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 T09572 Target Info
Target Name Melanin-concentrating hormone receptor 1 (MCHR1)
Synonyms Somatostatinreceptor-like protein; Somatostatin receptor-like protein; SLC1; SLC-1; Melanin-concentrating hormone receptor subtype 1; MCHR-1; MCHR; MCH1R; MCH-R1; MCH-1R; MCH(1) receptor; MCH receptor1; MCH receptor 1; GPR24; G-protein coupled receptor 24; G protein coupled receptor 24
Target Type Clinical trial Target
Gene Name MCHR1
Biochemical Class GPCR rhodopsin
UniProt ID
MCHR1_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2013168759
Title Aromatic Ring Compound.
Abstract The present invention provides an aromatic ring compound that has melanin-concentrating hormone receptor antagonism, and is useful as an agent for preventing or treating obesity and the like. The present invention pertains to a compound represented by formula (I), or a salt thereof. (Each symbol in the formula is synonymous with that of the specification.).
Applicant(s) Takeda Pharmaceutical Co., Ltd
Representative Drug(s) D0DB8G Drug Info 97% inhibition = 100 nM Click to Show More [1]
2 D0M8KC Drug Info 97% inhibition = 100 nM [1]
3 D0MT7T Drug Info 100% inhibition = 100 nM [1]
Patent ID WO2013105676
Title Benzimidazole Derivatives As Mch Receptor Antagonists.
Abstract The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula (I) wherein each symbol as defined in the specification, or a salt thereof.
Applicant(s) Takeda Pharmaceutical Company Limited
Representative Drug(s) D03KWP Drug Info 100% inhibition = 100 nM Click to Show More [1]
2 D0Q1NA Drug Info 95% inhibition = 100 nM [1]
Patent ID WO2011037771
Title Diarylmethylamide Derivative Having Melanin-Concentrating Hormone Receptor Antagonism.
Abstract The present invention is directed to diarylmethylamide derivatives represented of structural formula I which are melanin-concentrating hormone receptor antagonists, and are useful as an agent for the prevention, treatment, or remedy of various circulatory diseases, neurological diseases, metabolic diseases, reproductive system diseases, respiratory diseases, digestive diseases, and the like. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the melanin-concentrating hormone is involved. I.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D01SYN Drug Info IC50 = 2.5 nM Click to Show More [1]
2 D02MTQ Drug Info IC50 = 2.6 nM [1]
Patent ID WO2011003012
Title Azinone-Substituted Azapolycycle Mch-1 Antagonists, Methods of Making, and Use Thereof.
Abstract Novel MCH-I receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
Applicant(s) Albany Molecular Research, Inc
Representative Drug(s) D0R0YB Drug Info 72% inhibition = 1000 nM; Ki = 5.3 nM Click to Show More [1]
2 D08JMZ Drug Info Ki = 7.4 nM [1]
3 D0L2EQ Drug Info 68% inhibition = 1000 nM; Ki = 17 nM [1]
Patent ID WO2011003007
Title Azabicycloalkane-Indole and Azabicycloalkane-Pyrrolo-Pyridine Mch-1 Antagonists, Methods of Making, and Use Thereof.
Abstract Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
Applicant(s) Albany Molecular Research, Inc
Representative Drug(s) D0R0YB Drug Info 72% inhibition = 1000 nM; Ki = 5.3 nM Click to Show More [1]
2 D08JMZ Drug Info Ki = 7.4 nM [1]
3 D0L2EQ Drug Info 68% inhibition = 1000 nM; Ki = 17 nM [1]
Patent ID WO2011003005
Title Azinone-Substituted Azepino[B]Indole and Pyrido-Pyrrolo-Azepine Mch-1 Antagonists, Methods of Making, and Use Thereof.
Abstract Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
Applicant(s) Albany Molecular Research, Inc
Representative Drug(s) D04NIU Drug Info Ki = 10 nM Click to Show More [1]
2 D0CC6Q Drug Info Ki = 10 nM [1]
3 D0I9BT Drug Info Ki = 10 nM [1]
Patent ID WO2011083804
Title Indole Derivative.
Applicant(s) Takeda Pharmaceutical Company Limited
Representative Drug(s) D0A2NT Drug Info 98% inhibition = 100 nM Click to Show More [1]
2 D0TK2N Drug Info 97% inhibition = 100 nM [1]
Patent ID WO201236233
Title Condensed Heterocyclic Derivative Having Melanine-Concentrating Hormone Receptor Antagonistic Activity.
