PATENT CLAIM ANALYSIS

Application Number: 16135593
Application Type: Utility
Filing Date: 2018-09
Publication Date: 2019-02
Patent Classification: ["548", "240000"]

Abstract:
This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.

Claim (Index 18):
A compound of formula (BB1) or a stereoisomer, enantiomer or tautomer thereof, wherein,\n each dotted line individually represents an optional double bond, wherein maximally two dotted lines selected from the five dotted lines are a double bond; \n E 1  is independently selected from CR 1 ; and N; \n E 2  is independently selected from NR 2 ; and O; \n E 3  is independently selected from CR 3 ; and N; \n R a  is hydrogen or can be taken together with R b  to form a substituted or unsubstituted 4, 5, 6, 7 or 8 membered ring containing one N atom, preferably a piperidine ring; \n R b  is hydrogen or can be taken together with R a  to form a substituted or unsubstituted 4, 5, 6, 7 or 8 membered ring containing one N atom, preferably a piperidine ring; \n Q is independently selected from NR b \u2014C(O); C(O); and C(O)NH; \n each R 1 , R 3 , R 4 , and R 6  is independently selected from hydrogen; halogen; \u2014OH; \u2014OR 10 ; \u2014SH; \u2014SR 10 ; \u2014S(O)R 11 ; \u2014S(O) 2 R 11 ; \u2014SO 2 NR 12 R 13 ; trifluoromethyl; trifluoromethoxy; nitro; \u2014NHC(O)R 10 ; \u2014NHS(O) 2 R 10 ; \u2014NHC(O)NR 12 R 13 ; \u2014NR 10 C(O)R 10 ; \u2014NR 10 S(O) 2 R 10 ; \u2014NR 10 C(O)NR 12 R 13 ; \u2014NR 12 R 13 ; -cyano; \u2014COOH; \u2014COOR 10 ; \u2014C(O)NR 12 R 13 ; \u2014C(O)R 11 ; alkyl; alkenyl; alkynyl; aryl; heterocycle; arylalkylene; arylalkenylene; arylalkynylene; heterocycle-alkylene; heterocycle-alkenylene; heterocycle-alkynylene; \n and wherein said alkyl, alkenyl, alkynyl, aryl, heterocycle, arylalkylene, arylalkenylene, arylalkynylene, heterocycle-alkylene, heterocycle-alkenylene or heterocycle-alkynylene, optionally includes one or more heteroatoms in the alkyl(ene), alkenyl(ene) or alkynyl(ene) moiety, said heteroatoms being selected from the atoms O, S and N; \n and wherein said alkyl, alkenyl, alkynyl, aryl, heterocycle, arylalkylene, arylalkenylene, arylalkynylene, heterocycle-alkylene, heterocycle-alkenylene or heterocycle-alkynylene can be unsubstituted or substituted with Z; \n and wherein a carbon atom or heteroatom of said alkyl, alkenyl, alkynyl, aryl, heterocycle, arylalkylene, arylalkenylene, arylalkynylene, heterocycle-alkylene, heterocycle-alkenylene or heterocycle-alkynylene, can be oxidized to form a C\u2550O, C\u2550S, N\u2550O, N\u2550S, S\u2550O or S(O) 2 ; \n R 5  is selected from halogen; \u2014OH; \u2014SH; \u2014SR 10 ; \u2014S(O)R 11 ; \u2014S(O) 2 R 11 ; \u2014SO 2 NR 12 R 13 ; trifluoromethyl; trifluoromethoxy; nitro; \u2014NHC(O)R 10 ; \u2014NHS(O) 2 R 10 ; \u2014NHC(O)NR 12 R 13 ; \u2014NR 10 C(O)R 10 ; \u2014NR 10 S(O) 2 R 10 ; \u2014NR 10 C(O)NR 12 R 13 ; \u2014NR 12 R 13 ; -cyano; \u2014COOH; \u2014COOR 10 ; \u2014C(O)NR 12 R 13 ; \u2014C(O)R 11 ; alkyl; alkenyl; alkynyl; aryl; heterocycle; arylalkylene; arylalkenylene; arylalkynylene; heterocycle-alkylene; heterocycle-alkenylene; heterocycle-alkynylene; \n and wherein said alkyl, alkenyl, alkynyl, aryl, heterocycle, arylalkylene, arylalkenylene, arylalkynylene, heterocycle-alkylene, heterocycle-alkenylene or heterocycle-alkynylene, optionally