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    Sulfonamide derivatives
    2.
    发明授权
    Sulfonamide derivatives 失效
    磺酰胺衍生物

    公开(公告)号：US06673804B1

    公开(公告)日：2004-01-06

    申请号：US09678294

    申请日：2000-10-02

    申请人： Tomio Kimura ,  Shoujiro Miyazaki ,  Keiji Ueda ,  Kazuhiko Tanzawa ,  Shigeru Ushiyama ,  Wataru Takasaki

    发明人： Tomio Kimura ,  Shoujiro Miyazaki ,  Keiji Ueda ,  Kazuhiko Tanzawa ,  Shigeru Ushiyama ,  Wataru Takasaki

    IPC分类号： C07D20946

    CPC分类号： C07D209/48 ,  C07C311/29 ,  C07D209/66 ,  C07D233/78 ,  C07D239/54 ,  C07D239/70 ,  C07D239/96 ,  C07D275/06 ,  C07D277/34 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D473/04 ,  C07D475/02 ,  C07D495/04

    摘要： A compound of the formula (I) or a pharmacologically acceptable salt, ester or other derivative thereof: R1 is H or NHOH. R2 is H, optionally substituted alkyl, cycloalkyl or a group —AR6. A is an alkylene which may be optionally interrupted by O, —S(O)m— or —N(R9). R6 is a group (II), (III), (IV) X is O, S, —N(R10)—, —C(R11)(R12)—. Y is O, CO, —S(O)n—, —N(R10)—, —C(R11)(R12)—. Each of R7 and R8 is H, alkyl, COOH, optionally substituted alkyl, etc. Each of R9, R10, R11, and R12 is H, alkyl, etc. Each of m and n is 0 to 2. R3 is H, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted alkenyl, optionally substituted alkynyl. R4 is optionally substituted (hetero)arylene. R5 is optionally substituted alkyl, optionally substituted (hetero)aryl. These compounds have matrixmetalloproteinase—13 inhibitory activity and aglycanase inhibitory activity.

    摘要翻译： 式（I）的化合物或其药理学上可接受的盐，酯或其它衍生物：R 1是H或NHOH。 R 2是H，任选取代的烷基，环烷基或基团-AR 6 .A是可以任选被O，-S（O）m - 或-N（R 9）间隔的亚烷基。 R 6为（II），（III），（IV）X为O，S，-N（R 10） - ， - C（R 11）（R 12） Y是O，CO，-S（O）n - ， - N（R 10） - ， - C（R 11）（R 12） - 。 R 7和R 8中的每一个是H，烷基，COOH，任选取代的烷基等。R 9，R 10，R 11和R 12中的每一个是H，烷基 等等。m和n各自为0至2.R 3为H，任选取代的烷基，任选取代的环烷基，任选取代的烯基，任选取代的炔基。 R 4是任选取代的（杂）亚芳基。 R 5是任选取代的烷基，任选取代的（杂）芳基。 这些化合物具有基质金属蛋白酶-13抑制活性和糖苷连结酶抑制活性。

    Heteroaryl-substituted pyrrole derivatives, their preparation and their therapeutic uses
    3.
    发明申请
    Heteroaryl-substituted pyrrole derivatives, their preparation and their therapeutic uses 审中-公开
    杂芳基取代的吡咯衍生物，其制备及其治疗用途

    公开(公告)号：US20060128756A1

    公开(公告)日：2006-06-15

    申请号：US11339390

    申请日：2006-01-25

    申请人： Tomio Kimura ,  Kazumasa Aoki ,  Akira Nakao ,  Shigeru Ushiyama ,  Takaichi Shimozato ,  Nobuyuki Ohkawa

    发明人： Tomio Kimura ,  Kazumasa Aoki ,  Akira Nakao ,  Shigeru Ushiyama ,  Takaichi Shimozato ,  Nobuyuki Ohkawa

    IPC分类号： C07D401/02 ,  A61K31/444 ,  C07D401/14

    CPC分类号： C07D451/02 ,  C07D401/04 ,  C07D401/14 ,  C07D453/02 ,  C07D455/02 ,  C07D471/04 ,  C07D487/04

    摘要： Compounds having activity against production of an inflammatory cytokine of formula (I)′: A′ is pyrrole; R1′ is phenyl or naphthyl; R2′ is pyridyl or pyrimidinyl; R3′ is (IIa)′, (IIb)′ or (IIc)′: m′ is 1; E′ is nitrogen; D′ is >C(R5′), R5′ is hydrogen, Substituent α′ or Substituent β′; B′ is nitrogen-containing 5-membered heterocyclic; R4′ is 1 to 3 substituents from Substituent α′, Substituent β′ and Substituent γ′; R1′ and R3′ are bonded to two atoms of the pyrrole adjacent to the pyrrole atom bonded to R2′; Substituent α′ is hydroxyl, nitro, cyano, halogen, alkoxy, halogeno alkoxy, alkylthio, halogeno alkylthio or —NRa′Rb′; Ra′ and Rb′ are hydrogen, alkyl, alkenyl, alkynyl, aralkyl or alkylsulfonyl, or Ra′ and Rb′ with the nitrogen atom form a heterocyclyl; Substituent β′ is alkyl, alkenyl, alkynyl, aralkyl or cycloalkyl; Substituent γ′is oxo, hydroxyimino, alkoxyimino, alkylene, alkylenedioxy, alkylsulfinyl, alkylsulfonyl, aryl, aryloxy, alkylidenyl or aralkylidenyl.

