EA201200975A1 - Тиено[2,3-b]пиридиндионовые активаторы амфк и их терапевтическое применение - Google Patents
Тиено[2,3-b]пиридиндионовые активаторы амфк и их терапевтическое применениеInfo
- Publication number
- EA201200975A1 EA201200975A1 EA201200975A EA201200975A EA201200975A1 EA 201200975 A1 EA201200975 A1 EA 201200975A1 EA 201200975 A EA201200975 A EA 201200975A EA 201200975 A EA201200975 A EA 201200975A EA 201200975 A1 EA201200975 A1 EA 201200975A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- activators
- pyridinion
- amphic
- tieno
- therapeutic application
- Prior art date
Links
- 239000012190 activator Substances 0.000 title abstract 2
- 230000001225 therapeutic effect Effects 0.000 title 1
- 102000014156 AMP-Activated Protein Kinases Human genes 0.000 abstract 3
- 108010011376 AMP-Activated Protein Kinases Proteins 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 208000001145 Metabolic Syndrome Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 230000001105 regulatory effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4365—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Child & Adolescent Psychology (AREA)
- Epidemiology (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Изобретение относится к соединениям, которые являются прямыми активаторами АМФК (АМФ-активируемая протеинкиназа), и их применению в лечении нарушений, регулируемых путем активации АМФК. Например, соединения по изобретению являются пригодными для лечения диабетов, метаболического синдрома, ожирения, воспаления, рака и сердечно-сосудистых заболеваний.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09306344 | 2009-12-29 | ||
| PCT/EP2010/070811 WO2011080277A1 (en) | 2009-12-29 | 2010-12-28 | Thieno [2,3-b] pyridinedione activators of ampk and therapeutic uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201200975A1 true EA201200975A1 (ru) | 2012-12-28 |
| EA020588B1 EA020588B1 (ru) | 2014-12-30 |
Family
ID=41691577
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201200975A EA020588B1 (ru) | 2009-12-29 | 2010-12-28 | ТИЕНО[2,3-b]ПИРИДИНДИОНОВЫЕ АКТИВАТОРЫ АМФК И ИХ ТЕРАПЕВТИЧЕСКОЕ ПРИМЕНЕНИЕ |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US9365584B2 (ru) |
| EP (1) | EP2519527B1 (ru) |
| JP (1) | JP5559894B2 (ru) |
| KR (1) | KR101469002B1 (ru) |
| CN (1) | CN102803269B (ru) |
| AU (1) | AU2010338280B2 (ru) |
| BR (1) | BR112012016330B8 (ru) |
| CA (1) | CA2784553C (ru) |
| CY (1) | CY1114952T1 (ru) |
| DK (1) | DK2519527T3 (ru) |
| EA (1) | EA020588B1 (ru) |
| ES (1) | ES2445537T3 (ru) |
| HR (1) | HRP20140035T1 (ru) |
| IL (1) | IL220432A (ru) |
| ME (1) | ME01558B (ru) |
| MX (1) | MX2012007548A (ru) |
| PL (1) | PL2519527T3 (ru) |
| PT (1) | PT2519527E (ru) |
| RS (1) | RS53282B (ru) |
| SI (1) | SI2519527T1 (ru) |
| SM (1) | SMT201400013B (ru) |
| TW (1) | TWI574968B (ru) |
| WO (1) | WO2011080277A1 (ru) |
| ZA (1) | ZA201205604B (ru) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LT3329919T (lt) | 2011-11-11 | 2020-02-10 | Gilead Apollo, Llc | Acc inhibitoriai ir jų panaudojimas |
| US8889730B2 (en) | 2012-04-10 | 2014-11-18 | Pfizer Inc. | Indole and indazole compounds that activate AMPK |
| CA2905242C (en) | 2013-03-15 | 2016-11-29 | Pfizer Inc. | Indole compounds that activate ampk |
| US10143703B2 (en) | 2014-01-02 | 2018-12-04 | Massachusetts Eye And Ear Infirmary | Treating ocular neovascularization |
| WO2017011917A1 (en) * | 2015-07-23 | 2017-01-26 | Thrasos Therapeutics Inc. | Methods for treating and preventing polycystic kidney diseases (pkd) using amp-activated protein kinase (ampk) modulators and activators |
