GB2545025A - Pharmaceutical composition - Google Patents
Pharmaceutical composition Download PDFInfo
- Publication number
- GB2545025A GB2545025A GB1521462.0A GB201521462A GB2545025A GB 2545025 A GB2545025 A GB 2545025A GB 201521462 A GB201521462 A GB 201521462A GB 2545025 A GB2545025 A GB 2545025A
- Authority
- GB
- United Kingdom
- Prior art keywords
- mometasone
- formoterol
- pharmaceutical composition
- weight
- compound
- 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.)
- Withdrawn
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 124
- -1 mometasone compound Chemical class 0.000 claims abstract description 101
- 229960001664 mometasone Drugs 0.000 claims abstract description 95
- 229960002848 formoterol Drugs 0.000 claims abstract description 87
- 239000003380 propellant Substances 0.000 claims abstract description 69
- NPNPZTNLOVBDOC-UHFFFAOYSA-N 1,1-difluoroethane Chemical compound CC(F)F NPNPZTNLOVBDOC-UHFFFAOYSA-N 0.000 claims abstract description 44
- 229940071648 metered dose inhaler Drugs 0.000 claims abstract description 36
- 239000000203 mixture Substances 0.000 claims abstract description 30
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 22
- 239000004094 surface-active agent Substances 0.000 claims abstract description 19
- 239000004411 aluminium Substances 0.000 claims abstract description 17
- 229910052782 aluminium Inorganic materials 0.000 claims abstract description 17
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 claims abstract description 17
- 229960002744 mometasone furoate Drugs 0.000 claims abstract description 16
- 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 abstract description 16
- RATSWNOMCHFQGJ-TUYNVFRMSA-N (e)-but-2-enedioic acid;n-[2-hydroxy-5-[(1s)-1-hydroxy-2-[[(2s)-1-(4-methoxyphenyl)propan-2-yl]amino]ethyl]phenyl]formamide;dihydrate Chemical compound O.O.OC(=O)\C=C\C(O)=O.C1=CC(OC)=CC=C1C[C@H](C)NC[C@@H](O)C1=CC=C(O)C(NC=O)=C1.C1=CC(OC)=CC=C1C[C@H](C)NC[C@@H](O)C1=CC=C(O)C(NC=O)=C1 RATSWNOMCHFQGJ-TUYNVFRMSA-N 0.000 claims abstract description 15
- 229960003610 formoterol fumarate dihydrate Drugs 0.000 claims abstract description 15
- 208000006673 asthma Diseases 0.000 claims abstract description 6
- BPZSYCZIITTYBL-UHFFFAOYSA-N formoterol Chemical compound C1=CC(OC)=CC=C1CC(C)NCC(O)C1=CC=C(O)C(NC=O)=C1 BPZSYCZIITTYBL-UHFFFAOYSA-N 0.000 claims description 43
- 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 claims description 41
- 238000000034 method Methods 0.000 claims description 33
- 239000012453 solvate Substances 0.000 claims description 33
- 238000003860 storage Methods 0.000 claims description 28
- 150000003839 salts Chemical class 0.000 claims description 24
- 229940002612 prodrug Drugs 0.000 claims description 22
- 239000000651 prodrug Chemical class 0.000 claims description 22
- 239000012535 impurity Substances 0.000 claims description 20
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 14
- 230000015556 catabolic process Effects 0.000 claims description 10
- 238000006731 degradation reaction Methods 0.000 claims description 10
- 239000000725 suspension Substances 0.000 claims description 10
- 239000000443 aerosol Substances 0.000 claims description 8
- 238000002360 preparation method Methods 0.000 claims description 6
- 208000023504 respiratory system disease Diseases 0.000 claims description 6
- 230000000694 effects Effects 0.000 claims description 5
- 230000000717 retained effect Effects 0.000 claims description 5
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 4
- 230000003019 stabilising effect Effects 0.000 claims description 2
- 229940051271 1,1-difluoroethane Drugs 0.000 abstract description 8
- 208000019693 Lung disease Diseases 0.000 abstract 1
- 230000001684 chronic effect Effects 0.000 abstract 1
- 230000000414 obstructive effect Effects 0.000 abstract 1
- 239000002798 polar solvent Substances 0.000 abstract 1
- 239000003814 drug Substances 0.000 description 33
- 229940079593 drug Drugs 0.000 description 30
