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 T32880 Target Info
Target Name HIF-prolyl hydroxylase 2 (HPH-2)
Synonyms SM-20; Prolyl hydroxylase domain-containing protein 2; PHD2; Hypoxia-inducible factor prolyl hydroxylase 2; HPH-2; HIF-PH2; Egl nine homolog 1; C1orf12
Target Type Patented-recorded Target
Gene Name EGLN1
Biochemical Class Paired donor oxygen oxidoreductase
UniProt ID
EGLN1_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
United States Patent and Trademark Office (USPTO)
Patent ID US9708269
Title Process for making isoquinoline compounds
Abstract The present invention relates to methods for making isoquinoline compounds and the intermediate compounds achieved thereby. Such compounds can be used to prepare compounds and compositions capable of decreasing HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
Applicant(s) FibroGen, Inc.
Representative Drug(s) D0LO2C Drug Info IC50 = 2200 nM Click to Show More [1]
2 D0D8AV Drug Info IC50 = 3500 nM [1]
Patent ID US9708269
Title Process for making isoquinoline compounds
Abstract The present invention relates to methods for making isoquinoline compounds and the intermediate compounds achieved thereby. Such compounds can be used to prepare compounds and compositions capable of decreasing HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
Applicant(s) FibroGen, Inc.
Representative Drug(s) D0LO2C Drug Info IC50 = 2200 nM Click to Show More [1]
2 D0D8AV Drug Info IC50 = 3500 nM [1]
Patent ID US9708269
Title Process for making isoquinoline compounds
Abstract The present invention relates to methods for making isoquinoline compounds and the intermediate compounds achieved thereby. Such compounds can be used to prepare compounds and compositions capable of decreasing HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
Applicant(s) FibroGen, Inc.
Representative Drug(s) D0LO2C Drug Info IC50 = 2200 nM Click to Show More [1]
2 D0D8AV Drug Info IC50 = 3500 nM [1]
Patent ID US9695170
Title Naphthyridine derivatives as inhibitors of Hypoxia inducible factor (HIF) hydroxylase
Abstract The present disclosure relates to novel compounds, methods, and compositions capable of inhibiting HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
Applicant(s) FibroGen, Inc.
Representative Drug(s) D04YMG Drug Info IC50 = 630 nM Click to Show More [2]
2 D02IRO Drug Info IC50 = 12000 nM [2]
Patent ID US9695170
Title Naphthyridine derivatives as inhibitors of Hypoxia inducible factor (HIF) hydroxylase
Abstract The present disclosure relates to novel compounds, methods, and compositions capable of inhibiting HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
Applicant(s) FibroGen, Inc.
Representative Drug(s) D04YMG Drug Info IC50 = 630 nM Click to Show More [2]
2 D02IRO Drug Info IC50 = 12000 nM [2]
Patent ID US9695170
Title Naphthyridine derivatives as inhibitors of Hypoxia inducible factor (HIF) hydroxylase
Abstract The present disclosure relates to novel compounds, methods, and compositions capable of inhibiting HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
Applicant(s) FibroGen, Inc.
Representative Drug(s) D04YMG Drug Info IC50 = 630 nM Click to Show More [2]
2 D02IRO Drug Info IC50 = 12000 nM [2]
Patent ID US9598370
Title Prolyl hydroxylase inhibitors and methods of use
Abstract The present disclosure relates to HIF-1 prolyl hydroxylase inhibitors, compositions which comprise the HIF-1 prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.
Applicant(s) Akebia Therapeutics, Inc.
Representative Drug(s) D00ECX Drug Info IC50 = 3700 nM [3]
Patent ID US9422240
Title Partially saturated nitrogen-containing heterocyclic compound
Abstract There are provided compounds having a superior PHD2 inhibitory effect that are represented by general formula (I): (in the above-mentioned general formula (I),W, Y, R2, R3, R4, and Y4 are as described hereinabove), or pharmaceutically acceptable salts thereof.
Applicant(s) TAISHO PHARMACEUTICAL CO., LTD
Representative Drug(s) D0L9XU Drug Info IC50 = 61 nM Click to Show More [4]
2 D05EHX Drug Info IC50 = 77 nM [4]
3 D00CAO Drug Info IC50 = 79 nM [4]
4 D0K5UR Drug Info IC50 = 89 nM [4]
Patent ID US9422240
Title Partially saturated nitrogen-containing heterocyclic compound
Abstract There are provided compounds having a superior PHD2 inhibitory effect that are represented by general formula (I): (in the above-mentioned general formula (I),W, Y, R2, R3, R4, and Y4 are as described hereinabove), or pharmaceutically acceptable salts thereof.
Applicant(s) TAISHO PHARMACEUTICAL CO., LTD
Representative Drug(s) D0L9XU Drug Info IC50 = 61 nM Click to Show More [4]
2 D05EHX Drug Info IC50 = 77 nM [4]
3 D00CAO Drug Info IC50 = 79 nM [4]
4 D0K5UR Drug Info IC50 = 89 nM [4]
Patent ID US9422240
Title Partially saturated nitrogen-containing heterocyclic compound
Abstract There are provided compounds having a superior PHD2 inhibitory effect that are represented by general formula (I): (in the above-mentioned general formula (I),W, Y, R2, R3, R4, and Y4 are as described hereinabove), or pharmaceutically acceptable salts thereof.
Applicant(s) TAISHO PHARMACEUTICAL CO., LTD
Representative Drug(s) D0L9XU Drug Info IC50 = 61 nM Click to Show More [4]
2 D05EHX Drug Info IC50 = 77 nM [4]
3 D00CAO Drug Info IC50 = 79 nM [4]
4 D0K5UR Drug Info IC50 = 89 nM [4]
Patent ID US9422240
Title Partially saturated nitrogen-containing heterocyclic compound
Abstract There are provided compounds having a superior PHD2 inhibitory effect that are represented by general formula (I): (in the above-mentioned general formula (I),W, Y, R2, R3, R4, and Y4 are as described hereinabove), or pharmaceutically acceptable salts thereof.
Applicant(s) TAISHO PHARMACEUTICAL CO., LTD
Representative Drug(s) D0L9XU Drug Info IC50 = 61 nM Click to Show More [4]
2 D05EHX Drug Info IC50 = 77 nM [4]
3 D00CAO Drug Info IC50 = 79 nM [4]
4 D0K5UR Drug Info IC50 = 89 nM [4]
Patent ID US9409892
Title 4-hydroxy-isoquinoline compounds as HIF hydroxylase inhibitors
Abstract The present invention relates to novel compounds of formula (I), and compositions capable of inhibiting PHD1 enzyme activity selectively over other isoforms, for example, PHD2 and/or PHD3 enzymes. The invention also relates to compounds of formula (I) for use in disorders such as muscle degeneration, colitis, IBD, and certain ischemias.
Applicant(s) FibroGen, Inc.
Representative Drug(s) D0R4CX Drug Info IC50 = 860 nM Click to Show More [5]
2 D0SM8Z Drug Info IC50 = 24480 nM [5]
Patent ID US9409892
Title 4-hydroxy-isoquinoline compounds as HIF hydroxylase inhibitors
Abstract The present invention relates to novel compounds of formula (I), and compositions capable of inhibiting PHD1 enzyme activity selectively over other isoforms, for example, PHD2 and/or PHD3 enzymes. The invention also relates to compounds of formula (I) for use in disorders such as muscle degeneration, colitis, IBD, and certain ischemias.
Applicant(s) FibroGen, Inc.
Representative Drug(s) D0R4CX Drug Info IC50 = 860 nM Click to Show More [5]
2 D0SM8Z Drug Info IC50 = 24480 nM [5]
Patent ID US9409892
Title 4-hydroxy-isoquinoline compounds as HIF hydroxylase inhibitors
Abstract The present invention relates to novel compounds of formula (I), and compositions capable of inhibiting PHD1 enzyme activity selectively over other isoforms, for example, PHD2 and/or PHD3 enzymes. The invention also relates to compounds of formula (I) for use in disorders such as muscle degeneration, colitis, IBD, and certain ischemias.
Applicant(s) FibroGen, Inc.
