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    • 3. 发明授权
    • Modulator
    • 调制器
    • US08293796B2
    • 2012-10-23
    • US12707812
    • 2010-02-18
    • Masahiro OkuyamaDavid SelwoodCristina VisintinDavid BakerGareth Pryce
    • Masahiro OkuyamaDavid SelwoodCristina VisintinDavid BakerGareth Pryce
    • A01N37/18
    • C07C235/42A61K31/165C07C69/76C07C69/78C07C233/11C07C233/65C07C233/66C07C233/69C07C235/34C07C235/78C07C235/84C07C237/32C07C237/38C07C237/42C07C255/41C07C255/44
    • The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is OR1 or NR1R2 wherein each of R1 and R2 is independently H, or a hydrocarbyl group; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO2-alkyl, alkenyl, CN, NH2, hydroxy, halo, alkoxy, CF3 and nitro; Y is a polar functional group selected from OH, NO2, CN, COR3, COOR3, NR3R4, CONR3R4, SO3H, SO2—R3, SO2NR3R4 and CF3, where each of R3 and R4 is independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH2)n where n is 0, 1, 2, 3, 4 or 5; with the proviso that: (i) when A is phenyl, n is 0, and Z is OH, X—Y is other than meta-C≡—C—(CH2)2CO2H, meta-C≡—C—(CH2)2OH, meta-C≡C—(CH2)2CO2Me, meta-(CH2)4CO2H, ortho-CH2CO2H, ortho-(CH2)2CO2H and ortho-(CH2)4CO2H; and (ii) when A is phenyl, n is 0, and Z is OMe, X—Y is other than meta-C≡C—(CH2)4OH. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors.
    • 本发明涉及式(I)化合物或其药学上可接受的盐,其中Z为OR 1或NR 1 R 2,其中R 1和R 2各自独立地为H或烃基; X是亚烷基,亚烯基或亚炔基,其各自可以任选地被一个或多个选自烷基,COOH,CO 2 - 烷基,烯基,CN,NH 2,羟基,卤素,烷氧基,CF 3和硝基的取代基取代; Y是选自OH,NO2,CN,COR3,COOR3,NR3R4,CONR3R4,SO3H,SO2-R3,SO2NR3R4和CF3的极性官能团,其中R3和R4各自独立地为H或烃基; A是芳基或杂芳基,其各自可以任选被取代; 和B是(CH 2)n,其中n是0,1,2,3,4或5; 条件是:(i)当A是苯基时,n是0,Z是OH,X-Y不是间位-C≡-C-(CH 2)2 CO 2 H,间-C≡C-(CH 2) (CH 2)2 CO 2 Me,间 - (CH 2)4 CO 2 H,邻-CH 2 CO 2 H,邻 - (CH 2)2 CO 2 H和邻 - (CH 2)4 CO 2 H; 和(ii)当A是苯基时,n是0,Z是OMe,X-Y不是间位-C≡C-(CH 2)4 OH。 本发明的其它方面涉及这样的化合物在制备用于治疗肌肉疾病,胃肠道疾病或用于控制痉挛或震颤的药物中的用途。
    • 8. 发明授权
    • 3-substituted-4-pyrimidone derivatives
    • 3-取代-4-嘧啶酮衍生物
    • US07683069B2
    • 2010-03-23
    • US10538766
    • 2003-12-12
    • Yoshihiro UsuiMasahiro OkuyamaTokushi Hanano
    • Yoshihiro UsuiMasahiro OkuyamaTokushi Hanano
    • C07D401/14A61K31/505
    • C07D401/14C07D409/14C07D413/14
    • A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof useful as a tau protein kinase 1 inhibitor: wherein X represents CH or nitrogen atom; R1 represents a C?1#191-C?12#191 alkyl group which may be substituted; R2 represents a C?1#191-C?8#191 alkyl group which may be substituted, a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom, and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.
    • 用作tau蛋白激酶1抑制剂的由式(I)表示的嘧啶酮衍生物或其盐或其溶剂合物或其水合物:其中X表示CH或氮原子; R1表示可被取代的C 1〜191-C 12〜191烷基; R2表示可被取代的C 1〜191-C 18〜191烷基,可被取代的苯环,可被取代的萘环,可被取代的茚满环,可以被取代的四氢萘环, 或具有1〜4个选自氧原子,硫原子和氮原子的杂原子的任意取代的杂环,并且总共具有5〜10个构成环的原子。
    • 10. 发明授权
    • Active matrix type electroluminescence display device
    • 有源矩阵型电致发光显示装置
    • US07119767B1
    • 2006-10-10
    • US09671843
    • 2000-09-27
    • Naoaki KomiyaMasahiro Okuyama
    • Naoaki KomiyaMasahiro Okuyama
    • G09G3/30
    • G09G3/3266G09G3/3225G09G2300/0842G09G2320/0223
    • An active matrix type electroluminescence display device is provided which comprises a plurality of display pixels GS11, GS12, GS13, arranged in a matrix of rows and columns; gate signal lines GL1, GL2, Gli connected to and shared by a plurality of display pixels arranged in each row; and gate drive circuits for sequentially supplying a select signal SCAN to the gate signal lines GL1, GL2, GL3, Gli. Each display pixel includes an electroluminescence element, a first thin film transistor in which a display signal DATA is applied to the drain and which is switched on and off in response to the select signal SCAN, and a second thin film transistor for driving the EL element based on the display signal DATA. The gate drive circuits are placed so that each of the gate signal lines GL1, GL2, GL3, Gli is driven from both ends.
    • 提供一种有源矩阵型电致发光显示装置,其包括排列成行和列的矩阵的多个显示像素GS 11,GS 12,GS 13; 连接到每行布置的多个显示像素并共享的栅极信号线GL 1,GL 2,Gli; 以及用于将选通信号SCAN顺序提供给栅极信号线GL 1,GL 2,GL 3,Gli的栅极驱动电路。 每个显示像素包括电致发光元件,其中显示信号DATA被施加到漏极并且响应于选择信号SCAN而导通和截止的第一薄膜晶体管和用于驱动EL元件的第二薄膜晶体管 基于显示信号DATA。 栅极驱动电路被放置成使得每个栅极信号线GL1,GL2,GL3,Gli都从两端驱动。