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HUP0400710A2 - Tioéter helyettesítővel helyettesített imidazokinolinszármazékok, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények - Google Patents

Tioéter helyettesítővel helyettesített imidazokinolinszármazékok, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények Download PDF

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HUP0400710A2
HUP0400710A2 HU0400710A HUP0400710A HUP0400710A2 HU P0400710 A2 HUP0400710 A2 HU P0400710A2 HU 0400710 A HU0400710 A HU 0400710A HU P0400710 A HUP0400710 A HU P0400710A HU P0400710 A2 HUP0400710 A2 HU P0400710A2
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alkyl
imidazo
butyl
amine
quinolin
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HU0400710A
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Joseph F. Dellaria
Bryon A. Merrill
Matthew R. Radmer
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3M Innovative Properties Company
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Abstract

A találmány tárgyát az 1-helyzetben tioéter funkciós csoportottartalmazó imidazokinolin- és tetrahidroimidazokinolin-származékokképezik, amelyek immunválasz-módosítókként hasznosak. A találmánytárgyát képezik még a fenti hatóanyagokat tartalmazó gyógyászatikészítmények is. A találmány szerinti vegyületek és gyógyászatikészítmények különféle citokinek bioszintézisének indukálásáraképesek, és különféle állapotok, köztük vírusos megbetegedések ésdaganatos megbetegedések kezelésére alkalmasak. A találmány szerintivegyületek az (I) és (II) általános képleteknek megfelelőek, valamintezen vegyületek gyógyászati szempontból elfogadható sói - aképletekben X jelentése -CHR3-, -CHR3-alkil- vagy -CHR3-alkenil-; Z'jelentése -S-, -SO- vagy -SO2-; R1 jelentése alkil-, aril-,heteroaril-, heterogyűrűs, alkenil-, -R4-aril-, -R4-heteroaril-, -R4-heterogyűrűs csoport; R2 jelentése hidrogén, alkil-, alkenil-, aril-,heteroaril-, heterogyűrűs, alkil-Y-alkil-, alkil-Y-alkenil-, alkil-Y-aril- és helyettesített alkil- vagy alkenilcsoport; minden R3jelentése egymástól függetlenül hidrogénatom vagy alkilcsoport; mindenR4 jelentése egymástól függetlenül alkil- vagy alkenilcsoport; mindenY jelentése egymástól függetlenül -O- vagy -S(O)0-2-; n értéke 0-4; ésminden R jelentése egymástól függetlenül alkil-, alkoxi-, hidroxi-,halogénatom és/vagy trifluormetil-csoport. Ó

Claims (31)

