Target General Information
Target ID T13629 Target Info
Target Name PD-1-PD-L1 interaction (PD-1/PD-L1 PPI)
Synonyms Programmed cell death 1/Programmed cell death 1 ligand 1 PPI
Target Type Patented-recorded Target
Gene Name PDCD1-CD274
UniProt ID
Patent(s) and the Corresponding Patented Drug(s)
World Intellectual Property Organization (WIPO)
Patent ID WO2017066227
Title Compounds Useful As Immunomodulators.
Abstract The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases. The compounds have formula (I), wherein R2 is selected from (II) and (III).
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D0KA7I Drug Info IC50 = 0.48 nM Click to Show More [1]
2 D04ESH Drug Info IC50 = 0.5 nM [1]
Patent ID WO2015160641
Title Compounds Useful As Immunomodulators.
Abstract The present disclosure generally relates to inhibitors of the PD-l/PD- Ll protein/protein and CD80/PD-L1 protein/protein interactions useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D03TWD Drug Info IC50 = 1.4 nM Click to Show More [1]
2 D01MSP Drug Info IC50 = 2.3 nM [1]
Patent ID WO2018045142
Title Immune Checkpoint Inhibitors, Compositions and Methods Thereof.
Abstract The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula (I), or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof. For Formula (I) compounds R1, R2, X1, Y1 and n are as defined in the specification. The inventive Formula (I) compounds are inhibitors of the PD-1/PD-L1 protein/protein binding or functional interaction and find utility in any number of therapeutic applications, including but not limited to treatment of proliferative disorders such as cancer and infectious diseases.
Applicant(s) Polaris Pharmaceuticals, Inc
Representative Drug(s) D0R7YI Drug Info IC50 = 0.1 to 10 nM Click to Show More [1]
2 D04CCX Drug Info IC50 = 11 to 100 nM [1]
Patent ID WO2018044963
Title Biaryl Compounds Useful As Immunomodulators.
Abstract The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D0N5NV Drug Info IC50 = 1.1 nM Click to Show More [1]
2 D0D3RS Drug Info IC50 = 6 nM [1]
Patent ID WO2018026971
Title Symmetric or Semi-Symmetric Compounds Useful As Immunomodulators.
Abstract A compound having Formula I:(I), or a pharmaceutical acceptable salt thereof. A is a bivalent arene or a bivalent heteroarene; Ring B and Ring B' are independently a 6-membered aromatic hydrocarbon ring, a 6-membered heterocyclic ring, a 8- to 10-membered aromatic hydrocarbon ring, or a 8- to 10-membered heterocyclic ring; Y and Y' are independently, null (direct bond), -CHR1-, -CH2-CH2-, -NR1-, -0-, -OCH2-, -CH2O-, -SCH2-, -CH2S-, -SOCH2-, -CH2SO-, or -SO2CH2-, and R1 is H, C1-6 alkyl, or C3-6 cycloalkyl.
Applicant(s) Arising International, Inc
Representative Drug(s) D04PCT Drug Info IC50 = 100 to 25000 nM Click to Show More [1]
2 D0M6WW Drug Info IC50 < 100 nM [1]
Patent ID WO2018013789
Title Heterocyclic Compounds As Immunomodulators.
Abstract Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
Applicant(s) Incyte Corporation
Representative Drug(s) D01OQQ Drug Info IC50 <= 100 nM Click to Show More [1]
2 D02UJS Drug Info IC50 <= 100 nM [1]
Patent ID WO2018009505
Title 1,3-Dihydroxy-Phenyl Derivatives Useful As Immunomodulators.
Abstract The present disclosure generally relates to compounds of formula (I), wherin R2 is a phenyl or pyridinyl moiety, useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D0O8FI Drug Info IC50 = 1 to 10 nM Click to Show More [1]
2 D0XV7Y Drug Info IC50 = 120 nM [1]
Patent ID WO2018006795
Title Aromatic Acetylene or Aromatic Ethylene Compound, Intermediate, Preparation Method, Pharmaceutical Composition and Use Thereof.
