DK2688403T3 - Opioidreceptorligander og fremgangsmåder til anvendelse og fremstilling af samme - Google Patents

Opioidreceptorligander og fremgangsmåder til anvendelse og fremstilling af samme Download PDF

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DK2688403T3
DK2688403T3 DK12760456.9T DK12760456T DK2688403T3 DK 2688403 T3 DK2688403 T3 DK 2688403T3 DK 12760456 T DK12760456 T DK 12760456T DK 2688403 T3 DK2688403 T3 DK 2688403T3
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compound
alkyl
pharmaceutically acceptable
acceptable salt
formula
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Dennis Yamashita
Dimitar Gotchev
Philip Pitis
Xiao-Tao Chen
Guodong Liu
Catherine C K Yuan
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Trevena Inc
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
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    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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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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  • Urology & Nephrology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (20)

1. Forbindelse med en formel af Formel IV-1, eller et farmaceutisk acceptabelt salt deraf,:
hvor: R21 og R22 er uafhængigt H eller CFb; A4 er en eventuelt substitueret cykel af formlen C(CH2)n, hvor n = 2-5, hvor den eventuelle substitution er halo, cyano, C1-C6 alkyl, C1-C6 forgrenet alkyl, halogeneret C1-C6 alkyl, hydroxyl, C1-C6 alkyloxy, amino, eller C1-C6 alkylamino; B3 er H eller et eventuelt substitueret C1-C6 alkyl, hvor den eventuelle substitution er halo, hydroxy eller C1-C3 alkoxy; B4 er Ci-Ce alkylen; Di er en eventuelt substitueret monocyklisk eller bicyklisk aryl eller heteroaryl, hvor hver ring er en 5-, 6- eller 7-leddet ring og den eventuelle substitution er halo, cyano, C1-C6 alkyl, Ci-Ce forgrenet alkyl, halogeneret C1-C6 alkyl, hydroxyl, C1-C6 alkyloxy, amino, eller C1-C6 alkylamino; og B5 er en eventuelt substitueret monocyklisk eller bicyklisk aryl eller heteroaryl, hvor hver ring er en 5-, 6- eller 7-leddet ring og den eventuelle substitution er halo, cyano, C1-C6 alkyl, C1-C6 forgrenet alkyl, halogeneret C1-C6 alkyl, hydroxyl, C1-C6 alkyloxy, amino, eller C1-C6 alkylamino.
2. Forbindelsen ifølge krav 1, eller et farmaceutisk acceptabelt salt deraf, der har strukturen af Formel VIII:
hvor R26 og R27 er uafhængigt H eller en isotop deraf.
3. Forbindelsen ifølge krav 2, eller et farmaceutisk acceptabelt salt deraf, hvor forbindelsen har en formel af Formel IX
4. Forbindelsen ifølge kravene 2 eller 3, eller et farmaceutisk acceptabelt salt deraf, hvor forbindelsen har en formel af Formel VII-1
5. Forbindelsen ifølge et hvilket som helst af kravene 2-4, eller et farmaceutisk acceptabelt salt deraf, hvor forbindelsen har en formel af Formel X
6. Forbindelsen ifølge et hvilket som helst af kravene 1-5, eller et farmaceutisk acceptabelt salt deraf, hvor Di er et eventuelt substitueret phenyl, hvor den eventuelle substitution er halo, cyano, C1-C6 alkyl, C1-C6 forgrenet alkyl, halogeneret Ci-Ce alkyl, hydroxyl, Ci-Ce alkyloxy, amino, eller Ci-Ce alkylamino eller et eventuelt substitueret pyridyl, hvor den eventuelle substitution er halo, cyano, Ci-Ce alkyl, Ci-Ce forgrenet alkyl, halogeneret Ci-Ce alkyl, hydroxyl, Ci-Ce alkyloxy, amino, eller Ci-Ce alkylamino.
7. Forbindelsen ifølge et hvilket som helst af kravene 1-5, eller et farmaceutisk acceptabelt salt deraf, hvor Bs er ent eventuelt substitueret monocyklisk eller bicyklisk heteroaryl, hvor hver ring er en 5-, 6- eller 7-leddet ring og den eventuelle substitution er halo, cyano, C1-C6 alkyl, C1-C6 forgrenet alkyl, halogeneret C1-C6 alkyl, hydroxyl, C1-C6 alkyloxy, amino, eller C1-C6 alkylamino.
8. Forbindelsen ifølge et hvilket som helst af kravene 1-5, eller et farmaceutisk acceptabelt salt deraf, hvor Bs er et eventuelt substitueret aryl eller heteroaryl valgt fra gruppen bestående af
4
hvor den eventuelle substitution er halo, cyano, C1-C6 alkyl, C1-C6 forgrenet alkyl, halogeneret C1-C6 alkyl, hydroxyl, C1-C6 alkyloxy, amino, eller C1-C6 alkylamino.
9. Forbindelsen ifølge kravene 1-5, eller et farmaceutisk acceptabelt salt deraf, hvor B5 er valgt fra gruppen bestående af
hvor R.23, R.24, og R30 er hver uafhængigt null, H, OH, halo, forgrenet eller ikke-forgrenet Ci-Ce alkyl, cyano, Ci-Ce alkoxy, amino, Ci-Ce haloalkyl, eller, R23 og R24 danner sammen et aryl, et heteroaryl eller en cykel, der er bundet til et eller flere af atomerne af Bs; og R25 er H eller et eventuelt substitueret forgrenet eller ikke-forgrenet alkyl, hvor den eventuelle substitution er halo, hydroxy eller C1-C3 alkoxy.
10. Forbindelsen ifølge krav 9, eller et farmaceutisk acceptabelt salt deraf, hvor R23, R24, og R30 er hver uafhængigt Η, NH2, OH, Cl, Br, F, I, OMe, CN, eller CH3.
11. Forbindelsen ifølge krav 9, eller et farmaceutisk acceptabelt salt deraf, hvor B5 er
12. Forbindelsen ifølge krav 9 eller 11, eller et farmaceutisk acceptabelt salt deraf, hvor R23 er Ci-Ce alkoxy.
13. Forbindelsen ifølge et hvilket som helst af kravene 1-12, eller et farmaceutisk acceptabelt salt deraf, hvor B3 er H eller C1-C6 alkyl.
14. Forbindelsen ifølge krav 1, eller et farmaceutisk acceptabelt salt deraf, der har formlen af:
15. Forbindelsen ifølge krav 1, eller et farmaceutisk acceptabelt salt deraf, der har formlen af:
16. Forbindelsen ifølge krav 1, eller et farmaceutisk acceptabelt salt deraf, der har formlen af:
17. Forbindelsen ifølge krav 1, eller et farmaceutisk acceptabelt salt deraf, der har formlen af:
18. Farmaceutisk sammensætning omfattende en forbindelse, eller et farmaceutisk acceptabelt salt deraf, ifølge et hvilket som helst af kravene 1-17 og en farmaceutisk acceptabel bærer.
19. Forbindelse eller et farmaceutisk acceptabelt salt deraf, eller sammensætning ifølge et hvilket som helst af kravene 1-18 til anvendelse i behandlingen af smerte.
20. Fremgangsmåde til fremstilling af en forbindelse, eller et farmaceutisk acceptabelt salt deraf, ifølge krav 2, hvor R26 og R27 er H, hvilken fremgangsmåde omfatter: at bringe
5 under egnede forhold til at danne en forbindelse, der har strukturen af
DK12760456.9T 2011-03-23 2012-03-23 Opioidreceptorligander og fremgangsmåder til anvendelse og fremstilling af samme DK2688403T3 (da)

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US201161466809P 2011-03-23 2011-03-23
US201261596808P 2012-02-09 2012-02-09
PCT/US2012/030327 WO2012129495A1 (en) 2011-03-23 2012-03-23 Opioid receptor ligands and methods of using and making same

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US (8) US8835488B2 (da)
EP (3) EP2688403B1 (da)
JP (6) JP5912169B2 (da)
KR (3) KR102129247B1 (da)
CN (1) CN103702561B (da)
AU (2) AU2012230761B2 (da)
CA (1) CA2830742C (da)
CY (1) CY1119057T1 (da)
DK (2) DK2688403T3 (da)
EA (1) EA025456B1 (da)
ES (2) ES2632009T3 (da)
HK (1) HK1250984A1 (da)
HR (1) HRP20171021T1 (da)
HU (2) HUE054055T2 (da)
IL (4) IL228506A (da)
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ME (1) ME02754B (da)
PL (2) PL3290415T3 (da)
PT (2) PT3290415T (da)
RS (1) RS56111B1 (da)
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WO (1) WO2012129495A1 (da)

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