Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylam ides and analogues thereof, having the structure: or a pharmaceutically acceptable salt thereof, as set forth in the Description. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.
Type:
Grant
Filed:
March 1, 2017
Date of Patent:
September 7, 2021
Assignee:
Pfizer Inc.
Inventors:
Atli Thorarensen, Matthew Frank Brown, Agustin Casimiro-Garcia, Ye Che, Jotham Wadsworth Coe, Mark Edward Flanagan, Adam Matthew Gilbert, Matthew Merrill Hayward, Jonathan David Langille, Justin Ian Montgomery, Jean-Baptiste Telliez, Rayomand Jal Unwalla, John I. Trujillo
Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylamides and analogues thereof, having the structure: or a pharmaceutically acceptable salt or solvate thereof, or an enantiomer or diastereomer thereof, as set forth in the Description. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.
Type:
Grant
Filed:
December 3, 2014
Date of Patent:
April 11, 2017
Assignee:
Pfizer Inc.
Inventors:
Atli Thorarensen, Matthew Frank Brown, Agustin Casimiro-Garcia, Ye Che, Jotham Wadsworth Coe, Mark Edward Flanagan, Adam Matthew Gilbert, Matthew Merrill Hayward, Jonathan David Langille, Justin Ian Montgomery, Jean-Baptiste Telliez, Rayomand Jal Unwalla, John I. Trujillo
Abstract: Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula (I) and Formula (II) have the following structures: (I); (II). Intermediates (V) are also claimed.
Type:
Grant
Filed:
November 3, 2017
Date of Patent:
August 11, 2020
Assignee:
AMGEN INC.
Inventors:
Matthew Brown, Ning Chen, Xiaoqi Chen, Yinhong Chen, Alan C. Cheng, Richard V. Connors, Jeffrey Deignan, Paul John Dransfield, Xiaohui Du, Zice Fu, James S. Harvey, Julie Anne Heath, Lars V. Heumann, Jonathan Houze, Frank Kayser, Aarif Yusuf Khakoo, David j. Kopecky, Su-Jen Lai, Zhihua Ma, Julio C. Medina, Jeffrey T. Mihalic, Steven H. Olson, Vatee Pattaropong, Gayathri Swaminath, Xiaodong Wang, Malgorzata Wanska, Wen-Chen Yeh
Abstract: The present invention relates to compounds of the formula I 1
Type:
Application
Filed:
October 16, 2003
Publication date:
May 13, 2004
Applicant:
Pfizer Inc
Inventors:
Laura C. Blumberg, Matthew F. Brown, Anderson S. Gaweco, Ronald P. Gladue, Matthew M. Hayward, Gregory D. Lundquist, Christopher S. Poss, Andrei Shavnya
Abstract: The invention relates to compounds of formula I and to pharmaceutically acceptable salts, prodrugs, solvates or hydrates thereof. This invention also relates to a method of using such compounds in the treatment of hyperproliferative diseases and autoimmune diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
Type:
Application
Filed:
November 7, 2008
Publication date:
September 10, 2009
Inventors:
Samit K. Bhattacharya, Matthew F. Brown, Peter H. Dorff, Susan D. LaGreca, John W. Mickelson, Joseph A. Cornicelli, David L. Brown, Rex Jennings, John K. Walker, Rita Huff, Joseph W. Strohbach, Robert J. Maguire
Abstract: The present invention relates to compounds of the formula I and the pharmaceutically acceptable forms thereof; wherein X, Y, a, b, c, d, R1, R2, R3, R4 and R5 are as defined herein. Moreover, the present invention is also directed at pharmaceutical compositions comprising a compound of the formula I and a pharmaceutically acceptable carrier. Furthermore, the present invention is directed at methods of using the herein described compounds and compositions for treating or preventing a disorder or condition that can be treated or prevented by antagonizing the CCR1 receptor in a mammal.
Type:
Grant
Filed:
October 18, 2002
Date of Patent:
August 29, 2006
Inventors:
Laura C. Blumberg, Matthew F. Brown, Matthew M. Hayward, Gregory D. Lundquist, Christopher S. Poss, Andrei Shavnya
Abstract: The invention relates to compounds of formula I and to pharmaceutically acceptable salts, prodrugs, solvates or hydrates thereof. This invention also relates to a method of using such compounds in the treatment of hyperproliferative diseases and autoimmune diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
Type:
Application
Filed:
May 13, 2010
Publication date:
September 16, 2010
Inventors:
Samit K. Bhattacharya, Matthew F. Brown, Peter H. Dorff, Susan D. LaGreca, John W. Mickelson, Joseph A. Cornicelli, David L. Brown, Jennings Rex, John K. Walker, Rita Huff, Joseph W. Strohbach, Robert J. Maguire
Abstract: Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use.
