WO2009150381A3 - Derives d'azacarbolines, leur preparation et leur utilisation therapeutique en tant qu'inhibiteurs de kinases - Google Patents

Derives d'azacarbolines, leur preparation et leur utilisation therapeutique en tant qu'inhibiteurs de kinases Download PDF

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Publication number
WO2009150381A3
WO2009150381A3 PCT/FR2009/051100 FR2009051100W WO2009150381A3 WO 2009150381 A3 WO2009150381 A3 WO 2009150381A3 FR 2009051100 W FR2009051100 W FR 2009051100W WO 2009150381 A3 WO2009150381 A3 WO 2009150381A3
Authority
WO
WIPO (PCT)
Prior art keywords
optionally substituted
branched
heterocycloalkyl
therapeutic use
linear
Prior art date
Application number
PCT/FR2009/051100
Other languages
English (en)
Other versions
WO2009150381A2 (fr
Inventor
Christopher Arendt
Didier Babin
Olivier Bedel
Thierry Gouyon
Mikhail Levit
Serge Mignani
Neil Moorcroft
David Papin
Ronghua Li
Original Assignee
Sanofi-Aventis
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
Priority to UAA201100324A priority Critical patent/UA101668C2/ru
Priority to CA2725093A priority patent/CA2725093A1/fr
Priority to EA201170002A priority patent/EA018945B1/ru
Priority to NZ589839A priority patent/NZ589839A/en
Priority to MX2010013699A priority patent/MX2010013699A/es
Priority to CN2009801313693A priority patent/CN102124007A/zh
Priority to BRPI0915204A priority patent/BRPI0915204A2/pt
Priority to JP2011513034A priority patent/JP2011522867A/ja
Application filed by Sanofi-Aventis filed Critical Sanofi-Aventis
Priority to EP09761932A priority patent/EP2303882A2/fr
Priority to US12/997,326 priority patent/US20110178053A1/en
Priority to AU2009259114A priority patent/AU2009259114B2/en
Publication of WO2009150381A2 publication Critical patent/WO2009150381A2/fr
Publication of WO2009150381A3 publication Critical patent/WO2009150381A3/fr
Priority to TNP2010000529A priority patent/TN2010000529A1/fr
Priority to ZA2010/08387A priority patent/ZA201008387B/en
Priority to IL209840A priority patent/IL209840A0/en
Priority to MA33499A priority patent/MA32460B1/fr

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/14Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/72Nitrogen atoms
    • C07D213/73Unsubstituted amino or imino radicals

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)

Abstract

Nouvelles azacarbolines de formule :(I) dans laquelle : R3, R4 représentent indépendamment l'un de l'autre H;hal; CF3; oxy substituée; alkoxy éventuellement substitué; amino éventuellement substitué; carbonyle substitué; carboxyle éventuellement substitué; amide éventuellement substitué; soufre tels que les sulfures, sulfoxides ou sulfones éventuellement substitués;C1-C10 alkyle linéaire, ramifié ou cyclique comportant éventuellement un hétéroatome éventuellement substitué;C2-C7 alkenyle linéaire, ramifié ou cyclique éventuellement substitué; C2-C6 alkynyle linéaire ou ramifié éventuellement substitué; aryle ou hétéroaryle éventuellement substitué;hétérocycloalkyle éventuellement substitué; R6 représente hétéroaryle, C(O)NR1aR1b, hétérocycloalkyle ou -C(O)hétérocycloalkyle tous éventuellement substitués; à l'état de base ou de sel d'addition à un acide. Utilisation en thérapeutique pour le traitement du cancer et procédés de synthèse.
PCT/FR2009/051100 2008-06-12 2009-06-11 Derives d'azacarbolines, leur preparation et leur utilisation therapeutique WO2009150381A2 (fr)

Priority Applications (15)

Application Number Priority Date Filing Date Title
EP09761932A EP2303882A2 (fr) 2008-06-12 2009-06-11 Derives d'azacarbolines, leur preparation et leur utilisation therapeutique en tant qu'inhibiteurs de kinases
CA2725093A CA2725093A1 (fr) 2008-06-12 2009-06-11 Derives d'azacarbolines, leur preparation et leur utilisation therapeutique
US12/997,326 US20110178053A1 (en) 2008-06-12 2009-06-11 Azacarboline derivatives, preparation method thereof and therapeutic use of same
MX2010013699A MX2010013699A (es) 2008-06-12 2009-06-11 Derivados de azacarbolinas, su preparacion y su uso terapeutico.
CN2009801313693A CN102124007A (zh) 2008-06-12 2009-06-11 氮杂咔啉衍生物、其制备方法和其作为激酶抑制剂的治疗用途
BRPI0915204A BRPI0915204A2 (pt) 2008-06-12 2009-06-11 derivados de azacarbolinas, a respectiva preparação e sua utilização terapêutica
JP2011513034A JP2011522867A (ja) 2008-06-12 2009-06-11 アザカルボリン誘導体、この調製およびキナーゼ阻害剤としてのこの治療上の使用
UAA201100324A UA101668C2 (ru) 2008-06-12 2009-06-11 Производные азакарболинов, способ их получения и применения в терапии
EA201170002A EA018945B1 (ru) 2008-06-12 2009-06-11 Производные азакарболинов, способ их получения и применение в терапии
NZ589839A NZ589839A (en) 2008-06-12 2009-06-11 Azacarboline derivatives, preparation thereof, and therapeutic use thereof as kinase inhibitors
AU2009259114A AU2009259114B2 (en) 2008-06-12 2009-06-11 Azacarboline derivatives, preparation thereof, and therapeutic use thereof as kinase inhibitors
TNP2010000529A TN2010000529A1 (fr) 2009-06-11 2010-11-12 Derives d'azacarbolines, leur preparation et leur utilisation therapeutique en tant qu'inhibiteurs de kinases
ZA2010/08387A ZA201008387B (en) 2008-06-12 2010-11-23 Azacarboline derivatives,preparation thereof,and therapeutic use thereof as kinase inhibitors
IL209840A IL209840A0 (en) 2008-06-12 2010-12-08 Azacarboline derivatives, preparation thereof, and therapeutic use thereof as kinase inhibitors
MA33499A MA32460B1 (fr) 2008-06-12 2011-01-07 Derives d'azacarbolines, leur preparation et leur utilisation therapeutique en tant qu'inhibiteurs de kinases

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR0803262 2008-06-12
FR08/03262 2008-06-12

Publications (2)

Publication Number Publication Date
WO2009150381A2 WO2009150381A2 (fr) 2009-12-17
WO2009150381A3 true WO2009150381A3 (fr) 2010-02-18

Family

ID=40445526

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/FR2009/051100 WO2009150381A2 (fr) 2008-06-12 2009-06-11 Derives d'azacarbolines, leur preparation et leur utilisation therapeutique

Country Status (26)

