JPWO2020165838A5 - - Google Patents
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- Publication number
- JPWO2020165838A5 JPWO2020165838A5 JP2021547546A JP2021547546A JPWO2020165838A5 JP WO2020165838 A5 JPWO2020165838 A5 JP WO2020165838A5 JP 2021547546 A JP2021547546 A JP 2021547546A JP 2021547546 A JP2021547546 A JP 2021547546A JP WO2020165838 A5 JPWO2020165838 A5 JP WO2020165838A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- subject
- corneal
- pain
- reduction
- 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
- 238000000034 method Methods 0.000 claims description 52
- 150000001875 compounds Chemical class 0.000 claims description 49
- 208000002193 Pain Diseases 0.000 claims description 37
- 230000036407 pain Effects 0.000 claims description 34
- 230000009467 reduction Effects 0.000 claims description 23
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims description 10
- 206010015958 Eye pain Diseases 0.000 claims description 10
- 239000000902 placebo Substances 0.000 claims description 10
- 229940068196 placebo Drugs 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 9
- 239000012453 solvate Substances 0.000 claims description 9
- 206010010984 Corneal abrasion Diseases 0.000 claims description 8
- 208000028006 Corneal injury Diseases 0.000 claims description 8
- 208000003923 Hereditary Corneal Dystrophies Diseases 0.000 claims description 8
- 208000002205 allergic conjunctivitis Diseases 0.000 claims description 8
- 206010011005 corneal dystrophy Diseases 0.000 claims description 8
- 206010023332 keratitis Diseases 0.000 claims description 8
- 201000001119 neuropathy Diseases 0.000 claims description 8
- 230000007823 neuropathy Effects 0.000 claims description 8
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 8
- 238000001356 surgical procedure Methods 0.000 claims description 8
- 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 6
- 206010015150 Erythema Diseases 0.000 claims description 6
- 241000224422 Acanthamoeba Species 0.000 claims description 4
- 206010010741 Conjunctivitis Diseases 0.000 claims description 4
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims description 4
- 206010011013 Corneal erosion Diseases 0.000 claims description 4
- 206010015084 Episcleritis Diseases 0.000 claims description 4
- 201000004173 Epithelial basement membrane dystrophy Diseases 0.000 claims description 4
- 206010015995 Eyelid ptosis Diseases 0.000 claims description 4
- 208000001640 Fibromyalgia Diseases 0.000 claims description 4
- 208000010412 Glaucoma Diseases 0.000 claims description 4
- 208000009329 Graft vs Host Disease Diseases 0.000 claims description 4
- 208000003084 Graves Ophthalmopathy Diseases 0.000 claims description 4
- 206010020649 Hyperkeratosis Diseases 0.000 claims description 4
- 201000002287 Keratoconus Diseases 0.000 claims description 4
- 208000001126 Keratosis Diseases 0.000 claims description 4
- 206010065062 Meibomian gland dysfunction Diseases 0.000 claims description 4
- 206010027137 Meibomianitis Diseases 0.000 claims description 4
- 208000023715 Ocular surface disease Diseases 0.000 claims description 4
- 201000002154 Pterygium Diseases 0.000 claims description 4
- 241001303601 Rosacea Species 0.000 claims description 4
- 206010039705 Scleritis Diseases 0.000 claims description 4
- 208000021386 Sjogren Syndrome Diseases 0.000 claims description 4
- 206010042033 Stevens-Johnson syndrome Diseases 0.000 claims description 4
- 231100000168 Stevens-Johnson syndrome Toxicity 0.000 claims description 4
- 206010044604 Trichiasis Diseases 0.000 claims description 4
- 208000024998 atopic conjunctivitis Diseases 0.000 claims description 4
- 210000002469 basement membrane Anatomy 0.000 claims description 4
- 208000010217 blepharitis Diseases 0.000 claims description 4
- 201000000009 conjunctivochalasis Diseases 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 208000024908 graft versus host disease Diseases 0.000 claims description 4
