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1. 发明申请

WO2003074058A1 AEROSOL FORMULATIONS CONTAINING ESTERS OF 3,17-DIHYDROXY OESTRATRIENE DERIVATIVES FOR PULMONARY DELIVERY 审中-公开
标题翻译：含有3,17-DIHYDROXY OESTRATRIENE衍生物的用于脉冲递送的产品的气溶胶配方
公开(公告)号：WO2003074058A1
公开(公告)日：2003-09-12
申请号：PCT/EP2003/001856
申请日：2003-02-24
申请人： CHIESI FARMACEUTICI S.p.A. , DAVIES, Rebecca, Jaine , GANDERTON, David , LEWIS, David, Andrew , MEAKIN, Brian, John , BRAMBILLA, Gaetano , FERRARIS, Alessandra
发明人： DAVIES, Rebecca, Jaine , GANDERTON, David , LEWIS, David, Andrew , MEAKIN, Brian, John , BRAMBILLA, Gaetano , FERRARIS, Alessandra
IPC分类号： A61K31/565
CPC分类号： A61K9/008 , A61K31/565 , A61K47/10
摘要： The invention discloses formulations for administration with pressurized metered dose inhalers containing as active ingredient esters of 3,17-dihydroxy oestratriene derivatives, in solution in a hydrofluorocarbon propellant, optionally one or more co-solvents, and their use for the treatment of postmenopausal symptoms as well as of menstrual migraine headaches.
摘要翻译：本发明公开了用于给予含有3,17-二羟基雌三烯衍生物的活性成分的加压计量吸入器的制剂，在氢氟烃推进剂的溶液中，任选的一种或多种共溶剂，以及它们用于治疗绝经后症状的用途以及月经偏头痛。

2. 发明申请

WO2003074024A1 FORMOTEROL SUPERFINE FORMULATION 审中-公开
标题翻译：福莫特罗超级配方
公开(公告)号：WO2003074024A1
公开(公告)日：2003-09-12
申请号：PCT/EP2003/001964
申请日：2003-02-26
申请人： CHIESI FARMACEUTICI S.P.A , DAVIES, Rebecca, Jaine , GANDERTON, David , LEWIS, David, Andrew , MEAKIN, Brian, John , CHURCH, Tanya, Kathleen , BRAMBILLA, Gaetano , FERRARIS, Alessandra
发明人： DAVIES, Rebecca, Jaine , GANDERTON, David , LEWIS, David, Andrew , MEAKIN, Brian, John , CHURCH, Tanya, Kathleen , BRAMBILLA, Gaetano , FERRARIS, Alessandra
IPC分类号： A61K9/00
CPC分类号： A61K9/008 , A61K31/4704 , A61K31/485 , A61K45/06 , A61K47/10 , A61K2300/00
摘要： The present invention relates to a pharmaceutical formulation for use in the administration of a long-acting ß 2 -agonist by inhalation. In particular this invention relates to a chemically stable highly efficient formoterol HFA solution formulation to be administered by pressurised metered dose inhalers (pMDIs) characterized by a deep lung penetration. The invention also relates to methods for the preparation of said formulation and to its use in respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD).
摘要翻译：本发明涉及用于通过吸入施用长效β2激动剂的药物制剂。特别地，本发明涉及一种化学稳定的高效福莫特罗HFA溶液制剂，其由以深层肺穿透为特征的加压计量剂量吸入器（pMDI）施用。本发明还涉及制备所述制剂及其在呼吸系统疾病如哮喘和慢性阻塞性肺疾病（COPD）中的应用的方法。

