PATENT CLAIM ANALYSIS

Application Number: 15894025
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-06
Patent Classification: ["514", "215000"]

Abstract:
The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1). The invention further relates to the use of DUB inhibitors in the treatment of cancer and other indications. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R8 are as defined herein.

Claim (Index 18):
A compound of formula (I): a tautomer thereof, or a pharmaceutically acceptable salt of said compound or tautomer, wherein: R 1  represents a 5 to 10-membered heteroaryl ring; R 2 , R 3 , R 4 , R 5 , R 6  and R 8  each independently represent a hydrogen atom, cyano, C 1 -C 3  alkyl, C 1 -C 3  alkoxy group, or R 2  is linked to R 8  to form a C 3 -C 4  cycloalkyl ring, or R 6  is linked to R 7  to form a C 3 -C 4  cycloalkyl ring; wherein said alkyl, alkoxy and cycloalkyl groups may be optionally substituted with one or more substituents, which may be the same or different, selected from halo, deutero, C 1-3  alkyl, C 1-3  alkoxy, and cyano; R 7  represents a hydrogen atom, a fluorine atom, cyano, C 1 -C 3  alkyl, CF 3 , C 1 -C 3  alkoxy group or an aryl or heteroaryl ring or is linked to R 8  to form a spirocyclic group or is linked to R 6  to form a C 3 -C 4  cycloalkyl ring; wherein R 1  may be optionally substituted with one or more of Q 1 -(R 9 ) n ; n is 0 or 1; Q 1  represents a hydrogen atom, a halogen atom, cyano, a covalent bond, \u2014NR 10 \u2014, \u2014CONR 10 \u2014, \u2014NR 10 CO\u2014, an oxygen atom, oxo, nitro, \u2014S(O) m \u2014, C 1 -C 6  alkoxy, C 1 -C 6  haloalkoxy, C 1 -C 6  hydroxyalkyl, \u2014CO\u2014, \u2014SO 2 R 11 , \u2014NR 11 R 12 , \u2014NR 11 COR 12 , \u2014NR 10 CONR 11 R 12 , \u2014CONR 11 R 12 , \u2014CO 2 R 11 , \u2014NR 11 CO 2 R 12 , \u2014SO 2 NR 11 R 12 , \u2014C(O)R 11 , \u2014NR 11 SO 2 R 12 , NR 11 SO 2 NR 13 R 14 , and SO 2 NR 11 , C 1 -C 6  alkylene, \u2014C 2 -C 6  alkenylene, \u2014C 1 -C 6  alkyl, or C 1 -C 2  haloalkyl group; m is 0, 1 or 2; R 9  represents a 3 to 10-membered heterocyclyl, heteroaryl, aryl or cycloalkyl ring; and R 10 , R 11  and R 12  each independently represent a hydrogen atom, a C 1 -C 6  alkyl, or a C 1 -C 6  alkylene group; wherein R 9  may be optionally substituted with one or more substituents selected from halogen, C 1 -C 6  haloalkyl, C 1 -C 6  alkoxy, C 1 -C 6  haloalkoxy, C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 1 -C 6  hydroxyalkyl, oxo, cyano, nitro, heterocyclyl, cycloalkyl, heteroaryl, aryl, -Q 2 -NR 13 CONR 14 R 15 , -Q 2 -NR 13 R 14 , -Q 2 -NR 13 COR 4 , -Q 2 -COR 13 , -Q 2 -SO 2 R 13 , -Q 2 -CONR 13 , Q 2 -CONR 13 R 14 , -Q 2 -CO 2 R 13 , -Q 2 -SO 2 NR 13 R 14 , -Q 2 -NR 13 SO 2 R 14 , and -Q 2 -NR 13 SO 2 NR 14 R 15 ; wherein said alkyl, alkoxy and heteroaryl groups may be optionally substituted with halo, deutero, C 1-3  alkyl, hydroxy, C 1-3  alkoxy, cyano, amino, nitro, oxo, aryl, heteroaryl, heterocyclyl, C 3 -C 6  cycloalkyl, C 1-3  alkylamino, C 2-6  alkenylamino, di-C 1-3  alkylamino, C 1-3  acylamino, di-C 1-3  acylamino, carboxy, C 1-3  alkoxycarbonyl, carbamoyl, mono-C 1-3  carbamoyl, di-C 1-3  carbamoyl or any of the above in which a hydrocarbyl moiety is itself substituted by halo; or R 9  may be substituted with a 3 to 10-membered heterocyclyl, heteroaryl, aryl or cycloalkyl ring either directly attached or via linking group selected from oxygen, a carbonyl, an optionally substituted C 1 -C 6  alkylene or an optionally substituted C 1 -C 6  alkyleneoxy chain; Q 2  represents a covalent bond or a C 1 -C 6  alkylene or C 2 -C 6  alkenylene group; and R 13 , R 14  and R 15  each independently represent hydrogen, C 1 -C 6  alkyl, heterocyclyl, heteroaryl, aryl, or cycloalkyl; wherein said alkyl group may be optionally substituted with halo, deutero, C 1-3  alkyl, hydroxy, C 1-3  alkoxy, cyano, amino, nitro, oxo, aryl, heteroaryl, heterocyclyl, C 3 -C 6  cycloalkyl, C 1-3  alkylamino, C 2-6  alkenylamino, di-C 1-3  alkylamino, C 1-3  acylamino, di-C 1-3  acylamino, carboxy, C 1-3  alkoxycarbonyl, carbamoyl, mono-C 1-3  carbamoyl, di-C 1-3  carbamoyl or any of the above in which a hydrocarbyl moiety is itself substituted by halo.

Metadata:
- Claim Count in Document: 50.0
- Percentile: 88.0
- Lexical Diversity: 1.56364
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15513125', '16070936', '16060299', '15738900', '16080506']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8278505560406889
- 35 USC 102 Novelty (BERT): 0.6647640131471187
- Combined Prediction Score: 0.8115419017513319
- Mean Citation Score: 564.0303700000002
- Max Citation Score: 695.69135
- Similarity Product: 606.7798891741007

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