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 T20958 Target Info
Target Name Neuropeptide S receptor (NPSR)
Synonyms PGR14; Gprotein coupled receptor for asthma susceptibility; Gprotein coupled receptor PGR14; Gprotein coupled receptor 154; GPRA; GPR154; G-protein coupled receptor for asthma susceptibility; G-protein coupled receptor PGR14; G-protein coupled receptor 154
Target Type Patented-recorded Target
Gene Name NPSR1
Biochemical Class GPCR rhodopsin
UniProt ID
NPSR1_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2013086200
Title Composition and Method for Neuropeptide S Receptor (Npsr) Antagonists.
Abstract Neuropeptide S receptor antagonists are provided that bind in functional assays to neuropeptide S receptors; methods are provided for use of these antagonists in treatment of conditions or disease states that are ameliorated by blocking of the neuropeptide S receptor, including substance abuse and substance abuse relapse; and for use of neuropeptide S receptor antagonists in the manufacture of therapeutics and pro-drugs for therapeutics useful in disease states and conditions sensitive to binding of the neuropeptide S receptor.
Applicant(s) Research Triangle Institute
Representative Drug(s) D0K1ZY Drug Info pA2 = 5.8 Click to Show More [1]
2 D09JFR Drug Info pA2 = 6.2 [1]
3 D06TFC Drug Info pA2 = 7.5 [1]
4 D02BPJ Drug Info N.A. [1]
Patent ID WO2013068785
Title Indanone and Indandione Derivatives and Heterocyclic Analogs.
Abstract The invention relates to indanone/indandione derivatives and heterocyclic analogs of Formula (I) wherein Ar1, A, B, L1, Y, Z, and (R1)n n are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as NPS receptor antagonists.
Applicant(s) Actelion Pharmaceuticals Ltd
Representative Drug(s) D0M3DM Drug Info pIC50 = 7.6 Click to Show More [1]
2 D0O4ML Drug Info pIC50 = 8.2 [1]
3 D09DZI Drug Info pIC50 = 8.5 [1]
4 D0Y9XS Drug Info N.A. [1]
Patent ID WO2011137220
Title Small Molecule Neuropeptide S Antagonists for The Treatment of Addictive Disorders, Mood, Anxiety and Sleep Disorders.
Abstract Disclosed are compounds of General Formula I: wherein R1, R2, R3, X and Y are described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for neuropsychiatric disorders including pain, sleep, mood, anxiety, eating and addictive disorders, are also provided.
Applicant(s) The United States of America, As Represented By the Secretary, Department of Health and Human Services
Representative Drug(s) D0K7OV Drug Info pIC50 = 7 to 7.1 Click to Show More [1]
2 D06FUK Drug Info pIC50 = 8.3 to 8.5 [1]
3 D00ODC Drug Info N.A. [1]
Patent ID WO2010056567
Title Imidazoisoindole Neuropeptide S Receptor Antagonists.
Abstract The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. 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 neuropeptide S receptor is involved.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0YU5R Drug Info pIC50 = 6.4 Click to Show More [1]
2 D09AVU Drug Info pIC50 = 7.1 [1]
3 D0H1LQ Drug Info pA2 = 7.9; pKB = 8.5 [1]
4 D00IVM Drug Info N.A. [1]
Patent ID WO2010056564
Title Quinolone Neuropeptide S Receptor Antagonists.
Abstract The present invention is directed to quinolone compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. 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 neuropeptide S receptor is involved.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0WI0P Drug Info pIC50 = 7.3; pKB = 9.6 Click to Show More [1]
2 D0AT0A Drug Info pIC50 = 7.7 [1]
3 D0I8ZE Drug Info pIC50 = 8.2 [1]
4 D0X8JD Drug Info N.A. [1]
Patent ID WO2005021555
Title Bicyclic Piperazine Compound and Use Thereof.
Abstract A compound represented by the formula (I) (wherein R<sup>1</sup> represents acyl; R<sup>2</sup> represents an optionally substituted hydrocarbon group, etc.; R<sup>3</sup> represents an optionally sub.
Applicant(s) Takeda Pharmaceutical Company Limited
Representative Drug(s) D00JCQ Drug Info pA2 = 6.3 Click to Show More [1]
2 D0QY3L Drug Info pA2 = 6.5 [1]
3 D0S3TL Drug Info pA2 = 7.1 [1]
4 D06FJL Drug Info pA2/pKB (hNPSRAsn) = 7.3 to 8.2 [1]
5 D0QN7I Drug Info pA2 = 7.3 [1]
6 D0I0BN Drug Info pA2 = 7.5 [1]
7 D0S1AT Drug Info N.A. [1]
Patent ID WO2012131109
Title Peptides and Pharmaceutical Compositions for Use In The Treatment By Nasal Administration of Patients Suffering From Anxiety and Sleep Disorders.
Abstract The present invention provides peptides for use in a medicament which is administered nasally, wherein the peptide is an agonist of neuropeptide S receptor (NPSR), of the receptor TGR23 and/or of vasopressin receptor-related receptor 1 (VRR1) or for use in the treatment of a patient by causing, promoting or increasing relieve or healing of phobic anxiety, avoidance anxiety, dissociative anxiety such as flashbacks, depersonalisation, derealisation, intrusions, vegetative symptoms related to anxiety symptoms, especially in panic attacks, in posttraumatic stress disorder, in generalised anxiety disorder and in anxiety accompanying depressive, or psychotic episodes, arousal, awakening, alertness, activity, spontaneous movement, an anxiolytic effect or a combination thereof in the patient, wherein the peptide is administered nasally or for use in the prophylaxis and/or treatment of an anxiety or sleep disorder, especially in any type of hypersomnia like idiopathic hypersomnia, wherein the peptide is administered nasally. Further provided are pharmaceutical compositions for nasal administration comprising at least one of said peptides, uses of said peptide or said pharmaceutical composition. The invention also provides a method for identifying target neurons of a peptide in an animal, wherein the peptide is administered nasally.
Applicant(s) Boyce Thompson Institute for Plant Research Inc
References  Top
REF 1 Neuropeptide S receptor ligands: a patent review (2005-2016).Expert Opin Ther Pat. 2017 Mar;27(3):347-362.

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