JP2013504325A - Ｐｉ３キナーゼインヒビターおよびその使用 - Google Patents

Ｐｉ３キナーゼインヒビターおよびその使用 Download PDF

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JP2013504325A
JP2013504325A JP2012528906A JP2012528906A JP2013504325A JP 2013504325 A JP2013504325 A JP 2013504325A JP 2012528906 A JP2012528906 A JP 2012528906A JP 2012528906 A JP2012528906 A JP 2012528906A JP 2013504325 A JP2013504325 A JP 2013504325A
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ring
nitrogen
membered
oxygen
sulfur
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JP2013504325A5 (https=
Inventor
デチャン ニュー，
ラッセル シー． ペッター，
ジャスウィンダー シン，
アーサー エフ． クルーグ，
ホルモズ マジヤスニ，
シェンドン シュー，
リーシン チャオ，
ケビン カンツ，
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アビラ セラピューティクス， インコーポレイテッド
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Publication of JP2013504325A publication Critical patent/JP2013504325A/ja
Publication of JP2013504325A5 publication Critical patent/JP2013504325A5/ja
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
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    • C—CHEMISTRY; METALLURGY
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    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • C12N9/1205—Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases

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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Wood Science & Technology (AREA)
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  • Neurosurgery (AREA)
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  • General Engineering & Computer Science (AREA)
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  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
JP2012528906A 2009-09-09 2010-09-09 Ｐｉ３キナーゼインヒビターおよびその使用 Pending JP2013504325A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US24094709P 2009-09-09 2009-09-09
US61/240,947 2009-09-09
US37139610P 2010-08-06 2010-08-06
US61/371,396 2010-08-06
PCT/US2010/048317 WO2011031896A2 (en) 2009-09-09 2010-09-09 Pi3 kinase inhibitors and uses thereof

Publications (2)

Publication Number Publication Date
JP2013504325A true JP2013504325A (ja) 2013-02-07
JP2013504325A5 JP2013504325A5 (https=) 2013-10-31

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US (1) US20110230476A1 (https=)
EP (1) EP2475375A4 (https=)
JP (1) JP2013504325A (https=)
KR (1) KR20120063515A (https=)
CN (1) CN102625708A (https=)
AU (1) AU2010292198A1 (https=)
BR (1) BR112012008385A2 (https=)
CA (1) CA2773848A1 (https=)
IL (1) IL218555A0 (https=)
MX (1) MX339584B (https=)
NZ (2) NZ598808A (https=)
PH (1) PH12012500491A1 (https=)
RU (1) RU2595718C2 (https=)
SG (2) SG10201405598QA (https=)
TW (2) TW201609747A (https=)
WO (1) WO2011031896A2 (https=)

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JP2014210769A (ja) * 2013-04-03 2014-11-13 株式会社ヤクルト本社 チアゾリジン誘導体又はその塩を有効成分とするＰｉｍ阻害剤
JP2016510000A (ja) * 2013-02-20 2016-04-04 カラ ファーマシューティカルズ インコーポレイテッド 治療用化合物およびその使用
JP2016518383A (ja) * 2013-05-01 2016-06-23 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ビヘテロアリール化合物及びその使用
JP2016519072A (ja) * 2013-03-15 2016-06-30 アラクセス ファーマ エルエルシー Ｋｒａｓｇ１２ｃの共有結合性阻害剤
US10111874B2 (en) 2014-09-18 2018-10-30 Araxes Pharma Llc Combination therapies for treatment of cancer
US10273207B2 (en) 2013-03-15 2019-04-30 Araxes Pharma Llc Covalent inhibitors of kras G12C
US10280172B2 (en) 2016-09-29 2019-05-07 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10370386B2 (en) 2013-10-10 2019-08-06 Araxes Pharma Llc Substituted quinolines as inhibitors of KRAS G12C
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
US10414757B2 (en) 2015-11-16 2019-09-17 Araxes Pharma Llc 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
US10428064B2 (en) 2015-04-15 2019-10-01 Araxes Pharma Llc Fused-tricyclic inhibitors of KRAS and methods of use thereof
JP2021521179A (ja) * 2018-04-10 2021-08-26 ニューロポア セラピーズ インコーポレイテッド Ｖｐｓ３４の阻害剤としてのモルホリン誘導体
JP2021532157A (ja) * 2018-08-01 2021-11-25 アラクセス ファーマ エルエルシー がんを処置するための複素環式スピロ化合物およびその使用方法

