MX2016014878A - Pirazolopiridinas y pirazolopirimidinas. - Google Patents

Pirazolopiridinas y pirazolopirimidinas.

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Publication number
MX2016014878A
MX2016014878A MX2016014878A MX2016014878A MX2016014878A MX 2016014878 A MX2016014878 A MX 2016014878A MX 2016014878 A MX2016014878 A MX 2016014878A MX 2016014878 A MX2016014878 A MX 2016014878A MX 2016014878 A MX2016014878 A MX 2016014878A
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MX
Mexico
Prior art keywords
alkyl
cycloalkyl
phenyl
heteroaryl
naphthyl
Prior art date
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MX2016014878A
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English (en)
Inventor
Martin Dehnhardt Christoph
Jones Peter
Anil Sabnis Yogesh
Michael Wakenhut Florian
Wadsworth Coe Jotham
Walter Strohbach Joseph
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Pfizer
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=53264695&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MX2016014878(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer filed Critical Pfizer
Publication of MX2016014878A publication Critical patent/MX2016014878A/es

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    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
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Abstract

Un compuesto que tiene la estructura: (ver Fórmula) o una de sus sales farmacéuticamente aceptables o un solvato farmacéuticamente aceptable de dicho compuesto o sal farmacéuticamente aceptable, en donde A y A' son, de modo independiente, C o N, donde C puede no estar sustituido o puede estar sustituido con halo o alquilo C1-C6; R y R0 se seleccionan, de modo independiente, del grupo que consiste en H, alquilo C1-C6, hidroxi(alquilo C1-C6), fenil(alquilo C1-C6) y -(CH2)n-W, donde W es cicloalquilo C3-C5, fenilo, naftilo, heteroarilo de 5 ó 6 miembros o heterocíclico que contiene 1-3 átomos de N, S y/u O, -SO2-R', -NHSO2-R', -NR"SO2-R' y SR', donde R' y R" son, de modo independiente, alquilo C1-C6 o cicloalquilo C3-C8, etc.; en donde cada uno de dichos alquilo, cicloalquilo, heterocíclico, fenilo, naftilo o heteroarilo puede no estar sustituido o puede estar sustituido con fenilo, heteroarilo, etc.; o R y R0 y el átomo de N al que están unidos forman un anillo heterocíclico monocíclico o bicíclico que puede no estar sustituido o puede estar sustituido con (a) halo, hidroxi, heteroarilo, alquilo C1-C6, alcoxi C1-C6, etc. o (b) -(CH2)-W, donde W es cicloalquilo C3-C8, fenilo, etc.; R1 es H, halo o ciano; R2 y R2' son, de modo independiente, H, alquilo C1-C6, ciano, alcoxi C1-C6, alquil C1-C6-tio o cicloalquilo C3-C8, donde alquilo, alcoxi o cicloalquilo está opcionalmente sustituido con uno o varios átomos de flúor; X es un enlace, -CO-, -CONH-, -SO2-, - SONH o (CH2)m--; R3 es H, alquilo C1-C4, fenilo, naftilo, heteroarilo de 5 ó 6 miembros o heterocíclico que contiene 1-3 átomos de N, un heteroarilo de 5 miembros o heterocíclico, etc. o (c) 2 átomos de O o S y 0-2 átomos de N; en donde cada uno de dichos fenilo, naftilo, heteroarilo o heterocíclico está opcionalmente sustituido con alquilo, 1 sustituyente -Y-R4 y/o 1-4 sustituyentes seleccionados cada uno, de modo independiente, de R5; siempre que, cuando X es -CO- o -SO2-, R3 no sea H; Y es un enlace, -(CH2)m- u -o-; R4 es (a) H, alquilo C1-C6, cicloalquilo C3-C8, halo, oxo, -OR6, -NR7R8, -SR6, -SOR9, -SO2R9, -COR6, -OCOR6, -COOR6, -NR6COR6, -CONR7R8, etc.; (b) fenilo o naftilo, estando dicho fenilo y naftilo opcionalmente sustituidos con 1-5 sustituyentes seleccionados de alquilo C1-C6, cicloalquilo C3-C8, halo, ciano, -OR6, -NR7R8, etc.; o (c) un heteroarilo monocíclico saturado o parcialmente insaturado de 3 a 8 miembros, etc.; R6 es H, alquilo C1-C6 o cicloalquilo C3-C8, etc.; R7 y R8 son cada uno, de modo independiente, H, alquilo C1-C6 o cicloalquilo C3-C8 o se toman junto con el átomo de nitrógeno al que están unidos para formar un anillo heterocíclico saturado de 4, 5 ó 6 miembros que contiene 1-2 átomos de nitrógeno o 1 átomo de nitrógeno y 1 átomo de oxígeno, dicho alquilo C1-C6 está opcionalmente sustituido con cicloalquilo C3-C8, halo, etc. y estando dicho anillo heterocíclico opcionalmente sustituido con uno o varios grupos alquilo C1-C6 o cicloalquilo C3-C8; R9 es alquilo C1-C6 o cicloalquilo C3-C8; y, m y n son, de modo independiente, 0, 1, 2 ó 3. La invención también se refiere a sales farmacéuticamente aceptables de estos compuestos y solvatos farmacéuticamente aceptables; a composiciones que contienen tales compuestos; y a los usos de tales compuestos en el tratamiento de diversas enfermedades, en particular asma y EPOC.
MX2016014878A 2014-05-14 2015-04-30 Pirazolopiridinas y pirazolopirimidinas. MX2016014878A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461993138P 2014-05-14 2014-05-14
PCT/IB2015/053174 WO2015173683A1 (en) 2014-05-14 2015-04-30 Pyrazolopyridines and pyrazolopyrimidines

