DK2604595T3 - Triazinderivat og farmaceutisk forbindelse, der indeholder dette og fremviser analgetisk aktivitet - Google Patents

Triazinderivat og farmaceutisk forbindelse, der indeholder dette og fremviser analgetisk aktivitet Download PDF

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DK2604595T3
DK2604595T3 DK11816413.6T DK11816413T DK2604595T3 DK 2604595 T3 DK2604595 T3 DK 2604595T3 DK 11816413 T DK11816413 T DK 11816413T DK 2604595 T3 DK2604595 T3 DK 2604595T3
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substituted
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ring
alkyl
mmol
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Akira Iida
Sae Jikihara
Tsuyoshi Hasegawa
Miho Oohara
Yukio Tada
Toshikatsu Maki
Hiroyuki Kai
Takayuki Kameyama
Tohru Horiguchi
Kentaro Asahi
Takeshi Endoh
Yasuhiko Fujii
Takuya Shintani
Ken Ichiroh Nakamura
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Shionogi & Co
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Claims (29)

1. Forbindelse med formel (VIII): [Kemisk funnel 1]
(VIII) hvor Z1 og Z2 hver for sig er et oxygenatom, et svovlatom eller =N-Rx; Rx er et hydrogenatom, substitueret eller usubstitueret alkyl, substitueret eller usubstitueret alkenyl, substitueret eller usubstitueret alkynyl, substitueret eller usubstitueret cycloalkyl, substitueret eller usubstitueret cycloalkenyl, en substitueret eller usubstitueret ikke-aromatisk heterocyklisk gruppe, substitueret eller usubstitueret aryl eller substitueret eller usubstitueret heteroaryl; Rc er et hydrogenatom, substitueret eller usubstitueret alkyl, substitueret eller usubstitueret alkenyl, substitueret eller usubstitueret alkynyl, substitueret eller usubstitueret acyl, substitueret eller usubstitueret cycloalkyl, substitueret eller usubstitueret cycloalkenyl, en substitueret eller usubstitueret ikke-aromatisk heterocyklisk gruppe, substitueret eller usubstitueret aryl eller substitueret eller usubstitueret heteroaryl; R4a og R4b hver for sig er et hydrogenatom eller substitueret eller usubstitueret alkyl, eller R4a og R4b, der er bundet til det samme carbonatom, sammen danner oxo eller thioxo; n er et helt tal fra 1 til 4; R2 er substitueret eller usubstitueret cycloalkyl, substitueret eller usubstitueret cycloalkenyl, en substitueret eller usubstitueret ikke-aromatisk heterocyklisk gruppe, substitueret eller usubstitueret aryl eller substitueret eller usubstitueret heteroaryl; -X- er -0-, -S-, -N(R5)- eller -(CR5aR5b)-; -L- er -0-, -S-, -N(R5')- eller - (CR5a'-R5b') -; R5 og R5' hver for sig er et hydrogenatom, substitueret eller usubstitueret alkyl, substitueret eller usubstitueret alkenyl, substitueret eller usubstitueret alkynyl eller substitueret eller usubstitueret acyl; R5a, R5b, R5a' og R5b' hver for sig er et hydrogenatom, halogen, hydroxy, substitueret eller usubstitueret alkyl, substitueret eller usubstitueret alkenyl, substitueret eller usubstitueret alkynyl, substitueret eller usubstitueret alkyloxy, substitueret eller usubstitueret alkynyloxy eller substitueret eller usubstitueret alkenyloxy; ring D er en benzenring, en pyridinring, en pyrimidinring, en pyrazinring eller en pyridazinring; carbonatom a og carbonatom b er carbonatomer, der udgør ring D; ring B er en aromatisk heterocyklisk ring; s og s' hver for sig er et helt tal fra 0 til 3; og R9 og R9' hver for sig er halogen, hydroxy, carboxy, cyano, nitro, substitueret eller usubstitueret alkyl, substitueret eller usubstitueret alkenyl, substitueret eller usubstitueret alkynyl, substitueret eller usubstitueret alkyloxy, substitueret eller usubstitueret