RU2006139030A - Ингибиторы gsk-3 - Google Patents
Ингибиторы gsk-3 Download PDFInfo
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- RU2006139030A RU2006139030A RU2006139030/04A RU2006139030A RU2006139030A RU 2006139030 A RU2006139030 A RU 2006139030A RU 2006139030/04 A RU2006139030/04 A RU 2006139030/04A RU 2006139030 A RU2006139030 A RU 2006139030A RU 2006139030 A RU2006139030 A RU 2006139030A
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- 102000002254 Glycogen Synthase Kinase 3 Human genes 0.000 title claims 3
- 108010014905 Glycogen Synthase Kinase 3 Proteins 0.000 title claims 3
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 15
- 201000010099 disease Diseases 0.000 claims 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 3
- 239000000651 prodrug Substances 0.000 claims 3
- 229940002612 prodrug Drugs 0.000 claims 3
- -1 —N = CR 7 R 8 Inorganic materials 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 206010012289 Dementia Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000027089 Parkinsonian disease Diseases 0.000 claims 2
- 206010034010 Parkinsonism Diseases 0.000 claims 2
- 208000006011 Stroke Diseases 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 230000006931 brain damage Effects 0.000 claims 2
- 231100000874 brain damage Toxicity 0.000 claims 2
- 208000029028 brain injury Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 239000003153 chemical reaction reagent Substances 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 208000030507 AIDS Diseases 0.000 claims 1
- 201000004384 Alopecia Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 1
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 1
- 208000011990 Corticobasal Degeneration Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 206010061598 Immunodeficiency Diseases 0.000 claims 1
- 208000029462 Immunodeficiency disease Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000019022 Mood disease Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000037065 Subacute sclerosing leukoencephalitis Diseases 0.000 claims 1
- 206010042297 Subacute sclerosing panencephalitis Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 206010044688 Trisomy 21 Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 208000037849 arterial hypertension Diseases 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 230000003143 atherosclerotic effect Effects 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 239000012472 biological sample Substances 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000037976 chronic inflammation Diseases 0.000 claims 1
- 208000037893 chronic inflammatory disorder Diseases 0.000 claims 1
- 206010014599 encephalitis Diseases 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 208000024963 hair loss Diseases 0.000 claims 1
- 230000003676 hair loss Effects 0.000 claims 1
- 206010020718 hyperplasia Diseases 0.000 claims 1
- 230000003463 hyperproliferative effect Effects 0.000 claims 1
- 230000007813 immunodeficiency Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 150000002540 isothiocyanates Chemical class 0.000 claims 1
- 201000002364 leukopenia Diseases 0.000 claims 1
- 231100001022 leukopenia Toxicity 0.000 claims 1
- 210000004558 lewy body Anatomy 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 230000000626 neurodegenerative effect Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 125000000962 organic group Chemical group 0.000 claims 1
- 201000010065 polycystic ovary syndrome Diseases 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 238000011084 recovery Methods 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- RLTPJVKHGBFGQA-UHFFFAOYSA-N thiadiazolidine Chemical compound C1CSNN1 RLTPJVKHGBFGQA-UHFFFAOYSA-N 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 208000019553 vascular disease Diseases 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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- A61P9/00—Drugs for disorders of the cardiovascular system
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- 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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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Immunology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychology (AREA)
- Reproductive Health (AREA)
- Dermatology (AREA)
- Gynecology & Obstetrics (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
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- Hospice & Palliative Care (AREA)
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- Urology & Nephrology (AREA)
- Pregnancy & Childbirth (AREA)
- Vascular Medicine (AREA)
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Claims (22)
1. Соединение общей формулы (I)
в которой R1 обозначает органическую группу, содержащую по меньшей мере 8 атомов, выбранных из C или О, которая не связана непосредственно с N через -C(O)- и включающую по меньшей мере ароматическое кольцо;
Ra, Rb, R2, R3, R4, R5, R6 независимо выбраны из водорода, замещенного или незамещенного алкила, замещенного или незамещенного циклоалкила, замещенного или незамещенного алкенила, замещенного или незамещенного арила, замещенного или незамещенного гетероциклила, -COR7, -C(O)OR7, -C(O)NR7R8, -C=NR7, -CN, -OR7, -OC(O)R7, -S(O)t-R7, -NR7R8, -NR7C(О)R8, -NO2, -N=CR7R8 или галогена,
причем Ra и Rb вместе могут образовывать группу =О, и причем любая из пар Ra R2, R2 R3, R3 R4, R4 R5, R5 R6, R6 Rb или R7 R8 может образовывать циклический заместитель;
t=0, 1, 2 или 3,
R7 и R8, каждый независимо, выбраны из водорода, замещенного или незамещенного алкила, замещенного или незамещенного циклоалкила, замещенного или незамещенного алкенила, замещенного или незамещенного арила, замещенного или незамещенного гетероциклила, замещенного или незамещенного алкокси, замещенного или незамещенного арилокси, галогена;
или его фармацевтически приемлемая соль, пролекарство или сольват.
