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CY1116388T1 - 5-(φαινυλο/πυριδινυλο-αιθινυλο)-2-πυριδινο/2-πυριμιδινο-καρβοξαμιδια ως mglur5 ρυθμιστες - Google Patents

5-(φαινυλο/πυριδινυλο-αιθινυλο)-2-πυριδινο/2-πυριμιδινο-καρβοξαμιδια ως mglur5 ρυθμιστες

Info

Publication number
CY1116388T1
CY1116388T1 CY20151100450T CY151100450T CY1116388T1 CY 1116388 T1 CY1116388 T1 CY 1116388T1 CY 20151100450 T CY20151100450 T CY 20151100450T CY 151100450 T CY151100450 T CY 151100450T CY 1116388 T1 CY1116388 T1 CY 1116388T1
Authority
CY
Cyprus
Prior art keywords
halogen
group
alkyl group
hydrogen
ring
Prior art date
Application number
CY20151100450T
Other languages
English (en)
Inventor
Georg Jaeschke
Synese Jolidon
Lothar Lindemann
Antonio Ricci
Daniel Rueher
Heinz Stadler
Eric Vieira
Original Assignee
F. Hoffmann-La Roche Ag
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=CY1116388(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by F. Hoffmann-La Roche Ag filed Critical F. Hoffmann-La Roche Ag
Publication of CY1116388T1 publication Critical patent/CY1116388T1/el

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Abstract

Η παρούσα εφεύρεση σχετίζεται με αιθινυλο παράγωγα του τύπου (I), όπου το Υ είναι Ν ή C-R3 και το R3 είναι υδρογόνο, μεθυλο ομάδα, αλογόνο ή νιτρίλιο, το R1 είναι φαινυλο ομάδα ή πυριδινυλο ομάδα, οι οποίες είναι προαιρετικώς αποκατεστημένες με αλογόνο, κατώτερο αλκυλο ομάδα ή κατώτερο αλκοξυ ομάδα, τα R2/R2' είναι ανεξαρτήτως το καθένα υδρογόνο, κατώτερο αλκυλο ομάδα ή κατώτερο αλκυλο ομάδα υποκατεστημένη με αλογόνο ή τα R2 και R2' μπορεί να σχηματίζουν μαζί με το Ν-άτομο στο οποίο είναι συνδεδεμένα έναν δακτύλιο μορφολίνης, έναν δακτύλιο πιπεριδίνης ή έναν δακτύλιο αζετιδίνης, οι οποίοι είναι μη αποκατεστημένοι ή υποκατεστημένοι με έναν ή περισσότερους υποκατάστατες που επιλέγονται από κατώτερο αλκοξυ ομάδα, αλογόνο, υδροξυ ομάδα ή μεθυλο ομάδα, τα R4/R4' είναι ανεξαρτήτως το καθένα υδρογόνο ή κατώτερο αλκυλο ομάδα ή τα R4 και R4' σχηματίζουν μαζί έναν C3-5 κυκλοαλκυλο-, τετραϋδροφουρανο- ή έναν οξετανο-δακτύλιο ή με ένα φαρμακευτικώς αποδεκτό άλας προσθήκης οξέος, με ένα ρακεμικό μίγμα ή με το αντίστοιχο εναντιομερές και/ή οπτικό ισομερές και/ή στερεοϊσομερές αυτών. Αναπάντεχα βρέθηκε ότι οι ενώσεις του γενικού τύπου (I) είναι θετικοί αλλοστερικοί ρυθμιστές (ΡΑM) του μεταβοτροπικού γλουταμικού υποδοχέα υποτύπου 5 (mGluR5).
CY20151100450T 2011-04-19 2015-05-20 5-(φαινυλο/πυριδινυλο-αιθινυλο)-2-πυριδινο/2-πυριμιδινο-καρβοξαμιδια ως mglur5 ρυθμιστες CY1116388T1 (el)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11162945 2011-04-19
EP11185137 2011-10-14
EP12714324.6A EP2699547B1 (en) 2011-04-19 2012-04-17 5-(phenyl/pyridinyl-ethinyl)-2-pyridine/2-pyrimidine-carborxamides as mglur5 modulators

Publications (1)

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CY1116388T1 true CY1116388T1 (el) 2017-02-08

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CY20151100450T CY1116388T1 (el) 2011-04-19 2015-05-20 5-(φαινυλο/πυριδινυλο-αιθινυλο)-2-πυριδινο/2-πυριμιδινο-καρβοξαμιδια ως mglur5 ρυθμιστες

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MX2015004086A (es) * 2012-10-18 2015-07-06 Hoffmann La Roche Derivados de etinilo como moduladores de la actividad del receptor de glutamato metabotropico 5 (mglur5).
CA2921427A1 (en) * 2013-08-16 2015-02-19 Duke University Substituted hydroxamic acid compounds
JP6603334B2 (ja) 2015-06-03 2019-11-06 エフ．ホフマン−ラ ロシュ アーゲー エチニル誘導体
MA42442B1 (fr) 2015-07-15 2019-07-31 Hoffmann La Roche Dérivés d'éthynyle comme modulateurs du récepteur métabotropique au glutamate
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