alkenyloxy, substitueret eller usubstitueret alkynyloxy, substitueret eller usubstitueret alkylthio, substitueret eller usubstitueret alkenylthio, substitueret eller usubstitueret alkynylthio, substitueret eller usubstitueret acyl, substitueret eller usubstitueret alkyloxycarbonyl, substitueret eller usubstitueret alkenyloxycarbonyl, substitueret eller usubstitueret alkynyloxycarbonyl, substitueret eller usubstitueret carbamoyl, substitueret eller usubstitueret amino, substitueret eller usubstitueret sulfamoyl, substitueret sulfonyl, substitueret sulfinyl, substitueret eller usubstitueret cycloalkyl, substitueret eller usubstitueret cycloalkenyl, en substitueret eller usubstitueret ikke-aromatisk heterocyklisk gruppe, substitueret eller usubstitueret aryl, substitueret eller usubstitueret heteroaryl, substitueret eller usubstitueret cycloalkyloxy, substitueret eller usubstitueret cycloalkenyloxy, substitueret eller usubstitueret ikke- aromatisk heterocyclyloxy, substitueret eller usubstitueret aryloxy eller substitueret eller usubstitueret heteroaryloxy; eller dens farmaceutisk acceptable salt eller et solvat deraf, hvor tilladte substituenter for "substitueret alkyl", "substitueret alkenyl", "substitueret alkynyl", "substitueret alkyloxy", "substitueret alkenyloxy", "substitueret alkynyloxy", "substitueret alkylthio", "substitueret alkenylthio", "substitueret alkynylthio", "substitueret alkyloxycarbonyl", "substitueret alkenyloxycarbonyl" og "substitueret alkynyloxycarbonyl" inkluderer en eller flere, ens eller forskellige substituenter udvalgt fra gruppen, der består af: hydroxy, carboxy, halogen, haloalkyloxy, cycloalkyl, cycloalkenyl, methoxy, ethoxy, propoxy, butoxy, alkenyloxy, alkyloxycarbonyl, nitro, nitroso, amino, alkylamino, acylamino, arylalkylamino, hydroxyamino, alkylsulfonylamino, alkylsulfinylamino, imino, hydroxyimino, alkylimino, alkyloxyimino, acylimino, azido, aryl, arylalkyl, arylalkyloxy, en ikke-aromatisk heterocyklisk gruppe, heteroaryl, heteroarylalkyl, cyano, isocyano, isocyanato, thiocyanato, isothiocyanato, mercapto, alkylthio, alkylsulfonyl, carbamoyl, alkylcarbamoyl, sulfamoyl, alkylsulfamoyl, acyl, formyloxy, thioformyl, thiocarboxy, dithiocarboxy, thiocarbamoyl, sulfino, sulfo, hydrazino, azido, ureido, amidino, guanidino, phthalimido, tri-alkylsilyl og oxo, substituenter for "substitueret acyl" er udvalgt blandt substituenterne, der er defineret ovenfor for "substitueret alkyl", en lige eller forgrenet kæde monovalent carbonhydridgruppe med et carbonantal på 1 til 15, en lineær eller forgrenet alkenyl med et carbonantal på 2 til 15 og en lineær eller forgrenet alkynyl med et carbonantal på 2 til 15, hvis R i acyl (R-C(=0)-) er cycloalkyl, cycloalkenyl, en ikke-aromatisk heterocyklisk gruppe, aryl eller heteroaryl, så kan hver ring være substitueret med alkyl, haloalkyl, alkenyl, alkynyl, alkyloxy, halogen, substituenter for "substitueret carbamoyl" og "substitueret sulfamoyl" er en eller flere, ens eller forskellige grupper udvalgt fra gruppen, der består af: hydroxy, carboxy, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkyloxycarbonyl, amino, alkylamino, acylamino, arylalkylamino, hydroxyamino, aryl, cyano, isocyano, isocyanato, thiocyanato, isothiocyanato og acyl, substituenter for "substitueret amino" er en eller flere, ens eller forskellige grupper udvalgt fra gruppen, der består af: alkyl, haloalkyl, hydroxyalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkyloxy, haloalkyloxy, alkenyloxy, alkyloxycarbonyl, alkyloxycarbonylalkyl, amino, alkylamino, acylamino, arylalkylamino, hydroxyamino, imino, hydroxyimino, alkylimino, alkyloxyimino, acylimino, aryl, arylalkyl, aryloxy, en