KR870011100A - 1.5-디아릴-3-치환된-피라졸 및 그의 합성방법 - Google Patents
1.5-디아릴-3-치환된-피라졸 및 그의 합성방법 Download PDFInfo
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- KR870011100A KR870011100A KR870005383A KR870005383A KR870011100A KR 870011100 A KR870011100 A KR 870011100A KR 870005383 A KR870005383 A KR 870005383A KR 870005383 A KR870005383 A KR 870005383A KR 870011100 A KR870011100 A KR 870011100A
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Abstract
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Claims (30)
- 하기 일반식의 화합물 및 약제학적으로 허용되는 그의 염.상기식에서 R1, R2, R3및 R4는 동일하거나 상이하며, 독립적으로 수소, 저급알킬, 저급 알콕시, 페닐, 할로, 하이드록시, 저급 알킬설포닐, 저급알킬티오, 니트로, 트리플루오로메틸, ω-트리플루오로메틸, 저급 알콕시, 아미노, 아세트아미도, 카복시, 알킬하이드록삼산으로 이루어진 그룹 중에서 선택되거나, R1, R2,또는 R3, R4가 이들이 부착된 페닐그룹과함께 나프틸 또는 치환된 나프틸 그룹을 형성하고; R은 탄소수 2내지 16의 포화 또는 불포화된 직쇄 탄화수소이며; Y는 수소, 브로모, 클로로 또는 저급 알킬이고; X는 카복시, 하이드록시, 아세톡시, 알카노일옥시, 저급알콕시, 저급 알킬 카보닐, 옥시미노, 시아노, 아미노, C(O)-R5및 -C(O)C(O)-R5로 이루어진 그룹중에서 선택되며; R5는 수소, 알킬, 저급 알콕시 및 NR6R7로 이루어진 그룹중에서 선택되고, R6및R7은 동일하거나 상이하며 수소 및 저급 알킬로 이루어진 그룹중에서 선택되거나 R6또는R7은 수소, 저급알킬, 저급 알콕시, 하이드록시, 아실옥시, 벤질옥시, 2-하이드록시 저급 알킬, 저급 알킬 카복시, 페닐, 치환된 페닐, 피리딜, 타이졸릴, 디하이드로 타이졸릴, 5-테트라졸릴, -OCO(CH2)nCOR9[여기에서, R9는 -OH-ONa, 디알킬 아미노(예, 디에틸아미노)및 모폴리노이고, n은 2또는 3이다]; -OCOR10[여기에서, R10은 -CH2NR11R12{여기에서, R11및R12는 알킬(예,메틸), 사이클로알킬(예, 사이클로헥실)이거나, 함께는 헤테로사이틀릭 환(예, N-메틸피페라지노)이다},-CH2Cl, -CH2O-저급알킬 또는 t-부틸, -CH-저급알킬-CO2-Q{여기에서, Q는 저급알킬 또는 -H, 아실(예, 아세틸, 프로피오닐 또는 부티릴)이다}이다]; -NR8OH[여기에서, R8은 수소, -CO-저급알킬, -CO-t-부틸, -COC7H15,-CO-페닐, SO2-저급알킬 및 -COCONHOH이다]; -NHR13[여기에서, R13은 수소, -CO-저급알킬, -CO-t-부틸, -COC7H15, -CO-페닐, SO2-저급알킬-COCO2-저급알킬, -COCONHOH, -COCO2H, -COCO2H, COCON(저급알킬)OH, 및 PO(O-저급알킬)2이다[;-C(R14)=NNH-2-티아졸리노,-CH(OH)R14및 -C(O)R14[여기에서,R14는 수소,저급알킬,페닐 및 t-부틸이다];-C(=NOH)NH2및 -C(=NH)N(OH)-저급알킬, ω-알카노에이트 및 O-NR8R9[여기에서, R8및 R9는 동일하거나 상이하며 수소, 저급알킬, 페닐 및 치환된 페닐로 이루어진 그룹중에서 선택된다]로 이루어진 그룹중에서 선택되며;단,(a)Y가 브로모 또는 클로로인 경우, X는 -COOH,CH2OH또는 -C(O)-R5[여기에서, R5는 NR6R7이고, 이때 R6는 -OH이며 R7은 저급알킬이다]이고; (b)(i)R-X가 (CH2)3CO2H또는 (CH2)2CO(O)NHOH이고 (ii)R3및 R4가 4-메톡시, 3-메톡시-4-하이드록시, 2-하이드록시 및 수소인 경우, R1및 R2중 적어도 하나는 수소 이외의 것이며; (c)R-X가 함께 탄소-탄소 결합에 의해 서로 결합된 3개의 포화된 탄소원자를 함유하는 경우, R1및 R2중 적어도 하나, 또는 R3및R4중 적어도 하나는 수소 이외의 것이다.
