CY1117810T1 - Πολυμορφα ενος ανταγωνιστη υποδοχεα mglur5 - Google Patents
Πολυμορφα ενος ανταγωνιστη υποδοχεα mglur5Info
- Publication number
- CY1117810T1 CY1117810T1 CY20161100705T CY161100705T CY1117810T1 CY 1117810 T1 CY1117810 T1 CY 1117810T1 CY 20161100705 T CY20161100705 T CY 20161100705T CY 161100705 T CY161100705 T CY 161100705T CY 1117810 T1 CY1117810 T1 CY 1117810T1
- Authority
- CY
- Cyprus
- Prior art keywords
- mglur5
- receptor
- multiplicator
- treatment
- present
- Prior art date
Links
- 102000005962 receptors Human genes 0.000 title abstract 2
- 108020003175 receptors Proteins 0.000 title abstract 2
- 101150087728 Grm5 gene Proteins 0.000 title 1
- 102100038357 Metabotropic glutamate receptor 5 Human genes 0.000 title 1
- 230000002860 competitive effect Effects 0.000 title 1
- 208000002193 Pain Diseases 0.000 abstract 2
- 230000001684 chronic effect Effects 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- RPRPXJNEEIIWAL-UHFFFAOYSA-N 2-chloro-4-[2-[1-(4-fluorophenyl)-2,5-dimethylimidazol-4-yl]ethynyl]pyridine sulfuric acid Chemical class OS(O)(=O)=O.Cc1nc(C#Cc2ccnc(Cl)c2)c(C)n1-c1ccc(F)cc1 RPRPXJNEEIIWAL-UHFFFAOYSA-N 0.000 abstract 1
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 206010003805 Autism Diseases 0.000 abstract 1
- 208000020706 Autistic disease Diseases 0.000 abstract 1
- 208000000094 Chronic Pain Diseases 0.000 abstract 1
- 208000001914 Fragile X syndrome Diseases 0.000 abstract 1
- 206010067125 Liver injury Diseases 0.000 abstract 1
- 102000012777 Metabotropic Glutamate 5 Receptor Human genes 0.000 abstract 1
- 108010065028 Metabotropic Glutamate 5 Receptor Proteins 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 206010046543 Urinary incontinence Diseases 0.000 abstract 1
- 230000001154 acute effect Effects 0.000 abstract 1
- 208000005298 acute pain Diseases 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000007812 deficiency Effects 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 231100000234 hepatic damage Toxicity 0.000 abstract 1
- 230000008818 liver damage Effects 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 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
- C07D401/02—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
- 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
- A61K31/435—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- 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
- A61P25/04—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
- A61P25/22—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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Child & Adolescent Psychology (AREA)
- Obesity (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Η παρούσα εφεύρεση σχετίζεται με μονοθειικά και ημιθειικά άλατα της 2-χλωρο-4-[1-(4-φθορο-φαινυλο)-2,5-διμεθυλο-1Η-ιμιδαζολ-4-υλοαιθυνυλο]-πυριδίνης, με κρυσταλλικές και άμορφες μορφές αυτών και με τη χρήση τους σε φαρμακευτικές τυποποιήσεις. Οι ενώσεις της παρούσας εφεύρεσης είναι δραστικές στον υποδοχέα mGluR5, για τη θεραπευτική αντιμετώπιση παθήσεων που σχετίζονται με αυτόν τον υποδοχέα, όπως οξειών και/ή χρόνιων νευρολογικών διαταραχών, συγκεκριμένα του άγχους, ή για τη θεραπευτική αντιμετώπιση του χρόνιου και οξέος πόνου, την προστασία έναντι ηπατικής βλάβης, της ανεπάρκειας που προκαλείται είτε από φάρμακο είτε από πάθηση, της ακράτειας ούρων, της παχυσαρκίας, του συνδρόμου εύθραυστου Χ ή του αυτισμού.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87639806P | 2006-12-21 | 2006-12-21 | |
