Patent SG-11201903182X-A (SG)
Title: 6,7,8,9-tetrahydro-3h-pyrazolo[4,3-f]isoquinoline derivatives useful in the treatment of cancer
Inventor: SCOTT JAMES
IPC: C07D471/04
Filed: 2017-10-13
Abstract: Lin (CouNR? ° 8000 6000 4000 2000 W O 20 18/077 630 Al (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 03 May 2018 (03.05.2018) WIPO I PCT ~~ll~~~~~~~~ 011101110VIIIOH olo olomo milo111110 Elio ow (10) International Publication Number WO 2018/077630 Al L 10 (51) International Patent Classification: CO7D 471/04 (2006.01) A61K 31/497 (2006.01) A61K 31/4738 (2006.01) A61P 35/00 (2006.01) (21) International Application Number: PCT/EP2017/076191 (22) International Filing Date: 13 October 2017 (13.10.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/411,799 24 October 2016 (24.10.2016) US 62/435,159 16 December 2016 (16.12.2016) US (71) Applicant: ASTRAZENECA AB [SE/SE]; SE-151 85 Sodertalje (SE). (72) Inventors: SCOTT, James, Stewart; AstraZeneca Dar- win Building, Cambridge Science Park, Milton Road Cambridge CB4 OWG (GB). BARLAAM, Bernard, Christophe; AstraZeneca, Darwin Building Cambridge Science Park, Milton Road, Cambridge Cambridgeshire CB4 OWG (GB). YANG, Bin; AstraZeneca 35 Gatehouse Drive, Waltham, MA 02451 (US). MOSS, Thomas, An- drew; AstraZeneca, Darwin Building Darwin Building, Cambridge Science Park, Milton Road Cambridgeshire CB4 OWG (GB). HUGHES, Samantha, Jayne; As- traZeneca Darwin Building, Cambridge Science Park, Milton Road, Cambridge Cambridgeshire CB4 OWG (GB). NISSINK, Johannes, Wilhelmus, Maria; As- traZeneca, Darwin Building Cambridge Science Park, Mil- ton Road, Cambridge Canbridgeshire CB4 OWG (GB). O'DONOVAN, Daniel, Hillebrand; AstraZeneca Darwin Building, Cambridge Science Park, Milton Road, Cam- bridge Cambridgeshire CB4 OWG (GB). (74) Agent: COOK, Andrew, James; AstraZeneca Milstein Building, Cambridge Cambridgeshire CB21 6GH (GB). (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. = (54) Title: 6,7,8,9-TETRAHYDRO-3H-PYRAZOLO[4,3-F]ISOQUINOLINE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER (57) : The specification relates to compounds of Formula (I) and to pharmaceutically acceptable salts thereof, to processes and intermedi- ates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of cell proliferative disorders. (I) Figure 1: X-Ray Ponder Diffraction Pattern for Form A of 13-043- finoropropyhamtiffin 3 yl) 6 ((6S,8R) 8 methyl 7 (2,2,2 trifluoroethyl)-6,7,8.8- lelrahydro-311-pyrazoloi4,3-flisoquinolin-6-ylipyridin-3-amine 16000 14000 20 2-Theta - Scale [Continued on next page] WO 2018/077630 Al IMEDIMOM0101011MERI00 IIEMEHIIIIHMEDIMIE (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 4.17(ii)) Published: — with international search report (Art. 21(3))