DK3002283T3 - Thiazol-derivater. - Google Patents

Thiazol-derivater. Download PDF

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Publication number
DK3002283T3
DK3002283T3 DK15192381.0T DK15192381T DK3002283T3 DK 3002283 T3 DK3002283 T3 DK 3002283T3 DK 15192381 T DK15192381 T DK 15192381T DK 3002283 T3 DK3002283 T3 DK 3002283T3
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Prior art keywords
compound
substituted
mmol
unsubstituted
furyl
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DK15192381.0T
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English (en)
Inventor
Takao Nakajima
Masamori Sugawara
Shin-Ichi Uchida
Tetsuji Ohno
Yuji Nomoto
Noriaki Uesaka
Yoshisuke Nakasato
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Kyowa Hakko Kirin Co Ltd
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    • 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
    • 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
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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
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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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    • A61K31/435—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
    • A61K31/445—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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    • A61K31/47—Quinolines; Isoquinolines
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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Claims (20)

1. Pharmaceutisk sammensætning omfattende, som virksomt stof, et thiazol-derivat angivet ved formlen (IA) eller et pharmaceutisk acceptabelt salt deraf:
hvor: R1A angiver substitueret eller ikke-substitueret furyl (med undtagelse af en gruppe valgt fra 5-phosphonofuran-2-yl og 5-nitrofuran-2-yl); R12 angiver substitueret eller ikke-substitueret Ci-io-alkyl, substitueret eller ikke-sub-stitueret Ci io-alkoxy, substitueret eller ikke-substitueret cykloalkyl, substitueret eller ikke-substitueret aryl, substitueret eller ikke-substitueret aralkyl, en substitueret eller ikke-substitueret alicyklisk heterocyclisk gruppe, en substitueret eller ikke-substitueret aromatisk heterocyklisk gruppe, substitueret eller ikke-substitueret alicyklisk heterocyklicalkyl eller substitueret eller ikke-substitueret aromatisk heterocyklisk-alkyl; n er 0; R3A angiver et hydrogenatom; og R2A angiver -COR8 (hvor R8 angiver substitueret eller ikke-substitueret cykloalkyl, substitueret eller ikke-substitueret aryl, en substitueret eller ikke-substitueret alicyklisk heterocyklisk gruppe eller en substitueret eller ikke-substitueret aromatisk heterocyklisk gruppe).
2. Pharmaceutisk sammensætning ifølge krav 1, hvor R8 er substitueret eller ikke-substitueret aryl, en substitueret eller ikke-substitueret alicyklisk heterocyklisk gruppe eller en substitueret eller ikke-substitueret aromatisk heterocyklisk gruppe.
3. Pharmaceutisk sammensætning ifølge krav 1, hvor R8 er substitueret eller ikke-substitueret aryl.
4. Pharmaceutisk sammensætning ifølge krav 1, hvor R8 er aryl.
5. Pharmaceutisk sammensætning ifølge krav 1, hvor R8 er en substitueret eller ikke-substitueret aromatisk heterocyklisk gruppe.
6. Pharmaceutisk sammensætning ifølge krav 1, hvor R8 er en aromatisk heterocyklisk gruppe.
7. Pharmaceutisl sammensætning ifølge krav 1, hvor R8 er en substitueret eller ikke-substitueret alicyklisk heterocyklisk gruppe.
8. Pharmaceutisk sammensætning ifølge krav 1, hvor R8 er en alicyklisk heterocyklisk gruppe.
9. Pharmaceutisk sammensætning ifølge krav 1, hvor R8 er en substitueret eller ikke-substitueret alicyklisk heterocyklisk gruppe, der i det mindste indeholder ét oxygenatom.
10. Pharmaceutisk sammensætning ifølge krav 1, hvor R8 er en alicyklisk heterocyklisk gruppe, der i det mindste indeholder ét oxygenatom.
11. Pharmaceutisk sammensætning ifølge et hvilket som helst af krav 1 til 10, hvor R12 er substitueret eller ikke-substitueret aryl, en substitueret eller ikke-substitueret alicyk-lisk heterocyklisk gruppe eller en substitueret eller ikke-substitueret aromatisk heterocyklisk gruppe.
12. Pharmaceutisk sammensætning ifølge et hvilket som helst af krav 1 til 10, hvor R12 er substitueret eller ikke-substitueret aryl eller en substitueret eller ikke-substitueret aromatisk heterocyklisk gruppe.
13. Pharmaceutisk sammensætning ifølge et hvilket som helst af krav 1 til 10, hvor R12 er substitueret eller ikke-substitueret phenyl eller en substitueret eller ikke-substitueret aromatisk heterocyklisk gruppe.
14. Pharmaceutisk sammensætning ifølge et hvilket som helst af krav 1 til 10, hvor R12 er en substitueret eller ikke-substitueret aromatisk heterocyklisk gruppe.
15. Pharmaceutisk sammensætning ifølge et hvilket som helst af krav 1 til 10, hvor R12 er substitueret eller ikke-substitueret alicyklisk heterocyklisk-methyl eller substitueret eller ikke-substitueret aromatisk heterocyklisk-methyl.
16. Pharmaceutisk sammensætning ifølge et hvilket som helst af krav 1 til 15, hvor R1A er furyl.
17. Pharmaceutisk sammensætning ifølge et hvilket som helst af krav 1 til 16 omfattende, som virksomt stof, et thiazol-derivat angivet ved følgende formler (99), (149), (170), (187), (191), (206), (228), (234), (249), (348), (431), (455), (456), (462), (468), (502), (504), (511), (515) or (558) eller et pharmaceutisk acceptabelt salt deraf:
18. Pharmaceutisk sammensætning ifølge et hvilket som helst af krav 1, 2, 7 til 14 og 16 omfattende, som virksomt stof, et thiazol-derivat angivet ved den følgende formel (504) eller et pharmaceutisk acceptabelt salt deraf:
19. Pharmaceutisk sammensætning ifølge et hvilket som helst af krav 1 til 18 til anvendelse i behandling og/eller forebyggelse af en sygdom af centralnervesystemet.
20. Pharmaceutisk sammensætning ifølge et hvilket som helst af krav 1 til 18 til anvendelse i behandling og/eller forebyggelse af Parkinsons sygdom.
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EP3002283A1 (en) 2016-04-06
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KR20060126519A (ko) 2006-12-07
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