KR20080075055A - 안지오텐신 수용체 길항제 및 nep 억제제의 제약 조합물 - Google Patents
안지오텐신 수용체 길항제 및 nep 억제제의 제약 조합물 Download PDFInfo
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- KR20080075055A KR20080075055A KR1020077015021A KR20077015021A KR20080075055A KR 20080075055 A KR20080075055 A KR 20080075055A KR 1020077015021 A KR1020077015021 A KR 1020077015021A KR 20077015021 A KR20077015021 A KR 20077015021A KR 20080075055 A KR20080075055 A KR 20080075055A
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Abstract
Description
Claims (85)
- (a) 안지오텐신 수용체 길항제;(b) 중성 엔도펩티다제 억제제 (NEPi); 및 임의로(c) 제약상 허용되는 양이온을 포함하는 이중-작용 화합물.
- 제1항에 있어서, 복합체 형태의 화합물.
- 제2항에 있어서, 초분자 복합체 형태의 화합물.
- 제1항 내지 제3항 중 어느 한 항에 있어서, 안지오텐신 수용체 길항제 및 NEPi가 비-공유 결합을 통해 연결된 것인 화합물.
- 제1항 내지 제4항 중 어느 한 항에 있어서, 안지오텐신 수용체 길항제 및 NEPi가 제약상 허용되는 양이온을 통해 연결된 것인 화합물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, 안지오텐신 수용체 길항제가 발사르탄, 로사르탄, 이르베사르탄, 텔미사르탄, 에프로사르탄, 칸데사르탄, 올메사르탄, 및 이들의 조합으로 이루어진 군으로부터 선택된 것인 화합물.
- 제6항에 있어서, 안지오텐신 수용체 길항제가 발사르탄인 화합물.
- 제1항 내지 제8항 중 어느 한 항에 있어서, NEPi가 (3S,2'R)-3-{1-[2'-(에톡시카르보닐)-4'-페닐-부틸]-시클로펜탄-1-카르보닐아미노}-2,3,4,5-테트라히드로-2-옥소-1H-1-벤즈아제핀-1-아세트산 또는 그의 제약상 허용되는 염인 화합물.
- 제1항 내지 제9항 중 어느 한 항에 있어서, 양이온이 Na, K 및 NH4로 이루어진 군으로부터 선택된 것인 화합물.
- 제10항에 있어서, 제약상 허용되는 양이온이 Na인 화합물.
- 제1항 내지 제11항 중 어느 한 항에 있어서, 결정질, 부분 결정질, 무정형, 또는 다형 형태, 바람직하게는 결정질 형태의 화합물.
- 제1항 내지 제12항 중 어느 한 항에 있어서, 용매화물 형태의 화합물.
- 제13항에 있어서, 수화물 형태의 화합물.
- 제1항 내지 제14항 중 어느 한 항에 있어서, 안지오텐신 수용체 길항제 및 중성 엔도펩티다제 억제제가 1:1의 몰 비율로 존재하는 것인 화합물.
- 제1항 내지 제15항 중 어느 한 항에 있어서, 안지오텐신 수용체 길항제, 중성 엔도펩티다제 억제제 및 양이온이 1:1:3의 몰 비율로 존재하는 것인 화합물.
- 제1항 내지 제16항 중 어느 한 항에 있어서, 총 화학식 [ARB(NEPi)]Na1-3· xH2O (여기서, x는 0 내지 3, 예를 들어 2.5임)을 갖는 화합물.
- 제1항 내지 제17항 중 어느 한 항에 있어서, 총 화학식 (N-발레릴-N-{[2'- (1H-테트라졸-5-일)-비페닐-4-일]-메틸}-발린) (5-비페닐-4-일-5-(3-카르복시-프로피오닐아미노)-2-메틸-펜탄산 에틸 에스테르]Na3·x H2O (여기서, x는 0 내지 3임)을 갖는 화합물.
