摘要:
Substituted indazoles, compositions containing them, method of production and use. The present invention relates in particular to novel specific substituted indazoles exhibiting kinase-inhibiting activity, having therapeutic activity, in particular in oncology.
摘要:
Substituted indazoles, compositions containing them, method of production and use. The present invention relates in particular to novel specific substituted indazoles exhibiting kinase-inhibiting activity, having therapeutic activity, in particular in oncology.
摘要:
Substituted indazoles, compositions containing them, method of production and use. The present invention relates in particular to novel specific substituted indazoles exhibiting kinase-inhibiting activity, having therapeutic activity, in particlar in oncology.
摘要:
The present invention relates to a class of 2-aminothiazoline derivatives of formula I: in which either R1 is a hydrogen atom or an alkyl radical and R2 is an alkyl, -alk-NH2, —CH2—R3, —CH2—S—R4 or phenyl radical substituted with a nitro or —NH—C(═NH)CH3 radical, or R1 is an alkyl radical and R2 is a hydrogen atom, R3 is a (3-6C) cycloalkyl, pyridyl, pyridyl N-oxide, thienyl, thiazolyl, imidazolyl, pyrazinyl, triazolyl or phenyl radical or a phenyl radical substituted with a nitro, hydroxy or carboxyl radical, R4 represents a pyridyl or pyridyl N-oxide radical, alk represents an alkylene radical, or pharmaceutically acceptable salts thereof, which are useful as inhibitors of inducible NO-synthase.
摘要:
The present invention relates to the use of 2-aminothiazoline derivatives of formula: in which either R1 is a hydrogen atom or an alkyl radical and R2 is an alkyl, -alk—NH2, —CH2—R3, —CH2—S—R4 or phenyl radical substituted with a nitro or —NH— C (═NH) CH3 radical, or R1 is an alkyl radical and R2 is a hydrogen atom, R3 is a (3-6C) cycloalkyl, pyridyl, pyridyl N-oxide, thienyl, thiazolyl, imidazolyl, pyrazinyl, triazolyl or phenyl radical or a phenyl radical substituted with a nitro, hydroxy or carboxyl radical, R4 represents a pyridyl or pyridyl N-oxide radical, alk represents an alkylene radical, or pharmaceutically acceptable salts thereof, as inhibitors of inducible NO-synthase.
摘要:
The present invention relates to pharmaceutical compositions containing, as active principle, a 4,5-dihydro-1,3-thiazol-2-ylamine derivative of formula (I): in which R represents an -alk-S-alk-Ar radical, a phenyl radical or a phenyl radical substituted with alkoxy or halogen, or to one of the pharmaceutically acceptable salts thereof, to the novel derivatives of formula (I) and to their preparation.
摘要:
Compounds of formula (I), wherein R is a hydrogen atom or a carboxy, alkoxycarbonyl, --CO--NR.sub.4 R.sub.5, --PO.sub.3 H.sub.2 or --CH.sub.2 OH radical, and R.sub.1 is an -alk-NH.sub.2, -alk-NH--CO--R.sub.3, -alk-COOR.sub.4, -alk-CO--NR.sub.5 R.sub.6 or --CO--NH--R.sub.7 radical. The compounds of formula (I) have valuable pharmacological properties and are antagonists of the .alpha.-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor also known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive antagonists of the N-methyl-D-aspartame (NMDA) receptor and more specifically are ligands for NMDA receptor glycine modulator sites.
摘要:
The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, —COORc-CO-Rc or —CO—NRcRd; where Rc represents alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd represents H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.
摘要:
A compound of the formula ##STR1## in which Ra represents an -alk-COOalk' radical, a --CH.sub.2 --PO(Oalk).sub.2 radical, a --CH.dbd.CH--COOalk' radical or a phenyl radical substituted with an alkoxycarbonyl radical.
摘要:
A compound of formula (II): ##STR1## in which R is a hydrogen atom or a carboxy, alkoxycarbonyl, --CO--NR.sub.4 R.sub.5, --PO.sub.3 H.sub.2 or --CH.sub.2 OH radical, and R.sub.1 is an -alk-NH.sub.2, -alk-NH--CO--R.sub.3, -alk-COOR.sub.4, -alk-CO--NR.sub.5 R.sub.6 or --CO--NH--R.sub.7 radical. The compounds of formula (II) can be used to prepare compounds of formula (I): ##STR2## in which R and R.sub.1 have the same meanings as above. The compounds of formula (I) have valuable pharmacological properties and are antagonists of the .alpha.-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor, also known as the quisqualate receptor. The compounds of formula (I) are also non-competitive antagonists of the N-methyl-D-aspartate (NMDA) receptor and more specifically are ligands for NMDA receptor glycine modulator sites.