ikke-aromatisk heterocyklisk gruppe, heteroaryl, heteroarylalkyl, ikke-aromatisk heterocyclyloxy, heteroaryloxy, hydroxy, halogen, cyano, acyl, alkylsulfonyl, alkylsulfinyl, carbamoyl, alkylcarbamoyl, alkylcarbamoylalkyl, carbamoylalkyl, carboxyalkyl, sulfamoyl, alkylsulfamoyl, alkylsulfamoylalkyl og sulfamoylalkyl, substituenter for "substitueret cycloalkyl", "substitueret cycloalkenyl", "substitueret aryl", "substitueret heteroaryl" og "en substitueret ikke-aromatisk heterocyklisk gruppe" er en eller flere, ens eller forskellige grupper udvalgt fra gruppen, der består af: alkyl, haloalkyl, haloalkyloxy, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkyloxy, alkenyloxy, alkyloxycarbonyl, nitro, nitroso, amino, alkylamino, acylamino, arylalkylamino, hydroxyamino, amino, der er substitueret med en eller to, ens eller forskellige substituenter udvalgt fra nedennævnte substituentgruppe Y, imino, hydroxyimino, alkylimino, alkyloxyimino, acylimino, azido, aryl, arylalkyl, usubstitueret ikke-aromatisk carbocyclyloxy, ikke-aromatisk carbocyclyloxy, der er substitueret med en eller flere, ens eller forskellige substituenter udvalgt fra nedennævnte substituentgruppe Z, usubstitueret ikke-aromatisk carbocyclylalkyloxy, ikke-aromatisk carbocyclylalkyloxy, der er substitueret med en eller flere, ens eller forskellige substituenter udvalgt fra nedennævnte substituentgruppe Z, usubstitueret aryloxy, aryloxy, der er substitueret med en eller flere, ens eller forskellige substituenter udvalgt fra nedennævnte substituentgruppe Z, usubstitueret arylalkyloxy, arylalkyloxy, der er substitueret med en eller flere, ens eller forskellige substituenter udvalgt fra nedennævnte substituentgruppe Z, en ikke-aromatisk heterocyklisk gruppe, heteroaryl, heteroarylalkyl, usubstitueret ikke-aromatisk heterocyclyloxy, ikke-aromatisk heterocyclyloxy, der er substitueret med en eller flere, ens eller forskellige substituenter udvalgt fra nedennævnte substituentgruppe Z, usubstitueret heteroaryloxy, heteroaryloxy, der er substitueret med en eller flere, ens eller forskellige substituenter udvalgt fra nedennævnte substituentgruppe Z, cyano, isocyano, isocyanato, thiocyanato, isothiocyanato, mercapto, alkylthio, alkylsulfonyl, substitueret eller usubstitueret carbamoyl, substitueret eller usubstitueret alkylcarbamoyl, sulfamoyl, alkylsulfamoyl, hydroxy, carboxy, halogen, acyl, formyloxy, thioformyl, thiocarboxy, dithiocarboxy, thiocarbamoyl, sulfino, sulfo, hydrazino, azido, ureido, amidino, guanidino, phthalimido og oxo, substituentgruppe Y inkluderer hydroxy alkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, alkylsulfonyl, alkylsulfinyl, carbamoyl, alkylcarbamoyl, alkylcarbamoylalkyl, carbamoylalkyl, carboxyalkyl, sulfamoyl, alkylsulfamoyl, alkylsulfamoylalkyl og sulfamoylalkyl, substituentgruppe Z inkluderer halogen, hydroxy, carboxy, cyano, nitro, alkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, alkenyl, alkynyl, alkyloxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, acyl, alkyloxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, carbamoyl, alkylcarbamoyl, haloalkylcarbamoyl, hydroxyalkylcarbamoyl, cyanocarbamoyl, amino, acylamino, amino, der er substitueret med en eller to, ens eller forskellige substituenter udvalgt fra ovennævnte substituentgruppe Y, sulfamoyl, methylsulfonyl, methylsulfinyl, cycloalkyl, cycloalkenyl, en ikke-aromatisk heterocyklisk gruppe, aryl, heteroaryl, cycloalkyloxy, cycloalkenyloxy, ikke-aromatisk heterocyclyloxy, aryloxy og heteroaryloxy.
