EA201200174A1 - Производные оксазина и их применение в качестве ингибиторов bace для лечения неврологических нарушений - Google Patents
Производные оксазина и их применение в качестве ингибиторов bace для лечения неврологических нарушенийInfo
- Publication number
- EA201200174A1 EA201200174A1 EA201200174A EA201200174A EA201200174A1 EA 201200174 A1 EA201200174 A1 EA 201200174A1 EA 201200174 A EA201200174 A EA 201200174A EA 201200174 A EA201200174 A EA 201200174A EA 201200174 A1 EA201200174 A1 EA 201200174A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- treatment
- application
- neurological disorders
- bace inhibitors
- oxazin
- Prior art date
Links
- BCHZICNRHXRCHY-UHFFFAOYSA-N 2h-oxazine Chemical class N1OC=CC=C1 BCHZICNRHXRCHY-UHFFFAOYSA-N 0.000 title 1
- 208000012902 Nervous system disease Diseases 0.000 title 1
- 208000025966 Neurological disease Diseases 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 239000003814 drug Substances 0.000 abstract 2
- 229940079593 drug Drugs 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)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Pyridine Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
В заявке описаны новые гетероциклические соединения формулыв которой все переменные являются такими, как определено в описании, в свободной форме или в форме соли, их получение, их применение в медицине и содержащие их лекарственные средства.
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 |
|---|---|
| EA201200174A1 true EA201200174A1 (ru) | 2012-08-30 |
Family
ID=42629546
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201200174A EA201200174A1 (ru) | 2009-07-24 | 2010-07-23 | Производные оксазина и их применение в качестве ингибиторов bace для лечения неврологических нарушений |
Country Status (26)
| Country | Link |
|---|---|
| US (5) | US8207164B2 (ru) |
| EP (1) | EP2456763B1 (ru) |
| JP (1) | JP5767214B2 (ru) |
| KR (2) | KR101422965B1 (ru) |
| CN (1) | CN102471293B (ru) |
| AR (1) | AR077328A1 (ru) |
| AU (1) | AU2010274913B2 (ru) |
| CA (1) | CA2768980A1 (ru) |
| CL (1) | CL2012000185A1 (ru) |
| CO (1) | CO6491058A2 (ru) |
| CR (1) | CR20120002A (ru) |
| CU (1) | CU24083B1 (ru) |
| EA (1) | EA201200174A1 (ru) |
| EC (1) | ECSP12011622A (ru) |
| ES (1) | ES2534315T3 (ru) |
| GT (1) | GT201200016A (ru) |
| IL (1) | IL217378A (ru) |
| MA (1) | MA33450B1 (ru) |
| MX (1) | MX2012001070A (ru) |
| NZ (1) | NZ597529A (ru) |
| PE (1) | PE20121440A1 (ru) |
| SG (1) | SG177397A1 (ru) |
| TW (1) | TW201107316A (ru) |
| UY (1) | UY32799A (ru) |
| WO (1) | WO2011009943A1 (ru) |
| ZA (1) | ZA201200155B (ru) |
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 |
| EP1942105B8 (en) | 2005-10-25 | 2014-08-13 | Shionogi&Co., Ltd. | Aminodihydrothiazine derivative |
| 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 |
| RU2476430C2 (ru) | 2007-04-24 | 2013-02-27 | Сионоги Энд Ко., Лтд. | Производные аминодигидротиазина, замещенные циклической группой |
| US8637504B2 (en) | 2008-06-13 | 2014-01-28 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta secretase inhibitory 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 |
| 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 |
| 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 |
| US8557826B2 (en) | 2009-10-08 | 2013-10-15 | 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 | |
| UA103272C2 (ru) | 2009-12-11 | 2013-09-25 | Ф. Хоффманн-Ля Рош Аг | 2-амино-5,5-дифтор-5,6-дигидро-4h-оксазины как ингибиторы bace1 и/или bace2 |
| MX2012006491A (es) | 2009-12-11 | 2012-07-03 | Shionogi & Co | Derivados de oxazina. |
