[go: up one dir, main page]

RU2014117666A - Лечение рака поджелудочной железы и немелкоклеточного рака легкого ингибиторами атr - Google Patents

Лечение рака поджелудочной железы и немелкоклеточного рака легкого ингибиторами атr Download PDF

Info

Publication number
RU2014117666A
RU2014117666A RU2014117666/15A RU2014117666A RU2014117666A RU 2014117666 A RU2014117666 A RU 2014117666A RU 2014117666/15 A RU2014117666/15 A RU 2014117666/15A RU 2014117666 A RU2014117666 A RU 2014117666A RU 2014117666 A RU2014117666 A RU 2014117666A
Authority
RU
Russia
Prior art keywords
therapy
patient
pancreatic cancer
administering
combination
Prior art date
Application number
RU2014117666/15A
Other languages
English (en)
Other versions
RU2648507C2 (ru
Inventor
Джон Роберт ПОЛЛАРД
Филип Майкл РИПЕР
Original Assignee
Вертекс Фармасьютикалз Инкорпорейтед
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
Application filed by Вертекс Фармасьютикалз Инкорпорейтед filed Critical Вертекс Фармасьютикалз Инкорпорейтед
Publication of RU2014117666A publication Critical patent/RU2014117666A/ru
Application granted granted Critical
Publication of RU2648507C2 publication Critical patent/RU2648507C2/ru

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/4965Non-condensed pyrazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/555Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • A61K33/24Heavy metals; Compounds thereof
    • A61K33/243Platinum; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00Preparations for use in therapy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61NELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00Radiation therapy
    • A61N5/10X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
    • A61N2005/1092Details
    • A61N2005/1098Enhancing the effect of the particle by an injected agent or implanted device

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Radiation-Therapy Devices (AREA)

Abstract

1. Способ лечения рака поджелудочной железы у пациента посредством введения пациенту ингибитора ATR, выбранного изв сочетании с другим видом противоопухолевой терапии, выбранным из терапии гемцитабином, лучевой терапии или обеих терапий гемцитабином и лучевой терапии вместе.2. Способ повышения чувствительности клеток рака поджелудочной железы к противоопухолевой терапии, выбранной из терапии гемцитабином или лучевой терапии у пациента посредством введения пациенту ингибитора ATR, выбранного изв сочетании с противоопухолевой терапией.3. Способ по п. 1, в котором противоопухолевая терапия представляет собой терапию гемцитабином.4. Способ по п. 1, в котором противоопухолевая терапия представляет собой лучевую терапию.5. Способ повышения чувствительности гипоксических клеток рака поджелудочной железы к противоопухолевой терапии, выбранной из терапии гемцитабином или лучевой терапии у пациента посредством введения пациенту ингибитора ATR, выбранного изв сочетании с противоопухолевой терапией.6. Способ ингибирования фосфорилирования Chkl (Ser 345) в клетках рака поджелудочной железы, содержащий введение пациенту ингибитора ATR, выбранного изв сочетании с гемцитабином и/или облучением.7. Способ радиосенсибилизации гипоксических клеток рака поджелудочной железы посредством введения пациенту ингибитора ATR, выбранного изв сочетании с лучевой терапией.8. Способ повышения чувствительности гипоксических клеток рака поджелудочной железы посредством введения пациенту ингибитора ATR, выбранного изв сочетании с гемцитабином.9. Способ повышения чувствительности клеток рака поджелудочной железы к химиолучевой терапии поср�

Claims (22)

1. Способ лечения рака поджелудочной железы у пациента посредством введения пациенту ингибитора ATR, выбранного из
Figure 00000001
в сочетании с другим видом противоопухолевой терапии, выбранным из терапии гемцитабином, лучевой терапии или обеих терапий гемцитабином и лучевой терапии вместе.
2. Способ повышения чувствительности клеток рака поджелудочной железы к противоопухолевой терапии, выбранной из терапии гемцитабином или лучевой терапии у пациента посредством введения пациенту ингибитора ATR, выбранного из
Figure 00000002
в сочетании с противоопухолевой терапией.
3. Способ по п. 1, в котором противоопухолевая терапия представляет собой терапию гемцитабином.
4. Способ по п. 1, в котором противоопухолевая терапия представляет собой лучевую терапию.
5. Способ повышения чувствительности гипоксических клеток рака поджелудочной железы к противоопухолевой терапии, выбранной из терапии гемцитабином или лучевой терапии у пациента посредством введения пациенту ингибитора ATR, выбранного из
Figure 00000003
в сочетании с противоопухолевой терапией.
6. Способ ингибирования фосфорилирования Chkl (Ser 345) в клетках рака поджелудочной железы, содержащий введение пациенту ингибитора ATR, выбранного из
Figure 00000004
в сочетании с гемцитабином и/или облучением.
7. Способ радиосенсибилизации гипоксических клеток рака поджелудочной железы посредством введения пациенту ингибитора ATR, выбранного из
Figure 00000005
в сочетании с лучевой терапией.
8. Способ повышения чувствительности гипоксических клеток рака поджелудочной железы посредством введения пациенту ингибитора ATR, выбранного из
Figure 00000006
в сочетании с гемцитабином.
9. Способ повышения чувствительности клеток рака поджелудочной железы к химиолучевой терапии посредством введения пациенту ингибитора ATR, выбранного из
Figure 00000007
в сочетании с химиолучевой терапией.
10. Способ по п. 9, в котором химиотерапия представляет собой терапию гемцитабином.
11. Способ прерывания клеточного цикла, обусловленного повреждением, в сверочных точках посредством введения пациенту ингибитора ATR, выбранного из
Figure 00000008
в сочетании с лучевой терапией.
12. Способ ингибирования репарации поврежденной ДНК посредством гомологической рекомбинации в клетке рака поджелудочной железы посредством введения ингибитора ATR, выбранного из
Figure 00000009
в сочетании с лучевой терапией.
13. Способ по любому и пп. 1-12, в котором клетки рака поджелудочной железы получены из клеточной линии поджелудочной железы, выбранной из PSN-1, MiaPaCa-2 или Panc-1.
14. Способ по любому из пп. 1-12, в котором клетки рака поджелудочной железы находятся в организме онкологического пациента.
15. Способ по любому из пп. 1-12, в котором соединение вводится в организм пациента.
16. Способ по любому из пп. 1-12, в котором соединение вводится в клетки рака поджелудочной железы.
17. Способ лечения немелкоклеточного рака легкого у пациента, содержащий введение пациенту соединения с формулой 821 или 822:
Figure 00000010
в сочетании с одним или более из следующих дополнительных лекарственных агентов: цисплатин или карбоплатин, этопозид и ионизирующее излучение.
18. Способ по п. 17, содержащий введение пациенту соединения с формулой 821 или 822 в сочетании с противоопухолевой терапией, выбранной из группы, состоящей из цисплатина или карбоплатина, этопозида и ионизирующего излучения.
19. Способ по п. 18, в котором противоопухолевая терапия представляет собой терапию цисплатином или карбоплатином и этопозидом.
20. Способ по п. 18, в котором противоопухолевая терапия представляет собой терапию цисплатином или карбоплатином и этопозидом и ионизирующим излучением.
21. Способ по п. 18, в котором противоопухолевая терапия представляет собой ионизирующее излучение.
22. Способ в соответствии с одним из пп. 1-21, в котором ингибитор ATR представляет собой 822.
RU2014117666A 2011-09-30 2012-10-01 Лечение рака поджелудочной железы и немелкоклеточного рака легкого ингибиторами atr RU2648507C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161542084P 2011-09-30 2011-09-30
US61/542,084 2011-09-30
PCT/US2012/058374 WO2013049859A1 (en) 2011-09-30 2012-10-01 Treating pancreatic cancer and non-small cell lung cancer with atr inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
RU2018108589A Division RU2018108589A (ru) 2011-09-30 2012-10-01 Лечение рака поджелудочной железы и немелкоклеточного рака легкого ингибиторами atr

