公开(公告)号：US20220127262A1

公开(公告)日：2022-04-28

申请号：US17423143

申请日：2020-01-13

Applicant: Pfizer Inc.

Inventor： Douglas Carl Behenna ,  Martha Alicia Ornelas

IPC: C07D471/04 ,  A61P35/00

Abstract: The invention relates to a crystalline form of 6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcyclopentyl]-2-{[1-(methylsulfonyl) piperidin-4-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one (PF-06873600) free base (Form 1). The invention also relates to pharmaceutical compositions comprising this crystalline form and to methods of using the crystalline form and such compositions for the treatment of abnormal cell growth, such as cancer, in a mammal Formula (I):

公开(公告)号：US11203594B2

公开(公告)日：2021-12-21

申请号：US16849329

申请日：2020-04-15

Applicant: Pfizer Inc.

Inventor： Samit Kumar Bhattacharya ,  Douglas Carl Behenna ,  Kimberly O. Cameron ,  Ping Chen ,  John M. Curto ,  Kevin Daniel Freeman-Cook ,  Mehran Jalaie ,  Robert Steven Kania ,  Yajing Lian ,  Sajiv Krishnan Nair ,  Cynthia Louise Palmer ,  Martin Youngjin Pettersson ,  Eugene Yuanjin Rui ,  Matthew Sammons ,  Qingyi Yang ,  Liying Zhang

IPC: C07D471/04 ,  A61P9/12

Abstract: This invention relates to compounds of general Formula I in which A, R1, R2, R3 and R4 are as defined herein, and the pharmaceutically acceptable salts thereof; to pharmaceutical compositions comprising such compounds and salts; to methods of using such compounds, salts and compositions for treating pulmonary hypertension and related diseases, like pulmonary arterial hypertension; to methods of using such compounds, salts and compositions for treating abnormal cell growth, such as cancer; and to processes to make such compounds, salts and compositions.

公开(公告)号：US20210269425A1

公开(公告)日：2021-09-02

申请号：US17235846

申请日：2021-04-20

Applicant: Pfizer Inc.

Inventor： Douglas Carl Behenna ,  Kevin Daniel Freeman-Cook ,  Robert Louis Hoffman ,  Asako Nagata ,  Sacha Ninkovic ,  Scott Channing Sutton

IPC: C07D403/12 ,  A61P35/00 ,  C07D413/12

Abstract: This invention relates to compounds of Formula (I) and enantiomers thereof, and to pharmaceutically acceptable salts of Formula (I) and said enantiomers, wherein R1, R2 and R3 are as defined herein. The invention further relates to pharmaceutical compositions comprising such compounds and salts, and to methods and uses of such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer, in a subject in need thereof.

公开(公告)号：US20190135817A1

公开(公告)日：2019-05-09

申请号：US16251032

申请日：2019-01-17

Applicant: Pfizer Inc.

Inventor： Douglas Carl Behenna ,  Ping Chen ,  Kevin Daniel Freeman-Cook ,  Robert Louis Hoffman ,  Mehran Jalaie ,  Asako Nagata ,  Sajiv Krishnan Nair ,  Sacha Ninkovic ,  Martha Alicia Ornelas ,  Cynthia Louise Palmer ,  Eugene Yuanjin Rui

IPC: C07D487/04 ,  C07D401/14 ,  C07D471/04

Abstract: This invention relates to compounds of general Formula (I) and pharmaceutically acceptable salts thereof, in which R1, R2 , R2A , R2B, R3, R4, R5A, R5B, R6, R7, R8, R9, p, q and r are as defined herein, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.

公开(公告)号：US20150141402A1

公开(公告)日：2015-05-21

申请号：US14548749

申请日：2014-11-20

Applicant: PFIZER INC.

Inventor： Douglas Carl Behenna ,  Hengmiao Cheng ,  Sujin Cho-Schultz ,  Theodore Otto Johnson, JR. ,  John Charles Kath ,  Asako Nagata ,  Sajiv Krishnan Nair ,  Simon Paul Planken

IPC: C07D473/16

CPC classification number: C07D473/16 ,  A61K31/519 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/5386 ,  C07D473/18 ,  C07D519/00

Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, G, ring A, ring B, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, and m are defined herein. The novel purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，其中Q，G，环A，环B，R1，R2，R3，R4，R5，R5a，R6，R7，R8，R9， R 11，R 12，R 13，R 14，R 15，R 16，R 17，R 18，R 19，R 20，R 21，R 22，R 23，R 24和m如本文所定义。 新型嘌呤衍生物可用于治疗哺乳动物中异常细胞生长，如癌症。 另外的实施方案涉及含有化合物的药物组合物和使用化合物和组合物治疗哺乳动物异常细胞生长的方法。