RU2761457C2 - N1-(4-(5-(циклопропилметил)-1-метил-1h-пиразол-4-ил)пиридин-2-ил)циклогексан-1,4-диаминовые производные и родственные соединения в качестве ингибиторов сk1 и/или irak1 для лечения рака - Google Patents

N1-(4-(5-(циклопропилметил)-1-метил-1h-пиразол-4-ил)пиридин-2-ил)циклогексан-1,4-диаминовые производные и родственные соединения в качестве ингибиторов сk1 и/или irak1 для лечения рака Download PDF

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RU2761457C2
RU2761457C2 RU2019127038A RU2019127038A RU2761457C2 RU 2761457 C2 RU2761457 C2 RU 2761457C2 RU 2019127038 A RU2019127038 A RU 2019127038A RU 2019127038 A RU2019127038 A RU 2019127038A RU 2761457 C2 RU2761457 C2 RU 2761457C2
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pharmaceutically acceptable
acceptable salt
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Даньсу ЛИ
Ирит СНИР-АЛКАЛАЙ
Йозеф ВАККА
Йинон БЕН НЕРИАХ
Авантика ВЕНКАТАК-ИАЛАМ
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Йиссум Рисерч Дивелопмент Компани Оф Дзе Хебрю Юниверсити Оф Иерусалим Лтд.
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
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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
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P35/02Antineoplastic agents specific for leukemia
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
RU2019127038A 2017-02-01 2018-01-30 N1-(4-(5-(циклопропилметил)-1-метил-1h-пиразол-4-ил)пиридин-2-ил)циклогексан-1,4-диаминовые производные и родственные соединения в качестве ингибиторов сk1 и/или irak1 для лечения рака RU2761457C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762453192P 2017-02-01 2017-02-01
US62/453,192 2017-02-01
PCT/IL2018/050100 WO2018142393A1 (en) 2017-02-01 2018-01-30 N1 -(4-(5-(cyclopropylmethyl)-1 -methyl-1 h-pyrazol-4-yl)pyridin-2-yl)cyclohexane-1,4-diamine derivatives and related compounds as ck1 and/or iraki inhibitors for treating cancer

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RU2019127038A RU2019127038A (ru) 2021-03-02
RU2019127038A3 RU2019127038A3 (instruction) 2021-03-17
RU2761457C2 true RU2761457C2 (ru) 2021-12-08

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US (2) US11072599B2 (instruction)
EP (1) EP3577108B1 (instruction)
JP (1) JP7142646B2 (instruction)
KR (1) KR20190115017A (instruction)
CN (1) CN110475771B (instruction)
AU (1) AU2018215809B2 (instruction)
CA (1) CA3052247A1 (instruction)
ES (1) ES2902885T3 (instruction)
IL (1) IL268128B2 (instruction)
MX (1) MX394556B (instruction)
NZ (1) NZ755447A (instruction)
RU (1) RU2761457C2 (instruction)
SG (1) SG11201906681PA (instruction)
TW (1) TW201837027A (instruction)
WO (1) WO2018142393A1 (instruction)

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EP3331877B1 (en) * 2015-08-04 2021-09-22 Yissum Research Development Company of the Hebrew University of Jerusalem Ltd. Pyrazole pyrimidine derivative and uses thereof
AU2019219678A1 (en) * 2018-02-08 2020-08-27 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use
CN114127058B (zh) * 2019-07-04 2024-06-25 深圳国顺康医药科技有限公司 一种杂环化合物、其药物组合物及用途
KR20230069169A (ko) * 2020-09-17 2023-05-18 얀센 파마슈티카 엔.브이. 카제인 키나제 1 델타 조절제
CA3215697A1 (en) * 2021-04-28 2022-11-03 Cornell University Soluble adenylyl cyclase (sac) inhibitors and uses thereof

