WO2011052888A3 - (3-플루오로-2-히드록시)프로필 작용기가 도입된 아릴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 퇴행성 뇌질환의 진단 또는 치료용 약학적 조성물 - Google Patents

(3-플루오로-2-히드록시)프로필 작용기가 도입된 아릴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 퇴행성 뇌질환의 진단 또는 치료용 약학적 조성물 Download PDF

Info

Publication number
WO2011052888A3
WO2011052888A3 PCT/KR2010/006252 KR2010006252W WO2011052888A3 WO 2011052888 A3 WO2011052888 A3 WO 2011052888A3 KR 2010006252 W KR2010006252 W KR 2010006252W WO 2011052888 A3 WO2011052888 A3 WO 2011052888A3
Authority
WO
WIPO (PCT)
Prior art keywords
aryl derivatives
fluoro
propyl
hydroxy
brain diseases
Prior art date
Application number
PCT/KR2010/006252
Other languages
English (en)
French (fr)
Other versions
WO2011052888A2 (ko
Inventor
지대윤
이병세
우타이완시리온
추소영
배유진
박찬수
문대혁
류진숙
김재승
오승준
Original Assignee
(주)퓨쳐켐
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 (주)퓨쳐켐 filed Critical (주)퓨쳐켐
Priority to CN201080048112.4A priority Critical patent/CN102725285B/zh
Priority to US13/505,159 priority patent/US9133143B2/en
Publication of WO2011052888A2 publication Critical patent/WO2011052888A2/ko
Publication of WO2011052888A3 publication Critical patent/WO2011052888A3/ko

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • C07D277/66—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2 with aromatic rings or ring systems directly attached in position 2
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D471/02—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 system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

본 발명은 (3-플루오로-2-히드록시)프로필기가 도입된 아릴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 퇴행성 뇌질환의 진단 또는 치료용 약학적 조성물에 관한 것으로, 상기 아릴 유도체는 3-플루오로-2-히드록시)프로필기가 도입되어 극성이 증가하므로 약물의 뇌-혈관막 침투가 용이하여 약물의 효과가 증대되고, β-아밀로이드에 강하게 결합하므로 방사성 동위원소로 표지할 경우 비침습적인 방법으로 알츠하이머 질병을 조기에 진단할 수 있는 진단시약으로 활용될 수 있을 뿐만 아니라, 저분자의 β-아밀로이드 펩타이드 결합체와 결합하여 악성의 고분자 β-아밀로이드 침전체의 생성을 억제시키므로 알츠하이머 질병과 같은 퇴행성 뇌질환의 치료제로 유용하게 이용될 수 있다.
PCT/KR2010/006252 2009-10-29 2010-09-14 (3-플루오로-2-히드록시)프로필 작용기가 도입된 아릴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 퇴행성 뇌질환의 진단 또는 치료용 약학적 조성물 WO2011052888A2 (ko)

Priority Applications (2)

Application Number Priority Date Filing Date Title
CN201080048112.4A CN102725285B (zh) 2009-10-29 2010-09-14 (3-氟-2-羟基)丙基功能性化芳香基衍生物或其药学可接受盐和其制备方法,以及包含该芳香基衍生物作为活性成分用于诊断或治疗脑退化性疾病的药物组合物
US13/505,159 US9133143B2 (en) 2009-10-29 2010-09-14 (3-fluoro-2-hydroxy)propyl-functionalized aryl derivatives or pharmaceutically acceptable salts thereof, method for preparing same, and pharmaceutical composition containing same as active ingredient for the diagnosis or treatment of neurodegenerative brain diseases

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR1020090103668A KR101116234B1 (ko) 2009-10-29 2009-10-29 (3-플루오로-2-히드록시)프로필 작용기가 도입된 아릴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 퇴행성 뇌질환의 진단 또는 치료용 약학적 조성물
KR10-2009-0103668 2009-10-29

Publications (2)

Publication Number Publication Date
WO2011052888A2 WO2011052888A2 (ko) 2011-05-05
WO2011052888A3 true WO2011052888A3 (ko) 2011-09-01

