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    PAR-2 antagonists
    2.
    发明授权
    PAR-2 antagonists 失效
    PAR-2拮抗剂

    公开(公告)号：US08268789B2

    公开(公告)日：2012-09-18

    申请号：US11576304

    申请日：2005-09-30

    申请人： Mototsugu Kabeya ,  Kyoko Yasuoka ,  Toru Kanke ,  Hiroyuki Ishiwata ,  Junya Tagashira

    发明人： Mototsugu Kabeya ,  Kyoko Yasuoka ,  Toru Kanke ,  Hiroyuki Ishiwata ,  Junya Tagashira

    IPC分类号： A61K38/06 ,  A61K38/02

    CPC分类号： C07K5/0827 ,  A61K38/00 ,  C07D209/14 ,  C07K5/0806 ,  C07K5/0812

    摘要： Compounds represented by the general formula (1) or salts thereof or solvates of both; PAR-2 antagonists containing the compounds; and preventive or therapeutic agents for PAR-2 related diseases containing the antagonists as the active ingredient: (1) wherein R1 is hydrogen, halogeno, or a group represented by the general formula (2): (wherein R11 is straight-chain or branched C1-6 alkylene or the like; and R12 and R13 together with the nitrogen atom adjacent to them form a 5- to 7-membered ring); R2 is straight-chain or branched C1-6 alkyl or the like; R3 and R4 are each independently hydrogen, one to three halogen atoms, or the like; and A1-A2-A3 is a tripeptide residue composed of α-amino acids each independently selected from the group consisting of glycine, alanine, cyclohexylalanine, and so on.

    摘要翻译： 由通式（1）表示的化合物或其盐或两者的溶剂合物; 含有这些化合物的PAR-2拮抗剂; 以及含有拮抗剂作为活性成分的PAR-2相关疾病的预防或治疗剂：（1）其中R1是氢，卤素或由通式（2）表示的基团：（其中R11是直链或支链的 C 1-6亚烷基等; R 12和R 13与它们相邻的氮原子一起形成5-至7-元环）; R2是直链或支链C 1-6烷基等; R3和R4各自独立地为氢，一至三个卤素原子等; A1-A2-A3是由各自独立地选自甘氨酸，丙氨酸，环己基丙氨酸等的α-氨基酸组成的三肽残基。

    Process for Production of (1,3-Disubstituted Indolyl)-Urea Derivatives, Intermediates Therefor, and Process for Production of the Intermediates
    3.
    发明申请
    Process for Production of (1,3-Disubstituted Indolyl)-Urea Derivatives, Intermediates Therefor, and Process for Production of the Intermediates 审中-公开
    （1,3-二取代吲哚基） - 脲衍生物的制备方法，其中间体及其制备方法

    公开(公告)号：US20090012263A1

    公开(公告)日：2009-01-08

    申请号：US11576311

    申请日：2005-09-30

    申请人： Mototsugu Kabeya ,  Kyoko Yasuoka

    发明人： Mototsugu Kabeya ,  Kyoko Yasuoka

    IPC分类号： C07K5/083 ,  C07D209/04

    CPC分类号： C07K5/0827 ,  A61K38/00 ,  C07D209/14 ,  C07K5/0806 ,  C07K5/0812

    摘要： A process for the production of (1,3-disubstituted indolyl) urea derivatives represented by the general formula (1), characterized by reacting a 1-substituted-aminoindole derivative with a phenyl halocarbonate to form a carbamate derivative, subjecting the carbamate derivative to Mannich reaction with a secondary amine and formaldehyde to form a 3-aminomethylindole derivative represented by the general formula (6), and then reacting the derivative (6) with a peptide derivative; indole derivatives represented by the general formula (6) which are intermediates for the above process; and a process for the production of the indole derivatives.

    摘要翻译： 一种制备由通式（1）表示的（1,3-二取代的吲哚基）脲衍生物的方法，其特征在于使1-取代的 - 氨基吲哚衍生物与卤代碳酸苯酯反应形成氨基甲酸酯衍生物，使氨基甲酸酯衍生物 曼尼希与仲胺和甲醛反应形成由通式（6）表示的3-氨基甲基吲哚衍生物，然后使衍生物（6）与肽衍生物反应; 由通式（6）表示的作为上述方法的中间体的吲哚衍生物; 以及生产吲哚衍生物的方法。

    Benzofuran derivative
    6.
    发明授权
    Benzofuran derivative 失效
    苯并呋喃衍生物

    公开(公告)号：US07314877B2

    公开(公告)日：2008-01-01

    申请号：US10547779

    申请日：2004-03-03

    申请人： Seiichi Sato ,  Tomoyuki Koshi ,  Toshimi Mizoguchi ,  Kyoko Yasuoka ,  Natsuyo Kumai ,  Junko Totsuka ,  Masahiro Tamura ,  Masao Ohkuchi

    发明人： Seiichi Sato ,  Tomoyuki Koshi ,  Toshimi Mizoguchi ,  Kyoko Yasuoka ,  Natsuyo Kumai ,  Junko Totsuka ,  Masahiro Tamura ,  Masao Ohkuchi

    IPC分类号： C07D405/04 ,  A61K31/501

    CPC分类号： C07D405/04

    摘要： The present invention is directed to a compound represented by formula (1): (wherein R1 represents an alkyl group which may have a substituent or an alkenyl group which may have a substituent; and each of R2 and R3 represents a hydrogen atom, an alkyl group, a hydroxyalkyl group, a dihydroxyalkyl group, or an alkynyl group, or R2 and R3 form, together with the nitrogen atom adjacent thereto, a nitrogen-containing saturated heterocyclic group which may have a substituent) and a drug composition containing the compound. The compound exhibits tumor necrosis factor (TNF-α) production inhibitory effect and improved absorption upon oral administration.

