PATENT CLAIM ANALYSIS

Application Number: 16084927
Application Type: Utility
Filing Date: 2018-09
Publication Date: 2019-03
Patent Classification: ["514", "019300"]

Abstract:
The peptides of the invention are of formula (I) or (IV). The peptides of the invention are useful in the treatment of cancer.

Claim (Index 16):
A peptide or a pharmaceutical salt thereof of formula (I) or an active metabolite thereof wherein\n one of m, n, p, and q is 1 and the others are 0, \n j is 1, and \n v is comprised from 1 to 10, and \n L corresponds to a birradical of formula (II)\n \u2014P-[(R 1 ) a \u2014(R 2 )\u2014(R 3 ) b ] c -Q- \u2003\u2003(II) \n \n wherein \n \u201ca\u201d and \u201cb\u201d are the same or different and are 0 or 1; \n \u201cc\u201d is comprised from 1 to 10; \n R 1  and R 3  are birradicals independently selected from the group consisting of: (C 1 -C 10 )alkyl, (C 2 -C 10 )alkenyl, (C 2 -C 10 )alkynyl, (C 1 -C 10 )alkyl-O\u2014(C 1 -C 10 )alkyl, (C 1 -C 10 )alkyl-C(\u2550O)\u2014(C 1 -C 10 )alkyl, (C 1 -C 10 )alkyl-O\u2014C(O)\u2014(C 1 -C 10 )alkyl, (C 1 -C 10 )alkyl-C(O)\u2014NR 8 -(C 1 -C 10 )alkyl, (C 1 -C 10 )alkyl-S\u2014(C 1 -C 10 )alkyl, (C 1 -C 10 )alkyl-SR 9 \u2014(C 1 -C 10 )alkyl, (C 1 -C 10 )alkyl-S(\u2550O) 2 -(C 1 -C 10 )alkyl, (C 1 -C 10 )alkyl-S(\u2550O)\u2014(C 1 -C 10 )alkyl, (C 1 -C 10 )alkyl-O\u2014S(\u2550O) 2 -O\u2014(C 1 -C 10 )alkyl, and (C 1 -C 10 )alkyl-NR 10 -(C 1 -C 10 )alkyl; \n R 2  is a birradical selected from the group consisting of: \u2014O\u2014, C(\u2550O), C(\u2550O)R 4 , C(\u2550O)NR 5 , C(\u2550O)O, S(\u2550O), S(\u2550O) 2 , S(R 6 ), N(R 7 ), (C 1 -C 10 )alkyl, (C 2 -C 10 )alkenyl, (C 2 -C 10 )alkynyl, NR 13 R 14 , \u2014NH\u2014NH\u2014, \u2014N\u2550N\u2014, \u2014S\u2014S\u2014, and a known ring system comprising from 3 to 14 carbon atoms, the system comprising from 1 to 3 rings, where:\n each one of the rings is saturated, partially unsaturated, or aromatic; \n the rings are isolated, partially or totally fused, \n each one of the members forming the known ring system is selected from the group consisting of: \u2014CH\u2014, \u2014CH 2 \u2014, \u2014NH\u2014, \u2014N\u2014, \u2014SH\u2014, \u2014S\u2014, and \u2014O\u2014; and \n the ring system is optionally substituted by one or more radicals independently selected from the group consisting of halogen, \u2014OH, \u2014NO 2 , (C 1 -C 10 )alkyl, (C 1 -C 10 )haloalkyl, and (C 1 -C 10 )alkyl-O\u2014; \n \n R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 13 , and R 14  are monoradicals selected from the group consisting of: hydrogen, (C 1 -C 10 )alkyl, (C 2 -C 10 )alkenyl, and (C 2 -C 10 )alkynyl; \n P and Q are birradicals, the same or different, provided that when \u201ca\u201d and \u201cb\u201d are 0, or alternatively one of \u201ca\u201d and \u201cb\u201d is 0, then P and Q have a meaning different from R 2  radical, said P and Q birradicals being selected from the group consisting of: (C 1 -C 10 )alkyl, (C 2 -C 10 )alkenyl, and (C 2 -C 10 )alkynyl; or, alternatively, \n when \u201ca\u201d and \u201cb\u201d are 0, or alternatively one of \u201ca\u201d and \u201cb\u201d is 