PATENT CLAIM ANALYSIS

Application Number: 15759084
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2019-02
Patent Classification: ["514", "210000"]

Abstract:
The present application relates to novel azetidinimine of formula (I). Wherein R 1 -R 6  are as defined in claim  1 . The azetidinimine of the invention are useful as antibiotics and as inhibitors of a carbapenemases. The present invention thus further relates to their use in antibiotic therapies and their methods of synthesis.

Claim (Index 1):
Compound of formula (I): characterized in that:\n R 1  represents a chemical moiety chosen in the group consisting of hydrogen, cyano, C 1 -C 10  alkyl, C 3 -C 10  cycloalkyl, C 1 -C 10  alkoxy, C 1 -C 10  haloalkoxy, (C 1 -C 6 )-alkoxy-(C 1 -C 6 )-alkyl, (C 1 -C 6 )-haloalkoxy-(C 1 -C 6 )-alkyl, C 1 -C 10  thioalkyl, (C 1 -C 6 )-alkylthio-(C 1 -C 6 )-alkyl, C 1 -C 10  alkylsulfinyl, C 1 -C 10  haloalkylsulfinyl, C 1 -C 10  haloalkylsulfonyl, C 3 -C 10  trialkylsilyl, C 1 -C 10  alkylsulfonyl, C 5 -C 12  arylsulfonyl, formyl, C 2 -C 10  alkylcarbonyl, C 2 -C 10  alkenyl, C 2 -C 10  alkynyl, C 2 -C 10  alkenyloxy, C 2 -C 10  alkynyloxy, C 2 -C 10  alkenylthio, C 2 -C 10  alkynylthio, C 1 -C 10  haloalkyl, C 2 -C 10  haloalkenyl, C 2 -C 10  haloalkynyl, C 2 -C 10  haloalkylcarbonyl, C 1 -C 10  haloalkylthio, C 2 -C 10  haloalkenyloxy, C 2 -C 10  haloalkynyloxy, C 2 -C 10  haloalkenylthio, C 2 -C 10  haloalkynylthio, (C 5 -C 12 )-aryl-(C 1 -C 6 )-alkyl, (C 5 -C 12 )-aryl-(C 1 -C 6 )-alkyl ester or a mono or polycyclic C 5 -C 12  aryl or mono or polycyclic C 3 -C 12  heteroaryl fragments, \n wherein the aryl or heteroaryl fragments are optionally substituted by\n one or several halogen atoms, hydroxyl (OH), nitro, cyano, formyl, C 1 -C 6  alkyl, C 3 -C 7  cycloalkyl, amino-C 1 -C 10  alkoxy, (carboxylic acid)-C 1 -C 10  alkoxy, (carboxylic (C 1 -C 6 )alkyl ester)-C 1 -C 10  alkoxy, (1,2 diol)-C 2 -C 10  alkoxy, \u2014O\u2014(C 1 -C 6 )alkyl-O\u2014(C 1 -C 6 )alkyl-OH, (C 1 -C 6 )-alkoxy-(C 1 -C 6 )-alkyl, C 2 -C 6  alkylcarbonyl, C 1 -C 6  alkylthio, C 1 -C 6  thioalkyl, (C 1 -C 6 )-alkylthio-(C 1 -C 6 )-alkyl, C 1 -C 6  alkylsulfinyl, C 1 -C 6  alkylsulfonyl, C 1 -C 6  haloalkyl, C 1 -C 6  haloalkoxy, C 1 -C 6  haloalkoxy alkyl, C 2 -C 6  haloalkylcarbonyl, C 1 -C 6  haloalkylthio, C 1 -C 6  haloalkylsulfinyl, C 1 -C 6  haloalkylsulfonyl, C 3 -C 6  trialkylsilyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 2 -C 6  haloalkynyl, C 2 -C 6  haloalkenyl, C 2 -C 6  haloalkenyloxy, C 2 -C 6  haloalkynyloxy, C 2 -C 6  alkenyloxy, C 2 -C 6  alkynyloxy, C 2 -C 6  alkenylthio, C 2 -C 6  alkynylthio, C 2 -C 6  haloalkenylthio, C 2 -C 6  haloalkynylthio and/or a C 1 -C 6  alkoxy optionally substituted by a mono or polycyclic C 5 -C 12  aryl group, and/or \n a bridging group of formula \u2014O\u2014CH 2 \u2014O\u2014 or \u2014O\u2014CH 2 CH 2 \u2014O\u2014; \n \n R 2 , R 3 , R 4  and R 5 , independently one from each other, represent a chemical moiety chosen in the group consisting of hydrogen, halogen, nitro, cyano, C 1 -C 10  alkyl, C 3 -C 10  cycloalkyl, C 1 -C 10  alkoxy, C 1 -C 10  haloalkoxy, (C 1 -C 6 )-alkoxy-(C 1 -C 6 )-alkyl, (C 1 -C 6 )-haloalkoxy-(C 1 -C 6 )-alkyl, C 1 -C 10  thioalkyl, (C 5 -C 12 )-aryl-(C 1 -C 6 )-alkyl ester, (C 1 -C 6 )-alkylthio-(C 1 -C 6 )-alkyl, C 1 -C 10  alkylsulfinyl, C 1 -C 10  haloalkylsulfinyl, C 1 -C 10  haloalkylsulfonyl, C 3 -C 10  trialkylsilyl, C 1 -C 10  alkylsulfonyl, C 5 -C 12  arylsulfonyl, formyl, C 2 -C 10  