Abstract Provided is a novel compound which has MCH R1 receptor antagonistic activity and is represented by formula (I), a pharmaceutically acceptable salt thereof, or a solvate of the same. (In the formula, the portion AA represented by formula (1) is BB etc., the broken lines indicate whether or not a bond is present, X1 is O or S, when the broken lines joined to X2 indicate that a bond is not present, X2 is N or C(R3), X4-X3-X2 is X4-O-C(R4)(R4)-C(R4)(R4)-X2 etc., -Y1- is a single bond etc., -Y2- is a single bond etc., each R2 is independently a halogen etc., R3 is hydrogen etc., R4 is hydrogen etc., D is an alkyl etc., ring B is a cycloalkyl etc., p is an integer of 0 to 4, and q is an integer of 1 to 4.
Applicant(s) Shionogi & Co., Ltd
Representative Drug(s) D0I6YT Drug Info IC50 = 2 nM Click to Show More [1]
2 D0TK3S Drug Info N.A. [1]
Patent ID WO2014039412
Title Pyrrolone or Pyrrolidinone Melanin Concentrating Hormone Receptor-1 Antagonists.
Abstract The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are melanin concentrating hormone receptor-1 (MCHR1) antagonists which may be used as medicaments.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D0CV5F Drug Info N.A. Click to Show More [1]
2 D0JY4C Drug Info N.A. [1]
Patent ID WO2014039411
Title Pyrrolone or Pyrrolidinone Melanin Concentrating Hormore Receptor-1 Antagonists.
Abstract The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are melanin concentrating hormone receptor-1 (MCHR1) antagonists which may be used as medicaments.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D0L3ZZ Drug Info N.A. Click to Show More [1]
2 D0M9JM Drug Info N.A. [1]
Patent ID WO2013131935
Title Pyridinone and Pyridazinone Derivatives As Mch - Receptor Modulators.
Abstract The present invention relates to compounds of general formula I, wherein the groups R1, R2, L1, L2, U and B are as defined in the application, which have valuable pharmacological properties, and in particular modulate the activity of the MCH receptor.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D0HH1O Drug Info IC50 = 17 nM [1]
Patent ID WO2013011285
Title Azetidine Derivatives for Treatment of Melanin Related Disorders.
Abstract Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin- concentrating hormone related disease or condition.
Applicant(s) Astrazeneca Ab
Representative Drug(s) D0FQ4W Drug Info IC50 = 15 nM [1]
Patent ID WO2012153154
Title Oxetane Substituted Thieno Pyrimidinones.
Abstract The present invention provides a compound of Formula (I) or pharmaceutically acceptable salt thereof wherein is selected from the group consisting of unsubstituted aryl and heteroaryl groups and aryl and heteroaryl groups substituted with Q; Q represents fluoro, chloro, bromo, C1-6 straight or branched alkyl, alkylthio, cyano, trihaloalkyl, trihaloalkoxy; Y represents CH or N; R is selected from a group consisting of hydrogen, C1-6 straight or branched alkyl, C1-6 alkoxy, trihaloalkyl, trihaloalkoxy, amino, alkylamino, dialkylamino, hydroxy cyano, acetyl, alkylthio and halo; k is independently an integer 2 or 3; n is an integer from 0 to 2 and m is an integer from 1 to 4 provided that sum of the integers m and n is equal to an integer from 2 to 4. The invention also relates to pharmaceutical compositions containing them, to processes for their preparation, new intermediate compounds thereof and to their use in the treatment and/or prophylaxis of a melanin concentrating hormone receptor 1 and optionally H3 receptor related disease or condition.
Applicant(s) Richter Gedeon Nyrt
Representative Drug(s) D0GH0Z Drug Info IC50 = 5.6 nM [1]
Patent ID WO2012004588
Title Therapeutic Agents 976.
Abstract Disclosed herein are azetidinyl compounds of formula (I), as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.
Applicant(s) Astrazeneca Ab
Representative Drug(s) D03TCR Drug Info IC50 = 10 nM [1]
Patent ID WO2011130086
Title Pyridone Derivatives.
Abstract The present invention is directed to novel phenylpyridone derivative compounds. The compounds act as a melanin concentrating hormone receptor antagonists, and can be useful in preventing, treating or acting as a remedial agent for various circular system diseases, nervous system diseases, metabolic diseases, genital diseases, respiratory diseases and digestive diseases.
Applicant(s) Merck Sharp &Amp
Representative Drug(s) D0S6DD Drug Info IC50 = 11 nM [1]
Patent ID WO2011127643
Title Pyridone Derivatives.
