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1. 发明申请

WO2015140527A1 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2015140527A1
公开(公告)日：2015-09-24
申请号：PCT/GB2015/050765
申请日：2015-03-17
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED
发明人： BERGLUND, Susanne, Elisabeth , CONNOLLY, Stephen , HEMMERLING, Martin , HOSSAIN, Nafizal , KRISTOFFERSSON, Anna , LUNDKVIST, Johan, Rune, Michael , NIKITIDIS, Grigorios , RIPA, Lena, Elisabeth , SHAMOVSKY, Igor
IPC分类号： C07D401/06 , C07D241/28 , A61K31/497 , A61P11/00
CPC分类号： C07D401/12 , A61K31/4965 , A61K31/497 , A61K45/06 , C07D241/26 , C07D241/28 , C07D401/06
摘要： The present invention provides a compound of a formula (I): or a pharmaceutically acceptable salt thereof; a process for preparing such a compound; and to the use of such a compound in the treatment of an ENaC mediated disease state (such as asthma, CF or COPD).
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐; 制备这种化合物的方法; 以及在治疗ENaC介导的疾病状态（例如哮喘，CF或COPD）中使用这种化合物。

2. 发明申请

WO2013008002A1 N- (6- ( (2R,3S) -3,4-DIHYDROXYBUTAN-2-YLOXY) -2- (4 - FLUOROBENZYLTHIO) PYRIMIDIN- 4 - YL) -3- METHYLAZETIDINE- 1 - SULFONAMIDE AS CHEMOKINE RECEPTOR MODULATOR 审中-公开
标题翻译： N-（6 - （（2R，3S）-3,4-二羟基丁-2-炔基）-2-（4-氟代苄基）吡咯烷-4-基）-3-甲基噻嗪-1-磺酰胺作为化合物受体调节剂
公开(公告)号：WO2013008002A1
公开(公告)日：2013-01-17
申请号：PCT/GB2012/051620
申请日：2012-07-10
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , CONNOLLY, Stephen , EBDEN, Mark, Richard , LANGER, Thomas , STEVEN, Alan, Robert , STEWART, Craig, Robert , TOMLIN, Paula, Margaret , WALTERS, Iain, Alastair, Stewart , WILLIAMS, Andrew, John
发明人： CONNOLLY, Stephen , EBDEN, Mark, Richard , LANGER, Thomas , STEVEN, Alan, Robert , STEWART, Craig, Robert , TOMLIN, Paula, Margaret , WALTERS, Iain, Alastair, Stewart , WILLIAMS, Andrew, John
IPC分类号： C07D403/12 , C07D205/04 , A61K31/506 , C07D317/20 , C07D317/24 , C07C69/92
CPC分类号： C07D403/12 , A61K31/506 , C07C65/21 , C07C69/78 , C07C69/92 , C07D205/04 , C07D239/56 , C07D307/12 , C07D317/18 , C07D317/20 , C07D317/24 , C07D317/26
摘要： There is provided a compound which is (a) a pyrimidine sulfonamide of formula (I) or (b) a pharmaceutically acceptable salt thereof, crystalline forms of the compound, processes for obtaining the compound, pharmaceutical intermediates used in the manufacture of the compound, and pharmaceutical compositions containing the compound. The compound is useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.
摘要翻译：提供了化合物，其为（a）式（I）或（b）的嘧啶磺酰胺或其药学上可接受的盐，化合物的结晶形式，获得化合物的方法，用于制备化合物的药物中间体，和含有该化合物的药物组合物。该化合物可用于治疗调节趋化因子受体活性有益的疾病/病症。

3. 发明申请

WO2008096119A1 SALTS 669 审中-公开
公开(公告)号：WO2008096119A1
公开(公告)日：2008-08-14
申请号：PCT/GB2008/000394
申请日：2008-02-06
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , CONNOLLY, Stephen
发明人： CONNOLLY, Stephen
IPC分类号： C07D277/68 , A61K31/428 , A61P11/00
CPC分类号： C07D277/68
摘要： A pharmaceutically acceptable salt of N-[2-(Diethylamino)ethyl]-N-(2-{[2-(4-hydroxy-2-oxo-2,3-dihydro-1,3-benzothiazol-7-yl)ethyl]amino}ethyl)-3-[2-(3-chlorophenyl)ethoxy]pro panamide provided it is not the ditrifluoroacetate salt; and the use of such a compound as a medicament (for example in the treatment of respiratory diseases (such as asthma or COPD).
摘要翻译： N- [2-（二乙基氨基）乙基] -N-（2 - {[2-（4-羟基-2-氧代-2,3-二氢-1,3-苯并噻唑-7-基）乙基]氨基}乙基）-3- [2-（3-氯苯基）乙氧基]丙酰胺，只要它不是二（三氟乙酸盐）盐; 以及使用这种化合物作为药物（例如用于治疗呼吸系统疾病（如哮喘或COPD））。

