公开(公告)号：US20140243312A1

公开(公告)日：2014-08-28

申请号：US14183946

申请日：2014-02-19

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Ashley Edward Fenwick ,  Mark Edward Flanagan ,  Andrea Gonzales ,  Timothy Allan Johnson ,  Neelu Kaila ,  Mark J. Mitton-Fry ,  Joseph Walter Strohbach ,  Ruth E. TenBrink ,  John David Trzupek ,  Rayomand Jal Unwalla ,  Michael L. Vazquez

IPC: C07D487/04

CPC classification number: A61K31/519 ,  A61K31/5386 ,  C07D207/18 ,  C07D487/04 ,  C07D519/00

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

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，以及含有它们的药物组合物。

公开(公告)号：US20140206651A1

公开(公告)日：2014-07-24

申请号：US14223061

申请日：2014-03-24

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Charles Francis Donovan ,  Edmund Lee Ellsworth ,  Denton Wade Hoyer ,  Timothy Allan Johnson ,  Manjinder Singh Lall ,  Chris Limberakis ,  Sean Timothy Murphy ,  Debra Ann Sherry ,  Clarke Bentley Taylor ,  Joseph Scott Warmus

IPC: C07C259/06 ,  C07D213/55 ,  C07F9/653 ,  C07D261/08 ,  C07D239/26 ,  C07D277/30 ,  C07D233/64 ,  C07D307/54

CPC classification number: C07C259/06 ,  C07C2601/04 ,  C07D207/267 ,  C07D213/30 ,  C07D213/38 ,  C07D213/55 ,  C07D231/12 ,  C07D233/64 ,  C07D237/04 ,  C07D239/26 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04 ,  C07D261/08 ,  C07D261/10 ,  C07D263/32 ,  C07D271/06 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D285/06 ,  C07D307/14 ,  C07D307/42 ,  C07D307/54 ,  C07D309/10 ,  C07D413/04 ,  C07D413/12 ,  C07D471/04 ,  C07F9/653

Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II): and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B, L1-L4, A, B, R1-R4, and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，其中：G为式（II）的基团：及其药学上可接受的盐，前体药物，水合物或溶剂合物，其中A， B，L1-L4，A，B，R1-R4和m如本文所定义。 本发明还涉及包含式（I）化合物及其在治疗细菌感染中的用途的药物组合物。

公开(公告)号：US09035074B2

公开(公告)日：2015-05-19

申请号：US14183946

申请日：2014-02-19

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Ashley Edward Fenwick ,  Mark Edward Flanagan ,  Andrea Gonzales ,  Timothy Allan Johnson ,  Neelu Kaila ,  Mark J. Mitton-Fry ,  Joseph Walter Strohbach ,  Ruth E. TenBrink ,  John David Trzupek ,  Rayomand Jal Unwalla ,  Michael L. Vazquez ,  Mihir D. Parikh

IPC: C07D207/18 ,  C07D487/04 ,  C07D519/00

CPC classification number: A61K31/519 ,  A61K31/5386 ,  C07D207/18 ,  C07D487/04 ,  C07D519/00

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

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，以及含有它们的药物组合物。

公开(公告)号：US09340493B2

公开(公告)日：2016-05-17

申请号：US14223061

申请日：2014-03-24

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Charles Francis Donovan ,  Edmund Lee Ellsworth ,  Denton Wade Hoyer ,  Timothy Allan Johnson ,  Manjinder Singh Lall ,  Chris Limberakis ,  Sean Timothy Murphy ,  Debra Ann Sherry ,  Clarke Bentley Taylor ,  Joseph Scott Warmus

IPC: A61K31/685 ,  A61K31/19 ,  A61K31/415 ,  A61K31/44 ,  A61K31/34 ,  A61K31/42 ,  A61K31/425 ,  A61K31/535 ,  C07D233/64 ,  C07D213/55 ,  C07D307/54 ,  C07C259/06 ,  C07D207/267 ,  C07D213/30 ,  C07D213/38 ,  C07D231/12 ,  C07D237/04 ,  C07D239/26 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04 ,  C07D261/08 ,  C07D261/10 ,  C07D263/32 ,  C07D271/06 ,  C07D277/24 ,  C07D277/28 ,  C07D285/06 ,  C07D307/14 ,  C07D307/42 ,  C07D309/10 ,  C07D413/04 ,  C07D413/12 ,  C07D471/04 ,  C07F9/653 ,  C07D277/30

CPC classification number: C07C259/06 ,  C07C2601/04 ,  C07D207/267 ,  C07D213/30 ,  C07D213/38 ,  C07D213/55 ,  C07D231/12 ,  C07D233/64 ,  C07D237/04 ,  C07D239/26 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04 ,  C07D261/08 ,  C07D261/10 ,  C07D263/32 ,  C07D271/06 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D285/06 ,  C07D307/14 ,  C07D307/42 ,  C07D307/54 ,  C07D309/10 ,  C07D413/04 ,  C07D413/12 ,  C07D471/04 ,  C07F9/653

Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II): and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B, L1-L4, A, B, R1-R4, and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，其中：G为式（II）的基团：及其药学上可接受的盐，前体药物，水合物或溶剂合物，其中A， B，L1-L4，A，B，R1-R4和m如本文所定义。 本发明还涉及包含式（I）化合物及其在治疗细菌感染中的用途的药物组合物。