Publications (2)

Publication Number Publication Date
RU2014117666A true RU2014117666A (ru) 2015-11-10
RU2648507C2 RU2648507C2 (ru) 2018-03-26

Family

ID=47019166

Family Applications (2)

Application Number Title Priority Date Filing Date
RU2018108589A RU2018108589A (ru) 2011-09-30 2012-10-01 Лечение рака поджелудочной железы и немелкоклеточного рака легкого ингибиторами atr
RU2014117666A RU2648507C2 (ru) 2011-09-30 2012-10-01 Лечение рака поджелудочной железы и немелкоклеточного рака легкого ингибиторами atr

Family Applications Before (1)

Application Number Title Priority Date Filing Date
RU2018108589A RU2018108589A (ru) 2011-09-30 2012-10-01 Лечение рака поджелудочной железы и немелкоклеточного рака легкого ингибиторами atr

Country Status (16)

Country Link
US (3) US20130089626A1 (ru)
EP (2) EP3733185B1 (ru)
JP (4) JP6162126B2 (ru)
KR (1) KR102056586B1 (ru)
CN (3) CN108685922A (ru)
AU (3) AU2012315384B2 (ru)
BR (1) BR112014007690B1 (ru)
CA (2) CA2850491C (ru)
ES (2) ES2899880T3 (ru)
IL (1) IL231813B (ru)
IN (1) IN2014CN02501A (ru)
MX (2) MX373340B (ru)
RU (2) RU2018108589A (ru)
SG (2) SG11201401095YA (ru)
WO (1) WO2013049859A1 (ru)
ZA (1) ZA201402627B (ru)

Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2009327357C1 (en) 2008-12-19 2017-02-02 Vertex Pharmaceuticals Incorporated Pyrazine derivatives useful as inhibitors of ATR kinase
WO2011143399A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
MX2012013081A (es) 2010-05-12 2013-05-09 Vertex Pharma Compuestos utiles como inhibidores de cinasa atr.
US8962631B2 (en) 2010-05-12 2015-02-24 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
JP2013526540A (ja) 2010-05-12 2013-06-24 バーテックス ファーマシューティカルズ インコーポレイテッド Atrキナーゼ阻害剤として有用な化合物
WO2011143422A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated 2 -aminopyridine derivatives useful as inhibitors of atr kinase
WO2011143423A2 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8623869B2 (en) 2010-06-23 2014-01-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
MX2013011450A (es) 2011-04-05 2014-02-03 Vertex Pharma Compuestos de aminopirazina utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr).
WO2012178123A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US9096602B2 (en) 2011-06-22 2015-08-04 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-B]pyrazines as ATR kinase inhibitors
JP2014517079A (ja) 2011-06-22 2014-07-17 バーテックス ファーマシューティカルズ インコーポレイテッド Atrキナーゼ阻害剤として有用な化合物
EP2751088B1 (en) 2011-09-30 2016-04-13 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2751099B1 (en) 2011-09-30 2017-06-14 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
SG11201401095YA (en) 2011-09-30 2014-04-28 Vertex Pharma Treating pancreatic cancer and non-small cell lung cancer with atr inhibitors
RS59337B1 (sr) 2011-09-30 2019-10-31 Vertex Pharma Postupak za izradu jedinjenja, korisnih kao inhibitori atr kinaze
WO2013049720A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8841450B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
US8846917B2 (en) 2011-11-09 2014-09-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2776429A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2013071090A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2776419B1 (en) 2011-11-09 2016-05-11 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
ES2654670T3 (es) 2012-04-05 2018-02-14 Vertex Pharmaceuticals Incorporated Compuestos útiles como inhibidores de la cinasa ATR y terapias de combinación de los mismos
WO2014055756A1 (en) 2012-10-04 2014-04-10 Vertex Pharmaceuticals Incorporated Method for measuring atr inhibition mediated increases in dna damage
EP2909202A1 (en) 2012-10-16 2015-08-26 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
PT4190786T (pt) 2012-12-07 2025-05-29 Vertex Pharma Compostos úteis como inibidores da quinase atr
EP2970286A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
WO2015057461A2 (en) 2013-10-18 2015-04-23 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Antibodies that specifically bind ataxia telangiectasia-mutated and rad3-related kinase phosphorylated at position 1989 and their use
CA2932757C (en) 2013-12-06 2023-10-31 Vertex Pharmaceuticals Incorporated 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof
KR102575125B1 (ko) 2014-06-05 2023-09-07 버텍스 파마슈티칼스 인코포레이티드 Atr 키나제의 저해제로서 유용한 2-아미노-6-플루오로-n-[5-플루오로-피리딘-3-일]-피라졸로[1,5-a]피리미딘-3-카복스아미드 화합물의 방사성표지된 유도체, 상기 화합물의 제조 및 이의 다양한 고체 형태
RU2736219C2 (ru) * 2014-06-17 2020-11-12 Вертекс Фармасьютикалз Инкорпорейтед Способ лечения рака с использованием комбинации ингибиторов снк1 и atr
TWI700283B (zh) 2014-08-04 2020-08-01 德商拜耳製藥公司 2-(嗎啉-4-基)-1,7-萘啶
US20190000850A1 (en) * 2015-02-09 2019-01-03 The Regents Of The University Of California Combination cancer therapy
AU2016331955B2 (en) * 2015-09-30 2022-07-21 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors
CN108697811B (zh) * 2016-01-11 2023-04-07 梅里麦克制药股份有限公司 抑制共济失调毛细血管扩张和Rad3相关蛋白(ATR)
US11730734B2 (en) 2016-09-12 2023-08-22 University Of Florida Research Foundation, Incorporated Use of ATR and Chk1 inhibitor compounds
EA039513B1 (ru) * 2017-01-09 2022-02-04 Селатор Фармасьютикалз, Инк. Ингибитор атаксии-телеангиэкстазии и rad3-родственного белка (atr) и содержащие его липосомные композиции
WO2018153971A1 (en) * 2017-02-24 2018-08-30 Bayer Pharma Aktiengesellschaft Combination of atr kinase inhibitors
JOP20190197A1 (ar) 2017-02-24 2019-08-22 Bayer Pharma AG مثبط كيناز ايه تي آر للاستخدام في طريقة لعلاج مرض فرط التكاثر
WO2018153972A1 (en) 2017-02-24 2018-08-30 Bayer Pharma Aktiengesellschaft Combination of atr kinase inhibitors and antiandrogens
AR110995A1 (es) 2017-02-24 2019-05-22 Bayer Ag Combinación de inhibidores de quinasa atr con sal de radio-223
WO2018206547A1 (en) 2017-05-12 2018-11-15 Bayer Pharma Aktiengesellschaft Combination of bub1 and atr inhibitors
WO2019025440A1 (en) 2017-08-04 2019-02-07 Bayer Pharma Aktiengesellschaft COMBINATION OF ATR KINASE INHIBITORS AND PD-1 / PD-L1 INHIBITORS
EP3461480A1 (en) 2017-09-27 2019-04-03 Onxeo Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer
CA3084863A1 (en) 2017-12-08 2019-06-13 Bayer Aktiengesellschaft Predictive markers for atr kinase inhibitors
US20210196751A1 (en) * 2017-12-29 2021-07-01 Vertex Pharmaceuticals Incorporated Methods of cancer treatment using an atr inhibitor
WO2020055187A1 (ko) * 2018-09-12 2020-03-19 기초과학연구원 유전자가 변이된 세포의 사멸 유도 조성물 및 상기 조성물을 이용한 유전자가 변형된 세포 사멸 유도 방법
JP2022502399A (ja) 2018-09-26 2022-01-11 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung がんの治療のためのpd−1アンタゴニスト、atrインヒビター、および白金製剤の組合せ
EP3866785A1 (en) 2018-10-15 2021-08-25 Merck Patent GmbH Combination therapy utilizing dna alkylating agents and atr inhibitors
US20210369724A1 (en) 2018-10-16 2021-12-02 Bayer Aktiengesellschaft Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds
US11801246B2 (en) 2018-11-09 2023-10-31 East Tennessee State University Research Foundatio Methods of treating ischemic disease by administering an ATR kinase inhibitor
US20220274929A1 (en) * 2019-02-25 2022-09-01 The Regents Of The University Of California Thiosemicarbazone compounds and uses thereof
AU2021368138A1 (en) 2020-11-02 2023-06-22 Trethera Corporation Crystalline forms of a deoxycytidine kinase inhibitor and uses thereof
CN113073139A (zh) * 2021-04-06 2021-07-06 浙江大学 一种胰腺癌肿瘤标志物及其应用
JP2024526791A (ja) * 2021-07-16 2024-07-19 セレーター ファーマシューティカルズ インコーポレイテッド リポソーム製剤の調製方法
CN115300512B (zh) * 2022-08-05 2024-01-12 华中科技大学同济医学院附属协和医院 Atr抑制剂ve-822在治疗肺腺癌中的应用
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ras相關疾病或病症之組合療法
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. Ras inhibitors
KR20250074713A (ko) 2023-11-15 2025-05-28 주식회사 레이메드 방사성 테크네튬-99엠 표지 금속나노입자를 포함하는 췌장암 치료용 조성물
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025217307A1 (en) 2024-04-09 2025-10-16 Revolution Medicines, Inc. Methods for predicting response to a ras(on) inhibitor and combination therapies
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors

Family Cites Families (218)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4309430A (en) 1980-06-27 1982-01-05 Merck & Co., Inc. Pyrazinyl-1,2,4-oxadiazole-5-ones, for treatment of edema, and processes for preparing same
JPS62270623A (ja) 1985-12-07 1987-11-25 Daicel Chem Ind Ltd ビス(4−アミノフエニル)ピラジンおよびその製法、ならびにポリイミドおよびその製法
JPS63208520A (ja) 1987-02-26 1988-08-30 Terumo Corp ピラジン誘導体を含有する血小板凝集抑制剤
US5329012A (en) 1987-10-29 1994-07-12 The Research Foundation Of State University Of New York Bis(acyloxmethyl)imidazole compounds
JP2597917B2 (ja) 1990-04-26 1997-04-09 富士写真フイルム株式会社 新規な色素形成カプラー及びそれを用いたハロゲン化銀カラー写真感光材料
US5572248A (en) 1994-09-19 1996-11-05 Teleport Corporation Teleconferencing method and system for providing face-to-face, non-animated teleconference environment
CA2253910A1 (en) 1996-05-11 1997-11-20 King's College London Pyrazines
JP2002241379A (ja) 1997-03-21 2002-08-28 Dainippon Pharmaceut Co Ltd 3−オキサジアゾリルキノキサリン誘導体
WO1999044609A1 (en) 1998-03-03 1999-09-10 Merck & Co., Inc. FUSED PIPERIDINE SUBSTITUTED ARYLSULFONAMIDES AS β3-AGONISTS
DE19826671A1 (de) 1998-06-16 1999-12-23 Hoechst Schering Agrevo Gmbh 1,3-Oxazolin- und 1,3-Thiazolin-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Schädlingsbekämpfungsmittel
JP3910365B2 (ja) 1998-07-16 2007-04-25 塩野義製薬株式会社 抗腫瘍活性を有するピリミジン誘導体
US7023913B1 (en) 2000-06-14 2006-04-04 Monroe David A Digital security multimedia sensor
PT1150999E (pt) 1999-02-05 2006-10-31 Debiopharm Sa Derivados da ciclosporina em que a sequencia peptidica contem pelo menos um aminoacido nao natural do tipo pseudo-prolina e metodo para preparacao dos mesmos
US6738073B2 (en) 1999-05-12 2004-05-18 Imove, Inc. Camera system with both a wide angle view and a high resolution view
CA2412345A1 (en) 1999-06-16 2000-12-21 University Of Iowa Research Foundation Antagonism of immunostimulatory cpg-oligonucleotides by 4-aminoquinolines and other weak bases
US7015954B1 (en) 1999-08-09 2006-03-21 Fuji Xerox Co., Ltd. Automatic video system using multiple cameras
US6660753B2 (en) 1999-08-19 2003-12-09 Nps Pharmaceuticals, Inc. Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
ATE384704T1 (de) 1999-12-17 2008-02-15 Novartis Vaccines & Diagnostic Pyrazin-basierte hemmer der glycogen-synthase- kinase 3
US6849660B1 (en) 2000-08-01 2005-02-01 Isis Pharmaceuticals, Inc. Antimicrobial biaryl compounds
JP2002072370A (ja) 2000-08-29 2002-03-12 Fuji Photo Optical Co Ltd ペーパーマガジン及び写真焼付装置
JP2002072372A (ja) 2000-09-04 2002-03-12 Fuji Photo Film Co Ltd 画像形成用シート体の切断装置
US6829391B2 (en) 2000-09-08 2004-12-07 Siemens Corporate Research, Inc. Adaptive resolution system and method for providing efficient low bit rate transmission of image data for distributed applications
EP1217000A1 (en) 2000-12-23 2002-06-26 Aventis Pharma Deutschland GmbH Inhibitors of factor Xa and factor VIIa
US8085293B2 (en) 2001-03-14 2011-12-27 Koninklijke Philips Electronics N.V. Self adjusting stereo camera system
US6759657B2 (en) 2001-03-27 2004-07-06 Kabushiki Kaisha Toshiba Infrared sensor
JPWO2002080899A1 (ja) 2001-03-30 2005-01-06 エーザイ株式会社 消化器疾患治療剤
US6469002B1 (en) 2001-04-19 2002-10-22 Millennium Pharmaceuticals, Inc. Imidazolidine compounds
EP1408986B1 (en) 2001-05-08 2008-09-24 Yale University Proteomimetic compounds and methods
SE0102439D0 (sv) 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
SE0102438D0 (sv) 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
JP2003074370A (ja) 2001-09-05 2003-03-12 Suzuki Motor Corp エンジンのベルト保護装置
CA2457642C (en) 2001-09-26 2009-01-06 Merck & Co., Inc. Crystalline forms of ertapenem sodium
GB0124939D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
US6992087B2 (en) 2001-11-21 2006-01-31 Pfizer Inc Substituted aryl 1,4-pyrazine derivatives
ATE447561T1 (de) 2001-11-21 2009-11-15 Pharmacia & Upjohn Co Llc Substituierte aryl 1,4-pyrazin derivate
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
JP4656838B2 (ja) 2002-02-06 2011-03-23 バーテックス ファーマシューティカルズ インコーポレイテッド Gsk−3の阻害剤として有用なヘテロアリール化合物
EA006707B1 (ru) 2002-03-13 2006-02-24 Янссен Фармацевтика Н. В. Сульфонилпроизводные в качестве новых ингибиторов гистон-деацетилазы
GB0206860D0 (en) 2002-03-22 2002-05-01 Glaxo Group Ltd Compounds
TWI319387B (en) 2002-04-05 2010-01-11 Astrazeneca Ab Benzamide derivatives
US7043079B2 (en) 2002-04-25 2006-05-09 Microsoft Corporation “Don't care” pixel interpolation
GB0209715D0 (en) 2002-04-27 2002-06-05 Astrazeneca Ab Chemical compounds
JP4901102B2 (ja) 2002-05-03 2012-03-21 エクセリクシス, インク. プロテインキナーゼモジュレーターおよびその使用方法
US7704995B2 (en) 2002-05-03 2010-04-27 Exelixis, Inc. Protein kinase modulators and methods of use
TW200406385A (en) 2002-05-31 2004-05-01 Eisai Co Ltd Pyrazole compound and pharmaceutical composition containing the same
US20040082627A1 (en) 2002-06-21 2004-04-29 Darrow James W. Certain aromatic monocycles as kinase modulators
US7015227B2 (en) 2002-06-21 2006-03-21 Cgi Pharmaceuticals, Inc. Certain amino-substituted monocycles as kinase modulators
WO2004033431A2 (en) 2002-10-04 2004-04-22 Arena Pharmaceuticals, Inc. Hydroxypyrazoles for use against metabolic-related disorders
US20040075741A1 (en) 2002-10-17 2004-04-22 Berkey Thomas F. Multiple camera image multiplexer
US7385626B2 (en) 2002-10-21 2008-06-10 Sarnoff Corporation Method and system for performing surveillance
US20040100560A1 (en) 2002-11-22 2004-05-27 Stavely Donald J. Tracking digital zoom in a digital video camera
SE0203752D0 (sv) 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
SE0203754D0 (sv) 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
DK1603570T5 (da) 2003-02-26 2013-12-09 Sugen Inc Aminoheteroarylforbindelser som proteinkinaseinhibitorer
US7684624B2 (en) 2003-03-03 2010-03-23 Smart Technologies Ulc System and method for capturing images of a target area on which information is recorded