- 제18항에 있어서, 총 화학식 [((S)-N-발레릴-N-{[2'-(1H-테트라졸-5-일)-비페닐-4-일]-메틸}-발린) ((2R,4S)-5-비페닐-4-일-5-(3-카르복시-프로피오닐아미노)-2-메틸-펜탄산 에틸 에스테르]Na3·x H2O (여기서, x는 0 내지 3임)을 갖는 화합물.
- 제18항 또는 제19항에 있어서, x가 2.5인 화합물.
- 제18항 내지 제20항 중 어느 한 항에 있어서, 상반 파동수 (cm-1)(±2 cm-1)로 표현되는 하기 흡수 밴드를 갖는 감쇠 총 반사 푸리에 변환 적외선 (ATR-FTIR) 스펙트럼을 특징으로 하는 화합물: 2956 (w), 1711 (st), 1637 (st), 1597 (st), 1488 (w), 1459 (m), 1401 (st), 1357 (w), 1295 (m), 1266 (m), 1176 (w), 1085 (m), 1010 (w), 1942 (w), 907 (w), 862 (w), 763 (st), 742 (m), 698 (m), 533 (st).
- 제18항 내지 제21항 중 어느 한 항에 있어서, 하기 상호격자 평면 간격 ([Å] 단위의 d) (±0.1 Å)을 포함하는 신태그(Scintag) XDS2000 분말 회절계로 취해진 X-선 분말 회절 패턴을 특징으로 하는 화합물: 21.2(s), 17.0(w), 7.1(s), 5.2(w), 4.7(w), 4.6(w), 4.2(w), 3.5(w), 3.3(w).
- (i) 안지오텐신 수용체 길항제 및 중성 엔도펩티다제 억제제 (NEPi)를 적합한 용매에 용해시키는 단계;(ii) Cat (여기서, Cat는 양이온임)의 염기성 화합물을 적합한 용매에 용해시키는 단계;(iii) 단계 (i) 및 (ii)에서 수득된 용액을 배합하는 단계;(iv) 고체를 침전시키고, 이를 건조시켜 이중-작용 화합물을 수득하는 단계; 또는 별법으로(iva) 생성된 용액을 증발 건조시키고;(va) 고체를 적합한 용매에 재-용해시키고;(via) 고체를 침전시키고, 이를 건조시켜 이중-작용 화합물을 수득하는 것에 의해, 단계 (i) 및 (ii)에서 사용된 용매(들)를 교환함으로써 이중-작용 화합물을 수득하는 단계에 의해 수득가능한 이중-작용 화합물.
- 제23항에 있어서, 복합체 형태의 화합물.
- 제24항에 있어서, 초분자 복합체 형태의 화합물.
- 제23항 내지 제25항 중 어느 한 항에 있어서, 단계 (i) 및 (iv)에서의 적합한 용매가 아세톤인 화합물.
- 제23항 내지 제26항 중 어느 한 항에 있어서, (Cat)의 염기성 화합물이 (Cat)OH, (Cat)2CO3, (Cat)HCO3, CatOMe, CatOAc 또는 CatOCHO인 화합물.
- 제23항 내지 제27항 중 어느 한 항에 있어서, 안지오텐신 수용체 길항제가 발사르탄, 로사르탄, 이르베사르탄, 텔미사르탄, 에프로사르탄, 칸데사르탄, 올메사르탄, 및 이들의 조합으로 이루어진 군으로부터 선택된 것인 화합물.
- 제28항에 있어서, 안지오텐신 수용체 길항제가 발사르탄인 화합물.
- 제23항 내지 제29항 중 어느 한 항에 있어서, NEPi가 (3S,2'R)-3-{1-[2'-(에톡시카르보닐)-4'-페닐-부틸]-시클로펜탄-1-카르보닐아미노}-2,3,4,5-테트라히드로-2-옥소-1H-1-벤즈아제핀-1-아세트산 또는 그의 제약상 허용되는 염인 화합물.
