KR890000412A - 과지지질혈증을 방지하고 아테롬성 동맥경화증을 방지하는 우레아 및 카바메이트 화합물 - Google Patents
과지지질혈증을 방지하고 아테롬성 동맥경화증을 방지하는 우레아 및 카바메이트 화합물 Download PDFInfo
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Abstract
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Claims (34)
- 다음 구조식을 갖는 화합물 또는 그것의 제약학적으로 허용가능한 염.식중, Ar은 페닐; 나프틸; C1-v 알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸 또는 R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 치환된 페닐; C1-6알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리츤루오로메틸 또는 R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 치환된 나프틸; X는 산소 또는 황; Y는 산소 또는 -NH-; n은 0 또는 1-3인 정수; n′는 2-6인 정수; 및 n″는 0,1 또는 2; Ar′는 페닐; 나프틸; 티에닐; 피리디닐; C1-v알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는 R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 페닐; C1-v알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는 R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 나프틸; C1-6알킬, C1-6알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는R1및 R2가 각각 수소, 또는 C1-6알킬인 -NR1R2로 임의 치환된 티에닐; 또는 C1-6알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는 R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 피리디닐로부터 선택됨.
- 제1항에 있어서, X가 산소인 화합물.
- 제1항에 있어서, Y가 -NH-인 화합물.
- 제1항에 있어서, Ar이 페닐이거나 C1-v알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 페닐인 화합물.
- 제1항에 있어서, Ar′가 티에닐; 페닐; C1-v알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는 R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 티에닐; 또는 C1-v알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 페닐로부터 선택된 화합물.
- 제1항에 있어서, N-(2,6-디메틸페닐)-N′-(1-페닐사이클로펜틸)우레아인 화합물.
- 제1항에 있어서, N-(2,6-디메틸페닐)-N′-(1-페닐사이클로부틸)우레아인 화합물.
- 제1항에 있어서, N-(2,6-디에틸페닐)-N′-(1-페닐사이클로펜틸)우레아인 화합물.
- 제1항에 있어서, N-(2,6-디메틸페닐)-N′-[(1-페닐사이클로펜틸) 메틸]우레아인 화합물.
- 제1항에 있어서, N-(페닐사이클로펜틸)-N′-(2,4,6-트리메톡시페닐)우레아인 화합물.
- 제1항에 있어서, N-(2,6-디메틸페닐)-N′-[1-(2-티에닐) 사이클로헥실]우레아인 화합물.
- 제1항에 있어서, N-(2,6-디메틸페닐)-N′-[1-(2-티에닐) 사이클로헥실]우레아인 화합물.
- 제1항에 있어서, N-[2,6-비스(1-메틸에틸)]-N′-[1-(2-티에닐) 사이클로헥실]우레아인 화합물.
- 제1항에 있어서, N-(2,6-디에틸페닐)-N′-[(1-페닐사이클로헥실) 에틸]우레아인 화합물.
- 제1항에 있어서, N-(2,6-디메틸페닐)-N′-[(1-페닐사이클로펜틸) 에틸]우레아인 화합물.
- 제1항에 있어서, N-(2,6-디메틸페닐)-N′-[(1-페닐사이클로헥실) 메틸]우레아인 화합물.
- 제1항에 있어서, N-(2,6-디에틸페닐)-N′-[(1-페닐사이클로펜틸) 메틸]우레아인 화합물.
- 제1항에 있어서, N-[2,6-비스(1-메틸에틸)페닐]-N′-[(1-페닐사이클로헥실) 에틸]우레아인 화합물.
- 제1항에 있어서, N-[2,6-비스(1-메틸에틸)페닐]-N′-[(1-페닐사이클로펜틸) 에틸]우레아인 화합물.
- 제1항에 있어서, N-[2-에틸-6-(1-메틸에틸)페닐]-N′-[1-(2-티에닐) 사이클로헥실]우레아인 화합물.
- 제1항에 있어서, N-[2-(1,1-디메틸에틸)-6-메틸페닐]-N′-[1-(2-티에닐)사이클로헥실]우레아인 화합물.
- 제1항에 있어서, N-[2-메틸-6-(1-메틸에틸페닐]-N′-[1-페닐사이클로헥실) 에틸]우레아인 화합물.
- 제1항에 있어서, N-[2-(1.1-디메틸에틸)-6-메틸페닐]-N′-[1-페닐사이클로헥실) 에틸]우레아인 화합물.