  1. -51 SZABADALMI IGÉNYPONTOK
    1. Az (I) általános képletű vegyületek és gyógyászati szempontból elfogadható sóik - a képletben
    X jelentése -CHR3-, -CHR3-alkil- vagy -CHR3-alkenil-;
    Z jelentése -S-, -SO- vagy -SO2-;
    Rí jelentése alkil-, aril-, heteroaril-, heterogyűrűs-, alkenil-, -R4-aril-, -R4-heteroaril-, -R4-heterogyűrüs-csoport;
    R2 jelentése hidrogén, alkil-, alkenil-, aril-, heteroaril-, heterogyűrűs-, alkil-Y-alkil-, alkil-Y-alkenil-, alkil-Y-aril- és alkil- vagy alkenilcsoport, amelyek egy vagy több helyettesítővel helyettesítettek, a helyettesítők jelentése
    -OH, halogén, -N(R3)2, -CO-N(R3)2, -CO-(1 - 10 szénatomos alkil)-, -CO-O-(1 - 10 szénatomos alkil)-,
    -52-n3, aril-, heteroaril-, heterogyűrűs-, -CO-aril- és
    -CO-heteroaril-csoport;
    minden R3 jelentése egymástól függetlenül hidrogénatom vagy 1-10 szénatomos alkilcsoport;
    minden R4 jelentése egymástól függetlenül alkil- vagy alkenilcsoport;
    minden Y jelentése egymástól függetlenül -O- vagy -S(O)0-2-;
    n értéke 0 - 4; és minden R jelentése egymástól függetlenül 1-10 szénatomos alkil-, 1-10 szénatomos alkoxi-, hidroxi-, halogénatom és/vagy trifluormetil-csoport.
  2. 2. Az 1. igénypont szerinti vegyület, amelynek képletében Z jelentése -S-.
  3. 3. Az 1. igénypont szerinti vegyület, amelynek képletében Z jelentése -SO2-.
  4. 4. Az 1. igénypont szerinti vegyület, amelynek képletében Rt jelentése alkilcsoport.
  5. 5. Az 1. igénypont szerinti vegyület, amelynek képletében Rt jelentése arilcsoport.
  6. 6. Az 1. igénypont szerinti vegyület, amelynek képletében Rt jelentése fenilcsoport.
  7. 7. Az 1. igénypont szerinti vegyület, amelynek képletében Rt jelentése heteroarilcsoport.
  8. 8. Az 1. igénypont szerinti vegyület, amelynek képletében X jelentése (CH2)2-6-.
  9. 9. Az 1. igénypont szerinti vegyület, amelynek képletében R2 jelentése H.
  10. 10. Az 1. igénypont szerinti vegyület, amelynek képletében R2 jelentése -alkil-O-alkil-csoport.
  11. 11. Az 1. igénypont szerinti vegyület, amelynek képletében R2 jelentése alkilcsoport.
  12. 12. Az alábbi körbe tartozó valamely vegyület vagy gyógyászati szempontból elfogadható sója:
    -532-butil-1-[4-(feniltio)butil]-1H-imidazo[4,5-c]kinolin-4-amin, 2-butil-1-[2-(feniltio)etil]-6,7,8,9-tetrahidro-1H-imidazo[4,5-c]kinolin-4-amin, 2-butil-1-[4-(fenilszulfonil)butil]-1H-imidazo[4,5-c]kinolin-4-amin, 2-butil-1-[4-(metiltio)butil]-1H-imidazo[4,5-c]kinolin-4-amin, 2-butil-1-[4-(metilszulfonil)butil]-1H-imidazo[4,5-c]kinolin-4-amin, 1-[2-(feniltio)etil]-1H-imidazo[4,5-c]kinolin-4-amin, 1 -[4-(fen i Iszu Ifo η i I) buti I]-1 H-imidazo[4,5-c]kinolin-4-amin, 1 -[4-(metilszu Ifon i l)buti I]-1 H-imidazo[4,5-c]kinolin-4-amin, 1 -[4-(fen i ltio)b úti I]-1 H-imidazo[4,5-c]kinolin-4-amin, 1 -[4-(meti Itio) b util]-1 H-imidazo[4,5-c]kinolin-4-amin, 2-butil-1-[5-(metilszulfonil)pentil]-1H-imidazo[4,5-c]kinolin-4-amin, 2-metil-1-[5-(metilszulfonil)pentil]-1H-imidazo[4,5-c]kinolin-4-amin, 2-etil-1-[5-(metilszulfonil)pentil]-1H-imidazo[4,5-c]kinolin-4-amin, 1-[5-(metilszulfonil)pentil]-1H-imidazo[4,5-c]kinolin-4-amin, 2-hexil-1-[5-(metilszulfonil)pentil]-1H-imidazo[4,5-c]kinolin-4-amin, 2-(2-metoxietil)-1-[5-(metilszulfonil)pentil]-1H-imidazo[4,5-c]kinolin-4-amin, 2-butil-1-[5-(metiltio)pentil]-1H-imidazo[4,5-c]kinolin-4-amin, 2-butil-1-[5-(metilszulfinil)pentil]-1H-imidazo[4,5-c]kinolin-4-amin, 2-butil-1 -[3-(metilszulfonil)propil]-1 H-imidazo[4,5-c]kinolin-4-amin, és 2-butil-1-[3-(fenilszulfonil)propil]-1H-imidazo[4,5-c]kinolin-4-amin.
  13. 13. A (II) általános képletű vegyületek és gyógyászati szempontból elfogadható sóik - a képletben
    X jelentése -CHR3-, -CHR3-alkil-vagy-CHR3-alkenil-;
    Z jelentése -S-, -SO- vagy -SO2-;
    R! jelentése alkil-, aril-, heteroaril-, heterogyűrűs-, alkenil-,
    -R4-aril-,
    -R4-heteroaril- és
    -54-R4-heterogyűrűs-csoport;
    R2 jelentése hidrogén, alkil-, alkenil-, aril-, heteroaril-, heterogyűrűs-, alkil-Y-alkil-, alkil-Y-alkenil-, alkil-Y-aril- és alkil- vagy alkenilcsoport, amelyek egy vagy több helyettesítővel helyettesítettek, a helyettesítők jelentése
    -OH, halogén,
    -N(R3)2,
    -CO-N(R3)2,
