CO6541656A2 - 2-amino-5.5- difluor-5.6-dihidro-4h-oxazinas como inhibidores de bace1 y/o bace 2 - Google Patents
2-amino-5.5- difluor-5.6-dihidro-4h-oxazinas como inhibidores de bace1 y/o bace 2Info
- Publication number
- CO6541656A2 CO6541656A2 CO12113850A CO12113850A CO6541656A2 CO 6541656 A2 CO6541656 A2 CO 6541656A2 CO 12113850 A CO12113850 A CO 12113850A CO 12113850 A CO12113850 A CO 12113850A CO 6541656 A2 CO6541656 A2 CO 6541656A2
- Authority
- CO
- Colombia
- Prior art keywords
- difluor
- amino
- oxazinas
- dihidro
- bace1
- Prior art date
Links
Classifications
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- 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
- C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
- C07D265/06—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings
- C07D265/08—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- 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
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
La presente invención se refiere a derivados de la 2-amino-5,5-difluor-5,6- dihidro-4H-[1,3]oxazin-4-il)-fenil]-amida de la fórmula Ique tienen actividad inhibidora de la BACEI y/o de la BACE2, a su obtención, a composiciones farmacéuticas que los contienen y a su utilización como sustancias terapéuticamente activas. Los compuestos activos de la presente invención son útiles para el tratamiento terapéutico y/o profiláctico p.ej. de la enfermedad de Alzheimer y de la diabetes de tipo 2.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP09178983 | 2009-12-11 |
Publications (1)
Publication Number | Publication Date |
---|---|
CO6541656A2 true CO6541656A2 (es) | 2012-10-16 |
Family
ID=43585547
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CO12113850A CO6541656A2 (es) | 2009-12-11 | 2012-07-06 | 2-amino-5.5- difluor-5.6-dihidro-4h-oxazinas como inhibidores de bace1 y/o bace 2 |
Country Status (25)
Country | Link |
---|---|
US (1) | US8389513B2 (es) |
EP (1) | EP2509965A1 (es) |
JP (1) | JP5584778B2 (es) |
KR (1) | KR101506773B1 (es) |
CN (1) | CN102712609A (es) |
AR (1) | AR079327A1 (es) |
AU (1) | AU2010330031B2 (es) |
BR (1) | BR112012013175A2 (es) |
CA (1) | CA2776727C (es) |
CL (1) | CL2012001464A1 (es) |
CO (1) | CO6541656A2 (es) |
CR (1) | CR20120262A (es) |
EC (1) | ECSP12011961A (es) |
IL (1) | IL219107A (es) |
IN (1) | IN2012DN03043A (es) |
MA (1) | MA34779B1 (es) |
MX (1) | MX2012006493A (es) |
MY (1) | MY169962A (es) |
NZ (1) | NZ599008A (es) |
PE (1) | PE20121500A1 (es) |
RU (1) | RU2515221C2 (es) |
SG (1) | SG181610A1 (es) |
TW (1) | TWI487704B (es) |
UA (1) | UA103272C2 (es) |
WO (1) | WO2011069934A1 (es) |
Families Citing this family (65)
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BRPI0617852A2 (pt) | 2005-10-25 | 2011-08-09 | Shionogi & Co | compostos derivados de aminodi-hidrotiazina assim como composições contendo os mesmos |
AU2008245082B8 (en) | 2007-04-24 | 2012-09-13 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
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 |
WO2009151098A1 (ja) | 2008-06-13 | 2009-12-17 | 塩野義製薬株式会社 | βセクレターゼ阻害作用を有する含硫黄複素環誘導体 |
EP2360155A4 (en) | 2008-10-22 | 2012-06-20 | Shionogi & Co | 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT |
AR077328A1 (es) | 2009-07-24 | 2011-08-17 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
EP2485591B1 (en) | 2009-10-08 | 2016-03-23 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
WO2011044184A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | 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 | |
US8569310B2 (en) | 2009-10-08 | 2013-10-29 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use |
RU2012129168A (ru) † | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
EP2580200B1 (en) | 2010-06-09 | 2016-09-14 | Janssen Pharmaceutica, N.V. | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
AU2011321427A1 (en) | 2010-10-29 | 2013-05-02 | Shionogi & Co., Ltd. | Naphthyridine derivative |
US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
WO2012071279A1 (en) | 2010-11-23 | 2012-05-31 | Amgen Inc. | Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use |
EP2655376B1 (en) | 2010-12-22 | 2017-08-23 | 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 |
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JP2014514302A (ja) | 2011-04-13 | 2014-06-19 | メルク・シャープ・アンド・ドーム・コーポレーション | Bace阻害薬としての5−置換されたイミノチアジン類およびそれのモノおよびジオキシド、組成物およびそれらの使用 |
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CN110747276B (zh) * | 2019-11-22 | 2020-06-30 | 山东大学齐鲁医院 | Bace2作为胶质瘤预后/诊断/治疗标志物的应用 |
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DE60003791T2 (de) * | 1999-02-09 | 2004-02-05 | The University Of Virginia Alumni Patents Foundation | Felbamat-derivate |