- 201000010884 herpes simplex virus keratitis Diseases 0.000 claims description 4
- 201000004614 iritis Diseases 0.000 claims description 4
- 201000010666 keratoconjunctivitis Diseases 0.000 claims description 4
- 206010023365 keratopathy Diseases 0.000 claims description 4
- 201000006417 multiple sclerosis Diseases 0.000 claims description 4
- 208000004296 neuralgia Diseases 0.000 claims description 4
- 206010069732 neurotrophic keratopathy Diseases 0.000 claims description 4
- 201000003004 ptosis Diseases 0.000 claims description 4
- 201000002002 recurrent corneal erosion Diseases 0.000 claims description 4
- 230000000306 recurrent effect Effects 0.000 claims description 4
- 201000004700 rosacea Diseases 0.000 claims description 4
- 208000011580 syndromic disease Diseases 0.000 claims description 4
- 208000018464 vernal keratoconjunctivitis Diseases 0.000 claims description 4
- 230000000007 visual effect Effects 0.000 claims description 4
- 208000005494 xerophthalmia Diseases 0.000 claims description 4
- 206010020565 Hyperaemia Diseases 0.000 claims description 3
- 239000003814 drug Substances 0.000 description 7
- 239000013078 crystal Substances 0.000 description 6
- 230000001684 chronic effect Effects 0.000 description 5
- 206010034960 Photophobia Diseases 0.000 description 3
- 230000002045 lasting effect Effects 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 230000004048 modification Effects 0.000 description 3
- 238000012986 modification Methods 0.000 description 3
- 230000035807 sensation Effects 0.000 description 3
- 238000006467 substitution reaction Methods 0.000 description 3
- 229940124597 therapeutic agent Drugs 0.000 description 3
- 238000002679 ablation Methods 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 230000008569 process Effects 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 206010013774 Dry eye Diseases 0.000 description 1
- 208000006550 Mydriasis Diseases 0.000 description 1
- 206010052143 Ocular discomfort Diseases 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 210000004087 cornea Anatomy 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 230000004410 intraocular pressure Effects 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000004489 tear production Effects 0.000 description 1
- 230000004304 visual acuity Effects 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024177283A JP2025004186A (ja) | 2019-02-15 | 2024-10-09 | 眼表面疼痛を治療する方法 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962806682P | 2019-02-15 | 2019-02-15 | |
| US62/806,682 | 2019-02-15 | ||
| PCT/IB2020/051210 WO2020165838A1 (en) | 2019-02-15 | 2020-02-13 | Methods for treating ocular surface pain |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024177283A Division JP2025004186A (ja) | 2019-02-15 | 2024-10-09 | 眼表面疼痛を治療する方法 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022520832A JP2022520832A (ja) | 2022-04-01 |
| JPWO2020165838A5 true JPWO2020165838A5 (https=) | 2023-02-21 |
| JP2022520832A5 JP2022520832A5 (https=) | 2023-02-21 |
| JP7571037B2 JP7571037B2 (ja) | 2024-10-22 |
Family
ID=69740423
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021547546A Active JP7571037B2 (ja) | 2019-02-15 | 2020-02-13 | 眼表面疼痛を治療する方法 |
| JP2024177283A Pending JP2025004186A (ja) | 2019-02-15 | 2024-10-09 | 眼表面疼痛を治療する方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024177283A Pending JP2025004186A (ja) | 2019-02-15 | 2024-10-09 | 眼表面疼痛を治療する方法 |
Country Status (17)
| Country | Link |
|---|---|
| US (4) | US20200261456A1 (https=) |
| EP (1) | EP3923909A1 (https=) |
| JP (2) | JP7571037B2 (https=) |
| KR (1) | KR20210129677A (https=) |
| CN (1) | CN113453686B (https=) |
| AU (2) | AU2020222348B2 (https=) |
| BR (1) | BR112021015998A2 (https=) |
| CA (1) | CA3130038A1 (https=) |
| CL (1) | CL2021002152A1 (https=) |
| IL (1) | IL284629A (https=) |
| JO (1) | JOP20210217A1 (https=) |
| MX (2) | MX2021009702A (https=) |
| PH (1) | PH12021551968A1 (https=) |
| SG (1) | SG11202107260VA (https=) |
| TW (2) | TW202515576A (https=) |
| WO (1) | WO2020165838A1 (https=) |
| ZA (1) | ZA202104593B (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2022029656A1 (en) * | 2020-08-06 | 2022-02-10 | Novartis Ag | Crystalline forms of 4-(7-hydroxy-2-isopropyl-4-oxo-4h-quinazolin-3-yl)-benzonitrile and formulations thereof |
| CN119184616A (zh) * | 2024-09-03 | 2024-12-27 | 中山大学附属第三医院粤东医院(梅州市梅县区人民医院) | 一种疼痛等级的测评方法及其评估系统 |
Family Cites Families (28)
| 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) |
| GB0412769D0 (en) * | 2004-06-08 | 2004-07-07 | Novartis Ag | Organic compounds |
| US7893260B2 (en) | 2005-11-04 | 2011-02-22 | Hydra Biosciences, Inc. | Substituted quinazolin-4-one compounds for antagonizing 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 |
| BRPI0620264A2 (pt) | 2005-12-22 | 2011-11-08 | Prolexys Pharmaceuticals Inc | quinazolonas aril-substituìdas e sua utilização |
| TW200738232A (en) | 2006-01-31 | 2007-10-16 | Alcon Mfg Ltd | Use of vanilloid receptor-1 antagonists for the prevention and treatment of glaucoma |
| WO2008140750A1 (en) | 2007-05-10 | 2008-11-20 | Hydra Biosciences Inc. | Compounds for modulating trpv3 function |
| AR067631A1 (es) | 2007-07-18 | 2009-10-21 | Novartis Ag | Combinaciones sinergicas de antagonistas de vr-1 e inhibidores de cox-2 , composicion farmaceutica y uso |
| 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 |
| EP2390327A1 (en) * | 2010-05-27 | 2011-11-30 | Sylentis S.A. | siRNA and their use in methods and compositions for the treatment and/or prevention of eye conditions |
| EP2627178B1 (en) | 2010-10-11 | 2018-05-02 | Merck Sharp & Dohme Corp. | Quinazolinone-type compounds as crth2 antagonists |
| 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 |
| US9827225B2 (en) * | 2016-01-25 | 2017-11-28 | Jenivision Inc. | Use of prostacyclin antagonists for treating ocular surface nociception |
| US10590077B2 (en) | 2016-09-20 | 2020-03-17 | Glaxosmithkline Intellectual Property Development Limited | TRPV4 antagonists |
| CN109790116B (zh) | 2016-09-20 | 2022-10-28 | 葛兰素史密斯克莱知识产权（第2 号）有限公司 | Trpv4拮抗剂 |
| 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 |
| 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 |
| JP2022520410A (ja) * | 2019-02-15 | 2022-03-30 | 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）－ベンゾニトリルの結晶形態及びその製剤 |
-
2020
- 2020-02-13 SG SG11202107260VA patent/SG11202107260VA/en unknown
- 2020-02-13 PH PH1/2021/551968A patent/PH12021551968A1/en unknown
- 2020-02-13 KR KR1020217028994A patent/KR20210129677A/ko active Pending
- 2020-02-13 WO PCT/IB2020/051210 patent/WO2020165838A1/en not_active Ceased
- 2020-02-13 TW TW113123791A patent/TW202515576A/zh unknown
- 2020-02-13 JP JP2021547546A patent/JP7571037B2/ja active Active
- 2020-02-13 MX MX2021009702A patent/MX2021009702A/es unknown
- 2020-02-13 BR BR112021015998-3A patent/BR112021015998A2/pt unknown
- 2020-02-13 EP EP20708629.9A patent/EP3923909A1/en active Pending
- 2020-02-13 CA CA3130038A patent/CA3130038A1/en active Pending
- 2020-02-13 US US16/789,963 patent/US20200261456A1/en not_active Abandoned
- 2020-02-13 CN CN202080013685.7A patent/CN113453686B/zh active Active
- 2020-02-13 TW TW109104537A patent/TWI878266B/zh active
- 2020-02-13 AU AU2020222348A patent/AU2020222348B2/en active Active
-
2021
- 2021-04-08 US US17/225,290 patent/US11234982B2/en active Active
- 2021-07-01 ZA ZA2021/04593A patent/ZA202104593B/en unknown
- 2021-07-05 IL IL284629A patent/IL284629A/en unknown
- 2021-08-12 MX MX2025000353A patent/MX2025000353A/es unknown
- 2021-08-12 JO JOP/2021/0217A patent/JOP20210217A1/ar unknown
- 2021-08-13 CL CL2021002152A patent/CL2021002152A1/es unknown
-
2022
- 2022-03-08 US US17/653,982 patent/US20220193078A1/en not_active Abandoned
-
2023
- 2023-06-14 AU AU2023203716A patent/AU2023203716B2/en active Active
-
2024
- 2024-03-06 US US18/597,497 patent/US20240342174A1/en active Pending
- 2024-10-09 JP JP2024177283A patent/JP2025004186A/ja active Pending
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