PE20121512A1 - Novedosos derivados de triazol sustituidos como moduladores de la gamma secretasa - Google Patents
Novedosos derivados de triazol sustituidos como moduladores de la gamma secretasaInfo
- Publication number
- PE20121512A1 PE20121512A1 PE2012000992A PE2012000992A PE20121512A1 PE 20121512 A1 PE20121512 A1 PE 20121512A1 PE 2012000992 A PE2012000992 A PE 2012000992A PE 2012000992 A PE2012000992 A PE 2012000992A PE 20121512 A1 PE20121512 A1 PE 20121512A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- gamma secretase
- modulators
- novelty
- triazole derivatives
- Prior art date
Links
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 title abstract 2
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 title abstract 2
- 229940042055 systemic antimycotics triazole derivative Drugs 0.000 title 1
- -1 MORPHOLINYL Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- UGFAIRIUMAVXCW-UHFFFAOYSA-N Carbon monoxide Chemical class [O+]#[C-] UGFAIRIUMAVXCW-UHFFFAOYSA-N 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000030886 Traumatic Brain injury Diseases 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- QBEPLGCTCQKYSU-UHFFFAOYSA-N n-[3-methoxy-4-(2-methylpyridin-4-yl)phenyl]-1-propan-2-yl-5-[3-(trifluoromethyl)piperidin-1-yl]-1,2,4-triazol-3-amine Chemical compound C=1C=C(C=2C=C(C)N=CC=2)C(OC)=CC=1NC(=NN1C(C)C)N=C1N1CCCC(C(F)(F)F)C1 QBEPLGCTCQKYSU-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000009529 traumatic brain injury Effects 0.000 abstract 1
Classifications
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- 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
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- 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
-
- 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- C07D403/10—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 carbon chain containing aromatic rings
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biomedical Technology (AREA)
- Medicinal Chemistry (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
SE REFIERE A UN COMPUESTO DE FORMULA (I) DONDE: HET1 ES UN HETEROCICLO DE FORMULA (a-1), (a-2), ENTRE OTROS; A1 ES CR9 O N; A2, A3 Y A4 SON INDEPENDIENTEMENTE CH O N SIEMPRE QUE MAXIMO DOS DE ELLOS SEAN N; L1 ES O, CARBONILO, NH(C=O), ENTRE OTROS; R1 ES CICLOALQUILO C3-7, ALQUENILO C2-6 O ALQUILO C1-6 OPCIONALMENTE SUSTITUIDO, ENTRE OTROS; L2 ES UN ENLACE DIRECTO, CARBONILO, O, S, ENTRE OTROS; R2 ES MORFOLINILO, PIPERIDINILO, PIPERAZINILO, ENTRE OTROS; R9 ES H, HALO O ALQUILOXI C1-4; R3 ES ALQUILO C1-4; R4, R5, Y R6 SON INDEPENDIENTEMENTE H, O ALQUILO C1-4; Xa ES CH O N; Xb ES O O S. SON COMPUESTOS PREFERIDOS: 5-(2-CLOROFENOXI)-N-[3-METOXI-4-(4-METIL-1H-IMIDAZOL-1-IL)FENIL]-1-(1-METILETIL)-1H-1,2,4-TRIAZOL-3-AMINA; N-[3-METOXI-4-(2-METIL-4-PIRIDINIL)FENIL]-1-(1-METILETIL)-5-[3-(TRIFLUORMETIL)-1-PIPERIDINIL]-1H-1,2,4-TRIAZOL-3-AMINA.2.2HCL.2.7H2O; ENTRE OTROS. REFERIDA ADEMAS A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHO COMPUESTO ES MODULADOR DE LA ENZIMA GAMMA SECRETASA UTIL PARA EL TRATAMIENTO DE ENFERMEDAD DE ALZHEIMER, LESION CEREBRAL TRAUMATICA
