MX2012001070A - Derivados de oxazina y su uso como inhibidores de bace para el tratamiento de trastornos neurologicos. - Google Patents
Derivados de oxazina y su uso como inhibidores de bace para el tratamiento de trastornos neurologicos.Info
- Publication number
- MX2012001070A MX2012001070A MX2012001070A MX2012001070A MX2012001070A MX 2012001070 A MX2012001070 A MX 2012001070A MX 2012001070 A MX2012001070 A MX 2012001070A MX 2012001070 A MX2012001070 A MX 2012001070A MX 2012001070 A MX2012001070 A MX 2012001070A
- Authority
- MX
- Mexico
- Prior art keywords
- treatment
- neurological disorders
- bace inhibitors
- oxazine derivatives
- bace
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 101150058765 BACE1 gene Proteins 0.000 title 1
- 208000012902 Nervous system disease Diseases 0.000 title 1
- 208000025966 Neurological disease Diseases 0.000 title 1
- 150000004893 oxazines Chemical class 0.000 title 1
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract 1
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 150000002391 heterocyclic compounds Chemical class 0.000 abstract 1
- 150000003839 salts Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—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
- A61K31/535—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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D267/02—Seven-membered rings
- C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
- C07D267/10—Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
-
- 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
-
- 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
- C07D413/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07D417/12—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 linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La invención se refiere a novedosos compuestos heterocíclicos novedosos de la fórmula (I): (ver fórmula (I)) en donde todas las variables son como se definen en la memoria descriptiva, en forma libre o en forma de sal, a su preparación, a su uso médico como inhibidores de BACE para el tratamiento de la enfermedad de Alzheimer, y a medicamentos que los comprenden.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22847209P | 2009-07-24 | 2009-07-24 | |
| US25891109P | 2009-11-06 | 2009-11-06 | |
| US36370210P | 2010-07-13 | 2010-07-13 | |
| PCT/EP2010/060718 WO2011009943A1 (en) | 2009-07-24 | 2010-07-23 | Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2012001070A true MX2012001070A (es) | 2012-03-16 |
Family
ID=42629546
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2012001070A MX2012001070A (es) | 2009-07-24 | 2010-07-23 | Derivados de oxazina y su uso como inhibidores de bace para el tratamiento de trastornos neurologicos. |
Country Status (26)
| Country | Link |
|---|---|
| US (5) | US8207164B2 (es) |
| EP (1) | EP2456763B1 (es) |
| JP (1) | JP5767214B2 (es) |
| KR (2) | KR20140004810A (es) |
| CN (1) | CN102471293B (es) |
| AR (1) | AR077328A1 (es) |
| AU (1) | AU2010274913B2 (es) |
| CA (1) | CA2768980A1 (es) |
| CL (1) | CL2012000185A1 (es) |
| CO (1) | CO6491058A2 (es) |
| CR (1) | CR20120002A (es) |
| CU (1) | CU24083B1 (es) |
| EA (1) | EA201200174A1 (es) |
| EC (1) | ECSP12011622A (es) |
| ES (1) | ES2534315T3 (es) |
| GT (1) | GT201200016A (es) |
| IL (1) | IL217378A (es) |
| MA (1) | MA33450B1 (es) |
| MX (1) | MX2012001070A (es) |
| NZ (1) | NZ597529A (es) |
| PE (1) | PE20121440A1 (es) |
| SG (1) | SG177397A1 (es) |
| TW (1) | TW201107316A (es) |
| UY (1) | UY32799A (es) |
| WO (1) | WO2011009943A1 (es) |
| ZA (1) | ZA201200155B (es) |
Families Citing this family (65)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| AU2006307314C1 (en) | 2005-10-25 | 2011-08-25 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
| WO2008133273A1 (ja) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | アルツハイマー症治療用医薬組成物 |
