公开(公告)号：US11111242B2

公开(公告)日：2021-09-07

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: A61K31/4523 ,  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 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.

公开(公告)号：US10328082B2

公开(公告)日：2019-06-25

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

Abstract: The present invention relates to a compound of Formula 1, 2 or 3: 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, C1-C6 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：US20180002331A1

公开(公告)日：2018-01-04

申请号：US15637071

申请日：2017-06-29

Applicant: Pfizer Inc.

Inventor： Lei Zhang ,  Christopher Ryan Butler ,  Elizabeth Mary Beck ,  Michael Aaron Brodney ,  Matthew Frank Brown ,  Laura Ann McAllister ,  Erik Alphie LaChapelle ,  Adam Matthew Gilbert

IPC: C07D471/04

CPC classification number: C07D471/04

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.

公开(公告)号：US20140155390A1

公开(公告)日：2014-06-05

申请号：US14093812

申请日：2013-12-02

Applicant: Pfizer Inc.

Inventor： James Thomas Anderson ,  Eugene Lvovich Piatnitski Chekler ,  Edmund L. Ellsworth ,  Bruce Kipp Erickson ,  Adam Matthew Gilbert ,  Anthony P. Ricketts ,  David P. Thompson ,  Rayomand Jal Unwalla ,  Patrick Robert Verhoest

IPC: C07D417/04 ,  C07C255/59

CPC classification number: C07D417/04 ,  C07C255/58 ,  C07C255/59 ,  C07D205/04 ,  C07D207/08 ,  C07D211/22 ,  C07D217/26 ,  C07D285/10 ,  C07D401/04

Abstract: The present invention relates to a compound of Formula 1, 2 or 3: 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, C1-C6 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, to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly, those affected or mediated by the androgen receptor.

Abstract translation: 本发明涉及式1,2或3的化合物：其中A是N或-CR 0-，其中R 0是氢，C 1 -C 6直链或支链烷基等，Z是-CRe-或 - N-，其中Re为氢，C1-C6直链或支链烷基等; R1是氢，C1-C6直链或支链烷基等; R2独立地为氢或C1-C6直链或支链烷基; R3和R4独立地是氢，C1-C6直链或支链烷基等。 R5和R6独立地是氢或C1-C6直链或支链烷基等; R8是氢，C1-C6直链或支链烷基等; R9和R10独立地为氢或C1-C6直链或支链烷基等; Q是-CO-， - （CH 2）q - ， - （CHRs）q-或（CRsRt）q-，其中R 5和R 5独立地是C 1 -C 6直链或支链烷基，芳基，烷基芳基，杂芳基或烷基杂芳基; 其中q是0,1,2或3; 并且其中n为0,1,2,3,4或5; 或其药学上可接受的盐包含含有这些化合物的组合物; 以及这些化合物在治疗各种疾病，特别是受雄激素受体影响或介导的疾病的用途。