0, then P and Q are C(\u2550O), and R 2  is selected from the group consisting of: \u2014O\u2014, S(R 6 ), N(R 7 ), (C 1 -C 10 )alkyl, (C 2 -C 10 )alkenyl, (C 2 -C 10 )alkynyl, \u2014NR 13 R 14 , \u2014NH\u2014NH\u2014, \u2014N\u2550N\u2014, \u2014S\u2014S\u2014, and a known ring system comprising from 3 to 14 carbon atoms, the system comprising from 1 to 3 rings, where:\n each one of the rings is saturated, partially unsaturated, or aromatic; \n the rings are isolated, partially or totally fused, \n each one of the members forming the known ring system is selected from the group consisting of: \u2014CH\u2014, \u2014CH 2 \u2014, \u2014NH\u2014, \u2014N\u2014, \u2014SH\u2014, \u2014S\u2014, and \u2014O\u2014; and \n the ring system is optionally substituted by one or more radicals independently selected from the group consisting of halogen, \u2014OH, \u2014NO 2 , (C 1 -C 10 )alkyl, (C 1 -C 10 )haloalkyl, and (C 1 -C 10 )alkyl-O\u2014; \n \n when both \u201ca\u201d and \u201cb\u201d, are 1, then P and Q are selected from the group consisting of: \u2014S\u2014, (C 1 -C 10 )alkyl\u2014S\u2014, \u2014NR\u2032 10 \u2014, (C 1 -C 10 )alkyl-NR\u2032 10\u2032 , \u2014O\u2014, (C 1 -C 10 )-alkyl-O\u2014, \u2014C(\u2550O), (C 1 -C 10 )alkyl-C(\u2550O)\u2014, C(\u2550O)O, (C 1 -C 10 )alkylC(\u2550O)O\u2014, C(\u2550O)N\u2014, (C 1 -C 10 )alkylC(\u2550O)\u2014, C(\u2550O)S\u2014 and (C 1 -C 10 )alkyl-C(+O)S\u2014 being R\u2032 10  a radical selected from the group consisting of: hydrogen, (C 1 -C 10 )alkyl, (C 2 -C 10 )alkenyl, and (C 1 -C 10 )alkynyl; \n the L birradical being bound to the backbone of the peptide sequence of formula (I) via X 1  and X 3  birradicals, or alternatively via X 1  and X 5  birradicals, or alternatively via X 2  and X 4  birradicals, or alternatively via X 3  and X 6  birradicals, \n the X birradicals which are bound to L birradical having the same or different meaning and being of formula (III): \n wherein\n the L birradical binds to the X birradical of formula (III) via the alpha carbon atom; R 11  is a monoradical selected from the group consisting of: (C 1 -C 10 )alkyl, (C 2 -C 10 )alkenyl, (C 2 -C 10 )alkynyl, (C 1 -C 10 )alkyl-O\u2014(C 1 -C 10 )alkyl, (C 1 -C 10 )alkyl-C(\u2550O)\u2014(C 1 -C 10 )alkyl, (C 1 -C 10 )alkyl-O\u2014C(O)\u2014 (C 1 -C 10 )alkyl, (C 1 -C 10 )alkyl-C(O)\u2014NR 8 \u2014(C 1 -C 10 )alkyl, (C 1 -C 10 )alkyl-S\u2014(C 1 -C 10 )alkyl, (C 1 -C 10 )alkyl-SR 9 \u2014(C 1 -C 10 )alkyl, (C 1 -C 10 )alkyl-S(\u2550O) 2 -(C 1 -C 10 )alkyl, (C 1 -C 10 )alkyl-S(\u2550O)\u2014(C 1 -C 10 )alkyl, (C 1 -C 10 )alkyl-O\u2014S(\u2550O) 2 -O\u2014(C 1 -C 10 )alkyl, (C 1 -C 10 )alkyl-NR 10 -(C 1 -C 10 )alkyl, and a known ring system comprising from 3 to 14 carbon atoms, the system comprising from 1 to 3 rings, where: each one of the rings is saturated, partially unsaturated, or aromatic; the rings are isolated, partially or totally fused, each one of the members forming the known ring system is selected from the group consisting of: \u2014CH\u2014, \u2014CH 2 \u2014, \u2014NH\u2014, \u2014N\u2014, \u2014SH\u2014, \u2014S\u2014, and \u2014O\u2014; and the ring