HRP20110408T1 - Inhibitori nukleozidnih fosforilaza i hidrolaza acikličkog amina - Google Patents

Inhibitori nukleozidnih fosforilaza i hidrolaza acikličkog amina Download PDF

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HRP20110408T1
HRP20110408T1 HR20110408T HRP20110408T HRP20110408T1 HR P20110408 T1 HRP20110408 T1 HR P20110408T1 HR 20110408 T HR20110408 T HR 20110408T HR P20110408 T HRP20110408 T HR P20110408T HR P20110408 T1 HRP20110408 T1 HR P20110408T1
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compound according
pyrrolo
pyrimidin
hydroxy
methyl
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HR20110408T
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English (en)
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Clinch Keith
Brian Evans Gary
Hubert Furneaux Richard
Michael Kelly Peter
L. Schramm Vern
Charles Tyler Peter
David Woolhouse Anthony
Ashwin Gulab Shivali
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Industrial Research Limited
Albert Einstein College Of Medicine Of Yeshiva University
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Publication of HRP20110408T1 publication Critical patent/HRP20110408T1/hr

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
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    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06Antimalarials
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
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    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

Spoj formule (I): naznačen time da: R4 je dihidroksipropil, dihidroksibutil, trihidroksibutil, dihidroksipentil ilitrihidroksipentil; A je N ili CH; B je OH ili alkoksi; iD je H, OH, NH2, ili SCH3;ili njegov tautomer ili njegova farmaceutski prihvatljiva sol ili njegov ester oblika prolijeka. Patent sadrži još 14 patentnih zahtjeva.

Claims (15)

1. Spoj formule (I): [image] naznačen time da: R4 je dihidroksipropil, dihidroksibutil, trihidroksibutil, dihidroksipentil ili trihidroksipentil; A je N ili CH; B je OH ili alkoksi; i D je H, OH, NH2, ili SCH3; ili njegov tautomer ili njegova farmaceutski prihvatljiva sol ili njegov ester oblika prolijeka.
2. Spoj prema zahtjevu 1 naznačen time da A je CH.
3. Spoj prema zahtjevu 1 ili zahtjevu 2 naznačen time da B je OH.
4. Spoj prema bilo kojem od zahtjeva 1 do 3 naznačen time da D je H ili NH2.
5. Spoj prema bilo kojem od zahtjeva 1 do 4 naznačen time da D je H.
6. Spoj prema zahtjevu 1, naznačen time da ima formulu: [image]
7. Spoj prema zahtjevu 1 naznačen time da je: (2R*,3S*)-3-((4-hidroksi-5H-pirolo[3,2-d]pirimidin-7-il)metilamino)butan-1,2,4-triol; (R)-3-((4-hidroksi-5H-pirolo[3,2-d]pirimidin-7-il)metilamino)-propan-1,2-diol hidroklorid; (2R,3R)-3-((4-hidroksi-5H-pirolo[3,2-d]pirimidin-7-il)metilamino)butan-1,2,4-triol hidroklorid; 2-amino-7-((2,4-dihidroksibutilamino)metil)-3H-pirolo[3,2-d]pirimidin-4(5H)-on; 7-((2,4-dihidroksibutilamino)metil)-3H-pirolo[3,2-d]pirimidin-4(5H)-on; 2-amino-7-((3,4-dihidroksi-2-(hidroksimetil)butilamino)metil)-3H-pirolo[3,2-d]pirimidin-4(5H)-on; 7-((3,4-dihidroksi-2-(hidroksimetil)butilamino)metil)-3H-pirolo[3,2-d]pirimidin-4(5H)-on; 2-amino-7-((3-hidroksi-2-(hidroksimetil)propilamino)metil)-3H-pirolo[3,2-d]pirimidin-4(5H)-on; 7-((3-hidroksi-2-(hidroksimetil)propilamino)metil)-3H-pirolo[3,2-d]pirimidin-4(5H)-on.
8. Optički izomer ili stereoizomer spoja prema bilo kojem od zahtjeva 1-7.
9. Spoj prema zahtjevu 1 naznačen time da je (2S,3R)-3-((4-hidroksi-5H-pirolo[3,2-d]pirimidin-7-il)-metilamino)butan-1,2,4-triol koji ima formulu: [image]
10. Farmaceutski pripravak naznačen time da sadrži farmaceutski učinkovitu količinu spoja prema bilo kojem od zahtjeva 1 do 9.
11. Spoj prema bilo kojem od zahtjeva 1 do 9 naznačen time da je za upotrebu kao lijek.
12. Spoj prema bilo kojem od zahtjeva 1 do 9 naznačen time da je za upotrebu kod liječenja bolesti ili stanja kod kojeg je poželjno inhibirati purinsku nukleozidnu fosforilazu ili nukleozidnu hidrolazu.
13. Upotreba spoja prema bilo kojem od zahtjeva 1 do 9 naznačena time da je za proizvodnju lijeka za liječenje bolesti ili stanja kod kojeg je poželjno inhibirati purinsku nukleozidnu fosforilazu ili nukleozidnu hidrolazu.
14. Spoj prema zahtjevu 12 ili upotreba prema zahtjevu 13 naznačen time da bolest ili stanje je rak, bakterijska infekcija, protozoa infekcija, ili bolest ili stanje posredovano T-stanicama.
15. Upotreba spoja prema bilo kojem od zahtjeva 12 do 14 naznačena time da purinska nukleozidna fosforilaza je humana purinska nukleozidna fosforilaza (Hs PNP) ili Plasmodium falciparum purinska nukleozidna fosforilaza (Pf PNP).
HR20110408T 2006-09-07 2011-05-31 Inhibitori nukleozidnih fosforilaza i hidrolaza acikličkog amina HRP20110408T1 (hr)

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US84286706P 2006-09-07 2006-09-07
PCT/NZ2007/000261 WO2008030119A1 (en) 2006-09-07 2007-09-07 Acyclic amine inhibitors of nucleoside phosphorylases and hydrolases

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US (1) US8853224B2 (hr)
EP (2) EP2395005A1 (hr)
JP (1) JP5388067B2 (hr)
KR (1) KR101433621B1 (hr)
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AT (1) ATE502038T1 (hr)
AU (1) AU2007293774C1 (hr)
CA (1) CA2662628C (hr)
CY (1) CY1111507T1 (hr)
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PT2057165E (pt) 2011-05-12
NZ575365A (en) 2012-02-24
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JP2010502696A (ja) 2010-01-28
EP2057165B1 (en) 2011-03-16
EP2057165A1 (en) 2009-05-13
CN101528749B (zh) 2013-07-31
JP5388067B2 (ja) 2014-01-15
DE602007013252D1 (de) 2011-04-28
WO2008030119A9 (en) 2009-09-24
ATE502038T1 (de) 2011-04-15
EP2057165A4 (en) 2009-09-02
AU2007293774C1 (en) 2014-12-18
SI2057165T1 (sl) 2011-07-29
KR101433621B1 (ko) 2014-08-27
US20110130412A1 (en) 2011-06-02
DK2057165T3 (da) 2011-06-27
US8853224B2 (en) 2014-10-07
RS51864B (en) 2012-02-29
HK1131612A1 (en) 2010-01-29
AU2007293774B2 (en) 2013-07-04
KR20090069281A (ko) 2009-06-30
CA2662628C (en) 2016-02-09
CY1111507T1 (el) 2015-08-05

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