[Federal Register Volume 59, Number 157 (Tuesday, August 16, 1994)]
[Unknown Section]
[Page 0]
From the Federal Register Online via the Government Publishing Office [www.gpo.gov]
[FR Doc No: 94-19941]


[[Page Unknown]]

[Federal Register: August 16, 1994]


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DEPARTMENT OF HEALTH AND HUMAN SERVICES
 

Prospective Grant of Exclusive License: Acetylcholinesterase 
Inhibitors for the Treatment of Alzheimer's Disease and Cognitive 
Disorders

AGENCY: National Institutes of Health, Public Health Service, DHHS.

ACTION: Notice.

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SUMMARY: This is notice in accordance with 35 U.S.C. 209(c)(1) and 37 
CFR 404.7(a)(1)(i) that the National Institutes of Health (NIH), 
Department of Health and Human Services, is contemplating the grant of 
an exclusive world-wide licenses to practice the inventions embodied in 
U.S. Patent 5,171,750, entitled ``Substituted Phenserines as Specific 
Inhibitors of Acetylcholinesterase'' and U.S. Patent Applications SN 
07/861,329 and 08/096,207, both entitled ``Phenylcarbamates of (-)-
Eseroline, (-)-N1-Noreseroline and (-)-N1-Benzylnoreseroline: Selective 
Inhibitors of Acetyl and/or Butyrylcholinesterase,'' 07/765,766, 
entitled ``Thiapysovenine and Carbamate Analogs, Pharmaceutical 
Compositions and Method for Inhibiting Cholinesterases,'' 07/845,081 
and 08/182,301, both entitled ``Carbamate Analogs of Thiaphysovenine, 
Pharmaceutical Compositions, and Method for Inhibiting 
Cholinesterases,'' and 07/980,399, entitled ``Method for Treating 
Cognitive Disorders With Phenserine'' to CURE, Inc. of Baltimore, 
Maryland. The patent rights in these inventions have been assigned to 
the United States of America.
    The prospective exclusive license will be royalty-bearing and will 
comply with the terms and conditions of 35 U.S.C. 209 and 37 CFR 404.7. 
The prospective exclusive licenses may be granted unless within 60 days 
from the date of this published notice, NIH receives written evidence 
and argument that establishes that the grant of the license would not 
be consistent with the requirements of 35 U.S.C. 209 and 37 CFR 404.7.
    The patent and patent applications disclose several novel, potent 
and long-acting anti-cholinesterase agents that enhance cognition and 
are highly promising drug candidates for the treatment of Alzheimer's 
disease and other neurological disorders as well as methods for 
treating these conditions. The two series of drugs are based loosely on 
the first-generation cholinesterase inhibitor, physostigmine. 
Physostigmine has produced demonstrable but small clinical improvements 
in patient's with Alzheimer's disease, but these are severely limited 
by (i) its short half-life (approximately 30 minutes) and (ii) its high 
incidence of toxic side-effects at doses that produce only modest 
enzyme inhibition. It is widely accepted that the narrow therapeutic 
index of physostigmine and some other first generation 
acetylcholinesterase inhibitors limits the administration of these at 
adequate doses to affect cognition. The present drug candidates are 
long-acting and highly selective for acetyl- (AChE) as opposed to 
butyrylcholinesterase (BChE). Whereas AChE is involved in the 
metabolism of ACh, and inhibiting AChE augments the action of ACh and 
thereby cholinergic function and memory in Alzheimer's disease, BChE 
has been proposed to be involved in lipid and phospholipid metabolism, 
in permeability control and transport of ions across membranes, and in 
slow nerve conduction. Co-inhibition of BChE in Alzheimer's patients, 
as a consequence of anticholinesterase therapy, probably is not of 
clinical value, and may be deleterious.

ADDRESSES: Requests for copies of the patent and the patent 
applications, inquiries, comments and other materials relating to the 
contemplated licenses should be directed to: Mr. Arthur J. Cohn, Esq., 
Technology Licensing Specialist, Office of Technology Transfer, 
National Institutes of Health, 6011 Executive Boulevard, Suite 325, 
Rockville, Maryland 20892. Telephone: (301) 496-7735; Facsimile: (301) 
402-0220. A signed Confidentiality Agreement will be required to 
receive copies of the patent applications. Applications for a license 
in the any field of use filed in response to this notice will be 
treated as objections to the grant of the contemplated licenses. Only 
written comments and/or applications for a license which are received 
by NIH within sixty (60) days of this notice will be considered.

    Dated: August 9, 1994.
Barbara M. McGarey,
Deputy Director, Office of Technology Transfer.
[FR Doc. 94-19941 Filed 8-15-94; 8:45 am]
BILLING CODE 4140-01-P