KR900002799A - 뉴로펩티드 y 애고니스트 - Google Patents

뉴로펩티드 y 애고니스트 Download PDF

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KR900002799A
KR900002799A KR1019890012042A KR890012042A KR900002799A KR 900002799 A KR900002799 A KR 900002799A KR 1019890012042 A KR1019890012042 A KR 1019890012042A KR 890012042 A KR890012042 A KR 890012042A KR 900002799 A KR900002799 A KR 900002799A
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nlx
trqry
peptide derivative
alrhyx
aoc
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KR1019890012042A
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KR0149160B1 (ko
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레오나드 크르스테난스키 죤
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게리 디.스트리트
메렐 다우 파마슈티칼스 인코포레이티드
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C07K14/57545—Neuropeptide Y
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biophysics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Toxicology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

내용 없음

Description

뉴로펩티드 Y 애고니스트
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (12)

  1. 하기 일반식(1) 내지 (4')의 펩티드 유도체 또는 이의 약제학적으로 허용되는 염.
    Y-P-S-K-P-D-N-P-G-E-D-A-P-A-E-X1-L-X2-R-Y-Y-X3-A-L-R-H-Y-X4-N-L-X5-T-R-X6-R-Y-Tc (1)
    Y-P-S-K-C-D-θ-Y-X3-A-c-R-H-Y-X4-N-L-X5-T-R-Q-R-Y-Tc (2)
    Y-P-S-K-P-D-θ-Y-X3-A-L-R-H-Y-X4-N-L-X5-T-R-Q-R-Y-T-C (2')
    Y-P-S-K-P-D-c-θ-X2-R-C-Y-X3-A-L-R-H-Y-X4-N-L-X5-T-R-Q-R-Y-Tc (3)
    Y-P-S-K-P-D-N-θ-X2-R-Y-Y-X3-A-L-R-H-Y-X4-N-L-X5-T-R-Q-R-Y-Tc (3')
    Y-C-S-K-θ-R-H-c-X4-N-L-X5-T-R-Q-R-Y-Tc (4)
    Y-P-S-K-θ-R-H-Y-X4-N-L-X5-T-R-Q-R-Y-Tc (4')
    상기식에서, X1은 E 또는 D이고 ; X2및 X3는 각각 S 또는 A이며 ; X4및 X5는 각각 L,I,M,Nle 또는 V이고 ; X6은 Q,P,H 또는 I이며 ; Tc는 OR' 또는 NHR'이고 ; R'는 수소 또는 (C1-C4)알킬 그룹이며 ; θ는 일반식 -NH-(CH2)n-CO2-의 그룹이고 ; n은 1 내지 11의 정수이다.
  2. 제 1 항에 있어서, X2가 A인 펩티드 유도체.
