PATENT CLAIM ANALYSIS

Application Number: 15993683
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-12
Patent Classification: ["514", "252020"]

Abstract:
Disclosed are compounds of Formula (I) or a salt thereof,wherein R 1  is:  each W is independently NR 1b  or O; Z is a bond or CHR 1d ; and R 1 , R 2 , R d , R 3a , R 3b , L 1 , B, V, Y, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.

Claim (Index 1):
A compound having the structure of Formula (I) or a salt thereof, wherein: R 1  is: each W is independently NR 1b  or O; Z is a bond or CHR 1d ; X is independently N or CR 1a , wherein X is N at only 0, 1, or 2 positions; each R 1a  is independently H, F, Cl, \u2014OH, \u2014CN, C 1-3  alkyl, C 1-3  fluoroalkyl, C 3-6  cycloalkyl, C 1-3  alkoxy, or C 1-3  fluoroalkoxy; each R 1b  is independently H, C 1-3  alkyl, C 2-3  fluoroalkyl, C 3-6  cycloalkyl R 1c  is independently H, deuterium, C 1-4  alkyl, C 1-4  fluoroalkyl, or C 3-6  cycloalkyl; R 1d  is H, C 1-3  alkyl, C 1-4  fluoroalkyl, or C 3-6  cycloalkyl; Y is \u2014C(R 6 ) 2 \u2014, \u2014C(R 6 ) 2 \u2014C(R 6 ) 2 \u2014, \u2014C(O)\u2014, \u2014C(O)\u2014C(R 6 ) 2 \u2014, \u2014C(R 6 ) 2 \u2014C(O)\u2014, or \u2014SO 2 \u2014; V is \u2014O\u2014, \u2014NR 4 \u2014, \u2014CR 5 R 5 \u2014, \u2014S\u2014, \u2014S(O)\u2014, \u2014SO 2 \u2014, or \u2014C(O)\u2014; wherein if V is \u2014O\u2014, \u2014S\u2014, \u2014S(O)\u2014, \u2014SO 2 \u2014, or \u2014C(O)\u2014, then Y is not \u2014SO 2 \u2014, and wherein if V is \u2014O\u2014, \u2014S\u2014, or NR 4 , then Y is not C(R 6 ) 2 , and wherein if V is \u2014S(O)\u2014, \u2014SO 2 \u2014, or C(\u2550O)\u2014, then Y is not \u2014C(\u2550O)\u2014, \u2014C(\u2550O)\u2014C(R 6 ) 2 \u2014; L 1  is \u2014C(R) 2 \u2014, \u2014C(O)\u2014, or \u2014C(R) 2 \u2014C(R) 2 \u2014; wherein R is independently H, F, OH, C 1-3  alkyl, C 1-3  hydroxyalkyl, C 1-3  alkoxyalkyl, or C 1-3  fluoroalkyl; wherein R is not \u2014OH or F if it is attached to a carbon atom that is adjacent to a nitrogen atom: Ring B is phenyl, pyridinyl, pyrimidinyl, pyrrazolyl, thiazolyl, imidazolyl, triazolyl, tetrazolyl, oxadiazolyl, thiadiazolyl, isoxazolyl, isothiazolyl, pyrrolyl, pyrazinyl, oxazolyl, pyridazinyl, pyrrolidinyl, or imidazolidinyl; R 2  is a C 6-10  aryl, or a 5 to 10 membered heterocycle ring containing 1 to 4 heteroatoms selected from N, O, and S, the heterocycle ring optionally containing an oxo substitution, the aryl or heterocycle ring are substituted with 0-3 R 2a ; R 2a  is independently OH, \u2550O, CN, halo, C 1-4  alkyl, C 1-4  deuteroalkyl, C 1-4  fluoroalkyl, C 1-4  alkoxy, C 1-4  deuteroalkoxy, C 1-4  fluoroalkoxy, C 3-6  cycloalkyl, C 3-6  cycloalkoxy, C(\u2550O)NR 4b R 4b , C(\u2550O)C 1-4  alkyl, SO 2 R e , NR 4b SO 2 R 4b , or a 4 to 6 membered heterocycle having 1, 2, 3, or 4 heteroatoms selected from O, S, and N, the heterocycle optionally containing an oxo substitution and is substituted with 0-3 R 2b ; R 2b  is independently C 1-3  alkyl, C 1-3  fluoralkyl, C 1-3  hydroxyalkyl, C 3-6  cycloalkyl, or C 3-6  fluorocycloalkyl; R 3a  is H, halo, OH, CN, C 1-3  alkyl, C 1-3  hydroxyalkyl, C 1-3  fluoroalkyl, C 1-3  alkoxy, or C 3-6  cycloalkyl, wherein if V is \u2014O\u2014, \u2014NR 4 \u2014, \u2014S\u2014, \u2014S(O)\u2014, \u2014SO 2 \u2014, or \u2014C(\u2550O)\u2014, then R 3a  is not halo, and wherein if V is \u2014O\u2014, \u2014NR 4 \u2014, \u2014S\u2014, then R 3a  is not OH, CN; R 3b  is H, \u2550O, C 1-3  alkyl, C 1-3  hydroxyalkyl, C 1-3  fluoroalkyl, C 1-3  alkoxy, or C 3-6  cycloalkyl; R 4  is H, C 1-3  alkyl, C 2-3  fluoroalkyl, C 2-3  hydroxyalkyl, CO 2 R 4a , C(O)R 4a , SO 2 R 4a , C(O)N(R 4b R 4b ), SO 2 N(R 4b R 4b ), or OH; R 4a  is C 1-3  alkyl, C 1-3  