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 T83813 Target Info
Target Name 5-HT 2C receptor (HTR2C)
Synonyms Serotonin receptor 2C; HTR1C; 5HT-1C; 5-hydroxytryptamine receptor 2C; 5-hydroxytryptamine receptor 1C; 5-HTR2C; 5-HT2C receptor; 5-HT2C; 5-HT1C; 5-HT-2C; 5-HT-1C
Target Type Successful Target
Gene Name HTR2C
Biochemical Class GPCR rhodopsin
UniProt ID
5HT2C_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2007019083
Title Pyrimidine Compounds As Serotonin Receptor Modulators.
Abstract Certain pyrimidine-containing compounds are serotonin receptor modulators useful in the treatment of serotonin-mediated diseases.
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D00YGY Drug Info Ki = 20 nM Click to Show More [1]
2 D0P9VX Drug Info Ki = 70 nM [1]
3 D0B7NS Drug Info Ki = 90 nM [1]
4 D0N2VA Drug Info Ki = 900 nM [1]
5 D0SE9K Drug Info Ki = 1170 nM [1]
6 D08DJY Drug Info Ki = 1000 nM [1]
Patent ID WO2003086306
Title 5Ht2C Receptor Modulators.
Abstract The present invention relates to novel compounds of: (Formula I); which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.
Applicant(s) Arena Pharmaceuticals, Inc
Representative Drug(s) D0L4UC Drug Info IC50(IP accumulation assay) = 1.4 nM Click to Show More [1]
2 D03IZY Drug Info IC50(IP accumulation assay) = 2.1 nM [1]
3 D0A5FR Drug Info IC50(IP accumulation assay) = 4.2 nM [1]
4 D0T5ER Drug Info IC50(IP accumulation assay) = 4.5 nM [1]
5 D0BU6K Drug Info EC50 = 5 nM [1]
6 D0I3QY Drug Info IC50(IP accumulation assay) = 6.3 nM [1]
7 D0GW5F Drug Info IC50(IP accumulation assay) = 12.1 nM [1]
8 D0HV0D Drug Info N.A. [1]
9 D0OA6W Drug Info N.A. [1]
Patent ID WO2007081299
Title Tricyclic Indeno-Pyrrole Derivatives As Serotonin Receptor Modulators.
Abstract The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).
Applicant(s) Athersys, Inc
Representative Drug(s) D0AA9F Drug Info N.A. Click to Show More [1]
2 D0AV8R Drug Info N.A. [1]
3 D0SO0F Drug Info N.A. [1]
Patent ID WO2006028961
Title Tricyclic Heteroaryl Piperazines, Pyrrolidines and Azetidines As Serotonin Receptor Modulators.
Abstract The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are hexahydroazepinoindole and octahydroazepinoindole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).
Applicant(s) Athersys, Inc
Representative Drug(s) D0AA9F Drug Info N.A. Click to Show More [1]
2 D0AV8R Drug Info N.A. [1]
3 D0SO0F Drug Info N.A. [1]
Patent ID WO2006004931
Title Substituted Azepine Derivatives As Serotonin Receptor Modulators.
Abstract The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are hexahydroazepinoindole and octahydroazepinoindole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).
Applicant(s) Athersys, Inc
Representative Drug(s) D00DFK Drug Info N.A. Click to Show More [1]
2 D00YRD Drug Info N.A. [1]
3 D06VJM Drug Info N.A. [1]
4 D07KZR Drug Info N.A. [1]
5 D09EPG Drug Info N.A. [1]
6 D0AI8S Drug Info N.A. [1]
7 D0AJ0O Drug Info N.A. [1]
8 D0BD3M Drug Info N.A. [1]
9 D0FK0Y Drug Info N.A. [1]
10 D0FS3J Drug Info N.A. [1]
11 D0KO2E Drug Info N.A. [1]
12 D0MQ7F Drug Info N.A. [1]
13 D0R6EF Drug Info N.A. [1]
Patent ID WO2002040456
Title Piperazinylpyrazine Compounds As Agonist or Antagonist of Serotonin 5Ht-2 Receptor.
