EA200602154A1 - Пиридин-4-илэтинилимидазолы и -пиразолы как антагонисты рецептора mglu5 - Google Patents
Пиридин-4-илэтинилимидазолы и -пиразолы как антагонисты рецептора mglu5Info
- Publication number
- EA200602154A1 EA200602154A1 EA200602154A EA200602154A EA200602154A1 EA 200602154 A1 EA200602154 A1 EA 200602154A1 EA 200602154 A EA200602154 A EA 200602154A EA 200602154 A EA200602154 A EA 200602154A EA 200602154 A1 EA200602154 A1 EA 200602154A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- ileetinilimidazoles
- pyrazoles
- pyridin
- antagonists
- mglu5 receptor
- Prior art date
Links
- 101001032845 Homo sapiens Metabotropic glutamate receptor 5 Proteins 0.000 title 1
- 102100038357 Metabotropic glutamate receptor 5 Human genes 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000000034 method Methods 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
- 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
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- 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
- A61P25/02—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
- A61P25/14—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
- A61P25/22—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
-
- 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)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Gastroenterology & Hepatology (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
В заявке описаны производные диазола общей формулы (I)в которой А, Е, R, Rи Rявляются такими, как определено в формуле изобретения и описании, их применение для приготовления лекарственных средств, предназначенных для лечения заболеваний, и способы их получения.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/EP2004/005881 WO2004108701A1 (en) | 2003-06-05 | 2004-06-01 | Imidazole derivatives as glutmate receptor antagonists |
EP04021216 | 2004-09-07 | ||
PCT/EP2005/005559 WO2005118568A1 (en) | 2004-06-01 | 2005-05-23 | Pyridin-4-yl-ethynyl-imidazoles and pyrazoles as mglu5 receptor antagonists |
Publications (2)
Publication Number | Publication Date |
---|---|
EA200602154A1 true EA200602154A1 (ru) | 2007-06-29 |
EA011722B1 EA011722B1 (ru) | 2009-04-28 |
Family
ID=35758209
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200602154A EA011722B1 (ru) | 2004-06-01 | 2005-05-23 | Пиридин-4-илэтинилимидазолы и -пиразолы как антагонисты рецептора mglu5 |
Country Status (19)
Country | Link |
---|---|
US (2) | US20060030559A1 (ru) |
JP (1) | JP4690395B2 (ru) |
KR (2) | KR101057032B1 (ru) |
AR (1) | AR054072A1 (ru) |
BR (1) | BRPI0511678A (ru) |
CR (1) | CR8742A (ru) |
CY (1) | CY1108232T1 (ru) |
DK (1) | DK1756086T3 (ru) |
EA (1) | EA011722B1 (ru) |
EC (1) | ECSP067039A (ru) |
ES (1) | ES2307182T3 (ru) |
HK (1) | HK1105972A1 (ru) |
HR (1) | HRP20080363T3 (ru) |
IL (1) | IL179524A (ru) |
MA (1) | MA28602B1 (ru) |
NZ (1) | NZ551253A (ru) |
PT (1) | PT1756086E (ru) |
SI (1) | SI1756086T1 (ru) |
TW (1) | TWI297683B (ru) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8329703B2 (en) * | 2005-02-15 | 2012-12-11 | Xtl Biopharmaceuticals Ltd. | Pyrazole compounds |
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 |
WO2017117708A1 (en) * | 2016-01-05 | 2017-07-13 | Hua Medicine (Shanghai) Ltd. | Pyrazole derivatives |
CN108883104A (zh) | 2016-03-30 | 2018-11-23 | 森泰克希斯公司 | 用于在治疗成熟脑损伤中使用的mGluR5的负性变构调节剂 |
AU2021285273A1 (en) | 2020-06-05 | 2023-01-19 | Noema Pharma Ag | Methods of treatment of tuberous sclerosis complex |
EP4188370A1 (en) * | 2020-07-30 | 2023-06-07 | Noema Pharma AG | Methods of treatment of trigeminal neuralgia |
Family Cites Families (29)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3033199A (en) * | 1959-10-13 | 1962-05-08 | Jacobs Clifford Roy | Closure for protective device |
US3045022A (en) | 1960-04-07 | 1962-07-17 | Reilly Tar & Chem Corp | Process of preparing ethynylpyridines |
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 |
EP0079312A3 (de) | 1981-11-11 | 1984-04-25 | Ciba-Geigy Ag | Heterocyclische Acetylenverbindungen |
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 |
DE69025473T2 (de) | 1989-06-30 | 1996-10-17 | Du Pont | Substituierte imidazole und ihre verwendung als hemmmstoff fur angiotensin ii |
TW544448B (en) | 1997-07-11 | 2003-08-01 | Novartis Ag | Pyridine derivatives |
TR200000405T2 (tr) | 1997-08-14 | 2000-08-21 | F.Hoffmann-La Roche Ag | Nörolojik rahatsızlıklara karşı heterosiklik vinileterler. |
WO2001016121A1 (en) * | 1999-08-31 | 2001-03-08 | Merck & Co., Inc. | Heterocyclic compounds and methods of use thereof |
