| Patent(s) and the Corresponding Patented Drug(s) |
Top |
| World Intellectual Property Organization (WIPO) |
| Patent ID |
WO2015075665 |
| Title |
Pyrrolopyrrolone Derivatives and Their Use As Bet Inhibitors. |
| Abstract |
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. |
| Applicant(s) |
Novartis Ag |
| Representative Drug(s) |
D09FVR |
Drug Info
|
IC50 < 11 nM |
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[1] |
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2
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D0HO8V
|
Drug Info
|
IC50 < 11 nM
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[1] |
|
3
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D0PE1R
|
Drug Info
|
IC50 < 11 nM
|
[1] |
| Patent ID |
WO2015074081 |
| Title |
Benzopiperazine 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 X, Y, Z, R1, R2, R4 and R7 are defined herein. |
| Applicant(s) |
Forma Therapeutics, Inc |
| Representative Drug(s) |
D07CSE |
Drug Info
|
IC50 < 50 nM |
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[1] |
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2
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D0S5ID
|
Drug Info
|
IC50 < 50 nM
|
[1] |
| Patent ID |
WO2015031824 |
| Title |
Cyclic Vinylogous Amides As Bromodomain Inhibitors. |
| Abstract |
Cyclic vinylogous amides of Formula (I) are disclosed. The compounds are useful for treating diseases that arise from inappropriate activity of proteins containing an acetyl-lysine. The compositions comprise a genus of cyclic vinylogous amides that are inhibitors of bromodomain. |
| Applicant(s) |
Icahn School of Medicine at Mount Sinai |
| Representative Drug(s) |
D04HTM |
Drug Info
|
IC50 < 1000 nM |
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[1] |
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2
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D08JHQ
|
Drug Info
|
IC50 < 1000 nM
|
[1] |
|
3
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D09QSH
|
Drug Info
|
IC50 < 1000 nM
|
[1] |
|
4
|
D0AU3O
|
Drug Info
|
IC50 < 1000 nM
|
[1] |
|
5
|
D0KF8C
|
Drug Info
|
IC50 < 1000 nM
|
[1] |
|
6
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D0N6JZ
|
Drug Info
|
IC50 < 1000 nM
|
[1] |
| Patent ID |
WO2015184405 |
| Title |
Aromatic Compounds, Compositions and Uses Thereof. |
| Abstract |
Aromatic compounds that are bromodomain inhibitors are provided. The compounds may be used in a method of treating cancer. Pharmaceutical compositions comprising an aromatic compound as detailed herein are provided, as are kits comprising a compound or a salt thereof and instructions for use, e.g., in a method of treating cancer. |
| Applicant(s) |
Medivation Technologies, Inc |
| Representative Drug(s) |
D03RPJ |
Drug Info
|
IC50 = 41 nM |
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[1] |
|
2
|
D03NWT
|
Drug Info
|
N.A.
|
[1] |
|
3
|
D05XXS
|
Drug Info
|
N.A.
|
[1] |
|
4
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D0NN4U
|
Drug Info
|
N.A.
|
[1] |
| Patent ID |
WO2015156601 |
| Title |
Bromodomain-Inhibiting Compounds and Pharmaceutical Composition Comprising Same for Preventing or Treating A Cancer. |
| Abstract |
Provided is a novel compound having bromodomain and extra terminal domain (BET) protein inhibiting activities, and a pharmaceutical composition comprising the same which can be useful for prevention or treatment of precancerous transformation or cancer. |
| Applicant(s) |
Kainos Medicine, Inc |
| Representative Drug(s) |
D00MXR |
Drug Info
|
N.A. |
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[1] |
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2
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D07IYX
|
Drug Info
|
N.A.
|
[1] |
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3
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D08BCK
|
Drug Info
|
N.A.
|
[1] |
|
4
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D0C9RQ
|
Drug Info
|
N.A.
|
[1] |
|
5
|
D0FN6F
|
Drug Info
|
N.A.
|
[1] |
| Patent ID |
WO2015129927 |
| Title |
Heterocyclic Compounds. |
| Abstract |
Provided herein are compounds of formula I and compositions containing the compounds. The compounds and compositions are useful in the methods of inhibiting the action of ERK5, a BET family protein or both. In certain embodiments, the compounds and compositions are useful in the prevention, amelioration or treatment of a ERK5 -mediated disease, a BET protein-mediated disease or both. |
| Applicant(s) |
Kyorin Pharmaceutical Co., Ltd |
| Representative Drug(s) |
D0CB8D |
Drug Info
|
N.A. |
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[1] |
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2
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D0L7SK
|
Drug Info
|
N.A.
|
[1] |
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3
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D0SB3H
|
Drug Info
|
N.A.
