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 T58998 Target Info
Target Name Bromodomain and extraterminal domain protein (BET)
Synonyms Bromodomain and Extra Terminal protein
Target Type Clinical trial Target
Gene Name NO-GeName
UniProt ID
NOUNIPROTAC
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2015104653
Title Bicyclic Heterocyclic Derivatives As Bromodomain Inhibitors.
Abstract The present invention provides bicyclic heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as bromodomain inhibitors; (I), in which R1, R2, R3, R4, L1, L2, Cy1, Cy2, X, n and dotted line are have the same meaning given in the specification, and pharmaceutically acceptable salts or pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder associated as bromodomain inhibitors. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of bicyclic heterocyclic derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
Applicant(s) Orion Corporation
Representative Drug(s) D08IZA Drug Info IC50 <= 1000 nM Click to Show More [1]
2 D0A4RP Drug Info IC50 <= 1000 nM [1]
3 D0PK4M Drug Info IC50 <= 1000 nM [1]
4 D0TF2N Drug Info IC50 <= 1000 nM [1]
Patent ID WO2015004075
Title Modified Bet-Protein-Inhibiting Dihydroquinoxalinones and Dihydropyridopyrazinones.
Abstract The invention relates to BET-protein-inhibiting, in particular BRD4-inhibiting, dihydroquinoxalinones and dihydropyridopyrazinones of general formula (I), in which A, X, R1, R2, R3, R4, R5, R6, and n have the meanings indicated in the description, intermediate products for producing the compounds according to the invention, pharmaceutical agents containing the compounds according to the invention, and the prophylactic and therapeutic use of said pharmaceutical agents in the case of hyperproliferative diseases, in particular in the case of tumor diseases. The invention further relates to the use of BET protein inhibitors in the case of viral infections, neurodegenerative diseases, inflammatory diseases, and atherosclerotic diseases and in male fertility control.
Applicant(s) Bayer Pharma Aktiengesellschaft
Representative Drug(s) D0R6KH Drug Info IC50 = 11 nM Click to Show More [1]
2 D04WNN Drug Info IC50 = 15 to 16 nM [1]
3 D0R8CR Drug Info IC50 = 15 to 16 nM [1]
4 D0T9ZO Drug Info IC50 = 16 nM [1]
5 D0OJ1R Drug Info IC50 = 25 nM [1]
Patent ID WO2015131005
Title 9H-Pyrimido[4,5-B]Indoles and Related Analogs As Bet Bromodomain Inhibitors.
Abstract The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula (I) and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.
Applicant(s) The Regents of the University of Michigan
Representative Drug(s) D0HB3F Drug Info IC50 = 0.5 to 1.6 nM Click to Show More [1]
2 D0KG1T Drug Info IC50 = 0.5 to 1.6 nM [1]
3 D0P5SF Drug Info N.A. [1]
Patent ID WO2015074064
Title Tetrahydroquinoline Compositions As Bet Bromodomain Inhibitors.
Abstract The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula (I): wherein W, X, Y, Z, R1, R2, R5, and R8 are as described herein.
Applicant(s) Forma Therapeutics Inc
Representative Drug(s) D0SV2S Drug Info IC50 < 50 nM Click to Show More [1]
2 D0U5BE Drug Info IC50 < 100 nM [1]
3 D05PZG Drug Info N.A. [1]
Patent ID WO2015164480
Title 1H-Pyrrolo[2,3-C]Pyridin-7(6H)-Ones and Pyrazolo[3,4-C]Pyridin-7(6H)-Ones As Inhibitors of Bet Proteins.
Abstract The present invention relates to substituted pyrrolopyridinones and substituted pyrazolopyridinones which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
Applicant(s) Incyte Corporation
Representative Drug(s) D0E4UV Drug Info N.A. Click to Show More [1]
2 D0G5UR Drug Info N.A. [1]
3 D0JR5G Drug Info N.A. [1]
Patent ID WO2015015318
Title Novel Quinazolinones As Bromodomain Inhibitors.
Abstract The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
Applicant(s) Zenith Epigenetics Corp
Representative Drug(s) D09ENS Drug Info N.A. Click to Show More [1]
2 D0FY9K Drug Info N.A. [1]
3 D0I6HB Drug Info N.A. [1]
Patent ID WO2015004534
Title Novel Substituted Bicyclic Compounds As Bromodomain Inhibitors.
