KR20090007651A - 5ht2c 수용체 조절제 - Google Patents
5ht2c 수용체 조절제 Download PDFInfo
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- KR20090007651A KR20090007651A KR1020097000060A KR20097000060A KR20090007651A KR 20090007651 A KR20090007651 A KR 20090007651A KR 1020097000060 A KR1020097000060 A KR 1020097000060A KR 20097000060 A KR20097000060 A KR 20097000060A KR 20090007651 A KR20090007651 A KR 20090007651A
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- tetrahydro
- benzazine
- methyl
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- IHRBUEKNYVJQIC-UHFFFAOYSA-N CC(C)C(CNCCc1c2)c1cc(Br)c2OC Chemical compound CC(C)C(CNCCc1c2)c1cc(Br)c2OC IHRBUEKNYVJQIC-UHFFFAOYSA-N 0.000 description 1
- WBGUZBYKIJAQIY-UHFFFAOYSA-N CC(CNCCc1c2)c1cc(C(C(F)(F)F)(F)F)c2OC Chemical compound CC(CNCCc1c2)c1cc(C(C(F)(F)F)(F)F)c2OC WBGUZBYKIJAQIY-UHFFFAOYSA-N 0.000 description 1
- FIODSXIEFAJLSL-UHFFFAOYSA-N CC(CNCCc1c2)c1ccc2-c1c(C(F)(F)F)cccc1 Chemical compound CC(CNCCc1c2)c1ccc2-c1c(C(F)(F)F)cccc1 FIODSXIEFAJLSL-UHFFFAOYSA-N 0.000 description 1
- RYYXCFYKJMRFPZ-UHFFFAOYSA-N CCC(CNCCc1c2)c1cc(I)c2OC Chemical compound CCC(CNCCc1c2)c1cc(I)c2OC RYYXCFYKJMRFPZ-UHFFFAOYSA-N 0.000 description 1
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Abstract
Description
체질량 지수 (BMI)에 의한 체중의 분류 | |
BMI | 분류 |
<18.5 | 저체중 |
18.5 - 24.9 | 정상 |
25.0 - 29.9 | 과체중 |
30.0 - 34.9 | 비만 (등급 I) |
35.0 - 39.9 | 비만 (등급 II) |
>40 | 극도 비만 (등급 III) |
Claims (48)
- 하기 화학식 I의 화합물의 용매화물 또는 하기 화학식 I의 화합물의 제약학적으로 허용되는 염의 용매화물.<화학식 I>상기 식에서,R1은 H 또는 C1 -8 알킬이고;R2는 C1 -8 알킬, -CH2-O-C1 -8 알킬, -OH 또는 -CH2OH이고;R2a는 H이거나;R2 및 R2a는 함께 -CH2-CH2-를 형성하고;R3은 할로겐, C1 -8 퍼할로알킬, CN, SR5, NHR5, N(R5)2, 아릴 또는 헤테로아릴이고, 상기 아릴은 C1 -8 알킬, 할로겐, C1 -8 퍼할로알킬 및 C1 -8 알콕시로부터 선택된 2개 이하의 치환기로 치환될 수 있고, 상기 헤테로아릴은 할로겐 및 C1 -8 알킬로부터 선택된 2개 이하의 치환기로 치환될 수 있고;R4는 H, 할로겐, C1 -8 퍼할로알킬, CN, OR5, SR5, NHR5, N(R5)2, OH, 아릴 또는 헤테로아릴이고, 상기 아릴은 C1 -8 알킬, 할로겐, C1 -8 퍼할로알킬 및 C1 -8 알콕시로부터 선택된 2개 이하의 치환기로 치환될 수 있고, 상기 헤테로아릴은 할로겐 및 C1 -8 알킬로부터 선택된 2개 이하의 치환기로 치환될 수 있거나;R3 및 R4는 이들이 부착된 원자와 함께 1개의 O 원자를 갖는 5 또는 6원 헤테로시클릭 고리를 형성할 수 있고;각각의 R5는 독립적으로 C1 -8 알킬, C2 -8 알케닐, 아릴, 헤테로아릴, 아릴C1 - 8알킬, 헤테로아릴C1 - 8알킬, C1 -8 퍼할로알킬 또는 알릴이고;R6은 H 또는 C1 -8 알킬이되, 단R6이 H 이외의 것일 경우, R4는 H일 수 없고;R1 및 R2가 메틸이고, R4가 H일 경우, R3은 NHR5 또는 N(R5)2일 수 없고;R1 및 R2가 메틸이고, R4가 H일 경우, R3은 이미다졸, 치환된 이미다졸 또는 이미다졸 유도체일 수 없으며;여기서, "아릴"은 3 내지 14개의 탄소 원자를 가진 모노시클릭 또는 폴리시클릭 방향족기를 나타내고, "헤테로아릴"은 O, N 또는 S와 같은 1 내지 4개의 비탄소 원자를 포함하는 아릴기를 나타내고, "아릴C1 - 8알킬"은 아릴 치환기를 포함하는 C1-8 알킬을 나타내고, "헤테로아릴C1 - 8알킬"은 헤테로아릴 치환기를 포함하는 C1 -8 알킬을 나타내고, "치환된 이미다졸"은 하나 이상의 치환기를 포함하는 이미다졸로부 터 유도된 라디칼을 나타내고, "이미다졸 유도체"는 융합된 고리들 중 하나가 이미다졸인 융합된 고리계를 나타낸다.