  3. 제 1 항에 있어서, X3가 S인 펩티드 유도체.
  4. 제 1 항에 있어서, X4가 I인 펩티드 유도체.
  5. 제 1 항에 있어서, X5가 I인 펩티드 유도체.
  6. 제 1 항에 있어서, X6이 Q인 펩티드 유도체.
  7. 제 1 항에 있어서, θ가 Aoc인 펩티드 유도체.
  8. 제 1 항에 있어서, 하기 일반식의 펩티드 유도체.
    Y-P-S-K-P-D-N-P-G-E-D-A-P-A-E-E-L-S-R-Y-Y-A-A-L-R-H-Y-L-N-L-L-T-R-Q-R-Y-#
    Y-P-S-K-C-D-Aoc-Y-S-A-c-R-H-Y-I-N-L-I-T-R-Q-R-Y-#
    Y-P-S-K-P-D-Aoc-Y-S-A-L-R-H-Y-I-N-L-I-T-R-Q-R-Y-#
    Y-P-S-K-P-D-c-Aoc-A-R-C-Y-S-A-L-R-H-Y-I-N-L-I-T-R-Q-R-Y-#
    Y-P-S-K-P-D-N-Aoc-A-R-C-Y-S-A-L-R-H-Y-I-N-L-I-T-R-Q-R-Y-H
    Y-C-S-K-Aoc-R-H-c-I-N-L-I-T-R-Q-R-Y-#
    Y-P-S-Aoc-R-H-Y-I-N-L-I-T-R-Q-R-Y-#
  9. 뉴로펩티드 Y수용체와 제 1 항 내지 제 8 항중 어느 한항의 펩티드 유도체를 접촉시킴을 특징으로 하여, 뉴로펩티드 Y 수용체를 활성화시키는 방법.
  10. 저혈압 치료가 필요한 환자에게 제 1 항 내지 제 8 항중 어느 한항의 펩티드 유도체 유효량을 투여함을 특징으로 하여, 환자의 저혈압을 치료하는 방법.
  11. 식사 거부성 질환(eating aversion disorder) 치료가 필요한 환자에게 제 1 항 내지 제 8 항중 어느 한 항의 펩티드 유도체 유효량을 투여함을 특징으로 하여, 환자의 식사 거부성 질환을 치료하는 방법.
  12. 적합하게 보호된 티로신을 활성화 수지 지지체에 결합시키고, 계속해서 다른 알파 아미노 보호된, 프롤린 또는 시스테인으로부터의 아미노산을, 이의 아미노 보호그룹을 제거함으로써 노출된 성장 펩티드 쇄의 말단 아미노 그룹에 대한 카복시 말단 티로신에 결합시키고(여기에서, 내부 폐환된 펩티드 유도체는 선형 펩티드의 산화성 커플링의 수행에 바람직하다), 최종적으로 바람직한 펩티드 또는 이의 약제학적으로 허용되는 염을 분리시킴을 특징으로 하여, 하기 일반식(1) 내지 (4')의 펩티드 유도체 또는 이의 약제학적으로 허용되는 염을 제조하는 방법.
    Y-P-S-K-P-D-N-P-G-E-D-A-P-A-E-X1-L-X2-R-Y-Y-X3-A-L-R-H-Y-X4-N-L-X5-T-R-X6-R-Y-Tc (1)
    Y-P-S-K-C-D-θ-Y-X3-A-c-R-H-Y-X4-N-L-X5-T-R-Q-R-Y-Tc (2)
    Y-P-S-K-P-D-θ-Y-X3-A-L-R-H-Y-X4-N-L-X5-T-R-Q-R-Y-Tc (2')
    Y-P-S-K-P-D-c-θ-X2R-C-Y-X3-A-L-R-H-Y-X4-N-L-X5-T-R-Q-R-Y-Tc (3)
    Y-P-S-K-P-D-N-θ-X2-R-Y-Y-X3-A-L-R-H-Y-X4-N-L-X5-T-R-Q-R-Y-Tc (3')
    Y-C-S-K-θ-R-H-c-X4-N-L-X5-T-R-Q-R-Y-Tc (4)
    Y-P-S-K-θ-R-H-Y-X4-N-L-X5-T-R-Q-R-Y-Tc (4')
    상기식에서, X1,X2,X3,X4,X5,X6,Tc, 및 θ는 제 1 항에서 정의한 바와같다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890012042A 1988-08-26 1989-08-24 뉴로펩티드 y효능제 KR0149160B1 (ko)

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US23759188A 1988-08-26 1988-08-26
US237,591 1988-08-26

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KR0149160B1 KR0149160B1 (ko) 1998-10-15

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EP (1) EP0355793B1 (ko)
JP (1) JP2791955B2 (ko)
KR (1) KR0149160B1 (ko)
CN (1) CN1042155A (ko)
AT (1) ATE140235T1 (ko)
AU (1) AU618118B2 (ko)
CA (1) CA1341336C (ko)
DE (1) DE68926804T2 (ko)
DK (1) DK420789A (ko)
ES (1) ES2091757T3 (ko)
FI (1) FI894006A (ko)
HU (1) HU204852B (ko)
IL (1) IL91395A0 (ko)
NO (1) NO893430L (ko)
NZ (1) NZ230384A (ko)
PT (1) PT91538B (ko)
ZA (1) ZA896376B (ko)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
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JP3419454B2 (ja) * 1991-11-06 2003-06-23 ガーヴァン インスティチュート オブ メディカル リサーチ ヒト神経ペプチドｙ−ｙ１レセプター
AU662032B2 (en) * 1991-12-19 1995-08-17 Garvan Institute Of Medical Research A novel molecule which inhibits neuropeptide tyrosine biological function
JPH08501055A (ja) * 1991-12-19 1996-02-06 ガーヴァン インスティチュート オブ メディカル リサーチ 神経ペプチドチロシンの生物学的機能を抑制する新規な分子
GB9213215D0 (en) * 1992-06-20 1992-08-05 Wellcome Found Peptides
JPH11501281A (ja) * 1993-06-18 1999-02-02 ユニバーシティ オブ シンシナティ 神経ペプチドｙアンタゴニスト及びアゴニスト
US5516653A (en) * 1993-12-28 1996-05-14 Synaptic Pharmaceutical Corporation DNA encoding a human neuropeptide Y/peptide YY/pancreatic polypeptide receptor (Y4) and uses thereof
US5545549A (en) 1994-02-03 1996-08-13 Synaptic Pharmaceutical Corporation DNA encoding a human neuropeptide Y/peptide YY (Y2) receptor and uses thereof
US5989920A (en) 1994-12-02 1999-11-23 Synaptic Pharmaceutical Corporation Methods of modifying feeding behavior compounds useful in such methods and DNA encoding a hypothalmic atypical neuropeptide Y/peptide YY receptor Y5
US5602024A (en) 1994-12-02 1997-02-11 Synaptic Pharmaceutical Corporation DNA encoding a hypothalamic atypical neuropeptide Y/peptide YY receptor (Y5) and uses thereof
AUPN646795A0 (en) 1995-11-09 1995-11-30 Garvan Institute Of Medical Research Neuropeptide Y-Y5 receptor
DE19652033A1 (de) * 1996-12-13 1998-06-18 Irmgard Dr Med Guertner Neuropeptid (CGRP) als Modulator zur Zelldifferenzierung und Proliferation
US6713265B1 (en) 1997-06-04 2004-03-30 Synaptic Pharmaceutical Corporation Methods of modifying feeding behavior, compounds useful in such methods, and DNA encoding a hypothalamic atypical neuropeptide Y/peptide YY receptor (Y5)
EP1620091B1 (en) 2003-05-05 2010-03-31 Probiodrug AG Inhibitors of glutaminyl cyclase
NZ546887A (en) 2003-11-03 2009-04-30 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
JP4996926B2 (ja) 2004-02-05 2012-08-08 プロビオドルグ エージー グルタミニルシクラーゼの新規の阻害剤
WO2008055945A1 (en) 2006-11-09 2008-05-15 Probiodrug Ag 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
US9126987B2 (en) 2006-11-30 2015-09-08 Probiodrug Ag Inhibitors of glutaminyl cyclase
CA2679446C (en) 2007-03-01 2016-05-17 Probiodrug Ag New use of glutaminyl cyclase inhibitors
DK2142514T3 (da) 2007-04-18 2015-03-23 Probiodrug Ag Thioureaderivater som glutaminylcyclase-inhibitorer
WO2011029920A1 (en) 2009-09-11 2011-03-17 Probiodrug Ag Heterocylcic derivatives as inhibitors of glutaminyl cyclase
JP6026284B2 (ja) 2010-03-03 2016-11-16 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤
BR112012022478B1 (pt) 2010-03-10 2021-09-21 Probiodrug Ag Inibidores heterocíclicos de glutaminil ciclase (qc, ec 2.3.2.5), seu processo de preparação, e composição farmacêutica
EP2560953B1 (en) 2010-04-21 2016-01-06 Probiodrug AG Inhibitors of glutaminyl cyclase
EP2686313B1 (en) 2011-03-16 2016-02-03 Probiodrug AG Benzimidazole derivatives as inhibitors of glutaminyl cyclase
EP3461819B1 (en) 2017-09-29 2020-05-27 Probiodrug AG Inhibitors of glutaminyl cyclase
CN111494606B (zh) * 2020-04-24 2021-12-14 广州医科大学 神经肽y的新应用

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3811193A1 (de) * 1988-04-01 1989-10-19 Boehringer Ingelheim Kg Neue peptide, verfahren zu ihrer herstellung und diese peptide enthaltende pharmazeutische zusammensetzungen

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NO893430D0 (no) 1989-08-25
EP0355793B1 (en) 1996-07-10
HUT50849A (en) 1990-03-28
JPH02111794A (ja) 1990-04-24
DE68926804T2 (de) 1996-12-12
CN1042155A (zh) 1990-05-16
IL91395A0 (en) 1990-04-29
AU618118B2 (en) 1991-12-12
NZ230384A (en) 1996-03-26
PT91538A (pt) 1990-03-08
FI894006A0 (fi) 1989-08-25
AU4082889A (en) 1990-03-01
DK420789A (da) 1990-02-27
ES2091757T3 (es) 1996-11-16
EP0355793A3 (en) 1992-04-22
DE68926804D1 (de) 1996-08-14
HU204852B (en) 1992-02-28
KR0149160B1 (ko) 1998-10-15
ZA896376B (en) 1990-05-30
ATE140235T1 (de) 1996-07-15
EP0355793A2 (en) 1990-02-28
CA1341336C (en) 2002-01-29
NO893430L (no) 1990-02-27
PT91538B (pt) 1995-05-04
DK420789D0 (da) 1989-08-25
FI894006A (fi) 1990-02-27
JP2791955B2 (ja) 1998-08-27

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