MXPA05009245A (es) 2003-03-11 2005-10-19 Pfizer Prod Inc Nuevos compuestos de pirazina como inhibidores del factor de crecimiento transformante (tgf).
WO2004084813A2 (en) 2003-03-21 2004-10-07 Smithkline Beecham Corporation Chemical compounds
CN1791580A (zh) 2003-03-24 2006-06-21 麦克公司 联芳基取代的6元杂环钠通道阻滞剂
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
GB2400514B (en) 2003-04-11 2006-07-26 Hewlett Packard Development Co Image capture method
WO2004103279A2 (en) 2003-05-15 2004-12-02 Merck & Co., Inc. 3-(2-amino-1-azacyclyl)-5-aryl-1,2,4-oxadiazoles as s1p receptor agonists
WO2004103991A1 (en) 2003-05-20 2004-12-02 'chemical Diversity Research Institute', Ltd. 2-substituted piperidines, focused library and a pharmaceutical compound
US20050123902A1 (en) 2003-05-21 2005-06-09 President And Fellows Of Harvard College Human papillomavirus inhibitors
PE20050206A1 (es) * 2003-05-26 2005-03-26 Schering Ag Composicion farmaceutica que contiene un inhibidor de histona deacetilasa
US7986339B2 (en) 2003-06-12 2011-07-26 Redflex Traffic Systems Pty Ltd Automated traffic violation monitoring and reporting system with combined video and still-image data
JP2005020227A (ja) 2003-06-25 2005-01-20 Pfu Ltd 画像圧縮装置
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
US7807696B2 (en) 2003-10-07 2010-10-05 The Feinstein Institute For Medical Research Isoxazole and isothiazole compounds useful in the treatment of inflammation
US20050116968A1 (en) 2003-12-02 2005-06-02 John Barrus Multi-capability display
WO2005058876A1 (en) 2003-12-16 2005-06-30 Gpc Biotech Ag Pyrazine derivatives as effective compounds against infectious diseases
CN1933838A (zh) 2004-02-12 2007-03-21 默克公司 作为代谢型谷氨酸受体-5调节剂的联吡啶酰胺
US20050276765A1 (en) 2004-06-10 2005-12-15 Paul Nghiem Preventing skin damage
US20080153869A1 (en) 2004-06-14 2008-06-26 Bressi Jerome C Kinase Inhibitors
EP1778687A2 (en) 2004-07-27 2007-05-02 SGX Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
US7626021B2 (en) 2004-07-27 2009-12-01 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
JP4242911B2 (ja) 2004-08-26 2009-03-25 ファイザー・インク プロテインキナーゼ阻害薬としてのエナンチオピュアなアミノヘテロアリール化合物
MX2007001986A (es) 2004-08-26 2007-05-10 Pfizer Compuestos de aminoheteroarilo como inhibidores de proteina quinasa.
US7730406B2 (en) 2004-10-20 2010-06-01 Hewlett-Packard Development Company, L.P. Image processing system and method
JP5008569B2 (ja) 2004-10-22 2012-08-22 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ C−fmsキナーゼのインヒビターとしての芳香族アミド
WO2006053342A2 (en) 2004-11-12 2006-05-18 Osi Pharmaceuticals, Inc. Integrin antagonists useful as anticancer agents
NZ555566A (en) 2004-11-22 2009-12-24 Vertex Pharma Pyrrolopyrazines and pyrazolopyrazines useful as inhibitors of protein kinases
JP4810669B2 (ja) 2004-11-25 2011-11-09 コニカミノルタホールディングス株式会社 有機エレクトロルミネッセンス素子、表示装置及び照明装置
GB0428235D0 (en) 2004-12-23 2005-01-26 Glaxo Group Ltd Novel compounds
KR100994173B1 (ko) 2004-12-27 2010-11-15 알콘, 인코퍼레이티드 녹내장 및 다른 로 키나아제-매개 질환 치료용아미노피라진 유사체
GB0500492D0 (en) 2005-01-11 2005-02-16 Cyclacel Ltd Compound
US7622583B2 (en) 2005-01-14 2009-11-24 Chemocentryx, Inc. Heteroaryl sulfonamides and CCR2
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
JP4873352B2 (ja) 2005-02-16 2012-02-08 シェーリング コーポレイション Cxcr3アンタゴニスト活性を有する、複素環で置換されたピペラジン
CA2605738C (en) 2005-04-25 2013-10-01 Merck Patent Gesellschaft Mit Beschraenkter Haftung Novel azaheterocyclic compounds as kinase inhibitors
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
US20090233896A1 (en) 2005-06-09 2009-09-17 Arrington Kenneth L Inhibitors of checkpoint kinases
EP1919895A2 (en) 2005-08-02 2008-05-14 Lexicon Pharmaceuticals, Inc. 2-aminoaryl pyridines as protein kinases inhibitors
WO2007015632A1 (en) 2005-08-04 2007-02-08 Cgk Co., Ltd. Atm and atr inhibitor
US7394926B2 (en) 2005-09-30 2008-07-01 Mitutoyo Corporation Magnified machine vision user interface
US7806604B2 (en) 2005-10-20 2010-10-05 Honeywell International Inc. Face detection and tracking in a wide field of view
AR056786A1 (es) 2005-11-10 2007-10-24 Smithkline Beecham Corp Compuesto de 1h- imidazo ( 4,5-c) piridin-2-ilo, composicion farmaceutica que lo comprende, procedimiento para preparar dicha composicion, su uso para preparar unmedicamento, uso de una combinacion que omprende al compuesto y al menos un agente antineoplasico para preparar un medicamento y dicha com
PL1959951T3 (pl) 2005-12-01 2010-06-30 Hoffmann La Roche Heteroarylo-podstawione pochodne piperydyny jako inhibitory l-cpt1
JP5064237B2 (ja) 2005-12-09 2012-10-31 Meiji Seikaファルマ株式会社 リンコマイシン誘導体およびこれを有効成分とする抗菌剤
US20090143410A1 (en) 2005-12-14 2009-06-04 Kanu Maganbhai Patel Isoxazolines for Controlling Invertebrate Pests
EP1962853A1 (en) 2005-12-22 2008-09-03 Alcon Research, Ltd. (indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)- pyrazines for treating rho kinase-mediated diseases and conditions
PE20070978A1 (es) 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
ITMI20060311A1 (it) 2006-02-21 2007-08-22 Btsr Int Spa Dispositivo perfezionato di alimentazione di filo o filatio ad una macchina tessile e metodo per attuare tale alimentazione
GB0603684D0 (en) 2006-02-23 2006-04-05 Novartis Ag Organic compounds
WO2007096764A2 (en) 2006-02-27 2007-08-30 Glenmark Pharmaceuticals S.A. Bicyclic heteroaryl derivatives as cannabinoid receptor modulators
TW200800203A (en) 2006-03-08 2008-01-01 Astrazeneca Ab New use
WO2007111904A2 (en) 2006-03-22 2007-10-04 Vertex Pharmaceuticals Incorporated C-met protein kinase inhibitors for the treatment of proliferative disorders
US7574131B2 (en) 2006-03-29 2009-08-11 Sunvision Scientific Inc. Object detection system and method
AR060336A1 (es) 2006-03-31 2008-06-11 Schering Corp Derivados de indazolilpirazinilo inhibidores de proteinquinasas, composiciones farmaceuticas que los contienen y usos como agentes anticancer,entre otros.
