HRP20070529T3 - Derivati imidazola kao antagonisti receptora glutamata - Google Patents
Derivati imidazola kao antagonisti receptora glutamataInfo
- Publication number
- HRP20070529T3 HRP20070529T3 HR20070529T HRP20070529T HRP20070529T3 HR P20070529 T3 HRP20070529 T3 HR P20070529T3 HR 20070529 T HR20070529 T HR 20070529T HR P20070529 T HRP20070529 T HR P20070529T HR P20070529 T3 HRP20070529 T3 HR P20070529T3
- Authority
- HR
- Croatia
- Prior art keywords
- alkyl
- cycloalkyl
- optionally substituted
- hydrogen
- denotes
- Prior art date
Links
- 150000002460 imidazoles Chemical class 0.000 title 1
- 229940079865 intestinal antiinfectives imidazole derivative Drugs 0.000 title 1
- 239000002464 receptor antagonist Substances 0.000 title 1
- 229940044551 receptor antagonist Drugs 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000005988 1,1-dioxo-thiomorpholinyl group Chemical group 0.000 abstract 1
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000005322 morpholin-1-yl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 229910052717 sulfur Chemical group 0.000 abstract 1
- 239000011593 sulfur Chemical group 0.000 abstract 1
Classifications
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Addiction (AREA)
- Hospice & Palliative Care (AREA)
- Anesthesiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Spoj opće formule,naznačen time, daR1 označava halogen ili cijano; R2 označava C1-C6-alkil; R3 označava fenil ili heteroarilni prsten sa 5 ili 6 članova koji sadrži jedan ili više heteroatoma izabranih od dušika, kisika ili sumpora, koji su opcijskisupstituirani sa jednim, dva ili tri supstituentaizabranih iz skupine koja se sastoji od halogen, C1-C6-alkil, C3-C6-cikloalkil, C1-C6-alkil-halogen, cijano, C1-C6-alkoksi, NR'R" ili sa 1-morfolinilom, ili sa1-pirolidinilom, opcijski supstituiranogsa (CH2)0,1OR, ili sa piperidinilom, opcijski supstituiranog sa (CH2)0,1OR, ili sa 1,1-diokso-tiomorfolinilom ili sa piperazinilom, opcijski supstituiranog sa C1-C6-alkilom ili (CH2)0,1-C3-C6-cikloalkilom; R je vodik, C1-C6-alkil ili (CH2)0,1-C3-C6-cikloalkil; R', R" su neovisno jedan od drugog vodik, C1-C6-alkil, (CH2)0,1-C3-C6-cikloalkil ili (CH2)nOR; n je 1 ili 2; R4 je vodik, C(O)H, CH2R5 gdje je R5 vodik, OH, C1-C6-alkil ili C3-C12-cikloalkil, jednako kao i njegove farmaceutski prihvatljive soli. Patent sadrži još 11 patentnih zahtjeva.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP03012200 | 2003-06-05 | ||
| PCT/EP2004/005881 WO2004108701A1 (en) | 2003-06-05 | 2004-06-01 | Imidazole derivatives as glutmate receptor antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20070529T3 true HRP20070529T3 (hr) | 2008-05-31 |
Family
ID=33483899
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20070529T HRP20070529T3 (hr) | 2003-06-05 | 2007-11-20 | Derivati imidazola kao antagonisti receptora glutamata |
Country Status (39)
| Country | Link |
|---|---|
| US (3) | US7332510B2 (hr) |
| EP (1) | EP1636206B1 (hr) |
| JP (1) | JP4401384B2 (hr) |
| KR (1) | KR100778948B1 (hr) |
| CN (1) | CN100408572C (hr) |
| AR (1) | AR044478A1 (hr) |
| AT (1) | ATE377008T1 (hr) |
| AU (1) | AU2004245208B2 (hr) |
| BR (1) | BRPI0411095B8 (hr) |
| CA (1) | CA2527315C (hr) |
| CL (1) | CL2004001347A1 (hr) |
| CR (1) | CR8094A (hr) |
| CY (1) | CY1107856T1 (hr) |
| DE (1) | DE602004009796T2 (hr) |
| DK (1) | DK1636206T3 (hr) |
| EA (1) | EA010577B1 (hr) |
| EC (1) | ECSP056202A (hr) |
| ES (1) | ES2294504T3 (hr) |
| GT (1) | GT200400117A (hr) |
