HRP20120434T2 - Spojevi 4-oksadiazolil-piperidina i njihova uporaba - Google Patents

Spojevi 4-oksadiazolil-piperidina i njihova uporaba Download PDF

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Publication number
HRP20120434T2
HRP20120434T2 HRP20120434TT HRP20120434T HRP20120434T2 HR P20120434 T2 HRP20120434 T2 HR P20120434T2 HR P20120434T T HRP20120434T T HR P20120434TT HR P20120434 T HRP20120434 T HR P20120434T HR P20120434 T2 HRP20120434 T2 HR P20120434T2
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alkyl
compound according
pharmaceutically acceptable
image
substituted
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HRP20120434TT
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English (en)
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Laykea Tafesse
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Purdue Pharma Lp
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Publication of HRP20120434T1 publication Critical patent/HRP20120434T1/hr
Publication of HRP20120434T2 publication Critical patent/HRP20120434T2/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • 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
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • 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)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Claims (29)

1. Spoj formule (I): [image] ili njegova farmaceutski prihvatljiva sol, naznačen time da: Ar1 je fenil nesupstituiran ili supstituiran sa jednom ili više R2 skupina; Ar2 je fenil nesupstituiran ili supstituiran sa jednom, dvije ili tri R2 skupine; Ar4 je fenil nesupstituiran ili supstituiran sa jednom, dvije ili tri R2 skupine; G je -H, -C(O)(CH2)nCO2R4, -C(O)(CH2)nR5, -(C1-C5 alkilen)C(O)OR4, ili -(C1-C5 alkilen)R5; R1 = -H, -C(O)NH2, -C(O)NHOH, -CO2R4, -CHO, -CN, -(C1-C4 alkil), -C(O)NH(C1-C4 alkil), -C(O)N(C1-C4 alkil)2, -CF3, -CHF2, -CH2F, [image] R2 i R3 su svaki nezavisno -halogen, -C1-C3 alkil, -O(C1-C3 alkil), -NH(C1-C3 alkil), -N(C1-C3 alkil)2, -CF3 ili -OCF3; R4 = -H, -C1-C10 alkil, -CH2O(C1-C4 alkil), -CH2N(C1-C4 alkil)2, ili -CH2NH(C1-C4 alkil); R5 = -NH2, -NHSO2R4, -C(O)NH2, -C(O)NHOH, -SO2NH2, -C(O)NH(C1-C4 alkil), -C(O)N(C1-C4 alkil)2, -SO2NH(C1-C4 alkil), -SO2N(C1-C4 alkil)2, -H, -OH, -CN, -C3-C8 cikloalkil, fenil, naftil, antril, fenantril, ili -(5- do 7-člani) heteroaril, svaki -C3-C8 cikloalkil, fenil, naftil, antril, fenantril, ili -(5- do 7-člani) heteroaril je nesupstituiran ili supstituiran sa jednom ili više R2 skupina; m = cijeli broj u rasponu od 0 do 4; n = cijeli broj u rasponu od 1 do 4; p = 0 ili 1; i q = cijeli broj u rasponu od 1 do 6.
2. Spoj formule (II): [image] ili njegova farmaceutski prihvatljiva sol, naznačen time da: Ar3 je fenil nesupstituiran ili supstituiran sa jednom, dvije ili tri R2 skupine; Ar4 fenil nesupstituiran ili supstituiran sa jednom, dvije ili tri R2 skupine; G = -H, -C(O)(CH2)nC(O)OR4, -C(O)(CH2)nR5, -(C1-C5 alkilen)C(O)OR4, ili -(C1-C5 alkilen)R5 ; R1 = H, -C(O)NH2, -C(O)NHOH, -CO2R4, -CHO, -CN, -(C1-C4 alkil), -C(O)NH(C1-C4 alkil), -C(O)N(C1-C4 alkil)2, -CF3, -CHF2, -CH2F, [image] R2 i R3 su svaki nezavisno halogen, -C1-C3 alkil, -O(C1-C3 alkil), -NH(C1-C3 alkil), -N(C1-C3 alkil)2, -CF3, ili -OCF3; R4 = -H, -C1-C10 alkil, -CH2O(C1-C4 alkil), -CH2N(C1-C4 alkil)2, ili -CH2NH(C1-C4 alkil); R5 = -NH2, -NHSO2R4, -C(O)NH2, -C(O)NHOH, - SO2NH2, -C(O)NH(C1-C4 alkil), -C(O)N(C1-C4 alkil)2, -SO2NH(C1-C4 alkil), -SO2N(C1-C4 alkil)2, -H, -OH, -CN, -C3-C8 cikloalkil, fenil, naftil, antril, fenantril, ili -(5- do 7-člani) heteroaril, svaki -C3-C8 cikloalkil, fenil, naftil, antril, fenantril, ili -(5- do 7-člani) heteroaril, je nesupstituiran ili supstituiran sa jednom, dvije ili tri R2 skupine; m = cijeli broj u rasponu od 0 do 4; n = cijeli broj u rasponu od 1 do 4; p = 0 ili 1; i q = cijeli broj u rasponu od 1 do 6.  
