-
公开(公告)号:US20240124450A1
公开(公告)日:2024-04-18
申请号:US18466034
申请日:2023-09-13
Applicant: Pfizer Inc.
Inventor: Andrea Nicole Bootsma , David Christopher Ebner , Daniel Wei-Shung Kung , Matthew Alexander Perry , Daniel Copley Schmitt , Joseph Walter Strohbach , Atli Thorarensen
IPC: C07D471/04
CPC classification number: C07D471/04
Abstract: A compound of formula I having the structure:
or a pharmaceutically acceptable salt thereof, wherein A1 and A2 are independently O or S; X is selected from CH2, CD2, NR3, O, and S, where R3 is selected from hydrogen, C1-C4 linear or branched chain alkyl, halo(C1-C4)linear or branched chain alkyl, and hydroxyl(C1-C4)linear or branched chain alkyl; Y and Z are selected from C and N, where when Y is C, then Z is N, and when Y is N, then Z is C; R1 and R2 are independently selected from hydrogen, deuterium, C1-C4 linear or branched chain alkyl, etc.; or a C1-C2 alkyl substituted with a C3-C5 cycloalkyl ring; or taken together to form a C3-C6 cycloalkyl ring; or where X is CH2 or CD2, then R1 and R2 are independently selected from hydrogen, deuterium, halogen, hydroxyl, C1-C4 linear or branched chain alkyl, etc.; R4 is selected from hydrogen, deuterium, cyano, halogen, (C1-C3) alkoxy, etc.; R5 is selected from hydrogen, deuterium, halogen, C1-C3 alkoxy, amino, (C1-C4 linear or branched chain alkyl)amino, etc.; R6 is selected from hydrogen, deuterium, halogen, CO2R7 where R7 is selected from H and C1-C4 linear or branched chain alkyl, etc.; R8 is selected from hydrogen, deuterium, and C1-C3 linear or branched chain alkyl; R9 is selected from C1-C3 linear or branched chain alkyl, and a halo(C1-C3)linear or branched chain alkyl; and, n and m are independently selected from 0, 1 and 2. The invention also relates to pharmaceutical compositions thereof and therapeutic methods of use therewith.-
公开(公告)号:US11661419B2
公开(公告)日:2023-05-30
申请号:US17126358
申请日:2020-12-18
Applicant: Pfizer Inc.
Inventor: Scott William Bagley , Agustin Casimiro-Garcia , Xiayun Cheng , Jennifer Elizabeth Davoren , Rajiah Aldrin Denny , Brian Stephen Gerstenberger , Frank Eldridge Lovering , Mihir Dineshkumar Parikh , Joseph Walter Strohbach , John Isidro Trujillo
IPC: C07D413/14 , A61P17/00 , A61K45/06
CPC classification number: C07D413/14 , A61K45/06 , A61P17/00
Abstract: The invention relates to benzimidazoles of Formula (I)
and pharmaceutically acceptable salts thereof, wherein R1 to R6 are as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes.
The benzimidazoles of Formula (I) are ITK inhibitors and are therefore potentially useful in the treatment of a wide range of disorders including, atopic dermatitis.-
公开(公告)号:US11559538B2
公开(公告)日:2023-01-24
申请号:US17082102
申请日:2020-10-28
Applicant: Pfizer Inc.
Inventor: Joseph Walter Strohbach , Tsutomu Akama , David Clive Blakemore , Robert Toms Jacobs , Peter Jones , David Christopher Limburg , Martins Sunday Oderinde , Matthew Alexander Perry , Jacob John Plattner , Rubben Federico Torella , Yasheen Zhou , Thean Yeow Yeoh
IPC: C07F5/02 , A61K31/69 , A61K31/519
Abstract: The present invention relates to boron containing compounds of Formula (IA): that inhibit phosphodiesterase 4 (PDE4). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating diseases, conditions, or disorders ameliorated by inhibition of PDE4.
-
公开(公告)号:US10946031B2
公开(公告)日:2021-03-16
申请号:US16593171
申请日:2019-10-04
Applicant: Pfizer Inc.
IPC: C07F5/02 , A61K31/69 , A61K31/519
Abstract: The present invention relates to PDE4 inhibitor (R)-4-(5-(4-methoxy-3-propoxyphenyl)pyridin-3-yl)-1,2-oxaborolan-2-ol including the crystalline monohydrate thereof.
-
公开(公告)号:US10022376B2
公开(公告)日:2018-07-17
申请号:US15342601
申请日:2016-11-03
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 , A61K31/519 , A61K31/437 , A61K31/4725
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 Ro 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.
