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1. 发明申请

WO2019043139A1 FUSED [1,2,4]THIADIAZINE DERIVATIVES WHICH ACT AS KAT INHIBITORS OF THE MYST FAMILY 审中-公开
公开(公告)号：WO2019043139A1
公开(公告)日：2019-03-07
申请号：PCT/EP2018/073431
申请日：2018-08-31
申请人： CTXT PTY LIMITED
发明人： MORROW, Benjamin Joseph , FOITZIK, Richard Charles , CAMERINO, Michelle Ang , LAGIAKOS, Helen Rachel , WALKER, Scott Raymond , BOZIKIS, Ylva Elisabet Bergman , STEVENSON, Graeme Irvine , CUZZUPE, Anthony Nicholas , STUPPLE, Paul Anthony
IPC分类号： C07D417/12 , C07D417/14 , C07D513/04 , C07D285/24 , A61P35/00 , A61K31/549 , A61K31/542
摘要： A compound of formula (I): which inhibits the activity of one or more KATs of the MYST family, i.e., TIP60, KAT6B, MOZ, HBO1 and MOF.

2. 发明申请

WO2017153520A1 BENZOPIPERIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER AND HEMOGLOBINOPATHIES 审中-公开
标题翻译：苯并哌啶衍生物及其在治疗癌症和血红蛋白病中的用途
公开(公告)号：WO2017153520A1
公开(公告)日：2017-09-14
申请号：PCT/EP2017/055537
申请日：2017-03-09
申请人： CTXT PTY LIMITED
发明人： BERGMAN, Ylva Elisabet , CAMERINO, Michelle Ang , STUPPLE, Paul Anthony
IPC分类号： A61P35/00 , A61P7/06 , C07D401/12 , A61K31/444 , A61K31/451 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/553
摘要： A compound of formula I: (I) wherein: n is 1 or 2; p is 0 or 1; R 1a , R 1b , R 1c and R 1d are independently selected from H, halo, C 1-4 alkyl, C 1-4 fluoroalkyl, C 3-4 cycloalkyl, C 1-4 alkyloxy, NH-C 1-4 alkyl and cyano; R 2a and R 2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH 2 OH; R 2c and R 2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH 2 OH; R 2e is H or Me; R 3a and R 3b are independently selected from H and Me; R 4 is either H or Me; R 5 is either H or Me; R 6a and R 6b are independently selected from H and Me; A is either (IIa), where R 7a is selected from N-linked N-containing C 5-7 heterocycyl and (A); or (ii) (IIb), where X is selected from CH 2 , N H and O, one of R 8a and R 8b is selected from CI and ethoxy and the other of R 8a and R 8b is H.
摘要翻译：式I化合物：（I）其中：n是1或2; p是0或1; R 1a，R 1b，R 1c和R 1d独立地选自H，卤素，C _{> 1-4烷基，C 1-4氟代烷基，C 3-4环烷基，C 1-4烷氧基，NH -C 1-4烷基和氰基; R 2a和R 2b独立地选自：（i）F; （ii）H; （iii）我; 和（iv）CH 2 OH; R 2c和R 2d独立地选自：（i）F; （ii）H; （iii）我; 和（iv）CH 2 OH; R 2e是H或Me; R 3a和R 3b独立地选自H和Me; R 4是H或Me; R 5是H或Me; R 6a和R 6b独立地选自H和Me; A是（IIa），其中R 7a选自N-连接的含N的C 5-7杂环基和（A）; 或（ii）式（IIb），其中X选自CH <子> 2 ，NH和O，R中的一个^{8A 和R选自^{8B 选择由Cl和乙氧基组成，而R 8a和R 8b中的另一个为H。}}}

