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PE20200447A1 - Compuestos de biheteroarilo y usos de los mismos - Google Patents

Compuestos de biheteroarilo y usos de los mismos

Info

Publication number
PE20200447A1
PE20200447A1 PE2019002479A PE2019002479A PE20200447A1 PE 20200447 A1 PE20200447 A1 PE 20200447A1 PE 2019002479 A PE2019002479 A PE 2019002479A PE 2019002479 A PE2019002479 A PE 2019002479A PE 20200447 A1 PE20200447 A1 PE 20200447A1
Authority
PE
Peru
Prior art keywords
pyrimidin
biheteroaril
compounds
compound
dlk
Prior art date
Application number
PE2019002479A
Other languages
English (en)
Inventor
Anthony Estrada
Paul Gibbons
Terry Kellar
Wen Liu
Changyou Ma
Alan Olivero
Snahel Patel
Daniel Shore
Michael Siu
Kevin X Chen
Malcolm Huestis
Liting Dong
Joseph P Lyssikatos
Original Assignee
Hoffmann La Roche
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
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20200447A1 publication Critical patent/PE20200447A1/es

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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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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Abstract

Referido a un compuesto de formula (I-I) o sus sales, en el que R1, R2 y R3 son cada uno independientemente H, F, Cl, Br, I, alquilo C1-6 o haloalquilo C1-6; X1 es N; X2 es N o CH; y A y Cy se selecciona entre el grupo que consiste en pirrolidina, piperidina, azetidina, entre otros. Un compuesto preferido es 5-[2-(3,3-difluoro-1-piperidil)-6-[(1S,4S)-2-oxa-5-azabiciclo[2.2.1]heptan-5-il]pirimidin-4-il]pirimidin-2-amina. Estos compuestos biheteroarilos inhiben la actividad de la doble quinasa de cremallera de leucina (DLK), siendo util para el tratamiento de enfermedades neurodegenerativas.
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Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX363118B (es) * 2012-05-03 2019-03-11 Genentech Inc Derivados de pirazol aminopirimidina como moduladores de cinasa 2 de repeticion rica en leucina (lrrk2).
BR112015016395A2 (pt) 2013-01-18 2017-07-11 Hoffmann La Roche pirazóis 3-substituídos e uso como inibidores de dlk
MA42164B1 (fr) * 2013-05-01 2019-12-31 Hoffmann La Roche Composes biheteroaryle et leurs utilisations
KR20160002850A (ko) * 2013-05-01 2016-01-08 에프. 호프만-라 로슈 아게 C-연결된 헤테로사이클로알킬 치환된 피리미딘 및 이의 용도
MX2016008110A (es) * 2013-12-20 2016-08-19 Hoffmann La Roche Derivados de pirazol como inhibidores de la cinasa de cremallera de leucina dual (dlk) y usos de los mismos.
