PATENT CLAIM ANALYSIS

Application Number: 15743424
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2018-08
Patent Classification: ["546", "276700"]

Abstract:
The invention provides compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, wherein D 1 , D 2 , D 3 , X, Y, A 1 , A 2 , R 1 , R 5  and the subscript a are as described herein. The compounds are CETP inhibitors and are useful for raising FIDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis:

Claim (Index 1):
A compound of Formula I, or a pharmaceutically acceptable salt thereof: wherein:\n X is \u2014C(\u2550O)\u2014, \u2014S(O) 2 \u2014, \u2014C(\u2550S)\u2014, or \u2014C(\u2550NR);\n R is H, \u2014CN, \u2014C 1 -C 5  alkyl, phenyl, C 3 -C 6  cycloalkyl optionally having 1-2 double bonds, or HET(3),\n wherein when R is phenyl, C 3 -C 6  cycloalkyl, or HET(3), R is optionally substituted with 1-5 substituent groups which are each independently halogen, \u2014CN, C 1 -C 4  alkyl optionally substituted with 1-5 halogens, \u2014OC 1 -C 4  alkyl optionally substituted with 1-5 halogens, C 3 -C 6  cycloalkyl optionally substituted with 1-5 halogens, \u2014NR 6 R 7 , \u2014CO 2 R 8 , \u2014C(O)NR 6 R 7 , or \u2014SO 2 NR 6 R 7 , and \n when R is \u2014C 1 -C 5  alkyl or \u2014OC 1 -C 5  alkyl, R is optionally substituted with 1-5 substituent groups which are independently halogen, \u2014OC 1 -C 4  alkyl optionally substituted with 1-5 halogens, \u2014CN, C 3 -C 6  cycloalkyl optionally substituted with 1-5 halogens, \u2014NR 6 R 7 , \u2014CO 2 R 8 , \u2014C(O)NR 6 R 7 , or \u2014SO 2 NR 6 R 7 ; \n \n \n Y is \u2014CHR 9 \u2014 or S;\n R 9  is H or \u2014C 1 -C 5 alkyl optionally substituted with 1-11 halogens; \n \n R 1  is H, \u2014C 1 -C 5  alkyl, \u2014OC 1 -C 5  alkyl, \u2014C 2 -C 5  alkenyl, \u2014OC 2 -C 5  alkenyl, \u2014C 2 -C 5  alkynyl, \u2014OC 2 -C 5  alkynyl, \u2014OH, halogen, \u2014CN, \u2014NR 6 R 7 , \u2014CO 2 R 8 , \u2014C(O)NR 6 R 7 , \u2014SO 2 NR 6 R 7 , HET(3), or C 3 -C 6  cycloalkyl optionally having 1-2 double bonds,\n wherein said \u2014C 1 -C 5  alkyl, \u2014OC 1 -C 5  alkyl, \u2014C 2 -C 5  alkenyl, \u2014OC 2 -C 5  alkenyl, \u2014C 2 -C 5  alkynyl, and \u2014OC 2 -C 5  alkynyl of R 1  are each optionally substituted with 1-7 halogens, and \n said HET(3) and C 3 -C 6  cycloalkyl optionally having 1-2 double bonds of R 1  are optionally substituted with 1-3 substituent groups which are each independently halogen, \u2014C 1 -C 3  alkyl, \u2014OC 1 -C 3  alkyl, \u2014C 2 -C 3  alkenyl, \u2014OC 2 -C 3  alkenyl, \u2014C 2 -C 3  alkynyl, or \u2014OC 2 -C 3  alkynyl,\n wherein \u2014C 1 -C 3  alkyl, \u2014OC 1 -C 3  alkyl, \u2014C 2 -C 3  alkenyl, \u2014OC 2 -C 3  alkenyl, \u2014C 2 -C 3  alkynyl, and \u2014OC 2 -C 3  alkynyl are each optionally substituted with 1-7 halogens; \n \n \n R 6  and R 7  are each independently H, \u2014C 1 -C 5  alkyl, phenyl, naphthyl, C 3 -C 6  cycloalkyl optionally having 1-2 double bonds, or HET(3),\n wherein said phenyl, naphthyl, C 3 -C 6  cycloalkyl, and HET(3) of R 6  and R 7  are optionally substituted with 1-3 substituent groups which are each independently halogen, \u2014C 1 -C 3  alkyl, \u2014OC 1 -C 3  alkyl, \u2014C 2 -C 3  alkenyl, \u2014OC 2 -C 3  alkenyl, \u2014C 2 -C 3  alkynyl, or \u2014OC 2 -C 3  alkynyl,\n wherein \u2014C 1 -C 3  alkyl, \u2014OC 1 -C 3  alkyl, \u2014C 2 -C 3  alkenyl, \u2014OC 2 -C 3  alkenyl, \u2014C 2 -C 3 alkynyl, and \u2014OC 2 -C 3  alkynyl are each optionally substituted with 1-7 halogens; \n \n \n R 8  is H or \u2014C 1 -C 5  alkyl optionally substituted with 1-7 halogens; \n HET(3) is a 3-6 membered heterocyclic ring having 1-3 heteroatom groups which are each independently N, NH, O, S, S(O), or S(O) 2  and optionally having 1-3 double bonds; \n the dashed line in Formula I represents an optional double bond; \n D 1  is N or CR 2 ; \n D 2  is N or CR 3 ; \n D 3  is N or CR 4 ; \n R 2 , R 3 , and R 4  are each independently H, \u2014C 1 -C 5  alkyl, \u2014OC 1 -C 5  alkyl, \u2014C 2 -C 5  alkenyl, \u2014OC 2 -C 5  alkenyl, \u2014C 2 -C 5  alkynyl, \u2014OC 2 -C 5  alkynyl, \u2014OH, halogen, \u2014CN, \u2014NR 6 R 7 , \u2014CO 2 R 8 , \u2014C(O)NR 6 R 7 , or \u2014SO 2 NR 6 R 7 ,\n wherein said \u2014C 1 -C 5  alkyl, \u2014OC 1 -C 5  alkyl, \u2014C 2 -C 5  alkenyl, \u2014OC 2 -C 5  alkenyl, \u2014C 2 -C 5  alkynyl, and \u2014OC 2 -C 5  alkynyl of R 2 , R 3 , and R 4  are optionally substituted with 1-7 halogens; \n \n each R 5  is independently \u2014C 1 -C 5  alkyl, \u2014OC 1 -C 5  alkyl, \u2014C 2 -C 5  alkenyl, \u2014OC 2 -C 5  alkenyl, \u2014C 2 -C 5  alkynyl, \u2014OC 2 -C 5  alkynyl, \u2014OH, halogen, \u2014CN, \u2014NR 6 R 7 , \u2014CO 2 R 8 , \u2014C(O)NR 6 R 7 , or \u2014SO 2 NR 6 R 7 ,\n wherein said \u2014C 1 -C 5  alkyl, \u2014OC 1 -C 5  alkyl, \u2014C 2 -C 5  alkenyl, \u2014OC 2 -C 5  alkenyl, \u2014C 2 -C 5  alkynyl, and \u2014OC 2 -C 5  alkynyl of R 5  are optionally substituted with 1-7 halogens; \n \n A 1  is phenyl, HET(1), or C 3 -C 8  cycloalkyl optionally having 1-2 double bonds, wherein A 1  is optionally substituted with one substituent group Z and is optionally substituted with 1-3 groups which are each independently \u2014C 1 -C 5  alkyl, \u2014OC 1 -C 5  alkyl, \u2014C 2 -C 5  alkenyl, \u2014OC 2 -C 5  alkenyl, \u2014C 2 -C 5  alkynyl, \u2014OC 2 -C 5  alkynyl, halogen, \u2014OH, or \u2014CN,\n wherein said \u2014C 1 -C 5  alkyl, \u2014OC 1 -C 5  alkyl, \u2014C 2 -C 5  alkenyl, \u2014OC 2 -C 5  alkenyl, \u2014C 2 -C 5  alkynyl, and \u2014OC 2 -C 5  alkynyl are optionally substituted with 1-7 halogens; \n \n HET(1) is a 5- or 6-membered heterocyclic ring having 1-4 heteroatom groups which are each independently \u2014N\u2014, \u2014NH\u2014, \u2014S\u2014, \u2014O\u2014, \u2014S(O)\u2014, or \u2014S(O) 2 \u2014, optionally having one group \u2014C(\u2550O)\u2014, and optionally having 1-3 double bonds; \n Z is A 3 , \u2014C 1 -C 3  alkylene-CO 2 R 8 , \u2014C 1 -C 3 alkylene-C(O)NR 6 R 7 , \u2014C 1 -C 3  alkylene-SO 2 NR 6 R 7 , \u2014CO 2 R 8 , \u2014C(O)NR 6 R 7 , \u2014SO 2 NR 6 R 7 , or \u2014C 1 -C 3 alkylene-HET(2),\n wherein said \u2014C 1 -C 3  alkylene in all uses of Z is optionally substituted with 1-7 halogens, and HET(2) is optionally substituted with 1-3 substituents which are independently \u2014C 1 -C 3 alkyl optionally substituted with 1-5 halogens, \u2014OC 1 -C 3  alkyl optionally substituted with 1-5 halogens, halogen or NR 6 R 7 ; \n \n A 3  is phenyl, C 3 -C 6  cycloalkyl optionally having 1-2 double bonds, or HET(1),\n wherein A 3  is optionally substituted with 1-3 groups which are each independently \u2014C 1 -C 5  alkyl, \u2014OC 1 -C 5  alkyl, \u2014C 2 -C 5  alkenyl, \u2014OC 2 -C 5  alkenyl, \u2014C 2 -C 5  alkynyl, \u2014OC 2 -C 5  alkynyl, halogen, \u2014OH, or \u2014CN,\n wherein said \u2014C 1 -C 5  alkyl, \u2014OC 1 -C 5  alkyl, \u2014C 2 -C 5  alkenyl, \u2014OC 2 -C 5  alkenyl, \u2014C 2 -C 5  alkynyl, and \u2014OC 2 -C 5  alkynyl are optionally substituted with 1-7 halogens; and \n \n wherein A 3  is optionally substituted with one group which is HET(2), \u2014C 1 -C 4  alkylene-CO 2 R 8 , \u2014C 1 -C 4 alkylene \u2014C(O)NR 6 R 7 , \u2014C 1 -C 4 alkylene-SO 2 NR 6 R 7 , \u2014CO 2 R 8 , \u2014C(O)NR 6 R 7 , \u2014SO 2 NR 6 R 7 , or \u2014C(O)NR 6 C 3 -C 6 cycloalkyl;\n wherein said C 3 -C 6  cycloalkyl of \u2014C(O)NR 6 C 3 -C 6 cycloalkyl is optionally substituted with 1-3 substituents which are independently selected from halogen, C 1 -C 2 alkyl, and \u2014CN, \n wherein \u2014C 1 -C 4 alkylene in all uses of said optional substituents of A 3  is optionally substituted with 1-7 halogens; and \n wherein HET(2) is optionally substituted with 1-3 groups which are each independently halogen, \u2014C 1 -C 5  alkyl optionally substituted with 1-7 halogens, \u2014OC 1 -C 5 alkyl optionally substituted with 1-7 halogens, or NR 6 R 7 ; \n \n \n HET(2) is a 5-6 membered heterocyclic ring having 1-3 heteroatom groups which are each independently N, NH, O, or S, optionally having one group \u2014C(\u2550O)\u2014, and optionally having 1-3 double bonds; \n A 2  is phenyl or HET(1), wherein A 2  is optionally substituted with 1-3 substituent groups which are each independently \u2014C 1 -C 5  alkyl, \u2014OC 1 -C 5  alkyl, \u2014C 2 -C 5  alkenyl, \u2014OC 2 -C 5  alkenyl, \u2014C 2 -C 5 alkynyl, \u2014OC 2 -C 5 alkynyl, halogen, \u2014CN, \u2014OH, or C 3 -C 6 cycloalkyl,\n wherein \u2014C 1 -C 5  alkyl, \u2014OC 1 -C 5  alkyl, \u2014C 2 -C 5  alkenyl, \u2014OC 2 -C 5  alkenyl, \u2014C 2 -C 5  alkynyl, and \u2014OC 2 -C 5  alkynyl are optionally substituted with 1-7 halogens, and \n C 3 -C 6 cycloalkyl is optionally substituted with 1-3 substituents which are each independently halogen, \u2014C 1 -C 3  alkyl, or \u2014OC 1 -C 3  alkyl,\n wherein-C 1 -C 3  alkyl and \u2014OC 1 -C 3  alkyl are each optionally substituted with 1-7 halogens; and \n \n \n a is 0 or an integer from 1-3.

Metadata:
- Claim Count in Document: 16.0
- Percentile: 86.0
- Lexical Diversity: 1.63043
- Patent Class: 546.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['14908180', '13660010', '15329284', '15104351', '15028306']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8432931426291411
- 35 USC 102 Novelty (BERT): 0.5633061631144967
- Combined Prediction Score: 0.8152944446776766
- Mean Citation Score: 434.067694
- Max Citation Score: 454.36414
- Similarity Product: 393.4973533951497

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

Dataset: test