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AR058401A1 - Pirimidinas sustituidas con sulfoximinas proceso para su produccion y uso de las mismas como farmacos - Google Patents

Pirimidinas sustituidas con sulfoximinas proceso para su produccion y uso de las mismas como farmacos

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Publication number
AR058401A1
AR058401A1 ARP060105693A ARP060105693A AR058401A1 AR 058401 A1 AR058401 A1 AR 058401A1 AR P060105693 A ARP060105693 A AR P060105693A AR P060105693 A ARP060105693 A AR P060105693A AR 058401 A1 AR058401 A1 AR 058401A1
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AR
Argentina
Prior art keywords
group
alkyl
alkoxy
nr8r9
halogen
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ARP060105693A
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English (en)
Inventor
Konrad Krolikiewicz
Ahsen Oliver Von
Martin Krueger
Hans Briem
Georg Kettschau
Ulrich Luecking
Ingo Hartung
Duy Nguyen
Anne Mengel
Bonin Arne Von
Olaf Prien
Ulf Boemer
Ulrich Bothe
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Schering Ag
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Application filed by Schering Ag filed Critical Schering Ag
Publication of AR058401A1 publication Critical patent/AR058401A1/es

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Abstract

La presente se relaciona con pirimidinas sustituidas con sulfoximinas de la formula general (1), procesos para su preparacion, uso como fármacos y composiciones farmacéuticas que las contienen. Reivindicacion 1: Compuestos caracterizado porque responde a la formula general (1), donde R1 significa un grupo heteroarilo monocíclico o bicíclico, opcionalmente total o parcialmente hidrogenado, opcionalmente sustituido, o un grupo arilo opcionalmente sustituido; R2 un átomo de hidrogeno, un grupo alquilo C1-10, un grupo alquenilo C2-10, un grupo alquinilo C2-10, un grupo cicloalquilo C3-8, un grupo heterociclilo C3-8, un grupo arilo o heteroarilo, que está opcionalmente sustituido una o más veces, de forma idéntica o diferente, con un grupo seleccionado entre halogeno, hidroxi, ciano, SO2NR8R9, SO2R10, S(O)(NR8)R9, alquilo C1-6, perfluoroalquilo C1-6, hidroxialquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, alcoxi C1-6-alquilo C1-6, alcoxi C1-6-alcoxi C1-6-alquilo C1-6, - COR6, -alquilo C1-6(CO) alquilo C1-6, -COO-alquil C1-6-O-alquilo C1-6, alquil C1-6 (CO)O-, cicloalquilo C3-10, =N-OH, -NR8R9, -NH-alquilo C1-6, -N(alquil C1-6)2, -NH(CO) alquilo C1-6, -N[(CO)(alquil C1-6)]2, -NH(CO) alquilen C1-6-NH-(CO)arilo, - NH(CO)(alquilen C1-6)arilo, -NH-(CH2)n-cicloalquilo C3-10, -(CH2)narilo, -(CH2)n-O-arilo, -(CH2)n-heteroarilo, -(CH2)n-heterociclilo C3-8, -CF3, -OCF3, -NR7-C(O)-O alquilo C1-3, -NR7-C(O)-NR8R9 o -NR7-SO2-R10, donde, si el grupo cicloalquilo C3-10, el grupo (CH2)n-heterociclilo C3-8, el grupo (CH2)narilo o (CH2)n-heteroarilo son sustituyentes de R2, estos a su vez pueden estar opcionalmente sustituidos una o más veces, de forma idéntica o diferente, con halogeno, hidroxi, alquilo C1-6, halogeno-alquilo C1-4, alcoxi C1-6, -O-(CH2)o-O-, halogeno alcoxi C1-4, -(CH2)narilo, NR8R9, COOR7 o SO2NR8R9, y/o el anillo de cualquier grupo cicloalquilo C3-10, grupo heterociclilo C3-8 el grupo alquilo C1-10 pueden contener opcionalmente uno o varios -NR8, átomos de oxígeno y/o azufre y/o pueden contener opcionalmente uno o varios grupos -C(O)-en el anillo y/o opcionalmente