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 T16739 Target Info
Target Name Lysine-specific histone demethylase 1 (LSD)
Synonyms Lysine-specific histone demethylase 1A; LSD1; KIAA0601; KDM1; Flavin-containing amine oxidase domain-containing protein 2; BRAF35-HDAC complex protein BHC110; AOF2
Target Type Clinical trial Target
Gene Name KDM1A
Biochemical Class CH-NH(2) donor oxidoreductase
UniProt ID
KDM1A_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2015181380
Title Cyclopropylamine Compounds As Histone Demethylase Inhibitors.
Abstract The present disclosure relates to cyclopropyl compounds of general formula (I), wherein R1, and R2 are as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy.
Applicant(s) Ieo - Istituto Europeo Di Oncologia Srl
Representative Drug(s) D06XEU Drug Info IC50 < 1000 nM Click to Show More [1]
2 D0L4OH Drug Info IC50 < 1000 nM [1]
Patent ID WO2015156417
Title Cyclopropanamine Compound and Use Thereof.
Abstract The present invention provides a compound having a lysine-specific demethylase-1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for schizophrenia, developmental disorders, particularly diseases having intellectual disability (e.g., autistic spectrum disorders, Rett syndrome, Down's syndrome, Kabuki syndrome, fragile X syndrome, Kleefstra syndrome, neurofibromatosis type 1, Noonan syndrome, tuberous sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, spinocerebellar degeneration (e.g., dentatorubural pallidoluysian atrophy) and Huntington's disease), epilepsy (e.g., Dravet syndrome) or drug dependence, and the like. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.
Applicant(s) Takeda Pharmaceutical Company Limited
Representative Drug(s) D07DIJ Drug Info IC50 < 100 nM Click to Show More [1]
2 D02CIX Drug Info IC50 = 180 nM [1]
3 D0R2YA Drug Info IC50 = 210 nM [1]
4 D04PWX Drug Info IC50 = 230 nM [1]
5 D0W9VF Drug Info IC50 = 240 nM [1]
Patent ID WO2015120281
Title Aminotriazole- and Aminotetrazole-Based Kdm1A Inhibitors As Epigenetic Modulators.
Abstract In some aspects, the present invention provides compounds of the formula (IV), wherein the variables are as defined herein, which may be used as inhibitors of histone demethylase or spermine oxidase. Also provided herein are pharmaceutical compositions of the compounds and methods using the compounds in the treatment of diseases such as cancer and cardiovascular disease.
Applicant(s) Musc Foundation for Research Development
Representative Drug(s) D0W8XM Drug Info IC50 = 1190 nM Click to Show More [1]
2 D02YGX Drug Info IC50 = 2220 nM [1]
Patent ID WO2014205213
Title Substituted (E)-N'-(1-Phenylethylidene) Benzohydrazide Analogs As Histone Demethylase Inhibitors.
Abstract Substituted (E)-N'-(1-phenylethylidene)benzohydrazide analogs or (3-(5-chloro-2-hydroxyphenyl)-4-METHYL-1 H-pyrazol-1-YL)(3- (morpholinosulfonyl)phenyl)methanone, derivatives thereof, and related compounds are useful as inhibitors of lysine-specific histone demethylase, including LSD1. Synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1 (lysine-specific demethylase). A pharmaceutically acceptable salt, hydrate, solvate, or polymorph thereof, and one or more of: (a) at least one agent known to increase histone demethylase activity; (b) at least one agent known to decrease histone demethylase activity; (c) at least one agent known to treat a disorder of uncontrolled cellular proliferation; (d) at least one agent known to treat a neurodegenerative disorder; (e) instructions for treating a neurodegenerative disorder; or (f) instructions for treating a disorder associated with uncontrolled cellular proliferation.
Applicant(s) University of Utah Research Foundation
Representative Drug(s) D0WT1Z Drug Info IC50 = 13 nM Click to Show More [1]
2 D05FVW Drug Info IC50 = 19 nM [1]
3 D0GA7D Drug Info IC50 > 3000 nM [1]
4 D0UG5Q Drug Info IC50 > 3000 nM [1]
Patent ID WO2014194280
Title Novel Suicidal Lsd1 Inhibitors Targeting Sox2-Expressing Cancer Cells.
