CA2286190C - Gnrh antagonists being modified in positions 5 and 6 - Google Patents

Gnrh antagonists being modified in positions 5 and 6 Download PDF

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Publication number
CA2286190C
CA2286190C CA002286190A CA2286190A CA2286190C CA 2286190 C CA2286190 C CA 2286190C CA 002286190 A CA002286190 A CA 002286190A CA 2286190 A CA2286190 A CA 2286190A CA 2286190 C CA2286190 C CA 2286190C
Authority
CA
Canada
Prior art keywords
4aph
ala
hor
peptide
xaa6
Prior art date
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 - Lifetime
Application number
CA002286190A
Other languages
English (en)
French (fr)
Other versions
CA2286190A1 (en
Inventor
Graeme Semple
Guangcheng Jiang
Jean E. F. Rivier
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Ferring BV
Original Assignee
Ferring BV
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
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=CA2286190(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Ferring BV filed Critical Ferring BV
Publication of CA2286190A1 publication Critical patent/CA2286190A1/en
Application granted granted Critical
Publication of CA2286190C publication Critical patent/CA2286190C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

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

Landscapes

  • 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)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Reproductive Health (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Diabetes (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gynecology & Obstetrics (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)
CA002286190A 1997-04-11 1998-04-13 Gnrh antagonists being modified in positions 5 and 6 Expired - Lifetime CA2286190C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US08/837,042 US5925730A (en) 1997-04-11 1997-04-11 GnRH antagonists
US837,042 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
CA2286190A1 CA2286190A1 (en) 1998-10-22
CA2286190C true CA2286190C (en) 2007-01-09

Family

ID=25273352

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002286190A Expired - Lifetime CA2286190C (en) 1997-04-11 1998-04-13 Gnrh antagonists being modified in positions 5 and 6

Country Status (36)

Country Link
US (2) US5925730A (enExample)
EP (1) EP1003774B1 (enExample)
JP (2) JP4249806B2 (enExample)
KR (1) KR100519421B1 (enExample)
CN (1) CN1230442C (enExample)
AR (1) AR011217A1 (enExample)
AT (1) ATE319736T1 (enExample)
AU (1) AU728642B2 (enExample)
BR (1) BR9808523B1 (enExample)
CA (1) CA2286190C (enExample)
CY (2) CY1108063T1 (enExample)
CZ (1) CZ299097B6 (enExample)
DE (2) DE122009000033I2 (enExample)
DK (1) DK1003774T3 (enExample)
EE (1) EE03974B1 (enExample)
ES (1) ES2260833T3 (enExample)
FR (1) FR09C0028I2 (enExample)
HR (1) HRP980197B1 (enExample)
HU (1) HU224836B1 (enExample)
IL (1) IL132303A0 (enExample)
LU (1) LU91585I2 (enExample)
MY (1) MY114811A (enExample)
NL (1) NL300395I2 (enExample)
NO (2) NO324991B1 (enExample)
NZ (1) NZ500142A (enExample)
PL (1) PL194509B1 (enExample)
PT (1) PT1003774E (enExample)
RU (1) RU2199549C2 (enExample)
SI (1) SI1003774T1 (enExample)
SK (1) SK285381B6 (enExample)
TR (1) TR199902956T2 (enExample)
TW (1) TW505658B (enExample)
UA (1) UA58547C2 (enExample)
UY (1) UY24958A1 (enExample)
WO (1) WO1998046634A1 (enExample)
ZA (1) ZA983062B (enExample)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US5977302A (en) * 1997-11-20 1999-11-02 Ortho-Mcneil Pharmaceutical, Inc. Liquid phase process for the preparation of GnRH peptides
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
US8119159B2 (en) * 1999-02-22 2012-02-21 Merrion Research 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
DE20321887U1 (de) 2003-11-10 2012-01-20 Allergan, Inc. Arzneimittel umfassend niedrige Dosierungen von Desmopressin
WO2005046707A1 (en) 2003-11-10 2005-05-26 Fein Seymour H Pharmaceutical compositions including low dosages of 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
BRPI0710503A2 (pt) * 2006-04-07 2011-08-16 Merrion Res Iii Ltd uso de uma composição farmacêutica, composição farmacêutica, e, forma de dosagem oral
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
US20090280169A1 (en) * 2008-05-07 2009-11-12 Merrion Research Iii Limited Compositions of peptides and processes of preparation thereof
TWI480286B (zh) * 2009-02-25 2015-04-11 Merrion Res Iii Ltd 雙膦酸鹽類組合物及藥物遞送
EP2421887B1 (en) * 2009-04-24 2015-04-22 Polypeptide Laboratories A/S Method for the manufacture of degarelix
KR101795643B1 (ko) * 2009-05-01 2017-11-09 훼링 비.브이. 전립선암 치료용 조성물
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
US9089484B2 (en) * 2010-03-26 2015-07-28 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
WO2012055903A1 (en) 2010-10-27 2012-05-03 Ferring B.V. Process for the manufacture of degarelix and its intermediates
CA2822442C (en) 2010-12-22 2021-03-16 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
KR102140982B1 (ko) 2012-06-01 2020-08-05 훼링 비.브이. 데가렐릭스의 제조 방법
JP7211704B2 (ja) 2015-01-29 2023-01-24 ノヴォ ノルディスク アー/エス Glp-1アゴニスト及び腸溶コーティングを含む錠剤
ES2885869T3 (es) * 2015-12-17 2021-12-15 Fresenius Kabi Ipsum S R L Procedimiento para la fabricación de degarelix y sus productos intermedios
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
WO2021018105A1 (en) 2019-07-29 2021-02-04 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
EP4656241A2 (en) 2021-11-01 2025-12-03 Shandong Luye Pharmaceutical Co., Ltd. Gonadotropin-releasing hormone antagonist, and preparation method therefor and use thereof
WO2026068660A1 (en) 2024-09-26 2026-04-02 Ferring B.V. Lipidated gonadotropin releasing hormone analogues

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US4866160A (en) * 1985-04-09 1989-09-12 The Administrators Of The Tulane Educational Fund Therapeutic decapeptides
US5073624A (en) * 1985-04-09 1991-12-17 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
ATE144538T1 (de) * 1991-04-25 1996-11-15 Romano Deghenghi Lhrh-antagonisten
CA2136079A1 (en) * 1992-12-18 1994-07-07 Fortuna Haviv Lhrh antagonists having modified aminoacyl residues at positions 5 and 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
US5506207A (en) * 1994-03-18 1996-04-09 The Salk Institute For Biological Studies GNRH antagonists XIII
US5843901A (en) * 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
US5925730A (en) * 1997-04-11 1999-07-20 Ferring Bv GnRH antagonists

Also Published As

Publication number Publication date
EP1003774B1 (en) 2006-03-08
BR9808523A (pt) 2000-05-23
CY2009008I2 (el) 2012-01-25
NO324991B1 (no) 2008-01-14
HRP980197A2 (en) 1999-02-28
WO1998046634A1 (en) 1998-10-22
SK285381B6 (sk) 2006-12-07
HUP0002704A3 (en) 2003-08-28
JP2005120101A (ja) 2005-05-12
AU728642B2 (en) 2001-01-11
NO994906L (no) 1999-12-13
NL300395I1 (nl) 2009-09-01
NL300395I2 (nl) 2010-01-04
KR20010006233A (ko) 2001-01-26
CZ358699A3 (cs) 2000-06-14
EE9900479A (et) 2000-06-15
JP4249806B2 (ja) 2009-04-08
AU6969898A (en) 1998-11-11
JP3645255B1 (ja) 2005-05-11
DE69833751D1 (de) 2006-05-04
NO2009016I2 (no) 2014-08-25
LU91585I2 (fr) 2009-09-17
CZ299097B6 (cs) 2008-04-23
CA2286190A1 (en) 1998-10-22
HUP0002704A2 (hu) 2000-12-28
IL132303A0 (en) 2001-03-19
NO2009016I1 (no) 2009-08-10
JP2001523229A (ja) 2001-11-20
MY114811A (en) 2003-01-31
NZ500142A (en) 2001-10-26
US5925730A (en) 1999-07-20
HK1025104A1 (en) 2000-11-03
FR09C0028I2 (fr) 2010-06-11
RU2199549C2 (ru) 2003-02-27
SI1003774T1 (sl) 2006-08-31
ES2260833T3 (es) 2006-11-01
SK139699A3 (en) 2000-11-07
CY1108063T1 (el) 2012-01-25
AR011217A1 (es) 2000-08-02
ATE319736T1 (de) 2006-03-15
DE122009000033I1 (de) 2009-09-17
HU224836B1 (en) 2006-03-28
DE122009000033I2 (de) 2011-07-21
CN1230442C (zh) 2005-12-07
DE69833751T2 (de) 2006-11-09
HRP980197B1 (en) 2002-08-31
CN1259959A (zh) 2000-07-12
PL336213A1 (en) 2000-06-05
TW505658B (en) 2002-10-11
DK1003774T3 (da) 2006-07-03
CY2009008I1 (el) 2012-01-25
TR199902956T2 (xx) 2000-08-21
UA58547C2 (uk) 2003-08-15
BR9808523B1 (pt) 2010-02-09
PL194509B1 (pl) 2007-06-29
KR100519421B1 (ko) 2005-10-06
FR09C0028I1 (enExample) 2009-09-25
PT1003774E (pt) 2006-05-31
UY24958A1 (es) 2001-03-16
EP1003774A1 (en) 2000-05-31
ZA983062B (en) 1998-10-20
US6214798B1 (en) 2001-04-10
EE03974B1 (et) 2003-02-17
NO994906D0 (no) 1999-10-08

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Effective date: 20180413