KR920702620A - 암치료에 유용하며 항히스타민성 특성을 갖는 약물 - Google Patents

암치료에 유용하며 항히스타민성 특성을 갖는 약물

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KR920702620A
KR920702620A KR1019910701934A KR910701934A KR920702620A KR 920702620 A KR920702620 A KR 920702620A KR 1019910701934 A KR1019910701934 A KR 1019910701934A KR 910701934 A KR910701934 A KR 910701934A KR 920702620 A KR920702620 A KR 920702620A
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hydrogen
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halogen
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윌리엄 레버 오스카
크리스티에 킹 앤
하페니스트 모르톤
유-슈안 카오 에스터
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엠. 피. 잭슨
더 웰컴 파운데이숀 리미티드
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Priority claimed from GB898914062A external-priority patent/GB8914062D0/en
Priority claimed from GB898914040A external-priority patent/GB8914040D0/en
Priority claimed from GB898914060A external-priority patent/GB8914060D0/en
Priority claimed from GB898914061A external-priority patent/GB8914061D0/en
Application filed by 엠. 피. 잭슨, 더 웰컴 파운데이숀 리미티드 filed Critical 엠. 피. 잭슨
Publication of KR920702620A publication Critical patent/KR920702620A/ko

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Abstract

내용 없음

Description

암치료에 유용하며 항히스타민성 특성을 갖는 약물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (18)

  1. 항종양성 제제의 치료 효과를 증가시킬수 있는 약물을 제조함에 있어서 하기 일반식(I)의 화합물 또는 그의 약학적 허용염을 사용하는 방법.
    상기식에서, A는또는로부터 선택된 기이며 X는-CH-또는-N-을 나타내고
    R1은 수소 또는 할로겐 원자, C1-4알콕시기, C1-4알킬기, 또는 1 내지 3개의 할로겐 원자로 치환된 C1-4알킬기를 나타내며; R2는 수소 또는 할로겐 원자, C1-4알콕시키, 벤질옥시, -R7COOR8(이때, R7은 단일결합 또는 C1-72가 지방족 탄화수소기를 나타내며 R8은 수소원자 또는 C1-4알킬기를 나타낸다) 또는 R7CONR8aR8b(이때, R8a및R8b각각은 수소원자 또는 알킬기를 나타내거나 또는 질소원자와 함께 4 내지 6원 포화 헤테로사이클릭 고리를 형성하기도 한다)를 나타내고; R3및R4각각 수소원자 또는 C1-4알킬기를 나타내는 것으로서 서로 같거나 다를수 있거나, 또는 R3및R4가 부착된 질소원자와 함께 4 내지 6원포화 헤테로사이클릭 고리를 형성할수 있는데 이때 시소원자 또는 추가의 질소원자를 임의로 함유할 수 있고 이들은C1-4알킬기에 의해 치환될 수도 있으며; R5및R6는 수소원자를 나타내거나 또는 -CH2CH2-,CH2O-, -OCH2-, -NHCH2- 또는 -CH2NH-로부터 선택된, 방향족 고리사이의 연결기를 함께 형성할 수도 있으며; n은 0 또는 1 내지 3의 정수이고; 그리고 p 및 q는 1 내지 4의 정수로 부터 각각 선택되며, 단, (a)R5와 R6가 연결기를 형성할 경우, A는-(CH2)n-일 수 없으며, (b) A가기이고 n은 1이며 R1은 메틸이고, NR3R4는 피롤리디노이며 R5및 R가 모두 수소인 경우 R2는 수소 또는 -CH=CHCO2H가 될 수 없다.
  2. 제 1항에 있어서, 상기 일반식 (I)의 화합물은 하기 일반식 (Ⅱ)의 화합물 또는 그것의 약학적 허용염으로 표시될수 있음을 특징으로 하는 방법:
    상기 식에서 R9는 할로겐이고;R10는 수소, 할로겐, C1-4알콕시 -OCH2C6H5, 또는 -CH=CHCO2R12이며 이때 R12는 C1-4알킬, 바람직하게는 에틸이며; 그리고 R11은 C1-4알킬, -CH2CH2=CH2또는 CH2C6H4CH3-이다.
  3. 제 1항에 있어서, 상기 일반식(I)의 화합물은 하기 일반식(Ⅲ)의 화합물 또는 그것의 약학적 허용염으로 표시될 수 있음을 특징으로 하는 방법.
    상기 식에서R13은 C1-72가 지방족 탄화수소기 또는 단일 결합을 나타내며;R14는 C1-4알킬이고;R15는 수소, 할로겐, C1-4알콕시, C1-4알킬 또는 1 내지 3 할로겐 원자로 치환된 C1-4알킬이며;R16및 R17은 각각 수소원자 또는 C1-4알킬기를 나타내는 것으로서 서로 같거나 다를 수 있으며 또는 질소원자와 함께 4 내지 6원 포화헤테로 사이클릭기를 형성할 수도 있고; 그리고 A'은 각각이 수소원자를 나타내거나, -A'C - CA'는 -C=C-를 나타낸다.
  4. 제1항에 있어서, 상기 일반식(1)의 화합물은 하기 일반식(Ⅳ)의 화합물 또는 그것의 약학적 허용염으로 표시될 수 있음을 특징으로 하는 방법.
    상기 식에서 R19는 -CH2CH2-, -CH2O-, -OCH2-,-NHCH2-, 또는 -CH2NH-이고; Y는 1,2,3 또는 4위치에 결합된 수소 또는 할로겐이며; Y'은 7,8,9 또는 10 위치에 결합된 수소 또는 할로겐이며; n은 0 또는 3이고; p 및 q 각각은 1 내지 4이며; 그리고 R20및R21은 수소 또는 C1-4알킬로 부터 각각 선택되거나 또는 질소원자와 함께 4내지 6원으로 구성된 질소-함유 헤테로사이클릭고리를 형성할수도 있다.
  5. 제1항에 있어서, 상기 일반식(I)의 화합물은 하기 일반식(Ⅴ)의 화합물 또는 그것의 약학적 허용염으로 표시될 수 있음을 특징으로 하는 방법.
    상기 식에서 R22는 할로겐, -COOH-, -CH=CH-COOH-, -CH2COOH 또는 -(CH2)2COOH이고;R23은 수소, 할로겐, C1-4알콕시 또는 C1-4알킬이며; 그리고R24및R25는 같거나 상이하며 각각은 수소 또는C1-4이거나 또는 NR24R25는 피롤리디노일 수도 있다.
  6. 제1항에 있어서, 상기 일반식(I)의 화합물은 하기 일반식(Ⅵ)의 화합물 또는 그것의 약학적 허용염으로 표시될 수 있음을 특징으로 하는 방법.
    상기 식에서 R22는 할로겐, -COOH, -CH=CH-COOH, -CH2COOH 또는 -(CH2)2COOH이다.
  7. 제1항 내지 제6항중 어느 한 항에 있어서, 항종양성 제제에 대해 내성을 갖는 종양의 상기 항종양성 제제에 대한 감수성을 증가시키기 위한 약물을 제조함에 있어서 상기 일반식(I)의 화합물을 사용하는 방법.
  8. 제1항 내지 제6항중 어느 한 항에 있어서, 종양세포의 성장을 선택적으로 억제시킬 수 있는 약물을 제조함에 있어서 상기 일반식(I)의 화합물을 사용하는 방법.
  9. 제1항 내지 제6항중 어느 한 항에 있어서, 종양에 대한 다형 약물 내성을 억제할 수 있는 약물의 제조시 상기 일반식(I)의 화합물을 사용하는 방법.
