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 T62820 Target Info
Target Name Metabotropic glutamate receptor 2 (mGluR2)
Synonyms mGLUR2; Group II metabotropic glutamate receptor; Glutamate receptor mGLU2; GPRC1B
Target Type Clinical trial Target
Gene Name GRM2
Biochemical Class GPCR glutamate
UniProt ID
GRM2_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2014133022
Title Tetrahydroimidazo[1,5-D][1,4]Oxazepine Derivative.
Abstract A compound represented by general formula (I) [wherein R represents a hydrogen atom, a C1-6 alkyl group or the like; R1 represents a C1-6 alkyl group, a C1-6 alkoxy group or the like; R2 represents a.
Applicant(s) Eisai R & D Management Co., Ltd
Representative Drug(s) D0LI2E Drug Info IC50 = 1.1 nM Click to Show More [1]
2 D0NE0W Drug Info IC50 = 3.7 nM [1]
3 D0Q2FC Drug Info IC50 = 4.7 nM [1]
4 D0C2ZJ Drug Info IC50 = 10 nM [1]
5 D0N9IA Drug Info IC50 = 60 nM [1]
6 D0CZ6T Drug Info IC50 = 103.4 nM [1]
Patent ID WO2013066736
Title Quinoline Carboxamide and Quinoline Carbonitrile Derivatives As Mglur2-Negative Allosteric Modulators, Compositions, and Their Use.
Abstract The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0K1RU Drug Info IC50 = 5 nM Click to Show More [1]
2 D09NRH Drug Info IC50 = 9 nM [1]
3 D0OT4O Drug Info IC50 = 12 nM [1]
4 D03KYL Drug Info IC50 = 21 nM [1]
5 D09JZA Drug Info IC50 = 21 nM [1]
6 D04LRT Drug Info IC50 = 24 nM [1]
7 D0E5QO Drug Info IC50 = 38 nM [1]
Patent ID WO2012068067
Title 4-Substituted-3-Phenylsulfanylmethyl-Bicyclo[3.1.0]Hexane Compounds As Mglur 2/3 Antagonists.
Abstract A mGlu2/3 receptor antagonist of the formula (I):, its uses, and methods for its preparation are described.
Applicant(s) Eli Lilly and Company
Representative Drug(s) D0SF1E Drug Info IC50 = 12.7 nM Click to Show More [1]
2 D0KV7D Drug Info IC50 = 15.4 nM [1]
Patent ID WO2012068041
Title 4-Substituted-3-Benzyloxy-Bicyclo[3.1.0]Hexane Compounds As Mglur 2/3 Antagonists.
Abstract A mGlu2/3 receptor antagonist of the formula: (formula), its uses, and methods for its preparation are described.
Applicant(s) Eli Lilly and Company
Representative Drug(s) D01VZE Drug Info IC50 = 13.1 nM Click to Show More [1]
2 D0D4OW Drug Info IC50 = 43.3 nM [1]
Patent ID WO2008119689
Title Pyridine and Pyrimidine Derivatives As Mglur2 Antagonists.
Abstract The present invention relates to compounds of formula (I), a process for the manufacture thereof, their use for the preparation of medicaments for treating CNS disorders and pharmaceutical compositions containing them. Compounds of formula (I) are represented by general formula (I) wherein Q, A, B, X, Y, R 1 and R 2 are defined as in the specification.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0H2BU Drug Info Ki = 2 nM Click to Show More [1]
2 D0O9TL Drug Info Ki = 5.3 nM [1]
3 D09OQZ Drug Info Ki = 14.3 nM [1]
4 D0YZ7D Drug Info Ki = 15 nM [1]
5 D0N0FA Drug Info Ki = 15.6 nM [1]
Patent ID WO2003066623
Title Dihydrobenzodiazepin-2-One Derivatives for The Treatment of Neurological Disorders.
Abstract This invention relates to dihydro-benzo [b] [1, 4] diazepin-2-one derivatives of the general formula: (Formula I); wherein R1, R2, X and Y are as defined in the specification and R3 is a six-membered aromatic heterocycle containing 1 to 3 nitrogen atoms or a pyridine-N-oxide as further defined in the specification. The invention further relates to medicaments containing these compounds, a process for their preparation as well as their use for preparation of medicaments for the treatment or prevention of acute and/or chronic neurological disorders.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D09WXH Drug Info IC50 = 6.4 nM Click to Show More [1]
2 D04VAE Drug Info IC50 = 34 nM [1]
Patent ID WO200283665
Title Dihydrobenzo[B][1,4]Diazepin-2-One Derivatives As Metabotropic Glutamate Receptor 2 (Mglur2) Antagonists.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D09WXH Drug Info IC50 = 6.4 nM Click to Show More [1]
2 D04VAE Drug Info IC50 = 34 nM [1]
Patent ID WO200283652
Title Dihydrobenzo[B][1,4]Diazepin-2-Ones As Mglur2 Antagonists for Treatment of Neurological Disorders.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D09WXH Drug Info IC50 = 6.4 nM Click to Show More [1]
2 D04VAE Drug Info IC50 = 34 nM [1]
Patent ID WO200129012
Title Benzodiazepine Derivatives As Metabotropic Glutamate Receptor Antagonists.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D09WXH Drug Info IC50 = 6.4 nM Click to Show More [1]
2 D04VAE Drug Info IC50 = 34 nM [1]
Patent ID WO200129011
Title Benzodiazepine Derivatives As Metabotropic Glutamate Receptor Antagonists.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D09WXH Drug Info IC50 = 6.4 nM Click to Show More [1]
2 D04VAE Drug Info IC50 = 34 nM [1]
Patent ID WO2012099200
Title Pyrazole Derivative.
