869663-62-7

Upstream product

• 626-02-8 3-Iodophenol 
• 82560-12-1 3-tert-butyl-1H-pyrazole-5-amine 
• 725686-47-5 5-tert-butyl-2-(3-methoxyphenyl)-2H-pyrazol-3-ylamine 
• 59997-51-2 trimethylacetylacetonitrile 
• 56239-39-5 3-Benzyloxyphenylhydrazine 

Downstream Products

• 1443252-53-6 5-tert-butyl-2-[3-(2-morpholin-4-ylethoxy)phenyl]-2H-pyrazol-3-ylamine 
• 1443251-70-4 1-{5-tert-butyl-2-[3-(2-dimethylaminoethoxy)phenyl]-2H-pyrazol-3-yl}-3-[(1S,4R)-4-(3-isopropyl[1,2,4]triazolo[4,3-a]pyridin-6-yloxy)-1,2,3,4-tetrahydronaphthalen-1-yl]urea 
• 1443252-63-8 N-(3-tert-butyl-1-{3-[2-(dimethylamino)ethoxy]phenyl}-1H-pyrazol-5-yl)carbamic acid 2,2,2-trichloroethyl ester 
• 946050-88-0 5-tert-butyl-2-[3-(2-dimethylaminoethoxy)phenyl]-2H-pyrazol-3-ylamine 
• 1443240-87-6 1-{5-tert-butyl-2-[3-(2-dimethylamino-ethoxy)-phenyl]-2H-pyrazol-3-yl}-3-{(1S,4R)-4-[3-(cis-2,6-dimethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea formate salt 
• 1443245-35-9 methanesulfonic acid 2-{3-[3-tert-butyl-5-(3-{(1S,4R)-4-[3-((2S,6R)-2,6-dimethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-ureido)-pyrazol-1-yl]-phenoxy}-ethyl ester 
• 1443245-34-8 1-{5-tert-butyl-2-[3-(2-hydroxy-ethoxy)-phenyl]-2H-pyrazol-3-yl}-3-{(1S,4R)-4-[3-(cis-2,6-dimethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-c]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea 
• 1443245-33-7 1-(5-tert-butyl-2-{3-[2-(tetrahydro-pyran-2-yloxy)-ethoxy]-phenyl}-2H-pyrazol-3-yl)-3-{(1S,4R)-4-[3-(cis-2,6-dimethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea 
• 1443240-85-4 1-{5-tert-butyl-2-[3-(2-dimethylamino-ethoxy)-phenyl]-2H-pyrazol-3-yl}-3-{(1S,4R)-4-[3-((S)-2-methyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydronaphthalen-1-yl}-urea 
• 1443245-29-1 1-{5-tert-butyl-2-[3-(2-hydroxy-ethoxy)-phenyl]-2H-pyrazol-3-yl}-3-{(1S,4R)-4-[3-((S)-2-methyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a] pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphtalen-1-yl}-urea 
• 1443245-28-0 1-(5-tert-butyl-2-{3-[2-(tetrahydro-pyran-2-yloxy)-ethoxy]-phenyl}-2-pyrazol-3-yl)-3-{(1S,4R)-4-[3-((S)-2-methyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea 
• 1443240-11-6 1-{5-tert-butyl-2-[3-(2-hydroxy-ethoxy)-phenyl]-2H-pyrazol-3-yl}-3-{(1S,4R)-4-[3-((S)-1-methyl-pyrrolidin-2-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea 
• 1443243-64-8 1-(5-tert-butyl-2-{3-[2-(tetrahydro-pyran-2-yloxy)-ethoxy]-phenyl}-2H-pyrazol-3-yl)-3-{(1S,4R)-4-[3-((S)-1-methyl-pyrrolidin-2-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea 
• 1443243-63-7 methanesulfonic acid 2-[3-(3-tert-butyl-5-{3-[(1S,4R)-4-(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy)-1,2,3,4-tetrahydro-naphthalen-1-yl]-ureido}-pyrazol-1-yl)-phenoxy]-ethyl ester 

Relevant academic research and scientific papers

KINASE INHIBITORS

Disclosed are compounds having [1,2,4]triazolo[4,3-a]pyridine groups and pharmaceutically acceptable salts thereof. The compounds are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.

KINASE INHIBITORS

Compounds of formula (I) or a pharmaceutically acceptable salt thereof: formula (I) wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.

DERIVATIVES OF 4-HYDROXY-1,2,3,4-TETRAHYDRONAPHTALEN-1-YL UREA AND THEIR USE IN THE TREATMENT OF, INTER ALIA, DISEASES OF THE RESPIRATORY TRACT

Disclosed are compounds having [1,2,4]triazolo[4,3-a] pyridine groups and pharmaceutically acceptable salts thereof. The compounds are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.

Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease

This paper describes the identification and optimization of a novel series of DFG-out binding p38 inhibitors as inhaled agents for the treatment of chronic obstructive pulmonary disease. Structure based drug design and "inhalation by design" principles have been applied to the optimization of the lead series exemplied by compound 1a. Analogues have been designed to be potent and selective for p38, with an emphasis on slow enzyme dissociation kinetics to deliver prolonged lung p38 inhibition. Pharmacokinetic properties were tuned with high intrinsic clearance and low oral bioavailability in mind, to minimize systemic exposure and reduce systemically driven adverse events. High CYP mediated clearance and glucuronidation were targeted to achieve high intrinsic clearance coupled with multiple routes of clearance to minimize drug-drug interactions. Furthermore, pharmaceutical properties such as stability, crystallinity, and solubility were considered to ensure compatibility with a dry powder inhaler. 1ab (PF-03715455) was subsequently identified as a clinical candidate from this series with efficacy and safety profiles confirming its potential as an inhaled agent for the treatment of COPD.

UREA COMPOUNDS USEFUL IN THE TREATMENT OF CANCER

Pyrazole urea compounds, pharmaceutical compositions which contain them and methods for treating cancer using them.

Triazolopyridinylsulfanyl derivatives as p38 MAP kinase inhibitors

A compound of formula (I), or a pharmaceutically acceptable salt and/or solvate (including hydrate) thereof; and the use of a compound of formula (I) in the treatment of a TNF-mediated disease, disorder, or condition, or a p38-mediated disease, disorder, or condition, in particular the allergic and non-allergic airways diseases, more particularly obstructive or inflammatory airways diseases, preferably chronic obstructive pulmonary disease.