Abstract Disclosed are an aromatic acetylene or aromatic ethylene compound, an intermediate, a preparation method, a pharmaceutical composition and a use thereof. The aromatic acetylene or aromatic ethylene compound has a significant inhibitory effect on PD-1 and PD-L1, and can effectively relieve or treat cancers and other related diseases.
Applicant(s) Uangzhou Maxinovel Pharmaceuticals Co Ltd
Representative Drug(s) D0A5OT Drug Info IC50 = 18 nM Click to Show More [1]
2 D0RK4V Drug Info IC50 = 1300 nM [1]
Patent ID WO2017205464
Title Heterocyclic Compounds As Immunomodulators.
Abstract Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. (I).
Applicant(s) Incyte Corporation
Representative Drug(s) D0FJ1N Drug Info IC50 <= 100 nM Click to Show More [1]
2 D0HC9K Drug Info IC50 <= 100 nM [1]
Patent ID WO2017202276
Title Phenylate Derivative, Preparation Method Therefor, and Pharmaceutical Composition and Uses Thereof.
Abstract A phenylate derivative, a preparation method therefor, and a pharmaceutical composition and uses thereof. Specifically, the present invention relates to a phenylate derivative represented by formula I, a pharmaceutically-acceptable salt thereof, a stereoisomer thereof, a preparation method therefor, and a pharmaceutical composition containing the one or more compounds, and uses of the compounds in treating diseases related to PD-1/PD-L1 signal channels, such as cancers, infectious diseases and autoimmune diseases.
Applicant(s) Inst of Materia Medica Chinese Academy of Of Medical Sciences
Representative Drug(s) D00CRQ Drug Info IC50 = 18 nM Click to Show More [1]
2 D02XVC Drug Info IC50 = 41 nM [1]
Patent ID WO2017202275
Title Bromo Benzyl Ether Derivative, Preparation Method Therefor, and Pharmaceutical Composition and Uses Thereof.
Abstract Disclosed in the present invention are a bromo benzyl ether derivative, a preparation method therefor, and a pharmaceutical composition and uses thereof. Specifically, the present invention relates to a bromo benzyl ether derivative represented by formula I, a pharmaceutically-acceptable salt thereof, a stereoisomer thereof, and a preparation method therefor, a pharmaceutical composition containing the one or more compounds, and uses of the compounds in treating diseases related to PD-1/PD-L1 signal channels, such as cancers, infectious diseases and autoimmune diseases.
Applicant(s) Inst of Materia Medica Chinese Academy of Of Medical Sciences
Representative Drug(s) D01AYP Drug Info IC50 = 0.08 pM Click to Show More [1]
2 D0R7CP Drug Info IC50 = 31 pM [1]
Patent ID WO2017202273
Title Benzyl Phenyl Ether Derivative, Preparation Method Therefor, and Pharmaceutical Composition and Uses Thereof.
Abstract Disclosed in the present invention are a benzyl phenyl ether derivative, a preparation method therefor, and a pharmaceutical composition and uses thereof. Specifically, the present invention relates to a benzyl phenyl ether derivative represented by formula I, a pharmaceutically-acceptable salt thereof, a stereoisomer thereof, a preparation method therefor, and a pharmaceutical composition containing the one or more compounds, and uses of the compounds in treating diseases related to PD-1/PD-L1 signal channels, such as cancers, infectious diseases and autoimmune diseases.
Applicant(s) Inst of Materia Medica Chinese Academy of Of Medical Sciences
Representative Drug(s) D0B2VS Drug Info IC50 = 2.5 nM Click to Show More [1]
2 D0I6RC Drug Info IC50 = 5.3 nM [1]
Patent ID WO2017192961
Title Heterocyclic Compounds As Immunomodulators.
