HUP0303559A2 - Magas intracelluláris kalciumkoncentrációnál funkcionáló szelektív maxi-K káliumcsatorna nyitók és alkalmazásuk - Google Patents
Magas intracelluláris kalciumkoncentrációnál funkcionáló szelektív maxi-K káliumcsatorna nyitók és alkalmazásukInfo
- Publication number
- HUP0303559A2 HUP0303559A2 HU0303559A HUP0303559A HUP0303559A2 HU P0303559 A2 HUP0303559 A2 HU P0303559A2 HU 0303559 A HU0303559 A HU 0303559A HU P0303559 A HUP0303559 A HU P0303559A HU P0303559 A2 HUP0303559 A2 HU P0303559A2
- Authority
- HU
- Hungary
- Prior art keywords
- maxi
- compounds
- opening
- channel
- potassium channel
- Prior art date
Links
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 title abstract 5
- 239000011575 calcium Substances 0.000 title abstract 5
- 229910052791 calcium Inorganic materials 0.000 title abstract 5
- 230000003834 intracellular effect Effects 0.000 title abstract 3
- 229940127315 Potassium Channel Openers Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 6
- 102000016469 Large-Conductance Calcium-Activated Potassium Channels Human genes 0.000 abstract 3
- 108010092555 Large-Conductance Calcium-Activated Potassium Channels Proteins 0.000 abstract 3
- PRQZENXGVVLPIF-UHFFFAOYSA-N 1-chloro-3h-indol-2-one Chemical class C1=CC=C2N(Cl)C(=O)CC2=C1 PRQZENXGVVLPIF-UHFFFAOYSA-N 0.000 abstract 2
- 102000004257 Potassium Channel Human genes 0.000 abstract 2
- 108020001213 potassium channel Proteins 0.000 abstract 2
- SCRXASNUPJPFGP-UHFFFAOYSA-N 1-fluoro-3h-indol-2-one Chemical compound C1=CC=C2N(F)C(=O)CC2=C1 SCRXASNUPJPFGP-UHFFFAOYSA-N 0.000 abstract 1
- 108091006146 Channels Proteins 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 230000003213 activating effect Effects 0.000 abstract 1
- 238000003556 assay Methods 0.000 abstract 1
- 208000037765 diseases and disorders Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000000472 traumatic effect Effects 0.000 abstract 1
Classifications
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- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
- A61P25/06—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
- A61P25/08—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
- 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
- A61P25/28—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Steroid Compounds (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Indole Compounds (AREA)
Abstract
A találmány kalciumszenzitív és szelektív maxi-K káliumcsatornanyitó/aktiváló vegyületekre vonatkozik, amelyek funkciójuk szerintnyitják a maxi-K csatornákat magas intracelluláriskalciumkoncentrációk jelenlétében és szignifikánsan nem befolyásoljáka maxi-K csatorna proteinek nyílását alacsony vagy fiziológiásannormális kalciumkoncentrációk jelenlétében. Rendelkezésre bocsátanakvizsgáló módszereket ilyen vegyületekre és eljárásokat ilyenvegyületek alkalmazására. A találmány szerint a teljessejt-feszültségpatch-clamp kísérletek legújabban kimutatták, hogy a nyitóvegyületek,például a fluor-oxindolok és klór oxindolok, maxi-K csatornanyitóképessége érzékeny volt az intracelluláris Ca2+ koncentrációra([Ca2+]i), azaz több csatornát nyitottak negatívabb potenciálokmellett. Speciális fluor-oxindol és klór-oxindol vegyületekszignifikáns növekedést hoztak létre teljessejt maxi-K káliumcsatorna-közvetített outward áramokban kizárólag olyan sejtekben, amelyekbenmagasabb volt a[Ca2+]i, összehasonlítva az alacsonyabb[Ca2+]i-nélkapott hatásokkal. Az ilyen vegyületek olyan Ca2+-szenzitív ésszelektív maxi-K csatornanyitókat biztosítanak, amelyek maximálishatásosságot mutatnak megnövekedett[Ca2+]i esetén és mint ilyenek,olyan betegségek és rendellenességek kezelését teszik lehetővé,amelyekben a sejtek traumás stresszen mennek keresztül vagy traumásstressz alatt állnak magas belső kalciumszintek következtében, mintpéldául sztrók esetén. Ó
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24014600P | 2000-10-13 | 2000-10-13 | |
| PCT/US2001/032079 WO2002030868A1 (en) | 2000-10-13 | 2001-10-12 | Selective maxi-k- potassium channel openers functional under conditions of high intracellular calcium concentration, methods and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0303559A2 true HUP0303559A2 (hu) | 2004-03-01 |
| HUP0303559A3 HUP0303559A3 (en) | 2006-02-28 |
Family
ID=22905295
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0303559A HUP0303559A3 (en) | 2000-10-13 | 2001-10-12 | Selective maxi-k-potassium channel openers functional under conditions of high intracellular calcium concentration and uses thereof |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US20020045566A1 (hu) |
| EP (1) | EP1330426A4 (hu) |
| JP (1) | JP2004511457A (hu) |
| AU (1) | AU2002213204A1 (hu) |
| CA (1) | CA2425771A1 (hu) |
| HU (1) | HUP0303559A3 (hu) |
| WO (1) | WO2002030868A1 (hu) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002072088A2 (en) * | 2001-02-20 | 2002-09-19 | Bristol-Myers Squibb Company | Modulators of kcnq potassium channels and use thereof in treating migraine and mechanistically related diseases |
| SE0302546D0 (sv) | 2003-09-24 | 2003-09-24 | Astrazeneca Ab | New compounds |
| SE0200979D0 (sv) | 2002-03-28 | 2002-03-28 | Astrazeneca Ab | New compounds |
| TW200508197A (en) * | 2003-03-31 | 2005-03-01 | Ucb Sa | Indolone-acetamide derivatives, processes for preparing them and their uses |
| US8058056B2 (en) * | 2004-03-12 | 2011-11-15 | The Regents Of The University Of California | Method and apparatus for integrated cell handling and measurements |
| AR053710A1 (es) | 2005-04-11 | 2007-05-16 | Xenon Pharmaceuticals Inc | Compuestos espiroheterociclicos y sus usos como agentes terapeuticos |
| AR056968A1 (es) | 2005-04-11 | 2007-11-07 | Xenon Pharmaceuticals Inc | Compuestos espiro-oxindol y composiciones farmacéuticas |
| AR056317A1 (es) * | 2005-04-20 | 2007-10-03 | Xenon Pharmaceuticals Inc | Compuestos de oxindol y composicion farmaceutica |
| US8293524B2 (en) * | 2006-03-31 | 2012-10-23 | Fluxion Biosciences Inc. | Methods and apparatus for the manipulation of particle suspensions and testing thereof |
| MX2009003876A (es) | 2006-10-12 | 2009-05-11 | Xenon Pharmaceuticals Inc | Uso de compuestos de espiro-oxindol como agentes terapeuticos. |
| KR101286323B1 (ko) | 2008-10-17 | 2013-07-15 | 제논 파마슈티칼스 인크. | 스피로-옥스인돌 화합물 및 치료제로서의 그의 용도 |
| CA2741024A1 (en) | 2008-10-17 | 2010-04-22 | Xenon Pharmaceuticals Inc. | Spiro-oxindole compounds and their use as therapeutic agents |
| AR077252A1 (es) | 2009-06-29 | 2011-08-10 | Xenon Pharmaceuticals Inc | Enantiomeros de compuestos de espirooxindol y sus usos como agentes terapeuticos |
| MY165579A (en) | 2009-10-14 | 2018-04-05 | Xenon Pharmaceuticals Inc | Synthetic methods for spiro-oxindole compounds |
| CN105726531A (zh) | 2010-02-26 | 2016-07-06 | 泽农医药公司 | 用于局部给药的螺-羟吲哚化合物的药物组合物及其作为治疗剂的用途 |
| EP2540295A1 (en) | 2011-06-27 | 2013-01-02 | Centre national de la recherche scientifique | Compositions for the treatment of Fragile X syndrome |
| WO2016127068A1 (en) | 2015-02-05 | 2016-08-11 | Teva Pharmaceuticals International Gmbh | Methods of treating postherpetic neuralgia with a topical formulation of a spiro-oxindole compound |
| US10167502B2 (en) | 2015-04-03 | 2019-01-01 | Fluxion Biosciences, Inc. | Molecular characterization of single cells and cell populations for non-invasive diagnostics |
| CN106770618A (zh) * | 2015-11-20 | 2017-05-31 | 中国康复研究中心 | 一种建立急性缺血性脑卒中特征蛋白的质谱模型的方法 |
| WO2018157046A1 (en) * | 2017-02-24 | 2018-08-30 | Ovid Therapeutics Inc. | Methods of treating seizure disorders |
| CN110240558B (zh) * | 2019-07-10 | 2022-05-27 | 上海华理生物医药股份有限公司 | 一种Flindokalner消旋体的新合成方法 |
| CA3217887A1 (en) * | 2021-05-04 | 2022-11-10 | Joseph V. Pergolizzi | Large-conductance potassium channel modulators, compositions thereof, methods of manufacturing thereof, and methods of use thereof |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5621007A (en) * | 1993-11-03 | 1997-04-15 | Bristol-Myers Squibb Company | Method for regulation of transmembrane chloride conductance |
| US5637470A (en) * | 1994-05-13 | 1997-06-10 | Merck & Co., Inc. | Screening array using cells expressing recombinant α and β subunits of the mammalian large-conductance (maxi-K) potassium channel |
| IT1273701B (it) * | 1994-07-29 | 1997-07-09 | Enichem Elastomers | Derivati metallorganici del grupo iiia e procedimento per la loro preparazione |
| US5565483A (en) * | 1995-06-07 | 1996-10-15 | Bristol-Myers Squibb Company | 3-substituted oxindole derivatives as potassium channel modulators |
| TW467902B (en) * | 1996-07-31 | 2001-12-11 | Bristol Myers Squibb Co | Diphenyl heterocycles as potassium channel modulators |
| TW504504B (en) * | 1996-11-26 | 2002-10-01 | Bristol Myers Squibb Co | 4-aryl-3-hydroxyquinolin-2-one derivatives as ion channel modulators |
| HUP0002449A3 (en) * | 1997-05-30 | 2001-12-28 | Bristol Myers Squibb Company W | Process for producing 3-fluoro oxindole derivatives and intermediates of the preparation |
| CA2318814A1 (en) * | 1998-01-29 | 1999-08-05 | Xi Chen | Benzoate derivatives of diaryl 1,3,4-oxadiazolone |
| EP1085890A1 (en) * | 1998-06-08 | 2001-03-28 | Advanced Medicine, Inc. | Novel sodium channel drugs and uses |
| AU755202B2 (en) * | 1998-12-04 | 2002-12-05 | Bristol-Myers Squibb Company | 3-substituted-4-arylquinolin-2-one derivatives as potassium channel modulators |
| KR20010101869A (ko) * | 1999-01-29 | 2001-11-15 | 스티븐 비. 데이비스 | 디아릴 1,3,4-옥사디아졸론의 카바메이트 유도체 |
-
2001
- 2001-10-12 HU HU0303559A patent/HUP0303559A3/hu unknown
- 2001-10-12 CA CA002425771A patent/CA2425771A1/en not_active Abandoned
- 2001-10-12 JP JP2002534257A patent/JP2004511457A/ja active Pending
- 2001-10-12 WO PCT/US2001/032079 patent/WO2002030868A1/en not_active Application Discontinuation
- 2001-10-12 EP EP01981570A patent/EP1330426A4/en not_active Withdrawn
- 2001-10-12 US US09/975,881 patent/US20020045566A1/en not_active Abandoned
- 2001-10-12 AU AU2002213204A patent/AU2002213204A1/en not_active Abandoned
-
2004
- 2004-09-28 US US10/952,523 patent/US20050043293A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP1330426A4 (en) | 2005-09-14 |
| WO2002030868A1 (en) | 2002-04-18 |
| CA2425771A1 (en) | 2002-04-18 |
| EP1330426A1 (en) | 2003-07-30 |
| US20050043293A1 (en) | 2005-02-24 |
| HUP0303559A3 (en) | 2006-02-28 |
| JP2004511457A (ja) | 2004-04-15 |
| US20020045566A1 (en) | 2002-04-18 |
| AU2002213204A1 (en) | 2002-04-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD9A | Lapse of provisional protection due to non-payment of fees |