ES2589558T3 - Derivados de pirimidin pirazolilo - Google Patents

Derivados de pirimidin pirazolilo Download PDF

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Publication number
ES2589558T3
ES2589558T3 ES13737134.0T ES13737134T ES2589558T3 ES 2589558 T3 ES2589558 T3 ES 2589558T3 ES 13737134 T ES13737134 T ES 13737134T ES 2589558 T3 ES2589558 T3 ES 2589558T3
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Stefano Crosignani
Catherine Jorand-Lebrun
Patrick Gerber
Mathilde Muzerelle
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Ares Trading SA
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Ares Trading SA
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    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • A61K31/53751,4-Oxazines, e.g. morpholine
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  • Plural Heterocyclic Compounds (AREA)

Abstract

Un compuesto de Fórmula (I)**Fórmula** en donde R1 denota ausencia o denota A o Q-Het, Z denota un grupo: en donde X denota O, S o N, Y denota C o N, T denota C o N, o Z denota una piridina o un grupo piridazina, Ra está ausente o denota OR3, CF3, Hal, NO2, Rb está ausente o denota uno de los grupos seleccionados de A y COHet, R2 denota H, Het, Q-Het, Cyc, A o OA, Het denota un anillo monocíclico de 4-9 miembros o un anillo bicíclico fusionado, espiro o puenteado, que es saturado, insaturado o aromático, que contiene 1 a 3 heteroátomos seleccionados independientemente de N, O, S y un grupo CO, SO o SO2, y en donde 1 o átomos de H pueden ser reemplazados por A, OA, COA, CN, Hal, NO2, OR3, SOA y/o SO2A, Cyc denota un anillo carbocíclico saturado de 4-8 que contiene opcionalmente SO, SO2, CO, y opcionalmente sustituido una vez o dos veces por un grupo seleccionado de CO(NR3)2, y COHet, OR3, Het1, A, CH2Het1, NH2, NHCOA, OCH2Cyc1, SO2A y/o -SA(>=NH)(>=O), Q denota un alquileno lineal o ramificado, que tiene 1 a 6 átomos de carbono en donde 1 a 5 átomos de H pueden ser reemplazados por un grupo seleccionado independientemente de OR3, Hal, N(R3)2, y en donde 1 o 2 grupos CH2 pueden ser reemplazados por un grupo seleccionado independientemente de CO, SO, SO2 y NR3, o Q denota un anillo heterocíclico bivalente de 4-8 miembros, que es saturado, insaturado o aromático y que contiene 1 a 3 heteroátomos seleccionados independientemente de N, O y S, A denota un alquilo lineal o ramificado que tiene de 1 a 10 átomos de carbono en donde 1 a 7 átomos de H pueden ser reemplazados por un grupo seleccionado independientemente de -OR3, Hal, NHSO2A, SO2A, SOA, N(R3)2, y en donde 1, 2 o 3 grupos -CH2- no adyacentes pueden ser reemplazados por un grupo seleccionado independientemente de -CO-, NR3 y/o -O-, Hal denota F, Cl, Br o I, R3 denota H o C1-C6-alquilo en donde 1 átomo de H puede ser reemplazado por un grupo seleccionado de OH, OC1- C6-alquilo, y Hal, Het1 denota un heterociclo monocíclico saturado de cinco o seis miembros que contiene 1-3 átomos de N y/u O, que opcionalmente es monosustituido por A, Cyc1 denota cicloalquilo con 3-7 átomos, y solvatos, tautómeros, sales, hidratos y estereoisómeros farmacéuticamente aceptables de los mismos, incluyendo mezclas de los mismos en todas las proporciones.
ES13737134.0T 2012-07-10 2013-07-03 Derivados de pirimidin pirazolilo Active ES2589558T3 (es)