  10. 제1항 내지 제7항중 어느 한 항에 있어서, 상기 항종양성 제제는 빈카 알카로이드, 에피포도필로톡신 안트라사이클린 항생제, 엑티노마이신 D, 플리카마이신, 퓨로마이신, 그라미시딘 D, 탁솔, 콜키신, 시토칼라신 B, 에메틴, 메이탄신 및 암사트린으로부터 선택된 것을 특징으로 하는 방법.
  11. 제1항 내지 제10항중 어느 한 항에 있어서, 상기 약물이 선암의 치료를 목적으로 하는 것을 특징으로 하는 방법.
  12. 항종양성 제제의 치료효과를 증가시키는 데에 사용될 수 있는 제1항 내지 제6항중 어느 한 항에 정의된 일반식(1)의 화합물.
  13. 제1항 내지 제6항중 어느 한 항에 있어서 정의된 일반식(I)의 화합물 및 항종양성 제제를 약학적 허용담체 또는 부형제와 함께 포함하는, 종양의 치료에 사용될 수 있는 약학적 조성물.
  14. 제12항에 있어서, 상기 항종양성 제제는 제10항에서 정의된 것임을 특징으로 하는 조성물.
  15. 하기 일반식(Ⅳa)의 화합물 또는 그것의 약학적 허용염;
    상기 식에서, R19는 -CH2CH2-,CH2O-, -OCH2-,-NHCH2- 또는-CH2NH-이고; Y는 1,2,3 또는 4위치에 부착된 수소 또는 할로겐이며; Y'은 7,8,9 또는 10 위치에 부착된 수소 또는 할로겐이며; n은 0 또는 3이고 p 및 q 각각은 1 내지 4이며; 그리고 R20및R21은 수소 또는 C1-4알킬로부터 각각 선택되거나 또는 질소원자와 함께 4내지 6원으로 구성된 질소-함유 헤테로사이클릭고리를 형성할수도 있으며, 단, a)R19가 -CH2CH2-,-CH2O 또는 -OCH2-이고 p와 q는 각각 1이며, Y와 Y'중 하나가 할로겐인 경우 나머지는 수소가 아니며, b)R19가 -CH2CH2또는 -CH2O-이고 p와 q는 둘 모두 1이며, Y와 Y'은 각각 수소 또는 할로겐인 경우 n은 2가 아니어야 한다.
  16. a) 하기 일반식(Ⅷ)의 화합물을 적절한 위티크 시약 또는 그리그나드 시약과 반응시킨후 탈수시키는 단계; b) 하기 일반식(Ⅸ)의 화합물을 할로겐화하는 단계; 및 c) 일반식(Ⅳ)의 화합물을 할로겐 교환에 의해 또 다른 일반식(Ⅳ)의 화합물로 전환시키는 단계를 포함하는, 제15항에서 정의된 일반식(Ⅳa)이 화합물의 제조방법.
  17. 치료제로 사용될 수 있는 하기 일반식(Ⅳb)의 화합물 또는 그것의 약학적 허용염:
    상기 식에서R19는 -CH2CH2-,CH2O-,-COH2-,-NHCH2- 또는 -CH2NH-이고: Y는 1,2,3 또는 4위치에 부착된 수소 또는 할로겐이며; Y'은 7,8,9 또는 10 위치에 부착된 수소 또는 할로겐이며; n은 0 또는 3이고 p 및 q 각각은 1 내지 4이며; 그리고 R20및 R21은 수소 또는 C1-4알킬로부터 각각 선택되거나 또는 질소원자와 함께 4내지 6원으로 구성된 질소-함유 헤테로사이클릭고리를 형성할수도 있으며, 단, R19가 -CH2CH2-, 또는-CH2O-이고, p와 q는 둘 모두 1이며 Y와 Y'은 각소 수소 또는 할로겐인 경우, n은 2가 아니어야한다.
  18. 일반식(Ⅳa) 또는 (Ⅳb)의 화합물 또는 그것의 약학적 허용염을 그것의 약학적 허용 담체와 함께 포함하는 약학적 제제.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019910701934A 1989-06-19 1990-06-18 암치료에 유용하며 항히스타민성 특성을 갖는 약물 KR920702620A (ko)

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GB898914062A GB8914062D0 (en) 1989-06-19 1989-06-19 Agents for potentiating the effects of antitumour agents and combating multiple drug resistance
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GB898914040A GB8914040D0 (en) 1989-06-19 1989-06-19 Agents for potentiating the effects of antitumour agents and combating multiple drug resistance
GB8914061.2 1989-06-19
GB898914060A GB8914060D0 (en) 1989-06-19 1989-06-19 Agents for potentiating the effects of antitumour agents and combating multiple drug resistance
GB898914061A GB8914061D0 (en) 1989-06-19 1989-06-19 Agents for potentiating the effects of antitumour agents and combating multiple drug resistance
PCT/GB1990/000935 WO1990015599A1 (en) 1989-06-19 1990-06-18 Medicaments useful in cancer therapy and having antihistaminic properties

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