BR112013021848A2 - 5-(fenil/piridinil-etinil)-2-piridina/2-pirimidina-carboxamidas como moduladores de mglur5 - Google Patents
5-(fenil/piridinil-etinil)-2-piridina/2-pirimidina-carboxamidas como moduladores de mglur5Info
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- BR112013021848A2 BR112013021848A2 BR112013021848A BR112013021848A BR112013021848A2 BR 112013021848 A2 BR112013021848 A2 BR 112013021848A2 BR 112013021848 A BR112013021848 A BR 112013021848A BR 112013021848 A BR112013021848 A BR 112013021848A BR 112013021848 A2 BR112013021848 A2 BR 112013021848A2
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- halogen
- lower alkyl
- phenyl
- ring
- hydrogen
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Abstract
resumo patente de invenção: "5-(fenil/piridinil-etinil)-2-piridina/2-pirimidina-carboxamidas como moduladores de mglur5". a presente invenção refere-se a derivados de etinila de fórmula (i) i em que y é n ou c-r3; e r3 é hidrogênio metila, halogênio ou nitrila; r1 é fenila ou piridinila, que são opcionalmente substituídas por halogênio, alquila inferior ou alcóxi inferior; r2/r2' são independentemente um do outro hidrogênio, alquila inferior ou alquila inferior substituída por halogênio, ou r2 e r2' podem formar junto com o átomo n ao qual eles são anexados um anel de morfolina, um anel de piperidina ou um anel de azetidina, que são não substituídos ou são substituídos por um ou mais substituintes selecionados a partir de alcóxi inferior, halogênio, hidróxi ou metila; r4/r4' são independentemente um do outro hidrogênio ou alquila inferior, ou r4 e r4' formam juntos um anel c3-5 cicloalquila-, tetra-hidrofurano- ou oxetano; ou a um sal de adição de ácido farmaceuticamente aceitável, a uma mistura racêmica, ou a seu enantiômero correspondente e/ou isômero ótico e/ou estereoisômero do mesmo. é agora surpreendentemente descoberto que compostos de fórmula (i) são moduladores alostéricos positivos (pam) do receptor de glutamato metabotrópico subtipo 5 (mglur5).
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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EP11162945 | 2011-04-19 | ||
EP11185137 | 2011-10-14 | ||
PCT/EP2012/056966 WO2012143340A1 (en) | 2011-04-19 | 2012-04-17 | 5-(phenyl/pyridinyl-ethinyl)-2-pyridine/ 2-pyrimidine-carborxamides as mglur5 modulators |
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BR112013021848A2 true BR112013021848A2 (pt) | 2016-10-25 |
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BR112013021848A BR112013021848A2 (pt) | 2011-04-19 | 2012-04-17 | 5-(fenil/piridinil-etinil)-2-piridina/2-pirimidina-carboxamidas como moduladores de mglur5 |
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US (1) | US8772300B2 (pt) |
EP (1) | EP2699547B1 (pt) |
JP (1) | JP5753625B2 (pt) |
KR (1) | KR101573998B1 (pt) |
CN (1) | CN103582629B (pt) |
AR (1) | AR086024A1 (pt) |
AU (1) | AU2012244870B2 (pt) |
BR (1) | BR112013021848A2 (pt) |
CA (1) | CA2825971C (pt) |
CL (1) | CL2013002971A1 (pt) |
CO (1) | CO6741199A2 (pt) |
CR (1) | CR20130431A (pt) |
CY (1) | CY1116388T1 (pt) |
DK (1) | DK2699547T3 (pt) |
EA (1) | EA023369B1 (pt) |
EC (1) | ECSP13012980A (pt) |
ES (1) | ES2534086T3 (pt) |
HK (1) | HK1191940A1 (pt) |
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HU (1) | HUE025033T2 (pt) |
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MY (1) | MY161403A (pt) |
PE (1) | PE20140984A1 (pt) |
PL (1) | PL2699547T3 (pt) |
PT (1) | PT2699547E (pt) |
RS (1) | RS53909B1 (pt) |
SG (1) | SG194513A1 (pt) |
SI (1) | SI2699547T1 (pt) |
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Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
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UA110862C2 (uk) * | 2011-10-07 | 2016-02-25 | Ф. Хоффманн-Ля Рош Аг | Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5 |
CA2879489A1 (en) * | 2012-10-18 | 2014-04-24 | F.Hoffmann-La Roche Ag | Ethynyl derivatives as modulators of mglur5 receptor activity |
PE20150628A1 (es) * | 2012-10-18 | 2015-05-11 | Hoffmann La Roche | Derivados de etinilo como moduladores de la actividad del receptor mglur5 |
US10647664B2 (en) * | 2013-08-16 | 2020-05-12 | Duke University | Substituted hydroxamic acid compounds |
MA42508B1 (fr) | 2015-06-03 | 2020-05-29 | Hoffmann La Roche | Dérivés d'éthynyle |
HUE045145T2 (hu) | 2015-07-15 | 2019-12-30 | Hoffmann La Roche | Etinil-származékok metabotróp glutamátreceptor-modulátorokként |
MX2019000442A (es) | 2016-07-18 | 2019-06-20 | Hoffmann La Roche | Derivados de etinilo. |
JP2023536137A (ja) * | 2020-07-29 | 2023-08-23 | ヴィヴォゾン・インコーポレイテッド | mGluR5及び5-HT2A受容体の二重調節剤及びその使用 |
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TW544448B (en) * | 1997-07-11 | 2003-08-01 | Novartis Ag | Pyridine derivatives |
GB0325956D0 (en) | 2003-11-06 | 2003-12-10 | Addex Pharmaceuticals Sa | Novel compounds |
US7879882B2 (en) * | 2004-10-07 | 2011-02-01 | Merck Sharp & Dohme Corp. | Thiazolyl mglur5 antagonists and methods for their use |
WO2006048771A1 (en) | 2004-11-04 | 2006-05-11 | Addex Pharmaceuticals Sa | Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors |
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