MX2012012560A - Piperazinotriazinas como inhibidores pi3k, para utilizar en el tratamiento de desordenes antiproliferativos. - Google Patents

Piperazinotriazinas como inhibidores pi3k, para utilizar en el tratamiento de desordenes antiproliferativos.

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Publication number
MX2012012560A
MX2012012560A MX2012012560A MX2012012560A MX2012012560A MX 2012012560 A MX2012012560 A MX 2012012560A MX 2012012560 A MX2012012560 A MX 2012012560A MX 2012012560 A MX2012012560 A MX 2012012560A MX 2012012560 A MX2012012560 A MX 2012012560A
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MX
Mexico
Prior art keywords
piperazinotriazines
treatment
pi3k inhibitors
acryloylaminoethyl
acryloyl
Prior art date
Application number
MX2012012560A
Other languages
English (en)
Inventor
Vladimir Cmiljanovic
Natasa Cmiljanovic
Bernd Giese
Matthias Wymann
Original Assignee
Univ Basel
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 Univ Basel filed Critical Univ Basel
Publication of MX2012012560A publication Critical patent/MX2012012560A/es

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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P17/06—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
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    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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    • 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
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    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
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    • 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
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    • 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]
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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    • A61P35/02—Antineoplastic agents specific for leukemia
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    • A—HUMAN NECESSITIES
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)

Abstract

La invención se refiere a compuestos de la fórmula (I) en donde R1 es metilo, n-hexilo, aminoetilo, metilaminoetilo, etilaminoetilo, dimetilaminoetilo, acriloilaminoetilo, metacriloilaminoetilo, metoxietilo, etoxietilo, C1-C4-alquil-sulfonilo, acriloilo o metacriloilo; o R1 es aminoetilo, acriloilo o acriloilaminoetilo que transporta un enlazador y una etiqueta y R2 y R3, independientemente entre si son, hidrógeno o C1-C4-alquilo, o R2 y R3 juntos forman un puente metileno o etileno; y tautómeros, solvatos y sales farmacéuticamente aceptables de los mismos. Estos compuestos son efectivos para evitar o tratar una enfermedad o desorden modulado por PI3 quinasas y/o mTOR, en particular tratamiento de un desorden hiperproliferativo.
MX2012012560A 2010-04-30 2011-04-27 Piperazinotriazinas como inhibidores pi3k, para utilizar en el tratamiento de desordenes antiproliferativos. MX2012012560A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1007227.0A GB201007227D0 (en) 2010-04-30 2010-04-30 Piperazinotriazines
PCT/IB2011/051829 WO2011135520A1 (en) 2010-04-30 2011-04-27 Piperazinotriazines as pi3k inhibitors for use in the treatment antiproliferative disorders

Publications (1)

Publication Number Publication Date
MX2012012560A true MX2012012560A (es) 2012-12-17

Family

ID=42289874

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2012012560A MX2012012560A (es) 2010-04-30 2011-04-27 Piperazinotriazinas como inhibidores pi3k, para utilizar en el tratamiento de desordenes antiproliferativos.

Country Status (16)

Country Link
US (1) US20130040912A1 (es)
EP (1) EP2563368A1 (es)
JP (1) JP2013525419A (es)
KR (1) KR20130118731A (es)
CN (1) CN103002899A (es)
AU (1) AU2011246952A1 (es)
BR (1) BR112012027813A2 (es)
CA (1) CA2797808A1 (es)
GB (1) GB201007227D0 (es)
IL (1) IL222692A0 (es)
MX (1) MX2012012560A (es)
NZ (1) NZ603859A (es)
RU (1) RU2012151201A (es)
SG (1) SG185067A1 (es)
WO (1) WO2011135520A1 (es)
ZA (1) ZA201206898B (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2968345B1 (en) 2013-03-13 2017-12-13 The Regents of The University of Michigan Dual mek/pi3k inhibitors and their application in the treatment of cancer diseases
US9951040B2 (en) 2014-11-20 2018-04-24 Council Of Scientific And Industrial Research 1,3,5 -triazine based PI3K inhibitors as anticancer agents and a process for the preparation thereof
CN105130960B (zh) * 2015-07-31 2018-07-06 沈阳药科大学 1,3,5-三嗪类衍生物及其应用
CN109563088B (zh) 2016-07-06 2022-10-11 密歇根大学董事会 MEK/PI3K和mTOR/MEK/PI3K的多功能抑制剂和治疗用途
CN109810100B (zh) * 2017-11-21 2022-03-11 中国药科大学 含有苯并呋喃的parp-1和pi3k双靶点抑制剂
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

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1020462T3 (da) 1997-07-24 2004-04-26 Zenyaku Kogyo Kk Heterocykliske forbindelser og antitumormiddel indeholdende disse som aktiv ingrediens
DE60217322T2 (de) 2001-04-27 2007-10-04 Zenyaku Kogyo K.K. Heterocyclische verbindung und antitumormittel, das diese als wirkstoff enthält
JP2005531347A (ja) 2002-07-01 2005-10-20 アミジッチ，オグニエン 試験人物の認知または感覚運動の能力もしくは才能を評価するために使用されるデータを生成するための方法
CA2507100C (en) * 2002-11-21 2012-10-09 Chiron Corporation 2,4,6-trisubstituted pyrimidines as phosphotidylinositol (pi) 3-kinase inhibitors and their use in the treatment of cancer
PT1864665E (pt) 2005-03-11 2012-06-27 Zenyaku Kogyo Kk Agente imunossupressor compreendendo um composto heterocíclico como ingrediente activo
WO2008032033A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidazolyl-2-morpholino-6-piperazinylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2009066084A1 (en) * 2007-11-21 2009-05-28 F. Hoffmann-La Roche Ag 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors
EP2276750A2 (en) * 2008-03-27 2011-01-26 Auckland Uniservices Limited Substituted pyrimidines and triazines and their use in cancer therapy
US8513221B2 (en) * 2008-07-07 2013-08-20 Xcovery Holding, LLC PI3K isoform selective inhibitors
US8461158B2 (en) * 2009-03-27 2013-06-11 Pathway Therapeutics Inc. Pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy

Also Published As

Publication number Publication date
ZA201206898B (en) 2013-07-31
GB201007227D0 (en) 2010-06-16
IL222692A0 (en) 2012-12-31
RU2012151201A (ru) 2014-06-10
US20130040912A1 (en) 2013-02-14
WO2011135520A8 (en) 2012-09-27
CN103002899A (zh) 2013-03-27
BR112012027813A2 (pt) 2018-05-15
AU2011246952A1 (en) 2012-12-20
JP2013525419A (ja) 2013-06-20
SG185067A1 (en) 2012-12-28
KR20130118731A (ko) 2013-10-30
CA2797808A1 (en) 2011-11-03
EP2563368A1 (en) 2013-03-06
WO2011135520A1 (en) 2011-11-03
NZ603859A (en) 2014-07-25

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