- 제23항 내지 제31항 중 어느 한 항에 있어서, Cat가 Na, K 및 NH4로 이루어진 군으로부터 선택된 것인 화합물.
- 제32항에 있어서, Cat가 Na인 화합물.
- 제23항 내지 제33항 중 어느 한 항에 있어서, 결정질, 부분 결정질, 무정형, 또는 다형 형태, 바람직하게는 결정질 형태의 화합물.
- 제23항 내지 제34항 중 어느 한 항에 있어서, 용매화물 형태의 화합물.
- 제35항에 있어서, 수화물 형태의 화합물.
- 제23항 내지 제36항 중 어느 한 항에 있어서, 안지오텐신 수용체 길항제 및 중성 엔도펩티다제 억제제가 1:1의 몰 비율로 존재하는 것인 화합물.
- 제23항 내지 제37항 중 어느 한 항에 있어서, 안지오텐신 수용체 길항제, 중성 엔도펩티다제 억제제 및 양이온이 1:1:3의 몰 비율로 존재하는 것인 화합물.
- 제21항 내지 제36항 중 어느 한 항에 있어서, 총 화학식 [ARB(NEPi)]Na1-3· xH2O (여기서, x는 0 내지 3, 예를 들어 2.5임)을 갖는 화합물.
- 제21항 내지 제37항 중 어느 한 항에 있어서, 총 화학식 (N-발레릴-N-{[2'-(1H-테트라졸-5-일)-비페닐-4-일]-메틸}-발린) (5-비페닐-4-일-5-(3-카르복시-프로피오닐아미노)-2-메틸-펜탄산 에틸 에스테르]Na3·x H2O (여기서, x는 0 내지 3임)을 갖는 화합물.
- 제38항에 있어서, 총 화학식 [((S)-N-발레릴-N-{[2'-(1H-테트라졸-5-일)-비페닐-4-일]-메틸}-발린) ((2R,4S)-5-비페닐-4-일-5-(3-카르복시-프로피오닐아미 노)-2-메틸-펜탄산 에틸 에스테르]Na3·x H2O (여기서, x는 0 내지 3임)을 갖는 화합물.
- 제38항 또는 제39항에 있어서, x가 2.5인 화합물.
- 제38항 내지 제40항 중 어느 한 항에 있어서, 상반 파동수 (cm-1)(±2 cm-1)로 표현되는 하기 흡수 밴드를 갖는 감쇠 총 반사 푸리에 변환 적외선 (ATR-FTIR) 스펙트럼을 특징으로 하는 화합물: 2956 (w), 1711 (st), 1637 (st), 1597 (st), 1488 (w), 1459 (m), 1401 (st), 1357 (w), 1295 (m), 1266 (m), 1176 (w), 1085 (m), 1010 (w), 1942 (w), 907 (w), 862 (w), 763 (st), 742 (m), 698 (m), 533 (st).
- 제38항 내지 제41항 중 어느 한 항에 있어서, 하기 상호격자 평면 간격 ([Å] 단위의 d) (±0.1 Å)을 포함하는 신태그 XDS2000 분말 회절계로 취해진 X-선 분말 회절 패턴을 특징으로 하는 화합물: 21.2(s), 17.0(w), 7.1(s), 5.2(w), 4.7(w), 4.6(w), 4.2(w), 3.5(w), 3.3(w).
- (a) 안지오텐신 수용체 길항제 또는 그의 제약상 허용되는 염; 및(b) 중성 엔도펩티다제 억제제 (NEPi) 또는 그의 제약상 허용되는 염을 포함 하며, 안지오텐신 수용체 길항제 또는 그의 제약상 허용되는 염 및 NEPi 또는 그의 제약상 허용되는 염이 연결 부분에 의해 연결된 것인 연결된 프로드러그.
- 제45항에 있어서, 연결 부분이 비-공유 결합인 연결된 프로드러그.