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MX2016014878A true MX2016014878A (es) 2017-03-08

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EP (1) EP3143021B1 (es)
JP (1) JP6663857B2 (es)
KR (1) KR20170002623A (es)
CN (1) CN106459048A (es)
AP (1) AP2016009562A0 (es)
AR (1) AR100438A1 (es)
AU (1) AU2015260905A1 (es)
CA (1) CA2948587C (es)
CL (1) CL2016002888A1 (es)
CR (1) CR20160525A (es)
CU (1) CU20160167A7 (es)
DO (1) DOP2016000298A (es)
EA (1) EA201650029A1 (es)
EC (1) ECSP16087271A (es)
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MX (1) MX2016014878A (es)
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PE (1) PE20161475A1 (es)
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Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GEP20186921B (en) 2014-05-14 2018-11-12 Pfizer Pyrazolopyridines and pyrazolopyrimidines
TWI714528B (zh) 2014-05-14 2021-01-01 瑞士商諾華公司 甲醯胺衍生物
MY195427A (en) 2015-11-03 2023-01-20 Theravance Biopharma R&D Ip Llc Jak Kinase Inhibitor Compounds for Treatment of Respiratory Disease
WO2017077288A1 (en) 2015-11-03 2017-05-11 Topivert Pharma Limited 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as janus kinase inhibitors
WO2017077283A1 (en) 2015-11-03 2017-05-11 Topivert Pharma Limited 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as janus kinase inhibitors
CN110382498B (zh) 2017-03-09 2022-07-12 施万生物制药研发Ip有限责任公司 稠合咪唑-哌啶jak抑制剂
JP7153031B2 (ja) 2017-05-01 2022-10-13 セラヴァンス バイオファーマ アール&ディー アイピー, エルエルシー Jak阻害剤化合物を使用する処置方法
AR111495A1 (es) 2017-05-01 2019-07-17 Theravance Biopharma R&D Ip Llc Compuestos de imidazo-piperidina fusionada como inhibidores de jak
JP7096268B2 (ja) 2017-05-01 2022-07-05 セラヴァンス バイオファーマ アール&ディー アイピー, エルエルシー Jak阻害剤化合物の結晶形態
US10392368B2 (en) 2017-08-01 2019-08-27 Theravance Biopharma R&D Ip, Llc Pyrazolo and triazolo bicyclic compounds as JAK kinase inhibitors
MX2020004946A (es) 2017-11-03 2020-09-25 Aclaris Therapeutics Inc Inhibidores jak de pirrolopiridina sustituidos y metodos para producir y utilizar los mismos.
JP2021534244A (ja) 2018-08-10 2021-12-09 アクラリス セラピューティクス,インコーポレイテッド ピロロピリミジンitk阻害剤
CN110833555B (zh) * 2018-08-15 2023-03-24 广西梧州制药(集团)股份有限公司 吡唑并嘧啶衍生物在治疗溃疡性结肠炎的用途
IL281152B2 (en) 2018-09-04 2023-12-01 Theravance Biopharma R& D Ip Llc Process for preparing JAK inhibitors and their intermediates
WO2020051139A1 (en) 2018-09-04 2020-03-12 Theravance Biopharma R&D Ip, Llc 5 to 7 membered heterocyclic amides as jak inhibitors
TWI791886B (zh) 2018-09-04 2023-02-11 美商施萬生物製藥研發 Ip有限責任公司 作為jak抑制劑之二甲基胺基氮雜環丁烷醯胺
KR20210084512A (ko) 2018-10-29 2021-07-07 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 Jak 억제제로서 2-아자비시클로 헥산 화합물
JP2022518741A (ja) 2019-01-23 2022-03-16 セラヴァンス バイオファーマ アール&ディー アイピー, エルエルシー JAKキナーゼ阻害剤としてのイミダゾ[1,5-a]ピリジン、1,2,4-トリアゾロ[4,3-a]ピリジンおよびイミダゾ[1,5-a]ピラジン
BR112021016751B8 (pt) * 2019-02-25 2023-11-21 Henan Medinno Pharmaceutical Tech Co Ltd Compostos, composições farmacêuticas e usos dos compostos
KR20220004726A (ko) 2019-05-02 2022-01-11 어클라리스 쎄라퓨틱스, 인코포레이티드 Jak 억제제로서의 치환된 피롤로피리딘
US20220235043A1 (en) * 2019-07-31 2022-07-28 Aclaris Therapeutics, Inc. Substituted sulfonamide pyrrolopyridines as jak inhibitors
EP4071145A4 (en) * 2019-12-30 2023-04-19 Liang Lu JAK INHIBITOR COMPOUND AND ITS USE
CN113101975B (zh) * 2020-01-13 2022-04-22 万华化学集团股份有限公司 一种多膦配体催化剂体系及其在乙烯齐聚反应的应用
TW202144343A (zh) 2020-03-02 2021-12-01 美商施萬生物製藥研發 Ip有限責任公司 Jak抑制劑化合物之結晶水合物
CN111548269B (zh) * 2020-04-29 2023-10-27 兰州大学 一种二芳基甲烷结构化合物的制备方法
GB202010408D0 (en) * 2020-07-07 2020-08-19 Reviral Ltd Pharmaceutical compounds
MX2023002850A (es) 2020-09-10 2023-07-07 Precirix N V Fragmento de anticuerpo contra proteina activadora de fibroblastos (fap).
CN115557947B (zh) * 2021-07-02 2024-04-02 成都百裕制药股份有限公司 吡唑并[4,3-c]吡啶衍生物及其在医药上的应用
CN113480543B (zh) * 2021-07-07 2022-05-17 无锡市第二人民医院 2,6,8-多取代咪唑并[1,2-a]吡嗪及其合成方法和应用
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
WO2023213801A1 (en) 2022-05-02 2023-11-09 Precirix N.V. Pre-targeting

