JO3569B1 - مركبات بروبيل حلقي متحد مع ثيازين-2-أمين كمثبطات انزيم بيتا سكريتاز وطرق استخدامها - Google Patents
مركبات بروبيل حلقي متحد مع ثيازين-2-أمين كمثبطات انزيم بيتا سكريتاز وطرق استخدامهاInfo
- Publication number
- JO3569B1 JO3569B1 JOP/2015/0190A JOP20150190A JO3569B1 JO 3569 B1 JO3569 B1 JO 3569B1 JO P20150190 A JOP20150190 A JO P20150190A JO 3569 B1 JO3569 B1 JO 3569B1
- Authority
- JO
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- Prior art keywords
- compounds
- beta
- methods
- bace
- thiazin
- Prior art date
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Classifications
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- 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
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- 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
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- 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
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- 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
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- 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
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
- C07D279/08—1,3-Thiazines; Hydrogenated 1,3-thiazines condensed with carbocyclic rings or ring systems
-
- 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
- C07D417/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D417/14—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 three or more hetero rings
-
- 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
-
- 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
- C07D513/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
يوفر هذا الاختراع فئة جديدة من مركبات مفيدة لتعديل نشاط بيتا سكريتاز (BACE). المركبات بها الصيغة العامة I: (I) فيها المتغيرات A4, A5, A6, A8, وكل من Ra, Rb, R1, R2, R3 وR7 من الصيغة (I) تم تعريفها في الوصف التفصيلي. يوفر هذا الاختراع تركيبات صيدلانية متضمنة مركبات، واستخدامات هذه المركبات وتركيبات لعلاج اضكطرابات و/ أو حالات متعلقة بتكوين وترسيب لوحة بيتا، الناتج عن النشاط البيولوجي لـ BACE. حيث تشمل الاضطرابات التي يسببها BACE، على سبيل المثال، مرض الزهايمر، والعجز المعرفي، العاهات الذهنية وانفصام الشخصية وغيرها من حالات الجهاز العصبي المركزي. يوفر الاختراع ايضا مركبات ذات الصيغة II و III، والصيغ فرعية لتجسيمات منها، مركبات وسيطة وطرق لتحضير مركبات الاختراع.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US201462035269P | 2014-08-08 | 2014-08-08 |
Publications (1)
Publication Number | Publication Date |
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JO3569B1 true JO3569B1 (ar) | 2020-07-05 |
Family
ID=54150645
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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JOP/2015/0190A JO3569B1 (ar) | 2014-08-08 | 2015-08-09 | مركبات بروبيل حلقي متحد مع ثيازين-2-أمين كمثبطات انزيم بيتا سكريتاز وطرق استخدامها |
Country Status (12)
Country | Link |
---|---|
US (2) | US9550762B2 (ar) |
EP (1) | EP3177618A1 (ar) |
JP (1) | JP6576433B2 (ar) |
CN (1) | CN106795147B (ar) |
AR (1) | AR101483A1 (ar) |
AU (1) | AU2015301028B2 (ar) |
CA (1) | CA2957544C (ar) |
JO (1) | JO3569B1 (ar) |
MX (1) | MX2017001794A (ar) |
TW (1) | TWI614250B (ar) |
UY (1) | UY36263A (ar) |
WO (1) | WO2016022724A1 (ar) |
Families Citing this family (11)
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AU2015301028B2 (en) | 2014-08-08 | 2019-09-26 | Amgen Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
WO2017024180A1 (en) | 2015-08-06 | 2017-02-09 | Amgen Inc. | Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
