PATENT CLAIM ANALYSIS

Application Number: 15977569
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-12
Patent Classification: ["514", "050000"]

Abstract:
The invention provides a new bioorthogonal deprotection method for preparing heterocyclic compounds by bond cleavage using palladium. The methods have general application in the field of biological synthetic chemistry. Compounds, such as prodrugs, which are useful in such methods are also provided.

Claim (Index 1):
A method of preparing a heterocyclic compound or a salt thereof, the method comprising:\n a) providing a first compound comprising a first group defined according to formula (II): bonded to a second group defined according to formula (III) at the positions indicated by asterisks and\n b) cleaving the bond between the first and second groups by reacting the first compound with palladium in aqueous conditions \n wherein\n X and Y taken together with the endocyclic nitrogen atom and ring carbonyl group to which they are attached form a heterocyclic group; and \n R 1 , R 2  and R 3  are selected independently from the group consisting of H, optionally substituted C 1-10 alkyl, optionally substituted C 3-10 cycloalkyl, optionally substituted C 2-10 alkenyl, optionally substituted C 3-10 cycloalkenyl, optionally substituted C 2-10 alkynyl, optionally substituted C 2-10 heteroalkyl, optionally substituted C 3-10 heterocycloalkyl, optionally substituted C 2-10 heteroalkenyl, optionally substituted C 3-10 heterocycloalkenyl, optionally substituted C 2-10 heteroalkynyl, optionally substituted C 6-14 aryl and optionally substituted C 5-14 heteroaryl, wherein the heterocyclic compound or salt thereof is a drug compound, and wherein the drug compound is selected from the group consisting of 5-fluorouracil, olaparib, ropinirole, pemetrexed, milrinone, amrinone, aciclovir, iodoxuridine, sunitinib, pimobendan, enoximone, cilostazol, nitrofurantoin, aripiprazole, sertindole, ziprasidone, mosapramine, phenobarbital, methylphenobarbital, primidone, lorazepam, nitrazepam, clonazepam, ethotoin, phenytoin, mephenytoin, fosphenytoin, floxuridine, flucytosine, stavudine, telbivudine, zidovudine, trifluridine, entecavir and uramustine; or a derivative thereof.

Metadata:
- Claim Count in Document: 7.0
- Percentile: 93.0
- Lexical Diversity: 1.20513
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['14901314', '10541328', '14428501', '14764236', '14156314']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7285752038971475
- 35 USC 102 Novelty (BERT): 0.5139941896391775
- Combined Prediction Score: 0.7071171024713505
- Mean Citation Score: 251.51086400000003
- Max Citation Score: 262.73773
- Similarity Product: 178.53416705186248

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