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Gastrin releasing peptide compounds

A composition, radionuclide technology, used in animal repellents, biomaterial analysis, peptide/protein composition, etc.

Inactive Publication Date: 2011-05-25
BRACCO IMAGINIG SPA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Conversely, too rapid clearance of radiopharmaceuticals from the bloodstream by the kidneys is also undesirable if longer-term diagnostic imaging or high tumor uptake by radiation therapy is required

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0502] The following examples are provided as examples of different methods that can be used to prepare the various compounds of the invention. In the various examples, there are compounds identified with a single bold capital letter (eg, A, B, C), which are related to the corresponding compounds with the same label in the drawings.

[0503] General experiment

[0504] A. Definition of other abbreviations used

[0505] The following common abbreviations are used throughout the manual:

[0506] 1,1-Dimethylethoxycarbonyl (Boc or Boc);

[0507] 9-fluorenylmethoxycarbonyl (Fmoc);

[0508] Allyloxycarbonyl (Aloc);

[0509] 1-Hydroxybenzotriazole (HOBt or HOBT);

[0510] N,N'-Diisopropylcarbodiimide (DIC);

[0511] N-Methylpyrrolidone (NMP);

[0512] Acetic anhydride (Ac 2 O);

[0513] (4,4-Dimethyl-2,6-dioxocyclohexylene-1-yl)-3-methylbutyl (iv-Dde);

[0514] Trifluoroacetic acid (TFA);

[0515] Reagent B (TFA: H 2 O:phenol:triisopropylsilane, 88:5:5:2);

[0516] Diisopropylethylamine (DIEA);

[051...

Embodiment I-

[0564] Example I- Figure 1A -B

[0565] Synthetic L62

[0566] Overview: such as Figure 1A As shown in -B, L62 is prepared with the following steps:

[0567] (3β,5β)-3-aminocholane-24-acid methyl ester A was hydrolyzed with NaOH to obtain the corresponding acid B, and then reacted with Fmoc-Cl to obtain intermediate product C. Use octapeptide Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH 2 (BBN[7-14][SEQ ID NO: 1]) functionalized Rink amide resin was reacted with C, Fmoc-glycine and DOTA tri-tert-butyl ester in sequence. After cleavage and deprotection with reagent B, the crude product was purified by preparative HPLC to obtain L62. Total yield: 2.5%. More details are provided below:

[0568] A. Rink amide resin functionalized with bombesin [7-14] (SEQ ID NO:1), (A)

[0569] In a solid-phase peptide synthesis container, mix Fmoc-amino acid (24mmol), N-hydroxybenzotriazole (HOBt) (3.67g; 24mmol) and N,N'-diisopropylcarbodiimide (DIC) ( 3.75mL; 24mmol) were added sequentially to Rink Amide No...

Embodiment II-

[0580] Example II- Figure 2A -F

[0581] Synthesize L70, L73, L74, L115 and L116

[0582] Overview: The product is obtained by the following method: The octapeptide Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH on Rink amide resin 2 (BBN[7-14][SEQ ID NO:1]) (with suitable side chain protection) was coupled with different linkers, and then functionalized with DOTA tri-tert-butyl ester. After cleavage and deprotection with reagent B, the final product was purified by preparative HPLC. The total yield is 3-9%.

[0583] A. Synthetic L70 ( Figure 2A ):

[0584] Resin A (0.5g; 0.3mmol) was shaken with 50% morpholine in DMA (7mL) in a solid phase peptide synthesis vessel for 10 minutes, the solution was emptied and fresh 50% in DMA (7mL) was added Morpholine. The suspension was stirred for 20 minutes, then the solution was emptied and the resin was washed with DMA (5×7 mL). Fmoc-4-aminobenzoic acid (0.43g; 1.2mmol), HOBT (0.18g; 1.2mmol), DIC (0.19mL; 1.2mmol) and DMA (7mL) were added to the resi...

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Abstract

Methods and compositions for diagnosing, staging disease, monitoring therapeutic effect of drugs and imaging a patient are provided, including radiopharmaceutical formulations. Compositions comprising Ga-AMBA complexed with a radioactive isotope are provided; as are methods of imaging Gastrin Releasing Peptide receptor (GRP-R) bearing tissue and methods of diagnosing or staging disease in patients suspected of having disease associated with aberrant GRP-R function. Further, methods of monitoring therapeutic effect of a drug targeted to a receptor that crosstalks with GRP-R are provided; as are methods of pre-dosing / co-dosing non-target tissues containing GRP-R. Particularly, methods of monitoring activity of receptors and receptor pathways in vivo / in vitro by using a ligand that binds to the GRP-R are provided; as are methods of measuring the activity of a receptor or group of receptors and their associated pathways that exhibit crosstalk with the GRP-R by using such a ligand which is also detectable by external means.

Description

[0001] Cross reference of related applications [0002] This application claims the rights and interests of each of the following applications, which are fully incorporated herein by reference: USSN61 / 054,335 filed on February 19, 2008; USSN11 / 352,156 filed on February 10, 2006, which is The partial continuation application of USSN11 / 165,721 filed on June 24, 2005 is the partial continuation application of USSN10 / 828,925 filed on April 20, 2004, which is the international application PCT / Part of the continuation application of US2003 / 041328, which is a part of the continuation application of USSN 10 / 341,577 filed on January 13, 2003, all of the above applications are hereby incorporated by reference in their entirety. Technical field [0003] The present invention relates to a new gastrin-releasing peptide (GRP) compound used as a diagnostic imaging agent or a radiotherapy agent. These GRP compounds are labeled with radionuclides or labels that can be detected by in vivo optical ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N37/18A61K38/00
CPCA61K51/088A61K41/0057A61K49/0056G01N33/57492G01N2333/5758
Inventor L·拉图阿达E·卡佩勒蒂K·E·林德A·D·努恩L·兰特里
Owner BRACCO IMAGINIG SPA
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