Representative Drug(s) D0R4CX Drug Info IC50 = 860 nM Click to Show More [5]
2 D0SM8Z Drug Info IC50 = 24480 nM [5]
Patent ID US9409892
Title 4-hydroxy-isoquinoline compounds as HIF hydroxylase inhibitors
Abstract The present invention relates to novel compounds of formula (I), and compositions capable of inhibiting PHD1 enzyme activity selectively over other isoforms, for example, PHD2 and/or PHD3 enzymes. The invention also relates to compounds of formula (I) for use in disorders such as muscle degeneration, colitis, IBD, and certain ischemias.
Applicant(s) FibroGen, Inc.
Representative Drug(s) D0R4CX Drug Info IC50 = 860 nM Click to Show More [5]
2 D0SM8Z Drug Info IC50 = 24480 nM [5]
Patent ID US9340511
Title Process for making isoquinoline compounds
Abstract The present invention relates to methods for making isoquinoline compounds and the intermediate compounds achieved thereby. Such compounds can be used to prepare compounds and compositions capable of decreasing HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
Applicant(s) FibroGen, Inc.
Representative Drug(s) D0MS5W Drug Info IC50 = 5200 nM [6]
Patent ID US9115085
Title Crystalline forms of a prolyl hydroxylase inhibitor
Abstract The present disclosure relates to crystalline solid forms of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, the process of preparing the forms, and pharmaceutical compositions and methods of use thereof.
Applicant(s) FIBROGEN, INC.
Patent ID US8921389
Title Naphthyridine derivatives as inhibitors of hypoxia inducible factor (HIF) hydroxylase
Abstract The present disclosure relates to novel compounds, methods, and compositions capable of inhibiting HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
Applicant(s) Fibrogen, Inc.
Representative Drug(s) D0I4PX Drug Info IC50 = 10000 nM [8]
Patent ID US8921389
Title Naphthyridine derivatives as inhibitors of hypoxia inducible factor (HIF) hydroxylase
Abstract The present disclosure relates to novel compounds, methods, and compositions capable of inhibiting HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
Applicant(s) Fibrogen, Inc.
Representative Drug(s) D0I4PX Drug Info IC50 = 10000 nM [8]
Patent ID US8778412
Title Methods for increasing the stabilization of hypoxia inducible factor-1 alpha
Abstract Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1 prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1.
Applicant(s) Aerpio Therapeutics Inc.
Representative Drug(s) D01PPR Drug Info IC50 = 11000 nM [9]
Patent ID US8722895
Title Prolyl hydroxylase inhibitors and method of use
Abstract The present disclosure relates to HIF-1 prolyl hydroxylase inhibitors, compositions which comprise the HIF-1 prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.
Applicant(s) Akebia Therapeutics, Inc.
Representative Drug(s) D00XHH Drug Info IC50 = 3700 nM [10]
Patent ID US8598210
Title Prolyl hydroxylase inhibitors and methods of use
Abstract The present disclosure relates to HIF-1 prolyl hydroxylase inhibitors, compositions which comprise the HIF-1 prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.
Applicant(s) Akebia Therapeutics, Inc.
Representative Drug(s) D01XZT Drug Info IC50 = 650 nM Click to Show More [11]
2 D0Q9AF Drug Info IC50 = 2800 nM [11]
Patent ID US8598210
Title Prolyl hydroxylase inhibitors and methods of use
Abstract The present disclosure relates to HIF-1 prolyl hydroxylase inhibitors, compositions which comprise the HIF-1 prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.
Applicant(s) Akebia Therapeutics, Inc.
Representative Drug(s) D01XZT Drug Info IC50 = 650 nM Click to Show More [11]
2 D0Q9AF Drug Info IC50 = 2800 nM [11]
Patent ID US8536181
Title Prolyl hydroxylase inhibitors
Abstract Disclosed herein are prolyl hydroxylase inhibitors that can stabilize hypoxia inducible factor-1 alpha (HIF-1), as well as hypoxia inducible factor-2 (HIF-2). Also disclosed herein are pharmaceutical compositions comprising one or more of the disclosed compounds. Yet further disclosed are methods for stimulating the cellular immune response in a mammal such as increasing phagocytosis, for example, prolonging the life of phagocytes, inter alia, kerotyiocytes, neutrophils. As such the disclosed compounds provide methods for treating diseases that relate to the body's immune response.
Applicant(s) Aerpio Therapeutics Inc.