Family

ID=43922742

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2010/006252 WO2011052888A2 (ko) 2009-10-29 2010-09-14 (3-플루오로-2-히드록시)프로필 작용기가 도입된 아릴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 퇴행성 뇌질환의 진단 또는 치료용 약학적 조성물

Country Status (5)

Country Link
US (1) US9133143B2 (ko)
KR (1) KR101116234B1 (ko)
CN (1) CN102725285B (ko)
TW (1) TWI397412B (ko)
WO (1) WO2011052888A2 (ko)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2012397435B2 (en) * 2012-12-21 2017-03-30 National Institutes For Quantum And Radiological Science And Technology Novel compound for imaging TAU protein accumulated in the brain
US9246108B2 (en) 2012-12-28 2016-01-26 Dow Global Technologies Llc Quinoline-benzoxazole derived compounds for electronic films and devices
CN103613589B (zh) * 2013-11-29 2016-03-30 江苏华益科技有限公司 一种用于神经退行性疾病领域的新型pet显像剂前体及标准品的合成方法
CN104059028B (zh) * 2014-06-06 2020-10-16 北京智博高科生物技术有限公司 与Aβ斑块具有亲和力的含手性侧链取代的氟代2-芳基苯并杂环化合物、其制备方法及应用
KR101709731B1 (ko) * 2015-05-22 2017-02-23 한국과학기술연구원 벤조옥사졸 또는 벤조티아졸 화합물, 그의 제조, 및 용도
EP3307798B2 (en) 2015-06-12 2024-06-05 Transitions Optical, Inc. Alignment compounds
AR110038A1 (es) 2016-05-26 2019-02-20 Kalyra Pharmaceuticals Inc Compuestos inhibidores de egfr; composición farmacéutica que lo comprende; métodos para mejorar o tratar un cáncer; método para inhibir la replicación de un crecimiento maligno o un tumor; métodos para inhibir la actividad del egfr; y usos de los compuestos
US10793551B2 (en) 2017-10-19 2020-10-06 Effector Therapeutics Inc. Benzimidazole-indole inhibitors of Mnk1 and Mnk2
EP3790883A4 (en) 2018-05-09 2022-08-24 Aprinoia Therapeutics Limited HETEROARYL COMPOUNDS AND USES THEREOF
CN112105393A (zh) * 2018-05-16 2020-12-18 爱默蕾大学 苯乙烯基苯并噻唑衍生物及在成像中的用途
CN112010846A (zh) * 2019-05-30 2020-12-01 四川大学华西医院 一种吡啶衍生物及其制备方法和用途
AU2020383593A1 (en) 2019-11-13 2022-06-09 Aprinoia Therapeutics Limited Compounds for degrading Tau protein aggregates and uses thereof
JP2023534837A (ja) 2020-07-20 2023-08-14 ニド・バイオサイエンシーズ・インコーポレイテッド アンドロゲン受容体モジュレーターとしてのインドール化合物

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007093364A1 (en) * 2006-02-15 2007-08-23 Sanofi-Aventis Azacyclyl-substituted aryldihydroisoquinolinones, process for their preparation and their use as medicaments
WO2008109080A2 (en) * 2007-03-01 2008-09-12 Siemens Medical Solutions Usa, Inc. Nucleoside based proliferation imaging markers
WO2009077680A1 (fr) * 2007-10-03 2009-06-25 Sanofi-Aventis Dérivés de quinazolinedione, leur préparation et leurs applications thérapeutiques

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090185975A1 (en) 2005-12-26 2009-07-23 Tohoku University Diagnostic probe for conformation disease

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007093364A1 (en) * 2006-02-15 2007-08-23 Sanofi-Aventis Azacyclyl-substituted aryldihydroisoquinolinones, process for their preparation and their use as medicaments
WO2008109080A2 (en) * 2007-03-01 2008-09-12 Siemens Medical Solutions Usa, Inc. Nucleoside based proliferation imaging markers
WO2009077680A1 (fr) * 2007-10-03 2009-06-25 Sanofi-Aventis Dérivés de quinazolinedione, leur préparation et leurs applications thérapeutiques

