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1. 发明申请

WO2010019097A1 PHARMACEUTICAL PRODUCT COMPRISING A MUSCARINIC RECEPTOR ANTAGONIST AND A SECOND ACTIVE INGREDIENT 审中-公开
标题翻译：药物产品，包括一个muscarinic受体拮抗剂和第二个有效成分
公开(公告)号：WO2010019097A1
公开(公告)日：2010-02-18
申请号：PCT/SE2009/050924
申请日：2009-08-11
申请人： ASTRAZENECA AB , ARGENTA DISCOVERY Ltd. , AVITABILE, Barbara Guiseppina , NADIN, Alan John , RAY, Nicholas Charles
发明人： AVITABILE, Barbara Guiseppina , NADIN, Alan John , RAY, Nicholas Charles
IPC分类号： A61K31/439 , A61P11/06 , A61P11/08 , C07D471/08 , A61K31/438 , A61K31/4468 , C07D261/08 , C07D271/06
CPC分类号： A61K45/06 , A61K31/438 , A61K31/439 , A61K31/4468 , 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：本发明提供了药物产品，药盒或组合物，其包含作为选择的毒蕈碱性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，蛋白酶抑制剂，甾体糖皮质激素受体激动剂，非甾体糖皮质激素受体激动剂和嘌呤受体拮抗剂，用于治疗呼吸疾病如慢性阻塞性肺病和哮喘。

2. 发明申请

WO2010019098A1 PHARMACEUTICAL PRODUCT COMPRISING A MUSCARINIC RECEPTOR ANTAGONIST AND A BETA-2-ADRENOCEPTOR AGONIST 审中-公开
标题翻译：含药物受体拮抗剂和β-2-ADRENOCEPTOR AGONIST的药物产品
公开(公告)号：WO2010019098A1
公开(公告)日：2010-02-18
申请号：PCT/SE2009/050925
申请日：2009-08-11
申请人： ASTRAZENECA AB , ARGENTA DISCOVERY Ltd. , AVITABILE, Barbara Guiseppina , NADIN, Alan John , RAY, Nicholas Charles
发明人： AVITABILE, Barbara Guiseppina , NADIN, Alan John , RAY, Nicholas Charles
IPC分类号： A61K31/439 , A61P11/06 , A61P11/08 , C07D471/08 , C07D261/08 , C07D271/06
CPC分类号： A61K45/06 , A61K31/167 , 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 selected, 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：本发明提供药物产品，试剂盒或组合物，其包含选择的选择的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，其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

WO2010071582A1 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：WO2010071582A1
公开(公告)日：2010-06-24
申请号：PCT/SE2009/051443
申请日：2009-12-17
申请人： ASTRAZENECA AB , ARGENTA DISCOVERY Ltd. , RAY, Nicholas Charles , VAN NEIL, Monique Bodil
发明人： RAY, Nicholas Charles , VAN NEIL, Monique Bodil
IPC分类号： A61K31/381 , A61K31/352 , A61P11/00 , A61K31/4468 , A61K31/4525
CPC分类号： A61K45/06 , A61K31/352 , A61K31/381 , A61K31/4468 , A61K31/4525 , 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。

4. 发明申请

WO2011154678A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2011154678A1
公开(公告)日：2011-12-15
申请号：PCT/GB2010/052111
申请日：2010-12-16
申请人： ASTRAZENECA AB , PULMAGEN THERAPEUTICS (SYNERGY) LIMITED , JENNINGS, Andrew, Stephen, Robert , RAY, Nicholas Charles , ROUSSEL, Fabien , SUTTON, Jonathan, Mark
发明人： JENNINGS, Andrew, Stephen, Robert , RAY, Nicholas Charles , ROUSSEL, Fabien , SUTTON, Jonathan, Mark
IPC分类号： A61P11/08 , A61P29/00 , A61K31/4709 , A61K31/538 , A61K31/454 , C07D265/36 , C07D471/08
CPC分类号： C07D413/14 , A61K31/454 , A61K31/4709 , A61K31/538 , A61K45/06 , C07D211/22 , C07D401/12 , C07D409/14 , C07D413/12 , C07D417/12 , A61K2300/00
摘要： Compounds of formula (I), having activities at muscarinic and β2-receptors (MABAs) for use in therapy.
摘要翻译：式（I）化合物，其在毒蕈碱和β2受体（MABA）中具有用于治疗的活性。

