SG11201805318SA - Formulations of phosphoramidate derivatives of nucleoside drugs - Google Patents

Formulations of phosphoramidate derivatives of nucleoside drugs

Info

Publication number
SG11201805318SA
SG11201805318SA SG11201805318SA SG11201805318SA SG11201805318SA SG 11201805318S A SG11201805318S A SG 11201805318SA SG 11201805318S A SG11201805318S A SG 11201805318SA SG 11201805318S A SG11201805318S A SG 11201805318SA SG 11201805318S A SG11201805318S A SG 11201805318SA
Authority
SG
Singapore
Prior art keywords
international
formulations
lochside
edinburgh
place
Prior art date
Application number
SG11201805318SA
Inventor
Gordon Kennovin
Hugh Griffith
Original Assignee
NuCana plc
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 NuCana plc filed Critical NuCana plc
Publication of SG11201805318SA publication Critical patent/SG11201805318SA/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 29 June 2017 (29.06.2017) WIPOIPCT (10) International Publication Number WO 2017/109491 A1 (51) International Patent Classification: A61K 9/00 (2006.01) A61K 31/7076 (2006.01) A61K 9/08 (2006.01) A61P 35/00 (2006.01) A61K31/7072 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/GB2016/054025 21 December 2016 (21.12.2016) English English (30) Priority Data: 1522764.8 23 December 2015 (23.12.2015) GB (71) Applicant: NUCANA BIOMED LIMITED [GB/GB]; 10 Lochside Place, Edinburgh Scotland EH 12 9RG (GB). (72) Inventors: KENNOVIN, Gordon; c/o NuCana BioMed Limited, 10 Lochside Place, Edinburgh EH 12 9RG (GB). GRIFFITH, Hugh; c/o NuCana BioMed Limited, 10 Lochside Place, Edinburgh EH 12 9RG (GB). (74) Agent: HGF LIMITED (LEEDS); 1 City Walk, Leeds LSI 1 9DX (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, 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). Published: — with international search report (Art. 21(3)) 0\ •t o\ © o CJ (54) Title: FORMULATIONS OF PHOSPHORAMIDATE DERIVATIVES OF NUCLEOSIDE DRUGS (57) : This invention relates to pharmaceutical formulations and formulation strategies of protides (phosphoramidate deriv­ atives of nucleosides) and, in particular, protides useful in the treatment of cancer such as NUC-3373 (5-fluoro-2'-deoxyuridine-5'-0- [1-naphthyl (benzoxy-L-alaninyl)] phosphate) and NUC-7738 (3'-deoxyadenosine-5'-0-[phenyl(benzyloxy-L-alaninyl)] phosphate). In particular, the invention relates to formulations which comprise a polar aprotic solvent, for example dimethyl acetamide (DMA).
SG11201805318SA 2015-12-23 2016-12-21 Formulations of phosphoramidate derivatives of nucleoside drugs SG11201805318SA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1522764.8A GB201522764D0 (en) 2015-12-23 2015-12-23 Formulations of phosphate derivatives
PCT/GB2016/054025 WO2017109491A1 (en) 2015-12-23 2016-12-21 Formulations of phosphoramidate derivatives of nucleoside drugs

Publications (1)

Publication Number Publication Date
SG11201805318SA true SG11201805318SA (en) 2018-07-30

Family

ID=55311533

Family Applications (2)

Application Number Title Priority Date Filing Date
SG11201805318SA SG11201805318SA (en) 2015-12-23 2016-12-21 Formulations of phosphoramidate derivatives of nucleoside drugs
SG10202008554RA SG10202008554RA (en) 2015-12-23 2016-12-21 Formulations of phosphoramidate derivatives of nucleoside drugs

Family Applications After (1)

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SG10202008554RA SG10202008554RA (en) 2015-12-23 2016-12-21 Formulations of phosphoramidate derivatives of nucleoside drugs

Country Status (20)

