37801-55-1

Upstream product

• 3528-51-6 1-benzyl-1H-pyrazol-5-amine 
• 87-13-8 diethyl 2-ethoxymethylenemalonate 
• 37799-73-8 1-Benzyl-5-(2,2-bis-ethoxycarbonyl-vinyl-amino)pyrazol 

Downstream Products

• 1224047-93-1 C₂₆H₂₂ClN₅O₂ 
• 1340592-19-9 1-benzyl-4-(4-fluoro-2-methyl-phenyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid ethyl ester 
• 1340591-83-4 N-[1-benzyl-4-(4-fluoro-2-methyl-phenyl)-1H-pyrazolo[3,4-b]pyridin-5-yl]-2-(3,5-bis-trifluoromethyl-phenyl)-N-methyl-isobutyramide 
• 1340592-00-8 2-(3,5-bis-trifluoromethyl-phenyl)-N-[4-(4-fluoro-2-methyl-phenyl)-1H-pyrazolo[3,4-b]pyridin-5-yl]-N-methyl-isobutyramide 
• 1340592-20-2 [1-Benzyl-4-(4-fluoro-2-methyl-phenyl)-1H-pyrazolo[3,4-b]pyridin-5-yl]-carbamic acid tert-butyl ester 
• 1340591-78-7 2-(3,5-bis-trifluoromethylphenyl)-N-[1-(2,2-difluoroethyl)-4-(4-fluoro-2-methylphenyl)-1H-pyrazolo[3,4-b]pyridin-5-yl]-N-methylisobutyramide 
• 1340592-21-3 C₂₁H₁₆FN₃O₂ 
• 1340592-22-4 [1-benzyl-4-(4-fluoro-2-methyl-phenyl)-1H-pyrazolo[3,4-b]pyridin-5-yl]-methyl-amine 

Relevant academic research and scientific papers

PYRRAZOLOPYRIDINE DERIVATIVES

The present invention relates to a compound of formula (I), wherein R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, benzyl, -C(0)-lower alkyl, -C(0)-CH2-lower alkoxy, -C(0)-C3-6-cycloalkyl, -(CH2)°-C(0)-NR,R', -(CH2)°S(0)2- lower alkyl or -S(0)2-NR,R'; o is 0 or 1; R,R' are independently from each other hydrogen or lower alkyl, or may form together with the N atom to which they are attached a 5 or 6 membered heterocycloalkyl ring; R2 is hydrogen or lower alkyl; R3 is halogen, lower alkoxy, lower alkyl substituted by halogen or lower alkoxy substituted by halogen; and may be the same or different in case n is 2; n is 1 or 2; Ar is phenyl optionally substituted by one or two substituents selected from lower alkyl, halogen, lower alkoxy, lower alkyl substituted by hydroxy or cyano, or is a five or six membered heteroaryl group, selected from thiophenyl or pyridinyl which are optionally substituted by lower alkyl or halogen; or to a pharmaceutically active acid addition salt. It has surprisingly been found that the compounds of formula I show a high affinity simultaneously to both the NK1 and the NK3 receptors (dual NK1/NK3 receptor antagonists), useful in the treatment of schizophrenia.

PYRRAZOLOPYRIDINE COMPOUNDS AS DUAL NK1/NK3 RECEPTOR ANTAGONISTS

The present invention relates to a compound of formula I wherein R1, R2, R3, Ar, and n are as defined herein or to a pharmaceutically active acid addition salt. Compounds of formula I show a high affinity simultaneously to

The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist

The identification of novel, potent, non-steroidal/small molecule functional GR antagonist GSK1564023A selective over PR is described. Associated structure-activity relationships and the process of optimisation of an initial HTS hit are also described.