PATENT CLAIM ANALYSIS

Application Number: 15864499
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2018-05
Patent Classification: ["514", "264000"]

Abstract:
The present invention relates to compounds of formula I wherein R 1 , R 4 , Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

Claim (Index 18):
A method of treating a proliferative disorder in a patient in need of such treatment, said method comprising administering to said patient a therapeutically effective amount of a compound according to formula I, or a pharmaceutically acceptable salt or solvate thereof: wherein: W is N or C\u2014R 3 ; X is CH or N; Z is N or CH, R 1  is selected from chloro, (1-6C)alkyl, (1-8C)heteroalkyl, aryl, aryl(1-2C)alkyl, heteroaryl, heteroaryl(1-2C)alkyl, heterocyclyl, heterocyclyl(1-2C)alkyl, (3-8C)cycloalkyl, (3-8C)cycloalkyl(1-2C)alkyl, NR 7 R 8 , OR 9 , C(O)R 9 , C(O)OR 9 , OC(O)R 9 , N(R 10 )OR 9 , N(R 10 )C(O)OR 9 , C(O)N(R 10 )R 9 , N(R 10 )C(O)R 9 , S(O) p R 9  (where p is 0, 1 or 2), SO 2 N(R 10 )R 9 , N(R 10 )SO 2 R 9 , N(R 10 )SOR 9  and SON(R 10 )R 9 , and wherein R 1  is optionally substituted by one or more substituent groups selected from fluoro, chloro, trifluoromethyl, trifluoromethoxy, cyano, nitro, hydroxy, amino, carboxy, carbamoyl, sulphamoyl, (1-4C)alkyl, (1-4C)alkoxy, S(O) q CH 3  (where q is 0, 1 or 2), methylamino or dimethylamino, aryl, aryl(1-2C)alkyl, heteroaryl, heteroaryl(1-2C)alkyl, heterocyclyl, heterocyclyl(1-2C)alkyl, (3-8C)cycloalkyl, and (3-8C)cycloalkyl(1-2C)alkyl, and wherein any (1-4C)alkyl, (1-4C)alkoxy, aryl, heteroaryl, heterocyclyl, or (3-8C)cycloalkyl moiety present within a substituent group on R 1  is optionally further substituted by fluoro, chloro, trifluoromethyl, trifluoromethoxy, cyano, nitro, hydroxy, amino, carboxy, carbamoyl, sulphamoyl, (1-4C)alkyl, NR a R b , OR a , C(O)R a , C(O)OR d , OC(O)R a , N(R b )OR a , C(O)N(R b )R a , N(R b )C(O)R a , S(O) p R a  (where p is 0, 1 or 2), SO 2 N(R b )R a , or N(R b )SO 2 R a , wherein R a  and R b  are each independently selected from H and (1-4C)alkyl; R3 is hydrogen, (1-4C)alkyl, (3-6C)cycloalkyl, halo, CF 3 , CN or (1-4C)alkoxy; R4 is hydrogen, (1-3C)alkyl, (1-3C)alkoxy, fluoro, chloro or CF, Ar has the formula: wherein: (i) all of A 1 , A 2  and A 3  are CH; (ii) one of A 1 , A 2  and A 3  is N and the others are CH; or (iii) two of A 1 , A 2  and A 3  are N and the other is CH; R 5  is selected from hydrogen, cyano, (1-3C)alkyl, (1-3C)fluoroalkyl, (1-3C)alkoxy, (1-3C)fluoroalkoxy, halo, (1-3C)alkanoyl, C(O)NR 15 R 16  or S(O) 2 NR 15 R 16 , and wherein R 15  and R 16  are each independently selected from H and (1-3C)alkyl, and wherein any alkyl or alkoxy moities present within a R 5  substituent group are optionally further substituted by hydroxy or methoxy; R 6  is selected from halo, trifluoromethyl, trifluoromethoxy, cyano, nitro, hydroxy, amino, carboxy, carbamoyl, sulphamoyl, ureido, (1-6C)alkyl, (2-6C)alkenyl, and (2-6C)alkynyl, or R 6  is a group of the formula:\n -L 1 -L 2 -R 17  \n wherein \n L 1  is absent or a linker group of the formula \u2014[CR 18 R 19 ] n \u2014 in which n is an integer selected from 1, 2, 3 and 4, and R 18  and R 19  are each independently selected from hydrogen and (1-2C)alkyl; \n L 2  is absent or is selected from O, S, SO, SO 2 , N(R 20 ), C(O), C(O)O, OC(O), CH(OR 20 ), C(O)N(R 20 ), N(R 20 )C(O), N(R 20 )C(O)N(R 21 ), S(O) 2 N(R 20 ), and N(R 21 )SO 2 , wherein R 20  and R 21  are each independently selected from hydrogen and (1-2C)alkyl; and \n R 17  is (1-6C)alkyl, aryl, aryl-(1-6C)alkyl, (3-6C)cycloalkyl, (3-6C)cycloalkyl-(1-4C)alkyl, heteroaryl, heteroaryl-(1-4C)alkyl, heterocyclyl, or heterocyclyl-(1-4C)alkyl; \n and wherein R 17  is optionally further substituted by one or more substituent groups independently selected from oxo, halo, cyano, nitro, hydroxy, NR 22 R 23 , (1-4C)alkoxy, (1-4C)alkyl, (3-8C)cycloalkyl, (3-8C)cycloalkyl-(1-3C)alkyl, (1-5C)alkanoyl, (1-5C)alkylsulphonyl, heterocyclyl, heterocyclyl-(1-2C)alkyl, heteroaryl, heteroaryl-(1-2C)alkyl, CONR 22 R 23 , and SO 2 NR 22 R 23 ; wherein R 22  and R 23  are each independently selected from hydrogen, (1-4C)alkyl, (3-6C)cycloalkyl and (3-6C)cycloalkyl(1-2C)alkyl; \n and wherein when said substituent group comprises an alkyl, cycloalkyl, heterocyclyl or heteroaryl moiety then said moiety is optionally further substituted by hydroxy, fluoro, chloro, cyano, CF 3 , OCF 3 , (1-2C)alkyl, (1-2C)alkoxy, SO 2 (1-2C)alkyl or NR e R f  (where R e  and R f  are each independently selected from hydrogen, (1-3C)alkyl, (3-6C)cycloalkyl, and (3-6C)cycl \u00b0 alkyl(1-2C)alkyl);\n or R 17  is a group having the formula:\n -L 3 -L 4 -R 24  \n \n \n wherein L 3  is absent or a linker group of the formula \u2014[CR 25 R 26 ] n \u2014 in which n is an integer selected from 1, 2, 3 and 4, and R 25  and R 26  are each independently selected from hydrogen and (1-2C)alkyl; \n L 4  is absent or is selected from O, S, SO, SO 2 , N(R 27 ), C(O), C(O)O, OC(O), CH(OR 27 ), C(O)N(R 27 ), N(R 27 )C(O), N(R 27 )C(O)N(R 28 ), S(O) 2 N(R 27 ), and N(R 28 )SO 2 , wherein R 27  and R 28  are each independently selected from hydrogen and (1-2C)alkyl; and \n R 24  is (1-6C)alkyl, aryl, aryl-(1-6C)alkyl, (3-6C)cycloalkyl, (3-6C)cycloalkyl-(1-4C)alkyl, heteroaryl, heteroaryl-(1-4C)alkyl, heterocyclyl, or heterocyclyl-(1-4C)alkyl; \n R 8  and R 9  are each independently selected from hydrogen, (1-6C)alkyl, (1-6C)alkoxy, (3-9C)cycloalkyl, (3-9C)cycloalkyl-(1-2C)alkyl, aryl, aryl-(1-2C)alkyl, heterocyclyl, heterocyclyl-(1-2C)alkyl, heteroaryl, and heteroaryl-(1-2C)alkyl; and wherein R 8  and R 9  are optionally further substituted by one or more substituents selected from hydroxy, fluoro, chloro, cyano, CF 3 , OCF 3  (1-2C)alkyl and (1-2C)alkoxy; R 7  and R 10  are independently selected from hydrogen, (1-6C)alkyl, (3-6C)cycloalkyl, and (3-6C)cycloalkyl-(1-2C)alkyl; and wherein R 7  and R 10  are optionally further substituted by one or more substituents selected from hydroxy, fluoro, chloro, cyano, CF 3 , OCF 3 , (1-2C)alkyl and (1-2C)alkoxy; subject to the provisos that:\n X is only N when Z is N; \n W is only N when X and Z are both N; and \n R 6  is not methoxy when R 1  is S(O) 2 R 9  and R 9  is heterocyclyl.

Metadata:
- Claim Count in Document: 56.0
- Percentile: 86.0
- Lexical Diversity: 1.69118
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15091887', '15121432', '15069012', '14426574', '15091980']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7987038899430702
- 35 USC 102 Novelty (BERT): 0.6147146754688534
- Combined Prediction Score: 0.7803049684956486
- Mean Citation Score: 495.849256
- Max Citation Score: 593.34357
- Similarity Product: 478.139920860976

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

Dataset: test