PATENT CLAIM ANALYSIS

Application Number: 15774655
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-10
Patent Classification: ["514", "210000"]

Abstract:
In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , L, R 4 , Q and R 5  are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

Claim (Index 1):
A compound having the structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is selected from the group consisting of \u2014N\u2014 and \u2014CH\u2014; R 1  is selected from the group consisting of H, methyl, and halogen; R 2  is selected from the group consisting of H and halogen; R 4  is selected from the group consisting of H and methyl; L is a bond and R 3  is selected from the group consisting of \u2014(C 1 -C 6 )alkyl and \u2014(C 1 -C 6 )alkyl-OH; or, alternatively, L is a divalent moiety selected from the group consisting of \u2014C(O)\u2014 and \u2014S(O) 2 \u2014; and R 3  is \u2014N(R N1 )(R N2 ), wherein:\n R N1  is selected from the group consisting of H and \u2014(C 1 -C 6 )alkyl; and \n R N2  is selected from the group consisting of: H, \u2014(C 1 -C 6 )alkyl, \u2014O\u2014(C 1 -C 6 )alkyl, \u2014OH, halogen, \u2014CN, and \u2014(C 1 -C 6 )alkyl which is substituted with 1 or 2 groups independently selected from:\n \u2014OH, halogen, \u2014CN, \n optionally substituted phenyl, (wherein said optional substitutents on said phenyl are 1 to 3 groups independently selected from OH, CN, \u2014(C 1 -C 4 )alkyl, \u2014(C 1 -C 4 )alkoxyl), \n optionally substituted heteroaryl, (wherein said optional substituents on said heteroaryl are 1 to 3 groups independently selected from \u2014(C 1 -C 6 )alkyl, \u2014(C 1 -C 4 )alkoxyl, and cyclopropyl), \n optionally substituted cyclopropyl (wherein said optional substituents on said cyclopropyl are 1 to 3 groups independently selected from \u2014(C 1 -C 6 )alkyl), and \n optionally substituted heterocycloalkyl (wherein said optional substitutents on said heterocycloalkyl are 1 to 3 groups independently selected from halogen \u2014OH, oxo, CN, and \u2014(C 1 -C 6 )alkyl, \n \n or, alternatively, R N1  and R N2  are taken together with the nitrogen atom to which they are shown attached to form a 4-, 5-, or 6-membered fully saturated heterocyclic ring comprising (including said nitrogen atom) 1, 2, or 3 ring heteroatoms selected from the group consisting of N, N-oxide, O, S, and S-oxide,\n wherein said heterocyclic ring is unsubstituted or substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen \u2014OH, oxo, CN, \u2014(C 1 -C 6 )alkyl, amino-substituted \u2014(C 1 -C 6 )alkyl (wherein said amino is 1, 2, or 3 groups independently selected from the group consisting of \u2014NH 2 , \u2014N(C 1 -C 4 alkyl) 2 , and \u2014NH(C 1 -C 4 alkyl)), \u2014O\u2014(C 1 -C 6 )alkyl, \u2014(C 1 -C 6 )alkyl-OH, \u2014(C 1 -C 6 )haloalkyl, \u2014C(O)O\u2014(C 1 -C 6 )alkyl, cyclopropyl, spirocyclopropyl, \u2014CH 2 \u2014NHC(O)O\u2014(C 1 -C 6 )alkyl, \u2014CH 2 \u2014N(CH 3 )C(O)O\u2014(C 1 -C 6 )alkyl, phenyl, benzyl, \u2014NHC(O)-phenyl, heteroaryl, and \u2014(C 1 -C 4 )alkylheteroaryl, heterocycloalkyl; \n \n Q is a bond or a divalent moiety selected from the group consisting of \u2014C(O)\u2014, \u2014S(O) 2 \u2014, and \u2014C(O)O\u2014; and R 5  is selected from the group consisting of: \u2014C(R 5A )(R 5B )(R 5C ), wherein:\n each of R 5A , R 5B  and R 5C  is independently selected from the group consisting of: H, halogen, OH, \u2014(C 1 -C 6 )alkyl, \u2014(C 1 -C 6 )haloalkyl, \u2014(C 1 -C 6 )alkenyl, \u2014(C 1 -C 6 )alkynyl, \u2014(C 3 -C 6 )cycloalkyl, \u2014(C 3 -C 6 )cycloalkyl substituted with \u2014(C 1 -C 6 )alkyl, \u2014(C 1 -C 6 )alkenyl, \u2014(C 1 -C 6 )alkynyl, phenyl, phenyl substituted with from 1 to 3 groups independently selected from halogen, \u2014(C 1 -C 6 )alkyl, \u2014O\u2014(C 1 -C 6 )alkyl, and \u2014C(O)O\u2014(C 1 -C 6 )alkyl, \n wherein:\n \u2003n is an integer from 1 to 4; and R 5D  is selected from the group consisting of H, \u2014(C 1 -C 6 )alkyl, \u2014(C 1 -C 6 )haloalkyl, phenyl, and phenyl substituted with from 1 to 3 groups independently selected from the group consisting of OH, halogen, \u2014(C 1 -C 6 )alkyl, and \u2014O\u2014(C 1 -C 6 )alkyl, and \n phenyl, wherein:\n said phenyl is unsubstituted or substituted with 1, 2, or 3 groups independently selected from the group consisting of halogen, CN, \u2014(C 1 -C 6 )alkyl, and \u2014(C 1 -C 6 )haloalkyl.

Metadata:
- Claim Count in Document: 14.0
- Percentile: 93.0
- Lexical Diversity: 1.51282
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15774157', '14721262', '15204422', '14657179', '15182749']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7834439692970004
- 35 USC 102 Novelty (BERT): 0.5612162711364611
- Combined Prediction Score: 0.7612211994809465
- Mean Citation Score: 340.497268
- Max Citation Score: 447.61417
- Similarity Product: 368.0687640458328

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

Dataset: test