4. 发明申请

WO2011073662A1 COMBINATION OF A BENZOXAZINONE AND A FURTHER AGENT FOR TREATING RESPIRATORY DISEASES 审中-公开
标题翻译：苯并噻嗪酮与治疗呼吸道疾病的进一步药物的联合
公开(公告)号：WO2011073662A1
公开(公告)日：2011-06-23
申请号：PCT/GB2010/052103
申请日：2010-12-16
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BONNERT, Roger, Victor , CONNOLLY, Stephen
发明人： BONNERT, Roger, Victor , CONNOLLY, Stephen
IPC分类号： A61K31/40 , A61K31/439 , A61K31/46 , A61K31/538 , A61P11/00
CPC分类号： A61K31/46 , A61K31/40 , A61K31/439 , A61K31/538 , A61K45/06 , A61K2300/00
摘要： The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is N-Cyclohexyl-N-(2-(2-(5-hydroxy-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-8-yl)ethylamino)ethyl)-3-(3-(1-methyl-1H-pyrazol-4- yl)phenethoxy)propanamide or a pharmaceutically acceptable 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 Inducer; an IKK2 inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; 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 (for example chronic obstructive pulmonary disease (COPD) or asthma).
摘要翻译：本发明提供包含N-环己基-N-（2-（2-（5-羟基-3-氧代-3,4-二氢-2H-苯并[b] 乙基氨基）乙基）-3-（3-（1-甲基-1H-吡唑-4-基）苯乙氧基）丙酰胺或其药学上可接受的盐，选择第二活性成分来自：非类固醇糖皮质激素受体（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; 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）; 及其在治疗呼吸系统疾病（例如慢性阻塞性肺疾病（COPD）或哮喘）中的应用）。

5. 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。

6. 发明申请

WO2015110826A1 (2S)-N-[(1S)-1-CYANO-2-PHENYLETHYL]-1,4-OXAZEPANE-2-CARBOXAMIDES AS DIPEPTIDYL PEPTIDASE I INHIBITORS 审中-公开
标题翻译：（2S）-N - [（1S）-1-氰基-2-苯基] -1,4-氧杂环己烷-2-羧酰胺作为DIPEPTIDYL PEPTIDASE I抑制剂
公开(公告)号：WO2015110826A1
公开(公告)日：2015-07-30
申请号：PCT/GB2015/050155
申请日：2015-01-23
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED
发明人： LÖNN, Hans, Roland , CONNOLLY, Stephen , SWALLOW, Steven , KARLSSON, Staffan PO , AURELL, Carl-Johan , PONTÉN, John Fritiof , DOYLE, Kevin, James , VAN DE POËL, Amanda, Jane , JONES, Graham, Peter , WATSON, David, Wyn , MACRITCHIE, Jaqueline, Anne , PALMER, Nicholas, John
IPC分类号： C07D267/10 , C07D413/14 , C07D413/12 , C07D417/12 , A61K31/553 , A61P11/00
CPC分类号： C07D267/10 , A61K31/553 , A61K45/06 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present disclosure relates to certain (2 S )- N -[(1 S )-1-cyano-2-phenylethyl]-1,4- oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), (Formula (I)) that inhibit dipeptidyl peptidase 1(DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.
摘要翻译：本公开内容涉及某些（2S）-N - [（1S）-1-氰基-2-苯基乙基] -1,4-氧氮杂环庚烷-2-甲酰胺化合物（包括其药学上可接受的盐），（式（I））抑制二肽基肽酶1（DPP1）活性在治疗和/或预防包括呼吸系统疾病如哮喘和慢性阻塞性肺疾病（COPD）在内的临床病症中的用途，用于治疗，包含它们的药物组合物和制备这些化合物的方法。

7. 发明申请

WO2008096121A1 COMBINATIONS OF BETA-2-ADRENOCEPTOR AGONISTIC BENZOTHIAZOLONE 审中-公开
标题翻译： β-2-ADRENOCEPTOR AGONISTIC BENZOTHIAZOLONE的组合
公开(公告)号：WO2008096121A1
公开(公告)日：2008-08-14
申请号：PCT/GB2008/000396
申请日：2008-02-06
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , CADOGAN, Elaine, Bridget , CONNOLLY, Stephen , NICHOLLS, David, John , WILEY, Katherine, Elisabeth , YOUNG, Alan
发明人： CADOGAN, Elaine, Bridget , CONNOLLY, Stephen , NICHOLLS, David, John , WILEY, Katherine, Elisabeth , YOUNG, Alan
IPC分类号： A61K31/428
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 N-[2-(Diethylamino)ethyl]-N-(2-{[2-(4-hydroxy-2-oxo-2,3-dihydro-1,3-benzothiazol-7-yl)ethyl]amino}ethyl)-3-[2-(3-chlorophenyl)ethoxy]pro panamide 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 Inducer; an IKK2 inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; an MPO inhibitor; a muscarinic antagonist; a p38 inhibitor; a PDE inhibitor; a PPARΥ 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：本发明提供包含第一活性成分的药物产品，试剂盒或组合物，其为N- [2-（二乙基氨基）乙基] -N-（2 - {[2-（4-羟基-2-氧代-2,3- 二氢-1,3-苯并噻唑-7-基）乙基]氨基}乙基）-3- [2-（3-氯苯基）乙氧基]丙酰胺或其盐，和第二活性成分，选自：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; 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。

