KR920004354A - 3-아미도피라졸 유도체 및 그 제조방법과 그것을 함유한 약학 조성물 - Google Patents
3-아미도피라졸 유도체 및 그 제조방법과 그것을 함유한 약학 조성물 Download PDFInfo
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Abstract
Description
Claims (8)
- 하기식(Ⅰ)또는 (Ⅰ')의 3-아미도피라졸 또는 그의 유기 또는 무기산과의 가능한 염 또는 그의 유기 또는 무기산과의 가능한 염 :식중, -R1은 하기의 기들을 나타내고,[식중, R1,R1'및 R1"는 각각 독립적으로 수소원자, 할로겐원자, 히드록실, 직쇄 또는 측쇄의 C1~C4알킬기, C1~C4알콕시기, 트리플루오르 메틸기, 트리플루오로메톡시기, 니트로기, 카르복실기 또는 아미노기를 나타낸다. ㆍ알킬이 C1~C4기인 카르복시알킬 또는 알콕시카르보닐알킬기, ㆍ알킬이 C3~C6기인 시클로알킬기, ㆍ테트라히드로나프틸리, ㆍ피리딜기, ㆍ상기 정의된 R1,R1'및R1"로 치환된 나프틸기, ㆍ상기 정의된 R1,R1'및 R1"로 치환된 벤질기, ㆍ방향족 고리위에 할로겐, 히드록실 또는 C1~C4알콕시로 임의 치환된 신나밀기,ㆍ상기 정의된 R1,R1'및 R1"로 임의 치환된 퀴놀릴 또는 이소퀴놀릴기, ㆍ2-벤조티아졸릴기, ㆍ퀴녹살리닐디온기, 1-프탈라지닐기, ㆍ벤조티아디아졸릴기, ㆍ특히,피리딜 및 티에닐 같은 5-또는 6-원 헤테로고리기로 치환된 메틸렌기, -RIa는 상기 정의된 R1,R1'및 R1"로 치환된 벤질기를 나타내며, -R은 수소원자 또는 직쇄 또는 측쇄의 C1~C4알킬기를 나타내고, -n은 0,1,2또는 3이고, -X가 수소를 나타내고 X'가 수소, 직쇄 또는 측쇄의 C1~C6알킬, 아릴, C1~C4알아미노알킬, C1~C4히드록시알킬, 알킬기가 C1~C4기인 카르복실알킬,알킬기가 C1~C4기인 아세트아미도아라킬시스테인, 알킬기가 C1~C4기인 구아니디노알킬, 알킬기가 C1~C4기인 니트로구아니디노알킬, C3~C7시클로알킬, 알킬이C1~C4기이고 이릴이 할로겐 또는 히드록실로 또는 C1~C3알킬로 임의 치환된 알릴알킬, 헤테로아릴이 C1~C4알킬, 히드록실 또는 C1~C4알콕시로 치환되거나 치환되지 않은 인돌릴 또는 이미다졸릴을 나타내고 알킬이 C1~C4기인 헤테로알릴알킬을 나타내거나, -또는, n이 0일때, X가 수소를 나타내고 X'및이 하기식의 히드록실로 치환되거나 치환되지 않은 고리를 함께 형성하거나:(식중, m=2,3 또는 4) 또는 하기식의 고리계이거나 :(식중, t=1또는 2) 또는 하기식의 고리계이거나 :또는 인돌리닐, 퍼히드로인돌 또는 4,5,6,7-테트라히드로티에노[2,3-c]피리드-6-일 고리계이거나, -또는 X및 X'가 각각 독립적으로 C1~C4알킬 또는 C3~C6시클로알킬, 페닐을 나타내거나, -또는 X및 X'가 연결되어 2내지 12개의 탄소원자를 갖는, C1-C3알킬로 임의 치환된 시클로알킬기를 함께 형성하거나, -또는 X, X'및 그들이 연결된 탄소원자가 아다만탈기, 하나 또는 둘의 메틸기로 또는 히드록실, C1~C3알콕시 또는 할로겐 원자로 치환된 아다만틸기, 1-아자아다만틸기, 퀴뉴클리디닐기, 벤질기로 임의로 N-치환된 4-피페리딜기, 2,2,6,6-테트라메틸피페리딜기, 테트라히드로나프틸기, 테트라히드로피란-4-일 또는 테트라히드로티오피란-4-일기, 2,3-디히드로-4H-벤조피란-4-일기, 2,3-디히드로-4H-벤조티오피란-4-일기, 하나의 고리 또는 다른 고리의 탄소원자를 통해 상기에서 정의된 -N(R)-및-C(O)-Z에 결합된 하기 a의 기(식중, n1=0 또는 1, n1'=또는 2, n2=1, n3=2 또는 3이고 W는 탄소원자 또는 산소원자를 나타낸다), 또는 하나의 고리 또는 다른 고리 또는 다른 고리의 탄소원자를 통해 상기에서 정의된 -N(R)-및-C(O)-Z에 하기식 b의 기.