- LVGUZGTVOIAKKC-UHFFFAOYSA-N 1,1,1,2-tetrafluoroethane Chemical compound FCC(F)(F)F LVGUZGTVOIAKKC-UHFFFAOYSA-N 0.000 description 13
- 230000006641 stabilisation Effects 0.000 description 10
- 150000001875 compounds Chemical class 0.000 description 6
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 description 5
- 235000019404 dichlorodifluoromethane Nutrition 0.000 description 5
- 239000006185 dispersion Substances 0.000 description 5
- 239000013583 drug formulation Substances 0.000 description 5
- 238000002156 mixing Methods 0.000 description 5
- 238000009472 formulation Methods 0.000 description 4
- 239000007788 liquid Substances 0.000 description 4
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 4
- 239000002245 particle Substances 0.000 description 4
- 210000002345 respiratory system Anatomy 0.000 description 4
- 239000002904 solvent Substances 0.000 description 4
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 4
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 3
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 3
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 3
- 239000004338 Dichlorodifluoromethane Substances 0.000 description 3
- 239000005642 Oleic acid Substances 0.000 description 3
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 description 3
- CBENFWSGALASAD-UHFFFAOYSA-N Ozone Chemical compound [O-][O+]=O CBENFWSGALASAD-UHFFFAOYSA-N 0.000 description 3
- 238000004378 air conditioning Methods 0.000 description 3
- RWRIWBAIICGTTQ-UHFFFAOYSA-N difluoromethane Chemical compound FCF RWRIWBAIICGTTQ-UHFFFAOYSA-N 0.000 description 3
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 3
- 239000000463 material Substances 0.000 description 3
- 239000007921 spray Substances 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- 229940029284 trichlorofluoromethane Drugs 0.000 description 3
- CDOOAUSHHFGWSA-OWOJBTEDSA-N (e)-1,3,3,3-tetrafluoroprop-1-ene Chemical compound F\C=C\C(F)(F)F CDOOAUSHHFGWSA-OWOJBTEDSA-N 0.000 description 2
- DDMOUSALMHHKOS-UHFFFAOYSA-N 1,2-dichloro-1,1,2,2-tetrafluoroethane Chemical compound FC(F)(Cl)C(F)(F)Cl DDMOUSALMHHKOS-UHFFFAOYSA-N 0.000 description 2
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 2
- FXRLMCRCYDHQFW-UHFFFAOYSA-N 2,3,3,3-tetrafluoropropene Chemical compound FC(=C)C(F)(F)F FXRLMCRCYDHQFW-UHFFFAOYSA-N 0.000 description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- LCGLNKUTAGEVQW-UHFFFAOYSA-N Dimethyl ether Chemical compound COC LCGLNKUTAGEVQW-UHFFFAOYSA-N 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
- ATUOYWHBWRKTHZ-UHFFFAOYSA-N Propane Chemical compound CCC ATUOYWHBWRKTHZ-UHFFFAOYSA-N 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- 239000003246 corticosteroid Substances 0.000 description 2
- 229960001334 corticosteroids Drugs 0.000 description 2
- NNPPMTNAJDCUHE-UHFFFAOYSA-N isobutane Chemical compound CC(C)C NNPPMTNAJDCUHE-UHFFFAOYSA-N 0.000 description 2
- 229940067606 lecithin Drugs 0.000 description 2
- 239000000787 lecithin Substances 0.000 description 2
- 235000010445 lecithin Nutrition 0.000 description 2
- 210000004072 lung Anatomy 0.000 description 2
- 229910052751 metal Inorganic materials 0.000 description 2
- 239000002184 metal Substances 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
- 230000001105 regulatory effect Effects 0.000 description 2
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 2
- 238000010792 warming Methods 0.000 description 2
- NWLPAIVRIWBEIT-SEPHDYHBSA-N (e)-but-2-enedioic acid;dihydrate Chemical compound O.O.OC(=O)\C=C\C(O)=O NWLPAIVRIWBEIT-SEPHDYHBSA-N 0.000 description 1
- SMNDYUVBFMFKNZ-UHFFFAOYSA-N 2-furoic acid Chemical compound OC(=O)C1=CC=CO1 SMNDYUVBFMFKNZ-UHFFFAOYSA-N 0.000 description 1
- PZSMUPGANZGPBF-UHFFFAOYSA-N 4-[5-(dithiolan-3-yl)pentanoylamino]butanoic acid Chemical compound OC(=O)CCCNC(=O)CCCCC1CCSS1 PZSMUPGANZGPBF-UHFFFAOYSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 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
