AR070352A1 - Derivado de pirrolopirimidina como inhibidor de la enzima pi3k, un procedimiento de elaboracion del compuesto, una composicion farmaceutica y un agente preventivo o terapeutico en base al compuesto. - Google Patents

Derivado de pirrolopirimidina como inhibidor de la enzima pi3k, un procedimiento de elaboracion del compuesto, una composicion farmaceutica y un agente preventivo o terapeutico en base al compuesto.

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Publication number
AR070352A1
AR070352A1 ARP090100424A ARP090100424A AR070352A1 AR 070352 A1 AR070352 A1 AR 070352A1 AR P090100424 A ARP090100424 A AR P090100424A AR P090100424 A ARP090100424 A AR P090100424A AR 070352 A1 AR070352 A1 AR 070352A1
Authority
AR
Argentina
Prior art keywords
alkyl
halogen
preventive
composition
heteroaryl
Prior art date
Application number
ARP090100424A
Other languages
English (en)
Inventor
Hirosato Ebiike
Woo Sang Hong
Kohei Koyama
Jun Ohwada
Takeshi Murata
Original Assignee
Chugai Pharmaceutical Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Chugai Pharmaceutical Co Ltd filed Critical Chugai Pharmaceutical Co Ltd
Publication of AR070352A1 publication Critical patent/AR070352A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
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    • A61P35/00Antineoplastic agents
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    • A61P37/00Drugs for immunological or allergic disorders
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    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
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  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
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  • Communicable Diseases (AREA)
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  • AIDS & HIV (AREA)
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  • Endocrinology (AREA)
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  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
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Abstract

Se proporciona un agente preventivo o terapéutico de una enfermedad proliferativa, tal como el cáncer, que tiene efectos inhibidores de la enzima PI3K de características superiores, una accion inhibidora de la proliferacion celular superior, al igual que una mejorada estabilidad en el organismo e hidrosolubilidad. Reivindicacion 1: Un compuesto representado por la formula (1) caracterizado porque Q representa un grupo ligador representado por -X-Y-; X representa un enlace simple, -CO-, -CONH-, -CONalquilo C1-4-, -CS-, -CSNH-, -CSNalquilo C1-4- o -SO2-; Y representa un enlace simple, arileno o heteroarileno (el arileno y el heteroarileno pueden estar insustituidos o sustituidos en las posiciones 1 a 4 por -halogeno, -alquilo C1-6, -OH o -Oalquilo C1-6; siempre que X e Y no sean simultáneamente enlaces simples; R1 representa -alquileno C0-6-(A)m-alquilo C1-6, o alquileno C0-6-(A)m-alquileno C0-6-(heterociclo); A representa -CO-, -CS-, -CONH-, -CONalquilo C1-4-, -CSNH-, - CSNalquilo C1-4-, -NH- o -Nalquilo C1-4-; m representa 0 o 1; el mencionado -(heterociclo) es heteroarilo, o un grupo representado por la formula (2), donde Ra y Rb son iguales o diferentes y representan un átomo de hidrogeno, -alquilo C1-6, -halogeno, -OH o -Oalquilo C1-6; W representa -CRcRd-, -O-, -S-, -SO-, SO2 o -NRe-; n representa 0 o 1; Rc y Rd son iguales o diferentes y representan un átomo de hidrogeno, -halogeno, -alquilo C1-6, -OH, -Oalquilo C1-6 o heteroarilo; Re representa un átomo de hidrogeno, -alquilo C1-6, -OH, -Oalquilo C1-6 o heteroarilo (-alquilo C1-6 y -Oalquilo C1-6 en Rc, Rd y Re pueden estar sustituidos por -halogeno o -OH), o una de sus sales farmacéuticamente aceptables.
ARP090100424A 2008-02-07 2009-02-06 Derivado de pirrolopirimidina como inhibidor de la enzima pi3k, un procedimiento de elaboracion del compuesto, una composicion farmaceutica y un agente preventivo o terapeutico en base al compuesto. AR070352A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP2008027423 2008-02-07

Publications (1)

Publication Number Publication Date
AR070352A1 true AR070352A1 (es) 2010-03-31

Family

ID=40952235

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090100424A AR070352A1 (es) 2008-02-07 2009-02-06 Derivado de pirrolopirimidina como inhibidor de la enzima pi3k, un procedimiento de elaboracion del compuesto, una composicion farmaceutica y un agente preventivo o terapeutico en base al compuesto.