US7629346B2 (en) 2006-06-19 2009-12-08 Hoffmann-La Roche Inc. Pyrazinecarboxamide derivatives as CB1 antagonists
DE602007004618D1 (de) 2006-06-22 2010-03-18 Biovitrum Ab Publ Pyridin- und pyrazinderivate als mnk-kinaseinhibitoren
CA2655857C (en) 2006-06-22 2014-12-02 Mallinckrodt Inc. Pyrazine derivatives with extended conjugation and uses thereof
EP1900727A1 (en) 2006-08-30 2008-03-19 Cellzome Ag Aminopyridine derivatives as kinase inhibitors
BRPI0717564A2 (pt) 2006-09-29 2013-10-22 Novartis Ag Pirazolopirimidinas como inibidores de pi3k lipídeo cinase
GB0619342D0 (en) 2006-09-30 2006-11-08 Vernalis R&D Ltd New chemical compounds
BRPI0717845A2 (pt) 2006-10-04 2015-06-16 Hoffmann La Roche Uso de compostos, composições farmacêuticas e métodos para o tratamento e/ou profilaxia de enfermidades que podem ser tratadas com agentes de elevação de colesterol-hdl e compostos
EP2457913B1 (en) 2006-10-19 2017-04-19 Signal Pharmaceuticals, LLC Heteroaryl compounds, compositions thereof, and methods of treatment therewith
US8148361B2 (en) 2006-11-10 2012-04-03 Bristol-Myers Squibb Company Kinase inhibitors
US20080132698A1 (en) 2006-11-30 2008-06-05 University Of Ottawa Use of N-oxide compounds in coupling reactions
TW200833690A (en) 2006-12-15 2008-08-16 Bayer Schering Pharma Ag 3-H-pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
AU2007338792B2 (en) 2006-12-20 2012-05-31 Amgen Inc. Substituted heterocycles and methods of use
PE20121126A1 (es) 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
GB0625659D0 (en) 2006-12-21 2007-01-31 Cancer Rec Tech Ltd Therapeutic compounds and their use
AU2008219166B2 (en) 2007-02-16 2013-05-16 Amgen Inc. Nitrogen-containing heterocyclyl ketones and their use as c-Met inhibitors
EA019951B1 (ru) 2007-03-01 2014-07-30 Новартис Аг Ингибиторы киназы pim и способы их применения
RU2009141185A (ru) 2007-04-10 2011-05-20 Байер КропСайенс АГ (DE) Инсектицидные производные арилизоксазолина
JP2008260691A (ja) 2007-04-10 2008-10-30 Bayer Cropscience Ag 殺虫性アリールイソオキサゾリン誘導体
JP2010526823A (ja) 2007-05-10 2010-08-05 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Pi3キナーゼ阻害物質としてのキノキサリン誘導体
PE20090717A1 (es) 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
UY31137A1 (es) 2007-06-14 2009-01-05 Smithkline Beecham Corp Derivados de quinazolina como inhibidores de la pi3 quinasa
JP2009027904A (ja) 2007-06-19 2009-02-05 Hitachi Ltd 回転電機
EP2012409A2 (en) 2007-06-19 2009-01-07 Hitachi, Ltd. Rotating electrical machine
JPWO2008156174A1 (ja) 2007-06-21 2010-08-26 大正製薬株式会社 ピラジンアミド化合物
KR20100037047A (ko) 2007-06-26 2010-04-08 렉시컨 파마슈티컬스 인코퍼레이티드 세로토닌-매개 질환 및 장애의 치료 방법
WO2009005638A2 (en) 2007-06-27 2009-01-08 Merck & Co., Inc. Pyridyl and pyrimidinyl derivatives as histone deacetylase inhibitors
GB0713259D0 (en) 2007-07-09 2007-08-15 Astrazeneca Ab Pyrazine derivatives 954
AU2008275891B2 (en) 2007-07-19 2013-10-10 H.Lundbeck A/S 5-membered heterocyclic amides and related compounds
CN101801958B (zh) 2007-07-19 2014-01-29 默沙东公司 作为蛋白质激酶抑制剂的杂环酰胺化合物
KR20100038119A (ko) 2007-08-01 2010-04-12 화이자 인코포레이티드 피라졸 화합물 및 raf 억제제로서 이의 용도
WO2009024825A1 (en) 2007-08-21 2009-02-26 Astrazeneca Ab 2-pyrazinylbenzimidazole derivatives as receptor tyrosine kinase inhibitors
WO2009037247A1 (en) 2007-09-17 2009-03-26 Neurosearch A/S Pyrazine derivatives and their use as potassium channel modulators
AU2008315746A1 (en) 2007-10-25 2009-04-30 Astrazeneca Ab Pyridine and pyrazine derivatives useful in the treatment of cell proliferative disorders
JP2011511005A (ja) 2008-02-04 2011-04-07 オーエスアイ・フアーマスーテイカルズ・インコーポレーテツド 2−アミノピリジン系キナーゼ阻害薬
CN101939324B (zh) 2008-02-25 2014-10-15 霍夫曼-拉罗奇有限公司 吡咯并吡嗪激酶抑制剂
ATE519763T1 (de) 2008-02-25 2011-08-15 Hoffmann La Roche Pyrrolopyrazin-kinasehemmer
CN101945877B (zh) 2008-02-25 2013-07-03 霍夫曼-拉罗奇有限公司 吡咯并吡嗪激酶抑制剂
PT2250172E (pt) 2008-02-25 2011-11-30 Hoffmann La Roche Inibidores de pirrolpirazina-cinase
TW200940537A (en) 2008-02-26 2009-10-01 Astrazeneca Ab Heterocyclic urea derivatives and methods of use thereof
JP2011513332A (ja) 2008-02-29 2011-04-28 アレイ バイオファーマ、インコーポレイテッド 癌の治療のためのraf阻害剤としてのn−(6−アミノピリジン−3−イル)−3−(スルホンアミド)ベンズアミド誘導体
US8268834B2 (en) 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
US8110576B2 (en) 2008-06-10 2012-02-07 Plexxikon Inc. Substituted pyrrolo[2,3b]pyrazines and methods for treatment of raf protein kinase-mediated indications
GB0814364D0 (en) 2008-08-05 2008-09-10 Eisai London Res Lab Ltd Diazaindole derivatives and their use in the inhibition of c-Jun N-terminal kinase
CA2731368C (en) 2008-08-06 2013-05-14 Pfizer Inc. 6 substituted 2-heterocyclylamino pyrazine compounds as chk-1 inhibitors
EP2326650B9 (en) 2008-08-06 2014-09-10 BioMarin Pharmaceutical Inc. Dihydropyridophthalazinone inhibitors of poly(adp-ribose)polymerase (parp)
JP2010077286A (ja) 2008-09-26 2010-04-08 Aica Kogyo Co Ltd シリコーン樹脂組成物および粘着フィルム
AU2009307770A1 (en) 2008-10-21 2010-04-29 Vertex Pharmaceuticals Incorporated C-Met protein kinase inhibitors
WO2010054398A1 (en) 2008-11-10 2010-05-14 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2379561B1 (en) 2008-11-25 2015-11-04 University Of Rochester Mlk inhibitors and methods of use
EP2373653B1 (en) 2008-12-05 2014-04-02 F. Hoffmann-La Roche AG Pyrrolopyrazinyl urea kinase inhibitors
AU2009327357C1 (en) 2008-12-19 2017-02-02 Vertex Pharmaceuticals Incorporated Pyrazine derivatives useful as inhibitors of ATR kinase
CA2748099C (en) 2008-12-22 2017-02-28 Array Biopharma Inc. 7-phenoxychroman carboxylic acid derivatives
TW201028410A (en) 2008-12-22 2010-08-01 Astrazeneca Ab Chemical compounds 610
MX2011006332A (es) 2008-12-23 2011-06-27 Abbott Lab Compuestos antivirales.
WO2010087430A1 (ja) 2009-01-30 2010-08-05 富山化学工業株式会社 N-アシルアントラニル酸誘導体またはその塩
JP5353279B2 (ja) 2009-02-06 2013-11-27 Jnc株式会社 セレンテラミド又はその類縁体の製造方法