Country Link
US (1) US20110178053A1 (fr)
EP (1) EP2303882A2 (fr)
JP (1) JP2011522867A (fr)
KR (1) KR20110016998A (fr)
CN (1) CN102124007A (fr)
AR (1) AR072084A1 (fr)
AU (1) AU2009259114B2 (fr)
BR (1) BRPI0915204A2 (fr)
CA (1) CA2725093A1 (fr)
CO (1) CO6280536A2 (fr)
CR (1) CR11814A (fr)
DO (1) DOP2010000366A (fr)
EA (1) EA018945B1 (fr)
EC (1) ECSP10010670A (fr)
IL (1) IL209840A0 (fr)
MA (1) MA32460B1 (fr)
MX (1) MX2010013699A (fr)
NI (1) NI201000210A (fr)
NZ (1) NZ589839A (fr)
PE (1) PE20110122A1 (fr)
SV (1) SV2010003754A (fr)
TW (1) TW201002711A (fr)
UA (1) UA101668C2 (fr)
UY (1) UY31895A (fr)
WO (1) WO2009150381A2 (fr)
ZA (1) ZA201008387B (fr)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2009258124C1 (en) * 2008-06-11 2016-01-07 Genentech, Inc. Diazacarbazoles and methods of use
MY158927A (en) 2008-06-12 2016-11-30 Janssen Pharmaceutica Nv Diamino-pyridine, pyrimidine, and pyridazine modulators of the histamine h4 receptor
CA2756152A1 (fr) * 2009-03-24 2010-09-30 Sanofi Derives d'azacarbolines 9h-pyrrolo[2,3-b:5,4-c']dipyridine, leur preparation et leur utilisation therapeutique
FR2950891B1 (fr) * 2009-10-06 2012-11-09 Sanofi Aventis Derives d'azacarbolines 9h-pyrrolo[2,3-b:5,4-c']dipyridine, leur preparation et leur utilisation therapeutique
FR2953838B1 (fr) * 2009-12-10 2012-02-24 Sanofi Aventis Derives de 9h-beta-carboline (ou 9h-pyridino[3,4-b]indole) trisubstitues, leur preparation et leur utilisation therapeutique
US20110183938A1 (en) * 2009-12-16 2011-07-28 Genentech, Inc. 1,7-diazacarbazoles and methods of use
AU2014249192B2 (en) * 2013-03-11 2017-12-21 The Regents Of The University Of Michigan BET bromodomain inhibitors and therapeutic methods using the same
KR101652577B1 (ko) * 2013-04-19 2016-08-30 영남대학교 산학협력단 아미도피리딘올 유도체 또는 이의 약제학적 허용가능한 염 및 이를 유효성분으로 함유하는 혈관신생으로 인한 질환의 예방 또는 치료용 약학조성물
CN103408573B (zh) * 2013-07-12 2015-12-23 上海工程技术大学 硼酸衍生物及其制备方法和应用
WO2018137655A1 (fr) * 2017-01-25 2018-08-02 江苏豪森药业集团有限公司 Dérivé de pyrrolo-pyridine n-oxyde, son procédé de préparation et son utilisation
KR102700664B1 (ko) * 2017-08-07 2024-08-29 조인트 스탁 컴퍼니 “바이오케드” Cdk8/19 저해제로서 새로운 헤테로사이클릭 화합물
CR20200591A (es) 2018-05-04 2021-03-31 Incyte Corp Sales de un inhibidor de fgfr
WO2020072675A1 (fr) 2018-10-02 2020-04-09 Northwestern University Bêta-carbolines servant de modulateurs allostériques positifs du récepteur humain de la sérotonine 2c (5-ht2c)
CN116693449A (zh) 2022-03-04 2023-09-05 上海致根医药科技有限公司 用作tyk2抑制剂的化合物、其制备方法及其在医药上的应用

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007044779A1 (fr) * 2005-10-07 2007-04-19 Takeda San Diego, Inc. Inhibiteurs de kinase

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2009258124C1 (en) * 2008-06-11 2016-01-07 Genentech, Inc. Diazacarbazoles and methods of use

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007044779A1 (fr) * 2005-10-07 2007-04-19 Takeda San Diego, Inc. Inhibiteurs de kinase

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
CHENEY ET AL: "Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, ELSEVIER SCIENCE, GB, vol. 17, no. 6, 20 February 2007 (2007-02-20), pages 1679 - 1683, XP005895389, ISSN: 0960-894X *

Also Published As

Publication number Publication date
UA101668C2 (ru) 2013-04-25
UY31895A (es) 2010-01-29
AU2009259114B2 (en) 2013-05-23
MX2010013699A (es) 2011-02-23
NI201000210A (es) 2011-05-09
MA32460B1 (fr) 2011-07-03
CN102124007A (zh) 2011-07-13
EP2303882A2 (fr) 2011-04-06
NZ589839A (en) 2012-07-27
US20110178053A1 (en) 2011-07-21
IL209840A0 (en) 2011-02-28
KR20110016998A (ko) 2011-02-18
CA2725093A1 (fr) 2009-12-17
SV2010003754A (es) 2011-03-15
PE20110122A1 (es) 2011-03-07
WO2009150381A2 (fr) 2009-12-17
BRPI0915204A2 (pt) 2019-01-15
EA018945B1 (ru) 2013-11-29
JP2011522867A (ja) 2011-08-04
EA201170002A1 (ru) 2011-08-30
AU2009259114A1 (en) 2009-12-17
CO6280536A2 (es) 2011-05-20
ECSP10010670A (es) 2011-01-31
DOP2010000366A (es) 2010-12-31
TW201002711A (en) 2010-01-16
CR11814A (es) 2011-01-10
AR072084A1 (es) 2010-08-04
ZA201008387B (en) 2012-02-29

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