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AR061804A1 - Inhibidores de tirosina quinasa - Google Patents

Inhibidores de tirosina quinasa

Info

Publication number
AR061804A1
AR061804A1 ARP070102972A ARP070102972A AR061804A1 AR 061804 A1 AR061804 A1 AR 061804A1 AR P070102972 A ARP070102972 A AR P070102972A AR P070102972 A ARP070102972 A AR P070102972A AR 061804 A1 AR061804 A1 AR 061804A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
heterocyclyl
cycloalkyl
alkenyl
Prior art date
Application number
ARP070102972A
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 AR061804A1 publication Critical patent/AR061804A1/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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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
    • C07D401/14Heterocyclic 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
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

Son utiles para tratar enfermedades proliferativas celulares, para tratar trastornos asociados con actividad MET, y para inhibir la tirosina quinasa de receptor MET. Se refiere también a composiciones las cuales comprenden estos compuestos, y a procedimientos para tratar cáncer en mamíferos. Reivindicacion 1: Un compuesto de formula (1) o una sal farmacéuticamente aceptable o estereoisomero del mismo, en la que a es independientemente 0 o 1; b es independientemente 0 o 1; m es independientemente 0, 1 o 2; R1 está seleccionada de hidrogeno, OH, O-alquilo C1-6, -O-arilo, -O-heterociclilo, SH, -S-alquilo C1-6, -S-arilo, -S-heterociclilo, arilo, heterociclilo y NR8R9; dicho grupo alquilo, arilo y heterociclilo opcionalmente sustituidos con de uno a cinco sustituyentes, cada sustituyente independientemente seleccionados de R6; R2 y R3 están independientemente seleccionados de: hidrogeno, halo, (C=O)a-Ob-alquilo C1-10, (C=O)a-Ob-arilo, heterociclilo-(C=O)a-Ob, Ob- perfluoroalquilo C1-6, o cicloalquilo C3-8-(C=O)a-Ob, dichos alquilo, arilo, heterociclilo, y cicloalquilo opcionalmente sustituidos con uno, dos o tres sustituyentes seleccionados de R7; R4 y R5 están independientemente seleccionados de hidrogeno, alquilo C1-6, alquenilo C2-10, alquinilo C2-10, arilo, heterociclilo, OH, -O-alquilo C1-6, perfluoroalquilo C1-3, cada alquilo, alquenilo, alquinilo, heterociclilo y arilo opcionalmente sustituido con de uno a tres sustituyentes, cada sustituyente independientemente seleccionado de R6; R6 es independientemente: (C=O)a-Ob-alquilo C1-10, arilo-(C=O)a-Ob, alquenilo C2-10, alquinilo C2-10, heterociclilo-(C=O)a-Ob, CO2H, halo, CN, OH, Ob-perfluoroalquilo C1-6, Oa-(C=O)b-NR8R9, S(O)mRa, S(O)2NR8R9, OS(=O)Ra, oxo, CHO, (N=O)R8R9, o (C=O)a-Ob-cicloalquilo C3-8, dichos alquilo, arilo, alquenilo, alquinilo, heterociclilo, y cicloalquilo opcionalmente sustituidos con uno, dos o tres sustituyentes seleccionados de R7; R7 está independientemente seleccionado de: (C=O)a-Ob-alquilo C1-10, Ob-perfluoroalquilo C1-3, oxo, OH, halo, CN, alquenilo C2-10, alquinilo C2-10, (C=O)a-Ob-cicloalquilo C3-6, (C=O)a-Ob-alquileno C0-6-arilo, (C=O)a-Ob-alquileno C0-6-heterociclilo, (C=O)a-Ob-alquileno C0-6- N(Rb)2, C(O)Ra, alquileno C0-6-CO2Ra, C(O)H, alquileno C0-6-CO2H, C(O)N(Rb)2, S(O)mRa, y S(O)2NR8R9; dicho alquilo, alquenilo, alquinilo, cicloalquilo, arilo, y heterociclilo está opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados de Rb, OH, alcoxi C1-6, halogeno, CO2H, CN, O(C=O)alquilo C1-6, oxo, y N(Rb)2; R8 y R9 se seleccionan independientemente de: H, (C=O)Ob-alquilo C1-10, (C=O)Ob-cicloalquilo C3-8, (C=O)Ob-arilo, (C=O)Ob-heterociclilo, alquilo C1-10, arilo, alquenilo C2-10, alquinilo C2-10, heterociclilo, cicloalquilo C3-8, SO2Ra, y (C=O)NRb2, dicho alquilo, cicloalquilo, arilo, heterociclilo, alquenilo, y alquinilo está opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados de R6, o R8 y R9 se pueden tomar conjuntamente con el nitrogeno al cual se han anclado para formar un heterociclo monocíclico o bicíclico con 5-7 miembros en cada anillo y que contienen opcionalmente, además del nitrogeno, uno o dos heteroátomos adicionales seleccionados de N, O y S, dicho heterociclo monocíclico o bicíclico opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados de R7; Ra está independientemente seleccionado de: alquilo C1-6, alquenilo C2-6, cicloalquilo C3-6, arilo, alquileno C1-6-arilo, heterociclilo y alquileno C1-6-heterociclilo; y Rb está independientemente seleccionado de: H, alquilo C1-6, arilo, alquileno C1-6-arilo, heterociclo, alquileno C1-6-heterociclilo, cicloalquilo C3-6, (C=O)O-alquilo C1-6, (C=O)-alquilo C1-6 o S(O)2Ra.
ARP070102972A 2006-07-10 2007-07-03 Inhibidores de tirosina quinasa AR061804A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US81976406P 2006-07-10 2006-07-10

Publications (1)

Publication Number Publication Date
AR061804A1 true AR061804A1 (es) 2008-09-24

Family

ID=38923821

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070102972A AR061804A1 (es) 2006-07-10 2007-07-03 Inhibidores de tirosina quinasa

Country Status (24)

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US (2) US8222269B2 (es)
EP (1) EP2049494B1 (es)
JP (2) JP4203121B1 (es)
KR (1) KR20090026187A (es)
CN (1) CN101535268B (es)
AR (1) AR061804A1 (es)
AU (1) AU2007273081B2 (es)
BR (1) BRPI0713941A2 (es)
CA (1) CA2656578C (es)
CO (1) CO6190518A2 (es)
CR (1) CR10560A (es)
EC (1) ECSP099051A (es)
ES (1) ES2497493T3 (es)
GT (1) GT200900004A (es)
HN (1) HN2009000018A (es)
IL (1) IL196337A0 (es)
MA (1) MA30631B1 (es)
MX (1) MX2009000410A (es)
NO (1) NO20090608L (es)
PE (1) PE20080275A1 (es)
RU (1) RU2009104303A (es)
TW (1) TW200813021A (es)
WO (1) WO2008008310A2 (es)
ZA (1) ZA200900019B (es)

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US7893081B2 (en) 2007-12-20 2011-02-22 Merck & Co., Inc. Tyrosine kinase inhibitors
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CA2771338A1 (en) * 2009-09-30 2011-04-07 Merck Sharp & Dohme Corp. Crystalline hydrochloride salts of c-met kinase inhibitors
EP2482803B1 (en) * 2009-09-30 2021-12-22 Merck Sharp & Dohme (UK) Limited Formulations for c-met kinase inhibitors
DK2571878T3 (en) 2010-05-17 2019-02-11 Indian Incozen Therapeutics Pvt Ltd Hitherto unknown 3,5-DISUBSTITUTED-3H-IMIDAZO [4,5-B] PYRIDINE AND 3,5- DISUBSTITUTED -3H- [1,2,3] TRIAZOL [4,5-B] PYRIDINE COMPOUNDS AS MODULATORS OF PROTEIN CHINES
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
CN107082779A (zh) 2012-03-30 2017-08-22 理森制药股份公司 作为c‑met 蛋白激酶调节剂的新化合物
CA2880896C (en) 2012-06-26 2021-11-16 Del Mar Pharmaceuticals Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof
US11491154B2 (en) 2013-04-08 2022-11-08 Dennis M. Brown Therapeutic benefit of suboptimally administered chemical compounds
EP3027654B1 (en) * 2013-07-30 2019-09-25 Blueprint Medicines Corporation Pik3c2g fusions
WO2015017533A1 (en) * 2013-07-30 2015-02-05 Blueprint Medicines Corporation Ntrk2 fusions
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
EP4327879A3 (en) * 2016-06-17 2024-05-22 The Trustees of the University of Pennsylvania Compounds, compositions and methods for prevention and/or treatment of cancer
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

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Also Published As

Publication number Publication date
RU2009104303A (ru) 2010-08-20
ZA200900019B (en) 2009-11-25
WO2008008310A2 (en) 2008-01-17
US20090012076A1 (en) 2009-01-08
BRPI0713941A2 (pt) 2012-12-04
MA30631B1 (fr) 2009-08-03
CA2656578C (en) 2012-09-04
JP4203121B1 (ja) 2008-12-24
JP2009173622A (ja) 2009-08-06
HN2009000018A (es) 2011-01-24
AU2007273081B2 (en) 2011-04-07
AU2007273081A1 (en) 2008-01-17
CN101535268B (zh) 2012-11-14
IL196337A0 (en) 2009-09-22
KR20090026187A (ko) 2009-03-11
MX2009000410A (es) 2009-01-27
ECSP099051A (es) 2009-02-27
CO6190518A2 (es) 2010-08-19
EP2049494B1 (en) 2014-06-25
US8222269B2 (en) 2012-07-17
US8101603B2 (en) 2012-01-24
GT200900004A (es) 2010-04-13
JP2009512698A (ja) 2009-03-26
PE20080275A1 (es) 2008-04-03
CN101535268A (zh) 2009-09-16
ES2497493T3 (es) 2014-09-23
CR10560A (es) 2009-02-26
CA2656578A1 (en) 2008-01-17
EP2049494A2 (en) 2009-04-22
NO20090608L (no) 2009-04-14
US20090203684A1 (en) 2009-08-13
JP5245045B2 (ja) 2013-07-24
WO2008008310A3 (en) 2008-05-15
TW200813021A (en) 2008-03-16

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