PATENT CLAIM ANALYSIS

Application Number: 15969907
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-08
Patent Classification: ["514", "256000"]

Abstract:
The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.

Claim (Index 1):
A compound of formula I in which X denotes CH, R 1  denotes NH 2 , CONH 2  or H, R 2  denotes Hal, Ar 1  or Het 1 , R 3  denotes NR 5 [C(R 5 ) 2 ] n Het 2 , NR 5 [C(R 5 ) 2 ] n Cyc, Het 2 , O[C(R 5 ) 2 ] n Ar 2 , NR 5 [C(R 5 ) 2 ] n Ar 2 , O[C(R 5 ) 2 ] n Het 2 , NR 5 (CH 2 ) p NR 5 R 6 , O(CH 2 ) p NR 5 R 6  or NR 5 (CH 2 ) p CR 7 R 8 NR 5 R 6 , R 4  denotes H, CH 3  or NH 2 , R 5  denotes H or alkyl having 1, 2, 3 or 4 C atoms, R 6  N(R 5 ) 2 CH 2 CH\u2550CHCONH, Het 3 CH 2 CH\u2550CHCONH, CH 2 \u2550CHCONH(CH 2 ) n , Het 4 (CH 2 ) n COHet 3 -diyl-CH 2 CH\u2550CHCONH, HC\u2261CCO, CH 3 C\u2261CCO, CH 2 \u2550CH\u2014CO, CH 2 \u2550C(CH 3 )CONH, CH 3 CH\u2550CHCONH(CH 2 ) n , N\u2014CCR 7 R 8 CONH(CH 2 ) n , Het 4 NH(CH 2 ) p COHet 3 -diyl-CH 2 CH\u2550CHCONH, Het 4 (CH 2 ) p CONH(CH 2 CH 2 O) p (CH 2 ) p COHet 3 -diyl-CH 2 CH\u2550CHCONH, CH 2 \u2550CHSO 2 , ACH\u2550CHCO, CH 3 CH\u2550CHCO, Het 4 (CH 2 ) p CONH(CH 2 ) p Het 3 -diyl-CH 2 CH\u2550CHCONH, Ar 3 CH\u2550CHSO 2 , CH 2 \u2550CHSO 2 NH or N(R 5 )CH 2 CH\u2550CHCO, R 7 , R 8  denote together alkylene having 2, 3, 4, or 5 C atoms, Ar 1  denotes phenyl or naphthyl, each of which is unsubstituted or mono-, di- or trisubstituted by R 6 , Hal, (CH 2 ) n NH 2 , CONHAr 3 , (CH 2 ) n NHCOA, O(CH 2 ) n Ar 3 , OCyc, A, COHet 3 , OA and/or OHet 3  (CH 2 ), Ar 2  denotes phenyl, naphthyl or pyridyl each of which is unsubstituted or mono-, di- or trisubstituted by R 6 , Hal, OAr 3 , (CH 2 ) n NH 2 , (CH 2 ) n NHCOA and/or Het 3 , Ar 3  denotes phenyl, which is unsubstituted or mono-, di- or trisubstituted by OH, OA, Hal, CN and/or A, Het 1  denotes a mono- or bicyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono-, di- or trisubstituted by R 6 , O(CH 2 ) n Ar 3  and/or (CH 2 ) n Ar 3 , Het 2  each independently denotes a mono- or bicyclic saturated heterocycle having 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono-, di- or trisubstituted by R 6 , Het 3 , CycSO 2 , OH, Hal, COOH, OA, COA, COHet 3 , CycCO, SO 2  and/or \u2550O, Het 3  each independently denotes a monocyclic unsaturated, saturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono-, di- or trisubstituted by Hal, A and/or \u2550O, Het 4  each independently denotes a bi- or tricyclic unsaturated, saturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono-, di-, tri- or tetrasubstituted by A, NO 2 , Hal and/or \u2550O, Cyc each independently denotes cyclic alkyl having 3, 4, 5 or 6 C atoms, which is unsubstituted, monosubstituted or disubstituted by R 6  and/or OH and which may comprise a double bond, A each independently denotes unbranched or branched alkyl having 1-10 C atoms, in which 1-7H atoms may be replaced by F and/or Cl and/or in which one or two non-adjacent CH 2  and/or CH-groups may be replaced by O, NH and/or by N, Hal each independently denotes F, Cl, Br or I, n each independently denotes 0, 1, 2, 3 or 4, p each independently denotes 1, 2, 3, 4, 5 or 6, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.

Metadata:
- Claim Count in Document: 15.0
- Percentile: 93.0
- Lexical Diversity: 1.75
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['14112428', '15417953', '14727050', '14772430', '12668864']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8250404609887269
- 35 USC 102 Novelty (BERT): 0.7279527561259768
- Combined Prediction Score: 0.8153316905024519
- Mean Citation Score: 623.8532299999998
- Max Citation Score: 879.4858
- Similarity Product: 768.7336635137798

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