PATENT CLAIM ANALYSIS

Application Number: 15767775
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2019-02
Patent Classification: ["548", "466000"]

Abstract:
The invention provides a compound of formula (0): or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and C—F; Z is selected from C—R z  and N; R 1  is selected from:     -(Alk 1 ) t -Cyc 1 ; wherein t is 0 or 1; Optionally substituted C 1-6  acyclic hydrocarbon groups       R 2  is selected from hydrogen; halogen; and C 1-3  hydrocarbon groups optionally substituted with one or more fluorine atoms; R 3  is hydrogen or a group L 1 -R 7 ; R 4  is selected from hydrogen; methoxy; and optionally substituted C 1-3  alkyl; and R 4a  is selected from hydrogen and a C 1-3  alkyl group; wherein R z , Alk 1 , Cyc 1 , L 1  and R 7  are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof. The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.

Claim (Index 3):
A compound of formula (1); or a pharmaceutically acceptable salt or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and C\u2014F; Z is selected from C\u2014R z  and N; R z  is selected from hydrogen; halogen; and C 1-3  alkyl optionally substituted with hydroxy or methoxy; R 1  is selected from:\n -(Alk 1 ) t -Cyc 1 ; wherein t is 0 or 1; and Alk 1  is a C 1-4  straight chain or branched alkylene group optionally substituted with 1 or 2 hydroxy groups; and \n C 1-6  acyclic hydrocarbon groups which are unsubstituted or substituted with 1, 2 or 3 substituents R 5  selected from hydroxy; oxo; fluorine; and wherein 1 or 2 but not all of the carbon atoms of the hydrocarbon group can be replaced by O or N; \n Cyc 1  is a cyclic group selected from (a) 3 to 9 membered non-aromatic monocyclic and bicyclic carbocyclic and heterocyclic groups containing 0, 1, 2, or 3 heteroatom ring members selected from O, N, S and S(O) 2 ; (b) 5 to 6 membered monocyclic heteroaryl groups containing 1, 2 or 3 heteroatom ring members of which 1 is N and the others, when present, are selected from O, N and S; and (c) 3 to 7 membered monocyclic carbocyclic groups; wherein each cyclic group (a), (b) and (c) is unsubstituted or substituted with 1, 2 or 3 substituents R 6  selected from hydroxy; oxo; fluorine; amino; mono- or di-C 1-4  alkylamino; O-Hyd 1 ; \u2014C(\u2550O)\u2014Hyd 1 ; \u2014C(\u2550O)\u2014O\u2014Hyd 1  and Hyd 1 ; where Hyd 1  is a C 1-4  non-aromatic hydrocarbon group optionally substituted with one or more substituents selected from fluorine, hydroxyl and methoxy; R 2  is selected from hydrogen; halogen; and C 1-3  hydrocarbon groups optionally substituted with one or more fluorine atoms; R 3  is hydrogen or a group L 1 -R 7 ; R 4  is selected from hydrogen and C 1-2  alkyl optionally substituted with hydroxy, amino, mono- or di-C 1-2  alkylamino, a cyclic amino group or methoxy; wherein the cyclic amino group is a saturated 4-7 membered heterocyclic group containing a nitrogen ring member and optionally a second heteroatom ring member selected from O, N and S, wherein the cyclic amino group is linked via a nitrogen ring member thereof to the C 1-2  alkyl, and wherein the cyclic amino group is optionally substituted with one or two methyl groups; provided that no more than one R 4  can be other than hydrogen or methyl; L 1  is selected from a bond; Alk 2 , Alk 2 -O and Alk 2 -C(\u2550O) wherein Alk 2  is a C 1-4  straight chain or branched alkylene group which is optionally substituted with one or more substituents selected from hydroxy, methoxy, amino, methylamino, dimethylamino and fluorine; R 7  is selected from:\n hydrogen; \n CO 2 H; \n NR 8 R 9 ; \n a carbocyclic or heterocyclic group having from 3 to 12 ring members, of which 0, 1, 2 or 3 are heteroatom ring members selected from O, N and S and oxidised forms of S, the carbocyclic or heterocyclic group being optionally