Global Patent Index - EP 1146035 A9

EP 1146035 A9 2001-12-05 - CRYSTAL POLYMORPHISM OF AMINOETHYLPHENOXYACETIC ACID DERIVATIVE

Title (en)

CRYSTAL POLYMORPHISM OF AMINOETHYLPHENOXYACETIC ACID DERIVATIVE

Title (de)

KRISTAL-POLYMORPHISMUS VON DERIVATEN DER AMINOETHYL-PHENOXYESSIGSÄURE

Title (fr)

POLYMORPHISME CRISTALLIN DE DERIVE D'ACIDE AMINOETHYLPHENOXYACETIQUE

Publication

EP 1146035 A9 (EN)

Application

EP 00900407 A

Priority

  • JP 0000168 W
  • JP 1363999 A

Abstract (en)

[origin: EP1146035A1] Crystal polymorphism of 2-Ä4-Ä2-ÄÄ1s,2RÜ-2-hydroxy-2-(4-hydroxyphenyl)-1-methyl ethylÜaminoÜethylÜphenoxyÜacetic acid which has potent beta 2 adrenergic receptor stimulating and beta 3-adrenergic receptor stimulating effects, is useful in relieving a pain, promoting calculi removal, etc. in urinary lithiasis and shows intense diffraction peaks at 10.8, 19.1, 19.3, 19.8, 20.6 and 27.0 DEG in the powder x-ray diffractometry pattern at a diffraction angle (2/θ0+/-0.1). It is produced by, for example, hydrolyzing ethyl 2-Ä4-Ä2-ÄÄ1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethylÜaminoÜeth yÜphenoxyÜacetate phosphate by using sodium hydroxide, adding an aqueous solution of phosphoric acid at 40 DEG C or above to give the above compound, adding a solvent mixture comprising methanol with water or methanol and then stirring in a suspended state at from 40 DEG C to the reflux point for 30 minutes to several hours.

IPC 1-7 (main, further and additional classification)

C07C 217/60

IPC 8 full level (invention and additional information)

A61K 31/19 (2006.01); A61P 13/04 (2006.01); A61P 29/00 (2006.01); C07C 213/10 (2006.01); C07C 217/60 (2006.01)

CPC (invention and additional information)

C07C 217/60 (2013.01); C07C 213/10 (2013.01)

Designated contracting state (EPC)

AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE

EPO simple patent family

EP 1146035 A1 20011017; EP 1146035 A9 20011205; EP 1146035 B1 20051116; AR 022319 A1 20020904; AT 309978 T 20051215; AU 2004700 A 20000807; AU 778091 B2 20041118; CA 2359061 A1 20000727; CA 2359061 C 20040406; CN 1216855 C 20050831; CN 1337937 A 20020227; CO 5160240 A1 20020530; CZ 20012621 A3 20020213; CZ 302572 B6 20110720; DE 60024053 D1 20051222; DE 60024053 T2 20060720; DK 1146035 T3 20060327; ES 2251956 T3 20060516; IL 144253 A 20040831; IL 144253 D0 20020523; JP 4005771 B2 20071114; MY 119093 A 20050331; NO 20013537 A 20010918; NO 20013537 D0 20010717; NO 327638 B1 20090907; NZ 512965 A 20021126; PE 13982000 A1 20001222; RU 2237656 C2 20041010; TW I223647 B 20041111; US 6376707 B1 20020423; WO 0043350 A1 20000727; ZA 200105830 B 20000716

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