DK2987796T3 - Halogen-substituerede boronophthalider til behandling af infektioner - Google Patents

Halogen-substituerede boronophthalider til behandling af infektioner Download PDF

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DK2987796T3
DK2987796T3 DK15171026.6T DK15171026T DK2987796T3 DK 2987796 T3 DK2987796 T3 DK 2987796T3 DK 15171026 T DK15171026 T DK 15171026T DK 2987796 T3 DK2987796 T3 DK 2987796T3
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species
formulation
compound
product
pharmaceutical formulation
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Stephen Baker
Tsutomu Akama
Carolyn Bellinger-Kawahara
Vincent Hernandez
Karin Hold
James Leyden
Kirk Maples
Jacob J Plattner
Virginia Sanders
Yong-Kang Zhang
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Anacor Pharmaceuticals Inc
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    • C07F5/02—Boron compounds
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Claims (46)

1. Produkt til anvendelse som et medikament, hvor produktet indgives fra en eller to gange om dagen op til 3 eller 4 gange om dagen og er udvalgt fra en forbindelse med følgende struktur:
og farmaceutisk acceptable salte deraf, eventuelt hvor saltet er et baseadditionssalt opnået ved at bringe den neutrale form af en sådan forbindelse i kontakt med en tilstrækkelig mængde af den ønskede base i et egnet inert opløsningsmiddel.
2. Produkt til anvendelse som et medikament, hvor produktet indgives fra en eller to gange om dagen op til 3 eller 4 gange om dagen og er udvalgt fra en forbindelse med følgende struktur:
og farmaceutisk acceptable salte deraf, eventuelt hvor saltet er et baseadditionssalt opnået ved at bringe den neutrale form af en sådan forbindelse i kontakt med en tilstrækkelig mængde af den ønskede base i et egnet inert opløsningsmiddel.
3. Formulering til farmaceutisk anvendelse, hvor formuleringen indgives fra en eller to gange om dagen op til 3 eller 4 gange om dagen, omfattende: (a) en farmaceutisk acceptabel excipiens; og (b) en forbindelse med en struktur:
eller et farmaceutisk acceptabelt salt deraf, eventuelt hvor saltet er et baseadditionssalt opnået ved at bringe den neutrale form af en sådan forbindelse i kontakt med en tilstrækkelig mængde af den ønskede base i et egnet inert opløsningsmiddel.
4. Farmaceutisk formulering ifølge krav 3, hvor forbindelsen forekommer i en form, som er et element udvalgt blandt et hydrat, et solvat med en alkohol, et addukt med en aminoforbindelse og et addukt med en syre.
5. Farmaceutisk formulering ifølge krav 4, hvor forbindelsen er i form af et solvat med propylenglycol.
6. Farmaceutisk formulering ifølge et hvilket som helst af kravene 3 til 5, som er en topisk formulering.
7. Farmaceutisk formulering ifølge krav 6, hvor forbindelsen forekommer i den farmaceutiske formulering i en koncentration fra 0,5 % til 15 % w/v.
8. Farmaceutisk formulering ifølge krav 6, hvor forbindelsen forekommer i den farmaceutiske formulering i en koncentration fra 0,1 % til 12,5 % w/v, og eventuelt yderligere hvor forbindelsen forekommer i den farmaceutisk formulering i en koncentration på fra ca. 1 % til ca. 10 %; og eventuelt yderligere hvor forbindelsen forekommer i en koncentration fra ca. 1 % til ca. 5 % w/v.
9. Farmaceutisk formulering ifølge krav 7 eller krav 8, hvor forbindelsen forekommer i formuleringen i en koncentration fra ca. 2 % til ca. 8 % w/v.
10. Farmaceutisk formulering ifølge krav 7 eller krav 8, hvor forbindelsen forekommer i formuleringen i en koncentration fra ca. 4 % til ca. 9 % w/v.
11. Farmaceutisk formulering ifølge et hvilket som helst af kravene 6 til 10, omfattende fluide eller halvfaste vehikler udvalgt fra gruppen bestående af: polymerer, fortykningsmidler, buffere, neutraliserende stoffer, chelaterings-midler, konserveringsmidler, overfladeaktive stoffer eller emulgatorer, antioxi- danter, vokser eller olier, blødgøringsmidler, solpræparater og et opløsningsmiddel eller blandet opløsningsmiddelsystem.