Country Link
US (3) US20180369266A1 (en)
EP (1) EP3393453A1 (en)
JP (2) JP6913095B2 (en)
KR (1) KR20180091919A (en)
CN (1) CN108697636A (en)
AU (2) AU2016375866B2 (en)
BR (2) BR112018012951B1 (en)
CA (1) CA3008751C (en)
CL (1) CL2018001672A1 (en)
EA (2) EA202190058A1 (en)
GB (1) GB201522764D0 (en)
HK (1) HK1255108A1 (en)
IL (1) IL260008A (en)
MA (1) MA44117A (en)
MX (2) MX2018007794A (en)
MY (1) MY196741A (en)
PH (1) PH12018501341A1 (en)
SA (1) SA518391858B1 (en)
SG (2) SG11201805318SA (en)
WO (1) WO2017109491A1 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0317009D0 (en) 2003-07-21 2003-08-27 Univ Cardiff Chemical compounds
SG192841A1 (en) 2011-03-01 2013-09-30 Nucana Biomed Ltd Phosphoramidate derivatives of 5 - fluoro - 2 ' - deoxyuridine for use in the treatment of cancer
TWI674097B (en) 2014-06-25 2019-10-11 英商努卡那公眾有限公司 Formulations of phosphate derivatives
LT3224268T (en) 2014-11-28 2019-09-25 NuCana plc New 2` and/or 5` amino-acid ester phosphoramidate 3`-deoxy adenosine derivatives as anti-cancer compounds
GB201609600D0 (en) 2016-06-01 2016-07-13 Nucuna Biomed Ltd Cancer treatments
GB201709471D0 (en) 2017-06-14 2017-07-26 Nucana Biomed Ltd Diastereoselective synthesis of hosphate derivatives
GB201713916D0 (en) * 2017-08-30 2017-10-11 Nucana Biomed Ltd Treatment regimens
CN110840907B (en) * 2019-08-16 2022-11-25 南京医科大学 Free radical sensitive uracil ProTide prodrug and pharmaceutical application thereof
WO2023218202A2 (en) 2022-05-12 2023-11-16 NuCana plc Cancer treatment

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GB201609600D0 (en) 2016-06-01 2016-07-13 Nucuna Biomed Ltd Cancer treatments
GB201709471D0 (en) 2017-06-14 2017-07-26 Nucana Biomed Ltd Diastereoselective synthesis of hosphate derivatives
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Also Published As

Publication number Publication date
CA3008751C (en) 2023-10-03
PH12018501341A1 (en) 2019-02-18
CL2018001672A1 (en) 2019-02-01
EA037320B1 (en) 2021-03-11
EA202190058A1 (en) 2021-06-30
EA201891471A1 (en) 2018-12-28
AU2022211797A1 (en) 2022-08-25
KR20180091919A (en) 2018-08-16
BR122023000551B1 (en) 2023-12-05
MY196741A (en) 2023-05-03
BR112018012951A2 (en) 2018-12-11
MX2021010601A (en) 2021-09-28
SA518391858B1 (en) 2022-10-30
MA44117A (en) 2021-03-31
US20240082287A1 (en) 2024-03-14
AU2016375866B2 (en) 2022-06-09
US11786544B2 (en) 2023-10-17
JP2018538342A (en) 2018-12-27
US20220031728A1 (en) 2022-02-03
EP3393453A1 (en) 2018-10-31
MX2018007794A (en) 2019-07-01
IL260008A (en) 2018-07-31
HK1255108A1 (en) 2019-08-02
WO2017109491A1 (en) 2017-06-29
CA3008751A1 (en) 2017-06-29
AU2022211797B2 (en) 2024-04-04
JP2021165310A (en) 2021-10-14
SG10202008554RA (en) 2020-10-29
AU2016375866A1 (en) 2018-07-05
US20180369266A1 (en) 2018-12-27
CN108697636A (en) 2018-10-23
GB201522764D0 (en) 2016-02-03
BR112018012951B1 (en) 2023-12-12
JP6913095B2 (en) 2021-08-04

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