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1. 发明申请

WO2009037503A2 NEW COMBINATION - 012 审中-公开
标题翻译：新组合 - 012
公开(公告)号：WO2009037503A2
公开(公告)日：2009-03-26
申请号：PCT/GB2008/050831
申请日：2008-09-17
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , ALCARAZ, Lilian , CADOGAN, Elaine, Bridget , CONNOLLY, Stephen , NICHOLLS, David, John , YOUNG, Alan
发明人： ALCARAZ, Lilian , CADOGAN, Elaine, Bridget , CONNOLLY, Stephen , NICHOLLS, David, John , YOUNG, Alan
IPC分类号： A61K45/06 , A61P31/06
CPC分类号： A61K45/06 , A61K31/428 , A61K2300/00
摘要： The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is 4-hydroxy-7-[1 R -hydroxy-2-(2-{3-[(2-methoxy-benzylamino)- methyl]-phenyl}-ethylamino)-ethyl]-3H-benzothiazol-2-one or a salt thereof, and a second active ingredient selected from: a non-steroidal Glucocorticoid Receptor (GR Receptor) Agonist; an antioxidant; a CCRl antagonist; a chemokine antagonist (not CCRl); a corticosteroid; a CRTh2 antagonist; a DPI antagonist; an Histone Deacetylase Inducer; an IKK2 inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; a MABA,; an MPO inhibitor; a muscarinic antagonist; a p38 inhibitor; a PDE inhibitor; a PPARγ agonist; a protease inhibitor; a Statin; a thromboxane antagonist; a vasodilator; or, an ENAC blocker (Epithelial Sodium-channel blocker); and its use in the treatment of respiratory disease.
摘要翻译：本发明提供包含4-羟基-7- [1R-羟基-2-（2- {3 - [（2-甲氧基 - 苄基氨基） - 甲基] - 苯基} - 苯甲酸的第一活性成分的药物产品，试剂盒或组合物，乙基氨基） - 乙基] -3H-苯并噻唑-2-酮或其盐，和第二活性成分，选自：非甾体糖皮质激素受体（GR Receptor）激动剂; 抗氧化剂 CCR1拮抗剂; 趋化因子拮抗剂（不是CCR1）; 皮质类固醇 CRTh2拮抗剂; DPI拮抗剂; 组蛋白脱乙酰酶诱导剂; IKK2抑制剂; COX抑制剂; 脂氧合酶抑制剂; 白细胞三烯受体拮抗剂; 一个MABA MPO抑制剂; 毒蕈碱拮抗剂一种p38抑制剂; PDE抑制剂; 一个PPAR？激动剂; 蛋白酶抑制剂; 他汀类血栓素拮抗剂; 血管扩张剂或ENAC阻断剂（上皮钠通道阻断剂）; 并用于治疗呼吸系统疾病。

2. 发明申请

WO2008075025A1 AMINE DERIVATIVES AND THEIR USE IN BETA-2-ADRENORECEPTOR MEDIATED DISEASES 审中-公开
标题翻译：胺衍生物及其在β-2受体介导的疾病中的应用
公开(公告)号：WO2008075025A1
公开(公告)日：2008-06-26
申请号：PCT/GB2007/004859
申请日：2007-12-19
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , ALCARAZ, Lilian , BONNERT, Roger, Victor , CONNOLLY, Stephen , COOK, Anthony, Ronald , FISHER, Adrian , HUMPHRIES, Alexander , RAUBO, Piotr
发明人： ALCARAZ, Lilian , BONNERT, Roger, Victor , CONNOLLY, Stephen , COOK, Anthony, Ronald , FISHER, Adrian , HUMPHRIES, Alexander , RAUBO, Piotr
IPC分类号： C07C237/08 , C07C237/10 , C07D209/34 , C07D265/36 , C07D215/227 , A61K31/4704 , A61K31/536 , A61P11/00 , A61P29/00 , C07C233/01
CPC分类号： C07D265/36 , C07C233/43 , C07C2601/14 , C07D209/34 , C07D215/26 , C07D409/12 , C07D413/12
摘要： The present invention provides compounds of formula (I), wherein k, Ar, R 2 , R 3 , R 4 , R 5 , R 4' , R 5' , R 6 , R 7 , A, D, m and E are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译：本发明提供式（I）化合物，其中k，Ar，R 2，R 3，R 4，R 4， 5，R 4'，R 5'，R 6，R 7，A， D，m和E如说明书中所定义，其制备方法，含有它们的药物组合物及其在治疗中的用途。

