PATENT CLAIM ANALYSIS

Application Number: 16319951
Application Type: Utility
Filing Date: 2019-01
Publication Date: 2019-07
Patent Classification: ["544", "277000"]

Abstract:
There are provided substituted purine and 3-deazapurine analogues, which modulate the activity of Choline Kinase (ChoK). The compounds of this invention are therefore useful in treating diseases caused by an altered choline metabolism, such as cancer, cell proliferative disorders, infectious diseases of different origin, immune-related disorders and neurodegenerative disorders. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.

Claim (Index 6):
A process for the preparing a compound or a pharmaceutically acceptable salt according to  claim 1 , which comprises one of the following sequences of steps:\n either SEQUENCE A: Step a) alkylating an intermediate compound of formula (VI): wherein X and R3 are as defined in  claim 1 , with an intermediate compound of formula (V): wherein A, R1, R2 and n are as defined in  claim 1  and J is selected from the group consisting of bromine, iodine, hydroxy, methansulfonyl (-OMs) and p-toluensulfonyl (-OTs); Step b) substituting the chlorine of the resultant intermediate compound of formula (III) wherein X, A, R1, R2, R3 and n are as defined in  claim 1 , with a protected nitrogen source compound NH(PG) 2  (IV), wherein PG is independently hydrogen or a protecting group \u2014COOR7, wherein R7 is a (C 1 -C 6 )alkyl, such as for instance methyl, ethyl or tert-butyl, or an aryl(C 1 -C 6 )alkyl, such as for instance benzyl, with the proviso that such PGs are not simultaneously hydrogen; and Step c) removing the protecting group(s) PG of the resultant intermediate compound of formula (II) wherein X, A, R1, R2, R3, PG and n are as defined above, to yield a compound of general formula (I), as defined in  claim 1 ; or Step d) substituting the chlorine of the intermediate compound of formula (III), resulting from step a), with a nitrogen source, such as an ammonia solution, to yield a compound of general formula (I), as defined in  claim 1 ; or SEQUENCE B Step b\u2032) substituting the chlorine of an intermediate compound of formula (VI): as defined in step a, with a protected nitrogen source compound NH(PG) 2  (IV), as described for step b, to yield an intermediate compound of formula (VIII): wherein X, R3 and PG are as defined above; or Step d\u2032) substituting the chlorine of an intermediate compound of formula (VI), as defined above, with a nitrogen source, such as an ammonia solution, as described for step d); and Step e) protecting the NH 2  group of the resultant intermediate compound of formula (VII) wherein X and R3 are as defined in  claim 1 , with a reagent of formula (PG) 2 O or PGCl to yield an intermediate compound of formula (VIII), as defined in step b\u2032); then Step a\u2032) alkylating the protected intermediate compound of formula (VIII), resulting from either step b\u2032 or step e, with an intermediate compound of formula (V), as defined in step a and in the conditions described therein; Step c) removing the protecting group(s) PG of the resultant intermediate compound of formula (II) as defined in step c of Sequence A, to yield a compound of general formula (I), as defined in  claim 1 ; or SEQUENCE C Step d\u2032) substituting the chlorine of an intermediate compound of formula (VI) according to Sequence B; Step a\u2033) alkylating the resulting intermediate compound of formula (VII), as defined in Sequence B, with an intermediate of formula (V), as defined in step a, according to the conditions described therein; optionally converting said compound of formula (I) into another compound of formula (I), converting said compound of formula (I) into a pharmaceutically acceptable salt thereof, or converting said salt into a free compound (I).

Metadata:
- Claim Count in Document: 3.0
- Percentile: 99.0
- Lexical Diversity: 1.52632
- Patent Class: 544.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['12678806', '13377854', '14874513', '15335619', '13780557']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8159079275089074
- 35 USC 102 Novelty (BERT): 0.5062880116844508
- Combined Prediction Score: 0.7849459359264617
- Mean Citation Score: 270.152288
- Max Citation Score: 281.84406
- Similarity Product: 193.977042273016

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

Dataset: test