UA118219C2 - Макроциклічні похідні піримідину - Google Patents

Макроциклічні похідні піримідину

Info

Publication number
UA118219C2
UA118219C2 UAA201611005A UAA201611005A UA118219C2 UA 118219 C2 UA118219 C2 UA 118219C2 UA A201611005 A UAA201611005 A UA A201611005A UA A201611005 A UAA201611005 A UA A201611005A UA 118219 C2 UA118219 C2 UA 118219C2
Authority
UA
Ukraine
Prior art keywords
compounds
pyrimidine derivatives
inhibitory activity
present
macrocylic
Prior art date
Application number
UAA201611005A
Other languages
English (en)
Inventor
Ґастон Станіслас Марсела Дилс
Бруно Схунтьєс
Матіас Люк Еме Версель
Дидьє Жан-Клод Бертло
Марк Вілемс
Марсель В'єєвуа
Вернер Констант Йохан Ембрехтс
Бертольд Вробловскі
Лівен 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 UA118219C2 publication Critical patent/UA118219C2/uk

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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Даний винахід стосується заміщених макроциклічних похідних піримідину формули (І) , де змінні мають значення, визначені у формулі винаходу. Сполуки згідно з даним винаходом мають ЕР2K-інгібуючу активність і необов'язково також Vps34-інгібуючу активність. Даний винахід, крім того, стосується способів одержання таких нових сполук, фармацевтичних композицій, які містять вказані сполуки як активний інгредієнт, а також застосування вказаних сполук як лікарського препарату.
UAA201611005A 2014-04-03 2015-04-02 Макроциклічні похідні піримідину UA118219C2 (uk)

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 (1)

Publication Number Publication Date
UA118219C2 true UA118219C2 (uk) 2018-12-10

Family

ID=52781117

Family Applications (1)

Application Number Title Priority Date Filing Date
UAA201611005A UA118219C2 (uk) 2014-04-03 2015-04-02 Макроциклічні похідні піримідину

Country Status (21)

Country Link
US (1) US10017509B2 (uk)
EP (1) EP3126364B1 (uk)
JP (1) JP6529513B2 (uk)
KR (1) KR102390276B1 (uk)
CN (2) CN114213415A (uk)
AU (1) AU2015239098B2 (uk)
BR (1) BR112016021982B1 (uk)
CA (1) CA2942636C (uk)
CL (1) CL2016002461A1 (uk)
EA (1) EA031246B1 (uk)
ES (1) ES2667723T3 (uk)
IL (1) IL248005B (uk)
MA (1) MA39822A (uk)
MX (1) MX369798B (uk)
MY (1) MY185491A (uk)
NZ (1) NZ725399A (uk)
PE (1) PE20161362A1 (uk)
PH (1) PH12016501963A1 (uk)
SG (1) SG11201608240RA (uk)
UA (1) UA118219C2 (uk)
WO (1) WO2015150555A1 (uk)

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CA3015005A1 (en) 2016-02-19 2017-08-24 Sprint Bioscience Ab 6-heterocyclyl-4-morpholin-4-ylpyridine-2-one compounds useful for the treatment of cancer and diabetes
US11077113B2 (en) 2016-02-19 2021-08-03 Sprint Bioscience Ab 6-aryl-4-morpholin-1-ylpyridone compounds useful for the treatment of cancer and diabetes
US11242356B2 (en) 2017-03-28 2022-02-08 Bayer Aktiengesellschaft PTEFb inhibiting macrocyclic compounds
ES2900199T3 (es) 2017-03-28 2022-03-16 Bayer Ag Novedosos compuestos macrocíclicos inhibidores de PTEFB
ES2910157T3 (es) 2017-08-23 2022-05-11 Sprint Bioscience Ab Compuestos de morfolinilpiridona
CN116589462A (zh) 2017-08-23 2023-08-15 思普瑞特生物科学公司 氮杂吲哚基吡啶酮化合物和二氮杂吲哚基吡啶酮化合物
CN116041321A (zh) 2017-08-23 2023-05-02 思普瑞特生物科学公司 吡啶胺-吡啶酮化合物和嘧啶胺-吡啶酮化合物
PL3672941T3 (pl) 2017-08-23 2022-06-13 Sprint Bioscience Ab Związki pirydylopirydonu
MX2022010128A (es) * 2020-02-18 2023-01-04 Theseus Pharmaceuticals Inc Compuestos macrocíclicos y usos de estos.
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
WO2024094171A1 (zh) * 2022-11-04 2024-05-10 江苏恒瑞医药股份有限公司 取代的氨基嘧啶类化合物、其制备方法及其在医药上的应用

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WO2004078682A2 (en) * 2003-03-05 2004-09-16 Irm Llc Cyclic compounds and compositions as protein kinase inhibitors
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PA8603801A1 (es) 2003-05-27 2004-12-16 Janssen Pharmaceutica Nv Derivados de la quinazolina
EP1697384B1 (en) 2003-12-18 2008-04-02 Janssen Pharmaceutica N.V. Pyrido- and pyrimidopyrimidine derivatives as anti-proliferative agents
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WO2007058627A1 (en) * 2005-11-16 2007-05-24 S*Bio Pte Ltd Oxygen linked pyrimidine derivatives
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BRPI1011612A2 (pt) 2009-05-28 2019-09-24 Tetralogic Pharm Corp composto, composição farmacêutica, e, métodos para induzir apoptose em uma célula, para tratar câncer, e para tratar uma doença autoimune.
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TWI513695B (zh) 2009-10-27 2015-12-21 Merck Sharp & Dohme （１，１，１，３，３，３－六氟－２－羥基丙－２－基）苯基衍生物

Also Published As

Publication number Publication date
AU2015239098B2 (en) 2019-08-01
NZ725399A (en) 2023-01-27
MX369798B (es) 2019-11-21
MY185491A (en) 2021-05-19
EP3126364A1 (en) 2017-02-08
EP3126364B1 (en) 2018-02-07
EA201692003A1 (ru) 2017-06-30
PH12016501963B1 (en) 2017-01-09
PE20161362A1 (es) 2016-12-17
MX2016012992A (es) 2016-12-07
KR102390276B1 (ko) 2022-04-22
CN114213415A (zh) 2022-03-22
IL248005B (en) 2018-12-31
PH12016501963A1 (en) 2017-01-09
US20170022202A1 (en) 2017-01-26
SG11201608240RA (en) 2016-10-28
CL2016002461A1 (es) 2017-06-23
US10017509B2 (en) 2018-07-10
KR20160142316A (ko) 2016-12-12
AU2015239098A1 (en) 2016-09-29
MA39822A (fr) 2018-02-06
BR112016021982B1 (pt) 2022-07-26
JP6529513B2 (ja) 2019-06-12
ES2667723T3 (es) 2018-05-14
CA2942636A1 (en) 2015-10-08
EA031246B1 (ru) 2018-12-28
WO2015150555A1 (en) 2015-10-08
CN106164075A (zh) 2016-11-23
CN106164075B (zh) 2021-11-26
BR112016021982A2 (uk) 2017-08-15
JP2017509687A (ja) 2017-04-06
CA2942636C (en) 2023-03-21

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