CN105263923B - 嘧啶化合物及它们作为γ分泌酶调节剂的用途 - Google Patents
嘧啶化合物及它们作为γ分泌酶调节剂的用途 Download PDFInfo
- Publication number
- CN105263923B CN105263923B CN201480032083.0A CN201480032083A CN105263923B CN 105263923 B CN105263923 B CN 105263923B CN 201480032083 A CN201480032083 A CN 201480032083A CN 105263923 B CN105263923 B CN 105263923B
- Authority
- CN
- China
- Prior art keywords
- methyl
- pyrimidine
- groups
- phenyl
- imidazole
- 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(C)(C)*CC1C*CC1 Chemical compound CC(C)C(C)(C)*CC1C*CC1 0.000 description 6
- BYCPUOJBUFPSKH-FBVCYTKGSA-N CC/C(/N=C(\N)/NC(/C=C\C(\[n]1cnc(C)c1)=C(/C)\OC)=C)=C/C(C(OCC)=C)=C Chemical compound CC/C(/N=C(\N)/NC(/C=C\C(\[n]1cnc(C)c1)=C(/C)\OC)=C)=C/C(C(OCC)=C)=C BYCPUOJBUFPSKH-FBVCYTKGSA-N 0.000 description 1
- LRBDGKIVGQSDHM-UHFFFAOYSA-N CCOC(c1nc(Cl)nc(COC)c1)=C Chemical compound CCOC(c1nc(Cl)nc(COC)c1)=C LRBDGKIVGQSDHM-UHFFFAOYSA-N 0.000 description 1
- ZEAGQRSSDAMPOI-SPGFALGASA-N Cc(nc1)c[n]1C(C(CC(N)=C1)[F]C(COCC(/C=C(/CN(CC2)CCC2(F)F)\N)=N)(F)F)=C1OC Chemical compound Cc(nc1)c[n]1C(C(CC(N)=C1)[F]C(COCC(/C=C(/CN(CC2)CCC2(F)F)\N)=N)(F)F)=C1OC ZEAGQRSSDAMPOI-SPGFALGASA-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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE1350685-2 | 2013-06-04 | ||
| SE1350685 | 2013-06-04 | ||
| PCT/EP2014/061503 WO2014195323A1 (en) | 2013-06-04 | 2014-06-03 | Pyrimidine compounds and their use as gamma secretase modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105263923A CN105263923A (zh) | 2016-01-20 |
| CN105263923B true CN105263923B (zh) | 2017-06-23 |
Family
ID=50877325
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201480032083.0A Expired - Fee Related CN105263923B (zh) | 2013-06-04 | 2014-06-03 | 嘧啶化合物及它们作为γ分泌酶调节剂的用途 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US9439904B2 (https=) |
| EP (1) | EP3004079B1 (https=) |
| JP (1) | JP6368777B2 (https=) |
| CN (1) | CN105263923B (https=) |
| DK (1) | DK3004079T3 (https=) |
| ES (1) | ES2665421T3 (https=) |
| NO (1) | NO3004079T3 (https=) |
| PL (1) | PL3004079T3 (https=) |
| WO (1) | WO2014195323A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3481829B1 (en) * | 2016-07-08 | 2021-04-07 | H. Hoffnabb-La Roche Ag | Fused pyrimidine derivatives |
| 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 |
| CA3214360A1 (en) | 2021-03-23 | 2022-09-29 | Halia Therapeutics, Inc. | Pyrimidine derivatives useful as lrrk2 kinase inhibitors |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000025780A1 (en) * | 1998-10-29 | 2000-05-11 | Bristol-Myers Squibb Company | Compounds derived from an amine nucleus that are inhibitors of impdh enzyme |
| WO2007053452A1 (en) * | 2005-11-01 | 2007-05-10 | Targegen, Inc. | Bi-aryl meta-pyrimidine inhibitors of kinases |
| WO2009103652A1 (en) * | 2008-02-22 | 2009-08-27 | F. Hoffmann-La Roche Ag | Modulators for amyloid beta |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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. |
| US20080153817A1 (en) | 2003-08-07 | 2008-06-26 | Dirk Beher | Treatment for Alzheimer's Disease and Related Conditions |
| DE602004023762D1 (de) | 2003-12-03 | 2009-12-03 | Merck Sharp & Dohme | Für die behandlung von alzheimer-krankheit und ähnlichen leiden geeignete 1-alkyl-3-thiosubstituierte indol-2-alkinsäuren |
| MY149038A (en) * | 2004-05-26 | 2013-07-15 | Eisai R&D Man Co Ltd | Cinnamide compound |
