Soluble tachykinin antagonists, the preparation and use thereof

Details Soluble tachykinin antagonists, the preparation and use thereof Soluble tachykinin antagonists, the preparation and use thereof

C - Chemistry, Metallurgy

07

K

C07K 9/00 (2006.01) A61K 38/12 (2006.01) A61K 38/14 (2006.01) A61K 47/48 (2006.01) C07K 7/22 (2006.01) C07K 7/56 (2006.01) C07K 17/08 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2247802

The compounds of formula (I) cyclo[X11-Z12-X23-X34-Z25-X46]cyclo(2.beta.- 5.beta.) wherein: X1= (D or L)Cys(Y) or (D or L)SeCys(Y), Z1=Asp and Z2=Dap or Z1=Dap and Z2=Asp and X2, X3 and X4 = natural or synthetic hydrophobic amino acids, having Z1, Z2, X2, X3 and X4 the same D or L configuration; Y= is a glycosidic group selected from the aldo and keto hexoses in the furanose or pyranose form bound to the cysteine with an .alpha. or .beta. thioacetalic bond or a cyclithol or a polyvinyl alcohol or PEG, constituted of 5 to 10 monomeric unities, bound to the cysteine with a thioether bond, are endowed of high solubility and of potent tachykinin-antagonistic activity.

L'invention concerne des composés de la formule (I) cycloX¿1??1¿-Z¿1??2¿-X¿2??3¿-X¿3??4¿-Z¿2??5¿-X¿4??6¿]cyclo(2.beta.-5.beta.) dans laquelle: X¿1?= (D ou L)Cys(Y) ou (D ou L)SeCys(Y), Z¿1?= Asp et Z¿2?= Dap ou Z¿1?= Dap et Z¿2?= Asp et X¿2?, X¿3? et X¿4? = aminoacide hydrophobe, naturel ou de synthèse, avec Z¿1?, Z¿2?, X¿2?, X¿3? et X¿4? ayant la même configuration D ou L; Y est un groupe glycosidique, choisi parmi les aldohexoses et les cétohexoses sous la forme furanose ou pyranose, fixé à la cystéine par une liaison .alpha. ou .beta. thioacétal, ou un inositol, un alcool polyvinylique ou un PEG constitué de 5 à 10 unités monomères, lié à la cystéine par une liaison thioéther. Ces composés sont très solubles et ils ont une activité puissante d'antagoniste de la tachikinine.

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