KR900701792A - Acat 효소를 차단하는데 효과적인 이가 리간드 - Google Patents

Acat 효소를 차단하는데 효과적인 이가 리간드

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Publication number
KR900701792A
KR900701792A KR1019900700773A KR900700773A KR900701792A KR 900701792 A KR900701792 A KR 900701792A KR 1019900700773 A KR1019900700773 A KR 1019900700773A KR 900700773 A KR900700773 A KR 900700773A KR 900701792 A KR900701792 A KR 900701792A
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KR
South Korea
Prior art keywords
alkyl
aryl
dipiperidine
composition
bis
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KR1019900700773A
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English (en)
Inventor
비이 갬밀 로날드
피이 벨 프랭크
Original Assignee
로버어트 에이 아미테이지
디 엎죤 캄파니
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Application filed by 로버어트 에이 아미테이지, 디 엎죤 캄파니 filed Critical 로버어트 에이 아미테이지
Publication of KR900701792A publication Critical patent/KR900701792A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
    • C07F7/0814—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring said ring is substituted at a C ring atom by Si

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Immobilizing And Processing Of Enzymes And Microorganisms (AREA)

Abstract

내용 없음

Description

ACAT 효소를 차단하는데 효과적인 이가 리간드
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. α가 일반식:
    (여기서, X 및 Y는 독립적으로 O, N 또는 S이고: A는 C=CH-Z, N=C-Z 또는 CR5=C-(CH2)n-Z이고: R1및 R2는 독립적으로 a) H, b) 할로, c) 알킬, d) -(CH2)p-아릴, e) -(CH2)p-헤테로아릴, f) -(CH2)p-CO2R6, g) -(CH2)p-C0NR7R8, h) -Si(R9), i) -(CH2)n-NR7R8, j) -(CH2)n-OR10, k) -CF3, 또는 1)-(CH2)n-SR6-(CH2)n-S0R6, -(CH2)n-SO2R6이고: R3는a) 0H, b) OCH2CH=CH2, c) OCH2CH(OH)CH2NHR6, d) -O-알킬, e) -O-(CH2)n-CO2R6, 또는 f) -O-(CH2)n-C0NR|7R8:이고; R4는 a) 수소, b) 할로 c) NO2, d) NH2, e) CF3, f) 알킬, g) 아릴, h) -S-알킬 또는 아틸, i) -SO-알킬 또는 아틸, j) -SO2-알킬 또는 아릴, k) R3, 또는 1) -(CH2)n-NR7R|8: 이고: Z는 일차, 이차 또는 삼차 아민이고: R5는 수소, NO2, NH2, CF3, 알킬, 아릴, -S-알킬, -S-아릴 또는 헤테로아릴, -SO-알킬 또는 아릴, -SO2-알킬 또는 아릴 또는 R3이고: R6는 H. CF3, 알킬 또는 아릴, Li+, Na+, K+, Ca2+및 카르복시산에 대한 다른 제약학적으로 허용가능한 반대 이온이고;R7및 R8은 H, CO -알킬, CO-아릴, 알킬시클로알킬, 알킬-아릴, 아릴, 헤테로알킬, 아릴이거나 R7및 R8은 함께 피페리딘 고리 또는 모르폴린 고리를 형성할 수 있고: R9는 알킬 또는 아릴이고: R10은 H, CF3, 알킬, 아릴 또는 헤테로아릴이고: n은 O-5이고 P는 O-8임)에 의해 구조적으로 표현되고, β는
    (여기서, W는 -CH2-(Xn-CH2)n-이고: X는 N,O 또는 S이고: R11은 알킬, CO-알킬 또는 CON-알킬 또는 -아릴이고 m은 O-4이고, n은 O-5이고 O는 1-5임)으로 구성되는 군으로부터 선택되는, 이가 리간드 α-β-α로 구성되는 화합물.
  2. 제1항에 있어서, 상기 사슬이 a) 트리메틸렌-4,4-디피페리딘, b) 1,2-에탄디일-4,4-디피페리딘, c) 1,4-비스(아미노프로필피페라진), 또는 d) 1,8-디아미노옥탄인 화합물.
  3. 제1항에 있어서, 7,7'-〔1,2-에탄디일비스(4,1-피페리딘디일메틸렌)〕-비스-〔4,9-디메톡시-5H-푸로〔3,2-g〕〔1〕-벤조피란-5-온인 화합물.
  4. 제1항의 조성물의 약리학적양을 투여시킴으로 구성되는 ACAT효소를 차단하거나 억제하는 방법.
  5. 상기 투여를 보조외과, 관상의 보조 외과, 혈관형성 또는 이식조직으로 계속해서 실시하는 방법.
  6. 제4항에 있어서, 상기 사슬이 a) 트리메틸렌-4,4-디피페라딘, b) 1,2-에탄디일-4,4-디피페리딘, c) 1,4-비스(아미노프로필페라진), 또는 d) 1,8-디아미노옥탄인 방법.
  7. 제4항에 있어서, 상기 조성물이 7,7'-〔1,2-에탄디일비스(4,1-피페리딘디일메틸렌)〕-비스〔4,9-디메톡시-5H-푸로〔3,2-g〕〔1〕-벤조피란-5-온인 방법.
  8. 제1항의 조성물의 약리학적 양을 투여시킴으로 구성되는 아테롬성 동맥경화증을 예방 또는 치료하는 방법.
  9. 제8항에 있어서, 상기 사슬이 a) 트리에틸렌-4,4-디피페리딘, b) 1,2-에탄디일-4,4-디피페리딘, c) 1,4-비스(아미노프로필리페라진). 또는 d) 1,8-디아미노옥탄인 방법.
  10. 제8항에 있어서, 상기 조성물이 7,7'-〔1,2-에탄디일비스(4,1-피페리딘디일메틸렌)〕-비스〔4,9-디메톡시-5H-푸로〔3,2-g〕〔1〕-벤조피란-5-온인 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900700773A 1988-08-16 1989-06-16 Acat 효소를 차단하는데 효과적인 이가 리간드 KR900701792A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US23293188A 1988-08-16 1988-08-16
US07/232,931 1988-08-16
PCT/US1989/002572 WO1990002129A1 (en) 1988-08-16 1989-06-16 Bivalent ligands effective for blocking acat enzyme

