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US 2003/0144262 A1Published application
N-heterocyclyl hydrazides as neurotrophic agents
AssigneeOrtho-McNeil Pharmaceutical, Inc.
InventorsZhihua Sui, Mark Macielag, James Lanter
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Abstract
This invention relates to a series of N-heterocyclyl hydrazides of Formula I, 1 and pharmaceutical compositions containing them. The compounds of the invention have neurotrophic activity and are useful in the treatment and prevention of neuronal disorders such as Parkinson's disease, Alzheimer's disease, stroke, multiple sclerosis, amyotrophic lateral sclerosis diabetic neuropathy and Bell's palsy.
Claims19
A compound of Formula I,
- 20
- or a pharmaceutically acceptable salt thereof, wherein
- H1 is selected from the group consisting of a 4-membered nitrogen-containing heterocyclyl having 3 carbon ring atoms, a 5-membered nitrogen-containing heterocyclyl having 0 or 1 additional heteroatom ring member selected from O, S, and N, and a 6- or 7-membered nitrogen-containing heterocyclyl having 0, 1, or 2 additional heteroatom ring members selected from O, S, and N;
- H2 is a 5- or 6-membered heteroaryl;
- R1 is selected from urea, C1-C10 alkyl, aryl, heteroaryl, heterocyclyl, —C(O)R, —C(O)—C(O)R, —SO2R, and —P(O)(OR′)(OR″), wherein R, R′, and R″ are independently selected from the group consisting of alkyl, aryl, heteroaryl, and heterocyclyl;
- and
- R2 and R3 are independently hydrogen or C1-C10 alkyl.
4 more elements
A process for preparing the compound of Formula I,
- 23
- which process comprises:
- (a) converting compound 1 to compound 2;
- and
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- (b) reacting compound 2 with compound 4 to form the compound 1.
3 more elements
Dependencies are inferred from the claim text.