KR970702255A - 벤즈아미드 화합물 및 그의 약제학적 용도(benzamide compounds and pharmaceutical use thereof) - Google Patents
벤즈아미드 화합물 및 그의 약제학적 용도(benzamide compounds and pharmaceutical use thereof)Info
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- KR970702255A KR970702255A KR1019960705864A KR19960705864A KR970702255A KR 970702255 A KR970702255 A KR 970702255A KR 1019960705864 A KR1019960705864 A KR 1019960705864A KR 19960705864 A KR19960705864 A KR 19960705864A KR 970702255 A KR970702255 A KR 970702255A
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- hydrogen
- alkyl
- pyridin
- benzamide
- aminoethyl
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Abstract
하기 화학식(1)의 벤즈아미드 화합물
(식 중, 각 기호는 명세서에서 정의한 바와 같다), 그의 이성체 및 약제학적으로 허용가능한 그의 산부가염, 약제학적 조성물은 이 화합물 및 약제학적으로 허용가능한 첨가제의 치료적 유효량을 포함하며, 이 화합물은 고혈압 치료제, 협심증 치료제, 천식 치료제, 신장 및 말초 순환 장해 치료제 및 대뇌 현관 경련 저해제를 포함한다.
본 발명의 화합물은 장기 지속성 신장 및 말초 순환 개선 작용 뿐 아니라 강한 평활근 이완 작용을 가지며 종래의 칼슘 길항제와 같이 저혈압 작용 및 대뇌, 관상 현관 확장 작용을 나타낸다. 칼슘 길항제와는 달리, 이것은 경구 투여되어 여러 길항제에 의해 야기되는 현관 수축을 억제하며, 프로필락시스 및 관상, 대뇌, 신장 및 말초 현관에서의 순환 장해의 치료용의 강력하고 장기 작용성인 시약, 고혈압, 협심증 및 신장 및 말초 순환 장해의 치료제, 대뇌 현관 경련의 저해제 등으로서 유용하다. 또한, 본 발명의 화합물은 천식 치료제로서 유용하다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (10)
- 하기 화학식(1)의 벤즈아미드 화합물, 그의 이성체 및 약제학적으로 허용가능한 그의 산부가염.[식중, R은 수소, 알킬, 또는 시클로알킬, 시클로알킬알킬, 페닐 또는 임의로는 고리상에 치환체를 갖는 아르알킬, 또는 화학식(2)의 기[식중, R6은 수소, 알킬 또는 식; -NR8R9(식중, 동일 또는 상이한 R8및 R9은 각각 수소, 알킬, 아르알킬 또는 페닐이다)이며, R7은 수소, 알킬, 아르알킬, 페닐, 니트로 또는 시아노이거나, R6및 R7은 결합하여 임의로는 산소 원자, 황 원자 또는 고리내에 부가적으로 임의로 치환된 질소 원자를 갖는 헤테로사이클을 형성한다]이며; R1은 수소, 알킬 또는 시클로알킬, 시클로알킬알킬, 페닐 또는 고리상에 치환체를 갖는 아르알킬이거나; R 및 R1은 인접한 질소 원자와 결합하여 산소 원자, 황 원자 또는 부가적으로 고리내에 임의로 치환된 질소원자를 갖는 헤테로사이클을 형성하며; 동일 또는 상이한 R2및 R3은 각각 수소, 알킬, 아르알킬, 할로겐, 니트로, 아미노, 알킬아미노, 아실아이노, 히드록시, 알콕시, 아르알킬옥시, 시아노, 아실, 메르캅토, 알킬티오, 아르알킬티오, 카르복시, 알콕시카르보닐, 카르바모일, 알킬카르바모일 또는 아지드이며; R4은 수소 또는 알킬이며, R5은 질소를 갖는 임의로 치환된 헤테로사이클이며; A는 화학식(3)(식중, 동일 또는 상이한 R10및 R11은 각각 수소, 알킬, 할로알킬, 아르알킬, 히드록시알킬, 카르복시 또는 알콕시카르보닐이거나, R10및 R11은 결합하여 시클로알킬을 형성하며, 1, m 및 n은 각각 0 또는 1 내지 3의 정 수이다)이다].
