KR20050094849A - 디펩티딜 펩티다아제 iv를 저해하는 화합물 - Google Patents
디펩티딜 펩티다아제 iv를 저해하는 화합물 Download PDFInfo
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Abstract
Description
중간체 실시예 | 화합물명 | ESI/MS(m/z) |
6 | 3-(2'-클로로아세틸)티아졸리딘 | 166 (M+H)+164 (M-H)- |
7 | 1-(2'-클로로아세틸)피롤리딘 | 148 (M+H)+146 (M-H)- |
8 | 1-(2'-클로로아세틸)피페라진-2-카르보니트릴 | 187 (M+H)+185 (M-H)- |
9 | 1-(2'-클로로아세틸)모르폴린 | 164 (M+H)+162 (M-H)- |
Claims (10)
- 하기 화학식(I)로 표시되는 화합물, 또는 그의 의약적으로 허용되는 염인 화합물:(I)식중에서,R1 및 R2는 동시에 또는 개별적으로 수소원자, 치환되어 있어도 좋은 C1-6 알킬기 또는 -COOR5를 나타내거나, 또는 R1 및 R2 가 이들이 부착된 탄소원자와 합쳐져서 3~6원 시클로알킬기를 나타내며,R5 는 수소원자, 또는 치환되어 있어도 좋은 C1-6 알킬기를 나타내고,R3은 수소원자, 또는 치환되어 있어도 좋은 C6-10 아릴기를 나타내며,R4 는 수소원자, 또는 시아노기를 나타내며,D는 -CONR6-, -CO-, 또는 -NR6CO- 를 나타내고,R6 은 수소원자, 또는 치환되어 있어도 좋은 C1-6 알킬기를 나타내며,E는 -(CH2)m- (m은 1~3의 정수임), -CH2OCH2- 또는 -SCH2- 를 나타내고,n은 0~3의 정수를 나타내며,A는 치환되어 있어도 좋은 비시클릭 헤테로시클릭 기, 또는 비시클릭 탄화수소기를 나타냄.
- 제 1항에 있어서, 화학식(I) 중의 A가 치환되어 있어도 좋은 비시클릭 헤테로시클릭 기이고, 상기 비시클릭 헤테로시클릭 기가 질소, 산소, 황 원자중 적어도 1개의 헤테로 원자를 포함하며, 6-5계의 비시클릭 헤테로시클릭기인 화합물.
- 제 2항에 있어서, 화학식(I) 중의 R1 및 R2가 메틸기이고, R3 이 수소원자이며, R4는 시아노 기이고, D가 -CONH- 또는 -CO-이며, E가 -CH2CH2-이며, n이 1 또는 2인 화합물.
- 제 3항에 있어서, 화학식(I) 중의 D가 -CO-이고, A가 하기 화학식(II)로 표시되는 6-5계의 비시클릭의 지환식 헤테로시클릭 기인 화합물:(II)식중에서, x는 0~2의 정수를 나타내고, R7, R8, R9 및 R10은 동시에 또는 개별적으로 수소원자, 할로겐 원자, 히드록시 기, 트리플루오로메틸 기, 치환되어 있어도 좋은 C1-6 알킬기 또는 치환되어 있어도 좋은 C1-6 알콕시 기를 나타냄.
- 제 3항에 있어서, 화학식(I) 중의 D가 -CONH- 이고, A가 하기 화학식(III)으로 표시되는 6-5계의 비시클릭 헤테로시클릭 기인 화합물:(III)식중에서, 는 단일결합 또는 이중결합을 나타내고, y, z, v, w의 적어도 1개는 산소, 질소, 황 원자중의 어느 하나이며, R11, R12 및 R13은 고리 상의 어느 수소원자에 치환되어 있어도 좋고, 동시에 또는 개별적으로 수소원자, 히드록시 기, 트리플루오로메틸 기, 트리플루오로아세틸 기, 옥소 기, 치환되어 있어도 좋은 C1-6 알킬기, 치환되어 있어도 좋은 C1-6 알콕시 기 또는 치환되어 있어도 좋은 C6-10 아릴 기를 나타냄.
- 제 5항에 있어서, 화학식(III) 중의 y, z, v, w 내의 1~3개가 질소원자이고, 나머지가 탄소원자인 화합물.
- 제 2항 내지 제 6항 중 어느 한 항에 기재된 화합물을 유효성분으로 하는 디펩티딜 펩티다아제 IV 활성의 저해제.
- 제 7항에 있어서, 당뇨병 치료를 위한 디펩티딜 펩티다아제 IV 활성의 저해제.
- 제 7항에 있어서, 당뇨병 합병증 치료를 위한 디펩티딜 펩티다아제 IV 활성의 저해제.
- 제 2항 내지 제 6항 중 어느 한 항에 기재된 화합물을 유효성분으로 함유하는 의약조성물.
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EP (1) | EP1595866B1 (ko) |
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JP4184378B2 (ja) | 2008-11-19 |
AU2004207731A1 (en) | 2004-08-12 |
CA2514191A1 (en) | 2004-08-12 |
EP1595866B1 (en) | 2016-06-08 |
EP1595866A1 (en) | 2005-11-16 |
CA2514191C (en) | 2011-10-11 |
EP1595866A4 (en) | 2009-03-04 |
KR100998796B1 (ko) | 2010-12-06 |
CN100434420C (zh) | 2008-11-19 |
AU2004207731B2 (en) | 2009-08-13 |
DK1595866T3 (en) | 2016-08-22 |
PT1595866T (pt) | 2016-09-14 |
US20060229286A1 (en) | 2006-10-12 |
US7345180B2 (en) | 2008-03-18 |
ES2587885T3 (es) | 2016-10-27 |
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JPWO2004067509A1 (ja) | 2006-05-18 |
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