836684-71-0

Upstream product

• 21667-60-7 3-methoxybenzoylacetonitrile 
• 864131-95-3 N,N'-diphenylformamidine 
• 586-38-9 3-Methoxybenzoic acid 
• 5368-81-0 methyl 3-methoxybenzoate 

Downstream Products

• 836684-72-1 3-[5-amino-4-(3-methoxybenzoyl)-pyrazol-1-yl]-4-methyl-benzoic acid 
• 1044590-54-6 [5-amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]{3-[(R)-(2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]phenyl}ketone 
• 249936-55-8 [14C]-Ro 3201195 
• 249937-13-1 [5-amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]-(3-hydroxyphenyl)methanone 
• 1044590-49-9 C₁₇H₁₀F₅N₃O₂ 
• 1044590-47-7 C₁₂H₁₃N₃O₂ 
• 1044590-43-3 C₁₇H₁₄N₄O₄ 
• 1032826-48-4 C₁₇H₁₃F₂N₃O₂ 

Relevant academic research and scientific papers

The effect of RO3201195 and a pyrazolyl ketone P38 MAPK inhibitor library on the proliferation of Werner syndrome cells

Microwave-assisted synthesis of the pyrazolyl ketone p38 MAPK inhibitor RO3201195 in 7 steps and 15% overall yield, and the comparison of its effect upon the proliferation of Werner Syndrome cells with a library of pyrazolyl ketones, strengthens the evidence that p38 MAPK inhibition plays a critical role in modulating premature cellular senescence in this progeroid syndrome and the reversal of accelerated ageing observed in vitro on treatment with SB203580.

KINASE MODULATORS FOR THE TREATMENT OF CANCER

A method of treating cancer in which a compound that inhibits the expression, production or release of IL-10 by immune cells is combined with a compound that stimulates the production of IL-12 when given in combination with, or in the presence of TNFa. Sa

Microwave-assisted synthesis of 5-aminopyrazol-4-yl ketones and the p38MAPK inhibitor RO3201195 for study in Werner syndrome cells

5-Aminopyrazol-4-yl ketones are prepared rapidly and efficiently using microwave dielectric heating from β-ketonitriles by treatment with N,N′-diphenylformamidine followed by heterocyclocondensation by irradiation with a hydrazine. The inhibitory activity of RO3201195 prepared by this methodology was confirmed in hTERT-immortalized HCA2 and WS dermal fibroblasts at 200 nM concentration, both by ELISA and immunoblot assay, and displays excellent kinase selectivity for p38α MAPK over the related stress-activated kinase JNK.

2-(HETERO-)ARYL,4-CARBONYL SUBSTITUTED PYRAZOLE DERIVATIVES AS INHIBITORS OF P38 MITOGEN-ACTIVATED PROTEIN KINASE

Compounds of formula (I) are inhibitors of p38 MAP kinase activity, and are useful in the treatment of, inter alia, inflammatory and autoimmune disease wherein Ring A is aryl, heteroaryl or heterocyclyl of 5-13 atoms; Ring B is optionally substituted aryl or heteroaryl of 5-13 atoms; Z is (a) a radical of formula -(CH2)z-X1-L1-Y- NHCHR1R2 or (b) a radical of formula -(CH2)z-Y1-L1-R wherein R1R2CHNH- and R are respectively N- and C-linked amino acid or amino acid ester groups as defined in the description, and -Y-L1-X1-(CH2)z- and -L1-Y1-(CH2)z- are linker radicals as defined in the description; R7 is hydrogen or -C(=O)R' where R' is hydrogen, (C1-C6)alkyl, (C3-C6)cycloalkyl or (C1-C6)haloalkyl; R8 is hydrogen or (C1C6)alkyl; R9 is hydrogen, halogen, hydroxyl, (C1-C6)alkoxy, (C1-C6)alkyl; R18 is hydrogen, halogen, hydroxyl, (C1C6)alkoxy (C1-C6)alkyl, - NRaRb where Ra and Rb are hydrogen or (C1-C6)alkyl, or optionally substituted aryl, heteroaryl or heterocyclyl or Ra and Rb when taken together with the nitrogen to which they are attached form a cyclic amino group of up to 6 ring atoms; R19 is hydrogen, halogen, (C1C6)alkoxy, or (C1C6)alkyl.

5-MEMBERED HETEROCYCLE-BASED P38 KINASE INHIBITORS

Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38α and p38β kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of u