摘要:
Glycoprotein (GPIR) the ribosome-inhibiting activity of the native GPIR and having a prolongedaction in vivo which is obtained by oxidation of its osidic units by the action of periodate ions, and simultaneous blocking of the oxidation product by formation of a Schiff's base with a suitable primary amine. Said modified glycoprotein may be coupled to an antibody or a fragment thereof in order to form an immunotoxin.
摘要:
Glycoprotein (GPIR) having the ribosome-inhibiting activity of the native GPIR and having a prolonged-action in vivo which is obtained by oxidation of its osidic units by the action of periodate ions, and simultaneous reduction with cyanoborohydride ions. Said modified glycoprotein may be coupled to an antibody or a fragment thereof in order to form an immunotoxin having a prolonged-action in vivo.
摘要:
Glycoprotein which inactivates ribosomes (GPIR) having the ribosome-inhibiting activity of the native GPIR and having a prolonged-action in vivo which is obtained by oxidation of its osidic units by the action of periodate ions, and simultaneous reduction with cyanoborohydride ions. Said modified glycoprotein may be coupled to an antibody or a fragment thereof in order to form an immunotoxin having a prolonged-action in vivo.
摘要:
Glycoprotein which inactivates ribosomes (GPIR) the ribosome-inhibiting activity of the native GPIR and having a prolonged-action in vivo which is obtained by oxidation of its osidic units by the action of periodate ions, and simultaneous blocking of the oxidation product by formation of a Schiff's base with a suitable primary amine. Said modified glycoprotein may be coupled to an antibody or a fragment thereof in order to form an immunotoxin.
摘要:
The disclosure relates to pyrido[2,3-d]pyrimidone compounds, to the preparation thereof and to the therapeutic use thereof, wherein said compounds are of general formula (I): in the form of a base or of an addition salt with an acid which is pharmaceutically acceptable, in the form of hydrates or of solvates, and also in the form of enantiomers, diastereoisomers and a mixture thereof. The disclosure also relates to processes for preparing said compounds, to pharmaceutical compositions containing a compound of general formula (I), and to the therapeutic use of said compounds and compositions.
摘要:
The disclosure concerns pyrido[2,3-d]pyrimidine derivatives, their preparation and their therapeutic application, of general formula (I): and acid addition salts, hydrates and solvates thereof, as well as in the form of enantiomers, diastereoisomers and mixtures thereof. The disclosure also concerns methods for preparing said derivatives, pharmaceutical compositions containing a compound of general formula (I), and their therapeutic use.
摘要:
The present invention relates to pyridoindolone derivatives substituted in the 3-position by a heterocyclic group of general formula (I): in which: R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 represents a hydrogen atom or a (C1-C4)alkyl group; R3 represents a thienyl mono- or polysubstituted by a methyl group; or a monocyclic or bicyclic heterocyclic radical chosen from: a pyridyl, an N-oxidopyridinio, a pyrazolyl, an (N-phenyl)pyrazolyl, an (N-halophenyl)pyrazolyl, a furyl, an indolyl, an (N-benzyl)indolyl, an (N-halobenzyl)indolyl, a benzothienyl or a benzofuryl, the said radicals being unsubstituted or substituted one or more times by a halogen atom or a methyl or methoxy group; R4 and R5 are identical or different and each independently represent a hydrogen or halogen atom or a hydroxyl, hydroxymethyl, (C1-C4)alkyl, trifluoromethyl, C1-C4)alkoxy, (C1-C4)alkoxycarbonyl or cyano group. Preparation process and application in therapeutics.
摘要:
The present invention relates to compounds of formula (I): in which R1 represents a hydrogen or halogen atom, or a group CF3; R2 and R3 represent, independently, a hydrogen atom or a methyl group; n and n′ each represent, independently, 0 or 1; * represents the positions of attachment; A represents N or CH; X represents a sulfur or oxygen atom; R4 and R5 represent, independently, a hydrogen atom or a (C1-C6) alkyl group; and also their salts or solvates, to a method for the preparation thereof and to the pharmaceutical compositions containing them.
摘要:
Compounds of formula: and pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2, R3, R4, and R5, have the meanings given in the description; pharmaceutical compositions comprising said compounds; and processes for preparing said compounds and methods of use thereof.