UY24958A1 - Antagonistas de gnrh - Google Patents
Antagonistas de gnrhInfo
- 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
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.
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)
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 |
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 |
Family Cites Families (14)
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 |
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 |
-
1997
- 1997-04-11 US US08/837,042 patent/US5925730A/en not_active Expired - Lifetime
-
1998
- 1998-04-08 AR ARP980101612A patent/AR011217A1/es active IP Right Grant
- 1998-04-09 HR HR980197A patent/HRP980197B1/xx not_active IP Right Cessation
- 1998-04-09 MY MYPI98001566A patent/MY114811A/en unknown
- 1998-04-09 ZA ZA983062A patent/ZA983062B/xx unknown
- 1998-04-13 JP JP54418398A patent/JP4249806B2/ja not_active Expired - Lifetime
- 1998-04-13 UA UA99105726A patent/UA58547C2/uk unknown
- 1998-04-13 ES ES98915539T patent/ES2260833T3/es not_active Expired - Lifetime
- 1998-04-13 EP EP98915539A patent/EP1003774B1/en not_active Expired - Lifetime
- 1998-04-13 UY UY24958A patent/UY24958A1/es not_active Application Discontinuation
- 1998-04-13 NZ NZ500142A patent/NZ500142A/en not_active IP Right Cessation
- 1998-04-13 KR KR10-1999-7009315A patent/KR100519421B1/ko not_active IP Right Cessation
- 1998-04-13 DE DE69833751T patent/DE69833751T2/de not_active Expired - Lifetime
- 1998-04-13 BR BRPI9808523-9A patent/BR9808523B1/pt not_active IP Right Cessation
- 1998-04-13 AU AU69698/98A patent/AU728642B2/en not_active Expired
- 1998-04-13 DK DK98915539T patent/DK1003774T3/da active
- 1998-04-13 PL PL98336213A patent/PL194509B1/pl unknown
- 1998-04-13 IL IL13230398A patent/IL132303A0/xx active Protection Beyond IP Right Term
- 1998-04-13 RU RU99123619/04A patent/RU2199549C2/ru not_active IP Right Cessation
- 1998-04-13 WO PCT/US1998/007438 patent/WO1998046634A1/en active IP Right Grant
- 1998-04-13 CZ CZ0358699A patent/CZ299097B6/cs not_active IP Right Cessation
- 1998-04-13 SI SI9830832T patent/SI1003774T1/sl unknown
- 1998-04-13 DE DE200912000033 patent/DE122009000033I2/de active Active
- 1998-04-13 PT PT98915539T patent/PT1003774E/pt unknown
- 1998-04-13 CA CA002286190A patent/CA2286190C/en not_active Expired - Lifetime
- 1998-04-13 US US09/402,698 patent/US6214798B1/en not_active Expired - Lifetime
- 1998-04-13 CN CNB988060337A patent/CN1230442C/zh not_active Expired - Lifetime
- 1998-04-13 AT AT98915539T patent/ATE319736T1/de active
- 1998-04-13 TR TR1999/02956T patent/TR199902956T2/xx unknown
- 1998-04-13 SK SK1396-99A patent/SK285381B6/sk not_active IP Right Cessation
- 1998-04-13 EE EEP199900479A patent/EE03974B1/xx active Protection Beyond IP Right Term
- 1998-04-13 HU HU0002704A patent/HU224836B1/hu active Protection Beyond IP Right Term
- 1998-05-06 TW TW087106980A patent/TW505658B/zh not_active IP Right Cessation
-
1999
- 1999-10-08 NO NO19994906A patent/NO324991B1/no not_active IP Right Cessation
-
2000
- 2000-07-13 HK HK00104333A patent/HK1025104A1/xx not_active IP Right Cessation
-
2004
- 2004-11-04 JP JP2004320615A patent/JP3645255B1/ja not_active Expired - Lifetime
-
2006
- 2006-06-07 CY CY20061100747T patent/CY1108063T1/el unknown
-
2009
- 2009-07-03 CY CY2009008C patent/CY2009008I2/el unknown
- 2009-07-15 FR FR09C0028C patent/FR09C0028I2/fr active Active
- 2009-07-17 LU LU91585C patent/LU91585I2/fr unknown
- 2009-07-17 NL NL300395C patent/NL300395I2/nl unknown
- 2009-07-23 NO NO2009016C patent/NO2009016I2/no unknown
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
RDES | Application refused |
Effective date: 20040310 |