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 T68547 Target Info
Target Name Histone deacetylase 1 (HDAC1)
Synonyms RPD3L1; HD1
Target Type Successful Target
Gene Name HDAC1
Biochemical Class Carbon-nitrogen hydrolase
UniProt ID
HDAC1_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2016008836
Title 4,5-Diarylimidazole Derivatives As Hdac Inhibitors.
Abstract The present invention relates to a 4,5-diarylimidazole derivative of formulae (I), (II) or (III): or a pharmaceutically acceptable salt thereof, wherein the 4,5-diarylimidazole derivative has a hydroxamic acid residue at a first aryl ring and a residue R1 at a second aryl ring; and wherein R1 is hydrogen, a halogen atom or an unsubstituted or substituted alkoxy group; R2 is independently selected from an unsubstituted or substituted alkyl, alkoxy or alkene group; M is a metal atom; L is a halogen atom, an unsubstituted or substituted phosphane, sulfane, arene or alkene group or a 4,5-diarylimidazole-derivative of formula (I); and n is an integer of from 1 to 5.
Applicant(s) Charit Universitts Medizin Berlin
Representative Drug(s) D0Z7QI Drug Info IC50 = 28 nM Click to Show More [1]
2 D0V5IQ Drug Info IC50 = 187 nM [1]
Patent ID WO2014181137
Title Novel Histone Deacetylase Inhibitors.
Abstract The present invention is a compound of the formula or a pharmaceutically acceptable salt thereof. The compounds are useful as HDAC inhibitors.
Applicant(s) Karus Therapeutics Ltd
Representative Drug(s) D00ACL Drug Info IC50 >= 1000 nM; IC50 <= 10000 nM Click to Show More [1]
2 D00LLN Drug Info IC50 >= 1000 nM; IC50 <= 10000 nM [1]
3 D03EUD Drug Info IC50 >= 1000 nM; IC50 <= 10000 nM [1]
4 D04MVN Drug Info IC50 >= 1000 nM; IC50 <= 10000 nM [1]
5 D04VQE Drug Info IC50 >= 1000 nM; IC50 <= 10000 nM [1]
6 D08GBR Drug Info IC50 >= 1000 nM; IC50 <= 10000 nM [1]
7 D08SNJ Drug Info IC50 >= 1000 nM; IC50 <= 10000 nM [1]
8 D08XLK Drug Info IC50 >= 1000 nM; IC50 <= 10000 nM [1]
9 D08ZJZ Drug Info IC50 >= 1000 nM; IC50 <= 10000 nM [1]
10 D0BY1R Drug Info IC50 >= 1000 nM; IC50 <= 10000 nM [1]
11 D0CH4M Drug Info IC50 >= 1000 nM; IC50 <= 10000 nM [1]
12 D0DH7R Drug Info IC50 >= 1000 nM; IC50 <= 10000 nM [1]
13 D0HM6Y Drug Info IC50 >= 1000 nM; IC50 <= 10000 nM [1]
14 D0JN0A Drug Info IC50 >= 1000 nM; IC50 <= 10000 nM [1]
15 D0K2UF Drug Info IC50 >= 1000 nM; IC50 <= 10000 nM [1]
16 D0RD7T Drug Info IC50 >= 1000 nM; IC50 <= 10000 nM [1]
17 D0SF8N Drug Info IC50 >= 1000 nM; IC50 <= 10000 nM [1]
18 D0W1AX Drug Info IC50 >= 1000 nM; IC50 <= 10000 nM [1]
19 D00GLJ Drug Info IC50 >= 10000 nM [1]
20 D00XWZ Drug Info IC50 >= 10000 nM [1]
21 D01LCZ Drug Info IC50 >= 10000 nM [1]
22 D02YDG Drug Info IC50 >= 10000 nM [1]
23 D04AMI Drug Info IC50 >= 10000 nM [1]
24 D04KQU Drug Info IC50 >= 10000 nM [1]
25 D06IIL Drug Info IC50 >= 10000 nM [1]
26 D08GQL Drug Info IC50 >= 10000 nM [1]
27 D0CX1Y Drug Info IC50 >= 10000 nM [1]
28 D0E5CO Drug Info IC50 >= 10000 nM [1]
29 D0ET4U Drug Info IC50 >= 10000 nM [1]
30 D0EU5A Drug Info IC50 >= 10000 nM [1]
31 D0L3CU Drug Info IC50 >= 10000 nM [1]
32 D0M7XL Drug Info IC50 >= 10000 nM [1]
33 D0MQ2D Drug Info IC50 >= 10000 nM [1]
34 D0MR7U Drug Info IC50 >= 10000 nM [1]
35 D0N1RX Drug Info IC50 >= 10000 nM [1]
36 D0O6SJ Drug Info IC50 >= 10000 nM [1]
37 D0Q9XK Drug Info IC50 >= 10000 nM [1]
38 D0QF0Y Drug Info IC50 >= 10000 nM [1]
39 D0QN8W Drug Info IC50 >= 10000 nM [1]
40 D0S3ZB Drug Info IC50 >= 10000 nM [1]
41 D0SK9K Drug Info IC50 >= 10000 nM [1]
42 D0TH3L Drug Info IC50 >= 10000 nM [1]
43 D0TN6E Drug Info IC50 > 10000 nM [1]
44 D0YC2M Drug Info IC50 >= 10000 nM [1]
Patent ID WO2017136451
Title Hdac1/2 Inhibitors for The Treatment of Neurodegenerative and/or Cognitive Disorders.
