Invention Grant
- Patent Title: Tetrahydroisoquinolines as PRMT5 inhibitors
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Application No.: US16081745Application Date: 2017-03-09
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Publication No.: US10550096B2Publication Date: 2020-02-04
- Inventor: Alexandra Elizabeth Stupple , Scott Raymond Walker , Paul Anthony Stupple
- Applicant: CTXT PTY LTD
- Applicant Address: AU Victoria
- Assignee: CTXT PTY LTD
- Current Assignee: CTXT PTY LTD
- Current Assignee Address: AU Victoria
- Agency: Stites & Harbison PLLC
- Agent Richard S. Meyers, Jr.
- Priority: GB1604022.2 20160309
- International Application: PCT/EP2017/055531 WO 20170309
- International Announcement: WO2017/153515 WO 20170914
- Main IPC: C07D401/06
- IPC: C07D401/06 ; C07D498/08 ; C07D401/14 ; C07D413/14 ; C07D491/048 ; A61P35/00

Abstract:
A compound of formula (I) wherein: n is 1 or 2; p is 0 or 1; R1a, R1b, R1c and R1d are independently selected from H, halo, methyl and methoxy; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2e is H or Me; R3a and R3b are independently selected from H and Me; R4 is either H or Me; R6a and R6b are independently selected from H and Me; X is either N or CH; R7 is selected from H and C1-4 alkyl; (a) one of R8a, R8b, R8c, and R8d is selected from H, halo, C1-4 alkyl, C1-4 alkoxy, NHC1-4 alkyl; (b) another of R8a, R8b, R8c and R8d is selected from H, C1-4 alkyl, C1-4 fluoroalkyl, C3-6 cycloalkyl, C5-6 heteroaryl, C5-6 heteroaryl methyl, C4-6 heterocyclyl, C4-6 heterocyclyl methyl, phenyl, benzyl, halo, amido, amidomethyl, acylamido, acylamidomethyl, C1-4 alkyl ester, C1-4 alkyl ester methyl, C1-4 alkyl carbamoyl, C1-4 alkyl carbamoyl methyl, C1-4 alkylacyl, C1-4 alkylacyl methyl, phenylcarbonyl, carboxy, carboxymethyl, ether, amino, amino methyl, sulfonamido, sulfonamino, sulfone, sulfoxide, nitrile and nitrilemethyl; (c) the others of R8a, R8b, R8c and R8d are H.
Public/Granted literature
- US20190062304A1 TETRAHYDROISOQUINOLINES AS PRMT5 INHIBITORS Public/Granted day:2019-02-28
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