Patent(s) and the Corresponding Patented Drug(s) |
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World Intellectual Property Organization (WIPO) |
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) |
D02CIX |
Drug Info
|
IC50 > 100000 nM |
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[1] |
2
|
D04PWX
|
Drug Info
|
IC50 > 100000 nM
|
[1] |
3
|
D07DIJ
|
Drug Info
|
IC50 > 100000 nM
|
[1] |
4
|
D0R2YA
|
Drug Info
|
IC50 > 100000 nM
|
[1] |
5
|
D0W9VF
|
Drug Info
|
IC50 > 100000 nM
|
[1] |
Patent ID |
WO2013016580 |
Title |
Monoamine Oxidase Inhibitors and Methods for Treatment and Diagnosis of Prostate Cancer. |
Abstract |
A mechanism of monoamine oxidases (MAOs) driven epithelium-to-mesenchymal transition (EMT) is disclosed. Also disclosed are methods for treating cancer by inhibiting or suppressing MAOs in cancer cells. Novel MAOs inhibitors, such as small molecules, siRNA, shRNA, antisense oligonucleotides, aptamers, decoys, and pharmaceutical compositions useful for treating cancer by disrupting the workings of MAOs are provided. In particular, a class of conjugates formed by covalently conjugating near infrared dye 783, IR-780, and MHI-148 to a MAO inhibitor, such as clorgyline, with and without encapsulation it in a nanoparticle is provided. Other aspects of the invention include methods for forming the nano-conjugates, method for monitoring treatment progress in a cancer patient by monitoring the changes in MAO activity, methods for screening patients who are at risk of cancer or differentiating different forms of cancer by assaying the level and location of MAO activity. |
Applicant(s) |
University of Southern California |
Representative Drug(s) |
D01ZSO |
Drug Info
|
N.A. |
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[2] |
2
|
D09QDP
|
Drug Info
|
N.A.
|
[2] |
3
|
D0H0HJ
|
Drug Info
|
N.A.
|
[2] |
4
|
D0P9AC
|
Drug Info
|
N.A.
|
[2] |
5
|
D0R0UJ
|
Drug Info
|
N.A.
|
[2] |
Patent ID |
WO2012051374 |
Title |
Use of Monoamine Oxidase Inhibitors To Improve Epithelial Biology. |
Abstract |
The invention provides a method for improving hair biology, e.g., hair growth. The method comprises administering to a subject a monoamine oxidase inhibitor and a vasodilator, a zinc salt of a carboxylic acid, a xanthine compound, pyrithione or a salt thereof, saponin, tritapene, crataegolic acid, celastrol, asiatic acid, an inhibitor of 5-alpha-reductase, 1,4-methyl-4-azasteroid, an androgen receptor antagonist, azelaic acid or a derivate thereof, cyclosporin, triiodothyronine, diazoxide, retinoic acid, a prostaglandin analogue, aminexil, carnitine tartrate, apigenin, procapil, or adenosine, in an amount effective to achieve a desired effect. The invention further provides a method of reducing or delaying the appearance of an age-related skin imperfection. The method comprises administering to the subject a composition comprising an MAO inhibitor. A kit for improving hair growth also is provided. |
Applicant(s) |
Procter & Gamble |
Representative Drug(s) |
D01ZSO |
Drug Info
|
N.A. |
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[2] |
2
|
D06QRW
|
Drug Info
|
N.A.
|
[2] |
3
|
D09QDP
|
Drug Info
|
N.A.
|
[2] |
4
|
D0P9AC
|
Drug Info
|
N.A.
|
[2] |
5
|
D0R0UJ
|
Drug Info
|
N.A.
|
[2] |
6
|
D0S2UG
|
Drug Info
|
N.A.
