KR960034202A - 전립선암의 치료 및 예방방법 - Google Patents

전립선암의 치료 및 예방방법 Download PDF

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KR960034202A
KR960034202A KR1019960007405A KR19960007405A KR960034202A KR 960034202 A KR960034202 A KR 960034202A KR 1019960007405 A KR1019960007405 A KR 1019960007405A KR 19960007405 A KR19960007405 A KR 19960007405A KR 960034202 A KR960034202 A KR 960034202A
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alkyl
octahydrobenzo
quinolin
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dimethyl
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에드먼드 오디아 제임스
리 누바우어 블레이크
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피터 지. 스트링거
일라이 릴리 앤드 캄파니
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Priority claimed from US08/407,822 external-priority patent/US5635197A/en
Priority claimed from US08/408,745 external-priority patent/US5629007A/en
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Publication of KR960034202A publication Critical patent/KR960034202A/ko

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Abstract

본 발명은 전립선암의 진행을 예방하거나, 또는 전립선암의 뼈로의 전이를 예방 또는 치료하는데 효과적인 약제인 일련의 벤조퀴놀린-3-온에 관한 것이다.

Description

전립선암의 치료 및 예방방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (7)

  1. 전립선암의 지행을 예방하거나, 또는 전립선암의 뼈로의 전이를 예방 또는 치료하는 약제를 제조하기 위한, 하기 일반식(Ⅰ)의 화합물 또는 (+)-(4aS)-(10bS)-8-클로로-4-메틸-1,2,3,4,4a,5,6,10b-옥타하이드벤조[f]퀴놀린-3-온; 또는 이들의 약학적으로 허용 가능한 염의 용도;
    상기 식에서 R 및 R1은 둘 다 수소이거나 또는 함께 단일결합을 형성하고; R2는 수소 또는 C1-C3알킬이고; R3은 수소, 메틸 또는 에틸이고; R4와 X-R5가 하기의 정의를 가지고 (R6)m이 존재하지 않으면, R3은 수소가 아니거나; 또는 (R6)m이 하기의 정의를 가지고 R4와 X-R5가 존재하지 않으면, R3은 에틸이 아니고; R4와 X-R5는 각각 7-, 8- 및 9-위치 중 하나를 차지하고; R4는 수소, 할로, 메틸 또는 에틸이고; X는 C1-C4알킬, C2-C4알케닐, C2-C4알키닐, 단일결합, -SO-, -SO2-, -CO-Y-(CH2)n-, -Y-CO-(CH2)n, -CO-, -Z-(CH2)n- 또는 -SO3-이고, 이 대 대칭이 아닌 X기는 둘 중 한 배향일 수 있고; Y는 -S-, -O- 또는 -NH-이고; Z는 -O- 또는 -S-이고; n은 O S내지 3이고; R3은 페닐, 나프탈레닐, 피리디닐, 피라지닐, 피리다지닐, 피리미디닐, 안트라세닐, 아세프탈레닐, 티아졸릴, 벤즈이미다졸릴, 인다졸릴, 