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    Novel Heterocyclidene Acetamide Derivative
    1.
    发明申请
    Novel Heterocyclidene Acetamide Derivative 有权
    新型杂环亚乙基乙酰胺衍生物

    公开(公告)号：US20080287428A1

    公开(公告)日：2008-11-20

    申请号：US11988659

    申请日：2006-07-24

    申请人： Hideharu Uchida ,  Naoto Kosuga ,  Tsutomu Satoh ,  Daido Hotta ,  Tomoyuki Kamino ,  Yoshitaka Maeda ,  Ken-ichi Amano ,  Yasushige Akada

    发明人： Hideharu Uchida ,  Naoto Kosuga ,  Tsutomu Satoh ,  Daido Hotta ,  Tomoyuki Kamino ,  Yoshitaka Maeda ,  Ken-ichi Amano ,  Yasushige Akada

    IPC分类号： A61K31/5383 ,  C07D405/02 ,  A61K31/4709 ,  C07D313/08 ,  A61K31/335 ,  C07D498/04

    CPC分类号： C07D405/12 ,  C07D215/14 ,  C07D215/38 ,  C07D313/08 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

    摘要： A compound represented by formula (I′): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q′ represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.

    摘要翻译： 由式（I'）表示的化合物：其中m，n和p各自表示0〜2; q表示0或1; R 1表示卤素，烃基，杂环基， 烷氧基，烷氧基羰基，氨磺酰基，CN基，NO 2 2基等; R 2表示卤素，氨基，烃基， 芳族杂环基或氧代基; X 1表示O，-NR 3 - 或-S（O）r - ; X 2， SUB>表示亚甲基，O，-NR 3 - 或-S（O）r - ; Q'表示杂芳基，杂芳基烷基，取代的芳基或芳烷基 ;环状部分表示芳基环或杂芳基环;波浪线表示E-异构体或Z-异构体），化合物的盐或化合物或其盐的溶剂合物。 药物组合物和瞬时受体电位型I（TRPV1）受体拮抗剂各自含有化合物，化合物的盐和化合物或其盐的溶剂合物中的至少一种作为活性成分。

    Heterocyclidene acetamide derivative
    3.
    发明授权
    Heterocyclidene acetamide derivative 有权
    杂环亚乙酰胺衍生物

    公开(公告)号：US07910751B2

    公开(公告)日：2011-03-22

    申请号：US11988659

    申请日：2006-07-24

    申请人： Hideharu Uchida ,  Naoto Kosuga ,  Tsutomu Satoh ,  Daido Hotta ,  Tomoyuki Kamino ,  Yoshitaka Maeda ,  Ken-ichi Amano ,  Yasushige Akada

    发明人： Hideharu Uchida ,  Naoto Kosuga ,  Tsutomu Satoh ,  Daido Hotta ,  Tomoyuki Kamino ,  Yoshitaka Maeda ,  Ken-ichi Amano ,  Yasushige Akada

    IPC分类号： C07D313/00 ,  C07D309/00

    CPC分类号： C07D405/12 ,  C07D215/14 ,  C07D215/38 ,  C07D313/08 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

    摘要： A compound represented by formula (I′): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q′ represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.

    摘要翻译： 由式（I'）表示的化合物：其中m，n和p各自表示0〜2; q表示0或1; R1表示卤素，烃基，杂环基，烷氧基，烷氧基羰基， 氨磺酰基，CN基，NO 2基等; R 2表示卤素，氨基，烃基，芳香族杂环基或氧代基; X 1表示O，-NR 3 - 或-S（O） R 2; X 2表示亚甲基，O，-NR 3 - 或-S（O）r - ; Q'表示杂芳基，杂芳基烷基，取代的芳基或芳烷基; 环或杂芳环;波浪线表示E-异构体或Z-异构体），化合物的盐或化合物或其盐的溶剂合物。 药物组合物和瞬时受体电位型I（TRPV1）受体拮抗剂各自含有化合物，化合物的盐和化合物或其盐的溶剂合物中的至少一种作为活性成分。

