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HK1088892A1 - 1-(4-piperidinyl)-1,3-dihydro-2h-benzoxazole-2-one derivatives and related compounds as nociceptin analogs and orl1 ligands for the treatment of pain - Google Patents

1-(4-piperidinyl)-1,3-dihydro-2h-benzoxazole-2-one derivatives and related compounds as nociceptin analogs and orl1 ligands for the treatment of pain Download PDF

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Publication number
HK1088892A1
HK1088892A1 HK06105934.2A HK06105934A HK1088892A1 HK 1088892 A1 HK1088892 A1 HK 1088892A1 HK 06105934 A HK06105934 A HK 06105934A HK 1088892 A1 HK1088892 A1 HK 1088892A1
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Hong Kong
Prior art keywords
alkyl
piperidinyl
dihydro
group
benzoxazol
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HK06105934.2A
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English (en)
French (fr)
Chinese (zh)
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HK1088892B (en
Inventor
Qun Sun
Richard R. Goehring
Donald Kyle
Zhengming Chen
Sam Victory
John Whitehead
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Euro-Celtique S.A.
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27501377&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HK1088892(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from HK04105109.3A external-priority patent/HK1063149B/en
Application filed by Euro-Celtique S.A. filed Critical Euro-Celtique S.A.
Publication of HK1088892A1 publication Critical patent/HK1088892A1/en
Publication of HK1088892B publication Critical patent/HK1088892B/en

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Claims (19)

