Piperidine analogs and conjugates of procainamide and napa

Details Piperidine analogs and conjugates of procainamide and napa Piperidine analogs and conjugates of procainamide and napa

C - Chemistry, Metallurgy

07

D

C07D 211/60 (2006.01) C07D 211/62 (2006.01) C07D 401/12 (2006.01) C07K 14/00 (2006.01) C07K 16/44 (2006.01) C08B 37/00 (2006.01) C12N 9/96 (2006.01) G01N 33/53 (2006.01) G01N 33/531 (2006.01) G01N 33/573 (2006.01) G01N 33/94 (2006.01)

Patent

CA 2181898

Novel derivatives of procainamide and N-acetylprocainamide (NAPA) are disclosed having formula (1) wherein: X - hydrogen or acetyl; n = 1 to p where p = MW of Z/1000; Z = a poly(amino acid) or polysaccharide; and R3 = a bond or (2) wherein R2 = an alkyl, cycloalkyl or aryl group having 2 to 10 carbon atoms. The derivatives include malamide conjugates of proteins or poly(amino acids), enzymes, enzyme donor polypeptides and labeling substances. Novel activated conjugates and methods for synthesis of the hapten intermediates and derivatives are also disclosed.

Nouveaux dérivés de la procaïnamide et de la N-acétylprocaïnamide (NAPA) de formule (1) (dans laquelle X est hydrogène ou acétyle; n est 1 à p (p étant MM de Z/1000; Z est un poly(acide aminé) ou polysaccharide; et R¿3? une liaison) ou de formule (2) (dans laquelle R2 est un groupe alkyle, cycloalkyle ou aryle à 2 à 10 atomes de carbone). Ces dérivés comportent des conjugués maléimidiques de protéines ou de poly(acides aminés) d'enzymes, de polypeptides donneurs d'enzyme et de substances de marquage. Sont également présentés de nouveaux conjugués activés et des procédés de synthèse d'intermédiaires d'haptènes et de leurs dérivés.

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