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Withdrawn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Withdrawn legal-status Critical Current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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Anesthesiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole 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
GBGB9603370.9A GB9603370D0 (en) 1996-02-16 1996-02-16 Antagonists of gonadotropin releasing hormone
GB9603370 1996-02-16
PCT/US1996/020004 WO1997021435A1 (en) 1995-12-14 1996-12-10 Antagonists of gonadotropin releasing hormone
US8632P 2007-12-21

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
JP3092946B2 (ja) * 1995-12-14 2000-09-25 メルク エンド カンパニー インコーポレーテッド ゴナドトロピン放出ホルモン拮抗剤
EP0986385A4 (de) * 1997-06-05 2001-05-16 Merck & Co Inc Antagonisten des gonadorelins
GB9718833D0 (en) 1997-09-04 1997-11-12 Merck Sharp & Dohme Therapeutic agents
EP1077967B1 (de) * 1998-05-12 2002-12-04 Wyeth Zur behandlung von insulin-resistenz und hyperglycemie geeignete biphenyl-oxo-essigsäuren
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
WO2001055119A2 (en) 2000-01-25 2001-08-02 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
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
EP1411941A2 (de) 2001-08-02 2004-04-28 Neurocrine Biosciences, Inc. Pyridinon- und pyridazinonderivate als antagonisten des gonadotropin-freisetzungshormon-rezeptors
JP2005500352A (ja) 2001-08-02 2005-01-06 ニューロクライン バイオサイエンシーズ， インコーポレイテッド ゴナドトロピン放出ホルモンレセプター（ＧｎＲＨ）アンタゴニストとしての１，２，４−トリアジン−３，５−ジオン
US6939883B2 (en) 2001-08-02 2005-09-06 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
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
WO2003068769A1 (en) 2002-02-12 2003-08-21 Pfizer Inc. Non-peptide compounds affecting the action of gonadotropin-releasing hormone (gnrh)
CA2489252A1 (en) 2002-06-13 2003-12-24 Pfizer Inc. Non-peptide gnrh agents, pharmaceutical compositions and methods for their use
TW200413351A (en) 2002-08-21 2004-08-01 Astrazeneca Ab Chemical compounds
GB0219472D0 (en) * 2002-08-21 2002-10-02 Astrazeneca Ab Chemical compounds
JP2006508050A (ja) 2002-08-21 2006-03-09 アストラゼネカ アクチボラグ ゴナドトロピン放出ホルモンのアンタゴニストとしてのチエノピロール化合物
TW200407127A (en) 2002-08-21 2004-05-16 Astrazeneca Ab Chemical compounds
DE60314158T2 (de) 2002-08-21 2008-01-31 Astrazeneca Ab Pyrazolderivate als gnrh-inhibitoren
DE602004020638D1 (de) 2003-07-07 2009-05-28 Neurocrine Biosciences Inc Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten
AU2004257639B2 (en) 2003-07-07 2011-01-06 Neurocrine Biosciences, Inc. Pyrimidine-2, 4-dione derivatives as gonadotropin-releasing hormone receptor antagonists
ES2387495T3 (es) 2003-07-07 2012-09-25 Neurocrine Biosciences, Inc. Arilpirimidinas útiles en el tratamiento de trastornos relacionados con las hormonas sexuales, tales como endometriosis, cáncer de próstata y similares
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)
AU2007303219A1 (en) 2006-10-02 2008-04-10 Cortendo Ab (Publ) 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
US10821152B2 (en) 2014-08-26 2020-11-03 Betanien Hospital Methods, agents and compositions for treatment of inflammatory conditions
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
WO1997021704A1 (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

Family Cites Families (3)

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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
WO1997021704A1 (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

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

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