HK1199020A1 - -二氫吡嗪並 吡嗪- -種化合物作為用於與 /途徑相關的腫瘤適應症和疾病的 激酶抑制劑 - Google Patents

-二氫吡嗪並 吡嗪- -種化合物作為用於與 /途徑相關的腫瘤適應症和疾病的 激酶抑制劑

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Publication number
HK1199020A1
HK1199020A1 HK14112447.8A HK14112447A HK1199020A1 HK 1199020 A1 HK1199020 A1 HK 1199020A1 HK 14112447 A HK14112447 A HK 14112447A HK 1199020 A1 HK1199020 A1 HK 1199020A1
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Hong Kong
Prior art keywords
mtor
akt
dihydropyrazino
pi3k
pyrazin
Prior art date
Application number
HK14112447.8A
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English (en)
Inventor
簡．埃爾斯納
洛伊．
．哈瑞斯
布蘭登．李
黛博拉．莫特森
加里克．帕卡德
帕特里克．帕佩
索菲．佩蘭-寧科維奇
詹尼弗．里格斯
薩比塔．桑卡爾
約翰．塞派澤
格拉茨埃拉．謝烏林
琳達．泰赫拉尼
許衛明
趙晶晶
詹森．帕尼斯
隆伊．瑪達卡姆提
金柏莉．富特茲
拉瑪．
．娜爾拉
Original Assignee
西格諾藥品有限公司
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41490345&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HK1199020(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 西格諾藥品有限公司 filed Critical 西格諾藥品有限公司
Publication of HK1199020A1 publication Critical patent/HK1199020A1/zh

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
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    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
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    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds

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  • Veterinary Medicine (AREA)
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  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Psychology (AREA)
  • Endocrinology (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
HK14112447.8A 2008-10-27 2014-12-10 -二氫吡嗪並 吡嗪- -種化合物作為用於與 /途徑相關的腫瘤適應症和疾病的 激酶抑制劑 HK1199020A1 (zh)

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US10862708P 2008-10-27 2008-10-27

Publications (1)

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HK1199020A1 true HK1199020A1 (zh) 2015-06-19

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HK11109149.8A HK1154858A1 (zh) 2008-10-27 2011-08-30 用於與 途徑相關的腫瘤適應症和疾病的 激酶抑制劑
HK14112450.2A HK1200442A1 (zh) 2008-10-27 2014-12-10 用於與 /途徑相關的腫瘤適應症和疾病的 激酶抑制劑
HK14112447.8A HK1199020A1 (zh) 2008-10-27 2014-12-10 -二氫吡嗪並 吡嗪- -種化合物作為用於與 /途徑相關的腫瘤適應症和疾病的 激酶抑制劑

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HK11109149.8A HK1154858A1 (zh) 2008-10-27 2011-08-30 用於與 途徑相關的腫瘤適應症和疾病的 激酶抑制劑
HK14112450.2A HK1200442A1 (zh) 2008-10-27 2014-12-10 用於與 /途徑相關的腫瘤適應症和疾病的 激酶抑制劑

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US (10) US8110578B2 (zh)
EP (5) EP3660020B1 (zh)
JP (3) JP5689420B2 (zh)
KR (2) KR101815604B1 (zh)
CN (3) CN102245611B (zh)
AR (2) AR073995A1 (zh)
AU (1) AU2009320137C1 (zh)
BR (1) BRPI0920254A2 (zh)
CA (1) CA2740975C (zh)
CO (1) CO6501147A2 (zh)
CR (1) CR20110223A (zh)
CY (2) CY1117272T1 (zh)
DK (2) DK2740732T3 (zh)
EC (1) ECSP11011084A (zh)
