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WO2018155916A3 - 피롤로-피리미딘 유도체 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 단백질 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물 - Google Patents

피롤로-피리미딘 유도체 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 단백질 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물 Download PDF

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Publication number
WO2018155916A3
WO2018155916A3 PCT/KR2018/002164 KR2018002164W WO2018155916A3 WO 2018155916 A3 WO2018155916 A3 WO 2018155916A3 KR 2018002164 W KR2018002164 W KR 2018002164W WO 2018155916 A3 WO2018155916 A3 WO 2018155916A3
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WIPO (PCT)
Prior art keywords
compound
pharmaceutical composition
effective ingredient
protein kinase
preventing
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Ceased
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PCT/KR2018/002164
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English (en)
French (fr)
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WO2018155916A2 (ko
Inventor
최환근
박종배
고은화
손정범
조중희
고이경
박진희
김소영
강석용
이승연
김남두
이윤호
이선화
김다예
이선주
배재현
홍은미
장태호
김상범
이승훈
남도현
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National Cancer Center Japan
National Cancer Center Korea
Samsung Life Public Welfare Foundation
Daegu Gyeongbuk Medical Innovation Foundation
Original Assignee
National Cancer Center Japan
National Cancer Center Korea
Samsung Life Public Welfare Foundation
Daegu Gyeongbuk Medical Innovation Foundation
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Publication date
Application filed by National Cancer Center Japan, National Cancer Center Korea, Samsung Life Public Welfare Foundation, Daegu Gyeongbuk Medical Innovation Foundation filed Critical National Cancer Center Japan
Priority to EP18757481.9A priority Critical patent/EP3587422A4/en
Priority to US16/488,194 priority patent/US11208412B2/en
Publication of WO2018155916A2 publication Critical patent/WO2018155916A2/ko
Publication of WO2018155916A3 publication Critical patent/WO2018155916A3/ko
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2200/00—Function of food ingredients
    • A23V2200/30—Foods, ingredients or supplements having a functional effect on health
    • A23V2200/308—Foods, ingredients or supplements having a functional effect on health having an effect on cancer prevention
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2200/00—Function of food ingredients
    • A23V2200/30—Foods, ingredients or supplements having a functional effect on health
    • A23V2200/322—Foods, ingredients or supplements having a functional effect on health having an effect on the health of the nervous system or on mental function
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers

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

Abstract

본 발명은 신규한 피롤로-피리미딘 유도체 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 단백질 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물에 관한 것이다. 본 발명에 따른 화학식 1로 표시되는 화합물, 이의 광학 이성질체, 또는 이의 약학적으로 허용 가능한 염 및 이를 유효성분으로 하는 약학적 조성물은 LRRK2 키나아제에 대한 억제활성이 우수하며, LRRK2 발현 세포주인 NIH-3T3 세포주 및 뇌종양 환자 유래 세포주인 NCC01과 448T 세포주에서의 인산화 억제 효과가 뛰어나다. 또한, LRRK2 이외에도 다양한 단백질 키나아제에 대하여 저해활성을 가지는 것이 실험을 통해 확인되었으므로, 단백질 키나아제 관련 질환의 치료 또는 예방에 효과적으로 사용될 수 있다.
PCT/KR2018/002164 2017-02-22 2018-02-22 피롤로-피리미딘 유도체 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 단백질 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물 Ceased WO2018155916A2 (ko)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP18757481.9A EP3587422A4 (en) 2017-02-22 2018-02-22 PYRROLO-PYRIMIDINE DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME AS ACTIVE INGREDIENT FOR THE PREVENTION OR TREATMENT OF A PROTEIN KINASE-RELATED DISEASE
US16/488,194 US11208412B2 (en) 2017-02-22 2018-02-22 Pyrrolo-pyrimidine derivative compound, preparation method therefor, and pharmaceutical composition comprising same compound as effective ingredient for preventing or treating protein kinase-related disease

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR20170023393 2017-02-22
KR10-2017-0023393 2017-02-22

Publications (2)

Publication Number Publication Date
WO2018155916A2 WO2018155916A2 (ko) 2018-08-30
WO2018155916A3 true WO2018155916A3 (ko) 2018-12-06

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2018/002164 Ceased WO2018155916A2 (ko) 2017-02-22 2018-02-22 피롤로-피리미딘 유도체 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 단백질 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물

Country Status (4)

Country Link
US (1) US11208412B2 (ko)
EP (1) EP3587422A4 (ko)
KR (2) KR20180097162A (ko)
WO (1) WO2018155916A2 (ko)

