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：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.