HRP20110860T1 - Supstituirani derivati heteroarilpiperidina kao modulatori receptora melanokortina-4 - Google Patents

Supstituirani derivati heteroarilpiperidina kao modulatori receptora melanokortina-4 Download PDF

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HRP20110860T1
HRP20110860T1 HR20110860T HRP20110860T HRP20110860T1 HR P20110860 T1 HRP20110860 T1 HR P20110860T1 HR 20110860 T HR20110860 T HR 20110860T HR P20110860 T HRP20110860 T HR P20110860T HR P20110860 T1 HRP20110860 T1 HR P20110860T1
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alkyl
halogen
optionally substituted
alkylene
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Herzner Holger
Soeberdt Michael
Weyermann Philipp
Nordhoff Sonja
Feurer Achim
Deppe Holger
Siendt Herv�
Terinek Miroslav
Rummey Christian
Henneb�hle Marco
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Abstract

Spoj prema formuli (I) i enantiomeri, diastereomeri, tautomeri, solvati i njegove farmaceutski prihvatljive soli, naznačen time daR1 je -N(R10)-(C(R6)2)m-T-(C(R6)2)l-T ili-O-(C(R6)2)m-T; R6 je neovisno odabran izmeđuH, F, OH, OCH3,C1-6-alkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN, OH i OCH3 iC3-6-cikloalkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN, OH i OCH3;T je NR7R8,R7 i R8 neovisno su jedan od drugoga odabrani između H, C1-6-alkila, C2-6-alkenila, C2-6-alkinila iC2-6-alkilen-O- C1-6-alkila, pri čemu je svaki alkil, alkenil i alkinil po izboru supstituiran s jednim ili više atoma halogena, CN ili OH; R9 neovisno je odabran izmeđuhalogena, CN, OH, C1-6-alkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN i OH i O- C1-6-alkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN i OH, C1-6-alkilen-O- C1-6-alkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN i OH iliNR12R13;R10 je H ili C1-6-alkil; R11 neovisno je odabran izmeđuhalogena, CN, OH, C1-6-alkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN i OH, C2-6-alkenila, C2-6-alkinila, O- C1-6-alkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN i OH, C1-6-alkilen-O- C1-6-alkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN i OH, C0-6-alkil-C3-6-cikloalkila, -OC(O) C1-6-alkila, -NH2,-NH(C1-6-alkil) i-N(C1-6-alkil)2;R12 i R13 neovisno su jedan od drugoga odabrani izmeđuC1-6-alkila, koji je po izboru supstituiran s OH, C2-6-alkenila, C2-6-alkinila, C2-6-alkilen-O- C1-6alkila iC2-6-alkilen-N-(C1-6-alkil)2;W je CH, O ili NR10;X je CH ili N; Y je CH ili N; Z je CH ili N; A je 3-člani do 7-člani zasićeni, nezasićeni ili aromatski prsten koji sadržava 0-2 atoma dušika; B je CR2 ili N; G je CR2 ili N; D je CR2 ili N; E je CR2 ili N; pod uvjetom da jedna ili dvije od varijabli B, G, D i E mora biti N; R2 neovisno je odabran izmeđuH, F, Cl, CH3,OCH3 iCF3;R3 je H, Cl, F ili CH3;R4 je Cl, F ili CH3;R5 jemorfolin, po izboru supstituiran s 1 do 3 ista ili različita supstituenta R14, 4-članim do 7-članim, zasićenim ilidjelomično zasićenim heterociklom koji u prstenu ima jedan atom dušika i po izboru još jedan heteroatomkoji je odabran između O, N and S, pri čemu je heterocikl po izboru supstituiran s 1 do 4 ista ili različita supstituentaR11 iliNR12R13;R14 je C1-6-alkil, C1-6-alkilen-O- C1-6-alkil, C1-6-alkilen-OH, C1-6-alkilen-NH2,C1-6-alkilen-NH- C1-6-alkil iliC1-6-alkilen-N(C1-6-alkil)2;R15 je H ili C1-6-alkil; I je 0, 1, 2, 3 ili 4; m je 0, 1, 2, 3 ili 4; o je 0, 1 ili 2; p je 0, 1, 2, 3 ili 4; r je 0, 1, 2, 3 ili 4; s je 1 ili 2 it je 0 ili 1. Patent sadrži još 11 patentnih zahtjeva.

