PATENT CLAIM ANALYSIS

Application Number: 16171236
Application Type: Utility
Filing Date: 2018-10
Publication Date: 2019-02
Patent Classification: ["514", "211100"]

Abstract:
The present invention relates to compounds of formula I wherein R 1 , R 2 , R 3 , R 4a , R 4b , R 4c , R 4d , L, A, Q, W and HET are each as defined herein. The compounds of the present invention are inhibitors of autotaxin (ATX) enzyme activity. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions (e.g. fibrosis) in which ATX activity is implicated.

Claim (Index 37):
A method of treating a cancer selected from lung, colon, breast, ovarian, prostate, liver, pancreas, brain, bladder, kidney, bone, nerve and skin cancer in a patient in need of such treatment, said method comprising administering to said patient a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt or solvate thereof, having the structural formula (I) shown below: wherein:\n R 1  and R 2  are independently selected from H, (1-8C)alkyl, (4-7C)cycloalkyl, 4-7 membered heterocyclyl, 5-6 membered heteroaryl, \u2014S(O) y R a  or C(O)R a , wherein R a  is selected from H, (1-4C)alkyl or (1-4C)alkoxy, y is 0, 1 or 2, and wherein any (1-8C)alkyl, (4-7C)cycloalkyl, 4-7 membered heterocyclyl or 5-6 membered heteroaryl is optionally substituted by one or more substituents selected from oxo, (1-4C)alkyl, halo, cyano, nitro, hydroxyl, amino, (1-4C)haloalkyl, (1-4C)alkoxy, (1-4C)haloalkoxy, carboxyl, carbamoyl, sulphamoyl, NR b R c , OR b , C(O)R b , C(O)OR b , OC(O)R b , C(O)N(R b )R c , N(R b )C(O)R c , S(O) y R b  (where y is 0, 1 or 2), SO 2 N(R b )R c , N(R b )SO 2 R c  or (CH 2 ) z NR b R c  (where z is 1, 2 or 3), (4-6C)heterocycyl, 6 membered aryl or 5 or 6 membered heteroaryl, wherein R b  and R c  are each independently selected from H or (1-4C)alkyl; or \n R 1  and R 2  are linked such that, together with the nitrogen atom to which they are attached, they form a 4 to 10 membered mono or bicyclic heterocyclic ring which is optionally substituted by one or more substituents selected from oxo, (1-4C)alkyl, halo, cyano, nitro, hydroxyl, amino, (1-4C)haloalkyl, (1-4C)alkoxy, (1-4C)haloalkoxy, carboxyl, carbamoyl, sulphamoyl, NR d R e , OR d , C(O)R d , C(O)OR d , OC(O)R d , C(O)N(R e )R d , N(R e )C(O)R d , S(O) y R d  (where y is 0, 1 or 2), SO 2 N(R e )R d , N(R e )SO 2 R d  or (CH 2 ) z NR d R e  (where z is 1, 2 or 3), (4-6C)heterocycyl, 6 membered aryl or 5 or 6 membered heteroaryl, wherein R d  and R e  are each independently selected from H or (1-4C)alkyl; L is a (1-3C)alkylene optionally substituted by fluoro, (1-2C)alkyl or oxo; R 4a , R 4b , R 4c  and R 4d  are each independently selected from H, halo, (1-2C)alkyl, cyano, nitro, hydroxyl, amino, (1-2C)haloalkyl, (1-2C)alkoxy, or (1-2C)haloalkoxy; A is C(\u2550X) or CR f R g ;\n wherein X is O, NH or S; and \n R f  and R g  are independently selected from H or (1-2C)alkyl; \n Q is selected from \u2014NH\u2014S(O) y \u2014, \u2014S(O) y \u2014NH\u2014, \u2014C(O)NR h \u2014, \u2014NR h C(O)\u2014, \u2014NR h \u2014S(O)(NH)\u2014, \u2014S(O)(NH)\u2014NR h \u2014, \u2014C(O)O\u2014, \u2014OC(O)\u2014, \u2014CH 2 CH 2 \u2014, \u2014CH 2 NR h \u2014 or \u2014NR h CH 2 \u2014, wherein y is 0, 1 or 2 and R h  is selected from H or (1-2C)alkyl; HET is a 5 or 6 membered nitrogen containing heteroaryl optionally substituted with one or more substituents selected from H, (1-4C)alkyl, halo, cyano, nitro, hydroxyl, amino, (1-4C)haloalkyl, (1-4C)alkoxy, (1-4C)haloalkoxy, carboxyl, carbamoyl, amido or sulphamoyl; W is either a group of the formula:\n -Q 1 -R i \u2014 \n wherein:\n Q 1  is attached to HET and is \u2014C(O)\u2014 or \u2014CH 2 \u2014; and \n R i  is attached to R 3  and is selected from \u2014CHR j \u2014, \u2014NR j \u2014, or \u2014O\u2014, wherein R j  is selected from H or (1-2C)alkyl; \n or W is a group of the formula:\n \u2014R k -Q 2 - \n wherein:\n Q 2  is attached to R 3  and is selected from \u2014C(O)\u2014 or \u2014CH 2 \u2014; and \n R k  is attached to HET and is selected from CHR 1 , NR 1 , O or S(O) y , wherein y is 0, 1 or 2 and R 1  is H or (1-4C)alkyl; \n R 3  is selected from (1-6C)alkyl, phenyl, (4-8C)carbocyclyl, heteroaryl or heterocyclyl, each of which is optionally substituted with one or more substituents selected from (1-4C)alkyl, halo, (1-4C)haloalkyl, (1-4C)alkoxy, (1-4C)haloalkoxy, (3-6C)cycloalkyl, (3-6C)cycloalkyl(1-2C)alkyl, (2-4C)alkenyl or (2-4C)alkynyl.

Metadata:
- Claim Count in Document: 47.0
- Percentile: 97.0
- Lexical Diversity: 1.75758
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15547776', '15554354', '10718337', '15533804', '10922425']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7548607934931945
- 35 USC 102 Novelty (BERT): 0.6256365069402631
- Combined Prediction Score: 0.7419383648379014
- Mean Citation Score: 412.327196
- Max Citation Score: 672.92206
- Similarity Product: 489.2836852822243

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