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 T18664 Target Info
Target Name Monoglyceride lipase (MAGL)
Synonyms Monoacylglycerol lipase; MGL; Lysophospholipaselike; Lysophospholipase-like; Lysophospholipase homolog; HUK5; HU-K5
Target Type Clinical trial Target
Gene Name MGLL
Biochemical Class Carboxylic ester hydrolase
UniProt ID
MGLL_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2017021805
Title 1,1,1-Trifluoro-3-Hydroxypropan-2-Yl Carbamate Derivatives and 1,1,1-Trifluoro-4-Hydroxybutan-2-Yl Carbamate Derivatives As Magl Inhibitors.
Abstract The present invention provides, in part, compounds of Formula I and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, traumatic brain injury, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.
Applicant(s) Pfizer Inc
Representative Drug(s) D08EMW Drug Info IC50 = 1 nM Click to Show More [1]
2 D0C5SQ Drug Info IC50 = 1 nM [1]
3 D0FK7E Drug Info IC50 = 1 nM [1]
4 D0Y7LM Drug Info IC50 = 4 nM [1]
5 D0L6XG Drug Info IC50 = 7 nM [1]
6 D05DBG Drug Info IC50 = 8 nM [1]
7 D0NK4T Drug Info IC50 > 3000 nM [1]
8 D0Q4OB Drug Info IC50 > 3000 nM [1]
Patent ID WO2016014975
Title Urea/Carbamates Faah Magl or Dual Faah/Magl Inhibitors and Uses Thereof.
Abstract Disclosed are compounds that may be used to inhibit the action of fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL) or dual FAAH/MAGL.
Applicant(s) Northeastern University
Representative Drug(s) D08SMT Drug Info IC50 = 10 to 100 nM Click to Show More [1]
2 D00IPI Drug Info IC50 > 1000 nM [1]
3 D02ZUW Drug Info IC50 > 1000 nM [1]
4 D09RGE Drug Info IC50 > 1000 nM [1]
Patent ID WO2015179559
Title Pyrazole Compounds and Methods of Making and Using Same.
Abstract Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of one or more of MAGL, ABHD6, and FAAH. Furthermore, the subject compounds and compositions are useful for the treatment of, for example, pain, solid tumors and/or obesity.
Applicant(s) Abide Therapeutics, Inc
Representative Drug(s) D0LL0X Drug Info IC50 < 100 to 1000 nM Click to Show More [1]
2 D0O9DS Drug Info IC50 < 100 to 1000 nM [1]
3 D0X9GC Drug Info IC50 < 100 to 1000 nM [1]
Patent ID WO2013142307
Title Carbamate Compounds and of Making and Using Same.
Abstract Provided herein are carbamate compounds which may be useful in the treatment of, for example, pain, solid tumors and/or obesity.
Applicant(s) Abide Therapeutics, Inc
Representative Drug(s) D00TVG Drug Info IC50 <= 100 nM Click to Show More [1]
2 D0Z7FL Drug Info IC50 <= 100 nM [1]
Patent ID WO2017087863
Title Pyrazole Compounds and Methods of Making and Using Same.
Abstract Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL and/or FAAH. Furthermore, the subject compounds and compositions are useful for the treatment of, for example, pain.
Applicant(s) Abide Therapeutics, Inc
Representative Drug(s) D0S2JF Drug Info IC50 < 100 nM Click to Show More [1]
2 D0YM0G Drug Info IC50 < 100 nM [1]
3 D04ZEX Drug Info N.A. [1]
Patent ID WO2017087854
Title Pyrazole Compounds and Methods of Making and Using Same.
Abstract Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL and/or ABHD6. Furthermore, the subject compounds and compositions are useful for the treatment of, for example, pain.
Applicant(s) Abide Therapeutics, Inc
Representative Drug(s) D0S2JF Drug Info IC50 < 100 nM Click to Show More [1]
2 D0YM0G Drug Info IC50 < 100 nM [1]
3 D04ZEX Drug Info N.A. [1]
Patent ID WO2015003002
Title Pyrrolo-Pyrrole Carbamate and Related organic Compounds, Pharmaceutical Compositions, and Medical Uses Thereof.
