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1. (WO2015121836) COMPLEXES OF SIROLIMUS AND ITS DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2015/121836 International Application No.: PCT/IB2015/051086
Publication Date: 20.08.2015 International Filing Date: 13.02.2015
IPC:
A61K 9/16 (2006.01) ,A61K 47/10 (2006.01) ,A61K 47/20 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
14
Particulate form, e.g. powders
16
Agglomerates; Granulates; Microbeadlets
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
06
Organic compounds
08
containing oxygen
10
Alcohols; Phenols; Salts 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
06
Organic compounds
20
containing sulfur
Applicants:
DRUGGABILITY TECHNOLOGIES IP HOLDCO LIMITED [IE/MT]; Tower Business Centre, Tower Street Swatar, BKR 4013, MT
Inventors:
ANGI, Erzsébet Réka; HU
SOLYMOSI, Tamás; HU
KÁRPÁTI, Richard Balázs; HU
FENYVESI, Zsófia; HU
ÖTVÖS, Zsolt; HU
MOLNÁR, László; HU
GLAVINAS, Hristos; HU
FILIPCSEI, Genovéva; HU
FERENCZI, Katalin; HU
HELTOVICS, Gábor; HU
Agent:
DR. MOLNÁR, István; HU
Priority Data:
P140007514.02.2014HU
Title (EN) COMPLEXES OF SIROLIMUS AND ITS DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
(FR) COMPLEXES DE SIROLIMUS ET LEUR DÉRIVÉS, LEUR PROCÉDÉ DE PRÉPARATION ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT
Abstract:
(EN) The invention is directed to a stable complex with controlled particle size, increased apparent solubility and increased dissolution rate comprising as active compound Sirolimus or derivatives thereof, which is useful in in the prophylaxis of organ rejection in patients receiving renal transplants, in the treatment of psoriasis, facial angiofibromas associated with tuberous sclerosis, fibrofolliculomas found in Birt-Hogg-Dubé Syndrome, chronic erosive oral lichen planus, Early Stage Cutaneous T-cell Lymphoma, Treatment of Autoimmune Active Anterior Uveitis, dry eye syndrome, age-related macular degeneration, diabetic macular edema, noninfectious uveitis, telangiectasia, inflammatory skin diseases (dermatitis, including psoriasis and lichen ruber planus), Pachyonychia Congenita and in the suppression of angiogenesis pathways. More specifically, the complex of the present invention possesses increased apparent solubility, permeability and enhanced biological performance including significantly improved exposure, earlier tmax, higher Cmax and higher trough concentrations at 24 hours which will allow the reduction of the dose. Furthermore, the complex of the present invention possesses exceptional stability as a redispersed solution allowing the development of liquid based formulation for transdermal and other topical applications. The invention also relates to methods of formulating and manufacturing complex according to the invention, pharmaceutical compositions containing it, its uses and methods of treatment using the complex and its compositions.
(FR) L'invention concerne un complexe stable présentant une taille particulaire contrôlée, une solubilité apparente accrue et une vitesse de dissolution accrue, comprenant à titre de composé actif le sirolimus ou des dérivés de celui-ci, qui est/sont utile(s) dans la prophylaxie du rejet d'organe chez des patients recevant des transplantations rénales, dans le traitement du psoriasis, des angiofibromes faciaux associés à la sclérose tubéreuse, des fibrofolliculomes du syndrome de Birt-Hogg-Dubé, du lichen plan buccal inflammatoire chronique, du lymphome T cutané à un stade précoce, le traitement de l'uvéite active antérieure auto-immune, du syndrome de l'oeil sec, de la dégénérescence maculaire liée à l'âge, de l'oedème maculaire diabétique, de l'uvéite non infectieuse, de la télangiectasie, des maladies cutanées inflammatoires (la dermatite, notamment le psoriasis et le lichen plan), de la pachyonychie congénitale et dans la suppression des voies de l'angiogenèse. De manière plus spécifique, le complexe de l'invention possède une solubilité et une perméabilité apparentes accrues, et une performance biologique améliorée notamment une exposition significativement améliorée, un tmax plus précoce, un Cmax supérieur et des concentrations minimales plus élevées à 24 heures, ce qui permet de réduire la dose. En outre, le complexe de l'invention présente une stabilité exceptionnelle en tant que solution redispersée permettant de développer des formulations à base de liquide pour des applications topiques et autres applications transdermiques. L'invention concerne également des procédés pour formuler et fabriquer un complexe selon l'invention, des compositions pharmaceutiques le contenant, ses utilisations et des procédés de traitement utilisant le complexe et ses compositions.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, 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, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, 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, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, 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, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)