MXPA05002705A (es) * | 2002-09-10 | 2005-09-08 | Pharmacia & Upjohn Co Llc | Aminoeteres sustituidos para el tratamiento de la enfermedad de alzheimer. |
CA2505098A1 (en) * | 2002-11-12 | 2004-05-27 | Merck & Co., Inc. | Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease |
KR20060066057A (ko) * | 2003-06-30 | 2006-06-15 | 다이이찌 세이야꾸 가부시기가이샤 | 복소환 메틸 설폰 유도체 |
WO2006032851A1 (en) | 2004-09-20 | 2006-03-30 | Biolipox Ab | Pyrazole compounds useful in the treatment of inflammation |
US20090221579A1 (en) * | 2004-10-15 | 2009-09-03 | Jeffrey Scott Albert | Substituted Amino-Compounds and Uses Thereof |
BRPI0617852A2 (pt) | 2005-10-25 | 2011-08-09 | Shionogi & Co | compostos derivados de aminodi-hidrotiazina assim como composições contendo os mesmos |
SA08290245B1 (ar) | 2007-04-23 | 2012-02-12 | استرازينيكا ايه بي | مشتقات كربو كساميد جديدة من -n (8-اريل رباعي هيدرو نفثالين غير متجانس- 2- يل) أو -n (5-اريل كرومان غير متجانس -3-يل) لعلاج الألم |
AU2008245082B8 (en) | 2007-04-24 | 2012-09-13 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
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 |
US20100317850A1 (en) | 2008-01-18 | 2010-12-16 | Yuichi Suzuki | Condensed aminodihydrothiazine derivative |
BRPI0907563A2 (pt) | 2008-02-18 | 2015-08-04 | Hoffmann La Roche | Derivados de 4,5-di-hidro-xazol-2-il amina |
GB0912778D0 (en) * | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
AR077328A1 (es) | 2009-07-24 | 2011-08-17 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
JPWO2011071109A1 (ja) * | 2009-12-11 | 2013-04-22 | 塩野義製薬株式会社 | アミノ基を有する縮合ヘテロ環化合物 |
-
2010
- 2010-06-12 UA UAA201208098A patent/UA103272C2/uk unknown
- 2010-12-03 US US12/959,412 patent/US8389513B2/en not_active Expired - Fee Related
- 2010-12-06 EP EP10785437A patent/EP2509965A1/en not_active Withdrawn
- 2010-12-06 MA MA34922A patent/MA34779B1/fr unknown
- 2010-12-06 KR KR1020127017919A patent/KR101506773B1/ko not_active IP Right Cessation
- 2010-12-06 BR BR112012013175A patent/BR112012013175A2/pt not_active IP Right Cessation
- 2010-12-06 NZ NZ599008A patent/NZ599008A/xx not_active IP Right Cessation
- 2010-12-06 IN IN3043DEN2012 patent/IN2012DN03043A/en unknown
- 2010-12-06 JP JP2012542481A patent/JP5584778B2/ja not_active Expired - Fee Related
- 2010-12-06 CA CA2776727A patent/CA2776727C/en not_active Expired - Fee Related
- 2010-12-06 RU RU2012126989/04A patent/RU2515221C2/ru not_active IP Right Cessation
- 2010-12-06 WO PCT/EP2010/068912 patent/WO2011069934A1/en active Application Filing
- 2010-12-06 PE PE2012000803A patent/PE20121500A1/es not_active Application Discontinuation
- 2010-12-06 SG SG2012042560A patent/SG181610A1/en unknown
- 2010-12-06 AU AU2010330031A patent/AU2010330031B2/en not_active Ceased
- 2010-12-06 CN CN2010800561519A patent/CN102712609A/zh active Pending
- 2010-12-06 MX MX2012006493A patent/MX2012006493A/es active IP Right Grant
- 2010-12-06 MY MYPI2012002594A patent/MY169962A/en unknown
- 2010-12-08 TW TW099142877A patent/TWI487704B/zh not_active IP Right Cessation
- 2010-12-09 AR ARP100104535A patent/AR079327A1/es unknown
-
2012
- 2012-04-05 IL IL219107A patent/IL219107A/en not_active IP Right Cessation
- 2012-05-21 CR CR20120262A patent/CR20120262A/es unknown
- 2012-06-05 CL CL2012001464A patent/CL2012001464A1/es unknown
- 2012-06-08 EC ECSP12011961 patent/ECSP12011961A/es unknown
- 2012-07-06 CO CO12113850A patent/CO6541656A2/es unknown
Also Published As
Publication number | Publication date |
---|---|
US20110144097A1 (en) | 2011-06-16 |
PE20121500A1 (es) | 2012-11-05 |
JP5584778B2 (ja) | 2014-09-03 |
MX2012006493A (es) | 2012-07-03 |
NZ599008A (en) | 2013-08-30 |
CN102712609A (zh) | 2012-10-03 |
CL2012001464A1 (es) | 2014-03-07 |
RU2515221C2 (ru) | 2014-05-10 |
AR079327A1 (es) | 2012-01-18 |
KR101506773B1 (ko) | 2015-03-27 |
AU2010330031B2 (en) | 2013-06-20 |
SG181610A1 (en) | 2012-07-30 |
US8389513B2 (en) | 2013-03-05 |
CA2776727C (en) | 2016-05-31 |
CA2776727A1 (en) | 2011-06-16 |
JP2013513563A (ja) | 2013-04-22 |
IL219107A0 (en) | 2012-06-28 |
MY169962A (en) | 2019-06-19 |
WO2011069934A1 (en) | 2011-06-16 |
BR112012013175A2 (pt) | 2019-09-24 |
KR20120104598A (ko) | 2012-09-21 |
AU2010330031A1 (en) | 2012-06-07 |
IL219107A (en) | 2015-10-29 |
TW201124408A (en) | 2011-07-16 |
TWI487704B (zh) | 2015-06-11 |
MA34779B1 (fr) | 2014-01-02 |
IN2012DN03043A (es) | 2015-07-31 |
UA103272C2 (uk) | 2013-09-25 |
RU2012126989A (ru) | 2014-01-20 |
CR20120262A (es) | 2012-07-27 |
ECSP12011961A (es) | 2012-07-31 |
EP2509965A1 (en) | 2012-10-17 |
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