3. 发明申请

WO2003053501A1 METERED DOSE INHALER 审中-公开
标题翻译：计量剂量吸入器
公开(公告)号：WO2003053501A1
公开(公告)日：2003-07-03
申请号：PCT/EP2002/014588
申请日：2002-12-19
申请人： CHIESI FARMACEUTICI S.P.A.
发明人： DAVIES, Rebecca, Jayne , GANDERTON, David , LEWIS, David, Andrew , MEAKIN, Brian, John
IPC分类号： A61M15/00
CPC分类号： A61K9/008 , A61K31/352 , A61K47/10 , A61K47/14 , A61M15/009
摘要： The present invention relates to pressurized metered dose inhaler (pMDI) actuators (2) with laser drilled orifices and to medicinal aerosol solution formulation products comprising these actuators (2). In particular, the present invention relates to the optimisation of the output characteristics of drug solution formulations in hydrofluoroalkanes (HFAs) by use of pMDIs with actuators (2) with laser drilled orifices of specific dimensions. Moreover, the actuators (2) of the present invention allow the use of solution formulations with a high ethanol content and a high ratio of ethanol to active ingredients and thus, the use of poorly soluble active ingredients in solution formulations and allow the use of solution formulations which are substantially free of low volatility components.
摘要翻译：本发明涉及具有激光钻孔的加压计量吸入器（pMDI）致动器（2）和包括这些致动器（2）的医用气溶胶制剂产品。特别地，本发明涉及通过使用具有特定尺寸的激光钻孔的致动器（2）的pMDI来优化氢氟烷烃（HFAs）中药物溶液制剂的输出特性。此外，本发明的致动器（2）允许使用具有高乙醇含量和高比例的乙醇与活性成分的溶液制剂，因此在溶液制剂中使用难溶性活性成分并允许使用溶液基本上不含低挥发性组分的制剂。

4. 发明申请

WO2002072448A1 INHALER WITH MEANS FOR IMPROVING CHEMICAL STABILITY OF MEDICINAL AEROSOL SOLUTION CONTAINED THEREIN 审中-公开
标题翻译：具有改善含有药物溶解度的化学稳定性的方法的吸入剂
公开(公告)号：WO2002072448A1
公开(公告)日：2002-09-19
申请号：PCT/EP2002/002710
申请日：2002-03-12
申请人： CHIESI FARMACEUTICI S.P.A. , LEWIS, David , GANDERTON, David , MEAKIN, Brian , BRAMBILLA, Gaetano , FERRARIS, Alessandra
发明人： LEWIS, David , GANDERTON, David , MEAKIN, Brian , BRAMBILLA, Gaetano , FERRARIS, Alessandra
IPC分类号： B65D83/14
CPC分类号： B65D83/54 , A61K9/008 , B65D83/38
摘要： The present invention relates to a medicinal aerosol solution formulation product with improed chemical stability, comprising a pressurized metered dose inhaler (10), comprising an aerosol canister (16) equipped with a metering valve (18) and containing a medicinal aerosol solution formulation (12) containing an active ingredient subject to a degradation by means of peroxides or other leachables, a hydrofluorocarbon propellant, a co-solvent and optionally a low-volatility component, wherein optionally part or all of the internal surfaces of said inhaler consists of stainless steel, anodized aluminum or are lined with an inert organic coating, and wherein the canister has a rim with rounded edges which avoids contact of a sharp edge with the rubbers used as valve gaskets.
摘要翻译：本发明涉及具有改善的化学稳定性的药物气溶胶溶液制剂产品，其包括加压计量剂量吸入器（10），其包括装有计量阀（18）并含有药物气溶胶制剂（12）的气溶胶罐（16）），其包含通过过氧化物或其它可浸出物降解的活性成分，氢氟烃推进剂，共溶剂和任选的低挥发性组分，其中所述吸入器的任选部分或全部内表面由不锈钢，阳极氧化铝或衬有惰性有机涂层，并且其中罐具有带有圆形边缘的边缘，避免尖锐边缘与用作阀垫片的橡胶接触。

5. 发明申请

WO2003074025A2 PRESSURISED METERED DOSE INHALERS CONTAINING SOLUTIONS OF BETA-2 AGONISTS 审中-公开
标题翻译：含有BETA-2激动剂解决方案的压力计量剂吸入剂
公开(公告)号：WO2003074025A2
公开(公告)日：2003-09-12
申请号：PCT/EP2003/002004
申请日：2003-02-27
申请人： CHIESI FARMACEUTICI S.P.A. , DAVIES, Rebecca, Jaine , GANDERTON, David , LEWIS, David, Andrew , MEAKIN, Brian, John , CHURCH, Tanya, Kathleen , BRAMBILLA, Gaetano , FERRARIS, Alessandra
发明人： DAVIES, Rebecca, Jaine , GANDERTON, David , LEWIS, David, Andrew , MEAKIN, Brian, John , CHURCH, Tanya, Kathleen , BRAMBILLA, Gaetano , FERRARIS, Alessandra
IPC分类号： A61K9/00
CPC分类号： A61K9/008 , A61K31/4704 , A61K31/485 , A61K45/06 , A61K47/10 , A61K2300/00
摘要： The present invention relates to a pharmaceutical formulation for use in the administration of 2(1H)-quinolinone derivatives long-acting β 2 -agonists by inhalation. In particular this invention relates to a chemically stable highly efficient TA 2005 HFA solution formulation to be administered by pressurised metered dose inhalers (pMDIs) characterized by a deep lung penetration. The invention also relates to methods for the preparation of said formulation and to its use in respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD).
摘要翻译：本发明涉及用于通过吸入给药2（1H） - 喹啉酮衍生物长效β2-激动剂的药物制剂。特别地，本发明涉及一种化学稳定高效的TA 2005 HFA溶液制剂，其通过深层肺穿透特征的加压计量剂量吸入器（pMDI）来施用。本发明还涉及制备所述制剂及其在呼吸系统疾病如哮喘和慢性阻塞性肺疾病（COPD）中的应用的方法。

