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 T60182 Target Info
Target Name Glucagon receptor (GCGR)
Synonyms GLR; GL-R
Target Type Successful Target
Gene Name GCGR
Biochemical Class GPCR secretin
UniProt ID
GLR_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2012162409
Title Biphenyl Derivatives Useful As Glucagon Receptor Antagonists.
Abstract The present invention is directed to biphenyl derivatives of Formula (I), pharmaceutical compositions containing them and their use in the treatment and / or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity. (I).
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D06HMY Drug Info Ki = 42 nM Click to Show More [1]
2 D00QJA Drug Info Ki = 70 nM [1]
3 D0FS8K Drug Info Ki = 4850 nM [1]
4 D0SA6K Drug Info N.A. [1]
Patent ID WO2012162407
Title Picolinamido - Propanoic Acid Derivatives Useful As Glucagon Receptor Antagonists.
Abstract The present invention is directed to picolanmido-propanoic acid derivatives, pharmaceutical compositions containing them and their use in the treatment and / or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D04ELA Drug Info Ki = 3.7 nM Click to Show More [1]
2 D0IT9C Drug Info Ki = 17.2 nM [1]
3 D0HV7T Drug Info Ki = 20 nM [1]
4 D0SA6K Drug Info N.A. [1]
Patent ID WO2012085745
Title Glucagon Receptor Modulators.
Abstract The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
Applicant(s) Pfizer Inc
Representative Drug(s) D00NCJ Drug Info Kb = 54 nM Click to Show More [1]
2 D0IL0U Drug Info Kb = 67 nM [1]
3 D07CLY Drug Info Kb = 130 nM [1]
4 D01TGE Drug Info Kb = 1500 nM [1]
5 D0TR5T Drug Info N.A. [1]
Patent ID WO2011119559
Title Novel Spiro Imidazolones As Glucagon Receptor Antagonists, Compositions, and Methods for Their Use.
Abstract The present invention relates to compounds of the general formula: wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D05AWM Drug Info IC50 = 22 nM Click to Show More [1]
2 D0AJ3F Drug Info IC50 = 61 nM [1]
3 D07AMZ Drug Info N.A. [1]
Patent ID WO2011037815
Title Novel Pyrrolidines As Glucagon Receptor Antagonists, Compositions, and Methods for Their Use.
Abstract The present invention relates to compounds of the general formula: (I) wherein ring B, R1, R2, R3, Z, and L1 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
Applicant(s) Schering Corp
Representative Drug(s) D09IGN Drug Info IC50 < 3000 nM Click to Show More [1]
2 D0JY2I Drug Info IC50 < 3000 nM [1]
3 D03KUD Drug Info N.A. [1]
Patent ID WO2011007722
Title 3-Substituted-2-Furancarboxylic Acid Hydrazide Derivative and Pharmaceutically Acceptable Salt Thereof.
Abstract Disclosed are a compound represented by formula (I) and a pharmaceutically acceptable salt thereof. (In the formula, ring A represents a phenylene or the like; R1 represents an optionally substituted C6-10 aryl group or the like; R2 and R3 may be the same or different and each represents a hydrogen atom or a C1-4 alkyl group; R4 represents a hydrogen atom, a halogen atom or the like; R5 and R6 may be the same or different and each represents a hydrogen atom, a halogen atom or the like; X represents an NR7 group or the like; R7 represents a hydrogen atom or the like; R8 represents a cyano group or a nitro group; and n represents 1 or the like.).
Applicant(s) Dainippon Sumitomo Pharma Co
Representative Drug(s) D0YP5U Drug Info IC50 = 1.1 nM Click to Show More [1]
2 D0HS9X Drug Info N.A. [1]
Patent ID WO2013014569
Title Quinolinyl Glucagon Receptor Modulators.
Abstract The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
Applicant(s) Pfizer Inc
Representative Drug(s) D05EON Drug Info Kb = 23 nM Click to Show More [1]
2 D01EWH Drug Info N.A. [1]
Patent ID WO2011119541
Title Novel Spiro Imidazolone Derivatives As Glucagon Receptor Antagonists, Compositions, and Methods for Their Use.
