Pyridazin-3-one derivatives and medicines containing the same
    7.
    发明授权
    Pyridazin-3-one derivatives and medicines containing the same 失效
    哒嗪-3-酮衍生物及含有其的药物

    公开(公告)号:US06680316B1

    公开(公告)日:2004-01-20

    申请号:US09926040

    申请日:2001-08-20

    IPC分类号: C07D23724

    CPC分类号: C07D237/24

    摘要: Objects of the invention are to provide compounds having excellent activity against interleukin-1&bgr; production and also medicines comprising them as effective ingredients. Pyridazin-3-one derivatives represented by the following formula (1): wherein Ar1 represents a substituted or unsubstituted aromatic group, Ar2 represents a phenyl group having a substituent at least at the 4-position thereof, R1 represents a linear or branched alkyl group, an alkyl group having a cyclic structure, a substituted or unsubstituted phenyl group or a substituted or unsubstituted phenyl(lower alkyl) group, and R2 represents a cyano group, a carboxyl group, a (lower alkoxy)carbonyl group, a substituted or unsubstituted lower alkyl group or a substituted or unsubstituted carbamoyl group, or salts thereof; and medicines comprising them as effective ingredients.

    摘要翻译: 本发明的目的是提供对白细胞介素-1β生产具有优异活性的化合物以及包含它们作为有效成分的药物。由下式(1)表示的哒嗪-3-酮衍生物:其中Ar 1表示取代或未取代的 芳基,Ar 2表示至少在其4位具有取代基的苯基,R 1表示直链或支链烷基,具有环状结构的烷基,取代或未取代的苯基或 取代或未取代的苯基(低级烷基),R 2表示氰基,羧基,(低级烷氧基)羰基,取代或未取代的低级烷基或取代或未取代的氨基甲酰基,或盐 的; 和包含它们作为有效成分的药物。

    Benzofuran derivative
    8.
    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

    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
    9.
    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

    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

    IPC分类号: A61K38/06 A61K38/02

    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。