- 제1항에 있어서, R2및R4가 수소이고, R1및 R2이 할로, 트리플루오로메틸, 저급알킬 및 저급알콕시로 이루어진 그룹중에서 선택되는 화합물.
- 제2항에 있어서, R이 포화되는 직쇄이고 탄소-탄소 결합에 의해 서로 결합된 3개의 탄소원자를 함유하는 화합물.
- 제3항에 있어서, X가 하이드록시, 카복시, 약제학적으로 허용되는 양이온의 카복실레이트염, C(O)-NR6R7[여기에서, R6및 R7은 수소, 하이드록시, 메틸, t-부ㅣㄹ, 2-하이드록시에틸 및 카복시메틸로 이루어진 그룹중에서 선택된다]로 이루어진 그룹중에서 선택되는 화합물.
- 제2항에 있어서, R이 불포화되고 2내지 16개의 탄소원자를 함유하는 화합물.
- 제5항에 있어서, X가 카복실인 화합물 또는 그의 염.
- 하기 일반식의 화합물.상기식에서, R1및 R3는 할로, 트리플루오로메틸, 메틸 및 메톡시로 이루어진 그룹중에서 선택된다.
- 하기 일반식의 화합물.상기식에서, R1및 R3는 할로, 트리플루오로메틸, 메틸 및 메톡시로 이루어진 그룹중에서 선택되고, X는 카복시 및 C(O)-R5[여기에서, R5는 N(CH3)OH, N(t-C4H9)OH, NHOH, ONH(CH3)및 ONH(t-C4H9)로 이루어진 그룹중에서 선택된다]로 이루어진 그룹중에서 선택된다.
- 제1항에 있어서, 3-[5-(4-클로로페닐)-1-(4-메톡시페닐)-3-피라졸릴]-N-하이드록시-N-메틸프로판 아마이드인 화합물.
- 제1항에 있어서, 5-[(4-클로로페닐)-3-(3-하이드록시프로필)-1-(4-메톡시페닐)피라졸인 화합물.
- 제1항에 있어서, 5-[(4-트루플루오로메틸페닐)-3-(3-하이드록시프로필)-1-(4-메톡시페닐)피라졸인 화합물.
- 제1항에 있어서, 1-(4-브로모피닐)-5-(4-클로로페닐)-3-(3-하이드록시프로필)피라졸인 화합물.
- 제1항에 있어서, 나트륨8-[5-(4-클로로페닐)-1-(4-메톡시페닐)-3-피라졸릴]-5(Z)-옥테노에이트인 화합물.
- 제1항에 있어서, 나트륨3-[5-(4-클로로페닐)-1-(4-메톡시페닐)-3-피라졸릴]프로파노에이트인 화합물.
- 제1항에 있어서, 3-[5-(4-클로로페페)-1-(4-메톡시페닐)-3-피라졸릴]-N-3급-부틸-N-하이드록시 프로판아마이드인 화합물.
- 제1항에 있어서, N-카복시메틸-3-[5-(4-클로로페닐)-1-(4-메톡시페닐)-3-피라졸릴]-프로판아마이드인 화합물.
- 제1항에 있어서, N-카복시메틸-3-[5-(4-클로로페닐)-1-(4-메톡시페닐)-3-피라졸릴]프로판아마이드, 3-[5-(4-클로로페닐-1-(4-메톡시페닐)-3-피라졸릴]-N-하이드록시-N-이소프로필프로판아마이드, 3-[5-(4-클로로페닐-1-(4-메톡시페닐)-3-피라졸릴]-N-사이클로헥실-N-하이드록시프로판아마이드 및 3-[5-(4-클로로페닐-1-(4-메톡시페닐)-3-피라졸릴]-N-에틸-하이드록시프로판아마이드로 이루어진 그룹중에서 선택되는 화합물.