- 제1항에 있어서, N-[2-에틸-6-(1-에틸에틸)페닐]-N′-[(1-페닐사이클로헥실) 메틸]우레아인 화합물.
- 제1항에 있어서, N-[2-메틸-6-(1-메틸에틸)페닐]-N′-[(1-페닐사이클로펜틸) 에틸]우레아인 화합물.
- 제1항에 있어서, N-[2-(1.1-디메틸에틸)-6-메틸페닐]-N′-[(1-페닐사이클로펜틸) 에틸]우레아인 화합물.
- 제1항에 있어서, N-[2-에틸-6-(1-메틸에틸)페닐]-N′-[1-(1-페닐사이클로펜틸) 메틸]우레아인 화합물.
- 제1항에 있어서, N-[2,4-디플루오로페닐)-N′-[1-(2-티에닐)사이클로헥실]우레아인 화합물.
- 제1항에 있어서, N-[2,4-디플루오로페닐)-N′-[(1-페닐사이클로펜틸) 에틸]우레아인 화합물.
- 제1항에 있어서, N-[2,4-디플루오로페닐)-N′-[(1-페닐사이클로헥실) 메틸]우레아인 화합물.
- 제1항에 있어서, N-(2,6-디브로오-4-플루오로페닐)-N′[(1-페닐사이클로헥실) 메틸]우레아인 화합물.
- 제약학적으로 허용가능한 담체와 함께 제1항에 정의된 화합물의 ACAT-억제 효과량으로 구성되는, 콜레스테롤을 조절하는 제약학적 조성물.
- 제약학적으로 허용가능한 담체와 함께 제1항에 정의된 화합물의 ACAT-억제 효과량을 환자에게 투여하는 것으로 구성되는, 콜레스테롤의 조절방법.
- a) 다음 구조식의 화합물은 Ar-N=C=0식중 Ar은 상기 정의된 바와 같음. 극성인 중성 유기용매내 주변 온도에서 다음 구조식의 화합물과 반응시키고;식중, y, n, n′, n″및 Ar′는 상기 정의된 바와 같음.b) 그후에 상기 반응 단계의 생성무를 분리하며; c) 원한다면, 상기 분리한 생성물을 제약학적으로 허용가능한 염으로 전화시키는 단계로 구성되는, 다음 구조식의 화합물 또는 그것의 제약학적으로 허용 가능한 염의 제조방법.식중 Ar은 페닐; 나프틸; C1-v알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 치환된 페닐; C1-v알킬, C1-2알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 치환된 나프틸; X는 산소 또는 황; Y는 산소 또는 -NH-; n은 0 또는 1-3인 정수; n′는 2-6인 정수; 및 n″는 0.1 또는 2; Ar′는 페닐; 나프틸; 티에닐; 피리디닐; C1-v알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 페닐; C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 나프틸; C1-v알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 티에틸; 또는 C1-v알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는 R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 피리디닐로부터 선택됨.※참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US5757687A | 1987-06-02 | 1987-06-02 | |
US057,576 | 1987-06-02 | ||
US14703788A | 1988-02-05 | 1988-02-05 | |
US147,037 | 1988-02-05 |
Publications (1)
Publication Number | Publication Date |
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KR890000412A true KR890000412A (ko) | 1989-03-14 |
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KR1019880006438A KR890000412A (ko) | 1987-06-02 | 1988-05-31 | 과지지질혈증을 방지하고 아테롬성 동맥경화증을 방지하는 우레아 및 카바메이트 화합물 |
Country Status (15)
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EP (1) | EP0293880B1 (ko) |
JP (1) | JP2575183B2 (ko) |
KR (1) | KR890000412A (ko) |
AU (1) | AU601846B2 (ko) |
CA (1) | CA1296339C (ko) |
DE (1) | DE3873992T2 (ko) |
DK (1) | DK175791B1 (ko) |
ES (1) | ES2051797T3 (ko) |
FI (1) | FI882588A (ko) |
GR (1) | GR3006297T3 (ko) |
IE (1) | IE61716B1 (ko) |
NO (1) | NO167200C (ko) |
NZ (1) | NZ224670A (ko) |
PH (1) | PH24216A (ko) |
PT (1) | PT87622B (ko) |
Families Citing this family (25)
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US5015644A (en) * | 1987-06-02 | 1991-05-14 | Warner-Lambert Company | Antihyperlipidemic and antiatherosclerotic urea and carbamate compounds |
US4868210A (en) * | 1988-03-30 | 1989-09-19 | Warner-Lambert Company | Antihyperlipidemic and antiatherosclerotic compounds and compositions |
US4994465A (en) * | 1989-02-17 | 1991-02-19 | Warner-Lambert Company | Antihyperlipidemic and antiatherosclerotic trisubstituted urea compounds |
