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1. (WO2010112615) LYSINE DERIVATIVES FUNCTIONALISED WITH LIPIDS
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2010/112615 International Application No.: PCT/EP2010/054518
Publication Date: 07.10.2010 International Filing Date: 06.04.2010
IPC:
C07C 235/12 (2006.01) ,A61K 31/16 (2006.01) ,A61P 27/02 (2006.01) ,A61P 43/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
235
Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
02
having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
04
the carbon skeleton being acyclic and saturated
12
having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
16
Amides, e.g. hydroxamic acids
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27
Drugs for disorders of the senses
02
Ophthalmic agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43
Drugs for specific purposes, not provided for in groups A61P1/-A61P41/108
Applicants:
MIHOV, George [BG/NL]; NL (UsOnly)
DSM IP Assets B.V. [NL/NL]; Het Overloon 1 NL-6411 TE Heerlen, NL (AllExceptUS)
Inventors:
MIHOV, George; NL
Agent:
VANDEVIJVER, Pascale; P.O. Box 9 NL-6160 MA Geleen, NL
Priority Data:
09157325.303.04.2009EP
09165069.709.07.2009EP
Title (EN) LYSINE DERIVATIVES FUNCTIONALISED WITH LIPIDS
(FR) DÉRIVÉS DE LYSINE FONCTIONNALISÉS AVEC DES LIPIDES
Abstract:
(EN) The present invention relates to amino-acid derivatives functionalized with lipids. The amino-acid derivatives are functionalized with lipids via amide, urea or urethane bonds. The derivatives preferably have melting points in the range from 40 to 80 °C. The amino-acid derivative comprises protected lysinediisocyanate. The lipids are chosen from fatty alcohols, fatty amines, fatty acids, cholesterol or sterols. The invention also relates to a process for the preparation of amino-acid derivatives functionalized with lipids via amide, urea or urethane bonds by the reaction of a lipid with a protected lysinediisocyanate. The present invention further relates to the use of the amino acid derivatives in drug delivery.
(FR) L'invention concerne des dérivés d'acides aminés fonctionnalisés avec des lipides. Les dérivés d'acides aminés sont fonctionnalisés avec des lipides par l'intermédiaire de liaisons amide, urée ou uréthane. Ces dérivés présentent de préférence des points de fusion compris entre 40 et 80°C. Les dérivés d'acides aminés comprennent un diisocyanate de lysine protégé. Les lipides sont choisis dans le groupe comprenant des alcools gras, des amines grasses, des acides gras, du cholestérol ou des stérols. L'invention concerne aussi un procédé de préparation de dérivés d'acides aminés fonctionnalisés avec des lipides par l'intermédiaire de liaisons amide, urée ou uréthane, par la mise en réaction d'un lipide avec un diisocyanate de lysine protégé. L'invention concerne de plus l'utilisation de ces dérivés d'acides aminés dans l'apport de médicaments.
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, TH, 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, LR, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (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: English (EN)
Filing Language: English (EN)