CN104926716A (zh) * 2015-06-10 2015-09-23 哈尔滨工业大学 吡啶衍生物2,6-二[(6-甲氧基吡啶-2-基)甲基]吡啶及其合成方法
BR112019004243A2 (pt) * 2016-08-29 2019-06-04 Univ Texas composto, composição farmacêutica, método para inibição de quinase do zíper de leucina dupla, método para tratamento de uma doença mediada por quinase do zíper de leucina dupla e método para obter um efeito em um paciente
KR20190087622A (ko) 2016-12-08 2019-07-24 보드 오브 리전츠 더 유니버시티 오브 텍사스 시스템 질환 치료를 위한 이중 류신 지퍼 (dlk) 키나아제의 바이시클로[1.1.1]펜탄 억제제
KR102664604B1 (ko) 2017-07-14 2024-05-14 에프. 호프만-라 로슈 아게 이환형 케톤 화합물 및 이의 사용 방법
EP3694858B1 (en) 2017-10-11 2023-01-11 F. Hoffmann-La Roche AG Bicyclic compounds for use as rip1 kinase inhibitors
TWI797176B (zh) * 2017-10-17 2023-04-01 西班牙商帕羅製藥有限公司 ４-胺基嘧啶化合物之合成
AU2018360270A1 (en) 2017-10-31 2020-03-26 F. Hoffmann-La Roche Ag Bicyclic sulfones and sulfoxides and methods of use thereof
JP7398391B2 (ja) 2018-04-20 2023-12-14 エフ． ホフマン－ラ ロシュ アーゲー Ｎ－［４－オキソ－２，３－ジヒドロ－１，５－ベンズオキサゼピン－３－イル］－５，６－ジヒドロ－４Ｈ－ピロロ［１，２－ｂ］ピラゾール－２－カルボキサミド誘導体及び例えば過敏性腸症候群（ＩＢＳ）を処置するためのＲＩＰ１キナーゼ阻害剤としての関連化合物
EP3870291A1 (en) 2018-10-22 2021-09-01 Cadent Therapeutics, Inc. Crystalline forms of potassium channel modulators
CA3123215C (en) 2018-12-19 2024-04-02 Disarm Therapeutics, Inc. Inhibitors of sarm1 in combination with neuroprotective agents
CN113302193A (zh) 2019-01-11 2021-08-24 豪夫迈·罗氏有限公司 双环吡咯并三唑酮化合物及其使用方法
KR20210123337A (ko) * 2019-01-31 2021-10-13 더 내셔널 인스티튜츠 오브 파마슈티컬 알앤디 컴퍼니 리미티드 방향족 고리 또는 헤테로방향족 고리 화합물, 이의 제조 방법 및 이의 의학 용도
US11560366B2 (en) 2019-10-21 2023-01-24 Board Of Regents, The University Of Texas System Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (DLK) kinase for the treatment of disease
JP2021070684A (ja) * 2019-10-30 2021-05-06 東ソー株式会社 ハロゲン化合物の製造方法
JP7785004B2 (ja) * 2020-01-29 2025-12-12 カマリ ファーマ リミテッド 皮膚障害の治療に使用するための化合物及び組成物
BR112023005853A2 (pt) * 2020-10-02 2023-05-02 Genentech Inc Processo para preparar um composto de fórmula i, compostos, processos para preparar o composto 1, forma cristalina, composição farmacêutica, processo de preparação da forma cristalina do composto i e método para tratar uma condição neurodegenerativa
US20250032489A1 (en) * 2021-09-01 2025-01-30 The U.S.A., As Represented By The Secretary, Department Of Health And Human Services Mixed lineage kinase inhibitors and methods of use
WO2023067550A1 (en) * 2021-10-20 2023-04-27 Yousef Najajreh Allosteric inhibitor compounds for overcoming cancer resistance
TW202435863A (zh) 2023-01-28 2024-09-16 芬蘭商奧利安公司 Cbl-b抑制劑

