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Title:
【発明の名称】脳内滞留性化合物およびその用途
Document Type and Number:
Japanese Patent JP2804177
Kind Code:
B2
Abstract:
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 R<1> 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, R<2> represents hydrogen or C1-C6 alkyl, R<3> represents hydrogen or C1-C6 alkyl which may be hydroxylated, R<4> represents hydrogen or C1-C6 alkyl, R<5> represents amino acid residue, or -S-R<6> or -CO-R<6> (wherein R<6> 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 R<1>, R<2>, R<3> and R<4> are each as defined above, and symbol ......... represents either a single or a double bond, provided that at least one of R<1>, R<3> and R<5> represents hydroxy, carboxy or amino.

Inventors:
Toyoaki Ishikura
Teruomi Ito
Takashi Kato
Kazutoshi Horie
Hiroyuki Ishihara
Keiji Senou
Application Number:
JP50387294A
Publication Date:
September 24, 1998
Filing Date:
July 30, 1993
Export Citation:
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Assignee:
DDS Research Institute Co., Ltd.
International Classes:
A61K47/20; A61K47/22; A61K47/48; C07C323/41; C07C327/30; C07D207/16; C07D239/42; C07D295/12; C07D295/13; C07D405/12; (IPC1-7): C07C323/41; A61K47/20; A61K47/22; C07D295/12
Domestic Patent References:
JP1319466A
JP5134347A
Other References:
【文献】米国特許3510480(US,A)
Attorney, Agent or Firm:
Kazuo Sato (2 outside)