Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T84780 Target Info
Target Name Cellular inhibitor of apoptosis 1 (BIRC2)
Synonyms hIAP2; hIAP-2; TNFR2TRAFsignaling complex protein 2; TNFR2-TRAF-signaling complex protein 2; RNF48; RING-type E3 ubiquitin transferase BIRC2; RING finger protein 48; MIHB; Inhibitor of apoptosis protein 2; IAP2; IAP homolog B; CIAP1; C-IAP1; Baculoviral IAP repeatcontaining protein 2; Baculoviral IAP repeat-containing protein 2; API1
Target Type Clinical trial Target
Gene Name BIRC2
Biochemical Class Acyltransferase
UniProt ID
BIRC2_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2010138496
Title Iap Inhibitors.
Abstract The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.
Applicant(s) Tetralogic Pharmaceuticals Corp
Representative Drug(s) D03PTG Drug Info KD < 100 nM Click to Show More [1]
2 D0CV9K Drug Info KD < 100 nM [1]
Patent ID WO2010033531
Title Iap Inhibitors.
Abstract The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.
Applicant(s) Tetralogic Pharmaceuticals Corp
Representative Drug(s) D0M3BY Drug Info KD < 100 nM Click to Show More [1]
2 D0MH4B Drug Info KD < 100 nM [1]
Patent ID WO2014060770
Title Bicyclic Heterocycle Compounds and Their Uses In Therapy.
Abstract The invention relates to new bicyclic heterocycle compounds of formula (I):,to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
Applicant(s) Astex Therapeutics Limited
Representative Drug(s) D0ID3R Drug Info 98% inhibition = 12 nM [1]
Patent ID WO2014060768
Title Bicyclic Heterocycle Compounds and Their Uses In Therapy.
Abstract The invention relates to new bicyclic heterocycle compounds of formula (I): wherein R1 is seected from specific pyrazolyl, imidazolyl, pridinyl and triazolyl groups. The invention also realtes to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
Applicant(s) ASTEX THERAPEUTICS LIMITED
Representative Drug(s) D02ZHC Drug Info 98% inhibition = 12 nM [1]
Patent ID WO2014060767
Title Bicyclic Heterocycle Compounds and Their Uses In Therapy.
Abstract The invention relates to new bicyclic heterocycle compounds of formula (I): (Formula (I)), pharmaceutical compositions comprising said compounds and to use of said compounds in the treatment of diseases, e.g. cancer.
Applicant(s) ASTEX THERAPEUTICS LIMITED
Representative Drug(s) D02UOD Drug Info 100% inhibition = 12 nM [1]
Patent ID WO2014031487
Title Bivalent Inhibitors of Iap Proteins and Therapeutic Methods Using The Same.
Abstract Inhibitors of IAP proteins and compositions containing the same are disclosed. Methods of using the IAP protein inhibitors in the treatment of diseases and conditions wherein inhibition of IAP proteins provides a benefit, like cancers, also are disclosed.
Applicant(s) THE REGENTS OF THE UNIVERSITY OF MICHIGAN
Representative Drug(s) D0YN1X Drug Info IC50 < 100 nM [1]
Patent ID WO2012080271
Title Dimeric Iap Inhibitors.
Abstract The present invention provides compounds of formula M-L-M' (where M and M' are each independently a monomeric moiety of Formula (I) and L is a linker). The dimeric compounds have been found to be effective in promoting apoptosis in rapidly dividing cells. (I).
Applicant(s) NOVARTIS AG STRAUB, Christopher Sean CHEN, Zhuoliang
Representative Drug(s) D0AC8H Drug Info EC50 = 1.2 nM [1]
Patent ID WO2012080260
Title Dimeric Iap Inhibitors.
Abstract The present invention provides compounds of formula M-L-M' (where M and M' are each independently a monomeric moiety of Formula (I), (II), (III) or (IV) and L is a linker). The dimeric compounds have been found to be effective in promoting apoptosis in rapidly dividing cells.