Abstract Disclosed are inhibitors of lysine-specific demethylase I (LSD1); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating cancers characterized by the presence of Sox2 using the compounds and compositions Also disclosed are methods of treating cancers characterized by the presence of Sox2 using inhibitors of LSD 1 and/or histone deacetylation I (HDAC1). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Applicant(s) The Board of Regents of the Nevada System of Higher Education On Behalf of the University of Nevada, Las Vegas
Representative Drug(s) D08FVR Drug Info IC50 = 31380 nM Click to Show More [1]
2 D0I9QC Drug Info IC50 = 39380 nM [1]
Patent ID WO2013025805
Title Substituted (E)-N'-(1-Phenylethylidene) Benzohydrazide Analogs As Histone Demethylase Inhiitors.
Abstract In one aspect, the invention relates to substituted (E)-N'-(1- phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Applicant(s) University of Utah Research Foundation
Representative Drug(s) D0WT1Z Drug Info IC50 = 13 nM Click to Show More [1]
2 D05FVW Drug Info IC50 = 19 nM [1]
Patent ID WO2012071469
Title Histone Demethylase Inhibitors and Uses Thereof for Treatment O F Cancer.
Abstract A compound of formula I: or a pharmaceutically acceptable salt, Ri is an optionally substituted heterocyclic group; R and R' are independently H, CH3, NO2, SO2N(CH3)2, SO2N((CH3)SO2), COOH, COOCH3, CO(N(CH3)), alkyl, alkenyl, alkynyl, aryl, aralkyl, cycloalkyl, heteroaryl, heterocycloalkyl, alkoxy, alkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, aryloxycarbonyloxy, carboxylate, alkylcarbonyl, alkylaminocarbonyl, aralkylaminocarbonyl, alkenylaminocarbonyl, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, alkenylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylthiocarbonyl, trifluoromethyl, pentafluoroethyl, halogen, cyano, thio, amido, ether, ester, hydroxyl, hydroxyalkyl, saturated or unsaturated fatty acids, azido, phosphonamido, sulfonamido, lactam, phosphate, phosphonato, phosphinato, amino, acylamino, amidino, imino, guanidino, sulfhydryl, alkylthio, arylthio, thiocarboxylate, sulfates, alkylsulfinyl, sulfonato, sulfamoyl, sulfonamido, nitro, cyano, or azido; m and n are independently integers from 1 to 4; T, U, V, and Z are independently CH, N, or CR; L is NH, CH2, O, S, or SO2; X is N or CH; Y and Y' are independently O or S; and R3 is an optionally substituted aryl, heteroaryl, cycloalkyl, or heterocycloalkyl group.
Applicant(s) Nevada Cancer Institute
Representative Drug(s) D0DD4I Drug Info IC50 = 5270 nM Click to Show More [1]
2 D0YX4R Drug Info IC50 = 10540 nM [1]
3 D0VB7F Drug Info IC50 = 11160 nM [1]
Patent ID WO2012042042
Title Selective Lsd1 and Dual Lsd1/Mao-B Inhibitors for Modulating Diseases Associated with Alterations In Protein Conformation.
Abstract The invention relates to methods and compositions for the treatment or prevention of protein conformation disorders. In particular, the invention relates to an LSD1 inhibitor for use in treating or preventing a protein conformation disorder, such as, e.g., Huntington Disease.
Applicant(s) Oryzon Genomics, Sa
Representative Drug(s) D0IO2A Drug Info IC50 < 20 nM Click to Show More [2]
2 D06KBT Drug Info IC50 < 30 nM [2]
3 D0Q1EG Drug Info IC50 < 50 nM [2]
4 D01CIK Drug Info IC50 = 100 nM [2]
5 D06VMN Drug Info IC50 = 100 nM [2]
6 D0AI6J Drug Info IC50 < 100 nM [2]
7 D0PM2S Drug Info IC50 < 100 nM [2]
8 D02WXS Drug Info IC50 < 200 nM [2]
9 D0E7SF Drug Info IC50 < 200 nM [2]
Patent ID WO2012013728
Title Arylcyclopropylamine Based Demethylase Inhibitors of Lsd1 and Their Medical Use.
