WO2012059932A1 - Dérivés de 2,4-diaminopyrimidine en tant qu'inhibiteurs de protéine kinases - Google Patents

Dérivés de 2,4-diaminopyrimidine en tant qu'inhibiteurs de protéine kinases Download PDF

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Publication number
WO2012059932A1
WO2012059932A1 PCT/IN2010/000718 IN2010000718W WO2012059932A1 WO 2012059932 A1 WO2012059932 A1 WO 2012059932A1 IN 2010000718 W IN2010000718 W IN 2010000718W WO 2012059932 A1 WO2012059932 A1 WO 2012059932A1
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alkyl
formula
compound
nitro
cycloalkyl
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PCT/IN2010/000718
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English (en)
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Saumitra Sengupta
Srinivasan Rajagopalan
Ningaraddi Belavagi
Muralidhara Ramachandra
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Aurigene Discovery Technologies Limited
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Publication of WO2012059932A1 publication Critical patent/WO2012059932A1/fr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509Six-membered rings
    • C07F9/6512Six-membered rings having the nitrogen atoms in positions 1 and 3

Abstract

La présente invention concerne de nouveaux dérivés de pyrimidine de formule (I) : pouvant être employés en tant qu'inhibiteurs de kinases. Plus particulièrement, la présente invention concerne de nouveaux composés de type pyrimidine, leurs méthodes de synthèse, les compositions pharmaceutiques les incluant et leur utilisation dans le traitement de troubles prolifératifs.
PCT/IN2010/000718 2010-11-01 2010-11-01 Dérivés de 2,4-diaminopyrimidine en tant qu'inhibiteurs de protéine kinases WO2012059932A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
PCT/IN2010/000718 WO2012059932A1 (fr) 2010-11-01 2010-11-01 Dérivés de 2,4-diaminopyrimidine en tant qu'inhibiteurs de protéine kinases

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/IN2010/000718 WO2012059932A1 (fr) 2010-11-01 2010-11-01 Dérivés de 2,4-diaminopyrimidine en tant qu'inhibiteurs de protéine kinases

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WO2012059932A1 true WO2012059932A1 (fr) 2012-05-10

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Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8314119B2 (en) 2006-11-06 2012-11-20 Abbvie Inc. Azaadamantane derivatives and methods of use
CN103232397A (zh) * 2013-04-28 2013-08-07 江苏双乐化工颜料有限公司 5-氨基-n-取代苯并咪唑酮的合成方法
WO2015123595A1 (fr) 2014-02-14 2015-08-20 The Regents Of The University Of California Peroxydes cycliques utilisés en tant que promédicaments pour l'administration sélective d'agents
US9464078B2 (en) 2010-09-23 2016-10-11 Abbvie Inc. Monohydrate of azaadamantane derivatives
JP2017510644A (ja) * 2014-03-28 2017-04-13 キャリター・サイエンシーズ・リミテッド・ライアビリティ・カンパニーCalitor Sciences, Llc 置換されたヘテロアリール化合物および使用方法
WO2017162661A1 (fr) 2016-03-22 2017-09-28 Bayer Pharma Aktiengesellschaft 1h-benzo[de]isoquinoléine-1,3(2h)-diones
US9932344B2 (en) 2014-02-21 2018-04-03 Cancer Research Technology Limited Pyrazolo[1,5-A]pyrimidine-5,7-diamine compounds as CDK inhibitors and their therapeutic use
CN109096152A (zh) * 2018-07-31 2018-12-28 乐平市赛复乐医药化工有限公司 一种间甲磺酰胺基苯胺的制备方法
US11857552B2 (en) 2017-09-20 2024-01-02 Carrick Therapeutics Limited 4-[[(7-aminopyrazolo[1,5-a]pyrimidin-5-yl)amino]methyl]piperidin-3-ol compounds as CDK inhibitors

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WO2007132010A1 (fr) * 2006-05-15 2007-11-22 Boehringer Ingelheim International Gmbh 2, 4 -diamino pyrimidine en tant qu'inhibiteurs de kinases du cycle cellulaire
WO2010024430A1 (fr) * 2008-09-01 2010-03-04 アステラス製薬株式会社 Composé 2,4-diaminopyrimidine

