ITUA20164278A1 - COMPOSTI 2-OXO-1,2-DIIDROPIRIDIN-3-CARBOSSAMMIDE E LORO USO COME INIBITORI DUALI DI PDK1/AurA - Google Patents

COMPOSTI 2-OXO-1,2-DIIDROPIRIDIN-3-CARBOSSAMMIDE E LORO USO COME INIBITORI DUALI DI PDK1/AurA

Info

Publication number
ITUA20164278A1
ITUA20164278A1 ITUA2016A004278A ITUA20164278A ITUA20164278A1 IT UA20164278 A1 ITUA20164278 A1 IT UA20164278A1 IT UA2016A004278 A ITUA2016A004278 A IT UA2016A004278A IT UA20164278 A ITUA20164278 A IT UA20164278A IT UA20164278 A1 ITUA20164278 A1 IT UA20164278A1
Authority
IT
Italy
Prior art keywords
carbossamide
pdk1
dihydropyridin
aura
oxo
Prior art date
Application number
ITUA2016A004278A
Other languages
English (en)
Inventor
Simona Sestito
Simona Daniele
Claudia Martini
Simona Raposelli
Guido Puricelli
Original Assignee
International Soc For Drug Development S R L
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 International Soc For Drug Development S R L filed Critical International Soc For Drug Development S R L
Priority to ITUA2016A004278A priority Critical patent/ITUA20164278A1/it
Priority to EP17734646.7A priority patent/EP3468556A1/en
Priority to US16/308,690 priority patent/US20190160049A1/en
Priority to JP2019517158A priority patent/JP2019517595A/ja
Priority to PCT/EP2017/063950 priority patent/WO2017211946A1/en
Priority to RU2018145969A priority patent/RU2018145969A/ru
Publication of ITUA20164278A1 publication Critical patent/ITUA20164278A1/it

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
    • A61K31/435—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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
ITUA2016A004278A 2016-06-10 2016-06-10 COMPOSTI 2-OXO-1,2-DIIDROPIRIDIN-3-CARBOSSAMMIDE E LORO USO COME INIBITORI DUALI DI PDK1/AurA ITUA20164278A1 (it)

Priority Applications (6)

Application Number Priority Date Filing Date Title
ITUA2016A004278A ITUA20164278A1 (it) 2016-06-10 2016-06-10 COMPOSTI 2-OXO-1,2-DIIDROPIRIDIN-3-CARBOSSAMMIDE E LORO USO COME INIBITORI DUALI DI PDK1/AurA
EP17734646.7A EP3468556A1 (en) 2016-06-10 2017-06-08 2-oxo-1,2-dihydropyridine-3-carboxamide compounds and their use as dual inhibitors of pdk1/aura
US16/308,690 US20190160049A1 (en) 2016-06-10 2017-06-08 2-oxo-1,2-dihydropyridine-3-carboxamide compounds and their use as dual inhibitors of pdk1/aura
JP2019517158A JP2019517595A (ja) 2016-06-10 2017-06-08 ２−オキソ−１，２−ジヒドロピリジン−３−カルボキサミド化合物及びＰＤＫ１／ＡｕｒＡの二重阻害剤としてのそれらの使用
PCT/EP2017/063950 WO2017211946A1 (en) 2016-06-10 2017-06-08 2-oxo-1,2-dihydropyridine-3-carboxamide compounds and their use as dual inhibitors of pdk1/aura
RU2018145969A RU2018145969A (ru) 2016-06-10 2017-06-08 2-ОКСО-1,2-ДИГИДРОПИРИДИН-3-КАРБОКСАМИДНЫЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ДВОЙНЫХ ИНГИБИТОРОВ PDK1/AurA

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
ITUA2016A004278A ITUA20164278A1 (it) 2016-06-10 2016-06-10 COMPOSTI 2-OXO-1,2-DIIDROPIRIDIN-3-CARBOSSAMMIDE E LORO USO COME INIBITORI DUALI DI PDK1/AurA

Publications (1)

Publication Number Publication Date
ITUA20164278A1 true ITUA20164278A1 (it) 2017-12-10

Family

ID=57133316

Family Applications (1)

Application Number Title Priority Date Filing Date
ITUA2016A004278A ITUA20164278A1 (it) 2016-06-10 2016-06-10 COMPOSTI 2-OXO-1,2-DIIDROPIRIDIN-3-CARBOSSAMMIDE E LORO USO COME INIBITORI DUALI DI PDK1/AurA

