SG11201810137UA - Beta-hairpin peptidomimetic with elastase inhibitory activity and aerosol dosage forms thereof - Google Patents

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization MD 1101/110 111010101111101011111 0 0111111111111111111111111111111111111111111 International Bureau (10) International Publication Number (43) International Publication Date ......0\"\" WO 2017/207117 Al 07 December 2017 (07.12.2017) WIP0 I PCT (51) International Patent Classification: SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, A61K 8/64 (2006.01) A61K 9/00 (2006.01) TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. A61K 38/12 (2006.01) CO7K 7/64 (2006.01) (84) Designated States (unless otherwise indicated, for every (21) International Application Number: kind of regional protection available): ARIPO (BW, GH, PCT/EP2017/025156 GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, (22) International Filing Date: UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, 31 May 2017 (31.05.2017) TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, (25) Filing Language: English MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, (26) Publication Language: English TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). (30) Priority Data: 16020210.7 31 May 2016 (31.05.2016) EP Published: (71) Applicant: POLYPHOR AG [CH/CH]; Hegenheimermat- — with international search report (Art. 21(3)) tweg 125, 4123 Allschwil (CH). (72) Inventors: LUDIN, Christian; Im Drissel 24, 4104 Ober- wil (CH). KELLER, Manfred; Neunkirchner Str. 60, 81379 Mfinchen (DE). (81) Designated States (unless otherwise indicated, for every kind of national protection available): 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, 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, = Title: BETA-HAIRPIN PEPTIDOMIMETIC WITH ELASTASE INHIBITORY ACTIVITY AND AEROSOL DOSAGE FOR- = (54) = MS THEREOF = = Fig. 1 (57) : The present invention relates to pharmaceuti- cal aerosols comprising a 0-hairpin peptidomimetic of formu- la cyclo(-OctG-Glu-Thr-Ala-Ser-lle-Pro-Pro-Gln-Lys-Tyr- D Pro- = = Pro-), or a pharmaceutically acceptable salt thereof, having in- hibitory activity against human neutrophil elastase. It further re- lates to solid or liquid pharmaceutical compositions and kits for = * **** preparing and administering such aerosols. The invention can be v** -1- used for the prevention, management or treatment of pulmonary diseases, such as alpha-1 antitrypsin deficiency (AATD), cystic fi- brosis (CF), non-cystic fibrosis bronchiactasis (NCFB), or chronic — = • 1 obstructive pulmonary disease (COPD), or infections, or diseases, — 1-1 5 w or conditions of the lungs, being mediated by or resulting from human neutrophil elastase activity. Thus, the invention further re- IN lates to a pharmaceutical composition or a pharmaceutical aerosol 1-1 comprising the active compound cyclo(-OctG-Glu-Thr-Ala-Ser- 1-1 IN lle-Pro-Pro-Gln-Lys-Tyr- D Pro-Pro-), or any pharmaceutically ac- © ceptable salt thereof, for use in a method for the prevention, man- e , ' agement or treatment of diseases or conditions of the lungs being IN mediated by or resulting from human neutrophil elastase activity 1-1 0 ei Inhalation dosing in a subject. O