公开(公告)号：US20230002352A1

公开(公告)日：2023-01-05

申请号：US17760861

申请日：2020-09-18

申请人： Step Pharma S.A.S.

发明人： Andrew Novak ,  Abdul Quddus ,  David Cousin ,  Joseph Wrigglesworth ,  Emma Blackham ,  Geraint Jones ,  Lorna Duffy ,  Louise Birch ,  Pascal George ,  Saleh Ahmed

IPC分类号： C07D401/12 ,  C07D403/12 ,  C07D405/14 ,  C07D401/14

摘要： The invention provides a compound of formula (I): formula (I) and the use of such compounds as cytidine triphosphate synthase 1 inhibitors, particularly in the treatment or prophylaxis of disorders associated with cell proliferation.

公开(公告)号：US20210387965A1

公开(公告)日：2021-12-16

申请号：US17287137

申请日：2019-10-23

申请人： Step Pharma S.A.S.

发明人： Abdul Quddus ,  Andrew Novak ,  David Cousin ,  Emma Blackham ,  Geraint Jones ,  Joseph Wrigglesworth ,  Lorna Duffy ,  Louise Birch ,  Pascal George ,  Saleh Ahmed

IPC分类号： C07D401/14 ,  C07D405/14

摘要： Compounds of formula (I), and related aspects.

公开(公告)号：US20230020663A1

公开(公告)日：2023-01-19

申请号：US17760886

申请日：2020-09-18

申请人： Step Pharma S.A.S.

发明人： Andrew Novak ,  Abdul Quddus ,  David Cousin ,  Joseph Wrigglesworth ,  Emma Blackham ,  Geraint Jones ,  Lorna Duffy ,  Louise Birch ,  Pascal George ,  Saleh Ahmed

IPC分类号： C07D401/12 ,  C07D403/12 ,  C07D405/14 ,  C07D401/14 ,  C07D239/42 ,  C07D417/12 ,  C07D277/54

摘要： The invention provides a compound of formula (I) and processes for the manufacture of such compounds, related intermediates, compositions comprising such compounds and the use of such compounds as cytidine triphosphate synthase 1 inhibitors, particularly in the treatment or prophylaxis of disorders associated with cell proliferation.

公开(公告)号：US11505547B2

公开(公告)日：2022-11-22

申请号：US16767379

申请日：2018-11-30

申请人： STEP PHARMA S.A.S.

发明人： Andrew Novak ,  Geraint Jones ,  Joseph Wrigglesworth ,  Lorna Duffy ,  Louise Birch ,  Pascal George

IPC分类号： C07D241/12 ,  C07D401/12 ,  C07D417/12 ,  C07D417/14 ,  C07D277/52 ,  C07D213/22 ,  C07D213/38 ,  A61K31/425 ,  A61P35/00 ,  A61P37/00

摘要： Compounds of formula (I) and related aspects.

公开(公告)号：US20220324837A1

公开(公告)日：2022-10-13

申请号：US17615873

申请日：2020-06-04

申请人： Step Pharma S.A.S.

发明人： Abdul Quddus ,  Andrew Novak ,  David Cousin ,  Emma Blackham ,  Geraint Jones ,  Joseph Wrigglesworth ,  Lorna Duffy ,  Louise Birch ,  Pascal George ,  Saleh Ahmed

IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D239/42 ,  C07D405/04 ,  C07D401/04 ,  C07D239/38

摘要： Compounds of formula (I) as human cytidine triphosphate synthase 1 (CTPS1) inhibitors for the treatment of prolifera-tive diseases, such as e.g. cancer, such as e.g. leukemia and lymphoma, e.g. inflammatory skin diseases such as psoriasis, or e.g. multiple sclerosis. The present description discloses the synthesis and characterisa-tion of exemplary compounds as well as pharmacological data thereof (e.g. pages 64 to 80; examples; biological examples 1 and 2; e.g. compounds P140, P231 to P263; tables 1 to 10). Specific examples are e.g.: N-(5-(6-ethoxypyrazin-2-yl)pyridin-2-yl)-4-(2-(methylsulfonami-N do) pyrimidin-4-yl)tetrahydro-2H-pyran-4-carboxamide (Formula (II)), or 1-(2-(cyclopropanesulfonamido)pyrimidin-4-yl)-N-(5-(6-ethoxypyrazin-2-yl)pyridin-2-yl)cyclohexane-1-carboxamide (Formula (III)).

