SG11201902529WA - Naphthyridinone derivatives and their use in the treatment of arrhythmia - Google Patents

Naphthyridinone derivatives and their use in the treatment of arrhythmia

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Publication number
SG11201902529WA
SG11201902529WA SG11201902529WA SG11201902529WA SG11201902529WA SG 11201902529W A SG11201902529W A SG 11201902529WA SG 11201902529W A SG11201902529W A SG 11201902529WA SG 11201902529W A SG11201902529W A SG 11201902529WA SG 11201902529W A SG11201902529W A SG 11201902529WA
Authority
SG
Singapore
Prior art keywords
novartis
cambridge
international
institutes
avenue
Prior art date
Application number
SG11201902529WA
Inventor
Guillaume Barbe
Gregory Raymond Bebernitz
Sicong Geng
Efthymiou Hatice Belgin Gulgeze
Lv Liao
Fupeng Ma
Ruowei Mo
David Thomas Parker
Yunshan Peng
Stefan Peukert
Ken Yamada
Kayo Yasoshima
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of SG11201902529WA publication Critical patent/SG11201902529WA/en

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    • 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 1#11101111 0 11101 HOE 3E1 0 0111E1111001 HE ME 110 11110 1111 OEN Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\" WO 2018/073788 Al 26 April 2018 (26.04.2018) WIP0 I PCT (51) International Patent Classification: gin; Novartis Institutes for BioMedical Research, Inc., CO7D 471/04 (2006.01) A61P 9/06 (2006.01) 250 Massachusetts Avenue, Cambridge, MA 02139 (US). A61K 31/4375 (2006.01) LIAO, Lv; Shanghai Novartis Trading Ltd., 4218 Jinke (21) International Application Number: Road, Zhangjiang Hi-Tech Park, Pudong, Shanghai 201203 (CN). MA, Fupeng; Novartis Institutes for BioMedical Re- PCT/IB2017/056515 search, Inc., 250 Massachusetts Avenue, Cambridge, MA (22) International Filing Date: 02139 (US). MO, Ruowei; Novartis Institutes for BioMed- 19 October 2017 (19.10.2017) ical Research, Inc., 250 Massachusetts Avenue, Cambridge, MA 02139 (US). PARKER, David Thomas; 25 Crestwood (25) Filing Language: English Road, Windham, NH 03087 (US). PENG, Yunshan; No- (26) Publication Language: English vartis Institutes for Biomedical Research, Inc., 250 Mass- achusetts Avenue, Cambridge, MA 02139 (US). PEUK- (30) Priority Data: ERT, Stefan; Novartis Institutes for Biomedical Research, PCT/CN2016/102928 Inc., 250 Massachusetts Avenue, Cambridge, MA 02139 21 October 2016 (21.10.2016) CN (US). YAMADA, Ken; Novartis Institutes for Biomed- 62/410,930 21 October 2016 (21.10.2016) US ical Research, Inc., 250 Massachusetts Avenue, Cambridge, 62/413,292 26 October 2016 (26.10.2016) US MA 02139 (US). YASOSHIMA, Kayo; Novartis Institutes (71) Applicant: NOVARTIS AG [CH/CH]; Lichtstrasse 35, for Biomedical Research, Inc., 250 Massachusetts Avenue, 4056 Basel (CH). Cambridge, MA 02139 (US). (72) Inventors: BARBE, Guillaume; 583 Pleasant Street, Mil- (74) Agent: NOVARTIS AG; Lichtstrasse 35, 4056 Basel ton, MA 02186 (US). BEBERNITZ, Gregory Raymond; (CH). _ 799 Bartlett Carry Road, Tupper Lake, NY 12986 (US). (81) Designated States (unless otherwise indicated, for every = GENG, Sicong; Jinke Road, Zhangjiang Hi-Tech Park, Pudong, Shanghai Shanghai Novartis Trading Ltd., 4218 kind AO, of national protection available): AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, _ 201203 (CN). CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, GULGEZE EFTHYMIOU, Hatice Bel- CA, (54) Title: NAPHTHYRIDINONE DERIVATIVES AND THEIR USE IN THE TREATMENT OF ARRHYTHMIA (57) : The present invention provides a compound of formu- = = ElgUre 1. PCIRP0.0 example 1 11Yd.R 1 0 X.R. e la (I) or a pharmaceutically acceptable salt thereof; (I) Wherein R 1 , R 3 -R 6 , X 2 and X 3 are as defined herein, a method for manufacturing = the compounds of the invention, and its therapeutic uses. The present i invention further provides a combination of pharmacologically active = = agents and a pharmaceutical composition. I = _ = = h = = _ _ = — Il GC CI 11 0 R s GC R° IN en N R' IN I 1 1 © ,-.... x ,...,„. 11 Fe 0 (I) © N O [Continued on next page] WO 2018/073788 Al MIDEDIMOMOIDEIREEMOOMEIIIIIIIIMOMEEN 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. (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(H)) Published: — with international search report (Art. 21(3)) — before the expiration of the time limit for amending the claims and to be republished in the event of receipt of amendments (Rule 48.2(h))
SG11201902529WA 2016-10-21 2017-10-19 Naphthyridinone derivatives and their use in the treatment of arrhythmia SG11201902529WA (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201662410930P 2016-10-21 2016-10-21
CN2016102928 2016-10-21
US201662413292P 2016-10-26 2016-10-26
PCT/IB2017/056515 WO2018073788A1 (en) 2016-10-21 2017-10-19 Naphthyridinone derivatives and their use in the treatment of arrhythmia

