HRP20170154T1 - Analozi antibakterijskog aminoglikozida - Google Patents

Analozi antibakterijskog aminoglikozida Download PDF

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HRP20170154T1
HRP20170154T1 HRP20170154TT HRP20170154T HRP20170154T1 HR P20170154 T1 HRP20170154 T1 HR P20170154T1 HR P20170154T T HRP20170154T T HR P20170154TT HR P20170154 T HRP20170154 T HR P20170154T HR P20170154 T1 HRP20170154 T1 HR P20170154T1
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hydroxy
amino
sisomycin
hydrogen
compound
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HRP20170154TT
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James Aggen
Adam Aaron Goldblum
Martin Linsell
Paola Dozzo
Heinz Ernst Moser
Darin Hildebrandt
Micah Gliedt
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Achaogen, Inc.
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Publication of HRP20170154T1 publication Critical patent/HRP20170154T1/hr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20—Carbocyclic rings
    • C07H15/22—Cyclohexane rings, substituted by nitrogen atoms
    • C07H15/222—Cyclohexane rings substituted by at least two nitrogen atoms
    • C07H15/224—Cyclohexane rings substituted by at least two nitrogen atoms with only one saccharide radical directly attached to the cyclohexyl radical, e.g. destomycin, fortimicin, neamine
    • 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
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/7036—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20—Carbocyclic rings
    • C07H15/22—Cyclohexane rings, substituted by nitrogen atoms
    • C07H15/222—Cyclohexane rings substituted by at least two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20—Carbocyclic rings
    • C07H15/22—Cyclohexane rings, substituted by nitrogen atoms
    • C07H15/222—Cyclohexane rings substituted by at least two nitrogen atoms
    • C07H15/226—Cyclohexane rings substituted by at least two nitrogen atoms with at least two saccharide radicals directly attached to the cyclohexane rings
    • C07H15/234—Cyclohexane rings substituted by at least two nitrogen atoms with at least two saccharide radicals directly attached to the cyclohexane rings attached to non-adjacent ring carbon atoms of the cyclohexane rings, e.g. kanamycins, tobramycin, nebramycin, gentamicin A2
    • C07H15/236—Cyclohexane rings substituted by at least two nitrogen atoms with at least two saccharide radicals directly attached to the cyclohexane rings attached to non-adjacent ring carbon atoms of the cyclohexane rings, e.g. kanamycins, tobramycin, nebramycin, gentamicin A2 a saccharide radical being substituted by an alkylamino radical in position 3 and by two substituents different from hydrogen in position 4, e.g. gentamicin complex, sisomicin, verdamycin
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
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  • Genetics & Genomics (AREA)
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  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)

Claims (25)

1. Spoj, naznačen time, da ima sljedeću strukturu (I): [image] ili stereoizomer, farmaceutski prihvatljiva sol, pri čemu: Q1 je vodik, [image] Q2 je vodik, po izboru supstituirani aril, po izboru supstituirani aralkil, po izboru supstituirani cikloalkil, po izboru supstituirani cikloalkilalkil, po izboru supstituirani hetcrociklil, po izboru supstituirani hetcrociklilalkil, po izboru supstituirani heteroaril, po izboru supstituirani hetcroarilalkil, -C(=NH)NR4R5, (CR10R11)pR12, [image] Q3 je vodik, po izboru supstituirani aril, po izboru supstituirani aralkil, po izboru supstituirani cikloalkil, po izboru supstituirani cikloalkilalkil, po izboru supstituirani hetcrociklil, po izboru supstituirani heterociklilalkil, po izboru supstituirani heteroaril, po izboru supstituirani heteroarilalkil, -C(=NH)NR4R5, (CR10R11)pR12, [image] svaki R1, R2, R3, R4, R5, R8 and R10 je, neovisno, vodik ili C1-C6 alkil ili R1 i R2 zajedno s atomima za kojih su vezani mogu tvoriti heterociklički prsten koji ima od 4 do 6 atoma prstena ili R1 i R3 zajedno s atomima za kojih su vezani mogu tvoriti heterociklički prsten koji ima od 4 do 6 atoma prstena ili R1 i R3 zajedno s atomima za kojih su vezani mogu tvoriti heterociklički prsten koji ima od 4 do 6 atoma prstena ili R4 i R5 zajedno s atomima za kojih su vezani mogu tvoriti heterociklički prsten koji ima od 4 do 6 atoma prstena; svaki R6 i R7 je, neovisno, vodik, hidroksil, amino ili C1-C6 alkil ili R6 i R7 zajedno s atomima za kojih su vezani mogu tvoriti heterociklički prsten koji ima od 4 do 6 atoma prstena; svaki R9 je, neovisno, vodik ili metil; svaki R11 je, neovisno, vodik, hidroksil, amino ili C1-C6 alkil; svaki R12 je, neovisno, hidroksil ili amino; svaki n je, neovisno, cijeli broj od 0 do 4; svaki m je, neovisno, cijeli broj od 0 do 4 i svaki p je, neovisno, cijeli broj od 1 do 5 a pri čemu je (i) najmanje dva od Q1 Q2i Q3 su drugačiji od vodika i (ii) ako Q1, je vodik, tada najmanje jedan od Q2 i Q3 je -C(=NH)N R4R5.
2. Spoj iz patentnog zahtjeva 1, naznačen time, da je R8 vodik.
3. Spoj iz patentnog zahtjeva 1 ili 2, naznačen time, da je svaki R9 metil.
4. Spoj prema bilo koje od patentnih zahtjeva 1-3, naznačen time, da Q1 i Q2 nisu vodik.
5. Spoj iz patentnog zahtjeva 4, naznačen time, da je Q3 vodik.
6. Spoj iz patentnog zahtjeva 4 ili 5, naznačen time, da je Q1: [image] pri čemu: R1 je vodik; R2 je vodik i svaki R3 je vodik.
7. Spoj iz patentnog zahtjeva 6, naznačen time da je Q1 [image]
8. Spoj iz patentnog zahtjeva 4 ili 5, naznačen time da je Q1: [image] pri čemu: R1 je vodik; i R2 i R3 zajedno s atomima za kojih su vezani tvore heterociklički prsten koji ima od 4 do 6 atoma prstena.
9. Spoj iz patentnog zahtjeva 4 ili 5, naznačen time da je Q1: [image] pri čemu: R3 je vodik; i R1 i R2 zajedno s atomima za kojih su vezani tvore heterociklički prsten koji ima od 4 do 6 atoma prstena.
10. Spoj iz patentnog zahtjeva 4 ili 5, naznačen time da je Q1: [image] pri čemu: R2 je vodik; i R1 i R3 zajedno s atomima za koje su vezani tvore karbociklički prsten koji ima od 4 do 6 atoma prstena.
11. Spoj iz patentnog zahtjeva 4 ili 5, naznačen time da je Q1: [image] pri čemu: R2 je vodik; i svaki R3 je vodik.
12. Spoj iz patentnog zahtjeva 4 ili 5, naznačen time da je Q1: [image] pri čemu: R2 je vodik; i svaki R2 je vodik.
13. Spoj prema bilo kojem od patentnih zahtjeva 4-12, naznačen time, da je Q2 (CR10R11)pR12-
14. Spoj iz patentnog zahtjeva 13, naznačen time, da je svaki R10 vodik.
15. Spoj iz patentnog zahtjeva 14, naznačen time, da je svaki R11 vodik.
16. Spoj prema bilo kojem od patentnih zahtjeva 4-12, naznačen time, da je Q2 po izbom supstituiran s cikoalkilalkilom.
17. Spoj prema bilo kojem od patentnih zahtjeva 4-12, naznačen time, da je Q2 po izboru supstituiran s heterocikloalkilom.
18. Spoj iz patentnog zahtjeva 4, naznačen time, da je spoj: 6'-(2-Hidroksi-etil)-1-(4-amino-2(S)-hidroksi-butiril)-sizomicin; 6'-(2-Hidroksi-etil)-1-(4-amino-2(R)-hidroksi-butiril)-sizomicin; 6'-(2-Hidroksi-propanol)-1-(4-amino-2(R)-hidroksi-butiril)-sizomicin; 6'-(Metil-pipcridin-4-il)-1-(4-amino-2(R)-hidroksi-butiril)-sizomicin; 6'-(Metil-ciklopropil)-1-(4-amino-2(R)-hidroksi-butiril)-sizomicin; 6'-(3-Amino-propil)-1-(4-amino-2(R)-hidroksi-butiril)-sizomicin; 6'-Metil-ciklopropil-l-(3-amino-2(R)-hidroksi-propionil)-sizomicin; 6'-Metil-pipcridinil-l-(3-amino-2(R)-hidroksi-propionil)-sizomicin; 6'-(2-Hidroksi-etil)-1-(3-amino-2(R)-hidroksi-propionil)-sizomicin; 6'-(2-Hidroksi-propanol)-1-(3-amino-2(R)-hidroksi-propionil)-sizomicin; 6'-(3-Amino-propil)-1-(3-amino-2(R)-hidroksi-propionil)-sizomicin; 6'-(Metil-pipcridin-4-il)-1-(4-amino-2(S)-hidroksi-butiril)-sizomicin; 6'-(Metil-ciklopropil)-1-(3-amino-2(S)-hidroksi-propionil)-sizomicin; 6'-(2-Hidroksi-propanol)-1-(3-amino-2(S)-hidroksi-propionil)-sizomicin; 6'-(Metil-pipcridin-4-il)-1-(3-amino-2(S)-hidroksi-propionil)-sizomicin; 6'-(2-Hidroksi-etil)-1-(3-amino-2(S)-hidroksi-propionil)-sizomicin; 6'-(3-Amino-propil)-1-(3-amino-2(S)-hidroksi-propionil)-sizomicin; 6'-(Metil-ciklopropil)-1-(4-amino-2(S)-hidroksi-butiril)-sizomicin; 6'-(2-Hidroksi-propanol)-1-(4-amino-2(S)-hidroksi-butiril)-sizomicin, 6'-(3-Amino-2-hidroksi-propil)-1-(3-amino-2(S)-hidroksi-propionil)-sizomicin; 6'-(2-Hidroksi-etil)-1 -(2-hidroksi-acetil)-sizomicin; 6'-(3-Amino-propil)-1-(2-amino-etilsulfonamid)-sizomicin; 6'-(2-Hidroksi-propanol)-1-(2-amino-etilsulfonamid)-sizomicin; 6'-(2(S)-Hidroksi-propanol)-1-(4-amino-2(S)-hidroksi-butiril)-sizomicin; 6'-(2-Hidroksi-etil)-1-(2-amino-etilsulfonamid)-sizomicin; 6'-(Metil-trans-3-amino-ciklobutil)-1-(4-amino-2(S)-hidroksi-butiril)-sizomicin; 6'-(2-Hidroksi-etil)-1-(3-hidroksi-pirolidin-3-il-acetil)-sizomicin; 6'-(2-Hidroksi-4-amino-butil)-1-(3-hidroksi-pirolidin-3-il-acetil)-sizomicin; 6'-(Metil-ciklopropil)-1-(3-hidroksi-azetidin-3-il-acetil)-sizomicin; 6'-(2-Hidroksi-etil)-1-(3-hidroksi-azetidin-3-il-acetil)-sizomicin; 6'-(Metil-(l-hidroksi-3-Metilamino-ciklobutil)-1-(4-amino-2(S)-hidroksi-butiril)-sizomicin; 6'-(3-Amino-propil)-1-(3-hidroksi-pirolidin-3-il-acetil)-sizomicin; 6'-(Metil-ciklopropil)-1-(3-hidroksi-pirolidin-3-il-acetil)-sizomicin; 6'-(2-Hidroksi-3-amino-propil)-1-(3-hidroksi-pirolidin-3-il-acetil)-sizomicin; 6'-(3-Amino-propil)-1-(4-amino-2(S)-hidroksi-butiril)-sizomicin; 6'-(Metil-pirolidin-2-il)-1-(4-amino-2(S)-hidroksi-butiril)-sizomicin; 6'-(3-Amino-propil)-1-(3-hidroksi-azetidin-3-il-acetil)-sizomicin; 6'-(3-Amino-propil)-1-(l-hidroksi-3-amino-ciklobutil-acetil)-sizomicin; 6'-(Metil-trans-3-amino-ciklobutil)-1-(3-amino-2(S)-hidroksi-propionil)-sizomicin; 6'-(Metil-trans-3-amino-ciklobutil)-1 -(1 -hidroksi-3-amino-ciklobutil-acetil)-sizomicin; 6'-(2-Hidroksi-etil)-1-(l-hidroksi-3-amino-ciklobutil-acetil)-sizomicin; 6'-Metilciklopropil-l-(2-(azetidin-3-il)-2-hidroksi-acetil)-sizomicin; 6'-(Metil-trans-3-amino-ciklobutil)-1-(2-(azetidin-3-il)-2-hidroksi-acetil)-sizomicin; 6'-(2-Hidroksi-etil)-1-(2-(azetidin-3-il)-2-hidroksi-acetil)-sizomicin; 6'-(3-Amino-propil)-1-(2-(azetidin-3-il)-2-hidroksi-acetil)-sizomicin; 6'-(Metil-trans-3-amino-ciklobutil)-1-(3-hidroksi-pirolidin-3-il-acetil)-sizomicin; 6'-(2-Hidroksi-3-amino-propil)-1-(2-(azetidin-3-il)-2-hidroksi-acetil)-sizomicin; ili 6'-(Metil-3-amino-l-hidroksi-ciklobutil)-1-(2-(azetidin-3-il)-2-hidroksi-acetil)-sizomicin.
19. Spoj prema bilo kojem od patentnih zahtjeva 1-3, naznačen time, da su Q1 i Q3 različiti od vodika.
20. Spoj iz patentnog zahtjeva 19, naznačen time, da je Q2 vodik.
21. Spoj prema bilo kojem od patentnih zahtjeva 1-3, naznačen time, da su Q2 i Q3 različiti od vodika.
22. Spoj iz patentnog zahtjeva 21, naznačen time, da je Q1 vodik.
23. Farmaceutski pripravak, naznačen time, da sadrži spoj iz bilo kojeg od patentnih zahtjeva 1-22 ili stereoizomer, farmaceutski prihvatljivu sol i farmaceutski prihvatljiv nosač, razrjeđivač ili ekscipijens.
24. Spoj prema bilo kojem od patentnih zahtjeva 1-22 ili pripravak iz patentnog zahtjeva 23, naznačen time, da se koristi za liječenje bakterijske infekcije kod sisavaca kojima je potrebno liječenje.
25. Spoj iz patentnog zahtjeva 4, naznačen time, da je spoj 6'-(2-Hidroksi-etil)-1-(4-amino-2(S)-hidroksi- butiril)-sizomicin.
HRP20170154TT 2007-11-21 2017-01-31 Analozi antibakterijskog aminoglikozida HRP20170154T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US98964507P 2007-11-21 2007-11-21
EP08851633.1A EP2217610B1 (en) 2007-11-21 2008-11-21 Antibacterial aminoglycoside analogs
PCT/US2008/084399 WO2009067692A1 (en) 2007-11-21 2008-11-21 Antibacterial aminoglycoside analogs

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HRP20170154T1 true HRP20170154T1 (hr) 2017-03-24

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US (5) US8383596B2 (hr)
EP (2) EP2217610B1 (hr)
JP (2) JP4986310B2 (hr)
KR (1) KR101296099B1 (hr)
CN (2) CN101868472B (hr)
AU (1) AU2008326297B2 (hr)
BR (1) BRPI0819319B8 (hr)
CA (1) CA2706369C (hr)
CY (1) CY1118915T1 (hr)
DK (1) DK2217610T3 (hr)
EA (1) EA017824B1 (hr)
ES (1) ES2613936T3 (hr)
HR (1) HRP20170154T1 (hr)
HU (1) HUE030523T2 (hr)
IL (1) IL205880A (hr)
LT (1) LT2217610T (hr)
MX (1) MX2010005632A (hr)
PL (1) PL2217610T3 (hr)
PT (1) PT2217610T (hr)
SI (1) SI2217610T1 (hr)
TW (1) TWI425947B (hr)
WO (1) WO2009067692A1 (hr)

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CN110885350A (zh) * 2019-08-28 2020-03-17 山东安信制药有限公司 一种普拉佐米星的制备方法
CN110642907B (zh) * 2019-10-12 2020-11-06 上海博璞诺科技发展有限公司 普拉唑米星或其盐的合成方法
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