PATENT CLAIM ANALYSIS

Application Number: 15768960
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-11
Patent Classification: ["514", "220000"]

Abstract:
The present invention relates to a benzodiazepine derivative of Formula I as a short-acting anesthetic, a pharmaceutical composition comprising the same, a kit comprising the same, a preparation method thereof, an method of anesthesia using the same and use thereof in the manufacture of an anesthetic medicament.

Claim (Index 1):
A compound of Formula I, wherein, R 1  is selected from the group consisting of hydrogen, C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocyclyl, 6-14 membered aryl and 5-14 membered heteroaryl, wherein the C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocyclyl, 6-14 membered aryl and 5-14 membered heteroaryl are each optionally substituted with one or more (e.g., 1, 2, 3 or 4) substituents independently selected from the group consisting of halogen, hydroxy, R 6 R 7 N\u2014, cyano, nitro, C 1-6  alkyl, C 1-6  alkoxy, R 8 S\u2014, R 8 S(O)\u2014, R 8 S(O) 2 \u2014, 3-10 membered cycloalkyl, 3-10 membered heterocyclyl, 6-14 membered aryl and 5-14 membered heteroaryl, preferably, R 1  is C 1-6  alkyl, more preferably, R 1  is methyl or ethyl; R 2  is selected from the group consisting of 3-10 membered cycloalkyl, 3-10 membered heterocyclyl, 6-14 membered aryl and 5-14 membered heteroaryl, wherein the 3-10 membered cycloalkyl, 3-10 membered heterocyclyl, 6-14 membered aryl and 5-14 membered heteroaryl are each optionally substituted with one or more (e.g., 1, 2, 3 or 4) substituents independently selected from the group consisting of halogen, hydroxy, cyano, nitro, C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, R 8 C(O)\u2014, R 8 S\u2014, R 8 S(O)\u2014, R 8 S(O) 2 \u2014, R 6 R 7 N\u2014, C 1-6  alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocyclyl, 6-14 membered aryl and 5-14 membered heteroaryl, preferably, R 2  is selected from the group consisting of 6-14 membered aryl and 5-14 membered heteroaryl optionally substituted with one or more (e.g., 1, 2, 3 or 4) halogen, more preferably, R 2  is selected from the group consisting of pyridyl and phenyl optionally substituted with one or more (e.g., 1, 2, 3 or 4) halogen, even more preferably, R 2  is selected from the group consisting of pyridyl and phenyl optionally substituted with one or more (e.g., 1, 2, 3 or 4) fluorines, most preferably, R 2  is selected from the group consisting of 2-pyridyl, 2-fluorophenyl and phenyl; R 3  is selected from the group consisting of hydrogen, halogen, cyano, nitro, C 1-6  alkyl, C 2-6  alkenyl and C 2-6  alkynyl, wherein the C 1-6  alkyl, C 2-6  alkenyl, and C 2-6  alkynyl are each optionally substituted with one or more (e.g., 1, 2, 3 or 4) substituents independently selected from halogen, preferably, R 3  is halogen, more preferably, R 3  is selected from the group consisting of chlorine and bromine; K, J are each independently selected from the group consisting of N and CR 4 , preferably, K, J are not CR 4  at the same time; R 4  at each occurrence is independently selected from the group consisting of hydrogen, halogen, hydroxy, R 6 R 7 N\u2014, cyano, carboxy, nitro, C 1-6  alkyl, C 1-6  alkoxy, C 2-6  alkenyl, C 2-6  alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocyclyl, 6-14 membered aryl and 5-14 membered heteroaryl, wherein the C 1-6  alkyl, C 1-6  alkoxy, C 2-6  alkenyl, C 2-6  alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocyclyl, 6-14 membered aryl and 5-14 membered heteroaryl are each optionally substituted with one or more (e.g., 1, 2, 3 or 4) substituents independently selected from the group consisting of halogen, hydroxy, C 1-6  alkyl, R 6 R 7 N\u2014, C 1-6  alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocyclyl, 6-14 membered aryl and 5-14 membered heteroaryl, preferably, R 4  at each occurrence is independently selected from the group consisting of hydrogen and C 1-6  alkyl optionally substituted with R 6 R 7 N\u2014, more preferably, R 4  at each occurrence is independently selected from the group consisting of hydrogen, methyl, N,N-dimethylaminomethyl and N,N-diethylaminomethyl; R 5  is independently selected from the group consisting of halogen, hydroxy, R 6 R 7 N\u2014, cyano, C 1-6  alkyl, C 1-6  alkoxy, C 2-6  alkenyl, C 2-6  alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocyclyl, 6-14 membered aryl, 5-14 membered heteroaryl, R 8 C(O)\u2014, R 8 S\u2014, R 8 S(O)\u2014 and R 8 S(O) 2 \u2014, wherein the C 1-6  alkyl is substituted with one or more (e.g., 1, 2, 3 or 4) substituents independently selected from the group consisting of deuterium, halogen, cyano, R 6 R 7 N\u2014, C 1-6  alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocyclyl, 6-14 membered aryl and 5-14 membered heteroaryl, and the C 1-6  alkoxy, C 2-6  alkenyl, C 2-6  alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocyclyl, 6-14 membered aryl, 5-14 membered heteroaryl, R 