CA2939333C - Pyrazole compounds as chk1 inhibitors for the treatment of cancer - Google Patents

Pyrazole compounds as chk1 inhibitors for the treatment of cancer Download PDF

Info

Publication number
CA2939333C
CA2939333C CA2939333A CA2939333A CA2939333C CA 2939333 C CA2939333 C CA 2939333C CA 2939333 A CA2939333 A CA 2939333A CA 2939333 A CA2939333 A CA 2939333A CA 2939333 C CA2939333 C CA 2939333C
Authority
CA
Canada
Prior art keywords
methoxy
pyrazol
carbonitrile
amino
pyrazine
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CA2939333A
Other languages
English (en)
French (fr)
Other versions
CA2939333A1 (en
Inventor
Robert George Boyle
David Winter Walker
Richard Justin Boyce
Scott Peterson
Francine Farouz
Cong Hung Vo
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sentinel Oncology Ltd
Original Assignee
Sentinel Oncology Ltd
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 Sentinel Oncology Ltd filed Critical Sentinel Oncology Ltd
Publication of CA2939333A1 publication Critical patent/CA2939333A1/en
Application granted granted Critical
Publication of CA2939333C publication Critical patent/CA2939333C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2939333A 2014-02-10 2015-02-09 Pyrazole compounds as chk1 inhibitors for the treatment of cancer Active CA2939333C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GBGB1402277.6A GB201402277D0 (en) 2014-02-10 2014-02-10 Pharmaceutical compounds
GB1402277.6 2014-02-10
US201462083687P 2014-11-24 2014-11-24
US62/083,687 2014-11-24
PCT/US2015/015030 WO2015120390A1 (en) 2014-02-10 2015-02-09 Pharmaceutical compounds

Publications (2)

Publication Number Publication Date
CA2939333A1 CA2939333A1 (en) 2015-08-13
CA2939333C true CA2939333C (en) 2022-12-06

Family

ID=50390744

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2939333A Active CA2939333C (en) 2014-02-10 2015-02-09 Pyrazole compounds as chk1 inhibitors for the treatment of cancer

Country Status (21)

Country Link
US (3) US10010547B2 (enExample)
EP (2) EP3811944B1 (enExample)
JP (2) JP6506779B2 (enExample)
KR (3) KR20190127997A (enExample)
CN (3) CN106170288B (enExample)
AU (2) AU2015213679B2 (enExample)
BR (1) BR112016018384B1 (enExample)
CA (1) CA2939333C (enExample)
ES (1) ES3036500T3 (enExample)
GB (1) GB201402277D0 (enExample)
IL (2) IL247150B (enExample)
MX (1) MX380250B (enExample)
MY (1) MY192588A (enExample)
PH (1) PH12016501578B1 (enExample)
PL (1) PL3811944T3 (enExample)
RS (1) RS67122B1 (enExample)
RU (1) RU2687060C2 (enExample)
SG (2) SG10201810879VA (enExample)
UA (1) UA121747C2 (enExample)
WO (1) WO2015120390A1 (enExample)
ZA (1) ZA201605812B (enExample)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201402277D0 (en) 2014-02-10 2014-03-26 Sentinel Oncology Ltd Pharmaceutical compounds
PL3411036T3 (pl) * 2016-02-04 2022-04-04 Pharmaengine, Inc. 3,5-dipodstawione pirazole przydatne jako inhibitory kinazy punktu kontrolnego 1 (chk1) oraz ich preparaty i zastosowanie
IT201600092469A1 (it) * 2016-09-14 2018-03-14 Lundbeck Pharmaceuticals Italy S P A Processo per la produzione di Blonanserina
SG11201903013SA (en) 2016-10-18 2019-05-30 Seattle Genetics Inc Targeted delivery of nicotinamide adenine dinucleotide salvage pathway inhibitors
SG11201908788YA (en) * 2017-03-31 2019-10-30 Seattle Genetics Inc Combinations of chk1- and wee1 - inhibitors
CA3090233A1 (en) 2018-02-07 2019-08-15 Korea Research Institute Of Chemical Technology Compounds for inhibiting tnik and medical uses thereof
KR20220042159A (ko) 2019-08-01 2022-04-04 인테그랄 바이오사이언스 피브이티. 엘티디. 키나제 억제제로서의 헤테로사이클릭 화합물 및 이의 용도
CN112457306A (zh) * 2019-09-06 2021-03-09 上海瑛派药业有限公司 3,5-二取代吡唑化合物作为激酶抑制剂及其应用
EP4067351B1 (en) * 2019-11-29 2025-01-22 NovaOnco JS Therapeutics Co., Ltd. Diazaindole derivative and use thereof as chk1 inhibitor
WO2021113661A1 (en) 2019-12-05 2021-06-10 Seagen Inc. Amorphous and polymorphic form of a specific chk1 inhibitor
WO2021119236A1 (en) 2019-12-10 2021-06-17 Seagen Inc. Preparation of a chk1 inhibitor compound
CN112194586B (zh) * 2020-09-08 2023-03-10 青岛职业技术学院 一种沙丁胺醇二聚体的制备方法
US12410154B2 (en) 2020-11-30 2025-09-09 Sumitomo Pharma Co., Ltd. 5-heteroaryl-1H-pyrazol-3-amine derivative
US11564920B2 (en) 2020-11-30 2023-01-31 Sumitomo Pharma Co., Ltd. 5-heteroaryl-1H-pyrazol-3-amine derivative
US12036286B2 (en) 2021-03-18 2024-07-16 Seagen Inc. Selective drug release from internalized conjugates of biologically active compounds
BR112023024571A2 (pt) * 2021-05-27 2024-02-06 Boundless Bio Inc Inibidores de quinase do ponto de verificação 1 (chk1) e usos dos mesmos
GB202107932D0 (en) 2021-06-03 2021-07-21 Sentinel Oncology Ltd Preparation of a CHK1 Inhibitor Compound
GB202107924D0 (en) * 2021-06-03 2021-07-21 Sentinel Oncology Ltd A pharmaceutical salt
MX2024007910A (es) * 2021-12-24 2024-09-04 Sumitomo Pharma Co Ltd Derivado de 1h-pirazol-3-amina que tiene una estructura principal bicíclica.
EP4532492A1 (en) * 2022-05-25 2025-04-09 Sperogenix Therapeutics Limited Nitrogen-containing five-membered heterocyclic derivatives as checkpoint kinase 1 inhibitor and uses thereof
WO2023229032A1 (ja) * 2022-05-27 2023-11-30 住友ファーマ株式会社 免疫チェックポイント阻害剤に対して治療抵抗性を示すがんの治療薬
JP7546104B2 (ja) * 2022-05-27 2024-09-05 住友ファーマ株式会社 ５－ヘテロアリール－１ｈ－ピラゾール－３－アミン誘導体からなる医薬
GB202213792D0 (en) 2022-09-21 2022-11-02 Benevolentai Bio Ltd New compounds and method
TW202440549A (zh) * 2022-11-29 2024-10-16 美商無界生物公司 檢查點激酶１（ｃｈｋ１）抑制劑及其用途
WO2024196923A1 (en) * 2023-03-20 2024-09-26 Boundless Bio, Inc. Uses of a checkpoint kinase 1 (chk1) inhibitor
GB202403910D0 (en) 2024-03-19 2024-05-01 Benovental Cambridge Ltd New processes and intermediates for pharmaceutical products

