UY24958A1 - Antagonistas de gnrh - Google Patents

Antagonistas de gnrh

Info

Publication number
UY24958A1
UY24958A1 UY24958A UY24958A UY24958A1 UY 24958 A1 UY24958 A1 UY 24958A1 UY 24958 A UY24958 A UY 24958A UY 24958 A UY24958 A UY 24958A UY 24958 A1 UY24958 A1 UY 24958A1
Authority
UY
Uruguay
Prior art keywords
ala
4aph
4cpa
xaa10
2nal
Prior art date
Application number
UY24958A
Other languages
English (en)
Inventor
Jean E F Rivier
Guangcheng Jiang
Graeme Semple
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=UY24958(A1) "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 UY24958A1 publication Critical patent/UY24958A1/es

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)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Reproductive Health (AREA)
  • Proteomics, Peptides & Aminoacids (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)

Abstract

Esta invención proporciona péptidos, los cuales tienen mejorada la duración de las propiedades antagonistas de GnRH (hormona liberadora de gonadotropina humana). Estos antagonistas pueden usarse para regular la fertilidad y para el tratamiento de tumores dependientes de esteroides y para otros tratamientos de corta y larga duración. Estos derivados están modificados de tal manera de obtener un grupo carbamoílo o heterociclo, incluyendo una porción de urea en su cadena lateral. Particularmente son decapéptidos eficaces que continúan exhibiendo una supresión muy sustancial de la secreción de LH hasta 96 horas después de su inyección en el cuerpo, y que tienen la siguiente fórmula: Ac-D-2Nal-D-4Cpa-D-3-Pal-Ser-4Aph(L-hidrorotil)-D-4Aph(acetil)-Leu-Lys(isopropil)-Pro-D-Ala-NH2, y Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph(L-hidroorotil)-D-4Amf(Q2)-Leu-Lys(isopropil)-Pro-Xaa10, donde Q2 es Cbm ó MeCbm y Xaa10 es D-Ala-NH2, D-Ala-ol ó Ala-ol.
UY24958A 1997-04-11 1998-04-13 Antagonistas de gnrh UY24958A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US08/837,042 US5925730A (en) 1997-04-11 1997-04-11 GnRH antagonists

Publications (1)

Publication Number Publication Date
UY24958A1 true UY24958A1 (es) 2001-03-16

Family

ID=25273352

Family Applications (1)

Application Number Title Priority Date Filing Date
UY24958A UY24958A1 (es) 1997-04-11 1998-04-13 Antagonistas de gnrh

Country Status (37)

Country Link
US (2) US5925730A (es)
EP (1) EP1003774B1 (es)
JP (2) JP4249806B2 (es)
KR (1) KR100519421B1 (es)
CN (1) CN1230442C (es)
AR (1) AR011217A1 (es)
AT (1) ATE319736T1 (es)
AU (1) AU728642B2 (es)
BR (1) BR9808523B1 (es)
CA (1) CA2286190C (es)
CY (2) CY1108063T1 (es)
CZ (1) CZ299097B6 (es)
DE (2) DE69833751T2 (es)
DK (1) DK1003774T3 (es)
EE (1) EE03974B1 (es)
ES (1) ES2260833T3 (es)
FR (1) FR09C0028I2 (es)
HK (1) HK1025104A1 (es)
HR (1) HRP980197B1 (es)
HU (1) HU224836B1 (es)
IL (1) IL132303A0 (es)
LU (1) LU91585I2 (es)
MY (1) MY114811A (es)
NL (1) NL300395I2 (es)
NO (2) NO324991B1 (es)
NZ (1) NZ500142A (es)
PL (1) PL194509B1 (es)
PT (1) PT1003774E (es)
RU (1) RU2199549C2 (es)
SI (1) SI1003774T1 (es)
SK (1) SK285381B6 (es)
TR (1) TR199902956T2 (es)
TW (1) TW505658B (es)
UA (1) UA58547C2 (es)
UY (1) UY24958A1 (es)
WO (1) WO1998046634A1 (es)
ZA (1) ZA983062B (es)

Families Citing this family (37)

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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
US5977302A (en) * 1997-11-20 1999-11-02 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
DE20321887U1 (de) 2003-11-10 2012-01-20 Allergan, Inc. Arzneimittel umfassend niedrige Dosierungen von Desmopressin
EP2322195A2 (en) 2003-11-10 2011-05-18 Reprise Biopharmaceutics, LLC 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
EP2526950A1 (en) * 2006-04-07 2012-11-28 Merrion Research III Limited Solid oral dosage form containing an enhancer
JOP20090061B1 (ar) 2008-02-11 2021-08-17 Ferring Int Center Sa طريقة معالجة سرطان البروستاتا بمضادات الهرمونات التناسلية GnRH
KR20110007614A (ko) * 2008-05-07 2011-01-24 메리온 리서치 Ⅲ 리미티드 ＧｎＲＨ 관련 화합물의 조성물 및 제조 방법
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
CN102421414A (zh) * 2009-05-01 2012-04-18 辉凌公司 用于治疗前列腺癌的组合物
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
US9260480B2 (en) 2010-10-27 2016-02-16 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
CN103476419A (zh) 2011-01-07 2013-12-25 梅里翁第三研究有限公司 口服投药的含铁药物组合物
JO3755B1 (ar) 2011-01-26 2021-01-31 Ferring Bv تركيبات تستوستيرون
WO2013104745A1 (en) 2012-01-13 2013-07-18 Ferring Bv Pharmaceutical composition
EP2854831B1 (en) 2012-06-01 2024-07-10 Ferring B.V. Manufacture of degarelix
EP3250191B1 (en) 2015-01-29 2024-01-17 Novo Nordisk A/S Tablets comprising glp-1 agonist and enteric coating
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
CN111943960B (zh) 2019-07-29 2022-02-15 广东东阳光药业有限公司 取代的嘧啶二酮类化合物及其用途
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

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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
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
DE593491T1 (de) * 1991-04-25 1994-11-17 Romano S.-Cergue 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
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
JP4249806B2 (ja) 2009-04-08
US6214798B1 (en) 2001-04-10
NL300395I1 (nl) 2009-09-01
SK139699A3 (en) 2000-11-07
CZ358699A3 (cs) 2000-06-14
ES2260833T3 (es) 2006-11-01
MY114811A (en) 2003-01-31
CN1230442C (zh) 2005-12-07
AU728642B2 (en) 2001-01-11
SI1003774T1 (sl) 2006-08-31
EP1003774B1 (en) 2006-03-08
US5925730A (en) 1999-07-20
CA2286190C (en) 2007-01-09
CZ299097B6 (cs) 2008-04-23
KR20010006233A (ko) 2001-01-26
EE03974B1 (et) 2003-02-17
UA58547C2 (uk) 2003-08-15
DE122009000033I2 (de) 2011-07-21
NO2009016I2 (no) 2014-08-25
FR09C0028I2 (fr) 2010-06-11
JP2005120101A (ja) 2005-05-12
DK1003774T3 (da) 2006-07-03
CA2286190A1 (en) 1998-10-22
DE69833751T2 (de) 2006-11-09
ZA983062B (en) 1998-10-20
TW505658B (en) 2002-10-11
PL336213A1 (en) 2000-06-05
HK1025104A1 (en) 2000-11-03
RU2199549C2 (ru) 2003-02-27
WO1998046634A1 (en) 1998-10-22
FR09C0028I1 (es) 2009-09-25
HUP0002704A2 (hu) 2000-12-28
CY2009008I1 (el) 2012-01-25
TR199902956T2 (xx) 2000-08-21
CY2009008I2 (el) 2012-01-25
BR9808523B1 (pt) 2010-02-09
HRP980197A2 (en) 1999-02-28
CY1108063T1 (el) 2012-01-25
HRP980197B1 (en) 2002-08-31
HUP0002704A3 (en) 2003-08-28
IL132303A0 (en) 2001-03-19
JP2001523229A (ja) 2001-11-20
NL300395I2 (nl) 2010-01-04
NO994906L (no) 1999-12-13
PL194509B1 (pl) 2007-06-29
HU224836B1 (en) 2006-03-28
JP3645255B1 (ja) 2005-05-11
CN1259959A (zh) 2000-07-12
DE69833751D1 (de) 2006-05-04
AR011217A1 (es) 2000-08-02
BR9808523A (pt) 2000-05-23
NZ500142A (en) 2001-10-26
EE9900479A (et) 2000-06-15
LU91585I2 (fr) 2009-09-17
NO2009016I1 (no) 2009-08-10
NO994906D0 (no) 1999-10-08
PT1003774E (pt) 2006-05-31
DE122009000033I1 (de) 2009-09-17
NO324991B1 (no) 2008-01-14
SK285381B6 (sk) 2006-12-07
AU6969898A (en) 1998-11-11
ATE319736T1 (de) 2006-03-15
EP1003774A1 (en) 2000-05-31
KR100519421B1 (ko) 2005-10-06

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