Claims (12)

1. Spoj prema formuli (I) [image] i enantiomeri, diastereomeri, tautomeri, solvati i njegove farmaceutski prihvatljive soli, naznačen time da R1 je -N(R10)-(C(R6)2)m-T -(C(R6)2)l-T ili -O-(C(R6)2)m-T; R6 je neovisno odabran između H, F, OH, OCH3, C1-6-alkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN, OH i OCH3 i C3-6-cikloalkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN, OH i OCH3; T je NR7R8, [image] [image] [image] [image] R7 i R8 neovisno su jedan od drugoga odabrani između H, C1-6-alkila, C2-6-alkenila, C2-6-alkinila i C2-6-alkilen-O- C1-6-alkila, pri čemu je svaki alkil, alkenil i alkinil po izboru supstituiran s jednim ili više atoma halogena, CN ili OH; R9 neovisno je odabran između halogena, CN, OH, C1-6-alkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN i OH i O- C1-6-alkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN i OH, C1-6-alkilen-O- C1-6-alkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN i OH ili NR12R13; R10 je H ili C1-6-alkil; R11 neovisno je odabran između halogena, CN, OH, C1-6-alkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN i OH, C2-6-alkenila, C2-6-alkinila, O- C1-6-alkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN i OH, C1-6-alkilen-O- C1-6-alkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN i OH, C0-6-alkil-C3-6-cikloalkila, -OC(O) C1-6-alkila, -NH2, -NH(C1-6-alkil) i -N(C1-6-alkil)2; R12 i R13 neovisno su jedan od drugoga odabrani između C1-6-alkila, koji je po izboru supstituiran s OH, C2-6-alkenila, C2-6-alkinila, C2-6-alkilen-O- C1-6alkila i C2-6-alkilen-N-(C1-6-alkil)2; W je CH, O ili NR10; X je CH ili N; Y je CH ili N; Z je CH ili N; A je 3-člani do 7-člani zasićeni, nezasićeni ili aromatski prsten koji sadržava 0-2 atoma dušika; B je CR2 ili N; G je CR2 ili N; D je CR2 ili N; E je CR2 ili N; pod uvjetom da jedna ili dvije od varijabli B, G, D i E mora biti N; R2 neovisno je odabran između H, F, Cl, CH3, OCH3 i CF3; R3 je H, Cl, F ili CH3; R4 je Cl, F ili CH3; R5 je [image] morfolin, po izboru supstituiran s 1 do 3 ista ili različita supstituenta R14, 4-članim do 7-članim, zasićenim ili djelomično zasićenim heterociklom koji u prstenu ima jedan atom dušika i po izboru još jedan heteroatom koji je odabran između O, N and S, pri čemu je heterocikl po izboru supstituiran s 1 do 4 ista ili različita supstituenta R11 ili NR12R13; R14 je C1-6-alkil, C1-6-alkilen-O- C1-6-alkil, C1-6-alkilen-OH, C1-6-alkilen-NH2, C1-6-alkilen-NH- C1-6-alkil ili C1-6-alkilen-N(C1-6-alkil)2; R15 je H ili C1-6-alkil; I je 0, 1, 2, 3 ili 4; m je 0, 1, 2, 3 ili 4; o je 0, 1 ili 2; p je 0, 1, 2, 3 ili 4; r je 0, 1, 2, 3 ili 4; s je 1 ili 2 i t je 0 ili 1.
2. Spoj prema 1. patentnom zahtjevu, naznačen time da R1 je -N(R10)-(C(R6)2)m-T -(C(R6)2)l-T ili -O-(C(R6)2)m-T; R6 neovisno je odabran između H, F, OH, OCH3, C1-6-alkila, koji je prema izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN, OH i OCH3 i C3-6-cikloalkila, koji je prema izboru supstituiran s 1 to 3 supstituenata odabranih između halogena, CN, OH i OCH3; T je NR7R8, morfolin, [image] [image] [image] R7 i R8 neovisno su jedan od drugoga odabrani između H, C1-6-alkila, C2-6-alkenila, C2-6-alkinila i C2-6-alkilen-O-C1-6-alkila, pri čemu je svaki alkil, alkenil i alkinil po izboru supstituiran s jednim ili s više atoma halogena, CN ili OH; R9 neovisno je odabran između halogena, CN, OH, C1-6-alkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN i OH i O- C1-6-alkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN i OH, C1-6-alkolen-O- C1-6-alkila, koji je po izboru supstituiran s 1 to 3 supstituenta odabranih između halogena, CN