PE20160204A1 - Compuestos y composiciones como inhibidores de la mek - Google Patents

Compuestos y composiciones como inhibidores de la mek

Info

Publication number
PE20160204A1
PE20160204A1 PE2016000238A PE2016000238A PE20160204A1 PE 20160204 A1 PE20160204 A1 PE 20160204A1 PE 2016000238 A PE2016000238 A PE 2016000238A PE 2016000238 A PE2016000238 A PE 2016000238A PE 20160204 A1 PE20160204 A1 PE 20160204A1
Authority
PE
Peru
Prior art keywords
methyl
compounds
compositions
mek inhibitors
imidazo
Prior art date
Application number
PE2016000238A
Other languages
English (en)
Inventor
Samajdar Susanta
Gary Bock Mark
Ramulu Poddutoori
Henrik Moebitz
Kumar Panigrahi Sunil
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of PE20160204A1 publication Critical patent/PE20160204A1/es

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
    • C07D471/02Heterocyclic 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
    • 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
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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

Landscapes

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

Abstract

La presente invencion se relaciona con compuestos de la formula I: Capaces de inhibir la actividad de MEK. Donde N es 0, 1, 2 o 3, R1 es i), ii), etc. R2 es cloro, metilo, etc. R3a es ciano-metilo, 2-hidroxi-etilo, etc. R4 es hidrogeno, halo, etc. R5 es hidrogeno y metilo. Son compuestos preferidos: 1-((3S,4S)- 4-(8-(2-cloro-4-(pirimidin-2-iloxi)fenil)-7-fluoro-2-metil-1H- imidazo[4,5-c]quinolin-1 il)-3-fluoropiperidin-1-il)-2Hidroxietanona; 8-(2-cloro-4-(pirimidim- 2- iloxi)fenil)- 7-fluoro-1-(1- (2-metoxietil)piperidin-4-il)-2-metil-1H-imidazo[4,5-c]quinolina. La invencion proporciona ademas un procedimiento para la preparacion de compuestos que son utiles en el manejo de enfermedades hiperproliferitivas similares al cancer
PE2016000238A 2013-08-14 2014-08-14 Compuestos y composiciones como inhibidores de la mek PE20160204A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN2418DE2013 2013-08-14
IN1686DE2014 2014-06-24

Publications (1)

Publication Number Publication Date
PE20160204A1 true PE20160204A1 (es) 2016-04-27

Family

ID=51844790

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016000238A PE20160204A1 (es) 2013-08-14 2014-08-14 Compuestos y composiciones como inhibidores de la mek

Country Status (33)

Country Link
US (3) US9227969B2 (es)
EP (1) EP3033343B1 (es)
JP (1) JP6473453B2 (es)
KR (1) KR102354208B1 (es)
CN (1) CN105473588B (es)
AP (1) AP2016008981A0 (es)
AU (1) AU2014307593C1 (es)
BR (1) BR112016001783B1 (es)
CA (1) CA2921300C (es)
CL (1) CL2016000150A1 (es)
CR (1) CR20160072A (es)
CU (1) CU20160020A7 (es)
DO (1) DOP2016000047A (es)
EA (1) EA029093B1 (es)
ES (1) ES2714718T3 (es)
GE (1) GEP201706725B (es)
HK (1) HK1219271A1 (es)
IL (1) IL243349A0 (es)
MX (1) MX359401B (es)
NI (1) NI201600014A (es)
PE (1) PE20160204A1 (es)
PH (1) PH12016500003A1 (es)
PL (1) PL3033343T3 (es)
PT (1) PT3033343T (es)
SG (1) SG11201510727VA (es)
SV (1) SV2016005153A (es)
TN (1) TN2015000574A1 (es)
TR (1) TR201902709T4 (es)
TW (1) TW201536782A (es)
UA (1) UA116566C2 (es)
UY (1) UY35704A (es)
WO (1) WO2015022662A1 (es)
ZA (1) ZA201509337B (es)

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