HUP0402191A2 - Humán metabotrop glutamát receptor antagonista aktivitással rendelkező acetilénszármazékok, eljárás előállításukra, az ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents
Humán metabotrop glutamát receptor antagonista aktivitással rendelkező acetilénszármazékok, eljárás előállításukra, az ezeket tartalmazó gyógyszerkészítmények és alkalmazásukInfo
- Publication number
- HUP0402191A2 HUP0402191A2 HU0402191A HUP0402191A HUP0402191A2 HU P0402191 A2 HUP0402191 A2 HU P0402191A2 HU 0402191 A HU0402191 A HU 0402191A HU P0402191 A HUP0402191 A HU P0402191A HU P0402191 A2 HUP0402191 A2 HU P0402191A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- hydrogen atom
- alkyl
- matabotropic
- human
- Prior art date
Links
- 150000000475 acetylene derivatives Chemical class 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 102000018899 Glutamate Receptors Human genes 0.000 title 1
- 108010027915 Glutamate Receptors Proteins 0.000 title 1
- 230000003042 antagnostic effect Effects 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 7
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000001037 epileptic effect Effects 0.000 abstract 1
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 abstract 1
- 239000012458 free base Substances 0.000 abstract 1
- 230000000848 glutamatergic effect Effects 0.000 abstract 1
- 208000028867 ischemia Diseases 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- -1 phenyl- Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000008054 signal transmission Effects 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/16—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/24—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
-
- 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
- A61P25/32—Alcohol-abuse
-
- 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
- A61P25/34—Tobacco-abuse
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
- C07C233/23—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/04—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
- C07D215/08—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/20—Oxygen atoms
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Indole Compounds (AREA)
- Quinoline Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
A találmány szabad bázis vagy savaddíciós só formájában lévő (I)általános képletű acetilénszármazékokra - amelyek képletében m 0 vagyl; n 0 vagy l; és A hidroxicsoport, X hidrogénatom, és Y hidrogénatom;vagy A X-szel vagy Y-nal egy egyes kötést képez; R0 előnyösenhidrogénatom, alkil-, alkoxi-, trifluor-metil-COOR1, vagy -COR2csoport, és R -COR3, -COOR3, -CONR4R5 vagy -SO2R6 csoport, ahol R3alkil-, cikloalkilcsoport vagy adott esetben szubsztituált fenil-, 2-piridil- csoport, R' hidrogénatom vagy alkilcsoport, és R"hidrogénatom vagy alkilcsoport, vagy R' és R" együtt egy -CH2-(CH2)p-csoportot képez, ahol p 0, 1 vagy 2, amely esetben n és p egyikének azértéke 0-tól eltérő; azzal a megkötéssel, hogy R0 jelentésehidrogénatomtól, trifluor-metil- vagy metoxicsoporttól eltérő, ha mértéke 0, n értéke 0, A jelentése hidroxicsoport, X és Y mindegyikénekjelentése hidrogénatom, R jelentése etoxi-karbonil-csoport, valamintR' és R" együtt egy -(CH2)2- képletű csoportot képez -, a vegyületekelőállítási eljárásaira, a vegyületeket tartalmazógyógyszerkészítményekre és a glutamáterg szignál transzmisszióvalkapcsolatos rendellenességek, például epilepszia ichémiák kezelésérehasználható gyógyszerkészítmények előállítására történő alkalmazásáravonatkozik. Ó
