UA109927C2 - Конденсированные производные аминодигидротиазина, полезные как ингибиторы васе - Google Patents
Конденсированные производные аминодигидротиазина, полезные как ингибиторы васеInfo
- Publication number
- UA109927C2 UA109927C2 UAA201310161A UAA201310161A UA109927C2 UA 109927 C2 UA109927 C2 UA 109927C2 UA A201310161 A UAA201310161 A UA A201310161A UA A201310161 A UAA201310161 A UA A201310161A UA 109927 C2 UA109927 C2 UA 109927C2
- Authority
- UA
- Ukraine
- Prior art keywords
- derivatives useful
- fused aminodihydrothiazine
- bace inhibitors
- inhibitory effect
- aminodihydrothiazine derivatives
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
-
- 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
- A61P25/28—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
- 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
- A61P3/08—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Это изобретение касается конденсированного производного аминдигидротиазина формулы (I): EMBED ISISServer , (I) где X - водород или фтор; А - СН или N; Υ - метил, этил, монофторметил, дифторметил, трифторметил, дифторетил, метокси, этокси, метоксиметил или -C=N; и его фармацевтически приемлемых солей; причем это соединение имеет ингибирующее действие на выработку Αβ или на ВАСЕ1 и служит средством для профилактики или лечения нейродегенеративной болезни, вызванной Αβ, типичным проявлением которой является деменция типа Альцгеймера.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB1101140.0A GB201101140D0 (en) | 2011-01-21 | 2011-01-21 | Fused aminodihydrothiazine derivatives |
PCT/EP2012/050833 WO2012098213A1 (en) | 2011-01-21 | 2012-01-20 | Fused aminodihydrothiazine derivatives useful as bace inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
UA109927C2 true UA109927C2 (ru) | 2015-10-26 |
Family
ID=43769479
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
UAA201310161A UA109927C2 (ru) | 2011-01-21 | 2012-01-20 | Конденсированные производные аминодигидротиазина, полезные как ингибиторы васе |
Country Status (21)
Country | Link |
---|---|
US (3) | US8338407B2 (ru) |
EP (1) | EP2665732B1 (ru) |
JP (1) | JP5947815B2 (ru) |
KR (1) | KR101906466B1 (ru) |
CN (1) | CN103328486B (ru) |
AR (1) | AR084903A1 (ru) |
AU (1) | AU2012208526B2 (ru) |
BR (1) | BR112013018602A2 (ru) |
CA (1) | CA2828738A1 (ru) |
CL (1) | CL2013002083A1 (ru) |
ES (1) | ES2575914T3 (ru) |
GB (1) | GB201101140D0 (ru) |
IL (1) | IL226596A (ru) |
MX (1) | MX2013007917A (ru) |
PE (1) | PE20141182A1 (ru) |
RU (1) | RU2593756C2 (ru) |
SG (1) | SG190908A1 (ru) |
TW (1) | TW201309710A (ru) |
UA (1) | UA109927C2 (ru) |
WO (1) | WO2012098213A1 (ru) |
ZA (1) | ZA201303801B (ru) |
Families Citing this family (40)
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EP1942105B8 (en) | 2005-10-25 | 2014-08-13 | Shionogi&Co., Ltd. | Aminodihydrothiazine derivative |
KR20100017255A (ko) | 2007-04-24 | 2010-02-16 | 시오노기 앤드 컴파니, 리미티드 | 환식기로 치환된 아미노다이하이드로싸이아진 유도체 |
US8653067B2 (en) | 2007-04-24 | 2014-02-18 | Shionogi & Co., Ltd. | Pharmaceutical composition for treating Alzheimer's disease |
KR101564634B1 (ko) | 2008-01-18 | 2015-10-30 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 축합 아미노디하이드로 티아진 유도체 |
US8637504B2 (en) | 2008-06-13 | 2014-01-28 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity |
EP2360155A4 (en) | 2008-10-22 | 2012-06-20 | Shionogi & Co | 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT |
GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
WO2011044185A2 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
EP2485591B1 (en) | 2009-10-08 | 2016-03-23 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
RU2012129168A (ru) | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
JP5766198B2 (ja) | 2010-10-29 | 2015-08-19 | 塩野義製薬株式会社 | 縮合アミノジヒドロピリミジン誘導体 |
CA2816285A1 (en) | 2010-10-29 | 2012-05-03 | Shionogi & Co., Ltd. | Naphthyridine derivative |
GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
SG10201601516QA (en) | 2011-01-21 | 2016-03-30 | Eisai R&D Man Co Ltd | Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives |
GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
CN103608345A (zh) | 2011-04-26 | 2014-02-26 | 盐野义制药株式会社 | 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂 |
EP2763676B1 (en) * | 2011-10-03 | 2019-12-25 | The University of Utah Research Foundation | Application of 5-ht6 receptor antagonists for the alleviation of cognitive deficits of down syndrome |
WO2014015125A1 (en) | 2012-07-19 | 2014-01-23 | Eisai R&D Management Co., Ltd. | Fused aminodihydrothiazine derivative salts and uses thereof |
GB201212816D0 (en) * | 2012-07-19 | 2012-09-05 | Eisai Ltd | Novel compounds |
EP2893042B1 (en) * | 2012-09-05 | 2018-02-14 | Emory University | Diagnostic testing in dementia and methods related thereto |
WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
TWI593692B (zh) * | 2013-03-12 | 2017-08-01 | 美國禮來大藥廠 | 四氫吡咯并噻嗪化合物 |
JO3318B1 (ar) | 2013-06-18 | 2019-03-13 | Lilly Co Eli | مثبطات bace |
TWI599358B (zh) * | 2014-09-16 | 2017-09-21 | 美國禮來大藥廠 | 組合療法 |
AR103680A1 (es) * | 2015-02-23 | 2017-05-24 | Lilly Co Eli | Inhibidores selectivos de bace1 |
EP3271356B1 (en) * | 2015-03-19 | 2019-10-16 | Eli Lilly and Company | Selective bace1 inhibitors |
AR104241A1 (es) * | 2015-04-29 | 2017-07-05 | Lilly Co Eli | Derivados de tetrahidrofuro tiazina como inhibidores de bace1 selectivos |
TW201740954A (zh) * | 2016-03-16 | 2017-12-01 | 美國禮來大藥廠 | 組合療法 |
KR20170108203A (ko) * | 2016-03-16 | 2017-09-27 | 주식회사 피플바이오 | 응집형-형성 폴리펩타이드의 응집형을 검출하는 방법 |
TWI675034B (zh) * | 2016-05-20 | 2019-10-21 | 美商美國禮來大藥廠 | 四氫呋喃并<img align="absmiddle" height="18px" width="27px" file="d10999.TIF" alt="其他非圖式 ed10999.png" img-content="tif" orientation="portrait" inline="yes" giffile="ed10999.png"></img>化合物及其作為選擇性BACE1抑制劑之用途 |
WO2018034977A1 (en) * | 2016-08-18 | 2018-02-22 | Eli Lilly And Company | Combination therapy of bace-1 inhibitor and anti-n3pglu abeta antibody |
AR110470A1 (es) * | 2016-10-21 | 2019-04-03 | Lilly Co Eli | Terapia de combinación para tratar la enfermedad de alzheimer |
EP3555085B1 (en) | 2016-12-15 | 2020-12-02 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
EP3555106B1 (en) * | 2016-12-15 | 2022-03-09 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
WO2018112081A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Oxazine derivatives as beta-secretase inhibitors and methods of use |
CA3047288A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Thiazine derivatives as beta-secretase inhibitors and methods of use |
US11021493B2 (en) | 2016-12-15 | 2021-06-01 | Amgen Inc. | 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use |
CN116143621A (zh) * | 2022-12-14 | 2023-05-23 | 湖南农业大学 | 一种硼盐催化激活酰胺用于制备苯甲酸酯类化合物的方法 |
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KR20100017255A (ko) | 2007-04-24 | 2010-02-16 | 시오노기 앤드 컴파니, 리미티드 | 환식기로 치환된 아미노다이하이드로싸이아진 유도체 |
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GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
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GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
SG10201601516QA (en) | 2011-01-21 | 2016-03-30 | Eisai R&D Man Co Ltd | Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives |
-
2011
- 2011-01-21 GB GBGB1101140.0A patent/GB201101140D0/en not_active Ceased
-
2012
- 2012-01-10 TW TW101100946A patent/TW201309710A/zh unknown
- 2012-01-20 WO PCT/EP2012/050833 patent/WO2012098213A1/en active Application Filing
- 2012-01-20 US US13/354,716 patent/US8338407B2/en not_active Expired - Fee Related
- 2012-01-20 KR KR1020137019966A patent/KR101906466B1/ko active IP Right Grant
- 2012-01-20 RU RU2013138717/04A patent/RU2593756C2/ru not_active IP Right Cessation
- 2012-01-20 BR BR112013018602-0A patent/BR112013018602A2/pt not_active IP Right Cessation
- 2012-01-20 PE PE2013001464A patent/PE20141182A1/es not_active Application Discontinuation
- 2012-01-20 ES ES12708716.1T patent/ES2575914T3/es active Active
- 2012-01-20 JP JP2013549820A patent/JP5947815B2/ja not_active Expired - Fee Related
- 2012-01-20 CA CA2828738A patent/CA2828738A1/en not_active Abandoned
- 2012-01-20 UA UAA201310161A patent/UA109927C2/ru unknown
- 2012-01-20 CN CN201280004902.1A patent/CN103328486B/zh not_active Expired - Fee Related
- 2012-01-20 EP EP12708716.1A patent/EP2665732B1/en not_active Revoked
- 2012-01-20 AU AU2012208526A patent/AU2012208526B2/en not_active Ceased
- 2012-01-20 SG SG2013041033A patent/SG190908A1/en unknown
- 2012-01-20 MX MX2013007917A patent/MX2013007917A/es active IP Right Grant
- 2012-01-20 AR ARP120100191A patent/AR084903A1/es unknown
- 2012-11-26 US US13/685,109 patent/US8592408B2/en not_active Expired - Fee Related
-
2013
- 2013-05-24 ZA ZA2013/03801A patent/ZA201303801B/en unknown
- 2013-05-27 IL IL226596A patent/IL226596A/en active IP Right Grant
- 2013-07-19 CL CL2013002083A patent/CL2013002083A1/es unknown
- 2013-10-18 US US14/057,403 patent/US8940734B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
ZA201303801B (en) | 2014-07-30 |
CN103328486B (zh) | 2016-08-17 |
CN103328486A (zh) | 2013-09-25 |
JP5947815B2 (ja) | 2016-07-06 |
NZ611365A (en) | 2015-04-24 |
EP2665732B1 (en) | 2016-03-30 |
GB201101140D0 (en) | 2011-03-09 |
KR20140002724A (ko) | 2014-01-08 |
US8592408B2 (en) | 2013-11-26 |
WO2012098213A1 (en) | 2012-07-26 |
US8940734B2 (en) | 2015-01-27 |
PE20141182A1 (es) | 2014-09-14 |
KR101906466B1 (ko) | 2018-10-10 |
JP2014502987A (ja) | 2014-02-06 |
AU2012208526B2 (en) | 2015-09-24 |
AR084903A1 (es) | 2013-07-10 |
AU2012208526A1 (en) | 2013-05-02 |
TW201309710A (zh) | 2013-03-01 |
US8338407B2 (en) | 2012-12-25 |
SG190908A1 (en) | 2013-07-31 |
EP2665732A1 (en) | 2013-11-27 |
US20120190672A1 (en) | 2012-07-26 |
ES2575914T3 (es) | 2016-07-04 |
US20130203740A1 (en) | 2013-08-08 |
US20140142091A1 (en) | 2014-05-22 |
CL2013002083A1 (es) | 2013-12-06 |
BR112013018602A2 (pt) | 2020-09-01 |
CA2828738A1 (en) | 2012-07-26 |
RU2013138717A (ru) | 2015-02-27 |
MX2013007917A (es) | 2013-08-29 |
IL226596A (en) | 2016-04-21 |
RU2593756C2 (ru) | 2016-08-10 |
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