NZ545443A - Combination of an aclidinium salt known as 3-(2-hydroxy-2,2-dithiophen-2-yl-acetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane and a steroid and its use to treat respiratory disorders by inhalation - Google Patents

Combination of an aclidinium salt known as 3-(2-hydroxy-2,2-dithiophen-2-yl-acetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane and a steroid and its use to treat respiratory disorders by inhalation

Info

Publication number: NZ545443A
Authority: NZ; New Zealand
Prior art keywords: pharmaceutical composition; composition according; inhalable; propellant; examples
Prior art date: 2003-07-29

Application number

NZ545443A

Other languages

English (en)

Inventor

Michel Pairet

Michael P Pieper

Christopher John Montague Meade

Original Assignee

Boehringer Ingelheim Int

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2003-07-29

Filing date

2004-07-17

Publication date

2010-04-30

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34130038&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NZ545443(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2004-07-17 Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int

2010-04-30 Publication of NZ545443A publication Critical patent/NZ545443A/en

Links

150000003431 steroids Chemical class 0.000 title claims abstract description 23
208000023504 respiratory system disease Diseases 0.000 title description 2
ASMXXROZKSBQIH-UHFFFAOYSA-N [1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octan-3-yl] 2-hydroxy-2,2-dithiophen-2-ylacetate Chemical compound C=1C=CSC=1C(C=1SC=CC=1)(O)C(=O)OC(C(CC1)CC2)C[N+]21CCCOC1=CC=CC=C1 ASMXXROZKSBQIH-UHFFFAOYSA-N 0.000 title 1
ASMXXROZKSBQIH-VITNCHFBSA-N aclidinium Chemical class C([C@@H](C(CC1)CC2)OC(=O)C(O)(C=3SC=CC=3)C=3SC=CC=3)[N+]21CCCOC1=CC=CC=C1 ASMXXROZKSBQIH-VITNCHFBSA-N 0.000 title 1
239000008194 pharmaceutical composition Substances 0.000 claims abstract description 56
239000000203 mixture Substances 0.000 claims abstract description 47
239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 30
150000003839 salts Chemical class 0.000 claims abstract description 30
CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 claims abstract description 23
VOVIALXJUBGFJZ-KWVAZRHASA-N Budesonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H]3OC(CCC)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O VOVIALXJUBGFJZ-KWVAZRHASA-N 0.000 claims abstract description 13
229960004436 budesonide Drugs 0.000 claims abstract description 13
230000002757 inflammatory effect Effects 0.000 claims abstract description 10
230000000414 obstructive effect Effects 0.000 claims abstract description 10
230000000241 respiratory effect Effects 0.000 claims abstract description 10
HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims abstract description 7
239000003814 drug Substances 0.000 claims abstract description 4
239000012453 solvate Substances 0.000 claims abstract description 4
239000000443 aerosol Substances 0.000 claims description 39
239000013543 active substance Substances 0.000 claims description 36
239000003380 propellant Substances 0.000 claims description 27
239000000843 powder Substances 0.000 claims description 22
239000004615 ingredient Substances 0.000 claims description 21
239000002904 solvent Substances 0.000 claims description 19
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 18
239000002253 acid Substances 0.000 claims description 18
-1 polyoxyethylene Polymers 0.000 claims description 15
238000002360 preparation method Methods 0.000 claims description 13
ATUOYWHBWRKTHZ-UHFFFAOYSA-N Propane Chemical compound CCC ATUOYWHBWRKTHZ-UHFFFAOYSA-N 0.000 claims description 12
239000008139 complexing agent Substances 0.000 claims description 12
PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 9
KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 9
DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 9
239000002245 particle Substances 0.000 claims description 9
239000003963 antioxidant agent Substances 0.000 claims description 7
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XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 7
229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 6
NNPPMTNAJDCUHE-UHFFFAOYSA-N isobutane Chemical compound CC(C)C NNPPMTNAJDCUHE-UHFFFAOYSA-N 0.000 claims description 6
IJDNQMDRQITEOD-UHFFFAOYSA-N n-butane Chemical compound CCCC IJDNQMDRQITEOD-UHFFFAOYSA-N 0.000 claims description 6
239000003381 stabilizer Substances 0.000 claims description 6
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239000000796 flavoring agent Substances 0.000 claims description 5
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239000011782 vitamin Substances 0.000 claims description 5
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LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 4
NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical class OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims description 4
XBDQKXXYIPTUBI-UHFFFAOYSA-N Propionic acid Chemical class CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims description 4
150000001298 alcohols Chemical class 0.000 claims description 4
PMPVIKIVABFJJI-UHFFFAOYSA-N Cyclobutane Chemical class C1CCC1 PMPVIKIVABFJJI-UHFFFAOYSA-N 0.000 claims description 3
LVZWSLJZHVFIQJ-UHFFFAOYSA-N Cyclopropane Chemical class C1CC1 LVZWSLJZHVFIQJ-UHFFFAOYSA-N 0.000 claims description 3
OTMSDBZUPAUEDD-UHFFFAOYSA-N Ethane Chemical class CC OTMSDBZUPAUEDD-UHFFFAOYSA-N 0.000 claims description 3
229910019142 PO4 Inorganic materials 0.000 claims description 3
239000002202 Polyethylene glycol Substances 0.000 claims description 3
239000001273 butane Chemical class 0.000 claims description 3
235000014113 dietary fatty acids Nutrition 0.000 claims description 3
MTHSVFCYNBDYFN-UHFFFAOYSA-N diethylene glycol Chemical compound OCCOCCO MTHSVFCYNBDYFN-UHFFFAOYSA-N 0.000 claims description 3
150000002016 disaccharides Chemical class 0.000 claims description 3
229930195729 fatty acid Natural products 0.000 claims description 3
239000000194 fatty acid Substances 0.000 claims description 3
125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 3
239000001282 iso-butane Substances 0.000 claims description 3
VNWKTOKETHGBQD-UHFFFAOYSA-N methane Chemical class C VNWKTOKETHGBQD-UHFFFAOYSA-N 0.000 claims description 3
150000002772 monosaccharides Chemical class 0.000 claims description 3
OFBQJSOFQDEBGM-UHFFFAOYSA-N n-pentane Chemical class CCCCC OFBQJSOFQDEBGM-UHFFFAOYSA-N 0.000 claims description 3
235000021317 phosphate Nutrition 0.000 claims description 3
229920001223 polyethylene glycol Polymers 0.000 claims description 3
229920001451 polypropylene glycol Polymers 0.000 claims description 3
239000001294 propane Chemical class 0.000 claims description 3
229960004063 propylene glycol Drugs 0.000 claims description 3
235000013772 propylene glycol Nutrition 0.000 claims description 3
229940037001 sodium edetate Drugs 0.000 claims description 3
ZMPRRFPMMJQXPP-UHFFFAOYSA-N 2-sulfobenzoic acid Chemical class OC(=O)C1=CC=CC=C1S(O)(=O)=O ZMPRRFPMMJQXPP-UHFFFAOYSA-N 0.000 claims description 2
150000001242 acetic acid derivatives Chemical class 0.000 claims description 2
150000004676 glycans Chemical class 0.000 claims description 2
WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims description 2
TWBYWOBDOCUKOW-UHFFFAOYSA-N isonicotinic acid Chemical class OC(=O)C1=CC=NC=C1 TWBYWOBDOCUKOW-UHFFFAOYSA-N 0.000 claims description 2
150000002482 oligosaccharides Polymers 0.000 claims description 2
150000002942 palmitic acid derivatives Chemical class 0.000 claims description 2
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239000005017 polysaccharide Substances 0.000 claims description 2
159000000000 sodium salts Chemical class 0.000 claims description 2
150000005846 sugar alcohols Polymers 0.000 claims description 2
ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 claims 2
239000003795 chemical substances by application Substances 0.000 abstract 1
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238000009472 formulation Methods 0.000 description 23
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239000002775 capsule Substances 0.000 description 14
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LUKZNWIVRBCLON-GXOBDPJESA-N Ciclesonide Chemical compound C1([C@H]2O[C@@]3([C@H](O2)C[C@@H]2[C@@]3(C[C@H](O)[C@@H]3[C@@]4(C)C=CC(=O)C=C4CC[C@H]32)C)C(=O)COC(=O)C(C)C)CCCCC1 LUKZNWIVRBCLON-GXOBDPJESA-N 0.000 description 10
GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 10
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239000008101 lactose Substances 0.000 description 10
KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 9
CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 8
LERNTVKEWCAPOY-VOGVJGKGSA-N C[N+]1(C)[C@H]2C[C@H](C[C@@H]1[C@H]1O[C@@H]21)OC(=O)C(O)(c1cccs1)c1cccs1 Chemical compound C[N+]1(C)[C@H]2C[C@H](C[C@@H]1[C@H]1O[C@@H]21)OC(=O)C(O)(c1cccs1)c1cccs1 LERNTVKEWCAPOY-VOGVJGKGSA-N 0.000 description 8
238000000034 method Methods 0.000 description 8
229960000257 tiotropium bromide Drugs 0.000 description 8
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MGNNYOODZCAHBA-GQKYHHCASA-N fluticasone Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)SCF)(O)[C@@]2(C)C[C@@H]1O MGNNYOODZCAHBA-GQKYHHCASA-N 0.000 description 7
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QLIIKPVHVRXHRI-CXSFZGCWSA-N mometasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CCl)(O)[C@@]1(C)C[C@@H]2O QLIIKPVHVRXHRI-CXSFZGCWSA-N 0.000 description 7
229920000858 Cyclodextrin Polymers 0.000 description 6
150000004677 hydrates Chemical class 0.000 description 6
VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 5
DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 5
FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 5
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VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 5
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150000001450 anions Chemical class 0.000 description 4
230000001078 anti-cholinergic effect Effects 0.000 description 4
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LVGUZGTVOIAKKC-UHFFFAOYSA-N 1,1,1,2-tetrafluoroethane Chemical compound FCC(F)(F)F LVGUZGTVOIAKKC-UHFFFAOYSA-N 0.000 description 3
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GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 2
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Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
General Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
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Medicinal Chemistry (AREA)
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Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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Rheumatology (AREA)
Medicinal Preparation (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)

