HRP20140010T1 - Derivati 5-amino-2-(1-hidroksi-etil)-tetrahidropirana - Google Patents

Derivati 5-amino-2-(1-hidroksi-etil)-tetrahidropirana Download PDF

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HRP20140010T1
HRP20140010T1 HRP20140010AT HRP20140010T HRP20140010T1 HR P20140010 T1 HRP20140010 T1 HR P20140010T1 HR P20140010A T HRP20140010A T HR P20140010AT HR P20140010 T HRP20140010 T HR P20140010T HR P20140010 T1 HRP20140010 T1 HR P20140010T1
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compound
amino
methoxy
pyran
tetrahydro
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HRP20140010AT
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Christian Hubschwerlen
Georg Rueedi
Jean-Philippe Surivet
Cornelia Zumbrunn Acklin
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Actelion Pharmaceuticals Ltd.
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/056Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D497/00Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D497/02Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D497/04Ortho-condensed systems
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Claims (17)

1. Spoj, naznačen time, da ima formulu I [image] u kojoj R1 predstavlja alkoksi; R2 predstavlja H ili F; gdje svaki od R3, R4, R5 i R6 predstavlja neovisno H ili D; V predstavlja CH i W predstavlja CH ili N, ili V predstavlja N i W predstavlja CH; Y predstavlja CH ili N; Z predstavlja O, S ili CH2; i A predstavlja CH2, CH2CH2 ili CD2CD2; ili sol takvoga spoja.
2. Spoj formule I prema zahtjevu 1, naznačen time, da svaki od R3, R4, R5 i R6 predstavlja H i A predstavlja CH2 ili CH2CH2; ili sol takvoga spoja.
3. Spoj formule I prema zahtjevu 1, naznačen time, da - R1 predstavlja (C1- C3) alkoksi; i - najviše jedan od R3, R4, R5 i R6 predstavlja D i A predstavlja CH2 ili CH2CH2, ili svaki od R3, R4, R5 i R6 predstavlja H i A predstavlja CH2, CH2CH2 ili CD2CD2; ili sol takvoga spoja.
4. Spoj formule I prema zahtjevu 1 ili 2, naznačen time, da je to također spoj formule Ip [image] u kojoj R1 predstavlja alkoksi; R2 predstavlja H ili F; W predstavlja CH ili N; Y predstavlja CH ili N; Z predstavlja O, S ili CH2; i n predstavlja 0 ili 1; ili sol takvoga spoja.
5. Spoj formule I prema jednom od zahtjeva 1 do 4, naznačen time, da R1 je metoksi; ili sol takvoga spoja.
6. Spoj formule I prema jednom od zahtjeva 1 do 5, naznačen time, da R2 predstavlja H; ili sol takvoga spoja.
7. Spoj formule I prema jednom od zahtjeva 1 do 5, naznačen time, da R2 predstavlja F; ili sol takvoga spoja.
8. Spoj formule I prema jednom od zahtjeva 1 do 7, naznačen time, da Wpredstavlja N; ili sol takvoga spoja.
9. Spoj formule I prema jednom od zahtjeva 1 do 7, naznačen time, da Wpredstavlja CH; ili sol takvoga spoja.
10. Spoj formule I prema jednom od zahtjeva 1 do 9, naznačen time, da Ypredstavlja CH; ili sol takvoga spoja.
11. Spoj formule I prema jednom od zahtjeva 1 do 9, naznačen time, da Ypredstavlja N; ili sol takvoga spoja.
12. Spoj formule I prema zahtjevu 1, naznačen time, da je on odabran od sljedećih: -(1S)-1-{(1S,5R)-5-[(2,3-dihidro-[1,4]dioksino[2,3-c]piridin-7-ilmetil)-amino]-tetrahidro-piran-2-il}-2-(6-metoksi-[1,5]naftiridin-4-il)-etanol; -(1S)-1-{(2S,5R)-5-[(6,7-dihidro-[1,4]dioksino[2,3-c]piridazin-3-ilmetil)-amino]-tetrahidro-piran-2-il}-2-(6-metoksi-[1,5]naftiridin-4-il)-etanol; -(1S)-1-{(2S,5R)-5-[(2,3-dihidro-[1,4]dioksino[2,3-c]piridin-7-ilmetil)-amino]-tetrahidro-piran-2-il}-2-(3-fluoro-6-metoksi-[1,5]naftiridin-4-il)-etanol; -(1S)-1-{(2S,5R)-5-[(6,7-dihidro-[1,4]dioksino [2,3-c]piridazin-3-ilmetil)-amino]-tetrahidro-piran-2-il}-2-(3-fluoro-6-metoksi-[1,5]naftiridin-4-il)-etanol; -(1S)-1-{(2S,5R)-5-[(2,3-dihidro-[1,4]dioksino[2,3-c]piridin-7-ilmetil)-amino]-tetrahidro-piran-2-il}-2-(7-fluoro-2-metoksi-kinolin-8-il)-etanol; -(1S) -1-{(2S,5R)-5-[(2,3-dihidro-4-oksa-1-tia-6-aza-naftalen-7-ilmetil)-amino]-tetrahidro-piran-2-il}-2-(3-fluoro-6-metoksi-[1,5]naftiridin-4-il)-etanol; -(1S)-1-{(2S,5R)-5-[(2,3-dihidro-4-oksa-1-tia-6-aza-naftalen-7-ilmetil)-amino]-tetrahidro-piran-2-il}-2-(7-fluoro-2-metoksi-kinolin-8-il)-etanol; -(1S)-2-(3-fluoro-6-metoksi-[1,5]naftiridin-4-il)-1-{(2S,5R)-5-[(3-oksa-1-tia-5-aza-indan-6-ilmetil)-amino]-tetrahidro-piran-2-il}-etanol; -(1S)-2-(7-fluoro-2-metoksi-kinolin-8-il)-1-{(2S,5R)-5-[(3-oksa-1-tia-5-aza-indan-6-ilmetil)-amino]-tetrahidro-piran-2-il}-etanol; -(1S)-1-{(2S,5R)-5-[(3,4-dihidro-2H-pirano[2,3-c]piridin-6-ilmetil)-amino]-tetrahidro-piran-2-il}-2-(3-fluoro-6-metoksi-[1,5]naftiridin-4-il)-etanol; -(1S)-1-{(2S,5R)-5-[(6,7-dihidro-8-oksa-5-tia-1,2-diaza-naftalen-3-ilmetil)-amino]-tetrahidro-piran-2-il}-2-(3-fluoro-6-metoksi-[1,5]naftiridin-4-il)-etanol; -(1S)-1-{(2S,5R)-5-[(2,3-dihidro-[1,4]dioksino[2, 3-c]piridin-7-ilmetil)-amino]-tetrahidro-piran-2-il}-2-(6-fluoro-3-metoksi-kinoksalin-5-il)-etanol; -(1S)-1-{(2S,5R)-5-[(6,7-dihidro-[1,4]dioksino[2,3-c]piridazin-3-ilmetil)-amino]-tetrahidro-piran-2-il}-2-(6-fluoro-3-metoksi-kinoksalin-5-il)-etanol; -(1S)-1-{(2S,5R)-5-[(2,3-dihidro-4-oksa-1-tia-6-aza-naftalen-7-ilmetil)-amino]-tetrahidro-piran-2-il}-2-(6-fluoro-3-metoksi-kinoksalin-5-il)-etanol; -(1S)-1-{(2S,5R)-5-[(6,7-dihidro-8-oksa-5-tia-1,2-diaza-naftalen-3-ilmetil)-amino]-tetrahidro-piran-2-il}-2-(6-fluoro-3-metoksi-kinoksalin-5-il)-etanol; -(1S)-1-((2S,5R)-5-(((2,3-dihidro-[1,4]dioksino[2,3-c]piridin-7-il)metil-d1)amino)tetrahidro-2H-piran-2-il)-2-(3-fluoro-6-metoksi-1,5-naftiridin-4-il) etanol; -(1S)-1-((2S,5R)-5-(((2,3-dihidro-[1,4]dioksino-2,2,3,3-d4-[2,3-c]piridin-7-il) metil)amino) tetrahidro-2H-piran-2-il)-2-(3-fluoro-6-metoksi-1,5-naftiridin-4-il)-etanol; -(1S)-1-((2S,SR)-5-(((2,3-dihidro-[1,4]dioksino[2,3-c]piridin-7-il)metil)amino)tetrahidro-2H-piran-2-il)-2-(3-fluoro-6-metoksi-1,5-naftiridin-4-il)etanol-1-d1; -(S)-1-((2S,5R)-5-(((2,3-dihidro-[1,4]oksatiino[2,3-c]piridin-7-il)metil-d1)amino)tetrahidro-2H-piran-2-il)-2-(3-fluoro-6-metoksi-1,5-naftiridin-4-il)-etanol; -(1S)-1-((2S,5R)-5-(((2,3-dihidro-[1,4]dioksino-[2,3-c]piridin-7-il)metil)amino)tetrahidro-2H-piran-2-il)-2-(3-fluoro-6-metoksi-1,5-naftiridin-4-il)-etanol-2-d1; -(S)-1-((2S,5R)-5-(((2,3-dihidro-[1,4]oksatiino[2,3-c]piridin-7-il)metil)amino)tetrahidro-2H-piran-2-il)-2-(3-fluoro-6-metoksi-1,5-naftiridin-4-il)-etanol-2-d1; -(S)-1-((2S,5R)-5-(((2,3-dihidro-[1,4]oksatiino[2,3-c]piridin-7-il)metil)amino)tetrahidro-2H-piran-2-il)-2-(3-fluoro-6-metoksi-1,5-naftiridin-4-il)-etanol-1-d1; -(S)-1-{(2S,SR)-5-[(6,7-dihidro-8-oksa-5-tia-1,2-diaza-naftalen-3-ilmetil-d1)-amino]-tetrahidro-piran-2-il}-2-(3-fluoro-6-metoksi-[1,5]naftiridin-4-il)-etanol; -(1S)-1-((2S,5R)-5-(((2,3-dihidro-[1,4]dioksino[2,3-c]piridin-7-il)metil-d2)amino)tetrahidro-2H-piran-2-il)-2-(3-fluoro-6-metoksi-1,5-naftiridin-4-il)-etanol; ili sol takvoga spoja.
13. Spoj formule I prema zahtjevu 1, naznačen time, da je on (1S)-1-{(2S,5R)-5-[(6,7-dihidro-8-oksa-5-tia-1,2-diaza-naftalen-3-ilmetil)-amino]-tetrahidro-piran-2-il}-2-(3-fluoro-6-metoksi-[1,5]naftiridin-4-il)-etanol; ili sol takvoga spoja.
14. Spoj formule I prema jednom od zahtjeva 1 do 13, ili njegova farmacutski prihvatljiva sol, naznačen(a) time, da se upotrebljava kao lijek.
15. Farmaceutski sastav, naznačen time, da kao djelotvorni sastojak sadrži spoj formule I prema jednom od zahtjeva 1 do 13 ili njegovu farmaceutski prihvatljivu sol te najmanje jedno terapeutski inertno pomoćno sredstvo.
16. Uporaba spoja formule I prema jednom od zahtjeva 1 do 13 ili njegove farmaceutski prihvatljive soli, naznačena time, da je za proizvodnju lijeka za sprečavanje ili liječenje bakterijske infekcije.
17. Spoj formule I prema jednom od zahtjeva 1 do 13 ili njegova farmaceutski prihvatljiva sol, naznačen(a) time, da se upotrebljava za sprečavanje ili liječenje bakterijske infekcije.
HRP20140010AT 2008-12-12 2014-01-07 Derivati 5-amino-2-(1-hidroksi-etil)-tetrahidropirana HRP20140010T1 (hr)

