Pharmaceutical dopamine glycoconjugate compositions and...

C - Chemistry – Metallurgy – 07 – H

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C07H 17/00 (2006.01) A61K 31/70 (2006.01) A61K 47/48 (2006.01)

Patent

CA 2443774

Hydrophilic transportable N-linked glycosyl dopaminergic prodrug compounds according to FORMULA V, (see formula V) wherein, Ring 1 comprises a cyclic or heterocyclic ring, or aryl or heteroaryl ring, all of said rings comprising 4 to 8 carbon atoms, among which atoms are counted "X" and "Y"; R0, R1, R2, R3 and R4 comprise substituents of Ring 1; either of X or Y is optional; each of X and Y, when present comprise a carbon atom, a halogen atom or a lower alkyl; Z, R5 and R5' are optional; when Z is present it comprises a lower alkyl having substituents R5, R5'; R6 and R6' comprise substituents on a carbon atom linking Z with N through a single bond, or when Z is absent, linking N with Ring 1; N comprises a nitrogen atom of an amine or an amide linked with E through a single bond and having R7 as a substituent; and E comprises a saccharide.

L'invention concerne des composés de promédicament dopaminergique glycosyl à liaison N transportable et hydrophile, de formule V, dans laquelle le cycle <u>1</u> comprend un noyau cyclique ou hétérocyclique, ou bien un noyau aryle ou hétéroaryle, tous ces noyaux comportant 4 à 8 atomes de carbone, parmi lesquels sont comptés "X" et "Y"; R0, R1, R2, R3 et R4 comportent des substituants du cycle <u>1</u>; soit X soit Y est optionnel; X et Y, s'ils sont présents, comprennent chacun un atome de carbone, un atome d'halogène ou un alkyle inférieur; Z, R5 et R5' sont optionnels; quand Z est présent, il comporte un alkyle inférieur ayant les substituants R5, R5'; R6 et R6' comprennent des substituants sur un atome de carbone liant Z et N par une liaison simple, ou, lorsque Z est absent, liant N et le cycle <u>1</u>; N comprend un atome d'azote d'une amine ou d'un amide lié à E par une liaison simple et avec R7 comme substituant; et E comporte un saccharide.

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