PATENT CLAIM ANALYSIS

Application Number: 15887214
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-08
Patent Classification: ["546", "160000"]

Abstract:
Disclosed are compounds of Formula (I) or a salt thereof, wherein: A is CR 1  or N; B is CR 3  or N; D is CR 4  or N; L 1  is —(CR 7 R 7 ) m —; L 2  is —(CR 7 R 7 ) n —; and X, Z, R 1 , R 2 , R 3 , R 4 , R 5 , and R 6  are define herein. Also disclosed are methods of using such compounds as modulators of TNFα, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

Claim (Index 6):
A compound of Formula (I): or a salt thereof, wherein: A is CR 1  or N; B is CR 3  or N; D is CR 4  or N; X is \u2014CH(OH)\u2014, \u2014C(O)\u2014, \u2014CH(NH 2 )\u2014, or \u2014NR 8 \u2014; L 1  is \u2014(CR 7 R 7 ) m \u2014; L 2  is \u2014(CR 7 R 7 ) n \u2014; Z is C 4-8  alkyl substituted with zero to 6 R q ; R 1  is H, halo, \u2014CN, C 1-4  alkyl, C 1-6  haloalkyl, or C 1-3  alkoxy; R 2  is H, R 1a , C 1-6  haloalkyl, C 2-6  alkenyl substituted with zero to 6 R 1a , C 2-6  alkynyl substituted with zero to 4 R 1a , \u2014(CR g R g ) r (3- to 14-membered carbocyclyl substituted with zero to 3 R 1a ), \u2014(CR g R g ) r (aryl substituted with zero to 3 R 1a ), \u2014(CR g R g ) r (5- to 7-membered heterocyclyl substituted with zero to 3 R 1a ), or \u2014(CR g R g ) r (mono- or bicyclic heteroaryl substituted with zero to 3 R 1a ); R 3  is H, halo, \u2014CN, \u2014CF 3 , \u2014OCF 3 , \u2014NO 2 , C 1-6  alkyl substituted with zero to 6 R 1a , \u2014(CR g R g ) r OR e , \u2014(CR g R g ) r NR c R c , \u2014(CR g R g ) r S(O) p R b , \u2014(CR g R g ) r (3- to 14-membered carbocyclyl substituted with zero to 3 R 1a ), \u2014(CR g R g ) r (aryl substituted with zero to 3 R 1a ), \u2014(CR g R g ) r (5- to 7-membered heterocyclyl substituted with zero to 3 R 1a ), or \u2014(CR g R g ) r (monocyclic heteroaryl substituted with zero to 3 R 1a ); R 4  is H, halo, \u2014CN, C 1-4  alkyl, C 1-6  haloalkyl, or C 1-3  alkoxy; R 5  is H, halo, \u2014OH, \u2014CN, C 1-5  alkyl substituted with zero to 6 R a , C 3-6  cycloalkyl substituted with zero to 6 R a , C 1-5  alkylthio substituted with zero to 6 R a , arylthio substituted with zero to 6 R a , C 1-5  alkoxy substituted with zero to 6 R a , aryloxy substituted with zero to 6 R a , \u2014C(O)OR h , \u2014C(O)NR h R h , \u2014NR h R h , \u2014NR b C(O)NR c R c , \u2014NR h C(O)R y , \u2014NR b C(O)OR b , \u2014NR b S(O) 2 NR c R c , or \u2014NR h S(O) 2 R y ; R 6  is F, Cl, or \u2014CH 3 ; each R 7  is independently H, \u2014OH, C 1-3  alkyl, C 1-3  fluoroalkyl, C 1-3  hydroxyalkyl, C 1-2  aminoalkyl, \u2014CH 2 CH\u2550CH 2 , C 3-6  cycloalkyl, phenyl or \u2014NR h R h ; or two R 7  along with the carbon atom to which they are attached form a 3- to 7-membered spirocarbocyclyl or spiroheterocyclyl group; R 8  is H or C 1-3  alkyl; each R 1a  is independently F, Cl, Br, \u2014CN, C 1-6  alkyl substituted with zero to 6 R a , C 3-6  cycloalkyl substituted with zero to 6 R a , C 1-3  alkoxy substituted with zero to 7 R a , heterocyclyl substituted with zero to 6 R a , aryl substituted with zero to 6 R a , mono- or bicyclic heteroaryl substituted with zero to 6 R a , \u2014C(O)R b , \u2014C(O)OR b , \u2014C(O)NR c R c , \u2014OC(O)R b , \u2014OC(O)NR c R c , \u2014OC(O)OR d , \u2014NR c R c , \u2014NR b C(O)R d , \u2014NR b C(O)OR d , \u2014NR b S(O) p R d , \u2014NR