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    Unsymmetrical cyclic diamine compound
    2.
    发明申请
    Unsymmetrical cyclic diamine compound 失效
    不对称环状二胺化合物

    公开(公告)号：US20030022887A1

    公开(公告)日：2003-01-30

    申请号：US09893699

    申请日：2001-06-29

    申请人： Kowa Co., Ltd.

    发明人： Tatsuhiko Komada ,  Masahiro Tamura ,  Toshiaki Oda ,  Yukiyoshi Yamazaki ,  Masahiro Nishikawa ,  Shunji Takemura ,  Takeshi Doi ,  Yoshinori Kyotani

    IPC分类号： A61K031/55 ,  A61K031/551 ,  A61K031/496 ,  A61K031/444 ,  C07D43/14

    CPC分类号： C07D213/81 ,  C07D213/36 ,  C07D213/82 ,  C07D401/12

    摘要： A cyclic diamine compound of formula (1): 1 wherein A is (CH2)n, (CH2)nnullCHnullCH, COnull(CH2)n or COnull(CH2)nnullCHnullCH, in which n is a number of 0 to 3; Z represents a formula (2) or (3): 2 in which R1, R2, R4, R5 and R6 are individually a hydrogen atom, alkyl group, alkoxy group, halogen atom or nitro group; R3 is a hydrogen atom, alkyl group, alkoxy group, halogen atom, nitro group, naphthyl group, or phenyl group which may be substituted by 1 to 3 substituents selected from the group consisting of alkyl groups, alkoxy groups, halogen atoms, a nitro group and a phenyl group; and X and Y are individually CH or a nitrogen atom; and m is 1 or 2; an acid-addition salt thereof, or a hydrate thereof, and a medicine containing such a compound.

    摘要翻译： 式（1）的环状二胺化合物：其中A为（CH 2）n，（CH 2）n -CH = CH，CO-（CH 2）n或CO-（CH 2）n -CH = CH，其中n为 数字0到3; Z表示式（2）或（3）：其中R1，R2，R4，R5和R6分别为氢原子，烷基，烷氧基，卤素原子或硝基; R3是氢原子，烷基，烷氧基，卤素原子，硝基，萘基或可以被1〜3个选自烷基，烷氧基，卤原子，硝基的取代基取代的苯基 基团和苯基; X和Y分别是CH或氮原子; m为1或2; 其酸加成盐或其水合物，以及含有这种化合物的药物。

    Water-soluble phenylpyridazine compounds and compositions containing the same
    4.
    发明申请
    Water-soluble phenylpyridazine compounds and compositions containing the same 失效
    水溶性苯基哒嗪化合物及其组合物

    公开(公告)号：US20040002497A1

    公开(公告)日：2004-01-01

    申请号：US10396726

    申请日：2003-03-26

    申请人： KOWA CO., LTD.

    发明人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

    IPC分类号： A61K031/501 ,  A61K031/50 ,  C07D43/02 ,  C07D237/02

    CPC分类号： A61K31/50 ,  A61K31/501 ,  C07D237/14 ,  C07D237/24

    摘要： Compounds having the formula (1): 1 wherein R1 represents an alkyl or alkenyl group, R2 and R3 each independently represents a hydrogen atom or an alkyl, hydroxyalkyl, dihydroxyalkyl or alkynyl group, or R2 and R3 may be fused together with the adjacent nitrogen atom to form a substituted or unsubstituted, nitrogen-containing, saturated heterocyclic group, X, Y and Z each independently represents a hydrogen atom, an alkyl group, a halogen atom or the like, and n stands for an integer of from 1 to 5; and also to pharmaceutical compositions containing them. These compounds have inhibitory activity against IL-1null production, high water solubility and good oral absorbability.

    摘要翻译： 具有式（1）的化合物：其中R 1表示烷基或烯基，R 2和R 3各自独立地表示氢原子或烷基，羟基烷基，二羟基烷基或炔基，或R 2 >和R 3可以与相邻的氮原子一起形成取代或未取代的含氮饱和杂环基，X，Y和Z各自独立地表示氢原子，烷基，卤素原子或 n，n表示1〜5的整数， 以及含有它们的药物组合物。 这些化合物对IL-1β生产具有抑制活性，水溶性高，口服吸收性好。

    Novel pyridazine derivatives and medicines containing the same as effective ingredients
    5.
    发明申请
    Novel pyridazine derivatives and medicines containing the same as effective ingredients 审中-公开
    新颖的哒嗪衍生物和含有与有效成分相同的药物

    公开(公告)号：US20040147516A1

    公开(公告)日：2004-07-29

    申请号：US10757525

    申请日：2004-01-15

    申请人： Kowa Co., Ltd.

