Inhibitors of bace
First Claim
Patent Images
2. A BACE inhibitor having the following features:
- (a) HB-1;
(b) HPB-4;
(c) HPB-1 and at least one of the following (d) and (e);
(d) HPB-2; and
(e) HPB-3.
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Accused Products
Abstract
The present invention relates to inhibitors of aspartic proteinases, particularly, BACE. The present invention also relates to compositions thereof and methods therewith for inhibiting BACE activity in a mammal, and for treating Alzheimer'"'"'s Disease and other BACE-mediated diseases.
116 Citations
70 Claims
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2. A BACE inhibitor having the following features:
-
(a) HB-1;
(b) HPB-4;
(c) HPB-1 and at least one of the following (d) and (e);
(d) HPB-2; and
(e) HPB-3. - View Dependent Claims (6, 7, 8)
-
- 26. A method of inhibiting BACE activity in a mammal, comprising the step of administering to said mammal a compound of formula IA:
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40. A method of inhibiting BACE activity in a mammal, comprising the step of administering to said mammal a compound of formula IAB:
- 43. A method of inhibiting BACE activity in a mammal, comprising the step of administering to said mammal a compound of formula ID:
- 45. A method of inhibiting BACE activity in a mammal, comprising the step of administering to said mammal a compound of formula IE:
- 49. A method of inhibiting BACE activity in a mammal, comprising the step of contacting said mammal with a compound selected from Tables IA-ID.
- 51. A compound of formula II:
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58. The compound according to claim 58, wherein W or W4 is an eight to eleven membered bicyclic ring, wherein either or both rings is aromatic, and either or both rings has zero to three heteroatoms independently selected from O, S, N, or NH, wherein W or W4 has up to 3 substituents independently selected from J.
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59. The compound according to claim 59, wherein W or W4 is selected from naphthyl, 3-1H-benzimidazol-2-one, (1-substituted)-2-oxo-benzimidazol-3-yl, 1-phthalimidinyl, benzoxanyl, benzopyrrolidinyl, benzopiperidinyl, benzoxolanyl, benzothiolanyl, benzothianyl, indolinyl, chromanyl, phenanthridinyl, tetrahydroquinolinyl, carbazolyl, benzimidazolyl, benzothienyl, benzofuranyl, indolyl, quinolinyl, benzotriazolyl, benzothiazolyl, benzooxazolyl, benzimidazolyl, isoquinolinyl, indolyl, isoindolyl, acridinyl, benzoisoxazolyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, or pyrido[3,4-d]pyrimidiny, wherein W or W4 has up to 3 J substituents.
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64-1. The compound according to claim 51, wherein J is independently selected from halogen, —
- R′
, —
OR′
, —
NO2, —
CN, —
CF3, —
OCF3, oxo, 1,2-methylenedioxy, —
N(R′
)2, —
SR′
, —
S(O)R′
, —
S(O)N(R′
)2, —
SO2R′
, —
C(O)R′
, —
CO2R′
or —
C(O)N(R′
)2, wherein R′
is independently selected from hydrogen or (C1-C6)-alkyl.
- R′
Specification