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    PPAR-activating compound and pharmaceutical composition comprising the compound
    1.
    发明授权
    PPAR-activating compound and pharmaceutical composition comprising the compound 有权
    PPAR活化化合物和包含该化合物的药物组合物

    公开(公告)号：US07183295B2

    公开(公告)日：2007-02-27

    申请号：US11407076

    申请日：2006-04-20

    申请人： Yukiyoshi Yamazaki ,  Tsutomu Toma ,  Masahiro Nishikawa ,  Hidefumi Ozawa ,  Ayumu Okuda ,  Takaaki Araki ,  Kazutoyo Abe ,  Soichi Oda

    发明人： Yukiyoshi Yamazaki ,  Tsutomu Toma ,  Masahiro Nishikawa ,  Hidefumi Ozawa ,  Ayumu Okuda ,  Takaaki Araki ,  Kazutoyo Abe ,  Soichi Oda

    IPC分类号： A61K31/4439 ,  C07D413/12 ,  C07D411/12 ,  C07D401/12

    CPC分类号： C07D413/12 ,  C07D263/58

    摘要： A compound represented by the following formula (1): (wherein each of R1 and R2, which may be identical to or different from each other, represents a hydrogen atom, a methyl group, or an ethyl group; each of R3a, R3b, R4a, and R4b, which may be identical to or different from each other, represents a hydrogen atom, a halogen atom, a nitro group, a hydroxyl group, a C1-4 alkyl group, a trifluoromethyl group, a C1-4 alkoxy group, a C1-4 alkylcarbonyloxy group, a di-C1-4 alkylamino group, a C1-4 alkylsulfonyloxy group, a C1-4 alkylsulfonyl group, a C1-4 alkylsulfinyl group, or a C1-4 alkylthio group, or R3a and R3b, or R4a and R4b may be linked together to form an alkylenedioxy group; X represents an oxygen atom, a sulfur atom, or N—R5 (R5 represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkylsulfonyl group, or a C1-4 alkyloxycarbonyl group); Y represents an oxygen atom, S(O)l (l is a number of 0 to 2), a carbonyl group, a carbonylamino group, an aminocarbonyl group, a sulfonylamino group, or an aminosulfonyl group; Z represents CH or N; n is a number of 1 to 6; and m is a number of 2 to 6) or a salt thereof; and therapeutic drugs containing any of such a compound or salt.

    摘要翻译： 由下式（1）表示的化合物：其中R 1和R 2各自可以相同或不同，表示氢原子 ，甲基或乙基; R 3a，R 3b，R 4a和R 4b中的每一个， 它们可以相同或不同，表示氢原子，卤素原子，硝基，羟基，C 1-4烷基，三氟甲基， C 1-4烷氧基，C 1-4烷基羰基氧基，二-C 1-4烷基氨基，C 1 -C 4烷基氨基， C 1-4烷基磺酰氧基，C 1-4烷基磺酰基，C 1-4烷基亚磺酰基或C 1〜 4个烷硫基或R 3a和R 3b，或R 4a和R 4b可以是 连接在一起形成亚烷基二氧基; X表示氧原子，硫原子或NR 5（R 5）表示氢原子，C

    PPAR-activating compound and pharmaceutical composition comprising the compound
    3.
    发明申请
    PPAR-activating compound and pharmaceutical composition comprising the compound 有权
    PPAR活化化合物和包含该化合物的药物组合物

    公开(公告)号：US20060189667A1

    公开(公告)日：2006-08-24

    申请号：US11407076

    申请日：2006-04-20

    申请人： Yukiyoshi Yamazaki ,  Tsutomu Toma ,  Masahiro Nishikawa ,  Hidefumi Ozawa ,  Ayumu Okuda ,  Takaaki Araki ,  Kazutoyo Abe ,  Soichi Oda

    发明人： Yukiyoshi Yamazaki ,  Tsutomu Toma ,  Masahiro Nishikawa ,  Hidefumi Ozawa ,  Ayumu Okuda ,  Takaaki Araki ,  Kazutoyo Abe ,  Soichi Oda