-
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.
-
公开(公告)号:US20150246048A1
公开(公告)日:2015-09-03
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 , A61K31/5386
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:US12202836B2
公开(公告)日:2025-01-21
申请号:US18342977
申请日:2023-06-28
Applicant: Pfizer Inc.
Inventor: John David Trzupek , Katherine Lin Lee , Mark Edward Bunnage , Seungil Han , David Hepworth , Frank Eldridge Lovering , John Paul Mathias , Nikolaos Papaioannou , Betsy Susan Pierce , Joseph Walter Strohbach , Stephen Wayne Wright , Christoph Wolfgang Zapf , Lori Krim Gavrin , Arthur Lee , David Randolph Anderson , Kevin Joseph Curran , Christoph Martin Dehnhardt , Eddine Saiah , Joel Adam Goldberg , Xiaolun Wang , Horng-Chih Huang , Richard Vargas , Michael Dennis Lowe , Akshay Patny
IPC: C07D491/056 , A61K31/40 , A61K31/4015 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , C07C69/94 , C07D207/08 , C07D207/26 , C07D207/267 , C07D207/273 , C07D209/52 , C07D215/48 , C07D217/02 , C07D217/22 , C07D217/24 , C07D239/86 , C07D239/88 , C07D263/24 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D407/14 , C07D413/12 , C07D417/12 , C07D487/04 , C07D498/04 , C07F7/18
Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. In an embodiment, a pharmaceutical composition can be in a liquid dosage form and can comprise a therapeutically effective amount of the compound or a pharmaceutically acceptable salt thereof as an adjuvant and a therapeutic agent. In another embodiment, a method of adjuvant treating a disorder or condition can comprising administering the pharmaceutical composition to a patient.
-
公开(公告)号:US11702424B2
公开(公告)日:2023-07-18
申请号:US16996117
申请日:2020-08-18
Applicant: Pfizer Inc.
Inventor: John David Trzupek , Katherine Lin Lee , Mark Edward Bunnage , Seungil Han , David Hepworth , Frank Eldridge Lovering , John Paul Mathias , Nikolaos Papaioannou , Betsy Susan Pierce , Joseph Walter Strohbach , Stephen Wayne Wright , Christoph Wolfgang Zapf , Lori Krim Gavrin , Arthur Lee , David Randolph Anderson , Kevin Joseph Curran , Christoph Martin Dehnhardt , Eddine Saiah , Joel Adam Goldberg , Xiaolun Wang , Horng-Chih Huang , Richard Vargas , Michael Dennis Lowe , Akshay Patny
IPC: C07D491/056 , C07F7/18 , C07D401/14 , C07D405/14 , C07D217/02 , C07D217/22 , C07D217/24 , C07D239/86 , C07D239/88 , C07D263/24 , C07D207/273 , C07D498/04 , C07D209/52 , A61K31/4015 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , C07C69/94 , A61K31/541 , A61K45/06 , C07D207/26 , C07D215/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/14 , C07D413/12 , C07D417/12 , C07D487/04 , A61K31/40 , C07D207/08 , C07D207/267
CPC classification number: C07D491/056 , A61K31/40 , A61K31/4015 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , C07C69/94 , C07D207/08 , C07D207/26 , C07D207/267 , C07D207/273 , C07D209/52 , C07D215/48 , C07D217/02 , C07D217/22 , C07D217/24 , C07D239/86 , C07D239/88 , C07D263/24 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D407/14 , C07D413/12 , C07D417/12 , C07D487/04 , C07D498/04 , C07F7/1804
Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia,
as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.-
公开(公告)号:US20210069219A1
公开(公告)日:2021-03-11
申请号:US17082102
申请日:2020-10-28
Applicant: Pfizer Inc.
Inventor: Joseph Walter Strohbach , Tsutomu Akama , David Clive Blakemore , Robert Toms Jacobs , Peter Jones , David Christopher Limburg , Martins Sunday Oderinde , Matthew Alexander Perry , Jacob John Plattner , Rubben Federico Torella , Yasheen Zhou , Thean Yeow Yeoh
IPC: A61K31/69 , A61K31/519 , C07F5/02
Abstract: The present invention relates to boron containing compounds of Formula (I) X—Y—Z Formula (I) that inhibit phosphodiesterase 4 (PDE4). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating diseases, conditions, or disorders ameliorated by inhibition of PDE4.
-
-
-
-
-
-
-
-
-