2. Соединение по п.1, в котором R1 имеет по меньшей мере 10 ароматических атомов углерода.
3. Соединение по п.1, в котором ароматический радикал непосредственно связан с N тиадиазолидина.
4. Соединение по п.3, в котором R1 обозначает замещенный или незамещенный нафтил.
5. Соединение по п.4, в котором R1 обозначает замещенный или незамещенный альфа-нафтил, предпочтительно, незамещенный альфа-нафтил.
6. Соединение по п.1, в котором R1 обозначает группу, выбранную из:
7. Соединение по п. 1, в котором и Ra и Rb обозначают Н.
8. Соединение по п. 1, в котором R2, R3, R4, R5, R6 независимо выбраны из водорода, замещенного или незамещенного алкила, COR7, -C(O)OR7, -OR7, -NR7R8 или галогена, где R7 и R8 имеют значения, определенные в п.1.
9. Соединение по п.8, в котором R2, R3, R4, R5, R6 обозначают Н.
10. Соединение по п.1, которое имеет формулу:
или его фармацевтически приемлемая соль, пролекарство или сольват.
11. Способ получения соединения формулы (I) или его соли или сольвата по любому из пп.1-10, который включает введение в реакцию бензил-замещенного изотиоцианата формулы
с соединением формулы R1-N=C=O.
12. Способ по п.11, который включает реакцию:
где R1 имеет значение, определенное в п.1, предпочтительно определенное в п.6.
13. Фармацевтическая композиция, которая включает соединение по любому из пп.1-10 или его фармацевтически приемлемую соль, пролекарство или сольват и фармацевтически приемлемую основу, адъювант или носитель.
14. Фармацевтическая композиция по п.13 для перорального введения.
15. Применение соединения по любому из пп.1-10 в получении лекарственного средства.
16. Применение по п.15, в котором лекарственное средство предназначено для лечения опосредуемого GSK-3 заболевания или состояния.
17. Применение по п.16, в котором заболевание или состояние представляет собой диабет, состояния, связанные с диабетом, хронические нейродегенеративные состояния, включая деменции, такие как болезнь Альцгеймера, болезнь Паркинсона, прогрессирующий надъядерный паралич, подострый склерозирующий панэнцефалитный паркинсонизм, постэнцефалитный паркинсонизм, боксерский энцефалит, комплекс острова Гуам, болезнь Пика, кортикобазальную дегенерацию, лобно-височную деменцию, болезнь Гентингтона, СПИД-деменцию, боковой амиотрофический склероз, рассеянный склероз и нейротравматические заболевания, такие как острый инсульт, эпилепсия, нарушения настроения, такие как депрессия, шизофрения и биполярные нарушения, поддержка функционального восстановления после инсульта, мозговое кровотечение, например, вследствие солитарной церебральной амилоидной ангиопатии, выпадение волос, ожирение, атеросклеротическое сердечно-сосудистое заболевание, артериальную гипертензию, поликистозный синдром яичника, синдром X, ишемию, повреждение головного мозга, травматическое повреждение головного мозга, рак, лейкопению, синдром Дауна, заболевание с тельцами Леви, воспаление, хронические воспалительные заболевания, рак и гиперпролиферативные заболевания, такие как гиперплазии, и иммунодефицит.
18. Применение по п.17, в котором заболевание представляет собой болезнь Альцгеймера.
19. Применение по п.17, в котором заболевание представляет собой диабет типа II.
20. Применение по п.17, в котором заболевание представляет собой депрессию.
21. Применение по п.17, в котором заболевание представляет собой повреждение головного мозга.