ES (4) ES2620774T3 (zh)
HK (3) HK1154858A1 (zh)
HR (2) HRP20160084T1 (zh)
HU (1) HUE026834T2 (zh)
IL (1) IL212440A (zh)
LT (1) LT2740732T (zh)
MX (2) MX2011004401A (zh)
MY (1) MY159235A (zh)
NI (1) NI201100080A (zh)
NZ (4) NZ603831A (zh)
PE (3) PE20110575A1 (zh)
PL (2) PL2740732T3 (zh)
PT (1) PT2740732T (zh)
RU (2) RU2546658C2 (zh)
SG (3) SG10201402273RA (zh)
SI (2) SI2740733T1 (zh)
SM (1) SMT201600089B (zh)
TW (3) TWI605047B (zh)
UA (1) UA108601C2 (zh)
WO (1) WO2010062571A1 (zh)
ZA (1) ZA201102813B (zh)

Families Citing this family (115)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LT2300013T (lt) 2008-05-21 2017-12-27 Ariad Pharmaceuticals, Inc. Fosforo dariniai kaip kinazių inhibitoriai
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
US8110578B2 (en) 2008-10-27 2012-02-07 Signal Pharmaceuticals, Llc Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
WO2010056311A1 (en) 2008-11-12 2010-05-20 Ariad Pharmaceuticals, Inc. Pyrazinopyrazines and derivatives as kinase inhibitors
DE102009043260A1 (de) 2009-09-28 2011-04-28 Merck Patent Gmbh Pyridinyl-imidazolonderivate
NZ599549A (en) 2009-10-26 2013-11-29 Signal Pharm Llc Methods of synthesis and purification of heteroaryl compounds
BR112012019459A2 (pt) * 2010-02-03 2017-10-17 Signal Pharm Llc identificação de mutação de lkb1 como um biomarcador preditivo para sensibilidade para inibidores de tor quinase.
US20110275699A1 (en) * 2010-03-16 2011-11-10 University Of California Treatment For Obesity And Diabetes
US20120028972A1 (en) * 2010-07-30 2012-02-02 Lilly Wong Biomarker assays for detecting or measuring inhibition of tor kinase activity
CA2827673C (en) * 2011-02-18 2020-10-27 Novartis Pharma Ag Mtor/jak inhibitor combination therapy
WO2012122405A2 (en) * 2011-03-08 2012-09-13 The Trustees Of Columbia University In The City Of New York Screening assays using stem cells and stem cell-derived neurons from mouse models of alzheimer's disease
CN103501612B (zh) 2011-05-04 2017-03-29 阿里亚德医药股份有限公司 抑制表皮生长因子受体导致的癌症中细胞增殖的化合物
CN103857804A (zh) * 2011-08-03 2014-06-11 西格诺药品有限公司 作为lkb1状态的预测性生物标志物的基因表达谱的鉴定
AU2015200318B2 (en) * 2011-10-19 2016-10-20 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
WO2013059396A2 (en) * 2011-10-19 2013-04-25 Signal Pharmaceuticals, Llc Treatment of cancer with tor kinase inhibitors
CN104093398B (zh) * 2011-12-02 2017-03-15 西格诺药品有限公司 7‑(6‑(2‑羟基丙烷‑2‑基)吡啶‑3‑基)‑1‑((反式)‑4‑甲氧基环己基)‑3,4‑二氢吡嗪并[2,3‑b]吡嗪‑2(1h)‑酮、其固体形式的药物组合物及其使用方法
AU2015201807B2 (en) * 2011-12-02 2016-12-08 Signal Pharmaceuticals, Llc Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methocyclohexyl)-3,4-dihydropyrazino[2,3-b] pyrazin-2(1H)-one, a solid form thereof and methods of their use
WO2013109610A1 (en) * 2012-01-17 2013-07-25 Steven Hoffman Pharmaceutical compositions and methods
