PATENT CLAIM ANALYSIS

Application Number: 16098244
Application Type: Utility
Filing Date: 2018-11
Publication Date: 2019-05
Patent Classification: ["514", "218000"]

Abstract:
The present invention relates to new compounds of general formula (I) that show great affinity and activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially α2δ-1 subunit of voltage-gated calcium channels or dual activity towards subunit α2δ of voltage-gated calcium channels (VGCC), especially α2δ-1 subunit of voltage-gated calcium channels, and noradrenaline transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.

Claim (Index 18):
A compound of general formula (I): wherein: X is CRx or N; Rx is a hydrogen atom; a branched or unbranched C 1-6  alkyl radical; or a halogen atom; Y is CH 2  or C\u2550O; m is 0, 1 or 2; R 1  is a hydrogen atom; or a linear or branched C 1-6  alkyl radical; R 2  is a hydrogen atom; a branched or unbranched C 1-6  alkyl radical; a halogen atom; haloalkyl; \u2014SR 2a ; \u2014NR 2a R 2b ; or \u2014OR 2a ; R 2a  and R 2b  independently represent a hydrogen atom; a branched or unbranched C 1-4  alkyl radical; a C 3-6  cycloalkyl radical; \u2014(CH 2 ) r -aryl, wherein the aryl group is 5 or 6-membered ring and r is 0, 1 or 2; \u2014(CH 2 ) s -heteroaryl, wherein the heteroaryl group is 5 or 6-membered ring having at least one nitrogen atom optionally substituted by at least one halogen atom and s is 0, 1 or 2; or \u2014(CH 2 ) 2 \u2014O\u2014CH 3 ; R 3  is a hydrogen atom; \u2014CN; \u2014OH; halogen; branched or unbranched C 1-6  alkyl radical; \u2014(CH 2 ) p \u2014O\u2014R 4 , wherein p is 0, 1 or 2; \u2014(CH 2 ) q \u2014NR 5 R 6 , wherein q is 0, 1, 2 or 3; \u2014C(CH 3 ) 2 \u2014CH 2 \u2014NR 5 R 6 ; \u2014C(\u2550O)NR 5 R 6 ; a 5 or 6 membered heteroaryl group having at least one heteroatom selected from N, O or S, and being substituted by one or two R 7  substituents and which may be attached to the phenyl ring by a C 1-3  alkylene group; a 5 or 6 membered heterocycoalkyl radical having one or two nitrogen atoms and being unsubstituted or optionally substituted by one or two R 5  substituents and which may be attached to the phenyl ring by a C 1-3  alkylene group; or \u2014C(\u2550O)OR 9 ; R 4  is a hydrogen atom; a branched or unbranched C 1-6  alkyl radical; a tert-butyldimethylsilyl radical; a methylbenzenesulfonate radical; a \u2014CHR 4a R 4b ; a \u2014CH 2 \u2014CHR 4a R 4b ; or a 5 or 6-membered heterocycloalkyl radical having at least one N atom and being optionally substituted by one or two R 4c  radical; R 4a  is a hydrogen atom; a branched or unbranched C 1-6  alkyl radical; a 5 or 6-membered aryl group optionally substituted by a at least one halogen atom; or a 5 or 6-membered heteroaryl group, having at least one heteroatom selected from N, O or S, and being optionally substituted by at least a branched or unbranched C 1-6  alkyl radical; R 4b  is a \u2014(CH 2 ) j \u2014NR 4b\u2032 R 4b\u2033 , wherein j is 0, 1, 2 or 3; R 4b\u2032  and R 4b\u2033  independently represent a hydrogen atom; a branched or unbranched C 1-6  alkyl radical; a C 1-6  haloalkyl radical; a benzyl group; a phenethyl group; a tert-butyloxycarbonyl group; or a (trimethylsilyl)ethyloxycarbonyl group; or R 4b\u2032  and R 4b\u2033 , together with the nitrogen to which they are attached, form a 5 or 6-membered heterocycloalkyl radical optionally containing an additional heteroatom selected from N, O and S; R 4c  is a hydrogen atom; a branched or unbranched C 1-6  alkyl radical; a phenyl group; a benzyl group; or a tert-butyloxycarbonyl group; R 5  and R 6  independently represent a hydrogen atom; a branched or unbranched C 1-6  alkyl radical; a tert-butyloxycarbonyl