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 T89697 Target Info
Target Name Indoleamine 2,3-dioxygenase 1 (IDO1)
Synonyms Indoleamine-pyrrole 2,3-dioxygenase; INDO; IDO-1; IDO
Target Type Successful Target
Gene Name IDO1
Biochemical Class Oxygenase
UniProt ID
I23O1_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2017134555
Title Derivatives of Pyrroloimidazole or Analogues Thereof Which Are Useful for The Treatment of Inter Alia Cancer.
Abstract Present invention relates to novel heterocyclic compounds as indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) modulators. Compounds of the present invention inhibit tryptophan degradation by modulating IDO and/or TDO. Formula (I) The invention further relates to the process of their preparation, pharmaceutical composition and their use in modulating the activity of indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3- dioxygenase (TDO). The compounds of the invention can be used alone or in combination for the treatment of conditions that benefits from the inhibition of tryptophan degradation.
Applicant(s) EMCURE PHARMACEUTICALS LIMITED
Representative Drug(s) D03CTR Drug Info IC50 < 500 nM Click to Show More [1]
2 D0R0QY Drug Info IC50 < 500 nM [1]
Patent ID WO2017034420
Title Inhibitors of Tryptophan Dioxygenases (Ido1 and Tdo) and Their Use In Therapy.
Abstract Pharmaceutical compositions comprising 3-aminoisoxazolopyridine compounds of the Formula I having IDO1 and/or TDO inhibitory activity are described, where W is CR1, N or N-oxide; X is CR2, N or N-oxide; Y is CR3, N or N-oxide; Z is CR4, N or N-oxide; and at least one of W, X, Y, and Z is N or N-oxide; and R9 and R10 are as defined. Also described are methods of using such compounds in the treatment of various conditions, such as cancer.
Applicant(s) AUCKLAND UNISERVICES LIMITED
Representative Drug(s) D0DW4P Drug Info IC50 < 1000 nM Click to Show More [1]
2 D0L8KM Drug Info IC50 < 1000 nM [1]
Patent ID WO2017024996
Title Hydroxy Amidine Derivative, Preparation Method and Use In Medicine Thereof.
Abstract Provided are a hydroxy amidine derivative, a preparation method and a use in medicine thereof. In particular, provided are the hydroxy amidine derivative as shown by general formula (I), the preparati.
Applicant(s) Jiangsu Hengrui Medicine Co., Ltd
Representative Drug(s) D05BYE Drug Info IC50 = 2 nM Click to Show More [1]
2 D05QAL Drug Info IC50 = 4 nM [1]
Patent ID WO2017007700
Title Pharmaceutical Compound.
Abstract Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the general formula (I) detailed within.
Applicant(s) IOMET PHARMA LTD. MERCK SHARP & DOHME CORP. COWLEY, Phillip, M. WISE, Alan BROWN, Thomas, J. MCGOWAN, Meredeth, A. ZHOU, Hua HAN, Yongxin
Representative Drug(s) D0K8EV Drug Info IC50 < 1000 nM Click to Show More [1]
2 D0L9BG Drug Info IC50 < 1000 nM [1]
Patent ID WO2016210414
Title Ido Inhibitors.
Abstract There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
Applicant(s) BRISTOL-MYERS SQUIBB COMPANY
Representative Drug(s) D0F3VN Drug Info IC50 < 5 nM Click to Show More [1]
2 D0K4KM Drug Info IC50 < 5 nM [1]
Patent ID WO2016165613
Title Heterocycles Useful As Ido and Tdo Inhibitors.
Abstract Provided are compounds of Formula (I) shown below using for treatment of diseases or disorders mediated by IDO and/or TDO, pharmaceutical compositions and methods of preparation thereof.
Applicant(s) Hangzhou Innogate Pharma Co., Ltd
Representative Drug(s) D03PQB Drug Info IC50 < 100 nM Click to Show More [1]
2 D09TSM Drug Info IC50 < 100 nM [1]
Patent ID WO2016161960
Title Novel 5 or 8-Substituted Imidazo [1, 5-A] Pyridines As Indoleamine and/or Tryptophane 2, 3-Dioxygenases.
