公开(公告)号：US20190292157A1

公开(公告)日：2019-09-26

申请号：US16380256

申请日：2019-04-10

Applicant: Pfizer Inc.

Inventor： Agustin Casimiro-Garcia ,  Jeffrey Scott Condon ,  Andrew Christopher Flick ,  Ariamala Gopalsamy ,  Steven J. Kirincich ,  John Paul Mathias ,  Joseph Walter Strohbach ,  Jason Shaoyun Xiang ,  Li Huang Xing ,  Xiaolun Wang

IPC: C07D239/42 ,  A61P35/00 ,  A61P1/04 ,  A61P1/00 ,  C07D405/10 ,  A61K31/505 ,  C07D401/12 ,  C07D241/14 ,  C07D239/28 ,  C07D403/12

Abstract: Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US10308615B2

公开(公告)日：2019-06-04

申请号：US15574625

申请日：2016-05-16

Applicant: Pfizer Inc.

Inventor： Agustin Casimiro-Garcia ,  Jeffrey Scott Condon ,  Andrew Christopher Flick ,  Ariamala Gopalsamy ,  Steven J. Kirincich ,  John Paul Mathias ,  Joseph Walter Strobach ,  Jason Shaoyun Xiang ,  Li Huang Xing ,  Xiaolun Wang

IPC: C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  A61K31/505 ,  C07D239/28 ,  C07D241/14 ,  A61P1/00 ,  A61P1/04 ,  A61P35/00 ,  C07D405/10

Abstract: Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US20180148420A1

公开(公告)日：2018-05-31

申请号：US15574625

申请日：2016-05-16

Applicant: Pfizer Inc.

Inventor： Agustin Casimiro-Garcia ,  Jeffrey Scott Condon ,  Andrew Christopher Flick ,  Ariamala Gopalsamy ,  Steven J. Kirincich ,  John Paul Mathias ,  Joseph Walter Strobach ,  Jason Shaoyun Xiang ,  Li Huang Xing ,  Xiaolun Wang

IPC: C07D239/42 ,  A61P1/00 ,  A61P1/04 ,  A61P35/00 ,  C07D401/12 ,  C07D403/12 ,  C07D405/10

CPC classification number: C07D239/42 ,  A61K31/505 ,  A61P1/00 ,  A61P1/04 ,  A61P35/00 ,  C07D239/28 ,  C07D241/14 ,  C07D401/12 ,  C07D403/12 ,  C07D405/10

Abstract: Compounds, pharmaceutically acceptable salts thereof are disclosed wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US09663526B2

公开(公告)日：2017-05-30

申请号：US14829753

申请日：2015-08-19

Applicant: Pfizer Inc.

Inventor： Andrew Fensome ,  Ariamala Gopalsamy ,  Brian S. Gerstenberger ,  Ivan Viktorovich Efremov ,  Zhao-Kui Wan ,  Betsy Pierce ,  Jean-Baptiste Telliez ,  John I. Trujillo ,  Liying Zhang ,  Li Xing ,  Eddine Saiah

IPC: A61K31/506 ,  C07D487/08 ,  A61K45/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D519/00

CPC classification number: A61K31/55 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D487/08 ,  C07D519/00

Abstract: A compound having the structure: or an acceptable salt thereof, wherein X is N or CR, where R is hydrogen, alkyl, etc.; A is selected from the group consisting of a bond, C═O, —SO2—, etc.; A′ is selected from the group consisting of a bond, C═O, etc.; Z is —(CH2)h— or a bond, etc.; R1 and R1′ are independently selected from the group consisting of hydrogen, alkyl, etc.; R2 is selected from hydrogen, alkyl, etc.; R3 is selected from the group consisting of hydrogen, and amino; R4 is monocyclic or bicyclic, etc.; R5 is independently selected from hydrogen, alkyl, etc.; h, j, k, m, n and q are integers as defined in the specification. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations with other therapeutic agents.

公开(公告)号：US08575159B2

公开(公告)日：2013-11-05

申请号：US13718928

申请日：2012-12-18

Applicant: Pfizer Inc.

Inventor： Aranapakam Mudumbai Venkatesan ,  Zecheng Chen ,  Christoph Martin Dehnhardt ,  Osvaldo Dos Santos ,  Efren Guillermo Delos Santos ,  Arie Zask ,  Jeroen Cunera Verheijen ,  Joshua Aaron Kaplan ,  David James Richard ,  Semiramis Ayral-Kaloustian ,  Tarek Suhayl Mansour ,  Ariamala Gopalsamy ,  Kevin Joseph Curran ,  Mengxiao Shi

IPC: A61K31/535 ,  C07D413/14

CPC classification number: C07D401/12 ,  A61K31/5377 ,  A61K45/06 ,  C07D251/18 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D407/14 ,  C07D409/12 ,  C07D413/04 ,  C07D413/14 ,  C07D451/06 ,  C07D453/02 ,  C07D491/113 ,  C07D498/08

Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.