Also Published As

Publication number Publication date
US20120214994A1 (en) 2012-08-23
KR101116234B1 (ko) 2014-03-06
US9133143B2 (en) 2015-09-15
KR20110046943A (ko) 2011-05-06
WO2011052888A2 (ko) 2011-05-05
TW201116302A (en) 2011-05-16
CN102725285B (zh) 2015-05-20
CN102725285A (zh) 2012-10-10
TWI397412B (zh) 2013-06-01

Similar Documents

Publication Publication Date Title
WO2011052888A3 (ko) (3-플루오로-2-히드록시)프로필 작용기가 도입된 아릴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 퇴행성 뇌질환의 진단 또는 치료용 약학적 조성물
WO2006003488A3 (en) Annexins, derivatives thereof, and annexin-cys variants, as well as therapeutic and diagnostic uses thereof
WO2010115843A3 (en) Pharmaceutical composition
WO2005072061A3 (en) Conjugates for cancer therapy and diagnosis
UA104320C2 (ru) Фармацевтическая композиция на основе митохондриально-адресованного антиоксиданта для применения в медицинской и ветеринарной офтальмологии
EA201270144A1 (ru) Комбинированная терапия при лечении диабета
WO2008131056A3 (en) Sustained release monoeximic formulations of opioid and nonopioid analgesics
NZ591810A (en) Pharmaceutical compositions and related methods of delivery the composition comprises a medium chain fatty acid
AR068816A1 (es) Composiciones de brimonidina mejorada para el tratamiento del eritema
ATE470151T1 (de) Diagnose, behandlung und prävention von gefässerkrankungen mittels il-1alpha- autoantikörpern
JP6640725B2 (ja) ｓｐａｄｉｎのレトロ−インベルソ類似体は増大された抗うつ作用を示す
AR062659A1 (es) Composicion de liberacion sostenida de levodopa y metodo para su uso
WO2011059263A3 (ko) 뇌혈관 장벽을 통과하여 퇴행성 뇌신경 질환 부위의 세포사멸을 표적하는 펩타이드 및 이의 용도
Muñoz-Espín Nanocarriers targeting senescent cells
US11331391B2 (en) Phosphonate-drug conjugates
BR112021010982A2 (pt) Ligantes
WO2006131833A3 (en) New hybrid oligomers. their preparation process and pharmaceutical compositions containing them
AU2021421391A1 (en) Inhibitors of atp synthase - cosmetic and therapeutic uses
ATE418540T1 (de) Galloylpeptide
JP2009526834A5 (ko)
MX2009009113A (es) Nuevos indoles 2-heteroaril sustituidos 695.
EP3137097A1 (en) Treatment and prevention of alzheimer's disease (ad)
CN103079556A (zh) 一种用于预防或治疗神经退行性脑功能紊乱的药物组合物
WO2011149250A2 (ko) 트리카르보닐 테크네슘-99ｍ 또는 레늄-188 표지 고리 알지디 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 신생혈관 관련 질환의 진단 또는 치료용 약학적 조성물
WO2015165961A1 (en) Treatment and prevention of alzheimer's disease (ad)

Legal Events

Date Code Title Description
WWE Wipo information: entry into national phase

Ref document number: 201080048112.4

Country of ref document: CN

121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 10826973

Country of ref document: EP

Kind code of ref document: A1

NENP Non-entry into the national phase

Ref country code: DE

WWE Wipo information: entry into national phase

Ref document number: 13505159

Country of ref document: US

32PN Ep: public notification in the ep bulletin as address of the adressee cannot be established

Free format text: NOTING OF LOSS OF RIGHTS PURSUANT TO RULE 112(1) EPC (EPO FORM 1205N DATED 05.07.2012)

122 Ep: pct application non-entry in european phase

Ref document number: 10826973

Country of ref document: EP

Kind code of ref document: A2