- 제1항에 있어서, 3-[5-(4-클로로페닐-1-(4-메톡시페닐)-3-피라졸릴]-N-하이드록시-N-페닐프로판아마이드, 3-[5-(4-클로로페닐-1-(4-메톡시페닐)-3-피라졸릴]프로필아민, 3-[5-(4-클로로페닐-1-(4-메톡시페닐)-3-피라졸릴]프로판알, 5-(4-클로로페닐-3-(3-옥시미노-프로필)-1-(4-메톡시페닐)피라졸릴 및3-(3-하이드록시프로필)-1-(4-메틸옥시페닐)-5-(4-톨릴)피라졸릴로 이루어진 그룹중에서 선택되는 화합물.
- 약제학적으로 허용되는 담체중에 분산된 활성성분으로서 제1항에 따른 치환된 피라졸 화합물의 유효량을 함유하는 국소, 경구, 비경구 및 에어로졸 두여용의 약제학적 조성물.
- 제19항에 있어서, 조성물이 포유류에 유입될 경우 치환된 피라졸 화합물이 조성물에 존재하는 양으로 사이클로옥시게네이스 및 리폭시게네이스 경로를 억제할 수 있느 약제학적 조성물.
- 제19항에 따른 약제학적 조성물을 포유류에게 투여하여 염증반응을 나타내는 포유류의 염증을 경감시키는 방법.
- 제19항에 따른 약제학적 조성물을 포유류에게 투여하여 건선 또는 다른 피부병을 포함한 피부의 염증상태를 치료하는 방법.
- 약제학적으로 허용되는 담체중에 분산된 활성성분으로 제1항에 따른 치환된 피라졸 화합물의 심근부전증에 대한 유효량을 함유하는 약제학적 조성물을 포유류에게 투여하여 앙기나, 혈관경련, 경색을 포함한 심근부전증을 치료하는 방법.
- 제19항에 따른 약제학적 조성물을 포유류에게 투여하여 천식 및 알레르기성 과민성 질환을 치료하는 방법.
- 아릴하이드라진을 알킬쇄의 탄소수가 적어도 4인 1-아릴-(오메가-치환된)-알킬-1,3-디온과 반응시키되, 상기 반응을 상기 반응조건에 대해 실질적으로 불활성인 용매중에서 수행하고, 상기 오메가-치환체는 상기 반응조건에 대해 실질적으로 불활성이며, 상기 아릴그룹은 동일하거나 상이하고 일-또는이-치환된 페닐이며, 여기에서 페닐치환체는 수소,저급알킬, 저급알콕시, 페닐, 할로, 하이드록시, 저급알킬설포닐, 저급알킬티오, 니트로, 트리플루오로메틸, 오메가-트리플루오로메틸 저급알콕시, 나프틸 및 치환된 나프닐로 이루어진 그룹중에서 선택됨을 특징으로하여, 제1항의 1,5-디아릴-3-(오메가-치환된 저급알킬)-피라졸을 합성하는 방법.
- 제1항에 있어서, 3-[1-(4-메톡시페닐)-5-(4-메틸페닐)-3-피라졸릴]-N-하이드록시-N-메틸프로판아마이드인 화합물.
- 제1항에 있어서, 3-[1-(4-메톡시페닐)-5-(4-메틸페닐)-3-피라졸릴]-N-석시닐옥시프로판아미드인 화합물.
- 제1항에 있어서, 3-[5-(4-클로로페닐)-1-(4-메톡시페닐)-3-피라졸릴]-N′-N′-디메틸글리시닐옥시-N-메틸프로판아마이드인 화합물.
- 제1항에 있어서, N-[3-5-(4-클로로페닐)-1-(4-메톡시페닐)-3-피라졸릴]프로필]-N,N′-디하이드록시-옥사마이드인 화합물.
- 제1항에 있어서, N-아세틸-N-아세톡시[5-(4-클로로페닐)-1-(4-메톡시페닐)-3-피라졸릴]프로판아마이드인 화합물.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (6)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US86799686A | 1986-05-29 | 1986-05-29 | |
US867,996 | 1986-05-29 | ||
US867996 | 1986-05-29 | ||
US042661 | 1987-04-29 | ||
US042,661 | 1987-04-29 | ||
US07/042,661 US4826868A (en) | 1986-05-29 | 1987-04-29 | 1,5-Diaryl-3-substituted pyrazoles pharmaceutical compositions and use |
Publications (2)
Publication Number | Publication Date |
---|---|
KR870011100A true KR870011100A (ko) | 1987-12-21 |
KR960007163B1 KR960007163B1 (ko) | 1996-05-29 |
Family
ID=26719497
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019870005383A KR960007163B1 (ko) | 1986-05-29 | 1987-05-29 | 1,5-디아릴-3-치환된-피라졸, 이의 합성방법 및 이를 포함하는 약제학적 조성물 |
Country Status (21)
Country | Link |
---|---|
US (1) | US4826868A (ko) |
EP (1) | EP0248594B1 (ko) |
JP (1) | JP2512751B2 (ko) |
KR (1) | KR960007163B1 (ko) |
CN (1) | CN1028227C (ko) |
AU (1) | AU596844B2 (ko) |
CA (1) | CA1337122C (ko) |
DE (2) | DE3788244T2 (ko) |
DK (1) | DK170202B1 (ko) |
ES (1) | ES2059377T3 (ko) |
FI (1) | FI94340C (ko) |
HK (1) | HK14094A (ko) |
HU (1) | HU221300B1 (ko) |
IE (1) | IE63856B1 (ko) |
IL (1) | IL82671A0 (ko) |
LU (1) | LU90829I2 (ko) |
NL (1) | NL300057I2 (ko) |
NO (2) | NO172236C (ko) |
NZ (1) | NZ220353A (ko) |
PH (1) | PH25126A (ko) |
PT (1) | PT84964B (ko) |
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1987
- 1987-04-29 US US07/042,661 patent/US4826868A/en not_active Expired - Lifetime
- 1987-05-18 NZ NZ220353A patent/NZ220353A/xx unknown
- 1987-05-27 AU AU73608/87A patent/AU596844B2/en not_active Expired
- 1987-05-27 CA CA000538137A patent/CA1337122C/en not_active Expired - Lifetime
- 1987-05-27 IL IL82671A patent/IL82671A0/xx unknown
- 1987-05-27 DK DK273587A patent/DK170202B1/da active Protection Beyond IP Right Term
- 1987-05-27 NO NO872228A patent/NO172236C/no not_active IP Right Cessation
- 1987-05-28 DE DE87304720T patent/DE3788244T2/de not_active Expired - Lifetime
- 1987-05-28 EP EP87304720A patent/EP0248594B1/en not_active Expired - Lifetime
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- 1987-05-28 IE IE140387A patent/IE63856B1/en not_active IP Right Cessation
- 1987-05-28 DE DE2001199049 patent/DE10199049I2/de active Active
- 1987-05-28 ES ES87304720T patent/ES2059377T3/es not_active Expired - Lifetime
- 1987-05-28 HU HU466/87A patent/HU221300B1/hu unknown
- 1987-05-28 PH PH35317A patent/PH25126A/en unknown
- 1987-05-28 FI FI872379A patent/FI94340C/fi not_active IP Right Cessation
- 1987-05-29 CN CN87103953A patent/CN1028227C/zh not_active Expired - Lifetime
- 1987-05-29 JP JP62134789A patent/JP2512751B2/ja not_active Expired - Lifetime
- 1987-05-29 KR KR1019870005383A patent/KR960007163B1/ko not_active IP Right Cessation
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1994
- 1994-02-24 HK HK140/94A patent/HK14094A/xx not_active IP Right Cessation
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2001
- 2001-09-10 NL NL300057C patent/NL300057I2/nl unknown
- 2001-09-10 NO NO2001016C patent/NO2001016I1/no unknown
- 2001-09-10 LU LU90829C patent/LU90829I2/fr unknown
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