JPWO2019190885A5 - - Google Patents
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- JPWO2019190885A5 JPWO2019190885A5 JP2020551973A JP2020551973A JPWO2019190885A5 JP WO2019190885 A5 JPWO2019190885 A5 JP WO2019190885A5 JP 2020551973 A JP2020551973 A JP 2020551973A JP 2020551973 A JP2020551973 A JP 2020551973A JP WO2019190885 A5 JPWO2019190885 A5 JP WO2019190885A5
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- JP
- Japan
- Prior art keywords
- substituted
- optionally substituted
- nhc
- alkyl
- group
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 57
- 150000001875 compounds Chemical class 0.000 claims 56
- 125000004452 carbocyclyl group Chemical group 0.000 claims 45
- 125000003118 aryl group Chemical group 0.000 claims 38
- 229910052799 carbon Inorganic materials 0.000 claims 35
- 125000000623 heterocyclic group Chemical group 0.000 claims 35
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 29
- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 125000001475 halogen functional group Chemical group 0.000 claims 19
- 125000001188 haloalkyl group Chemical group 0.000 claims 13
- 229910052717 sulfur Inorganic materials 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 11
- 229910052760 oxygen Inorganic materials 0.000 claims 10
- 206010016654 Fibrosis Diseases 0.000 claims 9
- 239000002202 Polyethylene glycol Substances 0.000 claims 8
- 230000004761 fibrosis Effects 0.000 claims 8
- 229920001223 polyethylene glycol Polymers 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 5
- 125000003275 alpha amino acid group Chemical group 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 229910005965 SO 2 Inorganic materials 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 208000019425 cirrhosis of liver Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 230000003176 fibrotic effect Effects 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- 206010059245 Angiopathy Diseases 0.000 claims 1
- 101150065749 Churc1 gene Proteins 0.000 claims 1
- 208000014919 IgG4-related retroperitoneal fibrosis Diseases 0.000 claims 1
- 208000029523 Interstitial Lung disease Diseases 0.000 claims 1
- 206010028594 Myocardial fibrosis Diseases 0.000 claims 1
- 208000003510 Nephrogenic Fibrosing Dermopathy Diseases 0.000 claims 1
- 206010067467 Nephrogenic systemic fibrosis Diseases 0.000 claims 1
- 206010035664 Pneumonia Diseases 0.000 claims 1
- 206010036805 Progressive massive fibrosis Diseases 0.000 claims 1
- 102100038239 Protein Churchill Human genes 0.000 claims 1
- 206010063837 Reperfusion injury Diseases 0.000 claims 1
- 206010038979 Retroperitoneal fibrosis Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 230000000735 allogeneic effect Effects 0.000 claims 1
- 230000009787 cardiac fibrosis Effects 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 230000007850 degeneration Effects 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 238000002955 isolation Methods 0.000 claims 1
- 230000000938 luteal effect Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 201000002793 renal fibrosis Diseases 0.000 claims 1
- 238000002271 resection Methods 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 208000037921 secondary disease Diseases 0.000 claims 1
- 210000000952 spleen Anatomy 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862649451P | 2018-03-28 | 2018-03-28 | |
| US62/649,451 | 2018-03-28 | ||
| PCT/US2019/023457 WO2019190885A1 (en) | 2018-03-28 | 2019-03-21 | Calpain modulators and therapeutic uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021519312A JP2021519312A (ja) | 2021-08-10 |
| JP2021519312A5 JP2021519312A5 (https=) | 2022-03-03 |
| JPWO2019190885A5 true JPWO2019190885A5 (https=) | 2022-03-03 |
Family
ID=68060735
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020551973A Pending JP2021519312A (ja) | 2018-03-28 | 2019-03-21 | カルパインモジュレーター及びその治療的使用 |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US20210009564A1 (https=) |
| EP (1) | EP3774737A4 (https=) |
| JP (1) | JP2021519312A (https=) |
| KR (1) | KR20200139702A (https=) |
| CN (1) | CN112204014A (https=) |
| AR (1) | AR115303A1 (https=) |
| AU (1) | AU2019242387A1 (https=) |
| BR (1) | BR112020019560A2 (https=) |
| CA (1) | CA3095164A1 (https=) |
| CL (1) | CL2020002496A1 (https=) |
| CO (1) | CO2020012359A2 (https=) |
| EC (1) | ECSP20068210A (https=) |
| IL (1) | IL277548A (https=) |
| MX (1) | MX2020010033A (https=) |
