KR890009890A - 하이드록시 피리미딘의 아실 유도체 - Google Patents

하이드록시 피리미딘의 아실 유도체 Download PDF

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KR890009890A
KR890009890A KR1019880015981A KR880015981A KR890009890A KR 890009890 A KR890009890 A KR 890009890A KR 1019880015981 A KR1019880015981 A KR 1019880015981A KR 880015981 A KR880015981 A KR 880015981A KR 890009890 A KR890009890 A KR 890009890A
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substituted
dimethyl
phenyl
alkyl
phenylalkyl
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젓슨 워커 프레드릭
로렌스 라마티나 죤
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알렌 제이.스피겔
화이자 인코포레이티드
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Abstract

내용 없음

Description

하이드록시 피리미딘의 아실 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 일반식(Ⅰ)의 화합물, 이의 약제학적으로 허용되는 산부가염, 및 일반식(Ⅰ)에서 R5가 (C2-C3)알킬카복시인 경우, 이의 약제학적으로 허용되는 염기부가염.
    상기식에서, R1은 수소 또는 (C1-C15)알킬이고; R2는 수소, (C1-C15)알킬, 사이클로펜틸, 사이클로헥실, (C2-C15알케닐,페닐, 치환된 페닐, (C7-C20)페닐알킬, 또는 치환된 (C7-C20)페닐알킬이거나; R1및 R2가 이들의 결합된 질소원자와 함께는 하나의 (C1-C6)알킬, 페닐 또는 치환된 페닐,(C7-C20)페닐알킬,치환된 (C7-C20)페닐알킬, 푸틸, 티에틸, 하나의 (C1-C6)알킬에 의해 치환된 푸릴, 또는 하나의 (C1-C2)알킬에 의해 치환된 테에닐이며; R4는 수소,(C1-C6)알킬, 페닐, 치환된 페닐, (C7-C10)페닐알킬, 또는 치환된(C7-C10)페닐알킬이며; R6는 수소,(C1-C10)알킬, (C7-C10)알콕시, 페닐,(C7-C10)페닐알킬, 치환된 (C7-C20)페닐알킬, (C2-C3)알킬카복시, 또는 -NR6R7(여기에서, R6및 R7은 독립적으로, (C1-C10)알킬, 페닐, 치환된 페닐, (C7-C20)페닐알킬 및 치환된 (C7-C20)페닐알킬로 구성된 그룹에서 선택된다)이고; 상기의 치환된 페닐 및 치환된 피닐알킬상의 페닐 잔기는 플루오로, 플로로,(C1-C3)알킬,(C1-C3)알콕시 및 CF3로 구성된 그룹에서 선택된 잔기 하나 또는 두개에 의해 치환될수 있으며, 단, R1및 R2둘다 수소인 경우, R5는 메틸일 수 없다.
  2. 제1항에 있어서, R2가 수소, (C1-C15)알킬, 페닐, 치환된 페닐, (C7-C20)페닐알킬, 또는 치환된 (C7-C20)페닐알킬, (여기에서, 치환된 페닐 및 치환된 페닐알킬상의 페닐 잔기는 클로로 및 (C1-C3)알킬로 구성된 그룹으로부터 선택된 잔기 하나 또는 두개에 의해 치환되며);이고R2가 (C1-C6)알킬 또는 페닐기이거나,또는 플루오로, 클로로, 메틸, 에틸, 메톡시, 에톡시, 및 C2로 구성된 그룹으로부터 선택된 잔기 하나 또는2개에 의해 치환된 페닐이며;R4는 수소, (C1-C6)알킬, 또는 페닐기이거나, 메틸 및 에틸로 구성된 그룹으로부터 선택된 잔기 하나 또는 두개에 의해 치환된 페닐인 화합물.
  3. 제2항에 있어서, R1이 수소이고, R2가 수소가 아닌 화합물.
  4. 제1항에 있어서, R1이 수소이고, R2는 플루오로, 플로로, (C1-C3)알킬, (C1-C6)알콕시, 및 CF3로구성된 그룹으로부터 선택된 잔기 하나 또는 두개에 의해 페닐잔기가 치환될 수 있는 (C7-C12)페닐알킬인 화합물.
  5. 제1항에 있어서, R1이 수소이고, R2가 (C8-C9)알킬, (C9-C12)페닐알킬, (C10-C12)p-클로로페닐알킬 또는(C10-C12)P- 메틸페닐알킬이며, R3및 R4각각이 메틸이고, R5가 (C1-C6)-알킬 또는 (C1-C6)알콕시인 화합물.
  6. 제1항에 있어서, 5-아세톡시-4,6-디메틸-2-페닐헥실아미노피리미딘 및 4,6-디메틸-2-페닐헥실아미노-5-(에틸옥시포르밀)-옥시피리미딘으로 구성된 그룹으로부터 선택된 화합물 및 이의 산부가염.
  7. 제1항에 있어서, 5-벤조일옥시-4,6-디메틸-2-페닐헥실아미노피리미딘, 4,6-디메틸-2-페닐헥실아미노-5-O-톨루일옥시피리미딘, 5-카프로일옥시-4,6-디메틸-2-페닐헥실아미노피리미딘, 5-[옥소-(1-카복시-5-페닐펜탄)]-4,6-디메틸-2-페닐헥실아미노피리미딘, 4,6-디메틸-5-[(p-N,N-디에틸메틸아미노)]벤조일옥시-2-페닐헥실아미노피리미딘, 4,6-디메틸-2-페닐헥실아미노-5-석시노일옥시피리미딘, 4,6-디메틸-5-[(-모르폴리노메틸)]벤조일옥시-2-페닐헥실아미노피리미딘, 4,6-디메틸-2-페닐헥실아미노-5-프로파노일옥시피리미딘, 4,6-디메틸-2-페닐아미노-5-(2-티에노일)옥시피리미딘, 4,6-디메틸-2-페닐헥실아미노-5-(페닐옥시포르밀)옥시피리미딘, 4,6-디메틸-2-페닐헥실아미노-5-(이소부틸옥시프로밀)옥시피리미딘, 5-(N,N-디메틸아미노포르밀)옥시-4,6-디메틸-2-페닐헥실아미노피리미딘, 5-(N,N-디메틸아미노포르밀)옥시-4-이소프로필-6-메틸-2-페닐헥실아미노피리미딘, 4,6-디메틸-5-옥소(1-카복시-2,2-디메틸프로판)-2-페닐펜틸아미노피리미딘, 4,6-디메틸-2-페닐펜틸아미노-5-(이소부틸옥시포르밀)옥시피리미딘, 5-벤조일옥시-4,6-디메틸-2-페닐헥실아미노피리미딘 및 5-(N,N-디메틸아미노포르밀)옥시-4,6-디메틸-2-페닐펜틸아미노피리미딘으로 구성된 그룹으로부터 선택된 화합물 및 이의 산부가염.
  8. 폐질환, 천식, 알레르기성 질환 또는 염증성 질환중 하나 이상의 질환을 치료하기에 유용한 양의 제1 내지 7항중 어느 한 항에 따라 화합물 및 약제학적으로 허용되는 담체를 함유함을 특징으로 하는, 상기의 질환치료용 약제학적 조성물.
  9. 폐질환, 천식, 알레르기성 질환,건선, 또는 염증성 질환의 치료를 필요로 하는 포유동물에 제1내지7항중 어느 한 항에 따른 화합물을 투여함을 특징으로 하는 상기 질환의 치료방법.
  10. 류코트리엔의 합성억제를 필요로 하는 포유동물에 유효량의 제1내지 7항중 어느 한 항에 따른 화합물을 투여함을 특징으로 하여, 포유동물의 류코트리엔 합성을 억제하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019880015981A 1987-12-02 1988-12-01 하이드록시 피리미딘의 아실 유도체 KR910000415B1 (ko)

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PCT/US1987/003171 WO1989005295A1 (en) 1987-12-02 1987-12-02 Acyl derivatives of hydroxypyrimidines
USPCT/US87/03171 1987-12-02
USPCT/8703171 1987-12-02

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KR890009890A true KR890009890A (ko) 1989-08-04
KR910000415B1 KR910000415B1 (ko) 1991-01-25

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US5270319A (en) * 1991-09-09 1993-12-14 Warner-Lambert Company 5-hydroxy-2-pyrimidinylmethylene derivatives useful as antiinflammatory agents
US5220025A (en) * 1992-02-24 1993-06-15 Warner-Lambert Company 2-substituted amino-4, 6-di-tertiary-butyl-5-hydroxy-1, 3-pyrimidines as antiinflammatory agents
US5196431A (en) * 1992-02-24 1993-03-23 Warner-Lambert Company 2-substituted amino-4, 6-di-tertiary-buthyl-5-hydroxy-1, 3-pyrimidines as antiinflammatory agents
AU2003232650A1 (en) * 2003-05-06 2004-11-26 Il Yang Pharm Co., Ltd. N-phenyl-2-pyrimidine-amine derivatives and process for the preparation thereof
KR20170057191A (ko) * 2017-05-04 2017-05-24 김점식 유압을 이용한 전기 자동차 구동장치

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US4554276A (en) * 1983-10-03 1985-11-19 Pfizer Inc. 2-Amino-5-hydroxy-4-methylpyrimidine derivatives
US4711888A (en) * 1985-07-24 1987-12-08 Pfizer Inc. Hydroxy and alkoxy pyrimidines

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PL276122A1 (en) 1989-06-12
WO1989005295A1 (en) 1989-06-15
JPH01250364A (ja) 1989-10-05
MX14001A (es) 1993-06-01
DE3879410D1 (de) 1993-04-22
PT89124A (pt) 1988-12-01
EP0319170A2 (en) 1989-06-07
DK671188D0 (da) 1988-12-01
HUT55003A (en) 1991-04-29
ATE86983T1 (de) 1993-04-15
JPH0725740B2 (ja) 1995-03-22
DD277275A5 (de) 1990-03-28
DE3879410T2 (de) 1993-06-24
EP0319170A3 (en) 1990-08-01
YU217988A (en) 1990-10-31
HU894552D0 (en) 1990-11-28
MY103499A (en) 1993-06-30
PT89124B (pt) 1993-04-30
ES2053769T3 (es) 1994-08-01
IE883598L (en) 1989-06-02
CA1336516C (en) 1995-08-01
KR910000415B1 (ko) 1991-01-25
FI893648A0 (fi) 1989-08-01
EG19003A (en) 1994-06-30
RU2036909C1 (ru) 1995-06-09
HU206203B (en) 1992-09-28
IE63456B1 (en) 1995-04-19
ZA888969B (en) 1990-07-25
AU609547B2 (en) 1991-05-02
EP0319170B1 (en) 1993-03-17
YU47013B (sh) 1994-11-15
CN1033379A (zh) 1989-06-14
NZ227163A (en) 1990-11-27
NO893105L (no) 1989-09-27
AU2647088A (en) 1989-06-08
PL158165B1 (pl) 1992-08-31
DK671188A (da) 1989-07-28
IL88512A0 (en) 1989-06-30
NO893105D0 (no) 1989-08-01

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