PE20091486A1 - Derivado de pirrolopirimidina como inhibidor de la enzima pi3k - Google Patents

Derivado de pirrolopirimidina como inhibidor de la enzima pi3k

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Publication number
PE20091486A1
PE20091486A1 PE2009000176A PE2009000176A PE20091486A1 PE 20091486 A1 PE20091486 A1 PE 20091486A1 PE 2009000176 A PE2009000176 A PE 2009000176A PE 2009000176 A PE2009000176 A PE 2009000176A PE 20091486 A1 PE20091486 A1 PE 20091486A1
Authority
PE
Peru
Prior art keywords
pyrimidin
pirrolo
pi3k
inhibitor
morfolin
Prior art date
Application number
PE2009000176A
Other languages
English (en)
Inventor
Hirosato Ebiike
Jun Ohwada
Kohei Koyama
Takeshi Murata
Woo Sang Hong
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 PE20091486A1 publication Critical patent/PE20091486A1/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
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    • 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
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    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
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    • A61P37/00Drugs for immunological or allergic disorders
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    • AHUMAN NECESSITIES
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Emergency Medicine (AREA)
  • Rheumatology (AREA)

Abstract

REFERIDA A UN DERIVADO DE PIRROLOPIRIMIDINA DE FORMULA (I), DONDE Q ES UN GRUPO LIGADOR -X-Y-; X ES UN ENLACE SIMPLE, CO, CONH, CSNH, ENTRE OTROS; Y ES UN ENLACE SIMPLE, ARILENO, HETEROARILENO, ENTRE OTROS; R1 ES ALQUILENO C0-C6-(A)m-ALQUILO C1-C6 O ALQUILO C0-C6-(A)m-ALQUILENO C0-C6-(HETEROCICLO); A ES CO, CS, CONH, CSNH, ENTRE OTROS; m ES 0 O 1. SON COMPUESTOS PREFERIDOS: 5-{7-[2-(4-ETIL-PIPERAZIN-1-IL)-PIRIDIN-4-IL]-2-MORFOLIN-4-IL-7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL}-PIRIMIDIN-2-ILAMINA, {3-[4-(2-AMINO-PIRIMIDIN-5-IL)-2-MORFOLIN-4-IL-PIRROLO[2,3-d]PIRIMIDIN-7-IL]-4-METIL-FENIL}-MORFOLIN-4-IL-METANONA, 5-(7-METANOSULFONIL-2-MORFOLIN-4-IL-7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-PIRIMIDIN-2-ILAMINA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA Y A UN METODO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE LA ENZIMA PI3K Y SON UTILES EN EL TRATAMIENTO DEL CANCER, ENFERMEDADES PROLIFERATIVAS, ENTRE OTRAS
PE2009000176A 2008-02-07 2009-02-05 Derivado de pirrolopirimidina como inhibidor de la enzima pi3k PE20091486A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
PE20091486A1 true PE20091486A1 (es) 2009-10-14

Family

ID=40952235

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2009000176A PE20091486A1 (es) 2008-02-07 2009-02-05 Derivado de pirrolopirimidina como inhibidor de la enzima pi3k