3. 发明申请

WO2006056752A1 PHENOXYACETIC ACID DERIVATIVES USEFUL FOR TREATING RESPIRATORY DISEASES 审中-公开
标题翻译：用于治疗呼吸道疾病的苯氧基酸衍生物
公开(公告)号：WO2006056752A1
公开(公告)日：2006-06-01
申请号：PCT/GB2005/004464
申请日：2005-11-22
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BONNERT, Roger, Victor , ALCARAZ, Lilian , MOHAMMED, Rukhsana, Tasneem , COOK, Anthony, Ronald , THOM, Stephen , LUKER, Timothy, Jon
发明人： BONNERT, Roger, Victor , ALCARAZ, Lilian , MOHAMMED, Rukhsana, Tasneem , COOK, Anthony, Ronald , THOM, Stephen , LUKER, Timothy, Jon
IPC分类号： C07D207/48 , C07C59/72 , C07D333/24 , C07D213/34 , C07D213/56 , C07D241/08 , A61K31/495 , A61P11/00
CPC分类号： C07D333/24 , C07D207/48 , C07D213/34 , C07D213/56 , C07D241/08
摘要： The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Formula (I)
摘要翻译：本发明涉及取代的苯氧基乙酸作为治疗呼吸系统疾病的有用药物化合物，含有它们的药物组合物及其制备方法。（I）

4. 发明申请

WO2008041914A1 5-(2-AMINO-L-HYDROXYETHYL)-8-HYDROXY-2-OXOQUINOLINE DERIVATIVES AND OTHER COMPOUNDS AS β2 -ADRENERGIC AGONISTS 审中-公开
标题翻译： 5-（2-氨基-L-羟基乙基）-8-羟基-2-氧杂环丁烷衍生物和其它化合物作为β2-ADRENERGIC AGONISTS
公开(公告)号：WO2008041914A1
公开(公告)日：2008-04-10
申请号：PCT/SE2007/000885
申请日：2007-10-05
申请人： ASTRAZENECA AB , ALCARAZ, Lilian , CONNOLLY, Stephen
发明人： ALCARAZ, Lilian , CONNOLLY, Stephen
IPC分类号： C07D215/14 , A61K31/4704 , A61P11/00
CPC分类号： C07D215/26
摘要： The present invention provides 5-(2-amino-l-hydroxyethyl)-8-hydroxy-2-oxoquinoline derivatives and other compounds of formula (I) wherein R 1 is formula (A) wherein R 4 , R 5 and M 1 are as defined in the specification, or R 1 is as defined in the specification, and wherein R 2 , R 3 , W, A, X and Y are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or conditions in which modulation of β 2 adrenoreceptor activity is beneficial, e.g. adult respiratory distress syndrome (ARDS), pulmonary emphysema, bronchitis, bronchiectasis, chronic obstructive pulmonary disease (COPD), asthma or rhinitis. The compounds are β 2 -adrenergic agonists.
摘要翻译：本发明提供5-（2-氨基-1-羟基乙基）-8-羟基-2-氧代喹啉衍生物和式（I）的其它化合物，其中R 1为式（A） SUP> 4，R 5和M 1如说明书中所定义，或R 1如本说明书中所定义，其中R 2，R 3，W，A，X和Y如说明书中所定义，其制备方法，含有它们的药物组合物及其在治疗β2/2肾上腺素受体活性调节的疾病或病症是有益的，例如，成人呼吸窘迫综合征（ARDS），肺气肿，支气管炎，支气管扩张，慢性阻塞性肺疾病（COPD），哮喘或鼻炎。化合物是β2 - 肾上腺素能激动剂。

5. 发明申请

WO2010067102A1 DIAZASPIRO [5.5] UNDECANE DERIVATIVES AND RELATED COMPOUNDS AS MUSCARINIC-RECEPTOR ANTAGONISTS AND BETA-ADRENORECEPTOR AGONISTS FOR THE TREATMENT OF PULMONARY DISORDERS 审中-公开
标题翻译： DIAZASPIRO [5.5]作为治疗肺动脉疾病的药物 - 受体拮抗剂和β-受体激动剂的非依赖衍生物和相关化合物
公开(公告)号：WO2010067102A1
公开(公告)日：2010-06-17
申请号：PCT/GB2009/051657
申请日：2009-12-07
申请人： ASTRAZENECA AB , ARGENTA DISCOVERY LIMITED , ALCARAZ, Lilian , KINDON, Nicholas , STOCKS, Michael, John
发明人： ALCARAZ, Lilian , KINDON, Nicholas , STOCKS, Michael, John
IPC分类号： C07D498/10 , A61K31/537 , A61P11/06 , A61P11/08
CPC分类号： C07D498/10
摘要： Spirocyclicmorpholine-substituted amides of formula (I): processes for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions, their use in therapy and intermediates of use in their preparation.
摘要翻译：式（I）的螺环基吗啉取代的酰胺：其制备方法，含有它们的药物组合物，制备药物组合物的方法，它们在治疗中的用途及其制备中使用的中间体。

