Daniel OBRECHT,Frank Otto GOMBERT,Johann ZIMMERMANN,Alexander LEDERER,Christian OEFNER
申请号：
MX2014014840
公开号：
MX355396B
申请日:
2012.06.06
申请国别(地区):
MX
年份:
2018
代理人:
摘要：
ß-Hairpin peptidomimetics of the general formula cyclo(-Tyr1-His2-Xaa3-Cys 4-Ser5-Xaa6-DPro7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-Xaa15-P ro16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa3, Xaa6, Xaa8, Xaa13, Xaa14 and Xaa15 being amino acid residues of certain types which are defined in the description and the claims, have favorable pharmacological properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients or where cancer is mediated or resulting from CXCR4 receptor activity or where immunological diseases are mediated or resulting from CXCR4 receptor activity or for treating immunosuppression or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid-and solution phase synthetic strategy.La presente invención se refiere a un compuesto de la fórmula general ciclo (-Tyr1-His2-Xaa3-Cys4-Ser5-Xaa6-DPro7-Xaa8-Arg9-Tyr1 0-Cys11-Tyr12-Xaa13-Xaa14-Xaa15-Pro16-), el enlace disulfuro entre Cys4 y Cys11, y las sales aceptables farmacéuticamente del mismo, con Xaa3 es Try Try(Me) o Tyr (CF3), Try(Me) es ácido (2S)-2-amino-(4-metoxifenil)-3-propionico, Tyr (CF3) es ácido (2S)-2-amino-(4-trifluorometoxifenil)-3-propionico, Xaa6 es Ala o Acc Acc es ácido 1-aminociclopropano-carboxílico, Xaa8 es Orn (iPr), Orn(iPr) es ácido (2S)-Nw-isopropil-2,5-diaminopentanoico, Xaa13 es Gln o Glu, Xaa14 es Lys (iPr), Lys(iPr) es ácido (2S)-Nw-isopropil-2,6-diaminohexanoico, Xaa15 es DPro o DLys(iPr) , Dlys (iPr) es ácido (2R)-Nw-isopropil-2,6-diaminohexan oico, con la provisión de que si Xaa6 es Ala, entonces Xaa15 es DLys (iPr).
