式的化合物其中A是-O-; B是任选含有-O - ， - S - ， - （NR 7） - ， - CO-或-N =的亚烷基或亚烯基; R1和R2是烷基，烯基，炔基，环烷基或环烯基，其中烷基，烯基，炔基，环烷基或环烯基是未取代的或被卤素，环烷基，芳基，金刚烷基或氨基取代; R3是取代或未取代的吡啶环; R5和R6是氢或烷基; R7是氢或烷基; X是O或S; 并且所述氨基的每个氢未被取代或被烷基，烷氧基羰基，环烷氧基羰基，芳基烷氧基羰基或卤代烷氧基羰基取代。 该化合物是可用于治疗自身免疫疾病如类风湿性关节炎的TNF-α产生抑制剂。