PATENT CLAIM ANALYSIS

Application Number: 15750339
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-08
Patent Classification: ["540", "508000"]

Abstract:
The invention relates to processes for the synthesis of benzodiazepine derivatives of Formula I: (I)

Claim (Index 1):
A process for producing a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein\n R 1  is \n \u2014CH 2 C(O)C(R 2 )(R 3 )-L-R 4 , \u2014CH 2 CHOHC(R 2 )(R 3 )-L-R 4 , \u2014CH 2 CHOH(CH 2 ) a R 7 , \u2014CH 2 C(O)(CH 2 ) 2 R 8 , or an optionally substituted aliphatic moiety; \n R 2  and R 3  are each, independently, H or C 1-3  aliphatic, halo, or C 1-3  haloaliphatic; or R 2  and R 3  together with the intervening carbon atom to which they are bonded, form a C 3-6  carbocyclic moiety; \n L is a bond or C 1-3  alkylene; \n R 4  is \u2014OR 5  or \u2014SR 5 ; \n R 5  is hydrogen, optionally substituted alkyl, a protecting group or \u2014C(O)R 6 ; \n R 6  is optionally substituted aliphatic, heteroaliphatic, aromatic or heteroaromatic moiety; \n a is 0 or 1; \n R 7  and R 5  are selected from alkyl and cycloalkyl groups and saturated heterocyclic groups optionally substituted at a heteroatom; \n W and X are, independently, hydrogen, halo, C 1-8  alkyl or C 1-8  alkoxy; and \n rings A and B are each, independently, a monocyclic aryl or heteroaryl, optionally substituted with one or more substituents independently selected from halo, hydroxy, amino, nitro, carboxyl, carboxamido, cyano, \u2014SO 3 H, and optionally substituted C 1-8  alkyl, C 1-8  alkoxy, C 1-8  alkylamino or di(C 1-8  alkyl)amino; wherein any one or more substituent on R 1 , ring A or ring B may be unprotected or in a protected form; \n wherein the process comprises:\n (a) providing a reaction mixture by adding a compound of formula (I-A): \n a compound of formula (I-B): and a phosgene synthetic equivalent or phosgene to an aprotic solvent, to form a compound of formula (I); or (b) providing a reaction mixture by adding a compound of formula (I-C): and a phosgene synthetic equivalent or phosgene, to an aprotic solvent and, subsequently, adding a compound of formula (I-B): to the reaction mixture to form a compound of formula (I); wherein the phosgene synthetic equivalent is carbonyldiimidazole (CDI), diphosgene, triphosgene, a chloroformate, or disuccinimidyl carbonate.

Metadata:
- Claim Count in Document: 2.0
- Percentile: 88.0
- Lexical Diversity: 1.125
- Patent Class: 540.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15502490', '14761843', '15322854', '13140915', '13412997']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7070290238532725
- 35 USC 102 Novelty (BERT): 0.5308154998821908
- Combined Prediction Score: 0.6894076714561643
- Mean Citation Score: 251.47708
- Max Citation Score: 342.33792
- Similarity Product: 258.410605994339

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

Dataset: test