66955-75-7

Upstream product

• 501357-70-6 acetic acid-(2-bromo-4-cyanomethyl-anilide) 
• 1197-55-3 4-aminophenylacetic acid 
• 3544-25-0 p-aminophenylacetonitrile 
• 25025-06-3 N-(4-cyanomethyl-phenyl)-acetamide 
• 39552-81-3 methyl p-aminophenylacetate 
• 66956-60-3 (4-acetylamino-3-bromo-phenyl)-acetic acid 

Downstream Products

• 1878-67-7 3-Bromophenylacetic acid 
• 954424-79-4 2-(4-amino-3-bromo-phenyl)-N-(2-dimethylamino-ethyl)-acetamide 
• 1258845-86-1 2-(4-tert-butylbenzyl)-3-[2-(4-amino-3-bromophenyl)acetamido]propyl pivalate 
• 209809-20-1 4-amino-3-bromophenylacetic acid methyl ester 

Relevant academic research and scientific papers

Halogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin

As an extension of our analysis of the effect of halogenation on thiourea TRPV1 agonists, we have now modified selected 4-hydroxy(or 4-amino)-3- methoxyphenyl acetamide TRPV1 agonists by 5- or 6-halogenation on the aromatic A-region and evaluated them for potency for TRPV1 binding and regulation and for their pattern of agonism/antagonism (efficacy). Halogenation shifted the functional activity at TRPV1 toward antagonism with a greater extent of antagonism as the size of the halogen increased (I > Br > Cl), as previously observed for the thiourea series. The extent of antagonism was greater for halogenation at the 5-position than at the 6-position, in contrast to SAR for the thiourea series. In this series, compounds 55 and 75 showed the most potent antagonism, with Ki (ant) = 2.77 and 2.19 nM, respectively, on rTRPV1 expressed in Chinese hamster ovary cells. The compounds were thus ca. 40-60-fold more potent than 6′-iodononivamide.

INHIBITORS OF C-FMS KINASE

The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.

Pyrazol-1-ylphenylacetic acids

Pyrazol-1-ylphenylacetic acids of the formula STR1 wherein R1, R2 and R3 are the same or different and denote a hydrogen atom or a halogen atom, R4 denotes a hydrogen atom or an alkyl group, A B denotes a carbon-carbon single or double bond, and their salts are pharmacologically active and are useful as medicaments. Medicament compositions are produced therefrom. Their functional carboxylic acid derivatives and other new intermediates are used in their preparation.