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
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 |
|---|---|---|---|
| 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 (20)
| Country | Link |
|---|---|
| US (2) | US9145399B2 (es) |
| EP (2) | EP2523949B1 (es) |
| JP (2) | JP5824464B2 (es) |
| KR (2) | KR20120123677A (es) |
| CN (2) | CN102906083A (es) |
| AR (2) | AR079904A1 (es) |
| AU (2) | AU2011206635B2 (es) |
| BR (2) | BR112012017442A2 (es) |
| CA (2) | CA2784765A1 (es) |
| CL (2) | CL2012001956A1 (es) |
| EA (2) | EA022093B1 (es) |
| ES (2) | ES2523977T3 (es) |
| IL (2) | IL220840A (es) |
| MX (2) | MX2012008260A (es) |
| NZ (2) | NZ600648A (es) |
| PE (2) | PE20121512A1 (es) |
| SG (2) | SG182505A1 (es) |
| TW (2) | TWI491608B (es) |
| WO (2) | WO2011086099A1 (es) |
| ZA (2) | ZA201205245B (es) |
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| EP2393804B1 (en) | 2009-02-06 | 2014-04-16 | Janssen Pharmaceuticals, Inc. | Novel substituted bicyclic heterocyclic compounds as gamma secretase modulators |
| US8835482B2 (en) | 2009-05-07 | 2014-09-16 | Janssen Pharmaceuticals, Inc. | Substituted indazole and aza-indazole derivatives as gamma secretase modulators |
| WO2010141796A2 (en) * | 2009-06-05 | 2010-12-09 | Cephalon, Inc. | PREPARATION AND USES OF 1,2,4-TRIAZOLO [1,5a] PYRIDINE DERIVATIVES |
| US8946266B2 (en) | 2009-07-15 | 2015-02-03 | Janssen Pharmaceuticals, Inc. | Substituted triazole and imidazole derivatives as gamma secretase modulators |
| 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 |
| CN102906083A (zh) | 2010-01-15 | 2013-01-30 | 杨森制药公司 | 作为γ分泌酶调节剂的新的取代的三唑衍生物 |
| UY33452A (es) | 2010-06-16 | 2012-01-31 | Bayer Schering Pharma Ag | Triazolopiridinas sustituidas |
| MX2013002198A (es) * | 2010-08-27 | 2013-03-18 | Merck Patent Gmbh | Derivados de triazolopirazina. |
| KR20130139895A (ko) | 2010-09-02 | 2013-12-23 | 다케다 야쿠힌 고교 가부시키가이샤 | 경도인지 장애의 치료 또는 예방용 융합 트리아졸 |
| JP2014508794A (ja) | 2011-03-24 | 2014-04-10 | 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 | γ−セクレターゼ調節剤としての新規な置換トリアゾリルピペラジンおよびトリアゾリルピペラジン誘導体 |
| EA023045B1 (ru) | 2011-07-15 | 2016-04-29 | Янссен Фармасьютикалз, Инк. | Новые замещенные производные индола в качестве модуляторов гамма-секретазы |
| UA112096C2 (uk) | 2011-12-12 | 2016-07-25 | Байєр Інтеллектуал Проперті Гмбх | Заміщені триазолопіридини та їх застосування як інгібіторів ttk |
| WO2013124026A1 (en) * | 2012-02-21 | 2013-08-29 | Merck Patent Gmbh | 8 - substituted 2 -amino - [1,2,4] triazolo [1, 5 -a] pyrazines as syk tryrosine kinase inhibitors and gcn2 serin kinase inhibitors |
| US20150051202A1 (en) * | 2012-03-07 | 2015-02-19 | Merck Patent Gmbh | Triazolopyrazine derivatives |
| EP2825540B1 (en) | 2012-03-14 | 2016-09-14 | Bayer Intellectual Property GmbH | Substituted imidazopyridazines |
| JP6106745B2 (ja) | 2012-05-16 | 2017-04-05 | ヤンセン ファーマシューティカルズ，インコーポレーテッド | （特に）アルツハイマー病の治療に有用な置換３，４−ジヒドロ−２Ｈ−ピリド［１，２−ａ］ピラジン−１，６−ジオン誘導体 |
| 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 |
| CN104918938B (zh) | 2012-12-20 | 2017-08-15 | 詹森药业有限公司 | 新颖的作为γ分泌酶调节剂的三环3，4‑二氢‑2H‑吡啶并[1，2‑a]吡嗪‑1，6‑二酮衍生物 |
| EP2945944B1 (en) | 2013-01-17 | 2016-11-09 | Janssen Pharmaceutica, N.V. | Novel substituted pyrido-piperazinone derivatives as gamma secretase modulators |
| EP3004081B1 (en) * | 2013-06-04 | 2017-11-15 | Acturum Real Estate AB | Triazole compounds and their use 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 |
| US9718805B2 (en) | 2013-06-04 | 2017-08-01 | Acturum Life Science AB | Triazole compounds and their use as gamma secretase modulators |
| CN105377848A (zh) | 2013-06-11 | 2016-03-02 | 拜耳制药股份公司 | 取代的三唑并吡啶的前体药物衍生物 |
| 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 |
| KR20170092634A (ko) | 2014-12-05 | 2017-08-11 | 에이엔2에이치 디스커버리 리미티드 | 파킨 리가제 활성화 방법 및 조성물 |
| 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 |
| WO2017210694A1 (en) * | 2016-06-03 | 2017-12-07 | An2H Discovery Limited | Triazole benzamide derivatives and the compositions and methods of treatment regarding the same |
| WO2018001918A1 (en) * | 2016-06-27 | 2018-01-04 | F. Hoffmann-La Roche Ag | Triazolopyridines as gamma-secretase modulators |
| 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 |
| 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 |
| AR110122A1 (es) | 2016-11-08 | 2019-02-27 | Hoffmann La Roche | Fenoxitriazoles |
| 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 |
| 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 |
| 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 |
| CN114787163A (zh) | 2019-11-29 | 2022-07-22 | 豪夫迈·罗氏有限公司 | 用于制备 (9S)-2-溴-9-(2,3,4-三氟苯基)-6,7,8,9-四氢-5H-[1,2,4]三唑并[1,5-a]氮杂䓬的方法 |
| JP2023553051A (ja) | 2020-12-11 | 2023-12-20 | エフ． ホフマン－ラ ロシュ アーゲー | （９Ｓ）－Ｎ－［３－（６－メチルピリミジン－４－イル）－３－アザビシクロ［３．２．１］オクタン－８－イル］－９－（２，３，４－トリフルオロフェニル）－６，７，８，９－テトラヒドロ－５Ｈ－［１，２，４］トリアゾロ［１，５－ａ］アゼピン－２－アミンの調製のための方法、および、その固体形態 |
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