PATENT CLAIM ANALYSIS

Application Number: 15890040
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-06
Patent Classification: ["514", "183000"]

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 cancer 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 2):
A compound of  claim 1  according to the general formula: Wherein each R N  is independently H or a C 3 -C 3  alkyl group when N is an amine group or each R N  is absent when N forms all isoxazole group by binding to the adjacent oxygen atom; R 1 , R 2 , R 3 , R 4  and R 5  are each independently H, a halogen (F, Cl, Br, I, preferably F), 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 (preferably H or CH 3 , most often H); R a  is a sidechain derived from a natural or unnatural amino acid (D- or L-, preferably a L-amino acid) preferably selected from the group consisting of alanine (methyl), arginine (propyleneguanidine), asparagine (methylenecarboxyamide), aspartic acid (ethanoic acid), cysteine (thiol, reduced or oxidized di-thiol), glutamine (ethylcarboxyamide), glutamic acid (propanoic acid), histidine (methyleneimidazole), isoleucine (1-methylpropane), leucine (2-methylpropane), lysine (butyleneamine), methionine (ethylmethylthioether), phenylalanine (benzyl), proline (R\u2032 forms a cyclic ring with R a  and the adjacent nitrogen group to form a pyrrolidine group), hydroxyproline, serine (methanol), threonine (ethanol, 1-hydroxyethane), tryptophan (methyleneindole), tyrosine (methylene phenol) or valine (isopropyl) 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 (preferably R E  is H or a C 1 -C 3  alkyl group); R 1\u2032 , R 2\u2032 , R 3\u2032 , R 4\u2032  and R 5\u2032  are each independently H, a halogen (F, Cl, Br, I, preferably F), a C 1 -C 6  (preferably C 1 -C 3 ) alkyl group optionally substituted with one or two hydroxyl groups or up to three chloro or fluoro groups, NO 2 , CN, a (CH) 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; Each m\u2032 is independently 0, 1, 2, 3, 4, 5, or 6 (preferably 0, 1, 2 or 3, more preferably 0 or 1); Each y\u2032 is independently 0, 1 or 2 (preferably 0 or 1); R LABT  is an \u2003group, where L is a bond, at least one linker (preferably a single linker) which comprises a first linker group L1 which optionally includes a connector group CT and an optional linker group L2 which itself optionally includes a connector group CT, said first linker group L1 being linked to said second linker group L2 optionally (preferably) through a CT group; and  is an antibody binding moiety comprising a hapten which is capable of binding to an antibody in said patient or subject, or a pharmaceutically acceptable salt, stereoisomer, enantiomer, solvate or polymorph thereof.

Metadata:
- Claim Count in Document: 104.0
- Percentile: 88.0
- Lexical Diversity: 1.93976
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14397995', '15374272', '13173480', '14480204', '12991926']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7926424493463661
- 35 USC 102 Novelty (BERT): 0.5198717482760642
- Combined Prediction Score: 0.7653653792393359
- Mean Citation Score: 313.007338
- Max Citation Score: 320.29672
- Similarity Product: 222.92316975022788

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

Dataset: test