fluoroalkyl, C 3-6  cycloalkyl, C 3-6  fluorocycloalkyl, C 6-10  aryl or a 4 to 10 membered heterocycle having 1, 2, 3 or 4 heteroatoms selected from O, S, and N, the aryl or heterocycle being substituted with 0-3 R 4c ; R 4b  is independently H, C 1-3  alkyl, C 2-3  fluoroalkyl, C 3-6  cycloalkyl, C 3-6  fluorocycloalkyl, C 6-10  aryl or a 4 to 10 membered heterocycle having 1, 2, 3 or 4 heteroatoms selected from O, S, and N; alternatively, 2 R 4b s, along with the atom to which they are attached, join to form a 3 to 6 membered saturated ring containing an additional 0-2 heteroatoms selected from O, S, and N; R 4c  is independently H, F, Cl, or C 1-3  alkyl; R 5  is independently H, F, OH, C 1-3  alkoxy, C 1-3  fluoroalkoxy, C 1-3  alkyl, C 1-3  fluoroalkyl, C 1-3  hydroxyalkyl, C 3-6  cycloalkyl, C 3-6  fluorocycloalkyl, NR 5b R 5b , O\u2014R 5c , or 2 R 5 s are \u2550O; wherein if one R 5  is F, OH or NR 5b R 5b , then the other R 5  is not OH, or NR 5b R 5b . R 5b  is independently H, C 1-3  alkyl, C 3-6  cycloalkyl, C(O)R a , SO 2 R a , or C(O)NR b R b ; alternatively, 2 R 5b s, along with the atom to which they are attached, join to form a 3 to 6 membered saturated ring containing 0-2 heteroatoms selected from O, S, or N; R 5c  is independently H, C 1-3  alkyl, C 3-6  cycloalkyl, or C(O)NR b R b ; R 6  is independently H, OH, F, C 1-3  alkyl, C 1-3  deuteroalkyl, C 1-3  fluoroalkyl, C 3-6  cycloalkyl, C 3-6  fluorocycloalkyl, C 1-3  alkoxy, C 1-3  hydroxyalkyl, C 1-3  hydroxydeuteroalkyl, C 1-3  alkoxyalkyl, or C 1-3  fluoroalkoxyalkyl, or NR 6b R 6b ; wherein if one R 6  on one carbon atom is F, OH or NR 6b R 6b , then the other R 6  on the same carbon atom is not OH or NR 6b R 6b . R 6b  is independently H, C 1-3  alkyl, C 3-6  cycloalkyl, C(O)R a , SO 2 R a , or C(O)NR b R b ; alternatively, 2 R 6 s along with the same atom to which they are attached can form a 3 to 6 membered saturated ring containing 0-2 heteroatoms selected from O, S, and N; R a  is independently H, C 1-3  alkyl, C 2-3  fluoroalkyl, C 3-6  cycloalkyl, C 3-6  fluorocycloalkyl, C 6-10  aryl or a 4 to 10 membered heterocycle having 1, 2, 3, or 4 heteroatoms selected from O, S, and N; R b  is independently H, C 1-3  alkyl, C 2-3  fluoroalkyl, C 3-6  cycloalkyl, C 3-6  fluorocycloalkyl, C 6-10  aryl or a 4 to 10 membered heterocycle having 1, 2, 3 or 4 heteroatoms selected from O, S, and N; alternatively, 2 R b 's along with the atom to which they are attached, join to form a 3 to 6 membered saturated ring, containing 0-2 heteroatoms selected from O, S, and N; each R d  is independently H, F, C 1-3  alkyl, C 1-3  fluoroalkyl, C 1-3  alkoxy, C 1-3  fluoroalkoxy, C 1-3  hydroxyalkyl, C 3-6  cycloalkyl, halo, OH, \u2550O, CN, OCF 3 , OCHF 2 , CHF 2 CF 3 , or C(O)NR e R e ; each R e  is independently H, C 1-3  alkyl, C 2-3  fluoroalkyl, C 3-6  cycloalkyl, C 2-3  hydroxyalkyl, C 2-3  alkoxyalkyl, C 6-10  aryl, or a 5 to 10 membered heteroaryl having 1, 2, 3, or 4 heteroatoms selected from O, S, and N; alternatively, 2 R e s along with the atom to which they are attached, join to form a 3 to 6 membered saturated ring, containing 0-2 heteroatoms selected from O, S, or N; and n is 0, 1, or 2.

Metadata:
- Claim Count in Document: 41.0
- Percentile: 93.0
- Lexical Diversity: 1.61017
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['12519376', '14441698', '15749611', '16067619', '14588470']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8193049759431011
- 35 USC 102 Novelty (BERT): 0.5237308708607206
- Combined Prediction Score: 0.789747565434863
- Mean Citation Score: 326.921486
- Max Citation Score: 330.612
- Similarity Product: 238.8184851179124

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

Dataset: test