JP6110937B2 - APP、BACE1、およびBACE2の阻害剤としての複素環式置換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 - Google Patents
APP、BACE1、およびBACE2の阻害剤としての複素環式置換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 Download PDFInfo
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- JP6110937B2 JP6110937B2 JP2015509531A JP2015509531A JP6110937B2 JP 6110937 B2 JP6110937 B2 JP 6110937B2 JP 2015509531 A JP2015509531 A JP 2015509531A JP 2015509531 A JP2015509531 A JP 2015509531A JP 6110937 B2 JP6110937 B2 JP 6110937B2
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- Prior art keywords
- difluorophenyl
- mmol
- compound
- hexahydropyrano
- methyl
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- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- DRUZLDCISSQJRK-BPQIPLTHSA-N C[C@@]1(C[C@H](c2n[n](C)cc2)OC2)[C@@]2(c(ccc(F)c2)c2F)N=C(N)SC1 Chemical compound C[C@@]1(C[C@H](c2n[n](C)cc2)OC2)[C@@]2(c(ccc(F)c2)c2F)N=C(N)SC1 DRUZLDCISSQJRK-BPQIPLTHSA-N 0.000 description 1
- 0 C[C@](C[C@](*)OC1)([C@@](*)S2)[C@@]1(c(c(F)c1)ccc1F)NC2=N Chemical compound C[C@](C[C@](*)OC1)([C@@](*)S2)[C@@]1(c(c(F)c1)ccc1F)NC2=N 0.000 description 1
Classifications
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- 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
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- 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
- A61K31/542—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 heterocyclic ring systems
-
- A—HUMAN NECESSITIES
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- A61P25/08—Antiepileptics; Anticonvulsants
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Anesthesiology (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Ophthalmology & Optometry (AREA)
- Endocrinology (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261642480P | 2012-05-04 | 2012-05-04 | |
| US61/642,480 | 2012-05-04 | ||
| PCT/IB2013/053178 WO2013164730A1 (en) | 2012-05-04 | 2013-04-22 | Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin- 2 -amine compounds as inhibitors of app, bace1 and bace 2. |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015520140A JP2015520140A (ja) | 2015-07-16 |
| JP2015520140A5 JP2015520140A5 (enExample) | 2016-06-16 |
| JP6110937B2 true JP6110937B2 (ja) | 2017-04-05 |
Family
ID=48536971
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015509531A Expired - Fee Related JP6110937B2 (ja) | 2012-05-04 | 2013-04-22 | APP、BACE1、およびBACE2の阻害剤としての複素環式置換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 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US8962616B2 (enExample) |
| EP (1) | EP2852597B1 (enExample) |
| JP (1) | JP6110937B2 (enExample) |
| AR (1) | AR090928A1 (enExample) |
| CA (1) | CA2872154C (enExample) |
| ES (1) | ES2585262T3 (enExample) |
| TW (1) | TW201406765A (enExample) |
| UY (1) | UY34778A (enExample) |
| WO (1) | WO2013164730A1 (enExample) |
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| WO2013030713A1 (en) | 2011-08-31 | 2013-03-07 | Pfizer Inc. | Hexahydropyrano [3,4-d][1,3] thiazin-2-amine compounds |
| WO2013164730A1 (en) * | 2012-05-04 | 2013-11-07 | Pfizer Inc. | Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin- 2 -amine compounds as inhibitors of app, bace1 and bace 2. |
| JP2015529239A (ja) | 2012-09-20 | 2015-10-05 | ファイザー・インク | アルキル置換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 |
| WO2014091352A1 (en) | 2012-12-11 | 2014-06-19 | Pfizer Inc. | Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds as inhibitors of bace1 |
| CA2893333C (en) * | 2012-12-19 | 2017-10-24 | Pfizer Inc. | Carbocyclic-and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| WO2014120658A1 (en) | 2013-01-29 | 2014-08-07 | Amgen Inc. | Fused multicyclic 3-amino-5,6-dihydro-2h-1,4-thiazine derivatives and their use as beta-secretase inhibitors |
| EP2956458B1 (en) | 2013-02-13 | 2017-08-09 | Pfizer Inc | Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| US9233981B1 (en) * | 2013-02-15 | 2016-01-12 | Pfizer Inc. | Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| 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 |
| JP6374889B2 (ja) | 2013-03-08 | 2018-08-15 | 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過フッ素化シクロプロピル縮合1,3−オキサジン−2−アミン化合物、及び使用方法 |
| JO3318B1 (ar) | 2013-06-18 | 2019-03-13 | Lilly Co Eli | مثبطات bace |
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| CA2944971C (en) | 2014-04-10 | 2019-05-07 | Pfizer Inc. | 2-amino-6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8h)-yl-1,3-thiazol-4-yl amides |
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| EP3353182A1 (en) * | 2015-09-24 | 2018-08-01 | Pfizer Inc | Tetrahydropyrano[3,4-d][1,3]oxazin derivatives and their use as bace inhibitors |
| CA3047286A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Oxazine derivatives as beta-secretase inhibitors and methods of use |
| EP3555085B1 (en) | 2016-12-15 | 2020-12-02 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| EP3555106B1 (en) | 2016-12-15 | 2022-03-09 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
| MX387729B (es) | 2016-12-15 | 2025-03-18 | Amgen Inc | Derivados de dióxido de 1,4-tiazina y dióxido 1,2,4-tiadiazina como inhibidores de beta-secretasa y métodos de uso. |
| EP3555084B1 (en) | 2016-12-15 | 2022-03-16 | Amgen Inc. | Thiazine derivatives as beta-secretase inhibitors and methods of use |
| 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 |
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-
2013
- 2013-04-22 WO PCT/IB2013/053178 patent/WO2013164730A1/en not_active Ceased
- 2013-04-22 JP JP2015509531A patent/JP6110937B2/ja not_active Expired - Fee Related
- 2013-04-22 ES ES13725822.4T patent/ES2585262T3/es active Active
- 2013-04-22 CA CA2872154A patent/CA2872154C/en not_active Expired - Fee Related
- 2013-04-22 EP EP13725822.4A patent/EP2852597B1/en not_active Not-in-force
- 2013-05-02 TW TW102115730A patent/TW201406765A/zh unknown
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- 2013-05-03 AR ARP130101513A patent/AR090928A1/es unknown
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|---|---|
| WO2013164730A1 (en) | 2013-11-07 |
| JP2015520140A (ja) | 2015-07-16 |
| US20130296308A1 (en) | 2013-11-07 |
| EP2852597A1 (en) | 2015-04-01 |
| AR090928A1 (es) | 2014-12-17 |
| US8962616B2 (en) | 2015-02-24 |
| ES2585262T3 (es) | 2016-10-04 |
| US20150133438A1 (en) | 2015-05-14 |
| CA2872154C (en) | 2016-08-23 |
| TW201406765A (zh) | 2014-02-16 |
| CA2872154A1 (en) | 2013-11-07 |
| UY34778A (es) | 2013-12-31 |
| EP2852597B1 (en) | 2016-06-08 |
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