PATENT CLAIM ANALYSIS

Application Number: 16033632
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2018-11
Patent Classification: ["544", "298000"]

Abstract:
Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.

Claim (Index 1):
A compound of Formula I or Formula II: or a pharmaceutically acceptable salt thereof, a tautomer thereof, a pharmaceutically acceptable salt of the tautomer, a stereoisomer of any of the foregoing, or a mixture thereof, wherein:\n R 1  is an unsubstituted pyridyl, pyridonyl, or pyridine N-oxide, or is a pyridyl, pyridonyl, or pyridine N-oxide substituted with 1, 2, 3, or 4 R 1a  substituents; \n R 1a  in each instance is independently selected from \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014CN, \u2014C 1 -C 6  alkyl, \u2014C 1 -C 6  haloalkyl, \u2014C 1 -C 6  perhaloalkyl, \u2014C 1 -C 6  alkyl-OH, \u2014C 1 -C 6  haloalkyl-OH, \u2014C 1 -C 6  perhaloalkyl-OH, \u2014OH, \u2014O\u2014(C 1 -C 6  alkyl), \u2014O\u2014(C 1 -C 6  haloalkyl), \u2014O\u2014(C 1 -C 6  perhaloalkyl), \u2014C 2 -C 6  alkenyl, \u2014O\u2014(C 1 -C 6  alkyl)-OH, \u2014O\u2014(C 1 -C 6  alkyl)-O\u2014(C 1 -C 6  alkyl), \u2014O\u2014(C 1 -C 6  haloalkyl)-OH, \u2014O\u2014(C 1 -C 6  haloalkyl)-O\u2014(C 1 -C 6  alkyl), \u2014O\u2014(C 1 -C 6  perhaloalkyl)-OH, \u2014O\u2014(C 1 -C 6  perhaloalkyl)-O\u2014(C 1 -C 6  alkyl), \u2014NH 2 , \u2014NH(C 1 -C 6  alkyl), \u2014N(C 1 -C 6  alkyl) 2 , \u2014C(\u2550O)\u2014(C 1 -C 6  alkyl), \u2014C(\u2550O)OH, \u2014C(\u2550O)\u2014O\u2014(C 1 -C 6  alkyl), \u2014C(\u2550O)NH 2 , \u2014C(\u2550O)NH(C 1 -C 6  alkyl), \u2014C(\u2550O)N(C 1 -C 6  alkyl) 2 , phenyl, \u2014C(\u2550O)-(heterocyclyl), a C 3 -C 6  cycloalkyl group or a heterocyclyl group, wherein the heterocyclyl group of the \u2014C(\u2550O)-(heterocyclyl) or heterocyclyl group is a 3 to 7 membered ring containing 1, 2, or 3 heteroatoms selected from N, O, or S; \n R 2  is selected from \u2014H, or C 1 -C 4  alkyl or is absent in the compounds of Formula II; \n R 3  is selected from an unsubstituted C 1 -C 10  alkyl, a C 1 -C 10  alkyl substituted with 1, 2, or 3 R 3a  substituents, a group of formula \u2014(CR 3b R 3c )-Q, a group of formula \u2014NH\u2014(CR 3b R 3c )-Q, a group of formula \u2014(CR 3b R 3c )\u2014C(\u2550O)-Q, a group of formula \u2014(CR 3d R 3e )\u2014(CR 3f R 3g )-Q, a group of formula \u2014(CR 3b \u2550CR 3c )-Q, or a group of formula -(heterocyclyl)-Q, wherein the heterocyclyl of the -(heterocyclyl)-Q has 5 to 7 ring members of which 1, 2, or 3 are heteroatoms selected from N, O, or S and is unsubstituted or is substituted with 1, 2, or 3 R 3h  substituents; \n R 3a  in each instance is independently selected from \u2014F, \u2014Cl, \u2014CN, \u2014OH, \u2014O\u2014(C 1 -C 6  alkyl), \u2014O\u2014(C 1 -C 6  haloalkyl), \u2014O\u2014(C 1 -C 6  perhaloalkyl), \u2014O\u2014(C 1 -C 6  alkyl)-OH, \u2014O\u2014(C 1 -C 6  alkyl)-O\u2014(C 1 -C 6  alkyl), C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, \u2014NH 2 , \u2014NH(C 1 -C 6  alkyl), or \u2014N(C 1 -C 6  alkyl) 2 ; \n R 3b  and R 3c  are independently selected from \u2014H, \u2014F, \u2014Cl, \u2014CN, \u2014C 1 -C 6  alkyl, \u2014C 1 -C 6  haloalkyl, \u2014C 1 -C 6  perhaloalkyl, \u2014OH, \u2014O\u2014(C 1 -C 6  alkyl), \u2014O\u2014(C 1 -C 6  haloalkyl), \u2014O\u2014(C 1 -C 6  perhaloalkyl), \u2014O\u2014(C 1 -C 6  alkyl)-OH, \u2014O\u2014(C 1 -C 6  alkyl)-O\u2014(C 1 -C 6  alkyl), \u2014NH 2 , \u2014NH(C 1 -C 6  alkyl), or \u2014N(C 1 -C 6  alkyl) 2 ; \n R 3d  and R 3e  are independently selected from \u2014H, \u2014F, \u2014Cl, \u2014CN, \u2014C 1 -C 6  alkyl, \u2014C 1 -C 6  haloalkyl, \u2014C 1 -C 6  perhaloalkyl, \u2014OH, \u2014O\u2014(C 1 -C 6  alkyl), \u2014O\u2014(C 1 -C 6  haloalkyl), \u2014O\u2014(C 1 -C 6  perhaloalkyl), \u2014O\u2014(C 1 -C 6  alkyl)-OH, \u2014O\u2014(C 1 -C 6  alkyl)-O\u2014(C 1 -C 6  alkyl), \u2014NH 2 , \u2014NH(C 1 -C 6  alkyl), or \u2014N(C 1 -C 6  alkyl) 2 ; \n R 3f  and R 3g  are independently selected from \u2014H, \u2014F, \u2014Cl, \u2014CN, \u2014C 1 -C 6  alkyl, \u2014C 1 -C 6  haloalkyl, \u2014C 1 -C 6  perhaloalkyl, \u2014OH, \u2014O\u2014(C 1 -C 6  alkyl), \u2014O\u2014(C 1 -C 6  haloalkyl), \u2014O\u2014(C 1 -C 6  perhaloalkyl), \u2014O\u2014(C 1 -C 6  alkyl)-OH, \u2014O\u2014(C 1 -C 6  alkyl)-O\u2014(C 1 -C 6  alkyl), \u2014NH 2 , \u2014NH(C 1 -C 6  alkyl), \u2014N(C 1 -C 6  alkyl) 2 , a C 3 -C 6  cycloalkyl group, or a 3 to 7 membered heterocyclyl group containing 1, 2, or 3 heteroatoms selected from N, O, or S, wherein the C 3 -C 6  cycloalkyl group, or the 3 to 7 membered heterocyclyl R 3f  or R 3g  group may be unsubstituted or substituted with 1 or 2 substituents independently selected from \u2014F, \u2014Cl, \u2014CN, \u2014C 1 -C 6  alkyl, \u2014C 1 -C 6  haloalkyl, \u2014C 1 -C 6  perhaloalkyl, \u2014OH, \u2014O\u2014(C 1 -C 6  alkyl), \u2014O\u2014(C 1 -C 6  haloalkyl), \u2014O\u2014(C 1 -C 6  perhaloalkyl), \u2014O\u2014(C 1 -C 6  alkyl)-OH, \u2014O\u2014(C 1 -C 6  alkyl)-O\u2014(C 1 -C 6  alkyl), \u2014NH 2 , \u2014NH(C 1 -C 6  alkyl), \u2014N(C 1 -C 6  alkyl) 2 , or oxo; \n R 3h  in each instance is independently selected from \u2014F, \u2014Cl, \u2014CN, \u2014C 1 -C 6  alkyl, \u2014C 1 -C 6  haloalkyl, \u2014C 1 -C 6  perhaloalkyl, \u2014OH, \u2014O\u2014(C 1 -C 6  alkyl), \u2014O\u2014(C 1 -C 6  haloalkyl), \u2014O\u2014(C 1 -C 6  perhaloalkyl), \u2014O\u2014(C 1 -C 6  alkyl)-OH, \u2014O\u2014(C 1 -C 6  alkyl)-O\u2014(C 1 -C 6  alkyl), \u2014NH 2 , \u2014NH(C 1 -C 6  alkyl), \u2014N(C 1 -C 6  alkyl) 2 , or oxo; \n Q is a monocyclic or bicyclic C 6 -C 10  aryl group, a monocyclic or bicyclic heteroaryl group with 5 to 10 ring members containing 1, 2, or 3 heteroatoms selected from N, O, or S, a C 3 -C 8  cycloalkyl group, or a 3 to 7 membered heterocyclyl group containing 1, 2, or 3 heteroatoms selected from N, O, or S, wherein the C 6 -C 10  aryl group, the heteroaryl group, the cycloalkyl group, and the heterocyclyl group are unsubstituted or are substituted with 1, 2, 3, or 4 R Q  substituent; \n R Q  in each instance is independently selected from \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014CN, \u2014C 1 -C 6  alkyl, \u2014C 1 -C 6  haloalkyl, \u2014C 1 -C 6  perhaloalkyl, \u2014C 2 -C 6  alkenyl, \u2014C 2 -C 6  alkynyl, \u2014OH, \u2014O\u2014(C 1 -C 6  alkyl), \u2014O\u2014(C 1 -C 6  haloalkyl), \u2014O\u2014(C 1 -C 6  perhaloalkyl), \u2014NH 2 , \u2014NH(C 1 -C 6  alkyl), \u2014N(C 1 -C 6  alkyl) 2 , \u2014C(\u2550O)\u2014(C 1 -C 6  alkyl), \u2014C(\u2550O)OH, \u2014C(\u2550O)\u2014O\u2014(C 1 -C 6  alkyl), \u2014C(\u2550O)NH 2 , \u2014C(\u2550O)NH(C 1 -C 6  alkyl), \u2014C(\u2550O)N(C 1 -C 6  alkyl) 