- 제45항에 있어서, 연결 부분이 이온인 연결된 프로드러그.
- 제47항에 있어서, 이온이 금속 이온인 연결된 프로드러그.
- 제48항에 있어서, 금속 이온이 2가 금속 이온인 연결된 프로드러그.
- 제49항에 있어서, 2가 금속 이온이 칼슘인 연결된 프로드러그.
- 제45항에 있어서, 안지오텐신 수용체 길항제가 발사르탄, 로사르탄, 이르베사르탄, 텔미사르탄, 에프로사르탄, 칸데사르탄, 올메사르탄, 및 이들의 조합으로 이루어진 군으로부터 선택된 것인 연결된 프로드러그.
- 제51항에 있어서, 안지오텐신 수용체 길항제가 발사르탄인 연결된 프로드러그.
- 제45항에 있어서, 구조 NEPi·Xa·ARB (여기서, X는 Ca, Mg, Zn 및 Fe로부터 선택되고; a는 1+, 2+ 또는 3+임)를 갖는 연결된 프로드러그.
- 제45항에 있어서, 구조 NEPi·XaYb·ARB (여기서, X는 Ca, Mg, Zn 또는 Fe이고; Y는 Na, K 또는 NH4이고; a 및 b는 1+, 2+ 또는 3+임)를 갖는 연결된 프로드러그.
- 제45항에 있어서, 구조 NEPi·Zc·ARB (여기서, Z는 수소 결합 관능기를 제공하는 화합물이고; c는 0임)를 갖는 연결된 프로드러그.
- (a) 안지오텐신 수용체 길항제의 제약상 허용되는 염; 및(b) 중성 엔도펩티다제 억제제 (NEPi)의 제약상 허용되는 염을 포함하며, 안지오텐신 수용체 길항제 및 NEPi의 제약상 허용되는 염이 동일하고, Na, K 또는 NH4의 염으로부터 선택된 것인 조합물.
- 제57항에 있어서, 안지오텐신 수용체 길항제가 발사르탄, 로사르탄, 이르베사르탄, 텔미사르탄, 에프로사르탄, 칸데사르탄, 올메사르탄, 및 이들의 조합으로 이루어진 군으로부터 선택된 것인 조합물.
- 제58항에 있어서, 안지오텐신 수용체 길항제가 발사르탄인 조합물.
- 제57항 내지 제59항 중 어느 한 항에 있어서, NEPi가 (3S,2'R)-3-{1-[2'-(에톡시카르보닐)-4'-페닐-부틸]-시클로펜탄-1-카르보닐아미노}-2,3,4,5-테트라히드로-2-옥소-1H-1-벤즈아제핀-1-아세트산 또는 그의 제약상 허용되는 염인 조합물.
- 제57항 내지 제61항 중 어느 한 항에 있어서, 제약상 허용되는 염이 Na 염인 조합물.
- 제57항 내지 제62항 중 어느 한 항에 있어서, 안지오텐신 수용체 길항제 및 중성 엔도펩티다제 억제제가 1:1의 몰 비율로 존재하는 것인 조합물.
- (a) 제1항 내지 제44항 중 어느 한 항에 따른 화합물, 또는 제45항 내지 제56항 중 어느 한 항에 따른 연결된 프로드러그, 또는 제57항 내지 제63항 중 어느 한 항에 따른 조합물; 및(b) 1종 이상의 제약상 허용되는 첨가제를 포함하는 제약 조성물.
- 제64항에 있어서, 제약상 허용되는 첨가제가 희석제 또는 충전제, 붕해제, 유동화제, 윤활제, 결합제, 착색제, 및 이들의 조합으로 이루어진 군으로부터 선택된 것인 제약 조성물.
