BRPI1014184A8 - compostos carboxamida e seus usos como inibidores de calpaína - Google Patents
compostos carboxamida e seus usos como inibidores de calpaínaInfo
- Publication number
- BRPI1014184A8 BRPI1014184A8 BRPI1014184A BRPI1014184A BRPI1014184A8 BR PI1014184 A8 BRPI1014184 A8 BR PI1014184A8 BR PI1014184 A BRPI1014184 A BR PI1014184A BR PI1014184 A BRPI1014184 A BR PI1014184A BR PI1014184 A8 BRPI1014184 A8 BR PI1014184A8
- Authority
- BR
- Brazil
- Prior art keywords
- compounds
- carboxamide compounds
- meanings mentioned
- carboxamide
- tautomers
- Prior art date
Links
- -1 carboxamide compounds Chemical class 0.000 title abstract 5
- 108010079785 calpain inhibitors Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102000007590 Calpain Human genes 0.000 abstract 2
- 108010032088 Calpain Proteins 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 abstract 1
- 102000005927 Cysteine Proteases Human genes 0.000 abstract 1
- 108010005843 Cysteine Proteases Proteins 0.000 abstract 1
- 229910052791 calcium Inorganic materials 0.000 abstract 1
- 239000011575 calcium Substances 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
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- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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Abstract
COMPOSTOS CARBOXAMIDA E SEUS USOS COMO INIBIDORES DE CALPAÍNA. A presente invenção refere-se aos novos compostos carboxamida e seus usos para a fabricação de um medicamento. Os compostos carboxamida são inibidores de calpaína (proteases de cisteína dependentes de cálcio). A invenção portanto ainda refere-se ao uso destes compostos carboxamida para o tratamento de um transtorno associado com uma atividade elevada de calpaína. Os compostos carboxamida são compostos de fórmula geral I. No qual R1, R2, R3a, R3b, R4, Q, Y, A e X têm os significados nas reivindicações e na descrição, os tautômeros e os sais farmaceuticamente apropriados dos mesmos. Em particular,os compostos têm a fórmula geral la e Ib. Na qual R1, r, R2b, R3a, R3b, R4, Y e X têm os significados mencionados nas reivindicações, incluindo os tautômeros e os sais farmaceuticamente apropriados dos mesmos. Destes compostos, são preferenciais aqueles onde Y é uma fração CH2-CH2, CH2-CH2-CH2, N(Ry#)-CH2, N(Ry#)-CH2-CH2 or CH=CH-CH=, cada uma opcionalmente contendo 1 ou 2 átomos de H substituídos com radicais Ry idênticos ou diferentes, onde Ry e Ry# têm os significados nas reivindicações.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17613809P | 2009-05-07 | 2009-05-07 | |
| US28975309P | 2009-12-23 | 2009-12-23 | |
| PCT/EP2010/056166 WO2010128102A1 (en) | 2009-05-07 | 2010-05-06 | Carboxamide compounds and their use as calpain inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BRPI1014184A2 BRPI1014184A2 (pt) | 2017-05-16 |
| BRPI1014184A8 true BRPI1014184A8 (pt) | 2017-11-07 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI1014184A BRPI1014184A8 (pt) | 2009-05-07 | 2010-05-06 | compostos carboxamida e seus usos como inibidores de calpaína |
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| US (4) | US8236798B2 (pt) |
| EP (1) | EP2427429B1 (pt) |
| JP (1) | JP5709846B2 (pt) |
| KR (1) | KR20140014388A (pt) |
| CN (1) | CN102482212B (pt) |
| AR (1) | AR076755A1 (pt) |
| AU (1) | AU2010244443B2 (pt) |
| BR (1) | BRPI1014184A8 (pt) |
| CA (1) | CA2760464A1 (pt) |
| CL (1) | CL2011002766A1 (pt) |
| CO (1) | CO6470862A2 (pt) |
| CR (1) | CR20110630A (pt) |
| DO (2) | DOP2011000338A (pt) |
| EC (1) | ECSP11011503A (pt) |
| ES (1) | ES2625437T3 (pt) |
| IL (1) | IL215835A (pt) |
| MX (2) | MX341176B (pt) |
| NZ (1) | NZ596000A (pt) |
| PE (1) | PE20120901A1 (pt) |
| PH (1) | PH12013502359A1 (pt) |
| RU (1) | RU2540856C2 (pt) |
| SG (2) | SG2014014740A (pt) |
| TW (1) | TWI457334B (pt) |
| UA (1) | UA107459C2 (pt) |
| UY (1) | UY32615A (pt) |
| WO (1) | WO2010128102A1 (pt) |
Families Citing this family (12)
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| US9051304B2 (en) * | 2009-12-22 | 2015-06-09 | AbbVie Deutschland GmbH & Co. KG | Carboxamide compounds and their use as calpain inhibitors V |
| WO2012166389A1 (en) | 2011-05-31 | 2012-12-06 | Theravance, Inc. | Neprilysin inhibitors |
| ES2653215T3 (es) | 2011-05-31 | 2018-02-06 | Theravance Biopharma R&D Ip, Llc | Inhibidores de neprilisina |
| JP5959075B2 (ja) * | 2011-05-31 | 2016-08-02 | セラヴァンス バイオファーマ アール&ディー アイピー, エルエルシー | ネプリライシン阻害剤 |
| ITMI20121668A1 (it) * | 2012-10-05 | 2014-04-06 | Dipharma Francis Srl | Sintesi di un intermedio di un composto antivirale |
| CN104458709A (zh) * | 2013-09-12 | 2015-03-25 | 中国药科大学 | 一种筛选钙激活中性蛋白酶-1抑制剂高通量筛选方法 |
| DE102014110782A1 (de) * | 2014-07-30 | 2016-02-04 | Eberhard Karls Universität Tübingen Medizinische Fakultät | Herstellung von Pyrrolidinderivaten |
| 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 |
| WO2018050631A1 (en) * | 2016-09-13 | 2018-03-22 | Haplogen Gmbh | Antiviral compounds |
| BR112019006110A2 (pt) | 2016-09-28 | 2019-09-10 | Blade Therapeutics Inc | moduladores de calpaína e usos terapêuticos dos mesmos |
| EP4488264A4 (en) * | 2022-03-01 | 2026-03-04 | Westvac Biopharma Co Ltd | CETO AMIDE DERIVATIVES AND THEIR PHARMACEUTICAL USE |
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