C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 14/62 (2006.01) A61K 9/00 (2006.01) A61K 38/28 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2503670
The invention relates to crystals of an insulin analogue, in which asparagine (Asn) in position B3 of the B chain is replaced by a naturally occurring basic amino acid residue, and at least one amino acid residue in positions B27, B28 or B29 of the B chain is replaced by another naturally occurring neutral or acid amino acid residue. According to the invention, phenylalanine (Phe) can optionally be absent in position B1 of the B chain, and the crystals exist in space group R3 (Nr. 146) with cell axes A=81.5 .ANG. .plusmn. 1 .ANG. and C=33.3 .ANG. .plusmn. 1 .ANG.. The invention also relates to the production and use of said crystals, and to a pharmaceutical composition containing these crystals.
Cristaux d'un analogue d'insuline dans lequel de l'asparagine (Asn) en position B3 de la chaîne B est remplacée par un reste d'acide aminé basique naturel et au moins un reste d'acide aminé dans les positions B27, B28 ou B29 de la chaîne B est remplacé par un autre reste d'acide aminé neutre ou acide naturel. Selon la présente invention, la phénylalanine (Phe) peut éventuellement manquer en position B1 de la chaîne B, et les cristaux du groupe spatial R3 (no 146) possèdent des axes cellulaires A=81,5 .ANG. .plusmn. 1 .ANG. et C=33,3 .ANG. .plusmn. 1 .ANG.. La présente invention concerne également la production desdits cristaux ainsi que leur utilisation et des compositions pharmaceutiques les contenant.
Aventis Pharma Deutschland Gmbh
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Sanofi-Aventis Deutschland Gmbh
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