PATENT CLAIM ANALYSIS

Application Number: 16438135
Application Type: Utility
Filing Date: 2019-06
Publication Date: 2019-10
Patent Classification: ["544", "281000"]

Abstract:
Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein.

Claim (Index 1):
A compound of Formula (00A): and stereoisomers and salts thereof, wherein: R 00  is H or CH 3 ; R 01  is H or NH 2 ; R 0  is H or NH 2 ; and Ring Q is either (i) or (ii):\n (i) \n (ii) wherein: t 1  and t 2  are each independently 0 or 1; X A  and X B  are independently selected from the group consisting of H, C 1 -C 6  alkyl, C 2 -C 4  alkenyl, \u2014NR a R b , C 2 -C 5  alkynyl, 3-6-membered cycloalkyl, 6-10 membered aryl, 3-11 membered heterocycloalkyl, 5-6 membered heterocycloalkenyl, and 5-10 membered heteroaryl; wherein when either of X A  and X B  are independently C 1 -C 6  alkyl, C 2 -C 4  alkenyl, C 2 -C 5  alkynyl, 3-6-membered cycloalkyl, 6-10 membered aryl, 3-11 membered heterocycloalkyl, 5-6 membered heterocycloalkenyl, and 5-10 membered heteroaryl, each of X A  and X B  is independently optionally substituted by Y 1 , wherein Y 1  is selected from:\n (a) C 1 -C 6  alkyl optionally substituted by T 1 , wherein T 1  is selected from the group consisting of OH, halo, CN, imino, 3-6 membered cycloalkyl, 3-11 membered heterocycloalkyl, 3-11 membered heterocycloalkenyl, 5-10 membered heteroaryl, \u2014O\u2014(C 1 -C 6  alkyl), C(O)OH, oxetan-3-ylmethyl, \u2014C(O)O\u2014(C 1 -C 6  alkyl), \u2014S\u2014(C 1 -C 6  alkyl), \u2014SO 2 \u2014(C 1 -C 6  alkyl), \u2014NR a R b , \u2014N(+)R a R b R c  wherein R c  is methyl, \u2014C(O)NR a R b , -(2-oxoindolin-1-yl), \u2014OC(O)-3-6 membered cycloalkyl, and phenyl, wherein each alkyl, cycloalkyl, heterocycloalkyl, heterocycloalkenyl, heteroaryl, and phenyl of Ti is optionally substituted by OH, \u2014C(O)O\u2014(C 1 -C 6  alkyl), C 1 -C 6  alkyl, halo, CN, oxo, \u2014(C 1 -C 6  alkyl)CONR a R b , \u2014NR a R b , phenyl, or \u2014O\u2014(C 1 -C 6  alkyl) optionally substituted by OH; \n (b) 3-11 membered heterocycloalkyl, \u2014(C 1 -C 6  alkylene)-3-11 membered heterocycloalkyl, \u2014C(O)-3-11 membered heterocycloalkyl, \u2014(C 1 -C 6  alkylene)C(O)-3-11 membered heterocycloalkyl, or \u2014OC(O)-4-6 membered heterocycloalkyl; wherein the heterocycloalkyl is optionally substituted by OH, halo, CN, C 1 -C 6  alkyl, \u2014(C 1 -C 6  alkylene)-CF 3 , oxo, \u2014C(O)\u2014(C 1 -C 6  alkyl), \u2014C(O)O\u2014(C 1 -C 6  alkyl), \u2014C(O)O\u2014(C 1 -C 6  alkylene)-phenyl, \u2014SO 2 \u2014(C 1 -C 6  alkyl), \u2014C(O)NR a R b , \u2014NR a R b , \u2014(C 1 -C 6  alkylene)-phenyl, or \u2014C(O)-4-6 membered heterocycloalkyl optionally substituted by \u2014NR a R b ; \n (c) N(+)(AA) 3 , wherein each AA is independently C 1 -C 6  alkyl optionally substituted by phenyl; \n (d) 3-6 membered cycloalkyl optionally substituted by OH, halo, NR a R b , or CN; \n (e) CN, halo, or oxo; \n (f) \u2014C(O)\u2014(C 1 -C 6  alkyl), \u2014C(O)OH, \u2014C(O)O\u2014(C 1 -C 6  alkylene)-phenyl, \u2014SO 2 \u2014(C 1 -C 6  alkyl), \u2014C(O)NR a R b , or \u2014C(O)-4-6 membered heterocycloalkyl optionally substituted by \u2014(C 1 -C 6  alkyl) or \u2014NR a R b , or \u2014C(O)O\u2014(C 1 -C 6  alkyl) optionally substituted by OH, NR a R b , or 3-11 membered heterocycloalkyl wherein said heterocycloalkyl is optionally substituted by C 1 -C 6  alkyl; \n (g) OH, \u2014O-phenyl, or \u2014O\u2014(C 1 -C 6  alkyl), wherein the alkyl is optionally substituted by OH or \u2014NR a R b ; \n (h) phenyl optionally substituted by OH, halo, C 1 -C 6  alkyl, CF 3 , or CN; \n (i) 5-6 membered heteroaryl optionally substituted by OH, halo, C 1 -C 6  alkyl, CF 3 , CN, or 3-11 membered heterocycloalkyl optionally substituted by C 1 -C 6  alkyl or 3-11 membered heterocycloalkyl; \n (j) isoindolin-2-yl optionally substituted by halo; \n (k) \u2014NR a R b , and \n (l) \u2014O\u2014CH 2 C(O)-3-11 membered heterocycloalkyl; \n wherein R a  and R b  are independently selected from: \n (a) H, \n (b) C 1 -C 6  alkyl optionally substituted by OH, halo, CN, \u2014C(O)OH, \u2014C(O)O\u2014(C 1 -C 6 alkyl), \u2014C(O)O-(3-11 membered heterocycloalkyl), \u2014C(O)O\u2014(C 1 -C 6  alkyl)-S\u2014(C 1 -C 6  alkyl), \u2014S\u2014(C 1 -C 6  alkyl), naphthylenyl, \u2014NR az R bz , \u2014C(O)NR az R bz , oxo, \u2014O\u2014(C 1 -C 6  alkyl), 5-6 membered heteroaryl optionally substituted by C 1 -C 6  alkyl or halo, or benzo[1,3]dioxol-2-yl, or 3-11 membered heterocycloalkenyl optionally substituted by oxo; \n (c) \u2014(C 1 -C 6  alkylene)-3-6 membered cycloalkyl wherein the alkylene is optionally substituted by OH, halo, or CN; \n (d) \u2014(C 1 -C 6  alkylene)-phenyl wherein alkylene is optionally substituted by halo and the phenyl is optionally substituted by OH, halo, CF 3 , C 1 -C 6  alkyl, \u2014O\u2014(C 1 -C 6  alkyl), \u2014S\u2014(C 1 -C 6  alkyl, or \u2014O-phenyl; \n (e) \u2014(C 1 -C 6  alkylene)-4-6 membered heterocycloalkyl wherein the heterocycloalkyl is optionally substituted by halo, oxo, or C 1 -C 6  alkyl; \n (f) \u2014(C 1 -C 6  alkylene)-O-phenyl wherein the phenyl is optionally substituted by halo, C 1 -C 6  alkyl, or \u2014O-phenyl; \n (g) \u2014(C 1 -C 6  alkyl) 3-6  membered cycloalkyl optionally substituted by OH, halo, CN, or C 1 -C 6  alkyl optionally substituted by OH or CN; \n (h) C 2 -C 5  alkenyl; \n (i) 4-6 membered heterocycloalkyl optionally substituted by halo, \n (j) \u2014(C 1 -C 6  alkylene)-3-6 membered cycloalkyl substituted by hydroxymethyl, \n (k) phenyl, \n (l) \u2014C(O)(C 1 -C 6  alkyl), \n (m) \u2014C(O)O(C 1 -C 6  alkyl), \n (n) \u2014C(O)O(3-6 membered cycloalkyl), and \n (o) \u2014C(O)-phenyl, \n wherein R az  and R bz  are each independently selected from\n (a) H, \n (b) C 1 -C 6  alkyl optionally substituted by OH, halo, CN, \u2014C(O)OH, \u2014C(O)O\u2014(C 1 -C 6 alkyl), \u2014C(O)O-(3-11 membered heterocycloalkyl), \u2014C(O)O\u2014(C 1 -C 6  alkyl)-S\u2014(C 1 -C 6  alkyl), \u2014S\u2014(C 1 -C 6  alkyl), naphthylenyl, -oxo, \u2014O\u2014(C 1 -C 6  alkyl), 5-6 membered heteroaryl optionally substituted by C 1 -C 6  alkyl or halo, or benzo[1,3]dioxol-2-yl, or 3-11 membered heterocycloalkenyl optionally substituted by oxo; \n (c) \u2014(C 1 -C 6  alkylene)-3-6 membered cycloalkyl wherein the alkylene is optionally substituted by OH, halo, or CN; \n (d) \u2014(C 1 -C 6  alkylene)-phenyl wherein alkylene is optionally substituted by halo and the phenyl is optionally substituted by OH, halo, CF 3 , C 1 -C 6  alkyl, \u2014O\u2014(C 1 -C 6  alkyl), \u2014S\u2014(C 1 -C 6  alkyl, or \u2014O-phenyl; \n (e) \u2014(C 1 -C 6  alkylene)-4-6 membered heterocycloalkyl wherein the heterocycloalkyl is optionally substituted by halo, oxo, or C 1 -C 6  alkyl; \n (f) \u2014(C 1 -C 6  alkylene)-O-phenyl wherein the phenyl is optionally substituted by halo, C 1 -C 6  alkyl, or \u2014O-phenyl; \n (g) \u2014(C 1 -C 6  alkyl) 3-6  membered cycloalkyl optionally substituted by OH, halo, CN, or C 1 -C 6  alkyl optionally substituted by OH or CN; \n (h) C 2 -C 5  alkenyl; \n (i) 4-6 membered heterocycloalkyl optionally substituted by halo, \n (j) \u2014(C 1 -C 6  alkylene)-3-6 membered cycloalkyl substituted by hydroxymethyl, \n (k) phenyl, \n (l) \u2014C(O)(C 1 -C 6  alkyl), \n (m) \u2014C(O)O(C 1 -C 6  alkyl), \n (n) \u2014C(O)O(3-6 membered cycloalkyl), and \n (o) \u2014C(O)-phenyl, \n with the following provisos: when R 0 , R 00 , and R 01  are each H and Ring Q is where t 1  is 0, then X A  is not methyl, 2-methylpropan-2-ol, or tetrahydropyranyl.

Metadata:
- Claim Count in Document: 50.0
- Percentile: 100.0
- Lexical Diversity: 1.05882
- Patent Class: 544.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15139164', '15543826', '14904801', '14451600', '15257926']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8112229196251415
- 35 USC 102 Novelty (BERT): 0.5778269047311398
- Combined Prediction Score: 0.7878833181357414
- Mean Citation Score: 405.063252
- Max Citation Score: 495.0762
- Similarity Product: 396.8783903073549

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

Dataset: test