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HRP20220060T1 - Predlijekovi supstituiranih derivata triazola i njihova upotreba - Google Patents

Predlijekovi supstituiranih derivata triazola i njihova upotreba Download PDF

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Publication number
HRP20220060T1
HRP20220060T1 HRP20220060TT HRP20220060T HRP20220060T1 HR P20220060 T1 HRP20220060 T1 HR P20220060T1 HR P20220060T T HRP20220060T T HR P20220060TT HR P20220060 T HRP20220060 T HR P20220060T HR P20220060 T1 HRP20220060 T1 HR P20220060T1
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HR
Croatia
Prior art keywords
compound
general formula
syndrome
solvates
formula
Prior art date
Application number
HRP20220060TT
Other languages
English (en)
Inventor
Marie-Pierre COLLIN-KROEPELIN
Peter Kolkhof
Thomas Neubauer
Chantal Fuerstner
Elisabeth Pook
Matthias Beat WITTWER
Carsten Schmeck
Pierre Wasnaire
Heiko Schirmer
Hana CERNECKA
Karoline Droebner
Hanna Tinel
Anja Buchmueller
Thomas MONDRITZKI
Axel Kretschmer
Klemens Lustig
Robert Fricke
Guillaume Levilain
Ursula Krenz
Norbert Witowski
Original Assignee
Bayer Aktiengesellschaft
Bayer Pharma Aktiengesellschaft
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 Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft filed Critical Bayer Aktiengesellschaft
Publication of HRP20220060T1 publication Critical patent/HRP20220060T1/hr

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    • 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
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

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

Claims (11)

