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US 2015/0148522 A1Published application
Somatostatin-dopamine chimeric analogs
AssigneeIpsen Pharma S.A.S.
InventorsZheng Xin DONG, Yeelana SHEN
Life of this patent
Estimating the term…
Abstract
The present invention relates to novel somatostatin-dopamine chimeric analogs and their therapeutic uses for the inhibition, prevention, and/or treatment of neoplasia, neuroendocrine tumors, Cushing's disease/syndrome, and other conditions.
Claims21
1-2. (canceled)
A method of treating a neuroendocrine tumor in a subject, said method comprising administering to said subject a therapeutically effective amount of a compound, wherein the compound is:
- (SEQ ID NO:
- 4)
- Dop1-Tyr-psi(CH2NH)-cyclo(DLys-Arg-Phe-4Pal-DTrp-
- Lys-Thr-Phe);
- (SEQ ID NO:
- 5)
- Dop1-Tyr-psi(CH2NH)-cyclo(DLys-Arg-Phe-Phe-DTrp-
- Lys-Thr-4FPhe);
- (SEQ ID NO:
- 6)
- Dop1-psi(CH2NH)-cyclo(DLys-Arg-Phe-Phe-DTrp-Lys-
- Thr-4FPhe);
- (SEQ ID NO:
- 12)
- Dop1-psi(CH2NH)-cyclo(DLys-Arg-Phe-4Pal-DTrp-Lys-
- Thr-Tyr);
- (SEQ ID NO:
- 13)
- Dop1-Lys(Dop1)-psi(CH2NH)-cyclo(DLys-Arg-Phe-
- 4Pal-DTrp-Lys-Thr-Tyr);
- (SEQ ID NO:
- 14)
- Dop1-Lys(Dop1)-psi(CH2NH)-cyclo(DLys-Arg-Phe-
- 4Pal-DTrp-Lys-Thr-Phe);
- (SEQ ID NO:
- 15)
- Dop1(SO2)-psi(CH2NH)-cyclo(DLys-Arg-Phe-Phe-DTrp-
- Lys-Thr-4FPhe);
- (SEQ ID NO:
- 18)
- Dop1(SO)-psi(CH2NH)-cyclo(DLys-Arg-Phe-4Pal-DTrp-
- Lys-Thr-Tyr);
- (SEQ ID NO:
- 19)
- Dop1(SO)-Tyr-psi(CH2NH)-cyclo(DLys-Arg-Phe-Phe-
- DTrp-Lys-Thr-4FPhe);
- (SEQ ID NO:
- 20)
- Dop1(SO)-psi(CH2NH)-cyclo(DLys-Arg-Phe-Phe-DTrp-
- Lys-Thr-4FPhe);
- (SEQ ID NO:
- 21)
- Dop1(SO)-Tyr-psi(CH2NH)-cyclo(DLys-Arg-Phe-4Pal-
- DTrp-Lys-Thr-Phe);
- (SEQ ID NO:
- 22)
- Dop1(SO)-Lys[Dop1(SO)]-psi(CH2NH)-cyclo(DLys-Arg-
- Phe-4Pal-DTrp-Lys-Thr-Tyr);
- (SEQ ID NO:
- 23)
- Dop1(SO)-Lys[Dop1(S0)]-psi(CH2NH)-cyclo(DLys-Arg-
- Phe-4Pal-DTrp-Lys-Thr-Phe);
- (SEQ ID NO:
- 24)
- Dop1(SO2)-Tyr-psi(CH2NH)-cyclo(DLys-Arg-Phe-Phe-
- DTrp-Lys-Thr-4FPhe);
- (SEQ ID NO:
- 25)
- Dop1(SO2)-psi(CH2NH)-cyclo(DLys-Arg-Phe-4Pal-
- DTrp-Lys-Thr-Tyr);
- (SEQ ID NO:
- 26)
- Dop1(SO2)-Tyr-psi(CH2NH)-cyclo(DLys-Arg-Phe-
- 4Pal-DTrp-Lys-Thr-Phe);
- (SEQ ID NO:
- 28)
- Dop1-psi(CH2NH)-cyclo(DLys-Arg-Phe-4Pal-DTrp-Lys-
- Thr-Phe);
- (SEQ ID NO:
- 29)
- Dop1-cyclo(DLys-Arg-Phe-4Pal-DTrp-Lys-Thr-Phe);
- (SEQ ID NO:
- 30)
- Dop1-cyclo(DLys-Arg-Phe-4Pal-DTrp-Lys-Thr-Tyr);
- (SEQ ID NO:
- 31)
- Dop1-psi(CH2NH)-cyclo(DLys-Arg-Phe-Phe-DTrp-Lys-
- Thr-Phe);
- (SEQ ID NO:
- 35)
- bis[Dop1-psi(CH2N)]-cyclo(DLys-Arg-Phe-4Pal-DTrp-
- Lys-Thr-Phe);
- (SEQ ID NO:
- 39)
- Dop1-Tyr-psi(CH2NH)-cyclo(DLys-Arg-Phe-Phe-DTrp-
- Lys-Thr-Phe);
- (SEQ ID NO:
- 40)
- Dop1-Tyr-psi(CH2NH)-cyclo(DLys-Arg-Phe-Phe-DTrp-
- Lys-Thr-Tyr);
- (SEQ ID NO:
- 41)
- Dop1-cyclo(DLys-Arg-Phe-Phe-DTrp-Lys-Thr-4FPhe);
- (SEQ ID NO:
- 42)
- bis[Dop1-psi(CH2N)]-cyclo(DLys-Arg-Phe-4Pal-DTrp-
- Lys-Thr-Tyr);
- (SEQ ID NO:
- 43)
- Dop1-DTyr-cyclo(DLys-Arg-Phe-Phe-DTrp-Lys-Thr-
- Phe);
- (SEQ ID NO:
- 44)
- Dop1-Tyr-psi(CH2NH)-cyclo(DLys-Arg-Phe-3Pal-DTrp-
- Lys-Thr-Phe);
- (SEQ ID NO:
- 45)
- bis[Dop1-psi(CH2N)]-cyclo(DLys-Arg-Phe-Phe-DTrp-
- Lys-Thr-4FPhe);
- (SEQ ID NO:
- 46)
- bis[Dop1-psi(CH2N)]-cyclo(DLys-Arg-Phe-Phe-DTrp-
- Lys-Thr-Phe);
- (SEQ ID NO:
- 47)
- Dop1-DTyr-psi(CH2NH)-cyclo(DLys-Arg-Phe-Phe-DTrp-
- Lys-Thr-Phe);
- (SEQ ID NO:
- 50)
- Dop1-cyclo(DLys-Arg-Phe-Phe-DTrp-Lys-Thr-Phe);
- (SEQ ID NO:
- 51)
- Dop1-DTyr-psi(CH2NH)-cyclo(DLys-Arg-4Pal-Tyr-
- DTrp-Lys-Thr-Phe);
- or
- (SEQ ID NO:
- 52)
- Dop1-Lys(Dop1)-psi(CH2NH)-cyclo(DLys-Arg-Phe-Phe-
- DTrp-Lys-Thr-4FPhe);
- or a pharmaceutically acceptable salt thereof, and wherein said therapeutically effective amount is the amount effective to treat said disease or disorder in said subject.
127 more elements
Dependencies are inferred from the claim text.