MX339640B - Derivados de 5, 6-dihidro-2h-[1, 4] oxazin-3-il-amina utiles como inhibidores de la beta-secretasa (bace). - Google Patents
Derivados de 5, 6-dihidro-2h-[1, 4] oxazin-3-il-amina utiles como inhibidores de la beta-secretasa (bace).Info
- Publication number
- MX339640B MX339640B MX2012014368A MX2012014368A MX339640B MX 339640 B MX339640 B MX 339640B MX 2012014368 A MX2012014368 A MX 2012014368A MX 2012014368 A MX2012014368 A MX 2012014368A MX 339640 B MX339640 B MX 339640B
- Authority
- MX
- Mexico
- Prior art keywords
- beta
- secretase
- bace
- oxazin
- dihydro
- Prior art date
Links
- COPFSXJBOSOUGF-UHFFFAOYSA-N 3,6-dihydro-2h-1,4-oxazin-5-amine Chemical class N=C1COCCN1 COPFSXJBOSOUGF-UHFFFAOYSA-N 0.000 title abstract 2
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 title abstract 2
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 title abstract 2
- 101150058765 BACE1 gene Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract 4
- 206010012289 Dementia Diseases 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 208000024827 Alzheimer disease Diseases 0.000 abstract 2
- 102000013455 Amyloid beta-Peptides Human genes 0.000 abstract 2
- 108010090849 Amyloid beta-Peptides Proteins 0.000 abstract 2
- 101710150192 Beta-secretase 1 Proteins 0.000 abstract 2
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 206010067889 Dementia with Lewy bodies Diseases 0.000 abstract 1
- 201000010374 Down Syndrome Diseases 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 201000002832 Lewy body dementia Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 206010039966 Senile dementia Diseases 0.000 abstract 1
- 239000002439 beta secretase inhibitor Substances 0.000 abstract 1
- 238000003776 cleavage reaction Methods 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 208000027061 mild cognitive impairment Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 230000007017 scission Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
-
- 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
- A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Biomedical Technology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invención se refiere a derivados novedosos de 5, 6-dihidro-2H-[1, 4]oxazin-3-ilamina como inhibidores de la beta-secretasa, conocida también como enzima de escisión amiloide del sitio beta, BACE, BACE1, Asp2 o memapsina2; la invención se refiere también a composiciones farmacéuticas que comprenden dichos compuestos, a procedimientos para la preparación de dichos compuestos y composiciones, y al uso de dichos compuestos y composiciones para la prevención y el tratamiento de trastornos en los cuales se encuentra involucrada la beta-secretasa, tales como en enfermedad de Alzheimer (EA), deterioro cognitivo leve, senilidad, demencia, demencia con cuerpos de Lewy, síndrome de Down, demencia asociada con el accidente cerebrovascular, demencia asociada con la enfermedad de Parkinson o demencia asociada con beta-amiloide.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10165335 | 2010-06-09 | ||
| EP11152314 | 2011-01-27 | ||
| EP11157765 | 2011-03-10 | ||
| EP11164999 | 2011-05-05 | ||
| PCT/EP2011/059441 WO2011154431A1 (en) | 2010-06-09 | 2011-06-08 | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2012014368A MX2012014368A (es) | 2013-01-22 |
| MX339640B true MX339640B (es) | 2016-06-01 |
Family
ID=44317911
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2012014368A MX339640B (es) | 2010-06-09 | 2011-06-08 | Derivados de 5, 6-dihidro-2h-[1, 4] oxazin-3-il-amina utiles como inhibidores de la beta-secretasa (bace). |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US20130109683A1 (es) |
