PATENT CLAIM ANALYSIS

Application Number: 16068559
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2019-01
Patent Classification: ["544", "331000"]

Abstract:
The present invention provides compounds of Formula (I) or a subgeneric structure or species thereof or a pharmaceutically acceptable salt, ester, solvate, and/or prodrug thereof and methods and compositions for treating or ameliorating abnormal cell proliferative disorders, such as cancer, wherein A, R 2 , R 3 , R 10 , E 1 , E 2 , E 3 , Y, and Z are as defined herein.

Claim (Index 2):
The compound of  claim 1 , wherein the compound has the structure of formula (IB) or a stereoisomer or a pharmaceutically acceptable salt, solvate, ester, tautomer, or prodrug thereof; wherein,\n A is \n each of X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , and X 8  is independently CR 4  or N; wherein not more than two of X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , and X 8  are N; each of X 10  and X 12  is independently S, N, or CR 4 ; wherein at least one of X 10  and X 12  is S;\n Z is CH or N; \n Y is \n R 1  is independently selected from hydrogen, fluoro, chloro, bromo, methyl, ethyl, hydroxyl, methoxy, ethoxy, isopropoxy, cyclopropoxy, \u2014OCF 3 , \u2014OCH 2 CF 3 , \u2014OCH 2 CHF 2 , ethenyl, ethynyl, \u2014CF 3 , \u2014CHF 2 , \u2014CHO, \u2014CH 2 OH, \u2014CONH 2 , \u2014CO 2 Me, \u2014CONHMe, \u2014CONMe 2 , and cyano; R 2  is \u2014OCF 3 , \u2014OCHF 2 , \u2014OCF 2 CF 3 , \u2014OCH 2 CHF 2 , \u2014OCH 2 CF 3 , cyclopropyl, cyclopropoxy, methoxy, \u2014OCD 3 , ethoxy, or isopropoxy; R 3  is \u2014N(R 10 )C 2-6  alkyl-NR 10 R 10 , \u2014N(R 10 )C 2-6  alkyl-R 7 , \u2014O(CH 2 ) p R 7 , \u2014N(R 10 )C(\u2550O)(CH 2 ) p R 7 , or R 7 ; each R 4  is independently H, cyano, nitro, halo, \u2014C 1-6  alkyl, \u2014C 1-6  haloalkyl, -carboxy-C 1-6  alkyl, \u2014C 1-6  hydroxyalkyl, R 8 R 9 N\u2014C 1-6  alkyl-, \u2014C 2-6  alkenyl, \u2014C 2-6  alkynyl, C 1-6  acyl-, R 7 \u2014(CH 2 ) p C(\u2550O)\u2014, C 1-6  hydroxyalkyl-C(\u2550O)\u2014, carboxy, \u2014C 1-6  alkoxycarbonyl, \u2014C(\u2550O)NR 8 R 9 , hydroxyl, \u2014C 1-6  alkoxy, \u2014C 1-6  acyloxy, \u2014NR 8 R 9 , C 1-6  acyl-N(R 10 )\u2014, pyrazole, 123-triazole, tetrazole, (C 1-6  alkyl)SO 2 \u2014, or R 7 SO 2 \u2014; R 4N  is H, \u2014CD 3 , \u2014C 1-6  alkyl, \u2014C 1-6  haloalkyl, or \u2014CH 2 C(\u2550O)NR 8 R 9 ; in Y 1  and Y 2 , R 5a  is H, F, Cl, CF 3 , CHF 2 , CF 2 C 1-6  alkyl, CF 2 CH 2 NR 8 R 9 , CH 2 NR 8 R 9 , CN, or C 1-6  alkyl; in Y 1  and Y 2 , R 6e  is R 10 , H, F, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, (CH 2 ) m CHR 10 R 10 , CF 2 (CH 2 ) m CHR 10 R 7 , or C(R 10 ) 2 R 7 ; in Y 4  and Y 5 , R 6t  is C 1-6  alkyl, C 3-6  cycloalkyl, aryl, heteroaryl, heterocycloalkyl, (CH 2 ) m CHR 10 R 7 , C(R 10 ) 2 R 7 ; in Y 1  and Y 2 , R 6z  is H, F, Cl, CF 3 , CHF 2 , CF 2 C 1-6  alkyl or C 1-6  alkyl; or alternatively in Y 1  and Y 2 , R 6e  and R 6z , taken together, form \u2550CR 6e\u2032 R 6z\u2032  (allene), wherein R 6e\u2032  is R 10 , H, F, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, (CH 2 ) m CHR 10 R 7 , CF 2 (CH 2 ) m CHR 10 R 7 , or C(R 10 ) 2 R 7  and wherein, R 6z\u2032  is H, F, Cl, CF 3 , CHF 2 , CF 2 C 1-6  alkyl or C 1-6  alkyl; or alternatively in Y 1  and Y 2 , R 6e  and R 6z , taken together with the sp 2  carbon atom to which both are attached, form an alicyclic ring of 4 to 7 members wherein one of the ring atoms are optionally replaced by NR 8 , O, S(O) x , S(\u2550O)(\u2550NR 8 ), P\u2550O, P(\u2550O)(OR 8 ), OP(\u2550O)(OR 8 )O, and the alicyclic ring is optionally substituted with one or more substituents selected from the group consisting of