Abstract A compound of the general formula (I), wherein R1, R2, X, Y and Z are as described in the specification.
Applicant(s) Biovitrum Ab
Representative Drug(s) D00DFK Drug Info N.A. Click to Show More [1]
2 D00YRD Drug Info N.A. [1]
3 D06VJM Drug Info N.A. [1]
4 D07KZR Drug Info N.A. [1]
5 D09EPG Drug Info N.A. [1]
6 D0AI8S Drug Info N.A. [1]
7 D0AJ0O Drug Info N.A. [1]
8 D0BD3M Drug Info N.A. [1]
9 D0FK0Y Drug Info N.A. [1]
10 D0FS3J Drug Info N.A. [1]
11 D0KO2E Drug Info N.A. [1]
12 D0MQ7F Drug Info N.A. [1]
13 D0R6EF Drug Info N.A. [1]
Patent ID WO2008113360
Title 4- [2- (4-Methylphenylsulfanyd-Phenyl] Piperidine with Combined Serotonin and Norepinephrine Reuptake Inhibition for The Treatment of Adhd, Melancholia, Treatment Resistent Depression or Residual Symptoms In Depression.
Abstract The use of 4-[2-(4-methylphenylsulfayl)phenyl]peridine and acid additions salts thereof for the treatment of ADHD, melancholia, treatment resistant depression or residual.symptoms in depression is provided.
Applicant(s) H. Lundbeck A/S
Representative Drug(s) D06YCW Drug Info N.A. [1]
Patent ID WO2006116165
Title Chromane and Chromene Derivatives and Uses Thereof.
Abstract Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R2, R3, R4, y, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
Applicant(s) HEFFERNAN, Gavin, David et al
Patent ID WO2003091250
Title [1,4]Diazepino[6,7,1-Ij]Quinoline Derivatives As Anti Psychotic and Antiobesity Agents.
Abstract Compounds of formula 1 or a pharmaceutically acceptable salt thereof are provided: I where R1 through R7 are defined herein. The compounds of formula I are 5HT2c agonists or partial agonists, and are useful for treating a variety of disorders.
Applicant(s) RAMAMOORTHY, Sivaramakrishnan, P et al
Representative Drug(s) D01LVT Drug Info N.A. [1]
Patent ID WO2009063993
Title Fused Pyridine Derivative and Use Thereof.
Abstract Disclosed is a serotonin 5-HT2c receptor activator containing a compound represented by the formula (I) below or a salt thereof. (In the formula, the symbols are as defined in the description.).
Applicant(s) Takeda Pharmaceutical
Patent ID WO2009063992
Title Condensed Pyridine Derivative and Use Thereof.
Abstract Provided are a condensed pyridine derivative having an action of activating a serotonin 5HT2c receptor, a preventive or therapeutic agent for a disease such as lower urinary tract symptom, obesity and.
Applicant(s) Takeda Pharmaceutical Company Limited
Patent ID WO2009063991
Title Pyridooxazepine Derivative and Use Thereof.
Abstract Disclosed is a compound represented by the formula below, which has excellent serotonin 5-HT2C receptor activating activity. Specifically disclosed is a compound represented by the formula below or a salt thereof. (In the formula, A represents -OR1 or -S(O)pR2; R1 and R2 each represent a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group; and p represents 0, 1 or 2.).
Applicant(s) Takeda Pharmaceutical Co., Ltd
Patent ID WO2008117169
Title Pyrimido [4, 5-D] Azepine Derivatives As 5-Ht2C Agonists.
Abstract The present invention relates to compounds of formula (I): wherein R1, R2, R3a, R3b, R3c, R3d and R100 are as defined in the specification. These compounds act as 5-HT2C agonists.