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10150892 | 2010-01-15 | ||
| EP10171292 | 2010-07-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20121512A1 true PE20121512A1 (es) | 2012-12-06 |
Family
ID=43569255
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2012000991A PE20121511A1 (es) | 2010-01-15 | 2011-01-12 | Novedosos derivados biciclicos de triazol sustituidos como moduladores de gamma secretasa |
| PE2012000992A PE20121512A1 (es) | 2010-01-15 | 2011-01-12 | Novedosos derivados de triazol sustituidos como moduladores de la gamma secretasa |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2012000991A PE20121511A1 (es) | 2010-01-15 | 2011-01-12 | Novedosos derivados biciclicos de triazol sustituidos como moduladores de gamma secretasa |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US9145399B2 (es) |
| EP (2) | EP2523955B1 (es) |
| JP (2) | JP5824464B2 (es) |
| KR (2) | KR20120123677A (es) |
| CN (2) | CN102803261A (es) |
| AR (2) | AR079904A1 (es) |
| AU (2) | AU2011206635B2 (es) |
| BR (2) | BR112012017310A2 (es) |
| CA (2) | CA2784765A1 (es) |
| CL (2) | CL2012001956A1 (es) |
| EA (2) | EA021776B1 (es) |
| ES (2) | ES2512840T3 (es) |
| IL (2) | IL220840A (es) |
| MX (2) | MX2012008259A (es) |
| NZ (2) | NZ600648A (es) |
| PE (2) | PE20121511A1 (es) |
| PH (2) | PH12012501381A1 (es) |
| SG (2) | SG182506A1 (es) |
| TW (2) | TWI473807B (es) |
| WO (2) | WO2011086099A1 (es) |
| ZA (2) | ZA201205240B (es) |
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| ES2481715T3 (es) | 2009-02-06 | 2014-07-31 | Janssen Pharmaceuticals, Inc. | Compuestos heterocíclicos bicíclicos sustituidos novedosos como moduladores de gamma-secretasa |
| AU2010262036B2 (en) | 2009-05-07 | 2014-10-30 | Cellzome Limited | Novel substituted indazole and aza-indazole derivatives as gamma secretase modulators |
| BRPI1009637A2 (pt) * | 2009-06-05 | 2019-04-30 | Cephalon, Inc | composto, composição e uso de um composto |
| BR112012000915A2 (pt) | 2009-07-15 | 2019-09-24 | Janssen Pharmaceuticals Inc | derivados de triazol e imidazol substituídos como moduladores de gama secretase. |
| EP2343294A1 (en) | 2009-11-30 | 2011-07-13 | Bayer Schering Pharma AG | Substituted triazolopyridines |
| EP2343297A1 (en) | 2009-11-30 | 2011-07-13 | Bayer Schering Pharma AG | Triazolopyridines |
| CA2784765A1 (en) | 2010-01-15 | 2011-07-21 | Janssen Pharmaceuticals, Inc. | Novel substituted bicyclic triazole derivatives as gamma secretase modulators |
| UY33452A (es) | 2010-06-16 | 2012-01-31 | Bayer Schering Pharma Ag | Triazolopiridinas sustituidas |
| SG188296A1 (en) * | 2010-08-27 | 2013-04-30 | Merck Patent Gmbh | Triazolopyrazine derivatives |
| BR112013004746A2 (pt) | 2010-09-02 | 2016-06-07 | Takeda Pharmaceutical | "composto, medicamento, inibidor da produção de beta-amilóide, modulador de gama-secretase, métodos para inibir a produção de beta-amilóide, para modular gama-secretase, e para prevenir ou tratar deficiência cognitiva branda ou mal de alzheimer, e, uso do composto." |
| CN103502225B (zh) | 2011-03-24 | 2015-11-25 | 杨森制药公司 | 作为γ分泌酶调节剂的经取代的三唑基哌嗪以及三唑基哌啶衍生物 |
| AU2012285931B2 (en) | 2011-07-15 | 2017-01-12 | Cellzome Limited | Novel substituted indole derivatives as gamma secretase modulators |
