Patent SG-11201907058T-A (SG)
Title: Hiv inhibitor compounds
Inventor: BACON ELIZABETH M
IPC: A61K31/5365
Filed: 2018-02-05
Abstract: International Publication Date (19) World Intellectual Property Organization International Bureau (10) International Publication Number WO 2018/145021 Al onion °nolo VIII oimIE R n 1 ci R 5 IR - R - 0 OH 0 R 3 H R7 R8 (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) 09 August 2018 (09.08.2018) WIP0 I PCT (51) International Patent Classification: 94404 (US). LINK, John O.; c/o Gilead Sciences, Inc., 333 C07D 403/12 (2006.01) CO7C 243/28 (2006.01) Lakeside Drive, Foster City, CA 94404 (US). SHAPIRO, CO7D 405/14 (2006.01) A61K 31/495 (2006.01) Nathan; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Fos- C07C 275/16 (2006.01) A61K 31/504 (2006.01) ter City, CA 94404 (US). TREJO MARTIN, Teresa Ale- CO7D 401/12 (2006.01) A61K 31/506 (2006.01) j andr a ; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Fos- CO7D 471/08 (2006.01) A61K 31/5365 (2006.01) ter City, CA 94404 (US). YANG, Zheng-Yu; c/o Gilead CO7D 487/08 (2006.01) A61K 31/4155 (2006.01) Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404 CO7D 487/10 (2006.01) A61K 31/337 (2006.01) (US). CO7D 491/04 (2006.01) (74) Agent: LECHNER, Jolie D. et al.; Gilead Sciences, Inc., (21) International Application Number: PCT/US2018/016893 (22) International Filing Date: 05 February 2018 (05.02.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/455,348 06 February 2017 (06.02.2017) US (71) Applicant: GILEAD SCIENCES, INC. [US/US]; 333 Lakeside Drive, Foster City, CA 94404 (US). (72) Inventors: BACON, Elizabeth M.; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404 (US). CHIN, Elbert; c/o Gilead Sciences, Inc., 333 Lakeside Dri- ve, Foster City, CA 94404 (US). COTTELL, Jeromy J.; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404 (US). KATANA, Ashley Anne; 6599 Nancy Drive, North Olmsted, OH 44070 (US). KATO, Darryl; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 333 Lakeside Drive, Foster City, California 94404 (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, 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. (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, O 00 O O (54) Title: ATAZANAVIR (ATV) ANALOGUES FOR TREATING HIV INFECTIONS (57) : The invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof as described here- in. The invention also provides pharmaceutical compositions comprising a compound of Formula I, processes for preparing com- pounds of Formula I, the compound of formula (I) for use in therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS symptoms in a mammal using compounds of Formula I. Preferred compounds are N-[(2S) -1 -[2-[(2S,35)-2-hydroxy-3- [[(25)-2-(methoxycarbonylamino) -3,3-dimethylbutanoyl] amino]-4-phenylbuty1]-2- [(phenyl) methyl]hydraziny1]-3,3-dimethy1-1-oxobutan-2-yl]carbamate atazanavir (ATV) analogues substituted by several heterocycles, such as e.g. pyrazole (R1); e.g. oxetane (substituent of X2); e.g. pyridine or pyrimidine (X1); e.g. piperazine or 3,8-diazabicyclo[3.2.1]octan (X2). —R p X l , X 2 [Continued on next page] WO 2018/145021 Al 111110H31010101111E1013010111110011011011EVOIS 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 4.17(11)) 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))