| PCT/EP2007/063721 WO2008074697A1 (en) | 2006-12-21 | 2007-12-11 | Polymorphs of a mglur5 receptor antagonist |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CY1117810T1 true CY1117810T1 (el) | 2017-05-17 |
Family
ID=39186951
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CY20161100705T CY1117810T1 (el) | 2006-12-21 | 2016-07-19 | Πολυμορφα ενος ανταγωνιστη υποδοχεα mglur5 |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US8063076B2 (el) |
| EP (1) | EP2125779B1 (el) |
| JP (1) | JP5405311B2 (el) |
| KR (1) | KR101148580B1 (el) |
| CN (1) | CN101568531B (el) |
| AR (1) | AR064654A1 (el) |
| AU (1) | AU2007336369B2 (el) |
| CA (1) | CA2673444C (el) |
| CL (1) | CL2007003695A1 (el) |
| CO (1) | CO6210731A2 (el) |
| CY (1) | CY1117810T1 (el) |
| DK (1) | DK2125779T3 (el) |
| EC (1) | ECSP099431A (el) |
| ES (1) | ES2577391T3 (el) |
| HR (1) | HRP20160950T1 (el) |
| HU (1) | HUE029324T2 (el) |
| IL (1) | IL199181A (el) |
| MA (1) | MA31008B1 (el) |
| MX (1) | MX2009006694A (el) |
| MY (1) | MY148217A (el) |
| NO (1) | NO342451B1 (el) |
| NZ (1) | NZ577440A (el) |
| PE (1) | PE20081484A1 (el) |
| PL (1) | PL2125779T3 (el) |
| PT (1) | PT2125779T (el) |
| RS (1) | RS54853B1 (el) |
| RU (1) | RU2460728C2 (el) |
| SI (1) | SI2125779T1 (el) |
| TW (1) | TWI347320B (el) |
| UA (1) | UA96970C2 (el) |
| WO (1) | WO2008074697A1 (el) |
| ZA (1) | ZA200904289B (el) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2125779T (pt) | 2006-12-21 | 2016-07-19 | Hoffmann La Roche | Polimorfos de um antagonista de um recetor de mglur5 |
| US20120039999A1 (en) * | 2010-08-11 | 2012-02-16 | Ashish Chatterji | Pharmaceutical compositions of metabotropic glutamate 5 receptor (mglu5) antagonists |
| MX2013010698A (es) | 2011-03-18 | 2014-02-17 | Novartis Ag | Combinaciones de activadores del receptor de acetil-colina nicotinico alfa-7 y antagonistas del receptor de glutamato metabotropico 5 (mglur5) para usarse en la discinesia inducida por dopamina en la enfermedad de parkinson. |
| EP2837631A1 (en) * | 2013-08-14 | 2015-02-18 | Merck & Cie | New stable salt of 5,10-methylene-(6R)-tetrahydrofolic acid |
| GB201317022D0 (en) * | 2013-09-25 | 2013-11-06 | Addex Pharmaceuticals Sa | Polymorphs |
| CA2936377A1 (en) | 2014-01-10 | 2015-07-16 | Shanghai Birdie Biotech, Inc. | Compounds and compositions for treating egfr expressing tumors |
| CN115252792A (zh) | 2016-01-07 | 2022-11-01 | 博笛生物科技有限公司 | 用于治疗肿瘤的抗-egfr组合 |
| CN118515666A (zh) | 2017-04-27 | 2024-08-20 | 博笛生物科技有限公司 | 2-氨基-喹啉衍生物 |
| KR20230027145A (ko) | 2020-06-05 | 2023-02-27 | 노에마 파르마 아게 | 결절성 경화증 복합증의 치료 방법 |
| TW202220649A (zh) * | 2020-07-30 | 2022-06-01 | 瑞士商諾埃瑪製藥公司 | 三叉神經痛之治療方法 |
| CN120459099A (zh) * | 2025-06-17 | 2025-08-12 | 北京大学成都前沿交叉生物技术研究院 | mGlu5抑制剂在治疗或预防非酒精性脂肪肝病和/或肥胖、改善瘦素敏感性方面的应用 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3303199A (en) | 1963-07-15 | 1967-02-07 | Geigy Chem Corp | Certain imidazolone derivatives and process for making same |
| US3341548A (en) | 1964-04-29 | 1967-09-12 | Hoffmann La Roche | Nitroimidazoles and their preparation |
| DE2035905A1 (de) | 1970-07-20 | 1972-02-03 | Chemische Fabrik Stockhausen & Cie.,4150Krefeld | Imidazolverbindungen und deren Herstellungsverfahren |
| CA1174673A (en) | 1981-02-27 | 1984-09-18 | Walter Hunkeler | Imidazodiazepines |
| US4508560A (en) | 1981-11-11 | 1985-04-02 | Ciba Geigy Corporation | Certain pyridylacetylene compounds, compositions containing same and herbicidal methods of use |
| US4711962A (en) | 1984-10-18 | 1987-12-08 | Stauffer Chemical Company | Process for selective preparation of ratios of isomers formed on N-substitution of asymmetric imidazoles |