Country Status (6)

Country Link
US (1) US20190160049A1 (it)
EP (1) EP3468556A1 (it)
JP (1) JP2019517595A (it)
IT (1) ITUA20164278A1 (it)
RU (1) RU2018145969A (it)
WO (1) WO2017211946A1 (it)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010017047A1 (en) * 2008-08-05 2010-02-11 Merck & Co., Inc. Therapeutic compounds
WO2012036974A1 (en) * 2010-09-14 2012-03-22 Schering Corporation Novel thiazol-carboximide derivatives as pdk1 inhibitors
WO2016198597A1 (en) * 2015-06-11 2016-12-15 International Society For Drug Development S.R.L. 2-oxo-1,2-dihydropyridine-3-carboxamide compounds and their use as inhibitors of pdk1

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101541783B (zh) * 2006-06-30 2014-10-01 苏尼西斯制药有限公司 吡啶酮基pdk1抑制剂

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010017047A1 (en) * 2008-08-05 2010-02-11 Merck & Co., Inc. Therapeutic compounds
WO2012036974A1 (en) * 2010-09-14 2012-03-22 Schering Corporation Novel thiazol-carboximide derivatives as pdk1 inhibitors
WO2016198597A1 (en) * 2015-06-11 2016-12-15 International Society For Drug Development S.R.L. 2-oxo-1,2-dihydropyridine-3-carboxamide compounds and their use as inhibitors of pdk1

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
BAI LI-YUAN ET AL: "BX795, a TBK1 inhibitor, exhibits antitumor activity in human oral squamous cell carcinoma through apoptosis induction and mitotic phase arrest", EUROPEAN JOURNAL OF PHARMACOLOGY, vol. 769, 27 November 2015 (2015-11-27), pages 287 - 296, XP029334499, ISSN: 0014-2999, DOI: 10.1016/J.EJPHAR.2015.11.032 *
M. MAURER ET AL: "3-Phosphoinositide-Dependent Kinase 1 Potentiates Upstream Lesions on the Phosphatidylinositol 3-Kinase Pathway in Breast Carcinoma", CANCER RESEARCH, vol. 69, no. 15, 1 August 2009 (2009-08-01), pages 6299 - 6306, XP055338140, ISSN: 0008-5472, DOI: 10.1158/0008-5472.CAN-09-0820 *
SEAN T. MURPHY ET AL: "Discovery of Novel, Potent, and Selective Inhibitors of 3-Phosphoinositide-Dependent Kinase (PDK1)", JOURNAL OF MEDICINAL CHEMISTRY, vol. 54, no. 24, 22 December 2011 (2011-12-22), US, pages 8490 - 8500, XP055338366, ISSN: 0022-2623, DOI: 10.1021/jm201019k *
SESTITO SIMONA ET AL: "Locking PDK1 in DFG-out conformation through 2-oxo-indole containing molecules: Another tools to fight glioblastoma", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, EDITIONS SCIENTIFIQUE ELSEVIER, PARIS, FR, vol. 118, 20 April 2016 (2016-04-20), pages 47 - 63, XP029562541, ISSN: 0223-5234, DOI: 10.1016/J.EJMECH.2016.04.003 *
SILVA ANDRES ET AL: "Aurora kinase A is a possible target of OSU-03012 to destabilize MYC family proteins.", ONCOLOGY REPORTS SEP 2014, vol. 32, no. 3, September 2014 (2014-09-01), pages 901 - 905, XP002766290, ISSN: 1791-2431 *
SIMONA DANIELE ET AL: "Dual Inhibition of PDK1 and Aurora Kinase A: An Effective Strategy to Induce Differentiation and Apoptosis of Human Glioblastoma Multiforme Stem Cells", ACS CHEMICAL NEUROSCIENCE, vol. 8, no. 1, 18 January 2017 (2017-01-18), US, pages 100 - 114, XP055338363, ISSN: 1948-7193, DOI: 10.1021/acschemneuro.6b00251 *

Also Published As

Publication number Publication date
RU2018145969A3 (it) 2020-11-06
JP2019517595A (ja) 2019-06-24
WO2017211946A1 (en) 2017-12-14
EP3468556A1 (en) 2019-04-17
US20190160049A1 (en) 2019-05-30
RU2018145969A (ru) 2020-06-25

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