PATENT CLAIM ANALYSIS

Application Number: 16007532
Application Type: Utility
Filing Date: 2018-06
Publication Date: 2018-10
Patent Classification: ["548", "159000"]

Abstract:
Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.

Claim (Index 1):
A method of treating a disease comprising administering to a human subject a compound,\n wherein the disease is a fibrotic disease of the lung, a fibrotic disease of the liver, or a fibrotic disease of the skin; wherein the compound is a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein one of X 1 , X 2 , X 3 , and X 4  is and the remaining members of X 1 , X 2 , X 3 , and X 4  are independently N or G is hydrogen, \u2014C 1-8  alkyl, \u2014C 3-10  cycloalkyl, \u2014C 1-6  alkylene-C 3-10  cycloaklyl, heterocyclyl, \u2014C 1-6  alkylene-C 3-10  heterocyclyl, phenyl, heteroaryl, or NR h R k , where the alkyl, alkylene, cycloalkyl, heterocyclyl, phenyl, and heteroaryl groups are optionally substituted one or more times with substituents independently selected from R c ; L is \u2014CH 2 \u2014C(O)N(R 6 )\u2014, \u2014C(O)N(R 6 )\u2014, \u2014C(O)\u2014O\u2014, \u2014SO 2 \u2014, \u2014C(O)\u2014, heteroarylene optionally substituted one or more times with substituents independently selected from R x , or heterocyclylene optionally substituted one or more times with substituents independently selected from R x ; or the group -L-G is -cyano; R 1  is hydrogen, R a , phenyl, or heteroaryl, where the phenyl and heteroaryl groups are optionally substituted one or more times with substituents independently selected from R x ; R 2  is R b ; R 3  is hydrogen, \u2014C 1-6  alkyl, or \u2014C 1-6  alkylene-C 3-10  cycloaklyl, where the alkyl, alkylene, and cycloalkyl groups are optionally substituted one or more times with substituents independently selected from R z ; R 4  is \u2014C 1-6  alkyl or \u2014C 1-6  alkylene-C 3-10  cycloaklyl, where the alkyl, alkylene, and cycloalkyl groups are optionally substituted one or more times with substituents independently selected from R Y ; R 6  is hydrogen, \u2014C 1-6  alkyl, \u2014C 1-6  alkylene-C 3-10  cycloaklyl, where the alkyl, alkylene, and cycloalkyl groups are optionally substituted one or more times with substituents independently selected from R x ; R a  is\n a) -halogen, \n b) \u2014C 1-6  alkyl, \n c) \u2014C 3-10  cycloalkyl, \n d) -heterocyclyl, \n e) -cyano, \n f) \u2014CF 3 , \n g) \u2014OCF 3 , \n h) \u2014O\u2014R d , \n i) \u2014S(O) w \u2014R d , \n j) \u2014S(O) 2 O\u2014R d , \n k) \u2014NR d R e , \n l) \u2014C(O)\u2014R d , \n m) \u2014C(O)\u2014O\u2014R d , \n n) \u2014OC(O)\u2014R d , \n o) \u2014C(O)NR d R e , \n p) \u2014C(O)-heterocyclyl, \n q) \u2014NR d  C(O)R e , \n r) \u2014OC(O)NR d R e , \n s) \u2014NR d  C(O)OR d , or \n t) \u2014NR d  C(O)NR d R e , \n where the alkyl, cycloalkyl, and heterocyclyl groups are optionally substituted one or more times with substituents independently selected from R y ; \n R b  is\n a) -halogen, \n b) \u2014C 1-6  alkyl, \n c) \u2014C 3-10  cycloalkyl, \n d) -heterocyclyl, \n e) -phenyl, \n f) -heteroaryl, \n g) -cyano, \n h) \u2014CF 3 , \n i) \u2014OCF 3 , \n j) \u2014O\u2014R f , \n k) \u2014S(O) w \u2014R f , \n l) \u2014S(O) 2 O\u2014R f , \n m) \u2014NR f R g , \n n) \u2014C(O)\u2014R f , \n o) \u2014C(O)\u2014O\u2014R f , \n p) \u2014OC(O)\u2014R f , \n q) \u2014C(O)NR f R g , \n r) \u2014C(O)-heterocyclyl, \n s) \u2014NR C(O)R g , \n t) \u2014OC(O)NR f R g , \n u) \u2014NR f C(O)OR f , or \n v) \u2014NR f C(O)NR f R g , \n where the alkyl, cycloalkyl, heterocyclyl, phenyl, and heteroaryl groups are optionally substituted one or more times with substituents independently selected from R Z ; \n R c  is\n a) -halogen, \n b) \u2014C 1-6  alkyl, \n c) \u2014C 3-10  cycloalkyl, \n d) -heterocyclyl, \n e) -cyano, \n f) \u2014CF 3 , \n g) \u2014OCF 3 , \n h) \u2014O\u2014R h , \n i) \u2014S(O) w \u2014R h , \n j) \u2014S(O) 2 O\u2014R h , \n k) \u2014NR h R k , \n l) \u2014C(O)\u2014R h , \n m) \u2014C(O)\u2014O\u2014R h , \n n) \u2014OC(O)\u2014R h , \n o) \u2014C(O)NR h R k , \n p) \u2014C(O)-heterocyclyl, \n q) \u2014NR h C(O)R k , \n r) \u2014OC(O)NR h R k , \n s) \u2014NR h C(O)OR k , \n t) \u2014NR h C(O)NR h R k , \n u) \u2014NR h  S(O) w R k , \n v) -phenyl, \n w) -heteroaryl, or \n x) \u2014O\u2014(C 1-4  alkylene)-O\u2014(C 1-4  alkylene)-N(R h )C(O)\u2014OR k , \n where the alkylene, alkyl, cycloalkyl, heterocyclyl, phenyl, and heteroaryl groups are optionally substituted one or more times with substituents independently selected from R x ; \n R d  and R e  are independently hydrogen, C 1-6  alkyl, or C 3-10  cycloalkyl, where the alkyl and cycloalkyl groups are optionally substituted one or more times with substituents independently selected from R y ; or, if R d  and R e  are both attached to the same nitrogen atom, together with that nitrogen atom may optionally form a heterocyclic ring selected from the group consisting of