Details for Patent: 7,982,049

Title:	.alpha.-form or .beta.-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 .alpha.-form crystal and .beta.-form crystal of (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]a- cetanilide. The .alpha.-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 .beta.-form crystal does not relatively exhibit hygroscopicity and is also useful as a production intermediate of the .alpha.-form crystal.
Inventor(s):	Kawazoe; Souichirou (Takahagi, JP), Sakamoto; Kenichirou (Takahagi, JP), Awamura; Yuji (Tsukuba, JP), Maruyama; Tatsuya (Tsukuba, JP), Suzuki; Takayuki (Tsukuba, JP), Onda; Kenichi (Tsukuba, JP), Takasu; Toshiyuki (Tsukuba, JP)
Assignee:	Astellas Pharma Inc. (Tokyo, JP)
Filing Date:	Jan 14, 2008
Application Number:	12/007,653
Claims:	1. A solid pharmaceutical composition comprising the .alpha.-form crystal of (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethy- l]acetanilide and a pharmaceutically acceptable carrier. 2. A method of treating diabetes in a patient in need thereof, comprising administering to the patient a solid pharmaceutical composition comprising the .alpha.-form crystal of (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]a- cetanilide and a pharmaceutically acceptable carrier. 3. A solid pharmaceutical composition comprising the .beta.-form crystal of (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethy- l]acetanilide and a pharmaceutically acceptable carrier. 4. A method of treating diabetes in a patient in need thereof, comprising administering to the patient a solid pharmaceutical composition comprising the .beta.-form crystal of (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]a- cetanilide and a pharmaceutically acceptable carrier. 5. The pharmaceutical composition of claim 1, wherein the pharmaceutically acceptable carrier is selected from a group consisting of lactose, mannitol, glucose, hydroxypropyl cellulose, microcrystalline cellulose, starch, polyvinylpyrolidone, and magnesium metasilicate aluminate. 6. The method of claim 2, wherein the pharmaceutically acceptable carrier is selected from a group consisting of lactose, mannitol, glucose, hydroxypropyl cellulose, microcrystalline cellulose, starch, polyvinylpyrolidone, and magnesium metasilicate aluminate. 7. The pharmaceutical composition of claim 3, wherein the pharmaceutically acceptable carrier is selected from a group consisting of lactose, mannitol, glucose, hydroxypropyl cellulose, microcrystalline cellulose, starch, polyvinylpyrolidone, and magnesium metasilicate aluminate. 8. The method of claim 4, wherein the pharmaceutically acceptable carrier is selected from a group consisting of lactose, mannitol, glucose, hydroxypropyl cellulose, microcrystalline cellulose, starch, polyvinylpyrolidone, and magnesium metasilicate aluminate. 9. The pharmaceutical composition of claim 1, wherein the .alpha.-form crystal of (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]a- cetanilide contains less than 0.2% of moisture. 10. The method of claim 2, wherein the .alpha.-form crystal of (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]a- cetanilide contains less than 0.2% of moisture. 11. The pharmaceutical composition of claim 3, wherein the .beta.-form crystal of (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]a- cetanilide contains less than 3% of moisture. 12. The method of claim 4, wherein the .beta.-form crystal of (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]a- cetanilide contains less than 3% of moisture. 13. The pharmaceutical composition of claim 1 in the form of a tablet, a pill, a capsule, granules, or powder. 14. The method of claim 2 wherein the solid pharmaceutical composition is in the form of a tablet, a pill, a capsule, granules, or powder. 15. The pharmaceutical composition of claim 3 in the form of a tablet, a pill, a capsule, granules, or powder. 16. The method of claim 4 wherein the solid pharmaceutical composition is in the form of a tablet, a pill, a capsule, granules, or powder.