- 제1항에 있어서, R1이 H인 용매화물.
- 제1항에 있어서, R1이 C1 -8 알킬인 용매화물.
- 제1항에 있어서, R1이 메틸, 에틸 또는 n-프로필인 용매화물.
- 제1항에 있어서, R1이 메틸인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R2가 C1 -8 알킬인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R2가 메틸, 에틸, n-프로필 또는 이소프로필인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R2가 메틸 또는 에틸인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R2 및 R2a가 함께 -CH2-CH2-를 형성하는 것인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R3이 할로겐인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R3이 염소인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R3이 브롬인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R3이 C1 -8 퍼할로알킬인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R3이 CF3인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R3이 O, N 및 S로부터 선택된 2개 이하의 헤테로원자를 갖는 5원 헤테로아릴 고리인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R3이 티에닐, 푸라닐, 피롤릴, 피라졸릴 및 이미다졸릴로 이루어지는 군으로부터 선택된 것인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R4가 C1 -8 퍼할로알킬인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R4가 CF3인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R4가 -OR5인 용매화물.
- 제19항에 있어서, R5가 메틸, 에틸, n-프로필, 이소프로필 또는 알릴인 용매화물.
- 제19항에 있어서, R5가 메틸 또는 알릴인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R4가 O, N 및 S로부터 선택된 2개 이하의 헤테로원자를 갖는 5원 헤테로아릴 고리이고, 상기 헤테로아릴은 할로겐 및 C1 -8 알킬로부터 선택된 1 또는 2개의 치환기로 치환될 수 있는 것인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R4가 할로겐 및 메틸로부터 선택 된 1 또는 2개의 치환기로 치환될 수 있는, 티에닐, 푸라닐, 피롤릴, 피라졸릴 및 이미다졸릴로 이루어지는 군으로부터 선택된 것인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R4가 C1 -8 알킬, 할로겐 및 C1 -8 알콕시로부터 선택된 2개 이하의 치환기로 치환될 수 있는 페닐인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R3 및 R4가 함께 -O-CH=C(CH3)-를 형성하는 것인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R3이 할로겐이고, R4가 -OR5이고, R5가 C1 -8 알킬인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R3이 염소이고, R4가 -OR5이고, R5가 C1 -8 알킬인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R3이 브롬이고, R4가 -OR5이고, R5가 C1 -8 알킬인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R3이 요오드이고, R4가 -OR5이고, R5가 C1 -8 알킬인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R3이 할로겐이고, R4가 메톡시인 용매화물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, R3이 할로겐이고, R4가 알릴옥시인 용매화물.