公开(公告)号：US09549929B2

公开(公告)日：2017-01-24

申请号：US14715046

申请日：2015-05-18

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Ashley Edward Fenwick ,  Mark Edward Flanagan ,  Andrea Gonzales ,  Timothy Allan Johnson ,  Neelu Kaila ,  Mark J. Mitton-Fry ,  Joseph Walter Strohbach ,  Ruth E. TenBrink ,  John David Trzupek ,  Rayomand Jal Unwalla ,  Michael L. Vazquez ,  Mihir D. Parikh

IPC: A61K31/519 ,  C07D487/04 ,  C07D519/00 ,  A61K31/5386 ,  C07D207/18

CPC classification number: A61K31/519 ,  A61K31/5386 ,  C07D207/18 ,  C07D487/04 ,  C07D519/00

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

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，以及含有它们的药物组合物。

公开(公告)号：US20150225408A1

公开(公告)日：2015-08-13

申请号：US14691606

申请日：2015-04-21

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Ashley Edward Fenwick ,  Mark Edward Flanagan ,  Andrea Gonzales ,  Timothy Allan Johnson ,  Neelu Kaila ,  Mark J. Mitton-Fry ,  Joseph Walter Strohbach ,  Ruth E. TenBrink ,  John David Trzupek ,  Rayomand Jal Unwalla ,  Michael L. Vazquez ,  Mihir D. Parikh

IPC: C07D487/04 ,  C07D519/00

CPC classification number: A61K31/519 ,  A61K31/5386 ,  C07D207/18 ,  C07D487/04 ,  C07D519/00

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

公开(公告)号：US11981696B2

公开(公告)日：2024-05-14

申请号：US16980616

申请日：2019-03-14

Applicant: Pfizer Inc.

Inventor： Tamim Fehme Braish ,  Matthew Frank Brown ,  Ye Che ,  Richard Andrew Ewin ,  Timothy Allan Johnson ,  Michael Joseph Melnick ,  Justin Ian Montgomery ,  Mark Stephen Plummer ,  Loren Michael Price ,  Usa Reilly ,  Daniel Uccello

IPC: C07F9/58 ,  A61P31/04 ,  C07F5/02

CPC classification number: C07F9/58 ,  A61P31/04 ,  C07F5/022

Abstract: The present invention is directed to a new fluoro-pyridinone hydroxamic acid phosphates and boronates of Formulae I, II and III




wherein Q is selected from the group consisting of —P(O)(OH)2, —P(O)(OH)(O−M+), —P(O)(O−M+)2 and —P(O)(O−)2M2+; M+ at each occurrence is a pharmaceutically acceptable monovalent cation; and M2+ is a pharmaceutically acceptable divalent cation and their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.

公开(公告)号：US20210017206A1

公开(公告)日：2021-01-21

申请号：US16980473

申请日：2019-03-14

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Ye Che ,  Anthony Marfat ,  Michael Joseph Melnick ,  Justin Ian Montgomery ,  Timothy Allan Johnson ,  Richard Andrew Ewin ,  Daniel Paul Uccello ,  Usa Reilly ,  Tamim Fehme Braish

IPC: C07F9/6558 ,  C07F9/58 ,  C07F5/04 ,  A61P31/04

Abstract: The present invention is directed to new pyridinone or pyrimidinone hydroxamic acid phosphates of Formula (1) and boronates of Formula (2), stereoisomers thereof; wherein Q is selected from the group consisting of —P(O)(OH)2, —P(O)(OH)(O−M+), —P(O)(O−M+)2 and —P(O)(O−)2M2+; M+ at each occurrence is a pharmaceutically acceptable monovalent cation; and M2+ is a pharmaceutically acceptable divalent cation; X is CH or N; and Z is as defined herein; and their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.

公开(公告)号：US20210017205A1

公开(公告)日：2021-01-21

申请号：US16980616

申请日：2019-03-14

Applicant: Pfizer Inc.

Inventor： Tamim Fehme Braish ,  Matthew Frank Brown ,  Ye Che ,  Richard Andrew Ewin ,  Timothy Allan Johnson ,  Michael Joseph Melnick ,  Justin Ian Montgomery ,  Mark Stephen Plummer ,  Loren Michael Price ,  Usa Reilly ,  Daniel Uccello

IPC: C07F9/58 ,  C07F5/02 ,  A61P31/04

Abstract: The present invention is directed to a new fluoro-pyridinone hydroxamic acid phosphates and boronates of Formulae I, II and III wherein Q is selected from the group consisting of —P(O)(OH)2, —P(O)(OH)(O−M+), —P(O)(O−M+)2 and —P(O)(O−)2M2+; M+ at each occurrence is a pharmaceutically acceptable monovalent cation; and M2+ is a pharmaceutically acceptable divalent cation and their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.

公开(公告)号：US09545405B2

公开(公告)日：2017-01-17

申请号：US14691606

申请日：2015-04-21

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Ashley Edward Fenwick ,  Mark Edward Flanagan ,  Andrea Gonzales ,  Timothy Allan Johnson ,  Neelu Kaila ,  Mark J. Mitton-Fry ,  Joseph Walter Strohbach ,  Ruth E. TenBrink ,  John David Trzupek ,  Rayomand Jal Unwalla ,  Michael L. Vazquez ,  Mihir D. Parikh

IPC: A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C07D487/04 ,  C07D519/00 ,  A61K31/5386 ,  C07D207/18

CPC classification number: A61K31/519 ,  A61K31/5386 ,  C07D207/18 ,  C07D487/04 ,  C07D519/00

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