KR100519421B1 - 5 및 6 위치에서 변형되는 지엔알에이치 길항제 - Google Patents

5 및 6 위치에서 변형되는 지엔알에이치 길항제 Download PDF

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Publication number
KR100519421B1
KR100519421B1 KR10-1999-7009315A KR19997009315A KR100519421B1 KR 100519421 B1 KR100519421 B1 KR 100519421B1 KR 19997009315 A KR19997009315 A KR 19997009315A KR 100519421 B1 KR100519421 B1 KR 100519421B1
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KR
South Korea
Prior art keywords
xaa
4aph
ala
peptide
hor
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Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
KR10-1999-7009315A
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English (en)
Korean (ko)
Other versions
KR20010006233A (ko
Inventor
그레임 셈플
구앙쳉 지앙
진 이.에프. 리바이어
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페링 비.브이
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=25273352&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=KR100519421(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 페링 비.브이 filed Critical 페링 비.브이
Publication of KR20010006233A publication Critical patent/KR20010006233A/ko
Application granted granted Critical
Publication of KR100519421B1 publication Critical patent/KR100519421B1/ko
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/23—Luteinising hormone-releasing hormone [LHRH]; Related peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • A61K38/09—Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • 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
    • 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
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S930/00—Peptide or protein sequence
    • Y10S930/01—Peptide or protein sequence
    • Y10S930/11—Gonadotropin; related peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Endocrinology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Reproductive Health (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Diabetes (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
KR10-1999-7009315A 1997-04-11 1998-04-13 5 및 6 위치에서 변형되는 지엔알에이치 길항제 Expired - Fee Related KR100519421B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US08/837,042 US5925730A (en) 1997-04-11 1997-04-11 GnRH antagonists
US08/837,042 1997-04-11
PCT/US1998/007438 WO1998046634A1 (en) 1997-04-11 1998-04-13 GnRH ANTAGONISTS BEING MODIFIED IN POSITIONS 5 AND 6

Publications (2)

Publication Number Publication Date
KR20010006233A KR20010006233A (ko) 2001-01-26
KR100519421B1 true KR100519421B1 (ko) 2005-10-06

Family

ID=25273352

Family Applications (1)

Application Number Title Priority Date Filing Date
KR10-1999-7009315A Expired - Fee Related KR100519421B1 (ko) 1997-04-11 1998-04-13 5 및 6 위치에서 변형되는 지엔알에이치 길항제

Country Status (36)

Country Link
US (2) US5925730A (https=)
EP (1) EP1003774B1 (https=)
JP (2) JP4249806B2 (https=)
KR (1) KR100519421B1 (https=)
CN (1) CN1230442C (https=)
AR (1) AR011217A1 (https=)
AT (1) ATE319736T1 (https=)
AU (1) AU728642B2 (https=)
BR (1) BR9808523B1 (https=)
CA (1) CA2286190C (https=)
CY (2) CY1108063T1 (https=)
CZ (1) CZ299097B6 (https=)
DE (2) DE69833751T2 (https=)
DK (1) DK1003774T3 (https=)
EE (1) EE03974B1 (https=)
ES (1) ES2260833T3 (https=)
FR (1) FR09C0028I2 (https=)
HR (1) HRP980197B1 (https=)
HU (1) HU224836B1 (https=)
IL (1) IL132303A0 (https=)
LU (1) LU91585I2 (https=)
MY (1) MY114811A (https=)
NL (1) NL300395I2 (https=)
NO (2) NO324991B1 (https=)
NZ (1) NZ500142A (https=)
PL (1) PL194509B1 (https=)
PT (1) PT1003774E (https=)
RU (1) RU2199549C2 (https=)
SI (1) SI1003774T1 (https=)
SK (1) SK285381B6 (https=)
TR (1) TR199902956T2 (https=)
TW (1) TW505658B (https=)
UA (1) UA58547C2 (https=)
UY (1) UY24958A1 (https=)
WO (1) WO1998046634A1 (https=)
ZA (1) ZA983062B (https=)

