JP2016512494A5 - - Google Patents

Info

Publication number

JP2016512494A5

JP2016512494A5 JP2015562509A JP2015562509A JP2016512494A5 JP 2016512494 A5 JP2016512494 A5 JP 2016512494A5 JP 2015562509 A JP2015562509 A JP 2015562509A JP 2015562509 A JP2015562509 A JP 2015562509A JP 2016512494 A5 JP2016512494 A5 JP 2016512494A5

Authority

JP

Japan

Prior art keywords

particles

pharmaceutically acceptable

ester

acceptable salt

active agent

Prior art date

2014-03-13

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.)

Granted

Links

• Espacenet
• Global Dossier
• Discuss

• 239000002245 particle Substances 0.000 claims 58
• 150000003839 salts Chemical class 0.000 claims 27
• 150000002148 esters Chemical class 0.000 claims 26
• 239000013543 active substance Substances 0.000 claims 16
• 239000000843 powder Substances 0.000 claims 16
• 239000008194 pharmaceutical composition Substances 0.000 claims 15
• 229960002462 glycopyrronium bromide Drugs 0.000 claims 11
• ANGKOCUUWGHLCE-HKUYNNGSSA-N [(3s)-1,1-dimethylpyrrolidin-1-ium-3-yl] (2r)-2-cyclopentyl-2-hydroxy-2-phenylacetate Chemical compound C1[N+](C)(C)CC[C@@H]1OC(=O)[C@](O)(C=1C=CC=CC=1)C1CCCC1 ANGKOCUUWGHLCE-HKUYNNGSSA-N 0.000 claims 9
• 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 claims 9
• 229960004078 indacaterol Drugs 0.000 claims 9
• 229960001664 mometasone Drugs 0.000 claims 9
• 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 9
• 239000000203 mixture Substances 0.000 claims 8
• 239000003814 drug Substances 0.000 claims 5
• 238000000034 method Methods 0.000 claims 5
• NRJAVPSFFCBXDT-HUESYALOSA-N 1,2-distearoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCCCCCCCCCCC NRJAVPSFFCBXDT-HUESYALOSA-N 0.000 claims 4
• 229940079593 drug Drugs 0.000 claims 4
• 229940112141 dry powder inhaler Drugs 0.000 claims 3
• ANGKOCUUWGHLCE-UHFFFAOYSA-N 2-cyclopentyl-2-hydroxy-2-phenylacetic acid (1,1-dimethyl-3-pyrrolidin-1-iumyl) ester Chemical compound C1[N+](C)(C)CCC1OC(=O)C(O)(C=1C=CC=CC=1)C1CCCC1 ANGKOCUUWGHLCE-UHFFFAOYSA-N 0.000 claims 2
• UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 claims 2
• HZHXFIDENGBQFQ-FTBISJDPSA-N acetic acid;5-[(1r)-2-[(5,6-diethyl-2,3-dihydro-1h-inden-2-yl)amino]-1-hydroxyethyl]-8-hydroxy-1h-quinolin-2-one Chemical compound CC(O)=O.N1C(=O)C=CC2=C1C(O)=CC=C2[C@@H](O)CNC1CC(C=C(C(=C2)CC)CC)=C2C1 HZHXFIDENGBQFQ-FTBISJDPSA-N 0.000 claims 2
• 239000000654 additive Substances 0.000 claims 2
• 230000000996 additive effect Effects 0.000 claims 2
• 229910001628 calcium chloride Inorganic materials 0.000 claims 2
• 239000001110 calcium chloride Substances 0.000 claims 2
• 238000009472 formulation Methods 0.000 claims 2
• 230000002209 hydrophobic effect Effects 0.000 claims 2
• 239000000463 material Substances 0.000 claims 2
• 229960002744 mometasone furoate Drugs 0.000 claims 2
• 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 2
• 230000002685 pulmonary effect Effects 0.000 claims 2
• 230000000241 respiratory effect Effects 0.000 claims 2
• 239000002904 solvent Substances 0.000 claims 2
• 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 1
• 208000007934 ACTH-independent macronodular adrenal hyperplasia Diseases 0.000 claims 1
• 230000003796 beauty Effects 0.000 claims 1
• 230000008021 deposition Effects 0.000 claims 1
• 239000002552 dosage form Substances 0.000 claims 1
• 230000003434 inspiratory effect Effects 0.000 claims 1
• 239000007791 liquid phase Substances 0.000 claims 1
• 210000004072 lung Anatomy 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• 230000029058 respiratory gaseous exchange Effects 0.000 claims 1
• 238000001694 spray drying Methods 0.000 claims 1
• 239000000725 suspension Substances 0.000 claims 1