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 7):
Method to prepare a compound according to any one of  claims 1  to  6  including the explicitly excluded compounds of  claim 1  characterized in the following steps:\n a. to a compound of formula (II): \n wherein R 4  and R 6  are as defined in any one of  claims 1  to  6  including the excluded definitions of  claim 1 , and R 7  represents a leaving group such as amides, sulfonyles, or oxy-carbonyls, optionally, R 6 \u2014N\u2014R 7  may form at least one ring wherein R 6  and R 7  directly linked one to each other and wherein said ring comprises from 3 to 12 atoms chosen from C, N, O, S, B and P, substituted by at least one hydrogen, oxygen, nitrogen, hydroxyl, thiol, amine, cyano, C 1 -C 6  alkyl, C 3 -C 6  cycloalkyl, C 1 -C 6  alkoxy, C 1 -C 6  haloalkoxy, (C 1 -C 6 )-alkoxy-(C 1 -C 6 )-alkyl, (C 1 -C 6 )-haloalkoxy-(C 1 -C 6 )-alkyl, C 1 -C 6  thioalkyl, (C 1 -C 6 )-alkylthio-(C 1 -C 6 )-alkyl, C 1 -C 6  alkylsulfinyl, C 1 -C 6  haloalkylsulfinyl, C 1 -C 6  haloalkylsulfonyl, C 3 -C 6  trialkylsilyl, C 1 -C 6  alkylsulfonyl, C 5 -C 12  arylsulfonyl, formyl, C 2 -C 6  alkylcarbonyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 2 -C 6  alkenyloxy, C 2 -C 6  alkynyloxy, C 2 -C 6  alkenylthio, C 2 -C 6  alkynylthio, C 1 -C 6  haloalkyl, C 2 -C 6  haloalkenyl, C 2 -C 6  haloalkynyl, C 2 -C 6  haloalkylcarbonyl, C 1 -C 6  haloalkylthio, C 2 -C 6  haloalkenyloxy, C 2 -C 6  haloalkynyloxy, C 2 -C 6  haloalkenylthio, C 2 -C 6  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, 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 and/or nitro fragments; is added a compound of formula (III): wherein R 1 , R 2  and R 3  are as defined in any one of  claims 1  to  5 in the presence of a base B1, preferably R 1  is an electro-donating group and/or R 2  and/or R 3  are electron-withdrawing groups, preferably under microwaves, advantageously step (a) is carried out under pressure and/or at a temperature above 50\u00b0 C., and in particular without the presence of a metal compound, such as copper, whether it is in its metallic or one of its oxidized or reduced forms; b. an optional addition step of R 5  as defined in any one of  claims 1  to  5  through a nucleophilic addition to the compound obtained in step a., preferably with R5-X, wherein X is a halogen atom in the presence of a base B2; c. retrieving the compound of formula (I) as defined in any one of  claims 1  to  5 .

Metadata:
- Claim Count in Document: 28.0
- Percentile: 90.0
- Lexical Diversity: 1.51282
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15029377', '14785034', '14382232', '13356729', '13538399']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8200509553161908
- 35 USC 102 Novelty (BERT): 0.5345142467860489
- Combined Prediction Score: 0.7914972844631766
- Mean Citation Score: 357.41369799999984
- Max Citation Score: 368.19736
- Similarity Product: 235.30416273916245

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

Dataset: test