PATENT CLAIM ANALYSIS

Application Number: 15966642
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-08
Patent Classification: ["514", "007200"]

Abstract:
The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue and a second K residue, at positions corresponding to position 26, and 37, respectively, of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of eight amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1: HOOC—(CH 2 ) x —CO-*, and Chem. 2: HOOC—C 6 H 4 —O—(CH 2 ) y —CO-*, in which x is an integer in the range of 8-16, and y is an integer in the range of 6-13; and the linker comprises Chem. 3: *—NH—(CH 2 ) q —CH[(CH 2 ) w —NR 1 R 2 ]—CO-*, which is connected at its CO-* end to the epsilon amino group of the first or the second K residue of the GLP-1 analogue, and wherein q is an integer in the range of 0-5, R 1  and R 2  independently represent *—H or *—CH 3 , and w is an integer in the range of 0-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel peptide and linker intermediates. The derivatives are potent, stable, protracted, and suitable for oral administration.

Claim (Index 11):
The derivative of  claim 1 , wherein the analogue is a peptide of Formula I:\n Xaa 7 -Xaa 8 -Glu-Gly-Thr-Xaa 12 -Thr-Ser-Asp-Xaa 16 -Ser-Xaa 18 -Xaa 19 -Xaa 20 -Glu-Xaa 22 -Xaa 23 -Ala-Xaa 25 -Lys-Xaa 27 -Phe-Ile-Xaa 30 -Xaa 31 -Leu-Xaa  33 -Xaa 34 -Xaa 35 -Xaa 36 -Lys-Xaa 38  (SEQ ID NO: 11), wherein Xaa 7  is L-histidine, imidazopropionyl, \u03b1-hydroxy-histidine, D-histidine, desamino-histidine, 2-amino-histidine, \u03b2-hydroxy-histidine, homohistidine, N \u03b1 -acetyl-histidine, N \u03b1 -formyl-histidine, \u03b1-fluoromethyl-histidine, \u03b1-methyl-histidine, 3-pyridylalanine, 2-pyridylalanine, or 4-pyridylalanine; Xaa 8  is Ala, Gly, Val, Leu, Ile, Thr, Ser, Lys, Aib, (1-aminocyclopropyl) carboxylic acid, (1-aminocyclobutyl) carboxylic acid, (1-aminocyclopentyl) carboxylic acid, (1-aminocyclohexyl) carboxylic acid, (1-aminocycloheptyl) carboxylic acid, or (1-aminocyclooctyl) carboxylic acid; Xaa 12  is Phe or Leu; Xaa 16  is Val or Leu; Xaa 18  is Ser, Val, or Leu; Xaa 19  is Tyr or Gln; Xaa 20  is Leu or Met; Xaa 22  is Gly, Glu, or Aib; Xaa 23  is Gln, Glu, or Arg; Xaa 25  is Ala or Val; Xaa 27  is Glu or Leu; Xaa 30  is Ala, Glu, or Arg; Xaa 31  is Trp or His; Xaa 33  is Val; Xaa 34  is Glu, Asn, Gly, Gln, Arg, or His; Xaa 35  is Gly or Aib; Xaa 36  is Arg or Gly; and Xaa 38  is Ser, Gly, Ala, Glu, Pro, Arg, or absent.

Metadata:
- Claim Count in Document: 34.0
- Percentile: 91.0
- Lexical Diversity: 2.45161
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15404808', '14399087', '13883946', '15301960', '13882947']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8488021451518007
- 35 USC 102 Novelty (BERT): 0.6864990148187378
- Combined Prediction Score: 0.8325718321184945
- Mean Citation Score: 636.651352
- Max Citation Score: 695.37006
- Similarity Product: 679.4984023128031

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