HRP20010828A2 - Novel medicament compositions, based on anticholinergically effective compounds and beta-mimetics - Google Patents
Novel medicament compositions, based on anticholinergically effective compounds and beta-mimetics Download PDFInfo
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- HRP20010828A2 HRP20010828A2 HR20010828A HRP20010828A HRP20010828A2 HR P20010828 A2 HRP20010828 A2 HR P20010828A2 HR 20010828 A HR20010828 A HR 20010828A HR P20010828 A HRP20010828 A HR P20010828A HR P20010828 A2 HRP20010828 A2 HR P20010828A2
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- 239000000203 mixture Substances 0.000 title claims description 18
- 239000003814 drug Substances 0.000 title claims description 11
- 150000001875 compounds Chemical class 0.000 title description 7
- 239000000808 adrenergic beta-agonist Substances 0.000 title 1
- 230000003454 betamimetic effect Effects 0.000 title 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 51
- 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 claims description 30
- 229960000257 tiotropium bromide Drugs 0.000 claims description 30
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 18
- OBRNDARFFFHCGE-PERKLWIXSA-N (S,S)-formoterol fumarate Chemical compound OC(=O)\C=C\C(O)=O.C1=CC(OC)=CC=C1C[C@H](C)NC[C@@H](O)C1=CC=C(O)C(NC=O)=C1.C1=CC(OC)=CC=C1C[C@H](C)NC[C@@H](O)C1=CC=C(O)C(NC=O)=C1 OBRNDARFFFHCGE-PERKLWIXSA-N 0.000 claims description 17
- 229960000193 formoterol fumarate Drugs 0.000 claims description 17
- -1 C1-C4-alkyl radical Chemical class 0.000 claims description 16
- 125000001544 thienyl group Chemical group 0.000 claims description 16
- 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 description 14
- BPZSYCZIITTYBL-UHFFFAOYSA-N formoterol Chemical compound C1=CC(OC)=CC=C1CC(C)NCC(O)C1=CC=C(O)C(NC=O)=C1 BPZSYCZIITTYBL-UHFFFAOYSA-N 0.000 claims description 14
- 229960002848 formoterol Drugs 0.000 claims description 14
- 230000001078 anti-cholinergic effect Effects 0.000 claims description 13
- 229910052739 hydrogen Inorganic materials 0.000 claims description 12
- 239000001257 hydrogen Substances 0.000 claims description 12
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 12
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 10
- 229910052731 fluorine Inorganic materials 0.000 claims description 10
- 239000011737 fluorine Substances 0.000 claims description 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
- 239000002253 acid Substances 0.000 claims description 9
- 238000002360 preparation method Methods 0.000 claims description 9
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 9
- 150000003839 salts Chemical class 0.000 claims description 9
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 8
- 229910052801 chlorine Chemical group 0.000 claims description 8
- 239000000460 chlorine Chemical group 0.000 claims description 8
- 125000001153 fluoro group Chemical group F* 0.000 claims description 8
- GIIZNNXWQWCKIB-UHFFFAOYSA-N Serevent Chemical compound C1=C(O)C(CO)=CC(C(O)CNCCCCCCOCCCCC=2C=CC=CC=2)=C1 GIIZNNXWQWCKIB-UHFFFAOYSA-N 0.000 claims description 7
- 150000001450 anions Chemical class 0.000 claims description 7
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 7
- 150000003254 radicals Chemical class 0.000 claims description 7
- 229960004017 salmeterol Drugs 0.000 claims description 7
- YUDRVAHLXDBKSR-UHFFFAOYSA-N [CH]1CCCCC1 Chemical compound [CH]1CCCCC1 YUDRVAHLXDBKSR-UHFFFAOYSA-N 0.000 claims description 6
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical group [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 claims description 6
- 150000001414 amino alcohols Chemical class 0.000 claims description 6
- 238000004519 manufacturing process Methods 0.000 claims description 6
- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 claims description 5
