公开(公告)号：US20230192654A1

公开(公告)日：2023-06-22

申请号：US17969479

申请日：2022-10-19

申请人： PFIZER, INC.

发明人： 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分类号： C07D401/14 ,  C07D401/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/107

CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/107

摘要： 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

申请人： Pfizer Inc.

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

IPC分类号： C07D471/20 ,  C07D519/00

摘要： 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：US11452711B2

公开(公告)日：2022-09-27

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： C07D403/12 ,  A61K31/403 ,  A61P31/14 ,  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：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：US11203594B2

公开(公告)日：2021-12-21

申请号：US16849329

申请日：2020-04-15

申请人： Pfizer Inc.

发明人： Samit Kumar Bhattacharya ,  Douglas Carl Behenna ,  Kimberly O. Cameron ,  Ping Chen ,  John M. Curto ,  Kevin Daniel Freeman-Cook ,  Mehran Jalaie ,  Robert Steven Kania ,  Yajing Lian ,  Sajiv Krishnan Nair ,  Cynthia Louise Palmer ,  Martin Youngjin Pettersson ,  Eugene Yuanjin Rui ,  Matthew Sammons ,  Qingyi Yang ,  Liying Zhang

IPC分类号： C07D471/04 ,  A61P9/12

摘要： This invention relates to compounds of general Formula I in which A, R1, R2, R3 and R4 are as defined herein, and the pharmaceutically acceptable salts thereof; to pharmaceutical compositions comprising such compounds and salts; to methods of using such compounds, salts and compositions for treating pulmonary hypertension and related diseases, like pulmonary arterial hypertension; to methods of using such compounds, salts and compositions for treating abnormal cell growth, such as cancer; and to processes to make such compounds, salts and compositions.

公开(公告)号：US20230120254A1

公开(公告)日：2023-04-20

申请号：US17932151

申请日：2022-09-14

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 ,  A61K31/427 ,  C07D403/12 ,  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：US20220062232A1

公开(公告)日：2022-03-03

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

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：US20200331909A1

公开(公告)日：2020-10-22

申请号：US16849329

申请日：2020-04-15

申请人： Pfizer Inc.

发明人： Samit Kumar Bhattacharya ,  Douglas Carl Behenna ,  Kimberly O. Cameron ,  Ping Chen ,  John M. Curto ,  Kevin Daniel Freeman-Cook ,  Mehran Jalaie ,  Robert Steven Kania ,  Yajing Lian ,  Sajiv Krishnan Nair ,  Cynthia Louise Palmer ,  Martin Youngjin Pettersson ,  Eugene Yuanjin Rui ,  Matthew Sammons ,  Qingyi Yang ,  Liying Zhang

IPC分类号： C07D471/04 ,  A61P9/12

摘要： This invention relates to compounds of general Formula I in which A, R1, R2, R3 and R4 are as defined herein, and the pharmaceutically acceptable salts thereof; to pharmaceutical compositions comprising such compounds and salts; to methods of using such compounds, salts and compositions for treating pulmonary hypertension and related diseases, like pulmonary arterial hypertension; to methods of using such compounds, salts and compositions for treating abnormal cell growth, such as cancer; and to processes to make such compounds, salts and compositions.

公开(公告)号：US20230339930A1

公开(公告)日：2023-10-26

申请号：US18004996

申请日：2021-07-07

申请人： Pfizer Inc.

发明人： Dafydd Rhys Owen ,  Martin Youngjin Pettersson ,  Matthew Richard Reese ,  Matthew Forrest Sammons ,  Jamison Bryce Tuttle ,  Qingyi Yang

IPC分类号： C07D417/14 ,  A61P31/14

CPC分类号： C07D417/14 ,  A61P31/14

摘要： The invention relates to compounds of Formula I




wherein R1, R2, p, m, A, Z1, Z2, Z3 and Z4 are as defined herein, pharmaceutical compositions comprising the compounds, methods of treating COVID-19 in a patient by administering therapeutically effective amounts of the compounds, and methods of inhibiting or preventing replication of SARS-CoV-2 with the compounds.

公开(公告)号：US20230174532A1

公开(公告)日：2023-06-08

申请号：US18162052

申请日：2023-01-31

申请人： Pfizer Inc.

发明人： Christopher Ryan BUTLER ,  Michelle Renee GARNSEY ,  Kevin Alexander OGILVIE ,  Jana POLIVKOVA ,  Matthew Forrest SAMMONS ,  Aaron Christopher SMITH ,  Qingyi Yang

IPC分类号： C07D471/20 ,  C07D519/00

CPC分类号： C07D471/20 ,  C07D519/00 ,  C07B2200/13

摘要： Described herein are methods of treating MC4R-related conditions, diseases, or disorders by administering compounds of Formula I:




or their pharmaceutically acceptable salts, wherein R1, R2, R3, X1, Y1, Y2, Y3, Y4 and Y5 are defined herein. Such conditions, diseases, or disorders include cachexia, anorexia, or anorexia nervosa.