PT117825A - SILA-ANALOGS OF VITAMIN D, METHOD OF PRODUCTION OF SAID COMPOUNDS, USES THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE COMPOUNDS - Google Patents

SILA-ANALOGS OF VITAMIN D, METHOD OF PRODUCTION OF SAID COMPOUNDS, USES THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE COMPOUNDS

Info

Publication number
PT117825A
PT117825A PT117825A PT11782522A PT117825A PT 117825 A PT117825 A PT 117825A PT 117825 A PT117825 A PT 117825A PT 11782522 A PT11782522 A PT 11782522A PT 117825 A PT117825 A PT 117825A
Authority
PT
Portugal
Prior art keywords
analogs
compounds
vitamin
vdr
sila
Prior art date
Application number
PT117825A
Other languages
Portuguese (pt)
Inventor
Borges Rodríguez
Manuel Romão De Castro Baltazar
Loureiro Martínez Julián
Emanuel Sampaio Dias Ivo
Perez Fernandez Román
Seoane Ruzo Samuel
Mouriño Mosquera Antonio
Original Assignee
Univ Santiago Compostela
Univ Do Porto
Requimte Rede De Quim E Tecnologia
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 Univ Santiago Compostela, Univ Do Porto, Requimte Rede De Quim E Tecnologia filed Critical Univ Santiago Compostela
Priority to PT117825A priority Critical patent/PT117825A/en
Priority to PCT/IB2022/052839 priority patent/WO2023161688A1/en
Priority to ES202330169A priority patent/ES2946255B2/en
Publication of PT117825A publication Critical patent/PT117825A/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F11/00—Compounds containing elements of Groups 6 or 16 of the Periodic Table
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C401/00—Irradiation products of cholesterol or its derivatives; Vitamin D derivatives, 9,10-seco cyclopenta[a]phenanthrene or analogues obtained by chemical preparation without irradiation
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • 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
    • A61K31/59—Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/0825—Preparations of compounds not comprising Si-Si or Si-cyano linkages
    • C07F7/0827—Syntheses with formation of a Si-C bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/0825—Preparations of compounds not comprising Si-Si or Si-cyano linkages
    • C07F7/083—Syntheses without formation of a Si-C bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0834—Compounds having one or more O-Si linkage
    • C07F7/0836—Compounds with one or more Si-OH or Si-O-metal linkage
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0896—Compounds with a Si-H linkage

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

O PRESENTE PEDIDO DESCREVE A SÍNTESE E IMPORTANTES APLICAÇÕES BIOLÓGICAS DE NOVOS ANÁLOGOS DA VITAMINA D BASEADOS NA TROCA DE CARBONO POR SILÍCIO NA CADEIA LATERAL DA HORMONA NATURAL E SEUS ANÁLOGOS. EM COMPARAÇÃO COM O METABOLITO NATURAL 1Α,25-DI-HIDROXIVITAMINA D3 (1,25D) DO RECETOR DA VITAMINA D (VDR), OS PRINCIPAIS RESULTADOS BIOLÓGICOS DESSES NOVOS DERIVADOS INDICAM QUE: A) ESTES ANÁLOGOS APRESENTAM UMA DIFERENCIAÇÃO CELULAR SEMELHANTE, B) A PROLIFERAÇÃO DE LINHAS DE CÉLULAS TUMORAIS É SIGNIFICATIVAMENTE MENOR, C) GRANDE CAPACIDADE DE ATIVAR GENES-ALVO DA 1,25D E D) ALTA AFINIDADE AO VDR. ALÉM DISSO, UM DOS ANÁLOGOS INDUZ UM AUMENTO SIGNIFICATIVO NO PESO DE ALGUNS ANIMAIS, O QUE PODE SUGERIR UM AUMENTO NA DENSIDADE ÓSSEA.THIS APPLICATION DESCRIBES THE SYNTHESIS AND IMPORTANT BIOLOGICAL APPLICATIONS OF NEW VITAMIN D ANALOGS BASED ON THE EXCHANGE OF CARBON FOR SILICON IN THE SIDE CHAIN OF THE NATURAL HORMONE AND ITS ANALOGS. IN COMPARISON WITH THE NATURAL METABOLITE 1Α,25-DIHYDROXIVITAMIN D3 (1,25D) OF THE VITAMIN D RECEPTOR (VDR), THE MAIN BIOLOGICAL RESULTS OF THESE NEW DERIVATIVES INDICATE THAT: A) THESE ANALOGS SHOW SIMILAR CELLULAR DIFFERENTIATION, B) THE PROLIFERATION OF TUMOR CELL LINES IS SIGNIFICANTLY LOWER, C) GREAT CAPACITY TO ACTIVATE 1,25D TARGET GENES AND D) HIGH AFFINITY TO THE VDR. IN ADDITION, ONE OF THE ANALOGS INDUCES A SIGNIFICANT INCREASE IN THE WEIGHT OF SOME ANIMALS, WHICH MAY SUGGEST AN INCREASE IN BONE DENSITY.