- 239000004215 Carbon black (E152) Substances 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 1
- RGHNJXZEOKUKBD-SQOUGZDYSA-M D-gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O RGHNJXZEOKUKBD-SQOUGZDYSA-M 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 description 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-M Methanesulfonate Chemical compound CS([O-])(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-M 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 description 1
- 206010070834 Sensitisation Diseases 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- 229940022663 acetate Drugs 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000007059 acute toxicity Effects 0.000 description 1
- 231100000403 acute toxicity Toxicity 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 238000005054 agglomeration Methods 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 229940072107 ascorbate Drugs 0.000 description 1
- 235000010323 ascorbic acid Nutrition 0.000 description 1
- 239000011668 ascorbic acid Substances 0.000 description 1
- 239000012298 atmosphere Substances 0.000 description 1
- 229940092705 beclomethasone Drugs 0.000 description 1
- 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 1
- 230000009286 beneficial effect Effects 0.000 description 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 1
- 238000009835 boiling Methods 0.000 description 1
- 210000003123 bronchiole Anatomy 0.000 description 1
- 229960004436 budesonide Drugs 0.000 description 1
- 239000004067 bulking agent Substances 0.000 description 1
- 239000001273 butane Substances 0.000 description 1
- 230000000747 cardiac effect Effects 0.000 description 1
- KVSASDOGYIBWTA-UHFFFAOYSA-N chloro benzoate Chemical compound ClOC(=O)C1=CC=CC=C1 KVSASDOGYIBWTA-UHFFFAOYSA-N 0.000 description 1
- 230000007665 chronic toxicity Effects 0.000 description 1
- 231100000160 chronic toxicity Toxicity 0.000 description 1
- 230000008021 deposition Effects 0.000 description 1
- 229940087091 dichlorotetrafluoroethane Drugs 0.000 description 1
- 238000012377 drug delivery Methods 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 238000005429 filling process Methods 0.000 description 1
- 238000007667 floating Methods 0.000 description 1
- 229960002714 fluticasone Drugs 0.000 description 1
- 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 1
- 239000011521 glass Substances 0.000 description 1
- 229940050410 gluconate Drugs 0.000 description 1
- JFCQEDHGNNZCLN-UHFFFAOYSA-N glutaric acid Chemical compound OC(=O)CCCC(O)=O JFCQEDHGNNZCLN-UHFFFAOYSA-N 0.000 description 1
- 239000012456 homogeneous solution Substances 0.000 description 1
- 229930195733 hydrocarbon Natural products 0.000 description 1
- 150000002430 hydrocarbons Chemical class 0.000 description 1
- 239000001282 iso-butane Substances 0.000 description 1
- 229940001447 lactate Drugs 0.000 description 1
- 229940125389 long-acting beta agonist Drugs 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- IZYBEMGNIUSSAX-UHFFFAOYSA-N methyl benzenecarboperoxoate Chemical compound COOC(=O)C1=CC=CC=C1 IZYBEMGNIUSSAX-UHFFFAOYSA-N 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- IJDNQMDRQITEOD-UHFFFAOYSA-N n-butane Chemical compound CCCC IJDNQMDRQITEOD-UHFFFAOYSA-N 0.000 description 1
- OFBQJSOFQDEBGM-UHFFFAOYSA-N n-pentane Natural products CCCCC OFBQJSOFQDEBGM-UHFFFAOYSA-N 0.000 description 1
- 229940049964 oleate Drugs 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 230000035515 penetration Effects 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
- 239000004033 plastic Substances 0.000 description 1
- 229920003023 plastic Polymers 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 239000001294 propane Substances 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 239000003507 refrigerant Substances 0.000 description 1
- 238000005057 refrigeration Methods 0.000 description 1
- 229960001860 salicylate Drugs 0.000 description 1