azetidino, pyrrolidino, pyrazolidino, imidazolidino, oxazolidino, isoxazolidino, thiazolidino, isothiazolidino, piperidino, piperazino, morpholino, thiomorpholino, and azepano, where each ring is optionally substituted one or more times with substituents independently selected from R y ; R f  and R g  are independently hydrogen, C 1-6  alkyl, C 3-10  cycloalkyl, phenyl, or heteroaryl, where the alkyl, cycloalkyl, phenyl, and heteroaryl groups are optionally substituted one or more times with substituents independently selected from R z ; or, if R f  and R g  are both attached to the same nitrogen atom, together with that nitrogen atom may optionally form a heterocyclic ring selected from the group consisting of azetidino, pyrrolidino, pyrazolidino, imidazolidino, oxazolidino, isoxazolidino, thiazolidino, isothiazolidino, piperidino, piperazino, morpholino, thiomorpholino, and azepano, where each ring is optionally substituted one or more times with substituents independently selected from R z ; R h  and R k  are independently hydrogen, C 1-6  alkyl, C 3-10  cycloalkyl, heterocyclyl, phenyl, or heteroaryl, where the alkyl, cycloalkyl, heterocyclyl, phenyl, and heteroaryl groups are optionally substituted one or more times with substituents independently selected from R x ; or, if R h  and R k  are both attached to the same nitrogen atom, together with that nitrogen atom may optionally form a heterocyclic ring selected from the group consisting of azetidino, pyrrolidino, pyrazolidino, imidazolidino, oxazolidino, isoxazolidino, thiazolidino, isothiazolidino, piperidino, piperazino, morpholino, thiomorpholino, and azepano, where each ring is optionally substituted one or more times with substituents independently selected from R x ; R y  is\n a) -halogen, \n b) \u2014NH 2 , \n c) -cyano, \n d) -carboxy, \n e) -hydroxy, \n f) -thiol, \n g) \u2014CF 3 , \n h) \u2014OCF 3 , \n i) \u2014C(O)\u2014NH 2 , \n j) \u2014S(O) 2 \u2014NH 2 , \n k) oxo, \n l) \u2014C 1-6  alkyl, optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 , \n m) -heterocyclyl optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 , \n n) \u2014C 3-10  cycloalkyl optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 , \n o) \u2014O\u2014C 1-6  alkyl optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 , \n p) \u2014O\u2014C 3-10  cycloalkyl optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 , \n q) \u2014NH\u2014C 1-6  alkyl optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 , \n r) \u2014N(C 1-6  alkyl) 2  optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 , \n s) \u2014C(O)\u2014C 1-6  alkyl, optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 , \n t) \u2014C(O)\u2014O\u2014C 1-6  alkyl, optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 , \n u) \u2014S\u2014C 1-6  alkyl, optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 , \n v) \u2014S(O) 2 \u2014C 1-6  alkyl, optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 , \n w) \u2014C(O)\u2014NH\u2014C 1-6  alkyl, optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 , \n x) \u2014C(O)\u2014N(C 1-6  alkyl) 2 , optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 , \n y) \u2014S(O) 2 \u2014NH\u2014C 1-6  alkyl, optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 , \n z) \u2014S(O) 2 \u2014N(C 1-6  alkyl) 2 , optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 , \n aa) \u2014NH\u2014C(O)\u2014C 1-6  alkyl, optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 , or \n bb) \u2014NH\u2014S(O) 2 \u2014C 1-6  alkyl, optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 ; \n R x  is\n a) \u2014R y  \n b) -phenyl, optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 , \n c) -heteroaryl, optionally substituted one or more times with substituents selected independently from the group consisting of halogen, \u2014OH, \u2014O\u2014C 1-6  alkyl, \u2014NH 2 , \u2014NH\u2014C 1-6  alkyl, and \u2014N(C 1-6  alkyl) 2 , \n d) \u2014O-phenyl, \n e) \u2014O-heteroaryl, \n f) \u2014C(O)-phenyl, \n g) \u2014C(O)-heteroaryl, \n h) \u2014C(O)\u2014O-phenyl, or \n i) \u2014C(O)\u2014O-heteroaryl; \n R z  is\n a) \u2014R y  \n b) -phenyl, \n c) -heteroaryl; \n d) \u2014O-phenyl, \n e) \u2014O-heteroaryl, \n f) \u2014C(O)-phenyl, \n g) \u2014C(O)-heteroaryl, \n h) \u2014C(O)\u2014O-phenyl, or \n i) \u2014C(O)\u2014O-heteroaryl; \n v is an integer from 0 to 4, and w is an integer from 0 to 2.

Metadata:
- Claim Count in Document: 56.0
- Percentile: 94.0
- Lexical Diversity: 1.59375
- Patent Class: 548.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14215873', '13028406', '15584459', '11704431', '12446088']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7538471926962678
- 35 USC 102 Novelty (BERT): 0.5841089523494595
- Combined Prediction Score: 0.7368733686615869
- Mean Citation Score: 422.415368
- Max Citation Score: 525.0577400000002
- Similarity Product: 395.1128018959024

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