SG173639A1 (en) 2009-02-11 2011-09-29 Sunovion Pharmaceuticals Inc Histamine h3 inverse agonists and antagonists and methods of use thereof
CN101537007A (zh) 2009-03-18 2009-09-23 中国医学科学院血液病医院(血液学研究所) N-(噻吩-2)吡唑并[1,5-a]嘧啶-3-甲酰胺类化合物在制备抗恶性肿瘤药物方面的应用
EP2411007A4 (en) 2009-03-27 2012-12-05 Uab Research Foundation MODULATION OF IRES-MEDIATED TRANSLATION
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
JP2012533248A (ja) 2009-07-13 2012-12-20 ヴェーデクス・アクティーセルスカプ 脳波検出に適する補聴器およびそのような補聴器を適応する方法
ES2483594T3 (es) 2009-07-15 2014-08-06 Abbott Laboratories Pirrolopirazinas inhibidoras de quinasas
AP3534A (en) 2009-08-07 2016-01-13 Dow Agrosciences Llc Pesticidal compositions
JP2011042639A (ja) 2009-08-24 2011-03-03 Kowa Co ビフェニルピラジン化合物及びこれを有効成分として含有するエリスロポエチン産生促進剤
CN101671336B (zh) 2009-09-23 2013-11-13 辽宁利锋科技开发有限公司 芳杂环并嘧啶衍生物和类似物及其制备方法和用途
DE102009043260A1 (de) 2009-09-28 2011-04-28 Merck Patent Gmbh Pyridinyl-imidazolonderivate
RU2017109664A (ru) 2009-10-06 2019-01-23 Милленниум Фармасьютикалз, Инк. Гетероциклические соединения, используемые в качестве ингибиторов pdk1
BR112012017713A2 (pt) 2010-01-18 2020-06-23 Mmv Medicines For Malaria Venture Aminopiridina, formulação farmacêutica, processo para a preparação de um derivado de aminopiridina, intermediário, e, uso de uma aminopiridina ou de uma formulação farmacêutica
US8518945B2 (en) 2010-03-22 2013-08-27 Hoffmann-La Roche Inc. Pyrrolopyrazine kinase inhibitors
WO2011124998A1 (en) 2010-04-08 2011-10-13 Pfizer Inc. Substituted 3,5- di phenyl - isoxazoline derivatives as insecticides and acaricides
EP2558866B1 (en) 2010-04-15 2016-08-17 Tracon Pharmaceuticals, Inc. Potentiation of anti-cancer activity through combination therapy with ber pathway inhibitors
WO2011138751A2 (en) 2010-05-04 2011-11-10 Pfizer Inc. Heterocyclic derivatives as alk inhibitors
WO2011143422A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated 2 -aminopyridine derivatives useful as inhibitors of atr kinase
US8962631B2 (en) 2010-05-12 2015-02-24 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2011143399A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
JP2013526540A (ja) 2010-05-12 2013-06-24 バーテックス ファーマシューティカルズ インコーポレイテッド Atrキナーゼ阻害剤として有用な化合物
WO2011143423A2 (en) * 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
MX2012013081A (es) 2010-05-12 2013-05-09 Vertex Pharma Compuestos utiles como inhibidores de cinasa atr.
RU2012152352A (ru) 2010-05-20 2014-06-27 Ф. Хоффманн-Ля Рош Аг ПРОИЗВОДНЫЕ ПИРРОЛО[2,3-b]ПИРАЗИН-7-КАРБОКСАМИДА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ JAK И SYK
EP2571881A1 (en) 2010-05-20 2013-03-27 F.Hoffmann-La Roche Ag Pyrrolopyrazine derivatives as syk and jak inhibitors
US8623869B2 (en) 2010-06-23 2014-01-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
CN102311396B (zh) 2010-07-05 2015-01-07 暨南大学 一种吡嗪类衍生物和其制备方法及在制药中的应用
EP2407478A1 (en) 2010-07-14 2012-01-18 GENETADI Biotech, S.L. New cyclotetrapeptides with pro-angiogenic properties
JP5782238B2 (ja) 2010-07-30 2015-09-24 ルネサスエレクトロニクス株式会社 電圧検出回路及びその制御方法
US8440652B2 (en) 2011-03-04 2013-05-14 Lexicon Pharmaceuticals, Inc. MST1 kinase inhibitors and methods of their use
US8962623B2 (en) 2011-03-04 2015-02-24 Locus Pharmaceuticals, Inc. Aminopyrazine compounds
MX2013011450A (es) 2011-04-05 2014-02-03 Vertex Pharma Compuestos de aminopirazina utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr).
EP2710006A1 (en) 2011-05-17 2014-03-26 Principia Biopharma Inc. Azaindole derivatives as tyrosine kinase inhibitors
US9096602B2 (en) 2011-06-22 2015-08-04 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-B]pyrazines as ATR kinase inhibitors
WO2012178123A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
JP2014517079A (ja) 2011-06-22 2014-07-17 バーテックス ファーマシューティカルズ インコーポレイテッド Atrキナーゼ阻害剤として有用な化合物
EP2751088B1 (en) 2011-09-30 2016-04-13 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2751099B1 (en) 2011-09-30 2017-06-14 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
SG11201401095YA (en) 2011-09-30 2014-04-28 Vertex Pharma Treating pancreatic cancer and non-small cell lung cancer with atr inhibitors
WO2013049720A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
RS59337B1 (sr) 2011-09-30 2019-10-31 Vertex Pharma Postupak za izradu jedinjenja, korisnih kao inhibitori atr kinaze
US8846917B2 (en) 2011-11-09 2014-09-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
US8841450B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2013071090A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2776419B1 (en) 2011-11-09 2016-05-11 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
EP2776429A1 (en) * 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
ES2654670T3 (es) 2012-04-05 2018-02-14 Vertex Pharmaceuticals Incorporated Compuestos útiles como inhibidores de la cinasa ATR y terapias de combinación de los mismos
CN103373996A (zh) 2012-04-20 2013-10-30 山东亨利医药科技有限责任公司 作为crth2受体拮抗剂的二并环衍生物
WO2014055756A1 (en) 2012-10-04 2014-04-10 Vertex Pharmaceuticals Incorporated Method for measuring atr inhibition mediated increases in dna damage
EP2909202A1 (en) 2012-10-16 2015-08-26 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
PT4190786T (pt) 2012-12-07 2025-05-29 Vertex Pharma Compostos úteis como inibidores da quinase atr
JP6096005B2 (ja) 2013-02-26 2017-03-15 リンテック株式会社 シート剥離装置および剥離方法
CA2932757C (en) 2013-12-06 2023-10-31 Vertex Pharmaceuticals Incorporated 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof
KR102575125B1 (ko) 2014-06-05 2023-09-07 버텍스 파마슈티칼스 인코포레이티드 Atr 키나제의 저해제로서 유용한 2-아미노-6-플루오로-n-[5-플루오로-피리딘-3-일]-피라졸로[1,5-a]피리미딘-3-카복스아미드 화합물의 방사성표지된 유도체, 상기 화합물의 제조 및 이의 다양한 고체 형태
RU2736219C2 (ru) 2014-06-17 2020-11-12 Вертекс Фармасьютикалз Инкорпорейтед Способ лечения рака с использованием комбинации ингибиторов снк1 и atr

