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PE20140192A1 - Derivados de bencimidazol como inhibidores de cinasa pi3 - Google Patents

Derivados de bencimidazol como inhibidores de cinasa pi3

Info

Publication number
PE20140192A1
PE20140192A1 PE2013000787A PE2013000787A PE20140192A1 PE 20140192 A1 PE20140192 A1 PE 20140192A1 PE 2013000787 A PE2013000787 A PE 2013000787A PE 2013000787 A PE2013000787 A PE 2013000787A PE 20140192 A1 PE20140192 A1 PE 20140192A1
Authority
PE
Peru
Prior art keywords
methyl
alkyl
benzhimidazole
kinase
inhibitors
Prior art date
Application number
PE2013000787A
Other languages
English (en)
Inventor
Junya Qu
Ralph A Rivero
Robert Sanchez
Rosanna Tedesco
Original Assignee
Glaxosmithkline Llc
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 Glaxosmithkline Llc filed Critical Glaxosmithkline Llc
Publication of PE20140192A1 publication Critical patent/PE20140192A1/es

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    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08—Radicals containing only hydrogen and carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/10—Radicals substituted by halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C—CHEMISTRY; METALLURGY
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    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/10—Heterocyclic 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 carbon chain containing aromatic rings
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D405/02—Heterocyclic 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 two hetero rings
    • C07D405/04—Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
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    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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 two hetero rings
    • C07D405/10—Heterocyclic 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 two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D417/02—Heterocyclic 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
    • C07D417/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/10—Heterocyclic 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 linked by a carbon chain containing aromatic rings

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

Abstract

SE REFIERE A DERIVADOS DE BENCIMIDAZOL COMO INHIBIDORES DE CINASA PI3 DE FORMULA I, DONDE: R1 ES H, ALQUILO C1-C6, ALCOXI, ENTRE OTROS; R2 ES H, -NHRa, ALCOXI, ENTRE OTROS; R3 ES ARILO, HETEROARILO ENTRE OTROS; R4 ES H O Ra, DONDE Ra ES ALQUILO C1-C3; R5 ES ALQUILO C1-C6 Y n ES 0-2. TAMBIEN HACE REFERENCIA A UN COMPUESTO DE FORMULA (I)(C); DONDE R6, R7 Y R8 SON ALQUILO C1-C3, HALOGENO, CF3, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 2-(1-METIL-ETIL)-6-(4-MORFOLINIL)-1-(1-NAFTALENIL-METIL)-1H-BENCIMIDAZOL-4-OL, 2-ETIL-6-(4-MORFOLINIL)-1-(1-NAFTALENIL-METIL)-1H-BENCIMIDAZOL-4-OL, 1- (2,3-DICLORO-FENIL)-METIL -2-(1-METIL-ETIL)-6-(4-MORFOLINIL)-1H-BENCIMIDAZOL-4-OL, ENTRE OTROS. REFERIDA ADEMAS A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON UTILES EN EL TRATAMIENTO DE CANCER.
PE2013000787A 2010-10-06 2011-09-23 Derivados de bencimidazol como inhibidores de cinasa pi3 PE20140192A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US39031410P 2010-10-06 2010-10-06
US201161528397P 2011-08-29 2011-08-29

Publications (1)

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PE20140192A1 true PE20140192A1 (es) 2014-02-24

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PE2013000787A PE20140192A1 (es) 2010-10-06 2011-09-23 Derivados de bencimidazol como inhibidores de cinasa pi3

Country Status (39)

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US (10) US20130196990A1 (es)
EP (2) EP3170813B1 (es)
JP (1) JP5719028B2 (es)
KR (1) KR101594002B1 (es)
CN (1) CN103124496B (es)
AR (1) AR083296A1 (es)
AU (1) AU2011312594B2 (es)
BR (1) BR112013008259A2 (es)
CA (1) CA2812608C (es)
CL (1) CL2013000935A1 (es)
CO (1) CO6700852A2 (es)
CR (1) CR20130192A (es)
CY (1) CY1118792T1 (es)
DK (1) DK2624696T3 (es)
DO (1) DOP2013000059A (es)
EA (1) EA022623B1 (es)
ES (2) ES2714384T3 (es)
HR (1) HRP20170279T1 (es)
HU (1) HUE033209T2 (es)
IL (1) IL225140A (es)
JO (1) JO3194B1 (es)
LT (1) LT2624696T (es)
MA (1) MA34591B1 (es)
ME (1) ME02663B (es)
MX (1) MX337662B (es)
MY (1) MY170236A (es)
NZ (1) NZ608069A (es)
PE (1) PE20140192A1 (es)
PH (1) PH12013500646A1 (es)
PL (1) PL2624696T3 (es)
PT (1) PT2624696T (es)
RS (1) RS55662B1 (es)
SG (1) SG188974A1 (es)
SI (1) SI2624696T1 (es)
SM (1) SMT201700158T1 (es)
TW (1) TWI513690B (es)
UY (1) UY33648A (es)
WO (1) WO2012047538A1 (es)
ZA (1) ZA201301951B (es)

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US10660898B2 (en) 2020-05-26
EP3170813A1 (en) 2017-05-24
US9156797B2 (en) 2015-10-13
SMT201700158T1 (it) 2017-05-08
EP2624696A1 (en) 2013-08-14
MA34591B1 (fr) 2013-10-02
CL2013000935A1 (es) 2013-07-05
CA2812608C (en) 2020-07-14
KR20130099142A (ko) 2013-09-05
US20120088767A1 (en) 2012-04-12
US8674090B2 (en) 2014-03-18
US20150246889A1 (en) 2015-09-03
US9872860B2 (en) 2018-01-23
LT2624696T (lt) 2017-03-10
MX337662B (es) 2016-03-14
CN103124496A (zh) 2013-05-29
US20130197221A1 (en) 2013-08-01
PT2624696T (pt) 2017-03-21
JO3194B1 (ar) 2018-03-08
SI2624696T1 (sl) 2017-04-26
US20180263994A1 (en) 2018-09-20
CO6700852A2 (es) 2013-06-28
NZ608069A (en) 2014-06-27
TWI513690B (zh) 2015-12-21
ES2616238T3 (es) 2017-06-12
EP3170813B1 (en) 2018-12-12
WO2012047538A1 (en) 2012-04-12
DOP2013000059A (es) 2013-05-31
US8435988B2 (en) 2013-05-07
IL225140A (en) 2016-09-29
US20140378456A1 (en) 2014-12-25

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