Title:
【発明の名称】ベンゾシクロアルケニルジヒドロキシアルカン酸化合物、その製造方法及びそれを含有する医薬組成物
Document Type and Number:
Japanese Patent JP2561354
Kind Code:
B2
Abstract:
Derivatives of benzocycloalkenyldihydroxyalkanoic acids, inhibitors of HMG CoA reductase, antagonists of thromoboxane A2 receptors and antifungals, denoted by the formula I 1 in which X=CH2, O or S; R1 and R2, identical or different, =H, C1-3 alkyl or together from a -(CH2)n- chain (n=4,5) optionally substituted symmetrically by one or two C1-3 alkyl radicals. R3 and R4, identical or different, =H, CF3, halogen (Cl, F, Br), C1-5 N,N-dialkylamino, C1-4 alkyl, C1-5-alkoxy, C1-3 alkylthio, or phenyl optionally substituted by at most two substitutents which may be identical or different and may denote C1-3 alkyl or C1-3 alkoxy radicals or halogens (F, Cl), it being understood that when one of R3 and R4 denotes the radicals: CF3, N,N-dialkylamino, C6H5 or substituted phenyl, it is present at the vertices 3', 4'or 5' according to formula 1 and the other denotes a hydrogen atom. R5 and R6, (which may be identical or different)=H, halogen (F, Cl, Br), CF3, C1-3 alkyl, C1-3 alkoxy, C6H5, optionally substituted by at most two substitutents which may be identical or different and may denote radicals: C1-3 alkyl or C1-3 alkoxy or halogen atoms (F, Cl), on condition that when one of R5 and R6=CF3, C6H5 or substituted phenyl, it is present at the vertex 6 or 7 and the other denotes a hydrogen atom. The substitutents R3 and R4 or R5 and R6 may also together form, on condition of being at two contiguous vertices, diradicals of formulae: -CH=CH-CH=CH-, -(CH2)m- and -O(CH2)pO-, in which m=3 or 4, p=1 or 2, it being understood that when R3 and R4 or R5 and R6 form the chain sequence -O(CH2)pO-, the latter is linked to the vertices 3' and 4' or 4' and 5' or 6 and 7 according to the formula 1. R7 and R8=H or, together with the existing C-C bond, form a double bond of trans geometry; R9 and R10=H or together form a C1-3 dialkylmethylene residue. In the form of free acids, salts, esters, amides or delta -lactones. Hypocholesterolaemiant, antithrombotic and antifungal medications containing them.
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Inventors:
DEIDEIE FUESUTARU
JANNIBE NIOSHU
DENISU DESUKUURU
ROBERU BERUMAN
JATSUKU DESERUPURITSUTO
JANNIBE NIOSHU
DENISU DESUKUURU
ROBERU BERUMAN
JATSUKU DESERUPURITSUTO
Application Number:
JP1274690A
Publication Date:
December 04, 1996
Filing Date:
January 24, 1990
Export Citation:
Assignee:
RIFUA RYONEEZU IND FUARUMASUTEIIKU
International Classes:
A61K31/19; A61K31/215; A61K31/35; A61K31/352; A61K31/38; A61K31/382; A61K31/47; A61K31/16; A61K31/473; A61P3/06; A61P7/02; A61P9/00; A61P31/10; C07C17/10; C07C17/12; C07C23/18; C07C25/22; C07C33/28; C07C33/48; C07C35/23; C07C35/52; C07C43/20; C07C43/305; C07C45/29; C07C45/46; C07C45/57; C07C45/68; C07C47/238; C07C47/24; C07C47/277; C07C47/453; C07C47/457; C07C47/47; C07C49/67; C07C57/30; C07C59/48; C07C59/54; C07C59/56; C07C59/64; C07C67/31; C07C69/732; C07C69/734; C07C215/70; C07C217/76; C07C223/06; C07C229/40; C07C235/06; C07C235/32; C07C323/09; C07C323/18; C07C323/22; C07C323/62; C07D215/14; C07D215/18; C07D215/20; C07D221/08; C07D221/10; C07D221/20; C07D309/30; C07D311/04; C07D311/58; C07D311/96; C07D333/50; C07D335/04; C07D335/06; C07D407/06; C07D409/06; (IPC1-7): C07C59/54; A61K31/38; C07C69/732; C07C69/734; C07D311/96; C07D315/00; C07D335/06
Other References:
【文献】 米国特許4556676(US,A)
【文献】 欧州出願公開298466(EP,A2)
【文献】 欧州出願公開230270(EP,A2)
【文献】 Tetrahedron(1987年)第43巻第12号第2853~2871頁
【文献】 Chem Lett(1986年)第5号第759~762頁
【文献】 Izv.Akad.Nauk SSSR,Ser.Khim(1975年)第2号第374~380頁
【文献】 欧州出願公開298466(EP,A2)
【文献】 欧州出願公開230270(EP,A2)
【文献】 Tetrahedron(1987年)第43巻第12号第2853~2871頁
【文献】 Chem Lett(1986年)第5号第759~762頁
【文献】 Izv.Akad.Nauk SSSR,Ser.Khim(1975年)第2号第374~380頁
Attorney, Agent or Firm:
Shigeru Yagita (2 outside)