Abstract Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2.
Applicant(s) Regenacy Pharmaceuticals, Llc
Representative Drug(s) D0C9NX Drug Info IC50 = 3 nM [1]
Patent ID WO2017053360
Title Bicyclic and Tricyclic Cap Bearing Mercaptoacetamide Derivatives As Histone Deacetylase Inhibitors.
Abstract Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
Applicant(s) The Board of Trustes of the University of Illinois
Representative Drug(s) D0F3TB Drug Info IC50 = 13800 nM [1]
Patent ID WO2017040564
Title Hdac Inhibitors and Therapeutic Methods Using The Same.
Abstract Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
Applicant(s) The Board of Trustes of the University of Illinois
Representative Drug(s) D0LN1T Drug Info IC50 = 16900 nM [1]
Patent ID WO2017039726
Title Novel Hdac Inhibitors and Methods of Treatment Using The Same.
Abstract Disclosed herein are novel HDAC inhibitors. The HDAC inhibitors may be used in methods of treating cancer. The HDAC inhibitors may be used in methods of treating a neurological disorder.
Applicant(s) Uwm Research Foundation, Inc
Representative Drug(s) D0JB4S Drug Info IC50 = 2.6 nM [1]
Patent ID WO2016190630
Title Heterocyclicalkyl Derivative Compounds As Selective Histone Deacetylase Inhibitors and Pharmaceutical Compositions Comprising The Same.
Abstract The present invention relates to novel heterocyclicalkyl derivatives having histone deacetylase (HDAC) inhibitory activity, optical isomers thereof or pharmaceutically acceptable salts thereof, the use thereof for the preparation of medicaments, pharmaceutical compositions containing the same, a method for treating diseases using the composition, and methods for preparing the novel heterocyclicalkyl derivatives. The novel heterocyclicalkyl derivatives according to the present invention are selective histone deacetylase (HDAC) inhibitors, and may be effectively used for the treatment of histone deacetylase-mediated diseases, such as cell proliferative diseases, inflammatory diseases, autosomal dominant diseases, genetic metabolic diseases, autoimmune diseases, acute/chronic neurological disease, hypertrophy, heart failure, ocular diseases, or neurodegenerative diseases.
Applicant(s) Chong Kun Dang Pharmaceutical Corp
Representative Drug(s) D0L7HG Drug Info IC50 = 3840 nM [1]
Patent ID WO2016090230
Title Pyrimidine Hydroxy Amide Compounds for Treating Peripheral Neuropathy.
Abstract The invention relates to HDAC inhibitors for the treatment of peripheral neuropathy in a subject in need thereof. Also provided herein are methods for treating peripheral neuropathy in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an HDAC inhibitor.
Applicant(s) Acetylon Pharmaceuticals, Inc
Representative Drug(s) D0Q1QY Drug Info IC50 = 94 nM [1]
Patent ID WO2016067040
Title Diheteroaryl Histone Deacetylase Inhibitors and Their Use In Therapy.
Abstract The present invention is a compound having the following formula: (Formula (I)) or a pharmaceutically acceptable salt thereof, wherein e.g. X is C or N; n is 1 to 10; each L is independently a 5- to 12-membered heteroaryl containing at least two nitrogen atoms; and W is a zinc-binding group. The compounds are useful as histone deacetylase (HDAC) inhibitors.
Applicant(s) Karus Therapeutics Ltd
Representative Drug(s) D0JR9L Drug Info IC50 > 1000 nM [1]
Patent ID WO2016067038
Title Polyheteroaryl Histone Deacetylase Inhibitors and Their Use In Therapy.
Abstract The present invention is a compound having the following formula: or a pharmaceutically acceptable salt thereof, wherein e.g. L and Y are each independently an optionally substituted 6-membered nitrogen-containing heteroaryl; M is an optionally substituted 5- to 10-membered heteroaryl; W is a zinc-binding group; each R2 is independently hydrogen or C1-C6 alkyl; and R3 is an aryl or heteroaryl. The compounds are useful as histone deacetylase (HDAC) inhibitors.
