PATENT CLAIM ANALYSIS

Application Number: 16161409
Application Type: Utility
Filing Date: 2018-10
Publication Date: 2019-02
Patent Classification: ["544", "182000"]

Abstract:
According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A 1 -A 2b  or, particularly, the A 2a  receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy 1  or Het A ; Cy 1  represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cy 1  group is optionally substituted by one or more R 4a  substituents; Het A  represents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cy 2  or Het B ; Cy 2  represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, which Cy 2  group is optionally substituted by one or more R 4c  substituents; Het B  represents a 3- to 10-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one or two rings and which Het B  group is optionally substituted by one or more R 4d  substituents.

Claim (Index 18):
A method of treatment of cancer comprising administering an effective amount of a compound to a patient in need of such treatment, wherein the compound is represented by formula A1: wherein: A represents Cy AA  or Het AA ; Cy AA  represents a 6-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system, which Cy AA  group is substituted, in the 3-position relative to the point of attachment to the triazine ring, with a R 4a  substituent and is optionally substituted by one or more additional R 4a  substituents; Het AA  represents a 6-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, and which Het AA  group is substituted, in the 3-position relative to the point of attachment to the triazine ring, with a R 4b  substituent and is optionally substituted by one or more additional R 4b  substituents; B represents a Cy BB  or Het BB ; Cy BB  represents phenyl optionally substituted by one or more R 4c  substituents; Het BB  represents a 6-membered aromatic heterocyclic group which contains one or more N atoms, and which Het BB  group is optionally substituted by one or more R 4d  substituents; R 4a  to R 4d  represent, independently at each occurrence, (a) halo, (b) CN, (c) C 1-12  alkyl, C 2-12  alkenyl, C 2-12  alkynyl, which latter three groups are optionally substituted by one or more substituents selected from halo, nitro, CN, C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl (which latter three groups are optionally substituted by one or more substituents selected from OH, \u2550O, halo, C 1-4  alkyl and C 1-4  alkoxy), OR 5a , S(O) q R 5b , S(O) 2 N(R 5c )(R 5d ), N(R 5e )S(O) 2 R 5f , N(R 5g )(R 5h ), B 1 \u2014C(G 1 )-B 2 \u2014R 5i , aryl and Het 1 , (d) Cy 3 , which Cy 3  group is optionally substituted by one or more substituents selected from halo, nitro, CN, C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl (which latter three groups are optionally substituted by one or more substituents selected from OH, \u2550O, halo, C 1-4  alkyl and C 1-4  alkoxy), OR 6a , S(O) q R 6b , S(O) 2 N(R 6c )(R 6d ), N(R 6e )S(O) 2 R 6f , N(R 6g )(R 6h ), B 3 \u2014C(G 1 )-B 4 \u2014R 6i , aryl and Het 2 , (e) Het a , which Het a  group is optionally substituted by one or more substituents selected from halo, nitro, CN, C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl (which latter three groups are optionally substituted by one or more substituents selected from OH, \u2550O, halo, C 1-4  alkyl and C 1-4  alkoxy), OR 7a , S(O) q R 7b , S(O) 2 N(R 7c )(R 7d ), N(R 7e )S(O) 2 R 7f , N(R 7g )(R 7h ), B 5 \u2014C(G 1 )-B 6 \u2014R 7i , aryl and Het 3 , (f) OR 8 , (g) S(O) r R 9a , (h) S(O) 2 N(R 9b )(R 9c ), (i) N(R 9d )S(O) 2 R 9e , (j) N(R 9f )(R 9g ), (k) B 7 \u2014C(G 1 )-B 8 \u2014R 9h , (l) \u2550O, (m) \u2550S, or when two R 4a , R 4b , R 4c  or R 4d  groups are attached to the same carbon atom in a non-aromatic portion of a Cy AA , Het AA , Cy BB  or Het BB  group, they may form, together with the carbon atom to which they are attached, a saturated or unsaturated 3 to 6-membered ring, which ring optionally contains one to three heteroatoms selected from O, S and N, and which ring is