JP2020121985A5 - - Google Patents
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- Publication number
- JP2020121985A5 JP2020121985A5 JP2020068158A JP2020068158A JP2020121985A5 JP 2020121985 A5 JP2020121985 A5 JP 2020121985A5 JP 2020068158 A JP2020068158 A JP 2020068158A JP 2020068158 A JP2020068158 A JP 2020068158A JP 2020121985 A5 JP2020121985 A5 JP 2020121985A5
- Authority
- JP
- Japan
- Prior art keywords
- medicament
- weeks
- manufactured
- period
- use according
- 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.)
- Pending
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- 239000003814 drug Substances 0.000 claims description 44
- 150000001875 compounds Chemical class 0.000 claims description 22
- 229940079593 drug Drugs 0.000 claims description 19
- 150000003839 salts Chemical class 0.000 claims description 18
- 230000001225 therapeutic effect Effects 0.000 claims description 17
- 229930105110 Cyclosporin A Natural products 0.000 claims description 16
- PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical group CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 claims description 16
- 108010036949 Cyclosporine Proteins 0.000 claims description 16
- 229960001265 ciclosporin Drugs 0.000 claims description 15
- 230000003287 optical effect Effects 0.000 claims description 15
- 239000012453 solvate Substances 0.000 claims description 15
- 150000002148 esters Chemical class 0.000 claims description 14
- 239000008194 pharmaceutical composition Substances 0.000 claims description 14
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 11
- 150000004677 hydrates Chemical class 0.000 claims description 9
- 230000004968 inflammatory condition Effects 0.000 claims description 9
- 208000015181 infectious disease Diseases 0.000 claims description 8
- 230000002458 infectious effect Effects 0.000 claims description 8
- 238000004519 manufacturing process Methods 0.000 claims description 8
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims description 6
- 206010010741 Conjunctivitis Diseases 0.000 claims description 4
- 206010039705 Scleritis Diseases 0.000 claims description 4
- 206010046851 Uveitis Diseases 0.000 claims description 4
- 239000000126 substance Substances 0.000 claims 18
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000005557 antagonist Substances 0.000 description 6
- 102100032818 Integrin alpha-4 Human genes 0.000 description 5
- 108010041012 Integrin alpha4 Proteins 0.000 description 5
- 229960004833 dexamethasone phosphate Drugs 0.000 description 4
- VQODGRNSFPNSQE-CXSFZGCWSA-N dexamethasone phosphate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)COP(O)(O)=O)(O)[C@@]1(C)C[C@@H]2O VQODGRNSFPNSQE-CXSFZGCWSA-N 0.000 description 4
- 210000000265 leukocyte Anatomy 0.000 description 4
- 229940124597 therapeutic agent Drugs 0.000 description 4
- 230000000694 effects Effects 0.000 description 3
- -1 limexolone Chemical compound 0.000 description 3
- 210000001165 lymph node Anatomy 0.000 description 3
- 230000007246 mechanism Effects 0.000 description 3
- 150000003431 steroids Chemical class 0.000 description 3
- 230000009885 systemic effect Effects 0.000 description 3
- 230000000699 topical effect Effects 0.000 description 3
- 102100022339 Integrin alpha-L Human genes 0.000 description 2
- 108010064548 Lymphocyte Function-Associated Antigen-1 Proteins 0.000 description 2
- LRJOMUJRLNCICJ-JZYPGELDSA-N Prednisolone acetate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)COC(=O)C)(O)[C@@]1(C)C[C@@H]2O LRJOMUJRLNCICJ-JZYPGELDSA-N 0.000 description 2
- 210000000612 antigen-presenting cell Anatomy 0.000 description 2
- 229960003655 bromfenac Drugs 0.000 description 2
- ZBPLOVFIXSTCRZ-UHFFFAOYSA-N bromfenac Chemical compound NC1=C(CC(O)=O)C=CC=C1C(=O)C1=CC=C(Br)C=C1 ZBPLOVFIXSTCRZ-UHFFFAOYSA-N 0.000 description 2
- 210000000795 conjunctiva Anatomy 0.000 description 2
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 description 2
- 229960001259 diclofenac Drugs 0.000 description 2
- DCOPUUMXTXDBNB-UHFFFAOYSA-N diclofenac Chemical compound OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl DCOPUUMXTXDBNB-UHFFFAOYSA-N 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 239000003889 eye drop Substances 0.000 description 2
- 229960001048 fluorometholone Drugs 0.000 description 2
- FAOZLTXFLGPHNG-KNAQIMQKSA-N fluorometholone Chemical compound C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@]2(F)[C@@H](O)C[C@]2(C)[C@@](O)(C(C)=O)CC[C@H]21 FAOZLTXFLGPHNG-KNAQIMQKSA-N 0.000 description 2
- 229960001629 fluorometholone acetate Drugs 0.000 description 2
- YRFXGQHBPBMFHW-SBTZIJSASA-N fluorometholone acetate Chemical compound C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@]2(F)[C@@H](O)C[C@]2(C)[C@@](OC(C)=O)(C(C)=O)CC[C@H]21 YRFXGQHBPBMFHW-SBTZIJSASA-N 0.000 description 2
- 229960002390 flurbiprofen Drugs 0.000 description 2
- SYTBZMRGLBWNTM-UHFFFAOYSA-N flurbiprofen Chemical compound FC1=CC(C(C(O)=O)C)=CC=C1C1=CC=CC=C1 SYTBZMRGLBWNTM-UHFFFAOYSA-N 0.000 description 2
- 230000004941 influx Effects 0.000 description 2
- 230000005012 migration Effects 0.000 description 2
- 238000013508 migration Methods 0.000 description 2
- 229960001002 nepafenac Drugs 0.000 description 2
- QEFAQIPZVLVERP-UHFFFAOYSA-N nepafenac Chemical compound NC(=O)CC1=CC=CC(C(=O)C=2C=CC=CC=2)=C1N QEFAQIPZVLVERP-UHFFFAOYSA-N 0.000 description 2
- 239000002997 ophthalmic solution Substances 0.000 description 2
- 229940054534 ophthalmic solution Drugs 0.000 description 2
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical group [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 2
- 229960002800 prednisolone acetate Drugs 0.000 description 2
- 229960004786 prednisolone phosphate Drugs 0.000 description 2
- JDOZJEUDSLGTLU-VWUMJDOOSA-N prednisolone phosphate Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)COP(O)(O)=O)[C@@H]4[C@@H]3CCC2=C1 JDOZJEUDSLGTLU-VWUMJDOOSA-N 0.000 description 2
- 229960002117 triamcinolone acetonide Drugs 0.000 description 2
- YNDXUCZADRHECN-JNQJZLCISA-N triamcinolone acetonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O YNDXUCZADRHECN-JNQJZLCISA-N 0.000 description 2
- 206010061218 Inflammation Diseases 0.000 description 1
- 210000001744 T-lymphocyte Anatomy 0.000 description 1
- 108010000134 Vascular Cell Adhesion Molecule-1 Proteins 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 230000008485 antagonism Effects 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 210000004087 cornea Anatomy 0.000 description 1
- 230000004890 epithelial barrier function Effects 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 102000006495 integrins Human genes 0.000 description 1
- 108010044426 integrins Proteins 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 239000003595 mist Substances 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 238000010172 mouse model Methods 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 238000010186 staining Methods 0.000 description 1
- 230000003637 steroidlike Effects 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562189813P | 2015-07-08 | 2015-07-08 | |
| US62/189,813 | 2015-07-08 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018520045A Division JP6752276B2 (ja) | 2015-07-08 | 2016-07-07 | 眼炎症状態を処置する際に使用するための、インテグリンα４アンタゴニストを含む薬学的組成物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020121985A JP2020121985A (ja) | 2020-08-13 |
| JP2020121985A5 true JP2020121985A5 (https=) | 2020-11-05 |
Family
ID=56373100
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018520045A Expired - Fee Related JP6752276B2 (ja) | 2015-07-08 | 2016-07-07 | 眼炎症状態を処置する際に使用するための、インテグリンα４アンタゴニストを含む薬学的組成物 |
| JP2020068158A Pending JP2020121985A (ja) | 2015-07-08 | 2020-04-06 | 眼炎症状態を処置する際に使用するための、インテグリンα４アンタゴニストを含む薬学的組成物 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018520045A Expired - Fee Related JP6752276B2 (ja) | 2015-07-08 | 2016-07-07 | 眼炎症状態を処置する際に使用するための、インテグリンα４アンタゴニストを含む薬学的組成物 |
Country Status (21)
| Country | Link |
|---|---|
| US (3) | US10413535B2 (https=) |
| EP (1) | EP3319639B1 (https=) |
| JP (2) | JP6752276B2 (https=) |
| KR (2) | KR20220062688A (https=) |
| CN (1) | CN107921136A (https=) |
| AU (1) | AU2016290197B2 (https=) |
| BR (1) | BR112018000112A2 (https=) |
| CA (1) | CA2989522C (https=) |
| CL (1) | CL2018000057A1 (https=) |
| ES (1) | ES2835274T3 (https=) |
| HK (1) | HK1247120A1 (https=) |
| IL (2) | IL256770B (https=) |
| MA (2) | MA42016A1 (https=) |
| MX (1) | MX385229B (https=) |
| MY (1) | MY187552A (https=) |
| PL (1) | PL3319639T3 (https=) |
| RU (1) | RU2018103940A (https=) |
| TN (1) | TN2017000538A1 (https=) |
| UA (1) | UA123728C2 (https=) |
| WO (1) | WO2017006272A1 (https=) |
| ZA (1) | ZA201708601B (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018165218A1 (en) * | 2017-03-09 | 2018-09-13 | Allysta Pharmaceuticals, Inc | Peptides for dry eye disease |
| EP3624773A4 (en) * | 2017-05-19 | 2021-04-07 | Ocugen, Inc. | OPHTHALMIC COMPOSITIONS AND METHOD OF USE |
| KR102659859B1 (ko) | 2018-10-30 | 2024-04-25 | 길리애드 사이언시즈, 인코포레이티드 | 알파4β7 인테그린의 억제를 위한 화합물 |
| AU2019373242B2 (en) | 2018-10-30 | 2023-07-13 | Gilead Sciences, Inc. | Compounds for inhibition of alpha 4 beta 7 integrin |
| EP4541422A3 (en) | 2018-10-30 | 2025-06-25 | Gilead Sciences, Inc. | Quinoline derivatives as alpha4beta7 integrin inhibitors |
| CN112969700B (zh) | 2018-10-30 | 2024-08-20 | 吉利德科学公司 | 作为α4β7整合素抑制剂的咪唑并吡啶衍生物 |
| MX2022001062A (es) * | 2019-07-26 | 2022-02-14 | Allegro Pharmaceuticals Llc | Peptidos para el tratamiento de degeneracion macular no exudativa y otros trastornos del ojo. |
| KR102908219B1 (ko) | 2019-08-14 | 2026-01-08 | 길리애드 사이언시즈, 인코포레이티드 | 알파 4 베타 7 인테그린의 저해용 화합물 |
| KR20230110514A (ko) * | 2020-10-21 | 2023-07-24 | 아주라 오프탈믹스 엘티디 | 안구 장애의 치료를 위한 화합물 및 방법 |
| KR102391198B1 (ko) * | 2021-08-27 | 2022-04-27 | 한림제약(주) | 리피테그라스트 또는 이의 약제학적으로 허용가능한 염을 포함하는 수용액 형태의 점안액 조성물 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9828074D0 (en) * | 1998-12-18 | 1999-02-17 | Glaxo Group Ltd | Therapeutically useful compounds |
| GB0014892D0 (en) | 2000-06-16 | 2000-08-09 | Glaxo Group Ltd | Novel pharmaceutical formulation |
| DK2444079T3 (en) | 2005-05-17 | 2017-01-30 | Sarcode Bioscience Inc | Compositions and Methods for the Treatment of Eye Diseases |
| WO2007056457A2 (en) * | 2005-11-09 | 2007-05-18 | Combinatorx, Incorporated | Methods, compositions, and kits for the treatment of medical conditions |
| US20130217657A1 (en) | 2011-12-21 | 2013-08-22 | Insite Vision Incorporated | Combination anti-inflammatory ophthalmic compositions |
-
2016
- 2016-07-07 ES ES16736636T patent/ES2835274T3/es active Active
- 2016-07-07 CA CA2989522A patent/CA2989522C/en active Active
- 2016-07-07 PL PL16736636T patent/PL3319639T3/pl unknown
- 2016-07-07 JP JP2018520045A patent/JP6752276B2/ja not_active Expired - Fee Related
- 2016-07-07 UA UAA201800954A patent/UA123728C2/uk unknown
- 2016-07-07 BR BR112018000112-0A patent/BR112018000112A2/pt not_active Application Discontinuation
- 2016-07-07 CN CN201680040066.0A patent/CN107921136A/zh active Pending
- 2016-07-07 KR KR1020227015200A patent/KR20220062688A/ko not_active Ceased
- 2016-07-07 MY MYPI2017001928A patent/MY187552A/en unknown
- 2016-07-07 TN TNP/2017/000538A patent/TN2017000538A1/en unknown
- 2016-07-07 RU RU2018103940A patent/RU2018103940A/ru unknown
- 2016-07-07 WO PCT/IB2016/054073 patent/WO2017006272A1/en not_active Ceased
- 2016-07-07 EP EP16736636.8A patent/EP3319639B1/en active Active
- 2016-07-07 KR KR1020187003454A patent/KR102440162B1/ko active Active
- 2016-07-07 AU AU2016290197A patent/AU2016290197B2/en not_active Ceased
- 2016-07-07 MA MA42016A patent/MA42016A1/fr unknown
- 2016-07-07 HK HK18106821.2A patent/HK1247120A1/zh unknown
- 2016-07-07 MX MX2017017163A patent/MX385229B/es unknown
- 2016-07-07 US US15/742,867 patent/US10413535B2/en not_active Expired - Fee Related
-
2017
- 2017-12-18 ZA ZA2017/08601A patent/ZA201708601B/en unknown
-
2018
- 2018-01-07 IL IL256770A patent/IL256770B/en active IP Right Grant
- 2018-01-08 CL CL2018000057A patent/CL2018000057A1/es unknown
- 2018-02-08 MA MA44935A patent/MA44935A1/fr unknown
-
2019
- 2019-09-12 US US16/569,465 patent/US10751334B2/en not_active Expired - Fee Related
-
2020
- 2020-04-06 JP JP2020068158A patent/JP2020121985A/ja active Pending
- 2020-07-13 US US16/927,825 patent/US20200405703A1/en not_active Abandoned
-
2021
- 2021-02-11 IL IL280827A patent/IL280827A/en unknown
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