JP2020073494A5 - - Google Patents

Info

Publication number

JP2020073494A5

JP2020073494A5 JP2019224873A JP2019224873A JP2020073494A5 JP 2020073494 A5 JP2020073494 A5 JP 2020073494A5 JP 2019224873 A JP2019224873 A JP 2019224873A JP 2019224873 A JP2019224873 A JP 2019224873A JP 2020073494 A5 JP2020073494 A5 JP 2020073494A5

Authority

JP

Japan

Prior art keywords

pharmaceutical composition

aqueous pharmaceutical

composition according

pirfenidone

dose

Prior art date

2019-12-12

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

• 239000008194 pharmaceutical composition Substances 0.000 claims 23
• 239000007788 liquid Substances 0.000 claims 11
• 230000008685 targeting Effects 0.000 claims 8
• 239000000443 aerosol Substances 0.000 claims 7
• ISWRGOKTTBVCFA-UHFFFAOYSA-N pirfenidone Chemical compound C1=C(C)C=CC(=O)N1C1=CC=CC=C1 ISWRGOKTTBVCFA-UHFFFAOYSA-N 0.000 claims 7
• 229960003073 pirfenidone Drugs 0.000 claims 7
• 239000003446 ligand Substances 0.000 claims 6
• 239000006199 nebulizer Substances 0.000 claims 6
• 150000003384 small molecules Chemical class 0.000 claims 5
• 208000029523 Interstitial Lung disease Diseases 0.000 claims 3
• 239000007864 aqueous solution Substances 0.000 claims 3
• KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 3
• 239000003814 drug Substances 0.000 claims 3
• 210000004072 lung Anatomy 0.000 claims 3
• 150000003839 salts Chemical class 0.000 claims 3
• 102000018233 Fibroblast Growth Factor Human genes 0.000 claims 2
• 108050007372 Fibroblast Growth Factor Proteins 0.000 claims 2
• TWRXJAOTZQYOKJ-UHFFFAOYSA-L Magnesium chloride Chemical compound [Mg+2].[Cl-].[Cl-] TWRXJAOTZQYOKJ-UHFFFAOYSA-L 0.000 claims 2
• 102000010780 Platelet-Derived Growth Factor Human genes 0.000 claims 2
• 108010038512 Platelet-Derived Growth Factor Proteins 0.000 claims 2
• FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 2
• 230000037396 body weight Effects 0.000 claims 2
• 229940079593 drug Drugs 0.000 claims 2
• 229940126864 fibroblast growth factor Drugs 0.000 claims 2
• LVWZTYCIRDMTEY-UHFFFAOYSA-N metamizole Chemical compound O=C1C(N(CS(O)(=O)=O)C)=C(C)N(C)N1C1=CC=CC=C1 LVWZTYCIRDMTEY-UHFFFAOYSA-N 0.000 claims 2
• 239000006186 oral dosage form Substances 0.000 claims 2
• 230000003204 osmotic effect Effects 0.000 claims 2
• 239000002245 particle Substances 0.000 claims 2
• JHJLBTNAGRQEKS-UHFFFAOYSA-M sodium bromide Chemical compound [Na+].[Br-] JHJLBTNAGRQEKS-UHFFFAOYSA-M 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
• 102100031168 CCN family member 2 Human genes 0.000 claims 1
• UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 claims 1
• 108090000386 Fibroblast Growth Factor 1 Proteins 0.000 claims 1
• 102100031706 Fibroblast growth factor 1 Human genes 0.000 claims 1
• 101000777550 Homo sapiens CCN family member 2 Proteins 0.000 claims 1
• 101000950669 Homo sapiens Mitogen-activated protein kinase 9 Proteins 0.000 claims 1
• 101001092910 Homo sapiens Serum amyloid P-component Proteins 0.000 claims 1
• -1 IW001 Proteins 0.000 claims 1
• 108010005716 Interferon beta-1a Proteins 0.000 claims 1
• 102000008070 Interferon-gamma Human genes 0.000 claims 1
• 108010074328 Interferon-gamma Proteins 0.000 claims 1
• PWKSKIMOESPYIA-BYPYZUCNSA-N L-N-acetyl-Cysteine Chemical compound CC(=O)N[C@@H](CS)C(O)=O PWKSKIMOESPYIA-BYPYZUCNSA-N 0.000 claims 1
• 102100037809 Mitogen-activated protein kinase 9 Human genes 0.000 claims 1
• 108010089484 PRM-151 Proteins 0.000 claims 1
• 102100036202 Serum amyloid P-component Human genes 0.000 claims 1
• 102000004887 Transforming Growth Factor beta Human genes 0.000 claims 1
• 108090001012 Transforming Growth Factor beta Proteins 0.000 claims 1
• 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 claims 1
• 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 claims 1
• 239000003963 antioxidant agent Substances 0.000 claims 1
• 230000003078 antioxidant effect Effects 0.000 claims 1
• 210000004204 blood vessel Anatomy 0.000 claims 1
• 229910001622 calcium bromide Inorganic materials 0.000 claims 1
• 239000001110 calcium chloride Substances 0.000 claims 1
• 229910001628 calcium chloride Inorganic materials 0.000 claims 1
• WGEFECGEFUFIQW-UHFFFAOYSA-L calcium dibromide Chemical compound [Ca+2].[Br-].[Br-] WGEFECGEFUFIQW-UHFFFAOYSA-L 0.000 claims 1
• 239000002738 chelating agent Substances 0.000 claims 1
• 239000006184 cosolvent Substances 0.000 claims 1
• 230000008021 deposition Effects 0.000 claims 1
• 235000003599 food sweetener Nutrition 0.000 claims 1
• 239000004615 ingredient Substances 0.000 claims 1
• 229960004461 interferon beta-1a Drugs 0.000 claims 1
• 229960003130 interferon gamma Drugs 0.000 claims 1
• 150000002500 ions Chemical class 0.000 claims 1
• OTCKOJUMXQWKQG-UHFFFAOYSA-L magnesium bromide Chemical compound [Mg+2].[Br-].[Br-] OTCKOJUMXQWKQG-UHFFFAOYSA-L 0.000 claims 1
• 229910001623 magnesium bromide Inorganic materials 0.000 claims 1
• 229910001629 magnesium chloride Inorganic materials 0.000 claims 1
• 239000012528 membrane Substances 0.000 claims 1
• XZXHXSATPCNXJR-ZIADKAODSA-N nintedanib Chemical compound O=C1NC2=CC(C(=O)OC)=CC=C2\C1=C(C=1C=CC=CC=1)\NC(C=C1)=CC=C1N(C)C(=O)CN1CCN(C)CC1 XZXHXSATPCNXJR-ZIADKAODSA-N 0.000 claims 1
• 229960004378 nintedanib Drugs 0.000 claims 1
• 239000008363 phosphate buffer Substances 0.000 claims 1
• 230000002685 pulmonary effect Effects 0.000 claims 1
• 239000011780 sodium chloride Substances 0.000 claims 1
• 239000007921 spray Substances 0.000 claims 1
• 239000004094 surface-active agent Substances 0.000 claims 1
• 239000003765 sweetening agent Substances 0.000 claims 1
• 239000006068 taste-masking agent Substances 0.000 claims 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 claims 1
• 229940124597 therapeutic agent Drugs 0.000 claims 1
• 230000001256 tonic effect Effects 0.000 claims 1
• 239000000080 wetting agent Substances 0.000 claims 1