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB0128996.6A GB0128996D0 (en) | 2001-12-04 | 2001-12-04 | Organic compounds |
PCT/EP2002/013670 WO2003047581A1 (en) | 2001-12-04 | 2002-12-03 | Acetylene derivatives having mglur 5 antagonistic activity |
Publications (3)
Publication Number | Publication Date |
---|---|
HUP0402191A2 true HUP0402191A2 (hu) | 2005-02-28 |
HUP0402191A3 HUP0402191A3 (en) | 2010-03-29 |
HU229429B1 HU229429B1 (en) | 2013-12-30 |
Family
ID=9926969
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0402191A HU229429B1 (en) | 2001-12-04 | 2002-12-03 | Acetylene derivatives having mglur 5 antagonistic activity |
Country Status (32)
Country | Link |
---|---|
US (4) | US7348353B2 (hu) |
EP (1) | EP1453512B8 (hu) |
JP (2) | JP4176020B2 (hu) |
KR (2) | KR100959204B1 (hu) |
CN (2) | CN101366714B (hu) |
AR (2) | AR037682A1 (hu) |
AT (1) | ATE327755T1 (hu) |
AU (1) | AU2002358585B2 (hu) |
BR (1) | BR0214666A (hu) |
CA (1) | CA2466560C (hu) |
CO (1) | CO5590929A2 (hu) |
CY (1) | CY1105460T1 (hu) |
DE (1) | DE60211944T2 (hu) |
DK (1) | DK1453512T3 (hu) |
EC (1) | ECSP045139A (hu) |
EG (1) | EG24936A (hu) |
ES (1) | ES2263842T3 (hu) |
GB (1) | GB0128996D0 (hu) |
HK (1) | HK1071510A1 (hu) |
HU (1) | HU229429B1 (hu) |
IL (1) | IL161990A0 (hu) |
MX (1) | MXPA04005456A (hu) |
MY (1) | MY137774A (hu) |
NO (1) | NO327005B1 (hu) |
NZ (1) | NZ533266A (hu) |
PE (1) | PE20030640A1 (hu) |
PL (1) | PL212996B1 (hu) |
PT (1) | PT1453512E (hu) |
RU (1) | RU2341515C2 (hu) |
TW (1) | TWI328578B (hu) |
WO (1) | WO2003047581A1 (hu) |
ZA (1) | ZA200403713B (hu) |
Families Citing this family (44)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB0128996D0 (en) * | 2001-12-04 | 2002-01-23 | Novartis Ag | Organic compounds |
US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
GB0325956D0 (en) * | 2003-11-06 | 2003-12-10 | Addex Pharmaceuticals Sa | Novel compounds |
US20080125403A1 (en) | 2004-04-02 | 2008-05-29 | Merck & Co., Inc. | Method of Treating Men with Metabolic and Anthropometric Disorders |
GB0503646D0 (en) * | 2005-02-22 | 2005-03-30 | Novartis Ag | Organic compounds |
GB0508319D0 (en) * | 2005-04-25 | 2005-06-01 | Novartis Ag | Organic compounds |
GB0508314D0 (en) * | 2005-04-25 | 2005-06-01 | Novartis Ag | Organic compounds |
GB0508318D0 (en) * | 2005-04-25 | 2005-06-01 | Novartis Ag | Organic compounds |
GB0514296D0 (en) * | 2005-07-12 | 2005-08-17 | Novartis Ag | Organic compounds |
WO2008031550A2 (en) * | 2006-09-11 | 2008-03-20 | Novartis Ag | Nicotinic acid derivatives as modulators of metabotropic glutanate receptors |
ES2393885T7 (es) | 2007-06-04 | 2014-01-30 | Synergy Pharmaceuticals Inc. | Agonistas de la guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos |
US8969514B2 (en) | 2007-06-04 | 2015-03-03 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases |
SG185293A1 (en) * | 2007-10-12 | 2012-11-29 | Novartis Ag | Organic compounds |
AU2012254934B2 (en) * | 2007-10-12 | 2013-10-17 | Novartis Ag | Metabotropic glutamate receptor modulators for the treatment of Parkinson's disease |
ES2522968T3 (es) | 2008-06-04 | 2014-11-19 | Synergy Pharmaceuticals Inc. | Agonistas de guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos |
AU2009265760B2 (en) * | 2008-06-30 | 2013-07-18 | Novartis Ag | Combinations comprising mGluR modulators for the treatment of parkinson's disease |
US8084487B2 (en) * | 2008-08-12 | 2011-12-27 | Novartis Ag | Processes for the preparation of 4-oxo-octahydro-indole-1-carbocyclic acid methyl ester and derivatives thereof |
US8334287B2 (en) | 2009-07-17 | 2012-12-18 | Hoffmann-La Roche Inc. | Imidazoles |
EP2456438A2 (en) | 2009-07-23 | 2012-05-30 | Novartis AG | Use of azabicycloalkyl derivatives or pyrrolidine-2-one derivatives |
TWI558398B (zh) | 2009-09-22 | 2016-11-21 | 諾華公司 | 菸鹼乙醯膽鹼受體α7活化劑之用途 |
EP2490691A1 (en) | 2009-10-20 | 2012-08-29 | Novartis AG | Use of 1h-quinazoline-2,4-diones |
KR20130100906A (ko) | 2010-04-30 | 2013-09-12 | 노파르티스 아게 | 취약 x 증후군 (fxs) 치료에 유용한 예측용 마커 |
EP2585070A1 (en) | 2010-06-24 | 2013-05-01 | Novartis AG | Use of 1h-quinazoline-2,4-diones |
US9616097B2 (en) | 2010-09-15 | 2017-04-11 | Synergy Pharmaceuticals, Inc. | Formulations of guanylate cyclase C agonists and methods of use |
WO2012084873A1 (en) | 2010-12-20 | 2012-06-28 | Novartis Ag | 4- (hetero) aryl - ethynyl - octahydro - indole - 1 - carboxylic acid esters |
US9067881B2 (en) | 2011-01-24 | 2015-06-30 | Novartis Ag | 4-tolyl-ethynyl-octahydro-indole-1-ester derivatives |
BR112013018726A2 (pt) | 2011-01-27 | 2016-10-25 | Novartis Ag | uso de ativadores de alfa 7 do receptor nicotínico de acetilcolina |
BR112013023813A2 (pt) | 2011-03-18 | 2016-12-13 | Novartis Ag | combinações de ativadores do receptor acetilcolina nicotínico alfa 7 e antagonistas de mglur5 para uso em dopamina induzida por discinesia na doença de parkinson |
CA2846503A1 (en) | 2011-09-07 | 2013-03-14 | Novartis Ag | Use of 1h-quinazoline-2,4-diones for use in the prevention or treatment of photosensitive epilepsy |
WO2013131981A1 (en) | 2012-03-08 | 2013-09-12 | Novartis Ag | Predictive markers useful in the diagnosis and treatment of fragile x syndrome (fxs) |
GB201215033D0 (en) | 2012-08-23 | 2012-10-10 | Novartis Ag | Diazepinone derivatives |
CN105263492B (zh) | 2013-01-15 | 2018-04-10 | 诺华有限公司 | α7烟碱型乙酰胆碱受体激动剂在治疗发作性睡病中的应用 |
WO2014111837A1 (en) | 2013-01-15 | 2014-07-24 | Novartis Ag | Use of alpha 7 nicotinic acetylcholine receptor agonists |
JP2016514671A (ja) | 2013-03-15 | 2016-05-23 | シナジー ファーマシューティカルズ インコーポレイテッド | グアニル酸シクラーゼのアゴニストおよびその使用 |
CA2905435A1 (en) | 2013-03-15 | 2014-09-25 | Synergy Pharmaceuticals Inc. | Compositions useful for the treatment of gastrointestinal disorders |
US10011637B2 (en) | 2013-06-05 | 2018-07-03 | Synergy Pharmaceuticals, Inc. | Ultra-pure agonists of guanylate cyclase C, method of making and using same |
WO2014199316A1 (en) * | 2013-06-12 | 2014-12-18 | Novartis Ag | Modified release formulation |
CN105669686B (zh) * | 2014-11-19 | 2018-08-03 | 上海合全药业股份有限公司 | 一种6-(叔丁氧羰基)八氢呋喃[2,3-c]吡啶-4-羧酸的合成方法 |
JP2020529975A (ja) | 2017-07-31 | 2020-10-15 | ノバルティス アーゲー | コカイン使用の低減又はコカイン使用再燃の予防におけるマボグルラントの使用 |
CA3067688A1 (en) | 2017-07-31 | 2019-02-07 | Novartis Ag | Use of mavoglurant in the reduction of alcohol use or in preventing relapse into alcohol use |
US20220175793A1 (en) | 2019-01-29 | 2022-06-09 | Novartis Ag | The use of an mglur5 antagonist for treating opioid analgesic tolerance |
CA3181961A1 (en) | 2020-07-17 | 2022-01-20 | Novartis Ag | Use of mglur5 antagonists |
US20240050408A1 (en) | 2020-12-11 | 2024-02-15 | Novartis Ag | Use of mglur5 antagonists for treating amphetamine addiction |
US20240082215A1 (en) | 2020-12-14 | 2024-03-14 | Novartis Ag | Use of mglur5 antagonists for treating gambling disorder |
Family Cites Families (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE2741009A1 (de) * | 1976-09-22 | 1978-03-23 | Sandoz Ag | 4-styryl-4-indolinol-derivate, ihre verwendung und herstellung |
DE2802833A1 (de) | 1978-01-23 | 1979-07-26 | Sandoz Ag | 4-styryl-4-indolinol-derivate, ihre verwendung und herstellung |
US5264456A (en) | 1989-12-29 | 1993-11-23 | Allergan, Inc. | Acetylenes disubstituted with a furyl group and a substituted phenyl group having retinoid like activity |
US5284957A (en) * | 1992-09-03 | 1994-02-08 | Eli Lilly And Company | Excitatory amino acid receptor antagonists |
US5593994A (en) | 1994-09-29 | 1997-01-14 | The Dupont Merck Pharmaceutical Company | Prostaglandin synthase inhibitors |
DE69634822T2 (de) | 1995-08-22 | 2006-04-27 | Japan Tobacco Inc. | Amid-verbindungen und ihre anwendung |
WO1997048697A1 (en) | 1996-06-19 | 1997-12-24 | Rhone-Poulenc Rorer Limited | Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase |
TW544448B (en) * | 1997-07-11 | 2003-08-01 | Novartis Ag | Pyridine derivatives |
US6313071B1 (en) | 1998-06-04 | 2001-11-06 | Kumiai Chemical Industry Co., Ltd. | Phenylacetylene derivatives and agricultural/horticultural fungicides |
ID29095A (id) | 1998-10-02 | 2001-07-26 | Novartis Ag Cs | Antagonis mglur5 untuk pengobatan rasa sakit dan kegelisahan |
TR200200066T2 (tr) | 1999-07-06 | 2002-04-22 | Eli Lilly And Company | Migrenin tedavisi için seçici iGluR5 reseptör antagonistleri |
GB0007108D0 (en) | 2000-03-23 | 2000-05-17 | Novartis Ag | Organic compounds |
AU1339302A (en) | 2000-10-20 | 2002-05-06 | Biocryst Pharm Inc | Biaryl compounds as serine protease inhibitors |
ATE288898T1 (de) | 2000-12-04 | 2005-02-15 | Hoffmann La Roche | Phenylethenyl- oder phenylethinylderivate als glutamatrezeptorantagonisten |
GB0103045D0 (en) * | 2001-02-07 | 2001-03-21 | Novartis Ag | Organic Compounds |
US7138404B2 (en) | 2001-05-23 | 2006-11-21 | Hoffmann-La Roche Inc. | 4-aminopyrimidine derivatives |
TW200303309A (en) | 2001-12-04 | 2003-09-01 | Bristol Myers Squibb Co | Novel n-[4-(1h-imidazol-1-yl)-2-fluorophenyl]-3-trifluoromethyl)-1h-pyrazole-5-carboxamides as factor Xa inhibitors |
GB0128996D0 (en) * | 2001-12-04 | 2002-01-23 | Novartis Ag | Organic compounds |
