JP6368777B2 - ピリミジン化合物およびガンマセクレターゼモジュレーターとしてのその使用 - Google Patents
ピリミジン化合物およびガンマセクレターゼモジュレーターとしてのその使用 Download PDFInfo
- Publication number
- JP6368777B2 JP6368777B2 JP2016517275A JP2016517275A JP6368777B2 JP 6368777 B2 JP6368777 B2 JP 6368777B2 JP 2016517275 A JP2016517275 A JP 2016517275A JP 2016517275 A JP2016517275 A JP 2016517275A JP 6368777 B2 JP6368777 B2 JP 6368777B2
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- methoxy
- imidazol
- trifluoroethoxy
- mmol
- 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 *c(c(Cl)nc(Cl)n1)c1Cl Chemical compound *c(c(Cl)nc(Cl)n1)c1Cl 0.000 description 7
- AKALAVDNYHGPHY-UHFFFAOYSA-N CC(C)Nc1nc(Cl)nc(COCC(F)(F)F)c1 Chemical compound CC(C)Nc1nc(Cl)nc(COCC(F)(F)F)c1 AKALAVDNYHGPHY-UHFFFAOYSA-N 0.000 description 1
- WXTDETIAYNQYPU-UHFFFAOYSA-N CC(c1nc(Nc2ccc(-c3cnnc(C)c3)c(OC)c2)nc(COCC(C2)CC2(F)F)c1)=O Chemical compound CC(c1nc(Nc2ccc(-c3cnnc(C)c3)c(OC)c2)nc(COCC(C2)CC2(F)F)c1)=O WXTDETIAYNQYPU-UHFFFAOYSA-N 0.000 description 1
- KGXMPDQOLBVYBT-UHFFFAOYSA-N CCOC(C1)(C1(F)F)c1nc(Nc(cc2OC)ccc2-[n]2cnc(C)c2)nc(C(C)(C)O)c1 Chemical compound CCOC(C1)(C1(F)F)c1nc(Nc(cc2OC)ccc2-[n]2cnc(C)c2)nc(C(C)(C)O)c1 KGXMPDQOLBVYBT-UHFFFAOYSA-N 0.000 description 1
- GCAKQQJWCMBUIE-UHFFFAOYSA-N CCOC(Cc1cc(COCC(F)(F)F)nc(Nc(cc2)cc(OC)c2-[n]2cnc(C)c2)n1)=O Chemical compound CCOC(Cc1cc(COCC(F)(F)F)nc(Nc(cc2)cc(OC)c2-[n]2cnc(C)c2)n1)=O GCAKQQJWCMBUIE-UHFFFAOYSA-N 0.000 description 1
- CGBHNDATBBEZBV-UHFFFAOYSA-N CCOC(c1cc(COCC2CC2)nc(Nc(cc2)cc(OC)c2-[n]2cnc(C)c2)n1)=C Chemical compound CCOC(c1cc(COCC2CC2)nc(Nc(cc2)cc(OC)c2-[n]2cnc(C)c2)n1)=C CGBHNDATBBEZBV-UHFFFAOYSA-N 0.000 description 1
- NQHFTZIIOJKBOS-UHFFFAOYSA-O CC[OH+]C(c1nc(Cl)nc(C(C)OCC(F)(F)F)c1)=C Chemical compound CC[OH+]C(c1nc(Cl)nc(C(C)OCC(F)(F)F)c1)=C NQHFTZIIOJKBOS-UHFFFAOYSA-O 0.000 description 1
- BKARZTSOFHUZDW-UHFFFAOYSA-N Cc(nc1)c[n]1-c(c(OC)c1)ccc1Nc1nc(C(C2CC2)O)cc(COCC(F)(F)F)n1 Chemical compound Cc(nc1)c[n]1-c(c(OC)c1)ccc1Nc1nc(C(C2CC2)O)cc(COCC(F)(F)F)n1 BKARZTSOFHUZDW-UHFFFAOYSA-N 0.000 description 1
- AGCLXJHYJKAFKF-UHFFFAOYSA-N FC(COCc1cc(NC2COC2)nc(Cl)n1)(F)F Chemical compound FC(COCc1cc(NC2COC2)nc(Cl)n1)(F)F AGCLXJHYJKAFKF-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P25/16—Anti-Parkinson drugs
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE1350685 | 2013-06-04 | ||
| SE1350685-2 | 2013-06-04 | ||
| PCT/EP2014/061503 WO2014195323A1 (en) | 2013-06-04 | 2014-06-03 | Pyrimidine compounds and their use as gamma secretase modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016520637A JP2016520637A (ja) | 2016-07-14 |
| JP2016520637A5 JP2016520637A5 (enExample) | 2017-06-01 |
| JP6368777B2 true JP6368777B2 (ja) | 2018-08-01 |
Family
ID=50877325
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016517275A Expired - Fee Related JP6368777B2 (ja) | 2013-06-04 | 2014-06-03 | ピリミジン化合物およびガンマセクレターゼモジュレーターとしてのその使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US9439904B2 (enExample) |
| EP (1) | EP3004079B1 (enExample) |
| JP (1) | JP6368777B2 (enExample) |
| CN (1) | CN105263923B (enExample) |
| DK (1) | DK3004079T3 (enExample) |
| ES (1) | ES2665421T3 (enExample) |
| NO (1) | NO3004079T3 (enExample) |
| PL (1) | PL3004079T3 (enExample) |
| WO (1) | WO2014195323A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6975514B2 (ja) * | 2016-07-08 | 2021-12-01 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 縮合ピリミジン誘導体 |
| CN108191776A (zh) * | 2018-01-22 | 2018-06-22 | 无锡富泽药业有限公司 | 一种尿嘧啶的绿色生产工艺 |
| WO2020247707A1 (en) * | 2019-06-05 | 2020-12-10 | Chunyu Wang | SYSTEMS AND METHOD FOR INHIBITING γ-SECRETASE PRODUCTION OF AMYLOID-β PEPTIDES |
| US12297244B2 (en) | 2019-06-05 | 2025-05-13 | Rensselaer Polytechnic Institute | Systems and methods for inhibiting γ-secretase production of amyloid-β peptides |
| CN110372603A (zh) * | 2019-06-24 | 2019-10-25 | 南京普锐达医药科技有限公司 | 一种2-氯-5-氟-6-乙基嘧啶的合成方法 |
| CN113149977A (zh) | 2020-01-22 | 2021-07-23 | 苏州爱科百发生物医药技术有限公司 | 一类呼吸道合胞病毒抑制剂的合成与用途 |
| MX2023011027A (es) | 2021-03-23 | 2023-09-27 | Halia Therapeutics Inc | Derivados de pirimidina utiles como inhibidores de la proteina cinasa de repeticion 2 rica en leucina (lrrk2). |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2002528499A (ja) * | 1998-10-29 | 2002-09-03 | ブリストル−マイヤーズ スクイブ カンパニー | Impdh酵素のインヒビターであるアミノ核誘導化合物 |
| ITMI20030312A1 (it) | 2003-02-21 | 2004-08-22 | Chiesi Farma Spa | Derivati di acidi 2-fenil-2-alchil-acetici per il trattamento della malattia di alzheimer. |
| ATE464048T1 (de) | 2003-08-07 | 2010-04-15 | Merck Sharp & Dohme | Behandlung von alzheimer-krankheit und verwandten zuständen |
| JP2007513128A (ja) | 2003-12-03 | 2007-05-24 | メルク エンド カムパニー インコーポレーテッド | アルツハイマー病および関連状態の治療に有用な1−アルキル−3−チオ置換インドール−2−アルキン酸 |
| US7667041B2 (en) | 2004-05-26 | 2010-02-23 | Eisai R&D Management Co., Ltd. | Cinnamide compound |
| MY167260A (en) * | 2005-11-01 | 2018-08-14 | Targegen Inc | Bi-aryl meta-pyrimidine inhibitors of kinases |
| CA2649996A1 (en) | 2006-04-26 | 2007-11-08 | Merck Sharp & Dohme Limited | Piperidines and related compounds for treatment of alzheimer's disease |
| AU2007252643A1 (en) | 2006-05-19 | 2007-11-29 | Eisai R & D Management Co., Ltd. | Urea type cinnamide derivative |
| JP2009184924A (ja) | 2006-05-31 | 2009-08-20 | Eisai R & D Management Co Ltd | 生物学的試薬用化合物 |
| WO2008097538A1 (en) | 2007-02-08 | 2008-08-14 | Merck & Co., Inc. | Therapeutic agents |
| CA2676920A1 (en) | 2007-02-12 | 2008-08-21 | Merck & Co., Inc. | Piperidine derivatives |
| CA2676715A1 (en) | 2007-02-12 | 2008-08-21 | Merck & Co., Inc. | Piperazine derivatives for treatment of ad and related conditions |
