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    • 1. 发明授权
    • 2-amino-3-(alkyl)-pyrimidone derivatives
    • 2-氨基-3-(烷基) - 嘧啶酮衍生物
    • US07378413B2
    • 2008-05-27
    • US11035264
    • 2005-01-13
    • Antonio Almario CarciaRyoichi AndoKeiichi ArimotoFumiaki UeharaAdrien Tak LiAya ShodaJonathan Reid FrostKazutoshi Watanabe
    • Antonio Almario CarciaRyoichi AndoKeiichi ArimotoFumiaki UeharaAdrien Tak LiAya ShodaJonathan Reid FrostKazutoshi Watanabe
    • A61K31/505C07D401/04
    • A61K31/505C07D401/04C07D401/14C07D409/14
    • A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: R1 represents a hydrogen atom or a C1-6 alkyl group which may be substituted by a C6,10 aryl group; R2 represents a C1-10 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C3-6 alkynyl group which may be substituted, a C3-6 cycloalkyl group which may be substituted, or a C6-10 ARYL group which may be substituted; or R1 and R2 form together a C2-6 alkylene group which may be substituted; or R1 and R2 form together a chain of formula —(CH2)2—X—(CH2)2— or —(CH2)2—X—(CH2)3— where X represents a oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted; R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or halogen atom; and R4 represents a C1-10 alkyl group optionally substituted by a hydroxyl group, amino, C1-6 monoalkylamino group, C2-12 dialkylamino group or C6,10 aryl group which may be substituted. And a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β such as Alzheimer's disease.
    • 由式(I)表示的嘧啶酮衍生物或其盐:其中R1表示氢原子或可以被C 6-10取代的C 1-6烷基, / SUB>芳基; R 2表示可以被取代的C 1-10烷基,可以被取代的C 2-6亚烷基,C 3-6亚烷基, 可以被取代的亚炔基,可被取代的C 3-6亚烷基或可以被取代的C 6〜6-亚芳基; 或者R 1和R 2一起形成可以被取代的C 2-6亚烷基; 或者R 1和R 2一起形成式 - (CH 2 CH 2)2 - (CH 2)2 - 或 - (CH 2)2 -X-(CH 2)3 - - 其中X表示 氧原子,硫原子或可被取代的氮原子; R 3表示任选被C 1-4烷基,C 1-4烷氧基或卤素原子取代的2,3或4-吡啶基; 并且R 4表示任选被羟基,氨基,C 1-6 - 单烷基氨基,C 2-12-12任意取代的C 1-10烷基。 >可以被取代的二烷基氨基或C 6,10 芳基。 以及包含所述衍生物或其盐作为活性成分的药物,其用于由GSK3β如阿尔茨海默氏病的异常活性引起的神经变性疾病的预防和/或治疗性治疗。
    • 5. 发明授权
    • Amide derivatives
    • 酰胺衍生物
    • US06444849B1
    • 2002-09-03
    • US09469354
    • 1999-12-22
    • Ryoichi AndoMakoto KawamuraNoriko ChibaKazutoshi Watanabe
    • Ryoichi AndoMakoto KawamuraNoriko ChibaKazutoshi Watanabe
    • C07C23305
    • C07D307/79C07C237/42C07C2601/08C07C2601/14C07D209/18C07D317/60C07D333/60
    • A compound represented by the following general formula (1); wherein X represents R1(R2)(R3)C— where R1 represents a C3-C8 cycloalkyl group, an optionally substituted C6-C14 aryl group, an optionally substituted heterocyclic residue, an optionally substituted C6-C14 aryloxy group, or an optionally substituted C7-C15 arylmethyl group; R2 and R3 independently represent hydrogen atom or a C1-C5 alkyl group, or R2 and R3 may combine to represent a C2-C7 alkylene group; or X represents R7—A— wherein R7 represents (i) a C1-C10 alkyl group which may optionally be substituted with an optionally substituted C6-C14 aryl group, an optionally substituted fluorenyl group or an optionally substituted heterocyclic group, (ii) an optionally substituted C6-C14 aryl group or (iii) an optionally substituted heterocyclic group, and A represents an oxygen atom or —N—R8 where R8 represents hydrogen atom or a C1-C5 alkyl group, Y represents an oxygen atom or a sulfur atom, R4 and R5 independently represent hydrogen atom or a C1-C5 alkyl group; and R6 represents hydrogen atom, a C1-C5 alkyl group which may optionally be substituted with a hydroxyl group, a hydroxyl group or a C1-C5 alkoxy group, provided that the compounds wherein R7 is a benzyl group, A and Y are an oxygen atom, R4 and R5 are hydrogen atom, and R6 is a propyl group are excluded, or a salt thereof, or a solvate thereof or a hydrate thereof.
    • 由以下通式(1)表示的化合物:其中X表示R 1(R 2)(R 3)C-,其中R 1表示C 3 -C 8环烷基,任选取代的C 6 -C 14芳基,任选取代的杂环残基, 任选取代的C 6 -C 14芳氧基,或任选取代的C 7 -C 15芳基甲基; R2和R3独立地表示氢原子或C1-C5烷基,或R2和R3可以组合以表示C2-C7亚烷基; 或X表示R7-A,其中R7表示(i)可任选被任选取代的C 6 -C 14芳基取代的C 1 -C 10烷基,任选取代的芴基或任选取代的杂环基,(ii)任选地 取代的C 6 -C 14芳基或(iii)任选取代的杂环基,A表示氧原子或-N-R 8,其中R 8表示氢原子或C 1 -C 5烷基,Y表示氧原子或硫原子, R4和R5独立地表示氢原子或C1-C5烷基; 并且R 6表示氢原子,可任选被羟基,羟基或C 1 -C 5烷氧基取代的C 1 -C 5烷基,条件是其中R 7为苄基,A和Y为氧的化合物为氧 原子,R 4和R 5为氢原子,并且R 6为丙基,或其盐,或其溶剂合物或其水合物。
    • 6. 发明授权
    • Electrostatic damage protection device with protection transistor
    • 具有保护晶体管的静电损伤保护装置
    • US07274071B2
    • 2007-09-25
    • US10979804
    • 2004-11-03
    • Ryoichi AndoAkira UemotoToshio Kakiuchi
    • Ryoichi AndoAkira UemotoToshio Kakiuchi
    • H01L23/62
    • H01L27/0266
    • This invention provides an electrostatic damage protection device which can protects a device to be protected enough from an electrostatic damage and prevents damages of protection transistors themselves. A N-channel type first MOS transistor and a N-channel type second MOS transistor serving as protection transistors are connected in series between an output terminal and a ground potential. On the other hand, a P-channel type third MOS transistor and a P-channel type fourth MOS transistor serving as protection transistors are connected in series between a high power supply potential and the output terminal. These first, second, third, and fourth MOS transistors are formed of low withstand voltage MOS transistors.
    • 本发明提供了一种静电损伤保护装置,其能够保护装置受到足够的保护以免受到静电损坏,并且防止保护晶体管本身的损坏。 用作保护晶体管的N沟道型第一MOS晶体管和N沟道型第二MOS晶体管串联连接在输出端和地电位之间。 另一方面,用作保护晶体管的P沟道型第三MOS晶体管和P沟道型第四MOS晶体管串联连接在高电源电位和输出端之间。 这些第一,第二,第三和第四MOS晶体管由低耐压MOS晶体管形成。