| AU644802B2 (en) | 1989-06-30 | 1993-12-23 | E.I. Du Pont De Nemours And Company | Substituted imidazoles |
| TW544448B (en) * | 1997-07-11 | 2003-08-01 | Novartis Ag | Pyridine derivatives |
| CN1154489C (zh) | 1997-08-14 | 2004-06-23 | 弗·哈夫曼-拉罗切有限公司 | 抗神经学疾病的杂环乙烯基醚 |
| AU780009B2 (en) | 1999-08-31 | 2005-02-24 | Merck Sharp & Dohme Corp. | Heterocyclic compounds and methods of use thereof |
| JP5154728B2 (ja) | 2000-07-24 | 2013-02-27 | クレニツキー・ファーマシューティカルズ，インコーポレイテッド | 神経栄養活性を有する置換５−アルキニルピリミジン |
| MXPA03004862A (es) | 2000-12-04 | 2005-02-14 | Hoffmann La Roche | Derivados de feniletenilo o feniletinilo como antagonistas del receptor de glutamato. |
| US6627646B2 (en) * | 2001-07-17 | 2003-09-30 | Sepracor Inc. | Norastemizole polymorphs |
| AU2002360621B2 (en) | 2001-12-19 | 2007-01-25 | Merck & Co., Inc. | heteroaryl substituted imidazole modulators of metabotropic glutamate receptor-5 |
| 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 |
| US7452909B2 (en) | 2003-09-04 | 2008-11-18 | Hoffman-La Roche Inc. | Imidazole derivatives |
| ATE397601T1 (de) * | 2004-06-01 | 2008-06-15 | Hoffmann La Roche | Pyridin-4-yl-ethynylimidazole und -pyrazole als antagonisten des mglu5-rezeptors |
| PT2125779T (pt) | 2006-12-21 | 2016-07-19 | Hoffmann La Roche | Polimorfos de um antagonista de um recetor de mglur5 |
-
2007
- 2007-12-11 PT PT78574084T patent/PT2125779T/pt unknown
- 2007-12-11 MY MYPI20092393A patent/MY148217A/en unknown
- 2007-12-11 MX MX2009006694A patent/MX2009006694A/es active IP Right Grant
- 2007-12-11 NZ NZ577440A patent/NZ577440A/en unknown
- 2007-12-11 HU HUE07857408A patent/HUE029324T2/en unknown
- 2007-12-11 DK DK07857408.4T patent/DK2125779T3/en active
- 2007-12-11 RU RU2009123135/04A patent/RU2460728C2/ru active
- 2007-12-11 CN CN2007800475969A patent/CN101568531B/zh active Active
- 2007-12-11 SI SI200731792A patent/SI2125779T1/sl unknown
- 2007-12-11 RS RS20160461A patent/RS54853B1/sr unknown
- 2007-12-11 UA UAA200907474A patent/UA96970C2/ru unknown
- 2007-12-11 AU AU2007336369A patent/AU2007336369B2/en active Active
- 2007-12-11 PL PL07857408.4T patent/PL2125779T3/pl unknown
- 2007-12-11 HR HRP20160950TT patent/HRP20160950T1/hr unknown
- 2007-12-11 KR KR1020097012810A patent/KR101148580B1/ko active Active
- 2007-12-11 WO PCT/EP2007/063721 patent/WO2008074697A1/en not_active Ceased
- 2007-12-11 CA CA2673444A patent/CA2673444C/en active Active
- 2007-12-11 ES ES07857408.4T patent/ES2577391T3/es active Active
- 2007-12-11 JP JP2009541986A patent/JP5405311B2/ja active Active
- 2007-12-11 EP EP07857408.4A patent/EP2125779B1/en active Active
- 2007-12-14 PE PE2007001802A patent/PE20081484A1/es not_active Application Discontinuation
- 2007-12-17 US US11/957,515 patent/US8063076B2/en active Active
- 2007-12-19 CL CL200703695A patent/CL2007003695A1/es unknown
- 2007-12-19 TW TW096148786A patent/TWI347320B/zh active
- 2007-12-21 AR ARP070105822A patent/AR064654A1/es not_active Application Discontinuation
-
2009
- 2009-06-04 IL IL199181A patent/IL199181A/en active IP Right Grant
- 2009-06-05 CO CO09058653A patent/CO6210731A2/es not_active Application Discontinuation
- 2009-06-15 EC EC2009009431A patent/ECSP099431A/es unknown
- 2009-06-17 MA MA32012A patent/MA31008B1/fr unknown
- 2009-06-18 ZA ZA200904289A patent/ZA200904289B/xx unknown
- 2009-06-19 NO NO20092357A patent/NO342451B1/no unknown
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2011
- 2011-10-14 US US13/273,266 patent/US8329912B2/en active Active
-
2016
- 2016-07-19 CY CY20161100705T patent/CY1117810T1/el unknown
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