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 T32060 Target Info
Target Name 5-HT 2A receptor (HTR2A)
Synonyms Serotonin receptor 2A; HTR2; 5-hydroxytryptamine receptor 2A; 5-HT-2A; 5-HT-2
Target Type Successful Target
Gene Name HTR2A
Biochemical Class GPCR rhodopsin
UniProt ID
5HT2A_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2014180165
Title Benzoisothiazole Compounds and Use In Preparation of Antipsychotic Drugs.
Abstract Disclosed are benzoisothiazole compounds and a use in the preparation of anti-schizophrenia drugs. The benzoisothiazole compounds of the present invention not only have strong affinity for dopamine D3 receptor, 5-HT1A receptor and 5-HT2A receptor, but also can observably improve the symptoms of schizophrenia relevant to apomorphine model and MK-801 model mice, with oral absorption being good, safety being high and side-effect being less, and having developmental value as new anti-neurotic disease drugs. The present invention is the compounds having a structure of general formula (I), or geometric isomers, free alkalies, salts, hydrates or solvates thereof.
Applicant(s) Shanghai Inst Pharm Industry
Representative Drug(s) D0Z9WY Drug Info Ki = 0.058 nM Click to Show More [1]
2 D0M1UF Drug Info Ki = 0.23 nM [1]
Patent ID WO2009019174
Title Benzoyl-Piperidine Derivatives As Dual Modulators of The 5-Ht2A and D3 Receptors.
Abstract The present invention relates to compounds of the general Formula (I) wherein R1 and A are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use as medicaments. Compounds of general Formula (I) have high affinity for the dopamine D3 and serotonin (5-Hydroxytryptamine; 5-HT) 5-HT2A receptors and are effective in the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D06RIO Drug Info Ki = 4.88 nM Click to Show More [2]
2 D02GTU Drug Info Ki = 6 nM [2]
3 D0J7SD Drug Info Ki = 8.65 nM [2]
4 D0FR1P Drug Info Ki = 34 nM [2]
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 = 0.55 nM Click to Show More [2]
2 D0B7NS Drug Info Ki = 4 nM [2]
3 D0P9VX Drug Info Ki = 4 nM [2]
4 D0U9UH Drug Info Ki = 11 nM [2]
5 D08DJY Drug Info Ki = 12.5 nM [2]
6 D0N2VA Drug Info Ki = 25 nM [2]
7 D0SE9K Drug Info Ki = 25 nM [2]
Patent ID WO2008042388
Title Pyrazole Derivatives As Modulators of The 5-Ht2A Serotonin Receptor Useful for The Treatment of Disorders Related Thereto.
Abstract Pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the serotonin 5HT2A receptor. Formula (Ia). Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic- related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.
Applicant(s) Arena Pharmaceuticals, Inc
Representative Drug(s) D03IAB Drug Info N.A. Click to Show More [2]
2 D0DW6V Drug Info N.A. [2]
Patent ID WO2005012254
Title Diaryl and Arylheteroaryl Urea Derivatives As Modulators of The 5-Ht2A Serotonin Receptor Useful for The Prophylaxis and Treatment of Disorders Related Therto.
Abstract The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders and the like. The present invention also relates to the method of prophylaxis or treatment of 5-HT2A serotonin receptor mediated disorders in combination with a dopamine D2 receptor antagonist such as haloperidol, administered separately or together.
Applicant(s) Arena Pharmaceuticals, Inc
Representative Drug(s) D0JT3F Drug Info N.A. Click to Show More [2]
2 D0ZF0Z Drug Info N.A. [2]
Patent ID WO2012175531
Title Method of Administration of 4-((1R,3S)-6-Chloro-3-Phenyl-Indan-1-Yl)-1,2,2-Trimethyl-Piperazine and The Salts Thereof In The Treatment of Schizophrenia.
Abstract The present invention relates to 4-((1 R,3S)-6-chloro-3-phenyl-indan-1 -yl)-1,2,2-trimethyl- piperazine and the salts thereof with activity at dopamine D1 and D2 receptors as well as the serotonin 5HT2 receptor for the treatment of diseases in the central nervous system in a once weekly dosing regime.
Applicant(s) H. Lundbeck A / S
Representative Drug(s) D0J4AZ Drug Info Ki = 4.2 nM [2]
Patent ID WO2010062323
Title Compositions of A 5-Ht2A Serotonin Receptor Modulator Useful for The Treatment of Disorders Related Thereto.
Abstract The present invention relates to certain compositions of a 5-HT2A serotonin receptor modulator and methods for their preparation. The compositions disclosed herein are useful for increasing slow wave sleep, improving sleep consolidation, improving sleep maintenance and improving sleep quality, and for treating insomnia and related sleep disorders, dyssomnias, parasomnias and nonrestorative sleep and the like. The compositions disclosed herein are further useful for treating platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders and progressive multifocal leukoencephalopathy and the like.
Applicant(s) Arena Pharmaceuticals, Inc
Representative Drug(s) D0H8IH Drug Info N.A. [2]
Patent ID WO2006100519
Title Arylsulfonyl Benzofused Heterocycles As 5-Ht2A Antagonists.
Abstract Compounds of formula (I): are potent and selective antagonists of the 5-HT2A receptor, and hence are useful in treatment of various CNS disorders.
