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    • 5. 发明申请
      WO2005075469A1 THIAZOLYL-HYDROXAMIC ACIDS AND THIADIAZOLYL-HYDROXAMIC ACIDS, AND USE THEREOF FOR TREATING DISEASES ASSOCIATED WITH HISTONE DEACETYLASE ENZYMATIC ACTIVITY 审中-公开
    • THIAZOLYL-HYDROXAMIC ACIDS AND THIADIAZOLYL-HYDROXAMIC ACIDS, AND USE THEREOF FOR TREATING DISEASES ASSOCIATED WITH HISTONE DEACETYLASE ENZYMATIC ACTIVITY
    • 噻唑 - 羟肟酸和噻二唑 - 羟肟酸，以及其用于治疗与HISTONE脱乙酰酶活性相关的疾病的用途
    • WO2005075469A1
    • 2005-08-18
    • PCT/GB2005/000282
    • 2005-01-27
    • ARGENTA DISCOVERY LIMITED , BORDOGNA, Walter , SUTTON, Jonathan, Mark , HYND, George , DYKE, Hazel, Joan , PRICE, Stephen , HARRIS, Neil, Victor , GILL, Mathew, Iain, Andrew
    • BORDOGNA, Walter , SUTTON, Jonathan, Mark , HYND, George , DYKE, Hazel, Joan , PRICE, Stephen , HARRIS, Neil, Victor , GILL, Mathew, Iain, Andrew
    • C07D417/04
    • C07D417/04 , C07D417/14
    • A compound of formula: (I) in which A represents optionally substituted monocyclic heteroaryl or phenyl; B represents optionally substituted heteroaryl, aryl, aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl, or B represents H when L represents a single bond; L represents a single bond, alkylene, (CH 2 ) n X(CH 2 ) m , (CH2) n X(CH 2 ) p Y(CH 2 ) m ; Q represents N or CR 2 ; T represents N or CR 2 , provided that Q and T do not both represent CR 2 simultaneously; X represents -O-, -NR 3 -, -CO-, -SO 2 -, -NR 3 C0-, -NR 3 SO 2 -, -CONR 3 -, -SO 2 NR 3 -, -NR 1 CONR 1 -; Y represents -NR 3 - or -O-; R l represents H or alkyl; R 2 represents hydrogen, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, CN; R 3 represents H, alkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, cycloalkylalkyl, or alkyl substituted by -OR 4 , -NR 5 R 6 , -NR 6 COR 7 , -NR 6 SO 2 R 7 , -CONR 5 R 6 or -SO 2 NR 5 R 6 ; R 4 represents H, alkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl or cycloalkyl; R 5 represents H or alkyl; R 6 represents H, alkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl or cycloalkyl or NR 5 R 6 represents a cyclic amine; R 7 represents alkyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl or heterocycloalkylalkyl; n represents 0-3; m represents 0-3; p represents 1-3; and corresponding N-oxides, pharmaceutically acceptable salts, solvates and prodrugs thereof; and use to treat a disease in which inhibition of histone deacetylase can prevent, inhibit or ameliorate the pathology and/or symptomatology of the disease.
    • 式（I）的化合物，其中A表示任选取代的单环杂芳基或苯基; B表示任选取代的杂芳基，芳基，芳基稠合 - 杂环烷基，杂芳基 - 稠合环烷基，杂芳基 - 稠合 - 杂环烷基或芳基 - 稠合环烷基，或当L表示单键时，B表示H; L表示单键，亚烷基，（CH 2）n X（CH 2）m，（CH 2）n X（CH 2）p Y（CH 2）m; Q表示N或CR 2; T表示N或CR 2，条件是Q和T不同时同时表示CR 2; X代表-O - ， - NR 3 - ， - CO - ， - SO 2 - ， - NR 3 C 0 - ， - NR 3 SO 2 - ， - CONR 3 - ， - SO 2 NR 3 - ，-NR 1 CONR 1 - ; Y表示-NR 3 - 或-O-; R 1表示H或烷基; R 2表示氢，卤素，烷基，卤代烷基，烷氧基，卤代烷氧基，CN; R 3表示H，烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，环烷基烷基或被-OR 4取代的烷基，-NR 5 R 6，-NR 6 COR 7， 6 SO 2 R 7，-CONR 5 R 6或-SO 2 NR 5 R 6; R 4表示H，烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，环烷基烷基，芳基，杂芳基，杂环烷基或环烷基; R 5表示H或烷基; R 6代表H，烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，环烷基烷基，芳基，杂芳基，杂环烷基或环烷基或NR 5 R 6表示环状胺; R 7表示烷基，芳基，杂芳基，环烷基，杂环烷基，芳烷基，杂芳基烷基，环烷基烷基或杂环烷基烷基; n表示0-3; m表示0-3; p表示1-3; 及其相应的N-氧化物，其药学上可接受的盐，溶剂合物和前药; 并且用于治疗组蛋白脱乙酰酶的抑制可以预防，抑制或改善疾病的病理学和/或症状学的疾病。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 6. 发明申请