6. 发明申请

WO2003074023A1 AEROSOL FORMULATIONS FOR PULMONARY ADMINISTRATION OF MEDICAMENTS TO PRODUCE A SYSTEMIC EFFECT 审中-公开
标题翻译：用于产生药物作用的药物的脉管制剂的气雾剂制剂
公开(公告)号：WO2003074023A1
公开(公告)日：2003-09-12
申请号：PCT/EP2003/001962
申请日：2003-02-26
申请人： CHIESI FARMACEUTICI S.p.A. , DAVIES, Rebecca, Jaine , GANDERTON, David , LEWIS, David, Andrew , MEAKIN, Brian, John , BRAMBILLA, Gaetano , FERRARIS, Alessandra
发明人： DAVIES, Rebecca, Jaine , GANDERTON, David , LEWIS, David, Andrew , MEAKIN, Brian, John , BRAMBILLA, Gaetano , FERRARIS, Alessandra
IPC分类号： A61K9/00
CPC分类号： A61K9/008 , A61K31/00 , A61K31/4704 , A61K31/485 , A61K45/06 , A61K47/10 , A61K2300/00
摘要： The invention discloses an aerosol pharmaceutical composition comprising a medicament in solution in a mixture of a hydrofluoroalkane propellant and one or more co-solvents wherein the aerosol liquid droplets delivered on actuation of the inhaler have a particle size comprised between 0,5 µm and 2.5 µm, with a mass median aerodynamic diameter of about 1-2 µm and wherein the fine particle fraction is at least 30%.
摘要翻译：本发明公开了一种气溶胶药物组合物，其包含在氢氟烷烃推进剂和一种或多种助溶剂的混合物中的溶液中的药物，其中在致动吸入器时输送的气溶胶液滴的粒径为0.5微米至2.5微米，质量中值空气动力学直径为约1-2微米，其中细颗粒分数为至少30％。

7. 发明申请

WO2005084640A1 STABLE PHARMACEUTICAL SOLUTION FORMULATIONS FOR PRESSURIZED METERED DOSE INHALERS 审中-公开
标题翻译：用于加压计量剂量吸入器的稳定的药物溶液制剂
公开(公告)号：WO2005084640A1
公开(公告)日：2005-09-15
申请号：PCT/EP2005/002042
申请日：2005-02-25
申请人： CHIESI FARMACEUTICI S.p.A. , LEWIS, David , GANDERTON, David , MEAKIN, Brian , DELCANALE, Maurizio , PIVETTI, Fausto
发明人： LEWIS, David , GANDERTON, David , MEAKIN, Brian , DELCANALE, Maurizio , PIVETTI, Fausto
IPC分类号： A61K9/12
CPC分类号： A61K9/008 , A61K31/137 , A61K31/47 , A61K31/4704 , A61K47/02 , A61M15/009 , A61M2205/0222 , A61K2300/00
摘要： Aerosol solution formulations for use in an aerosol inhaler which comprise 8-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino] ethyl]-2(1H)-quinolinone or a salt thereof, in particular the hydrochloride salt (TA 2005), as an active ingredient, a propellant containing a hydrofluoroalkane, and a cosolvent, stabilized by addition of a specific small amount of a high concentrated phosphoric acid and optionally by the use of a suitable can having part or all of its internal metallic surfaces lined with an inert organic coating.
摘要翻译：用于气溶胶吸入器的气溶胶溶液制剂，其包含8-羟基-5 - [（1R）-1-羟基-2 - [[（1R）-2-（4-甲氧基苯基）-1-甲基乙基]氨基]乙基] -2（1H） - 喹啉酮或其盐，特别是盐酸盐（TA 2005）作为活性成分，含有氢氟烷烃和助溶剂的推进剂，通过加入特定量的高浓度磷酸并且任选地通过使用合适的罐，其具有内衬有惰性有机涂层的部分或全部内部金属表面。

