JP2010522770A - Akt活性の阻害物質 - Google Patents

Akt活性の阻害物質 Download PDF

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Publication number
JP2010522770A
JP2010522770A JP2010501246A JP2010501246A JP2010522770A JP 2010522770 A JP2010522770 A JP 2010522770A JP 2010501246 A JP2010501246 A JP 2010501246A JP 2010501246 A JP2010501246 A JP 2010501246A JP 2010522770 A JP2010522770 A JP 2010522770A
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JP
Japan
Prior art keywords
methyl
cancer
amino
ethyl
pyrazol
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
JP2010501246A
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English (en)
Japanese (ja)
Other versions
JP2010522770A5 (enExample
Inventor
マーク・アンドリュー・シーフェルド
ミーガン・ビー・ラウズ
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
GlaxoSmithKline LLC
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GlaxoSmithKline LLC
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Publication date
Application filed by GlaxoSmithKline LLC filed Critical GlaxoSmithKline LLC
Publication of JP2010522770A publication Critical patent/JP2010522770A/ja
Publication of JP2010522770A5 publication Critical patent/JP2010522770A5/ja
Withdrawn legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/041,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/061,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2010501246A 2007-03-29 2008-03-28 Akt活性の阻害物質 Withdrawn JP2010522770A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US90874107P 2007-03-29 2007-03-29
PCT/US2008/058603 WO2008121786A1 (en) 2007-03-29 2008-03-28 Inhibitors of akt activity

Publications (2)

Publication Number Publication Date
JP2010522770A true JP2010522770A (ja) 2010-07-08
JP2010522770A5 JP2010522770A5 (enExample) 2011-05-12

Family

ID=39808679

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2010501246A Withdrawn JP2010522770A (ja) 2007-03-29 2008-03-28 Akt活性の阻害物質

Country Status (4)

Country Link
US (1) US8338434B2 (enExample)
EP (1) EP2134175A4 (enExample)
JP (1) JP2010522770A (enExample)
WO (1) WO2008121786A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015506347A (ja) * 2011-12-23 2015-03-02 ミレニアム ファーマシューティカルズ, インコーポレイテッドMillennium Pharmaceuticals, Inc. ヘテロアリールおよびその使用

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
US8598209B2 (en) * 2008-10-31 2013-12-03 Merck Sharp & Dohme Corp. P2X3, receptor antagonists for treatment of pain
PE20120003A1 (es) 2009-01-30 2012-02-12 Glaxosmithkline Llc Hidrocloruro de n-{(1s)-2-amino-1-[(3-fluorofenil)metil)etil}-5-cloro-4-(4-cloro-1-metil-1h-pirazol-5-il)-2-tiofenocarboxamida cristalino
WO2010094009A2 (en) * 2009-02-13 2010-08-19 Children's Hospital Medical Center Methods and compositions for the treatment of ras associated disorders
US20130225524A1 (en) * 2010-11-05 2013-08-29 Deping Chai Chemical Compounds
TW201321371A (zh) 2011-10-14 2013-06-01 Incyte Corp 做為akt抑制劑之異吲哚啉酮及吡咯并吡啶酮衍生物
WO2013096151A1 (en) * 2011-12-22 2013-06-27 Glaxosmithkline Llc Chemical compounds
WO2013096153A1 (en) * 2011-12-22 2013-06-27 Glaxosmithkline Llc Chemical compounds
KR20160104612A (ko) 2013-07-26 2016-09-05 업데이트 파마 인코포레이트 비산트렌의 치료 효과 개선용 조성물
WO2020078865A1 (en) 2018-10-16 2020-04-23 F. Hoffmann-La Roche Ag Use of akt inhibitors in ophthalmology

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA04001088A (es) * 2001-08-03 2004-05-20 Vertex Pharma Derivados de pirazol como inhibidores de cinasa y uso de los mismos.
TW200306819A (en) * 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
GB0215844D0 (en) * 2002-07-09 2002-08-14 Novartis Ag Organic compounds
WO2004041185A2 (en) 2002-10-31 2004-05-21 University Of Rochester Hyfroxyflutamide induced pathways related to androgen receptor negative prostate cancer cells
ATE522525T1 (de) * 2003-05-01 2011-09-15 Bristol Myers Squibb Co Arylsubstituierte pyrazolamidverbindungen, die als kinase-inhibitoren von nutzen sind
CN101253152A (zh) * 2005-09-02 2008-08-27 安斯泰来制药株式会社 作为rock抑制剂的酰胺衍生物

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015506347A (ja) * 2011-12-23 2015-03-02 ミレニアム ファーマシューティカルズ, インコーポレイテッドMillennium Pharmaceuticals, Inc. ヘテロアリールおよびその使用

Also Published As

Publication number Publication date
US20100137338A1 (en) 2010-06-03
EP2134175A4 (en) 2012-01-11
EP2134175A1 (en) 2009-12-23
WO2008121786A1 (en) 2008-10-09
US8338434B2 (en) 2012-12-25

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