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公开(公告)号:US20150246026A1
公开(公告)日:2015-09-03
申请号:US14712866
申请日:2015-05-14
Applicant: ALMIRALL, S.A.
IPC: A61K31/439 , A61K9/00 , A61K31/56 , A61K47/26 , A61K45/06
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—, —CR6122—, —CO—, —O—, —S—, —S(O)—, SO2 or NR6— group, wherein R6 and R2 each independently represent a hydrogen atom, straight or branched lower alkyl group, or R6 and 122 together form an alicyclic ring; m 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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2.NOVEL QUINUCLIDINE DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME 有权
Title translation: 新颖的喹啉衍生物和含有它们的药物组合物公开(公告)号:US20160296503A1
公开(公告)日:2016-10-13
申请号:US15095036
申请日:2016-04-09
Applicant: ALMIRALL, S.A.
IPC: A61K31/439 , A61K45/06 , A61K31/56 , A61K9/00 , A61K47/26
CPC classification number: A61K31/439 , A61K9/0073 , A61K9/0075 , A61K31/4745 , A61K31/56 , A61K45/06 , A61K47/26 , C07D453/02 , Y10S514/826 , A61K2300/00
Abstract: Provided is an aerosol container comprising a powder inhalant comprising 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane wherein an anion X− is associated with the positive charge of the nitrogen atom and wherein X− is a pharmaceutically acceptable anion of a mono- or polyvalent acid.
Abstract translation: 本发明提供一种气溶胶容器,其包含粉末吸入剂,其包含3(R) - (2-羟基-2,2-二噻吩-2-基乙酰氧基)-1-(3-苯氧基丙基)-1-氮鎓二环[2.2.2]辛烷,其中 阴离子X-与氮原子的正电荷相关,其中X-是单价或多价酸的药学上可接受的阴离子。
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公开(公告)号:US20190183867A1
公开(公告)日:2019-06-20
申请号:US16045333
申请日:2018-07-25
Applicant: ALMIRALL, S.A.
IPC: A61K31/439 , A61K9/00 , A61K47/26 , A61K31/4745 , C07D453/02 , A61K45/06 , A61K31/56
Abstract: Provided is a method for treating chronic obstructive pulmonary disease or chronic bronchitis, or inhibiting bronchospasm, which method comprises use of a powder inhaler to administer to a human patient in need of such treatment an effective amount of a powder inhalant, wherein the powder inhalant comprises 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropy1)-1-azoniabicyclo[2.2.2]octane bromide.
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公开(公告)号:US20170319557A1
公开(公告)日:2017-11-09
申请号:US15599646
申请日:2017-05-19
Applicant: ALMIRALL, S.A.
IPC: A61K31/439 , C07D453/02 , A61K9/00 , A61K31/56 , A61K31/4745 , A61K45/06 , A61K47/26
CPC classification number: A61K31/439 , A61K9/0073 , A61K9/0075 , A61K31/4745 , A61K31/56 , A61K45/06 , A61K47/26 , C07D453/02 , Y10S514/826 , A61K2300/00
Abstract: Provided is a powder inhaler comprising a powder inhalant comprising 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane wherein an anion X− is associated with the positive charge of the nitrogen atom and wherein X− is a pharmaceutically acceptable anion of a mono- or polyvalent acid
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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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