PATENT CLAIM ANALYSIS

Application Number: 15769223
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-10
Patent Classification: ["514", "282000"]

Abstract:
The purpose of the present invention is to provide a compound useful as a prophylactic or therapeutic agent for various diseases and symptoms related to orexin receptors, and a medical usage of the same. The present invention provides a morphinan derivative represented by the general formula (I) below or a pharmaceutically acceptable acid addition salt thereof, the morphinan derivative having excellent selectivity for and antagonism against orexin receptors and excellent therapeutic and prophylactic effects on drug dependence, and an orexin receptor antagonist and a therapeutic or prophylactic agent for drug dependence each containing it as an active ingredient.

Claim (Index 11):
A morphinan derivative represented by the general formula (I) below or a pharmaceutically acceptable acid addition salt thereof for use in treatment or prevention of drug dependence [wherein L 1 -L 2 -L 3  represents C(R 9 )\u2014CH 2 \u2014CH 2 , C(R 9 )\u2014CH\u2550CH, or C\u2550CH\u2014CH 2 , wherein R 9  represents a hydrogen atom, hydroxy, nitro, C 1 -C 5  alkanoyloxy, C 1 -C 5  alkoxy, C 1 -C 5  alkyl, amino, monoalkylamino (the alkyl moiety has one to five carbon atoms), dialkylamino (the alkyl moiety has one to five carbon atoms), C 1 -C 5  alkanamide, benzamide, or C 7 -C 14  aryl-alkanamide;\n A represents \u2014C(\u2550O)\u2014 or \u2014SO 2 \u2014; \n R 1  represents C 1 -C 7  linear or branched alkyl, C 3 -C 6  cycloalkyl, C 4 -C 7  cycloalkylalkyl, C 4 -C 6  cycloalkenyl, C 5 -C 7  cycloalkenylalkyl, C 7 -C 13  aralkyl, C 4 -C 7  alkenyl, allyl, or an organic group containing any of basic skeletons (II) below, wherein, in the basic skeletons (II), Q represents N, O, or S; T represents CH 2 , NH, S, or O; l represents an integer of 0 to 5; m and n each independently represent an integer of 0 to 5, provided that the sum of m and n is not more than 5; said organic group represented by R 1  is optionally substituted by at least one substituent selected from the group consisting of C 1 -C 5  alkyl, C 1 -C 5  alkoxy, C 1 -C 5  alkanoyloxy, hydroxy, fluorine, chlorine, bromine, iodine, amino, monoalkylamino (the alkyl moiety has one to five carbon atoms), dialkylamino (the alkyl moiety has one to five carbon atoms), nitro, cyano, carboxy, carbamoyl, N,N-dialkylcarbamoyl (the alkyl moiety has one to five carbon atoms), amidino, guanidino, isothiocyanate, trifluoromethyl, phenyl, trifluoromethoxy, and methylenedioxy; \n both R 2  and R 3  represent a hydrogen atom, or one of R 2  and R 3  represents a hydrogen atom and the other represents hydroxy, or R 2  and R 3  together represent oxo; R 4  represents a hydrogen atom, hydroxy, C 1 -C 5  alkoxy, C 3 -C 7  alkenyloxy, C 7 -C 13  aralkyloxy, or C 1 -C 5  alkanoyloxy; R 5  and R 6  together represent \u2014O\u2014, \u2014S\u2014, or \u2014CH 2 \u2014, or R 6  represents a hydrogen atom and R 5  represents a hydrogen atom, hydroxy, C 1 -C 5  alkoxy, or C 1 -C 5  alkanoyloxy; R 7  represents a hydrogen atom, C 1 -C 5  alkyl, C 2 -C 5  alkenyl, or C 7 -C 13  aralkyl; B 1  represents \u2014N(R 10 )C(\u2550O)\u2014 or \u2014NR 10 \u2014, wherein R 10  represents a hydrogen atom, C 1 -C 5  linear or branched alkyl; B 2  represents a valence bond, C 1 -C 14  linear or branched alkylene (provided that said alkylene is optionally substituted with at least one substituent selected from the group consisting of C 1 -C 5  alkoxy, C 1 -C 5  alkanoyloxy, hydroxy, fluorine, chlorine, bromine, iodine, amino, monoalkylamino (the alkyl moiety has one to five carbon atoms), dialkylamino (the alkyl moiety has one to five carbon atoms), nitro, cyano, carboxy, carbamoyl, amidino, guanidino, trifluoromethyl, phenyl and phenoxy; and one to three methylene groups are optionally replaced with carbonyl groups), C 2 -C 14  linear or branched acyclic unsaturated divalent hydrocarbon group containing one to three double and/or triple bonds (provided that said hydrocarbon group is optionally substituted with at least one substituent selected from the group consisting of C 1 -C 5  alkoxy, C 1 -C 5  alkanoyloxy, hydroxy, fluorine, chlorine, bromine, iodine, amino, monoalkylamino (the alkyl moiety has one to five carbon atoms), dialkylamino (the alkyl moiety has one to five carbon atoms), nitro, cyano, carboxy, carbamoyl, amidino, guanidino, trifluoromethyl, trifluoromethoxy, phenyl, and phenoxy; and one to three methylene groups are optionally replaced with carbonyl groups), or C 1 -C 14  linear or branched saturated or unsaturated divalent hydrocarbon group containing one to five thioether bonds, ether bonds, and/or amino bonds (\u2014N(H)\u2014) (provided that the hetero atom comprised in said thioether bond, ether bond, or amino bond is not directly linked to B 1 ; and one to three methylene groups are optionally replaced with carbonyl or sulfonyl groups); R 8  represents a hydrogen atom or an organic group containing any of basic skeletons (III) below, wherein, in the basic skeletons (III), Q represents N, O, or S; T represents CH 2 , NH, S, or O; l represents an integer of 0 to 5; m and n each independently represent an integer of 0 to 5, provided that the sum of m and n is not more than 5; said organic group represented by R 8  is optionally substituted by at least one substituent selected from the group consisting of C 1 -C 5  alkyl, C 1 -C 5  alkoxy, C 1 -C 5  alkanoyloxy, hydroxy, fluorine, chlorine, bromine, iodine, amino, monoalkylamino (the alkyl moiety has one to five carbon atoms), dialkylamino (the alkyl moiety has one to five carbon atoms), nitro, cyano, isothiocyanate, trifluoromethyl, phenyl, phenoxy, trifluoromethoxy, and methylenedioxy; and said general formula (I) inclusively represents the (+)-form, the (\u2212)-form, and the (\u00b1)-form of the molecule].

Metadata:
- Claim Count in Document: 23.0
- Percentile: 91.0
- Lexical Diversity: 1.64062
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['14343218', '14772188', '10530664', '15558026', '11736064']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7954975851207314
- 35 USC 102 Novelty (BERT): 0.5386965722657452
- Combined Prediction Score: 0.7698174838352329
- Mean Citation Score: 314.99592799999994
- Max Citation Score: 366.32556
- Similarity Product: 266.89727926579707

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