JP5763053B2 - アダプタ、吸入器具及びアトマイザ - Google Patents
アダプタ、吸入器具及びアトマイザ Download PDFInfo
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- JP5763053B2 JP5763053B2 JP2012511164A JP2012511164A JP5763053B2 JP 5763053 B2 JP5763053 B2 JP 5763053B2 JP 2012511164 A JP2012511164 A JP 2012511164A JP 2012511164 A JP2012511164 A JP 2012511164A JP 5763053 B2 JP5763053 B2 JP 5763053B2
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- JP
- Japan
- Prior art keywords
- adapter
- nebulizer
- amino
- phenyl
- quinazoline
- Prior art date
- Legal status (The legal status 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 status listed.)
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- 239000006199 nebulizer Substances 0.000 claims description 107
- 239000000443 aerosol Substances 0.000 claims description 52
- 230000000241 respiratory effect Effects 0.000 claims description 10
- 230000008878 coupling Effects 0.000 claims description 6
- 238000010168 coupling process Methods 0.000 claims description 6
- 238000005859 coupling reaction Methods 0.000 claims description 6
- 238000002347 injection Methods 0.000 claims description 2
- 239000007924 injection Substances 0.000 claims description 2
- -1 and is a betamimetic Substances 0.000 description 114
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 103
- 239000003570 air Substances 0.000 description 59
- 150000001875 compounds Chemical class 0.000 description 26
- 150000003839 salts Chemical class 0.000 description 22
- 239000000825 pharmaceutical preparation Substances 0.000 description 15
- 239000008194 pharmaceutical composition Substances 0.000 description 14
- 239000002253 acid Substances 0.000 description 13
- 238000009423 ventilation Methods 0.000 description 13
- 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 description 10
- 230000003454 betamimetic effect Effects 0.000 description 10
- 230000029058 respiratory gaseous exchange Effects 0.000 description 10
- 239000005557 antagonist Substances 0.000 description 9
- 238000013461 design Methods 0.000 description 9
- 239000000243 solution Substances 0.000 description 9
- 150000004677 hydrates Chemical class 0.000 description 8
- 238000000034 method Methods 0.000 description 8
- 239000012453 solvate Substances 0.000 description 8
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 7
- 238000000889 atomisation Methods 0.000 description 7
- 229940121647 egfr inhibitor Drugs 0.000 description 7
- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 description 6
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical group Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 6
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 description 6
- 239000012530 fluid Substances 0.000 description 6
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 description 6
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 description 6
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 5
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 5
- JZUFKLXOESDKRF-UHFFFAOYSA-N Chlorothiazide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NCNS2(=O)=O JZUFKLXOESDKRF-UHFFFAOYSA-N 0.000 description 5
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 5
- 150000001450 anions Chemical class 0.000 description 5
- 239000002585 base Substances 0.000 description 5
- 150000003842 bromide salts Chemical class 0.000 description 5
- 239000000812 cholinergic antagonist Substances 0.000 description 5
- 239000003246 corticosteroid Substances 0.000 description 5
- 238000012432 intermediate storage Methods 0.000 description 5
- 238000002663 nebulization Methods 0.000 description 5
- 230000008569 process Effects 0.000 description 5
- 239000000126 substance Substances 0.000 description 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 4
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 description 4
- 229910019142 PO4 Inorganic materials 0.000 description 4
- 230000009471 action Effects 0.000 description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 4
- 235000021317 phosphate Nutrition 0.000 description 4
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 4
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 4
- ODELFXJUOVNEFZ-UHFFFAOYSA-N 2,2-diphenylpropanoic acid Chemical compound C=1C=CC=CC=1C(C(O)=O)(C)C1=CC=CC=C1 ODELFXJUOVNEFZ-UHFFFAOYSA-N 0.000 description 3
- GXAMYUGOODKVRM-UHFFFAOYSA-M 9-hydroxyfluorene-9-carboxylate Chemical compound C1=CC=C2C(O)(C([O-])=O)C3=CC=CC=C3C2=C1 GXAMYUGOODKVRM-UHFFFAOYSA-M 0.000 description 3
- DTZDZCNXNYMMOW-UHFFFAOYSA-N 9-hydroxyxanthene-9-carboxylic acid Chemical compound C1=CC=C2C(C(=O)O)(O)C3=CC=CC=C3OC2=C1 DTZDZCNXNYMMOW-UHFFFAOYSA-N 0.000 description 3
- PUPWRKQSVGUBQS-UHFFFAOYSA-N 9-methylfluorene-9-carboxylic acid Chemical compound C1=CC=C2C(C)(C(O)=O)C3=CC=CC=C3C2=C1 PUPWRKQSVGUBQS-UHFFFAOYSA-N 0.000 description 3