| EP2147914B1 (en) | 2007-04-24 | 2014-06-04 | Shionogi&Co., Ltd. | Aminodihydrothiazine derivatives substituted with cyclic groups |
| EA020740B1 (ru) | 2008-06-13 | 2015-01-30 | Шионоги & Ко., Лтд. | Серосодержащее гетероциклическое производное, обладающее активностью ингибитора бета-секретазы |
| 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 |
| AR077328A1 (es) * | 2009-07-24 | 2011-08-17 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
| US8188079B2 (en) * | 2009-08-19 | 2012-05-29 | Hoffman-La Roche Inc. | 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| 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 |
| US8563543B2 (en) | 2009-10-08 | 2013-10-22 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| TWI488852B (zh) | 2009-12-11 | 2015-06-21 | Shionogi & Co | 衍生物 |
| UA103272C2 (uk) | 2009-12-11 | 2013-09-25 | Ф. Хоффманн-Ля Рош Аг | 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2 |
| CA2785341A1 (en) * | 2009-12-31 | 2011-07-07 | Novartis Ag | Pyrazine derivatives and their use in the treatment of neurological disorders |
| EP2547686B1 (en) | 2010-03-15 | 2014-01-22 | Amgen Inc. | Amino-dihydrooxazine and amino-dihydrothiazine spiro compounds as beta-secretase modulators and their medical use |
| US8673894B2 (en) * | 2010-05-07 | 2014-03-18 | Hoffmann-La Roche Inc. | 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds |
| WO2011154431A1 (en) | 2010-06-09 | 2011-12-15 | Janssen Pharmaceutica Nv | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
| RS53096B (sr) * | 2010-07-13 | 2014-06-30 | Novartis Ag | Derivati oksazina i njihova upotreba u lečenju neuroloških oboljenja |
| EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
| AU2011321427A1 (en) | 2010-10-29 | 2013-05-02 | Shionogi & Co., Ltd. | Naphthyridine derivative |
| MY170715A (en) | 2010-12-22 | 2019-08-27 | Janssen Pharmaceutica Nv | 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (bace) |
| US8524897B2 (en) * | 2011-01-12 | 2013-09-03 | Novartis Ag | Crystalline oxazine derivative |
| MX2013008111A (es) * | 2011-01-12 | 2013-10-30 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de transtornos neurologicos. |
| KR20140010031A (ko) * | 2011-01-13 | 2014-01-23 | 노파르티스 아게 | 대사 장애의 치료를 위한 bace-2 억제제 |
| CN106117193B (zh) | 2011-01-13 | 2019-09-13 | 诺华股份有限公司 | 新的杂环衍生物及其在神经性疾病治疗中的应用 |
| US9242943B2 (en) * | 2011-01-18 | 2016-01-26 | Siena Biotech S.P.A. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| US8399459B2 (en) * | 2011-02-02 | 2013-03-19 | Hoffmann-La Roche Inc. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| US8815841B2 (en) * | 2011-02-18 | 2014-08-26 | Hoffmann-La Roche Inc. | 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors |
| HUE026338T2 (en) * | 2011-03-01 | 2016-05-30 | Janssen Pharmaceutica Nv | 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-ylamine derivatives useful as inhibitors of beta-secretase (bace) |
| US9067924B2 (en) * | 2011-03-04 | 2015-06-30 | Hoffmann-La Roche Inc. | 1,4 thiazepines/sulfones as BACE1 and/or BACE2 inhibitors |
| JP5853035B2 (ja) | 2011-03-09 | 2016-02-09 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap | β−セクレターゼ(BACE)の阻害剤として有用な3,4−ジヒドロ−ピロロ[1,2−a]ピラジン−1−イルアミン誘導体 |
| US8748418B2 (en) * | 2011-03-18 | 2014-06-10 | Hoffmann-La Roche Inc. | 1,4-oxazepines as BACE1 and/or BACE2 inhibitors |
| US8877744B2 (en) | 2011-04-04 | 2014-11-04 | Hoffmann-La Roche Inc. | 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors |
| US9221839B2 (en) | 2011-04-07 | 2015-12-29 | Merck Sharp & Dohme Corp. | C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
| US9145426B2 (en) | 2011-04-07 | 2015-09-29 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
| US8754075B2 (en) * | 2011-04-11 | 2014-06-17 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE1 and/or BACE2 inhibitors |
| CA2832473A1 (en) | 2011-04-13 | 2012-10-18 | Merck Sharp & Dohme Corp. | 5-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions, and their use |