includes one or more heteroatoms in the alkyl(ene), alkenyl(ene) or alkynyl(ene) moiety, said heteroatoms being selected from the atoms O, S and N; \n and wherein said alkyl, alkenyl, alkynyl, aryl, heterocycle, arylalkylene, arylalkenylene, arylalkynylene, heterocycle-alkylene, heterocycle-alkenylene or heterocycle-alkynylene can be unsubstituted or substituted with Z; \n and wherein a carbon atom or heteroatom of said alkyl, alkenyl, alkynyl, aryl, heterocycle, arylalkylene, arylalkenylene, arylalkynylene, heterocycle-alkylene, heterocycle-alkenylene or heterocycle-alkynylene, can be oxidized to form a C\u2550O, C\u2550S, N\u2550O, N\u2550S, S\u2550O or S(O) 2 ;- \n R 2  is selected from hydrogen; alkyl; alkenyl; and alkynyl; \n n is selected from 0; 1 or 2; \n each of X, Y, T, W and V is independently selected from \u2014CZ 1 H\u2014; \u2014CZ 1 \u2014; \u2014C\u2014; \u2014N\u2014; NR 101 ; \u2014O\u2014; \u2014S\u2014; or \u2014CO\u2014; wherein at least one of X, Y, T; W or V is selected from \u2014CZ 1 H\u2014 or \u2014CZ 1 \u2014 or \u2014Cl\u2014; \n L is independently selected from being not present; \u2014O\u2014; \u2014NH\u2014; \u2014NR 10 \u2014; C 1-6 alkylene; C 1-6 alkenylene; C 1-6 alkynylene; \n wherein each of said C 1-6 alkylene, C 1-6 alkenylene or C 1-6 alkynylene optionally includes one or more heteroatoms, said heteroatoms being selected from the heteroatoms consisting of O, S and N, and wherein each of said C 1-6 alkylene, C 1-6 alkenylene or C 1-6 alkynylene, can be unsubstituted or substituted; \n and wherein a carbon atom or heteroatom of said C 1-6 alkylene, C 1-6 alkenylene or C 1-6 alkynylene, can be oxidized to form a C\u2550S, N\u2550O, N\u2550S, S\u2550O or S(O) 2 ; \n B represents a cyclic structure selected from cycloalkyl; cycloalkenyl; cycloalkynyl; aryl; and heterocycle; \n m is selected from 0; 1; 2; 3; 4 and 5; \n R 8  is independently selected from hydrogen; halogen; alkyl; alkenyl; alkynyl; \u2014OH; \u2014OR 10 ; \u2014SH; \u2014SR 10 ; \u2014S(O)R 11 ; \u2014S(O) 2 R 11 ; \u2014SO 2 NR 12 R 13 ; trifluoromethyl; trifluoromethoxy; nitro; \u2014NHC(O)R 10 ; \u2014NHS(O) 2 R 10 ; \u2014NHC(O)NR 12 R 13 ; \u2014NR 10 C(O)R 10 ; \u2014NR 10 S(O) 2 R 10 ; \u2014NR 10 C(O)NR 12 R 13 ; \u2014NR 12 R 13 ; -cyano; \u2014COOH; \u2014COOR 10 ; \u2014C(O)NR 12 R 13 ; \u2014C(O)R 11 ; \n wherein said alkyl, alkenyl and alkynyl optionally includes one or more heteroatoms, said heteroatoms being selected from the atoms O, S and N; \n and wherein said alkyl, alkenyl and alkynyl can be unsubstituted or substituted with Z; \n and wherein a carbon atom or heteroatom of said alkyl, alkenyl and alkynyl, can be oxidized to form a C\u2550O, C\u2550S, N\u2550O, N\u2550S, S\u2550O or S(O) 2 ; \n each Z is independently selected from halogen; \u2014OH; \u2014OR 10 ; \u2014SH; \u2014SR 10 ; \u2014S(O)R 11 ; \u2014S(O) 2 R 11 ; \u2014SO 2 NR 13 ; trifluoromethoxy; nitro; \u2014NHC(O)R 10 ; \u2014NHS(O) 2 R 10 ; \u2014NHC(O)NR 12 R 13 ; \u2014NR 10 C(O)R 10 ; \u2014NR 10 S(O) 2 R 10 ; \u2014NR 10 C(O)NR 12 R 13 ; \u2014NR 12 R 13 ; -cyano; \u2014COOH; \u2014COOR 10 ; \u2014C(O)NR 12 R 13 ; \u2014C(O)R 11 ; \n each Z 1  is independently selected from hydrogen; alkyl; and Z; \n each R 10  is independently selected from alkyl; alkenyl; alkynyl; aryl; heterocycle; \n