摘要:
Described are lantibiotic-based compounds, pharmaceutical compositions comprising the same and use of the compounds and said compositions, for the treatment of microbial infection, for example Clostridium difficile or Micrococcus luteus infection. The lantibiotic-based compounds have antimicrobial activity and in comparison to one or more of actagardine, actagardine B, deoxyactagardine B and deoxyactagardine have retained activity or improved activity.
摘要:
Described are lantibiotic-based compounds, pharmaceutical compositions comprising the same and use of the compounds and said compositions, for the treatment of microbial infection, for example Clostridium difficile or Micrococcus luteus infection. The lantibiotic-based compounds have antimicrobial activity and in comparison to one or more of actagardine, actagardine B, deoxyactagardine B and deoxyactagardine have retained activity or improved activity.
摘要:
The present invention provides methods for the treatment or prophylaxis of a microbial infection of the lower intestine or colon in a subject, the method comprising administering to the subject a type-B lantibiotic. In particular, the invention provides methods for the treatment or prophylaxis of a Clostridium difficile infection. The type-B lantibiotics may include compounds selected from the group consisting of mersacidin, actagardine, plantaricin, planosporicin, ruminococcin, antibiotic 10789, michiganin and haloduracin, and derivatives and variants thereof.
摘要:
A method for the treatment or prophylaxis of a microbial infection of the lower intestine or colon in a subject is described, wherein the method comprises administration to the subject of a type-B lantibiotic, wherein the type-B lantibiotic may include compounds selected from the group consisting of mersacidin, actagardine, plantaricin, planosporicin, ruminococcin, antibiotic 10789, michiganin and haloduracin, and derivatives and variants thereof.
摘要:
A method for the treatment or prophylaxis of a microbial infection of the lower intestine or colon in a subject is described, wherein the method comprises administration to the subject of a type-B lantibiotic, wherein the type-B lantibiotic may include compounds selected from the group consisting of mersacidin, actagardine, plantaricin, planosporicin, ruminococcin, antibiotic 10789, michiganin and haloduracin, and derivatives and variants thereof.
摘要:
Described is a pharmaceutical formulation of a capsule for oral delivery of a type B lantibiotic to the stomach comprising a hard gelatine, HPMC or starch capsule, and a type B lantibiotic of formula (I): wherein X is —NH(CH2)qNH2 and q is an integer 2 to 12.
摘要:
A liquid colloidal pharmaceutical formulation of a type B lantibiotic for infusion or direct injection is described, the formulation being clear of visual particulates and comprising a type B lantibiotic or a salt thereof, an isotonic aqueous solution comprising a sugar alcohol and optionally a buffer.
摘要:
Described is a A liquid colloidal pharmaceutical formulation of a type B lantibiotic for infusion or direct injection comprising a type B lantibiotic or a salt thereof, an isotonic aqueous solution comprising a sugar alcohol such as glycerol and/or a saccharide and optionally a buffer, wherein said final formulation for infusion or direct injection is clear of visual particulates.
摘要:
Described are certain salts of certain lantibiotic compounds, pharmaceutical compositions comprising the same and use of the salts and compositions for the treatment of microbial infection, particularly Methicillin-resistant Staphylococcus aureus (MRSA) infection. The salts have an aqueous solubility of 2.5 mg/mL or more.
摘要:
The present invention provides actagardine, actagradine B and deoxy actagardine B derivatives of formula (I), wherein: X1 denotes that the residue is Leu; Val; or Ile; X2 denotes that the residue is Leu; Val; or Ile; R1 represents an alkyl or heteroalkyl group, substituted by at least one hydroxyl substituent, and R2 represents hydrogen, or an alkyl or heteroalkyl group, optionally substituted by at least one hydroxyl substituent, or R1 and R2 taken together with the nitrogen atom represent a heterocyclic group having at least one hydroxyl substituent, wherein the heterocyclic group optionally further contains one or more heteroatoms; Z is an amino acid residue, —NR3R4, —NR5COR6, —NR5C(O)OR6; —NR5SOR6, NR5SO2R6; —NR5C(S)NR6R7, —NR5C(NR8)NR6R7, or —N═R9, where R3, R4, R5, R6, R7, R8 and R9 are independently hydrogen, or a group, optionally substituted, selected from alkyl, heteroalkyl, aryl, heteroaryl, aralkyl and heteroaralkyl, with the proviso that R9 is not hydrogen; and Y is —S— or —S(O)—. The compounds find use in the treatment of microbial infections.