Applicant(s) NOVARTIS AG STRAUB, Christopher Sean CHEN, Zhuoliang
Representative Drug(s) D07FRU Drug Info EC50 = 0.9 nM [1]
Patent ID WO2011104266
Title Dimeric Iap Inhibitors.
Abstract The present invention provides compounds of formula M-L-M' (where M and M' are each independently a monomeric moiety of Formula (I) and L is a linker). The dimeric compounds have been found to be effective in promoting apoptosis in rapidly dividing cells.
Applicant(s) NOVARTIS AG STRAUB, Christopher Sean CHEN, Zhuoliang PALERMO, Mark G.
Representative Drug(s) D0GF3P Drug Info EC50 = 0.6 nM [1]
Patent ID WO2011098904
Title Iap Bir Domain Binding Compounds.
Abstract A compound of Formula 1 : (I) or salt thereof, as well as methods of making compounds of Formula 1, methods of using compounds of Formula 1 to treat proliferative disorders such as cancer, and related compounds, composition, and methods.
Applicant(s) Pharmascience Inc
Representative Drug(s) D0R3YM Drug Info Ki < 25 nM [1]
Patent ID WO2011082285
Title Ligand-Directed Covalent Modification of Protein.
Abstract The present invention relates to enzyme inhibitors. More specifically, the present invention relates to ligand-directed covalent modification of proteins; method of designing same; pharmaceutical formulation of same; and method of use.
Applicant(s) Avila Therapeutics, Inc
Representative Drug(s) D09VAX Drug Info Ki < 1000 nM [1]
Patent ID WO2011068926
Title Iap Inhibitors.
Abstract The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.
Applicant(s) Tetralogic Pharmaceuticals Corp
Representative Drug(s) D03VPP Drug Info KD < 100 nM [1]
Patent ID WO2011050068
Title Bivalent Diazo Bicyclic Smac Mimetics and The Uses Thereof.
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.
Applicant(s) The Regents of the University of Michigan
Representative Drug(s) D0HY5Q Drug Info IC50 < 10 nM [1]
Patent ID WO2011016576
Title Alanine Derivatives As Inhibitors of Apoptosis Proteins.
Abstract The present invention provides a compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof. The compound of the present invention shows a strong IAP antagonistic activity.
Applicant(s) TAKEDA PHARMACEUTICAL COMPANY LIMITED
Representative Drug(s) D08XOV Drug Info 100.50% inhibition = 3000 nM [1]
Patent ID WO2010142994
Title 2, 3-Dihydro-1H-Indene Compounds and Their Use To Treat Cancer.
Abstract Provided herein are 2,3-dihydro-1H-indene compounds, methods for making the compounds, pharmaceutical compositions containing the compounds. The described compounds inhibit IAP proteins and can be used to treat various cancers.
Applicant(s) Astrazeneca Ab
Representative Drug(s) D0B6KC Drug Info IC50 = 15 nM [1]
Patent ID WO2010138666
Title Iap Inhibitors.
Abstract The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.
Applicant(s) Tetralogic Pharmaceuticals Corp
Representative Drug(s) D03DQW Drug Info KD < 100 nM [1]
United States Patent and Trademark Office (USPTO)
Patent ID US20130225567
Title International Gmbh. 5-Alkynyl Pyridine.
Representative Drug(s) D0O8ZD Drug Info IC50 = 47 nM [1]
Japan Patent Office (JPO)
Patent ID JP2012176934
Title Heterocyclic Compounds As Iap (Inhibitors of Apoptosis Protein) Antagonists and Pharmaceuticals Containing Them.
Representative Drug(s) D05HBW Drug Info 99% inhibition = 3000 nM [1]
Patent ID JP2012106958
Title Heterocyclic Compounds, Pharmaceuticals Containing Them, Method for Antagonizing Inhibitors of Apoptosis Proteins By The Compounds, and Prevention or Treatment of Cancer Using Them.
Representative Drug(s) D0F4GT Drug Info 96% inhibition = 3000 nM [1]
References  Top
REF 1 Small molecule inhibitor of apoptosis proteins antagonists: a patent review.Expert Opin Ther Pat. 2015 Jul;25(7):755-74.

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