公开(公告)号：US11142525B2

公开(公告)日：2021-10-12

申请号：US16679820

申请日：2019-11-11

Applicant: Pfizer Inc.

Inventor： Rebecca Anne Gallego ,  Sajiv Krishnan Nair ,  Robert Steven Kania ,  Omar Khaled Ahmad ,  Ted William Johnson ,  Jamison Bryce Tuttle ,  Mehran Jalaie ,  Michele Ann McTigue ,  Dahui Zhou ,  Matthew L. Del Bel ,  Ru Zhou ,  Mingying He ,  Anne-Marie Dechert Schmitt

IPC: C07D471/04 ,  A61P35/00

Abstract: This invention relates to compounds of general Formula (I) and pharmaceutically acceptable salts thereof, in which R1, R1a, R2, R3, R4, and (R5)a are as defined herein, to pharmaceutical compositions comprising such compounds and pharmaceutically acceptable salts thereof, and to methods of using such compounds, pharmaceutically acceptable salts and compositions for the treatment of abnormal cell growth, including cancer.

公开(公告)号：US20150353579A1

公开(公告)日：2015-12-10

申请号：US14829842

申请日：2015-08-19

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Christopher John Helal ,  Bethany Lyn Kormos ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest

IPC: C07D519/00 ,  C07D487/04

CPC classification number: C07D519/00 ,  A61K31/4353 ,  A61K31/53 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention is directed to a new class of triazine derivatives as described by formula I below in which A, X, R1, R2, R3, and R4 are as defined herein and to the use of the compounds as PDE10 inhibitors.

Abstract translation: 本发明涉及如下式I所述的新一类三嗪衍生物，其中A，X，R 1，R 2，R 3和R 4如本文所定义，以及该化合物作为PDE10抑制剂的用途。

公开(公告)号：US08933224B2

公开(公告)日：2015-01-13

申请号：US14265458

申请日：2014-04-30

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Christopher John Helal ,  Bethany Lyn Kormos ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest

IPC: C07D487/04 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/53 ,  A61K31/4353 ,  A61P25/14

CPC classification number: C07D519/00 ,  A61K31/4353 ,  A61K31/53 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention is directed to a new class of triazine derivatives as described by formula I below in which A, X, R1, R2, R3, and R4 are as defined herein and to the use of the compounds as PDE10 inhibitors.

公开(公告)号：US20230120254A1

公开(公告)日：2023-04-20

申请号：US17932151

申请日：2022-09-14

Applicant: Pfizer Inc.

Inventor： Dafydd Rhys Owen ,  Matthew Richard Reese ,  Matthew Forrest Sammons ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest ,  Qingyi Yang

IPC: A61K31/403 ,  A61P31/14 ,  A61K31/427 ,  C07D403/12 ,  A61K31/401

Abstract: The invention relates to compounds of Formula I″ wherein R, R1, R2, R3, p, q and q′ are as defined herein, pharmaceutical compositions comprising the compounds, methods of treating coronavirus infection such as COVID-19 in a patient by administering therapeutically effective amounts of the compounds, and methods of inhibiting or preventing replication of coronaviruses such as SARS-CoV-2 with the compounds.

公开(公告)号：US20220401424A1

公开(公告)日：2022-12-22

申请号：US17246551

申请日：2021-04-30

Applicant: PFIZER INC.

Inventor： Joyann Barber ,  Sujin Cho-Schultz ,  Matthew L. Del Bel ,  Rebecca Anne Gallego ,  Mingying He ,  Mehran Jalaie ,  Robert Steven Kania ,  Michele Ann McTigue ,  Sajiv Krishnan Nair ,  Anne-Marie Dechert Schmitt ,  Jamison Bryce Tuttle ,  Dahui Zhou ,  Ru Zhou

IPC: A61K31/444 ,  A61K45/06 ,  C07D519/00 ,  C07D471/04

Abstract: This invention relates to compounds of general Formula I and pharmaceutically acceptable salts thereof, in which R1, R2, R3a, R3b, and R4 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：US20220062232A1

公开(公告)日：2022-03-03

申请号：US17395139

申请日：2021-08-05

Applicant: Pfizer Inc.

