PATENT CLAIM ANALYSIS

Application Number: 16041117
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2018-11
Patent Classification: ["514", "348000"]

Abstract:
The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.

Claim (Index 19):
The compound or a salt thereof according to claim  1 , wherein:\n X is S or NR 4 ; R 1  is H; C 1-10  alkyl; -(lower alkylene)-O-(lower alkyl); C 3-12  cycloalkyl which optionally has one to five substituents selected from the group consisting of lower alkyl, halogen and \u2014O\u2014(C 3-4  alkylene)-; C 5-6  cycloalkenyl condensed with a benzene ring, aryl which optionally has one to five substituents selected from the group consisting of halogen and \u2014O-(lower alkyl); -(lower alkylene)-R 11 ; -(lower alkylene)-O\u2014(C 3-12  cycloalkyl); -(lower alkylene)-O-aryl or -(lower alkylene)-O-(lower alkylene)-aryl; R 11  is C 3-12  cycloalkyl which is optionally substituted by one to five lower alkyls or aryl which optionally has one to five substituents selected from the group consisting of halogen, lower halogenoalkyl, \u2014O-(lower alkyl) and \u2014O-(lower halogenoalkyl); R 3  is C 1-10  alkyl which is optionally substituted by one to five halogens; -(lower alkylene)-O-(lower alkyl which optionally has one to five substituents selected from the group consisting of halogen and OH); -(lower alkylene)-O-(lower alkenyl); aryl which optionally has one to five substituents selected from the group consisting of halogen, CN, -(lower alkylene)-O-(lower alkyl), C 3-8  cycloalkyl, aryl which is optionally substituted by \u2014S(O) 2 -(lower alkyl) and \u2014S(O) 2 \u2014(C 3-8  cycloalkyl); -(lower alkylene)-(C 3-8  cycloalkyl); -(lower alkylene)-O\u2014(C 3-8  cycloalkyl); -(lower alkylene)-O-{aryl which optionally has one to five substituents selected from the group consisting of halogen, \u2014O-(lower alkyl), CN and -(lower alkylene)-O-(lower alkyl)}; -(lower alkylene)-O-(lower alkylene)-aryl; -(lower alkylene)-O-(lower alkylene)-(C 3-8  cycloalkyl); -(lower alkylene)-S(O) n -(lower alkyl), wherein n is 0, 1, or 2; -(lower alkylene)-S\u2014(C 3-8  cycloalkyl); -(lower alkylene)-S-(lower alkylene)-(C 3-8  cycloalkyl); or -(lower alkenylene)-aryl; and R P  is H.

Metadata:
- Claim Count in Document: 2.0
- Percentile: 95.0
- Lexical Diversity: 1.71429
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15313712', '15532772', '16076781', '13642320', '11990822']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7948083816693136
- 35 USC 102 Novelty (BERT): 0.5854379113264994
- Combined Prediction Score: 0.7738713346350322
- Mean Citation Score: 352.503112
- Max Citation Score: 474.03998
- Similarity Product: 441.8387912111856

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