US8481498B1 (en) 2012-01-17 2013-07-09 Steven Hoffman Pharmaceutical compositions and methods
US10646552B2 (en) 2012-01-17 2020-05-12 Tyme, Inc. Pharmaceutical compositions and methods
US10272068B2 (en) 2012-01-17 2019-04-30 Tyme, Inc. Pharmaceutical compositions and methods
US20130183263A1 (en) 2012-01-17 2013-07-18 Steven Hoffman Pharmaceutical compositions and methods
FR2986230B1 (fr) * 2012-01-30 2014-03-07 Univ Paris Diderot Paris 7 Nouveaux composes et compositions utilises comme anticancereux
BR112014020786A2 (pt) 2012-02-24 2020-10-27 Signal Pharmaceuticals, Llc método para tratamento de câncer de pulmão, método para alcançar um critério de avaliação de resposta em tumores sólidos, método para aumento da sobrevivência
EA028414B1 (ru) * 2012-03-15 2017-11-30 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Лечение рака ингибиторами tor киназы
KR102057359B1 (ko) * 2012-03-15 2019-12-18 시그날 파마소티칼 엘엘씨 Tor 키나아제 억제제를 사용하는 암 치료법
KR20200034818A (ko) * 2012-03-15 2020-03-31 시그날 파마소티칼 엘엘씨 Tor 키나제 억제제를 사용한 암의 치료
AU2015213400B2 (en) * 2012-03-15 2017-07-27 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
CA2867174C (en) * 2012-03-15 2020-06-23 Signal Pharmaceuticals, Llc Treatment of cancer with tor kinase inhibitors
AU2015201138B2 (en) * 2012-03-15 2016-06-23 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
US20150166591A1 (en) 2012-05-05 2015-06-18 Ariad Pharmaceuticals, Inc. Methods and compositions for raf kinase mediated diseases
SG10201610416TA (en) 2012-06-13 2017-01-27 Incyte Corp Substituted tricyclic compounds as fgfr inhibitors
AU2013203714B2 (en) * 2012-10-18 2015-12-03 Signal Pharmaceuticals, Llc Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity
AU2013202768B2 (en) * 2012-10-18 2015-11-05 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
AU2015213397B2 (en) * 2012-10-18 2017-07-27 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
EA039396B1 (ru) * 2012-10-18 2022-01-24 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Лечение рака молочной железы с тройным негативным фенотипом ингибиторами tor-киназы
EP2945636B1 (en) 2013-01-16 2017-06-28 Signal Pharmaceuticals, LLC Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith
ES2797376T3 (es) 2013-01-24 2020-12-02 Palvella Therapeutics Inc Composiciones para la administración transdérmica de inhibidores de mTOR
AU2014223501A1 (en) 2013-02-28 2015-09-17 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
JP6382949B2 (ja) * 2013-04-17 2018-08-29 シグナル ファーマシューティカルズ，エルエルシー 癌を治療するためのｔｏｒキナーゼ阻害剤及び５−置換キナゾリノン化合物を含む組合せ療法
MX2015014589A (es) * 2013-04-17 2016-04-25 Signal Pharm Llc Tratamiento de cancer con dihidropirazino-pirazinas.
WO2014172426A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
MX2015014596A (es) * 2013-04-17 2016-03-03 Signal Pharm Llc Terapia de combinacion que comprende un inhibidor de tor cinasa y un compuesto imid para tratar cancer.