3. Spoj prema zahtjevu 1 ili 2, naznačen time da m = 1 i G = H.
4. Spoj prema zahtjevu 1 ili 2 naznačen time da R1 je -C(O)NH2, -C(O)NH(C1-C4 alkil), ili -C(O)N(C1-C4 alkil) (C1-C4 alkil).
5. Spoj prema zahtjevu 1 ili 2, naznačen time da R1 je -CN.
6. Spoj prema zahtjevu 1 ili 2, naznačen time da m = 1, p = 0 i q = 3.
7. Spoj prema zahtjevu 1 ili 2, naznačen time da G = -(CH2)2NHSO2H.
8. Spoj prema zahtjevu 1 ili 2, naznačen time da G = -CH2C(O)NH2, -CH2C(O)NH(C1-C4 alkil) ili -CH2C(O)N(C1-C4 alkil) (C1-C4 alkil), poželjno -CH2C(O)NH2.
9. Spoj prema zahtjevu 1 ili 2, naznačen time da G = -CH2C(O)OCH2CH3.
10. Spoj prema zahtjevu 8 ili 9, naznačen time da R1 = -C(O)N(CH3)2.
11. Spoj prema zahtjevu 8 ili 9, naznačen time da R1 je [image] .
12. Spoj prema zahtjevu 1 ili 2, naznačen time da G = -(CH2)2C(O)OCH2CH3.
13. Spoj prema zahtjevu 1 ili 2, naznačen time da G = -(CH2)4C(O)OCH2CH3.
14. Spoj prema zahtjevu 1 ili 2, naznačen time da p = 1.
15. Pripravak naznačen time da sadrži spoj prema zahtjevu 1 ili 2 i farmaceutski prihvatljiv nosač ili pomoćnu tvar.
16. Pripravak prema zahtjevu 15, naznačen time da nadalje sadrži barem jedan spoj koji je odabran iz skupine koja sadrži opioidni analgetik, ne-opioidni analgetik, te sredstvo protiv povraćanja.
17. Postupak za dobivanje pripravka, naznačen time da postupak sadrži miješanje spoja prema zahtjevu 1 ili 2 i farmaceutski prihvatljivog nosača ili pomoćne tvari.
18. Kit naznačen time da sadrži spremnik koji sadrži pripravak prema zahtjevu 15, te poželjno dodatno sadrži sredstvo protiv proljeva.
19. Uporaba spoja prema zahtjevu 1 ili 2 ili njegove farmaceutski prihvatljive soli naznačena time da je za dobivanje lijeka za liječenje ili sprečavanje boli ili proljeva.
20. Uporaba prema zahtjevu 19 naznačena time da nadalje sadrži davanje učinkovite količine barem jednog spoja koji je odabran iz skupine koja sadrži opioidni analgetik, ne-opioidni analgetik, te sredstvo protiv povraćanja.
21. Spoj prema zahtjevu 1, naznačen time da je opisan sa slijedećom formulom [image] ili njegova farmaceutska sol.
22. Spoj prema zahtjevu 1, naznačen time da je opisan sa slijedećom formulom [image] ili njegova farmaceutska sol.
23. Spoj prema zahtjevu 1, naznačen time da je opisan sa slijedećom formulom [image] ili njegova farmaceutska sol.
24. Spoj prema zahtjevu 1, naznačen time da je opisan sa slijedećom formulom [image] ili njegova farmaceutska sol.
25. Uporaba spoja prema zahtjevu 1 ili 2 ili njegove farmaceutski prihvatljive soli naznačena time da se koristi kao lijek.
26. Uporaba spoja prema zahtjevu 1 ili 2 ili njegove farmaceutski prihvatljive soli naznačena time da je za dobivanje lijeka za stimuliranje funkcije opioidnog-receptora u stanici koje se sastoji od dovođenja u kontakt stanice koja može eksprimirati opioidni receptor sa učinkovitom količinom spoja prema zahtjevu 1 ili 2 ili njegove farmaceutski prihvatljive soli kod liječenja boli ili proljeva.
27. Uporaba prema zahtjevu 26, naznačena time da je receptor odabran iz skupine koja sadrži κ-opioidni receptor, µ-opioidni receptor, δ-opioidni receptor ili ORL-1 receptor za liječenje boli ili proljeva.
28. Spoj prema zahtjevu 1 ili 2 ili njegova farmaceutski prihvatljiva sol naznačen time da je za liječenje boli ili proljeva
29. Spoj prema zahtjevu 1 ili 2 ili njegova farmaceutski prihvatljiva sol naznačen time da je za stimuliranje funkcije opioidnog-receptora u stanici, kod liječenja boli ili proljeva.
HRP20120434TT 2005-11-21 2012-05-23 Spojevi 4-oksadiazolil-piperidina i njihova uporaba HRP20120434T2 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US73910705P 2005-11-21 2005-11-21
PCT/EP2006/011150 WO2007057229A1 (en) 2005-11-21 2006-11-21 4-oxadiazolyl-piperidine compounds and use thereof