22. Применение соединений формулы (I), определенной в любом из пп.1-10, в качестве реагентов для биологических проб, предпочтительно в качестве реагентов для ингибирования GSK-3.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04075997.9 | 2004-04-05 | ||
| EP04075997A EP1586318A1 (en) | 2004-04-05 | 2004-04-05 | Thiadiazolidinones as GSK-3 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2006139030A true RU2006139030A (ru) | 2008-05-20 |
| RU2379300C2 RU2379300C2 (ru) | 2010-01-20 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2006139030/04A RU2379300C2 (ru) | 2004-04-05 | 2005-04-04 | Ингибиторы gsk-3 |
Country Status (29)
| Country | Link |
|---|---|
| US (2) | US7531561B2 (ru) |
| EP (2) | EP1586318A1 (ru) |
| JP (1) | JP4995076B2 (ru) |
| KR (1) | KR101151647B1 (ru) |
| CN (1) | CN1946398B (ru) |
| AR (2) | AR048820A1 (ru) |
| AT (1) | ATE446090T1 (ru) |
| AU (1) | AU2005230392B2 (ru) |
| BR (1) | BRPI0508788A (ru) |
| CA (1) | CA2559740C (ru) |
| CY (1) | CY1109724T1 (ru) |
| DE (1) | DE602005017215D1 (ru) |
| DK (1) | DK1586319T3 (ru) |
| EC (1) | ECSP066858A (ru) |
| ES (1) | ES2335505T3 (ru) |
| HR (1) | HRP20100032T1 (ru) |
| IL (1) | IL178125A (ru) |
| MA (1) | MA28515B1 (ru) |
| MX (1) | MXPA06011194A (ru) |
| NO (1) | NO332751B1 (ru) |
| NZ (1) | NZ549904A (ru) |
| PL (1) | PL1586319T3 (ru) |
| PT (1) | PT1586319E (ru) |
| RS (1) | RS51340B (ru) |
| RU (1) | RU2379300C2 (ru) |
| SI (1) | SI1586319T1 (ru) |
| TW (1) | TWI352084B (ru) |
| WO (1) | WO2005097117A1 (ru) |
| ZA (1) | ZA200608221B (ru) |
Families Citing this family (62)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR0110734A (pt) | 2000-05-11 | 2003-02-04 | Consejo Superior Investigacion | Inibidores heterocìclicos de cinase de sintase de glicogênio 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 |
| NZ574619A (en) * | 2006-07-18 | 2012-03-30 | Univ Rochester | THIADIAZOLIDINEDIONE DERIVATIVES including 4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione (TDZD-8) |
| WO2008012031A2 (en) * | 2006-07-25 | 2008-01-31 | Universität Bern | Blockers of gsk3 for the prevention and treatment of pemphigus vulgaris |
| AU2007283113A1 (en) | 2006-08-08 | 2008-02-14 | Sanofi-Aventis | Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, processes for preparing them, medicaments comprising these compounds, and their use |
| MX2009004140A (es) | 2006-10-21 | 2009-07-10 | Abbott Gmbh & Co Kg | Compuestos heterociclicos y su uso como inhibidores de la glucogeno sintasa quinasa 3. |
| 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 |
| EP2242745A1 (de) * | 2008-02-07 | 2010-10-27 | Sanofi-Aventis | Neue phenyl-substituierte imidazolidine, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| EP2310372B1 (en) | 2008-07-09 | 2012-05-23 | Sanofi | Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof |
| 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 |
| ES2443016T3 (es) | 2009-08-26 | 2014-02-17 | Sanofi | Nuevos hidratos cristalinos de fluoroglicósidos heteroaromáticos, productos farmacéuticos que comprenden estos compuestos, y su empleo |
| 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 |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, 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 |
| WO2012041814A1 (en) | 2010-09-27 | 2012-04-05 | Abbott Gmbh & Co. Kg | Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors |
| WO2012065065A1 (en) * | 2010-11-12 | 2012-05-18 | Follica, Inc. | Methods and compositions for modulating hair growth, wound healing and scar revision |
| WO2012078649A1 (en) | 2010-12-06 | 2012-06-14 | Follica, Inc. | Methods for treating baldness and promoting hair growth |
| US9090592B2 (en) | 2010-12-30 | 2015-07-28 | AbbVie Deutschland GmbH & Co. KG | Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors |
| US8809324B2 (en) | 2011-03-08 | 2014-08-19 | Sanofi | Substituted phenyl-oxathiazine derivatives, method for producing them, drugs containing said compounds and the use thereof |
| EP2683705B1 (de) | 2011-03-08 | 2015-04-22 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| EP2683700B1 (de) | 2011-03-08 | 2015-02-18 | Sanofi | Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| WO2012120057A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| EP2766349B1 (de) | 2011-03-08 | 2016-06-01 | Sanofi | Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| EP2683699B1 (de) | 2011-03-08 | 2015-06-24 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| US8846666B2 (en) | 2011-03-08 | 2014-09-30 | Sanofi | Oxathiazine derivatives which are substituted with benzyl or heteromethylene groups, method for producing them, their use as medicine and drug containing said derivatives and the use thereof |
| US8828995B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
| US8809325B2 (en) | 2011-03-08 | 2014-08-19 | Sanofi | Benzyl-oxathiazine derivatives substituted with adamantane and noradamantane, medicaments containing said compounds and use thereof |
| 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 |
| RU2509155C1 (ru) * | 2012-10-25 | 2014-03-10 | Федеральное государственное бюджетное учреждение науки Институт биохимии им. А.Н. Баха Российской академии наук | Способ детекции белков в амилоидном состоянии и набор для детекции белков в амилоидном состоянии |
| 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 |
| WO2015075051A1 (en) | 2013-11-19 | 2015-05-28 | Universitaet Des Saarlandes | Allosteric inhibitors of atypical protein kinases c |
| US20170165230A1 (en) | 2014-04-09 | 2017-06-15 | Christopher Rudd | Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity |
| ES2960601T3 (es) | 2014-06-12 | 2024-03-05 | Cedars Sinai Medical Center | Composiciones y métodos para el tratamiento del cáncer |
| 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抑制剂在调节精子运动能力中的用途 |
| CA3017341A1 (en) * | 2016-03-10 | 2017-09-14 | Alma Mater Studiorum - Universita Di Bologna | Treatment of cdkl5 disorders with gsk3.beta. inhibitor tideglusib |
| GB201617820D0 (en) * | 2016-10-21 | 2016-12-07 | King S College London | Dental treatment |
| WO2018226721A1 (en) * | 2017-06-06 | 2018-12-13 | The J. David Gladstone Institutes | Compositions and methods for reactivating latent immunodeficiency virus using a gsk-3 inhibitor |
| US20230218644A1 (en) | 2020-04-16 | 2023-07-13 | Som Innovation Biotech, S.A. | Compounds for use in the treatment of viral infections by respiratory syndrome-related coronavirus |
| CN113827592B (zh) * | 2020-06-24 | 2024-06-18 | 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 |
| JP2024508732A (ja) * | 2021-02-11 | 2024-02-28 | ベンカ リサーチ，インコーポレイティド | 不整脈原性心筋症を治療するための組成物および方法 |
| US20240173304A1 (en) | 2021-02-24 | 2024-05-30 | Teva Pharmaceuticals International Gmbh | Solid state forms of tideglusib and process for preparation thereof |
| CA3219537A1 (en) | 2021-05-21 | 2022-11-24 | Michael Snape | Method of treating rna repeat mediated diseases with rna repeat binding compound |
| EP4094760A1 (en) | 2021-05-24 | 2022-11-30 | Consejo Superior De Investigaciones Científicas | Thiadiazolidinones for their use in the treatment of limb-girdle muscular dystrophy |
| CN115197167B (zh) * | 2022-07-22 | 2023-07-28 | 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 |
| CN117986202B (zh) * | 2024-04-03 | 2024-06-14 | 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 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR0110734A (pt) * | 2000-05-11 | 2003-02-04 | Consejo Superior Investigacion | Inibidores heterocìclicos de cinase de sintase de glicogênio gsk-3 |
| ES2166328B1 (es) * | 2000-05-11 | 2003-09-16 | Consejo Superior Investigacion | Inhibidores heterociclicos del enzima gsk 3 utiles en el tratamiento de procesos neurodegenerativos e hiperproliferativos |
| EP1586318A1 (en) * | 2004-04-05 | 2005-10-19 | Neuropharma S.A.U. | Thiadiazolidinones as GSK-3 inhibitors |
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2004
- 2004-04-05 EP EP04075997A patent/EP1586318A1/en not_active Withdrawn
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- 2005-04-01 AR ARP050101293A patent/AR048820A1/es not_active Application Discontinuation
- 2005-04-04 SI SI200530879T patent/SI1586319T1/sl unknown
- 2005-04-04 RS RSP-2010/0017A patent/RS51340B/sr unknown
- 2005-04-04 AU AU2005230392A patent/AU2005230392B2/en not_active Expired
- 2005-04-04 ES ES05075779T patent/ES2335505T3/es not_active Expired - Lifetime
- 2005-04-04 EP EP05075779A patent/EP1586319B1/en not_active Expired - Lifetime
- 2005-04-04 PT PT05075779T patent/PT1586319E/pt unknown
- 2005-04-04 CN CN2005800121414A patent/CN1946398B/zh not_active Expired - Lifetime
- 2005-04-04 DK DK05075779.8T patent/DK1586319T3/da active
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- 2005-04-04 BR BRPI0508788-0A patent/BRPI0508788A/pt not_active IP Right Cessation
- 2005-04-04 WO PCT/EP2005/003613 patent/WO2005097117A1/en not_active Ceased
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- 2005-04-04 PL PL05075779T patent/PL1586319T3/pl unknown
- 2005-04-04 RU RU2006139030/04A patent/RU2379300C2/ru active
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- 2006-10-02 NO NO20064456A patent/NO332751B1/no unknown
- 2006-10-11 KR KR1020067021121A patent/KR101151647B1/ko not_active Expired - Lifetime
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- 2009-04-22 US US12/428,442 patent/US8158661B2/en not_active Expired - Lifetime
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