      WO2005075466A1 SUBSTITUTED THIENYL-MERCAPTOKETONES, AND USE THEREOF FOR TREATING DISEASES ASSOCIATED WITH HISTONE DEACETYLASE ENZYMATIC ACTIVITY 审中-公开
    • SUBSTITUTED THIENYL-MERCAPTOKETONES, AND USE THEREOF FOR TREATING DISEASES ASSOCIATED WITH HISTONE DEACETYLASE ENZYMATIC ACTIVITY
    • 取代的三烯酰基甜菜碱及其用于治疗与组织脱乙酰酶酶活性相关的疾病
    • WO2005075466A1
    • 2005-08-18
    • PCT/GB2005/000283
    • 2005-01-27
    • ARGENTA DISCOVERY LIMITED , BORDOGNA, Walter , BULL, Richard , SUTTON, Jonathon, Mark , SMITH, Helen, Katherine , DYKE, Hazel, Joan , PRICE, Stephen , HARRIS, Neil, Victor
    • BORDOGNA, Walter , BULL, Richard , SUTTON, Jonathon, Mark , SMITH, Helen, Katherine , DYKE, Hazel, Joan , PRICE, Stephen , HARRIS, Neil, Victor
    • C07D409/04
    • C07D409/04
    • A compound of formula: (I): in which A represents optionally substituted monocyclic heteroaryl or phenyl; B represents optionally substituted heteroaryl, aryl, aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl, or B represents H when L represents a single bond; L represents a single bond, alkylene, (CH 2 ) n X(CH 2 ) m , (CH 2 ) n X(CH 2 ) p Y(CH 2 ) m ; X represents -O-, -NR 3 -, -CO-, -SO 2 -, -NR 3 CO-, -NR 3 SO 2 -, -CONR 3 -, -SO 2 NR 3 -, -NR 5 CONR 5a -; Y represents NR 3 - or -O-; R 1 represents H, COR 8 ; R 2 represents halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, CN; R 3 represents H, alkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, cycloalkylalkyl, or alkyl substituted by -OR 4 , -NR 5 R 6 , -NR 6 COR 7 , -NR 6 SO 2 R 7 , -CONR 5 R 6 or -SO 2 NR 5 R 6 ; R 4 represents H, alkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl or cycloalkyl; R 5 and R 5a represent H or alkyl; R 6 represents H, alkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl or cycloalkyl or NR 5 R 6 represents a cyclic amine; R 7 represents alkyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl or heterocycloalkylalkyl; R 8 represents alkyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl or heterocycloalkylalkyl; n represents 0-3; m represents 0-3; p represents 1-3; and corresponding disulphides, N -oxides, pharmaceutically acceptable salts, solvates and prodrugs thereof; and use to treat a disease in which inhibition of histone deacetylase can prevent, inhibit or ameliorate the pathology and/or symptomatology of the disease.
    • 式（I）的化合物：其中A表示任选取代的单环杂芳基或苯基; B表示任选取代的杂芳基，芳基，芳基稠合 - 杂环烷基，杂芳基 - 稠合环烷基，杂芳基 - 稠合 - 杂环烷基或芳基 - 稠合环烷基，或当L表示单键时，B表示H; L表示单键，亚烷基，（CH 2）n X（CH 2）m，（CH 2）n X（CH 2）p Y（CH 2）m; X表示-O - ， - NR 3 - ， - CO - ， - SO 2 - ， - NR 3 CO - ， - NR 3 SO 2 - ， - CONR 3 - ， - SO 2 NR 3 - ，-NR 5 CONR 5a - ; Y表示NR 3 - 或-O-; R 1表示H，COR 8; R 2表示卤素，烷基，卤代烷基，烷氧基，卤代烷氧基，CN; R 3表示H，烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，环烷基烷基或被-OR 4取代的烷基，-NR 5 R 6，-NR 6 COR 7， 6 SO 2 R 7，-CONR 5 R 6或-SO 2 NR 5 R 6; R 4表示H，烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，环烷基烷基，芳基，杂芳基，杂环烷基或环烷基; R 5和R 5a代表H或烷基; R 6代表H，烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，环烷基烷基，芳基，杂芳基，杂环烷基或环烷基或NR 5 R 6表示环状胺; R 7表示烷基，芳基，杂芳基，环烷基，杂环烷基，芳烷基，杂芳基烷基，环烷基烷基或杂环烷基烷基; R 8表示烷基，芳基，杂芳基，环烷基，杂环烷基，芳基烷基，杂芳基烷基，环烷基烷基或杂环烷基烷基; n表示0-3; m表示0-3; p表示1-3; 和相应的二硫化物，N-氧化物，其药学上可接受的盐，溶剂化物和前药; 并且用于治疗组蛋白脱乙酰酶的抑制可以预防，抑制或改善疾病的病理学和/或症状学的疾病。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 9. 发明申请