Abstract Disclosed herein are 5 or 8-substituted imidazo[l,5-a]pyridines and pharmaceutical compositions comprising at least one such 5 or 8-substituted imidazo[l,5-a]pyridines, processes for the preparation thereof, and the use thereof in therapy. Disclosed herein are certain 5 or 8- substituted imidazo[l,5-a]pyridines that can be useful for inhibiting indoleamine 2,3- dioxygenase and/or tryptophane 2,3-dioxygenase and for treating diseases or disorders mediated thereby.
Applicant(s) BEIGENE, LTD. WANG, Hexiang
Representative Drug(s) D0ZV6F Drug Info IC50 = 9.6 nM Click to Show More [1]
2 D0RH9K Drug Info IC50 = 78 nM [1]
Patent ID WO2016161286
Title Inhibitors of Indoleamine 2,3-Dioxygenase for The Treatment of Cancer.
Abstract There are disclosed compounds of formula (I) that modulate or inhibit the enzymatic activity of indoleamine-2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D03NHO Drug Info IC50 < 5 nM Click to Show More [1]
2 D0GV6B Drug Info IC50 < 5 nM [1]
Patent ID WO2016161279
Title Inhibitors of Indoleamine 2,3-Dioxygenase for The Treatment of Cancer.
Abstract There are disclosed compounds of formula (I) that modulate or inhibit the enzymatic activity of indoleamine-2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
Applicant(s) BRISTOL-MYERS SQUIBB COMPANY
Representative Drug(s) D03NHO Drug Info IC50 < 5 nM Click to Show More [1]
2 D0GV6B Drug Info IC50 < 5 nM [1]
Patent ID WO2016161269
Title Inhibitors of Indoleamine 2,3-Dioxygenase for The Treatment of Cancer.
Abstract There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
Applicant(s) BRISTOL-MYERS SQUIBB COMPANY
Representative Drug(s) D03NHO Drug Info IC50 < 5 nM Click to Show More [1]
2 D0GV6B Drug Info IC50 < 5 nM [1]
Patent ID WO2016059412
Title 6,7-Heterocyclic Fused 5H-Pyrrolo[1,2-C]Imidazole Derivatives and Their Use As Indoleamine 2,3-Dioxygenase (Ido) and/or Tryptophan 2,3-Dioxygenase (Td02) Modulators.
Abstract This invention relates to novel compounds of formula (I) wherein 'A' is a 5 or 6 membered heteroaryl group, unsubstituted or substituted with 1, 2 or 3 groups as defined in claim 1; X is a bond or -(CRA1RB1)n-; Y is selected from: a bond, -(CRDRE)m-, -O-, -NRF, -S-, -C(O)-, -C(NRF) -, -C(ORF)Rc-, -C(NRFRG)RC-, -C(O)NRF, -NRFC(O)-, -NRFC(O)NRG-, - NRFSO2NRG-, -SO2-, -SO2NRF-, -NRFSO2-, -OC(O)- and -C(O)O-; Z is a bond or -(CRA2RB2)k-; wherein m, n and k are each independently selected from 1, 2, 3 and 4; R1 is H or a 3 to 16 membered fully saturated, partially unsaturated or aromatic mono-, di- or tri-cyclic moiety, which optionally may include 1, 2 or 3 heteroatoms selected from O, N and S, and which is unsubstituted or substituted with 1 to 5 substituents as defined in claim 1; R2 is selected from: H, halo, C1-4alkyl, C1-4 haloalkyl, -ORA4 and C1-4alkyl substituted with -ORA4; and R3 and R4 are each independently selected from: H, halo, C1-4alkyl, C1-4haloalkyl, C3-6cycloalkyl, -ORA4, -NRA5RB4, -CN, -SRAS and C1-4alkyl substituted with -ORA5; and pharmaceutical compositions comprising the novel compounds. More specifically, the invention relates to compounds useful as indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3- dioxygenase (TD02) modulators (e.g. IDOl, and ID02 and/or TD02 inhibitors).
