WO2003051837A8 - Derives tetrahydrocarbazol servant de ligands de recepteurs couples aux proteines g (gpcr) - Google Patents

Derives tetrahydrocarbazol servant de ligands de recepteurs couples aux proteines g (gpcr)

Info

Publication number
WO2003051837A8
WO2003051837A8 PCT/EP2002/014344 EP0214344W WO03051837A8 WO 2003051837 A8 WO2003051837 A8 WO 2003051837A8 EP 0214344 W EP0214344 W EP 0214344W WO 03051837 A8 WO03051837 A8 WO 03051837A8
Authority
WO
WIPO (PCT)
Prior art keywords
gpcr
tetrahydrocarbozole
ligands
derivatives
protein coupled
Prior art date
Application number
PCT/EP2002/014344
Other languages
German (de)
English (en)
Other versions
WO2003051837A2 (fr
WO2003051837A3 (fr
Inventor
Marcus Koppitz
Hans Peter Muhn
Ken Shaw
Holger Hess-Stumpp
Klaus Paulini
Original Assignee
Zentaris Gmbh
Marcus Koppitz
Hans Peter Muhn
Ken Shaw
Holger Hess-Stumpp
Klaus Paulini
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 DE10164564A external-priority patent/DE10164564B4/de
Priority to EP02796648A priority Critical patent/EP1453803A2/fr
Priority to CA002468880A priority patent/CA2468880A1/fr
Priority to BR0214958-3A priority patent/BR0214958A/pt
Priority to IL16162602A priority patent/IL161626A0/xx
Priority to AU2002361430A priority patent/AU2002361430B2/en
Priority to KR10-2004-7009212A priority patent/KR20040072657A/ko
Priority to RU2004121776/04A priority patent/RU2319692C2/ru
Priority to NZ533430A priority patent/NZ533430A/en
Priority to UA20040503889A priority patent/UA77025C2/xx
Priority to HU0500014A priority patent/HUP0500014A3/hu
Priority to MXPA04005768A priority patent/MXPA04005768A/es
Priority to JP2003552724A priority patent/JP2005518375A/ja
Application filed by Zentaris Gmbh, Marcus Koppitz, Hans Peter Muhn, Ken Shaw, Holger Hess-Stumpp, Klaus Paulini filed Critical Zentaris Gmbh
Publication of WO2003051837A2 publication Critical patent/WO2003051837A2/fr
Publication of WO2003051837A3 publication Critical patent/WO2003051837A3/fr
Publication of WO2003051837A8 publication Critical patent/WO2003051837A8/fr
Priority to NO20042198A priority patent/NO326692B1/no
Priority to HR20040609A priority patent/HRP20040609A2/hr
Priority to IL192991A priority patent/IL192991A0/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • 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
    • 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
    • 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
    • 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
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • C07D209/86—Carbazoles; Hydrogenated carbazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the ring system
    • 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
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • C07D209/88—Carbazoles; Hydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Biophysics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Biochemistry (AREA)
  • Diabetes (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La présente invention concerne de nouveaux dérivés tétrahydrocarbazol servant de ligands de récepteurs couplés aux protéines G (GPCR), notamment d'antagonistes de gonadolibérine (GnRH). L'invention concerne également une composition pharmaceutique contenant ces nouveaux dérivés tétrahydrocarbazol ainsi qu'un procédé de fabrication de ceux-ci. L'invention concerne par ailleurs l'administration de dérivés tétrahydrocarbazol pour le traitement de troubles à médiation par GPCR, notamment pour l'inhibition de GnRH, à des mammifères, notamment des humains, nécessitant un tel traitement, ainsi que l'utilisation de dérivés tétrahydrocarbazol pour la fabrication d'un agent pharmaceutique destiné au traitement de troubles à médiation par GPCR, notamment à l'inhibition de GnRH.
PCT/EP2002/014344 2001-12-14 2002-12-16 Derives tetrahydrocarbazol servant de ligands de recepteurs couples aux proteines g (gpcr) WO2003051837A2 (fr)

Priority Applications (15)

Application Number Priority Date Filing Date Title
CA002468880A CA2468880A1 (fr) 2001-12-14 2002-12-16 Derives tetrahydrocarbazol servant de ligands de recepteurs couples aux proteines g (gpcr)
HU0500014A HUP0500014A3 (en) 2001-12-14 2002-12-16 Tetrahydrocarbozole derivatives as ligands for g-protein coupled receptors (gpcr) and pharmaceutical compositions containing them
UA20040503889A UA77025C2 (en) 2001-12-14 2002-12-16 Tetrahydrocarbozole derivatives as ligands for g-protein coupled receptors (gpcr), a pharmaceutical composition and a method for preparation of compounds
IL16162602A IL161626A0 (en) 2001-12-14 2002-12-16 Tetrahydrocarbozole derivatives as ligands for g-protein coupled receptors (gpcr)
AU2002361430A AU2002361430B2 (en) 2001-12-14 2002-12-16 Tetrahydrocarbozole derivatives as ligands for G-protein coupled receptors (GPCR)
KR10-2004-7009212A KR20040072657A (ko) 2001-12-14 2002-12-16 Ｇ-단백질 커플링된 수용체(ｇｐｃｒ)에 대한리간드로서의 테트라하이드로카바졸 유도체
RU2004121776/04A RU2319692C2 (ru) 2001-12-14 2002-12-16 Производные тетрагидрокарбазола, способ получения производных тетрагидрокарбазола (варианты), их применение (варианты) и фармацевтическая композиция, обладающая активностью антагониста гонадотропин-рилизинг-гормона (варианты)
NZ533430A NZ533430A (en) 2001-12-14 2002-12-16 Tetrahydrocarbozole derivatives as ligands for G-protein coupled receptors (GPCR)
BR0214958-3A BR0214958A (pt) 2001-12-14 2002-12-16 Derivados de tetraidrocarbazol como ligandos para receptores acoplados à proteìna-g (gpcr)
EP02796648A EP1453803A2 (fr) 2001-12-14 2002-12-16 Derives tetrahydrocarbazol servant de ligands de recepteurs couples aux proteines g (gpcr)
JP2003552724A JP2005518375A (ja) 2001-12-14 2002-12-16 Ｇタンパク質結合受容体（ｇｐｃｒ）のためのリガンドとしてのテトラヒドロカルバゾール誘導体
MXPA04005768A MXPA04005768A (es) 2001-12-14 2002-12-16 Derivados de tetrahidrocarbazol como ligandos para receptores acoplados a proteina g (gpcr).
NO20042198A NO326692B1 (no) 2001-12-14 2004-05-26 Tetrahydrokarbazolderivater som ligander for G-proteinkoplede reseptorer (GPCR), anvendelse derav samt farmasøytiske preparater inneholdende disse
HR20040609A HRP20040609A2 (en) 2001-12-14 2004-07-05 Tetrahydrocarbozole derivatives as ligands for g-protein coupled receptors (gpcr)
IL192991A IL192991A0 (en) 2001-12-14 2008-07-23 Use of tetrahydrocarbazole derivatives for the manufacture of medicanents for treating gonadotropin-releasing hormone

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DE10164564A DE10164564B4 (de) 2001-12-14 2001-12-14 Tetrahydrocarbazolderivate als Liganden für G-Protein gekoppelte Rezeptoren (GPCR)
DE10164564.3 2001-12-14
US34187801P 2001-12-21 2001-12-21
US60/341,878 2001-12-21

Publications (3)

Publication Number Publication Date
WO2003051837A2 WO2003051837A2 (fr) 2003-06-26
WO2003051837A3 WO2003051837A3 (fr) 2004-02-26
WO2003051837A8 true WO2003051837A8 (fr) 2004-05-06

Family

ID=26010882

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2002/014344 WO2003051837A2 (fr) 2001-12-14 2002-12-16 Derives tetrahydrocarbazol servant de ligands de recepteurs couples aux proteines g (gpcr)

Country Status (17)

Country Link
EP (1) EP1453803A2 (fr)
JP (1) JP2005518375A (fr)
CN (1) CN100500654C (fr)
AR (1) AR037863A1 (fr)
AU (1) AU2002361430B2 (fr)
BR (1) BR0214958A (fr)
CA (1) CA2468880A1 (fr)
HR (1) HRP20040609A2 (fr)
HU (1) HUP0500014A3 (fr)
IL (2) IL161626A0 (fr)
MX (1) MXPA04005768A (fr)
NO (1) NO326692B1 (fr)
NZ (1) NZ533430A (fr)
PL (1) PL373400A1 (fr)
RU (1) RU2319692C2 (fr)
TW (1) TWI246423B (fr)
WO (1) WO2003051837A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008107446A1 (fr) * 2007-03-05 2008-09-12 Æterna Zentaris Gmbh Utilisation d'antagonistes de lhrh pour traitement de symptômes du tractus urinaire inférieur, vessie hyperactive et/ou hyperactivité du détrusor en particulier