el anillo puede incluir uno o varios posibles enlaces dobles; n significa 0-6; o significa 1-4; R3 hidroxi, halogeno, nitro, ciano, -(CO)NR8R9, -(CS)NR8R9, CF3, OCF3, -R9N(CO)NR8R9, -R7N(CO)R8, -R7NS(O)2R8 , el grupo -NR8R9 o un grupo alquilo C1-6, un grupo cicloalquilo C3-7 o un grupo alcoxi C1-6, que está opcionalmente sustituido una o más veces, de forma idéntica o diferente, con halogeno, hidroxi, alcoxi C1-6 o el grupo -NR8R9; R4 un átomo de hidrogeno, un grupo -C(O)O-R10, -C(O)-R10, -C(O)-NR8R9, -C(S)-NR8R9, NO2, -Si(R15R16R17), -R18-Si(R15R16R17), -SO2-R18-Si(R15R16R17) o un grupo -SO2R10 o un grupo alquilo C1-10, cicloalquilo C3-10, alquenilo C2-10, o alquinilo C2-10, que está opcionalmente sustituido una o más veces, de forma idéntica o diferente, con hidroxi, halogeno, alcoxi C1-6, alquiltio C1-6, ciano, cicloalquilo C3-10, hidroxialquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6-alquilo C1-6, alcoxi C1-6-alcoxi C1-6-alquilo C1-6, -COR6, -CSR6, -CF3, -OCF3 o -NR8R9 o un grupo -(CH2)n-arilo o -(CH2)n-heteroarilo opcionalmente sustituido o R3 y R5 juntos forman un anillo de entre 5 y 7 miembros, donde el anillo puede estar opcionalmente sustituido una o más veces, de forma idéntica o diferente, con hidroxi, alquilo C1-6, alcoxi C1-6, halogeno o el grupo -NR8R9 y puede contener 1-2 enlaces dobles y R3 y el residuo sulfoximina deben estar conectados en posiciones adyacentes de Q; R4 y R5 juntos forman un anillo de entre 5 y 8 miembros de la formula (2), donde V, W e Y representan en forma independiente entre sí un grupo -CH2 que está opcionalmente sustituido una o más veces, de forma idéntica o diferente, con hidroxi, alquilo C1-10, alcoxi C1-10 o -NR8R9, donde el grupo alquilo C1-10 o alcoxi C1-10 de la misma manera puede estar sustituido una o más veces, de forma idéntica o diferente, con hidroxi, alcoxi C1-6 o NR8R9 y/o el anillo puede estar interrumpido por uno o varios grupos -C(O)- y/o opcionalmente puede contener uno o varios enlaces dobles, y R5 un grupo alquilo C1-6, alquenilo C2-6, alquinilo C2-6, o cicloalquilo C3-7 que está opcionalmente sustituido una o más veces, de forma idéntica o diferente, con hidroxi, alcoxi C1-6, cicloalquilo C3-10, halogeno, ciano, -CF3, -OCF3 o el grupo -NR8R9, un grupo arilo o grupo heteroarilo que está opcionalmente sustituido una o más veces, de forma idéntica o diferente, con halogeno, hidroxi, alquilo C1-6, halogeno-alquilo C1-4, alcoxi C1-6, halogeno alcoxi C1-4, -COR6, COOR7, -NR8R9, CN, NO2, o SO2NR8R9; X un átomo de oxígeno, un átomo de azufre o un grupo -NR8- o X y R2 juntos forman un anillo de entre 3 y 8 miembros, que contiene uno o varios heteroátomos, y que está opcionalmente sustituido una o más veces, de forma idéntica o diferente, con hidroxi, alquilo C1-6, alcoxi C1-6, halogeno o el grupo -NR8R9, si X significa un grupo -NR8-; Q arileno C6-10, heteroarileno con 5-10 átomos del anillo; m es 0-4, R6 es un átomo de hidrogeno o un grupo hidroxi, benciloxi o -NR8R9 o un grupo alquilo C1-6, grupo alquenilo C2-6, grupo alquinilo C2-6, grupo alcoxi C1-6, grupo alquiltio C1-6, grupo cicloalquilo C3-7, grupo arilo C5-10 o grupo heteroarilo con 5 o 6 átomos del anillo, que está opcionalmente sustituido una o más veces, de forma idéntica o diferente, con hidroxi, -NR8R9, ciano, halogeno, -CF3, alquilo C1-6, alcoxi C1-6 o -OCF3; R7 es un átomo de hidrogeno o un grupo alquilo C1-6; R8, R9 significan en forma independiente entre