PATENT CLAIM ANALYSIS

Application Number: 15764071
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2018-12
Patent Classification: ["546", "256000"]

Abstract:
Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.

Claim (Index 1):
A compound represented by Formula (I), or a pharmaceutically acceptable salt thereof: wherein, independently for each occurrence: R 1  represents \u2014OH, \u2014OR c , \u2014NH 2 , \u2014NHR c , \u2014NR c R d , alkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, halo, haloalkyl, cycloalkyl, (cycloalkyl)alkyl, \u2014C(O)R c , \u2014C(O)OH, \u2014C(O)OR c , \u2014OC(O)R c , \u2014C(O)NH 2 , \u2014C(O)NHR c , \u2014C(O)NR c R d , \u2014NHC(O)R c , or \u2014NR c C(O)R d ; or two geminal occurrences of R 1  taken together with the carbon to which they are attached represent \u2014C(O)\u2014; or two vicinal or geminal occurrences of R 1  taken together form an optionally substituted fused or spirocyclic carbocyclic or heterocyclic ring; W is a bond, \u2014C(O)NH\u2014, \u2014C(O)N(R c )\u2014, \u2014C(O)O\u2014, \u2014CH 2 \u2014, or \u2014C(O)\u2014; R 2  represents optionally substituted aryl, heteroaryl, aralkyl, heteroaralkyl, cycloalkyl, heterocycloalkyl, (cycloalkyl)alkyl), or (heterocycloalkyl)alkyl; V represents optionally substituted aryl or heteroaryl; Z is absent or represents one or more substituents independently selected from the group consisting of halo, haloalkyl, \u2014NO 2 , \u2014CN, \u2014C(O)R c , \u2014C(O)OH, \u2014C(O)OR c , \u2014OC(O)R c , \u2014C(O)NH 2 , \u2014C(O)NHR c , \u2014C(O)NR c R d , \u2014NHC(O)R c , \u2014N(R c )C(O)R d , \u2014OS(O) p (R c ), \u2014NHS(O) p (R c ), and \u2014NR c S(O) p (R c ); X represents \u2014C(NH 2 )\u2014, \u2014C(NH(R c ))\u2014, \u2014C(NR c R d )\u2014, \u2014C(NHS(O) p R c )\u2014, \u2014C(NHC(O)R c )\u2014, \u2014C(NHC(O)NH 2 )\u2014, \u2014C(NHC(O)NHR c )\u2014, \u2014C(NHC(O)NR c R d )\u2014, \u2014C(OH)\u2014, \u2014C(O(alkyl))-, \u2014C(N 3 )\u2014, \u2014C(CN)\u2014, \u2014C(NO 2 )\u2014, \u2014C(S(O) n R a )\u2014, \u2014C[\u2014C(\u2550O)R c ]\u2014, \u2014C[\u2014C(\u2550O)NR c R d ]\u2014, \u2014C[\u2014C(\u2550O)SR c ]\u2014, \u2014C[\u2014S(O)R c ]\u2014, \u2014C[\u2014S(O) 2 R]\u2014, \u2014C[S(O)(OR c )]\u2014, \u2014C[\u2014S(O) 2 (OR c )]\u2014, \u2014C[\u2014SO 2 NR c R d ]\u2014, \u2014C(halogen)-, \u2014C(alkyl), \u2014C((cycloalkyl)alkyl), \u2014C(alkenyl)-, \u2014C(alkynyl)-, or \u2014C(aralkyl)-; R 3  represents optionally substituted aryl, heteroaryl, cycloalkyl, or heterocycloalkyl; R 3a  is absent or represents one or more substituents independently selected from the group consisting of halo, hydroxy, alkyl, \u2014CF 3 , \u2014OCF 3 , alkoxy, aryl, heteroaryl, aryloxy, amino, aminoalkyl, \u2014C(O)NH 2 , cyano, \u2014NHC(O)alkyl, \u2014SO 2 alkyl, \u2014SO 2 NH 2 , cycloalkyl, \u2014(CH 2 ) r OR a , \u2014NO 2 , \u2014(CH 2 ) r NR a R b , \u2014(CH 2 ) r C(O)R a , \u2014NR a C(O)R b , \u2014C(O)NR c R d , \u2014NR a C(O)NR c R d , \u2014C(\u2550NR a )NR c R d , \u2014NHC(\u2550NR a )NR c R d , \u2014NR a R b , \u2014SO 2 NR c R d , \u2014NR a SO 2 NR c R d , \u2014NR a SO 2 alkyl, \u2014NR a SO 2 R a , \u2014S(O) p R a , \u2014(CF 2 ) r CF 3 , \u2014NHCH 2 R a , \u2014OCH 2 R a , \u2014SCH 2 R a , \u2014NH(CH 2 ) 2 (CH 2 ) r R a , \u2014O(CH 2 ) 2 (CH 2 ) r R a , or \u2014S(CH 2 ) 2 (CH 2 ) r R a ; Y represents a bond; or \u2014Y\u2014R 4  represents optionally substituted -alkylene-R 4 , \u2014CH 2 C(O)\u2014R 4 , \u2014CH 2 NH\u2014R 4 , \u2014CH 2 N(alkyl)-R 4 , \u2014CR a R b \u2014R 4 , \u2014NH\u2014R 4 , \u2014NHCH 2 \u2014R 4 , \u2014NHC(O)\u2014R 4 , \u2014N(alkyl)-R 4 , \u2014N(alkyl)CH 2 \u2014R 4 , \u2014N((CH 2 ) 2 OH)\u2014R 4 , \u2014N((cycloalkyl)alkyl)R 4 , -heterocyclyl-R 4 , \u2014OR 4 , \u2014OCH 2 \u2014R 4 , \u2014OC(O)\u2014R 4 , \u2014OC(O)NR a R b , \u2014SCH 2 R 4 , or \u2014SR 4 ; R 4  represents hydrogen, hydroxy, optionally substituted alkyl, cycloalkyl, (heterocycloalkyl)alkyl, (cycloalkyl)alkyl, \u2014CH 2 OH, \u2014CH(alkyl)OH, \u2014CH(NH 2 )CH(alkyl) 2 , aryl, aralkyl, heteroaryl, heteroaralkyl, \u2014CH 2 S(alkyl), amino, or cyano; or \u2014(CR a R b ) r (CR a R b ) p \u2014 fused to the 4-position of the ring bearing Z to form a 5- to 7-membered heterocyclic ring with optional substituents; or, when R 3  is phenyl, R 4  can represent \u2014NR a \u2014 fused to the position ortho to X on that phenyl; each R a  and R b  is independently H, alkyl, alkenyl, alkynyl, aralkyl, (cycloalkyl)alkyl, \u2014C(\u2550O)R c , \u2014C(\u2550O)OR c , \u2014C(\u2550O)NR c R d , \u2014C(\u2550O)SR c , \u2014S(O)R c , \u2014S(O) 2 R c , \u2014S(O)(OR c ), or \u2014SO 2 NR c R d ; R c  and R d  represent, independently for each occurrence, optionally substituted alkyl, alkenyl, alkynyl, haloalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, (cycloalkyl)alkyl, heterocycloalkyl, (heterocycloalkyl)alkyl, \u2014C(O)alkyl, or \u2014S(O) p (alkyl); or R c  and R d  can be taken together to form an optionally substituted heterocyclic ring; can represent r is 0, 1, 2, or 3; n is an integer from 0 to 6; and p is 0, 1, or 2.

Metadata:
- Claim Count in Document: 5.0
- Percentile: 90.0
- Lexical Diversity: 1.575
- Patent Class: 546.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15123059', '15697755', '15199779', '15380836', '12774544']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.818564493190959
- 35 USC 102 Novelty (BERT): 0.5588978943061063
- Combined Prediction Score: 0.7925978333024738
- Mean Citation Score: 377.365504
- Max Citation Score: 445.71603
- Similarity Product: 338.05748130804784

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