公开(公告)号：US20240245673A1

公开(公告)日：2024-07-25

申请号：US18532424

申请日：2023-12-07

Applicant: Pfizer Inc.

Inventor： James Matthew Frick ,  Michelle Renee Garnsey ,  Brian Stephen Gerstenberger ,  Xinjun Hou ,  Magdalena Korczynska ,  Alpha Albert Lee ,  Luong Tien Nguyen ,  Usa Reilly ,  Matthew Christopher Robinson ,  Alexandria Paige Taylor ,  Thomas Reynold Vargo ,  Lei Zhang

IPC: A61K31/4709 ,  A61K31/415 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D215/38 ,  C07D231/12 ,  C07D249/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D495/04

CPC classification number: A61K31/4709 ,  A61K31/415 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D215/38 ,  C07D231/12 ,  C07D249/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D495/04

Abstract: The invention relates to compounds of Formula (I)




and pharmaceutically acceptable salts thereof as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The compounds of Formula (I) may inhibit the activity of papain-like protease (PLpro) and may be useful in the treatment of viral infections, in particular viral infections associated with PLpro activity and/or expression such as coronaviruses infections.

公开(公告)号：US20240238425A1

公开(公告)日：2024-07-18

申请号：US18541015

申请日：2023-12-15

Applicant: Pfizer Inc.

Inventor： Jan Antoinette Cusi Romero Adams ,  Yotam Ashkenazi ,  Matthew Frank Brown ,  Jason Kenneth Dutra ,  Michelle Renee Garnsey ,  Xinjun Hou ,  Jisun Lee ,  Yajing Lian ,  Deane Milford Nason, II ,  Steven Victor O'Neil ,  Amanda Brooke Pecora ,  Alistair Dean Richardson ,  Matthew Forrest Sammons ,  Yang Wang ,  Ann Sorrentino Wright ,  Jun Xiao ,  Lei Zhang ,  Liying Zhang

IPC: A61K47/55 ,  A61K45/06

CPC classification number: A61K47/55 ,  A61K45/06

Abstract: Described herein are 3-fluoro-4-hydroxybenzamide-containing inhibitors and/or degraders, and pharmaceutical compositions containing 3-fluoro-hydroxybenzamide-containing inhibitors and/or degraders. In some embodiments, the 3-fluoro-4-hydroxybenzamide-containing compounds of the disclosure can be used to treat a condition, for example, nonalcoholic fatty liver disease and nonalcoholic steatohepatitis.

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：US11065249B2

公开(公告)日：2021-07-20

申请号：US17090619

申请日：2020-11-05

Applicant: Pfizer Inc.

Inventor： David James Edmonds ,  Kevin James Filipski ,  Kentaro Futatsugi ,  Michelle Renee Garnsey ,  Jack Chang Hung Lee ,  Daniel Jonathan Smaltz

IPC: A61K31/506 ,  A61P3/06 ,  A61K31/155 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/7048 ,  A61K45/06 ,  C07D401/14

Abstract: Described herein are compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are defined herein, their use as diacylglycerol acyltransferase 2 (DGAT2) inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, NASH.

公开(公告)号：US11471458B2

公开(公告)日：2022-10-18

申请号：US17062982

申请日：2020-10-05

Applicant: Pfizer Inc.

Inventor： David James Edmonds ,  Kevin James Filipski ,  Kentaro Futatsugi ,  Michelle Renee Garnsey ,  Jack Chang Hung Lee ,  Daniel Jonathan Smaltz

IPC: A61K31/506 ,  A61P3/06 ,  A61K31/155 ,  A61K31/4545 ,  C07D401/14 ,  A61K31/4985 ,  A61K31/7048 ,  A61K45/06

Abstract: Described herein are compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are defined herein, their use as diacylglycerol acyltransferase 2 (DGAT2) inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, NASH.

公开(公告)号：US20210100798A1

公开(公告)日：2021-04-08

申请号：US17090619

申请日：2020-11-05

Applicant: Pfizer Inc.

