公开(公告)号：US20170247372A1

公开(公告)日：2017-08-31

申请号：US15446500

申请日：2017-03-01

Applicant: Pfizer Inc.

Inventor： 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

IPC: C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D471/08 ,  C07D498/04

CPC classification number: C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylamides and analogues thereof. 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.

公开(公告)号：US09617275B2

公开(公告)日：2017-04-11

申请号：US14820611

申请日：2015-08-07

Applicant: PFIZER INC.

Inventor： Jotham Wadsworth Coe ,  John Arthur Allen ,  Jennifer Elizabeth Davoren ,  Amy Beth Dounay ,  Ivan Viktorovich Efremov ,  David Lawrence Firman Gray ,  Edward Raymond Guilmette ,  Anthony Richard Harris ,  Chris John Helal ,  Jaclyn Louise Henderson ,  Scot Richard Mente ,  Deane Milford Nason ,  Steven Victor O'Neil ,  Chakrapani Subramanyam ,  Wenjian Xu

IPC: C07D491/048 ,  C07D491/04 ,  C07D495/04 ,  C07D519/04 ,  C07D519/00

CPC classification number: A61K31/53 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/519 ,  A61P25/00 ,  A61P25/06 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00 ,  C07D519/04

Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes and intermediates for preparation of; and compositions and uses thereof. The present invention further provides D1 agonists with reduced D1R desensitization, D1 agonists with a reduced β-arrestin recruitment activity relative to Dopamine, D1 agonists interacting significantly with the Ser188 but not significantly with the Ser202 of a D1R when binding to the D1R, D1 agonists interacting less strongly with the Asp103 and interacting less strongly with the Ser198 of a D1R when binding to the D1R, and their uses.

公开(公告)号：US09617258B2

公开(公告)日：2017-04-11

申请号：US14559294

申请日：2014-12-03

Applicant: Pfizer Inc.

Inventor： 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

IPC: A61K31/519 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

CPC classification number: C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

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.

公开(公告)号：US09518052B2

公开(公告)日：2016-12-13

申请号：US14710631

申请日：2015-05-13

Applicant: Pfizer Inc.

Inventor： Jotham Wadsworth Coe ,  Christoph Martin Dehnhardt ,  Peter Jones ,  Yogesh Anil Sabnis ,  Joseph Walter Strohbach ,  Florian Michel Wakenhut ,  Gavin Alistair Whitlock

IPC: C07D471/04 ,  C07D487/04

CPC classification number: A61K31/519 ,  A61K31/437 ,  A61K31/4725 ,  C07D471/04 ,  C07D487/04

Abstract: A compound having the structure: or a pharmaceutically acceptable salt or solvate thereof, wherein A and A′ are C or N, where C may be substituted by halo or C1-C6 alkyl; R and R0 are selected from the group consisting of H, C1-C6 alkyl, —(CH2)n—W, etc., where W is 5- or 6-membered heteroaryl or heterocyclic containing N, S and/or O atoms, —NR″SO2—R′, etc., where R′ and R″ are C1-C6 alkyl, etc.; wherein each alkyl, etc., may be substituted; or, R and R0 and the N atom to which they are bonded together to form a monocyclic or bicyclic heterocyclic ring, etc.; R1 is H, halo or cyano; R2 and R2′ are H, C1-C6 alkyl, etc.; X is a bond, etc.; R3 is H, C1-C4 alkyl, etc.; Y is a bond, —(CH2)m—, etc. The invention also relates to compositions and uses in the treatment of various diseases.