ES2530519T3 - Compuestos macrocíclicos completamente sintéticos, con conformación restringida - Google Patents

Compuestos macrocíclicos completamente sintéticos, con conformación restringida Download PDF

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ES2530519T3
ES2530519T3 ES09781527T ES09781527T ES2530519T3 ES 2530519 T3 ES2530519 T3 ES 2530519T3 ES 09781527 T ES09781527 T ES 09781527T ES 09781527 T ES09781527 T ES 09781527T ES 2530519 T3 ES2530519 T3 ES 2530519T3
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cr29r30
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Daniel Obrecht
Philipp Ermert
Said Oumouch
Franck Lach
Anatol Luther
Karsten Marx
Kerstin Möhle
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Abstract

Compuestos de fórmula I, que incorporan los bloques componentes A, B y C.**Fórmula** en las que los restos a, b y c de los bloques componentes A, B y C son seleccionados de las tablas 1, 2 y 3, respectivamente, y son apropiadamente sustituidos independientemente, tal como se define a continuación,**Fórmula** en las que los sustituyentes R1 a R17 acoplados directamente a los bloques componentes A, B y C, se definen del modo siguiente: R1: H; F; Cl; Br; I; CF3; OCF3; OCHF2; NO2; CN; alquilo; alquenilo; alquinilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; -(CR18R19)qOR20; -(CR18R19)qSR20; -(CR18R19)qNR4R11; -(CR18R19)qOCONR4R11; -(CR18R19)qOCOOR21; -(CR18R19)qNR4COOR21; -(CR18R19)qNR4COR22 ; -(CR18R19)qNR4CONR4R11; -(CR18R19)qNR4SO2R23;-(CR18R19)qNR4SO2NR4R11; -(CR18R19)qCOOR21; -(CR18R19)qCONR4R11; -(CR18R19)qSO2NR4R11; -(CR18R19)qPO(OR21)2; -(CR18R19)qOPO(OR21)2; -(CR18R19)qCOR22; -(CR18R19)qSO2R23; -(CR18R19)qOSO3R21; -(CR18R19)qR24; -(CR18R19)qR25; o -(CR18R19)qR26; R2:H; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; -(CR18R19)qOR20; -(CR18R19)qSR20; -(CR18R19)qNR4R11; -(CR18R19)qOCONR4R11; -(CR18R19)qOCOOR21; -(CR18R19)qNR4COOR21; -(CR18R19)qNR4COR22 ; -(CR18R19)qNR4CONR4R11; -(CR18R19)qNR4SO2R23; -(CR18R19)qNR4SO2NR4R11;-(CR18R19)qCOOR21; -(CR18R19)qCONR4R11; -(CR18R19)qSO2NR4R11; -(CR18R19)qPO(OR21)2; -(CR18R19)qCOR22; -(CR18R19)qSO2R23; -(CR18R19)qR24; -(CR18R19)qR25; o -(CR18R19)qR26; R3: H; CF3; alquilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; R4: H; aqluilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; R5, R7 y R9 se definen independientemente como: H; F; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilaquilo; -(CR18R19)sOR20; -(CR18R19)sSR20; -(CR18R19)sNR4R11; -(CR18R19)sOCONR4R11; -(CR18R19)sOCOOR21; -(CR18R19)sNR4COOR21; -(CR18R19)sNR4COR22 ; -(CR18R19)sNR4CONR4R11; -(CR18R19)sNR4SO2R23; -(CR18R19)sNR4SO2NR4R11; -(CR18R19)qCOOR21; -(CR18R19)qCONR4R11; -(CR18R19)qSO2NR4R11; -(CR18R19)qPO(OR21)2; -(CR18R19)qCOR22; -(CR18R19)qSO2R23; -(CR18R19)qR24; -(CR18R19)qR25; o -(CR18R19)qR26; R6, R8 y R10 se definen independientemente como: H; F; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; o