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MA35113B1 - 5-(phényl/pyridinyl-éthinyl)-2-pyridine/2 pyrimidine-carboxamides comme modulateur de mglur5 - Google Patents

5-(phényl/pyridinyl-éthinyl)-2-pyridine/2 pyrimidine-carboxamides comme modulateur de mglur5

Info

Publication number
MA35113B1
MA35113B1 MA36413A MA36413A MA35113B1 MA 35113 B1 MA35113 B1 MA 35113B1 MA 36413 A MA36413 A MA 36413A MA 36413 A MA36413 A MA 36413A MA 35113 B1 MA35113 B1 MA 35113B1
Authority
MA
Morocco
Prior art keywords
group
lower alkyl
halogen atom
alkyl group
ring
Prior art date
Application number
MA36413A
Other languages
English (en)
Inventor
Georg Jaeschke
Synese Jolidon
Lothar Lindemann
Antonio Ricci
Daniel Rueher
Heinz Stadler
Eric Vieira
Original Assignee
Hoffmann La Roche
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45954677&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MA35113(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MA35113B1 publication Critical patent/MA35113B1/fr

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  • Pyridine Compounds (AREA)
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Abstract

La présente invention porte sur des dérivés éthinyliques de formule (i), dans laquelle y représente n ou c-r3; r3 représente l'atome d'hydrogène, le groupe méthyle, un atome d'halogène ou le groupe nitrile; r1 représente le groupe phényle ou le groupe pyridinyle, qui sont éventuellement substitués par un atome d'halogène, un groupe alkyle inférieur ou un groupe alcoxyle inférieur; r2/r2' représentent chacun indépendamment de l'autre l'atome d'hydrogène, un groupe alkyle inférieur ou un groupe alkyle inférieur substitué par un atome d'halogène ou r2 et r2' peuvent former conjointement avec l'atome de n auquel ils sont liés un noyau morpholine, un noyau pipéridine ou un noyau azétidine, qui sont non substitués ou substitués par un ou plusieurs substituants choisis parmi un groupe alcoxyle inférieur, un atome d'halogène, le groupe hydroxyle ou le groupe méthyle; r4/r4' représentent chacun indépendamment de l'autre l'atome d'hydrogène ou un groupe alkyle inférieur ou r4 et r4' forment ensemble un noyau cycloalkyle en c3-5, tétrahydrofurane ou oxétane; ou sur un sel d'addition d'acide pharmaceutiquement acceptable, sur un mélange racémique ou sur son énantiomère et/ou un isomère optique et/ou stéréoisomère de ceux-ci. Il a été désormais étonnamment trouvé que les composés représentés par la formule générale (i) sont des modulateurs allostériques positifs (map) du sous-type 5 des récepteurs métabotropiques au glutamate (mglur5).
MA36413A 2011-04-19 2013-11-11 5-(phényl/pyridinyl-éthinyl)-2-pyridine/2 pyrimidine-carboxamides comme modulateur de mglur5 MA35113B1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11162945 2011-04-19
EP11185137 2011-10-14
PCT/EP2012/056966 WO2012143340A1 (fr) 2011-04-19 2012-04-17 5-(phényl/pyridinyl-éthinyl)-2-pyridine/2 pyrimidine-carboxamides comme modulateur de mglur5

Publications (1)

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MA35113B1 true MA35113B1 (fr) 2014-05-02

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MA36413A MA35113B1 (fr) 2011-04-19 2013-11-11 5-(phényl/pyridinyl-éthinyl)-2-pyridine/2 pyrimidine-carboxamides comme modulateur de mglur5

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US (1) US8772300B2 (fr)
EP (1) EP2699547B1 (fr)
JP (1) JP5753625B2 (fr)
KR (1) KR101573998B1 (fr)
CN (1) CN103582629B (fr)
AR (1) AR086024A1 (fr)
AU (1) AU2012244870B2 (fr)
BR (1) BR112013021848A2 (fr)
CA (1) CA2825971C (fr)
CL (1) CL2013002971A1 (fr)
CO (1) CO6741199A2 (fr)
CR (1) CR20130431A (fr)
CY (1) CY1116388T1 (fr)
DK (1) DK2699547T3 (fr)
EA (1) EA023369B1 (fr)
EC (1) ECSP13012980A (fr)
ES (1) ES2534086T3 (fr)
HR (1) HRP20150569T1 (fr)
HU (1) HUE025033T2 (fr)
IL (1) IL227662A (fr)
MA (1) MA35113B1 (fr)
MX (1) MX338631B (fr)
MY (1) MY161403A (fr)
PE (1) PE20140984A1 (fr)
PH (1) PH12013501572A1 (fr)
PL (1) PL2699547T3 (fr)
PT (1) PT2699547E (fr)
RS (1) RS53909B1 (fr)
SG (1) SG194513A1 (fr)
SI (1) SI2699547T1 (fr)
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WO (1) WO2012143340A1 (fr)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA110862C2 (uk) * 2011-10-07 2016-02-25 Ф. Хоффманн-Ля Рош Аг Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5
UA114008C2 (xx) * 2012-10-18 2017-04-10 Похідні етинілу як модулятори активності рецептора mglur5
SG11201501375YA (en) * 2012-10-18 2015-03-30 Hoffmann La Roche Ethynyl derivatives as modulators of mglur5 receptor activity
JP6458270B2 (ja) * 2013-08-16 2019-01-30 デューク ユニバーシティ 置換されたヒドロキサム酸化合物
MX378334B (es) 2015-06-03 2025-03-10 Hoffmann La Roche Modulador alostérico negativo de un receptor de glutamato metabotrópico (nam) y el uso del mismo para tratar ansiedad, dolor, depresión, parkinson y reflujo gastroesofágico.
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