6. 发明申请

WO2010015792A1 NITROGEN CONTAINING HETEROCYCLIC COMPOUNDS USEFUL AS BIFUNCTIONAL MODULATORS OF M3 RECEPTORS AND BETA-2 RECEPTORS 审中-公开
标题翻译：含有作为M3受体和β2受体的双功能调节剂的含氮杂环化合物
公开(公告)号：WO2010015792A1
公开(公告)日：2010-02-11
申请号：PCT/GB2008/002692
申请日：2008-08-06
申请人： ARGENTA DISCOVERY LIMITED , ASTRAZENECA AB , SUTTON, Jonathan, Mark , ROUSSEL, Fabien , VAN DEN HEUVEL, Marco , RAY, Nicholas, Charles , ALCARAZ, Lilian
发明人： SUTTON, Jonathan, Mark , ROUSSEL, Fabien , VAN DEN HEUVEL, Marco , RAY, Nicholas, Charles , ALCARAZ, Lilian
IPC分类号： C07D413/12 , C07D417/12 , C07D413/14 , A61K31/41 , A61P1/00 , A61P9/00 , A61P11/00 , A61P13/00 , A61P15/00 , A61P17/00 , A61P19/00 , A61P25/00 , A61P27/02 , A61P29/00 , A61P35/00
CPC分类号： C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention relates to named compounds of the formula (I) having both M3 receptor antagonist and β2 agonist activity; compositions comprising such compounds; the use of such compounds in therapy (such as respiratory tract disorders); and a method of treating a patient with such compounds.
摘要翻译：本发明涉及具有M3受体拮抗剂和β2激动剂活性的具有式（I）的命名化合物; 包含这些化合物的组合物; 这些化合物在治疗中的应用（如呼吸道疾病）; 以及用这些化合物治疗患者的方法。

7. 发明申请

WO2008149110A1 BICYCLOR [2.2.1] HEPT-7-YLAMINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASES AND CONDITIONS IN WHICH M3 MUSCARINIC RECEPTOR ACTIVITY AND BETA-ADRENERGIC ACTIVITY ARE IMPLICATED 审中-公开
标题翻译： BICYCLOR [2.2.1] HEPT-7-氯胺衍生物及其在治疗M3受体活性和β受体活性的疾病和病症中的用途是隐含的
公开(公告)号：WO2008149110A1
公开(公告)日：2008-12-11
申请号：PCT/GB2008/001955
申请日：2008-06-06
申请人： ARGENTA DISCOVERY LIMITED , ASTRAZENECA AB , ALCARAZ, Lilian , KINDON, Nicholas , SUTTON, Jonathan, Mark
发明人： ALCARAZ, Lilian , KINDON, Nicholas , SUTTON, Jonathan, Mark
IPC分类号： C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , A61K31/428 , A61K31/4704 , A61K31/536 , A61P11/00 , A61P1/04 , A61P29/00
CPC分类号： C07D417/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/14
摘要： The present invention relates to compounds of formula (I) having muscarinic M3 receptor and β-adrenergic receptor modulating activity; wherein R 1 , R 2 , R 3 and X are as defined herein.
摘要翻译：本发明涉及具有毒蕈碱M3受体和β-肾上腺素能受体调节活性的式（I）化合物; 其中R1，R2，R3和X如本文所定义。