Abstract The present invention relates to compounds of the general formula (I): wherein ring A, ring B, G, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0F9RK Drug Info IC50 = 209 nM Click to Show More [1]
2 D04NUS Drug Info IC50 = 290 nM [1]
3 D0DE4E Drug Info N.A. [1]
4 D0O0DJ Drug Info N.A. [1]
Patent ID WO2013147026
Title Aromatic Ring Compound.
Abstract To provide an aromatic ring compound which has glucagon antagonist activity and is useful for the prophylaxis or treatment of diabetes and the like. A compound represented by formula (I) (wherein the symbols are as defined in the description) or a salt thereof has excellent glucagon antagonist activity and is useful as a glucagon antagonist, a sugar production inhibitor or a prophylactic/therapeutic agent for diabetes and the like.
Applicant(s) Takeda Pharmaceutical Co., Ltd
Representative Drug(s) D07ZDJ Drug Info N.A. Click to Show More [1]
2 D0FA5D Drug Info N.A. [1]
3 D0XT3V Drug Info N.A. [1]
4 D0Y5DU Drug Info N.A. [1]
Patent ID WO2011027849
Title Heterocyclic Compound.
Abstract Disclosed is a prophylactic or therapeutic agent for diabetes, which has excellent pharmacological efficacy. Specifically disclosed is 3-{[(6-{[cyclohexyl(5-fluoro-1-methyl-1H-indol- 2-yl)methyl]amino.
Applicant(s) Takeda Pharmaceutical Company Limited
Patent ID WO2010131669
Title 3-(4-Aminophenyl)-2-Furancarboxylic Acid Derivative and Pharmaceutically Acceptable Salt Thereof.
Applicant(s) Dainippon Sumitomo Pharma Co Ltd
Representative Drug(s) D0HS9X Drug Info N.A. [1]
United States Patent and Trademark Office (USPTO)
Patent ID US20120202834
Title Preparation of 3-[4-(Heterocyclyl-Substituted)-Benzamido]Propanoic Acids As Glucagon Receptor Modulators.
Representative Drug(s) D0FW5U Drug Info Kb = 84.1 nM Click to Show More [1]
2 D0UA4Y Drug Info Kb = 164 nM [1]
3 D0JA0A Drug Info Kb = 1420 nM [1]
Patent ID US8809342
Title Glucagon Receptor Modulators.
Representative Drug(s) D00NCJ Drug Info Kb = 54 nM Click to Show More [1]
2 D0IL0U Drug Info Kb = 67 nM [1]
3 D07CLY Drug Info Kb = 130 nM [1]
4 D01TGE Drug Info Kb = 1500 nM [1]
5 D0TR5T Drug Info N.A. [1]
Patent ID US8748624
Title Picolinamido-Propanoic Acid Derivatives Useful As Glucagon Receptor Antagonists.
Representative Drug(s) D04ELA Drug Info Ki = 3.7 nM Click to Show More [1]
2 D0IT9C Drug Info Ki = 17.2 nM [1]
3 D0HV7T Drug Info Ki = 20 nM [1]
4 D0SA6K Drug Info N.A. [1]
Patent ID US8735604
Title Pyrrolidines As Glucagon Receptor Antagonists, Compositions, and Methods for Their Use.
Representative Drug(s) D09IGN Drug Info IC50 < 3000 nM Click to Show More [1]
2 D0JY2I Drug Info IC50 < 3000 nM [1]
3 D03KUD Drug Info N.A. [1]
Patent ID US8507533
Title Glucagon Receptor Modulators.
Representative Drug(s) D0UA4Y Drug Info Kb = 164 nM [1]
References  Top
REF 1 Small molecule glucagon receptor antagonists: a patent review (2011 - 2014).Expert Opin Ther Pat. 2015 Jul;25(7):819-30.

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