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AR057377A1 - Derivados de cicloheptapiridina como inhibidores de tirosina quinasa. composiciones farmaceuticas - Google Patents

Derivados de cicloheptapiridina como inhibidores de tirosina quinasa. composiciones farmaceuticas

Info

Publication number
AR057377A1
AR057377A1 ARP060102571A ARP060102571A AR057377A1 AR 057377 A1 AR057377 A1 AR 057377A1 AR P060102571 A ARP060102571 A AR P060102571A AR P060102571 A ARP060102571 A AR P060102571A AR 057377 A1 AR057377 A1 AR 057377A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
heterocyclyl
alkenyl
cycloalkyl
Prior art date
Application number
ARP060102571A
Other languages
English (en)
Original Assignee
Merck & Co Inc
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 Merck & Co Inc filed Critical Merck & Co Inc
Publication of AR057377A1 publication Critical patent/AR057377A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04Ortho- or peri-condensed ring systems
    • C07D221/06Ring systems of three rings
    • C07D221/16Ring systems of three rings containing carbocyclic rings other than six-membered
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero rings
    • 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente se refiere a derivados de 5H-benzo[4,5]ciclohepta[1,2-b]piridina, que son utiles para tratar enfermedades proliferativas celulares, para tratar trastornos asociados con actividad de MET, y para inhibir la tirosina quinasa de receptor MET. La presente también se refiere a composiciones que comprenden estos compuestos, y a procedimientos para usarlos para tratar el cáncer en mamíferos. Reivindicacion 1: Un compuesto de formula (1), o una sal o estereoisomero farmacéuticamente aceptable del mismo, en la que una línea discontinua representa un doble enlace opcional; a es independientemente 0 o 1; b es independientemente 0 o 1; m es independientemente 0, 1, o 2; Rl se selecciona entre arilo, heterociclilo y NR10R11; estando dicho grupo arilo y heterociclilo opcionalmente sustituido con uno a cinco sustituyentes, cada sustituyente seleccionado independientemente entre R8; R5 se selecciona entre hidrogeno, alquilo C1-6, alquenilo C2-6, OH, -O-alquilo C1-6, -O- C(=O)alquiloC1-6, -O-arilo, S(O)mRa, -C(=O)NRl0R11, -NHS(O)2NR10R11 y NRl0R11, estando cada grupo alquilo, alquenilo y arilo opcionalmente sustituido con uno a cinco sustituyentes, cada sustituyente seleccionado independientemente entre R8; R8 independencia es: (C=O)aObalquiloC1-10, (C=O)aObarilo, alquenilo C2-C10, alquinilo C2-C10, (C=O)aObheterociclilo, CO2H, halo, CN, OH, ObperfluoroalquiloC1-6, Oa(C=O)bNRl0Rll, S(O)mRa, S(O)2NRl0R11, OS(=O)Ra, oxo, CHO, (N=O)R10R11, o (C=O)aObcicloalquiloC3-8, estando dichos grupos alquilo, arilo, alquenilo, alquinilo, heterociclilo, y cicloalquilo opcionalmente sustituido con uno, dos o tres sustituyentes seleccionado entre R9; R9 se selecciona independientemente entre: (C=O)aObalquiloC1-10, ObperfluoroalquiloC1-3, oxo, OH, halo, CN, alquenilo C2-10, alquinilo C2-10, (C=O)aObcicloalquiloC3-6, (C=O)aObalquilenC0-6-arilo, (C=O)aObalquilenC0-6-heterociclilo, (C=O)aObalquilenC0-6-N(Rb)2, C(O)Ra, alqulenC0-6-CO2Ra, C(O)H, alquilenC0-6-CO2H, C(O)N(Rb)2, S(O)mRa, y S(O)2NR10R11; estando dichos grupos alquilo, alquenilo, alquinilo, cicloalquilo, arilo, y heterociclilo opcionalmente sustituidos con uno, dos o tres sustituyentes seleccionados entre Rb, OH, alcoxi C1-6, halogeno, CO2H, CN, O(C=O)alquiloC1-6, oxo, y N(Rb)2; R10 y R11 se seleccionan independientemente entre: H, (C=O)ObalquiloC1-10, (C=O)ObcicloalquiloC3-8, (C=O)Obarilo, (C=O)Obheterociclilo, alquilo C1-10, arilo, alquenilo C2-10, alquinilo C2- 10, heterociclilo, cicloalquilo C3-8, SO2Ra, y (C=O)NRb2, estando dichos grupos alquilo, cicloalquilo, arilo, heterociclilo, alquenilo, y alquinilo opcionalmente sustituidos con uno, dos o tres sustituyentes seleccionados entre R8; o R10 y R11 pueden tomarse junto con el nitrogeno al que están unidos para formar un heterociclo monocíclico o bicíclico con 5-7 miembros en cada anillo y conteniendo opcionalmente, además del nitrogeno, uno o dos heteroátomos adicionales seleccionados entre N, O y S, estando dicho heterociclo monocíclico o bicíclico opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados entre R9; Ra se selecciona independientemente entre: alquilo C1-6, alquenilo C2-6, cicloalquilo C3-6, arilo, - alquilenC1-6-arilo, heterociclilo y -alquilenC1-6-heterociclilo; y Rb se selecciona independientemente entre: H, alquilo C1-6, arilo, -alquilenC1-6arilo, heterociclilo, -alquilenC1-6-heterociclilo, cicloalquilo C3-6, (C=O)OalquiloC1-6, (C=O)alquiloC1-6 o S(O)2Ra.
ARP060102571A 2005-06-23 2006-06-16 Derivados de cicloheptapiridina como inhibidores de tirosina quinasa. composiciones farmaceuticas AR057377A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US69322905P 2005-06-23 2005-06-23
US72906105P 2005-10-21 2005-10-21
US78947306P 2006-04-05 2006-04-05

