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    Tetrazole derivatives
    1.
    发明授权
    Tetrazole derivatives 失效
    四唑衍生物

    公开(公告)号：US6117886A

    公开(公告)日：2000-09-12

    申请号：US357156

    申请日：1999-07-19

    申请人： Hendrik Timmerman ,  Mingqiang Zang ,  Kazuhiro Onogi ,  Takeo Deushi ,  Masahiro Tamura ,  Tsutomu Tohma ,  Yasushi Wada ,  Jiro Matsumoto ,  Toru Kanke

    发明人： Hendrik Timmerman ,  Mingqiang Zang ,  Kazuhiro Onogi ,  Takeo Deushi ,  Masahiro Tamura ,  Tsutomu Tohma ,  Yasushi Wada ,  Jiro Matsumoto ,  Toru Kanke

    IPC分类号： A61P11/06 ,  C07D401/14 ,  A61K31/4709

    CPC分类号： C07D401/14

    摘要： The present invention is directed to a tetrazole derivative represented by the following formula (1) or a salt thereof: ##STR1## wherein R.sup.1 and R.sup.2 independently represent a hydrogen atom, a hydroxyl group, a lower alkyl group, a substituted or unsubstituted alkoxy group, or a substituted or unsubstituted alkanoyloxy group; R.sup.3 represents a hydrogen atom or a substituted or unsubstituted lower alkyl group; A represents a methyleneoxy group or a vinylene group; Z represents a substituted or unsubstituted benzimidazolyl group; and a broken line indicates that there may be a double bond; and to a medicine containing the compound as an active ingredient. The medicine according to the present invention is endowed with excellent antileukotriene activity and antihistaminic activity, and is useful for the prevention and treatment of, for example, asthma.

    摘要翻译： 本发明涉及由下式（1）表示的四唑衍生物或其盐：其中R1和R2独立地表示氢原子，羟基，低级烷基，取代或未取代的烷氧基或 取代或未取代的烷酰氧基; R3表示氢原子或取代或未取代的低级烷基; A表示亚甲氧基或亚乙烯基; Z表示取代或未取代的苯并咪唑基; 虚线表示可能存在双键; 和含有该化合物作为活性成分的药物。 根据本发明的药物具有优异的抗白三烯活性和抗组胺活性，可用于预防和治疗例如哮喘。

    Tetrazole derivatives
    2.
    发明授权
    Tetrazole derivatives 失效
    四唑衍生物

    公开(公告)号：US6121286A

    公开(公告)日：2000-09-19

    申请号：US158774

    申请日：1998-09-23

    申请人： Hendrik Timmerman ,  Mingqiang Zang ,  Kazuhiro Onogi ,  Takeo Deushi ,  Masahiro Tamura ,  Tsutomu Tohma ,  Yasushi Wada ,  Jiro Matsumoto ,  Toru Kanke

    发明人： Hendrik Timmerman ,  Mingqiang Zang ,  Kazuhiro Onogi ,  Takeo Deushi ,  Masahiro Tamura ,  Tsutomu Tohma ,  Yasushi Wada ,  Jiro Matsumoto ,  Toru Kanke

    IPC分类号： A61P11/06 ,  C07D401/14 ,  A61K31/47

    CPC分类号： C07D401/14

    摘要： The present invention is directed to a tetrazole derivative represented by the following formula (1) or a salt thereof: ##STR1## wherein R.sup.1 and R.sup.2 independently represent a hydrogen atom, a hydroxyl group, a lower alkyl group, a substituted or unsubstituted alkoxy group, or a substituted or unsubstituted alkanoyloxy group; R.sup.3 represents a hydrogen atom or a substituted or unsubstituted lower alkyl group; A represents a methyleneoxy group or a vinylene group; B represents a substituted or unsubstituted quinolyl group, a substituted or unsubstituted quinazolyl group, or a substituted or unsubstituted benzimidazolyl group; and a broken line indicates that there may be a double bond; and to a medicine containing the compound as an active ingredient. The medicine according to the present invention is endowed with excellent antileukotriene activity and antihistaminic activity, and is useful for the prevention and treatment of, for example, asthma.

