DK2624696T3 - Benzimidazolderivater som pi3-kinaseinhibitorer - Google Patents

Benzimidazolderivater som pi3-kinaseinhibitorer Download PDF

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DK2624696T3
DK2624696T3 DK11831214.9T DK11831214T DK2624696T3 DK 2624696 T3 DK2624696 T3 DK 2624696T3 DK 11831214 T DK11831214 T DK 11831214T DK 2624696 T3 DK2624696 T3 DK 2624696T3
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cancer
leukemia
compound
cell
formula
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DK11831214.9T
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Junya Qu
Ralph Rivero
Robert Sanchez
Rosanna Tedesco
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Glaxosmithkline Llc Corp Service Company
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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
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    • 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
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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
    • C07D235/24—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
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • 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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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • 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
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D405/04—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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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    • C07—ORGANIC CHEMISTRY
    • 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
    • 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
    • C07D413/04—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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    • 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
    • C07D417/04—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

Claims (14)

1. Forbindelse med formel (la)
som er 2-methyl-1 -{[2-methyl-3-(trifluormethyl)phenyl]methyl}-6-(4- morpholinyl)-1 H-benzimidazol-4-carboxylsyre eller et farmaceutisk accepta-belt salt deraf.
2. Forbindelse ifølge krav 1 med formel (la) som er
2-methyl-1 -{[2-methyl-3-(trifluormethyl)phenyl]methyl}-6-(4- morpholinyl)-1 H-benzimidazol-4-carboxylsyre.
3. Farmaceutisk acceptabelt salt af forbindelsen med formel (la) ifølge krav 1.
4. Farmaceutisk acceptabelt salt af forbindelsen med formel (la) ifølge krav 3, hvor saltet er 1:1 Trissalt.
5. Farmaceutisk sammensætning, som omfatter en forbindelse med formel (la) eller et farmaceutisk acceptabelt salt deraf ifølge et hvilket som helst af kravene 1 -4 og en farmaceutisk acceptabel bærer.
6. Farmaceutisk sammensætning ifølge krav 5 til anvendelse ved behandling af en modtagelig neoplasme hos et pattedyr med behov herfor.
7. Forbindelse med formel (la) eller et farmaceutisk acceptabelt salt deraf ifølge et hvilket som helst af kravene 1-4 til anvendelse i terapi.
8. Kombination af (a) 2-methyl-1-{[2-methyl-3-(trifluormethyl)phenyl]methyl}-6-(4-morpholinyl)-1 H-benzimidazol-4-carboxylsyre eller et farmaceutisk acceptabelt salt deraf og (b) mindst et anti-neoplastisk middel; til anvendelse ved behandling af cancer.
9. Forbindelse med formel (la) eller et farmaceutisk acceptabelt salt deraf ifølge et hvilket som helst af kravene 1-4, eller en farmaceutisk sammensæt-ning ifølge krav 5, eller en kombination ifølge krav 8, til anvendelse ved behandling af en PTEN-deficient følsom neoplasme udvalgt blandt hjerne (gli-omer), glioblastomer, leukæmier, Bannayan-Zonanas syndrom, Cowdens sygdom, Lhermitte-Duclos-sygdom, brystcancer, inflammatorisk brystcancer, kolorektal cancer, Wilms tumor, Ewings sarkom, rhabdomyosarkom, epen-dymom, medulloblastom, coloncancer, hoved- og halscancer, nyrecancer, lungecancer, levercancer, melanom, pladecellekarcinom, ovariecancer, pan-creascancer, prostatacancer, sarkom, cancer, osteosarkom, kæmpecelletu-mor i knogle, thyroideacancer, lymfatisk T-celle-leukæmi, kronisk myeloid leukæmi, kronisk lymfatisk leukæmi, hårcelleleukæmi, akut lymfatisk