| WO2008156580A1 (en) | 2007-06-13 | 2008-12-24 | Merck & Co., Inc. | Triazole derivatives for treating alzheimer's disease and related conditions |
| US20110009392A1 (en) | 2007-08-06 | 2011-01-13 | Schering Corporation | Gamma secretase modulators |
| ATE535515T1 (de) | 2008-01-11 | 2011-12-15 | Hoffmann La Roche | Modulatoren für amyloid beta |
| RU2010137300A (ru) | 2008-02-22 | 2012-03-27 | Ф. Хоффманн-Ля Рош Аг (Ch) | Модуляторы бета-амилоида |
| CN102177151A (zh) * | 2008-10-09 | 2011-09-07 | 弗·哈夫曼-拉罗切有限公司 | β-淀粉样蛋白的调节剂 |
| CN102272133A (zh) | 2008-11-06 | 2011-12-07 | 阿斯利康(瑞典)有限公司 | 淀粉样β的调节剂 |
| MX2011004954A (es) | 2008-11-10 | 2011-05-30 | Hoffmann La Roche | Moduladores heterociclicos de gamma-secretasa. |
| TW201030002A (en) | 2009-01-16 | 2010-08-16 | Bristol Myers Squibb Co | Bicyclic compounds for the reduction of beta-amyloid production |
| UY32622A (es) | 2009-05-12 | 2010-12-31 | Astrazeneca Ab | Nuevos compuestos para el tratamiento de patologías relacionadas con ab(beta) |
| EA021047B1 (ru) | 2009-07-15 | 2015-03-31 | Янссен Фармасьютикалз, Инк. | Замещенные производные триазола и имидазола в качестве модуляторов гамма-секретазы |
| TWI468402B (zh) | 2009-07-31 | 2015-01-11 | 必治妥美雅史谷比公司 | 降低β-類澱粉生成之化合物 |
| MX2012008260A (es) | 2010-01-15 | 2012-08-17 | Janssen Pharmaceuticals Inc | Novedosos derivados de triazol sustituidos como moduladores de la gamma secretasa. |
| US20110190269A1 (en) | 2010-02-01 | 2011-08-04 | Karlheinz Baumann | Gamma secretase modulators |
| TW201206946A (en) | 2010-07-15 | 2012-02-16 | Bristol Myers Squibb Co | Compounds for the reduction of beta-amyloid production |
-
2014
- 2014-06-03 NO NO14727562A patent/NO3004079T3/no unknown
- 2014-06-03 WO PCT/EP2014/061503 patent/WO2014195323A1/en not_active Ceased
- 2014-06-03 PL PL14727562T patent/PL3004079T3/pl unknown
- 2014-06-03 DK DK14727562.2T patent/DK3004079T3/en active
- 2014-06-03 ES ES14727562.2T patent/ES2665421T3/es active Active
- 2014-06-03 JP JP2016517275A patent/JP6368777B2/ja not_active Expired - Fee Related
- 2014-06-03 EP EP14727562.2A patent/EP3004079B1/en active Active
- 2014-06-03 US US14/895,528 patent/US9439904B2/en not_active Expired - Fee Related
- 2014-06-03 CN CN201480032083.0A patent/CN105263923B/zh not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| NO3004079T3 (enExample) | 2018-06-16 |
| ES2665421T3 (es) | 2018-04-25 |
| US20160129002A1 (en) | 2016-05-12 |
| WO2014195323A1 (en) | 2014-12-11 |
| JP2016520637A (ja) | 2016-07-14 |
| EP3004079B1 (en) | 2018-01-17 |
| EP3004079A1 (en) | 2016-04-13 |
| CN105263923A (zh) | 2016-01-20 |
| CN105263923B (zh) | 2017-06-23 |
| US9439904B2 (en) | 2016-09-13 |
| DK3004079T3 (en) | 2018-04-16 |
| PL3004079T3 (pl) | 2018-07-31 |
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