NZ545443A 2003-07-29 2004-07-17 Combination of an aclidinium salt known as 3-(2-hydroxy-2,2-dithiophen-2-yl-acetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane and a steroid and its use to treat respiratory disorders by inhalation NZ545443A (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
EP03017162		2003-07-29
PCT/EP2004/008029 WO2005014005A1 (en)	2003-07-29	2004-07-17	Combination of an anticholinergic and a steroid and its use to treat respiratory disorders by inhalation

Publications (1)

Publication Number	Publication Date
NZ545443A true NZ545443A (en)	2010-04-30

Family

ID=34130038

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
NZ545443A NZ545443A (en)	2003-07-29	2004-07-17	Combination of an aclidinium salt known as 3-(2-hydroxy-2,2-dithiophen-2-yl-acetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane and a steroid and its use to treat respiratory disorders by inhalation

Country Status (12)

Country	Link
EP (1)	EP1651236A1 (ru)
JP (1)	JP2007500150A (ru)
KR (1)	KR20060052912A (ru)
CN (1)	CN1829520A (ru)
AU (1)	AU2004262901B2 (ru)
BR (1)	BRPI0413054A (ru)
CA (1)	CA2534128C (ru)
IL (1)	IL173370A0 (ru)
MX (1)	MXPA06001046A (ru)
NZ (1)	NZ545443A (ru)
RU (1)	RU2361586C2 (ru)
WO (1)	WO2005014005A1 (ru)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
ES2165768B1 (es)	1999-07-14	2003-04-01	Almirall Prodesfarma Sa	Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
ES2298049B1 (es)	2006-07-21	2009-10-20	Laboratorios Almirall S.A.	Procedimiento para fabricar bromuro de 3(r)-(2-hidroxi-2,2-ditien-2-ilacetoxi)-1-(3-fenoxipropil)-1-azoniabiciclo (2.2.2) octano.
EP2100599A1 (en)	2008-03-13	2009-09-16	Laboratorios Almirall, S.A.	Inhalation composition containing aclidinium for treatment of asthma and chronic obstructive pulmonary disease
EP2100598A1 (en) *	2008-03-13	2009-09-16	Laboratorios Almirall, S.A.	Inhalation composition containing aclidinium for treatment of asthma and chronic obstructive pulmonary disease
US8815258B2 (en)	2009-05-29	2014-08-26	Pearl Therapeutics, Inc.	Compositions, methods and systems for respiratory delivery of two or more active agents
KR20170070274A (ko)	2009-05-29	2017-06-21	펄 테라퓨틱스 인코포레이티드	지속형 무스카린 안타고니스트 및 지속형 ｂ₂아드레날린 수용체 아고니스트의 폐 전달용 조성물, 및 연관된 방법 및 시스템
EP2510928A1 (en)	2011-04-15	2012-10-17	Almirall, S.A.	Aclidinium for use in improving the quality of sleep in respiratory patients
JP6454323B2 (ja)	2013-03-15	2019-01-16	パールセラピューティクス，インコーポレイテッド	粒子状結晶性材料のコンディショニングのための方法及びシステム