  1. Eine Verbindung der Formel (IA): wobei
    Z ausgewählt ist aus der Gruppe bestehend aus einer Bindung, -NH-, -CH2O-,-CH2NH-, -CH2N(CH3)-, -NHCH2-, -CH2CONH-, -NHCH2CO-, -CH2CO-, - CH2COCH2-, -CH(CH3)-, -CH= und -HC=CH-, wobei die Kohlenstoff und/oder Stickstoffatome unsubstituiert oder substituiert sind mit einer niedrigen Alkyl-, Halogen-, Hydroxy- oder Alkoxy-Gruppe;
    R1 ausgewählt ist aus der Gruppe bestehend aus Wasserstoff, C3-12 cycloalkyl, C2-10alkenyl, Amino, C1-10alkylamino-, C3-12cycloalkylamino-, Benzyl, C3-12 Cycloalkenyl-, einem monozyklischen, bizyklischen oder trizyklischen Aryl- oder Heteroarylring, einem hetero-monozyklischen Ring, einem hetero-bizyklischen Ringsystem, und einem Spiroringsystem der Formel (V): wobei X1 und X2 unabhängig ausgewählt sind aus der Gruppe bestehend aus NH, O, S und CH2; wobei besagtes Alkyl, Cycloalkyl, Alkenyl, C1-10alkylamino-, C3-12cycloalkylamino-, oder Benzyl wahlweise substituiert ist mit 1-3 Substituenten ausgewählt aus der Gruppe bestehend aus Halogen, C1-10Alkyl, C1-10 Alkoxy, Nitro, Trifluormethyl-, Cyano, Phenyl, Benzyl, Benzyloxy, besagtes Phenyl, Benzyl, und Benzyloxy wahlweise substituiert mit 1-3 Substituenten ausgewählt aus der Gruppe bestehend aus Halogen, C1-10Alkyl-, C1-10Alkoxy-, und Cyano; wobei besagtes C3-12Cycloalkyl, C3-12Cycloalkenyl, monozyklisches, bizyklisches oder trizyklisches Aryl, Heteroarylring, hetero-monozylischer Ring, heterobizyklisches Ringsystem, oder Spiroringsystem der Formel (V) wahlweise substituiert ist mit 1-3 Substituenten ausgewählt aus der Gruppe bestehend aus Halogen, C1-10 Alkyl, C1-10 Alkoxy, Nitro, Trifluormethyl-, Phenyl, Benzyl, Phenyloxy und Benzyloxy, wobei besagtes Phenyl, Benzyl, Phenyloxy oder Benzyloxy wahlweise substituiert ist mit 1-3 Substituenten ausgewählt aus der Gruppe bestehend aus Halogen, C1-10 Alkyl, C1-10 Alkoxy, und Cyano; aber keine Verbindung der folgenden Formel wobei Ar ein monozyklischer Arylring ist, wahlweise substituiert mit Halogen, C1-5 Alkoxy, C1-5 Alkyl und Cyano und wobei R7 und R8 unabhängig voneinander Wasserstoff, C1-5 Alkyl und C1-5 Alkoxy oder Halogen sind; alternativ können R7 und R8 so zusammen hängen, dass sie einen wahlweise substituierten 5- bis 7-gliedrigen carbozyklischen oder heterozyklischen Ring bilden, wobei dieser Ring gesättigt, ungesättigt oder aromatisch sein kann; oder ein pharmazeutisches verträgliches Salz davon.
  2. Eine Verbindung gemäß Anspruch 1, wobei R1 ein Alkyl ausgewählt aus der Gruppe bestehend aus Methyl, Ethyl, Propyl, Butyl, Pentyl und Hexyl ist.
  3. Eine Verbindung gemäß Anspruch 1, wobei R1 ein Cycloalkyl ausgewählt aus der Gruppe bestehend aus Cyclohexyl, Cycloheptyl, Cyclooctyl, Cyclononyl, Cyclodecyl, und Norbornyl ist.
  4. Eine Verbindung gemäß Anspruch 1, wobei R1 Tetrahydronaphthyl, Decahydronaphthyl oder Dibenzocycloheptyl ist.
  5. Eine Verbindung gemäß Anspruch 1, wobei R1 Phenyl oder Benzyl ist.
  6. Eine Verbindung gemäß Anspruch 1, wobei R1 ein bizyklischer aromatischer Ring ist.
  7. Eine Verbindung gemäß Anspruch 6, wobei besagter bizyklischer aromatischer Ring Indenyl, Quinolin oder Naphthyl ist.
  8. Eine Verbindung gemäß Anspruch 1, wobei Z eine Bindung ist.
  9. Eine Verbindung gemäß Anspruch 1, wobei X1 und X2 beide O sind.
  10. Eine Verbindung gemäß Anspruch 1 ausgewählt aus der Gruppe bestehend aus 3-[1-(p-Phenylbenzyl)-4-piperidinyl]-2H-benzoxazol-2-on; 3-[1-(p-Phenyloxybenzyl)-4-piperidinyl]-2H-benzoxazol-2-on; 3-[1-(p-Cyanobenzyl)-4-piperidinyl]-2H-benzoxazol-2-on; 3-[1-[4,4-Bis-(4-fluorphenyl)butyl]-4-piperidinyl]-2H-benzoxazol-2-on; 3-[1-(1,2,3,4-Tetrahydro-2-naphtyl)-4-piperidinyl]-2H-benzoxazol-2-on; 3-[1-(5-Methylhex-2-yl)-4-piperidinyl]-2H-benzoxazol-2-on; 3-[1-(10,11-Dihydro-5H-dibenzo[a,d]-5-cyclohepten-5-yl)-4-piperidinyl]-2H-benzoxazol-2-on; 3-[1-(4-Propyl-cyclohexyl)-4-piperidinyl]-2H-benzoxazol-2-on; 3-[1-(Norbornan-2-yl)-4-piperidinyl]-2H-benzoxazol-2-on; 3-[1-(Decahydro-2-naphtyl)-4-piperidinyl]-2H-benzoxazol-2-on; 3-[1-(3,3-Dimethyl-1,5-dioxaspiro[5.5]undeca-9-yl)-4-piperidinyl]-2H-benzoxazol-2-on; 3-[1-[4-(1-Methylethyl)-cyclohexyl]-4-piperidinyl]-2H-benzoxazol-2-on; 3-[1-(1,3-Dihydroinden-2-yl)-4-piperidinyl]-2H-benzoxazol-2-on; 3-[1-(Cyclooctyl)-4-piperidinyl]-2H-benzoxazol-2-on; und pharmazeutisch verträgliche Salze davon.
  11. Eine pharmazeutische Zusammensetzung umfassend eine Verbindung gemäß Anspruch 1 und mindestens einen pharmazeutisch verträglichen Hilfsstoff.