Country Status (15)

Country Link
US (1) US20100324284A1 (es)
EP (1) EP2239261A4 (es)
JP (1) JP5350277B2 (es)
KR (1) KR20100120680A (es)
CN (1) CN101932584A (es)
AR (1) AR070352A1 (es)
AU (1) AU2009211622A1 (es)
BR (1) BRPI0907931A2 (es)
CA (1) CA2711778A1 (es)
CL (1) CL2009000241A1 (es)
IL (1) IL207452A0 (es)
MX (1) MX2010008686A (es)
PE (1) PE20091486A1 (es)
TW (1) TW200938201A (es)
WO (1) WO2009099163A1 (es)

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EP2209786B1 (en) 2007-10-05 2013-02-27 Verastem, Inc. Pyrimidine substituted purine derivatives
TWI378933B (en) 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
AU2009314544C1 (en) * 2008-11-11 2015-11-12 Xcovery Holding Company Llc PI3K/mTOR kinase inhibitors
TW201038567A (en) 2009-03-27 2010-11-01 Pathway Therapeutics Ltd Pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy
WO2010114484A1 (en) 2009-04-03 2010-10-07 S*Bio Pte Ltd Pyrimidine substituted purine compounds as kinase (s) inhibitors
CA2767008C (en) 2009-07-07 2018-01-30 Pathway Therapeutics, Inc. Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy
TWI572599B (zh) 2011-03-28 2017-03-01 Mei製藥公司 (α-經取代之芳烷胺基及雜芳烷胺基)嘧啶基及1,3,5-三基苯并咪唑,其醫藥組合物及其在治療增生性疾病之用途
US9376715B2 (en) 2011-12-09 2016-06-28 Roche Molecular Systems, Inc Methods for detecting mutations in the catalytic subunit of the phosphoinositol-3 kinase (PIK3CA) gene
CN103450204B (zh) * 2012-05-31 2016-08-17 中国科学院上海药物研究所 吡咯[2,1-f][1,2,4]并三嗪类化合物,其制备方法及用途
CA2905123A1 (en) 2013-03-15 2014-09-18 Genentech, Inc. Methods of treating cancer and preventing cancer drug resistance
CN104557872B (zh) * 2013-10-16 2017-05-24 上海璎黎药业有限公司 稠合杂环化合物、其制备方法、药物组合物和用途
ES2727374T3 (es) 2014-04-04 2019-10-15 Crown Bioscience Inc Taicang Gen de fusión HNF4G-RSPO2
ES2877799T3 (es) * 2015-12-31 2021-11-17 Shanghai Pharmaceuticals Holding Co Ltd Sal de derivado de quinolina, formas polimórficas de la misma, métodos de preparación de la misma, composición y aplicaciones
US10822336B2 (en) * 2016-09-29 2020-11-03 Daiichi Sankyo Company, Limited Crystals of [2-(1-methyl-1H-pyrazol-4-yl)-6(morpholin-4-yl)-9H-purin-8-yl][4-(morpholin-4-yl)piperidin-1-yl]methanone and pharmaceutically acceptable salt thereof
US11304953B2 (en) 2017-05-23 2022-04-19 Mei Pharma, Inc. Combination therapy
KR20200041358A (ko) 2017-08-14 2020-04-21 메이 파마, 아이엔씨. 병용 요법
IT201800004082A1 (it) * 2018-03-29 2019-09-29 Berlin Chemie Ag Composizioni farmaceutiche antitumorali per terapia combinata
CN113200969B (zh) * 2021-05-19 2022-11-25 中国药科大学 一种PI3Kα选择性抑制剂及其制备方法和应用

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EP2050749B1 (en) * 2006-08-08 2017-11-22 Chugai Seiyaku Kabushiki Kaisha Pyrimidine derivative as pi3k inhibitor and use thereof

Also Published As

Publication number Publication date
JPWO2009099163A1 (ja) 2011-05-26
IL207452A0 (en) 2010-12-30
PE20091486A1 (es) 2009-10-14
US20100324284A1 (en) 2010-12-23
WO2009099163A1 (ja) 2009-08-13
CN101932584A (zh) 2010-12-29
CL2009000241A1 (es) 2010-09-03
EP2239261A1 (en) 2010-10-13
AU2009211622A1 (en) 2009-08-13
JP5350277B2 (ja) 2013-11-27
TW200938201A (en) 2009-09-16
CA2711778A1 (en) 2009-08-13
BRPI0907931A2 (pt) 2015-07-28
KR20100120680A (ko) 2010-11-16
MX2010008686A (es) 2010-08-30
EP2239261A4 (en) 2011-06-08

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