테오페닐, 페난트레닐, 퀴놀리닐, 플루오로레닐, 이소퀴놀닐, 인다닐, 벤조피라닐, 인돌릴, 벤즈이소퀴리놀, 벤즈인돌릴, 벤조티아졸릴, 벤조니오페닐,퀴녹살리닐, 벤족사졸릴, 테트라졸릴, 나프토티아졸리, 퀴나졸리닐, 티아졸로피리디닐, 피리다지노퀴나졸리닐, 벤즈이소티아졸릴, 벤조디옥솔릴, 벤조디옥시닐, 디페닐메틸 또는 트리페닐메틸이고; 상기, R5기는 치환되지 않거나 또는 할로, 트리플루오로메틸, 트리플루오로에톡시, C1-C4알킬, 트리플루오로메톡시, 하이드록시, C1-C3알콕시, 니트로, C1-C3알킬티오, C1-C6아카노일, 페닐, 옥소, 페녹시, 페닐티오, C1-C3알킬설피닐, C1-C3알킬설포닐, 시아노, 아미노, C1-C3알킬아미노, 디페닐메틸아미노, 트리페닐메틸아미노, 벤질옥시, 벤질티오, (모노-할로, 니트로 또는 CF3)벤질(옥시 또는 티오), 디(C1-C3알킬, C3-C6사이클로알킬, 또는 C4-C8사이클로알킬알킬)아미노, (모노-C1-C3알킬, C1-C3알콕시 또는 할로)-(페닐, 페녹시, 페닐티오, 페닐설포닐 또는 페녹시설포닐), C2-C6알카노일아미노, 베노일아미노, 디페닐메틸아미노(C1-C3알킬), 아미노카보닐, C1-C3알킬아미노카보닐, 디(C1-C3알킬)아미노카보닐, 할로-C1-C6알카노일, 아미노설포닐, C1-C3알킬아미노설포닐, 디(C1-C3알킬)아미노설포닐, 페닐(옥시 또는 티오)(C1-C3알킬), (할로, C1-C3알킬 또는 C1-C3알콕시)페닐(옥시 또는 티오)(C1-C3알킬), 벤조일, 또는 (아미노, C1-C3알킬아미노 또는 디(C1-C3알킬)아미노)(C1-C3알킬)로 구성된 그룹 중에서 선택되는 1 내지 3개의 기로 치환되거나; 또는 상기 R5기는 모폴리노(C1-C3알킬)기, 페닐(C1-C3알킬)피페리디닐 기, 페닐(C1-C3알킬)피페리디닐아미노카보닐 기, C2-C6알카노일아미노티오페닐 기 또는 (아미노, C1-C3알킬아미노 또는 디(C1-C3알킬)아미노)나프탈레닐설포닐아미노 기로 치환되거나; 또는 R5는 과할로페닐 기이고; m은 1 또는 2이고; R6은 수소, 할로겐, NO2, 시아노, CF3, C1-C6알킬, C1-C6알콕시, 카복시, C1-C6알콕시카보닐, 아미노, C1-C4알킬아미노, C1-C4디알킬아미노, 아미도, C1-C4알킬아미도, C1-C4디알킬아미도, 메르캅토, C1-C6알킬티오, C1-C6알킬설피닐, C1-C6알킬설포닐, 또는 A-R7이며, 이때는 A는 C1-C6알킬렌, C2-C6알케닐렌 또는 C2-C6알키닐렌이고; R7은 할로겐, 하이드록시, CF3, C1-C6알콕시, 카복시, C1-C6알콕시카보닐, 아미노, C1-C4알킬아미노, C1-C4디알킬아미노, 아미도, C1-C4알킬아미도, C1-C4디알킬아미도, C1-C4알킬설포닐아미노, 아미노설포닐 또는 C1-C4알킬아미노설포닐이다.
  2. 제1항에 있어서, 상기 약제가 양성 전립선 과형성증을 앓고 있거나; 전립선암의 병력이 있거나; 비정상적으로 고농도의 순환 전립선 특이성 항체를 가지거나; 또는 전립선 세포에 신생물성 이상증이 있는 환자의 전립선암의 진행을 예방하기 위한 용도.
  3. 제1항 또는 제2항에 있어서, 상기 화합물이 (-)-(4aR)-(10bR)-8-클로로-4-메틸-1,2,3,4,4a,5,6,10b-옥타하이드로벤조[f]퀴놀린-3-온; (+)-(4aR)-(10bR)-8-클로로-4,10b-디메틸-1,2,3,4,4a,5,6,10b-옥타하이드로벤조[f]퀴놀린-3-온; 8-클로로-4,10b-디메틸-1,2,3,4,4a,5,6,10b-옥타하이드로벤조[f]퀴놀린-3-온; (+)-(4aR)-(10bR)-8,9-디클로로-4,10b-디메틸-1,2,3,4,4a,5,6,10b-옥타하이드로벤조[f]퀴놀린-3-온; (+)-(4aR)-(10bR)-4,10b-디메틸-8-(2-페닐에틸)-1,2,3,4,4a,5,6,10b-옥타하이드로벤조[f]퀴놀린-3-온; (+)-(4aR)-(10bR)-8-벤질티오-4,10b-디메틸-1,2,3,4,4a,5,6,10b-옥타하이드로벤조[f]퀴놀린-3-온; (+)-(4aR)-(10bR)-8-클로로-4-메틸-1,2,3,4,4a,5,6,10b-옥타하이드로벤조[f]퀴놀린-3-온; 또는 이들의 약학적으로 허용가능한 염인 농도.
