公开(公告)号：US10421743B2

公开(公告)日：2019-09-24

申请号：US16081696

申请日：2017-03-09

申请人： CTXT PTY LTD

发明人： Ylva Elisabet Bergman ,  Michelle Ang Camerino ,  Scott Raymond Walker ,  Paul Anthony Stupple

IPC分类号： C07D217/16 ,  A61K31/472 ,  C07D401/14 ,  C07D405/14 ,  C07D401/12 ,  C07D413/12 ,  C07D471/04 ,  C07D498/08 ,  C07D217/24 ,  C07D491/08 ,  A61P35/00

摘要： 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 the group consisting of H, halo, C1-4 alkoxy, C1-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, NH—C1-4 alkyl and cyano; 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; R5 is either H or Me; R6a and R6b are independently selected from H and Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl; wherein when R2e is H, at least one of R1a, R1b, R1c and R1d is selected from C1-4 alkoxy, C2-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, NH—C1-4 alkyl and cyano.

公开(公告)号：US20190071425A1

公开(公告)日：2019-03-07

申请号：US16081696

申请日：2017-03-09

申请人： CTXT PTY LTD

发明人： Ylva Elisabet Bergman ,  Michelle Ang Camerino ,  Scott Raymond Walker ,  Paul Anthony Stupple

IPC分类号： C07D401/14 ,  C07D401/12 ,  C07D491/08 ,  C07D413/12 ,  C07D471/04 ,  C07D217/24 ,  C07D405/14

CPC分类号： C07D401/14 ,  A61P35/00 ,  C07D217/16 ,  C07D217/24 ,  C07D401/12 ,  C07D405/14 ,  C07D413/12 ,  C07D471/04 ,  C07D491/08 ,  C07D498/08

摘要： 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 the group consisting of H, halo, C1-4 alkoxy, C1-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, NH—C1-4 alkyl and cyano; 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; R5 is either H or Me; R6a and R6b are independently selected from H and Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl; wherein when R2e is H, at least one of R1a, R1b, R1c and R1d is selected from C1-4 alkoxy, C2-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, NH—C1-4 alkyl and cyano.

公开(公告)号：US10787434B2

公开(公告)日：2020-09-29

申请号：US16082196

申请日：2017-03-09

申请人： CTXT PTY LTD

发明人： Ylva Elisabet Bergman ,  Michelle Ang Camerino ,  Paul Anthony Stupple

IPC分类号： C07D401/14 ,  C07D413/14

摘要： A compound of formula I: (I) wherein: n is 1 or 2; p is 0 or 1; R1a, R1b, R1c and R1d are independently selected from H, halo, C1-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, C1-4 alkyloxy, NH—C1-4 alkyl and cyano; 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; R5 is either H or Me; R6a and R6b are independently selected from H and Me; A is either (IIa), where R7a is selected from N-linked N-containing C5-7 heterocycyl and (A); or (ii) (IIb), where X is selected from CH2, NH and O, one of R8a and R8b is selected from CI and ethoxy and the other of R8a and R8b is H.

公开(公告)号：US20200010451A1

公开(公告)日：2020-01-09

申请号：US16082196

申请日：2017-03-09

申请人： CTXT PTY LTD

发明人： Ylva Elisabet Bergman ,  Michelle Ang Camerino ,  Paul Anthony Stupple

IPC分类号： C07D401/14 ,  C07D413/14

摘要： A compound of formula I: (I) wherein: n is 1 or 2; p is 0 or 1; R1a, R1b, R1c and R1d are independently selected from H, halo, C1-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, C1-4 alkyloxy, NH—C1-4 alkyl and cyano; 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; R5 is either H or Me; R6a and R6b are independently selected from H and Me; A is either (IIa), where R7a is selected from N-linked N-containing C5-7 heterocycyl and (A); or (ii) (IIb), where X is selected from CH2, NH and O, one of R8a and R8b is selected from CI and ethoxy and the other of R8a and R8b is H.

公开(公告)号：US10005792B2

公开(公告)日：2018-06-26

申请号：US15508074

申请日：2015-09-03

申请人： CTXT PTY LTD

发明人： Ylva Elisabet Bergman ,  Romina Lessene ,  Danny Ganame ,  Richard Charles Foitzik ,  Benjamin Joseph Morrow ,  Michelle Ang Camerino ,  Scott Raymond Walker ,  H. Rachel Lagiakos ,  John Feutrill ,  Paul Anthony Stupple

IPC分类号： C07D207/12 ,  C07D209/44 ,  C07D211/22 ,  C07D211/46 ,  C07D211/58 ,  C07D211/76 ,  C07D213/81 ,  C07D213/82 ,  C07D217/06 ,  C07D217/12 ,  C07D231/14 ,  C07D231/20 ,  C07D231/56 ,  C07D235/08 ,  C07D271/08 ,  C07D271/10 ,  C07D261/18 ,  C07D277/56 ,  C07D277/68 ,  C07D265/30 ,  C07D265/34 ,  C07D401/04 ,  C07D401/12 ,  C07D413/04 ,  C07D451/02 ,  C07D451/14 ,  C07D491/08 ,  C07D491/107 ,  C07C233/78 ,  C07C235/42 ,  C07C235/60 ,  C07D295/192

