Charles H Walter

US Patent:

55254748, Jun 11, 1996

Filed:

Jan 31, 1994

Appl. No.:

8/190348

Inventors:

Gerald F. Sigler - Carmel IN
Charles F. Walter - Carmel IN
Todd Glancy - Fairmount IN
Erasmus Huber - Finning, DE
Frank E. Klein - Eklton MD

Assignee:

Boehringer Mannheim Corporation - Indianapolis IN

International Classification:

G01N 33542
C12N 996
C07D207273
C07D21160

US Classification:

435 77

Abstract:

Novel derivatives of procainamide and N-acetylprocainamide (NAPA) are disclosed having the following formula: ##STR1## 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 ##STR2## wherein R2=an alkyl, cycloalkyl or aryl group having 2 to 10 carbon atoms. The derivatives include maleimide conjugates of proteins or poly(amino acids), enzymes, enzyme donor polypeptides and labeling substances. Novel activated hapten intermediates useful in the preparation of the conjugates and methods for synthesis of the hapten intermediates and derivatives are also disclosed.

US Patent:

54397987, Aug 8, 1995

Filed:

Dec 17, 1993

Appl. No.:

8/169851

Inventors:

Gerald F. Sigler - Carmel IN
Charles F. Walter - Carmel IN
Charles E. Durant - Indianapolis IN
Todd Glancy - Fairmount IN
Frank E. Klein - Elkton MD
Allan R. Dorn - Carmel IN

Assignee:

Boehringer Mannheim Corporation - Indianapolis IN

International Classification:

G01N 33542
C07K 1644
C12N 996
C07D207448

US Classification:

435 77

Abstract:

Novel derivatives of procainamide and N-acetylprocainamide (NAPA) are disclosed having the following formula: ##STR1## wherein: X=hydrogen or acetyl; R. sub. 1 =an alkyl group having 1 to 3 carbon atoms; m=an integer from 2 to 10; R. sub. 2 =an alkyl, cycloalkyl or aryl group having 2 to 10 carbon atoms; Z=a poly(amino acid); and n=1 to p where p=MW of Z/1000. The derivatives include maleimide conjugates of proteins or poly(amino acids), enzymes, enzyme donor polypeptides and labeling substances. Novel activated hapten intermediates useful in the preparation of the conjugates and methods for synthesis of the hapten intermediates and derivatives are also disclosed.