AR084832A1 - Derivado cristalino de oxazina - Google Patents
Derivado cristalino de oxazinaInfo
- Publication number
- AR084832A1 AR084832A1 ARP120100096A ARP120100096A AR084832A1 AR 084832 A1 AR084832 A1 AR 084832A1 AR P120100096 A ARP120100096 A AR P120100096A AR P120100096 A ARP120100096 A AR P120100096A AR 084832 A1 AR084832 A1 AR 084832A1
- Authority
- AR
- Argentina
- Prior art keywords
- oxazine
- crystalline form
- methyl
- compound
- crystal derivative
- Prior art date
Links
- BCHZICNRHXRCHY-UHFFFAOYSA-N 2h-oxazine Chemical compound N1OC=CC=C1 BCHZICNRHXRCHY-UHFFFAOYSA-N 0.000 title 1
- 239000013078 crystal Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- PFENLEKZZJZJBJ-UHFFFAOYSA-N 5-cyano-3-methylpyridine-2-carboxylic acid Chemical compound CC1=CC(C#N)=CN=C1C(O)=O PFENLEKZZJZJBJ-UHFFFAOYSA-N 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- 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
- 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
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Psychiatry (AREA)
- Heart & Thoracic Surgery (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)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente se refiere a la [3-((3R,6R)-5-amino-3,6-dimetil-6-trifluoro-metil-3,6-dihidro-2H-[1,4]oxazin-3-il)-4-fluoro-fenil]-amida del ácido 5-ciano-3-metil-piridina-2-carboxílico en forma cristalina, su preparación, su uso médico, una composición farmacéutica que contiene dicho compuesto en forma cristalina. Estos compuestos pueden usarse como medicamentos útiles para el tratamiento de la enfermedad de Alzheimer.Reivindicación 1: Una forma cristalina del compuesto (1).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161432058P | 2011-01-12 | 2011-01-12 | |
| US201161435088P | 2011-01-21 | 2011-01-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR084832A1 true AR084832A1 (es) | 2013-06-26 |
Family
ID=45833304
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120100096A AR084832A1 (es) | 2011-01-12 | 2012-01-12 | Derivado cristalino de oxazina |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8524897B2 (es) |
| EP (1) | EP2663560A1 (es) |
| JP (1) | JP2014502625A (es) |
| KR (1) | KR20140051823A (es) |
| CN (1) | CN103429588A (es) |
| AR (1) | AR084832A1 (es) |
| AU (1) | AU2012206633A1 (es) |
| BR (1) | BR112013017757A2 (es) |
| CA (1) | CA2824207A1 (es) |
| CY (1) | CY1114757T1 (es) |
| EA (1) | EA201391026A1 (es) |
| MX (1) | MX2013008112A (es) |
| TW (1) | TW201309685A (es) |
| UY (1) | UY33864A (es) |
| WO (1) | WO2012095451A1 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA020740B1 (ru) | 2008-06-13 | 2015-01-30 | Шионоги & Ко., Лтд. | Серосодержащее гетероциклическое производное, обладающее активностью ингибитора бета-секретазы |
| AR077328A1 (es) | 2009-07-24 | 2011-08-17 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
| US8563543B2 (en) | 2009-10-08 | 2013-10-22 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace 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 |
| TWI488852B (zh) | 2009-12-11 | 2015-06-21 | Shionogi & Co | 衍生物 |
| 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 |
| WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
| 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 |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW385308B (en) | 1994-03-04 | 2000-03-21 | Merck & Co Inc | Prodrugs of morpholine tachykinin receptor antagonists |
| TW200505902A (en) | 2003-03-20 | 2005-02-16 | Schering Corp | Cannabinoid receptor ligands |
| 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 |
| EP2147914B1 (en) | 2007-04-24 | 2014-06-04 | Shionogi&Co., Ltd. | Aminodihydrothiazine derivatives substituted with cyclic groups |
| 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 |
| 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 |
| 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 |
| EP2518059A4 (en) | 2009-12-24 | 2013-05-29 | Shionogi & Co | 4-AMINO-1,3-THIAZINE OR OXAZINE DERIVATIVE |
| CA2785341A1 (en) | 2009-12-31 | 2011-07-07 | Novartis Ag | Pyrazine derivatives and their use in the treatment of neurological disorders |
| 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) |
| 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 |
| RS53096B (sr) | 2010-07-13 | 2014-06-30 | Novartis Ag | Derivati oksazina i njihova upotreba u lečenju neuroloških oboljenja |
-
2012
- 2012-01-10 US US13/347,067 patent/US8524897B2/en active Active
- 2012-01-11 WO PCT/EP2012/050367 patent/WO2012095451A1/en not_active Ceased
- 2012-01-11 AU AU2012206633A patent/AU2012206633A1/en not_active Abandoned
- 2012-01-11 EA EA201391026A patent/EA201391026A1/ru unknown
- 2012-01-11 UY UY0001033864A patent/UY33864A/es not_active Application Discontinuation
- 2012-01-11 MX MX2013008112A patent/MX2013008112A/es not_active Application Discontinuation
- 2012-01-11 TW TW101101119A patent/TW201309685A/zh unknown
- 2012-01-11 EP EP12708688.2A patent/EP2663560A1/en not_active Withdrawn
- 2012-01-11 JP JP2013548825A patent/JP2014502625A/ja active Pending
- 2012-01-11 CN CN201280012775XA patent/CN103429588A/zh active Pending
- 2012-01-11 KR KR1020137021074A patent/KR20140051823A/ko not_active Withdrawn
- 2012-01-11 BR BR112013017757A patent/BR112013017757A2/pt not_active IP Right Cessation
- 2012-01-11 CA CA2824207A patent/CA2824207A1/en not_active Abandoned
- 2012-01-12 AR ARP120100096A patent/AR084832A1/es not_active Application Discontinuation
-
2014
- 2014-01-16 CY CY20141100037T patent/CY1114757T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20120178745A1 (en) | 2012-07-12 |
| JP2014502625A (ja) | 2014-02-03 |
| MX2013008112A (es) | 2013-10-01 |
| EP2663560A1 (en) | 2013-11-20 |
| WO2012095451A1 (en) | 2012-07-19 |
| CY1114757T1 (el) | 2016-12-14 |
| CA2824207A1 (en) | 2012-07-19 |
| UY33864A (es) | 2012-08-31 |
| US8524897B2 (en) | 2013-09-03 |
| BR112013017757A2 (pt) | 2016-10-11 |
| CN103429588A (zh) | 2013-12-04 |
| AU2012206633A1 (en) | 2013-08-01 |
| TW201309685A (zh) | 2013-03-01 |
| EA201391026A1 (ru) | 2013-12-30 |
| KR20140051823A (ko) | 2014-05-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |