Daniel L Mcpherson

US Patent:

48746002, Oct 17, 1989

Filed:

Apr 17, 1986

Appl. No.:

6/853105

Inventors:

Daniel W. McPherson - Baltimore MD
Joanna S. Fowler - Bellport NY
Alfred P. Wolf - Setauket NY

Assignee:

The United States of America as Represented by the United States
Department of Energy - Washington DC

International Classification:

A61K 4902
C07C 8714

US Classification:

424 11

Abstract:

The invention relates to a new radiolabeled imaging agent, no-carrier-added [1-. sup. 11 C]putrescine, and to the use of this very pure material as a radiotracer with positron emission tomography for imaging brain tumors. The invention further relates to the synthesis of no-carrier-added [1-. sup. 11 C]putrescine based on the Michael addition of potassium. sup. 11 C-labeled cyanide to acrylonitrile followed by reduction of the. sup. 11 C-labeled dinitrile. The new method is rapid and efficient and provides radiotracer with a specific activity greater than 1. 4 curies per millimol and in a purity greater than 95%.

US Patent:

50361074, Jul 30, 1991

Filed:

Nov 16, 1989

Appl. No.:

7/437165

Inventors:

Waclaw J. Rzeszotarski - Millersville MD
Daniel W. McPherson - Baltimore MD
Ciro J. Spagnuolo - Cockeysville MD
Kenneth J. Natalie - Baltimore MD

Assignee:

Marion Merrell Dow Inc. - Kansas City MO

International Classification:

A61K 31135
C07C22518

US Classification:

514648

Abstract:

1-Phenyl-7-substituted-hept-5-yn-2-ones substituted with a C. sub. 1 to C. sub. 7 alkyl, C. sub. 3 to C. sub. 6 cycloalkyl, aryl, heteroaryl or heterocycloalkyl group at the 1-position and an amino, a dialkylamino, a piperidyl, a pyrrolidyl or a hexahydroazepinyl group at the 7-position are disclosed which may have one or two substituents in addition to the phenyl group at the 1-position and also may have a p-fluoro substituent on the phenyl group. The preferred compounds are, 1-cyclohexyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2-one, 1-cyclobutyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2-one and 1-cyclo-1-phenyl-1-hydroxy-7-ethylaminohept-5-yn-2-one. The compounds are highly specific M. sub. 1 -AChR antagonists with relatively prolonged duration of activity. They are particularly useful in the treatment of neurogenic bladder disorders and may be administered orally or parenterally in conventional formulations containing optional conventional additives such as binders, surfactants, emulsifiers, flavorants, preservatives and the like.