PATENT CLAIM ANALYSIS

Application Number: 15765933
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-10
Patent Classification: ["530", "315000"]

Abstract:
The present invention relates to new solid phase peptide methods for synthesizing analogues that exhibit oxytocin antagonist activity, specifically Barusiban and its intermediates. Specifically, the present invention relates to a solid phase process for preparing a compound having the formula c[AA 1 -AA 6 ]-AA 7 -ol, wherein AA 1  is propionic acid, AA 2  is preferably D-Trp, AA 3  is Ile, AA 4  is preferably AlloIle, AA 5  is Asn, AA 6  is hCy, and AA 7  is preferably N-Me-Orn-ol, or a pharmaceutically acceptable salt or solvate thereof.

Claim (Index 1):
A solid phase process for preparing a compound having the formula c[AA 1 -AA 6 ]-AA 7 -OH, wherein AA 1  and AA 6  are linked through a thiol from the AA 6  homocysteine, or a pharmaceutically acceptable salt or solvate thereof, wherein AA 1  is propionic acid, AA 2  is AA b , AA 3  is Ile, AA 4  is AA d , AA S  is Asn, AA 6  is hCy, and AA 7  is \u2014NR-CHQ-CH 2 OH, Q is (CH 2 ) n \u2014NH 2 , the process comprising the steps of:\n a) reacting protected (P 5 P 3  P 4 )AA 7  with a resin to provide (P 5 P 3 P 4 )AA 7 -  wherein protected (P 5 P 3 P 4 ) AA 7  as added to the resin during the synthesis in step a) is (P 5 )NR-CHQ\u2032-CH 2 OH; b) stepwise lengthening (P 5 P 3 P 4 )AA 7 -  to provide (P 7 )AA 2 AA 3 AA 4 (P 1 )AA 5 (Trt)AA 6 -(P 3 P 4 )AA 7 - ; c) reacting X-AA 1  (wherein X is an halogen atom selected from F, Cl, Br and I) with (P 7 )AA 2 AA 3 AA 4 (P 1 )AA 5 (Trt)AA 6 -(P 3 P  4 )AA 7 -  to provide X-AA 1 (P 7 )AA 2 AA 3 AA 4 (P 1 )AA 5 (Trt)AA 6 -(P 3 P 4 )AA 7 - ; d) carrying out a cleavage and deprotection step to provide X-AA 1 AA 2 AA 3 AA 4 AA 5 AA 6 AA 7 -ol; and e) cyclizing X-AA 1 AA 2 AA 3 AA 4 AA 5 AA 6 AA 7 -ol, obtaining the cyclic peptide: c[AA 1 -AA 6 ]-AA 7 -ol wherein AA 1  and AA 6  are linked through a thiol from the AA 6  homocysteine, wherein: P 1 , P 5 , and P 7  are protecting groups, AA b  is a D-aromatic \u03b1-amino acid; AA d  is an aliphatic \u03b1-amino acid; X is a halogen residue; R is CH 3  or C 2 H 5 ; Q\u2032 is (CH2) n \u2014NP 3 P 4 ; n is 2, 3, or 4; P 3  and P 4  are independently H or an amino-acid protecting group, which may be the same or different from each other and which may the same or different to P 1 .

Metadata:
- Claim Count in Document: 19.0
- Percentile: 91.0
- Lexical Diversity: 1.65079
- Patent Class: 530.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['11929494', '11457743', '13959931', '15145901', '11938776']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.6440354821240568
- 35 USC 102 Novelty (BERT): 0.5188976323158105
- Combined Prediction Score: 0.6315216971432321
- Mean Citation Score: 268.686994
- Max Citation Score: 288.8439
- Similarity Product: 190.4022354423523

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