Agarofuan derivatives, their preparation, pharmaceutical composition containing them and their use as medicine
AssigneeInstitute of Materia Medica, Chinese Academy of Medical Science (CN)
InventorsJiyu Guo, Weijun Wang, Hongju Fang, Qian Liu, Wuyan Zhang, Dali Yin, Sujuan Sun, Ruiwu Liu, Chun Li, Haifan Liu, Donghui Wang
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Abstract
The compound represented by formula (I), in which the substitutes are defined as in the specification and the claims, or their stereoisomers, the process for preparing them, pharmaceutical composition containing them and their use as medicine.
Claims19
A compound of formula (I),
- wherein a double bond is present at position 2-3 of the A ring,
- R1 is located at position 2 or 3 of the A ring and is a C2-6 straight or branched chain alkyl wherein said alkyl is optionally substituted with hydroxyl, carbonyl, benzyl, or halogen-substituted benzyl, and
- R2 and R3 are hydrogen;
- or stereoisomers thereof.
A method for the treatment of anxiety and/or depression, comprising administering at least one compound of formula (I),
- wherein a double bond is present at position 2-3 of the A ring,
- R1 is located at position 2 or 3 of the A ring and is a C2-6 straight or branched chain alkyl wherein said alkyl is optionally substituted with hydroxyl, carbonyl, benzyl, or halogen-substituted benzyl, and
- R2 and R3 are hydrogen;
- or stereoisomers thereof, in effective amount for treatment of anxiety and/or depression to mammals.
A method for the treatment of anxiety and/or depression, comprising administering a composition comprising at least one compound of formula (I),
- wherein a double bond is present at position 2-3 of the A ring,
- R1 is located at position 2 or 3 of the A ring and is a C2-6 straight or branched chain alkyl wherein said alkyl is optionally substituted with hydroxyl, carbonyl, benzyl, or halogen-substituted benzyl, and
- R2 and R3 are hydrogen;
- or stereoisomers thereof;
- as an active ingredient, and a conventional pharmaceutical carrier or excipient in effective amount for treatment of anxiety and/or depression to mammals.
A process of preparation of compound of formula (Ia)
- wherein R1 is butyl;
- or stereoisomers thereof, comprising
- (i) reacting compound of formula (1) with R1X in basic medium and organic solvent
- wherein R1 is butyl and X is a halogen,
- to form compounds of formula (2)
- (ii) reaction of compound of formula (2) obtained from (i) with organic peracid to form compound of formula (3),
- (iii) reduction of compound of formula (3) with reducing agent to form compounds of formula (4),
- (iv) cyclization of compound of formula (4) in acidic medium to produce compound of formula (Ia).
Dependencies are inferred from the claim text.