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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Publication number
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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Japanese (ja)
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JP2013504325A5 (enExample
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
    • 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)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Wood Science & Technology (AREA)
  • Molecular Biology (AREA)
  • Zoology (AREA)
  • 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)
  • Oncology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biochemistry (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 (enExample) 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 (enExample)
EP (1) EP2475375A4 (enExample)
JP (1) JP2013504325A (enExample)
KR (1) KR20120063515A (enExample)
CN (1) CN102625708A (enExample)
AU (1) AU2010292198A1 (enExample)
BR (1) BR112012008385A2 (enExample)
CA (1) CA2773848A1 (enExample)
IL (1) IL218555A0 (enExample)
MX (1) MX339584B (enExample)
NZ (2) NZ598808A (enExample)
PH (1) PH12012500491A1 (enExample)
RU (1) RU2595718C2 (enExample)
SG (2) SG10201405598QA (enExample)
TW (2) TW201609747A (enExample)
WO (1) WO2011031896A2 (enExample)

Cited By (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Families Citing this family (123)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101402474B1 (ko) * 2006-04-26 2014-06-19 제넨테크, 인크. 포스포이노시티드 3-키나제 억제제 화합물 및 이를 포함하는 약학적 조성물
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
PL2300013T5 (pl) 2008-05-21 2025-04-28 Takeda Pharmaceutical Company Limited Pochodne fosforu jako inhibitor kinazy
EP2478361A4 (en) 2009-09-16 2014-05-21 Celgene Avilomics Res Inc CONJUGATES AND INHIBITORS OF PROTEIN KINASE
WO2011060321A1 (en) 2009-11-16 2011-05-19 Chdi, Inc. Transglutaminase tg2 inhibitors, pharmaceutical compositions, and methods of use thereof
CN102812167A (zh) 2009-12-30 2012-12-05 阿维拉制药公司 蛋白的配体-介导的共价修饰
JP6130305B2 (ja) 2011-02-23 2017-05-17 インテリカイン， エルエルシー キナーゼ阻害剤の組み合わせおよびそれらの使用
US20120258967A1 (en) * 2011-03-09 2012-10-11 Avila Therapeutics, 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
AU2012283775A1 (en) 2011-07-13 2014-01-23 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase
MX342326B (es) 2011-09-27 2016-09-26 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras 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
US20150087628A1 (en) 2012-04-10 2015-03-26 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
AU2013251475B2 (en) 2012-04-26 2018-01-04 The General Hospital Corporation Agents and methods for treating and preventing seborrheic keratosis
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物
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
US9572811B2 (en) 2012-08-03 2017-02-21 Principia Biopharma Inc. Treatment of dry eye
US11458199B2 (en) 2012-08-21 2022-10-04 Opko Pharmaceuticals, Llc Liposome formulations
HUE058912T2 (hu) 2012-08-21 2022-09-28 Opko Pharmaceuticals Llc Liposzóma készítmények
SMT201900344T1 (it) 2012-09-10 2019-07-11 Principia Biopharma Inc Composti di pirazolopirimidina come inibitori di chinasi
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
US9296733B2 (en) 2012-11-12 2016-03-29 Novartis Ag Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases
NZ708870A (en) 2012-12-21 2016-09-30 Gilead Calistoga Llc Isoquinolinone or quinazolinone phosphatidylinositol 3-kinase inhibitors
JP6125663B2 (ja) 2012-12-21 2017-05-10 ギリアード カリストガ エルエルシー ホスファチジルイノシトール３−キナーゼ阻害剤としての置換ピリミジンアミノアルキル−キナゾロン
PE20151939A1 (es) 2013-03-14 2016-01-08 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutante
US10202356B2 (en) 2013-03-14 2019-02-12 Tolero Pharmaceuticals, Inc. JAK2 and ALK2 inhibitors and methods for their use
CN105246482A (zh) * 2013-03-15 2016-01-13 因特利凯有限责任公司 激酶抑制剂的组合及其用途
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
US10508309B2 (en) * 2013-05-17 2019-12-17 The General Hospital Corporation Methods for detecting and treating variants of seborrheic keratoses
NZ714710A (en) 2013-06-14 2016-11-25 Gilead Sciences Inc Phosphatidylinositol 3-kinase inhibitors
UY35675A (es) 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
US9624224B2 (en) 2013-09-30 2017-04-18 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase
WO2015057655A1 (en) 2013-10-14 2015-04-23 Eisai R&D Management Co., Ltd. Selectively substituted quinoline compounds
MD4635C1 (ro) 2013-10-14 2020-01-31 Eisai R&D Management Co., Ltd. Compuşi de chinolină substituiţi selectiv
ES2676734T3 (es) * 2013-10-18 2018-07-24 Syros Pharmaceuticals, Inc. Compuestos heteroatómicos útiles para el tratamiento de enfermedades proliferativas
AU2014352463B2 (en) * 2013-11-20 2017-05-11 Beijing Forelandpharma Co. Ltd. Ketone derivatives of imidazoles, pharmaceutical combinations and uses thereof
KR102331833B1 (ko) 2013-12-02 2021-11-25 케모센트릭스, 인크. Ccr6 화합물
KR20220027271A (ko) 2014-02-21 2022-03-07 프린시피아 바이오파마, 인코퍼레이티드 Btk 억제제의 염 및 고체 형태
US9862701B2 (en) 2014-09-25 2018-01-09 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
CA2970723C (en) 2014-12-18 2023-09-05 Principia Biopharma Inc. Treatment of pemphigus
RU2704826C2 (ru) * 2014-12-24 2019-10-31 Китер Бьотек С.Р.Л. НОВЫЙ ПЕПТИД-ИНГИБИТОР PI3Kγ ДЛЯ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ ОРГАНОВ ДЫХАНИЯ
EP3280708B1 (en) 2015-04-10 2021-09-01 Araxes Pharma LLC Substituted quinazoline compounds and methods of use thereof
WO2016172952A1 (zh) 2015-04-30 2016-11-03 江苏挪贝肽医药科技有限公司 PI4KIIIα蛋白及相关的膜蛋白复合体在治疗阿尔茨海默病中的应用
EP3297629A1 (en) 2015-05-20 2018-03-28 Novartis AG Pharmaceutical combination of everolimus with dactolisib
MA42242A (fr) 2015-06-24 2018-05-02 Principia Biopharma Inc Inhibiteurs de la tyrosine kinase
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
US10647703B2 (en) 2015-09-28 2020-05-12 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10858343B2 (en) 2015-09-28 2020-12-08 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058792A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10975071B2 (en) 2015-09-28 2021-04-13 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058807A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10730867B2 (en) 2015-09-28 2020-08-04 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3364977A4 (en) 2015-10-19 2019-09-04 Araxes Pharma LLC PROCESS FOR SCREENING INHIBITORS OF RAS
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
RU2617694C1 (ru) * 2015-12-24 2017-04-26 Федеральное государственное бюджетное учреждение науки Институт элементоорганических соединений им. А.Н. Несмеянова Российской академии наук (ИНЭОС РАН) Амиды акриловой и метакриловой кислот с олигопиперидинами и способ их получения