12. Farmaceutisk formulering ifølge krav 11, omfattende et opløsningsmiddel eller blandet opløsningsmiddelsystem.
13. Farmaceutisk formulering ifølge et hvilket som helst af kravene 6 til 12, hvor den farmaceutiske formulering er et element udvalgt blandt en lotion, creme, gel, stick, spray, salve, pasta, skum eller mousse.
14. Farmaceutisk formulering ifølge et hvilket som helst af kravene 6 til 12, hvor formuleringen er en lak.
15. Farmaceutisk formulering ifølge et hvilket som helst af kravene 6 til 14, som yderligere omfatter en gelfasebærer.
16. Farmaceutisk formulering ifølge et hvilket som helst af kravene 6 til 14, som yderligere omfatter et egnet viskositetsforøgende middel.
17. Farmaceutisk formulering ifølge et hvilket som helst af kravene 6 til 12, hvor formuleringen indbefatter en simpel opløsning, som indbefatter en alkohol og eventuelt indbefatter en alkohol og vand.
18. Farmaceutisk formulering ifølge krav 17, hvor alkoholen er ethanol.
19. Farmaceutisk formulering ifølge krav 17 eller krav 18, hvor alkoholen er polypropylenglycol.
20. Farmaceutisk formulering ifølge krav 17 eller krav 18, hvor alkoholen er propylenglycol.
21. Farmaceutisk formulering ifølge et hvilket som helst af kravene 6 til 12, som er en spray, der tilvejebringer produktet i en vandig og/eller alkoholisk opløsning.
22. Farmaceutisk formulering ifølge et hvilket som helst af kravene 6 til 21, som omfatter et chelateringsmiddel, eventuelt hvor chelateringsmidlet er udvalgt fra gruppen udvalgt blandt citronsyre, ethylendiamintetraeddikesyre (EDTA), ethylenglycol-bis(beta-aminoethylether)-N,N,N',N'-tetraeddikesyre (EGTA) og 8-amino-2-[(2-amino-5-methylphenoxy)methyl]-6- methoxyquinolin-N,N,N',N'-tetraeddikesyre, tetrakaliumsalt (QUIN-2).
23. Farmaceutisk formulering ifølge krav 22, hvor chelateringsmidlet er ethylendiamintetraeddikesyre.
24. Farmaceutisk formulering ifølge krav 22 eller krav 23, hvor chelateringsmidlet forekommer i en mængde fra 0,005 til 2 vægt-%.
25. Formulering ifølge et hvilket som helst af kravene 6 til 24, hvor den topiske formulering afgiver forbindelsen fra det dorsale lag af neglepladen til neglele-jet.
26. Produkt ifølge krav 1 eller krav 2 eller formulering ifølge et hvilket som helst af kravene 3 til 25, til anvendelse til behandling eller forebyggelse af en kutan infektion hos et dyr, eventuelt hvor infektionen er en kutan svampeinfektion.
27. Produkt ifølge krav 1 eller krav 2 eller formulering ifølge et hvilket som helst af kravene 3 til 25, til anvendelse til inhibering af væksten af, eller til at dræbe, en svamp i eller på overfladen af et dyr.
28. Produkt ifølge krav 1 eller krav 2 eller formulering ifølge et hvilket som helst af kravene 3 til 25, til anvendelse til behandling eller forebyggelse af en infektion hos et dyr.
29. Produkt eller formulering ifølge krav 28, hvor infektionen er en systemisk infektion eller en ungual eller periungual infektion.
30. Produkt eller formulering ifølge krav 28, hvor infektionen er forårsaget af en bakterie; eventuelt hvor bakterien er en grampositiv bakterie; eventuelt hvor den grampositive bakterie er element udvalgt blandt Staphylococcus-arter, Streptococcus-arter, Bacillus-arter, Mycobacterium-arter, Corynebacterium- arter (Propionibacterium-arter), Clostridium-arter, Actinomyces-arter, Entero-coccus-arter og Streptomyces-arter-, eventuelt hvor bakterien er en gramnegativ bakterie; eventuelt hvor den gramnegative bakterie er et element udvalgt blandt Acinetobacter-arter, Neisseria-arter, Pseudomonas-arter, Brucella-ar-ter, Agrobacterium-arter, Bordetella-arter, Escherichia-arter, Shigella-arter, Yersinia-arter, Salmonella-arter, Klebsiella-arter, Enterobacter-arter, Ha-emophilus-arter, Pasteurella-arter, Streptobacillus-arter, Spirochetal-arter, Campylobacter-arter, Vibrio-arter og Helicobacter-arter.
31. Produkt eller formulering ifølge krav 28, hvor infektionen er forårsaget af en svamp eller gær.
32. Produkt eller formulering ifølge krav 31, hvor svampen eller gæren er et element udvalgt blandt Candida-arter, Trichophyton-arter, Microsporum-arter, Aspergillus-arter, Cryptococcus-arter, Blastomyces-arter, Coccidioides-arter, Histoplasma-arter, Paracoccidioides-arter, Phycomycetes-arter, Malassezia-arter, Fusarium-arter, Epidermophyton-arter, Scytalidium-arter, Scopulariop-s/s-arter, Alternaria-arter, Penicillium-arter, Phialophora-arter, Rhizopus-arter, Scedosporium-arter og Zygomycetes-arter.
33. Produkt eller formulering ifølge krav 31, hvor svampen eller gæren er et element udvalgt blandt Aspergillus fumigatus, Blastomyces dermatitidis, Candida albicans, Candida glabrata, Candida krusei, Cryptococcus neoformans, Candida parapsilosis, Candida tropicalis, Coccidioides immitis, Epidermophyton floccosum, Fusarium solani, Histoplasma capsulatum, Malassezia furfur, Malassezia pachydermatis, Malassezia sympodialis, Microsporum audouinii, Microsporum canis, Microsporum gypseum, Paracoccidioides brasiliensis, Trichophyton mentagrophytes, Trichophyton rubrum og Trichophyton tonsurans.
34. Produkt eller formulering ifølge krav 31, hvor svampen eller gæren er et element udvalgt blandt Trichophyton concentricum, Trichophyton violaceum, Trichophyton schoenleinii, Trichophyton verrucosum, Trichophyton soudanense, Microsporum gypseum, Microsporum equinum, Candida guHlier- mondii, Malassezia globosa, Malassezia obtusa, Malassezia restricta, Malassezia slooffiae og Aspergillus flavus.
35. Produkt eller formulering ifølge krav 31, hvor svampen eller gæren er en dermatophyt.
36. Produkt eller formulering ifølge krav 28, hvor infektionen er et element udvalgt blandt chloronychia, paronychia, erysipeloid, gonorré, swimming-pool-granulom, spedalskhed, akut bakteriel perionyxis, sporotrichose, syfilis, tuberculosis verrucosa cutis, tularæmi, mykotisk keratitis, ekstension-oculomykose, endogen oculomykose, lobomykose, mycetom, piedra, pityriasis versicolor, tinea corporis, tinea cruris, tinea pedis, tinea barbae, tinea capitis, tinea nigra, otomykose, tinea favosa, chromomykose og tinea imbricata.
37. Produkt eller formulering ifølge krav 28 eller krav 29, hvor infektionen er onychomykose.
38. Produkt eller formulering ifølge krav 37, hvor onychomykose er tinea unguium.
39. Produkt eller formulering ifølge krav 37, hvor onychomykose er tånegl-ony-chomykose.
40. Produkt eller formulering ifølge krav 38 eller krav 39, hvor tinea unguium eller tånegl-onychomykose er forårsaget af en dermatophyt udvalgt blandt Trichophyton rubrum og Trichophyton mentagrophytes.
41. Produkt eller formulering ifølge krav 28 eller krav 29, hvor dyret er menneske, kreatur, ged, svin, får, hest, ko, tyr, hund, marsvin, gerbil, kanin, kat, kylling eller kalkun.
42. Produkt eller formulering ifølge krav 41, hvor dyret er et menneske.
43. Produkt ifølge et hvilket som helst af kravene 1 og 2 eller 26 til 42 eller farmaceutiske formuleringer ifølge et hvilket som helst af kravene 4 til 42, som er til anvendelse ved topisk påføring.
44. Produkt eller formulering ifølge et hvilket som helst af kravene 28 til 42, hvor forbindelsen eller formuleringen skal indgives på et sted, der er udvalgt blandt hud, negl, hår, hov og klo.
45. Farmaceutisk formulering ifølge et hvilket som helst af kravene 3 til 44, som endvidere indbefatter et yderligere farmaceutisk virksomt middel, f.eks. et anti-inflammatorisk middel og/eller et middel til behandling af akne.
46. Farmaceutisk formulering ifølge et hvilket som helst af de foregående krav, hvor forbindelsen er i form af syren.
DK15171026.6T 2005-02-16 2006-02-16 Halogen-substituerede boronophthalider til behandling af infektioner DK2987796T3 (da)

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