PATENT CLAIM ANALYSIS

Application Number: 16073897
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2019-02
Patent Classification: ["544", "262000"]

Abstract:
Disclosed herein is a new route of synthesis and a new stable amorphous form of ibrutinib. Also disclosed are pharmaceutical compositions, oral dosage forms and the use of the amorphous ibrutinib in the treatment of mantle cell lymphoma or chronic lymphocytic leukemia.

Claim (Index 1):
A process for the production of amorphous ibrutinib at least comprising the following synthesis steps:\n a) reacting compound (1) (3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine) and an in 3 position functionalized and amino-protected piperidine, wherein the 3 position is functionalized by a leaving group X and the piperidine amino-group is protected by the amino-protecting group Z, to yield compound (2) (1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]Z) b) deprotection of compound (2) to yield compound (3) (1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin]); c) reacting compound (3) and acryloyl chloride (2-propenoyl chloride) in an pharmaceutically acceptable solvent to yield compound (4) ibrutinib (1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one); d) filtration of the reaction mixture obtained in step c); and e) evaporation of the solvent to precipitate essentially amorphous compound (4); wherein the pharmaceutically acceptable solvent of step c) comprises an electric dipole moment \u03bc/D of \u22652 and \u22648.

Metadata:
- Claim Count in Document: 2.0
- Percentile: 95.0
- Lexical Diversity: 1.32353
- Patent Class: 544.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['16073809', '15336418', '15853368', '15516285', '11455338']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7518727399901489
- 35 USC 102 Novelty (BERT): 0.4847658901687871
- Combined Prediction Score: 0.7251620550080127
- Mean Citation Score: 205.95125
- Max Citation Score: 240.31172
- Similarity Product: 194.0636610072804

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