| 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 |
| US9079919B2 (en) * | 2011-05-27 | 2015-07-14 | Hoffmann-La Roche Inc. | Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as BACE1 and/or BACE2 inhibitors |
| KR20140041590A (ko) * | 2011-06-07 | 2014-04-04 | 에프. 호프만-라 로슈 아게 | [1,3]옥사진 |
| JP2014516063A (ja) * | 2011-06-07 | 2014-07-07 | エフ.ホフマン−ラ ロシュ アーゲー | Bace1及び/又はbace2阻害剤としてのハロゲン−アルキル−1,3オキサジン |
| US8927535B2 (en) * | 2011-07-06 | 2015-01-06 | Hoffman-La Roche Inc. | Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors |
| BR112014004181A2 (pt) | 2011-08-22 | 2017-06-13 | Merck Sharp & Dohme | composto, composição farmacêutica, e, método de tratamento, prevenção, e / ou retardo do início de uma doença ou patologia |
| US9296759B2 (en) | 2011-09-21 | 2016-03-29 | Amgen Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| EA201490774A1 (ru) | 2011-10-13 | 2014-08-29 | Новартис Аг | Новые производные оксазина и их применение при лечении заболевания |
| UA111749C2 (uk) * | 2011-12-05 | 2016-06-10 | Янссен Фармацевтика Нв | Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну |
| EA024716B1 (ru) * | 2011-12-06 | 2016-10-31 | Янссен Фармацевтика Нв | Производные 5-(3-аминофенил)-5-алкил-5,6-дигидро-2h-[1,4]оксазин-3-амина |
| AR089781A1 (es) * | 2012-01-26 | 2014-09-17 | Hoffmann La Roche | Fluorometil-5,6-dihidro-4h-[1,3]oxazinas |
| 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 |
| WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
| WO2014078314A1 (en) | 2012-11-15 | 2014-05-22 | Amgen Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| AU2013363151A1 (en) | 2012-12-20 | 2015-06-04 | Merck Sharp & Dohme Corp. | C5, C6 oxacyclic-fused iminothiazine dioxide compounds as BACE inhibitors |
| TW201512171A (zh) | 2013-04-19 | 2015-04-01 | Pfizer Ltd | 化學化合物 |
| CN105452251B (zh) | 2013-06-12 | 2017-12-26 | 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‑3(2H)‑酮衍生物 |
| WO2014198853A1 (en) | 2013-06-12 | 2014-12-18 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
| CA2911693C (en) | 2013-06-12 | 2021-08-24 | 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) |
| FR3025591B1 (fr) * | 2014-09-05 | 2016-10-14 | Technofan | Dispositif de ventilation, aeronef comportant un tel dispositif de ventilation et procede de surveillance associe |
| WO2016096979A1 (en) | 2014-12-18 | 2016-06-23 | Janssen Pharmaceutica Nv | 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine compound inhibitors of beta-secretase |
| TW201726651A (zh) * | 2015-09-23 | 2017-08-01 | 健生藥品公司 | 2,3,4,5-四氫吡啶-6-胺衍生物 |
| JP2019524825A (ja) | 2016-08-26 | 2019-09-05 | イーライ リリー アンド カンパニー | 選択的bace1阻害剤として有用な1,4−オキサジン |
| US10159191B2 (en) | 2016-09-23 | 2018-12-25 | Deere & Company | Harvester grain unloader |
| CN110018266B (zh) * | 2019-02-15 | 2022-03-04 | 广州市妇女儿童医疗中心 | 一种快速定量分析48种氨基酸的方法 |
| CN112250580A (zh) * | 2020-10-28 | 2021-01-22 | 上海昂卓新材料科技有限公司 | 一种2-硝基-2-取代苯基丙烷-1,3-二醇的制备方法 |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL6911868A (es) | 1968-08-31 | 1970-03-03 | ||
| PT72878B (en) | 1980-04-24 | 1983-03-29 | Merck & Co Inc | Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents |
| TW385308B (en) | 1994-03-04 | 2000-03-21 | Merck & Co Inc | Prodrugs of morpholine tachykinin receptor antagonists |
| TW200502221A (en) * | 2002-10-03 | 2005-01-16 | Astrazeneca Ab | Novel lactams and uses thereof |
| EP1631260A2 (en) | 2003-02-28 | 2006-03-08 | Transform Pharmaceuticals, Inc. | Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen |
| TW200505902A (en) | 2003-03-20 | 2005-02-16 | Schering Corp | Cannabinoid receptor ligands |
| US7728025B2 (en) | 2003-12-29 | 2010-06-01 | Banyu Pharmaceutical Co., Ltd. | 2-heteroaryl-substituted benzimidazole derivative |
| US20070149547A1 (en) | 2004-02-12 | 2007-06-28 | Celine Bonnefous | Bipyridyl amides as modulators of metabotropic glutamate receptor-5 |
| TW200624426A (en) * | 2004-09-21 | 2006-07-16 | Lilly Co Eli | BACE inhibitors |
