Patent SG-11201407837W-A (SG)
Title: Beta-hairpin peptidomimetics
Inventor: GOMBERT FRANK OTTO
IPC: C07K7/64
Filed: 2012-06-06
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 12 December 2013 (12.12.2013) WIPOIPCT (10) International Publication Number WO 2013/182240 A1 (51) International Patent Classification: C07K 7/64 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/EP2012/060766 6 June 2012 (06.06.2012) English English (71) Applicant (for all designated States except US): POLY- PHOR AG; Hegenheimermattweg 125, CH-4123 All- schwil (CH). (72) Inventors; and (75) Inventors/Applicants (for US only)-. GOMBERT, Frank Otto [DE/CH]; Dornacherstrasse 120, CH-4053 Basel (CH). OBRECHT, Daniel [CH/CH]; Im Eichacker 21, CH-4112 Battwil (CH). LEDERER, Alexander [DE/CH]; Schillerstrasse 10, CH-4053 Basel (CH). ZIMMER- MANN, Johann [DE/DE]; Oberdorfstrasse 8, 79424 Aug- gen (DE). OEFNER, Christian [DE/DE]; Miihlewinkel 3, 79108 Freiburg (DE). (74) Agent: BRAUN, Andre; Reusstrasse 22, CH-4054 Basel (CH). (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, 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, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, 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. (84) Designated States (unless otherwise indicated, for every kind of regional protection available)'. ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, 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, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG). Published: — with international search report (Art. 21(3)) © •t CJ CJ oo i-H cn i-H o CJ o & (54) Title: BETA-HAIRPIN PEPTIDOMIMETICS (57) Abstract: (3-Hairpin peptidomimetics of the general formula cyclo(-Tyr -His -Xaa -Cys -Ser -Xaa -DPro -Xaa -Arg -Tyr - 1 2 3 4 5 6 7 8 9 10 Cys -Tyr -Xaa -Xaa -Xaa -Pro -), disulfide u 12 13 14 15 16 bond between Cys 4 and Cys , 11 and pharmaceutically acceptable salts thereof, with Xaa , Xaa , Xaa , Xaa , 3 6 8 13 Xaa 14 and Xaa 15 being amino acid residues of certain types which are defined in the description and the claims, have favorable pharmacological properties and can be used for preventing HIV infections in healthy individuals or for slow - ing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immunosuppression; or dur­ ing apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells regulate to tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid-and solution phase synthetic strategy.