Compounds which can be retained in brain

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 323/41 (2006.01) A61K 47/06 (2006.01) A61K 47/48 (2006.01) C07C 327/30 (2006.01) C07D 207/16 (2006.01) C07D 209/20 (2006.01) C07D 213/56 (2006.01) C07D 233/64 (2006.01) C07D 239/42 (2006.01) C07D 295/13 (2006.01) C07D 295/145 (2006.01) C07D 307/54 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01)

Patent

CA 2120248

2120248 9403424 PCTABS00030 A group of novel compounds which can pass through the blood-brain barrier (BBB) with a drug carried thereon and reside in the brain to release the drug and a group of known compounds having the above characteristics. More specifically, a compound represented by general formula (Ia) and a salt thereof, wherein R1 represents hydroxy, carboxy, amino which may be substituted by C1-C6 alkyl, or C1-C6 alkyl which may be substituted by a 5- to 7-membered saturated heterocyclic group, R2 represents hydrogen or C1-C6 alkyl, R3 represents hydrogen or C1-C6 alkyl which may be hydroxylated, R4 represents hydrogen or C1-C6 alkyl, R5 represents amino acid residue, or -S-R6 or -CO-R6 (wherein R6 represents C1-C14 alkyl which may be substituted by a 5- to 7-membered saturated heterocyclic group, C1-C14 alkyl, C2-C6 alkenyl, aryl or a 5- to 7-membered saturated ring group), or a group represented by general formula (IVa), wherein R1, R2, R3 and R4 are each as defined above, and symbol .......... represents either a single or a double bond, provided that at least one of R1, R3 and R5 represents hydroxy, carboxy or amino.

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