Also Published As

Publication number Publication date
JP2020059753A (ja) 2020-04-16
EP2750679A1 (en) 2014-07-09
US10813929B2 (en) 2020-10-27
ES2940121T3 (es) 2023-05-03
IL231813A0 (en) 2014-05-28
IN2014CN02501A (ru) 2015-06-26
AU2012315384B2 (en) 2017-08-10
AU2019203240A1 (en) 2019-05-30
AU2012315384A8 (en) 2014-05-08
CN103957917A (zh) 2014-07-30
JP2017119724A (ja) 2017-07-06
CA3089792A1 (en) 2013-04-04
MX392542B (es) 2025-03-24
MX2019006684A (es) 2019-08-21
SG11201401095YA (en) 2014-04-28
MX2014003785A (es) 2014-07-24
CN108685922A (zh) 2018-10-23
AU2019203240B2 (en) 2021-01-28
CA2850491C (en) 2020-10-27
MX373340B (es) 2020-05-13
BR112014007690B1 (pt) 2022-10-04
EP3733185B1 (en) 2022-12-07
ZA201402627B (en) 2015-10-28
BR112014007690A2 (pt) 2017-04-18
KR20140068254A (ko) 2014-06-05
KR102056586B1 (ko) 2019-12-18
RU2018108589A3 (ru) 2021-12-03
CA3089792C (en) 2023-03-14
CN108464983A (zh) 2018-08-31
EP2750679B1 (en) 2021-09-01
US20130089626A1 (en) 2013-04-11
ES2899880T3 (es) 2022-03-15
SG10201602515QA (en) 2016-05-30
RU2648507C2 (ru) 2018-03-26
JP2018119014A (ja) 2018-08-02
CA2850491A1 (en) 2013-04-04
NZ623119A (en) 2016-10-28
JP2014528423A (ja) 2014-10-27
JP7162585B2 (ja) 2022-10-28
IL231813B (en) 2019-12-31
EP3733185A1 (en) 2020-11-04
JP6162126B2 (ja) 2017-08-23
RU2018108589A (ru) 2019-02-25
AU2012315384A1 (en) 2014-04-17
WO2013049859A1 (en) 2013-04-04
AU2017206224A1 (en) 2017-08-03
US20140356456A1 (en) 2014-12-04
US20200390761A1 (en) 2020-12-17

Similar Documents

Publication Publication Date Title
RU2014117666A (ru) Лечение рака поджелудочной железы и немелкоклеточного рака легкого ингибиторами атr
JP2014528423A5 (ru)
JOP20210231A1 (ar) مركبات ترابطية مستهدفة كمركبات علاجية
EA201490472A1 (ru) Комбинированная терапия рака hsp90-ингибитором и антиметаболитом
CY1119676T1 (el) Συνθεσεις και μεθοδοι για τη θεραπεια του καρκινου
CY1123010T1 (el) Διεγερση γονιδιου τrail με μικρο μοριο απο κανονικα και ογκου κυτταρα ως αντικαρκινικη θεραπεια
CY1122707T1 (el) Ετεροκυκλικοι αναστολεις γλουταμινασης
EA201201186A1 (ru) ИСПОЛЬЗОВАНИЕ ErbB3 ИНГИБИТОРОВ В ЛЕЧЕНИИ ТРИЖДЫ НЕГАТИВНОГО И БАЗАЛЬНО-ПОДОБНОГО ВИДОВ РАКА МОЛОЧНОЙ ЖЕЛЕЗЫ
CY1118771T1 (el) Μακροκυκλικα παραγωγα για την αγωγη υπερπλαστικων παθησεων
PH12017501500A1 (en) Methods for treating non- small cell lung cancer using tor kinase inhibitor combination therapy
MY183661A (en) Treatment of cancer with tor kinase inhibitors
EA201490673A1 (ru) Производные пирролопиримидина и пурина
TR201807411T4 (tr) DNA-PK inhibitörleri.
EA201791284A1 (ru) Селективные ингибиторы cdk8/cdk19 и их применение в качестве противометастатических и химиопрофилактических агентов для лечения рака
MD20160016A2 (ru) Новые индолизиновые соединения, способ их получения ифармацевтические композиции, их содержащие
JP2018508593A5 (ru)
NZ723971A (en) Methods and compositions for treating ewings sarcoma family of tumors
EA201500334A1 (ru) Fgfr3 гибридный ген и лекарственный препарат, нацеленный на него
EA201500373A1 (ru) Маситиниб или его соль для лечения рака, фармацевтическая композиция, лекарственное средство и набор
PH12013502144A1 (en) Multiple myeloma treatment
JP2013525283A5 (ru)
CY1121973T1 (el) Θεραπεια φαρμακευτικα ανθεκτικου καρκινου η οποια στοχευει καρκινικα βλαστοκυτταρα
ECSP14019113A (es) Inhibidores de pirazolopirimidinilo de enzima activadora de ubiquitina
MX2015006004A (es) Inhibicion de celulas cancerosas resistentes a farmacos.
Li et al. AAZ2 induces mitochondrial-dependent apoptosis by targeting PDK1 in gastric cancer