heteroarilaquilo; R11: H; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; -(CR18R19)rOR20; -(CR18R19)rSR20; -(CR18R19)rNR4R27; -(CR18R19)rOCONR4R27; -(CR18R19)rOCOOR2; -(CR18R19)rNR4COOR21; -(CR18R19)rNR4CONR4R27; -(CR18R19)rNR4SO2R23; -(CR18R19)rNR4SO2NR4R27; -(CR18R19)qCOOR21; -(CR18R19)qCONR4R27; -(CR18R19)qCOR22; -(CR18R19)qSO2R23; -(CR18R19)qSO2NR4R27; -(CR18R19)qR24; -(CR18R19)sR25; o -(CR18R19)qR26; R12 y R13 se definen independientemente como H; o alquilo; R14 y R16 se definen independientemente como: H; F; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilaquilo; -(CR18R19)sOR20; -(CR18R19)sNR4R11; -(CR18R19)sNR4COOR21; -(CR18R19)sNR4COR22 ; -(CR18R19)sNR4CONR4R11; -(CR18R19)sNR4SO2R23; -(CR18R19)sNR4SO2NR4R11; -(CR18R19)qCOOR21; -(CR18R19)qCONR4R11; -(CR18R19)qSO2NR4R11; o -(CR18R19)qCOR22; R15 y R17 se definen independientemente como: H; F; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; o heteroarilalquilo; en el que los sustituyentes R1 a R17 se definen del modo siguiente: R18: H; F; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; -(CR29R30)sOR31; -(CR29R30)sSR31; -(CR29R30)sNR28R31; -(CR29R30)sOCONR28R31; -(CR29R30)sOCOOR21; -(CR29R30)sNR28COOR21; -(CR29R30)sNR28COR31; -(CR29R30)sNR28CONR28R31; -(CR29R30)sNR28SO2R23; -(CR29R30)sNR28SO2NR28R31; -(CR29R30)qCOOR21; -(CR29R30)qCONR28R31; -(CR29R30)qSO2NR28R31; -(CR29R30)qPO(OR21)2; -(CR29R30)qCOR31; -(CR29R30)qSO2R23; -(CR29R30)qR24; -(CR29R30)qR25; o -(CR29R30)qR26; R19: H; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; R20: H; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; heteroarilalquilo; -(CR29R30)rOR31; -(CR29R30)rSR31; -(CR29R30)rNR28R31; -(CR29R30)rOCONR28R31; -(CR29R30)rNR28COOR21; -(CR29R30)rNR28COR31; -(CR29R30)rNR28CONR28R31; -(CR29R30)rNR28SO2R23;-(CR29R30)rNR28SO2NR28R31; -(CR29R30)qCOOR21; -(CR29R30)qCONR28R31; -(CR29R30)qSO2NR28R31; -(CR29R30)qCOR31; -(CR29R30)qSO2R23; -(CR29R30)qR24; -(CR29R30)qR25; o -(CR29R30)qR26; R21: alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; R22: alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; -(CR29R30)sOR31; -(CR29R30)sSR31; -(CR29R30)sNR28R31; -(CR29R30)sOCONR28R31; -(CR29R30)sNR28COOR21; -(CR29R30)sNR28COR31 ; -(CR29R30)sNR28CONR28R31; -(CR29R30)sNR28SO2R23; -(CR29R30)sNR28SO2NR28R31; -(CR29R30)sCOOR21; -(CR29R30)sCONR28R31; -(CR29R30)sSO2NR28R31; -(CR29R30)tCOR31; -(CR29R30)sSO2R23; -(CR29R30)tR24; -(CR29R30)tR25; o -(CR29R30)tR26; R23: H; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; o bien -(CR32R33)tR24; R24: arilo, o un grupo opcionalmente sustituido del tipo C6H2R34R35R31; o un grupo heteroarilo, uno de los grupos de fórmulas H1-H34, tal como se muestran a continuación en la Tabla 4:
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Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007079597A1 (en) 2006-01-16 2007-07-19 Polyphor Ltd. Template - fixed peptidomimetics with antimicrobial activity