2. Forbindelse ifølge krav 1, hvor -L- er -0-, eller dens farmaceutisk acceptable salt eller et solvat deraf.
3. Forbindelse ifølge et hvilket som helst af kravene 1 til 2, hvor ring B er en thiazolring, en isothiazolring, en oxazolring, en isoxazolring, en pyrazolring, en imidazolring, en triazolring, en furanring, en thiophenring, en thiadiazolring, en oxadiazolring, en pyridinring, en pyrimidinring, en pyrazinring, en pyridazinring, en triazinring eller en benzoxazolring, eller dens farmaceutisk acceptable salt eller et solvat deraf.
4. Forbindelse ifølge et hvilket som helst af kravene 1 til 3, hvor ring B er en thiazolring, en isothiazolring, en oxazolring, en isoxazolring, en thiadiazolring, en oxadiazolring, en pyridinring, en pyrimidinring, en pyrazinring eller en pyridazinring, eller dens farmaceutisk acceptable salt eller et solvat deraf.
5. Forbindelse ifølge et hvilket som helst af kravene 1 til 4, hvor s' er et helt tal fra 1 til 2, og mindst én af R9' er hydroxy, carboxy, cyano, substitueret alkyl, substitueret eller usubstitueret carbamoyl, substitueret eller usubstitueret amino, substitueret eller usubstitueret sulfamoyl, substitueret sulfonyl eller substitueret sulfinyl, eller dens farmaceutisk acceptable salt eller et solvat deraf, hvor substituenter for "substitueret sulfonyl" eller "substitueret sulfinyl" er udvalgt blandt den "substituerede eller usubstituerede alkyl" ifølge krav 1, den "substituerede eller usubstituerede alkenyl" ifølge krav 1, den "substituerede eller usubstituerede alkynyl" ifølge krav 1, den "substituerede eller usubstituerede cycloalkyl" ifølge krav 1, den "substituerede eller usubstituerede cycloalkenyl" ifølge krav 1, den "substituerede eller usubstituerede ikke- aromatiske heterocykliske gruppe" ifølge krav 1, den "substituerede eller usubstituerede aryl" ifølge krav 1 og den "substituerede eller usubstituerede heteroaryl" ifølge krav 1, hvis R i R-S(=0)2- eller R-S(=0)- er cycloalkyl, cycloalkenyl, en ikke-aromatisk heterocyklisk gruppe, aryl, heteroaryl, så kan hver ring være substitueret med alkyl, haloalkyl, alkenyl, alkynyl, alkyloxy, halogen.
6. Forbindelse ifølge et hvilket som helst af kravene 1 til 5, hvor s' er 1, og R9' er carboxy eller substitueret eller usubstitueret carbamoyl, eller dens farmaceutisk acceptable salt eller et solvat deraf.
7. Forbindelse ifølge et hvilket som helst af kravene 1 til 6, hvor ring D er en benzenring, eller dens farmaceutisk acceptable salt eller et solvat deraf.
8. Forbindelse ifølge et hvilket som helst af kravene 1 til 7, hvor carbonatom a er placeret på ring D i et 1,4-position i forhold til carbonatom b, eller dens farmaceutisk acceptable salt eller et solvat deraf.
9. Forbindelse ifølge et hvilket som helst af kravene 1 til 8, hvor s og s' hver for sig er et helt tal fra 0 til 2; og R9 og R9' hver for sig er halogen, hydroxy, carboxy, cyano, nitro, substitueret eller usubstitueret alkyl, substitueret eller usubstitueret alkenyl, substitueret eller usubstitueret alkynyl, substitueret eller usubstitueret alkyloxy, substitueret eller usubstitueret alkenyloxy, substitueret eller usubstitueret alkynyloxy, substitueret eller usubstitueret alkylthio, substitueret eller usubstitueret alkenylthio, substitueret eller usubstitueret alkynylthio, substitueret eller usubstitueret acyl, substitueret eller usubstitueret alkyloxycarbonyl, substitueret eller usubstitueret alkenyloxycarbonyl, substitueret eller usubstitueret alkynyloxycarbonyl, substitueret eller usubstitueret carbamoyl, substitueret eller usubstitueret amino, substitueret eller usubstitueret sulfamoyl, substitueret sulfonyl eller substitueret sulfinyl, eller dens farmaceutisk acceptable salt eller et solvat deraf.