3. 发明申请

WO2021009365A1 BENZOTHIOPHENE, THIENOPYRIDINE AND THIENOPYRIMIDINE DERIVATIVES FOR THE MODULATION OF STING 审中-公开
公开(公告)号：WO2021009365A1
公开(公告)日：2021-01-21
申请号：PCT/EP2020/070334
申请日：2020-07-17
申请人： CTXT PTY LIMITED
发明人： MORROW, Benjamin Joseph , HUBERT, Jonathan Grant , BOZIKIS, Ylva Elisabet Bergman , CAMERINO, Michelle Ang , CUZZUPE, Anthony Nicholas , STUPPLE, Paul Anthony
IPC分类号： A61P31/00 , A61P35/00 , C07D417/04 , C07D495/04 , A61K31/381 , C07D471/14 , C07D519/00
摘要： A compound of formula (I): wherein: Y is (CH2)n, where n is from 2 to 4; W1 and W11 are independently selected from OH and ORP, where RP is Me or Et.

4. 发明申请

WO2017153518A1 PRMT5 INHIBITORS 审中-公开
标题翻译： PRMT5抑制剂
公开(公告)号：WO2017153518A1
公开(公告)日：2017-09-14
申请号：PCT/EP2017/055535
申请日：2017-03-09
申请人： CTxT PTY LIMITED
发明人： STUPPLE, Paul Anthony , WALKER, Scott Raymond , CAMERINO, Michelle Ang
IPC分类号： C07D237/32 , C07D498/08 , A61K31/502 , A61P7/00 , A61P35/00
摘要： A compound of formula (Ia), (Ib) or (Ic) wherein: n is 1 or 2; R N is H or Me; R 1 is optionally one or more halo or methyl groups; R 2a and R 2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH 2 OH; R 2c and R 2d (if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH 2 OH; R 3a and R 3b are independently selected from H and Me; R 4a is selected from OH, -NH 2 , -C(=O)NH 2 , and -CH 2 OH; R 4b is either H or Me; X is either N or CH; R 7 is selected from H and C 1-4 alkyl; (a) one of R 8a , R 8b , R 8c and R 8d is selected from H, halo, C 1-4 alkyl, C 1-4 alkoxy, NHC 1-4 alkyl; (b) another of R 8a , R 8b , R 8c and R 8d is selected from H, C 1-4 alkyl, C 1-4 fluoroalkyl, C 3-6 cycloalkyl, C 5-6 heteroaryl, C 5-6 heteroaryl methyl, C 4-6 heterocyclyl, C 4-6 heterocyclyl methyl, phenyl, benzyl, halo, amido, amidomethyl, acylamido, acylamidomethyl, C 1-4 alkyl ester, C 1-4 alkyl ester methyl, C 1-4 alkyl carbamoyl, C 1-4 alkyl carbamoyl methyl, C 1-4 alkylacyl, C 1-4 alkylacyl methyl, phenylcarbonyl, carboxy, carboxymethyl, ether, amino, amino methyl, sulfonamido, sulfonamino, sulfone, sulfoxide, nitrile and nitrilemethyl; (c) the others of R 8a , R 8b , R 8c and R 8d are H.
摘要翻译：式（Ia），（Ib）或（Ic）的化合物，其中：n是1或2; R N是H或Me; R 1任选地是一个或多个卤素或甲基; R 2a和R 2b独立地选自：（i）F; （ii）H; （iii）我; 和（iv）CH 2 OH; R 2c和R 2d（如果存在）独立地选自：（i）F; （ii）H; （iii）我; 和（iv）CH 2 OH; R 3a和R 3b独立地选自H和Me; R 4a选自OH，-NH 2 2，-C（= O）NH 2和-CH 2，子> OH; R 4b是H或Me; X是N或CH; R 7选自H和C 1-4烷基; （a）R 8a，R 8b，R 8c和R 8d中的一个选自H，卤素，C 1-4烷基，C 1-4烷氧基，NHC 1-4烷基; （b）R 8a，R 8b，R 8c和R 8d中的另一个选自H，C C 1-4烷基，C 1-4氟代烷基，C 3-6环烷基，C 5-6杂芳基，C 5 -C 6杂芳基甲基，C 4-6杂环基，C 4-6杂环基甲基，苯基，苄基，卤素，酰氨基，酰胺基甲基，酰基酰胺基，酰基酰胺基甲基，C 1-4烷基酯，C 1-4烷基酯甲基，C 1-4烷基氨基甲酰基，C C 1-4烷基氨基甲酰基甲基，C 1-4烷基酰基，C 1-4烷基酰基甲基，苯基羰基，羧基，羧甲基，醚，氨基，氨基甲基，亚磺酰氨基，磺酰氨基，砜，亚砜，腈和腈甲基; （c）R 8a，R 8b，R 8c和R 8d其余为H。 p>

