JP2017511305A5 - - Google Patents
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- JP2017511305A5 JP2017511305A5 JP2016556997A JP2016556997A JP2017511305A5 JP 2017511305 A5 JP2017511305 A5 JP 2017511305A5 JP 2016556997 A JP2016556997 A JP 2016556997A JP 2016556997 A JP2016556997 A JP 2016556997A JP 2017511305 A5 JP2017511305 A5 JP 2017511305A5
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- JP
- Japan
- Prior art keywords
- bond
- substituted
- unsubstituted
- aryl
- alkyl
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims description 85
- 125000003118 aryl group Chemical group 0.000 claims description 82
- 150000001875 compounds Chemical class 0.000 claims description 77
- 125000001072 heteroaryl group Chemical group 0.000 claims description 72
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 54
- 125000000623 heterocyclic group Chemical group 0.000 claims description 51
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 48
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 48
- 101100481408 Danio rerio tie2 gene Proteins 0.000 claims description 43
- 101100481410 Mus musculus Tek gene Proteins 0.000 claims description 43
- 125000003342 alkenyl group Chemical group 0.000 claims description 42
- 125000000304 alkynyl group Chemical group 0.000 claims description 42
- 239000012190 activator Substances 0.000 claims description 35
- 125000002947 alkylene group Chemical group 0.000 claims description 35
- 239000008194 pharmaceutical composition Substances 0.000 claims description 34
- 125000004450 alkenylene group Chemical group 0.000 claims description 32
- 125000004419 alkynylene group Chemical group 0.000 claims description 32
- 150000003839 salts Chemical class 0.000 claims description 30
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Chemical group CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 22
- 239000000126 substance Substances 0.000 claims description 19
- 229910052757 nitrogen Inorganic materials 0.000 claims description 17
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 17
- 125000003545 alkoxy group Chemical group 0.000 claims description 15
- 238000000034 method Methods 0.000 claims description 15
- 229940124530 sulfonamide Drugs 0.000 claims description 13
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 7
- 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 6
- KXDHJXZQYSOELW-UHFFFAOYSA-N Carbamic acid Chemical group NC(O)=O KXDHJXZQYSOELW-UHFFFAOYSA-N 0.000 claims description 6
- 125000003368 amide group Chemical group 0.000 claims description 6
- 125000003277 amino group Chemical group 0.000 claims description 6
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 claims description 6
- 125000005587 carbonate group Chemical group 0.000 claims description 6
- 125000002843 carboxylic acid group Chemical group 0.000 claims description 6
- 125000004185 ester group Chemical group 0.000 claims description 6
- 125000001033 ether group Chemical group 0.000 claims description 6
- 150000007970 thio esters Chemical group 0.000 claims description 6
- -1 thioacid group Chemical group 0.000 claims description 6
- 125000000101 thioether group Chemical group 0.000 claims description 6
- 239000003153 chemical reaction reagent Substances 0.000 claims description 5
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical group C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims description 3
- 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 2
- BEHLMOQXOSLGHN-UHFFFAOYSA-N benzenamine sulfate Chemical group OS(=O)(=O)NC1=CC=CC=C1 BEHLMOQXOSLGHN-UHFFFAOYSA-N 0.000 claims 7
- PXFORDPOPVGNJL-UHFFFAOYSA-N diphenylsulfamic acid Chemical class C=1C=CC=CC=1N(S(=O)(=O)O)C1=CC=CC=C1 PXFORDPOPVGNJL-UHFFFAOYSA-N 0.000 claims 2
- 150000003457 sulfones Chemical class 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 8
- 0 COC(N[C@@](C(N[C@@](Cc(cc1)ccc1NS(*)(=*)=O)c1c[s]c(-c2ccc[s]2)n1)=O)N=Cc1ccccc1)=* Chemical compound COC(N[C@@](C(N[C@@](Cc(cc1)ccc1NS(*)(=*)=O)c1c[s]c(-c2ccc[s]2)n1)=O)N=Cc1ccccc1)=* 0.000 description 4
- 239000007858 starting material Substances 0.000 description 4
- 239000002552 dosage form Substances 0.000 description 1
- 125000000524 functional group Chemical group 0.000 description 1
- 239000011541 reaction mixture Substances 0.000 description 1
- 125000003107 substituted aryl group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461953680P | 2014-03-14 | 2014-03-14 | |
| US61/953,680 | 2014-03-14 | ||
| PCT/US2015/020425 WO2015138882A1 (en) | 2014-03-14 | 2015-03-13 | Hptp-beta inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018246712A Division JP6661744B2 (ja) | 2014-03-14 | 2018-12-28 | ＨＰＴＰ−β阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017511305A JP2017511305A (ja) | 2017-04-20 |
| JP2017511305A5 true JP2017511305A5 (enExample) | 2018-04-12 |
| JP6483148B2 JP6483148B2 (ja) | 2019-03-13 |
Family
ID=54068203
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016556997A Active JP6483148B2 (ja) | 2014-03-14 | 2015-03-13 | ＨＰＴＰ−β阻害剤 |
| JP2018246712A Active JP6661744B2 (ja) | 2014-03-14 | 2018-12-28 | ＨＰＴＰ−β阻害剤 |
| JP2019077696A Withdrawn JP2019108407A (ja) | 2014-03-14 | 2019-04-16 | ＨＰＴＰ−β阻害剤 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018246712A Active JP6661744B2 (ja) | 2014-03-14 | 2018-12-28 | ＨＰＴＰ−β阻害剤 |
| JP2019077696A Withdrawn JP2019108407A (ja) | 2014-03-14 | 2019-04-16 | ＨＰＴＰ−β阻害剤 |
Country Status (5)
| Country | Link |
|---|---|
| US (3) | US9994560B2 (enExample) |
| EP (1) | EP3116503A4 (enExample) |
| JP (3) | JP6483148B2 (enExample) |
| CN (1) | CN106456614A (enExample) |
| WO (1) | WO2015138882A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11724982B2 (en) | 2014-10-10 | 2023-08-15 | The Research Foundation For The State University Of New York | Trifluoromethoxylation of arenes via intramolecular trifluoromethoxy group migration |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2371865B1 (en) | 2006-04-07 | 2017-07-12 | Aerpio Therapeutics, Inc. | Antibodies that bind human protein tyrosine phosphatase beta (HPTP-ß) and uses thereof |
| US7622593B2 (en) | 2006-06-27 | 2009-11-24 | The Procter & Gamble Company | Human protein tyrosine phosphatase inhibitors and methods of use |
| RU2014146121A (ru) * | 2009-01-12 | 2015-06-10 | Аэрпио Терапьютикс Инк. | Способы лечения синдрома сосудистой утечки |
| EP3556367A1 (en) | 2009-07-06 | 2019-10-23 | Aerpio Therapeutics, Inc. | Benzosulfonamide derivatives, compositions thereof, and their use in the treatment of cancer or metastasis |
| CA2850830A1 (en) | 2011-10-13 | 2013-04-18 | Aerpio Therapeutics, Inc. | Methods for treating vascular leak syndrome and cancer |
| US20150050277A1 (en) | 2013-03-15 | 2015-02-19 | Aerpio Therapeutics Inc. | Compositions and methods for treating ocular diseases |
| BR112015023753A2 (pt) | 2013-03-15 | 2017-07-18 | Aerpio Therapeutics Inc | composições, formulações e métodos para o tratamento de doenças oculares |
| CN106456614A (zh) | 2014-03-14 | 2017-02-22 | 爱尔皮奥治疗有限公司 | HPTP‑β抑制剂 |
| WO2016022813A1 (en) | 2014-08-07 | 2016-02-11 | Aerpio Therapeutics, Inc. | Combination of immunotherapies with activators of tie-2 |
| ES2981607T3 (es) * | 2015-09-23 | 2024-10-09 | Eyepoint Pharmaceuticals Inc | Activadores de Tie-2 para uso en el tratamiento de la presión intraocular |
| JP7107914B2 (ja) | 2016-07-20 | 2022-07-27 | 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 | ＶＥ－ＰＴＰ（ＨＰＴＰ－β）を標的化するヒト化モノクローナル抗体 |
| JP2021515035A (ja) * | 2018-02-26 | 2021-06-17 | エアーピオ ファーマシューティカルズ， インコーポレイテッド | ＨＰＴＰβ阻害剤を使用して糖尿病性腎症を処置する方法 |
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| PL3873605T3 (pl) | 2018-10-30 | 2025-03-03 | Gilead Sciences, Inc. | Związki hamujące integrynę alfa4beta7 |
| WO2020092383A1 (en) | 2018-10-30 | 2020-05-07 | Gilead Sciences, Inc. | Compounds for inhibition of alpha 4 beta 7 integrin |
| EP3873900B1 (en) | 2018-10-30 | 2025-01-08 | Gilead Sciences, Inc. | Imidazo[1,2-a]pyridine derivatives as alpha4beta7 integrin inhibitors for the treatment of inflammatory diseases |
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| AU2020264969B2 (en) | 2019-04-29 | 2025-06-05 | EyePoint, Inc. | Tie-2 activators targeting the schlemm's canal |
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| EP4013499A1 (en) | 2019-08-14 | 2022-06-22 | Gilead Sciences, Inc. | Compounds for inhibition of alpha 4 beta 7 integrin |
| EP4051267A4 (en) | 2019-10-29 | 2023-12-06 | EyePoint Pharmaceuticals, Inc. | TIE-2 SMALL MOLECULE ACTIVATORS |
| CN113060789A (zh) * | 2019-12-31 | 2021-07-02 | 大连乾丰生物科技有限公司 | 一种海蜇池塘水底质改良剂 |
| US20240190857A1 (en) * | 2020-12-18 | 2024-06-13 | EyePoint Pharmaceuticals, Inc. | Methods for manufacture of small molecule activators of tie-2 |
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| PT3062811T (pt) | 2013-11-01 | 2019-06-11 | Regeneron Pharma | Intervenções à base de angiopoietina para o tratamento da malária cerebral |
| CN106456614A (zh) | 2014-03-14 | 2017-02-22 | 爱尔皮奥治疗有限公司 | HPTP‑β抑制剂 |
| JP2015199733A (ja) | 2014-04-04 | 2015-11-12 | 国立大学法人東北大学 | 眼圧降下剤 |
| US9719135B2 (en) | 2014-07-03 | 2017-08-01 | Mannin Research Inc. | Conditional angiopoietin-1/angiopoietin-2 double knock-out mice with defective ocular drainage system |
| WO2016022813A1 (en) | 2014-08-07 | 2016-02-11 | Aerpio Therapeutics, Inc. | Combination of immunotherapies with activators of tie-2 |
| WO2016049183A1 (en) | 2014-09-24 | 2016-03-31 | Aerpio Therapeutics, Inc. | Ve-ptp extracellular domain antibodies delivered by a gene therapy vector |
| TWI705827B (zh) | 2014-11-07 | 2020-10-01 | 瑞士商諾華公司 | 治療眼部疾病之方法 |
| US20160144025A1 (en) | 2014-11-25 | 2016-05-26 | Regeneron Pharmaceuticals, Inc. | Methods and formulations for treating vascular eye diseases |
-
2015
- 2015-03-13 CN CN201580026210.0A patent/CN106456614A/zh active Pending
- 2015-03-13 EP EP15760687.2A patent/EP3116503A4/en not_active Withdrawn
- 2015-03-13 WO PCT/US2015/020425 patent/WO2015138882A1/en not_active Ceased
- 2015-03-13 US US14/657,276 patent/US9994560B2/en active Active
- 2015-03-13 JP JP2016556997A patent/JP6483148B2/ja active Active
-
2018
- 2018-05-07 US US15/972,863 patent/US10858354B2/en active Active
- 2018-12-28 JP JP2018246712A patent/JP6661744B2/ja active Active
-
2019
- 2019-04-16 JP JP2019077696A patent/JP2019108407A/ja not_active Withdrawn
-
2020
- 2020-10-02 US US17/062,098 patent/US20210130341A1/en not_active Abandoned
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11724982B2 (en) | 2014-10-10 | 2023-08-15 | The Research Foundation For The State University Of New York | Trifluoromethoxylation of arenes via intramolecular trifluoromethoxy group migration |
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