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1. WO1999004815 - MEDICINAL COMPOSITIONS WITH CHOLESTEROL-LOWERING EFFECT

Publication Number WO/1999/004815
Publication Date 04.02.1999
International Application No. PCT/JP1998/003266
International Filing Date 22.07.1998
Chapter 2 Demand Filed 13.11.1998
IPC
A61K 31/192 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19Carboxylic acids, e.g. valproic acid
192having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
C07K 14/705 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
705Receptors; Cell surface antigens; Cell surface determinants
CPC
A61K 31/192
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic, hydroximic acids
19Carboxylic acids, e.g. valproic acid
192having aromatic groups, e.g. sulindac, 2-arylpropionic acids, ethacrynic acid
A61P 3/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
06Antihyperlipidemics
C07K 14/705
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
705Receptors; Cell surface antigens; Cell surface determinants
Applicants
  • YAMANOUCHI PHARMACEUTICAL CO., LTD. [JP]/[JP] (AL, AM, AT, AU, AZ, BA, BB, BE, BF, BG, BJ, BR, BY, CA, CF, CG, CH, CI, CM, CN, CU, CY, CZ, DE, DK, EE, ES, FI, FR, GA, GB, GE, GH, GM, GN, GR, GW, HR, HU, ID, IE, IL, IS, IT, JP, KE, KG, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MC, MD, MG, MK, ML, MN, MR, MW, MX, NE, NL, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, SN, SZ, TD, TG, TJ, TM, TR, TT, UA, UG, UZ, VN, YU, ZW)
  • SHIMOKAWA, Teruhiko [JP]/[JP] (UsOnly)
  • NISHIJIMA, Satomi [JP]/[JP] (UsOnly)
  • MATSUDA, Koyo [JP]/[JP] (UsOnly)
  • IIZUMI, Yuichi [JP]/[JP] (UsOnly)
  • HASHIMOTO, Seiichi [JP]/[JP] (UsOnly)
Inventors
  • SHIMOKAWA, Teruhiko
  • NISHIJIMA, Satomi
  • MATSUDA, Koyo
  • IIZUMI, Yuichi
  • HASHIMOTO, Seiichi
Agents
  • NAGAI, Shozo
Priority Data
9/19823224.07.1997JP
Publication Language Japanese (ja)
Filing Language Japanese (JA)
Designated States
Title
(EN) MEDICINAL COMPOSITIONS WITH CHOLESTEROL-LOWERING EFFECT
(FR) COMPOSITIONS MEDICINALES HYPOCHOLESTEROLEMIANTES
Abstract
(EN) Medicinal compositions with a cholesterol-lowering effect containing as the active ingredient compounds having the effect of activating a peroxisome proliferating agent activating receptor PPAR$g(d) or the effect of activating PPAR$g(d) or pharmaceutically acceptable salts thereof; medicinal compositions with an LDL-cholesterol-lowering effect; and a method for identifying compounds with a cholesterol-lowering effect characterized by assaying the effect of activating a peroxisome proliferating agent activating receptor PPAR$g(d) or the effect of activating PPARS$g(d) and $g(g). Means for Solution: it has been found that compounds with an excellent cholesterol-lowering effect on humans or higher organisms such as ape have the effects of activating PPAR $g(d) alone or together with PPAR $g(g). There has been established a method for identifying compounds with a cholesterol-lowering effect whereby the aimed compounds can be quickly and efficiently screened and selected from among a number of compounds by assaying the effects of activating PPAR $g(d) alone or together with PPAR $g(g).
(FR) La présente invention concerne des compositions médicinales hypocholestérolémiantes contenant en principe actif des composés dont l'effet est, soit d'activer un agent de prolifération péroxisome activant le récepteur PPAR$g(d), soit d'activer le PPAR$g(d) ou l'un de ses sels pharmaceutiquement admis. L'invention concerne également de telles compositions médicinales hypocholestérolémiantes des LDL. L'invention concerne enfin un procédé qui permet d'identifier des composés hypocholestérolémiants et qui est caractérisé en ce qu'il teste l'activation d'un agent de prolifération péroxisome activant le récepteur PPAR$g(d), l'activation du récepteur PPAR$g(d) et du PPAR$g(g). En l'occurrence, on a constaté que des composés particulièrement hypocholestérolémiants chez l'homme ou d'autres organismes supérieurs tels que le singe, ont pour effet d'activer le PPAR $g(d) seul ou en même temps que le PPAR $g(g). On a établi un procédé d'identification des composés hypocholestérolémiants permettant d'analyser rapidement les composés cibles et de les sélectionner parmi un certain nombre de composés en testant l'activation du PPAR $g(d) seul ou en même temps que le PPAR $g(g).
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