公开(公告)号：US20160002264A1

公开(公告)日：2016-01-07

申请号：US14653549

申请日：2013-12-04

Applicant: PFIZER INC.

Inventor： Michael Aaron Brodney ,  Brian Thomas O'Neill ,  Christopher Ryan Butler ,  Erik Alphie LaChapelle

IPC: C07D513/04

CPC classification number: C07D513/04

Abstract: The present invention provides compounds of formula I, wherein the variables R1, R2, R5 and b are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract translation: 本发明提供式I化合物，其中变量R1，R2，R5和b如说明书中所定义。 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：US20150239908A1

公开(公告)日：2015-08-27

申请号：US14429215

申请日：2013-09-09

Applicant: PFIZER INC.

Inventor： Michael Aaron Brodney ,  Elizabeth Mary Beck ,  Christopher Ryan Butler ,  Jennifer Elizabeth Davoren

IPC: C07D513/04

CPC classification number: C07D513/04

Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, 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，互变异构体和药学上可接受的盐，其中化合物具有如说明书中定义的式I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：US09045499B2

公开(公告)日：2015-06-02

申请号：US14464935

申请日：2014-08-21

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Elizabeth Mary Beck ,  Jennifer Elizabeth Davoren ,  Erik Alphie LaChapelle ,  Brian Thomas O'Neill

IPC: C07D513/04 ,  A61K31/542

CPC classification number: A61K31/542 ,  C07D513/04

Abstract: 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 and R2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract translation: 本发明涉及所公开的化合物的化合物，互变异构体和药学上可接受的盐，其中化合物具有式I的结构，并且变量R1和R2如说明书中所定义。 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：US20140364426A1

公开(公告)日：2014-12-11

申请号：US14464935

申请日：2014-08-21

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Elizabeth Mary Beck ,  Jennifer Elizabeth Davoren ,  Erik Alphie LaChapelle ,  Brian Thomas O'Neill

IPC: C07D513/04

CPC classification number: A61K31/542 ,  C07D513/04

Abstract: 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 and R2 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：US20230192654A1

公开(公告)日：2023-06-22

申请号：US17969479

申请日：2022-10-19

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 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/107

CPC classification number: C07D401/14 ,  C07D401/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/107

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：US20230019853A1

公开(公告)日：2023-01-19

申请号：US17341877

申请日：2021-06-08

Applicant: Pfizer Inc.

Inventor： Christopher Ryan Butler ,  Michelle Renee Garnsey ,  Kevin Alexander Ogilvie ,  Jana Polivkova ,  Matthew Forrest Sammons ,  Aaron Christopher Smith ,  Qingyi Yang

IPC: C07D471/20 ,  C07D519/00

Abstract: Described herein are compounds of Formula I: and their pharmaceutically acceptable salts, wherein R1, R2, R3, X1, Y1, Y2, Y3, Y4 and Y5 are defined herein; their use as MC4R antagonists; pharmaceutical compositions containing such compounds and salts; the use of such compounds and salts to treat, for example, cachexia, anorexia, or anorexia nervosa; and intermediates and processes for preparing such compounds and salts.

公开(公告)号：US11198692B2

公开(公告)日：2021-12-14

申请号：US16625202

申请日：2018-06-14

Applicant: Pfizer Inc.

Inventor： Elizabeth Mary Beck ,  Michael Aaron Brodney ,  Matthew Frank Brown ,  Christopher Ryan Butler ,  Adam Matthew Gilbert ,  Erik Alphie Lachapelle ,  Laura Ann McAllister ,  Daniel Paul Uccello ,  Lei Zhang

IPC: C07D471/04

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: (R1)a, (R2)b, (R3)c, L, A, and E 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, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

公开(公告)号：US10253042B2

公开(公告)日：2019-04-09

申请号：US15678511

申请日：2017-08-16

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Lei Zhang ,  Brian Thomas O'Neill

IPC: A01N43/00 ,  A61K31/553 ,  C07D498/04 ,  C07D498/10

Abstract: 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, wherein the variables R1, R2, R3, R4 and X 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：US20180002331A1

公开(公告)日：2018-01-04

申请号：US15637071

申请日：2017-06-29

Applicant: Pfizer Inc.

Inventor： Lei Zhang ,  Christopher Ryan Butler ,  Elizabeth Mary Beck ,  Michael Aaron Brodney ,  Matthew Frank Brown ,  Laura Ann McAllister ,  Erik Alphie LaChapelle ,  Adam Matthew Gilbert

IPC: C07D471/04

CPC classification number: C07D471/04

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: R1, R2, L, A, and E 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, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

公开(公告)号：US20170304312A1

公开(公告)日：2017-10-26

申请号：US15629215

申请日：2017-06-21

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Elizabeth Mary Beck ,  Christopher Ryan Butler ,  Lei Zhang ,  Brian Thomas O'Neill ,  Gabriela Barreiro ,  Erik Alphie LaChapelle ,  Bruce Nelsen Rogers

IPC: A61K31/542

CPC classification number: A61K31/542 ,  C07D513/04 ,  C07D519/00

Abstract: 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 variable R1 is as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.