8 C(O)\u2014, R 8 S\u2014, R 8 S(O)\u2014 and R 8 S(O) 2 \u2014 are each optionally substituted with one or more (e.g., 1, 2, 3 or 4) substituents independently selected from the group consisting of deuterium, halogen, hydroxy, cyano, C 1-6  alkyl, R 6 R 7 N\u2014, C 1-6  alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocyclyl, 6-14 membered aryl and 5-14 membered heteroaryl, preferably, R 5  is independently selected from the group consisting of C 1-6  alkyl, C 1-6  alkoxy, C 2-6  alkenyl, C 2-6  alkynyl, 3-10 membered cycloalkyl, and 3-10 membered heterocyclyl, wherein the C 1-6  alkyl is substituted with one or more (e.g., 1, 2, 3 or 4) substituents independently selected from the group consisting of deuterium, halogen, R 6 R 7 N\u2014, and C 1-6  alkoxy, and the C 1-6  alkoxy, C 2-6  alkenyl, C 2-6  alkynyl, 3-10 membered cycloalkyl, or 3-10 membered heterocyclyl is each optionally substituted with one or more (e.g., 1, 2, 3 or 4) substituents independently selected from the group consisting of deuterium, halogen, hydroxy, C 1-6  alkyl, R 6 R 7 N\u2014, and C 1-6  alkoxy, more preferably, R 5  is independently selected from the group consisting of cyclopropyl, methylcyclopropyl, cyclobutyl, oxetanyl, trifluoromethyl, difluoromethyl, methoxymethyl, N,N-dimethylaminomethyl, N,N-dimethylaminoethyl, N,N-diethylaminomethyl, deuteromethyl, ethenyl, ethynyl and methoxy; R 6 , R 7  at each occurrence are each independently selected from the group consisting of hydrogen, C 1-6  alkyl, C 2-6  alkenyl and C 2-6  alkynyl, preferably, R 6 , R 7  at each occurrence are each independently selected from the group consisting of hydrogen and C 1-6  alkyl, more preferably, R 6 , R 7  at each occurrence are each independently selected from the group consisting of hydrogen, methyl and ethyl; R 8  at each occurrence is independently selected from the group consisting of hydroxy, R 6 R 7 N\u2014, C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocyclyl, 6-14 membered aryl and 5-14 membered heteroaryl; X, Y are each independently \u2014(R 9 R 10 )C\u2014, and the bond between X and Y is a single bond, a double bond or a triple bond, preferably, the bond between X and Y is a single bond or a double bond; one or both of R 9  and R 10  are absent, or R 9  and R 10  at each occurrence are independently selected from the group consisting of hydrogen, halogen, hydroxy, R 6 R 7 N\u2014, cyano, carboxy, nitro, C 1-6  alkoxy, C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocyclyl, 6-14 membered aryl and 5-14 membered heteroaryl, wherein the C 1-6  alkoxy, C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocyclyl, 6-14 membered aryl and 5-14 membered heteroaryl are each optionally substituted with one or more (e.g., 1, 2, 3 or 4) substituents independently selected from the group consisting of halogen, hydroxy, C 1-6  alkyl, R 6 R 7 N\u2014, C 1-6  alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocyclyl, 6-14 membered aryl and 5-14 membered heteroaryl, preferably, one of R 9  and R 10  is absent, or R 9  and R 10  at each occurrence are independently selected from the group consisting of hydrogen and C 1-6  alkyl, more preferably, one of R 9  and R 10  is absent, or R 9  and R 10  at each occurrence are independently selected from the group consisting of hydrogen and methyl; m, n are each independently selected from the group consisting of 0, 1 and 2, and m+n\u22651; and W is selected from the group consisting of hydrogen, halogen, hydroxy, cyano, C 1-6  alkoxy, C 1-6  alkyl, C 2-6  alkenyl and C 2-6  alkynyl, wherein the C 1-6  alkoxy, C 1-6  alkyl, C 2-6  alkenyl and C 2-6  alkynyl are each optionally substituted with one or more (e.g., 1, 2, 3 or 4) substituents independently selected from the group consisting of halogen, hydroxy, C 1-6  alkyl, R 6 R 7 N\u2014, C 1-6  alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocyclyl, 6-14 membered aryl and 5-14 membered heteroaryl group, preferably, W is hydrogen; wherein the above-mentioned hydrogen and the hydrogen contained in the above-mentioned substituents are independently selected from the group consisting of protium, deuterium and tritium, preferably, selected from the group consisting of protium or deuterium, or a pharmaceutically acceptable salt, stereoisomer, tautomer, polymorph, solvate, metabolite or prodrug thereof.

Metadata:
- Claim Count in Document: 29.0
- Percentile: 91.0
- Lexical Diversity: 1.57576
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['12598882', '14858159', '14448160', '09927324', '15150038']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8351805705827762
- 35 USC 102 Novelty (BERT): 0.5329111581690087
- Combined Prediction Score: 0.8049536293413994
- Mean Citation Score: 356.00754
- Max Citation Score: 373.12048
- Similarity Product: 325.4903969063187

Labels:
- Claim Label 101: 1
- Claim Label 102: 1
- Claim Label 103: 0
- Claim Label 112: 0
- Combined Label: 1
- Label 101 Adjusted: 1

Dataset: test