PATENT CLAIM ANALYSIS

Application Number: 16039813
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2019-01
Patent Classification: ["514", "006900"]

Abstract:
The invention relates to thioether monomer and dimer peptide molecules which inhibit binding of α4β7 to the mucosal addressing cell adhesion molecule (MAdCAM) in vivo.

Claim (Index 20):
A peptide molecule comprising a structure of Formula (VI):\n Xaa 1 -Xaa 2 -Xaa 3 -Xaa 4 -Xaa 5 -Xaa 6 -Xaa 7 -Xaa 8 -Xaa 9 -Xaa 10 -Xaa 11 \u2003\u2003 (Formula VI) \n or a pharmaceutically acceptable salt thereof, wherein Xaa 1  is a 2-Me-benzoyl group capable of forming a thioether bond with Xaa 7 ; Xaa 2  is selected from the group consisting of N(alpha)-Me-Arg, Arg, HArg, Dap, Dab, Arg-Me-sym, Arg-Me-asym, 4-Guan, Cit, Cav, and suitable isostere replacements; Xaa 3  is selected from the group consisting of Ser, Gly, and suitable isostere replacements; Xaa 4  is selected from the group consisting of Asp, N-Me-Asp, Asp(OMe), D-Asp, and a suitable isostere replacements; Xaa 5  is selected from the group consisting of Thr, Gln, Ser, Asp, Pro, Gly, His, Ala, Ile, Phe, Lys, Arg, Asn, Glu, Val, Tyr, Trp, Leu, Met, and N-Methyl amino acids including N-Me-Thr, and suitable isostere replacements; Xaa 6  is selected from the group consisting of Gln, Asn, Asp, Pro, Gly, Ala, Phe, Leu, Glu, Ile, Val, HLeu, n-Butyl Ala, n-Pentyl Ala, n-Hexyl Ala, Nle, cyclobutyl-Ala, N-Me-Leu, and suitable isostere replacements; Xaa 7  is selected from the group consisting of Cys, N-Me-Cys, D-Cys, HCys, Pen, and D-Pen; Xaa 8  is selected from the group consisting of absent, Gly, Gln, Asn, Asp, Ala, Ile, Leu, Val, Met, Thr, Lys, Trp, Tyr, His, Glu, Ser, Arg, Pro, Phe, Sar, 1-Nal, 2-Nal, HPhe, Phe(4-F), O-Me-Tyr, dihydro-Trp, Dap, Dab, Dab(Ac), Orn, D-Orn, N-Me-Orn, N-Me-Dap, D-Dap, D-Dab, Bip, Ala(3,3diphenyl), Biphenyl-Ala, aromatic ring substituted Phe, aromatic ring substituted Trp, aromatic ring substituted His, hetero aromatic amino acids, N-Me-Lys, N-Me-Lys(Ac), Bpa, Phe(3-Me), Phe(2-Me), Phe(2-CF3), \u03b2-Me-Phe, 4-Me-Phe, and corresponding D-amino acids and suitable isostere replacements; Xaa 9  is selected from the group consisting of absent, Glu, Amide, Lys, COOH, CONH 2 , Gln, Pro, Gly, His, Ala, Ile, Phe, Lys, Arg, Leu, Val, Tyr, Trp, Met, Gla, Ser, Asn, D-Glu, \u03b2-HGlu, 2-Nal, 1-Nal, D-Asp, Bip, \u03b2-HPhe, \u03b2-Glu, D-Tyr, D-Lys, Dap, Dab, Orn, D-Orn, N-Me-Orn, N-Me-Dap, N-Me-Dab, N-Me Lys, D-Dap, D-Dab, Glu, N-Me-Asp, alpha-H-Glu, suitable isosteres, and corresponding D-amino acids; Xaa 10  is selected from the group consisting of absent, Gln, Pro, Gly, His, Ala, Ile, Phe, Lys, Arg, Leu, Val, Tyr, Trp, Met, Glu, Ser, Asn, Gla, Dap, Dab, Orn, D-Orn, D-Lys, N-Me-Orn, N-Me-Dap, N-Me-Dab, N-Me-Lys, D-Dap, D-Dab, COOH, CONH 2 , suitable isosteres, and corresponding D-amino acids; and Xaa 11  is selected from the group consisting of absent, Gln, Pro, Gly, His, Ala, Ile, Phe, Lys, Arg, Leu, Val, Tyr, Trp, Met, Glu, Ser, Asn, Gla, Dap, Dab, Orn, D-Orn, D-Lys, N-Me-Orn, N-Me-Dap, N-Me-Dab, N-Me-Lys, D-Dap, D-Dab, COOH, CONH 2 , suitable isosteres, and corresponding D-amino acids, wherein the peptide further comprises a thioether bond between Xaa 1  and Xaa 7 , wherein the peptide further comprises a thioether bond between Xaa 1  and Xaa 7 .

Metadata:
- Claim Count in Document: 35.0
- Percentile: 95.0
- Lexical Diversity: 1.03704
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14714198', '15514983', '15614047', '14050349', '14872975']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8855486080377151
- 35 USC 102 Novelty (BERT): 0.732579229769916
- Combined Prediction Score: 0.8702516702109352
- Mean Citation Score: 845.1664359999999
- Max Citation Score: 1016.0851
- Similarity Product: 809.4796309246063

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