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IB2008055261 2008-12-12
PCT/IB2009/055689 WO2010067332A1 (en) 2008-12-12 2009-12-11 5-amino-2-(1-hydroxy-ethyl)-tetrahydropyran derivatives

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CL2011001413A1 (es) 2011-11-11
CN102232078A (zh) 2011-11-02
RU2011128550A (ru) 2013-01-20
ZA201105095B (en) 2012-12-27
AU2009325902B2 (en) 2015-01-29
US8211890B2 (en) 2012-07-03
SI2376497T1 (sl) 2014-01-31
CN102232078B (zh) 2014-07-16
IL213432A (en) 2013-11-28
RU2525541C2 (ru) 2014-08-20
EP2376497A1 (en) 2011-10-19
BRPI0924081A2 (pt) 2018-03-20
KR101297450B1 (ko) 2013-08-20
CA2744456C (en) 2017-09-26
KR20110086643A (ko) 2011-07-28
CY1114869T1 (el) 2016-12-14
JP4955835B2 (ja) 2012-06-20
EP2376497B1 (en) 2013-09-18
MA32956B1 (fr) 2012-01-02
SG172088A1 (en) 2011-07-28
WO2010067332A1 (en) 2010-06-17
PT2376497E (pt) 2013-11-21
NZ593891A (en) 2013-05-31
TWI426076B (zh) 2014-02-11
AR074604A1 (es) 2011-01-26
TW201026699A (en) 2010-07-16
MX2011005905A (es) 2011-06-20
US20110245259A1 (en) 2011-10-06
MY159183A (en) 2016-12-30

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