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1. WO1996026925 - ARYLTHIOACETAMIDE DERIVATIVES

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Publication Number WO/1996/026925
Publication Date 06.09.1996
International Application No. PCT/JP1996/000412
International Filing Date 23.02.1996
Chapter 2 Demand Filed 18.09.1996
IPC
C07D 213/75 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72Nitrogen atoms
75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C07D 239/58 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02not condensed with other rings
24having three or more double bonds between ring members or between ring members and non-ring members
28with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46Two or more oxygen, sulfur or nitrogen atoms
58Two sulfur atoms
CPC
C07D 213/75
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72Nitrogen atoms
75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C07D 239/58
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02not condensed with other rings
24having three or more double bonds between ring members or between ring members and non-ring members
28with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46Two or more oxygen, sulfur or nitrogen atoms
58Two sulfur atoms
Applicants
  • BANYU PHARMACEUTICAL CO., LTD. [JP]/[JP] (AllExceptUS)
  • ISHIKAWA, Kiyofumi [JP]/[JP] (UsOnly)
  • HAYAMA, Takashi [JP]/[JP] (UsOnly)
  • KAMEI, Toshio [JP]/[JP] (UsOnly)
  • NAGATA, Yasufumi [JP]/[JP] (UsOnly)
Inventors
  • ISHIKAWA, Kiyofumi
  • HAYAMA, Takashi
  • KAMEI, Toshio
  • NAGATA, Yasufumi
Priority Data
7/15217326.05.1995JP
7/6526301.03.1995JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) ARYLTHIOACETAMIDE DERIVATIVES
(FR) DERIVES DE L'ARYLTHIOACETAMIDE
Abstract
(EN)
Arylthioacetamide derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof, wherein Ar represents phenyl, naphthyl or pyridyl optionally having one to four substituents selected from the group consisting of lower alkyl, lower alkoxy and halogeno; R1 represents hydrogen or lower alkyl; R2 and R3 may be the same or different and each represents hydrogen, lower alkyl, lower alkoxy, lower alkylthio, mono(lower alkyl)amino or di(lower alkyl)amino, provided that the lower alkyl, lower alkoxy, lower alkylthio, mono(lower alkyl)amino or di(lower alkyl)amino may be substituted by pyrrolidino, etc. at arbitrary hydrogen atoms; n represents 0, 1 or 2; and X represents CH or N. The compounds inhibit ACAT to thereby suppress the formation of cholesterol esters, are expected to be usable as a remedy or preventive for hypercholesterolemia, hyperlipidemia, arteriosclerosis and cardiac diseases, etc. accompanying the same.
(FR)
Dérivés de l'arylthioacétamide représentés par la formule générale (I) ou ses sels, compatibles sur le plan pharmaceutique. Dans cette formule, Ar correspond à phényle, naphtyle ou pyridyle ayant éventuellement un à quatre substituts choisis dans le groupe constitué d'alkyle inférieur, alcoxy inférieur et d'halogéno; R1 correspond à hydrogène ou à alkyle inférieur; R2 et R3 peuvent être les mêmes ou être différents et chacun correspond à hydrogène, alkyle inférieur, alcoxy inférieur, alkylthio, mono(alkyle inférieur)amino ou di(alkyle inférieur)amino, à condition qu'alkyle inférieur, alcoxy inférieur, alkylthio inférieur, mono(alkyle inférieur)amino ou di(alkyle inférieur)amino puissent être substitués par pyrrolidino, etc. sur n'importe quel atome d'hydrogène; n correspond à 0, 1 ou 2; et X correspond à CH ou N. Les composés, qui inhibent l'ACAT afin de supprimer la formation d'esters de cholesterol, devraient pouvoir être utilisés comme agent thérapeutique ou prophylactique dans l'hypercholestérolémie, l'hyperlipémie, l'artériosclérose et les maladies cardiovasculaires associées.
Also published as
JPWO1996026925
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