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公开(公告)号：US20220017548A1
公开(公告)日：2022-01-20
申请号：US17365213
申请日：2021-07-01
Applicant: Pfizer Inc.
Inventor： Robert Steven Kania , Padmavani Bezawada , Emma Louise Hawking , Rohit Jaini , Samir Kulkarni , Matthew Nathan O'Brien Laramy , Jonathan Richard Lillis , Suman Luthra , Dafydd Rhys Owen , Klimentina Dimitrova Pencheva , Martin Youngjin Pettersson , Anil Mahadeo Rane , Matthew Forrest Sammons , Bradley Paul Sullivan , Andrew John Thiel , Martyn David Ticehurst , Jamison Bryce Tuttle , Robert Louis Hoffman
Abstract: The invention relates to compounds of formula I wherein R1, R2 and - - - - - are as defined herein, pharmaceutical compositions comprising the compounds and methods of treating COVID-19 in a patient by administering therapeutically effective amounts of the compounds and methods of inhibiting or preventing replication of SARS-CoV-2 with the compounds.
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![Salts and polymorphs of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one](/abs-image/US/2015/06/02/US09045487B2/abs.jpg.150x150.jpg)
2.发明授权Salts and polymorphs of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one 有权8-氟-2- {4 - [（甲基氨基）甲基]苯基} -1,3,4,5-四氢-6H-吖庚因并[5,4，3-c]吲哚-6-酮的盐和多晶型物公开(公告)号：US09045487B2
公开(公告)日：2015-06-02
申请号：US14272589
申请日：2014-05-08
Applicant: Pfizer Inc.
Inventor： Patricia Ann Basford , Anthony Michael Campeta , Adam Gillmore , Matthew Cameron Jones , Eleftherios Kougoulos , Suman Luthra , Robert Walton
IPC: C07D487/06 , C07C57/145 , C07C309/19
CPC classification number: A61K31/55 , A61K45/06 , C07C57/145 , C07C309/19 , C07D487/06
Abstract: The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
Abstract translation: 本发明涉及8-氟-2- {4 - [（甲基氨基）甲基]苯基} -1,3,4,5-四氢-6H-氮杂[5,43-cd]吲哚的新型多晶型物 -6-one，以及其准备过程。 这样的多晶型物可以是药物组合物的组分，并且可以用于治疗由聚（ADP-核糖）聚合酶活性介导的哺乳动物疾病状况，包括疾病状况如癌症。
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![SALTS AND POLYMORPHS OF 8-FLUORO-2-{4-[(METHYLAMINO)METHYL]PHENYL}-1,3,4,5-TETRAHYDRO-6H-AZEPINO[5,4,3-CD]INDOL-6-ONE](/abs-image/US/2018/04/05/US20180092925A1/abs.jpg.150x150.jpg)
3.发明申请公开(公告)号：US20180092925A1
公开(公告)日：2018-04-05
申请号：US15833073
申请日：2017-12-06
Applicant: Pfizer Inc.
Inventor： Patricia Ann Basford , Anthony Michael Campeta , Adam Gillmore , Matthew Cameron Jones , Eleftherios Kougoulos , Suman Luthra , Robert Walton
IPC: A61K31/55 , A61K45/06 , C07D487/06 , C07C57/145 , C07C309/19
CPC classification number: A61K31/55 , A61K45/06 , C07C57/145 , C07C309/19 , C07D487/06
Abstract: The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
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公开(公告)号：US09637500B2
公开(公告)日：2017-05-02
申请号：US14898582
申请日：2014-06-17
Applicant: Pfizer Inc.
Inventor： Andrew James Jensen , Suman Luthra , Paul Francis Richardson
IPC: C07D213/65 , A61K31/4439 , C07D498/18
CPC classification number: C07D498/18
Abstract: This invention relates to crystalline solvates of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benz- oxadiazacyclotetradecine-3-carbonitrile, useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to pharmaceutical compositions comprising such crystalline solvates, and to methods of using such solvates and compositions in the treatment of abnormal cell growth in mammals, especially humans.
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Patent Agency Ranking
![SALTS AND POLYMORPHS OF 8-FLUORO-2--1,3,4,5-TETRAHYDRO-6H-AZEPINO[5,4,3-CD]INDOL-6-ONE](/abs-image/US/2014/08/28/US20140243318A1/abs.jpg.150x150.jpg)
5.发明申请SALTS AND POLYMORPHS OF 8-FLUORO-2--1,3,4,5-TETRAHYDRO-6H-AZEPINO[5,4,3-CD]INDOL-6-ONE 有权8-氟-2-（1,2,3,4,5-四氢-6H-吡啶并[5,4,3-CD]吲哚-6-酮的盐和多元醇公开(公告)号：US20140243318A1
公开(公告)日：2014-08-28
申请号：US14272589
申请日：2014-05-08
Applicant: Pfizer Inc.
