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PE20091738A1 - Inhibidores de quinasa de pirrolopirazina - Google Patents

Inhibidores de quinasa de pirrolopirazina

Info

Publication number
PE20091738A1
PE20091738A1 PE2009000261A PE2009000261A PE20091738A1 PE 20091738 A1 PE20091738 A1 PE 20091738A1 PE 2009000261 A PE2009000261 A PE 2009000261A PE 2009000261 A PE2009000261 A PE 2009000261A PE 20091738 A1 PE20091738 A1 PE 20091738A1
Authority
PE
Peru
Prior art keywords
alkyl
phenyl
pirrolo
methyl
pirazin
Prior art date
Application number
PE2009000261A
Other languages
English (en)
Inventor
Daisy Joe Du Bois
Todd Richard Elworthy
Robert Than Hendricks
Johannes Cornelius Hermann
Rama K Kondru
Yan Lou
Timothy D Owens
David Bernard Smith
Jaehyeon Park
Michael Soth
Original Assignee
Hoffmann La Roche
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40514045&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20091738(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20091738A1 publication Critical patent/PE20091738A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

REFERIDA A UN DERIVADO DE PIRROLOPIRAZINA DE FORMULA (I), DONDE R ES R1, R2, R3 O R4; R1 ES ALQUILO C1-C6, FENILO, BENCILO, ENTRE OTROS; R2 ES N(R2a)2; R2a ES H O R2b; R2b ES ALQUILO C1-C6, FENILO, CICLOALQUILO C3-C8; ENTRE OTROS; R3 ES -C(=O)R3a; R3a ES ALQUILO C1-C6, FENILO, ALCOXI C1-C6, ENTRE OTROS; R4 ES -O(R4a); R4a ES H O R4b; R4b ES ALQUILO C1-C6, FENILO, BENCILO, CICLOALQUILO C3-C8, ENTRE OTROS; Q4 ES Q4a O Q4b; Q4a ES H, OH, CIANO, HALOGENO; Q4b ES ALQUILO C1-C6, HIDROXIALQUILO C1-C6, AMINO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 1-(2-BROMO-5H-PIRROLO[2,3-b]PIRAZIN-7-IL)-3-METIL-BUTAN-1-ONA, (2-BROMO-5H-PIRROLO[2,3-b]PIRAZIN--7-IL)-(1-METIL-CICLOHEXIL)-METANONA, 1-(2-ETINIL-5H-PIRROLO[2,3-b]PIRAZIN-7-IL)-(1-METIL-CICLOPENTIL)-METANONA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LAS QUINASAS DE JANUS (JAK) Y TIROSINA-QUINASA DEL BAZO (SYK), PARTICULARMENTE JAK 3, Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES INFLAMATORIAS Y AUTOINMUNES
PE2009000261A 2008-02-25 2009-02-23 Inhibidores de quinasa de pirrolopirazina PE20091738A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US3103508P 2008-02-25 2008-02-25
US14651409P 2009-01-22 2009-01-22

Publications (1)

Publication Number Publication Date
PE20091738A1 true PE20091738A1 (es) 2009-11-13

Family

ID=40514045

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2009000261A PE20091738A1 (es) 2008-02-25 2009-02-23 Inhibidores de quinasa de pirrolopirazina

Country Status (18)

Country Link
US (1) US8119636B2 (es)
EP (1) EP2247593B1 (es)
JP (1) JP5284377B2 (es)
KR (1) KR20100114095A (es)
CN (1) CN101952296B (es)
AR (1) AR070467A1 (es)
AT (1) ATE519763T1 (es)
AU (1) AU2009218609A1 (es)
BR (1) BRPI0907928A2 (es)
CA (1) CA2713718A1 (es)
CL (1) CL2009000405A1 (es)
IL (1) IL206818A0 (es)
MX (1) MX2010009023A (es)
PE (1) PE20091738A1 (es)
RU (1) RU2010139284A (es)
TW (1) TW200942543A (es)
WO (1) WO2009106444A1 (es)
ZA (1) ZA201004942B (es)