    IPC分类号： A61K31/428 ,  A61K31/423

    CPC分类号： C07D413/12 ,  C07D263/58

    摘要： A compound represented by the following formula (1): (wherein each of R1 and R2, which may be identical to or different from each other, represents a hydrogen atom, a methyl group, or an ethyl group; each of R3a, R3b, R4a, and R4b, which may be identical to or different from each other, represents a hydrogen atom, a halogen atom, a nitro group, a hydroxyl group, a C1-4 alkyl group, a trifluoromethyl group, a C1-4 alkoxy group, a C1-4 alkylcarbonyloxy group, a di-C1-4 alkylamino group, a C1-4 alkylsulfonyloxy group, a C1-4 alkylsulfonyl group, a C1-4 alkylsulfinyl group, or a C1-4 alkylthio group, or R3a and R3b, or R4a and R4b may be linked together to form an alkylenedioxy group; X represents an oxygen atom, a sulfur atom, or N—R5 (R5 represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkylsulfonyl group, or a C1-4 alkyloxycarbonyl group); Y represents an oxygen atom, S(O)l (l is a number of 0 to 2), a carbonyl group, a carbonylamino group, an aminocarbonyl group, a sulfonylamino group, or an aminosulfonyl group; Z represents CH or N; n is a number of 1 to 6; and m is a number of 2 to 6) or a salt thereof; and therapeutic drugs containing any of such a compound or salt.

    摘要翻译： 由下式（1）表示的化合物：其中R 1和R 2各自可以相同或不同，表示氢原子 ，甲基或乙基; R 3a，R 3b，R 4a和R 4b中的每一个， 它们可以相同或不同，表示氢原子，卤素原子，硝基，羟基，C 1-4烷基，三氟甲基， C 1-4烷氧基，C 1-4烷基羰基氧基，二-C 1-4烷基氨基，C 1 -C 4烷基氨基， C 1-4烷基磺酰氧基，C 1-4烷基磺酰基，C 1-4烷基亚磺酰基或C 1〜 4个烷硫基或R 3a和R 3b，或R 4a和R 4b可以是 连接在一起形成亚烷基二氧基; X表示氧原子，硫原子或NR 5（R 5）表示氢原子，C

    Preparation process of biphenylcarboxylic acid amide derivatives
    5.
    发明授权
    Preparation process of biphenylcarboxylic acid amide derivatives 失效
    联苯羧酸酰胺衍生物的制备方法

    公开(公告)号：US06787653B2

    公开(公告)日：2004-09-07

    申请号：US10162602

    申请日：2002-06-06

    申请人： Hiroyuki Ishiwata ,  Seiichi Sato ,  Mototsugu Kabeya ,  Soichi Oda

    发明人： Hiroyuki Ishiwata ,  Seiichi Sato ,  Mototsugu Kabeya ,  Soichi Oda

    IPC分类号： C07D21126

    CPC分类号： C07D295/192

    摘要： A process for preparing a biphenylcarboxylic acid amide derivative represented by the following formula (1): wherein, R1, R2 and R3 each independently represents a hydrogen atom or a substituent, which comprises reacting, in the presence of a metal catalyst, a halogenobenzoic acid derivative represented by the following formula (2): wherein, X represents a halogen atom with a compound represented by the following formula (3): wherein, R1, R2 and R3 have the same meanings as described above, and Y represents an leaving group having an element selected from the group consisting of boron, silicon, zinc, tin and magnesium; or salt thereof. According to the present invention, biphenylcarboxylic acid amide derivatives of the formula (1) or salts thereof having excellent inhibitory activity against IgE antibody production can be prepared by the reduced number of steps, conveniently, at lower cost and in a high yield.

    摘要翻译： 一种制备由下式（1）表示的联苯羧酸酰胺衍生物的方法：其中R 1，R 2和R 3各自独立地表示氢原子或取代基，其包括在 存在金属催化剂，由下式（2）表示的卤代苯甲酸衍生物：其中，X表示与下式（3）表示的化合物的卤素原子：其中，R 1，R 2和 R 3具有与上述相同的含义，Y表示具有选自硼，硅，锌，锡和镁的元素的离去基团; 或其盐。根据本发明，具有优异的抗IgE抗体产生抑制活性的式（1）的联苯基羧酸酰胺衍生物或其盐可以通过减少数量的步骤，以较低的成本和较高的成本 产量。

    Pyridazine derivatives and drugs containing the same as the active ingredient
    7.
    发明授权
    Pyridazine derivatives and drugs containing the same as the active ingredient 有权
    哒嗪衍生物和含有与活性成分相同的药物

