HRP20110805T1 - Homo- i heterociklički spojevi prikladni kao cetp inhibitori - Google Patents

Homo- i heterociklički spojevi prikladni kao cetp inhibitori Download PDF

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HRP20110805T1
HRP20110805T1 HR20110805T HRP20110805T HRP20110805T1 HR P20110805 T1 HRP20110805 T1 HR P20110805T1 HR 20110805 T HR20110805 T HR 20110805T HR P20110805 T HRP20110805 T HR P20110805T HR P20110805 T1 HRP20110805 T1 HR P20110805T1
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Croatia
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compound according
pharmaceutically acceptable
compound
stereoisomers
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HR20110805T
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Inventor
E. Salvati Mark
Finlay Heather
Chen Bang-Chi
S. Harikrishnan Lalgudi
Jiang Ji
A. Johnson James
G. Kamau Muthoni
R. Lawrence Michael
Li Jianqing
Lloyd John
Pi Zulan
X. Qiao Jennifer
Rampulla Richard
C. Wang Tammy
Wang Yufeng
Yang Wu
Y. Roberge Jacques
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Bristol-Myers Squibb Company
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Application filed by Bristol-Myers Squibb Company filed Critical Bristol-Myers Squibb Company
Publication of HRP20110805T1 publication Critical patent/HRP20110805T1/hr

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    • C07C275/26—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of rings other than six-membered aromatic rings
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Abstract

Spoj formule Ia ili Ib ili ili njegovi stereoizomeri ili farmaceutski prihvatljive soli, gdje: A je: B je: ili C je: R1 je: (a) -C(O)R3, pri čemu je R3: (b) -C(O)NHR3, pri čemu je R3: ili (c) -C(O)NR2R3, pri čemu je NR2R3: ili (d) -C(O)OR4, pri čemu je R4: (e) -SO2R5, pri čemu je R5: ili (f) -CSNHR7, pri čemu je R7: (g) -CH2R8, pri čemu je R8: ili (h) -C(S)R3, pri čemu je R3: (i) -C(=NR3)Oalkil, pri čemu je R3: Patent sadrži još 13 patentnih zahtjeva.

Claims (14)

1. Spoj formule Ia ili Ib [image] ili [image] ili njegovi stereoizomeri ili farmaceutski prihvatljive soli, gdje: A je: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] B je: [image] [image] [image] [image] [image] [image] ili [image] C je: [image] [image] [image] [image] [image] [image] R1 je: (a) -C(O)R3, pri čemu je R3: [image] [image] [image] [image] [image] (b) -C(O)NHR3, pri čemu je R3: [image] [image] [image] [image] [image] [image] [image] ili [image] (c) -C(O)NR2R3, pri čemu je NR2R3: [image] [image] [image] ili [image] (d) -C(O)OR4, pri čemu je R4: [image] (e) -SO2R5, pri čemu je R5: [image] ili [image] (f) -CSNHR7, pri čemu je R7: [image] (g) -CH2R8, pri čemu je R8: [image] [image] [image] [image] [image] ili [image] (h) -C(S)R3, pri čemu je R3: [image] (i) -C(=NR3)Oalkil, pri čemu je R3: [image]
2. Spoj formule Ia [image] ili njegovi stereoizomeri ili farmaceutski prihvatljive soli, gdje: A je: [image] [image] [image] [image] [image] ili [image] B je: [image] [image] [image] ili [image] C je: [image] [image] [image] [image] [image] ili [image] R1 je H ili: (a) -C(O)R3, gdje je R3: [image] [image] [image] [image] ili [image] (b) -C(O)NHR3, pri čemu je R3: [image] [image] [image] [image] [image] ili [image] (c) -C(O)NR2R3, pri čemu je NR2R3: [image] (d) -C(O)OR4, pri čemu je R4: [image] [image] ili [image] (e) -SO2R5, pri čemu je R5: [image] ili [image] (f) -CSNHR7, pri čemu je R7: [image] ili [image] (g) -CH2R8, pri čemu je R8: [image] [image] [image] [image] [image] ili [image] (h) -C(S)R3, pri čemu je R3: [image]
3. Spoj prema zahtjevu 1, pri čemu se spoj izabire iz grupe koja obuhvaća: [image] [image] [image] [image] [image] ili njegovi stereoizomeri ili farmaceutski prihvatljivi oblici soli.
4. Spoj prema zahtjevu 3 koji je (R)-N-(1-(3-ciklopropoksi-4-fluorofenil)-1-(3-fluoro-5-(1,1,2,2-tetrafluoroetoksi)fenil)-2-feniletil)-4-fluoro-3-(trifluorometil)-benzamid, njegovi stereoizomeri i farmaceutski prihvatljivi oblici soli.
5. Spoj prema zahtjevu 3, pri čemu je spoj (R)-4-fluoro-N-(1-(4-fluoro-3-izopropoksifenil)-1-(3-fluoro-5-(1,1,2,2-tetrafluoroetoksi)fenil)-2-feniletil)-3-(trifluorometil)benzamid, njegovi stereoizomeri i farmaceutski prihvatljivi oblici soli.
6. Spoj prema zahtjevu 3, pri čemu je spoj 2-amino-N-((R)-1-(3-ciklopropoksi-4-fluorofenil)-1-(3-fluoro-5-(1,1,2,2-tetrafluoro-etoksi)fenil)-2-feniletil)-4,4,4-trifluoro-3-hidroksi-3-(trifluorometil)butanamid, njegovi stereoizomeri i farmaceutski prihvatljivi oblici soli.
7. Farmaceutska smjesa koja sadrži spoj prema bilo kojem od zahtjeva 1 do 6.
8. Farmaceutska smjesa prema zahtjevu 6 koja dalje sadrži farmaceutski prihvatljivi nosač.
9. Farmaceutska smjesa prema zahtjevu 7 koja dalje sadrži barem jednu dodatnu terapijsku tvar.
10. Spoj prema bilo kojem od zahtjeva 1 do 6 za uporabu u postupku inhibicije proteina prijenosnika kolesteril estera.
11. Spoj prema bilo kojem od zahtjeva 1 do 6 za uporabu u postupku liječenja, prevencije ili usporavanja napredovanja Alzheimerove bolesti, ateroskleroze, venske tromboze, periferne vaskularne bolesti, dislipidemije, hiperbetalipoproteinemije, hipoalfalipoproteinemije, hiperkolesterolemije, hipertrigliceridemije, obiteljske hiperkolesterolemije, kardiovaskularnih poremećaja, angine, ishemije, srčane ishemije, moždanog udara, infarkta miokarda, reperfuzijske ozljede, angioplastične restenoze, hipertenzije, vaskularnih komplikacija dijabetesa, pretilosti ili endotoksemije kod sisavca.
12. Spoj prema bilo kojem od zahtjeva 1 do 6 za uporabu u postupku liječenja, prevencije ili usporavanja napredovanja bolesti kod koje je potrebna terapija inhibitorom proteina prijenosnika kolesteril estera.
13. Spoj prema bilo kojem od zahtjeva 1 do 6 za uporabu u postupku inhibicije proizvodnje lipoproteinskih ostataka.
14. Spoj prema bilo kojem od zahtjeva 1 do 6 za uporabu u postupku povećanja HDL kolesterola kod sisavca.
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