| EP (1) | EP2580200B1 (es) |
| JP (1) | JP5711813B2 (es) |
| KR (1) | KR101730937B1 (es) |
| CN (1) | CN102933564B (es) |
| AR (1) | AR081587A1 (es) |
| AU (1) | AU2011263797B2 (es) |
| BR (1) | BR112012031094A2 (es) |
| CA (1) | CA2799640C (es) |
| CL (1) | CL2012003428A1 (es) |
| CO (1) | CO6602112A2 (es) |
| DK (1) | DK2580200T3 (es) |
| EA (1) | EA021240B1 (es) |
| ES (1) | ES2607083T3 (es) |
| IL (1) | IL223423A (es) |
| MX (1) | MX339640B (es) |
| NZ (1) | NZ603427A (es) |
| PH (1) | PH12012502377A1 (es) |
| SG (1) | SG185651A1 (es) |
| TW (1) | TWI537263B (es) |
| WO (1) | WO2011154431A1 (es) |
| ZA (1) | ZA201209297B (es) |
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| CN101346357B (zh) | 2005-10-25 | 2014-04-02 | 盐野义制药株式会社 | 氨基二氢噻嗪衍生物 |
| EP2689780A1 (en) | 2007-04-24 | 2014-01-29 | Shionogi & Co., Ltd. | Intermediates for aminodihydrothiazine derivatives substituted with a cyclic group |
| JP5383483B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | アルツハイマー症治療用医薬組成物 |
| KR101324426B1 (ko) | 2008-06-13 | 2013-10-31 | 시오노기세야쿠 가부시키가이샤 | β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체 |
| 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 |
| UY32799A (es) | 2009-07-24 | 2011-02-28 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos |
| US8557826B2 (en) | 2009-10-08 | 2013-10-15 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions, and their use |
| EP2485920B1 (en) | 2009-10-08 | 2016-04-27 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| EP2485591B1 (en) | 2009-10-08 | 2016-03-23 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| KR20120104570A (ko) | 2009-12-11 | 2012-09-21 | 시오노기세야쿠 가부시키가이샤 | 옥사진 유도체 |
| KR101730937B1 (ko) | 2010-06-09 | 2017-04-27 | 얀센 파마슈티카 엔.브이. | 베타-세크레타아제(bace) 저해제로 유용한 5,6-디하이드로-2h-[1,4]옥사진-3-일-아민 유도체 |
| EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
| CN103261199A (zh) | 2010-10-29 | 2013-08-21 | 盐野义制药株式会社 | 萘啶衍生物 |
| BR112013015430A2 (pt) | 2010-12-22 | 2016-09-20 | Janssen Pharmaceutica Nv | derivados de 5,6-diidro-imidazo[1,2-a]pirazin-8-ilamina úteis como inibidores de beta-secretase (bace) |
| US8524897B2 (en) | 2011-01-12 | 2013-09-03 | Novartis Ag | Crystalline oxazine derivative |
| DK2663561T3 (en) | 2011-01-13 | 2016-06-06 | Novartis Ag | New heterocyclic derivatives and their use in treating neurological disorders |
| US8399459B2 (en) * | 2011-02-02 | 2013-03-19 | Hoffmann-La Roche Inc. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| CN103415519B (zh) * | 2011-03-01 | 2016-03-02 | 詹森药业有限公司 | 作为β-分泌酶(BACE)抑制剂有用的6,7-二氢-吡唑[1,5-a]吡嗪-4-基胺衍生物 |
| PH12013501805A1 (en) | 2011-03-09 | 2013-11-18 | Janssen Pharmaceutica Nv | 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
| US8877744B2 (en) * | 2011-04-04 | 2014-11-04 | Hoffmann-La Roche Inc. | 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors |
| US9145426B2 (en) | 2011-04-07 | 2015-09-29 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
| EP2694489B1 (en) | 2011-04-07 | 2017-09-06 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| RU2013150349A (ru) | 2011-04-13 | 2015-05-20 | Мерк Шарп И Доум Корп. | 5-замещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов васе, содержащие их композиции и их применение |
| 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 |
| US20140235626A1 (en) | 2011-04-26 | 2014-08-21 | Shionogi & Co., Ltd. | Pyridine derivatives and a pharmaceutical composition for inhibiting bace1 containing them |
| AU2012266544A1 (en) | 2011-06-07 | 2013-11-21 | F. Hoffmann-La Roche Ag | Halogen-alkyl-1,3 oxazines as BACE1 and/or BACE2 inhibitors |
| US9181236B2 (en) | 2011-08-22 | 2015-11-10 | Merck Sharp & Dohme Corp. | 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use |
