CN1946398A - 噻二唑二酮作为gsk-3抑制剂 - Google Patents
噻二唑二酮作为gsk-3抑制剂 Download PDFInfo
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- CN1946398A CN1946398A CNA2005800121414A CN200580012141A CN1946398A CN 1946398 A CN1946398 A CN 1946398A CN A2005800121414 A CNA2005800121414 A CN A2005800121414A CN 200580012141 A CN200580012141 A CN 200580012141A CN 1946398 A CN1946398 A CN 1946398A
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- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/433—Thidiazoles
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- 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
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- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
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- A61P9/00—Drugs for disorders of the cardiovascular system
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- 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
- C07D417/02—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 two hetero rings
- C07D417/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
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- Bioinformatics & Cheminformatics (AREA)
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- Biomedical Technology (AREA)
- Diabetes (AREA)
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- Obesity (AREA)
- Immunology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Reproductive Health (AREA)
- Psychology (AREA)
- Child & Adolescent Psychology (AREA)
- Gynecology & Obstetrics (AREA)
- Hospice & Palliative Care (AREA)
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- Emergency Medicine (AREA)
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- Pregnancy & Childbirth (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
Abstract
Description
时间(分钟) | %A | %B |
0 | 100 | 0 |
20 | 0 | 100 |
21 | 100 | 0 |
25 | 100 | 0 |
化合物 | %未结合化合物 | |
谷胱甘肽 | 白蛋白 | |
1 | 34.7 | 80.2 |
2 | 95.0 | 98.0 |
3(对比) | 15.0 | 54.0 |
4 | 32.3 | 67.2 |
5 | 72.0 | 65.5 |
6 | 52.0 | 84.0 |
7 | 31.0 | 68.3 |
8 | 59.4 | 62.3 |
9 | 71.7 | 91.4 |
10 | 100.0 | 98.9 |
剂量 | 200mg/kg | 20mg/kg |
C max | 9061.34ng/mL | 904.95ng/mL |
生物利用度 | 未评估 | 31.87% |
Claims (22)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP04075997A EP1586318A1 (en) | 2004-04-05 | 2004-04-05 | Thiadiazolidinones as GSK-3 inhibitors |
EP04075997.9 | 2004-04-05 | ||
PCT/EP2005/003613 WO2005097117A1 (en) | 2004-04-05 | 2005-04-04 | Thiadiazolidinones as gsk-3 inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
CN1946398A true CN1946398A (zh) | 2007-04-11 |
CN1946398B CN1946398B (zh) | 2011-03-30 |
Family
ID=34928129
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN2005800121414A Active CN1946398B (zh) | 2004-04-05 | 2005-04-04 | 噻二唑二酮作为gsk-3抑制剂 |
Country Status (30)
Country | Link |
---|---|
US (2) | US7531561B2 (zh) |
EP (2) | EP1586318A1 (zh) |
JP (1) | JP4995076B2 (zh) |
KR (1) | KR101151647B1 (zh) |
CN (1) | CN1946398B (zh) |
AR (2) | AR048820A1 (zh) |
AT (1) | ATE446090T1 (zh) |
AU (1) | AU2005230392B2 (zh) |
BR (1) | BRPI0508788A (zh) |
CA (1) | CA2559740C (zh) |
CY (1) | CY1109724T1 (zh) |
DE (1) | DE602005017215D1 (zh) |
DK (1) | DK1586319T3 (zh) |
EC (1) | ECSP066858A (zh) |
ES (1) | ES2335505T3 (zh) |
HK (1) | HK1100426A1 (zh) |
HR (1) | HRP20100032T1 (zh) |
IL (1) | IL178125A (zh) |
MA (1) | MA28515B1 (zh) |
MX (1) | MXPA06011194A (zh) |
NO (1) | NO332751B1 (zh) |
NZ (1) | NZ549904A (zh) |
PL (1) | PL1586319T3 (zh) |
PT (1) | PT1586319E (zh) |
RS (1) | RS51340B (zh) |
RU (1) | RU2379300C2 (zh) |
SI (1) | SI1586319T1 (zh) |
TW (1) | TWI352084B (zh) |
WO (1) | WO2005097117A1 (zh) |
ZA (1) | ZA200608221B (zh) |
Cited By (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN103992313A (zh) * | 2013-02-18 | 2014-08-20 | 江苏欧威医药有限公司 | 1,2,4-噻二唑-3,5-二酮衍生物及其药物组合物和用途 |
CN103992312A (zh) * | 2013-02-18 | 2014-08-20 | 江苏欧威医药有限公司 | 1,2,4-噻二唑-3,5-二酮衍生物及其药物组合物和应用 |
CN107151235A (zh) * | 2016-03-04 | 2017-09-12 | 上海市计划生育科学研究所 | 噻二唑烷二酮基gsk3抑制剂在调节***运动能力中的用途 |
CN113827592A (zh) * | 2020-06-24 | 2021-12-24 | 中国科学院上海药物研究所 | 一种噻二唑烷二酮基化合物在治疗致病性感染中的应用 |
CN115197167A (zh) * | 2022-07-22 | 2022-10-18 | 中国药科大学 | 1,2,4-噻二唑烷-3,5-二酮化合物及其制备方法和应用 |
CN117986202A (zh) * | 2024-04-03 | 2024-05-07 | 中国药科大学 | 具有ptpn2抑制活性的1,2,4-噻二唑烷-3,5-二酮化合物及其制备方法和应用 |
Families Citing this family (54)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2288948T3 (es) | 2000-05-11 | 2008-02-01 | Consejo Superior De Investigaciones Cientificas | Inhibidores heterociclicos del glicogeno sintasa quinasa gsk-3. |
EP1586318A1 (en) * | 2004-04-05 | 2005-10-19 | Neuropharma S.A.U. | Thiadiazolidinones as GSK-3 inhibitors |
WO2006045581A1 (en) * | 2004-10-21 | 2006-05-04 | Neuropharma, S.A. | The use of 1, 2, 4-thiadiazolidine-3, 5-diones as ppar activators |
ES2258406B1 (es) * | 2005-02-10 | 2007-12-01 | Neuropharma, S.A. | Uso de compuestos heterociclicos como agentes neurogenicos. |
EP1749523A1 (en) * | 2005-07-29 | 2007-02-07 | Neuropharma, S.A. | GSK-3 inhibitors |
CA2658263A1 (en) * | 2006-07-18 | 2008-01-24 | University Of Rochester | Thiadiazolidinone derivatives |
WO2008012031A2 (en) * | 2006-07-25 | 2008-01-31 | Universität Bern | Blockers of gsk3 for the prevention and treatment of pemphigus vulgaris |
CA2666193A1 (en) | 2006-08-08 | 2008-02-14 | Sanofi-Aventis | Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, process for preparing them, medicaments comprising these compounds, and their use |
CN101573352A (zh) | 2006-10-21 | 2009-11-04 | 艾博特股份有限两合公司 | 杂环化合物和其作为糖原合酶激酶3抑制剂的用途 |
KR100837785B1 (ko) * | 2007-01-17 | 2008-06-13 | 한국화학연구원 | 1,2,4-티아다이아졸리딘-3,5-다이온 화합물을 포함하는염증관련 질환의 치료 및 예방을 위한 약제학적 조성물 |
KR100829468B1 (ko) * | 2007-01-17 | 2008-05-16 | 한국화학연구원 | 신규한 1,2,4-티아다이아졸리딘-3,5-다이온 화합물 및 이의제조방법 |
EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
WO2009097995A1 (de) * | 2008-02-07 | 2009-08-13 | Sanofi-Aventis | Neue phenyl-substituierte imidazolidine, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
AR072707A1 (es) | 2008-07-09 | 2010-09-15 | Sanofi Aventis | Compuestos heterociclicos, procesos para su preparacion, medicamentos que comprenden estos compuestos y el uso de los mismos |
EP2177510A1 (en) | 2008-10-17 | 2010-04-21 | Universität des Saarlandes | Allosteric protein kinase modulators |