- CBNOKZSYCBHRAD-UHFFFAOYSA-N 9-methylxanthene-9-carboxylic acid Chemical compound C1=CC=C2C(C)(C(O)=O)C3=CC=CC=C3OC2=C1 CBNOKZSYCBHRAD-UHFFFAOYSA-N 0.000 description 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 3
- 238000010276 construction Methods 0.000 description 3
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 description 3
- 230000035515 penetration Effects 0.000 description 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 3
- 239000010452 phosphate Substances 0.000 description 3
- 239000002699 waste material Substances 0.000 description 3
- ULMFXAMQUGLVGA-LJQANCHMSA-N 3-[[2-methoxy-4-[(2-methylphenyl)sulfonylcarbamoyl]phenyl]methyl]-1-methyl-n-[(2r)-4,4,4-trifluoro-2-methylbutyl]indole-5-carboxamide Chemical compound C=1C=C(CC=2C3=CC(=CC=C3N(C)C=2)C(=O)NC[C@H](C)CC(F)(F)F)C(OC)=CC=1C(=O)NS(=O)(=O)C1=CC=CC=C1C ULMFXAMQUGLVGA-LJQANCHMSA-N 0.000 description 2
- CVDXFPBVOIERBH-JWQCQUIFSA-N 4-[(4ar,10bs)-9-ethoxy-8-methoxy-2-methyl-3,4,4a,10b-tetrahydro-1h-benzo[c][1,6]naphthyridin-6-yl]-n,n-di(propan-2-yl)benzamide Chemical compound N([C@@H]1CCN(C)C[C@@H]1C=1C=C(C(=CC=11)OC)OCC)=C1C1=CC=C(C(=O)N(C(C)C)C(C)C)C=C1 CVDXFPBVOIERBH-JWQCQUIFSA-N 0.000 description 2
- BHEFSGMUMYBJRZ-UHFFFAOYSA-N 9-fluorofluorene-9-carboxylic acid Chemical compound C1=CC=C2C(C(=O)O)(F)C3=CC=CC=C3C2=C1 BHEFSGMUMYBJRZ-UHFFFAOYSA-N 0.000 description 2
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 2
- KRHYYFGTRYWZRS-UHFFFAOYSA-M Fluoride anion Chemical compound [F-] KRHYYFGTRYWZRS-UHFFFAOYSA-M 0.000 description 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
- 229910002651 NO3 Inorganic materials 0.000 description 2
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 description 2
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 description 2
- 239000000808 adrenergic beta-agonist Substances 0.000 description 2
- 229910052783 alkali metal Inorganic materials 0.000 description 2
- 150000001340 alkali metals Chemical class 0.000 description 2
- 150000003797 alkaloid derivatives Chemical class 0.000 description 2
- 229940125715 antihistaminic agent Drugs 0.000 description 2
- 239000000739 antihistaminic agent Substances 0.000 description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 2
- 230000000903 blocking effect Effects 0.000 description 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 2
- 229960001334 corticosteroids Drugs 0.000 description 2
- JXTHNDFMNIQAHM-UHFFFAOYSA-N dichloroacetic acid Chemical compound OC(=O)C(Cl)Cl JXTHNDFMNIQAHM-UHFFFAOYSA-N 0.000 description 2
- 239000003136 dopamine receptor stimulating agent Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 238000003780 insertion Methods 0.000 description 2
- 230000037431 insertion Effects 0.000 description 2
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 2
- 239000003595 mist Substances 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- DPHDSIQHVGSITN-UHFFFAOYSA-N n-(3,5-dichloropyridin-4-yl)-2-[1-[(4-fluorophenyl)methyl]-5-hydroxyindol-3-yl]-2-oxoacetamide Chemical compound C1=C(C(=O)C(=O)NC=2C(=CN=CC=2Cl)Cl)C2=CC(O)=CC=C2N1CC1=CC=C(F)C=C1 DPHDSIQHVGSITN-UHFFFAOYSA-N 0.000 description 2
- 238000001556 precipitation Methods 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 239000003380 propellant Substances 0.000 description 2
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 description 2
- 125000006850 spacer group Chemical group 0.000 description 2
- 239000007921 spray Substances 0.000 description 2
- 150000003431 steroids Chemical class 0.000 description 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 2
- 229940095064 tartrate Drugs 0.000 description 2
- ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 description 2
- 238000013022 venting Methods 0.000 description 2
- JWZZKOKVBUJMES-UHFFFAOYSA-N (+-)-Isoprenaline Chemical compound CC(C)NCC(O)C1=CC=C(O)C(O)=C1 JWZZKOKVBUJMES-UHFFFAOYSA-N 0.000 description 1
- XWTYSIMOBUGWOL-UHFFFAOYSA-N (+-)-Terbutaline Chemical compound CC(C)(C)NCC(O)C1=CC(O)=CC(O)=C1 XWTYSIMOBUGWOL-UHFFFAOYSA-N 0.000 description 1
- NDAUXUAQIAJITI-LBPRGKRZSA-N (R)-salbutamol Chemical compound CC(C)(C)NC[C@H](O)C1=CC=C(O)C(CO)=C1 NDAUXUAQIAJITI-LBPRGKRZSA-N 0.000 description 1
- VSOSXKMEQPYESP-UHFFFAOYSA-N 1,6-naphthyridine Chemical compound C1=CN=CC2=CC=CN=C21 VSOSXKMEQPYESP-UHFFFAOYSA-N 0.000 description 1
- AOPATQAZIRXNOX-UHFFFAOYSA-N 2-(1-methylcyclopropyl)acetic acid Chemical compound OC(=O)CC1(C)CC1 AOPATQAZIRXNOX-UHFFFAOYSA-N 0.000 description 1
- SPCKHVPPRJWQRZ-UHFFFAOYSA-N 2-benzhydryloxy-n,n-dimethylethanamine;2-hydroxypropane-1,2,3-tricarboxylic acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 SPCKHVPPRJWQRZ-UHFFFAOYSA-N 0.000 description 1
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- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 description 1
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- 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 description 1
- PGXRCDQAQVJKHT-UHFFFAOYSA-N 5-thiophen-2-yl-3,4,6,11,12-pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,10-pentaene Chemical compound C1=CSC(C=2N3C=CC=4C=NNC=4C3=NN=2)=C1 PGXRCDQAQVJKHT-UHFFFAOYSA-N 0.000 description 1
- DHSSDEDRBUKTQY-UHFFFAOYSA-N 6-prop-2-enyl-4,5,7,8-tetrahydrothiazolo[4,5-d]azepin-2-amine Chemical compound C1CN(CC=C)CCC2=C1N=C(N)S2 DHSSDEDRBUKTQY-UHFFFAOYSA-N 0.000 description 1
- PYUGFOWNYMLROI-KPKJPENVSA-N 8-[(e)-2-[4-[4-(4-fluorophenyl)butoxy]phenyl]ethenyl]-2-(2h-tetrazol-5-yl)chromen-4-one Chemical compound C1=CC(F)=CC=C1CCCCOC(C=C1)=CC=C1\C=C\C1=CC=CC2=C1OC(C=1NN=NN=1)=CC2=O PYUGFOWNYMLROI-KPKJPENVSA-N 0.000 description 1
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- 229950001879 salmefamol Drugs 0.000 description 1
- 229960004017 salmeterol Drugs 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 229940124818 soft mist inhaler Drugs 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 229950010289 soterenol Drugs 0.000 description 1
- 125000000446 sulfanediyl group Chemical group *S* 0.000 description 1
- HGKLFYLYWZXWPO-UHFFFAOYSA-N sulfo benzoate Chemical compound OS(=O)(=O)OC(=O)C1=CC=CC=C1 HGKLFYLYWZXWPO-UHFFFAOYSA-N 0.000 description 1
- 229950007862 sulfonterol Drugs 0.000 description 1
- 229950008418 talipexole Drugs 0.000 description 1
- 229960000195 terbutaline Drugs 0.000 description 1
- 229960004558 terguride Drugs 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 125000004192 tetrahydrofuran-2-yl group Chemical group [H]C1([H])OC([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 229960000278 theophylline Drugs 0.000 description 1
- 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 description 1
- OOGJQPCLVADCPB-HXUWFJFHSA-N tolterodine Chemical compound C1([C@@H](CCN(C(C)C)C(C)C)C=2C(=CC=C(C)C=2)O)=CC=CC=C1 OOGJQPCLVADCPB-HXUWFJFHSA-N 0.000 description 1
- 229960004045 tolterodine Drugs 0.000 description 1
- 229960000575 trastuzumab Drugs 0.000 description 1
- 229960005294 triamcinolone Drugs 0.000 description 1
- GFNANZIMVAIWHM-OBYCQNJPSA-N triamcinolone Chemical compound O=C1C=C[C@]2(C)[C@@]3(F)[C@@H](O)C[C@](C)([C@@]([C@H](O)C4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 GFNANZIMVAIWHM-OBYCQNJPSA-N 0.000 description 1
- OYYDSUSKLWTMMQ-JKHIJQBDSA-N trospium Chemical class [N+]12([C@@H]3CC[C@H]2C[C@H](C3)OC(=O)C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CCCC1 OYYDSUSKLWTMMQ-JKHIJQBDSA-N 0.000 description 1
- BDIAUFOIMFAIPU-UHFFFAOYSA-N valepotriate Natural products CC(C)CC(=O)OC1C=C(C(=COC2OC(=O)CC(C)C)COC(C)=O)C2C11CO1 BDIAUFOIMFAIPU-UHFFFAOYSA-N 0.000 description 1
- 229960004764 zafirlukast Drugs 0.000 description 1
- XJSMBWUHHJFJFV-VTIMJTGVSA-N α-dihydroergocryptine Chemical compound C([C@H]1N(C)C2)C([C]34)=CN=C4C=CC=C3[C@H]1C[C@H]2C(=O)N[C@@]1(C(C)C)C(=O)N2[C@@H](CC(C)C)C(=O)N3CCC[C@H]3[C@]2(O)O1 XJSMBWUHHJFJFV-VTIMJTGVSA-N 0.000 description 1
Images
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M15/00—Inhalators
- A61M15/0086—Inhalation chambers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M11/00—Sprayers or atomisers specially adapted for therapeutic purposes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M11/00—Sprayers or atomisers specially adapted for therapeutic purposes
- A61M11/006—Sprayers or atomisers specially adapted for therapeutic purposes operated by applying mechanical pressure to the liquid to be sprayed or atomised
- A61M11/007—Syringe-type or piston-type sprayers or atomisers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M11/00—Sprayers or atomisers specially adapted for therapeutic purposes
- A61M11/06—Sprayers or atomisers specially adapted for therapeutic purposes of the injector type
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M15/00—Inhalators
- A61M15/0001—Details of inhalators; Constructional features thereof
- A61M15/0013—Details of inhalators; Constructional features thereof with inhalation check valves
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M15/00—Inhalators
- A61M15/0001—Details of inhalators; Constructional features thereof
- A61M15/0018—Details of inhalators; Constructional features thereof with exhalation check valves
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M15/00—Inhalators
- A61M15/0001—Details of inhalators; Constructional features thereof
- A61M15/0021—Mouthpieces therefor
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M15/00—Inhalators
- A61M15/0065—Inhalators with dosage or measuring devices
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M16/00—Devices for influencing the respiratory system of patients by gas treatment, e.g. mouth-to-mouth respiration; Tracheal tubes
- A61M16/08—Bellows; Connecting tubes ; Water traps; Patient circuits
- A61M16/0816—Joints or connectors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M16/00—Devices for influencing the respiratory system of patients by gas treatment, e.g. mouth-to-mouth respiration; Tracheal tubes
- A61M16/20—Valves specially adapted to medical respiratory devices
- A61M16/208—Non-controlled one-way valves, e.g. exhalation, check, pop-off non-rebreathing valves
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M16/00—Devices for influencing the respiratory system of patients by gas treatment, e.g. mouth-to-mouth respiration; Tracheal tubes
- A61M16/10—Preparation of respiratory gases or vapours
- A61M16/12—Preparation of respiratory gases or vapours by mixing different gases
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B05—SPRAYING OR ATOMISING IN GENERAL; APPLYING FLUENT MATERIALS TO SURFACES, IN GENERAL
- B05B—SPRAYING APPARATUS; ATOMISING APPARATUS; NOZZLES
- B05B11/00—Single-unit hand-held apparatus in which flow of contents is produced by the muscular force of the operator at the moment of use
- B05B11/01—Single-unit hand-held apparatus in which flow of contents is produced by the muscular force of the operator at the moment of use characterised by the means producing the flow
- B05B11/02—Membranes or pistons acting on the contents inside the container, e.g. follower pistons
- B05B11/026—Membranes separating the content remaining in the container from the atmospheric air to compensate underpressure inside the container
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B05—SPRAYING OR ATOMISING IN GENERAL; APPLYING FLUENT MATERIALS TO SURFACES, IN GENERAL
- B05B—SPRAYING APPARATUS; ATOMISING APPARATUS; NOZZLES
- B05B11/00—Single-unit hand-held apparatus in which flow of contents is produced by the muscular force of the operator at the moment of use
- B05B11/01—Single-unit hand-held apparatus in which flow of contents is produced by the muscular force of the operator at the moment of use characterised by the means producing the flow
- B05B11/10—Pump arrangements for transferring the contents from the container to a pump chamber by a sucking effect and forcing the contents out through the dispensing nozzle
- B05B11/1001—Piston pumps
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B05—SPRAYING OR ATOMISING IN GENERAL; APPLYING FLUENT MATERIALS TO SURFACES, IN GENERAL
- B05B—SPRAYING APPARATUS; ATOMISING APPARATUS; NOZZLES
- B05B11/00—Single-unit hand-held apparatus in which flow of contents is produced by the muscular force of the operator at the moment of use
- B05B11/01—Single-unit hand-held apparatus in which flow of contents is produced by the muscular force of the operator at the moment of use characterised by the means producing the flow
- B05B11/10—Pump arrangements for transferring the contents from the container to a pump chamber by a sucking effect and forcing the contents out through the dispensing nozzle
- B05B11/1042—Components or details
- B05B11/1066—Pump inlet valves
- B05B11/1067—Pump inlet valves actuated by pressure
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B05—SPRAYING OR ATOMISING IN GENERAL; APPLYING FLUENT MATERIALS TO SURFACES, IN GENERAL
- B05B—SPRAYING APPARATUS; ATOMISING APPARATUS; NOZZLES
- B05B11/00—Single-unit hand-held apparatus in which flow of contents is produced by the muscular force of the operator at the moment of use
- B05B11/01—Single-unit hand-held apparatus in which flow of contents is produced by the muscular force of the operator at the moment of use characterised by the means producing the flow
- B05B11/10—Pump arrangements for transferring the contents from the container to a pump chamber by a sucking effect and forcing the contents out through the dispensing nozzle
- B05B11/109—Pump arrangements for transferring the contents from the container to a pump chamber by a sucking effect and forcing the contents out through the dispensing nozzle the dispensing stroke being affected by the stored energy of a spring
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B05—SPRAYING OR ATOMISING IN GENERAL; APPLYING FLUENT MATERIALS TO SURFACES, IN GENERAL
- B05B—SPRAYING APPARATUS; ATOMISING APPARATUS; NOZZLES
- B05B11/00—Single-unit hand-held apparatus in which flow of contents is produced by the muscular force of the operator at the moment of use
- B05B11/01—Single-unit hand-held apparatus in which flow of contents is produced by the muscular force of the operator at the moment of use characterised by the means producing the flow
- B05B11/10—Pump arrangements for transferring the contents from the container to a pump chamber by a sucking effect and forcing the contents out through the dispensing nozzle
- B05B11/109—Pump arrangements for transferring the contents from the container to a pump chamber by a sucking effect and forcing the contents out through the dispensing nozzle the dispensing stroke being affected by the stored energy of a spring
- B05B11/1091—Pump arrangements for transferring the contents from the container to a pump chamber by a sucking effect and forcing the contents out through the dispensing nozzle the dispensing stroke being affected by the stored energy of a spring being first hold in a loaded state by locking means or the like, then released
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Anesthesiology (AREA)
- General Health & Medical Sciences (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pulmonology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Emergency Medicine (AREA)
- Mechanical Engineering (AREA)
- Biophysics (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Containers And Packaging Bodies Having A Special Means To Remove Contents (AREA)
Description
先の実施形態の場合と同様、吸入器具32は、アダプタ23を介してネブライザ1に取り付け可能である。しかしながら、吸入器具32の第1の連結部33は又、ネブライザ1又はマウスピース13に直接連結可能であるように構成されていても良い。所望ならば、アダプタ23又はそのオプションとしてのロック弁31を吸入器具32又はその連結部33に組み込んでも良い。特に、この場合、吸入器具32の第1の連結部33は、ネブライザ1又はそのマウスピース13に流体力学的に且つ/或いは機械的に連結可能であるように構成されている。
‐Wは、抗コリン作用薬、コルチコステロイド、PDE4‐阻害薬、EGFR‐阻害薬又はLTD4‐拮抗薬と組み合わされるベータミメティックを意味する。
‐Wは、ベータミメティック、コルチコステロイド、PDE4‐阻害薬、EGFR‐阻害薬又はLTD4‐拮抗薬と組み合わされる抗コリン作用薬を意味する。
‐Wは、PDE4‐阻害薬、EGFR‐阻害薬又はLTD4‐拮抗薬と組み合わされるコルチコステロイドを意味する。
‐Wは、EGFR‐阻害薬又はLTD4‐拮抗薬と組み合わされるPDE4‐阻害薬を意味する。
‐Wは、LTD4‐拮抗薬と組み合わされるEGFR‐阻害薬を意味する。
‐3‐(4‐{6‐[2‐ヒドロキシ‐2‐(4‐ヒドロキシ‐3‐ヒドロキシメチル‐フェニル)‐エチルアミノ]‐ヘキシロキシ}‐ブチル)‐ベンジル‐スルホナミド、
‐5‐[2‐(5,6‐ジエチル‐インダン‐2‐イルアミノ)‐1‐ヒドロキシ‐エチル]‐8‐ヒドロキシ‐1H‐キノリン‐2‐オン、
‐4‐ヒドロキシ‐7‐[2‐{[2‐{[3‐(2‐フェニルエトキシ)プロピル]スルホニル}エチル]‐アミノ}エチル]‐2(3H)‐ベンゾチアゾロン、
‐1‐(2‐フルオロ‐4‐ヒドロキシフェニル)‐2‐[4‐(1‐ベンジミダゾリル)‐2‐メチル‐2‐ブチルアミノ]エタノール、
‐1‐[3‐(4‐メトキシベンジル‐アミノ)‐4‐ヒドロキシフェニル]‐2‐[4‐(1‐ベンジミダゾリル)‐2‐メチル‐2‐ブチルアミノ]エタノール、
‐1‐[2H‐5‐ヒドロキシ‐3‐オキソ‐4H‐1,4‐ベンゾキサジン‐8‐イル]‐2‐[3‐(4‐N,N‐ジメチルアミノフェニル)‐2‐メチル‐2‐プロピルアミノ]エタノール、
‐1‐[2H‐5‐ヒドロキシ‐3‐オキソ‐4H‐1,4‐ベンゾキサジン‐8‐イル]‐2‐[3‐(4‐メトキシフェニル)‐2‐メチル‐2‐プロピルアミノ]エタノール、
‐1‐[2H‐5‐ヒドロキシ‐3‐オキソ‐4H‐1,4‐ベンゾキサジン‐8‐イル]‐2‐[3‐(4‐n‐ブチルオキシフェニル)‐2‐メチル‐2‐プロピルアミノ]エタノール、
‐1‐[2H‐5‐ヒドロキシ‐3‐オキソ‐4H‐1,4‐ベンゾキサジン8‐イル]‐2‐{4‐[3‐(4‐メトキシフェニル)‐1,2,4‐トリアゾル‐3‐イル]‐2‐メチル‐2‐ブチルアミノ}エタノール、
‐5‐ヒドロキシ‐8‐(1‐ヒドロキシ‐2‐イソプロピルアミノブチル)‐2H‐1,4‐ベンゾキサジン‐3‐(4H)‐オン、
‐1‐(4‐アミノ‐3‐クロロ‐5‐トリフルオロメチルフェニル)‐2‐t‐ブチルアミノ)エタノール、
‐6‐ヒドロキシ‐8‐{1‐ヒドロキシ‐2‐[2‐(4‐メトキシ‐フェニル)‐1,1‐ジメチル‐エチルアミノ]‐エチル}‐4H‐ベンゾ[1,4]オキサジン‐3‐オン、
‐6‐ヒドロキシ‐8‐{1‐ヒドロキシ‐2‐[2‐(エチル4‐フェノキシ‐アセテート)‐1,1‐ジメチル‐エチルアミノ]‐エチル}‐4H‐ベンゾ[1,4]オキサジン‐3‐オン、
‐6‐ヒドロキシ‐8‐{1‐ヒドロキシ‐2‐[2‐(4‐フェノキシ‐酢酸)‐1,1‐ジメチル‐エチルアミノ]‐エチル}‐4H‐ベンゾ[1,4]オキサジン‐3‐オン、
‐8‐{2‐[1,1‐ジメチル‐2‐(2,4,6‐トリメチルフェニル)‐エチルアミノ]‐1‐ヒドロキシ‐エチル}‐6‐ヒドロキシ‐4H‐ベンゾ[1,4]オキサジン‐3‐オン、
‐6‐ヒドロキシ‐8‐{1‐ヒドロキシ‐2‐[2‐(4‐ヒドロキシ‐フェニル)‐1,1‐ジメチル‐エチルアミノ]‐エチル}‐4H‐ベンゾ[1,4]オキサジン‐3‐オン、
‐6‐ヒドロキシ‐8‐{1‐ヒドロキシ‐2‐[2‐(4‐イソプロピル‐フェニル)‐1,1‐ジメチル‐エチルアミノ]‐エチル}‐4H‐ベンゾ[1,4]オキサジン‐3‐オン、
‐8‐{2‐[2‐(4‐エチル‐フェニル)‐1,1‐ジメチル‐エチルアミノ]‐1‐ヒドロキシ‐エチル}‐6‐ヒドロキシ‐4H‐ベンゾ[1,4]オキサジン‐3‐オン、
‐8‐{2‐[2‐(4‐エトキシ‐フェニル)‐1,1‐ジメチル‐エチルアミノ]‐1‐ヒドロキシ‐エチル}‐6‐ヒドロキシ‐4H‐ベンゾ[1,4]オキサジン‐3‐オン、
‐4‐(4‐{2‐[2‐ヒドロキシ‐2‐(6‐ヒドロキシ‐3‐オキソ‐3,4‐ジヒドロ‐2H‐ベンゾ[1,4]オキサジン‐8‐イル)‐エチルアミノ]‐2‐メチル‐プロピル}‐フェノキシ)‐酪酸、
‐8‐{2‐[2‐(3,4‐ジフルオロ‐フェニル)‐1,1‐ジメチル‐エチルアミノ]‐1‐ヒドロキシ‐エチル}‐6‐ヒドロキシ‐4H‐ベンゾ[1,4]オキサジン‐3‐オン、
‐1‐(4‐エトキシ‐カルボニルアミノ‐3‐シアノ‐5‐フルオロフェニル)‐2‐(t‐ブチルアミノ)エタノール、
‐2‐ヒドロキシ‐5‐(1‐ヒドロキシ‐2‐{2‐[4‐(2‐ヒドロキシ‐2‐フェニル‐エチルアミノ)‐フェニル]‐エチルアミノ}‐エチル)‐ベンズアルデヒド、
‐N‐[2‐ヒドロキシ‐5‐(1‐ヒドロキシ‐2‐{2‐[4‐(2‐ヒドロキシ‐2‐フェニル‐エチルアミノ)‐フェニル]‐エチルアミノ}‐エチル)‐フェニル]‐ホルムアミド、
‐8‐ヒドロキシ‐5‐(1‐ヒドロキシ‐2‐{2‐[4‐(6‐メトキシ‐ビフェニル‐3‐イルアミノ)‐フェニル]‐エチルアミノ}‐エチル)‐1H‐キノリン‐2‐オン、
‐8‐ヒドロキシ‐5‐(1‐ヒドロキシ‐2‐(6‐フェネチルアミノ‐ヘキシルアミノ)‐エチル)‐1H‐キノリン‐2‐オン、
‐5‐[2‐(2‐{4‐[4‐(2‐アミノ‐2‐メチル‐プロポキシ)‐フェニルアミノ]‐フェニル}‐エチルアミノ)‐1‐ヒドロキシ‐エチル]‐8‐ヒドロキシ‐1H‐キノリン‐2‐オン、
‐[3‐(4‐{6‐[2‐ヒドロキシ‐2‐(4‐ヒドロキシ‐3‐ヒドロキシメチル‐フェニル)‐エチルアミノ]‐ヘキシルオキシ}‐ブチル)‐5‐メチル‐フェニル]‐ウレア、
‐4‐(2‐{6‐[2‐(2,6‐ジクロロ‐ベンジルオキソ)‐エトキシ]‐ヘキシルアミノ}‐1‐ヒドロキシ‐エチル)‐2‐ヒドロキシメチル‐フェノール、
‐3‐(4‐{6‐[2‐ヒドロキシ‐2‐(4‐ヒドロキシ‐3‐ヒドロキシメチル‐フェニル)‐エチルアミノ]‐ヘキシルオキシ}‐ブチル)‐ベンジルスルホンアミド、
‐3‐(3‐{7‐[2‐ヒドロキシ‐2‐(4‐ヒドロキシ‐3‐ヒドロキシメチル‐フェニル)‐エチルアミノ]‐ヘプチルオキシ}‐プロピル)‐ベンジルスルホンアミド、
‐4‐(2‐{6‐[4‐(3‐シクロペンタンスルホニル‐フェニル)‐ブトキシ]‐ヘキシルアミノ}‐1‐ヒドロキシ‐エチル)‐2‐ヒドロキシメチル‐フェノール、
‐N‐アダマンタン‐2‐イル‐2‐(3‐{2‐[2‐ヒドロキシ‐2‐(4‐ヒドロキシ‐3‐ヒドロキシメチル‐フェニル)‐エチルアミノ]‐プロピル}‐フェニル)‐アセトアミドの中から選択された化合物であり、
オプションとして上記化合物のラセミ化合物、エナンチオマー又はジアステレオマー及びオプションとして上記化合物の薬理学的に容認できる酸添加塩、溶媒化合物又は水和物である。本発明によれば、ベータミメティックの酸添加塩は、好ましくは、ヒドロクロリド(塩酸塩)、ヒドロブロミド(臭化水素酸塩)、ヒドロイオジド(沃化水素酸塩)、ヒドロスルフェート、ヒドロホスフェート、ヒドロメタンスルホネート、ヒドロニトレート、ヒドロマレエート、ヒドロアセテート、ヒドロシトレート、ヒドロフマレート、ヒドロタルトレート、ヒドロオキサレート、ヒドロスクシネート、ヒドロベンゾエート及びヒドロ‐p‐トルエンスルホネートの中から選択される。
‐トロペノール2,2‐ジフェニルプロピオネートメトブロミド、
‐スコピン2,2‐ジフェニルプロピオネートメトブロミド、
‐スコピン2,2‐フルオロ‐2,2‐ジフェニルアセテートメトブロミド、
‐トロペノール2‐フルオロ‐2,2‐ジフェニルアセテートメトブロミド、
‐トロペノール3,3′,4,4′‐テトラフルオロベンジレートメトブロミド、
‐スコピン3,3′,4,4′‐テトラフルオロベンジレートメトブロミド、
‐トロペノール4,4′‐ジフルオロベンジレートメトブロミド、
‐スコピン4,4′‐ジフルオロベンジレートメトブロミド、
‐トロペノール3,3′‐ジフルオロベンジレートメトブロミド、
‐スコピン3,3′‐ジフルオロベンジレートメトブロミド、
‐トロペノール9‐ヒドロキシ‐フルオレン‐9‐カルボキシレートメトブロミド、
‐トロペノール9‐フルオロ‐フルオレン‐9‐カルボキシレートメトブロミド、
‐スコピン9‐ヒドロキシ‐フルオレン‐9‐カルボキシレートメトブロミド、
‐スコピン9‐フルオロ‐フルオレン‐9‐カルボキシレートメトブロミド、
‐トロペノール9‐メチル‐フルオレン‐9‐カルボキシレートメトブロミド、
‐スコピン9‐メチル‐フルオレン‐9‐カルボキシレートメトブロミド、
‐シクロプロピルトロピンベンジレートメトブロミド、
‐シクロプロピルトロピン2,2‐ジフェニルプロピオネートメトブロミド、
‐シクロプロピルトロピン9‐ヒドロキシ‐キサンテン‐9‐カルボキシレートメトブロミド、
‐シクロプロピルトロピン9‐メチル‐フルオレン‐9‐カルボキシレートメトブロミド、
‐シクロプロピルトロピン9‐メチル‐キサンテン‐9‐カルボキシレートメトブロミド、
‐シクロプロピルトロピン9‐ヒドロキシ‐フルオレン‐9‐カルボキシレートメトブロミド、
‐シクロプロピルトロピンメチル4,4′‐ジフルオロベンジレートメトブロミド、
‐トロペノール9‐ヒドロキシ‐キサンテン‐9‐カルボキシレートメトブロミド、
‐スコピン9‐ヒドロキシ‐キサンテン‐9‐カルボキシレートメトブロミド、
‐トロペノール9‐メチル‐キサンテン‐9‐カルボキシレートメトブロミド、
‐スコピン9‐メチル‐キサンテン‐9‐カルボキシレートメトブロミド、
‐トロペノール9‐エチル‐キサンテン‐9‐カルボキシレートメトブロミド、
‐トロペノール9‐ジフルオロメチル‐キサンテン‐9‐カルボキシレートメトブロミド、
‐スコピン9‐ヒドロキシメチル‐キサンテン‐9‐カルボキシレートメトブロミド。
‐(S)‐フルオロメチル 6,9‐ジフルオロ‐17‐[(2‐フラニルカルボニル)オキシ]‐11‐ヒドロキシ‐16‐メチル‐3‐オキソ‐アンドロスタ‐1,4‐ジエン‐17‐カルボチオネート、
‐(S)‐(2‐オキソ‐テトラヒドロ‐フラン‐3S‐イル)6,9‐ジフルオロ‐11‐ヒドロキシ‐16‐メチル‐3‐オキソ‐17‐プロピオニルオキシ‐アンドロスタ‐1,4‐ジエン‐17‐カルボチオネート、
‐シアオメチル 6α,9α‐ジフルオロ‐11β‐ヒドロキシ‐16α‐メチル‐3‐オキソ‐17α‐(2,2,3,3‐テトラメチルシクロプロピルカルボニル)オキシ‐アンドロスタ‐1,4‐ジエン‐17β‐カルボン酸シアノメチルエステルの中から選択された化合物を用いることが好ましく、
オプションとして上記化合物のラセミ化合物、エナンチオマー又はジアステレオマー及びオプションとして上記化合物の薬理学的に容認できる塩及びその誘導体、溶媒化合物及び/又は水和物が用いられる。ステロイドと言った場合、これは、存在し得るステロイドの塩又はその誘導体、水和物又は溶媒化合物を含む。考えられるステロイドの塩及びその誘導体の例は、アルカリ金属、例えばナトリウム塩、カリウム塩、スルホベンゾエート、ホスフェート、イソニコチネート、アセテート、ジクロロアセテート、プロピオネート、ジヒドロゲンホスフェート、パルミテート、ピバレート又はフロエートである。
‐N‐(3,5‐ジクロロ‐1‐オキソ‐ピリジン‐4‐イル)‐4‐ジフルオロメトキシ‐3‐シクロプロピルメトキシベンザミド、
‐(‐)p‐[(4aR*,10bS*)‐9‐エトキシ‐1,2,3,4,4a,10b‐ヘキサヒドロ‐8‐メトキシ‐2‐メチルベンゾ[s][1,6]ナフチリジン‐6‐イル]‐N,N‐ジイソプロピルベンザミド、
‐(R)‐(+)‐1‐(4‐ブロモベンジル)‐4‐[(3‐シクロペンチルオキシ)‐4‐メトキシフェニル]‐2‐ピロリドン、
‐3‐(シクロペンチルオキシ‐4‐メトキシフェニル)‐1‐(4‐N′‐[N‐2‐シアノ‐S‐メチル‐イソチオウレイド]ベンジル)‐2‐ピロリドン、
‐シス[4‐シアノ‐4‐(3‐シクロペンチルオキシ‐4‐メトキシフェニル)シクロヘキサン‐1‐カルボン酸]、
‐2‐カルボメトキシ‐4‐シアノ‐4‐(3‐シクロプロピルメトキシ‐4‐ジフルオロメトキシフェニル)シクロヘキサン‐1‐オン、
‐シス[4‐シアノ‐4‐(3‐シクロプロピルメトキシ‐4‐ジフルオロメトキシフェニル)シクロヘキサン‐1‐オル]、
‐(R)‐(+)‐エチル[4‐(3‐シクロペンチルオキシ‐4‐メトキシフェニル)ピロリジン‐2‐イリデン]アセテート、
‐(S)‐(‐)‐エチル[4‐(3‐シクロペンチルオキシ‐4‐メトキシフェニル)ピロリジン‐2‐イリデン]アセテート、
‐9‐シクロペンチル‐5,6‐ジヒドロ‐7‐エチル‐3(2‐チエニル)‐9H‐ピラゾロ[3,4‐c]‐1,2,4‐トリアゾロ[4,3‐a]ピリジン、
‐9‐シクロペンチル‐5,6‐ジヒドロ‐7‐エチル‐3‐(t‐ブチル)‐9H‐ピラゾロ[3,4‐c]‐1,2,4‐トリアゾロ[4,3‐a]ピリジンの中から選択された化合物であり、
オプションとして上記化合物のラセミ化合物、エナンチオマー又はジアステレオマー及びオプションとして上記化合物の薬理学的に容認できる酸添加塩、溶媒化合物及び/又は水和物である。本発明によれば、ベータミメティックの酸添加塩は、好ましくは、ヒドロクロリド、ヒドロブロミド、ヒドロイオジド、ヒドロスルフェート、ヒドロホスフェート、ヒドロメタンスルホネート、ヒドロニトレート、ヒドロマレエート、ヒドロアセテート、ヒドロシトレート、ヒドロフマレート、ヒドロタルトレート、ヒドロオキサレート、ヒドロスクシネート、ヒドロベンゾエート及びヒドロ‐p‐トルエンスルホネートの中から選択される。
‐1‐(((R)‐(3‐(2‐(6,7‐ジフルオロ‐2‐キノリニル)エテニル)フェニル)‐3‐(2‐(2‐ヒドロキシ‐2‐プロピル)フェニル)チオ)メチルシクロプロパン‐酢酸、
‐1‐(((1(R)‐3(3‐(2‐(2,3‐ジクロロチエノ[3,2‐b]ピリジン‐5‐イル)‐(E)‐エテニル)フェニル)‐3‐(2‐(1‐ヒドロキシ‐1‐メチレチル)フェニル)プロピル)チオ)メチル)シクロプロパン‐酢酸、
‐[2‐[[2‐(4‐t‐ブチル‐2‐チアゾリル)‐5‐ベンゾフラニル]オキシメチル]フェニル]酢酸の中から選択された化合物であり、
オプションとして上記化合物のラセミ化合物、エナンチオマー又はジアステレオマー及びオプションとして上記化合物の薬理学的に容認できる酸添加塩、溶媒化合物及び/又は水和物である。本発明によれば、ベータミメティックの酸添加塩は、好ましくは、ヒドロクロリド、ヒドロブロミド、ヒドロイオジド、ヒドロスルフェート、ヒドロホスフェート、ヒドロメタンスルホネート、ヒドロニトレート、ヒドロマレエート、ヒドロアセテート、ヒドロシトレート、ヒドロフマレート、ヒドロタルトレート、ヒドロオキサレート、ヒドロスクシネート、ヒドロベンゾエート及びヒドロ‐p‐トルエンスルホネートの中から選択される。LTD4‐拮抗薬がオプションとして形成できる塩又はその誘導体は、例えば、アルカリ金属、例えばナトリウム塩、カリウム塩、スルホベンゾエート、ホスフェート、イソニコチネート、アセテート、ジクロロアセテート、プロピオネート、ジヒドロゲンホスフェート、パルミテート、ピバレート又はフロエートを意味している。
‐4‐[(3‐クロロ‐4‐フルオロフェニル)アミノ]‐6‐{[4‐(モルフォリン‐4‐イル)‐1‐オキソ‐2‐ブテン‐1‐イル]アミノ}‐7‐シクロプロピルメトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロフェニル)アミノ]‐6‐{[4‐(N,N‐ジエチルアミノ)‐1‐オキソ‐2‐ブテン‐1‐イル]アミノ}‐7‐シクロプロピルメトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロフェニル)アミノ]‐6‐{[4‐(N,N‐ジメチルアミノ)‐1‐オキソ‐2‐ブテン‐1‐イル]アミノ}‐7‐シクロプロピルメトキシ‐キナゾリン、
‐4‐[(R)‐(1‐フェニル‐エチル)アミノ]‐6‐{[4‐(モルフォリン‐4‐イル)‐1‐オキソ‐2‐ブテン‐1‐イル]アミノ}‐7‐シクロペンチルオキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{((R)‐6‐メチル‐2‐オキソ‐モルフォリン‐4‐イル)‐1‐オキソ‐2‐ブテン‐1‐イル]アミノ}‐7‐シクロプロピルメトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{[4‐((R)‐6‐メチル‐2‐オキソ‐モルフォリン‐4‐イル)‐1‐オキソ‐2‐ブテン‐1‐イル]アミノ}‐7‐[(S)‐(テトラヒドロフラン‐3‐イル)オキシ]‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{[4‐((R)‐2‐メトキシメチル‐6‐オキソ‐モルフォリン‐4‐イル)‐1‐オキソ‐2‐ブテン‐1‐イル]アミノ}‐7‐シクロプロピルメトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐[2‐((S)‐6‐メチル‐2‐オキソ‐モルフォリン‐4‐イル)‐エトキシ]‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロフェニル)アミノ]‐6‐({4‐[N‐(2‐メトキシ‐エチル)‐N‐メチル‐アミノ]‐1‐オキソ‐2‐ブテン‐1‐イル]アミノ)‐7‐シクロプロピルメトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロフェニル)アミノ]‐6‐({4‐[N,N‐ジメチルアミノ]‐1‐オキソ‐2‐ブテン‐1‐イル}アミノ)‐7‐シクロペンチルオキシ‐キナゾリン、
‐4‐[(R)‐(1‐フェニル‐エチル)アミノ]‐6‐({4‐[N,N‐ビス(‐(2‐メトキシ‐エチル)‐アミノ)‐1‐オキソ‐2‐ブテン‐1‐イル]アミノ}‐7‐シクロプロピルメトキシ‐キナゾリン、
‐4‐[(R)‐(1‐フェニル‐エチル)アミノ]‐6‐({4‐[N‐(2‐メトキシ‐エチル)‐N‐メチル‐アミノ]‐1‐オキソ‐2‐ブテン‐1‐イル}アミノ)‐7‐シクロプロピルメトキシ‐キナゾリン、
‐4‐[(R)‐(1‐フェニル‐エチル)アミノ]‐6‐({4‐[N‐(2‐メトキシ‐エチル)‐N‐メチル‐アミノ)‐1‐オキソ‐2‐ブテン‐1‐イル}アミノ)‐7‐シクロプロピルメトキシ‐キナゾリン、
‐4‐[(R)‐(1‐フェニル‐エチル)アミノ]‐6‐({4‐[N‐(テトラヒドロピラン‐4‐イル)‐N‐メチル‐アミノ]‐1‐オキソ‐2‐ブテン‐1‐イル}アミノ)‐7‐シクロプロピルメトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロフェニル)アミノ]‐6‐({4‐[N,N‐ジメチルアミノ]‐1‐オキソ‐2‐ブテン‐1‐イル]アミノ}‐7‐((R)‐テトラヒドロフラン‐3‐イルオキシ]‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロフェニル)アミノ]‐6‐({4‐[N,N‐ジメチルアミノ]‐1‐オキソ‐2‐ブテン‐1‐イル]アミノ}‐7‐((S)‐テトラヒドロフラン‐3‐イルオキシ]‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロフェニル)アミノ]‐6‐({4‐[N‐(2‐メトキシ‐エチル)‐N‐メチル‐アミノ]‐1‐オキソ‐2‐ブテン‐1‐イル}アミノ)‐7‐シクロペンチルオキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロフェニル)アミノ]‐6‐({4‐(N‐シクロプロピル‐N‐メチル‐アミノ)‐1‐オキソ‐2‐ブテン‐1‐イル]アミノ}‐7‐シクロペンチルロキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロフェニル)アミノ]‐6‐{[4‐(N,N‐ジメチルアミノ)‐1‐オキソ‐2‐ブテン‐1‐イル]アミノ}‐7‐[(R)‐(テトラヒドロフラン‐2‐イル)メトキシ]‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロフェニル)アミノ]‐6‐{[4‐(N,N‐ジメチルアミノ)‐1‐オキソ‐2‐ブテン‐1‐イル]アミノ}‐7‐[(S)‐(テトラヒドロフラン‐2‐イル)メトキシ]‐キナゾリン、
‐4‐[(3‐エチニル‐フェニル)アミノ]‐6,7‐ビス‐(2‐メトキシ‐エトキシ)‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロフェニル)アミノ]‐7‐モルフォリン‐4‐イル)‐プロピルオキシ]‐6‐[ビニルカルボニル)アミノ]キナゾリン、
‐4‐[(R)‐(1‐フェニル‐エチル)アミノ]‐6‐(4‐ヒドロキシ‐フェニル)‐7H‐ピロロ[2,3‐d]ピリミジン、
‐3‐シアノ‐4‐[(3‐クロロ‐4‐フルオロフェニル)アミノ]‐6‐{[4‐(N,N‐ジメチルアミノ)‐1‐オキソ‐2‐ブテン‐1‐イル]アミノ}‐7‐エトキシ‐キノリン、
‐4‐{[(3‐クロロ‐4‐(3‐フルオロ‐ベンジルオキシ)‐フェニル]アミノ}‐6‐(5‐{[2‐メタンスルホニル‐エチル)アミノ]メチル}‐フラン‐2‐イル)キナゾリン、
‐4‐[(R)‐(1‐フェニル‐エチル)アミノ]‐6‐{[4‐((R)‐6‐メチル‐2‐オキソ‐モルフォリン‐4‐イル)‐1‐オキソ‐2‐ブテン‐1‐イル]アミノ}‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロフェニル)アミノ]‐6‐{[4‐(モルフォリン‐4‐イル)‐1‐オキソ‐2‐ブテン‐1‐イル]アミノ}‐7‐[(テトラヒドロフラン‐2‐イル)メトキシ]‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロフェニル)アミノ]‐6‐({4‐[N,N‐ビス‐(2‐メトキシ‐エチル)‐アミノ]‐1‐オキソ‐2‐ブテン‐1‐イル}アミノ)‐7‐[テトラヒドロフラン‐2‐イル)メトキシ]‐キナゾリン、
‐4‐[(3‐エチニル‐フェニル)アミノ]‐6‐{[4‐(5,5‐ジメチル‐2‐オキソ‐モルフォリン‐4‐イル)‐1‐オキソ‐2‐ブテン‐1‐イル]アミノ}‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐[2‐(2,2‐ジメチル‐6‐オキソ‐モルフォリン‐4‐イル)エトキシ]‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐[2‐(2,2‐ジメチル‐6‐オキソ‐モルフォリン‐4‐イル)エトキシ]‐7‐[(R)‐(テトラヒドロフラン‐2‐イル)メトキシ]‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐7‐[2‐(2,2‐ジメチル‐6‐オキソ‐モルフォリン‐4‐イル)エトキシ]‐6‐[(S)‐(テトラヒドロフラン‐2‐イル)メトキシ]‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{2‐[4‐(2‐オキソ‐モルフォリン‐4‐イル)‐ピペリジン‐1‐イル]‐エトキシ}‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐[1‐(t‐ブチルオキシカルボニル)‐ピペリジン‐4‐イルオキシ]‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(トランス‐4‐アミノ‐シクロヘキサン‐1‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(トランス‐4‐メタンスルホニルアミノ‐シクロヘキサン‐1‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(テトラヒドロピラン‐3‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(1‐メチル‐ピペリジン‐4‐イルオキシ]‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{1‐[(モルフォリン‐4‐イル)カルボニル]‐ピペリジン‐4‐イルオキシ}‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{1‐[(メトキシメチル)カルボニル]‐ピペリジン‐4‐イルオキシ}‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(ピペリジン‐3‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐[1‐(2‐アセチルアミノ‐エチル)‐ピペリジン‐4‐イルオキシ]‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(テトラヒドロピラン‐4‐イルオキシ)‐7‐エトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐((S)‐テトラヒドロピラン‐3‐イルオキシ)‐7‐ヒドロキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(テトラヒドロピラン‐4‐イルオキシ)‐7‐(2‐メトキシ‐エトキシ)‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{トランス‐4[(ジメチルアミノ)スルホニルアミノ]‐シクロヘキサン‐1‐イルオキシ}‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{トランス‐4‐[(モルフォリン‐4‐イル)カルボニルアミノ]‐シクロヘキサン‐1‐イルオキシ}‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{トランス‐4‐[(モルフォリン‐4‐イル)スルホニルアミノ]‐シクロヘキサン‐1‐イルオキシ}‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(テトラヒドロピラン‐4‐イルオキシ)‐7‐(2‐アセチルアミノ‐エトキシ)‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(テトラヒドロフラン‐4‐イルオキシ)‐7‐(2‐メタンスルホニルアミノ‐エトキシ)‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{1‐[(ピペリジン‐1‐イル)カルボニル]‐ピペリジン‐4‐イルオキシ}‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(1‐アミノカルボニルメチル‐ピペリジン‐4‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(シス‐4‐{N[(テトラヒドロピラン‐4‐イル)カルボニル]‐N‐メチル‐アミノ}‐シクロヘキサン‐1‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(シス‐4‐{N‐[(モルフォリン‐4‐イル)カルボニル]‐N‐メチル‐アミノ}‐シクロヘキサン‐1‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(シス‐4‐{N‐[(モルフォリン‐4‐イル)スルホニル]‐N‐メチル‐アミノ}‐シクロヘキサン‐1‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(トランス‐4‐エタンスルホニルアミノ‐シクロヘキサン‐1‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(1‐メタンスルホニル‐ピペリジン‐4‐イルオキシ}‐7‐エトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(1‐メタンスルホニル‐ピペリジン‐4‐イルオキシ)‐7‐(2‐メトキシ‐エトキシ)‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐[1‐(2‐メトキシ‐アセチル)‐ピペリジン‐4‐イルオキシ]‐7‐(2‐メトキシ‐エトキシ)‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(シス‐4‐アセチルアミノ‐シクロヘキサン‐1‐イルオキシ]‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐エチニル‐4‐フェニル)アミノ]‐6‐[1‐(t‐ブチルオキシカルボニル)‐ピペリジン‐4‐イルオキシ]‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐エチニル‐フェニル)アミノ]‐6‐(テトラヒドロピラン‐4‐イルオキシ]‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(シス‐4‐{N‐[(ピペリジン‐1‐イル)カルボニル]‐N‐メチル‐アミノ}‐シクロヘキサン‐1‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(シス‐4‐{N‐[(4‐メチル‐ピペリジン‐1‐イル)カルボニル]‐N‐メチル‐アミノ}‐シクロヘキサン‐1‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{シス‐4‐[(モルフォリン‐4‐イル)カルボニルアミノ]‐シクロヘキサン‐1‐イルオキシ}‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{1‐[2‐(2‐オキソピロリジン‐1‐イル)エチル]‐ピペリジン‐4‐イルオキシ}‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{1‐[(モルフォリン‐4‐イル)カルボニル]‐ピペリジン‐4‐イルオキシ}‐7‐(2‐メトキシ‐エトキシ)‐キナゾリン、
‐4‐[(3‐エチニル‐フェニル)アミノ]‐6‐(1‐アセチル‐ピペリジン‐4‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐エチニル‐フェニル)アミノ]‐6‐(1‐メチル‐ピペリジン‐4‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐エチニル‐フェニル)アミノ]‐6‐(1‐メタンスルホニル‐ピペリジン‐4‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(1‐メチル‐ピペリジン‐4‐イルオキシ)‐7(2‐メトキシ‐エトキシ)‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(1‐イソプロピルオキシカルボニル‐ピペリジン‐4‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(シス‐4‐メチルアミノ‐シクロヘキサン‐1‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(シス‐4‐[N‐(2‐メトキシ‐アセチル)‐N‐メチル‐アミノ]‐シクロヘキサン‐1‐イルオキシ}‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐エチニル‐フェニル)アミノ]‐6‐(ピペリジン‐4‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐エチニル‐フェニル)アミノ]‐6‐[1‐(2‐メトキシ‐アセチル)‐ピペリジン‐4‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐エチニル‐フェニル)アミノ]‐6‐{1‐[(モルフォリン‐4‐イル)カルボニル]‐ピペリジン‐4‐イルオキシ}‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{1‐[(シス‐2,6‐ジメチル‐モルフォリン‐4‐イル)カルボニル]‐ピペリジン‐4‐イルオキシ}‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{1‐[(2‐メチル‐モルフォリン‐4‐イル)カルボニル]‐ピペリジン‐4‐イルオキシ}‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{1‐[(S,S)‐(2‐オキサ‐5‐アザ‐ビシクロ[2.2.1]ヘプト‐5‐イル)カルボニル]‐ピペリジン‐4‐イルオキシ}‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{1‐[N‐メチル‐N‐2‐メトキシエチル‐アミノ]カルボニル]‐ピペリジン‐4‐イルオキシ}‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(1‐エチル‐ピペリジン‐4‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{1‐[(2‐メトキシエチル)カルボニル]‐ピペリジン‐4‐イルオキシ}‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐{1‐[(3‐メトキシプロピル‐アミノ)‐カルボニル]‐ピペリジン‐4‐イルオキシ}‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐[シス‐4‐(N‐メタンスルホニル‐N‐メチル‐アミノ)‐シクロヘキサン‐1‐イルオキシ]‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐[シス‐4‐(N‐アセチル‐N‐メチル‐アミノ)‐シクロヘキサン‐1‐イルオキシ]‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(トランス‐4‐メチルアミノ‐シクロヘキサン‐1‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐[トランス‐4‐(N‐メタンスルホニル‐N‐メチル‐アミノ)‐シクロヘキサン‐1‐イルオキシ]‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(トランス‐4‐ジメチルアミノ‐シクロヘキサン‐1‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(トランス‐4‐{N‐[(モルフォリン‐4‐イル)カルボニル]‐N‐メチル‐アミノ}‐シクロヘキサン‐1‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐[2‐(2,2‐ジメチル‐6‐オキソ‐モルフォリン‐4‐イル)‐エトキシ]‐7‐[(S)‐(テトラヒドロフラン‐2‐イル)メトキシ]‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(1‐メタンスルホニル‐ピペリジン‐4‐イルオキシ)‐7‐メトキシ‐キナゾリン、
‐4‐[(3‐クロロ‐4‐フルオロ‐フェニル)アミノ]‐6‐(1‐シアノ‐ピペリジン‐4‐イルオキシ)‐7‐メトキシ‐キナゾリンの中から選択された化合物であり、
オプションとして上記化合物のラセミ化合物、エナンチオマー又はジアステレオマー及びオプションとして上記化合物の薬理学的に容認できる酸添加塩、溶媒化合物又は水和物である。本発明によれば、ベータミメティックの酸添加塩は、好ましくは、ヒドロクロリド、ヒドロブロミド、ヒドロイオジド、ヒドロスルフェート、ヒドロホスフェート、ヒドロメタンスルホネート、ヒドロニトレート、ヒドロマレエート、ヒドロアセテート、ヒドロシトレート、ヒドロフマレート、ヒドロタルトレート、ヒドロオキサレート、ヒドロスクシネート、ヒドロベンゾエート及びヒドロ‐p‐トルエンスルホネートの中から選択される。
2 医薬製剤又は調合薬
3 容器
4 袋
5 圧力発生器
6 ホルダ
7 駆動ばね
8 ロック要素
9 運搬管
10 逆止弁
11 圧力チャンバ
12 噴出ノズル
13 マウスピース
14 エーロゾル
15 給気開口部
16 第1のハウジング部品(上側部品)
17 内側部品
17a 内側部品の上側部分
17b 内側部品の下側部分
18 第2のハウジング部品(下側部品)
19 保持要素
20 ばね(下側ハウジング部品のばね)
21 容器ベース
22 穿通要素
23 アダプタ
24 第1の連結部(アダプタ)
25 連結部分
26 筒状部材
27 第2の連結部(アダプタ)
28 第3の連結部(アダプタ)
29 管
30 環状チャネル
31 ロック弁
32 吸入器具
33 第1の連結部(吸入器具)
34 第2の連結部(吸入器具)
35 第3の連結部(吸入器具)
36 弁要素
37 突出部
38 チャンバ
39 ハウジング
40 入口弁
41 入口開口部
42 弁要素
43 連結チャネル
44 出口開口部
45 出口弁
46 弁開口部
47 弁要素
48 呼息空気
49 エーロゾル流
50 吸息空気
Claims (14)
- ネブライザ(1)用の第1の連結部(24)と患者側に設けられた第2の連結部(27)と呼吸適合空気用の第3の連結部(28)とを有するアダプタ(23)において、
前記アダプタ(23)は、前記第2の連結部(27)から前記アダプタ(23)の内側に延び、前記ネブライザ(1)の噴出ノズル(12)に隣接して配置される筒状部材(26)を有し、
前記第1の連結部(24)は、前記噴出ノズル(12)を保持し又は包囲した突出部(37)に実質的に漏れ止め状態で連結可能であり、給気が前記突出部(37)の周囲を通って前記アダプタ(23)内に流入せず、
前記第3の連結部(28)を通って、呼吸適合空気は、前記アダプタ(23)により形成され又はこの中に形成された環状チャネル(30)を経て、前記第1の連結部(24)に供給可能であり、前記呼吸適合空気を前記ネブライザ(1)からのエーロゾル(14)と混合することができると共に、前記エーロゾル(14)と一緒に前記呼吸適合空気は前記筒状部材(26)を経て、前記第2の連結部(27)を通って放出可能である、
ことを特徴とするアダプタ(23)。 - 前記アダプタ(23)が前記ネブライザ(1)に連結されると、必然的に開き、且つ、前記アダプタ(23)が前記ネブライザ(1)から分離されると、閉じるロック弁(31)を有している、
請求項1に記載のアダプタ(23)。 - 前記ロック弁(31)が、少なくとも1つの可動弁要素(36)を備え、該可動弁要素が、噴出ノズル(12)によって、または噴出ノズル(12)を保持するネブライザ(1)の前記突出部(37)によって、作動させられる、
請求項2に記載のアダプタ(23)。 - 前記ロック弁(31)が、付勢され、且つ/又は自動閉鎖されるように構成されている、
請求項3に記載のアダプタ(23)。 - 前記第1の連結部(24)は、
前記ネブライザ(1)のマウスピース(13)の内側輪郭に外側輪郭が合わせられ、前記マウスピース(13)内に挿入可能な連結部分(25)を有し、
前記アダプタ(23)が前記ネブライザ(1)に連結されたとき、前記連結部分(25)は、前記マウスピース(13)内に延びる、
請求項1ないし4のいずれか1項に記載のアダプタ(23)。 - 前記アダプタ(23)が前記ネブライザ(1)に連結されたとき、前記連結部分(25)は、前記突出部(37)と前記マウスピース(13)の内壁との間の実質的に環状の中間空間を閉鎖すると共に/或いは前記ネブライザ(1)の給気開口部(15)を閉鎖し、前記ネブライザ(1)又はアダプタ(23)が用いられるとき給気が1つ又は複数の前記給気開口部(15)を通って前記マウスピース(13)内に流入しないようにする、
請求項5に記載のアダプタ(23)。 - 前記第1の連結部(24)は、前記ネブライザ(1)の長円形マウスピース(13)に連結可能な長円形断面を有する、
請求項1ないし6のいずれか1項に記載のアダプタ(23)。 - 前記第2の連結部(27)は、丸形断面を有する、
請求項1ないし7のいずれか1項に記載のアダプタ。 - 前記第2の連結部(27)は、管(29)又は吸入器具(32)に連結可能に構成されている、
請求項1ないし8のいずれか1項に記載のアダプタ。 - 前記第1の連結部(24)及び前記第2の連結部(27)は、枝分かれすることなく互いに流体結合されている、
請求項1ないし9のいずれか1項に記載のアダプタ(23)。 - 前記アダプタ(23)は、一体品として且つ/或いは射出成形品の形態で構成されている、
請求項1ないし10のいずれか1項に記載のアダプタ。 - 前記第3の連結部(28)は、管(29)又はベンチレータに連結可能である、
請求項1ないし11のいずれか1項に記載のアダプタ。 - 前記呼吸適合空気が、少なくとも実質的に環状の形状で且つ/或いは前記噴出ノズル(12)の付近でひねりを付けた状態で流れ、前記エーロゾル(14)と一緒に前記筒状部材(26)を通って前記第2の連結部(27)に流れることができるようにする、
請求項1ないし12のいずれか1項に記載のアダプタ。 - 請求項1ないし13のいずれか1項に記載のアダプタを有することを特徴とするネブライザ。
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WO2010133294A2 (de) | 2010-11-25 |
EP2432531A2 (de) | 2012-03-28 |
WO2010133294A3 (de) | 2011-01-13 |
US9682202B2 (en) | 2017-06-20 |
JP2015142803A (ja) | 2015-08-06 |
EP3508239A1 (de) | 2019-07-10 |
EP3508239B1 (de) | 2020-12-23 |
US20160095992A1 (en) | 2016-04-07 |
US20120138049A1 (en) | 2012-06-07 |
EP2432531B1 (de) | 2019-03-06 |
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