JP2022017260A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2022017260A5 JP2022017260A5 JP2021164372A JP2021164372A JP2022017260A5 JP 2022017260 A5 JP2022017260 A5 JP 2022017260A5 JP 2021164372 A JP2021164372 A JP 2021164372A JP 2021164372 A JP2021164372 A JP 2021164372A JP 2022017260 A5 JP2022017260 A5 JP 2022017260A5
- Authority
- JP
- Japan
- Prior art keywords
- formulation
- amount
- less
- compound
- salt
- 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.)
- Granted
Links
- 239000000203 mixture Substances 0.000 claims description 120
- 238000009472 formulation Methods 0.000 claims description 116
- 150000001875 compounds Chemical class 0.000 claims description 66
- 150000003839 salts Chemical class 0.000 claims description 58
- 239000000375 suspending agent Substances 0.000 claims description 39
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 32
- 239000013078 crystal Substances 0.000 claims description 30
- 239000003755 preservative agent Substances 0.000 claims description 29
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical group [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 28
- 239000000872 buffer Substances 0.000 claims description 26
- 239000012929 tonicity agent Substances 0.000 claims description 25
- 208000002193 Pain Diseases 0.000 claims description 24
- 239000000725 suspension Substances 0.000 claims description 23
- JFPXRFIBKKSHGY-UHFFFAOYSA-N 4-(7-hydroxy-4-oxo-2-propan-2-ylquinazolin-3-yl)benzonitrile Chemical compound CC(C)C1=NC2=CC(O)=CC=C2C(=O)N1C1=CC=C(C#N)C=C1 JFPXRFIBKKSHGY-UHFFFAOYSA-N 0.000 claims description 22
- 239000004094 surface-active agent Substances 0.000 claims description 22
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 21
- 229960004224 tyloxapol Drugs 0.000 claims description 17
- 229920001664 tyloxapol Polymers 0.000 claims description 17
- MDYZKJNTKZIUSK-UHFFFAOYSA-N tyloxapol Chemical compound O=C.C1CO1.CC(C)(C)CC(C)(C)C1=CC=C(O)C=C1 MDYZKJNTKZIUSK-UHFFFAOYSA-N 0.000 claims description 17
- 235000011187 glycerol Nutrition 0.000 claims description 16
- 229920005862 polyol Polymers 0.000 claims description 16
- 150000003077 polyols Chemical class 0.000 claims description 16
- 229940075508 carbomer homopolymer type b Drugs 0.000 claims description 15
- 239000011780 sodium chloride Substances 0.000 claims description 14
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims description 13
- 229940009662 edetate Drugs 0.000 claims description 13
- 229910019142 PO4 Inorganic materials 0.000 claims description 12
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 12
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 12
- 239000010452 phosphate Substances 0.000 claims description 12
- BTBUEUYNUDRHOZ-UHFFFAOYSA-N Borate Chemical compound [O-]B([O-])[O-] BTBUEUYNUDRHOZ-UHFFFAOYSA-N 0.000 claims description 11
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 11
- 229930195725 Mannitol Natural products 0.000 claims description 11
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 11
- 239000000594 mannitol Substances 0.000 claims description 11
- 235000010355 mannitol Nutrition 0.000 claims description 11
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 11
- 230000002335 preservative effect Effects 0.000 claims description 11
- 239000002202 Polyethylene glycol Substances 0.000 claims description 10
- 229920001983 poloxamer Polymers 0.000 claims description 10
- 229920001223 polyethylene glycol Polymers 0.000 claims description 10