Abstract Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
Applicant(s) Incyte Corporation
Representative Drug(s) D03HAA Drug Info IC50 <= 100 nM Click to Show More [1]
2 D06BSV Drug Info IC50 <= 100 nM [1]
Patent ID WO2017176608
Title Macrocyclic Inhibitors of The Pd-1/Pd-L1 and Cd80/Pd-L1 Protein/Protein Interactions.
Abstract The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-Ll and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases. wherein: A is selected from a bond.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D0R7JW Drug Info IC50 = 2.5 nM Click to Show More [1]
2 D03BCV Drug Info IC50 = 3 nM [1]
3 D0N4TZ Drug Info IC50 = 3 to 9.9 nM [1]
4 D0NI2B Drug Info IC50 = 4 nM [1]
5 D0QF4W Drug Info IC50 = 4.1 nM [1]
Patent ID WO2017118762
Title Inhibitors of The Pd-1/Pd-L1 Protein/Protein Interaction.
Abstract The present invention provides novel compounds of formula (I) that are useful as inhibitors of the PD-1/PD-L1 protein/protein interaction.
Applicant(s) Rijksuniversiteit Groningen
Representative Drug(s) D04HBL Drug Info IC50 = 1 to 1000000 nM Click to Show More [1]
2 D0FM9V Drug Info IC50 = 1 to 1000000 nM [1]
Patent ID WO2017106634
Title N-Phenyl-Pyridine-2-Carboxamide Derivatives and Their Use As Pd-1/Pd-L1 Protein/Protein Interaction Modulators.
Abstract Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
Applicant(s) Incyte Corporation
Representative Drug(s) D0EI4B Drug Info IC50 <= 10 nM Click to Show More [1]
2 D0F4IF Drug Info IC50 <= 10 nM [1]
Patent ID WO2017070089
Title Heterocyclic Compounds As Immunomodulators.
Abstract Disclosed are compounds of Formula (I'), methods of using the compounds to modulate PD-1/PD-L1 interaction, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or viral infections.
Applicant(s) Incyte Corporation
Representative Drug(s) D0H0CH Drug Info IC50 <= 10 nM Click to Show More [1]
2 D0J4LV Drug Info IC50 <= 10 nM [1]
Patent ID WO2016100608
Title Immunomodulators.
Abstract The present disclosure provides novel macrocyclic peptides of formula (I) which inhibit the PD-l/PD-Ll and PD-L1/CD80 protein/ protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D0R7JW Drug Info IC50 = 2.5 nM Click to Show More [1]
2 D03BCV Drug Info IC50 = 3 nM [1]
3 D0N4TZ Drug Info IC50 = 3 to 9.9 nM [1]
4 D0NI2B Drug Info IC50 = 4 nM [1]
5 D0QF4W Drug Info IC50 = 4.1 nM [1]
Patent ID WO2016077518
Title Macrocyclic Peptides Useful As Immunomodulators.
Abstract The present disclosure provides compounds which are immunomodulators and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D0R7JW Drug Info IC50 = 2.5 nM Click to Show More [1]
2 D03BCV Drug Info IC50 = 3 nM [1]
3 D0N4TZ Drug Info IC50 = 3 to 9.9 nM [1]
4 D0NI2B Drug Info IC50 = 4 nM [1]
5 D0QF4W Drug Info IC50 = 4.1 nM [1]
Patent ID WO2016039749
Title Macrocyclic Inhibitors of The Pd-1/Pd-L1 and Cd80 (B7-1)/Pd-Li Protein/Protein Interactions.
Abstract The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D0R7JW Drug Info IC50 = 2.5 nM Click to Show More [1]
2 D03BCV Drug Info IC50 = 3 nM [1]
3 D0N4TZ Drug Info IC50 = 3 to 9.9 nM [1]
4 D0NI2B Drug Info IC50 = 4 nM [1]
5 D0QF4W Drug Info IC50 = 4.1 nM [1]
Patent ID WO2016126646
Title Immunomodulators.
Abstract The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D07ZQS Drug Info IC50 = 8 nM [1]
Patent ID WO2016142894
Title 3-Substituted 1,3,4-Oxadiazole and Thiadiazole Compounds As Immunomodulators.