Family Cites Families (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5443720B2 (enExample) 1972-02-18 1979-12-21
JPS5219583B2 (enExample) 1973-07-17 1977-05-28
JPS5431279Y2 (enExample) 1975-07-31 1979-09-29
JPS5443720U (enExample) 1977-09-01 1979-03-26
JP2004508373A (ja) 2000-09-07 2004-03-18 バイエル・フアーマシユーチカルズ・コーポレーシヨン 環式および非環式アミジンおよびプロゲステロン受容体結合剤として使用するためのそれらを含有する医薬組成物
UA76977C2 (en) 2001-03-02 2006-10-16 Icos Corp Aryl- and heteroaryl substituted chk1 inhibitors and their use as radiosensitizers and chemosensitizers
WO2003010444A1 (en) 2001-07-23 2003-02-06 Shock-Proof Solutions Pty Ltd Mechanical shock absorbing apparatus
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
US7074809B2 (en) 2002-08-09 2006-07-11 Astrazeneca Ab Compounds
TW200812986A (en) 2002-08-09 2008-03-16 Nps Pharma Inc New compounds
WO2004048343A1 (en) * 2002-11-28 2004-06-10 Schering Aktiengesellschaft Chk-, pdk- and akt-inhibitory pyrimidines, their production and use as pharmaceutical agents
AR043633A1 (es) 2003-03-20 2005-08-03 Schering Corp Ligandos de receptores de canabinoides
BRPI0412820A (pt) * 2003-07-25 2006-09-26 Pfizer compostos de aminopirazol e utilização como inibidores de chk1
US7163939B2 (en) 2003-11-05 2007-01-16 Abbott Laboratories Macrocyclic kinase inhibitors
GB0326601D0 (en) * 2003-11-14 2003-12-17 Novartis Ag Organic compounds
HRP20100675T1 (hr) 2003-12-23 2011-01-31 Astex Therapeutics Limited Derivati pirazola kao modulatori protein kinaze
WO2005072733A1 (en) 2004-01-20 2005-08-11 Millennium Pharmaceuticals, Inc. Dyarylurea compounds as chk-1 inhibitors
WO2005077368A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
JP2008505112A (ja) 2004-07-02 2008-02-21 イコス・コーポレイション Ｃｈｋ１の阻害に有用な化合物
AU2005272586A1 (en) 2004-08-19 2006-02-23 Icos Corporation Compounds useful for inhibiting CHK1
EP2038257A1 (en) * 2006-06-12 2009-03-25 Sentinel Oncology Limited N-oxides of diarylurea derivatives and their use as chk1 inhibitors for the treatment of cancer
WO2008063558A2 (en) * 2006-11-17 2008-05-29 Schering Corporation Combination of an inhibitor of dna polymerase-alpha and an inhibitor of a checkpoint kinase for proliferative disorders
JP5219583B2 (ja) 2008-03-31 2013-06-26 住友化学株式会社 組成物、光学フィルムとその製造方法、光学部材及び表示装置
JP5443720B2 (ja) 2008-09-05 2014-03-19 住友化学株式会社 組成物、光学フィルム及びその製造方法、光学部材ならびに表示装置
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
PA8850801A1 (es) * 2008-12-17 2010-07-27 Lilly Co Eli Compuestos útiles para inhibir chk1
US8314108B2 (en) 2008-12-17 2012-11-20 Eli Lilly And Company 5-(5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine-2-carbonitrile, pharmaceutically acceptable salts thereof, or solvate of salts
EP2416773B1 (en) 2009-04-11 2016-09-28 Array Biopharma, Inc. Checkpoint kinase 1 inhibitors for potentiating dna damaging agents
GB0911042D0 (en) 2009-06-25 2009-08-12 Istituto Superiore Di Sanito Treatment of tumorigenic cells in solid tumours
