JO3318B1 - مثبطات bace - Google Patents
مثبطات baceInfo
- Publication number
- JO3318B1 JO3318B1 JOP/2014/0177A JOP20140177A JO3318B1 JO 3318 B1 JO3318 B1 JO 3318B1 JO P20140177 A JOP20140177 A JO P20140177A JO 3318 B1 JO3318 B1 JO 3318B1
- Authority
- JO
- Jordan
- Prior art keywords
- bace inhibitors
- bace
- inhibitors
- compound
- pharmaceutically acceptable
- Prior art date
Links
- 101150058765 BACE1 gene Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—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
- A61K31/5365—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 ortho- or peri-condensed with heterocyclic ring 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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/5415—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 sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
يتعلق الاختراع الحالي بتقديم مركب بالصيغة III: حيث A هي: و Z، R1، R2، R3، وR4 هي كما تم تعريفها في هذه الوثيقة، أو ملح مقبول صيدلياً منه.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361836175P | 2013-06-18 | 2013-06-18 | |
US201361877373P | 2013-09-13 | 2013-09-13 |
Publications (1)
Publication Number | Publication Date |
---|---|
JO3318B1 true JO3318B1 (ar) | 2019-03-13 |
Family
ID=51059662
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JOP/2014/0177A JO3318B1 (ar) | 2013-06-18 | 2014-05-29 | مثبطات bace |
Country Status (14)
Country | Link |
---|---|
US (2) | US9029367B2 (ar) |
EP (1) | EP3010925B1 (ar) |
JP (1) | JP2016522254A (ar) |
KR (1) | KR101780140B1 (ar) |
CN (1) | CN105324385A (ar) |
AU (1) | AU2014281032B2 (ar) |
BR (1) | BR112015029348A8 (ar) |
CA (1) | CA2910415C (ar) |
EA (1) | EA027880B1 (ar) |
ES (1) | ES2657905T3 (ar) |
JO (1) | JO3318B1 (ar) |
MX (1) | MX2015017156A (ar) |
TW (1) | TWI639607B (ar) |
WO (1) | WO2014204730A1 (ar) |
Families Citing this family (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
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 |
AR103680A1 (es) * | 2015-02-23 | 2017-05-24 | Lilly Co Eli | Inhibidores selectivos de bace1 |
TW201717948A (zh) | 2015-08-10 | 2017-06-01 | H 朗德貝克公司 | 包括給予2-胺基-3,5,5-三氟-3,4,5,6-四氫吡啶的聯合治療 |
US20180230160A1 (en) * | 2015-08-12 | 2018-08-16 | H. Lundbeck A/S | 2-amino-7a-phenyl-3,4,4a,5,7,7a-hexahydrofuro[3,4-b]pyridines as bace1 inhibitors |
TW201718543A (zh) | 2015-08-12 | 2017-06-01 | H 朗德貝克公司 | 作爲bace1抑制劑之2-胺基-3-氟-3-(氟甲基)-6-甲基-6-苯基-3,4,5,6-四氫吡啶 |
TWI675034B (zh) * | 2016-05-20 | 2019-10-21 | 美商美國禮來大藥廠 | 四氫呋喃并<img align="absmiddle" height="18px" width="27px" file="d10999.TIF" alt="其他非圖式 ed10999.png" img-content="tif" orientation="portrait" inline="yes" giffile="ed10999.png"></img>化合物及其作為選擇性BACE1抑制劑之用途 |
JP6889466B2 (ja) * | 2016-12-09 | 2021-06-18 | 学校法人 名城大学 | アミド基を含む単離された化合物の塩、その製造方法及びこれを用いたアミド化合物の合成方法 |
CN107892697B (zh) | 2016-12-26 | 2020-11-03 | 郑州泰基鸿诺医药股份有限公司 | 一种[1,3]噻嗪-2-胺类化合物及应用,药物组合物 |
CN111217709A (zh) * | 2018-11-27 | 2020-06-02 | 南京药石科技股份有限公司 | 一种(1-氟环丙基)甲胺盐酸盐的制备方法 |
Family Cites Families (30)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20080029965A (ko) | 2005-06-14 | 2008-04-03 | 쉐링 코포레이션 | 아스파르틸 프로테아제 억제제 |
JP5281794B2 (ja) | 2005-10-25 | 2013-09-04 | 塩野義製薬株式会社 | アミノジヒドロチアジン誘導体 |
JP5383484B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | 環式基で置換されたアミノジヒドロチアジン誘導体 |
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 |
RS54311B1 (en) * | 2008-01-18 | 2016-02-29 | Eisai R&D Management Co. Ltd. | KONDEZOVANI AMINODIHYDROTIAZINE DERIVATIVE |
TWI431004B (zh) * | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
AU2009258496B8 (en) | 2008-06-13 | 2014-06-26 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
AR073406A1 (es) | 2008-09-30 | 2010-11-03 | Eisai R&D Man Co Ltd | Aminodihidrotiazinas fusionadas con tetrahidropiranos,inhibidoras de bace1 y de la produccion de abeta amiloide, composiciones farmaceuticas que las contienen y usos de las mismas para el tratamiento de enfermedades neurodegenerativas,tales como alzheimer. |
AR077277A1 (es) * | 2009-07-09 | 2011-08-17 | Lilly Co Eli | Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer |
GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
US20120245154A1 (en) | 2009-12-09 | 2012-09-27 | Shionogi & Co., Ltd. | Substituted aminothiazine derivative |
US20120245155A1 (en) | 2009-12-11 | 2012-09-27 | Shionogi & Co., Ltd. | Fused heterocyclic compound having amino group |
AU2010328975B2 (en) | 2009-12-11 | 2015-01-22 | Shionogi & Co. Ltd. | Oxazine derivative |
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 |
GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
SG191710A1 (en) | 2011-01-21 | 2013-08-30 | Eisai R&D Man Co Ltd | Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives |
GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
EP2694521B1 (en) | 2011-04-07 | 2015-11-25 | 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 |
US8785436B2 (en) | 2011-05-16 | 2014-07-22 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE 1 and/or BACE2 inhibitors |
AR086539A1 (es) | 2011-05-24 | 2014-01-08 | Bristol Myers Squibb Co | COMPUESTOS PARA LA REDUCCION DE LA PRODUCCION DE b-AMILOIDE |
WO2012168175A1 (en) | 2011-06-07 | 2012-12-13 | F. Hoffmann-La Roche Ag | [1,3]oxazines |
UY34278A (es) | 2011-08-25 | 2013-04-05 | Novartis Ag | Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades |
JP6043355B2 (ja) | 2011-08-31 | 2016-12-14 | ファイザー・インク | ヘキサヒドロピラノ[3,4−d][1,3]チアジン−2−アミン化合物 |
CA3040720C (en) | 2011-11-25 | 2021-06-15 | Adverio Pharma Gmbh | Method for producing substituted 5-fluoro-1h-pyrazolopyridines |
ES2615304T3 (es) | 2012-04-27 | 2017-06-06 | Eisai R&D Management Co., Ltd. | Método para producir el ácido 5-(difluorometil)pirazin-2-carboxílico y un intermedio de la producción de este |
CA2872154C (en) | 2012-05-04 | 2016-08-23 | Pfizer Inc. | Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin-2-amine compounds as inhibitors of app, bace1 and bace2 |
WO2014015125A1 (en) | 2012-07-19 | 2014-01-23 | Eisai R&D Management Co., Ltd. | Fused aminodihydrothiazine derivative salts and uses thereof |
GB201212871D0 (en) | 2012-07-20 | 2012-09-05 | Eisai Ltd | Novel compounds |
-
2014
- 2014-05-29 JO JOP/2014/0177A patent/JO3318B1/ar active
- 2014-05-29 TW TW103118874A patent/TWI639607B/zh not_active IP Right Cessation
- 2014-06-11 US US14/301,358 patent/US9029367B2/en not_active Expired - Fee Related
- 2014-06-11 JP JP2016521454A patent/JP2016522254A/ja active Pending
- 2014-06-11 CA CA2910415A patent/CA2910415C/en not_active Expired - Fee Related
- 2014-06-11 EA EA201592183A patent/EA027880B1/ru not_active IP Right Cessation
- 2014-06-11 KR KR1020157035519A patent/KR101780140B1/ko not_active Expired - Fee Related
- 2014-06-11 AU AU2014281032A patent/AU2014281032B2/en not_active Ceased
- 2014-06-11 BR BR112015029348A patent/BR112015029348A8/pt not_active Application Discontinuation
- 2014-06-11 MX MX2015017156A patent/MX2015017156A/es unknown
- 2014-06-11 EP EP14734712.4A patent/EP3010925B1/en not_active Not-in-force
- 2014-06-11 WO PCT/US2014/041825 patent/WO2014204730A1/en active Application Filing
- 2014-06-11 CN CN201480034958.0A patent/CN105324385A/zh active Pending
- 2014-06-11 ES ES14734712.4T patent/ES2657905T3/es active Active
-
2015
- 2015-04-02 US US14/677,113 patent/US9169271B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
US9169271B2 (en) | 2015-10-27 |
BR112015029348A8 (pt) | 2020-03-17 |
CA2910415C (en) | 2017-09-05 |
MX2015017156A (es) | 2016-03-16 |
CN105324385A (zh) | 2016-02-10 |
US20140371212A1 (en) | 2014-12-18 |
EP3010925A1 (en) | 2016-04-27 |
US9029367B2 (en) | 2015-05-12 |
CA2910415A1 (en) | 2014-12-24 |
TWI639607B (zh) | 2018-11-01 |
ES2657905T3 (es) | 2018-03-07 |
TW201536793A (zh) | 2015-10-01 |
BR112015029348A2 (pt) | 2017-07-25 |
AU2014281032B2 (en) | 2016-09-29 |
EA027880B1 (ru) | 2017-09-29 |
US20150210716A1 (en) | 2015-07-30 |
EP3010925B1 (en) | 2017-10-04 |
AU2014281032A1 (en) | 2015-11-12 |
EA201592183A1 (ru) | 2016-05-31 |
KR20160009052A (ko) | 2016-01-25 |
KR101780140B1 (ko) | 2017-09-19 |
JP2016522254A (ja) | 2016-07-28 |
WO2014204730A1 (en) | 2014-12-24 |
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