Triazole derivative
    1.
    发明授权
    Triazole derivative 失效
    三唑衍生物

    公开(公告)号:US08022091B2

    公开(公告)日:2011-09-20

    申请号:US12278054

    申请日:2007-02-05

    CPC分类号: C07D249/08

    摘要: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2—, or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, R3 represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-10 carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).

    摘要翻译: 本发明的目的是提供具有抑制S1P与其受体Edg-1(S1P1)结合的作用的化合物,可用作药物化合物。 化合物或其药学上可接受的盐,其化合物由下式表示(其中A表示氧原子,硫原子,由式-SO-表示的基团,由式-SO2-表示的基团等) R1表示氢原子,具有1-6个碳原子的烷基等,R1A表示氢原子等,R2表示具有1-6个碳原子的烷基,具有3-6个碳原子的环烷基 原子等,R 3表示芳基,R 4表示氢原子或具有1-6个碳原子并且任选被羧基取代的烷基,R 5表示具有1-10个碳原子的烷基,环烷基 具有3-8个碳原子的基团,任选取代的芳基等)。

    Aminothiazole derivative
    3.
    发明授权
    Aminothiazole derivative 失效
    氨基噻唑衍生物

    公开(公告)号:US08637557B2

    公开(公告)日:2014-01-28

    申请号:US13502636

    申请日:2010-10-04

    CPC分类号: C07D417/04 C07D417/14

    摘要: A compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which has a PI3 kinase γ inhibitory effect and is useful as a prophylactic or therapeutic agent for articular rheumatism, Crohn's disease, irritable colitis, Sjoegren's syndrome, multiple sclerosis, systemic lupus erythematosus, asthma, atopic dermatitis, arteriosclerosis, organ transplant rejection, cancer, retinopathy, psoriasis, arthrosis deformans, age-related macular degeneration, type II diabetes, insulin resistance, obesity, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), hyperlipemia, etc.

    摘要翻译: 由式(1)表示的化合物或其药学上可接受的盐,其具有PI3激酶γ抑制作用,并且可用作关节风湿病,克罗恩病,过敏性结肠炎,Sjoegren综合征,多发性硬化症,系统性狼疮的预防或治疗剂 红斑狼疮,哮喘,特应性皮炎,动脉硬化,器官移植排斥,癌症,视网膜病变,牛皮癣,变形性关节炎,年龄相关性黄斑变性,II型糖尿病,胰岛素抵抗,肥胖,非酒精性脂肪性肝病(NAFLD),非酒精性 脂肪性肝炎(NASH),高脂血症等

    TRIAZOLE DERIVATIVE
    5.
    发明申请
    TRIAZOLE DERIVATIVE 审中-公开
    三唑衍生物

    公开(公告)号:US20110269960A1

    公开(公告)日:2011-11-03

    申请号:US13180011

    申请日:2011-07-11

    CPC分类号: C07D249/08

    摘要: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2—, or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, R3 represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-10 carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).

    摘要翻译: 本发明的目的是提供具有抑制S1P与其受体Edg-1(S1P1)结合的作用的化合物,可用作药物化合物。 化合物或其药学上可接受的盐,其化合物由下式表示(其中A表示氧原子,硫原子,由式-SO-表示的基团,由式-SO2-表示的基团等) R1表示氢原子,具有1-6个碳原子的烷基等,R1A表示氢原子等,R2表示具有1-6个碳原子的烷基,具有3-6个碳原子的环烷基 原子等,R 3表示芳基,R 4表示氢原子或具有1-6个碳原子并且任选被羧基取代的烷基,R 5表示具有1-10个碳原子的烷基,环烷基 具有3-8个碳原子的基团,任选取代的芳基等)。

    Thiazole derivative
    6.
    发明授权
    Thiazole derivative 失效
    噻唑衍生物

    公开(公告)号:US07678810B2

    公开(公告)日:2010-03-16

    申请号:US10591614

    申请日:2005-03-04

    摘要: A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein: X1 and X2 are different from each other and represent a sulfur atom or a carbon atom; R1 represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula. The present invention provides an inhibitory substance against ALK5 which is a TGF-β type I receptor and provides a hair growth stimulant or a hair growth agent based on its novel activities.

    摘要翻译: 由下式表示的噻唑咪唑衍生物或其药学上可接受的盐,以及ALK5抑制剂,秃发治疗剂或具有上述作为活性成分的毛发生长剂,其中:X1和X2彼此不同,表示 硫原子或碳原子; R1表示苯基; 取代的苯基; 与杂芳环稠合的苯基; 吡啶基; 或与杂芳环稠合的吡啶基; R2表示氢原子,卤素原子,碳原子数1〜6的烷基,碳原子数1〜5的碳原子数1〜5的烷基,碳原子数1〜6的烷氧基,烷氧基 具有1至5个碳原子,或具有1至6个碳原子的羟烷基,A表示由下式表示的基团。 本发明提供一种抗ALK5抑制物质,其为TGF- I型受体,并且基于其新的活性提供毛发生长兴奋剂或毛发生长剂。

    TRIAZOLE DERIVATIVE
    7.
    发明申请
    TRIAZOLE DERIVATIVE 失效
    三唑衍生物

    公开(公告)号:US20100041655A1

    公开(公告)日:2010-02-18

    申请号:US12278054

    申请日:2007-02-05

    CPC分类号: C07D249/08

    摘要: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2— or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).

    摘要翻译: 本发明的目的是提供具有抑制S1P与其受体Edg-1(S1P1)结合的作用的化合物,可用作药物化合物。 一种化合物或其药学上可接受的盐,该化合物由下式表示(其中A表示氧原子,硫原子,由式-SO-表示的基团,由式-SO2-等表示的基团, R1表示氢原子,具有1-6个碳原子的烷基等,R1A表示氢原子等,R2表示具有1-6个碳原子的烷基,具有3-6个碳原子的环烷基 等表示芳基,R 4表示氢原子或具有1-6个碳原子并且任选被羧基取代的烷基,R 5表示具有1个碳原子的烷基,环烷基具有3个 -8个碳原子,任选取代的芳基等)。