10. Forbindelse ifølge et hvilket som helst af kravene 1 til 9, hvor Z1 og Z2 begge er oxygenatomer eller begge er svovlatomer, eller dens farmaceutisk acceptable salt eller et solvat deraf.
11. Forbindelse ifølge et hvilket som helst af kravene 1 til 10, hvor Z1 og Z2 begge er oxygenatomer, eller dens farmaceutisk acceptable salt eller et solvat deraf.
12. Forbindelse ifølge et hvilket som helst af kravene 1 til 11, hvor R° er usubstitueret alkyl, alkyl, der er substitueret med en eller flere substituenter udvalgt fra substituentgruppe A (substituentgruppe A: halogen, cyano, hydroxy, carboxy, sulfo, substitueret eller usubstitueret alkyloxy, substitueret eller usubstitueret alkenyloxy, substitueret eller usubstitueret alkynyloxy, substitueret eller usubstitueret cycloalkyl, substitueret eller usubstitueret cycloalkenyl, en substitueret eller usubstitueret ikke-aromatisk heterocyklisk gruppe, substitueret eller usubstitueret aryl, substitueret eller usubstitueret heteroaryl, substitueret eller usubstitueret alkyloxycarbonyl, substitueret eller usubstitueret alkenyloxycarbonyl, substitueret eller usubstitueret alkynyloxycarbonyl, substitueret eller usubstitueret carbamoyl, substitueret eller usubstitueret sulfamoyl, substitueret eller usubstitueret amino, substitueret eller usubstitueret imino, substitueret eller usubstitueret guanidyl, substitueret eller usubstitueret alkylthio, substitueret eller usubstitueret alkenylthio, substitueret eller usubstitueret alkynylthio, substitueret eller usubstitueret acyl, substitueret eller usubstitueret cycloalkyloxycarbonyl, substitueret eller usubstitueret cycloalkenyloxycarbonyl, substitueret eller usubstitueret ikke-aromatisk heterocyclyloxycarbonyl, substitueret eller usubstitueret aryloxycarbonyl, substitueret eller usubstitueret heteroaryloxycarbonyl, nitro, oxo og thioxo), usubstitueret alkenyl, alkenyl, der er substitueret med en eller flere substituenter udvalgt fra substituentgruppe A, usubstitueret alkynyl eller alkynyl, der er substitueret med en eller flere substituenter udvalgt fra substituentgruppe A, eller dens farmaceutisk acceptable salt eller et solvat deraf, hvor substituenter for "substitueret imino" er en eller flere, ens eller forskellige grupper udvalgt fra gruppen, der består af: alkyl, haloalkyl, hydroxyalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkyloxy, haloalkyloxy, alkenyloxy, alkyloxycarbonyl, alkyloxycarbonylalkyl, amino, alkylamino, acylamino, arylalkylamino, hydroxyamino, imino, hydroxyimino, alkylimino, alkyloxyimino, acylimino, aryl, arylalkyl, aryloxy, en ikke-aromatisk heterocyklisk gruppe, heteroaryl, heteroarylalkyl, ikke-aromatisk heterocyclyloxy, heteroaryloxy, hydroxy, halogen, cyano, acyl, alkylsulfonyl, alkylsulfinyl, carbamoyl, alkylcarbamoyl, alkylcarbamoylalkyl, carbamoylalkyl, carboxyalkyl, sulfamoyl, alkylsulfamoyl, alkylsulfamoylalkyl og sulfamoylalkyl, substituenter for "substitueret cycloalkyloxycarbonyl", "substitueret cycloalkenyloxycarbonyl", "substitueret ikke-aromatisk heterocyclyloxycarbonyl", "substitueret aryloxycarbonyl" og "substitueret heteroaryloxycarbonyl" er en eller flere, ens eller forskellige grupper udvalgt fra gruppen, der består af: alkyl, haloalkyl, haloalkyloxy, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkyloxy, alkenyloxy, alkyloxycarbonyl, nitro, nitroso, amino, alkylamino, acylamino, arylalkylamino, hydroxyamino, amino, der er substitueret med en eller to, ens eller forskellige substituenter udvalgt fra nedennævnte substituentgruppe Y, imino, hydroxyimino, alkylimino, alkyloxyimino, acylimino, azido, aryl, arylalkyl, usubstitueret ikke-aromatisk carbocyclyloxy, ikke-aromatisk carbocyclyloxy, der er substitueret med en eller flere, ens eller forskellige substituenter udvalgt fra nedennævnte substituentgruppe Z, usubstitueret ikke-aromatisk carbocyclylalkyloxy, ikke-aromatisk carbocyclylalkyloxy, der er substitueret med en eller flere, ens eller forskellige substituenter udvalgt fra nedennævnte substituentgruppe Z, usubstitueret aryloxy, aryloxy, der er substitueret med en eller flere, ens eller forskellige substituenter udvalgt fra nedennævnte substituentgruppe Z, usubstitueret arylalkyloxy, arylalkyloxy, der er substitueret med en eller flere, ens eller forskellige substituenter udvalgt fra nedennævnte substituentgruppe Z, en ikke-aromatisk heterocyklisk gruppe, heteroaryl, heteroarylalkyl, usubstitueret ikke-aromatisk heterocyclyloxy, ikke-aromatisk heterocyclyloxy, der er substitueret med en eller flere, ens eller forskellige substituenter udvalgt fra nedennævnte substituentgruppe Z, usubstitueret heteroaryloxy, heteroaryloxy, der er substitueret med en eller flere, ens eller forskellige substituenter udvalgt fra nedennævnte substituentgruppe Z, cyano, isocyano, isocyanato, thiocyanato, isothiocyanato, mercapto, alkylthio, alkylsulfonyl, substitueret eller usubstitueret carbamoyl, substitueret eller usubstitueret alkylcarbamoyl, sulfamoyl, alkylsulfamoyl, hydroxy, carboxy, halogen, acyl, formyloxy, thioformyl, thiocarboxy, dithiocarboxy, thiocarbamoyl, sulfino, sulfo, hydrazino, azido, ureido, amidino, guanidino, phthalimido og oxo, substituentgruppe Y inkluderer hydroxy alkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, alkylsulfonyl, alkylsulfinyl, carbamoyl, alkylcarbamoyl, alkylcarbamoylalkyl, carbamoylalkyl, carboxyalkyl, sulfamoyl, alkylsulfamoyl, alkylsulfamoylalkyl og sulfamoylalkyl, substituentgruppe Z inkluderer halogen, hydroxy, carboxy, cyano, nitro, alkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, alkenyl, alkynyl, alkyloxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, acyl, alkyloxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, carbamoyl, alkylcarbamoyl, haloalkylcarbamoyl, hydroxyalkylcarbamoyl, cyanocarbamoyl, amino, acylamino, amino, der er substitueret med en eller to, ens eller forskellige substituenter udvalgt fra ovennævnte substituentgruppe Y, sulfamoyl, methylsulfonyl, methylsulfinyl, cycloalkyl, cycloalkenyl, en ikke-aromatisk heterocyklisk gruppe, aryl, heteroaryl, cycloalkyloxy, cycloalkenyloxy, ikke-aromatisk heterocyclyloxy, aryloxy og heteroaryloxy.
13. Forbindelse ifølge et hvilket som helst af kravene 1 til 12, hvor Rc er usubstitueret alkyl, alkyl, der er substitueret med en eller flere substituenter udvalgt fra substituentgruppe B" (substituentgruppe B": hydroxy, carboxy, sulfo, en substitueret eller usubstitueret ikke-aromatisk heterocyklisk gruppe, tetrazolyl, substitueret eller usubstitueret alkyloxycarbonyl, substitueret eller usubstitueret alkenyloxycarbonyl, substitueret eller usubstitueret alkynyloxycarbonyl, substitueret eller usubstitueret carbamoyl, substitueret eller usubstitueret sulfamoyl, substitueret eller usubstitueret amino, substitueret eller usubstitueret imino og substitueret eller usubstitueret guanidyl) , usubstitueret alkenyl, alkenyl, der er substitueret med en eller flere substituenter udvalgt fra substituentgruppe B", usubstitueret alkynyl eller alkynyl, der er substitueret med en eller flere substituenter udvalgt fra substituentgruppe B", eller dens farmaceutisk acceptable salt eller et solvat deraf, hvor substituenter for "substitueret guanidyl" er en eller flere, ens eller forskellige grupper udvalgt fra gruppen, der består af: alkyl, haloalkyl, hydroxyalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkyloxy, haloalkyloxy, alkenyloxy, alkyloxycarbonyl, alkyloxycarbonylalkyl, amino, alkylamino, acylamino, arylalkylamino, hydroxyamino, imino, hydroxyimino, alkylimino, alkyloxyimino, acylimino, aryl, arylalkyl, aryloxy, en ikke-aromatisk heterocyklisk gruppe, heteroaryl, heteroarylalkyl, ikke-aromatisk heterocyclyloxy, heteroaryloxy, hydroxy, halogen, cyano, acyl, alkylsulfonyl, alkylsulfinyl, carbamoyl, alkylcarbamoyl, alkylcarbamoylalkyl, carbamoylalkyl, carboxyalkyl, sulfamoyl, alkylsulfamoyl, alkylsulfamoylalkyl og sulfamoylalkyl.
14. Forbindelse ifølge et hvilket som helst af kravene 1 til 13, hvor Rc er usubstitueret alkyl, eller dens farmaceutisk acceptable salt eller et solvat deraf.
15. Forbindelse ifølge et hvilket som helst af kravene 1 til 14, hvor Rc er - (CRllaRllb)m-0H; Rlla og Rllb hver for sig er et hydrogenatom, substitueret eller usubstitueret alkyl, substitueret eller usubstitueret alkenyl eller substitueret eller usubstitueret alkynyl, eller Rlla og Rllb sammen med carbonatomet, hvortil de er bundet, danner en substitueret eller usubstitueret cycloalkanring, en substitueret eller usubstitueret cycloalkenring eller en substitueret eller usubstitueret ikke-aromatisk heterocyklisk ring; og m er et helt tal fra 2 til 4, eller dens farmaceutisk acceptable salt eller et solvat deraf.
16. Forbindelse ifølge et hvilket som helst af kravene 1 til 13 og 15, hvor Rc er en gruppe med formlen: [KeinRk forind 4]
eller dens farmaceutisk acceptable salt eller et solvat deraf.
17. Forbindelse ifølge et hvilket som helst af kravene 1 til 13, hvor Rc er (CR14aR14b) t-N (R15a) (R15b) ; R14a og R14b hver for sig er et hydrogenatom, substitueret eller usubstitueret alkyl, substitueret eller usubstitueret alkenyl eller substitueret eller usubstitueret alkynyl, eller R14a og R14b sammen med carbonatomet, hvortil de er bundet, danner en substitueret eller usubstitueret cycloalkanring, en substitueret eller usubstitueret cycloalkenring eller en substitueret eller usubstitueret ikke-aromatisk heterocyklisk ring; t er et helt tal fra 2 til 4; og R15a og R15b hver for sig er et hydrogenatom, substitueret eller usubstitueret alkyl, substitueret eller usubstitueret alkenyl, substitueret eller usubstitueret alkynyl, substitueret eller usubstitueret carbamoyl, substitueret eller usubstitueret sulfamoyl, substitueret eller usubstitueret acyl, substitueret sulfonyl eller substitueret sulfinyl; eller -(CR14a'R14b')t'-C(=0)N(R15a') (R15b') ; R14a' og R14b' hver for sig er et hydrogenatom, substitueret eller usubstitueret alkyl, substitueret eller usubstitueret alkenyl eller substitueret eller usubstrtueret alkynyl, eller R og R sammen med carbonatomet, hvortil de er bundet, danner en substitueret eller usubstitueret cycloalkanring, en substitueret eller usubstitueret cycloalkenring eller en substitueret eller usubstitueret ikke-aromatisk heterocyklisk ring; t' er et helt tal fra 1 til 4; og R15a' og R15b' hver for sig er et hydrogenatom, cyano, substitueret eller usubstitueret alkyl, substitueret eller usubstitueret alkenyl, substitueret eller usubstitueret alkynyl, substitueret eller usubstitueret carbamoyl, substitueret eller usubstitueret sulfamoyl, substitueret eller usubstitueret acyl, substitueret sulfonyl eller substitueret sulfinyl, eller dens farmaceutisk acceptable salt eller et solvat deraf.
