BR112015010019A2 - benzimidazóis tricíclicos substituídos - Google Patents

benzimidazóis tricíclicos substituídos

Info

Publication number
BR112015010019A2
BR112015010019A2 BR112015010019A BR112015010019A BR112015010019A2 BR 112015010019 A2 BR112015010019 A2 BR 112015010019A2 BR 112015010019 A BR112015010019 A BR 112015010019A BR 112015010019 A BR112015010019 A BR 112015010019A BR 112015010019 A2 BR112015010019 A2 BR 112015010019A2
Authority
BR
Brazil
Prior art keywords
compounds
substituted tricyclic
benzimidazoles
diseases
kinase
Prior art date
Application number
BR112015010019A
Other languages
English (en)
Other versions
BR112015010019A8 (pt
BR112015010019B1 (pt
Inventor
Zarebski Adrian
Dreas Agnieszka
Fogt Joanna
Osowska Karolina
Kucwaj Katarzyna
Wiklik Katarzyna
Brzózka Krzysztof
Cholody Marek
Milik Mariusz
Galezowski Michal
Horvath Raymond
Rzymski Tomasz
Czardybon Wojciech
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 BR112015010019A2 publication Critical patent/BR112015010019A2/pt
Publication of BR112015010019A8 publication Critical patent/BR112015010019A8/pt
Publication of BR112015010019B1 publication Critical patent/BR112015010019B1/pt

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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)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (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)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Emergency Medicine (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Oncology (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

abstract disclosed are substituted tricyclic benzimidazoles compounds as defined herein in formula (i) or pharmaceutically acceptable salts thereof. the compounds of the invention selectively inhibit cdk8 and are therefore useful for treating diseases related to this kinase, especially colorectal and melanoma cancers and other solid and hemathological malignancies, autoimmune diseases and inflammatory diseases. also disclosed are processes for preparing these compounds. tradução do resumo resumo: patente de invenção para "benzimidazóis tricíclicos substituídos" descritos são os compostos de benzimidazóis tricíclicos substituídos como definido aqui na fórmula (i) ou sais farmaceuticamente aceitáveis dos mesmos. os compostos da invenção seletivamente inibem cdk8 e são, portanto, úteis para tratar doenças relacionadas a esta cinase, especialmente cânceres colorretal e melanoma e outras malignidades sólidas e hematológicas, doenças autoimunes e doenças inflamatórias. da mesma forma descritos são os processos para preparar estes compostos.
BR112015010019-8A 2012-11-08 2013-11-07 Benzimidazóis tricíclicos substituídos, seus usos, e composição farmacêutica BR112015010019B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1220157.0 2012-11-08
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 (3)

Publication Number Publication Date
BR112015010019A2 true BR112015010019A2 (pt) 2017-07-11
BR112015010019A8 BR112015010019A8 (pt) 2019-09-17
BR112015010019B1 BR112015010019B1 (pt) 2022-08-09

Family

ID=47470315

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112015010019-8A BR112015010019B1 (pt) 2012-11-08 2013-11-07 Benzimidazóis tricíclicos substituídos, seus usos, e composição farmacêutica

Country Status (22)

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

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Publication number Priority date Publication date Assignee Title
EP3133075B1 (en) 2014-04-18 2020-12-30 Takeda Pharmaceutical Company Limited Fused heterocyclic compound
BR112018008931A8 (pt) 2015-11-03 2019-02-26 Lu License Ab ?compostos para tratamento de distúrbios hipoproliferativos?
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 FOR PRODUCING PANCREATIC ANALYZER CELLS
EP3607944A4 (en) * 2017-04-03 2020-11-18 Kyoto Pharmaceutical Industries, Ltd. NEW INHIBITOR OF THE CYCLINE-DEPENDENT KINASE 8 AND / OR 19
US11261184B2 (en) 2017-10-02 2022-03-01 Boehringer Ingelheim International Gmbh [1,6]naphthyridine compounds and derivatives as CDK8/CDK19 inhibitors
WO2020038387A1 (zh) * 2018-08-24 2020-02-27 杭州阿诺生物医药科技有限公司 高活性sting蛋白激动剂
EP3873896A4 (en) * 2018-12-14 2022-08-31 Jiangsu Hengrui Medicine Co., Ltd. TRICYCLIC COMPOUNDS AS STING AGONISTS AND METHODS OF MANUFACTURE AND MEDICAL USES THEREOF
EP4041236A4 (en) * 2019-10-03 2023-10-25 Dana-Farber Cancer Institute, Inc. TRICYCLIC KINASE INHIBITORS AND THEIR USES
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
TW202204350A (zh) 2020-05-06 2022-02-01 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
CN116391028A (zh) 2020-11-20 2023-07-04 千纸鹤治疗公司 促熟剂
KR20230145101A (ko) 2021-02-09 2023-10-17 오리즈루 세라퓨틱스 가부시키가이샤 성숙화제
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
US11970494B2 (en) 2021-11-09 2024-04-30 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors
WO2023241627A1 (en) * 2022-06-15 2023-12-21 Insilico Medicine Ip Limited Cdk8/19 dual inhibitors and methods of use thereof

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JP2899757B2 (ja) 1989-06-26 1999-06-02 持田製薬株式会社 ジヒドロイミダゾキノリノンオキシムスルホン酸誘導体
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WO2003104233A1 (en) * 2002-06-07 2003-12-18 Altana Pharma Ag 4,5-dihydro-imidazo (4,5,1-ij) quinolin-6-ones derivatives and their use as poly (adp-ribosyl) transferase (parp) inhibitors
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KR20080049130A (ko) * 2005-09-30 2008-06-03 아스트라제네카 아베 세포 증식 억제 활성을 갖는 이미다조 [1,2-ａ] 피리딘
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MX2013008822A (es) * 2011-02-09 2013-10-07 Hoffmann La Roche Compuestos heterociclicos como inhibidores de cinasa fosfatidilinositol-3 (pi3).

Also Published As

Publication number Publication date
US9745299B2 (en) 2017-08-29
SI2917217T1 (sl) 2017-08-31
BR112015010019A8 (pt) 2019-09-17
HUE033485T2 (en) 2017-12-28
KR20150091074A (ko) 2015-08-07
CY1119084T1 (el) 2018-01-10
MX363609B (es) 2019-03-28
CN104903321B (zh) 2017-10-24
JP6101812B2 (ja) 2017-03-22
AU2013343550B2 (en) 2016-09-22
IL238693A0 (en) 2015-06-30
MX2015005772A (es) 2015-11-18
LT2917217T (lt) 2017-07-25
BR112015010019B1 (pt) 2022-08-09
EP2917217A1 (en) 2015-09-16
PT2917217T (pt) 2017-06-07
AU2013343550A1 (en) 2015-05-14
KR101812390B1 (ko) 2017-12-26
US20150274726A1 (en) 2015-10-01
PL2917217T3 (pl) 2017-10-31
CA2890643C (en) 2018-05-22
GB201220157D0 (en) 2012-12-26
JP2016503408A (ja) 2016-02-04
EP2917217B1 (en) 2017-03-08
CA2890643A1 (en) 2014-05-15
WO2014072435A1 (en) 2014-05-15
ES2628046T3 (es) 2017-08-01
CN104903321A (zh) 2015-09-09
HRP20170802T1 (hr) 2017-08-11
RS56056B1 (sr) 2017-09-29
DK2917217T3 (en) 2017-06-19

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
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