JP7597714B2 - 涙液分泌促進用眼科組成物 - Google Patents
涙液分泌促進用眼科組成物 Download PDFInfo
- Publication number
- JP7597714B2 JP7597714B2 JP2021537387A JP2021537387A JP7597714B2 JP 7597714 B2 JP7597714 B2 JP 7597714B2 JP 2021537387 A JP2021537387 A JP 2021537387A JP 2021537387 A JP2021537387 A JP 2021537387A JP 7597714 B2 JP7597714 B2 JP 7597714B2
- Authority
- JP
- Japan
- Prior art keywords
- ophthalmic composition
- delgocitinib
- salt
- corneal
- eye
- 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
- 239000000203 mixture Substances 0.000 title claims description 46
- 230000028327 secretion Effects 0.000 title claims description 27
- 230000001737 promoting effect Effects 0.000 title claims description 21
- LOWWYYZBZNSPDT-ZBEGNZNMSA-N delgocitinib Chemical compound C[C@H]1CN(C(=O)CC#N)[C@@]11CN(C=2C=3C=CNC=3N=CN=2)CC1 LOWWYYZBZNSPDT-ZBEGNZNMSA-N 0.000 claims description 73
- 150000003839 salts Chemical class 0.000 claims description 48
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 30
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims description 19
- 206010013774 Dry eye Diseases 0.000 claims description 19
- 239000003889 eye drop Substances 0.000 claims description 13
- 229940125772 JTE-052 Drugs 0.000 description 57
- 238000012360 testing method Methods 0.000 description 25
- 208000035475 disorder Diseases 0.000 description 23
- 239000000243 solution Substances 0.000 description 21
- 241000700159 Rattus Species 0.000 description 18
- 230000000694 effects Effects 0.000 description 11
- 238000000034 method Methods 0.000 description 7
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 6
- 229940012356 eye drops Drugs 0.000 description 6
- 230000001965 increasing effect Effects 0.000 description 6
- 208000023275 Autoimmune disease Diseases 0.000 description 5
- 102000015617 Janus Kinases Human genes 0.000 description 5
- 108010024121 Janus Kinases Proteins 0.000 description 5
- 230000008378 epithelial damage Effects 0.000 description 5
- 239000011780 sodium chloride Substances 0.000 description 5
- 238000012453 sprague-dawley rat model Methods 0.000 description 5
- OWTGMPPCCUSXIP-FNXFGIETSA-J tetrasodium;[[(2r,3s,4r,5r)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl] [[[(2r,3s,4r,5r)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl]oxy-oxidophosphoryl] phosphate Chemical compound [Na+].[Na+].[Na+].[Na+].N1([C@@H]2O[C@@H]([C@H]([C@H]2O)O)COP([O-])(=O)OP([O-])(=O)OP([O-])(=O)OP([O-])(=O)OC[C@@H]2[C@H]([C@H]([C@@H](O2)N2C(NC(=O)C=C2)=O)O)O)C=CC(=O)NC1=O OWTGMPPCCUSXIP-FNXFGIETSA-J 0.000 description 5
- 235000001014 amino acid Nutrition 0.000 description 4
- 150000001413 amino acids Chemical class 0.000 description 4
- 201000010099 disease Diseases 0.000 description 4
- 210000004561 lacrimal apparatus Anatomy 0.000 description 4
- 238000004519 manufacturing process Methods 0.000 description 4
- QCHFTSOMWOSFHM-WPRPVWTQSA-N (+)-Pilocarpine Chemical compound C1OC(=O)[C@@H](CC)[C@H]1CC1=CN=CN1C QCHFTSOMWOSFHM-WPRPVWTQSA-N 0.000 description 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- 206010002091 Anaesthesia Diseases 0.000 description 3
- 241000699670 Mus sp. Species 0.000 description 3
- 241000283973 Oryctolagus cuniculus Species 0.000 description 3
- BELBBZDIHDAJOR-UHFFFAOYSA-N Phenolsulfonephthalein Chemical compound C1=CC(O)=CC=C1C1(C=2C=CC(O)=CC=2)C2=CC=CC=C2S(=O)(=O)O1 BELBBZDIHDAJOR-UHFFFAOYSA-N 0.000 description 3
- QCHFTSOMWOSFHM-UHFFFAOYSA-N SJ000285536 Natural products C1OC(=O)C(CC)C1CC1=CN=CN1C QCHFTSOMWOSFHM-UHFFFAOYSA-N 0.000 description 3
- 208000021386 Sjogren Syndrome Diseases 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 230000037005 anaesthesia Effects 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 150000001875 compounds Chemical class 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- GNBHRKFJIUUOQI-UHFFFAOYSA-N fluorescein Chemical class O1C(=O)C2=CC=CC=C2C21C1=CC=C(O)C=C1OC1=CC(O)=CC=C21 GNBHRKFJIUUOQI-UHFFFAOYSA-N 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 238000005259 measurement Methods 0.000 description 3