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2379169T3 (es) * 2003-05-19 2012-04-23 Irm Llc Composiciones y compuestos inmunosupresores
JP2007501284A (ja) * 2003-06-10 2007-01-25 スミスクライン ビーチャム コーポレーション テトラヒドロカルバゾール誘導体およびそれらの薬学的使用
US20060074124A1 (en) * 2003-09-12 2006-04-06 Andrew Napper Methods of treating a disorder
EP1677794B1 (fr) * 2003-09-12 2014-12-03 Elixir Pharmaceuticals, Inc. Procedes de traitement de troubles
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)
ES2369782T3 (es) * 2004-12-27 2011-12-05 Actelion Pharmaceuticals Ltd. Derivados de 2,3,4,9-tetrahidro-1h-carbazol como antagonistas del receptor crth2.
DK1902026T3 (da) * 2005-06-24 2010-04-26 Lilly Co Eli Tetrahydrocarbazol-derivater, der kan anvendes som androgen-receptor-modulatorer (SARM)
KR101411820B1 (ko) * 2006-08-07 2014-06-24 액테리온 파마슈티칼 리미티드 (3-아미노-1,2,3,4-테트라하이드로-9ｈ-카르바졸-9-일)-아세트산 유도체
EP1988098A1 (fr) * 2007-04-27 2008-11-05 AEterna Zentaris GmbH Nouveaux dérivés de tétrahydrocarbazole en tant que ligands de récepteurs couplés à la protéine G
EP2095818A1 (fr) 2008-02-29 2009-09-02 AEterna Zentaris GmbH Utilisation d'antagonistes LHRH dans des doses n'impliquant pas de castration
BR112012024114B1 (pt) 2010-03-22 2021-02-09 Idorsia Pharmaceuticals Ltd Compostos derivados de 3-(heteroarilamino)-1,2,3,4-tetrahidro-9h-carbazol, uso dos mesmos, e, composição farmacêutica
AU2012241442B2 (en) 2011-04-14 2017-01-12 Idorsia Pharmaceuticals Ltd 7-(heteroaryl-amino)-6,7,8,9-tetrahydropyrido(1,2-a)indol acetic acid derivatives and their use as prostaglandin D2 receptor modulators
LT3119779T (lt) 2014-03-17 2018-09-10 Idorsia Pharmaceuticals Ltd Azaindolo acto rūgšties dariniai ir jų panaudojimas kaip prostaglandino d2 receptoriaus moduliatorių
TW201620909A (zh) 2014-03-18 2016-06-16 艾克泰聯製藥有限公司 氮雜吲哚乙酸衍生物及彼等作為前列腺素ｄ２受體調節劑之用途
MX2018003202A (es) 2015-09-15 2018-06-08 Idorsia Pharmaceuticals Ltd Formas cristalinas.

Family Cites Families (4)

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Publication number Priority date Publication date Assignee Title
GB1418703A (en) * 1973-06-02 1975-12-24 Pfizer Ltd 3-alkyl-9-substituted-1,2,3,4-tetrahydrocarbazoles
ATE90076T1 (de) * 1986-03-27 1993-06-15 Merck Frosst Canada Inc Tetrahydrocarbazole ester.
US5607939A (en) * 1994-04-28 1997-03-04 Takeda Chemical Industries, Ltd. Condensed heterocyclic compounds, their production and use
CA2292881A1 (fr) * 1997-06-05 1998-12-10 Merck & Co., Inc. Antagonistes de gonadoliberine

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008107446A1 (fr) * 2007-03-05 2008-09-12 Æterna Zentaris Gmbh Utilisation d'antagonistes de lhrh pour traitement de symptômes du tractus urinaire inférieur, vessie hyperactive et/ou hyperactivité du détrusor en particulier

Also Published As

Publication number Publication date
WO2003051837A2 (fr) 2003-06-26
PL373400A1 (en) 2005-08-22
HUP0500014A3 (en) 2010-06-28
CN100500654C (zh) 2009-06-17
AU2002361430A1 (en) 2003-06-30
HRP20040609A2 (en) 2005-06-30
TWI246423B (en) 2006-01-01
IL161626A0 (en) 2004-09-27
AR037863A1 (es) 2004-12-09
NO20042198L (no) 2004-07-09
RU2004121776A (ru) 2005-05-10
CA2468880A1 (fr) 2003-06-26
TW200305405A (en) 2003-11-01
WO2003051837A3 (fr) 2004-02-26
EP1453803A2 (fr) 2004-09-08
BR0214958A (pt) 2004-12-28
RU2319692C2 (ru) 2008-03-20
JP2005518375A (ja) 2005-06-23
NZ533430A (en) 2005-12-23
HUP0500014A2 (hu) 2005-04-28
AU2002361430B2 (en) 2007-09-13
IL192991A0 (en) 2011-08-01
MXPA04005768A (es) 2004-09-10
CN1599720A (zh) 2005-03-23
NO326692B1 (no) 2009-02-02

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