Publications (2)

Publication Number Publication Date
HRP20120434T1 HRP20120434T1 (hr) 2012-06-30
HRP20120434T2 true HRP20120434T2 (hr) 2012-11-30

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Application Number Title Priority Date Filing Date
HRP20120434TT HRP20120434T2 (hr) 2005-11-21 2012-05-23 Spojevi 4-oksadiazolil-piperidina i njihova uporaba

Country Status (23)

Country Link
US (1) US20080319020A1 (hr)
EP (3) EP2298764A1 (hr)
JP (1) JP4991746B2 (hr)
KR (1) KR20080080138A (hr)
CN (1) CN101312964A (hr)
AT (1) ATE547414T1 (hr)
AU (1) AU2006314730B2 (hr)
BR (1) BRPI0619679A2 (hr)
CA (1) CA2628750C (hr)
CY (1) CY1112773T1 (hr)
DK (1) DK1951718T3 (hr)
EA (1) EA013510B1 (hr)
ES (1) ES2382712T3 (hr)
HR (1) HRP20120434T2 (hr)
NO (1) NO20082752L (hr)
NZ (1) NZ568430A (hr)
PL (1) PL1951718T3 (hr)
PT (1) PT1951718E (hr)
RS (1) RS52258B (hr)
SI (1) SI1951718T1 (hr)
UA (1) UA91250C2 (hr)
WO (1) WO2007057229A1 (hr)
ZA (1) ZA200803101B (hr)

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EP1951718A1 (en) 2008-08-06
CA2628750C (en) 2013-02-12
EP2298764A1 (en) 2011-03-23
NO20082752L (no) 2008-08-06
WO2007057229A1 (en) 2007-05-24
AU2006314730A1 (en) 2007-05-24
AU2006314730B2 (en) 2011-02-03
JP2009516664A (ja) 2009-04-23
PT1951718E (pt) 2012-05-21
CY1112773T1 (el) 2016-02-10
CA2628750A1 (en) 2007-05-24
EP1951718B1 (en) 2012-02-29
BRPI0619679A2 (pt) 2011-10-11
ATE547414T1 (de) 2012-03-15
JP4991746B2 (ja) 2012-08-01
PL1951718T3 (pl) 2012-08-31
ES2382712T3 (es) 2012-06-12
KR20080080138A (ko) 2008-09-02
DK1951718T3 (da) 2012-05-14
NZ568430A (en) 2011-02-25
RS52258B (en) 2012-10-31
ZA200803101B (en) 2009-03-25
EA200801392A1 (ru) 2008-10-30
EP2298765A1 (en) 2011-03-23
EP1951718B9 (en) 2012-08-15
HRP20120434T1 (hr) 2012-06-30
SI1951718T1 (sl) 2012-06-29
ES2382712T9 (es) 2012-10-30
CN101312964A (zh) 2008-11-26
UA91250C2 (en) 2010-07-12
US20080319020A1 (en) 2008-12-25
EA013510B1 (ru) 2010-06-30

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