JPH0395153A (ja) * | 1989-06-15 | 1991-04-19 | Mitsubishi Kasei Corp | ジフェニル尿素誘導体 |
AU629376B2 (en) * | 1989-08-04 | 1992-10-01 | Mitsubishi Chemical Corporation | 1-phenylalkyl-3-phenylurea derivatives |
US5153226A (en) * | 1989-08-31 | 1992-10-06 | Warner-Lambert Company | Acat inhibitors for treating hypocholesterolemia |
WO1992001681A1 (fr) * | 1990-07-25 | 1992-02-06 | Teijin Limited | Derive de benzopyrane, sa production, et composition pharmaceutique le contenant |
IL100915A (en) * | 1991-02-19 | 1996-03-31 | Erba Carlo Spa | Double-transformed urea and theories, their preparation and pharmaceutical preparations containing them |
US5420164A (en) * | 1991-04-04 | 1995-05-30 | Yoshitomi Pharmaceutical Industries, Ltd. | Cycloalkylurea compounds |
WO1993024458A1 (en) * | 1992-05-28 | 1993-12-09 | Pfizer Inc. | New n-aryl and n-heteroarylurea derivatives as inhibitors of acyl coenzyme a:cholesterol acyl transferase (acat) |
CA2107196A1 (en) * | 1992-09-29 | 1994-03-30 | Mitsubishi Chemical Corporation | Carboxamide derivatives |
US5534529A (en) * | 1993-06-30 | 1996-07-09 | Sankyo Company, Limited | Substituted aromatic amides and ureas derivatives having anti-hypercholesteremic activity, their preparation and their therapeutic uses |
DE4401893A1 (de) * | 1994-01-24 | 1995-07-27 | Bayer Ag | Substituierte Arylharnstoffe |
US6133326A (en) | 1994-08-31 | 2000-10-17 | Pfizer Inc | Compositions and methods for decreasing sebum production |
DE4443891A1 (de) * | 1994-12-09 | 1996-06-13 | Bayer Ag | Heterocyclisch substituierte Oxy-phenyl-(phenyl)glycinolamide |
US6605623B1 (en) | 1998-12-18 | 2003-08-12 | Bristol-Myers Squibb Pharma Co. | N-ureidoalkyl-piperidines as modulators of chemokine receptor activity |
ES2239145T3 (es) | 2000-02-02 | 2005-09-16 | Warner-Lambert Company Llc | Inhibidor doble de la sintesis de ester de colesterilo y de ester de cera avasimibe para el tratamiento de trastornos de la glandula sebacea. |
DE10308356A1 (de) * | 2003-02-27 | 2004-09-09 | Aventis Pharma Deutschland Gmbh | Cycloalkyl substituierte Alkansäurederivate, Verfahren zu ihrer Herstellung und ihre Anwendung als Arzneimittel |
DE10308352A1 (de) * | 2003-02-27 | 2004-09-09 | Aventis Pharma Deutschland Gmbh | Arylcycloalkylderivate mit verzweigten Seitenketten, Verfahren zu ihrer Herstellung und ihre Anwendung als Arzneimittel |
US8604244B2 (en) | 2010-07-02 | 2013-12-10 | Reviva Pharmaceuticals, Inc. | Compositions, synthesis, and methods of using cycloalkylmethylamine derivatives |
JP2010503709A (ja) | 2006-09-15 | 2010-02-04 | レビバ ファーマシューティカルズ,インコーポレーテッド | シクロアルキルメチルアミンの合成、使用方法および組成物 |
FR2946340B1 (fr) | 2009-06-05 | 2011-06-24 | Galderma Res & Dev | Nouveaux n-phenyl acetamie, inhibiteurs de l'enzyme soat-1, compositions pharmaceutiques et cosmetiques les contenant. |
FR2946345B1 (fr) | 2009-06-05 | 2011-05-20 | Galderma Res & Dev | Nouveaux derives dioxo-imidazolidine, inhibiteurs de l'enzyme soat-1, compositions pharmaceutiques et cosmetiques les contenant. |
