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 T99347 Target Info
Target Name Metabotropic glutamate receptor 5 (mGluR5)
Synonyms MGLUR5; GPRC1E
Target Type Clinical trial Target
Gene Name GRM5
Biochemical Class GPCR glutamate
UniProt ID
GRM5_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2015098991
Title N-Alkylamide Derivative and Medicinal Use Thereof.
Abstract The purpose of the present invention is to provide a novel compound, which strongly inhibits metabotropic glutamate receptor 5 signal transduction. The present invention provides the N-alkylamide derivative represented below or a pharmacologically permissible acid addition salt thereof.
Applicant(s) Toray Industries, Inc
Representative Drug(s) D0OH5L Drug Info IC50 = 2.4 nM Click to Show More [1]
2 D0KG5I Drug Info IC50 = 8.2 nM [1]
Patent ID WO2015077246
Title Substituted Imidazopyridine and Triazolopyridine Compounds As Negative Allosteric Modulators of Mglur5.
Abstract Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. 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) Vanderbilt University
Representative Drug(s) D03ZXG Drug Info IC50 = 12 nM Click to Show More [1]
2 D08DMM Drug Info IC50 = 25 nM [1]
3 D0NJ9E Drug Info IC50 = 28 nM [1]
4 D0LI2I Drug Info IC50 = 75 nM [1]
Patent ID WO2015008073
Title 4-(3-Cyanophenyl)-6-Pyridinylpyrimidine Mglu5 Modulators.
Abstract The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 and n are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of inflammation, neurological or psychiatric disorders associated with modulating mGlu5 receptor function.
Applicant(s) Heptares Therapeutics Limited
Representative Drug(s) D0FS2X Drug Info Ki = 0.5 nM Click to Show More [1]
2 D0M4KF Drug Info Ki = 0.5 nM [1]
3 D0UX1S Drug Info Ki = 0.5 nM [1]
Patent ID WO2014124560
Title Mglur Regulators.
Abstract Provided herein are compounds of the formula I: (I), as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment or prevention of mGluR5 mediated disorders, such as acute and/or chronic neurological disorders, cognitive disorders and memory deficits, as well as acute and chronic pain.
Applicant(s) Hua Medicine (Shanghai) Ltd
Representative Drug(s) D01AFN Drug Info IC50 < 500 nM Click to Show More [1]
2 D04IGZ Drug Info IC50 < 500 nM [1]
3 D09CAM Drug Info IC50 < 500 nM [1]
4 D0DZ0M Drug Info IC50 < 500 nM [1]
5 D0Q1WV Drug Info IC50 < 500 nM [1]
6 D0QM1D Drug Info IC50 < 500 nM [1]
7 D0RG9J Drug Info IC50 < 500 nM [1]
Patent ID WO2014065270
Title Tetrahydrooxazolo-Pyridine Derivative.
Abstract Provided is a therapeutic agent for neurodegenerative disorders and psychiatric disorders related to mGluR5, the therapeutic agent comprising a compound represented by formula (I) or a pharmaceutical.
Applicant(s) Dainippon Sumitomo Pharma Co Ltd
Representative Drug(s) D0RU0W Drug Info IC50 = 32 nM Click to Show More [1]
2 D0LU9X Drug Info IC50 = 38 nM [1]
3 D0XX9N Drug Info IC50 = 46 nM [1]
4 D0AK4X Drug Info IC50 = 50 nM [1]
Patent ID WO2014060384
Title Ethynyl Derivatives As Modulators of Mglur5 Receptor Activity.
Abstract The present invention relates to ethynyl derivatives of formula (I) wherein Y is N or CH R1 is fluoro or chloro or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula (I) are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrom, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0O4KM Drug Info Ki = 24 nM Click to Show More [1]
2 D07EFT Drug Info Ki = 42 nM [1]
3 D05RUG Drug Info Ki = 46 nM [1]
4 D05VWD Drug Info Ki = 94 nM [1]
Patent ID WO2014034898
Title Pyridine Derivative and Medicine.
Abstract The main purpose of the invention is to provide a novel pyridine derivative or a pharmaceutically acceptable salt thereof. Examples of the invention include a pyridine derivative represented by general formula [1], and a pharmaceutically acceptable salt thereof. This compound or a pharmaceutically acceptable salt thereof exhibits mGluR5 inhibitory activity, and can therefore be used as an agent for the prevention or treatment of, e.g., pain (for example, acute pain, chronic pain, inflammatory pain, neuropathic pain, hyperalgesia, thermal hyperalgesia, allodynia, pain due to noxious thermal stimulation, pain due to noxious mechanical stimulation, pain in the lower urinary tract or reproductive organs, or migraine), pruritus, lower urinary tract symptoms or lower urinary tract disorders, gastroesophageal reflux disease (GERD), gastroesophageal reflux associated with transient lower esophageal sphincter relaxation (TLESR), and diseases of the central nervous system.