Applicant(s) Pfizer Limited
Patent ID WO2008108445
Title Benzoxazepine Derivatives and Use Thereof.
Abstract Compounds represented by the general formula (I) wherein each symbol is as defined in the description [with the proviso that 9-chloro-7-(1,1-dimethylethyl)-2,3,4,5-tetrahydro-1,4-benz-oxazepine and N-.
Applicant(s) Takeda Pharmaceutical Company Limited
Patent ID WO2008052078
Title Benzoxathiine and Benzoxathiole Derivatives and Uses Thereof.
Abstract Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided, wherein each of R1, R2, R3, R4, y, n, m, p, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
Applicant(s) STACK, Gary, Paul et al
Patent ID WO2007028082
Title 6-Substituted- 2,3,4,5-Tetrahydro-1H-Benzo[D]Azepines As 5-Ht2C Receptor Agonists.
Abstract The present invention provides 6-substituted 2,3,4,5-tetrahydro-lH- benzo[d]azepines of Formula (I) as selective 5-HT2C receptor agonists for the treatment of 5-HT2c associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: R6 D R N-R' R* where R6 is -(CrC3)alkyl-S-(C0-C3)alkyl-R10, -(C1-C3)alkyl-NR11R12, -(CrC3)alkyl-O- R 13. and other substituents are as defined in the specification.
Applicant(s) Eli Lilly and Company
Patent ID WO2006116158
Title Benzodioxane and Benzodioxolane Derivatives and Uses Thereof.
Abstract Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided, wherein each of R1, R2, R3, R4, y, n, m, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
Applicant(s) ZHOU, Dahui et al
Patent ID WO2006116150
Title Dihydrobenzofuran Derivatives and Uses Thereof.
Abstract Compounds of formula (I) are described herein which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. Formula (I), or pharmaceutically acceptable salts thereof, wherein each of R1, R2, R3, R4, Rx, Ry, and n are as defined herein. Such compounds, and compositions thereof, are useful for treating a variety of central nervous system disorders such as schizophrenia.
Applicant(s) STACK, Gary Paul et al
Patent ID WO2006050007
Title Substituted Indolizines and Derivatives As Cns Agents.
Abstract Compounds of formula (I) of pharmaceutically acceptable salts thereof are provided: formula (I), which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
Applicant(s) SABB, Annmarie, Louise et al
Patent ID WO2005082859
Title 6-Substituted 2,3,4,5-Tetrahydro-1H-Benzo[D]Azepines As 5-Ht2C Receptor Agonists.
Abstract The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT2C receptor agonists for the treatment of 5-HT2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: I where: R6 is -C=C-R10, -O-R12, -S-R14, or -NR24R25; and other substituents are as defined in the specification.
Applicant(s) Eli Lilly and Company
Patent ID WO2005044812
Title Dihydrobenzofuranyl Alkanamine Derivatives As 5Ht2C Agonists.
Abstract Compounds of Formula (I) or pharmaceutically acceptable salts thereof are provided: Formula (I) which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
Applicant(s) GROSS, Jonathan, Laird et al
Patent ID WO2005040146
Title Dihydrobenzofuranyl Alkanamines and Pharmaceutical Compositions Containing Them.
Abstract Compounds of formula (1) or pharmaceutically acceptable salts thereof are provided : Formula (1) which are agonists and partial agonists of the 2c subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
Applicant(s) GROSS, Jonathan, Laird et al
Patent ID WO2005019180
Title 6-(2,2,2-Trifluoroethylamino)-7-Chloro-2,3,4,5-Tetrahydro-1H-Benzo[D]Azepine As A 5-Ht2C Receptor Agonist.
Abstract The present invention provides a 7-chloro-6-(2,2,2-trifluoroethylamino)-2,3,4,5-tetrahydro-1H-benzo[d]azepine of formula (I): or a pharmaceutically acceptable salt thereof, and its use as a selective 5-HT2c agonist for the treatment of 5-HT2c associated disorders including obesity, obsessive/compulsive disorder, anxiety, and depression.
