EA201792087A1 - ПРОИЗВОДНЫЕ 7-(МОРФОЛИН-4-ИЛ)ПИРАЗОЛО[1,5-a]ПИРИМИДИНА, ПРИГОДНЫЕ ДЛЯ ЛЕЧЕНИЯ ИММУННЫХ ИЛИ ВОСПАЛИТЕЛЬНЫХ ЗАБОЛЕВАНИЙ ИЛИ РАКА - Google Patents

ПРОИЗВОДНЫЕ 7-(МОРФОЛИН-4-ИЛ)ПИРАЗОЛО[1,5-a]ПИРИМИДИНА, ПРИГОДНЫЕ ДЛЯ ЛЕЧЕНИЯ ИММУННЫХ ИЛИ ВОСПАЛИТЕЛЬНЫХ ЗАБОЛЕВАНИЙ ИЛИ РАКА

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Publication number
EA201792087A1
EA201792087A1 EA201792087A EA201792087A EA201792087A1 EA 201792087 A1 EA201792087 A1 EA 201792087A1 EA 201792087 A EA201792087 A EA 201792087A EA 201792087 A EA201792087 A EA 201792087A EA 201792087 A1 EA201792087 A1 EA 201792087A1
Authority
EA
Eurasian Patent Office
Prior art keywords
cancer
treatment
fragment
inflammatory diseases
immune
Prior art date
Application number
EA201792087A
Other languages
English (en)
Other versions
EA032826B1 (ru
Inventor
Барбара Димек
Марцин Загозда
Мацей Вечорек
Кшиштоф Дубель
Александра Станчак
Даря Здзалик
Павел Гунерка
Марёля Секуляр
Мацей Дзяхан
Original Assignee
Целон Фарма С.А.
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 Целон Фарма С.А. filed Critical Целон Фарма С.А.
Publication of EA201792087A1 publication Critical patent/EA201792087A1/ru
Publication of EA032826B1 publication Critical patent/EA032826B1/ru

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/535—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Соединение общей формулы (I), где Y представляет собой -CH- или >C=O; Rвыбран из группы, состоящей из A1, A2 и A3; Rпредставляет собой диоксотиоморфолиновый фрагмент B1, пиперазинильный фрагмент B2, азетидинильный фрагмент B3 или пиперидинильный фрагмент B4; Rвыбран из группы, состоящей из H, галогена и C-Cалкила; Rвыбран из группы, состоящей из C-Cалкила, C-C-циклоалкила, C-Cалкила, замещенного посредством C-Cалкокси и CHF; и его фармацевтически приемлемые соли. Фармацевтические композиции, содержащие указанные соединения, и их применение для лечения заболеваний иммунной системы, воспалительных заболеваний и рака.
EA201792087A 2015-04-02 2016-03-30 ПРОИЗВОДНЫЕ 7-(МОРФОЛИН-4-ИЛ)ПИРАЗОЛО[1,5-a]ПИРИМИДИНА, ПРИГОДНЫЕ ДЛЯ ЛЕЧЕНИЯ ИММУННЫХ ИЛИ ВОСПАЛИТЕЛЬНЫХ ЗАБОЛЕВАНИЙ ИЛИ РАКА EA032826B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
PL411864A PL236355B1 (pl) 2015-04-02 2015-04-02 Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-α]pirymidyny jako inhibitory kinazy PI3
PCT/IB2016/051792 WO2016157091A1 (en) 2015-04-02 2016-03-30 7-(morpholin-4-yl)pyrazole[1,5-a]pyrimidine derivatives which are useful for the treatment of immune or inflammatory diseases or cancer

Publications (2)

Publication Number Publication Date
EA201792087A1 true EA201792087A1 (ru) 2018-03-30
EA032826B1 EA032826B1 (ru) 2019-07-31

Family

ID=55650626

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201792087A EA032826B1 (ru) 2015-04-02 2016-03-30 ПРОИЗВОДНЫЕ 7-(МОРФОЛИН-4-ИЛ)ПИРАЗОЛО[1,5-a]ПИРИМИДИНА, ПРИГОДНЫЕ ДЛЯ ЛЕЧЕНИЯ ИММУННЫХ ИЛИ ВОСПАЛИТЕЛЬНЫХ ЗАБОЛЕВАНИЙ ИЛИ РАКА

Country Status (18)

