JPWO2021247900A5 - - Google Patents
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- JPWO2021247900A5 JPWO2021247900A5 JP2022574480A JP2022574480A JPWO2021247900A5 JP WO2021247900 A5 JPWO2021247900 A5 JP WO2021247900A5 JP 2022574480 A JP2022574480 A JP 2022574480A JP 2022574480 A JP2022574480 A JP 2022574480A JP WO2021247900 A5 JPWO2021247900 A5 JP WO2021247900A5
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- pharmaceutical composition
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- pharma
- eye disease
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- 208000030533 eye disease Diseases 0.000 claims description 14
- 208000002158 Proliferative Vitreoretinopathy Diseases 0.000 claims description 9
- 206010038934 Retinopathy proliferative Diseases 0.000 claims description 9
- 208000021971 neovascular inflammatory vitreoretinopathy Diseases 0.000 claims description 9
- 230000006785 proliferative vitreoretinopathy Effects 0.000 claims description 9
- 206010038848 Retinal detachment Diseases 0.000 claims description 6
- 230000004264 retinal detachment Effects 0.000 claims description 5
- 210000001525 retina Anatomy 0.000 claims description 3
- 206010061218 Inflammation Diseases 0.000 claims description 2
- 230000004663 cell proliferation Effects 0.000 claims description 2
- 230000008602 contraction Effects 0.000 claims description 2
- 230000004054 inflammatory process Effects 0.000 claims description 2
- 238000000034 method Methods 0.000 claims description 2
- 230000035755 proliferation Effects 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 23
- 150000001875 compounds Chemical class 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 10
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 3
- 208000000208 Wet Macular Degeneration Diseases 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 claims 1
- 201000007917 background diabetic retinopathy Diseases 0.000 claims 1
- 210000003161 choroid Anatomy 0.000 claims 1
- 210000004240 ciliary body Anatomy 0.000 claims 1
- 230000007705 epithelial mesenchymal transition Effects 0.000 claims 1
- 210000000554 iris Anatomy 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 201000007914 proliferative diabetic retinopathy Diseases 0.000 claims 1
- 210000003583 retinal pigment epithelium Anatomy 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 210000005167 vascular cell Anatomy 0.000 claims 1
- 210000004127 vitreous body Anatomy 0.000 claims 1
- 230000002207 retinal effect Effects 0.000 description 4
- 238000001356 surgical procedure Methods 0.000 description 4
- 238000004458 analytical method Methods 0.000 description 2
- 208000014674 injury Diseases 0.000 description 2
- 239000012528 membrane Substances 0.000 description 2
- 230000002093 peripheral effect Effects 0.000 description 2
- 230000008733 trauma Effects 0.000 description 2
- XMGGYBQTSVRRCF-VQHVLOKHSA-N 2-[[(e)-3-[4-(difluoromethoxy)-3-methoxyphenyl]prop-2-enoyl]amino]benzoic acid Chemical compound C1=C(OC(F)F)C(OC)=CC(\C=C\C(=O)NC=2C(=CC=CC=2)C(O)=O)=C1 XMGGYBQTSVRRCF-VQHVLOKHSA-N 0.000 description 1
- 208000002367 Retinal Perforations Diseases 0.000 description 1
- 208000017442 Retinal disease Diseases 0.000 description 1
- 206010038897 Retinal tear Diseases 0.000 description 1
- 206010038923 Retinopathy Diseases 0.000 description 1
- 208000034698 Vitreous haemorrhage Diseases 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 230000012292 cell migration Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000001294 liquid chromatography-tandem mass spectrometry Methods 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 238000011002 quantification Methods 0.000 description 1
- 208000019793 rhegmatogenous retinal detachment Diseases 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- 230000029663 wound healing Effects 0.000 description 1
Description
いくつかの実施形態において、眼疾患は、創傷治癒に関連する眼疾患である。いくつかの実施形態において、上記状態は、増殖性硝子体網膜症（ＰＶＲ）である。ＰＶＲは、裂孔原性網膜剥離と網膜剥離を補正する関連手術との合併症として発症し得る疾患である。ＰＶＲは、網膜における破壊又は外傷後の細胞の遊走及び増殖に関連しており、網膜周辺領域における膜の形成、その後の、網膜剥離を引き起こし得る膜の収縮及び網膜における牽引につながり得る。増殖性硝子体網膜症はまた、高度硝子体退縮又は高度網膜周囲増殖とも称され得る。ＰＶＲの可能性に影響する因子として、手術前のＰＶＲの存在、手術を行う前の網膜剥離の継続期間、網膜裂傷のサイズ、眼内炎症の存在、硝子体出血、及び眼への外傷が挙げられる。ＰＶＲは、網膜復位術の成功に対する最も大きな障害であるとして記載されている。Ｓｐｉｒｎ ａｎｄ Ｒｅｇｉｌｌｏ；Ｐｒｏｌｉｆｅｒａｔｉｖｅ
Ｒｅｔｉｎｏｐａｔｈｙ；Ｒｅｔｉｎａｌ Ｐｈｙｓｉｃｉａｎ；Ｊａｎ／Ｆｅｂ ２００８を参照されたい。
In some embodiments, the eye disease is an eye disease associated with wound healing. In some embodiments, the condition is proliferative vitreoretinopathy (PVR). PVR is a disease that can develop as a complication of rhegmatogenous retinal detachment and associated surgery to correct the retinal detachment. PVR is associated with cell migration and proliferation after breakage or trauma in the retina, which can lead to the formation of a membrane in the peripheral retinal area, followed by contraction of the membrane and traction on the retina that can cause retinal detachment. Proliferative vitreoretinopathy can also be referred to as severe vitreous involution or severe peripheral retinal proliferation. Factors that influence the likelihood of PVR include the presence of PVR before surgery, the duration of retinal detachment before surgery, the size of the retinal break, the presence of intraocular inflammation, vitreous hemorrhage, and trauma to the eye. PVR has been described as the greatest obstacle to successful retinal reattachment surgery. Spirn and Regillo; Proliferative
See Retinopathy; Retinal Physician; Jan/Feb 2008 .
血漿中の（Ｅ）－２－［［３－メトキシ－４－（ジフルオロメトキシ）フェニル－１－オキソ－２－プロペニル］アミノ］安息香酸の濃度を、有効なＬＣ－ＭＳ／ＭＳ法を使用して求めた。非コンパートメント解析を、ＷｉｎＮｏｎＬｉｎソフトウエアを使用して実施した。名目上の用量及びサンプリング時間を使用した。定量下限未満の濃度値を薬物動態分析についてゼロとして処理した。結果を表１Ｂに示す。ヒトにおける平均薬物動態プロファイルも図１に示す。
Claims (19)
前記化合物又はその薬学的に許容可能な塩が、１日１回及び１日２回から選択される頻度で投与される、医薬組成物。 1. A pharmaceutical composition for preventing, treating, reducing the severity and/or reducing the likelihood of recurrence of an eye disease in a subject , comprising a compound of formula (I):
The pharmaceutical composition, wherein the compound, or a pharma- ceutically acceptable salt thereof, is administered at a frequency selected from once a day and twice a day.
前記投与される化合物の量が、１日５ｍｇ～２５０ｍｇの範囲内であり、又は、前記投与される薬学的に許容可能な塩の量が、１日５ｍｇ～２５０ｍｇの範囲内の化合物の量を与える、前記医薬組成物。 1. A pharmaceutical composition for preventing, treating, reducing the severity and/or reducing the likelihood of recurrence of an eye disease in a subject , comprising a compound of formula (I):
The pharmaceutical composition, wherein the amount of the compound administered is in the range of 5 mg to 250 mg per day, or the amount of a pharma- ceutically acceptable salt administered provides an amount of the compound in the range of 5 mg to 250 mg per day .
第１用量又は一連の第１用量の前記式（Ｉ）の化合物又はその薬学的に許容可能な塩が前記対象に投与されるものであり、及び
第２用量又は一連の第２用量の前記式（Ｉ）の化合物又はその薬学的に許容可能な塩が前記対象に続いて投与されるものであり、
前記又は各第１用量における化合物又は薬学的に許容可能な塩の量が、前記又は各第２用量における化合物又は薬学的に許容可能な塩の量よりも多い、前記医薬組成物。 1. A pharmaceutical composition for preventing, treating, reducing the severity and/or reducing the likelihood of recurrence of an eye disease in a subject , comprising a compound of formula (I):
a first dose or a series of first doses of said compound of formula (I) or a pharma- ceutically acceptable salt thereof is administered to said subject; and
a second dose or series of second doses of said compound of formula (I) or a pharma- ceutically acceptable salt thereof is subsequently administered to said subject;
The pharmaceutical composition, wherein the amount of compound or pharma- ceutically acceptable salt in the or each first dose is greater than the amount of compound or pharma- ceutically acceptable salt in the or each second dose.
である、請求項１～１１のいずれか一項に記載の医薬組成物。 The pharmaceutical composition according to any one of claims 1 to 11 , wherein the eye disease is an eye disease associated with non-vascular cell proliferation, epithelial-mesenchymal transition, and/or tissue contraction.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2020901856A AU2020901856A0 (en) | 2020-06-05 | Compounds and Methods for the Treatment of Eye Disorders | |
| AU2020901858 | 2020-06-05 | ||
| AU2020901856 | 2020-06-05 | ||
| AU2020901858A AU2020901858A0 (en) | 2020-06-05 | Compounds and Methods for the Treatment of Eye Disorders | |
| PCT/US2021/035749 WO2021247900A1 (en) | 2020-06-05 | 2021-06-03 | Compounds and methods for the treatment of eye disorders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2023529845A JP2023529845A (en) | 2023-07-12 |
| JPWO2021247900A5 true JPWO2021247900A5 (en) | 2024-05-15 |
Family
ID=78829970
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022574480A Pending JP2023529845A (en) | 2020-06-05 | 2021-06-03 | Compounds and methods for the treatment of ocular disorders |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20230270703A1 (en) |
| EP (1) | EP4161527A4 (en) |
| JP (1) | JP2023529845A (en) |
| KR (1) | KR20230024331A (en) |
| CN (1) | CN116033901A (en) |
| AU (1) | AU2021284380A1 (en) |
| BR (1) | BR112022024728A2 (en) |
| CA (1) | CA3185849A1 (en) |
| IL (1) | IL298733A (en) |
| MX (1) | MX2022015327A (en) |
| WO (2) | WO2021247900A1 (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20230156931A (en) * | 2021-03-17 | 2023-11-15 | 오쿠렉스 피티와이 리미티드 | Compounds and salts and polymorphs thereof for the treatment of diseases |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU6748398A (en) * | 1997-04-18 | 1998-11-13 | Kissei Pharmaceutical Co. Ltd. | Preventives or remedies for diseases affecting excessive proliferation of retinal pigment epithelial cells |
| CN1602207A (en) * | 2001-12-11 | 2005-03-30 | 法布罗根股份有限公司 | Methods for inhibiting ocular processes |
| DK1660057T3 (en) * | 2003-08-27 | 2012-08-20 | Ophthotech Corp | Combination therapy for the treatment of neovascular eye disorders |
| US8168584B2 (en) * | 2005-10-08 | 2012-05-01 | Potentia Pharmaceuticals, Inc. | Methods of treating age-related macular degeneration by compstatin and analogs thereof |
| EP3797775A1 (en) * | 2007-10-19 | 2021-03-31 | Novartis AG | Compositions and methods for treatment of diabetic retinopathy |
| WO2010137681A1 (en) * | 2009-05-29 | 2010-12-02 | 参天製薬株式会社 | Prophylactic or therapeutic agent for retinal diseases comprising tranilast, method for prevention or treatment of retinal diseases, and tranilast or pharmaceutically acceptable salt thereof and use thereof |
| CA2815390C (en) * | 2010-11-24 | 2021-07-13 | Fibrotech Therapeutics Pty Ltd | Methods of treating eye diseases associated with inflammation and vascular proliferation |
| US10780070B2 (en) * | 2013-10-18 | 2020-09-22 | The Schepens Eye Research Institute, Inc. | Alpha-aminoadipate for treatment of vision loss and restoring sight |
-
2021
- 2021-06-03 WO PCT/US2021/035749 patent/WO2021247900A1/en unknown
- 2021-06-03 WO PCT/US2021/035750 patent/WO2021247901A1/en active Application Filing
- 2021-06-03 US US18/007,714 patent/US20230270703A1/en active Pending
- 2021-06-03 BR BR112022024728A patent/BR112022024728A2/en unknown
- 2021-06-03 JP JP2022574480A patent/JP2023529845A/en active Pending
- 2021-06-03 MX MX2022015327A patent/MX2022015327A/en unknown
- 2021-06-03 CA CA3185849A patent/CA3185849A1/en active Pending
- 2021-06-03 AU AU2021284380A patent/AU2021284380A1/en active Pending
- 2021-06-03 EP EP21818477.8A patent/EP4161527A4/en active Pending
- 2021-06-03 CN CN202180056862.4A patent/CN116033901A/en active Pending
- 2021-06-03 KR KR1020237000380A patent/KR20230024331A/en active Search and Examination
- 2021-06-03 IL IL298733A patent/IL298733A/en unknown
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