CPC分类号： C07D491/107 ,  C07C233/78 ,  C07C235/42 ,  C07C235/50 ,  C07C235/60 ,  C07C311/08 ,  C07C2602/06 ,  C07C2602/08 ,  C07C2602/10 ,  C07D205/04 ,  C07D207/12 ,  C07D209/44 ,  C07D211/22 ,  C07D211/46 ,  C07D211/58 ,  C07D211/76 ,  C07D213/81 ,  C07D213/82 ,  C07D217/06 ,  C07D231/12 ,  C07D231/14 ,  C07D231/20 ,  C07D231/56 ,  C07D235/08 ,  C07D261/18 ,  C07D265/30 ,  C07D265/34 ,  C07D271/08 ,  C07D271/10 ,  C07D277/56 ,  C07D277/68 ,  C07D295/185 ,  C07D295/192 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/04 ,  C07D451/02 ,  C07D451/14 ,  C07D491/08

摘要： A compound of formula (1a), (1b) or (1c) wherein: n is 1 or 2; RN is H or Me; R1 is optionally one or more halo or methyl groups; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d (if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R3a and R3b are independently selected from H and Me; R4a is selected from OH, —NH2, —C(═O)NH2, and —CH2OH; R4b is either H or Me; R5 is either H or Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl.

公开(公告)号：US20170313713A1

公开(公告)日：2017-11-02

申请号：US15508074

申请日：2015-09-03

申请人： CTXT PTY LTD

发明人： Ylva Elisabet Bergman ,  Romina Lessene ,  Danny Ganame ,  Richard Charles Foitzik ,  Benjamin Joseph Morrow ,  Michelle Ang Camerino ,  Scott Raymond Walker ,  H. Rachel Lagiakos ,  John Feutrill ,  Paul Anthony Stupple

IPC分类号： C07D491/107 ,  C07C233/78 ,  C07D451/02 ,  C07D413/04 ,  C07D401/12 ,  C07D401/04 ,  C07D295/192 ,  C07D277/68 ,  C07D277/56 ,  C07D271/10 ,  C07D271/08 ,  C07D265/34 ,  C07D265/30 ,  C07D261/18 ,  C07D235/08 ,  C07D231/56 ,  C07D231/20 ,  C07D231/14 ,  C07D217/06 ,  C07D213/82 ,  C07D213/81 ,  C07D211/76 ,  C07D211/58 ,  C07D211/46 ,  C07D211/22 ,  C07D209/44 ,  C07D207/12 ,  C07C235/60 ,  C07C235/42 ,  C07D451/14 ,  C07D491/08

CPC分类号： C07D491/107 ,  C07C233/78 ,  C07C235/42 ,  C07C235/50 ,  C07C235/60 ,  C07C311/08 ,  C07C2602/06 ,  C07C2602/08 ,  C07C2602/10 ,  C07D205/04 ,  C07D207/12 ,  C07D209/44 ,  C07D211/22 ,  C07D211/46 ,  C07D211/58 ,  C07D211/76 ,  C07D213/81 ,  C07D213/82 ,  C07D217/06 ,  C07D231/12 ,  C07D231/14 ,  C07D231/20 ,  C07D231/56 ,  C07D235/08 ,  C07D261/18 ,  C07D265/30 ,  C07D265/34 ,  C07D271/08 ,  C07D271/10 ,  C07D277/56 ,  C07D277/68 ,  C07D295/185 ,  C07D295/192 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/04 ,  C07D451/02 ,  C07D451/14 ,  C07D491/08

摘要： A compound of formula (1a), (1b) or (1c) wherein: n is 1 or 2; RN is H or Me; R1 is optionally one or more halo or methyl groups; R1 and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d (if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R3a and R3b are independently selected from H and Me; R4a is selected from OH, —NH2, —C(═O)NH2, and —CH2OH; R4b is either H or Me; R5 is either H or Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl.

公开(公告)号：US20170298075A1

公开(公告)日：2017-10-19

申请号：US15508053

申请日：2015-09-03

申请人： CTXT PTY LTD

发明人： Ylva Elisabet Bergman ,  Richard Charles Foitzik ,  Benjamin Joseph Morrow ,  Michelle Ang Camerino ,  Scott Raymond Walker ,  H. Rachel Lagiakos ,  John Feutrill ,  Graeme Irvine Stevenson ,  Paul Anthony Stupple

IPC分类号： C07D491/08 ,  C07D487/08 ,  C07D471/04 ,  C07D417/12 ,  C07D409/12 ,  C07D217/16 ,  C07D405/14 ,  C07D405/12 ,  C07D401/14 ,  C07D401/12 ,  C07D491/048 ,  C07D413/12

CPC分类号： C07D491/08 ,  C07D217/00 ,  C07D217/16 ,  C07D231/12 ,  C07D239/42 ,  C07D271/10 ,  C07D295/18 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/08 ,  C07D491/048

摘要： A compound of formula I wherein: n is 1 or 2: p is 0 or 1; R1 is optionally one or more halo or methyl groups; 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; R3a and R3b are independently selected from H and Me; R4 is either H or Me; R5 is either H or Me; R6a and R6b are independently selected from H and Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl.