SI9111010B - 3,5-disubstituirani indolni derivati kot "5-HT1-podobni" receptorski agonisti - Google Patents
3,5-disubstituirani indolni derivati kot "5-HT1-podobni" receptorski agonisti Download PDFInfo
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- SI9111010B SI9111010B SI9111010A SI9111010A SI9111010B SI 9111010 B SI9111010 B SI 9111010B SI 9111010 A SI9111010 A SI 9111010A SI 9111010 A SI9111010 A SI 9111010A SI 9111010 B SI9111010 B SI 9111010B
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- compound
- physiologically
- solvate
- acceptable salt
- functional derivative
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- 239000000018 receptor agonist Substances 0.000 title claims 3
- 229940044601 receptor agonist Drugs 0.000 title claims 3
- -1 3,5-disubstituted indole Chemical class 0.000 title 1
- 229940054051 antipsychotic indole derivative Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 13
- 150000003839 salts Chemical class 0.000 claims abstract 10
- 239000012453 solvate Substances 0.000 claims abstract 10
- 239000003814 drug Substances 0.000 claims abstract 8
- 239000000203 mixture Substances 0.000 claims abstract 6
- ASNHGEVAWNWCRQ-UHFFFAOYSA-N 4-(hydroxymethyl)oxolane-2,3,4-triol Chemical compound OCC1(O)COC(O)C1O ASNHGEVAWNWCRQ-UHFFFAOYSA-N 0.000 claims abstract 5
- 238000000034 method Methods 0.000 claims abstract 5
- 238000011321 prophylaxis Methods 0.000 claims abstract 5
- 238000011282 treatment Methods 0.000 claims abstract 5
- 208000019695 Migraine disease Diseases 0.000 claims abstract 3
- 206010027599 migraine Diseases 0.000 claims abstract 3
- 238000002360 preparation method Methods 0.000 claims abstract 3
- 229940124597 therapeutic agent Drugs 0.000 claims abstract 2
- ULSDMUVEXKOYBU-UHFFFAOYSA-N 2-Oxazolidinone, 4-[[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl]- Chemical compound C1=C2C(CCN(C)C)=CNC2=CC=C1CC1COC(=O)N1 ULSDMUVEXKOYBU-UHFFFAOYSA-N 0.000 claims 3
- 239000013543 active substance Substances 0.000 claims 2
- 239000002775 capsule Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000003277 amino group Chemical group 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 238000011065 in-situ storage Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- ULSDMUVEXKOYBU-ZDUSSCGKSA-N zolmitriptan Chemical compound C1=C2C(CCN(C)C)=CNC2=CC=C1C[C@H]1COC(=O)N1 ULSDMUVEXKOYBU-ZDUSSCGKSA-N 0.000 claims 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 239000005864 Sulphur Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic 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
- C07D413/06—Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Cephalosporin Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Steroid Compounds (AREA)
Claims (12)
1 SI 9111010-0 Patentni zahtevki 1. Spojina N,N-dimetil-2-[5-(2-okso-l,3-oksazolidin-4-ilmetil)-lH-indol-3-il]-etilamin, v bodisi njegovi (S) ali (R) obliki ali kot njuna zmes v kakršnihkoli razmerjih, ali njegova fiziološko sprejemljiva sol, solvat ali njegov fiziološko funkcionalni derivat.
2. Spojina s formulo (I), kot je zahtevana v zahtevku 1, kije (S)-N,N-dimetil-2-[5-(2-okso-l,3-oksazolidin-4-ilmetil)-lH-indol-3-il]etilamin ali njegova fiziološko sprejemljiva sol, solvat ali njegov fiziološko funkcionalni derivat.
3. Spojina, kot je zahtevana v zahtevku 1 ali zahtevku 2, ali njena fiziološko sprejemljiva sol, solvat ali njen fiziološko funkcionalni derivat za uporabo kot terapevtsko sredstvo.
4. Spojina, kot je zahtevana v zahtevku 1 ali zahtevku 2, ali njena fiziološko sprejemljiva sol, solvat ali njen fiziološko funkcionalni derivat za uporabo v profilaksi ali zdravljenju kliničnega stanja, za katero je indiciran "5-HTr podoben" receptorski agonist.
5. Spojina, kot je zahtevana v zahtevku 1 ali zahtevku 2, ali njena fiziološko sprejemljiva sol, solvat ali njen fiziološko funkcionalni derivat za uporabo v profilaksi ali zdravljenju migrene.
6. Uporaba spojine, kot je zahtevana v zahtevku 1 ali zahtevku 2, ali njene fiziološko sprejemljive soli, solvata ali njenega fiziološko funkcionalnega derivata v izdelavi zdravila za profilakso ali zdravljenje kliničnega stanja, za katero je indiciran "5-HTj-podoben" receptorski agonist. 2 SI 9111010-0
7. Uporaba spojine, kot je zahtevana v zahtevku 1 ali zahtevku 2, ali njene fiziološko sprejemljive soli, solvata ali njenega fiziološko funkcionalnega derivata v izdelavi zdravila za profilakso ali zdravljenje migrene.
8. Zdravilo, ki obsega spojino, kot je zahtevana v zahtevku 1 ali zahtevku 2, ali njeno fiziološko sprejemljivo sol, sol vat ali njen fiziološko funkcionalni derivat, farmacevtsko sprejemljiv nosilec in, po izbiri, eno ali več drugih fiziološko aktivnih sredstev.
9. Zdravilo, kot je zahtevano v zahtevku 8, ki je v obliki tablete ali kapsule.
10. Postopek za pripravo spojine N,N-dimetil-2-[5-(2-okso-l,3-oksazolidin-4-ilmetil)-lH-indol-3-il]etilamina, v bodisi njegovi (S) ali (R) obliki ali kot njune zmesi v kakršnihkoli razmeijih, ki obsega reagiranje spojine s formulo (II)
nhnh2 (Π) kjer je n 1 in je W skupina O
$ in je kiralni center v svoji (S) ali (R) obliki ali je njuna zmes v kakršnihkoli razmerjih, s spojino s formulo (III) 3 SI 9111010-0 3 SI 9111010-0
m L ali njeno karbonilno-zaščiteno obliko, kjer je L ustrezna odhodna skupina ali zaščitena amino skupina, ki se lahko pretvori in situ v dimetil amino skupino, ali je -NR^2, kjer je vsak R1 in R2 metil.
11. Postopek priprave zdravila, ki obsega a) pripravo spojine N,N-dimetil-2-[5-(2-okso-l,3-oksazolidin-4-ilmetil)-lH-indol-3-il]etilamina, v bodisi njegovi (S) ali (R) obliki ali kot njune zmesi v kakršnihkoli razmerjih, ali njegove fiziološko sprejemljive soli, solvata ali njegovega fiziološko funkcionalnega derivata, s postopkom, kot je zahtevan v zahtevku 10; in b) mešanje produkta iz koraka a) s farmacevtsko sprejemljivim nosilcem in, po izbiri, enim ali več drugimi fiziološko aktivnimi sredstvi.
12. Postopek, kot je zahtevan v zahtevku 11, ki obsega dodatni korak c), v katerem se zmes iz koraka b) oblikuje v tableto ali kapsulo.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB909012672A GB9012672D0 (en) | 1990-06-07 | 1990-06-07 | Therapeutic heterocyclic compounds |
GB919102182A GB9102182D0 (en) | 1991-02-01 | 1991-02-01 | Therapeutic heterocyclic compounds |
YU101091A YU48855B (sh) | 1990-06-07 | 1991-06-06 | Heterociklična jedinjenja i njihovi derivati koji su modifikatori dejstva 5-hidroksi-triptamina i postupak njihovog dobijanja |
Publications (2)
Publication Number | Publication Date |
---|---|
SI9111010A SI9111010A (en) | 1997-12-31 |
SI9111010B true SI9111010B (sl) | 2005-02-28 |
Family
ID=26297174
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
SI9119001A SI21560B (sl) | 1990-06-07 | 1991-06-06 | 3,5-disubstituirani indolni derivati kot "5-HT1-podobni" receptorski agonisti |
SI9111010A SI9111010B (sl) | 1990-06-07 | 1991-06-06 | 3,5-disubstituirani indolni derivati kot "5-HT1-podobni" receptorski agonisti |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
SI9119001A SI21560B (sl) | 1990-06-07 | 1991-06-06 | 3,5-disubstituirani indolni derivati kot "5-HT1-podobni" receptorski agonisti |
Country Status (37)
Country | Link |
---|---|
US (3) | US5399574A (sl) |
EP (2) | EP0486666B1 (sl) |
JP (1) | JP2738461B2 (sl) |
KR (1) | KR100215627B1 (sl) |
AT (2) | ATE156823T1 (sl) |
AU (1) | AU646871B2 (sl) |
CA (2) | CA2064815C (sl) |
CZ (1) | CZ288351B6 (sl) |
DE (3) | DE19775091I2 (sl) |
DK (1) | DK0486666T3 (sl) |
EG (1) | EG19650A (sl) |
ES (1) | ES2104708T3 (sl) |
FI (3) | FI105686B (sl) |
GR (1) | GR3024828T3 (sl) |
HK (1) | HK1000534A1 (sl) |
HR (1) | HRP940524B1 (sl) |
HU (2) | HU219974B (sl) |
IE (1) | IE911931A1 (sl) |
IL (3) | IL114690A (sl) |
LT (1) | LT3264B (sl) |
LU (1) | LU90205I2 (sl) |
LV (1) | LV10274B (sl) |
MC (1) | MC2210A1 (sl) |
MX (1) | MX9203421A (sl) |
MY (1) | MY110226A (sl) |
NL (1) | NL980001I2 (sl) |
NO (2) | NO300634B1 (sl) |
NZ (1) | NZ238424A (sl) |
PL (1) | PL166214B1 (sl) |
PT (1) | PT97888B (sl) |
RU (1) | RU2160736C2 (sl) |
SA (1) | SA05260104B1 (sl) |
SI (2) | SI21560B (sl) |
SK (1) | SK281621B6 (sl) |
UA (1) | UA37178C2 (sl) |
WO (1) | WO1991018897A1 (sl) |
YU (1) | YU48855B (sl) |
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GB9208463D0 (en) * | 1992-04-16 | 1992-06-03 | Merck Sharp & Dohme | Therapeutic agents |
GB9209882D0 (en) * | 1992-05-07 | 1992-06-24 | Glaxo Lab Sa | Compositions |
GB9211277D0 (en) | 1992-05-28 | 1992-07-15 | Glaxo Group Inc | Pharmaceutical compositions |
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ES2056025B1 (es) * | 1992-10-08 | 1995-05-01 | Almirall Lab | Nuevos derivados de indol. |
TW251284B (sl) * | 1992-11-02 | 1995-07-11 | Pfizer | |
GB9226532D0 (en) * | 1992-12-21 | 1993-02-17 | Smithkline Beecham Plc | Compounds |
FR2701026B1 (fr) * | 1993-02-02 | 1995-03-31 | Adir | Nouveaux dérivés de l'indole, de l'indazole et du benzisoxazole, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent. |
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1996
- 1996-01-12 FI FI960155A patent/FI106262B/fi not_active IP Right Cessation
-
1997
- 1997-09-24 GR GR970402466T patent/GR3024828T3/el unknown
- 1997-11-07 HK HK97102131A patent/HK1000534A1/xx not_active IP Right Cessation
-
1998
- 1998-01-06 NL NL980001C patent/NL980001I2/nl unknown
- 1998-01-21 NO NO1998005C patent/NO1998005I1/no unknown
- 1998-01-28 LU LU90205C patent/LU90205I2/fr unknown
-
2000
- 2000-06-13 FI FI20001406A patent/FI20001406A/fi unknown
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OU02 | Decision according to article 73(2) ipa 1992, publication of decision on partial fulfilment of the invention and change of patent claims |
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