Applicant(s) Karus Therapeutics Ltd
Representative Drug(s) D0LV6K Drug Info IC50 = 500 to 1000 nM [1]
Patent ID WO2016018795
Title Histone Deacetylase Inhibitors.
Abstract Provided herein are brain penetrant histone deacetylase (HDAC) inhibitors useful for treating diseases or disorders associated with HDAC. An exemplary HDAC inhibitor provided herein exhibits a brain-to-plama ratio of 20: 1. Pharmaceutical compositions comprising HDAC inhibitors and methods for treating diseases associated with HDAC are also provided.
Applicant(s) The General Hospital Corporation
Representative Drug(s) D0DI9S Drug Info IC50 = 0.3 nM [1]
Patent ID WO2015175813
Title Heterocyclic Hydroxamic Acids As Protein Deacetylase Inhibitors and Dual Protein Deacetylase-Protein Kinase Inhibitors and Methods of Use Thereof.
Abstract The present invention relates to novel hydroxamic acids which are specific histone deacetylase (HDAC) inhibitors and/or TTK/Mpsl kinase inhibitors, including pharmaceutically acceptable salts thereof, which are useful for modulating HDAC and/or TTK/Mpsl kinase activity, pharmaceutical compositions comprising these compounds, and processes for their preparation.
Applicant(s) The Regents of the University of Colorado, A Body Corporate
Representative Drug(s) D0BP8I Drug Info IC50 = 23 nM [1]
Patent ID WO2015137887
Title Fused Pyrimidine-Based Hydroxamate Derivatives.
Abstract The present invention relates to fused pyrimidine-based hydroxamate compounds of formula (I), comprising a hydroxamate group, that are inhibitors of histone deacetylase (HDAC) and kinases. More particularly, the present invention relates to hydroxamate substituted purine or 5H-pyrrolo[3,2-d]pyrimidine derivatives, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of disorders/conditions/diseases involving, relating to or associated with enzymes having histone deacetylase, non-histone deacetylase and kinase activities/functions and/or via unspecified/multi-targeted mechanisms.
Applicant(s) Agency for Science, Technology and Research
Representative Drug(s) D0YT8O Drug Info IC50 = 10 to 100 nM [1]
Patent ID WO2015087151
Title Novel Azaindole Derivatives As Selective Histone Deacetylase (Hdac) Inhibitors and Pharmaceutical Compositions Comprising The Same.
Abstract The present invention relates to novel azaindole derivatives, and more particularly, to novel azaindole derivatives having histone deacetylase (HDAC) inhibitory activity, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof or solvates thereof, the use thereof for the preparation of pharmaceutical compositions, pharmaceutical compositions containing the same, a method of treating disease using the pharmaceutical compositions, and methods for preparing the novel azaindole derivatives. The novel azaindole derivatives according to the present invention are selective histone deacetylase (HDAC) inhibitors, and may be used as agents for treating malignant tumor diseases, inflammatory diseases, rheumatoid arthritis, and neurodegenerative diseases.
Applicant(s) Chong Kun Dang Pharmaceutical Corp
Representative Drug(s) D09PVH Drug Info IC50 = 382 nM [1]
Patent ID WO2015054474
Title Pyrimidine Hydroxy Amide Compounds As Histone Deacetylase Inhibitors.
Abstract Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDACl, HDAC2, and/or HDAC6. Also provided herein are methods for inhibiting migration of a neuroblastoma cell, inducing maturation of a neuroblastoma cell, and altering cell cycle progression of a neuroblastoma cell comprising administering to the cell a therapeutically effective amount of a HDACl, HDAC2, and/or HDAC6 selective inhibitor or a pharmaceutically acceptable salt thereof.
Applicant(s) Acetylon Pharmaceuticals, Inc
Representative Drug(s) D0EH2K Drug Info IC50 = 21 nM [1]
Patent ID WO2014178606
Title Novel Compounds for Selective Histone Deacetylase Inhibitors, and Pharmaceutical Composition Comprising The Same.
Abstract The present invention relates to novel urea derivatives and, more particularly, to novel urea derivatives with histone deacetylase (HDAC) inhibitory activity, isomers thereof, pharmaceutically acceptable salts thereof, their use for the preparation of a medicaments comprising the same, a pharmaceutical composition comprising the same, a treatment method using the composition, and a method for preparing novel urea derivatives. The novel urea derivatives as selective histone deacetylase (HDAC) inhibitors are effective for the treatment of histone deacetylase-mediated diseases such as malignant tumors, inflammatory diseases, rheumatoid arthritis, neurodegeneration, etc.
Applicant(s) Chong Kun Dang Pharmaceutical Corp
Representative Drug(s) D0LP1K Drug Info IC50 = 2120 nM [1]
Patent ID WO2014152444
Title Histone Deacetylase Inhibitors.
