EP0868178A4 - Antagonisten des gonadotropin releasing hormons - Google Patents

Antagonisten des gonadotropin releasing hormons

Info

Publication number
EP0868178A4
EP0868178A4 EP96943763A EP96943763A EP0868178A4 EP 0868178 A4 EP0868178 A4 EP 0868178A4 EP 96943763 A EP96943763 A EP 96943763A EP 96943763 A EP96943763 A EP 96943763A EP 0868178 A4 EP0868178 A4 EP 0868178A4
Authority
EP
European Patent Office
Prior art keywords
gonadoliberin
antagonists
gonadoliberin antagonists
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.)
Withdrawn
Application number
EP96943763A
Other languages
English (en)
French (fr)
Other versions
EP0868178A1 (de
Inventor
Mark Goulet
Robert L Bugianesi
Wallace T Ashton
Lin Chu
Michael H Fisher
Peter Lin
Roy G Smith
Mitree M Ponpipom
Matthew J Wyvratt
Yi Tien Yang
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.)
Merck and Co Inc
Original Assignee
Merck and Co Inc
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
Priority claimed from GBGB9603370.9A external-priority patent/GB9603370D0/en
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of EP0868178A1 publication Critical patent/EP0868178A1/de
Publication of EP0868178A4 publication Critical patent/EP0868178A4/de
Withdrawn legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C07D209/16—Tryptamines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/16—Central respiratory analeptics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P15/16—Masculine 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
    • A61P15/18—Feminine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Anesthesiology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EP96943763A 1995-12-14 1996-12-10 Antagonisten des gonadotropin releasing hormons Withdrawn EP0868178A4 (de)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US863295P 1995-12-14 1995-12-14
US8632P 1995-12-14
GB9603370 1996-02-16
GBGB9603370.9A GB9603370D0 (en) 1996-02-16 1996-02-16 Antagonists of gonadotropin releasing hormone
PCT/US1996/020004 WO1997021435A1 (en) 1995-12-14 1996-12-10 Antagonists of gonadotropin releasing hormone

Publications (2)

Publication Number Publication Date
EP0868178A1 EP0868178A1 (de) 1998-10-07
EP0868178A4 true EP0868178A4 (de) 2000-03-29

Family

ID=26308743

Family Applications (1)

Application Number Title Priority Date Filing Date
EP96943763A Withdrawn EP0868178A4 (de) 1995-12-14 1996-12-10 Antagonisten des gonadotropin releasing hormons

Country Status (5)