Abstract The present invention discloses phenylpyridone derivative compounds. The compounds act as a melanin concentrating hormone receptor antagonists, and can be used in preventing, treating or acting as a remedial agent for various circular system diseases, nervous system diseases, metabolic diseases, genital diseases, respiratory diseases and digestive diseases.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0J6MM Drug Info IC50 = 11 nM [1]
Patent ID WO2011003021
Title Azinone-Substituted Azabicycloalkane-Indole and Azabicycloalkane-Pyrrolo-Pyridine Mch-1 Antagonists, Methods of Making, and Use Thereof.
Abstract Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
Applicant(s) Albany Molecular Research, Inc
Representative Drug(s) D07MJJ Drug Info Ki = 6.4 nM [1]
Patent ID WO2010141545
Title Bis-Pyridylpyridones As Melanin-Concentrating Hormone Receptor 1 Antagonists.
Abstract The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1 ), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes.
Applicant(s) Glaxosmithkline Llc
Representative Drug(s) D0GN5K Drug Info IC50 = 49 nM [1]
Patent ID WO2010141539
Title Bis-Pyridylpyridones As Melanin-Concentrating Hormone Receptor 1 Antagonists.
Abstract The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1 ), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes.
Applicant(s) Chengde Xiao, et al
Representative Drug(s) D0DN8Z Drug Info IC50 = 25 nM [1]
Patent ID WO2010141538
Title Bis-Pyridylpyridones As Melanin-Concentrating Hormone Receptor 1 Antagonists.
Abstract The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1 ), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes.
Applicant(s) Gang Yuan
Representative Drug(s) D0Y0RS Drug Info IC50 = 48 nM [1]
Patent ID WO2010125390
Title Therapeutic Agents 713.
Abstract Disclosed herein are compounds of Formula (I) in which R1, R2, R3, R4, R5, A, X, Y are as described in the specification, their use in pharmaceutical compositions and in methods of treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.
Applicant(s) Astrazeneca Ab
Representative Drug(s) D03JJW Drug Info IC50 = 10 nM [1]
Patent ID WO2010038901
Title 7-Piperidinoalkyl-3,4-Dihydroquinolone Derivative.
Abstract To provide a novel compound, a pharmaceutically acceptable salt or a hydrate thereof useful for preventing or treating for depression, anxiety disorders (such as generalized anxiety disorder, posttraumatic stress disorder, panic disorder, obsessive-compulsive disorder or social anxiety disorder), attention deficit disorder, mania, manic-depressive illness, schizophrenia, mood disorders, stress, sleep disorders, attacks, memory impairment, cognitive impairment, dementia, amnesia, delirium, obesity, eating disorder, appetite disorder, hyperphagia, bulimia, cibophobia, diabetes, cardiovascular diseases, hypertension, dyslipidemia, myocardial infarction, movement disorder (such as Parkinson's disease, epilepsy, convulsion or tremor), drug abuse, drug addiction or sexual dysfunction, based on a melanin-concentrating hormone receptor (MCH receptor) antagonistic action. SOLUTION A compound, a pharmaceutically acceptable salt or a hydrate thereof represented by the formula (I).
Applicant(s) Taisho Pharmaceutical Co., Ltd
Representative Drug(s) D09CER Drug Info IC50 = 6.2 nM [1]
Patent ID WO2013166621
Title 1-(Dihydronaphthalenyl)Pyridones As Melanin-Concentrating Hormone Receptor 1 Antagonists.
Abstract This invention relates to novel 1-(dihydronaphthalenyl)pyridones which are antagonists of the melanin-concentrating hormone receptor 1 (MCHR1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of obesity and diabetes.
Applicant(s) Glaxosmithkline Llc
Representative Drug(s) D0RX2U Drug Info N.A. [1]
Patent ID WO2013149362
Title 1-(Dihydronaphthalenyl)Pyridones As Melanin-Concentrating Hormone Receptor 1 Antagonists.
Abstract Provided are 1-(dihydronaphthalenyl)pyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy for the treatment of obesity and diabetes.
Applicant(s) Glaxosmithkline Llc
Representative Drug(s) D0T6UX Drug Info N.A. [1]
Patent ID WO2010141540
Title Bis-Pyridylpyridones As Melanin-Concentrating Hormone Receptor 1 Antagonists.
Abstract The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1 ), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes.
Applicant(s) Glaxosmithkline Llc
Representative Drug(s) D0TY8S Drug Info N.A. [1]
United States Patent and Trademark Office (USPTO)
Patent ID US2012157460
Title Preparation of Tetrahydro-Azacarboline Mch-1 Antagonists.