Representative Drug(s) D0HN5O Drug Info IC50 = 12000 nM Click to Show More [12]
2 D03PGC Drug Info IC50 = 12000 nM [12]
3 D00IKR Drug Info IC50 = 14000 nM [12]
Patent ID US8536181
Title Prolyl hydroxylase inhibitors
Abstract Disclosed herein are prolyl hydroxylase inhibitors that can stabilize hypoxia inducible factor-1 alpha (HIF-1), as well as hypoxia inducible factor-2 (HIF-2). Also disclosed herein are pharmaceutical compositions comprising one or more of the disclosed compounds. Yet further disclosed are methods for stimulating the cellular immune response in a mammal such as increasing phagocytosis, for example, prolonging the life of phagocytes, inter alia, kerotyiocytes, neutrophils. As such the disclosed compounds provide methods for treating diseases that relate to the body's immune response.
Applicant(s) Aerpio Therapeutics Inc.
Representative Drug(s) D0HN5O Drug Info IC50 = 12000 nM Click to Show More [12]
2 D03PGC Drug Info IC50 = 12000 nM [12]
3 D00IKR Drug Info IC50 = 14000 nM [12]
Patent ID US8536181
Title Prolyl hydroxylase inhibitors
Abstract Disclosed herein are prolyl hydroxylase inhibitors that can stabilize hypoxia inducible factor-1 alpha (HIF-1), as well as hypoxia inducible factor-2 (HIF-2). Also disclosed herein are pharmaceutical compositions comprising one or more of the disclosed compounds. Yet further disclosed are methods for stimulating the cellular immune response in a mammal such as increasing phagocytosis, for example, prolonging the life of phagocytes, inter alia, kerotyiocytes, neutrophils. As such the disclosed compounds provide methods for treating diseases that relate to the body's immune response.
Applicant(s) Aerpio Therapeutics Inc.
Representative Drug(s) D0HN5O Drug Info IC50 = 12000 nM Click to Show More [12]
2 D03PGC Drug Info IC50 = 12000 nM [12]
3 D00IKR Drug Info IC50 = 14000 nM [12]
Patent ID US10149841
Title Compound of 3-hydroxyl pyridine, preparation method thereof and pharmaceutical use thereof
Abstract A compound of the following formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently H; R3 is selected from H, a C1-C7 straight-chain, and a branched or cyclic alkyl; and R4, R5, R6, R7, and R8 are each independently selected from C1-C7 alkyl, halo C1-C7 alkyl and the like. Also provided is a method for preparing the compound, pharmaceutical compositions including the compound or pharmaceutically acceptable salts thereof, and uses of the compound or pharmaceutically acceptable salt thereof in the preparation of a medicine for inhibiting HIF prolyl hydroxylase or a medicine for promoting the generation of endogenous EPO.
Applicant(s) SHENYANG SUNSHINE PHARMACEUTICAL CO. LTD.
Representative Drug(s) D0QI0J Drug Info IC50 = 15000 nM Click to Show More [13]
2 D0F0DX Drug Info IC50 = 63000 nM [13]
3 D0JR2Q Drug Info IC50 = 84000 nM [13]
4 D0OR4X Drug Info IC50 = 237000 nM [13]
Patent ID US10149841
Title Compound of 3-hydroxyl pyridine, preparation method thereof and pharmaceutical use thereof
Abstract A compound of the following formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently H; R3 is selected from H, a C1-C7 straight-chain, and a branched or cyclic alkyl; and R4, R5, R6, R7, and R8 are each independently selected from C1-C7 alkyl, halo C1-C7 alkyl and the like. Also provided is a method for preparing the compound, pharmaceutical compositions including the compound or pharmaceutically acceptable salts thereof, and uses of the compound or pharmaceutically acceptable salt thereof in the preparation of a medicine for inhibiting HIF prolyl hydroxylase or a medicine for promoting the generation of endogenous EPO.
Applicant(s) SHENYANG SUNSHINE PHARMACEUTICAL CO. LTD.
Representative Drug(s) D0QI0J Drug Info IC50 = 15000 nM Click to Show More [13]
2 D0F0DX Drug Info IC50 = 63000 nM [13]
3 D0JR2Q Drug Info IC50 = 84000 nM [13]
4 D0OR4X Drug Info IC50 = 237000 nM [13]
Patent ID US10149841
Title Compound of 3-hydroxyl pyridine, preparation method thereof and pharmaceutical use thereof
Abstract A compound of the following formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently H; R3 is selected from H, a C1-C7 straight-chain, and a branched or cyclic alkyl; and R4, R5, R6, R7, and R8 are each independently selected from C1-C7 alkyl, halo C1-C7 alkyl and the like. Also provided is a method for preparing the compound, pharmaceutical compositions including the compound or pharmaceutically acceptable salts thereof, and uses of the compound or pharmaceutically acceptable salt thereof in the preparation of a medicine for inhibiting HIF prolyl hydroxylase or a medicine for promoting the generation of endogenous EPO.
Applicant(s) SHENYANG SUNSHINE PHARMACEUTICAL CO. LTD.
Representative Drug(s) D0QI0J Drug Info IC50 = 15000 nM Click to Show More [13]
2 D0F0DX Drug Info IC50 = 63000 nM [13]
3 D0JR2Q Drug Info IC50 = 84000 nM [13]
4 D0OR4X Drug Info IC50 = 237000 nM [13]
Patent ID US10149841
Title Compound of 3-hydroxyl pyridine, preparation method thereof and pharmaceutical use thereof
Abstract A compound of the following formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently H; R3 is selected from H, a C1-C7 straight-chain, and a branched or cyclic alkyl; and R4, R5, R6, R7, and R8 are each independently selected from C1-C7 alkyl, halo C1-C7 alkyl and the like. Also provided is a method for preparing the compound, pharmaceutical compositions including the compound or pharmaceutically acceptable salts thereof, and uses of the compound or pharmaceutically acceptable salt thereof in the preparation of a medicine for inhibiting HIF prolyl hydroxylase or a medicine for promoting the generation of endogenous EPO.
Applicant(s) SHENYANG SUNSHINE PHARMACEUTICAL CO. LTD.
Representative Drug(s) D0QI0J Drug Info IC50 = 15000 nM Click to Show More [13]
2 D0F0DX Drug Info IC50 = 63000 nM [13]
3 D0JR2Q Drug Info IC50 = 84000 nM [13]
4 D0OR4X Drug Info IC50 = 237000 nM [13]
Patent ID US10100051
Title Compound of 5-hydroxyl-1,7-naphthyridine substituted by aryloxy or heteroaryloxy, preparation method thereof and pharmaceutical use thereof
Abstract A compound of 5-hydroxyl-1,7-naphthyridine substituted by aryloxy or heteroaryloxy, a preparation method thereof and a pharmaceutical use thereof are provided. In particular, the compound has the following Formula (I), wherein R2 and R3 are each independently H; R1 is H or C1-C3 alkyl; Ar is an aromatic ring or a heteroaromatic ring selected from a naphthalene ring, a pyridine ring, a thiophene ring, a furan ring and a substituted benzene ring. Pharmaceutically acceptable salts of the present compound, are provided, as well as uses of the compound or pharmaceutically acceptable salts thereof in the preparation of a medicine for inhibiting HIF prolyl hydroxylase or a medicine for promoting the generation of endogenous EPO.
Applicant(s) SHENYANG SUNSHINE PHARMACEUTICAL CO. LTD.
Representative Drug(s) D05TTX Drug Info IC50 = 330 nM Click to Show More [14]
2 D05FDR Drug Info IC50 = 33000 nM [14]
3 D04BTN Drug Info IC50 = 73000 nM [14]
Patent ID US10100051
Title Compound of 5-hydroxyl-1,7-naphthyridine substituted by aryloxy or heteroaryloxy, preparation method thereof and pharmaceutical use thereof
Abstract A compound of 5-hydroxyl-1,7-naphthyridine substituted by aryloxy or heteroaryloxy, a preparation method thereof and a pharmaceutical use thereof are provided. In particular, the compound has the following Formula (I), wherein R2 and R3 are each independently H; R1 is H or C1-C3 alkyl; Ar is an aromatic ring or a heteroaromatic ring selected from a naphthalene ring, a pyridine ring, a thiophene ring, a furan ring and a substituted benzene ring. Pharmaceutically acceptable salts of the present compound, are provided, as well as uses of the compound or pharmaceutically acceptable salts thereof in the preparation of a medicine for inhibiting HIF prolyl hydroxylase or a medicine for promoting the generation of endogenous EPO.