- 238000004062 sedimentation Methods 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 229940086735 succinate Drugs 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 229910021653 sulphate ion Inorganic materials 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 description 1
- 230000002110 toxicologic effect Effects 0.000 description 1
- 231100000027 toxicology Toxicity 0.000 description 1
- 238000009736 wetting Methods 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
-
- 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
- A61K31/573—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 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
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- 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
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
-
- 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
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
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- 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
- A61K9/008—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K9/08—Solutions
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
- A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- 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
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)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pulmonology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Otolaryngology (AREA)
- Pain & Pain Management (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Anesthesiology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Priority Applications (22)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1521462.0A GB2545025A (en) | 2015-12-04 | 2015-12-04 | Pharmaceutical composition |
| CN202111072725.8A CN113908164A (zh) | 2015-12-04 | 2016-12-02 | 药物组合物 |
| EP19178815.7A EP3563831A1 (en) | 2015-12-04 | 2016-12-02 | Pharmaceutical composition |
| US15/781,060 US20180264007A1 (en) | 2015-12-04 | 2016-12-02 | Pharmaceutical composition |
| CN201680071093.4A CN108289842B (zh) | 2015-12-04 | 2016-12-02 | 药物组合物 |
| AU2016364005A AU2016364005B2 (en) | 2015-12-04 | 2016-12-02 | Pharmaceutical composition |
| EP16823027.4A EP3383367B1 (en) | 2015-12-04 | 2016-12-02 | Pharmaceutical composition |
| MX2018006799A MX375784B (es) | 2015-12-04 | 2016-12-02 | Composiciones farmacéuticas que comprenden al menos un compuesto de mometasona y un componente propelente. |
| PCT/GB2016/053804 WO2017093755A1 (en) | 2015-12-04 | 2016-12-02 | Pharmaceutical composition |
| JP2018529067A JP6993335B2 (ja) | 2015-12-04 | 2016-12-02 | 薬学的組成物 |
| ES16823027T ES2796343T3 (es) | 2015-12-04 | 2016-12-02 | Composición farmacéutica |
| EP19178833.0A EP3563832A1 (en) | 2015-12-04 | 2016-12-02 | Pharmaceutical composition |
| CA3007046A CA3007046C (en) | 2015-12-04 | 2016-12-02 | Pharmaceutical composition comprising a mometasone compound |
| BR112018011269-0A BR112018011269B1 (pt) | 2015-12-04 | 2016-12-02 | Composição farmacêutica, e, métodos para aumentar o tempo de assentamento de uma composição farmacêutica, para estabilizar uma composição farmacêutica e para melhorar o desempenho de aerossolização |
| AU2019201520A AU2019201520C1 (en) | 2015-12-04 | 2019-03-05 | Pharmaceutical composition |
| AU2019201521A AU2019201521B2 (en) | 2015-12-04 | 2019-03-05 | Pharmaceutical composition |
| US16/565,217 US20200000826A1 (en) | 2015-12-04 | 2019-09-09 | Pharmaceutical composition |
| US16/565,226 US20190388438A1 (en) | 2015-12-04 | 2019-09-09 | Pharmaceutical composition |
| JP2019231998A JP6993398B2 (ja) | 2015-12-04 | 2019-12-23 | 薬学的組成物 |
| US17/944,637 US20230029180A1 (en) | 2015-12-04 | 2022-09-14 | Pharmaceutical composition |
| US17/944,666 US20230029174A1 (en) | 2015-12-04 | 2022-09-14 | Pharmaceutical composition |
| US17/969,250 US20230051849A1 (en) | 2015-12-04 | 2022-10-19 | Pharmaceutical composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1521462.0A GB2545025A (en) | 2015-12-04 | 2015-12-04 | Pharmaceutical composition |
