PATENT CLAIM ANALYSIS

Application Number: 16039858
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2019-04
Patent Classification: ["424", "001690"]

Abstract:
The present invention is directed to novel non-invasive diagnostic tools/compounds to image cancers, especially, melanoma, including metastatic melanoma in vivo. The present compounds exhibit enhanced uptake in cancerous cells and tissue and decreased renal uptake in kidney, evidencing favorable pharmacokinetics of compounds of the present invention. The compounds according to the present invention represent an advance in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention are also useful for initiating therapy for melanoma as well as monitor patients' response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma. Compounds according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states.

Claim (Index 1):
A compound according to the chemical structure:\n (Y 1 ) 4 \u2014X m -(ABC)-CycMSH hex  Where Y 1  is a chelate group, wherein Y 1  optionally incorporates or complexes with a radioisotope;\n Each X is independently an amino acid residue which may be optionally acylated at its amino terminal end or an amino acid linker according to the chemical structure: \n ABC is an amino acid linker wherein A is absent or is a neutral or negatively charged amino acid at physiological pH which is optionally acylated at its amino terminal end; B is a neutral or negatively charged amino acid at physiological pH which is optionally acylated (preferably C 2 -C 20  acylated) at its amino terminal end; C is absent or is a neutral or negatively charged amino acid at physiological pH; m is an integer from 0 to 250, preferably 0 to 5, preferably 0 or 1; n is 0 or 1, preferably 1; p is an integer from 0 to 20, preferably 0 to 10; k is an integer from 0 to 10, preferably 1 or 2; s is an integer from 0 to 10, preferably 0, 1 or 2; i is an integer from 0 to 10, preferably 1 or 2; q is 0 or 1, and CycMSH hex  is a cyclic peptide comprising six amino acids according to the general structure: Wherein W is a C\u2014H group from an aspartic acid or glutamic acid residue (preferably an aspartic acid residue), wherein the alkylene carboxylic acid sidechain of said aspartic acid or glutamic acid and the alkyleneamine sidechain of lysine are bonded together to form an amide linkage as indicated; X 1  is phenylalanine, tyrosine or tryptophan, preferably D-phenylalanine; Y is arginine or lysine, preferably arginine; Z is tryptophan, phenylalanine or tyrosine, preferably tryptophan; Z\u2032 and the alkyleneamine to which Z\u2032 is attached is Lys(CONH 2 ) or Ont(CONH 2 ), preferably Lys(CONH 2 ); j is 1 or 2 (preferably 1); and r is 0 or 1, or a pharmaceutically acceptable salt thereof, wherein said compound is optionally complexed with at least one radioisotope, preferably a polyvalent cationic radioisotope, even more preferably selected from the group consisting of  86 Y,  90 Y,  111 In,  177 Lu,  225 Ac,  212 Bi,  213 Bi,  66 Ga,  67 Ga,  68 Ga,  64 Cu,  67 Cu,  71 As,  72 As,  76 As,  77 As,  65 Zn,  65 Zn,  48 V,  203 Pb,  209 Pb,  212 Pb,  166 Ho,  149 Pm,  153 Sm,  201 Tl,  188 Re,  186 Re and  99m Tc The compound according to  claim 1  complexed with a radioisotope wherein said radioisotope is polycationic.

Metadata:
- Claim Count in Document: 4.0
- Percentile: 95.0
- Lexical Diversity: 1.85185
- Patent Class: 424.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14629791', '14622217', '13497738', '14067064', '15186764']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7949374870430156
- 35 USC 102 Novelty (BERT): 0.612221274678624
- Combined Prediction Score: 0.7766658658065764
- Mean Citation Score: 505.8832
- Max Citation Score: 599.9566
- Similarity Product: 493.05269787609575

Labels:
- Claim Label 101: 1
- Claim Label 102: 0
- Claim Label 103: 1
- Claim Label 112: 0
- Combined Label: 0
- Label 101 Adjusted: 1

Dataset: test