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HRP20151336T1 - Tetrahidroizokinolin-1-on derivat ili njegova sol - Google Patents

Tetrahidroizokinolin-1-on derivat ili njegova sol Download PDF

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HRP20151336T1
HRP20151336T1 HRP20151336TT HRP20151336T HRP20151336T1 HR P20151336 T1 HRP20151336 T1 HR P20151336T1 HR P20151336T T HRP20151336T T HR P20151336TT HR P20151336 T HRP20151336 T HR P20151336T HR P20151336 T1 HRP20151336 T1 HR P20151336T1
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Croatia
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alkylene
alkyl
group
halogen
aryl
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HRP20151336TT
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Hiroyuki Hisamichi
Itsuro Shimada
Tsukasa Ishihara
Tomofumi Takuwa
Takafumi Shimizu
Noriko Ishikawa
Kyoichi Maeno
Norio Seki
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Seldar Pharma Inc.
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Claims (12)

1. Derivat tetrahidroizokinolin-1-ona predstavljen formulom (I) ili njegova farmaceutski prikladna sol: [image] gdje simboli u formuli imaju sljedeća značenja: R1: (C1-6 alkilen koji može biti supstituiran skupinom izabranom iz grupe koju čini fenil koji može biti supstituiran s halogenom, C1-6 alkilom ili -OR0, i -OH)-OH, ili cikloalkil supstituiran skupinom izabranom iz grupe koju čine -OR0, - N(R0)2, -N(R0)C(O)R0, -N(R0)C(O)-C1-6 alkilen-OR0, -N(R0)S(O)2-C1-6 alkil, i heterociklička skupina, R0: međusobno jednaki ili različiti, svaki predstavlja -H ili C1-6 alkil, R2: fenil koji može biti supstituiran s halogenom ili -OR0, R3: -H, R4: -N(R0)-O-C1-6alkilen-(aril ili heteroaril, od kojih svaki može biti supstituiran skupinom izabranom iz grupe G6), Grupa G6: halogen, C1-6 alkil koji može biti supstituiran s -OR0, halogen-C1-6 alkil koji može biti supstituiran s -OR0, -CN, -N(R0)2, -CO2R0, -CO2-C1-6 alkilen-aril, -C(O)N(R0)2, C1-6 alkilen-OC(O)R0, C1-6 alkilen-OC(O)aril, C1-6 alkilen-CO2R0, halogen-C1-6 alkilen-CO2R0, C1-6 alkilen-CO2-C1-6 alkilen-aril, C1-6alkilen-C(O)N(R0)2, halogen-C1-6 alkilen-C(O)N(R0)2, -O-C1-6 alkilen-CO2R0, -O-C1-6 alkilen-CO2-C1-6 alkilen-aril, -O-C1-6 alkilen-C(O)N(R0)2, -O-halogen-C1-6 alkilen-CO2R0, -O-halogen-C1-6 alkilen-C(O)N(R0)2, -C(O)N(R0)S(O)2-C1-6 alkil, C1-6 alkilen-C(O)N(R0)S(O)2-C1-6 alkil, -S(O)2-C1-6 alkil, -S(O)2N(R0)2, heterociklička skupina, -C(=NH)NH2, -C(-NH)=NO-C(O)O-C1-10 alkil, -C(=NOH)NH2, -C(O)N=C(N(R0)2)2, -N(R0)C(O)R0, -N(R0)C(O)-C1-6 alkilen-OR0, -N(R0)C(O)OR0, -N(R0)S(O)2-C1-6 alkil, -C(aril)3, i okso, gdje "aril" i "heterociklička skupina" u Grupi G6 svaki može biti supstituiran skupinom izabranom iz grupe koju čine halogen, C1-6 alkil, halogen-C1-6 alkil, -OR0, -O-halogen-C1-6 alkil, okso, i tiokso (=S), m: cijeli broj od 0 do 3, i R5: C1-6 alkil, halogen-C1-6 alkil, halogen, nitro, -OR0, -O-halogen-C1-6 alkil, -N(R0)2, -O-C1-6 alkilen-CO2R0, ili -O-C1-6 alkilen-aril, gdje aril u R5 može biti supstituiran skupinom izabranom iz grupe koju čine halogen, C1-6 alkil, halogen-C1-6 alkil, -OR0 i -O-halogen-C1-6 alkil.
2. Spoj kako je opisan prema zahtjevu 1, gdje R4 jest -NH-O-C1-6alkilen-(fenil, piridil, N-oksidopiridil, tienil, ili tiazolil, od kojih svaki može biti supstituiran skupinom izabranom iz grupe koju čine halogen, -OR0, C1-6 alkilen-OR0, -CO2R0, C1-6 alkilen-CO2R0, i -OC1-6 alkilen-CO2R0).
3. Spoj kako je opisan prema zahtjevu 2, gdje je R1 cikloalkil supstituiran skupinom izabranom iz grupe koju čine -OR0, -N(R0)2, -N(R0)C(O)R0, -N(R0)C(O)-C1-6alkilen-OR0, -N(R0)S(O)2-C1-6 alkil, i heterociklička skupina.