sí un átomo de hidrogeno, grupo alcoxi C1-6, un grupo alquilo C1-6, grupo hidroxialquilo C1-6, grupo dihidroxialquilo C1- 6, cicloalquilo C3-7, (CH2)n-NR11R12, NR11R12, -(CO)-alquilo C1-6, -(CO)-fenilo, -(CO)-alquil C1-6-NH-, -(CO)arilo, -(CO)bencilo, -(CO)O-alquilo C1-6, un grupo -(CH2)n-arilo C6-10 o un grupo heteroarilo con 5 o 6 átomos del anillo, que está opcionalmente sustituido una o más veces, de forma idéntica o diferente, con hidroxi, -NR11R12, ciano, halogeno, -CF3, alquilo C1-6, alcoxi C1-6, o -OCF3, o R8y R9 juntos forman un anillo saturado o insaturado de entre 5 y 7 miembros, que puede contener opcionalmente 1-3 heteroátomos adicionales seleccionados entre el grupo oxígeno, azufre, =N-o -NR11- y que está opcionalmente sustituido una o más veces, de forma idéntica o diferente, con hidroxi, -NR11R12, ciano, halogeno, -CF3, alcoxi C1- 6 y/o -OCF3; un grupo alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, heterociclilo C3-10, heteroarilo con 5 o 6 átomos del anillo o un grupo arilo, que está opcionalmente sustituido una o más veces, de forma idéntica o diferente, con halogeno, hidroxi, alquilo C1-6, alcoxi C1-6, ciano, -CF3, -OCF3, -NR8R9 o con el grupo -SiR15R16R17; R11, R12 significan en forma independiente entre sí un átomo de hidrogeno, un grupo alquilo C1-6, alcoxi C1-6-, hidroxialquilo C1-6, dihidroxi- alquilo C1-6, (CO)-alquilo C1-6, (CO)-fenilo, o un grupo bencilo, que está opcionalmente sustituido una o más veces, de forma idéntica o diferente, con hidroxi, ciano, halogeno, -CF3, alcoxi C1-6 y/o -OCF3, o NR11R12 forma un anillo saturado o insaturado de entre 5 y 7 miembros, en donde hasta dos grupos metileno pueden reemplazarse por -O-, -NR7-, o -C(=O)-; R15, R16 y R17 pueden ser en forma independiente entre sí un grupo alquilo C1-6, y/o un grupo fenilo; y R18 representa un grupo alquileno C1-3.
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Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1878726A1 (en) * 2006-07-12 2008-01-16 Bayer Schering Pharma Aktiengesellschaft Substituted sulphoximines as Tie2 inhibitors and salts thereof, pharmaceutical compositions comprising the same, methods of preparing the same and uses of the same
DE102007024470A1 (de) * 2007-05-24 2008-11-27 Bayer Schering Pharma Aktiengesellschaft Neue Sulfoximin-substituierte Chinolin- bzw. Chinazolinderivate als Kinase-Inhibitoren
JP2010527951A (ja) 2007-05-24 2010-08-19 バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト キナーゼ阻害剤としての新規なスルホキシイミン置換型キノリン及びキナゾリン誘導体
BRPI0909036A8 (pt) * 2008-03-03 2018-10-23 Dow Agrosciences Llc pesticidas
EA029131B1 (ru) 2008-05-21 2018-02-28 Ариад Фармасьютикалз, Инк. Фосфорсодержащие производные в качестве ингибиторов киназы
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
EP2179991A1 (de) 2008-10-21 2010-04-28 Bayer Schering Pharma Aktiengesellschaft Sulfoximinsubstituierte Anilino-Pyrimidinderivate als CDK-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
EP2179992A1 (de) 2008-10-21 2010-04-28 Bayer Schering Pharma Aktiengesellschaft Sulfonsubstituierte Anlinopyrimidinderivative als CDK-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
EP2179993A1 (de) 2008-10-21 2010-04-28 Bayer Schering Pharma Aktiengesellschaft Sulfoxidsubstituierte Anilinopyrimidinderivative als CDK-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
MX2012002596A (es) * 2009-09-03 2012-07-03 Allergan Inc Compuestos como moduladores de tirosina cinasas.