- 239000002997 ophthalmic solution Substances 0.000 description 3
- 229940054534 ophthalmic solution Drugs 0.000 description 3
- 229960003531 phenolsulfonphthalein Drugs 0.000 description 3
- 229960001416 pilocarpine Drugs 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 238000000585 Mann–Whitney U test Methods 0.000 description 2
- QGMRQYFBGABWDR-UHFFFAOYSA-M Pentobarbital sodium Chemical compound [Na+].CCCC(C)C1(CC)C(=O)NC(=O)[N-]C1=O QGMRQYFBGABWDR-UHFFFAOYSA-M 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 2
- 229910000831 Steel Inorganic materials 0.000 description 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 2
- 230000002378 acidificating effect Effects 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- -1 alkali metal salts Chemical class 0.000 description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 229960002143 fluorescein Drugs 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 150000007529 inorganic bases Chemical class 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 150000007522 mineralic acids Chemical class 0.000 description 2
- 150000007524 organic acids Chemical class 0.000 description 2
- 235000005985 organic acids Nutrition 0.000 description 2
- 150000007530 organic bases Chemical class 0.000 description 2
- 239000008213 purified water Substances 0.000 description 2
- 239000012192 staining solution Substances 0.000 description 2
- 239000010959 steel Substances 0.000 description 2
- 230000001954 sterilising effect Effects 0.000 description 2
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 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
- 238000011282 treatment Methods 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- LSIXBBPOJBJQHN-UHFFFAOYSA-N 2,3-Dimethylbicyclo[2.2.1]hept-2-ene Chemical compound C1CC2C(C)=C(C)C1C2 LSIXBBPOJBJQHN-UHFFFAOYSA-N 0.000 description 1
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 description 1
- 239000004475 Arginine Substances 0.000 description 1
- 239000005711 Benzoic acid Substances 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
- 238000001061 Dunnett's test Methods 0.000 description 1
- 206010015150 Erythema Diseases 0.000 description 1
- 206010015958 Eye pain Diseases 0.000 description 1
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 description 1
- PIWKPBJCKXDKJR-UHFFFAOYSA-N Isoflurane Chemical compound FC(F)OC(Cl)C(F)(F)F PIWKPBJCKXDKJR-UHFFFAOYSA-N 0.000 description 1
- AHLPHDHHMVZTML-BYPYZUCNSA-N L-Ornithine Chemical compound NCCC[C@H](N)C(O)=O AHLPHDHHMVZTML-BYPYZUCNSA-N 0.000 description 1
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 description 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 1
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 description 1
- 206010023644 Lacrimation increased Diseases 0.000 description 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 description 1
- 239000004472 Lysine Substances 0.000 description 1
- MBBZMMPHUWSWHV-BDVNFPICSA-N N-methylglucamine Chemical compound CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 description 1
- GRYLNZFGIOXLOG-UHFFFAOYSA-N Nitric acid Chemical compound O[N+]([O-])=O GRYLNZFGIOXLOG-UHFFFAOYSA-N 0.000 description 1
- AHLPHDHHMVZTML-UHFFFAOYSA-N Orn-delta-NH2 Natural products NCCCC(N)C(O)=O AHLPHDHHMVZTML-UHFFFAOYSA-N 0.000 description 1
- UTJLXEIPEHZYQJ-UHFFFAOYSA-N Ornithine Natural products OC(=O)C(C)CCCN UTJLXEIPEHZYQJ-UHFFFAOYSA-N 0.000 description 1
- 241000283977 Oryctolagus Species 0.000 description 1
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 1
