SG11201903182XA - 6,7,8,9-tetrahydro-3h-pyrazolo[4,3-f]isoquinoline derivatives useful in the treatment of cancer - Google Patents

6,7,8,9-tetrahydro-3h-pyrazolo[4,3-f]isoquinoline derivatives useful in the treatment of cancer

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Publication number
SG11201903182XA
SG11201903182XA SG11201903182XA SG11201903182XA SG11201903182XA SG 11201903182X A SG11201903182X A SG 11201903182XA SG 11201903182X A SG11201903182X A SG 11201903182XA SG 11201903182X A SG11201903182X A SG 11201903182XA SG 11201903182X A SG11201903182X A SG 11201903182XA
Authority
SG
Singapore
Prior art keywords
cambridge
building
astrazeneca
owg
darwin
Prior art date
Application number
SG11201903182XA
Inventor
James Scott
Bernard Barlaam
Bin Yang
Thomas Moss
Samantha Hughes
Johannes Nissink
Daniel O'donovan
Original Assignee
Astrazeneca Ab
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of SG11201903182XA publication Critical patent/SG11201903182XA/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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))
SG11201903182XA 2016-10-24 2017-10-13 6,7,8,9-tetrahydro-3h-pyrazolo[4,3-f]isoquinoline derivatives useful in the treatment of cancer SG11201903182XA (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662411799P 2016-10-24 2016-10-24
US201662435159P 2016-12-16 2016-12-16
PCT/EP2017/076191 WO2018077630A1 (en) 2016-10-24 2017-10-13 6,7,8,9-tetrahydro-3h-pyrazolo[4,3-f]isoquinoline derivatives useful in the treatment of cancer

Publications (1)

Publication Number Publication Date
SG11201903182XA true SG11201903182XA (en) 2019-05-30

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US (4) US10131663B2 (en)
EP (2) EP3640251B1 (en)
JP (2) JP6744489B2 (en)
KR (1) KR102178692B1 (en)
CN (2) CN114656464A (en)
AU (1) AU2017349797B2 (en)
BR (1) BR112019007393A2 (en)
CA (1) CA3040040A1 (en)
CL (1) CL2019001077A1 (en)
CO (1) CO2019003950A2 (en)
CR (1) CR20190204A (en)
CY (1) CY1122566T1 (en)
DK (2) DK3640251T3 (en)
DO (1) DOP2019000104A (en)
EC (1) ECSP19028657A (en)
ES (2) ES2907759T3 (en)
HR (1) HRP20220255T1 (en)
HU (2) HUE057524T2 (en)
IL (1) IL266245B (en)
JO (1) JOP20190090B1 (en)
LT (2) LT3640251T (en)
ME (1) ME03547B (en)
MX (1) MX2019004685A (en)
NI (1) NI201900039A (en)
NZ (1) NZ753459A (en)
PE (1) PE20191078A1 (en)
PH (1) PH12019500830A1 (en)
PL (2) PL3640251T3 (en)
PT (2) PT3433256T (en)
RS (1) RS59445B1 (en)
SG (1) SG11201903182XA (en)
SI (2) SI3433256T1 (en)
TW (1) TWI735681B (en)
UA (1) UA125824C2 (en)
WO (1) WO2018077630A1 (en)

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US10131663B2 (en) 2018-11-20
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UA125824C2 (en) 2022-06-15
US20180111931A1 (en) 2018-04-26
AU2017349797A1 (en) 2019-05-30
PH12019500830A1 (en) 2019-07-24
BR112019007393A2 (en) 2019-07-02
US20190100520A1 (en) 2019-04-04
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US20200239467A1 (en) 2020-07-30
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WO2018077630A1 (en) 2018-05-03
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RS59445B1 (en) 2019-11-29
DK3640251T3 (en) 2022-03-07

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