PATENT CLAIM ANALYSIS

Application Number: 15779353
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-10
Patent Classification: ["514", "210180"]

Abstract:
The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.

Claim (Index 1):
A compound of Formula I, including pharmaceutically acceptable salts, polymorphs, and isomers thereof: wherein:\n X is CH or N; \n Z is CH or N; with the proviso that when X is CH, Z is not also CH; \n Y is selected from the group consisting of hydrogen (H), Cl, C 1-6  alkyl, C 3-10  cycloalkyl, 4-10 membered heterocycloalkyl, OR 5 , NR 6 R 7 , \u2014C(O)OR 11 , \u2014C(O)NR 11 R 12 , C 6-10  aryl and 5-10 membered heteroaryl, wherein said 4-10 membered heterocycloalkyl and 5-10 membered heteroaryl include one or more nitrogen (N), oxygen (O) or sulfur (S) atoms; wherein said C 1-6  alkyl, C 3-10  cycloalkyl, 4-10 membered heterocycloalkyl, C 6-10  aryl and 5-10 membered heteroaryl may each optionally be substituted by one or more R 8 ; \n is (CR 9 R 10 ) n \u2014, C(O) or S(O) 2 ; \n n is 0, 1, 2, or 3; \n R 1  is selected from the group consisting of C 6-10  aryl and 5-10 membered heteroaryl, wherein said 5-10 membered heteroaryl includes one or more N, O or S atoms; wherein each of said C 6-10  aryl and 5-10 membered heteroaryl may optionally be substituted with one or more R 8 ; \n R 2  is H, C 1-6  alkyl, \u2014C(O)R 11 , \u2014CH 2 C(O)OR 11 , \u2014C(O)NR 11 R 12 , S(O) 2 NR 11 R 12  or \u2014C(O)OR 11 , wherein said C 1-6  alkyl is optionally substituted with one or more R 8 ; \n or optionally, R 1  and R 2 , together with the included nitrogen atom and L 1 , may form a 4-, 5-, 6- or 7-membered heterocyclic or heteroaryl ring system, wherein said heterocyclic or heteroaryl ring system may include one or more additional N, O or S atoms; and wherein said heterocyclic or heteroaryl ring system may optionally be substituted with one or more R 8 ; \n R 3  and R 4  are independently selected from the group consisting of H, C 1-6  alkyl, \u2014OR 11 , halogen, \u2014CN, \u2014CF 3 , \u2014NO 2 , \u2014C(O)OR 11 , \u2014OC(O)NR 11 R 12 , \u2014C(O)NR 11 R 12 , \u2014NR 11 R 12 , \u2014NR 11 C(O)R 12 , \u2014NR 11 C(O)OR 12 , \u2014NR 11 S(O) 2 R 12 , \u2014NR 11 C(O)NR 12 R 13 , S(O) 2 NR 11 R 12 , C 6-10  aryl, 5-10 membered heteroaryl, C 3-10  cycloalkyl and 4-10 membered heterocycloalkyl, wherein each of said 4-10 membered heterocycloalkyl and 5-10 membered heteroaryl include one or more N, O or S atoms; wherein said C 1-6  alkyl, C 6-10  aryl, 5-10 membered heteroaryl, C 3-10  cycloalkyl or 4-10 membered heterocycloalkyl are each optionally substituted with one or more R 8 ; \n R 5  is C 1-6  alkyl, C 3-10  cycloalkyl, 4-10 membered heterocycloalkyl, C 6-10  aryl or 5-10 membered heteroaryl, wherein each of said C 1-6  alkyl, C 3-10  cycloalkyl, 4-10 membered heterocycloalkyl, C 6-10  aryl or 5-10 membered heteroaryl is optionally substituted with one or more R 8 ; \n R 6  and R 7  are independently selected for each occurrence from the group consisting of H, C 1-6  alkyl, C 6-10  aryl, 5-10 membered heteroaryl, C3_10 cycloalkyl and 4-10 membered heterocycloalkyl, wherein said 4-10 membered heterocycloalkyl or 5-10 membered heteroaryl include one or more N, O or S atoms; wherein each of said C 1-6  alkyl, C 6-10  aryl, 5-10 membered heteroaryl, C 3-10  cycloalkyl, and 4-10 membered heterocycloalkyl may optionally be substituted with one or more R 8 ; \n or optionally, R 6  and R 7 , together with the included nitrogen, may form a 4-, 5-, 6- or 7-membered heterocyclic or heteroaryl ring system, wherein said heterocyclic or heteroaryl ring system is a mono- or bicyclic ring optionally having an additional from one to four heteroatoms selected from N, O and S; wherein said heterocyclic or heteroaryl ring system may optionally be substituted with one or more R 8 ; \n R 8  is selected independently for each occurrence from the group consisting of H, OH, SH, halogen, \u2014CN, \u2014CF 3 , \u2014NO 2 , \u2014OR 11 , \u2014SR 11 , \u2014C(O)R 11 , \u2014C(O)OR 11 , \u2014OC(O)NR 11 R 12 , \u2014C(O)NR 11 R 12 , \u2014NR 11 R 12 , \u2014NR 11 C(O)R 12 , \u2014NR 11 C(O)OR 12 , \u2014NR 11 S(O) 2 R 12 , \u2014NR 11 C(O)NR 12 R 13 , \u2014(CH 2 ) m \u2014R 16 , \u2014(CH 2 ) q \u2014R 17 , \u2014S(O)R 11 , \u2014S(O) 2 R 11 , C 1-6  alkyl, C 6-10  aryl, 5-10 membered heteroaryl, C 3-10  cycloalkyl and 4-10 membered heterocycloalkyl, wherein said C 1-6  alkyl, C 6-10  aryl, 5-10 membered heteroaryl, C 3-10  cycloalkyl and 4-10 membered heterocycloalkyl are each optionally substituted with one or more R 14 ; \n m is 1, 2, 3 or 4; \n q is 2, 3 or 4; \n R 9  and R 10  are independently chosen for each occurrence from H or C 1-6  alkyl, wherein said C 1-6  alkyl may optionally be substituted with one or more R 8 ; \n or optionally, R 9  and R 10 , together with the included carbon, may form a 3-, 4-, 5-, or 6-membered carbocyclic ring system; \n R 11 , R 12 , and R 13  are independently chosen for each occurrence from the group consisting of H, C 1-6  alkyl, C 3-10  cycloalkyl, 4-10 membered heterocycloalkyl, C 6-10  aryl and 5-10 membered heteroaryl, wherein each of said C 1-6  alkyl, C 3-10  cycloalkyl, 4-10 membered heterocycloalkyl, C 6-10  aryl and 5-10 membered heteroaryl may optionally be substituted with one or more R 14 ; \n or optionally, R 11  and R 12 , or R 12  and R 13 , together with the included nitrogen, may form a 4-, 5-, 6- or 7-membered heterocyclic or heteroaryl ring system, wherein said heterocyclic or heteroaryl ring system is a mono- or bicyclic ring optionally having an additional from one to four heteroatoms selected from N, O and S; wherein said heterocyclic or heteroaryl ring system may optionally be substituted with one or more R 8 ; \n R 14  is selected independently for each occurrence from the group consisting of H, OH, OR 18 , SH, SR 18 , halogen, CN, CF 3 , NO 2 , C(O)R 18 , C(O)OR 18 , OC(O)NR 18 R 19 , C(O)NR 18 R 19 , NR 18 R 19 , NR 18 C(O)R 19 , NR 18 C(O)OR 19 , NR 18 S(O) 2 R 19 , NR 18 C(O)NR 19 R 20 , S(O)R 18 , S(O) 2 R 18 , C 1-6  alkyl, C 3-10  cycloalkyl, 4-10 membered heterocycloalkyl, C 6-10  aryl and 5-10 membered heteroaryl, wherein said C 1-6  alkyl, C 3-10  cycloalkyl, 4-10 membered heterocycloalkyl, C 6-10  aryl and 5-10 membered heteroaryl groups may be optionally substituted with one or more of R 15 ; \n R 15  is selected independently for each occurrence from the group consisting of H, \u2014CH 3 , \u2014CH 2 CH 3 , n-propyl, isopropyl, \u2014OCH 3 , halogen, \u2014CN, \u2014CF 3 , \u2014NH 2 , \u2014N(CH 3 ) 2 , \u2014CO 2 H, \u2014C(O)NH 2 , \u2014C(O)NH(CH 3 ), and \u2014C(O)N(CH 3 ) 2 , \n each R 16  is independently \u2014CO 2 H or \u2014C(O)NR 6 R 7 ; \n each R 17  is independently \u2014OH or \u2014NR 6 R 7 ; and \n each R 18 , R 19 , and R 20  are independently selected for each occurrence from the group consisting of H, C 1-6  alkyl, C 3-10  cycloalkyl, 4-10 membered heterocycloalkyl, C 6-10  aryl and 5-10 membered heteroaryl.

Metadata:
- Claim Count in Document: 3.0
- Percentile: 93.0
- Lexical Diversity: 1.48485
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15398907', '15906163', '14977508', '15110361', '15424616']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8107977936436853
- 35 USC 102 Novelty (BERT): 0.537101844807073
- Combined Prediction Score: 0.7834281987600241
- Mean Citation Score: 352.129134
- Max Citation Score: 384.88992
- Similarity Product: 281.9940206073761

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

Dataset: test