MX363609B - Bencimidazoles triciclicos sustituidos como inhibidores de cinasas. - Google Patents

Bencimidazoles triciclicos sustituidos como inhibidores de cinasas.

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Publication number
MX363609B
MX363609B MX2015005772A MX2015005772A MX363609B MX 363609 B MX363609 B MX 363609B MX 2015005772 A MX2015005772 A MX 2015005772A MX 2015005772 A MX2015005772 A MX 2015005772A MX 363609 B MX363609 B MX 363609B
Authority
MX
Mexico
Prior art keywords
substituted tricyclic
compounds
kinase inhibitors
tricyclic benzimidazoles
disclosed
Prior art date
Application number
MX2015005772A
Other languages
English (en)
Other versions
MX2015005772A (es
Inventor
Rzymski Tomasz
Zarebski Adrian
Dreas Agnieszka
Osowska Karolina
Kucwaj Katarzyna
Fogt Joanna
Cholody Marek
Czardybon Wojciech
Horvath Raymond
Wiklik Katarzyna
Milik Mariusz
Brzózka Krzysztof
Galezowski Michal
Original Assignee
Selvita Sa
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 Sa filed Critical Selvita Sa
Publication of MX2015005772A publication Critical patent/MX2015005772A/es
Publication of MX363609B publication Critical patent/MX363609B/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/06—Peri-condensed systems
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/06—Peri-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Transplantation (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

Se dan a conocer compuestos bencimidazoles tricíclicos sustituidos, tal como se definen en este documento en la fórmula (I), o sales farmacéuticamente aceptables de los mismos. Los compuestos de la invención inhiben de manera selectiva a CDK8 y, por lo tanto, son útiles para tratar enfermedades relacionadas con esta cinasa, especialmente cáncer colorrectal y melanoma, y otras malignidades sólidas y hematológicas, enfermedades autoinmunes y enfermedades inflamatorias. También se dan a conocer procesos para preparar estos compuestos.
MX2015005772A 2012-11-08 2013-11-07 Bencimidazoles triciclicos sustituidos como inhibidores de cinasas. MX363609B (es)

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 (2)

Publication Number Publication Date
MX2015005772A MX2015005772A (es) 2015-11-18
MX363609B true MX363609B (es) 2019-03-28

Family

ID=47470315

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2015005772A MX363609B (es) 2012-11-08 2013-11-07 Bencimidazoles triciclicos sustituidos como inhibidores de cinasas.

Country Status (23)

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

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JP6521387B2 (ja) 2014-04-18 2019-05-29 武田薬品工業株式会社 縮合複素環化合物
US11471446B2 (en) 2015-11-03 2022-10-18 Lu License Ab Compounds for treatment of hypoproliferative disorders
JP7142846B2 (ja) 2017-01-30 2022-09-28 国立大学法人京都大学 新規化合物及び制御性ｔ細胞の製造方法
EP3591040A4 (en) * 2017-03-03 2020-11-11 Kyoto University METHOD OF PRODUCTION OF PANCREATIC PROGENITOR CELLS
CA3058880A1 (en) * 2017-04-03 2018-10-11 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
US20240287093A1 (en) * 2018-08-24 2024-08-29 Adlai Nortye Biopharma Co., Ltd. High activity sting protein agonist
US12415816B2 (en) 2018-11-07 2025-09-16 Dana-Farber Cancer Institute, Inc. Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof
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
EP3938340B1 (en) * 2019-03-11 2025-07-09 Collaborative Medicinal Development, LLC Heteroaromatic and heterobicyclic aromatic derivatives for the treatment of ferroptosis-related disorders
US20240360132A9 (en) * 2019-10-03 2024-10-31 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
EP4146639A1 (en) 2020-05-06 2023-03-15 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
CN116391028A (zh) 2020-11-20 2023-07-04 千纸鹤治疗公司 促熟剂
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
CN116829697A (zh) 2021-02-09 2023-09-29 千纸鹤治疗公司 促熟剂
EP4313050A4 (en) * 2021-03-25 2025-02-12 University of South Carolina CDK8/19 INHIBITORS FOR CYTOKINIC STORM TREATMENT
TW202330910A (zh) 2021-09-27 2023-08-01 國立大學法人京都大學 Ｔ細胞的製造方法
WO2023086320A1 (en) 2021-11-09 2023-05-19 Ajax Therapeutics, Inc. Forms and compositions of inhibitors of jak2
JP7782035B2 (ja) 2021-11-09 2025-12-08 エイジャックス セラピューティクス， インコーポレイテッド Ｊａｋ２阻害剤としての６－ヘテロアリールオキシベンゾイミダゾール及びアザベンゾイミダゾール
CN118591619A (zh) 2021-11-24 2024-09-03 雷格细胞股份有限公司 人诱导性调节性t细胞及其制作方法
US20250352578A1 (en) 2021-11-24 2025-11-20 Regcell Co., Ltd. Pharmaceutical composition for treating or preventing t cell-related disorders
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
EP4516894A1 (en) 2022-04-25 2025-03-05 Orizuru Therapeutics, Inc. Maturing agent having both of alk5 inhibitory activity and cdk8/19 inhibitory activity
WO2023241627A1 (en) * 2022-06-15 2023-12-21 Insilico Medicine Ip Limited Cdk8/19 dual inhibitors and methods of use thereof
JPWO2024014497A1 (es) 2022-07-14 2024-01-18
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IL238693A0 (en) 2015-06-30
PL2917217T3 (pl) 2017-10-31
SMT201700291T1 (it) 2017-07-18
ES2628046T3 (es) 2017-08-01
AU2013343550A1 (en) 2015-05-14
AU2013343550B2 (en) 2016-09-22
LT2917217T (lt) 2017-07-25
KR20150091074A (ko) 2015-08-07
CA2890643A1 (en) 2014-05-15
EP2917217A1 (en) 2015-09-16
BR112015010019A2 (pt) 2017-07-11
WO2014072435A1 (en) 2014-05-15
MX2015005772A (es) 2015-11-18
SI2917217T1 (sl) 2017-08-31
US20150274726A1 (en) 2015-10-01
CN104903321B (zh) 2017-10-24
EP2917217B1 (en) 2017-03-08
HRP20170802T1 (hr) 2017-08-11
KR101812390B1 (ko) 2017-12-26
GB201220157D0 (en) 2012-12-26
RS56056B1 (sr) 2017-09-29
HUE033485T2 (en) 2017-12-28
JP2016503408A (ja) 2016-02-04
US9745299B2 (en) 2017-08-29
CY1119084T1 (el) 2018-01-10
CN104903321A (zh) 2015-09-09
PT2917217T (pt) 2017-06-07
CA2890643C (en) 2018-05-22
BR112015010019B1 (pt) 2022-08-09
DK2917217T3 (en) 2017-06-19
JP6101812B2 (ja) 2017-03-22
BR112015010019A8 (pt) 2019-09-17

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