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1. (WO1997015550) FLUORO-SUBSTITUTED BENZOYLPROPIONIC ACID DERIVATIVES
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/015550 International Application No.: PCT/EP1996/004321
Publication Date: 01.05.1997 International Filing Date: 04.10.1996
Chapter 2 Demand Filed: 15.03.1997
IPC:
C07C 229/36 (2006.01) ,C07C 237/20 (2006.01) ,C07C 259/06 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
229
Compounds containing amino and carboxyl groups bound to the same carbon skeleton
02
having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
34
the carbon skeleton containing six-membered aromatic rings
36
with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
237
Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
02
having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
20
the carbon skeleton containing six-membered aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
259
Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
04
without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
06
having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
Applicants:
PHARMACIA & UPJOHN S.P.A. [IT/IT]; Via Robert Koch, 1.2 I-20152 Milan, IT (AllExceptUS)
VARASI, Mario [IT/IT]; IT (UsOnly)
GIORDANI, Antonio [IT/IT]; IT (UsOnly)
SPECIALE, Carmela [IT/IT]; IT (UsOnly)
CINI, Massimo [IT/IT]; IT (UsOnly)
BIANCHETTI, Alberto [IT/IT]; IT (UsOnly)
Inventors:
VARASI, Mario; IT
GIORDANI, Antonio; IT
SPECIALE, Carmela; IT
CINI, Massimo; IT
BIANCHETTI, Alberto; IT
Priority Data:
9521486.220.10.1995GB
Title (EN) FLUORO-SUBSTITUTED BENZOYLPROPIONIC ACID DERIVATIVES
(FR) DERIVES DE L'ACIDE BENZOYLPROPIONIQUE SUBSTITUES PAR FLUORO
Abstract:
(EN) A fluoro-substituted benzoyl propionic acid derivative of formula (I) either as single isomer or as mixture of isomers, wherein R is hydroxy, amino, hydroxylamine, -OR', -NHR', N(R')2 or -NHOR' in which R' is C1-C6 alkyl or benzyl, or a pharmaceutically acceptable salt thereof, which act as kynurenine-3-hydroxylase enzyme inhibitor and can be useful in the treatment of neurodegenerative diseases. A process for preparing compounds of formula (I) and pharmaceutical compositions comprising them are also described.
(FR) On décrit un dérivé de l'acide benzoylpropionique substitué par fluoro, de la formule (I), ou un sel de celui-ci acceptable sur le plan pharmacologique, soit en tant qu'isomère seul, soit en tant que mélange d'isomères. Dans cette formule, R représente hydroxy, amino, hydroxylamine, -OR', -NHR', N(R')2 ou -NHOR', où R' représente alkyle C1-C6 ou benzyle. Ce dérivé agit en tant qu'inhibiteur de la kynurénine-3-hydroxylase et il peut être utile dans le traitement des maladies neurodégénératives. On décrit encore un procédé de préparation de composés de la formule (I) ainsi que des compositions pharmaceutiques comprenant ceux-ci.
Designated States: AL, AU, BB, BG, BR, BY, CA, CN, CZ, EE, GE, HU, IL, IS, JP, KP, KR, KZ, LK, LR, LT, LV, MG, MK, MN, MX, NO, NZ, PL, RO, RU, SG, SI, SK, TR, TT, UA, US, UZ, VN
African Regional Intellectual Property Organization (ARIPO) (KE, LS, MW, SD, SZ, UG)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
ES2148800EP0862551US5973006JPH11513694CA2233075DE000069608699
PT862551AU1996072852