ES2439793T3 - Compuestos de pirimidina, su uso como inhibidores de la mTOR quinasa y de la PI3 quinasa, y su síntesis - Google Patents

Compuestos de pirimidina, su uso como inhibidores de la mTOR quinasa y de la PI3 quinasa, y su síntesis Download PDF

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Publication number
ES2439793T3
ES2439793T3 ES10716162.2T ES10716162T ES2439793T3 ES 2439793 T3 ES2439793 T3 ES 2439793T3 ES 10716162 T ES10716162 T ES 10716162T ES 2439793 T3 ES2439793 T3 ES 2439793T3
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Spain
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alkyl
heteroaryl
kinase
inhibitors
synthesis
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Active
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ES10716162.2T
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ES2439793T9 (es
Inventor
Jeroen Cunera Verheijen
Arie Zask
David James Richard
Joshua Aaron Kaplan
Kevin Joseph Curran
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Wyeth LLC
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Wyeth LLC
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Compuesto de Fórmula I: o una sal farmacéuticamente aceptable del mismo en la que; R1 es independientemente alquil C1-C6-, aril C6-C14-, heteroaril C1-C9-, halógeno, o hidroxilo; p es 0, 1, 2, 3 o 4; het es un grupo heterobiciclil C5-C9- con puente que contiene al menos un átomo de oxígeno, al menos un átomo denitrógeno, y opcionalmente heteroátomos adicionales seleccionados entre oxígeno, azufre y nitrógeno, y estáconectado al grupo pirimidinilo a través de uno de los átomos de nitrógeno; uno de A es C-R5 y los otros dos son N; Ar es aril C6-C14- o heteroaril C1-C9- en el que el aril C6-C14- o heteroaril C1-C9- está opcionalmente sustituido con 1 a4 sustituyentes seleccionados independientemente entre alquil C1-C6-, halógeno, haloalquil-, hidroxilo, hidroxil(alquilC1-C6)-, H2N-, aminoalquil-, di(alquil C1-C6)amino-, HO2C-, (alcoxi C1-C6)carbonil-, (alquil C1-C6)carboxil-, di(alquil C1-C6)amido-, H2NC(O)-, (alquil C1-C6)amido-, y O2N-; y en el que el aril C6-C14- o heteroaril C1-C9- está unido al núcleo de pirimidina a través de un átomo de carbono delaril C6-C14- o heteroaril C1-C9-; R2 es H o alquil C1-C6-; R3 es R6, R7R8N-, R9S-, o R9O-.
ES10716162.2T 2009-04-17 2010-04-15 Compuestos de pirimidina, su uso como inhibidores de la mTOR quinasa y de la PI3 quinasa, y su síntesis Active ES2439793T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US17013809P 2009-04-17 2009-04-17
US170138P 2009-04-17
PCT/US2010/031191 WO2010120998A1 (en) 2009-04-17 2010-04-15 Pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses

Publications (2)

Publication Number Publication Date
ES2439793T3 true ES2439793T3 (es) 2014-01-24
ES2439793T9 ES2439793T9 (es) 2016-03-10

Family

ID=42269326

Family Applications (1)

Application Number Title Priority Date Filing Date
ES10716162.2T Active ES2439793T3 (es) 2009-04-17 2010-04-15 Compuestos de pirimidina, su uso como inhibidores de la mTOR quinasa y de la PI3 quinasa, y su síntesis

Country Status (6)

Country Link
US (1) US8835429B2 (es)
EP (1) EP2419432B9 (es)
JP (1) JP5649643B2 (es)
CA (1) CA2755554C (es)
ES (1) ES2439793T3 (es)
WO (1) WO2010120998A1 (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9249129B2 (en) 2010-03-04 2016-02-02 Cellzome Limited Morpholino substituted urea derivatives as mTOR inhibitors
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
US20140163023A1 (en) 2011-04-04 2014-06-12 Cellzome Limited Dihydropyrrolo pyrimidine derivatives as mtor inhibitors
EP2758379B1 (en) 2011-09-21 2016-10-19 Cellzome Limited Urea and carbamate derivatives of 2-morpholino-1,3,5-triazine as mTOR inhibitors for the treatment of immunological or proliferative diseases
RU2609208C2 (ru) 2011-10-07 2017-01-31 Селлзоум Лимитед МОРФОЛИНО-ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ БИЦИКЛИЧЕСКИХ ПИРИМИДИНМОЧЕВИНЫ ИЛИ КАРБАМАТА В КАЧЕСТВЕ ИНГИБИТОРОВ mTOR
CN104302294A (zh) * 2011-11-01 2015-01-21 埃克塞利希斯股份有限公司 用于治疗淋巴组织增生性恶性肿瘤的作为磷脂酰肌醇3-激酶抑制剂的n-(3-{[(3-{[2-氯-5-(甲氧基)苯基]氨基}喹喔啉-2-基)氨基]磺酰基}苯基)-2-甲基丙氨酰胺
CN104230952B (zh) * 2014-08-16 2017-02-01 沈阳药科大学 含有嘧啶骨架的化合物及其制备方法和用途
AU2015366357B2 (en) * 2014-12-17 2018-07-19 Shanghai Haiyan Pharmaceutical Technology Co. Ltd. 2-morpholin-4,6-disubstituted pyrimidine derivative, and preparation method and pharmaceutical use thereof

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9009A (en) * 1852-06-08 Bat-trap
US20060240014A1 (en) * 2003-06-03 2006-10-26 Beth Israel Deaconess Medical Center Methods and compounds for the treatment of vascular stenosis
GB0520657D0 (en) * 2005-10-11 2005-11-16 Ludwig Inst Cancer Res Pharmaceutical compounds
GB0525083D0 (en) * 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
MX2009002046A (es) * 2006-08-24 2009-03-06 Astrazeneca Ab Derivados de morfolino pirimidina utiles en el tratamiento de trastornos proliferativos.
EP2150114A4 (en) * 2007-05-18 2012-01-18 Merck Sharp & Dohme OXO-BRIDGED DIAZEPANOREXINE RECEPTOR ANTAGONISTS
CA2702838A1 (en) * 2007-10-16 2009-04-23 Wyeth Llc Thienopyrimidine and pyrazolopyrimidine compounds and their use as mtor kinase and pi3 kinase inhibitors

Also Published As

Publication number Publication date
CA2755554A1 (en) 2010-10-21
CA2755554C (en) 2013-09-24
EP2419432B9 (en) 2016-02-17
EP2419432A1 (en) 2012-02-22
US8835429B2 (en) 2014-09-16
JP5649643B2 (ja) 2015-01-07
EP2419432B1 (en) 2013-11-20
ES2439793T9 (es) 2016-03-10
WO2010120998A1 (en) 2010-10-21
JP2012524103A (ja) 2012-10-11
US20120134959A1 (en) 2012-05-31

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