CY1116896T1 - Ανταγωνιστες του υποδοχεα trpm8 - Google Patents

Ανταγωνιστες του υποδοχεα trpm8

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Publication number
CY1116896T1
CY1116896T1 CY20151100989T CY151100989T CY1116896T1 CY 1116896 T1 CY1116896 T1 CY 1116896T1 CY 20151100989 T CY20151100989 T CY 20151100989T CY 151100989 T CY151100989 T CY 151100989T CY 1116896 T1 CY1116896 T1 CY 1116896T1
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Cyprus
Prior art keywords
branched
substituted
alkyl
linear
unsubstituted
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CY20151100989T
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English (en)
Inventor
Alessio Moriconi
Gianluca Bianchini
Laura Brandolini
Andrea Aramini
Chiara Liberati
Silvia Bovolenta
Andrea Beccari
Simone Lorenzi
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Dompé Farmaceutici S.P.A.
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Publication of CY1116896T1 publication Critical patent/CY1116896T1/el

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Abstract

Ενώσεις δρώντας ως επιλεκτικοί ανταγωνιστές του μέλους 8 της υπο-οικογένειας Μ διαύλων κατιόντων Παροδικών Δυναμικών Υποδοχέων (εις το παρόν και μεταταύτα αναφέρεται και ως TRPM8), έχοντας τον χημικό τύπο (I), όπου το R επιλέγεται από - Η, Br, CN, ΝΟ2, SO2NH2, SΟ2NHR' και SO2NR'2 όπου το R' επιλέγεται από γραμμικό ή διακλαδισμένο C1-C4 αλκύλιο· το Χ επιλέγεται από: -F, C1, C1-C3 αλκύλιο, ΝΗ2 και ΟΗ· το Υ επιλέγεται από: - Ο, CH2, ΝΗ και SO2· τα R1 και R2, ανεξαρτήτως του ένα από το άλλο, επιλέγονται από - Η, F και γραμμικό ή διακλαδισμένο C1-C4 αλκύλιο· τα R3 και R4, ανεξαρτήτως του ένα από το άλλο, επιλέγονται από - Η και γραμμικό ή διακλαδισμένο C1-C4 αλκύλιο· το Ζ επιλέγεται από: - NR6 και R6R7N+, όπου τα R6 και R7, ανεξαρτήτως το ένα από το άλλο, επιλέγονται από: - Η και γραμμικό ή διακλαδισμένο C1-C4 αλκύλιο· το R5 είναι ένα κατάλοιπο που επιλέγεται από: - Η και γραμμικό ή διακλαδισμένο C1-C4 αλκύλιο· το Het είναι ένα μια ομάδα ετεροαρυλίου που επιλέγεται από: -ένα υποκατεστημένο ή μη-υποκατεστημένο πυρρολύλιο, ένα υποκατεστημένο ή μη-υποκατεστημένο Ν- μεθυλπυρρολύλιο, ένα υποκατεστημένο ή μη-υποκατεστημένο θειοφαινύλιο, ένα υποκατεστημένο ή μη-υποκατεστημένο φουρύλιο και ένα υποκατεστημένο ή μη-υποκατεστημένο πυριδινύλιο. Οι εν λόγω ενώσεις είναι χρήσιμες στην πρόληψη και αγωγή παθολογιών εξαρτώμενης της δραστηριότητας του TRPM8 όπως είναι ο πόνος, η φλεγμονή, η ισχαιμία, η νευροεκφύλιση, το εγκεφαλικό επεισόδιο, οι ψυχιατρικές διαταραχές, οι φλεγμονώδεις καταστάσεις και οι ουρολογικές διαταραχές.
CY20151100989T 2011-01-28 2015-11-05 Ανταγωνιστες του υποδοχεα trpm8 CY1116896T1 (el)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11425021A EP2481727A1 (en) 2011-01-28 2011-01-28 TRPM8 receptor antagonists
EP12705078.9A EP2668160B1 (en) 2011-01-28 2012-01-27 Trpm8 receptor antagonists

Publications (1)

Publication Number Publication Date
CY1116896T1 true CY1116896T1 (el) 2017-04-05

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US (1) US8906946B2 (el)
EP (2) EP2481727A1 (el)
JP (1) JP6043298B2 (el)
KR (1) KR101872553B1 (el)
CN (1) CN103443077B (el)
AU (1) AU2012210472B2 (el)
CY (1) CY1116896T1 (el)
DK (1) DK2668160T3 (el)
EA (1) EA022943B1 (el)
ES (1) ES2552533T3 (el)
HK (1) HK1192228A1 (el)
HR (1) HRP20151163T1 (el)
HU (1) HUE026587T2 (el)
ME (1) ME02290B (el)
PL (1) PL2668160T3 (el)
PT (1) PT2668160E (el)
RS (1) RS54337B1 (el)
SI (1) SI2668160T1 (el)
SM (1) SMT201500296B (el)
WO (1) WO2012101244A1 (el)
ZA (1) ZA201305576B (el)

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WO2017058594A1 (en) * 2015-10-01 2017-04-06 Senomyx, Inc. Compounds useful as modulators of trpm8
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CA3022808A1 (en) 2016-06-13 2017-12-21 Mitsubishi Tanabe Pharma Corporation Compositions for treating or preventing vasomotor symptoms
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WO2024126650A1 (en) 2022-12-15 2024-06-20 Syngenta Crop Protection Ag Novel bicyclic-carboxamide compounds useful as pesticides

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US8906946B2 (en) 2014-12-09
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