Inventor： Patricia Ann Basford , Anthony Michael Campeta , Adam Gillmore , Matthew Cameron Jones , Eleftherios Kougoulos , Suman Luthra , Robert Walton
IPC: C07D487/06 , C07C57/145 , C07C309/19
CPC classification number: A61K31/55 , A61K45/06 , C07C57/145 , C07C309/19 , C07D487/06
Abstract: The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
Abstract translation: 本发明涉及8-氟-2- {4 - [（甲基氨基）甲基]苯基} -1,3,4,5-四氢-6H-氮杂[5,43-cd]吲哚的新型多晶型物 -6-one，以及其准备过程。 这样的多晶型物可以是药物组合物的组分，并且可以用于治疗由聚（ADP-核糖）聚合酶活性介导的哺乳动物疾病状况，包括疾病状况如癌症。
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![SALTS AND POLYMORPHS OF 8-FLUORO-2--1,3,4,5-TETRAHYDRO-6H-AZEPINO[5,4,3-CD]INDOL-6-ONE](/abs-image/US/2015/08/27/US20150238504A1/abs.jpg.150x150.jpg)
6.发明申请SALTS AND POLYMORPHS OF 8-FLUORO-2--1,3,4,5-TETRAHYDRO-6H-AZEPINO[5,4,3-CD]INDOL-6-ONE 有权8-氟-2-（1,2,3,4,5-四氢-6H-吡啶并[5,4,3-CD]吲哚-6-酮的盐和多元醇公开(公告)号：US20150238504A1
公开(公告)日：2015-08-27
申请号：US14698463
申请日：2015-04-28
Applicant: Pfizer Inc.
Inventor： Patricia Ann Basford , Anthony Michael Campeta , Adam Gillmore , Matthew Cameron Jones , Eleftherios Kougoulos , Suman Luthra , Robert Walton
CPC classification number: A61K31/55 , A61K45/06 , C07C57/145 , C07C309/19 , C07D487/06
Abstract: The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
Abstract translation: 本发明涉及8-氟-2- {4 - [（甲基氨基）甲基]苯基} -1,3,4,5-四氢-6H-氮杂[5,43-cd]吲哚的新型多晶型物 -6-one，以及其准备过程。 这样的多晶型物可以是药物组合物的组分，并且可以用于治疗由聚（ADP-核糖）聚合酶活性介导的哺乳动物疾病状况，包括疾病状况如癌症。
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公开(公告)号：US11926642B2
公开(公告)日：2024-03-12
申请号：US17365213
申请日：2021-07-01
Applicant: Pfizer Inc.
Inventor： Robert Steven Kania , Padmavani Bezawada , Emma Louise Hawking , Rohit Jaini , Samir Kulkarni , Matthew Nathan O'Brien Laramy , Jonathan Richard Lillis , Suman Luthra , Dafydd Rhys Owen , Klimentina Dimitrova Pencheva , Anil Mahadeo Rane , Matthew Forrest Sammons , Bradley Paul Sullivan , Andrew John Thiel , Martyn David Ticehurst , Jamison Bryce Tuttle , Robert Louis Hoffman
CPC classification number: C07F9/5728 , A61P31/14 , C07B2200/13
Abstract: The invention relates to compounds of formula I
wherein R1, R2 and - - - - - are as defined herein, pharmaceutical compositions comprising the compounds and methods of treating COVID-19 in a patient by administering therapeutically effective amounts of the compounds and methods of inhibiting or preventing replication of SARS-CoV-2 with the compounds.-
![Salts and polymorphs of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one](/abs-image/US/2019/05/07/US10278974B2/abs.jpg.150x150.jpg)
公开(公告)号：US10278974B2
公开(公告)日：2019-05-07
申请号：US15833073
申请日：2017-12-06
Applicant: Pfizer Inc.
Inventor： Patricia Ann Basford , Anthony Michael Campeta , Adam Gillmore , Matthew Cameron Jones , Eleftherios Kougoulos , Suman Luthra , Robert Walton
IPC: C07D487/06 , A61K31/55 , C07C57/145 , C07C309/19 , A61K45/06
Abstract: The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
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![Salts and polymorphs of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one](/abs-image/US/2018/01/09/US09861638B2/abs.jpg.150x150.jpg)
公开(公告)号：US09861638B2
公开(公告)日：2018-01-09
申请号：US14698463
申请日：2015-04-28
Applicant: Pfizer Inc.
Inventor： Patricia Ann Basford , Anthony Michael Campeta , Adam Gillmore , Matthew Cameron Jones , Eleftherios Kougoulos , Suman Luthra , Robert Walton
IPC: A61K31/55 , C07D487/06 , C07C57/145 , C07C309/19 , A61K45/06
CPC classification number: A61K31/55 , A61K45/06 , C07C57/145 , C07C309/19 , C07D487/06
Abstract: The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
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