PATENT CLAIM ANALYSIS

Application Number: 16090728
Application Type: Utility
Filing Date: 2018-10
Publication Date: 2019-05
Patent Classification: ["514", "017200"]

Abstract:
Neuropeptide S receptor agonists are provided. The NPS agonists include trimeric, tetrameric, pentameric or hexameric peptidomimetic analogs exhibiting affinity for and activity at the neuropeptide S receptor. The peptidomimetic molecules may be useful in the treatment of disorders, syndromes and conditions mediated by modulation of the neuropeptide S receptor such as substance abuse, narcolepsy, insomnia, obesity, cognitive decline, dementia, Alzheimer's disease, panic disorder, generalized anxiety, PTSD, phobias, schizophrenia and as supportive medication during any kind of cessation program in cognitive behavioral therapy, such as drug addiction, eating disorders and gambling.

Claim (Index 17):
A pharmaceutical composition comprising a compound according to Formula IA-ID, Formula IIA-IIE, Formula III, or Formula IV:\n (i) Formula IA-ID: wherein R 1  is CH(NHCH 3 )CH 2 OH, CH(NH 2 )(CH 2 ) 2 CH 3 , CH(NH 2 )CH 2 OCH 3 , CH 2 CH 2 OH, NHCH 2 CH 3 , CH(NH 2 )CH 2 OH, CH 2 CH 2 OCH 3 , branched or unbranched C 1 -C 6  alkyl, heterocycle, heteroaryl, C 1 -C 4  aralkyl, cycloalkyl, or aryl optionally substituted with halo, alkoxy, amino, or alkoxyaminoalkyl; R 2  is H, phenylalanine side chain, alkylcycloalkyl, unbranched C 1 -C 6  alkyl, or benzyl substituted with nitro or halo; R 3  is arginine side chain or lysine side chain; R 3\u2032  is H, lysine side chain, C 1 -C 3  alkylated or benzylated lysine side chain, alanine side chain, unbranched C 1 -C 6  alkyl, (CH 2 ) 4 NHCOCF 3 , or benzyl optionally substituted with nitro; R 4  is asparagine side chain or C 1 -C 3  alkyl; R 4\u2032  is H, asparagine side chain, C 1 -C 3  alkyl heteroaryl, C 1 -C 6  alkyl, CH 2 OH, CH 2 CONHCH 3 , CH 2 COOCH 3 , or CH 2 CN; R 5  is H, OH, unbranched C 1 -C 6  alkyl, or C 1 -C 4  alkylcycloalkyl; c is 0 when R 5  is OH, or c is 1 when R 5  is hydrogen, unbranched C 1 -C 6  alkyl, or C 1 -C 4  alkylcycloalkyl; R 7  is H or a lysine side chain, provided that when R 7  is a lysine side chain, R 3\u2032  is H; R 8  is H or CH 3 ; d is 0, or when R 4  is H, d is 1, or when R 4  is CH 3 , d is 0 or 1; d 1  is 0, or when R 4  is CH 3 , d 1  is 1; B is a five membered saturated ring substituted with one C(O)NH 2  group, or a six membered saturated or aromatic ring substituted with one C(O)NH 2  group; and E is provided that R 1  is not CH(NH 2 )CH 2 OH when each of R 2  is phenylalanine side chain, R 3  is arginine side chain, and R 4  is asparagine side chain; (ii) Formula IIA-IIE: wherein R 3\u2033  is arginine side chain, lysine side chain, or C 1 -C 3  alkyl; R 4\u2032  is asparagine side chain; the depicted dashed bond in Formula IIA   is a cis or trans bond; and A is CH 2  or CO; (iii) Formula III: wherein R 1  is CH(NHCH 3 )CH 2 OH, CH(NH 2 )(CH 2 ) 2 CH 3 , CH(NH 2 )CH 2 OCH 3 , CH 2 CH 2 OH, NHCH 2 CH 3 , CH(NH 2 )CH 2 OH, CH 2 CH 2 OCH 3 , branched or unbranched C 1 -C 6  alkyl, heterocycle, heteroaryl, C 1 -C 4  aralkyl, cycloalkyl, or aryl optionally substituted with halo, alkoxy, amino, or alkoxyaminoalkyl; R 2  is H, phenylalanine side chain, alkylcycloalkyl, unbranched C 1 -C 6  alkyl, or benzyl optionally substituted with nitro or halo; R 3  is arginine side chain or lysine side chain; R 4\u2033  is asparagine side chain; provided that R 1  is not CH(NH 2 )CH 2 OH when each of R 2  is phenylalanine side chain, R 3  is arginine side chain, and R 4\u2033  is asparagine side chain; (iv) Formula IV: wherein R 1  is CH(NHCH 3 )CH 2 OH, CH(NH 2 )(CH 2 ) 2 CH 3 , CH(NH 2 )CH 2 OCH 3 , CH 2 CH 2 OH, NHCH 2 CH 3 , CH(NH 2 )CH 2 OH, CH 2 CH 2 OCH 3 , branched or unbranched C 1 -C 6  alkyl, heterocycle, heteroaryl, C 1 -C 4  aralkyl, cycloalkyl, or aryl optionally substituted with halo, alkoxy, amino or alkoxyaminoalkyl; R 2  is H, phenylalanine side chain, alkylcycloalkyl, unbranched C 1 -C 6  alkyl, or benzyl optionally substituted with nitro or halo; R 3  is arginine side chain or lysine side chain; R 4\u2033  is asparagine side chain; and R 9  is a valine side chain or a phenylalanine side chain; provided that R 1  is not CH(NH 2 )CH 2 OH when each of R 2  is phenylalanine side chain, R 3  is arginine side chain, and R 4  is asparagine side chain; or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier.

Metadata:
- Claim Count in Document: 16.0
- Percentile: 97.0
- Lexical Diversity: 1.52778
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15229942', '13160086', '13483926', '10846482', '11721910']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7673592600024531
- 35 USC 102 Novelty (BERT): 0.5086477920252632
- Combined Prediction Score: 0.7414881132047342
- Mean Citation Score: 274.275638
- Max Citation Score: 282.69418
- Similarity Product: 200.6170364313412

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

Dataset: test