Abstract The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).
Applicant(s) Oryzon Genomics Sa
Patent ID WO2011131697
Title Lysine Specific Demethylase-1 Inhibitors and Their Use.
Abstract The present invention relates to a compound of Formula 1, wherein: (A) is heteroaryl or aryl; each ('), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (') is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, -CH2C(=0)NH2, heteroaryl, cyano, sulfonyl, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is -NH-; (L) is chosen from a single bond, -CH2-, -CH2CH2-, -CH2CH2CH2-, and -CH2CH2CH2CH2-; and (D) is an aliphatic carbocyclic group or benzocycloalkyl, wherein said aliphatic carbocyclic group or said benzocycloalkyl has 0, 1, 2, or 3 substituents independently chosen from - NH2, -NH(C1-C6 alkyl), -N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy. (A')X-(A)-(B)-(Z)-(L)-(D) formula (I) The compounds of the invention show activity for inhibiting LSD1, which makes them useful in the treatment or prevention of diseases such as cancer.
Applicant(s) Oryzon Genomics Sa
Representative Drug(s) D07NTA Drug Info EC50 = 8 nM Click to Show More [1]
2 D01CIK Drug Info IC50 = 100 nM [1]
3 D06VMN Drug Info IC50 = 100 nM [1]
4 D0LK8A Drug Info IC50 = 100 to 1000 nM [1]
Patent ID WO2011131576
Title Tranylcypromine Derivatives As Inhibitors of Histone Demethylase Lsd1 and/or Lsd2.
Abstract Tranylcypromine derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of histone demethylases LSD1 and LSD2, such as the diseases characterized by deregulation of gene transcription, cell differentiation and proliferation, e.g. tumors, viral infections, are herein described. These compounds belong to the structural formula (I) wherein A and R3 are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to compositions containing them and to therapeutic use thereof.
Applicant(s) Univ Roma
Representative Drug(s) D04OHC Drug Info IC50 = 1100 to 1900 nM Click to Show More [1]
2 D0BG7B Drug Info Ki = 1300 nM [1]
3 D0O7IH Drug Info IC50 = 1300 to 40000 nM [1]
Patent ID WO2011106573
Title Lysine Demethylase Inhibitors for Diseases and Disorders Associated with Hepadnaviridae.
Abstract The present invention provides for the treatment or prevention of Hepadnaviridae infection and disease caused by Hepadnaviridae infection. In particular, the invention provides compositions and methods that affect the ability of Hepadnaviridae to utilize the host's cellular machinery as part of the virus' lifecycle. The invention relates to the discovery that interfering with the normal ability of viruses to utilize the host cell machinery with LSD1 inhibitors reduces HBV replication. Thus, the treatment and prevention of Hepadnaviridae infection and disease caused by Hepadnaviridae according to the invention comprises administering to an individual in need of treatment, a therapeutically effective amount of a LSD1 inhibitor. The individual in need of treatment can be a human or, e.g., another mammal.
Applicant(s) Oryzon Genomics, Sa
Representative Drug(s) D07MQD Drug Info IC50 = 1 to 100 nM Click to Show More [1]
2 D0UE4K Drug Info IC50 = 1 to 100 nM [1]
3 D0YI0V Drug Info IC50 = 100 nM [1]
Patent ID WO2011035941
Title Lysine Specific Demethylase-1 Inhibitors and Their Use.
