| 摘要 |
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date W O 2013/135648 A1 19 September 2013 (19.09.2013) W I P 0 I P C T (51) International Patent Classification: (74) Agent: BEYERMANN, Jochen; Grenzacherstrasse 124, C07D 207/16 (2006.01) A61K31/40 (2006.01) CH-4070 Basel (CH). C07D 405/12 (2006.01) A61K31/4035 (2006.01) (81) Designated States (unless otherwise indicated, for every C07D 493/04 (2006.01) A6JP 35/00 (2006.01) kind of national protection available): AE, AG, AL, AM, C07F 9/572 (2006.01) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, (21) International Application Number: BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, PCT/EP2013/054920 DO, DZ, EC, EE, EG, ES, Fl, GB, GD, GE, GH, GM, GT, ) .a HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, (22) International Filng Date: KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, 12 March 2013 (12.03.2013) ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, (25) Filing Language: English NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, (26) Publication Language: English TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, (30) Priority Data: ZM, ZW. 61/611,200 15 March 2012 (15.03.2012) US (84) Designated States (unless otherwise indicated, for every (71) Applicant (for all designated States except US): F. HOFF- kind of regional protection available): ARIPO (BW, GH, MANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, 124, CH-4070 Basel (CH). UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, (72) Inventors; and EE, ES, Fl, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, - (71) Applicants (for US only): BARTKOVITZ, David Joseph MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, [US/US]; 21 Povershon Road, Nutley, New Jersey 07110 TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, (US). CHU, Xin-Jie [US/US]; 21 Riker Hill Road, Living- ML, MR, NE, SN, TD, TG). ston, New Jersey 07039 (US). VU, Binh Thanh [US/US]; 1 Willow Lane, North Caldwell, New Jersey 07006 (US). Published: ZHAO, Chunlin [US/CN]; 590 Ruiqing Road, Zhangjiang - with international search report (Art. 21(3)) East Campus, Pudong, Shanghai 201201 (CN). (72) Inventor: FISHLOCK, Daniel; Klingelbergstrasse 91, CH-4056 Basel (CH). (54) Title: SUBSTITUTED PYRROLIDINE-2-CARBOXAMIDES == Z H O'R O N O 4 R He N H0 R2 1H 0" R oc X 1" y (57) Abstract: There are provided compounds of formula (I) wherein X, Y, Z, R 1, R2, R3 and R4 are as described herein, and enan 0 tiomers and pharmaceutically acceptable salts and esters thereof; as well as methods for making such compounds, pharmaceutical compositions comprising said compounds, and their use in the treatment of cancer. |