Applicant(s) Nippon Shinyaku
Representative Drug(s) D0L7YW Drug Info IC50 = 5.3 nM Click to Show More [1]
2 D0V3SA Drug Info IC50 = 10 nM [1]
3 D0AZ6X Drug Info IC50 = 36 nM [1]
4 D0CI9L Drug Info IC50 = 74 nM [1]
5 D0V2VM Drug Info IC50 = 131 nM [1]
6 D0DR0S Drug Info IC50 = 161 nM [1]
Patent ID WO2014030128
Title Diazepinone Derivatives Useful for The Treatment of Fragile X Syndrome, Parkinsons or Reflux Disease.
Abstract The invention relates to compound of the formula (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
Applicant(s) Novartis Ag
Representative Drug(s) D0J4QE Drug Info IC50 < 1 nM Click to Show More [1]
2 D0DL7P Drug Info IC50 = 7 nM [1]
3 D0MM8M Drug Info IC50 = 14 nM [1]
4 D09QQS Drug Info IC50 = 24 nM [1]
5 D0Q4ST Drug Info IC50 = 44 nM [1]
Patent ID WO2013144172
Title Novel Pyrazolopyrimidines.
Abstract This invention relates to novel pyrazolopyrimidines and their use as metabotropic glutamate receptor antagonists (mGlu5 receptor antagonists), pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of mGlu5 receptor mediated disorders.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D06JFS Drug Info IC50 = 33 nM Click to Show More [1]
2 D0M3VE Drug Info IC50 = 43 nM [1]
3 D0K4LQ Drug Info IC50 = 59 nM [1]
4 D0A7NX Drug Info IC50 = 63 nM [1]
5 D0B3CG Drug Info IC50 = 63 nM [1]
Patent ID WO2013040535
Title Bicarbocyclic and Tricarbocyclic Ethynyl Derivatives and Uses of Same.
Abstract The present invention provides compounds of formula (1): where R1, R2, X. Y and n are as described herein, and pharmaceutical compositions, uses and methods comprising same.
Applicant(s) H. Lundbeck A / S
Representative Drug(s) D0MI7K Drug Info IC50 = 1.6 nM Click to Show More [1]
2 D06FVQ Drug Info IC50 = 3.8 nM [1]
3 D09UVF Drug Info IC50 = 5.9 nM [1]
Patent ID WO2014060398
Title Ethynyl Derivatives As Modulators of Mglur5 Receptor Activity.
Abstract The present invention relates to ethynyl derivatives of formula (I) wherein Y is N or CH R1 is fluoro or chloro R2 is hydrogen or methyl or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrom, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0IK9N Drug Info Ki = 67 nM [1]
Patent ID WO2014060394
Title Ethynyl Derivatives As Modulators of Mglur5 Receptor Activity.
Abstract The present invention relates to ethynyl derivatives of formula (I) or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula (I) are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrom, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D01BSX Drug Info Ki = 15 nM [1]
Patent ID WO2013081094
Title Imidazo[1,2-A]Pyridine Derivative and Use Thereof for Medical Purposes.
Abstract The purpose of the present invention is to provide a compound that can act on mGluR5 selectively to inhibit the signaling of mGluR5. The present invention provides an imidazo[1,2-a]pyridine derivative typified by the compound shown below or a pharmacologically acceptable acid addition salt thereof.
Applicant(s) Toray Industries, Inc
Representative Drug(s) D0VI3F Drug Info IC50 = 13 nM [1]
Patent ID WO2012139876
Title Enteric formulations of Metabotropic Glutamate Receptor Modulators.
Abstract A pharmaceutical formulation comprising at least one negative allosteric modulator of the mGluR5 receptor and at least one pharmaceutically acceptable excipient in the form of an enteric tablet, enteric capsule or multiple unit dosage form has improved activity for the treatment of Parkinson's disease.
Applicant(s) Merz Pharma Gmbh & Co Kgaa
Representative Drug(s) D0SZ5A Drug Info N.A. [1]
Patent ID WO2008015269
Title Substituted Pyrazolopyrimidines, A Process for Their Preparation and Their Use As Medicine.
Abstract Substituted pyrazolopyrimidine derivatives of formula (I) wherein Y1, Y2, Y3, Y4 represent N or C-, whereby at least two of the groups Y1 to Y4 denote a carbon atom, R1 represents chloro or bromo, R2 to R7 represent e.g. hydrogen, methyl or ethyl; and R10 and R11 independent ly represent e.g. hydrogen or C1-C6alkyl, are potent mGluR5 modulators and are useful for the prevention of acute and chronic neurological disorders.