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 claims description 10
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 9
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 9
- 239000006172 buffering agent Substances 0.000 claims description 8
- 229960000281 trometamol Drugs 0.000 claims description 8
- 229920002125 Sokalan® Polymers 0.000 claims description 7
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims description 5
- 229960001631 carbomer Drugs 0.000 claims description 5
- 238000003860 storage Methods 0.000 claims description 5
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims description 4
- KQWCLZDEKIKCND-UHFFFAOYSA-N CC(C)c1nc2cc(O)ccc2c(=O)n1-c1ccccc1C#N Chemical compound CC(C)c1nc2cc(O)ccc2c(=O)n1-c1ccccc1C#N KQWCLZDEKIKCND-UHFFFAOYSA-N 0.000 claims description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 4
- 230000001684 chronic effect Effects 0.000 claims description 4
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 3
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 3
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 claims description 3
- GOOHAUXETOMSMM-UHFFFAOYSA-N Propylene oxide Chemical compound CC1CO1 GOOHAUXETOMSMM-UHFFFAOYSA-N 0.000 claims description 3
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 3
- 229920001400 block copolymer Polymers 0.000 claims description 3
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 3
- 229920000136 polysorbate Polymers 0.000 claims description 3
- 229950008882 polysorbate Drugs 0.000 claims description 3
- 235000013772 propylene glycol Nutrition 0.000 claims description 3
- 239000000600 sorbitol Substances 0.000 claims description 3
- 235000010356 sorbitol Nutrition 0.000 claims description 3
- 239000000811 xylitol Substances 0.000 claims description 3
- 235000010447 xylitol Nutrition 0.000 claims description 3
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 3
- 229960002675 xylitol Drugs 0.000 claims description 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims description 2
- BVKZGUZCCUSVTD-UHFFFAOYSA-M Bicarbonate Chemical compound OC([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-M 0.000 claims description 2
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims description 2
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 2
- 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 claims description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims description 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 claims description 2
- 229940072107 ascorbate Drugs 0.000 claims description 2
- 235000010323 ascorbic acid Nutrition 0.000 claims description 2
- 239000011668 ascorbic acid Substances 0.000 claims description 2
- 229940050410 gluconate Drugs 0.000 claims description 2
- 229960003943 hypromellose Drugs 0.000 claims description 2
- 230000002045 lasting effect Effects 0.000 claims description 2
- 238000004062 sedimentation Methods 0.000 claims description 2
- 238000000034 method Methods 0.000 description 53
- 239000002736 nonionic surfactant Substances 0.000 description 19
- 230000009467 reduction Effects 0.000 description 17
- 239000003795 chemical substances by application Substances 0.000 description 13
- 239000000546 pharmaceutical excipient Substances 0.000 description 10
- 208000003556 Dry Eye Syndromes Diseases 0.000 description 9
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 description 7
- 229960000502 poloxamer Drugs 0.000 description 7
- 206010010984 Corneal abrasion Diseases 0.000 description 6
- 208000028006 Corneal injury Diseases 0.000 description 6
- 206010015958 Eye pain Diseases 0.000 description 6
- 208000003923 Hereditary Corneal Dystrophies Diseases 0.000 description 6
- 208000002205 allergic conjunctivitis Diseases 0.000 description 6
- 206010011005 corneal dystrophy Diseases 0.000 description 6
- 206010023332 keratitis Diseases 0.000 description 6
- 201000001119 neuropathy Diseases 0.000 description 6
- 230000007823 neuropathy Effects 0.000 description 6
- -1 or polymorph thereof Substances 0.000 description 6
- 208000033808 peripheral neuropathy Diseases 0.000 description 6
- 238000001356 surgical procedure Methods 0.000 description 6
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Substances N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 description 5
- 229920000858 Cyclodextrin Polymers 0.000 description 4
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 4
- 206010015150 Erythema Diseases 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 229940068196 placebo Drugs 0.000 description 4
- 239000000902 placebo Substances 0.000 description 4
- 235000000346 sugar Nutrition 0.000 description 4
- 230000004304 visual acuity Effects 0.000 description 4
- 241000224422 Acanthamoeba Species 0.000 description 3
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
- 206010010741 Conjunctivitis Diseases 0.000 description 3
- 206010010744 Conjunctivitis allergic Diseases 0.000 description 3
- 206010011013 Corneal erosion Diseases 0.000 description 3
- 206010015084 Episcleritis Diseases 0.000 description 3
- 201000004173 Epithelial basement membrane dystrophy Diseases 0.000 description 3
- 206010015995 Eyelid ptosis Diseases 0.000 description 3
- 208000001640 Fibromyalgia Diseases 0.000 description 3
- 208000010412 Glaucoma Diseases 0.000 description 3
- 208000009329 Graft vs Host Disease Diseases 0.000 description 3
- 208000003084 Graves Ophthalmopathy Diseases 0.000 description 3
- 206010020649 Hyperkeratosis Diseases 0.000 description 3
- 201000002287 Keratoconus Diseases 0.000 description 3
- 208000001126 Keratosis Diseases 0.000 description 3
- 206010065062 Meibomian gland dysfunction Diseases 0.000 description 3
- 206010027137 Meibomianitis Diseases 0.000 description 3
- 208000023715 Ocular surface disease Diseases 0.000 description 3
- 206010034960 Photophobia Diseases 0.000 description 3
- 201000002154 Pterygium Diseases 0.000 description 3
- 241001303601 Rosacea Species 0.000 description 3
- 206010039705 Scleritis Diseases 0.000 description 3
- 208000021386 Sjogren Syndrome Diseases 0.000 description 3
- 206010042033 Stevens-Johnson syndrome Diseases 0.000 description 3
- 231100000168 Stevens-Johnson syndrome Toxicity 0.000 description 3
- 206010044604 Trichiasis Diseases 0.000 description 3
- 238000002679 ablation Methods 0.000 description 3
- 239000002253 acid Substances 0.000 description 3
- 150000007513 acids Chemical class 0.000 description 3
- 208000024998 atopic conjunctivitis Diseases 0.000 description 3
- 210000002469 basement membrane Anatomy 0.000 description 3
- 208000010217 blepharitis Diseases 0.000 description 3
- 201000000009 conjunctivochalasis Diseases 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 208000024908 graft versus host disease Diseases 0.000 description 3
- 201000010884 herpes simplex virus keratitis Diseases 0.000 description 3