| AR106472A1 (es) | 2015-10-26 | 2018-01-17 | Gilead Apollo Llc | Inhibidores de acc y usos de los mismos |
| EA201890949A1 (ru) | 2015-11-25 | 2018-12-28 | Джилид Аполло, Ллс | СЛОЖНОЭФИРНЫЕ ИНГИБИТОРЫ АЦЕТИЛ-КоА-КАРБОКСИЛАЗЫ И ВАРИАНТЫ ИХ ПРИМЕНЕНИЯ |
| BR112018010453B1 (pt) | 2015-11-25 | 2022-06-14 | Gilead Apollo, Llc | Compostos triazólicos inibindores de acetil coa carboxilase (acc) |
| EA201890910A1 (ru) | 2015-11-25 | 2018-11-30 | Джилид Аполло, Ллс | ФУНГИЦИДНЫЕ КОМПОЗИЦИИ, СОДЕРЖАЩИЕ ПРОИЗВОДНЫЕ 2,4-ДИОКСО-1,4-ДИГИДРОТИЕНО[2,3-d]ПИРИМИДИНА |
| JP2019502660A (ja) | 2015-11-25 | 2019-01-31 | ギリアド アポロ, エルエルシー | ピラゾールacc阻害剤およびその使用 |
| TWI844474B (zh) | 2016-03-02 | 2024-06-01 | 美商基利阿波羅有限責任公司 | 噻吩并嘧啶二酮acc抑制劑之固體型式及其製造方法 |
| US10793527B2 (en) | 2016-09-07 | 2020-10-06 | National Yang-Ming University | Adenosine monophosphate-activated protein kinase agonist |
| EP4424364A3 (en) | 2017-03-28 | 2024-11-27 | Gilead Sciences, Inc. | Methods of treating liver disease |
| WO2019185413A1 (en) | 2018-03-27 | 2019-10-03 | Basf Se | Pesticidal substituted cyclopropyl derivatives |
| JP2023526625A (ja) | 2020-05-19 | 2023-06-22 | キャリーオペ,インク. | Ampkアクチベーター |
| CN116390925A (zh) | 2020-06-26 | 2023-07-04 | 卡尔优普公司 | Ampk活化剂 |
| EP4221700A1 (en) | 2020-09-30 | 2023-08-09 | Bioverativ Therapeutics Inc. | Ampk activators and methods of use thereof |
| US12404348B2 (en) | 2021-11-19 | 2025-09-02 | The Brigham And Women's Hospital, Inc. | Bifunctional chimeric molecules for labeling of kinases with target binding moieties and methods of use thereof |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7119205B2 (en) | 2003-05-16 | 2006-10-10 | Abbott Laboratories | Thienopyridones as AMPK activators for the treatment of diabetes and obesity |
| MX2010011047A (es) * | 2008-04-11 | 2010-10-26 | Merck Patent Gmbh | Derivados de tienopiridonas como activadores de proteina cinasa activada por amp (ampk). |
-
2010
- 2010-12-28 EA EA201200975A patent/EA020588B1/ru not_active IP Right Cessation
- 2010-12-28 DK DK10800766.7T patent/DK2519527T3/da active
- 2010-12-28 KR KR1020127018478A patent/KR101469002B1/ko not_active Expired - Fee Related
- 2010-12-28 CN CN201080064452.6A patent/CN102803269B/zh not_active Expired - Fee Related
- 2010-12-28 MX MX2012007548A patent/MX2012007548A/es active IP Right Grant
- 2010-12-28 JP JP2012546437A patent/JP5559894B2/ja not_active Expired - Fee Related
- 2010-12-28 ME MEP-2014-10A patent/ME01558B/me unknown
- 2010-12-28 AU AU2010338280A patent/AU2010338280B2/en not_active Ceased
- 2010-12-28 RS RS20140028A patent/RS53282B/sr unknown
- 2010-12-28 CA CA2784553A patent/CA2784553C/en not_active Expired - Fee Related
- 2010-12-28 PT PT108007667T patent/PT2519527E/pt unknown
- 2010-12-28 ES ES10800766.7T patent/ES2445537T3/es active Active
- 2010-12-28 US US13/519,407 patent/US9365584B2/en not_active Expired - Fee Related
- 2010-12-28 PL PL10800766T patent/PL2519527T3/pl unknown
- 2010-12-28 EP EP10800766.7A patent/EP2519527B1/en active Active
- 2010-12-28 HR HRP20140035AT patent/HRP20140035T1/hr unknown
- 2010-12-28 TW TW099146432A patent/TWI574968B/zh not_active IP Right Cessation
- 2010-12-28 WO PCT/EP2010/070811 patent/WO2011080277A1/en not_active Ceased
- 2010-12-28 SI SI201030501T patent/SI2519527T1/sl unknown
- 2010-12-28 BR BR112012016330A patent/BR112012016330B8/pt not_active IP Right Cessation
-
2012
- 2012-06-14 IL IL220432A patent/IL220432A/en active IP Right Grant
- 2012-07-25 ZA ZA2012/05604A patent/ZA201205604B/en unknown
-
2014
- 2014-01-24 CY CY20141100066T patent/CY1114952T1/el unknown
- 2014-01-29 SM SM201400013T patent/SMT201400013B/xx unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM |