KR101693133B1 - Tarp-감마 8 의존성 ampa 수용체 길항제로서의 6-((s)-1-｛1-[5-(2-히드록시-에톡시)-피리딘-2-일]-1h-피라졸-3-일｝-에틸)-3h-1,3-벤조티아졸-2-온 - Google Patents
Tarp-감마 8 의존성 ampa 수용체 길항제로서의 6-((s)-1-｛1-[5-(2-히드록시-에톡시)-피리딘-2-일]-1h-피라졸-3-일｝-에틸)-3h-1,3-벤조티아졸-2-온 Download PDFInfo
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- KR101693133B1 KR101693133B1 KR1020157013470A KR20157013470A KR101693133B1 KR 101693133 B1 KR101693133 B1 KR 101693133B1 KR 1020157013470 A KR1020157013470 A KR 1020157013470A KR 20157013470 A KR20157013470 A KR 20157013470A KR 101693133 B1 KR101693133 B1 KR 101693133B1
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- pyridin
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- benzothiazol
- pyrazol
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- 238000011287 therapeutic dose Methods 0.000 description 1
- 229940126585 therapeutic drug Drugs 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 229960003495 thiamine Drugs 0.000 description 1
- DPJRMOMPQZCRJU-UHFFFAOYSA-M thiamine hydrochloride Chemical compound Cl.[Cl-].CC1=C(CCO)SC=[N+]1CC1=CN=C(C)N=C1N DPJRMOMPQZCRJU-UHFFFAOYSA-M 0.000 description 1
- 229960002663 thioctic acid Drugs 0.000 description 1
- 229960002898 threonine Drugs 0.000 description 1
- 229940104230 thymidine Drugs 0.000 description 1
- 230000001256 tonic effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 230000001052 transient effect Effects 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 210000001364 upper extremity Anatomy 0.000 description 1
- 238000010200 validation analysis Methods 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- 235000019163 vitamin B12 Nutrition 0.000 description 1
- 239000011715 vitamin B12 Substances 0.000 description 1
- 229940011671 vitamin b6 Drugs 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- NWONKYPBYAMBJT-UHFFFAOYSA-L zinc sulfate Chemical compound [Zn+2].[O-]S([O-])(=O)=O NWONKYPBYAMBJT-UHFFFAOYSA-L 0.000 description 1
- 229960001763 zinc sulfate Drugs 0.000 description 1
- 229910000368 zinc sulfate Inorganic materials 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
-
- 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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261730273P | 2012-11-27 | 2012-11-27 | |
| US61/730,273 | 2012-11-27 | ||
| PCT/US2013/070885 WO2014085153A1 (en) | 2012-11-27 | 2013-11-20 | 6-((s)-1-{1-[5-(2-hydroxy-ethoxy)-pyridin-2-yl]-1h-pyrazol-3-yl}- ethyl)-3h-1,3-benzothiazol-2-one as a tarp-gamma 8 dependent ampa receptor antagonist |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20150070401A KR20150070401A (ko) | 2015-06-24 |
| KR101693133B1 true KR101693133B1 (ko) | 2017-01-04 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020157013470A Active KR101693133B1 (ko) | 2012-11-27 | 2013-11-20 | Tarp-감마 8 의존성 ampa 수용체 길항제로서의 6-((s)-1-｛1-[5-(2-히드록시-에톡시)-피리딘-2-일]-1h-피라졸-3-일｝-에틸)-3h-1,3-벤조티아졸-2-온 |
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| TW201609719A (zh) * | 2014-05-28 | 2016-03-16 | 美國禮來大藥廠 | 作為ＴＡＲＰ－γ８依賴性ＡＭＰＡ受體拮抗劑之６－經取代－３Ｈ－１，３－苯并噻唑－２－酮化合物 |
| WO2016176449A1 (en) * | 2015-04-29 | 2016-11-03 | Janssen Pharmaceutica Nv | Benzimidazolone and benzothiazolone compounds and their use as ampa receptor modulators |
| DK3288940T5 (da) | 2015-04-29 | 2021-09-20 | Janssen Pharmaceutica Nv | Azabenzimidazoler og deres anvendelse som ampa-receptormodulatorer |
| AU2016256413B2 (en) | 2015-04-29 | 2020-10-08 | Janssen Pharmaceutica Nv | Indolone compounds and their use as AMPA receptor modulators |
| WO2016176457A1 (en) | 2015-04-29 | 2016-11-03 | Janssen Pharmaceutica Nv | Imidazopyrazines and pyrazolopyrimidines and their use as ampa receptor modulators |
| JP6953527B2 (ja) * | 2016-10-26 | 2021-10-27 | ヤンセン ファーマシューティカ エヌ．ベー． | 縮合二環ピリジン化合物、及びａｍｐａ受容体調節因子としてのそれらの使用 |
| RU2650523C1 (ru) * | 2017-07-24 | 2018-04-16 | федеральное государственное автономное образовательное учреждение высшего образования "Казанский (Приволжский) федеральный университет" (ФГАОУ ВО КФУ) | Производное пиридоксина для лечения эпилепсии |
| RU2703286C1 (ru) * | 2019-06-18 | 2019-10-16 | федеральное государственное автономное образовательное учреждение высшего образования "Казанский (Приволжский) федеральный университет" (ФГАОУ ВО КФУ) | Соли (5-гидрокси-3,4-бис(гидроксиметил)-6-метилпиридин-2-ил)метансульфокислоты и способ их получения |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20150344468A1 (en) | 2014-05-28 | 2015-12-03 | Eli Lilly And Company | 6-substituted-3h-1,3-benzothiazol-2-one compounds as tarp-gamma 8 dependent ampa receptor antagonists |
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| MY132385A (en) * | 1995-08-31 | 2007-10-31 | Novartis Ag | 2,3-dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives |
| JP2000281676A (ja) * | 1999-01-25 | 2000-10-10 | Yamanouchi Pharmaceut Co Ltd | Ａｍｐａ拮抗化合物の新規製造法 |
| KR100904011B1 (ko) * | 2000-06-12 | 2009-06-22 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 1,2-디하이드로피리딘 화합물 및 그의 제조 방법 |
| US8995993B2 (en) * | 2000-10-11 | 2015-03-31 | Gogo Llc | System for managing mobile internet protocol addresses in an airborne wireless cellular network |
| BRPI0517425A (pt) * | 2004-12-17 | 2008-10-07 | Lilly Co Eli | composto ou um sal, solvato, enanciÈmero, diastereÈmero ou mistura de diastereÈmeros do mesmo, composição farmacêutica, uso de composto |
| WO2007076161A2 (en) | 2005-12-27 | 2007-07-05 | Myriad Genetics, Inc | Compounds with therapeutic activity |
| TW200817385A (en) * | 2006-07-04 | 2008-04-16 | Organon Nv | Heterocyclic derivatives |
| US20110178165A1 (en) * | 2008-10-08 | 2011-07-21 | Pfizer Inc. | Tetrahydrofuranyl sulfonamides and pharmaceutical compositions thereof |
| GEP20135992B (en) * | 2009-01-12 | 2013-12-25 | Icagen Inc | Sulfonamide derivatives |
| EP2576544A4 (en) * | 2010-06-01 | 2013-09-11 | Angion Biomedica Corp | INHIBITORS OF CYTOCHROMES P450 AND USES THEREOF |
| EP2694472B1 (en) * | 2011-04-05 | 2020-03-11 | Takeda Pharmaceutical Company Limited | Sulfonamide derivative and use thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20150344468A1 (en) | 2014-05-28 | 2015-12-03 | Eli Lilly And Company | 6-substituted-3h-1,3-benzothiazol-2-one compounds as tarp-gamma 8 dependent ampa receptor antagonists |
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