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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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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compound
pharmaceutical composition
effective ingredient
protein kinase
preventing
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WO2018155916A2 (ko
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최환근
박종배
고은화
손정범
조중희
고이경
박진희
김소영
강석용
이승연
김남두
이윤호
이선화
김다예
이선주
배재현
홍은미
장태호
김상범
이승훈
남도현
Original Assignee
재단법인 대구경북첨단의료산업진흥재단
국립암센터
사회복지법인 삼성생명공익재단
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Priority to US16/488,194 priority Critical patent/US11208412B2/en
Priority to EP18757481.9A priority patent/EP3587422A4/en
Publication of WO2018155916A2 publication Critical patent/WO2018155916A2/ko
Publication of WO2018155916A3 publication Critical patent/WO2018155916A3/ko

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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 COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • 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
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    • 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)
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  • Veterinary Medicine (AREA)
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  • Polymers & Plastics (AREA)
  • Food Science & Technology (AREA)
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  • 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 WO2018155916A2 (ko)

Priority Applications (2)

Application Number Priority Date Filing Date Title
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
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

Applications Claiming Priority (2)

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

Publications (2)

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

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PCT/KR2018/002164 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)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT3604304T (pt) * 2017-03-23 2022-11-30 Korea Res Inst Bioscience & Biotechnology Composto derivado de pirrolo-piridina, método para a sua preparação e composição farmacêutica que o contém como substância ativa para prevenção ou tratamento de doenças relacionadas com proteína quinase
WO2019112269A1 (ko) * 2017-12-05 2019-06-13 주식회사 오스코텍 Lrrk2 억제제로서의 피롤로(피라졸로)피리미딘 유도체
KR20200029144A (ko) 2018-09-10 2020-03-18 김성우 확장용 블록놀이 받침판이 장착된 블록놀이용 탈것
AU2020209789A1 (en) * 2019-01-18 2021-09-16 Voronoi Co., Ltd. Pyrrolopyrimidine derivative, and pharmaceutical composition for preventing or treating protein kinase-related disease comprising same as active ingredient
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
EP3915986A4 (en) * 2019-03-13 2023-01-25 Voronoi Inc. HETEROARYL DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING THEM AS ACTIVE PRINCIPLE
CA3135409A1 (en) * 2019-05-16 2020-11-19 Dana-Farber Cancer Institute, Inc. Pyrrolopyrimidine inhibitors of wild-type and mutant forms of lrrk2
CN114423434A (zh) * 2019-05-22 2022-04-29 沃若诺伊公司 吡咯并吡啶衍生物化合物用于预防和/或治疗癌症的新用途
IL297867A (en) 2020-05-06 2023-01-01 Servier Lab Novel 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
EP4238975A4 (en) * 2020-10-29 2024-06-12 Suzhou Yabao Pharmaceutical R&D Co., Ltd. SUBSTITUTED DIARYLAMINE COMPOUND, PHARMACEUTICAL COMPOSITION THEREOF, MANUFACTURING PROCESS THEREOF AND USE THEREOF
CA3213388A1 (en) 2021-03-18 2022-09-22 Les Laboratoires Servier Macrocyclic lrrk2 kinase inhibitors
WO2022203466A1 (ko) * 2021-03-26 2022-09-29 주식회사 스탠다임 Lrrk2에 대해 저해 활성을 갖는 신규한 페닐아미노피리미딘 화합물 및 이의 용도
IL309195A (en) 2021-06-15 2024-02-01 Sanofi Sa Converted pyrrolo[2,3-D]pyrimidines, their preparation and therapeutic application
EP4105218A1 (en) * 2021-06-15 2022-12-21 Sanofi Substituted pyrrolo[2,3-d] pyrimidines, their preparation and their therapeutic application
BR112023012947A2 (pt) 2021-10-27 2024-04-30 H Lundbeck As Inibidores de lrrk2
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
US11958865B1 (en) 2022-09-15 2024-04-16 H. Lundbeck A/S Leucine-rich repeat kinase 2 (LRRK2) inhibitors

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007042299A1 (en) * 2005-10-13 2007-04-19 Glaxo Group Limited Pyrrolopyrimidine derivatives as syk inhibitors
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
KR20160106622A (ko) * 2014-01-29 2016-09-12 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 화합물
KR20160106623A (ko) * 2014-01-29 2016-09-12 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 화합물

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0808651A2 (pt) 2007-03-09 2014-08-19 Green Cross Corp Pró-medicamentos oralmente biodisponíveis de (+)-3-hidroximorfinano para a prevenção ou o tratamento da doença de parkinson.
ES2717757T3 (es) 2014-01-29 2019-06-25 Glaxosmithkline Ip Dev Ltd Compuestos

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007042299A1 (en) * 2005-10-13 2007-04-19 Glaxo Group Limited Pyrrolopyrimidine derivatives as syk inhibitors
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
KR20160106622A (ko) * 2014-01-29 2016-09-12 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 화합물
KR20160106623A (ko) * 2014-01-29 2016-09-12 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 화합물

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

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