US9340555B2 (en) 2009-09-03 2016-05-17 Allergan, Inc. Compounds as tyrosine kinase modulators
DE102010014426A1 (de) * 2010-04-01 2011-10-06 Bayer Schering Pharma Aktiengesellschaft Verwendung neuer pan-CDK-Inhibitoren zur Behandlung von Tumoren
EP2593447B1 (de) 2010-07-15 2016-08-17 Bayer Intellectual Property GmbH 3-pyridyl-heteroarylcarboxamidverbindungen als schädlingsbekämpfungsmittel
DE102010046720A1 (de) * 2010-09-23 2012-03-29 Bayer Schering Pharma Aktiengesellschaft Verfahren zur Herstellung von pan-CDK-Inhibitoren der Formel (l), sowie Intermediate der Herstellung
JP5886411B2 (ja) 2011-03-24 2016-03-16 ノビガ・リサーチ・エービーＮｏｖｉｇａ Ｒｅｓｅａｒｃｈ ＡＢ 新規のピリミジン誘導体
EP2502924A1 (en) * 2011-03-24 2012-09-26 Chemilia AB Novel pyrimidine derivatives
EA201391626A1 (ru) 2011-05-04 2014-03-31 Ариад Фармасьютикалз, Инк. Соединения для ингибирования клеточной пролиферации в egfr-стимулированных типах рака
EP2527332A1 (en) 2011-05-24 2012-11-28 Bayer Intellectual Property GmbH 4-Aryl-N-phenyl-1,3,5-triazin-2-amines containing a sulfoximine group as CDK9 inhibitors
TWI555737B (zh) 2011-05-24 2016-11-01 拜耳知識產權公司 含有硫醯亞胺基團之４－芳基－ｎ－苯基－１，３，５－三氮雜苯－２－胺
CN103930399B (zh) 2011-09-16 2016-03-16 拜耳知识产权有限责任公司 包含亚氨基亚磺酰基的二取代的5-氟嘧啶衍生物
EP2758400A1 (en) 2011-09-23 2014-07-30 Bayer Intellectual Property GmbH Substituted imidazopyridazines
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物
EP2711365A1 (en) 2012-09-21 2014-03-26 Chemilia AB 4-Indazolylamino-2-(2-(indol-3-yl)ethyl)aminopyrimidines useful for the treatment of cancer
EP2711364A1 (en) 2012-09-21 2014-03-26 Chemilia AB 4-(Indolyl or benzimidazolyl)amino-2-(2-(indol-3-yl)ethyl)aminopyrimidines useful for the treatment of cancer
CN103724280A (zh) * 2012-10-11 2014-04-16 韩冰 一类治疗脑性瘫痪的化合物及其用途
TW201418243A (zh) 2012-11-15 2014-05-16 Bayer Pharma AG 含有磺醯亞胺基團之ｎ－（吡啶－２－基）嘧啶－４－胺衍生物
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
HK1222852A1 (zh) 2013-06-21 2017-07-14 Bayer Pharma Aktiengesellschaft 二氨基杂芳基取代的吡唑
CN105452236A (zh) * 2013-06-21 2016-03-30 拜耳制药股份公司 取代的苄基吡唑
CN105764893A (zh) 2013-10-30 2016-07-13 拜耳制药股份公司 杂芳基取代的吡唑
EP3736268A1 (en) * 2013-12-20 2020-11-11 Signal Pharmaceuticals, LLC Process for the preparation of substituted diaminopyrimidyl compounds
NZ715903A (en) * 2014-01-30 2017-06-30 Signal Pharm Llc Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use
TWI656121B (zh) 2014-08-04 2019-04-11 德商拜耳製藥公司 ２－（嗎啉－４－基）－１，７－萘啶
CA3001085A1 (en) 2015-10-08 2017-04-13 Bayer Pharma Aktiengesellschaft Novel modified macrocyclic compounds