5. 发明申请

WO2021119753A1 COMPOUNDS 审中-公开
公开(公告)号：WO2021119753A1
公开(公告)日：2021-06-24
申请号：PCT/AU2020/051394
申请日：2020-12-18
申请人： CTXT PTY LIMITED
发明人： MORROW, Benjamin Joseph , HUBERT, Jonathan Grant , STUPPLE, Paul Anthony , CAMERINO, Michelle Ang , DENNIS, Matthew Lloyd , CUZZUPE, Anthony Nicholas
IPC分类号： C07D413/14 , C07D403/14 , C07D235/18 , A61P35/00 , A61K31/4184
摘要： This disclosure relates to compounds of formula (I), which are modulators of STING. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods of using compounds of formula (I) in the treatment or prevention of diseases ameliorated by the modulation of STING.

6. 发明申请

WO2017153513A1 TETRAHYDROISOQUINOLINES AS PRMT5 INHIBITORS 审中-公开
标题翻译：四氢异喹啉作为PRMT5抑制剂
公开(公告)号：WO2017153513A1
公开(公告)日：2017-09-14
申请号：PCT/EP2017/055529
申请日：2017-03-09
申请人： CTxT PTY LIMITED
发明人： BERGMAN, Ylva Elisabet , CAMERINO, Michelle Ang , WALKER, Scott Raymond , STUPPLE, Paul Anthony
IPC分类号： C07D401/14 , C07D405/14 , C07D217/16 , C07D401/12 , C07D413/12 , C07D471/04 , C07D498/08 , A61K31/4725 , A61K31/437 , A61P7/00 , A61P35/00
摘要： A compound of formula (I) wherein: n is 1 or 2; p is 0 or 1; R 1a , R 1b , R 1c and R 1d are independently selected from the group consisiting of H, halo, C 1-4 alkoxy, C 1-4 alkyl, C 1-4 fluoroalkyl, C 3-4 cycloalkyl, NH-C 1-4 alkyl and cyano; R 2a and R 2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH 2 OH; R 2c and R 2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH 2 OH; R 2e is H or Me; R 3a and R 3b are independently selected from H and Me; R 4 is either H or Me; R 5 is either H or Me; R 6a and R 6b are independently selected from H and Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C 5-12 heteroaryl; wherein when R 2e is H, at least one of R 1a , R 1b , R 1c and R 1d is selected from C 1-4 alkoxy, C 2-4 alkyl, C 1-4 fluoroalkyl, C 3-4 cycloalkyl, NH-C 1-4 alkyl and cyano.
摘要翻译：式（I）的化合物，其中：n是1或2; p是0或1; R 1a，R 1b，R 1c和R 1d独立地选自H，卤素，C 1-4烷氧基，C 1-4烷基，C 1-4氟代烷基，C 3-4 - / - 亚烷基 NH 2 -C 1-4烷基和氰基; R 2a和R 2b独立地选自：（i）F; （ii）H; （iii）我; 和（iv）CH 2 OH; R 2c和R 2d独立地选自：（i）F; （ii）H; （iii）我; 和（iv）CH 2 OH; R 2e是H或Me; R 3a和R 3b独立地选自H和Me; R 4是H或Me; R 5是H或Me; R 6a和R 6b独立地选自H和Me; A是（i）任选取代的苯基; （ii）任选取代的萘基; 或（iii）任选取代的C 5-12杂芳基; 其中当R 2ee为H时，R 1a，R 1b，R 1c和R 1b中至少一个为氢，其中1d选自C 1-4烷氧基，C 2-4烷基，C 1-4氟代烷基，C 3-4环烷基，NH-C 1-4烷基和氰基

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