Patent SG-11201806109R-A (SG)
Title: Crystalline form of 1,3-thiazol-5-ylmethyl [(2r,5r)-5-{[(2s)-2-[(methyl{[2-(propan-2-yl)-1,3-thiazol-4-yl]methyl}carbamoyl)amino]-4-(morpholin-4-yl)butanoyl 9amino}-1,6-diphenylhexan-2-yl]carbamate or cobicistat
Inventor: CHIAJEN LAI
IPC: C07D277/28
Filed: 2017-01-24
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property , Organization MD 1111101110101011111 HO 1111101110111001011101 Ell 10111110 IIE III International Bureau 0.. .... .. (10) International Publication Number (43) International Publication Date ..... ...r .....1 WO 2017/132158 Al 3 August 2017 (03.08.2017) W I P0 I P CT (51) International Patent Classification: BZ, C07D 277/28 (2006.01) A61K 31/5377 (2006.01) DO, A61K 45/06 (2006.01) HN, KP, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, (21) International Application Number: MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, PCT/US2017/014761 NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, (22) International Filing Date: RU, 24 January 2017 (24.01.2017) TH, ZA, ZM, ZW. RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, (25) Filing Language: English (84) Designated States (unless otherwise indicated, for every (26) Publication Language: English kind of regional protection available): ARIPO (BW, GH, (30) Priority Data: GM, 62/288,029 28 January 2016 (28.01.2016) US TZ, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, (71) Applicant: GILEAD SCIENCES, INC. [US/US]; 333 DK, Lakeside Drive, Foster City, CA 94404 (US). LV, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, (72) Inventors: LAI, Chiajen; c/o Gilead Sciences, Inc., 333 SM, Lakeside Drive, Foster City, CA 94404 (US). YU, Lok GW, KM, ML, MR, NE, SN, TD, TG). TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, Him Lawrence; c/o Gilead Sciences, Inc., 333 Lakeside Declarations under Rule 4.17: Drive, Foster City, CA 94404 (US). YU, Richard Hung as to applicant's entitlement to apply for and be granted a Chiu; c/o Gilead Sciences, Inc., 333 Lakeside Drive, patent (Rule 4.17(ii)) Foster City, CA 94404 (US). — as to the applicant's entitlement to claim the priority of the — _ (74) Agents: SILVER, Joel et al.; Gilead Sciences, Inc., 333 earlier application (Rule 4.17(iii)) _ Lakeside Drive, Foster City, California 94404 (US). = Published: Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, — with (81) international search report (Art. 21(3)) = AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, = = = = = = = = = = = = _ (54) Title: CRYSTALLINE FORM OF 1,3-THIAZOL-5-YLMETHYL [(2R,5R)-5-{[(2S)-2-[(METHYL{[2-(PROPAN-2-YL)-1,3-THIAZOL-4- YL]METHYLICARBAMOYL)AMIN0]-4-(MORPHOLIN-4-YL)BUTANOYL 9AMINO}-1,6-DIPHENYLHEXAN-2-YL]CARBAMATE OR _ — COBICISTAT Il GC N ) kr) Il Ph el 0 en ,-1 IN i T-- , \ : i . N.,......,,,..,/,. N . 7 , Ph ° (1a) 11 © N (57) : The invention provides a crystalline form of the compound of formula (Ia), methods for making the crystalline form (\") of the compound of formula (Ia), and therapeutic methods for the use of the crystal line form of the compound of formula (Ia).