- VPNYRYCIDCJBOM-UHFFFAOYSA-M Glycopyrronium bromide Chemical compound [Br-].C1[N+](C)(C)CCC1OC(=O)C(O)(C=1C=CC=CC=1)C1CCCC1 VPNYRYCIDCJBOM-UHFFFAOYSA-M 0.000 claims description 5
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- 229960002462 glycopyrronium bromide Drugs 0.000 claims description 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 5
- DBCKRBGYGMVSTI-UHFFFAOYSA-N 2-oxo-7-[2-[2-[3-(2-phenylethoxy)propylsulfonyl]ethylazaniumyl]ethyl]-3h-1,3-benzothiazol-4-olate Chemical compound C1=2SC(=O)NC=2C(O)=CC=C1CCNCCS(=O)(=O)CCCOCCC1=CC=CC=C1 DBCKRBGYGMVSTI-UHFFFAOYSA-N 0.000 claims description 4
- MNJNSRQVLNIPFN-UHFFFAOYSA-N 4-[2-[[4-(benzimidazol-1-yl)-2-methylbutan-2-yl]amino]-1-hydroxyethyl]-2-[(4-methoxyphenyl)methylamino]phenol Chemical compound C1=CC(OC)=CC=C1CNC1=CC(C(O)CNC(C)(C)CCN2C3=CC=CC=C3N=C2)=CC=C1O MNJNSRQVLNIPFN-UHFFFAOYSA-N 0.000 claims description 4
- KOTMQCNDGLTIHR-UHFFFAOYSA-N 4-[2-[[4-(benzimidazol-1-yl)-2-methylbutan-2-yl]amino]-1-hydroxyethyl]-3-fluorophenol Chemical compound C1=NC2=CC=CC=C2N1CCC(C)(C)NCC(O)C1=CC=C(O)C=C1F KOTMQCNDGLTIHR-UHFFFAOYSA-N 0.000 claims description 4
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- 238000000034 method Methods 0.000 claims description 4
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- LERNTVKEWCAPOY-DZZGSBJMSA-N tiotropium Chemical class O([C@H]1C[C@@H]2[N+]([C@H](C1)[C@@H]1[C@H]2O1)(C)C)C(=O)C(O)(C=1SC=CC=1)C1=CC=CS1 LERNTVKEWCAPOY-DZZGSBJMSA-N 0.000 claims description 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 3
- 125000004429 atom Chemical group 0.000 claims description 3
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- RTLJQOLVPIGICL-UHFFFAOYSA-N 4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(methylsulfonylmethyl)phenol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(CS(C)(=O)=O)=C1 RTLJQOLVPIGICL-UHFFFAOYSA-N 0.000 claims description 2
- LSLYOANBFKQKPT-DIFFPNOSSA-N 5-[(1r)-1-hydroxy-2-[[(2r)-1-(4-hydroxyphenyl)propan-2-yl]amino]ethyl]benzene-1,3-diol Chemical compound C([C@@H](C)NC[C@H](O)C=1C=C(O)C=C(O)C=1)C1=CC=C(O)C=C1 LSLYOANBFKQKPT-DIFFPNOSSA-N 0.000 claims description 2
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- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims description 2
- VQDBNKDJNJQRDG-UHFFFAOYSA-N Pirbuterol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=N1 VQDBNKDJNJQRDG-UHFFFAOYSA-N 0.000 claims description 2
- WKHOPHIMYDJVSA-UHFFFAOYSA-N [3-[2-(tert-butylamino)-1-hydroxyethyl]-5-(2-methylpropanoyloxy)phenyl] 2-methylpropanoate Chemical compound CC(C)C(=O)OC1=CC(OC(=O)C(C)C)=CC(C(O)CNC(C)(C)C)=C1 WKHOPHIMYDJVSA-UHFFFAOYSA-N 0.000 claims description 2
- ANZXOIAKUNOVQU-UHFFFAOYSA-N bambuterol Chemical compound CN(C)C(=O)OC1=CC(OC(=O)N(C)C)=CC(C(O)CNC(C)(C)C)=C1 ANZXOIAKUNOVQU-UHFFFAOYSA-N 0.000 claims description 2
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- FZGVEKPRDOIXJY-UHFFFAOYSA-N bitolterol Chemical compound C1=CC(C)=CC=C1C(=O)OC1=CC=C(C(O)CNC(C)(C)C)C=C1OC(=O)C1=CC=C(C)C=C1 FZGVEKPRDOIXJY-UHFFFAOYSA-N 0.000 claims description 2
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- STJMRWALKKWQGH-UHFFFAOYSA-N clenbuterol Chemical compound CC(C)(C)NCC(O)C1=CC(Cl)=C(N)C(Cl)=C1 STJMRWALKKWQGH-UHFFFAOYSA-N 0.000 claims description 2
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- A61K9/007—Pulmonary tract; Aromatherapy
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- A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
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- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/0078—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Pulmonology (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyrrole Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19921693A DE19921693A1 (de) | 1999-05-12 | 1999-05-12 | Neuartige Arzneimittelkompositionen auf der Basis von anticholinergisch wirksamen Verbindungen und ß-Mimetika |
| PCT/EP2000/003943 WO2000069468A1 (fr) | 1999-05-12 | 2000-05-03 | Nouvelles compositions medicamenteuses a base de composes a action anticholinergique et de betamimetiques |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HRP20010828A2 true HRP20010828A2 (en) | 2003-02-28 |
| HRP20010828B1 HRP20010828B1 (fr) | 2013-01-31 |
Family
ID=7907709
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20010828A HRP20010828A2 (en) | 1999-05-12 | 2001-11-08 | Novel medicament compositions, based on anticholinergically effective compounds and beta-mimetics |
Country Status (41)
| Country | Link |
|---|---|
| US (3) | US6455524B1 (fr) |
| EP (7) | EP1570861A3 (fr) |
| JP (5) | JP4612956B2 (fr) |
| KR (2) | KR100962059B1 (fr) |
| CN (2) | CN1839833A (fr) |
| AR (1) | AR023972A1 (fr) |
| AT (1) | ATE245976T1 (fr) |
| AU (1) | AU775588B2 (fr) |
| BG (1) | BG65189B1 (fr) |
| BR (1) | BR0010498A (fr) |
| CA (1) | CA2368583C (fr) |
| CO (1) | CO5140068A1 (fr) |
| CZ (1) | CZ302328B6 (fr) |
| DE (2) | DE19921693A1 (fr) |
| DK (1) | DK1178832T3 (fr) |
| EA (1) | EA004657B1 (fr) |
| EE (4) | EE05193B1 (fr) |
| ES (1) | ES2203470T3 (fr) |
| HK (1) | HK1043064B (fr) |
| HR (1) | HRP20010828A2 (fr) |
| HU (1) | HUP0201103A3 (fr) |
| IL (3) | IL146119A0 (fr) |
| ME (1) | MEP36608A (fr) |
| MX (1) | MXPA01011400A (fr) |
| MY (2) | MY134222A (fr) |
| NO (2) | NO328423B1 (fr) |
| NZ (1) | NZ515596A (fr) |
| PE (1) | PE20010133A1 (fr) |
| PL (2) | PL199442B1 (fr) |
| PT (1) | PT1178832E (fr) |
| RS (2) | RS20090083A (fr) |
| SA (1) | SA00210064B1 (fr) |
| SG (4) | SG175465A1 (fr) |
| SI (1) | SI1178832T1 (fr) |
| SK (1) | SK287072B6 (fr) |
| TR (2) | TR200103233T2 (fr) |
| TW (2) | TW200505483A (fr) |
| UA (1) | UA74547C2 (fr) |
| UY (1) | UY26139A1 (fr) |
| WO (1) | WO2000069468A1 (fr) |
| ZA (1) | ZA200108942B (fr) |
Families Citing this family (107)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030215396A1 (en) * | 1999-09-15 | 2003-11-20 | Boehringer Ingelheim Pharma Kg | Method for the production of propellant gas-free aerosols from aqueous medicament preparations |
| DE19653969A1 (de) * | 1996-12-20 | 1998-06-25 | Boehringer Ingelheim Kg | Neue wässrige Arzneimittelzubereitung zur Erzeugung treibgasfreier Aerosole |
| GB9902689D0 (en) * | 1999-02-08 | 1999-03-31 | Novartis Ag | Organic compounds |
| DE19921693A1 (de) * | 1999-05-12 | 2000-11-16 | Boehringer Ingelheim Pharma | Neuartige Arzneimittelkompositionen auf der Basis von anticholinergisch wirksamen Verbindungen und ß-Mimetika |
| US20040002548A1 (en) * | 1999-05-12 | 2004-01-01 | Boehringer Ingelheim Pharma Kg | Medicament compositions containing anticholinergically-effective compounds and betamimetics |
| US20100197719A1 (en) * | 1999-05-12 | 2010-08-05 | Boehringer Ingelheim Pharma Kg | Medicament compositions containing anticholinergically-effective compounds and betamimetics |
| ES2165768B1 (es) | 1999-07-14 | 2003-04-01 | Almirall Prodesfarma Sa | Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen. |
| US7214687B2 (en) | 1999-07-14 | 2007-05-08 | Almirall Ag | Quinuclidine derivatives and medicinal compositions containing the same |
| WO2002026223A2 (fr) * | 2000-09-29 | 2002-04-04 | Board Of Trustees Operating Michigan State University | Preparations pharmaceutiques de catecholamine et procedes |
| US20020137764A1 (en) * | 2000-10-31 | 2002-09-26 | Karin Drechsel | Inhalable formulation of a solution containing a tiotropium salt |
| DE10206505A1 (de) * | 2002-02-16 | 2003-08-28 | Boehringer Ingelheim Pharma | Neue Arzneimittelkompositionen auf der Basis von Anticholinergika und EGFR-Kinase-Hemmern |