b C(O)NR c R c , \u2014NR b S(O) p NR c R c , \u2014S(O) p R b , \u2014S(O) p NR c R c , or \u2014C(O)NR b (CH 2 ) 1-3 NR c R c ; each R a  is independently halo, \u2014CN, \u2014OH, \u2014NO 2 , \u2014NH 2 , \u2014N 3 , C 1-7  alkyl substituted with zero to 6 R w ; C 2-4  alkenyl, C 2-4  alkynyl, C 1-3  alkoxy, C 1-3  fluoroalkoxy, C 1-3  hydroxyalkoxy, \u2014O(CH\u2550CH 2 ), \u2014(CH 2 ) r C(O)OH, \u2014O(CH 2 ) r C(O)OH, \u2014(CH 2 ) r C(O)(C 1-6  alkyl), \u2014C(O)O(C 1-4  alkyl), \u2014OC(O)(C 1-3  alkyl), \u2014NH(C 1-6  alkyl), \u2014N(C 1-3  alkyl) 2 , \u2014(CH 2 ) 0-2 C(O)NH 2 , \u2014(CH 2 ) 0-2 C(O)NH(C 1-3  alkyl), \u2014(CH 2 ) 0-2 C(O)N(C 1-3  alkyl) 2 , \u2014OC(O)NH(C 1-3  alkyl), \u2014C(O)CH(NH 2 )(CH 2 ) 1-2 C(O)OH, \u2014C(O)CH(NH 2 )(CH 2 ) 1-2 OH, \u2014C(O)(CH 2 ) 1-2 C(O)OH, \u2014C(O)(C 2-4  alkenyl), \u2014C(O)(C 2-4  alkynyl), \u2014C\u2261CH, \u2014C\u2261C(phenyl), \u2014NHC(O)NH 2 , \u2014NHC(O)NH(C 1-3  alkyl), \u2014CH\u2550NOH, \u2014C(\u2550NH)(NH 2 ), C 3-7  carbocyclyl, aryl, 5- to 7-membered heterocyclyl, monocyclic or bicyclic heteroaryl, \u2014(CH 2 ) r (aryl), \u2014(CH 2 ) r (heteroaryl), \u2014O(aryl), \u2014O(benzyl), \u2014O(heterocyclyl), \u2014O(heteroaryl), \u2014S(O) 2 NH 2 , \u2014S(O) 2 CH 2 CH 2 C(O)O(C 1-3  alkyl), \u2014S(O) p (C 1-3  alkyl), \u2014S(O) p (aryl), \u2014S(O) p (heterocyclyl), \u2014NHS(O) 2 (aryl), \u2014NHS(O) 2 (heterocyclyl), \u2014NHS(O) 2 NH(aryl), \u2014NHS(O) 2 NH(heterocyclyl), \u2014NH(aryl substituted with zero to 3 R x ), \u2014NH(heterocyclyl), \u2014NHC(O)(aryl), \u2014NHC(O)(C 1-3  alkyl), \u2014NHC(O)(heterocyclyl), \u2014OC(O)(aryl), \u2014OC(O)(heterocyclyl), \u2014NHC(O)NH(aryl), \u2014NHC(O)NH(heterocyclyl), \u2014OC(O)O(C 1-3  alkyl), \u2014OC(O)O(aryl), \u2014OC(O)O(heterocyclyl), \u2014OC(O)NH(aryl), \u2014OC(O)NH(heterocyclyl), \u2014NHC(O)O(aryl), \u2014NHC(O)O(heterocyclyl), \u2014NHC(O)O(C 1-4  alkyl), \u2014C(O)NH(aryl), \u2014C(O)NH(heterocyclyl), \u2014C(O)O(aryl), \u2014C(O)O(heterocyclyl), \u2014N(C 1-3  alkyl)S(O) 2 (aryl), \u2014N(C 1-3  alkyl)S(O) 2 (heterocyclyl), \u2014N(C 1-3  alkyl)S(O) 2 NH(aryl), \u2014N(C 1-3  alkyl)S(O) 2 NH(heterocyclyl), \u2014N(C 1-3  alkyl)(aryl), \u2014N(C 1-3  alkyl)(heterocyclyl), \u2014N(C 1-3  alkyl)C(O)(aryl), \u2014N(C 1-3  alkyl)C(O)(heterocyclyl), \u2014N(C 1-3  alkyl)C(O)NH(aryl), \u2014(CH 2 ) 0-3 C(O)NH(heterocyclyl), \u2014OC(O)N(C 1-3  alkyl)(aryl), \u2014OC(O)N(C 1-3  alkyl)(heterocyclyl), \u2014N(C 1-3  alkyl)C(O)O(aryl), \u2014N(C 1-3  alkyl)C(O)O(heterocyclyl), \u2014C(O)N(C 1-3  alkyl)(aryl), \u2014C(O)N(C 1-3  alkyl)(heterocyclyl), \u2014NHS(O) 2 N(C 1-3  alkyl)(aryl), \u2014NHS(O) 2 N(C 1-3  alkyl)(heterocyclyl), \u2014NHP(O) 2 N(C 1-3  alkyl)(aryl), \u2014NHC(O)N(C 1-3  alkyl)(aryl), \u2014NHC(O)N(C 1-3  alkyl)(heterocyclyl), \u2014N(C 1-3  alkyl)S(O) 2 N(C 1-3  alkyl)(aryl), \u2014(CH 2 ) 0-2 C(O)NHS(O) 2 (C 1-3  alkyl), \u2014N(C 1-3  alkyl)S(O) 2 N(C 1-3  alkyl)(heterocyclyl), \u2014N(C 1-3  alkyl)C(O)N(C 1-3  alkyl)(aryl), \u2014N(C 1-3  alkyl)C(O)N(C 1-3  alkyl)(heterocyclyl), or \u2014Si(C 1-3  alkyl) 3 , wherein each of said carbocyclyl, aryl, heterocyclyl, and heteroaryl is substituted with zero to 4 R z ; or two R a  attached to the same carbon atom form \u2550O; each R b  is independently H, C 1-6  alkyl substituted with zero to 6 R f , C 3-7  cycloalkyl substituted with zero