TW201527300A (zh) * 2013-04-17 2015-07-16 Signal Pharm Llc 關於１－乙基－７－（２－甲基－６－（１Ｈ－１，２，４－***－３－基）吡啶－３－基）－３，４－二氫吡并［２，３－ｂ］吡－２（１Ｈ）－酮之醫藥調配物、方法、固態型式及使用方法
WO2014172424A1 (en) * 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
EA029072B1 (ru) 2013-04-17 2018-02-28 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Комбинированная терапия, включающая соединение дигидропиразинопиразина и антагонист рецептора андрогена для лечения рака простаты
WO2014172432A1 (en) * 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer
BR112015026021A2 (pt) * 2013-04-17 2017-07-25 Signal Pharm Llc terapia de combinação compreendendo um inibidor de tor quinase e n-(3-(5-flúor-2-(4-(2-met-oxietoxi)fenilamino)pirimidin-4-ilamino)fenil)acrilamida para o tratamento de câncer
SI2986610T1 (en) 2013-04-19 2018-04-30 Incyte Holdings Corporation Bicyclic heterocycles as inhibitors of FGFR
NZ629486A (en) * 2013-05-29 2017-11-24 Signal Pharm Llc Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use
CN105792816A (zh) 2013-10-04 2016-07-20 西格诺药品有限公司 以基因突变为特征的癌症的预防或治疗中的tor激酶抑制剂
US9326962B2 (en) 2013-10-22 2016-05-03 Steven Hoffman Compositions and methods for treating intestinal hyperpermeability
US10751313B2 (en) 2013-10-22 2020-08-25 Yamo Pharmaceuticals Llc Compositions and methods for treating autism
US9585841B2 (en) 2013-10-22 2017-03-07 Tyme, Inc. Tyrosine derivatives and compositions comprising them
US9763903B2 (en) 2013-10-22 2017-09-19 Steven Hoffman Compositions and methods for treating intestinal hyperpermeability
US10813901B2 (en) 2013-10-22 2020-10-27 Yamo Pharmaceuticals Llc Compositions and methods for treating autism
WO2015069217A1 (en) * 2013-11-05 2015-05-14 Baylor College Of Medicine Src kinase inhibition as treatment for lympangioleiomyomatosis and tuberous sclerosis
NZ714742A (en) * 2014-04-16 2017-04-28 Signal Pharm Llc Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use
US9737535B2 (en) 2014-04-16 2017-08-22 Signal Pharmaceuticals, Llc Methods for treating cancer using TOR kinase inhibitor combination therapy comprising administering substituted pyrazino[2,3-b]pyrazines
US20150297605A1 (en) * 2014-04-16 2015-10-22 Signal Pharmaceuticals, Llc Methods for treating cancer using tor kinase inhibitor combination therapy
US9718824B2 (en) 2014-04-16 2017-08-01 Signal Pharmaceuticals, Llc Solid forms comprising 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, and a coformer, compositions and methods of use thereof
US9512129B2 (en) 2014-04-16 2016-12-06 Signal Pharmaceuticals, Llc Solid forms comprising 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one and a coformer
NZ629796A (en) 2014-07-14 2015-12-24 Signal Pharm Llc Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use
WO2016010886A1 (en) 2014-07-14 2016-01-21 Signal Pharmaceuticals, Llc Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof
CN107073066B (zh) 2014-09-11 2021-09-17 加利福尼亚大学董事会 mTORC1抑制剂
US9987241B2 (en) 2014-09-25 2018-06-05 The Board Of Regents Of The University Of Oklahoma Enzyme conjugate and prodrug cancer therapy
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
MX2020004108A (es) 2015-02-20 2022-01-03 Incyte Corp Heterociclos biciclicos como inhibidores de receptores del factor de crecimiento fibroblastico (fgfr).
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
JP2019509352A (ja) * 2016-03-23 2019-04-04 ルイス ハバシュ， ヒトの被験物質をニトロキシドで処理することによってａｐｏｐｔｏｓｉｓ関連遺伝子の発現レベルを増加させる
