72775-83-8

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Uses

(3-Ethoxyphenyl)acetic acid

Upstream product

• 52600-91-6 1-(3-ethoxyphenyl)ethan-1-one 
• 139988-02-6 methyl 3-ethoxyphenylacetate 
• 621-37-4 m-hydroxyphenylacetic acid 
• 42058-59-3 3-hydroxy-benzeneacetic acid, methyl ester 

Downstream Products

• 106462-42-4 N-[2-(2,5-Dimethoxy-phenyl)-ethyl]-2-(3-ethoxy-phenyl)-acetamide 
• 373361-73-0 (3-Ethoxy-phenyl)-acetyl chloride 
• 188544-70-9 2-(3-ethoxyphenylacetylamino)benzamide 
• 1446490-45-4 N-(4-(4-bromophenyl)thiazol-2-yl)-2-(3,4-diethoxyphenyl)acetamide 
• 1446490-35-2 2-(3,4-diethoxyphenyl)-N-(4-phenylthiazol-2-yl)acetamide 
• 1344688-68-1 C₂₃H₂₉NO₆ 

Relevant academic research and scientific papers

Fragment based discovery of arginine isosteres through REPLACE: Towards non-ATP competitive CDK inhibitors

In order to develop non-ATP competitive CDK2/cyclin A inhibitors, the REPLACE strategy has been applied to generate fragment alternatives for the N-terminal tetrapeptide of the cyclin binding motif (HAKRRLIF) involved in substrate recruitment prior to phosphotransfer. The docking approach used for the prediction of small molecule mimics for peptide determinants was validated through reproduction of experimental binding modes of known inhibitors and provides useful information for evaluating binding to protein-protein interaction sites. Further to this, potential arginine isosteres predicted using the validated LigandFit docking method were ligated to the truncated C-terminal peptide, RLIF using solid phase synthesis and evaluated in a competitive binding assay. After testing, identified fragments were shown to represent not only appropriate mimics for a critical arginine residue but also to interact effectively with a minor hydrophobic pocket present in the binding groove. Further evaluation of binding modes was undertaken to optimize the potency of these compounds. Through further application of the REPLACE strategy in this study, peptide-small molecule hybrid CDK2 inhibitors were identified that are more drug-like and suitable for further optimization as anti-tumor therapeutics.

COMPOSITIONS USEFUL AS INHIBITORS OF ROCK AND OTHER PROTEIN KINASES

The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

AZAINDOLES USEFUL AS INHIBITORS OF ROCK AND OTHER PROTEIN KINASES

The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

COMPOSITIONS USEFUL AS INHIBITORS OF ROCK AND OTHER PROTEIN KINASES

The present invention relates to substitute thiazole and thiophene derivatives useful as inhibitors of rock and other protein kinaeses. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders, including proliferative, cardiac and neurodegenerative diseases.

Pharmaceutically active benzoquinazoline compounds

Compounds of formula (I) or salts thereof, wherein the dotted line represents a single or double bond, R1is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group; R2, R3, R4and R5are the same or different and each is selected from hydrogen, phenyl, halo, nitro, a group S(O)nR8wherein n is the integer 0, 1 or 2 and R8is halo or alkyl or a group NR9R10wherein R9and R10are both hydrogen, a group NR11R12wherein R11and R12are the same or different and each is hydrogen or alkyl, a group OR13wherein R13is hydrogen or C1-4alkyl optionally substituted by halo; a C1-4aliphatic group optionally substituted by a group OR14or NR14R15wherein R14and R15are the same or different and each is hydrogen or alkyl; or two of R2to R5are linked together to form a benzo group, or one of R2to R5is a group -X-Y-R16wherein X is CH2, NR17, CO or S(O)m, and Y is CH2, NR17, O, or S(O)m, or -X-Y- is a group -O-, -NR17-, -CH=CH- or -N=N-, are disclosed as pharmacological agents useful in the treatment of tumours. Pharmaceutical compositions and methods for the preparation of compounds of formula (I) are also described.

Quaternary ammonium salts of aromatic amine compounds, their preparation and pharmaceutical compositions in which they are present

The present invention relates to quaternary ammonium salts of the formula STR1 in which: J is either a group Ar--CXX''--CX"" or a group Ar--(CH 2) x CH 1, in which:Ar is a substituted or unsubstituted phenyl, a cycloalkyl, a pyridyl or a thienyl;X is hydrogen;X'' is hydrogen or is combined with X"" below to form a carbon-carbon bond, or else X and X'' together form an oxo group;X"" is hydrogen or forms a carbon-carbon bond with X'';X is zero or one; andX 1 is hydrogen (n=0), a hydroxyl, an alkoxy, an acyloxy, a carboxyl, a carbalkoxy, a cyano or an alkoxyamino group;Q is an alkyl group or a benzyl group;A is an anion;m is 2 or 3;Ar'', R, T and Z are as defined in the specification, are neurokinin receptor antagonists.

PHARMACEUTICAL COMPOUNDS

The present invention relates to novel benzoquinazoline thymidylate synthase inhibitors, to pharmaceutical formulations containing them and to their use in medicine

Benzoquinazoline inhibitors of thymidylate synthase: Enzyme inhibitory activity and cytotoxicity of some 3-amino- and 3-methylbenzo[f]quinazolin- 1(2H)-ones

The synthesis and thymidylate synthase (TS) inhibitory activity of a series of simple benzo[f]-quinazolin-1(2H)-ones are described. Fully aromatic 3-amino compounds with compact lipophilic substituents in the 9-position were found to have I50 values as low as 20 nM on the isolated enzyme, and represent the first examples of potent, folate-based TS inhibitors that completely lack any structural feature corresponding to the (p- aminobenzoyl)glutamate moiety of the cofactor. A number of the compounds also showed moderate growth inhibitory activity against a human colon adenocarcinoma cell line (SW480), with IC50 values as low as 2 μM.