(식중, n4=2,3 또는 4, n5=2 또는 3이고 W는 탄소 또는 산소원자를 나타낸다)상기b및b의 고리는 하나의 고리 및/또는 다른 고리위에 하나 또는 둘의 C1~C4알킬기로 임의 치환이 가능하며 W가 산소를 나타낼때 W에 대해 α-위치에서 아미노기의 치환이 가능하지는 않다. 비시클로[2,2,1]헵트-5-엔-2-일기,8-옥사비시클로[3,2,1]옥트-6-3-일기, 8-티아비시클로-[3.2.1]옥트-3-일기를 형성하거나, -또는, X가 수소를 나타내고 X'가 아다만틸기, 하나 또는 둘의 메틸, 히드록실, C1~C3알콕시기 또는 할로겐 원자로 치환된 아다만틸기, 1-아자 아다만틸기, b의 W가 산소를 나타낼때 W에 대해 α-위치에 이러한 고리계들 사이의 결합과 -COZ및 N-R을 운반하는 탄소가 존재하는 것이 가능하지 못한, 상기 정의된 식b또는b의 기이고 -Z가 히드록실기 또는 C1~C6알킬,트리플루오로메틸, 트리플루오로메톡시 또는 카르보닐길 치환된 벤질, 벤질,t-부틸과 같은 카르복실산-보호기로 치환된 탄소원자, Z가 알킬이 직쇄 또는측쇄의 C1~C6기인 카르복시알킬로 치환된 질소원자를 나타내고 n=0이면, X=H일때 X'는 하기의 기 :(식중, X=1또는 2이고 Q는 히드록실, 자유아미노 또는 C1~C6디알킬 또는 C1~C6알콕시로 치환된 아미노이다)일수 없다는 제한하에 상기 정의된 바와같이 치환된 질소원자를 나타내고, -RIv수소원자, 할로겐원자 또는 C1~C6알킬을 나타내며, -Rv는 하기의 기들을 나타내며,(식중, R5,R5'및 R5"는 각각 독립적으로, 수소원자, 할로겐원자, 직쇄 또는 측쇄의 C1~C4알킬, 히드록실, C1~C4알콕시, 니트로, 트리플루오로메틸, 트리플루오로메톡시, 시아노, 아미노, 카르복실, C1~C4카르복시알킬 또는 페닐을나타낸다. ㆍC1~C4알킬로 치환되거나 치환되지 않은 나프틸기, ㆍ피리딜기,ㆍC1~C4알킬로 치환되거나 치환되지 않은 스티릴기, -또는 대신, RIv및 Rv가 함꼐 하기를 기를 나타내는 것으로 고려된다.(식중, 페닐기 5위치에서 피라졸을 치환하고 -(CH2)i-기(i=1내지 3가 4위치에서 피라졸을 치환하며, W1,W2및 W3이 벤젠고리를 치환하고 독립적으로 수소,할로겐 또는 히드록실기를 나타낸다)
- R1이 제1항에서 정의된 R1,R1'및 R1"로 치환된 나프틸 또는 페닐기를 나타냄을 특징으로 하는 식(Ⅰ)의 3-아미도피라졸(식중, R,X,X',n,Z,RIv및 Rv는 제1항에서 정의된 바와 같다)또는 그와 유기 또는 무기산과의 가능한 염 또는그와 유기 또는 무기염기와 가능한 염.
- Rv가 제1항에서 정의된, 바람직하게는 수소 또는 C1~C4알콕시인 R5,R5'및 R5"로 치환된 나프틸 또는 페닐기를 나타냄을 특징으로 하는 식(Ⅰ)또는(Ⅰ')의3-아미도피라졸(식중, R,X,X',n,Z,R1또는 RIa및 RIv는 제1항에서 정의된 바와같다)또는 그와 유기 또는 무기산과의 가능한 염 또는 그와 유기 또는 무기명기와의 가능한 염.
- X,X'및 그들이 연결된 탄소원자가 하기식의 기:(식중, n1,n1',n2,n3및 W는 제1항에서 정의된 바와 같다)또는 하기식의아다만틸기 ;(식중, n4,n5및 W는 제1항에서 정의된 바와 같다)를 형성하고 언급된a및b의 기가 하나의 고리 또는 다른고리의 한 탄소원자를 통해 상기 정의된 -N(R)-및-C(O)-Z에 결합되고 상기a및b의 고리가 하나의 고리 및/도는 다른 고리위에서 한 또는 둘의 C1~C4알킬기로 임의 치환가능하며 아미노산이 W가 산소를 나타낼때 W에 대해 α-위치에 존재하는 것이 가능하지 않음을 특징으로하는 식(Ⅰ)의 3-아미도피라졸(식중, R,Z,n,RIv및 Rv는 제1항에서 정의된 바와 같다)또는 그와 유기 또는 무기산과의 가능한 염 또는 그와 유기 또는 무기 염기와의 가능한 염.
- 하기식(Ⅱ)또는 (Ⅱ')의 피라졸카르복실산 :(식중, R1,RIv,Rv및 RIa는 상기 정의된 바와 같다)작용유도체를 펩티드 합성에서 관습적인 보호기에 의해 임의 보호된 하기식의 아미노산 :(식중, R,n,X,X'및 Z는 상기 정의된 바와같다)으로 처리하고 그렇게 수득한화합물을 그의 염중 하나로 변환시킴을 특징으로 하는 식(Ⅰ)및(Ⅰ')의 화합물의 제조방법.
- 제1항 내지 4항중 어느 하나에 따르는 화합물을 활성 성분으로 함유하는 약학 조성물 또는 그의 약학적으로 수용 가능한 염.
- 제6항에 있어서, 단위 투여 형태를 갖는 약학 조성물.
- 제7항에 있어서, 적어도 하나의 부형제와 혼합된 1내지 250mg의 활성 성분을 함유함을 특징으로 하는 약학 조성물.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR90-10486 | 1990-08-20 | ||
| FR9010486A FR2665898B1 (fr) | 1990-08-20 | 1990-08-20 | Derives d'amido-3 pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
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| Publication Number | Publication Date |
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| KR920004354A true KR920004354A (ko) | 1992-03-27 |
| KR100223074B1 KR100223074B1 (ko) | 1999-10-15 |
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| KR1019910014358A Expired - Fee Related KR100223074B1 (ko) | 1990-08-20 | 1991-08-20 | 3-아미도피라졸 유도체 및 그 제조방법과 그것을 함유한 약학 조성물 |
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| JP (1) | JP2694932B2 (ko) |
| KR (1) | KR100223074B1 (ko) |
| AR (1) | AR248133A1 (ko) |
| AT (1) | ATE187167T1 (ko) |
| AU (1) | AU646683B2 (ko) |
| BR (1) | BR9103550A (ko) |
| CA (4) | CA2166903C (ko) |
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| DE (1) | DE69131813T2 (ko) |
| DK (1) | DK0477049T3 (ko) |
| ES (1) | ES2142798T3 (ko) |
| FI (1) | FI104170B1 (ko) |
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| IE (1) | IE912932A1 (ko) |
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| US4792565A (en) * | 1986-04-24 | 1988-12-20 | Mitsui Toatsu Chemicals, Inc. | Pyrazolecarbonylamine derivatives and agricultural and horticultural fungicides containing said compounds |
| US4826868A (en) * | 1986-05-29 | 1989-05-02 | Ortho Pharmaceutical Corporation | 1,5-Diaryl-3-substituted pyrazoles pharmaceutical compositions and use |
| US4791112A (en) * | 1987-02-02 | 1988-12-13 | The Boc Group, Inc. | N-heterocyclic-N-(4-piperidyl)amides and pharmaceutical compositions and methods employing such compounds |
| US4954506A (en) * | 1987-02-02 | 1990-09-04 | Boc, Inc. | N-heterocyclic-N-(4-piperidinyl)amides and pharmaceutical compositions and methods employing such compounds |
| US4912109A (en) * | 1987-02-02 | 1990-03-27 | Boc, Inc. | N-heterocyclic-N-(4-piperidinyl) amides and pharmaceutical compositions and methods employing such compounds |
| US4916142A (en) * | 1987-02-02 | 1990-04-10 | Boc, Inc. | N-heterocyclic-N-(4-piperidinyl)amides and pharmaceutical compositions and their use as analgesics |
| JPS6425763A (en) * | 1987-04-24 | 1989-01-27 | Mitsubishi Chem Ind | Pyrazoles and insecticide and acaricide containing said pyrazoles as active ingredient |
| US4971978A (en) * | 1987-09-21 | 1990-11-20 | Nadzan Alex M | Derivatives of D-glutamic acid and D-aspartic acid |
| WO1989005300A1 (en) * | 1987-11-30 | 1989-06-15 | E.I. Du Pont De Nemours And Company | Heterocyclic pyrazoline carboxanilides |
| JP2861104B2 (ja) * | 1988-10-14 | 1999-02-24 | 三菱化学株式会社 | ピラゾールアミド類およびこれを有効成分とする殺虫、殺ダニ剤 |
| AU5650890A (en) * | 1989-05-24 | 1990-12-18 | Nippon Shinyaku Co. Ltd. | Indole derivatives and medicine |
-
1990
- 1990-08-20 FR FR9010486A patent/FR2665898B1/fr not_active Expired - Fee Related
-
1991
- 1991-08-17 HU HU750/91A patent/HU217435B/hu unknown
- 1991-08-19 FI FI913917A patent/FI104170B1/fi active
- 1991-08-19 RU SU5001452/04A patent/RU2066317C1/ru not_active IP Right Cessation
- 1991-08-19 IE IE293291A patent/IE912932A1/en not_active IP Right Cessation
- 1991-08-19 PT PT98717A patent/PT98717B/pt not_active IP Right Cessation
- 1991-08-19 AR AR91320430A patent/AR248133A1/es active
- 1991-08-19 TW TW080106546A patent/TW366337B/zh not_active IP Right Cessation
- 1991-08-19 NO NO913234A patent/NO300212B1/no unknown
- 1991-08-19 BR BR919103550A patent/BR9103550A/pt not_active Application Discontinuation
- 1991-08-19 PL PL91291463A patent/PL169085B1/pl not_active IP Right Cessation
- 1991-08-19 IL IL9922591A patent/IL99225A/en not_active IP Right Cessation
- 1991-08-20 CA CA002166903A patent/CA2166903C/en not_active Expired - Fee Related
- 1991-08-20 CA CA002166902A patent/CA2166902C/en not_active Expired - Fee Related
- 1991-08-20 JP JP3208108A patent/JP2694932B2/ja not_active Expired - Fee Related
- 1991-08-20 AT AT91402269T patent/ATE187167T1/de not_active IP Right Cessation
- 1991-08-20 AU AU82596/91A patent/AU646683B2/en not_active Ceased
- 1991-08-20 CA CA002049514A patent/CA2049514C/en not_active Expired - Fee Related
- 1991-08-20 NZ NZ239476A patent/NZ239476A/xx not_active IP Right Cessation
- 1991-08-20 CZ CS912574A patent/CZ281864B6/cs not_active IP Right Cessation
- 1991-08-20 ES ES91402269T patent/ES2142798T3/es not_active Expired - Lifetime
- 1991-08-20 DE DE69131813T patent/DE69131813T2/de not_active Expired - Fee Related
- 1991-08-20 ZA ZA916583A patent/ZA916583B/xx unknown
- 1991-08-20 CA CA002166901A patent/CA2166901C/en not_active Expired - Fee Related
- 1991-08-20 MY MYPI91001513A patent/MY121908A/en unknown
- 1991-08-20 DK DK91402269T patent/DK0477049T3/da active
- 1991-08-20 KR KR1019910014358A patent/KR100223074B1/ko not_active Expired - Fee Related
- 1991-08-20 EP EP91402269A patent/EP0477049B1/fr not_active Expired - Lifetime
- 1991-08-20 SG SG1996002749A patent/SG52322A1/en unknown
-
1992
- 1992-06-26 MX MX9203576A patent/MX9203576A/es unknown
-
1993
- 1993-02-25 LV LVP-93-138A patent/LV10434B/en unknown
- 1993-06-15 LT LTIP656A patent/LT3520B/lt not_active IP Right Cessation
- 1993-09-13 US US08/119,830 patent/US5420141A/en not_active Expired - Lifetime
-
1995
- 1995-02-24 US US08/393,829 patent/US5635526A/en not_active Expired - Fee Related
- 1995-02-27 US US08/394,757 patent/US5607958A/en not_active Expired - Fee Related
- 1995-02-27 US US08/394,756 patent/US5616592A/en not_active Expired - Fee Related
- 1995-06-30 HU HU95P/P00632P patent/HU211970A9/hu unknown
-
1996
- 1996-12-31 US US08/775,150 patent/US5744493A/en not_active Expired - Fee Related
-
1997
- 1997-01-02 US US08/778,105 patent/US5744491A/en not_active Expired - Fee Related
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2000
- 2000-02-23 GR GR20000400431T patent/GR3032732T3/el not_active IP Right Cessation
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