Country Link
EP (1) EP0868178A4 (de)
JP (2) JP3092947B2 (de)
AU (1) AU704937B2 (de)
CA (1) CA2240115A1 (de)
WO (1) WO1997021435A1 (de)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ183198A3 (cs) * 1995-12-14 1998-10-14 Merck And Co., Inc. Nepeptidové deriváty, antagonizující hormon, uvolňující gonadotropin a farmaceutický prostředek
CA2292881A1 (en) * 1997-06-05 1998-12-10 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
GB9718833D0 (en) * 1997-09-04 1997-11-12 Merck Sharp & Dohme Therapeutic agents
WO1999058518A2 (en) * 1998-05-12 1999-11-18 American Home Products Corporation Biphenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia
US6232322B1 (en) 1998-05-12 2001-05-15 American Home Products Corporation Biphenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia
US6346534B1 (en) 1998-09-23 2002-02-12 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
US6310081B1 (en) 1999-05-10 2001-10-30 American Home Products Corporation Biphenyl sulfonyl aryl carboxylic acids useful in the treatment of insulin resistance and hyperglycemia
US6537998B1 (en) 1999-10-15 2003-03-25 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
CA2398018C (en) 2000-01-25 2011-10-18 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
GB0022670D0 (en) 2000-09-15 2000-11-01 Astrazeneca Ab Molecules
GB0031315D0 (en) * 2000-12-21 2001-02-07 Glaxo Group Ltd Indole derivatives
SE0100566D0 (sv) 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
SE0101692D0 (sv) 2001-05-14 2001-05-14 Astrazeneca Ab Compounds
MXPA04000986A (es) 2001-08-02 2005-02-17 Neurocrine Biosciences Inc 1,2,3-triazin-3,5-dionas sustituidas como antagonistas del receptor de hormona de liberacion de gonadotropina (gnrh).
WO2003011293A2 (en) 2001-08-02 2003-02-13 Neurocrine Biosciences, Inc. Pyridinone and pyridazinone derivatives as gonadotropin-releasing hormone receptor antagonists
KR20040030893A (ko) 2001-08-02 2004-04-09 뉴로크린 바이오사이언시즈 인코퍼레이티드 치환된 피리딘-4-온 및 고나도트로핀 분비 호르몬 수용체길항제로서의 이의 용도
AU2002324586B2 (en) 2001-08-02 2008-04-24 Neurocrine Biosciences, Inc. 1,3,5-triazine-2,4,6-triones, preparation and use as gonadotropin-releasing hormone receptor antagonists
WO2003011870A1 (en) 2001-08-02 2003-02-13 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists
FR2833948B1 (fr) * 2001-12-21 2004-02-06 Sod Conseils Rech Applic Nouveaux derives de benzimidazole et leur utilisation en tant que medicament
AU2003202115A1 (en) 2002-02-12 2003-09-04 Pfizer Inc. Non-peptide compounds affecting the action of gonadotropin-releasing hormone (gnrh)
BR0312123A (pt) 2002-06-13 2005-03-29 Pfizer Agentes de gnrh não peptìdicos, composições farmacêuticas e métodos para o seu uso
TW200407127A (en) 2002-08-21 2004-05-16 Astrazeneca Ab Chemical compounds
GB0219472D0 (en) 2002-08-21 2002-10-02 Astrazeneca Ab Chemical compounds
ES2286493T3 (es) 2002-08-21 2007-12-01 Astrazeneca Ab Derivados de pirazol como inhibidores de gnrh.
DE60318716T2 (de) 2002-08-21 2009-01-08 Astrazeneca Ab Thieno-pyrrole verbindungen als antagonisten der gonadotropin-freisetzenden hormonrezeptoren
TW200413351A (en) 2002-08-21 2004-08-01 Astrazeneca Ab Chemical compounds
EP1644342B1 (de) 2003-07-07 2012-05-09 Neurocrine Biosciences, Inc. Arylpyrimidine geeignet zur Behandlung von sexualhormonbedingten Zuständen wie Endometriose, Prostatakrebs und dergleichen
ATE428427T1 (de) 2003-07-07 2009-05-15 Neurocrine Biosciences Inc Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten
CA2531508C (en) 2003-07-07 2013-10-08 Neurocrine Biosciences, Inc. Pyrimidine-2, 4-dione derivatives as gonadotropin-releasing hormone receptor antagonists
FR2860514A1 (fr) * 2003-10-03 2005-04-08 Sanofi Synthelabo Derives d'arylalkylcarbamates, leur preparation et leur application en therapeutique
DE102004033902A1 (de) 2004-07-14 2006-02-16 Zentaris Gmbh Neue Tetrahydrocarbazolderivate mit verbesserter biologischer Wirkung und verbesserter Löslichkeit als Liganden für G-Protein gekoppelte Rezeptoren (GPCR's)
CA2664800A1 (en) 2006-10-02 2008-04-10 Timothy Andrew Stewart Ketoconazole enantiomer in humans
EP2095818A1 (de) 2008-02-29 2009-09-02 AEterna Zentaris GmbH Verwendung von LHRH-Antagonisten in nicht-kastrierenden Dosen
TW201130854A (en) 2009-12-22 2011-09-16 Bayer Schering Pharma Ag Pyridinone derivatives and pharmaceutical compositions thereof
WO2012175514A1 (en) 2011-06-21 2012-12-27 Bayer Intellectual Property Gmbh Pyridinone derivatives and pharmaceutical compositions thereof
EP3185881B1 (de) 2014-08-26 2022-03-09 Betanien Hospital Verfahren, wirkstoffe und zusammensetzungen zur behandlung von entzündlichen erkrankungen
CN105348168B (zh) * 2015-11-06 2018-04-10 厦门大学 1‑(2‑(金刚烷‑1‑基)‑1h‑吲哚‑5‑基)‑3‑取代脲衍生物及制备和用途

