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    • 3. 发明申请
    • MEDICAL USE OF CYCLIN DEPENDENT KINASES INHIBITORS
    • 环孢霉素依赖性激酶抑制剂的医学应用
    • WO2008009954A1
    • 2008-01-24
    • PCT/GB2007/002753
    • 2007-07-20
    • ASTEX THERAPEUTICS LIMITEDPIKE, AndrewLYONS, John, Francis
    • PIKE, AndrewLYONS, John, Francis
    • A61K31/415A61K31/44A61P13/12A61P29/00A61P25/00A61P9/10A61P9/12A61P3/10
    • A61K31/415A61K31/44
    • The invention provides the use of a compound for the manufacture of a medicament for the treatment of pain, wherein the compound is a compound of the formula (0) : or a salt or tautomers or N-oxides or solvate thereof; wherein X is a group R 1 -A-NR 4 - or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO 2 , C=O, NR 9 (C=O) or O(C=O) wherein R 9 is hydrogen or C 1-4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R 1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C 1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen, hydroxy, C 1-4 hydrocarbyloxy, amino, mono- or di-C 1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO 2 ; R 2 is hydrogen; halogen; C 1-4 alkoxy; or a C 1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or C 1-4 alkoxy (e.g. methoxy); R 3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R 4 is hydrogen or a C 1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C 1-4 alkoxy. The invention also provides the use of the compounds of the formula (0) for the treatment of stroke and for the treatment of polycystic kidney disease.
    • 本发明提供化合物在制备用于治疗疼痛的药物中的用途,其中所述化合物是式(O)的化合物:或其盐或互变异构体或N-氧化物或其溶剂化物; 其中X是基团R 1 -A-NR 4 - 或5或6元碳环或杂环; A是一个键,SO 2,C = O,NR 9(C = O)或O(C = O),其中R 9, 是任选被羟基或C 1-4烷氧基取代的氢或C 1-4烃基; Y是长度为1,2或3个碳原子的键或亚烷基链; R 1是氢; 具有3至12个环成员的碳环或杂环基; 或任选被一个或多个选自卤素,羟基,C 1-4烷氧基,氨基,一或二-C 1的取代基取代的C 1-8烃基, 具有3至12个环成员的碳环或杂环基团,并且其中烃基的1或2个碳原子可以任选地被选自下列的原子或基团取代:O, S,NH,SO,SO 2; R 2是氢; 卤素; C 1-4烷氧基; 或任选被卤素,羟基或C 1-4烷氧基(例如甲氧基)取代的C 1-4烷基; R 3选自具有3至12个环成员的氢和碳环和杂环基; 和R 4是氢或任选被卤素(例如氟),羟基或C 1-4烷氧基取代的C 1-4烷基 。 本发明还提供式(O)化合物用于治疗中风和治疗多囊肾病的用途。
    • 5. 发明公开
    • MEDICAL USE OF CYCLIN DEPENDENT KINASES INHIBITORS
    • 激酶抑制剂细胞周期蛋白的医疗用途
    • EP2046327A1
    • 2009-04-15
    • EP07766316.9
    • 2007-07-20
    • Astex Therapeutics Limited
    • PIKE, AndrewLYONS, John Francis
    • A61K31/415A61K31/44A61P13/12A61P29/00A61P25/00A61P9/10A61P9/12A61P3/10
    • A61K31/415A61K31/44
    • The invention provides the use of a compound for the manufacture of a medicament for the treatment of pain, wherein the compound is a compound of the formula (0) : or a salt or tautomers or N-oxides or solvate thereof; wherein X is a group R1-A-NR4- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C=O, NR9(C=O) or O(C=O) wherein R9 is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen, hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy; or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy. The invention also provides the use of the compounds of the formula (0) for the treatment of stroke and for the treatment of polycystic kidney disease.