RU2617409C1 (ru) * 2015-12-24 2017-04-25 Федеральное государственное бюджетное учреждение науки Институт элементоорганических соединений им. А.Н. Несмеянова Российской академии наук (ИНЭОС РАН) Амиды акриловой и метакриловой кислот с n-алкилпиперазино-пиперидинами и способ их получения
GB201602527D0 (en) * 2016-02-12 2016-03-30 Glaxosmithkline Ip Dev Ltd Chemical compounds
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
EP3464275B1 (en) 2016-05-26 2024-05-08 Recurium IP Holdings, LLC Egfr inhibitor compounds
WO2018005849A1 (en) 2016-06-29 2018-01-04 Principia Biopharma Inc. Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
WO2018002958A1 (en) 2016-06-30 2018-01-04 Sun Pharma Advanced Research Company Limited Novel hydrazide containing compounds as btk inhibitors
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
BR112019010470A2 (pt) 2016-11-23 2019-09-10 Novartis Ag métodos de realce de resposta imune com everolimo, dactolisib ou ambos
CN106755343A (zh) * 2016-12-01 2017-05-31 北京致成生物医学科技有限公司 胰腺癌预后诊断分子标记物
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
WO2018140600A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused hetero-hetero bicyclic compounds and methods of use thereof
WO2018140512A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
WO2018140514A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
US11279689B2 (en) 2017-01-26 2022-03-22 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer
WO2018195649A1 (en) * 2017-04-26 2018-11-01 Alberta Research Chemicals Inc. Substituted tetrahydropyridine derivatives as ido-1 inhibitors and uses thereof
CN110869357A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 化合物及其用于治疗癌症的使用方法
US11639346B2 (en) 2017-05-25 2023-05-02 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS
AU2018271990A1 (en) 2017-05-25 2019-12-12 Araxes Pharma Llc Covalent inhibitors of KRAS
US10596165B2 (en) 2018-02-12 2020-03-24 resTORbio, Inc. Combination therapies
CA3096984A1 (en) 2018-04-05 2019-10-10 Sumitomo Dainippon Pharma Oncology, Inc. Axl kinase inhibitors and use of the same
ES3032793T3 (en) 2018-04-10 2025-07-24 Neuropore Therapies Inc Tri-substituted aryl and heteroaryl derivatives as modulators of pi3-kinase and autophagy pathways
MX2021000977A (es) 2018-07-26 2021-04-12 Sumitomo Pharma Oncology Inc Metodos para tratar enfermedades asociadas con expresion anormal de receptor de activina a tipo 1 (acvr1) e inhibidores de acvr1 para uso en los mismos.
KR102328682B1 (ko) 2018-08-27 2021-11-18 주식회사 대웅제약 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물
EP3849545A1 (en) * 2018-09-10 2021-07-21 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of neurofibromatosis
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
CN120789282A (zh) * 2019-09-19 2025-10-17 托特斯医药公司 治疗性缀合物
TWI877239B (zh) 2019-10-14 2025-03-21 美商普林斯匹亞生物製藥公司 藉由投予(R)-2-[3-[4-胺基-3-(2-氟-4-苯氧基-苯基)吡唑并[3,4-d]嘧啶-1-基]哌啶-1-羰基]-4-甲基-4-[4-(氧呾-3-基)哌-1-基]戊-2-烯腈來治療免疫血小板減少症之方法
EP4045485A1 (en) 2019-10-18 2022-08-24 The Regents Of The University Of California 3-phenylsulphonyl-quinoline derivatives as agents for treating pathogenic blood vessels disorders
WO2021142252A1 (en) * 2020-01-10 2021-07-15 Incyte Corporation Tricyclic compounds as inhibitors of kras
US11530218B2 (en) 2020-01-20 2022-12-20 Incyte Corporation Spiro compounds as inhibitors of KRAS
BR112022014149A2 (pt) 2020-01-22 2022-09-27 Principia Biopharma Inc Formas cristalinas de 2-[3-[4-amino-3-(2-fluoro-4-fenóxi-fenil)-1h-pirazolo[3,4-d]pirimidina-1-il]piperidina-1-carbonil]-4-metil-4-[4-(oxetan-3-il)piperazin-1-il]pent-2-enenitrila