- 제1항에 있어서,R2가 메틸, 에틸, 이소프로필 또는 CH2OH이거나; R2 및 R2a가 함께 -CH2-CH2-를 형성하고;R3이 할로겐이거나, 또는 O, N 및 S로부터 선택된 2개 이하의 헤테로원자를 포함하고 할로겐 및 C1 -8 알킬로부터 선택된 2개 이하의 치환기를 갖는 5원 헤테로아릴 고리이고;R4가 H; C1 -8 알콕시; O, N 및 S로부터 선택된 2개 이하의 헤테로원자를 포함하고 할로겐 및 C1 -8 알킬로부터 선택된 2개 이하의 치환기를 갖는 5원 헤테로아릴 고리; 또는 C1 -8 알킬, 할로겐 및 C1 -8 알콕시로부터 선택된 2개 이하의 치환기로 치환될 수 있는 페닐이거나;R3 및 R4가 함께 -O-CH=C(CH3)-를 형성하고;R6이 H 또는 메틸인 용매화물.
- 제1항에 있어서,R2가 메틸, 에틸, 이소프로필 또는 CH2OH이거나; R2 및 R2a가 함께 -CH2-CH2-를 형성하고;R3이 염소, 브롬 또는 요오드이고;R4가 H 또는 C1 -8 알콕시이고;R6이 H 또는 메틸인 용매화물.
- 제1항에 있어서,R1이 H이고;R2가 메틸이고;R3이 염소, 브롬 또는 티오펜이고;R4가 H, C1 -8 알콕시, 피라졸-3-일 또는 페닐이고, 상기 피라졸-3-일은 할로 겐 및 C1 -8 알킬로부터 선택된 2개 이하의 치환기로 치환될 수 있고, 상기 페닐은 1개의 할로겐 치환기로 치환될 수 있고;R6이 H인 용매화물.
- 제1항에 있어서,8-브로모-7-히드록시-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;7-알릴옥시-8-브로모-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;7-벤질옥시-8-브로모-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-브로모-7-에톡시-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-브로모-7-이소프로폭시-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;N-프로필-8-브로모-7-메톡시-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;7-히드록시-8-요오도-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;7-알릴옥시-8-요오도-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;3,5-디메틸-6,7,8,9-테트라히드로-5H-1-옥사-7-아자-시클로헵타인덴;7-알릴옥시-8-클로로-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;7-메톡시-1-메틸-8-(2-티에닐)-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-시아노-7-메톡시-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-브로모-1-시클로프로필-7-메톡시-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-브로모-1-히드록시메틸-7-메톡시-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-브로모-1-이소프로필-7-메톡시-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-브로모-7-히드록시-1-이소프로필-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;7-알릴옥시-8-브로모-1-이소프로필-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-브로모-7-메톡시-1,4-디메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;7-알릴옥시-8-브로모-1,4-디메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-클로로-1-히드록시-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-플루오로-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;7,8-디클로로-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;N-메틸-8-클로로-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-요오도-1-메틸-7-트리플루오로메톡시-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;N-프로필-8-요오도-7-메톡시-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;1-에틸-8-요오도-7-메톡시-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;7-(2-플루오로페닐)-8-클로로-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-(2-클로로페닐)-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀; 및8-브로모-1-메톡시메틸-7-메톡시-2,3,4,5-테트라히드로-1H-3-벤즈아제핀으로 이루어지는 군으로부터 선택되는 화학식 I의 화합물의 용매화물 또는 화학식 I의 화합물의 제약학적으로 허용되는 염의 용매화물.
- 제1항에 있어서,8-브로모-7-메톡시-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-클로로-7-메톡시-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-요오도-7-메톡시-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;N-메틸-8-브로모-7-메톡시-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-브로모-1-에틸-7-메톡시-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-클로로-1-에틸-7-메톡시-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-요오도-1-에틸-7-메톡시-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;7-메톡시-1-메틸-8-트리플루오로메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀; 및7-메톡시-1-메틸-8-펜타플루오로에틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀으로 이루어지는 군으로부터 선택되는 화학식 I의 화합물의 용매화물 또는 화학식 I의 화합물의 제약학적으로 허용되는 염의 용매화물.
