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MX2016014878A - Pirazolopiridinas y pirazolopirimidinas. - Google Patents

Pirazolopiridinas y pirazolopirimidinas.

Info

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
Authority
MX
Mexico
Prior art keywords
alkyl
cycloalkyl
phenyl
heteroaryl
naphthyl
Prior art date
Application number
MX2016014878A
Other languages
English (en)
Inventor
Martin Dehnhardt Christoph
Jones Peter
Anil Sabnis Yogesh
Michael Wakenhut Florian
Wadsworth Coe Jotham
Walter Strohbach Joseph
Original Assignee
Pfizer
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
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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    • A—HUMAN NECESSITIES
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
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    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A61K31/437—Heterocyclic 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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    • A61K31/435—Heterocyclic 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
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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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MX2016014878A MX2016014878A (es) 2014-05-14 2015-04-30 Pirazolopiridinas y pirazolopirimidinas.

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US (2) US9518052B2 (es)
EP (1) EP3143021B1 (es)
JP (1) JP6663857B2 (es)
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Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2016014878A (es) 2014-05-14 2017-03-08 Pfizer Pirazolopiridinas y pirazolopirimidinas.
TW201946921A (zh) 2014-05-14 2019-12-16 瑞士商諾華公司 甲醯胺衍生物
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
CN108349972B (zh) 2015-11-03 2021-06-08 施万生物制药研发Ip有限责任公司 用于治疗呼吸疾病的jak激酶抑制剂化合物
PL3371185T3 (pl) 2015-11-03 2021-04-06 Topivert Pharma Limited Pochodne 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pirydyny i 1,4,5,6,7,8-heksahydroimidazo[4,5-d]azepiny jako inhibitory kinaz janusowych
KR102526764B1 (ko) 2017-03-09 2023-04-27 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 융합된 이미다조-피페리딘 jak 저해제
AR111495A1 (es) 2017-05-01 2019-07-17 Theravance Biopharma R&D Ip Llc Compuestos de imidazo-piperidina fusionada como inhibidores de jak
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
AU2018261591B2 (en) 2017-05-01 2021-09-02 Theravance Biopharma R&D Ip, Llc Crystalline forms of a JAK inhibitor compound
AR112348A1 (es) 2017-08-01 2019-10-16 Theravance Biopharma R&D Ip Llc Compuestos bicíclicos de pirazolo y triazolo como inhibidores de quinasas jak
SG11202002947TA (en) 2017-11-03 2020-04-29 Aclaris Therapeutics Inc Substituted pyrrolopyrimidine jak inhibitors and methods of making and using the same
MX2021001558A (es) 2018-08-10 2021-04-28 Aclaris Therapeutics Inc Inhibidores de itk de pirrolopirimidina.
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
LT3837258T (lt) 2018-09-04 2024-05-27 Theravance Biopharma R&D Ip, Llc Dimetilamino azetidino amidai kaip jak inhibitoriai
EP3837010B1 (en) 2018-09-04 2023-07-05 Theravance Biopharma R&D IP, LLC 5 to 7 membered heterocyclic amides as jak inhibitors
AR116116A1 (es) 2018-09-04 2021-03-31 Theravance Biopharma R&D Ip Llc Proceso para elaborar inhibidores de jak e intermediarios de los mismos
CN112955451A (zh) 2018-10-29 2021-06-11 施万生物制药研发Ip有限责任公司 作为jak抑制剂的2-氮杂双环已烷化合物
CN113498352A (zh) 2019-01-23 2021-10-12 施万生物制药研发Ip有限责任公司 作为jak抑制剂的咪唑并[1,5-a]吡啶、1,2,4-三唑并[4,3-a]吡啶和咪唑并[1,5-a]吡嗪
DK3932919T3 (da) 2019-02-25 2024-07-15 Henan Medinno Pharmaceutical Tech Co Ltd Jak-inhibitorforbindelse og anvendelse deraf
CN114075199A (zh) 2020-08-14 2022-02-22 河南迈英诺医药科技有限公司 Jak抑制剂化合物及其用途
JP2022531088A (ja) 2019-05-02 2022-07-06 アクラリス セラピューティクス，インコーポレイテッド Ｊａｋ阻害剤としての置換ピロロピリジン
US20220235043A1 (en) * 2019-07-31 2022-07-28 Aclaris Therapeutics, Inc. Substituted sulfonamide pyrrolopyridines as jak inhibitors
WO2021136345A1 (zh) * 2019-12-30 2021-07-08 路良 Jak抑制剂化合物及其用途
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
CA3192236A1 (en) 2020-09-10 2022-03-17 Tony Lahoutte Antibody fragment against 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
AU2003280838A1 (en) 2002-11-19 2004-06-15 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
ES2593486T3 (es) 2007-04-18 2016-12-09 Pfizer Products Inc. Derivados de sulfonil amida para el tratamiento del crecimiento celular anómalo
BRPI0817681A2 (pt) * 2007-10-16 2015-04-14 Wyeth Llc Compostos de tienopirimidina e pirazolopirimidina e seu uso como inibidores de mtor quinase e pi3 quinase
JP2011503103A (ja) * 2007-11-07 2011-01-27 フォールドアールエックス ファーマシューティカルズ インコーポレーティッド タンパク質輸送の調節方法
WO2009070524A1 (en) * 2007-11-27 2009-06-04 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
US8987280B2 (en) * 2008-01-30 2015-03-24 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
EP2361902A4 (en) 2008-11-21 2012-04-25 Astellas Pharma Inc 4,6-DIAMINONICOTINSÄUREAMIDVERBINDUNG
CN102428084B (zh) * 2009-03-19 2016-05-18 医疗技术研究局 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
MX2016014878A (es) 2014-05-14 2017-03-08 Pfizer Pirazolopiridinas y pirazolopirimidinas.

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