to 6 R f , heterocyclyl substituted with zero to 6 R f , aryl substituted with zero to 3 R f , or mono- or bicyclic heteroaryl substituted with zero to 3 R f ; each R e  is independently H, C 1-6  alkyl substituted with zero to 6 R f , C 3-7  cycloalkyl substituted with zero to 6 R f , heterocyclyl substituted with zero to 6 R f , aryl substituted with zero to 3 R f , or mono- or bicyclic heteroaryl substituted with zero to 3 R f ; or two R c  attached to the same nitrogen atom form a 4- to 8-membered heterocyclic ring substituted with zero to 3 R g ; each R d  is independently H, C 1-6  alkyl substituted with zero to 6 R f , C 3-7  cycloalkyl substituted with zero to 6 R f , heterocyclyl substituted with zero to 6 R f , aryl substituted with zero to 3 R f , or mono- or bicyclic heteroaryl substituted with zero to 3 R f ; each R e  is independently H, C 1-6  alkyl substituted with zero to 7 R f , C 3-7  cycloalkyl substituted with zero to 6 R f , heterocyclyl substituted with zero to 6 R f , aryl substituted with zero to 3 R f , or mono- or bicyclic heteroaryl substituted with zero to 3 R f ; each R f  is independently H, halo, \u2014OH, \u2014CN, \u2014NH 2 , C 1-6  alkyl substituted with zero to 6 R a , C 1-3  alkoxy substituted with zero to 7 R a , C 3-7  cycloalkyl substituted with zero to 6 R a , heterocyclyl substituted with zero to 6 R a , aryl substituted with zero to 3 R a , or mono- or bicyclic heteroaryl substituted with zero to 3 R a ; each R g  is independently H, F, \u2014OH, \u2014CN, C 1-3  alkyl, \u2014CF 3 , or phenyl; each R h  is independently H, C 1-5  alkyl substituted with zero to 2 R x , C 3-7  cycloalkyl substituted with zero to 2 R x , mono- or bicyclic heterocyclyl substituted with zero to 2 R x , aryl substituted with zero to 2 R x , or mono- or bicyclic heteroaryl substituted with zero to 2 R x ; each R q  is independently H, halo, \u2014CN, \u2014OH, C 1-3  haloalkyl, or C 1-3  alkoxy; each R w  is independently F, \u2014OH, \u2014CN, \u2014NH 2 , \u2014C(O)OH, \u2014C(O)(C 1-3  alkyl), \u2014C(O)NH 2 , \u2014C(O)NH(C 1-3  alkyl), \u2014NHC(O)(C 1-3  alkyl), or \u2014C(O)NHS(O) 2 (C 1-3  alkyl); each R x  is independently H, halo, \u2014CN, C 1-4  alkyl, C 1-6  haloalkyl, or C 1-3  alkoxy; each R y  is independently C 1-5  alkyl; each R z  is independently H, halo, \u2014CN, C 1-4  alkyl, C 1-4  hydroxyalkyl, C 1-6  haloalkyl, C 1-3  alkoxy, \u2014NH 2 , \u2014NH(C 1-3  alkyl), \u2014N(C 1-3  alkyl) 2 , \u2014OC(O)(C 1-4  alkyl), \u2014C(O)OH, \u2014CH 2 C(O)OH, \u2014CH 2 (phenyl), \u2014CH 2 CH 2 (morpholinyl), \u2014C(O)(morpholinyl), C 3-6  cycloalkyl, and morpholinyl; or two R z  attached to the same carbon atom form \u2550O; m is zero, 1, 2, 3, or 4; n is zero, 1, 2, 3, or 4; each p is independently zero, 1, or 2; and each r is independently zero, 1, 2, 3, or 4.

Metadata:
- Claim Count in Document: 3.0
- Percentile: 88.0
- Lexical Diversity: 2.06897
- Patent Class: 546.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['15749611', '15558692', '15558708', '15558724', '14588470']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8434819811922902
- 35 USC 102 Novelty (BERT): 0.5586419765120796
- Combined Prediction Score: 0.8149979807242692
- Mean Citation Score: 430.14112400000016
- Max Citation Score: 456.6969
- Similarity Product: 355.81505953758364

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