Publications (1)

Publication Number Publication Date
SG11201902529WA true SG11201902529WA (en) 2019-05-30

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201902529WA SG11201902529WA (en) 2016-10-21 2017-10-19 Naphthyridinone derivatives and their use in the treatment of arrhythmia

Country Status (33)

Country Link
US (3) US10266531B2 (en)
EP (2) EP3529251B1 (en)
JP (1) JP7030802B2 (en)
KR (1) KR102540872B1 (en)
CN (1) CN109843887B (en)
AU (2) AU2017344489C1 (en)
BR (1) BR112019007863A2 (en)
CA (1) CA3038624A1 (en)
CL (1) CL2019001023A1 (en)
CO (1) CO2019003894A2 (en)
CR (1) CR20190201A (en)
CU (1) CU24599B1 (en)
DO (1) DOP2019000100A (en)
EC (1) ECSP19026973A (en)
ES (1) ES2934234T3 (en)
FI (1) FI3529251T3 (en)
HR (1) HRP20221516T1 (en)
HU (1) HUE060882T2 (en)
IL (1) IL266128B (en)
JO (1) JOP20190086A1 (en)
LT (1) LT3529251T (en)
MX (1) MX2019004484A (en)
PE (1) PE20190735A1 (en)
PH (1) PH12019500849A1 (en)
PL (1) PL3529251T3 (en)
PT (1) PT3529251T (en)
RS (1) RS63841B1 (en)
SA (1) SA519401614B1 (en)
SG (1) SG11201902529WA (en)
SI (1) SI3529251T1 (en)
TW (1) TWI759343B (en)
UY (1) UY37445A (en)
WO (1) WO2018073788A1 (en)

Families Citing this family (4)

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JOP20190086A1 (en) 2016-10-21 2019-04-18 Novartis Ag Naphthyridinone derivatives and their use in the treatment of arrhythmia
SG11202012973RA (en) * 2018-06-27 2021-01-28 Bristol Myers Squibb Co Naphthyridinone compounds useful as t cell activators
WO2022074567A1 (en) 2020-10-06 2022-04-14 Novartis Ag Pharmaceutical compositions comprising naphthyridinone derivatives and their use in the treatment of arrhythmia
AR127698A1 (en) * 2021-11-23 2024-02-21 Novartis Ag NAFTYRIDINOONE DERIVATIVES FOR THE TREATMENT OF A DISEASE OR DISORDER

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