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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compound
pharmaceutically acceptable
acceptable salt
alkyl
cancer
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RU2019127038A
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RU2019127038A3 (enExample
RU2019127038A (ru
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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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and 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
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and 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
    • A61K31/435—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
    • A61K31/495—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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/04—Heterocyclic 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • 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

Publications (3)

Publication Number Publication Date
RU2019127038A RU2019127038A (ru) 2021-03-02
RU2019127038A3 RU2019127038A3 (enExample) 2021-03-17
RU2761457C2 true RU2761457C2 (ru) 2021-12-08

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RU2019127038A RU2761457C2 (ru) 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

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

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS62728B1 (sr) * 2015-08-04 2022-01-31 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd Derivat pirazol pirimidina i njegove upotrebe
KR20200130287A (ko) * 2018-02-08 2020-11-18 이슘 리서치 디벨롭먼트 컴퍼니 오브 더 히브루 유니버시티 오브 예루살렘 엘티디. 헤테로아릴 화합물, 이의 약학 조성물 및 이의 치료적 용도
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
WO2022232259A1 (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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WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
BR112014010563B1 (pt) 2011-11-04 2021-01-12 Jasco Pharmaceuticals, LLC compostos inibidores da aminopirimidina quinase
EP3049086A4 (en) 2013-09-27 2017-02-22 Nimbus Iris, Inc. Irak inhibitors and uses thereof
AU2014337044A1 (en) * 2013-10-18 2016-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
LT3221306T (lt) * 2014-11-20 2020-03-10 Merck Patent Gmbh Heteroarilo junginiai, kaip irak inhibitoriai ir jų panaudojimas
WO2016149756A1 (en) * 2015-03-23 2016-09-29 The University Of Melbourne Treatment of respiratory diseases
RS62728B1 (sr) 2015-08-04 2022-01-31 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd Derivat pirazol pirimidina i njegove upotrebe

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

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