US8633163B2 (en) 2007-01-29 2014-01-21 Polyphor Ltd. Template-fixed peptidomimetics
AU2007348171B2 (en) 2007-02-28 2012-09-06 Polyphor Ltd. Template-fixed peptidomimetics
ES2530519T3 (es) * 2009-08-05 2015-03-03 Polyphor Ag Compuestos macrocíclicos completamente sintéticos, con conformación restringida
EP2836485B1 (en) * 2012-03-17 2018-01-10 Polyphor Ag Conformationally constrained, fully synthetic macrocyclic compounds
WO2013142873A2 (en) 2012-03-23 2013-09-26 The Board Of Trustees Of The University Of Illinois Complex and structurally diverse compounds
TWI655213B (zh) 2012-07-13 2019-04-01 目立康股份有限公司 自我組織化肽衍生物的製造方法
EP3041934A1 (en) 2013-09-03 2016-07-13 Moderna Therapeutics, Inc. Chimeric polynucleotides
EP3215519A1 (en) 2014-11-06 2017-09-13 Novartis AG Amatoxin derivatives and conjugates thereof as inhibitors of rna polymerase
JP2015155430A (ja) * 2015-04-02 2015-08-27 ポリフォー・アクチェンゲゼルシャフトＰｏｌｙｐｈｏｒ Ａｇ コンホメーションを固定された、合成マクロ環化合物
WO2017063756A1 (en) * 2015-10-12 2017-04-20 Polyphor Ag Conformationally constrained macrocyclic compounds as pin1 modulators
WO2017063757A1 (en) 2015-10-12 2017-04-20 Polyphor Ag Conformationally constrained macrocyclic compounds
WO2017063754A1 (en) 2015-10-12 2017-04-20 Polyphor Ag Conformationally constrained macrocyclic compounds as pin1 modulators
WO2017063755A1 (en) 2015-10-12 2017-04-20 Polyphor Ag Conformationally constrained macrocyclic compounds
US10464969B2 (en) 2016-05-05 2019-11-05 Novartis Ag Amatoxin derivatives and conjugates thereof as inhibitors of RNA polymerase
JP2017160247A (ja) * 2017-05-10 2017-09-14 ポリフォー・アクチェンゲゼルシャフトＰｏｌｙｐｈｏｒ Ａｇ コンホメーションを固定された、合成マクロ環化合物
US11267809B2 (en) 2017-09-14 2022-03-08 The Board Of Trustees Of The Leland Stanford Junior University BAF complex modulating compounds and methods of using the same
WO2020014524A1 (en) 2018-07-12 2020-01-16 The Board Of Trustees Of The Leland Stanford Junior University Methods for reversing hiv latency using baf complex modulating compounds
CN113121567A (zh) * 2021-04-22 2021-07-16 中国科学院大学 分子内正交结构的环状三吡咯化合物的合成方法
CN115057848B (zh) * 2022-08-04 2023-08-18 江苏师范大学 一种轴手性异吡喃酮-吲哚衍生物及其合成方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5734012A (en) 1996-05-16 1998-03-31 Ohmeda Pharmaceutical Products Division Inc. Cyclic motilin-like polypeptides with gastrointestinal motor stimulating activity
SK14192002A3 (sk) * 2000-04-05 2003-03-04 Schering Corporation Makrocyklické zlúčeniny, farmaceutický prostriedok s ich obsahom a ich použitie
DK1633774T3 (da) * 2003-06-18 2010-05-25 Tranzyme Pharma Inc Makrocykliske motilinreceptorantagonister
EP2004166A2 (en) 2006-03-31 2008-12-24 La Jolla Pharmaceutical Company Inhibitors of semicarbazide-sensitive amine oxidase (ssao) and vap-1 mediated adhesion useful for treatment and prevention of diseases
ES2530519T3 (es) * 2009-08-05 2015-03-03 Polyphor Ag Compuestos macrocíclicos completamente sintéticos, con conformación restringida

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