US10159665B2 (en) 2016-03-23 2018-12-25 Louis Habash Preventing amyloid plaque formation by treating a human subject with a nitroxide
US20180078539A1 (en) 2016-03-23 2018-03-22 Louis Habash T-cell regulation in t-cell mediated diseases by reducing pathogenic function of th17 in a human subject through treatment with a nitroxide
US10231959B2 (en) 2016-03-23 2019-03-19 Louis Habash Increasing expression level of apoptosis-related genes by treating a human subject with a nitroxide
US10818331B2 (en) 2016-09-27 2020-10-27 Spin Memory, Inc. Multi-chip module for MRAM devices with levels of dynamic redundancy registers
WO2018129364A1 (en) 2017-01-06 2018-07-12 Palvella Therapeutics Llc Anhydrous compositions of mtor inhibitors and methods of use
WO2018183868A1 (en) * 2017-03-31 2018-10-04 Bioventures, Llc Inhibitors of dna pk and uses thereof
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
IL271491B2 (en) 2017-06-22 2023-09-01 Celgene Corp Treatment of carcinoma of the liver characterized by hepatitis b virus infection
US11446365B2 (en) 2017-08-09 2022-09-20 The Board Of Regents Of The University Of Oklahoma Antimalarial enzyme conjugates, kits containing same, and methods of producing and using same
KR102133794B1 (ko) * 2017-08-24 2020-07-15 주식회사 셀투인 세포 소기관 내 글루타치온 측정용 실시간 형광 이미징 센서 및 이의 제조 방법
US10656994B2 (en) 2017-10-24 2020-05-19 Spin Memory, Inc. Over-voltage write operation of tunnel magnet-resistance (“TMR”) memory device and correcting failure bits therefrom by using on-the-fly bit failure detection and bit redundancy remapping techniques
EP3704229B1 (en) 2017-11-01 2023-12-20 Juno Therapeutics, Inc. Process for producing a t cell composition
KR102083916B1 (ko) 2017-11-23 2020-03-03 서울대학교산학협력단 대장암 진단을 위한 ｔｃｆ７ 돌연변이의 용도 및 게다토리십 약물내성을 갖는 대장암 치료용 조성물
CA3082337A1 (en) * 2017-12-04 2019-06-13 Bial - Portela & Ca, S.A. Dopamine-b-hydroxylase inhibitors
US10886330B2 (en) 2017-12-29 2021-01-05 Spin Memory, Inc. Memory device having overlapping magnetic tunnel junctions in compliance with a reference pitch
US10840439B2 (en) 2017-12-29 2020-11-17 Spin Memory, Inc. Magnetic tunnel junction (MTJ) fabrication methods and systems
US10596165B2 (en) 2018-02-12 2020-03-24 resTORbio, Inc. Combination therapies
MX2020011564A (es) 2018-05-01 2021-01-29 Revolution Medicines Inc Analogos de rapamicina unidos a c26 como inhibidores de mtor.
CA3098692A1 (en) 2018-05-01 2019-11-07 Revolution Medicines, Inc. C40-, c28-, and c-32-linked rapamycin analogs as mtor inhibitors
TW201946630A (zh) 2018-05-04 2019-12-16 美商英塞特公司 Fgfr抑制劑之鹽
WO2019213544A2 (en) 2018-05-04 2019-11-07 Incyte Corporation Solid forms of an fgfr inhibitor and processes for preparing the same
US10411185B1 (en) 2018-05-30 2019-09-10 Spin Memory, Inc. Process for creating a high density magnetic tunnel junction array test platform
EP3813946B1 (en) 2018-06-15 2024-05-22 Janssen Pharmaceutica NV Rapamycin analogs and uses thereof
WO2020010073A1 (en) 2018-07-02 2020-01-09 Palvella Therapeutics, Inc. ANHYDROUS COMPOSITIONS OF mTOR INHIBITORS AND METHODS OF USE
US10650875B2 (en) 2018-08-21 2020-05-12 Spin Memory, Inc. System for a wide temperature range nonvolatile memory
US11621293B2 (en) 2018-10-01 2023-04-04 Integrated Silicon Solution, (Cayman) Inc. Multi terminal device stack systems and methods
US10971680B2 (en) 2018-10-01 2021-04-06 Spin Memory, Inc. Multi terminal device stack formation methods
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