    发明人： Masao Ohkuchi ,  Yoshinori Kyotani ,  Hiromichi Shigyo ,  Tomoyuki Koshi ,  Takahiro Kitamura ,  Tadaaki Ohgiya ,  Takayuki Matsuda ,  Yukiyoshi Yamazaki ,  Natsuyo Kumai ,  Kyoko Kotaki ,  Hideo Yoshizaki ,  Yuriko Habata

    IPC分类号： A61K031/501 ,  C07D43/02

    CPC分类号： C07D401/04 ,  C07D237/02 ,  C07D237/04 ,  C07D237/14 ,  C07D237/18 ,  C07D401/06 ,  C07D401/14 ,  C07D413/04

    摘要： This invention relates to pyridazine derivatives represented by the formula (1): 1 wherein R1 represents a (substituted) aryl group, R2 represents a phenyl group substituted at 4-position by a lower alkoxyl group or a lower alkylthio group, R3 represents a lower alkoxyl group, a halogenated lower alkyl group, a lower cycloalkyl group, a (subsituted) aryl group, a (substituted) aryloxy group, a (substituted) nitrogen-containing heterocyclic ring residue, a (substituted) aminocarbonyl group or a lower alkylcarbonyl group, A represents a single bond, a lower alkylene group or a lower alkenylene group, X represents O or S, and the dashed line indicates that the carbon-carbon bond between the 4-position and the 5-position is a single bond or a double bond, or salts thereof; and also to medicines containing them as effective ingredients. These compounds have excellent inhibitory activity against interleukin-1null production, and are useful as preventives and therapeutics for immune system diseases, inflammatory diseases, ischemic diseases and the like.

    摘要翻译： 本发明涉及由式（1）表示的哒嗪衍生物：其中R 1表示（取代的）芳基，R 2表示在4-位被低级烷氧基或低级烷硫基取代的苯基 R 3表示低级烷氧基，卤代低级烷基，低级环烷基，（取代的）芳基，（取代的）芳氧基，（取代的）含氮杂环残基，（取代的） ）氨基羰基或低级烷基羰基，A表示单键，低级亚烷基或低级亚烯基，X表示O或S，虚线表示4-位和5位之间的碳 - 碳键 - 位是单键或双键，或其盐; 以及含有它们作为有效成分的药物。 这些化合物对白细胞介素-1β生产具有优异的抑制活性，可用作免疫系统疾病，炎性疾病，缺血性疾病等的预防药物和治疗剂。

    Cyclic amine compounds and pharmaceutical composition containing the same
    6.
    发明申请
    Cyclic amine compounds and pharmaceutical composition containing the same 失效
    环胺化合物和含有其的药物组合物

    公开(公告)号：US20040010147A1

    公开(公告)日：2004-01-15

    申请号：US10191534

    申请日：2002-07-10

    申请人： KOWA CO., LTD.

    发明人： Tatsuhiko Kodama ,  Masahiro Tamura ,  Toshiaki Oda ,  Yukiyoshi Yamazaki ,  Masahiro Nishikawa ,  Shunji Takemura ,  Takeshi Doi ,  Yoshinori Kyotani ,  Masao Ohkuchi

    IPC分类号： C07D41/14 ,  C07D41/02

    CPC分类号： C07D401/06 ,  A61K31/4545 ,  C07D211/58 ,  C07D211/62 ,  C07D213/38 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14

    摘要： A cyclic amine compound represented by the following general formula (1): 1 wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group; W1 and W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.

    摘要翻译： 由下列通式（1）表示的环胺化合物：其中，R 1，R 2和R 3各自独立地表示氢原子或烷氧基; W 1和W 2各自独立地表示N或CH; X表示O，NR 4，CONR 4或NR 4 CO; R 4表示氢原子，或烷基，芳基，杂芳基，芳烷基或杂芳烷基; l，m和n各自表示0或1的数，其盐及其水合物。 这些化合物对细胞粘附和细胞浸润具有抑制作用，并且可用作抗哮喘药，抗过敏剂，抗风湿剂，抗动脉硬化剂，抗炎剂，抗干燥素综合征剂等。

    Water-soluble phenylpyridazine compounds and compositions containing the same
    7.
    发明申请
    Water-soluble phenylpyridazine compounds and compositions containing the same 失效
    水溶性苯基哒嗪化合物及其组合物

    公开(公告)号：US20030119838A1

    公开(公告)日：2003-06-26

    申请号：US10253523

    申请日：2002-09-25

    申请人： KOWA CO., LTD.