Abstract A compound represented by formula [I] [wherein R1 represents an alkyl group or the like; R2 represents a hydrogen atom or the like; the ring A represents a phenyl group or the like; R3 represents a hy.
Applicant(s) Taisho Pharmaceutical Co., Ltd
Representative Drug(s) D0QM1R Drug Info IC50 = 2.7 nM Click to Show More [1]
2 D02RRE Drug Info IC50 = 36.4 nM [1]
3 D0S5SK Drug Info IC50 < 100 nM [1]
4 D0HD8F Drug Info N.A. [1]
Patent ID WO2012020820
Title Heteroaryl-Pyrazole Derivative.
Abstract A compound represented by formula [I] and a pharmaceutically accepted salt of said compound are a novel compound exerting antagonistic activity against group II metabotropic glutamate (mGlu) receptors and a pharmaceutically accepted salt of said novel compound, and are effective as a novel preventive or therapeutic agent for disorders such as mood disorders (depressive disorder, bipolar disorder), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, a specific phobic disorder, acute stress disorder), schizophrenia, Alzheimer's disease, cognitive impairment, dementia, drug dependence, convulsions, shivering, pain, and sleep disorders.
Applicant(s) Taisho Pharmaceutical Co., Ltd
Representative Drug(s) D03PRA Drug Info IC50 = 1.29 nM Click to Show More [1]
2 D0K0ZX Drug Info IC50 = 9.06 nM [1]
3 D0O6QC Drug Info N.A. [1]
Patent ID WO2012015024
Title Ethinyl-Pyrazole Derivative.
Abstract Provided is a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof having antagonistic activity against group II metabolism-type glutamic acid (m-Glu) receptors. The.
Applicant(s) Taisho Pharmaceutical Co., Ltd
Representative Drug(s) D0BP6R Drug Info IC50 = 2.72 nM Click to Show More [1]
2 D0B6DN Drug Info IC50 = 13.8 nM [1]
3 D01EVT Drug Info N.A. [1]
Patent ID WO2007110337
Title Pyridine and Pyrimidine Derivatives As Mglur2 Antagonists.
Abstract The present invention relates to compounds of formula (I), a process for the manufacture thereof, their use for the preparation of medicaments for treating CNS disorders and pharmaceutical compositions containing them: wherein A, B, X, Y, R1, R2, R3 and R4 are as defined in the description and claims.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0IY8T Drug Info Ki = 0.7 nM Click to Show More [1]
2 D0I6LO Drug Info Ki = 1.7 nM [1]
3 D0H2LD Drug Info Ki = 3 nM [1]
4 D06NZY Drug Info Ki = 5 nM [1]
5 D0Y5DN Drug Info Ki = 7 nM [1]
6 D08PHH Drug Info Ki = 9 nM [1]
7 D0KZ6Q Drug Info Ki = 28 nM [1]
8 D0RX0M Drug Info Ki = 28 nM [1]
9 D0N1CC Drug Info Ki = 32 nM [1]
10 D0IL4Z Drug Info Ki = 74 nM [1]
11 D05CBS Drug Info Ki = 140 nM [1]
Patent ID WO2013111796
Title N-Substituted Pyrazole Derivative.
Applicant(s) Taisho Pharmaceutical Co., Ltd
Representative Drug(s) D0V0BC Drug Info IC50 = 1.39 nM Click to Show More [1]
2 D0WP5S Drug Info IC50 = 4.66 nM [1]
3 D08JPW Drug Info N.A. [1]
Patent ID WO2014059111
Title Method for Increasing The oral Bioavailability of A Metabotropic Glutamate 2/3 Receptor Antagonist.
Abstract A method of increasing the oral bioavailability of an mGluR 2/3 antagonist by administration of an oral dosage form with food is provided, as well as an article of manufacture comprising an oral dosage form of the mGluR 2/3 antagonist in a suitable container and associated with printed labeling which describes the increased oral bioavailability of the medication in the container when taken with food.
Applicant(s) Braincells, Inc
Representative Drug(s) D0P7DA Drug Info Ki > 1000 nM [1]
Patent ID WO2013062680
Title Novel Compounds and Compositions Thereof for Treating Nervous System Disorders.
Abstract The present invention relates to a novel compound, methods of synthesizing the compound, compositions containing the compound, and methods for using the compound or composition to treat and/or prevent diseases and/or conditions of the central and peripheral nervous system.
Applicant(s) Braincells, Inc
Representative Drug(s) D0P7DA Drug Info Ki > 1000 nM [1]
Patent ID WO2015004007
Title Ethynyl Derivatives As Metabotropic Glutamate Receptor Antagonists.
Abstract The present invention relates to ethynyl derivatives of formula (I) wherein Y is N or CH; R1 is hydrogen, fluoro or chloro; and R2 is hydrogen or lower alkyl; or to a pharmaceutically acceptable acid addition salt 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 syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
Applicant(s) F. Hoffmann-La Roche Ag
Patent ID WO2012052451
Title Metabotropic Glutamate Receptor Modulators.
Abstract The invention relates to heterocyclic derivatives of formula (I) as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are mGluR5 modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorders wherein Y, W, R1, R2 and R3 are as defined in claim 1.
Applicant(s) Merz Pharma Gmbh & Co Kgaa
References  Top
REF 1 Novel metabotropic glutamate receptor 2/3 antagonists and their therapeutic applications: a patent review (2005 - present).Expert Opin Ther Pat. 2015 Jan;25(1):69-90.
REF 2 mGlu5 negative allosteric modulators: a patent review (2013 - 2016).Expert Opin Ther Pat. 2017 Jun;27(6):691-706.

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