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1. (WO2017063755) CONFORMATIONALLY CONSTRAINED MACROCYCLIC COMPOUNDS
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2017/063755 International Application No.: PCT/EP2016/025111
Publication Date: 20.04.2017 International Filing Date: 12.10.2016
IPC:
C07D 498/18 (2006.01) ,A61K 31/429 (2006.01) ,A61P 35/00 (2006.01)
Applicants: POLYPHOR AG[CH/CH]; Hegenheimermattweg 125 CH-4123 Allschwil, CH
Inventors: OBRECHT, Daniel; CH
ERMERT, Philipp; CH
Agent: POLYPHOR AG; Hegenheimermattweg 125 4123 Allschwil, CH
Priority Data:
15002907.212.10.2015EP
Title (EN) CONFORMATIONALLY CONSTRAINED MACROCYCLIC COMPOUNDS
(FR) COMPOSÉS MACROCYCLIQUES À CONFORMATION LIMITÉE
Abstract: front page image
(EN) Formula (I); Conformationally constrained macrocyclic compounds of formula (I), including substituents E with at least one ester moiety, G and Q, as defined in the description and the claims, and salts thereof, can be metabolized to compounds that have the property to modulate the activity of the peptidyl-prolyl cis/trans isomerase Pin1. In addition, they show antiproliferative activity on various cancer cell lines. Thus, these compounds and pharmaceutical compositions containing said compounds may be useful in the treatment and/or prevention of diseases or conditions in the area of proliferative disorders and diseases, such as e.g. cancer, inflammatory diseases, transplant rejection, viral infections, osteolytic bone diseases, cardiac diseases, cardiovascular diseases, respiratory diseases, acute neurological diseases, neurodegenerative diseases, immune disorders, and lymphoproliferative theileriosis.
(FR) Formule (I); L'invention concerne des composés macrocycliques à conformation limitée de formule (I), y compris les substituants E avec au moins une fraction ester, G et Q, tels que définis dans la description et les revendications, et leurs sels, lesdits composés pouvant être métabolisés en composés ayant la propriété de moduler l'activité des peptidyl-prolyl cis/trans isomérases Pin1. Ils présentent par ailleurs une activité anti-proliférative sur diverses lignées de cellules cancéreuses. Ces composés et ces compositions pharmaceutiques contenant lesdits composés peuvent être utiles pour traiter et/ou prévenir les maladies ou les pathologies relevant du domaine des affections et des maladies prolifératives, comme le cancer, les maladies inflammatoires, le rejet de greffe, les infections virales, les maladies osseuses ostéolytiques, les maladies cardiaques, les maladies cardiovasculaires, les maladies respiratoires, les maladies neurologiques aiguës, les maladies neurodégénératives, les maladies immunitaires et la theilériose lymphoproliférative.
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, JP, KE, KG, 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)