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US6828415B2 (en) * 1993-02-19 2004-12-07 Zentaris Gmbh Oligopeptide lyophilisate, their preparation and use
US5925730A (en) * 1997-04-11 1999-07-20 Ferring Bv GnRH antagonists
WO1999026964A1 (en) * 1997-11-20 1999-06-03 Ortho-Mcneil Pharmaceutical, Inc. LIQUID PHASE PROCESS FOR THE PREPARATION OF GnRH PEPTIDES
US8119159B2 (en) * 1999-02-22 2012-02-21 Merrion Research Iii Limited Solid oral dosage form containing an enhancer
US20070148228A1 (en) * 1999-02-22 2007-06-28 Merrion Research I Limited Solid oral dosage form containing an enhancer
US7658938B2 (en) * 1999-02-22 2010-02-09 Merrion Reasearch III Limited Solid oral dosage form containing an enhancer
GB0117057D0 (en) * 2001-07-12 2001-09-05 Ferring Bv Pharmaceutical composition
IL147138A0 (en) * 2001-12-17 2002-08-14 Yeda Res & Dev Methods of and pharmaceutical compositions for modulating cell adhesion, migration and extravasation
EP2322196A2 (en) 2003-11-10 2011-05-18 Reprise Biopharmaceutics, LLC Pharmaceutical compositions including low dosages of desmopressin
DE20321887U1 (de) 2003-11-10 2012-01-20 Allergan, Inc. Arzneimittel umfassend niedrige Dosierungen von Desmopressin
CN101037472B (zh) * 2006-03-14 2013-03-27 中国人民解放军军事医学科学院毒物药物研究所 具有低组胺释放作用的促黄体生成素释放激素拮抗剂
KR101191322B1 (ko) * 2006-04-07 2012-10-16 메리온 리서치 Ⅲ 리미티드 증진제를 함유하는 고형 경구용 투여 제형
TWI442932B (zh) * 2008-02-11 2014-07-01 Ferring Int Ct Sa 以ＧｎＲＨ拮抗劑治療攝護腺癌的方法
CN107096012A (zh) * 2008-05-07 2017-08-29 诺和诺德股份有限公司 肽的组合物及其制备方法
US20100215743A1 (en) * 2009-02-25 2010-08-26 Leonard Thomas W Composition and drug delivery of bisphosphonates
KR101621725B1 (ko) 2009-04-24 2016-05-17 폴리펩타이드 라보라토리즈 에이/에스 데가렐릭스의 제조 방법
EP2424503B1 (en) * 2009-05-01 2017-07-05 Ferring BV Composition for the treatment of prostate cancer
TW201043221A (en) * 2009-05-06 2010-12-16 Ferring Int Ct Sa Kit and method for preparation of a Degarelix solution
US20110039787A1 (en) 2009-07-06 2011-02-17 Ferring International Center S.A. Compositions, kits and methods for treating benign prostate hyperplasia
WO2011066386A1 (en) 2009-11-25 2011-06-03 Novetide, Ltd. Process for production of degarelix
US20110182985A1 (en) * 2010-01-28 2011-07-28 Coughlan David C Solid Pharmaceutical Composition with Enhancers and Methods of Preparing thereof
WO2011120033A1 (en) * 2010-03-26 2011-09-29 Merrion Research Iii Limited Pharmaceutical compositions of selective factor xa inhibitors for oral administration
EP2447276A1 (en) 2010-10-27 2012-05-02 Ferring B.V. Process for the manufacture of Degarelix and its intermediates
PT2632934T (pt) 2010-10-27 2017-01-06 Ferring Bv Processo para o fabrico de degarelix e seus intermediários
EP2654772B1 (en) 2010-12-22 2018-09-26 The Salk Institute for Biological Studies Cyclic crf antagonist peptides
EP2661273A4 (en) 2011-01-07 2014-06-04 Merrion Res Iii Ltd IRON PHARMACEUTICAL COMPOSITIONS FOR ORAL ADMINISTRATION
JO3755B1 (ar) 2011-01-26 2021-01-31 Ferring Bv تركيبات تستوستيرون
WO2013104745A1 (en) 2012-01-13 2013-07-18 Ferring Bv Pharmaceutical composition
SG11201407679PA (en) 2012-06-01 2014-12-30 Ferring Bv Manufacture of degarelix
US10265384B2 (en) 2015-01-29 2019-04-23 Novo Nordisk A/S Tablets comprising GLP-1 agonist and enteric coating
WO2017103275A1 (en) * 2015-12-17 2017-06-22 Fresenius Kabi Anti-Infectives S.R.L Process for the manufacture of degarelix and its intermediates
CN107778355B (zh) * 2016-08-25 2021-04-20 成都圣诺生物制药有限公司 一种合成西曲瑞克的方法
WO2019110688A1 (en) 2017-12-05 2019-06-13 Ferring B.V. A composition comprising degarelix for use in the treatment of breast cancer
EP4004001B1 (en) 2019-07-29 2025-09-03 Sunshine Lake Pharma Co., Ltd. Substituted pyrimidinedione compounds and uses thereof
US11332495B2 (en) 2019-09-21 2022-05-17 RK Pharma Solutions LLC Process for the preparation of Degarelix acetate and Degarelix acetate-mannitol premix
CN114456236A (zh) * 2020-11-09 2022-05-10 深圳市健翔生物制药有限公司 一种地加瑞克乙酰化杂质的制备方法
WO2023072284A1 (zh) 2021-11-01 2023-05-04 山东绿叶制药有限公司 促性腺素释放激素拮抗剂及其制备方法和应用
WO2026068660A1 (en) 2024-09-26 2026-04-02 Ferring B.V. Lipidated gonadotropin releasing hormone analogues

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996040757A2 (en) * 1995-06-07 1996-12-19 Indiana University Foundation Lhrh antagonist peptides

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US4547370A (en) * 1983-11-29 1985-10-15 The Salk Institute For Biological Studies GnRH Antagonists
US4508921A (en) * 1984-06-28 1985-04-02 Merck & Co., Inc. Process for preparation of alpha-alkyl amino acids
US5073624A (en) * 1985-04-09 1991-12-17 Administrators Of The Tulane Educational Fund Therapeutic decapeptides
US4866160A (en) * 1985-04-09 1989-09-12 The Administrators Of The Tulane Educational Fund Therapeutic decapeptides
US4800191A (en) * 1987-07-17 1989-01-24 Schally Andrew Victor LHRH antagonists
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
US5171835A (en) * 1988-10-21 1992-12-15 The Administrators Of The Tulane Educational Fund LHRH antagonists
US5296468A (en) * 1989-10-30 1994-03-22 The Salk Institute For Biological Studies GnRH analogs
DE69214818T2 (de) * 1991-04-25 1997-02-27 Romano S.-Cergue Deghenghi LHRH-Antagonisten
ATE206136T1 (de) * 1992-12-18 2001-10-15 Abbott Lab Lhrh antagonisten mit modifizierten aminoacylresten an den positionen 5 und 6
IL108509A0 (en) * 1993-02-22 1994-05-30 Salk Inst For Biological Studi GnRH antagonist peptides
RU2084458C1 (ru) * 1993-05-27 1997-07-20 Институт высокомолекулярных соединений РАН Декапептид, обладающий противоопухолевой активностью
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WO1996040757A2 (en) * 1995-06-07 1996-12-19 Indiana University Foundation Lhrh antagonist peptides

Also Published As

Publication number Publication date
WO1998046634A1 (en) 1998-10-22
JP3645255B1 (ja) 2005-05-11
TR199902956T2 (xx) 2000-08-21
FR09C0028I1 (https=) 2009-09-25
ES2260833T3 (es) 2006-11-01
DE69833751T2 (de) 2006-11-09
CZ358699A3 (cs) 2000-06-14
EE03974B1 (et) 2003-02-17
PL336213A1 (en) 2000-06-05
BR9808523B1 (pt) 2010-02-09
IL132303A0 (en) 2001-03-19
BR9808523A (pt) 2000-05-23
CN1230442C (zh) 2005-12-07
MY114811A (en) 2003-01-31
HUP0002704A3 (en) 2003-08-28
TW505658B (en) 2002-10-11
AR011217A1 (es) 2000-08-02
UA58547C2 (uk) 2003-08-15
CN1259959A (zh) 2000-07-12
PT1003774E (pt) 2006-05-31
UY24958A1 (es) 2001-03-16
JP2001523229A (ja) 2001-11-20
CY1108063T1 (el) 2012-01-25
CZ299097B6 (cs) 2008-04-23
JP2005120101A (ja) 2005-05-12
EP1003774A1 (en) 2000-05-31
EP1003774B1 (en) 2006-03-08
AU6969898A (en) 1998-11-11
HUP0002704A2 (hu) 2000-12-28
NO324991B1 (no) 2008-01-14
DE69833751D1 (de) 2006-05-04
ZA983062B (en) 1998-10-20
JP4249806B2 (ja) 2009-04-08
AU728642B2 (en) 2001-01-11
NO994906D0 (no) 1999-10-08
HRP980197A2 (en) 1999-02-28
CA2286190A1 (en) 1998-10-22
DE122009000033I2 (de) 2011-07-21
CY2009008I2 (el) 2012-01-25
SI1003774T1 (sl) 2006-08-31
NL300395I2 (nl) 2010-01-04
NO2009016I1 (no) 2009-08-10
KR20010006233A (ko) 2001-01-26
HRP980197B1 (en) 2002-08-31
US6214798B1 (en) 2001-04-10
EE9900479A (et) 2000-06-15
RU2199549C2 (ru) 2003-02-27
DK1003774T3 (da) 2006-07-03
HU224836B1 (en) 2006-03-28
SK285381B6 (sk) 2006-12-07
LU91585I2 (fr) 2009-09-17
US5925730A (en) 1999-07-20
NO2009016I2 (no) 2014-08-25
CY2009008I1 (el) 2012-01-25
NO994906L (no) 1999-12-13
SK139699A3 (en) 2000-11-07
NL300395I1 (nl) 2009-09-01
PL194509B1 (pl) 2007-06-29
NZ500142A (en) 2001-10-26
ATE319736T1 (de) 2006-03-15
CA2286190C (en) 2007-01-09
HK1025104A1 (en) 2000-11-03
DE122009000033I1 (de) 2009-09-17
FR09C0028I2 (fr) 2010-06-11

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