PATENT CLAIM ANALYSIS

Application Number: 15962814
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-08
Patent Classification: ["514", "359000"]

Abstract:
The invention relates to compounds which are mGlu2/3 negative allosteric modulators for use in the treatment of intellectual disabilities. In another aspect, the invention relates to a pharmaceutical composition for use in the treatment of intellectual disabilities comprising a compound according to the invention and a pharmaceutically acceptable carrier.

Claim (Index 1):
A mGlu2/3 negative allosteric modulator selected from a compound of formula (I) and formula (II): wherein either E and J are N, G is C and one of L or M is N and the other is CH; or L and G are N, E is C, and J and M are CH; or J, G and L are N, E is C and M is CH; or E and L are N, J and M are CH and G is C; A is selected from the group consisting of phenyl, pyridin-2-yl, pyridin-3-yl, pyridine-4-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyridazin-2-yl, pyridazin-3-yl, thiazol-2-yl, thiazol-5-yl, and thiophen-2-yl which are optionally substituted by one to four R a ; B is selected from the group consisting of imidazolyl, [1,2,4]oxadiazolyl], pyrrolyl, 1H-pyrazolyl, pyridinyl, [1,2,4]triazolyl, thiazolyl, pyrimidinyl and thiophenyl, each of which is optionally substituted by C 1-6 -alkyl; C is an optionally substituted aryl or an optionally substituted 5 or 6 membered heteroaryl, wherein the substituents are selected from the group consisting of: xii. halo, xiii. nitro, xiv. C 1-6 -alkyl optionally substituted by hydroxy, xv. NR aa R bb , wherein R aa  and R bb  independently H, C 1-6 -alkyl or \u2014(CO)\u2014C 1-6 -alkyl, xvi. \u2014S\u2014C 1-6 -alkyl, xvii. \u2014(SO 2 )\u2014OH, xviii. \u2014(SO 2 )\u2014C 1-6 -alkyl, xix. \u2014(SO 2 )\u2014NR cc R dd , wherein R cc  and R dd  are independently: j. H, k. C 1-6 -alkyl optionally substituted by hydroxy, l. C 1-6 -haloalkyl, m. C 1-6 -alkoxy, n. \u2014(CO)C 1-6 -alkyl optionally substituted by C 1-6 -alkoxy, o. \u2014(CH 2 CH 2 O) n CHR ee , wherein R ee  is H or CH 2 OH and n is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10,  p . \u2014(CH 2 ) m -aryl, wherein m is 1 or 2 and the aryl is optionally substituted by halo or C 1-6 -alkoxy, q. \u2014(CH 2 ) p \u2014C 3-6 -cycloalkyl, wherein p is 0 or 1, r. 5 or 6-membered heterocycloalkyl, xx. \u2014(SO 2 )\u2014N ff R gg , wherein R ff  and R gg  together with the nitrogen atom to which they are attached form a 4, 5 or 6 membered heterocycloalkyl ring optionally containing a further heteroatom selected from nitrogen, oxygen, sulphur or a SO 2  group, wherein said 4, 5 or 6 membered heterocycloalkyl ring is optionally substituted by:a substituent selected from the group consisting of hydroxy, C 1-6 -alkyl, C 1-6 -alkoxy which is optionally substituted by hydroxy, and 5 or 6 membered heteroaryloxy, xxi. NHSO 2 \u2014C 1-6 -alkyl, and xxii. NHSO 2 -NR hh R ii  wherein R hh  and R ii  are independently H, C 1-6 -alkyl, \u2014(CO)O\u2014C 1-6 -alkyl, or R hh  and R ii  together with the nitrogen atom to which they are attached form a 4, 5 or 6 membered heterocycloalkyl ring optionally containing a further heteroatom selected from nitrogen, oxygen or sulphur, wherein said 4, 5 or 6 membered heterocycloalkyl ring is optionally