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DK3604304T3 (da) * 2017-03-23 2022-10-31 Daegu Gyeongbuk Medical Innovation Found Pyrrolo-pyridinderivatforbindelse, fremgangsmåde til fremstilling deraf og farmaceutisk sammensætning indeholdende denne som aktiv ingrediens til forebyggelse eller behandling af proteinkinase-relaterede sygdomme
CN111433208B (zh) * 2017-12-05 2023-06-30 奥斯考泰克公司 作为lrrk2抑制剂的吡咯并(吡唑并)嘧啶衍生物
KR20200029144A (ko) 2018-09-10 2020-03-18 김성우 확장용 블록놀이 받침판이 장착된 블록놀이용 탈것
US12240844B2 (en) 2019-01-18 2025-03-04 Voronoi, Inc. Pyrrolopyridine derivative and use thereof in prevention and treatment of protein kinase-related disease
WO2020149723A1 (ko) * 2019-01-18 2020-07-23 주식회사 보로노이 피롤로피리미딘 유도체 및 이를 유효성분으로 함유하는 단백질 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물
CN111662295B (zh) * 2019-03-05 2021-09-10 珠海宇繁生物科技有限责任公司 一种irak4激酶抑制剂及其制备方法
CA3130478A1 (en) * 2019-03-13 2020-09-17 Voronoi Co., Ltd. Heteroaryl derivatives, and pharmaceutical composition comprising the same as active ingredient
AU2020273443B2 (en) * 2019-05-16 2025-11-06 Dana-Farber Cancer Institute, Inc. Pyrrolopyrimidine inhibitors of wild-type and mutant forms of LRRK2
WO2020235973A1 (ko) * 2019-05-22 2020-11-26 주식회사 보로노이 암의 예방 및/또는 치료를 위한 피롤로-피리딘 유도체 화합물의 신규 용도
GEP20247661B (en) 2020-05-06 2024-09-10 Servier Lab New macrocyclic lrrk2 kinase inhibitors
CN111620878A (zh) * 2020-06-10 2020-09-04 中国药科大学 吡咯并嘧啶类衍生物作为蛋白激酶抑制剂及其应用
CA3197034A1 (en) * 2020-10-29 2022-05-05 Suzhou Yabao Pharmaceutical R&D Co., Ltd. Substituted diarylamine compound, pharmaceutical composition thereof, preparation method therefor, and use thereof
KR20220081631A (ko) 2020-12-09 2022-06-16 보로노이 주식회사 염증성 질환의 예방 및/또는 치료를 위한 피롤로-피리딘 유도체 화합물의 신규 용도
MX2023010910A (es) 2021-03-18 2023-09-27 Servier Lab Nuevos inhibidores macrociclicos de la quinasa de lrrk2.
KR102585194B1 (ko) * 2021-03-26 2023-10-10 주식회사 스탠다임 Lrrk2에 대해 저해 활성을 갖는 신규한 페닐아미노피리미딘화합물 및 이의 용도
EP4105218A1 (en) * 2021-06-15 2022-12-21 Sanofi Substituted pyrrolo[2,3-d] pyrimidines, their preparation and their therapeutic application
IL309195A (en) 2021-06-15 2024-02-01 Sanofi Sa Substituted pyrrolo[2,3-d]pyrimidines, their preparation and their therapeutic application
US11780851B2 (en) 2021-10-27 2023-10-10 H. Lundbeck A/S LRRK2 inhibitors
WO2024035771A2 (en) * 2022-08-09 2024-02-15 H. Lee Moffitt Cancer Center And Research Institute, Inc. Ulk3 inhibitors and uses thereof
KR102651320B1 (ko) * 2022-08-11 2024-03-28 환인제약 주식회사 신규한 헤테로아릴 치환 유도체 및 이를 포함하는 신경퇴행성 질환, 암, 및 염증성 질환의 예방 또는 치료용 조성물
WO2024035194A1 (ko) * 2022-08-11 2024-02-15 환인제약 주식회사 신규한 헤테로아릴 치환 유도체 및 이를 포함하는 신경퇴행성 질환, 암, 및 염증성 질환의 예방 또는 치료용 조성물
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WO2009131687A2 (en) * 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
KR20140059246A (ko) * 2011-09-22 2014-05-15 화이자 인코포레이티드 피롤로피리미딘 및 퓨린 유도체
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Also Published As

Publication number Publication date
WO2018155916A2 (ko) 2018-08-30
EP3587422A2 (en) 2020-01-01
KR20180132575A (ko) 2018-12-12
US11208412B2 (en) 2021-12-28
EP3587422A4 (en) 2020-05-06
KR102092812B1 (ko) 2020-03-25
US20200239474A1 (en) 2020-07-30
KR20180097162A (ko) 2018-08-30

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