    摘要翻译： 本发明涉及由下式（1）表示的四唑衍生物或其盐：其中R1和R2独立地表示氢原子，羟基，低级烷基，取代或未取代的烷氧基或 取代或未取代的烷酰氧基; R3表示氢原子或取代或未取代的低级烷基; A表示亚甲氧基或亚乙烯基; B表示取代或未取代的喹啉基，取代或未取代的喹唑基，或取代或未取代的苯并咪唑基; 虚线表示可能存在双键; 和含有该化合物作为活性成分的药物。 根据本发明的药物具有优异的抗白三烯活性和抗组胺活性，可用于预防和治疗例如哮喘。

    Pharmaceutical composition for delayed hypersensitivity
    4.
    发明申请
    Pharmaceutical composition for delayed hypersensitivity 审中-公开
    用于延迟超敏反应的药物组合物

    公开(公告)号：US20060183664A1

    公开(公告)日：2006-08-17

    申请号：US10496851

    申请日：2002-12-13

    申请人： Toshiaki Takizawa ,  Masaki Tamiya ,  Naohiro Saito ,  Toru Kanke ,  Jiro Matsumoto ,  Yasushi Wada ,  Junichi Kawagoe ,  William Ferrell ,  John Lockhart

    发明人： Toshiaki Takizawa ,  Masaki Tamiya ,  Naohiro Saito ,  Toru Kanke ,  Jiro Matsumoto ,  Yasushi Wada ,  Junichi Kawagoe ,  William Ferrell ,  John Lockhart

    IPC分类号： A61K38/54

    CPC分类号： A61K45/06 ,  A61K31/00 ,  Y02A50/423 ,  A61K2300/00

    摘要： The present invention provides a pharmaceutical composition by a novel action mechanism without serious side effects for delayed hypersensitivity and a screening method of the same. The invention also provides a novel assay method of inhibitors/suppressive agents of PAR-2. The invention relates to a pharmaceutical composition for delayed hypersensitivity containing one or two or more active ingredients selected from the group consisting of inhibitors of PAR-2 and suppressive agents of PAR-2 gene expression and a pharmaceutically acceptable carrier, and to a method for screening active ingredients for pharmaceutical composition for delayed hypersensitivity by contacting a subject substance with cells expressing PAR-2 and by determining expression or activity of PAR-2. The invention also relates to a method for detecting or quantifying actions of the subject substance for PAR-2 using cells expressing PAR-2 in a culture containing inositol.

    摘要翻译： 本发明通过新颖的作用机理提供药物组合物，对迟发性超敏反应没有严重的副作用及其筛选方法。 本发明还提供了PAR-2抑制剂/抑制剂的新型测定方法。 本发明涉及一种用于延迟超敏反应的药物组合物，其含有选自PAR-2的抑制剂和PAR-2基因表达的抑制剂的一种或两种以上活性成分和药学上可接受的载体，以及筛选方法 通过使受试物质与表达PAR-2的细胞接触并通过测定PAR-2的表达或活性来延迟超敏反应的药物组合物的活性成分。 本发明还涉及使用含有肌醇的培养物中表达PAR-2的细胞检测或定量PAR-2的物质的作用的方法。

    Method for treatment of kidney diseases
    5.
    发明授权
    Method for treatment of kidney diseases 失效
    肾脏疾病治疗方法

    公开(公告)号：US07423009B2

    公开(公告)日：2008-09-09

    申请号：US10673380

    申请日：2003-09-30

    申请人： Takashi Nakagawa ,  Hiroyuki Ishiwata ,  Toshiaki Takizawa ,  Toru Kanke ,  Yasushi Wada ,  Junichi Kawagoe

    发明人： Takashi Nakagawa ,  Hiroyuki Ishiwata ,  Toshiaki Takizawa ,  Toru Kanke ,  Yasushi Wada ,  Junichi Kawagoe

    IPC分类号： A61K38/00 ,  A61K38/43 ,  A61K38/48

    CPC分类号： A61K38/4846 ,  A61K38/08 ,  A61K38/482 ,  A61K38/4826 ,  G01N33/6893 ,  G01N2500/00 ,  G01N2800/347

    摘要： The present invention relates to a composition for prevention and treatment of kidney diseases comprising one or more effective component(s) of a PAR-2 activating agent which is able to activate PAR-2 and a pharmaceutically acceptable carrier. The present invention further relates to a method for prevention and treatment of kidney diseases comprising administration of a composition for prevention and treatment of kidney diseases containing a PAR-2 activating agent which is able to activate PAR-2 to patients suffering from kidney diseases, and also relates to the use of a PAR-2 activating agent which is able to activate PAR-2 for the manufacture of a composition for prevention and treatment of kidney diseases. The present invention furthermore relates to a method for screening an effective ingredient for prevention and treatment of kidney diseases comprising screening of the activating action of the test substance to PAR-2.

