Title:
CRF1受容体モジュレータとしての2,5-ジアリールピラジン、2,5-ジアリールピリジンおよび2,5-ジアリールピリミジン
Document Type and Number:
Japanese Patent JP2005500286
Kind Code:
A
Abstract:
Diarylpyrimidine compounds of Formula I are provided, wherein. or a pharmaceutically acceptable salt thereof, wherein: Ar1 and Ar2 are independently chosen from: phenyl which is mono-, di-, or tri-substituted, 1-naphthyl and 2-naphthyl, each of which is optionally mono-, di-, or tri-substituted, and optionally mono-, di-, or tri-substituted heteroaryl, said heteroaryl having from 1 to 3 rings, 5 to 7 ring members in each ring and, in at least one of said rings, from 1 to about 3 heteroatoms selected from the group consisting of N, O, and S; R is oxygen or absent; Z2 is CR2; Z3 is nitrogen; R1 and R2 are independently chosen from hydrogen, halogen, amino, cyano, nitro, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted mono- or di-alkylamino, optionally substituted cycloalkyl, optionally substituted (cycloalkyl)alkyl, optionally substituted (cycloalkyl)oxy, optionally substituted (cycloalkyl)alkoxy, optionally substituted alkylthio, optionally substituted alkylsulfinyl, optionally substituted alkylsulfonyl, and optionally substituted mono- or dialkylcarboxamide; with the proviso that not all of R1, R3, and R4 are hydrogen. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatments of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of Formula I are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
Inventors:
Juan Guang Hua
Hodgets Kevin
Dolla Dario
Geping
Yasufumi Yamaguchi
Hodgets Kevin
Dolla Dario
Geping
Yasufumi Yamaguchi
Application Number:
JP2003503606A
Publication Date:
January 06, 2005
Filing Date:
May 22, 2002
Export Citation:
Assignee:
Neurogen Corporation
International Classes:
A61K31/00; A61K31/44; A61K31/4439; A61K31/495; A61K31/496; A61K31/4965; A61K31/497; A61K31/505; A61K31/5377; A61K51/04; A61P1/04; A61P25/00; A61P25/22; A61P25/24; A61P43/00; C07D213/74; C07D239/34; C07D241/12; G01N33/566; C07D401/04; C07D403/04; C07D405/10; G01N33/58; (IPC1-7): C07D239/34; A61K31/4439; A61K31/496; A61K31/4965; A61K31/497; A61K31/505; A61K31/5377; A61P1/04; A61P25/00; A61P25/22; A61P25/24; A61P43/00; C07D241/12; C07D401/04; C07D403/04; C07D405/10; G01N33/566; G01N33/58
Attorney, Agent or Firm:
Hatsushi Shimizu
Kazunori Hashimoto
Koichi Niimi
Kazunori Hashimoto
Koichi Niimi