Title:
RECEPTOR ANTAGONIST
Document Type and Number:
WIPO Patent Application WO/2003/028732
Kind Code:
A1
Abstract:
[In the formula, p is an integer of 1 to 3&semi R1 represents a heterocyclic group, etc.&semi R2 represents −N(−R4)(−R5) (wherein R4 and R5 are the same or different and each represents hydrogen, aralkyl, etc. or R4 and R5 in cooperation with the adjacent nitrogen atom form a heterocyclic group), etc.&semi and Q represents −N=C(−R7)− (wherein R7 represents substituted amino, etc.), etc.] An adrenergic &agr 2C receptor antagonist which contains as an active ingredient a fused−ring pyrimidine derivative represented by the general formula (I) or a pharmacologically acceptable salt of the derivative is provided. The antagonist is useful in treatments for and&sol or prevention of various diseases attributable to the hyperenergia of an adrenergic &agr 2C receptor.
Inventors:
UESAKA NORIAKI (JP)
IMMA HIRONORI (JP)
KASHIMA HAJIME (JP)
KUROKAWA MASAKO (JP)
NONAKA HIROMI (JP)
KANDA TOMOYUKI (JP)
KUWANA YOSHIHISA (JP)
TOKI SHINICHIRO (JP)
SHIMADA JUNICHI (JP)
IMMA HIRONORI (JP)
KASHIMA HAJIME (JP)
KUROKAWA MASAKO (JP)
NONAKA HIROMI (JP)
KANDA TOMOYUKI (JP)
KUWANA YOSHIHISA (JP)
TOKI SHINICHIRO (JP)
SHIMADA JUNICHI (JP)
Application Number:
PCT/JP2002/009911
Publication Date:
April 10, 2003
Filing Date:
September 26, 2002
Export Citation:
Assignee:
KYOWA HAKKO KOGYO KK (JP)
UESAKA NORIAKI (JP)
IMMA HIRONORI (JP)
KASHIMA HAJIME (JP)
KUROKAWA MASAKO (JP)
NONAKA HIROMI (JP)
KANDA TOMOYUKI (JP)
KUWANA YOSHIHISA (JP)
TOKI SHINICHIRO (JP)
SHIMADA JUNICHI (JP)
UESAKA NORIAKI (JP)
IMMA HIRONORI (JP)
KASHIMA HAJIME (JP)
KUROKAWA MASAKO (JP)
NONAKA HIROMI (JP)
KANDA TOMOYUKI (JP)
KUWANA YOSHIHISA (JP)
TOKI SHINICHIRO (JP)
SHIMADA JUNICHI (JP)
International Classes:
A61K31/4196; A61K31/519; A61P3/04; A61P3/10; A61P9/12; A61P15/10; A61P25/00; A61P25/14; A61P25/16; A61P25/24; A61P43/00; C07D487/04; C07D519/00; (IPC1-7): A61K31/519; A61K31/5377; A61K31/537; A61K31/5365; A61K31/527; A61K31/5383; A61K45/00; A61P3/04; A61P3/10; A61P9/12; A61P15/10; A61P25/00; A61P25/14; A61P25/16; A61P25/24; A61P43/00; C07D487/04; C07D487/14; C07D519/00; C07D455/04
Domestic Patent References:
| WO2002039991A2 | 2002-05-23 | |||
| WO2001019371A1 | 2001-03-22 |
Foreign References:
| EP0976753A1 | 2000-02-02 |
Other References:
CHEMICAL ABSTRACTS, vol. 129, 1998, Columbus, Ohio, US; abstract no. 49522, TOMOTUKI KANDA ET AL.: "Adenosine A2A antagonist: A novel antiperkinsonian agent that does not provoke dyskinesia in parkinsonian monkeys" XP008004872
HAAPALINNA A. ET AL.: "Evaluation of the effects of a specific alpha 2-adrenoceptor antagonist, atipamezole, on alpha 1- and alpha 2-adrenoceptor subtype binding, brain neurochemistry and behavior in comparison with yohimbine", NAUNYN-SCHMIEDEBERG'S ARCH. PHARMACOL., vol. 356, no. 5, 1997, pages 570 - 582, XP002961706
GRONDIN RICHARD ET AL.: "Noradrenoceptor antagonism with idazoxan improves L-dopa-induced dyskinesias in MPTP monkeys", NAUNYN-SCHMIEDEBERG'S ARCH. PHARMACOL., vol. 361, no. 2, 2000, pages 181 - 186, XP002902470
See also references of EP 1430898A4
HAAPALINNA A. ET AL.: "Evaluation of the effects of a specific alpha 2-adrenoceptor antagonist, atipamezole, on alpha 1- and alpha 2-adrenoceptor subtype binding, brain neurochemistry and behavior in comparison with yohimbine", NAUNYN-SCHMIEDEBERG'S ARCH. PHARMACOL., vol. 356, no. 5, 1997, pages 570 - 582, XP002961706
GRONDIN RICHARD ET AL.: "Noradrenoceptor antagonism with idazoxan improves L-dopa-induced dyskinesias in MPTP monkeys", NAUNYN-SCHMIEDEBERG'S ARCH. PHARMACOL., vol. 361, no. 2, 2000, pages 181 - 186, XP002902470
See also references of EP 1430898A4
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