PATENT CLAIM ANALYSIS

Application Number: 16336363
Application Type: Utility
Filing Date: 2019-03
Publication Date: 2019-07
Patent Classification: ["514", "234200"]

Abstract:
The present invention relates to a class of cyano-substituted-heterocycles of Formula (I) with activity as inhibitors of deubiquitilating enzymes, in particular, ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30), having utility in a variety of therapeutic areas including cancer and conditions involving mitochondrial dysfunction. (I)

Claim (Index 1):
A compound of formula (I): a tautomer thereof, or a pharmaceutically acceptable salt of said compound or tautomer, wherein:\n X is selected from O, N(R h ), and C(R i )(R j ); \n R a  is selected from hydrogen, fluoro, optionally substituted C 1 -C 3  alkyl, and optionally substituted C 1 -C 3  alkoxy; or R a  is linked to R b  or R 1  to form an optionally substituted C 3 -C 4  cycloalkyl ring; \n R b , R c , R d  and R e , are each independently selected from hydrogen and optionally substituted C 1 -C 3  alkyl; or form one or more spirocyclic groups where R b  is linked to R c  or R d  is linked to R e , or R b  is linked to R a  to form an optionally substituted C 3 -C 4  cycloalkyl ring; \n R f  and R g , are each independently selected from hydrogen, fluoro, cyano, optionally substituted C 1 -C 3  alkyl, and optionally substituted C 1 -C 3  alkoxy; or form a spirocyclic group where R f  is linked to R g , or R g  is linked to R i  to form an optionally substituted C 3 -C 4  cycloalkyl ring; \n when X is O or N(R h ), none of R a , R f  and R g , are fluoro or optionally substituted C 1 -C 3  alkoxy; \n R h  is selected from hydrogen, optionally substituted C 1 -C 3  alkyl, optionally substituted C(O)C 1 -C 3  alkyl, optionally substituted S(O) 2 C 1 -C 3  alkyl, and optionally substituted 3 to 6-membered ring; \n R i  and R j  are each independently selected from hydrogen, fluoro, cyano, optionally substituted C 1 -C 3  alkyl, optionally substituted C 1 -C 3  alkoxy, and optionally substituted 3 to 6-membered ring; or form a spirocyclic group where R i  is linked to R j , or R i  is linked to R a  or R g  to form an optionally substituted C 3 -C 4  cycloalkyl ring; \n ring A is a 5 to 10-membered monocyclic or bicyclic, heteroaryl or heterocyclyl ring, which is unsubstituted, or substituted with one or more Q 1 (R 1 ) n  groups, which may be the same or different; \n n is 0 or 1; \n Q 1  is selected from Q 1a  and Q 1b ; \n Q 1a  is selected from oxo, halo, cyano, nitro, hydroxyl, SR 4 , NR 2 R 3 , CONR 2 R 3 , C 0 -C 3  alkylene-NR 4 COR 5 , NR 4 CONR 5 R 6 , COR 4 , C(O)OR 4 , SO 2 R 4 , SO 2 NR 4 R 5 , NR 4 SO 2 R 5 , NR 4 SO 2 NR 5 R 6 , NR 4 C(O)OR 5 , optionally substituted C 1 -C 6  alkyl, optionally substituted C 1 -C 6  alkoxy, and optionally substituted C 2 -C 6  alkenyl; \n Q 1b  is selected from a covalent bond, an oxygen atom, a sulfur atom, OR 7 , SO, SO 2 , CO, C(O)O, C 0 -C 3  alkylene-C(O)NR 4 \u2014C 0 -C 3  alkylene, C 0 -C 3  alkylene-NR 4 \u2014C 0 -C 3  alkylene, C 0 -C 3  alkylene-NR 4 C(O)\u2014C 0 -C 3  alkylene, NR 4 CONR 5 , SO 2 NR 4 , NR 4 SO 2 , NR 4 SO 2 NR 5 , NR 4 C(O)O, NR 4 C(O)OR 7 , optionally substituted C 1 -C 6  alkylene, and optionally substituted C 2 -C 6  alkenylene; \n R 1  is a 3 to 10-membered monocyclic or bicyclic, heterocyclyl, heteroaryl, cycloalkyl, or aryl ring; \n R 2 , R 3 , R 4 , R 5  and R 6 , are each independently selected from hydrogen and optionally substituted C 1 -C 6  alkyl; \n R 7  is optionally substituted C 1 -C 6  alkylene; \n R 1  is unsubstituted or substituted with one or more substituents, each independently selected from halo, cyano, oxo, nitro, hydroxyl, SR 8 , optionally substituted C 1 -C 6  alkyl, optionally substituted C 1 -C 6  alkoxy, optionally substituted C 2 -C 6  alkenyl, optionally substituted C 2 -C 6  alkynyl, Q 2a -R 11 , Q 2a -O-Q 2b -R 11 , Q 2a -S-Q 2b -R 11 , Q 2a -SO-Q 2b -R 11 , Q 2a -NR 8 CONR 9 R 10 , Q 2a -NR 8 CONR 9 -Q 2a -R 11 , Q 2a -NR 8 R 9 , Q 2a -NR 8 -Q 2b -R 11 , Q 2a -COR 8 , Q 2a -CO-Q 2b -R 11 , Q 2a -NR 8 COR 9 , Q 2a -NR 8 CO-Q 2b -R 11 , Q 2a -NR 8 C(O)OR 9 , Q 2a -NR 8 C(O)O-Q 2b -R 11 , Q 2a -SO 2 R 8 , Q 2a -SO 2 -Q 2b -R 11 , Q 2a -CONR 8 R 9 , Q 2a -CONR 8 -Q 2b -R 11 , Q 2a -CO 2 R 8 , Q 2a -CO 2 -Q 2b -R 11 , Q 2a -SO 2 NR 8 R 9 , Q 2a -SO 2 NR 8 -Q 2b -R 11 , Q 2a -NR 8 SO 2 R 9 , Q 2a -NR 8 SO 2 -Q 2b -R 11 , Q 2a -NR 8 SO 2 NR 9 R 10 , and Q 2a -NR 8 SO 2 NR 9 -Q 2b -R 11 ; \n Q 2a  and Q 2b  are each independently selected from a covalent bond, optionally substituted C 1 -C 6  alkylene, and optionally substituted C 2 -C 6  alkenylene; \n R 8 , R 9  and R 10 , are each independently selected from hydrogen and optionally substituted C 1 -C 6  alkyl; and \n R 11  is selected from optionally substituted heterocyclyl, optionally substituted heteroaryl, optionally substituted aryl, and optionally substituted cycloalkyl; \n for use in the treatment of a disorder or condition where inhibition of USP30 is known, or can be shown, to produce a beneficial effect, in a mammal.

Metadata:
- Claim Count in Document: 32.0
- Percentile: 99.0
- Lexical Diversity: 1.32558
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['16070936', '16080506', '15738900', '15894025', '16078518']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8434976798457242
- 35 USC 102 Novelty (BERT): 0.5615069360561646
- Combined Prediction Score: 0.8152986054667682
- Mean Citation Score: 433.761262
- Max Citation Score: 448.00748
- Similarity Product: 366.7375607883597

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

Dataset: test