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 T73482 Target Info
Target Name Orexin receptor type 1 (HCRTR1)
Synonyms Ox1r; Ox1-R; Ox-1-R; Orexin-1 receptor; Hypocretin receptor type 1; HFGAN72 receptor; 7-transmembrane G-protein coupledneuropeptide receptor
Target Type Clinical trial Target
Gene Name HCRTR1
Biochemical Class GPCR rhodopsin
UniProt ID
OX1R_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2015124934
Title Substituted Cyclopentanes, Tetrahydrofuranes and Pyrrolidines As orexin Receptor Antagonists.
Abstract The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, Formula (I) wherein L,X, Ra, Rb, R 1, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
Applicant(s) Takeda Cambridge Limited Takeda Pharmaceutical Company Limited
Representative Drug(s) D0CG0D Drug Info IC50 = 8.6 nM Click to Show More [1]
2 D0EG3N Drug Info IC50 = 21 nM [1]
Patent ID WO2015124932
Title 1,2-Substituted Cyclopentanes As orexin Receptor Antagonists.
Abstract The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, (I) wherein L,X, Ra, Rb, R1, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
Applicant(s) Takeda Cambridge Limited Takeda Pharmaceutical Company Limited
Representative Drug(s) D0S4UG Drug Info IC50 = 6 nM Click to Show More [1]
2 D06OTA Drug Info IC50 = 7 nM [1]
3 D09XLY Drug Info IC50 = 8 nM [1]
4 D0U9WX Drug Info IC50 = 8 nM [1]
Patent ID WO2015055994
Title Cyclopentylbenzamide Derivatives and Their Use for The Treatment of Psychotic and Cognitive Disorders.
Abstract The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein n, L, X, Ra, Rb, R1, R2 and R3 their preparation, pharmaceutical compositions containing them and their use in therapy.
Applicant(s) Takeda Cambridge Limited Takeda Pharmaceutical Company Limited
Representative Drug(s) D0WX1B Drug Info IC50 = 0.84 nM Click to Show More [1]
2 D06NRQ Drug Info IC50 = 1 nM [1]
3 D0L0YA Drug Info IC50 = 1 nM [1]
4 D0VE3H Drug Info IC50 = 1 nM [1]
5 D01NWU Drug Info IC50 = 4.2 nM [1]
6 D0U7VC Drug Info IC50 = 4.7 nM [1]
7 D0NX4W Drug Info IC50 = 6.7 nM [1]
8 D02LWJ Drug Info IC50 = 8.3 nM [1]
9 D0VR1K Drug Info IC50 = 12 nM [1]
10 D0YI3Z Drug Info IC50 = 12 nM [1]
11 D0AL3I Drug Info IC50 = 14 nM [1]
12 D0P8AX Drug Info IC50 = 14 nM [1]
13 D0C6GE Drug Info IC50 = 16 nM [1]
14 D00VEM Drug Info IC50 = 18 nM [1]
15 D08KYM Drug Info IC50 = 21 nM [1]
16 D04JLF Drug Info IC50 = 23 nM [1]
17 D0J4YW Drug Info IC50 = 27 nM [1]
18 D03JAZ Drug Info IC50 = 35 nM [1]
19 D0ZC1O Drug Info IC50 = 35 nM [1]
20 D05QWJ Drug Info IC50 = 36 nM [1]
21 D08ZRN Drug Info IC50 = 41 nM [1]
22 D05WDQ Drug Info IC50 = 64 nM [1]
23 D04DCO Drug Info IC50 = 65 nM [1]
24 D02CCF Drug Info IC50 = 150 nM [1]
25 D0FI1W Drug Info IC50 = 220 nM [1]
26 D0DO4J Drug Info IC50 = 340 nM [1]
27 D05PMY Drug Info IC50 = 780 nM [1]
References  Top
REF 1 Substituted cyclopentanes, tetrahydrofurans and pyrrolidines as orexin-1-receptor antagonists for treatment of various CNS disorders (WO2015/055994; WO2015/124932; WO2015/124934).Expert Opin Ther Pat. 2016;26(3):409-15.

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