- 229920002385 Sodium hyaluronate Polymers 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- 206010042033 Stevens-Johnson syndrome Diseases 0.000 description 1
- 231100000168 Stevens-Johnson syndrome Toxicity 0.000 description 1
- 238000000692 Student's t-test Methods 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- 230000013564 activation of immune response Effects 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 229910052783 alkali metal Inorganic materials 0.000 description 1
- 229910052784 alkaline earth metal Inorganic materials 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- AZDRQVAHHNSJOQ-UHFFFAOYSA-N alumane Chemical class [AlH3] AZDRQVAHHNSJOQ-UHFFFAOYSA-N 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 150000003863 ammonium salts Chemical class 0.000 description 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 description 1
- 239000000607 artificial tear Substances 0.000 description 1
- 235000003704 aspartic acid Nutrition 0.000 description 1
- 235000010233 benzoic acid Nutrition 0.000 description 1
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 description 1
- KGBXLFKZBHKPEV-UHFFFAOYSA-N boric acid Chemical compound OB(O)O KGBXLFKZBHKPEV-UHFFFAOYSA-N 0.000 description 1
- 239000004327 boric acid Substances 0.000 description 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 1
- 159000000007 calcium salts Chemical class 0.000 description 1
- 229960003333 chlorhexidine gluconate Drugs 0.000 description 1
- YZIYKJHYYHPJIB-UUPCJSQJSA-N chlorhexidine gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.C1=CC(Cl)=CC=C1NC(=N)NC(=N)NCCCCCCNC(=N)NC(=N)NC1=CC=C(Cl)C=C1 YZIYKJHYYHPJIB-UUPCJSQJSA-N 0.000 description 1
- 235000015165 citric acid Nutrition 0.000 description 1
- 210000004087 cornea Anatomy 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- ZBCBWPMODOFKDW-UHFFFAOYSA-N diethanolamine Chemical compound OCCNCCO ZBCBWPMODOFKDW-UHFFFAOYSA-N 0.000 description 1
- HPNMFZURTQLUMO-UHFFFAOYSA-N diethylamine Chemical compound CCNCC HPNMFZURTQLUMO-UHFFFAOYSA-N 0.000 description 1
- 229950003529 diquafosol Drugs 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 210000003560 epithelium corneal Anatomy 0.000 description 1
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 description 1
- 230000001747 exhibiting effect Effects 0.000 description 1
- 238000013230 female C57BL/6J mice Methods 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
- 235000013922 glutamic acid Nutrition 0.000 description 1
- 239000004220 glutamic acid Substances 0.000 description 1
- 230000005934 immune activation Effects 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 239000003983 inhalation anesthetic agent Substances 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 229960002725 isoflurane Drugs 0.000 description 1
- 230000004317 lacrimation Effects 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 159000000003 magnesium salts Chemical class 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
- 239000011976 maleic acid Substances 0.000 description 1
- 229960003194 meglumine Drugs 0.000 description 1
- GXHMMDRXHUIUMN-UHFFFAOYSA-N methanesulfonic acid Chemical compound CS(O)(=O)=O.CS(O)(=O)=O GXHMMDRXHUIUMN-UHFFFAOYSA-N 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- ACTNHJDHMQSOGL-UHFFFAOYSA-N n',n'-dibenzylethane-1,2-diamine Chemical compound C=1C=CC=CC=1CN(CCN)CC1=CC=CC=C1 ACTNHJDHMQSOGL-UHFFFAOYSA-N 0.000 description 1
- 229910017604 nitric acid Inorganic materials 0.000 description 1
- 102000037979 non-receptor tyrosine kinases Human genes 0.000 description 1
- 108091008046 non-receptor tyrosine kinases Proteins 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 229960003104 ornithine Drugs 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- 229960002139 pilocarpine hydrochloride Drugs 0.000 description 1