    摘要翻译： 本发明涉及由式（1）表示的化合物：其中R 1表示可以具有取代基的烷基或可具有取代基的烯基; R 1， SO 2和R 3表示氢原子，烷基，羟基烷基，二羟基烷基或炔基，或R 2和 R 3形式与与其相邻的氮原子，可以具有取代基的含氮饱和杂环基）和含有该化合物的药物组合物。 该化合物表现出肿瘤坏死因子（TNF-α）产生抑制作用和口服给药改善吸收。

    Benzofuran derivative
    7.
    发明申请
    Benzofuran derivative 失效
    苯并呋喃衍生物

    公开(公告)号：US20060189621A1

    公开(公告)日：2006-08-24

    申请号：US10547779

    申请日：2004-03-03

    申请人： Seiichi Sato ,  Tomoyuki Koshi ,  Toshimi Mizoguchi ,  Kyoko Yasuoka ,  Junko Totsuka ,  Masahiro Tamura ,  Masao Ohkuchi

    发明人： Seiichi Sato ,  Tomoyuki Koshi ,  Toshimi Mizoguchi ,  Kyoko Yasuoka ,  Junko Totsuka ,  Masahiro Tamura ,  Masao Ohkuchi

    IPC分类号： A61K31/501 ,  C07D405/02

    CPC分类号： C07D405/04

    摘要： The present invention is directed to a compound represented by formula (1): (wherein R1 represents an alkyl group which may have a substituent or an alkenyl group which may have a substituent; and each of R2 and R3 represents a hydrogen atom, an alkyl group, a hydroxyalkyl group, a dihydroxyalkyl group, or an alkynyl group, or R2 and R3 form, together with the nitrogen atom adjacent thereto, a nitrogen-containing saturated heterocyclic group which may have a substituent) and a drug composition containing the compound. The compound exhibits tumor necrosis factor (TNF-α) production inhibitory effect and improved absorption upon oral administration.

    摘要翻译： 本发明涉及由式（1）表示的化合物：其中R 1表示可以具有取代基的烷基或可具有取代基的烯基; R 1， SO 2和R 3表示氢原子，烷基，羟基烷基，二羟基烷基或炔基，或R 2和 R 3形式与与其相邻的氮原子，可以具有取代基的含氮饱和杂环基）和含有该化合物的药物组合物。 该化合物表现出肿瘤坏死因子（TNF-α）产生抑制作用和口服给药改善吸收。

    Par-2 Antagonists
    10.
    发明申请
    Par-2 Antagonists 失效
    Par-2拮抗剂

    公开(公告)号：US20090012006A1

    公开(公告)日：2009-01-08

    申请号：US11576304

    申请日：2005-09-30

    申请人： Mototsugu Kabeya ,  Kyoko Yasuoka ,  Toru Kanke ,  Hiroyuki Ishiwata ,  Junya Tagashira

    发明人： Mototsugu Kabeya ,  Kyoko Yasuoka ,  Toru Kanke ,  Hiroyuki Ishiwata ,  Junya Tagashira

    IPC分类号： A61K38/06 ,  C07K5/083 ,  A61P35/00 ,  A61P11/06

    CPC分类号： C07K5/0827 ,  A61K38/00 ,  C07D209/14 ,  C07K5/0806 ,  C07K5/0812

    摘要： Compounds represented by the general formula (1) or salts thereof or solvates of both; PAR-2 antagonists containing the compounds; and preventive or therapeutic agents for PAR-2 related diseases containing the antagonists as the active ingredient: (1) wherein R1 is hydrogen, halogeno, or a group represented by the general formula (2): (wherein R11 is straight-chain or branched C1-6 alkylene or the like; and R12 and R13 together with the nitrogen atom adjacent to them form a 5- to 7-membered ring); R2 is straight-chain or branched C1-6 alkyl or the like; R3 and R4 are each independently hydrogen, one to three halogen atoms, or the like; and A1-A2-A3 is a tripeptide residue composed of α-amino acids each independently selected from the group consisting of glycine, alanine, cyclohexylalanine, and so on.

    摘要翻译： 由通式（1）表示的化合物或其盐或两者的溶剂合物; 含有这些化合物的PAR-2拮抗剂; 以及含有拮抗剂作为活性成分的PAR-2相关疾病的预防或治疗剂：（1）其中R1是氢，卤素或由通式（2）表示的基团：（其中R11是直链或支链的 C 1-6亚烷基等; R 12和R 13与它们相邻的氮原子一起形成5-至7-元环）; R2是直链或支链C 1-6烷基等; R3和R4各自独立地为氢，一至三个卤素原子等; 并且A1-A2-A3是由各自独立地选自甘氨酸，丙氨酸，环己基丙氨酸等的α-氨基酸组成的三肽残基。