| US7776315B2 (en) * | 2000-10-31 | 2010-08-17 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pharmaceutical compositions based on anticholinergics and additional active ingredients |
| US6620438B2 (en) * | 2001-03-08 | 2003-09-16 | Boehringer Ingelheim Pharma Kg | Pharmaceutical compositions based on anticholinergics and NK1-receptor antagonists |
| US6608054B2 (en) * | 2001-03-20 | 2003-08-19 | Boehringer Ingelheim Pharma Kg | Pharmaceutical compositions based on anticholinergics and endothelin antagonists |
| US20020111363A1 (en) * | 2000-10-31 | 2002-08-15 | Karin Drechsel | Inhalable formulation of a solution containing a tiotropium salt |
| US20020193392A1 (en) * | 2000-11-13 | 2002-12-19 | Christel Schmelzer | Pharmaceutical compositions based on tiotropium salts of salts of salmeterol |
| DE10056104A1 (de) * | 2000-11-13 | 2002-05-23 | Boehringer Ingelheim Pharma | Neue Arzneimittelkompositionen auf der Basis von Tiotropiumsalzen und Salzen des Salmeterols |
| US20100310477A1 (en) * | 2000-11-28 | 2010-12-09 | Boehringer Ingelheim Pharma Gmbh & Co. Kg. | Pharmaceutical compositions based on anticholingerics and additional active ingredients |
| US6667344B2 (en) * | 2001-04-17 | 2003-12-23 | Dey, L.P. | Bronchodilating compositions and methods |
| AU2002303425A1 (en) * | 2001-04-24 | 2002-11-05 | Epigenesis Pharmaceuticals, Inc. | Composition, formulations and kit for treatment of respiratory and lung disease with non-glucocorticoid steroids and/or ubiquinone and a bronchodilating agent |
| DE10126924A1 (de) * | 2001-06-01 | 2002-12-05 | Boehringer Ingelheim Pharma | Inhalationskapseln |
| US20030018019A1 (en) * | 2001-06-23 | 2003-01-23 | Boehringer Ingelheim Pharma Kg | Pharmaceutical compositions based on anticholinergics, corticosteroids and betamimetics |
| US20040244794A1 (en) * | 2001-08-09 | 2004-12-09 | Richards David Hugh | Inhalation device with a pharmaceutical composition |
| US6919325B2 (en) | 2001-09-14 | 2005-07-19 | Boehringer Ingelheim Pharma Kg | Pharmaceutical compositions containing tiotropium salts and low-solubility salmeterol salts |
| EP1429768B1 (fr) * | 2001-09-14 | 2016-11-16 | Boehringer Ingelheim Pharma GmbH & Co.KG | Agents pharmaceutiques d'inhalation |
| US7754242B2 (en) * | 2002-03-20 | 2010-07-13 | Alkermes, Inc. | Inhalable sustained therapeutic formulations |
| DE10212264A1 (de) † | 2002-03-20 | 2003-10-02 | Boehringer Ingelheim Pharma | Kristallines Mikronisat, Verfahren zu dessen Herstellung und dessen Verwendung zur Herstellung eines Arzneimittels |
| US7309707B2 (en) * | 2002-03-20 | 2007-12-18 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Crystalline micronisate, process for the manufacture thereof and use thereof for the preparation of a medicament |
| DE10214263A1 (de) * | 2002-03-28 | 2003-10-16 | Boehringer Ingelheim Pharma | HFA-Suspensionsformulierungen enthaltend ein Anticholinergikum |
| US7244415B2 (en) * | 2002-03-28 | 2007-07-17 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | HFA suspension formulations of an anhydrate |
| EP1494648B1 (fr) * | 2002-04-04 | 2006-09-20 | Boehringer Ingelheim Pharma GmbH & Co.KG | Preparations en poudre pour inhalation |
| UA80123C2 (en) * | 2002-04-09 | 2007-08-27 | Boehringer Ingelheim Pharma | Inhalation kit comprising inhalable powder of tiotropium |
| US20030225089A1 (en) * | 2002-04-10 | 2003-12-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pharmaceutical compositions based on anticholinergics and p38 kinase inhibitors |
| DE10216427A1 (de) * | 2002-04-12 | 2003-10-23 | Boehringer Ingelheim Pharma | Arzneimittelkompositionen enthaltend heterocyclische Verbindungen und ein neues Anticholinergikum |
| US7084153B2 (en) * | 2002-04-12 | 2006-08-01 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Medicaments comprising steroids and a novel anticholinergic |
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