- (i) 안지오텐신 수용체 길항제 및 중성 엔도펩티다제 억제제 (NEPi)를 적합한 용매에 용해시키는 단계;(ii) Cat (여기서, Cat는 양이온임)의 염기성 화합물을 적합한 용매에 용해시키는 단계;(iii) 단계 (i) 및 (ii)에서 수득된 용액을 배합하는 단계;(iv) 고체를 침전시키고, 이를 건조시켜 이중-작용 화합물을 수득하는 단계; 또는 별법으로(iva) 생성된 용액을 증발 건조시키고;(va) 고체를 적합한 용매에 재-용해시키고;(via) 고체를 침전시키고, 이를 건조시켜 이중-작용 화합물을 수득하는 것에 의해, 단계 (i) 및 (ii)에서 사용된 용매(들)를 교환함으로써 이중-작용 화합물을 수득하는 단계를 포함하는,(a) 안지오텐신 수용체 길항제;(b) 중성 엔도펩티다제 억제제 (NEPi); 및(c) 제약상 허용되는 양이온을 포함하는 이중-작용 화합물의 제조 방법.
- 제66항에 있어서, 단계 (i) 및/또는 (iva)에서의 적합한 용매가 아세톤인 방법.
- 제66항 또는 제67항에 있어서, (Cat)의 염기성 화합물이 (Cat)OH, (Cat)2CO3, (Cat)HCO3, CatOMe, CatOAc 또는 CatOCHO인 방법.
- 제66항 내지 제68항 중 어느 한 항에 있어서, 단계 (i)에서의 안지오텐신 수용체 길항제가 발사르탄, 로사르탄, 이르베사르탄, 텔미사르탄, 에프로사르탄, 칸데사르탄, 올메사르탄, 및 이들의 조합으로 이루어진 군으로부터 선택된 것인 방법.
- 제69항에 있어서, 단계 (i)에서의 안지오텐신 수용체 길항제가 발사르탄인 방법.
- 제66항 내지 제70항 중 어느 한 항에 있어서, NEPi가 (3S,2'R)-3-{1-[2'-(에톡시카르보닐)-4'-페닐-부틸]-시클로펜탄-1-카르보닐아미노}-2,3,4,5-테트라히드로-2-옥소-1H-1-벤즈아제핀-1-아세트산 또는 그의 제약상 허용되는 염인 방법.
- 제66항 내지 제72항 중 어느 한 항에 있어서, 단계 (ii)에서의 양이온 (c) 및 Cat가 Na, K 및 NH4로 이루어진 군으로부터 선택된 것인 방법.
- 제73항에 있어서, 단계 (ii)에서의 Cat가 Na인 방법.
- (a) 무기 염 형성제를 용매에 첨가하여 연결된 프로드러그 염 형성 용액을 형성하는 단계;(b) 염 형성 용액을, 안지오텐신 수용체 차단제 또는 그의 제약상 허용되는 염 및 NEPi 또는 그의 제약상 허용되는 염의 혼합물에 첨가하여 ARB 및 NEPi가 연결된 프로드러그를 형성하도록 하는 단계; 및(c) 연결된 프로드러그를 단리하는 단계를 포함하는,안지오텐신 수용체 길항제 또는 그의 제약상 허용되는 염; 및 NEPi 또는 그의 제약상 허용되는 염을 포함하며, 안지오텐신 수용체 길항제 또는 그의 제약상 허용되는 염 및 NEPi 또는 그의 제약상 허용되는 염이 연결 부분에 의해 연결된 것인 연결된 프로드러그의 제조 방법.
- 제75항에 있어서, 무기 염 형성제가 수산화칼슘, 수산화아연, 메톡시화칼슘, 아세트산칼슘, 탄산수소칼슘, 포름산칼슘, 수산화마그네슘, 아세트산마그네슘, 포름산마그네슘 또는 탄산수소마그네슘으로부터 선택된 것인 방법.
