ME02663B - Derivati benzimidazola kao inhibitori pi3 kinaze - Google Patents

Derivati benzimidazola kao inhibitori pi3 kinaze

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Publication number
ME02663B
ME02663B MEP-2017-59A MEP5917A ME02663B ME 02663 B ME02663 B ME 02663B ME P5917 A MEP5917 A ME P5917A ME 02663 B ME02663 B ME 02663B
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Montenegro
Prior art keywords
cancer
leukemia
cell
lymphoma
pharmaceutically acceptable
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MEP-2017-59A
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German (de)
English (en)
French (fr)
Inventor
Junya Qu
Ralph Rivero
Robert Sanchez
Rosanna Tedesco
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Glaxosmithkline Llc
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Publication of ME02663B publication Critical patent/ME02663B/me

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    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • 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
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    • 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
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    • 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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    • C07D403/04—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
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    • 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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    • 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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    • C07D413/02—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
    • C—CHEMISTRY; METALLURGY
    • 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)
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  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
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  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (14)

1.Jedinjenje formule (Ia) koje je 2-metil-1-{[2-metil-3-(trifluorometil)fenil]metil}-6-(4-morfolinil) 1H-benzimidazol-4-karboksilna kiselina, ili njegova farmaceutski prihvatljiva so.
2.Jedinjenje prema zahtevu 1 formule (Ia) koje je 2-metil-1-{[2-metil-3-(trifluorometil)fenil]metil}-6-(4-morfolinil) 1H-benzimidazol-4-karboksilna kiselina.
3.Farmaceutski prihvatljiva so jedinjenja formule (Ia) prema zahtevu 1.
4.Farmaceutski prihvatljiva so jedinjenja formule (Ia) prema zahtevu 3, gde je so 1 : 1 tris so.
5.Farmaceutska kompozicija koja sadrži jedinjenje formule (Ia) ili njegovu farmaceutski prihvatljivu so prema bilo kom od zahteva 1-4 i farmaceutski prihvatljiv nosač.
6.Farmaceutska kompozicija prema zahtevu 5 za upotrebu u lečenju osetljive neoplazme kod sisara kojima je to potrebno.
7.Jedinjenje formule (Ia) ili njegova farmaceutski prihvatljiva so prema bilo kom od zahteva 1-4 za upotrebu u terapiji.
8.Kombinacija (a) 2-metil-1-{[2-metil-3-(trifluorometil)fenil]metil}-6-(4-morfolinil)-1H-benzimidazol- 4-karboksilne kiseline ili njene farmaceutski prihvatljive soli i (b) bar jednog anti-neoplastičnog sredstva; za upotrebu u lečenju kancera.
9.Jedinjenje formule (Ia) ili njegove farmaceutski prihvatljive soli prema bilo kom od zahteva 1-4, ili farmaceutske kompozicije prema zahtevu 5, ili kombinacije prema zahtevu 8, za upotrebu u lečenju osetljive neoplazme na nedostatak PTEN izabrane između moždanih (glioma), glioblastoma, leukemija, Bannayan-Zonana-ovog sindroma, Cowden-ove bolesti, Lhermitte-Duclos-ove bolesti, kancera grudi, zapaljenskog kancera grudi, kolorektalnog kancera, Wilm-ovog tumora, Ewing-ov sarkoma, rabdomiosarkoma, ependimoma, meduloblastoma, kancera creva, kancera glave i vrata, kancera bubrega, kancera pluća, kancera jetre, melanoma, karcinoma skvamoznih ćelija, kancera jajnika, kancera pankreasa, kancera prostate, sarkoma, kancera, osteosarkoma, tumora gigantskih ćelija kosti, kancera tiroidee, limfoblasne leukemije t-ćelija, hronične mijeloidne leukemije, hronične limfocitne leukemije, leukemije dlakavih ćelija, akutne leukemija limfoblasta, akutne mijeloidne leukemije, hronične leukemije neutrofila, akutne limfoblastne leukemije T ćelija, plazmacitoma, leukemije imunoblastnih velikih ćelija, leukemije mantle ćelija, višestrukog mijeloma, leukemije megakarioblasta, akutne megakariocitne leukemije, promijelocitne leukemije, eritroleukemija, malignog limfoma, hodžkinovog limfoma, nehodžkinovog limfoma, limfoblastičnog limfoma T ćelija, Burkit-ovog limfoma, folikularnog limfoma, neuroblastoma, kancera bešike, urotelijalnog kancera, kancera vulve, cervikalnog kancera, kancera endometrijuma, kancera bubrega, mezotelioma, kancera jednjaka, kancera pljuvačnih žlezda, hepatocelularnog kancera, kancera želudca, kancera nazofaringsa, bukalnog kancerkancer usta, GIST (gastrointestinalnog stromalnog tumora), i kancera testisa.
10.Jedinjenje formule (Ia) ili njegova farmaceutski prihvatljiva so za upotrebu, ili farmaceutska kompozicija za upotrebu, ili kombinacija za upotrebu, prema zahtevu 9, gde neoplazma u vezi sa nedostatkom PTEN je izabrana između kancera prostate kancera nemalih ćelija pluća, kancera endometrijuma, kancera želudca, melanoma, kancera glave i vrata, kancera grudi, uključujući trostuko negativni kancer grudi i gliom.
11.Jedinjenje formule (Ia) ili njegove farmaceutski prihvatljive soli za upotrebu, ili farmaceutska kompozicija za upotrebu, ili kombinacija za upotrebu, prema zahtevu 10, gde pomenuti kancer prostate je hormonski refraktorni kancer prostate.
12.Upotreba jedinjenja formule (Ia), ili njegove farmaceutski prihvatljive soli, prema bilo kom od zahteva 1-4 u proizvodnji leka za upotrebu u lečenju PTEN izabrane između moždanih (glioma), glioblastoma, leukemija, Bannayan-Zonana-ovog sindroma, Cowden-ove bolesti, Lhermitte-Duclos-ove bolesti, kancera grudi, zapaljenskog kancera grudi, kolorektalnog kancera, Wilm-ovog tumora, Ewing-ov sarkoma, rabdomiosarkoma, ependimoma, meduloblastoma, kancera creva, kancera glave i vrata, kancera bubrega, kancera pluća, kancera jetre, melanoma, karcinoma skvamoznih ćelija, kancera jajnika, kancera pankreasa, kancera prostate, sarkoma, kancera, osteosarkoma, tumora gigantskih ćelija kosti, kancera tiroidee, limfoblasne leukemije t-ćelija, hronične mijeloidne leukemije, hronične limfocitne leukemije, leukemije dlakavih ćelija, akutne leukemija limfoblasta, akutne mijeloidne leukemije, hronične leukemije neutrofila, akutne limfoblastne leukemije T ćelija, plazmacitoma, leukemije imunoblastnih velikih ćelija, leukemije mantle ćelija, višestrukog mijeloma, leukemije megakarioblasta, akutne megakariocitne leukemije, promijelocitne leukemije, eritroleukemija, malignog limfoma, hodžkinovog limfoma, nehodžkinovog limfoma, limfoblastičnog limfoma T ćelija, Burkit-ovog limfoma, folikularnog limfoma, neuroblastoma, kancera bešike, urotelijalnog kancera, kancera vulve, cervikalnog kancera, kancera endometrijuma, kancera bubrega, mezotelioma, kancera jednjaka, kancera pljuvačnih žlezda, hepatocelularnog kancera, kancera želudca, kancera nazofaringsa, bukalnog kancerkancer usta, GIST (gastrointestinalnog stromalnog tumora), i kancera testisa.
13.Upotreba prema zahtevu 12, gde pomenuta osetljiva neoplazma na nedostatak PTEN je izabrana između kancera prostate kancera nemalih ćelija pluća, kancera endometrijuma, kancera želudca, melanoma, kancera glave i vrata, kancera grudi, uključujući trostuko negativni kancer grudi i gliom.
14. Upotreba prema zahtevu 13, gde je kancer prostate hormonski refraktorni kancer prostate.
MEP-2017-59A 2010-10-06 2011-09-23 Derivati benzimidazola kao inhibitori pi3 kinaze ME02663B (me)

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US39031410P 2010-10-06 2010-10-06
US201161528397P 2011-08-29 2011-08-29
EP11831214.9A EP2624696B1 (en) 2010-10-06 2011-09-23 Benzimidazole derivatives as pi3 kinase inhibitors
PCT/US2011/052857 WO2012047538A1 (en) 2010-10-06 2011-09-23 Benzimidazole derivatives as pi3 kinase inhibitors

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