leukæ-mi, akut myeloid leukæmi, kronisk neutrofil leukæmi, akut lymfatisk T-celle-leukæmi, plasmacytom, immunoblastisk storcellet leukæmi, mantle celle-leukæmi, myelomatose, megakaryoblastleukæmi, akut megakaryocytleukæ-mi, promyelocytleukæmi, erythroleukæmi, malignt lymfom, Hodgkins lymfom, non-Hodgkins lymfom, lymfoblastært T-celle-lymfom, Burkitts lymfom, folliku-lært lymfom, neuroblastom, blærecancer, urotelial cancer, vulvacancer, cer-vixcancer, endometriecancer, renal cancer, mesotheliom, øsofaguscancer, spytkirtelcancer, hepatocellulær cancer, gastrisk cancer, nasopharynxcancer, kindcancer, mundcancer, GIST (gastrointestinal stromal tumor) og testikel-cancer.
10. Forbindelse med formel (la) eller et farmaceutisk acceptabelt salt deraf til anvendelse, eller en farmaceutisk sammensætning til anvendelse, eller en kombination til anvendelse, ifølge krav 9, hvor den PTEN-deficiente neoplasme er udvalgt blandt prostatacancer, ikke-småcellet lungecancer, endometriecancer, gastrisk cancer, melanom, hoved- og halscancer, brystcancer, herunder triple-negativ brystkræft, og gliom.
11. Forbindelse med formel (la) eller et farmaceutisk acceptabelt salt deraf til anvendelse, eller en farmaceutisk sammensætning til anvendelse, eller en kombination til anvendelse, ifølge krav 10, hvor prostatacanceren er hormon-refraktær prostatacancer.
12. Anvendelse af en forbindelse med formel (la) eller et farmaceutisk acceptabelt salt deraf, ifølge et hvilket som helst af kravene 1-4 til fremstilling af et lægemiddel til anvendelse ved behandling af en PTEN-deficient følsom neo-plasme, som er udvalgt blandt hjerne (gliomer), glioblastomer, leukæmier, Bannayan-Zonanas syndrom, Cowdens sygdom, Lhermitte-Duclos-sygdom, brystcancer, inflammatorisk brystcancer, kolorektal cancer, Wilms tumor, Ewings sarkom, rhabdomyosarkom, ependymom, medulloblastom, colon-cancer, hoved- og halscancer, nyrecancer, lungecancer, levercancer, mela-nom, pladecellekarcinom, ovariecancer, pancreascancer, prostatacancer, sarkom, cancer, osteosarkom, kæmpecelletumor i knogle, thyroideacancer, lymfatisk T-celle-leukæmi, kronisk myeloid leukæmi, kronisk lymfatisk leu-kæmi, hårcelleleukæmi, akut lymfatisk leukæmi, akut myeloid leukæmi, kronisk neutrofil leukæmi, akut lymfatisk T-celle-leukæmi, plasmacytom, im-munoblastisk storcellet leukæmi, mantle celle-leukæmi, myelomatose, mega-karyoblastleukæmi, akut megakaryocytleukæmi, promyelocytleukæmi, eryt-hroleukæmi, malignt lymfom, Hodgkins lymfom, non-Hodgkins lymfom, lym-foblastært T-celle-lymfom, Burkitts lymfom, follikulært lymfom, neuroblastom, blærecancer, urotelial cancer, vulvacancer, cervixcancer, endometriecancer, renal cancer, mesotheliom, øsofaguscancer, spytkirtelcancer, hepatocellulær cancer, gastrisk cancer, nasopharynxcancer, kindcancer, mundcancer, GIST (gastrointestinal stromal tumor) og testikelcancer.
13. Anvendelse ifølge krav 12, hvor den PTEN-deficiente følsomme neopla-sme er udvalgt blandt prostatacancer, ikke-småcellet lungecancer, endometriecancer, gastrisk cancer, melanom, hoved- og halscancer, brystcancer, herunder triple-negativ brystkræft, og gliom.
14. Anvendelse ifølge krav 13, hvor prostatacanceren er hormonrefraktær prostatacancer.
DK11831214.9T 2010-10-06 2011-09-23 Benzimidazolderivater som pi3-kinaseinhibitorer DK2624696T3 (da)

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

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EP (2) EP2624696B1 (da)
JP (1) JP5719028B2 (da)
KR (1) KR101594002B1 (da)
CN (1) CN103124496B (da)
AR (1) AR083296A1 (da)
AU (1) AU2011312594B2 (da)
BR (1) BR112013008259A2 (da)
CA (1) CA2812608C (da)
CL (1) CL2013000935A1 (da)
CO (1) CO6700852A2 (da)
CR (1) CR20130192A (da)
CY (1) CY1118792T1 (da)
DK (1) DK2624696T3 (da)
DO (1) DOP2013000059A (da)
EA (1) EA022623B1 (da)
ES (2) ES2714384T3 (da)
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ME (1) ME02663B (da)
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MY (1) MY170236A (da)
NZ (1) NZ608069A (da)
PE (1) PE20140192A1 (da)
PL (1) PL2624696T3 (da)
PT (1) PT2624696T (da)
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SG (1) SG188974A1 (da)
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