| WO2011080176A1 (en) * | 2009-12-31 | 2011-07-07 | Novartis Ag | Pyrazine derivatives and their use in the treatment of neurological disorders |
| MX2012010657A (es) | 2010-03-15 | 2013-02-07 | Amgen Inc | Compuestos de espiro amino-dihidrooxazina y amino-dihidrotiazina como moduladores de beta-secretasa y su uso medico. |
| 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) |
| SG178311A1 (en) * | 2010-07-13 | 2012-03-29 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| 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 |
| UA109459C2 (xx) | 2010-12-22 | 2015-08-25 | ПОХІДНІ 5,6-ДИГІДРОІМІДАЗО[1,2-a]ПІРАЗИН-8-ІЛАМІНУ, ПРИДАТНІ ЯК ІНГІБІТОРИ БЕТА-СЕКРЕТАЗИ (BACE) | |
| US8524897B2 (en) * | 2011-01-12 | 2013-09-03 | Novartis Ag | Crystalline oxazine derivative |
| AU2012206555A1 (en) * | 2011-01-12 | 2013-08-01 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| KR20140010031A (ko) * | 2011-01-13 | 2014-01-23 | 노파르티스 아게 | 대사 장애의 치료를 위한 bace-2 억제제 |
| US8637508B2 (en) | 2011-01-13 | 2014-01-28 | Novartis Ag | Heterocyclic derivatives and their use in the treatment of neurological disorders |
| 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 |
| WO2012117027A1 (en) * | 2011-03-01 | 2012-09-07 | 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 |
| SG193342A1 (en) | 2011-03-09 | 2013-10-30 | Janssen Pharmaceutica Nv | 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
| 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 |
| TW201247635A (en) | 2011-04-26 | 2012-12-01 | Shionogi & Co | Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them |
| 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 |
| CN103717592A (zh) * | 2011-06-07 | 2014-04-09 | 霍夫曼-拉罗奇有限公司 | 作为bace1和/或bace2抑制剂的卤代-烷基-1,3噁嗪类 |
| KR20140041590A (ko) * | 2011-06-07 | 2014-04-04 | 에프. 호프만-라 로슈 아게 | [1,3]옥사진 |
| US8927535B2 (en) * | 2011-07-06 | 2015-01-06 | Hoffman-La Roche Inc. | Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors |
| JP2014524472A (ja) | 2011-08-22 | 2014-09-22 | メルク・シャープ・アンド・ドーム・コーポレーション | Bace阻害剤としての2−スピロ置換イミノチアジンならびにそのモノオキシドおよびジオキシド、組成物、ならびにそれらの使用 |
| US9296759B2 (en) | 2011-09-21 | 2016-03-29 | Amgen Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| MX2014004479A (es) * | 2011-10-13 | 2014-08-01 | Novartis Ag | Derivados de oxazina novedosos y su uso en el tratamiento de enfermedades. |
| UA111749C2 (uk) * | 2011-12-05 | 2016-06-10 | Янссен Фармацевтика Нв | Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну |
| KR102002345B1 (ko) * | 2011-12-06 | 2019-07-22 | 얀센 파마슈티카 엔.브이. | 5-(3-아미노페닐)-5-알킬-5,6-디하이드로-2h-[1,4]옥사진-3-아민 유도체 |
| CA2856892C (en) * | 2012-01-26 | 2020-05-12 | F. Hoffmann-La Roche Ag | Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines |
| 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 |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING 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 |
| JP2016504998A (ja) | 2012-12-20 | 2016-02-18 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | Bace阻害剤としてのc5,c6オキサ環縮合イミノチアジンジオキシド化合物、組成物およびそれらの使用 |
| TW201512171A (zh) | 2013-04-19 | 2015-04-01 | Pfizer Ltd | 化學化合物 |
| ES2697684T3 (es) | 2013-06-12 | 2019-01-25 | Janssen Pharmaceutica Nv | Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5 a]pirazina como inhibidores de beta-secretasa (BACE) |
| EA032662B1 (ru) | 2013-06-12 | 2019-06-28 | Янссен Фармацевтика Нв | ПРОИЗВОДНЫЕ 4-АМИНО-6-ФЕНИЛ-5,6-ДИГИДРОИМИДАЗО[1,5-а]ПИРАЗИН-3(2H)-ОНА В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (BACE) |
| CN105324383B (zh) | 2013-06-12 | 2017-10-31 | 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‑6,7‑二氢[1,2,3]三唑并[1,5‑A]吡嗪衍生物 |
