DK2467377T3 - Substituerede benzoazepiner som modulatorer af toll-lignende receptorer - Google Patents

Substituerede benzoazepiner som modulatorer af toll-lignende receptorer Download PDF

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DK2467377T3
DK2467377T3 DK10810563.6T DK10810563T DK2467377T3 DK 2467377 T3 DK2467377 T3 DK 2467377T3 DK 10810563 T DK10810563 T DK 10810563T DK 2467377 T3 DK2467377 T3 DK 2467377T3
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mmol
propyl
benzo
mixture
compound
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DK10810563.6T
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James Jeffry Howbert
Gregory Dietsch
Robert Hershberg
Laurence E Burgess
Joseph P Lyssikatos
Brad Newhouse
Hong Woon Yang
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Ventirx Pharmaceuticals Inc
Array Biopharma Inc
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    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16—Benzazepines; Hydrogenated benzazepines
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
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    • C07D401/14—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 three or more hetero rings
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    • 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
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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
    • C07D403/12—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 chain containing hetero atoms as chain links
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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
    • 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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  • Chemical & Material Sciences (AREA)
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  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
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Claims (14)

1. Forbindelse med formlen I:
eller en tautomer, en enantiomer, eller et salt, fortrinsvis et farmaceutisk acceptabelt salt, deraf, hvor: Y er -(0)x(CH2)yR11; x er valgt blandt 0 og 1; y er valgt blandt 0,1,2 og 3; R11 er valgt blandt aryl, heteroaryl og en mættet eller delvist mættet heterocykel, hvor aryl eller heteroaryl er substitueret med T, når x er 0; R12 er valgt blandt (C3-Ci2)-cycloalkyl og aryl; T er valgt blandt en heterocykel, -(CHR7)zOR9, -(0)U(CH2)SC(0)R8, -OSO2R13 og -CH(OH)CH2OH; R7 er H eller -OH; R8 er valgt blandt -OR10 og (Ci-Ci2)-alkyl; R9 er valgt blandt (Ci-Ci2)-alkyl og H; R10 er valgt blandt (Ci-Ci2)-alkyl, -(CH2)R12 og hydrogen, hvor (Ci-Ci2)-alkyl eventuelt er substitueret med halogen, amin, (Ci-Ci2)-alkylamin eller di((Ci-Ci2)-alkyl)amin; R13 er valgt blandt -OH, (Ci-Ci2)-alkyl, CF3, (C3-Ci2)-cycloalkyl, en heterocykel, aryl og heteroaryl; u er valgt blandt 0 og 1; z er valgt blandt 1, 2 og 3; s er valgt blandt 1 og 2; R5 er valgt blandt -NR3R4 og -OR10; R3 og R4 er uafhængigt valgt blandt H, (Ci-Ci2)-alkyl, -(0)q(CH2)rP; hvor (Ci-Ci2)-alkyl eventuelt er substitueret med en eller flere -OH; q er valgt blandt 0 og 1; r er valgt blandt 0,1,2 og 3; P er valgt blandt aryl, -SO2R6 og en heterocykel; og R6 er valgt blandt -NH2, -NH((Ci-Ci2)-alkyl), -N((Ci-Ci2)-alkyl)2.
2. Forbindelse ifølge krav 1, som har formlen II:
eller en tautomer, en enantiomer eller et salt, fortrinsvis et farmaceutisk acceptabelt salt, deraf, hvor: W er valgt blandt N, C-T og CH.
3. Forbindelse ifølge krav 2, som har formlen Ila eller llb:
en tautomer, en enantiomer, eller et salt, fortrinsvis et farmaceutisk acceptabelt salt, deraf.
4. Forbindelse ifølge krav 1, som har formlen VI:
eller en tautomer, en enantiomer, eller et salt deraf, hvor: R11 er valgt blandt aryl og en mættet eller delvist mættet heterocykel, hvor aryl er substitueret med T; T er valgt blandt en heterocykel, -(0)U(CH2)SC(0)R8 og -CH(0H)CH20H; R8 er valgt blandt -OR10 og (Ci-Ci2)-alkyl; R10 er valgt blandt (Ci-Ci2)-alkyl, -(CH2)R12 og hydrogen, hvor (Ci-Ci2)-alkyl eventuelt er substitueret med halogen, amin, (Ci-Ci2)-alkylamin eller di((Ci-Ci2)-alkyl)amin; R12 er valgt blandt (C3-Ci2)-cycloalkyl og aryl; u er valgt blandt 0 og 1; s er valgt blandt 1 og 2; og R3 og R4 uafhængigt er (Ci-Ci2)-alkyl; hvor (Ci-Ci2)-alkyl eventuelt er substitueret med en eller flere -OFI.
5. Forbindelse ifølge krav 4, hvor: R11 er valgt blandt aryl og en mættet eller delvist mættet heterocykel, hvor aryl er substitueret med T; T er valgt blandt en heterocykel og -(0)U(CH2)SC(0)R8, som fortrinsvis er valgt blandt -(0)u(CH2)sC(0)R8 og -CH(OH)CH2OH; R8 er valgt blandt -OR10 og (Ci-Ci2)-alkyl; R10 er valgt blandt (Ci-Ci2)-alkyl, -(CFhJR12 og hydrogen, hvor (Ci-Ci2)-alkyl eventuelt er substitueret med halogen, amin, (Ci-Ci2)-alkylamin eller di((Ci-Ci2)-alkyl)amin; R12 er valgt blandt (C3-Ci2)-cycloalkyl og aryl; u er valgt blandt 0 og 1; s er valgt blandt 1 og 2; og R3 og R4 uafhængigt er (Ci-Ci2)-alkyl; hvor (Ci-Ci2)-alkyl eventuelt er substitueret med en eller flere -OH.
6. Forbindelse ifølge krav 1, som er valgt fra gruppen bestående af:
og tautomerer, enantiomerer og salte, fortrinsvis farmaceutisk acceptable salte deraf.
7. Forbindelse ifølge krav 6, som er valgt fra gruppen bestående af:
og tautomerer, enantiomerer og salte, fortrinsvis farmaceutisk acceptable salte deraf.
8. Forbindelse ifølge krav 6, som er valgt fra gruppen bestående af:
og tautomerer, enantiomerer og salte, fortrinsvis farmaceutisk acceptable salte deraf.
9. Forbindelse ifølge krav 6, som er valgt fra gruppen bestående af:
og tautomerer, enantiomerer og salte, fortrinsvis farmaceutisk acceptable salte deraf.
10. Forbindelse valgt fra gruppen bestående af:
11. Kit til behandling af en TLR7- og/eller TLR8-medieret tilstand, hvilket kit omfatter: a) en farmaceutisk sammensætning, som omfatter en forbindelse ifølge et hvilket som helst af kravene 1 til 10 eller en tautomer, en enantiomer, eller et salt, fortrinsvis et farmaceutisk acceptabelt salt, deraf; og b) eventuelt en brugsanvisning.
12. Farmaceutisk sammensætning, som omfatter en forbindelse ifølge et hvilket som helst af kravene 1 til 10 eller en tautomer, en enantiomer, eller et salt, fortrinsvis et farmaceutisk acceptabelt salt, deraf, sammen med et farmaceutisk acceptabelt fortyndingsmiddel eller en farmaceutisk acceptabel bærer.
13. Forbindelse ifølge krav 1 til 10 eller en tautomer, en enantiomer, elleret salt deraf, fortrinsvis et farmaceutisk acceptabelt salt deraf, til anvendelse ved behandling af en TLR7- og/eller TLR8-medieret tilstand.
14. Forbindelse ifølge krav 1 til 10 eller en tautomer, en enantiomer, elleret salt, fortrinsvis et farmaceutisk acceptabelt salt, deraf, til anvendelse ved modulering afen patients immunsystem.
DK10810563.6T 2009-08-18 2010-08-18 Substituerede benzoazepiner som modulatorer af toll-lignende receptorer DK2467377T3 (da)

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US23496909P 2009-08-18 2009-08-18
US23558609P 2009-08-20 2009-08-20
PCT/US2010/045934 WO2011022508A2 (en) 2009-08-18 2010-08-18 Substituted benzoazepines as toll-like receptor modulators

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EP (2) EP2467377B1 (da)
JP (2) JP5756804B2 (da)
CN (2) CN105669553A (da)
AU (2) AU2010284240B2 (da)
BR (1) BR112012003757A2 (da)
CA (1) CA2771609C (da)
DK (1) DK2467377T3 (da)
ES (1) ES2620629T3 (da)
HR (1) HRP20170404T1 (da)
HU (1) HUE032626T2 (da)
IL (1) IL218193A (da)
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