IT202000001390A1 - Processo per la preparazione del sale sodico dell’acido 4-[[(1r)-2-[5-(2-fluoro-3-metossifenil)-3-[[2-fluoro-6-(trifluorometil)fenil]metil]-3,6-diidro-4-metil-2,6-diosso-1(2h)-pirimidinil]-1-feniletil]ammino]-butanoico (elagolix sale sodico) e intermedi di detto processo - Google Patents

Processo per la preparazione del sale sodico dell’acido 4-[[(1r)-2-[5-(2-fluoro-3-metossifenil)-3-[[2-fluoro-6-(trifluorometil)fenil]metil]-3,6-diidro-4-metil-2,6-diosso-1(2h)-pirimidinil]-1-feniletil]ammino]-butanoico (elagolix sale sodico) e intermedi di detto processo

Info

Publication number
IT202000001390A1
IT202000001390A1 IT102020000001390A IT202000001390A IT202000001390A1 IT 202000001390 A1 IT202000001390 A1 IT 202000001390A1 IT 102020000001390 A IT102020000001390 A IT 102020000001390A IT 202000001390 A IT202000001390 A IT 202000001390A IT 202000001390 A1 IT202000001390 A1 IT 202000001390A1
Authority
IT
Italy
Prior art keywords
fluoro
methyl
sodium salt
metoxyphenyl
butanoic
Prior art date
Application number
IT102020000001390A
Other languages
English (en)
Inventor
Roberto Lenna
Andrea Fasana
Jerry Ortiz
Original Assignee
Ind Chimica Srl
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 Ind Chimica Srl filed Critical Ind Chimica Srl
Priority to IT102020000001390A priority Critical patent/IT202000001390A1/it
Priority to FR2007887A priority patent/FR3100246B1/fr
Priority to BR112022003622A priority patent/BR112022003622A2/pt
Priority to DE112020004177.8T priority patent/DE112020004177T5/de
Priority to US17/639,638 priority patent/US11840519B2/en
Priority to GB2203781.6A priority patent/GB2603328B/en
Priority to PCT/IB2020/057065 priority patent/WO2021044230A1/en
Priority to CN202080062002.7A priority patent/CN114641468A/zh
Priority to CH000210/2022A priority patent/CH718005B1/it
Priority to CA3149179A priority patent/CA3149179A1/en
Priority to ES202290012A priority patent/ES2915123B2/es
Publication of IT202000001390A1 publication Critical patent/IT202000001390A1/it

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
IT102020000001390A 2019-09-03 2020-01-24 Processo per la preparazione del sale sodico dell’acido 4-[[(1r)-2-[5-(2-fluoro-3-metossifenil)-3-[[2-fluoro-6-(trifluorometil)fenil]metil]-3,6-diidro-4-metil-2,6-diosso-1(2h)-pirimidinil]-1-feniletil]ammino]-butanoico (elagolix sale sodico) e intermedi di detto processo IT202000001390A1 (it)

Priority Applications (11)

