C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 313/00 (2006.01) A61K 31/335 (2006.01) C12P 17/08 (2006.01)
Patent
CA 2376010
The present invention provides, <i>inter alia</i>, polyketide macrolides including a polyketide macrolide of structure (2) wherein R1-R5 are the same or different and each is independently selected from the group consisting of hydrogen, R6, a C(O)R7, a C(S)R7, a C(O)NHR7, and a C(S)NHR7, each occurrence of R6 is independently selected from the group consisting of a C1-C6 alkyl, a C5-C12 aryl, and a sugar, each occurrence of R7 is independently selected from the group consisting of hydrogen, a C1-C6 alkyl, and a C5-C12 aryl, and wherein R1 and R2, R2 and R3, and/or R4 and R5 can be taken together to form a ketal ring. Also provided are asceptic mixtures of polyketide macrolides isolated from <i>M. ulcerans</i> in a pharmaceutically acceptable carrier, methods of using the polyketide macrolides and aseptic mixtures to inhibit cancer and suppress an inflammatory response in a mammal, a method of inducing an immune response to <i>Mycobacteria ulcerans</i> without inducing a buruli ulcer, and a composition comprising <i>M. ulcerans</i>.
La présente invention concerne, entre autres, des macrolides de polycétides comprenant un macrolide de polycétide correspondant à la structure (2) dans laquelle R1-R5 sont identiques ou différents, chacun étant sélectionné indépendamment dans le groupe comprenant l'hydrogène, R6, un C(O)R7, un C(S)R7, un C(O)NHR7 et un C(S)NHR7, chaque R6 étant sélectionné indépendamment dans le groupe constitué d'un alkyle C1-C6, d'un aryle C5-C12 et d'un sucre, R1 et R2, R2 et R3, et/ou R4 et R5 pouvant être pris ensemble pour former un noyau de cétal. L'invention concerne aussi des mélanges aseptiques de macrolides de polycétides isolés à partir de <i>M. ulcerans</i> dans un excipient pharmaceutiquement acceptable, des procédés pour utiliser les macrolides de polycétides et les mélanges aseptiques pour inhiber le cancer et supprimer une réponse inflammatoire chez un mammifère, un procédé pour induire une réponse immune à <i>Mycobacteria ulcerans</i> sans induire d'ulcère de Buruli et une composition comprenant <i>M. ulcerans</i>.
George Kathleen M.
Small Pamela L. C.
Department O. F. Health And Human Services The United States Of America Represented By The Secretary
R. William Wray & Associates
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