JP6895424B2 - Ｂａｃｅ１阻害剤 - Google Patents
Ｂａｃｅ１阻害剤 Download PDFInfo
- Publication number
- JP6895424B2 JP6895424B2 JP2018506862A JP2018506862A JP6895424B2 JP 6895424 B2 JP6895424 B2 JP 6895424B2 JP 2018506862 A JP2018506862 A JP 2018506862A JP 2018506862 A JP2018506862 A JP 2018506862A JP 6895424 B2 JP6895424 B2 JP 6895424B2
- Authority
- JP
- Japan
- Prior art keywords
- fluorophenyl
- trimethyl
- tetrahydro
- isothiazolo
- oxide
- Prior art date
- 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.)
- Expired - Fee Related
Links
- 0 CC(*)(*)C(*)*(C*)=S(C1)(C(*)(*)C(*)=N[C@]1(*)c1cc(BrC)ccc1*)=O Chemical compound CC(*)(*)C(*)*(C*)=S(C1)(C(*)(*)C(*)=N[C@]1(*)c1cc(BrC)ccc1*)=O 0.000 description 10
- VTHGSCVSLASTMX-OZAOTIOVSA-N CC(C)(C(NC(OC(C)(C)N1)=O)=N[C@@](C)([C@@H]2CCN=3)c4cc1ccc4F)[S@]2=3=O Chemical compound CC(C)(C(NC(OC(C)(C)N1)=O)=N[C@@](C)([C@@H]2CCN=3)c4cc1ccc4F)[S@]2=3=O VTHGSCVSLASTMX-OZAOTIOVSA-N 0.000 description 5
- GFTZOVWMBHUJPG-INZNITTPSA-N CC(C)(C(N)=N[C@@](C)(C1CCN=2)c3cc(NC(c4c(C)cc(C)cn4)=O)ccc3F)[S@]1=2=O Chemical compound CC(C)(C(N)=N[C@@](C)(C1CCN=2)c3cc(NC(c4c(C)cc(C)cn4)=O)ccc3F)[S@]1=2=O GFTZOVWMBHUJPG-INZNITTPSA-N 0.000 description 1
- TVORWXLXWSTRPQ-KSLFGHPJSA-N CC(C)(C(N)=N[C@@](C)(C1CCN=2)c3cc(NC(c4cnc(C)nc4)=O)ccc3F)[S@]1=2=O Chemical compound CC(C)(C(N)=N[C@@](C)(C1CCN=2)c3cc(NC(c4cnc(C)nc4)=O)ccc3F)[S@]1=2=O TVORWXLXWSTRPQ-KSLFGHPJSA-N 0.000 description 1
- FFWZIDJYTKTCMJ-INCWNZBPSA-N CC(C)(C(N)=N[C@@](C)([C@@H]1CCN=2)c3cc(NC(c(nc4)c(C)cc4OC)=O)ccc3F)[S@]1=2=O Chemical compound CC(C)(C(N)=N[C@@](C)([C@@H]1CCN=2)c3cc(NC(c(nc4)c(C)cc4OC)=O)ccc3F)[S@]1=2=O FFWZIDJYTKTCMJ-INCWNZBPSA-N 0.000 description 1
- WNYXVVHEPSBAEH-WVSGJHDHSA-N CC(C)(C(N)=N[C@@](C)([C@@H]1CCN=2)c3cc(NC(c(nc4)ccc4Cl)=O)ccc3F)[S@]1=2=O Chemical compound CC(C)(C(N)=N[C@@](C)([C@@H]1CCN=2)c3cc(NC(c(nc4)ccc4Cl)=O)ccc3F)[S@]1=2=O WNYXVVHEPSBAEH-WVSGJHDHSA-N 0.000 description 1
- VFAVDRKPGHTWKT-BFQPASHQSA-N CC(C)(C(N)=N[C@@](C)([C@@H]1CCN=2)c3cc(NC(c(nc4)cnc4OCC(F)F)=O)ccc3F)[S@]1=2=O Chemical compound CC(C)(C(N)=N[C@@](C)([C@@H]1CCN=2)c3cc(NC(c(nc4)cnc4OCC(F)F)=O)ccc3F)[S@]1=2=O VFAVDRKPGHTWKT-BFQPASHQSA-N 0.000 description 1
- ZYHHCTMKCFCYOH-RPWUZVMVSA-N CC(C)(C(N)=N[C@]1(C)c2cc(NC(c(nc3)ccc3OCC(F)F)=O)ccc2F)S[C@]1(CCN)NC Chemical compound CC(C)(C(N)=N[C@]1(C)c2cc(NC(c(nc3)ccc3OCC(F)F)=O)ccc2F)S[C@]1(CCN)NC ZYHHCTMKCFCYOH-RPWUZVMVSA-N 0.000 description 1
- OOCYGPINVMVSOD-SXOMAYOGSA-N CC(C)(C)OC(NC(C(C)(C)S[C@]1(CCN)NC)=N[C@]1(C)c1cc(NC(c(nc2)ccc2Cl)=O)ccc1F)=O Chemical compound CC(C)(C)OC(NC(C(C)(C)S[C@]1(CCN)NC)=N[C@]1(C)c1cc(NC(c(nc2)ccc2Cl)=O)ccc1F)=O OOCYGPINVMVSOD-SXOMAYOGSA-N 0.000 description 1
