403660-57-1

Upstream product

• 53857-57-1 5-bromo-1H-indazole 
• 1066-54-2 trimethylsilylacetylene 
• 55919-82-9 5-iodo-1H-indazole 
• 13194-68-8 4-iodo-2-methylaniline 
• 850363-46-1 1-acetyl-5-iodo-1H-indazole 
• 1001907-23-8 tert-butyl 5-iodo-1H-indazole-1-carboxylate 
• 1093847-82-5 5-[2-(trimethylsilyl)ethynyl]-1H-indazole 
• 651780-02-8 tert-butyl 5-bromo-1H-indazole-1-carboxylate 
• 1093306-78-5 tert-butyl 5-((trimethylsilyl)ethynyl)-1H-indazole-1-carboxylate 

Downstream Products

• 1093302-41-0 5-[1-(2-methylbenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole 
• 1093303-14-0 5-(3-benzylisoxazol-5-yl)-1H-indazole 
• 1093302-40-9 5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazole 
• 1093302-38-5 5-(1-benzyl-1H-1,2,3-triazol-5-yl)-1H-indazole 
• 1093303-55-9 5-[4-(2-phenylethyl)-1H-1,2,3-triazol-1-yl]-1H-indazole 
• 1093303-56-0 5-[4-(cyclohexylmethyl)-1H-1,2,3-triazol-1-yl]-1H-indazole 
• 1093303-32-2 5-(4-benzyl-1H-1,2,3-triazol-1-yl)-1H-indazole 
• 1093303-61-7 5-[4-(3-phenylpropyl)-1H-1,2,3-triazol-1-yl]-1H-indazole 
• 1093302-68-1 5-[1-(2,3-dichlorobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole 
• 1093302-70-5 5-[1-(2,5-dichlorobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole 
• 1093302-48-7 5-[1-(2-chlorobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole 
• 1093302-45-4 5-[1-(2-fluorobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole 
• 1093302-71-6 5-[1-(3,5-dichlorobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole 
• 1093302-49-8 5-[1-(3-chlorobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole 

Relevant academic research and scientific papers

INHIBITORS OF FIBROBLAST GROWTH FACTOR RECEPTOR KINASES

Provided herein are heteroaryl inhibitors of fibroblast growth factor receptor kinases, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.

The impact of binding site waters on the activity/selectivity trade-off of Janus kinase 2 (JAK2) inhibitors

Structure based optimization of B39, an indazole-based low micromolar JAK2 virtual screening hit is reported. Analysing the effect of certain modifications on the activity and selectivity of the analogues suggested that these parameters are influenced by

PYRROLIDINE DERIVATIVES AND THEIR USE AS COMPLEMENT PATHWAY MODULATORS

The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as complement pathway modulators for the treatment of ocular diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl) benzamide derivatives as potent pan Bcr-Abl inhibitors including the threonine315←isoleucine315 mutant

A series of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives were designed and synthesized as new Bcr-Abl inhibitors by using combinational strategies of bioisosteric replacement, scaffold hopping, and conformational constraint. The compounds displayed significant inhibition against a broad spectrum of Bcr-Abl mutants including the gatekeeper T315I and p-loop mutations, which are associated with disease progression in CML. The most potent compounds 6q and 6qo strongly inhibited the kinase activities of Bcr-AblWT and Bcr-AblT315I with IC50 values of 0.60, 0.36 and 1.12, 0.98 nM, respectively. They also potently suppressed the proliferation of K562, KU812 human CML cells, and a panel of murine Ba/F3 cells ectopically expressing either Bcr-AblWT or any of a panel of other Bcr-Abl mutants that have been shown to contribute to clinical acquired resistance, including Bcr-AblT315I, with IC50 values in low nanomolar ranges. These compounds may serve as lead compounds for further development of new Bcr-Abl inhibitors capable of overcoming clinical acquired resistance against imatinib.

Scaffold oriented synthesis. Part 3: Design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions

We report the synthesis and biological evaluation of 5-substituted indazoles and amino indazoles as kinase inhibitors. The compounds were synthesized in a parallel synthesis fashion from readily available starting materials employing [2+3] cycloaddition r

HETEROCYCLIC MODULATORS OF PKB

The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein Formula (I). The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

5-HETEROARYL SUBSTITUTED INDAZOLES AS KINASE INHIBITORS

The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.

ALKYNYLPYRIMIDINES AS TIE2 KINASE INHIBITORS

The invention relates to alkynylpyrimidines according to the general formula (I) in which A, R1, R2, R3, R4, R5, and R6 are as defined in the claims, to pharmaceutical compositions comprising said alkynylpyrimidines, to methods of preparing said alkynylpyrimidines, as well as to uses thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 and VEGFR2 signalling.