    - CO-(1 - 10 szénatomos alkil)-,
    - CO-O-(1 - 10 szénatomos alkil)-,
    - N3, aril-, heteroaril-, heterogyűrűs-, -CO-aril- és
    -CO-heteroaril-csoport;
    minden R3 jelentése egymástól függetlenül hidrogénatom vagy 1-10 szénatomos alkilcsoport;
    minden R4 jelentése egymástól függetlenül alkil- vagy alkenilcsoport;
    minden Y jelentése egymástól függetlenül -O- vagy -S(0)o-2-;
    n értéke 0 - 4; és minden R jelentése egymástól függetlenül 1-10 szénatomos alkil-, 1-10 szénatomos alkoxi-, hidroxi-, halogénatom és/vagy trifluormetil-csoport.
  14. 14. A 13. igénypont szerinti vegyület, amelynek képletében R! jelentése fenilcsoport.
  15. 15. A 13. igénypont szerinti vegyület, amelynek képletében R2 jelentése alkilcsoport.
  16. 16. A 13. igénypont szerinti vegyület, amelyben R2 jelentése -alkil-O-alkil-csoport.
  17. 17. Gyógyászati készítmény, amely terápiásán hatásos mennyiségű 1. igénypont szerinti vegyületet és gyógyászati szempontból elfogadható hordozóanyagot tartalmaz.
  18. 18. Gyógyászati készítmény, amely a 12. igénypont szerinti vegyületek valamelyikének terápiásán hatásos mennyiségét és gyógyászati szempontból elfogadható hordozóanyagot tartalmaz.
  19. 19. Eljárás citokin bioszintézis indukálására állatban, azzal jellemezve, hogy az állatnak az 1. igénypont szerinti vegyület terápiásán hatásos mennyiségét adagoljuk.
  20. 20. A 19. igénypont szerinti eljárás, azzal jellemezve, hogy IFN-α bioszintézist indukálunk.
  21. 21. Eljárás vírusos megbetegedés kezelésére állatban, azzal jellemezve, hogy az állatnak az 1. igénypont szerinti vegyület terápiásán hatásos mennyiségét adagoljuk.
  22. 22. Eljárás állat daganatos betegségének kezelésére, azzal jellemezve, hogy az állatnak az 1. igénypont szerinti vegyület terápiásán hatásos mennyiségét adagoljuk.
  23. 23. Eljárás citokin bioszintézis indukálására állatban, azzal jellemezve, hogy az állatnak a 12. igénypont szerinti vegyület terápiásán hatásos mennyiségét adagoljuk.
  24. 24. A 23. igénypont szerinti eljárás, azzal jellemezve, hogy IFN-α bioszintézist indukálunk.
  25. 25. Eljárás vírusos megbetegedés kezelésére állatban, azzal jellemezve, hogy az állatnak egy, a 12. igénypont szerinti vegyület terápiásán hatásos mennyiségét adagoljuk.
  26. 26. Eljárás állat daganatos betegségének kezelésére, azzal jellemezve, hogy az állatnak egy, a 12. igénypont szerinti vegyület terápiásán hatásos mennyiségét adagoljuk.
  27. 27. Gyógyászati készítmény, amely valamely, a 13. igénypont szerinti vegyület terápiásán hatásos mennyiségét és gyógyászati szempontból elfogadható hordozóanyagot tartalmaz.
  28. 28. Eljárás citokin bioszintézis indukálására állatban, azzal jellemezve, hogy az állatnak a 13. igénypont szerinti vegyület terápiásán hatásos mennyiségét adagoljuk.
  29. 29. A 29. igénypont szerinti eljárás, azzal jellemezve, hogy IFN-α bioszintézist indukálunk.
  30. 30. Eljárás vírusos megbetegedés kezelésére állatban, azzal jellemezve, hogy az állatnak a 13. igénypont szerinti vegyület terápiásán hatásos mennyiségét adagoljuk.
  31. 31. Eljárás állat daganatos betegségének kezelésére, azzal jellemezve, hogy az állatnak a 13. igénypont szerinti vegyület terápiásán hatásos mennyiségét adagoljuk.
    A bejelentő helyett a meghatalmazott:
    DANUBIA
    Szabadalmi és Védjegy Iroda Kft.
    Dr. Valyon Józsefné szabadalmi ügyvivő
    J ocitL ,ΪΟΟ·
HU0400710A 2000-12-08 2001-12-06 Tioéter helyettesítővel helyettesített imidazokinolinszármazékok, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények HUP0400710A2 (hu)

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HU0400710A HUP0400710A2 (hu) 2000-12-08 2001-12-06 Tioéter helyettesítővel helyettesített imidazokinolinszármazékok, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények
HU0400704A HUP0400704A2 (hu) 2000-12-08 2001-12-06 Heterociklusos éterrel szubsztituált imidazokinolinok, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények
HU0600600A HUP0600600A2 (en) 2000-12-08 2001-12-06 Sulfonamido ether substituted imidazoquinolines, pharmaceutical compositions containing them and intermediates
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