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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RU2518098C2 (ru) 2007-10-05 2014-06-10 Верастэм,Инк. Пиримидинзамещенные производные пурина, фармацевтическая композиция на их основе, способ ингибирования протеинкиназ, способ лечения или профилактики заболеваний, чувствительных к ингибированию протеинкиназ и способ лечения пролиферативных заболеваний
TWI378933B (en) 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
WO2010056320A2 (en) * 2008-11-11 2010-05-20 Tyrogenex, Inc. Pi3k/mtor kinase inhibitors
AR075974A1 (es) 2009-03-27 2011-05-11 Pathway Therapeutics Ltd Pirimidinil y 1,3,5-triazinilbencimidazolsulfonamidas y su uso en terapia del cancer
MX2011010332A (es) 2009-04-03 2011-11-29 S Bio Pte Ltd Compuestos de purina sustituidos con pirimidina como inhibidores de cinasa(s).
DK3072890T3 (en) 2009-07-07 2019-02-11 Mei Pharma Inc Pyrimidinyl and 1,3,5-triazinylbenzimidazoles and their use in cancer therapy
BR112013024907A2 (pt) 2011-03-28 2016-12-20 Mei Pharma Inc composto, composição farmacêutica, método para o tratamento, prevenção ou atenuação de um ou mais sintomas de um distúrbio, doença ou condição mediada por pi3k em um sujeito, método para modular a atividade enzimática de pi3k
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
BR112015023203A8 (pt) 2013-03-15 2018-01-23 Constellation Pharmaceuticals Inc métodos para tratamento de câncer, método para aumentar a eficiência de um tratamento de câncer, método para retardar e/ou prevenir o desenvolvimento de câncer, método para tratar um indivíduo com câncer, método para aumentar a sensibilidade para um agente de terapia para câncer, método para estender um período de sensibilidade e método para estender a duração da resposta para uma terapia para câncer.
KR101982912B1 (ko) * 2013-10-16 2019-09-10 상하이 잉리 파마슈티컬 컴퍼니 리미티드 융합된 헤테로사이클릭 화합물, 이의 제조 방법, 약학적 조성물, 및 그 용도
PT3126528T (pt) 2014-04-04 2021-09-09 Crown Bioscience Inc Taicang Métodos para determinar a responsividade a inibidores de mek/erk
CN106928232B (zh) * 2015-12-31 2019-07-09 上海医药集团股份有限公司 喹啉类化合物及其盐的晶型、制备方法、组合物与应用
TW201817731A (zh) * 2016-09-29 2018-05-16 日商第一三共股份有限公司 [2-(1-甲基-1h-吡唑-4-基)-6-( 啉-4-基)-9h-嘌呤-8-基][4-( 啉-4-基)哌啶-1-基]甲酮及其製藥上容許鹽之結晶
CN110996959A (zh) 2017-05-23 2020-04-10 梅制药公司 联合疗法
JP2020531414A (ja) 2017-08-14 2020-11-05 エムイーアイ ファーマ,インク. 併用療法
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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Publication number Priority date Publication date Assignee Title
US5378700A (en) 1989-10-11 1995-01-03 Teijin Limited Fused pyrimidine derivative, process for preparation of same and pharmaceutical preparation comprising same as active ingredient
DE69329574T2 (de) * 1992-04-03 2001-05-31 Pharmacia & Upjohn Co., Kalamazoo Pharmazeutisch wirksame bicyclisch heterocyclische amine
US5502187A (en) * 1992-04-03 1996-03-26 The Upjohn Company Pharmaceutically active bicyclic-heterocyclic amines
CN1186324C (zh) * 2000-04-27 2005-01-26 山之内制药株式会社 稠合杂芳基衍生物
GB0100622D0 (en) * 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical compounds V111
UY29177A1 (es) * 2004-10-25 2006-05-31 Astex Therapeutics Ltd Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos
JP2009533323A (ja) * 2006-03-11 2009-09-17 ヴァーナリス アールアンドディー リミテッド Hsp90阻害剤として用いられるピロロピリミジン誘導体
WO2008018426A1 (fr) * 2006-08-08 2008-02-14 Chugai Seiyaku Kabushiki Kaisha Dérivé de pyrimidine comme inhibiteur de la PI3K et son utilisation

Also Published As

Publication number Publication date
CL2009000241A1 (es) 2010-09-03
CN101932584A (zh) 2010-12-29
TW200938201A (en) 2009-09-16
WO2009099163A1 (ja) 2009-08-13
IL207452A0 (en) 2010-12-30
BRPI0907931A2 (pt) 2015-07-28
JPWO2009099163A1 (ja) 2011-05-26
MX2010008686A (es) 2010-08-30
KR20100120680A (ko) 2010-11-16
AU2009211622A1 (en) 2009-08-13
JP5350277B2 (ja) 2013-11-27
EP2239261A1 (en) 2010-10-13
US20100324284A1 (en) 2010-12-23
EP2239261A4 (en) 2011-06-08
AR070352A1 (es) 2010-03-31
CA2711778A1 (en) 2009-08-13

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