Publications (1)

Publication Number Publication Date
KR900701792A true KR900701792A (ko) 1990-12-04

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ID=22875168

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Application Number Title Priority Date Filing Date
KR1019900700773A KR900701792A (ko) 1988-08-16 1989-06-16 Acat 효소를 차단하는데 효과적인 이가 리간드

Country Status (7)

Country Link
EP (1) EP0429464B1 (ko)
JP (1) JPH04500506A (ko)
KR (1) KR900701792A (ko)
AT (1) ATE114311T1 (ko)
DE (1) DE68919475T2 (ko)
DK (1) DK25691A (ko)
WO (1) WO1990002129A1 (ko)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5304548A (en) * 1988-08-16 1994-04-19 The Upjohn Company Bivalent ligands effective for blocking ACAT enzyme for lowering plasma triglycerides and for elevating HDL cholesterol
US5180717A (en) * 1988-08-16 1993-01-19 The Upjohn Company Bivalent ligands effective for blocking ACAT enzyme for lowering plasma triglycerides and for elevating HDL cholesterol
WO1995027964A1 (en) * 1994-04-12 1995-10-19 Qualcomm Incorporated Method and apparatus for freight transportation using a satellite navigation system
JPWO2009038064A1 (ja) * 2007-09-19 2011-01-06 株式会社医薬分子設計研究所 Ｉ型１１βヒドロキシステロイド脱水素酵素阻害活性を有する複素環誘導体
PL2268644T3 (pl) * 2008-03-05 2012-01-31 Boehringer Ingelheim Int Tricykliczne pochodne piperydyny, leki zawierające te związki, ich zastosowanie i sposoby ich wytwarzania
MX2012009149A (es) 2010-02-19 2012-09-28 Boehringer Ingelheim Int Derivados de piridina triciclicos, medicamentos que contienen tales compuestos, su uso y proceso para su preparacion.
US9150583B2 (en) 2011-08-17 2015-10-06 Boehringer Ingelheim International Gmbh Furo[3,4-c]quinoline derivatives, medicaments containing such compounds, their use and process for their preparation
CN107021940A (zh) * 2017-05-03 2017-08-08 天津国际生物医药联合研究院 一种双哌嗪类化合物及其应用

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU529561B2 (en) * 1979-02-13 1983-06-09 Upjohn Company, The Antiatherogenic 6-halofurochromones
US4412071A (en) * 1982-05-17 1983-10-25 The Upjohn Company Antiatherosclerotic compositions

Also Published As

Publication number Publication date
EP0429464B1 (en) 1994-11-23
DE68919475D1 (de) 1995-01-05
EP0429464A1 (en) 1991-06-05
ATE114311T1 (de) 1994-12-15
DK25691D0 (da) 1991-02-14
WO1990002129A1 (en) 1990-03-08
AU3835889A (en) 1990-03-23
DK25691A (da) 1991-02-14
JPH04500506A (ja) 1992-01-30
DE68919475T2 (de) 1995-05-11
AU631801B2 (en) 1992-12-10

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