EA201692003A1 - Макроциклические производные пиримидина - Google Patents

Макроциклические производные пиримидина

Info

Publication number
EA201692003A1
EA201692003A1 EA201692003A EA201692003A EA201692003A1 EA 201692003 A1 EA201692003 A1 EA 201692003A1 EA 201692003 A EA201692003 A EA 201692003A EA 201692003 A EA201692003 A EA 201692003A EA 201692003 A1 EA201692003 A1 EA 201692003A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
present
pyrimidine
inhibitory activity
relates
Prior art date
Application number
EA201692003A
Other languages
English (en)
Other versions
EA031246B1 (ru
Inventor
Гастон Станислас Марселла Дилс
Брюно Схунтьес
Маттиас Люк Эме Версель
Дидье Жан-Клод Бертело
Марк Виллемс
Марсель Вьейевуа
Вернер Констант Йохан Эмбрехтс
Бертольд Вробловски
Ливен Мерпул
Original Assignee
Янссен Фармацевтика Нв
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 Янссен Фармацевтика Нв filed Critical Янссен Фармацевтика Нв
Publication of EA201692003A1 publication Critical patent/EA201692003A1/ru
Publication of EA031246B1 publication Critical patent/EA031246B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed systems contains four or more hetero 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
    • A61K31/495—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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/582—Recycling of unreacted starting or intermediate materials

Abstract

Настоящее изобретение относится к замещенным макроциклическим производным пиримидина формулы (I)где переменные имеют значение, определенное в формуле изобретения. Соединения в соответствии с настоящим изобретением обладают EF2K-ингибирующей активностью и необязательно также Vps34-ингибирующей активностью. Настоящее изобретение, кроме того, относится к способам получения таких новых соединений, к фармацевтическим композициям, содержащим указанные соединения в качестве активного ингредиента, а также к применению указанных соединений в качестве лекарственного препарата.
EA201692003A 2014-04-03 2015-04-02 Макроциклические производные пиримидина EA031246B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14163443 2014-04-03
EP14183747 2014-09-05
PCT/EP2015/057399 WO2015150555A1 (en) 2014-04-03 2015-04-02 Macrocylic pyrimidine derivatives

Publications (2)

Publication Number Publication Date
EA201692003A1 true EA201692003A1 (ru) 2017-06-30
EA031246B1 EA031246B1 (ru) 2018-12-28

Family

ID=52781117

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201692003A EA031246B1 (ru) 2014-04-03 2015-04-02 Макроциклические производные пиримидина

Country Status (21)

Country Link
US (1) US10017509B2 (ru)
EP (1) EP3126364B1 (ru)
JP (1) JP6529513B2 (ru)
KR (1) KR102390276B1 (ru)
CN (2) CN106164075B (ru)
AU (1) AU2015239098B2 (ru)
BR (1) BR112016021982B1 (ru)
CA (1) CA2942636C (ru)
CL (1) CL2016002461A1 (ru)
EA (1) EA031246B1 (ru)
ES (1) ES2667723T3 (ru)
IL (1) IL248005B (ru)
MA (1) MA39822A (ru)
MX (1) MX369798B (ru)
MY (1) MY185491A (ru)
NZ (1) NZ725399A (ru)
PE (1) PE20161362A1 (ru)
PH (1) PH12016501963B1 (ru)
SG (1) SG11201608240RA (ru)
UA (1) UA118219C2 (ru)
WO (1) WO2015150555A1 (ru)

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RS60900B1 (sr) 2016-02-19 2020-11-30 Sprint Bioscience Ab Jedinjenja 6-heterociklil-4-morfolin-4-ilpiridin-2-ona korisna za lečenje kancera i dijabetesa
HUE050863T2 (hu) 2016-02-19 2021-01-28 Sprint Bioscience Ab Rák és cukorbetegség kezelésére alkalmazható 6-aril-4-(morfolin-4-il)-1H-piridin-2-on vegyületek
PL3601253T3 (pl) 2017-03-28 2022-01-17 Bayer Aktiengesellschaft Nowe hamujące ptefb związki makrocykliczne
US11242356B2 (en) 2017-03-28 2022-02-08 Bayer Aktiengesellschaft PTEFb inhibiting macrocyclic compounds
CA3073142A1 (en) 2017-08-23 2019-02-28 Sprint Bioscience Ab Morpholinylpyridone compounds
US11208423B2 (en) 2017-08-23 2021-12-28 Sprint Bioscience Ab Pyridinamine-pyridone and pyrimidinamine- pyridone compounds
JP7199738B2 (ja) 2017-08-23 2023-01-06 スプリント バイオサイエンス アクティエボラーグ アザインドリルピリドンおよびジアザインドリルピリドン化合物
ES2910839T3 (es) 2017-08-23 2022-05-13 Sprint Bioscience Ab Compuestos de piridilpiridona
CN115551868A (zh) * 2020-02-18 2022-12-30 特修斯制药公司 大环化合物和其用途
CN113735856A (zh) * 2020-05-29 2021-12-03 百极弘烨(南通)医药科技有限公司 大环jak抑制剂及其应用
WO2023046030A1 (zh) * 2021-09-23 2023-03-30 河南晟翔医药科技有限公司 一种egfr小分子抑制剂、含其的药物组合物及其用途
KR102613509B1 (ko) * 2021-12-15 2023-12-13 환인제약 주식회사 마크로사이클릭 피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 신경 퇴행성 질환의 예방 또는 치료용 약학적 조성물
WO2024078263A1 (zh) * 2022-10-09 2024-04-18 药雅科技(上海)有限公司 大环杂环类化合物作为egfr抑制剂的制备及其应用

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Also Published As

Publication number Publication date
PH12016501963A1 (en) 2017-01-09
CN106164075B (zh) 2021-11-26
ES2667723T3 (es) 2018-05-14
AU2015239098B2 (en) 2019-08-01
AU2015239098A1 (en) 2016-09-29
KR20160142316A (ko) 2016-12-12
EA031246B1 (ru) 2018-12-28
KR102390276B1 (ko) 2022-04-22
MA39822A (fr) 2018-02-06
PE20161362A1 (es) 2016-12-17
IL248005B (en) 2018-12-31
CA2942636A1 (en) 2015-10-08
MX369798B (es) 2019-11-21
MX2016012992A (es) 2016-12-07
JP6529513B2 (ja) 2019-06-12
CN106164075A (zh) 2016-11-23
UA118219C2 (uk) 2018-12-10
BR112016021982A2 (ru) 2017-08-15
EP3126364B1 (en) 2018-02-07
BR112016021982B1 (pt) 2022-07-26
MY185491A (en) 2021-05-19
PH12016501963B1 (en) 2017-01-09
CN114213415A (zh) 2022-03-22
WO2015150555A1 (en) 2015-10-08
US10017509B2 (en) 2018-07-10
US20170022202A1 (en) 2017-01-26
SG11201608240RA (en) 2016-10-28
EP3126364A1 (en) 2017-02-08
CA2942636C (en) 2023-03-21
NZ725399A (en) 2023-01-27
CL2016002461A1 (es) 2017-06-23
JP2017509687A (ja) 2017-04-06

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