AR101198A1 - Pirimidinas 2,5-sustituidas como inhibidores de pde4b - Google Patents

Pirimidinas 2,5-sustituidas como inhibidores de pde4b

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AR101198A1
AR101198A1 ARP150102233A ARP150102233A AR101198A1 AR 101198 A1 AR101198 A1 AR 101198A1 AR P150102233 A ARP150102233 A AR P150102233A AR P150102233 A ARP150102233 A AR P150102233A AR 101198 A1 AR101198 A1 AR 101198A1
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Argentina
Prior art keywords
alkyl
alkylene
co2h
cycloalkyl
alkoxy
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ARP150102233A
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English (en)
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Dr Hesslinger Christian
Dr Craan Tobias
Dr Konetzki Ingo
Dr Jakob Florian
Dr Nardi Antonio
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Gruenenthal Gmbh
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Publication of AR101198A1 publication Critical patent/AR101198A1/es

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Abstract

Su uso como medicamentos, en particular como medicamentos para el tratamiento de condiciones y enfermedades que se pueden tratar por inhibición de la enzima PDE4. Reivindicación 1: Pirimidinas 2,5-sustituidas caracterizadas porque tienen la fórmula general (1), en donde A, B, C en forma independiente entre sí significan N o CH; R¹ significa C₁₋₆-alquilo, C₁₋₆-hidroxialquilo, C₁₋₆-haloalquilo, C₃₋₆-cicloalquilo, SOˣ-C₁₋₆-alquilo, CONH₂, CONH-C₁₋₆-alquilo, CON(C₁₋₆-alquilo)₂; x es 0, 1 ó 2; G es un fenilo o heteroarilo de 5 ó 6 miembros opcionalmente sustituido con al menos un sustituyente Y que contiene al menos un átomo de oxígeno, azufre o nitrógeno, donde los átomos de nitrógeno presentes en el heteroarilo pueden estar sustituidos con R⁴; R⁴ es hidrógeno, C₁₋₆-alquilo, C₁₋₆-haloalquilo, CO-C₁₋₆-alquilo, SO-C₁₋₆-alquilo, SO₂-C₁₋₆-alquilo; Y es OH, CN, SH, C₁₋₆-alquilo, C₂₋₆-alquenilo, C₂₋₆-alquinilo, C₃₋₆-cicloalquilo, C₁₋₆-alcoxi, C₁₋₆-tioalquilo, C₁₋₆-haloalquilo, C₁₋₆-tiohaloalquilo, C₁₋₆-haloalcoxi, CO₂H, CO₂-C₁₋₆-alquilo, CHO, CO-C₁₋₆-alquilo, OCO-C₁₋₆-alquilo, CONH₂, CONH-C₁₋₆-alquilo, CON(C₁₋₆-alquilo)₂, OCO-NH-C₁₋₆-alquilo, OCO-N(C₁₋₆-alquilo)₂, NH₂, NH-C₁₋₆-alquilo, N(C₁₋₆-alquilo)₂, N-pirrolidinilo, N-piperidinilo, N-morfolinilo, NH-CO-C₁₋₆-alquilo, NH-CO₂-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO₂-C₁₋₆-alquilo, NH-CO-NH₂, NH-CO-NH-C₁₋₆-alquilo, NH-CO-N(C₁₋₆-alquilo)₂, N-C₁₋₆-alquil-CO-NH₂, N-C₁₋₆-alquil-CO-NH-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO-N(C₁₋₆-alquilo)₂, NH-SO₂-C₁₋₆-alquilo, N-C₁₋₆-alquil-SO₂-C₁₋₆-alquilo, S-C₁₋₆-alquilo, SO-C₁₋₆-alquilo, SO₂-C₁₋₆-alquilo, SO₂H, SO₂OH, SO₂NH₂, SO₂NH-C₁₋₆-alquilo, SO₂N(C₁₋₆-alquilo)₂, C(=N)-NH, NHC(=N)-NH₂, -N=C=O, -S-CN, donde