Inventor： David James Edmonds ,  Kevin James Filipski ,  Kentaro Futatsugi ,  Michelle Renee Garnsey ,  Jack Chang Hung Lee ,  Daniel Jonathan Smaltz

IPC: A61K31/506 ,  A61K31/4545 ,  A61K31/155 ,  A61K31/7048 ,  A61K31/4985 ,  A61P3/06 ,  C07D401/14 ,  A61K45/06

Abstract: Described herein are compounds of Formula (1) wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are defined herein, their use as diacylglycerol acyltransferase 2 (DGAT2) inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, NASH.

公开(公告)号：US20210100796A1

公开(公告)日：2021-04-08

申请号：US17062982

申请日：2020-10-05

Applicant: Pfizer Inc.

Inventor： David James Edmonds ,  Kevin James Filipski ,  Kentaro Futatsugi ,  Michelle Renee Garnsey ,  Jack Chang Hung Lee ,  Daniel Jonathan Smaltz

IPC: A61K31/506 ,  C07D401/14 ,  A61K45/06 ,  A61P3/06 ,  A61K31/155 ,  A61K31/4985 ,  A61K31/7048 ,  A61K31/4545

Abstract: Described herein are compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are defined herein, their use as diacylglycerol acyltransferase 2 (DGAT2) inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, NASH.

公开(公告)号：US12187727B2

公开(公告)日：2025-01-07

申请号：US18162052

申请日：2023-01-31

Applicant: Pfizer Inc.

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

IPC: A61K31/438 ,  A61P1/08 ,  A61P3/04 ,  A61P19/00 ,  A61P21/00 ,  A61P29/00 ,  C07D471/20 ,  C07D519/00

Abstract: 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.

公开(公告)号：US20240150334A1

公开(公告)日：2024-05-09

申请号：US18482129

申请日：2023-10-06

Applicant: Pfizer Inc.

Inventor： Jan Antoinette Cusi Romero Adams ,  Bruce Michael Bechle ,  Jason Kenneth Dutra ,  Michelle Renee Garnsey ,  Xinjun Hou ,  Jisun Lee ,  Deane Milford Nason, II ,  Steven Victor O'Neil ,  Danica Antonia Rankic ,  Yang Wang ,  Ann Sorrentino Wright ,  Lei Zhang ,  Liying Zhang ,  David James Edmonds

IPC: C07D413/04 ,  C07D231/56 ,  C07D263/56 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D498/04 ,  C07D513/04

CPC classification number: C07D413/04 ,  C07D231/56 ,  C07D263/56 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D498/04 ,  C07D513/04

Abstract: Described herein are compounds of Formula I,




wherein the variables are defined herein, their use as HSD17B13 inhibitors and/or degraders, pharmaceutical compositions containing such compounds and their use to treat, for example, NAFLD and NASH.

公开(公告)号：US20170073343A1

公开(公告)日：2017-03-16

申请号：US15262112

申请日：2016-09-12

Applicant: Pfizer Inc.

Inventor： Paul Galatsis ,  Jaclyn Louise Henderson ,  Bethany Lyn Kormos ,  Ravi G. Kurumbail ,  Matthew Richard Reese ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest ,  Travis T. Wager ,  Martin Youngjin Pettersson ,  Michelle Renee Garnsey

IPC: C07D471/04 ,  C07D471/14 ,  C07D519/00

CPC classification number: A61K31/435 ,  A61K31/4745 ,  C07D215/38 ,  C07D215/42 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00

Abstract: The present invention provides novel imidazo[4,5-c]quinoline and imidazo[4,5-c][1,5]naphthyridine derivatives of Formula (I), and the pharmaceutically acceptable salts thereof wherein R1, R1a, R1b, R2, R4, R5, R6, X and Z are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula (I) and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.

Abstract translation: 其中R1，R1a，R1b，R2，R4，R5，R6，X和Z如说明书中所定义。 本发明还涉及包含式（I）化合物的药物组合物，以及该化合物在治疗与LRRK2相关的疾病中的应用，例如包括帕金森病或阿尔茨海默氏病，癌症，克罗恩病或麻风病的神经变性疾病。