CA2819087A1 - Carboxamide compounds and their use as calpain inhibitors v - Google Patents
Carboxamide compounds and their use as calpain inhibitors v Download PDFInfo
- Publication number
- CA2819087A1 CA2819087A1 CA2819087A CA2819087A CA2819087A1 CA 2819087 A1 CA2819087 A1 CA 2819087A1 CA 2819087 A CA2819087 A CA 2819087A CA 2819087 A CA2819087 A CA 2819087A CA 2819087 A1 CA2819087 A1 CA 2819087A1
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- Prior art keywords
- alkyl
- hetaryl
- aryl
- cycloalkyl
- radicals
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- -1 Carboxamide compounds Chemical class 0.000 title claims abstract description 837
- 108010079785 calpain inhibitors Proteins 0.000 title description 25
- 150000001875 compounds Chemical class 0.000 claims abstract description 297
- 108010032088 Calpain Proteins 0.000 claims abstract description 91
- 102000007590 Calpain Human genes 0.000 claims abstract description 91
- 229910052736 halogen Inorganic materials 0.000 claims abstract description 35
- 150000002367 halogens Chemical class 0.000 claims abstract description 35
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract description 35
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract description 28
- 150000003839 salts Chemical class 0.000 claims abstract description 26
- 239000003814 drug Substances 0.000 claims abstract description 23
- 230000000694 effects Effects 0.000 claims abstract description 23
- 150000004677 hydrates Chemical class 0.000 claims abstract description 21
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract description 18
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical compound F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 claims abstract description 8
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- VUWZPRWSIVNGKG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH2] VUWZPRWSIVNGKG-UHFFFAOYSA-N 0.000 claims abstract description 8
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- QQPUPOYIRHLEPY-UHFFFAOYSA-N 2-(6-fluoroindazol-2-yl)-n-[4-(methoxyamino)-3,4-dioxo-1-phenylbutan-2-yl]pyridine-3-carboxamide Chemical compound C=1C=CN=C(N2N=C3C=C(F)C=CC3=C2)C=1C(=O)NC(C(=O)C(=O)NOC)CC1=CC=CC=C1 QQPUPOYIRHLEPY-UHFFFAOYSA-N 0.000 claims 1
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Classifications
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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Landscapes
- Health & Medical Sciences (AREA)
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Applications Claiming Priority (3)
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| US42132310P | 2010-12-09 | 2010-12-09 | |
| US61/421,323 | 2010-12-09 | ||
| PCT/EP2011/072164 WO2012076639A1 (en) | 2010-12-09 | 2011-12-08 | Carboxamide compounds and their use as calpain inhibitors v |
Publications (1)
| Publication Number | Publication Date |
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| CA2819087A1 true CA2819087A1 (en) | 2012-06-14 |
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| CA2819087A Abandoned CA2819087A1 (en) | 2010-12-09 | 2011-12-08 | Carboxamide compounds and their use as calpain inhibitors v |
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| US (1) | US9062027B2 (https=) |
| EP (1) | EP2648731B1 (https=) |
| JP (1) | JP2013544866A (https=) |
| CN (1) | CN103501784A (https=) |
| CA (1) | CA2819087A1 (https=) |
| MX (1) | MX2013006419A (https=) |
| WO (1) | WO2012076639A1 (https=) |
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| US20150320706A1 (en) | 2014-05-12 | 2015-11-12 | Chiesi Farmaceutici S.P.A. | Formulations and methods of treating alzheimer's disease and other proteinopathies by combination therapy |