- 제75항에 있어서, 용매가 물, 메탄올, 에탄올, 2-프로판올, 에틸아세테이트, 메틸-t-부틸에테르, 아세토니트릴, 톨루엔 및 메틸렌 클로라이드, 및 이러한 용매의 혼합물로부터 선택된 것인 방법.
- 제75항에 있어서, 단리 단계가 크로마토그래피에 의한 것인 방법.
- 발사르탄의 칼슘 염을 (2R,4S)-5-비페닐-4-일-5-(3-카르복시-프로피오닐아미노)-2-메틸-펜탄산 에틸 에스테르와 접촉시키는 단계, 및 혼합된 염을 선택적 결정 화에 의해 단리하는 단계를 포함하는, 발사르탄 및 (2R,4S)-5-비페닐-4-일-5-(3-카르복시-프로피오닐아미노)-2-메틸-펜탄산 에틸 에스테르의 연결된 프로드러그의 합성 방법.
- 제79항에 있어서, 단리 단계가 리간드 특이적 수지, 역상 수지 또는 이온-교환 수지를 사용한 크로마토그래피를 포함하는 것인 방법.
- 제1항 내지 제44항 중 어느 한 항에 따른 화합물, 또는 제45항 내지 제56항 중 어느 한 항에 따른 연결된 프로드러그, 또는 제57항 내지 제63항 중 어느 한 항에 따른 조합물의 치료 유효량을 하기 치료가 필요한 포유동물에게 투여하는 것을 포함하는, 고혈압, 심부전증 (급성 및 만성), 울혈성 심부전증, 좌심실 기능장애, 비대 심근병증, 당뇨병성 심근증, 심실위 및 심실 부정맥, 심방 세동, 심방 조동, 유해 혈관 개형, 심근 경색증 및 그의 후유증, 죽상동맥경화증, 앙기나 (불안정 또는 안정), 신부전증 (당뇨병성 및 비-당뇨병성), 심부전증, 협심증, 당뇨병, 속발성 알도스테론증, 원발성 및 속발성 폐 고혈압, 당뇨병성 신장병증, 사구체신염, 공피증, 사구체 경화증, 원발성 신장 질환의 단백뇨, 신장 혈관 고혈압, 당뇨병성 망막병증, 편두통, 말초 혈관 질환, 레이노병, 관강내 과다형성, 인지 기능장애, 녹내장 및 뇌졸중으로 이루어진 군으로부터 선택된 상태 또는 질환의 치료 또는 예방 방법.
- 제81항에 있어서, 고혈압의 치료 방법.
- (a) 제1항 내지 제44항 중 어느 한 항에 따른 화합물, 또는 제45항 내지 제56항 중 어느 한 항에 따른 연결된 프로드러그, 또는 제57항 내지 제63항 중 어느 한 항에 따른 조합물;(b) 항당뇨제, 고지혈증 치료제, 항비만제 및 항고혈압제로부터 선택된 치료제; 및(c) 1종 이상의 제약상 허용되는 첨가제를 포함하는 제약 조성물.
- 제83항에 있어서, 치료제가 암로디핀 베실레이트인 제약 조성물.
- 제83항에 있어서, 치료제가 히드로클로로티아지드인 제약 조성물.
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KR20180044321A (ko) * | 2015-08-28 | 2018-05-02 | 헤테로 랩스 엘티디. | 이중-작용 안지오텐신 수용체-네프릴리신 저해제 화합물의 제조를 위한 공정 |
KR20180128393A (ko) * | 2016-01-20 | 2018-12-03 | 심천 사루브리스 퍼머수티칼스 컴퍼니 리미티드 | 안지오텐신 ii 수용체 길항제 대사물질과 nep 억제제의 화합물, 및 이의 제조 방법 |
KR102215623B1 (ko) * | 2020-07-24 | 2021-02-15 | 유니셀랩 주식회사 | 사쿠비트릴 칼슘염 및 사쿠비트릴 유리염기와 발사르탄을 공동분자로 사용한 새로운 신규 공결정 형태 |
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