公开(公告)号：US11351149B2

公开(公告)日：2022-06-07

申请号：US17395139

申请日：2021-08-05

申请人： Pfizer Inc.

发明人： 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分类号： C07D403/12 ,  A61K31/403 ,  A61P31/14 ,  A61K31/427

摘要： 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：US09815832B2

公开(公告)日：2017-11-14

申请号：US14804644

申请日：2015-07-21

申请人： Pfizer Inc.

发明人： Thomas Allen Chappie ,  Patrick Robert Verhoest ,  Nandini Chaturbhai Patel ,  Matthew Merrill Hayward

IPC分类号： A61K31/437 ,  C07D471/04

CPC分类号： C07D471/04

摘要： The present invention is directed to compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein.

公开(公告)号：US20170145022A1

公开(公告)日：2017-05-25

申请号：US15426423

申请日：2017-02-07

申请人： Pfizer Inc.

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

IPC分类号： C07D487/04 ,  C07D519/00

CPC分类号： C07D487/04 ,  C07D519/00

摘要： 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：US20170088558A1

公开(公告)日：2017-03-30

申请号：US15272501

申请日：2016-09-22

申请人： Pfizer Inc.

发明人： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Lei Zhang ,  Brian Thomas O'Neill ,  Patrick Robert Verhoest ,  Peter Justin Mikochik ,  John Charles Murray ,  Xinjun Hou

IPC分类号： C07D513/04 ,  C07D513/20 ,  C07D513/10

CPC分类号： C07D513/04 ,  C07D513/10 ,  C07D513/20

摘要： The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variables R1, R2 and R3 are as defined in the specification.Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US20160229847A1

公开(公告)日：2016-08-11

申请号：US15022313

申请日：2014-09-22

申请人： PFIZER INC.

发明人： Martin Youngjin Pettersson ,  Christopher William am Ende ,  Michael Eric Green ,  Douglas Scott Johnson ,  Gregory Wayne Kauffman ,  Christopher William O'Donnell ,  Nandini Chaturbhai Patel ,  Antonia Friederike Stepan ,  Cory Michael Stiff ,  Chakrapani Subramanyam ,  Tuan Phong Tran ,  Patrick Robert Verhoest

IPC分类号： C07D471/04 ,  C07D498/04

CPC分类号： C07D471/04 ,  C07D498/04

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

摘要翻译： 公开了化合物的化合物和药学上可接受的盐，其中所述化合物具有如说明书中定义的式II的结构。 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：US20160039828A1

公开(公告)日：2016-02-11

申请号：US14817606

申请日：2015-08-04

申请人： Pfizer Inc.

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

IPC分类号： C07D487/04 ,  C07D519/00

CPC分类号： C07D487/04 ,  C07D519/00

摘要： 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.

摘要翻译： 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

申请人： Pfizer Inc.

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

IPC分类号： C07D519/00 ,  C07D487/04

CPC分类号： C07D519/00 ,  A61K31/4353 ,  A61K31/53 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

摘要： 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.

摘要翻译： 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

申请人： Pfizer Inc.

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

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

CPC分类号： C07D519/00 ,  A61K31/4353 ,  A61K31/53 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

摘要： 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

申请人： Pfizer Inc.

发明人： Michelle Marie Claffey ,  Christopher John Helal ,  Patrick Robert Verhoest

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

CPC分类号： C07D487/04 ,  A61K31/13 ,  A61K31/27 ,  A61K31/444 ,  A61K31/445 ,  A61K31/473 ,  A61K31/519 ,  A61K31/55

摘要： 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.

摘要翻译： 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

申请人： Pfizer Inc.

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

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： 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.

摘要翻译： 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。