Inventor： Dafydd Rhys Owen ,  Martin Youngjin Pettersson ,  Matthew Richard Reese ,  Matthew Forrest Sammons ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest ,  Liuqing Wei ,  Qingyi Yang ,  Xiaojing Yang

IPC: A61K31/403 ,  C07D403/12 ,  A61K31/427 ,  A61P31/14

Abstract: The invention relates to compounds of Formula I″ wherein R, R1, R2, R3, p, q and q′ are as defined herein, pharmaceutical compositions comprising the compounds, methods of treating coronavirus infection such as COVID-19 in a patient by administering therapeutically effective amounts of the compounds, and methods of inhibiting or preventing replication of coronaviruses such as SARS-CoV-2 with the compounds.

公开(公告)号：US20200157098A1

公开(公告)日：2020-05-21

申请号：US16750505

申请日：2020-01-23

Applicant: PFIZER INC.

Inventor： Thomas Allen Chappie ,  Jaclyn Louise Henderson ,  Joseph Michael Young ,  Travis T. Wager ,  Bethany Lyn Kormos ,  Nandini Chaturbhai Patel ,  Simone Sciabola ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest ,  Joseph Walter Tucker

IPC: C07D471/04 ,  A61P25/22 ,  A61P25/24 ,  A61P25/18 ,  A61P25/16 ,  A61K31/55

Abstract: The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof wherein the variables R1, R2, R3, R4, R5, a and A are as defined herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D3-mediated (or D3-associated) disorders including, e.g., substance addiction, substance abuse, schizophrenia (e.g., its cognitive symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD or PD), Parkinson's disease, mania, anxiety, impulse control disorders, sexual disorders and depression.

公开(公告)号：US09296761B2

公开(公告)日：2016-03-29

申请号：US14829842

申请日：2015-08-19

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Christopher John Helal ,  Bethany Lyn Kormos ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest

IPC: C07D487/04 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00 ,  A61K31/53 ,  A61K31/4353

CPC classification number: C07D519/00 ,  A61K31/4353 ,  A61K31/53 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention is directed to a new class of triazine derivatives as described by formula I below in which A, X, R1, R2, R3, and R4 are as defined herein and to the use of the compounds as PDE10 inhibitors.

公开(公告)号：US20150080401A1

公开(公告)日：2015-03-19

申请号：US14549871

申请日：2014-11-21

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Christopher John Helal ,  Bethany Lyn Kormos ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest

IPC: C07D519/00 ,  C07D487/04

CPC classification number: C07D519/00 ,  A61K31/4353 ,  A61K31/53 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention is directed to a new class of triazine derivatives as described by formula I below in which A, X, R1, R2, R3, and R4 are as defined herein and to the use of the compounds as PDE10 inhibitors.

公开(公告)号：US11926642B2

公开(公告)日：2024-03-12

申请号：US17365213

申请日：2021-07-01

Applicant: Pfizer Inc.

Inventor： Robert Steven Kania ,  Padmavani Bezawada ,  Emma Louise Hawking ,  Rohit Jaini ,  Samir Kulkarni ,  Matthew Nathan O'Brien Laramy ,  Jonathan Richard Lillis ,  Suman Luthra ,  Dafydd Rhys Owen ,  Klimentina Dimitrova Pencheva ,  Anil Mahadeo Rane ,  Matthew Forrest Sammons ,  Bradley Paul Sullivan ,  Andrew John Thiel ,  Martyn David Ticehurst ,  Jamison Bryce Tuttle ,  Robert Louis Hoffman

IPC: C07F9/572 ,  A61P31/14

CPC classification number: C07F9/5728 ,  A61P31/14 ,  C07B2200/13

Abstract: The invention relates to compounds of formula I




wherein R1, R2 and - - - - - are as defined herein, pharmaceutical compositions comprising the compounds and methods of treating COVID-19 in a patient by administering therapeutically effective amounts of the compounds and methods of inhibiting or preventing replication of SARS-CoV-2 with the compounds.