Abstract The invention provides pyrrolo-pyrrole carbamate and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., solid tumor cancer, obesity, Down's syndrome, Alzheimer's disease, or pain, in a patient. The octahydropyrrolo pyrrole carbamates could be derived from hexafluoroisopropanol, ,-disuccinimide and such. The activity of carbamates in MAGL, FAAH, and ABHD6 assays are also described.
Applicant(s) Abide Therapeutics, Inc
Representative Drug(s) D0TU6D Drug Info IC50 < 100 nM Click to Show More [1]
2 D0GT0I Drug Info N.A. [1]
Patent ID WO2013103973
Title Carbamate Compounds and of Making and Using Same.
Abstract This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compunds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.
Applicant(s) Abide Therapeutics, Inc
Representative Drug(s) D0LC5Y Drug Info IC50 = 8 to 27 nM Click to Show More [1]
2 D0J6TA Drug Info N.A. [1]
Patent ID WO2016158956
Title Heterocyclic Compound.
Abstract Provided is a compound having an MAGL inhibitory effect, and expected to be useful as an agent for the prevention or treatment of neurodegenerative diseases (e.g., Alzheimer&#039;s disease, Parkinson&#039;s dis.
Applicant(s) Takeda Pharmaceutical Company Limited
Representative Drug(s) D0J0UC Drug Info N.A. Click to Show More [1]
2 D0S9MR Drug Info N.A. [1]
3 D0VS7X Drug Info N.A. [1]
Patent ID WO2016046130
Title Methods and Pharmaceutical Compositions for The Treatment of Fibrosis.
Abstract The present invention relates to methods and pharmaceutical compositions for the treatment of fibrosis. In particular, the present invention relates to a method of treating fibrosis in a subject in need thereof comprising administering the subject with a therapeutically effective amount of at least one monoacylglycerol lipase (MGL) inhibitor.
Applicant(s) Inserm Inst Nat De La Sant et De La Rech M Dicale
Representative Drug(s) D05SWA Drug Info N.A. Click to Show More [1]
2 D07YWE Drug Info N.A. [1]
3 D0UW6S Drug Info N.A. [1]
Patent ID WO2015099196
Title 4-(Piperrazin-1-Yl)-Pyrrolidin-2-One Compounds As Monoacylglycerol Lipase (Magl) Inhibitors.
Abstract The present invention aims to provide a compound having an MAGL inhibitory action, and useful as a prophylactic or therapeutic agent for neurodegenerative diseases (e.g., Alzheimer's disease, Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, traumatic brain injury, glaucoma, multiple sclerosis and the like), anxiety disorder, pain (e.g., inflammatory pain, carcinomatous pain, nervous pain and the like), epilepsy and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof.
Applicant(s) Takeda Pharmaceutical Company Limited
Representative Drug(s) D00VBP Drug Info N.A. Click to Show More [1]
2 D03HHN Drug Info N.A. [1]
3 D03LKM Drug Info N.A. [1]
4 D0D2YG Drug Info N.A. [1]
5 D0TT7U Drug Info N.A. [1]
6 D0TW7K Drug Info N.A. [1]
Patent ID WO2016183097
Title Methods of Treating Inflammation or Neuropathic Pain.
Abstract Provided herein are methods of treating inflammation or neuropathic pain using an effective dose of a monoacylglycerol lipase inhibitor or a composition thereof.
Applicant(s) Abide Therapeutics, Inc
Representative Drug(s) D0LC5Y Drug Info IC50 = 8 to 27 nM [1]
Patent ID WO2013049293
Title Monoacylglycerol Lipase Inhibitors for The Treatment of Metabolic Diseases and Related Disorders.
Abstract Disclosed are compounds, compositions and methods for treating metabolic diseases, including obesity and diabetes. Such compounds are represented by formula (I) as follows: wherein Y and Z are defined herein.