SG10201502484SA (en) 2010-03-30 2015-05-28 Verseon Corp Multisubstituted aromatic compounds as inhibitors of thrombin
GB201008005D0 (en) 2010-05-13 2010-06-30 Sentinel Oncology Ltd Pharmaceutical compounds
WO2012016133A2 (en) 2010-07-29 2012-02-02 President And Fellows Of Harvard College Ros1 kinase inhibitors for the treatment of glioblastoma and other p53-deficient cancers
JO3145B1 (ar) 2010-11-08 2017-09-20 Lilly Co Eli مركبات مفيدة لتثبيط chk1
EP2655334B1 (en) 2010-12-22 2018-10-03 Eutropics Pharmaceuticals, Inc. Compositions and methods useful for treating diseases
US9255072B2 (en) 2011-03-04 2016-02-09 National Health Rsearch Institutes Pyrazole compounds and thiazole compounds as protein kinases 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
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
GB201119799D0 (en) 2011-11-16 2011-12-28 Sentinel Oncology Ltd Pharmaceutical compounds
CN105793424B (zh) 2013-07-12 2021-02-19 亥姆霍兹感染研究中心有限公司 孢囊菌酰胺
KR102181235B1 (ko) 2013-08-30 2020-11-23 삼성디스플레이 주식회사 축합환 화합물 및 이를 포함한 유기 발광 소자
KR102191991B1 (ko) 2013-09-06 2020-12-17 삼성디스플레이 주식회사 축합환 화합물 및 이를 포함한 유기 발광 소자
KR102167042B1 (ko) 2013-09-06 2020-10-19 삼성디스플레이 주식회사 축합환 화합물 및 이를 포함한 유기 발광 소자
KR102191990B1 (ko) 2013-09-10 2020-12-17 삼성디스플레이 주식회사 축합환 화합물 및 이를 포함한 유기 발광 소자
WO2015084047A1 (ko) 2013-12-04 2015-06-11 주식회사 동진쎄미켐 신규한 화합물 및 이를 포함하는 유기발광소자
GB201402277D0 (en) 2014-02-10 2014-03-26 Sentinel Oncology Ltd Pharmaceutical compounds
WO2015124606A1 (en) 2014-02-18 2015-08-27 Basf Se N-substituted imino heterocyclic compounds for combating invertebrate pests
CN105017626B (zh) 2014-04-15 2018-03-23 中国石化扬子石油化工有限公司 一种乙烯‑α‑烯烃共聚物、其制造方法及其应用
CN105017625B (zh) 2014-04-15 2017-07-14 中国石化扬子石油化工有限公司 一种乙烯‑α‑烯烃共聚物、其制造方法及其应用
CN105001360B (zh) 2014-04-15 2018-03-20 中国石化扬子石油化工有限公司 一种乙烯‑α‑烯烃共聚物、其制造方法及其应用
CN105017456B (zh) 2014-04-15 2017-06-06 中国石化扬子石油化工有限公司 一种乙烯‑α‑烯烃共聚物、其制造方法及其应用
JP6096710B2 (ja) 2014-04-30 2017-03-15 東京瓦斯株式会社 燃料電池システム
EP3189551B1 (de) 2014-09-05 2021-01-27 Merck Patent GmbH Formulierungen und verfahren zur herstellung einer organischen elektrolumineszenzvorrichtung
JP6841759B2 (ja) 2014-12-19 2021-03-10 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 ビメソゲン化合物およびメソゲン性媒体
US10791739B2 (en) 2015-03-25 2020-10-06 Vanderbilt University Binary compositions as disruptors of orco-mediated odorant sensing
WO2017019822A1 (en) 2015-07-29 2017-02-02 Medivation Technologies, Inc. Pellet composition containing repair cells
WO2017019817A1 (en) 2015-07-29 2017-02-02 Medivation Technologies, Inc. Methods and compositions for targeted therapeutics
WO2017019830A1 (en) 2015-07-29 2017-02-02 Medivation Technologies, Inc. Methods and compositions for targeted therapeutics
WO2017105982A1 (en) 2015-12-15 2017-06-22 Eli Lilly And Company Combination therapy for cancer

