5-HT3 RECEPTOR AGONIST, NOVEL THIAZOLE DERIVATIVE, AND INTERMEDIATE THEREFOR

WIPO Patent Application WO/1995/024399

A1

A 5-HT3 receptor agonist containing a thiazole derivative represented by general formula (I) as the active ingredient, a specified compound useful as a 5-HT3 receptor agonist, and a specified thioamide derivative useful as an intermediate therefor, wherein ring A represents one of the following rings which may be substituted by at least one substituent selected from the group consisting of halogen, lower alkyl and lower alkoxy: (1) a benzene ring, and (2) a 5- or 6-membered unsaturated heterocycle having one or two heteroatoms selected from among nitrogen, oxygen and sulfur; one of L1 and L2 represents a single bond, and the other of them is absent, or represents C1-C4 alkylene or C2-C5 alkenylene; R represents a group represented by any of general formulae: (1), (2), (3) and (4); L3 represents lower alkylene; L4 represents a single bond or lower alkylene; R1 and R2 represent each independently hydrogen, lower alkyl or an amino-protecting group; R3 represents hydrogen, lower alkyl, oxo or optionally protected amino; R4 is absent, or represents hydrogen, lower alkyl, aralkyl or an amino-protecting group; ring B represents one of the following rings which are either monocyclic or bicyclic and may bear an oxygen atom(s): (1) a nitrogenous saturated heterocycle bearing four to sixteen ring atoms, and (2) a nitrogenous heterocycle having a double bond and bearing four to sixteen ring atoms: and ring D represents a saturated carbocycle bearing four to eight ring atoms; provided the nitrogen atom of R may form an unsubstituted quaternary ammonium salt.

JPH0830060	INDUSTRIAL APPLICABILITY: Heterocyclic primary amine diselenobis benzoic acid, a method for producing the same, and a drug containing the same.
WO/2004/000785	PHENYLOXYALKANONIC ACID DERIVATIVES AS HPPAR ACTIVATORS
WO/2000/007997	IMIDAZOLES AND RELATED COMPOUNDS AS $g(a)¿1A? AGONISTS

IWAOKA KIYOSHI (JP)
ANAN HIDEKI (JP)
IMANISHI NAOKI (JP)
KAZUTA KENICHI (JP)
KOSHIO HIROYUKI (JP)
SUZUKI TAKESHI (JP)
ITAHANA HIROTSUNE (JP)
ITO HIROYUKI (JP)
MIYATA KEIJI (JP)
OHTA MITSUAKI (JP)

PCT/JP1995/000385

September 14, 1995

March 09, 1995

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YAMANOUCHI PHARMA CO LTD (JP)
IWAOKA KIYOSHI (JP)
ANAN HIDEKI (JP)
IMANISHI NAOKI (JP)
KAZUTA KENICHI (JP)
KOSHIO HIROYUKI (JP)
SUZUKI TAKESHI (JP)
ITAHANA HIROTSUNE (JP)
ITO HIROYUKI (JP)
MIYATA KEIJI (JP)
OHTA MITSUAKI (JP)

C07D277/28; C07D277/60; C07D417/04; C07D417/06; C07D417/14; C07D471/04; C07D471/08; C07D487/04; C07D487/08; C07D513/04; C07D519/00; (IPC1-7): C07D277/28; C07D277/60; C07D277/84; C07D417/04; C07D417/06; C07D417/14; C07D513/04; A61K31/425; A61K31/435; A61K31/445; A61K31/535

WO1993002677A1	1993-02-18
WO1992007849A1	1992-05-14

JPH01268687A

1989-10-26

See also references of EP 0749966A4

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