BACE Review Proposal

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Recent development of -secretase inhibitors as potential disease-modifying treatments of Alzheimer’s Disease Nick Paras, Ana Minatti, and Wenge Zhong Chemistry Research & Discovery, Amgen Inc., Thousand Oaks, CA 91362 Proposed Contents 1. Introduction 2. The traditional hydroxyethylamine (HEA) derived inhibitors (potency, permeability and efflux properties, and in vivo efficacy will be discussed) 3. Novel aminoheterocyclic derived inhibitors 3.1. The aminoheteroaryls 3.2. The aminoquinoxalines 3.3. The cyclic acylguanidines 3.4. The cyclic amindines 3.5. The aminooxazolidines 3.6. The aminothiazolidines 4. Cyclic amine derived inhibitors 4.1. The pyrrolidines 4.2. The piperidines 4.3. The piperizines 5. Others – macrocyclic inhibitors and alternative scaffolds (publications between now and the time of completion of this review) 6. Summary

Transcript of BACE Review Proposal

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Recent development of -secretase inhibitors as potential disease-modifying treatments of Alzheimer’s Disease

Nick Paras, Ana Minatti, and Wenge ZhongChemistry Research & Discovery, Amgen Inc., Thousand Oaks, CA 91362

Proposed Contents

1. Introduction2. The traditional hydroxyethylamine (HEA) derived inhibitors (potency,

permeability and efflux properties, and in vivo efficacy will be discussed)

3. Novel aminoheterocyclic derived inhibitors3.1. The aminoheteroaryls3.2. The aminoquinoxalines3.3. The cyclic acylguanidines3.4. The cyclic amindines3.5. The aminooxazolidines3.6. The aminothiazolidines

4. Cyclic amine derived inhibitors4.1. The pyrrolidines4.2. The piperidines4.3. The piperizines

5. Others – macrocyclic inhibitors and alternative scaffolds(publications between now and the time of completion of this review)

6. Summary

(Generic structures and specific examples are listed in the subsequent pages)

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Specific examples:

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