Applicant(s) REDX PHARMA PLC
Representative Drug(s) D07JFY Drug Info IC50 = 141 nM Click to Show More [1]
2 D0MO3W Drug Info IC50 = 622 nM [1]
Patent ID WO2016037026
Title Cyclohexyl-Ethyl Substituted Diaza- and Triaza-Tricyclic Compounds As Indole-Amine-2,3-Dioxygenase (Ido) Antagonists for The Treatment of Cancer.
Abstract Cyclohexylethyl substituted diaza- and triaza-tricyclic compounds, such as e.g. 5-(2-(cyclohexyl)ethyl)-5H-imidazo[5,1-a]isoindole, 1-Cyclohexyl-2-[4,6,10-triazatricyclo[6.4.0.0^[2,6]]dodeca-1(8),2,4,9,11-pentaen-7-yl]ethan-1-ol derivatives and 1-Cyclohexyl-2-[4,6,9,11-tetraazatricyclo[6.4.0.0^[2,6]]dodeca-1(8),2,4,9,11-pentaen-7-yl]ethan-1-ol derivatives as indole-amine-2,3-dioxygenase (IDO) antagonists for the treatment of e.g. cancer, proliferative disorder, viral disease, sepsis, pneumonia, bacteremia, trauma, tuberculosis, parasitic disease, neuroinflammation, schizophrenia, depression, neurodegenerative disease and pain.
Applicant(s) Merck Patent Gmbh
Representative Drug(s) D01NST Drug Info IC50 < 100 nM Click to Show More [1]
2 D02XQE Drug Info IC50 < 100 nM [1]
3 D0CE7G Drug Info IC50 < 100 nM [1]
4 D0V3KH Drug Info IC50 < 100 nM [1]
Patent ID WO2016024233
Title Inhibitors of Tryptophan Dioxygenases (Ido1 and Tdo) and Their Use In Therapy.
Abstract Pharmaceutical compositions comprising 3-aminoisoxazolopyridine compounds of the Formula I having IDO1 and/or TDO inhibitory activity are described, where W is CR1, N or N-oxide; X is CR2, N or N-oxide; Y is CR3, N or N-oxide; Z is CR4, N or N-oxide; and at least one of W, X, Y, and Z is N or N-oxide; and R9 and R10 are as defined. Also described are methods of using such compounds in the treatment of various conditions, such as cancer.
Applicant(s) AUCKLAND UNISERVICES LIMITED
Representative Drug(s) D07NFQ Drug Info IC50 < 1000 nM Click to Show More [1]
2 D0XT4V Drug Info IC50 < 1000 nM [1]
Patent ID WO2015031295
Title Ido Inhibitors.
Abstract There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or autoimmune diseases utilizing the compounds of the invention.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D0B7LR Drug Info IC50 = 0.8 nM Click to Show More [1], [2]
2 D0L4GL Drug Info IC50 = 0.8 nM [1], [2]
Patent ID WO2015002918
Title Ido Inhibitors.
Abstract There are disclosed compounds of formula (I) that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D0YY4R Drug Info IC50 = 4.49 nM Click to Show More [1], [2]
2 D09LKN Drug Info IC50 = 6.49 nM [1], [2]
Patent ID WO2014186035
Title Inhibitors of The Kynurenine Pathway.
Abstract The present application provides novel inhibitors of indoleamine 2,3-dioxygenase-1 and/or indoleamine 2,3-dioxygenase-2 and/or tryptophan 2,3-dioxygenase, metabolites thereof, and phannaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. A therapeutically effective amount of one or more of the compounds of formula (I) is useful in treating diseases resulting from dysregulation of the kynurenine pathway. Compounds of formula (I) act by inhibiting the enzymatic activity or expression of indoleamine 2,3-dioxygenase-1 and/or indoleamine 2,3-dioxygenase-2 and/or tryptophan 2,3-dioxygenase.
Applicant(s) CURADEV PHARMA PRIVATE LTD.
