Some content of this application is unavailable at the moment.
If this situation persist, please contact us atFeedback&Contact
1. (WO2018024878) METHODS AND COMPOSITIONS FOR REDUCING PCSK9 EXPRESSION
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2018/024878 International Application No.: PCT/EP2017/069779
Publication Date: 08.02.2018 International Filing Date: 04.08.2017
IPC:
A61K 31/4745 (2006.01) ,A61K 31/551 (2006.01) ,A61P 35/00 (2006.01) ,A61P 31/00 (2006.01) ,A61P 9/10 (2006.01) ,A61P 3/06 (2006.01)
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
47
Quinolines; Isoquinolines
4738
ortho- or peri-condensed with heterocyclic ring systems
4745
condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
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
55
having seven-membered rings, e.g. azelastine, pentylenetetrazole
551
having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
10
for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
06
Antihyperlipidemics
Applicants:
INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE) [FR/FR]; 101, rue de Tolbiac 75013 Paris, FR
UNIVERSITÉ PARIS DESCARTES [FR/FR]; 12, rue de l'Ecole de Médecine 75006 Paris, FR
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) [FR/FR]; 3, Rue Michel Ange 75016 Paris, FR
Inventors:
SCHARFMANN, Raphaël; FR
HUIJBREGTS, Lukas; FR
Agent:
COLLIN, Matthieu; FR
Priority Data:
16306018.905.08.2016EP
Title (EN) METHODS AND COMPOSITIONS FOR REDUCING PCSK9 EXPRESSION
(FR) PROCÉDÉS ET COMPOSITIONS POUR RÉDUIRE L'EXPRESSION DE PCSK9
Abstract:
(EN) Inventors have worked on mouse embryonic pancreatic buds and primary cultures of mouse hepatocytes. They have observed that PCSK9 mRNA steady state levels surprisingly decreased by more than 90% after 24h of treatment with IBET-151 and JQ1. Inventors have also worked with human primary hepatocytes and have shown that there is a clear dose-response inhibition of Pcsk9 expression. These results show that Ibet-151 and (+)/-JQ1 treatment may represent a novel way to increase LDLR expression and hence reduce circulating LDL levels. Accordingly, the present invention relates to a method for reducing or inhibiting PCSK9 expression in a subject in need thereof comprising a step of administering to said subject a therapeutically amount of a I-BET 151 or JQ1.
(FR) Les inventeurs ont travaillé sur des bourgeons pancréatiques embryonnaires de souris et des cultures primaires d'hépatocytes de souris. Ils ont observé que les niveaux d'état stable de l'ARNm de PCSK9 diminuent de manière surprenante de plus de 90 % après 24h du traitement par des inhibiteurs de BET-151 et JQ1. Les inventeurs ont également travaillé avec des hépatocytes primaires humains et ils ont montré qu'il existe une inhibition nette en dose-réponse de l'expression de Pcsk9. Ces résultats montrent que le traitement utilisant des inhibiteurs de BET-151 et (+)/-JQ1 peut représenter une nouvelle manière d'augmenter l'expression de récepteur au LDL (LDLR) et donc de réduire les niveaux circulants des LDL. En conséquence, la présente invention concerne un procédé pour réduire ou inhiber l'expression de PCSK9 chez un sujet en ayant besoin comprenant une étape d'administration audit sujet d'une quantité thérapeutique d'un I-BET 151 ou JQ1.
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, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, 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 Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (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)