WO2010068601A1 (en) | 2008-12-08 | 2010-06-17 | Sanofi-Aventis | A crystalline heteroaromatic fluoroglycoside hydrate, processes for making, methods of use and pharmaceutical compositions thereof |
DK2470552T3 (en) | 2009-08-26 | 2014-02-17 | Sanofi Sa | NOVEL, CRYSTALLINE, heteroaromatic FLUORGLYCOSIDHYDRATER, MEDICINES COVERING THESE COMPOUNDS AND THEIR USE |
WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
WO2011151359A1 (en) * | 2010-06-02 | 2011-12-08 | Noscira, S.A. | Combined treatment with a cholinesterase inhibitor and a thiadiazolidinedione derivative |
EP2582709B1 (de) | 2010-06-18 | 2018-01-24 | Sanofi | Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen |
US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
CN103119035B (zh) | 2010-09-27 | 2015-09-30 | 雅培股份有限两合公司 | 杂环化合物和它们作为糖原合成酶激酶-3抑制剂的用途 |
WO2012065065A1 (en) * | 2010-11-12 | 2012-05-18 | Follica, Inc. | Methods and compositions for modulating hair growth, wound healing and scar revision |
JP2014500275A (ja) | 2010-12-06 | 2014-01-09 | フォリカ,インコーポレイテッド | 禿頭症を治療するため、および毛髪の成長を促進するための方法 |
US9090592B2 (en) | 2010-12-30 | 2015-07-28 | AbbVie Deutschland GmbH & Co. KG | Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors |
WO2012120058A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Mit benzyl- oder heteromethylengruppen substituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
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WO2012120051A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Mit adamantan- oder noradamantan substituierte benzyl-oxathiazinderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
WO2012149335A2 (en) * | 2011-04-28 | 2012-11-01 | Richard Neubig | Small molecule inhibitors of rgs proteins |
EP2527323A1 (en) | 2011-05-24 | 2012-11-28 | Noscira, S.A. | Urea carbonyl disulfide derivatives and their therapeutic uses |
WO2012170657A1 (en) * | 2011-06-07 | 2012-12-13 | Georgetown University | Targeting gsk-3beta for the treatment of parkinson's disease |
EP2567959B1 (en) | 2011-09-12 | 2014-04-16 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
EP2760862B1 (en) | 2011-09-27 | 2015-10-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
AU2013224041B2 (en) | 2012-02-24 | 2017-08-24 | Asd Therapeutics Partners Llc | Thiadiazolidinediones as GSK-3 inhibitors |
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EP1586318A1 (en) * | 2004-04-05 | 2005-10-19 | Neuropharma S.A.U. | Thiadiazolidinones as GSK-3 inhibitors |
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CN103992313A (zh) * | 2013-02-18 | 2014-08-20 | 江苏欧威医药有限公司 | 1,2,4-噻二唑-3,5-二酮衍生物及其药物组合物和用途 |
CN103992312A (zh) * | 2013-02-18 | 2014-08-20 | 江苏欧威医药有限公司 | 1,2,4-噻二唑-3,5-二酮衍生物及其药物组合物和应用 |
CN107151235A (zh) * | 2016-03-04 | 2017-09-12 | 上海市计划生育科学研究所 | 噻二唑烷二酮基gsk3抑制剂在调节***运动能力中的用途 |
CN107151235B (zh) * | 2016-03-04 | 2019-12-13 | 上海市计划生育科学研究所 | 噻二唑烷二酮基gsk3抑制剂在调节***运动能力中的用途 |
CN113827592A (zh) * | 2020-06-24 | 2021-12-24 | 中国科学院上海药物研究所 | 一种噻二唑烷二酮基化合物在治疗致病性感染中的应用 |
CN115197167A (zh) * | 2022-07-22 | 2022-10-18 | 中国药科大学 | 1,2,4-噻二唑烷-3,5-二酮化合物及其制备方法和应用 |
CN117986202A (zh) * | 2024-04-03 | 2024-05-07 | 中国药科大学 | 具有ptpn2抑制活性的1,2,4-噻二唑烷-3,5-二酮化合物及其制备方法和应用 |
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