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CN101952294B (zh) * 2008-02-25 2014-11-26 霍夫曼-拉罗奇有限公司 吡咯并吡嗪激酶抑制剂
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CN102264721B (zh) 2008-11-10 2015-12-09 沃泰克斯药物股份有限公司 用作atr激酶抑制剂的化合物
CN106518856B (zh) 2008-12-19 2020-04-28 沃泰克斯药物股份有限公司 用作atr激酶抑制剂的化合物
US8481541B2 (en) 2010-03-22 2013-07-09 Hoffmann-La Roche Inc. Pyrrolopyrazine kinase inhibitors
US8518945B2 (en) * 2010-03-22 2013-08-27 Hoffmann-La Roche Inc. Pyrrolopyrazine kinase inhibitors
SG185524A1 (en) 2010-05-12 2012-12-28 Vertex Pharma Compounds useful as inhibitors of atr kinase
JP2013526540A (ja) 2010-05-12 2013-06-24 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｒキナーゼ阻害剤として有用な化合物
US8969356B2 (en) 2010-05-12 2015-03-03 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
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MX2012013082A (es) 2010-05-12 2013-05-09 Vertex Pharma Derivados de 2-aminopiridina utiles como iinhibidores de cinasa atr.
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JP2014520161A (ja) 2011-06-22 2014-08-21 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｒキナーゼ阻害剤として有用な化合物
US9309250B2 (en) 2011-06-22 2016-04-12 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors
US9096602B2 (en) 2011-06-22 2015-08-04 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-B]pyrazines as ATR kinase inhibitors
WO2013030138A1 (en) * 2011-09-01 2013-03-07 F. Hoffmann-La Roche Ag Pyrrolopyrazine kinase inhibitors
CA2850566C (en) 2011-09-30 2022-05-03 Vertex Pharmaceuticals Incorporated Process for making 4-[chloro-n-hydroxycarbonimidoyl]phenyl derivative
EP3733185B1 (en) 2011-09-30 2022-12-07 Vertex Pharmaceuticals Incorporated Treating non-small cell lung cancer with atr inhibitors
CN103958507A (zh) 2011-09-30 2014-07-30 沃泰克斯药物股份有限公司 可用作atr激酶抑制剂的化合物
WO2013049720A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2013049719A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
BR112014008126A2 (pt) 2011-11-01 2017-04-18 Hoffmann La Roche composto, método para o tratamento, composição farmacêutica, utilização de um composto e invenção
US8846918B2 (en) 2011-11-09 2014-09-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2013071088A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2013071090A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8841449B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2013071093A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
WO2013104573A1 (en) 2012-01-10 2013-07-18 F. Hoffmann-La Roche Ag Pyridazine amide compounds and their use as syk inhibitors
EP2833973B1 (en) 2012-04-05 2017-09-13 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase and combination therapies thereof
CA2876543A1 (en) * 2012-08-21 2014-02-27 F. Hoffmann-La Roche Ag Pyrrolo[2,3-b]pyrazines as syk inhibitors
US8999632B2 (en) 2012-10-04 2015-04-07 Vertex Pharmaceuticals Incorporated Method for measuring ATR inhibition mediated increases in DNA damage
US8912198B2 (en) 2012-10-16 2014-12-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
DK3418281T3 (da) 2012-12-07 2020-12-07 Vertex Pharma Pyrazolo[1,5-a]pyrimidiner, der er anvendelige som inhibitorer af atr-kinase til behandling af cancersygdomme
JP2016512815A (ja) 2013-03-15 2016-05-09 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ａｔｒキナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体
WO2014186101A1 (en) * 2013-05-14 2014-11-20 3M Innovative Properties Company Pyridine- or pyrazine-containing compounds
PT3077397T (pt) 2013-12-06 2020-01-22 Vertex Pharma Composto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]pirazolo[1,5-a]pirimidin-3-carboxamida útil como inibidor da atr quinase, a sua preparação, diferentes formas sólidas e derivados radiomarcados do mesmo
KR102575125B1 (ko) 2014-06-05 2023-09-07 버텍스 파마슈티칼스 인코포레이티드 Atr 키나제의 저해제로서 유용한 2-아미노-6-플루오로-n-[5-플루오로-피리딘-3-일]-피라졸로[1,5-a]피리미딘-3-카복스아미드 화합물의 방사성표지된 유도체, 상기 화합물의 제조 및 이의 다양한 고체 형태
DK3157566T3 (da) 2014-06-17 2019-07-22 Vertex Pharma Fremgangsmåde til behandling af cancer under anvendelse af en kombination chk1- og atr-inhibitorer
MX395066B (es) 2015-09-30 2025-03-24 Vertex Pharma Método para tratar cáncer usando una combinación de agentes que dañan el adn e inhibidores de proteína relacionada con ataxia telangiectasia y rad3 (atr).
US20170100396A1 (en) 2015-10-07 2017-04-13 F. Hoffmann-La Roche Ag Pyrrolopyrazine derivatives for use in the treatment, amelioration or prevention of influenza
JP2023507138A (ja) 2019-12-20 2023-02-21 ファイザー・インク ベンゾイミダゾール誘導体

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Also Published As

Publication number Publication date
WO2009106444A1 (en) 2009-09-03
CA2713718A1 (en) 2009-09-03
CL2009000405A1 (es) 2010-02-26
ATE519763T1 (de) 2011-08-15
TW200942543A (en) 2009-10-16
EP2247593B1 (en) 2011-08-10
MX2010009023A (es) 2010-09-07
US8119636B2 (en) 2012-02-21
ZA201004942B (en) 2011-12-28
KR20100114095A (ko) 2010-10-22
JP2011513263A (ja) 2011-04-28
JP5284377B2 (ja) 2013-09-11
EP2247593A1 (en) 2010-11-10
IL206818A0 (en) 2010-12-30
BRPI0907928A2 (pt) 2015-07-28
RU2010139284A (ru) 2012-04-10
AR070467A1 (es) 2010-04-07
CN101952296A (zh) 2011-01-19
AU2009218609A1 (en) 2009-09-03
US20090215785A1 (en) 2009-08-27
CN101952296B (zh) 2013-08-21

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