PATENT CLAIM ANALYSIS

Application Number: 16246999
Application Type: Utility
Filing Date: 2019-01
Publication Date: 2019-05
Patent Classification: ["549", "214000"]

Abstract:
The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Horner-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.

Claim (Index 93):
A compound of formula (IVE): wherein Y is iodide, bromide, or trifluoromethanesulfonate; Z is an ester, a sulfonate, chloride, bromide, or iodide; each P 3  is independently H or a hydroxyl protecting group, and X 2  is oxo; or both P 3  groups and X 2 , together with the atoms to which each is attached, combine to form ketal; and (a1) R 2  is H or a hydroxyl protecting group, R 3  and R 4  combine to form a double bond; or (a2) R 2  and R 3  combine to form a bond, and R 4  is H; (b1) R 7  and R 8  combine to form a bond, and R 9  is H; or (b2) R 7  is H or a hydroxyl protecting group, and R 8  and R 9  combine to form a double bond; (c1) X 3  is oxo and R 10  is H or \u2014OP 5 , where P 5  is H or an ether hydroxyl protecting group; or (c2) X 3  and R 10  together with the carbon atom to which they are attached form \u2014CH 2 OP 6 , wherein P 6  is H or a hydroxyl protecting group, and R 10  is H.

Metadata:
- Claim Count in Document: 20.0
- Percentile: 99.0
- Lexical Diversity: 1.88679
- Patent Class: 549.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['15033970', '15707412', '15571921', '11874218', '14069057']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7486079426221104
- 35 USC 102 Novelty (BERT): 0.6025441729109282
- Combined Prediction Score: 0.7340015656509922
- Mean Citation Score: 425.015932
- Max Citation Score: 529.3929400000002
- Similarity Product: 454.8672254888177

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