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CY1119084T1 - Υποκατεστημενα τρικυκλικα βενζιμιδαζολια ως αναστολεις κινασης - Google Patents

Υποκατεστημενα τρικυκλικα βενζιμιδαζολια ως αναστολεις κινασης

Info

Publication number
CY1119084T1
CY1119084T1 CY20171100592T CY171100592T CY1119084T1 CY 1119084 T1 CY1119084 T1 CY 1119084T1 CY 20171100592 T CY20171100592 T CY 20171100592T CY 171100592 T CY171100592 T CY 171100592T CY 1119084 T1 CY1119084 T1 CY 1119084T1
Authority
CY
Cyprus
Prior art keywords
substituted tricyclic
compounds
disclosed
tricyclic benzimidazoles
inhibitors
Prior art date
Application number
CY20171100592T
Other languages
English (en)
Inventor
Tomasz Rzymski
Adrian Zarebski
Agnieszka Dreas
Karolina Osowska
Katarzyna Kucwaj
Joanna Fogt
Marek Cholody
Michal Galezowski
Wojciech Czardybon
Raymond Horvath
Katarzyna Wiklik
Mariusz Milik
Krzysztof Brzózka
Original Assignee
Selvita S.A.
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 Selvita S.A. filed Critical Selvita S.A.
Publication of CY1119084T1 publication Critical patent/CY1119084T1/el

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/06Peri-condensed systems
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/06Peri-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Εδώ αποκαλύπτονται ενώσεις υποκατεστημένων τρικυκλικών βενζιμιδαζολίων όπως ορίζονται εδώ στον τύπο (I) ή φαρμακευτικώς αποδεκτά άλατα αυτών. Οι ενώσεις της εφεύρεσης αναστέλλουν εκλεκτικώς την CDK8 και είναι συνεπώς χρήσιμες για τη θεραπεία νόσων που σχετίζονται με αυτή την κινάση, ειδικότερα ορθοκολικών και μελανωματικών καρκίνων και άλλων στερεών και αιματολογικών κακοηθειών, αυτοάνοσων νόσων και φλεγμονωδών νόσων. Επίσης αποκαλύπτονται διεργασίες για την παρασκευή αυτών των ενώσεων.
CY20171100592T 2012-11-08 2017-06-06 Υποκατεστημενα τρικυκλικα βενζιμιδαζολια ως αναστολεις κινασης CY1119084T1 (el)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1220157.0A GB201220157D0 (en) 2012-11-08 2012-11-08 Substitute tricyclic benzimidazoles as kinase inhibitors
PCT/EP2013/073311 WO2014072435A1 (en) 2012-11-08 2013-11-07 Substituted tricyclic benzimidazoles as kinase inhibitors

Publications (1)

Publication Number Publication Date
CY1119084T1 true CY1119084T1 (el) 2018-01-10

Family

ID=47470315

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20171100592T CY1119084T1 (el) 2012-11-08 2017-06-06 Υποκατεστημενα τρικυκλικα βενζιμιδαζολια ως αναστολεις κινασης

Country Status (23)

Country Link
US (1) US9745299B2 (el)
EP (1) EP2917217B1 (el)
JP (1) JP6101812B2 (el)
KR (1) KR101812390B1 (el)
CN (1) CN104903321B (el)
AU (1) AU2013343550B2 (el)
BR (1) BR112015010019B1 (el)
CA (1) CA2890643C (el)
CY (1) CY1119084T1 (el)
DK (1) DK2917217T3 (el)
ES (1) ES2628046T3 (el)
GB (1) GB201220157D0 (el)
HR (1) HRP20170802T1 (el)
HU (1) HUE033485T2 (el)
IL (1) IL238693A0 (el)
LT (1) LT2917217T (el)
MX (1) MX363609B (el)
PL (1) PL2917217T3 (el)
PT (1) PT2917217T (el)
RS (1) RS56056B1 (el)
SI (1) SI2917217T1 (el)
SM (1) SMT201700291T1 (el)
WO (1) WO2014072435A1 (el)