las cadenas alquilo mencionadas, precedentemente pueden estar sustituidas con al menos uno de los siguientes sustituyentes: OH, CN, C₃₋₆-cicloalquilo, C₁₋₆-alcoxi, CO₂H, CO₂-C₁₋₆-alquilo o -NH₂; R² y R³ en forma independiente entre sí significan hidrógeno o C₁₋₆-alquilo, C₁₋₆-haloalquilo, C₁₋₆-hidroxialquilo, C₁₋₆-alcoxi-C₁₋₆-alquileno, C₁₋₆-alquilen-CO₂H, C₁₋₆-alquilen-CO₂-C₁₋₆-alquilo, C₁₋₆-alquilen-CONH₂, C₁₋₆-alquilen-CONH-C₁₋₆-alquilo, C₁₋₆-alquilen-CON(C₁₋₆-alquilo)₂, C₁₋₆-alquilen-C₃₋₆-cicloalquilo, C₁₋₆-hidroxialquil-C₃₋₆-cicloalquileno opcionalmente sustituido, un grupo L¹V, un grupo L²W, o R² y R³ junto con el átomo de nitrógeno al cual están unidos forman un residuo heteroalifático monocíclico o bicíclico de entre 3 y 12 miembros opcionalmente sustituido con al menos un sustituyente XQ Q que puede contener adicionalmente al menos un átomo de oxígeno, azufre o nitrógeno adicional, donde estos átomos de nitrógeno adicionales están sustituidos con R⁵; XQ en forma independiente entre sí significan =O (carbonilo), halógeno, OH, CN, SH, C₁₋₆-alquilo, C₁₋₆-hidroxialquilo, C₁₋₆-cianoalquilo, C₂₋₆-alquenilo, C₂₋₆-alquinilo, C₃₋₆-cicloalquilo, C₁₋₆-alcoxi, C₁₋₆-alcoxi-C₁₋₆-alquileno, C₁₋₆-tioalquilo, C₁₋₆-haloalquilo, C₁₋₆-tiohaloalquilo, C₁₋₆-haloalcoxi, -NH₂, NH-C₁₋₆-alquilo, N(C₁₋₆-alquilo)₂, C₁₋₆-alquilen-NH-C₁₋₆-alquilo, C₁₋₆-alquilen-N(C₁₋₆-alquilo)₂, NH-CHO, NH-CO-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO-C₁₋₆-alquilo, NH-CO-O-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO-O-C₁₋₆-alquilo, NH-CO-NH₂, NH-CO-NH-C₁₋₆-alquilo, NH-CO-N(C₁₋₆-alquilo)₂, N-C₁₋₆-alquil-CO-NH₂, N-C₁₋₆-alquil-CO-NH-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO-N(C₁₋₆-alquilo)₂, NH-SO₂-C₁₋₆-alquilo, N-C₁₋₆-alquil-SO₂-C₁₋₆-alquilo, CO₂H, CO₂-C₁₋₆-alquilo, CHO, CO-C₁₋₆-alquilo, O-CO-C₁₋₆-alquilo, CO-NH₂, CO-NH-C₁₋₆-alquilo, CO-N(C₁₋₆-alquilo)₂, O-CO-NH-C₁₋₆-alquilo, O-CO-N(C₁₋₆-alquilo)₂, S-C₁₋₆-alquilo, SO-C₁₋₆-alquilo, SO₂-C₁₋₆-alquilo, SOOH, SO₂OH, SO₂NH₂, SO₂NH-C₁₋₆-alquilo, SO₂N(C₁₋₆-alquilo)₂, C(=N)-NH, NHC(=N)-NH₂, -N=C=O, -S-CN, donde las cadenas alquilo mencionadas precedentemente pueden estar sustituidas con al menos uno de los