PATENT CLAIM ANALYSIS

Application Number: 16444032
Application Type: Utility
Filing Date: 2019-06
Publication Date: 2019-10
Patent Classification: ["514", "210180"]

Abstract:
The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula (I): wherein X, Y, Z, R 1 , R 2 , R 4  and R 7  are defined herein.

Claim (Index 35):
A process of preparing a compound of Formula (VI): or a pharmaceutically acceptable salt thereof, wherein: R 10  is independently selected from the group consisting of C 1 -C 6  alkyl, C 1 -C 6  alkoxy, C 1 -C 6  hydroxyalkyl, C 1 -C 6  haloalkyl, C 1 -C 6  haloalkoxy, \u2014OR i , \u2014NR a R i , \u2014CN, \u2014(CR k R l ) n S(O) 2 R i , \u2014(CR k R l ) n NR a S(O) 2 R i , \u2014(CR k R l ) n S(O) 2 NR a R i , \u2014(CR k R l ) n C(O)OR a , \u2014(CR k R l ) n C(O)R i , \u2014(CR k R l ) n C(O)NR a R i , \u2014(CR k R l ) n R i , \u2014(CR k R l ) n NR a C(O)NR b , and \u2014(CR k R l ) n NR a C(O)OR b , wherein each alkyl is substituted with one or more R 11 ; each R 11  is independently selected from halogen, C 1 -C 6  alkyl, C 1 -C 6  alkoxy, C 1 -C 6  haloalkyl, hydroxy, \u2014CN, C 1 -C 6  hydroxyalkyl, \u2014(CR k R l ) m NH 2 , C 1 -C 6  alkylamino, C 1 -C 6  dialkylamino, \u2014C(O)NR a R b , \u2014C(O)OR a , \u2014C(O)R a , \u2014S(O) 2 R a , \u2014C(O)H, \u2014NR a C(O)OR a , \u2014NR a C(O)C 1 -C 6  alkyl, and oxo; or\n two R 11  together can form a heterocycloalkyl ring; \n R a  and R b  are each independently hydrogen, C 1 -C 6  alkyl, C 1 -C 4  alkyl(aryl), or aryl; R d  is C 1 -C 6  alkyl, C 1 -C 6  haloalkyl, C 3 -C 7  cycloalkyl, aryl, heteroaryl, or heterocycloalkyl, wherein cycloalkyl, aryl, heteroaryl, and heterocycloalkyl are optionally substituted with one or more R 12 ; R i  is hydrogen, C 1 -C 6  alkyl, C 1 -C 6  alkoxy, C 1 -C 6  hydroxyalkyl, C 1 -C 6  haloalkyl, \u2014(CH 2 ) q N(H)C 1 -C 6  alkyl, \u2014(CH 2 ) q N(C 1 -C 6  alkyl) 2 , \u2014(CR k R l ) m C3-C 7  cycloalkyl, \u2014(CR k R l ) m aryl, \u2014(CR k R l ) m heteroaryl, or \u2014(CR k R l ) m heterocycloalkyl, wherein alkyl, cycloalkyl, aryl, heteroaryl, and heterocycloalkyl are optionally substituted with one or more R 11 ; each R 12  is independently selected from C 1 -C 6  alkyl, halogen, \u2014CN, C 1 -C 6  alkoxy, C 1 -C 6  haloalkyl, C 1 -C 6  haloalkoxy, hydroxy, \u2014NO 2 , \u2014NH 2 , \u2014CH 2 NH 2 , \u2014(CH 2 ) q N(C 1 -C 6  alkyl) 2 , C 1 -C 6  alkylamino, C 1 -C 6  dialkylamino, \u2014O(CH 2 ) q N(H)C 1 -C 6  alkyl, \u2014O(CH 2 ) q N(C 1 -C 6  alkyl) 2 , aryl, heteroaryl, \u2014NH-heteroaryl, \u2014O-aryl, \u2014S(O) p \u2014C 1 -C 6  alkyl, \u2014S(O),\u2014N(H)C 1 -C 6  alkyl, \u2014S(O),\u2014N(C 1 -C 6  alkyl) 2 , \u2014C(O)C 1 -C 6  alkyl, \u2014C(O)OC 1 -C 6  alkyl, \u2014NHC(O)(C 1 -C 6  alkyl), and oxo, wherein aryl and heteroaryl are optionally substituted with one or more substituents selected from C 1 -C 6  alkyl, halogen, \u2014CN, C 1 -C 6  alkoxy, hydroxy, \u2014NO 2 , \u2014NH 2 , C 1 -C 6  alkylamino, or C 1 -C 6  dialkylamino; or\n two R 12  together with the carbon to which they are attached form a 4- to 6 membered heterospirocycle; \n or two R 12  together when on adjacent carbons form a C 4 -C 6  cycloalkyl optionally substituted with one or more R 13 ; or \n two R 12  together when on adjacent carbons form an aryl optionally substituted with one or more R 13 ; or \n two R 12  together when on adjacent carbons form a heteroaryl optionally substituted with one or more R 13 ; or \n two R 12  together when on adjacent carbons form a heterocycloalkyl optionally substituted with one or more R 13 ; or \n R 12  with the carbon to which it is attached and the adjacent carbon form a C 3  cycloalkyl optionally substituted with one or more R 13 ; \n each R 13  is independently at each occurrence selected from C 1 -C 6  alkyl, halogen, \u2014CN, C 1 -C 6  alkoxy, C 1 -C 6  haloalkyl, C 1 -C 6  haloalkoxy, hydroxy, \u2014NO 2 , \u2014NH 2 , \u2014CH 2 NH 2 , \u2014(CH 2 ) q N(C 1 -C 6  alkyl) 2 , C 1 -C 6  alkylamino, C 1 -C 6  dialkylamino, \u2014O(CH 2 ) q N(H) C 1 -C 6  alkyl, \u2014O(CH 2 ) q N(C 1 -C 6  alkyl) 2 , aryl, heteroaryl, \u2014NH-heteroaryl, \u2014O-aryl, \u2014S(O) p \u2014C 1 -C 6  alkyl, \u2014S(O) p \u2014N(H)C 1 -C 6  alkyl, \u2014S(O) p \u2014N(C 1 -C 6  alkyl) 2 , \u2014C(O)C 1 -C 6  alkyl, \u2014NHC(O)(C 1 -C 6  alkyl), or oxo, wherein aryl and heteroaryl are optionally substituted with one or more substituents selected from consisting of C 1 -C 6  alkyl, halogen, \u2014CN, C 1 -C 6  alkoxy, hydroxy, \u2014NO 2 , \u2014NH 2 , C 1 -C 6  alkylamino, and C 1 -C 6  dialkylamino; R k  and R l  are each independently at each occurrence selected from \u2014H, C 1 -C 6  alkyl, C 1 -C 6  alkoxy, C 1 -C 6  haloalkyl, or halogen; each m, n, and p is independently at each occurrence 0, 1, or 2; and each q is independently at each occurrence 1, 2, 3 or 4, wherein the process comprises a step of contacting an aryl bromide compound: with a boronic ester compound: in the presence of a palladium catalyst to give the compound of Formula (VI).

Metadata:
- Claim Count in Document: 92.0
- Percentile: 100.0
- Lexical Diversity: 1.39535
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['16029166', '14546896', '16225484', '14546775', '15247429']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8443575674167046
- 35 USC 102 Novelty (BERT): 0.6763412107113022
- Combined Prediction Score: 0.8275559317461644
- Mean Citation Score: 465.056012
- Max Citation Score: 586.20514
- Similarity Product: 557.7889347831618

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