HRP20080549T3 - 1,3,5-trisupstituirani derivati 4,5-dihidro-1h-pirazola kao antagonisti cb1 - Google Patents

1,3,5-trisupstituirani derivati 4,5-dihidro-1h-pirazola kao antagonisti cb1

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Publication number
HRP20080549T3
HRP20080549T3 HR20080549T HRP20080549T HRP20080549T3 HR P20080549 T3 HRP20080549 T3 HR P20080549T3 HR 20080549 T HR20080549 T HR 20080549T HR P20080549 T HRP20080549 T HR P20080549T HR P20080549 T3 HRP20080549 T3 HR P20080549T3
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Croatia
Prior art keywords
pyrazole derivatives
trisubstituted
dihydro
antagonistic activity
compounds
Prior art date
Application number
HR20080549T
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English (en)
Inventor
H. M. Lange Josephus
G. Kruse Cornelis
H. Van Stuivenberg Herman
Original Assignee
Solvay Pharmaceuticals B.V.
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Publication date
Application filed by Solvay Pharmaceuticals B.V. filed Critical Solvay Pharmaceuticals B.V.
Publication of HRP20080549T3 publication Critical patent/HRP20080549T3/hr

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    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/06—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
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Abstract

Spojevi prikazani općom formulom (I) naznačeni time da: - R1 i R2 neovisno predstavljaju fenil, tienil ili piridil, pri čemu ove skupine mogu biti supstituirane sa 1, 2 ili 3 supstituenta Y, koji mogu identični ili različiti, odabiru se iz skupine koju sačinjavaju razgranati ili ravnolančani C1-3-alkil ili alkoksi, fenil, hidroksi, kloro, bromo, fluoro, jodo, trifluorometil, trifluorometiltio, trifluorometoksi, metilsulfonil, karboksil, trifluorometilsulfonil, cijano, karbamoil, sulfamoil i acetil, ili R1 i/ili R2 predstavljaju naftil, -X predstavlja jednu od podskupina (i) ili (ii), u kojima-R3 predstavlja atom vodika ili razgranatu ili ravnolančanu C1-3 alkil skupinu, -R4 predstavlja razgranatu ili ravnolančanu C1-8 alkil ili C3-8-cikloalkil-C1-2-alkil skupinu, razgranati ili ravnolančani C1-8 alkoksi, C3-8 cikloalkil, C5-10 bicikloalkil, C6-10 tricikloalkil, koji mogu sadržavati jedan ili više heteroatoma iz skupine (O, N, S) i kojimogu biti supstituirani sa hidroksi skupinom, 1-3metil skupine, etil skupinom ili 1-3 atoma fluora, ili R4 predstavlja fenoksi, benzil, fenetil ili fenilpropil skupinu, opcionalno na vlastitom prstenu supstituirane sa 1-3 supstituenta Y, pri čemu Yima značenje navedeno u gornjem tekstu, ili R4 predstavlja piridil ili tienil skupinu, ili R4 predstavlja skupinu NR5R6 u kojoj R5 i R6 - zajedno sa dušikovim atomom na kojeg su vezani - tvore zasićenu ili nezasićenu, monocikličku ili bicikličku, heterocikličku skupinu sa 4 do 10 atoma u sklopu prstena, pri čemu heterociklička skupina sadržava jedan ili dva heteroatoma iz skupine (O, N, S) i samamože biti supstituirana sa razgranatom ili ravnolančanom C1-3 alkil, fenil, hidroksi ili trifluorometil skupinom ili atomom fluora, ili R3 i R4 - zajedno sa dušikovim atomom na kojeg su vezani - tvore zasićenu ili nezasićenu, monocikličku ili bicikličku, heterocikličku skupinu sa 4 do 10 atoma u sklopu prstena, pri čemu heterociklička skupina sadržava jedan ili dva heteroatoma iz skupine (O, N, S) i sama može biti supstituirana sa razgranatom ili ravnolančanom C1-3 alkil, fenil, amino, hidroksiili trifluorometil skupinom ili atomom fluora, - R7 predstavlja benzil, fenil, tienil ili piridil skupinu, koje na vlastitiom aromatskom prstenu mogubiti supstituirane sa 1, 2, 3 ili 4 supstituenta Y, pri čemu Y ima značenje navedeno u gornjem tekstu, koji mogu biti identični ili različiti, ili R7predstavlja C1-8 razgranati ili ravnolančani alkil, C3-8 alkenil, C3-10 cikloalkil, C5-10 bicikloalkil, C6-10 tricikloalkil ili C5-8 cikloalkenil iliR7 predstavlja naftil ili R7 predstavlja amino skupinu ili R7 predstavlja C1-8 dialkilamino skupinu, C1-8 monoalkilamino skupinu ili zasićenu ili nezasićenu, monocikličku ili bicikličku, heterocikličku skupinu sa 4 do 10 atoma u sklopu prstena, pri čemu heterociklička skupina sadržava jedan ili dvaatoma dušika i može sadržavati 1 heteroatom iz skupine (O, S) i može opcionalno biti supstituirana sa razgranatom ili ravnolančanom C1-3 alkil, fenil, hidroksi
HR20080549T 2004-01-30 2008-10-27 1,3,5-trisupstituirani derivati 4,5-dihidro-1h-pirazola kao antagonisti cb1 HRP20080549T3 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US53998304P 2004-01-30 2004-01-30
EP04100338 2004-01-30
PCT/EP2005/050339 WO2005074920A1 (en) 2004-01-30 2005-01-27 1,3,5-trisubstituted 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity

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HRP20080549T3 true HRP20080549T3 (hr) 2008-11-30

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HR20080549T HRP20080549T3 (hr) 2004-01-30 2008-10-27 1,3,5-trisupstituirani derivati 4,5-dihidro-1h-pirazola kao antagonisti cb1

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EP (1) EP1713475B1 (hr)
JP (1) JP4693787B2 (hr)
KR (1) KR20060131861A (hr)
CN (1) CN100563651C (hr)
AT (1) ATE402697T1 (hr)
AU (1) AU2005210163B2 (hr)
BR (1) BRPI0507005A (hr)
CA (1) CA2552940A1 (hr)
DE (1) DE602005008555D1 (hr)
DK (1) DK1713475T3 (hr)
ES (1) ES2311972T3 (hr)
HK (1) HK1099688A1 (hr)
HR (1) HRP20080549T3 (hr)
IL (1) IL176547A (hr)
MX (1) MXPA06008593A (hr)
NO (1) NO20063866L (hr)
PL (1) PL1713475T3 (hr)
PT (1) PT1713475E (hr)
RU (1) RU2360904C2 (hr)
SI (1) SI1713475T1 (hr)
WO (1) WO2005074920A1 (hr)

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