- 201000004614 iritis Diseases 0.000 description 3
- 201000010666 keratoconjunctivitis Diseases 0.000 description 3
- 206010023365 keratopathy Diseases 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 238000012986 modification Methods 0.000 description 3
- 230000004048 modification Effects 0.000 description 3
- 201000006417 multiple sclerosis Diseases 0.000 description 3
- 208000004296 neuralgia Diseases 0.000 description 3
- 206010069732 neurotrophic keratopathy Diseases 0.000 description 3
- 230000002085 persistent effect Effects 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- 201000003004 ptosis Diseases 0.000 description 3
- 201000002002 recurrent corneal erosion Diseases 0.000 description 3
- 230000000306 recurrent effect Effects 0.000 description 3
- 238000005057 refrigeration Methods 0.000 description 3
- 201000004700 rosacea Diseases 0.000 description 3
- 230000035807 sensation Effects 0.000 description 3
- 239000012453 solvate Substances 0.000 description 3
- 208000011580 syndromic disease Diseases 0.000 description 3
- 229940124597 therapeutic agent Drugs 0.000 description 3
- 208000018464 vernal keratoconjunctivitis Diseases 0.000 description 3
- 208000005494 xerophthalmia Diseases 0.000 description 3
- 239000001116 FEMA 4028 Substances 0.000 description 2
- 206010020565 Hyperaemia Diseases 0.000 description 2
- 241000283973 Oryctolagus cuniculus Species 0.000 description 2
- WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 description 2
- 235000011175 beta-cyclodextrine Nutrition 0.000 description 2
- 229960004853 betadex Drugs 0.000 description 2
- 239000003093 cationic surfactant Substances 0.000 description 2
- 238000013329 compounding Methods 0.000 description 2
- 210000004087 cornea Anatomy 0.000 description 2
- 239000007857 degradation product Substances 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 230000008569 process Effects 0.000 description 2
- 238000006467 substitution reaction Methods 0.000 description 2
- 150000005846 sugar alcohols Chemical class 0.000 description 2
- 150000008163 sugars Chemical class 0.000 description 2
- 125000004964 sulfoalkyl group Chemical group 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 210000001519 tissue Anatomy 0.000 description 2
- ODLHGICHYURWBS-LKONHMLTSA-N trappsol cyclo Chemical compound CC(O)COC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)COCC(O)C)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1COCC(C)O ODLHGICHYURWBS-LKONHMLTSA-N 0.000 description 2
- 206010052143 Ocular discomfort Diseases 0.000 description 1
- 239000008118 PEG 6000 Substances 0.000 description 1
- 229920002565 Polyethylene Glycol 400 Polymers 0.000 description 1
- 229920002584 Polyethylene Glycol 6000 Polymers 0.000 description 1
- 239000007983 Tris buffer Substances 0.000 description 1
- 238000002441 X-ray diffraction Methods 0.000 description 1
- 125000000129 anionic group Chemical group 0.000 description 1
- 239000003945 anionic surfactant Substances 0.000 description 1
- 239000013011 aqueous formulation Substances 0.000 description 1
- 239000000337 buffer salt Substances 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 229940097362 cyclodextrins Drugs 0.000 description 1
- MTHSVFCYNBDYFN-UHFFFAOYSA-N diethylene glycol Chemical compound OCCOCCO MTHSVFCYNBDYFN-UHFFFAOYSA-N 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 230000004410 intraocular pressure Effects 0.000 description 1
