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PE20141197A1 - INHIBIDORES DE mTOR CINASA PARA INDICADORES DE ONCOLOGIA Y ENFERMEDADES ASOCIADAS CON LA TRAYECTORIA mTOR/PI3K/AKT - Google Patents

INHIBIDORES DE mTOR CINASA PARA INDICADORES DE ONCOLOGIA Y ENFERMEDADES ASOCIADAS CON LA TRAYECTORIA mTOR/PI3K/AKT

Info

Publication number
PE20141197A1
PE20141197A1 PE2014000555A PE2014000555A PE20141197A1 PE 20141197 A1 PE20141197 A1 PE 20141197A1 PE 2014000555 A PE2014000555 A PE 2014000555A PE 2014000555 A PE2014000555 A PE 2014000555A PE 20141197 A1 PE20141197 A1 PE 20141197A1
Authority
PE
Peru
Prior art keywords
mtor
pirazin
kinase inhibitors
methyl
pi3k
Prior art date
Application number
PE2014000555A
Other languages
English (en)
Inventor
Jan Elsner
Roy L Harris
Branden Lee
Deborah Mortensen
Garrick Packard
Patrick Papa
Rama K Narla
Kimberly Fultz
Loui Madakamutil
Jason Parnes
Jingjing Zhao
Weiming Xu
Sophie Perrin-Ninkovic
Lida Tehrani
Graziella Shevlin
John Sapienza
Sabita Sankar
Jennifer Riggs
Original Assignee
Signal Pharm Llc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41490345&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20141197(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Signal Pharm Llc filed Critical Signal Pharm Llc
Publication of PE20141197A1 publication Critical patent/PE20141197A1/es

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    • A61K31/495Heterocyclic 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
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Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE 3,4-DIHIDROPIRAZINO[2,3-b]PIRAZIN-2(1H)-ONA TALES COMO 6-(1H-PIRROLO[2,3-b]PIRIDIN-3-IL)-4-(2-(TETRAHIDRO-2H-PIRAN-4-IL)ETIL)-3,4-DIHIDROPIRAZINO[2,3-b]PIRAZIN-2(1H)-ONA; 6-(4-METIL-6-(1H-1,2,4-TRIAZOL-3-IL)PIRIDIN-3-IL)-4-((TETRAHIDRO-2H-PIRAN-4-IL)METIL)-3,4-DIHIDROPIRAZINO[2,3-b]PIRAZIN-2(1H)-ONA; 6-(5-FLUORO-2-METIL-4-(1H-1,2,4-TRIAZOL-3-IL)FENIL)-4-((TRANS-4-METOXICICLOHEXIL)METIL)-3,4-DIHIDROPIRAZINO[2,3-b]PIRAZIN-2(1H)-ONA; 6-(6-(1H-1,2,4-TRIAZOL-3-IL)PIRIDIN-3-IL)-4-((TRANS-4-METOXICICLOHEXIL)METIL)-3,4-DIHIDROPIRAZINO[2,3-b]PIRAZIN-2(1H)-ONA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE CINASA SIENDO UTILES EN EL TRATAMIENTO DEL CANCER, TRANSTORNOS INFLAMATORIOS, INMUNOLOGICOS
PE2014000555A 2008-10-27 2009-10-27 INHIBIDORES DE mTOR CINASA PARA INDICADORES DE ONCOLOGIA Y ENFERMEDADES ASOCIADAS CON LA TRAYECTORIA mTOR/PI3K/AKT PE20141197A1 (es)

Applications Claiming Priority (1)

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US10862708P 2008-10-27 2008-10-27

Publications (1)

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PE20141197A1 true PE20141197A1 (es) 2014-09-22

Family

ID=41490345

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Application Number Title Priority Date Filing Date
PE2011000936A PE20110575A1 (es) 2008-10-27 2009-10-27 INHIBIDORES DE mTOR CINASA PARA INDICADORES DE ONCOLOGIA Y ENFERMEDADES ASOCIADAS CON LA TRAYECTORIA mTOR/PI3K/AKT
PE2012002515A PE20130457A1 (es) 2008-10-27 2009-10-27 INHIBIDORES DE mTOR CINASA PARA INDICADORES DE ONCOLOGIA Y ENFERMEDADES ASOCIADAS CON LA TRAYECTORIA mTOR/PI3K/AKT
PE2014000555A PE20141197A1 (es) 2008-10-27 2009-10-27 INHIBIDORES DE mTOR CINASA PARA INDICADORES DE ONCOLOGIA Y ENFERMEDADES ASOCIADAS CON LA TRAYECTORIA mTOR/PI3K/AKT

