Gluconic acid derivatives for use in the treatment and/or prevention of microbial infections
AssigneeGedea Biotech AB
InventorsUlf Ellervik, Olov Sterner, Helena Strevens, Sophie Manner
Life of this patent
Estimating the term…
Abstract
Pharmaceutical compositions and methods of using said pharmaceutical compositions are provided herein. A method of preventing preterm birth in a pregnant individual is also provided, said method comprising administering to said individual a pharmaceutical composition comprising a compound of Formula XX or a lactone thereof of formula XIX or XXI and preventing said preterm birth by said administration.
Claims120
A compound of Formula I,
- or a lactone thereof, wherein
- R is selected from the group consisting of —H, -alkyl, —C(O) alkyl and phenyl;
- R′ is independently selected from the group consisting of —OR, —H and halogen;
- and
- n is an integer 1, 2 or 3,
- for use in the treatment and/or prevention of a microbial infection, with the proviso that if the microbial infection is a fungal infection, then the compound of Formula I is not a compound of Formula (XIV)
- or a lactone thereof.
The compound for use according to any one of the preceding claims, wherein the microbial infection is an infection selected from the group consisting of a bacterial infection, a mixed fungal and bacterial infection and a viral infection, or a combination thereof.
The compound for use according to any one of the preceding claims, wherein the microbial infection is a bacterial infection.
The compound for use according to any one of the preceding claims, wherein the microbial infection is a urogenital infection.
The compound for use according to any one of the preceding claims, wherein the microbial infection is a vaginal infection.
The compound for use according to any one of the preceding claims, wherein the bacterial infection is bacterial vaginosis.
The compound for use according to any one of the preceding claims, wherein the infection is dermatitis and/or eczema.
The compound for use according to any one of the preceding claims, wherein the infection is a secondary infection of dermatitis or eczema.
The compound for use according to any one of the preceding claims, wherein the infection is acne and/or acneiform conditions.
The compound for use according to any one of the preceding claims, wherein the infection is furunculosis, carbunculosis or folliculitis.
The compound for use according to any one of the preceding claims, wherein the infection is impetigo or erysipelas.
The compound for use according to any one of the preceding claims, wherein the infection is cheilitis.
The compound for use according to any one of the preceding claims, wherein the bacterial infection is periodontitis.
The compound for use according to any one of the preceding claims, wherein the infection is secondary to secondary to colonization of group A or B streptococci multiresistant bacteria.
The compound for use according to any one of the preceding claims, wherein the infection is perianal streptococcal dermatitis.
The compound for use according to any one of the preceding claims, wherein the infection is intertriginous dermatitis or paronychia.
The compound for use according to any one of the preceding claims, wherein the bacterial infection is selected from the group consisting of caused by Gardnerella vaginalis-, Chlamydia trachomatis-, Neisseria gonorrhoeae-, Treponema pallidum(syphilis)-, Atopobium vaginae-, Prevotella spp-, Mobiluncus spp-, Peptostreptococcus spp-, Poryphyromonas spp-, Mycoplasma hominis-, Bacteroides spp-, Ureaplasma urealyticum-, Streptococcus spp-, Enterobacteriaceae-, Enterococci-, Staphylococcus spp-, Propionibacterium-, Escherichia coli-, Klebsiella-, Staphylococcus epidermidis-, Staphylococcus aureus-, Pseudomonas aeruginosa-, Acetinobacter baumanii-, Streptococcus pyogenes-, Streptococcus agalactiae-, Beta-Hemolytic Streptococci Groups C and G-and/or Porphyromonas gingivalis infection.
The compound for use according to any one of the preceding claims, wherein the infection is a Saccharomyces cerevisiae infection.
The compound for use according to any one of the preceding claims, wherein the fungal infection is a mycosis.
The compound for use according to any one of the preceding claims, wherein the mycosis is selected from the group consisting of Dermatophytosis, Candidiasis, Coccidioidomycosis, Histoplasmosis, Blastomycosis, Paracoccidioidomycosis, Sporotrichosis, Chromomycosis and phaeomycotic abscess, Aspergillosis, Cryptococcosis, Zygomycosis, and Mycetoma.
The compound for use according to any one of the preceding claims, wherein the mycosis is Candidiasis.
