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1. (WO2010123440) PHARMACEUTICAL COMPOSITION COMPRISING 4-AMINO-8-(2-FLUORO-6-METHOXY-PHENYL)-N- PROPYLCINNOLINE-3-CARBOXAMIDE HYDROGEN SULPHATE AND RATE-CONTROLLING POLYMER
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2010/123440 International Application No.: PCT/SE2010/050423
Publication Date: 28.10.2010 International Filing Date: 20.04.2010
IPC:
A61P 25/22 (2006.01) ,A61K 31/502 (2006.01) ,A61K 47/38 (2006.01) ,A61K 47/46 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
22
Anxiolytics
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
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
50
Pyridazines; Hydrogenated pyridazines
502
ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
30
Macromolecular compounds
36
Polysaccharides; Derivatives thereof
38
Cellulose; Derivatives thereof
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
46
Ingredients of undetermined constitution or reaction products thereof
Applicants: AVILOV, Dmytro[UA/US]; US (UsOnly)
BROWN, Daniel[US/US]; US (UsOnly)
CREEKMORE, Richard[US/US]; US (UsOnly)
REUS MEDINA, Marilu[MX/US]; US (UsOnly)
SCHULTZ, Sharon[US/US]; US (UsOnly)
SHARMA, Avadhesh[US/US]; US (UsOnly)
ASTRAZENECA AB[SE/SE]; SE-151 85 Södertälje, SE (AllExceptUS)
Inventors: AVILOV, Dmytro; US
BROWN, Daniel; US
CREEKMORE, Richard; US
REUS MEDINA, Marilu; US
SCHULTZ, Sharon; US
SHARMA, Avadhesh; US
Agent: ASTRAZENECA INTELLECTUAL PROPERTY; AstraZeneca AB SE-151 85 Södertälje, SE
Priority Data:
61/171,11421.04.2009US
Title (EN) PHARMACEUTICAL COMPOSITION COMPRISING 4-AMINO-8-(2-FLUORO-6-METHOXY-PHENYL)-N- PROPYLCINNOLINE-3-CARBOXAMIDE HYDROGEN SULPHATE AND RATE-CONTROLLING POLYMER
(FR) COMPOSITION PHARMACEUTIQUE COMPRENANT DE L'HYDROGÉNOSULFATE DE 4-AMINO-8-(2-FLUORO-6-MÉTHOXY-PHÉNYL)-N-PROPYLCINNOLINE-3-CARBOXAMIDE ET POLYMÈRE DE RÉGULATION DE LA VITESSE
Abstract:
(EN) Disclosed is a pharmaceutical composition for extended release of a cinnoline derivative in the gastrointestinal environment. The composition comprises an cinnoline derivative and a pharmaceutically acceptable polymer so that, when ingested orally, the composition induces statistically lower Cmax in the plasma than an immediate release composition of the cinnoline derivative while maintaining bioavailability and minimum concentration substantially equivalent to that of the immediate release composition of the cinnoline derivative upon multiple dosing. The compositions of the invention have reduced side effects as compared to those for the immediate release composition.
(FR) L'invention porte sur une composition pharmaceutique pour une libération prolongée d'un dérivé de cinnoline dans l'environnement gastro-intestinal. La composition comprend un dérivé de cinnoline et un polymère pharmaceutiquement acceptable de telle sorte que, lorsqu'elle est ingérée par voie orale, la composition induit une Cmax dans le plasma statistiquement inférieure à une composition à libération immédiate du dérivé de cinnoline tout en maintenant la biodisponibilité et une concentration minimale sensiblement équivalente à celle de la composition à libération immédiate du dérivé de cinnoline lors de l'administration de doses multiples. Les compositions de l'invention ont des effets secondaires réduits par comparaison à ceux pour la composition à libération immédiate.
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, 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)