8. 发明申请

WO2008099165A1 PIPERIDINE DERIVATIVES AND THEIR USE FOR TREATMENT OF CCR8 MEDIATED DISEASES 审中-公开
标题翻译：哌啶衍生物及其用于治疗CCR8介导性疾病的用途
公开(公告)号：WO2008099165A1
公开(公告)日：2008-08-21
申请号：PCT/GB2008/000490
申请日：2008-02-13
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , CONNOLLY, Stephen , KRISTOFFERSSON, Anna , SKRINJAR, Marco
发明人： CONNOLLY, Stephen , KRISTOFFERSSON, Anna , SKRINJAR, Marco
IPC分类号： C07D405/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D495/04 , A61K31/4525 , A61K31/453 , A61P11/06
CPC分类号： C07D405/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D495/04
摘要： The present invention provides compounds of formula (I) wherein n, R 1 , R 2 , R 3 and R 4 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译：本发明提供式（I）的化合物，其中n，R 1，R 2，R 3和R 4， SUP>如本说明书中所定义，其制备方法，含有它们的药物组合物及其在治疗中的用途。

9. 发明申请

WO2008096111A1 COMBINATIONS OF BETA- 2 -ADRENOCEPTOR AGONISTIC BENZOTHIAZOLONE 审中-公开
标题翻译： BETA-2 -ADRENOCEPTOR AGONISTIC BENZOTHIAZOLONE的组合
公开(公告)号：WO2008096111A1
公开(公告)日：2008-08-14
申请号：PCT/GB2008/000386
申请日：2008-02-06
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , CADOGAN, Elaine, Bridget , CONNOLLY, Stephen , NICHOLLS, David, John , WILEY, Katherine, Elisabeth , YOUNG, Alan
发明人： CADOGAN, Elaine, Bridget , CONNOLLY, Stephen , NICHOLLS, David, John , WILEY, Katherine, Elisabeth , YOUNG, Alan
IPC分类号： A61K31/428
CPC分类号： A61K45/06 , A61K31/428 , A61K2300/00
摘要： The invention provides a pharmaceutical product comprising a first active ingredient which is N-[2-(Diethylamino)ethyl]-N-(2-{[2-(4-hydroxy-2-oxo-2,3-dihydro-1,3-benzothiazol-7-yl)ethyl]amino}ethyl)-3-[2-(1-naphthyl)ethoxy]propan amide 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 Inducer; an IKK2 inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; an MPO inhibitor; a muscarinic antagonist which is Aclidinium bromide, Glycopyrrolate, Oxitropium bromide, Pirenzepine, telenzepine, Tiotropium bromide, 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide, 3(R)-1-phenethyl-3-(9H-xanthene-9-carbonyloxy)-1-azoniabicyclo[2.2.2]octane bromide or (3R)-3-[(2S)-2-cyclopentyl-2-hydroxy-2-thien-2-ylacetoxy]-1-(2-phenoxyethyl)-1-azoniabicyclo[2.2.2]actane bromide; a p38 inhibitor; a PDE inhibitor; a PPARy 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：本发明提供包含第一活性成分的药物产品，其为N- [2-（二乙基氨基）乙基] -N-（2 - {[2-（4-羟基-2-氧代-2,3-二氢-1,2- 3-苯并噻唑-7-基）乙基]氨基}乙基）-3- [2-（1-萘基）乙氧基]丙酰胺或其盐，和第二活性成分，选自：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; MPO抑制剂; 吖啶啶溴化物，乙酰丙酸乙酯，溴化氧氮，哌仑西平，替硝西泮，噻托溴铵，3（R） - （2-羟基-2,2-二噻吩-2-基乙酰氧基）-1-（3-苯氧基丙基）-1 （R）-1-苯乙基-3-（9H-呫吨-9-羰氧基）-1-氮鎓二环[2.2.2]辛烷溴化物或（3R）-3 - [（ 2S）-2-环戊基-2-羟基-2-噻吩-2-基乙酰氧基] -1-（2-苯氧基乙基）-1-氮鎓二环[2.2.2] 一种p38抑制剂; PDE抑制剂; PPARγ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。

10. 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。

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