  12. Verwendung einer analgetischen Verbindung gemäß Anspruch 1 zur Herstellung eines Medikamentes zur Behandlung von Schmerzen.
  13. Verwendung einer Verbindung gemäß Anspruch 1 zur Herstellung eines Medikamentes zur Modulation einer pharmakologischen Antwort vom ORL1-Rezeptor.
  14. Eine Verbindung der Formel (IA): wobei
    ZR1 folgende Struktur hat wobei Y1 R3-(C1-C12)alkyl, R4-Aryl, R5-Heteroaryl, R6-(C3-C12)cyclo-alkyl, R7-(C3-C12)heterocycloalkyl, -CO2(C1-C6)alkyl, CN oder -C(O)NR8R9 ist; Y2 Wasserstoff oder Y1 ist; Y3 Wasserstoff oder (C1-C6)alkyl ist; oder Y1, Y2 und Y3 zusammen mit dem Kohlenstoff an den sie gebunden sind, eine der folgenden Strukturen bilden: oder wobei r 0 bis 3 ist; c und d unabhängig 1 oder 2 sind; s 1 bis 5 ist; und Ring E ein fusionierter R4-phenyl oder R5-heteroarylring ist;
    R10 1 bis 3 Substituenten ist unabhängig ausgewählt aus der Gruppe bestehend aus H, (C1-C6)alkyl, -OR8, -(C1-C6)alkyl-OR8, -NR8R9 und -(C1-C6)alkyl-NR8R9;
    R11 1 bis 3 Substituenten ist unabhängig ausgewählt aus der Gruppe bestehend aus R10, -CF3, -OCF3, NO2 und Halo, oder R11 Substituenten an benachbarten Ringkohlenstoffatomen zusammen einen Methylendioxy- oder Ethylendioxyring bilden können;
    R8 und R9 unabhängig ausgewählt sind aus der Gruppe bestehend aus Wasserstoff, (C1-C6)alkyl, (C3-C12)cycloalkyl, Aryl und Aryl(C1-C6)alkyl;
    R3 1 bis 3 Substituenten ist unabhängig ausgewählt aus der Gruppe bestehend aus H, R4-aryl, R6-(C3-C12)cycloalkyl, R5-Heteroaryl, R7-(C3-C7) Heterocycloalkyl, - NR8R9, -OR12 und -S(O)0-2R12;
    R6 1 bis 3 Substituenten ist unabhängig ausgewählt aus der Gruppe bestehend aus H, (C1-C6)Alkyl, R4-Aryl, -NR8R9, -OR12 und -SR12; R4 ist 1 bis 3 Substituenten unabhängig ausgewählt aus der Gruppe bestehend aus Wasserstoff, Halo, (C1-C6)Alkyl, R13-Aryl, (C3-C12)cycloalkyl, -CN, -CF3, -OR8, -(C1-C6)alkyl-OR8, -OCF3, -NR8R9, -(C1-C6)alkyl, -NR8R9, -NHSO2R8, -SO2N(R14)2, -SO2R8, -SOR8, -SR8, -NO2, -CONR8R9, -NR9COR8, -COR8, -COCF3, -OCOR8, -OCO2R8, -COOR8, -(C1-C6)alkyl-NHCOOC(CH3)3, -(C1-C6)alkyl-NHCOCF3, -(C1-C6)Alkyl-NHSO2-(C1-C6)alkyl, -(C1-C6)alky-NHCONH-(C1-C6)-alkyl und wobei f0 bis 6 ist; oder R4 Substituenten an den benachbarten Ringkohlenstoffatomen zusammen einen Methylendioxy- oder Ethylendioxyring bilden können;
    R5 1 bis 3 Substituenten ist unabhängig ausgewählt aus der Gruppe bestehend aus Wasserstoff, Halo, (C1-C6)alkyl, R13-Aryl, (C3-C12)cycloalkyl, -CN, -CF3, -OR8, -(C1 C6)Alkyl-OR8, -OCF3, -NR8R9, -(C1-C6)Alkyl-NR8R9, -NHSO2R8, -SO2N(R14)2, -NO2, -CONR8R9, -NR9COR8, -COR8, -OCOR8, -OCO2R8 und -COOR8;
    R7 H, (C1-C6)alkyl,-OR8,- (C1-C6)Alkyl-OR8, -NR8R9 oder -(C1-C6)alkyl-NR8R9 ist;
    R12 H, (C1-C6)alkyl, R4-Aryl, -(C1-C6)alkyl-OR8, -(C1-C6)alkyl-NR8R9, -(C1-C6)alkyl-SR8, oder Aryl(C1-C6)alkyl ist;
    R13 1-3 Substituenten ist unabhängig ausgewählt aus der Gruppe bestehend aus H, (C1-C6)alkyl, (C1-C6)alkoxy und Halo;
    R14 unabhängig ausgewählt ist aus der Gruppe bestehend aus H, (C1-C6)alkyl and R13-C6H4-CH2-;
    oder ein pharmazeutisch verträgliches Salz davon.
  15. Eine pharmazeutische Zusammensetzung umfassend eine Verbindung gemäß Anspruch 14 und mindestens einen pharmazeutisch verträglichen Hilfsstoff.
  16. Verwendung einer analgetischen Verbindung gemäß Anspruch 14 zur Herstellung eines Medikamentes zur Behandlung von Schmerzen.
  17. Verwendung einer Verbindung gemäß Anspruch 14 zur Herstellung eines Medikamentes zur Modulation einer pharmakologischen Antwort vom ORL1-Rezeptor.
  18. Verwendung einer Verbindung gemäß Anspruch 1 zur Herstellung eines Medikamentes zur Modulation einer pharmakologischen Antwort von einem Opioid-Rezeptor.
  19. Verwendung einer Verbindung gemäß Anspruch 14 zur Herstellung eines Medikamentes zur Modulation einer pharmakologischen Antwort von einem Opioid-Rezeptor.
HK06105934.2A 2001-04-18 2004-07-13 1-(4-piperidinyl)-1,3-dihydro-2h-benzoxazole-2-one derivatives and related compounds as nociceptin analogs and orl1 ligands for the treatment of pain HK1088892B (en)

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US28466901P 2001-04-18 2001-04-18
US28466601P 2001-04-18 2001-04-18
US28466801P 2001-04-18 2001-04-18
US28466701P 2001-04-18 2001-04-18
US284669P 2001-04-18
US284666P 2001-04-18
US284667P 2001-04-18
US284668P 2001-04-18
HK04105109.3A HK1063149B (en) 2001-04-18 2002-04-18 Nociceptin analogs

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