- UHYODTAHLWTAGM-LQUBDEEZSA-N CC(C)(C)OC(NC(C(C)(C)[S@@]1=CN[C@@]11CCN)=N[C@]1(C)c1cc(NC(c(nc2)ccc2OCC(F)F)=O)ccc1F)=O Chemical compound CC(C)(C)OC(NC(C(C)(C)[S@@]1=CN[C@@]11CCN)=N[C@]1(C)c1cc(NC(c(nc2)ccc2OCC(F)F)=O)ccc1F)=O UHYODTAHLWTAGM-LQUBDEEZSA-N 0.000 description 1
- AXKLJFAORHYJFC-DNOKHDCISA-N CC(C)(C)OC(NC(C(C)(C)[S@]1(=NCC[C@H]11)=O)=N[C@]1(C)c1cc(NC(c(nc2)c(C)cc2OC(F)F)=O)ccc1F)=O Chemical compound CC(C)(C)OC(NC(C(C)(C)[S@]1(=NCC[C@H]11)=O)=N[C@]1(C)c1cc(NC(c(nc2)c(C)cc2OC(F)F)=O)ccc1F)=O AXKLJFAORHYJFC-DNOKHDCISA-N 0.000 description 1
- FLQOVZACLSTKHT-PZHABIFZSA-N CC(C)(C)OC(NC(C(C)(C)[S@]1(=NCC[C@H]11)=O)=N[C@]1(C)c1cc(NC(c(nc2)c(C)cc2OC)=O)ccc1F)=O Chemical compound CC(C)(C)OC(NC(C(C)(C)[S@]1(=NCC[C@H]11)=O)=N[C@]1(C)c1cc(NC(c(nc2)c(C)cc2OC)=O)ccc1F)=O FLQOVZACLSTKHT-PZHABIFZSA-N 0.000 description 1
- AJABEIPOVBJKTG-WADHJSKCSA-N CC(C)(C)OC(NC(C(C)(C)[S@]1(=NCC[C@H]11)=O)=N[C@]1(C)c1cc(NC(c2c(C)cc(C)cn2)=O)ccc1F)=O Chemical compound CC(C)(C)OC(NC(C(C)(C)[S@]1(=NCC[C@H]11)=O)=N[C@]1(C)c1cc(NC(c2c(C)cc(C)cn2)=O)ccc1F)=O AJABEIPOVBJKTG-WADHJSKCSA-N 0.000 description 1
- PMYBVVGKUDUCLP-IKDMDFKBSA-N CC1(C)[S@@]2=CN[C@]2(CCN)[C@@](C)(c2cc(NC(C)(C)O3)ccc2F)N=C1NC3=O Chemical compound CC1(C)[S@@]2=CN[C@]2(CCN)[C@@](C)(c2cc(NC(C)(C)O3)ccc2F)N=C1NC3=O PMYBVVGKUDUCLP-IKDMDFKBSA-N 0.000 description 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
- A61K31/54—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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (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)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15180767.4 | 2015-08-12 | ||
| EP15180767 | 2015-08-12 | ||
| PCT/EP2016/068830 WO2017025491A1 (en) | 2015-08-12 | 2016-08-08 | Bace1 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018522915A JP2018522915A (ja) | 2018-08-16 |
| JP2018522915A5 JP2018522915A5 (https=) | 2019-09-12 |
| JP6895424B2 true JP6895424B2 (ja) | 2021-06-30 |
Family
ID=53835951
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018506862A Expired - Fee Related JP6895424B2 (ja) | 2015-08-12 | 2016-08-08 | Ｂａｃｅ１阻害剤 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US10246468B2 (https=) |
| EP (1) | EP3334742B1 (https=) |
| JP (1) | JP6895424B2 (https=) |
| CN (1) | CN107683283B (https=) |
| WO (1) | WO2017025491A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017025491A1 (en) * | 2015-08-12 | 2017-02-16 | F. Hoffmann-La Roche Ag | Bace1 inhibitors |
