Patent SG-11201806388X-A (SG)
Title: C-3 and c-17 modified triterpenoids as hiv-1 inhibitors
Inventor: CHEN JIE
IPC: C12N9/50
Filed: 2017-02-02
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2017/134596 Al 10 August 2017 (10.08.2017) WIPO I PCT 11111111111111011101111111111101011111011101110111111111111111011111111111111110111111 W O 20 17 / 13 4596 Al (51) International Patent Classification: C07J 63/00 (2006.01) A61K 31/56 C12N 9/50 (2006.01) A61K 31/58 A61K 31/575 (2006.01) A61P 31/18 (21) International Application Number: PCT/IB2017/050568 (22) International Filing Date: 2 February 2017 (02.02.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/291,298 4 February 2016 (04.02.2016) US (71) Applicant: VIIV HEALTHCARE UK (NO.5) LIMITED [GB/GB]; 980 Great West Road, Brentford Middlesex TW89GS (GB). (72) Inventors: CHEN, Jie; 5 Research Parkway, Wallingford, Connecticut 06492 (US). CHEN, Yan; 5 Research Park- way, Wallingford, Connecticut 06492 (US). DICKER, Ira B.; 5 Research Parkway, Wallingford, Connecticut 06492 (US). HARTZ, Richard A; 5 Research Parkway, Walling- ford, Connecticut 06492 (US). MEANWELL, Nicholas A; 5 Research Parkway, Wallingford, Connecticut 06492 (US). (72) Inventor: NOWICKA-SANS, Beata (deceased). (72) Inventors: REGUEIRO-REN, Alicia; 5 Research Park- way, Wallingford, Connecticut 06492 (US). SIT, Sing- Yuen; 5 Research Parkway, Wallingford, Connecticut 06492 (US). SIN, Ny; 5 Research Parkway, Wallingford, Connecticut 06492 (US). SWIDORSKI, Jacob; 5 Re- search Parkway, Wallingford, Connecticut 06492 (US). VENABLES, Brian Lee; 5 Research Parkway, Walling- ford, Connecticut 06492 (US). (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, 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, ST, 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, KM, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.1700) as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) Published: with international search report (Art. 21(3)) before the expiration of the time limit for amending the claims and to be republished in the event of receipt of amendments (Rule 48.2(h)) (2006.01) (2006.01) (2006.01) — (54) Title: C-3 AND C-17 MODIFIED TRITERPENOIDS AS HIV-1 INHIBITORS (I) (57) : Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as rep - resented by compounds of Formula (I). These compounds are useful for the treatment of HIV and AIDS.