公开(公告)号：US20200308191A1

公开(公告)日：2020-10-01

申请号：US16650505

申请日：2018-10-04

Applicant: Pfizer Inc.

Inventor： Paul Bowles ,  Peter Robert Rose

IPC: C07D498/18

Abstract: This invention relates to a crystalline form of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahy-dro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclo-tetradecine-3-carbonitrile (lorlatinib) free base hydrate (Form 24). This invention also relates to pharmaceutical compositions comprising Form 24, and to methods of using Form 24 and such compositions in the treatment of abnormal cell growth, such as cancer, in a mammal.

公开(公告)号：US09056831B2

公开(公告)日：2015-06-16

申请号：US14176081

申请日：2014-02-08

Applicant: Pfizer Inc.

Inventor： Antone John deBettencourt, III ,  Peter Robert Rose ,  Evgenyi Shalaev ,  George Joseph Quallich ,  Carl Bernard Ziegler

IPC: C07D207/00 ,  A61K31/40 ,  C07D207/34 ,  A61K9/14 ,  A61K9/19

CPC classification number: C07D207/34 ,  A61K9/145 ,  A61K9/146 ,  A61K9/19 ,  A61K31/40

Abstract: A process for forming amorphous atorvastatin comprising the steps of dissolving atorvastatin in a non-hydroxylic solvent and removing the solvent by freeze-drying, as well as processes of dissolving atorvastatin in a hydroxylic solvent with a solubilizing agent or an alkalizing agent or an antioxidant and removing the solvent by freeze-drying to afford amorphous atorvastatin.

Abstract translation: 一种形成无定形阿托伐他汀的方法，包括以下步骤：将阿托伐他汀溶解在非羟基溶剂中并通过冷冻干燥除去溶剂，以及将阿托伐他汀溶解在羟基溶剂中与增溶剂或碱化剂或抗氧化剂，以及 通过冷冻干燥除去溶剂，得到无定形的阿托伐他汀。

公开(公告)号：US12116368B2

公开(公告)日：2024-10-15

申请号：US17286018

申请日：2019-10-21

Applicant: Pfizer Inc.

Inventor： Brian Matthew Samas ,  Yong Tao ,  Douglas James Critcher ,  David Sydney Bernard Daniels ,  Kevin Paul Girard ,  Gregory Scott Goeken ,  Peter Robert Rose

IPC: C07D487/04

CPC classification number: C07D487/04 ,  C07B2200/13

Abstract: The present invention discloses a novel p-toluenesulfonic acid salt and a crystalline polymorphic Form 1 of said salt of 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one, pharmaceutical composition containing the same, as well as preparations and uses thereof. The present invention also discloses a novel phosphoric acid salt of 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one, pharma-ceutical composition containing the same, as well as preparations and uses thereof.

公开(公告)号：US20210387989A1

公开(公告)日：2021-12-16

申请号：US17286018

申请日：2019-10-21

Applicant: Pfizer Inc.

Inventor： Brian Matthew SAMAS ,  Yong TAO ,  Douglas James Critcher ,  David Sydney Bernard Daniels ,  Kevin Paul Girard ,  Gregory Scott Goeken ,  Peter Robert Rose

IPC: C07D487/04

Abstract: The present invention discloses a novel p-toluenesulfonic acid salt and a crystalline polymorphic Form 1 of said salt of 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one, pharmaceutical composition containing the same, as well as preparations and uses thereof. The present invention also discloses a novel phosphoric acid salt of 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one, pharmaceutical composition containing the same, as well as preparations and uses thereof.

公开(公告)号：US11299500B2

公开(公告)日：2022-04-12

申请号：US16650505

申请日：2018-10-04

Applicant: Pfizer Inc.

Inventor： Paul Bowles ,  Peter Robert Rose

IPC: C07D498/18 ,  A61P35/00 ,  A61K31/439

Abstract: This invention relates to a crystalline form 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]benzoxadiazacyclo-tetradecine-3-carbonitrile (lorlatinib) free base hydrate (Form 24). This invention also relates to pharmaceutical compositions comprising Form 24, and to methods of using Form 24 and such compositions in the treatment of abnormal cell growth, such as cancer, in a mammal.

公开(公告)号：US20140155627A1

公开(公告)日：2014-06-05

申请号：US14176081

申请日：2014-02-08

Applicant: Pfizer Inc.

Inventor： Antone John deBettencourt, III ,  Peter Robert Rose ,  Evgenyi Shalaev ,  George Joseph Quallich ,  Carl Bernard Ziegler

IPC: C07D207/34

CPC classification number: C07D207/34 ,  A61K9/145 ,  A61K9/146 ,  A61K9/19 ,  A61K31/40

Abstract: A process for forming amorphous atorvastatin comprising the steps of dissolving atorvastatin in a non-hydroxylic solvent and removing the solvent by freeze-drying, as well as processes of dissolving atorvastatin in a hydroxylic solvent with a solubilizing agent or an alkalizing agent or an antioxidant and removing the solvent by freeze-drying to afford amorphous atorvastatin.

Abstract translation: 一种形成无定形阿托伐他汀的方法，包括以下步骤：将阿托伐他汀溶解在非羟基溶剂中，并通过冷冻干燥除去溶剂，以及将阿托伐他汀溶解在羟基溶剂中，与增溶剂或碱化剂或抗氧化剂，以及 通过冷冻干燥除去溶剂，得到无定形的阿托伐他汀。