WO2001029012A2 (en) | 1999-10-15 | 2001-04-26 | F. Hoffmann-La Roche Ag | Benzodiazepine derivatives as metabotropic glutamate receptor antagonists |
IL136553A0 (en) | 2000-06-05 | 2001-06-14 | Compugen Ltd | SPLICE VARIANT OF mGluR |
EP1303495B1 (en) | 2000-07-24 | 2010-05-26 | Krenitsky Pharmaceuticals, Inc. | Substituted 5-alkynyl pyrimidines having neurotrophic activity |
ATE288898T1 (de) * | 2000-12-04 | 2005-02-15 | Hoffmann La Roche | Phenylethenyl- oder phenylethinylderivate als glutamatrezeptorantagonisten |
EP1238586A1 (en) | 2001-03-09 | 2002-09-11 | Basf Aktiengesellschaft | Herbicidal 2-alkynyl-pyri(mi)dines |
US6596731B2 (en) | 2001-03-27 | 2003-07-22 | Hoffmann-La Roche Inc. | Substituted imidazo[1,2-A] pyridine derivatives |
US7253190B2 (en) | 2001-10-04 | 2007-08-07 | Merck & Co., Inc. | Heteroaryl substituted tetrazole modulators of metabotrophic glutamate receptor-5 |
US20030187026A1 (en) | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
JP2005516950A (ja) | 2001-12-19 | 2005-06-09 | メルク エンド カムパニー インコーポレーテッド | 代謝型グルタミン酸受容体−5のヘテロアリール置換イミダゾールモジュレータ |
CA2503245A1 (en) | 2002-10-24 | 2004-05-06 | Merck & Co., Inc. | Alkyne derivatives as tracers for metabotropic glutamate receptor binding |
ITMI20030151A1 (it) | 2003-01-30 | 2004-07-31 | Recordati Ind Chimica E Farma Ceutica S P A | Uso di antagonisti selettivi del recettore mglu5 per il trattamento di disfunzioni neuromuscolari del tratto urinario inferiore. |
TWI292318B (en) | 2003-03-10 | 2008-01-11 | Hoffmann La Roche | Imidazol-4-yl-ethynyl-pyridine derivatives |
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 |
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 |
DE102004032567A1 (de) | 2004-07-05 | 2006-03-02 | Grünenthal GmbH | Substituierte 1-Propiolyl-piperazine |
-
2005
- 2005-05-23 BR BRPI0511678-3A patent/BRPI0511678A/pt not_active Application Discontinuation
- 2005-05-23 EA EA200602154A patent/EA011722B1/ru not_active IP Right Cessation
- 2005-05-23 KR KR1020087022221A patent/KR101057032B1/ko not_active IP Right Cessation
- 2005-05-23 JP JP2007513776A patent/JP4690395B2/ja not_active Expired - Fee Related
- 2005-05-23 DK DK05744719T patent/DK1756086T3/da active
- 2005-05-23 SI SI200530280T patent/SI1756086T1/sl unknown
- 2005-05-23 NZ NZ551253A patent/NZ551253A/en not_active IP Right Cessation
- 2005-05-23 ES ES05744719T patent/ES2307182T3/es active Active
- 2005-05-23 PT PT05744719T patent/PT1756086E/pt unknown
- 2005-05-23 KR KR1020067025236A patent/KR100907108B1/ko not_active IP Right Cessation
- 2005-05-27 AR ARP050102179A patent/AR054072A1/es unknown
- 2005-05-27 TW TW094117351A patent/TWI297683B/zh not_active IP Right Cessation
- 2005-05-31 US US11/141,547 patent/US20060030559A1/en not_active Abandoned
-
2006
- 2006-11-09 CR CR8742A patent/CR8742A/es unknown
- 2006-11-22 MA MA29482A patent/MA28602B1/fr unknown
- 2006-11-23 IL IL179524A patent/IL179524A/en not_active IP Right Cessation
- 2006-11-28 EC EC2006007039A patent/ECSP067039A/es unknown
-
2007
- 2007-10-22 HK HK07111356.8A patent/HK1105972A1/xx not_active IP Right Cessation
-
2008
- 2008-07-21 HR HR20080363T patent/HRP20080363T3/xx unknown
- 2008-07-31 CY CY20081100804T patent/CY1108232T1/el unknown
-
2009
- 2009-11-05 US US12/613,089 patent/US8293916B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
HRP20080363T3 (en) | 2008-09-30 |
KR101057032B1 (ko) | 2011-08-16 |
BRPI0511678A (pt) | 2008-01-08 |
US8293916B2 (en) | 2012-10-23 |
AR054072A1 (es) | 2007-06-06 |
SI1756086T1 (sl) | 2008-08-31 |
IL179524A (en) | 2012-04-30 |
ECSP067039A (es) | 2006-12-29 |
DK1756086T3 (da) | 2008-08-04 |
CY1108232T1 (el) | 2014-02-12 |
PT1756086E (pt) | 2008-08-08 |
ES2307182T3 (es) | 2008-11-16 |
KR100907108B1 (ko) | 2009-07-09 |
KR20080089523A (ko) | 2008-10-06 |
US20060030559A1 (en) | 2006-02-09 |
TWI297683B (en) | 2008-06-11 |
US20100048569A1 (en) | 2010-02-25 |
JP4690395B2 (ja) | 2011-06-01 |
NZ551253A (en) | 2010-07-30 |
EA011722B1 (ru) | 2009-04-28 |
CR8742A (es) | 2007-08-28 |
KR20070021231A (ko) | 2007-02-22 |
IL179524A0 (en) | 2007-05-15 |
HK1105972A1 (en) | 2008-02-29 |
MA28602B1 (fr) | 2007-05-02 |
TW200609222A (en) | 2006-03-16 |
JP2008500979A (ja) | 2008-01-17 |
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Legal Events
Date | Code | Title | Description |
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MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ KG MD TJ TM |
|
MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): BY KZ RU |