- RNAICSBVACLLGM-GNAZCLTHSA-N pilocarpine hydrochloride Chemical compound Cl.C1OC(=O)[C@@H](CC)[C@H]1CC1=CN=CN1C RNAICSBVACLLGM-GNAZCLTHSA-N 0.000 description 1
- 230000002980 postoperative effect Effects 0.000 description 1
- 239000001103 potassium chloride Substances 0.000 description 1
- 235000011164 potassium chloride Nutrition 0.000 description 1
- 159000000001 potassium salts Chemical class 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000035807 sensation Effects 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
- 229940010747 sodium hyaluronate Drugs 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- YWIVKILSMZOHHF-QJZPQSOGSA-N sodium;(2s,3s,4s,5r,6r)-6-[(2s,3r,4r,5s,6r)-3-acetamido-2-[(2s,3s,4r,5r,6r)-6-[(2r,3r,4r,5s,6r)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2- Chemical compound [Na+].CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 YWIVKILSMZOHHF-QJZPQSOGSA-N 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000010186 staining Methods 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 230000000472 traumatic effect Effects 0.000 description 1
- 208000005494 xerophthalmia Diseases 0.000 description 1
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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K9/0048—Eye, e.g. artificial tears
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/04—Artificial tears; Irrigation solutions
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Ophthalmology & Optometry (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024207323A JP2025019313A (ja) | 2019-08-07 | 2024-11-28 | 涙液分泌促進用眼科組成物 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2019145670 | 2019-08-07 | ||
| JP2019145670 | 2019-08-07 | ||
| JP2019239605 | 2019-12-27 | ||
| JP2019239605 | 2019-12-27 | ||
| PCT/JP2020/030231 WO2021025129A1 (ja) | 2019-08-07 | 2020-08-06 | 涙液分泌促進用眼科組成物 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024207323A Division JP2025019313A (ja) | 2019-08-07 | 2024-11-28 | 涙液分泌促進用眼科組成物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPWO2021025129A1 JPWO2021025129A1 (https=) | 2021-02-11 |
| JP7597714B2 true JP7597714B2 (ja) | 2024-12-10 |
Family
ID=74503644
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021537387A Active JP7597714B2 (ja) | 2019-08-07 | 2020-08-06 | 涙液分泌促進用眼科組成物 |
| JP2024207323A Pending JP2025019313A (ja) | 2019-08-07 | 2024-11-28 | 涙液分泌促進用眼科組成物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024207323A Pending JP2025019313A (ja) | 2019-08-07 | 2024-11-28 | 涙液分泌促進用眼科組成物 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20220280515A1 (https=) |
| EP (1) | EP4011450A4 (https=) |
| JP (2) | JP7597714B2 (https=) |
| KR (1) | KR20220044288A (https=) |
| CN (2) | CN114173788A (https=) |
| TW (1) | TW202120094A (https=) |
| WO (1) | WO2021025129A1 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4674401A3 (en) * | 2019-12-27 | 2026-02-25 | Rohto Pharmaceutical Co., Ltd | Container accommodating an aqueous ophthalmic composition comprising delgocitinib |
| AU2021318236A1 (en) * | 2020-07-30 | 2023-03-09 | Rohto Pharmaceutical Co., Ltd. | Aqueous composition |
| US20230285564A1 (en) * | 2020-07-30 | 2023-09-14 | Rohto Pharmaceutical Co., Ltd. | Aqueous Composition |
| JP2025014078A (ja) * | 2021-11-30 | 2025-01-29 | 興和株式会社 | 新規ニコチンアミド化合物及びその用途 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009046470A (ja) | 2007-07-11 | 2009-03-05 | Pfizer Inc | ドライアイ障害を治療する医薬組成物および方法 |
| WO2011013785A1 (ja) | 2009-07-31 | 2011-02-03 | 日本たばこ産業株式会社 | 含窒素スピロ環化合物及びその医薬用途 |
| WO2017006968A1 (ja) | 2015-07-07 | 2017-01-12 | 日本たばこ産業株式会社 | ７Ｈ－ピロロ［２，３－ｄ］ピリミジン誘導体の製造方法及びその中間体 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102306276B1 (ko) * | 2013-10-21 | 2021-09-30 | 니뽄 다바코 산교 가부시키가이샤 | 안질환의 치료제 또는 예방제 |
| KR102702286B1 (ko) | 2016-12-21 | 2024-09-04 | 니뽄 다바코 산교 가부시키가이샤 | 7H-피롤로[2,3-d]피리미딘 유도체의 제조 방법 및 그의 공결정 |