halogen, oxo, OH, OR 8 , and NR 8 R 9 ; R 7  is OH, NR 8 R 9 , O(CH 2 ) q NR 8 R 9 , C 1-6  alkoxy, C 1-6  alkoxy-C 1-6  alkoxy, C 2-6  hydroxyalkoxy, oxetanyl, oxetanyloxy, oxetanylamino, oxolanyl, oxolanyloxy, oxolanylamino, oxanyl oxanyloxy, oxanylamino, oxepanyl, oxepanyloxy, oxepanylamino, azetidinyl, azetidinyloxy, azetidylamino, pyrrolidinyl, pyrolidinyloxy, pyrrolidinylamino, piperidinyl, piperidinyloxy, piperidinylamino, azepanyl, azepanyloxy, azepanylamino, dioxolanyl, dioxanyl, morpholino, thiomorpholino, thiomorpholino-S,S-dioxide, piperazino, dioxepanyl, dioxepanyloxy, dioxepanylamino, oxazepanyl, oxazepanyloxy, oxazepanylamino, diazepanyl, diazepanyloxy, diazepanylamino, (3R)-3-(dimethylamino)pyrrolidin-1-yl, (3S)-3-(dimethylamino)pyrrolidin-1-yl, 3-(dimethylamino)azetidin-1-yl, [2-(dimethylamino)ethyl](methyl)amino, [2-(methylamino)ethyl](methyl)amino, 5-methyl-2,5diazaspiro[3.4]oct-2-yl, (3aR,6aR)-5-methylhexa-hydro-pyrrolo[3,4-b]pyrrol-1(2H)-yl, 1-methyl-1,2,3,6-tetrahydropyridin-4-yl, 4-methylpiperizin-1-yl, 4-[2(dimethylamino)-2-oxoethyl]piperazin-1-yl, methyl[2-(4-methylpiperazin-1yl)ethyl]amino, methyl[2-(morpholin-4-yl)ethyl]amino, 1-amino-1,2,3,6tetrahydropyridin-4-yl, 4-[(2S)-2-aminopropanoyl]piperazin-1-yl, all of which may be optionally substituted with OH, OR 10 , oxo, halogen, R 10 , CH 2 OR 10 , or CH 2 NR 8 R 9 ; R 8  and R 9  are each independently H, \u2014CD 3 , C 1-6  alkyl, C 3-6  alkenyl, C 3-6  alkynyl, C 3-8  cycloalkyl, \u2014(C 1-3  alkyl)-(C 3-8  cycloalkyl), C 3-8  cycloalkenyl, C 1 -C 6  acyl, 4-12 membered monocyclic or bicyclic heterocyclyl, 4-12 membered monocyclic or bicyclic heterocyclyl-C 1 -C 6  alkyl-, C 6 -C 12  aryl, 5-12 membered heteroaryl: wherein R 8  and R 9  may be further independently substituted with up to three substituents chosen from hydroxyl, C 1-6  alkoxy, C 1-6  hydroxyalkyl, C 1-6  alkoxy-C 1-6  alkyl, C 1-6  alkoxy-C 1-6  alkoxy, C 2-6  hydroxyalkoxy, oxo, thiono, cyano or halo; or alternatively, R 8  and R 9 , taken together with the N atom to which they are both attached, form a heterocyclic ring of 4-7 members, containing up to one other heteroatom selected from O, S, or NR 11 , or a heterobicyclic ring of 7-12 members which may be fused, bridged or spiro, and contain up to two other heteroatoms chosen from O, S(O), or NR 11 , and these heterocyclic rings are optionally substituted with up to three substituents chosen from hydroxyl, C 1-6  alkoxy, C 1-6  hydroxyalkyl, C 1-6  alkoxy-C 1-6  alkyl, C 1-6  alkoxy-C 1-6  alkoxy, C 2-6  hydroxyalkoxy, oxo, thiono, cyano or halo; each R 10  is independently H, \u2014CD 3 , C 1-6  alkyl, C 3-6  cycloalkyl, C 2-6  hydroxyalkyl, C 1-6 alkoxy-C 1-6  alkyl or C 2-6  alkyl-NR 8 R 9 ; alternatively, two R 10  on the same N atom to which they are both attached, form a heterocyclic ring of 5-6 members, containing up to one other heteroatom selected from O, S, or NR 11 ; each R 11  is independently hydrogen or C 1 -C 6  alkyl, which is optionally substituted with up to three substituents selected from hydroxyl, oxo, thiono, cyano or halo; m is 0, 1, 2, or 3; p=0, 1, 2, 3, or 4, q=2, 3, or 4; and x=0, 1, or 2.

Metadata:
- Claim Count in Document: 70.0
- Percentile: 95.0
- Lexical Diversity: 1.5098
- Patent Class: 544.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['13229178', '12008840', '12842389', '11282119', '12310150']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8309601149714478
- 35 USC 102 Novelty (BERT): 0.5127027730789013
- Combined Prediction Score: 0.7991343807821932
- Mean Citation Score: 314.529296
- Max Citation Score: 321.7707200000001
- Similarity Product: 253.7619582342149

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