| WO2007125364A1 (en) | 2006-04-26 | 2007-11-08 | Merck Sharp & Dohme Limited | Piperidines and related compounds for treatment of alzheimer’s disease |
| KR20090018963A (ko) | 2006-05-19 | 2009-02-24 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 우레아계 신나미드 유도체 |
| JP2009184924A (ja) | 2006-05-31 | 2009-08-20 | Eisai R & D Management Co Ltd | 生物学的試薬用化合物 |
| JP2010518080A (ja) | 2007-02-08 | 2010-05-27 | メルク・シャープ・エンド・ドーム・コーポレイション | 治療薬 |
| EP2120573A4 (en) | 2007-02-12 | 2011-05-25 | Merck Sharp & Dohme | piperidine |
| CA2676715A1 (en) | 2007-02-12 | 2008-08-21 | Merck & Co., Inc. | Piperazine derivatives for treatment of ad and related conditions |
| EP2166854A4 (en) | 2007-06-13 | 2012-05-16 | Merck Sharp & Dohme | TRIAZONE DERIVATIVES FOR THE TREATMENT OF MORBUS ALZHEIMER AND RELATED SUFFERINGS |
| MX2010001506A (es) | 2007-08-06 | 2010-03-10 | Schering Corp | Moduladores de gamma secretasa. |
| ES2375919T3 (es) | 2008-01-11 | 2012-03-07 | F. Hoffmann-La Roche Ag | Moduladores de beta-amiloide. |
| ES2429517T3 (es) * | 2008-10-09 | 2013-11-15 | F. Hoffmann-La Roche Ag | Moduladores para la beta amiloide |
| CA2742897A1 (en) | 2008-11-06 | 2010-05-14 | Astrazeneca Ab | Modulators of amyloid beta. |
| CN102209537A (zh) | 2008-11-10 | 2011-10-05 | 弗·哈夫曼-拉罗切有限公司 | 杂环γ分泌酶调节剂 |
| 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) |
| JP2012532912A (ja) | 2009-07-15 | 2012-12-20 | ジヤンセン・フアーマシユーチカルズ・インコーポレーテツド | ガンマセクレターゼモジュレーターとしての置換されたトリアゾールおよびイミダゾール誘導体 |
| 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 |
| BR112012017310A2 (pt) | 2010-01-15 | 2016-04-19 | Janssen Pharmaceuticals Inc | derivados de triazol substituídos como moduladores de gama secretase |
| 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 WO PCT/EP2014/061503 patent/WO2014195323A1/en not_active Ceased
- 2014-06-03 ES ES14727562.2T patent/ES2665421T3/es active Active
- 2014-06-03 US US14/895,528 patent/US9439904B2/en not_active Expired - Fee Related
- 2014-06-03 NO NO14727562A patent/NO3004079T3/no unknown
- 2014-06-03 DK DK14727562.2T patent/DK3004079T3/en active
- 2014-06-03 CN CN201480032083.0A patent/CN105263923B/zh not_active Expired - Fee Related
- 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 PL PL14727562T patent/PL3004079T3/pl unknown
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000025780A1 (en) * | 1998-10-29 | 2000-05-11 | Bristol-Myers Squibb Company | Compounds derived from an amine nucleus that are inhibitors of impdh enzyme |
| WO2007053452A1 (en) * | 2005-11-01 | 2007-05-10 | Targegen, Inc. | Bi-aryl meta-pyrimidine inhibitors of kinases |
| WO2009103652A1 (en) * | 2008-02-22 | 2009-08-27 | F. Hoffmann-La Roche Ag | Modulators for amyloid beta |
Also Published As
| Publication number | Publication date |
|---|---|
| NO3004079T3 (https=) | 2018-06-16 |
| PL3004079T3 (pl) | 2018-07-31 |
| US9439904B2 (en) | 2016-09-13 |
| EP3004079A1 (en) | 2016-04-13 |
| US20160129002A1 (en) | 2016-05-12 |
| JP6368777B2 (ja) | 2018-08-01 |
| JP2016520637A (ja) | 2016-07-14 |
| WO2014195323A1 (en) | 2014-12-11 |
| DK3004079T3 (en) | 2018-04-16 |
| CN105263923A (zh) | 2016-01-20 |
| ES2665421T3 (es) | 2018-04-25 |
| EP3004079B1 (en) | 2018-01-17 |
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Legal Events
| Date | Code | Title | Description |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20170623 Termination date: 20210603 |