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    PAR-2 AGONIST
    1.
    发明申请
    PAR-2 AGONIST 失效

    公开(公告)号：US20090131330A1

    公开(公告)日：2009-05-21

    申请号：US11722952

    申请日：2005-12-27

    申请人： Hiroyuki Ishiwata ,  Mototsugu Kabeya ,  Toru Kanke

    发明人： Hiroyuki Ishiwata ,  Mototsugu Kabeya ,  Toru Kanke

    IPC分类号： A61K38/00 ,  C07K5/00 ,  A61P1/00

    CPC分类号： C07K5/1016 ,  A61K38/00 ,  C07K7/06

    摘要： Disclosed is a compound represented by the following general formula (1): Ar—CO-AA1-AA2-AA3-AA4-NH—X—NR1R2 (1) (wherein Ar represents an optionally substituted phenyl group or an aromatic heterocyclic group; AA1 represents a hydrophobic amino acid; AA2 represents an unsubstituted amino acid containing 2 or more carbon atoms; AA3 represents an unsubstituted amino acid containing 2 or more carbon atoms; AA4 represents a hydrophobic amino acid; X represents a divalent saturated aliphatic hydrocarbon group having 2-6 carbon atoms; and R1 and R2 may be the same or different and independently represent a saturated or unsubstituted aliphatic hydrocarbon group having 1-8 carbon atoms, or alternatively R1 and R2 may form a ring together with an adjacent nitrogen atom), a salt thereof, or a solvate of them. Also disclosed is a pharmaceutical composition for prevention/treatment of diseases associated with PAR-2 which is composed of the compound represented by the above general formula (1), a salt thereof or a solvate of them and a pharmaceutically acceptable carrier.

    摘要翻译： 公开了由以下通式（1）表示的化合物：Ar-CO-AA1-AA2-AA3-AA4-NH-X-NR1R2（1）（其中Ar表示任选取代的苯基或芳族杂环基; AA1 表示疏水性氨基酸; AA2表示含有2个以上碳原子的未取代氨基酸; AA3表示含有2个以上碳原子的未取代氨基酸; AA4表示疏水性氨基酸; X表示二价饱和脂肪族烃基， 6个碳原子; R1和R2可以相同或不同，并且独立地表示具有1-8个碳原子的饱和或未取代的脂族烃基，或者R1和R2可以与相邻的氮原子一起形成环），盐 或它们的溶剂合物。 还公开了用于预防/治疗与由上述通式（1）表示的化合物，其盐或它们的溶剂化物和药学上可接受的载体组成的PAR-2相关疾病的药物组合物。

    Bis(2-aryl-5-pyridyl) derivatives
    3.
    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。

    PAR-2 antagonists
    4.
    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
    5.
    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。

    PAR-2 Agonist
    8.
    发明申请
    PAR-2 Agonist 失效
    PAR-2激动剂

    公开(公告)号：US20090215703A1

    公开(公告)日：2009-08-27

    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： A61K38/03 ,  C07K4/00 ,  A61P27/00

    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，其盐或溶剂化物和药学上可接受的载体：Ar-CO-AA1-AA2-AA3-AA4-NH-XY（1）其中Ar表示苯基 基团或任选具有取代基的芳族杂环基：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表示不具有取代基的氨基酸， 两个以上碳原子：AA4表示碱性氨基酸：X表示碳原子数1〜6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具有6至10个碳原子的芳族烃基。 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。