CY1108063T1 - Gnrh ανταγωνιστες τροποποιημενοι στις θεσεις 5 και 6 - Google Patents

Gnrh ανταγωνιστες τροποποιημενοι στις θεσεις 5 και 6

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Publication number
CY1108063T1
CY1108063T1 CY20061100747T CY061100747T CY1108063T1 CY 1108063 T1 CY1108063 T1 CY 1108063T1 CY 20061100747 T CY20061100747 T CY 20061100747T CY 061100747 T CY061100747 T CY 061100747T CY 1108063 T1 CY1108063 T1 CY 1108063T1
Authority
CY
Cyprus
Prior art keywords
ala
4aph
modified
positions
hydroorotyl
Prior art date
Application number
CY20061100747T
Other languages
English (en)
Inventor
Guangcheng Jiang
Graeme Semple
Jean E.F. Dr. RIVIER
Original Assignee
Ferring B.V
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=CY1108063(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Ferring B.V filed Critical Ferring B.V
Publication of CY1108063T1 publication Critical patent/CY1108063T1/el

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    • 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)
  • 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

Πεπτίδια παρέχονται τα οποία έχουν βελτιωμένη διάρκεια GnRH ανταγωνιστικών ιδιοτήτων. Αυτοί οι ανταγωνιστές μπορεί να χρησιμοποιηθούν για να ρυθμίσουν τη γονιμότητα και να αντιμετωπίσουν εξαρτώμενους από στεροειδή όγκους και για βραχυπρόθεσμες και μακροπρόθεσμες ενδείξεις αγωγής. Αυτοί οι ανταγωνιστές έχουν ένα παράγωγο αμινοΡhe ή του ισοδυνάμου του στις 5- και 6- θέσεις. Αυτό το παράγωγο είναι τροποποιημένο έτσι ώστε να περιέχει μια καρβαμοϋλική ομάδα ή ετεροκυκλική, περιλαμβάνοντας ένα κομμάτι ουρίας στην πλευρική της αλυσίδα. Ιδιαίτερα αποτελεσματικά δεκαπεπτίδια, τα οποία συνεχίζουν να εμφανίζουν πολύ σημαντική καταστολή την έκκρισης LH στις 96 ώρες μετά από ένεση, έχουν τους τύπους: Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph(L-υδροοροτυλο)-D-4Aph(ακετυλο)-Leu-Lys(ισοπροπυλο)-Ρro-D-Ala-ΝΗ2, και Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph(L-υδροοροτυλο)-D-4Amf(Q2)-Leu-Lys(ισοπροπυλο)-Ρro-Χaa10, όπου το Q2 είναι Cbm ή MeCbm και Xaa10 είναι D-Ala-NH2, D-Ala-ol ή Ala-ol.
CY20061100747T 1997-04-11 2006-06-07 Gnrh ανταγωνιστες τροποποιημενοι στις θεσεις 5 και 6 CY1108063T1 (el)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
CY1108063T1 true CY1108063T1 (el) 2012-01-25

Family

ID=25273352

Family Applications (2)

Application Number Title Priority Date Filing Date
CY20061100747T CY1108063T1 (el) 1997-04-11 2006-06-07 Gnrh ανταγωνιστες τροποποιημενοι στις θεσεις 5 και 6
CY2009008C CY2009008I2 (el) 1997-04-11 2009-07-03 Gnrh ανταγωνιστες τροποποιημενοι στις θεσεις 5 και 6

Family Applications After (1)

Application Number Title Priority Date Filing Date
CY2009008C CY2009008I2 (el) 1997-04-11 2009-07-03 Gnrh ανταγωνιστες τροποποιημενοι στις θεσεις 5 και 6

Country Status (37)

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

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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
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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
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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
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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
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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 (el) 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
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
UY24958A1 (es) 2001-03-16
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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