Abstract The invention relates to a compound of Formula (I): (A')x-(A)-(B)-(Z)-(L)-(D), wherein: (A) is heteroaryl or aryl; each (A'), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A') is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, amido, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is -NH-; (L) is chosen from -CH2CH2-, -CH2CH2CH2-, and -CH2CH2CH2CH2-; and (D) is chosen from -N(-R1)-R2, -O-R3, and -S-R3, wherein: R1 and R2 are mutually linked to form a heterocyclic ring together with the nitrogen atom that R1 and R2 are attached to, wherein said heterocyclic ring has 0, 1, 2, or 3 substituents independently chosen from -NH2, -NH(C1-C6 alkyl), -N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, cyano, alkoxy, haloalkyl, and haloalkoxy, or R1 and R2 are independently chosen from -H, alkyl, cycloalkyl, haloalkyl, and heterocyclyl, wherein the sum of substituents on R1 and R2 together is 0, 1, 2, or 3, and the substituents are independently chosen from -NH2, -NH(C1-C6 alkyl), -N(C1-C6 alkyl)(C1-C6 alkyl), and fluoro; and R3 is chosen from -H, alkyl, cycloalkyl, haloalkyl, and heterocyclyl, wherein R3 has 0, 1, 2, or 3 substituents independently chosen from -NH2, -NH(C1-C6 alkyl), -N(C1-C6 alkyl)(C1-C6 alkyl), and fluoro; or an enantiomer, diastereomer, or mixture thereof, or a pharmaceutically acceptable salt or solvate thereof. The compounds of the invention show inhibitory LSD1 activity, which makes them useful in the treatment or prevention of diseases such as cancer.
Applicant(s) Oryzon Genomics Sa
Representative Drug(s) D03MPD Drug Info IC50 = 1 to 100 nM Click to Show More [1]
2 D0O2WW Drug Info IC50 = 1 to 100 nM [1]
Patent ID WO2010043721
Title Oxidase Inhibitors and Their Use.
Abstract The invention relates to phenylcyclopropylamine acetamide derivatives and their use in treating diseases.
Applicant(s) Oryzon Genomics Sa
Representative Drug(s) D0XH9M Drug Info IC50 = 18 nM Click to Show More [1]
2 D08IOP Drug Info IC50 = 22 nM [1]
3 D0UL9U Drug Info Ki < 1000 nM [1]
Patent ID WO2015031564
Title Substituted-1H-Benzo[D]Imidazole Compounds As Lysine-Specific Demethylase 1 (Lsd1 ) Inhibitors.
Abstract The present invention provides compounds which are useful as inhibitors of lysine-specific demethylase 1 (LSD1 ) and pharmaceutical compositions comprising the same. The present invention also relates to a method for decreasing histone demethylase activity and treating a mammalian disorder in which LSD1 levels are elevated by administering these compounds and compositions to a patient in need thereof.
Applicant(s) University of Utah
Representative Drug(s) D0WT1Z Drug Info IC50 = 13 nM Click to Show More [1]
2 D05FVW Drug Info IC50 = 19 nM [1]
3 D0J1HQ Drug Info IC50 = 81 nM [1]
4 D0RC0G Drug Info IC50 = 90 nM [1]
5 D0MO5Y Drug Info IC50 = 273 nM [1]
Patent ID WO2015089192
Title Inhibitors of Lysine Specific Demethylase-1.
Abstract The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Applicant(s) Celgene Quanticel Research, Inc
Representative Drug(s) D07LKA Drug Info IC50 < 100 nM Click to Show More [1]
2 D0L0DT Drug Info N.A. [1]
3 D0N2QZ Drug Info N.A. [1]
Patent ID WO2014084298
Title Lsd1-Selective Inhibitor Having Lysine Structure.
Abstract The present invention mainly addresses the problem of providing a novel compound having a LSD1-selective inhibitory activity and also having an antitumor/anti-cancer activity, an anti-virus activity.
Applicant(s) Kyoto Prefectural Public University Corporation
Representative Drug(s) D0BE4Z Drug Info IC50 = 10 to 1000 nM Click to Show More [1]
2 D0D9CK Drug Info N.A. [1]
Patent ID WO2012135113
Title Cyclopropylamines As Lsd1 Inhibitors.
Abstract This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1(LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.