group; a benzyl group; a phenethyl group; or R 5  and R 6 , together with the nitrogen to which they are attached, form a 5 or 6-membered heterocycloalkyl radical which may be mono or bisubstituted by a phenyl group, which may be optionally substituted by a branched or unbranched C 1-6  alkyl radical, a halogen atom, \u2014OH or \u2014CN; or by an \u2014NRR\u2032, wherein R and R\u2032 independently represent a hydrogen atom or a branched or unbranched C 1-6  alkyl radical; or R 5  and R 6 , together with the nitrogen atom to which they are attached, form 5 or 6-membered heterocycloalkyl radical which may be spirofused to another 5 or 6-membered heterocycloalkyl radical having at least one heteroatom selected from N, O and S, which may be substituted by one or more substituents selected from a branched or unbranched C 1-6  alkyl radical; a halogen atom, an \u2014OH, a \u2014CN and an \u2550O; R 7  is a hydrogen atom; a branched or unbranched C 1-6  alkyl radical; a \u2014C(\u2550O)H group; a \u2014(CH 2 ) p \u2014NR 7a R 7b , wherein p is 0, 1, 2 or 3; or a \u2014(CH)R 7c R 7d ; R 7a  and R 7b  independently represent a hydrogen atom; a branched or unbranched C 1-6  alkyl radical; a tert-butyloxycarbonyl group; a benzyl group optionally substituted by a halogen; a phenethyl group; a \u2014(CH 2 )-cyclopropyl; a hydroxyethoxyethyl group; an \u2014OH; a \u2014C(\u2550O)H group; a pyridinylmethyl group; or R 7a  and R 7b , together with the nitrogen to which they are attached, form a 5 or 6-membered heterocycloalkyl radical which may additionally contain a second N atom, which radical may be substituted by a \u2014NR 7a\u2032 R 7b\u2032 , wherein R 7a\u2032  and R 7b\u2032  independently represent a hydrogen atom or a branched or unbranched C 1-6  alkyl radical; or by a phenyl group, which may be optionally substituted by a branched or unbranched C 1-6  alkyl radical, a halogen atom, an \u2014OH or a \u2014CN; or R 7a  and R 7b , together with the nitrogen atom to which they are attached, form 5 or 6-membered heterocycloalkyl radical which may be fused to a 5 or 6 membered aromatic ring or may be spirofused to either a single 5 or 6-membered heterocycloalkyl ring having at least one heteroatom selected from N, O and S, which may be substituted by one or more substituents selected from a branched or unbranched C 1-6  alkyl radical, a halogen atom, an \u2014OH, a \u2014CN or an \u2550O; or may be spirofused to a bicyclic ring system formed by a 5 or 6-membered heterocycloalkyl ring having at least one heteroatom selected from N, O and S fused to 5 or 6-membered aromatic ring; R 7c  and R 7d  independently represent a hydrogen atom; a branched or unbranched C 1-6  alkyl radical; or C 1-6  alkoxy radical; and R 8  is a hydrogen atom; a branched or unbranched C 1-6  alkyl radical; a tert-butyloxycarbonyl group; a phenyl group; a benzyl group; a phenethyl group; or a \u2014NR8 a\u2032 R 8b\u2032 , wherein R 8a\u2032  and R 8b\u2032  represent a hydrogen atom or a branched or unbranched C 1-6  alkyl radical; and R 9  is a hydrogen atom; or a linear or branched C 1-6  alkyl radical; or a pharmaceutically acceptable salt, isomer, prodrug or solvate thereof.

Metadata:
- Claim Count in Document: 44.0
- Percentile: 98.0
- Lexical Diversity: 1.88235
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['14820711', '12680353', '12485108', '13910349', '11828457']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7928714797755207
- 35 USC 102 Novelty (BERT): 0.5392714018182777
- Combined Prediction Score: 0.7675114719797964
- Mean Citation Score: 342.51614000000006
- Max Citation Score: 362.67856
- Similarity Product: 256.0035809882927

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