    Heterocyclidene acetamide derivative
    4.
    发明授权
    Heterocyclidene acetamide derivative 失效
    杂环亚乙酰胺衍生物

    公开(公告)号：US08383839B2

    公开(公告)日：2013-02-26

    申请号：US13008456

    申请日：2011-01-18

    申请人： Hideharu Uchida ,  Naoto Kosuga ,  Tsutomu Satoh ,  Daido Hotta ,  Tomoyuki Kamino ,  Yoshitaka Maeda ,  Ken-ichi Amano ,  Yasushige Akada

    发明人： Hideharu Uchida ,  Naoto Kosuga ,  Tsutomu Satoh ,  Daido Hotta ,  Tomoyuki Kamino ,  Yoshitaka Maeda ,  Ken-ichi Amano ,  Yasushige Akada

    IPC分类号： C07D313/00 ,  C07D309/00

    CPC分类号： C07D405/12 ,  C07D215/14 ,  C07D215/38 ,  C07D313/08 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

    摘要： A compound represented by formula (I′): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q′ represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.

    摘要翻译： 由式（I'）表示的化合物：其中m，n和p各自表示0〜2; q表示0或1; R1表示卤素，烃基，杂环基，烷氧基，烷氧基羰基， 氨磺酰基，CN基，NO 2基等; R 2表示卤素，氨基，烃基，芳香族杂环基或氧代基; X 1表示O，-NR 3 - 或-S（O） R 2; X 2表示亚甲基，O，-NR 3 - 或-S（O）r - ; Q'表示杂芳基，杂芳基烷基，取代的芳基或芳烷基; 环或杂芳环;波浪线表示E-异构体或Z-异构体），化合物的盐或化合物或其盐的溶剂合物。 药物组合物和瞬时受体电位型I（TRPV1）受体拮抗剂各自含有化合物，化合物的盐和化合物或其盐的溶剂合物中的至少一种作为活性成分。

    3-hydroxy-5-arylisothiazole derivative
    5.
    发明授权
    3-hydroxy-5-arylisothiazole derivative 有权
    3-羟基-5-芳基异噻唑衍生物

    公开(公告)号：US08476287B2

    公开(公告)日：2013-07-02

    申请号：US13392350

    申请日：2010-12-24

    申请人： Akihiro Okano ,  Naoto Kosuga ,  Munetaka Ohkouchi ,  Daido Hotta ,  Muneyoshi Makabe

    发明人： Akihiro Okano ,  Naoto Kosuga ,  Munetaka Ohkouchi ,  Daido Hotta ,  Muneyoshi Makabe

    IPC分类号： A61K31/506 ,  A61K31/425 ,  A61K31/4436 ,  A61K31/4535 ,  C07D239/24 ,  C07D275/02 ,  C07D417/02

    CPC分类号： C07D275/03 ,  A61K9/1623 ,  A61K9/2018 ,  A61K9/4858 ,  C07D417/12 ,  C07D417/14

    摘要： [Problem]To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases.[Means of solving the problem]A compound of Formula (I): (where n is 0 to 2; p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is an aryl group which is optionally substituted with L or a heterocyclic group which is optionally substituted with L; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is O, S, —NR7—; and R1 to R7 are specific groups),a salt of the compound, or a solvate of the salt or the compound.

    摘要翻译： [问题]提供具有GPR40激动剂作用的新化合物，化合物的盐，盐或化合物等的溶剂合物作为活性成分的GPR40活化剂，特别是胰岛素促分泌素和 用于预防和/或治疗糖尿病，肥胖或其它疾病的药物。 解决问题的方法式（I）的化合物：（其中n为0〜2; p为0〜4; j为0〜3; k为0〜2，环A为 任选被L取代或被L取代的杂环基;环B是苯环，吡啶环或嘧啶环; X是O，S，-NR7-，R1至R7是特定基团） ，化合物的盐或盐或化合物的溶剂合物。