PATENT CLAIM ANALYSIS

Application Number: 16188652
Application Type: Utility
Filing Date: 2018-11
Publication Date: 2019-03
Patent Classification: ["514", "303000"]

Abstract:
The disclosure provides pharmaceutical compositions comprising Bach1 Inhibitors and Nrf2 Activators. The disclosure also provides methods of treating diseases such as psoriasis, multiple sclerosis, and COPD comprising administering a Bach1 Inhibitor and a Nrf2 Activator to a subject in need thereof.

Claim (Index 1):
A method of treatment of a condition, comprising administering an Nrf2 activator and a Bach1 Inhibitor to a subject in need thereof,\n wherein the condition is selected from the group consisting of psoriasis, scleroderma, chronic kidney disease (CKD), asthma, chronic obstructive pulmonary disorder (COPD), fibrosis, inflammatory arthritis disease, inflammatory bowel disease (IBD), multiple sclerosis, clinically isolated syndrome (CIS), amyotrophic lateral sclerosis, Alzheimer's disease, dementia, Huntington's disease, and Parkinson's disease; wherein the Nrf2 Activator is selected from the group consisting of\n a fumaric acid mono- and/or dialkyl ester, methyl 2-cyano-3,12-dioxooleana-1,9(11)dien-28-oate, ethyl 2-cyano-3,12-dioxooleana-1,9(11)dien-28-oate, 2-cyano-3,12-dioxooleana-1,9(11)dien-28-oic acid, 1[2-Cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl]imidazole, and 2-cyano-N-methyl-3,12-dioxooleana-1,9(11)-dien-28 amide, \n wherein the Bach1 Inhibitor is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein X 1  is \u2550N\u2014; 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 ; or G is \u2014CH 2 Y 3 , \u2014CH 2 CH 2 Y 3 , \u2014CH 2 CH 2 CH 2 Y 3 , \u2014CH(CH 3 )CH 2 Y 3 , \u2014CH 2 CH(Y 3 )CH 3 , \u2014CH(Y 3 )CH 3 , \u2014CH 2 C(Y 3 )(CH 3 ) 2 , \u2014C(Y 3 )(CH 3 ) 2 , or where Y 3  is cyclopropyl, \u2014CF 3 , \u2014OCF 3 , \u2014OCH 3 , \u2014OCH 2 CH 3 , \u2014F, \u2014Cl, \u2014OH, \u2014O(CH 2 ) 2 \u2014OH, \u2014O(CH 2 ) 2 \u2014F, \u2014SCH 3 , \u2014S(O) 2 \u2014CH 3 , \u2014SCH 2 CH 3 , \u2014S(O) 2 CH 2 CH 3 , \u2014NH\u2014CH 3 , \u2014NH\u2014CH 2 CH 3 , \u2014N(CH 3 ) 2 , tetrahydropyran-4-yl, tetrahydrofuran-2-yl, morpholin-2-yl, morpholin-4-yl, piperidin-1-yl, 4-hydroxy-piperidin-1-yl, 3-hydroxy-piperidin-1-yl, \u2014NH\u2014C(O)\u2014CH 3 , \u2014NH\u2014C(O)\u2014CH 2 CH 3 , tetrahydrofuran-2-yl-methyloxy, or \u2014C(O)\u2014Y 4 , where Y 4  is \u2014OH, \u2014OCH 3 , \u2014OCH 2 CH 3 , \u2014OC(CH 3 ) 3 , \u2014NH 2 , \u2014NH\u2014CH 3 , \u2014NH\u2014CH 2 CH 3 , \u2014N(CH 3 ) 2 , \u2014N(CH 2 CH 3 ) 2 , morpholin-4-yl, 4-methyl-piperazin-1-yl, pyrrolidin-1-yl, or piperazin-1-yl;\n 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; \n 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 ; \n R 2  is R b ; \n 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 ; \n 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 BY; \n 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 ; \n R a  is\n a) -halogen, \n b) \u2014C 1-6  alkyl, \n c) 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 BY; \n \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 f 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 \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 \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 ; \n 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 ; \n 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 ; \n 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 \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 \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 \n v is an integer from 0 to 4, and \n w is an integer from 0 to 2.

Metadata:
- Claim Count in Document: 13.0
- Percentile: 98.0
- Lexical Diversity: 1.36364
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15584459', '16007532', '14215873', '13028406', '15718987']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.761328061005944
- 35 USC 102 Novelty (BERT): 0.6427203080857588
- Combined Prediction Score: 0.7494672857139255
- Mean Citation Score: 423.0322560000001
- Max Citation Score: 588.17633
- Similarity Product: 580.7574174341762

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