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1. (WO2010072315) AMINO ACID ESTER PRODRUGS AND THE USE THEREOF
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/072315 International Application No.: PCT/EP2009/008618
Publication Date: 01.07.2010 International Filing Date: 03.12.2009
IPC:
C07D 413/12 (2006.01) ,A61K 31/4439 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
4439
containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
Applicants:
BAYER SCHERING PHARMA AKTIENGESELLSCHAFT [DE/DE]; Müllerstr. 178 13353 Berlin, DE (AllExceptUS)
MEIBOM, Daniel [DE/DE]; DE (UsOnly)
LERCHEN, Hans-Georg [DE/DE]; DE (UsOnly)
VAKALOPOULOS, Alexandros [GR/DE]; DE (UsOnly)
ALBRECHT-KÜPPER, Barbara [DE/DE]; DE (UsOnly)
NELL, Peter [DE/DE]; DE (UsOnly)
KELDENICH, Jörg [DE/DE]; DE (UsOnly)
ZIMMERMANN, Katja [DE/DE]; DE (UsOnly)
KRENZ, Ursula [DE/DE]; DE (UsOnly)
Inventors:
MEIBOM, Daniel; DE
LERCHEN, Hans-Georg; DE
VAKALOPOULOS, Alexandros; DE
ALBRECHT-KÜPPER, Barbara; DE
NELL, Peter; DE
KELDENICH, Jörg; DE
ZIMMERMANN, Katja; DE
KRENZ, Ursula; DE
Common
Representative:
BAYER SCHERING PHARMA AKTIENGESELLSCHAFT; Law and Patents Patents and Licensing 51368 Leverkusen, DE
Priority Data:
10 2008 062 566.316.12.2008DE
Title (DE) AMINOSÄUREESTER-PRODRUGS UND IHRE VERWENDUNG
(EN) AMINO ACID ESTER PRODRUGS AND THE USE THEREOF
(FR) PROMÉDICAMENTS D'ESTERS D'ACIDES AMINÉS ET LEUR UTILISATION
Abstract:
(DE) Die vorliegende Anmeldung betrifft Aminosäureester-Prodrυg-Derivate von 2-Amino-6-({[2-(4-chlorphenyl)-1,3-oxazol-4-yl]methyl}sulfanyl)4-(4-{[,3-dihydroxypropyl]oxy}phenyl)pyridin- 3,5-dicarbonitrilen der Formel (I), in welcher RA für Wasserstoff oder Methyl steht und R PD für eine Gruppe der Formel (II) oder (III) steht, worin # die Verknüpfungsstelle mit dem jeweiligen O-Atom bedeutet, Verfahren zu ihrer Herstellung, ihre Verwendung zur Behandlung und/oder Prophylaxe von Krankheiten sowie ihre Verwendung zur Herstellung von Arzneimitteln zur Behandlung und/oder Prophylaxe von Krankheiten, insbesondere von kardiovaskulären Erkrankungen.
(EN) The invention relates to amino acid ester prodrug derivatives of 2-amino-6-({[2-(4-chlorphenyl)-1,3-oxazol-4-yl]methyl}sulfanyl)4-(4-{[2,3-dihydroxypropyl]oxy}phenyl)pyridine- 3,5-dicarbonitriles of formula (I), where RA is hydrogen or methyl, and RPD is a group of the formulas (II) or (III), wherein # is the linking site having each O atom, to a method for the production thereof, to the use thereof for treating and/or preventing illnesses, and to the use thereof for producing pharmaceuticals for treating and/or preventing illnesses, particularly of cardiovascular diseases.
(FR) La présente invention concerne des dérivés promédicamenteux d'esters d'acides aminés, à savoir des dérivés promédicamenteux de 2-amino-6-([2-(4-chlorphényl)-1,3-oxazol-4-yl]méthylsulfanyl)4-(4-[2,3-dihydroxypropyl]oxyphényl)pyridin-3,5-dicarbonitrile de la formule (I) dans laquelle RA représente de l'hydrogène ou du méthyle et R PD un groupe de la formule (II) ou (III) où # représente le point de liaison avec l'atome O, son procédé de production, son utilisation pour le traitement et/ou la prophylaxie de maladies ainsi que son utilisation pour la fabrication de médicaments pour le traitement et/ou la prophylaxie de maladies, notamment de maladies cardiovasculaires.
front page image
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: German (DE)
Filing Language: German (DE)
Also published as:
EP2379539JP2012512203US20110237629CA2746727