HRP20210748T1 - Postupak priprave spojeva s aktivnošću inhibitora hiv integraze - Google Patents

Postupak priprave spojeva s aktivnošću inhibitora hiv integraze Download PDF

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Publication number
HRP20210748T1
HRP20210748T1 HRP20210748TT HRP20210748T HRP20210748T1 HR P20210748 T1 HRP20210748 T1 HR P20210748T1 HR P20210748T T HRP20210748T T HR P20210748TT HR P20210748 T HRP20210748 T HR P20210748T HR P20210748 T1 HRP20210748 T1 HR P20210748T1
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HR
Croatia
Prior art keywords
inhivitory
activity
hiv integrase
producing compounds
maxima
Prior art date
Application number
HRP20210748TT
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English (en)
Inventor
Yukihito Sumino
Kazuya Okamoto
Moriyasu Masui
Daisu Yamada
Fumiya Ikarashi
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Shionogi & Co., Ltd.
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 Shionogi & Co., Ltd. filed Critical Shionogi & Co., Ltd.
Publication of HRP20210748T1 publication Critical patent/HRP20210748T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/94Oxygen atom, e.g. piperidine N-oxide
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79Acids; Esters
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79Acids; Esters
    • C07D213/80Acids; Esters in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Heat Sensitive Colour Forming Recording (AREA)

Claims (2)

1. Kristal spoja kojeg prikazuje formula (U2) ili njegovog solvata: [image] , (gdje je Me metil, a Bn je benzil) naznačen time što ima maksimume u difrakcijskom spektaru rendgenskih zraka na prahu pod difrakcijskim kutom (2θ): 7,3° ± 0,2°, 14,4° ± 0,2°, 16,1° ± 0,2°, 18,4° ± 0,2°, 22,3° ± 0,2° i 23,1° ± 0,2°.
2. Kristal spoja kojeg prikazuje formula (U3) ili njegovog solvata: [image] , (gdje je Me metil, a Bn je benzil) naznačen time što ima maksimume u difrakcijskom spektaru rendgenskih zraka na prahu pod difrakcijskim kutom (2θ): 7,2° ± 0,2°, 16,1° ± 0,2°, 18,3° ± 0,2°, 20,6° ± 0,2°, 22,6° ± 0,2°, 23,1° ± 0,2° i 23,7° ± 0,2°.
HRP20210748TT 2010-08-05 2021-05-12 Postupak priprave spojeva s aktivnošću inhibitora hiv integraze HRP20210748T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2010175899 2010-08-05
JP2010277713 2010-12-14
EP18203589.9A EP3456721B1 (en) 2010-08-05 2011-08-04 Method of producing compounds having hiv integrase inhivitory activity

Publications (1)

Publication Number Publication Date
HRP20210748T1 true HRP20210748T1 (hr) 2021-06-25

Family

ID=45559561

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20210748TT HRP20210748T1 (hr) 2010-08-05 2021-05-12 Postupak priprave spojeva s aktivnošću inhibitora hiv integraze

Country Status (18)

Country Link
US (8) US20140011995A1 (hr)
EP (3) EP3456721B1 (hr)
JP (1) JP5636054B2 (hr)
CN (3) CN106083891B (hr)
BR (1) BR112013002461A2 (hr)
CY (1) CY1124582T1 (hr)
DK (1) DK3456721T3 (hr)
ES (3) ES2710609T3 (hr)
HR (1) HRP20210748T1 (hr)
HU (1) HUE054473T2 (hr)
LT (1) LT3456721T (hr)
PL (1) PL3456721T3 (hr)
PT (3) PT3456721T (hr)
RS (1) RS61796B1 (hr)
SG (1) SG187683A1 (hr)
SI (1) SI3456721T1 (hr)
TW (1) TWI510451B (hr)
WO (1) WO2012018065A1 (hr)

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Also Published As

Publication number Publication date
US9969750B2 (en) 2018-05-15
TWI510451B (zh) 2015-12-01
LT3456721T (lt) 2021-07-12
US10125147B2 (en) 2018-11-13
PT2602260T (pt) 2016-12-27
EP3456721A2 (en) 2019-03-20
EP2602260B1 (en) 2016-09-28
CN106083891A (zh) 2016-11-09
ES2608377T3 (es) 2017-04-10
US9802959B2 (en) 2017-10-31
EP3127908A2 (en) 2017-02-08
US20180044351A1 (en) 2018-02-15
BR112013002461A2 (pt) 2016-05-24
CN106046022B (zh) 2018-06-19
RS61796B1 (sr) 2021-06-30
PT3456721T (pt) 2021-05-04
US20180037591A1 (en) 2018-02-08
TW201210990A (en) 2012-03-16
US10000508B2 (en) 2018-06-19
PL3456721T3 (pl) 2021-10-25
SI3456721T1 (sl) 2021-05-31
EP2602260A4 (en) 2014-01-01
JP5636054B2 (ja) 2014-12-03
ES2710609T3 (es) 2019-04-26
HUE054473T2 (hu) 2021-09-28
US9650394B2 (en) 2017-05-16
SG187683A1 (en) 2013-03-28
PT3127908T (pt) 2019-02-04
US9321789B2 (en) 2016-04-26
CY1124582T1 (el) 2022-07-22
US10125146B2 (en) 2018-11-13
CN103154004A (zh) 2013-06-12
ES2870006T3 (es) 2021-10-26
US20150038702A1 (en) 2015-02-05
EP3127908B1 (en) 2018-11-28
CN106083891B (zh) 2018-03-23
JPWO2012018065A1 (ja) 2013-10-03
DK3456721T3 (da) 2021-04-26
WO2012018065A1 (ja) 2012-02-09
EP3127908A3 (en) 2017-02-15
EP3456721B1 (en) 2021-02-24
US20180037593A1 (en) 2018-02-08
CN103154004B (zh) 2016-07-06
US20160229870A1 (en) 2016-08-11
US20180037592A1 (en) 2018-02-08
EP3456721A3 (en) 2019-03-27
US20140011995A1 (en) 2014-01-09
EP2602260A1 (en) 2013-06-12
US20170240564A1 (en) 2017-08-24
CN106046022A (zh) 2016-10-26

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