      WO1997044337A1 BENZOFURAN CARBOXAMIDES AND THEIR THERAPEUTIC USE 审中-公开
    • BENZOFURAN CARBOXAMIDES AND THEIR THERAPEUTIC USE
    • 苯并呋喃类抗坏血酸及其治疗用途
    • WO1997044337A1
    • 1997-11-27
    • PCT/GB1997001361
    • 1997-05-20
    • CHIROSCIENCE LIMITED , DYKE, Hazel, Joan , LOWE, Christopher , MONTANA, John, Gary , KENDALL, Hannah, Jayne , SABIN, Verity, Jayne
    • CHIROSCIENCE LIMITED
    • C07D307/79
    • C07D405/12 , C07D307/86 , C07D405/14 , C07D417/14
    • A compound of general formula (i) wherein Z is CO or CS; R1 represents alkoxy optionally substituted with one or more halogens, OH or thioalkyl; R2 and R3 are the same or different and are each H, R6, OR10, COR6, C(=NOR6)R6, alkyl-C(=NOR6)R6, alkyl-C(=NOH)R6, C(=NOH)R6, halogen, NR8R9, CF3, CN, CO2H, CO2R10, CONH2, CONHR6 or CON(R6)2; R4 represents H, arylalkyl, heteroarylalkyl, heterocycloalkyl, S(O)mR10 or alkyl optionally substituted with one or more substituents chosen from hydroxy, alkoxy, CO2R7, SO2NR11R12, CONR11R12, CN, carbonyl oxygen, NR8R9, COR10 and S(O)nR10; R5 represents aryl, heteroaryl, heterocyclo, arylalkyl, heteroarylalkyl or heterocycloalkyl; in R4 and/or R5 the aryl/heteroaryl/heterocyclo portion is optionally substituted with one or more substituents alkyl-R13 or R13; R6 represents R10 optionally substituted at any position with R14; R7 represents H, alkyl, arylalkyl, heteroarylalkyl or heterocycloalkyl; R8 represents H, aryl, heteroaryl, heterocyclo, alkyl, cycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkyl, alkylcarbonyl, alkoxycarbonyl, arylsulphonyl, heteroarylsulphonyl, heterocyclosulphonyl, arylcarbonyl, heteroarylcarbonyl, heterocyclocarbonyl or alkylsulphonyl; R10 represents alkyl, cycloalkyl, aryl, heteroaryl, heterocyclo, arylalkyl, heteroarylalkyl or heterocycloalkyl; R9, R11 and R12 are the same or different and are each H or R10; R13 represents alkyl optionally substituted with halogen, alcoxy optionally substituted by halogen, aryl, heteroaryl, heterocyclo, hydroxy, aryloxy, heteroaryloxy, heterocyclooxy, arylalkyloxy, heteroarylalkyloxy, heterocycloalkoxy, CO2R7, CONR11R12, SO2NR11R12, halogen, -CN, -NR8R9, COR10, S(O)nR10 or carbonyl oxygen; R14 represents OH, carbonyl oxygen, OR10, NR8R9, CN, CO2H, CO2R10, CON11R12 or COR10; m is an integer of up to 2; and n represents 0.2, or a pharmaceutically acceptable salt thereof.
    • 通式（ⅰ）的化合物，其中Z为CO或CS; R 1表示任选被一个或多个卤素OH或硫代烷基取代的烷氧基; R2和R3相同或不同，分别为H，R6，OR10，COR6，C（= NOR6）R6，烷基-C（= NOR6）R6，烷基-C（= NOH）R6，C（= NOH）R6 ，卤素，NR8R9，CF3，CN，CO2H，CO2R10，CONH2，CONHR6或CON（R6）2; R4代表H，芳基烷基，杂芳基烷基，杂环烷基，S（O）mR10或任选被一个或多个选自羟基，烷氧基，CO 2 R 7，SO 2 NR 11 R 12，CONR 11 R 12，CN，羰基氧，NR 8 R 9，COR 10和S（O）n R 10 ; R5表示芳基，杂芳基，杂环基，芳基烷基，杂芳基烷基或杂环烷基; 在R 4和/或R 5中，芳基/杂芳基/杂环部分任选被一个或多个取代基烷基-R 13或R 13取代; R 6表示R 10任选在任何位置被R 14取代; R 7表示H，烷基，芳基烷基，杂芳基烷基或杂环烷基; R8代表H，芳基，杂芳基，杂环基，烷基，环烷基，芳基烷基，杂芳基烷基，杂环烷基，烷基羰基，烷氧基羰基，芳基磺酰基，杂芳基磺酰基，杂环磺酰基，芳基羰基，杂芳基羰基，杂环羰基或烷基磺酰基。 R10表示烷基，环烷基，芳基，杂芳基，杂环基，芳基烷基，杂芳基烷基或杂环烷基; R9，R11和R12相同或不同，分别为H或R10; R13表示任选被卤素取代的烷基，任选被卤素，芳基，杂芳基，杂环基，羟基，芳氧基，杂芳氧基，杂环氧基，芳基烷氧基，杂芳烷氧基，杂环烷氧基，CO 2 R 7，CONR 11 R 12，SO 2 NR 11 R 12，卤素，-CN，-NR 8 R 9，COR 10， S（O）nR 10或羰基氧; R14表示OH，羰基氧，OR10，NR8R9，CN，CO2H，CO2R10，CON11R12或COR10; m是最多2的整数; 和n表示0.2，或其药学上可接受的盐。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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