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
GB9518953D0 (en) 1995-09-15 1995-11-15 Pfizer Ltd Pharmaceutical formulations
WO2000035298A1 (en) 1996-11-27 2000-06-22 Wm. Wrigley Jr. Company Chewing gum containing medicament active agents
GB9711643D0 (en) 1997-06-05 1997-07-30 Janssen Pharmaceutica Nv Glass thermoplastic systems
US20030139427A1 (en) * 2002-08-23 2003-07-24 Osi Pharmaceuticals Inc. Bicyclic pyrimidinyl derivatives and methods of use thereof
EP1562898A1 (en) 2002-11-19 2005-08-17 Takeda Pharmaceutical Company Limited Indole derivatives as somatostatin agonists or antagonists
US20080234262A1 (en) * 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
CA2684447C (en) 2007-04-18 2012-01-24 Pfizer Products Inc. Sulfonyl amide derivatives for the treatment of abnormal cell growth
EP2212333A1 (en) * 2007-10-16 2010-08-04 Wyeth LLC Thienopyrimidine and pyrazolopyrimidine compounds and their use as mtor kinase and pi3 kinase inhibitors
US20100331297A1 (en) * 2007-11-07 2010-12-30 Foldrx Pharmaceuticals, Inc. Modulation of protein trafficking
US20090149458A1 (en) * 2007-11-27 2009-06-11 Wyeth PYRROLO[3,2-d]PYRIMIDINE COMPOUNDS AND THEIR USE AS PI3 KINASE AND mTOR KINASE INHIBITORS
CA2712267A1 (en) * 2008-01-15 2009-07-23 Wyeth Llc 3h-[1,2,3]triazolo[4,5-d]pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
EP2252616B1 (en) * 2008-01-30 2014-07-23 Genentech, Inc. Pyrazolopyrimidine pi3k inhibitor compounds and methods of use
JP5502858B2 (ja) * 2008-06-05 2014-05-28 グラクソ グループ リミテッド Pi3キナーゼの阻害剤として有用な4−カルボキサミドインダゾール誘導体
WO2009153261A1 (en) * 2008-06-18 2009-12-23 Solvay Pharmaceuticals Gmbh HYDROXYPHENYL-SUBSTITUTED PYRROLO[2,3d]PYRIMIDINE DERIVATIVES, PROCESSES AND INTERMEDIATE PRODUCTS FOR THEIR PREPARATION AND MEDICAMENTS CONTAINING THESE COMPOUNDS
WO2010058846A1 (ja) 2008-11-21 2010-05-27 アステラス製薬株式会社 4,6-ジアミノニコチンアミド化合物
JP5732036B2 (ja) * 2009-03-19 2015-06-10 メディカル リサーチ カウンシル テクノロジーMedical Research Council Technology 化合物
WO2012045195A1 (en) 2010-10-09 2012-04-12 Abbott Laboratories Pyrrolopyrimidines as fak and alk inhibiters for treatment of cancers and other diseases
US8575336B2 (en) * 2011-07-27 2013-11-05 Pfizer Limited Indazoles
GEP20186921B (en) 2014-05-14 2018-11-12 Pfizer Pyrazolopyridines and pyrazolopyrimidines

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