WO2010032986A2 - Nouveaux dérivés de 5-(4-aminophenyl)-isoquinoline, leurs sels pharmaceutiquement acceptables, procédé de production associé et composition contenant les dérivés comme principe actif pour la prophylaxie et le traitement d'états pathologiques induits par l'hyperactivité de la kinase raf - Google Patents

Nouveaux dérivés de 5-(4-aminophenyl)-isoquinoline, leurs sels pharmaceutiquement acceptables, procédé de production associé et composition contenant les dérivés comme principe actif pour la prophylaxie et le traitement d'états pathologiques induits par l'hyperactivité de la kinase raf Download PDF

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Publication number
WO2010032986A2
WO2010032986A2 PCT/KR2009/005326 KR2009005326W WO2010032986A2 WO 2010032986 A2 WO2010032986 A2 WO 2010032986A2 KR 2009005326 W KR2009005326 W KR 2009005326W WO 2010032986 A2 WO2010032986 A2 WO 2010032986A2
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WO
WIPO (PCT)
Prior art keywords
phenyl
formula
compound
trifluoromethyl
isoquinolin
Prior art date
Application number
PCT/KR2009/005326
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English (en)
Korean (ko)
Other versions
WO2010032986A3 (fr
Inventor
한철규
윤정혁
김남두
심은경
Original Assignee
주식회사 이큐스팜
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 주식회사 이큐스팜 filed Critical 주식회사 이큐스팜
Publication of WO2010032986A2 publication Critical patent/WO2010032986A2/fr
Publication of WO2010032986A3 publication Critical patent/WO2010032986A3/fr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38—Nitrogen atoms
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/18—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38—Nitrogen atoms
    • C07D215/40—Nitrogen atoms attached in position 8
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/04—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/08—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with a hetero atom directly attached to the ring nitrogen atom

Abstract

L'invention concerne un nouveau dérivé de 5-(4-aminophényl)-isoquinoline ou un de ses sels pharmaceutiquement acceptable, un procédé de production associé, et une composition contenant ledit dérivé en tant que principe actif utilisé dans la prophylaxie et le traitement d'états pathologiques induits par l'hyperactivité des kinases Raf. La composition contenant le dérivé de 5-(4-aminophenyl)-isoquinoline de l'invention inhibe efficacement l'activité des kinases Raf et particulièrement la kinase B-raf, et le dérivé peut être ainsi utilisé avec un effet positif dans la prophylaxie et le traitement de cancers ou de mélanomes induits par l'hyperactivité des kinases Raf.
PCT/KR2009/005326 2008-09-18 2009-09-18 Nouveaux dérivés de 5-(4-aminophenyl)-isoquinoline, leurs sels pharmaceutiquement acceptables, procédé de production associé et composition contenant les dérivés comme principe actif pour la prophylaxie et le traitement d'états pathologiques induits par l'hyperactivité de la kinase raf WO2010032986A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR1020080091405A KR20100032496A (ko) 2008-09-18 2008-09-18 신규 5-(4-아미노페닐)-이소퀴놀린 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 Ｒａｆ 키나제의 과활성에 의해 유발되는 질환의 예방 또는 치료용 조성물
KR10-2008-0091405 2008-09-18

Publications (2)

Publication Number Publication Date
WO2010032986A2 true WO2010032986A2 (fr) 2010-03-25
WO2010032986A3 WO2010032986A3 (fr) 2010-08-19

Family

ID=42040023

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2009/005326 WO2010032986A2 (fr) 2008-09-18 2009-09-18 Nouveaux dérivés de 5-(4-aminophenyl)-isoquinoline, leurs sels pharmaceutiquement acceptables, procédé de production associé et composition contenant les dérivés comme principe actif pour la prophylaxie et le traitement d'états pathologiques induits par l'hyperactivité de la kinase raf

Country Status (2)

Country Link
KR (1) KR20100032496A (fr)
WO (1) WO2010032986A2 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
WO2018146253A1 (fr) 2017-02-10 2018-08-16 INSERM (Institut National de la Santé et de la Recherche Médicale) Procédés et compositions pharmaceutiques pour le traitement de cancers associés à l'activation de la voie mapk
WO2019133810A1 (fr) 2017-12-28 2019-07-04 Tract Pharmaceuticals, Inc. Systèmes de culture de cellules souches pour cellules souches épithéliales colonnaires, et leurs utilisations

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102337870B1 (ko) * 2020-02-03 2021-12-10 순천대학교 산학협력단 세포자멸사를 유도하는 치환된 다이아릴우레아 화합물 및 이를 포함하는 항암용 조성물

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030114679A1 (en) * 2001-09-12 2003-06-19 Mceachern Ernest J. Synthesis of enantiomerically pure amino-substituted fused bicyclic rings
WO2005049576A1 (fr) * 2003-11-19 2005-06-02 Glaxo Group Limited Isoquinolines substituees utiles pour le traitement de maladies du type cancer et atherosclerose
WO2005049574A1 (fr) * 2003-11-20 2005-06-02 Warner-Lambert Company Llc Modulateurs du recepteur androgene
KR20070009530A (ko) * 2003-09-24 2007-01-18 노파르티스 아게 증식성 질환 치료에 유용한 ｒａｆ-키나아제 억제제로서의1,4-이치환된 이소퀴놀린 유도체
US20070037796A1 (en) * 2003-11-25 2007-02-15 Barda David A 7-Phenyl-isoquinoline-5-sulfonylamino derivatives as inhibitors of akt (proteinkinase b)

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030114679A1 (en) * 2001-09-12 2003-06-19 Mceachern Ernest J. Synthesis of enantiomerically pure amino-substituted fused bicyclic rings
KR20070009530A (ko) * 2003-09-24 2007-01-18 노파르티스 아게 증식성 질환 치료에 유용한 ｒａｆ-키나아제 억제제로서의1,4-이치환된 이소퀴놀린 유도체
WO2005049576A1 (fr) * 2003-11-19 2005-06-02 Glaxo Group Limited Isoquinolines substituees utiles pour le traitement de maladies du type cancer et atherosclerose
WO2005049574A1 (fr) * 2003-11-20 2005-06-02 Warner-Lambert Company Llc Modulateurs du recepteur androgene
US20070037796A1 (en) * 2003-11-25 2007-02-15 Barda David A 7-Phenyl-isoquinoline-5-sulfonylamino derivatives as inhibitors of akt (proteinkinase b)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
WO2018146253A1 (fr) 2017-02-10 2018-08-16 INSERM (Institut National de la Santé et de la Recherche Médicale) Procédés et compositions pharmaceutiques pour le traitement de cancers associés à l'activation de la voie mapk
WO2019133810A1 (fr) 2017-12-28 2019-07-04 Tract Pharmaceuticals, Inc. Systèmes de culture de cellules souches pour cellules souches épithéliales colonnaires, et leurs utilisations

Also Published As

Publication number Publication date
WO2010032986A3 (fr) 2010-08-19
KR20100032496A (ko) 2010-03-26

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