alkylcarbonyl, C 2 -C 10  alkenyl, C 2 -C 10  alkynyl, C 2 -C 10  alkenyloxy, C 2 -C 10  alkynyloxy, C 2 -C 10  alkenylthio, C 2 -C 10  alkynylthio, C 1 -C 10  haloalkyl, C 2 -C 10  haloalkenyl, C 2 -C 10  haloalkynyl, C 2 -C 10  haloalkylcarbonyl, C 1 -C 10  haloalkylthio, C 2 -C 10  haloalkenyloxy, C 2 -C 10  haloalkynyloxy, C 2 -C 10  haloalkenylthio, C 2 -C 10  haloalkynylthio, (C 5 -C 12 )-aryl-(C 1 -C 6 )-alkyl or a mono or polycyclic C 5 -C 12  aryl or mono or polycyclic C 3 -C 12  heteroaryl fragments, wherein the aryl or heteroaryl fragments are optionally substituted by one or several halogen atoms, nitro, cyano, formyl, COOH, \u2014COO(C 1 -C 6  alkyl), C 1 -C 6  alkyl, C 3 -C 7  cycloalkyl, C 1 -C 6  N 3 -substituted alkyl, C 1 -C 6  NH 2 -substituted alkyl, C 1 -C 6  alcohol, C 1 -C 6  alkoxy, (C 1 -C 6 )-alkoxy-(C 1 -C 6 )-alkyl, C 2 -C 6  alkylcarbonyl, C 1 -C 6  alkylthio, C 1 -C 6  thioalkyl, (C 1 -C 6 )-alkylthio-(C 1 -C 6 )-alkyl, C 1 -C 6  alkylsulfinyl, C 1 -C 6  alkylsulfonyl, C 1 -C 6  haloalkyl, C 1 -C 6  haloalkoxy, C 1 -C 6  haloalkoxy alkyl, C 2 -C 6  haloalkylcarbonyl, C 1 -C 6  haloalkylthio, C 1 -C 6  haloalkylsulfinyl, C 1 -C 6  haloalkylsulfonyl, C 3 -C 6  trialkylsilyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 2 -C 6  haloalkynyl, C 2 -C 6  haloalkenyl, C 2 -C 6  haloalkenyloxy, C 2 -C 6  haloalkynyloxy, C 2 -C 6  alkenyloxy, C 2 -C 6  alkynyloxy, C 2 -C 6  alkenylthio, C 2 -C 6  alkynylthio, C 2 -C 6  haloalkenylthio, C 2 -C 6  haloalkynylthio, a monocyclic C 5 -C 6  aryl group optionally substituted by a C 1 -C 6  alkyloxy group and/or a COO(C 1 -C 6  alkyl) group wherein the alkyl is substituted by NH 2  or NHCOO(C 1 -C 6 )alkyl or NHCOO(C 1 -C 6 )alkyl(mono or polycyclic C 5 -C 12 )aryl; \n R 6  represents a mono or polycyclic C 5 -C 12  aryl fragment, wherein the aryl fragment is optionally substituted by one or several halogen atoms, cyano, formyl, nitro, C 1 -C 6  alkyl, C 3 -C 7  cycloalkyl, C 1 -C 6  alkoxy, (C 1 -C 6 )-alkoxy-(C 1 -C 6 )-alkyl, C 2 -C 6  alkylcarbonyl, C 1 -C 6  alkylthio, C 1 -C 6  thioalkyl, (C 1 -C 6 )-alkylthio-(C 1 -C 6 )-alkyl, C 1 -C 6 alkylsulfinyl, C 1 -C 6  alkylsulfonyl, C 1 -C 6  haloalkyl, C 1 -C 6  haloalkoxy, C 1 -C 6  haloalkoxy alkyl, C 2 -C 6  haloalkylcarbonyl, C 1 -C 6  haloalkylthio, C 1 -C 6  haloalkylsulfinyl, C 1 -C 6  haloalkylsulfonyl, C 3 -C 6  trialkylsilyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 2 -C 6  haloalkynyl, C 2 -C 6  haloalkenyl, C 2 -C 6  haloalkenyloxy, C 2 -C 6  haloalkynyloxy, C 2 -C 6  alkenyloxy, C 2 -C 6  alkynyloxy, C 2 -C 6  alkenylthio, C 2 -C 6  alkynylthio, C 2 -C 6  haloalkenylthio, C 2 -C 6  haloalkynylthio fragments, and/or a monocyclic C 5 -C 6  aryl group optionally substituted by a C 1 -C 6  alkyloxy group; \n provided that at least two of R 3 , R 4  and R 5  represent a hydrogen atom and R 6  is not a substituted or unsubstituted \u2014SO 2 -phenyl group such as a tosyl group.

Metadata:
- Claim Count in Document: 28.0
- Percentile: 90.0
- Lexical Diversity: 1.51282
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15029377', '14785034', '14382232', '13356729', '13538399']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8398073451124672
- 35 USC 102 Novelty (BERT): 0.5312991017432583
- Combined Prediction Score: 0.8089565207755465
- Mean Citation Score: 357.41369799999984
- Max Citation Score: 368.19736
- Similarity Product: 283.6295921996689

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

Dataset: test