8. 发明申请

WO2004037227A1 SALMETEROL SUPERFINE FORMULATION 审中-公开
标题翻译：沙利度醇超级配方
公开(公告)号：WO2004037227A1
公开(公告)日：2004-05-06
申请号：PCT/EP2003/006444
申请日：2003-06-18
申请人： CHIESI FARMACEUTICI S.P.A. , CHURCH, Tanya, Kathleen , LEWIS, David, Andrew , GANDERTON, David , MEAKIN, Brian, John , BRAMBILLA, Gaetano
发明人： CHURCH, Tanya, Kathleen , LEWIS, David, Andrew , GANDERTON, David , MEAKIN, Brian, John , BRAMBILLA, Gaetano
IPC分类号： A61K9/12
CPC分类号： A61K9/008 , A61K31/4704 , A61K31/485 , A61K45/06 , A61K2300/00
摘要： The present invention relates to a pharmaceutical formulation for use in the administration of a long-acting β 2 -agonist by inhalation. In particular this invention relates to a chemically stable, highly efficient salmeterol HFA solution formulation to be administered by pressurised metered dose inhalers (pMDIs) characterized by a deep lung penetration. The invention also relates to methods for the preparation of said formulation and to its use in respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD).
摘要翻译：本发明涉及用于通过吸入施用长效β2-激动剂的药物制剂。特别地，本发明涉及一种化学稳定，高效的沙美特罗HFA溶液制剂，其由以深肺渗透为特征的加压计量剂量吸入器（pMDI）施用。本发明还涉及制备所述制剂及其在呼吸系统疾病如哮喘和慢性阻塞性肺疾病（COPD）中的应用的方法。

9. 发明申请

WO2003074025A3 PRESSURISED METERED DOSE INHALERS CONTAINING SOLUTIONS OF BETA-2 AGONISTS 审中-公开
公开(公告)号：WO2003074025A3
公开(公告)日：2003-09-12
申请号：PCT/EP2003/002004
申请日：2003-02-27
申请人： CHIESI FARMACEUTICI S.P.A. , DAVIES, Rebecca, Jaine , GANDERTON, David , LEWIS, David, Andrew , MEAKIN, Brian, John , CHURCH, Tanya, Kathleen , BRAMBILLA, Gaetano , FERRARIS, Alessandra
发明人： DAVIES, Rebecca, Jaine , GANDERTON, David , LEWIS, David, Andrew , MEAKIN, Brian, John , CHURCH, Tanya, Kathleen , BRAMBILLA, Gaetano , FERRARIS, Alessandra
IPC分类号： A61K9/00
摘要： The present invention relates to a pharmaceutical formulation for use in the administration of 2(1H)-quinolinone derivatives long-acting β 2 -agonists by inhalation. In particular this invention relates to a chemically stable highly efficient TA 2005 HFA solution formulation to be administered by pressurised metered dose inhalers (pMDIs) characterized by a deep lung penetration. The invention also relates to methods for the preparation of said formulation and to its use in respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD).

10. 发明授权

EP1480615B1 FORMOTEROL SUPERFINE FORMULATION 有权
标题翻译：福莫特罗的超细成分
公开(公告)号：EP1480615B1
公开(公告)日：2010-04-28
申请号：EP03718677.2
申请日：2003-02-26
申请人： CHIESI FARMACEUTICI S.p.A.
发明人： DAVIES, Rebecca, Jaine , GANDERTON, David , LEWIS, David, Andrew , MEAKIN, Brian, John , CHURCH, Tanya, Kathleen , BRAMBILLA, Gaetano , FERRARIS, Alessandra
IPC分类号： A61K9/00 , A61K31/485
CPC分类号： A61K9/008 , A61K31/4704 , A61K31/485 , A61K45/06 , A61K47/10 , A61K2300/00
摘要： The present invention relates to a pharmaceutical formulation for use in the administration of a long-acting ² 2 -agonist by inhalation. In particular this invention relates to a chemically stable highly efficient formoterol HFA solution formulation to be administered by pressurised metered dose inhalers (pMDIs) characterized by a deep lung penetration. The invention also relates to methods for the preparation of said formulation and to its use in respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD).

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