39062-69-6

Upstream product

• 777-37-7 4-chloro-3-(trifluoromethyl)nitrobenzene 
• 100-51-6 benzyl alcohol 
• 400-74-8 2-Fluoro-5-nitrobenzotrifluoride 
• 20194-18-7 sodium phenyl-methanolate 
• 1548-61-4 4-nitro-2-(trifluoromethyl)phenol 
• 100-39-0 benzyl bromide 

Downstream Products

• 70338-47-5 3-(trifluoromethyl)-4-(benzyloxy)aniline 
• 288384-62-3 5-benzyloxy-2-nitro-4-(trifluoromethyl)phenylacetonitrile 
• 1535-76-8 4-amino-2-(trifluoromethyl)phenol 
• 82578-53-8 5-Benzyloxy-N-(4-benzyloxy-3-trifluormethylphenyl)anthranilsaeure 
• 76874-95-8 5,4'-Dihydroxyflufenaminsaeure 
• 39062-71-0 4'-Benzyloxy-flufenaminsaeure 
• 39062-72-1 4'-Hydroxyflufenaminsaeure 
• 231278-32-3 5-(4-(4-benzyloxy-3-trifluoromethylphenylamino)-quinazolin-6-yl)-furan-2-carbaldehyde 
• 231278-27-6 (6-iodo-(4-benzyloxy-3-trifluoromethyl-phenyl)-quinazolin-4-yl)amine 
• 70338-48-6 4'-(Benzyloxy)-3'-trifluoromethyl-1-methylcyclopropanecarboxanilide 

Relevant academic research and scientific papers

Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors

A pharmaceutical formulation comprising the compound of formula

PYRROLIDINE DERIVATIVES AS ERK INHIBITORS

Disclosed are the ERK inhibitors of Formula (1.0): and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of Formula (1.0).

Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series

Synthetic modifications on a 6-furanylquinazoline scaffold to optimize the dual ErbB-1/ErbB-2 tyrosine kinase inhibition afforded consistent SAR whereby a 4-(3-fluorobenzyloxy)-3-haloanilino provided the best enzyme potency and cellular selectivity. Changes made to the 6-furanyl group had little impact on the enzyme activity, but appeared to dramatically affect the cellular efficacy. The discovery of lapatinib emerged from this work.

BISARYLUREA DERIVATIVES

The present invention relates to bisarylurea derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.

QUINAZOLINE DERIVATIVES AS ANGIOGENESIS INHIBITORS

The invention relates to the use of compounds of the formula I: wherein ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which optionally may contain 1-3 heteroatoms selected independently from O, N and S; Z is -O-, -NH-, -S-, -CH2- or a direct bond; n is 0-5; m is 0-3; R represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3alkylsulphanyl, -NRR (wherein R and R, which may be the same or different, each represents hydrogen or C1-3alkyl), or RX- (wherein X and R are as defined herein; R represents hydrogen, oxo, halogeno, hydroxy, C1-4alkoxy, C1-4alkyl, C1-4alkoxymethyl, C1-4alkanoyl, C1-4haloalkyl, cyano, amino, C2-5alkenyl, C2-5alkynyl, C1-3alkanoyloxy, nitro, C1-4alkanoylamino, C1-4alkoxycarbonyl, C1-4alkylsulphanyl, C1-4alkylsulphinyl, C1-4alkylsulphonyl, carbamoyl, N-C1-4alkylcarbamoyl, N,N-di(C1-4alkyl)carbamoyl, aminosulphonyl, N-C1-4alkylaminosulphonyl, N,N-di(C1-4alkyl)aminosulphonyl, N-(C1-4alkylsulphonyl)amino, N-(C1-4alkylsulphonyl)-N-(C1-4alkyl)amino, N,N-di(C1-4alkylsulphonyl)amino, a C3-7alkylene chain joined to two ring C carbon atoms, C1-4alkanoylaminoC1-4alkyl, carboxy or a group RX (wherein X and R are as defined herein); and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and compounds of formula I. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

Synthesis and properties of nuclear hydroxylated derivatives of flufenamic acid and etofenamate

Synthesis of six nuclear hydroxylated derivatives of flufenamic acid and etofenamate (5-OH-, 4'-OH and 5,4'-(OH2) on a preparative scale is described. All compounds show low toxicity, by only weak anti-inflammatory activity in the rat paw kaolin edema test as compared to 2-(2-hydroxyethoxy)ethyl-N-(α,α,α-trifluoro-m-tolyl)-anthranilate (etofenamate, active substance of Rheumon Gel).

Cycloalkanecarboxanilide derivative herbicides

Certain cycloalkanecarboxanilide derivatives are useful as herbicides.