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 18):
A compound represented by Formula (I) or a salt thereof: wherein: X is S or NR 4 ; R 4  is H, lower alkyl which is optionally substituted by one to five halogens, C 3-12  cycloalkyl, or \u2014C(O)\u2014(C 3-12  cycloalkyl which is optionally substituted by one to five lower alkyls); 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); 5- to 6-membered monocyclic heterocyclic group which is selected from the group consisting of piperidyl, tetrahydropyranyl, thienyl and pyrazolyl, and which optionally has one to five substituents selected from the group consisting of lower alkyl, \u2014C(O)-(lower alkyl) and \u2014C(O)\u2014O-(lower alkylene)-aryl; -(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; aryl which optionally has one to five substituents selected from the group consisting of halogen, lower halogenoalkyl, \u2014O-(lower alkyl) and \u2014O-(lower halogenoalkyl) or 5- to 6-membered monocyclic heterocyclic group which is selected from the group consisting of piperidyl, tetrahydropyranyl, thienyl and pyrazolyl, and which is optionally substituted by one to five lower alkyls; R 2 's are the same or different from each other, and are H, lower alkyl, halogen, -(lower alkylene)-aryl, or -(lower alkylene)-O-(lower alkylene)-aryl; 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), 5- to 6-membered monocyclic heterocyclic group which is selected from the group consisting of pyridyl, pyrazinyl, pyrimidinyl and pyrazolyl, and \u2014S(O) 2 \u2014(C 3-8  cycloalkyl); -(lower alkylene)-(C 3-8  cycloalkyl); -(lower alkylene)-(5- to 6-membered monocyclic heterocyclic group which is selected from the group consisting of pyridyl, pyrazinyl, pyrimidinyl and pyrazolyl); -(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-(5- to 6-membered monocyclic heterocyclic group which is selected from the group consisting of pyridyl, pyrazinyl, pyrimidinyl and pyrazolyl, and which optionally has one to five substituents selected from the group consisting of halogen, lower alkyl and lower halogenoalkyl); -(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); -(lower alkenylene)-aryl; or \u2014CH=tetrahydropyranyl; R P  is H or a lower alkyl, and R 6  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): 0.7967385820754911
- 35 USC 102 Novelty (BERT): 0.5789949504645593
- Combined Prediction Score: 0.7749642189143979
- Mean Citation Score: 352.503112
- Max Citation Score: 474.03998
- Similarity Product: 402.27491853081233

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