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 T01003 Target Info
Target Name Endoplasmic reticulum to nucleus signaling 1 (ERN1)
Synonyms Serine/threonine-protein kinase/endoribonuclease IRE1; Ire1-alpha; IRE1a; IRE1; Inositol-requiring protein 1; hIRE1p; Endoplasmic reticulum-to-nucleus signaling 1
Target Type Clinical trial Target
Gene Name ERN1
Biochemical Class Kinase
UniProt ID
ERN1_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
United States Patent and Trademark Office (USPTO)
Patent ID US9693992
Title IRE-1 inhibitors
Abstract Compounds which directly inhibit IRE-1 activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
Applicant(s) MannKind Corporation
Representative Drug(s) D0M2TO Drug Info IC50 < 100nM [1]
Patent ID US9493435
Title IRE-1 inhibitors
Abstract The invention provides compounds which directly inhibit IRE-1 activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
Applicant(s) MannKing Corporation
Representative Drug(s) D0GK1K Drug Info IC50 < 1000nM Click to Show More [2]
2 D0TA9C Drug Info IC50 < 1000nM [2]
3 D0XX5N Drug Info IC50 < 1000nM [2]
Patent ID US9493435
Title IRE-1 inhibitors
Abstract The invention provides compounds which directly inhibit IRE-1 activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
Applicant(s) MannKing Corporation
Representative Drug(s) D0GK1K Drug Info IC50 < 1000nM Click to Show More [2]
2 D0TA9C Drug Info IC50 < 1000nM [2]
3 D0XX5N Drug Info IC50 < 1000nM [2]
Patent ID US9493435
Title IRE-1 inhibitors
Abstract The invention provides compounds which directly inhibit IRE-1 activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
Applicant(s) MannKing Corporation
Representative Drug(s) D0GK1K Drug Info IC50 < 1000nM Click to Show More [2]
2 D0TA9C Drug Info IC50 < 1000nM [2]
3 D0XX5N Drug Info IC50 < 1000nM [2]
Patent ID US9241942
Title IRE-1 inhibitors
Abstract Compounds which directly inhibit IRE-1 activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
Applicant(s) MannKind Corporation
Representative Drug(s) D0AV6X Drug Info IC50 = 5665 nM [3]
Patent ID US9040714
Title IRE-1 inhibitors
Abstract Compounds which directly inhibit IRE-1 activity in vitro, prodrugs, and pharmaceutically acceptable salts there-of. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
Applicant(s) MannKind Corporation
Representative Drug(s) D0KF0D Drug Info IC50 < 100nM Click to Show More [4]
2 D00OUG Drug Info IC50 < 100nM [4]
3 D0ZP0G Drug Info IC50 < 1000nM [4]
Patent ID US9040714
Title IRE-1 inhibitors
Abstract Compounds which directly inhibit IRE-1 activity in vitro, prodrugs, and pharmaceutically acceptable salts there-of. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
Applicant(s) MannKind Corporation
Representative Drug(s) D0KF0D Drug Info IC50 < 100nM Click to Show More [4]
2 D00OUG Drug Info IC50 < 100nM [4]
3 D0ZP0G Drug Info IC50 < 1000nM [4]
Patent ID US9040714
Title IRE-1 inhibitors
Abstract Compounds which directly inhibit IRE-1 activity in vitro, prodrugs, and pharmaceutically acceptable salts there-of. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
Applicant(s) MannKind Corporation
Representative Drug(s) D0KF0D Drug Info IC50 < 100nM Click to Show More [4]
2 D00OUG Drug Info IC50 < 100nM [4]
3 D0ZP0G Drug Info IC50 < 1000nM [4]
Patent ID US8614253
Title IRE-1 inhibitors
Abstract Compounds which directly inhibit IRE-1 activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
Applicant(s) MannKind Corporation
Representative Drug(s) D01UPA Drug Info IC50 = 30 nM Click to Show More [5]
2 D0VP7R Drug Info IC50 = 170 nM [5]
3 D0DV4H Drug Info IC50 = 3797 nM [5]
Patent ID US8614253
Title IRE-1 inhibitors
Abstract Compounds which directly inhibit IRE-1 activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
Applicant(s) MannKind Corporation
Representative Drug(s) D01UPA Drug Info IC50 = 30 nM Click to Show More [5]
2 D0VP7R Drug Info IC50 = 170 nM [5]
3 D0DV4H Drug Info IC50 = 3797 nM [5]
Patent ID US8614253
Title IRE-1 inhibitors
Abstract Compounds which directly inhibit IRE-1 activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
Applicant(s) MannKind Corporation
Representative Drug(s) D01UPA Drug Info IC50 = 30 nM Click to Show More [5]
2 D0VP7R Drug Info IC50 = 170 nM [5]
3 D0DV4H Drug Info IC50 = 3797 nM [5]
References  Top
REF 1 IRE-1 inhibitors. US9693992.
REF 2 IRE-1 inhibitors. US9493435.
REF 3 IRE-1 inhibitors. US9241942.
REF 4 IRE-1 inhibitors. US9040714.
REF 5 IRE-1 inhibitors. US8614253.

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