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Last Updated: April 15, 2026

Claims for Patent: 7,342,117


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Summary for Patent: 7,342,117
Title:α-form or β-form crystal of acetanilide derivative
Abstract:To provide novel crystals useful as an ingredient for the production of a diabetes remedy. The invention is concerned with α-form crystal and β-form crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenyleth-yl)amino]ethyl]acetanilide. The α-form crystal does not exhibit hygroscopicity and has stability such that it can be used as a medicine, and is useful for mass synthesis in the industrial production. The β-form crystal does not relatively exhibit hygroscopicity and is also useful as a production intermediate of the α-form crystal.
Inventor(s):Souichirou Kawazoe, Kenichirou Sakamoto, Yuji Awamura, Tatsuya Maruyama, Takayuki Suzuki, Kenichi Onda, Toshiyuki Takasu
Assignee: Astellas Pharma Inc
Application Number:US10/494,018
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 7,342,117
Patent Claims: 1. A crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide having a heat absorption peak at 142 to 146° C. in the DSC analysis and having main peaks at around 5.32, 8.08, 15.28, 17.88, 9.04, 20.20, 23.16 and 24.34 in the terms of 2θ(°) in the powder X-ray diffraction.

2. A crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide having heat absorption peaks at 90 to 110° C. and at 142 to 146° C. in the DSC analysis and having main peaks at around 9.68, 19.76, 20.72, 22.10 and 23.52 in the terms of 2θ(°) in the powder X-ray diffraction.

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