    摘要翻译： 具有抗式产生式（I）的炎性细胞因子的活性化合物的化合物：A'是吡咯; R 1是苯基或萘基; R 2是吡啶基或嘧啶基; （IIa）'，（IIb）'或（IIc）'：m'为1; E'是氮; D'是> C（R 5'），R 5'是氢，取代基α'或取代基β'; B'是含氮5元杂环; R 4'是1至3个取代基α'，取代基β'和取代基γ'的取代基; R 1'和R 3'连接到与R 2'连接的吡咯原子相邻的吡咯的两个原子上; 取代基α'是羟基，硝基，氰基，卤素，烷氧基，卤代烷氧基，烷硫基，卤代烷硫基或-NR a R b B。 R a，O和R b'是氢，烷基，烯基，炔基，芳烷基或烷基磺酰基，或者R a'和R“ b'与氮原子形成杂环基; 取代基β'是烷基，烯基，炔基，芳烷基或环烷基; 取代基γ'是氧代，羟基亚氨基，烷氧基亚氨基，亚烷基，亚烷基二氧基，烷基亚磺酰基，烷基磺酰基，芳基，芳氧基，亚烷基或芳亚烷基。

    Heteroaryl-substituted pyrrole derivatives, their preparation and their therapeutic uses
    5.
    发明申请
    Heteroaryl-substituted pyrrole derivatives, their preparation and their therapeutic uses 审中-公开
    杂芳基取代的吡咯衍生物，其制备及其治疗用途

    公开(公告)号：US20050283006A1

    公开(公告)日：2005-12-22

    申请号：US10411061

    申请日：2003-04-10

    申请人： Tomio Kimura ,  Kazumasa Aoki ,  Akira Nakao ,  Shigeru Ushiyama ,  Takaichi Shimozato ,  Nobuyuki Ohkawa ,  Takayoshi Nagasaki ,  Takanori Yamazaki

    发明人： Tomio Kimura ,  Kazumasa Aoki ,  Akira Nakao ,  Shigeru Ushiyama ,  Takaichi Shimozato ,  Nobuyuki Ohkawa ,  Takayoshi Nagasaki ,  Takanori Yamazaki

    IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D451/02 ,  C07D453/02 ,  C07D455/02 ,  C07D471/04 ,  C07D487/04 ,  C07D491/20 ,  C07D41/14 ,  C07D43/02

    CPC分类号： C07D451/02 ,  C07D401/04 ,  C07D401/14 ,  C07D453/02 ,  C07D455/02 ,  C07D471/04 ,  C07D487/04

    摘要： Compounds having activity against production of inflammatory cytokines of formula (I)′: A′ is pyrrole; R1′ is aryl or heteroaryl; R2′ is heteroaryl having at least one nitrogen atom; R3′ is (IIa)′, (IIb)′ or (IIc)′: m′ is 1 or 2; one of D′ and E′ is nitrogen and the other is >C(R5′)—, R5′ is hydrogen, Substituent α′ or Substituent β′; B′ is nitrogen-containing 4- to 7-membered heterocyclic; R4′ is 1 to 3 substituents from Substituent α′, Substituent β′ and Substituent γ′; R1′ and R3′ are bonded to two atoms of the pyrrole adjacent to the pyrrole atom bonded to R2′; Substituent α′: hydroxyl, nitro, cyano, halogen, alkoxy, halogeno alkoxy, alkylthio, halogeno alkylthio or —NRa′Rb′; Ra′ and Rb′ are hydrogen, alkyl, alkenyl, alkynyl, aralkyl or alkylsulfonyl, or Ra′ and Rb′ with the nitrogen atom form a heterocyclyl; Substituent β′: alkyl, alkenyl, alkynyl, aralkyl or cycloalkyl; Substituent γ′: oxo, hydroxyimino, alkoxyimino, alkylene, alkylenedioxy, alkylsulfinyl, alkylsulfonyl, aryl, aryloxy, alkylidenyl or aralkylidenyl.

    摘要翻译： 具有抗式产生式（I）的炎性细胞因子的化合物的化合物：A'是吡咯; R 1是芳基或杂芳基; R 2是具有至少一个氮原子的杂芳基; （IIa）'，（IIb）'或（IIc）'：m'为1或2; D'和E'之一是氮，另一个是> C（R 5'） - ，R 5'是氢，取代基α'或取代基β'; B'是含氮的4-至7-元杂环; R 4'是1至3个取代基α'，取代基β'和取代基γ'的取代基; R 1'和R 3'连接到与R 2'连接的吡咯原子相邻的吡咯的两个原子上; 取代基α'：羟基，硝基，氰基，卤素，烷氧基，卤代烷氧基，烷硫基，卤代烷硫基或-NR a R b b。 R a，O和R b'是氢，烷基，烯基，炔基，芳烷基或烷基磺酰基，或者R a'和R“ b'与氮原子形成杂环基; 取代基β'：烷基，烯基，炔基，芳烷基或环烷基; 取代基γ'：氧代，羟基亚氨基，烷氧基亚氨基，亚烷基，亚烷基二氧基，烷基亚磺酰基，烷基磺酰基，芳基，芳氧基，亚烷基或芳烷基。