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1. 发明申请

WO2009139708A1 PHARMACEUTICAL PRODUCT COMPRISING A MUSCARINIC RECEPTOR ANTAGONIST AND A β2-ADRENOCEPTOR AGONIST 审中-公开
标题翻译：包含MUSCARINIC受体拮抗剂和Aβ2-肾上腺素激动剂的药物产品
公开(公告)号：WO2009139708A1
公开(公告)日：2009-11-19
申请号：PCT/SE2009/050525
申请日：2009-05-12
申请人： ASTRAZENECA AB , ARGENTA DISCOVERY Ltd. , BULL, Richard , FORD, Rhonan , MATHER, Andrew , METE, Antonio , WILEY, Katherine
发明人： BULL, Richard , FORD, Rhonan , MATHER, Andrew , METE, Antonio , WILEY, Katherine
IPC分类号： A61K31/439 , A61P11/06 , A61P11/08 , A61K31/428
CPC分类号： A61K45/06 , A61K31/428 , A61K31/439 , A61K2300/00
摘要： The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is a selected muscarinic receptor antagonist, and a second active ingredient which is a β 2 -adrenoceptor agonist, of use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma.
摘要翻译：本发明提供了包含选自毒蕈碱受体拮抗剂的第一活性成分和作为β2肾上腺素受体激动剂的第二活性成分的药物产品，试剂盒或组合物，其用于治疗呼吸系统疾病如慢性阻塞性肺疾病和哮喘。

2. 发明申请

WO2009139707A1 PHARMACEUTICAL PRODUCT COMPRISING A MUSCARINIC RECEPTOR ANTAGONIST AND A SECOND ACTIVE INGREDIENT 审中-公开
标题翻译：含有药物受体拮抗剂和第二活性成分的药物产品
公开(公告)号：WO2009139707A1
公开(公告)日：2009-11-19
申请号：PCT/SE2009/050524
申请日：2009-05-12
申请人： ASTRAZENECA AB , ARGENTA DISCOVERY Ltd. , BULL, Richard , FORD, Rhonan , MATHER, Andrew , METE, Antonio
发明人： BULL, Richard , FORD, Rhonan , MATHER, Andrew , METE, Antonio
IPC分类号： A61K31/439 , A61P11/00
CPC分类号： A61K45/06 , A61K31/439 , A61K2300/00
摘要： The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is a selected muscarinic receptor antagonist, and a second active ingredient which is selected from a phosphodiesterase inhibitor, a modulator of chemokine receptor function, an inhibitor of kinase function, a protease inhibitor, a steroidal glucocorticoid receptor agonist, a non-steroidal glucocorticoid receptor agonist and a purinoceptor antagonist, of use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma.
摘要翻译：本发明提供了包含选自毒蕈碱受体拮抗剂的第一活性成分和选自磷酸二酯酶抑制剂，趋化因子受体功能调节剂，激酶功能抑制剂，第二活性成分蛋白酶抑制剂，类固醇糖皮质激素受体激动剂，非类固醇糖皮质激素受体激动剂和嘌呤受体拮抗剂，用于治疗呼吸系统疾病如慢性阻塞性肺疾病和哮喘。

3. 发明申请

WO2005075466A1 SUBSTITUTED THIENYL-MERCAPTOKETONES, AND USE THEREOF FOR TREATING DISEASES ASSOCIATED WITH HISTONE DEACETYLASE ENZYMATIC ACTIVITY 审中-公开
标题翻译：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
公开(公告)号：WO2005075466A1
公开(公告)日：2005-08-18
申请号：PCT/GB2005/000283
申请日：2005-01-27
申请人： ARGENTA DISCOVERY LIMITED , BORDOGNA, Walter , BULL, Richard , SUTTON, Jonathon, Mark , SMITH, Helen, Katherine , DYKE, Hazel, Joan , PRICE, Stephen , HARRIS, Neil, Victor
发明人： BORDOGNA, Walter , BULL, Richard , SUTTON, Jonathon, Mark , SMITH, Helen, Katherine , DYKE, Hazel, Joan , PRICE, Stephen , HARRIS, Neil, Victor
IPC分类号： C07D409/04
CPC分类号： C07D409/04
摘要： 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.
摘要翻译：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。

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