Country Link
US (1) US10138247B2 (ru)
EP (1) EP3277687B1 (ru)
JP (1) JP6665201B2 (ru)
KR (1) KR102559190B1 (ru)
CN (1) CN107743489B (ru)
AU (1) AU2016241568B2 (ru)
BR (1) BR112017020131B1 (ru)
CA (1) CA2978828A1 (ru)
DK (1) DK3277687T3 (ru)
EA (1) EA032826B1 (ru)
ES (1) ES2765642T3 (ru)
HR (1) HRP20192195T1 (ru)
HU (1) HUE047822T2 (ru)
MX (1) MX2017011423A (ru)
PL (2) PL236355B1 (ru)
PT (1) PT3277687T (ru)
SI (1) SI3277687T1 (ru)
WO (1) WO2016157091A1 (ru)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11834467B2 (en) 2020-09-28 2023-12-05 1ST Biotherapeutics, Inc. Substituted indazoles as hematopoietic progenitor kinase 1 (HPK1) inhibitors
CN114957261B (zh) * 2022-05-17 2023-06-23 重庆文理学院 一种具有抗头颈癌作用的化合物及其制备方法和应用

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR9707391A (pt) * 1996-02-07 1999-07-20 Janssen Pharmaceutica Nv Pirazolpirimidinas como antagonistas de receptor de crf
WO2005062882A2 (en) 2003-12-23 2005-07-14 Activbiotics, Inc Rifamycin analogs and uses thereof
JP4708438B2 (ja) * 2005-02-11 2011-06-22 エフ．ホフマン−ラ ロシュ アーゲー ｍＧｌｕＲ２アンタゴニストとしてのピラゾロピリミジン誘導体
US8030304B2 (en) * 2006-09-20 2011-10-04 Eli Lilly And Company Thiazole pyrazolopyrimidines CRF1 receptor antagonists
JP5638955B2 (ja) * 2007-10-26 2014-12-10 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｐｉ３キナーゼ阻害剤として有用なプリン誘導体
AU2009218515A1 (en) 2008-02-26 2009-09-03 Novartis Ag Heterocyclic compounds as inhibitors of CXCR2
MX2010012583A (es) * 2008-05-30 2011-02-24 Genentech Inc Compuestos inhibidores de purina pi3k y métodos de uso.
CA2742550A1 (en) * 2008-10-03 2010-04-08 Merck Serono S.A. 4-morpholino-pyrido[3,2-d]pyrimidines
WO2010074284A1 (ja) * 2008-12-26 2010-07-01 味の素株式会社 ピラゾロピリミジン化合物
DK2419429T3 (da) * 2009-04-16 2014-06-23 Ct Nac De Investigaciones Oncológicas Cnio Imidazopyraziner som inhibitorer af proteinkinaser
CA2761445A1 (en) * 2009-05-27 2010-12-02 Genentech, Inc. Bicyclic pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use
WO2010136491A1 (en) * 2009-05-27 2010-12-02 F. Hoffmann-La Roche Ag Bicyclic indole-pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use
GB0912745D0 (en) 2009-07-22 2009-08-26 Wolfson Microelectronics Plc Improvements relating to DC-DC converters
CA2786294A1 (en) 2010-02-22 2011-08-25 F. Hoffmann-La Roche Ag Pyrido[3,2-d]pyrimidine pi3k delta inhibitor compounds and methods of use
BR112012021656A2 (pt) 2010-03-04 2017-02-07 Merck Sharp & Dohme composto, uso do mesmo, e, composição farmacêutica
WO2013028263A1 (en) * 2011-08-24 2013-02-28 Glaxosmithkline Llc Pyrazolopyrimidine derivatives as pi3 kinase inhibitors

Also Published As

Publication number Publication date
BR112017020131B1 (pt) 2023-02-28
US10138247B2 (en) 2018-11-27
US20180111939A1 (en) 2018-04-26
KR102559190B1 (ko) 2023-07-25
PT3277687T (pt) 2020-01-10
BR112017020131A2 (pt) 2018-05-29
PL3277687T3 (pl) 2020-09-21
CN107743489A (zh) 2018-02-27
EP3277687A1 (en) 2018-02-07
MX2017011423A (es) 2018-05-17
EA032826B1 (ru) 2019-07-31
EP3277687B1 (en) 2019-10-30
PL411864A1 (pl) 2016-10-10
AU2016241568B2 (en) 2019-09-26
DK3277687T3 (da) 2019-12-16
SI3277687T1 (sl) 2020-02-28
CA2978828A1 (en) 2016-10-06
WO2016157091A1 (en) 2016-10-06
AU2016241568A1 (en) 2017-10-19
JP6665201B2 (ja) 2020-03-13
HRP20192195T1 (hr) 2020-03-06
ES2765642T3 (es) 2020-06-10
JP2018510192A (ja) 2018-04-12
CN107743489B (zh) 2021-05-04
KR20170132275A (ko) 2017-12-01
HUE047822T2 (hu) 2020-05-28
PL236355B1 (pl) 2021-01-11

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