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TW200801012A (en) * 2006-04-26 2008-01-01 Piramed Ltd Phosphoinositide 3-kinase inhibitor compounds and methods of use
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
MX353308B (es) 2008-05-21 2018-01-08 Ariad Pharma Inc Derivados fosforosos como inhibidores de cinasa.
US9556426B2 (en) 2009-09-16 2017-01-31 Celgene Avilomics Research, Inc. Protein kinase conjugates and inhibitors
US8946197B2 (en) 2009-11-16 2015-02-03 Chdi Foundation, Inc. Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof
JP2013516422A (ja) 2009-12-30 2013-05-13 アビラ セラピューティクス， インコーポレイテッド タンパク質のリガンド−指向性共有的修飾
US9295673B2 (en) 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
CA2829558A1 (en) * 2011-03-09 2012-09-13 Celgene Avilomics Research, Inc. Pi3 kinase inhibitors and uses thereof
EP2704572B1 (en) 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
WO2012154608A1 (en) * 2011-05-06 2012-11-15 Intellikine, Llc Reactive mtor and pi3 kinase inhibitors and uses thereof
WO2012154610A1 (en) * 2011-05-06 2012-11-15 Intellikine, Llc Reactive pi3k kinase inhibitors and uses thereof
US8889716B2 (en) 2011-05-10 2014-11-18 Chdi Foundation, Inc. Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof
JP2014520863A (ja) 2011-07-13 2014-08-25 ファーマサイクリックス，インク． Ｂｒｕｔｏｎ型チロシンキナーゼの阻害剤
BR112014007310A2 (pt) 2011-09-27 2017-04-04 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inibidores de idh mutante
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
UY34632A (es) 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
WO2013144180A1 (en) * 2012-03-28 2013-10-03 Intervet International B.V. Heteroaryl compounds with cyclic bridging unit for use in the treatment helminth infection
EP2836482B1 (en) 2012-04-10 2019-12-25 The Regents of The University of California Compositions and methods for treating cancer
US9879003B2 (en) 2012-04-11 2018-01-30 Dana-Farber Cancer Institute, Inc. Host targeted inhibitors of dengue virus and other viruses
HUE051096T2 (hu) 2012-04-26 2021-03-01 Massachusetts Gen Hospital Ágensek és módszerek a sebészeti keratózis kezelésére és megelõzésére
WO2013169401A1 (en) 2012-05-05 2013-11-14 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
US20150204846A1 (en) * 2012-05-15 2015-07-23 New York University Phosphatidylinositol-3-kinase c2 beta modulators and methods of use thereof
WO2014012093A1 (en) * 2012-07-13 2014-01-16 Wake Forest University Health Sciences Prostate cancer targeted prodrugs and methods of use thereof
WO2014022569A1 (en) * 2012-08-03 2014-02-06 Principia Biopharma Inc. Treatment of dry eye
CA2879597C (en) 2012-08-21 2021-01-12 Opko Pharmaceuticals, Llc Ophthalmic liposome formulations for treating posterior segment disease
US11458199B2 (en) 2012-08-21 2022-10-04 Opko Pharmaceuticals, Llc Liposome formulations
SI2892900T1 (en) 2012-09-10 2018-01-31 Principia Biopharma Inc. Pyrazolopyrimidine compounds as kinase inhibitors
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WO2011031896A2 (en) 2011-03-17
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RU2012110024A (ru) 2013-11-10
EP2475375A4 (en) 2013-02-20
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