The compound for use according to any one of the preceding claims, wherein the Candidiasis is selected from the group consisting of Candidiasis of vulva and vagina;
- Candidiasis of skin and nail;
- Candidiasis of urogenital sites;
- Candidiasis of gastrointestinal sites;
- Candidal stomatitis;
- Candida of the breast and nipple;
- Pulmonary candidiasis;
- Candidal meningitis;
- Candidal endocarditis;
- and Candidal sepsis.
The compound for use according to any one of the preceding claims, wherein the mycosis is Dermatophytosis.
The compound for use according to any one of the preceding claims, wherein the Dermatophytosis is selected from the group consisting of Tinea unguium;
- toenail onychomycosis;
- Tinea inguinalis;
- Tinea amiantacea;
- Tinea pedis;
- Tinea manuum;
- Tinea barbae, Tinea capitis;
- Tinea corporis;
- Tinea imbricata;
- and Tinea cruris.
The compound for use according to any one of the preceding claims, wherein the mycosis is Pityriasis versicolor.
The compound for use according to any one of the preceding claims, wherein the fungal infection is selected from the group consisting of Candida albicans-, Candida krusei-, Candida glabrata-, Candida tropicalis-, Trichophyton verrucosum-, Trichophyton rubrum-, Trichophyton violaceum-, Trichophyton tonsurans-, Microsporum canis-, Malassezia-and Aspergillus infection.
The compound for use according to any one of the preceding claims, wherein the infection is an infection in a mammal.
The compound for use according to any one of the preceding claims, wherein the mammal is a human.
The compound for use according to any one of the preceding claims, wherein the human is a woman.
The compound for use according to any one of the preceding claims, wherein the woman is pregnant.
The compound for use according to any one of the preceding claims, wherein the infection is an infection of the face, scalp, torso and/or groin.
The compound for use according to any one of the preceding claims, the infection is an infection of infected skin wounds.
The compound for use according to any one of the preceding claims, wherein the infection is an infection of the feet.
The compound for use according to any one of the preceding claims, wherein the infection of feet is secondary to ingrown toenails or blisters of the feet.
The compound for use according to any one of the preceding claims, wherein the infection is a secondary infection arising after animal bite.
The compound for use according to any one of the preceding claims, wherein the infection is a secondary infection arising after insect bites, mosquito bites, tic bites, erythema migrans or lymphadenosis benigna cutis.
The compound for use according to any one of the preceding claims, wherein the infection is a secondary infection of herpes simplex.
The compound for use according to any one of the preceding claims, wherein the infection is a secondary infection of herpes zoster or varicella zoster.
The compound for use according to any one of the preceding claims, wherein the infection is a secondary infection of injury to the skin.
The compound for use according to any one of the preceding claims, wherein the infection is blepharitis.
The compound for use according to any one of the preceding claims, wherein the infection is conjunctivitis.
The compound for use according to any one of the preceding claims, wherein the infection is a vaginitis or a cervicitis.
The compound for use according to any one of the preceding claims, wherein the infection is trichomoniasis.
The compound for use according to any one of the preceding claims, wherein the infection is a Trichomonas vaginalis infection.
The compound for use according to any one of the preceding claims, wherein the microbial infection is a viral infection.
The compound for use according to any one of the preceding claims, wherein the viral infection is HIV.
The compound for use according to any one of the preceding claims, wherein the compound of Formula I is a lactone thereof.
The compound for use according to any one of the preceding claims, wherein alkyl is a C1 to C20 aliphatic chain wherein one or more hydrogens is optionally substituted for —OH, ═O, or phenyl, and wherein one or more of the CH2-groups of the aliphatic chain is optionally substituted for O, S, or NH.
The compound for use according to any one of the preceding claims, wherein at least one of R′is —OR.
The compound for use according to any one of the preceding claims, wherein at least two, such as at least three, such as at least four, such as at least five, such as at least six of R′ is OR.
The compound for use according to any one of the preceding claims, wherein R′ is —OR.
The compound for use according to any one of the preceding claims, wherein at least one of R′ is —OH.
The compound for use according to any one of the preceding claims, wherein no more than one of R′ is —H, such as no more than two of R′ is —H.