| US7888374B2 (en) | 2005-01-28 | 2011-02-15 | Abbott Laboratories | Inhibitors of c-jun N-terminal kinases |
| AU2006307314C1 (en) * | 2005-10-25 | 2011-08-25 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
| EP2132177B1 (en) | 2007-03-01 | 2013-07-17 | Novartis AG | Pim kinase inhibitors and methods of their use |
| WO2008133273A1 (ja) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | アルツハイマー症治療用医薬組成物 |
| EP2147914B1 (en) | 2007-04-24 | 2014-06-04 | Shionogi&Co., Ltd. | Aminodihydrothiazine derivatives substituted with cyclic groups |
| GB0713686D0 (en) | 2007-07-13 | 2007-08-22 | Addex Pharmaceuticals Sa | New compounds 2 |
| MY160690A (en) | 2008-01-18 | 2017-03-15 | Eisai R&D Man Co Ltd | Condensed aminodihydrothiazine derivative |
| US20100197688A1 (en) | 2008-05-29 | 2010-08-05 | Nantermet Philippe G | Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer |
| EA020740B1 (ru) | 2008-06-13 | 2015-01-30 | Шионоги & Ко., Лтд. | Серосодержащее гетероциклическое производное, обладающее активностью ингибитора бета-секретазы |
| TW201028381A (en) | 2008-07-14 | 2010-08-01 | Shionogi & Co | Pyridine derivative having ttk inhibition 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 |
| US9237972B2 (en) | 2008-12-16 | 2016-01-19 | Kimberly-Clark Worldwide, Inc. | Liquid surfactant compositions that adhere to surfaces and solidify and swell in the presence of water and articles using the same |
| US8461160B2 (en) | 2009-05-08 | 2013-06-11 | Hoffmann-La Roche, Inc. | Dihydropyrimidinones |
| AR077328A1 (es) | 2009-07-24 | 2011-08-17 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
| US8188079B2 (en) | 2009-08-19 | 2012-05-29 | Hoffman-La Roche Inc. | 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines |
| WO2011058763A1 (ja) | 2009-11-13 | 2011-05-19 | 塩野義製薬株式会社 | アミノリンカーを有するアミノチアジンまたはアミノオキサジン誘導体 |
| US7964594B1 (en) | 2009-12-10 | 2011-06-21 | Hoffmann-La Roche Inc. | Amino oxazine derivatives |
| UA103272C2 (uk) | 2009-12-11 | 2013-09-25 | Ф. Хоффманн-Ля Рош Аг | 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2 |
| TWI488852B (zh) | 2009-12-11 | 2015-06-21 | Shionogi & Co | 衍生物 |
| US8673894B2 (en) * | 2010-05-07 | 2014-03-18 | Hoffmann-La Roche Inc. | 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds |
| CN102918036A (zh) | 2010-06-09 | 2013-02-06 | 詹森药业有限公司 | 用作β-分泌酶(BACE)抑制剂的5-氨基-3,6-二氢-1H-吡嗪-2-酮衍生物 |
| WO2011154431A1 (en) | 2010-06-09 | 2011-12-15 | Janssen Pharmaceutica Nv | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
| RS53096B (sr) * | 2010-07-13 | 2014-06-30 | Novartis Ag | Derivati oksazina i njihova upotreba u lečenju neuroloških oboljenja |
| US8524897B2 (en) | 2011-01-12 | 2013-09-03 | Novartis Ag | Crystalline oxazine derivative |
| MX2013008111A (es) | 2011-01-12 | 2013-10-30 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de transtornos neurologicos. |
| CN106117193B (zh) | 2011-01-13 | 2019-09-13 | 诺华股份有限公司 | 新的杂环衍生物及其在神经性疾病治疗中的应用 |
| KR20140010031A (ko) | 2011-01-13 | 2014-01-23 | 노파르티스 아게 | 대사 장애의 치료를 위한 bace-2 억제제 |
| EA201490774A1 (ru) | 2011-10-13 | 2014-08-29 | Новартис Аг | Новые производные оксазина и их применение при лечении заболевания |
-
2010
- 2010-07-22 AR ARP100102667A patent/AR077328A1/es unknown
- 2010-07-22 UY UY0001032799A patent/UY32799A/es not_active Application Discontinuation
- 2010-07-23 JP JP2012521053A patent/JP5767214B2/ja not_active Expired - Fee Related
- 2010-07-23 CU CU2012000013A patent/CU24083B1/es not_active IP Right Cessation
- 2010-07-23 ES ES10737870.5T patent/ES2534315T3/es active Active
- 2010-07-23 TW TW099124438A patent/TW201107316A/zh unknown
- 2010-07-23 EA EA201200174A patent/EA201200174A1/ru unknown
- 2010-07-23 CA CA2768980A patent/CA2768980A1/en not_active Abandoned
- 2010-07-23 PE PE2012000094A patent/PE20121440A1/es not_active Application Discontinuation
- 2010-07-23 MA MA34558A patent/MA33450B1/fr unknown