Applicant(s) Glaxosmithkline Intellectual Property (No.2) Limited
Representative Drug(s) D0C0PK Drug Info N.A. Click to Show More [1]
2 D0F1CT Drug Info N.A. [1]
3 D0KZ5T Drug Info N.A. [1]
4 D0LR6D Drug Info N.A. [1]
5 D0NJ6B Drug Info N.A. [1]
Patent ID WO2014085613
Title Hydroxytyrosol and Oleuropein Compositions for Induction of Dna Damage, Cell Death and Lsd1 Inhibition.
Abstract Compositions comprising hydroxytyrosol-containing formulations and treatment regiments comprising hydroxytyrosol and/or oleuropein and chemotherapeutic agents are disclosed. Compositions and/or regiments may optionally include the administration of vitamins, minerals, and anti-oxidants. Methods for using these compositions and treatment regimens for treating subjects for diseases, such as a malignancy, and for inducing or enhancing angiogenesis, treating or preventing oxidative stress, for treating or preventing high glucose-induced dysfunction, treating or preventing chemotherapy-induced dysfunction, and for improving cell viability are provided. Various methods for use of the hydroxytyrosol compositions for inhibition of lysine specific demethylase 1 (LSD1) in various cancers are also provided.
Applicant(s) Mccord, Darlene E. et al
Representative Drug(s) D0DL5J Drug Info N.A. Click to Show More [1]
2 D0P4NF Drug Info N.A. [1]
Patent ID WO2013033688
Title Treatment of Cancer.
Abstract This disclosure provides agents, compositions and methods of treating cancer by inhibiting histone lysine specific demethylase 1 ( LSD1) and/or and a histone lysine specific demethylase 2 (LSD2). Agents and compositions comprise statins and/or inhibitors of LSD1/2.
Applicant(s) The Brigham and Women'S Hospital, Inc
Representative Drug(s) D09OMM Drug Info N.A. Click to Show More [1]
2 D0WO5W Drug Info N.A. [1]
3 D0Z7HE Drug Info N.A. [1]
Patent ID WO2012034116
Title Small Molecules As Epigenetic Modulators of Lysine-Specific Demethylase 1 and Methods of Treating Disorders.
Abstract The invention provides for novel compounds which are inhibitors of lysine- specific demethylase 1 (LSDl). Such compounds may be used to treat disorders, including cancer.
Applicant(s) The Johns Hopkins University
Representative Drug(s) D05HBM Drug Info N.A. Click to Show More [1]
2 D08WMK Drug Info N.A. [1]
3 D0KR0I Drug Info N.A. [1]
4 D0U1DY Drug Info N.A. [1]
Patent ID WO2015134973
Title Inhibitors of Histone Lysine Specific Demethylase (Lsd1) and Histone Deacetylases (Hdacs).
Abstract A series of phenelzine analogs comprising a phenelzine scaffold linked to an aromatic moiety and their use as inhibitors of lysine-specific demethylase 1 (LSD1) and/or one or more histone deacetylases (HDACs) is provided. The presently disclosed phenelzine analogs exhibit potency and selectivity for LSD1 versus MAO and LSD2 enzymes and exhibit bulk, as well as, gene specific histone methylation changes, anti-proliferative activity in several cancer cell lines, and neuroprotection in response to oxidative stress. Accordingly, the presently disclosed phenelzine analogs can be used to treat diseases, conditions, or disorders related to LSD1 and/or HDACs, including, but not limited to, cancers and neurodegenerative diseases.
Applicant(s) The Johns Hopkins University
Representative Drug(s) D0U4DT Drug Info IC50 = 59 nM [1]
Patent ID WO2014164867
Title Kdm1A Inhibitors for The Treatment of Disease.
Abstract Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDMIA, and methods of increasing gamma globin gene expression in a human or animal subject are also provided for the treatment diseases such as sickle cell disease.
Applicant(s) Imago Biosciences
Representative Drug(s) D0BE4Z Drug Info IC50 = 10 to 1000 nM [1]
Patent ID WO2013057322
Title (Hetero)Aryl Cyclopropylamine Compounds As Lsd1 Inhibitors.
Abstract The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
Applicant(s) Oryzon Genomics, Sa
Representative Drug(s) D07NTA Drug Info EC50 = 8 nM [1]
Patent ID WO2013057320
Title (Hetero)Aryl Cyclopropylamine Compounds As Lsd1 Inhibitors.
Abstract The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
Applicant(s) Oryzon Genomics, Sa
Representative Drug(s) D07NTA Drug Info EC50 = 8 nM [1]
Patent ID WO2012072713
Title Lysine Demethylase Inhibitors Such As Cyclylcyclopropanamine Derivatives for Use In The Treatment of Diseases and Disorders Associated with Flaviviridae.
Abstract The invention relates to methods and compositions for the treatment or prevention of Flaviviridae infections. In particular, the invention relates to an LSD1 inhibitor such as 2 - cyclyldyclopropan - 1 - amine derivatives, phenelzine derivatives and propargylamine derivatives for use in treating or preventing Flaviviridae infections, including hepatitis C virus infections.
Applicant(s) Oryzon Genomics, Sa
Representative Drug(s) D0YI0V Drug Info IC50 = 100 nM [1]
Patent ID WO2012045883
Title Cyclopropylamine Inhibitors of Oxidases.
Abstract The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I) as described and defined herein, and their use in therapy, including, e.g., the treatment or prevention of cancer.
Applicant(s) Oryzon Genomics Sa
Representative Drug(s) D0B6GK Drug Info IC50 = 1 to 100 nM [1]
Patent ID WO2012013727
Title Cyclopropylamine Derivatives Useful As Lsd1 Inhibitors.
Abstract The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.
Applicant(s) Oryzon Genomics S.A
Representative Drug(s) D0B6GK Drug Info IC50 = 1 to 100 nM [1]
Patent ID WO2014205511
Title Methods and Compositions for Modulating Cancer Stem Cells.
Abstract Disclosed are compositions and methods that use lysine demethylase inhibitors for inhibiting the growth of cancer stem cells or tumor initiating cells, for enhancing the biological effects of chemotherapeutic drugs or irradiation on cancer5 cells and/or for preventing cancer recurrence.
Applicant(s) University of Canberra
Representative Drug(s) D0D9CK Drug Info N.A. [1]
Patent ID WO2012156537
Title Lysine Demethylase Inhibitors Such As Cyclylcylopropamine Derivatives for Use In The Treatment of Thrombosis and Cardiovascular Diseases.
Abstract The invention relates to methods and compositions for the treatment or prevention of thrombosis, thrombus formation, a thrombotic event or complication, or a cardiovascular disease or event. In particular, the invention relates to an LSD inhibitor such as a 2-cyclylcyclopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing thrombosis, thrombus formation, a thrombotic event or complication, or a cardiovascular disease or event.
Applicant(s) Oryzon Genomics, Sa
Patent ID WO2012156531
Title Lysine Demethylase Inhibitors Such As Cyclylcylopropamine Derivatives for Use In The Treatment of Inflammatory Diseases or Conditions.
Abstract The invention relates to methods and compositions for the treatment or prevention of inflammation and inflammatory diseases or conditions. In particular, the invention relates to an LSD1 inhibitor, such as a 2-cyclylcylopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing inflammation and inflammatory diseases or conditions.
Applicant(s) Oryzon Genomics Sa
Patent ID WO2011106106
Title Lysine Demethylase Inhibitors for Diseases and Disorders Associated with Hepadnaviridae.
Abstract The present invention provides for the treatment or prevention of Hepadnaviridae infection and disease caused by Hepadnaviridae infection. In particular, the invention provides compositions and methods that affect the ability of Hepadnaviridae to utilize the host's cellular machinery as part of the virus' lifecycle. The invention relates to the discovery that interfering with the normal ability of viruses to utilize the host cell machinery with LSD1 inhibitors reduces HBV replication. Thus, the treatment and prevention of Hepadnaviridae infection and disease caused by Hepadnaviridae according to the invention comprises administering to an individual in need of treatment, a therapeutically effective amount of a LSD1 inhibitor. The individual in need of treatment can be a human or, e.g., another mammal.