- 239000002563 ionic surfactant Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000002911 mydriatic effect Effects 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 description 1
- 229920001707 polybutylene terephthalate Polymers 0.000 description 1
- 229920001343 polytetrafluoroethylene Polymers 0.000 description 1
- 239000004810 polytetrafluoroethylene Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 230000004489 tear production Effects 0.000 description 1
- WROMPOXWARCANT-UHFFFAOYSA-N tfa trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.OC(=O)C(F)(F)F WROMPOXWARCANT-UHFFFAOYSA-N 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023206043A JP2024037806A (ja) | 2019-02-15 | 2023-12-06 | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
| JP2024039978A JP2024095674A (ja) | 2019-02-15 | 2024-03-14 | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962806705P | 2019-02-15 | 2019-02-15 | |
| US62/806,705 | 2019-02-15 | ||
| JP2020021093A JP6994061B2 (ja) | 2019-02-15 | 2020-02-12 | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020021093A Division JP6994061B2 (ja) | 2019-02-15 | 2020-02-12 | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023206043A Division JP2024037806A (ja) | 2019-02-15 | 2023-12-06 | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
| JP2024039978A Division JP2024095674A (ja) | 2019-02-15 | 2024-03-14 | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022017260A JP2022017260A (ja) | 2022-01-25 |
| JP2022017260A5 true JP2022017260A5 (enExample) | 2023-05-09 |
| JP7465453B2 JP7465453B2 (ja) | 2024-04-11 |
Family
ID=69740424
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020021093A Active JP6994061B2 (ja) | 2019-02-15 | 2020-02-12 | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
| JP2021547131A Pending JP2022520795A (ja) | 2019-02-15 | 2020-02-13 | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
| JP2021164372A Active JP7465453B2 (ja) | 2019-02-15 | 2021-10-06 | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
| JP2023206043A Pending JP2024037806A (ja) | 2019-02-15 | 2023-12-06 | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
| JP2024039978A Pending JP2024095674A (ja) | 2019-02-15 | 2024-03-14 | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
Family Applications Before (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020021093A Active JP6994061B2 (ja) | 2019-02-15 | 2020-02-12 | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
| JP2021547131A Pending JP2022520795A (ja) | 2019-02-15 | 2020-02-13 | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023206043A Pending JP2024037806A (ja) | 2019-02-15 | 2023-12-06 | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
| JP2024039978A Pending JP2024095674A (ja) | 2019-02-15 | 2024-03-14 | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
Country Status (23)
| Country | Link |
|---|---|
| US (3) | US11478480B2 (enExample) |
| EP (1) | EP3923912A1 (enExample) |
| JP (5) | JP6994061B2 (enExample) |
| KR (1) | KR20210127197A (enExample) |
| CN (2) | CN117752662A (enExample) |
| AU (2) | AU2020220957B2 (enExample) |
| BR (1) | BR112021015737A2 (enExample) |
| CA (1) | CA3130237A1 (enExample) |
| CL (1) | CL2021002153A1 (enExample) |
| CO (1) | CO2021010689A2 (enExample) |
| CR (1) | CR20210428A (enExample) |
| EC (1) | ECSP21059628A (enExample) |
| IL (1) | IL284628A (enExample) |
| JO (1) | JOP20210224A1 (enExample) |
| MX (2) | MX2021009704A (enExample) |
| MY (1) | MY206327A (enExample) |
| PE (1) | PE20212106A1 (enExample) |
