PATENT CLAIM ANALYSIS

Application Number: 16044862
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2018-11
Patent Classification: ["514", "183000"]

Abstract:
Described herein are tricyclic compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.

Claim (Index 1):
A method of treating cancer in a patient having a cancer selected from the group consisting of breast cancer, lung cancer, ovarian cancer, endometrial cancer, prostate cancer, and uterine cancer, comprising administering to said patient a therapeutically effective amount of a compound selected from Formula I: or stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, wherein: the dotted/solid lines represent a single or double bond; X a  is CR a , N, NR b , O, or S; X b  is C or N; X c  is C or N; X d  is CR 2  or N; where at least one of X a , X b , and X c  is N, O, or S; R a  is selected from H, C 1 -C 6  alkyl, \u2014CN and F; R b  is selected from H and C 1 -C 6  alkyl; R 1  is selected from Br, Cl, I, C 2 -C 20  heterocyclyl, C 1 -C 20  heteroaryl, \u2014NR 3 R 4 , and \u2014OR 5 ; R 2  is selected from H, F, Cl, C 1 -C 6  alkyl, and \u2014O(C 1 -C 6  alkyl); R 3  is selected from H, and C 1 -C 6  alkyl; R 4  is selected from H, C 1 -C 6  alkyl, C 2 -C 20  heterocyclyl, and C 1 -C 20  heteroaryl; or R 3  and R 4  form a 4-membered, 5-membered or 6-membered heterocyclyl ring; R 5  is selected from C 1 -C 6  alkyl, C 2 -C 20  heterocyclyl, and C 1 -C 20  heteroaryl; R 6  is independently selected from H, C 1 -C 4  alkyl, and F; or two geminal or vicinal R 6  groups can form a 3, 4, or 5 membered-carbocyclic ring; p is 2, 3, or 4; A is selected from C 6 -C 20  aryl, \u2014(C 6 -C 20  aryl)-(C 6 -C 20  aryl), \u2014(C 6 -C 20  aryl)-(C 1 -C 20  heteroaryl), \u2014(C 6 -C 20  aryl)-(C 2 -C 20  heterocyclyl), \u2014(C 1 -C 20  heteroaryl)-(C 2 -C 20  heterocyclyl), \u2014(C 1 -C 20  heteroaryl)-(C 1 -C 20  heteroaryl), C 2 -C 20  heterocyclyl, and C 1 -C 20  heteroaryl; and where alkyl, aryl, heterocyclyl and heteroaryl are optionally substituted with one or more groups independently selected from F, Cl, Br, I, \u2014CN, \u2014CH 3 , \u2014CH 2 CH 3 , \u2014CH(CH 3 ) 2 , C(CH 3 ) 3 , \u2014CH 2 CH(CH 3 ) 2 , \u2014CH 2 OH, \u2014CH 2 OCH 3 , \u2014CH 2 CH 2 OH, \u2014C(CH 3 ) 2 OH, \u2014CH(OH)CH(CH 3 ) 2 , \u2014C(CH 3 ) 2 CH 2 OH, \u2014CH 2 CH 2 SO 2 CH 3 , \u2014CH 2 OP(O)(OH) 2 , \u2014CH 2 F, \u2014CHF 2 , \u2014CH 2 NH 2 , \u2014CH 2 NHSO 2 CH 3 , \u2014CH 2 NHCH 3 , \u2014CH 2 N(CH 3 ) 2 , \u2014CF 3 , \u2014CH 2 CF 3 , \u2014CH 2 CHF 2 , \u2014CH(CH 3 )CN, \u2014C(CH 3 ) 2 CN, \u2014CH 2 CN, \u2014CO 2 H, \u2014COCH 3 , \u2014CO 2 CH 3 , \u2014CO 2 C(CH 3 ) 3 , \u2014COCH(OH)CH 3 , \u2014CONH 2 , \u2014CONHCH 3 , \u2014CONHCH 2 CH 3 , \u2014CONHCH(CH 3 ) 2 , \u2014CON(CH 3 ) 2 , \u2014C(CH 3 ) 2 CONH 2 , \u2014NH 2 , \u2014NHCH 3 , \u2014N(CH 3 ) 2 , \u2014NHCOCH 3 , \u2014N(CH 3 )COCH 3 , \u2014NHS(O) 2 CH 3 , \u2014N(CH 3 )C(CH 3 ) 2 CONH 2 , \u2014N(CH 3 )CH 2 CH 2 S(O) 2 CH 3 , \u2014NO 2 , \u2550O, \u2014OH, \u2014OCH 3 , \u2014OCH 2 CH 3 , \u2014OCH 2 CH 2 OCH 3 , \u2014OCH 2 CH 2 OH, \u2014OCH 2 CH 2 N(CH 3 ) 2 , \u2014OP(O)(OH) 2 , \u2014S(O) 2 N(CH 3 ) 2 , \u2014SCH 3 , \u2014S(O) 2 CH 3 , \u2014S(O) 3 H, cyclopropyl, cyclobutyl, azetidinyl, oxetanyl, cyclopentyl, tetrahydrofuranyl, morpholinyl, piperidyl, piperazinyl, and tetrahydropyranyl.

Metadata:
- Claim Count in Document: 63.0
- Percentile: 95.0
- Lexical Diversity: 1.45902
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15258175', '14930929', '12890812', '13477587', '13424500']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7991869201867696
- 35 USC 102 Novelty (BERT): 0.6283501750721406
- Combined Prediction Score: 0.7821032456753068
- Mean Citation Score: 505.825478
- Max Citation Score: 671.0267
- Similarity Product: 503.1240384754777

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