PATENT CLAIM ANALYSIS

Application Number: 16221274
Application Type: Utility
Filing Date: 2018-12
Publication Date: 2019-04
Patent Classification: ["514", "300000"]

Abstract:
The invention relates to compounds of formula (I): wherein Q, A 1 , A 2 , A 3 , A 5 , A 6 , A 7 , A 8 , R 4a , R 4b  and R 5  are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.

Claim (Index 1):
A compound of formula (I): or a stereoisomer, tautomer, solvate, prodrug or salt thereof, wherein:\n ring A is a monocycle or a fused bicycle; \n Q is N or C, wherein when Q is N, then the bond between A 1  and Q is not a double bond and the bond between Q and A 4  is not a double bond; \n A 1  is NR 1 , N, S, CR 1  or CHR 1 ; \n A 2  is NR 2 , N, O, S, CR 2  or CHR 2 ; \n A 3  is N or C; \n A 4  is N; \n provided that no more than two of (i)-(iii) apply: (i) A 1  is NR 1  or N, (ii) A 2  is NR 2  or N, and (iii) A 3  is N; \n each R 1  is independently selected from the group consisting of H, halogen, \u2014NR a R b , \u2014NHC(O)NR a R b , \u2014NHS(O) 2 \u2014C 1 -C 3  alkyl, C 1 -C 3  alkyl, C 3 -C 7  cycloalkyl, C 1 -C 3  alkoxy and 3-11 membered heterocyclyl, wherein the C 1 -C 3  alkyl of R 1  is optionally substituted by F, OH, CN, SH, C 1 -C 3  alkoxy or 3-11 membered heterocyclyl; the C 3 -C 7  cycloalkyl of R 1  is optionally substituted by F, OH, CN, SH, CH 3  or CF 3 ; the C 1 -C 3  alkoxy of R 1  is optionally substituted by F, OH, CN or SH; and the 3-11 membered heterocyclyl of R 1  is optionally substituted by F, OH, CN, SH, CF 3  or C 1 -C 3  alkyl; \n each R 2  is independently selected from the group consisting of H, NR a R b , C 1 -C 6  alkyl, C 3 -C 7  cycloalkyl, C 1 -C 6  alkoxy, phenyl and 3-11 membered heterocyclyl, wherein the C 1 -C 6  alkyl, C 3 -C 7  cycloalkyl, C 1 -C 6  alkoxy, phenyl and 3-11 membered heterocyclyl of R 2  is optionally substituted by R c ; or\n R 1  and R 2  are taken together with the atoms to which they are attached to form a cyclic group selected from the group consisting of C 3 -C 7  cycloalkyl, phenyl and 3-11 membered heterocyclyl, wherein the cyclic group is optionally substituted by R d ; \n \n each R 4a  and R 4b  is independently H or F; \n R 5  is C 1 -C 6  alkyl or C 3 -C 4  cycloalkyl, wherein the C 1 -C 6  alkyl and C 3 -C 4  cycloalkyl of R 5  are independently optionally substituted by halogen, OH, or C 1 -C 6  alkoxy; \n each A 5 , A 6 , A 7  and A 8  is independently N or CR 6 , provided that at least three of A 5 , A 6 , A 7  and A 8  are independently CR 6 ; \n each R 6  is independently selected from the group consisting of H, F, Cl, NH 2 , NHCH 3 , N(CH 3 ) 2 , OH, OCH 3 , OCHF 2 , OCH 2 F, OCF 3 , SH, SCH 3 , SCHF 2 , SCH 2 F, CN, CH 3 , CHF 2 , CH 2 F, CH 2 OH, CF 3 , NO 2  and N 3 ; \n R a  is selected from the group consisting of H and C 1 -C 6  alkyl optionally substituted by C 1 -C 3  alkoxy, F, OH, CN, SH, CH 3  or CF 3 ; \n R b  is selected from the group consisting of H, C 1 -C 6  alkyl, C 1 -C 6  alkoxy, C 3 -C 6  cycloalkyl, C(O)R g , phenyl and 3-11 membered heterocyclyl wherein R b  may be optionally substituted by C 1 -C 3  alkoxy, F, OH, CN, SH, CH 3  or CF 3 ; \n R c  and R d  are each independently selected from the group consisting of halogen, \u2014(X 1 ) 0-1 \u2014CN, \u2014(X 1 ) 0-1 \u2014NO 2 , \u2014(X 1 ) 0-1 \u2014SF 5 , \u2014(X 1 ) 0-1 \u2014OH, \u2014(X 1 ) 0-1 \u2014NH 2 , \u2014(X 1 ) 0-1 \u2014N(H)(R 1a ), \u2014(X 1 ) 0-1 \u2014N(R 1b )(R 1a ), \u2014(X 1 ) 0-1 \u2014CF 3 , C 1 -C 6  alkyl, C 1 -C 6  haloalkyl, C 1 -C 6  heteroalkyl, C 1 -C 6  alkoxy, C 1 -C 6  alkylthio, oxo, \u2014(X 1 ) 0-1 C 1 -C 6  alkyl, \u2014(X 1 ) 0-1 \u2014C 3 -C 10  cycloalkyl, \u2014O\u2014C 3 -C 10  cycloalkyl, \u2014(X 1 ) 0-1 -3-11 membered heterocyclyl, \u2014(X 1 ) 0-1 \u2014C 6 -C 10  aryl, \u2014C(\u2550O)(X 1 ) 0-1 \u2014C 3 -C 10  cycloalkyl, \u2014C(\u2550O)(X 1 ) 0-1 -3-11 membered heterocyclyl, \u2014(X 1 ) 0-1 \u2014C(\u2550Y 1 )N(H)(R 1a ), \u2014(X 1 ) 0-1 \u2014C(\u2550Y 1 )NH 2 , \u2014(X 1 ) 0-1 \u2014C(\u2550Y 1 )N(R 1a )(R 1b ), \u2014(X 1 ) 0-1 \u2014C(\u2550Y)OR 1a , \u2014(X 1 ) 0-1 \u2014C(\u2550Y)OH, \u2014(X 1 ) 0-1 \u2014N(H)C(\u2550Y 1 )(R 1a ), \u2014(X 1 ) 0-1 \u2014N(R 1b )C(\u2550Y 1 )(R 1a ), \u2014(X 1 ) 0-1 \u2014N(R 1b )C(\u2550Y 1 )(H), \u2014(X 1 ) 0-1 \u2014N(H)C(\u2550Y)OR 1a , \u2014(X 1 ) 0-1 \u2014N(R 1b )C(\u2550Y 1 )OR 1a , \u2014(X 1 ) 0-1 \u2014S(O) 1-2 R 1a , \u2014(X 1 ) 0-1 \u2014N(H)S(O) 1-2 R 1a , \u2014(X 1 ) 0-1 \u2014N(R 1b )S(O) 1-2 R 1a , \u2014(X 1 ) 0-1 \u2014S(O) 0-1 N(H)(R 1a ), \u2014(X 1 ) 0-1 \u2014S(O) 0-1 N(R 1b )(R 1a ), \u2014(X 1 ) 0-1 \u2014S(O) 0-1 NH 2 , \u2014(X 1 ) 0-1 \u2014S(\u2550O)(\u2550NR 1b )R 1a , \u2014(X 1 ) 0-1 \u2014C(\u2550Y 1 )R 1a , \u2014(X 1 ) 0-1 \u2014C(\u2550Y 1 )H, \u2014(X 1 ) 0-1 \u2014C(\u2550NOH)R 1a , \u2014(X 1 ) 0-1 \u2014C(\u2550NOR 1b )R 1a , \u2014(X 1 ) 0-1 \u2014NHC(\u2550Y 1 )N(H)(R 1a ), \u2014(X 1 ) 0-1 \u2014NHC(\u2550Y 1 )NH 2 , \u2014(X 1 ) 0-1 \u2014NHC(\u2550Y 1 )N(R 1b )(R 1a ), \u2014(X 1 ) 0-1 \u2014N(R 1a )C(\u2550Y 1 )N(H)(R 1a ), \u2014(X 1 ) 0-1 \u2014N(R 1a )C(\u2550Y 1 )N(R 1a )(R 1b ), \u2014(X 1 ) 0-1 \u2014N(R 1a )C(\u2550Y 1 )NH 2 , \u2014(X 1 ) 0-1 \u2014OC(\u2550Y 1 )R 1a , \u2014(X 1 ) 0-1 \u2014OC(\u2550Y 1 )H, \u2014(X 1 ) 0-1 \u2014OC(\u2550O)OR 1a , \u2014(X 1 ) 0-1 \u2014OP(\u2550Y 1 )(OR 1a )(OR 1b ), \u2014(X 1 )\u2014SC(\u2550Y 1 )OR 1a  and \u2014(X 1 )\u2014SC(\u2550Y 1 )N(R 1a )(R 1b ); wherein X 1  is selected from the group consisting of C 1 -C 6  alkylene, C 1 -C 6  heteroalkylene, C 2 -C 6  alkenylene, C 2 -C 6  alkynylene, C 1 -C 6  alkyleneoxy, C 3 -C 7  cycloalkylene, 3-11 membered heterocyclylene and phenylene; R 1a  and R 1b  are each independently selected from the group consisting of C 1 -C 6  alkyl, C 1 -C 6  haloalkyl, C 1 -C 6  heteroalkyl, C 3 -C 7  cycloalkyl, (C 3 -C 7  cycloalkylene)C 1 -C 6  alkyl, 3-11 membered heterocyclyl, (3-11 membered heterocyclylene)C 