| PH (1) | PH12021551967A1 (enExample) |
| SA (1) | SA521430043B1 (enExample) |
| SG (1) | SG11202107259QA (enExample) |
| TW (1) | TWI827800B (enExample) |
| WO (1) | WO2020165839A1 (enExample) |
| ZA (1) | ZA202104594B (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JOP20210217A1 (ar) | 2019-02-15 | 2023-01-30 | Novartis Ag | طرق لعلاج ألم سطح عين |
| JP6994061B2 (ja) * | 2019-02-15 | 2022-01-14 | ノバルティス アーゲー | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
| WO2021191273A1 (en) * | 2020-03-24 | 2021-09-30 | Hovione Scientia Limited | Compositions for use in treating meibomian gland dysfunction |
| US12459902B2 (en) * | 2020-08-06 | 2025-11-04 | Bausch + Lomb Ireland Limited | Crystalline forms of 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile and formulations thereof |
| WO2022074557A1 (en) * | 2020-10-07 | 2022-04-14 | Novartis Ag | Drug containing dissolvable ocular inserts and method of using same |
| US20230159202A1 (en) * | 2021-11-23 | 2023-05-25 | Bausch + Lomb Ireland Limited | Method for making a preservative-free packaged ophthalmic device product |
| US20240197691A1 (en) * | 2022-12-15 | 2024-06-20 | Cn2 Therapeutics, Inc. | Tacrolimus compositions and methods of use |
| CN118340775A (zh) * | 2023-01-09 | 2024-07-16 | 维眸生物科技(浙江)有限公司 | 一种含vvn539的眼用组合物及其用途 |
| EP4454639A1 (en) * | 2023-04-14 | 2024-10-30 | Omnivision GmbH | Ophthalmic composition comprising carbomer and taurine |
Family Cites Families (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1280874B (de) | 1963-10-09 | 1968-10-24 | Boehringer Sohn Ingelheim | 2-Methyl-3-(2-dimethylaminophenyl)-8-amino-3H-chinazolon-(4) |
| US4027020A (en) | 1974-10-29 | 1977-05-31 | Millmaster Onyx Corporation | Randomly terminated capped polymers |
| US3931319A (en) | 1974-10-29 | 1976-01-06 | Millmaster Onyx Corporation | Capped polymers |
| US4407791A (en) | 1981-09-28 | 1983-10-04 | Alcon Laboratories, Inc. | Ophthalmic solutions |
| US4525346A (en) | 1981-09-28 | 1985-06-25 | Alcon Laboratories, Inc. | Aqueous antimicrobial ophthalmic solutions |
| US4836986A (en) | 1984-09-28 | 1989-06-06 | Bausch & Lomb Incorporated | Disinfecting and preserving systems and methods of use |
| US5037647A (en) | 1988-09-15 | 1991-08-06 | Alcon Laboratories, Inc. | Aqueous antimicrobial opthalmic solutions comprised of quaternary ammonium compound, citric acid, citrate and sodium chloride |
| US5145643A (en) | 1990-01-05 | 1992-09-08 | Allergan, Inc. | Nonoxidative ophthalmic compositions and methods for preserving and using same |
| US5300287A (en) | 1992-11-04 | 1994-04-05 | Alcon Laboratories, Inc. | Polymeric antimicrobials and their use in pharmaceutical compositions |
| PL201130B1 (pl) | 1999-09-24 | 2009-03-31 | Alcon Inc | Kompozycje zawiesinowe zawierające ciprofloksacynę i deksametazon do podawania miejscowego do oczu, uszu lub nosa |
| GB0412769D0 (en) * | 2004-06-08 | 2004-07-07 | Novartis Ag | Organic compounds |
| TWI358290B (en) * | 2004-12-02 | 2012-02-21 | Alcon Inc | Topical nepafenac formulations |
| AU2006311883A1 (en) | 2005-11-04 | 2007-05-18 | Hydra Biosciences, Inc. | Compounds for modulating TRPV3 function |
| GB0525069D0 (en) | 2005-12-08 | 2006-01-18 | Novartis Ag | Organic compounds |
| GB0525068D0 (en) | 2005-12-08 | 2006-01-18 | Novartis Ag | Organic compounds |
| AU2006330883A1 (en) | 2005-12-22 | 2007-07-05 | Prolexys Pharmaceuticals, Inc. | 3-aryl-substituted quinazolones, and uses thereof |
| TW200738232A (en) | 2006-01-31 | 2007-10-16 | Alcon Mfg Ltd | Use of vanilloid receptor-1 antagonists for the prevention and treatment of glaucoma |
| EP1964548A1 (en) | 2007-03-02 | 2008-09-03 | Novartis AG | Pharmaceutical compositions comprising a calcilytic agent |
| WO2008140750A1 (en) | 2007-05-10 | 2008-11-20 | Hydra Biosciences Inc. | Compounds for modulating trpv3 function |
| BRPI0813825A2 (pt) | 2007-07-18 | 2015-01-06 | Novartis Ag | Combinações sinergísticas de antagonistas de vr-1 e inibidores da cox-2 |
| TW200927192A (en) * | 2007-11-19 | 2009-07-01 | Alcon Res Ltd | Use of TRPV1 receptor antagonists for treating dry eye and ocular pain |
| WO2009081222A1 (en) | 2007-12-21 | 2009-07-02 | Glenmark Pharmaceuticals, S.A. | Substituted tricyclic pyridine or pyrimidine vanilloid receptor ligands |
| CA2707441A1 (en) | 2008-01-09 | 2009-07-16 | Renovis, Inc. | Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same |
| WO2009090548A2 (en) | 2008-01-17 | 2009-07-23 | Glenmark Pharmaceuticals, S.A. | 3-azabicyclo [3.1.0] hexane derivatives as vanilloid receptor ligands |
| WO2009149239A1 (en) | 2008-06-04 | 2009-12-10 | Children's Medical Center Corporation | Methods of modulating angiogenesis via trpv4 |
| WO2010023512A1 (en) | 2008-08-28 | 2010-03-04 | Matrix Laboratories Ltd. | Novel vanilloid receptor modulators, process for their preparation and pharmaceutical compositions containing them |
| US8349852B2 (en) | 2009-01-13 | 2013-01-08 | Novartis Ag | Quinazolinone derivatives useful as vanilloid antagonists |
| EP2316420B1 (en) | 2009-10-22 | 2014-02-26 | Consorzio Universitario Unifarm | Topical ophthalmic composition to reduce pain |
| EP2377850A1 (en) | 2010-03-30 | 2011-10-19 | Pharmeste S.r.l. | TRPV1 vanilloid receptor antagonists with a bicyclic portion |
| EP2627178B1 (en) | 2010-10-11 | 2018-05-02 | Merck Sharp & Dohme Corp. | Quinazolinone-type compounds as crth2 antagonists |
| CN102659629B (zh) * | 2012-02-14 | 2014-03-19 | 杭州华东医药集团新药研究院有限公司 | 化合物及其在制备埃罗替尼中的用途 |
| CN102875480A (zh) | 2012-04-23 | 2013-01-16 | 中国药科大学 | 喹唑啉酮类血管抑制剂、其制备方法及其医药用途 |
| GB201215857D0 (en) | 2012-09-05 | 2012-10-24 | Sylentis Sau | siRNA and their use in methods and compositions for the treatment and/or prevention of eye conditions |
| CA2903114A1 (en) * | 2013-03-15 | 2014-09-25 | Inotek Pharmaceuticals Corporation | Ophthalmic formulations |
| US20150352176A1 (en) * | 2014-06-06 | 2015-12-10 | Newport Research, Inc. | Oil-free and fat-free aqueous suspensions of cyclosporin |
| JP6567648B2 (ja) * | 2014-07-28 | 2019-08-28 | サン、ファーマ、アドバンスト、リサーチ、カンパニー、リミテッドＳｕｎ Ｐｈａｒｍａ Ａｄｖａｎｃｅｄ Ｒｅｓｅａｒｃｈ Ｃｏｍｐａｎｙ Ｌｉｍｉｔｅｄ | 薬物のバイオアベイラビリティーの増加および／または眼作用の持続方法 |
| PL3332767T3 (pl) * | 2014-09-15 | 2019-10-31 | Verona Pharma Plc | Płynna formulacja wziewna zawierająca RPL554 |
| PT3721868T (pt) * | 2015-01-26 | 2022-08-12 | Bausch & Lomb | Composição para suspensão oftálmica |
| JP7106528B2 (ja) | 2016-09-20 | 2022-07-26 | グラクソスミスクライン、インテレクチュアル、プロパティー、（ナンバー２）、リミテッド | Ｔｒｐｖ４拮抗薬 |
| TW201825458A (zh) | 2016-09-20 | 2018-07-16 | 英商葛蘭素史克智慧財產（第二）有限公司 | Ｔｒｐｖ４拮抗劑 |
| US10590077B2 (en) | 2016-09-20 | 2020-03-17 | Glaxosmithkline Intellectual Property Development Limited | TRPV4 antagonists |
| JP6994061B2 (ja) * | 2019-02-15 | 2022-01-14 | ノバルティス アーゲー | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
| JOP20210217A1 (ar) | 2019-02-15 | 2023-01-30 | Novartis Ag | طرق لعلاج ألم سطح عين |
-
2020
- 2020-02-12 JP JP2020021093A patent/JP6994061B2/ja active Active
- 2020-02-13 PH PH1/2021/551967A patent/PH12021551967A1/en unknown
- 2020-02-13 CN CN202310997308.7A patent/CN117752662A/zh active Pending
- 2020-02-13 AU AU2020220957A patent/AU2020220957B2/en active Active
- 2020-02-13 CN CN202010091672.3A patent/CN111568906B/zh active Active
- 2020-02-13 TW TW109104510A patent/TWI827800B/zh active
- 2020-02-13 JO JOP/2021/0224A patent/JOP20210224A1/ar unknown
- 2020-02-13 PE PE2021001336A patent/PE20212106A1/es unknown
- 2020-02-13 CA CA3130237A patent/CA3130237A1/en active Pending
- 2020-02-13 EP EP20708630.7A patent/EP3923912A1/en active Pending
- 2020-02-13 KR KR1020217028995A patent/KR20210127197A/ko not_active Ceased
- 2020-02-13 MY MYPI2021003795A patent/MY206327A/en unknown
- 2020-02-13 WO PCT/IB2020/051211 patent/WO2020165839A1/en not_active Ceased
- 2020-02-13 JP JP2021547131A patent/JP2022520795A/ja active Pending
- 2020-02-13 CR CR20210428A patent/CR20210428A/es unknown
- 2020-02-13 SG SG11202107259QA patent/SG11202107259QA/en unknown
- 2020-02-13 BR BR112021015737-9A patent/BR112021015737A2/pt unknown
- 2020-02-13 MX MX2021009704A patent/MX2021009704A/es unknown
- 2020-02-13 US US16/789,976 patent/US11478480B2/en active Active
- 2020-08-24 US US17/000,953 patent/US20200390767A1/en not_active Abandoned
-
2021
- 2021-07-01 ZA ZA2021/04594A patent/ZA202104594B/en unknown
- 2021-07-05 IL IL284628A patent/IL284628A/en unknown
- 2021-08-12 SA SA521430043A patent/SA521430043B1/ar unknown
- 2021-08-12 EC ECSENADI202159628A patent/ECSP21059628A/es unknown
- 2021-08-12 MX MX2024002989A patent/MX2024002989A/es unknown
- 2021-08-13 CO CONC2021/0010689A patent/CO2021010689A2/es unknown
- 2021-08-13 CL CL2021002153A patent/CL2021002153A1/es unknown
- 2021-10-06 JP JP2021164372A patent/JP7465453B2/ja active Active
-
2022
- 2022-09-08 US US17/930,578 patent/US12290517B2/en active Active
-
2023
- 2023-06-21 AU AU2023203933A patent/AU2023203933B2/en active Active
- 2023-12-06 JP JP2023206043A patent/JP2024037806A/ja active Pending
-
2024
- 2024-03-14 JP JP2024039978A patent/JP2024095674A/ja active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2022017260A5 (enExample) | ||
| JP2023058574A (ja) | アトロピン含有水性組成物 | |
| JP7465453B2 (ja) | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 | |
| EA034839B1 (ru) | Офтальмологический раствор | |
| WO2014204791A1 (en) | Ophthalmic lipophilic and hydrophilic drug delivery vehicle formulations | |
| CN106999543B (zh) | 包含环孢霉素和海藻糖的眼用组合物 | |
| TW202114697A (zh) | 用於穩定包括藥物的水性組成物之pH值的方法 | |
| JP2024161426A (ja) | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの結晶形態及びその製剤 | |
| EP3718535A1 (en) | Ophthalmic compositions containing a nitric oxide releasing prostamide | |
| KR102633606B1 (ko) | 활성 성분으로서 티오트로피움을 포함하는, 근시 예방, 근시 치료, 및/또는 근시 진행 예방을 위한 제제 | |
| US12459902B2 (en) | Crystalline forms of 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile and formulations thereof | |
| TW201838629A (zh) | 用於預防近視、治療近視及／或預防近視增長之包含蕪地銨作爲活性成分的藥劑 | |
| CN116897046A (zh) | 含有熊去氧胆酸或其盐的水性医药组合物 | |
| KR20120124059A (ko) | 치환된 감마 락탐을 함유하는 안과 제제 및 이의 사용 방법 | |
| JP7723851B1 (ja) | アトロピン含有水性医薬組成物 | |
| JP7427308B2 (ja) | 網膜の神経細胞の保護剤 | |
| JP2019163227A (ja) | 医薬組成物 | |
| TH2101004824A (th) | สูตรผสมของ 4-(7-ไฮดรอกซี-2-ไอโซโพรพิล-4-ออกโซ-4h-ควินาโซลิน-3-อิล)-เบนโซไนไตรล์ | |
| HK40016534A (en) | Agent for preventing myopia, treating myopia, and/or preventing myopia progression comprising tiotropium as active ingredient |