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Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10314841B2 (en) 2014-01-09 2019-06-11 Merck Patent Gmbh Substituted pyrazoles as IRAK inhibitors
CN106163521B (zh) * 2014-03-27 2021-02-09 艾科西斯有限责任公司 有效的可溶性环氧化物水解酶抑制剂
CA2964982C (en) * 2014-11-20 2022-07-05 Merck Patent Gmbh Heteroaryl compounds as irak inhibitors and uses thereof
CN105153211B (zh) * 2015-09-22 2017-02-01 上海晋鲁医药科技有限公司 一种合成1‑(N‑Boc‑4‑哌啶)‑4‑吡唑硼酸频哪醇酯的方法
EP3423446B1 (de) 2016-03-03 2020-09-16 Bayer Pharma Aktiengesellschaft Neue 2-substituierte indazole, verfahren zu ihrer herstellung, pharmazeutische präparate die diese enthalten, sowie deren verwendung zur herstellung von arzneimitteln
TW202340194A (zh) 2017-02-16 2023-10-16 美商基利科學股份有限公司 吡咯并[1,2-b]嗒𠯤衍生物
JP7282039B2 (ja) 2017-03-16 2023-05-26 セルジーン シーエーアール エルエルシー Mk2阻害剤、その合成、およびそれに至るまでの中間体
CN106967073A (zh) * 2017-04-24 2017-07-21 刘双伟 一种治疗类风湿性关节炎的药物
CN106946891B (zh) * 2017-05-08 2018-07-13 宿州市徽腾知识产权咨询有限公司 一种用于治疗类风湿性关节炎的药物
WO2019060693A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES THEREOF
MX2020003190A (es) 2017-09-22 2020-11-11 Kymera Therapeutics Inc Degradadores de proteinas y usos de los mismos.
WO2019111218A1 (en) 2017-12-08 2019-06-13 Cadila Healthcare Limited Novel heterocyclic compounds as irak4 inhibitors
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
WO2019140380A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Protein degraders and uses thereof
WO2019140387A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
WO2020010227A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Protein degraders and uses thereof
US11292792B2 (en) 2018-07-06 2022-04-05 Kymera Therapeutics, Inc. Tricyclic CRBN ligands and uses thereof
TWI842978B (zh) 2018-07-13 2024-05-21 美商基利科學股份有限公司 衍生物
JP7186874B2 (ja) * 2018-10-26 2022-12-09 アーリーン ファーマシューティカルズ エルエルシー ピラゾリル化合物およびその使用方法
JP7623943B2 (ja) 2018-11-30 2025-01-29 カイメラ セラピューティクス, インコーポレイテッド Irak分解剤およびそれらの使用
BR112021026517A2 (pt) 2019-06-28 2022-05-10 Kymera Therapeutics Inc Degradadores de irak e usos dos mesmos
WO2021011868A1 (en) 2019-07-17 2021-01-21 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2021099406A1 (en) * 2019-11-20 2021-05-27 F. Hoffmann-La Roche Ag Spiro(isobenzofuranazetidine) compounds for the treatment of autoimmune disease
US12551564B2 (en) 2019-12-10 2026-02-17 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
WO2021127190A1 (en) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2021127283A2 (en) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Irak degraders and uses thereof
CN110950839B (zh) * 2019-12-17 2023-04-14 蚌埠中实化学技术有限公司 4-(4-卤代-1h-吡唑-1-基)哌啶-1-羧酸叔丁酯的制备方法
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
PH12023500015A1 (en) 2020-12-30 2024-03-11 Kymera Therapeutics Inc Irak degraders and uses thereof
KR20230142529A (ko) * 2021-02-01 2023-10-11 셀진 코포레이션 Mk2 억제제, 이의 합성, 및 이의 중간체
WO2022174268A1 (en) 2021-02-15 2022-08-18 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof
AU2022271290A1 (en) 2021-05-07 2023-11-23 Kymera Therapeutics, Inc. Cdk2 degraders and uses thereof
US12187744B2 (en) 2021-10-29 2025-01-07 Kymera Therapeutics, Inc. IRAK4 degraders and synthesis thereof
EP4472967A4 (en) 2022-01-31 2026-04-15 Kymera Therapeutics Inc Iraqi Degradation Agents and Their Uses
EP4551218A2 (en) * 2022-07-07 2025-05-14 Dana-Farber Cancer Institute, Inc. Potent and selective irreversible inhibitors of irak1
CN115490621B (zh) * 2022-10-14 2024-06-21 浙江工业大学 一种碘代双环[1.1.1]戊烷衍生物的制备方法

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5559137A (en) * 1994-05-16 1996-09-24 Smithkline Beecham Corp. Compounds
NZ526472A (en) * 2000-12-21 2004-04-30 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors
US7659270B2 (en) * 2006-08-11 2010-02-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
DE102008025750A1 (de) * 2008-05-29 2009-12-03 Merck Patent Gmbh Dihydropyrazolderivate
DE102008062825A1 (de) * 2008-12-23 2010-06-24 Merck Patent Gmbh 3-(3-Pyrimidin-2-yl-benzyl)-[1,2,4]triazolo [4,3-b]pyridazin-derivate
WO2010100144A1 (en) 2009-03-04 2010-09-10 Merck Serono S.A. Fused bicyclic compounds as inhibitors for pi3 kinase
EP2414337B1 (en) * 2009-04-03 2013-05-01 Cellzome GmbH Methods for the identification of kinase interacting molecules and for the purification of kinase proteins
DE102009033208A1 (de) * 2009-07-15 2011-01-20 Merck Patent Gmbh Aminopyridinderivate
JP2013514973A (ja) * 2009-12-21 2013-05-02 メルク・シャープ・エンド・ドーム・コーポレイション チロシンキナーゼ阻害剤
JP5985473B2 (ja) * 2010-07-13 2016-09-06 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft IRAK4モジュレーターとしてのピラゾロ[1,5a]ピリミジン及びチエノ[3,2b]ピリミジン誘導体

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