    摘要翻译： 本发明涉及一种用于预防和治疗肾脏疾病的组合物，其包含能够激活PAR-2的PAR-2活化剂的一种或多种有效成分和药学上可接受的载体。 本发明还涉及一种用于预防和治疗肾脏疾病的方法，其包括给予含有能够使患有肾脏疾病的患者PAR-2的PAR-2激活剂的肾脏疾病的预防和治疗组合物，以及 还涉及能够激活PAR-2用于制备用于预防和治疗肾脏疾病的组合物的PAR-2活化剂的用途。 本发明还涉及筛选用于预防和治疗肾脏疾病的有效成分的方法，其包括将测试物质的活化作用筛选到PAR-2。

    PAR-2 agonist
    6.
    发明授权
    PAR-2 agonist 失效
    PAR-2激动剂

    公开(公告)号：US08133864B2

    公开(公告)日：2012-03-13

    申请号：US11909931

    申请日：2006-03-29

    申请人： Hiroyuki Ishiwata ,  Mototsugu Kabeya ,  Toru Kanke

    发明人： Hiroyuki Ishiwata ,  Mototsugu Kabeya ,  Toru Kanke

    IPC分类号： A61K38/08 ,  C07K5/083 ,  C07K5/087

    CPC分类号： C07K5/0812 ,  A61K38/00 ,  C07K5/101 ,  C07K5/1016

    摘要： The present invention relates to a pharmaceutical composition for preventing/treating conditions associated with PAR-2. The present invention also relates to a method for preventing/treating the condition using the pharmaceutical composition and use for manufacturing the pharmaceutical composition. The pharmaceutical composition comprises a compound represented by the following general formula (1), salt or solvate thereof and a pharmaceutically acceptable carrier: Ar—CO—AA1—AA2—AA3—AA4—NH—X—Y (1) wherein, Ar represents a phenyl group or an aromatic heterocyclic group optionally having substituent(s): AA1 represents a hydrophobic amino acid: AA2 represents an amino acid absent of substituent(s) having more than two carbon atoms: AA3 represents an amino acid absent of substituent(s) having more than two carbon atoms: AA4 represents a basic amino acid: X represents a straight chain or branched bivalent saturated aliphatic hydrocarbon group having 1 to 6 carbon atoms: Y represents basic substituent(s); straight chain, branched, or cyclic bivalent saturated aliphatic hydrocarbon group having 1 to 6 carbon atoms; or an aromatic hydrocarbon group having 6 to 10 carbon atoms. The compound represented by the general formula (1) has dramatically improved PAR-2 activation potency compared to peptide comprised of 6 amino acids (Tethered receptor agonist peptide: TRAP) in spite of reduction of the number of amino acid.

    摘要翻译： 本发明涉及用于预防/治疗与PAR-2相关的病症的药物组合物。 本发明还涉及使用药物组合物预防/治疗病症的方法以及用于制造药物组合物的方法。 药物组合物包含由以下通式（1）表示的化合物，其盐或溶剂合物和药学上可接受的载体：Ar-CO-AA1-AA2-AA3-AA4-NH-X-Y（1）其中Ar表示 任选具有取代基的苯基或芳族杂环基：AA1表示疏水性氨基酸：AA2表示不具有多于两个碳原子的取代基的氨基酸：AA3表示不存在取代基的氨基酸（s ）：AA4表示碱性氨基酸：X表示具有1〜6个碳原子的直链或支链二价饱和脂肪族烃基：Y表示碱性取代基; 具有1至6个碳原子的直链，支链或环状二价饱和脂族烃基; 或碳原子数为6〜10的芳香族烃基。 尽管氨基酸数量的减少，但由通式（1）表示的化合物与包含6个氨基酸的肽（束缚受体激动剂肽：TRAP）相比，显着提高了PAR-2的活化效力。

    Par-2 Antagonists
    7.
    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。

    PAR-2 antagonists
    10.
    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。