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D00KFI Drug Info IC50 = 12 nM [1]
Patent ID WO2013049289
Title Monoacylglycerol Lipase Inhibitors for The Treatment of Metabolic Diseases and Related Disorders.
Abstract Disclosed are compounds, compositions and methods for treating metabolic diseases, including obesity and diabetes, and for reducing weight gain. Such compounds are represented by formula (I) as follows: wherein Y and Z are defined herein.
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D0OK3K Drug Info IC50 < 5 nM [1]
Patent ID WO2016149401
Title Piperazine Carbamates and Methods of Making and Using Same.
Abstract Provided herein are piperazine carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL and/or ABHD6. Furthermore, the subject compounds and compositions are useful for the treatment of pain.
Applicant(s) Abide Therapeutics, Inc
Representative Drug(s) D09LAD Drug Info N.A. [1]
Patent ID WO2013177492
Title Novel Lipase Inhibitors, Reporter Substrates and Uses Thereof.
Abstract The invention provides for novel lipase inhibitors, and compositions and devices comprising the same. The invention further provides for methods for treatment of disorders comprising administration of novel diacylglycerol lipase inhibitors, and compositions and devices comprising said inhibitors. In some embodiments, the disorders are pancreatitis, obesity, shock or pancreatic necrosis. The invention further provides for novel ether lipid reporter compounds and methods of assaying enzymatic activity comprising contacting a compound with a novel ether lipid reporter compound.
Applicant(s) Northeastern University
Representative Drug(s) D0TL1G Drug Info N.A. [1]
Patent ID WO2013174508
Title Novel 1,3-Benzoxazol-2(3H)-Ones and Their Use As Medicaments and Cosmetics.
Abstract The present invention relates to a novel class of 1,3-benzoxazol-2(3H) -ones of formula (1) and their use as a medicament, preferably as a dermatologic agent, and as a cosmetic. These novel compounds are particularly useful in treating and/or preventing inflammation, irritation, itching, pruritus, pain, oedema and/or pro-allergic or allergic conditions in a patient. Usually they are topically applied to the skin or mucosa in the form of a pharmaceutical or cosmetic composition comprising the compound and a pharmaceutically and/or cosmetically acceptable carrier.
Applicant(s) Dr. August Wolff Gmbh & Co. Kg Arzneimittel
Representative Drug(s) D0V7PO Drug Info N.A. [1]
Patent ID WO2013049332
Title Inhibitors of Monoacylglycerol Lipase and Methods of Their Use.
Abstract Provided herein are compounds which mediate the activity of monoacyglycerol lipase (MAGL). Also provided are pharmaceutical compositions comprising a compound provided herein, and methods for treating, preventing and/or managing a MAGL mediated condition using a compound or pharmaceutical composition as provided herein.
Applicant(s) Infinity Pharmaceuticals, Inc
Representative Drug(s) D0G9NQ Drug Info N.A. [1]
Patent ID WO2010124122
Title Heteroaromatic and Aromatic Piperazinyl Azetidinyl Amides As Monoacylglycerol Lipase Inhibitors.
Abstract Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, W and (Ia): are defined herein.
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D0B5BT Drug Info N.A. [1]
Patent ID WO2010124121
Title Heteroaromatic and Aromatic Piperazinyl Azetidinyl Amides As Monoacylglycerol Lipase Inhibitor.
Abstract Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I), wherein Y, r, R2 and Z are defined herein.
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D0B5BT Drug Info N.A. [1]
United States Patent and Trademark Office (USPTO)
Patent ID US20130102584
Title Piperidin-4-Yl-Azetidine Diamides As Monoacylglycerol Lipase Inhibitors.
Representative Drug(s) D00PFS Drug Info IC50 < 5 nM Click to Show More [1]
2 D0VY7R Drug Info IC50 < 5 nM [1]
References  Top
REF 1 A patent review of Monoacylglycerol Lipase (MAGL) inhibitors (2013-2017).Expert Opin Ther Pat. 2017 Dec;27(12):1341-1351.

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