| HK (1) | HK1093070A1 (hr) |
| HN (1) | HN2004000208A (hr) |
| HR (1) | HRP20070529T3 (hr) |
| IL (1) | IL171930A (hr) |
| MA (1) | MA27881A1 (hr) |
| MX (1) | MXPA05013149A (hr) |
| MY (2) | MY137272A (hr) |
| NO (1) | NO332143B1 (hr) |
| NZ (1) | NZ543637A (hr) |
| PA (1) | PA8604101A1 (hr) |
| PE (1) | PE20050162A1 (hr) |
| PL (1) | PL1636206T3 (hr) |
| PT (1) | PT1636206E (hr) |
| RS (1) | RS53183B (hr) |
| SI (1) | SI1636206T1 (hr) |
| TN (2) | TNSN05309A1 (hr) |
| TW (1) | TWI338007B (hr) |
| UA (1) | UA80888C2 (hr) |
| WO (1) | WO2004108701A1 (hr) |
| ZA (2) | ZA200509807B (hr) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7531529B2 (en) | 2003-06-05 | 2009-05-12 | Roche Palo Alto Llc | Imidazole derivatives |
| UA80888C2 (en) * | 2003-06-05 | 2007-11-12 | Hoffmann La Roche | Imidazole derivatives as glutmate receptor antagonists |
| US7452909B2 (en) | 2003-09-04 | 2008-11-18 | Hoffman-La Roche Inc. | Imidazole derivatives |
| BRPI0511678A (pt) | 2004-06-01 | 2008-01-08 | Hoffmann La Roche | piridin-4-il-etinil-imidazóis e pirazóis como antagonistas de receptor de mglu5 |
| GB0514296D0 (en) * | 2005-07-12 | 2005-08-17 | Novartis Ag | Organic compounds |
| DE102006011574A1 (de) * | 2006-03-10 | 2007-10-31 | Grünenthal GmbH | Substituierte Imidazo[2,1-b]thiazol-Verbindungen und ihre Verwendung zur Herstellung von Arzneimitteln |
| MY148217A (en) * | 2006-12-21 | 2013-03-29 | Hoffmann La Roche | Polymorphs of a mglur5 receptor antagonist |
| US8334287B2 (en) * | 2009-07-17 | 2012-12-18 | Hoffmann-La Roche Inc. | Imidazoles |
| US20120039999A1 (en) * | 2010-08-11 | 2012-02-16 | Ashish Chatterji | Pharmaceutical compositions of metabotropic glutamate 5 receptor (mglu5) antagonists |
| US20120040008A1 (en) * | 2010-08-11 | 2012-02-16 | Ashish Chatterji | Pharmaceutical compositions of metabotropic glutamate 5 receptor (mglu5) antagonists |
| US20140228398A1 (en) | 2011-03-18 | 2014-08-14 | Novartis Ag | COMBINATIONS OF ALPHA 7 NICOTINIC ACETYLCHOLINE RECEPTOR ACTIVATORS AND mGluR5 ANTAGONISTS FOR USE IN DOPAMINE INDUCED DYSKINESIA IN PARKINSON'S DISEASE |
| AU2013333988B2 (en) * | 2012-10-18 | 2017-03-09 | F. Hoffmann-La Roche Ag | Ethynyl derivatives as modulators of mGluR5 receptor activity |
| PE20150733A1 (es) * | 2012-10-18 | 2015-05-17 | Hoffmann La Roche | Derivados de etinilo como moduladores de la actividad del receptor mglur5 |
| EP3436009B1 (en) * | 2016-03-30 | 2024-03-06 | Sinntaxis AB | Negative allosteric modulators of mglur5 for use in the treatment of mature brain damages. |
| CN116056701A (zh) * | 2020-06-05 | 2023-05-02 | 诺埃玛制药公司 | 治疗结节硬化复合症的方法 |
| MX2023001288A (es) * | 2020-07-30 | 2023-04-28 | Noema Pharma Ag | Metodos de tratamiento de la neuralgia del trigemino. |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0079312A3 (de) | 1981-11-11 | 1984-04-25 | Ciba-Geigy Ag | Heterocyclische Acetylenverbindungen |
| TW544448B (en) * | 1997-07-11 | 2003-08-01 | Novartis Ag | Pyridine derivatives |
| AU780009B2 (en) * | 1999-08-31 | 2005-02-24 | Merck Sharp & Dohme Corp. | Heterocyclic compounds and methods of use thereof |
| WO2002008205A1 (en) * | 2000-07-24 | 2002-01-31 | Krenitsky Pharmaceuticals, Inc. | Substituted 5-alkynyl pyrimidines having neurotrophic activity |
| KR100515549B1 (ko) * | 2000-12-04 | 2005-09-20 | 에프. 호프만-라 로슈 아게 | 글루타메이트 수용체 길항제로서의 페닐에테닐 또는페닐에티닐 유도체 |
| WO2003053922A2 (en) * | 2001-12-19 | 2003-07-03 | Merck & Co., Inc. | Heteroaryl substituted imidazole modulators of metabotropic glutamate receptor-5 |
