KR102390276B1 - 마크로사이클릭 피리미딘 유도체 - Google Patents

마크로사이클릭 피리미딘 유도체 Download PDF

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Publication number
KR102390276B1
KR102390276B1 KR1020167028764A KR20167028764A KR102390276B1 KR 102390276 B1 KR102390276 B1 KR 102390276B1 KR 1020167028764 A KR1020167028764 A KR 1020167028764A KR 20167028764 A KR20167028764 A KR 20167028764A KR 102390276 B1 KR102390276 B1 KR 102390276B1
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alkyl
independently
optionally substituted
hydrogen
alkanediyl
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KR20160142316A (ko
Inventor
가스톤 스타니슬라스 마르셀라 디엘스
브루노 쇼엔티에스
마티아스 룩 에이미 베르셀
디디에 쟝-클로드 베르텔로
마크 윌렘스
마르셀 빌레보예
베르너 콘스탄트 요한 엠브레흐츠
베르톨드 우로블로우스키
리벤 미르포엘
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얀센 파마슈티카 엔.브이.
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020167028764A 2014-04-03 2015-04-02 마크로사이클릭 피리미딘 유도체 Expired - Fee Related KR102390276B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP14163443.6 2014-04-03
EP14163443 2014-04-03
EP14183747 2014-09-05
EP14183747.6 2014-09-05
PCT/EP2015/057399 WO2015150555A1 (en) 2014-04-03 2015-04-02 Macrocylic pyrimidine derivatives

Publications (2)

Publication Number Publication Date
KR20160142316A KR20160142316A (ko) 2016-12-12
KR102390276B1 true KR102390276B1 (ko) 2022-04-22

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KR1020167028764A Expired - Fee Related KR102390276B1 (ko) 2014-04-03 2015-04-02 마크로사이클릭 피리미딘 유도체

Country Status (21)

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

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TWI721104B (zh) 2016-02-19 2021-03-11 瑞典商斯普林特生物科技公司 6‐芳基或6‐雜芳基‐4‐嗎啉‐4‐芳基‐吡啶‐2‐酮化合物
ES2821400T3 (es) 2016-02-19 2021-04-26 Sprint Bioscience Ab Compuestos de 6-heterociclil-4-morfolin-4-ilpiridin-2-ona útiles para el tratamiento del cáncer y la diabetes
EP3601236A1 (en) 2017-03-28 2020-02-05 Bayer Aktiengesellschaft Novel ptefb inhibiting macrocyclic compounds
ES2900199T3 (es) 2017-03-28 2022-03-16 Bayer Ag Novedosos compuestos macrocíclicos inhibidores de PTEFB
SI3672962T1 (sl) 2017-08-23 2022-06-30 Sprint Bioscience Ab Morfolinilpiridonske spojine
SI3672967T1 (sl) 2017-08-23 2022-04-29 Sprint Bioscience Ab Spojine azaindolilpiridona in diazaindolilpiridona
TW202325302A (zh) 2017-08-23 2023-07-01 瑞典商斯普林特生物科技公司 吡啶胺-吡啶酮及嘧啶胺-吡啶酮化合物
JP7199737B2 (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 ピリジルピリドン化合物
US20230148005A1 (en) * 2020-02-18 2023-05-11 Theseus Pharmaceuticals, Inc. Macrocyclic compounds and uses thereof
KR20230007369A (ko) * 2020-04-07 2023-01-12 아이테오스 벨지움 에스에이 암의 치료를 위한 ent 저해제로서의 거대환식 다이아민 유도체 및 이와 아데노신 수용체 길항제와의 조합물
CN113735879B (zh) * 2020-05-27 2022-05-17 百极弘烨（广东）医药科技有限公司 一种大环jak抑制剂及其应用
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
WO2022020651A1 (en) * 2020-07-22 2022-01-27 Fog Pharmaceuticals, Inc. Amino acids
CN118139846A (zh) * 2021-09-23 2024-06-04 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
CN117229300A (zh) * 2023-03-12 2023-12-15 药雅科技(上海)有限公司 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
CN116478076A (zh) * 2023-04-26 2023-07-25 南京优氟医药科技有限公司 一种(2s,4s)-1-叔丁氧羰基-2-(二氟甲基)-4-羟基吡咯烷的制备方法

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JP2009500307A (ja) 2005-06-30 2009-01-08 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 環式アニリノ−ピリジノトリアジン
JP2009517344A (ja) 2005-11-16 2009-04-30 エス＊バイオ プライベート リミティッド ヘテロアルキル結合ピリミジン誘導体
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JP2009500307A (ja) 2005-06-30 2009-01-08 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 環式アニリノ−ピリジノトリアジン
JP2009517344A (ja) 2005-11-16 2009-04-30 エス＊バイオ プライベート リミティッド ヘテロアルキル結合ピリミジン誘導体
WO2009112439A1 (en) 2008-03-10 2009-09-17 Janssen Pharmaceutica Nv 4-aryl-2-anilino-pyrimidines as plk kinase inhibitors

Also Published As

Publication number Publication date
US20170022202A1 (en) 2017-01-26
SG11201608240RA (en) 2016-10-28
PE20161362A1 (es) 2016-12-17
ES2667723T3 (es) 2018-05-14
UA118219C2 (uk) 2018-12-10
EP3126364A1 (en) 2017-02-08
EA201692003A1 (ru) 2017-06-30
AU2015239098B2 (en) 2019-08-01
AU2015239098A1 (en) 2016-09-29
EP3126364B1 (en) 2018-02-07
BR112016021982A2 (https=) 2017-08-15
CA2942636C (en) 2023-03-21
MA39822A (fr) 2018-02-06
IL248005B (en) 2018-12-31
KR20160142316A (ko) 2016-12-12
PH12016501963B1 (en) 2017-01-09
WO2015150555A1 (en) 2015-10-08
US10017509B2 (en) 2018-07-10
CL2016002461A1 (es) 2017-06-23
BR112016021982B1 (pt) 2022-07-26
PH12016501963A1 (en) 2017-01-09
CN106164075A (zh) 2016-11-23
MY185491A (en) 2021-05-19
CA2942636A1 (en) 2015-10-08
NZ725399A (en) 2023-01-27
JP2017509687A (ja) 2017-04-06
CN106164075B (zh) 2021-11-26
CN114213415A (zh) 2022-03-22
MX2016012992A (es) 2016-12-07
EA031246B1 (ru) 2018-12-28
MX369798B (es) 2019-11-21
JP6529513B2 (ja) 2019-06-12

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