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
US4485045A (en) 1981-07-06 1984-11-27 Research Corporation Synthetic phosphatidyl cholines useful in forming liposomes
EP0102324A3 (de) 1982-07-29 1984-11-07 Ciba-Geigy Ag Lipide und Tenside in wässriger Phase
US4544545A (en) 1983-06-20 1985-10-01 Trustees University Of Massachusetts Liposomes containing modified cholesterol for organ targeting
HUT35524A (en) 1983-08-02 1985-07-29 Hoechst Ag Process for preparing pharmaceutical compositions containing regulatory /regulative/ peptides providing for the retarded release of the active substance
US5004697A (en) 1987-08-17 1991-04-02 Univ. Of Ca Cationized antibodies for delivery through the blood-brain barrier
US5112596A (en) 1990-04-23 1992-05-12 Alkermes, Inc. Method for increasing blood-brain barrier permeability by administering a bradykinin agonist of blood-brain barrier permeability
US5268164A (en) 1990-04-23 1993-12-07 Alkermes, Inc. Increasing blood-brain barrier permeability with permeabilizer peptides
AU677216B2 (en) 1992-07-27 1997-04-17 Government Of The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services, The Targeting of liposomes to the blood-brain barrier
US6514221B2 (en) 2000-07-27 2003-02-04 Brigham And Women's Hospital, Inc. Blood-brain barrier opening
AU2001286930A1 (en) 2000-08-30 2002-03-13 The Board Of Trustees Of The Leland Stanford Junior University Glucocorticoid blocking agents for increasing blood-brain barrier permeability
US7034036B2 (en) 2000-10-30 2006-04-25 Pain Therapeutics, Inc. Inhibitors of ABC drug transporters at the blood-brain barrier
DE10121982B4 (de) 2001-05-05 2008-01-24 Lts Lohmann Therapie-Systeme Ag Nanopartikel aus Protein mit gekoppeltem Apolipoprotein E zur Überwindung der Blut-Hirn-Schranke und Verfahren zu ihrer Herstellung
US20030129186A1 (en) 2001-07-25 2003-07-10 Biomarin Pharmaceutical Inc. Compositions and methods for modulating blood-brain barrier transport
US20030162695A1 (en) 2002-02-27 2003-08-28 Schatzberg Alan F. Glucocorticoid blocking agents for increasing blood-brain barrier permeability
SI1549652T1 (sl) 2002-09-30 2009-04-30 Bayer Healthcare Ag Kondenzirani azolpirimidinski derivati
CA2791165C (en) 2002-12-03 2015-02-24 Blanchette Rockefeller Neurosciences Institute A conjugate comprising cholesterol linked to tetracycline
JP2007505142A (ja) 2003-09-10 2007-03-08 セダーズ−シナイ メディカル センター 血液脳関門を通過する薬剤のカリウムチャネル媒介性送達
GB0508471D0 (en) 2005-04-26 2005-06-01 Celltech R&D Ltd Therapeutic agents
JO2660B1 (en) * 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
WO2008064244A2 (en) 2006-11-20 2008-05-29 The Trustees Of Columbia University In The City Of New York Phosphoinositide modulation for the treatment of neurodegenerative diseases
US8173647B2 (en) 2007-02-06 2012-05-08 Gordana Atallah PI 3-kinase inhibitors and methods of their use
AU2008279776B2 (en) 2007-07-19 2013-05-23 Merck Sharp & Dohme Corp. Heterocyclic amide compounds as protein kinase inhibitors
WO2009066084A1 (en) * 2007-11-21 2009-05-28 F. Hoffmann-La Roche Ag 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors
US20100056609A1 (en) 2008-08-26 2010-03-04 Washington University Methods and compositions for inhibition of axonal degeneration by modulation of the dlk/jnk pathway
US20110195966A1 (en) * 2008-10-31 2011-08-11 Novartis Ag Combination of a phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor
GB2465405A (en) 2008-11-10 2010-05-19 Univ Basel Triazine, pyrimidine and pyridine analogues and their use in therapy
CN102625708A (zh) 2009-09-09 2012-08-01 阿维拉制药公司 Pi3激酶抑制剂及其用途
JP2013508401A (ja) 2009-10-22 2013-03-07 ジェネンテック， インコーポレイテッド 軸索変性の調節
GB201004200D0 (en) 2010-03-15 2010-04-28 Univ Basel Spirocyclic compounds and their use as therapeutic agents and diagnostic probes
NZ603644A (en) 2010-05-24 2014-10-31 Univ Rochester Bicyclic heteroaryl kinase inhibitors and methods of use
JP2014511395A (ja) * 2011-03-09 2014-05-15 セルジーン アヴィロミクス リサーチ， インコーポレイテッド Ｐｉ３キナーゼインヒビターおよびその使用
MA42164B1 (fr) 2013-05-01 2019-12-31 Hoffmann La Roche Composes biheteroaryle et leurs utilisations
CN103483345B (zh) 2013-09-25 2016-07-06 中山大学 Pi3k激酶抑制剂、包含其的药物组合物及其应用
JP5920747B1 (ja) 2015-04-07 2016-05-18 エイピーエス．エスエイ アプリケーションプログラムおよびカード

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