Representative Drug(s) D04BZI Drug Info IC50 < 200 nM Click to Show More [3]
2 D04MIQ Drug Info IC50 < 200 nM [3]
3 D0E8XV Drug Info IC50 = 200 to 1000 nM [3]
4 D0F4VD Drug Info IC50 < 200 nM [3]
5 D0FF6H Drug Info IC50 < 200 nM [3]
6 D0HV0Y Drug Info IC50 < 200 [3]
7 D0IT3V Drug Info IC50 < 200 nM [3]
8 D0RA7I Drug Info IC50 < 200 nM [3]
9 D05TIP Drug Info IC50 > 1000 nM [3]
10 D05ZGX Drug Info IC50 > 1000 nM [3]
Patent ID WO2017140274
Title Pesnot T 6,7-Heterocyclic Fused 5H-Pyrrolo[1,2-C]Imidazole Derivatives and Their Use As Indoleamine 2,3-Dioxygenase (Ido) and/or Tryptophan 2,3-Dioxygenase (Td02) Modulators.
Representative Drug(s) D05CNJ Drug Info IC50 = 7.22 nM Click to Show More [1]
2 D0UZ6C Drug Info IC50 = 46 nM [1]
3 D0T9XC Drug Info IC50 = 51.6 nM [1]
Patent ID WO2017051354
Title Modulators of Indoleamine 2,3-Dioxygenase.
Abstract Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of HIV; including the prevention of the progression of AIDS and general immunosuppression.
Applicant(s) GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED
Representative Drug(s) D03ZMX Drug Info IC50 = 2 nM Click to Show More [1]
2 D0E4BN Drug Info IC50 = 10 nM [1]
3 D0T5WX Drug Info N.A. [1]
Patent ID WO2017051353
Title Modulators of Indoleamine 2,3-Dioxygenase.
Abstract Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of HIV; including the prevention of the progression of AIDS and general immunosuppression.
Applicant(s) GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED
Representative Drug(s) D03ZMX Drug Info IC50 = 2 nM Click to Show More [1]
2 D0E4BN Drug Info IC50 = 10 nM [1]
3 D0T5WX Drug Info N.A. [1]
Patent ID WO2012142237
Title Fused Imidazole Derivatives Useful As Ido Inhibitors.
Abstract Presently provided are IDO inhibitors and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated inimunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.
Applicant(s) Newlink Genetics Corporation
Representative Drug(s) D0IY1Z Drug Info IC50 < 1000 nM Click to Show More [1], [2]
2 D0QZ8K Drug Info IC50 < 1000 nM [1], [2]
3 D0JR2C Drug Info N.A. [1], [2]
Patent ID WO2016027241
Title Novel Iminonitrile Derivatives.
Abstract The invention relates to a compound of formula (I) wherein X1 to X4 and RC to RG are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
Applicant(s) Curadev Pharma Pvt. Ltd
Representative Drug(s) D0IE8M Drug Info IC50 = 5000 nM Click to Show More [1]
2 D0BK2I Drug Info N.A. [1]
Patent ID WO2016073774
Title Immunoregulatory Agents.
Abstract Compounds that modulate the oxidoreductase enzyme indoleamine 2,3- dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.
Applicant(s) FLEXUS BIOSCIENCES, INC.
Representative Drug(s) D00JLX Drug Info N.A. Click to Show More [1]
2 D0M8KB Drug Info N.A. [1]
3 D0UI9T Drug Info N.A. [1]
Patent ID WO2016073770
Title Immunoregulatory Agents.
Abstract Compounds that modulate the oxidoreductase enzyme indoleamine 2,3- dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.
Applicant(s) FLEXUS BIOSCIENCES, INC.
Representative Drug(s) D0U3KX Drug Info N.A. [1]
Patent ID WO2016073738
Title Immunoregulatory Agents.
Abstract Compounds that modulate the oxidoreductase enzyme indoleamine 2,3- dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune -related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.
Applicant(s) FLEXUS BIOSCIENCES, INC.
Representative Drug(s) D0H3ZZ Drug Info N.A. Click to Show More [1]
2 D0YV6X Drug Info N.A. [1]
Patent ID WO2016071293
Title Pharmaceutical Compound.