- 2010-07-23 KR KR1020137033812A patent/KR20140004810A/ko not_active Withdrawn
- 2010-07-23 WO PCT/EP2010/060718 patent/WO2011009943A1/en not_active Ceased
- 2010-07-23 US US12/842,360 patent/US8207164B2/en active Active
- 2010-07-23 CN CN201080035169.0A patent/CN102471293B/zh not_active Expired - Fee Related
- 2010-07-23 MX MX2012001070A patent/MX2012001070A/es active IP Right Grant
- 2010-07-23 AU AU2010274913A patent/AU2010274913B2/en not_active Ceased
- 2010-07-23 EP EP10737870.5A patent/EP2456763B1/en not_active Revoked
- 2010-07-23 SG SG2011096823A patent/SG177397A1/en unknown
- 2010-07-23 NZ NZ597529A patent/NZ597529A/xx not_active IP Right Cessation
- 2010-07-23 KR KR1020127001651A patent/KR101422965B1/ko not_active Expired - Fee Related
-
2012
- 2012-01-05 IL IL217378A patent/IL217378A/en not_active IP Right Cessation
- 2012-01-09 ZA ZA2012/00155A patent/ZA201200155B/en unknown
- 2012-01-09 CR CR20120002A patent/CR20120002A/es unknown
- 2012-01-19 CO CO12007858A patent/CO6491058A2/es active IP Right Grant
- 2012-01-23 CL CL2012000185A patent/CL2012000185A1/es unknown
- 2012-01-24 GT GT201200016A patent/GT201200016A/es unknown
- 2012-01-24 EC EC2012011622A patent/ECSP12011622A/es unknown
- 2012-04-24 US US13/454,751 patent/US20120238560A1/en not_active Abandoned
-
2013
- 2013-07-12 US US13/940,354 patent/US20140088084A1/en not_active Abandoned
- 2013-12-20 US US14/136,679 patent/US8846658B2/en active Active
-
2014
- 2014-07-07 US US14/324,883 patent/US20150018338A1/en not_active Abandoned
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| MX2012001070A (es) | Derivados de oxazina y su uso como inhibidores de bace para el tratamiento de trastornos neurologicos. | |
| TN2012000249A1 (en) | Pyrazine derivatives and their use in the treatment of neurological disorders | |
| TN2013000285A1 (en) | Novel heterocyclic derivatives and their use in the treatment of neurological disorders | |
| PH12013501600A1 (en) | Novel heterocyclic derivatives | |
| IN2014DN03206A (es) | ||
| EA201200176A1 (ru) | Производные оксазина и их применение для лечения неврологических нарушений | |
| MX2009010059A (es) | Derivados de quinolina para el tratamiento de enfermedades inflamatorias. | |
| EA201391029A1 (ru) | Производные оксазина и их применение при лечении неврологических нарушений | |
| PH12015501385A1 (en) | Autotaxin inhibitors | |
| MX347241B (es) | Derivados de aminopirimidina para usarse como moduladores de la actividad de cinasa. | |
| TN2014000062A1 (en) | 2 -amino-4 - (pyridin- 2 -yl) - 5, 6 -dihydro-4h- 1, 3 -oxazine derivatives and their use as bace-1 and/or bace - 2 inhibitors | |
| UA107188C2 (uk) | Карбоксамідні похідні хіназолінів або хінолінів та фармацевтична композиція на їх основі | |
| MX2013012652A (es) | Derivados de n-[(1h-pirazol-1-il)aril]-1h-indol o 1h-indazol-3-carboxamida, su preparacion y su uso como antagonistas p2y12. | |
| MX2014000964A (es) | Derivados aza heterociclicos sustituidos. | |
| MX2012001134A (es) | Composiciones y metodos para inhibicion de la via jak. | |
| NZ702254A (en) | 5-amino[1,4]thiazines as bace 1 inhibitors | |
| MX2010002007A (es) | Sulfonas ciclicas sustituidas por amino-bencilo utiles como inhibidores de bace. | |
| TN2011000668A1 (en) | Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders | |
| TN2012000370A1 (en) | 5-alkynyl pyrimidines and their use as kinase inhibitors | |
| CA2863110A1 (en) | 1,2- pyridazine, 1,6- pyridazine or pyrimidine - benzamide derivatives as gpbar1 modulators | |
| TN2013000327A1 (en) | Novel heterocyclic derivatives | |
| MA33958B1 (fr) | Derives de pyrazine et leur utilisation dans le traitement de troubles neurologiques | |
| TN2010000488A1 (en) | Aminodihydrothiazine derivatives as bace inhibitors for the treatment of alzheimer's disease | |
| MX2010009382A (es) | Derivados de 4-aminociclohexano sustituidos para tratamiento de dolor. |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration |