JP6473738B2 - チオトロピウム乾燥粉末 - Google Patents
チオトロピウム乾燥粉末 Download PDFInfo
- Publication number
- JP6473738B2 JP6473738B2 JP2016505482A JP2016505482A JP6473738B2 JP 6473738 B2 JP6473738 B2 JP 6473738B2 JP 2016505482 A JP2016505482 A JP 2016505482A JP 2016505482 A JP2016505482 A JP 2016505482A JP 6473738 B2 JP6473738 B2 JP 6473738B2
- Authority
- JP
- Japan
- Prior art keywords
- dry powder
- less
- microns
- dry
- inhalable
- 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.)
- Active
Links
- 239000000843 powder Substances 0.000 title claims description 419
- LERNTVKEWCAPOY-DZZGSBJMSA-N tiotropium Chemical compound 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 title claims description 157
- 229940110309 tiotropium Drugs 0.000 title claims description 155
- 239000002245 particle Substances 0.000 claims description 353
- 229940112141 dry powder inhaler Drugs 0.000 claims description 225
- 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 185
- 229960000257 tiotropium bromide Drugs 0.000 claims description 185
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 162
- 239000002775 capsule Substances 0.000 claims description 114
- 239000003814 drug Substances 0.000 claims description 96
- 229940124597 therapeutic agent Drugs 0.000 claims description 84
- 239000011780 sodium chloride Substances 0.000 claims description 81
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims description 79
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims description 77
- 208000007934 ACTH-independent macronodular adrenal hyperplasia Diseases 0.000 claims description 40
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 39
- BLUGYPPOFIHFJS-UUFHNPECSA-N (2s)-n-[(2s)-1-[[(3r,4s,5s)-3-methoxy-1-[(2s)-2-[(1r,2r)-1-methoxy-2-methyl-3-oxo-3-[[(1s)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]-3-methyl-2-(methylamino)butanamid Chemical compound CN[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N(C)[C@@H]([C@@H](C)CC)[C@H](OC)CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C=1SC=CN=1)CC1=CC=CC=C1 BLUGYPPOFIHFJS-UUFHNPECSA-N 0.000 claims description 38
- 208000023504 respiratory system disease Diseases 0.000 claims description 31
- 208000006673 asthma Diseases 0.000 claims description 27
- 201000003883 Cystic fibrosis Diseases 0.000 claims description 22
- 238000011282 treatment Methods 0.000 claims description 19
- 201000009267 bronchiectasis Diseases 0.000 claims description 12
- 229960001469 fluticasone furoate Drugs 0.000 claims description 12
- XTULMSXFIHGYFS-VLSRWLAYSA-N fluticasone furoate Chemical compound O([C@]1([C@@]2(C)C[C@H](O)[C@]3(F)[C@@]4(C)C=CC(=O)C=C4[C@@H](F)C[C@H]3[C@@H]2C[C@H]1C)C(=O)SCF)C(=O)C1=CC=CO1 XTULMSXFIHGYFS-VLSRWLAYSA-N 0.000 claims description 12
- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 claims description 11
- 239000003246 corticosteroid Substances 0.000 claims description 11
- 229940125389 long-acting beta agonist Drugs 0.000 claims description 11
- 239000011859 microparticle Substances 0.000 claims description 11
- 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 claims description 10
- 229960003728 ciclesonide Drugs 0.000 claims description 10
- 229960001334 corticosteroids Drugs 0.000 claims description 10
- 229960002744 mometasone furoate Drugs 0.000 claims description 9
- WOFMFGQZHJDGCX-ZULDAHANSA-N mometasone furoate Chemical compound O([C@]1([C@@]2(C)C[C@H](O)[C@]3(Cl)[C@@]4(C)C=CC(=O)C=C4CC[C@H]3[C@@H]2C[C@H]1C)C(=O)CCl)C(=O)C1=CC=CO1 WOFMFGQZHJDGCX-ZULDAHANSA-N 0.000 claims description 9
- 230000001225 therapeutic effect Effects 0.000 claims description 9
- 230000009798 acute exacerbation Effects 0.000 claims description 8
- 229940125390 short-acting beta agonist Drugs 0.000 claims description 7
- 229940124599 anti-inflammatory drug Drugs 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 14
- 239000000203 mixture Substances 0.000 description 142
- 238000009472 formulation Methods 0.000 description 129
- DQHNAVOVODVIMG-UHFFFAOYSA-M Tiotropium bromide Chemical compound [Br-].C1C(C2C3O2)[N+](C)(C)C3CC1OC(=O)C(O)(C=1SC=CC=1)C1=CC=CS1 DQHNAVOVODVIMG-UHFFFAOYSA-M 0.000 description 107
- 229940046810 spiriva Drugs 0.000 description 107
- 238000000034 method Methods 0.000 description 80
- 229960003136 leucine Drugs 0.000 description 62
- 239000010419 fine particle Substances 0.000 description 44
- 239000000443 aerosol Substances 0.000 description 36
- 230000008859 change Effects 0.000 description 28
- 210000004072 lung Anatomy 0.000 description 27
- 239000007789 gas Substances 0.000 description 26
- 238000009826 distribution Methods 0.000 description 25
- 239000007788 liquid Substances 0.000 description 25
- 238000001694 spray drying Methods 0.000 description 25
- 210000002345 respiratory system Anatomy 0.000 description 24
- 239000007921 spray Substances 0.000 description 23
- 239000002904 solvent Substances 0.000 description 22
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 21
- 239000000243 solution Substances 0.000 description 21
- 239000012530 fluid Substances 0.000 description 20
- 230000004199 lung function Effects 0.000 description 20
- QLAKAJLYYGOZQL-UHFFFAOYSA-N Carboxyphosphamide Chemical compound ClCCN(CCCl)P(=O)(N)OCCC(O)=O QLAKAJLYYGOZQL-UHFFFAOYSA-N 0.000 description 18
- 208000019693 Lung disease Diseases 0.000 description 18
- 230000000694 effects Effects 0.000 description 18
- 239000003112 inhibitor Substances 0.000 description 18
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 18
- 206010006458 Bronchitis chronic Diseases 0.000 description 17
- 206010014561 Emphysema Diseases 0.000 description 17
- 206010006451 bronchitis Diseases 0.000 description 17
- 208000007451 chronic bronchitis Diseases 0.000 description 17
- 230000000241 respiratory effect Effects 0.000 description 17
- 239000006196 drop Substances 0.000 description 15
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 15
- 229940125369 inhaled corticosteroids Drugs 0.000 description 15
- 239000000047 product Substances 0.000 description 15
- 230000006872 improvement Effects 0.000 description 14
- 229940068196 placebo Drugs 0.000 description 14
- 239000000902 placebo Substances 0.000 description 14
- 229960002668 sodium chloride Drugs 0.000 description 14
- 239000000126 substance Substances 0.000 description 14
- 238000000889 atomisation Methods 0.000 description 13
- 239000006185 dispersion Substances 0.000 description 13
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 13
- 229910052740 iodine Inorganic materials 0.000 description 13
- 238000002156 mixing Methods 0.000 description 13
- 230000004044 response Effects 0.000 description 13
- 238000012360 testing method Methods 0.000 description 13
- 206010020751 Hypersensitivity Diseases 0.000 description 12
- 238000005259 measurement Methods 0.000 description 12
- 238000002411 thermogravimetry Methods 0.000 description 11
- MSIGGUSMCUUDGY-UHFFFAOYSA-M 2-methoxyethyl(trimethyl)azanium;chloride Chemical compound [Cl-].COCC[N+](C)(C)C MSIGGUSMCUUDGY-UHFFFAOYSA-M 0.000 description 10
- 230000008021 deposition Effects 0.000 description 10
- 229910052757 nitrogen Inorganic materials 0.000 description 10
- 230000003285 pharmacodynamic effect Effects 0.000 description 10
- -1 pyrbuterol Chemical compound 0.000 description 10
- 239000000725 suspension Substances 0.000 description 10
- 150000001768 cations Chemical class 0.000 description 9
- 239000003795 chemical substances by application Substances 0.000 description 9
- 229940079593 drug Drugs 0.000 description 9
- 230000003434 inspiratory effect Effects 0.000 description 9
- 230000009885 systemic effect Effects 0.000 description 9
- 229940124630 bronchodilator Drugs 0.000 description 8
- 238000001035 drying Methods 0.000 description 8
- 238000004128 high performance liquid chromatography Methods 0.000 description 8
- 150000003839 salts Chemical class 0.000 description 8
- 102100026992 Dermcidin Human genes 0.000 description 7
- 230000000875 corresponding effect Effects 0.000 description 7
- 230000001186 cumulative effect Effects 0.000 description 7
- 239000000839 emulsion Substances 0.000 description 7
- 239000003960 organic solvent Substances 0.000 description 7
- 230000008569 process Effects 0.000 description 7
- 230000009467 reduction Effects 0.000 description 7
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 6
- 208000026935 allergic disease Diseases 0.000 description 6
- 230000000172 allergic effect Effects 0.000 description 6
- 230000007815 allergy Effects 0.000 description 6
- 229940121363 anti-inflammatory agent Drugs 0.000 description 6
- 239000002260 anti-inflammatory agent Substances 0.000 description 6
- 208000010668 atopic eczema Diseases 0.000 description 6
- 230000006870 function Effects 0.000 description 6
- 230000009610 hypersensitivity Effects 0.000 description 6
- 238000000338 in vitro Methods 0.000 description 6
- 238000005070 sampling Methods 0.000 description 6
- 230000001932 seasonal effect Effects 0.000 description 6
- 239000007787 solid Substances 0.000 description 6
- 241000699670 Mus sp. Species 0.000 description 5
- 210000004369 blood Anatomy 0.000 description 5
- 239000008280 blood Substances 0.000 description 5
- 230000007423 decrease Effects 0.000 description 5
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 description 5
- 239000004615 ingredient Substances 0.000 description 5
- 238000001294 liquid chromatography-tandem mass spectrometry Methods 0.000 description 5
- 239000000463 material Substances 0.000 description 5
- 238000002360 preparation method Methods 0.000 description 5
- 230000009325 pulmonary function Effects 0.000 description 5
- 239000002464 receptor antagonist Substances 0.000 description 5
- 229940044551 receptor antagonist Drugs 0.000 description 5
- 210000002966 serum Anatomy 0.000 description 5
- 230000003068 static effect Effects 0.000 description 5
- 102100021943 C-C motif chemokine 2 Human genes 0.000 description 4
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 4
- 206010061218 Inflammation Diseases 0.000 description 4
- 102000003816 Interleukin-13 Human genes 0.000 description 4
- 108090000176 Interleukin-13 Proteins 0.000 description 4
- 102000004388 Interleukin-4 Human genes 0.000 description 4
- 108090000978 Interleukin-4 Proteins 0.000 description 4
- 239000004480 active ingredient Substances 0.000 description 4
- 239000013543 active substance Substances 0.000 description 4
- 230000001154 acute effect Effects 0.000 description 4
- 239000005557 antagonist Substances 0.000 description 4
- 239000003125 aqueous solvent Substances 0.000 description 4
- 210000003123 bronchiole Anatomy 0.000 description 4
- 201000010099 disease Diseases 0.000 description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- 230000009977 dual effect Effects 0.000 description 4
- 230000006698 induction Effects 0.000 description 4
- 230000004054 inflammatory process Effects 0.000 description 4
- 238000004519 manufacturing process Methods 0.000 description 4
- 229960001664 mometasone Drugs 0.000 description 4
- 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 4
- 239000000546 pharmaceutical excipient Substances 0.000 description 4
- 230000036470 plasma concentration Effects 0.000 description 4
- 238000000634 powder X-ray diffraction Methods 0.000 description 4
- 230000002685 pulmonary effect Effects 0.000 description 4
- 238000012552 review Methods 0.000 description 4
- 208000024891 symptom Diseases 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
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 description 3
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
- 108010010803 Gelatin Proteins 0.000 description 3
- 241000282412 Homo Species 0.000 description 3
- 108010002616 Interleukin-5 Proteins 0.000 description 3
- 102100039897 Interleukin-5 Human genes 0.000 description 3
- 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 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 241000700605 Viruses Species 0.000 description 3
- 230000004913 activation Effects 0.000 description 3
- 150000008064 anhydrides Chemical class 0.000 description 3
- 230000015572 biosynthetic process Effects 0.000 description 3
- 210000000621 bronchi Anatomy 0.000 description 3
- 230000001684 chronic effect Effects 0.000 description 3
- 230000002596 correlated effect Effects 0.000 description 3
- 230000001419 dependent effect Effects 0.000 description 3
- 238000000113 differential scanning calorimetry Methods 0.000 description 3
- 239000008393 encapsulating agent Substances 0.000 description 3
- 238000010304 firing Methods 0.000 description 3
- 229960002714 fluticasone Drugs 0.000 description 3
- 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 3
- 229920000159 gelatin Polymers 0.000 description 3
- 239000008273 gelatin Substances 0.000 description 3
- 235000019322 gelatine Nutrition 0.000 description 3
- 235000011852 gelatine desserts Nutrition 0.000 description 3
- 229940043355 kinase inhibitor Drugs 0.000 description 3
- 239000008101 lactose Substances 0.000 description 3
- 229960001375 lactose Drugs 0.000 description 3
- 238000013123 lung function test Methods 0.000 description 3
- 238000010172 mouse model Methods 0.000 description 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 3
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 3
- 238000009613 pulmonary function test Methods 0.000 description 3
- 238000005507 spraying Methods 0.000 description 3
- 230000002459 sustained effect Effects 0.000 description 3
- 238000011287 therapeutic dose Methods 0.000 description 3
- 239000003643 water by type Substances 0.000 description 3
- MSYGAHOHLUJIKV-UHFFFAOYSA-N 3,5-dimethyl-1-(3-nitrophenyl)-1h-pyrazole-4-carboxylic acid ethyl ester Chemical compound CC1=C(C(=O)OCC)C(C)=NN1C1=CC=CC([N+]([O-])=O)=C1 MSYGAHOHLUJIKV-UHFFFAOYSA-N 0.000 description 2
- KKYABQBFGDZVNQ-UHFFFAOYSA-N 6-[5-[(cyclopropylamino)-oxomethyl]-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)-3-pyridinecarboxamide Chemical compound CC1=C(F)C=C(C(=O)NC2CC2)C=C1C1=CC=C(C(=O)NCC(C)(C)C)C=N1 KKYABQBFGDZVNQ-UHFFFAOYSA-N 0.000 description 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 2
- 101710155857 C-C motif chemokine 2 Proteins 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 2
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-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
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-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
- 102100022086 GRB2-related adapter protein 2 Human genes 0.000 description 2
- 108060003951 Immunoglobulin Proteins 0.000 description 2
- 102000004559 Interleukin-13 Receptors Human genes 0.000 description 2
- 108010017511 Interleukin-13 Receptors Proteins 0.000 description 2
- 102100020941 Interleukin-4 Human genes 0.000 description 2
- 102000010787 Interleukin-4 Receptors Human genes 0.000 description 2
- 108010038486 Interleukin-4 Receptors Proteins 0.000 description 2
- 108010002335 Interleukin-9 Proteins 0.000 description 2
- 102000000585 Interleukin-9 Human genes 0.000 description 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 description 2
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-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
- 108010058846 Ovalbumin Proteins 0.000 description 2
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-L Phosphate ion(2-) Chemical compound OP([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-L 0.000 description 2
- 102000002255 Secretory Proteinase Inhibitory Proteins Human genes 0.000 description 2
- 108010000303 Secretory Proteinase Inhibitory Proteins Proteins 0.000 description 2
- DTQVDTLACAAQTR-UHFFFAOYSA-M Trifluoroacetate Chemical compound [O-]C(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-M 0.000 description 2
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 description 2
- 102000011017 Type 4 Cyclic Nucleotide Phosphodiesterases Human genes 0.000 description 2
- 108010037584 Type 4 Cyclic Nucleotide Phosphodiesterases Proteins 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 201000009961 allergic asthma Diseases 0.000 description 2
- 238000004458 analytical method Methods 0.000 description 2
- 150000001450 anions Chemical class 0.000 description 2
- 229950005794 anrukinzumab Drugs 0.000 description 2
- 238000003556 assay Methods 0.000 description 2
- NBMKJKDGKREAPL-DVTGEIKXSA-N beclomethasone 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)CO)(O)[C@@]1(C)C[C@@H]2O NBMKJKDGKREAPL-DVTGEIKXSA-N 0.000 description 2
- 230000008901 benefit Effects 0.000 description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 2
- 239000000168 bronchodilator agent Substances 0.000 description 2
- 229960001838 canakinumab Drugs 0.000 description 2
- 229910002092 carbon dioxide Inorganic materials 0.000 description 2
- 239000001569 carbon dioxide Substances 0.000 description 2
- 125000002091 cationic group Chemical group 0.000 description 2
- 238000012512 characterization method Methods 0.000 description 2
- 239000013078 crystal Substances 0.000 description 2
- 238000011161 development Methods 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-M dihydrogenphosphate Chemical compound OP(O)([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-M 0.000 description 2
- 238000012377 drug delivery Methods 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- 230000007613 environmental effect Effects 0.000 description 2
- 230000005713 exacerbation Effects 0.000 description 2
- 229910052731 fluorine Inorganic materials 0.000 description 2
- 239000011737 fluorine Substances 0.000 description 2
- 125000001153 fluoro group Chemical group F* 0.000 description 2
- 238000005187 foaming Methods 0.000 description 2
- 239000011521 glass Substances 0.000 description 2
- 238000004442 gravimetric analysis Methods 0.000 description 2
- 230000036541 health Effects 0.000 description 2
- QAOWNCQODCNURD-UHFFFAOYSA-M hydrogensulfate Chemical compound OS([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-M 0.000 description 2
- 102000018358 immunoglobulin Human genes 0.000 description 2
- 229960004078 indacaterol Drugs 0.000 description 2
- QZZUEBNBZAPZLX-QFIPXVFZSA-N indacaterol Chemical compound N1C(=O)C=CC2=C1C(O)=CC=C2[C@@H](O)CNC1CC(C=C(C(=C2)CC)CC)=C2C1 QZZUEBNBZAPZLX-QFIPXVFZSA-N 0.000 description 2
- 230000002757 inflammatory effect Effects 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 238000010902 jet-milling Methods 0.000 description 2
- 210000000867 larynx Anatomy 0.000 description 2
- 239000003591 leukocyte elastase inhibitor Substances 0.000 description 2
- 238000004895 liquid chromatography mass spectrometry Methods 0.000 description 2
- 230000007774 longterm 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
- 238000000691 measurement method Methods 0.000 description 2
- 229940071648 metered dose inhaler Drugs 0.000 description 2
- 238000010327 methods by industry Methods 0.000 description 2
- 150000004682 monohydrates Chemical class 0.000 description 2
- 210000000214 mouth Anatomy 0.000 description 2
- 229940092253 ovalbumin Drugs 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- 210000003800 pharynx Anatomy 0.000 description 2
- 108010010907 pitrakinra Proteins 0.000 description 2
- 229950008185 pitrakinra Drugs 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- 102000005962 receptors Human genes 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 238000011084 recovery Methods 0.000 description 2
- 238000004007 reversed phase HPLC Methods 0.000 description 2
- 159000000000 sodium salts Chemical class 0.000 description 2
- 239000012453 solvate Substances 0.000 description 2
- 238000000935 solvent evaporation Methods 0.000 description 2
- 238000010183 spectrum analysis Methods 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
- 210000000115 thoracic cavity Anatomy 0.000 description 2
- 210000003437 trachea Anatomy 0.000 description 2
- 230000003519 ventilatory effect Effects 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
- UCTWMZQNUQWSLP-VIFPVBQESA-N (R)-adrenaline Chemical compound CNC[C@H](O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-VIFPVBQESA-N 0.000 description 1
- 229930182837 (R)-adrenaline Natural products 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
- ABEXEQSGABRUHS-UHFFFAOYSA-N 16-methylheptadecyl 16-methylheptadecanoate Chemical compound CC(C)CCCCCCCCCCCCCCCOC(=O)CCCCCCCCCCCCCCC(C)C ABEXEQSGABRUHS-UHFFFAOYSA-N 0.000 description 1
- YREYLAVBNPACJM-UHFFFAOYSA-N 2-(tert-butylamino)-1-(2-chlorophenyl)ethanol Chemical compound CC(C)(C)NCC(O)C1=CC=CC=C1Cl YREYLAVBNPACJM-UHFFFAOYSA-N 0.000 description 1
- RYWCQJDEHXJHRI-XJMXIVSISA-N 2-[3-[5-[6-[3-[3-(carboxymethyl)phenyl]-4-[(2r,3s,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyphenyl]hexyl]-2-[(2r,3s,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyphenyl]phenyl]acetic acid Chemical compound O[C@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC(C(=C1)C=2C=C(CC(O)=O)C=CC=2)=CC=C1CCCCCCC(C=C1C=2C=C(CC(O)=O)C=CC=2)=CC=C1O[C@@H]1[C@@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 RYWCQJDEHXJHRI-XJMXIVSISA-N 0.000 description 1
- JWYIGNODXSRKGP-UHFFFAOYSA-N 2-[4-acetamido-3-(4-chlorophenyl)sulfanyl-2-methylindol-1-yl]acetic acid Chemical compound C1=2C(NC(=O)C)=CC=CC=2N(CC(O)=O)C(C)=C1SC1=CC=C(Cl)C=C1 JWYIGNODXSRKGP-UHFFFAOYSA-N 0.000 description 1
- AFTCWZSEWTXWTL-BTQNPOSSSA-N 2-hydroxy-n,n-dimethyl-3-[[2-[[(1r)-1-(5-methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobuten-1-yl]amino]benzamide;hydrate Chemical compound O.N([C@H](CC)C=1OC(C)=CC=1)C(C(C1=O)=O)=C1NC1=CC=CC(C(=O)N(C)C)=C1O AFTCWZSEWTXWTL-BTQNPOSSSA-N 0.000 description 1
- DVSPHWCZXKPJEQ-UHFFFAOYSA-N 2-methoxyethyl(trimethyl)azanium Chemical compound COCC[N+](C)(C)C DVSPHWCZXKPJEQ-UHFFFAOYSA-N 0.000 description 1
- IHOXNOQMRZISPV-YJYMSZOUSA-N 5-[(1r)-1-hydroxy-2-[[(2r)-1-(4-methoxyphenyl)propan-2-yl]azaniumyl]ethyl]-2-oxo-1h-quinolin-8-olate Chemical compound C1=CC(OC)=CC=C1C[C@@H](C)NC[C@H](O)C1=CC=C(O)C2=C1C=CC(=O)N2 IHOXNOQMRZISPV-YJYMSZOUSA-N 0.000 description 1
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.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 WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 description 1
- 229940122065 Alpha4beta7 integrin antagonist Drugs 0.000 description 1
- 208000035143 Bacterial infection Diseases 0.000 description 1
- 229940123321 Beta1 integrin antagonist Drugs 0.000 description 1
- 241000588832 Bordetella pertussis Species 0.000 description 1
- 206010006482 Bronchospasm Diseases 0.000 description 1
- 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 description 1
- 101710149863 C-C chemokine receptor type 4 Proteins 0.000 description 1
- 102100021942 C-C motif chemokine 28 Human genes 0.000 description 1
- 102100032367 C-C motif chemokine 5 Human genes 0.000 description 1
- 102100028989 C-X-C chemokine receptor type 2 Human genes 0.000 description 1
- 102100039435 C-X-C motif chemokine 17 Human genes 0.000 description 1
- 108010040471 CC Chemokines Proteins 0.000 description 1
- 102000001902 CC Chemokines Human genes 0.000 description 1
- 102100032976 CCR4-NOT transcription complex subunit 6 Human genes 0.000 description 1
- 229940124803 CXCR2 antagonist Drugs 0.000 description 1
- 101100136727 Caenorhabditis elegans psd-1 gene Proteins 0.000 description 1
- 108010055166 Chemokine CCL5 Proteins 0.000 description 1
- 241001647372 Chlamydia pneumoniae Species 0.000 description 1
- 208000017667 Chronic Disease Diseases 0.000 description 1
- 241000223205 Coccidioides immitis Species 0.000 description 1
- 241000711573 Coronaviridae Species 0.000 description 1
- 241000709687 Coxsackievirus Species 0.000 description 1
- 201000007336 Cryptococcosis Diseases 0.000 description 1
- 241000221204 Cryptococcus neoformans Species 0.000 description 1
- 102000004127 Cytokines Human genes 0.000 description 1
- 108090000695 Cytokines Proteins 0.000 description 1
- 241000701022 Cytomegalovirus Species 0.000 description 1
- 241001466953 Echovirus Species 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 241000709661 Enterovirus Species 0.000 description 1
- 102000009024 Epidermal Growth Factor Human genes 0.000 description 1
- 241000588724 Escherichia coli Species 0.000 description 1
- 108010008165 Etanercept Proteins 0.000 description 1
- 206010017533 Fungal infection Diseases 0.000 description 1
- 241001427367 Gardena Species 0.000 description 1
- 108010017213 Granulocyte-Macrophage Colony-Stimulating Factor Proteins 0.000 description 1
- 102100039620 Granulocyte-macrophage colony-stimulating factor Human genes 0.000 description 1
- 102100034221 Growth-regulated alpha protein Human genes 0.000 description 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 description 1
- 241000606768 Haemophilus influenzae Species 0.000 description 1
- 241000606766 Haemophilus parainfluenzae Species 0.000 description 1
- 241000228404 Histoplasma capsulatum Species 0.000 description 1
- 101000897480 Homo sapiens C-C motif chemokine 2 Proteins 0.000 description 1
- 101000897477 Homo sapiens C-C motif chemokine 28 Proteins 0.000 description 1
- 101000889048 Homo sapiens C-X-C motif chemokine 17 Proteins 0.000 description 1
- 101001069921 Homo sapiens Growth-regulated alpha protein Proteins 0.000 description 1
- 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 1
- 238000012695 Interfacial polymerization Methods 0.000 description 1
- 102100026720 Interferon beta Human genes 0.000 description 1
- 108010047761 Interferon-alpha Proteins 0.000 description 1
- 102000006992 Interferon-alpha Human genes 0.000 description 1
- 108090000467 Interferon-beta Proteins 0.000 description 1
- 108010002352 Interleukin-1 Proteins 0.000 description 1
- 102000000589 Interleukin-1 Human genes 0.000 description 1
- 102100026018 Interleukin-1 receptor antagonist protein Human genes 0.000 description 1
- 101710144554 Interleukin-1 receptor antagonist protein Proteins 0.000 description 1
- 102000000588 Interleukin-2 Human genes 0.000 description 1
- 108010002350 Interleukin-2 Proteins 0.000 description 1
- 102000010786 Interleukin-5 Receptors Human genes 0.000 description 1
- 108010038484 Interleukin-5 Receptors Proteins 0.000 description 1
- 108090001005 Interleukin-6 Proteins 0.000 description 1
- 102000004889 Interleukin-6 Human genes 0.000 description 1
- 108090001007 Interleukin-8 Proteins 0.000 description 1
- 108010018951 Interleukin-8B Receptors Proteins 0.000 description 1
- 241000764238 Isis Species 0.000 description 1
- RMSWMRJVUJSDGN-GOSISDBHSA-N Israpafant Chemical compound C1=CC(CC(C)C)=CC=C1CCC1=CC(C(=N[C@H](C)C2=NN=C(C)N22)C=3C(=CC=CC=3)Cl)=C2S1 RMSWMRJVUJSDGN-GOSISDBHSA-N 0.000 description 1
- 238000003109 Karl Fischer titration Methods 0.000 description 1
- 102100020880 Kit ligand Human genes 0.000 description 1
- 101710177504 Kit ligand Proteins 0.000 description 1
- 241000588747 Klebsiella pneumoniae Species 0.000 description 1
- 239000004395 L-leucine Substances 0.000 description 1
- 235000019454 L-leucine Nutrition 0.000 description 1
- 241000589242 Legionella pneumophila Species 0.000 description 1
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 description 1
- 241000989747 Maba Species 0.000 description 1
- 241000948268 Meda Species 0.000 description 1
- 101710151803 Mitochondrial intermediate peptidase 2 Proteins 0.000 description 1
- 241000588655 Moraxella catarrhalis Species 0.000 description 1
- 229940122424 Muscarinic antagonist-beta 2 agonist (MABA) Drugs 0.000 description 1
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 description 1
- 241000187479 Mycobacterium tuberculosis Species 0.000 description 1
- 241000202934 Mycoplasma pneumoniae Species 0.000 description 1
- 208000031888 Mycoses Diseases 0.000 description 1
- 102000015336 Nerve Growth Factor Human genes 0.000 description 1
- 108010025020 Nerve Growth Factor Proteins 0.000 description 1
- 102100033174 Neutrophil elastase Human genes 0.000 description 1
- 108010042215 OX40 Ligand Proteins 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 208000002606 Paramyxoviridae Infections Diseases 0.000 description 1
- 229940099471 Phosphodiesterase inhibitor Drugs 0.000 description 1
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 description 1
- VQDBNKDJNJQRDG-UHFFFAOYSA-N Pirbuterol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=N1 VQDBNKDJNJQRDG-UHFFFAOYSA-N 0.000 description 1
- 241000142787 Pneumocystis jirovecii Species 0.000 description 1
- 239000004698 Polyethylene Substances 0.000 description 1
- 239000004793 Polystyrene Substances 0.000 description 1
- 102100022364 Polyunsaturated fatty acid 5-lipoxygenase Human genes 0.000 description 1
- 101710156627 Polyunsaturated fatty acid 5-lipoxygenase Proteins 0.000 description 1
- 101710098940 Pro-epidermal growth factor Proteins 0.000 description 1
- 241000589517 Pseudomonas aeruginosa Species 0.000 description 1
- 208000002200 Respiratory Hypersensitivity Diseases 0.000 description 1
- 241001246910 Saba Species 0.000 description 1
- 102000003800 Selectins Human genes 0.000 description 1
- 108090000184 Selectins Proteins 0.000 description 1
- 206010070834 Sensitisation Diseases 0.000 description 1
- 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 description 1
- 241000607715 Serratia marcescens Species 0.000 description 1
- 108020004459 Small interfering RNA Proteins 0.000 description 1
- 241000191967 Staphylococcus aureus Species 0.000 description 1
- 241000193985 Streptococcus agalactiae Species 0.000 description 1
- 241000193998 Streptococcus pneumoniae Species 0.000 description 1
- 102000000551 Syk Kinase Human genes 0.000 description 1
- 108010016672 Syk Kinase Proteins 0.000 description 1
- 230000006044 T cell activation Effects 0.000 description 1
- 210000001744 T-lymphocyte Anatomy 0.000 description 1
- 241000223997 Toxoplasma gondii Species 0.000 description 1
- 102000004887 Transforming Growth Factor beta Human genes 0.000 description 1
- 108090001012 Transforming Growth Factor beta Proteins 0.000 description 1
- 102100026890 Tumor necrosis factor ligand superfamily member 4 Human genes 0.000 description 1
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 description 1
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 description 1
- 208000036142 Viral infection Diseases 0.000 description 1
- URWYQGVSPQJGGB-DHUJRADRSA-N [1-[3-[2-chloro-4-[[[(2r)-2-hydroxy-2-(8-hydroxy-2-oxo-1h-quinolin-5-yl)ethyl]amino]methyl]-5-methoxyanilino]-3-oxopropyl]piperidin-4-yl] n-(2-phenylphenyl)carbamate Chemical compound ClC=1C=C(CNC[C@H](O)C=2C=3C=CC(=O)NC=3C(O)=CC=2)C(OC)=CC=1NC(=O)CCN(CC1)CCC1OC(=O)NC1=CC=CC=C1C1=CC=CC=C1 URWYQGVSPQJGGB-DHUJRADRSA-N 0.000 description 1
- 208000038016 acute inflammation Diseases 0.000 description 1
- 230000006022 acute inflammation Effects 0.000 description 1
- 239000000971 adrenergic beta-2 receptor antagonist Substances 0.000 description 1
- 230000010085 airway hyperresponsiveness Effects 0.000 description 1
- 208000037883 airway inflammation Diseases 0.000 description 1
- NDAUXUAQIAJITI-UHFFFAOYSA-N albuterol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=C1 NDAUXUAQIAJITI-UHFFFAOYSA-N 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- 125000000217 alkyl group Chemical group 0.000 description 1
- 229940045714 alkyl sulfonate alkylating agent Drugs 0.000 description 1
- 239000013566 allergen Substances 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- SGRYPYWGNKJSDL-UHFFFAOYSA-N amlexanox Chemical compound NC1=C(C(O)=O)C=C2C(=O)C3=CC(C(C)C)=CC=C3OC2=N1 SGRYPYWGNKJSDL-UHFFFAOYSA-N 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 208000022362 bacterial infectious disease Diseases 0.000 description 1
- 229960003060 bambuterol Drugs 0.000 description 1
- 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 description 1
- 229940092705 beclomethasone Drugs 0.000 description 1
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical class OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 description 1
- 229940125388 beta agonist Drugs 0.000 description 1
- 230000001588 bifunctional effect Effects 0.000 description 1
- 229950007225 bimosiamose Drugs 0.000 description 1
- 238000007664 blowing Methods 0.000 description 1
- 230000007885 bronchoconstriction Effects 0.000 description 1
- 229960004436 budesonide Drugs 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 229950010713 carmoterol Drugs 0.000 description 1
- 230000005754 cellular signaling Effects 0.000 description 1
- 238000005119 centrifugation Methods 0.000 description 1
- 239000000812 cholinergic antagonist Substances 0.000 description 1
- 230000001713 cholinergic effect Effects 0.000 description 1
- 208000037976 chronic inflammation Diseases 0.000 description 1
- 230000006020 chronic inflammation Effects 0.000 description 1
- 229960001117 clenbuterol Drugs 0.000 description 1
- STJMRWALKKWQGH-UHFFFAOYSA-N clenbuterol Chemical compound CC(C)(C)NCC(O)C1=CC(Cl)=C(N)C(Cl)=C1 STJMRWALKKWQGH-UHFFFAOYSA-N 0.000 description 1
- 238000005354 coacervation Methods 0.000 description 1
- 239000011362 coarse particle Substances 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 239000006184 cosolvent Substances 0.000 description 1
- 230000000139 costimulatory effect Effects 0.000 description 1
- 238000003869 coulometry Methods 0.000 description 1
- 229960000265 cromoglicic acid Drugs 0.000 description 1
- 238000001739 density measurement Methods 0.000 description 1
- 238000013461 design Methods 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 229960003957 dexamethasone Drugs 0.000 description 1
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 description 1
- 229910001873 dinitrogen Inorganic materials 0.000 description 1
- VLARUOGDXDTHEH-UHFFFAOYSA-L disodium cromoglycate Chemical compound [Na+].[Na+].O1C(C([O-])=O)=CC(=O)C2=C1C=CC=C2OCC(O)COC1=CC=CC2=C1C(=O)C=C(C([O-])=O)O2 VLARUOGDXDTHEH-UHFFFAOYSA-L 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 230000005684 electric field Effects 0.000 description 1
- 229940073621 enbrel Drugs 0.000 description 1
- 229960005139 epinephrine Drugs 0.000 description 1
- QTTMOCOWZLSYSV-QWAPEVOJSA-M equilin sodium sulfate Chemical compound [Na+].[O-]S(=O)(=O)OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4C3=CCC2=C1 QTTMOCOWZLSYSV-QWAPEVOJSA-M 0.000 description 1
- HVCNNTAUBZIYCG-UHFFFAOYSA-N ethyl 2-[4-[(6-chloro-1,3-benzothiazol-2-yl)oxy]phenoxy]propanoate Chemical compound C1=CC(OC(C)C(=O)OCC)=CC=C1OC1=NC2=CC=C(Cl)C=C2S1 HVCNNTAUBZIYCG-UHFFFAOYSA-N 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 229960000676 flunisolide Drugs 0.000 description 1
- 229960002848 formoterol Drugs 0.000 description 1
- 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 description 1
- 229940021598 formoterol and budesonide Drugs 0.000 description 1
- 229940021593 formoterol and fluticasone Drugs 0.000 description 1
- 229940021608 formoterol and mometasone Drugs 0.000 description 1
- 238000004108 freeze drying Methods 0.000 description 1
- 238000012388 gravitational sedimentation Methods 0.000 description 1
- 239000003102 growth factor Substances 0.000 description 1
- 229940047650 haemophilus influenzae Drugs 0.000 description 1
- 210000003128 head Anatomy 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 230000002209 hydrophobic effect Effects 0.000 description 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 description 1
- 238000001119 image correlation spectroscopy Methods 0.000 description 1
- 238000005417 image-selected in vivo spectroscopy Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 230000004968 inflammatory condition Effects 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 238000012739 integrated shape imaging system Methods 0.000 description 1
- 238000001361 intraarterial administration Methods 0.000 description 1
- 238000010255 intramuscular injection Methods 0.000 description 1
- 239000007927 intramuscular injection Substances 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 230000001788 irregular Effects 0.000 description 1
- 238000010829 isocratic elution Methods 0.000 description 1
- 229940039009 isoproterenol Drugs 0.000 description 1
- 229950005222 israpafant Drugs 0.000 description 1
- 229960001021 lactose monohydrate Drugs 0.000 description 1
- 229950002183 lebrikizumab Drugs 0.000 description 1
- 229940115932 legionella pneumophila Drugs 0.000 description 1
- YEESKJGWJFYOOK-IJHYULJSSA-N leukotriene D4 Chemical compound CCCCC\C=C/C\C=C/C=C/C=C/[C@H]([C@@H](O)CCCC(O)=O)SC[C@H](N)C(=O)NCC(O)=O YEESKJGWJFYOOK-IJHYULJSSA-N 0.000 description 1
- 239000003199 leukotriene receptor blocking agent Substances 0.000 description 1
- 229950008204 levosalbutamol Drugs 0.000 description 1
- 229960004194 lidocaine Drugs 0.000 description 1
- 229950003265 losmapimod Drugs 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- JHPHVAVFUYTVCL-UHFFFAOYSA-M methacholine chloride Chemical compound [Cl-].C[N+](C)(C)CC(C)OC(C)=O JHPHVAVFUYTVCL-UHFFFAOYSA-M 0.000 description 1
- 229960002931 methacholine chloride Drugs 0.000 description 1
- 239000003094 microcapsule Substances 0.000 description 1
- 239000004005 microsphere Substances 0.000 description 1
- 238000003801 milling Methods 0.000 description 1
- 229950001768 milveterol Drugs 0.000 description 1
- 230000003278 mimic effect Effects 0.000 description 1
- 239000003226 mitogen Substances 0.000 description 1
- 239000011259 mixed solution Substances 0.000 description 1
- BMKINZUHKYLSKI-DQEYMECFSA-N n-[2-hydroxy-5-[(1r)-1-hydroxy-2-[2-[4-[[(2r)-2-hydroxy-2-phenylethyl]amino]phenyl]ethylamino]ethyl]phenyl]formamide Chemical compound C1([C@@H](O)CNC2=CC=C(C=C2)CCNC[C@H](O)C=2C=C(NC=O)C(O)=CC=2)=CC=CC=C1 BMKINZUHKYLSKI-DQEYMECFSA-N 0.000 description 1
- OHDXDNUPVVYWOV-UHFFFAOYSA-N n-methyl-1-(2-naphthalen-1-ylsulfanylphenyl)methanamine Chemical compound CNCC1=CC=CC=C1SC1=CC=CC2=CC=CC=C12 OHDXDNUPVVYWOV-UHFFFAOYSA-N 0.000 description 1
- 239000002105 nanoparticle Substances 0.000 description 1
- 210000003928 nasal cavity Anatomy 0.000 description 1
- 239000007923 nasal drop Substances 0.000 description 1
- 229940100662 nasal drops Drugs 0.000 description 1
- 238000002663 nebulization Methods 0.000 description 1
- 229960000470 omalizumab Drugs 0.000 description 1
- 238000005457 optimization Methods 0.000 description 1
- 210000003300 oropharynx Anatomy 0.000 description 1
- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 description 1
- 239000006174 pH buffer Substances 0.000 description 1
- 230000008506 pathogenesis Effects 0.000 description 1
- 238000005191 phase separation Methods 0.000 description 1
- JTJMJGYZQZDUJJ-UHFFFAOYSA-N phencyclidine Chemical class C1CCCCN1C1(C=2C=CC=CC=2)CCCCC1 JTJMJGYZQZDUJJ-UHFFFAOYSA-N 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 239000002571 phosphodiesterase inhibitor Substances 0.000 description 1
- 229910052698 phosphorus Inorganic materials 0.000 description 1
- 239000011574 phosphorus Substances 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 229920002223 polystyrene Polymers 0.000 description 1
- 229960002288 procaterol Drugs 0.000 description 1
- FKNXQNWAXFXVNW-BLLLJJGKSA-N procaterol Chemical compound N1C(=O)C=CC2=C1C(O)=CC=C2[C@@H](O)[C@@H](NC(C)C)CC FKNXQNWAXFXVNW-BLLLJJGKSA-N 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 229940072288 prograf Drugs 0.000 description 1
- AAEVYOVXGOFMJO-UHFFFAOYSA-N prometryn Chemical compound CSC1=NC(NC(C)C)=NC(NC(C)C)=N1 AAEVYOVXGOFMJO-UHFFFAOYSA-N 0.000 description 1
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 description 1
- 239000003909 protein kinase inhibitor Substances 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- MIXMJCQRHVAJIO-TZHJZOAOSA-N qk4dys664x Chemical compound O.C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O.C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O MIXMJCQRHVAJIO-TZHJZOAOSA-N 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 238000007634 remodeling Methods 0.000 description 1
- KQDRVXQXKZXMHP-LLVKDONJSA-N reparixin Chemical compound CC(C)CC1=CC=C([C@@H](C)C(=O)NS(C)(=O)=O)C=C1 KQDRVXQXKZXMHP-LLVKDONJSA-N 0.000 description 1
- 229950005650 reparixin Drugs 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 239000013557 residual solvent Substances 0.000 description 1
- 230000004202 respiratory function Effects 0.000 description 1
- 230000029058 respiratory gaseous exchange Effects 0.000 description 1
- 229960002052 salbutamol Drugs 0.000 description 1
- 229960004017 salmeterol Drugs 0.000 description 1
- 229940021597 salmeterol and fluticasone Drugs 0.000 description 1
- 238000013515 script Methods 0.000 description 1
- 230000008313 sensitization Effects 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 230000000405 serological effect Effects 0.000 description 1
- 229940127211 short-acting beta 2 agonist Drugs 0.000 description 1
- 238000007873 sieving Methods 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 229940055944 soliris Drugs 0.000 description 1
- 238000000638 solvent extraction Methods 0.000 description 1
- 238000001228 spectrum Methods 0.000 description 1
- 238000013125 spirometry Methods 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 229940031000 streptococcus pneumoniae Drugs 0.000 description 1
- 238000010254 subcutaneous injection Methods 0.000 description 1
- 239000007929 subcutaneous injection Substances 0.000 description 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 1
- 239000013589 supplement Substances 0.000 description 1
- 238000001308 synthesis method Methods 0.000 description 1
- NWJQLQGQZSIBAF-MLAUYUEBSA-N tacrolimus hydrate Chemical compound O.C1C[C@@H](O)[C@H](OC)C[C@@H]1\C=C(/C)[C@@H]1[C@H](C)[C@@H](O)CC(=O)[C@H](CC=C)/C=C(C)/C[C@H](C)C[C@H](OC)[C@H]([C@H](C[C@H]2C)OC)O[C@@]2(O)C(=O)C(=O)N2CCCC[C@H]2C(=O)O1 NWJQLQGQZSIBAF-MLAUYUEBSA-N 0.000 description 1
- ZRKFYGHZFMAOKI-QMGMOQQFSA-N tgfbeta Chemical compound C([C@H](NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCSC)C(C)C)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(O)=O)C1=CC=C(O)C=C1 ZRKFYGHZFMAOKI-QMGMOQQFSA-N 0.000 description 1
- 238000002076 thermal analysis method Methods 0.000 description 1
- 238000004448 titration Methods 0.000 description 1
- 230000000699 topical effect Effects 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
- 229960000859 tulobuterol Drugs 0.000 description 1
- 238000000825 ultraviolet detection Methods 0.000 description 1
- 241000701161 unidentified adenovirus Species 0.000 description 1
- 241001529453 unidentified herpesvirus Species 0.000 description 1
- 241000712461 unidentified influenza virus Species 0.000 description 1
- 230000009385 viral infection Effects 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
- 231100000054 whole-body exposure Toxicity 0.000 description 1
- MWLSOWXNZPKENC-UHFFFAOYSA-N zileuton Chemical compound C1=CC=C2SC(C(N(O)C(N)=O)C)=CC2=C1 MWLSOWXNZPKENC-UHFFFAOYSA-N 0.000 description 1
- 229940052267 zyflo Drugs 0.000 description 1
Images
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1611—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Otolaryngology (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361807063P | 2013-04-01 | 2013-04-01 | |
| US61/807,063 | 2013-04-01 | ||
| US201361874146P | 2013-09-05 | 2013-09-05 | |
| US61/874,146 | 2013-09-05 | ||
| US201461925400P | 2014-01-09 | 2014-01-09 | |
| US61/925,400 | 2014-01-09 | ||
| PCT/US2014/025660 WO2014165303A1 (en) | 2013-04-01 | 2014-03-13 | Tiotropium dry powders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016515576A JP2016515576A (ja) | 2016-05-30 |
| JP2016515576A5 JP2016515576A5 (enExample) | 2017-04-20 |
| JP6473738B2 true JP6473738B2 (ja) | 2019-02-20 |
Family
ID=50693973
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016505482A Active JP6473738B2 (ja) | 2013-04-01 | 2014-03-13 | チオトロピウム乾燥粉末 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US9737518B2 (enExample) |
| EP (1) | EP2981247B1 (enExample) |
| JP (1) | JP6473738B2 (enExample) |
| KR (1) | KR20150135328A (enExample) |
| CN (1) | CN105324106A (enExample) |
| AU (1) | AU2014248455B2 (enExample) |
| CA (1) | CA2907566C (enExample) |
| HK (1) | HK1221175A1 (enExample) |
| MX (1) | MX2015013845A (enExample) |
| RU (1) | RU2015146871A (enExample) |
| WO (1) | WO2014165303A1 (enExample) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NO2699580T3 (enExample) | 2014-01-24 | 2018-02-24 | ||
| WO2016057641A1 (en) * | 2014-10-08 | 2016-04-14 | Pulmatrix Operating Company, Inc. | Formulations containing tiotropium, amino acid and acid and methods thereof |
| WO2017068108A1 (en) * | 2015-10-23 | 2017-04-27 | Arven Ilac Sanayi Ve Ticaret A.S. | Blister for inhalable formulation of tiotropium bromide |
| KR20240091302A (ko) * | 2016-07-29 | 2024-06-21 | 인스메드 인코포레이티드 | 기관지확장증을 치료하기 위한 특정 (2s)-n-[(1s)-1-시아노-2-페닐에틸]-1,4-옥사제판-2-카르복스아미드 |
| NZ752353A (en) * | 2016-10-14 | 2023-06-30 | Pulmatrix Operating Co Inc | Antifungal dry powders |
| EP3692144A1 (en) * | 2017-10-05 | 2020-08-12 | Fulcrum Therapeutics, Inc. | Use of p38 inhibitors to reduce expression of dux4 |
| PT3505157T (pt) * | 2017-12-29 | 2022-02-18 | Celon Pharma Sa | Composição de cetamina em pó seco para administração pulmonar em depressão resistente ao tratamento |
| WO2019163520A1 (ja) * | 2018-02-26 | 2019-08-29 | 株式会社新日本科学 | 粉末製剤、カートリッジ、及びデバイス |
| AU2019228717C1 (en) | 2018-03-01 | 2025-01-09 | Astrazeneca Ab | Pharmaceutical compositions comprising (2S)-N-{(1S)-1-cyano-2-[4-(3-methyl-2- oxo-2,3-dihydro-1,3-benzoxazol-5-yl)phenyl]ethyl}-1,4-oxazepane-2-carboxamide |
| CA3106269A1 (en) | 2018-07-17 | 2020-01-23 | Insmed Incorporated | Certain (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides for treating lupus nephritis |
| WO2020096686A2 (en) | 2018-09-05 | 2020-05-14 | Sensory Cloud, Llc | Formulations and compositions for ortho- and/or retro-nasal delivery and associated systems, methods and articles |
| CN110161142A (zh) * | 2019-06-11 | 2019-08-23 | 珠海瑞思普利生物制药有限公司 | 一种表征干粉吸入制剂在呼吸系统空气动力学的仿真装置 |
| BE1027612B1 (fr) * | 2019-09-10 | 2021-05-03 | Aquilon Pharmaceuticals | Microparticules en forme de balle de golf pour une utilisation dans le traitement et la prevention de maladies pulmonaires |
| JP2024510564A (ja) * | 2021-03-03 | 2024-03-08 | パルマトリックス オペレーティング カンパニー，インコーポレイテッド | ジヒドロエルゴタミン乾燥粉末製剤及びその使用方法 |
| EP4108230A1 (en) * | 2021-06-24 | 2022-12-28 | Laboratoires SMB | New dry powder composition of tiotropium for inhalation |
| CN114272228B (zh) * | 2022-01-04 | 2023-08-22 | 丽珠医药集团股份有限公司 | 噻托溴铵吸入微球及其制备方法和吸入式制剂 |
| CN120584108A (zh) | 2023-01-06 | 2025-09-02 | 英斯梅德股份有限公司 | 新型可逆dpp1抑制剂及其用途 |
| CN117233286A (zh) * | 2023-09-19 | 2023-12-15 | 南京力成药业有限公司 | 一种噻托溴铵的定量检测方法 |
Family Cites Families (197)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1575050A1 (de) | 1966-01-12 | 1972-04-13 | Misto Gen Equipment Co | Ultraschall-Nebelerzeugungsgeraet |
| US4069819A (en) | 1973-04-13 | 1978-01-24 | Societa Farmaceutici S.P.A. | Inhalation device |
| US4085893A (en) | 1974-03-20 | 1978-04-25 | Durley Iii Benton A | Ultrasonic humidifiers, atomizers and the like |
| US4193009A (en) | 1976-01-26 | 1980-03-11 | Durley Benton A Iii | Ultrasonic piezoelectric transducer using a rubber mounting |
| JPS5550437U (enExample) | 1978-09-28 | 1980-04-02 | ||
| US4233405A (en) | 1979-10-10 | 1980-11-11 | Rohm And Haas Company | Process for spray drying enzymes |
| DE3229179C2 (de) | 1982-08-05 | 1986-04-17 | A. Nattermann & Cie GmbH, 5000 Köln | Lungensurfactant |
| US4643351A (en) | 1984-06-14 | 1987-02-17 | Tokyo Sanyo Electric Co. | Ultrasonic humidifier |
| US4637815A (en) | 1985-08-06 | 1987-01-20 | Lemole Gerald M | Irrigational hemostatic solution |
| FI82808C (fi) | 1987-12-31 | 1991-04-25 | Etelae Haemeen Keuhkovammayhdi | Ultraljudfinfoerdelningsanordning. |
| US4899914A (en) | 1988-11-04 | 1990-02-13 | Ciba-Geigy Corporation | Method for producing a sterile preservative-free aerosol saline solution |
| US4921639A (en) | 1988-11-09 | 1990-05-01 | Bernard Chiu | Ultrasonic humidifier |
| US4881541A (en) | 1988-12-21 | 1989-11-21 | The Regents Of The University Of California | Vaporizer for an anesthetic having a vapor pressure about one atmosphere |
| IT1228459B (it) | 1989-02-23 | 1991-06-19 | Phidea S R L | Inalatore con svuotamento regolare e completo della capsula. |
| DE3931041C2 (de) | 1989-09-16 | 2000-04-06 | Boehringer Ingelheim Kg | Ester von Thienylcarbonsäuren mit Aminoalkoholen, ihre Quaternierungsprodukte, Verfahren zu ihrer Herstellung und diese enthaltende Arzneimittel |
| US5610163A (en) | 1989-09-16 | 1997-03-11 | Boehringer Ingelheim Gmbh | Esters of thienyl carboxylic acids and amino alcohols and their quaternization products |
| US5230884A (en) | 1990-09-11 | 1993-07-27 | University Of Wales College Of Cardiff | Aerosol formulations including proteins and peptides solubilized in reverse micelles and process for making the aerosol formulations |
| US5175152A (en) | 1990-09-28 | 1992-12-29 | Singh Nikhilesh N | Composition containing ephedrine base and alkyl salicylate for the delivery of ephedrine base in vapor form |
| US5211944A (en) | 1990-10-12 | 1993-05-18 | Shaman Pharmaceuticals, Inc. | Proanthocyanidin polymers having antiviral activity and methods of obtaining same |
| US5571535A (en) | 1990-11-30 | 1996-11-05 | Flowers; Marianne | Treatment of topical infections |
| EP0940154B1 (en) | 1991-07-02 | 2007-04-18 | Nektar Therapeutics | Device for delivering aerosolized medicaments |
| JPH05123398A (ja) | 1991-11-06 | 1993-05-21 | Tsunemasa Kamiyama | 咽喉保護吸入剤並びに吸入器具 |
| GB2265845B (en) | 1991-11-12 | 1996-05-01 | Medix Ltd | A nebuliser and nebuliser control system |
| US5466680A (en) | 1992-03-26 | 1995-11-14 | Cytologics, Inc. | Method and compositions for enhancing white blood cell functioning on a mucosal or cutaneous surface |
| JP3961029B2 (ja) | 1992-06-24 | 2007-08-15 | 博 木戸 | インフルエンザウィルス感染防止剤 |
| US6582728B1 (en) | 1992-07-08 | 2003-06-24 | Inhale Therapeutic Systems, Inc. | Spray drying of macromolecules to produce inhaleable dry powders |
| US5785049A (en) | 1994-09-21 | 1998-07-28 | Inhale Therapeutic Systems | Method and apparatus for dispersion of dry powder medicaments |
| US5898037A (en) | 1992-11-13 | 1999-04-27 | Marx; Alvin J. | Formulations of magnesium compounds for local application and methods of treatment using the same |
| US5709202A (en) | 1993-05-21 | 1998-01-20 | Aradigm Corporation | Intrapulmonary delivery of aerosolized formulations |
| NZ328476A (en) | 1993-06-24 | 1999-05-28 | Astra Ab | Use of a two component insulin preparation in an inhalation device |
| US5514665A (en) | 1993-12-30 | 1996-05-07 | University Of British Columbia | Method of preventing or reducing the risk of infection by bacterial pathogens utilizing simple and conjugated dextrans |
| AUPM411494A0 (en) | 1994-02-25 | 1994-03-24 | Central Sydney Area Health Service | Method and device for the provocation of upper or lower airway narrowing and/or the induction of sputum |
| US5633003A (en) | 1994-03-31 | 1997-05-27 | Cantor; Jerome O. | Use of intratracheally administered hyaluronic acid to ameliorate emphysema |
| JP3414539B2 (ja) | 1994-05-11 | 2003-06-09 | 有限会社ドット | 経鼻吸収用組成物 |
| US6290991B1 (en) | 1994-12-02 | 2001-09-18 | Quandrant Holdings Cambridge Limited | Solid dose delivery vehicle and methods of making same |
| US6586006B2 (en) | 1994-08-04 | 2003-07-01 | Elan Drug Delivery Limited | Solid delivery systems for controlled release of molecules incorporated therein and methods of making same |
| HUT77609A (hu) | 1994-10-14 | 1998-06-29 | Yamanouchi Pharmaceutical Co. Ltd. | Azolszármazékok, az ezeket tartalmazó gyógyszerkészítmények és a vegyületek intermedierjei |
| US5863563A (en) | 1994-10-20 | 1999-01-26 | Alphagene Inc. | Treatment of pulmonary conditions associated with insufficient secretion of surfactant |
| US5747002A (en) | 1995-04-05 | 1998-05-05 | Genentech, Inc. | Preparation of sodium chloride aerosol formulations |
| US5612053A (en) | 1995-04-07 | 1997-03-18 | Edward Mendell Co., Inc. | Controlled release insufflation carrier for medicaments |
| US6165463A (en) | 1997-10-16 | 2000-12-26 | Inhale Therapeutic Systems, Inc. | Dispersible antibody compositions and methods for their preparation and use |
| US6258341B1 (en) | 1995-04-14 | 2001-07-10 | Inhale Therapeutic Systems, Inc. | Stable glassy state powder formulations |
| US5654007A (en) | 1995-06-07 | 1997-08-05 | Inhale Therapeutic Systems | Methods and system for processing dispersible fine powders |
| GB9515182D0 (en) | 1995-07-24 | 1995-09-20 | Co Ordinated Drug Dev | Improvements in and relating to powders for use in dry powder inhalers |
| US5628984A (en) | 1995-07-31 | 1997-05-13 | University Of North Carolina At Chapel Hill | Method of detecting lung disease |
| US20050054682A1 (en) | 1996-01-04 | 2005-03-10 | Phillips Jeffrey O. | Pharmaceutical compositions comprising substituted benzimidazoles and methods of using same |
| GB9606677D0 (en) | 1996-03-29 | 1996-06-05 | Glaxo Wellcome Inc | Process and device |
| US6083922A (en) | 1996-04-02 | 2000-07-04 | Pathogenesis, Corp. | Method and a tobramycin aerosol formulation for treatment prevention and containment of tuberculosis |
| USRE37053E1 (en) | 1996-05-24 | 2001-02-13 | Massachusetts Institute Of Technology | Particles incorporating surfactants for pulmonary drug delivery |
| US5874064A (en) | 1996-05-24 | 1999-02-23 | Massachusetts Institute Of Technology | Aerodynamically light particles for pulmonary drug delivery |
| US6254854B1 (en) | 1996-05-24 | 2001-07-03 | The Penn Research Foundation | Porous particles for deep lung delivery |
| US5985309A (en) | 1996-05-24 | 1999-11-16 | Massachusetts Institute Of Technology | Preparation of particles for inhalation |
| US5855913A (en) | 1997-01-16 | 1999-01-05 | Massachusetts Instite Of Technology | Particles incorporating surfactants for pulmonary drug delivery |
| DE19653969A1 (de) | 1996-12-20 | 1998-06-25 | Boehringer Ingelheim Kg | Neue wässrige Arzneimittelzubereitung zur Erzeugung treibgasfreier Aerosole |
| US20030203036A1 (en) | 2000-03-17 | 2003-10-30 | Gordon Marc S. | Systems and processes for spray drying hydrophobic drugs with hydrophilic excipients |
| GB9707934D0 (en) | 1997-04-18 | 1997-06-04 | Danbiosyst Uk | Improved delivery of drugs to mucosal surfaces |
| US5881720A (en) | 1997-04-29 | 1999-03-16 | The Procter & Gamble Company | Method of delivering halotherapy |
| US6339075B1 (en) | 1997-06-30 | 2002-01-15 | The University Of British Columbia | Use of dextran and other polysaccharides to improve mucus clearance |
| US6565885B1 (en) | 1997-09-29 | 2003-05-20 | Inhale Therapeutic Systems, Inc. | Methods of spray drying pharmaceutical compositions |
| PL343438A1 (en) | 1998-04-08 | 2001-08-13 | Lilly Co Eli | Pulmonary and nasal delivery of raloxifene |
| US5883084A (en) | 1998-06-08 | 1999-03-16 | Clarion Pharmaceuticals Inc. | Treatment of respiratory diseases utilizing α-tocopheryl-phosphocholine |
| SE9802073D0 (sv) | 1998-06-11 | 1998-06-11 | Astra Ab | New use |
| FR2780285B1 (fr) | 1998-06-29 | 2001-10-05 | Goemar Lab Sa | Utilisation de solutions salines isoosmotiques, leur procede de preparation et medicaments anti-inflammatoires a base de ces solutions |
| US6333051B1 (en) | 1998-09-03 | 2001-12-25 | Supratek Pharma, Inc. | Nanogel networks and biological agent compositions thereof |
| US6428814B1 (en) | 1999-10-08 | 2002-08-06 | Elan Pharma International Ltd. | Bioadhesive nanoparticulate compositions having cationic surface stabilizers |
| GB9827145D0 (en) | 1998-12-09 | 1999-02-03 | Co Ordinated Drug Dev | Improvements in or relating to powders |
| JP3312216B2 (ja) | 1998-12-18 | 2002-08-05 | オムロン株式会社 | 噴霧装置 |
| US6926911B1 (en) | 1998-12-22 | 2005-08-09 | The University Of North Carolina At Chapel Hill | Compounds and methods for the treatment of airway diseases and for the delivery of airway drugs |
| US6355271B1 (en) | 1999-02-03 | 2002-03-12 | Biosante Pharmaceuticals, Inc. | Therapeutic calcium phosphate particles and methods of manufacture and use |
| EP1173245B1 (en) | 1999-05-03 | 2004-09-01 | Battelle Memorial Institute | Compositions for aerosolization and inhalation |
| US6858199B1 (en) | 2000-06-09 | 2005-02-22 | Advanced Inhalation Research, Inc. | High efficient delivery of a large therapeutic mass aerosol |
| EP1210069B1 (en) | 1999-08-25 | 2004-12-29 | Advanced Inhalation Research, Inc. | Large porous particles obtainable by spray-drying and suitable for pulmonary administration |
| US6749835B1 (en) | 1999-08-25 | 2004-06-15 | Advanced Inhalation Research, Inc. | Formulation for spray-drying large porous particles |
| US7678364B2 (en) | 1999-08-25 | 2010-03-16 | Alkermes, Inc. | Particles for inhalation having sustained release properties |
| ES2343124T3 (es) | 1999-10-29 | 2010-07-23 | Novartis Ag | Composiciones de polvo seco con dispersabilidad mejorada. |
| US6962151B1 (en) | 1999-11-05 | 2005-11-08 | Pari GmbH Spezialisten für effektive Inhalation | Inhalation nebulizer |
| AU772096B2 (en) | 2000-03-14 | 2004-04-08 | Sumika Enviro-Science Co., Ltd. | Method for denaturing allergens |
| SK284948B6 (sk) | 2000-04-06 | 2006-03-02 | Zentiva, A. S. | Liečivý prípravok s obsahom vápnika alebo zmesi vápnika a vitamínu D, alebo zmesi vápnika a horčíka v novej liekovej forme |
| GB0008660D0 (en) | 2000-04-07 | 2000-05-31 | Arakis Ltd | The treatment of respiratory diseases |
| US6637432B2 (en) | 2000-05-09 | 2003-10-28 | Iep Pharmaceutical Devices Inc. | Inhalation actuated device |
| PT1280520E (pt) | 2000-05-10 | 2014-12-16 | Novartis Ag | Pós à base de fosfolípidos para administração de fármacos |
| US7871598B1 (en) | 2000-05-10 | 2011-01-18 | Novartis Ag | Stable metal ion-lipid powdered pharmaceutical compositions for drug delivery and methods of use |
| EP2266549B1 (en) | 2000-06-27 | 2019-08-07 | Vectura Limited | Method of making particles for use in a pharmaceutical composition |
| US7575761B2 (en) | 2000-06-30 | 2009-08-18 | Novartis Pharma Ag | Spray drying process control of drying kinetics |
| US6669959B1 (en) | 2000-07-18 | 2003-12-30 | Aeropharm Technology Incorporated | Modulated release particles for lung delivery |
| WO2002009574A2 (en) | 2000-08-01 | 2002-02-07 | Shofner Engineering Associates, Inc. | Generation, delivery, measurement and control of aerosol boli for diagnostics and treatment of the respiratory tract |
| US6613308B2 (en) | 2000-09-19 | 2003-09-02 | Advanced Inhalation Research, Inc. | Pulmonary delivery in treating disorders of the central nervous system |
| WO2002024116A1 (en) | 2000-09-20 | 2002-03-28 | Shahinian, Lee, Jr. | Self-preserved nasal, inhalable, and topical ophthalmic preparations and medications |
| US20040081627A1 (en) | 2000-10-09 | 2004-04-29 | Jinks Phillip A | Medicinal aerosol formulations |
| US6908928B2 (en) | 2000-10-12 | 2005-06-21 | Bi Pharma Kg. | Crystalline tiotropium bromide monohydrate, processes for the preparation thereof, and pharmaceutical compositions |
| DK1920763T3 (da) | 2000-11-30 | 2014-07-07 | Vectura Ltd | Farrmaceutiske præparater til inhalation |
| EP1343372A2 (en) | 2000-12-21 | 2003-09-17 | Nektar Therapeutics | Pulmonary delivery of polyene antifungal agents |
| DE10064816A1 (de) | 2000-12-22 | 2002-06-27 | Boehringer Ingelheim Pharma | Verfahren zur Herstellung eines Anticholinergikums |
| DK1353647T3 (da) | 2000-12-27 | 2011-06-14 | Gilead Sciences Inc | Inhalerbar aztreonam til behandling og forebyggelse af bakterielle lungeinfektioner |
| US20020141946A1 (en) | 2000-12-29 | 2002-10-03 | Advanced Inhalation Research, Inc. | Particles for inhalation having rapid release properties |
| AU2002240137A1 (en) | 2001-01-30 | 2002-08-12 | University Of Iowa Research Foundation | Antiviral activities of primate theta defensins and mammalian cathelicidins |
| JP5154732B2 (ja) | 2001-02-06 | 2013-02-27 | イノバータ・バイオメッド・リミテッド | 薬剤 |
| US6546927B2 (en) | 2001-03-13 | 2003-04-15 | Aerogen, Inc. | Methods and apparatus for controlling piezoelectric vibration |
| US6550472B2 (en) | 2001-03-16 | 2003-04-22 | Aerogen, Inc. | Devices and methods for nebulizing fluids using flow directors |
| US6766799B2 (en) | 2001-04-16 | 2004-07-27 | Advanced Inhalation Research, Inc. | Inhalation device |
| US6667344B2 (en) | 2001-04-17 | 2003-12-23 | Dey, L.P. | Bronchodilating compositions and methods |
| US6511050B2 (en) | 2001-05-02 | 2003-01-28 | Dynamo Aviation, Inc. | Humidifier |
| US6608055B2 (en) | 2001-06-22 | 2003-08-19 | Boehringer Ingelheim Pharma Kg | Crystalline anticholinergic, processes for preparing it and its use for preparing a pharmaceutical composition |
| US20030138403A1 (en) | 2001-06-29 | 2003-07-24 | Maxygen Aps | Interferon formulations |
| JP2003074919A (ja) | 2001-08-31 | 2003-03-12 | Sunbow Precision Co Ltd | 複合式加湿器 |
| WO2003035028A1 (en) | 2001-10-19 | 2003-05-01 | Nektar Therapeutics | Modulating charge density to produce improvements in the characteristics of spray-dried proteins |
| US20030203930A1 (en) | 2001-10-26 | 2003-10-30 | Imtiaz Chaudry | Albuterol and ipratropium inhalation solution, system, kit and method for relieving symptoms of chronic obstructive pulmonary disease |
| JP4368198B2 (ja) | 2001-11-20 | 2009-11-18 | アルカーメス，インコーポレイテッド | 肺送達用の改良された粒状組成物 |
| AU2002349513B2 (en) | 2001-11-26 | 2007-10-18 | Asubio Pharma Co., Ltd. | Medicinal compositions for nasal absorption |
| US6851626B2 (en) | 2002-01-07 | 2005-02-08 | Aerogen, Inc. | Methods and devices for nebulizing fluids |
| GB2384198B (en) | 2002-01-18 | 2005-03-02 | Profile Drug Delivery Ltd | Nebulizer metering |
| GB0217199D0 (en) | 2002-07-25 | 2002-09-04 | Glaxo Group Ltd | Medicament dispenser |
| WO2003072080A1 (en) | 2002-02-22 | 2003-09-04 | Advanced Inhalation Research, Inc. | Inhalable formulations for sustained release |
| EP2630954B1 (en) | 2002-03-20 | 2016-10-05 | Civitas Therapeutics, Inc. | Pulmonary delivery for levodopa |
| US7008644B2 (en) | 2002-03-20 | 2006-03-07 | Advanced Inhalation Research, Inc. | Method and apparatus for producing dry particles |
| GB0207906D0 (en) | 2002-04-05 | 2002-05-15 | 3M Innovative Properties Co | Formoterol and mometasone aerosol formulations |
| GB0209782D0 (en) | 2002-04-29 | 2002-06-05 | Glaxo Group Ltd | Medicament dispenser |
| US20050220720A1 (en) | 2002-05-02 | 2005-10-06 | David Edwards | Formulations limiting spread of pulmonary infections |
| EP1503744A1 (en) | 2002-05-13 | 2005-02-09 | Alexza Molecular Delivery Corporation | Delivery of drug amines through an inhalation route |
| EP1511467A1 (en) | 2002-06-10 | 2005-03-09 | Elan Pharma International Limited | Nanoparticulate polycosanol formulations and novel polycosanol combinations |
| US7947742B2 (en) | 2002-06-28 | 2011-05-24 | Civitas Therapeutics, Inc. | Inhalable epinephrine |
| GB0217198D0 (en) | 2002-07-25 | 2002-09-04 | Glaxo Group Ltd | Medicament dispenser |
| US20050271660A1 (en) | 2002-09-06 | 2005-12-08 | Alexion Pharmaceuticals, Inc. | Nebulization of monoclonal antibodies for treating pulmonary diseases |
| US7371729B2 (en) | 2002-09-09 | 2008-05-13 | Trigen Limited | Boronic acid salts useful in parenteral formulations |
| JP2006503865A (ja) | 2002-09-30 | 2006-02-02 | アキュスフィア， インコーポレイテッド | 吸入のための徐放性の多孔性微粒子 |
| KR20090087971A (ko) | 2002-11-22 | 2009-08-18 | 유 망 | 광범위 스펙트럼의 항-바이러스 치료제 및 예방제 |
| US7534781B2 (en) | 2003-03-21 | 2009-05-19 | Dsm Ip Assets B.V. | Crystalline amoxicillin trihydrate powder |
| CN1194062C (zh) | 2003-04-04 | 2005-03-23 | 王泽斌 | 一种融雪融冰组合物及其制备方法和应用 |
| US20080125488A1 (en) | 2003-05-01 | 2008-05-29 | Leverve Xavier M | Lactate Containing Pharmaceutical Composition and Uses Thereof |
| ATE501766T1 (de) | 2003-05-20 | 2011-04-15 | James F Collins | Ophthalmisches arzneimittelabgabesystem |
| US7195179B2 (en) | 2003-06-01 | 2007-03-27 | Piezo Technologies | Piezoelectric mist generation device |
| EP1646370A1 (en) | 2003-07-11 | 2006-04-19 | Glaxo Group Limited | Pharmaceutical formulations |
| GB0324897D0 (en) | 2003-10-24 | 2003-11-26 | Glaxo Group Ltd | Composition |
| GB0324918D0 (en) | 2003-10-24 | 2003-11-26 | Glaxo Group Ltd | Composition |
| US7968717B2 (en) | 2003-11-03 | 2011-06-28 | Boehringer Ingelhein International Gmbh | Crystalline anhydrate with anticholinergic efficacy |
| SE0303270L (sv) | 2003-12-03 | 2005-06-04 | Microdrug Ag | Metod för administration av tiotropium |
| KR20050056622A (ko) | 2003-12-10 | 2005-06-16 | 주식회사 대우일렉트로닉스 | 플레쉬롬 다운로드 장치 |
| US7192919B2 (en) | 2004-01-07 | 2007-03-20 | Stelios Tzannis | Sustained release compositions for delivery of pharmaceutical proteins |
| US20050207983A1 (en) | 2004-03-05 | 2005-09-22 | Pulmatrix, Inc. | Formulations decreasing particle exhalation |
| SE528121C2 (sv) | 2004-03-29 | 2006-09-05 | Mederio Ag | Preparering av torrpulver för på förhand uppmätt DPI |
| US20070275091A1 (en) | 2004-03-30 | 2007-11-29 | Malcolm King | Compositions And Methods For Improved Mucus Function |
| CA2561993A1 (en) | 2004-03-30 | 2006-04-13 | Painceptor Pharma Corporation | Compositions and methods for modulating gated ion channels |
| US20050281740A1 (en) | 2004-06-16 | 2005-12-22 | Glen Gong | Imaging damaged lung tissue |
| GB0415789D0 (en) * | 2004-07-15 | 2004-08-18 | Astrazeneca Ab | Novel combination |
| US20060147520A1 (en) | 2004-07-26 | 2006-07-06 | Curtis Ruegg | Treatment of pulmonary hypertension by inhaled iloprost with a microparticle formulation |
| DE102004041253A1 (de) | 2004-08-26 | 2006-03-02 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neues Verfahren zur Herstellung von Tiotropiumsalzen |
| EP1796677A4 (en) | 2004-09-07 | 2009-07-08 | Smithkline Beecham Corp | PROCESS FOR ACTIVATION OF TRPV4 CHANNEL RECEPTORS BY AGONISTS |
| US20060073173A1 (en) | 2004-10-04 | 2006-04-06 | Maria Banach | Large-scale manufacturing process for the production of pharmaceutical compositions |
| GB0425758D0 (en) | 2004-11-23 | 2004-12-22 | Vectura Ltd | Preparation of pharmaceutical compositions |
| US8627821B2 (en) | 2005-01-10 | 2014-01-14 | Pulmatrix, Inc. | Method and device for decreasing contamination |
| WO2006084131A2 (en) | 2005-02-01 | 2006-08-10 | The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Furin inhibitors and alpha-defensins for the treatment or prevention of papillomavirus infection |
| EP2463551B1 (en) | 2005-02-10 | 2015-04-08 | BorgWarner Inc. | Dual clutch transmission |
| WO2006102438A2 (en) | 2005-03-23 | 2006-09-28 | Ihc Intellectual Asset Management, Llc | Methods and compositions for irrigation of mucosal tissues |
| US20060229366A1 (en) | 2005-04-07 | 2006-10-12 | Lifschitz Carlos H | Method for preventing or treating respiratory infections in infants |
| DK1881980T3 (da) | 2005-05-02 | 2012-10-01 | Boehringer Ingelheim Int | Nye krystalline former af tiotropiumbromid |
| US20070053844A1 (en) | 2005-05-18 | 2007-03-08 | Pulmatrix Inc. | Formulations for alteration of biophysical properties of mucosal lining |
| US7838532B2 (en) | 2005-05-18 | 2010-11-23 | Mpex Pharmaceuticals, Inc. | Aerosolized fluoroquinolones and uses thereof |
| GB0520794D0 (en) | 2005-10-12 | 2005-11-23 | Innovata Biomed Ltd | Inhaler |
| EP1952160B1 (en) | 2005-10-31 | 2011-04-06 | Janssen Pharmaceutica NV | Methods for identifying modulators of trpv2 |
| GB0523576D0 (en) | 2005-11-18 | 2005-12-28 | Theradeas Ltd | Drug composition and its use in therapy |
| JP5086267B2 (ja) | 2005-12-19 | 2012-11-28 | シコール インコーポレイティド | 臭化チオトロピウムの新規な形態およびそれを製造する方法 |
| JP2009524646A (ja) | 2006-01-27 | 2009-07-02 | ザ・プロヴォスト，フェローズ・アンド・スカラーズ・オブ・ザ・カレッジ・オブ・ザ・ホーリー・アンド・アンディヴァイデッド・トリニティー・オブ・クイーン・エリザベス，ニア・ダブリン | 多孔性微粒子の製造方法 |
| US20070202051A1 (en) | 2006-02-10 | 2007-08-30 | Pari Gmbh | Aerosols for sinunasal drug delivery |
| US20080051582A1 (en) | 2006-07-10 | 2008-02-28 | Sicor Inc. | Process for the preparation of tiotropium bromide |
| AU2007323007A1 (en) | 2006-08-11 | 2008-05-29 | Panacea Biotec Limited | Particles for delivery of active ingredients, process of making and compositions thereof |
| WO2008025560A1 (en) | 2006-09-01 | 2008-03-06 | Pari Pharma Gmbh | Methods for taste masking of nebulised compositions for nasal and pulmonary inhalation therapy |
| US20080063722A1 (en) | 2006-09-08 | 2008-03-13 | Advanced Inhalation Research, Inc. | Composition of a Spray-Dried Powder for Pulmonary Delivery of a Long Acting Neuraminidase Inhibitor (LANI) |
| EP2101748B9 (en) | 2006-11-29 | 2015-02-25 | Yissum Research Development Company of the Hebrew University of Jerusalem, Ltd. | Use of incensole and derivatives thereof for neuroprotection and for the treatment of depression and anxiety |
| BRPI0719756A2 (pt) | 2006-12-01 | 2014-01-21 | Anterios Inc | Nanopartículas de entidades anfifílicas |
| GB0625322D0 (en) | 2006-12-19 | 2007-01-24 | Pharmakodex Ltd | Pharmaceutical compositions |
| GB0716026D0 (en) | 2007-08-16 | 2007-09-26 | Norton Healthcare Ltd | An inhalable medicament |
| WO2009037503A2 (en) | 2007-09-18 | 2009-03-26 | Astrazeneca Ab | New combination - 012 for the treatment of respiratory diseases |
| GB0719518D0 (en) | 2007-10-05 | 2007-11-14 | Therapeutics Ltd E | Therapy |
| EP2050437A1 (en) | 2007-10-15 | 2009-04-22 | Laboratoires SMB | Improved pharmaceutical dry powder compositions for inhalation. |
| EP2080508A1 (en) | 2008-01-15 | 2009-07-22 | CHIESI FARMACEUTICI S.p.A. | Dry powder formulation comprising an anticholinergic drug |
| EP2098219A1 (en) | 2008-03-05 | 2009-09-09 | PARI Pharma GmbH | Macrolide compositions having improved taste and stability |
| US8119647B2 (en) | 2008-04-23 | 2012-02-21 | Glenmark Pharmaceuticals S.A. | Fused pyrimidineone compounds as TRPV3 modulators |
| CA2724009C (en) | 2008-05-15 | 2016-10-11 | Novartis Ag | Pulmonary delivery of a fluoroquinolone |
| EP2172190A1 (en) | 2008-10-02 | 2010-04-07 | Laboratorios Liconsa, S.A. | Inhalable particles comprising tiotropium |
| GB0818476D0 (en) | 2008-10-09 | 2008-11-12 | Vectura Delivery Device Ltd | Inhaler |
| US20120135969A1 (en) | 2008-11-27 | 2012-05-31 | Boehringer Ingelheim International Gmbh | Novel powdered crystalline medicines for inhalation |
| JP2012522009A (ja) | 2009-03-26 | 2012-09-20 | パルマトリックス，インコーポレイテッド | 肺炎および人工呼吸器関連気管気管支炎を治療および予防するための方法 |
| US20120070417A1 (en) | 2009-03-26 | 2012-03-22 | Pulmatrix, Inc. | Anti-influenza formulations and methods |
| RU2577698C2 (ru) | 2009-03-26 | 2016-03-20 | Пулмэтрикс, Инк. | Сухие порошкообразные составы и способы лечения легочных заболеваний |
| KR20120002981A (ko) | 2009-03-26 | 2012-01-09 | 풀매트릭스 인코퍼레이티드 | 호흡기 감염 치료를 위한 약제 제형 및 방법 |
| KR20120015295A (ko) | 2009-03-26 | 2012-02-21 | 풀매트릭스 인코퍼레이티드 | 점막 내층의 생물물리학적 성질의 변경을 위한 구연산 칼슘 및 젖산 칼슘 제형 |
| EP2411008B1 (en) | 2009-03-27 | 2017-03-22 | Mahmut Bilgic | Complexes of tiotropium with improved properties of solubility and stability |
| JP2012524815A (ja) | 2009-04-24 | 2012-10-18 | シェーリング コーポレイション | 乾燥粉末吸引器において有用な凝集体配合物 |
| EP3106149B1 (en) | 2009-05-29 | 2019-11-20 | Pearl Therapeutics, Inc. | Compositions for pulmonary delivery of long-acting muscarinic antagonists and long-acting beta-2 adrenergic receptor agonists and associated methods and systems |
| JP6205133B2 (ja) | 2009-07-10 | 2017-09-27 | プレジデント アンド フェローズ オブ ハーバード カレッジ | 抗炎症剤としての恒久的に荷電したナトリウムおよびカルシウムチャンネルブロッカー |
| TR200907236A2 (tr) | 2009-09-23 | 2011-04-21 | Bi̇lgi̇ç Mahmut | Tiotropyum kuru toz formülasyonunun blister ambalajda taşınması. |
| GB0918450D0 (en) | 2009-10-21 | 2009-12-09 | Innovata Ltd | Composition |
| CA2809666C (en) | 2010-08-30 | 2020-09-22 | Michael M. Lipp | Dry powder formulations and methods for treating pulmonary diseases |
| US20130164338A1 (en) | 2010-08-30 | 2013-06-27 | Pulmatrix, Inc. | Treatment of cystic fibrosis using calcium lactate, leucine and sodium chloride in a respiraple dry powder |
| RU2640921C2 (ru) * | 2010-09-29 | 2018-01-12 | Пулмэтрикс, Инк. | Катионы одновалентных металлов сухих порошков для ингаляций |
| US20150093440A1 (en) | 2010-10-15 | 2015-04-02 | Glaxo Group Limited | Aggregate nanoparticulate medicament formulations, manufacture and use thereof |
| PT106094A (pt) | 2012-01-13 | 2013-07-15 | Hovione Farmaciencia S A | Administração por inalação de formulações com dose elevada |
-
2014
- 2014-03-13 MX MX2015013845A patent/MX2015013845A/es unknown
- 2014-03-13 JP JP2016505482A patent/JP6473738B2/ja active Active
- 2014-03-13 RU RU2015146871A patent/RU2015146871A/ru not_active Application Discontinuation
- 2014-03-13 KR KR1020157027064A patent/KR20150135328A/ko not_active Withdrawn
- 2014-03-13 CA CA2907566A patent/CA2907566C/en active Active
- 2014-03-13 EP EP14723543.6A patent/EP2981247B1/en active Active
- 2014-03-13 WO PCT/US2014/025660 patent/WO2014165303A1/en not_active Ceased
- 2014-03-13 CN CN201480019667.4A patent/CN105324106A/zh active Pending
- 2014-03-13 AU AU2014248455A patent/AU2014248455B2/en active Active
- 2014-03-13 HK HK16109456.0A patent/HK1221175A1/zh unknown
-
2015
- 2015-09-30 US US14/870,736 patent/US9737518B2/en active Active
-
2017
- 2017-07-14 US US15/650,437 patent/US20170312258A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU2014248455A1 (en) | 2015-10-15 |
| US20160120855A1 (en) | 2016-05-05 |
| JP2016515576A (ja) | 2016-05-30 |
| CA2907566C (en) | 2023-08-22 |
| MX2015013845A (es) | 2016-05-09 |
| US9737518B2 (en) | 2017-08-22 |
| AU2014248455B2 (en) | 2018-12-06 |
| CN105324106A (zh) | 2016-02-10 |
| US20170312258A1 (en) | 2017-11-02 |
| BR112015025160A2 (pt) | 2017-07-18 |
| RU2015146871A (ru) | 2017-05-10 |
| CA2907566A1 (en) | 2014-10-09 |
| KR20150135328A (ko) | 2015-12-02 |
| HK1221175A1 (zh) | 2017-05-26 |
| EP2981247B1 (en) | 2023-06-07 |
| EP2981247A1 (en) | 2016-02-10 |
| WO2014165303A1 (en) | 2014-10-09 |
| RU2015146871A3 (enExample) | 2018-03-05 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP6473738B2 (ja) | チオトロピウム乾燥粉末 | |
| JP7623854B2 (ja) | 乾燥粉末配合および使用方法 | |
| CN103052379A (zh) | 包含磷酸二酯酶抑制剂的干粉制剂 | |
| JP7549534B2 (ja) | イトラコナゾールを含む肺内投与のための抗真菌配合物 | |
| KR20180003572A (ko) | 다중 약물 취성 매트릭스 조성물 | |
| CN116687887A (zh) | 用于吸入的干粉制剂 | |
| US10532041B2 (en) | Formulation comprising glycopyrrolate, method and apparatus | |
| CA2963666A1 (en) | Formulations containing tiotropium, amino acid and acid and methods thereof | |
| RU2742376C1 (ru) | Способ получения состава сухого порошка, содержащего антихолинергическое средство, кортикостероид и бета-адренергетик | |
| US20170304198A1 (en) | Improved stability of dry powders containing tiotropium and amino acid | |
| KR102898819B1 (ko) | 흡입용 건조 분말 제제를 위한 신규 담체 입자 | |
| US20240033218A1 (en) | Dihydroergotamine dry powder formulations and methods of use | |
| RU2823554C1 (ru) | Новые частицы носителя для сухих порошковых составов для ингаляции | |
| BR112015025160B1 (pt) | Pós secos de tiotrópio | |
| KR20240025644A (ko) | 흡입용 티오트로피움의 신규한 건조 분말 조성물 | |
| HK40064779A (en) | Novel carrier particles for dry powder formulations for inhalation | |
| US20120097160A1 (en) | Agglomerate formulations including active pharmaceutical agents with targeted particle sizes |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20170310 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20170310 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20180111 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20180409 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20180611 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20180706 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20180905 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20181205 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20190104 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20190128 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 6473738 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |