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)
- Neurology (AREA)
- Neurosurgery (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Biomedical Technology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (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 |
|---|---|---|---|
| PE2012000992A PE20121512A1 (es) | 2010-01-15 | 2011-01-12 | Novedosos derivados de triazol sustituidos como moduladores de la gamma secretasa |
| PE2012000991A PE20121511A1 (es) | 2010-01-15 | 2011-01-12 | Novedosos derivados biciclicos de triazol sustituidos como moduladores de gamma secretasa |
Family Applications After (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) | US9079886B2 (es) |
| EP (2) | EP2523955B1 (es) |
| JP (2) | JP5824464B2 (es) |
| KR (2) | KR20120123677A (es) |
| CN (2) | CN102803261A (es) |
| AR (2) | AR079905A1 (es) |
| AU (2) | AU2011206635B2 (es) |
| BR (2) | BR112012017442A2 (es) |
| CA (2) | CA2784769A1 (es) |
| CL (2) | CL2012001956A1 (es) |
| EA (2) | EA022093B1 (es) |
| ES (2) | ES2523977T3 (es) |
| IL (2) | IL220838A0 (es) |
| MX (2) | MX2012008259A (es) |
| NZ (2) | NZ600648A (es) |
| PE (2) | PE20121512A1 (es) |
| PH (2) | PH12012501381A1 (es) |
| SG (2) | SG182505A1 (es) |
| TW (2) | TWI473807B (es) |
| WO (2) | WO2011086099A1 (es) |
| ZA (2) | ZA201205240B (es) |
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| CN102325765B (zh) | 2009-02-06 | 2014-12-24 | 杨森制药公司 | 作为γ-分泌酶调节剂的取代的双环杂环化合物 |
| CA2755467A1 (en) | 2009-05-07 | 2010-12-23 | Janssen Pharmaceuticals, Inc. | Novel substituted indazole and aza-indazole derivatives as gamma secretase modulators |
| NZ597140A (en) * | 2009-06-05 | 2014-01-31 | Cephalon Inc | Preparation and uses of 1,2,4-triazolo [1,5a] pyridine derivatives |
| BR112012000915A2 (pt) | 2009-07-15 | 2019-09-24 | Janssen Pharmaceuticals Inc | derivados de triazol e imidazol substituídos como moduladores de gama secretase. |
| EP2343297A1 (en) | 2009-11-30 | 2011-07-13 | Bayer Schering Pharma AG | Triazolopyridines |
| EP2343294A1 (en) | 2009-11-30 | 2011-07-13 | Bayer Schering Pharma AG | Substituted triazolopyridines |
| AU2011206635B2 (en) | 2010-01-15 | 2015-01-22 | Cellzome Limited | Novel substituted triazole derivatives as gamma secretase modulators |
| UY33452A (es) | 2010-06-16 | 2012-01-31 | Bayer Schering Pharma Ag | Triazolopiridinas sustituidas |
| AU2011295440B2 (en) | 2010-08-27 | 2015-06-11 | Merck Patent Gmbh | Triazolopyrazine derivatives |
| EP2611805A1 (en) | 2010-09-02 | 2013-07-10 | Takeda Pharmaceutical Company Limited | Fused triazoles for the treatment or prophylaxis of mild cognitive impairment |
| AU2012230348A1 (en) | 2011-03-24 | 2013-08-29 | Cellzome Limited | Novel substituted triazolyl piperazine and triazolyl piperidine derivatives as gamma secretase modulators |
| ES2555167T3 (es) | 2011-07-15 | 2015-12-29 | Janssen Pharmaceuticals, Inc. | Nuevos derivados de indol sustituidos como moduladores de gamma secretasa |
| UA112096C2 (uk) | 2011-12-12 | 2016-07-25 | Байєр Інтеллектуал Проперті Гмбх | Заміщені триазолопіридини та їх застосування як інгібіторів ttk |
| ES2674451T3 (es) * | 2012-02-21 | 2018-06-29 | Merck Patent Gmbh | 2-amino-[1,2,4]triazolo[1,5-a] pirazinas 8-sustituidos como inhibidores de la SYK tirosina quinasa e inhibidores de la serina quinasa GCN2 |
| JP6049768B2 (ja) * | 2012-03-07 | 2016-12-21 | 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 | トリアゾロピラジン誘導体 |
| JP6166289B2 (ja) | 2012-03-14 | 2017-07-19 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ | 置換イミダゾピリダジン |
| CN104583208B (zh) | 2012-05-16 | 2016-09-28 | 杨森制药公司 | 可用于治疗(尤其是)阿尔茨海默病的取代的3,4-二氢-2H-吡啶并[1,2-a]吡嗪-1,6-二酮衍生物 |
| 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 |
| CN107266405A (zh) * | 2012-08-07 | 2017-10-20 | 詹森药业有限公司 | 用于制备c‑fms激酶抑制剂的方法 |
| AU2013366668B2 (en) | 2012-12-20 | 2017-07-20 | Janssen Pharmaceutica Nv | Novel tricyclic 3,4-dihydro-2H-pyrido[1,2-alpha]pyrazine -1,6-dione derivatives as gamma secretase modulators |
| AU2014206834B2 (en) | 2013-01-17 | 2017-06-22 | Janssen Pharmaceutica Nv | Novel substituted pyrido-piperazinone derivatives as gamma secretase modulators |
| DK3004080T3 (da) * | 2013-06-04 | 2019-01-02 | Acturum Real Estate Ab | Triazolforbindelser og deres anvendelse som gamma-sekretase-modulatorer |
| WO2014195323A1 (en) | 2013-06-04 | 2014-12-11 | Acturum Life Science AB | Pyrimidine compounds and their use as gamma secretase modulators |
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| PE20160156A1 (es) | 2013-06-11 | 2016-04-20 | Bayer Pharma AG | Derivados de prodroga de triazolpiridinas sustituidas |
| 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 |
| WO2016090371A2 (en) | 2014-12-05 | 2016-06-09 | An2H Discovery Limited | Parkin ligase activation methods and compositions |
| KR101594470B1 (ko) | 2015-05-28 | 2016-02-16 | 주식회사 네비엔 | 프리캐스트 콘크리트 슬래브 및 이들의 결합구조 |
| KR101710943B1 (ko) | 2016-05-13 | 2017-02-28 | 강태성 | 구조물용 피씨 데크 슬래브 및 이의 제조방법 |
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| EP3481829B1 (en) | 2016-07-08 | 2021-04-07 | H. Hoffnabb-La Roche Ag | Fused pyrimidine derivatives |
| CN109476670B (zh) * | 2016-10-04 | 2022-06-28 | 豪夫迈·罗氏有限公司 | 二环杂芳基衍生物 |
| CN109790149B (zh) * | 2016-11-08 | 2022-05-17 | 豪夫迈·罗氏有限公司 | 苯氧基三唑类化合物 |
| 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 |
| CN110194743B (zh) * | 2018-02-26 | 2022-11-11 | 云南大学 | 苯基(3-甲氧基-4-(4-甲基-1h-咪唑-1-基)苯基)甲酮类化合物 |
| 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 |
| CN110194746B (zh) * | 2018-02-26 | 2022-11-18 | 云南大学 | 用于治疗阿尔茨海默症的化合物，其制备方法和用途 |
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