KR900001688A - 벤조디아제핀 유도체 - Google Patents

벤조디아제핀 유도체 Download PDF

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KR900001688A
KR900001688A KR1019890009654A KR890009654A KR900001688A KR 900001688 A KR900001688 A KR 900001688A KR 1019890009654 A KR1019890009654 A KR 1019890009654A KR 890009654 A KR890009654 A KR 890009654A KR 900001688 A KR900001688 A KR 900001688A
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alkyl
hydrogen
halogen
compound
amino
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KR1019890009654A
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English (en)
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요시나리 사토
테루아키 마투오
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후지사와 도모키치로
후지사와 야쿠힌 고오교오 가부시기가이샤
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Priority claimed from GB888816207A external-priority patent/GB8816207D0/en
Priority claimed from GB888820560A external-priority patent/GB8820560D0/en
Priority claimed from GB888823660A external-priority patent/GB8823660D0/en
Application filed by 후지사와 도모키치로, 후지사와 야쿠힌 고오교오 가부시기가이샤 filed Critical 후지사와 도모키치로
Publication of KR900001688A publication Critical patent/KR900001688A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • 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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P3/04—Anorexiants; Antiobesity 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Otolaryngology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Abstract

내용 없음

Description

벤조디아제핀 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 하기 구조식(I)의 화합물 및 그의 약학적 허용염.
    상기식에서, R1은 할로겐, 하나 또는 그 이상의 적합한 치환체를 지닌 헤테로 시클릭기, 하나 또는 그 이상의 적합한 치환체를 지닌 아릴, -NH-R5(R5는 할로겐, 저급 알카노일 또는 히드록시(저급)알킬임), -S-R6(R6는 저급 알킬, 카르복시 및 아미노로 치환된 저급알킬, 보호된 카르복시 및 보호된 아미노로 치환된 저급알킬 또는 피리딜임), -O-R7(R7은 수소, 히드록시 보호기, 저급 알킬, 저급 알케닐, 아르(저급)알킬, 할로(저급)알킬, 아미노(저급)알킬, 보호된 아미노(저급)알킬 또는 저급 알킬을 지닌 피페라지닐(저급)알킬임), -CONH-R8(R8은 시아노, 카르바모일(저급)알킬, 카르복시(저급)알킬, 보호된 카르복시(저급)알킬, 보호된 카르복시(저급)알킬, 또는 카르바모일 및 아릴로 치환된 저급 알킬), 또는 -Z-R9[R9는 수소 또는 저급 알킬이고, Z는(R10은 히드록시, 저급 알콕시 또는 아미노) 또는(R11은 카르복시 또는 보호된 카르복시이고, R12는 수소이고; 혹은 R11은 할로겐이고, R12는 할로게임)]이며 R12는 하나 또는 그 이상의 적합한 치환체를 지닌 아릴이며, R3는 수소, 또는 할로겐이며, R4는 수소 할로겐 또는 저급 알콕시이며, A는 저급 알킬렌임.
  2. 제 1 항에 있어서, R12는 하나 또는 그 이상의 적합한 치환체를 지니는 헤테로 시클릭기인 화합물.
  3. 제 2 항에 있어서, R1은 저급 알킬 또는 아미노 보호기를 지닌 2 또는 3의 질소 원자를 함유한 5-원 헤테로 모노 시클릭기이고, R2는 할로겐 원자를 지닌 페닐기인 화합물.
  4. 제 3 항에 있어서, R1은 이미다졸일, 피라졸일 또는 트리아졸일이며, 그 각각은 저급 알킬 및 이미노 보호기 또는 저급 알킬 또는 이미노 보호기를 지니는 화합물.
  5. 제 4 항에 있어서, R1은 가급 알킬기를 지니는 이미다졸일이고, R3는 수소이고, R4는 수소이고, A는 C1-C3알킬렌인 화합물.
  6. 제 5 항에 있어서, (3S)-1,3-디하이드로-1-(4-이미다졸일메틸)-3-(2-인돌일카르보닐아미노)-5-(2-플루오로페닐)-2H-1,4-벤조 디아제핀-2-온인 화합물.
  7. (1)하기식(II)의 화합물 또는 그 염을 하기식(III)의 화합물 또는 그 염과 반응시켜 하기식(I)의 화합물 또는 그 염을 제조하고, 또는 (2) 하기식(IV)의 화합물 또는 아미노기에서의 그의 반응성 유도체 또는 그 염을 하기식(V)의 화합물 또는 카르복실기에서의 그의 반응성 유도체 또는 그 염을 반응시켜 하기식(I)의 화합물 또는 그 염을 제조하고, 또는 (3) 하기식(I1) 또는 그 염을 이미노 보호기의 제거반응에 수반시켜 하기식(Im) 또는 그 염을 제조하는 것을 포함하는 하기식(I)의 화합물 또는 그 염을 제조하는 방법.
    상기식에서, R1은 할로겐, 하나 또는 그 이상의 적합한 치환체를 지닌 헤테로 시클릭기, 하나 또는 그 이상의 적합한 치환체를 지닌 아릴,-NH-R5(R5는 할로겐, 저급 알카노일 또는 히드록시(저급)알킬임), -S-R6(R6는 저급알킬, 카르복시 및 아미노로 치환된 저급알킬, 보호된 카르복시 및 보호된 아미노로 치환된 저급알킬 또는 피리딜임), -O-R7(R7은 수소, 히드록시 보호기, 저급 알킬, 저급 알케닐, 아르(저급)알킬, 할로(저급)알킬, 아미노(저급)알킬, 보호된 아미노(저급)알킬 또는 저급 알킬을 지닌 피페라지닐(저급)알킬임), -CONH-R8(R8은 시아노, 카르바모일(저급)알킬, 카르복시(저급)알킬, 보호된 카르복시(저급)알킬, 또는 카르바모일 및 아릴로 치환된 저급 알킬), 또는 -Z-R9(R9는 수소 또는 저급 알킬이고, Z는(R10은 히드록시, 저급 알콕시 또는 아미노)또는(R11은 카르복시 또는 보호된 카르복시이고, R12는 수소이고; 혹은 R11은 할로겐이고, R12는 할로겐임)]이며, R2는 하나 또는 그 이상의 적합한 치환체를 지닌 알릴이며, R3는 수소 또는 할로겐이며, R4는 수소, 할로겐 또는 저급 알콕시이며, A는 저급 알킬렌이며, X는 할로겐이며, R14는 수소 또는 저급 알킬이며, R15는 이미노 보호기이며, J는 CH 또는 N이며, Q는 CH 또는 N임.
  8. 활성 성분으로서의 제 1 항의 화합물 또는 그의 약학적 허용염과, 이와 혼합되는 약학적 허용 담체를 포함하는 약학적 조성물.
  9. 제 1 항의 화합물 또는 그의 약학적 허용염을 콜레시스토키닌 길항질로서 사용하는 방법.
  10. 제 1 항의 화합물 또는 그의 약학적 허용염을 사람 또는 동물에게 투여하는 것을 포함하는 구토 또는 췌장염의 치료 또는 예방방법.
    ※참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890009654A 1988-07-07 1989-07-06 벤조디아제핀 유도체 KR900001688A (ko)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
GB888816207A GB8816207D0 (en) 1988-07-07 1988-07-07 Benzodiazepine derivatives
JP8816207.8 1988-07-07
GB888820560A GB8820560D0 (en) 1988-08-31 1988-08-31 Benzodiazepine derivatives
JP8820560.4 1988-08-31
JP8823660.9 1988-10-07
GB888823660A GB8823660D0 (en) 1988-10-07 1988-10-07 Benzodiazepine derivatives

Publications (1)

Publication Number Publication Date
KR900001688A true KR900001688A (ko) 1990-02-27

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KR1019890009654A KR900001688A (ko) 1988-07-07 1989-07-06 벤조디아제핀 유도체

Country Status (17)

Country Link
US (1) US4970207A (ko)
EP (1) EP0349949B1 (ko)
JP (2) JP2536160B2 (ko)
KR (1) KR900001688A (ko)
CN (1) CN1041941A (ko)
AT (1) ATE147403T1 (ko)
AU (1) AU3785989A (ko)
CA (1) CA1334589C (ko)
DE (1) DE68927620T2 (ko)
DK (1) DK336589A (ko)
ES (1) ES2095833T3 (ko)
FI (1) FI95699C (ko)
GR (1) GR3022239T3 (ko)
HU (1) HUT50331A (ko)
IL (1) IL90830A (ko)
NO (1) NO173014C (ko)
PT (1) PT91092B (ko)

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FI893226A (fi) 1990-01-08
IL90830A0 (en) 1990-01-18
FI95699C (fi) 1996-03-11
US4970207A (en) 1990-11-13
ATE147403T1 (de) 1997-01-15
NO892799L (no) 1990-01-08
JPH07224060A (ja) 1995-08-22
EP0349949B1 (en) 1997-01-08
DE68927620D1 (de) 1997-02-20
IL90830A (en) 1995-06-29
PT91092A (pt) 1990-02-08
FI893226A0 (fi) 1989-07-03
AU3785989A (en) 1990-01-11
DK336589D0 (da) 1989-07-06
DE68927620T2 (de) 1997-04-24
EP0349949A2 (en) 1990-01-10
CN1041941A (zh) 1990-05-09
PT91092B (pt) 1995-05-04
NO173014C (no) 1993-10-13
CA1334589C (en) 1995-02-28
ES2095833T3 (es) 1997-03-01
FI95699B (fi) 1995-11-30
JPH0256481A (ja) 1990-02-26
EP0349949A3 (en) 1991-09-04
JP2536160B2 (ja) 1996-09-18
NO892799D0 (no) 1989-07-06
HUT50331A (en) 1990-01-29
GR3022239T3 (en) 1997-04-30
NO173014B (no) 1993-07-05
DK336589A (da) 1990-01-08

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