SI9620111B - Imidazole derivatives having affinity for alpha2 receptors activity - Google Patents
Imidazole derivatives having affinity for alpha2 receptors activity Download PDFInfo
- Publication number
- SI9620111B SI9620111B SI9620111A SI9620111A SI9620111B SI 9620111 B SI9620111 B SI 9620111B SI 9620111 A SI9620111 A SI 9620111A SI 9620111 A SI9620111 A SI 9620111A SI 9620111 B SI9620111 B SI 9620111B
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- Prior art keywords
- hydrogen
- alkyl
- derivative according
- derivative
- hydroxy
- Prior art date
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- 150000002460 imidazoles Chemical class 0.000 title claims abstract 3
- 229940079865 intestinal antiinfectives imidazole derivative Drugs 0.000 title abstract 2
- 102000005962 receptors Human genes 0.000 title 1
- 108020003175 receptors Proteins 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 22
- 239000001257 hydrogen Substances 0.000 claims abstract 22
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 13
- 208000002193 Pain Diseases 0.000 claims abstract 6
- 150000002431 hydrogen Chemical group 0.000 claims abstract 5
- -1 C3-C7-cycloalkyl Chemical group 0.000 claims abstract 3
- 208000000094 Chronic Pain Diseases 0.000 claims abstract 3
- 206010012335 Dependence Diseases 0.000 claims abstract 3
- 206010012735 Diarrhoea Diseases 0.000 claims abstract 3
- 208000010412 Glaucoma Diseases 0.000 claims abstract 3
- 206010020772 Hypertension Diseases 0.000 claims abstract 3
- 208000019695 Migraine disease Diseases 0.000 claims abstract 3
- 208000005298 acute pain Diseases 0.000 claims abstract 3
- 230000001684 chronic effect Effects 0.000 claims abstract 3
- 208000010877 cognitive disease Diseases 0.000 claims abstract 3
- 208000028867 ischemia Diseases 0.000 claims abstract 3
- 206010027599 migraine Diseases 0.000 claims abstract 3
- 201000009240 nasopharyngitis Diseases 0.000 claims abstract 3
- 239000000126 substance Substances 0.000 claims abstract 3
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims abstract 2
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims abstract 2
- 208000023178 Musculoskeletal disease Diseases 0.000 claims abstract 2
- 208000012902 Nervous system disease Diseases 0.000 claims abstract 2
- 208000025966 Neurological disease Diseases 0.000 claims abstract 2
- 229940124534 adjunct to anesthesia Drugs 0.000 claims abstract 2
- 229910052799 carbon Inorganic materials 0.000 claims abstract 2
- 150000001721 carbon Chemical group 0.000 claims abstract 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims abstract 2
- 150000001875 compounds Chemical class 0.000 claims abstract 2
- 150000002148 esters Chemical class 0.000 claims abstract 2
- 229910052736 halogen Inorganic materials 0.000 claims abstract 2
- 150000002367 halogens Chemical class 0.000 claims abstract 2
- 230000000926 neurological effect Effects 0.000 claims abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims abstract 2
- 208000020016 psychiatric disease Diseases 0.000 claims abstract 2
- 150000003839 salts Chemical class 0.000 claims abstract 2
- 150000003573 thiols Chemical class 0.000 claims abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- VREFGVBLTWBCJP-UHFFFAOYSA-N alprazolam Chemical compound C12=CC(Cl)=CC=C2N2C(C)=NN=C2CN=C1C1=CC=CC=C1 VREFGVBLTWBCJP-UHFFFAOYSA-N 0.000 claims 1
- 230000003444 anaesthetic effect Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000013589 supplement Substances 0.000 claims 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 208000019901 Anxiety disease Diseases 0.000 abstract 2
- 230000036506 anxiety Effects 0.000 abstract 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 2
- 101100495911 Arabidopsis thaliana CHR10 gene Proteins 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
-
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- 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
- A61K31/41—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
- A61K31/415—1,2-Diazoles
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Ophthalmology & Optometry (AREA)
- Physical Education & Sports Medicine (AREA)
- Otolaryngology (AREA)
- Hospice & Palliative Care (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Urology & Nephrology (AREA)
- Anesthesiology (AREA)
- Communicable Diseases (AREA)
- Vascular Medicine (AREA)
- Virology (AREA)
- Oncology (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Epoxy Resins (AREA)
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Description
IMIDAZOLOVI DERIVATI, KI IMAJO AFINITETO ZA AKTIVNOST ALFA2 RECEPTORJEV
Claims (18)
- PATENTNI ZAHTEVKI1. Derivat imidazola, ki je spojina s formulo I n je 0 ali 1R1 je vodik ali C^-C^alkilR2 je vodik, ali R2 in Rg skupaj tvorita dvojno vezRg je vodik ali C-j-C4-alkil, ali R2 in Rg skupaj tvorita dvojno vezR4 je vodik, C-j-C4-alkil, hidroksi ali C^C^alkoksiRg je vodik ali C-j-C^-alkil, ali R4 in Rg skupaj z atomom ogljika, na katerega sta vezana, tvorita karbonilno skupino.Rg, R7 in Rg so vsi enaki ali različni in so neodvisno vodik, C^-C4-alkil ali C2-C4-alkenil, Cg-Cy-cikloalkil, hidroksi, C^-C4-alkoksi, C^-C^-hidroksialkil, tiol, 4-alkiltio, 4-alkiltiol, halogen, trifluorometil, nitro ali po izbiri substituirani amino X je -CHR9-(CHRw)mm je 0 ali 1 in Rg in R^q sta oba enaka ali različna in sta neodvisno vodik ali C^-C4-alkil; ali farmacevtsko sprejemljiv ester ali sol le-teh.
- 2. Derivat v skladu z zahtevkom 1, označen s tem, da je n = m=0.
- 3. Derivat v skladu z zahtevkom 1 ali 2, označen s tem, da so Rg, Ry in Rg vsi vodik.
- 4. Derivat v skladu z zahtevkom 1 ali 2, označen s tem, da je Rg C^-C^alkil na poziciji 4 ali 6 indanovega obroča, R7 in Re pa sta vodik.
- 5. Derivat v skladu z zahtevkom 1 ali 2, označen s tem, da je R6 C,-C4-alkoksi na poziciji 7 indanovega obroča, R7 in R„ pa sta vodik.
- 6. Derivat v skladu z zahtevkom 1, označen s tem, da je n=1 in m=0.
- 7. Derivat v skladu z zahtevkom 6, označen s tem, da je R, metil ali etil.
- 8. Derivat v skladu z zahtevkom 6 ali 7, označen s tem, da so R6, R7 in R8 vsi vodik.
- 9. Derivat v skladu z zahtevkom 6 ali 7, označen s tem, da je R6 hidroksi na poziciji 4 aii 6 indanovega obroča, R7 in Re pa sta vodik.
- 10. Derivat v skladu z zahtevkom 6 ali 7, označen s tem, da je R6 hidroksi na poziciji 5 indanovega obroča in R7 je hidroksi ali CpC^alkil ali C,-C4-hidroksialkil na poziciji 6 indanovega obroča, Rg pa je vodik.
- 11. Derivat v skladu z zahtevkom 1, označen s tem, da je n=m=1.
- 12. Derivat v skladu z zahtevkom 11, označen s tem, da so Rs do R„ vsi vodik.
- 13. Derivat v skladu z zahtevkom 11, označen s tem, da je R6 hidroksi skupina na poziciji 71,2,3,4-tetrahidronaftil obroča, R7 in R8 pa sta vodik.
- 14. Farmacevtsko sprejemljiv sestavek, ki vsebuje derivat, kot je definiran v kateremkoli od zahtevkov 1 do 13 in farmacevtsko sprejemljiv nosilec.
- 15. Derivat, kot je definiran v kateremkoli od zahtevkov 1 do 13, za uporabo pri postopku zdravljenja telesa ljudi ali živali.
- 16. Derivat, kot je definiran v kateremkoli od zahtevkov 1 do 13, za uporabo pri zdravljenju hipertenzije, glavkoma, kronične in akutne bolečine, migrene, driske, običajnega prehlada, ishemije, zasvojenosti s kemičnimi substancami, strahu, posebno predoperativnega strahu in različnih nevrolo{kih, mišično-kostnih, psihičnih in kognitivnih motenj ali kot dodatek ob anesteziji.
- 17. Uporaba derivata, kot je definiran v kateremkoli od zahtevkov 1 do 13, za izdelavo zdravila za uporabo pri zdravljenju hipertenzije, glavkoma, kronične in akutne bolečine, migrene, driske, običajnega prehlada, ishemije, zasvojenosti s kemičnimi substancami, strahu, posebno predoperativnega strahu in različnih nevroloških, mišično-kostnih, psihičnih in kognitivnih motenj.
