公开(公告)号：US20170275277A1

公开(公告)日：2017-09-28

申请号：US15514294

申请日：2015-09-24

Applicant: Almirall, S.A.

Inventor： Carlos PUIG DURAN ,  Jose AIGUADE BOSCH ,  Silvia GUAL ROIG ,  Maria PRAT QUIÑONES

IPC: C07D453/02

CPC classification number: C07D453/02 ,  C07D401/12

Abstract: The present invention relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.

公开(公告)号：US09757383B2

公开(公告)日：2017-09-12

申请号：US14956767

申请日：2015-12-02

Applicant: ALMIRALL, S.A.

Inventor： Jose Aiguade Bosch ,  Silvia Gual Roig ,  Maria Prat Quinones ,  Carlos Puig Duran

IPC: A61K31/538 ,  C07D403/12 ,  C07D413/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/14 ,  A61K31/4178 ,  A61K31/423 ,  A61K31/428 ,  A61K31/4709 ,  A61K45/06 ,  C07D263/58 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/4184

CPC classification number: A61K31/538 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/4709 ,  A61K45/06 ,  C07D263/58 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.

公开(公告)号：US20170151264A1

公开(公告)日：2017-06-01

申请号：US15313737

申请日：2015-05-21

Applicant: Almirall, S.A.

Inventor： Nuria GODESSART MARINA ,  Cristina BALAGUE PELAEZ

IPC: A61K31/573 ,  A61K45/06 ,  A61K31/53

CPC classification number: A61K31/53 ,  A61K31/573 ,  A61K45/06 ,  C07B2200/13 ,  C07C309/04 ,  C07C309/30 ,  C07C309/35 ,  C07D487/04

Abstract: The present invention provides a pharmaceutical composition which comprises (a) a compound which is an inhibitor of phosphoinositide 3-kinase delta or a pharmaceutically acceptable salt and/or solvate thereof, and (b) a corticosteroid.

公开(公告)号：USRE46417E1

公开(公告)日：2017-05-30

申请号：US15019009

申请日：2016-02-09

Applicant: Almirall, S.A.

Inventor： Dolors Fernandez Forner ,  Maria Prat Quiñones ,  Maria Antonia Buil Albero

IPC: A61K31/439 ,  A61K31/46 ,  A61K31/4745 ,  A61K31/56 ,  C07D453/02 ,  C07D453/04 ,  A61K31/345 ,  A61K31/435 ,  A61P1/00 ,  A61P1/04 ,  A61P13/02 ,  A61P13/06 ,  A61K45/06 ,  A61K9/00 ,  A61K47/26 ,  A61P13/10 ,  A61P27/16 ,  A61P43/00 ,  A61P1/06 ,  A61P1/12 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P11/08 ,  A61P11/14 ,  A61P13/00 ,  C07D453/00

CPC classification number: A61K31/439 ,  A61K9/0073 ,  A61K9/0075 ,  A61K31/4745 ,  A61K31/56 ,  A61K45/06 ,  A61K47/26 ,  C07D453/02 ,  Y10S514/826 ,  A61K2300/00

Abstract: A compound according to formula (I) wherein: © is a phenyl ring, a C4 to C9 heteroaromatic compound containing one or more heteroatoms, or a naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl or biphenyl group; which shows high affinity for muscarinic M3 receptors (Hm3).

公开(公告)号：US20160310457A1

公开(公告)日：2016-10-27

申请号：US15103465

申请日：2014-12-05

Applicant: Almirall, S.A

Inventor： Maria PLANELLS JIMENEZ ,  Begoña DUARTE LOPEZ ,  Pere GUIRO COLL

IPC: A61K31/225 ,  A61K9/20

CPC classification number: A61K31/225 ,  A61K9/1623 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2846

Abstract: Pharmaceutical compositions are described comprising (a) dimethyl fumarate, (b) a diluent selected from monosaccharides, disaccharides, starch, and starch derivatives, calcium and magnesium inorganic salts, sugar alcohols, and mixtures thereof, (c) microcrystalline cellulose and (d) croscarmellose sodium, wherein the dimethyl fumarate is not covered with a gastro-resistant coating. These compositions are intended for the treatment of some inflammatory autoimmune diseases or disorders.

Abstract translation: 描述了药物组合物，其包含（a）富马酸二甲酯，（b）选自单糖，二糖，淀粉和淀粉衍生物的稀释剂，钙和镁无机盐，糖醇及其混合物，（c）微晶纤维素和（d） 交联羧甲基纤维素钠，其中富马酸二甲酯不被胃耐药涂层覆盖。 这些组合物旨在用于治疗一些炎症性自身免疫性疾病或病症。

公开(公告)号：US09388189B2

公开(公告)日：2016-07-12

申请号：US14435851

申请日：2013-10-15

Applicant: ALMIRALL, S.A.

Inventor： Montserrat Erra Sola ,  Marta Carrascal Riera ,  Joan Taltavull Moll ,  Juan Francisco Caturla Javaloyes ,  Francisco Javier Bernal Anchuela ,  Lluis Miquel Pages Santacana ,  Marta Mir Cepeda ,  Gaspar Casals Coll ,  Maria Begoña Hernandez Olasagarre

IPC: C07D487/04 ,  C07D519/00 ,  A61K31/53 ,  A61P11/06 ,  A61P11/00 ,  A61K45/06

CPC classification number: C07D487/04 ,  A61K31/53 ,  A61K45/06 ,  C07D519/00

Abstract: New pyrrolotriazinone derivatives having the chemical structure of Formula (I) are disclosed; as well as process for theft preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).