FR2946342B1 (fr) | 2009-06-05 | 2011-06-24 | Galderma Res & Dev | Nouveaux derives de dioxo-imidazolidine, inhibiteurs de l'enzyme soat-1, compositions pharmaceutiques et cosmetiques les contenant. |
FR2946346B1 (fr) | 2009-06-05 | 2011-05-20 | Galderma Res & Dev | Nouveaux derives dioxo-imidazolidine, inhibiteurs de l'enzyme soat-1, compositions pharmaceutiques et cosmetiques les contenant. |
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EP0049538A3 (de) * | 1979-07-14 | 1982-10-13 | Bayer Ag | Verwendung von Thioharnstoffderivaten als Arzneimittel bei der Behandlung von Fettstoffwechselstörungen |
DE2945530A1 (de) * | 1979-11-10 | 1981-06-04 | Chemische Werke Hüls AG, 4370 Marl | Harnstoffe mit cyclischen substituenten, ihre herstellung und verwendung als herbizide |
US4623662A (en) * | 1985-05-23 | 1986-11-18 | American Cyanamid Company | Antiatherosclerotic ureas and thioureas |
US4387105A (en) * | 1982-01-26 | 1983-06-07 | American Cyanamid Company | Methods of treating atherosclerosis with dialkylureas and dialkylthioureas |
-
1988
- 1988-05-06 IE IE138088A patent/IE61716B1/en unknown
- 1988-05-09 CA CA000566283A patent/CA1296339C/en not_active Expired - Fee Related
- 1988-05-17 NZ NZ224670A patent/NZ224670A/xx unknown
- 1988-05-24 AU AU16573/88A patent/AU601846B2/en not_active Ceased
- 1988-05-31 PT PT87622A patent/PT87622B/pt not_active IP Right Cessation
- 1988-05-31 KR KR1019880006438A patent/KR890000412A/ko not_active Application Discontinuation
- 1988-05-31 PH PH36994A patent/PH24216A/en unknown
- 1988-06-01 ES ES88108816T patent/ES2051797T3/es not_active Expired - Lifetime
- 1988-06-01 FI FI882588A patent/FI882588A/fi not_active Application Discontinuation
- 1988-06-01 DK DK198802979A patent/DK175791B1/da not_active IP Right Cessation
- 1988-06-01 DE DE8888108816T patent/DE3873992T2/de not_active Expired - Lifetime
- 1988-06-01 NO NO882406A patent/NO167200C/no unknown
- 1988-06-01 JP JP63132918A patent/JP2575183B2/ja not_active Expired - Fee Related
- 1988-06-01 EP EP88108816A patent/EP0293880B1/en not_active Expired - Lifetime
-
1992
- 1992-11-19 GR GR920402658T patent/GR3006297T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
AU1657388A (en) | 1988-12-08 |
IE61716B1 (en) | 1994-11-30 |
NO167200C (no) | 1991-10-16 |
DE3873992D1 (de) | 1992-10-01 |
PH24216A (en) | 1990-04-10 |
NO167200B (no) | 1991-07-08 |
NO882406D0 (no) | 1988-06-01 |
NZ224670A (en) | 1989-10-27 |
DK297988A (da) | 1988-12-03 |
ES2051797T3 (es) | 1994-07-01 |
PT87622B (pt) | 1992-09-30 |
CA1296339C (en) | 1992-02-25 |
DK175791B1 (da) | 2005-02-21 |
IE881380L (en) | 1988-12-02 |
GR3006297T3 (ko) | 1993-06-21 |
NO882406L (no) | 1988-12-05 |
EP0293880B1 (en) | 1992-08-26 |
PT87622A (pt) | 1988-06-01 |
FI882588A (fi) | 1988-12-03 |
DK297988D0 (da) | 1988-06-01 |
FI882588A0 (fi) | 1988-06-01 |
JP2575183B2 (ja) | 1997-01-22 |
AU601846B2 (en) | 1990-09-20 |
JPS63316761A (ja) | 1988-12-26 |
DE3873992T2 (de) | 1992-12-17 |
EP0293880A1 (en) | 1988-12-07 |
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