| UA112096C2 (uk) | 2011-12-12 | 2016-07-25 | Байєр Інтеллектуал Проперті Гмбх | Заміщені триазолопіридини та їх застосування як інгібіторів ttk |
| JP6479476B2 (ja) * | 2012-02-21 | 2019-03-06 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | ＳｙｋチロシンキナーゼインヒビターおよびＧＣＮ２セリンキナーゼインヒビターとしての８−置換２−アミノー［１，２，４］トリアゾロ［１，５−Ａ］ピラジン類 |
| EP2822948B1 (en) * | 2012-03-07 | 2016-04-06 | Merck Patent GmbH | Triazolopyrazine derivatives |
| ES2605946T3 (es) | 2012-03-14 | 2017-03-17 | Bayer Intellectual Property Gmbh | Imidazopiridazinas sustituidas |
| KR102096625B1 (ko) | 2012-05-16 | 2020-04-03 | 얀센 파마슈티칼즈, 인코포레이티드 | (무엇보다도) 알츠하이머병의 치료에 유용한 치환 3,4-디하이드로-2h-피리도[1,2-a]피라진-1,6-디온 유도체 |
| CN103508957B (zh) * | 2012-06-25 | 2017-02-08 | 中国科学院上海药物研究所 | 羟乙基吡唑类化合物或氨乙基吡唑类化合物及其制备方法和用途 |
| US20140010783A1 (en) * | 2012-07-06 | 2014-01-09 | Hoffmann-La Roche Inc. | Antiviral compounds |
| EP2687528A1 (en) | 2012-07-17 | 2014-01-22 | Ares Trading S.A. | Fused triazole derivatives as gamma secretase modulators |
| JOP20180012A1 (ar) * | 2012-08-07 | 2019-01-30 | Janssen Pharmaceutica Nv | عملية السلفنة باستخدام نونافلوروبوتانيسولفونيل فلوريد |
| KR102209418B1 (ko) | 2012-12-20 | 2021-01-29 | 얀센 파마슈티카 엔.브이. | 감마 세크레타제 조절 인자로서의 신규 삼환 3,4-디하이드로-2H-피리도[1,2-α]피라진-1,6-디온 유도체 |
| CA2891755C (en) | 2013-01-17 | 2021-10-26 | Janssen Pharmaceutica Nv | Substituted pyrido-piperazinone derivatives as gamma secretase modulators |
| DK3004079T3 (en) | 2013-06-04 | 2018-04-16 | Acturum Real Estate Ab | PYRIMIDE COMPOUNDS AND THEIR USE AS GAMMA SECRETASE MODULATORS |
| JP6368776B2 (ja) * | 2013-06-04 | 2018-08-01 | アクチュラム・ライフ・サイエンス・アクチエボラーグ | トリアゾール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 |
| JP6396438B2 (ja) * | 2013-06-04 | 2018-09-26 | アクチュラム・ライフ・サイエンス・アクチエボラーグ | トリアゾール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 |
| JP2016526534A (ja) | 2013-06-11 | 2016-09-05 | バイエル・ファルマ・アクティエンゲゼルシャフト | 置換トリアゾロピリジンのプロドラッグ誘導体 |
| US10562897B2 (en) | 2014-01-16 | 2020-02-18 | Janssen Pharmaceutica Nv | Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators |
| BR112017011644A2 (pt) | 2014-12-05 | 2018-02-14 | An2H Discovery Ltd | métodos e composições de ativação da ligase parkina |
| KR101594470B1 (ko) | 2015-05-28 | 2016-02-16 | 주식회사 네비엔 | 프리캐스트 콘크리트 슬래브 및 이들의 결합구조 |
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| JP7012715B2 (ja) * | 2016-06-27 | 2022-01-28 | エフ．ホフマン－ラ ロシュ アーゲー | γ－セクレターゼモジュレーターとしてのトリアゾロピリジン |
| EP3481829B1 (en) | 2016-07-08 | 2021-04-07 | H. Hoffnabb-La Roche Ag | Fused pyrimidine derivatives |
| EP3523304B1 (en) | 2016-10-04 | 2021-01-27 | H. Hoffnabb-La Roche Ag | Bicyclic heteroaryl derivatives |
| WO2018087018A1 (en) | 2016-11-08 | 2018-05-17 | F. Hoffmann-La Roche Ag | Phenoxytriazoles |
| US10889553B2 (en) | 2017-12-01 | 2021-01-12 | Nysnobio Ireland Dac | Asymmetric triazole benzamide derivatives and the compositions and methods of treatment regarding the same |
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| CN110194744B (zh) * | 2018-02-26 | 2022-11-11 | 云南大学 | 一种抑制β-淀粉样蛋白生成的化合物及其制备方法和用途 |
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