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91.PROCESS FOR PREPARING 5-(2--1(R)-HYDROXYETHYL)-8-HYDROXYQUINOLIN-2(1H)-ONE VIA A NOVEL INTERMEDIATE 有权
Title translation: 通过新型中间体制备5-(2--1(R) - 羟基乙基)-8-羟基喹啉-2(1H) - 酮的方法公开(公告)号:US20150011769A1
公开(公告)日:2015-01-08
申请号:US14350108
申请日:2012-10-02
Applicant: ALMIRALL, S.A.
Inventor: Iolanda Marchueta Hereu , Enrique Moyes Valls
IPC: C07D215/26
CPC classification number: C07D215/26 , A61K31/4704 , Y02P20/55
Abstract: The present invention is concerned with a process for preparing 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1(R)-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one or a pharmaceutically acceptable salt thereof.
Abstract translation: 本发明涉及制备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-2(1H ) - 酮或其药学上可接受的盐。
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公开(公告)号:US20140303126A1
公开(公告)日:2014-10-09
申请号:US14311102
申请日:2014-06-20
Applicant: ALMIRALL, S.A.
IPC: C07D453/02 , A61K45/06 , A61K31/439
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 z© 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; R1, R2 and R3 each independently represent a hydrogen or halogen atom, or a hydroxy group, or a phenyl, —OR4, —SR4, —NR4R5, —NHCOR4, —CONR4R5, —CN, —NO2, —COOR4 or —CF3 group, or a straight or branched lower alkyl group which may optionally be substituted, for example, with a hydroxy or alcoxy group, wherein R4 and R5 each independently represent a hydrogen atom, straight or branched lower alkyl group, or together form an alicyclic ring; or R1 and R2 together form an aromatic, alicyclic or heterocyclic ring; n is an integer from 0 to 4; A represents a —CH2—, —CH═CR6, —CR6═CH—, —CR6R7—, —CO—, —O—, —S—, —S(O)—, SO2 or NR6— group, wherein R6 and R7 each independently represent a hydrogen atom, straight or branched lower alkyl group, or R6 and R7 together form an alicyclic ring; in is an integer from 0 to 8; provided that when m=0, A is not —CH2—; p is an integer from 1 to 2 and the substitution in the azoniabicyclic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; B represents a group of formula (i) or (ii), wherein R10 represents a hydrogen atom, a hydroxy or methyl group; and R8 and R9 each independently represents formulae (a), (b), (c), (d) and wherein R11 represents a hydrogen or halogen atom, or a straight or branched lower alkyl group and Q represents a single bond, —CH2—, —CH2—CH2, —O—, —O—CH2—, —S—, —S—CH2— or —CH═CH—, and when (i) or (ii) contain a chiral centre they may represent either configuration; X represents a pharmaceutically acceptable anion of a mono or polyvalent acid, which shows high affinity for muscarinic M3 receptors (Hm3).
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公开(公告)号:US20130125884A1
公开(公告)日:2013-05-23
申请号:US13672893
申请日:2012-11-09
Applicant: Almirall, S.A.
Inventor: Rosa LAMARCA CASADO , Gonzalo De Miquel SERRA
CPC classification number: A61K9/0073 , A61K9/0075 , A61K31/167 , A61K31/439 , A61K31/46 , A61K31/58 , A61K45/06 , A61M15/0065 , A61K2300/00
Abstract: The present disclosure relates to pharmaceutical compositions for inhalation comprising aclidinium in the form of a dry powder of a pharmaceutically acceptable salt in admixture with a pharmaceutically acceptable dry powder carrier, providing a metered nominal dose of aclidinium equivalent to about 200 micrograms aclidinium bromide.
Abstract translation: 本公开涉及用于吸入的药物组合物,其包含药学上可接受的盐的干燥粉末形式的药物组合物,其与药学上可接受的干粉载体混合,提供等量的标称剂量的等价于约200微克溴化铱的吖啶鎓。
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