- 제1항에 있어서, 화학식 1에서 R, R1, R2, R3, R4, R5및 A중 하나 이상이 하기를 만족하는 것을 특징으로 하는 벤즈아미드 화합물, 그의 이성체 및 약제학적으로 허용가능한 그의 산부가염; R은 수소, 알킬, 또는 임의로는 고리상에 치환체를 갖는 아르알킬, 또는 화학식(2a)의 기{식 중, R6a은 수소 또는 식: -NR8aR9a(식 중, 동일 또는 상이한 R8a및 R9a은 각각 수소, 알킬 또는 아르알킬이다)이며, R7a은 수소, 알킬, 아르알킬 또는 페닐이거나, R6a및 R7a은 결합하여 임의로는 산소 원자, 황 원자 또는 고리내에 부가적으로 임의로 치환된 질소 원자를 갖는 헤테로사이클을 형성한다이며; R1은 수소, 알킬 또는 시클로알킬, 시클로알킬알킬, 페닐 또는 고리상에 치환체를 임의로 갖는 아르알킬이거나; R 및 R1은 인접한 질소 원자와 결합하여 산소 원자, 황 원자 또는 부가적으로 고리내에 임의로 치환된 질소원자를 갖는 헤테로사이클을 형성하며; 동일 또는 상이한 R2및 R3은 각각 수소, 알킬, 할로겐, 니트로, 아미노, 히드록시, 알콕시, 아르알킬옥시, 시아노, 아실, 카르복시, 알콕시카르보닐, 카르바모닐, 카르바모일 또는 아지드이며; R4은 수소 또는 알킬이며, R5은 질소를 갖는 임의로 치환된 헤테로사이클이며; A는 화학식(3a)(식중, 동일 또는 상이한 R10a및 R11a은 각각 수소, 알킬, 할로알킬, 히드록시알킬, 카르복시 또는 알콕시카르보닐이거나, R10a및 R11a은 결합하여 시클로알길을 형성하며, l, m 및 n은 각각 0 또는 1 내지 3의 정수이다)이다].
- 제1항에 있어서, 화학식 1에서 R, R1, R2, R3, R4, R5및 A중 하나 이상이 하기를 만족하는 것을 특징으로 하는 벤즈아미드 화합물, 그의 이성체 및 약제학적으로 허용가능한 그의 산부가염; R은 수소, 알킬 또는 화학식 (2b)의 기{식 중, R6b은 수소 또는 식: -NR8bR9b(식 중, 동일 또는 상이한 R8b및 R9b은 각각 수소, 또는 알킬이다)이며, R7b은 수소, 또는 알킬이거나, R6b및 R7b은 결합하여 임의로는 고리에 부가적으로 임의로 치환된 질소 원자를 갖는 헤테로사이클을 형성한다 이며; R1은 수소 또는 알킬이거나; R 및 R1은 인접한 질소 원자와 결합하여 임의로는 부가적으로 고리내에 임의로 치환된 질소원자를 갖는 헤테로사이클을 형성하며; 동일 또는 상이한 R2및 R3은 각각 수소, 할로겐, 니트로, 히드록시, 아르알킬옥시, 시아노, 카르복시, 알콕시카르보닐, 카르바모일 또는 아지드이며; R4은 수소이며, R5은 임의로 치환된 피리딘, lH-피롤로[2,3-b]피리딘 또는 1H-피라졸로[3,4-b]피리딘으로부터 유도되는 기이며; A는 화학식(3b)(식중, 동일 또는 상이한 R10b및 R11b은 각각 수소, 알킬, 히드록시알킬, 또는 카르복시이거나, R10a및 R11b은 결합하여 시클로알킬을 형성하며, l, m 및 n은 각각 0 또는 1 내지 3의 정수이며, m1은 0 또는 1이다)이다].
