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1. (WO1991017776) RADIOIODINATED BENZOVESAMICOL ANALOGS FOR CHOLINERGIC NERVE MAPPING
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1991/017776 International Application No.: PCT/US1991/003273
Publication Date: 28.11.1991 International Filing Date: 10.05.1991
Chapter 2 Demand Filed: 13.12.1991
IPC:
A61K 51/04 (2006.01) ,C07D 211/14 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51
Preparations containing radioactive substances for use in therapy or testing in vivo
02
characterised by the carrier
04
Organic compounds
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
211
Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06
having no double bonds between ring members or between ring members and non-ring members
08
with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
10
with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
14
with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
Applicants:
THE UNIVERSITY OF MICHIGAN [US/US]; Intellectual Properties Office 475 East Jefferson, Room 2354 Ann Arbor, MI 48109-1248, US
Inventors:
WIELAND, Donald, M.; US
JUNG, Yong-Woom; US
VAN DORT, Marcian, E.; US
GILDERSLEEVE, David, L.; US
Agent:
ROHM, Benita, J.; Rohm & Monsanto 512 Springfield Avenue Cranford, NJ 07016, US
Priority Data:
523,23314.05.1990US
Title (EN) RADIOIODINATED BENZOVESAMICOL ANALOGS FOR CHOLINERGIC NERVE MAPPING
(FR) ANALOGUES DE BENZOVESAMICOL RADIO-IODES DESTINES A LA CARTOGRAPHIE DES NEURONES CHOLINERGIQUES
Abstract:
(EN) Radioiodinated benzovesamicol analogs which selectively localize in presynaptic cholinergic neurons of general formula (I), where X is selected from the group consisting of H, OH, NH2, NHCO-3-[I]-Ph, and a radioactive isotope of iodine, and Y is selected from the group of H and a radioactive isotope of iodine, Y being H if X contains iodine. Illustrative examples include: (±)-trans-2-hydroxy-5-iodo-3-(4-phenylpiperidino)tetralin; (±)-trans-3-hydroxy-5-iodo-2-(4-phenylpiperidino)tetralin; (±)-trans-5-amino-2-hydroxy-8-iodo-3-(4-phenylpiperidino)tetralin; and (±)-trans-2-hydroxy-5-(3-iodobenzamido)-3-(4-phenylpiperidino)tetralin. The novel radioiodinated benzovesamicol analogs may be used as radiopharmaceuticals to visualize cholinergic neurons with conventional imaging devices which are typically found in most nuclear medicine or radiology clinics.
(FR) Analogues de benzovésamicol radio-iodés, qui se fixent sélectivement sur les neurones cholinergiques présynaptiques et correspondent à la formule générale (I), dans laquelle X est sélectionné dans le groupe formé par H, OH, NH2, HNCO-3-[I]-Ph et un isotope radioactif de l'iode, et Y est sélectionné dans le groupe formé par H et un isotope radioactif d'iode, Y étant H si X contient de l'iode. Ces analogues sont, à titre d'exemple, la (±)-trans-2-hydroxy-5-iodo-3-(4-phénylpipéridino)tétraline; la (±)-trans-3-hydroxy-5-iodo-2-(4-phénylpipéridino)tétraline; la (±)-trans-5-amino-2-hydroxy-8-iodo-3-(4-phénylpipéridino)tétraline et la (±)-trans-2-hydroxy-5-(3-iodobenzamido)-3-(4-phénylpipéridino)tétraline. Ces nouveaux analogues de benzovésamicol radio-iodés peuvent être utilisés comme produits pharmaceutiques radio-iodés pour visualiser des neurones cholinergiques à l'aide des dispositifs d'imagerie conventionnels présents dans la plupart des centres de médecine nucléaire ou de radiologie.
Designated States: CA, JP
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, NL, SE)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP0648130CA2082797