    发明人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

    IPC分类号： A61K031/501 ,  A61K031/50 ,  C07D43/02 ,  C07D237/02

    CPC分类号： C07D237/14 ,  A61K31/50 ,  A61K31/501 ,  C07D237/24

    摘要： Compounds having the formula (1): 1 wherein R1 represents an alkyl or alkenyl group, R2 and R3 each independently represent a hydrogen atom or an alkyl, hydroxyalkyl, dihydroxyalkyl or alkynyl group, or R2 and R3 may be fused together with the adjacent nitrogen atom to form a substituted or unsubstituted, nitrogen-containing, saturated heterocyclic group, X, Y and Z each independently represent a hydrogen atom, an alkyl group, a halogen atom or the like, and n stands for an integer of from 1 to 5; and also to medicinal compositions containing them. These compounds have inhibitory activity against IL-1null production, high water solubility and good oral absorbability.

    摘要翻译： 具有式（1）的化合物：其中R 1表示烷基或烯基，R 2和R 3各自独立地表示氢原子或烷基，羟基烷基，二羟基烷基或炔基，或者R 2和R 3可以与相邻的氮原子 为了形成取代或未取代的含氮饱和杂环基，X，Y和Z各自独立地表示氢原子，烷基，卤素原子等，n表示1〜5的整数， 以及含有它们的药物组合物。 这些化合物对IL-1β生产具有抑制活性，水溶性高，口服吸收性好。

    Novel pyridazine derivatives and medicines containing the same as effective ingredients
    8.
    发明申请
    Novel pyridazine derivatives and medicines containing the same as effective ingredients 审中-公开
    新颖的哒嗪衍生物和含有与有效成分相同的药物

    公开(公告)号：US20020123496A1

    公开(公告)日：2002-09-05

    申请号：US09996804

    申请日：2001-11-30

    申请人： Kowa Co., Ltd.

    发明人： Masao Ohkuchi ,  Yoshinori Kyotani ,  Hiromichi Shigyo ,  Tomoyuki Koshi ,  Takahiro Kitamura ,  Tadaaki Ohgiya ,  Takayuki Matsuda ,  Yukiyoshi Yamazaki ,  Natsuyo Kumai ,  Kyoko Kotaki ,  Hideo Yoshizaki ,  Yuriko Habata

    IPC分类号： C07D43/02 ,  A61K031/50 ,  A61K031/501

    CPC分类号： C07D401/04 ,  C07D237/02 ,  C07D237/04 ,  C07D237/14 ,  C07D237/18 ,  C07D401/06 ,  C07D401/14 ,  C07D413/04

    摘要： This invention relates to pyridazine derivatives represented by the formula (1): 1 wherein R1 represents a (substituted) aryl group, R2 represents a phenyl group substituted at 4-position by a lower alkoxyl group or a lower alkylthio group, R3 represents a lower alkoxyl group, a halogenated lower alkyl group, a lower cycloalkyl group, a (subsituted) aryl group, a (substituted) aryloxy group, a (substituted) nitrogen-containing heterocyclic ring residue, a (substituted) aminocarbonyl group or a lower alkylcarbonyl group, A represents a single bond, a lower alkylene group or a lower alkenylene group, X represents O or S, and the dashed line indicates that the carbon-carbon bond between the 4-position and the 5-position is a single bond or a double bond, or salts thereof; and also to medicines containing them as effective ingredients. These compounds have excellent inhibitory activity against interleukin-1null production, and are useful as preventives and therapeutics for immune system diseases, inflammatory diseases, ischemic diseases and the like.

    摘要翻译： 本发明涉及由式（1）表示的哒嗪衍生物：其中R1表示（取代的）芳基，R2表示通过低级烷氧基或低级烷硫基在4位被取代的苯基，R3表示低级烷氧基 基团，卤代低级烷基，低级环烷基，（取代的）芳基，（取代的）芳氧基，（取代的）含氮杂环残基，（取代的）氨基羰基或低级烷基羰基， A表示单键，低级亚烷基或低级亚烯基，X表示O或S，虚线表示4-位和5-位之间的碳 - 碳键为单键或双键 键或其盐; 以及含有它们作为有效成分的药物。 这些化合物对白细胞介素-1β生产具有优异的抑制活性，可用作免疫系统疾病，炎性疾病，缺血性疾病等的预防药物和治疗剂。