8. 发明申请

WO2012085582A1 COMPOUND 审中-公开
标题翻译：复合
公开(公告)号：WO2012085582A1
公开(公告)日：2012-06-28
申请号：PCT/GB2011/052559
申请日：2011-12-22
申请人： ASTRAZENECA AB , PULMAGEN THERAPEUTICS (SYNERGY) LIMITED , ALCARAZ, Lilian , BAILEY, Andrew , KINDON, Nicholas
发明人： ALCARAZ, Lilian , BAILEY, Andrew , KINDON, Nicholas
IPC分类号： A61K31/535 , A61K31/425
CPC分类号： A61K31/425 , A61K31/535 , A61K45/06 , A61K2300/00
摘要： The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is 3-(2-Chloro-3-((4-(2-ethylthiazole-4-carbonyl)-1-oxa-4,9-diazaspiro[5.5]undecan-9-yl)methyl)phenethoxy)-N-cyclopentyl-N-(2-(2-(5-hydroxy-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-8-yl(ethylamino)ethyl)propanamide or a salt thereof, and a second active ingredient selected from: a non-steroidal Glucocorticoid Receptor (GR Receptor) Agonist; an antioxidant; a CCR1 antagonist; a chemokine antagonist (not CCR1); a corticosteroid; a CRTh2 antagonist; a DP1 antagonist; an Histone Deacetylase activator; an IKK2 kinase inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; an MPO inhibitor; a PDE4 inhibitor; a PPARϒ agonist; a protease inhibitor; a p38 inhibitor, a selective glucocorticoid receptor agonist (SEGRA), a Statin; a thromboxane antagonist; a vasodilator; or, an ENAC blocker (Epithelial Sodium-channel blocker); and its use in the treatment of respiratory disease.
摘要翻译：本发明提供包含第一活性成分的药物产品，试剂盒或组合物，其为3-（2-氯-3 - （（4-（2-乙基噻唑-4-羰基）-1-氧杂-4,9-二氮杂螺[ 5.5]十一碳-9-基）甲基）苯乙氧基）-N-环戊基-N-（2-（2-（5-羟基-3-氧代-3,4-二氢-2H-苯并[b] [1,4 （乙基氨基）乙基）丙酰胺或其盐和选自以下的第二活性成分：非甾体糖皮质激素受体（GR受体）激动剂;抗氧化剂; CCR1拮抗剂;趋化因子拮抗剂（不是CCR1 ）;皮质类固醇; CRTh2拮抗剂; DP1拮抗剂;组蛋白脱乙酰酶激活剂; IKK2激酶抑制剂; COX抑制剂;脂氧合酶抑制剂;白三烯受体拮抗剂; MPO抑制剂; PDE4抑制剂;PPARα激动剂; 蛋白酶抑制剂; p38抑制剂，选择性糖皮质激素受体激动剂（SEGRA），他汀类药物;血栓烷拮抗剂;血管扩张剂;或ENAC阻滞剂（上皮钠通道阻滞剂）;及其在治疗中的用途的呼吸系统疾病。

9. 发明申请

WO2011012896A2 COMPOUNDS - 801 审中-公开
标题翻译：化合物 - 801
公开(公告)号：WO2011012896A2
公开(公告)日：2011-02-03
申请号：PCT/GB2010/051242
申请日：2010-07-29
申请人： ASTRAZENECA AB , PULMAGEN THERAPEUTICS (SYNGERY) LIMITED , ALCARAZ, Lilian , BAILEY, Andrew , KINDON, Nicholas
发明人： ALCARAZ, Lilian , BAILEY, Andrew , KINDON, Nicholas
CPC分类号： C07D498/10 , C07D519/00
摘要： Spirocyclic amide derivatives of formula (I) wherein ArCH 2 CH 2 NH- represents a β-adrenoceptor binding group, processes for their preparation, pharmaceutical compositions containing them, a process for preparing such pharmaceutical compositions, their use in therapy, and intermediates for use in their preparation.
摘要翻译：其中ArCH2CH2NH-表示β-肾上腺素能受体结合基团的式（I）的螺环酰胺衍生物，其制备方法，含有它们的药物组合物，制备该药物组合物的方法，其在治疗中的用途以及用于其制备的中间体。

10. 发明申请

WO2007106016A1 BEZOTHIAZOL DERIVATIVES AS BETA2 ADRENORECEPTOR AGONISTS 审中-公开
标题翻译： BEZOTHIAZOL衍生物作为BETA2 ADRENORECEPTOR AGONISTS
公开(公告)号：WO2007106016A1
公开(公告)日：2007-09-20
申请号：PCT/SE2007/000233
申请日：2007-03-12
申请人： ASTRAZENECA AB , ALCARAZ, Lilian , LISTER, Andrew , PAIRAUDEAU, Garry
发明人： ALCARAZ, Lilian , LISTER, Andrew , PAIRAUDEAU, Garry
IPC分类号： C07D277/68 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/55 , A61P11/00 , A61P11/06 , A61P11/08 , C07D417/12
CPC分类号： C07D277/68 , C07D417/12
摘要： The present invention relates to compounds according to formula (I) , a process for preparing them, the intermediate compounds of the process and the use of the compounds in the manufacture of a medicament for use in treating diseases such as ARDS, pulmonary emphysema, bronchitis, bronchiectasis, COPD, asthma and rhinitis. The compounds are beta2 adrenoreceptor agonists.
摘要翻译：本发明涉及式（I）化合物，其制备方法，该方法的中间体化合物和该化合物在制备用于治疗疾病如ARDS，肺气肿，支气管炎的药物中的用途，支气管扩张，COPD，哮喘和鼻炎。这些化合物是β2肾上腺素受体激动剂。

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