ES2910367T3 (es) | 2016-12-15 | 2022-05-12 | Amgen Inc | Derivados de tiazina y oxazina bicíclicos como inhibidores de beta-secretasa y métodos de uso |
AU2017376441B2 (en) | 2016-12-15 | 2021-10-14 | Amgen Inc. | Oxazine derivatives as beta-secretase inhibitors and methods of use |
WO2018112083A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Thiazine derivatives as beta-secretase inhibitors and methods of use |
JP7149271B2 (ja) | 2016-12-15 | 2022-10-06 | アムジエン・インコーポレーテツド | β-セクレターゼ阻害剤としての1,4-チアジンジオキシドおよび1,2,4-チアジアジンジオキシド誘導体ならびに使用方法 |
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EP2935256B1 (en) | 2012-12-19 | 2018-01-24 | Bristol-Myers Squibb Company | 4,6-diarylaminothiazines as bace1 inhibitors and their use for the reduction of beta-amyloid production |
AU2013363151A1 (en) | 2012-12-20 | 2015-06-04 | Merck Sharp & Dohme Corp. | C5, C6 oxacyclic-fused iminothiazine dioxide compounds as BACE inhibitors |
US9580396B2 (en) | 2012-12-21 | 2017-02-28 | Merck Sharp & Dohme Corp. | C6-spiro iminothiadiazine dioxides as BACE inhibitors, compositions, and their use |
EP2948446A1 (en) | 2013-01-22 | 2015-12-02 | F. Hoffmann-La Roche AG | Fluoro-[1,3]oxazines as bace1 inhibitors |
AU2014223334C1 (en) | 2013-03-01 | 2018-10-18 | Amgen Inc. | Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
EP2964644B1 (en) | 2013-03-08 | 2018-12-26 | Amgen, Inc. | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
CA2900433C (en) | 2013-04-11 | 2021-06-22 | F. Hoffmann-La Roche Ag | Bace1 inhibitors |
BR112015026759A2 (pt) | 2013-04-26 | 2017-07-25 | Hoffmann La Roche | síntese de inibidores bace |
TW201623295A (zh) | 2014-04-11 | 2016-07-01 | 塩野義製藥股份有限公司 | 具有bace1抑制活性之二氫噻及二氫衍生物 |
WO2016001266A1 (en) | 2014-07-04 | 2016-01-07 | F. Hoffmann-La Roche Ag | Fluoro-[1,3]oxazines as bace1 inhibitors |
AU2015301028B2 (en) | 2014-08-08 | 2019-09-26 | Amgen Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
-
2015
- 2015-08-05 AU AU2015301028A patent/AU2015301028B2/en active Active
- 2015-08-05 WO PCT/US2015/043868 patent/WO2016022724A1/en active Application Filing
- 2015-08-05 US US14/819,256 patent/US9550762B2/en active Active
- 2015-08-05 MX MX2017001794A patent/MX2017001794A/es unknown
- 2015-08-05 CN CN201580054674.2A patent/CN106795147B/zh active Active
- 2015-08-05 CA CA2957544A patent/CA2957544C/en active Active
- 2015-08-05 EP EP15766951.6A patent/EP3177618A1/en not_active Withdrawn
- 2015-08-05 JP JP2017506879A patent/JP6576433B2/ja active Active
- 2015-08-07 AR ARP150102557A patent/AR101483A1/es unknown
- 2015-08-07 UY UY0001036263A patent/UY36263A/es not_active Application Discontinuation
- 2015-08-07 TW TW104125848A patent/TWI614250B/zh active
- 2015-08-09 JO JOP/2015/0190A patent/JO3569B1/ar active
-
2016
- 2016-11-17 US US15/354,877 patent/US20170267673A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
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CN106795147B (zh) | 2020-09-22 |
TW201619154A (zh) | 2016-06-01 |
TWI614250B (zh) | 2018-02-11 |
US20160046618A1 (en) | 2016-02-18 |
MX2017001794A (es) | 2017-06-29 |
AU2015301028A1 (en) | 2017-03-09 |
JP6576433B2 (ja) | 2019-09-18 |
UY36263A (es) | 2016-02-29 |
US9550762B2 (en) | 2017-01-24 |
CA2957544A1 (en) | 2016-02-11 |
EP3177618A1 (en) | 2017-06-14 |
CA2957544C (en) | 2023-01-24 |
US20170267673A1 (en) | 2017-09-21 |
WO2016022724A1 (en) | 2016-02-11 |
JP2017523223A (ja) | 2017-08-17 |
AR101483A1 (es) | 2016-12-21 |
AU2015301028B2 (en) | 2019-09-26 |
CN106795147A (zh) | 2017-05-31 |
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