Abstract The invention relates to substituted bicyclic compounds, which are useful for inhibition of BET protein function by binding to bromodomains, pharmaceutical compositions comprising these compounds, and use of the compounds and compositions in therapy.
Applicant(s) Zenith Epigenetics Corp
Representative Drug(s) D0FC0Z Drug Info N.A. Click to Show More [1]
2 D0P8PE Drug Info N.A. [1]
3 D0T8DH Drug Info N.A. [1]
Patent ID WO2015004533
Title Novel Substituted Bicyclic Compounds As Bromodomain Inhibitors.
Abstract The invention relates to substituted bicyclic compounds, which are useful for inhibition of BET protein function by binding to bromodomains, pharmaceutical compositions comprising these compounds, and use of the compounds and compositions in therapy.
Applicant(s) Zenith Epigenetics Corp
Representative Drug(s) D0CY3L Drug Info N.A. Click to Show More [1]
2 D0CY9X Drug Info N.A. [1]
3 D0G8IM Drug Info N.A. [1]
4 D0QA4O Drug Info N.A. [1]
5 D0UU2U Drug Info N.A. [1]
6 D0W3NX Drug Info N.A. [1]
Patent ID WO2015002754
Title Novel Bicyclic Bromodomain Inhibitors.
Abstract The invention provides novel substituted, bicyclic compounds which are useful as inhibitors of extra terminal domain BET protein function by binding to bromodomains. The pharmaceutical compositions comprising such compounds are for the prevention and treatment of diseases and conditions that are associated with bromodornain and extra terminal domain (BET) proteins.
Applicant(s) Zenith Epigenetics Corp
Representative Drug(s) D05GPL Drug Info N.A. Click to Show More [1]
2 D0B8GA Drug Info N.A. [1]
3 D0BH7X Drug Info N.A. [1]
4 D0ON7G Drug Info N.A. [1]
5 D0SG9F Drug Info N.A. [1]
6 D0WM3Y Drug Info N.A. [1]
Patent ID WO2015011084
Title Substituted Dihydropyrido[3,4-B]Pyrazinones As Dual Inhibitors of Bet Proteins and Polo-Like Kinases.
Abstract The present invention relates to substituted dihydropyrido[3,4-b]pyrazinones as dual inhibitors of BET proteins, especially BRD4 proteins and polo-like kinases, especially Plk-1 proteins, of the general formula (I) in which A, X, R1, R2, R3, R4, R5, R6, R7 and n are each as defined in the description, to intermediates for preparation of the inventive compounds, to pharmaceutical compositions comprising the inventive compounds and to the prophylactic and therapeutic use thereof in hyperproliferative disorders, especially in neoplastic disorders. This invention further relates to the use of the inventive dihydropyrido[3,4-b]pyrazinones in viral infections, in neurodegenerative disorders, in inflammation disorders, in atherosclerotic disorders and in male fertility control.
Applicant(s) Bayer Pharma Aktiengesellschaft
Representative Drug(s) D0C1HS Drug Info IC50 = 126 nM [1]
Patent ID WO2015095492
Title Tricyclic Heterocycles As Bet Protein Inhibitors.
Abstract The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
Applicant(s) Incyte Corporation
Patent ID WO2015081203
Title Bicyclic Heterocycles As Bet Protein Inhibitors.
Abstract The present invention relates to bicyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
Applicant(s) Incyte Corporation
United States Patent and Trademark Office (USPTO)
Patent ID US20150307493
Title 1H-Pyrrolo[2,3-C]Pyridin-7(6H)-Ones and Pyrazolo[3,4C]Pyridin-7(6H)-Ones As Inhibitors of Bet Proteins.
Applicant(s) Incyte Corporation
Representative Drug(s) D0E4UV Drug Info N.A. Click to Show More [1]
2 D0G5UR Drug Info N.A. [1]
3 D0JR5G Drug Info N.A. [1]
Patent ID US20150175604
Title Tricyclic Heterocycles As Bet Protein Inhibitors.
Applicant(s) Incyte Corporation
References  Top
REF 1 BET inhibitors in cancer therapeutics: a patent review.Expert Opin Ther Pat. 2016;26(4):505-22.

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