- 제1항에 있어서, 화학식(1)의 화합물로 하기로 구성된 군으로부터 선택한 것임을 특징으로 하는 벤즈아미드 화합물, 그의 이성체 및 약제학적으로 허용가능간 그의 산부가염.;(R)-N-(4-피리딘)-4-(1-아미노에틸)벤즈아미드, (R)-N-(4-피리딜) -4-(1-아미노에틸)-3-니트로벤즈아미드, (R)-N-(4-피리딜)-4-(l-아미노에틸)-3-클로로벤즈아미드, (R)-N-(4-피리필)-4-(1-아미노에틸)-2-니트로벤즈아미드, (R)-N-(4-피리딜)-4-(1-아미노에틸)-2-클로로벤즈아미드, (R)-N-(lH-피롤로[2,3-b]피리딘-4-일)-4-(l-아미노에틸)벤즈아미드, (R)-N-(lH-피롤로[2,3-b]피리딘-4-일)-4-(1-아미노에틸)-3-니트로벤즈아미드, (R)-N-(lH-피롤로[2,3-b]피리딘-4-일)-4-(1-아미노에틸)-3-아지드벤즈아미드, (R)-N-(3-이오드-lH-피롤로[2,3-b]피리딘-4-일)-4-(1-아미노에틸)-3-아지드벤즈아미드, (R)-N-(lH-피라졸로[3,4-b]피리딘-4-일)-4-(1-아미노에틸)벤즈아미드, (R)-N-(lH-피라졸로[3,4-b]피리딘-4-일)-4-(1-아미노에틸)-3-니트로벤즈아미드, (R)-N-(lH-피라졸로[3,4-b]피리딘-4-일)-4-(1-아미노에틸)-2-니트로벤즈아미드, (R)-N-(lH-피라졸로[3,4-b]피리딘-4-일)-4-(1-아미노에틸)-3-아지드벤즈아미드, (R)-N-[4-피리딜)-4-[]-구아니디노에틸)벤즈아미드, N-(lH-피라졸로[3,4-b]피리딘-4-일)-4-구아니디노메틸벤즈아미드, (R)-N-(1H-피라졸로[3,4-b]피리딘-4-일)-4-(1-구아니디노에틸)벤즈아미드, N-(lH-피라졸로[3,4-b]피리딘-4-일)-4-구아니디노메틸-3-니트로벤즈아미드, (R)-N-(lH)-피라졸로[3,4-b]피리딘-4-일)-4-(l-구아니디노에틸)-3-니트로벤즈아미드, (R)-N-(lH-피라졸로[3,4-b]피리딘-4-일)-4-(1-구아니디노에틸)-2-니트로벤즈아미드, (R)-N-(lH-피롤로[2,3-b]피리딘-4-일)-4-(1-구아니디노에틸)벤즈아미드, (R)-N-(lH-피롤로[2,3-b]피리딘-4-일)-4-(1-(3-프로필구아니디노)-에틸)벤즈아미드, (R)-N-(lH-피라졸로[3,4-b]피리딘-4-일)-4-(1-아미노에틸)-3-시아노벤즈아미드, N-(lH-피라졸로[3,4-b]피리딘-4-일)-4-(1-아미노-2-히드록시에틸)벤즈아미드 및 (R)-N-(3-이오도-lH-피롤로[2,3-b]피리딘-4-일)-4-(1-아미노에틸)벤즈아미드.
- 제1항의 벤즈아미드 화합물, 그의 이성체 또는 약제학적으로 허용가능한 그의 산부가염, 및 약제학적으로 허용가능한 첨가제의 치료적 유효량을 포함하는 약제학적 조성물.
- 제1항의 벤즈아미드 화합물, 그의 이성체 또는 약제학적으로 허용가능한 그의 산부가염을 포함하는 고혈압 치료제.
- 제1항의 벤즈아미드 화합물, 그의 이성체 또는 약제학적으로 허용가능한 그의 산부가염을 포함하는 협심증 치료제.
- 제1항의 벤즈아미드 화합물, 그의 이성체 또는 약제학적으로 허용가능한 그의 산부가염을 포함하는 천식 치료제.
- 제1항의 벤즈아미드 화합물, 그의 이성체 또는 약제학적으로 허용가능한 그의 산부가염을 포함하는 신장 및 말초 순환 장해 치료제.
- 제1항의 벤즈아미드 화합물, 그의 이성체 또는 약제학적으로 허용가능한 그의 산부가염을 포함하는 대뇌 혈관 경련 저해제.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
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EP3064222B1 (en) | 2013-10-31 | 2020-10-21 | Kyoto Prefectural Public University Corporation | Therapeutic drug comprising tgf-beta signal inhibitor for diseases related to endoplasmic reticulum cell death in corneal endothelium |
US11624053B2 (en) | 2013-11-27 | 2023-04-11 | Kyoto Prefectural Public University Corporation | Application of laminin to corneal endothelial cell culture |
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US3971789A (en) * | 1972-10-21 | 1976-07-27 | John Wyeth & Brother Limited | O-(4-Quinolylamino)benzamides |
DE2520896A1 (de) * | 1975-05-10 | 1976-11-25 | Basf Ag | Azopigmente der beta-hydroxynaphthoesaeurereihe |
ES438120A1 (es) * | 1975-06-02 | 1977-02-01 | Gallardo Antonio Sa | Procedimiento para la preparacion de amidas aromaticas. |
FI763021A (ko) * | 1975-11-03 | 1977-05-04 | Thomae Gmbh Dr K | |
ES456989A1 (es) | 1977-03-18 | 1978-07-16 | Lafarquim | Procedimiento de obtencion de un derivado de 4-aminopiridinay sus sales. |
IT1126509B (it) * | 1979-12-07 | 1986-05-21 | Medea Res Srl | Benzimidi ad attivita' anestetica locale e antiaritmica,processo per la loro preparazione e composizioni farmaceutiche che le contengono |
JPS57206662A (en) * | 1981-06-15 | 1982-12-18 | Chugai Pharmaceut Co Ltd | Benzamide derivative |
US4720500A (en) * | 1985-07-11 | 1988-01-19 | Rhone-Poulenc Sante | N-1,8-naphthyridin-2-yl amides useful as immunostimulants |
FR2592882B2 (fr) * | 1986-01-16 | 1988-03-11 | Rhone Poulenc Sante | Nouveaux amides substitues, leur preparation et les medicaments qui les contiennent |
JPS6229566A (ja) * | 1985-07-30 | 1987-02-07 | Taiyo Yakuhin Kogyo Kk | 新規グアニジノメチル安息香酸誘導体 |
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JPS62158252A (ja) * | 1985-12-28 | 1987-07-14 | Kirin Brewery Co Ltd | 4−アミノピリジンベンズアミド誘導体 |
JPS62158253A (ja) * | 1985-12-28 | 1987-07-14 | Kirin Brewery Co Ltd | 4−アミノピリジンアミド誘導体 |
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EP0303445A1 (en) * | 1987-08-13 | 1989-02-15 | Walton S.A. | Clebopride transdermal patch |
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WO1990005723A1 (en) * | 1988-11-24 | 1990-05-31 | Yoshitomi Pharmaceutical Industries, Ltd. | Trans-4-amino(alkyl)-1-pyridylcarbamoyl-cyclohexane compounds and their medicinal use |
WO1993005021A1 (en) * | 1991-09-06 | 1993-03-18 | Yoshitomi Pharmaceutical Industries, Ltd. | 4-amino(alkyl)cyclohexane-1-carboxamide compound and use thereof |
-
1995
- 1995-04-14 EP EP01127632A patent/EP1195372A1/en not_active Withdrawn
- 1995-04-17 WO PCT/JP1995/000747 patent/WO1995028387A1/ja active IP Right Grant
- 1995-04-17 ES ES95915333T patent/ES2208678T3/es not_active Expired - Lifetime
- 1995-04-17 US US08/727,669 patent/US5958944A/en not_active Expired - Lifetime
- 1995-04-17 CA CA002188164A patent/CA2188164C/en not_active Expired - Lifetime
- 1995-04-17 AT AT95915333T patent/ATE255093T1/de not_active IP Right Cessation
- 1995-04-17 EP EP03025765A patent/EP1391454B1/en not_active Expired - Lifetime
- 1995-04-17 ES ES03025765T patent/ES2388917T3/es not_active Expired - Lifetime
- 1995-04-17 DE DE69532195T patent/DE69532195T2/de not_active Expired - Lifetime
- 1995-04-17 KR KR1019960705864A patent/KR100311438B1/ko not_active IP Right Cessation
- 1995-04-17 EP EP95915333A patent/EP0757038B1/en not_active Expired - Lifetime
-
1999
- 1999-02-18 US US09/252,079 patent/US6156766A/en not_active Expired - Lifetime
Also Published As
Publication number | Publication date |
---|---|
EP1391454A1 (en) | 2004-02-25 |
EP1195372A1 (en) | 2002-04-10 |
US5958944A (en) | 1999-09-28 |
US6156766A (en) | 2000-12-05 |
EP0757038A1 (en) | 1997-02-05 |
EP0757038A4 (en) | 1997-08-06 |
EP0757038B1 (en) | 2003-11-26 |
CA2188164A1 (en) | 1995-10-26 |
CA2188164C (en) | 2005-08-09 |
ES2388917T3 (es) | 2012-10-19 |
ES2208678T3 (es) | 2004-06-16 |
DE69532195T2 (de) | 2004-09-02 |
ATE255093T1 (de) | 2003-12-15 |
DE69532195D1 (de) | 2004-01-08 |
WO1995028387A1 (fr) | 1995-10-26 |
KR100311438B1 (ko) | 2002-06-20 |
EP1391454B1 (en) | 2012-05-30 |
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