substituted with one or more substituents R 10 ; and \n an acyclic C 1-8  hydrocarbon group optionally substituted with one or more substituents selected from hydroxy; oxo; halogen; cyano; carboxy; amino; mono- or di-C 1-4  alkylamino; and carbocyclic and heterocyclic groups having from 3 to 12 ring members, of which 0, 1, 2 or 3 are heteroatom ring members selected from O, N and S and oxidised forms of S, the carbocyclic or heterocyclic group being optionally substituted with one or more substituents R 10 ; wherein one or two but not all of the carbon atoms of the acyclic C 1-8  hydrocarbon group may optionally be replaced by O, S, SO, SO 2  or NR 11 ; \n R 8  is selected from hydrogen and a C 1-4  hydrocarbon group optionally substituted with hydroxy; amino or mono- or di-C 1-4  alkylamino R 9  is selected from:\n hydrogen; \n a carbocyclic or heterocyclic group having from 3 to 12 ring members, of which 0, 1, 2 or 3 are heteroatom ring members selected from O, N and S and oxidised forms of S, the carbocyclic or heterocyclic group being optionally substituted with one or more substituents R 10 ; and \n an acyclic C 1-8  hydrocarbon group optionally substituted with one or more substituents selected from hydroxy; oxo; halogen; cyano; carboxy; amino; mono- or di-C 1-4  alkylamino; and carbocyclic and heterocyclic groups having from 3 to 12 ring members, of which 0, 1, 2 or 3 are heteroatom ring members selected from O, N and S and oxidised forms of S, the carbocyclic or heterocyclic group being optionally substituted with one or more substituents R 10 ; wherein one or two but not all of the carbon atoms of the acyclic C 1-8  hydrocarbon group may optionally be replaced by O, S, SO, SO 2  or NR 11 ; \n or NR 8 R 9  forms a heterocyclic group having from 4 to 12 ring members wherein, in addition to the nitrogen atom of NR 8 R 9 , the heterocyclic group optionally contains 1 or 2 further heteroatom ring members selected from O, N and S and oxidised forms of S; and wherein the heterocyclic group is optionally substituted with one or more substituents R 10 ; R 10  is selected from:\n halogen; hydroxy; oxo; cyano; \n OR 12  wherein R 12  is C 1-6  alkyl or C 3-6  cycloalkyl, each being optionally substituted with halogen; \n an acyclic C 1-8  hydrocarbon group optionally substituted with one or more substituents selected from hydroxy; oxo; halogen; cyano; carboxy; amino; mono- or di-C 1-4  alkylamino; and carbocyclic and heterocyclic groups having 3 to 6 ring members of which 0, 1 or 2 are heteroatom ring members selected from N, O and S, wherein the carbocyclic and heterocyclic groups are optionally substituted with one or more substituents R 13  selected from hydroxy; halogen; cyano; and \u2014(O) v -Hyd 1  where v is 0 or 1; wherein one or two but not all of the carbon atoms of the acyclic C 1-8  hydrocarbon group may optionally be replaced by O, S, SO, SO 2  or NR 11 ; and \n carbocyclic and heterocyclic groups having 3 to 6 ring members of which 0, 1, 2, 3 or 4 are heteroatom ring members selected from N, O and S, wherein the carbocyclic and heterocyclic groups are optionally substituted with one or more substituents R 13 ; and \n R 11  is selected from hydrogen and a C 1-4  hydrocarbon group; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof.

Metadata:
- Claim Count in Document: 5.0
- Percentile: 91.0
- Lexical Diversity: 2.32075
- Patent Class: 548.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['14358678', '15764960', '14529902', '12298462', '15118072']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7656543680982042
- 35 USC 102 Novelty (BERT): 0.5552000891731401
- Combined Prediction Score: 0.7446089402056978
- Mean Citation Score: 389.51534
- Max Citation Score: 417.22003
- Similarity Product: 329.5417863646257

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