Publications (2)
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|---|---|
| GB201521462D0 GB201521462D0 (en) | 2016-01-20 |
| GB2545025A true GB2545025A (en) | 2017-06-07 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GB1521462.0A Withdrawn GB2545025A (en) | 2015-12-04 | 2015-12-04 | Pharmaceutical composition |
Country Status (10)
| Country | Link |
|---|---|
| US (6) | US20180264007A1 (enExample) |
| EP (3) | EP3563832A1 (enExample) |
| JP (2) | JP6993335B2 (enExample) |
| CN (2) | CN113908164A (enExample) |
| AU (3) | AU2016364005B2 (enExample) |
| CA (1) | CA3007046C (enExample) |
| ES (1) | ES2796343T3 (enExample) |
| GB (1) | GB2545025A (enExample) |
| MX (1) | MX375784B (enExample) |
| WO (1) | WO2017093755A1 (enExample) |
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| GB2545025A (en) * | 2015-12-04 | 2017-06-07 | Mexichem Fluor Sa De Cv | Pharmaceutical composition |
| CN116898804A (zh) * | 2016-09-19 | 2023-10-20 | 墨西哥氟石股份公司 | 药物组合物 |
| JP6781831B2 (ja) * | 2016-09-19 | 2020-11-04 | メキシケム フロー エセ・ア・デ・セ・ヴェ | 医薬組成物 |
| GB2573297A (en) * | 2018-04-30 | 2019-11-06 | Mexichem Fluor Sa De Cv | Pharmaceutical composition |
| JOP20200314A1 (ar) * | 2018-06-04 | 2020-12-06 | Lupin Inc | تركيبات صيدلانية مستقرة لأجهزة إستنشاق جرعات مضغوطة معايرة الجرعة |
| FR3107039B1 (fr) * | 2020-02-07 | 2022-03-18 | Aptar France Sas | Valve doseuse avec chambre de dosage améliorée |
| WO2021165348A1 (en) * | 2020-02-20 | 2021-08-26 | Chiesi Farmaceutici S.P.A. | Pressurised metered dose inhalers comprising a buffered pharmaceutical formulation |
| CN115813935A (zh) * | 2021-09-16 | 2023-03-21 | 上海上药信谊药厂有限公司 | 药物组合物、气雾剂及其制备方法和气雾剂产生系统 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002011711A2 (en) * | 2000-08-04 | 2002-02-14 | Longwood Pharmaceutical Research, Inc. | Formulations of mometasone and a bronchodilator for pulmonary administration |
| WO2005034911A1 (en) * | 2003-10-09 | 2005-04-21 | Jagotec Ag | Aerosol formulations comprising formoterol fumarate dihydrate, a propellant,ethanol and optionally a steroid,where the formoterol fumarate dihydrate has a water content of 4.8-4.28% by weight |
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| SK81197A3 (en) * | 1994-12-22 | 1997-11-05 | Astra Ab | Aerosol drug formulations, method for production thereof and its use |
| GB9904919D0 (en) * | 1999-03-03 | 1999-04-28 | Novartis Ag | Organic compounds |
| US6432415B1 (en) * | 1999-12-17 | 2002-08-13 | Axrix Laboratories, Inc. | Pharmaceutical gel and aerosol formulations and methods to administer the same to skin and mucosal surfaces |
| TWI324934B (en) * | 2001-08-28 | 2010-05-21 | Schering Corp | Pharmaceutical compositions for the treatment of asthma |
| GB0207906D0 (en) * | 2002-04-05 | 2002-05-15 | 3M Innovative Properties Co | Formoterol and mometasone aerosol formulations |
| EP2444080A3 (en) * | 2007-02-09 | 2012-05-02 | Schering Corporation | Stable Pharmaceutical Drug Aerosols |
| US8236786B2 (en) * | 2008-08-07 | 2012-08-07 | Pulmagen Therapeutics (Inflammation) Limited | Respiratory disease treatment |
| GB2465897B (en) * | 2008-08-07 | 2011-02-09 | Argenta Discovery Ltd | Respiratory disease treatment |
| US20120252824A1 (en) * | 2009-06-16 | 2012-10-04 | John Brew | Drug Combinations and Uses in Treating a Coughing Condition |
| US20120238559A1 (en) * | 2009-12-03 | 2012-09-20 | Glaxo Group Limited | Novel compounds |
| WO2011076843A2 (en) * | 2009-12-23 | 2011-06-30 | Chiesi Farmaceutici S.P.A. | Combination therapy for copd |
| CN102416179B (zh) * | 2010-09-28 | 2014-05-07 | 益得生物科技股份有限公司 | 用于哮喘的吸入性复方组合物 |
| GB201108039D0 (en) * | 2011-05-13 | 2011-06-29 | Mexichem Amanco Holding Sa | Compositions |
| GB201117619D0 (en) * | 2011-10-12 | 2011-11-23 | Mexichem Amanco Holding Sa | Compositions |
| GB201117621D0 (en) * | 2011-10-12 | 2011-11-23 | Mexichem Amanco Holding Sa | Compositions |
