Somatostatin analogs with inhibitory activity to growth hormone release
US-9200054-B2 · Dec 1, 2015 · US
Somatostatin analogs with inhibitory activity to growth hormone release
US9919065B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9919065-B2 |
| Application number | US-201514949473-A |
| Country | US |
| Kind code | B2 |
| Filing date | Nov 23, 2015 |
| Priority date | Aug 20, 2003 |
| Publication date | Mar 20, 2018 |
| Grant date | Mar 20, 2018 |
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- Title
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Abstract
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Provided are therapeutic and diagnostic somatostatin analogs including radiotherapeutic and radiodiagnostic reagents, and methods of making and use thereof.
First claim
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What is claimed is: 1. A method of visualizing malignant cells in a subject comprising administering to the subject a compound selected from the group consisting of 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-N H 2 , 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH 2 , 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-D-Asp-NH 2 , 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-D-Thr-NH 2 , 4-amino-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH 2 , 4-amino-3-iodo-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Thr-N H 2 , 4-amino-3-iodo-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-N H 2 , 4-amino-3-iodo-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH 2 , 4-amino-3-iodo-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH 2 , and D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH 2 and any combination thereof, wherein the compound is radiolabeled. 2. The method of claim 1 , wherein the compound comprises a di- or polyiodinated aromatic modification of a Tyr at position 3. 3. The method of claim 1 , wherein the radioactive element is selected from the group consisting of 188 Re, 186 Re, scandium-47, copper-67, gallium-72, yttrium-90, iodine-125, iodine-131, samarium-153, gadolinium-159, dysprosium-165, holmium-166, ytterbium-175, lutetium-177, rhenium-186, rhenium-188, astatine-211 and bismuth-212. 4. A method of treating a cell proliferative disorder in a subject comprising administering to the subject a compound selected from the group consisting of 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-N H 2 , 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Thr-N H 2 , 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-D-Asp-NH 2 , 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-D-Thr-NH 2 , 4-amino-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH 2 , 4-amino-3-iodo-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Thr-N H 2 , 4-amino-3-iodo-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-N H 2 , 4-amino-3-iodo-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH 2 , 4-amino-3-iodo-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH 2 , and D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH 2 and any combination thereof, wherein the compound is radiolabelled. 5. A method as in claim 4 , wherein the cell proliferative disorder is selected from the group consisting of a tumor, acromegaly, and diabetes. 6. The method of claim 4 , wherein the compound comprises a di- or polyiodinated aromatic modification of a Tyr at position 3. 7. The method of claim 4 , wherein the radioactive element is selected from the group consisting of 188 Re, 186 Re, scandium-47, copper-67, gallium-72, yttrium-90, iodine-125, iodine-131, samarium-153, gadolinium-159, dysprosium-165, holmium-166, ytterbium-175, lutetium-177, rhenium-186, rhenium-188, astatine-211 and bismuth-212. 8. A method of activating SST2 and/or SST5 receptors in a subject comprising administering to said mammal an effective amount of a compound selected from the group consisting of 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-N H 2 , 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH 2 , 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-D-Asp-NH 2 , 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-D-Thr-N H 2 , 4-amino-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Thr-N H 2 , 4-amino-3-iodo-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Thr-N H 2 ; 4-amino-3-iodo-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-N H 2 , 4-amino-3-iodo-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Thr-N H 2 , 4-amino-3-iodo-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Asp-N H 2 , and D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-N H 2 and any combination thereof or a pharmaceutically acceptable salt thereof, wherein the compound activates SST2 and/or SST5 receptors in the subject.
Assignees
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Classifications
Drugs for disorders of the cardiovascular system · CPC title
Antineoplastic agents · CPC title
for hyperglycaemia, e.g. antidiabetics · CPC title
Drugs for skeletal disorders · CPC title
Peptides having 5 to 11 amino acids {(A61K38/043 - A61K38/046 take precedence)} · CPC title
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Frequently asked questions
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- What does patent US9919065B2 cover?
- Provided are therapeutic and diagnostic somatostatin analogs including radiotherapeutic and radiodiagnostic reagents, and methods of making and use thereof.
- Who is the assignee on this patent?
- Univ California
- What technology area does this patent fall under?
- Primary CPC classification A61K51/083. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Tue Mar 20 2018 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 1 related publication on this page (citations in our corpus or others sharing the same primary CPC).