Abstract translation: 公开了具有式（I）化学结构的新的吡咯并三嗪酮衍生物; 以及盗窃制备方法，包含它们的药物组合物及其在治疗中作为磷酸肌醇3-激酶（PI3Ks）抑制剂的用途。

公开(公告)号：US09233108B2

公开(公告)日：2016-01-12

申请号：US14357344

申请日：2012-11-09

Applicant: ALMIRALL, S.A.

Inventor： Jose Aiguade Bosch ,  Silvia Gual Roig ,  Maria Prat Quinones ,  Carlos Puig Duran

IPC: C07D215/00 ,  A61K31/58 ,  A61K31/4709 ,  C07D403/12 ,  C07D413/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/14 ,  A61K31/4178 ,  A61K31/423 ,  A61K31/428 ,  A61K31/538 ,  A61K45/06 ,  C07D263/58 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

CPC classification number: A61K31/538 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/4709 ,  A61K45/06 ,  C07D263/58 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.

Abstract translation: 本发明涉及具有β-肾上腺素能激动剂和M3毒蕈碱拮抗剂双重活性的新化合物，含有它们的药物组合物，其制备方法及其在呼吸治疗中的用途。

公开(公告)号：US20150306089A9

公开(公告)日：2015-10-29

申请号：US14357344

申请日：2012-11-09

Applicant: ALMIRALL, S.A.

Inventor： Jose Aiguade Bosch ,  Silvia Gual Roig ,  Maria Prat Quinones ,  Carlos Puig Duran

IPC: A61K31/4709 ,  A61K45/06 ,  C07D401/12 ,  C07D409/12 ,  C07D413/14 ,  A61K31/428 ,  A61K31/4178 ,  C07D263/58 ,  A61K31/423 ,  A61K31/538 ,  C07D417/14 ,  C07D413/12 ,  C07D417/12

CPC classification number: A61K31/538 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/4709 ,  A61K45/06 ,  C07D263/58 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.

Abstract translation: 本发明涉及具有β-肾上腺素能激动剂和M3毒蕈碱拮抗剂双重活性的新化合物，含有它们的药物组合物，其制备方法及其在呼吸治疗中的用途。

公开(公告)号：US20150065471A1

公开(公告)日：2015-03-05

申请号：US14389843

申请日：2013-03-28

Applicant: ALMIRALL, S.A.

Inventor： Carlos Puig Duran ,  Francesc Carrera Carrera ,  Juan Bautista Pérez Garcia ,  Enrique Moyes Valles ,  Iolanda Marchueta Hereu

IPC: C07D215/26 ,  C07C55/10 ,  A61K31/56 ,  C07D275/06 ,  A61K31/4704 ,  A61K45/06 ,  C07C57/15 ,  C07C309/04

CPC classification number: C07D215/26 ,  A61K31/4704 ,  A61K31/56 ,  A61K45/06 ,  C07B2200/13 ,  C07C55/10 ,  C07C57/15 ,  C07C309/04 ,  C07D215/22 ,  C07D275/06 ,  A61K2300/00

Abstract: The present invention is directed to a pharmaceutically acceptable crystalline addition salt of 5-[(1R)-2-({2-[4-({4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof.

Abstract translation: 本发明涉及5 - [（1R）-2 - （{2- [4 - （{4-（2,2-二氟-2-苯基乙氧基）苯基]乙基}氨基）的药学上可接受的结晶加成盐， -1-羟乙基] -8-羟基喹啉-2（1H） - 酮，和（ii）二羧酸，磺酸或硫酰亚胺或其药学上可接受的溶剂合物。

公开(公告)号：US20150057256A1

公开(公告)日：2015-02-26

申请号：US14386424

申请日：2013-03-15

Applicant: ALMIRALL, S.A.

Inventor： Gemma Mestres Amat ,  Elvira Balaguer Ardanuy ,  Francesc Carrera Carrera ,  Iolanda Marcueta Hereu ,  Enrique Moyes Valls ,  Ravi Chandran Srinivasan

IPC: C07D215/227 ,  A61K45/06 ,  A61K31/4704

CPC classification number: C07D215/227 ,  A61K31/4704 ,  A61K45/06 ,  C07B2200/13 ,  C07D215/26

Abstract: The present invention is directed to novel polymorphic crystal forms of a 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1-(R)-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one, heminapadisylate. The invention is also directed to pharmaceutical compositions comprising said polymorphic crystal forms, methods of using them to treat respiratory diseases associated with β2 adrenergic receptor activity and a process for preparing such polymorphic crystal forms.

Abstract translation: 本发明涉及5-（2 - {[6-（2,2-二氟-2-苯基乙氧基）己基]氨基} -1-（R） - 羟基乙基）-8-羟基喹啉-3-酮的新型多晶型物， 2（1H） - 酮，半淀粉二酸酯。 本发明还涉及包含所述多晶型晶型的药物组合物，使用它们治疗与肾上腺素能受体活性相关的呼吸系统疾病的方法和制备这种多晶型晶形的方法。