Abstract Proivded herein are compounds and methods for inhibiting histone deacetylase (&quot;HDAC&quot;) enzymes (e.g., HDACl, HDAC2, and HDAC3).
Applicant(s) Biomarin Pharmaceutical Inc
Representative Drug(s) D0OU0J Drug Info IC50 < 1000 nM [1]
Patent ID WO2014143666
Title Hdac Inhibitors.
Abstract Disclosed herein are compounds of formula (I), and methods of inhibiting histone deacetylase (&quot;HDAC&quot;) enzymes (e.g., HDAC1, HDAC2, and HDAC3) using compounds of formula (I).
Applicant(s) Biomarin Pharmaceutical Inc
Representative Drug(s) D0UD9R Drug Info IC50 < 1000 nM [1]
Patent ID WO2014122222
Title Hydroxamate Derivatives Bearing Amide-Lactams As Potent Hdac Inhibitors and Their Uses As Medicaments.
Abstract The present invention relates to novel amide compounds of Formula (I), and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC is responsive, and the pharmaceutical composition containing such compounds.
Applicant(s) Sigma-Tau Industrie Farmaceutiche Riunite Spa
Representative Drug(s) D0N2DK Drug Info IC50 < 150 nM [1]
Patent ID WO2014072714
Title Novel Histone Deacetylase Inhibitors and Their Use In Therapy.
Abstract A compound of the formula:(I) or a pharmaceutically acceptable salt thereof, wherein: L is a 5-membered nitrogen-containing heteroaryl which is optionally fused to a benzene; Y is a 5, 6 or 7-membered nitrogen-containing heteroaryl, which is optionally fused to a benzene; and W is a zinc-binding group. The compounds are HDAC inhibitors and therefore have potential utility in therapy.
Applicant(s) Karus Therapeutics Ltd
Representative Drug(s) D0YD7B Drug Info IC50 = 226 nM [1]
Patent ID WO2013041480
Title New Thio Derivatives Bearing Lactams As Potent Hdac Inhibitors and Their Uses As Medicaments.
Abstract The present invention relates to novel amide compounds of Formula (I), and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC is responsive, and the pharmaceutical composition containing such compounds.
Applicant(s) Sigma-Tau Industrie Farmaceutiche Riunite Spa
Representative Drug(s) D07WAT Drug Info IC50 = 100 to 500 nM [1]
Patent ID WO2013005049
Title N- (2 -Aminophenyl) Benzamide Derivatives As Histone Deacetylase Inhibitors.
Abstract This invention relates to the discovery of novel compounds, or pharmaceutically acceptable salts thereof, which possess HDAC inhibitory activity. In particular, the compounds of the invention demonstrate selectivity towards Class I HDAC enzymes, and are accordingly expected to be useful for their anti-proliferative activity and in methods of treatment of the human or animal body, for example in preventing or inhibiting tumour growth and metastasis in cancers. The invention also relates to processes for the manufacture of the compounds defined herein, or pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-proliferative effect in a warm-blooded animal such as man.
Applicant(s) Cancer Research Technology Limited
Representative Drug(s) D0CH8Q Drug Info IC50 = 8700 nM [1]
Patent ID WO2013052110
Title Novel Molecules That Selectively Inhibit Histone Deacetylase 6 Relative To Histone Deacetylase 1.
Abstract The compounds of the present invention are HDAC6 selective inhibitors which are identified on the basis of accumulation of acetylated tubulin without accumulation of acetylated histones. Histone deacetylase or &quot;HDAC&quot; refers to enzymes capable of cleaving an acetyl group (-C(=0)CH3) from proteins, including histone and microtubulins. Compositions comprising the molecules and methods for their use to inhibit the activity of histone deacetylase, including for treatment, are also disclosed.
Applicant(s) The Trustes of Columbia University In the City of New York
Representative Drug(s) D0QX3G Drug Info N.A. [1]
United States Patent and Trademark Office (USPTO)
Patent ID US20170044185
Title Preparation of Histone Deacetylase (Hdac) Inhibitors and Methods for Use Thereof.
Representative Drug(s) D0RA0D Drug Info IC50 = 175 nM [1]
Patent ID US20170015655
Title Oxadiazolyl-Substituted Heterocyclic Compounds As Hdac Inhibitors and Their Preparation.
Representative Drug(s) D0T7OQ Drug Info IC50 = 1000 nM [1]
Patent ID US20130267542
Title Preparation of Substituted Quinazolinones As Histone Deacetylases (Hdacs) Inhibitors.
Representative Drug(s) D0ZG5X Drug Info IC50 >= 10000 nM [1]
References  Top
REF 1 HDAC inhibitors: a 2013-2017 patent survey.Expert Opin Ther Pat. 2018 Apr 19:1-17.

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