- 제1항에 있어서,8-브로모-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-요오도-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-트리플루오로메틸-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-트리플루오로메틸-1-에틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-클로로-1-에틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-브로모-1-에틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-요오도-1-에틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;7,8-디클로로-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;7,8-디클로로-1-에틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀;8-클로로-7-플루오로-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀; 및8-클로로-7-플루오로-1-에틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀으로 이루어지는 군으로부터 선택되는 화학식 I의 화합물의 용매화물 또는 화학식 I의 화합물의 제약학적으로 허용되는 염의 용매화물.
- 제1항에 있어서, 8-클로로-1-메틸-2,3,4,5-테트라히드로-1H-3-벤즈아제핀의 화학식 I의 화합물의 용매화물 또는 화학식 I의 화합물의 제약학적으로 허용되는 염의 용매화물.
- 제38항에 있어서, R 거울상 이성질체인 용매화물.
- 제38항에 있어서, S 거울상 이성질체인 용매화물.
- 제38항에 있어서, R 및 S 거울상 이성질체의 혼합물인 용매화물.
- 유효량의 제1항 내지 제5항 및 제32항 내지 제41항 중 어느 한 항에 따른 용 매화물 및 제약학적으로 허용되는 담체 또는 부형제를 포함하는, 요붕증 또는 수면 무호흡의 예방 또는 치료용 제약 조성물.
- 유효량의 제1항 내지 제5항 및 제32항 내지 제41항 중 어느 한 항에 따른 용매화물 및 제약학적으로 허용되는 담체 또는 부형제를 포함하는, 우울증, 비정형 우울증, 양극성 장애, 불안 장애, 강박 장애, 사회 공포증 또는 공황 상태, 수면 장애, 성기능 장애, 정신병, 정신분열증, 편두통, 및 두통 또는 다른 통증과 관련된 다른 증상, 두개내압 상승, 간질, 인격 장애, 연령 관련 행동 장애, 치매와 관련된 행동 장애, 기질성 정신 장애, 소아 정신 장애, 공격증, 연령 관련 기억 장애, 만성 피로 증후군, 약물 및 알코올 중독, 비만, 대식증, 신경성 식욕부진증 또는 월경전 긴장의 예방 또는 치료용 제약 조성물.
- 유효량의 제1항 내지 제5항 및 제32항 내지 제41항 중 어느 한 항에 따른 용매화물 및 제약학적으로 허용되는 담체 또는 부형제를 포함하는, 비만의 예방 또는 치료용 제약 조성물.
- 유효량의 제1항 내지 제5항 및 제32항 내지 제41항 중 어느 한 항에 따른 용매화물 및 제약학적으로 허용되는 담체 또는 부형제를 포함하는, 외상, 뇌졸중, 신경퇴행성 질환, 또는 독성 또는 감염성 CNS 질환에 의한 중추 신경계에 대한 손상의 예방 또는 치료용 제약 조성물.
- 제45항에 있어서, 상기 독성 또는 감염성 CNS 질환이 뇌염 또는 수막염인 제약 조성물.
- 유효량의 제1항 내지 제5항 및 제32항 내지 제41항 중 어느 한 항에 따른 용매화물 및 제약학적으로 허용되는 담체 또는 부형제를 포함하는, 혈전증의 예방 또는 치료용 제약 조성물.
- 유효량의 제1항 내지 제5항 및 제32항 내지 제41항 중 어느 한 항에 따른 용매화물 및 제약학적으로 허용되는 담체 또는 부형제를 포함하는, 위장관 운동 기능장애의 예방 또는 치료용 제약 조성물.
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KR20190133482A (ko) | 2018-05-23 | 2019-12-03 | 동국제약 주식회사 | 흰강낭콩 및 아위버섯 추출물을 함유하는 항비만 또는 체지방 감소용 조성물 |
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