substituted by C 1-6 -alkyl; R 1  is H, halo, CF 3 , CHF 2 , or C 1-6 -alkyl; R 2  is H, halo, C 1-6 -alkyl, C 1-6 -alkoxy, CF 3  or CHF 2 ; R 3  is H, \u2014C(CH 3 ) 2 OH; linear C 1-4 -alkyl or C 3-4 -cycloalkyl, which are optionally substituted by one or more substituents selected from the group consisting of 1 to 6 F and 1 to 2 OH; R 4  is H, halogen, C 1-6 -alkyl optionally substituted by hydroxy, C 1-6 -alkoxy, haloalkyl, C 3-6 -cycloalkyl; R 5  is H, cyano, halogen, C 1-6 -haloalkyl, C 1-6 -alkoxy, C 1-6 -haloalkoxy, C 1-6 -alkyl or C 3-6 -cycloalkyl; R 6  is halogen, H, C 1-6 -alkoxy, C 1-6 -haloalkyl, C 1-6 -alkyl, C 3-6 -cycloalkyl, C 1-6 -haloalkoxy, or is NR jj R kk  wherein R jj  and R kk  are independently selected from the group consisting of: H, C 3-8 -cycloalkyl, aryl, heteroaryl having from 5 to 12 ring atoms and C 1-6 -alkyl which optionally substituted by one or more substituent(s) selected from the group consisting of halogen, hydroxy, C 3-8 -cycloalkyl, aryl, heteroaryl having from 5 to 12 ring atoms and \u2014NR ll R mm , wherein R ll  and R mm  are independently selected from the group consisting of H and C 1-6 -alkyl; or R jj  and R kk  can, together with the nitrogen atom to which they are attached, form an optionally substituted heterocyclic group comprising 5 to 12 ring atoms optionally containing a further heteroatom selected from nitrogen, oxygen or sulphur, wherein said heteroaryl group is optionally substituted by one, two, three, four or five substituents are selected from the group consisting of halogen, hydroxy, C 1-6 -alkyl and C 1-6 -haloalkyl; or R 5  and R 6  can together form a dioxo bridge; R 7  is H or halo; R a  is halo; hydroxy; cyano; CF 3 ; NR e R f ; C 1-6 -alkyl optionally substituted by amino or by hydroxy; C 1-6 -alkoxy; C 3-4 -cycloalkyl; CO\u2014R b R c , SO 2 \u2014NR b R c ; or SO 2 \u2014R d ; R b  and R c  may be the same or different and are selected from the group consisting of: vii. H; viii. straight or branched C 1-6 -alkyl optionally substituted by one or more substituents selected from the group consisting of: ix. F, cyano, hydroxy, C 1-6 -alkoxy, \u2014NH\u2014C(O)\u2014O\u2014C 1-6 -alkyl, amino, (C 1-6 -alkyl)amino, di(C 1-6 -alkyl)amino, C 3-6 -cycloalkyl, heterocycloalkyl having 5 or 6 ring atoms, aryl or 5 or 6-membered heteroaryl; x. C 3-6 -cycloalkyl; xi. aryl; or xii. heteroaryl; or R b  and R c  may, together with the nitrogen atom to which they are attached, form an heterocyclic ring of 4 to 6 ring members which may be substituted by hydroxy or by C 1-6 -alkyl; R d  is OH or C 1-6 -alkyl; R e  and R f  are H, C 1-6 -alkyl optionally substituted by hydroxy, \u2014C(O)\u2014C 1-6 -alkyl; S(O) 2 \u2014C 1-6 -alkyl; or a pharmaceutically acceptable salt thereof.

Metadata:
- Claim Count in Document: 9.0
- Percentile: 91.0
- Lexical Diversity: 1.52941
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['12053648', '13178531', '12551625', '11726575', '12394083']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7214171136854917
- 35 USC 102 Novelty (BERT): 0.5153410441365915
- Combined Prediction Score: 0.7008095067306016
- Mean Citation Score: 237.48939600000003
- Max Citation Score: 243.01498
- Similarity Product: 149.72348785033466

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