Use of somatostatin analogs for the delivery of anti-tumor drugs to tumor cells
AssigneeAcademia Sinica
InventorsShui-Tein Chen, Ying-Ta Wu, Chun-Ming Huang
Life of this patent
Estimating the term…
Abstract
A conjugate of somatostatin-spacer-drug and a method of making the same. The conjugate can be used to enhance an anti-cancer drug's specificity on the targeted tumor cells, thus increasing its therapeutic efficacy while reducing side-effects.
Claims14
A compound comprising a somatostatin analog moiety, a spacer moiety and an anti-cancer drug moiety, said spacer moiety is selected from the group consisting of
- —CO—(—CH2CH2O—)n—CH2CH2—CO—;
- —CO—(—CH2CH2O—)n—CH2CH2—CO—;
- —NH—(—CH2CH2O—)n—CH2CH2—CO—;
- —NH—(—CH2—)n—CO—;
- —S—(—CH2CH2O—)n—CH2CH2—CO—;
- —S—(—CH2—)n—CO—NH-peptide;
- —(—CH2CH2O—)n—CH2CH2—CO—;
- and
- -maleimide-(—CH2—)n—CO—;
- where n=1-7.
A compound comprising a somatostatin analog moiety, a spacer moiety and an anti-cancer drug moiety, said compound having a structural formula selected from the group consisting of:
- wherein i=1-4;
- j=1-2;
- X1 is an anti-cancer drug moiety that has a —OH group for connecting to said spacer moiety;
- X2 is an anti-cancer drug moiety that has a —NH2 group for connecting to said spacer moiety;
- X3 is an anti-cancer drug moiety that has a —COOH group for connecting to said spacer moiety;
- X4 is an anti-cancer drug moiety that has a maleimide group for connecting to said spacer moiety;
- X5 is an anti-cancer drug moiety that has a —SH group for connecting to said spacer moiety;
- and R is said somatostatin analog moiety;
- Y1=CH3—O—(—CH2CH2O—) m—CH2CH2—CO— where m=45-225 or Y1=Sugar-CO— where Sugar is glucose, sialic acid or their analogues;
- Y2=CH3—O—(—CH2CH2O—) m—CH2CH2—NH— where m=45-225;
- Y3=CH3—O—(—CH2CH2O)m—CH2CH2-maleimide where m=45-225.
A compound having the following structure:
- wherein R is a H, biotin, sugar or PEG group.
A compound having a structural formula selected from the group consisting of:
- X2—CO—(—CH2CH20—)n—CH2CH2—CO—NH—R;
- X2—CO—(—CH2—)n—CO—NH—R;
- wherein n=1-7;
- i=1-4;
- j=1-2;
- R is a somatostatin analog moiety;
- Y1=CH3—O—(—CH2CH2O—) m—CH2CH2—CO— where m=45-225 or Y1=Sugar-CO— where Sugar is glucose, sialic acid or their analogues X2 is a phosphatidylethanoamine having the structural formula of:
- where R1 and R2 are alkyls.
A compound having the following structure:
- wherein R represent a spacer component and R′ represents a somatostatin component.
Dependencies are inferred from the claim text.