Application Number Priority Date Filing Date Title
IT102020000001390A IT202000001390A1 (it) 2020-01-24 2020-01-24 Processo per la preparazione del sale sodico dell’acido 4-[[(1r)-2-[5-(2-fluoro-3-metossifenil)-3-[[2-fluoro-6-(trifluorometil)fenil]metil]-3,6-diidro-4-metil-2,6-diosso-1(2h)-pirimidinil]-1-feniletil]ammino]-butanoico (elagolix sale sodico) e intermedi di detto processo
FR2007887A FR3100246B1 (fr) 2019-09-03 2020-07-27 Procede de preparation du sel sodique d'elagolix et intermediaires dudit procede
BR112022003622A BR112022003622A2 (pt) 2019-09-03 2020-07-27 Processo para a síntese do sal de sódio do ácido 4-[[(1r)-2-[5-(2-flúor-3-metoxifenil)-3-[[2-flúor-6-(trifluormetil)-fenil]metil]-3,6-diidro-4-metil-2,6-dioxo-1(2h)-pirimidinila]-1-feniletil]amino]-butanóico (sal de sódio de elagolix) e intermediários do referido processo
DE112020004177.8T DE112020004177T5 (de) 2019-09-03 2020-07-27 Verfahren zur herstellung des natriumsalzes von 4-[[(1r)-2-[5-(2-fluor-3-methoxyphenyl)-3-[[2-fluor-6-(trifluormethyl)-phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2h)-pyrimidinyl]-1-phenylethyl]amino]butansäure (elagolix-natriumsalz) und zwischenstufen dieses verfahrens
US17/639,638 US11840519B2 (en) 2019-09-03 2020-07-27 Process for the synthesis of the sodium salt of 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)-phenyl]methyl]-3,6-dihydro-4-methyl-2.6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]amino]-butanoic acid (elagolix sodium salt) and intermediates of said process
GB2203781.6A GB2603328B (en) 2019-09-03 2020-07-27 Process for the synthesis of elagolix sodium salt and intermediates of said process
PCT/IB2020/057065 WO2021044230A1 (en) 2019-09-03 2020-07-27 Process for the synthesis of the sodium salt of 4-[[(lr)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)-phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-l(2h)-pyrimidinyl]-l- phenylethyl]amino]-butanoic acid (elagolix sodium salt) and intermediates of said process
CN202080062002.7A CN114641468A (zh) 2019-09-03 2020-07-27 用于合成4-[[(1r)-2-[5-(2-氟-3-甲氧基苯基)-3-[[2-氟-6-(三氟甲基)-苯基]甲基]-3,6-二氢-4-甲基-2,6-二氧代-1(2h)-嘧啶基]-1-苯乙基]氨基]-丁酸的钠盐(elagolix钠盐)的工艺和所述工艺的中间体
CH000210/2022A CH718005B1 (it) 2019-09-03 2020-07-27 Processo per la preparazione del sale sodico dell'acido 4-[[(1R)-2-[5-(2-fluoro-3-metossifenil)-3-[[2-fluoro-6 (trifluorometil)fenil]metil]-3,6-diidro-4-metil-2,6-diosso-1(2H)-pirimidinil]-1-feniletil]ammino]-butanoico (elagolix sale sodico) e intermedi di detto processo.
CA3149179A CA3149179A1 (en) 2019-09-03 2020-07-27 Process for the synthesis of the sodium salt of 4-[[(1r)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)-phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2h)-pyrimidinyl]-1-phenylethyl]amino]-butanoic acid (elagolix sodium salt) and intermediates of said process
ES202290012A ES2915123B2 (es) 2019-09-03 2020-07-27 Proceso para la síntesis de la sal sódica del ácido 4-[[(1R)-2-[5-(2-fluoro-3-metoxifenil)-3-[[2-fluoro-6-(trifluorometil)-fenil]metil]-3,6-dihidro-4-metil-2,6-dioxo-1(2H)-pirimidinil]-1-feniletil]amino]-butanoico (sal sódica de Elagolix) y productos intermedios de dicho proceso

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IT102020000001390A IT202000001390A1 (it) 2020-01-24 2020-01-24 Processo per la preparazione del sale sodico dell’acido 4-[[(1r)-2-[5-(2-fluoro-3-metossifenil)-3-[[2-fluoro-6-(trifluorometil)fenil]metil]-3,6-diidro-4-metil-2,6-diosso-1(2h)-pirimidinil]-1-feniletil]ammino]-butanoico (elagolix sale sodico) e intermedi di detto processo

Publications (1)

Publication Number Publication Date
IT202000001390A1 true IT202000001390A1 (it) 2021-07-24

Family

ID=70295892

Family Applications (1)

Application Number Title Priority Date Filing Date
IT102020000001390A IT202000001390A1 (it) 2019-09-03 2020-01-24 Processo per la preparazione del sale sodico dell’acido 4-[[(1r)-2-[5-(2-fluoro-3-metossifenil)-3-[[2-fluoro-6-(trifluorometil)fenil]metil]-3,6-diidro-4-metil-2,6-diosso-1(2h)-pirimidinil]-1-feniletil]ammino]-butanoico (elagolix sale sodico) e intermedi di detto processo

Country Status (1)

Country Link
IT (1) IT202000001390A1 (it)

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005007165A1 (en) * 2003-07-07 2005-01-27 Neurocrine Biosciences, Inc. Pyrimidine-2, 4-dione derivatives as gonadotropin-releasing hormone receptor antagonists

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005007165A1 (en) * 2003-07-07 2005-01-27 Neurocrine Biosciences, Inc. Pyrimidine-2, 4-dione derivatives as gonadotropin-releasing hormone receptor antagonists
EP1646389B1 (en) 2003-07-07 2008-09-10 Neurocrine Biosciences, Inc. Pyrimidine-2,4-dione derivatives as gonadotropin-releasing hormone receptor antagonists

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