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1. (WO2018224736) 15.BETA.-[3-PROPANAMIDO]-SUBSTITUTED ESTRA-1,3,5(10)-TRIEN-17-ONE COMPOUNDS AND THEIR 17-OXIMES FOR USE IN INHIBITION OF 17.BETA.-HYDROXYSTEROID DEHYDROGENASES
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Pub. No.: WO/2018/224736 International Application No.: PCT/FI2018/050427
Publication Date: 13.12.2018 International Filing Date: 07.06.2018
IPC:
C07J 41/00 (2006.01) ,C07J 43/00 (2006.01) ,A61K 31/58 (2006.01) ,A61K 31/566 (2006.01) ,A61P 5/32 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
J
STEROIDS
41
Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
J
STEROIDS
43
Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
56
Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
58
containing heterocyclic rings, e.g. aldosterone, danazol, stanozolol, pancuronium, digitogenin
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
56
Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
565
not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
566
having an oxo group in position 17, e.g. oestrone
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5
Drugs for disorders of the endocrine system
24
of the sex hormones
32
Antioestrogens
Applicants:
FORENDO PHARMA LTD [FI/FI]; Itäinen Pitkäkatu 4 B 20520 Turku, FI
Inventors:
HIRVELÄ, Leena; FI
HAKOLA, Marjo; FI
LINNANEN, Tero; FI
KOSKIMIES, Pasi; FI
STJERNSCHANTZ, Camilla; FI
Agent:
KOLSTER OY AB; (Salmisaarenaukio 1) P.O.Box 204 00181 Helsinki, FI
Priority Data:
2017553008.06.2017FI
Title (EN) 15.BETA.-[3-PROPANAMIDO]-SUBSTITUTED ESTRA-1,3,5(10)-TRIEN-17-ONE COMPOUNDS AND THEIR 17-OXIMES FOR USE IN INHIBITION OF 17.BETA.-HYDROXYSTEROID DEHYDROGENASES
(FR) DÉRIVÉS STÉROÏDIENS THÉRAPEUTIQUEMENT ACTIFS
Abstract:
(EN) The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein Rl to R4 are as defined in the claims. The invention further relates to their use as inhibitors of 17P-HSD1 and in treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17P-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the compounds of formula (II) which defines the 17-ketone compounds corresponding to the 17- oximes of formula (I). The present invention further relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof.
(FR) L'invention concerne des composés de formule (I) et leurs sels pharmaceutiquement acceptables (I), formule dans laquelle R1 à R4 sont tels que définis dans les revendications. L'invention concerne en outre leur utilisation en tant qu'inhibiteurs de 17β-HSD1 et dans le traitement ou la prévention de maladies ou de troubles dépendants des hormones stéroïdes, tels que des maladies ou des troubles dépendants des hormones stéroïdes nécessitant l'inhibition de l'enzyme 17β-HSD1 et/ou l'abaissement de la concentration de l'estradiol endogène. La présente invention concerne également la préparation des composés susmentionnés et des compositions pharmaceutiques comprenant comme principe(s) actif(s) un ou plusieurs des composés ou des sels pharmaceutiquement acceptables associés susmentionnés.
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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, 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)