4. Spoj kako je opisan prema zahtjevu 3, gdje m je jednako 0.
5. Spoj kako je opisan prema zahtjevu 4, gdje je R1 cikloheksil supstituiran skupinom izabranom iz grupe koju čine -OR0, -N(R0)C(O)R0 i -N(R0)S(O)2-C1-6 alkil.
6. Spoj kako je opisan prema zahtjevu 1, a koji se izabire iz grupe koju čine: (3R,4R)-3-(2,4-diklorofenil)-2-{(1S,2S)-2-[(metilsulfonil)amino]-cikloheksil}-1-okso-N-(piridin-2-ilmetoksi)-1,2,3,4-tetrahidroizokinolin-4-karboksamid, (3R,4R)-3-(2,4-diklorofenil)-2-{(1S,2S)-2-[(metilsulfonil)amino]-cikloheksil}-N-[(1-oksidopiridin-2-il)metoksi]-1-okso-1,2,3,4-tetrahidroizokinolin-4-karboksamid, 3-{[({[(3R,4R)-3-(2,4-diklorofenil)-2-{(1S,2S)-2-[(metilsulfonil)-amino]cikloheksil}-1-okso-1,2,3,4-tetrahidroizokinolin-4-il]karbonil}amino)-oksi]metil}benzojeva kiselina, (4-{[({[(3R,4R)-3-(2,4-diklorofenil)-2-{(1S,2S)-2-[(metilsulfonil)-amino]-cikloheksil}-1-okso-1,2,3,4-tetrahidroizokinolin-4-il]karbonil}amino)-oksi]metil}fenil)octena kiselina, (3-{[({[(3R,4R)-3-(2,4-diklorofenil-2-{(1S,2S)-2-[(metilsulfonil)-amino]cikloheksil}-1-okso-1,2,3,4-tetrahidroizokinolin-4-il]karbonil}amino)-oksi]metil}fenoksi)octena kiselina, {3-[2-({[(3R,4R)-3-(2,4-diklorofenil)-2-{(1S,2S)-2-[(metilsulfonil)amino]-cikloheksil}-1-okso-1,2,3,4-tetrahidroizokinolin-4-il]karbonil}amino)-etil]fenil}(difluoro)octena kiselina, (3R,4R)-3-(2,4-diklorofenil)-2-{(1S,2S)-2-[(metilsulfonil)amino]-cikloheksil}-N-(2-{3-[(metilsulfonil)karbamoil]fenil}etil)-1-okso-1,2,3,4-tetrahidroizokinolin-4-karboksamid, {4-[2-({[(3R,4R)-3-(2,4-diklorofenil)-2-{(1S,2S)-2-[(metilsulfonil)amino]-cikloheksil}-1-okso-1,2,3,4-tetrahidroizokinolin-4-il]karbonil}amino)-etil]fenil}octena kiselina, i 4-(3-{[({[(3R,4R)-3-(2,4-diklorofenil)-2-{(18,28)-2-[(metilsulfonil)amino]-cikloheksil}-1-okso-1,2,3,4-tetrahidroizokinolin-4-il]karbonil}amino)-oksi]metil}fenoksi)butan kiselina; ili njegova farmaceutski prikladna sol.
7. Farmaceutski pripravak koji sadrži spoj kako je opisan prema bilo kojem od zahtjeva 1 do 6 ili njegovu farmaceutski prikladnu sol, i farmaceutski prikladan nosač.
