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. Author manuscript; available in PMC: 2015 Jun 14.
Published in final edited form as: Pharm Pat Anal. 2014 Jul;3(4):429–447. doi: 10.4155/ppa.14.22

Table 2.

The development of β-and γ-secretase inhibitors.

Compounds Chemical class Assignee Patent number Phases Ref.
β-secretase inhibitors
LY2886721 Aminothiazine derivatives Eli Lilly and Co., USA WO005738A1(2011) Phase I/II [44]
LY2811376 Aminodihydrothiazine derivatives Eli Lilly and Co., USA WO134617A1(2009) Phase I [45]
MK-8931 Imidazole derivatives Schering Corp., USA US0287692A1(2007) Phase II/III [46]
2a Lactams derivatives Pfizer, Inc., USA WO172449A1(2012) Discovery [41]
3a Thioamidine derivatives Pfizer, Inc., USA WO030713A1(2013) Discovery [42]
4a Tricyclicderivatives Array Biopharma Inc., USA; Genentech, Inc., USA WO148851A1(2013) Discovery [43]
γ-secretase inhibitors
LY-450139 Butanamides Eli Lilly and Co., USA US0299053A1(2007) Phase III [47]
BMS-708163 Trifluoropentanamides Bristol-Myers Squibb Co., USA US0260837A1(2010) Phase II [48]
NIC5-15 Pinitol Waratah Pharmaceuticals, Inc., USA US0105631A1(2010) Phase II [49]
GSI-953 Thiophene sulfonamide Wyeth, USA US0181932A1(2009) Phase I [50]
PF-3084014 Pentanamide derivatives Pfizer, Inc., USA US0215610A1(2005) Phase I [51]
BMS299897 Sulfonamide Elan Pharmaceuticals, Inc., USA US0045499A1(2008) Discovery [52]
CHF5074 Flurbiprofen derivatives Chiesi Pharmaceuticals, Inc., USA WO015287A2(2011) Phase II [53]
E2012 2-piperidinone derivatives Schering Corp., USA US20110027264A1 Preclinical [54]
5a Bicyclic pyridinones Pfizer, Inc., USA WO2012131539 A1 Discovery [55]
6a Tetrasubstituted benzenes Envivo Pharmaceuticals, Inc., USA US20130165486 A1 Discovery [56]