WO2017060322A2 (en) 2015-10-10 2017-04-13 Bayer Pharma Aktiengesellschaft Ptefb-inhibitor-adc
EP3445369A4 (en) * 2016-04-21 2020-03-04 Eip Pharma, LLC COMPOSITIONS AND METHODS FOR TREATING DEMENTIA
ES2940911T3 (es) * 2016-06-27 2023-05-12 Rigel Pharmaceuticals Inc Compuestos de 2,4-diamino-pirimidina y su uso como inhibidores de IRAK4
CN108218794A (zh) * 2016-12-21 2018-06-29 南京华威医药科技开发有限公司 一种新型的ido抑制剂
US11254690B2 (en) 2017-03-28 2022-02-22 Bayer Pharma Aktiengesellschaft PTEFb inhibiting macrocyclic compounds
EP3601236A1 (en) 2017-03-28 2020-02-05 Bayer Aktiengesellschaft Novel ptefb inhibiting macrocyclic compounds
WO2019056003A1 (en) 2017-09-18 2019-03-21 Eip Pharma, Llc CO-CRYSTALS FROM NEFLAMAPIMOD (VX -745)
CA3090843A1 (en) 2018-02-13 2019-08-22 Bayer Aktiengesellschaft Use of 5-fluoro-4-(4-fluoro-2-methoxyphenyl)-n-{4-[(s-methylsulfonimidoyl)methyl]pyridin-2-yl}pyridin-2-amine for treating diffuse large b-cell lymphoma
CN109796349A (zh) * 2019-03-01 2019-05-24 西南石油大学 一种还原芳香硝基化合物制备芳胺类化合物的方法
WO2021138391A1 (en) 2019-12-30 2021-07-08 Tyra Biosciences, Inc. Indazole compounds
BR112022025692A2 (pt) 2020-06-19 2023-02-28 Bayer Ag 1,3,4-oxadiazóis e seus derivados como fungicidas
WO2025180470A1 (zh) * 2024-02-29 2025-09-04 江苏亚虹医药科技股份有限公司 细胞周期蛋白依赖性激酶抑制剂及其医药用途

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9828511D0 (en) * 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
DE10212100A1 (de) * 2002-03-11 2003-10-23 Schering Ag CDK inhibitorische 2-Heteroaryl-Pyrimidine, deren Herstellung und Verwendung als Arzneimittel
US7288547B2 (en) 2002-03-11 2007-10-30 Schering Ag CDK-inhibitory 2-heteroaryl-pyrimidines, their production and use as pharmaceutical agents
EA200500721A1 (ru) * 2002-11-28 2005-12-29 Шеринг Акциенгезельшафт Пиримидины, ингибирующие chk, pdk и акт, их получение и применение в качестве лекарственных средств
DE10349423A1 (de) 2003-10-16 2005-06-16 Schering Ag Sulfoximinsubstituierte Parimidine als CDK- und/oder VEGF-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
CA2567228A1 (en) * 2004-05-20 2005-12-01 Sugen, Inc. Thiophene heteroaryl amines
JP2008514571A (ja) * 2004-09-29 2008-05-08 バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト 細胞周期−キナーゼまたはレセプター−チロシン−キナーゼインヒビターとしての置換２−置換アニリノピリミジン類、それらの製造および薬剤としての使用
EP1705177A1 (en) * 2005-03-23 2006-09-27 Schering Aktiengesellschaft N-aryl-sulfoximine-substituted pyrimidines as CDK- and/or VEGF inhibitors, their production and use as pharmaceutical agents

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