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EP2651405A2 (en) * 2010-12-14 2013-10-23 Electrophoretics Limited Casein kinase 1 (ck1 ) inhibitors
RU2604062C2 (ru) * 2010-07-13 2016-12-10 Ф.Хоффманн-Ля Рош Аг ПРОИЗВОДНЫЕ ПИРАЗОЛО[1,5-a]ПИРИМИДИНА И ТИЕНО[3,2-b]ПИРИМИДИНА В КАЧЕСТВЕ МОДУЛЯТОРОВ IRAK-4

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ES2629690T3 (es) 2011-11-04 2017-08-14 Jasco Pharmaceuticals, LLC Inhibidores de aminopirimidina quinasa
US9518065B2 (en) 2013-09-27 2016-12-13 Nimbus Iris, Inc. IRAK inhibitors and uses thereof
CN105849099B (zh) * 2013-10-18 2020-01-17 达纳-法伯癌症研究所股份有限公司 周期蛋白依赖性激酶7(cdk7)的多环抑制剂
HUE047586T2 (hu) 2014-11-20 2020-04-28 Merck Patent Gmbh Heteroaril vegyületek mint IRAK inhibitorok és alkalmazásaik
CN107847480B (zh) 2015-03-23 2021-06-25 墨尔本大学 呼吸性疾病的治疗
EP3331877B1 (en) * 2015-08-04 2021-09-22 Yissum Research Development Company of the Hebrew University of Jerusalem Ltd. Pyrazole pyrimidine derivative and uses thereof

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RU2604062C2 (ru) * 2010-07-13 2016-12-10 Ф.Хоффманн-Ля Рош Аг ПРОИЗВОДНЫЕ ПИРАЗОЛО[1,5-a]ПИРИМИДИНА И ТИЕНО[3,2-b]ПИРИМИДИНА В КАЧЕСТВЕ МОДУЛЯТОРОВ IRAK-4
EP2651405A2 (en) * 2010-12-14 2013-10-23 Electrophoretics Limited Casein kinase 1 (ck1 ) inhibitors

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Беликов В. Г. "Фармацевтическая химия". Глава 2.6 "Связь между химической структурой, свойствами веществ и их действием на организм". - М.: МЕДпресс-информ, 2007, С. 27-29. Birgit Schittek et al. "Biological functions of casein kinase 1 isoforms and putative roles in tumorigenesis", Molecular Cancer, 2014, Vol.13, P.1-14. https://official.academic.ru/28407/%D0%A4%D0%B0%D1%80%D0%BC%D0%B0%D1%86%D0%B5%D0%B2%D1%82%D0%B8%D1%87%D0%B5%D1%81%D0%BA%D0%B0%D1%8F_%D0%BA%D0%BE%D0%BC%D0%BF%D0%BE%D0%B7%D0%B8%D1%86%D0%B8%D1%8F, Wayback Internet Archive Machine, 04.12.2013. *

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ES2902885T3 (es) 2022-03-30
MX2019009083A (es) 2019-09-10
JP2020505468A (ja) 2020-02-20
AU2018215809A1 (en) 2019-08-15
CA3052247A1 (en) 2018-08-09
EP3577108B1 (en) 2021-10-20
US11072599B2 (en) 2021-07-27
RU2019127038A3 (instruction) 2021-03-17
IL268128B (en) 2022-11-01
US20220017493A1 (en) 2022-01-20
EP3577108A1 (en) 2019-12-11
TW201837027A (zh) 2018-10-16
WO2018142393A1 (en) 2018-08-09
IL268128A (en) 2019-09-26
AU2018215809B2 (en) 2021-12-23
RU2019127038A (ru) 2021-03-02
IL268128B2 (en) 2023-03-01
JP7142646B2 (ja) 2022-09-27
ES2902885T8 (es) 2022-04-06
MX394556B (es) 2025-03-24
CN110475771A (zh) 2019-11-19
SG11201906681PA (en) 2019-08-27
US11999721B2 (en) 2024-06-04
NZ755447A (en) 2023-05-26
KR20190115017A (ko) 2019-10-10
CN110475771B (zh) 2022-09-02
US20200354340A1 (en) 2020-11-12

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