Arylpyrimidine compounds are provided that can act as selective modulators of CRF receptors. 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 treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention 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.
Taeyoung Yoon - Guilford CT, US Ping Ge - Durham CT, US Raymond Horvath - Guilford CT, US Stephane DeLombaert - Madison CT, US Kevin Hodgetts - Killingworth CT, US Dario Doller - Wallingford CT, US Cunyu Zhang - Morrisville NC, US
Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRFreceptors, including human CRFreceptors. The invention thus includes methods for treatment of disorders and diseases associated with CRFreceptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.
Benzimidazole And Indole Derivatives As Crf Receptor Modulators
Benzimidazole and indole derivatives that act as selective modulators of CRF 1 receptors are provided. 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 treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention 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.
Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators of CRF receptors. The 5-substituted-2-arylpyrazine compounds provided herein are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds provided 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.
Taeyoung Yoon - Guilford CT, US Ping Ge - Durham CT, US Raymond Horvath - Guilford CT, US Stephane DeLombaert - Madison CT, US Kevin Hodgetts - Killingworth CT, US Dario Doller - Wallingford CT, US Cunyu Zhang - Morrisville NC, US
International Classification:
A61K031/4965 C07D239/02
US Classification:
514252100, 514255060, 544334000, 544406000
Abstract:
Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRFreceptors, including human CRFreceptors. The invention thus includes methods for treatment of disorders and diseases associated with CRFreceptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.
Carboxylic Acid, Phosphate Or Phosphonate Substituted Quinazolin-4-Ylamine Analogues As Capsaicin Receptor Modulators
Rajagopal Bakthavatchalam - Madison CT, US Charles Blum - Westbrook CT, US Harry Brielmann - Guilford CT, US Timothy Caldwell - Guilford CT, US Stephane DeLombaert - Madison CT, US Kevin Hodgetts - Killingworth CT, US Xiaozhang Zheng - Branford CT, US
Acid-substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
Rajagopal Bakthavatchalam - Madison CT, US Charles Blum - Westbrook CT, US Harry Brielmann - Guilford CT, US James Darrow - Wallingford CT, US Stephane DeLombaert - Madison CT, US Taeyoung Yoon - Newton MA, US Xiaozhang Zheng - Branford CT, US
Substituted biphenyl-4-carboxylic acid arylamide analogues capable of modulating receptor activity, are provided. Such ligands may be used to modulate receptor activity in vivo or in vitro, and are particularly useful in the treatment of pain and other conditions associated with receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for receptor localization studies.
Taeyoung Yoon - Guilford CT, US Ping Ge - Durham CT, US Raymond Horvath - Guilford CT, US Stephane DeLombaert - Madison CT, US Kevin Hodgetts - Killingworth CT, US Dario Doller - Wallingford CT, US Cunyu Zhang - Morrisville NC, US
Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRFreceptors, including human CRFreceptors. The invention thus includes methods for treatment of disorders and diseases associated with CRFreceptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.