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公开(公告)号:WO2023064519A1
公开(公告)日:2023-04-20
申请号:PCT/US2022/046645
申请日:2022-10-14
IPC分类号: C07C217/84 , C07C275/02 , A61K31/137 , A61K31/17 , A61P35/00
摘要: The present invention concerns a co-crystal of Elacestrant dihydrochloride and urea, its use in the preparation of another solid state form of Elecestrant or a salt thereof, and pharmaceutical compositions thereof.
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公开(公告)号:WO2022261401A1
公开(公告)日:2022-12-15
申请号:PCT/US2022/032952
申请日:2022-06-10
IPC分类号: A61P35/00 , C07C303/32 , C07D311/66 , A61K31/343 , C07C55/02
摘要: Solid state forms of Abexinostat salts and of Abexinostat tosylate : p-toluenesulfonic acid monohydrate complex, processes for preparation thereof, pharmaceutical compositions and uses thereof are disclosed.
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公开(公告)号:WO2022225712A1
公开(公告)日:2022-10-27
申请号:PCT/US2022/023758
申请日:2022-04-07
发明人: LAPIDO, Polina , RUDIK, Doron
IPC分类号: C07C323/66 , A61P9/12
摘要: The present disclosure encompasses solid state forms of Firibastat and salts or co-crystals thereof, processes for preparation thereof, and pharmaceutical compositions thereof.
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公开(公告)号:WO2022197884A1
公开(公告)日:2022-09-22
申请号:PCT/US2022/020684
申请日:2022-03-17
发明人: LAPIDO, Polina , SHUMACHER, Inbal , SHAUL, Ofir , RUDIK, Doron , ROMANOVA, Jana , KOLESA, Pavel
IPC分类号: C07D403/04 , C07D413/14 , A61K31/53 , A61P35/00
摘要: The present disclosure encompasses solid state forms of Zandelisib and HCI or HBr salts thereof, processes for preparation thereof, and pharmaceutical compositions thereof.
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公开(公告)号:WO2022020279A1
公开(公告)日:2022-01-27
申请号:PCT/US2021/042266
申请日:2021-07-20
IPC分类号: C07D471/04 , A61P35/00 , A61K31/437 , A61K31/4995
摘要: The present disclosure encompasses solid state forms of Selpercatinib, in embodiments crystalline polymorphs of Selpercatinib, processes for preparation thereof, and pharmaceutical compositions thereof.
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公开(公告)号:WO2021236709A1
公开(公告)日:2021-11-25
申请号:PCT/US2021/033060
申请日:2021-05-19
发明人: LAPIDO, Polina , RUDIK, Doron
摘要: The present disclosure encompasses solid state forms of Tapinarof, in embodiments crystalline polymorphs or co-crystals of Tapinarof, processes for preparation thereof, and pharmaceutical compositions thereof.
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公开(公告)号:WO2021046014A1
公开(公告)日:2021-03-11
申请号:PCT/US2020/048878
申请日:2020-09-01
IPC分类号: C07D487/22 , A61P35/00 , A61K31/55
摘要: The present disclosure encompasses solid state forms of Pamiparib, including crystalline polymorphs of Pamiparib, co-crystals and salts of Pamiparib, as well as processes for preparation thereof, and pharmaceutical compositions thereof.
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公开(公告)号:WO2021026307A1
公开(公告)日:2021-02-11
申请号:PCT/US2020/045128
申请日:2020-08-06
发明人: LUTHRA, Parven Kumar , AHMAD, Suhail , KISHOR, Neval , GOSWAMI, Miteshgir Kanchangir , SINGH, Alok , SINHA, Chandrasekhar , QUADRI, Syed Aziz Imam , JOSHI, Prashant Shankar , MAURYA, Sadanand Hardeo
IPC分类号: C07D217/26
摘要: The present invention provides new procedure and intermediates for the preparation of Roxadustat (1) comprising: (A) reducing a compound of formula 3', 3" or a mixture thereof: (3'), (3") wherein Pg is H or a OH protecting group, Ri is alkyl, aryl, or arylalkyl; R 2 , R 3 , R 4 , and Rs each independently represents alkyl, arylalkyl or alkenyl, or R 2 and R 3 and/or R 4 and Rs, taken together with the nitrogen atom to which they are bonded, each independently form a ring selected from: (I), wherein R 6 is H or C I- 6 alkyl; R 7 is Ci to C6 alkyl and X- is an anion selected from the group consisting of halide, O-SO 4 -R 7 wherein R 7 is Ci to C 6 alkyl, or O-SO 2 -Rs wherein Rs is phenyl, tolyl, methyl or trifluoromethyl; to form a compound of formula (2') wherein Pg is H or an OH protecting group, Ri is alkyl, aryl, or arylalkyl; and removing the Ri group and where present removing the OH protecting group; or (B) reducing a compound of formula 4', a compound of formula 4" or a mixture thereof: (4'), (4") wherein Pg is H or an OH protecting group; Ri is H, alkyl, aryl, or arylalkyl; R 2 , R 3 , R 4 , and R5 each independently represents alkyl, aryl, arylalkyl or alkenyl; or R 2 is Ci- 4 alkyl and R 3 is Ci- 4 alkoxy; or R 2 and R 3 and/or R 4 and R 5 , taken together with the nitrogen atom to which they are bonded, each independently form a group selected from: (I) wherein R 6 is H or C I-6 alkyl; and where Ri is not H, removing the Ri group, and, where present removing the OH protecting group.
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公开(公告)号:WO2021021775A1
公开(公告)日:2021-02-04
申请号:PCT/US2020/043815
申请日:2020-07-28
IPC分类号: C07D519/00 , A61P21/00 , A61P25/00
摘要: The present disclosure encompasses solid state forms of Risdiplam, including crystalline polymorphs of Risdiplam, processes for preparation thereof, and pharmaceutical compositions thereof.
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公开(公告)号:WO2021011345A1
公开(公告)日:2021-01-21
申请号:PCT/US2020/041524
申请日:2020-07-10
IPC分类号: C07D498/18 , A61P35/00
摘要: The present disclosure relates to crystalline Lorlatinib : Fumaric acid, solid state forms thereof, processes for preparation thereof, pharmaceutical compositions and methods of use thereof.
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