|
[1] |
| Patent ID |
WO2015018523 |
| Title |
A Novel Bet-Brd Inhibitor for Treatment of Solid Tumors. |
| Abstract |
A method of treating a solid in a mammal comprising the step of: administering a pharmaceutical acceptable amount of a thienotriazolodiazepine compound being represented by the following Formula (1): wherein R1 is alkyl having a carbon number of 1-4, R2 is a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, R3 is a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1 -4, alkoxy having a carbon number of 1-4 or cyano;...NR5...(CH2)m...R6 wherein R5 is a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and R6 is phenyl or pyridyl optionally substituted by a halogen atom; or -NR 7...CO...(CH2)n...R8 wherein R7 is a hydrogen atom or alkyl having a carbon number of 1-4, n is an integer of 0-2, and R8 is phenyl or pyridyl optionally substituted by a halogen atom, and R4 is ...(CH2)a...CO...NH...R9 wherein a is an integer of 1-4, and R9 is alkyl having a carbon number of 1-4; hydroxyalkyl having a carbon number of 1-4; alkoxy having a carbon number of 1-4; or phenyl or pyridyl optionally substituted by alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4, amino or a hydroxyl group or...(CH2)b...COOR10 wherein b is an integer of 1-4, and R10 is alkyl having a carbon number of 1-4, or a pharmaceutically acceptable salt thereof or a hydrate or solvate thereof. |
| Applicant(s) |
Oncoethix Gmbh |
| Patent ID |
WO2015121268 |
| Title |
1-Phenyl-3H-2,3-Benzodiazepines and Their Use As Bromodomain Inhibitors. |
| Abstract |
The invention relates to bromodomain protein-inhibiting, in particular BET protein-inhibiting, and preferably BRD4-inhibiting 3H-2,3-benzodiazepines of general formula (I), in which R1a, R1b, R1c, R2, R3, R4 and R5 have the meanings specified in the description, to pharmaceutical agents containing the compounds according to the invention, and to the prophylactic and therapeutic use of said pharmaceutical agents in hyperproliferative diseases, in particular tumor diseases. The invention further relates to the use of BET protein inhibitors in benign hyperplasias, atherosclerotic diseases, sepsis, autoimmune diseases, vascular diseases, viral infections, neurodegenerative diseases, inflammatory diseases, atherosclerotic diseases, and in male fertility control. |
| Applicant(s) |
Bayer Pharma Aktiengesellschaft |
| Patent ID |
WO2015121227 |
| Title |
6,9-Disubstituted 1-Phenyl-3H-2,3-Benzodiazepines and Their Use As Bromodomain Inhibitors. |
| Abstract |
The invention relates to bromodomain protein-inhibiting, in particular BET protein-inhibiting, and preferably BRD4-inhibiting 6,9-disubstituted 2,3-benzodiazepines of general formula (I), in which R1a, R1b, R1c, R2, R3, R4, R5, R6a and R6b have the meanings specified in the description, to pharmaceutical agents containing the compounds according to the invention, and to the prophylactic and therapeutic use of said pharmaceutical agents in hyperproliferative diseases, in particular tumor diseases. The invention further relates to the use of BET protein inhibitors in benign hyperplasias, atherosclerotic diseases, sepsis, autoimmune diseases, vascular diseases, viral infections, neurodegenerative diseases, inflammatory diseases, atherosclerotic diseases, and in male fertility control. |
| Applicant(s) |
Bayer Pharma Aktiengesellschaft |
| Patent ID |
WO2015121226 |
| Title |
6-Substituted 2,3-Benzodiazepines. |
| Abstract |
The invention relates to bromodomain protein-inhibiting, in particular BET protein-inhibiting, and preferably BRD4-inhibiting 6-substituted 2,3-benzodiazepines of general formula (I), in which R1a, R1b, R1c, R2, R3, R4, R5 and R6 have the meanings specified in the description, to pharmaceutical agents containing the compounds according to the invention, and to the prophylactic and therapeutic use of said pharmaceutical agents in hyperproliferative diseases, in particular tumor diseases. The invention further relates to the use of BET protein inhibitors in benign hyperplasias, atherosclerotic diseases, sepsis, autoimmune diseases, vascular diseases, viral infections, neurodegenerative diseases, inflammatory diseases, atherosclerotic diseases, and in male fertility control. |
| Applicant(s) |
Bayer Pharma Aktiengesellschaft |
| Patent ID |
WO2015081189 |
| 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 |
| Patent ID |
WO2009084693 |
| Title |
Antitumor Agent. |
| Abstract |
Disclosed is a novel antitumor agent containing, as an active ingredient, a compound inhibiting binding between an acetylated histone and a bromodomain-containing protein, preferably a thienotriazolodiazepine compound represented by the general formula (I) below or a pharmaceutically acceptable salt thereof, or a hydrate or solvate of any of those. (In the formula, the symbols are as defined in the description.). |
| Applicant(s) |
Mitsubishi Tanabe Pharma Corporation |
| Patent ID |
WO2015121230 |
| Title |
9-Substituted 2,3-Benzodiazepines. |
| Applicant(s) |
Bayer Pharma Ag |
| United States Patent and Trademark Office (USPTO) |
| Patent ID |
US20150315207 |
| Title |
Novel Heterocyclic Compound Classes for Signalling Modulation. |
| Applicant(s) |
Signalrx Pharmaceuticals, Inc |
| Representative Drug(s) |
D05LTB |
Drug Info
|
N.A. |
Click to Show More |
[1] |
|
2
|
D0EN4B
|
Drug Info
|
N.A.
|
[1] |
|
3
|
D0J4QG
|
Drug Info
|
N.A.
|
[1] |
|
4
|
D0SQ0F
|
Drug Info
|
N.A.
|
[1] |
| Patent ID |
US20150148375 |
| Title |
Bicyclic Heterocycles As Bet Protein Inhibitors. |
| Applicant(s) |
Incyte Corporation |
