公开(公告)号：US11643412B2

公开(公告)日：2023-05-09

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 ,  A61K31/438 ,  A61P1/08 ,  A61P3/04 ,  A61P19/00 ,  A61P21/00 ,  A61P29/00

CPC classification number: C07D471/20 ,  C07D519/00 ,  C07B2200/13

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：US11524954B2

公开(公告)日：2022-12-13

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 ,  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：US20210309669A1

公开(公告)日：2021-10-07

申请号：US17260247

申请日：2019-07-10

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Laura Ann McAllister ,  Steven Victor O'Neil

IPC: C07D491/107

Abstract: The present invention provides, in part, a compound selected from the group consisting of: 1,1,1,3,3,3-hexafluoropropan-2-yl (3R)-3-{[(cyclopropylmethyl)sulfonyl]amino}-1-oxa-8-azaspiro[4.5]decane-8-carboxylate; 1,1,1,3,3,3-hexafluoropropan-2-yl (3R)-3-[(cyclopropylsulfonyl)amino]-1-oxa-8-azaspiro[4.5]decane-8-carboxylate; 1,1,1,3,3,3-hexafluoropropan-2-yl 3-{[(cyclopropylmethyl)sulfonyl]amino}-1-oxa-9-azaspiro[5.5]undecane-9-carboxylate; 1,1,1,3,3,3-hexafluoropropan-2-yl 3-{[(cyclopropylmethyl)sulfonyl]amino}-1-oxa-9-azaspiro[5.5]undecane-9-carboxylate, ENT-1; and 1,1,1,3,3,3-hexafluoropropan-2-yl 3-{[(cyclopropylmethyl)sulfonyl]amino}-1-oxa-9-azaspiro[5.5]undecane-9-carboxylate, ENT-2, 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, steatohepatitis [e.g. nonalcoholic Steatohepatitis (NASH)], stroke, or cancer.

公开(公告)号：US20200262833A1

公开(公告)日：2020-08-20

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 ,  A61P25/28 ,  A61P25/30 ,  A61P25/18

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：US10723711B2

公开(公告)日：2020-07-28

申请号：US16547037

申请日：2019-08-21

Applicant: PFIZER INC.

Inventor： 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: 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

Abstract: 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：US10112958B2

公开(公告)日：2018-10-30

申请号：US15646572

申请日：2017-07-11

Applicant: Pfizer Inc.

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

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

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, 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：US09428523B2

公开(公告)日：2016-08-30

申请号：US15019342

申请日：2016-02-09

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: C07D513/04 ,  C07D519/00

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.

公开(公告)号：US09198917B2

公开(公告)日：2015-12-01

申请号：US14695920

申请日：2015-04-24

Applicant: Pfizer Inc.

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

IPC: C07D513/04 ,  A61K31/542

CPC classification number: A61K31/542 ,  C07D513/04

Abstract: The present invention provides compounds of Formula I, and the tautomers thereof, and the pharmaceutically acceptable salts of the compounds and tautomers, wherein the compounds have the structure 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：US09192612B2

公开(公告)日：2015-11-24

申请号：US14694288

申请日：2015-04-23

Applicant: Pfizer Inc.

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

IPC: A61K31/542 ,  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：US20150224110A1

公开(公告)日：2015-08-13

申请号：US14694288

申请日：2015-04-23

Applicant: Pfizer Inc.

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

IPC: 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。