Abstract Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises formula (I) wherein X1, and X2 may be the same or different and each is independently selected from C, N, O and S; X3, X4, X5, and X6 may be the same or different and each is independently selected from C and N; each bond represented by a dotted line may be present or absent, provided that at least one such bond is present; R1, R2, R3, R4, R5 and R6 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R1, R2, R3, R4, R5 and R6 groups present is such that the respective valencies of X1, X2, X3, X4, X5, and X6 are maintained; and wherein at least one of R5 and R6 comprises a group Y, wherein Y is a group having a formula selected from (II), (III), (IV), (V), (VI), (VII) wherein L may be present or absent, and may be a substituted or unsubstituted organic linking group; R31 and R32 may be the same or different and are selected from H and a substituted or unsubstituted organic group; each R34 may be the same or different and is selected from H and a substituted or unsubstituted organic group; R35 is selected from a substituted or unsubstituted alcohol group or ether group; each R36 may be the same or different and is selected from H and a substituted or unsubstituted organic group; X7 may be selected from C and N; X8, X9, X10, X11, X12, X13, X14, X15 and X16 may be the same or different and each is independently selected from C, N, O and S; each bond represented by a dotted line may be present or absent; and each R313 may be the same or different and is selected from H and a substituted or unsubstituted organic group.
Applicant(s) Iomet Pharma Ltd
Representative Drug(s) D06HOA Drug Info N.A. Click to Show More [1]
2 D0JB1V Drug Info N.A. [1]
Patent ID WO2016071283
Title Inhibitors of Tryptophan-2,3-Dioxygenase or Indoleamine-2,3-Dioxygenase.
Abstract Provided is a compound for use in medicine for inhibiting tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO), which compound comprises formula (I) wherein X1, X2, and X7, may be the same or different and each is independently selected from C and N; X3, X4, X5, and X6 may be the same or different and each is independently selected from C, N, O and S wherein when X3 is N it has a double bond and wherein when X6 is N it has a double bond; the dotted line is a bond which may be present or absent; R1, R2, R3, R4, R5, R6, and R7 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that at least one of R2, R3, R4 and R6 comprises a group Y; and provided that the number of R1, R2, R3, R4, R5, R6, and R7 groups present is such that the respective valencies of X1, X2, X3, X4, X5, X6, and X7 are maintained; and wherein Y is a group having a formula selected from (II), (III), (IV), (V) wherein L may be present or absent, and may be a substituted or unsubstituted organic linking group, and R31 and R32 may be the same or different and are selected from H and a substituted or unsubstituted organic group, X8 is selected from C and N, and each R313 may be the same or different and is selected from H and a substituted or unsubstituted organic group.
Applicant(s) Iomet Pharma Ltd
Representative Drug(s) D0DA8D Drug Info N.A. Click to Show More [1]
2 D0F4MN Drug Info N.A. [1]
Patent ID WO2016026772
Title Pharmaceutical Compound.
Abstract Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula (I): wherein X1 is selected from C and N; X3 and X5 may be the same or different and each is independently selected from C, N, O and S; Y is selected from N and O; Z is selected from C, N and O; each bond represented by a dotted line may independently be a double bond or a single bond, provided that valencies at each ring atom are maintained and provided that the ring Q contains at least one double bond and provided that the atom N has a double bond; R3 and R5 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R3 groups present is such that the valency of X3 is maintained, and the number of R5 groups present is such that the valency of X5 is maintained; each R11 and R12 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R11 and R12 groups present is such that the valency of Z is maintained; R21 is selected from H and a substituted or unsubstituted organic group; R22 may be present or absent and is selected from H and a substituted or unsubstituted organic group; and Cy is a cyclic organic group.
Applicant(s) IOMET PHARMA LTD
Representative Drug(s) D06FHJ Drug Info N.A. Click to Show More [1]
2 D0R8OW Drug Info N.A. [1]
Patent ID WO2017149469
Title Heterocyclic Compounds Useful As Ido and/or Tdo Modulators.
Abstract Present invention relates to novel heterocyclic compounds as indoleamine 2,3- dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) modulators. Compounds of the present invention inhibit tryptophan degradation by modulating IDO and/or TDO. Formula (I) The invention further relates to the process of their preparation, pharmaceutical composition and their use in modulating the activity of indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3- dioxygenase (TDO). The compounds of the invention can be used alone or in combination for the treatment of conditions that benefits from the inhibition of tryptophan degradation.
