公开(公告)号：US09200000B2

公开(公告)日：2015-12-01

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：US09156845B2

公开(公告)日：2015-10-13

申请号：US13928696

申请日：2013-06-27

Applicant: Pfizer Inc.

Inventor： Paul Galatsis ,  Matthew Merrill Hayward ,  Bethany Lyn Kormos ,  Travis T. Wager ,  Lei Zhang ,  Antonia Friederike Stepan ,  Jaclyn Louise Henderson ,  Ravi G. Kurumbail ,  Patrick Robert Verhoest

IPC: A61K31/519 ,  C07D207/18 ,  C07D487/04 ,  C07D519/00

CPC classification number: A61K31/5377 ,  C07D487/04 ,  C07D519/00

Abstract: The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4 and R5 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.

Abstract translation: 本发明提供了式I的新的4,5-二取代的-7H-吡咯并[2,3-d]嘧啶衍生物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4和R 5如说明书中所定义。 本发明还涉及包含式I化合物的药物组合物，以及该化合物在治疗与LRRK2相关的疾病中的应用，例如包括帕金森病或阿尔茨海默病，神经变性疾病或克罗恩病或麻风病的神经变性疾病。

公开(公告)号：US20150274721A1

公开(公告)日：2015-10-01

申请号：US14670746

申请日：2015-03-27

Applicant: Pfizer Inc.

Inventor： Martin Youngjin Pettersson ,  Christopher William am Ende ,  John Michael Humphrey ,  Douglas Scott Johnson ,  Gregory Wayne Kauffman ,  Danica Antonia Rankic ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I wherein X, R1, R2a, R2b, R4a, R4b, R5a, R5b, R6, R7, y and z are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract translation: 公开了化合物的化合物和药学上可接受的盐，其中化合物具有式I的结构，其中X，R1，R2a，R2b，R4a，R4b，R5a，R5b，R6，R7，y和z如本说明书中所定义 。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。

公开(公告)号：US20150175603A1

公开(公告)日：2015-06-25

申请号：US14405103

申请日：2013-06-03

Applicant: PFIZER INC.

Inventor： Amy Beth Dounay ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest

IPC: C07D471/14 ,  C07D471/06

CPC classification number: C07D471/14 ,  C07D471/04 ,  C07D471/06 ,  C07D498/04

Abstract: Compounds of Formula (I), wherein R1, R2, X1, Y1, Z1, and Z2 are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.

Abstract translation: 描述了其中R1，R2，X1，Y1，Z1和Z2如本文所定义的式（I）化合物及其药学上可接受的盐可用于治疗与精神分裂症，神经变性和其他精神病学，神经变性和 /或哺乳动物包括人类的神经障碍。

公开(公告)号：US08933095B2

公开(公告)日：2015-01-13

申请号：US14068707

申请日：2013-10-31

Applicant: Pfizer Inc.

Inventor： Amy Beth Dounay ,  Laura Ann McAllister ,  Vinod Dipak Parikh ,  Suobao Rong ,  Patrick Robert Verhoest

IPC: C07D235/02 ,  C07D403/00 ,  C07D231/56 ,  C07D487/00 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: Compounds of Formula I: wherein X, Y, Z, R1, R2, R3, R4 are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.

Abstract translation: 式I化合物：其中X，Y，Z，R 1，R 2，R 3，R 4如本文所定义，及其药学上可接受的盐被描述为可用于治疗与精神分裂症和其他精神病学，神经变性和/ 或哺乳动物包括人类的神经障碍。

公开(公告)号：US20250099424A1

公开(公告)日：2025-03-27

申请号：US18917336

申请日：2024-10-16

Applicant: Pfizer Inc.

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

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

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：US12049465B2

公开(公告)日：2024-07-30

申请号：US17886807

申请日：2022-08-12

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

CPC classification number: C07D471/14 ,  C07D471/22 ,  C07D487/04 ,  C07D487/14 ,  C07D491/147 ,  C07D491/22 ,  C07D498/22 ,  C07D513/14 ,  C07D519/00

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：US20230002386A1

公开(公告)日：2023-01-05

申请号：US17886807

申请日：2022-08-12

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：US11452711B2

公开(公告)日：2022-09-27

申请号：US17660270

申请日：2022-04-22

Applicant: Pfizer Inc.

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

IPC: C07D403/12 ,  A61K31/403 ,  A61P31/14 ,  A61K31/427 ,  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：US11312713B2

公开(公告)日：2022-04-26

申请号：US16492558

申请日：2018-03-06

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Thomas Allen Chappie ,  Jinshan Michael Chen ,  Jotham Wadsworth Coe ,  Karen Jean Coffman ,  Paul Galatsis ,  Michelle Renee Garnsey ,  Christopher John Helal ,  Jaclyn Louise Henderson ,  Bethany Lyn Kormos ,  Ravi G. Kurumbail ,  Luis Angel Martinez-Alsina ,  Martin Youngjin Pettersson ,  Matthew Richard Reese ,  Colin Richard Rose ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest ,  Travis T. Wager ,  Joseph Scott Warmus ,  Yuan Zhang

IPC: C07D471/04

Abstract: The present invention provides novel imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof I wherein R1, R2 and R3 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.