system is optionally substituted by one or more radicals independently selected from the group consisting of halogen, \u2014OH, \u2014NO 2 , (C 1 -C 10 )alkyl, (C 1 -C 10 )haloalkyl, and (C 1 -C 10 )alkyl-O\u2014, \n and the other X birradicals of the backbone peptide sequence of formula (I), which are not bound to the \u201cL\u201d birradical, are the same or different and represent amino acids; provided that at least one of the X birradicals not bound to the \u201cL\u201d birradical is selected from the group consisting of:\n X 1  represents an amino acid other than Glu, \n X 2  represents an amino acid other than Lys, \n X 3  represents an amino acid other than Ser, \n X 4  represents an amino acid other than Phe, \n X 5  represents an amino acid other than Ala, and \n X 6  represents an amino acid other than Gln; \n \n wherein:\n the (C 1 -C 10 )alkyl, (C 2 -C 10 )alkenyl, and (C 2 -C 10 )alkynyl are non-substituted or substituted, \n \u201csubstituted (C 1 -C 10 )alkyl\u201d means that the (C 1 -C 10 )alkyl is substituted by one or more radicals selected from the group consisting of: \n halogen, \u2014OR\u2032 11 , \u2014NO 2 , \u2014NR\u2032 11 R 12 , \u2014SR\u2032 11 , \u2014SO 2 R\u2032 11 , \u2014CO 2 R\u2032 11 , and (C 1 -C 10 )alkyl-O\u2014, being R\u2032 11  and R 12  the same or different and selected from the group consisting of: \u2014H, (C 1 -C 10 )alkyl, (C 2 -C 10 )alkenyl, and (C 1 -C 10 )alkynyl; \n \u201csubstituted (C 2 -C 10 )alkenyl\u201d means that the (C 2 -C 10 )alkenyl is substituted by one or more radicals selected from the group consisting of: \n halogen, \u2014OR\u2032 11 , \u2014NO 2 , \u2014NR\u2032 11 R 12 , \u2014SR\u2032 11 , \u2014SO 2 R\u2032 11 , \u2014CO 2 R\u2032 11 , and (C 1 -C 10 )alkyl-O\u2014, being R\u2032 11  and R 12  the same or different and selected from the group consisting of: \u2014H, (C 1 -C 10 )alkyl, (C 2 -C 10 )alkenyl, and (C 1 -C 10 )alkynyl; and \n \u201csubstituted (C 2 -C 10 )alkynyl\u201d means that the (C 2 -C 10 )alkynyl is substituted by one or more radicals selected from the group consisting of: \n halogen, \u2014OR\u2032 11 , \u2014NO 2 , \u2014NR\u2032 11 R 12 , \u2014SR\u2032 11 , \u2014SO 2 R\u2032 11 , \u2014CO 2 R\u2032 11 , and (C 1 -C 10 )alkyl-O\u2014, being R\u2032 11  and R 12  the same or different and selected from the group consisting of: \u2014H, (C 1 -C 10 )alkyl, (C 2 -C 10 )alkenyl, and (C 1 -C 10 )alkynyl; and \n \n the active metabolite is characterized by lacking the first amino acid of the N-terminal region and/or from 1 to 3 amino acids of the C-terminal region.

Metadata:
- Claim Count in Document: 69.0
- Percentile: 97.0
- Lexical Diversity: 1.70588
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['13984762', '14776668', '13397195', '11290735', '15581749']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7343839673290655
- 35 USC 102 Novelty (BERT): 0.5052174350458248
- Combined Prediction Score: 0.7114673141007415
- Mean Citation Score: 260.430318
- Max Citation Score: 267.25793
- Similarity Product: 213.19086696317672

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

Dataset: test