Applicant(s) EMCURE PHARMACEUTICALS LIMITED
Representative Drug(s) D04VUH Drug Info IC50 < 500 nM [1]
Patent ID WO2017139414
Title Inhibitor of Indoleamine-2,3-Dioxygenase (Ido).
Abstract The present disclosure provides compounds of Formula (I). The compounds described herein may be useful in treating a disease associated with IDO, for example, cancer or an infectious disease (e.g., viral or bacterial infectious diseases). Also, provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.
Applicant(s) INVENTISBIO INC.
Representative Drug(s) D03CYB Drug Info IC50 = 0.5 nM [1]
Patent ID WO2017079669
Title Pharmaceutical Compositions and Methods for Indoleamine 2,3-Dioxygenase Inhibition and Indications Therefor.
Abstract The present invention is directed to pharmaceutical compositions of an inhibitor of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders.
Applicant(s) INCYTE CORPORATION
Representative Drug(s) D04WCW Drug Info IC50 = 72 nM [1]
Patent ID WO2017075341
Title Fused Imidazole Derivatives As Ido/Tdo Inhibitors.
Abstract The present application relates to compounds and methods for the modulation (e.g., inhibition) of the enzyme indoleamine 2,3-dioxygenase and/or tryptophan 2,3-dioxygenase (IDO/TDO), and methods of treating diseases and disorders in which IDO/TDO plays a role. The present application provides compounds of Formula (I) or (II):.
Applicant(s) SCIFLUOR LIFE SCIENCES, INC.
Representative Drug(s) D0N6UO Drug Info IC50 = 49 nM [1]
Patent ID WO2016169421
Title Imidazo Isoindole Derivative, Preparation Method Therefor and Medical Use Thereof.
Abstract The present invention relates to an imidazo isoindole derivative, a preparation method therefor and a medical use thereof. In particular, the present invention relates to the imidazo isoindole derivative as shown in the formula (I), a preparation method and pharmaceutical composition containing the derivative, and a use thereof for treating diseases with the pathological characteristic of IDO-mediated tryptophan metabolic pathways. The diseases comprise cancers, Alzheimer's disease, autoimmune diseases, depression, anxiety disorders, cataracts, psychological disorders and AIDS, wherein the substituents in the formula (I) are the same as those defined in the description.
Applicant(s) JIANGSU HENGRUI MEDICINE CO [CN]; SHANGHAI HENGRUI PHARMACEUTICAL CO LTD [CN]
Representative Drug(s) D0WR7B Drug Info IC50 = 5.12 nM [1]
Patent ID WO2016051181
Title 4H-Imidazo[1,5-A]Indole Derivatives and Their Use As Indoleamine 2,3-Dioxygenase (Ido) and/or Tryptophan 2,3-Dioxygenase (Td02) Modulators.
Abstract This invention relates to novel compounds of formula (I) wherein wherein ' is a 5 or 6 membered aryl or heteroaryl group, unsubstituted or substituted with 1, 2 or 3 groups as defined in claim 1; X is a bond or -(CRA1R81)n- (wherein n is selected from 1, 2, 3 and 4); Y is selected from: a bond, -O-, -NRF, -S-, -C(O)-, -C(NRF)-, -C(ORF)Rc-, -C(NRFRG)RC-, -C(O)NRF-, -NRFC(O) -NRFC(O)NRG-, -NRFSO2NRG-, - SO2-, -SO2NRF-, -NRFSO2-, -OC(O)- and -C(O)O-; Z is a bond; R1 is H or a 3 to 16 membered fully saturated, partially unsaturated or aromatic mono-, di- or tri-cyc!ic moiety, which optionally may include 1, 2 or 3 heteroatoms selected from O, N and S, and which is unsubstituted or substituted with 1 to 5 substituents as defined in claim 1; R2 is selected from: H, halo, C1-4alkyl, C1-4haloalkyl, -ORA4 and C1-4alkyl substituted with -ORA4; and R3 and R4 are each independently selected from: H, halo, C1-4halkyl, C1-4haloalkyl, C3-6cycloalkyl, -ORA5, -NRA5RB4, -CN, -SRA5 and C1-4alkyl substituted with -ORA5; and pharmaceutical compositions comprising the novel compounds. More specifically, the invention relates to compounds useful as indoieamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxynase (TDO2) modulators (e.g. IDO1, IDO2 and/or TDO2 inhibitors).
