EA201992418A1 - Бициклические соединения и их применение в лечении рака - Google Patents

Бициклические соединения и их применение в лечении рака

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Publication number
EA201992418A1
EA201992418A1 EA201992418A EA201992418A EA201992418A1 EA 201992418 A1 EA201992418 A1 EA 201992418A1 EA 201992418 A EA201992418 A EA 201992418A EA 201992418 A EA201992418 A EA 201992418A EA 201992418 A1 EA201992418 A1 EA 201992418A1
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Prior art keywords
cancer
cell carcinoma
treatment
solvates
useful
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EA201992418A
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English (en)
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EA038381B1 (ru
Inventor
Ялда Браво
Джэйсон Дэвид Бёрч
Остин Чих-Ю Чэнь
Джо Фред Нагамизо
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Темпест Терапьютикс, Инк.
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Application filed by Темпест Терапьютикс, Инк. filed Critical Темпест Терапьютикс, Инк.
Publication of EA201992418A1 publication Critical patent/EA201992418A1/ru
Publication of EA038381B1 publication Critical patent/EA038381B1/ru

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/08Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
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    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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    • A61K31/00Medicinal preparations containing organic active ingredients
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    • 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
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    • 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
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  • Nitrogen Condensed Heterocyclic Rings (AREA)
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  • Indole Compounds (AREA)

Abstract

Настоящее изобретение относится к новым соединениям формулы I и их фармацевтически приемлемым солям, сольватам, сольватам соли и пролекарствам, применимым в профилактике (например, замедление возникновения или снижение риска развития) и лечении (например, контроль, облегчение или замедление прогрессирования) рака, включая в себя следующее: глиобластома, рак костей, рак головы и шеи, меланома, базальноклеточная карцинома, плоскоклеточная карцинома, аденокарцинома, рак ротовой полости, рак пищевода, рак желудка, рак кишечника, рак толстой кишки, рак мочевого пузыря, печеночноклеточная карцинома, почечноклеточная карцинома, рак поджелудочной железы, рак яичника, рак шейки матки, рак легких, рак молочной железы и рак предстательной железы. Соединения согласно настоящему раскрытию представляют собой селективные антагонисты рецептора ЕР4 и они являются применимыми при лечении различных заболеваний, интенсивность которых можно уменьшить путем блокады опосредованной PGE2 передачи сигналов.
EA201992418A 2017-04-18 2018-04-17 Бициклические соединения и их применение в лечении рака EA038381B1 (ru)

Applications Claiming Priority (2)

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US201762486765P 2017-04-18 2017-04-18
PCT/US2018/028034 WO2018195123A1 (en) 2017-04-18 2018-04-17 Bicyclic compounds and their use in the treatment of cancer

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EA201992418A1 true EA201992418A1 (ru) 2020-04-10
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US (2) US11738009B2 (ru)
EP (1) EP3612517B1 (ru)
JP (1) JP7264060B2 (ru)
KR (1) KR102588955B1 (ru)
CN (1) CN110891935B (ru)
AU (1) AU2018255300B2 (ru)
BR (1) BR112019021790A2 (ru)
CA (1) CA3060554A1 (ru)
DK (1) DK3612517T3 (ru)
EA (1) EA038381B1 (ru)
ES (1) ES2914311T3 (ru)
IL (1) IL270021B (ru)
SG (1) SG11201909730PA (ru)
WO (1) WO2018195123A1 (ru)

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BR112019021790A2 (pt) 2020-05-05
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JP2020517616A (ja) 2020-06-18
EP3612517B1 (en) 2022-03-02
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CN110891935A (zh) 2020-03-17
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US11738009B2 (en) 2023-08-29
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US20210387985A1 (en) 2021-12-16
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