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WO2006091737A1 (fr) 2005-02-24 2006-08-31 Kemia, Inc. Modulateurs de l'activite de gsk-3
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WO2007073117A1 (fr) 2005-12-22 2007-06-28 Crystalgenomics, Inc. Derives d'aminopyrimidine inhibiteurs de l'activite de la proteine kinase, son procede de preparation et composition pharmaceutique en contenant
WO2007132010A1 (fr) * 2006-05-15 2007-11-22 Boehringer Ingelheim International Gmbh 2, 4 -diamino pyrimidine en tant qu'inhibiteurs de kinases du cycle cellulaire
WO2010024430A1 (fr) * 2008-09-01 2010-03-04 アステラス製薬株式会社 Composé 2,4-diaminopyrimidine
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Cited By (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8987453B2 (en) 2006-11-06 2015-03-24 Abbvie Inc. Azaadamantane derivatives and methods of use
US8314119B2 (en) 2006-11-06 2012-11-20 Abbvie Inc. Azaadamantane derivatives and methods of use
US9464078B2 (en) 2010-09-23 2016-10-11 Abbvie Inc. Monohydrate of azaadamantane derivatives
CN103232397A (zh) * 2013-04-28 2013-08-07 江苏双乐化工颜料有限公司 5-氨基-n-取代苯并咪唑酮的合成方法
CN103232397B (zh) * 2013-04-28 2016-04-20 江苏双乐化工颜料有限公司 5-氨基-n-取代苯并咪唑酮的合成方法
US10662215B2 (en) 2014-02-14 2020-05-26 The Regents Of The University Of California Cyclic peroxides as prodrugs for selective delivery of agents
US10287312B2 (en) 2014-02-14 2019-05-14 The Regents Of The University Of California Cyclic peroxides as prodrugs for selective delivery of agents
US11014955B2 (en) 2014-02-14 2021-05-25 The Regents Of The University Of California Cyclic peroxides as prodrugs for selective delivery of agents
WO2015123595A1 (fr) 2014-02-14 2015-08-20 The Regents Of The University Of California Peroxydes cycliques utilisés en tant que promédicaments pour l'administration sélective d'agents
US11566029B2 (en) 2014-02-21 2023-01-31 Ip2Ipo Innovations Limited Pyrazolo[1,5-a]pyrimidine-5,7-diamine compounds as CDK inhibitors and their therapeutic use
US10927119B2 (en) 2014-02-21 2021-02-23 Ip2Ipo Innovations Limited Pyrazolo[1,5-a]pyrimidine-5,7-diamine compounds as CDK inhibitors and their therapeutic use
US9932344B2 (en) 2014-02-21 2018-04-03 Cancer Research Technology Limited Pyrazolo[1,5-A]pyrimidine-5,7-diamine compounds as CDK inhibitors and their therapeutic use
US10414772B2 (en) 2014-02-21 2019-09-17 Imperial Innovations Limited Pyrazolo[1,5-A]pyrimidine-5,7-diamine compounds as CDK inhibitors and their therapeutic use
EP3122728A4 (fr) * 2014-03-28 2017-10-25 Calitor Sciences, LLC Composés hétéroaryle substitués et leurs méthodes d'utilisation
EP3327006A1 (fr) * 2014-03-28 2018-05-30 Calitor Sciences, LLC Composés d'hétéroaryle substitués et procédés d'utilisation
JP2017510644A (ja) * 2014-03-28 2017-04-13 キャリター・サイエンシーズ・リミテッド・ライアビリティ・カンパニーCalitor Sciences, Llc 置換されたヘテロアリール化合物および使用方法
JP2017510643A (ja) * 2014-03-28 2017-04-13 キャリター・サイエンシーズ・リミテッド・ライアビリティ・カンパニーCalitor Sciences, Llc 置換されたヘテロアリール化合物および使用方法
WO2017162661A1 (fr) 2016-03-22 2017-09-28 Bayer Pharma Aktiengesellschaft 1h-benzo[de]isoquinoléine-1,3(2h)-diones
US11857552B2 (en) 2017-09-20 2024-01-02 Carrick Therapeutics Limited 4-[[(7-aminopyrazolo[1,5-a]pyrimidin-5-yl)amino]methyl]piperidin-3-ol compounds as CDK inhibitors
CN109096152A (zh) * 2018-07-31 2018-12-28 乐平市赛复乐医药化工有限公司 一种间甲磺酰胺基苯胺的制备方法
CN109096152B (zh) * 2018-07-31 2021-01-08 乐平市赛复乐医药化工有限公司 一种间甲磺酰胺基苯胺的制备方法

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