169883-31-2

Upstream product

• 288-32-4 1H-imidazole 
• 169883-22-1 2-(N-(2-bromo-4-isopropylphenyl)-N-ethyl)-6-methyl-4-(methanesulfonyloxy-methyl)pyrimidin-2-amine 
• 51605-97-1 2-bromo-4-isopropylaniline 
• 169880-48-2 methyl 2-((2-bromo-4-(1-methylethyl)phenyl)ethylamino)-6-methyl-4-pyrimidinecarboxylate 
• 257615-17-1 2-(N-(2-bromo-4-(2-propyl)phenyl)amino)-4-carbomethoxy-6-methylpyrimidinamine 
• 89793-11-3 methyl 2-chloro-6-methylpyrimidine-4-carboxylate 

Downstream Products

• 169883-22-1 2-(N-(2-bromo-4-isopropylphenyl)-N-ethyl)-6-methyl-4-(methanesulfonyloxy-methyl)pyrimidin-2-amine 

Relevant academic research and scientific papers

1N-ALKYL-N-ARYLPYRIMIDINAMINES AND DERIVATIVES THEREOF

The present invention provides novel compounds, compounds and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsy, irritable bowel syndrome, immune suppression, Alzheimer'disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: wherein R 1, R 3, R 4, R 5, Z, Y, V, X, X', J, K, L, and M are as defined herein.

1N-alkyl-N-arylpyrimidinamines and derivatives thereof

The present invention provides novel compounds, compounds and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsy, irritable bowel syndrome, immune suppression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: wherein R1, R3, R4, R5, Z, Y, V, X, X', J, K, L, and M are as defined herein.

Structure-activity studies on 4-substituted-2-anilinopyrimidine corticotropin releasing factor (CRF) antagonists

Structure-activity studies around the 4-position of 2-anilinopyrimidine corticotropin releasing factor (CRF) antagonists suggest that there is a large lipophilic cavity in the rat CRF receptor, which can accommodate a wide variety of substituents at this position in contrast to the steric constraints observed for other positions on the 2-anilinopyrimidine core. The chemical syntheses and biological activities of 2-anilinopyrimidine CRF antagonists with carbon-linked substituents at the 4-position are reported. Significant improvements in rat pharmacokinetic parameters were achieved relative to those for the lead structure. While the lead compound 1 (rCRF K(i) = 44 nM) afforded no detectable rat plasma levels after intraperitoneal (ip) or oral (po) dosing, compounds 3-3 (rCRF K(i) = 16 nM) and 3-4 (rCRF K(i) = 59 nM) gave high rat plasma levels at 30 mg/kg (ip, po) (C(max) = 1389 nM and 8581 nM (ip) respectively; C(max) = 113 nM and 988 nM (po), respectively). Furthermore 3-3 and 3-4 had superior bioavailabilities at these doses (59 and 46% (ip), respectively; 2 and 10% (po), respectively). (C) 1999 DuPont Pharmaceuticals Company.