PYRROLOTHIAZINE AND PYRROLOTHIAZEPINE COMPOUNDS HAVING SEROTONIN-2 RECEPTOR ANTAGONISTIC AND ALPHA1-BLOCKING ACTION

WIPO Patent Application WO1999033840

A3

A pyrrolesulfonamide derivative having formula (I) wherein the ring P represented by alpha is a pyrrole ring having structure beta or psi wherein R represents alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H but, when the bond is absent, Z1 represents H and Z2 represents OH or Z1 and Z2 are combined together to represent O or a group NOR1, in which R1 represents H, or alkyl, aralkyl or aryl; stands for 0 or 1; A represents alkylene, alkenylene or alkynylene; and Y represents a group delta in which W represents CH, C= or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is C=; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group. The compound (I) has strong serotonin-2 receptor antagonistic action and low toxicity and less side effects, and is useful as a therapeutic for circulatory diseases such as ischemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.

WO/2003/053912	$g(a)-(N-SULPHONAMIDO)ACETAMIDE DERIVATIVES AS $g(b)-AMYLOID INHIBITORS
JPH08157321	COSMETIC
JP3187535	MEDICINALLY ACTIVE HYDRAZINE DERIVATIVE AND ITS PRODUCTION

MIZUNO AKIRA (JP)
SHIBATA MAKOTO (JP)
KAMEI TOMOE (JP)
FUKAMI HARUKAZU (JP)
INOMATA NORIO (JP)

PCT/JP1998/005954

September 10, 1999

December 25, 1998

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SUNTORY LTD (JP)
MIZUNO AKIRA (JP)
SHIBATA MAKOTO (JP)
KAMEI TOMOE (JP)
FUKAMI HARUKAZU (JP)
INOMATA NORIO (JP)

A61K31/54; A61K31/55; A61P9/00; A61P9/02; A61P9/06; A61P9/08; A61P9/10; A61P9/12; A61P43/00; C07D207/36; C07D513/04; (IPC1-7): C07D513/04; A61K31/54; A61K31/55

EP0807632A1	1997-11-19
EP0511073A1	1992-10-28
EP0686632A1	1995-12-13

CHEMICAL ABSTRACTS, vol. 44, no. 3, 10 February 1950, Columbus, Ohio, US; abstract no. 1095i, TERENT'EV A P ET AL: "Sulfonation and sulfonic acids of acidophobic substances. VI. Sulfonation of alpha,alpha'- substituted pyrrole homologs." XP002098315

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