1 -C 6  alkyl, phenyl, and (C 6 -C 10  arylene)C 1 -C 6  alkyl, or R 1a  and R 1b , when attached to the same nitrogen atom, are taken together with the nitrogen to which they are attached to form a 3-11 membered heterocyclyl comprising 0-3 additional heteroatoms selected from N, O and S; Y 1  is O, NR 1c  or S wherein R 1c  is H or C 1 -C 6  alkyl; wherein any portion of an R c  or R d  substituent, including R 1a , R 1b  and R 1c , at each occurrence is independently further substituted by from 0 to 4 R f  substituents selected from the group consisting of halogen, CN, NO 2 , SF 5 , OH, NH 2 , \u2014N(C 1 -C 6  alkyl) 2 , \u2014NH(C 1 -C 6  alkyl), oxo, C 1 -C 6  alkyl, \u2014(C 2 -C 6  alkynylene)-(3-11 membered heterocyclyl, wherein the heterocyclyl is optionally substituted by R e ), C 1 -C 6  hydroxyalkyl, C 1 -C 6  heteroalkyl, C 1 -C 6  alkoxy, C 1 -C 6  alkylthio, C 3 -C 7  cycloalkyl, 3-11 membered heterocyclyl, \u2014C(\u2550O)N(H)(C 1 -C 6  alkyl), \u2014C(\u2550O)N(C 1 -C 6  alkyl) 2 , \u2014C(\u2550O)NH 2 , \u2014C(\u2550O)OC 1 -C 6  alkyl, \u2014C(\u2550O)OH, \u2014N(H)C(\u2550O)(C 1 -C 6  alkyl), \u2014N(C 1 -C 6  alkyl)C(\u2550O)(C 1 -C 6  alkyl), \u2014N(H)C(\u2550O)OC 1 -C 6  alkyl, \u2014N(C 1 -C 6  alkyl)C(\u2550O)OC 1 -C 6  (halo)alkyl, \u2014S(O) 1-2 C 1 -C 6  alkyl, \u2014N(H)S(O) 1-2 C 1 -C 6  alkyl, \u2014N(C 1 -C 6  alkyl)S(O) 1-2 C 1 -C 6  alkyl, \u2014S(O) 0-1 N(H)(C 1 -C 6  alkyl), \u2014S(O) 0-1 N(C 1 -C 6  alkyl) 2 , \u2014S(O) 0-1 NH 2 , \u2014C(\u2550O)C 1 -C 6  alkyl, \u2014C(\u2550O)C 3 -C 7  cycloalkyl, \u2014C(\u2550NOH)C 1 -C 6  alkyl, \u2014C(\u2550NOC 1 -C 6  alkyl)C 1 -C 6  alkyl, \u2014NHC(\u2550O)N(H)(C 1 -C 6  alkyl), \u2014NHC(\u2550O)N(C 1 -C 6  alkyl) 2 , \u2014NHC(\u2550O)NH 2 , \u2014N(C 1 -C 6  alkyl)C(\u2550O)N(H)(C 1 -C 6  alkyl), \u2014N(C 1 -C 6  alkyl)C(\u2550O)NH 2 , \u2014OC(\u2550O)C 1 -C 6  alkyl, \u2014OC(\u2550O)OC 1 -C 6  alkyl, \u2014OP(\u2550O)(OC 1 -C 6  alkyl) 2 , \u2014SC(\u2550O)OC 1 -C 6  alkyl and \u2014SC(\u2550O)N(C 1 -C 6  alkyl) 2 , wherein any alkyl portion of R f  is optionally substituted with halogen; \n R e  is selected from the group consisting of halogen, OH, C 1 -C 6  alkyl and oxo; and \n R g  is selected from the group consisting of C 1 -C 6  alkyl and C 3 -C 6  cycloalkyl wherein the C 1 -C 6  alkyl and C 3 -C 6  cycloalkyl of R g  may be optionally substituted by C 1 -C 3  alkoxy, F, OH, CN, SH, CH 3  or CF 3 .

Metadata:
- Claim Count in Document: 5.0
- Percentile: 98.0
- Lexical Diversity: 1.59184
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['16220963', '15314938', '15026250', '14378975', '15904143']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7314854715720951
- 35 USC 102 Novelty (BERT): 0.5748416023037715
- Combined Prediction Score: 0.7158210846452627
- Mean Citation Score: 329.27391
- Max Citation Score: 485.14618
- Similarity Product: 357.32818886910314

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

Dataset: test