Applicant(s) Eli Lilly and Company
Patent ID WO2008052096
Title Benzodioxane Derivatives and Uses Thereof.
Applicant(s) FITZWATER, Kelly, R et al
Patent ID WO2008007664
Title Bicyclic Heterocyclic Compound and Use Thereof.
Applicant(s) Takeda Pharmaceutical Company Limited
Patent ID WO2008007661
Title Tricyclic Heterocyclic Compound and Use Thereof.
Applicant(s) Takeda Pharmaceutical Company Limited
Patent ID WO2007132841
Title Fused Heterocyclic Compound and Use Thereof.
Applicant(s) Takeda Pharmaceutical Company Limited
Patent ID WO2006103511
Title 5-Ht2C Receptor Modulators.
Applicant(s) Pfizer Products, Inc
United States Patent and Trademark Office (USPTO)
Patent ID US8618288
Title Pyrimidine Compounds As Serotonin Receptor Modulators.
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D00YGY Drug Info Ki = 20 nM Click to Show More [1]
2 D0P9VX Drug Info Ki = 70 nM [1]
3 D0B7NS Drug Info Ki = 90 nM [1]
4 D0N2VA Drug Info Ki = 900 nM [1]
5 D0SE9K Drug Info Ki = 1170 nM [1]
6 D08DJY Drug Info Ki = 1000 nM [1]
Patent ID US7863442
Title Processes for The Synthesis of Olanzapine.
Applicant(s) Apotex Pharmachem Inc
Representative Drug(s) D01PAP Drug Info N.A. [1]
Patent ID US7425627
Title Methods of Synthesizing Olanzapine.
Applicant(s) Teva Pharmaceutical Industries Ltd
Representative Drug(s) D01PAP Drug Info N.A. [1]
Patent ID US7329747
Title Synthesis of Olanzapine and Intermediates Thereof.
Applicant(s) Synthon Ip Inc
Representative Drug(s) D01PAP Drug Info N.A. [1]
Patent ID US7022698
Title Pharmaceutical Compositions Containing New Polymorphic forms of Olanzapine and Uses Thereo.
Applicant(s) U & I Pharmaceuticals, Ltd
Representative Drug(s) D01PAP Drug Info N.A. [1]
Patent ID US6740753
Title Crystal Olanzapine with A Melting Point of 187-191 Degrees C.
Applicant(s) Geneva Pharmaceuticals, Inc
Representative Drug(s) D01PAP Drug Info N.A. [1]
Patent ID US6506746
Title Such As AlzheimerS Disease, By Administering Olanzapine or Salt Thereof.
Applicant(s) Eli Lilly and Company
Representative Drug(s) D01PAP Drug Info N.A. [1]
Patent ID US6147072
Title Administering Antidepressant and Serotonin Reuptake Inhibitor.
Applicant(s) Eli Lilly and Company
Representative Drug(s) D01PAP Drug Info N.A. [1]
Patent ID US5627178
Title Treating Central Nervous System Disorders.
Applicant(s) Lilly Industries Limited
Representative Drug(s) D01PAP Drug Info N.A. [1]
Patent ID US20110319395
Title Pharmaceutical formulation of Olanzapine.
Applicant(s) Krka, Tovarna Zdravil, Dd
Representative Drug(s) D01PAP Drug Info N.A. [1]
Patent ID US20120058185
Title Stable Pharmaceutical Compositions of Olanzapine and Process for Their Preparation.
Representative Drug(s) D01PAP Drug Info N.A. [1]
References  Top
REF 1 Novel serotonin receptor 2 (5-HT2R) agonists and antagonists: a patent review (2004-2014).Expert Opin Ther Pat. 2016;26(1):89-106.

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