PATENT CLAIM ANALYSIS

Application Number: 15747220
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2018-08
Patent Classification: ["514", "210200"]

Abstract:
The present invention relates to amide derivatives having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

Claim (Index 17):
A compound of general Formula (I): wherein m is 1 or 2; n is 0, 1 or 2; p is 0, 1 or 2; X is a bond, \u2014C(R x R x\u2032 )\u2014, C\u2550O or \u2014O\u2014;\n wherein R x  is selected from the group consisting of halogen, \u2014OR 8 , substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl and substituted or unsubstituted C 2-6  alkynyl; \n R x\u2032  is selected from the group consisting of hydrogen, halogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl and substituted or unsubstituted C 2-6  alkynyl; \n R 3  is selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl and substituted or unsubstituted C 2-6  alkynyl; \n W is nitrogen or carbon; R 1  is selected from the group consisting of substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl;\n wherein the cycloalkyl, aryl or heterocyclyl in R 1 , if substituted, is substituted with one or more substituent/s selected from the group consisting of halogen, \u2014R 11 , \u2014OR 11 , \u2014NO 2 , \u2014NR 11 C(O)R 11\u2032\u2033 , NR 11 C(O)R 11\u2032 , \u2014NR 11 S(O) 2 R 11\u2032 , \u2014S(O) 2 NR 11 R 11\u2032 , \u2014NR 11 C(O)NR 11\u2032 R 11\u2033 , \u2014SR 11 , \u2014S(O)R 11 , \u2014S(O) 2 R 11 , \u2014CN, haloalkyl, haloalkoxy, \u2014C(O)OR 11 , \u2014C(O)NR 11 R 11\u2032 , \u2014NR 11 S(O) 2 NR 11\u2032 R 11\u2033  and \u2014C(CH 3 ) 2 OR 11 ; \n and wherein the cycloalkyl or non-aromatic heterocyclyl in R 1 , if substituted, may also be substituted with \n \u2003or \u2550O; wherein the alkyl, alkenyl or alkynyl in R 1 , if substituted, is substituted with one or more substituent/s selected from the group consisting of \u2014OR 11 , halogen, \u2014CN, haloalkyl, haloalkoxy, \u2014SR 11 , \u2014S(O)R 11 , and \u2014S(O) 2 R 11 ; wherein R 11 , R 11\u2032  and R 11\u2033  are independently selected from the group consisting of hydrogen, unsubstituted C 1-6  alkyl, unsubstituted C 2-6  alkenyl and unsubstituted C 2-6  alkynyl; and wherein R 11\u2032\u2033  is selected from the group consisting of hydrogen, unsubstituted C 1-6  alkyl, unsubstituted C 2-6  alkenyl, unsubstituted C 2-6  alkynyl and -Boc; R 2  is selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, R 3  is selected from the group consisting of substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, \u2014NR 7 R 7\u2032  and \u2014CH 2 OR 7 ;\n wherein R 7  and R 7 \u2032 are independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; \n R 4  and R 4\u2032  are independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl and substituted or unsubstituted C 2-6  alkynyl, R 5  and R 5\u2032  are independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl and substituted or unsubstituted C 2-6  alkynyl; R 6  and R 6\u2032  are independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl and substituted or unsubstituted C 2-6  alkynyl; and wherein \u2003is selected from the group consisting of wherein R n  is selected from the group consisting of unsubstituted C 1-6  alkyl, unsubstituted C 2-6  alkenyl and unsubstituted C 2-6  alkynyl; wherein the alkyl, alkenyl or alkynyl, other than those defined in R 1  or R 2 , if substituted, is substituted with one or more substituent/s selected from the group consisting of \u2014OR 13 , halogen, \u2014ON, haloalkyl, haloalkoxy, \u2014SR 13 , \u2014S(O)R 13 , and \u2014S(O) 2 R 13 ;\n wherein R 13 , and R 13\u2032  are independently selected from the group consisting of hydrogen, unsubstituted C 1-6  alkyl, unsubstituted C 2-6  alkenyl, and unsubstituted C 2-6  alkynyl; \n optionally as a stereoisomer, including enantiomers and diastereomers, a racemate or a mixture of at least two stereoisomers, including enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

Metadata:
- Claim Count in Document: 74.0
- Percentile: 86.0
- Lexical Diversity: 1.35
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15746877', '15531810', '15571352', '16090403', '15315486']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8620225668411754
- 35 USC 102 Novelty (BERT): 0.5922213456627669
- Combined Prediction Score: 0.8350424447233346
- Mean Citation Score: 484.095566
- Max Citation Score: 527.3969
- Similarity Product: 457.2509032782554

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