Applicant(s) REDX PHARMA PLC
Representative Drug(s) D0IS1M Drug Info IC50 = 12 nM [1]
Patent ID WO2015070007
Title Process for The Synthesis of An Indoleamine 2,3-Dioxygenase Inhibitor.
Abstract The present application is directed to processes and intermediates for making 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful in the treatment of cancer and other disorders.
Applicant(s) INCYTE HOLDINGS CORPORATION
Representative Drug(s) D04WCW Drug Info IC50 = 72 nM [1]
Patent ID WO2015006520
Title Ido Inhibitors.
Abstract There are disclosed compounds of Formula (I) that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or autoimmune diseases utilizing the compounds of the invention.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D0OZ8W Drug Info IC50 = 4.37 nM [1], [2]
Patent ID WO2014150677
Title Inhibitors of Indoleamine 2,3-Dioxygenase (Ido).
Abstract There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D08XQG Drug Info IC50 = 0.5 nM [1], [2]
Patent ID WO2014150646
Title Ido Inhibitors.
Abstract There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or autoimmune diseases utilizing the compounds of the invention. Formula (I).
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D09HVV Drug Info IC50 = 0.7 nM [1], [2]
Patent ID WO2010005958
Title 1,2,5-Oxadiazoles As Inhibitors of Indoleamine 2,3-Dioxygenase.
Abstract The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives. The present invention provides, inter alia, IDO inhibitors of Formula I: or a pharmaceutically acceptable salt thereof, wherein: R1 is NH2 or CH3; R2 is C1, Br, CF3, CH3, or CN; R3 is H or F; and n is 1 or 2.
Applicant(s) INCYTE CORPORATION
Representative Drug(s) D04WCW Drug Info IC50 = 72 nM [1]
Patent ID WO2014159248
Title Tricyclic Compounds As Inhibitors of Immunosuppression Mediated By Tryptophan Metabolization.
Representative Drug(s) D0S7BW Drug Info IC50 < 1000 nM [1]
Patent ID WO2017106062
Title Novel Compounds As Indoleamine 2,3-Dioxygenase Inhibitors.
Abstract Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme:(I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
Applicant(s) MERCK SHARP & DOHME CORP. HAN, Yongxin ACHAB, Abdelghani BIJU, Purakkattle DENG, Yongqi FRADERA, Xavier GUO, Liangqin HE, Shuwen KOZLOWSKI, Joseph KURUKULASURIYA, Ravi LIU, Kun MCGOWAN, Meredeth, A. PU, Qinglin SCIAMMETTA, Nunzio ZHANG , Hongjun ZHOU, Hua
Representative Drug(s) D0P1HR Drug Info N.A. [1]
Patent ID WO2017010106
Title A Therapeutic Agent for A Tumor Comprising An Ido Inhibitor Administered In Combination with An Antibody.
Abstract The present invention provides a method for treating a tumor comprising administering an effective amount of an antibody which specifically binds to human CC chemokine receptor 4, human epidermal growth factor receptor 2, human CD20, or epidermal growth factor receptor, and an indoleamine 2,3-dioxygenase inhibitor to a human in need thereof, and the like.
Applicant(s) Kyowa Hakko Kirin Co., Ltd
Representative Drug(s) D0FY1Q Drug Info N.A. [1]
Patent ID WO2017002078
Title Inhibitors of Indoleamine 2,3-Dioxygenase.
Abstract Provided are compounds of formula (I) and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of HIV; including the prevention of the progression of AIDS and general immunosuppression.
Applicant(s) GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Representative Drug(s) D03TZE Drug Info N.A. [1]
Patent ID WO2015150097
Title Indole Derivatives for Use In Medicine.