| WO2004038374A2 (en) * | 2002-10-24 | 2004-05-06 | Merck & Co., Inc. | Alkyne derivatives as tracers for metabotropic glutamate receptor binding |
| TWI292318B (en) * | 2003-03-10 | 2008-01-11 | Hoffmann La Roche | Imidazol-4-yl-ethynyl-pyridine derivatives |
| UA80888C2 (en) * | 2003-06-05 | 2007-11-12 | Hoffmann La Roche | Imidazole derivatives as glutmate receptor antagonists |
| US7091222B2 (en) * | 2003-07-03 | 2006-08-15 | Hoffmann-La Roche Inc. | Imidazole derivatives |
-
2004
- 2004-01-06 UA UAA200512695A patent/UA80888C2/uk unknown
- 2004-06-01 AT AT04739484T patent/ATE377008T1/de active
- 2004-06-01 DK DK04739484T patent/DK1636206T3/da active
- 2004-06-01 PT PT04739484T patent/PT1636206E/pt unknown
- 2004-06-01 DE DE602004009796T patent/DE602004009796T2/de not_active Expired - Lifetime
- 2004-06-01 CA CA2527315A patent/CA2527315C/en not_active Expired - Lifetime
- 2004-06-01 BR BRPI0411095A patent/BRPI0411095B8/pt active IP Right Grant
- 2004-06-01 SI SI200430525T patent/SI1636206T1/sl unknown
- 2004-06-01 WO PCT/EP2004/005881 patent/WO2004108701A1/en active IP Right Grant
- 2004-06-01 AU AU2004245208A patent/AU2004245208B2/en not_active Expired
- 2004-06-01 JP JP2006508238A patent/JP4401384B2/ja not_active Expired - Lifetime
- 2004-06-01 EP EP04739484A patent/EP1636206B1/en not_active Expired - Lifetime
- 2004-06-01 RS YU20050892A patent/RS53183B/en unknown
- 2004-06-01 KR KR1020057023137A patent/KR100778948B1/ko active IP Right Grant
- 2004-06-01 MX MXPA05013149A patent/MXPA05013149A/es active IP Right Grant
- 2004-06-01 NZ NZ543637A patent/NZ543637A/en unknown
- 2004-06-01 PL PL04739484T patent/PL1636206T3/pl unknown
- 2004-06-01 EA EA200501887A patent/EA010577B1/ru not_active IP Right Cessation
- 2004-06-01 ES ES04739484T patent/ES2294504T3/es not_active Expired - Lifetime
- 2004-06-01 CN CNB2004800156669A patent/CN100408572C/zh not_active Expired - Lifetime
- 2004-06-02 CL CL200401347A patent/CL2004001347A1/es unknown
- 2004-06-02 PE PE2004000558A patent/PE20050162A1/es active IP Right Grant
- 2004-06-02 TW TW093115811A patent/TWI338007B/zh active
- 2004-06-02 US US10/858,969 patent/US7332510B2/en active Active
- 2004-06-02 PA PA20048604101A patent/PA8604101A1/es unknown
- 2004-06-03 GT GT200400117A patent/GT200400117A/es unknown
- 2004-06-03 AR ARP040101908A patent/AR044478A1/es active IP Right Grant
- 2004-06-03 MY MYPI20042150A patent/MY137272A/en unknown
- 2004-06-03 HN HN2004000208A patent/HN2004000208A/es unknown
-
2005
- 2005-05-27 MY MYPI20052424A patent/MY143353A/en unknown
- 2005-11-13 IL IL171930A patent/IL171930A/en active IP Right Grant
- 2005-11-14 CR CR8094A patent/CR8094A/es unknown
- 2005-11-18 NO NO20055465A patent/NO332143B1/no unknown
- 2005-12-01 TN TNP2005000309A patent/TNSN05309A1/fr unknown
- 2005-12-02 EC EC2005006202A patent/ECSP056202A/es unknown
- 2005-12-02 ZA ZA200509807A patent/ZA200509807B/en unknown
- 2005-12-09 MA MA28648A patent/MA27881A1/fr unknown
-
2006
- 2006-11-21 ZA ZA200609681A patent/ZA200609681B/xx unknown
- 2006-11-27 TN TNP2006000391A patent/TNSN06391A1/fr unknown
- 2006-12-18 HK HK06113874A patent/HK1093070A1/xx unknown
-
2007
- 2007-10-31 US US11/930,258 patent/US8481548B2/en active Active
- 2007-11-20 HR HR20070529T patent/HRP20070529T3/hr unknown
- 2007-12-13 US US11/955,421 patent/US7973165B2/en active Active
-
2008
- 2008-01-11 CY CY20081100047T patent/CY1107856T1/el unknown
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