JP2016516068A5 - - Google Patents
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- JP2016516068A5 JP2016516068A5 JP2016503207A JP2016503207A JP2016516068A5 JP 2016516068 A5 JP2016516068 A5 JP 2016516068A5 JP 2016503207 A JP2016503207 A JP 2016503207A JP 2016503207 A JP2016503207 A JP 2016503207A JP 2016516068 A5 JP2016516068 A5 JP 2016516068A5
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- substituted
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- aryl
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- Prior art date
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- 125000003118 aryl group Chemical group 0.000 claims description 67
- 150000001875 compounds Chemical class 0.000 claims description 53
- 125000000217 alkyl group Chemical group 0.000 claims description 52
- 125000001072 heteroaryl group Chemical group 0.000 claims description 44
- 101100481408 Danio rerio tie2 gene Proteins 0.000 claims description 39
- 101100481410 Mus musculus Tek gene Proteins 0.000 claims description 39
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 34
- 150000003839 salts Chemical class 0.000 claims description 34
- 125000000623 heterocyclic group Chemical group 0.000 claims description 30
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 26
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 26
- 208000024891 symptom Diseases 0.000 claims description 21
- 125000003545 alkoxy group Chemical group 0.000 claims description 20
- 239000003795 chemical substances by application Substances 0.000 claims description 19
- 125000003342 alkenyl group Chemical group 0.000 claims description 18
- 125000000304 alkynyl group Chemical group 0.000 claims description 18
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 16
- JOYRKODLDBILNP-UHFFFAOYSA-N Ethyl urethane Chemical compound CCOC(N)=O JOYRKODLDBILNP-UHFFFAOYSA-N 0.000 claims description 14
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims description 10
- MBVFRSJFKMJRHA-UHFFFAOYSA-N 4-fluoro-1-benzofuran-7-carbaldehyde Chemical group FC1=CC=C(C=O)C2=C1C=CO2 MBVFRSJFKMJRHA-UHFFFAOYSA-N 0.000 claims description 8
- 125000002947 alkylene group Chemical group 0.000 claims description 8
- 125000003368 amide group Chemical group 0.000 claims description 8
- 125000003277 amino group Chemical group 0.000 claims description 8
- 125000005587 carbonate group Chemical group 0.000 claims description 8
- 125000002843 carboxylic acid group Chemical group 0.000 claims description 8
- 125000004185 ester group Chemical group 0.000 claims description 8
- 125000001033 ether group Chemical group 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 150000007970 thio esters Chemical group 0.000 claims description 8
- 230000003213 activating effect Effects 0.000 claims description 7
- 150000001408 amides Chemical class 0.000 claims description 7
- 125000000101 thioether group Chemical group 0.000 claims description 7
- KXDHJXZQYSOELW-UHFFFAOYSA-N Carbamic acid Chemical group NC(O)=O KXDHJXZQYSOELW-UHFFFAOYSA-N 0.000 claims description 6
- 125000004450 alkenylene group Chemical group 0.000 claims description 6
- 125000004419 alkynylene group Chemical group 0.000 claims description 6
- 239000002552 dosage form Substances 0.000 claims description 6
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 6
- 239000000126 substance Substances 0.000 claims description 6
- -1 thioacid group Chemical group 0.000 claims description 6
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical group CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims description 3
- 201000011190 diabetic macular edema Diseases 0.000 claims description 3
- 229940079593 drug Drugs 0.000 claims description 3
- 229940124530 sulfonamide Drugs 0.000 claims description 3
- 150000003456 sulfonamides Chemical class 0.000 claims description 3
- 150000003457 sulfones Chemical class 0.000 claims description 3
- ODLHGICHYURWBS-LKONHMLTSA-N trappsol cyclo Chemical group 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 claims description 3
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims description 2
- 206010012689 Diabetic retinopathy Diseases 0.000 claims description 2
- 239000002253 acid Substances 0.000 claims description 2
- 150000001412 amines Chemical class 0.000 claims description 2
- 150000002148 esters Chemical class 0.000 claims description 2
- 208000002780 macular degeneration Diseases 0.000 claims description 2
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical group 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 claims description 2
- 238000006467 substitution reaction Methods 0.000 claims description 2
- 150000003568 thioethers Chemical class 0.000 claims description 2
- 230000002792 vascular Effects 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 44
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 230000008878 coupling Effects 0.000 claims 1
- 238000010168 coupling process Methods 0.000 claims 1
- 238000005859 coupling reaction Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000004149 thio group Chemical group *S* 0.000 claims 1
- 238000000034 method Methods 0.000 description 60
- 230000036470 plasma concentration Effects 0.000 description 3
- 0 C*N(*)C(*)C(N(*)*(C)C)=O Chemical compound C*N(*)C(*)C(N(*)*(C)C)=O 0.000 description 2
- 230000003993 interaction Effects 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical group C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 125000003275 alpha amino acid group Chemical group 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 125000003827 glycol group Chemical group 0.000 description 1
- LNOPIUAQISRISI-UHFFFAOYSA-N n'-hydroxy-2-propan-2-ylsulfonylethanimidamide Chemical compound CC(C)S(=O)(=O)CC(N)=NO LNOPIUAQISRISI-UHFFFAOYSA-N 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- 229940097346 sulfobutylether-beta-cyclodextrin Drugs 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 230000004304 visual acuity Effects 0.000 description 1
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361792868P | 2013-03-15 | 2013-03-15 | |
| US201361792679P | 2013-03-15 | 2013-03-15 | |
| US61/792,679 | 2013-03-15 | ||
| US61/792,868 | 2013-03-15 | ||
| US201361882048P | 2013-09-25 | 2013-09-25 | |
| US201361882056P | 2013-09-25 | 2013-09-25 | |
| US61/882,048 | 2013-09-25 | ||
| US61/882,056 | 2013-09-25 | ||
| US201461934570P | 2014-01-31 | 2014-01-31 | |
| US61/934,570 | 2014-01-31 | ||
| PCT/US2014/029723 WO2014145068A1 (en) | 2013-03-15 | 2014-03-14 | Compositions, formulations and methods for treating ocular diseases |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019147238A Division JP6865254B2 (ja) | 2013-03-15 | 2019-08-09 | 眼疾患を処置するための組成物、製剤、および方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016516068A JP2016516068A (ja) | 2016-06-02 |
| JP2016516068A5 true JP2016516068A5 (enExample) | 2017-04-20 |
| JP6572201B2 JP6572201B2 (ja) | 2019-09-04 |
Family
ID=51529957
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016503207A Active JP6572201B2 (ja) | 2013-03-15 | 2014-03-14 | 眼疾患を処置するための組成物、製剤、および方法 |
| JP2019147238A Active JP6865254B2 (ja) | 2013-03-15 | 2019-08-09 | 眼疾患を処置するための組成物、製剤、および方法 |
| JP2021064106A Active JP7249374B2 (ja) | 2013-03-15 | 2021-04-05 | 眼疾患を処置するための組成物、製剤、および方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019147238A Active JP6865254B2 (ja) | 2013-03-15 | 2019-08-09 | 眼疾患を処置するための組成物、製剤、および方法 |
| JP2021064106A Active JP7249374B2 (ja) | 2013-03-15 | 2021-04-05 | 眼疾患を処置するための組成物、製剤、および方法 |
Country Status (17)
| Country | Link |
|---|---|
| US (10) | US9440963B2 (enExample) |
| EP (3) | EP2967066B1 (enExample) |
| JP (3) | JP6572201B2 (enExample) |
| KR (1) | KR20150129019A (enExample) |
| CN (2) | CN105307498B (enExample) |
| AU (2) | AU2014233363B2 (enExample) |
| BR (1) | BR112015023753A2 (enExample) |
| CA (1) | CA2903871A1 (enExample) |
| ES (2) | ES2766326T3 (enExample) |
| GB (3) | GB2549865B (enExample) |
| HK (2) | HK1206558A1 (enExample) |
| IL (2) | IL240786B (enExample) |
| MX (1) | MX371382B (enExample) |
| MY (1) | MY171945A (enExample) |
| PH (2) | PH12015502153B1 (enExample) |
| SG (1) | SG11201507131WA (enExample) |
| WO (1) | WO2014145068A1 (enExample) |
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| MY150400A (en) | 2006-04-07 | 2014-01-15 | Aerpio Therapeutics Inc | Antibodies that bind human protein tyrosine phosphatase beta (hptpbeta) and uses thereof |
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| MY160399A (en) | 2009-07-06 | 2017-03-15 | Aerpio Therapeutics Inc | Compounds, compositions, and methods for preventing metastasis of cancer cells |
| US12186426B2 (en) | 2009-10-30 | 2025-01-07 | Ix Biopharma Ltd. | Solid dosage form |
| ES2712989T3 (es) | 2009-10-30 | 2019-05-17 | Ix Biopharma Ltd | Forma de dosificación sólida de disolución rápida |
| ES2541613T3 (es) | 2009-11-06 | 2015-07-22 | Aerpio Therapeutics Inc. | Composiciones y métodos para tratar colitis |
| US20180092883A1 (en) * | 2010-10-07 | 2018-04-05 | Aerpio Therapeutics, Inc. | Phosphatase inhibitors for treating ocular diseases |
| JP5965409B2 (ja) | 2010-12-08 | 2016-08-03 | コンバテック・テクノロジーズ・インコーポレイテッドＣｏｎｖａｔｅｃ Ｔｅｃｈｎｏｌｏｇｉｅｓ Ｉｎｃ | 創傷滲出液を評価するための統合システム |
| EP2648794B1 (en) | 2010-12-08 | 2019-08-28 | ConvaTec Technologies Inc. | Wound exudate system accessory |
| CN104039351A (zh) | 2011-10-13 | 2014-09-10 | 阿尔皮奥治疗学股份有限公司 | 用于治疗血管渗漏综合征和癌症的方法 |
| EP3501536B1 (en) | 2011-10-13 | 2025-12-24 | EyePoint Pharmaceuticals, Inc. | Treatment of ocular disease |
| EP2906201A4 (en) * | 2012-10-11 | 2016-10-19 | Ix Biopharma Ltd | SOLID DOSAGE FORM |
| WO2014145068A1 (en) * | 2013-03-15 | 2014-09-18 | Aerpio Therapeutics Inc. | Compositions, formulations and methods for treating ocular diseases |
| US20150050277A1 (en) | 2013-03-15 | 2015-02-19 | Aerpio Therapeutics Inc. | Compositions and methods for treating ocular diseases |
| US9388135B2 (en) | 2014-02-19 | 2016-07-12 | Aerpio Therapeutics, Inc. | Process for preparing N-benzyl-3-hydroxy-4-substituted-pyridin-2-(1H)-ones |
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| CN109996440A (zh) * | 2016-10-21 | 2019-07-09 | 曼宁研究有限公司 | Ve-ptp敲除 |
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| WO2020214851A1 (en) * | 2019-04-18 | 2020-10-22 | Aerpio Pharmaceuticals, Inc. | Methods of treating hypertension with activators of tie-2 |
| JP7564824B2 (ja) * | 2019-04-29 | 2024-10-09 | アイポイント ファーマシューティカルズ， インコーポレイテッド | シュレム管を標的とするＴｉｅ－２活性化物質 |
| GB2589400A (en) * | 2019-06-24 | 2021-06-02 | Aerpio Pharmaceuticals Inc | Formulations of tie-2 activators and methods of use thereof |
| WO2021086904A1 (en) | 2019-10-29 | 2021-05-06 | Aerpio Pharmaceuticals, Inc. | Small molecule activators of tie-2 |
| JP2023530457A (ja) * | 2020-06-16 | 2023-07-18 | リプカ，エイミー | 小分子ｖｅ－ｐｔｐ阻害剤 |
| CN116940355A (zh) * | 2020-12-18 | 2023-10-24 | 视点制药公司 | 用于制造tie-2的小分子激活剂的方法 |
| WO2025128706A1 (en) * | 2023-12-11 | 2025-06-19 | Massachusetts Eye And Ear Infirmary | Methods of using tie-2 activators |
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