| FR3025591B1 (fr) * | 2014-09-05 | 2016-10-14 | Technofan | Dispositif de ventilation, aeronef comportant un tel dispositif de ventilation et procede de surveillance associe |
| AU2015367594C1 (en) | 2014-12-18 | 2019-10-31 | 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 |
| WO2018039062A1 (en) | 2016-08-26 | 2018-03-01 | Eli Lilly And Company | 1,4-oxazines useful as selective bace1 inhibitors |
| 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 (ru) | 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 |
| EP1702919B1 (en) | 2003-12-29 | 2012-05-30 | Msd K.K. | Novel 2-heteroaryl-substituted benzimidazole derivative |
| EP1715867A4 (en) | 2004-02-12 | 2009-04-15 | Merck & Co Inc | BIPYRIDYLAMIDE 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 |
| EP1942105B8 (en) * | 2005-10-25 | 2014-08-13 | Shionogi&Co., Ltd. | Aminodihydrothiazine derivative |
| AU2008221263B2 (en) | 2007-03-01 | 2012-02-23 | Novartis Ag | Pim kinase inhibitors and methods of their use |
| RU2476430C2 (ru) | 2007-04-24 | 2013-02-27 | Сионоги Энд Ко., Лтд. | Производные аминодигидротиазина, замещенные циклической группой |
| 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 |
| GB0713686D0 (en) | 2007-07-13 | 2007-08-22 | Addex Pharmaceuticals Sa | New compounds 2 |
| PE20091438A1 (es) | 2008-01-18 | 2009-09-26 | Eisai Randd Man Co Ltd | Derivados fusionados de aminodihidrotiazina |
| US20100197688A1 (en) | 2008-05-29 | 2010-08-05 | Nantermet Philippe G | Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer |
| US8637504B2 (en) | 2008-06-13 | 2014-01-28 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity |
| WO2010007756A1 (ja) | 2008-07-14 | 2010-01-21 | 塩野義製薬株式会社 | Ttk阻害作用を有するピリジン誘導体 |
| 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 |
| EP2500344A4 (en) | 2009-11-13 | 2013-05-01 | Shionogi & Co | AMINOTHIAZIN OR AMINOOXAZINE DERIVATIVES WITH AN AMINO TERMINATION |
| US7964594B1 (en) | 2009-12-10 | 2011-06-21 | Hoffmann-La Roche Inc. | Amino oxazine derivatives |
| MX2012006491A (es) | 2009-12-11 | 2012-07-03 | Shionogi & Co | Derivados de oxazina. |
| UA103272C2 (ru) | 2009-12-11 | 2013-09-25 | Ф. Хоффманн-Ля Рош Аг | 2-амино-5,5-дифтор-5,6-дигидро-4h-оксазины как ингибиторы bace1 и/или bace2 |
| 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 |
| PH12012502379A1 (en) | 2010-06-09 | 2013-02-18 | Janssen Pharmaceutica Nv | 5-amino-3,6-dihydro-1h-pyrazin-2-one derivatives useful as inhibitors of beta-secretase (bace) |
| 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) |
| SG178311A1 (en) * | 2010-07-13 | 2012-03-29 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| AU2012206555A1 (en) | 2011-01-12 | 2013-08-01 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| US8524897B2 (en) | 2011-01-12 | 2013-09-03 | Novartis Ag | Crystalline oxazine derivative |
| US8637508B2 (en) | 2011-01-13 | 2014-01-28 | Novartis Ag | Heterocyclic derivatives and their use in the treatment of neurological disorders |
| KR20140010031A (ko) | 2011-01-13 | 2014-01-23 | 노파르티스 아게 | 대사 장애의 치료를 위한 bace-2 억제제 |
| MX2014004479A (es) | 2011-10-13 | 2014-08-01 | Novartis Ag | Derivados de oxazina novedosos y su uso en el tratamiento de enfermedades. |
-
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 WO PCT/EP2010/060718 patent/WO2011009943A1/en not_active Ceased
- 2010-07-23 CN CN201080035169.0A patent/CN102471293B/zh not_active Expired - Fee Related
- 2010-07-23 JP JP2012521053A patent/JP5767214B2/ja not_active Expired - Fee Related
- 2010-07-23 NZ NZ597529A patent/NZ597529A/xx not_active IP Right Cessation
- 2010-07-23 MX MX2012001070A patent/MX2012001070A/es active IP Right Grant
- 2010-07-23 EA EA201200174A patent/EA201200174A1/ru unknown
- 2010-07-23 KR KR1020127001651A patent/KR101422965B1/ko not_active Expired - Fee Related
- 2010-07-23 SG SG2011096823A patent/SG177397A1/en unknown
- 2010-07-23 AU AU2010274913A patent/AU2010274913B2/en not_active Ceased
- 2010-07-23 CA CA2768980A patent/CA2768980A1/en not_active Abandoned
- 2010-07-23 CU CU2012000013A patent/CU24083B1/es not_active IP Right Cessation
- 2010-07-23 TW TW099124438A patent/TW201107316A/zh unknown
- 2010-07-23 MA MA34558A patent/MA33450B1/fr unknown
- 2010-07-23 US US12/842,360 patent/US8207164B2/en active Active
- 2010-07-23 PE PE2012000094A patent/PE20121440A1/es not_active Application Discontinuation
- 2010-07-23 KR KR1020137033812A patent/KR20140004810A/ko not_active Withdrawn
- 2010-07-23 EP EP10737870.5A patent/EP2456763B1/en not_active Revoked
- 2010-07-23 ES ES10737870.5T patent/ES2534315T3/es active Active
-
2012
- 2012-01-05 IL IL217378A patent/IL217378A/en not_active IP Right Cessation
- 2012-01-09 CR CR20120002A patent/CR20120002A/es unknown
- 2012-01-09 ZA ZA2012/00155A patent/ZA201200155B/en 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 EC EC2012011622A patent/ECSP12011622A/es unknown
- 2012-01-24 GT GT201200016A patent/GT201200016A/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 |
|---|---|---|
| EA201200174A1 (ru) | Производные оксазина и их применение в качестве ингибиторов bace для лечения неврологических нарушений | |
| EA201200952A1 (ru) | Производные пиразина и их применение для лечения неврологических нарушений | |
| EA201200176A1 (ru) | Производные оксазина и их применение для лечения неврологических нарушений | |
| EA201391029A1 (ru) | Производные оксазина и их применение при лечении неврологических нарушений | |
| EA201391106A1 (ru) | Новые гетероциклические производные | |
| EA201490888A1 (ru) | Новые производные пурина и их применение для лечения заболевания | |
| EA201391032A1 (ru) | Новые гетероциклические производные и их применение в лечении неврологических расстройств | |
| EA201400412A1 (ru) | ЗАМЕЩЕННЫЕ БЕНЗИЛИНДАЗОЛЫ ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ Bub1 КИНАЗЫ ДЛЯ ЛЕЧЕНИЯ ГИПЕРПРОЛИФЕРАТИВНЫХ ЗАБОЛЕВАНИЙ | |
| EA201391752A1 (ru) | Спиро-[1,3]-оксазины и спиро-[1,4]-оксазепины в качестве ингибиторов bace1 и/или bace2 | |
| EA201190158A1 (ru) | Производные бензофуранила для применения в качестве ингибиторов глюкокиназы | |
| MX347241B (es) | Derivados de aminopirimidina para usarse como moduladores de la actividad de cinasa. | |
| EA200901488A1 (ru) | Замещенные имидазолопиридазины, как ингибиторы липидкиназы | |
| EA200901157A1 (ru) | Конденсированные кольцевые гетероциклические модуляторы киназы | |
| JO3007B1 (ar) | مركبات و تركيبات كمثبطات كيناز بروتين | |
| MX2014000964A (es) | Derivados aza heterociclicos sustituidos. | |
| NZ702254A (en) | 5-amino[1,4]thiazines as bace 1 inhibitors | |
| MX2013002208A (es) | Derivados de sulfonilpiperazina que interactuan con la proteina reguladora de glucocinasa para el tratamiento de diabetes. | |
| MX2010002007A (es) | Sulfonas ciclicas sustituidas por amino-bencilo utiles como inhibidores de bace. | |
| MX2013011561A (es) | Compuestos de benzodioxepina y benzodioxina que interactuan con la proteina reguladora de glucocinasa para el tratamiento de diabetes. | |
| UA107356C2 (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 | |
| EA201600411A1 (ru) | Производные пиперидина для применения при лечении или профилактики психиатрических и неврологических состояний | |
| MA33958B1 (fr) | Derives de pyrazine et leur utilisation dans le traitement de troubles neurologiques | |
| TN2013000327A1 (en) | Novel heterocyclic derivatives |