Type:
Application
Filed:
August 6, 2020
Publication date:
March 4, 2021
Inventors:
Celia Dominguez, John Wityak, Jonathan Bard, Christopher John Brown, Michael Edward Prime, Peter David Johnson, Thomas Martin Krulle, Daniel Clark-Frew, Duane Higgins, Matthew Robert Mills, Richard Waldron Marston, Samuel Coe, Samantha Brown, Sarah Hayes
Abstract: Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use.
Type:
Application
Filed:
October 26, 2018
Publication date:
June 6, 2019
Inventors:
Celia Dominguez, John Wityak, Jonathan Bard, Christopher John Brown, Michael Edward Prime, Peter David Johnson, Thomas Martin Krulle, Daniel Clark-Frew, Duane Higgins, Matthew Robert Mills, Richard Waldron Marston, Samuel Coe, Samantha Brown, Sarah Hayes
Abstract: Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use.
Type:
Grant
Filed:
August 6, 2020
Date of Patent:
May 31, 2022
Assignee:
CHDI FOUNDATION, INC.
Inventors:
Celia Dominguez, John Wityak, Jonathan Bard, Christopher John Brown, Michael Edward Prime, Peter David Johnson, Thomas Martin Krulle, Daniel Clark-Frew, Duane Higgins, Matthew Robert Mills, Richard Waldron Marston, Samuel Coe, Samantha Brown, Sarah Hayes
Abstract: Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use.
Type:
Grant
Filed:
October 26, 2018
Date of Patent:
September 8, 2020
Assignee:
CHDI Foundation, Inc.
Inventors:
Celia Dominguez, John Wityak, Jonathan Bard, Christopher John Brown, Michael Edward Prime, Peter David Johnson, Thomas Martin Krulle, Daniel Clark-Frew, Duane Higgins, Matthew Robert Mills, Richard Waldron Marston, Samuel Coe, Samantha Brown, Sarah Hayes
Abstract: Thienopyridone compounds of formula (I): or a salt thereof, pharmaceutical compositions containing such compounds and their use in therapy, in particular in the treatment of diseases or conditions for which a bromodomain inhibitor is indicated.
Type:
Application
Filed:
November 12, 2013
Publication date:
October 13, 2016
Inventors:
Dominique AMANS, Paul BAMBOROUGH, Rino Antonio BIT, John Alexander BROWN, Matthew CAMPBELL, Matthew John LINDON, Tracy Jane SHIPLEY, Natalie Hope THEODOULOU, Christopher Roland WELLAWAY, Susan Marie WESTAWAY
Abstract: Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use
Type:
Grant
Filed:
August 26, 2016
Date of Patent:
November 27, 2018
Assignee:
CHDI Foundation, Inc.
Inventors:
Celia Dominguez, John Wityak, Jonathan Bard, Christopher John Brown, Michael Edward Prime, Peter David Johnson, Thomas Martin Krulle, Daniel Clark-Frew, Duane Higgins, Matthew Robert Mills, Richard Waldron Marston, Samuel Coe, Samantha Brown, Sarah Hayes
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.
Type:
Application
Filed:
February 21, 2023
Publication date:
June 22, 2023
Inventors:
Lei Zhang, Christopher Ryan Butler, Elizabeth Mary Beck, Michael Aaron Brodney, Matthew Frank Brown, Laura Ann McAllister, Erik Alphie LaChapelle, Adam Matthew Gilbert
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.
Type:
Application
Filed:
June 29, 2017
Publication date:
January 4, 2018
Applicant:
Pfizer Inc.
Inventors:
Lei Zhang, Christopher Ryan Butler, Elizabeth Mary Beck, Michael Aaron Brodney, Matthew Frank Brown, Laura Ann McAllister, Erik Alphie LaChapelle, Adam Matthew Gilbert
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.
Type:
Application
Filed:
December 7, 2023
Publication date:
June 13, 2024
Inventors:
Lei Zhang, Christopher Ryan Butler, Elizabeth Mary Beck, Michael Aaron Brodney, Matthew Frank Brown, Laura Ann McAllister, Erik Alphie LaChapelle, Adam Matthew Gilbert
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.
Type:
Application
Filed:
June 1, 2021
Publication date:
October 7, 2021
Inventors:
Lei Zhang, Christopher Ryan Butler, Elizabeth Mary Beck, Michael Aaron Brodney, Matthew Frank Brown, Laura Ann McAllister, Erik Alphie LaChapelle, Adam Matthew Gilbert
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.
Type:
Application
Filed:
February 21, 2020
Publication date:
July 2, 2020
Inventors:
Lei Zhang, Christopher Ryan Butler, Elizabeth Mary Beck, Michael Aaron Brodney, Matthew Frank Brown, Laura Ann McAllister, Erik Alphie LaChapelle, Adam Matthew Gilbert