5. 发明申请

WO2008135537A1 TETRAHYDROPYRROLOPYRIMIDINEDIONES AND THEIR USE AS HUMAN NEUTROPHIL ELASTASE INHIBITORS 审中-公开
标题翻译：四氢吡咯并嘧啶及其作为人类中性粒细胞抑制剂的用途
公开(公告)号：WO2008135537A1
公开(公告)日：2008-11-13
申请号：PCT/EP2008/055439
申请日：2008-05-02
申请人： ARGENTA DISCOVERY LIMITED , RAY, Nicholas Charles , FINCH, Harry , EDWARDS, Christine , O'CONNOR, Elizabeth
发明人： RAY, Nicholas Charles , FINCH, Harry , EDWARDS, Christine , O'CONNOR, Elizabeth
IPC分类号： C07D487/04 , A61K31/519 , A61P11/00
CPC分类号： C07D487/04
摘要： Compounds of formula (I) and multimers therof are inhibitors of human neutrophil elastase activity, and of utility in the treatment of, e.g., COPD:(I) wherein A is aryl or heteroaryl; D is oxygen or sulphur; R 1 , R 2 and R 3 are independently each hydrogen, halogen, nitro, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, hydroxy or Cr 1 -C 6 -alkoxy or C 2 -C 6 -alkenyloxy, wherein C 1 -C 6 -alkyl and C 1 -C 6 -alkoxy can be further substituted with one to three identical or different radicals selected from the group consisting of halogen, hydroxy and Cr 1 C 4 -alkoxy; R and R 4 each independently represent a radical of formula -[X] m -[Alk 1 ]p-[Q] n -[Alk 2 ]q-[X 1 ] k -Z wherein k, m, n, p and q are independently 0 or 1; AIk 1 and AIk 2 each independently represent an optionally substituted C 1 -C 6 alkylene, or C 2 -C 6 alkenylene radical which may optionally contain an ether (-O-), thioether (-S-) or amino (-NR A -) link wherein R A is hydrogen or C 1 -C 3 alkyl; Q represents (i) -O-, -S-, -S(O)-, -S(O) 2- , -S + (R A )-, -N(R A )-, -N + (R A )(R B )-, -C(O)-, -C(O)O-, -OC(O)-, -C(=O)NR A -, -NR A C(=O)-, -S(O 2 )NR A -, -NR A S(O 2 )-, -NR A C(=O)NR B -, -NR A C(=NR A )NR B -, -C(=NR D )NR E -, -NR E C(=NR D )-, wherein R A , R B , R D and R E are independently hydrogen, d-C6 alkyl, or C 3 -C 6 cycloalkyl, or R A and R B or R D and R E taken together with the nitrogen to which they are attached form a monocyclic heterocyclic ring of 5 to 7 ring atoms which my contain a further heteroatom selected from N, O and S, or (ii) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 3-6 ring members; X represents -(C=O)-, -S(O 2 )-, -C(O)O-, -(C=O)NR A -, or -S(O2)NR A -, wherein R A is hydrogen, C 1 -C 6 alkyl, or C3-C6 cycloalkyl; X 1 represents -O-, -S-, or -NH; and Z is hydrogen or an optionally substituted mono- or bicyclic carbocyclic or heterocyclic radical having 3-6 ring members.
摘要翻译：式（I）和多聚体的化合物是人嗜中性粒细胞弹性蛋白酶活性的抑制剂，并且在治疗例如COPD中有用：（I）其中A是芳基或杂芳基; D是氧或硫; R 1，R 2和R 3各自独立地为氢，卤素，硝基，氰基，C 1〜 C 6 - 烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 羟基或C 1 -C 6 - 烷氧基或C 2 -C 6 - 烷氧基或C 1 -C 6 - 其中C 1 -C 6 - 烷基和C 1 -C 6 - 烷氧基可被进一步取代具有选自卤素，羟基和C 1 -C 4 - 烷氧基的一至三个相同或不同的基团; R和R 4各自独立地表示下式的基团 - [X] m - [Alk-1] p - [Q] n - 其中k，m，n，p和q，其中k，m，n，独立地为0或1; Alk 1和Alk 2各自独立地表示任选取代的C 1 -C 6亚烷基或C _{和R E独立地是氢，C 1 -C 6烷基或C 3 -C 6环烷基，或者R A' 和它们所连接的氮原子一起形成一个5〜15的单环杂环，其中R 1，R 2，R 2，R 3， 7个环原子，其含有另外的选自N，O和S的杂原子，或（ii）任选取代的具有3-6个环成员的二价单环或双环碳环或杂环基; X表示 - （C = O） - ， - S（O）2 - ， - C（O）O-， - （C = O）NR A - 或-S（O 2）NR A - ，其中R A是氢，C 1 -C 6 - 烷基，或C 3 -C 6环烷基; X 1表示-O - ， - S - 或-NH; Z是氢或任选取代的具有3-6个环成员的单环或双环碳环或杂环基。}

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