1. Spoj opće formule (I) [image] u kojoj R1 predstavlja skupinu s formulom [image] u kojoj # predstavlja točku vezivanja za prsten 1,2,4-triazolil, ili jedna od njegovih farmaceutski prihvatljivih soli, njegovih solvata ili solvata njegovih soli.
2. Spoj opće formule (I) prema patentnom zahtjevu 1, naznačen time što R1 predstavlja skupinu s formulom [image] u kojoj # predstavlja točku vezivanja za prsten 1,2,4-triazolil.
3. (2S)-3-[1-({5-Karbamoil-1-[3-(trifluorometil)piridin-2-il]-1H-1,2,4-triazol-3-il}metil)-3-(4-klorofenil)-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-1,1,1-trifluoropropan-2-il dihidrogenfosfat prema patentnom zahtjevu 1 s formulom u nastavku [image] ili jedna od njegovih farmaceutski prihvatljivih soli, njegovih solvata ili solvata njegovih soli.
4. (2S)-3-[1-({5-Karbamoil-1-[3-(trifluorometil)piridin-2-il]-1H-1,2,4-triazol-3-il}metil)-3-(4-klorofenil)-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-1,1,1-trifluoropropan-2-il dihidrogenfosfat prema patentnom zahtjevu 1 s formulom u nastavku [image]
5. Postupak za pripravu spoja opće formule (I) ili jedne od njegovih farmaceutski prihvatljivih soli, njegovih solvata ili solvata njegovih soli prema patentnom zahtjevu 1, naznačen time što [A] spoj s formulom [image] u kojoj R1 ima značenje kako je definirano za spojeve opće formule (I) navedeno u zahtjevu 1, reagira u prvom koraku s fosfornim oksikloridom i u drugom koraku se hidrolizira da se dobije spoj opće formule (I), ili [B] spoj s formulom [image] u kojoj R1 ima značenje kako je definirano za spojeve opće formule (I) navedeno u zahtjevu 1, reagira u prvom koraku s tetrabenzil difosfatom i u drugom koraku benzilne skupine su uklonjene pod redukcijskim uvjetima kako bi se dobio spoj opće formule (I), po izboru slijedi, gdje je prikladno, prevođenje spoja opće formule (I) u njegove odgovarajuće farmaceutski prihvatljive soli, njegove solvate ili solvate njegovih soli obradom s odgovarajućim otapalima i/ili bazama.
6. Spoj kako je definiran u bilo kojem od patentnih zahtjeva 1 do 4 naznačen time što je za upotrebu u liječenju i/ili prevenciji bolesti.
7. Spoj kako je definiran u bilo kojem od patentnih zahtjeva 1 do 4 naznačen time što je za upotrebu u liječenju i/ili prevenciji akutnih i kroničnih bubrežnih bolesti uključujući dijabetičku nefropatiju, akutno i kronično zatajenje srca, preeklampsiju, bolest perifernih arterija (PAD), koronarnu mikrovaskularnu disfunkciju (CMD), Rainaudov sindrom, dismenoreju, kardiorenalni sindrom, hipervolemijsku i euvolemijsku hiponatremiju, cirozu jetre, ascites, edem i sindrom neprimjerenog lučenja ADH (SIADH).
8. Upotreba spoja kako je definiran u bilo kojem od patentnih zahtjeva 1 do 4 naznačena time što je za proizvodnju farmaceutskog pripravka za liječenje i/ili prevenciju akutnih i kroničnih bubrežnih bolesti uključujući dijabetičku nefropatiju, akutno i kronično zatajenje srca, preeklampsiju, bolest perifernih arterija (PAD), koronarnu mikrovaskularnu disfunkciju (CMD), Rainaudov sindrom, dismenoreju, kardiorenalni sindrom, hipervolemijsku i euvolemijsku hiponatremiju, cirozu jetre, ascites, edem i sindrom neprimjerenog lučenja ADH (SIADH).
9. Farmaceutski pripravak naznačen time što sadrži spoj kako je definiran u bilo kojem od patentnih zahtjeva 1 do 4 i jednu ili više farmaceutski prihvatljivih pomoćnih tvari.
10. Farmaceutski pripravak prema patentnom zahtjevu 9 naznačen time što sadrži jedan ili više prvih aktivnih sastojaka, naročito spojeve opće formule (I) prema bilo kojem od zahtjeva 1 do 4, i jedan ili više daljnjih aktivnih sastojaka, naročito jedno ili više dodatnih terapijskih sredstava odabranih iz skupine koju čine diuretici, antagonisti All angiotenzina, inhibitori ACE, blokatori beta-receptora, antagonisti mineralokortikoidnih receptora, organski nitrati, donori NO, aktivatori i stimulatori topive gvanilat ciklaze, i pozitivno-inotropna sredstva, protuupalna sredstva, imunosupresivna sredstva, veziva fosfata i/ili spojevi koji moduliraju metabolizam vitamina D.
11. Farmaceutski pripravak kako je definiran u patentnom zahtjevu 9 ili 10 naznačen time što je za upotrebu u liječenju i/ili prevenciji akutnih i kroničnih bubrežnih bolesti uključujući dijabetičku nefropatiju, akutnog i kroničnog zatajenja srca, preeklampsije, bolesti perifernih arterija (PAD), koronarne mikrovaskularne disfunkcije (CMD), Rainaudovog sindroma, dismenoreje, kardiorenalnog sindroma, hipervolemijske i euvolemijske hiponatremije, ciroze jetre, ascites, edema i sindrom neprimjerenog lučenja ADH (SIADH).
HRP20220060TT 2017-10-24 2018-10-17 Predlijekovi supstituiranih derivata triazola i njihova upotreba HRP20220060T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP17197935 2017-10-24
PCT/EP2018/078364 WO2019081292A1 (en) 2017-10-24 2018-10-17 PRODRUGS OF SUBSTITUTED TRIAZOLE DERIVATIVES AND USES THEREOF
EP18785394.0A EP3700913B1 (en) 2017-10-24 2018-10-17 Prodrugs of substituted triazole derivatives and uses thereof

Publications (1)

Publication Number Publication Date
HRP20220060T1 true HRP20220060T1 (hr) 2022-04-15

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Country Status (38)

Country Link
US (1) US11298367B2 (hr)
EP (1) EP3700913B1 (hr)
JP (1) JP2021500365A (hr)
KR (1) KR20200069361A (hr)
CN (1) CN111225921A (hr)
AR (1) AR113791A1 (hr)
AU (1) AU2018356352A1 (hr)
BR (1) BR112020007983A2 (hr)
CA (1) CA3079767A1 (hr)
CL (1) CL2020001076A1 (hr)
CO (1) CO2020004945A2 (hr)
CR (1) CR20200176A (hr)
CU (1) CU24604B1 (hr)
CY (1) CY1124938T1 (hr)
DK (1) DK3700913T3 (hr)
DO (1) DOP2020000076A (hr)
EA (1) EA202091025A1 (hr)
EC (1) ECSP20023056A (hr)
ES (1) ES2906305T3 (hr)
HR (1) HRP20220060T1 (hr)
HU (1) HUE057278T2 (hr)
IL (1) IL273949A (hr)
JO (1) JOP20200099A1 (hr)
LT (1) LT3700913T (hr)
MA (1) MA50438B1 (hr)
MX (1) MX2020004191A (hr)
NI (1) NI202000030A (hr)
PE (1) PE20210394A1 (hr)
PH (1) PH12020550473A1 (hr)
PL (1) PL3700913T3 (hr)
PT (1) PT3700913T (hr)
RS (1) RS62984B1 (hr)
SG (1) SG11202003049WA (hr)
SI (1) SI3700913T1 (hr)
TW (1) TW201932117A (hr)
UA (1) UA126456C2 (hr)
UY (1) UY37948A (hr)
WO (1) WO2019081292A1 (hr)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021259852A1 (en) 2020-06-25 2021-12-30 Bayer Aktiengesellschaft Process for preparing 5-(alkoxycarbonyl)-and 5-(carboxamide)-1-aryl-1,2,4-triazole derivatives
WO2022112213A1 (en) 2020-11-30 2022-06-02 Bayer Aktiengesellschaft Crystalline forms of 3-[[3-(4-chlorophenyl)-5-oxo-4-((2s)-3,3,3-trifluoro- 2-hydroxypropyl)-4,5-dihydro-1h-1,2,4-triazol-1-yl]methyl]-1-[3- (trifluoromethyl)pyridin-2-yl]-1h-1,2,4-triazole-5-carboxamide

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Also Published As

Publication number Publication date
EP3700913A1 (en) 2020-09-02
NI202000030A (es) 2020-10-09
PT3700913T (pt) 2022-01-31
CO2020004945A2 (es) 2020-05-05
HUE057278T2 (hu) 2022-04-28
CL2020001076A1 (es) 2021-02-19
PH12020550473A1 (en) 2021-03-08
ECSP20023056A (es) 2020-12-31
MA50438B1 (fr) 2022-03-31
CY1124938T1 (el) 2023-01-05
DK3700913T3 (da) 2022-02-07
SI3700913T1 (sl) 2022-02-28
DOP2020000076A (es) 2020-08-31
TW201932117A (zh) 2019-08-16
EA202091025A1 (ru) 2020-07-30
MX2020004191A (es) 2020-08-03
CR20200176A (es) 2020-07-24
MA50438A (fr) 2020-09-02
KR20200069361A (ko) 2020-06-16
AU2018356352A1 (en) 2020-04-16
US11298367B2 (en) 2022-04-12
LT3700913T (lt) 2022-01-25
UY37948A (es) 2019-05-31
US20200338096A1 (en) 2020-10-29
SG11202003049WA (en) 2020-04-29
RS62984B1 (sr) 2022-03-31
PL3700913T3 (pl) 2022-02-21
JOP20200099A1 (ar) 2020-05-06
CU20200040A7 (es) 2021-03-11
JP2021500365A (ja) 2021-01-07
PE20210394A1 (es) 2021-03-02
ES2906305T3 (es) 2022-04-18
CA3079767A1 (en) 2019-05-02
AR113791A1 (es) 2020-06-10
WO2019081292A1 (en) 2019-05-02
UA126456C2 (uk) 2022-10-05
IL273949A (en) 2020-05-31
BR112020007983A2 (pt) 2020-10-27
EP3700913B1 (en) 2021-11-10
CN111225921A (zh) 2020-06-02
CU24604B1 (es) 2022-06-06

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