Applicant(s) SHENYANG SUNSHINE PHARMACEUTICAL CO. LTD.
Representative Drug(s) D05TTX Drug Info IC50 = 330 nM Click to Show More [14]
2 D05FDR Drug Info IC50 = 33000 nM [14]
3 D04BTN Drug Info IC50 = 73000 nM [14]
Patent ID US10100051
Title Compound of 5-hydroxyl-1,7-naphthyridine substituted by aryloxy or heteroaryloxy, preparation method thereof and pharmaceutical use thereof
Abstract A compound of 5-hydroxyl-1,7-naphthyridine substituted by aryloxy or heteroaryloxy, a preparation method thereof and a pharmaceutical use thereof are provided. In particular, the compound has the following Formula (I), wherein R2 and R3 are each independently H; R1 is H or C1-C3 alkyl; Ar is an aromatic ring or a heteroaromatic ring selected from a naphthalene ring, a pyridine ring, a thiophene ring, a furan ring and a substituted benzene ring. Pharmaceutically acceptable salts of the present compound, are provided, as well as uses of the compound or pharmaceutically acceptable salts thereof in the preparation of a medicine for inhibiting HIF prolyl hydroxylase or a medicine for promoting the generation of endogenous EPO.
Applicant(s) SHENYANG SUNSHINE PHARMACEUTICAL CO. LTD.
Representative Drug(s) D05TTX Drug Info IC50 = 330 nM Click to Show More [14]
2 D05FDR Drug Info IC50 = 33000 nM [14]
3 D04BTN Drug Info IC50 = 73000 nM [14]
Patent ID US10100051
Title Compound of 5-hydroxyl-1,7-naphthyridine substituted by aryloxy or heteroaryloxy, preparation method thereof and pharmaceutical use thereof
Abstract A compound of 5-hydroxyl-1,7-naphthyridine substituted by aryloxy or heteroaryloxy, a preparation method thereof and a pharmaceutical use thereof are provided. In particular, the compound has the following Formula (I), wherein R2 and R3 are each independently H; R1 is H or C1-C3 alkyl; Ar is an aromatic ring or a heteroaromatic ring selected from a naphthalene ring, a pyridine ring, a thiophene ring, a furan ring and a substituted benzene ring. Pharmaceutically acceptable salts of the present compound, are provided, as well as uses of the compound or pharmaceutically acceptable salts thereof in the preparation of a medicine for inhibiting HIF prolyl hydroxylase or a medicine for promoting the generation of endogenous EPO.
Applicant(s) SHENYANG SUNSHINE PHARMACEUTICAL CO. LTD.
Representative Drug(s) D05TTX Drug Info IC50 = 330 nM Click to Show More [14]
2 D05FDR Drug Info IC50 = 33000 nM [14]
3 D04BTN Drug Info IC50 = 73000 nM [14]
References  Top
REF 1 Process for making isoquinoline compounds. US9708269.
REF 2 Naphthyridine derivatives as inhibitors of Hypoxia inducible factor (HIF) hydroxylase. US9695170.
REF 3 Prolyl hydroxylase inhibitors and methods of use. US9598370.
REF 4 Partially saturated nitrogen-containing heterocyclic compound. US9422240.
REF 5 4-hydroxy-isoquinoline compounds as HIF hydroxylase inhibitors. US9409892.
REF 6 Process for making isoquinoline compounds. US9340511.
REF 7 Crystalline forms of a prolyl hydroxylase inhibitor. US9115085.
REF 8 Naphthyridine derivatives as inhibitors of hypoxia inducible factor (HIF) hydroxylase. US8921389.
REF 9 Methods for increasing the stabilization of hypoxia inducible factor-1 alpha. US8778412.
REF 10 Prolyl hydroxylase inhibitors and method of use. US8722895.
REF 11 Prolyl hydroxylase inhibitors and methods of use. US8598210.
REF 12 Prolyl hydroxylase inhibitors. US8536181.
REF 13 Compound of 3-hydroxyl pyridine, preparation method thereof and pharmaceutical use thereof. US10149841.
REF 14 Compound of 5-hydroxyl-1,7-naphthyridine substituted by aryloxy or heteroaryloxy, preparation method thereof and pharmaceutical use thereof. US10100051.

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