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WO2015159937A1 (ja) 2014-04-18 2015-10-22 武田薬品工業株式会社 縮合複素環化合物
CN108348509A (zh) * 2015-11-03 2018-07-31 Lu许可公司 用于治疗增殖减少性病症的化合物
EP3575297B1 (en) 2017-01-30 2024-12-18 Kyoto University Novel compound, and method for producing regulatory t cells
JPWO2018159805A1 (ja) * 2017-03-03 2020-01-09 国立大学法人京都大学 膵前駆細胞の製造方法
AU2018249154A1 (en) 2017-04-03 2019-11-21 Kyoto Pharmaceutical Industries, Ltd. Novel cyclin-dependent kinase 8 and/or 19 inhibitor
US11261184B2 (en) 2017-10-02 2022-03-01 Boehringer Ingelheim International Gmbh [1,6]naphthyridine compounds and derivatives as CDK8/CDK19 inhibitors
CN112552314B (zh) * 2018-08-24 2022-03-04 杭州阿诺生物医药科技有限公司 Sting激动剂小分子抗肿瘤化合物及其应用
JP2022511540A (ja) * 2018-12-14 2022-01-31 ジエンス ヘンルイ メデイシンカンパニー リミテッド Stingアゴニストとしての三環式化合物、ならびにその調製方法および医薬用途
CA3156828A1 (en) * 2019-10-03 2021-04-08 Dana-Farber Cancer Institute, Inc. Tricyclic kinase inhibitors and uses thereof
CN111349094B (zh) * 2020-04-23 2021-02-02 杭州师范大学 一种6H-咪唑[4,5,1-ij]并喹诺酮及其合成方法和应用
CN115996917A (zh) 2020-05-06 2023-04-21 艾捷斯治疗公司 作为jak2抑制剂的6-杂芳基氧基苯并咪唑和氮杂苯并咪唑
EP4249587A4 (en) 2020-11-20 2025-02-19 Orizuru Therapeutics Inc MATURING AGENT
TW202241889A (zh) 2020-12-23 2022-11-01 美商雅捷可斯治療公司 作為jak2抑制劑之6-雜芳基氧基苯并咪唑及氮雜苯并咪唑
CA3208794A1 (en) 2021-02-09 2022-08-18 Orizuru Therapeutics, Inc. Maturation agent
US20240180921A1 (en) * 2021-03-25 2024-06-06 University Of South Carolina Cdk8/19 inhibitors for the treatment of cytokine storm
AU2022349176A1 (en) 2021-09-27 2024-04-11 Kyoto University Method for producing t cell
US12162881B2 (en) 2021-11-09 2024-12-10 Ajax Therapeutics, Inc. Forms and compositions of inhibitors of JAK2
US11970494B2 (en) 2021-11-09 2024-04-30 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors
CA3238860A1 (en) 2021-11-24 2023-06-01 Norihisa MIKAMI Pharmaceutical composition for treating or preventing t cell-related disorders
MX2024006360A (es) 2021-11-24 2024-08-19 Regcell Co Ltd Celula t controlable por inducibilidad humana y metodo para prepararla.
CN119256076A (zh) 2022-03-23 2025-01-03 国立大学法人京都大学 用于产生调节性t细胞的方法
WO2023210578A1 (ja) 2022-04-25 2023-11-02 オリヅルセラピューティクス株式会社 Alk5阻害活性とcdk8/19阻害活性とを有する成熟化剤
WO2023241627A1 (en) * 2022-06-15 2023-12-21 Insilico Medicine Ip Limited Cdk8/19 dual inhibitors and methods of use thereof
CN119546748A (zh) 2022-07-14 2025-02-28 千纸鹤治疗公司 细胞移植用纤维蛋白凝胶片

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BRPI0616722A2 (pt) * 2005-09-30 2012-12-25 Astrazeneca Ab composto ou um sal farmaceuticamente aceitÁvel ou um Éster hidrolisÁvel in vivo do mesmo, processo para preparar o mesmo, composiÇço farmacÊutica, uso de um composto ou um sal farmaceuticamente aceitÁvel ou um Éster hidrolisÁvel in vivo do mesmo, e, mÉtodos para produzir um efeito anti-proliferaÇço celular e um efeito inibidor cdk2, para tratar cÂncer, e para tratar doenÇas
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Also Published As

Publication number Publication date
DK2917217T3 (en) 2017-06-19
AU2013343550A1 (en) 2015-05-14
CN104903321A (zh) 2015-09-09
JP2016503408A (ja) 2016-02-04
RS56056B1 (sr) 2017-09-29
AU2013343550B2 (en) 2016-09-22
EP2917217A1 (en) 2015-09-16
CA2890643A1 (en) 2014-05-15
KR101812390B1 (ko) 2017-12-26
HRP20170802T1 (hr) 2017-08-11
US9745299B2 (en) 2017-08-29
PL2917217T3 (pl) 2017-10-31
SMT201700291T1 (it) 2017-07-18
WO2014072435A1 (en) 2014-05-15
US20150274726A1 (en) 2015-10-01
HUE033485T2 (en) 2017-12-28
KR20150091074A (ko) 2015-08-07
MX363609B (es) 2019-03-28
PT2917217T (pt) 2017-06-07
BR112015010019A2 (pt) 2017-07-11
MX2015005772A (es) 2015-11-18
CA2890643C (en) 2018-05-22
LT2917217T (lt) 2017-07-25
JP6101812B2 (ja) 2017-03-22
BR112015010019A8 (pt) 2019-09-17
IL238693A0 (en) 2015-06-30
GB201220157D0 (en) 2012-12-26
SI2917217T1 (sl) 2017-08-31
CN104903321B (zh) 2017-10-24
ES2628046T3 (es) 2017-08-01
EP2917217B1 (en) 2017-03-08
BR112015010019B1 (pt) 2022-08-09

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