INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 01 November 2018 (01.11.2018) WIPO I PCT omit VIII °nolo VIII 110 mmoiliollIE (10) International Publication Number WO 2018/198077 A3 (51) International Patent Classification: CO7D 487/04 (2006.01) Cl 2N 5/079 (2010.01) CO7D 519/00 (2006.01) A61P 17/02 (2006.01) A61K 35/30 (2015.01) (21) International Application Number: PCT/IB2018/052919 (22) International Filing Date: 26 April 2018 (26.04.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/491,475 28 April 2017 (28.04.2017) US 62/491,484 28 April 2017 (28.04.2017) US 62/491,526 28 April 2017 (28.04.2017) US 62/491,573 28 April 2017 (28.04.2017) US 62/650,232 29 March 2018 (29.03.2018) US (71) Applicant: NOVARTIS AG [CH/CH]; Lichtstrasse 35, 4056 Basel (CH). (72) Inventors: BEHNKE, Dirk; Novartis Pharma AG, Post- fach, 4002 Basel (CH). BERENSHTEYN, Frada; Novar- tis Institutes for BioMedical Research, Inc., 250 Massa- chusetts Avenue, Cambridge, Massachusetts 02139 (US). HAO, Xueshi; Novartis Institute for Functional Genomics, Inc., 10675 John Jay Hopkins Drive, San Diego, Califor- nia 92121 (US). HOFFMAN, Timothy; Novartis Institute for Functional Genomics, Inc., 10675 John Jay Hopkins Drive, San Diego, California 92121 (US). JIN, Qihui; No- vartis Institute for Functional Genomics, Inc., 10675 John Jay Hopkins Drive, San Diego, California 92121 (US). LA- COSTE, Arnaud; Novartis Institutes for BioMedical Re- search, Inc., 250 Massachusetts Avenue, Cambridge, Mass- achusetts 02139 (US). LEE, Cameron; Novartis Institutes for BioMedical Research, Inc., 250 Massachusetts Avenue, Cambridge, Massachusetts 02139 (US). LIU, Jun; Novar- tis Institute for Functional Genomics, Inc., 10675 John — (54) Title: 6-6 FUSED BICYCLIC HETEROARYL COMPOUNDS AND THEIR USE AS LATS INHIBITORS A2 Al Fig. 1 OMSO Ex. 49 Ex