PATENT CLAIM ANALYSIS

Application Number: 15749611
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-08
Patent Classification: ["514", "394000"]

Abstract:
Disclosed are compounds of Formula (I) or a salt thereof, wherein: Ring A is 3- to 6-membered carbocyclic or heterocyclic ring; X is CR 1  or N; Y is —(CR 5 R 5 ) m —; Z is —(CR 5 R 5 ) n —; and q, R 1 , R 2 , R 3 , R 4 , R 6 , R 7 , R 8 , R 9 , and R 10  are defined 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 1):
A compound of Formula (I) or a salt thereof, wherein: Ring A is 3- to 6-membered carbocyclic or heterocyclic ring; X is CR 1  or N; Y is \u2014(CR 5 R 5 ) m \u2014; Z is \u2014(CR 5 R 5 ) n \u2014; m is zero, 1 or 2; n is zero, 1 or 2; provided that m+n is zero, 1, or 2; R 1  is H, halo, \u2014CN, C 1-4  alkyl, C 1-4  haloalkyl, or C 1-4  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 or bicyclic heteroaryl substituted with zero to 3 R 1a ); R 4  is H, halo, \u2014CN, C 1-4  alkyl, C 1-4  haloalkyl, or C 1-4  alkoxy; each R 5  is independently H, halo, \u2014CN, C 1-6  alkyl substituted with zero to 6 R h , C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, \u2014(CR g R g ) r C(O)R b , \u2014(CR g R g ) r C(O)OR b , \u2014(CR g R g ) r C(O)NR c R c , \u2014(CR g R g ) r OR e , \u2014(CR g R g ) r OC(O)R b , \u2014(CR g R g ) r OC(O)NR c R c , \u2014(CR g R g ) r OC(O)OR d , \u2014(CR g R g ) r NR c R c , \u2014(CR g R g ) r NR b C(O)R d , \u2014(CR g R g ) r NR b C(O)OR d , \u2014(CR g R g ) r NR b C(O)NR c R c , \u2014(CR g R g ) r NR b S(O) p R d , \u2014(CR g R g ) r S(O) p R b , \u2014(CR g R g ) r S(O) p NR c R c , \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 ); or two R 5  along with the carbon atom to which they are attached form C\u2550O, C\u2550NOR b , or 3- to 6-membered spirocarbocyclic or spiroheterocyclic ring substituted with zero to 3 R i ; R 6  and R 8  are independently H, halo, \u2014OH, \u2014CN, C 1-5  alkyl, C 1-5  hydroxyalkyl, C 1-5  haloalkyl, C 1-5  alkoxy, \u2014NR x R x , \u2014OC(O)NR x R x , \u2014NR x C(O)OR y , \u2014NR x C(O)R y , \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 10-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 ); each R 7  is independently halo, \u2014OH, \u2014CN, C 1-5  alkyl, C 1-5  hydroxyalkyl, C 1-5  haloalkyl, \u2014NR x R x , C 1-5  alkoxy, \u2014OC(O)NR x R x , \u2014NR x C(O)OR y , \u2014NR x C(O)R y , \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 10-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 9  is \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 10-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 10  is H, C 1-6  alkyl, or C 1-6  haloalkyl; or R 9  and R 10  together with the carbon atom to which they are attached form a 5- to 6-membered spirocarbocyclic or spiroheterocyclic ring, substituted with zero to 6 R i ; 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 6 R a , C 1-3  haloalkoxy, 5- to 7-membered 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 , C 1-3  alkyl, C 1-3  fluoroalkyl, C 2-4  alkenyl, C 2-4  alkynyl, C 1-3  alkoxy, C 1-3  fluoroalkoxy, \u2014(CH 2 ) r C(O)OH, \u2014C(O)(C 1-3  alkyl), \u2014C(O)O(C 1-4  alkyl), \u2014OC(O)(C 1-3  alkyl), \u2014NH(C 1-3  alkyl), \u2014N(C 1-3  alkyl) 2 , \u2014C(O)NH(C 1-3  alkyl), \u2014OC(O)NH(C 1-3  alkyl), \u2014NHC(O)NH(C 1-3  alkyl), \u2014C(\u2550NH)(NH 2 ), C 3-7  carbocyclyl, aryl, 5- to 7-membered heterocyclyl, mono- or bicyclic heteroaryl, \u2014O(aryl), \u2014O(benzyl), \u2014O(heterocyclyl), \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), \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 1-3  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)CO 2 H\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), \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 ; 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 , mono- or bicyclic 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 c  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 , mono- or bicyclic 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 when attached to the same nitrogen, two R c  along with the nitrogen atom to which they are attached form 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 , mono- or bicyclic 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 1-3  haloalkyl, C 3-7  cycloalkyl substituted with zero to 6 R f , mono- or bicyclic 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, C 1-6  alkyl substituted with zero to 6 R a , C 1-3  alkoxy, C 3-7  cycloalkyl substituted with zero to 6 R a , mono- or bicyclic 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 \u2014OH or halo; each R i  is independently H, halo, \u2014CN, \u2014OH, C 1-3  alkyl, C 1-3  fluoroalkyl, or C 1-3  alkoxy; or two R i  attached to the same carbon atom of the spirocarbocyclic or spiroheterocyclic ring, form \u2550O; or two R i  attached to neighboring carbon atoms of the spirocarbocyclic or spiroheterocyclic ring, form a benzo ring along with the carbon atoms to which they are attached, said benzo ring substituted with zero to 4 R f ; each R x  is independently H or C 1-5  alkyl; each R y  is independently C 1-5  alkyl; each p is independently zero, 1, or 2; q is zero, 1, or 2; and each r is independently zero, 1, 2, 3, or 4.

Metadata:
- Claim Count in Document: 5.0
- Percentile: 88.0
- Lexical Diversity: 1.8209
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['15558692', '15558724', '15558708', '15382778', '14588470']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8204386684086467
- 35 USC 102 Novelty (BERT): 0.5814415709307675
- Combined Prediction Score: 0.7965389586608588
- Mean Citation Score: 409.8369080000001
- Max Citation Score: 509.60876
- Similarity Product: 403.3147687554097

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

Dataset: test