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
ES2165768B1 (es) *	1999-07-14	2003-04-01	Almirall Prodesfarma Sa	Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
US20020183292A1 (en) *	2000-10-31	2002-12-05	Michel Pairet	Pharmaceutical compositions based on anticholinergics and corticosteroids
ES2257152B1 (es) *	2004-05-31	2007-07-01	Laboratorios Almirall S.A.	Combinaciones que comprenden agentes antimuscarinicos y agonistas beta-adrenergicos.

2004
- 2004-07-17 KR KR1020067001862A patent/KR20060052912A/ko not_active Ceased
- 2004-07-17 BR BRPI0413054-5A patent/BRPI0413054A/pt not_active IP Right Cessation
- 2004-07-17 EP EP04763322A patent/EP1651236A1/en not_active Withdrawn
- 2004-07-17 CA CA2534128A patent/CA2534128C/en not_active Expired - Lifetime
- 2004-07-17 MX MXPA06001046A patent/MXPA06001046A/es unknown
- 2004-07-17 NZ NZ545443A patent/NZ545443A/en not_active IP Right Cessation
- 2004-07-17 RU RU2006105719/15A patent/RU2361586C2/ru not_active IP Right Cessation
- 2004-07-17 WO PCT/EP2004/008029 patent/WO2005014005A1/en not_active Ceased
- 2004-07-17 JP JP2006521460A patent/JP2007500150A/ja active Pending
- 2004-07-17 AU AU2004262901A patent/AU2004262901B2/en not_active Revoked
- 2004-07-17 CN CNA2004800220913A patent/CN1829520A/zh active Pending
2006
- 2006-01-26 IL IL173370A patent/IL173370A0/en unknown

Also Published As

Publication number	Publication date
KR20060052912A (ko)	2006-05-19
WO2005014005A1 (en)	2005-02-17
EP1651236A1 (en)	2006-05-03
AU2004262901B2 (en)	2010-05-13
MXPA06001046A (es)	2006-04-24
CA2534128A1 (en)	2005-02-17
RU2006105719A (ru)	2007-12-10
CA2534128C (en)	2012-10-23
AU2004262901A1 (en)	2005-02-17
JP2007500150A (ja)	2007-01-11
IL173370A0 (en)	2006-06-11
CN1829520A (zh)	2006-09-06
RU2361586C2 (ru)	2009-07-20
BRPI0413054A (pt)	2006-10-17

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US20110038806A1 (en)	2011-02-17	Medicaments for inhalation comprising an anticholinergic and a steroid
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AU2003216921B2 (en)	2008-03-13	Medicaments containing steroids and a novel anticholinesterase drug
CA2568834A1 (en)	2006-01-12	Medicaments for inhalation comprising steroids and an anticholinergic
CA2534128C (en)	2012-10-23	Combination of an anticholinergic and a steroid and its use to treat respiratory disorders by inhalation
US20060110329A1 (en)	2006-05-25	Inhalable pharmaceutical compositions containing an anticholinergic, salmeterol, and a steroid
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US20050059643A1 (en)	2005-03-17	Medicaments for inhalation comprising a steroid and a betamimetic
CA2533792C (en)	2012-09-11	Medicaments for inhalation comprising steroids and fluorene carboxylic acid esters
CA2614631C (en)	2011-06-14	Pharmaceutical compositions based on anticholinergics and corticosteroids in the form of an inhalable solution or suspension
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Legal Events

Date	Code	Title
2010-08-27	PSEA	Patent sealed
2010-12-24	RENW	Renewal (renewal fees accepted)
2011-07-29	RENW	Renewal (renewal fees accepted)
2012-10-26	S43	Surrender of patents according section 43 patents act