|
[2] |
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 > 300000 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 > 300000 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 > 300000 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 > 40000 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 >= 40000 nM |
[1] |
Patent ID |
WO2014056070 |
Title |
(-)-Deprenyl and Related Compounds for The Treatment of Alopecia. |
Abstract |
The present invention includes methods of preventing or minimizing cancer therapy induced alopecia (hair loss) in a subject, the method including administering to the subject an effective amount of (-)-deprenyl, a related compound, or a salt thereof. The present invention also includes methods of preventing or minimizing additional side effects of cancer therapies other than cancer therapy induced alopecia by the administration of an effective amount of (-)- deprenyl, a related compound, or a salt thereof. |
Applicant(s) |
Brandon University |
Representative Drug(s) |
D0S7KA |
Drug Info
|
N.A. |
[2] |
Patent ID |
WO2012050594 |
Title |
Treatment for Cocaine Addiction. |
Abstract |
A novel pharmaceutical composition is provided for the control of stimulant effects, in particular treatment of cocaine addiction, or further to treatment of both cocaine and alcohol dependency, including simultaneous therapeutic dose application or a single dose of a combined therapeutically effective composition of disulfiram and selegiline compounds or pharmaceutically acceptable non-toxic salt thereof. |
Applicant(s) |
Tonix Pharmaceuticals, Inc |
Representative Drug(s) |
D0S2UG |
Drug Info
|
N.A. |
[2] |
Patent ID |
WO2013182625 |
Title |
Pharmaceutical formulation with Propargylamine Compound. |
Abstract |
Stable pharmaceutical formulations comprising a propargylamine monoamine oxidase inhibitor compound such as rasagiline or salt thereof, e.g. rasagiline tartrate, mesylate, succinate or hydrochloride. The formulations contain calcium sulphate as inert excipient, preferably in the form of calcium sulphate dihydrate. The formulations may additionally contain a weak acid such as critic acid, which enhances stability further. |
Applicant(s) |
Actavis Group Ptc Ehf |
Patent ID |
WO2013118126 |
Title |
Ladostigil Therapy for Immunomodulation. |
Abstract |
Methods for treating individuals suffering from inflammation, specifically systemic inflammation including septic shock and inflammatory conditions affecting the gastrointestinal, myocardial and endocrine systems with ladostigil, are provided. |
Applicant(s) |
Yissum Research Development Company of the Hebrew University of Jerusalem Ltd |
Patent ID |
WO2013070526 |
Title |
Methods for The Treatment of Skin Neoplasms. |
Abstract |
Methods of treating skin neoplasms using a monoamine oxidase inhibitor, e.g., a propynylaminoindan (such as rasagiline) are provided. Pharmaceutical compositions and kits comprising monoamine oxidase inhibitors are also provided. |
Applicant(s) |
Teikoku Pharma Usa, Inc |
Patent ID |
WO085437 |
Title |
Combinations for The Treatment of Dementia, and The Enhancement of Cognitive Function. |
Applicant(s) |
The Wwk Trust & Jd Med Services |
United States Patent and Trademark Office (USPTO) |
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 > 300000 nM |
[1] |
Patent ID |
US20120329800 |
Title |
Treatment of Muscular Dystrophies and Associated Conditions By Administration of Monoamine Oxidase Inhibitors. |
Applicant(s) |
University of Padua |
Representative Drug(s) |
D0R0UJ |
Drug Info
|
N.A. |
[2] |
Patent ID |
US0320742 |
Title |
Combinations Comprising 3-Phenyl-Sulfonyl-8-Piperazin-1-Yl-Quinoline. |
Applicant(s) |
Axovant Sciences Ltd |
Patent ID |
US0290201 |
Title |
Treatment of Muscular Distrophies and Associated Conditions By Administration of Monoamine Oxidase Inhibitors. |
Applicant(s) |
Universit Degli Studi Di Padova, Italy |
Patent ID |
US0182018 |
Title |
Treatment of Dopaminergic Disorders. |
Applicant(s) |
Northwestern University |
Patent ID |
US0143902 |
Title |
Combination of Morphinan Compounds and Antidepressant for The Treatment of Pseudobulbar Affect, Neurological Diseases, Intractable and Chronic Pain and Brain Injury. |
Applicant(s) |
Concert Pharmaceuticals, Inc |
Patent ID |
US0067187 |
Title |
Methods for Treating or Preventing Migraines. |
Applicant(s) |
Validus Pharmaceuticals Llc |
Patent ID |
US0038550 |
Title |
Methods and Compositions for Treating Conditions Associated with Memory Loss. |
Patent ID |
US0029371 |
Title |
Mao Inhibitors and Their Conjugates As Therapeutics for The Treatment of Brain Cancer. |
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 >= 40000 nM |
[1] |
China National Intellectual Property Administration (CNIPA) |
Patent ID |
CN105017195 |
Title |
4-Hydroxycoumarin-3-Schiff Base Derivate and Use Thereof for Curing AlzheimerS Disease. |
Applicant(s) |
University China Pharma |
Intellectual Property Office of United Kingdom (IPOUK) |
Patent ID |
GB25327444 |
Title |
A Chocolate Composition Comprising A Monoamine Oxidase Inhibitor. |