Also Published As

Publication number Publication date
IL247150A0 (en) 2016-09-29
US20210275525A1 (en) 2021-09-09
BR112016018384B1 (pt) 2023-01-17
AU2019202168A1 (en) 2019-04-18
EP3811944A1 (en) 2021-04-28
CN110141570A (zh) 2019-08-20
IL247150B (en) 2019-12-31
AU2015213679B2 (en) 2019-02-21
SG10201810879VA (en) 2019-01-30
CN106170288B (zh) 2019-07-19
MY192588A (en) 2022-08-29
WO2015120390A1 (en) 2015-08-13
US10010547B2 (en) 2018-07-03
RS67122B1 (sr) 2025-09-30
US20180271860A1 (en) 2018-09-27
KR20160125991A (ko) 2016-11-01
US20160361310A1 (en) 2016-12-15
PH12016501578A1 (en) 2017-02-06
CA2939333A1 (en) 2015-08-13
PH12016501578B1 (en) 2023-04-19
EP3811944B1 (en) 2025-07-16
EP3104860A1 (en) 2016-12-21
JP2017508787A (ja) 2017-03-30
EP3811944C0 (en) 2025-07-16
KR20190035937A (ko) 2019-04-03
EP3104860B1 (en) 2020-12-30
EP3104860A4 (en) 2017-08-16
NZ723051A (en) 2020-10-30
KR101964251B1 (ko) 2019-04-01
CN106170288A (zh) 2016-11-30
KR20190127997A (ko) 2019-11-13
BR112016018384A2 (enExample) 2017-08-08
AU2015213679A1 (en) 2016-08-25
ZA201605812B (en) 2023-02-22
JP2019070044A (ja) 2019-05-09
JP6506779B2 (ja) 2019-04-24
SG11201606553XA (en) 2016-09-29
US10973817B2 (en) 2021-04-13
PL3811944T3 (pl) 2025-10-06
ES3036500T3 (en) 2025-09-19
RU2016136116A (ru) 2018-03-15
CN110143950A (zh) 2019-08-20
UA121747C2 (uk) 2020-07-27
RU2687060C2 (ru) 2019-05-07
IL270954A (en) 2020-01-30
RU2016136116A3 (enExample) 2018-09-28
MX380250B (es) 2025-03-12
GB201402277D0 (en) 2014-03-26
US11786524B2 (en) 2023-10-17
MX2016010296A (es) 2017-01-11

Similar Documents

Publication Publication Date Title
US11786524B2 (en) Pharmaceutical compounds
JP7317878B2 (ja) 多環式ｔｌｒ７／８アンタゴニスト及び免疫障害の治療におけるそれらの使用
KR20240070619A (ko) 폴리사이클릭 융합 고리 유도체 및 이의 용도
EP3126364B1 (en) Macrocylic pyrimidine derivatives
AU2024203629A1 (en) TLR7/8 antagonists and uses thereof
NZ586756A (en) Indolyl-pyridone derivatives having checkpoint kinase 1 inhibitory activity
US20240408064A1 (en) Ras inhibitors, compositions and methods of use thereof
US20230019491A1 (en) PYRIMIDINE TBK/IKKe INHIBITOR COMPOUNDS AND USES THEREOF
IL312303A (en) Heterocyclic compounds with three rings, their preparation and pharmaceutical preparations containing them
AU2018352701A1 (en) Pyrimidine ΤΒΚ/ΙΚΚE inhibitor compounds and uses thereof
HK1231755B (en) Pharmaceutical compounds as chk1 inhibitors
NZ723051B2 (en) Pharmaceutical compounds

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20200204

EEER Examination request

Effective date: 20200204

EEER Examination request

Effective date: 20200204

EEER Examination request

Effective date: 20200204