266369-42-0Relevant articles and documents
3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH
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Page/Page column 164, (2014/09/29)
The invention is directed to a formula (I), or a pharmamceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.
Discovery of (S,E)-3-(2-fluorophenyl)-N-(1-(3-(pyridin-3-yloxy)phenyl) ethyl)-acrylamide as a potent and efficacious KCNQ2 (Kv7.2) opener for the treatment of neuropathic pain
Wu, Yong-Jin,Conway, Charles M.,Sun, Li-Qiang,Machet, Frederic,Chen, Jie,Chen, Ping,He, Huan,Bourin, Clotilde,Calandra, Vincenzo,Polino, Joseph L.,Davis, Carl D.,Heman, Karen,Gribkoff, Valentin K.,Boissard, Christopher G.,Knox, Ronald J.,Thompson, Mark W.,Fitzpatrick, William,Weaver, David,Harden, David G.,Natale, Joanne,Dworetzky, Steven I.,Starrett Jr., John E.
, p. 6188 - 6191 (2013/11/06)
Acrylamide (S)-6, a potent and efficacious KCNQ2 (Kv7.2) opener, demonstrated significant activity in two models of neuropathic pain and in the formalin test, suggesting that KCNQ2 openers may be useful in the treatment of neuropathic pain including diabetic neuropathy.
NOVEL N-PYRAZINIL-PHENYLSULFONAMIDE DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS FOR USE IN THE TREATMENT OF ASTHMA
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Page/Page column 33, (2010/11/26)
The invention provides a compound of formula (I), wherein R1, R2 and R3 are as defined in the specification, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.
Synthesis and structure-activity relationship of acrylamides as KCNQ2 potassium channel openers
Wu, Yong-Jin,He, Huan,Sun, Li-Qiang,L'Heureux, Alexandre,Chen, Jie,Dextraze, Pierre,Starrett Jr., John E.,Boissard, Christopher G.,Gribkoff, Valentin K.,Natale, Joanne,Dworetzky, Steven I.
, p. 2887 - 2896 (2007/10/03)
A new class of acrylamides was synthesized, and the effects of these analogues on outward potassium current were evaluated by using two electrode voltage clamp recordings from Xenopus laevis oocytes expressing cloned mKCNQ2 channels. SAR studies indicated that the pharmacophore of the acrylamide series includes the (S) absolute configuration at the (1-phenyl)ethyl moiety and the α,β-unsaturated acrylamide functionality with a free NH. This study identified (S)-N-[1-(3-morpholin-4-yl-phenyl)-ethyl]-3-phenyl-acrylamide ((S)-1) and (S)-N-[1-(4-fluoro-3-morpholin-4-yl-phenyl)-ethyl]-3- (4-fluoro-phenyl)-acrylamide ((S)-2) as KCNQ2 openers for further electrophysiological evaluations. These two acrylamides demonstrated significant activity in the cortical spreading depression model of migraine as we reported previously.
AROMATIC AMINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND AGENTS CONTAINING THE SAME
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, (2008/06/13)
Compounds of a formula: wherein Ring A represents an optionally-substituted aromatic ring; Ring B represents an optionally-substituted cyclic hydrocarbon group; Z represents an optionally-substituted cyclic group; R1 represents a hydrogen atom, an optionally-substituted hydrocarbon group, an optionally-substituted heterocyclic group, or an acyl group; R2 represents an optionally-substituted amino group; D represents a chemical bond or a divalent group; E represents -CO-, -CON(Ra)-, COO-, -N(Ra)CON(Rb)-, -N(Ra)COO-, -N(Ra)SO2-, -N(Ra)-, -O-, -S-,-SO- or -SO2- (in which Ra and Rb each independently represent a hydrogen atom or an optionally-substituted hydrocarbon group); G represents a chemical bond or a divalent group; L represents (1) a chemical bond or (2) a divalent hydrocarbon group optionally having from 1 to 5 substituents selected from;(i) a C1-6 alkyl group,(ii) a halogeno-C1-6 alkyl group,(iii) a phenyl group,(iv) a benzyl group,(v) an optionally-substituted amino group,(vi) an optionally-substituted hydroxy group, and(vii) a carbamoyl or thiocarbamoyl group optionally substituted by: a C1-6 alkyl group, an optionally-substituted phenyl group, or an optionally-substituted heterocyclic group, and optionally interrupted by -O- or -S-; X represents an oxygen atom, an optionally-oxidized sulfur atom, an optionally-substituted nitrogen atom, or an optionally-substituted divalent hydrocarbon group; Y represents two hydrogen atoms, an oxygen atom or a sulfur atom; .... means that R2 may be bonded to the atom on Ring B to form a ring, or their salts, and a method for producing them.