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
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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
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • 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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  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Neurology (AREA)
  • Wood Science & Technology (AREA)
  • Molecular Biology (AREA)
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  • Genetics & Genomics (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Biotechnology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
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  • Cardiology (AREA)
  • Psychology (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (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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JP2012528906A Pending JP2013504325A (ja) 2009-09-09 2010-09-09 Ｐｉ３キナーゼインヒビターおよびその使用

Country Status (16)

Country Link
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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CN101511840A (zh) * 2006-04-26 2009-08-19 吉宁特有限公司 磷酸肌醇3-激酶抑制剂化合物及其使用方法
PT2300013T (pt) 2008-05-21 2017-10-31 Ariad Pharma Inc Derivados de fósforo como inibidores de cinases
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
NZ620174A (en) 2009-09-16 2016-08-26 Celgene Avilomics Res Inc Protein kinase conjugates and inhibitors
WO2011060321A1 (en) 2009-11-16 2011-05-19 Chdi, Inc. Transglutaminase tg2 inhibitors, pharmaceutical compositions, and methods of use thereof
EP2519664A4 (en) 2009-12-30 2014-03-12 Avila Therapeutics Inc LIGAND-RELATED COVALENTS MODIFYING A PROTEIN
US9295673B2 (en) 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
EP2683243A4 (en) * 2011-03-09 2014-12-03 Celgene Avilomics Res Inc PI3 KINASE INHIBITORS AND USES THEREOF
US9834518B2 (en) 2011-05-04 2017-12-05 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in EGFR-driven cancers
WO2012154610A1 (en) * 2011-05-06 2012-11-15 Intellikine, Llc Reactive pi3k kinase inhibitors and uses thereof
WO2012154608A1 (en) * 2011-05-06 2012-11-15 Intellikine, Llc Reactive mtor and pi3 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
US9138436B2 (en) 2011-07-13 2015-09-22 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase
KR20140069235A (ko) 2011-09-27 2014-06-09 노파르티스 아게 돌연변이체 idh의 억제제로서의 3-피리미딘-4-일-옥사졸리딘-2-온
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
AU2013241854B2 (en) * 2012-03-28 2017-11-02 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
WO2013154778A1 (en) * 2012-04-11 2013-10-17 Dana-Farber Cancer Institute, Inc. Host targeted inhibitors of dengue virus and other viruses
DK2841075T3 (da) 2012-04-26 2020-06-22 Massachusetts Gen Hospital Midler og fremgangsmåder til behandling og forebyggelse af seboroisk keratose
US20150166591A1 (en) 2012-05-05 2015-06-18 Ariad Pharmaceuticals, Inc. Methods and compositions for raf kinase mediated diseases
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
KR102083700B1 (ko) 2012-08-21 2020-03-02 옵코 파마슈티칼스, 엘엘씨 리포좀 제제
US11458199B2 (en) 2012-08-21 2022-10-04 Opko Pharmaceuticals, Llc Liposome formulations
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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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