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WO2009049791A3 - Radiolabeled nk3 receptor antagonist - Google Patents

Radiolabeled nk3 receptor antagonist Download PDF

Info

Publication number
WO2009049791A3
WO2009049791A3 PCT/EP2008/008439 EP2008008439W WO2009049791A3 WO 2009049791 A3 WO2009049791 A3 WO 2009049791A3 EP 2008008439 W EP2008008439 W EP 2008008439W WO 2009049791 A3 WO2009049791 A3 WO 2009049791A3
Authority
WO
WIPO (PCT)
Prior art keywords
radiolabeled
nk3r
receptor antagonist
compound
antagonist
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.)
Ceased
Application number
PCT/EP2008/008439
Other languages
French (fr)
Other versions
WO2009049791A2 (en
Inventor
Caterina Bissantz
Parichehr Malherbe
Claus Riemer
Will Spooren
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.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
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
Application filed by F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of WO2009049791A2 publication Critical patent/WO2009049791A2/en
Publication of WO2009049791A3 publication Critical patent/WO2009049791A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/50—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 4
    • C07D215/52—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 4 with aryl radicals attached in position 2

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The present invention relates to a radiolabeled Neurokinin 3 receptor antagonist of the general formula (I) wherein R1 is a radiolabeled lower alkyl and a method for identifying a compound that can bind to a NK3R comprising a) contacting a compound of interest with a sample comprising the NK3R in the presence of the radiolabeled NK3R antagonist of any one of claims 1 to 3; and b) monitoring whether the compound of interest influences the binding of said radiolabeled NK3R antagonist to said NK3R. Furthermore, the present invention relates also to a mutant NK3R and uses thereof.
PCT/EP2008/008439 2007-10-15 2008-10-07 Radiolabeled nk3 receptor antagonist Ceased WO2009049791A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP07118495 2007-10-15
EP07118495.6 2007-10-15

Publications (2)

Publication Number Publication Date
WO2009049791A2 WO2009049791A2 (en) 2009-04-23
WO2009049791A3 true WO2009049791A3 (en) 2009-09-03

Family

ID=40159548

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2008/008439 Ceased WO2009049791A2 (en) 2007-10-15 2008-10-07 Radiolabeled nk3 receptor antagonist

Country Status (1)

Country Link
WO (1) WO2009049791A2 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201315846D0 (en) 2013-09-05 2013-10-23 Imp Innovations Ltd Method for treating or preventing hot flushes

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0940391A2 (en) * 1994-05-27 1999-09-08 Smithkline Beecham Farmaceutici S.p.A. Quinoline derivatives as tachykinin NK3 receptor antagonists

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0940391A2 (en) * 1994-05-27 1999-09-08 Smithkline Beecham Farmaceutici S.p.A. Quinoline derivatives as tachykinin NK3 receptor antagonists

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
BENNACEF IDRISS ET AL: "Functionalization through lithiation of (S)-N-(1-phenylpropyl)-2-phen ylquinoline-4-carboxamide. Application to the labeling with carbon-11 of NK-3 receptor antagonist SB 222200.", THE JOURNAL OF ORGANIC CHEMISTRY 16 MAR 2007, vol. 72, no. 6, 16 March 2007 (2007-03-16), pages 2161 - 2165, XP002509397, ISSN: 0022-3263 *
GIARDINA G A M ET AL: "DISCOVERY OF A NOVEL CLASS OF SELECTIVE NON-PEPTIDE ANTAGONISTS FOR THE HUMAN NEUROKININ-3 RECEPTOR. 2. IDENTIFICATION OF (S)-N- (1-PHENYLPROPYL)-3-HYDROXY-2-PHENYLQUINOLINE-4-CARBOXAMIDE (SB 223412)", JOURNAL OF MEDICINAL CHEMISTRY, US AMERICAN CHEMICAL SOCIETY. WASHINGTON, vol. 42, no. 6, 1 January 1999 (1999-01-01), pages 1053 - 1065, XP000882756, ISSN: 0022-2623 *
MALHERBE P ET AL: "Me-talnetant and osanetant interact within overlapping but not identical binding pockets in the human tachykinin neurokinin 3 receptor transmembrane domains", MOLECULAR PHARMACOLOGY, BALTIMORE, MD, US, vol. 73, no. 6, 1 June 2008 (2008-06-01), pages 1736 - 1750, XP009110370, ISSN: 0026-895X *
PERRIO C., GOURAND F., KERVERDO S., BARRE L.: "Synthesis of [18]F-fluoroquinolines for the labelling of a talnetant analogue as NK3-receptor ligand", J. LABEL. COMPD. RADIOPHARM., vol. 48, no. S1, 2005, pages S150, XP002509396 *
SMITH P W ET AL: "Neurokinin 3 (NK3) receptor modulators for the treatment of psychiatric disorders", RECENT PATENTS ON CNS DRUG DISCOVERY 200801 GB, vol. 3, no. 1, January 2008 (2008-01-01), pages 1 - 15, XP002509793, ISSN: 1574-8898 *
WU L H ET AL: "Identification of Methionine 134 and Alanine 146 in the Second Transmembrane Segment of the Human Tachykinin NK3 Receptor as Residues Involved in Species-Selective Binding to SR 48968", BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, ACADEMIC PRESS INC. ORLANDO, FL, US, vol. 198, no. 3, 14 February 1994 (1994-02-14), pages 961 - 966, XP024766519, ISSN: 0006-291X, [retrieved on 19940214] *

Also Published As

Publication number Publication date
WO2009049791A2 (en) 2009-04-23

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