公开(公告)号：US20150274721A1

公开(公告)日：2015-10-01

申请号：US14670746

申请日：2015-03-27

申请人： Pfizer Inc.

发明人： 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分类号： C07D471/04

CPC分类号： C07D471/04

摘要： 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.

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

申请人： PFIZER INC.

发明人： Amy Beth Dounay ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest

IPC分类号： C07D471/14 ,  C07D471/06

CPC分类号： C07D471/14 ,  C07D471/04 ,  C07D471/06 ,  C07D498/04

摘要： 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.

摘要翻译： 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

申请人： Pfizer Inc.

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

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

CPC分类号： C07D471/04 ,  C07D487/04

摘要： 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.

摘要翻译： 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：US20230405002A1

公开(公告)日：2023-12-21

申请号：US17904554

申请日：2021-02-22

申请人： Pfizer Inc.

发明人： Neeta Balkrishan Amin ,  Arthur James Bergman ,  Roberto Arnaldo Calle ,  Robert Gregory Dullea ,  David James Edmonds ,  William Paul Esler ,  Kevin James Filipski ,  James Richard Gosset ,  Albert Myung Kim ,  Jeffrey Allen Pfefferkorn ,  Patrick Robert Verhoest

IPC分类号： A61K31/506 ,  A61K31/4545 ,  A61P1/16 ,  A61P3/04

CPC分类号： A61K31/506 ,  A61K31/4545 ,  A61P1/16 ,  A61P3/04

摘要： Described herein are pharmaceutical compositions comprising 2-{5-[(3-ethoxypyridin-2-yl)oxy]pyridin-3-yl}-N-[(3S,5S)-5-fluoropiperidin-3-yl]pyrimidine-5-carboxamide, or pharmaceutically acceptable salt thereof, for treatment of liver disease and diseases related thereto. Also described are compositions comprising 2-{5-[(3-ethoxypyridin-2-yl)oxy]pyridin-3-yl}-N-[(3S,5S)-5-fluoropiperidin-3-yl]pyrimidine-5-carboxamide, or pharmaceutically acceptable salt thereof and 4-(4-(1-Isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4′-piperidine]-1′-carbonyl)-6-methoxypyridin-2-yl)benzoic acid, or pharmaceutically acceptable salt thereof, for treatment of liver disease and diseases related thereto.

公开(公告)号：US11472805B2

公开(公告)日：2022-10-18

申请号：US15736942

申请日：2016-06-09

申请人： Pfizer Inc.

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

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

摘要： 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：US20220257563A1

公开(公告)日：2022-08-18

申请号：US17660270

申请日：2022-04-22

申请人： Pfizer Inc.

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

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

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：US10858373B2

公开(公告)日：2020-12-08

申请号：US16429678

申请日：2019-06-03

申请人： Pfizer Inc.

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

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

摘要： 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.

公开(公告)号：US10590128B2

公开(公告)日：2020-03-17

申请号：US16069585

申请日：2017-01-09

申请人： Pfizer Inc.

发明人： 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分类号： C07D471/04 ,  A61K31/55 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/22

摘要： 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：US10428034B2

公开(公告)日：2019-10-01

申请号：US15808242

申请日：2017-11-09

申请人： PFIZER INC.

发明人： Christopher Ryan Butler ,  Laura Ann McAllister ,  Elizabeth Mary Beck ,  Michael Aaron Brodney ,  Adam Matthew Gilbert ,  Christopher John Helal ,  Douglas Scott Johnson ,  Justin Ian Montgomery ,  Steven Victor O'Neil ,  Bruce Nelsen Rogers ,  Patrick Robert Verhoest ,  Damien Webb

IPC分类号： C07D295/14 ,  C07D401/14 ,  C07D401/04 ,  C07D403/04 ,  C07D498/10 ,  C07D491/107 ,  C07D401/12 ,  C07D471/10 ,  C07D487/04 ,  C07D211/48 ,  C07D471/08 ,  C07D515/10 ,  C07F9/6561 ,  C07D405/14 ,  C07D413/14 ,  C07D405/12 ,  C07D493/10

摘要： The present invention provides, in part, 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, traumatic brain injury, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.

公开(公告)号：US20190292203A1

公开(公告)日：2019-09-26

申请号：US16429678

申请日：2019-06-03

申请人： Pfizer Inc.

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

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

摘要： 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.