| WO2014016548A2 (en) * | 2012-07-27 | 2014-01-30 | Cipla Limited | Pharmaceutical composition |
| BR112016014583B1 (pt) * | 2013-12-30 | 2022-12-20 | Chiesi Farmaceutici S.P.A | Composição de solução farmacêutica em aerossol, inalador pressurizado de dose calibrada e uso da dita composição |
| CN108289843B (zh) * | 2015-12-04 | 2021-08-17 | 墨西哥氟石股份公司 | 药物组合物 |
| GB2545025A (en) * | 2015-12-04 | 2017-06-07 | Mexichem Fluor Sa De Cv | Pharmaceutical composition |
| US10792256B2 (en) * | 2016-09-19 | 2020-10-06 | Mexichem Fluor S.A. De C.V. | Pharmaceutical composition |
-
2015
- 2015-12-04 GB GB1521462.0A patent/GB2545025A/en not_active Withdrawn
-
2016
- 2016-12-02 WO PCT/GB2016/053804 patent/WO2017093755A1/en not_active Ceased
- 2016-12-02 CN CN202111072725.8A patent/CN113908164A/zh active Pending
- 2016-12-02 EP EP19178833.0A patent/EP3563832A1/en active Pending
- 2016-12-02 ES ES16823027T patent/ES2796343T3/es active Active
- 2016-12-02 EP EP16823027.4A patent/EP3383367B1/en active Active
- 2016-12-02 CN CN201680071093.4A patent/CN108289842B/zh active Active
- 2016-12-02 AU AU2016364005A patent/AU2016364005B2/en active Active
- 2016-12-02 MX MX2018006799A patent/MX375784B/es active IP Right Grant
- 2016-12-02 CA CA3007046A patent/CA3007046C/en active Active
- 2016-12-02 US US15/781,060 patent/US20180264007A1/en not_active Abandoned
- 2016-12-02 JP JP2018529067A patent/JP6993335B2/ja active Active
- 2016-12-02 EP EP19178815.7A patent/EP3563831A1/en not_active Withdrawn
-
2019
- 2019-03-05 AU AU2019201520A patent/AU2019201520C1/en active Active
- 2019-03-05 AU AU2019201521A patent/AU2019201521B2/en active Active
- 2019-09-09 US US16/565,226 patent/US20190388438A1/en not_active Abandoned
- 2019-09-09 US US16/565,217 patent/US20200000826A1/en not_active Abandoned
- 2019-12-23 JP JP2019231998A patent/JP6993398B2/ja active Active
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2022
- 2022-09-14 US US17/944,666 patent/US20230029174A1/en active Pending
- 2022-09-14 US US17/944,637 patent/US20230029180A1/en active Pending
- 2022-10-19 US US17/969,250 patent/US20230051849A1/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002011711A2 (en) * | 2000-08-04 | 2002-02-14 | Longwood Pharmaceutical Research, Inc. | Formulations of mometasone and a bronchodilator for pulmonary administration |
| WO2005034911A1 (en) * | 2003-10-09 | 2005-04-21 | Jagotec Ag | Aerosol formulations comprising formoterol fumarate dihydrate, a propellant,ethanol and optionally a steroid,where the formoterol fumarate dihydrate has a water content of 4.8-4.28% by weight |
Also Published As
| Publication number | Publication date |
|---|---|
| BR112018011269A2 (pt) | 2018-11-21 |
| WO2017093755A1 (en) | 2017-06-08 |
| JP6993335B2 (ja) | 2022-01-13 |
| US20230029174A1 (en) | 2023-01-26 |
| AU2016364005A1 (en) | 2018-06-21 |
| EP3563832A1 (en) | 2019-11-06 |
| CN108289842B (zh) | 2021-10-22 |
| US20230051849A1 (en) | 2023-02-16 |
| US20180264007A1 (en) | 2018-09-20 |
| US20230029180A1 (en) | 2023-01-26 |
| US20190388438A1 (en) | 2019-12-26 |
| MX2018006799A (es) | 2018-11-09 |
| AU2016364005B2 (en) | 2019-09-26 |
| EP3383367A1 (en) | 2018-10-10 |
| CN108289842A (zh) | 2018-07-17 |
| GB201521462D0 (en) | 2016-01-20 |
| CA3007046A1 (en) | 2017-06-08 |
| CA3007046C (en) | 2021-05-11 |
| MX375784B (es) | 2025-03-07 |
| AU2019201520A1 (en) | 2019-03-28 |
| EP3383367B1 (en) | 2020-03-25 |
| CN113908164A (zh) | 2022-01-11 |
| AU2019201521A1 (en) | 2019-03-28 |
| AU2019201520C1 (en) | 2020-12-10 |
| AU2019201520B2 (en) | 2020-07-09 |
| JP2020073514A (ja) | 2020-05-14 |
| JP2019503997A (ja) | 2019-02-14 |
| JP6993398B2 (ja) | 2022-01-13 |
| AU2019201521B2 (en) | 2020-07-16 |
| ES2796343T3 (es) | 2020-11-26 |
| EP3563831A1 (en) | 2019-11-06 |
| US20200000826A1 (en) | 2020-01-02 |
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| WAP | Application withdrawn, taken to be withdrawn or refused ** after publication under section 16(1) |