132383-36-9Relevant academic research and scientific papers
Discovery of BI-2545: A Novel Autotaxin Inhibitor That Significantly Reduces LPA Levels in Vivo
Kuttruff, Christian A.,Ferrara, Marco,Bretschneider, Tom,Hoerer, Stefan,Handschuh, Sandra,Nosse, Bernd,Romig, Helmut,Nicklin, Paul,Roth, Gerald J.
supporting information, p. 1252 - 1257 (2017/12/26)
In an effort to find new therapeutic interventions addressing the unmet medical need of patients with idiopathic pulmonary fibrosis, we initiated a program to identify new autotaxin (ATX) inhibitors. Starting from a recently published compound (PF-8380), we identified several highly potent ATX inhibitors with improved pharmacokinetic and safety profiles. Further optimization efforts resulted in the identification of a single-digit nanomolar lead compound (BI-2545) that shows substantial lowering of LPA in vivo and is therefore considered a valuable tool for further studies.
2-OXO-3-BENZYLBENZOXAZOL-2-ONE DERIVATIVES AND RELATED COMPOUNDS AS MET KINASE INHIBITORS FOR THE TREATMENT OF TUMOURS
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Page/Page column 31-32, (2010/12/29)
Compounds of the formula (I), in which R1, R2, R3, R3′, R4, R4′, E, E′, E″ and E′″ have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
Radiosynthesis and pharmacological evaluation of [11C]EMD-95885: A high affinity ligand for NR2B-containing NMDA receptors
Roger,Dolle,De Bruin,Liu,Besret,Bramoulle,Coulon,Ottaviani,Bottlaender,Valette,Kassiou
, p. 3229 - 3237 (2007/10/03)
EMD-95885, 6-[3-[4-(4-fluorobenzyl)piperidino]propionyl]-3H-benzoxazol-2- one (1) has been described as a selective antagonist for the NMDA receptors containing NR2B subunits, displaying an IC50 of 3.9nM for this subtype. EMD-95885 (1) has been
AlCl3-DMF Reagent in the Friedel-Crafts Reaction. The Behavior of ω-Halogenoacid Chlorides
Poupaert, Jacques H.,Kanyonyo, Martial,Ucar, Huseyin,Mouithys, Ange M.,Diouf, Ousman,Lesieur, Daniel
, p. 397 - 402 (2007/10/03)
2(3H)-Benzoxazolones or 2(3H)-benzothiazolones react at 70-75 deg C with ω-halogenoacyl chlorides in the presence the AlCl3-DMF complex to produce the expected ketones in 55-88percent yield.Treatment of a 2(3H)-benzoxazolone or 2(3H)-benzothiazolone by 4-chlorobutyryl chloride produced an alcohol derivative, presumably via an anchimeric participation of the 6-acyl carbonyl moiety.
Benzoxazolinone compounds, compositions and use
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, (2008/06/13)
Compounds of general formula (I): STR1 in which: R1 denotes a hydrogen atom or a lower alkyl optionally substituted with a hydroxyl group, R2 and R3 : a--identical or different, denote a hydrogen atom, a lower alkyl, a lower alkenyl, a substituted or unsubstituted aryl, a substituted or unsubstituted (lower alkyl)aryl, b--are such that they form, with the nitrogen which carries them, a saturated or unsaturated, mono- or bicyclic heterocyclic system containing at most 3 hetero atoms per ring, substituted or unsubstituted, with the exception of 1-arylpiperazine systems, X denotes a hydrogen atom, Y denotes a hydrogen atom or a hydroxyl, or alternatively X and Y denote an oxygen atom, provided that R1 is then other than a methyl group, Z denotes a hydrogen atom or forms a ? bond with Y, and T denotes a hydrogen atom or a lower alkyl, their stereoisomers and their quaternary ammonium salts, as well as their addition salts with a pharmaceutically acceptable acid.
A Convenient and Efficient Method for the Preparation of 6-Acyl-2(3H)-benzoxazolones
Aichaoui, Hocine,Lesieur, Daniel,Henichart, Jean-Pierre
, p. 171 - 175 (2007/10/02)
Benzoxazolinone derivatives have been found to exhibit various pharmacological properties and 6-acyl-2(3H)-benzoxazolones are considered as key starting materials for the preparation of these compounds.Reported here are the optimal conditions for a regioselective acylation at the 6-position of the benzoxazolinone ring.A general method leading to the expected products in excellent yields consists in using a mixture of aluminum chloride-dimethylformamide as catalyst and acid anhydrides or chlorides as acylating agents.