2 , \u2014S(\u2550O) 2 \u2014(C 1 -C 6  alkyl), phenyl, or a heteroaryl group with 5 to 10 ring members containing 1, 2, or 3 heteroatoms selected from N, O, or S, a C 3 -C 8  cycloalkyl group, or a 3 to 7 membered heterocyclyl group containing 1, 2, or 3 heteroatoms selected from N, O, or S, and the Q heterocyclyl group and the Q cycloalkyl group may be substituted with 1 oxo R Q  substituent, and the R Q  cycloalkyl group and the R Q  heterocyclyl group may be unsubstituted or substituted with 1 or 2 substituents independently selected from F, \u2014Cl, \u2014Br, \u2014I, \u2014CN, \u2014C 1 -C 6  alkyl, \u2014C 1 -C 6  haloalkyl, \u2014C 1 -C 6  perhaloalkyl, \u2014C 2 -C 6  alkenyl, \u2014C 2 -C 6  alkynyl, \u2014OH, \u2014O\u2014(C 1 -C 6  alkyl), \u2014O\u2014(C 1 -C 6  haloalkyl), \u2014O\u2014(C 1 -C 6  perhaloalkyl), \u2014NH 2 , \u2014NH(C 1 -C 6  alkyl), \u2014N(C 1 -C 6  alkyl) 2 , \u2014C(\u2550O)\u2014(C 1 -C 6  alkyl), \u2014C(\u2550O)OH, \u2014C(\u2550O)\u2014O\u2014(C 1 -C 6  alkyl), \u2014C(\u2550O)NH 2 , \u2014C(\u2550O)NH(C 1 -C 6  alkyl), or \u2014C(\u2550O)N(C 1 -C 6  alkyl) 2 ; \n R 4  is selected from a monocyclic or bicyclic C 6 -C 10  aryl group, a monocyclic or bicyclic heteroaryl group with 5 to 10 ring members containing 1, 2, or 3 heteroatoms independently selected from N, O, or S, or a monocyclic or bicyclic heterocyclyl group with 5 to 10 ring members containing 1, 2, 3, or 4 heteroatoms independently selected from N, O, or S, wherein the C 6 -C 10  aryl group, the heteroaryl group, or the heterocyclyl group are unsubstituted or are substituted with 1, 2, or 3 R 4a  substituents; \n R 4a  in each instance is independently selected from \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014CN, \u2014C 1 -C 6  alkyl, \u2014C 1 -C 6  haloalkyl, \u2014C 1 -C 6  perhaloalkyl, \u2014OH, \u2014O\u2014(C 1 -C 6  alkyl), \u2014O\u2014(C 1 -C 6  haloalkyl), \u2014O\u2014(C 1 -C 6  perhaloalkyl), \u2014NH 2 , \u2014NH(C 1 -C 6  alkyl), \u2014N(C 1 -C 6  alkyl) 2 , \u2014C(\u2550O)\u2014(C 1 -C 6  alkyl), \u2014C(\u2550O)OH, \u2014C(\u2550O)\u2014O\u2014(C 1 -C 6  alkyl), \u2014C(\u2550O)NH 2 , \u2014C(\u2550O)NH(C 1 -C 6  alkyl), or \u2014C(\u2550O)N(C 1 -C 6  alkyl) 2 , and the heterocyclyl R 4  group may be further substituted with 1 oxo substituent; and \n further wherein: \n if R 4  is an unsubstituted or substituted phenyl ring and R 3  is a group of formula \u2014(CR 3b \u2550CR 3c )-Q, then at least one of the following is true:\n a) R 4  is substituted with at least one \u2014O\u2014(C 1 -C 6  alkyl) group; \n b) Q is not an oxadiazole; \n c) R 3b  is not \u2014H; \n d) R 3c  is not \u2014H; \n e) R 1  is not a 2-pyridyl group; or \n f) R 4  is substituted with two or more \u2014O\u2014(C 1 -C 6  alkyl) groups.

Metadata:
- Claim Count in Document: 56.0
- Percentile: 95.0
- Lexical Diversity: 1.64865
- Patent Class: 544.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['15298686', '15298434', '15297487', '15945852', '15297272']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.88327904979966
- 35 USC 102 Novelty (BERT): 0.6825929568346807
- Combined Prediction Score: 0.8632104405031621
- Mean Citation Score: 707.229046
- Max Citation Score: 724.00323
- Similarity Product: 662.7634088225037

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

Dataset: test