1049809-51-9

Upstream product

• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 
• 42860-04-8 4-chloro-3-iodobenzoic acid 
• 217807-98-2 4-morpholin-4-yl-3,6-dihydro-2H-pyridine-1-carboxylic acid ter-tbutyl ester 
• 42860-17-3 4-chloro-3-iodo-benzoyl chloride 

Downstream Products

• 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 
• 1049809-91-7 3-(4-chloro-3-iodo-phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo-[4,3-c]pyridine 
• 1049809-52-0 3-(4-Chloro-3-iodo-phenyl)-1-(2-cyano-ethyl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid tert-butyl ester 
• 1049811-09-7 (R)-3-(4-chloro-3-iodo-phenyl)-1-oxiranylmethyl-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid tert-butyl ester 
• 1215171-56-4 C₂₅H₃₄ClIN₄O₃ 
• 1215171-57-5 C₂₅H₃₄ClIN₄O₃ 
• 1049809-92-8 2-[3-(4-chloro-3-iodo-phenyl)-1,4,6,7-tetrahydro-pyrazolo-[4,3-c]pyridin-5-yl]-2-oxo-acetamide 
• 1049811-12-2 (S)-2-[3-(4-chloro-3-iodo-phenyl)-1-(2-hydroxy-3-thiomorpholin-4-yl-propyl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-oxo-acetamide 
• 1049811-59-7 2-(3-{4-Chloro-3-[(4-chloro-3-{[(phenylmethyl)amino]methyl}phenyl)ethynyl]phenyl}-1-{3-[(3S)-3-methylmorpholin-4-yl]propyl}-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-oxoacetamide 
• 1049811-08-6 (S)-2-[3-(4-Chloro-3-{4-[(4-chloro-benzylamino)-methyl]-phenylethynyl}-phenyl)-1-(2-hydroxy-3-thiomorpholin-4-yl-propyl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-oxo-acetamide 
• 1049811-10-0 (S)-3-(4-chloro-3-iodo-phenyl)-1-(2-hydroxy-3-thiomorpholin-4-yl-propyl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid tert-butyl ester 
• 1049809-93-9 2-{3-(4-chloro-3-iodo-phenyl)-1-[3-(3-methyl-morpholin-4-yl)-propyl]-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl}-2-oxo-acetamide 
• 1049809-89-3 2-{3-(4-chloro-3-{4-[(4-chloro-benzylamino)-methyl]-phenylethynyl}-phenyl)-1-[3-(3-methyl-morpholin-4-yl)-propyl]-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl}-2-oxo-acetamide 
• 1181359-24-9 2-{3-(4-chloro-3-{4-[(4-chloro-benzylamino)-methyl]-phenylethynyl}-phenyl)-1-[3-(3-methyl-morpholin-4-yl)-propyl]-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl}-2-oxo-acetamide L-tartrate 

Relevant academic research and scientific papers

Practical synthesis of a cathepsin S Inhibitor: Route identification, purification strategies, and serendipitous discovery of a crystalline salt form

Chemical Equation Presented A redox economical strategy resulted in a concise, modular synthesis of compound 1, a potent Cathepsin S inhibitor. Starting from three building blocks, crude drug substance was prepared, in a two-step sequence in high yield. Efficient purification of the crude drug substance was accomplished via the formation of an unusual monoethyl oxalate salt.

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

PROCESSES FOR THE PREPARATION OF CARBON-LINKED TETRAHYDRO-PYRAZOLO-PYRIDINE MODULATORS OF CATHEPSIN S

Method of making carbon-linked tetrahydro-pyrazolo-pyridine compounds of the following Formula (I) and pharmaceutically acceptable salts thereof: comprising reacting a compound of formula (IX): with a compound of formula (X): to form a compound of Formula

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.