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Application Number Title Priority Date Filing Date
PE2011000936A PE20110575A1 (es) 2008-10-27 2009-10-27 INHIBIDORES DE mTOR CINASA PARA INDICADORES DE ONCOLOGIA Y ENFERMEDADES ASOCIADAS CON LA TRAYECTORIA mTOR/PI3K/AKT
PE2012002515A PE20130457A1 (es) 2008-10-27 2009-10-27 INHIBIDORES DE mTOR CINASA PARA INDICADORES DE ONCOLOGIA Y ENFERMEDADES ASOCIADAS CON LA TRAYECTORIA mTOR/PI3K/AKT

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US (10) US8110578B2 (es)
EP (5) EP2358718B1 (es)
JP (3) JP5689420B2 (es)
KR (2) KR101815604B1 (es)
CN (3) CN104744475B (es)
AR (2) AR073995A1 (es)
AU (1) AU2009320137C1 (es)
BR (1) BRPI0920254A2 (es)
CA (1) CA2740975C (es)
CO (1) CO6501147A2 (es)
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PE (3) PE20110575A1 (es)
PL (2) PL2740733T3 (es)
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SG (3) SG10201402273RA (es)
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Families Citing this family (126)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
EA029131B1 (ru) 2008-05-21 2018-02-28 Ариад Фармасьютикалз, Инк. Фосфорсодержащие производные в качестве ингибиторов киназы
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
CA2743449C (en) 2008-11-12 2016-10-18 Ariad Pharmaceuticals, Inc. Pyrazinopyrazines and derivatives as kinase inhibitors
DE102009043260A1 (de) 2009-09-28 2011-04-28 Merck Patent Gmbh Pyridinyl-imidazolonderivate
CN102686225A (zh) * 2009-10-26 2012-09-19 西格诺药品有限公司 杂芳基化合物的合成和纯化方法
KR101942212B1 (ko) * 2010-02-03 2019-01-24 시그날 파마소티칼 엘엘씨 Tor 키나제 억제자에 대한 민감성 예측 바이오마커로서 lkb1 돌연변이의 동정
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
EA201391626A1 (ru) 2011-05-04 2014-03-31 Ариад Фармасьютикалз, Инк. Соединения для ингибирования клеточной пролиферации в egfr-стимулированных типах рака
WO2013019927A1 (en) * 2011-08-03 2013-02-07 Signal Pharmaceuticals, Llc Identification of gene expression profile as a predictive biomarker for lkb1 status
TWI629983B (zh) * 2011-10-19 2018-07-21 標誌製藥公司 以tor激酶抑制劑治療癌症
AU2015200318B2 (en) * 2011-10-19 2016-10-20 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
JP6076370B2 (ja) 2011-12-02 2017-02-08 シグナル ファーマシューティカルズ,エルエルシー 7−(6−(2−ヒドロキシプロパン−2−イル)ピリジン−3−イル)−1−((トランス)−4−メトキシシクロヘキシル)−3,4−ジヒドロピラジノ[2,3−b]ピラジン−2(1H)−オンの薬剤組成物、その固体形態、およびその使用方法
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
US20130183263A1 (en) 2012-01-17 2013-07-18 Steven Hoffman Pharmaceutical compositions and methods
US10272068B2 (en) 2012-01-17 2019-04-30 Tyme, Inc. 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
SMT201900024T1 (it) * 2012-01-17 2019-05-10 Tyme Inc Terapia combinata per il trattamento di cancro
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
AU2013202993B2 (en) * 2012-03-15 2015-09-03 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
AU2015213400B2 (en) * 2012-03-15 2017-07-27 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
SG11201405707XA (en) * 2012-03-15 2014-10-30 Signal Pharm 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
JP2015511964A (ja) * 2012-03-15 2015-04-23 シグナル ファーマシューティカルズ,エルエルシー Torキナーゼ阻害剤を用いた癌の治療
US20130245029A1 (en) * 2012-03-15 2013-09-19 Signal Pharmaceuticals, Llc Treatment of cancer with tor kinase inhibitors
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
NZ702747A (en) 2012-06-13 2017-03-31 Incyte Holdings Corp Substituted tricyclic compounds as fgfr inhibitors
AU2013202768B2 (en) * 2012-10-18 2015-11-05 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase 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