公开(公告)号：US20210024507A1

公开(公告)日：2021-01-28

申请号：US16982641

申请日：2019-03-22

申请人： Step Pharma S.A.S.

发明人： Abdul Quddus ,  Andrew Novak ,  David Cousin ,  Emma Blackham ,  Geraint Jones ,  Joseph Wrigglesworth ,  Lorna Duffy ,  Louise Birch ,  Pascal George ,  Saleh Ahmed

IPC分类号： C07D405/14 ,  C07D401/12 ,  C07D403/12 ,  C07D401/14 ,  C07D239/42

摘要： Compounds of formula (I): and related aspects.

公开(公告)号：US20230192673A1

公开(公告)日：2023-06-22

申请号：US17980186

申请日：2022-11-03

申请人： Step Pharma S.A.S.

发明人： Abdul Quddus ,  Andrew Novak ,  David Cousin ,  Emma Blackham ,  Geraint Jones ,  Joseph Wrigglesworth ,  Lorna Duffy ,  Louise Birch ,  Pascal George ,  Saleh Ahmed

IPC分类号： C07D405/14 ,  C07D239/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

CPC分类号： C07D405/14 ,  C07D239/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

摘要： Compounds of formula (I):




and related aspects.

公开(公告)号：US11655246B2

公开(公告)日：2023-05-23

申请号：US16767338

申请日：2018-11-30

申请人： STEP PHARMA S.A.S.

发明人： Abdul Quddus ,  Andrew Novak ,  David Cousin ,  Elli Chatzopoulou ,  Emma Blackham ,  Geraint Jones ,  Jennifer Thomas ,  Joseph Wrigglesworth ,  Lorna Duffy ,  Louise Birch ,  Pascal George ,  Saleh Ahmed

IPC分类号： C07D417/14 ,  C07D277/52 ,  C07D417/12

CPC分类号： C07D417/14 ,  C07D277/52 ,  C07D417/12

摘要： Compounds of formula (I): (I) and related aspects.

公开(公告)号：US20230086703A1

公开(公告)日：2023-03-23

申请号：US17615879

申请日：2020-06-04

申请人： Step Pharma S.A.S.

发明人： Abdul Quddus ,  Andrew Novak ,  David Cousin ,  Emma Blackham ,  Ellie Chatzopoulou ,  Geraint Jones ,  Jennifer Thomas ,  Joseph Wrigglesworth ,  Lorna Duffy ,  Louise Birch ,  Pascal George ,  Saleh Ahmed ,  Gianna Toschi

IPC分类号： C07D417/12 ,  C07D277/28 ,  C07D417/14

摘要： Compounds of formula (I) wherein ring B is selected from the group consisting of Formula (B-a) and Formula (B-bc) as human cytidine triphosphate synthase 1 (CTPS 1) inhibitors for the treatment of proliferative diseases, such as e.g. cancer, such as e.g. leukemia and lymphoma, e.g. inflammatory skin diseases such as psoriasis, or e.g. multiple sclerosis. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. page 129 to page 302; examples; biological examples 1 and 2; tables 1-17). Specific examples are e.g.: N-(4-(5-Chloropyridin-3-yl)phenyl)-2-(2-(cyclopropane-sulfonamido) pyrimidin-4-yl)butanamide (Formula P1) or 1-(2-(Cyclopropanesulfonamido)pyrimidin-4-yl)-N-(4-(6-ethoxypyrazin-2-yl)phenyl)cyclopentanecarboxamide (Formula P2).