Representative Drug(s) D08JKR Drug Info Ki = 7.1 nM [1]
Patent ID US20120157469
Title Preparation of Piperazinone-Substituted Tetrahydro-Carboline Mch-1 Antagonists.
Representative Drug(s) D0KF0X Drug Info Ki = 5.8 nM [1]
Patent ID US20110034375
Title New Substituted Benzene Compounds Are Melanin Concentrating Hormone Receptor-1 Modulators, Useful To Treat E.G. Obesity, Diabetes, Depression, Anxiety, Sleep Disorders and Psychiatric Disorders Such As Schizophrenia and Substance Abuse.
Representative Drug(s) D0N8CI Drug Info IC50 = 4 nM [1]
Patent ID US20110003759
Title New Substituted 1H-Pyrazin-2-One Compounds Are Melanin-Concentrating Hormone Receptor 1 Antagonists Useful To Treat E.G. Obesity, Diabetes, Arteriosclerosis, Hypertension, Polycystic Ovary Disease, Cardiovascular Disease, Osteoarthritis.
Representative Drug(s) D0N8CI Drug Info IC50 = 4 nM [1]
Japan Patent Office (JPO)
Patent ID JP2011219467
Title Preparation of 7-Piperidinoalkyl-3,4- Dihydroquinolone Compounds As Mch (Melanin Concentrating Hormone) Receptor Antagonists.
Representative Drug(s) D09CER Drug Info IC50 = 6.2 nM [1]
Korean Intellectual Property Office (KIPO)
Patent ID KR2012038039
Title 5,6-Dihydropyrrolo[3,4-B]Pyridin-7-One Derivative As Mch Receptor-1 Antagonist and Method for The Preparation Thereof.
Representative Drug(s) D00RUE Drug Info IC50 = 20 nM Click to Show More [1]
2 D0V8FC Drug Info IC50 = 30 nM [1]
Patent ID KR2013042847
Title Preparation of Phthalazinone Derivative As Mch Receptor-1 Antagonist and Preparation Method Thereof.
Representative Drug(s) D01RQE Drug Info IC50 = 5 nM [1]
Patent ID KR2013042846
Title Preparation of Naphtho[1,2-B]Furan-2-Carboxamide Derivative As Mch Receptor-1 Antagonist and Preparation Method Thereof.
Representative Drug(s) D09UGQ Drug Info IC50 = 3 nM [1]
Patent ID KR2012103243
Title Preparation of Pyrrolopyridinone Derivatives As Mch Receptor-1 Antagonists.
Representative Drug(s) D0C5RD Drug Info IC50 = 50 nM [1]
Patent ID KR2012103220
Title Preparation of Benzofuran-2-Carboxamide Derivatives As Mch Receptor-1 Antagonists.
Representative Drug(s) D0S2ED Drug Info IC50 = 10 nM [1]
Patent ID KR2012037720
Title Phthalazinone Derivative Containing 5-Membered Heteroaryl Moiety As Mch Receptor Antagonist and Method for The Preparation Thereof.
Representative Drug(s) D0BQ7K Drug Info IC50 = 10 nM [1]
Patent ID KR2012017856
Title 1,2,4- Oxadiazole Derivative As Mch Receptor Antagonist and Method for The Preparation Thereof.
Representative Drug(s) D0KJ9U Drug Info IC50 = 100 nM [1]
Patent ID KR20120034829
Title Phthalazinone Derivative Containing Aryl-Piperidine Moiety As Mch (Melanin-Concentrating Hormone) Receptor Antagonist and Method for The Preparation.
Representative Drug(s) D0V3OD Drug Info IC50 = 1 nM [1]
Patent ID KR2011094573
Title Preparation of 2-Substituted 6-(Biphenyl-4-Carboxamido) Quinoxaline Derivatives As Mch1R Inhibitors.
Representative Drug(s) D0TZ6J Drug Info IC50 = 50 nM [1]
Patent ID KR2011094566
Title Preparation of 1-(6,7-Difluoro-3-Methoxyquinoxalin-2- Yl)-3-[1- (Heteroarylmethyl)Piperidin-4- Yl]Urea Derivatives As Mch1R Inhibitors.
Representative Drug(s) D00HQJ Drug Info IC50 = 9 nM [1]
References  Top
REF 1 Novel MCH1 receptor antagonists: a patent review.Expert Opin Ther Pat. 2015 Feb;25(2):193-207.

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