Abstract The present invention relates to 3-substituted 1,3,4-oxadiazole and thiadiazole compounds of formula (I) and their use to inhibit the programmed cell death 1 (PD-1) signaling pathway and/or for treatment of disorders by inhibiting an immunosuppressive signal induced by PD-1, PD-L1 or PD-L2. 5.
Applicant(s) Aurigene Discovery Technologies Limited
Representative Drug(s) D0I0JE Drug Info N.A. Click to Show More [1]
2 D0N6NA Drug Info N.A. [1]
Patent ID WO2016142886
Title 3-Substituted-1,2,4-Oxadiazole and Thiadiazole Compounds As Immunomodulators.
Abstract The present invention relates to 3-substituted-1,2,4-oxadiazole and thiadiazole compounds of formula (I) or formula (II) and their use to inhibit the programmed cell death 1 (PD-1) signaling pathway and/or for treatment of disorders by inhibiting an immunosuppressive signal induced by PD-1, PD-L1 or PD-L2.
Applicant(s) Aurigene Discovery Technologies Limited
Representative Drug(s) D0MG6V Drug Info N.A. Click to Show More [1]
2 D0Z4QT Drug Info N.A. [1]
Patent ID WO2016142852
Title 1,3,4-Oxadiazole and Thiadiazole Compounds As Immunomodulators.
Abstract The present invention relates to 1,3,4-oxadiazole and thiadiazole compounds of formula (I) and their use to inhibit the programmed cell death 1 (PD-1) signaling pathway and/or for treatment of disorders by inhibiting an immunosuppressive signal induced by PD-1, PD-L1 or PD-L2.
Applicant(s) AURIGENE DISCOVERY TECHNOLOGIES LIMITED
Representative Drug(s) D0H0MO Drug Info N.A. Click to Show More [1]
2 D0Z0KL Drug Info N.A. [1]
Patent ID WO2016142833
Title 1,2,4-Oxadiazole and Thiadiazole Compounds As Immunomodulators.
Abstract The present invention relates to 1,2,4-oxadiazole compounds of formula (I) and their use to inhibit the programmed cell death (PD1) signaling pathway and/or for treatment of disorders by inhibiting an immunosuppressive signal induced by PD-1,PD-L1 or PD-L2.
Applicant(s) Aurigene Discovery Technologies Limited
Representative Drug(s) D0W0PC Drug Info N.A. Click to Show More [1]
2 D0X5IV Drug Info N.A. [1]
Patent ID WO2015044900
Title Therapeutic Immunomodulating Compounds.
Abstract The present invention relates to therapeutic immunomodulating compounds capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also encompasses the use of the said therapeutic compounds and their derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.
Applicant(s) Aurigene Discovery Technologies Limited
Representative Drug(s) D0S0OF Drug Info N.A. [1]
Patent ID WO2015036927
Title Immunomodulating Peptidomimetic Derivatives.
Abstract The present invention relates to immunomodulating peptidomimetic derivatives as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also refers to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.
Applicant(s) Aurigene Discovery Technologies Limited
Representative Drug(s) D0HF7V Drug Info N.A. Click to Show More [1]
2 D0I7UZ Drug Info N.A. [1]
3 D0Z9UJ Drug Info N.A. [1]
Patent ID WO2015033303
Title Cyclic Peptidomimetic Compounds As Immunomodulators.
Abstract The present invention relates to cyclic peptidomimetic compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also relates to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.
Applicant(s) Aurigene Discovery Technologies Limited
Representative Drug(s) D01PJZ Drug Info N.A. Click to Show More [1]
2 D04TLQ Drug Info N.A. [1]
3 D0EW3O Drug Info N.A. [1]
Patent ID WO2015033301
Title 1,3,4-Oxadiazole and 1,3,4-Thiadiazole Derivatives As Immunomodulators.
Abstract The present invention relates to 1,3,4-oxadiazole and 1,3,4-thiadiazole compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also refers to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.
Applicant(s) Aurigene Discovery Technologies Limited
Representative Drug(s) D0H6AL Drug Info N.A. Click to Show More [1]
2 D0YK8M Drug Info N.A. [1]
Patent ID WO2015033299
Title 1,2,4-Oxadiazole Derivatives As Immunomodulators.
Abstract The present invention relates to 1,2,4-oxadiazole and 1,2,4-thiadiazole compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signaling pathway. The invention also refers to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and 5 derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.
Applicant(s) Aurigene Discovery Technologies Limited
Representative Drug(s) D0EY9S Drug Info N.A. Click to Show More [1]
2 D0HE8M Drug Info N.A. [1]
United States Patent and Trademark Office (USPTO)
Patent ID US20180057486
Title Heterocyclic Compounds As Immunomodulators.
Applicant(s) Incyte Corporation
Representative Drug(s) D08RET Drug Info IC50 <= 100 nM Click to Show More [1]
2 D0FK4P Drug Info IC50 <= 100 nM [1]
Patent ID US20170362253
Title Heterocyclic Compounds As Immunomodulators.
Applicant(s) Incyte Corporation
Representative Drug(s) D05COE Drug Info IC50 <= 100 nM Click to Show More [1]
2 D0W0MT Drug Info IC50 <= 100 nM [1]
Patent ID US20170252432
Title Immunomodulators.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D0R7JW Drug Info IC50 = 2.5 nM Click to Show More [1]
2 D03BCV Drug Info IC50 = 3 nM [1]
3 D0N4TZ Drug Info IC50 = 3 to 9.9 nM [1]
4 D0NI2B Drug Info IC50 = 4 nM [1]
5 D0QF4W Drug Info IC50 = 4.1 nM [1]
Patent ID US20170174679
Title Heterocyclic Compounds As Immunomodulators.
Applicant(s) Incyte Corporation
Representative Drug(s) D0DP8E Drug Info IC50 <= 10 nM Click to Show More [1]
2 D0TJ4D Drug Info IC50 <= 10 nM [1]
Patent ID US20170107216
Title Heterocyclic Compounds As Immunomodulators.
Applicant(s) Incyte Corporation
Representative Drug(s) D08JWY Drug Info IC50 <= 100 nM Click to Show More [1]
2 D0W1RQ Drug Info IC50 <= 100 nM [1]
Patent ID US20160340391
Title Macrocyclic Inhibitors of The Pd-1/Pd-L1 and Cd80(B7-1)/Pd-L1 Protein/Protein Interactions.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D08EHL Drug Info EC50 = 300 nM; IC50 = 7 nM Click to Show More [1]
2 D06VTI Drug Info IC50 = 9 nM [1]
3 D0J4UO Drug Info EC50 = 150 nM [1]
Patent ID US20140294898
Title Macrocyclic Inhibitors of The Pd-1/Pd-L1 and Cd80(B7-1)/Pd-L1 Protein/Protein Interactions.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D08EHL Drug Info EC50 = 300 nM; IC50 = 7 nM Click to Show More [1]
2 D06VTI Drug Info IC50 = 9 nM [1]
3 D0J4UO Drug Info EC50 = 150 nM [1]
Patent ID US20150125491
Title Immunomodulating Cyclic Compounds.
Applicant(s) Aurigene Discovery Technologies Limited
Representative Drug(s) D0CH8E Drug Info N.A. Click to Show More [1]
2 D0MK2F Drug Info N.A. [1]
Patent ID US2014199334
Title Therapeutic Compounds for Immunomodulation.
Applicant(s) Aurigene Discovery Technologies Limited
Representative Drug(s) D02SES Drug Info N.A. Click to Show More [1]
2 D0FK6N Drug Info N.A. [1]
3 D0VB9M Drug Info N.A. [1]
References
REF 1 A patent review on PD-1/PD-L1 antagonists: small molecules, peptides, and macrocycles (2015-2018).Expert Opin Ther Pat. 2018 Sep;28(9):665-678.

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