IL258513B - History of quinoxaline and pyridopyrazine as pi3k inhibitors in the cell - Google Patents

History of quinoxaline and pyridopyrazine as pi3k inhibitors in the cell

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Publication number
IL258513B
IL258513B IL258513A IL25851318A IL258513B IL 258513 B IL258513 B IL 258513B IL 258513 A IL258513 A IL 258513A IL 25851318 A IL25851318 A IL 25851318A IL 258513 B IL258513 B IL 258513B
Authority
IL
Israel
Prior art keywords
pi3kbeta
quinoxaline
inhibitors
pyridopyrazine derivatives
pyridopyrazine
Prior art date
Application number
IL258513A
Other languages
English (en)
Hebrew (he)
Other versions
IL258513A (en
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of IL258513A publication Critical patent/IL258513A/en
Publication of IL258513B publication Critical patent/IL258513B/en

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    • 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
    • C07D403/10Heterocyclic 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 carbon chain containing aromatic rings
    • 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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  • Diabetes (AREA)
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  • Endocrinology (AREA)
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  • Gynecology & Obstetrics (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
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IL258513A 2015-10-09 2018-04-05 History of quinoxaline and pyridopyrazine as pi3k inhibitors in the cell IL258513B (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP15189163 2015-10-09
EP16174710 2016-06-16
PCT/EP2016/073962 WO2017060406A1 (en) 2015-10-09 2016-10-07 Quinoxaline and pyridopyrazine derivatives as pi3kbeta inhibitors

Publications (2)

Publication Number Publication Date
IL258513A IL258513A (en) 2018-05-31
IL258513B true IL258513B (en) 2020-08-31

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IL258513A IL258513B (en) 2015-10-09 2018-04-05 History of quinoxaline and pyridopyrazine as pi3k inhibitors in the cell

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US (2) US10526316B2 (enExample)
EP (1) EP3359533B1 (enExample)
JP (1) JP6912460B2 (enExample)
KR (1) KR102630111B1 (enExample)
CN (1) CN108349946B (enExample)
AU (1) AU2016335086B2 (enExample)
BR (1) BR112018007068B1 (enExample)
CA (1) CA2999818C (enExample)
EA (1) EA037401B1 (enExample)
ES (1) ES2905673T3 (enExample)
IL (1) IL258513B (enExample)
MA (1) MA45896A (enExample)
MX (1) MX382601B (enExample)
WO (1) WO2017060406A1 (enExample)

Families Citing this family (8)

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Publication number Priority date Publication date Assignee Title
JP6912460B2 (ja) 2015-10-09 2021-08-04 ヤンセン ファーマシューティカ エヌ.ベー. PI3Kβ阻害剤としてのキノキサリンおよびピリドピラジン誘導体
JP7149854B2 (ja) 2016-06-16 2022-10-07 ヤンセン ファーマシューティカ エヌ.ベー. Pi3k beta阻害薬としての二環式ピリジン、ピラジンおよびピリミジン誘導体
CN110461827A (zh) * 2017-03-29 2019-11-15 詹森药业有限公司 作为PI3K-β抑制剂的喹喔啉和吡啶并吡嗪衍生物
IL277071B2 (en) 2018-03-08 2024-07-01 Incyte Corp AMINOPYRAZINE DIOL COMPOUNDS AS PI3K-y INHIBITORS
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
CN111892597B (zh) * 2020-09-01 2023-07-25 山西天宏达安医药科技有限公司 一种喹喔啉基吡啶并吡嗪类化合物及其制备方法与应用
WO2024026419A1 (en) * 2022-07-27 2024-02-01 Black Diamond Therapeutics, Inc. Quinoxaline derivatives as pik3 alpha modulators
WO2024238221A1 (en) * 2023-05-12 2024-11-21 Mirati Therapeutics, Inc. Substituted quinoxalines

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Publication number Priority date Publication date Assignee Title
JP2009528385A (ja) 2006-03-02 2009-08-06 スミスクライン・ビーチャム・コーポレイション Pi3キナーゼ阻害剤として用いるためのチアゾロン
EP2046333A4 (en) 2006-07-24 2010-09-15 Glaxosmithkline Llc THIOZOLIDINEDIONE DERIVATIVES AS INHIBITORS OF P13-KINASE
EP2118076B1 (en) * 2007-02-22 2019-09-04 Merck Serono S.A. Quinoxaline compounds and use thereof
EP2173354A4 (en) * 2007-08-09 2011-10-05 Glaxosmithkline Llc CHINOXALIN DERIVATIVES AS PI3 KINASE INHIBITORS
KR101653842B1 (ko) 2008-01-04 2016-09-02 인텔리카인, 엘엘씨 특정 화학 물질, 조성물 및 방법
UA111579C2 (uk) 2009-08-17 2016-05-25 Інтеллікіне Ллк ГЕТЕРОЦИКЛІЧНІ ПОХІДНІ 2-АМІНОБЕНЗО[d]ОКСАЗОЛУ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ НА ЇХ ОСНОВІ ТА ЇХ ЗАСТОСУВАННЯ ДЛЯ ЛІКУВАННЯ ЗАХВОРЮВАННЯ, ПОВ'АНОГО З РІ3-КІНАЗОЮ
CA2775942A1 (en) 2009-09-29 2011-04-07 Xcovery Holding Company Llc Pi3k (delta) selective inhibitors
US8399460B2 (en) * 2009-10-27 2013-03-19 Astrazeneca Ab Chromenone derivatives
UY33304A (es) 2010-04-02 2011-10-31 Amgen Inc Compuestos heterocíclicos y sus usos
PT2624696T (pt) 2010-10-06 2017-03-21 Glaxosmithkline Llc Derivados de benzimidazole como inibidores da cinase pi3
EP2678016B1 (en) 2011-02-23 2016-08-10 Intellikine, LLC Heterocyclic compounds and uses thereof
UY34013A (es) * 2011-04-13 2012-11-30 Astrazeneca Ab ?compuestos de cromenona con actividad anti-tumoral?.
US9096605B2 (en) 2011-08-24 2015-08-04 Glaxosmithkline Llc Pyrazolopyrimidine derivatives as PI3 kinase inhibitors
US8906910B2 (en) 2011-12-20 2014-12-09 Glaxosmithkline Llc Imidazopyridine derivatives as PI3 kinase
US8778937B2 (en) 2011-12-20 2014-07-15 Glaxosmithkline Llc Benzimidazole boronic acid derivatives as PI3 kinase inhibitors
GB201212513D0 (en) 2012-07-13 2012-08-29 Ucb Pharma Sa Therapeutic agents
SI3233839T1 (sl) 2014-12-19 2019-12-31 Janssen Pharmaceutica Nv Heterociklil vezani derivati imidazopiridazina kot inhibitorji PI3Kbeta
JP6568588B2 (ja) 2014-12-19 2019-08-28 ヤンセン ファーマシューティカ エヌ.ベー. PI3Kβ阻害剤としてのイミダゾピリダジン誘導体
JP6912460B2 (ja) 2015-10-09 2021-08-04 ヤンセン ファーマシューティカ エヌ.ベー. PI3Kβ阻害剤としてのキノキサリンおよびピリドピラジン誘導体

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EA037401B1 (ru) 2021-03-24
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CA2999818A1 (en) 2017-04-13
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