The compound for use according to any one of the preceding claims, wherein the compound of Formula I is selected from the group consisting of
The compound for use according to any one of the preceding claims, wherein the compound of Formula I is selected from the group consisting of
The compound for use according to any one of the preceding claims, wherein alkyl is a C1 to C20 aliphatic chain, such as a C1 to C15 aliphatic chain, C1 to C10 aliphatic chain, C1 to C5 aliphatic chain, such as a C5 to C20 aliphatic chain, such as a C5 to C15 aliphatic chain, such as a C5 to C10 aliphatic chain, such as a C10 to C20 aliphatic chain, such as a C10 to C15 aliphatic chain.
The compound for use according to any one of the preceding claims, wherein alkyl is selected from the group consisting of methyl, ethyl, and propyl.
The compound for use according to any one of the preceding claims, wherein —OR is acetate or lactate.
The compound for use according to any one of the preceding claims, wherein R is —H.
The compound for use according to any one of the preceding claims, wherein n is 2.
The compound for use according to any one of the preceding claims, wherein the compound of Formula I is
The compound for use according to any one of the preceding claims, wherein the compound of Formula I is a compound of Formula XV,
The compound for use according to any one of the preceding claims, wherein the compound of Formula I is selected from the group consisting of
The compound for use according to any one of the preceding claims, wherein the compound of Formula I is selected from the group consisting of
The compound for use according to any one of the preceding claims, wherein the compound of Formula I is glucono-δ-lactone (Formula XIX),
The compound for use according to any one of the preceding claims, wherein the compound of Formula I is selected from the group consisting of
The compound for use according to any one of the preceding claims, wherein the compound of Formula I is selected from the group consisting of
The compound for use according to any one of the preceding claims, wherein the compound of Formula I is oligomerized to form an oligomer.
The compound for use according to any one of the preceding claims, wherein the compound of Formula I is polymerized to form a polymer.
The compound for use according to any one of the preceding claims, wherein the oligomer or polymer comprises one compound of Formula I.
The compound for use according to any one of the preceding claims, wherein the oligomer or polymer is a mixed oligomer/polymer.
The compound for use according to any one of the preceding claims, wherein the oligomer or polymer further comprises lactic acid.
The compound for use according to any one of the preceding claims, wherein the oligomer comprises at least two different compounds of Formula I.
The compound for use according to any one of the preceding claims, wherein two compounds of Formula I are linked to form a dimer.
The compound for use according to any one of the preceding claims, wherein the dimer comprises two compounds of Formula XIV.
The compound for use according to any one of the preceding claims, wherein the dimer comprises two different compounds of Formula I.
The compound for use according to any one of the preceding claims, wherein the compound is not glucono-δ-lactone (Formula XIX),
The compound for use according to any one of the preceding claims, with the proviso that if the compound of Formula I is the compound of Formula XIX, then the microbial infection is not a fungal infection.
The compound for use according to any one of the preceding claims, with the proviso that if the compound of Formula I is the compound of Formula XIX, then the microbial infection is not a urogenital fungal infection.
The compound for use according to any one of the preceding claims, with the proviso that if the compound of Formula I is the compound of Formula XIX, then the microbial infection is not vulvovaginal candidosis.
The compound for use according to any one of the preceding claims, with the proviso that if the microbial infection is a urogenital fungal infection, then the compound of Formula I is not a compound of Formula XIV,
The compound for use according to any one of the preceding claims, wherein the compound is in a pharmaceutical composition.
The compound for use according to any one of 90 to 96, wherein the antifungal agent is selected form the group consisting of miconazole, terconazole, isoconazole, fenticonazole, fluconazole, nystatin, ketoconazole, clotrimazole, butoconazole, econazole, tioconazole, itraconazole, 5-fluoracil, and metronidazole.
A method for prevention and/or reduction of biofilm formation, wherein the method comprises administration of a compound of Formula I or a composition comprising a compound of Formula I.
A compound of Formula I for use in preventing preterm birth.
A method of treatment of one or more microbial infections comprising co-administration of a compound of Formula I and an antimicrobial agent to an individual in need thereof.
A method of treatment of one or more microbial infections comprising co-administration of a compound of Formula I as defined in any one of the preceding claims to an individual in need thereof.
Use of a compound of Formula I as defined in any one of the preceding claims for the manufacture of a medicament for the treatment and/or prevention of a microbial infection.
Use of a compound of Formula I as defined in any one of the preceding claims for the manufacture of a medicament for the prevention and/or reduction of biofilm formation.
Dependencies are inferred from the claim text.