| WO2017156071A1 (en) | 2016-03-09 | 2017-09-14 | Blade Therapeutics, Inc. | Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof |
| 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 |
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| US4826835A (en) | 1985-10-23 | 1989-05-02 | Rorer Pharmaceutical Corporation | Pyridyl-pyridazinone and pyridyl-pyrazolinone compounds and their use in the treatment of congestive heart failure |
| US4743608A (en) | 1986-07-15 | 1988-05-10 | Rorer Pharmaceutical Corporation | Pyridone-pyridyl-imidazolyl and triazolyl compounds and their use as cardiotonic agents |
| DE19642591A1 (de) | 1996-10-15 | 1998-04-16 | Basf Ag | Neue Piperidin-Ketocarbonsäure-Derivate, deren Herstellung und Anwendung |
| DE19650975A1 (de) | 1996-12-09 | 1998-06-10 | Basf Ag | Neue heterocyclisch substituierte Benzamide und deren Anwendung |
| CN1245486A (zh) | 1996-12-11 | 2000-02-23 | Basf公司 | 用作钙蛋白酶抑制剂的酮苯甲酰胺 |
| US6083944A (en) | 1997-10-07 | 2000-07-04 | Cephalon, Inc. | Quinoline-containing α-ketoamide cysteine and serine protease inhibitors |
| WO1999054305A1 (de) | 1998-04-20 | 1999-10-28 | Basf Aktiengesellschaft | Heterocyclisch substituierte amide als calpainhemmer |
| TR200003068T2 (tr) | 1998-04-20 | 2001-03-21 | Basf Aktiengesellschaft | Yeni amidler, üretimi ve kullanımı |
| DE19817459A1 (de) | 1998-04-20 | 1999-10-21 | Basf Ag | Neue heterozyklische substituierte Amide, Herstellung und Anwendung |
| DE19818614A1 (de) | 1998-04-20 | 1999-10-21 | Basf Ag | Neue substituierte Amide, deren Herstellung und Anwendung |
| CN1306526A (zh) | 1998-04-20 | 2001-08-01 | Basf公司 | 具有半胱氨酸蛋白酶抑制作用的新的杂环取代酰胺 |
| EP1080074B1 (de) | 1998-05-25 | 2006-11-08 | Abbott GmbH & Co. KG | Heterocyclische substituierte Amide, deren Herstellung und Verwendung |
| DE10114762A1 (de) | 2001-03-26 | 2002-10-02 | Knoll Gmbh | Verwendung von Cysteinprotease-Inhibitoren |
| AU2006275413B2 (en) | 2005-08-02 | 2012-07-19 | 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 |
| JP2010519339A (ja) | 2007-02-26 | 2010-06-03 | アキリオン ファーマシューティカルズ，インコーポレーテッド | Ｈｃｖ複製阻害剤として有用な三級アミン置換ペプチド |
| TWI453019B (zh) * | 2007-12-28 | 2014-09-21 | Abbvie Deutschland | 甲醯胺化合物 |
| TWI519530B (zh) * | 2009-02-20 | 2016-02-01 | 艾伯維德國有限及兩合公司 | 羰醯胺化合物及其作為鈣蛋白酶（ｃａｌｐａｉｎ）抑制劑之用途 |
| US9051304B2 (en) * | 2009-12-22 | 2015-06-09 | AbbVie Deutschland GmbH & Co. KG | Carboxamide compounds and their use as calpain inhibitors V |
| US8598211B2 (en) * | 2009-12-22 | 2013-12-03 | Abbvie Inc. | Carboxamide compounds and their use as calpain inhibitors IV |
-
2011
- 2011-12-08 WO PCT/EP2011/072164 patent/WO2012076639A1/en not_active Ceased
- 2011-12-08 MX MX2013006419A patent/MX2013006419A/es not_active Application Discontinuation
- 2011-12-08 CA CA2819087A patent/CA2819087A1/en not_active Abandoned
- 2011-12-08 JP JP2013542537A patent/JP2013544866A/ja not_active Ceased
- 2011-12-08 CN CN201180067241.2A patent/CN103501784A/zh active Pending
- 2011-12-08 EP EP11796664.8A patent/EP2648731B1/en not_active Not-in-force
- 2011-12-08 US US13/992,582 patent/US9062027B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| EP2648731B1 (en) | 2017-01-25 |
| WO2012076639A1 (en) | 2012-06-14 |
| US9062027B2 (en) | 2015-06-23 |
| EP2648731A1 (en) | 2013-10-16 |
| US20140005227A1 (en) | 2014-01-02 |
| JP2013544866A (ja) | 2013-12-19 |
| CN103501784A (zh) | 2014-01-08 |
| MX2013006419A (es) | 2013-12-16 |
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| Date | Code | Title | Description |
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| FZDE | Discontinued |
Effective date: 20171208 |