| KR102567590B1 (ko) | 2018-09-06 | 2023-08-17 | 다이이찌 산쿄 가부시키가이샤 | 신규 고리형 디뉴클레오티드 유도체 및 그 항체 약물 콘쥬게이트 |
| JP7495430B2 (ja) | 2019-04-17 | 2024-06-04 | バード・アクセス・システムズ，インコーポレーテッド | 長尺状医療部材を安定させるための固定装置およびカテーテルアセンブリの固定方法 |
| CN116059192B (zh) | 2019-11-13 | 2024-10-29 | 润佳（苏州）医药科技有限公司 | 同位素富集的3-氨基-1-丙磺酸及其衍生物的用途 |
| AU2024222719A1 (en) | 2023-02-16 | 2025-08-21 | Gasherbrum Bio, Inc. | Heterocyclic glp-1 agonists |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2014111055A (ru) * | 2011-08-22 | 2015-09-27 | Мерк Шарп И Доум Корп. | 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение |
| EP2852596B1 (en) * | 2012-05-21 | 2016-06-22 | Bayer Pharma Aktiengesellschaft | Thienopyrimidines |
| PE20150021A1 (es) * | 2012-05-24 | 2015-01-28 | Hoffmann La Roche | 5-amino[1,4]tiazinas como inhibidores de bace1 |
| CN104968660A (zh) * | 2013-01-22 | 2015-10-07 | 霍夫曼-拉罗奇有限公司 | 作为bace1抑制剂的氟-[1,3]噁嗪类化合物 |
| WO2014150331A1 (en) * | 2013-03-15 | 2014-09-25 | Merck Sharp & Dohme Corp. | S-imino-s-oxo iminothiazine compounds as bace inhibitors, compositions, and their use |
| CN105683199B (zh) * | 2013-12-20 | 2018-06-26 | 豪夫迈·罗氏有限公司 | 5-芳基-1-亚氨基-1-氧代-[1，2，4]噻二嗪 |
| JP6594403B2 (ja) * | 2014-07-25 | 2019-10-23 | エフ．ホフマン−ラ ロシュ アーゲー | ピリジル−トリアザビシクル |
| JP6568937B2 (ja) * | 2014-10-10 | 2019-08-28 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | Ｂａｃｅ１阻害剤 |
| JP6554547B2 (ja) * | 2014-11-03 | 2019-07-31 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | Ｂａｃｅ１阻害剤 |
| WO2017025491A1 (en) * | 2015-08-12 | 2017-02-16 | F. Hoffmann-La Roche Ag | Bace1 inhibitors |
-
2016
- 2016-08-08 WO PCT/EP2016/068830 patent/WO2017025491A1/en not_active Ceased
- 2016-08-08 CN CN201680031828.0A patent/CN107683283B/zh not_active Expired - Fee Related
- 2016-08-08 EP EP16754452.7A patent/EP3334742B1/en not_active Not-in-force
- 2016-08-08 JP JP2018506862A patent/JP6895424B2/ja not_active Expired - Fee Related
- 2016-08-08 US US15/735,890 patent/US10246468B2/en not_active Expired - Fee Related
-
2019
- 2019-02-13 US US16/274,911 patent/US10696691B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| EP3334742A1 (en) | 2018-06-20 |
| US10696691B2 (en) | 2020-06-30 |
| WO2017025491A1 (en) | 2017-02-16 |
| US10246468B2 (en) | 2019-04-02 |
| US20190002476A1 (en) | 2019-01-03 |
| CN107683283A (zh) | 2018-02-09 |
| EP3334742B1 (en) | 2019-05-08 |
| US20190270757A1 (en) | 2019-09-05 |
| JP2018522915A (ja) | 2018-08-16 |
| CN107683283B (zh) | 2021-05-18 |
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