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|Title:||Neurotrophic pyrrolidines and piperidines, and related compositions and methods|
|Abstract:||This invention provides compounds having the following general structures: ##STR1## This invention also provides pharmaceutical compositions comprising same and methods of using these compositions to treat and prevent disorders characterized by neuronal damage.|
|Inventor(s):||Kanojia; Ramesh M. (Bridgewater, NJ), Jordan; Alfonzo D. (North Wales, PA), Reitz; Allen B. (Lansdale, PA), Macielag; Mark J. (Branchburg, NJ), Zhao; Boyu (Lansdale, PA)|
|Assignee:||Ortho-McNeil Pharmaceutical, Inc. (Raritan, NJ)|
|Filing Date:||Jun 14, 2000|
|Claims:||1. A compound having the structure ##STR243## |
or a pharmaceutically acceptable salt thereof, wherein (a) R.sup.1 is selected from the group consisting of H, COCOR.sup.2, COOR.sup.3 and SO.sub.2 R.sup.3, (i) R.sup.2 being selected from the group consisting of C.sub.1-6 straight or branched alkyl, C.sub.1-6 straight or branched alkenyl, C.sub.5-7 cycloalkyl, 2-thienyl, 3-thienyl or phenyl, the phenyl having one to three substituents independently selected from the group consisting of H, lower alkyl, lower alkoxyl, hydroxyl and halogen, and (ii) R.sup.3 being phenylalkyl, wherein the phenyl has one to three substituents independently selected from the group consisting of H, lower alkyl, lower alkoxyl, hydroxyl and halogen; (b) ##STR244## is either a saturated five-membered nitrogen containing heterocyclic ring, said ring containing one nitrogen atom, or a benzo-fused saturated six-membered nitrogen containing heterocyclic ring; (c) ##STR245## is an oxazole, an oxadiazole or a thiazole; and (d) A is attached to a carbon of the five-membered heteroaromatic ring and is selected from the group consisting of COO(CH.sub.2).sub.m Ar, ##STR246## (such R.sup.1 being the same as or different than the R.sup.1 described in part (a)), CONR.sup.4 (CH.sub.2).sub.m Ar, and (CH.sub.2).sub.m O(CH.sub.2).sub.n Ar (wherein R.sup.1 cannot be COCOR.sup.2 or SO.sub.2 R.sup.3), (i) R.sup.4 being H or C.sub.1-4 alkyl; (ii) Ar being selected from the group consisting of 2-pyridyl, 3-pyridyl, and 4 pyridyl; (iii) m being 1-4; and (iv) n being 0-4.
2. The compound of claim 1 having the structure ##STR247##
3. The compound of claim 1 having the structure ##STR248##
4. The compound of claim 1 having the structure ##STR249##
5. The compound of claim 1 having the structure ##STR250##
wherein each R.sup.1 is either the same as, or different than, the other.
6. The compound of claim 5 having the structure ##STR251##
7. The compound of claim 5 having the structure ##STR252##
8. The compound of claim 5 having the structure ##STR253##
9. The compound of claim 5 having the structure ##STR254##
10. The compound of claim 5 having the structure ##STR255##
11. The compound of claim 5 having the structure ##STR256##
12. A compound having the structure ##STR257##
13. A method of treating in a subject, Parkinson's disease, Alzheimer's disease, stroke, multiple sclerosis, amyotrophic lateral sclerosis, diabetic neuropathy or Bell's palsy, comprising administering to the subject a prophylactically effective amount of the compound of claim 1.
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