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 T16769 Target Info
Target Name X-linked inhibitor of apoptosis protein (XIAP)
Synonyms hILP; hIAP3; hIAP-3; Xlinked IAP; X-linked IAP; RING-type E3 ubiquitin transferase XIAP; Inhibitor of apoptosis protein 3; ILP; IAPlike protein; IAP3; IAP-like protein; IAP-3; E3 ubiquitinprotein ligase XIAP; E3 ubiquitin-protein ligase XIAP; Baculoviral IAP repeatcontaining protein 4; Baculoviral IAP repeat-containing protein 4; BIRC4; API3
Target Type Clinical trial Target
Gene Name XIAP
Biochemical Class Acyltransferase
UniProt ID
XIAP_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2014090709
Title Dimeric Compounds.
Abstract Disclosed are compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein Z, X, Q and R1 are as described in this application, and methods of using the compounds in the treatment of cancer.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0G9CR Drug Info IC50(BIR2) = 0.29 nM; IC50(BIR3) = 1900 nM Click to Show More [1]
2 D00VXV Drug Info IC50(BIR2) = 3.1 nM; IC50(BIR3) = 7.3 nM [1]
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 < 1000 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 WO2014085489
Title Inhibitor of Apoptosis Protein (Iap) Antagonists.
Abstract Provided herein are compounds that modulate the activity of inhibitor of apoptosis proteins (IAPs), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.
Applicant(s) SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTE
Representative Drug(s) D03JHD Drug Info Ki <= 25000 nM [1]
Patent ID WO2014074665
Title Macrocyclic Compounds for Inhibition of Inhibitors of Apoptosis.
Abstract There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
Applicant(s) Ensemble Therapeutics Corporation
Representative Drug(s) D01JEH Drug Info IC50(BIR2-3) = 1.1 nM; IC50(BIR3) = 4.9 nM [1]
Patent ID WO2014074658
Title Macrocyclic Compounds for Inhibition of Inhibitors of Apoptosis.
Abstract There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
Applicant(s) Ensemble Therapeutics Corporation
Representative Drug(s) D0S0XT Drug Info IC50(BIR2-3) = 57 nM; IC50(BIR3) = 80 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 54% inhibition = 40 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 IC50 = 91 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 94% inhibition = 40 nM [1]
Patent ID WO2014056871
Title Azaindolines.
Abstract Disclosed are compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein W, Y, Z, R1, R2, R3 and R4 are as described in this application, and methods of using the compounds in the treatment of cancer.
Applicant(s) F. HOFFMANN - LA ROCHE AG HOFFMANN - LA ROCHE INC.
Representative Drug(s) D0EZ9G Drug Info IC50 = 10 nM [1]
Patent ID WO2014055461
Title Iap Antagonists.
Abstract There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D08UPQ Drug Info IC50(BIR3) = 60 nM; IC50(BIR2) = 90 nM [1]
Patent ID WO2014047024
Title Iap Antagonists.
Abstract There are disclosed compounds of formula (I) that modulate the activity of inhibitors of apoptosis (lAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention. (Formula (I)).
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D03TQU Drug Info IC50(BIR2) = 45 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
Patent ID WO2014026882
Title Azaheterocycles As Bir2 and/or Bir3 Inhibitors.
Abstract Disclosed are compounds of Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, m, n and q are described in this application, and methods of using said compounds in the treatment of cancer.
Applicant(s) F. Hoffmann-La Roche Ag
Patent ID WO2014025759
Title Iap Antagonists.
Abstract There are disclosed compounds of formula (I) that modulate the activity of inhibitors of apoptosis (lAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing said compounds.
Applicant(s) BRISTOL-MYERS SQUIBB COMPANY
Representative Drug(s) D0K2PK Drug Info IC50(BIR3) = 60 nM; IC50(BIR2) = 220 nM [1]
Patent ID WO2014023708
Title Substituted Hetero-Azepinones.
Abstract There are provided compounds of the formula (1) wherein W, X, Y, Z, R1, R2, R3, R4, R5 and R6 are described herein. These compounds are useful for the treatment of proliferative diseases, including cancer.
Applicant(s) F. Hoffmann-La Roche Ag
Patent ID WO2014011712
Title Iap Antagonists.
Abstract There are disclosed compounds that modulate the activity of inhibitors of apoptosis (lAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
Applicant(s) BRISTOL-MYERS SQUIBB COMPANY
Representative Drug(s) D0Q1XF Drug Info IC50(BIR3)= 3 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 = 57 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 = 127 nM [1]
Patent ID WO2012030160
Title Quinoline or Quinazoline Derivatives with Apoptosis Inducing Activity On Cells.
Abstract Provided is a pharmaceutical composition comprising, as an active ingredient, a quinoline or quinazoline derivative of formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof, which is effective in the prevention and treatment of a cancer, inflammation, autoimmune diseases or neurodegenerative disorders which are induced by the overexpression of inhibitor of apoptosis proteins (IAPs).
Applicant(s) Hanmi Science Co., Ltd
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 = 60 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 < 250 nM [1]
Patent ID WO2011090317
Title Imidazopyrazinone Derivatives with Apoptosis Inducing Activity On Cells.
Abstract Provided is a pharmaceutical composition comprising, as an active ingredient, an imidazopyrazinone derivative of formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof, which is effective in the prevention and treatment of cancer, inflammation, autoimmune diseases and neurodegenerative disorders which are induced by the overexpression of inhibitor of apoptosis proteins (IAPs).
Applicant(s) HANMI HOLDINGS CO., LTD. BAE, In Hwan JUN, Mi Ae SONG, Ji Young JU, Hae Kyoung SONG, Tae Hun CHO, Ju Hyun KWEON, Eun Kyung AHN, Young Gil KIM, Cheol Kyung KIM, Maeng Sup
Representative Drug(s) D0PF7S Drug Info IC50 = 100 to 1000 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 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]
Patent ID WO2010021934
Title Azaindole Inhibitors of Iap.
Abstract The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: I wherein X1, X2, Y, Z1, Z2, Z3, Z4, R1, R2, R3, R3', R4, R4', R5, R6, R6' and R9 are as described herein.
Applicant(s) GENENTECH, INC. BERGERON, Philippe KOEHLER, Michael, FT
Representative Drug(s) D0P9PZ Drug Info Ki = 91 nM [1]
United States Patent and Trademark Office (USPTO)
Patent ID US20130338081
Title Iap Antagonists.
Representative Drug(s) D0NB0V Drug Info IC50(BIR2-3) = 3 nM; IC50(BIR3) = 11 nM [1]
Patent ID US20130225567
Title International Gmbh. 5-Alkynyl Pyridine.
Representative Drug(s) D0O8ZD Drug Info IC50 = 1 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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