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
TW201441227A (zh) 2013-01-16 2014-11-01 Signal Pharm Llc 經取代吡咯并嘧啶化合物、其組合物及其治療方法
WO2014117035A1 (en) 2013-01-24 2014-07-31 Transderm, Inc. COMPOSITIONS FOR TRANSDERMAL DELIVERY OF mTOR INHIBITORS
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
KR102223060B1 (ko) * 2013-04-17 2021-03-05 시그날 파마소티칼 엘엘씨 암 치료를 위한 TOR 키나제 억제제 및 IMiD 화합물을 포함하는 조합요법
TW201526894A (zh) * 2013-04-17 2015-07-16 Signal Pharm Llc 藉二氫吡并吡治療癌症
US9359364B2 (en) * 2013-04-17 2016-06-07 Signal Pharmaceuticals, Llc Pharmaceutical formulations, processes, solid forms and methods of use relating to 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
EP2986298A1 (en) * 2013-04-17 2016-02-24 Signal Pharmaceuticals, LLC Treatment of cancer with dihydropyrazino-pyrazines
KR102240356B1 (ko) * 2013-04-17 2021-04-14 시그날 파마소티칼 엘엘씨 Tor 키나제 억제제와 5-치환된 퀴나졸리논 화합물을 포함하는 암 치료용 조합 요법
SG10201801965RA (en) * 2013-04-17 2018-04-27 Signal Pharm Llc Treatment of cancer with dihydropyrazino-pyrazines
SG11201508302PA (en) * 2013-04-17 2015-11-27 Signal Pharm Llc Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer
CA2909579A1 (en) * 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and n-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer
HK1221144A1 (zh) * 2013-04-17 2017-05-26 西格诺药品有限公司 用於治疗癌症的包含tor激酶抑制剂和胞苷类似物的组合疗法
LT2986610T (lt) 2013-04-19 2018-04-10 Incyte Holdings Corporation Bicikliniai heterociklai, kaip fgfr inhibitoriai
CN105407892B (zh) * 2013-05-29 2019-05-07 西格诺药品有限公司 一种化合物的药物组合物、其固体形式及它们的使用方法
JP2016540726A (ja) 2013-10-04 2016-12-28 シグナル ファーマシューティカルズ,エルエルシー 遺伝子突然変異を特徴とする癌の予防又は治療におけるtorキナーゼ阻害剤
US9585841B2 (en) 2013-10-22 2017-03-07 Tyme, Inc. Tyrosine derivatives and compositions comprising them
US10813901B2 (en) 2013-10-22 2020-10-27 Yamo Pharmaceuticals Llc Compositions and methods for treating autism
US10751313B2 (en) 2013-10-22 2020-08-25 Yamo Pharmaceuticals Llc Compositions and methods for treating autism
US9326962B2 (en) 2013-10-22 2016-05-03 Steven Hoffman Compositions and methods for treating intestinal hyperpermeability
US9763903B2 (en) 2013-10-22 2017-09-19 Steven Hoffman Compositions and methods for treating intestinal hyperpermeability
WO2015069217A1 (en) * 2013-11-05 2015-05-14 Baylor College Of Medicine Src kinase inhibition as treatment for lympangioleiomyomatosis and tuberous sclerosis
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
JP2017514805A (ja) * 2014-04-16 2017-06-08 シグナル ファーマシューティカルズ,エルエルシー Torキナーゼ阻害剤組み合わせ療法を使用して癌を治療する方法
EP3131552B1 (en) * 2014-04-16 2020-07-15 Signal Pharmaceuticals, LLC Methods for treating cancer using tor kinase inhibitor combination therapy
EP3131551A4 (en) 2014-04-16 2017-09-20 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, COMPOSITIONS AND METHODS OF USE THEREOF
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
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
CN106715427A (zh) 2014-07-14 2017-05-24 西格诺药品有限公司 利用取代的吡咯并嘧啶化合物、其组合物治疗癌症的方法
CN113620978A (zh) * 2014-09-11 2021-11-09 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
SG10201913036RA (en) 2015-02-20 2020-02-27 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
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
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
US10159665B2 (en) 2016-03-23 2018-12-25 Louis Habash Preventing amyloid plaque formation by treating a human subject with a nitroxide
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
US10818331B2 (en) 2016-09-27 2020-10-27 Spin Memory, Inc. Multi-chip module for MRAM devices with levels of dynamic redundancy registers