| CA3044771A1 (en) * | 2016-12-21 | 2018-06-28 | Japan Tobacco Inc. | Crystalline forms of a janus kinase inhibitor |
| JP7722931B2 (ja) * | 2019-12-27 | 2025-08-13 | ロート製薬株式会社 | 水性組成物 |
| EP4674401A3 (en) * | 2019-12-27 | 2026-02-25 | Rohto Pharmaceutical Co., Ltd | Container accommodating an aqueous ophthalmic composition comprising delgocitinib |
| US20230285564A1 (en) * | 2020-07-30 | 2023-09-14 | Rohto Pharmaceutical Co., Ltd. | Aqueous Composition |
-
2020
- 2020-08-06 KR KR1020227005681A patent/KR20220044288A/ko active Pending
- 2020-08-06 US US17/632,419 patent/US20220280515A1/en active Pending
- 2020-08-06 EP EP20850966.1A patent/EP4011450A4/en active Pending
- 2020-08-06 CN CN202080055566.8A patent/CN114173788A/zh active Pending
- 2020-08-06 CN CN202410802175.8A patent/CN118903144A/zh active Pending
- 2020-08-06 WO PCT/JP2020/030231 patent/WO2021025129A1/ja not_active Ceased
- 2020-08-06 JP JP2021537387A patent/JP7597714B2/ja active Active
- 2020-08-07 TW TW109126866A patent/TW202120094A/zh unknown
-
2024
- 2024-11-28 JP JP2024207323A patent/JP2025019313A/ja active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009046470A (ja) | 2007-07-11 | 2009-03-05 | Pfizer Inc | ドライアイ障害を治療する医薬組成物および方法 |
| WO2011013785A1 (ja) | 2009-07-31 | 2011-02-03 | 日本たばこ産業株式会社 | 含窒素スピロ環化合物及びその医薬用途 |
| WO2017006968A1 (ja) | 2015-07-07 | 2017-01-12 | 日本たばこ産業株式会社 | ７Ｈ－ピロロ［２，３－ｄ］ピリミジン誘導体の製造方法及びその中間体 |
Non-Patent Citations (1)
| Title |
|---|
| 中村雅胤，ドライアイ研究の最前線，日薬理誌，2010年，135，第138-141頁 |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2025019313A (ja) | 2025-02-06 |
| TW202120094A (zh) | 2021-06-01 |
| EP4011450A4 (en) | 2023-08-09 |
| CN118903144A (zh) | 2024-11-08 |
| KR20220044288A (ko) | 2022-04-07 |
| WO2021025129A1 (ja) | 2021-02-11 |
| EP4011450A1 (en) | 2022-06-15 |
| CN114173788A (zh) | 2022-03-11 |
| US20220280515A1 (en) | 2022-09-08 |
| JPWO2021025129A1 (https=) | 2021-02-11 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP7597714B2 (ja) | 涙液分泌促進用眼科組成物 | |
| JP2025094111A (ja) | 翼状片を治療するための組成物及び方法 | |
| JP4934653B2 (ja) | Ｒｈｏキナーゼ阻害剤とβ遮断薬からなる緑内障治療剤 | |
| JP6060168B2 (ja) | レバミピドと涙液保持作用を有する薬剤からなる前眼部疾患治療剤 | |
| KR102902220B1 (ko) | 4-페닐부티르산을 함유하는 노시의 치료 또는 예방제 | |
| JP4482726B2 (ja) | Ｒｈｏキナーゼ阻害剤とプロスタグランジン類からなる緑内障治療剤 | |
| KR20210105916A (ko) | 우루소데옥시콜산을 함유하는 노시의 치료 또는 예방제 | |
| BR112020015567A2 (pt) | medicamento para prevenir ou tratar doença oftálmica associada com neovascularização intraocular e/ou permeabilidade vascular intraocular realçadas | |
| JP7599838B2 (ja) | エピナスチン又はその塩を含有する水性医薬組成物 | |
| WO2022025281A1 (ja) | 水性組成物 | |
| US20230285562A1 (en) | Aqueous Composition | |
| IL259562A (en) | Aminophosphinic derivatives for preventing and treating eye pain | |
| WO2018147409A1 (ja) | 水性点眼点鼻用組成物 | |
| JP2019104740A (ja) | 熱ゲル化人工涙液 | |
| JP2012250951A (ja) | アデノシン誘導体とプロスタグランジン類とβ受容体遮断薬の組合せ剤 | |
| US20100113456A1 (en) | Therapeutic agent for corneal disease | |
| US9187468B2 (en) | Topical ocular analgesic agents | |
| HK40066213A (zh) | 泪液分泌促进用眼科组合物 | |
| JP2024533539A (ja) | ドライアイの予防及び／又は治療剤 | |
| JP2012250953A (ja) | アデノシン誘導体とα２受容体作動薬の組合せ剤 | |
| RU2836815C1 (ru) | Офтальмологические композиции для местного применения на ксантановой основе с сокращенным режимом дозирования | |
| JP2012250949A (ja) | アデノシン誘導体と炭酸脱水酵素阻害剤とβ受容体遮断薬の組合せ剤 | |
| WO2019124523A1 (ja) | ＦＰ作動薬とβ遮断薬を含有する緑内障治療剤 | |
| JP2012250947A (ja) | アデノシン誘導体とβ受容体遮断薬の組合せ剤 | |
| JP2012250950A (ja) | アデノシン誘導体とプロスタグランジン類の組合せ剤 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20230726 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20240507 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20240702 |
|
| 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: 20241029 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20241128 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 7597714 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |