1049809-53-1

Upstream product

• 110-91-8 morpholine 
• 1049809-75-7 3-(4-Chloro-3-iodo-phenyl)-1-(3-oxo-propyl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid tert-butyl ester 
• 1049809-74-6 3-(4-Chloro-3-iodo-phenyl)-1-(3-hydroxy-propyl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid tert-butyl ester 
• 1049809-51-9 3-(4-chloro-3-iodo-phenyl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]-pyridine-5-carboxylic acid tert-butyl ester 

Downstream Products

• 1049809-54-2 3-[4-Chloro-3-(4-chloro-phenylethynyl)-phenyl]-1-(3-morpholin-4-yl-propyl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid tert-butyl ester 
• 1049810-02-7 1-[4-({2-Chloro-5-[1-(3-morpholin-4-ylpropyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl}ethynyl)phenyl]-N-[(4-chlorophenyl)methyl]methanamine 
• 1049817-50-6 3-(4-chloro-3-((4-((((4-chlorophenyl)methyl)amino)methyl)phenyl)ethynyl)phenyl)-1-(3-morpholin-4-ylpropyl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide 
• 1049809-78-0 N-(4-chloro-benzyl)-N-(4-{2-chloro-5-[1-(3-morpholin-4-yl-propyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenylethynyl}-benzyl)-2,2,2-trifluoro-acetamide 
• 1049817-58-4 3-(4-Chloro-3-{[4-({[(4-chlorophenyl)methyl]amino}methyl)phenyl]ethynyl}phenyl)-N-methyl-1-(3-morpholin-4-ylpropyl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide 

Relevant academic research and scientific papers

Pyrazole-based arylalkyne Cathepsin S inhibitors. Part III: Modification of P4 region

Novel classes of tetrahydropyrido-pyrazole thioether amines and arylalkynes that display potency against human Cathepsin S have been previously reported. Here, key pharmacophoric elements of these two classes are merged, and SAR investigations of the P4 region are described, in conjunction with re-optimization of the P5 and P1/P1′/P3 regions. Identification of meta-substituted arylalkynes with good potency and improved solubility is described.

Pyrazole-based cathepsin S inhibitors with arylalkynes as P1 binding elements

A crystal structure of 1 bound to a Cys25Ser mutant of cathepsin S helped to elucidate the binding mode of a previously disclosed series of pyrazole-based CatS inhibitors and facilitated the design of a new class of arylalkyne analogs. Optimization of the

CARBON-LINKED TETRAHYDRO-PYRAZOLO-PYRIDINE MODULATORS OF CATHEPSIN S

Carbon-linked tetrahydro-pyrazolo-pyridine compounds are described, which are useful as cathepsin S modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by cathepsin S activity, such as psoriasis, pain, multiple sclerosis, atherosclerosis, and rheumatoid arthritis.