Oxime-containing macrocyclic acyl guanidines as β-secretase inhibitors
AssigneeBristol-Myers Squibb Company
InventorsYong-Jin Wu, Samuel Gerritz, Shuhao Shi, Shirong Zhu
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Abstract
There is provided a series of oxime-containing macrocyclic acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, R4, n and X as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
Claims8
A compound of Formula (I);
- or a stereoisomer thereof
- wherein
- R1 and R2 are independently selected from hydrogen, C1-4alkyl, halogen and CF3;
- R3 is C1-4alkyl, allyl, C3-6cycloalkyl or CF3;
- R4 is hydrogen, halogen, CN, CF3, OH, —NH2, C1-6alkyl or C1-6alkoxy;
- n is an integer from 1 to 6;
- and
- X is (CH2)2 or CH═CH;
- or a nontoxic pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.