    公开(公告)号：US06403586B1

    公开(公告)日：2002-06-11

    申请号：US09622897

    申请日：2000-08-31

    申请人： Masao Ohkuchi ,  Yoshinori Kyotani ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Tomoyuki Koshi ,  Takahiro Kitamura ,  Takayuki Matsuda ,  Soichi Oda ,  Yuriko Habata ,  Kyoko Kotaki

    发明人： Masao Ohkuchi ,  Yoshinori Kyotani ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Tomoyuki Koshi ,  Takahiro Kitamura ,  Takayuki Matsuda ,  Soichi Oda ,  Yuriko Habata ,  Kyoko Kotaki

    IPC分类号： A61K3150

    CPC分类号： C07D401/06 ,  C07D237/02 ,  C07D237/04 ,  C07D237/22 ,  C07D237/24 ,  C07D401/12

    摘要： This invention relates to pyridazine derivatives represented by the formula (1): wherein R1 represents a lower alkoxyl group, a lower alkylthio group or a halogen atom; R2 represents H, a lower alkoxyl group, a lower alkylthio group or a halogen atom; R3 represents a lower alkyl or lower alkenyl group, which may be substituted by one or more OHs, CNs, lower cycloalkyl groups, (substituted) aromatic groups or (substituted) carbamoyl groups; R4 represents COOH, a lower alkoxycarbonyl group, a (substituted) carbamoyl group, a (substituted) amino group, or a (substituted) ureido group; 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-1&bgr; 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表示低级烷氧基，低级烷硫基或卤素原子; R2表示H，低级烷氧基，低级烷硫基或卤素原子; R 3表示低级烷基或低级烯基，其可以被一个或多个OH，CN，低级环烷基，（取代的）芳族基团或（取代的）氨基甲酰基取代; R4表示COOH，低级烷氧基羰基，（取代）氨基甲酰基，（取代）氨基或（取代）脲基; 虚线表示4位和5位之间的碳 - 碳键为单键或双键，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。

    Bis(2-aryl-5-pyridyl) derivatives
    9.
    发明授权
    Bis(2-aryl-5-pyridyl) derivatives 失效
    双（2-芳基-5-吡啶基）衍生物

    公开(公告)号：US06890940B2

    公开(公告)日：2005-05-10

    申请号：US09893680

    申请日：2001-06-29

    申请人： Hiroyuki Ishiwata ,  Seiichi Sato ,  Mototsugu Kabeya ,  Soichi Oda ,  Makoto Suda ,  Manabu Shibasaki

    发明人： Hiroyuki Ishiwata ,  Seiichi Sato ,  Mototsugu Kabeya ,  Soichi Oda ,  Makoto Suda ,  Manabu Shibasaki

    IPC分类号： A61P37/00 ,  A61P37/08 ,  A61P43/00 ,  C07D213/74 ,  C07D401/14 ,  C07D405/14 ,  A61K31/44 ,  C07D213/00

    CPC分类号： C07D213/74 ,  C07D401/14 ,  C07D405/14

    摘要： A bis(2-aryl-5-pyridyl) compound having formula (1) or a salt thereof: wherein A is a substituted or unsubstituted aromatic hydrocarbon group, and X is a substituent having one of the following formulas (2) to (4): wherein, in formula (2), R1 is a hydrogen atom or a di(lower alkyl)amino(lower alkyl) group, and m is an integer of 1 or 2; in formula (3), Y1 and Y2 each is a nitrogen atom or a CH group, and n is 0 or an integer of 1 to 6; in formula (4), R2 and R3 each is a hydrogen atom or a lower alkyl group, Z represents a single bond, a substituted methylene group, a substituted imino group, an oxygen atom or a cycloalkylene group, and p and q each is 0 or an integer of 1 to 6.

    摘要翻译： 具有式（1）的双（2-芳基-5-吡啶基）化合物或其盐：其中A是取代或未取代的芳族烃基，X是具有下式（2）至（4）中的一个的取代基 ）其中，在式（2）中，R 1是氢原子或二（低级烷基）氨基（低级烷基）基团，m是1或2的整数; 在式（3）中，Y 1和Y 2各自为氮原子或CH基团，n为0或1至6的整数; 在式（4）中，R 2和R 3各自为氢原子或低级烷基，Z表示单键，取代亚甲基，取代亚氨基 基团，氧原子或亚环烷基，p和q各自为0或1〜6的整数。