2) United States Patent
Ablordeppey et al.
(54) HALOPERIDOL ANALOG
(75) Inventors: Seth Y. Ablordeppey, Tallaassee, PI
(US); Donald M. N. Sikuzwe,
Tallahassee, FL (US)
Florida A&M University, Tallahassee,
FLQUS)
(93) Assignee:
Notice: Subject to any disclaimer, the term ofthis
pateat is extended of adjusted under 35
USC. 154(b) by 372 days.
an
Appl. No 101934,769
(22) Filed: Sep. 7, 2004
(65) Prior Publication Data
S 2006005236341 Mar. 9, 2006
(1) Ineck
AGIP 3518
AGIK 3155
AAGIK 31/445
AGIK 31/40
coz 20710
corp 20746
coz 21100
cor 2120
CozD 2254
07D 24308
coz 295/00
corp 48700
a
silat
(200601)
(200601)
(2006.01),
(2006.01)
(200601)
(2006.01),
(200601)
(2006.01),
(200601)
(200601),
(200601),
(2006.01)
514/218; 514/317; 5141327
S14i424; 514/428; S40/461; 840/575:
‘4/217: SA6/247, 48/556, 548/571
Field of Classification Search ‘514/218,
SLA/317, 327, 412, 424, 428; 540/46,
‘546/217, 287; SAN/SS
See application file for complete search history.
650) References Cited
US. PATENT DOCUMENTS
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AS09573 A AL97O Schima ta 260.268.
S2m0382 A 711993 Chakra et als wo $14220
OTHER PUBLICATIONS
Abloreppey et al Design and Synthesis of Novel Analogs of
Haloperdol Incapable of Fomning MPP+-Like Species, Medicinal
Chomisry Research, (7), pp 459-467, 19952
Iyles- Eggleston etal. Design, Symes, and Evaluation of Metabo-
lismBasod Analogues of Haloperidel Incapable of Forming MPP.
like Species dourmal of Metisinal Chemistry, Jan. 29,2004, vol 7,
No.3: pp 497-508, especially p 498 —relvan to claims 1-5,
'US007700587B2
(10) Patent No.
4s) Date of Patent:
US 7,700,587 B2
Apr. 20, 2010
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* cited by examiner
Primary Examiner
(73) Attorney
rend [Coleman
Agent, or Firm—Dennis . Clarke
on ABSTRACT
Haloperidel analo
_ o
wherein: Ris H, or (CH), OH,
nnisan integer from 0 to 2, and
\ isabetercyclic bridging group, consisting essentially
of earbon and atleast one nitrogen atom, which eff
tively maintains the distance between the moieties
connected theeeby sk thatthe compound (1 isinca
pable of metabolizing to BCPP" lke species, (2) has
in affinity’ forthe D2 receptor subtype of 15