siguientes sustituyentes: OH, CN, C₃₋₆-cicloalquilo, C₁₋₆-alcoxi, CO₂H, CO₂-C₁₋₆-alquil-CO-C₁₋₆-alquilo, NH-CO-O-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO-O-C₁₋₆-alquilo, NH-CO-NH₂, NH-CO-NH-C₁₋₆-alquilo, NH-CO-N-C₁₋₆-alquilo)₂, N-C₁₋₆-alquil-CO-NH₂, N-C₁₋₆-alquil-CO-NH-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO-N(C₁₋₆-alquilo)₂, NH-SO₂-C₁₋₆-alquilo, N-C₁₋₆-alquil-SO₂-C₁₋₆-alquilo, CO₂H, CO₂-C₁₋₆-alquilo, CHO, CO-C₁₋₆-alquilo, O-CO-C₁₋₆-alquilo, CO-NH₂, CO-NH-C₁₋₆-alquilo, CO-N(C₁₋₆-alquilo)₂, O-CO-NH-C₁₋₆-alquilo, O-CO-N(C₁₋₆-alquilo)₂, S-C₁₋₆-alquilo, SO-C₁₋₆-alquilo, SO₂-C₁₋₆-alquilo, SOOH, SO₂OH, SO₂NH₂, SO₂NH-C₁₋₆-alquilo, SO₂N(C₁₋₆-alquilo)₂, C(=N)-NH, NHC(=N)-NH₂, -N=C=O, -S-CN, donde las cadenas alquilo mencionadas precedentemente pueden estar sustituidas con al menos uno de los siguientes sustituyentes: OH, CN, C₃₋₆-cicloalquilo, C₁₋₆-alcoxi, CO₂H, CO₂-C₁₋₆-alquilo o -NH₂; R⁶ es hidrógeno, C₁₋₆-alquilo, C₁₋₆-haloalquilo, CO-C₁₋₆-alquilo, SO-C₁₋₆-alquilo, SO₂-C₁₋₆-alquilo; L² es una unión o un grupo C₁₋₆-alquileno de cadena ramificada o lineal opcionalmente sustituido conectado al nitrógeno de amida; W es un fenilo o heteroarilo de 5 ó 6 miembros opcionalmente sustituido con al menos un sustituyente Z que contiene al menos un átomo de oxígeno, azufre o nitrógeno; y Z en forma independiente entre sí significan halógeno, OH, CN, SH, C₁₋₆-alquilo, C₂₋₆-alquenilo, C₂₋₆-alquinilo, C₃₋₆-cicloalquilo, C₁₋₆-alcoxi, C₁₋₆-tioalquilo, C₁₋₆-haloalquilo C₁₋₆-tiohaloalquilo, C₁₋₆-haloalcoxi, -NH₂, NH-C₁₋₆-alquilo, N(C₁₋₆-alquilo)₂, N-pirrolidinilo, N-piperidinilo, N-morfolinilo, NH-CHO, NH-CO-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO-C₁₋₆-alquilo, NH-CO₂-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO₂-C₁₋₆-alquilo, NH-CO-NH₂, NH-CO-NH-C₁₋₆-alquilo, NH-CO-N(C₁₋₆-alquilo)₂, N-C₁₋₆-alquil-CO-NH₂, N-C₁₋₆-alquil-CO-NH-C₁₋₆-alquilo, N-C₁₋₆-alquil-CO-N(C₁₋₆-alquilo)₂, NH-SO₂-C₁₋₆-alquilo, N-C₁₋₆-alquil-SO₂-C₁₋₆-alquilo, CO₂H, CO₂-C₁₋₆-alquilo, CHO, CO-C₁₋₆-alquilo, O-CO-C₁₋₆-alquilo, CO-NH₂, CO-NH-C₁₋₆-alquilo, CO-N(C₁₋₆-alquilo)₂, O-CO-NH-C₁₋₆-alquilo, O-CO-N(C₁₋₆-alquilo)₂-, S-C₁₋₆-alquilo, SO-C₁₋₆-alquilo, SO₂-C₁₋₆-alquilo, SO₂H, SO₂OH, SO₂NH₂, SO₂NH-C₁₋₆-alquilo, SO₂N(C₁₋₆-alquilo)₂, C(=N)-NH, NHC(=N)-NH₂, -N=C=O, -S-CN, donde las cadenas alquilo mencionadas precedentemente pueden estar sustituidas con al menos uno de los siguientes sustituyentes: OH, CN, C₃₋₆-cicloalquilo, C₁₋₆-alcoxi, CO₂H, CO₂-C₁₋₆-alquilo o -NH₂.