| PE (1) | PE20212111A1 (https=) |
| PH (1) | PH12020551555A1 (https=) |
| RU (1) | RU2020130022A (https=) |
| SG (1) | SG11202008750XA (https=) |
| TW (1) | TW202003472A (https=) |
| WO (1) | WO2019190885A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3481835A4 (en) | 2016-07-05 | 2020-02-26 | Blade Therapeutics, Inc. | CALPAIN MODULATORS AND THERAPEUTIC USE THEREOF |
| BR112019006110A2 (pt) | 2016-09-28 | 2019-09-10 | Blade Therapeutics Inc | moduladores de calpaína e usos terapêuticos dos mesmos |
| KR20200139721A (ko) * | 2018-03-28 | 2020-12-14 | 블레이드 테라퓨틱스, 인크. | 섬유성 질환을 치료하는 방법 |
| WO2020006294A1 (en) * | 2018-06-28 | 2020-01-02 | Blade Therapeutics, Inc. | Methods of treating liver fibrosis using calpain inhibitors |
| PH12022553378A1 (en) | 2020-06-10 | 2024-03-25 | Univ Leuven Kath | Anti-viral compounds for treating coronavirus, picornavirus, and norovirus infections |
| JP2024525589A (ja) | 2021-07-09 | 2024-07-12 | アリゴス セラピューティクス インコーポレイテッド | 抗ウイルス化合物 |
| WO2023043816A1 (en) | 2021-09-17 | 2023-03-23 | Aligos Therapeutics, Inc. | Anti-viral compounds for treating coronavirus, picornavirus, and norovirus infections |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE9102462D0 (sv) * | 1991-08-28 | 1991-08-28 | Astra Ab | New isosteric peptides |
| JPH09500087A (ja) * | 1992-06-24 | 1997-01-07 | コーテックス ファーマシューティカルズ インコーポレイテッド | カルパイン活性の増大に関連した健康障害の抑制及び処置におけるカルパイン阻害剤の使用法 |
| DE19642591A1 (de) * | 1996-10-15 | 1998-04-16 | Basf Ag | Neue Piperidin-Ketocarbonsäure-Derivate, deren Herstellung und Anwendung |
| US6083944A (en) * | 1997-10-07 | 2000-07-04 | Cephalon, Inc. | Quinoline-containing α-ketoamide cysteine and serine protease inhibitors |
| HK1039110A1 (zh) * | 1999-03-15 | 2002-04-12 | Axys Pharmaceuticals, Inc. | 以新颖的合成物及组分作为蛋白酶抑制剂 |
| WO2005000793A1 (ja) * | 2003-06-26 | 2005-01-06 | Taisho Pharmaceutical Co., Ltd. | ２位置換シクロアルキルカルボン酸誘導体 |
| EP1493739A1 (fr) * | 2003-07-03 | 2005-01-05 | Warner-Lambert Company LLC | Dérivés thiophényliques d'aminoacides, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent |
| AR055395A1 (es) * | 2005-08-26 | 2007-08-22 | Vertex Pharma | Compuestos inhibidores de la actividad de la serina proteasa ns3-ns4a del virus de la hepatitis c |
| US7964624B1 (en) * | 2005-08-26 | 2011-06-21 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases |
| KR101578674B1 (ko) * | 2006-12-29 | 2015-12-18 | 아비에 도이치란트 게엠베하 운트 콤파니 카게 | 카복스아미드 화합물 및 칼페인 억제제로서의 이의 용도 |
| US9051304B2 (en) * | 2009-12-22 | 2015-06-09 | AbbVie Deutschland GmbH & Co. KG | Carboxamide compounds and their use as calpain inhibitors V |
| JP2017517475A (ja) * | 2014-02-19 | 2017-06-29 | エーテーハー チューリヒ | 化合物ライブラリーの製造方法 |
| CN109661229B (zh) * | 2016-06-29 | 2022-06-28 | 加利福尼亚大学董事会 | 用于治疗癌症的化合物和组合物 |
| BR112019006110A2 (pt) * | 2016-09-28 | 2019-09-10 | Blade Therapeutics Inc | moduladores de calpaína e usos terapêuticos dos mesmos |
| KR20200139721A (ko) * | 2018-03-28 | 2020-12-14 | 블레이드 테라퓨틱스, 인크. | 섬유성 질환을 치료하는 방법 |
-
2019
- 2019-03-21 CA CA3095164A patent/CA3095164A1/en active Pending
- 2019-03-21 EP EP19777469.8A patent/EP3774737A4/en not_active Withdrawn
- 2019-03-21 US US17/041,596 patent/US20210009564A1/en not_active Abandoned
- 2019-03-21 SG SG11202008750XA patent/SG11202008750XA/en unknown
- 2019-03-21 BR BR112020019560-0A patent/BR112020019560A2/pt not_active Application Discontinuation
- 2019-03-21 JP JP2020551973A patent/JP2021519312A/ja active Pending
- 2019-03-21 PE PE2020001468A patent/PE20212111A1/es unknown
- 2019-03-21 AU AU2019242387A patent/AU2019242387A1/en not_active Abandoned
- 2019-03-21 MX MX2020010033A patent/MX2020010033A/es unknown
- 2019-03-21 CN CN201980035887.9A patent/CN112204014A/zh active Pending
- 2019-03-21 KR KR1020207029538A patent/KR20200139702A/ko not_active Ceased
- 2019-03-21 RU RU2020130022A patent/RU2020130022A/ru unknown
- 2019-03-21 WO PCT/US2019/023457 patent/WO2019190885A1/en not_active Ceased
- 2019-03-28 AR ARP190100806A patent/AR115303A1/es not_active Application Discontinuation
- 2019-03-28 TW TW108111017A patent/TW202003472A/zh unknown
-
2020
- 2020-09-23 IL IL277548A patent/IL277548A/en unknown
- 2020-09-25 CL CL2020002496A patent/CL2020002496A1/es unknown
- 2020-09-25 PH PH12020551555A patent/PH12020551555A1/en unknown
- 2020-09-30 CO CONC2020/0012359A patent/CO2020012359A2/es unknown
- 2020-10-26 EC ECSENADI202068210A patent/ECSP20068210A/es unknown
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