8. Farmaceutski pripravak koji sadrži derivat tetrahidroizokinolin-1-ona predstavljen formulom (I’) ili njegovu farmaceutski prikladnu sol, i farmaceutski prikladan nosač: [image] gdje simboli u formuli imaju sljedeća značenja: R1: (C1-6 alkilen koji može biti supstituiran skupinom izabranom iz grupe G1)-OH, cikloalkil koji može biti supstituiran skupinom izabranom iz grupe G2, ili heterociklička skupina koja može biti supstituirana skupinom izabranom iz grupe G2, Grupa G1: halogen, -OR0, -N(R0)(R6), i aril, gdje "aril" u Grupi G1 može biti supstituiran skupinom izabranom iz grupe koju čine halogen, C1-6 alkil, halogen-C1-6 alkil, -OR0, i -O-halogen-C1-6 alkil, Grupa G2: halogen, C1-6 alkil, halogen-C1-6 alkil, C1-6 alkilen-OR0,-OR0, -O-halogen-C1-6 alkil, -N(R0)2, -N(R0)-C1-6 alkilen-OR0, -N(R0)-C1-6 alkilen-CO2R0, -N(R0)C(O)R0, -N(R0)C(O)OR0, -N(R0)C(O)-aril, -N(R0)C(O)-C1-6 alkilen-OR0, -N(R0)C(O)-C1-6 alkilen-N(R0)2, -N(R0)C(O)N(R0)2, -N(R0)C(=NR0)-C1-6 alkil, -N(R0)S(O)2-C1-6 alkil, -N(C1-6 alkilen-OR0)-S(O)2-C1-6 alkil, -N(C1-6 alkilen-CO2R0)-S(O)2-C1-6 alkil, -N(R0)S(O)2-C1-6 alkilen-CO2R0, -N(R0)S(O)2-C1-6 alkilen-S(O)2-C1-6 alkil, -N(R0)S(O)2-aril, -N(R0)S(O)2N(R0)2, -S(O)2-C1-6 alkil, -CO2R0, -CO2-C1-6 alkilen-Si(C1-6 alkil)3, -C(O)N(R0)2, -C(O)N(R0)-C1-6 alkilen-OR0, -C(O)N(R0)-C1-6 alkilen-N(R0)2, -C(O)N(R0)-C1-6 alkilen-CO2R0, -C(O)N(R0)-O-C1-6 alkilen-heterociklička skupina, heterociklička skupina, -C(O)R0, -C(O)-C1-6 alkilen-OR0, - C(O)-C1-6 alkilen-N(R0)2, -C(O)-heterociklička skupina, i okso, gdje "aril" i "heterociklička skupina" u Grupi G2 svaki može biti supstituiran skupinom izabranom iz grupe koju čine halogen, C1-6 alkil, halogen-C1-6 alkil, -OR0, -O-halogen-C1-6 alkil, i okso; R0: međusobno jednaki ili različiti, svaki predstavlja -H ili C1-6 alkil, R2: fenil koji može biti supstituiran s halogenom, C1-6 alkilom ili -OR0, R3: -H, R4: -N(R0)-O-C1-6 alkilen-(aril ili heteroaril, od kojih svaki može biti supstituiran skupinom izabranom iz grupe G6), Grupa G6: halogen, C1-6 alkil koji može biti supstituiran s -OR0, halogen-C1-6 alkil koji može biti supstituiran s -OR0, -CN, -N(R0)2, -CO2R0, -CO2-C1-6 alkilen-aril, -C(O)N(R0)2, C1-6 alkilen-OC(O)R0, C1-6 alkilen-OC(O)aril, C1-6 alkilen-CO2R0, halogen-C1-6 alkilen-CO2R0, C1-6 alkilen-CO2-C1-6 alkilen-aril, C1-6alkilen-C(O)N(R0)2, halogen-C1-6 alkilen-C(O)N(R0)2, -O-C1-6 alkilen-CO2R0, -O-C1-6 alkilen-CO2-C1-6 alkilen-aril, -O-C1-6 alkilen-C(O)N(R0)2, -O-halogen-C1-6 alkilen-CO2R0, -O-halogen-C1-6 alkilen-C(O)N(R0)2, -C(O)N(R0)S(O)2-C1-6 alkil, C1-6 alkilen-C(O)N(R0)S(O)2-C1-6 alkil, -S(O)2-C1-6 alkil, -S(O)2N(R0)2, heterociklička skupina, -C(=NH)NH2, -C(-NH)=NO-C(O)O-C1-10 alkil, -C(=NOH)NH2, -C(O)N=C(N(R0)2)2, -N(R0)C(O)R0, -N(R0)C(O)-C1-6alkilen-OR0, -N(R0)C(O)OR0, -N(R0)S(O)2-C1-6 alkil, -C(aril)3, i okso, gdje "aril" i "heterociklička skupina" u Grupi G6 svaki može biti supstituiran skupinom izabranom iz grupe koju čine halogen, C1-6 alkil, halogen-C1-6 alkil, -OR0, -O-halogen-C1-6 alkil, okso, i tiokso (=S), m: cijeli broj od 0 do 3, R5: C1-6 alkil, halogen-C1-6 alkil, halogen, nitro, -OR0, -O-halogen-C1-6 alkil, -N(R0)2, -O-C-1-6 alkilen-CO2R0, ili -O-C1-6 alkilen-aril, gdje aril u R5 može biti supstituiran skupinom izabranom iz grupe koju čine halogen, C1-6 alkil, halogen-C1-6 alkil, -OR0 i -O-halogen-C1-6 alkil, i R6: R0, -C(O)-R0, -CO2-C1-6 alkil ili -S(O)2-C1-6 alkil.
9. Uporaba spoja predstavljenog formulom (I’) prema zahtjevu 8 ili njegova farmaceutski prikladna sol za proizvodnju terapijskog sredstva za sindrom iritabilnog crijeva.
10. Uporaba spoja kako je opisan prema zahtjevu 1 ili njegove farmaceutski prikladne soli za proizvodnju terapijskog sredstva za rak.
11. Spoj predstavljen formulom (I’) prema zahtjevu 8 ili njegova sol za uporabu u liječenju sindroma iritabilnog crijeva.
12. Spoj kako je opisan prema zahtjevu 1 ili njegova sol za uporabu u liječenju raka.
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