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1. (WO1998049124) PRODUCTION OF ENANTIOMER-FREE BIARYLKETOCARBOXYLIC ACIDS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1998/049124 International Application No.: PCT/EP1998/002176
Publication Date: 05.11.1998 International Filing Date: 14.04.1998
Chapter 2 Demand Filed: 21.10.1998
IPC:
C07B 57/00 (2006.01) ,C07C 319/28 (2006.01) ,C07C 323/56 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
B
GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
57
Separation of optically-active organic compounds
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
319
Preparation of thiols, sulfides, hydropolysulfides or polysulfides
26
Separation; Purification; Stabilisation; Use of additives
28
Separation; Purification
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
323
Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
50
containing thio groups and carboxyl groups bound to the same carbon skeleton
51
having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
56
the carbon skeleton containing six-membered aromatic rings
Applicants:
BAYER AKTIENGESELLSCHAFT [DE/DE]; D-51368 Leverkusen, DE (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, HU, ID, IE, IL, IS, IT, JP, KE, KG, KP, 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)
PREISS, Michael [DE/DE]; DE (UsOnly)
Inventors:
PREISS, Michael; DE
Agent:
BAYER AKTIENGESELLSCHAFT; D-51368 Leverkusen, DE
Common
Representative:
BAYER AKTIENGESELLSCHAFT; D-51368 Leverkusen, DE
Priority Data:
197 17 429.925.04.1997DE
Title (DE) HERSTELLUNG ENANTIOMERENREINER BIARYLKETOCARBONSÄUREN
(EN) PRODUCTION OF ENANTIOMER-FREE BIARYLKETOCARBOXYLIC ACIDS
(FR) PREPARATION D'ACIDES BIARYLCETOCARBOXYLIQUES EXEMPTS D'ENANTIOMERES
Abstract:
(DE) Gegenstand der Erfindung ist ein fortschrittliches Verfahren zur Herstellung enantiomerenreiner Biarylketocarbonsäuren, wobei als Hilfsbase bei der Racematspaltung S-Phenylethylamin eingesetzt wird. Biarylketocarbonsäuren, im besonderen substituierte Biaryl-4-ketocarbonsäuren, sind Inhibitoren für Enzyme der Klasse der Matrix-Metallo-Proteinasen. Durch Inhibition der obengenannten Enzyme können z.B. Osteoarthritis, rheumatoide Arthritis und Metastasen bekämpft werden.
(EN) The invention relates to a novel method for producing enantiomer-free biarylketocarboxylic acids, whereby S-phenylethylamine is used as an auxiliary base in racemate resolution. Biarylketocarboxylic acids, specially substituted biaryl-4-ketocarboxylic acids, are inhibitors for enzymes of the matrix-metallo-proteinase class. Osteoarthritis, rheumatoid arthritis and metastases can, for instance, be combated by inhibiting the above-mentioned enzymes.
(FR) L'invention concerne un procédé novateur permettant de préparer des acides biarylcétocarboxyliques exempts d'énantiomères, selon lequel la base auxiliaire utilisée lors du dédoublement racémique est la S-phényléthylamine. Les acides biarylcétocarboxyliques, notamment des acides biaryle-4-cétocarboxyliques substitués sont des inhibiteurs des enzymes de la catégorie des matrice-métallo-protéinases. L'inhibition des enzymes précitées permet de lutter par ex. contre l'arthrose, la polyarthrite rhumatoïde et des métastases.
Designated States: AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GE, GH, GM, GW, HU, ID, IL, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, UA, UG, US, UZ, VN, YU, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, SD, SZ, UG, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, CY, 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: German (DE)
Filing Language: German (DE)
Also published as:
CZPV1999-3748NO19994977NZ500578SK145999TR1999/02451MXPA/a/1999/009739
KR1020010020236SG68151IL132065EP0977717US6172259JP2001524102
CN1253539CA2288107AU1998075251BG103776