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2181559A1 (en) * 1972-04-28 1973-12-07 Aec Chimie Organique Bio N-Phenylalkyl-N-3-indolylalkyl-alkylamines - with sedative, neuroleptic, analgesic, hypotensive, antiserotonin, adrenolytic activity
EP0348341A2 (de) * 1988-06-23 1989-12-27 Schering Aktiengesellschaft Aminoalkylindole, Verfahren zu deren Herstellung und diese enthaltende pharmazeutische Präparate
EP0679642A1 (de) * 1994-04-28 1995-11-02 Takeda Chemical Industries, Ltd. Kondensierte heterocyclische Verbindungen, ihre Herstellung und Anwendung
WO1997021707A1 (en) * 1995-12-14 1997-06-19 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
WO1997021703A1 (en) * 1995-12-14 1997-06-19 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
WO1997021704A1 (en) * 1995-12-14 1997-06-19 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2825734A (en) 1955-04-11 1958-03-04 Upjohn Co Reduction of carbonylic radicals in indolyl-3 compounds
US4070369A (en) * 1972-12-13 1978-01-24 Schering Corporation 2-Aminomethyl-5-chloro-3-(2,4-dichlorophenyl)indole
US4087444A (en) * 1976-09-08 1978-05-02 Eli Lilly And Company Amides as ovulation inhibitors

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2181559A1 (en) * 1972-04-28 1973-12-07 Aec Chimie Organique Bio N-Phenylalkyl-N-3-indolylalkyl-alkylamines - with sedative, neuroleptic, analgesic, hypotensive, antiserotonin, adrenolytic activity
EP0348341A2 (de) * 1988-06-23 1989-12-27 Schering Aktiengesellschaft Aminoalkylindole, Verfahren zu deren Herstellung und diese enthaltende pharmazeutische Präparate
EP0679642A1 (de) * 1994-04-28 1995-11-02 Takeda Chemical Industries, Ltd. Kondensierte heterocyclische Verbindungen, ihre Herstellung und Anwendung
WO1997021707A1 (en) * 1995-12-14 1997-06-19 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
WO1997021703A1 (en) * 1995-12-14 1997-06-19 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
WO1997021704A1 (en) * 1995-12-14 1997-06-19 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
DATABASE CHEMABS [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; RAO, RAVINDRA PRATAP: "Synthesis of some Mannich bases from 2-phenylindole and 5-nitro 2-phenylindole", XP002126977, retrieved from STN Database accession no. 71:91198 *
GARRATT, PETER J. ET AL: "Mapping the Melatonin Receptor. 3. Design and Synthesis of Melatonin Agonists and Antagonists Derived from 2-Phenyltryptamines", J. MED. CHEM. (1995), 38(7), 1132-9, XP002126976 *
LABDEV, PART A (1969), 7(2), 99-100 *
See also references of WO9721435A1 *

Also Published As

Publication number Publication date
JP3092947B2 (ja) 2000-09-25
AU704937B2 (en) 1999-05-06
WO1997021435A1 (en) 1997-06-19
AU1291997A (en) 1997-07-03
JP2001039871A (ja) 2001-02-13
CA2240115A1 (en) 1997-06-19
EP0868178A1 (de) 1998-10-07
JPH11504040A (ja) 1999-04-06

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