UY38806A (es) 2019-08-01 2021-02-26 Novartis Ag Compuestos inhibidores tricíclicos de kars dependientes de akr1c3, composiciones y sus usos
IL291901A (en) 2019-10-14 2022-06-01 Incyte Corp Bicyclyl heterocycles as fgr suppressors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021113462A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Derivatives of an fgfr inhibitor
BR112022010754A2 (pt) 2019-12-05 2022-08-23 Anakuria Therapeutics Inc Análogos de rapamicina e usos dos mesmos
CN115151532B (zh) * 2020-04-29 2023-06-06 北京泰德制药股份有限公司 喹喔啉二酮衍生物作为kras g12c突变蛋白的不可逆抑制剂
JP2023534551A (ja) * 2020-07-22 2023-08-09 南京正大天晴制薬有限公司 Ａｋｔ阻害剤の単位剤形組成物
WO2022166866A1 (zh) * 2021-02-08 2022-08-11 南京明德新药研发有限公司 二氢吡嗪并吡嗪类大环化合物
CA3207998A1 (en) 2021-02-16 2022-08-25 Geoffrey M. Lynn Self-assembling nanoparticles based on amphiphilic peptides
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
WO2022266251A1 (en) * 2021-06-16 2022-12-22 The Board Of Trustees Of The Leland Stanford Junior University Compositions for treatment of psoriasis
WO2023170107A1 (en) 2022-03-07 2023-09-14 Centre Hospitalier Universitaire Vaudois (Chuv) Pi3k/akt/mtor inhibitor for improving the cellular uptake of a radiopharmaceutical
WO2024092030A1 (en) 2022-10-25 2024-05-02 Vaccitech North America, Inc. Self-assembling nanoparticles

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE262026C (zh)
US3507866A (en) 1967-08-08 1970-04-21 Merck & Co Inc 1h - imidazo(4,5-b)pyrazin - 2 - one and processes for their preparation
US3567725A (en) 1968-11-20 1971-03-02 Merck & Co Inc Process for preparation of 1h-imidazo-(4,5-b)pyrazin-2-ones
US4294837A (en) 1980-03-28 1981-10-13 Sterling Drug Inc. 1,3-Dihydro-6-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones and -imidazo[4,5-b]pyridine-2-thiones and their cardiotonic use
US4294836A (en) 1980-03-24 1981-10-13 Sterling Drug Inc. 1,3-Dihydro-6-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones and -imidazo[4,5-b]-pyridine-2-thiones and their cardiotonic use
US4317909A (en) 1980-03-24 1982-03-02 Sterling Drug Inc. Preparation of 1,3-dihydro-5-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones
US4309537A (en) 1980-03-28 1982-01-05 Sterling Drug Inc. Production of imidazo[4,5-b]pyridin-2-ones or thiones
GB8709448D0 (en) 1987-04-21 1987-05-28 Pfizer Ltd Heterobicyclic quinoline derivatives
JPS63275582A (ja) 1987-05-02 1988-11-14 Naade Kenkyusho:Kk ２−アミノイミダゾ〔４，５−ｂ〕ピリジン誘導体の製造方法
DD262026A1 (de) 1987-07-10 1988-11-16 Akad Wissenschaften Ddr Verfahren zur herstellung von 4-substituierten 6-(pyrid-4-yl)-2,4-dihydro-1h-imidazo[4,5-b]pyrid-2-onen
FR2643903A1 (fr) 1989-03-03 1990-09-07 Union Pharma Scient Appl Nouveaux derives de benzimidazole, leurs procedes de preparation, intermediaires de synthese, compositions pharmaceutiques les contenant, utiles notamment pour le traitement des maladies cardiovasculaires, et des ulceres duodenaux
US4963561A (en) 1990-02-28 1990-10-16 Sterling Drug Inc. Imidazopyridines, their preparation and use
TW274550B (zh) 1992-09-26 1996-04-21 Hoechst Ag
WO1995003009A1 (en) 1993-07-22 1995-02-02 Oculex Pharmaceuticals, Inc. Method of treatment of macular degeneration
WO1995003807A1 (en) 1993-07-27 1995-02-09 The University Of Sydney Treatment of age-related macular degeneration
TJ342B (en) * 1994-11-14 2002-10-06 Warner Lambert Co Derivatives of 6-aryl pyrido Ä2,3-dÜ pyrimidines and naphthyridines pharmaceutical composition possess inhibiting effect of cellular proliferation pr ovoking protein tyrosine kinase and method of inhibiting cellular proliferation
IT1274549B (it) 1995-05-23 1997-07-17 Indena Spa Uso di flavanolignani per la preparazione di medicamenti ad attivita' antiproliferativa nei tumori dell'utero,dell'ovaio e del seno
DE19601627A1 (de) 1996-01-18 1997-07-24 Bayer Ag Heteroatomhaltige Cyclopentanopyridyl-Oxazolidinone
US5800819A (en) 1996-01-25 1998-09-01 National Institute For Pharmaceutical Research And Development Federal Ministry Of Science And Technology Piper guineense, pterocarpus osun, eugenia caryophyllata, and sorghum bicolor extracts for treating sickle cell disease
US5635517B1 (en) 1996-07-24 1999-06-29 Celgene Corp Method of reducing TNFalpha levels with amino substituted 2-(2,6-dioxopiperidin-3-YL)-1-oxo-and 1,3-dioxoisoindolines
US6281230B1 (en) 1996-07-24 2001-08-28 Celgene Corporation Isoindolines, method of use, and pharmaceutical compositions
WO1999016438A1 (en) 1997-09-26 1999-04-08 Asta Medica Aktiengesellschaft Azabenzimidazole-based compounds for modulating serine/threonine protein kinase function
ZA9810490B (en) 1997-12-03 1999-05-20 Dainippon Pharmaceutical Co 2-Aryl-8-oxodihydropurine derivative process for the preparation thereof pharmaceutical composition containing the same and intermediate therefor
US6015803A (en) 1998-05-04 2000-01-18 Wirostko; Emil Antibiotic treatment of age-related macular degeneration
US6225348B1 (en) 1998-08-20 2001-05-01 Alfred W. Paulsen Method of treating macular degeneration with a prostaglandin derivative
US6001368A (en) 1998-09-03 1999-12-14 Protein Technologies International, Inc. Method for inhibiting or reducing the risk of macular degeneration
JP2003146987A (ja) 1999-05-31 2003-05-21 Dainippon Pharmaceut Co Ltd ２−アリールプリン−９−アセトアミド誘導体
JP3814125B2 (ja) 1999-06-02 2006-08-23 大日本住友製薬株式会社 ２−アリール−８−オキソジヒドロプリン誘導体からなる医薬
PT1257537E (pt) * 2000-01-24 2007-08-03 Astrazeneca Ab Compostos terapêuticos morfolino-substituídos.
JP2002167387A (ja) 2000-11-29 2002-06-11 Dainippon Pharmaceut Co Ltd ２−（７，８−ジヒドロ−８−オキソ−９ｈ−プリン−９−イル）酢酸誘導体
BR0116113A (pt) 2000-12-12 2004-08-03 Neurogen Corp Espiro[isobenzofuran-1,4'-piperidin]-3-onas e 3h-espiroisoben-zofuran-1,4'-piperidinas
WO2002086989A2 (en) 2001-04-24 2002-10-31 Broadcom Corporation Alerting system, architecture and circuitry
CN1551881A (zh) 2001-09-04 2004-12-01 ���ָ��Ӣ��ķ�������Ϲ�˾ 新颖二氢喋啶酮,其制备方法及作为药物组合物的用途
CA2462441A1 (en) 2001-10-18 2003-04-24 Pier F. Cirillo 1,4-disubstituted benzo-fused urea compounds as cytokine inhibitors
US7968569B2 (en) 2002-05-17 2011-06-28 Celgene Corporation Methods for treatment of multiple myeloma using 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione
US20040204420A1 (en) 2002-08-05 2004-10-14 Rana Tariq M. Compounds for modulating RNA interference
US7189740B2 (en) 2002-10-15 2007-03-13 Celgene Corporation Methods of using 3-(4-amino-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione for the treatment and management of myelodysplastic syndromes
US20040091455A1 (en) 2002-10-31 2004-05-13 Zeldis Jerome B. Methods of using and compositions comprising immunomodulatory compounds for treatment and management of macular degeneration
US7563810B2 (en) 2002-11-06 2009-07-21 Celgene Corporation Methods of using 3-(4-amino-1-oxo-1,3-dihydroisoindol-2-yl)-piperidine-2,6-dione for the treatment and management of myeloproliferative diseases