PT117825A 2022-02-28 2022-02-28 SILA-ANALOGS OF VITAMIN D, METHOD OF PRODUCTION OF SAID COMPOUNDS, USES THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE COMPOUNDS PT117825A (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
PT117825A PT117825A (en) 2022-02-28 2022-02-28 SILA-ANALOGS OF VITAMIN D, METHOD OF PRODUCTION OF SAID COMPOUNDS, USES THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE COMPOUNDS
PCT/IB2022/052839 WO2023161688A1 (en) 2022-02-28 2022-03-28 Sila-analogues of vitamin d compounds, method of producing said compounds and uses thereof
ES202330169A ES2946255B2 (en) 2022-02-28 2023-02-27 SILA-ANALOGUES OF VITAMIN D COMPOUNDS, METHOD OF PRODUCTION OF SUCH COMPOUNDS AND USES THEREOF

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PT117825A PT117825A (en) 2022-02-28 2022-02-28 SILA-ANALOGS OF VITAMIN D, METHOD OF PRODUCTION OF SAID COMPOUNDS, USES THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE COMPOUNDS

Publications (1)

Publication Number Publication Date
PT117825A true PT117825A (en) 2023-09-20

Family

ID=81648787

Family Applications (1)

Application Number Title Priority Date Filing Date
PT117825A PT117825A (en) 2022-02-28 2022-02-28 SILA-ANALOGS OF VITAMIN D, METHOD OF PRODUCTION OF SAID COMPOUNDS, USES THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE COMPOUNDS

Country Status (3)

Country Link
ES (1) ES2946255B2 (en)
PT (1) PT117825A (en)
WO (1) WO2023161688A1 (en)

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006074227A2 (en) * 2005-01-04 2006-07-13 Johns Hopkins University HIGHLY ANTIPROLIFERATIVE, LOW-CALCEMIC, ANALOGS OF THE HORMONE 1α, 25-DIHYDROXYVITAMIN D3 WITH CARBONYL SIDE CHAINS
WO2012118154A1 (en) * 2011-03-02 2012-09-07 学校法人日本大学 Novel vitamin d receptor modulator with partial agonist activity
ES2396524B2 (en) * 2012-12-11 2013-08-01 Universidade De Santiago De Compostela Versatile and functionalized intermediates in the synthesis of vitamin D and new vitamin D derivatives
ES2714628B2 (en) * 2017-11-29 2019-10-02 Univ Santiago Compostela Compounds derived from vitamin D
WO2019106214A1 (en) * 2017-11-29 2019-06-06 Universidade De Santiago De Compostela Compounds derived from vitamin d
ES2759698A1 (en) * 2018-11-09 2020-05-11 Univ Santiago Compostela COMPOUNDS DERIVED FROM VITAMIN D (Machine-translation by Google Translate, not legally binding)

Also Published As

Publication number Publication date
ES2946255A1 (en) 2023-07-14
WO2023161688A1 (en) 2023-08-31
ES2946255B2 (en) 2024-08-16

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