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.

公开(公告)号：US20150251999A1

公开(公告)日：2015-09-10

申请号：US14716361

申请日：2015-05-19

Applicant: Pfizer Inc.

Inventor： Anthony Michael Campeta ,  Joseph Francis Krzyzaniak ,  Jason Albert Leonard

IPC: C07D207/34 ,  C07D295/027 ,  C07C215/08 ,  C07C211/07 ,  C07C229/26

CPC classification number: C07D207/34 ,  C07C211/07 ,  C07C215/08 ,  C07C229/26 ,  C07D295/027 ,  C07D295/037

Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.

Abstract translation: [R-（R *，R *）] - 2-（4-氟苯基） - ，b-的新型盐形式，δ-二羟基-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基 ] -1H-吡咯-1-庚酸，其特征在于它们的X射线粉末衍射图和固态NMR光谱，以及其制备方法和药物组合物，其可用作治疗高脂血症的药剂 ，高胆固醇血症，骨质疏松症，良性前列腺增生症和阿尔茨海默病。

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。

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.

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.

公开(公告)号：US20160185720A1

公开(公告)日：2016-06-30

申请号：US15061931

申请日：2016-03-04

Applicant: Pfizer Inc.

Inventor： Anthony Michael Campeta ,  Joseph Francis Krzyzaniak ,  Jason Albert Leonard

IPC: C07D207/34 ,  C07C215/08 ,  C07C229/26 ,  C07D295/027 ,  C07C211/07

CPC classification number: C07D207/34 ,  C07C211/07 ,  C07C215/08 ,  C07C229/26 ,  C07D295/027 ,  C07D295/037

Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.

公开(公告)号：US20140336395A1

公开(公告)日：2014-11-13

申请号：US14340067

申请日：2014-07-24

Applicant: Pfizer Inc.

Inventor： Anthony Michael Campeta ,  Joseph Francis Krzyzaniak ,  Jason Albert Leonard

IPC: C07D207/34 ,  C07C215/08 ,  C07D295/027 ,  C07C211/07 ,  C07C229/26

CPC classification number: C07D207/34 ,  C07C211/07 ,  C07C215/08 ,  C07C229/26 ,  C07D295/027 ,  C07D295/037

Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.

Abstract translation: [R-（R *，R *）] - 2-（4-氟苯基） - ，b-的新型盐形式，δ-二羟基-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基 ] -1H-吡咯-1-庚酸，其特征在于它们的X射线粉末衍射图和固态NMR光谱，以及其制备方法和药物组合物，其可用作治疗高脂血症的药剂 ，高胆固醇血症，骨质疏松症，良性前列腺增生症和阿尔茨海默病。

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。

公开(公告)号：US20170190663A1

公开(公告)日：2017-07-06

申请号：US15468419

申请日：2017-03-24

Applicant: Pfizer Inc.

Inventor： Anthony Michael Campeta ,  Joseph Francis Krzyzaniak ,  Jason Albert Leonard

IPC: C07D207/34 ,  C07C229/26 ,  C07D295/027 ,  C07C211/07

CPC classification number: C07D207/34 ,  C07C211/07 ,  C07C215/08 ,  C07C229/26 ,  C07D295/027 ,  C07D295/037

Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.

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

IPC: A61K31/55 ,  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.

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。