KR960702476A - Lhrh 길항제(lhrh antagonists) - Google Patents

Lhrh 길항제(lhrh antagonists)

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Publication number
KR960702476A
KR960702476A KR1019950705129A KR19950705129A KR960702476A KR 960702476 A KR960702476 A KR 960702476A KR 1019950705129 A KR1019950705129 A KR 1019950705129A KR 19950705129 A KR19950705129 A KR 19950705129A KR 960702476 A KR960702476 A KR 960702476A
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KR
South Korea
Prior art keywords
lys
antid
complex
carrier
lhrh antagonist
Prior art date
Application number
KR1019950705129A
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English (en)
Inventor
죤 러셀-죤스 그레고리
Original Assignee
로잘린드 앤 칼도르
바이오텍크 오스트레일리아 피티와이 리미티드
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Application filed by 로잘린드 앤 칼도르, 바이오텍크 오스트레일리아 피티와이 리미티드 filed Critical 로잘린드 앤 칼도르
Publication of KR960702476A publication Critical patent/KR960702476A/ko

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/23Luteinising hormone-releasing hormone [LHRH]; Related peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/24Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
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  • Oil, Petroleum & Natural Gas (AREA)
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

본 발명은 신규한 LHRH 길항제 및 이들 길항제와 VB12 간의 복합체를 제공한다. 본 발명은 특히 LHRH길항제의 경구투여에 유용하다. 본 발명의 길항제는 안티드-1, 안티드-2 및 안티드-3으로 이루어진 군으로부터 선택된다.

Description

LHRH 길항제(LHRH ANTAGONISTS)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 랫트의 뇌하수체 세포로부터의 안티드(ANTIDE), 1H의 LHRH-자극방츨의 억제를 알아보기 위한 생체밖 생물검정에 의해 결정된 중간 억제농도(IC50)를 보여주는 그래프이다.
제2도는 랫트의 뇌하수체 세포로부터의 안티드, 안티드-3 및 이것의 VB12-컨쥬게이트에 의한 1H의 LHRH-자극 방출의 억제를 알아보기 의한 생체밖 생을 검정을 보여주는 그래프이다.

Claims (9)

  1. N-Ac-D-Nal(2), D-Phe(pCl), D-Pal(3), Ser, Lys(Nic), D-Lys, Leu, Lys(iPr), Pro, D-Ala-NH2(D-Lys6안티드 또는 안티드-1); N-Ac-D-Nal(2), D-Phe(pCl), D-Pal(3), Ser, Lys, D-Lys(Nic), Leu, Lys(Tr), Pro, D-Ala-NH2(Lys5안티드 또는 안티드-2) 및 N-Ac-D-Nal(2), D-Phe(pCl), D-Pal(3), Ser, Lys(Nic), D-Lys(Nic), Leu, Lys, Pro, D-Ala-NH2(Lys8안티드 또는 안티드-3)로 이루어진 군으로부터 선택되는 LHRH 길항제.
  2. 환자의 화학적 난소제거 및/또는 고나도트로핀 의존적 장애의 치료에서의 이용을 위한 복합체에 있어서, 복합체는 결합제기를 통하여 비타민 B12나 이것의 유사체인 담체에 결합된 LHRH 길항제로 이루어지고 결합제기는 LHRH 길항제가 생체내에서 담체로부터 절단되는 것을 특징으로 하는 복합체.
  3. 제2항에 있어서, LHRH 길항제는 안티드-1, 안티드-2 및 안티드-3으로 이루어지는 군으로부터 선택되는 것을 특징으로 하는 복합체.
  4. 제3항에 있어서, LHRH 길항제는 안티드-3인 것을 특징으로 하는 복합체.
  5. 제2항 내지 제4항 중 어느 한 항에 있어서, 하나 이상의 LHRH 길항제가 담체에 결합되어 있는 것을 특징으로 하는 복합체.
  6. 제2항 내지 제5항 중 어느 한 항에 있어서, 담체는 시아노코발아민, 아쿠오코발아민, 아데노실코발아민, 메틸코발아민, 히드록시코발아민, 시아노코발아민, 카바날리드, 5-o-메틸 벤질코발아민, 상기한 모두의 데스디메틸, 모노에틸아미드 및 메틸아미드 유사체, 코발아미드, 조효소 B12, 5'-디옥시아데노실코발아민, 클로로코발아민, 술피토코발아민, 니트로코발아민, 티오시아나토코발아민, 벤즈이미다졸유도체, 아데노실시아노코발아민, 코발아민 락톤, 코발아민 락탐 및 아닐리드의 유사체와 동족체, 비타민 B12나 이것의 유사체의 에틸아미드, 프로피온아미드, 모노카르복실산 및 디카르복실산 유도체로 이루어진 군으로부터 선택되는 것을 특징으로 하는 복합체.
  7. 제2항 내지 제6항 중 어느 한 항에 있어서, LHRH 길항제는 티올-절단할 수 있는 교차-결합제를 통해 당체에 결합되는 것을 특징으로 하는 복합체.
  8. 제6항에 있어서, LHRH 길항제는 이황화 결합에 의해 담체에 결합되는 것을 특징으로 하는 복합체.
  9. 환자의 화학적 난소제거 및/또는 고나도트로핀 의존적 장애의 치료방법에 있어서, 환자에게 제2항 내지 제8항 중 어느 한 항에 따른 복합체의 유효량을 투여하는 것으로 이루어진 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950705129A 1993-05-20 1994-05-20 Lhrh 길항제(lhrh antagonists) KR960702476A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
AUPL888093 1993-05-20
AUPL8880 1993-05-20
PCT/AU1994/000262 WO1994028015A1 (en) 1993-05-20 1994-05-20 Lhrh antagonists

Publications (1)

Publication Number Publication Date
KR960702476A true KR960702476A (ko) 1996-04-27

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ID=3776905

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019950705129A KR960702476A (ko) 1993-05-20 1994-05-20 Lhrh 길항제(lhrh antagonists)

Country Status (8)

Country Link
US (1) US5863900A (ko)
EP (1) EP0698040A4 (ko)
JP (1) JPH08510260A (ko)
KR (1) KR960702476A (ko)
CA (1) CA2163225A1 (ko)
RU (1) RU2130464C1 (ko)
SG (1) SG50426A1 (ko)
WO (1) WO1994028015A1 (ko)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5574018A (en) * 1994-07-29 1996-11-12 Amgen Inc. Conjugates of vitamin B12 and proteins
US5843901A (en) * 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
EP1007533B1 (en) 1996-08-27 2005-06-22 University Of Utah Research Foundation Bioconjugates and delivery of bioactive agents
AUPP405098A0 (en) * 1998-06-12 1998-07-02 Access Pharmaceuticals Australia Pty Limited Novel methods of preparation of vitamin b12 derivatives suitable for conjugation to pharmaceuticals
FR2822834B1 (fr) * 2001-04-02 2005-02-25 Flamel Tech Sa Suspension colloidale de nanoparticules a base de copolymeres amphiphile pour la vectorisation de principes actifs et leur mode de preparation
FR2843117B1 (fr) * 2002-07-30 2004-10-15 Flamel Tech Sa Polyaminoacides fonctionnalises par au moins un groupement hydrophobe et leurs applications notamment therapeutiques
GB0307777D0 (en) 2003-04-04 2003-05-07 Medical Res Council Conjugate compounds
FR2855521B1 (fr) * 2003-05-28 2005-08-05 Flamel Tech Sa Polyaminoacides fonctionnalises par au moins un groupement h ydrophobe et leurs applications notamment therapeutiques.
US7232805B2 (en) * 2003-09-10 2007-06-19 Inflabloc Pharmaceuticals, Inc. Cobalamin conjugates for anti-tumor therapy
FR2860516B1 (fr) * 2003-10-03 2006-01-13 Flamel Tech Sa Homopolyaminoacides telecheliques fonctionnalises par des groupements hydrophobes et leurs applications notamment therapeutiques
FR2862536B1 (fr) * 2003-11-21 2007-11-23 Flamel Tech Sa Formulations pharmaceutiques pour la liberation prolongee de principe(s) actif(s), ainsi que leurs applications notamment therapeutiques
WO2008115805A2 (en) * 2007-03-19 2008-09-25 Inflabloc Pharmaceuticals, Inc. Cobalamin taxane bioconjugates
WO2011130716A2 (en) 2010-04-16 2011-10-20 Access Pharmaceuticals, Inc. A nanostructures containing vitamin b12 for facilitated delivery of drugs across biological barriers
KR20140026396A (ko) 2011-03-08 2014-03-05 어섹스 팔마큐티칼스 인코포레이티드 생물학적 막을 가로질러 활성물질의 전달을 위한 표적화된 나노담체 시스템

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU587658B2 (en) * 1985-10-10 1989-08-24 Access Pharmaceuticals Australia Pty Limited Oral delivery of biologically active substances bound to vitamin b12, or analogues thereof
NZ217821A (en) * 1985-10-10 1989-07-27 Biotech Australia Pty Ltd Oral delivery system; complex of active agent and vitamin b12 or analogue thereof
US4935491A (en) * 1987-08-24 1990-06-19 Board Of Regents, The University Of Texas System Effective antagonists of the luteinizing hormone releasing hormone which release negligible histamine
DK163689A (da) * 1988-04-08 1989-10-30 Sandoz Ag Peptidderivater
US5169935A (en) * 1990-06-20 1992-12-08 The Salk Institute For Biological Studies Method of making peptides

Also Published As

Publication number Publication date
JPH08510260A (ja) 1996-10-29
RU2130464C1 (ru) 1999-05-20
US5863900A (en) 1999-01-26
SG50426A1 (en) 1998-07-20
EP0698040A1 (en) 1996-02-28
CA2163225A1 (en) 1994-12-08
EP0698040A4 (en) 1999-01-07
WO1994028015A1 (en) 1994-12-08

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