optionally substituted by one or more R 9i  substituents; G 1  represents, independently at each occurrence, O, S or NR 5j ; R 8  represents, independently at each occurrence,\n H, \n Cy 3 , Het a , aryl a , C 1-8  alkyl, C 2-8  alkenyl, C 2-8  alkynyl, C 3-8  cycloalkyl, which latter seven groups are optionally substituted by one or more substituents selected from halo, \u2014CN, C 3-6  cycloalkyl, aryl, Het 4 , \u2014C(O)OR 10 , \u2014C(O)R 11 , \u2014C(O)N(R N1 )(R N2 ), S(O) r R 9aa , S(O) 2 N(R 9ba )(R 9ca ), N(R 9da )S(O) 2 R 9ea  and N(R 9fa )(R 9ga ); \n Cy 3  represents, independently at each occurrence, a 3- to 6-membered aromatic, fully saturated or partially unsaturated carbocyclic ring; Het a  represents, independently at each occurrence, a 3- to 6-membered heterocyclic ring that may be aromatic, fully saturated or partially unsaturated and which contains one or more heteroatoms selected from O, S and N; R 10  and R 11  independently represent (a) H, (b) C 1-6  alkyl optionally substituted by one or more substituents selected from halo, aryl, \u2014N(R N3 )(R N4 ) and \u2014OR a , (c) aryl or (d) C 3-7  cycloalkyl (which group is optionally substituted by one or more substituents selected from OH, \u2550O, halo, C 1-4  alkyl and C 1-4  alkoxy); B 1  to B 8  independently represent, at each occurrence, a direct bond, O, S or N(R N3 ); each aryl a  independently represents a C 6-14  carbocyclic aromatic group, which group may comprise one, two or three rings; each aryl independently represents a C 6-14  carbocyclic aromatic group, which group may comprise one, two or three rings and may be substituted by one or more substituents selected from\n halo, \n C 1-6  alkyl, which latter group is optionally substituted by one or more substituents selected from halo, \u2014N(R N4 )(R N5 ) and \u2014OR a , and \n OR a ; \n Het 1  to Het 4  independently represent 4- to 14-membered heterocyclic groups containing one or more heteroatoms selected from O, S and N, which heterocyclic groups may comprise one, two or three rings and may be substituted by one or more substituents selected from\n halo, \n C 1-6  alkyl, which latter group is optionally substituted by one or more substituents selected from halo, \u2014N(R N6 )(R N7 ) and \u2014OR a , and \n \u2014OR a : \n R N1  to R N7  independently represent\n H, \n C 1-6  alkyl or C 3-6  cycloalkyl, which latter two groups are optionally substituted by one or more substituents selected from halo and \u2014OR a : \n R a  represents, independently at each occurrence, (a) H; (b)C 1-12  alkyl, C 2-12  alkenyl, C 2-12  alkynyl, C 3-12  cycloalkyl, C 4-12  cycloalkenyl, which latter five groups are optionally substituted by one or more substituents selected from halo, nitro, CN, C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 3-8  cycloalkyl (which latter four groups are optionally substituted by one or more substituents selected from OH, \u2550O, halo, C 1-4  alkyl and C 1-4  alkoxy), OR 12a , S(O) q R 12b , S(O) 2 N(R 12c )(R 12d ), N(R 12e )S(O) 2 R 12f , N(R 12g )(R 12h ), B 9 \u2014C(G 2 )-B 10 \u2014R 12i , aryl 1  and Het b , and which C 3-12  cycloalkyl or C 4-12 , cycloalkenyl groups may additionally be substituted by \u2550O, (c) S(O) r R 13a , (d) S(O) 2 N(R 13b )(R 13c ) or (e) C(O)\u2014B 11 \u2014R 13d ; R 5a  to R 5j , R 6a  to R 6i , R 7a  to R 7i , R 9a  to R 9i , R 9aa  to R 9ga , R 12a  to R 12i  and R 13a  to R 13d  independently represent, at each occurrence, (a) H, (b) C 1-10  alkyl, C 2-10  alkenyl, C 2-10  alkynyl which latter three groups are optionally substituted by one or more substituents selected from halo, nitro, CN, C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 3-6  cycloalkyl (which latter three groups are optionally substituted by one or more substituents selected from OH, \u2550O, halo, C 1-4  alkyl and C 1-4  alkoxy), OR 5aa , S(O) q R 5ab , S(O) 2 N(R 5ac )(R 5ad ), N(R 5ae )S(O) 2 R 5af , N(R 5ag )(R 5ah ), B 12 \u2014C(G 2 )-B 13 \u2014R 5ai , aryl 1  and Het c ; (c) C 3-10  cycloalkyl, or C 4-10  cycloalkenyl (which latter two groups are optionally substituted by one or more substituents selected from halo, OH, \u2550O, C 1-6  alkyl and C 1-6  alkoxy), (d) Het d ; G 2  represents, independently at each occurrence, O, S, or NR 5aj ; R 5aa  to R 5aj  independently represent at each occurrence, (a) H, (b) C 1-4  alkyl, C 1-4  alkenyl, C 2-4  alkynyl which latter three groups are optionally substituted by one or more substituents selected from halo, nitro, CN, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl (which latter three groups are optionally substituted by one or more substituents selected from OH, \u2550O, halo, C 1-4  alkyl and C 1-4  alkoxy), (c) C 3-6  cycloalkyl, or C 4-6  cycloalkenyl (which latter two groups are optionally substituted by one or more substituents selected from halo, OH, \u2550O, C 1-4  alkyl and C 1-4  alkoxy), (d) Het e , or R 5ag  and R 5ah  may represent, together with the nitrogen atom to which they are attached, a 3- to 10-membered heterocyclic ring that may be aromatic, fully saturated or partially unsaturated and which may additionally contain one or more heteroatoms selected from O, S and N, which heterocyclic ring is optionally substituted by one or more substituents selected from halo, nitro, CN, C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl (which latter three groups are optionally substituted by one or more substituents selected from OH, \u2550O, halo, C 1-4  alkyl and C 1-4  alkoxy); B 9  to B 13  independently represent a direct bond, O, S or N(R N8 ); aryl 1  represents, independently at each occurrence, a C 6-10  carbocyclic aromatic group, which group may comprise one or two rings and may be substituted by one or more substituents selected from\n halo, \n C 1-6  alkyl, which latter group is optionally substituted by one or more substituents selected from halo, \u2014N(R N10 )(R N11 ) and C 1-6  alkoxy (which latter substituent is optionally substituted by one or more halo atoms), and \n C 1-6  alkoxy (which latter substituent is optionally substituted by one or more halo atoms); \n R N8 , R N10  and R N11  independently represent\n H, \n C 1-6  alkyl or C 3-6  cycloalkyl, which latter two groups are optionally substituted by one or more halo atoms: \n Het b  represents a 5- or 6-membered that may be aromatic, fully saturated or partially unsaturated and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may be substituted by one or more substituents selected from halo, \u2550O and C 1-6  alkyl; Het c  to Het e  independently represent, a 3- to 6-membered heterocyclic ring that may be aromatic, fully saturated or partially unsaturated and which contains one or more heteroatoms selected from O, S and N, which Het c  to Het e  groups are optionally substituted by one or more substituents selected from halo, nitro, CN, C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl (which latter three groups are optionally substituted by one or more substituents selected from OH, \u2550O, halo, C 1-4  alkyl and C 1-4  alkoxy); q and r independently represent at each occurrence 0, 1 or 2; and unless otherwise specified alkyl, alkenyl, alkynyl, cycloalkyl and the alkyl part of alkoxy groups may be substituted by one or more halo atoms; or a pharmaceutically acceptable salt or solvate, or a pharmaceutically functional derivative thereof, provided that the compound is not: (a) 5-(2-chlorophenyl)-6-(3,4-dimethoxyphenyl)-[1,2,4]triazin-3-ylamine; or (b) 5-(2-chlorophenyl)-6-(3,4,5-trimethoxyphenyl)-[1,2,4]triazin-3-ylamine.

Metadata:
- Claim Count in Document: 65.0
- Percentile: 97.0
- Lexical Diversity: 3.32099
- Patent Class: 544.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14322505', '13576798', '15344048', '15488155', '14112484']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8158215131951911
- 35 USC 102 Novelty (BERT): 0.6432909073353236
- Combined Prediction Score: 0.7985684526092044
- Mean Citation Score: 498.28573399999993
- Max Citation Score: 634.10547
- Similarity Product: 579.7307094541239

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