18. Forbindelse ifølge et hvilket som helst af kravene 1 til 13 og 17, hvor Rc er en gruppe med formlen:
hvor R , R , R1Sa' 0g R15b’ er gom defineret i krav 17, eller dens farmaceutisk acceptable salt eller et solvat deraf.
19. Forbindelse ifølge et hvilket som helst af kravene 1 til 18, hvor n er 1, eller dens farmaceutisk acceptable salt eller et solvat deraf.
20. Forbindelse ifølge et hvilket som helst af kravene 1 til 19, hvor R4a og R4b begge er hydrogenatomer, eller R4a og R4b, der er bundet til det samme carbonatom, sammen danner oxo, eller dens farmaceutisk acceptable salt eller et solvat deraf.
21. Forbindelse ifølge et hvilket som helst af kravene 1 til 20, hvor n er 1, og R4a og R4b begge er hydrogenatomer, eller dens farmaceutisk acceptable salt eller et solvat deraf.
22. Forbindelse ifølge et hvilket som helst af kravene 1 til 21, hvor R2 er substitueret eller usubstitueret cycloalkyl, substitueret eller usubstitueret aryl eller substitueret eller usubstitueret heteroaryl, eller dens farmaceutisk acceptable salt eller et solvat deraf.
23. Forbindelse ifølge et hvilket som helst af kravene 1 til 22, hvor R2 er cycloalkyl, der eventuelt er substitueret med en eller flere substituenter udvalgt fra substituentgruppe C (substituentgruppe C: halogen, alkyl, alkenyl, alkynyl, alkyloxy, alkenyloxy, alkynyloxy, cycloalkyl, cycloalkenyl, cycloalkynyl og alkylsilylalkynyl) , aryl, der eventuelt er substitueret med en eller flere substituenter udvalgt fra substituentgruppe C, eller heteroaryl, der eventuelt er substitueret med en eller flere substituenter udvalgt fra substituentgruppe C, eller dens farmaceutisk acceptable salt eller et solvat deraf.
24. Forbindelse ifølge et hvilket som helst af kravene 1 til 23, hvor -X- er -N (R5)-, og R5 er som defineret i krav 1, eller dens farmaceutisk acceptable salt eller et solvat deraf.
25. Forbindelse ifølge et hvilket som helst af kravene 1 til 24, hvor -X- er -NH-, eller dens farmaceutisk acceptable salt eller et solvat deraf.
26. Forbindelse ifølge krav 1, som er en af følgende:
eller dens farmaceutisk acceptable salt eller et solvat deraf.
27. Farmaceutisk sammensætning, der omfatter en forbindelse ifølge et hvilket som helst af kravene 1 til 26, eller dens farmaceutisk acceptable salt eller et solvat deraf.
28. Farmaceutisk sammensætning ifølge krav 27, hvor sammensætningen har en P2X3- og/eller P2X2/3-receptorantagonist-effekt.
29. Forbindelse ifølge et hvilket som helst af kravene 1 til 26 eller dens farmaceutisk acceptable salt eller et solvat deraf til anvendelse i en fremgangsmåde til behandling og/eller forebyggelse af en sygdom, der er relateret til P2X3-og/eller P2X2/3~receptoren.
DK11816413.6T 2010-08-10 2011-08-09 Triazinderivat og farmaceutisk forbindelse, der indeholder dette og fremviser analgetisk aktivitet DK2604595T3 (da)

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