i OH; R10 je H ili C1-C6-alkil; R11 neovisno je odabran između halogena, CN, OH, C1-6-alkila, koji je po izboru supstituiran s 1 to 3 supstituenta odabranih između halogena, CN i OH, O- C1-6-alkila, koji je po izboru supstituiran s 1 to 3 supstituenta odabranih između halogena, CN i OH, C1-6-alkilen-O- C1-6-alkila, koji je po izboru supstituiran s 1 do 3 supstituenta odabranih između halogena, CN i OH, -NH2, -NH(C1-6-alkil) i -N(C1-6-alkil)2; X je CH ili N; Y je CH ili N; Z je CH ili N; A je 3-člani do 7-člani zasićeni, nezasićeni ili aromatski prsten koji sadržava 0-2 atoma dušika; B je CR2 ili N; G je CR2 ili N; D je CR2 ili N; E je CR2 ili N; pod uvjetom da jedna ili dvije od varijabli B, G, D i E moraju biti N; R2 neovisno je odabran između H, F, Cl, CH3, OCH3 i CF3; R3 je H, Cl, F ili CH3; R4 je Cl ili F; R5 je [image] morfolin, po izboru supstituiran s 1 do 3 ista ili različita supstituenta R14 ili NR12R13; R12 i R13 neovisno su jedan od drugoga odabrani između C1-6-alkila, C2-6-alkenila, C2-6-alkinila, C2-6-alkilen-O- C1-6-alkila i C2-6-alkilen-N-( C1-6-alkil)2; R14 je C1-6-alkil, C1-6-alkilen-O- C1-6-alkil, C1-6-alkilen-OH, C1-6-alkilen-NH2, C1-6-alkilen-NH- C1-6-alkil ili C1-6-alkilen-N(C1-6-alkil)2; I je 0, 1, 2, 3 ili 4; m je 0, 1, 2, 3 ili 4; o je 0, 1 ili 2; p je 0, 1, 2, 3 ili 4; q je 0, 1, 2 ili 3; r je 0, 1, 2, 3 ili 4 i s je 1 ili 2.
3. Spoj iz 1. ili iz 2. patentnog zahtjeva prema formuli (I’) [image] naznačen time da su B, G, D, E, R1, R3, R4 i R5 onakvi kako su definirani u 1. ili u 2. patentnom zahtjevu.
4. Spoj iz bilo kojeg patentnog zahtjeva od 1. do 3., naznačen time da je barem jedan od R7 i R8 odabran između C2-6-alkenila, C2-6-alkinila i C2-6-alkilen-O-C1-6-alkila.
5. Spoj iz bilo kojeg patentnog zahtjeva od 1. do 4., naznačen time da R2 je odabran između H, F, Cl i CH3.
6. Spoj iz bilo kojeg patentnog zahtjeva od 1. do 5., naznačen time da I je 2 ili 3 ili m je 2 ili 3.
7. Spoj iz bilo kojeg patentnog zahtjeva od 1. do 6. naznačen time da je kao lijek.
8. Spoj iz bilo kojeg patentnog zahtjeva od 1. do 6., naznačen time da je za liječenje ili za profilaksu kaheksije uzrokovane karcinomom, gubitka mišićne mase, anoreksije, amiotrofične lateralne skleroze (ALS), anksioznosti i/ili depresije.
9. Spoj iz bilo kojeg patentnog zahtjeva od 1. do 6., naznačen time da je za liječenje ili profilaksu pretilosti, diabetesa mellitusa, muške ili ženske seksualne disfunkcije i/ili erektilne disfunkcije.
10. Upotreba spoja iz bilo kojeg patentnog zahtjeva od 1. do 6., naznačena time da je za pripremu lijeka za liječenje ili za profilaksu kaheksije uzrokovane karcinomom, gubitka mišićne mase, anoreksije, amiotrofične lateralne skleroze (ALS), anksioznosti i/ili depresije.
11. Upotreba spoja iz bilo kojeg patentnog zahtjeva od 1. do 6., naznačena time da je za pripremu lijeka za liječenje ili za profilaksu pretilosti, diabetesa mellitusa, muške ili ženske seksualne disfunkcije i/ili erektilne disfunkcije.
12. Farmaceutski pripravak naznačen time da sadržava spoj iz bilo kojeg patentnog zahtjeva od 1. do 6. i farmaceutski prihvatljiv nosač.
HR20110860T 2007-07-19 2011-11-18 Supstituirani derivati heteroarilpiperidina kao modulatori receptora melanokortina-4 HRP20110860T1 (hr)

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EP07014219A EP2019100A1 (en) 2007-07-19 2007-07-19 Substituted heteroarylpiperidine derivatives as melanocortin-4 receptor modulators
PCT/EP2008/005913 WO2009010299A1 (en) 2007-07-19 2008-07-18 Substituted heteroarylpiperidine derivatives as melanocortin-4 receptor modulators

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