公开(公告)号：US20230340530A1

公开(公告)日：2023-10-26

申请号：US18041447

申请日：2021-08-27

Applicant: Pfizer Inc.

Inventor： Timothy Leyden Foley ,  Christopher John Helal

IPC: C12N15/86 ,  C12N15/113

CPC classification number: C12N15/86 ,  C12N15/113 ,  C12N2310/11 ,  C12N2320/51 ,  C12N2320/52 ,  C12N2770/24243

Abstract: The present invention provides methods of protecting ribonucleic acid (RNA) from degradation under certain conditions by contacting the RNA with compounds that contain at least one boron atom. The present invention also provides compositions comprising such compounds and RNA.

公开(公告)号：US20170145022A1

公开(公告)日：2017-05-25

申请号：US15426423

申请日：2017-02-07

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Nandini Chaturbhai Patel ,  Matthew Merrill Hayward ,  Christopher John Helal ,  Simone Sciabola ,  Erik Alphie LaChapelle ,  Joseph Michael Young ,  Patrick Robert Verhoest

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents R1, R3, R6, R7, and b are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, and methods of preparing the compounds.

公开(公告)号：US20160039828A1

公开(公告)日：2016-02-11

申请号：US14817606

申请日：2015-08-04

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Patrick Robert Verhoest ,  Nandini Chaturbhai Patel ,  Matthew Merrill Hayward ,  Christopher John Helal ,  Simone Sciabola ,  Erik Alphie LaChapelle ,  Joseph Michael Young

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents R1, R3, R6, R7, and b are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, and methods of preparing the compounds.

Abstract translation: 本发明涉及式I化合物或其药学上可接受的盐，其中取代基R 1，R 3，R 6，R 7和b如本文所定义。 本发明还涉及包含化合物的药物组合物，使用该化合物的治疗方法，以及制备化合物的方法。

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：US20140088081A1

公开(公告)日：2014-03-27

申请号：US14091404

申请日：2013-11-27

Applicant: Pfizer Inc.

Inventor： Michelle Marie Claffey ,  Christopher John Helal ,  Patrick Robert Verhoest

IPC: C07D487/04 ,  A61K31/444 ,  A61K31/473 ,  A61K31/55 ,  A61K31/13 ,  A61K31/27 ,  A61K31/519 ,  A61K31/445

CPC classification number: C07D487/04 ,  A61K31/13 ,  A61K31/27 ,  A61K31/444 ,  A61K31/445 ,  A61K31/473 ,  A61K31/519 ,  A61K31/55

Abstract: The invention provides PDE9-inhibiting compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, A, and n are as defined herein. Pharmaceutical compositions containing the compounds of Formula I, and uses thereof in treating neurodegenerative and cognitive disorders, such as Alzheimer's disease and schizophrenia, are also provided.

Abstract translation: 本发明提供抑制PDE9的式（I）化合物及其药学上可接受的盐，其中R 1，R 2，R 3，A和n如本文所定义。 还提供了含有式I化合物的药物组合物及其用于治疗神经变性和认知障碍如阿尔茨海默病和精神分裂症的用途。

公开(公告)号：US20140066622A1

公开(公告)日：2014-03-06

申请号：US14069640

申请日：2013-11-01

Applicant: Pfizer Inc.

Inventor： Christopher John Helal ,  Thomas Allen Chappie ,  John Michael Humphrey ,  Patrick Robert Verhoest ,  Eddie Yang

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention relates to compounds of the Formula and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as a method for the treatment of a disease or condition selected from the group consisting of central nervous system disorders, cognitive disorders, schizophrenia, dementia and other disorders in a mammal.

Abstract translation: 本发明涉及式的化合物及其药学上可接受的盐，其制备方法，用于制备的中间体和含有这些化合物的组合物以及这些化合物的用途，作为治疗疾病的方法或 选自哺乳动物中的中枢神经系统疾病，认知障碍，精神分裂症，痴呆等紊乱的病症。

公开(公告)号：US11472805B2

公开(公告)日：2022-10-18

申请号：US15736942

申请日：2016-06-09

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Nandini Chaturbhai Patel ,  Patrick Robert Verhoest ,  Christopher John Helal ,  Simone Sciabola ,  Erik Alphie LaChapelle ,  Travis T. Wager ,  Ramalakshmi Yegna Chandrasekaran

IPC: C07D471/14 ,  C07D491/147 ,  C07D491/22 ,  C07D513/14 ,  C07D519/00 ,  C07D487/04 ,  C07D487/14 ,  C07D498/22 ,  C07D471/22

Abstract: The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents A, R1, R2, R3a, R3b, R4a, R4b and n are as defined herein. The inventions also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds and methods of preparing the compounds.

公开(公告)号：US20210024497A1

公开(公告)日：2021-01-28

申请号：US17040479

申请日：2019-03-25

Applicant: Pfizer Inc.

Inventor： Lei Zhang ,  Erik Alphie LaChapelle ,  Christopher Ryan Butler ,  Natasha Mariam Kablaoui ,  Michael Aaron Brodney ,  Laura Ann McAllister ,  Qingyi Yang ,  Christopher John Helal ,  Damien Webb

IPC: C07D401/14 ,  C07D401/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/107 ,  C07D413/14

Abstract: The present invention provides, in part, compounds of Formula I: or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: X1, X2, R1, R2, m and n are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, Parkinson's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

公开(公告)号：US10858373B2

公开(公告)日：2020-12-08

申请号：US16429678

申请日：2019-06-03

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Laura Ann McAllister ,  Christopher John Helal ,  Steven Victor O'Neil ,  Patrick Robert Verhoest

IPC: C07D513/10 ,  A61P37/00 ,  C07D401/12 ,  C07D471/10 ,  C07D493/10 ,  C07D498/10 ,  A61P3/00 ,  A61P9/00 ,  A61P25/00 ,  A61P35/00 ,  C07D221/20

Abstract: The present invention provides, in part, heterocyclic spiro compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.