59-07-4

Upstream product

• 59-06-3 methyl 4-acetamido-2-ethoxybenzoate 
• 2486-66-0 2-ethoxy-4-nitrobenzoic acid 
• 2486-55-7 methyl 2-ethoxy-4-acetamidobenzoate 
• 619-19-2 2-hydroxy-4-nitrobenzoic acid 
• 4136-97-4 methyl 4-aminosalicylate 
• 65-49-6 4-Aminosalicylic acid 
• 910572-96-2 2-ethoxy-4-nitro-benzoic acid ethyl ester 

Downstream Products

• 2486-68-2 4-acetylamino-2-ethoxy-benzoic acid 
• 100800-71-3 2-ethoxy-4-amino-benzoic acid-(2-dimethylamino-ethyl ester) 
• 316810-08-9 2-ethoxy-4-cyanobenzoic acid 
• 958227-62-8 4-[4-((1R,2S)-2-isopropylcarbamoyl-cyclopentylamino)-5-trifluoromethyl-pyrimidin-2-ylamino]-2-ethoxybenzoic acid 

Relevant academic research and scientific papers

Synthesis and evaluation of novel serotonin 4 receptor radiotracers for single photon emission computed tomography

Despite its implication in several physiological and pathological processes the serotonin subtype-4 receptor (5-HT4R) has seen limited effort for the development of radiolabeling agent especially concerning single photon emission computed tomography (SPECT). Bearing an ester function, the available ligands are rapidly susceptible to hydrolysis which limits their use in vivo. In this study the synthesis of iodinated benzamide and ketone analogs were described. Their affinity for the 5-HT4R and their lipophilicity were evaluated and the most promising derivatives were evaluated ex vivo for their binding to the receptor and for their ability to displace the reference ligand [125I]-SB207710.

New compounds

The present invention encompasses compounds of general formula (1) wherein R1, R2, R4, X, m, n and p are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.

4,4,5,5, Tetrasubstituted imidazolines

There is provided a compound of formula I and the pharmaceutically acceptable salts and esters thereof wherein X1, X2, R1, R2, R3, R4, R5 and R6 are herein described. The compounds exhibit activity as anticancer agents.

Cis-imidazolines

There are presented compounds of the formula or pharmaceutically acceptable salts thereof, wherein Y1, Y2, X1, X2, X3 and R are as described in this application. These compounds are believed to inhibit MDM2-p53 interaction and as such the compounds will have anti-hyperproliferative cellular activity.

Azolylbenzamides and analogues and their use for treating osteoporosis

A compound of formula (I) or a salt thereof, or a solvate thereof, wherein: X represents oxygen, sulphur, or NRb; Y and Z each independently represent nitrogen, CH, CR1 or CR2; A represents an unsubstituted or substituted aryl group or an unsubstituted or substituted heterocyclyl group; Ra represents —C(O)NRsRt; R1 and R2 each independently represents hydrogen or specific substituents; and the use of such a compound in the treatment and/or prophylaxis of diseases associated with over activity of osteoclasts in mammals.

Indole derivatives and their use for the treatment of osteoporosis amongst other applications

A compound of formula (1) or a salt thereof, or a solvate thereof, wherein; R1and R2each independently represents C1-6alkoxy or halo; R3and R4each independently represents hydrogen, C1-6alk

Synthesis of photoactivable inhibitors of osteoclast vacuolar ATPase

Amides of (2Z,4E)-5-[(5,6-dichloroindol-2-yl)]-2-methoxy-N-[3-[4-[3-(carboxymethoxy) phenyl)] piperazin-1-yl]propyl]-2,4-pentadienamide (1) and of 5-(5,6-dichloro-2-indolyl)-2-methoxy-2,4-pentadienoic acid (2) are strong inhibitors of the vacuolar ATPase located on the plasma membrane of osteoclasts. In order to understand which V-ATPase subunit is involved in the interaction with these novel inhibitors, analogues containing a photoactivable group and an iodine atom were designed. A series of alcohols or amines containing the photoactivable trifluoroaziridinophenyl or benzophenone moiety and an iodine atom were linked to the above acids via an ester or amide group. These compounds could be thereafter used as a radioactive photoprobe to label the protein. Whereas the compounds containing the photoactivable groups maintained good inhibitory activity, the introduction of the bulky iodine atom was generally detrimental, decreasing potency significantly. Better results were obtained by linking 3-(4-aminopiperidinomethyl)-3′-iodobenzophenone to 3-ethoxy-4-(2-(5,6-dichlorobenzimidazolyl))benzoic acid to give the corresponding amide 27, that inhibited vacuolar ATP-ase with a IC50=140 nM. The feasibility of introducing a radioactive 125I atom was ascertained by exchanging the iodine with a tributylstannyl group, that was again substituted by iodine.