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Title:
BIVALENT DIAZO BICYCLIC SMAC MIMETICS AND THE USES THEREOF
Document Type and Number:
WIPO Patent Application WO/2011/050068
Kind Code:
A3
Abstract:
The invention relates to diazo bicyclic Smac mimetics that are tethered through a covalent linker to give a bivalent species. Bivalent diazo bicyclic Smac mimetics function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs). The invention also relates to the use of bivalent diazo bicyclic Smac mimetics for inducing or sensitizing cells to the induction of apoptotic cell death. Thus, compounds of the invention are useful in the treatment, amelioration, or prevention of hyperproliferative diseases such as cancer.

Inventors:
WANG SHAOMENG (US)
SUN HAIYING (US)
Application Number:
PCT/US2010/053384
Publication Date:
September 29, 2011
Filing Date:
October 20, 2010
Export Citation:
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Assignee:
UNIV MICHIGAN (US)
WANG SHAOMENG (US)
SUN HAIYING (US)
International Classes:
C07D487/04; A61P35/00; C07D245/04; C07D403/14
Domestic Patent References:
WO2009126947A22009-10-15
WO2008128171A22008-10-23
Other References:
SUN, HAIYING ET AL.: "Design, Synthesis, and Characterization of a Potent, Nonpeptide, Cell-Permeable, Bivalent Smac Mimetic That Concurrently Targets Both the BIR2 and BIR3 Domains in XIAP.", J. AM. CHEM. SOC., vol. 129, 2007, pages 15279 - 15294
SUN, HAIYING ET AL.: "Design of Small-Molecule Peptidic and Nonpeptidic Smac Mimetics.", ACCOUNTS OF CHEMICAL RESEARCH, vol. 41, no. 10, October 2008 (2008-10-01), pages 1264 - 1277
PENG, YUEFENG ET AL.: "Potent, Orally Bioavailable Diazabicyclic Small- Molecule Mimetics of Second Mitochondria-Derived Activator of Caspases.", J. MED. CHEM., vol. 51, 2008, pages 8158 - 8162
SUN, HAIYING ET AL.: "Design, Synthesis, and Evaluation of a Potent, Cell- Permeable, Conformationally Second Mitochondria Derived Activator of Caspase (Smac) Mimetic.", J. MED. CHEM., vol. 49, 2006, pages 7916 - 7920
SUN, HAIYING ET AL.: "Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 15, 2005, pages 793 - 797
ZOBEL, KERRY ET AL.: "Design, Synthesis, and Biological Activity of a Potent Smac Mimetic That Sensitizes Cancer Cells to Apoptosis by Antagonizing IAPs.", ACS CHEMICAL BIOLOGY, vol. 1, no. 8, 2006, pages 525 - 533
SUN, HAIYING ET AL.: "Structure-Based Design of Potent, Conformationally Constrained Smac Mimetics.", J. AM. CHEM. SOC., vol. 126, 2004, pages 16686 - 16687
COSSU, FEDERICA ET AL.: "Designing Smac-mimetics as antagonists of XIAP, cIAPl, and cIAP2.", BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, vol. 378, 2009, pages 162 - 167
Attorney, Agent or Firm:
GOETZ, Robert A. (S.C.2275 Deming Way,Suite 31, Middleton Wisconsin, US)
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