KR20030015898A - 뉴로키닌-1 수용체 길항제로서의 4-페닐-피리딘 유도체 - Google Patents
뉴로키닌-1 수용체 길항제로서의 4-페닐-피리딘 유도체 Download PDFInfo
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Abstract
Description
mg/정제 | |
활성 물질 | 5 |
락토즈 | 45 |
옥수수 전분 | 15 |
미세정질 셀룰로즈 | 34 |
마그네슘 스테아레이트 | 1 |
총 중량 | 100 |
mg/캡슐 | |
활성 물질 | 10 |
락토즈 | 155 |
옥수수 전분 | 30 |
활석 | 5 |
캡슐 충전 중량 | 200 |
mg/좌약 | |
활성 물질 | 15 |
좌약 부형약 | 1285 |
총 중량 | 1300 |
Claims (16)
- 하기 화학식 IA 또는 IB의 화합물 또는 그의 약학적으로 허용가능한 산 부가염:화학식 IA화학식 IB상기 식에서,R1은이거나, 또는 -NH(CH2)2OH, -NR3C(O)CH3또는 -NR3C(O)-사이클로프로필이고;R2는 메틸 또는 클로로이고;R3은 수소 또는 메틸이고;R은 수소 또는 -(CH2)2OH이고;n은 1 또는 2이다.
- 제 1 항에 있어서,화학식 IA에서 R2가 메틸인 화합물.
- 제 2 항에 있어서,N-(3,5-비스-트리플루오로메틸-벤질)-N-메틸-4-o-톨릴-6-[1,2,4]트리아졸-1-일-니코틴아미드,N-(3,5-비스-트리플루오로메틸-벤질)-6-(2-하이드록시-에틸아미노)-N-메틸-4-o-톨릴-니코틴아미드,4-하이드록시-4'-o-톨릴-3,4,5,6-테트라하이드로-2H-[1,2']비피리디닐-5'-카복실산 (3,5-비스-트리플루오로메틸-벤질)-메틸-아미드,4-(2-하이드록시-에톡시)-4'-o-톨릴-3,4,5,6-테트라하이드로-2H-[1,2']비피리디닐-5'-카복실산 (3,5-비스-트리플루오로메틸-벤질)-메틸-아미드 또는(R)-N-(3,5-비스-트리플루오로메틸-벤질)-6-(3-하이드록시-피롤리딘-1-일)-N-메틸-4-o-톨릴-니코틴아미드인 화합물.
- 제 1 항에 있어서,화학식 IA에서 R2가 클로로인 화합물.
- 제 4 항에 있어서,4'-(2-클로로-페닐)-4-하이드록시-3,4,5,6-테트라하이드로-2H-[1,2']비피리디닐-5'-카복실산 (3,5-비스-트리플루오로메틸-벤질)-메틸-아미드인 화합물.
- 제 1 항에 있어서,화학식 IB에서 R2가 메틸인 화합물.
- 제 6 항에 있어서,2-(3,5-비스-트리플루오로메틸-페닐)-N-[6-(2-하이드록시-에틸아미노)-4-o-톨릴-피리딘-3-일]-N-메틸-이소부티르아미드,2-(3,5-비스-트리플루오로메틸-페닐)-N-[6-(2,3-디하이드로-[1,4]옥사진-4-일)-4-o-톨릴-피리딘-3-일]-N-메틸-이소부티르아미드,N-(6-아세틸아미노-4-o-톨릴-피리딘-3-일)-2-(3,5-비스-트리플루오로메틸-페닐)-N-메틸-이소부티르아미드,N-[6-(아세틸-메틸-아미노)-4-o-톨릴-피리딘-3-일]-2-(3,5-비스-트리플루오로메틸-페닐)-N-메틸-이소부티르아미드,사이클로프로판카복실산 (5-{[2-(3,5-비스-트리플루오로메틸-페닐)-2-메틸-프로피오닐]-메틸-아미노}-4-o-톨릴-피리딘-2-일)-아미드,사이클로프로판카복실산 (5-{[2-(3,5-비스-트리플루오로메틸-페닐)-2-메틸-프로피오닐]-메틸-아미노}-4-o-톨릴-피리딘-2-일)-메틸-아미드 또는2-(3,5-비스-트리플루오로메틸-페닐)-N-(6-이미다졸-1-일-4-o-톨릴-피리딘-3-일)-N-메틸-이소부티르아미드인 화합물.
- 제 1 항에 있어서,화학식 IB에서 R2가 클로로인 화합물.
- 제 8 항에 있어서,2-(3,5-비스-트리플루오로메틸-페닐)-N-[4-(2-클로로-페닐)-6-(2-하이드록시-에틸아미노)-피리딘-3-일]-N-메틸-이소부티르아미드인 화합물.
- 제 1 항 내지 제 9 항 중 어느 한 항에 따른 하나 이상의 화합물 및 약학적으로 허용가능한 부형제를 함유하는 약제.
- 제 10 항에 있어서,NK-1 수용체 길항제와 관련된 질병 치료용 약제.
- a) 하기 화학식 II의 화합물을 화학식 III의 화합물과 반응시켜 화학식 IB의 화합물을 제조하거나:화학식 II화학식 III화학식 IB(상기 식에서 R1및 R2는 제 1 항에 주어진 의미를 가짐),b) 하기 화학식 IV의 화합물을 화학식 V의 화합물과 반응시켜 화학식 IA의 화합물을 수득하거나:화학식 IV화학식 V화학식 IA(상기 식에서 R1및 R2는 제 1 항에 주어진 의미를 가짐),c) 하기 화학식 VI의 화합물을 화학식 VII의 화합물과 반응시켜 화학식 IA의 화합물을 제조하거나:화학식 VI화학식 VII화학식 IA(상기 식에서 Z는 Cl, Br, I, -OS(O)2C6H4CH3또는 -OS(O)2CH3이고 치환체의 다른 정의는 제 1 항에 주어짐),d) 하기 화학식 VIII 또는 IX의 화합물을 화학식 XIV의 화합물과 반응시켜 화학식 IA 또는 IB의 화합물을 제조하는 단계:화학식 VIII화학식 IX화학식 XIVR1H화학식 IA화학식 IB(상기 식에서 치환체의 정의는 제 1 항에 주어짐), 및바라는 경우 수득된 화합물을 약학적으로 허용가능한 산 부가염으로 전환시키는 단계를 포함하는, 제 1 항에 정의된 화학식 I의 화합물의 제조 방법.
- 제 1 항 내지 제 9 항 중 어느 한 항에 있어서,제 12 항의 방법 또는 그와 동등한 방법으로 제조된 화합물.
- NK-1 수용체 길항제와 관련된 질병 치료를 위한 제 1 항 내지 제 9 항 중 어느 한 항의 화합물의 용도.
- 화학식 I의 하나 이상의 화합물을 함유하는 NK-1 수용체 길항제와 관련된 질병 치료용 약제의 제조를 위한 제 1 항 내지 제 9 항 중 어느 한 항의 화합물의 용도.
- 본원에 기술된 바와 같은 발명.
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EP00115846 | 2000-07-24 | ||
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PCT/EP2001/008432 WO2002008232A1 (en) | 2000-07-24 | 2001-07-20 | 4-phenyl-pyridine derivatives as neurokinin-1 receptor antagonists |
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EP1103545B1 (en) * | 1999-11-29 | 2003-11-05 | F. Hoffmann-La Roche Ag | 2-(3,5-Bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide |
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WO2003091227A1 (en) | 2002-04-26 | 2003-11-06 | Eli Lilly And Company | Tachykinin receptor antagonists |
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EP1638944A1 (en) * | 2003-06-12 | 2006-03-29 | Eli Lilly And Company | Tachykinin receptor antagonists |
CA2530886C (en) * | 2003-07-03 | 2013-05-28 | F. Hoffmann-La Roche Ag | Dual nk1/nk3 antagonists for treating schizophrenia |
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KR101119365B1 (ko) | 2006-05-31 | 2012-03-07 | 에프. 호프만-라 로슈 아게 | 아릴-4-에틴일-아이속사졸 유도체 |
WO2008090117A1 (en) | 2007-01-24 | 2008-07-31 | Glaxo Group Limited | Pharmaceutical compositions comprising 3, 5-diamin0-6- (2, 3-dichl0phenyl) -l, 2, 4-triazine or r (-) -2, 4-diamino-5- (2, 3-dichlorophenyl) -6-fluoromethyl pyrimidine and an nk1 |
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TWI649307B (zh) | 2014-05-07 | 2019-02-01 | 日商橘生藥品工業股份有限公司 | Cyclohexylpyridine derivative |
US10538491B2 (en) | 2015-03-16 | 2020-01-21 | Vanderbilt University | 4,5-substituted picolinamide and picolinonitrile metabotropic glutamate receptor 2 negative allosteric modulators |
CN108712913B (zh) | 2015-12-22 | 2022-06-24 | 武田药品工业株式会社 | 内体g蛋白-偶联的受体的三部分调节剂 |
JP2021514976A (ja) | 2018-02-26 | 2021-06-17 | オスペダーレ・サン・ラッファエーレ・エッセエッレエッレ | 眼痛の治療における使用のためのnk−1拮抗薬 |
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