HUP0402344A2 (hu) | 2001-12-04 | 2005-02-28 | F. Hoffmann-La Roche Ag | Helyettesített 2-amino-cikloalkán-karboxamidok, felhasználásuk cisztein-proteáz-inhibitorként, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények |
-
2001
- 2001-12-04 GB GBGB0128996.6A patent/GB0128996D0/en not_active Ceased
-
2002
- 2002-12-01 EG EG2002121297A patent/EG24936A/xx active
- 2002-12-02 PE PE2002001157A patent/PE20030640A1/es not_active Application Discontinuation
- 2002-12-02 TW TW091134933A patent/TWI328578B/zh not_active IP Right Cessation
- 2002-12-02 AR ARP020104641A patent/AR037682A1/es not_active Application Discontinuation
- 2002-12-03 US US10/497,363 patent/US7348353B2/en not_active Expired - Lifetime
- 2002-12-03 KR KR1020047008477A patent/KR100959204B1/ko not_active IP Right Cessation
- 2002-12-03 DE DE60211944T patent/DE60211944T2/de not_active Expired - Lifetime
- 2002-12-03 MY MYPI20024525A patent/MY137774A/en unknown
- 2002-12-03 NZ NZ533266A patent/NZ533266A/en not_active IP Right Cessation
- 2002-12-03 CA CA2466560A patent/CA2466560C/en not_active Expired - Fee Related
- 2002-12-03 PL PL368739A patent/PL212996B1/pl unknown
- 2002-12-03 MX MXPA04005456A patent/MXPA04005456A/es active IP Right Grant
- 2002-12-03 BR BR0214666-5A patent/BR0214666A/pt not_active Application Discontinuation
- 2002-12-03 HU HU0402191A patent/HU229429B1/hu unknown
- 2002-12-03 CN CN200810166366.0A patent/CN101366714B/zh not_active Expired - Lifetime
- 2002-12-03 IL IL16199002A patent/IL161990A0/xx not_active IP Right Cessation
- 2002-12-03 AU AU2002358585A patent/AU2002358585B2/en not_active Ceased
- 2002-12-03 JP JP2003548836A patent/JP4176020B2/ja not_active Expired - Lifetime
- 2002-12-03 DK DK02792867T patent/DK1453512T3/da active
- 2002-12-03 ES ES02792867T patent/ES2263842T3/es not_active Expired - Lifetime
- 2002-12-03 CN CNB028232968A patent/CN100430059C/zh not_active Expired - Lifetime
- 2002-12-03 EP EP02792867A patent/EP1453512B8/en not_active Expired - Lifetime
- 2002-12-03 WO PCT/EP2002/013670 patent/WO2003047581A1/en active Application Filing
- 2002-12-03 AT AT02792867T patent/ATE327755T1/de active
- 2002-12-03 RU RU2004120781/04A patent/RU2341515C2/ru not_active IP Right Cessation
- 2002-12-03 KR KR1020107002745A patent/KR100980901B1/ko not_active IP Right Cessation
- 2002-12-03 PT PT02792867T patent/PT1453512E/pt unknown
-
2004
- 2004-05-14 ZA ZA2004/03713A patent/ZA200403713B/en unknown
- 2004-06-04 EC EC2004005139A patent/ECSP045139A/es unknown
- 2004-06-07 CO CO04053105A patent/CO5590929A2/es active IP Right Grant
- 2004-06-25 NO NO20042673A patent/NO327005B1/no not_active IP Right Cessation
-
2005
- 2005-02-28 HK HK05101701A patent/HK1071510A1/xx not_active IP Right Cessation
-
2006
- 2006-08-03 CY CY20061101091T patent/CY1105460T1/el unknown
-
2008
- 2008-02-29 US US12/040,081 patent/US20080146647A1/en not_active Abandoned
- 2008-07-09 JP JP2008179005A patent/JP5036648B2/ja not_active Expired - Lifetime
-
2011
- 2011-09-22 US US13/239,467 patent/US8536229B2/en not_active Expired - Lifetime
-
2012
- 2012-11-20 AR ARP120104356A patent/AR088921A2/es not_active Application Discontinuation
-
2013
- 2013-08-15 US US13/967,719 patent/US20130331568A1/en not_active Abandoned
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HUP0402191A2 (hu) | Humán metabotrop glutamát receptor antagonista aktivitással rendelkező acetilénszármazékok, eljárás előállításukra, az ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk | |
HUP0302167A2 (hu) | Metabotropikus glutamát receptor antagonista hatású kinolinszármazékok, a vegyületeket tartalmazó gyógyszerkészítmények és eljárás előállításukra | |
HUP0203312A2 (hu) | Farmakológiailag hatékony szulfonamidszármazékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk | |
HUP0402507A2 (hu) | N(fenilszulfonil)glicin-származékok, alkalmazásuk és az ezeket tartalmazó gyógyászati készítmények | |
HUP0300846A2 (hu) | Imidazopirimidin- és triazolopirimidin-származékok, eljárás előállításukra és ilyen vegyületeket tartalmazó gyógyszerkészítmények | |
HUP0001802A2 (hu) | Pirazin-származékok, eljárás előállításukra és a vegyületeket tartalmazó gyógyászati készítmények | |
HUP0102851A2 (hu) | Parazitaellenes artemizinin-származékok (endoperoxidok), eljárás előállításukra és a vegyületeket tartalmazó gyógyászati készítmények | |
HRP20040317A2 (en) | 1,8-naphthyridine derivatives as antidiabetics | |
EP1725536B8 (en) | Imidazoline derivatives having cb1-antagonistic activity | |
HUP0302474A2 (hu) | Terápiásan hatásos tropánszármazékok, eljárás az előállításukra, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk | |
HUP0204245A2 (hu) | Új N-aza-biciklo-amid-származékok, eljárás az előállításukra, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk | |
HUP0100266A2 (hu) | NMDA-receptor-antagonista hatású 1-aminoalkilciklohexánszármazékok, a vegyületeket tartalmazó gyógyszerkészítmények és előállításaik | |
HUP0102084A2 (hu) | Kinolinszármazékok, eljárás előállításukra és a vegyületeket tartalmazó gyógyszerkészítmények | |
WO2008080844A9 (en) | Azaspiro derivatives | |
DE60202958D1 (de) | Stabiles polymorph von flibanserin, industrielles verfahren zu dessen herstellung und dessen verwendung zur herstellung von medikamenten | |
EA200601194A1 (ru) | Новые производные бензофурана, используемые для профилактики или лечения нарушений, связанных с 5-ht-рецептором | |
HUP0303639A2 (hu) | Új amlodipin-kamzilát és eljárás annak előállítására | |
MX2009005507A (es) | Derivados de espiro-piperidina. | |
HUP0301587A2 (hu) | Foszfodiészteráz V gátló hatású 5-amino-alkil-pirazolo[4,3-d]pirimidinek, ezeket tartalmazó gyógyszerkészítmények és eljárások az elżállításaikra | |
WO2008077810A3 (en) | Spiro-piperidine derivatives | |
IL166057A0 (en) | Urea-substituted and urethane-substituted acylureas methods for the production thereof and their useas medicaments | |
HUP0400345A2 (hu) | Vírusellenes aktivitású foszfono-pirimidin-származékok | |
HUP0401018A2 (hu) | 2H-1-benzopirán-származékok, eljárás ezek előállítására és ezeket tartalmazó gyógyászati készítmények | |
HUP0302616A2 (hu) | Triptaminszármazékok és analóg vegyületek, alkalmazásuk és az ezeket tartalmazó gyógyszerkészítmények | |
HUP0401444A2 (hu) | Kombinált LH és FSH agonista aktivitással rendelkező tieno[2,3-d]pirimidinek, alkalmazásuk és az ezeket tartalmazó gyógyszerkészítmények |