公开(公告)号：US20210355117A1

公开(公告)日：2021-11-18

申请号：US16492558

申请日：2018-03-06

Applicant: Pfizer Inc.

Inventor： Michael Aaron BRODNEY ,  Thomas Allen CHAPPIE ,  Jinshan Michael CHEN ,  Jotham Wadsworth COE ,  Karen Jean COFFMAN ,  Paul GALATSIS ,  Michelle Renee GARNSEY ,  Christopher John HELAL ,  Jaclyn Louise Henderson ,  Bethany Lyn KORMOS ,  Ravi G. KURUMBAIL ,  Luis Angel MARTINEZ-ALSINA ,  Martin Youngjin PETTERSSON ,  Matthew Richard REESE ,  Colin Richard ROSE ,  Antonia Friederike STEPAN ,  Patrick Robert VERHOEST ,  Travis T. WAGER ,  Joseph Scott WARMUS ,  Yuan ZHANG

IPC: C07D471/04

Abstract: The present invention provides novel imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof I wherein R1, R2 and R3 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.

公开(公告)号：US20170252352A1

公开(公告)日：2017-09-07

申请号：US15314574

申请日：2015-05-18

Applicant: Pfizer Inc.

Inventor： Eugene Lvovich Piatnitski CHEKLER ,  Adam Matthew GILBERT ,  Rayomand Jal UNWALLA ,  Patrick Robert VERHOEST ,  James Thomas ANDERSON

IPC: A61K31/549 ,  A61K31/433 ,  A61K31/472 ,  A61K45/06 ,  A61K31/397 ,  A61K31/451 ,  A61K31/402 ,  A61K31/4725 ,  A61K31/277

CPC classification number: A61K31/549 ,  A61K31/277 ,  A61K31/397 ,  A61K31/402 ,  A61K31/433 ,  A61K31/451 ,  A61K31/472 ,  A61K31/4725 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention relates to a compound of Formula 1, 2 or 3: I II III wherein A is N or —CR0—, where R0 is hydrogen, C1-C6 linear or branched chain alkyl, etc., Z is —CRe—, or, —N—, where Re is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R1 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R2 are independently hydrogen or C1-C6 linear or branched chain alkyl; R3 and R4 are independently hydrogen, C1C6 linear or branched chain alkyl, etc.; R5 and R6 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; R8 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R9 and R10 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; Q is —CO—, —(CH2)q—, —(CHRs)q—, or —(CRsRt)q—, where Rs and Rt are independently C1-C6 linear or branched chain alkyl, aryl, alkylaryl, heteroaryl or alkylheteroaryl; where q is 0, 1, 2, or 3; and, where n is 0, 1, 2, 3, 4 or 5; or, a pharmaceutically acceptable salt thereof, for the treatment of certain diseases, particularly those affected or mediated by the androgen receptor; to combinations comprising such compounds with a second pharmaceutically active ingredient; to compositions containing such combinations; and to such combinations for the treatment of various diseases, particularly, those affected or mediated by the androgen receptor.

公开(公告)号：US20160045508A1

公开(公告)日：2016-02-18

申请号：US14822265

申请日：2015-08-10

Applicant: Pfizer Inc.

Inventor： Michael L. VAZQUEZ ,  Neelu KAILA ,  Jamison B. TUTTLE ,  Patrick Robert VERHOEST ,  Matthew R. REESE ,  Karen J. COFFMAN ,  Tarek SAMAD ,  James M. DUERR ,  Simone SCIABOLA ,  Mihir D. PARIKH

IPC: A61K31/519 ,  A61K31/5377 ,  C07D519/00 ,  A61K31/5386 ,  A61K45/06 ,  C07D487/04

CPC classification number: A61K31/519 ,  A61K31/5377 ,  A61K31/5386 ,  A61K45/06 ,  C07D487/04 ,  C07D491/044 ,  C07D491/052 ,  C07D498/08 ,  C07D519/00

Abstract: Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing them, and therapeutic uses thereof.

Abstract translation: 本文描述的是吡咯并[2,3-d]嘧啶衍生物，它们用作Janus Kinase（JAK）抑制剂，含有它们的药物组合物及其治疗用途。