EA201491260A1 - Соединения и композиции для ингибирования взаимодействия bcl2 с партнерами по связыванию - Google Patents

Соединения и композиции для ингибирования взаимодействия bcl2 с партнерами по связыванию

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Publication number
EA201491260A1
EA201491260A1 EA201491260A EA201491260A EA201491260A1 EA 201491260 A1 EA201491260 A1 EA 201491260A1 EA 201491260 A EA201491260 A EA 201491260A EA 201491260 A EA201491260 A EA 201491260A EA 201491260 A1 EA201491260 A1 EA 201491260A1
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EA
Eurasian Patent Office
Prior art keywords
compounds
interaction
bcl2
partners
linkage
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EA201491260A
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English (en)
Inventor
Дэниэл Форд
Джон Роберт Портер
Майкл Скотт Виссер
Наим Юсуфф
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Новартис Аг
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Publication of EA201491260A1 publication Critical patent/EA201491260A1/ru

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    • 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
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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    • 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
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    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • 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
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    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Изобретение относится к соединениям формулы (I)в которой R, R, Rи Rимеют значения, определенные в описании изобретения. Соединения формулы (I) способны нарушать взаимодействия BCL-2 с белками, содержащими домен ВН3. Нарушение данного взаимодействия может восстановить антиапоптозную функцию BCL-2 в раковых клетках и опухолевой ткани, экспрессирующих BCL-2. Изобретение также относится к способу получения соединений по изобретению, фармацевтическим препаратам, содержащим такие соединения, и способам применения таких соединений в лечении раковых заболеваний.
EA201491260A 2011-12-23 2012-12-12 Соединения и композиции для ингибирования взаимодействия bcl2 с партнерами по связыванию EA201491260A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161579715P 2011-12-23 2011-12-23
PCT/US2012/069273 WO2013096060A1 (en) 2011-12-23 2012-12-12 Compounds for inhibiting the interaction of bcl2 with binding partners

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EA201491260A1 true EA201491260A1 (ru) 2014-11-28

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EA201491260A EA201491260A1 (ru) 2011-12-23 2012-12-12 Соединения и композиции для ингибирования взаимодействия bcl2 с партнерами по связыванию

Country Status (11)

Country Link
US (1) US20140357633A1 (ru)
EP (1) EP2794592A1 (ru)
JP (1) JP2015503519A (ru)
KR (1) KR20140107574A (ru)
CN (1) CN104125953A (ru)
AU (1) AU2012355624A1 (ru)
BR (1) BR112014015339A2 (ru)
CA (1) CA2859876A1 (ru)
EA (1) EA201491260A1 (ru)
MX (1) MX2014007731A (ru)
WO (1) WO2013096060A1 (ru)

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AU2012355624A1 (en) 2014-07-17
MX2014007731A (es) 2015-01-12
BR112014015339A8 (pt) 2017-06-13
BR112014015339A2 (pt) 2017-06-13
CN104125953A (zh) 2014-10-29
CA2859876A1 (en) 2013-06-27
US20140357633A1 (en) 2014-12-04
JP2015503519A (ja) 2015-02-02
WO2013096060A1 (en) 2013-06-27
EP2794592A1 (en) 2014-10-29

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