  4. 제1항에 있어서, 상기 약제가 전립선암의 뼈로의 전이를 치료 또는 예방하기 위한 것인 용도.
  5. 제4항에 있어서, 상기 약제가 뼈의 전이성 병변을 치료하기 위한 것인 용도.
  6. 제4항에 있어서, 상기 약제가 아직 뼈로 전이되지 않은 전립선암을 앓고 있는 환자의 뼈로의 전이를 예방하기위한 것인 용도.
  7. 제4항 내지 제6항중 어느 한 항에 있어서, 상기 화합물이 (-)-(4aR)-(10bR)-8-클로로-4-메틸-1,2,3,4,4a,5,6,10b-옥타하이드로벤조[f]퀴놀린-3-온; (+)-(4aR)-(10bR)-8-클로로-4,10b-디메틸-1,2,3,4,4a,5,6,10b-옥타하이드로벤조[f]퀴놀린-3-온; 8-클로로-4,10b-디메틸-1,2,3,4,4a,5,6,10b-옥타하이드로벤조[f]퀴놀린-3-온; (+)-(4aR)-(10bR)-8,9-디클로로-4,10b-디메틸-1,2,3,4,4a,5,6,10b-옥타하이드로벤조[f]퀴놀린-3-온; (+)-(4aR)-(10bR)-4,10b-디메틸-8-(2-페닐에틸)-1,2,3,4,4a,5,6,10b-옥타하이드로벤조[f]퀴놀린-3-온; (+)-(4aR)-(10bR)-4,10b-디메틸-8-(2-페닐에틸)-1,2,3,4,4a,5,6,10b-옥타하이드로벤조[f]퀴놀린-3-온; (+)-(4aR)-(10bR)-8-벤질티오-4,10b-디메틸-1,2,3,4,4a,5,6,10b-옥타하이드로벤조[f]퀴놀린-3-온; 또는 (+)-(4aR)-(10bR)-8-클로로-4-메틸-1,2,3,4,4a,5,6,10b-옥타하이드로벤조[f]퀴놀린-3-온; 또는 이들의 약학적으로 허용가능한 염인 농도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960007405A 1995-03-21 1996-03-19 전립선암의 치료 및 예방방법 KR960034202A (ko)

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US08/408,745 1995-03-21
US08/407,822 1995-03-21
US08/407,822 US5635197A (en) 1995-03-21 1995-03-21 Treatment and prevention of prostatic cancer metastasis
US08/408,745 US5629007A (en) 1995-03-21 1995-03-21 Method of preventing prostatic cancer development

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US5550134A (en) * 1995-05-10 1996-08-27 Eli Lilly And Company Methods for inhibiting bone loss
ZA979612B (en) * 1996-10-30 1999-04-28 Lilly Co Eli Synthesis of benzo(f)quinolinones
US6111110A (en) * 1996-10-30 2000-08-29 Eli Lilly And Company Synthesis of benzo[f]quinolinones
AU754604B2 (en) * 1998-07-29 2002-11-21 Merck & Co., Inc. Tricyclic compounds
US6436489B1 (en) 1999-03-24 2002-08-20 Clariant International Ltd. Fluorine-containing benzothiazoles, and their use in liquid-crystalline mixtures
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