PATENT CLAIM ANALYSIS

Application Number: 16025199
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2018-10
Patent Classification: ["514", "364000"]

Abstract:
This invention pertains to the use of fused bicycle heterocyclic adducts of thiohydroxy pyridines or pyrimidines as diacylglycerol O-acyltransferase 1 (DGAT-1) inhibitors to treat hyperlipidiemias and various diseases and disorders associated therewith. Other conditions also be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease.

Claim (Index 1):
A compound of Formula (I), pharmaceutically acceptable salts or stereoisomers thereof,\n Q-G 1 -G 2 -G 3 -G 4 -Z\u2003\u2003Formula (I) wherein Q is: A is a fused ring selected from an aromatic 6-membered ring containing 0 or 2 N atoms; L is N or C(R 8 ); the number of R 8  substituents on A ring may be 0, 1, 2 or 3 and when two of said R substituents are: a) found on A ring: b) (C 1 -C 6 )alkyl and c) attached to adjacent carbon atoms of the Ring A, they may be joined together to form a 5 to 7-membered carbocyclic ring or they may be joined together to form a 5 to 7-membered ring containing 0, 1, 2 or 3 heteroatoms selected from O, N, S; R 8  is independently selected from halo, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 8 )alkynyl, aryl, heteroaryl, (C 3 -C 8 )cycloalkyl, cyano, (C 1 -C 6 )haloalkyl, (C 1 -C 6 )haloalkoxy, \u2014OR a , \u2014O\u2014C(O)(R a ), \u2014S(R a ), \u2014S(O)(R b ), \u2014S(O) 2 (R b ), \u2014C(O)(R a ), \u2014C(O)(OR a ), \u2014N(R a ) 2 , \u2014N(R a )\u2014C(O)(R a ), \u2014(O)N(R a ) 2 , \u2014S(O) 2 N(R a ) 2 , \u2014(CR a R b ) L OR a , \u2014(CR a R b ) r O\u2014C(O)(R a ), \u2014(CR a R b ), S(R a ), \u2014(CR a R b ) t S(O) (R b ), \u2014(CR a R b ) t S(O) 2 (R b ), \u2014(CR a R a ) t C(O)(R a ), \u2014(CR a R b ) t C(O) (OR a ), \u2014(CR a R b ) r N(R a R b )\u2014(CR a R b ) t N(R a )\u2014C(O)(R a ), \u2014(CR a R b ) t C(O)N(R a ) 2 , \u2014(CR a R a ) t S(O) 2 N(R a ) 2  or \u2014(CR a R b ) t R a , wherein t is an integer of 1, 2, 3, or 4; and R a  and R b  are independently selected from the group consisting of H, (C 1 -C 8 )alkyl, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, fluoro(C 1 -C 8 )alkyl, (C 3 -C 8 )cycloalkyl, aryl, heteroaryl and aryl(C 1 -C 4 )alkyl; G 1  and G 3  are independently selected from the group consisting of cyclo(C 3 -C 8 )alkylene, heterocyclo(C 3 -C 8 )alkylene, arylene and heteroarylene, optionally substituted with one or two groups independently selected from halo, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 1 -C 6 )alkoxy, cyano, (C 1 -C 6 )haloalkyl, (C 1 -C 6 )haloalkoxy, (C 1 -C 4 )perfluoroalkyl, \u2014N(R a R b ), \u2014N(R a )\u2014C(O)(R a ), \u2014C(O)N(R a ) 2 , \u2014S(O) 2 N(R a ) 2 , \u2014S(O) 2 (R b ), and \u2014C(O)(R a ); G 2  is selected from the group consisting of a bond, (C 1 -C 4 )alkylene, (C 2 -C 4 )alkenylene, O, N(R a )C(O), S and S(O) 2 ; G 4  is \u2014X\u2014Y\u2014; wherein X is selected from null, O, NH, CO, CHOH, S or S(O) 2 ; and Y is selected from (C 1 -C 4 )alkylene, C 3 -C 8 -cycloalkylene, heterocycloalkylene, \u2014CH(R 9 )C(R 10 R 11 )\u2014 or \u2014N(R 9 )C(R 10 R 11 )\u2014; wherein: i) R 10  and R 11  are both hydrogen, and R 9  is hydrogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, (C 2 -C 6 )alkenyl, phenoxy-(C 2 -C 6 )alkyl, 1-methyl-1H-indol-3-yl, bis[(C 1 -C 6 )alkyl]amino-(C 2 -C 6 )alkyl, 1-piperidinyl-(C 2 -C 6 )alkyl, 1-pyrrolidinyl-(C 2 -C 6 )alkyl, or 1-morpholinyl-(C 2 -C 6 )alkyl; or R 10  and R 11  are both hydrogen and R 9  is R 12 (CH 2 ) m , where m is 0 to 3, and R 12  is phenyl optionally substituted with one or more halogen, hydroxy, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, trifluoromethyl or cyano; or ii) R 10  and R 11  are both hydrogen and R 9  is R 12 (CH 2 ) m , where m is 0 to 3, and R 12  is 2-pyridinyl, 3-pyridinyl, or 4-pyridinyl, each of which is optionally substituted with halogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, trifluoromethyl or cyano; or iii) R 9  is hydrogen, and R 10  and R 11  together with the carbon atom to which they are attached, form a three to five-membered ring, with 0 to 2 heteroatoms independently selected from 0, S or N; or iv) R 10  is hydrogen, and R 9  and R 11  together with the two carbon atoms to which they are attached, form a three- to six-membered ring with 0 to 2 heteroatoms independently selected from O, S or N; Z is Z 1  or Z 2 ; and Z 1  is X 1  and X 2  are independently selected from null, (C(R a R b )) n , O, NR a , S or CO and n is 0 or 1; W is selected from H, (C 1 -C 6 )alkyl, aryl, heteroaryl or (C 3 -C 8 )cycloalkyl; wherein each of the (C 1 -C 6 )alkyl, aryl, heteroaryl and cycloalkyl is independently substituted with 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of (C 1 -C 8 )alkyl, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, \u2014CN, halogen, ethylenedioxy, methylenedioxy, haloalkyl, \u2014OR a , \u2014O\u2014C(O)(R a ), \u2014S(R a ), \u2014S(O)(R b ), \u2014S(O) 2 (R b ), \u2014C(O)(R a ), \u2014C(O)(OR a ), \u2014N(R a ) 2 , \u2014N(R a )\u2014C(O)(R a ), \u2014C(O)N(R a ) 2 , \u2014S(O) 2 N(R a ) 2 , \u2014(CR a R b ) t OR a , \u2014(CR a R b ) t \u2014O\u2014C(O)(R a ), \u2014(CR a R b ) t S(R a ), \u2014(CR a R b ) t S(O)(R b ), \u2014(CR a R b ) t S(O) 2 (R b ), \u2014(CR a R a ) t C(O)(R a ), (CR a R b ) t C(O)(OR a ), \u2014(CR a R b ) t N(R a R b )\u2014(CR a R b ) t N(R a )\u2014C(O)(R a ), \u2014(CR a R b ) t C(O)N(R a ) 2 , \u2014(CR a R a ) t S(O) 2 N(R a ) 2 , \u2014(CR a R b ) t R a , \u2014(CR a R b ) t P(O)(OH) 2 , and \u2014(CR a R b ) t P(O)(OH)(R a ), wherein t is an integer of 1, 2, 3, or 4; or X 1  and X 2  may be combined to form a 5-, 6- or 7-membered ring having from 0 to 3 heteroatoms selected from the group consisting of NR a , O and S; or X 1  or X 2  may be combined with W to form a 5-, 6- or 7-membered fused ring having from 0 to 3 heteroatoms selected from the group consisting of NR a , O and S; and Z 2  is Z 1 , H, \u2014OH, CO 2 R a  or \u2014C(O)N(R a ) 2 ; with a proviso that when X 2  is O, then X 1  is not (C(R a R b )) n .

Metadata:
- Claim Count in Document: 1.0
- Percentile: 95.0
- Lexical Diversity: 1.27273
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15151740', '13458452', '14628373', '15123791', '15866871']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7919112307824546
- 35 USC 102 Novelty (BERT): 0.5379435051747374
- Combined Prediction Score: 0.7665144582216828
- Mean Citation Score: 313.2950019999999
- Max Citation Score: 365.27896
- Similarity Product: 309.39382752682207

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