Applicant(s) Merck Sharp & Dohme Limited
Patent ID WO2006097766
Title Arylsulfonyl Benzyl Ethers As 5-Ht2A Antagonists.
Abstract Compounds of formula (I) are potent and selective antagonists of the 5-HT2A receptor, and hence are useful in treatment of various CNS disorders.
Applicant(s) Merck Sharp & Dohme Limited
Patent ID WO2001029008
Title Pyrazole Derivatives Which Modulate Human Serotonin Receptors.
Abstract Disclosed herein are non-endogenous, constitutively activated forms of the human 5-HT2A and human 5-HT2C receptors and uses of such receptors to screen candidate compounds. Further disclosed herein are candidate compounds identified by the screening method which act at the 5HT2A receptors. Yet further disclosed is a new class of compounds (I) which act at the 5HT2A receptors. This new class encompasses the candidate compounds. In Formula (A) W is F, Cl, Br, I, C1-8 straight chain or branched alkyl, C3-8 cycloalkyl, C4-9 alkylcycloalkyl, or C2-8 alkenyl; X is O or S or NR2; Y is NR3R4, or (CH)mR5, or O(CH)nR6; m is an integer between 0 and 4, inclusive; n is an integer between 0 and 4, inclusive; Z is H, C-8 straight chain or branched alkyl, C3-8 cycloalkyl, C4-9 alkylcycloalkyl, or C2-8 alkenyl; R1, R2, R3 and R10are as defined in the application.
Applicant(s) Arena Pharmaceuticals, 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 = 0.55 nM Click to Show More [2]
2 D0B7NS Drug Info Ki = 4 nM [2]
3 D0P9VX Drug Info Ki = 4 nM [2]
4 D0U9UH Drug Info Ki = 11 nM [2]
5 D08DJY Drug Info Ki = 12.5 nM [2]
6 D0N2VA Drug Info Ki = 25 nM [2]
7 D0SE9K Drug Info Ki = 25 nM [2]
Patent ID US7858630
Title Serotonin 5-Ht2A and Dopamine D3 Receptors ModuLators, Useful In The Treatment of Cognitive Disorders, Drug Addiction, Depression, Anxiety, Dementia and Psychological Disorders.
Applicant(s) Hoffmann-La Roche Inc
Representative Drug(s) D06RIO Drug Info Ki = 4.88 nM Click to Show More [2]
2 D02GTU Drug Info Ki = 6 nM [2]
3 D0J7SD Drug Info Ki = 8.65 nM [2]
4 D0FR1P Drug Info Ki = 34 nM [2]
Patent ID US20090186895
Title Ethers, Secondary Amines and Derivatives Thereof As Modulators of The 5-Ht2A Serotonin Receptor Useful for The Treatment of Disorders Related Thereto.
Applicant(s) Arena Pharmaceuticals, Inc
Representative Drug(s) D0H5XC Drug Info IC50(DOI binding assay) = 0.025 nM Click to Show More [2]
2 D0AQ1T Drug Info IC50(DOI binding assay) = 0.082 nM [2]
3 D0N8PF Drug Info IC50(DOI binding assay) = 0.26 nM [2]
4 D0KM0T Drug Info IC50(DOI binding assay) = 0.51 nM [2]
5 D0R6HF Drug Info IC50(DOI binding assay) = 1 nM [2]
6 D00PLP Drug Info IC50(DOI binding assay) = 1.2 nM [2]
7 D09WFK Drug Info IC50(DOI binding assay) = 4.4 nM [2]
Patent ID US20060229335
Title Diarylamine and Arylheteroarylamine Pyrazole Derivatives As Modulators of 5Ht2A.
Applicant(s) Arena Pharmaceuticals, Inc
Representative Drug(s) D0O3BR Drug Info IC50(IP accumulation assay) = 1.77 nM Click to Show More [2]
2 D0WC8M Drug Info IC50(IP accumulation assay) = 2.99 nM [2]
3 D0OR4G Drug Info IC50(IP accumulation assay) = 7 nM [2]
Patent ID US20160096811
Title Benzoisothiazole Compounds and Use In Preparation of Antipsychotic Drugs.
Representative Drug(s) D0Z9WY Drug Info Ki = 0.058 nM Click to Show More [1]
2 D0M1UF Drug Info Ki = 0.23 nM [1]
Patent ID US8785441
Title 3-Phenyl-Pyrazole Derivatives As Modulators of The 5-Ht2A Serotonin Receptor Useful for The Treatment of Disorders Related Thereto.
Applicant(s) Arena Pharmaceuticals, Inc
Representative Drug(s) D0HY3K Drug Info N.A. [2]
Patent ID US8148417
Title Primary Amines and Derivatives Thereof As Modulators of The 5-Ht2A Serotonin Receptor Useful for The Treatment of Disorders Related Thereto.
Applicant(s) Arena Pharmaceuticals, Inc
Patent ID US7884101
Title 3-Phenyl-Pyrazole Derivatives As Modulators of The 5-Ht2A Serotonin Receptor Useful for The Treatment of Disorders Related Thereto.
Applicant(s) Arena Pharmaceuticals, Inc
European Patent Office (EPO)
Patent ID EP0638073
Title 1-Piperazino-1,2-Dihydroindene Derivatives.
Applicant(s) H. Lundbeck A / S
Representative Drug(s) D0J4AZ Drug Info Ki = 4.2 nM [2]
References  Top
REF 1 5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689.
REF 2 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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