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SI3002283T1 - Tiazolni derivati - Google Patents

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Publication number
SI3002283T1
SI3002283T1 SI200432405T SI200432405T SI3002283T1 SI 3002283 T1 SI3002283 T1 SI 3002283T1 SI 200432405 T SI200432405 T SI 200432405T SI 200432405 T SI200432405 T SI 200432405T SI 3002283 T1 SI3002283 T1 SI 3002283T1
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SI
Slovenia
Prior art keywords
substituted
unsubstituted
pharmaceutical composition
heterocyclic group
composition according
Prior art date
Application number
SI200432405T
Other languages
English (en)
Inventor
Takao Nakajima
Masamori Sugawara
Shin-Ichi Uchida
Tetsuji Ohno
Yuji Nomoto
Noriaki Uesaka
Yoshisuke Nakasato
Original Assignee
Kyowa Hakko Kirin Co., Ltd.
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Filing date
Publication date
Application filed by Kyowa Hakko Kirin Co., Ltd. filed Critical Kyowa Hakko Kirin Co., Ltd.
Publication of SI3002283T1 publication Critical patent/SI3002283T1/sl

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K31/435—Heterocyclic 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
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • A—HUMAN NECESSITIES
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    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non 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
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Claims (20)

  1. Tiazolni derivati Patentni zahtevki
    1. Farmacevtski sestavek, ki obsega kot aktivno sestavino tiazolni derivat, prikazan s formulo (IA), ali njegovo farmacevtsko sprejemljivo sol:
    pri čemer: R1A pomeni substituiran ali nesubstituiran furil (razen skupine, izbrane izmed 5-fosfonofuran-2-ila in 5-nitrofiiran-2-ila); R12 pomeni substituiran ali nesubstituiran Ci_10-alkil, substituiran ali nesubstituiran Ci.io-alkoksi, substituiran ali nesubstituiran cikloalkil, substituiran ali nesubstituiran aril, substituiran ali nesubstituiran aralkil, substituirano ali nesubstituirano aliciklično heterociklično skupino, substituirano ali nesubstituirano aromatsko heterociklično skupino, substituiran ali nesubstituiran alicikličen heterocikel-alkil ali substituiran ali nesubstituiran aromatski heterocikel-alkil; nje 0; R3a pomeni atom vodika in R2a pomeni -COR8 (pri čemer R8 pomeni substituiran ali nesubstituiran cikloalkil, substituiran ali nesubstituiran aril, substituirano ali nesubstituirano aliciklično heterociklično skupino ali substituirano ali nesubstituirano aromatsko heterociklično skupino). o
  2. 2. Farmacevtski sestavek po zahtevku 1, pri čemer je R substituiran ali nesubstituiran aril, substituirana ali nesubstituirana aliciklična heterociklična skupina ali substituirana ali nesubstituirana aromatska heterociklična skupina. o
  3. 3. Farmacevtski sestavek po zahtevku 1, pri čemer je R substituiran ali nesubstituiran aril.
  4. 4. Farmacevtski sestavek po zahtevku 1, pri čemer je R8 aril.
  5. 5. Farmacevtski sestavek po zahtevku 1, pri čemer je R8 substituirana ali nesubstituirana aromatska heterociklična skupina.
  6. 6. Farmacevtski sestavek po zahtevku 1, pri čemer je R8 aromatska heterociklična skupina.
  7. 7. Farmacevtski sestavek po zahtevku 1, pri čemer je R8 substituirana ali nesubstituirana aliciklična heterociklična skupina.
  8. 8. Farmacevtski sestavek po zahtevku 1, pri čemer je R8 aliciklična heterociklična skupina.
  9. 9. Farmacevtski sestavek po zahtevku 1, pri čemer je R8 substituirana ali nesubstituirana aliciklična heterociklična skupina, ki vsebuje vsaj en atom kisika.
  10. 10. Farmacevtski sestavek po zahtevku 1, pri čemer je R8 aliciklična heterociklična skupina, ki vsebuje vsaj en atom kisika. 1 ο
  11. 11. Farmacevtski sestavek po katerem koli od zahtevkov 1-10, pri čemer je R substituiran ali nesubstituiran aril, substituirana ali nesubstituirana aliciklična heterociklična skupina ali substituirana ali nesubstituirana aromatska heterociklična skupina.
  12. 12. Farmacevtski sestavek po katerem koli od zahtevkov 1-10, pri čemer je R12 substituiran ali nesubstituiran aril ali substituirana ali nesubstituirana aromatska heterociklična skupina.
  13. 13. Farmacevtski sestavek po katerem koli od zahtevkov 1-10, pri čemer je R12 substituiran ali nesubstituiran fenil ali substituirana ali nesubstituirana aromatska heterociklična skupina.
  14. 14. Farmacevtski sestavek po katerem koli od zahtevkov 1-10, pri čemer je R12 substituirana ali nesubstituirana aromatska heterociklična skupina.
  15. 15. Farmacevtski sestavek po katerem koli od zahtevkov 1-10, pri čemer je R12 substituiran ali nesubstituiran alicikličen heterocikel-metil ali substituiran ali nesubstituiran aromatski heterocikel-metil.
  16. 16. Farmacevtski sestavek po katerem koli od zahtevkov 1-15, pri čemer je R1A furil.
  17. 17. Farmacevtski sestavek po katerem koli od zahtevkov 1-16, ki obsega kot aktivno sestavino tiazolni derivat, prikazan z naslednjo formulo (99), (149), (170), (187), (191), (206), (228), (234), (249), (348), (431), (455), (456), (462), (468), (502), (504), (511), (515) ali (558), ali njegovo farmacevtsko sprejemljivo sol:
  18. 18. Farmacevtski sestavek po katerem koli od zahtevkov 1, 2, 7-14 in 16, ki obsega kot aktivno sestavino tiazolni derivat, prikazan z naslednjo formulo (504), ali njegovo farmacevtsko sprejemljivo sol:
  19. 19. Farmacevtski sestavek po katerem koli od zahtevkov 1-18 za uporabo pri zdravljenju in/ali preprečevanju bolezni centralnega živčnega sistema.
  20. 20. Farmacevtski sestavek po katerem koli od zahtevkov 1-18 za uporabo pri zdravljenju in/ali preprečevanju parkinsonove bolezni.
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US7718808B2 (en) 2010-05-18
CA2551611C (en) 2013-06-25
US20110105486A1 (en) 2011-05-05
BRPI0418082B1 (pt) 2019-09-24
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AU2004309279A1 (en) 2005-07-14
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PL1700856T3 (pl) 2016-05-31
WO2005063743A1 (ja) 2005-07-14
EA200601235A1 (ru) 2006-12-29
JPWO2005063743A1 (ja) 2007-07-19
US8420827B2 (en) 2013-04-16
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US20100256361A1 (en) 2010-10-07
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