| EP2766358B1 (en) | 2011-10-13 | 2016-06-22 | Novartis AG | Novel oxazine derivatives and their use in the treatment of disease |
| UA111749C2 (uk) | 2011-12-05 | 2016-06-10 | Янссен Фармацевтика Нв | Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну |
| CA2853891C (en) * | 2011-12-06 | 2020-03-10 | Janssen Pharmaceutica Nv | 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives |
| US8338413B1 (en) | 2012-03-07 | 2012-12-25 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| WO2014059185A1 (en) | 2012-10-12 | 2014-04-17 | Amgen Inc. | Amino - dihydrothiazine and amino - dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use |
| WO2014062549A1 (en) | 2012-10-17 | 2014-04-24 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| EP2908824B1 (en) | 2012-10-17 | 2018-05-02 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
| AU2013363151A1 (en) | 2012-12-20 | 2015-06-04 | Merck Sharp & Dohme Corp. | C5, C6 oxacyclic-fused iminothiazine dioxide compounds as BACE inhibitors |
| US9489013B2 (en) | 2012-12-20 | 2016-11-08 | Merck Sharp & Dohme Corp. | C6-azaspiro iminothiadiazine dioxides as bace inhibitors, compositions, and their use |
| CN105283457B (zh) | 2013-06-12 | 2018-09-18 | 詹森药业有限公司 | 作为β-分泌酶(BACE)抑制剂的4-氨基-6-苯基-5,6-二氢咪唑并[1,5-A]吡嗪衍生物 |
| US9751886B2 (en) | 2013-06-12 | 2017-09-05 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-A]pyrazine derivatives as inhibitors of beta-secretase (BACE) |
| WO2014198851A1 (en) | 2013-06-12 | 2014-12-18 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace) |
| GEAP201814248A (en) * | 2014-02-19 | 2018-04-10 | H Lundbeck As | 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease |
| TWI684452B (zh) * | 2014-03-14 | 2020-02-11 | 美國禮來大藥廠 | 胺基噻嗪化合物 |
| CR20170187A (es) * | 2014-11-10 | 2018-02-01 | H Lundbeck As | 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer |
| MA40941A (fr) * | 2014-11-10 | 2017-09-19 | H Lundbeck As | 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1 |
| JO3458B1 (ar) * | 2014-11-10 | 2020-07-05 | H Lundbeck As | 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1 |
| ES2768823T3 (es) | 2014-12-18 | 2020-06-23 | Janssen Pharmaceutica Nv | Derivados de 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2H-pirrol-5-amina útiles como inhibidores de beta-secretasa |
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| Publication number | Publication date |
|---|---|
| EA201291435A1 (ru) | 2013-05-30 |
| KR101730937B1 (ko) | 2017-04-27 |
| JP2013531645A (ja) | 2013-08-08 |
| BR112012031094A2 (pt) | 2016-10-25 |
| DK2580200T3 (en) | 2017-01-09 |
| HK1182098A1 (en) | 2013-11-22 |
| CN102933564A (zh) | 2013-02-13 |
| US20130109683A1 (en) | 2013-05-02 |
| ES2607083T3 (es) | 2017-03-29 |
| US9828350B2 (en) | 2017-11-28 |
| MX2012014368A (es) | 2013-01-22 |
| AR081587A1 (es) | 2012-10-03 |
| NZ603427A (en) | 2013-08-30 |
| CL2012003428A1 (es) | 2013-04-01 |
| WO2011154431A1 (en) | 2011-12-15 |
| IL223423A (en) | 2016-03-31 |
| EP2580200A1 (en) | 2013-04-17 |
| PH12012502377A1 (en) | 2014-10-14 |
| CO6602112A2 (es) | 2013-01-18 |
| CN102933564B (zh) | 2015-07-22 |
| KR20130119851A (ko) | 2013-11-01 |
| JP5711813B2 (ja) | 2015-05-07 |
| TW201211037A (en) | 2012-03-16 |
| CA2799640A1 (en) | 2011-12-15 |
| AU2011263797A1 (en) | 2012-11-22 |
| TWI537263B (zh) | 2016-06-11 |
| CA2799640C (en) | 2018-10-16 |
| EP2580200B1 (en) | 2016-09-14 |
| AU2011263797B2 (en) | 2014-06-05 |
| SG185651A1 (en) | 2012-12-28 |
| EA021240B1 (ru) | 2015-05-29 |
| ZA201209297B (en) | 2014-09-25 |
| US20160152581A1 (en) | 2016-06-02 |
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