Applicant(s) Oryzon Genomics, Sa
Patent ID WO2011106105
Title Inhibitors for Antiviral Use.
Abstract The present invention relates to the use of potent selective LSD1 inhibitors and LSD1/MAO-B inhibitors for treating or preventing viral infections. Furthermore, the present invention relates to the new use of cyclopropylamine acetamide derivatives or cyclopropylamine derivatives, as defined herein, for treating or preventing viral infection and treating or preventing reactivation of a virus after latency.
Applicant(s) Oryzon Genomics, Sa
United States Patent and Trademark Office (USPTO)
Patent ID US20140343118
Title Preparation of Arylcyclopropylamine Compounds Useful for The Treatment of Breast Cancer.
Applicant(s) Duke University, USA
Representative Drug(s) D0JE6I Drug Info Ki = 173000 nM Click to Show More [1]
2 D07IAO Drug Info Ki = 352000 nM [1]
3 D0C1TH Drug Info Ki = 456000 nM [1]
Patent ID US20140163017
Title Preparation of Substituted (E)-N-(1-Phenylethylidene)Benzohydrazide Analogs As Histone Demethylase Inhibitors Patent.
Applicant(s) University of Utah, Usa
Representative Drug(s) D0WT1Z Drug Info IC50 = 13 nM Click to Show More [1]
2 D05FVW Drug Info IC50 = 19 nM [1]
3 D0GA7D Drug Info IC50 > 3000 nM [1]
4 D0UG5Q Drug Info IC50 > 3000 nM [1]
Patent ID US20150225401
Title Cyclopropylamines As Lsd1 Inhibitors and Their Preparation.
Applicant(s) Incyte Corporation, USA
Representative Drug(s) D0R7RY Drug Info IC50 = 100 to 500 nM [1]
Patent ID US20150225394
Title Cyclopropylamines As Lsd1 Inhibitors and Their Preparation.
Applicant(s) Incyte Corporation, USA
Representative Drug(s) D0R7RY Drug Info IC50 = 100 to 500 nM [1]
Patent ID US20150225379
Title Cyclopropylamines As Lsd1 Inhibitors and Their Preparation.
Applicant(s) Incyte Corporation, USA
Representative Drug(s) D0R7RY Drug Info IC50 = 100 to 500 nM [1]
Patent ID US20150225375
Title Cyclopropylamines As Lsd1 Inhibitors and Their Preparation.
Applicant(s) Incyte Corporation, USA
Representative Drug(s) D0R7RY Drug Info IC50 = 100 to 500 nM [1]
Patent ID US20150065434
Title Cyclic Peptide Inhibitors of Lysine-Specific Demethylase 1.
Applicant(s) Musc Foundation for Research Development
Representative Drug(s) D04OEV Drug Info IC50 = 5000 nM [1]
Patent ID US20100324147
Title Trans-2-Arylcyclopropylamine Derivatives As Inhibitors of Lysine-Specific Demethylase 1, Monoamine Oxidase A and B, and Their Preparation and Use for The Treatment of Cancer.
Applicant(s) Duke University, Usa
European Patent Office (EPO)
Patent ID EP2177502
Title Preparation of N-(2 Phenylcyclopropyl) Amino Acid Derivatives for Treatment of Cancer.
Applicant(s) Oryzon Genomics Sa, Spain
Representative Drug(s) D0XH9M Drug Info IC50 = 18 nM Click to Show More [1]
2 D08IOP Drug Info IC50 = 22 nM [1]
3 D0UL9U Drug Info Ki < 1000 nM [1]
References  Top
REF 1 LSD1 inhibitors: a patent review (2010-2015).Expert Opin Ther Pat. 2016 May;26(5):565-80.
REF 2 Novel monoamine oxidase inhibitors: a patent review (2012 - 2014).Expert Opin Ther Pat. 2015 Jan;25(1):91-110.

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