DK2703392T3 - Aromatisk heterocyklisk derivat i form af en 5-leddet ring med npy y5-receptorantagonistisk aktivitet - Google Patents

Aromatisk heterocyklisk derivat i form af en 5-leddet ring med npy y5-receptorantagonistisk aktivitet Download PDF

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DK2703392T3
DK2703392T3 DK12777012.1T DK12777012T DK2703392T3 DK 2703392 T3 DK2703392 T3 DK 2703392T3 DK 12777012 T DK12777012 T DK 12777012T DK 2703392 T3 DK2703392 T3 DK 2703392T3
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Kyohei Hayashi
Yuusuke Tamura
Naoki Omori
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Shionogi & Co
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Claims (12)

1. Forbindelse med formlen (I):
(i) eller farmaceutisk acceptabelt salt deraf, hvor R1 er substitueret eller usubstitueret, ligekædet eller forgrenet (C1-C10)-alkyl, substitueret eller usubstitueret, ligekædet eller forgrenet (C2-C10)-alkenyl, substitueret eller usubstitueret, ligekædet eller forgrenet (C2-C10)-alkynyl, substitueret eller usubstitueret (C3-C8) -cycloalkyl, substitueret eller usubstitueret (C3-C8)-cycloalkenyl eller substitueret amino, p er 1, og q og r er 0, en gruppe med formlen:
er en gruppe med formlen:
og R2 er substitueret eller usubstitueret, ligekædet eller forgrenet (C1-C10)-alkyl, substitueret eller usubstitueret (C3-Cs)-cycloalkyl, substitueret eller usubstitueret (Cs-Cs)- cycloalkenyl, substitueret eller usubstitueret aryl, substitueret eller usubstitueret heteroaryl eller substitueret eller usubstitueret heterocyclyl, hvor det "substituerede alkyl", "substituerede alkenyl", "substituerede alkynyl", "substituerede cycloalkyl", "substituerede cycloalkenyl", "substituerede aryl", "substituerede heteroaryl" eller "substituerede heterocyclyl" kan være substitueret i en eller flere vilkårlige positioner med en eller flere grupper valgt blandt halogen, hydroxy, mercapto, nitro, nitroso, cyano, azid, formyl, amino, carboxy, (Ci—Cio) -alkyl, (C1-C10) -halogenalkyl, (C2-C10) -alkenyl, (C2-C10)-alkynyl, (C3-C8) -cycloalkyl, (C3-C8) -cycloalkenyl, aryl, heteroaryl, heterocyclyl, substitueret carbamoyl, substitueret sulfamoyl, substitueret amidino, en gruppe med formlen: -O-R10, en gruppe med formlen: -O-C(=0)-R10, en gruppe med formlen: -C (=0) -R10, en gruppe med formlen: -C (=0)-O-R10, en gruppe med formlen: -S-R10 og en gruppe med formlen: -SO2-R10 (hvor R10 er (C1-C10) -alkyl, (C1-C10) -halogenalkyl, (C2-C10) -alkenyl, (C2-C10) - alkynyl, (C3-C8) -cycloalkyl, (C3-C8) -cycloalkenyl, aryl, heteroaryl, heterocyclyl, carbamoyl, sulfamoyl eller amidino), og hvor udtrykket "aryl" henviser til monocyklisk eller polycyklisk aromatisk carbocyclyl og monocyklisk eller polycyklisk aromatisk carbocyclyl kondenseret med en eller to 3- til 8-leddede cykliske grupper, udtrykket "heteroaryl" henviser til en monocyklisk eller polycyklisk aromatisk heterocyclylgruppe, som indeholder et eller flere heteroatomer, der er vilkårligt valgt blandt 0, S og N, på ringen, eller en monocyklisk eller polycyklisk aromatisk heterocyclylgruppe kondenseret med en eller to 3- til 8-leddede cykliske grupper, og udtrykket "heterocyclyl" henviser til en ikke-aromatisk heterocyclylgruppe, som indeholder et eller flere heteroatomer, der er vilkårligt valgt blandt 0, S og N, på ringen, eller en ikke-aromatisk heterocyclylgruppe kondenseret med en eller to 3- til 8-leddede cykliske grupper.
2. Forbindelse eller farmaceutisk acceptabelt salt deraf ifølge krav 1, hvor R1 er substitueret eller usubstitueret alkyl eller substitueret eller usubstitueret cycloalkyl.
3. Forbindelse eller farmaceutisk acceptabelt salt deraf ifølge krav 2, hvor R1 er substitueret eller usubstitueret alkyl.
4. Forbindelse eller farmaceutisk acceptabelt salt deraf ifølge krav 1, hvor R2 er substitueret eller usubstitueret aryl.
5. Forbindelse eller farmaceutisk acceptabelt salt deraf ifølge krav 1, hvor R2 er en gruppe med formlen:
hvor R3 er halogen, alkylsulfonyl, halogenalkyl eller halogenalkyloxy, og R4 er hydrogen, halogen, alkylsulfonyl, halogenalkyl eller halogenalkyloxy.
6. Forbindelse eller farmaceutisk acceptabelt salt deraf ifølge krav 1, hvor R2 er substitueret eller usubstitueret alkyl.
7. Forbindelse eller farmaceutisk acceptabelt salt deraf ifølge krav 1, hvor R2 er substitueret eller usubstitueret halogenalkyl.
8. Forbindelse eller farmaceutisk acceptabelt salt deraf ifølge krav 1, hvor R2 er substitueret eller usubstitueret cycloalkyl, substitueret eller usubstitueret cycloalkenyl eller substitueret eller usubstitueret heterocyclyl.
9. Forbindelse eller farmaceutisk acceptabelt salt deraf ifølge krav 1, hvor R2 er substitueret eller usubstitueret cycloalkyl.
10. Forbindelse med formlen (IV):
(IV) eller farmaceutisk acceptabelt salt deraf, hvor R1 er substitueret eller usubstitueret, ligekædet eller forgrenet (Ci-Cio)-alkyl, en gruppe med formlen:
er en gruppe med formlen:
og R2 er substitueret eller usubstitueret, ligekædet eller forgrenet (Ci-Cic) -halogenalkyl, hvor det "substituerede alkyl" kan være substitueret i en eller flere vilkårlige positioner med en eller flere grupper valgt blandt halogen, hydroxy, mercapto, nitro, nitroso, cyano, azid, formyl, amino, carboxy, (C1-C10) -alkyl, (C1-C10) -halogenalkyl, (C2-C10) -alkenyl, (C2-C10) -alkynyl, (C3-C8)- cycloalkyl, (C3-C8)-cycloalkenyl, aryl, heteroaryl, heterocyclyl, substitueret carbamoyl, substitueret sulfamoyl, substitueret amidino, en gruppe med formlen: -O-R10, en gruppe med formlen: -0-C (=0) -R10, en gruppe med formlen: -C(=0)-R10, en gruppe med formlen: -C (=0)-O-R10, en gruppe med formlen: -S-R10 og en gruppe med formlen: -SO2-R10 (hvor R10 er (C1-C10) -alkyl, (C1-C10)-halogenalkyl, (C2-C10) -alkenyl, (C2-C10) -alkynyl, (C3- Ce)-cycloalkyl, (C3-C8)-cycloalkenyl, aryl, heteroaryl, heterocyclyl, carbamoyl, sulfamoyl eller amidino), hvor substituenten i det "substituerede halogenalkyl" kan være substitueret i en eller flere vilkårlige positioner med en eller flere grupper valgt blandt hydroxy, mercapto, nitro, nitroso, cyano, azid, formyl, amino, carboxy, (C1-C10)-alkyl, (C1-C10)-halogenalkyl, (C2-C10) -alkenyl, (C2-C10) -alkynyl, (C3- Ce)-cycloalkyl, (C3-C8)-cycloalkenyl, aryl, heteroaryl, heterocyclyl, substitueret carbamoyl, substitueret sulfamoyl, substitueret amidino, en gruppe med formlen: -O-R10, en gruppe med formlen: -0-C (=0) -R10, en gruppe med formlen: -C(=0)-R10, en gruppe med formlen: -C (=0)-O-R10, en gruppe med formlen: -S-R10 og en gruppe med formlen: -SO2-R10 (hvor R10 er (C1-C10)-alkyl, (C1-C10)-halogenalkyl, (C2-C10) -alkenyl, (C2-C10) -alkynyl, (C3- Cs)-cycloalkyl, (C3-C8)-cycloalkenyl, aryl, heteroaryl, heterocyclyl, carbamoyl, sulfamoyl eller amidino), og hvor udtrykket "aryl" henviser til monocyklisk eller polycyklisk aromatisk carbocyclyl og monocyklisk eller polycyklisk aromatisk carbocyclyl kondenseret med en eller to 3- til 8-leddede cykliske grupper, udtrykket "heteroaryl" henviser til en monocyklisk eller polycyklisk aromatisk heterocyclylgruppe, som indeholder et eller flere heteroatomer, der er vilkårligt valgt blandt 0, S og N, på ringen, eller en monocyklisk eller polycyklisk aromatisk heterocyclylgruppe kondenseret med en eller to 3- til 8-leddede cykliske grupper, og udtrykket "heterocyclyl" henviser til en ikke-aromatisk heterocyclylgruppe, som indeholder et eller flere heteroatomer, der er vilkårligt valgt blandt 0, S og N, på ringen, eller en ikke-aromatisk heterocyclylgruppe kondenseret med en eller to 3- til 8-leddede cykliske grupper.
11. Farmaceutisk sammensætning, som omfatter forbindelsen eller et farmaceutisk acceptabelt salt deraf ifølge et hvilket som helst af kravene 1-10.
12. Farmaceutisk sammensætning ifølge krav 11, som har NPY Y5-receptorantagonistisk aktivitet. Forbindelse ifølge krav 1, som har formlen:
eller et farmaceutisk acceptabelt salt eller solvat deraf.
DK12777012.1T 2011-04-27 2012-04-25 Aromatisk heterocyklisk derivat i form af en 5-leddet ring med npy y5-receptorantagonistisk aktivitet DK2703392T3 (da)

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