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AR101196A1 (es) * 2014-07-16 2016-11-30 Gruenenthal Gmbh Compuestos de pirimidina sustituidos
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US11963823B2 (en) 2016-10-03 2024-04-23 Koninklijke Philips N.V. Radiopaque arrangement of electronic components in intra-cardiac echocardiography (ICE) catheter
CN108570052A (zh) * 2017-03-13 2018-09-25 中国科学院上海药物研究所 五元杂环并吡嗪化合物、制备方法、中间体、组合和应用
WO2018234353A1 (en) 2017-06-20 2018-12-27 Grünenthal GmbH NOVEL SUBSTITUTED INDOLE AND INDAZOLE COMPOUNDS AS INHIBITORS OF PHOSPHODIESTERASE
WO2018234354A1 (en) 2017-06-20 2018-12-27 Grünenthal GmbH NOVEL SUBSTITUTED 3-INDOLE AND 3-INDAZOLE COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS
WO2020083878A1 (en) * 2018-10-25 2020-04-30 Merck Patent Gmbh 5-azaindazole derivatives as adenosine receptor antagonists
CN110156785B (zh) * 2019-04-15 2020-08-28 浙江大学 吲唑类化合物及其制备方法和应用
EP4255904A2 (en) * 2020-12-03 2023-10-11 Domain Therapeutics Novel par-2 inhibitors
CN115108992B (zh) * 2022-06-29 2024-05-31 浙江手心制药有限公司 6-氯-2-甲基-2h-吲唑-5-胺的制备方法

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3818830A1 (de) 1988-06-03 1989-12-14 Boehringer Mannheim Gmbh Bicyclische carboxamide, verfahren zu ihrer herstellung, deren vorstufen, und diese verbindungen enthaltende arzneimittel
CA2165192C (en) 1993-07-02 2001-04-24 Hermann Amschler Fluoroalkoxy-substituted benzamides and their use as cyclic nucleotide phosphodiesterase inhibitors
JP2000198734A (ja) * 1998-12-30 2000-07-18 Pfizer Inc 胃運動性減弱および関連疾患の治療のための運動性増強薬
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
AU7683500A (en) * 1999-10-12 2001-04-23 Takeda Chemical Industries Ltd. Pyrimidine-5-carboxamide compounds, process for producing the same and use thereof
JP2001233875A (ja) * 1999-10-12 2001-08-28 Takeda Chem Ind Ltd ピリミジン−５−カルボキサミド化合物、その製造法およびその用途
US6436965B1 (en) 2000-03-02 2002-08-20 Merck Frosst Canada & Co. PDE IV inhibiting amides, compositions and methods of treatment
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
DE10163991A1 (de) 2001-12-24 2003-07-03 Merck Patent Gmbh Pyrrolo-pyrimidine
EP2489659B1 (en) 2004-06-24 2017-12-13 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US8354427B2 (en) 2004-06-24 2013-01-15 Vertex Pharmaceutical Incorporated Modulators of ATP-binding cassette transporters
US20060293343A1 (en) 2005-05-18 2006-12-28 Asahi Kasei Pharma Corporation Pyrimidine derivatives
US8580802B2 (en) 2005-09-30 2013-11-12 Vertex Pharmaceuticals Incorporated Pyrrolo[2,3-D]pyrimidines as inhibitors of Janus kinases
BRPI0621226A2 (pt) * 2006-01-19 2012-07-10 Orchid Reseach Lab Ltd compostos heterociclos
US7863446B2 (en) 2006-01-19 2011-01-04 Orchid Research Laboratories Limited Heterocycles
EP1958947A1 (en) 2007-02-15 2008-08-20 Ranbaxy Laboratories Limited Inhibitors of phosphodiesterase type 4
TW201512189A (zh) 2013-04-16 2015-04-01 Gruenenthal Chemie 新型被取代之嘧啶縮合化合物
AR101197A1 (es) * 2014-07-16 2016-11-30 Gruenenthal Gmbh Pirimidinas 2,5-sustituidas
AR101198A1 (es) 2014-07-16 2016-11-30 Gruenenthal Gmbh Pirimidinas 2,5-sustituidas como inhibidores de pde4b
AR101196A1 (es) * 2014-07-16 2016-11-30 Gruenenthal Gmbh Compuestos de pirimidina sustituidos

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