PE20141182A1 - Derivados fusionados de aminodihidrotiazina - Google Patents
Derivados fusionados de aminodihidrotiazinaInfo
- Publication number
- PE20141182A1 PE20141182A1 PE2013001464A PE2013001464A PE20141182A1 PE 20141182 A1 PE20141182 A1 PE 20141182A1 PE 2013001464 A PE2013001464 A PE 2013001464A PE 2013001464 A PE2013001464 A PE 2013001464A PE 20141182 A1 PE20141182 A1 PE 20141182A1
- Authority
- PE
- Peru
- Prior art keywords
- thiazin
- furo
- fluorophenyl
- tetrahydro
- amino
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- WZKSXHQDXQKIQJ-UHFFFAOYSA-N F[C](F)F Chemical group F[C](F)F WZKSXHQDXQKIQJ-UHFFFAOYSA-N 0.000 abstract 1
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- -1 MONOFLUOROMETHYL Chemical class 0.000 abstract 1
- QUPDWYMUPZLYJZ-UHFFFAOYSA-N ethyl Chemical class C[CH2] QUPDWYMUPZLYJZ-UHFFFAOYSA-N 0.000 abstract 1
- 235000013312 flour Nutrition 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- IXHBTMCLRNMKHZ-LBPRGKRZSA-N levobunolol Chemical compound O=C1CCCC2=C1C=CC=C2OC[C@@H](O)CNC(C)(C)C IXHBTMCLRNMKHZ-LBPRGKRZSA-N 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 239000002243 precursor Substances 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (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
REFERIDO A UN COMPUESTO DE FORMULA (I) O UNA SAL FARMACEUTICAMENTE ACEPTABLE DEL MISMO EN DONDE: X ES HIDROGENO, FLOUR; A ES CH O N, Y ES METILO, ETILO, MONOFLUOROMETILO, ENTRE OTROS. DICHO COMPUESTO TIENE UN EFECTO INHIBIDOR DE LA ENZIMA 1 DE ESCISION DE LA PROTEINA PRECURSORA DE ?-ALMILOIDE DE SITIO BETA (BACE1). SON COMPUESTOS PREFERIDOS N-(3-((4AS,5S,7AS)-2-AMINO-5-(TRIFLUOROMETIL)-4A,5,7,7 A -TETRAHIDRO-4H-FURO[3,4-D][1,3]TIAZIN-7 A -IL)-4-FLUOROFENIL)-5-METOXIPIRAZINA-2-CARBOXAMIDA, N-(3-((4AS,5S,7AS)-2-AMINO-5-(TRIFLUOROMETIL)-4 A, 5,7,7 A-TETRAHIDRO-4H-FURO[3,4-D][1,3]TIAZIN-7 A-IL)-4-FLUOROFENIL-5-CIANOPICOLINAMIDA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA QUE ES UTIL PARA EL TRATAMIENTO DE UNA ENFERMEDAD NEURODEGENERATIVA.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1101140.0A GB201101140D0 (en) | 2011-01-21 | 2011-01-21 | Fused aminodihydrothiazine derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20141182A1 true PE20141182A1 (es) | 2014-09-14 |
Family
ID=43769479
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2013001464A PE20141182A1 (es) | 2011-01-21 | 2012-01-20 | Derivados fusionados de aminodihidrotiazina |
Country Status (22)
| Country | Link |
|---|---|
| US (3) | US8338407B2 (es) |
| EP (1) | EP2665732B1 (es) |
| JP (1) | JP5947815B2 (es) |
| KR (1) | KR101906466B1 (es) |
| CN (1) | CN103328486B (es) |
| AR (1) | AR084903A1 (es) |
| AU (1) | AU2012208526B2 (es) |
| BR (1) | BR112013018602A2 (es) |
| CA (1) | CA2828738A1 (es) |
| CL (1) | CL2013002083A1 (es) |
| ES (1) | ES2575914T3 (es) |
| GB (1) | GB201101140D0 (es) |
| IL (1) | IL226596A (es) |
| MX (1) | MX2013007917A (es) |
| PE (1) | PE20141182A1 (es) |
| PH (1) | PH12013501085A1 (es) |
| RU (1) | RU2593756C2 (es) |
| SG (1) | SG190908A1 (es) |
| TW (1) | TW201309710A (es) |
| UA (1) | UA109927C2 (es) |
| WO (1) | WO2012098213A1 (es) |
| ZA (1) | ZA201303801B (es) |
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| KR20100017255A (ko) | 2007-04-24 | 2010-02-16 | 시오노기 앤드 컴파니, 리미티드 | 환식기로 치환된 아미노다이하이드로싸이아진 유도체 |
| EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| SI2233474T1 (sl) | 2008-01-18 | 2015-11-30 | Eisai R&D Management Co., Ltd. | Kondenziran derivat aminodihidrotiazina |
| EP2305672B1 (en) | 2008-06-13 | 2019-03-27 | Shionogi & Co., Ltd. | SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY |
| CN102186841A (zh) | 2008-10-22 | 2011-09-14 | 盐野义制药株式会社 | 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物 |
| 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 |
| EP2485920B1 (en) | 2009-10-08 | 2016-04-27 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| WO2011044187A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | 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 |
| CN103261199A (zh) | 2010-10-29 | 2013-08-21 | 盐野义制药株式会社 | 萘啶衍生物 |
| 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 |
| ES2624288T3 (es) | 2011-01-21 | 2017-07-13 | Eisai R&D Management Co., Ltd. | Métodos y compuestos útiles en la síntesis de derivados de aminodihidrotiazina condensados |
| GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| WO2012147763A1 (ja) | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | オキサジン誘導体およびそれを含有するｂａｃｅ１阻害剤 |
| 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 |
| US9618522B2 (en) * | 2012-09-05 | 2017-04-11 | Emory University | Diagnostic testing in dementia and methods related thereto |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING 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 |
| CN107257795A (zh) * | 2015-03-19 | 2017-10-17 | 伊莱利利公司 | 选择性bace1抑制剂 |
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| AR107774A1 (es) * | 2016-03-16 | 2018-05-30 | Lilly Co Eli | Terapia de combinación, método para el tratamiento de la enfermedad de alzheimer |
| 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 |
| JP2019530647A (ja) * | 2016-08-18 | 2019-10-24 | イーライ リリー アンド カンパニー | Ｂａｃｅ−１阻害剤と抗ｎ３ｐｇｌｕ ａベータ抗体の併用療法 |
| TWI669119B (zh) | 2016-10-21 | 2019-08-21 | 美國禮來大藥廠 | 組合療法 |
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| 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 |
| ES2624288T3 (es) | 2011-01-21 | 2017-07-13 | Eisai R&D Management Co., Ltd. | Métodos y compuestos útiles en la síntesis de derivados de aminodihidrotiazina condensados |
-
2011
- 2011-01-21 GB GBGB1101140.0A patent/GB201101140D0/en not_active Ceased
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2012
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- 2012-01-20 ES ES12708716.1T patent/ES2575914T3/es active Active
- 2012-01-20 WO PCT/EP2012/050833 patent/WO2012098213A1/en not_active Ceased
- 2012-01-20 PE PE2013001464A patent/PE20141182A1/es not_active Application Discontinuation
- 2012-01-20 EP EP12708716.1A patent/EP2665732B1/en not_active Revoked
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