IL302385B2 (en) 2017-01-06 2024-06-01 Palvella Therapeutics Inc Non-aqueous preparations 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
SG11201912403SA (en) 2017-06-22 2020-01-30 Celgene Corp Treatment of hepatocellular carcinoma 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
MX2020004239A (es) 2017-11-01 2020-09-09 Juno Therapeutics Inc Proceso para producir una composicion de celulas t.
KR102083916B1 (ko) 2017-11-23 2020-03-03 서울대학교산학협력단 대장암 진단을 위한 tcf7 돌연변이의 용도 및 게다토리십 약물내성을 갖는 대장암 치료용 조성물
KR20200096584A (ko) * 2017-12-04 2020-08-12 바이알 - 포르텔라 앤드 씨에이 에스에이 도파민-b-하이드록실라제 억제제
US10840439B2 (en) 2017-12-29 2020-11-17 Spin Memory, Inc. Magnetic tunnel junction (MTJ) fabrication methods and systems
US10886330B2 (en) 2017-12-29 2021-01-05 Spin Memory, Inc. Memory device having overlapping magnetic tunnel junctions in compliance with a reference pitch
WO2019157516A1 (en) 2018-02-12 2019-08-15 resTORbio, Inc. Combination therapies
MX2020011565A (es) 2018-05-01 2021-01-29 Revolution Medicines Inc Analogos de rapamicina ligados a c40, c28 y c-32 como inhibidores de mtor.
IL312291A (en) 2018-05-01 2024-06-01 Revolution Medicines Inc C-26-linked rapamycin analogs as MTOR inhibitors
EP3788046B1 (en) 2018-05-04 2025-12-10 Incyte Corporation Salts of an fgfr inhibitor
EP4309737A3 (en) 2018-05-04 2024-03-27 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
LT3813946T (lt) 2018-06-15 2024-07-10 Janssen Pharmaceutica Nv Rapamicino analogai ir jų panaudojimas
JP7312170B2 (ja) 2018-06-29 2023-07-20 国立大学法人大阪大学 眼表面組織を用いる結膜疾患検出方法及び老化バイオマーカー
EP3817743A4 (en) 2018-07-02 2022-07-06 Palvella Therapeutics, Inc. ANHYDROUS COMPOSITIONS OF MTOR INHIBITORS AND METHODS OF USE
JP2021530568A (ja) 2018-07-19 2021-11-11 ヤモ・ファーマシューティカルズ・エルエルシー 自閉症を処置するための組成物および方法
US10650875B2 (en) 2018-08-21 2020-05-12 Spin Memory, Inc. System for a wide temperature range nonvolatile memory
AU2019338207B2 (en) 2018-09-10 2025-01-02 Mirati Therapeutics, Inc. Combination therapies
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
US11591329B2 (en) 2019-07-09 2023-02-28 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
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CR20220169A (es) 2019-10-14 2022-10-27 Incyte Corp Heterociclos bicíclicos como inhibidores de fgfr
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
KR20220100627A (ko) 2019-11-13 2022-07-15 니뽄 신야쿠 가부시키가이샤 아자벤즈이미다졸 화합물 및 의약
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN115209897A (zh) 2019-12-05 2022-10-18 安纳库利亚治疗公司 雷帕霉素类似物及其用途
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021219091A2 (zh) * 2020-04-29 2021-11-04 北京泰德制药股份有限公司 喹喔啉酮衍生物作为kras g12c突变蛋白的不可逆抑制剂
CA3186565A1 (en) * 2020-07-22 2022-01-27 Lei Miao Unit dosage composition of akt inhibitor
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
AU2022224567A1 (en) 2021-02-16 2023-08-24 Barinthus Biotherapeutics North America, Inc. Self-assembling nanoparticles based on amphiphilic peptides
US12065494B2 (en) 2021-04-12 2024-08-20 Incyte Corporation Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
US20240226126A1 (en) * 2021-06-16 2024-07-11 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
JP2025522296A (ja) 2022-05-25 2025-07-15 レヴォリューション・メディスンズ,インコーポレイテッド mTOR阻害剤によりがんを処置する方法
US20240269269A1 (en) 2022-10-25 2024-08-15 Vaccitech North America, Inc. Self-Assembling Nanoparticles
US20250250542A1 (en) 2023-02-07 2025-08-07 Quell Therapeutics Limited Culture method
WO2025198867A1 (en) * 2024-03-18 2025-09-25 Convatec, Inc Brachytherapy composition and related methods

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE262026C (es)
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
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
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
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 (es) 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
US5770589A (en) 1993-07-27 1998-06-23 The University Of Sydney Treatment of macular degeneration
RU2191188C2 (ru) * 1994-11-14 2002-10-20 Варнер-Ламберт Компани Производные 6-арилпиридо[2,3-d]-пиримидины и -нафтиридины, фармацевтическая композиция, обладающая ингибирующим действием клеточной пролиферации, вызываемой протеиновой тирозинкиназой, и способ ингибирования клеточной пролиферации
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
IL158649A0 (en) 1997-09-26 2004-05-12 Zentaris Gmbh 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
AU3042601A (en) * 2000-01-24 2001-07-31 Thrombogenix Pty Ltd Therapeutic morpholino-substituted compounds
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
DE60115092T2 (de) 2000-12-12 2006-03-30 Neurogen Corp., Brandford Spiro[isobenzofuran-1,4'-piperidin]-3-one und 3h-spiroisobenzofuran-1,4'-piperidine
US8127015B2 (en) 2001-04-24 2012-02-28 Broadcom Corporation Alerting system, architecture and circuitry
HRP20040213A2 (en) 2001-09-04 2005-02-28 Boehringer Ingelheim Pharma Gmbh & Co.Kg Novel dihydropteridinones, method for producing the same and the use thereof as medicaments
WO2003032989A1 (en) 2001-10-18 2003-04-24 Boehringer Ingelheim Pharmaceuticals, Inc. 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
WO2004042002A2 (en) 2002-08-05 2004-05-21 University Of Massachusetts 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
ATE433967T1 (de) 2003-01-17 2009-07-15 Warner Lambert Co 2-aminopyridin-substituierteheterocyclen als inhibitoren der zellulären proliferation
HRP20050735B1 (hr) 2003-02-26 2013-08-31 Boehringer Ingelheim Pharma Gmbh & Co.Kg Dihidropteridinoni, metoda za njihovu proizvodnju i upotrebu u obliku lijekova
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
US20050130954A1 (en) * 2003-11-21 2005-06-16 Mitchell Ian S. AKT protein kinase inhibitors
AU2005226649B2 (en) 2004-03-22 2010-04-29 Celgene Corporation Methods of using and compositions comprising immunomodulatory compounds for the treatment and management of skin diseases or disorders
NZ550222A (en) * 2004-04-08 2010-09-30 Topotarget As Diphenyl ox-indol-2-one compounds and their use in the treatment of cancer
EP1755600A2 (en) 2004-04-23 2007-02-28 Celgene Corporation Methods of using and compositions comprising immunomodulatory compounds for the treatment and management of pulmonary hypertension
CN101123968A (zh) 2004-06-04 2008-02-13 艾科斯有限公司 肥大细胞病的治疗方法
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
AU2005289644A1 (en) 2004-09-24 2006-04-06 Janssen Pharmaceutica, N.V. Imidazo{4,5-b}pyrazinone inhibitors of protein kinases
CA2577588C (en) 2004-10-29 2013-09-10 Tibotec Pharmaceuticals Ltd. Hiv inhibiting bicyclic pyrimidine derivatives
MX2007005570A (es) 2004-11-12 2007-07-09 Celgene Corp Metodos y composiciones que usan compuestos inmunomoduladores para el tratamiento y manejo de padecimientos parasiticos.
BRPI0518282A2 (pt) 2004-11-23 2008-11-11 Celgene Corp uso de uma quantidade terapeuticamente ou profilaticamente efetiva de um composto imunomodulatàrio
WO2006060507A2 (en) 2004-12-01 2006-06-08 Celgene Corporation Compositions comprising immunomodulatory compounds and the use thereof for the treatment of immunodeficiency disorders
CA2590294A1 (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
AU2006217744A1 (en) * 2005-02-25 2006-08-31 Kudos Pharmaceuticals Limited 2,4-diamino-pyridopyrimidine derivatives and their use as MTOR inhibitors
NZ562468A (en) 2005-04-05 2009-10-30 Pharmacopeia Inc Purine and imidazopyridine derivatives for immunosuppression
RS51843B (sr) * 2005-11-17 2012-02-29 Osi Pharmaceuticals Llc. KONDENZOVANI BICIKLIČNI m TOR INHIBITORI
AU2007281468B2 (en) 2006-08-02 2012-12-06 Cytokinetics, Incorporated Certain chemical entities, compositions and methods
KR101504669B1 (ko) 2006-10-19 2015-03-20 시그날 파마소티칼 엘엘씨 헤테로아릴 화합물, 이들의 조성물 그리고 단백질 키나아제 억제제로서의 이들의 용도
EP2132177B1 (en) 2007-03-01 2013-07-17 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
CN102686225A (zh) * 2009-10-26 2012-09-19 西格诺药品有限公司 杂芳基化合物的合成和纯化方法

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