TWI874791B (zh) 2020-02-18 2025-03-01 美商基利科學股份有限公司 抗病毒化合物
AR121356A1 (es) 2020-02-18 2022-05-11 Gilead Sciences Inc Compuestos antivirales
TWI883391B (zh) 2020-02-18 2025-05-11 美商基利科學股份有限公司 抗病毒化合物
WO2021231526A1 (en) 2020-05-13 2021-11-18 Incyte Corporation Fused pyrimidine compounds as kras inhibitors
WO2021242859A1 (en) * 2020-05-27 2021-12-02 Duke University Compositions and methods for sensitizing acute myeloid leukemias to chemotherapy
WO2022047093A1 (en) 2020-08-28 2022-03-03 Incyte Corporation Vinyl imidazole compounds as inhibitors of kras
WO2022072783A1 (en) 2020-10-02 2022-04-07 Incyte Corporation Bicyclic dione compounds as inhibitors of kras
CN113045582B (zh) * 2021-02-05 2022-12-23 中国药科大学 Parp-1/pi3k双靶点抑制剂或其药学上可接受的盐及其制备方法与用途
EP4308121A4 (en) * 2021-03-18 2025-02-19 Totus Medicines Inc. THERAPEUTIC CONJUGATES
WO2022204112A1 (en) 2021-03-22 2022-09-29 Incyte Corporation Imidazole and triazole kras inhibitors
CN117396470A (zh) * 2021-04-09 2024-01-12 巴塞尔大学 作为pi3k的可逆和不可逆共价抑制剂的三嗪衍生物
JP2024516361A (ja) * 2021-04-09 2024-04-15 ウニヴェアズィテート バーゼル Ｐｉ３ｋの可逆的および不可逆的共有結合性阻害剤としてのトリアジン誘導体
EP4323362B1 (en) 2021-04-16 2025-05-07 Gilead Sciences, Inc. Methods of preparing carbanucleosides using amides
WO2023283213A1 (en) 2021-07-07 2023-01-12 Incyte Corporation Tricyclic compounds as inhibitors of kras
TW202321191A (zh) * 2021-07-29 2023-06-01 美商賽迪拉治療股份有限公司 Ｔｅａｄ抑制劑及其用途
CA3228162A1 (en) 2021-08-18 2023-02-23 Gilead Sciences, Inc. Phospholipid compounds and methods of making and using the same
CA3229855A1 (en) 2021-08-31 2023-03-09 Incyte Corporation Naphthyridine compounds as inhibitors of kras
WO2023049697A1 (en) 2021-09-21 2023-03-30 Incyte Corporation Hetero-tricyclic compounds as inhibitors of kras
CN113754680B (zh) * 2021-09-28 2022-07-22 云白药征武科技(上海)有限公司 一种α氟代酰基哌嗪衍生物及其制备和应用
WO2023056421A1 (en) 2021-10-01 2023-04-06 Incyte Corporation Pyrazoloquinoline kras inhibitors
MX2024004444A (es) 2021-10-14 2024-05-08 Incyte Corp Compuestos de quinolina como inhibidores de la proteina del virus de sarcoma de rata kirsten (kras).
WO2024182447A1 (en) * 2023-02-28 2024-09-06 Vividion Therapeutics, Inc. Compounds and methods for modulating ras-pi3k
WO2025188658A1 (en) * 2024-03-06 2025-09-12 Alterome Therapeutics, Inc. Akt1 modulators

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009036082A2 (en) * 2007-09-12 2009-03-19 Genentech, Inc. Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
WO2009055730A1 (en) * 2007-10-25 2009-04-30 Genentech, Inc. Process for making thienopyrimidine compounds

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6667300B2 (en) * 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
HRP20131159B1 (hr) * 2002-09-30 2019-11-01 Bayer Ip Gmbh Taljeni azol-pirimidin derivati
AR046845A1 (es) * 2003-11-21 2005-12-28 Novartis Ag Derivados de 1h-imidazo[4,5-c]quinolina para tratamiento de enfermedades dependientes de las proteino-quinasas
RS55546B1 (sr) * 2004-05-13 2017-05-31 Icos Corp Hinazolinoni kao inhibitori humane fosfatidilonozitol 3-delta kinaze
AU2006214190A1 (en) * 2005-02-17 2006-08-24 Icos Corporation Phosphoinositide 3-kinase inhibitors for inhibiting leukocyte accumulation
JO2660B1 (en) * 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
EP2041139B1 (en) * 2006-04-26 2011-11-09 F. Hoffmann-La Roche AG Pharmaceutical compounds
KR101402474B1 (ko) * 2006-04-26 2014-06-19 제넨테크, 인크. 포스포이노시티드 3-키나제 억제제 화합물 및 이를 포함하는 약학적 조성물
GB0611152D0 (en) * 2006-06-06 2006-07-19 Ucb Sa Therapeutic agents
DK2050749T3 (en) * 2006-08-08 2018-01-08 Chugai Pharmaceutical Co Ltd PYRIMIDINE DERIVATIVES AS PI3K INHIBITOR AND USE THEREOF
US20080234262A1 (en) * 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
PE20090717A1 (es) * 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
CA2689989A1 (en) * 2007-06-04 2008-12-11 Avila Therapeutics, Inc. Heterocyclic compounds and uses thereof
GB0805818D0 (en) * 2008-03-31 2008-04-30 Ucb Pharma Sa Therapeutic agents
EA024252B1 (ru) * 2009-01-08 2016-08-31 Кьюрис, Инк. Ингибиторы фосфоинозитид-3-киназ с цинксвязывающей группой

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009036082A2 (en) * 2007-09-12 2009-03-19 Genentech, Inc. Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
WO2009055730A1 (en) * 2007-10-25 2009-04-30 Genentech, Inc. Process for making thienopyrimidine compounds

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
CURR. MED. CHEM., vol. 16, no. 22, JPN6015036544, August 2009 (2009-08-01), pages 2839 - 2854, ISSN: 0003151812 *
J. MED. CHEM., vol. pp.5522-5532, JPN6014049962, 2008, ISSN: 0003151811 *

Cited By (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP2021006574A (ja) * 2013-02-20 2021-01-21 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
US10273207B2 (en) 2013-03-15 2019-04-30 Araxes Pharma Llc Covalent inhibitors of kras G12C
USRE50527E1 (en) 2013-03-15 2025-08-12 Araxes Pharma Llc Covalent inhibitors of KRAS G12C
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
US10919850B2 (en) 2013-03-15 2021-02-16 Araxes Pharma Llc Covalent inhibitors of KRas G12C
JP2019085414A (ja) * 2013-03-15 2019-06-06 アラクセス ファーマ エルエルシー Ｋｒａｓ ｇ１２ｃの共有結合性阻害剤
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
US10028954B2 (en) 2013-04-30 2018-07-24 Genentech, Inc. Biheteroaryl compounds and uses thereof
US10010549B2 (en) 2013-05-01 2018-07-03 Genentech, Inc. Biheteroaryl compounds and uses thereof
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
US11129832B2 (en) 2013-05-01 2021-09-28 Genentech, Inc. Biheteroaryl compounds and uses thereof
USRE47848E1 (en) 2013-05-01 2020-02-11 Genentech, Inc. Biheteroaryl compounds and uses thereof
JP2020079264A (ja) * 2013-05-01 2020-05-28 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
JP2018035187A (ja) * 2013-05-01 2018-03-08 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
US10370386B2 (en) 2013-10-10 2019-08-06 Araxes Pharma Llc Substituted quinolines as inhibitors of KRAS G12C
US10111874B2 (en) 2014-09-18 2018-10-30 Araxes Pharma Llc Combination therapies for treatment of cancer
US10428064B2 (en) 2015-04-15 2019-10-01 Araxes Pharma Llc Fused-tricyclic inhibitors of KRAS 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
US10723738B2 (en) 2016-09-29 2020-07-28 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10280172B2 (en) 2016-09-29 2019-05-07 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS 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
JP7369140B2 (ja) 2018-04-10 2023-10-25 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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KR20120063515A (ko) 2012-06-15
AU2010292198A1 (en) 2012-04-05
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PH12012500491A1 (en) 2018-03-21
WO2011031896A3 (en) 2011-05-12
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WO2011031896A2 (en) 2011-03-17
BR112012008385A2 (pt) 2019-09-24

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