arylalkylene; arylalkenylene; arylalkynylene; heterocycle-alkylene; heterocycle-alkenylene or heterocycle-alkynylene; \n and wherein said alkyl, alkenyl, alkynyl, aryl, heterocycle, arylalkylene, arylalkenylene, arylalkynylene, heterocycle-alkylene, heterocycle-alkenylene or heterocycle-alkynylene optionally include one or more heteroatoms in the alkyl(ene), alkenyl(ene) or alkynyl(ene) moiety, said heteroatom selected from O, S and N; \n and wherein a carbon atom or heteroatom of said alkyl, alkenyl, alkynyl, aryl, heterocycle, arylalkylene, arylalkenylene, arylalkynylene, heterocycle-alkylene, heterocycle-alkenylene or heterocycle-alkynylene, can be oxidized to form a C\u2550O, C\u2550S, N\u2550O, N\u2550S, S\u2550O or S(O) 2 ; \n each R 101  is independently selected from hydrogen and R 10 ; \n each R 11  is independently selected from hydroxyl; alkyl; alkenyl; alkynyl; aryl; heterocycle; arylalkylene; arylalkenylene; arylalkynylene; heterocycle-alkylene; heterocycle-alkenylene or heterocycle-alkynylene; \n and wherein said alkyl, alkenyl, alkynyl, aryl, heterocycle, arylalkylene, arylalkenylene, arylalkynylene, heterocycle-alkylene, heterocycle-alkenylene or heterocycle-alkynylene optionally include one or more heteroatoms in the alkyl(ene), alkenyl(ene) or alkynyl(ene) moiety, said heteroatom selected from O, S and N; \n and wherein a carbon atom or heteroatom of said alkyl, alkenyl, alkynyl, aryl, heterocycle, arylalkylene, arylalkenylene, arylalkynylene, heterocycle-alkylene, heterocycle-alkenylene or heterocycle-alkynylene, can be oxidized to form a C\u2550O, C\u2550S, N\u2550O, N\u2550S, S\u2550O or S(O) 2 ; \n each R 12  and R 13  is independently selected from hydrogen; alkyl; alkenyl; alkynyl; aryl; heterocycle; arylalkylene; arylalkenylene; arylalkynylene; heterocycle-alkylene; heterocycle-alkenylene or heterocycle-alkynylene; \n and wherein said alkyl, alkenyl, alkynyl, aryl, heterocycle, arylalkylene, arylalkenylene, arylalkynylene, heterocycle-alkylene, heterocycle-alkenylene or heterocycle-alkynylene optionally include one or more heteroatoms in the alkyl(ene), alkenyl(ene) or alkynyl(ene) moiety, said heteroatom selected from O, S and N; \n and wherein a carbon atom or heteroatom of said alkyl, alkenyl, alkynyl, aryl, heterocycle, arylalkylene, arylalkenylene, arylalkynylene, heterocycle-alkylene, heterocycle-alkenylene or heterocycle-alkynylene, can be oxidized to form a C\u2550O, C\u2550S, N\u2550O, N\u2550S, S\u2550O or S(O) 2 ; \n and wherein R 12  and R 13  can be taken together in order to form a (5-, 6-, or 7-membered) heterocycle which can be unsubstituted or substituted; \n and stereoisomers, enantiomers or tautomers, solvates, hydrates, or salts (in particular pharmaceutically acceptable salts) thereof.

Metadata:
- Claim Count in Document: 11.0
- Percentile: 97.0
- Lexical Diversity: 1.88235
- Patent Class: 548.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['14060563', '15215750', '13993723', '13993756', '13377505']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8892245226981147
- 35 USC 102 Novelty (BERT): 0.6719183740854284
- Combined Prediction Score: 0.8674939078368461
- Mean Citation Score: 683.32623
- Max Citation Score: 725.93085
- Similarity Product: 655.9897820739805

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