Abstract Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula: wherein X1, X2, X3, X4, and X5 may be the same or different and each is independently selected from C, N and O; each atom having a dotted line may independently have a double bond or a single bond, provided that valencies at each atom are maintained; each R1, R2, R3, R4, R5, and R7 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of such R groups present is such that the valencies of X1, X2, X3, X4, and X5 are maintained; one or two R6 groups may be present and are selected from H and a substituted or unsubstituted organic group, provided that the number of R6 groups present is such that the valency of the carbon atom to which they are attached is maintained, and provided that at least one R6 is an organic group comprising an atom double-bonded to an oxygen atom (preferably a carbonyl group or a sulphonyl group) at an alpha-, gama-, or gama-position to the carbon atom to which the R6 is attached and in which the atom double-bonded to an oxygen atom is also bonded to a hetero-atom.
Applicant(s) IOMET PHARMA LTD
Representative Drug(s) D03JQL Drug Info N.A. [1]
Patent ID WO2014081689
Title Compounds Useful As Inhibitors of Indoleamine 2,3-Dioxygenase.
Abstract The present invention relates to compounds useful as inhibitors of indoleamine 2,3-dioxygenase (IDO). The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications.. The compounds of this invention have formula I-A; wherein the variables are as defined herein.
Applicant(s) VERTEX PHARMACEUTICALS INCORPORATED
Representative Drug(s) D0Z5PM Drug Info N.A. [1]
Patent ID WO2017152857
Title Indoleamine-2,3-Dioxygenase Inhibitor Containing Nitrogen Alkylated and Arylated Sulphoxide Imines.
Representative Drug(s) D0YW4T Drug Info N.A. [1]
Patent ID WO2017133258
Title Driv De 1H-Indazole Et Utilisation Correspondante Comme Inhibiteur De LIdo.
Representative Drug(s) D0UC2S Drug Info N.A. [1]
Patent ID WO2017129139
Title Sulfamic Acid Ester As Indoleamine-2,3-Dioxygenase Inhibitor, Preparation Method Therefor and Use Thereof.
Representative Drug(s) D06SKI Drug Info N.A. [1]
Patent ID WO2015082499
Title Pharmaceutical Compound.
Representative Drug(s) D09FPV Drug Info N.A. [1]
Patent ID WO2015119944
Title Combination of A Pd-1 Antagonist and An Ido1 Inhibitor for Treating Cancer.
Abstract The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and a selective inhibitor of indoleamine 2, 3-dioxygenase 1 (IDO1), and the use of the combination therapies for the treatment of cancer, and in particular for treating cancers that express PD-L1.
Applicant(s) Incyte Corporation
Patent ID WO2011045340
Title Ido Inhibitors and Therapeutic Uses Thereof.
Abstract Use use of the compounds of formula I, and pharmaceutically acceptable salts thereof (Formula I), in which R1 represents hydrogen or cyclohexy and R2 represents hydrogen or alkyl C1-6 provided that R1 and R2 do not both simultaneously represent hydrogen; in the treatment of diseases in which inhibition of IDO plays a therapeutic role, eg in the treatment of cancer.
Applicant(s) Ludwig Institute for Cancer Research Ltd
United States Patent and Trademark Office (USPTO)
Patent ID US20160333009
Title Benzimidazole and Imadazopyridine Carboximidamide Compounds.
Representative Drug(s) D0Q3SU Drug Info IC50 = 111 nM Click to Show More [1]
2 D0B5FA Drug Info IC50 = 274 nM [1]
European Patent Office (EPO)
Patent ID EP2970173
Title Inhibitors of The Kynurenine Pathway.
Applicant(s) Curadev Pharma Private Ltd
Representative Drug(s) D04MIQ Drug Info IC50 < 200 nM Click to Show More [3]
2 D0RA7I Drug Info IC50 < 200 nM [3]
References  Top
REF 1 A patent review of IDO1 inhibitors for cancer.Expert Opin Ther Pat. 2018 Apr;28(4):317-330.
REF 2 Immune checkpoint inhibitors: a patent review (2010-2015).Expert Opin Ther Pat. 2016 May;26(5):555-64.
REF 3 Inhibitors of the kynurenine pathway as neurotherapeutics: a patent review (2012-2015).Expert Opin Ther Pat. 2016 Jul;26(7):815-32.

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