PATENT CLAIM ANALYSIS

Application Number: 16322391
Application Type: Utility
Filing Date: 2019-01
Publication Date: 2019-06
Patent Classification: ["546", "209000"]

Abstract:
The present invention relates to chimeric (including bifunctional) compounds, compositions comprising those compounds and methods of treating cancer in a patient or subject, especially including metastatic and other cancers where cancer cells exhibit overexpression (heightened expression) of cell surface urokinase-type plasminogen activator receptor (urokinase receptor) compared to normal (non-cancerous) cells. The compounds bind to the urokinase-type plasminogen activator receptor (uPAR) on the surface of a cancer cell, including a metastatic cancer cell, and consequently recruit native antibodies of the patient or subject where the antibodies can selectively degrade and/or deactivate targeted cancer cells through antibody-dependent cellular phagocytosis and antibody-dependent cellular cytotoxicity (ADCC) and/or complement dependent cytotoxicity (CDC) against a large number and variety of cancers, thus providing cancer cell death and an inhibition of growth, elaboration and/or metastasis of the cancer, including remission and cure of the patient's cancer.

Claim (Index 1):
A compound according the the general formula:\n TBT-LINKER-ABT Where;\n ABT is an antibody binding moiety comprising a hapten which is capable of binding to an antibody in said patient or subject; \n LINKER is a linker molecule which chemically links TBT to ABT; \n TBT is a moiety which binds to an active site of urokinase-type plasminogen activator receptor (uPAR) on the surface of cancer cells of a patient or subject, selected from a moiety according to the general formula: \n wherein X=H, F, Cl, Br, CF 3 , MeSO 2 , CH 3 O, CF 3 O N(R N ) 2 , where each R N  is in H or a C 1 -C 3  alkyl group; R 1 , R 2 , R 3 , R 4  and R 5  are each independently H, a halogen, a C 1 -C 3  alkyl group optionally substituted with one or two hydroxyl groups or up to three fluoro groups, NO 2 , CN, a (CH 2 ) m\u2032 OR E  (O-alkyl) group, a (CH 2 ) m\u2032 COR E  (keto) group, a (CH 2 ) m\u2032 COOR E  (carboxy ester) group, a (CH 2 ) m\u2032 SO 3 H group, a (CH 2 ) m\u2032 OCOR E  (oxycarbonyl ester) group, Each R\u2032 is independently H or a C 1 -C 3  alkyl group; R a  is a sidechain derived from a natural or unnatural amino acid (D- or L-)\u2032 Each R E  is H or a C 1 -C 6  alkyl group optionally substituted with one or two hydroxyl groups or up to three chloro or fluoro groups; R 1 , R 2 , R 3  R 4  and R 5  are each independently H, a halogen, a C 1 -C 6  alkyl group optionally substituted with one or two hydroxyl groups or up to three chloro or fluoro groups, NO 2 , CN, a (CH 2 ) m\u2032 OR E  (O-alkyl) group, a (CH 2 ) m\u2032 COOR E  (carboxy ester) group, a (CH 2 ) m\u2032 O\u2014COR E  (oxycarbonyl ester) group, or a (CH 2 ) m\u2032 COR E  (keto) group; R 1  is H or SO 3 H, R 2  is H, CO 2 H, SO 3 H, \u2014NHCH 2 \u2014CO 2 H, \u2014NHCH 2 \u2014SO 3 H, \u2014C(O)\u2014NHCH 2 \u2014CO 2 H or \u2014C(O)\u2014NHCH 2 \u2014SO 3 H, R 3  is H, CO 2 H, or SO 3 H, R 4  is H, CO 2 H, or SO 3 H, and R 5  is H, CO 2 H, or SO 3 H; Each m\u2032 is independently 0, 1, 2, 3, 4, 5, or 6; Each y\u2032 is independently 0, 1 or 2; R LABT  is a LIN-AST group, n=0-4, m=0-5, and R 6 =H, C1-C4 lower alkyl; or a pharmaceutically acceptable salt, stereoisomer, enantiomer, solvate or polymorph thereof.

Metadata:
- Claim Count in Document: 2.0
- Percentile: 99.0
- Lexical Diversity: 1.94048
- Patent Class: 546.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15890040', '15374272', '14397995', '14480204', '13173480']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7171120979841548
- 35 USC 102 Novelty (BERT): 0.5034220853176097
- Combined Prediction Score: 0.6957430967175002
- Mean Citation Score: 220.170034
- Max Citation Score: 282.3902
- Similarity Product: 243.47715638381248

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

Dataset: test