- 18. Uporaba derivata, kot je definiran v kateremkoli od zahtevkov 1 do 13, pri izdelavi zdravila za uporabo kot dodatek ob anesteziji.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9520150.5A GB9520150D0 (en) | 1995-10-03 | 1995-10-03 | New imidazole derivatives |
| PCT/FI1996/000518 WO1997012874A1 (en) | 1995-10-03 | 1996-10-02 | Imidazole derivatives having affinity for alpha2 receptors activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| SI9620111A SI9620111A (sl) | 1998-10-31 |
| SI9620111B true SI9620111B (en) | 2001-12-31 |
Family
ID=10781676
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SI9620111A SI9620111B (en) | 1995-10-03 | 1996-10-02 | Imidazole derivatives having affinity for alpha2 receptors activity |
Country Status (30)
| Country | Link |
|---|---|
| US (2) | US6313311B1 (sl) |
| EP (1) | EP0888309B1 (sl) |
| JP (1) | JP4129891B2 (sl) |
| KR (1) | KR19990064013A (sl) |
| CN (1) | CN1068592C (sl) |
| AT (1) | ATE234819T1 (sl) |
| AU (1) | AU708002B2 (sl) |
| BG (1) | BG63916B1 (sl) |
| CA (1) | CA2231535C (sl) |
| CZ (1) | CZ291576B6 (sl) |
| DE (1) | DE69626862T2 (sl) |
| DK (1) | DK0888309T3 (sl) |
| EE (1) | EE04436B1 (sl) |
| ES (1) | ES2195013T3 (sl) |
| GB (1) | GB9520150D0 (sl) |
| HK (1) | HK1014951A1 (sl) |
| HU (1) | HU224197B1 (sl) |
| IL (1) | IL123721A (sl) |
| LT (1) | LT4460B (sl) |
| LV (1) | LV12108B (sl) |
| NO (1) | NO311024B1 (sl) |
| NZ (1) | NZ319169A (sl) |
| PL (1) | PL189110B1 (sl) |
| PT (1) | PT888309E (sl) |
| RO (1) | RO120409B1 (sl) |
| RU (1) | RU2188194C2 (sl) |
| SI (1) | SI9620111B (sl) |
| SK (1) | SK283542B6 (sl) |
| UA (1) | UA49847C2 (sl) |
| WO (1) | WO1997012874A1 (sl) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA981080B (en) | 1997-02-11 | 1998-08-12 | Warner Lambert Co | Bicyclic inhibitors of protein farnesyl transferase |
| AU2002254265B2 (en) * | 1997-12-04 | 2008-05-15 | Allergan, Inc. | Imidiazole derivatives and their use as agonists selective at alpha 2B or 2B/2C adrenergic receptors |
| US6841684B2 (en) * | 1997-12-04 | 2005-01-11 | Allergan, Inc. | Imidiazoles having reduced side effects |
| RU2235092C2 (ru) * | 1997-12-04 | 2004-08-27 | Оллерган Инк. | Замещенные производные имидазола, способ введения активного соединения и способ лечения на основе этих соединений |
| US6329369B1 (en) | 1997-12-04 | 2001-12-11 | Allergan Sales, Inc. | Methods of treating pain and other conditions |
| JP4647785B2 (ja) * | 1998-09-28 | 2011-03-09 | オリオン コーポレーション | 脊椎内、髄腔内または硬膜外投与用医薬の製造における３−（１ｈ−イミダゾール−４−イルメチル）−インダン−５−オールの用途 |
| TWI283669B (en) * | 1999-06-10 | 2007-07-11 | Allergan Inc | Compounds and method of treatment having agonist-like activity selective at alpha 2B or 2B/2C adrenergic receptors |
| EP1196168A2 (en) * | 1999-06-25 | 2002-04-17 | Orion Corporation | Method of admistering an imidazole derivative to obtain analgesia |
| CA2388979C (en) | 1999-10-29 | 2010-09-14 | Orion Corporation | Treatment or prevention of hypotension and shock with use of an imidazole derivative |
| FI20000073A0 (fi) * | 2000-01-14 | 2000-01-14 | Orion Yhtymae Oy | Uusia imidatsolijohdannaisia |
| US6388090B2 (en) | 2000-01-14 | 2002-05-14 | Orion Corporation | Imidazole derivatives |
| CZ20023674A3 (cs) * | 2000-05-08 | 2003-09-17 | Orion Corporation | Nové polycyklické indanylimidazolové sloučeniny s alfa2 adrenergní aktivitou |
| TW200930291A (en) * | 2002-04-29 | 2009-07-16 | Bayer Cropscience Ag | Pesticidal heterocycles |
| FR2839719B1 (fr) * | 2002-05-16 | 2004-08-06 | Pf Medicament | Nouveaux composes imidazoliques, leur procede de preparation et leur utilisation a titre de medicaments |
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| US3636002A (en) * | 1969-12-15 | 1972-01-18 | Janssen Pharmaceutica Nv | 1-(2-halobenzyloxy-1-indanyl)-imidazoles |
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| US6388090B2 (en) * | 2000-01-14 | 2002-05-14 | Orion Corporation | Imidazole derivatives |
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