Applicant(s) Merz Pharma Gmbh & Co Kgaa
Representative Drug(s) D0SZ5A Drug Info N.A. [1]
Patent ID WO2015200682
Title Substituted 4-Alkoxypicolinamide Analogs Ds Mglur5 Negative Allosteric Modulators.
Abstract Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. 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) Vanderbilt University
Patent ID WO2015044270
Title Mono-Phosphate Salt of 6-Fluoro-2-[4-(Pyridin-2-Yl)But-3-Yn-1-Yl]Imidazo[1,2A]Pyridine and Polymorphs Thereof As Negative Allosteric Modulator of Mglu5 Receptor.
Abstract The present invention relates to crystalline and amorphous forms of 6-fluoro-2-[4-(pyridin-2-yl)but-3-yn-1-yl]imidazo[1,2-a]pyridine mono-phosphate salt and methods of making these solid forms thereof. The invention compounds are modulators of mGlu5 which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGlu5 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGlu5 is involved.
Applicant(s) Addex Pharma Sa
Patent ID WO2012088365
Title Bicyclo[3.2.1]Octyl Amide Derivatives and Uses of Same.
Abstract The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; pharmaceutical compositions and methods using the same.
Applicant(s) H. Lundbeck A / S
Patent ID WO2010011570
Title Adamantyl Diamide Derivatives and Uses of Same.
Abstract The present invention provides adamantyl-diamide derivatives of formula (I): wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
Applicant(s) H. Lundbeck A/S
Patent ID WO20110087758
Title Adamantyl Amide Derivatives and Uses of Same.
Applicant(s) H Lundbeck A / S
United States Patent and Trademark Office (USPTO)
Patent ID US20140206876
Title 2-(Substituted Ethynyl)Quinoline Derivatives As Mglur5 Antagonists.
Applicant(s) Korea Institute of Science and Technology
Representative Drug(s) D0PJ8X Drug Info IC50 = 410 nM Click to Show More [1]
2 D0MB0V Drug Info IC50 = 430 nM [1]
3 D0HG1W Drug Info IC50 = 750 nM [1]
4 D0XQ4T Drug Info IC50 = 940 nM [1]
Patent ID US20160096833
Title Substituted 6-Aryl-Imidazopyridine and 6-Aryl-Triazolopyridine Carboxamide Analogs As Negative Allosteric Modulators of Mglur5.
Representative Drug(s) D0XB2W Drug Info IC50 = 60 nM Click to Show More [1]
2 D0GS6T Drug Info IC50 = 170 nM [1]
3 D0T9IR Drug Info IC50 = 378 nM [1]
Patent ID US20150266866
Title Substituted Bicyclic Heteroaryl Carboxamide Analogs As Mglur5 Negative Allosteric Modulators.
Representative Drug(s) D0QE8S Drug Info IC50 = 3.4 nM Click to Show More [1]
2 D0CI3E Drug Info IC50 = 24 nM [1]
3 D0N6HP Drug Info IC50 = 39 nM [1]
European Patent Office (EPO)
Patent ID EP2650284
Title Heterocyclic Derivatives As Metabotropic Glutamate Receptor Modulators.
Applicant(s) Merz Pharma Gmbh & Co Kgaa
Representative Drug(s) D09VNK Drug Info IC50 = 51 nM Click to Show More [1]
2 D0B4IU Drug Info IC50 = 67 nM [1]
3 D0M8IR Drug Info IC50 = 76 nM [1]
Japan Patent Office (JPO)
Patent ID JP2015059118
Title Tetrahydopyrazolopyrazine Derivatives.
Applicant(s) Dainippon Sumitomo Pharma Co Ltd
Representative Drug(s) D0D3GL Drug Info IC50 = 75 nM Click to Show More [1]
2 D0BS0K Drug Info IC50 = 87 nM [1]
3 D0V5GR Drug Info IC50 = 106 nM [1]
4 D07KER Drug Info IC50 = 129 nM [1]
5 D07JTE Drug Info IC50 = 150 nM [1]
Patent ID JP2014185092
Title Tetrahydrooxazolopyridine Derivative.
Applicant(s) Dainippon Sumitomo Pharma Co Ltd
Representative Drug(s) D0DL1O Drug Info IC50 = 14 nM Click to Show More [1]
2 D0GQ2Z Drug Info IC50 = 42 nM [1]
References  Top
REF 1 mGlu5 negative allosteric modulators: a patent review (2013 - 2016).Expert Opin Ther Pat. 2017 Jun;27(6):691-706.

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