DE602004021558D1 (de) 2003-01-17 2009-07-30 Warner Lambert Co 2-aminopyridin-substituierteheterocyclen als inhibitoren der zellulären proliferation
BR0318145A (pt) 2003-02-26 2006-02-21 Boehringer Ingelheim Pharma dihidropteridinonas, processos para a sua preparação e sua aplicação como medicamento
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
US20050100529A1 (en) 2003-11-06 2005-05-12 Zeldis Jerome B. Methods of using and compositions comprising immunomodulatory compounds for the treatment and management of asbestos-related diseases and disorders
RU2006121990A (ru) * 2003-11-21 2007-12-27 Эррэй Биофарма Инк. (Us) Ингибиторы протеинкиназ акт
EP2505200A1 (en) 2004-03-22 2012-10-03 Celgene Corporation Methods of using and compositions comprising immunomodulatory compounds for the treatment and management of scleroderma
WO2005097107A2 (en) * 2004-04-08 2005-10-20 Topotarget A/S Diphenyl - indol-2-on compounds and their use in the treatment of cancer
US20050239842A1 (en) 2004-04-23 2005-10-27 Zeldis Jerome B Methods of using and compositions comprising immunomodulatory compounds for the treatment and management of pulmonary hypertension
CA2569406A1 (en) 2004-06-04 2005-12-22 Icos Corporation Methods for treating mast cell disorders
DE102004029784A1 (de) 2004-06-21 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 2-Benzylaminodihydropteridinone, Verfahren zur deren Herstellung und deren Verwendung als Arzneimittel
WO2006001266A1 (ja) 2004-06-23 2006-01-05 Banyu Pharmaceutical Co., Ltd. ２－アリールプリン誘導体の製造方法
WO2006020755A2 (en) 2004-08-10 2006-02-23 Beth Israel Deaconess Medical Center, Inc. Methods for identifying inhibitors of the mtor pathway as diabetes therapeutics
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
WO2006036883A2 (en) 2004-09-24 2006-04-06 Janssen Pharmaceutica, N.V. Imidazo{4,5-b}pyrazinone inhibitors of protein kinases
JP5118972B2 (ja) 2004-10-29 2013-01-16 テイボテク・フアーマシユーチカルズ Ｈｉｖ阻害性二環式ピリミジン誘導体
CN101098694A (zh) 2004-11-12 2008-01-02 细胞基因公司 使用免疫调节化合物治疗和控制寄生性疾病的方法和组合物
WO2006058008A1 (en) 2004-11-23 2006-06-01 Celgene Corporation Methods and compositions using immunomodulatory compounds for treatment and management of central nervous system injury
CN101111234A (zh) 2004-12-01 2008-01-23 细胞基因公司 包含免疫调节化合物的组合物及其治疗免疫缺陷疾病的用途
WO2006065703A1 (en) 2004-12-13 2006-06-22 Sunesis Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors
WO2006091737A1 (en) 2005-02-24 2006-08-31 Kemia, Inc. Modulators of gsk-3 activity
JP2008531538A (ja) * 2005-02-25 2008-08-14 クドス ファーマシューティカルズ リミテッド ２，４−ジアミノ−ピリドピリミジン誘導体とｍＴＯＲ阻害剤としてのその使用
EP1874772A1 (en) 2005-04-05 2008-01-09 Pharmacopeia, Inc. Purine and imidazopyridine derivatives for immunosuppression
ES2436877T3 (es) * 2005-11-17 2014-01-07 OSI Pharmaceuticals, LLC Intermedios para la preparación de inhibidores de mTOR bicíclicos condensados
PT2069352E (pt) 2006-08-02 2014-01-02 Cytokinetics Inc Certas entidades químicas, composições e métodos
EP2078016B1 (en) 2006-10-19 2012-02-01 Signal Pharmaceuticals LLC Heteroaryl compounds, compositions thereof, and methods of treatment therewith
CA2679659C (en) 2007-03-01 2016-01-19 Novartis Ag Pim kinase inhibitors and methods of their use
US8110578B2 (en) * 2008-10-27 2012-02-07 Signal Pharmaceuticals, Llc Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
NZ599549A (en) 2009-10-26 2013-11-29 Signal Pharm Llc Methods of synthesis and purification of heteroaryl compounds

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