Title:
放射能標識付きキノリンおよびキノリノン誘導体および代謝向性グルタメート受容体リガンドとしてのそれらの使用
Document Type and Number:
Japanese Patent JP4573533
Kind Code:
B2
Abstract:
The present invention is concerned with radiolabelled quinoline and quinolinone derivatives according Formula (I-A)* or (I-B)* showing metabotropic glutamate receptor antagonistic activity, in particular mGlu1 receptor activity, and their preparation; it further relates to compositions comprising them, as well as their use for marking and identifying metabotropic glutamate receptor sites and for imaging an organ. In a preferable embodiment, X represents O; R1 represents C1-6alkyl; cycloC3-12alkyl or (cycloC3-12alkyl)C1-6alkyl, wherein one or more hydrogen atoms in a C1-6alkyl-moiety or in a cycloC3-12alkyl-moiety optionally may be replaced by C1-6alkyloxy, aryl, halo or thienyl; R2 represents hydrogen; halo; C1-6alkyl or amino; R3 and R4 each independently represent hydrogen or C1-6alkyl; or R2 and R3 may be taken together to form -R2-R3-, which represents a bivalent radical of formula -Z4-CH2-CH2-CH2- or -Z4-CH2-CH2- with Z4 being O or NR11 wherein R11 is C1-6alkyl; and wherein each bivalent radical is optionally substituted with C1-6alkyl; or R3 and R4 may be taken together to form a bivalent radical of formula -CH2-CH2-CH2-CH2-; R5 represents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo. Most preferred are radiolabelled compounds in which the radioactive isotope is selected from the group of of 3H, 11C and 18F. The invention also relates to their use in a diagnostic method, in particular for marking and identifying a mGluR1 receptor in biological material, as well as to their use for imaging an organ, in particular using PET.
Inventors:
Roussaille, Anne Simone Giosephine
Bissyoff, Francois Paul
Cornelus Geraldus Maria, Janssen
Labraisen, Hilde
Bissyoff, Francois Paul
Cornelus Geraldus Maria, Janssen
Labraisen, Hilde
Application Number:
JP2003579882A
Publication Date:
November 04, 2010
Filing Date:
March 26, 2003
Export Citation:
Assignee:
JANSSEN PHARMACEUTICA NAAMLOZE VENNOOTSCHAP
International Classes:
C07D215/06; A61K31/47; A61K31/4704; A61K31/4709; A61K31/473; A61K31/4741; A61K31/4743; A61K31/4745; A61K31/496; A61K31/497; A61K31/506; A61K31/5377; A61K31/541; A61K51/00; A61K51/04; A61P3/08; A61P9/10; A61P25/00; A61P25/02; A61P25/04; A61P25/08; A61P25/14; A61P25/16; A61P25/18; A61P25/22; A61P25/24; A61P25/28; A61P25/30; A61P31/18; A61P43/00; C07D215/14; C07D215/18; C07D215/22; C07D215/26; C07D215/36; C07D215/38; C07D215/48; C07D215/50; C07D215/54; C07D215/60; C07D219/02; C07D221/10; C07D221/12; C07D221/16; C07D401/04; C07D401/06; C07D401/12; C07D405/04; C07D405/06; C07D405/12; C07D409/04; C07D409/06; C07D409/12; C07D413/12; C07D417/04; C07D453/06; C07D471/04; C07D491/048; C07D491/052; C07D495/04; C07D519/00
Domestic Patent References:
| JP55066560A | ||||
| JP7033743A | ||||
| JP57192366A | ||||
| JP59181275A | ||||
| JP2097957A | ||||
| JP8295690A | ||||
| JP8511004A | ||||
| JP1316356A | ||||
| JP2000169450A |
Foreign References:
| WO2000012498A1 | ||||
| WO2000039082A1 | ||||
| WO2000047574A1 | ||||
| GB1013224B | ||||
| US4348398 | ||||
| US2526232 | ||||
| WO2001066143A1 | ||||
| WO1999026927A1 | ||||
| WO1996005818A1 |
Other References:
Chemische Berichte,1960年,93,593-8
Canadian Journal of Chemistry,1971年,49(22),3765-6
Pharmaceutica Acta Helvetiae,1970年,45,198-202
Polymer,2001年,42(8),3323-3332
JOURNAL OF NEUROCHEMISTRY,2000年,vol.75, No.6,2590-2601
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,1996年,vol.6, No.5,499-504
Canadian Journal of Chemistry,1971年,49(22),3765-6
Pharmaceutica Acta Helvetiae,1970年,45,198-202
Polymer,2001年,42(8),3323-3332
JOURNAL OF NEUROCHEMISTRY,2000年,vol.75, No.6,2590-2601
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,1996年,vol.6, No.5,499-504
Attorney, Agent or Firm:
Patent business corporation Odashima patent office