Publications (1)

Publication Number Publication Date
AR057377A1 true AR057377A1 (es) 2007-11-28

Family

ID=37595817

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060102571A AR057377A1 (es) 2005-06-23 2006-06-16 Derivados de cicloheptapiridina como inhibidores de tirosina quinasa. composiciones farmaceuticas

Country Status (21)

Country Link
EP (1) EP1896422B1 (es)
KR (1) KR20080018907A (es)
AR (1) AR057377A1 (es)
AT (1) ATE520664T1 (es)
BR (1) BRPI0612518A2 (es)
CR (1) CR9579A (es)
CY (1) CY1112038T1 (es)
DO (1) DOP2006000143A (es)
EC (1) ECSP078017A (es)
IL (1) IL187895A0 (es)
MA (1) MA29643B1 (es)
MX (1) MX2007016533A (es)
NI (1) NI200700318A (es)
NO (1) NO20080417L (es)
NZ (1) NZ563711A (es)
PE (1) PE20070167A1 (es)
PL (1) PL1896422T3 (es)
PT (1) PT1896422E (es)
SI (1) SI1896422T1 (es)
TW (1) TW200738638A (es)
WO (1) WO2007002258A2 (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200813021A (en) * 2006-07-10 2008-03-16 Merck & Co Inc Tyrosine kinase inhibitors
US7893081B2 (en) * 2007-12-20 2011-02-22 Merck & Co., Inc. Tyrosine kinase inhibitors
EP2482803B1 (en) 2009-09-30 2021-12-22 Merck Sharp & Dohme (UK) Limited Formulations for c-met kinase inhibitors
CA2771338A1 (en) 2009-09-30 2011-04-07 Merck Sharp & Dohme Corp. Crystalline hydrochloride salts of c-met kinase inhibitors
EP2588107A1 (en) 2010-07-01 2013-05-08 Takeda Pharmaceutical Company Limited COMBINATION OF A cMET INHIBITOR AND AN ANTIBODY TO HGF AND/OR cMET
ES2764299T3 (es) 2014-12-09 2020-06-02 Inst Nat Sante Rech Med Anticuerpos monoclonales humanos contra AXL
WO2016135041A1 (en) 2015-02-26 2016-09-01 INSERM (Institut National de la Santé et de la Recherche Médicale) Fusion proteins and antibodies comprising thereof for promoting apoptosis
EP3942045A1 (en) 2019-03-21 2022-01-26 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE363473T1 (de) * 2001-09-19 2007-06-15 Pharmacia Corp Substituierte pyrazoloverbindungen zur behandlung von entzündungen
WO2003084931A1 (en) * 2002-04-02 2003-10-16 Merck & Co., Inc. 5h-benzo[4,5]cyclohepta[1,2-b]pyridine nmda/nr2b antagonists

Also Published As

Publication number Publication date
CR9579A (es) 2008-03-06
PL1896422T3 (pl) 2012-01-31
CY1112038T1 (el) 2015-11-04
EP1896422B1 (en) 2011-08-17
BRPI0612518A2 (pt) 2010-11-23
ATE520664T1 (de) 2011-09-15
MA29643B1 (fr) 2008-07-01
NZ563711A (en) 2010-12-24
EP1896422A2 (en) 2008-03-12
WO2007002258A2 (en) 2007-01-04
PE20070167A1 (es) 2007-04-16
IL187895A0 (en) 2008-03-20
ECSP078017A (es) 2008-01-23
NI200700318A (es) 2008-05-23
MX2007016533A (es) 2008-03-06
KR20080018907A (ko) 2008-02-28
PT1896422E (pt) 2011-11-08
SI1896422T1 (sl) 2011-11-30
NO20080417L (no) 2008-03-18
DOP2006000143A (es) 2007-02-28
WO2007002258A3 (en) 2007-06-07
TW200738638A (en) 2007-10-16

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